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(@Preptadder } or. Gobind Rai Garg Structured Notes PHARMACOLOGY Revision friendly Fully Colored Notes For best results, watch the video lectures along with reading notes Lay Dr. Gobind Rai Garg at 3 g a 2 a x E = i | Zz Q Ee = a a“ Ee 12 a we ° 2 = 9 a w 2 a 3 a o Ed ya eB SCTE CCN Tole Cme Coeeiee eR CORT ol aE Ren alms) ses EVAR eet teul fo) dara (60) " K by eT 1Mer lee gel mica) Structured Notes PHARMACOLOGY Revision friendly Fully Colored Notes For best results, watch the video lectures along with reading notes ISBN: 978-93-50901-94-6 © Dr. Gobind Rai Garg All rights reserved of these notes are reserved under Indian Copyright Act, 1956. No part of this publication may be reproduced stored in a retrieval system or transmitted, In any form or by any means electronic, electrical, chemical, mechanical, optical, photocopying, recording or otherwise, without the prior permission of the copyright owners. Indian Reprographic Rights Organization (IRRO), acopyright society registered under the Copyright Act, permits only up to 15% of a copyrighted work to be reproduced. Also, the usage should be non-commercial and non-profitable. Photocopying the whole book/uploading PDFs or images of the book without the due permission of the copyright owner is punishable under the copyright act as it weighs against the fair use policy because completely copying and distributing the work for free Online and physically would hinder the economic viability of creating and maintaining the source. Any person/organization found doing photocopy/PDF circulation, we would take strict legal actions against the alleged without any prior notice. PREFACE Pharmacology Structured Notes by Dr. Gobind Rai Garg are only for rapid revision purposes and are in no way a replacement of “Review of Pharmacology” book by Dr. Gobind Rai Garg. For effective preparation you must still study the reference book. For best results you must study these notes along with Dr. Gobind Rai Garg ‘s videos on PrepLadder app. For maximum gain, revise Pharmacology Structured Notes by Dr. Gobind Rai Garg multiple times. At the time of examination, going through Structured Notes would be advisable rather than reading the reference book In case of any discrepancy between notes and videos, always trust Dr. Gobind Rai Garg’s videos on PrepLadder. The copyright of ‘Pharmacology Structured Notes by Dr. Gobind Rai Garg’ belongs to the author and any attempt to reproduce or replicate it in any form will result in a legal action without prior warning. a With decades of experience in teaching, they're all considered to be the best faculty Ce Cee Ratoni ra een PRE CLINICAL SUBJECTS Ae es ea Paes aa eon) Cen pM ri Can ened Ceturc Peace) cee Microbiology pccaad MAIN CLINICAL SUBJECTS oe Peer en Carrs Pay es rea Coca) Oo Dr. Meenakshi Bothra Pod Peace ead es cn HORT SUBJECTS Pataca) Peo Paley ed ead een A @ . Pasa Pau) ec Pc cad eerie) GENERAL PHARMACOLOGY o1 Pharmacokinetics - Absorption Distribution 01 Pharmacokinetics — Metabolism , Excretion & calculakions 04 Pharmacodynamics = 1 08 Pharmacodynamics - 2 11 Plasma concentration vs Time graph 13 [1ypes OF Drug Antagoniam 13 Types OF emayme inhibitors 14 exp substrakes 14] Combined effete OF drugs 15 AvTONoMmIC NERVOUS SYSTEM 16| Cholinergic _prugs 16] Anti cholinergic orvgs 21 Adrenergic drugs 22 Anti Adrenergic drugs 27 Active & Passive mydriasis 31 Glaucoma 31 CARDIO VASCULAR. SYSTEM 35 congestive Heart failure 35| Angina pectoris . Myocardial infarction 37 Hypertension 44 Brrhythenias 44| Dyslipidermia. 46 Pulmonary Hypertension 48 coronary steal Phenomenon 49 Management OF Shock 49} Krpney 50 kadney 50) RESPLRATORY SYSTEM 53 Respirabory system 53| GAGTRO INTESTINAL TRACT 54 Gastro Intestinal Troe 5a Loxotive Purgabivec 58 ENDO cRINE System 60 Pituitary — Hypotbalamic system & Thyroid 60) Pancreas 65 Adrenal 69 OsteoporesiS.. SERMS & acPs 72 Mifepristone 76 Antenatol steroids 7 Neturol_ estrogens 7 Progesterone s 7 CENTRAL NERVOUS SYSTEM) 78 Sedative — Hypnotics & Parkinsonism 78 |Epilepsey 81 Psychiatric Lilnese 84 Opioids @ alcohols 88 HEMATOLOGY 92 Hemakologt 92 ANTE MICROBIAL DRUGS 97 Cell wall synthesis Inhibitors 97 Protein synthesis Inhibitors 102 Anti merobolites & @uvinolones 105 Mycobacterial Dizenkes 108 Malaria & Anti virols other than HIV 4141 Anti HIV, Anti Fungo! G Anti parasitic Orogs 114 BNITCANCER._& _LIMONOSUPPRESSANTS 119 Cytotoxic anticancer Drugs 119 Targezed anticancer Drugs & Irmmunosuppressants 123 AuTOCOLDS 129 HISTAMENE, 5-HT_& PGS 129 NSALDs, Gout &| Rheumaboid arthritis 132 Recent advances in migraine 136 Mechanigm oF colchicine 137 PNAESTHESTA, 138 Anaesthesia 138 MISCELLANEOUS 143.| Chelating Agents 143 PHARMEKO KENETECS 7 EFFeck OF body on Brug PHARMAKO DYNAMICS > EFFect OF Druq on Body PHARMACOKINETICS > aka Ape sty - Absorption ~ Distr bukion ORAL ~ Metaboligen RouTe ~ exeretion ABSORPTION 7 MOVEMENT OF DRUG FROM SITE OF ADMLNISTRATIDN TO BLOOD. 7% LAPLD SoLUBELETY - single most important Fatkor in absorye” ~ LIPLD SOLUBLE BPRUGS ARE ABSORBED > Fort oF DRDg Ho == tt on” HK —— sot x? ~ Tonined form oF Drug is cooker soluble — Non Tonized form oF Drug ig Liptd soluble — PRLG Is ABSORBED IN NON - JONIZABLE FORM > MEDIUM ‘~ WHEN THE MEDIUM TS SAME, THEN THE DRUG WILL CRoss DROG Mebrom Form | setosrurry cRosS Radic Rade Non ionized Liptd seluble v Basic Basic Non ionized Lipid Soluble v Radic Basic toniaed Waker Soluble x Bosic Acidic tontaed Water coluble x — Acidic Drug [ASPLRIN] + moinly absorbed from stomoch ~ Basic Oruq [MORPHINE] mainly absorhed from iniestine Bro AVATLABLLITY molecules > FRACTION OF GIVEN DOSE WHICH REACH ow SYSTEMIC CERCULATION > Bio Availability DP Wiis + dekermines the DOSE High bioavailability Low dose Low bicawoilobility 7 High close Excreted Fockors © Absorption Tabsorpt? >t‘ Bio availability fabsorpt? = + Bio Ourailabilihy Bioavailabiliky oF drugs qiven by IV rou [z 100% First Pass mitabolism | Pre systemic oli ge ! 7 mukosbs 4 Firsk Pass mikabolitm —% 4 Bio avoilability {First Pass mikabolitm > 7 Blo availability NT@ L Nitro qlyarine] ~ hes high first poss mubabolism SUB LINGUAL ROUTE ig prefered Advantages ~ Fast atking > can be used in erurgensts — No first pass mukaboligen — self odminishor® '¢ possible After desirable atkion . we con spit] ingest the extra doze DISTRIBUTION Factors | a © pw sowwerliTy > mest important factor Lipid Soluble Drugs Higher Dishribukion DISTRIBUTION Woke soluble Drugs > Lower biatribulion @ PuasmA PROTEIN BINDING Tt PPB > Lovo distribukion @ Barriers BBB CIRCoM VENTRICULAR ORGANS [ No Blood Brolin Borria] ctz Cowmoreupter Trigger 20ne] cee vomiting net comted by > Anti emebics cee nti Psyehofes alto has anti emetic property VOLUME OF DIGTRIBUTION Vag AMOURE given by IV Plasma Conantrakion. Vd > cases > case > cases - joomg 4 VOLUME OF DISTRIBUTION Vy % Pc Va Nd Pe Nd 190 10 = 2omqfL 10 mq |. " 3 C a mq it = 50L FMOUNT OF DRUG IN TESSUES more distribution more vg > CHLO RO QULNE Drug & maximum vg [7130013 mosHy dittributed fn Liver Bur Sil OF preferred action ig RBC LODING DOSE Lio) — Inittol high dose given to start the prefered action MAIN’ Lonpene, bese RESTS 1000 xy ™olecuby oF Drug {D = _Vq % Targe’ Plasma conantrakion TALNANCE DOSE LD depends on Uy x Torgek Plasma concnat” — weisermmuante Mp depends on clearance & Tore: plasma conc. Doce |. os MD = Clearance x Target Plogma cone <2 ey METABOLISM,EXCRETION ELIMINATION + Termination oF atkion of rq = > ELIMINATION > includes Metabolism e Excretion Metabolism FATE OF meTABOUSI © Active — ative @ active — Active DIAZEPAM —> OXAZEPAM @ Anative —> Active ‘LRoDRUG] LevopoPA «>A ER OF Parkinsonism ] Im of METABOLISM > To MAKE A DRUG WATER SOLUBLE PHASE 1 REACTLONS PHASE 11 REACTIONS > purpoge of PHASE > makes the drug Woker Soluble “> Purpose of PHASE T > maket Functional Group to attach the drug Water Soluble ENZYMES > pivided into Micro somal Enzymes > inside the microsomes Non micro somal > duk side the microsomes > erosome Cendoplasmic reticulum 2 > only Microsomel emymer con be Induced or inhibited WARFARIN, HEPARIN] case 100 Broq, 100 Broq 5D microsomal 50 non microsomal Enaymes [>| = Enaymes imeem eat + 50 Drug 50 prog cASER > long T RIFAMPICIN Lemayme inducer] - Me — ame = soNmE —> 50 NME 100 Sroq, 100 Broq 90 microsomal 50 non microsomal) Ve Enaymes [>| +30) Enzymes eeememe lane #0) to Brug 50 prog ~ rug dose & be intrensed — No change required CAGER > Along T CLMETLOLNE Lemyme inhibitor] - ME — tome — 5oNmE =—? 