Category Archives: Pharmacology

Mechanism of action of fluoroquinolones

Fluoroquinolones act by inhibiting nucleic acid synthesis of bacteria.These drugs inhibits the action of DNA gyrase(Topoisomerase II) and Topoisomerase IV which are essential for removing supercoils formed during  DNA replication,when replication fork proceeds downstream

Anti tumour Monoclonal antibodies

Monoclonal antibodies against tumour cells mainly act via antibody dependent cellular cytotoxicity. They also act via complement mediated lysis and by induction of apoptosis. Drugs Rituximab – CD20 – Non Hodgkins Lymphoma Ibritumomab -CD20 -NHL Tositumomab- CD20- NHL Ofatumumab -CD20 …

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Anti arrythmic drugs classification

Anti arrhythmic drugs are classified into four main classes. Class I – Sodium channel blockers(act on Phase 0) Class II – Beta blockers(act on phase 4) Class III- Potassium channel blockers(act on phase 3) Class IV – Calcium channel blockers(act …

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Adverse effects of Amioderone

Hyper/Hypothyroidism Peripheral neuropathy Myocardial depression Lung fibrosis Liver toxicity Corneal microdeposits Photosensitivity

Selective Beta1 blockers

Mnemonic: Beta Blockers Acting Exclusively At Myo Cardium Beta- Betaxolol Blockers-Bisoprolol Acting-Atenolol Exclusively- Esmolol At- Acebutolol Myo- Metoprolol Cardium- Celiprolol

Anti tubercular drugs

Bactericidal Rifampicin INH Streptomycin Pyrazinamide Bacteriostatic Ethambutol Thicetazone PAS Cycloserine

Drugs causing Pancreatitis

Drugs causing pancreatitis are: Mnemonic:12345 1 -ACE inhibitors 2 -Didanosine 3 -Trimethoprim 4 -Tetracycline 5 -Pentamidine

Corticosteroids

Zona Glomerulosa-Mineralocorticoids Zona Fasciculata-Glucocorticoids Zona Reticularis-Sex corticoids GFR from outside to inside. Points to remember Maximum glucocorticoid activity- Dexamethasone Maximum mineralocorticoid activity- Aldosterone Glucocorticoid with maximum mineralocorticoid action-Hydrocortisone Least potent Glucocorticoid- Cortisone Most potent Glucocorticoid- Betamethasone Selective mineralocorticoid action(zero glucocorticoid …

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General anaesthetics

This is the most confusing topic in Pharmacology,because of the similarity in names of drugs and mechanisms of actions this topic can be considered even more difficult to master than Skeletal Muscle relaxants. Inhalational agents N2O maximum MAC and minimum …

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Local anaesthetics

Classification Ester LA’s Cocaine(first used LA) Procaine(LA of choice in malignant hyperthermia) chlorprocaine(Shortest acting) Tetracaine Benzocaine Amide LA’s Lignocaine Prilocaine(Methemoglobinemia) Bupivacaine(Most cardiotoxic) Dibucaine(Longest acting) Mepivacaine Etidocaine Ropivacaine Properties of LA’s All LA’s are weak bases,so sodium bicarbonate speeds up the …

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Skeletal muscle relaxants

This topic falls into one of the most confusing parts in pharmacology, the names,duration of action etc can be confusing. Some of the names we come across very often are: Succinyl choline(Analogue of acetyl choline,acts on nicotinic Nm receptors) Pancuronium …

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Drugs causing methemoglobinemia

Aniline Aminophenones Chlorates Dapsone Prilocaine/benzocaine Nitrates/nitrites/napthalene Nitrobenzene Phenazopyridine Primaquine and related antimalarials Sulfonamides

Cephalosporins

First generation Parenteral: Cephalothin,cefazolin Oral: Cephalexin,cefadroxil,cefaridine Acts on gram positive cocci Second generation Parenteral: Cefuroxime,cefoxitin Oral: Cefaclor,Cefuroxime Most active against gram negative organisms cefuroxime higher CSF concentration Third generation Parenteral: Cefotaxime,ceftizoxime,ceftriaxone,ceftazidime,cefoperazone Oral: Cefixime,Cefpodoxime,cefdinir Highly active against gram negative enterobacteriacea Ceftyazidime …

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ACE inhibitors

All ACE inhibitors except captopril and lisinopril are prodrugs Enalapril—->Enalaprilat Enalapril has a half life on 1.3 hours only but enalaprilat has a halflife of 11 hours Lisinopril is lysine analogue of enalapril with half life of 12 hours. All …

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Alkylating agents

Transfer alkyl groups to various cellular constituents causing cell death. Alkylating agens—->cyclization—->Immonium ion/cabonium ion—–>transfer alkyl group. Major site of alkylation is N7 position of guanine with DNA. There are five major categories of alkylating agents. Nitrogen mustards Cyclophosphamide Mechlorethamine Chlorambucil …

