Author: Pankaj Saha

Pharmacology is a very important subject for every Medical, Pharmacy, and Nursing student. We have shared more than 100 Pharmacology Facts which will help every student to study and remember Pharmacology in a simple way. These pharmacology facts contains classification, mechanism of action, side effect, drug interaction of various drugs. Read the whole post and it will be so much helpful for everyone.

Introduction

1. The inhalational route is the route by which the rate of drug delivery can be controlled like i.v. infusion.
2. Pharmacokinetics is also called ADME study as it deals with Absorption, Distribution, Metabolism, and Excretion of a drug.
3. Bioavailability is the fraction of administered drug that reaches the systemic circulation in the unchanged form.
4. Absorption and first-pass metabolism are two important determinants of bioavailability.
5. AUC signifies the extent of absorption whereas Tmax. tells rate of absorption.
6. Glucuronidation is the most common phase II metabolic reaction.
7. The function of phase I reactions is to attach a functional group to the drug molecule whereas phase II reactions serve to attach a conjugate to the drug molecule.
8. Glomerular filtration does not depend on lipid solubility.
9. Lithium, KI, and rifampicin are secreted in saliva.
10. Urine should be alkalinized for acidic drug poisoning whereas acidified for basic drug poisoning.
11. Half-life is a secondary pharmacokinetic parameter derived from two primary parameters; Vd and CL.
12. Inotropic receptors include GABAA, NM, NN, NMDA (receptors of glutamate), and 5-HT3 receptors.
13. Insulin, growth hormone, prolactin, and cytokines act via enzymatic receptors.
14. Drugs having steep DRC have a narrow therapeutic index (like barbiturates) than those having less steep curves (e.g.benzodiazepines).
15. In phase 1 clinical trials, The drug is tested in healthy human volunteers and we cannot determine efficacy in this phase.
16. Recently, Phase O trial has also been added and is known as microdose studies. This is added to expedite the marketing of the drug.
17. Pharmacovigilance is the science and activities relating to the detection, assessment, understanding, and prevention of adverse effects or any other possible drug-related problems.
18. An orphan drug is a pharmaceutical agent that has been developed specifically to treat a rare medical condition (affecting fewer than 200,000 people)

Autonomic Nervous System

1. Acetylcholine (ACh) is the principal neurotransmitter at the neuromuscular junction as well as at all preganglionic fibers.
2. Saxitoxin (obtained from dinoflagellates) is a sodium channel blocker whereas α-bungarotoxin (a component of venom of banded krait) is an irreversible antagonist at NM receptors.
3. Atropine is an antidote of choice for both organophosphate and carbamate poisoning.
4. Latanoprost causes the growth of eyelashes as an adverse effect that can be utilized for the treatment of hypotrichosis.
5. Apraclonidine can cause lid retraction whereas brimonidine is associated with anterior uveitis. Both of these can cause drowsiness.
6. Tropicamide is the shortest-acting mydriatic.
7. Onabotulinum toxin A has recently been approved to prevent headaches in adult patients with chronic migraines.
8. Trospium has minimum CNS penetration among drugs used in overactive bladder.
9. Solefancin is the longest-acting and oxybutynin is the shortest-acting drug among this group.
10. The rate-limiting enzyme in catecholamine biosynthesis is tyrosine hydroxylase.
11. Adrenaline is the drug of choice for anaphylactic shock.
12. Dopamine is the drug of choice for a cardiogenic shock with oliguric renal failure.
13. Mirabegron is a new drug approved for overactive bladder. It acts by stimulating b3 receptors.
14. Ephedrine is the vasopressor of choice in pregnancy.
15. Tamsulosin and silodosin have been found to cause intraoperative ‘floppy iris syndrome during cataract surgery.
16. Contra-indications of nonselective β-blockers: A – Asthma, B – Block (AV), C – CHF, D – Diabetes.