50 NME 100 Oreq, 100 Brog 10 microsomal Js> non microsomal Enaymes ||" +9) Enaymes ieeemee |e +89) 10 Drug 50 org — prug dose & be deerensed = No change required ENZYME INDUCERS ENZYME INHIBITORS gq a _ vit VALPROATE Pp k KETOCONAZOLE R | Con? CIMETEOINE s | | Cause CIPROFLOXACIN cell Do] Gnagme ERYTHROMYCIN Phone ol Inhibit? ISONTAZEDE most of anti epllephcs > ENzYME INDUCERS most oF anti biotice > ENZYME INHIBLTORS ExcRErton GLOMERULAR FILTRATION > Lipid soluble drugs filtered easily Water soluble drugs also Filtered > Filtration L Plasma Protein binding > @eR = wmIjmin = 5 ter|br " ~ aso Ler] oays + @ourpur oF urine + aLloay TUBULAR RERBSORPTON + (997 OF GAR ik Teabsorbed — Lipid soluble droge reabsorbed — Water soluble drugs excreted + drug absorbed > of drvq & media are same rerent > drug not absorbed drug & media. ore + rctdic drvq poiconing CAspisin] R by Nalco, TFored eikaline Divresis] Alkaline drug poisoning Camphetamine 5 Ry by NH,Ci [forced acd pivresis] TUBULAR SECRETION > die purmps | transporters in proximal tubules 7 These transporters are SATURABLE — Penicillin is short acting — Benicillin + Probenecih % bong acking — Probenecid haz higher affinity for Eronsperies a Prevents Penicillin secretion SOME MORE FORMULAS RATE OF ELIMINATION LR] > incomplete parameter R > Bmounk oF brug Eliminared Time crearance [cul > comple. parometer la eR Pe = Plasma Concehkation Pe Howe Lee Ley,1 100 boty 50 dite as ft RS Io tia. 6.35 > by, For most drugs is constant @ ty, = ehrs , after 1 doy How much dreq remained in body > a= 7 How Much druq eliminated from body > GD 7 pese cant be calculated DOSING INTERVAL | FREQUENCY can be known F tyg & volume OF distribution [vy] ty 4. dearance ln es va la 0.693 x 3S ORDER of KINETICS FIRST ORDER KUNETECS ‘LeRO OROER KINETS > Froction ig constant 7 Amount ig constant pnst onpen Pa R a ey w es Jive Bole y hr 020] [ashe 50 Q + L t 1 dibr sib ‘a Ibe oas | abr 35 J 4 J JL L | thr 6} br Ya tbe 023 15 be as 4 4 1 JL J Libe | | eatsjhr ‘ the oso} [iby 635 R 4 PC = Constant tly = constant > moyority drugs follow Firet order Kinetes DRUGS FOLLOWING JERD ORDER KINETECS are Zeno > ZERD ORDER Kanlerteé a OS 5 + > i i >| poser | REASON > order oF Kinekics depends on Enayme Soburakion + te ensymes ore abundent —> follow 1st ordar Kinekice > ip emymes are Limiting factor > Follow ZERO ORDER KINETICS (sprunarion Kewertcs] perma, 6 TRANS - @ cnn I prog, RECEPTOR. perion AFFINITY > ability oF a drug tO bind to a receptor INTRINGIEG AEILVETY > ability to produce action after binding to receptor > CLASSTFICATION OF DRUGS BASED ON INTRINSIC ACTLVITY PGONLET > maximum intrinste ackivity [+2] PARTIAL AGONIST > submaninum totrinsic ackivity [oto +2] INVERSE AEONEST > Opposite atkion to agonist [—ve] > ANTAGONIST NO atkion Lo] bur Interrerec T fer atkivity peeantry. “DTRENSIC, . crear, mM, og perevery omg necerror, ferz0N t Signo trandutkion Mechanism CLASSTELCATION ‘OF DRUGS BASED ON SEGNAL TRANSDUCT® MEcHANESM © TNOTROPIC RECEPTORS foneeepic * an Fastest acking receptors SE Bo Boas > examples ca > aren, receptors = ON receptors > NMDA receptors Nyy receptors > AmPA receptors > Shy receptors @ enavmarte RECEPTORS Paka TYROSINE KINASE RECEPTORS Crmosty associated enayme ig Tyrosine kinase] SER ong > Examples cytokines P Prolactin L Insulin, 6 Growth hormones @G- PROTEIN CouPLED RECEPTORS L@PCR) cer 6 pretin Rarenaline Rarenaline a james 4 4 9 SE ten ane aus on p receptor aut on a receptor meate san $ t Shimslakes @ protein Stimolakes @ protein 1 J Aetive component fekive component 7 ame t co ~ pie — vaso constrice” — Bronchodilat” G PROTEIN @ stands for GoP/qrP binding protein Components A > GDP binds here in resting Stabe B v aaa tihen @ protein stimulated, phosphorylat” Occurs, GOP converted to GTP ‘smmBte FoR ‘ eran components Seperatex Sanus" B&T components are inaitive on a TGP ig ackive Produce one of Following ack” on > came cat ack” of ionowopic receptors = at?on | Component algo has GTPase activity JermGik Pomm reromi + convert. np to GDP > G protein Stabiliaak? occurs A Recyling OF G protein @ INTRACELLULAR RECEPTORS G. CYTOPLASMIC RECEPTORS oe b, NUCLEAR RECEPTOR > only Upid soluble drugs actt rough there receptors > slowest ateing receptors > commony named ap NUCLEAR RECEPTOR SUPERFAMILY feytoplozmic Receptors Nudear Reapror © > Cortcostroide [P > PPAR «| Glveo S > Gex Hormones, <3 FI sainarato vo vita b > vito lt > T., TH DOSE RESPONSE CURVE CoRC] raperbole, 7 HYPERBOLA SHAPE + Ar Loq DOSE RESPONSE cuRvE [log PREI R a) F 4 & Ghoped curve Csigmorp curved y clinically more useful than DRE BS ty D> @prency a 8 7% left sided curve iz more powerful (a) ; > > Right Sided curve ig less powerful (8) Rk R + relates to Gower yO > wD erercacy > felares to afeer regardless oF dose > © is more eFficoceous D ig lesc efficaceous 160 |-40 lao > EFF Icay Dose im mq 10 ° tomg | a0 0 20 mq oa 2D yo mq | 35 30 fomg [2s | 40 potene| _ EFFIcoRy 18 more important than poltney respeck to Ry 10 SLOPE ia Barbiturakes Bernodioneptcst Slope elated to sArETY w ra rug % ete slope ik more safer deep slope if less Safer a t le a Sleep Sedan” PHARMACOGENETICS ® q-6ro cerscrency mq > G-GPp protects Rec from free rodicle ingury > pRempaurNe SULFONAMIDES NITRO FURANTOIN FURR 20 LLDONE, @ Aceryiarion 7 emayme + NAT CN Aceky! Transferaee J > Freer INH > no response Sto TNH > Peripheral neuropathy +5 -f — ] o> to p> | 7 SHIP Drugs can couse Sie ®@ sch INoUcED APNER Sch C SUccLNYL eHoLINE? > mucele relaxant > shortest acting [<5smin} ~ dit Pseudocholinesterate > uted For Endotrocheal tnkubation IYPLCAL PSEUDO CHOLINESTERASE 7 meabolizes Sch in Jo minutes > coutses prolonged APnea THERAPEUTIC DRUG MONITORING CTDMmI case 12 > RIM > reduce BP from 160 > T2OmM Hg, Presibed droq @ @ toma for 1 Week, check BP after 4 week, Change the dose accordingly CASEQ > Epilepsy Potient , Prescribed DRUG @ @ toomg, then " > required plasma concentot® = —* 10-2 NgIL check plasma Concentrat? & Change the dose accordingly not uted commonly 7 cRireRIA TO USE TEM 1. RESPONSE CAN'T MEASURABLE 2 LoW THERAPEUTIC INDEX DRUGS 3. INCONSISTENT PHARMACOKINETIC DRUGS > tom done For RB > Antibiotics rug > DIGOXIN Possessing > PHENYTOTN [most antiepileptic drugs] low > utrHtom Therapeutic = TRECYCLEC ANTE DEPRESSANTS CICA] Index > -TmmuNo SUPPREGANT DRUGS > CYCLOSPORINE > TACROLIMUS, CLINICAL TRAILS Testing oF droq in humana PHASE > done in HEALTHY PEOPLE We cant do EFFICACY TESTING 7 mrp Emaximum tolerable dose] can be found > Phase T can also be done in Patiencz for Toxic drugs Paase > done in patients [20-200 number] EFFICACY INDICATION can be Known PHASE Or > done in patients Lupto 5000] > multicentric trails done (covers different genekic make up] > EFFICACY CONFIRMATION can be known PHASE > post morketing study done [ mox. no: of patients tested J > RARE SIDE EFFECTS can be studied 7 curonire Stok ERFECTS can be Studied Fon APPLLCATTONS INA > Tvestigokional New Drug Application 7 Applied before starting clinical trails NOR = > New Drug Application Applied wefore marketing the drag 12 PLASMA CONCENTRATION & TIME GRAPH. + max ro 12 obtai retro tebe © mma fax plastma conc. can be obtained = wa depends on dosage « aie 7 chovld ie bho MIN EC & max Te imam eft max 7% Eitne in wahich concentrak” becomes max. PC bell me RATE OF ASSORTION Puc Area under the curve Trax Time 7 tells the EXTENT OF ABSORPTION TYPES OF DRUG ANTAGONISM PhysteaL, 7 physical presence of drug stops the ad” oF omer [charcoal] cuerotcat > chemical renee” stops the ackion Canractos] PHystoLogtent, PHARMACOLOGTCAL PHYSTOLOGICAL ANTAGONTETS F aus on different veteptors produces opposite efrects 7 Htstamine Adrenaline L 4 4® Pa® 4 + Broncho constriction Bronchodilation . Higtamine iz physiological antagonist of Adrenaline PHARMACOLOGLCAL ANTRGONESTS Feces on same receptors to produce opposite eFfetks 7 PORENALINE, Propronolol t 4 Bak Pak 4 L Broncho dilation Broncho constsitkion S Propronolol ig — Pharmalogical antagonist oF adrenaline 13 ENIYME INHIBITION compertrtve 7 pruq can net bind to enayme Substrafi complex Non COMPETITIVE > rag. can bind to enzyme | ensyme Cubsivali Complex ON comperttive preg mainly binds [5 enayme Substrai Complex Tay @— Gh) sme competitive + = atin [Mont COMPETITIVE = T [ON compertreve ¥ z eve Leyp > cytochrome Pago] SUBSTRATES FOR cresng © CXCIDSPORINE , CALETUM CHANNEL BLOCKER + > TAcRoutmus Soo ene © > CASAPRIDE m var A > ASTemrzoLe © > cat orugs [t_ > _TERFENADINE 8 AMIADARONE 5 Thdrown dit Gr Prolongat™ Nn Nave cyp ape are > fp Blockers D> Depress? ANTE DEPRESSANTT DRUGS Ten SSRI SNR 6 7 THR > PNTE ARRYTHMICS Except AMLODARONE (by CYPzA4I 14 cy aia cvracig > CLOPLDOGREL —> acrtve > per — PPE acts a£ competitive inhibitor clopidogrel should not give E PPIE orp Co clotting > WARFARIN a> Pp > PHENYTOIN, COMBINED EFFECT OF DRUGS 4. POPITION / SoMMATION > a+ ai = 4 a. sYNeRGtem > ata za 3. POTENTIATION > ato 5 4. ANTAGDNESM eata ca AODETION /SummATION > idual effects oF a drugs, Simply acldad SYNER@EEM > corrtmaxoa0 > GULPHAMETHOARZOLE + TRIMETHOPRIM [eocteriocidal [eacterniostakic] Ceockeriostabic) POTENTIATION 7 Levonopn + cARGLDOPA Lenotkivel > EFFicacy oF levodopa tses ANTAGONISM > combined eFFect oF two drugs Will be lesser 15 Read and make the notes of following topics from the book “Review of Pharmacology” by Dr. Gobind Rai Garg. Routes of drug administration Drugs with high first pass metabolism Importance of plasma protein binding Prodrugs Steady state plasma concentration Quantal DRC Drug label Orphan drugs Golden Points PARA SYMPA~ THETIC eygrem Crone! eo = SYePATHETEC Svsrem Lumbar “SHEAT GLANDS PARA SYMPA~ THETEC SYSTEM 7 Preganglionic Fibres ore shorter in Sympathetic cystern Preqanglionic Fibres are Longer in para sympametic System 7 Poseganglionic Fibres are Longer in Sympothetic system Post ganglionic fibres are shorter in para sympametic System 7% Neurotransmitter secreted by all preqanglionic fibres > Ach 7 receptor present on post ganglionic Fibre Ny 7 Nr seureted by the post ganglionic Fibres of paracym. Sy¢km > ACh 7 NT Secreted by Pomsympametic system is ACh CHOLINERGIC SYcTEm 7 NT Secreted by post ganglionic Fibres oF gympamhekic system > NA — aka, ADRENERGIC s¥srem — EXCEPTION, postganglionic Fibres orsweatglondssecre > Ach PARR SYmPATHETIC Gvarem GNMPATHETIC Syerem HEART +t + FF omneRs ¥ Tt Bronchus > Broncho constrict" Ga Bronthodilat® @iT Zz > Diarrhoea > ~ Bladdar > Torin outflow => + offne outflow Glands > 7 Secretiong —> 4 Seurekions Popil > miosis > mydtasis PARASYMPATHETIC SYSTEM ORTGIN Cranial nerves: > 34,9,10 Sacral meres > a3, 4. 