14-PHARMACOLOGY

receptor ligand gated/ch link/ionotropic(fastest) GABAAR(open Cl ch), nAChR, 5HT3R, GlyR Gprot coupled/metabotropic shape-serpentine(7memb) Gprot-GDP couple with Alp(Active),β,γ subunit adenyl cyclase pathw(cAMP) Gs(βadr) Gi(M2,M4,α2adr,βadr antag)↑ cAMP-TSHR, FSHR, LHR, ACTHR, PTHR, glucagonR, calcitoninR, adrenalineR,

vasopressinR(V2)↓ cAMP-DR

phospholiase C pathw(IP3,DAG) Gq(M1,M3,M5,α1adr) Gt(transducin)-generate signal in rod

small Gprot(monomer)-Ras prot enzyme linked insulinR(tyrosine kinase), GHR(janase kinase), prolactin(janase kinase), cytokineR, ANFR(cGMP), NO(cGMP) intracellular(slowest) Cytoplasmic-Corticosteroid, mineraloCorticoid

nucleus-testosterone, E, vitA&D, thy h grp I-nuclear recept grp II-surf recept

2nd messenger hydrophobic-DAG,IP3 hydrophilic-cAMP,cGMP gas-NO,CO,H2S

clinical trial(HECP) 0-microdosing I-Human pharmacology

Healthy Human volunteer safety&tolerance ADR pharmacodynamic

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pharmacokinetic II-therapeutic Exploration Efficacy III-therapeutic Confirmation Comparision with established drug IV-Postmarketting suveillance

ADR/toxicity

pharmacogenetic-genetic basis for variable response pharmacogenomics-genetic information to guide DOC pharmacognosy-drug fr plant pharmacovigilance-detection, assessm, understand, prevent ADR

pharmacodynamic&pharmacokinetic 0 order kinetic indep of-pl conc ED50-potency area under time&pl conc-pl clearance loading dose-vol distribution maintenance dose-clearance chloroquine, digoxin, doxycycline, long acting sulfonamide, phenylbutazone, lignocaine(short t½) Li excreted by kidn, not metab

oscillatory response-+ve feedbackentrOPy not change-OPen system

biotransformat rxn phase I(non synth) rxn oxidation(MI-cytP450), reduction, hydrolysis, cyclization, decyclization

phase II(synth) rxn acetylation, glucuronide conjugation, Gly conjugation, SO4 conjugation, methylation, nucleotide synth

→ less polar more polar

bioavailability extensive 1st pass metab-oral route drug-bioavailability(%) bisphosphonate,remelteon=2 furosemide=60 sotalol,pindolol,penbutolol=100

Acidic drug-Albumin basic drug-α1glycoprot

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preparation-drug capsule hard-tetracycline soft-vitE sustain release-theophylline time release-indomethacin

depot preparation-flupentixol, fluphenazine, haloperidol, imipramine, risperidone ETT-adrenaline, atropine, diazepam, naloxone, lignocaine ID-BCG vacc inhaler aerosol-salbutamol, beclomethasone dry powder-salbutamol gas-GA spinhaler-diNa chromoglycate desmopressin, liposome, butorphanol, zanamivir, calcitonin

intravitreal-bevacizumab, foscarnet, ganciclovir, ranibizumab, pegaptanib nasal spray-sumatriptan SC-sumatriptan, morphine, vitB3, exenatide SL-isosorbide diNO3, buprenorphine, ergot amine tartrate, isoprenaline, nitroglycerine, desaminooxytocin, clonidine, nifedipine suppository-diclofenac, indomethacin, aminophyllin, diazepam, metronidazole, chlorpromazine, bisacodyl, glycerine, morphine, ergotamine, paracetamol tablet chewable-ergotamine tartrate, acarbose, Al(OH)3, Mg trisilicate double strength-cotrimoxazole enteric coated-bisacodyl mouth dissolving-ondansetron sugar coated-metronidazole sustain release-pyridostigmine, morphine, diclofenac, theophylline, pinacidil,