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Digitalis toxicity

Precipitated by: Hypokalemia Hypomagnesemia Renal insufficiency Advanced age Myxoedema Hypoxia Acute MI Hypercalcemia Thyrotoxicosis Quinidine and calcium channel blockers Furosemide,thiazide,amphotericin B cause hypokalemia Note that all the factors precipitating digitalis toxicity are hypo states except hypercalcemia and thyrotoxicosis. Digitalis toxicity …

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Cholinergic and anticholinergic

Organophosphates and Atropine comparison Organophosphates are classical cholinergics. Cholinergics (eg: organophosphates) effects If you know these, you will be “LESS DUMB”: Lacrimation Excitation of nicotinic synapses Salivation Sweating Diarrhea Urination Micturition Bronchoconstriction Atropine is the classical anticholinergic So anticholinergic overdose …

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Drugs increasing QT interval

I Imipramine C Cisapride H Haloperidol E Erythromycin A Amitryptiline and Amiodarone T Terfenidine Mnemonic:I CHEAT

Drugs and Pharmacokinetic interactions

Antacids Bile acid sequestrants Reduced absorption Antacids/tetracyclines Cholestryamine/digoxin Proton pump inhibitors H2-receptor blockers Altered gastric pH Ketoconazole absorption decreased Rifampin Carbamazepine Barbiturates Phenytoin St. John’s wort Glutethimide Induction of hepatic metabolism Decreased concentration and effects of warfarin quinidine cyclosporine losartan …

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CYP3A inhibitors

CYP3A Calcium channel blockers Amiodarone Antiarrhythmics (lidocaine, quinidine, mexiletine) Ketoconazole, itraconazole HMG-CoA reductase inhibitors (“statins”; see text) Erythromycin, clarithromycin Cyclosporine, tacrolimus Ritonavir Indinavir, saquinavir, ritonavir

Drugs and side effects

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Cell cycle Specific anticancer drugs

G1-Vinblastine S-Methotrexate,Mitomycin C,Doxorubicin,Daunorubicine,Cytarabine,Hydroxyurea,6MP,6TG,5-FU. G2-Daunorubicin,Bleomycin,Etoposide,Topotecan M-Vincristine,Vinblastine,Paclitaxel,Docetaxel

Mechanism of action of drugs

I.Cellwall synthesis Inhibitors 1.Beta lactams Penicillins and cephalosporins Inhibit cell wall cross linking. 2.Vancomycin 3.Bacitracin II.Inhibitors of protein synthesis Bind to 50 S subunit Macrolides-Erythromycin Lincosamides-Clindamycin Chloramphenicol Quinupristin/Dalfopristin Linezolid Bind to 30S subunit Tetracycline-Binds to 30 S subunit Aminoglycosides-Gentamycin-Bind to …

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Drugs causing Hyperkalemia and Hypokalemia

Hyperkalemia ACE inhibitors NSAID’s Heparin K+ Sparing Diuretics Trimethoprim Pentamidine Cyclosporine Hypokalemia Amphotericin B Penicillin derivatives Corticosteroids Diuretics Gentamycin Insulin Tetracycline Theophylline Carbenoxolone

Protein Synthesis Inhibitors

Drug and the step in protein synthesis they inhibit. Streptomycin- Initiation Tetracycline-Elongation Binds to 30 s Puromycin-Elongation Chloramphenicol-Elongation Clindamycin-Translocation Erythromycin-Translocation

Opioid’s

Exogenous opioids like Morphine and heroin can induce euphoric mood. Exercise released endogenous opioids  and is associated with mood enhancement. Beta endorphin is principal endogenous opioid. Analgesia and alteration of pain perception is the best documented function .

Anti Tuberculosis drugs.

Isoniazid(INH) Inhibits mycolic acid cellwall synthesis  via oxygen dependent pathways. Bactericidal to both extracellular and intracellular organism SE:Peripheral neuritis,seizures,hepatitis,optic neuritis,hemolysis in G6PD deficiency,SLE like syndrome. Pyridoxine 10mg orally given as prophylaxis for optic neuritis. INH-Is Hepatotoxic and Neurotoxic. Rifampicin Blocks …

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Drugs which follow zero order Kinetics

Mnemonic:Zero WATT Power Zero- Zero order Kinetics followed by W-Warfarin A-Aspirin and alcohol T-Theophylline T-Tolbutamide Power-Phenytoin

Enzyme Inducers and Inhibitors

Enzyme Inducers Enzyme Inducers increase the metabolism of other drugs. Mnemonic:GPRSCell Phone G-Griseofulvin P-Phenytoin R-Rifampicin S-Smoking Cell-Carbamazepine Phone-Phenobarbitone As you can see most of the antiepileptic drugs cause enzyme Induction,just like inducing an episode of epilepsy! Enzyme Inhibitors Decrease the …

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