16 ACETYL CHOLINE Ach] CHOLINE 3° oes > slowest step > vptoke of + Paro syrmpalmekic_ackivity Hema|cHo! Vesalmico. BoTOLINUM TOXIN 4 a 3 Ach Esteroge Inhibitor 4 PHYSOSTIGMINE RECEPTORS OF ACh ® ote Pa SQ CHOLINE 4 ach Ach Esterase Degradation SS a choline FT Paro sympatheeic ackivity NECOTINTE ® _Wocariow TMUSCARENEC © LOCATION Ny > Gongiio: My > Skomach Ny 7 NM Ma > Heart require Optimal stimulok™ Mg > Bronchus fn bot hyper & hypo qu shrmula:® muscle weakness Bladder occurs Glonde Pupil PARASYMPATHOMEMETICS DIRECTLY ACTING TNDERECTLY ACTING directly ace on receptors > _atks byting Ath AcEsterace DRUG AeIs ON ACIEON TNDECATION PLLOCARPINE | Popil (H3@) meiosie angle closure glan@ma BETHANECHOL | Bloddit Cm, ©) fr out Flow tonic bladdur TETHA CHOLINE] myocardium (M,@I | cardiac Suppression [Tachycardia Arrymmias CARBACHOL | common ARON Nieotinic® Muscarinic® Dog & man, nicotinic ackion > CARBACHOL 17 ACh E REVERSIBLE AChE # UIPED SOLUBLE DaUas WATER SOLUBLE PROGS PHYSOSTL@MENE NEOSTEGMINE L not Lipid Solobled au FF oranty given qr > xX > Injections BBB es central eFfetks tnt BeB > x > no Centro] effects Pupil > v7 _used in glaucoma Pupil “> no erect on pupil LIPrD SOLUBLE DADS — USES 2. ANGLE CLOSURE GLAUCOMA + by PhytOstigmine 2. PTROPENE POISONING > RTROPINE Muscarinic receptor blocker £m)im,,myI +> cross BBB > Dec For atropine poisoning > Physostigmine easal Nucleus oF 3. SENTLE DEMENTIA | ALZHIEMER'S OEMENTEA &) Meynert + > dit degeneration OF dholinergic neurons in acquiring & Basal Nucleus oF meynert PEHOING mtmony 7 Treatment PHYSosTgmINE > not osed > Peripheral action leads co side errecks TACRINE > has only central action, > Was the doc > disadvantages > very Short acting > hepatotoxic tm Some D > ponereare > Long acting R 7 RIVASTEQMENE > On hepatotoxic Gobind > GALANTAMINE * Doc for Aluhieme’s disease WATER SOLUBLE DRUGS. 4. NEO strqgmrNe a. PYREDOSTLQMINE, 3. EDROPHONTUM 18 WATER SOLUBLE DRUGS - USES 1 MYSTHENTA GRAVIS 4 A against Ny Receptor Nyq Receptors Under stimulated t MUSCLE WEAKNEGS Non Receptors overstimulated t CHOLINERGIC CRESTS EDROPHONTOM TEST fe — TREATMENT + NEDSTIGMINE oF PYRIDOCTEG MINE tACh @ nj Bereptore @® ™ receptors 4muscle weakness Side efrecks > Roc > NeostIgmINE + ATROPINE 2 COBRA BITE FON A + Neostigmine + Atropine FRC 3. POST OP PARALYTIC TLEDS 4. POST OP URINARY RETENTLON 19 + by Neostigmine 7 R by Neostigmine ERREVERSIBLE AChE ORGANO PHOSPHATES I. MALATHION 2. PARATHION CARBA MATES 1. CARBORYL, &. PROPOXUR, 7 Highly Lipid soluble = + can cross intact skin >t Ach —— MRO 7 1 Hy coma mR @ + 4 HR, + BP Mz R @® > Pinpoint pupil } seerekions ofarrhoea Urinary incontinence Bron choconstriction 7 TF Pinpoint pupil ®1 pene a poisoning + Seuetions ® 7 THR, TBP cam be seen rarely (dle Ny@® Stimolation] Muscle weakness occors usually Cdlt Nm® overstimulation] TREATMENT \ prroprne + doe For OP g carbamate poisoning > by tv roote, In every 5 min till signs OF Ptropiniaakion ocors + 4 Seerekions > most reliable specie sign > mydriasis > most common sign > HR > 100 > cante reverse moscle weakness 2. RchE REACTLVATORS oxrmes PRALIDOxIMmE CPAM) DE ACETYL monOxEME LOAM > met poc + only erfective in oP Poisoning > PAM acke only peripherally , DAM haz both actions 20 EscopoLAMINE] | PROPHYLAXIS [tnextPHENYord | (voc BIPERIDIN = BENZHEXOL | PARKTNSONISM For druq induced BENZTROPINE | Parkinsonism Ach #} © [wore on [omvas ‘oes se wipétomach |PERENZEPINE [PUD TeLeNzePINE HEART [ATROPINE CoOd | BRADYCARDIA PV BLOCK Ty] BRONCHUS |TpRATROPIOM | BRONCHERL AaTHMA sorroptum __| opp BLADDER | SOLEFENACIN | OVERACIIVE BLADDER | Urinary Retent” OXYBUTYNIN: or CILin BHP fiavoxate — |perruccon NSTARILLIY| ToLTERODENE TRosPrUm blo DAR RENACEN W,|@IANOS arRoP=Ne Pee ONESTHETEC Dryness Cent iy ehitdrend MEDICATION Sweating 4 Fever + fiyper errnia MW] Eve — FUNDOSCOPY Tiuin fngle closure qlauicomn, |] REFRACTION TESTING Blurred vision ditt CYCLDPLEGIA | | boc in « (oss oF aecommodak” | + children — ditm, 4 | eropine + ciliary mosce contra | | Emax cyctoplegic boy m cn impaired out”, 74 days sadutts — sropicamide L {shortest: axting J ens HYOSEINE MOTION SECKNESS [MOTION + _VESTBULAR SYSTEM © > a © > _Vomting —? MOTLON SLCKNESS Nery high altitudes Cleh tadakh) > YPO, > Hypoxia > MOUNTAIN SIUENESS} boc. For motion Sickness 7 boc For mountain sickness > HYOSCINE CENS Deppresant] BCETRZOLAMIDE. Th _PARKINSONTSM, balance Bi Ach & OA syskrn disturbed 2 NORADRENALINE JNA in Synopse TYROSINE, 4+ Sympathetic activity © me|tyROSINE. @ RESERPINE @ _QvANETHIDINE Revptake Inhibitor 7 sympathetic ackivity oz © Arevptare [@_cocine J NA L NA RECEPTORS ms Sa Location, Action Presynaptic a, receptor fetood vessds | vasoconstrick” + acts like brake to sympametic leye Mydriasis System (main Ranction of 43 Prosthakic vrethroa [+ OutFiow Post Synaptic et, receptor = Proaosine (4#) used for BHP 7 _indigtingvishable from a, © Ps > Acke on Adipose Eissues + causes Lipolysis B Pa locakion Retion location Rczion Heart THR, TBP. Lungs Bronchodilakion JG cells. Renin secekion |qrr constipar™ Bladder 4 OUkFloW jqtands 4 seerekions lueerus Tocolytic [Blood vessels vasodilation Iskeletolmusclespindies| Tremors. ver 7 Sugors > of, 7 vasoconstriction & By 7 Yasodilakion > erfeet depends predominance of type OF receptor 7 Heart & Muscles + Bara > vasodilation > Skin, Lnkrnal organs > 4,>p, * vasoconstriction 22 ‘2n hypoglycernia WARNING SYmproms > dle aympathebic system stimulation Pr Pa eh 4 4 4 rathycordia Tremors sweating Palpitakions + Have to toke sugars > IF sugars ore not taken , even then Pp, © > wer @ aiconesgenesis @ aiyeoqenolysis © aiycogenesis J + Sigor 4 Reversol of hypoglycemia > B Blockers causes 2. masking of taming symptoms a. nO reversal OF hypoglycemia. B blockers are contraindicated in hypoqiycemia Sweating If only reliable symptom of hypoglyemia in diobelcs on B Blocker medication SYMPATHOMLMETIC DRUGS DIRECTLY ACTING RUGS > norrecrir ACTING RUGS INOLRECTIY ACTING DRUGS &. Revptoxe Inhibitors, > cocAENe > ex B. Drugs aking by displacement > TRAmENE > present in cheese. L®) + EPHEDRINE } Nasal decongestants aS 7 Psev00 EPHEDRINE oe > PIMPHETAMINES > cross BEB 4 sleep &f attent” span Uses + Noranlepsy Eslesp attacks] ADHD In Children > ghoud TACHYPHYLAKES Cooe ~ memylpheniciog.3 Fost Tolerance, 23 DIRECTLY ACTING DRUGS cavecsiolpmrnes. cokechol > Di Hydroxy Benzene, oye" es. comT > Catechol ortho memy transferase retgnise catecholamint > abundant in GIT > not effective Orally ENDOGENOUS CATECHOLATMENES EXOGENOUS CATECHOLAMINES > ADRENALINE DOBUTAMINE NA ESOPRENALINE DOPAMENE FENOLDOPAM DOPAMENE fcks on max in Renal By BR @ Heart = FR @ > 10 pg 1kq [min > Vasoconstriction oses 1 CHE &. SHOCK + oLgpRTA C doc] DRUG T DOPA in thelr name acts on D,@, oMmers do not DOBUTAMINE > do not atk on dy receptors > mainiy atts on p, reaptors > used for cHe FENOLDOPAM, > stimula. only b, Receptors 7 used in Hypertensive emergencies HR DERECT EFFECT ON UiB)) | INDrREcTErrECT on O[FeunL| | | TORENAGINE EPINEPHRINE $1 442, Ba TOR ADRENATENE NOREPINEPHRENE] isda» Br THO PRENALINE Bis Pa 24 > Blood vessels contains Baroreceptors mainly sense MBP (DBP) mer = tose o> + 4opp + * BRO OF SS ee NA EFFECT oN HR. 1. In ® person ae a In G person T transplanted heart > % Eno indirect action 2 uses ISOPRENALINE > By > cHE > Ba > Asmma NA nan > shook 7p, > cHr ADRENALENE > 6,6 p, 7% 2 ANAPHYLACTEC SHOCK > poc > Route % Im > SC > cone. > 15 1000 Igro ip 1000 mI Solution Dose > 0.5mi of 121000 Concentrakion + IF donot improved , repeat the dose tin 10 min > rp still not responded Iv Adrenaline C14 10,000] a CARDIAC ARREST BLS || no response ty Adrenaline = 1£10.000 = main veing CJugular veins] ose preferred next preferred rovte > Intraosseous still next preferred route + endotracheal 25 VASOMOTOR REVERSAL OF DALE AORENALINE StroqGensitive El, ® Pa L 4 aa vp BIPHASIC RESPONSE When Adrenaline given ty ak high doses ok First BP increases L dic Cot, »p,> Stimulation] then BP will decreann C dit py stimulation When Adrenaline