Post on 02-Apr-2018
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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