Autacoids

1. Histamine is synthesized from histidine
2. Histamine-induced fall in blood pressure is mediated by both H1 (early) as well as H2 (delayed and persistent) receptors.
3. First-generation antihistamines are contraindicated in persons requiring constant attention.
4. Tiprolisant is H3 inverse agonist used for Narcolepsy.
5. Doxepin is a tricyclic antidepressant having the most potent H1 blocking action (800 times more potent than diphenhydramine).
6. Terfenadine and Astemizole result in polymorphic ventricular tachycardia (Torsades de pointes) manifested as prolongation of QTc interval.
7. Ergot derivatives can cause dry gangrene of hands and feet and coronary vasospasm.
8. Sumatriptan is the drug of choice for aborting acute attacks of migraines.
9. Frovatriptan is the longest acting and rizatriptan is the fastest acting 5HT1B/1D agonist.
10. Both triptans and ergot alkaloids can cause coronary vasospasm and are contraindicated in ischemic heart disease.
11. Triptans and ergotamine should not be administered within 24 hours of each other.
12. Propanolol is the most commonly used drug for the prophylaxis of migraine attacks.
13. Alprostadil is used to keep ductus arteriosus patent before surgery whereas NSAIDs like aspirin and indomethacin are used for the treatment of Patent ductus arteriosus.
14. Misoprostol is the most specific drug whereas proton pump inhibitors are drugs of choice for the treatment of peptic ulcers due to chronic NSAID use.
15. The use of misoprostol in pregnancy is associated with Moebius syndrome.
16. The most potent agent known to cause an increase in capillary permeability is the platelet-activating factor.
17. Paracetamol acts by inhibiting COX-3 in the brain
18. Paracetamol (acetaminophen) has no anti-inflammatory activity and Nimesulide and nefopam do not act by decreasing PG synthesis
19. Aspirin is the only irreversible inhibitor of the COX enzyme
20. Aspirin is contraindicated in children (<12 yrs old) due to the increased risk of Reye’s syndrome.
21. Piroxicam and tenoxicam are longest acting NSAIDs due to enterohepatic cycling.
22. Rofecoxib and valdecoxib were withdrawn due to increased risk of thrombotic disorders like myocardial infarction.
23. Hydroxychloroquine is the safest DMARD in pregnancy
24. Colchicine is more effective and faster acting than NSAIDs

Cardiovascular System

1. Spironolactone is the only diuretic that decreases mortality in patients with CHF.
2. Digoxin and digitoxin are the only inotropic drugs available that can be given orally.
3. Digitalis is contra-indicated in Wolff-Parkinson-White (WPW) syndrome because it decreases the conduction through the AV node but not through the aberrant pathway.
4. Digitalis can cause almost any cardiac arrhythmia except Mobitz type II heart block and atrial flutter.
5. Nesiritide is a recombinant BNP
6. ACE inhibitors and ARBs are indicated for all grades of CHF unless these are contraindicated.
7. The combination of hydralazine and isosorbide dinitrate has also been shown to decrease mortality in patients with CHF
8. The most widely used beta-blocker for CHF is carvedilol followed by metoprolol and bisoprolol.
9. Moxonidine and rilmenidine are congeners of clonidine with longer half-lives. These drugs are selective for imidazoline receptors.
10. Mecamylamine is a ganglion blocker used for smoking cessation.
11. Phentolamine and tolazoline are drugs of choice for hypertensive emergencies in clonidine withdrawal and cheese reaction.
12. Hydralazine is metabolized by acetylation and thus its effect is genetically determined due to the presence of slow and fast acetylation.
13. Prolonged administration of sodium nitroprusside can result in accumulation of cyanide leading to toxicity particularly in patients with renal disease.
14. Clevidipine is an ultrashort acting DHP, recently approved for hypertensive emergencies
15. Bradykinin is involved in the causation of dry cough and angioedema due to ACE inhibitors.
16. Verapamil can cause constipation and ankle edema.
17. Ranolazine has no effect on heart rate and blood pressure
18. Pentazocine and pethidine should not be used for myocardial infarction since these agents cause tachycardia and can worsen the symptoms.
19. Lignocaine is the drug of choice for digitals-induced ventricular arrhythmias
20. Amiodarone is the longest acting whereas adenosine is the shortest acting anti-arrhythmic drug
21. Vernakalant is a multi-ion channel blocker recommended for converting recent-onset atrial fibrillation to normal sinus rhythm.
22. Lomitapide acts by inhibiting microsomal triglyceride transfer protein (MTP). This protein is necessary for VLDL assembly and secretion in the liver.