given iv at high dose < a, plocter aon Exaggerated Fall of 8P occurs > vaSomoroR REVERSAL OF DALE pa 3m Pheochromocytoma + AP adrenaline + rer 9F Ry bY A blockers then vasomotor reversal of Dole Occurs & denim con occor @ blockers are CII in patients oF Phenthromocytoma NON CATE CHOLAMENES STEMULATES DRUGS ACTION ay Q. PHENYLEPHRINE EYE DROAS Mydriasis tout cycloplegia b. METHOXAMINE vasoconestrick® MEPHENTERMINE Used in shock MEDODRINE © XYLOMETAZOLINE Nasal dps | Nasal decongestants OXYMETAZOLENE Nasal drops NAPHAZOUNE Nasal drops CLONIDINE, Break for 6ymp. System METHYLDOPA used for HIN == Bronchodilation | sed For Asiana by | inhalakional rout. RETODRINE Tooolytics 1sOxsUPRINE used for Preterm labour Pa 26 SYMPRTHOLNTEC DRUGS & BIOCKERS 3,4 4, BLOCKERS &, BLOCKERS Jy BLOCKERS + —YoHIMBINE [no Clinical UseI Selective & non selective # used for HTN + Non selective q H can couse severe tachycardia Non Selective ot HH Used for Severe HTN Seleckive dH uged for mild to modumake HTN Non SELECTIVE TRREVE RSEBLE REVERSIGLE PHENOXY BENZAMINE PHENTOLAMINE TOLAZOLINE USES [ USES: Pheochromo aytoma cheese Reaction Clonidine withdrawal CHEESE REACTION Tyramine Tyramine Im =|" Break down reo | sano INHLAETORS Suddun Severe HIN [CHEESE REACTION] > poc % Phentolarine » Tolazoline CLONIDENE WETHDRAWAL > clonidine > ag, agonist +> reduces BP > suddin stoppage after prolonged use — dit opqradation of receptors Doc = > Phentolamine + Tolazoline &, BLOCKERS PRA 2OSEN TERR ZOStN Doxh ZoStN ALU ZOSIN ar REBOUND HIN oses 2 HTN + BHP Coord PERST DOSE / POSTURAL HYPOTENSION > 4, #% always started ok wed time Tyres Sin Sip ake on oc On Prostakic uremra, Blood vessels TAMEULOSEN StLODOSTN 7% 0 postural hypotension 7 voc For Normotensives t BHP P Blockers Pit pa H Colon selective} ast @eneration p # B, # and Genrabion BH B, # > BvTEXAMINE [no clinical Significance], > Bot, used for cardiac indications F Non selective By have bom cardiac & non cardioc indicaions Seleckive B # have only cordiac indications Pa os on Resor Pa L& Bronchus Brenchodilak™ Bronchoconstrict™ Asma, Blood vesset | vasodilat vasoeonstrice” Peripheral vas. p2| Liver bypogly aumia Ao such atkion DM reversal 1.B,3 OF CAROLO SELECTIVE Or and GENERATION @ # New era Blockers Ao Exclusively aE Myo cardiom, sp Soo toa i 7 These are relatively Safe in Asinma y PVD & Dm 28 INTRINSIC SYMPATHOTEEMETIC ACTEVETY LISA] / PARTIAL AGONISTS @ m @ m @ mm @ Wo V0 WV WD V0 J © DV VU qo fF a Boo fF ct Jom |e Vio oo ite 5 qo bes qo iA Ho [ef x J 10 J o ‘Hoo % J 0 V0 Ro 8 Jw J] Ko 8 ‘0 So ‘oo a JT «0 Ro ‘Koo A i an a a 8 Normal phenomenon 1@® stimvlotion > HR=I0 10 ® stimulation > HR = 10x10 =100 B. B blocker Usage in normal person B blocker blocks aoy. oF @ ~ HR = 10x8 = BO €. B blocker Usage in B blocker in a Bp blocker Sensitive person + B blocker blocks 87. oF R * HR = [0x2 = 20 + Severe bradycordia manifests > g, Sensitivity should be checked Z HR monitoring in p blocker prescribed pakienks + on these potions, portiol agonizts ore useful > tess chances oF causing Severe brody cordia (Safer drug] 7 Bur less eFficaceous contain > cELTPROLDL. Portial © = PINDOLOL Agonise > ALPRENOLOL Aeivity > ACEBUTOLOL 3 MEMBRANE STABLLEZING / Natchannel H] LOCAL ANESTHETIC PROPERTY > indicated in Arrhytimias > not indicated i) Glaucoma > commen is protected by Corea! refiex (Protective Reflex] -Engorg [tose a ermulot oF sensory 9. OF Trigeminal nen 4 Fotis. stile L conmestion oF orbiaslarts cul 4 eye closre Ceomnent REPU 29 © \s] 7 corneal rertex ig masked t thece drugs > prugs arama Possess, Membrane stabilising or Local Anesthetic Property heed LIATER SOLUBLE B BLOCKERS 7% cil in renal failure > prugs. A > ATENOLOL N 7 Napotot C Longest acting pH] S > Soro LoL BRO GENERATION & BLOCKERS 7 any BH T vasodilation property > vasodilation i dit & blockage > Exam PLES LaBETALOL CARVEDILOL OSES OF P BLOCKERS Bia uses 1 Hrs 2 classical Angina [ cz in variant: anginal 3 oma 4 chronic CHF Cot in acu cHe] Arrhythmia a 3. Migraine 4 Essential tremors 5. Thyrotoxicosis ADVERSE EFFECTS | ¢|t Bw 1 4 Rag > Bradycardia Sick sinus syndrome 2 4 conduction > Av Block 3 4 Contratkility > Acute cHE 30 Pall 2. Asma &. Peripheral vascular pisease 3. om B # contraindicated in 8 7 Asthma B&B * Block Cav) c o> CHE Cacute) bp > bm ACTIVE & PASSIVE MYDRIASTS ErFcT OF DRUGS ON EYE > Contraction of Sphicter pupillon > Active miosis contraction of bilekor pupiliat > ferive mydriasis Relative overactivity OF Bilotor pupilla + Passive mydriasis + Ackive miosis > caused by chelinergic drugs Active mydriasis > Caused by dt, agonists + Passive mydriass > carted by Anticholinegle drugs + @inucoma > 4 100 Aqueos humor production 4} Aqueous humor drainage 4 Aqueous Humor produced by Ciliary blood vessels + a, > vasoconstiction © > ADRENALINE } stimnvlali , receptors DEPIVERINE > PPRACLONEDINE } Stimulake post synoptic a, receptors BRIMONIOENE, > py % vosodilarion * Ba # can be osed 4 Aqueous ovtFiow + Trobeculor_oureiow + uveosatral oubFiow > major pati oxy > PGF, | LATANOPROST > progs + mrortes —~"poe For POAG, PLLOCARPINE, 31 AoveRse EFFECTS LaTANoPROST / PGF, Pigmentak” oF > HETERO CHROmEA ERIDES Growth oF eye lashes > HYPERTRECHOSIS Mrorrcs coerack Stenosis of nosolatimel system APRACLONI DINE. Lid retraction BRIMONIDINE Broin Suppression > CIE in new borry babies Iridocyclitis precipitat® 32 Read and make the notes of following topics from the book “Review of Pharmacology” by Dr. Gobind Rai Garg. Mirabegron Mushroom Poisoning Clonidine Uses Rabbit Eye Experiment Rabbit lleum experiment Golden points (CONGESTIVE HEART FAILURE ALM a 4 FLUID > prurettcs a, t PumpING “> INOTROPICS DIDRETICS THIAZIDES > weak) > Long acting 7 vsed in HIN Loop bruRertcs > strong > short axking used in cue COMMON SIE > + Nat >a +t >»? suger > 7? Lipids + 7 uric acid > Loop looses cat > 4 com [> Teor TNOTROPICS 2. py ABONTETS DA Fy dye dg acty = DosuTAMENE => By See Np Fay oP os ICOPRENALINE > pp, O Ob em x * [re a. PHOSPHODIESTERASE INHTBLTORS [PEL Degrade AMRINONE MILRINONE > also auts on Blood vessels > VASODTLATION - aka + ZINODTLATORS 3 pIGITALES | CAROTAC GLYCOSTDES > digitalis Inhibits Nat kt arrase 4 NEX Inhibition + team im cytoplasm 4 to in ER + 1 contractility > digitalis donot THR * no Tin Workload on heart 33 > vaso mimetsc EFFECT 4 LHR + Conduction 7 usefol in ATRIAL FLBRILLATEON % HR + yoo - 500 bpm Inerrecbive Contractions + Fibrillabions 7 aim of mg => 4 Ventriowar Contractions Digitalis 4ses Conduction from abrium to ventricles 5 BIGOXIN, DIGITOXLN Cwitidrawn 1 > moinly exeeted by Kidney mainly mekobolised by liver ¢|z_Renal Failure Clr in liver Fotlure DIGOXIN a Only inotrople drug that con be given ORALLY 7 Ble 1 Nausea, vomiting Cme] 2. Arthythmias me_arthytzmia > ventricular _bigeming Most Specific | charatrerictic * NPAT T AV Bleck [Non paroxysmal ¢ Atrial Tachycardia CAV Block J - not seen > Peril Floter Mobitz Type 1 heart block [DRUGS CAUSING QNNARCO MASTER) orgoxen 3 Gynaecomastia ey 4 4. XANTHOPSER | YELLOW VIStON 5 > scnmnowrcrone | c 7 amenpine i o> _cestrosens PIGCTALES ToxtctTy | FACTORS Ting OLGITAUIS TOXICITY METABOLIC DRUGS. PATHOLOGICAL peatt : RENAL FATLURE, 4 kt LIVER FAILURE + Mg>t | Mx OF DE@LTALIS TOKICITY 2, correct the cause 2. DOC for Digitalis induced arrhyimias > LI@NOCAINE | PHENYTOIN | 3, PIGIBIND for Sere poisoning 34 CHRONIC CHF CHE 4 4co 4 o L ve “oN $ 4 syrmpatberic Carina] | Veins Prterties By on heart J JPPRELOAD TP AFTERLOAD co AIM OF TREATMENT 2 4 Work a. 4 Fluid 3. 4 LVH (cardioe Remodelling] 2. 4 WORK > VASODILATORS P10 96 cells, t Renin setreéton L eee Angiotensina nee L 7 Angiotensin it eradytinin| L vo <— ATR OP AINA Lt Lv Aldosterone 4 1 Dea = FNat & Hyp retention tkt tut [WENO DELATORS ARTERLO OLLATORS VENO -+ ARTERLO OILATORS NETRATES HY DRALAZINE Na NITROPRUSSIDE, Bcet PINGIOTENSIN RECEPTOR BLOCKERS a. 4 FluID > Loop orureTiCs 3. + WH Ceardiac Remodelling] > tese ' poe B BLOCKERS CARVEDLLOL drogs 4 MORTALITY B BLOCKER pcet PINGIOTENSIN RECEPTOR BLOCKERS ALDOSTERONE ANTAGONISTS METOPROLOL BICO PROLOL ALDOSTERONE ANTASONICTS / POTASSIUM SPARING DIURETICS SPIRONOLACTONE, EPLERONONE 35 > cause qynaecomostia ACEI [ AcE INHIBITORS] * also inhibit Brady Kinin metaboligny £7 sradyKinins] < > ste > pry cough 4 Angioedema > paves > caro Pent A> Bae > LrernoPrrt © > captopril > ENALAPRL = Emalaprilak L_ > _Lsinoprst > RamIPREL > Ramiprilar > PeRINDOParL > Perindoprilat > rctive Forms > moeaxr Pett > Moexiprita > pverse errers, c > | ao p> 1 > o 7 ep > Ro I+ eeE ARBs 7 > Taste alterakion [ oysqusea] 0 Orthostatic / Posrural hypotens” P > at tm preqnanay R > cit ip BIL Renal Artery stenosis T o> at th Increased Kt Lo bower the risk oF Diabetic Nephropathy bros Canqrotenstn CaT,] receptor Glockers] Lo SARTAN S > Setecive VALSARTAN a> pT, TELMISARTAN R Recepror TRBE SARTAN v EPROSARTAN a Antagonists 7 CANDE SARTAN N + TELmESARTAN + also stimulates PPAR ~ 1 > Used to Reverse Insulin Resistance 36 NEW DRUGS BNP [Brain Natrivritic Peptide] * cause Nobriunsis (4 nat] cance vasodilation BNP | nee CNeprilysind begrodat” a. NASIRITIDE Recombinant BNP not given orally , given iv Short acking Used for Otuh cases thy a. NEP INHEBrTORS NCUBT TRE SACUBTTREL > Eefeckive Orally ECADO TAIL 3 VASOPEPTLDASE INHTBLTORS 7 Inhibit bom ACE & NEP + omarGar® Sam PAIRED 7 sig > cough angioedema ANGINA PECTORES 1 CLASSECAL [ EXERTTONAL Tr yerrAnt PRINZMETAL VASOSPASTIC CLASSICAL ANGINA PATHOLOGY > die aimerosdlerosic oF small branches oF coronary artery , 1sthemia occurs IscHemtA 4 t erreckive piomeber OF artery L No pain oF @ activity + puring Exercise Jexertion , 7 efFetkive diometer oF artuy nor suFFice For compengakion > PRIN occurs Aim oF TREATMENT > 4 Work on heart 37 VARIANT ANGINS PATHOLOGY dit SPASM OF MAIN CARONARY PRIERY 7 Pain @ rest occurs DRUGS I NrrRATES. J CALCLUM CHANNEL BLOCKERS M™ p Glockers Id POTASSIUM CHANNEL OPENERS 1 NITRATES. Bim OF TREATMENT + Dilakion OF Coronary artery Fak by releasing No > T camp > vasodilation Veins 7 arteries > mainly 4 Pretoad > prvgs + GININT@ & TON > hos high 4st pass metabo! 