Author: Pankaj Saha

Top 10 Best Pharma Companies in Hyderabad

Do you want the list of the top 10 best pharma companies in Hyderabad? Then you are at the right place. There are so many pharma companies in Hyderabad but from that huge list, we are introducing you to some Best pharma Companies in Hyderabad. Here you can get a Company Description, Ghete Products list, address, website, and contact details about pharma companies in Hyderabad.

Table of Contents

Introduction

Before telling about the Top 10 MNC Pharma companies which are in Hyderabad we have created a table of the Top 10 companies according to their company’s total revenue. Here in the table, we have listed the company name, their website so you can check out if they are recruiting. We have also shared their Phone numbers so if you have any queries you can directly reach them via a Phone call.

Company Name	Website	Contact	Revenue (INR)
Aurobindo Pharma Limited	www.aurobindo.com	+91 (40) 6672 1200	23,290 Crores
Hetero Drugs Limited	www.heteroworld.com	+91 (40) 23704923 / 24 / 25	1385 crores
Glochem industries limited	www.glochemindia.com	+91 (40) 3921 9900	Approx 800 crores
Divi’s Laboratories Ltd	www.divislabs.com	+91 (40) 6696 6300 / +91 (40) 2378 6300	5,584.05 crores
Novartis India Ltd	www.novartis.in	–	4,382.5 crores
Natco Pharma Ltd	www.natcopharma.co.in	+91 (40) 2354 7532 / +91 (40) 2354 5298 / +91 (40) 2354 8243	355.2 Crores
Lee Pharma Ltd	www.leepharma.com	+91 (40) 2377 0338 / +91 (40) 2377 0339	Above 100 crores
Rakshit Drugs Pvt Ltd	www.rakshitdrugspvtltd.com	+91 (40) 2381 0385 / +91 (40) 2381 2709	Approx 100 crores
SMS Pharmaceuticals Ltd	www.smspharma.com	+91 (40) 2525 9999 / +91 (40) 3535 9999	149.72 Crores
Dr Reddy’s Laboratories	www.drreddys.com	1800 425 0014 / +91 (40) 4900 2222	17,460 Crores

Aurobindo Pharma Ltd.

Aurobindo Pharma was established in 1986 by Mr. P. V. Ramprasad Reddy, Mr. K. Nityananda Reddy and their small group. Aurobindo Pharma Ltd. is a reputed company in the Pharmaceutical industry of Hyderabad, Telangana. Their Headquarter is located in Hyderabad.

Aurobindo Pharma Ltd. serves in 150 plus markets all over the world, with 25 manufacturing facilities that collaborates with 20000 plus employees. Aurobindo Pharma Ltd has 26 Billion plus diverse dosage forms.

In 1992, Aurobindo Pharma Ltd became a public company. In 1995, Aurobindo Pharma Ltd shares were listed on Indian Stock Exchange.

Products:

Amoxil
Norco
Maxalt

Website: www.aurobindo.com

Phone No: +91 (40) 6672 1200

Fax Details: +91 (40) 2374 1080 / +91 (40) 2374 6833

Email: info@aurobindo.com

Address:

Aurobindo Pharma Limited,

Plot no 2, Maitrivihar,

Ameerpet,

Hyderabad, – 500038

Telangana, India.

Hetero Drugs Ltd.

Hetero Drugs Ltd was established in 1993. Hetero Drugs are in news because of the Hetero’s Covifor ™ (Remedesivir). Hetero works on production of remedecivir injections that are applied in Covid-19 treatment.

Hetero Drugs Ltd presence in 126 plus countries globally with 300+ products from therapeutic categories such as HIV/AIDS, Oncology, Cardiovascular, Neurology, Hepatitis, Nephrology, etc.

Hetero Drugs Ltd has 36 manufacturing units all over the world with 21,000 employee.

Products:

Favivir
Covifor ™ (Remedesivir)
Amlodipine besylate
Linezolid
Valganciclovir

Website: www.heteroworld.com

Phone No: +91 (40) 23704923 / 24 / 25

Address:

7-2-A2, Hetero Corporate,

Industrial Estates, Sanath Nagar,

Hyderabad – 500018,

Telangana, INDIA

Glochem Industries Limited

Glochem Industries Private Limited was started in 1996. Glochem is one of the fastest growing pharmaceutical company in India. Their headquarter is located in Hyderabad, Telangana.

Glochem works worldwide. They manufacture the pharmaceutical products and also sell them in various countries rather than India like the USA, UK, Japan, Middle East Countries, Korea, Bangladesh, etc.

Products :

Amlodipine Maleate
Cetirizine Dihydrochloride
Levocetirizine Dihydrochloride

Website: www.glochemindia.com

Phone No: +91 (40) 3921 9900

Address:

Glochem Industries Limited, G V Chamber, 7-2-C8 & C8/2, IE Sanath Nagar, Hyderabad – 500018, State Telangana, India.

Divis Laboratories Ltd

Divis were established in 1990. They have two manufacturing units in India. Divi’s Laboratories Ltd is the premier company in the API sector, they work with so many MultiNational Companies and international companies by delivering them API formulations.

In the pharmaceutical industry, Divis has been working for 30 years. They have 2 R&D labs and also have 2 manufacturing units. Divis works with 14000 employees.

Products:

Capecitabine
Iopamidol
Dextromethorphan
Niacin

Website: www.divislabs.com

Phone No: +91 (40) 6696 6300 / +91 (40) 2378 6300

Fax Details: +91 (40) 2378 6460

Address :

Divis Labs Ltd., 1-72/23 (P)/ Divis/ 303, Divis Towers, Cyber Hills, Gachibowli, Hyderabad – 500032, Telangana, India.

Novartis India Ltd.

Novartis India Ltd is the multinational pharmaceutical company located in Hyderabad. Novartis was established in 1996.

In capitalization and sales of pharmaceutical drugs, Novartis is among the top companies in the world.

Novartis India Ltd is working in 155 countries all over the world with their Pharma services.

Products:

Galvus
Tafinlar
Xolair

Website: www.novartis.in

Address:

Salarpuria- sattva Knowledge City,

Inorbit Mall Road,

Durgam Cheruvu Road,

Hi-tech City, Hyderabad – 500081

Telangana, India.

Natco Pharma Limited

Natco Pharma Limited was started in Hyderabad in 1981. Their initial investment was 3.3 million INR with a single unit of 20 employees. Natco has 7 manufacturing units all over India.

Products:

Hepcinat
Dabigatran
Galtiramer
Liposomal doxorubicin

Website: www.natcopharma.co.in / www.nactopharma.com

Phone No: +91 (40) 2354 7532 / +91 (40) 2354 5298 / +91 (40) 2354 8243

Address:

Natco Pharma Ltd,

Natco House,

Road No 2, Banjara Hills,

Hyderabad – 500034

Telangana, India.

Lee Pharma Limited

In 1997, Lee Pharma was established in India. They are among those companies who work to develop cost effectiveness and quality products, for easy availability for needy peoples at affordable prices.

Lee Pharma Ltd is globally connected with popular companies like Mylan, Cipla, Alkem , etc.

Product:

Apixaban
Aspirin
Voriconazole
Azithromycin

Website: www.leepharma.com

Phone No: +91 (40) 2377 0338 / +91 (40) 2377 0339

Fax Details : +91 (40) 6617 0330

Email: info@leepharma.com

Address:

Lee Pharma Ltd,

SY. No. : 257 & 258/1, Door No. 11-6/ 56-C,

Opp to IDPL Factory, Moosapet,

Balanagar (Post),

Hyderabad – 500037,

Telangana, India.

Rakshit Drugs Private Limited

Rakshit Drugs Pvt Ltd was established in 2000. They are new among all Pharma Companies but they emerged as dependable and strong manufacturers of APIs and Intermediates.

Rakshit has 3 plants over Andra Pradesh and Telangana. They supply their products all over the world to the United States, Europe, Japan, Asia and Latin America Countries.

Products:

Sildenafil Citrate
Azathioprine
Mycophenolate Mofetil
Valganciclovir

Website: www.rakshitdrugspvtltd.com

Phone No: +91 (40) 2381 0385 / +91 (40) 2381 2709

Email: rajeshjoshi@rakshitdrugspvtltd.com

Address:

Rakshit Drugs Private Limited,

Plot 425/ 3RT, SR Nagar,

Hyderabad – 500038,

Telangana, India.

SMS Pharmaceuticals Ltd.

SMS pharmaceuticals Ltd started in 1990 with a single production unit. Now they own 4 multi production plants and 2 research and development centers in India.

SMS Pharmaceuticals Ltd working with presence along 70 countries all over the world. They also work on Developing a low cost non infringing process.

Products:

Almotriptan Malate
Zolmitriptan
Vildagliptin
Ranolazine
Penciclovir

Website: www.smspharma.com

Phone No: +91 (40) 2525 9999 / +91 (40) 3535 9999

Fax Details: +91 (40) 2525 9889

Email: info@smspharma.com

Address:

Plot No 72, H No 8-2-334/3 & 4,

Road No 5, Banjara Hills,

Opposite to SBI executive Enclave,

Hyderabad – 500034,

Telangana, India.

Dr Reddy’s Laboratories

In 1984, one scientist & entrepreneur Dr K Anji Reddy established Dr Reddy’s Laboratories.

In covid period they collaborated with Japan’s Fujifilm and Global Response aid to produce and distribute Avigan (Favipiravir) and they also get licensing rights for Redyx (Remdesivir) along 127 countries.

Products:

Avigan
Redyx ™ (Remdesivir)

Website: www.drreddys.com

Phone no: 1800 425 0014 / +91 (40) 4900 2222

Email: customerservices@drreddys.com

Address:

8-2-337, Banjara Hills, Road No 3,

SBI Executive Enclave,

Green Valley, Banjara Hills,

Hyderabad – 500034

Telangana, India.

Other Pharma Companies of Hydrabad

Some other pharma companies in Hyderabad are listed below:

Gland Pharma Limited

Address: Gandi Maisamma, Hyderabad, Telangana 500043

Phone No: +91 (40) 6662 1010

Website: www.glandpharma.com

Ammana Bio Pharma Limited

Address: 1-7-297/18, Above Godrej Showroom 125, M.G. Road, Kalasiguda, Secunderabad, Telangana 500003

Phone no: +91 (40) 2784 0777

Website: Not Available

Shri Krishna Pharmaceuticals

Address: C-4, industrial area, Uppal, Hyderabad, Telangana 500039

Phone No: +91 (40) 2720 3264

Website: www.shrikrishnapharma.com

Qualitek Pharma

Address: Plot no 115,Jeedimetla Industrial Area, Phase -V Extn, Doolapally Village, Quath Bullapur Mandal, Jeedimetla, Hyderabad, Telangana 500072

Phone No: +91 (40) 6598 7518

Website: www.qualitekpharma.com

Vista Pharmaceuticals Limited

Address: 7-1-212/A/70, Plot No 85, ShivBagh, Ameerpet, Hyderabad, Telangana 500016

Phone No: +91 (40) 6558 1585

Website: www.vistapharmaceuticals.com

Vance & Health Pharmaceutical Pvt. Ltd.