Kidney

1. Ethacrynic acid is a highly ototoxic diuretic.
2. Amiloride is the drug of choice for lithium-induced diabetes insipidus.
3. Aldosterone antagonists act from the interstitial site of the tubular cell whereas all other diuretics act from the luminal side.
4. Thiazides are used for the treatment of patients with recurrent Ca++ stones in the kidney.
5. Furosemide possesses vasodilatory action which is responsible for the quick relief in LVF and pulmonary edema.
6. Acetazolamide, dorzolamide, and brinzolamide are non-competitive but reversible inhibitors of carbonic anhydrase

Endocrinology

1. Nafarelin and buserelin can be administered by nasal route.
2. Oxidation, organification, and coupling reactions are catalyzed by the thyroid peroxidase enzyme.
3. Propylthiouracil is the drug of choice for hyperthyroidism in the first trimester of pregnancy and in lactation. For all other patients, methimazole is preferred.
4. Lispro, Glulisine, and Aspart, all contain the letter ‘s’, which means short-acting.
5. Insulin degludec is longest acting insulin and unlike insulin glargine, it can be mixed with other insulins too.
6. Sulfonylureas (except glyburide) and meglitinides (nateglinide and repaglinide) are safe in renal failure.
7. Metformin is the drug of choice for type 2 diabetes mellitus.
8. Metformin is the only oral agent that has been demonstrated to reduce macrovascular events in type 2 DM.
9. Dexamethasone suppression test is used to test the intactness of HPA axis function and diagnosis of Cushing’s syndrome.
10. Progesterone is added to hormone replacement to decrease the risk of endometrial carcinoma.
11. Ospemifene is a new SERM indicated for dyspareunia due to menopause

Central Nervous System

1. Barbiturates are absolutely contraindicated in acute intermittent porphyria
2. Tasimelteon is a melatonin receptor agonist (like ramelteon) indicated for the treatment of non24 hour sleep-wake disorder in totally blind.
3. Tolcapone inhibits COMT in the periphery as well as the brain whereas entacapone acts only in the periphery.
4. Pramipexole and ropinirole are long-acting and do not cause gangrene. These are now the first-choice drugs for Parkinsonism.
5. Pramipexole and Ropinirole are used for the treatment of restless leg syndrome
6. Rotigotine is a dopamine agonist that can be administered through a transdermal patch but was discontinued due to crystal formation on the patches.
7. Rivastigmine is approved for the treatment of dementia due to Alzheimer’s disease as well as due to Parkinsonism’s.
8. Penicillamine and trientine can worsen neurological symptoms in Wilson’s disease, therefore are not recommended for initial neurological therapy.
9. Benzodiazepines (preferably lorazepam) are the drug of choice for status epilepticus.
10. Eslicarbazepine is a Na+ channel blocker (like carbamazepine) indicated for adjunctive treatment of focal seizures.
11. Carbamazepine is the drug of choice for partial seizures and trigeminal neuralgia.
12. Zonisamide and topiramate can cause renal stones.
13. Clozapine-induced convulsions are dose-dependent adverse effects whereas agranulocytosis is independent of dose.
14. Prazosin decreases nightmares and improves the quality of sleep in post-traumatic stress disorder.
15. Mirtazapine is also known as nor-adrenergic and specific serotonergic anti-depressant (NSSA).
16. Bupropion is used for smoking cessation.
17. Naltrexone is an opioid antagonist that can be used to reduce alcohol craving.
18. Fentanyl is responsible for post-operative muscle rigidity whereas succinylcholine causes postoperative muscle pain and fasciculations.
19. Pethidine is used to reduce shivering after anesthesia

Anesthesia

1. Adrenaline is added to LA to make them long-acting whereas sodium bicarbonate makes them fast-acting.
2. Dantrolene is the drug of choice for the treatment of malignant hyperthermia and is also useful in neurolept malignant syndrome.
3. Rapacuronium has been withdrawn due to reports of severe bronchoconstriction
4. Sevoflurane, Trilene, and methoxyflurane should not be used in closed circuit
5. Enflurane is contra-indicated in epilepsy as it can raise intracranial tension and produce tonic-clonic seizures.
6. Isoflurane is an inhalational agent of choice for producing controlled hypotension.
7. Xenon can be considered as an ideal inhalational anesthetic

Hematology

1. The antidote to acute iron poisoning is desferrioxamine (i.m.) whereas, for chronic iron overload, deferiprone (oral) is preferred.
2. Vitamin B12 is absorbed in the terminal ileum whereas iron is absorbed in the duodenum.
3. Aspirin inhibits thromboxane synthesis but does not inhibit the enzyme thromboxane synthetase
4. Vitamin K is involved in the activation of various clotting factors (like II, VII, IX, and X) as well as anti-clotting proteins (like protein C and S)
5. Warfarin may lead to dermal vascular necrosis and hypercoagulation as early appearing (3-10 days after initiation of therapy) adverse effects.
6. Rivaroxaban and Apixaban are new oral anticoagulants that act by direct inhibition of factor Xa
7. Reteplase and tenecteplase are known as bolus fibrinolytic