7 Sub lingual route prefered > pec For cull attack OF angina IMN hogs minimum ase poss metabolism Longest atking > PETN Shortest onking 7 AN NITRATE FREE PERIOD > tolerance occur if nitrokes continuously present vides to avoid tolerance, 6-8 hrs of Nitra Free period should be maintoined 7 NITRATES L No SULDENAFIL 4 {© camp —hotshodiesiemse 4 L vasodilation NITRATES should not be qiven T StLDENAFEL [RISK OF Severe hypotension] q wyPot 38 M. CALCIUM CHANNEL BLOCKERS > cALerUM CHANNELS > Livre > present In cvs > TYPE Present fn CNS FL = CALCIUM CHANNEL BLOCKERS BLOOD VESSELS HEART RATE, pinect | INorrect| NET VERAPAMIL vasodilation vosr [iit |r w DILTIAZEM vasodilation BP [LY it + OHP CDLHYDROPYRIDINES) vasodilation bap | + + NIFE DIPCN AMLD DIPLN NICAROIPIN LENT DIPLN, DIHYDROPYRLDINES Shovld be avoided in angina (THR TM PoTASSIum CHANNEL OPENER NECORANEED 7 No Release + kt Channel opener TB Bickers pa 4 LHR + 4 WORK 1 osefel in classical angina > B Blockers are CIT In varient angina NEw DRUGS 1 BRADYcARDEAC AGENT > IVABRADINE ID GB GRAD ne + ; Not channels. in) 6A Node . a Tp blocker sje * visual ccuity| Fi current (ip) eong ra Bradicardiac agent > abradin tnhibit Nat channel Cunny current] > sie > 4 visual ocity + recently approved for CHE 39 2. Rho KINASE INHIBITOR —- fASUDIL > Rho Kinase causes vasoconstriction > Rho kinase > causes vasodilation > indicated in angina 3 METABOLIC moDULATORS > quweose + 100 0, wo ATP Comer ports oF Body] Fatty acids + 2000, 9 0 ATP [Heart] + FR require more 03 For some energy production 7 METABOLLC MODULATION > Making heart to oflise glucose instead OF fattyacids DRogs 1 TRIMETDZLDINE 2 RANOLA ZINE 7 also acts by blocking Nat channels along 7% FA metabolism, Inhibition Mr > ANGINA > Myocardial Ischemia (Reversible ] ML > Myocardial infarction C trreversible] > NON — steror > stemt Management. MANAGEMENT ™ MORPHINE S > STREPTOKINASE o > OxYEEN 0 > OxYeeEN N > NITRATES N 7% NITRATES Ro ASPIRIN B o> ASPIRIN ™m > MORPHINE 40 BLOOD PRESSURE > Laberal pressure exerted by moving column of BLOOD on WALL OF BLD VESSEL ANTI HYPERTENSIVE DRUGS 4, DIWRETICS > | Blood volume > Y HARDNESS oF BLOOD vEssEL L¥ s.Sodiom] 2. VASODILATORS SYMPATHETIC SYSTEM BLOCKERS 4, RAAS GLOCKERS o T proretrcs LOOP BIORETECS THEAZIOES > Strong weak > short acking long acting > _used_as ist line drugs for HIN v4 VASODILATORS a. ND RELEASERS 7 Na NETROPRUSSIDE > pyoRALAZENE > Bom ove Fast acting > used in HIN Emergencies > Nao Nitro prusside + macroprrp set used — 64 drops > ami > tong term vse > Leads to CYANEDE POISONING > Antidote % HYDROXOCOBALAMINE + metoholised by > Acetylation > se > SLE = CALCIUM CHANNEL BLOCKERS > VeRAPArAIL DELTEATEM DHP 3. KY CHANNEL OPENERS Mo MENO xrDIL Db > DIAZOXLDE H > BYDRALAZINE. Masala, wt 7 MENOXIDIL cauzes hair growth Seas ae > used for Alopecia > crew sPotNE 7% avoided in young females mt menonore > pIAZOKIDE 7 Decreages the releate of insulin > ait in pm Fused in INSULINOMA ~ TL sympatHeTiC System BLOCKERS 1. GANGLION BLOCKERS > NA Receptor antagonists 7 TRIMETHOPHAN HEKAMETHONLUM > mainly used as Antidote for NICOTINIC POISONING 2. &q RGONESTS > ctontorne } Bol are safe in pregnancy METHYLDOPA Bol con cause dry mouk & Sedation + CLONIDINE Sudden stoppage causes REBOUND HIN 7 METHYLDOPA con cause Hemolytic Anasmia 3. of & B BLOCKERS TZ RAAS BLOCKERS [ RAAS > Renin Angiotensin Aldosterone. system] @ Gp» ceus 0X2 4 Renin <—> CO) Angiotensinogen Angiotensin 1 @ XK vce Angiotensin t@ Vasoconstriction <——[ATi_B&CEPTORS] —> catecholamines J na T AldGsterone ee L + * not & HO 42 RENIN INHEBETORS > pirskDQED ems KOGEND | ona orvas ENAL KDGER RENIN INHIBITORS > ALISKIREN » REMIKIREN » ENALKIREN RENIN RELEASE INHIBITORS -> B BLOCKERS TREATMENT OF HTN Nc - 8 GUIDELINES 1. BP y 140/90 Lany one CSBP] DBF) can be considered ] a. START + Be % 140/90 not controlled inspite OF LIFESTYLE MoptFLCATION [ Low Nat diet & requiar exercise] 3, PERST LINE DRUGS LIF There are No Omer Compelling indications] A 7 pAcet/ ARG c oF cee b > prorertcs [ Thiazides] 4 GOAL < 140/90 in all pakients < 150/90 in >6Oyrs pakientgs tout Dm Or CKO > Bom SBP & DBP Ehould be corrected we 5. poe | INC -8) HARRISON HIN in Preqnanay => METHYLboPA | —> Oral LABETALOL HTN Emerqeney in Preqnancy |» HYDRALAZINE [tv LABETALOL aT = _THTATIDES ~>_THIRZEDES HTN Emergency > _NITROPROSSIDE| ->_ NECARDIPENE. ANTE HTN DRUGS SAFE IN PREGNANCY. Better a Momer care during Hypertensive PReqnanay a 43 Hyperpolarizal® C@ resting phase) a + 3 nat nal K* << pepotarizat C@ depolariged phase) tt 7 | at epotartzat® RESTING MEMBRANE POTENTIAL C - 40 mvJ > Relative negative charge inside the membrane dit Natk* ATPase DEPOLAREZATION > dit mat entry through Nat channel HYPERPOLARIZATION > dit kt entry Through Kt channel at resting stake REPOLARIZATION > _dit_kt entry through Kt channel ok depolasizat” stake nerton POTENTIAL, +30 2. NOT CHANNEL BLOCKERS ‘ > occe by + store [ “/de] oF Phase 0 a kt CHANNEL BLOCKERS, or 7 > Action Potentiol duration (App] - 7 ar IreRvAL + Depolorisat + s repolarsation ars. + manifectg ag tT interval on ECG > ToRSADES’ DE POINTES [TDP 7 QT Interval 3 KT CHANNEL OPENERS + 4 Potion Potential Curation [APDI ANTE ARRHYTHMEC DRUGS VAUGHAN WILLLAMS CLASSIFICATION. 7 Based on predominant mechanism oF attion CLASS 1 > Nat CHANNEL BLOCKERS class I > B® eockers Class Tl > kt CHANNEL alocKeRS Class TL =~ Ca CHANNEL BLOCKERS 7 CLASS DZ > OTHERS } 44 class 1 Nat CHANNEL BLOCKERS. > 4 Slope oF phase o 4 Ig % block Kt channelg > Precipitates TP 1,7 Open Kt channels I 7 no effet on Kt Channels © > Iq pruas QUINIDINE PROCAINAMIDE, Tp DRUGS > I,_ pRvGS ENCAINIDE FLECAINIDE PROPAFENONE class DB BLockERS Fused in Tody arrhytmmiag, CLASS M > k* CHANNEL BLOCKERS B > BRETYLUM > TeuTrLioe N D7 porertitpe 6 > RMTODARONE S 7 soratD > soraLoL has both class mt Cmajor] & closs a Actions AIODARONE > tongest acting Cty, * 7 Stks) anti arrhytmmic drug > Mon 1. Nat channel Blocker B blocker K+ channel Blocker [main action] co channel Blocker pop F Indicated in all arrhythmias except TDP a > Aoverse EFFECTS The + hyper or bupo Thyreidism Periphery of + Peripheral neuropommy my 7 Myocardial deprecsion tong & 7 Lung Fibrosis cornea is 7 cornea) cleposits Photosensitive > —Photosensitivity cinss 7 Lk = Ca CHANNEL BLOCKERS VERAPAMIL DILTEAZEM DuPs [not used J > used In Tachyarrhyinmias Should not combine E p blocker[ Risk oF Severe Cardiac depression] class V > oTHeRS. DIGOXIN 7 used in Atriod Fibrillation ATROPEN, * oc Fer bradycardia & Ay Block ADENOSINE 7 Shortest Cty, > bec For PsvT put ~ oYSLEPrOEMICS STaTINs mon 1 Inhibit HMq~- COA Reductase fawn] 2. compensatory T oF UL -© ‘3. Cholesterol ig taken from blood [crosnsrenon A. 4 Serum cholesterol includes TORVA STATIN NON ANTE BYSLLPLDEMICS| ROGUVA STATIN L Longest Acting] Enos & SIBTIN PRAVASTATIN CUNSTATIN sirmva st TIN Penrosraren FLUVASTATIN, SOMATOSTATIN. ceRtvastAatiN PLTAVASTATIN IMPORTANT POLNTS 3. Statins have maximum LDL-cholesterol lowering potential 2. Given @ Lake evening | night 46 + ptorvastakin g Rosuvastakin are long atking » coh be given of anytime of the day 3. ADVERSE EFFECTS Myopomy 4 Risk fuer Nd T FlBRATES Hepototoxicity 4. Tom 5, PLELOTROPIC EFFECTS [aeneficial ] PL > plaque stabilizar™ e 4 Endothelial dysfunction I > 4 Inelammation ° 7 4 Oxidakive strecs TR FL Thrombosis opie INTESTINAL CHOLESTEROL ABSORPTION INHIBITOR [ ELETIMIBE] + commoly combined t statins FIBRATES > includes CLOFIQRATE FENO FIORATE BEZAFTBRATE Gem FLBROZIL, > ack by PPAR & stimplation 4 4 LPL CLipo protein Lipase] 4 4 Triglycerides + Fibrokes have max. T@ lowering potential BLLE ACLD BINDING AGENTS [BABA] > includes CHOLE STYRAMINE coLestrPoL CHOLESEVALAM + mon ENTERS HEPATIC CYCLE > Bile Acid carry Substance From Gut & releases in blood & reabsorbed BABA Interupts enterDhepakle cycle GA exereked Liver Synmesixes BR Geom cholesterol —> 4 Chelesterel 47 F oc in children & pregnanay [sare drugs] F cholestyramine &% colectipel not easily palakable 1 (holesevalam can be torn