Address: 201, Rama Residency, H.No. 7-1-414, Srinivasa Nagar (east), Sanjeeva Reddy Nagar, Ameerpet, Hyderabad, Telangana 500038

Phone no : +91 (40) 2373 6533

Website: www.vancehealth.com

Mars Therapeutics & Chemicals Limited

Address: 8-290/1, Old Airport Rd, Ferozguda, Secunderabad, Telangana 500011

Phone no : +91 (40) 2795 9226

Website: www.marspharma.com

Therdose Pharma Private Limited

Address: Shop No.7-1-62/28/B, 3rd Floor, Behind Umesh, Beside Andhra Bank, Sanjeeva Reddy Nagar Office Area, Sanjeeva Reddy Nagar, Hyderabad, Telangana 500038

Phone no : +91 (40) 4261 2731

Website: www.therdose.com

Smilax Laboratories Limited

Address: Plot No. 12/A, Unit-I, Phase-III, IDA, Jeedimetla, Hyderabad, Telangana 500055

Phone no : +91 (40) 2309 0260

Website: www.smilaxlabs.com

Kopalle Pharma Chemicals Pvt Ltd

Address: D-133,130,127,124, Road No: 43,Phase-3, IDA Jeedimetla, Jeedimetla, Hyderabad, Telangana 500055

Phone no : +91 (40) 2309 5412

Website: www.kopalle.in

Emmennar Pharma Pvt Ltd

Address: Survey no 10,IDA, Gaddapotharam, Telangana 502319

Phone no: +91 92465 41687

Website: www.emmennar.com

Pellets Pharma Ltd

Address: Isnapur-Indira Karan Rd, IDA Pashamylaram, Hyderabad, Telangana 502329

Phone no : +91 91563 35508

Website: www.pelletspharma.com

Leiutis Pharmaceuticals

Address: Leiutis pharmaceuticals, TIE 1st Phase, VSR Complex, 23, Industrial Development Area Road, Hyderabad, Telangana 500037

Phone no: +91 (40) 2307 7773

Website: www.leiutis.com

Aristo Pharmaceuticals Pvt. Ltd.

Address: 6-3-629, Anand Nagar, Khairatabad, Hyderabad, Telangana 500004

Phone no : +91 (40) 2331 6117

Website: www.aristopharma.org

Hi-Tech Pharmaceuticals

Address: SivaSaiSannidhi Apartment, Plot No 102, 1st Floor, Opposite Saibaba Temple, Dwarkapuri colony,Hindi Nagar, Panjagutta,Pin-500082

Website: www.hi-techpharma.com

Biophore

Address: Biophore India Pharmaceuticals Pvt. Ltd. 1-98/2/92, Plot Number 92, Phase II, 500033, Kavuri Hills, Jubilee Hills, Hyderabad, Telangana

Phone no: +91 (40) 4747 4545

Website: www.biophore.com

Granules India Ltd.

Address: Pragathi Nagar Rd, ALEAP Industrial Area, Gajularamaram, Hyderabad, Telangana 500090

Phone no: +91 (40) 3066 0000

Website: www.granulesindia.com

Accrete Pharmaceutical Pvt ltd

Address: Habsiguda, Secunderabad, Telangana 500013

Phone no: +91 (40) 2717 9878

Website: www.accretepharma.com

Optimus Generics Ltd

Address: Ambatapur, Telangana 509301

Phone no : +91 (40) 3921 9900

Website: www.evertogen.com

Neuland Laboratories Ltd

Address: Road Number 2, Banjara Hills, Hyderabad, Telangana

Phone no: +91 (40) 3021 1669

Website: www.neulandlabs.com

DRL

Address: Bachupally, Ranga Reddy, Hyderabad, Telangana 500090

Phone no : +91 (40) 4434 6200

Website: www.drreddys.com

June 3, 2021

Anti Hyperlipidemic Drugs Free Pharmacology Note – 2021
Anti Hyperlipidemic drugs are used to lower the levels of lipids and lipoproteins in the blood. Some examples of antihyperlipidemic are Atorvastatin, Rosuvastatin, Colestipol, Fenofibrate, Omega-3 fatty acids, etc. In this note, we will learn about the Classification of Anti Hyperlipidemic Drugs, Mechanism of Action, Adverse Effects, Therapeutic Effects, and Drug Interactions. For more study notes keep visiting MyPharmaGuide.

Introduction of Anti Hyperlipidemic Drugs

The hypolipidaemic drugs have attracted considerable attention because of their potential to prevent cardiovascular disease by retarding the accelerated atherosclerosis in hyperlipidaemic individuals.

Lipids or fats, which are usually transported in various combinations with proteins (lipoproteins), play a key role in cardiovascular disorders. Lipids, including cholesterol and triglycerides, are essential elements in the body. They are synthesized in the liver; therefore, they can never be eliminated from the body. Anti Hyperlipidemic Drugs are the group of drugs prescribed in adjuvant therapy to reduce elevated cholesterol levels in patients with high cholesterol and LDL levels in the blood

Classification of Anti Hyperlipidemic Drugs

Antihyperlipidemics are classified between the following types:
- HMG-CoA reductase inhibitors (Statins): Lovastatin, Simvastatin, Pravastatin, and Atorvastatin.
- Bile Acid Sequestrants (Resins): Cholestyramine and Colestipol
- Fibric Acid Derivatives (Fibrates): Clofibrate, Gemfibrozil, Bezafibrate, and Fenofibrate.
- Triglyceride Synthesis and Lipolysis Inhibitors: Nicotinic acid
- Others: Probucol and Omega-3 fatty acids
Anti Hyperlipidemic Drugs Free Pharmacology Note – 2021

HMG-CoA Reductase Inhibitors (Statins)

Statins are the most effective and best-tolerated agents used to treat hyperlipidemia. Statins are competitive inhibitors of 3 -hydroxy-3-methylglutarylcoenzyme reductase and also the most effective and best-tolerated agents for treating hyperlipidemia. They catalyze an early, rate-limiting step in cholesterol biosynthesis. Higher doses are more potent and can even reduce the triglyceride levels caused by high VLDL levels.

Mechanism of Action
- Statins are the most potent LDL reducers.
- They are structural analogs of HMG-CoA
- Statins competitively inhibit the HMG-CoA reductase enzyme
- Statins block the rate-limiting step in hepatic cholesterol synthesis (conversion of hydroxymethyl glutaryl coenzyme A (HMG-CoA) to mevalonate by HMG-CoA reductase)
- Low intracellular cholesterol stimulates the synthesis of LDL receptors
- Promote uptake of LDL from the blood
- Low intracellular cholesterol decrease the secretion of VLDL to the blood
- Statins have direct anti-atherosclerotic effects and have been shown to prevent bone loss
Mechanism of Action of Statins

Therapeutic Uses

Therapeutics uses of Statins are given below:
- Statins are used for secondary prevention of myocardial infarction and stroke in patients having the symptomatic atherosclerotic disease (e.g., angina, transient ischemic attacks, following acute myocardial infarction or stroke).
- They are used for the primary prevention of arterial disease in patients having high risk due to increased serum cholesterol concentration, specifically when there are other risk factors for atherosclerosis.
- Serum cholesterol levels can be lowered by atorvastatin in patients with homozygous familial hypercholesterolemia.
- A bile acid-binding resin is added to treatment with a statin in cases of severe drug-resistant dyslipidemia (e.g., heterozygous familial hypercholesterolemia).
Adverse Effects

All statins are remarkably well tolerated; the overall incidence of side effects not differing from placebo. Notable side effects are: Gastrointestinal complaints and headaches are usually mild. Rashes and sleep disturbances are uncommon. The rise in serum transaminase can occur, but liver damage is rare. Monitoring of liver function is recommended.

Individual Drugs

Atorvastatin: This newer and most popular statin is more potent and appears to have the highest LDL-CH lowering efficacy at a maximal daily dose of 80 mg. At this dose, a greater reduction in TGs is noted if the same was raised at baseline. Atorvastatin has a much longer plasma t½ of 18– 24 hr than other statins and has additional antioxidant property.

Lovastatin: It is the first clinically used statin; is lipophilic and given orally in the precursor lactone form. Absorption is incomplete and first-pass metabolism is extensive. Metabolites are excreted mainly in bile. The t½ is short (1–4 hours).

Simvastatin: It is twice as potent as lovastatin; also more efficacious. A greater rise in HDLCH (when low) has been noted with simvastatin than lovastatin or pravastatin. Like lovastatin, it is lipophilic and given in the lactone precursor form. Oral absorption is better and first-pass metabolism extensive; t½ is 2–3 hr.

Bile Acid Sequestrants (Resins)

Mechanism of Action

Bile acid sequestrants are polymeric compounds that act as ion exchange resins. They exchange anions (like Cl− ions) for bile acids by binding with bile acid and sequestering them from enterohepatic circulation. They are not well-absorbed from the gut into the bloodstream because they have large polymeric structures. Therefore, the bile acid sequestrants along with the bile acid bound to the drug, are excreted via feces after passing through the gastrointestinal tract.

Therapeutic Uses
- Bile acid sequestrants are used for the treatment of hypercholesterolemia and dyslipidemia as they help in decreasing cholesterol levels.
- For patients with chronic liver diseases, bile acid sequestrants may be used for the prevention of pruritus.
- They are also used in the treatment of diarrhea caused by excess bile salts entering the colon rather than being absorbed in the end of the small intestine.
Adverse Effects

Bile acid sequestrants do not have any systemic side effects because they are designed to stay in the gut. However, they may cause problems like constipation, diarrhea, and flatulence in the gastrointestinal tract.

Individual Drug

Cholestyramine: Cholestyramine acts by preventing the reabsorption of bile in the gastrointestinal tract. It binds to bile as it is a strong anion exchange resin that can exchange its chloride anions with anionic bile acids in the GIT and bind them in the resin matrix strongly.

Fibric Acid Derivatives (Fibrates)

The fibrates (isobutyric acid derivatives) primarily activate lipoprotein lipase which is a key enzyme in the degradation of VLDL resulting in lowering of circulating TGs.

Mechanism of Action

The mechanism of action of fibrates is not completely understood but it is believed that they increase peripheral clearance and reduce hepatic triglyceride synthesis. The effects given by fibrates on blood lipids depend on their binding to Peroxisome Proliferators Activator Receptors (PPARs), which regulate gene transcription. alpha, beta, and gamma are the three PPAR isotopes
that have been identified. Fibrates act as agonists for the nuclear transcription factor Peroxisome Proliferators-Activated Receptor-alpha (PPAR-alpha), at the molecular level.
This mechanism is used by fibrates for the downregulation of the apolipoprotein C-III (apo C-III) gene and up-regulation of the genes for apolipoprotein A -I (apo A-I), fatty acid transport protein, fatty acid oxidation, and LPL. Thus, VLDL triglycerides get reduced due to the enhanced catabolism of triglycerides by LPL along with enhanced fatty acid oxidation.