Respiratory System

1. Potassium iodide acts directly (by irritating bronchial glands) as well as indirectly (by gastric irritation) to increase bronchial secretions.
2. The only drugs effective for the treatment of an acute attack of bronchial asthma are bronchodilators
3. Umeclidinium (anticholinergic) plus vilanterol (Laba) combination is recently approved for maintenance treatment of COPD.
4. Anticholinergic drugs are bronchodilators of choice in patients of bronchial asthma on β blocker therapy.
5. Theophylline is a potent vasodilator and can cause hypotension which leads to reflex tachycardia.
6. Children clear theophylline faster than adults (require high dose) whereas clearance of theophylline is slower in elderly, premature infants, and neonates (require less dose).
7. Ketotifen has antihistaminic action apart from mast cell stabilizing property.

Gastrointestinal Tract

1. The major role of antacids in peptic ulcers is to provide prompt relief from ulcer pain.
2. Recent studies have suggested an increase in the risk of hip fracture in patients taking PPI in long term.
3. Antihistamines (H2 blockers) are more effective for reducing basal (nocturnal) acid secretion (histamine-mediated) than stimulated acid secretion (stimulated by gastrin, ACh, as well as histamine).
4. Sucralfate should not be given with antacids as it polymerizes only in an acidic medium.
5. A combination of doxylamine (antihistaminic) with pyridoxine (Vit B6) in high dose is the safest antiemetic drug in pregnancy
6. Domperidone decreases l-dopa induced vomiting without interfering with its efficacy
7. Atropine is added to lopermide to decrease its addictive potential.

Chemotherapy

1. Ampicillin should be avoided in patients with viral illness particularly EBV because it can cause a rash in these patients.
2. Nafcillin can cause neutropenia
3. Ceftriaxone and cefoperazone are secreted in the bile.
4. Cefazolin is the drug of choice for surgical prophylaxis.
5. Cefotetan, cefmetazole, and cefoxitin are active against anaerobes like Bacteroides fragilis.
6. Aztreonam is the only beta-lactam antibiotic that can be used in patients having severe allergies to penicillins or cephalosporins.
7. Cycloserine has potential neurotoxic effects (tremors and seizures). It also causes neuropsychiatric symptoms.
8. Chloramphenicol may lead to grey baby syndrome and bone marrow suppression.
9. All tetracyclines are excreted primarily in the urine except doxycycline. Doxycycline is excreted in the feces and thus can be used in the presence of renal failure.
10. Sulfisoxazole is the most soluble sulfonamide. Thus it has a minimum risk of causing crystalluria
11. Cotrimoxazole is the drug of choice for pneumocystosis and nocardiosis.
12. Gatifloxacin has recently been withdrawn from India due to its dysglycemic effects.
13. Isoniazid is metabolized by ACETYLATION which is genetically controlled. Slow acetylators are predisposed to toxicity, particularly peripheral neuritis.
14. Rifampicin is secreted in bile, so does not require dose adjustment in renal failure.
15. Ethambutol and streptomycin are NOT hepatotoxic
16. Rifaximin is a rifampicin derivative indicated for Traveller’s diarrhea (E.coli) and hepatic encephalopathy.
17. Dapsone is the drug of choice for the treatment of dermatitis herpetiformis.
18. Fluconazole is antifungal DOC for prophylaxis whereas voriconazole is DOC for treatment of febrile neutropenia
19. Acyclovir is the drug of choice for H. Simplex encephalitis
20. Nelfinavir is the only protease inhibitor for which ritonavir boosting is not recommended.
21. Prolonged use of high doses of chloroquine can result in blindness due to retinal damage (Bull’s eye maculopathy).
22. Mefloquine is effective as a single dose treatment of malaria
23. Artemisinins are the fastest-acting drugs against malaria.
24. Liposomal amphotericin B is the treatment of choice for visceral leishmaniasis.
25. Miltefosine and sitamaquine can be administered orally for kala-azar.
26. Albendazole is the drug of choice for the treatment of all nematode infestations including cutaneous larva migrans (creeping eruption), visceral larva migrans (toxocariasis), and neurocysticercosis except Enterobius (mebendazole), wuchereria and brugia (DEC), onchocerca and Strongyloides (ivermectin), and dracunculus (Metronidazole).
27. Pertuzumab is a monoclonal antibody against her-2/neu. It is used in combination with trastuzumab (bind to a different region of the her-2 receptor) for metastatic breast carcinoma.
28. Abiraterone acts by inhibiting 17-a hydroxylase and is indicated in refractory prostate cancer
29. Lenalidomide is approved for the treatment of mantle cell lymphoma and multiple myeloma

Conclusion

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