orally) NiRCEN, C vttamen 65) has max. HDL - cholesiero! increasing property 7 only drug, tat can 4 Lipoprotein ca) > Lenst expensive 7% Not commonly ored die Pruritis q Flushing > can couse Hyperuricemig , Hepatotoxicity NEw DRUGS MOND CLONAL Ab agoinct PCSK -4 4% PCSK-S helps in breakdown of LoL-® 7 Includes PLERDCUMAB Evolo comas cc® UC co CHANNEL BLOCKER J IV VASOOTLATOR TESTING 7 If positive, Doc cB > IP negative, Doc > ENDOTHELIN ANTAGONIST BOSENTAN PMBRENTAN MACE ENTAN PDEL [ PHOSPHODLESTERASE INHTBtTORS ] > SLLDENAFrL Paty TLopRosT PGE, © TREPROSTINOL 7 most eFferkive drugs fer Pulmonary HIN + corre be given orally SELEXIPAG, SELE + Selective > Prostacyulin agonist XI non ingestable Loral] + can be given orally Poo Par, RQ > Agonist RrOCL qUAT 7 scirmpleG Guonylote ayclase > 7 camP 7 vasodilation 48 caused by Drugs ilo émall vessel only > 7 dit & blood Supply to iSchemic area Is taken towards dilaked small vessel Soe en acamcnen cy > Shown by i n> 1 oF) eo Le SE + shock > 4 Tissue perfosion > cop EXTREMITIES WARM EXTREMLILES cardiogenic shock Vasodi latory | distributive shock Hypovolumic shock > pistarBorrve sHock 1 Septic shock a. Anaphytadkic shock 3. Nuwrogenic shock 4. Hypoadrenal Shock > TREATMENT Lene 2. PLUID REPLACEMENT > vp chovid be maintained blo 8-12 mm oF Hg + Ng or RL preferred F blood given iF required 3. YASOPRESSORS + ceptic Shock 1 Na Cpocd 2. PHENYLEPHRINE [in case of risk OF amrhytimias) 3. N& + VASOPRESSIN also vsedl > cordiogente shock > poc + NA > oF > Amophyloctic Shock > pot > im ADRENALINE ? GC ADRENALINE > 121000 + 14% tocom! L img mid > pose > Sml oF 12 1000 Concentrak ' 14 10,000 iv Adrenaline given in non responsive cases A. SPECLFLC. TREATMENT a Septic Shock > Broad Spectrum Antibiotics 2 Mypoadrenal shock + stervids 49 Read and make the notes of following topics from the book “Review of Pharmacology” by Dr. Gobind Rai Garg. Plasma renin activity New hypolipidemic drugs Drug treatment of arrhythmias Golden Points proretees 7 cause loss of Nat & Hp in urine Pauaretzc > cause loss oF Ho only CLASSIFICATION based On Site OF ACEION 2. OsmoTic DIURETICS > Includes MANNITOL > properrtes > shovld be Freely Filteable + Shovid not be reabsorbed > ghovld not reer cheically should exert osmotic effect > ses CEREBRAL EDEMA 7 beneficial effect OF Mannitol in broin + Osmotic Fred J cit in ActIVE CEREBRAL HAEMORRHAGE + oral Mannitol couses Osmotic diarrhoea A. CARBONE ANHYORASE INHEBTTORS > pete on Proximal tubule piooo PT ce MEN > Imbibits carbonic anhydrase at nat 7 comses loss OF Nat & Hoos in vTine e - & wens nee De + ws Jnot Hp > otorests re + Heoy > ORTNARY ALKALOSIS Tea 5 Hye0g veo Merpgotre Actoosts TA Lea w,tnp | coth 7 hove self limiting action 2 emus > tndudes ACETA2LAMLDE BRIN ZOLAMEDE } given as eye. poR20LA MIDE > ReerAzoLAmEoe > con be given orally | Injectable Form Indications + movntoin sickness Looe] > glaucoma ee 7 Metobolic Acidosis 7% hypokalemia Emax. hypokalemia among divretics] > Poresthesia 50 3 Loor orureTscs Loop olureties > asks on ascending Limb oF lovp of Henle SS > Inhibits Natkt aci” syrmporter S. > inciudes | ASCENDING LIMB — _ oF UH 5 High ceiling divrekics CHigh arfieaty divreties ] > ap-a57 OF Not is reabsorbed from ascending Limb of LH ‘THEATIOES. 4 THIAZIDES > acts on digtel tubule not 7 fmhibits Nat ci7 syrmporter a > includes METHEAZIDE POLY THEAZEDE preTAL TUBULE CHLORTHTA2IDE INDAPAMZDE | Thiaaide lke xiPAMIDE Diuretics Nat + qiucose kt ® uric acid Mgt + Lipids at eee Loop looses co®* > 4 co * cot used in Hypercalcemia used in osteoporosis @ civretic preferred in Recurrent Rena) stones @ wor v. (Wea —= Se 8 Loop piurebics cae Even though Thiovides % 5.ca™, Less ca? reothes Kidney Z loop diuretics, more ca2* reaches Kidney uses. 2, Edema, a. HTN 3. Diabetes insipidus —> Thiarides indicoted 51 DIABETES INGIPTDUS 4 BDH retains only water TYPES. ETEOUGY TREATMENT CENTRAL OT IY Bor DESMOPRESSIN Coot] NEPHROGENIC DI [Renal couse THIaziDes > THrpatoes + mon in DE > pr FF orine [~ 100-2000) + > plasma osmolarity compensabory mechanisms 3, TROH a Thirst centre stimulation > Thiaaides cause excret® oF concentrated Urine 4 osmolarity, t 4 Thirst L 4 urine Formation 5. Kt SPARING DIURETICS > acts on collecting duck SPLRONOLACTONE AMMDRIDE EPLERDNONE TRIAMTERENE > tese drugs couse 4 noteHo > diuresis a Kt > Hyperkalemia aout > Metabolic Acidosis sp ep | a7 s 7 1? —e > eee ® 2. ALDOSTERONE © H 2. epiBelial Not channel # jeo—r-q > ALL DIORETTCS WORK FROM LUMINAL SIDE EXCEPT ALDOSTERDNE ANTAGONISTS ALDOSTERONE ANTAGONISTS WORK FROM BASOLATERAL SIDE 52 Read and make the notes of following topics from the book “Review of Pharmacology” by Dr. Gobind Rai Garg. a Free water clearance a ADH - Vaptans couse Day cougH PRODUCTEVE COUGH by GNTETUSEIVES R by MUCOLYTECS /EXPECTORANTS coDErNE BROMHEXENE PHOLCODETNE. MMBROXOL DEXTROMETHORPHAN GUANAPHESIN NoScAPINe kt BRONCHIAL ASTHMA 1, BRONCHODTLATORS a, SYMPATHOMIMETECS Ba AGONISTS SALBUTAMOL, short ACkINg qiven by | TERBUTALINE = used inauste atiacks inhalotion | SALMETEROL Long acting FORMETERDL = used For prophylaxis > SpimereroL 7% Slows acting > only used for Prophylaxis FormereRDL 7 Fast acting 7 also be used For Acute Attooks Cooc] > SIE of p, ABONTSTS 1 > Tachycardia Cme) TF tremors + F Tolerance b. PARASYTMPATHOLYTECS Mg BLOCKERS ‘TPRATROPLUTD Trorapprum > given by Inbalakionol roote > noc for acute attack in patients on B blotter therapy Cc. poet LC PHOSPHODEESTERASE INHIBLIORS] + —?re___, cAMP Degrodal? i 7 fnclodes THEOPHYLLINE = not efreckive by inhalational route 3 PHOSPHOLTPEDS sTeRDEDS @ - Phospholipase Aa PRACHTDONTC ACED © @ ELE UTON PROSTAGLANDINES LevcorRtens 4 LT REBRTORS aAFIRIDKAST ee @ ~~ MONTELUKAST BRONCHO CONSTRICIION, sreRorns > Bec For prophylaxtc 7 alto used in ctu anack atong t bronchodilators MAST CELL SmALLIZERS 7 Include SODEUIT CHRDMOGLYCATE. NEDocROMIL, 7 only Used for prophylaxis 4. OMALT2UMAB, 7 monocional antibody against 1g& > only used for prophylaxis > given subcutaneousiy 54 Read and make the notes of following topics from the book “Review of Pharmacology” by Dr. Gobind Rai Garg. a More details of steroids a expectorants and Antitussives PEPTIC ULCER DISEASE > dit feebolance between Aggressive & protective fockors Aggressive factors > Hcl » H. pylori Proteckive Factors > mucus & HOE TREATMENT a. 4 Rew Hel > produced by Posiekal cell oF Stomach > proron Pump CHtKt PumPI 7 helps in Seeree® oF Acid > stimutked by Ach CMI Hictarnine CHa) gastrin Leck] * Inbibited by PGES 55 mucus) Hel Hoos” | Hpyori 4 AetD M, BLOCKERS: Hy Blockers [PGES PPL PLRENZEPINE CLMETLOINE MISOPROSTOL | ELeNZE PINE, RANETIDINE PAMOTEDINE LORATLOINE. 7 most specific drug for NSATD induced Peptic oler + misoprostol PPIs [ PROTON Pump INHTBITORS) 7 Irreversible inhibitors > Example oF HIT AND RUN DRUGS F exerts systemic eFreck (not work locally] normally acid labile given & add resistant coating + Enteric coating > pec For PUD of any reason boc For GERD Doc For Zollinger Ellison syndrome. > SIE C chronic use] ~ + wt — (osteoporosis) — vit Bia [Megaloblastic anaimial — 1 infections Carcinoid syndrome Lnot noted in humans] 2 ANTACKDE > Fastest poin relievers oF PUD SS Paty > indudes ve AICO], cause constipat MgoH], cause Diarrhoea 3. ULCER PROTECTEVES > sucRALFATE COUDIDAL BISMUTH SUB CITRATE ad 7 SucralfoG axs by Polymerizat”, requires acidic pi L astecdystrophy ~ Brin + Encephalopatny 56 4. H.PYLORT DRUGS > BMOXYCILLIN METRONIDAZOLE, CLARLTHROMYCIN > TRIPLE DRUG THERAPY = > «PPL + 2 AMAL © 7 clARTTHROMYEIN Preferred AF MOXYCILLEN po per NTE EMETTC DRUGS, 1. ANTE CHOLINERSIC ORUgS > HyoscINE a. Hy BLOCKERS F _POKYLAMINE Looe for morning Sictnesc] 3B BHTg BLOCKERS ONDENCETRON oc For G@RANZCETRON brag induced vomiting TROPI CETRON. Radiomerapy induced vomiting PROLONOCETRON Lrnost potent] Post Op. induced vomiting 4. NEUROKENIN ANTAGONTEIS [SUBSTANCE P ANTAGONISTS] APREPITANT ]_ coc For NEOPITANT Delayed vomiting by CISPLATIN ROLR PLTANT 5 Dy ANTAGONISTS METOCLOPRAMEDE DOMPERTOONE cross 685 00 Ror Goss BBB cary cause dystonia DO Mok cause diystonio, oc For Levedopa induced vomiting} SHT3 # NO Omer action sat. ® _| PNTT DIARRHEAL DRUGS a. ORS > contains Nacl } Replenishes electrolytes. Kel Tri Sodium citra > prevent acidosis Glucose + to aid Nat absorption 2. BNTE MICRDBIALS FOR INFECTIONS METRONIDAZOLE For Orneobic infect } combined usage is CIPROFLOXACIN for bacterial infeck™ irrational 87 3. NON INFECTIVE prBRRHEA > LOPERRMIDE 4 Intestinal motility DIPHENOXYLATE, A SECRETORY OTARRHER > ocrreortoe + Somakestatin analogue 5 RACECADROTRIL > ey ung) <> ” NKEPHBLINS ocinase > Degradat! [erdeasnpes opioid > enkepholinase inhibitor INFLAMMATORY BOWEL DISEASE ULCERATIVE COLITIS 4, 5S ASA DERIVATIVES > doe 4. SULFASALAZINE > SASH - SULFMPYRIDINE a. OLSALAZINE > 5Ash — 5ASA 3. MESALAMINE, a. STEROIDS > TF Mok responding T 5 ASA derivakives CROHN®S OISERSE 1 STEROIDS > pot 2 TNE ot BLOCKERS > IF not responding ¢ sterofds PPALIMUMAS CERTOLE 2UMAB ETANERCEPT INFLEXIMAB 7 Laxative > causes semi Solid Stools purgabive % causes watery stools > uses 2. Functional constipakion (not for obstruckive constipakion] + constipation preferrably Ry by High fibre diet & regular exercise 2, TO PREVENT STRAENING > Hemia > Piles > Pal fissure 3. x RAYS OF KUB 4. Along T ANTE HELMINTHTC DRUGS CNICLOsAmiDe] 4 58 7% includes 2. BULK FORMING Cshould be given t plenty of wate] > brernay rere Psyutum METHYL CELLULOSE Fat in megacolon @. osmotic PURGATIVES > GALINE PuRgaTives 7 Mgsoy Mg Con), 7 cit in chronte renal failure. > LacruLose: % POLY ETHYLENE GLYCOL 3. STOOL SorrNeRS 7 4 Surface tension oF Fluids in |IT > DocUssATE - Di octyl Sodium sulfosuccinake 4 STEMULANT PURGATIVES > ORGANTC > BISACODYL No PICOSULPHATE. 