Therapeutic Uses

Therapeutic uses of fibrates are given in the below list
- Fibrates (gemfibrozil) are the first -line of drugs for patients with type III hyperlipidemia or familial dysbetalipoproteinemia.
- They are used to treat mixed hyperlipidemia, wherein the predominant abnormality is hypertriglyceridemia (in combination with resins), and to treat moderate to severe hypertriglyceridemia.
- They are used with statins in patients with a high risk of CHD and mixed hyperlipidemia. But because of the increased risk of myopathy, careful safety monitoring is required.
Adverse Effects

Generally, fibrates do not give any adverse reaction and are well-tolerated in most patients. But in some patients, minor side -effects like GI disturbance symptoms like abdominal pain, diarrhea, and nausea may be seen that are corrected by the discontinuation of the treatment.
An important but rare adverse effect of fibrates is myositis with muscle pain and tenderness and elevated creatinine kinase levels. Fibrates are contraindicated in patients with renal dysfunction, as they get accumulated in the kidney leading to the enhanced frequency of adverse effects
specially myositis.

Individual Drugs

Clofibrate: Clofibrate enhances lipoprotein triglyceride lipolysis by increasing the activity
of extrahepatic Lipoprotein Lipase (LL). Degradation of chylomicrons converts VLDLs to LDLs, which are further converted into HD Ls. These changes occur by a minor increase in the secretion of lipids into bile and finally in the intestine.

Triglyceride Synthesis and Lipolysis Inhibitors

Nicotinic Acid (Niacin)

Nicotinic acid is an organic compound that belongs to the pyridine carboxylic acids group of compounds. At high concentrations, this drug gives cholesterol and triglyceride-lowering effects, resulting in a decrease of LDLs and VLDLs and an increase in HDLs.

Mechanism Of Action

Nicotinic acid helps in the inhibition of the release of free fatty acids from adipose tissue and enhances lipoprotein activity. It results in an increased rate of triglyceride removal from plasma. These actions decrease the total LDL (bad cholesterol) and triglyceride levels, causing increased HDLs (good cholesterol).

Therapeutic Uses

Nicotinic acid is not used therapeutically due to its side effects but sometimes can be prescribed as an adjunct to diet for treatment of high serum triglyceride levels in adult patients who have a risk of pancreatitis, and who do not respond properly to dietary control.

Adverse Effects

The major adverse effects of nicotinic acid are headache, anxiety, hypotension, dry skin, flushing or burning of the skin, peptic ulcer, and abnormal liver function tests.
Other mild adverse effects are hyperuricemia, glucose intolerance, nausea, vomiting, diarrhea, hyperglycemia, and elevated plasma uric acid.

Probucol

It helps in the reduction of LDL and HDL levels, but shows minute effects on serum-triglyceride or VLDL cholesterol levels.

Mechanism of Action

Probucol acts by increasing the fractional rate of LDL catabolism in the final metabolic pathway for cholesterol elimination from the body. This results in the reduction of serum cholesterol level s. It can also inhibit the early stages of cholesterol biosynthesis and slightly inhibit dietary
cholesterol absorption. According to recent studies, probucol can also control atherogenesis as it may inhibit the oxidation and tissue deposition of LDL cholesterol.

Therapeutic Uses
Probucol is used to lower LDL and HDL cholesterol levels.

Adverse Effects
The common adverse effects of probucol are dizziness or fainting and fast or irregular heartbeat.
Some rarely occurring adverse effects are swellings on the face, hands, or feet, or in the mouth, unusual bleeding or bruising, and unusual tiredness or weakness.

Other Anti Hyperlipidemic Drugs

Some rarely used anti hyperlipidemic drugs are omega-3 fatty acids (fish oils).

Mechanism Of Action

Hepatic VLDL triglyceride synthesis is reduced by omega -3 fatty acids, thus, reducing the plasma triglyceride levels. Secretion of VLDL apo B is reduced at high doses of omega -3 fatty acids. The triglyceride levels are reduced at low doses of omega -3 fatty acids, but LDL cholesterol levels may rise due to the conversion of VLDL to LDL -HDL cholesterol. Because of the decrease in thromboxane synthesis, fish oils also have antiplatelet aggregatory activity.
Plasma fibrinogen levels are also reduced.

Adverse Effects

The most common side effect of fish oils is nausea. However, their long-term use
has no obvious side effect.

Therapeutic Uses

Therapeutic uses are listed below:
- Fish oils, available as gelatin capsules are used in severe hypertriglyceridemia along with fibrates.
- Fish oils along with statins (LDL-C may increase during monotherapy, thus they should not be used alone) are helpful in patients having mixed hyperlipidemia with a slight increase in triglycerides.
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May 1, 2021

Antiarrhythmic Drugs Free Pharmacology Note – 2021

Antiarrhythmic Drugs are used to treat Arrhythmia. Arrhythmia is a problem with the rate or rhythm of the heartbeat. During an arrhythmia, the heart can beat too fast, too slow, or with an irregular rhythm. In this Note, we are going to discuss Classification, Mechanism of Action, Adverse effect, therapeutic effect, and drug interactions of Antiarrhythmic drugs.

What is Arrhythmia and What is Antiarrhythmic Drugs ?

Arrhythmia is a common disorder of cardiac excitation. During an arrhythmia, the heart can beat too fast, too slow, or with an irregular rhythm. A heartbeat that is too fast is called tachycardia and A heartbeat that is too slow is called bradycardia.

There are four types of Arrhythmia and they are

Atrial fibrillation,
Bradycardia
Tachycardia
Ventricular arrhythmia

Symptoms of Arrhythmia includes

Shortness of breath
Feeling tired or light-headed
Rapid thumping in chest or palpitations
Chest pain
Losing consciousness

Antiarrhythmic drugs are used to control or correct cardiac rhythm. The ultimate goal of antiarrhythmic drug therapy is to restore normal rhythm and conduction. When it is not possible to revert to normal sinus rhythm, drugs may be used to prevent more serious and possibly l lethal arrhythmias from occurring. Antiarrhythmic drugs are used to: decrease or increase conduction velocity, alter the excitability of cardiac cells by changing the duration of the effective refractory period, suppress abnormal automaticity

Classifications of Antiarrhythmatics

The classification of these drugs are given in the below table

Class	Mechanism	Example
I. Sodium Channel Blockers	Reduce phase 0 slope and peak of action potential.
IA. Moderate	A moderate reduction in phase 0 slope; increase APD; increase ERP	Quinidine, Procainamide
IB. Weak	A small reduction in phase 0 slope; reduce APD; decrease ERP.	Lidocaine, Phenytoin
IC. Strong	Pronounced reduction in phase 0 slope; no effect on APD or ERP	Flecainide, Flecainide
II. β-Blockers	Block sympathetic activity; reduce rate and conduction.	Propranolol and Metoprolol
III. Potassium Channel Blocker	Delay repolarisation (phase 3) and thereby increase action potential duration and effective refractory period	Amiodaron and Bretylium.
IV. Calcium Channel Blockers	Block L-type calcium -channels; most effective at SA and AV nodes; reduce the rate and conduction	Verapamil, Diltiazem, and Nifedipine

Classes of Antiarrhythmic Drugs

Antiarrhythmic Drugs – Sodium Channel Blockers

Sodium channel blockers are the most widely used antiarrhythmic agents. They
act by blocking myocardial Na+ion channels. They are mainly used for the
treatment of supraventricular, nodal, and ventricular arrhythmias, especially after
MI and DC shock.

Mechanism of Action

Antiarrhythmic activity of sodium channel blockers is due to:

A decrease in the inflow of sodium during phase 0 slows the maximum rate of depolarisation
Decrease in excitability and conduction velocity
Prolongation of the effective refractory period
Decrease in the slope of phase 4 spontaneous depolarization (automaticity).

Therapeutic Uses

Therapeutic uses of the Sodium Channel Blockers are given below:

Treatment of supraventricular, nodal, and ventricular arrhythmias, especially after MI and DC shock.
After treatment of atrial flutter and fibrillation to maintain sinus rhythm.

Adverse Effect

The adverse effects of sodium channel blockers are marked depression of AV conduction, hypotension, bradycardia, anorexia, nausea, and vomiting.

Moderate (Class IA)

These drugs slow the rate of rising of action potential and prolong the duration of the action potential. They block Na+ ion channels and prolong the repolarisation time.

Quinidine: Quinidine binds to open and inactivated Na+ ion channels to prevent the influx of Na+ ions; thus slowing down the rapid upstroke during phase 0. It also reduces the slope of phase 4 spontaneous depolarisation and inhibits potassium channels. These actions result in
slow conduction velocity and increased refractoriness.

Procainamide: Procainamide stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action.

Weak (Class IB)

The characteristic effects of these drugs are reduced rate of rising of action potential and reduced or unchanged APD ( Action Potential Duration). The drugs of Class IB rapidly associate and dissociate from the sodium channels. Thus, their actions are manifested when the cardiac cells are depolarised or firing rapidly.

Lidocaine: It is a local anesthetic that shortens phase 3 repolarisation and decreases the duration of action potential . Lidocaine is useful in treating ventricular arrhythmias. It was the drug of choice for the emergency treatment of cardiac arrhythmias. It does not slow down conduction, thus has a little effect on the AV junction arrhythmia. Lidocaine in higher doses causes cardiac and CNS manifestations. SA nodal arrest and hypotension may also occur. Paraesthesia, tremor (facial twitching), vomiting, lightheadedness, slurred speech, and convulsions also occur commonly.

Phenytoin: It is an antiepileptic drug used in tonic-clonic seizures. It
produces unique cardiac electrophysiological effects, thus is used in digoxin-induced arrhythmia.

Strong (Class IC)

Drugs of this class are powerful blockers of fast Na +
ion channels, and thus reduce upstroke of AP in normal and diseased myocardium. There is delayed inactivation of slow Na+ ion channels during the downslope of AP, and this results in the prolongation of APD. In addition, there is inhibition of delayed rectifier K+ current (less K +
efflux), so the APD is prolonged in His Bundle and Purkinje fiber system.

Flecainide: It blocks Na+ and K+ ion channels in normal and ischemic myocardium, thus slowing down the recovery of blocked Na+ ion channels. It further slows down the conduction of electrical impulses in the heart, i.e., reduces excitability.

Propafenone: It blocks fast Na+ ion channels and gives a mild βblocking action (1/10 of propranolol) and class -IV action (Ca ++ ion channel blockage). QT interval does not change but QRS and PR intervals are prolonged. It is effective orally and is metabolized by CYP 2D6 (in persons with CYP 2D6 deficiency, it is slowly metabolized).