prazosin, pentoxyphylline uncoated-amlodipine

transdermal-fentanyl, nicotine, nitroglycerine, estradiol, hyoscine, rotigotineability of vehicle to retard evaporation fr skin ointment> foam> cream> paste> powder> aerosol> gel> lotion> wet dress> tincture

liposome anticancer drug-daunorubicin, vincristin, camptothecin, mtx, cisplatin, mitoxantron antifungal-amphotericinB, nystatin antibiotic-amikacin, ampicillin, ciproflox, ribavirin, ganciclovir, chloroquine other-IL2, cyclosporine

food

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↑ -CBZ, chloroquine, griseofulvin(fatty), halofantrine, LiCO3, nitrofurantoin, vitB2, spironolactone↓ -ampicillin, aspirin, captopril, digoxin, furosemide, hydrochlothiazide, INH, Ldopa,

penicillinG, phenytoin, rifampicin, tetracycline

drug with extensive 1st pass metab V-Verapamil P-Propranolol Singh-Salbutamol Not-Nitroglycerine A-Amitryptyline Popular-Propoxyphene P-Pethidine M-Methyltestosterone

drug with low 1st pass metab Phenobarbitone Phenylephrine Pindolol Theophylline Tolbutamide

ts-drug conc adipose ts-thiopentone, ether, minocycline, phenoxybenzamine, DDT bone,teeth-tetracycline, heavy metal, bisphosphonat brain-chlorpromazine, acetazolamide, INH iris-ephedrine, atropine kidn-digoxin, chloroquine, emetine liver-chloroquine, tetracycline, emetine, digoxin retina-chloroquine sk m,heart-digoxin, emetine thy gld-I2

drug-source cephalosporin-fungus colistin-bact griseofulvin-fungus penicillin(fung) discover fr-Penicillium notatum now develop fr-P chrysogenum

→ → → αKG+acetylcoA homocitrate αaminoadipic acid Lys+penicillin Rifamycin-Streptomyces mediteRRanei streptomycin-Streptomyces griseus

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tobramycin-Streptomyces tenebrarius

drug causing hemolysis in G6PD def A-Aspirin D-Dapsone Na-Nalidixic acid N-Nitrofurantoin Sami-Sulfonamide Pe-Primaquine,Phenacetin M-Menadione(vitK3) C-Chloroquine Q-Quinine

drug causing hyperpigmentation(CCAM) Chlorpromazine Clofazimine Amiodarone Minocycline

drug causing disulfiram like rxn C-Chlorpropamide, Cefoperazone, Cefamandole, Citrate Ca carbamide, Cyanamide, animal Charcoal M-Metronidazole Praised-Procarbazine G-Griseofulvon T-Tinidazole Naidu-Nitrofurantoin

drug causing deafness(BEDEAFM2C2Q) Bleomycin Ethacrynic acid Desferoxamine Erythromycin Aminoglycoside Furosemide Minocycline Mustine Chloroquine Cisplatin Quinine

enzyme inducer G-Griseofulvin

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P-Phenytoin R-Rifampicin S-Smoking Cell-CBZ Phone-Pnenobarbitone

enzyme inhibitor Vitamin-Valproate K-Ketoconazole Cannot-Cimetidine Cause-Ciprofloxacin Enzyme-Erythromycin Inhibition-INH grape fruit juice

drug metab by acetylation(SHIPCD) Sulfonamide Hydralazine INH Procainamide,PAS Clonazepam Dapsone fAsT acet-hepATiTis sLOw acet-peripheraL neurOpathy

drug with low therapeutic index V-Vancomycin C-Clonidine D-Digoxin P-Phenytoin Layer-Lithium G-Glipizide I-Imipramine F-Flucytosine T-Theophylline

drug with 0 order kinetic Zero-Zidovudine W-Warfarin A-Aspirin T-Theophylline T-Tolbutamide Power-Phenytoin