7 SIE = colonic atony Con longterm usogel > PNTHRAQUINONES > SENNA CASCARA, > SIE - Melanosis cols > castor on 7 Stimulant purgakives are cit in obstuctive Constipakion 5 NEW DRDGS 2, LENACLOTIDE cl channel twerprostone J stimulants 2 PLECANATIDE 7 CFTR Stimulant 3 OPIOID ANTAGONESTS Cu HI METHYLNALTRERONE AlvimorAN NALAXIGOL NALDE MEDIN 59 Read and make the notes of following topics from the book “Review of Pharmacology’ by Dr. Gobind Rai Garg. GERD Irritable Bowel Syndrome Composition of ORS Golden Points PITUITARY HYPOTHALAMIC SYSTEMS. PRULTARY GUND HORMONES HYPOTHALAMUS CONTROL GHRHL GH Releasing Hormone] Sroiam Hormone Cant CT Guin C@h inhibiting Hormone! Thyroid Stimulating Hormone (rst ¢————— TRH thyroid Releosing Hormonel dreno corticotropic Hormone (acm) <————— cr Ccerticotrepin Releasing Hormond Gonadotropins ———— nari Can Releasing Hormone] Prolackiny «————— Pt Prolactin Inhibiting Hormone] GROTH HORMONE INHIBITING HORMONES [GHIH) / SomATOSTATIN ORGAN ACTION, USES © PLTUTTARY [> v6 > Peromeqaly Pancreas « cells [Glucagon } > 1 Blood suger B celts Cinsolin ] > + Blood sugar 6 celtg [somatostatin]! J glucagon > Hekcell tumors + Insulin eart > L Seerstions > Gexretory diarrhoeo Blood vEsseLs =? vasoconstriction | > Oesophageal vorices > * Somotostakin > Short acting OctREOTIPE = Long atking somatostabin derivative RNY PHYSIOLOGICAL SUBSTANCE ENDING tN? Is PEPTIDE * They will be degrodkd when given by ore! rout, OCTREOTIDE > given by Sc route GONABOTROPIN RELEASING HORMONE [GnRH] GONADOTROPIN RELEASING HORMONE CGaRHI POLSATILE FASHEON CONTENUOUS FASHZON Gonadotropins 4 Gonadotropins 1 Estrogen, 7 Progesterone 4 estrogen, 4 Progesterone Testosterone 4 Testosterone 60 INDICATIONS OF GnRH In Pulsatile manner @ typogonadotropic hypogonadism ® delayed Puberty In continuous fashion © cancers > prostate cancer + Brest concer @ Endometriosis ® precocious puberty GnRH AGONTSTS LEUPROLIDE NAFARELIN GOSERELIN Busv RELIN HISTORELIN ®@8 O00 + FLRRE UP REACTION + uthen these drugs given in Continuous manner, Initial 2-3 daye there is aggrevakion of disease GnRH ANTAGONESTS CERO RELIX GANT RELIX BA RELEX DegARELEX @@600e0 ‘ No Flare up reaction but they do not Tse Sex hormones 4+ > Eimer GnRH Agonists oF GNRH antagoniste , Not effective Orally PROLACTIN, INHTSTTING HORMONE C PIHT DopAMINE Lond > DA ogtt through Dy Receptors > rugs stimulating Og Receptors ack Uke PIH >_>, RECEPTOR AGONISTS > BROMOCRIPTINE > CABERGOLINE [Long acting] > inprcrrions @ HYPER PROLACTINELA + CABERGOLINE % DOC, Can be given orolly 61 @ perkinsontsm © rcromeaary : 7 CABERGOLINE Is the preferred drug 4 > 4 aH 7 can be given omally | Peg uisominnT Tan RECEPTOR ANTASONTSTT > PEGVISOMANT —> _Somakotropin Antagonist 7 PEG VI SOMANT > causes Visual Field defect 7 _PEG VISOmANT > Polyétryleneqiycol Long acting ®@ wre a om % BROMOCRIPTENE 4 Insulin resistance THYROID > secrets 13 T CALEETONEN 3 Tq 7 short acting > longer acting > __more active > less active > LLOTHYRONINE 7 L-THYROXINE. = only indicak” > = bee For hypornyroidtistn Myxedema coma 7 Doc For myxedema coma Cemergency} PHYSLOLOGY OF THYROLD HORMONE PRODUCTION 62 @ todide (171 enters into thyroid Follicle by Nat 1 Symporter ® From follicles 1Odids enters into colloid ® in cotioro ir TL oxidation argenificak® t tyresine, T_ coupling + all ne 5 reactions catalysed by Thyroid Peroxidase > tg, Ta stored in colloid, @ Ts stimulates myroid © 13,14 released into cirenlation © Hormone reaches peripheral tissues jorgans [ Liver] + in me blood, Ty if ackive bul Less in quantity Ty If abundant but not much active @ Peripheral conversion tater place in peripheral tiesves jorgans [ Liver] metabolised 13 HYPERTHYROIDISM — DRUGS @ nis tnneearors @ THYROID PEROKEDASE INHEBETORS @ SecRETION INHIBETORS @ PERIPHERAL CONVERSION INHEBTTORS © THYROID DESTROYING DADS NTS TNHEBTTORS @ PERCHLORATE @ PERTECHTENATE @ THrocvanaTe > not used clinically Ctoxic) > cabbage is 0 rich sousce OF Thiocyonate 7 GoITROGEN 63 THYROLD PEROXLDASE INHTBITORS @ cARSMAZOLE Cinacive @ PROPYUTHIOURACLL CPO J @_merHrmazoce Cactive) more potenE tess potent more plasma tt/y tess plasma ty, “crossec placinka easily less crossing oF Placenta 7 doc in ast trimester pregnancy] F__po action on peripheral convers” | > _decreages Peripheral conversion > Slow acting drugs 7 on @ person, stored Tg, SuFFice For Ia UOks 9 bypertbyroidism , they Suffice For 3-4 lake Dose Inereont oF mete drugs should be done after A wks. SECRETION INHEBLTORS. @ not @ kt © wweor's tootne > Fastest acking ontimyroid drugs i @ERLPHERAL CONVERSION INHIBITORS © PROPRNOLOL @ ptu © prepnisotone | THYROID DESTROYING pRUgS C13!) | > Used because © Nad1~ symporter ig gpecific For Iodine intake > restrices 113! t0 thyroid gland © 113 stored in colloid, emission of radioactive rays confined ® 1 emits p rays, have lece penetraking power > ax In pregnanug > con be given orally > Radioactive drugs cole irreversible hypotmyroidiim , tequires life long Thyroid hormone thearapy cit in < 35 YrE aged patients “7 BIL omer ontimyroid drugs couse Reversible hypothyroidism , discontinuok” OF drug suffice 7 1% cy. > 8 days 64 SECRETES BETEON uses. a eens Glucagon + Blood sogor | hypoglycemia Bp cells insulin acai amaytin & cets SomeaboStoting GLUCAGON oses 4. HYPOGLYCEMIA pea OB eae — Moe acke bY GLYCOGENOLYSTS vseFul in hypoglycemia caused by Storvation Mleohol induced hypoglycemia 2. PBLCKER Porsonttng Loc] INSULIN INDICATIONS PREPARATIONS RAPED ACTING > LESPRO ASPART @LULTSENE SHORT ACTING, LONG ACTING INTERMEDIATE ACTENG => NPH ULTRA LONG ACTING __GLARGINE REGULAR, Sem - LENTE LENTE ULTRA - LENTE > BI tnsvlin preparations of given by > Sub wtaneouss Foote Requiar tnsolin alco be given by = > Iv route > Pil insulin preparations are at > Neutral PH Glargine is oF acidic PH € bypogiycemia > >307, Functional B cellz Should present DRUGS ACTS BY % INSULIN SULFONYLUREAS a8C_ GENERATION CHLORPROPAMIDE ToLaUTAMIOE 204 GENERATION Gisptztoe eLicLazt0e GUIBENCLAMIDE W omer than insulin, drugs ending % “Ine” con couse > SULPONYLUREAS couse hypoglycemia > couse weight gain > CHLoPROPAMLOE sie. — Jaundice — disuifiram like reaction HO hypoglycemia > po such requirement MEG LITENEDES NATE GLINIDE REPA GLINEDE hypoglycemia — + ROH Lretsins Hj0] —* Dilukional hyponatremia + also indicated for Diobetes insipidus MEGLITINIDES > short aking L~ thr] + indicated in Post prandial hyperglycemia DRUGS ACTS BY OTHER MECHANISMS 1. METFORMIN PHENFORMIN > se 2. Megaloblastic Anoamia 7 more alud Metformin a. Latkic acidosis > more aw Phenformin Lot used now] > PHENFORMIN > has more alto Latkic Acidosis (noe used now] > METFORMIN 7% hak more alo Megaloblastic anosmia > 46 can also cause tatkic acidosis, ~ contraindicated in, CFT ' L | + voc for TYRE a Om = 0 Tick oF hypoglycemia — max. reduction in HbA. — can couse weight loss Y most Mo Metformin preferred in © + obese patients S 7% Sulphonylureat preferred in T 7 Thin patients > Metformin also indicatecl for PcoD [ reverses Insulin Resistonce] Q. TROGLETAZONE ROST @LETAZONE PIOGLETAZONE > acke by stimulating PPAR-F —? Reversal oF insulin Resistonce Sere a. Hepatotoxic > max. hepatotoxicity > Troglitazone Cwirhdrowh] % Rosi glitarone & Pioglitazone requires LT monitoring 2. Nat& water Retention * avoid im CHF & HTN 3. t risk oF m1 by Rosiglitaone 4. t risk OF urinary bladdir carcinoma by Pioglitazone 67 Ba GWCOSIDASE INHEBrTORS % Acte by inhibiting the absorpt” oF carbohydrates > GeaBose ® QQ MagutToL Nentecce! ‘[aqifcosidase 29900] | Aasor- . 