Antiarrhythmic Drugs – β -Blockers

The β-blockers or β-adrenergic receptor blockers produce some important electrophysiological effects. They are highly effective in arrhythmias in which excess catecholamine plays a role after MI, CHF, pheochromocytoma, anxiety, anesthesia and postoperative period, exercise, and mitral valve prolapse. Excess of cAMP is considered to be responsible for causing ischemia induced
ventricular fibrillation.

Mechanism of Action

Reduction in intracellular Ca ++ ions leads to reduced phase 2 of AP. There is a reduction in SA nodal automaticity, slowing of conduction, and prolongation of ERP (Effective Refractive Period ) in the AV node. They counteract catecholamine-induced after depolarisations (arrhythmias) by reducing cAMP and Ca ++ ion accumulation.
Beta-blockers are also effective prophylactically in suppressing supraventricular tachycardia because they suppress the automaticity of ectopic foci and slow AV nodal conduction, thereby reducing ventricular response in atrial fibrillation. They reduce cardiac contractility and blood pressure.

Therapeutic Uses

At present beta-blockers are considered to be better antiarrhythmic agents because they improve survival, have a broader spectrum of antiarrhythmic action, and are comparatively safer. In addition , they act synergistically with many other antiarrhythmic agents reducing their arrhythmogenic potential.

Adverse Effect

Some common adverse effects of β-blockers are:

Worsening of CHF
Bronchospasm
Cardiac conduction blocks
Bradycardia
Peripheral vasospasm
Insomnia
Hypotension

Antiarrhythmic Drugs – Potassium Channel Blockers

Class III agents block K+ ion channels, thus the outward potassium current during
re-polarisation of cardiac cells diminishes. These agents prolong the duration of action potential without altering phase 0 of depolarisation or the resting membrane potential. They prolong the effective refractory period and increase refractoriness. All class III drugs have the potential to induce arrhythmias.

Mechanism of Action

Blocking of K+ ion channels in phase 3 of the action potential reduce the efflux
of K+ ions from the myocyte; thus slowing down the repolarisation rate of the
cell and increasing the length of the plateau phase of the action potential. These
actions result in an increase of the refractory period of atrial, ventricular and
Purkinje cells as well as the increase of the QT interval.

Therapeutic Uses

Potassium channel blockers are used to treat:

Recurrent ventricular fibrillation
Unstable ventricular tachycardia
Atrial fibrillation

Adverse Effects

Common adverse effects of potassium channel blockers are pulmonary fibrosis, photosensitivity, corneal micro-deposits, hypothyroidism, and peripheral neuropathy, AV block, bradycardia, ventricular arrhythmia s, bronchospasm, and severe hypotension.

Antiarrhythmic Drugs – Calcium Channel Blockers

The drugs included in CCBs are verapamil, diltiazem, and bepridil (blocks Na+ ion channels also).

Mechanism of Action

CCBs block the slow in ward calcium channels, and slow down the conduction
through the AV node

Therapeutic Uses

CCBs are used to treat atrial fibrillation and flutter, prinzmetal and variant angina
and unstable or chronic stable angina pectoris, and hypertension.

Adverse Effects

CCBs give rise to dizziness, hypotension, bradycardia, edema, constipation, AV
block, ventricular systole, ventricular fibrillation, and nausea.

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April 28, 2021

Antianginal Drugs Free Pharmacology Notes – 2021
Antianginal drugs are used to treat Angina Pectoris (chest pain) which is a symptom of ischemic heart disease. Due to anigina pectoris heart do no get the required amount of oxygen and nutrients and fails to work to properly. In this Note, we will learn about the Classification, Mechanism of Action, Adverse Effects, Advantages and Drug Interection of antianginal drugs.

Antianginal Drugs Free Pharmacology Notes – 2021

What is Angina Pectoris ?

Anginal pectoris disease affect the coronary arteries which supply oxygenated blood from left
ventricle to heart tissues. In angina pectoris the lumen of artery become restricted and it becomes less efficient in supplying the blood and oxygen to heart called as ischemia.

The following two types of angina are mainly seen:
1) Classic Angina (Angina of Exercise): This angina pain occurs w hen the demand of oxygen exceeds the s upply of oxygen, most commonly due to diminished coronary flow.
2) Vasospastic (Prinzmetal’s or Variant) Angina: This angina pain occurs at rest and is characterised by reversible coronary vasospasm , which in turn reduces the supply of oxygen

Some individuals however show mixed angina, characterised by both exercise induced and resting attacks of angina.

Symptoms of Angina Pectoris includes:
- Weakness
- Heartburn
- Cramping
- Indigestion
- Sweating
- Nausea
- Shortness of breath
Classification of Antianginal Drugs

The antianginal drugs are are classified between the following types:
- Nitrates:
  - Short acting: Glyceryl trinitrate (GTN)
  - Long acting: Isosorbide dinitrate, Isosorbide mononitrate ,Erythrityl tetranitrate, Pentaerythrityl tetranitrate
- β Blockers: Metoprolol, Atenolol, Bisoprolol, Celiprolol
- Cytoprotective Drugs: Trimetazidine, Ranolazine.
- Potassium Channel Opener: Nicorandil, Pinacidil, Cromakalim,Minoxidil, Diazoxide
- Calcium Channel Blockers:
  - Verapamil, Diltiazem
  - Dihydropyridine —Nifedipine, Amlodipine, Nitrendipine,Nimodipine
Antianginal Drugs – Nitrates

Organic nitrites and nitrates are simple nitric and nitrous acid esters of glycerol having different
volatilities (e.g., isosorbide dinitrate and isosorbide mononitrate are solids at room temperature, nitroglycerine is moderately volatile, and amyl nitrite is highly volatile). These compounds are used in angina pectoris. They rapidly reduce the myocardial oxygen demand, followed by rapid relief of symptoms. They are effective in classic as well as in variant angina pectoris.

Mechanism of Action

Nitrates inhibit coronary vasoconstriction or spasm as a result of which perfusion of the myocardium increases, thus, relieving vasospastic angina. Nitrates also cause venodilation, resulting in decreased preload and myocardial oxygen consumption. Due to this action, nitrates are effectively used in classic angina

Mechanism of Action of Nitrates

Therapeutic Uses

Therapeutic uses of Nitrates are given below:
- Angina pectoris
- Acute coronary syndromes
- Myocardial infarction (MI)
- CHF and acute LVF
- Biliary colic
- Esophageal spasm
- Cynaide poisoning
Adverse Effect

The most common toxic effects of nitrates are the responses evoked by vasodilation.
- These include tachycardia (from the baroreceptor reflex)
- Orthostatic hypotension (a direct extension of the venodilator effect), and
- Throbbing headache from meningeal artery vasodilatation.
Drug Interection

Nitrates + Sildenafil can lead to severe hypotension, myocardial infarction and death.

Antianginal Drugs – Calcium Channel Blockers

Calcium channel blockers invariably block L-type Ca2+ channel, and decrease heart rate, contracitility and conduction velocity. They also reduce left-ventricular filling pressure, which reduces workload and overall oxygen demand of the heart.

Mechanism of Action

Calcium channel blockers act by blocking the voltage -sensitive calcium channels. They act on the inner side of the membrane and bind to the channels in depolarized membrane .
As a result of drug binding , the channels open rarely after depolarization. A marked decrease in trans membrane Ca2+ion current relaxes the smooth muscles.

Therapeutic Action

Calcium channel blockers are used for the treatment of stable as well as variant angina. In variant angina, they cause relaxation of coronary artery spasm , thus increasing the cardiac oxygen supply; while in stable angina, they cause relaxation of peripheral arterioles, resulting in decreased after load and cardiac oxygen demand. Verapamil and Diltiazem moderately reduce oxygen demand by suppressing the heart rate and contractility.

Adverse Effects

Calcium channel blockers give rise to cardiovascular adverse effects. Blood pressure reduces due to dilation of peripheral arterioles , resulting in induced reflex tachycardia. This reaction mainly occurs with nifedipine and rarely with verapamil and diltiazem. Due to their suppressant effects on the heart, verapamil and diltiazem should be used carefully in patients taking β-blockers and suffering from bradycardia, heart failure, or AV block.

Antianginal Drugs – β Blockers

β blockers are the drugs that block the action of cathecholamines through β receptors. Some β Blockers drugs are Timolol, metoprolol, atenolol, and propranolol.

Mechanism of Action

The β-adrenergic antagonists decrease the oxygen demand by reducing the heart rate. They oppose sympathetic stimulation , which increases heart rate, contraction force, and oxygen rate.

Therapeutic Effect

The β-adrenergic antagonists in combination with nitrates are used for the treatment of angina pectoris. Persistent angina can be trea ted using drugs from two or more classes, i.e., β adrenergic blockers combined with long -acting nitrates or calcium channel blockers.
The β-adrenergic antagonists due to their antihypertensive action are ideal for patients having hypertension and coronary artery disease. They are the drugs of choice for the prophylaxis of chronic angina

Adverse Effects

The adverse effects of β-adrenergic antagonists are hypotension, bradycardia, insomnia (inability to sleep), bizarre dreams, diminished sex drive, impotence, and depression.

Antianginal Drugs – Potassium Channel Openers

The potassium channel openers which were used earlier for the treatment of severe hypertension and hypertensive eme rgencies are minoxidil and diazoxide; but use of these agents has been reduced after synthesis of some novel potassium channel openers, like nicorandil, pinacidil, and cromakalim.

Mechanism of Action
- These drug opens the ATP – sensitive K channels
- Opening of this leads to hyper polarization
- Followed by closing of calcium channels
- Less intracellular calcium — muscle relaxation
Therapeutic Uses

Potassium channel openers are used in patients who have undergone optimal management with other d rugs, but still remain symptomatic, often while they await surgery or angioplasty.

Adverse Effects

Common adverse effects o f potassium channel openers are flushing, palpitation, weakness, headache, mouth ulcers, nausea, and vomiting.

Newer Antianginal Drugs

Some new antianginal drugs are discussed below:

Ranolazine: This drug reduces the number of angina episodes per week and increases exercise tolerance. These benefits were however moderate and smaller in women than in men.

Trimetazidine: It is an anti -ischemic (anti-anginal) metabolic agent. It improves myocardial glucose utilization by inhibiting fatty acid metabolism.

Dipyridamole: It is a powerful coronary dilator; increases total coronary flow by preventing uptake and degradation of adenosine.

Conclusion

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April 27, 2021
Antiparkinsonian Drugs Free Pharmacology Notes – 2021
Antiparkinsonian Drugs or agents are used to treat Parkinson’s disease or Parkinsonism’s. Parkinsonism is a progressive neurodegenerative disorder that affecting mostly older peoples. In this post, we going to discuss Antiparkinosian agents, their classification, mechanism of action, and adverse effects of these agents. At the end of this post, there is a Download button from where you can also download the note you read.

Antiparkinsonian Drugs Free Pharmacology Notes – 2021

What is Parkinsonism or Parkinson’s Disease ?