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drug causing pulm fibrosis amiodarone, bleomycin, busulfan, Au, mtx, cyclophosphamide, methysergide, nitrofurantoin, phenytoin

drug causing cataract Au(gold),Amiodarone Busulfan Chlorpromazine Dexamethasone(oral) Echothiophate,pilocarpine

drug ppt a/c interm porphyria barbiturate, OCP, griseofulvin, estrogen, chlorpropamide, phenytoin, rifampicin, sulfonamide

drug inh nephrogenesis ACEI, ARB, dexamethasone, gentamicin, NSAID

drug cause peptic ulcer bisphosphonate, CT, clopidogrel, cocaine, steroid, mycophenolate mofetil, KCl

prophylaxis TB child-INH(5mg/kg)×6mth posttrauma myelopathy-methylprednisolone(30mg/kg<3h) 75mg/d-aspirin, clopidogrel, oseltamivir, amiodarone 75mg/w-mtx

chemical Adrenalectomy-Aminoglutethimide pancreatectomy-streptozocin defibrillator-bretylium

antibiotic SMR(MAQ) Macrolide Aminoglycoside(neomycin) Quinolone

orphan drug Na nitrite, fomepizole, liposomal amphotericinB, miltefosine, rifabutin, succimer, somatropine, digoxin immune Fab, liothrionine

GnRH agonist(A-F&HIP) A-Adenomyosis

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B-irritable Bowel synd C-Ca Breast(tamoxifen+GnRH agonist) D-DUB E-Endometriosis F-Fibromyoma uterus H-Hirsutism I-Infertility P-Precocious puberty

topical steroid potency betamethasone diproprionate> betamethasone valerate> clobetasol propionate> hydrocortisone butyrate

antiHTN drug lipid hostilE-βblockEr, thiazidE lipid neutral-ACEI, ARB, CCB, indapamide lipid friendly-doxazosin, prazosin erectile dysfn highest risk-diuretic high risk-atenolol, carvedilol,metoprolol↓ risk-ACEI

antibiotic acting on cell wall βlactam antibiotic vancomycin teicoplanin bacitracin cycloserine fosfomycinantibiotic acting on cell memb polypeptide-polymyxinB, polymyxinE(colistin) polyene antifungal-amphotericinB azole antifungal-ketoconazole allylamine-terbinafine

antimicrobial sensitivity method disc diffusion

broth culture with break pt potency Min Inh Conc(MIC)-lowest conc which prevent visible growth of bact Min Bact Conc(MBC)-kill 99.9% bact↑ MBC–MIC-bacteriostatic

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↓ MBC–MIC-bactericidal

warfarin INR=ptPT/contrPT=2-3, prosthetic valve=2.5-3.5, long term=1.5-1.9

paracetamol does not stimulate respiration affect acid base balance cause gastric irritation have CVS affect affect PLT fn cause uricosuria

pethidine(meperidine)→ hydrolysis meperidinic acid(maj), inh by MAOI producing more demethylation→ → demethylat norpethidine(min) sz

opioid recept endorphin(μ),enkephaLin(DeLta)

↑ P-Physical dependence, Prolactin M-Miosis C-Constipation,Convusion(M3G) A-Analgesic(spinal,supraspinal) R-Resp depression E-Euphoria S-Sedation

Dynorphin(κ) D-Dysphoria M-Miosis A-Analgesic R-Resp depression D-Diuresis S-Sedation

Muscle rigidity-Mu

digitalis↑ toxicity-hypokalemia, hypercalcemia, hypermagnesemia, ren failure

CFTR corrector-lumacaftor-correct trafficking defect potentIator-Ivacaftor-open Cl ch

drug act on

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↓ cortical part nephron- +ve H2O clearance↓ medullary part- –ve H2O clearance