As we already told above that Parkinsonism is a progressive neurodegenerative disorder that mostly affects older peoples. It is an extrapyramidal motor disorder characterized by rigidity, tremor, and hypokinesia with secondary manifestations like defective posture, gait, and mask-like face.

Symptoms of Parkinson’s Disease

Symptoms of Parkinson’s disease are given below:
- Pill rolling tremors
- Akathesia: Inability to sit still
- Rigidity
- Kinesias (akinesia, bradykinesia)
- Unstable (stooped) posture
- No arm swinging in rhythm with legs
- Sialorrhea: profused salivary secretion
- Masked facial expression
Symptoms of Parkinson’s Disease (Antiparkinsonian Drugs)

Classification of Antiparkinsonian Drugs

Antiparkisonian drugs are classsified between two types Drugs affecting Brain dopaminergic System and Drugs Affecting Brain Cholinergic System. Detailed classification in given in the below list.
- Drugs Affecting Brain Dopaminergic System
  1. Dopamine Precursor: Levodopa
  2. Peripheral Decarboxylase Inhibitors: Carbidopa, Benserazide
  3. Dopaminergic Agonist: Bromocriptine, Ropinirole, Pergolide
  4. MAO B Inhibitors: Selegiline
  5. COMT Inhibitors: Entacapone, Tolcapone
  6. Dopamine Facilitator: Amantadine
- Drugs Affecting Brain Cholinergic System
  - Central anticholinergics: Trihexyphenidyl, Procyclidine, Biperiden
  - Antihistaminics: Orphenadrine, Promethazine
Dopamine Precursor- Levodopa

Levodopa is widely used for the treatment of all types of Parkinsonism, except the one
which is associated with antipsychotic therapy. All clinical manifestations respond to the
combination of Levodopa with Carbidopa. Rigidity, bradykinesia, abnormalities of posture, and locomotion respond well to the combination while tremors are less responsive. The
therapy started with a small dose of Carbidopa 25 mg + Levodopa 100 mg (1:4 ratio) three
times a day, 1 hour before meals. The dose of Levodopa is increased up to 250 mg (1:10
ratio) gradually. If necessary, a dopamine agonist like Bromocriptine may be added.

Mechanism of Action

Levodopa is an immediate precursor for transmitter DA which is stored and released as a transmitter.

Image Credit: Solution Pharmacy YouTube Channel ( Mechanism of Action of Antiparkinsonian Drugs )

Pharmacological Actions

Pharmacological actions of Levodopa on Parkinson’s disease are given below.
- Action on CNS
  - Hypokinesia and Rigidity resolved
  - Secondary Symptoms of Posture, Gait, Handwriting, Speech, Facial Expression, Mood, Selfcare and interest in life are generally normalized
- Action on CVS: Acts on β Receptors produces central action.
  - Postural Hypotension
- CTZ: Triggers the center leading to nausea and Vomiting
- Endocrine:
  - Mammotropes- Inhibit Prolactin Release
  - Somatotropes- Increase GH Release
Adverse effects

Levodopa may cause mydriasis and may precipitate an attack of glaucoma in some
patients. Abnormalities in smell/taste, hot flushes, and precipitation of gout may occur. Mild
but transient increase in blood urea, serum transaminases, alkaline phosphatize and bilirubin
may also be observed.

Dose

2-3 gm/day (LEVOPA 0.5gm Tablet)

Peripheral Decarboxylase Inhibitors

Mechanism of Action

Administered along with levodopa and it increase its t½ in periphery and make more DA available to cross along with the BBB

Levodopa+ Carbidopa= Co-careldopa

Advantages
- Plasma t½ ↑, the dose is reduced
- Cardiac complications are minimized
- Pyridoxine reversal of Levodopa effect does not occur
- The ‘On-off ‘ effect is minimized since levels of DA sustained.
- The degree of improvement also higher
Dose

TIDOMET-LS : 10mg Carbidopa +100mg Levodopa

Dopaminergic Agonists

These drugs directly stimulate DA receptors and do not depend on the formation of DA from Levodopa. They have the following advantages:
- They do not require metabolic conversion to DA.
- They do not depend on the functional integrity of dopaminergic neurons.
- They have a longer duration of action and lesser on-off phenomenon as compared to Levodopa.
- They are more selective than Levodopa on DA receptors.
- They are less likely to generate damaging free radicals.
Mechanism of Action

Selective activation of DA receptors in dopaminergic tract particularly on D2 receptors.
Eg. Bromocriptine

Pharmacokinetics

A – Orally

D – in major organ brain and its capillaries

M – liver , t½= 6-10hrs.

E – in Urine

Side Effects

Side effects of these drugs contains Vomiting, Hallucinations, Hypotension, Nasal Stiffness,
Conjunctival infection, Fall in BP

Dose

5-10mg thrice daily smoothens ‘on-off’ Fluctuations

MAO B Inhibitor

Inhibitors of the enzyme MAO-B are useful to treat PD. Selegiline is an irreversible
inhibitor of MAO-B, an enzyme in dopaminergic neurons responsible for the metabolism of DA.
It makes more DA available for stimulation of its receptors. Initially, Selegiline may be used
alone. Later, it is used along with Levodopa + Carbidopa to minimize the problem of dyskinesia
associated with long-term use of Levodopa. Selegiline may cause insomnia. It should not be coadministered with TCAs and SSRIs for the risk of acute toxic reactions like hyperpyrexia, agitation, delirium, and coma.
Selegiline is available as 5 mg tablet: SELGIN, SALERIN, ELEGELIN

COMT Inhibitors

Mechanism of action: COMT plays a role in the degradation of DA in brain as well, COMT INHIBITORS could preserve DA formed in the striatum and supplement the peripheral effect eg: entacapone acts only in the periphery (due to short duration of action) , For tolcapone also the
central action is less important.

Pharmacokinetics:
A- Orally
D- By binding with plasma albumin
M- in the liver by cytochrome P450
E- in Faeces and Urine

Side effects: Nausea, Vomiting, Dyskinesia, Hallucination
Dose: Entacapone: 200mg with each dose of levedopa and carbidopa Tolcapone: 100-200mg BD or TDS

Dopamine Facilitator

Mechanism of action: It appears to act by promoting presynaptic synthesis and release of DA in the brain. Action on glutamate receptors through which the striatal dopaminergic system exerts its influence has also been suggested eg: AMANTADINE
Side effects: These are not generally serious: insomnia, dizziness, confusion, nightmares, rarely hallucination.
Dose: Fixed doses of 100mg BD is used

Central Acting Anticholinergics

Mechanism of action: They act by reducing the unbalanced cholinergic activity in the striatum of parkinsonian patients, similarly H1 antagonist act as central acting anticholinergics
Side effects: Impairment of memory and organic confusional states are more common in elders

Dose: Trihexyphenidyl : 2-10 mg/day
Procyclidine : 5-20mg/day
Promethazine : 25-75mg/day

Conclusion

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April 22, 2021
Pharmaceutics 1 Book PDF Free Download

Download Pharmaceutics 1 Book in PDF For Free for the B.Pharm and D.Pharm students. Pharmaceutic is one of the main subjects for Pharmacy students. The pharmaceutic subject is also in the syllabus of the GPAT exam. In order to get more marks on the Pharmaceutic exam, you must have to follow some good books. In this post, we are providing some of the best Pharmaceutics Books to download. Download Books for other subjects from your website. We have the largest collection of Books for B.Pharm, D.Pharm, and Pharm. D students.

Download Pharmaceutics 1 Book PDF Online

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Dispensing Pharmacy is one the best books for the subject Pharmaceutics. Dispensing Pharmacy book is written by RM Mehta who has very good knowledge of pharmacy subjects. This books is good for your university exams.

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Remington Essentials of Pharmaceutics Book Free Download

Remington’s has been in print for more than 100 years and is a well-known reference text for pharmacists, pharmacy students, and pharmaceutical scientists alike. Over the past century, each edition has been updated to reflect the current state of the science and practice of pharmacy. Following the recent publication of the 22nd edition, the publishers asked me, as the
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April 21, 2021

Antipsychotics Free Pharmacology Notes – 2021

Antipsychotics are the drugs that are used in Psychosis. Psychosis is a mental disorder that may be a result of Schizophrenia. Schizophrenia is a mental disorder that affects a person’s ability to think, feel and behave clearly. The exact reason behind Schizophrenia is still unknown but there are three hypotheses, based on neurotransmitters used to explain the pathogenesis of schizophrenia. In this note, we will learn about different antipsychotic drugs, their mechanism of action, they have any side effects or not. Read the full note for complete details about Antipsychotic drugs.

What are Antipsychotics ?

Antipsychotics are the drugs that work against Psychosis which may be a result of mental disorders like Schizophrenia. The exact reason behind the Schizophrenia but researchers give three hypotheses which may the reason behind Schizophrenia.

Dopamine Hypothesis

The dopamine hypothesis was put forward by Arvid Carlsson. It is believed that Dopamine abnormality is the basis for most of the manifestations of schizophrenic patients. An excess amount of dopamine in some areas of the brain is considered responsible for schizophrenia. Typical antipsychotic drugs like Haloperidol bind to D2 receptors of DA. However, dopamine antagonists are not a cure for all schizophrenics. Probably, other neurotransmitters are involved.

5-HT/Serotonin Hypothesis

The role of 5-HT in schizophrenia is based on the finding that LSD, a central 5-HT2
receptor agonists produce hallucinations and sensory disturbances, which are symptoms. observed in psychosis. Atypical neuroleptics like Clozapine and Olanzapine are potent
5-HT2A receptor antagonists. These receptors modulate the release of DA in some areas of
the brain. Hence, both 5-HT and DA hypotheses for schizophrenia are compatible.

Glutamate Hypothesis

The involvement of glutamate is based on the finding that glutamate-NMDA receptor
antagonists like Phencyclidine and Ketamine when administered to a normal subject,
produce psychotic symptoms like hallucinations and thought disorders. In addition,
reduced glutamate densities have been reported in the brains of schizophrenics. Drugs
which may enhance NMDA receptor activity may be useful in treating schizophrenia.

Classification of Antipsychotics

Antipsychotic drugs are classified between Typical or First Generation Antipsychotics and Atypical or Second-Generation Antipsychotics.

Typical or First Generation Antipsychotic Drugs

Typical antipsychotic drugs are further classified into:

Phenothiazines: Phenothiazines have many effects, including Central Nervous System depression, autonomic nervous system depression (antiadrenergic and anticholinergic effects), antiemetic effects, lowering of body temperature, hypersensitivity reactions, and others. They are further sub-classified based on side chains attached to phenothiazines.
- Aliphatic side chain: Chlorpromazine
- Piperidine side chain: Thioridazine
- Piperazine as side chain: Trifluoperazine, Perfenazine, Fluphenazine

Thioxanthenes: Flupenthixol, Thiothixene, Zuclopenthixol.
Butyrophenones: Haloperidol, Benperidol, Droperidol.
Miscellaneous: Pimozide, Penfluridol, Molindone, Loxapine, Sulpiride, Amisulpride, Remoxipride

Atypical or Second Generation Antipsychotic Drugs

Clozapine, Olanzapine, Quetiapine, Zotepine, Risperidone, Ziprasidone, Paliperidone, Aripiprazole, Sertindole, Asenapine

Mechanism of Action

Typical Antipsychotic Drugs

Typical or First generation antipsychotics act as antagonist at brain dopamine D2 receptors.
Typical antipsychotic drugs also blocks the muscarinic acetylcholine receptors, anti histamine receptors, and alpha adrenoceptors.

Atypical Antipsychotic Agents

Atypical or Second-generation antipsychotic agent is predominant antagonism of 5-HT2A receptors with a lesser degree antagonism of dopamine D2 receptors.
Atypical antipsychotic agents have efficacy against negative symptoms especially clonazepam.

All antipsychotic drugs exhibit a latent period of 2-3 weeks for attaining therapeutic
effects. The majority of them are given orally; however, their bioavailability increases tenfold
when given by the intramuscular route.

Therapeutic Uses

Antipsychotic agents are usually use in three type of indications.

Psychiatric indications: They are primarily used to treat schizophrenia. In addition, they are also used to treat drug-induced psychoses like delusions associated with LSD, Amphetamine-induced psychoses, and delirium following infectious psychoses. They are also used to treat schizoaffective disorders in which schizo refers to schizophrenia and affective refers to mania.
Neuro-psychiatric indications: It involves use in Tourette’s syndrome which is marked by tics, grunts, and vocalizations that are frequently obscene. Haloperidol and Pimozide are preferred for this condition. In addition, they are also useful for Huntington’s disease which involves progressive choreoathetosis and dementia. Haloperidol and Chlorpromazine are preferred for this condition.
Non-psychiatric indications: All antipsychotics have antiemetic effects of varying degrees. It is due to the blockade of the D2receptor in CTZ as well as in GIT. Prochlorpromazine is preferred for this purpose. Antipsychotic like Promethazine is used as a pre-operative sedative since it has antihistaminic, anticholinergic and antiemetic effects also. Droperidol is a short-acting antipsychotic with antiemetic, sedative, and anticonvulsant effects. Parenteral chlorpromazine or Haloperidol is useful in controlling intractable hiccups.

Adverse Effects

Adverse Effects of Typical or First Generation Antipsychotics

Extrapyramidal Motor Effects: Due to Dopamine D2 receptors blockade in the nigrostriatal pathway.
- Acute dystonia
- Akathisia
- Parkinsonism
- Tardive Dyskinesia

Endocrine Effects: Due to blockade of dopamine D2 receptor in tuberohypophyseal pathway that increase the release of prolactin.
- Gynaecomastia
- Galactorrhoea
- amenorrhea in women
- sexual disinfection or infertility in men

Adverse Cardiac Effects
Increased risk for cerebrovascular events and all- cause mortality in dementia patients.
Lowers seizure threshold.
Increased triglycerides
Hyperglycaemia

Adverse effects of Atypical or Second Generation Antipsychotics

Extrapyramidal Motor Effects
- Considerably less compared to typical antipsychotics
- Blockage of 5-HT2A receptors increases dopamine in the striatum preventing extrapyramidal effects.

Cardiotoxicity: Less associated with QT prolongation at therapeutic doses
High risk of new onset diabetes and diabetes ketoacidosis esp. with clozapine and olanzapine
Agranulocytosis common with clozapine esp. in first 6 months

Drug Interactions

Drug interactions of Antipsychotic drugs are given in the below table

Drug	Effects
Antacids	Decreased absorption of antipsychotic drugs
Anticholinergics	Increased anticholinergic effects
Alcohol	More sedation
Antithyroid drugs	Increased risk of agranulocytosis (with Clozapine)
Barbiturates	Decreased antipsychotic effects, more sedation
Carbamazepine/Phenytoin	Decreased antipsychotic effects and lowering of seizure threshold
Chloroquine	May precipitate extrapyramidal symptoms with Phenothiazines
Lithium	Enhancement of neurotoxicity and precipitation of NMS (Haloperidol)
Levodopa	Decreased efficacy of neuroleptics
Oral contraceptives	May potentiate hyperprolactinemia
Cigarette smoking	Increased metabolism of antipsychotics; higher dose needed

Drug interactions with antipsychotic drugs

Preparations of various antipsychotic drugs are given in below table

Drug	Formulations and strength
Chlorpromazine	25 mg, 50 mg, 100 mg, 200 mg tablet; 25 mg/ml injection
Fluphenazine	25 mg/ml injection
Trifluoperazine	5 mg, 10 mg tablet
Thioridazine	10 mg, 25 mg, 50 mg, 100 mg tablet
Flupenthixol	0.5 mg, 1 mg, 3 mg tablet; 20 mg/ml depot injection
Zuclopenthixol	200 mg/ml injection
Haloperidol	1.5 mg, 5 mg, 10 mg, 20 mg tablet; 2 mg/ml, 5 mg/ml injection, 50 mg/ml depot injection
Penfluridol	20 mg tablet
Pimozide	2 mg, 4 mg tablet
Loxapine	10 mg, 25 mg capsule; 25 mg/ml liquid
Sulpiride	100 mg, 200 mg, 400 mg tablet
Amisulpiride	50 mg, 100 mg, 200 mg tablet
Levosulpiride	25 mg tablet
Clozapine	25 mg, 50 mg, 100 mg tablet
Olanzapine	2.5 mg, 5 mg, 7.5 mg, 10 mg, 15 mg, 20 mg tablet
Risperidone	1 mg, 2 mg, 3 mg, 4 mg tablet; 1 mg/ml syrup
Ziprasidone	20 mg, 40 mg, 80 mg tablet
Paliperidone	3 mg, 6 mg, 9 mg ER tablet
Aripiprazole	10 mg, 15 mg, 20 mg, 30 mg tablet
Quetiapine	25 mg, 50 mg, 100 mg, 200 mg, 300 mg tablet

Available preparations of antipsychotic drugs

Conclusion

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April 20, 2021

Route Of Drug Administration Free Pharmacology Note – 2021

In this topic “Route of Drug Administration” we are going to discuss the different types of Routes from where we can administrate the drugs. There are many ways to administrate a drug like the Parenteral route, Oral route, Local route, systemic route, and many other routes. In this post, we will do a detailed discussion on these routes and the advantages, disadvantages of these routes.

What is Route of Drug Administration

Route of drug administrations refers to the starting point of the body from where the drug will be introduced to the body and will be reached the target organ or system to show its effects. Most of these drugs can be administrated via different routes and they also depend on different factors

Factors Affecting Route of Drug Administration

There are many routes of drug administration and it is depend on many factors also. The factors that effect on the route of drug administration are given below:

The physical and chemical properties of drug molecules affect the routes for drug administration.
The site for the desired action also affects the routes
The route for administration of the drug also depends upon the condition of the patient. The route can change for unconscious, vomiting, diarrhea patients.
The age of the patient is also an important factor.
The route also depends on the usage type of the drug. This can be changed on emergency usages or routine usages.
Effects of gastric pH, digestive enzymes, and first-pass metabolism also affect the route of drug administration.

Different Routes of Drug Administrations

There are different type of routes for drug administration. There are mainly two different routes 1. Local Route and 2. Systemic Route.

Oral Routes

Drugs absorption via oral administration can be quite variable. Dosage form design may also be used modify the rate of absorption.

Advantages of Oral Drug Administration

Drugs administrated via Oral routes are safe, cheap and easy to take.
Drug administration via oral routes are very convenient.
Variety of dosage forms are available for oral administration.

Disadvantages of Oral Drug Administration

Sometimes inefficient – high dose or low solubility drugs may suffer poor availability, only part of the dose may be absorbed. Griseofulvin was reformulated about 1970 to include the drug as a micronized powder. The recommended dose at that time was decreased by a factor of two because of the improved bioavailability.
First-pass effect – drugs absorbed orally are transported to the general circulation via the liver. Thus drugs that are extensively metabolized will be metabolized in the liver during absorption.
Food – Food and G-I motility can affect drug absorption. Often patient instructions include a direction to take with food or take on an empty stomach. Absorption is slower with food for tetracyclines and penicillins, etc. However, for propranolol bioavailability is higher after food, and for griseofulvin, absorption is higher after a fatty meal.
Local effect – Antibiotics may kill normal gut flora and allow overgrowth of fungal varieties. Thus, antifungal agents may be included with an antibiotic.
Unconscious patient – The patient must be able to swallow solid dosage forms. Liquids may be given by tube

Buccal and Sublingual

Some of the drugs are taken as smaller tablets that are held in the mouth or under the tongue. These are buccal or sublingual dosage forms. Buccal tablets are usually harder tablets [4 hour disintegration time], designed to dissolve slowly. Nitroglycerin, as a softer sublingual tablet [2 min disintegration time], may be used for the rapid relief of angina. This Route of Administration is also used for some steroids such as testosterone and oxytocin. Nicotine-containing chewing gum may be used for cigarette smoking replacement.

Advantages

First pass – In this route, the Liver is bypassed so there is no loss of drug by the first-pass effect like the Oral administration route for buccal or sublingual administration. Bioavailability is higher also.
Rapid absorption – Because of the good blood supply to the area of absorption is usually quite rapid, especially for drugs with good lipid solubility.
Drug stability – pH in mouth relatively neutral (cf. stomach – acidic). Thus the drug may be more stable.

Disadvantages

Holding the dose in the mouth is somewhat difficult. If any part of the dose is swallowed mistakenly then that portion must be treated as an oral dose and it will be then subject to first pass metabolism.
Usually Buccal and Sublingual routes more suitable for drugs with small doses.
Drug taste may need to be masked

Rectal

Drugs are given by the rectal route of drug administration are most commonly given as suppository or enema. Some of the drugs that are given by this route include aspirin, theophylline, chlorpromazine, and some barbiturates.

Advantages

By-pass liver – Some (but not all) of the veins draining the rectum lead directly to the general circulation thus bypassing the liver. Therefore there may be a reduced first-pass effect.
Useful – This route may be most useful for patients unable to take drugs orally or with younger children.

Disadvantages

Erratic absorption – Drug absorption from a suppository is often incomplete and erratic. However, for some drugs, it is quite useful. There is research being conducted to look at methods of improving the extent and variability of rectal administration. Absorption from solutions used as an enema may be more reliable.

Intravenous

Drugs that are given via Intravenous are usually given into a peripheral vein. Rapid injections are used to treat epileptic seizures, acute asthma, or cardiac arrhythmias.

Advantages

Rapid – A quick response is possible for the drugs that are given via the Intravenous route. Plasma concentration can be precisely controlled using IV infusion administration.
Total dose – The whole dose is delivered to the bloodstream that is given via the Intravenous route. That is the bioavailability is generally considered to 100% after IV administration.