βadr antag loNgest-Nadolol Shortest-eSmolol c/i ren fail(PANS)-Pindolol, Atenolol, Nadolol, Sotalol H2O soluble-ANS lipid soluble(MP3)-Metoprolol, Pindolol, Propranolol(max), Penbutolol hep elimina(LMP)-Labetalol, Metoprolol, Propranolol memb stabilising(LMPTAPCB)-Labetalol, Metoprolol, Propranolol(max), Timolol, Acebutolol, Pindolol, Carvedilol(max), Betaxolol no memb stabilising-bevantolol acebutolol-cardioselective, partial agonist, memb stabilising, lipid insoluble CHF-Carvedilol(α1+β1+β2) 100% bioavail(PPS)-Pindolol, Penbutol, Sotalol mAx prot bind-cArvedilol mIn prot bind-celIprolol l isomer-propranolol, atenolol, esmolol, metoprolol, timolol d isomer-nebivolol

iron dextran-IM, IV, high molec wt, 10-30% get locally bound, no excret, absorb through lymphat, not bound to transferrin iron sorbitoL citric acid-IM, Low molec wt, not locally bound, 30%excret in urine, absorb directly in circulat, bound to transferrin parenteral Fe req=4.3×body wt(kg)×Hb deficit(g/dl)

gramicidin A:B:C=80:6:14=D(linear pentadecapeptide 15AA chain) S-cyclic peptide chain G+ve bact(except G+ve bacilli), N gonorrhoea

BDZ midbrain ascending reticular formation, limbic Medulla-M relaxation cerebellum-ataxia

↑ ↓ sleep- stage2, REM,stage3,4↑ nitRazEpaM- REM

SMR-clonazepam, diazepam anticonv-clonazepam, diazepam, nitrazepam, flurazepam coronary dilatat-IV diazepam

↓ analgesic, nocturn gastric secretion, stress ulcer-diazepam

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tamoxifen E antag-Breast,Bld vess E agonist-uterus,bone,lipid

dopamine dose(μg/kg/min)-action low(1-2)-renal&mesenteric vasodilat moder high(2-10)-β1adr agonist, +ve ionotropic high(>10)-α1adr agonist, vasoconstrict

steroid 0mineralocort-triamcinolone, paramethasone, dexamethasone, betamethasone 0glucocort-DOCA(DeOxyCorticosterone Acetate) most potent glucocort-betamethasone least potent glucocort-cortisone max mineralocort-aldosterone> fludrocortisone> DOCA max glucocort-dexa&betamethasone hydrocortisone:prednisolone:dexamethasone= 1:4:40

advantage 2nd gen antihistam less-sedation, interaction with alcohol, psychomotor disturb

FDC malaria-artemether+lumefantrine

Abbreviations a-artery, AA-amino acid, abtc-antibiotic, AI-autoimmune bef-before, bel-below, b/l-bilateral, bld-blood, b/n-between, bn-benign, br-branch, Bx-biopsy ca-carcinoma, carb-carbohydrate, c/i-contraindication, c/l-contralateral, conc-concentration, cong-congenital, Cx-cervix d-day, def-deficient, ds-disease, d/t-due to, Dx-diagnosis E-estrogen fem-female, fr-from gld-gland, glu-glucose h-hormone idiop-idiopathic, i/l-ipsilateral, inf-infection, inj-injury lig-ligament, LL-lower limb, l/t-leading to m-muscle, maj-major, mal-male, MC-most common, met-metastasis, min-minor, mtx-methotrexate, Mx-management n-nerve, norm-normal P-progesterone, pl-plasma, prot-protein, pt-patient Rx-treatment SCC-squamous cell carcinoma, sr-serum, Sx-surgery, sz-seizure tm-tumour, ts-tissue UL-upper limb, u/l-unilateral vag-vagina, VC-vocal cord, vel-velocity, vert-vertebra, vit-vitamin, vol-volume w-week, wt-weight

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Xr-X ray y-year #-fracture °-degree

THESE NOTES ARE ONLY FOR THE PURPOSE OF GUIDANCE AND HELP TO PG ASPIRANTS, NOT FOR COMMERCIAL OR OTHER PURPOSE. REFERENCE HAS BEEN TAKEN FROM VARIOUS STANDARD TEXTBOOKS.

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