Disadvantages

Finding Suitable vein – It may be difficult to find a suitable vein to give the drug via the Intravenous route. There may be also some tissue damage at the site of injection if it is not given carefully.
Maybe toxic – As the drugs administrated via the Intravenous show the rapid response, toxicity can be a problem with rapid drug administrations.
Requires trained personnel – Trained personnel are required to give intravenous injections.
Expensive – Sterility, pyrogen testing, and larger volume of solvent mean greater cost for preparation, transport, and storage.

Subcutaneous

By Subcutaneous method the drugs are given under the skin. Insulin Injection is given to the patients via this route of administration.

Advantages

Drugs of this route can be given by the patient.
Absorption can be fast from an aqueous solution but slower with depot formulations. Absorption is usually complete. Improved by massage or heat. Vasoconstrictor may be added to reduce the absorption of a local anesthetic agent, thereby prolonging its effect at the site of interest.

Disadvantages

Can be painful. Finding suitable sites for repeat injection can be a problem.
Irritant drugs can cause local tissue damage.
Maximum of 2 ml injection thus often small doses limit use.

Intramuscular

Advantages

A larger volume than Subcutaneous can be given by Intramuscular. They may be easier to administer than intravenous injections.
A depot or sustained release effect is possible with the intramuscular injections, e.g. procaine penicillin

Disadvantages

Trained personnel required to give injections via Intramuscular routes.
Absorption can be rapid from an aqueous solution. Absorption is sometimes erratic, especially for poorly soluble drugs,e.g. diazepam, phenytoin. The solvent may be absorbed faster than the drug causing precipitation of the drug at the site of injection.
Sometime this method can be painful

Inhalation

Inhalation may be used for local effects like bronchodilators. Inhalation can also be use for systemic effects like general anesthesia. Drugs taken via Inhalation shows rapid absorption as it by pass the liver.

Topical

Local effect – ear drops, eye drops or ointment, antiseptic creams and ointments, sunscreens, callous removal products, etc.
Systemic effect – e.g., nitroglycerin ointment
Generally, absorption is quite slow. Absorption through the skin especially via cuts and abrasions or from sites where the skin is quite thin can be quite marked. This can be a real problem in handling toxic materials in the laboratory or pharmacy. This can also be a serious problem with garden chemicals.

Effect of Route of Drug Administration on Initiation of Effect of Drugs

Route of administration	Time
Intravenous	30 – 60 sec
Intraosseous	30 – 60 sec
Endotracheal	2 – 3 min
Inhalation	2 – 3 min
Sublingual	3 – 5 min
Intramuscular	10 – 20 min
Subcutaneous	15 – 30 min
Rectal	5 – 3 min
Oral	39 – 90 min
Transdermal or Topical	mins to hours

Conclusion

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April 19, 2021

Antihypertensive Drugs Free Pharmacology Notes – 2021

Antihypertensive Drugs are used to treat hypertension which is caused due to high blood pressure. In this note, we will learn about the classification of Antihypertensive drugs, their type, mechanism of action, advantages, and side effects of the drugs. At the end of this note, there will be an MCQ test where you test your knowledge of how much you learn about Antihypertensive Drugs. So read this note carefully and participate in the MCQ Test. Best of Luck ?.

Antihypertensive Drugs Notes Read Online

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Antihypertensive Drugs Pharmacology Notes

Classification of Antihypertensive Drugs

Antihypertensive Drugs are classified into the following types

Diuretics
Beta adrenergic blockers
Calcium channel blockers
Angiotensin converting enzyme inhibitors
Angiotensin receptor blockers
Sympatholytics and adrenergic blockers
Direct arterial vasodilators

We will discuss these classifications in this post. We will cover topics like Types of these classifications, Mechanism of Action. Advantages of the drugs, side effects, practical consideration, and special indications.

Diuretics

Diuretics drugs are a type of Antihypertensive drug that are used to treat Hypertension. Diuretics drugs are used to increase the amount of urine produced by the Kidney and increase the excretion of sodium and other types of electrolytes.

Types of Diuretic Drugs

Thiazides and related diuretics
Loop diuretics
Potassium sparing diuretics

Mechanism of Action

Initial effects: through reduction of plasma volume and cardiac output.
Long-term effect: through the decrease in total peripheral vascular resistance.

Advantages

Advantages of the Diuretics drugs are given below

Documented reduction in cardiovascular morbidity and mortality.
Least expensive antihypertensive drugs.
Best drug for the treatment of systolic hypertension and for hypertension in the elderly.
Can be combined with all other antihypertensive drugs to produce a synergetic effect.

Side Effects

Side effects of Diuretic drugs are listed below

Metabolic effects (uncommon with small doses): hypokalemia, hypomagnesemia, hyponatremia, hyperuricemia, dyslipidemia (increased total and LDL cholesterol), impaired glucose tolerance, and hypercalcemia (with thiazides).
Postural hypotension.
Impotence in up to 22% of patients.

Practical Considerations

Moderate salt restriction is the key for the effective antihypertensive effect of diuretics and for protection from diuretic-induced hypokalaemia.
Thiazides are not effective in patients with renal failure (serum creatinine >2mg /dl) because of reduced glomerular filtration rate.
Frusemide needs frequent doses ( 2-3 /day ). Thiazides can be given once daily or every other day
Potassium supplements should not be routinely combined with thiazide or loop diuretics. They are indicated with hypokalemia (serum potassium < 3.5mEq/L) especially with concomitant digitalis therapy or left ventricular hypertrophy.
Nonsteroidal anti-inflammatory drugs can antagonize diuretics’ effectiveness.

Special Indications

Diuretics should be the primary choice in all hypertensives.
They are indicated in:
- Volume dependent forms of hypertension: blacks, elderly, diabetic, renal, and obese hypertensives.
- Hypertension is complicated with heart failure.
- Resistant hypertension: loop diuretics in large doses are recommended.
- Renal impairment: loop diuretics.

Beta – Adrenergic Blocking Agents

Beta-Adrenergic Blocking agents are widely used to treat Hypertension, Angina pectoris, and cardiac arrhythmia. These antihypertensive agents are also used to treat anxiety and to reduce the side effects of Hyperthyroidism.

Mechanism of Action

The initial decrease in cardiac output, followed by a reduction in peripheral vascular resistance.
Other actions include decrease plasma renin activity, resetting of baroreceptors, the release of vasodilator prostaglandins, and blockade of prejunctional beta-receptors.

Advantages

The advantages of Beta-Adrenergic blocking agents are given below.

Documented reduction in cardiovascular morbidity and mortality.
Cardioprotection: primary and secondary prevention against coronary artery events (i.e. ischemia, infarction, arrhythmias, death).
Relatively not expensive.

Practical Considerations

Beta blockers are used with caution in patients with bronchospasm.
Contraindicated in more than grade I AV, heart block.
Do not discontinue abruptly.

Side Effects

Side effects of the Beta-Adrenergic Blocking Agents are listed below.

Bronchospasm and obstructive airway disease.
Bradycardia
Metabolic effects (raise triglyceride levels and decrease HDL cholesterol; may worsen insulin sensitivity and cause glucose intolerance). Increased incidence of diabetes mellitus.
Coldness of extremities.
Fatigue.
Mask symptoms of hypoglycemia.
Impotence.

Special Indications

special indications of Beta-Adrenergic are discussed below.

First-line treatment for hypertension as an alternative to diuretics.
Hypertension associated with coronary artery disease.
Hyperkinetic circulation and high cardiac output hypertension (e.g., young hypertensives).
Hypertension associated with supraventricular tachycardia, migraine, essential tremors, or hypertrophic cardiomyopathy

Calcium Channel blockers

Calcium channel blockers are one type of Antihypertensive drug that is used to control high blood pressure. These calcium channel blockers work by slowing the movement of calcium into the cells of the human heart and blood vessel walls, which makes it easier for the heart to pump and widens blood vessels.

Types

Dihydropyridine: nifedipine, amlodipine, felodipine, nicardipine, lacidipine.
Nondihydropyridine: Phenylalkylamine, verapamil, Benzothiazepine, diltiazem

Mechanism of Action

It decreases the concentration of free intracellular calcium ions results in decreased contraction and vasodilation.
It shows diuretic effect through an increase in renal blood flow and glomerular filtration rate
Inhibition of aldosterone secretion.

Advantages

Some advantages of the calcium channel blockers are discussed below.

No metabolic distrubances: no change in blood glucose, potassium, uric acid and lipids.
May improve renal function.
Maintain optimal physical, mental, and sexual activities.

Practical Considerations

Short-acting dihydropyridine should be combined with beta-blockers in coronary artery disease and should be avoided in stroke, and hypertensive crisis.

Special Indications

Some special indication of calcium channel blockers are discussed below.

Ischemic heart disease: when beta-blockers are ineffective or contraindicated and in vasospastic angina.
Elderly hypertensives: second agent of choice after diuretics.
Peripheral vascular disease (e.g., Raynaud’s phenomenon).

Side Effects

Some side effects of calcium channel blockers are

Dihydropyridine: flushing, headache, and lower limb oedema.
Nondihydropyridine: aggravation of heart failure and heart block. Verapamil may cause constipation.

Angiotensin Converting Enzyme Inhibitors

Angiotensin-converting enzyme (ACE) inhibitors are a type of antihypertensive drug that is used to treat high blood pressure and to prevent heart attacks. Calcium channel blockers are work by relaxing the blood vessels and by decreasing the blood volume.

Types

Class I: captopril
Class II (prodrug) : e.g., ramipril, enalapril, perindopril
Class III ( water soluble) : lisinopril.

Mechanism of Action

Inhibition of circulating and tissue angiotensin- converting enzyme.
Increased formation of bradykinin and vasodilatory prostaglandins
Decreased secretion of aldosterone; help sodium excretion.

Advantages

Reduction of cardiovascular morbidity and mortality in patients with atherosclerotic vascular disease, diabetes, and heart failure.
Favorable metabolic profile.
Improvement in glucose tolerance and insulin resistance.
Renal glomerular protection effect especially in diabetes mellitus.
Do not adversely affect the quality of life.

Special Indications

Diabetes mellitus, particularly with nephropathy
Congestive heart failure
Following myocardial infraction.

Side Effects

Cough (10 – 30%): a dry irritant cough with tickling sensation in the throat.
Skin rash (6%).
Postural hypotension in salt depleted or blood volume depleted patients
Angioedema (0.2%) : life threatening.
Renal failure: rare, high risk with bilateral renal artery stenosis
Hyperkalaemia.
Teratogenicity.

Practical considerations

Contraindications include bilateral renal artery stenosis, pregnancy, known allergy, and hyperkalemia.
High serum creatinine (> 3 mg/dl) is an indication for careful monitoring of renal function and potassium. Benefits can still be obtained in spite of renal insufficiency.
A slight stable increase in serum creatinine after the introduction of ACE inhibitors does not limit use.
ACE-I is more effective when combined with diuretics and moderate salt restriction.

Angiotensin Receptor Blockers

Angiotensin receptor blockers (ARBs), also known as angiotensin II receptor antagonists, These are a type of antihypertensive drugs that are used to treat high blood pressure and heart failure

Mechanism of Action

They act by blocking type I angiotensin II receptors generally, producing more blockade of the renin-angiotensin-aldosterone axis.

Advantages

Similar metabolic profile to that of ACE-I
Renal protection.
They do not produce cough

Practical Indications

Patients with a compelling indication for ACE-I and who can not tolerate them because of cough or allergic reactions.

Sympatholytics And Alpha Adrenergic Blockers

Types

Alpha 1-receptor blockers: prazocin,doxazocin.
Centrally acting alpha 2- agonists: methyldopa, clonidine.
Peripherally acting adrenergic antagonists: reserpine
Imidazoline receptor agonists: rilmenidine, moxonidine.

Advantages

Alpha1- receptor blockers and imidazoline receptor agonists improve lipid profile and insulin sensitivity
Methyldopa: increases renal blood flow. Drug of choice during pregnancy.
Reserpine: neutral metabolic effects and cheap.

Special indications

Diabetes mellitus: alpha1- receptor blockers, imidazoline receptor agonists.
Dyslipidemia: alpha 1- receptor blockers, imidazoline receptor agonists.
Prostatic hypertrophy: alpha 1- receptor blockers.
When there is a need for rapid reduction in blood pressure: clonidine.

Side Effects

Prazosin: postural hypotension, diarrhea, occasional tachycardia, and tolerance (due to fluid retention).
Methyldopa: sedation, hepatotoxicity, hemolytic anemia, and tolerance
Reserpine: depression, lethargy, weight loss, peptic ulcer, diarrhea, and impotence.
Clonidine: dry mouth, sedation, bradycardia, impotence, and rebound hypertension if stopped suddenly

Practical Considerations

Prazosin, methyldopa, and reserpine should be combined with a diuretic because of fluid retention.
In Egypt, reserpine is only available as a combination pill with thiazide (Bernardine) which contains 0.1 mg of reserpine per tablet.

Direct Arterial Vasodilators

Types

hydralazine
diazoxide
nitroprusside
minoxidil

Patients’ compliance to antihypertensive medications

Poor adherence to antihypertensive therapy remains a major therapeutic challenge contributing to the lack of adequate control of blood pressure in more than two-thirds of patients with hypertension. One-half of all patients discontinue antihypertensive medications within one year

Causes of Poor Compliance.

Hypertension has no symptoms and treatment has to continue indefinitely.
Poor communication with the patient. Very long intervals between follow-up visits, and frequent change of doctors impair the doctor-patient relationship.
Logistic barriers e.g. expense of medications, inability to read instructions, complicated multidose regimens, etc….
Adverse drug effects

Strategies to Improve Compliance

Educate patients about the disease and involve their families in the treatment
Stress that treatment is life-long.
Consider cost while prescribing.
Consider adverse effects at initial prescription and follow up visits.
Prescribe simple once-daily regimens.
Allow extra visits for blood pressure measurement at no extra charge to the patient.
Arrange follow-up visits at intervals no more than three months apart, during the first year.
Encourage life style modifications.

Preparations and Dosages of Antihypertensive Drugs

Class	Generic Name	Daily Dose (mg)
Diuretics	Hydrochlorothiazide	12.5-50
	Indapamide	1.25-5
	Chlorthalidone	25-50
	Frusemide	200-4000
	Bumetanide	1-4
Beta adrenergic blockers	Atenolol	25-100
	Metoprolol	50-200
	Bisoprolol	2.5-10
Calcium antagonists	Verapamil	120-480
	Diltiazem	90-240
	Nifedipine	20-80
	Amlodipine	2.5-10
	Lacidipine	2-4
ACE inhibitors	Captopril	50-100
	Enalapril	2.5-4
	Lisinopril	10-40
	Ramipril	2.5-20
	Perindopril	2-8
Angiotensin Receptor blockers	Losartan	25-100
	Valsartan	80-230
	Candesartan	4-32
	Telmisartan	20-80
Alpha-adrenergic blockers	Prazocin	1-16
	Doxazocin	1-16
Centrally acting drugs	Methyldopa	500-2000
	Clonidine	0.1-1.2
	Rilmenidine	1-2
	Reserpine	0.1

Commonly Used Oral Antihypertensive drugs

MCQ Test

MCQ Test of antihypertensive drugs are under process will be added soon. Kindly visit later to participate.

Disclaimer

Conclusion

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April 16, 2021

Best BPharm Entrance Exam Guide – 2021

BPharm course is gaining popularity day by day in India. This post is a guidepost about BPharm Entrance Exam in India. We have covered all the Entrance Examinations for the BPharm course of every state of India. By doing this course you can set a very good life in the Pharmaceutical and Medicine world not only in India but the whole world. Several state and national level universities organize entrance examinations every year for admission in the BPharm course..

Students who have passed the 12th Board examination in science stream with Physics, Chemistry and Mathematics are eligible for this course.

Online BPharm Exam Entrance Guide

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Best BPharm Entrance Exam Guide - 2021 — Best BPharm Entrance Exam Guide – 2021

Basic Details of BPharm Course

Course	Eligibility Criteria	Entrance Exams
B.Pharm or B.Pharma or Bachelor in Pharmacy	Candidate must be passed 12 Board with Science Stream. The candidate must score at least 40% in his 12 Board Exams. Candidate must have Physics, Chemistry, and Mathematics or Biology Subject in his/her 12th. Candidates, age must be more than 17 years old.	WBJEE CG PPHT GUJCET BITSAT MHT CET UPSEE TSEAMCET APEAMCET KCET OJEE KEAM

As we already said B.Pharm course is gaining popularity day by day and if you want to make a good carrier life in the field of Pharmaceutical Sciences and Medicines then you can easily choose B.Pharm as your Bachelor’s degree. You can get placed in many Government as well as many Private companies and a good package. You can start your carrier life as a Hospital Pharmacist, Marketing Representative or can work in Pharmaceutical Manufacturing plants in different posts and also can open your own Medical Shop.

Statewise BPharm Entrance Exams

Different states of India have different entrance examinations for the candidates. Candidates must have to qualify for the entrance exam and secure a good rank to get admission to the best colleges of the states. Here is the list of entrance exams of the different states of India.

Entrance Exam	State
WBJEE	West Bengal
CG PPHT	Chhattisgarh
GUJCET	Gujrat
BITSAT	Hyderabad, Goa, Pilani
MHT CET	Maharashtra
UPSEE	Uttar Pradesh
TS EAMCET	Telangana
AP EAMCET	Andhra Pradesh
KCET	Karnataka
KEAM	Kerala
OJEE	Odisha

How to Prepare for BPharm Entrance Exams

As we already mentioned candidates must passed the 12th Board exam with Physics, Chemistry, Mathematics or Biology to get admission in B.Pharm course. Unlike other entrance exam like B.Tech you have sit for Biology paper differently to eligible for the Pharmacy course.

You have to read the textbooks of class 11 and 12 very clearly to clear these entrance exams and to secure good rank. You may buy some competitive exam books to practice for the exams.

You may follow the below given syllabus for the Entrance examinations.

Physics Syllabus

Units and Measurement
Motion in a Straight line
Law of motion
Work
Power and Energy
Gravitation
Oscillation
Fluid Mechanics
Heat and Thermodynamics
Wave Motion
Magnetism
Electrostatics and Current Electricity
Chemical Effect of Electric Current and its Applications
Atomic Structure
Modern Physics

Chemistry Syllabus

Physical Chemistry
Inorganic Chemistry
Organic Chemistry

Biology Syllabus

Botany
Zoology

Mathematics Syllabus

Sets
Relation and Function
Trigonometric Functions
Principle of Mathematical Induction
Complex Number and Quadratic Equation
Linear Inequality

Tips for BPharm Entrance Exam

To make a good carrier life after the B.Pharm course you have to choose a good Pharmacy college. You have to secure a good rank so you can easily take admission of top colleges of your state. Here are some tips for you which can help you.

Create a good study plan
Clear the basics of the subjects
Clear if you have any doubt about any questions with the help of your teachers, friends
Revise regularly
Make notes
Solve previous year question papers
Maintain a proper sleep routine.

Disclaimer

Conclusion

April 11, 2021

Author: Pankaj Saha

Introduction

Aurobindo Pharma Ltd.

Hetero Drugs Ltd.

Glochem Industries Limited

Divis Laboratories Ltd

Novartis India Ltd.

Natco Pharma Limited

Lee Pharma Limited

Rakshit Drugs Private Limited

SMS Pharmaceuticals Ltd.

Dr Reddy’s Laboratories

Other Pharma Companies of Hydrabad

Introduction of Anti Hyperlipidemic Drugs

Classification of Anti Hyperlipidemic Drugs

HMG-CoA Reductase Inhibitors (Statins)

Bile Acid Sequestrants (Resins)

Fibric Acid Derivatives (Fibrates)

Triglyceride Synthesis and Lipolysis Inhibitors

Nicotinic Acid (Niacin)

Probucol

Other Anti Hyperlipidemic Drugs

Disclaimer

Conclusion

What is Arrhythmia and What is Antiarrhythmic Drugs ?

Classifications of Antiarrhythmatics

Antiarrhythmic Drugs – Sodium Channel Blockers

Moderate (Class IA)

Weak (Class IB)

Strong (Class IC)

Antiarrhythmic Drugs – β -Blockers

Antiarrhythmic Drugs – Potassium Channel Blockers

Antiarrhythmic Drugs – Calcium Channel Blockers

Disclaimer

Conclusion

What is Angina Pectoris ?

Classification of Antianginal Drugs

Antianginal Drugs – Nitrates

Antianginal Drugs – Calcium Channel Blockers

Antianginal Drugs – β Blockers

Antianginal Drugs – Potassium Channel Openers

Newer Antianginal Drugs

Conclusion

What is Parkinsonism or Parkinson’s Disease ?

Classification of Antiparkinsonian Drugs

Dopamine Precursor- Levodopa

Peripheral Decarboxylase Inhibitors

Dopaminergic Agonists

MAO B Inhibitor

COMT Inhibitors

Dopamine Facilitator

Central Acting Anticholinergics

Conclusion

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Remington Essentials of Pharmaceutics Book Free Download

Disclaimer

Conclusion

What are Antipsychotics ?

Classification of Antipsychotics

Typical or First Generation Antipsychotic Drugs

Atypical or Second Generation Antipsychotic Drugs

Mechanism of Action

Therapeutic Uses

Adverse Effects

Drug Interactions

Conclusion

What is Route of Drug Administration

Factors Affecting Route of Drug Administration

Different Routes of Drug Administrations

Oral Routes

Buccal and Sublingual

Rectal

Intravenous

Subcutaneous

Intramuscular

Inhalation

Topical

Effect of Route of Drug Administration on Initiation of Effect of Drugs