82991, pase Flakvlence. > me side effect 99990 > cit im Inflommakor bowel dixeases coroohydraln larative colitis chron's dizease > hypoglycemic prophylaxis in AGL > only by Glucose NEW DRUGS 1. INCRETING > releases Insulins atocagON LIKE PEPTIO® I [moet Importane endogenous Ineekin] | pep 4 Coipeptidy! peptidase 4] Degradation a. GLP Agonasts > ExeNATeSED LIRA@LUTEDED alco couse weight loss (tiraglutide indicaked for Obesity ] > not eFFeckive orally . given Subcotaneously > cause hypoglycemia > b OPP INHTBLIORS > GITRA@LIPTIN VIELDA GLIPTEN SAXA GLIPTEN BLOGLIPTEN LINAQLIPTIN efrective orally Only DPPL Safe in renal failure > Linagliptine me sie > Nosopharyngitis do not cauge hypoglycemia yedvu 7 SIE oF INCRETINS * Pancreakitis 68 A AMYLIN ANALOGE > PRAMLEN TIDE 7 given by Subcutaneous rows 7 causes hypoglycemia ONLY DRUG INDICATED IN BOTH TYPE1 & TYPEQ DM 3 S@iT- a INHrBTTORS > cana DERDED W torined . DAPA GLEFLOZEN eEmpA @LteLoZIN > se > =? Infetkions - on — Genital track infeckions 4 BROMOCRIPINE > Reverses Insulin Resistance 7 Exate mechanism de Known Teouun conrex > Secrets > Searekes 8 guuco corticoids NA Mineralp corticoids Da PLOOSTERONE «Major endogenous Mineratocarticofd acrions 2, TNot, TH aU kts tH HYDROCORTISONE > Mojor endogenous Glucocortico! ACTIONS 1, eATRBOLEC ACTION carohydrakes (cHol breakdown to glucose Proteins breakdown fake breakdoon Lmainly fromm periphery 1 ca®* metabolism teyy 69 avoided 19 Drm myopatiles con occur CUSHING SYNDROME causes OStenporosis @. ANTE - INFLAMMATORY ACILON F mainly by inhibition of Chemotaxis J osed in inFlarmmatory conditions Citis* 7 cause delayed wound healing 3B IMMUNO SUPPRESSANT ACTION > Indicated in Troncplantab? a ukoimrpnity F bur predispose to inteckions 4. NTE CANCER ACTION > indicaked in [ oes > elt Th Raposi sarcoma ° 7 aero > cortisone like _ackivitey aicocorrecozDs C anti inelarnmakory] MINERALO CoRTECOIDS (TNA Pol feHORT AerENG, ALDOSTERONE, CORTESONE PLUDROCORTISONE HYDRO CORTESONE, boca ENTERMEDLATE ACTENG PREDNISONE PREDNISOLONE TRIAMCINOLONE LONG AcrtNG L 2! days J} DEXAMETHASONE BETA ME THASONE PARAMETHASONE max. glucocorticoid activity DEXAMETHASONE Trax. glucocorticoid _pokeney > BETA ME THA SONE | glucocorticoid 7% max. mineraly corticoid oskivitey —> HYDRO CORTISONE max. mineralo corticoid atkivity 7 ALDOSTERONE minerolocoyticoid tT max glucocorticoid ack ivity, > __FLODROCORTISONE. Glucocorticoid & aero mineralocorticoid ockivity > TRIAMCINOLE 6 5 DEXAMETHACONE M > minerlocerticoid activity BETAME THADONE PARAMETHASONE minerglocovticoid & zero glucocorticoid activity > BOCA 70 OSES OF CORTICOSTERDEDS PNTENATAL USES REPLACEMENT OSES OTHER USES Dexa] Bekamemmasone [Revte Adrenal insuFFiciendy | [INFLAMMATIONS For Fetal lung maturity |pddisonian crisis Ley iva | Aur tmmUNE OrsEASES TRANSPLANTATIONS. Chronic Adrenal Insufficiency! | ANTE CANCER THEARAPY Addison's disease Coy oral] ASTHMA HYPOTHALAMO - PITUITARY — ADRENAL Axts [HPA AxtSJ HYPOTHALAMUS = ——> RH v PITUtTRRY —_— ACTH a 4 SS} tnibition PPRENAL — + |alececorttenids Minerale corticoids HPA AXIS SUPPRESSION > occurs When corticosteroids are qiven contintovily for 7 auxs PREVENFEVE MEASURES 1. STOP UNNECESSARY USE OF Steroids A. ff indicated, prescribe Thm for < awKS 3B fe Indicated for long perfods , prescribe them on ALTERNATE DAY = Long acting steroids are avoidd 4. if indicaked daily & longer perfode -% DON'T sToP ABRUPTLY tapering should be cone OTHER USES | NON - REPLACEMENT USES 2. INELARnATIONS 2. BUT IMMUNE DISEASES E TRANSPLANTATION 3. BINTE CANCER THEARAPY 7 HL (Hodgkin Lymphoma] > NHL [Non Hodgkin tymphomal > UL [bymphoeytic levkermia) + Ms Eeutiple myeloma] 4 pSTHM A, 1 ROVERSE EFFECTS & CONTRA INDICATIONS OF GLUCOCORTICOLDS aa Lo] es eee cu > <3 R > 7 aS a oF] 1°? b> s 7] i - - ‘Serum POP VETAMIN 0 7 CALCLTONEN T + PTH [Parathyroid Hormone] 7 + Viramtno, 7 Serum coleium by + absorption } P Bone ca*t > used in osteoporosic + Excretion PTH, 7 Serum calcium by Resorption of Bone ~ 1 Bone ca™* causes osteoporosis calcitonin, + Serum calcium by moving co** to bone + t Bone Co + Used in osteoporosis osteoporosis DRUGS USED 2. VETAMEN © CALELTONEN Tatazzoes 4. BISPHOSPHONATES > prenGRonare) REGE ORONATE OLENDRONATE op 72 BrSPHOSPHONATES > inhibit osteoclasts Leone eaters) + poe For Osteoporosis Lfor any reason] > Highly toxic to oesophagus Preventive measures 1. Given on empty Stomach a. Given % full glacs oF waker 3. should not Lie down for a min. oF Jomin after taking Plendronale Risendronol. Zolendronaii Given IV once yearly t given orally POST MENOPAUSAL OSTEOPOROSIS. ESTROGEN + responsible for Post menoposnal osteoporosis + ActIONS BONE + 4 Formation BLoo 2 oP HL BREAST > +t carcinoma ENOOMETRIUM Ft corcinoma her 7 > clobing fatkors > Thrombo EMbolism > not preferred for Ry OF Pm Osteoporosic + earlier HRTLEstrogen + Progesteron 1 given , bur not now SERM [ SELECTIVE ESTROGEN RECEPTOR MODULATORS ] 2. RALOKIFENE 7 used in Pm ostenporesis 7 Additional Benefitz > ot BOL > 4 Breast & Endometrial carcinoma tisk > se + Thromboembolism a, TAMOKLFENE, DOLOXIFENE TOREMIFENE, 4 mese drugs have beneficial efrects on Bone Blood Breast [Strong erect] > beneficial in Breast cordooma > have detremental effects on endometriom >t Endornttriol cA Liver > & Trombo embolism 73 3) clomiPHENE Hypothalamus «=> [SNR Fen Feedboxk Pituitary a2 = 2) O] tmhibition ovary > [PROgeSTERDN /ESTROGEN > estrogen receptor antagonist at pituitory 7 Indicakion > Snovulatory Infertility NEW DRUGS 1 TERL@ARADIDE > @ PM contain 1-84 amino acids & activates osteoclasts > Teriparakide contaln PTH t I-34 AM & otkivata Osteoblasts 3 STRONTIUM RANE LATE > doAL RenuEry 7 stimvlakes osteoblastic activity 7% hibits osteoclastic activity oe i RANK 3 Denied} * soma vend Fa > monoctonal Ab aginst RANK L® on osteoclast] tf RESORPTEON ® owen falile overs -— 1@ cxenueus tick & hostile Y sper MAN MECHANESM™ comainen ocP LE4P) Inhibition oF Ovulakion PROGESTERONE ONLY PILE | MENEPILS Gq mucus thick & hostile lEmERGENCY / PosT COITAL] MORNING AFTER PILIS Bisioging oF irnplontation 74 COMBENED ORAL CONTRACEPIVE PILLS Estrogen > ETHINYL ESTRADTOL Progesterone =F LevoNoRGESTROL 7 posage > a tablet daily for al dayt from ist day oF menstrual cyde 7 no table: For next F day > 10 7 compilot”, a8 Tablebs strip c 4st Al Lablets contains drug next + tablets contains Fe 7 2, TR 2 tablet is missed Ss a. LF a tablets missed Toke & tablets on next day > Discard remaining tablets & Start arresh and prackice omer method OF contracept? c tt + BREAKTHROUGH BLEEDING > bleedi @ @ t-al doe 7 prevented by PHASTC PLLLS — gradual 1 OF Progesterone from 2t0 ai days POP / rmtNTPELS + contains ING > inorcartons 2. Trromoembolismn isk A. Lackakion C contraceptive of choice] EMERGENCY CONTRACEPTIVES 4. ¢0C > atoblets ot Styt + atoblers after labrc a. Por (ING? > 1 coblet ob Stort + 2 tablet after hrs or > ababletc ak start 3. MEFEPRISTONE > sprm - Seleckive Progesterone Receptor Modularor > oses 1. Emerqency Contraception 2. Induction OF abortion * Above 3 drugs should be Used Tin ene. CVS Cthrombe Embol is ri] oF) | weight gain CNS C Depression] Ro | chloasma cholestasis Im | | cancers pb >) to Breast em Lh | ? cervical cy | NON CONTRACEPTIVE GENEFITS omer Endo metriosic Eckopic pregnangy ibroid Put e eeu ehebeeeece B E N e re 1 a s MTFEPRUSTONE, Ovarian cyst Coc For Pop] Benign Breost Disease Tron deritieney syndrom Premenstrual tension syndrome Skeletal Digeace Lostepporos!é) Neoplasia [ endometrial & ovarion concers] 7 SPRm - Seleckive Progesterone Receptor Modularor > pcitons, 4. Progesterone R antagonist Androgen R antagonicts M > Morning after pill > Anduckion of abot” > Fibxoid 7 Endometriosis Breast cancer G meningjoma } a } Cushing Syndrome Steroids, 76 in endormetsium A Glucocorticoid R antagonist 1 F € P } Progesterone R tive cancers R 1 s ANTE NATAL STEROEDS BETAMETHASONE, DEXAMETHASONE, NATURAL ESTROGENS £, 7 EsrRONE &, > EsTRADIONE ey EsTREOL ‘Total Oose > im tamg per auhrs x 2 Doses > a4mg 7% tm @mg per lahrs x 4 Ooses > ay mg > predominant > predominant > predominant: im Post meNOPAUSAL PERIOD im REPRODUCTIVE PEREOD im PREGNANCY ‘ore. orok® agbr ABhT PROGESTERONES KB POTENCY | ANOROGE NIC ACTEVITY ast GENERATION ESTRANES| + tt and gewerntzon | GONANES| ++ + 3rd GENERATION +tt + A _GENERATEON tat | Pati Androgenie ast __ GENERATION and GENERBTEON, NOR - ETHENDRONE NOR — ETHINODREL NORGESTREL LEVONORGESTREL [ING] Brd_ GENERATION AB GENERATION DESOGESTREL NOMEGESTREL NOR QESTEMATE DRDSPLRENONE QesttDONE DRDSPLRENONE: + also has anti mineralo corticoid activity 7 Read and make the notes of following topics from the book “Review of Pharmacology” by Dr. Gobind Rai Garg. Insulin Preparations Dexamethasone suppression test Glucocorticoids synthesis inhibitors SERD Aromatase inhibitors Androgens Uterine stimulants Golden points a ftory neurobransmiter oF Brain} @ ot) BARBITURATES ]_BenaoprAzePines reolanan® GABA mimekics GABA Fatilitabory e8 X charred 4 duration t_ Frequency pac Steep Flat Enducers [+++ RX W sempormerne Addiaion| ++ ++ + L Amnesia | No + pureed Antidote XX FLOmMAZENEL [ansidote? BENZODIAZEPINES 7 includes DIAZEPAM —%_OKALEPRM Lattive mebnbolite] FLURAZE PAM NITRAZEPAM FLUNTTRAZEPAM 7 BaD are Long AGING dit ative metabolites > cause Hangover Foci in elerly 7 gj th Liver foilure 7% 82D NoT FORMING ActIVe merABOLITES s > ' a o 7 Lo? E> Iqooo Quality SLEEP Sleep orchitechture [ phases OFREM & Non - REM), maintolned frorbitwals € 82D + Distort the normol Sleep architecture Cquditys 7 also L Latency oF sleep onset FF quantity oF Sleep 2 pRUaS =F DEC For INsoMNIa. ZOLPLRE Mm 4 lokerey oF Sleep onset ZOPLCLONE Nok effete Quality ‘2PLE PLON not eFFet Quantity Non addictive 78 Normally, Balance bju Dopaminergic CDA) & cholinergic CAch) neurons % 8m Parkinsonism , this bolance is Last [Relative cholinergic excess bR == Ah DA Ach 100. 100 50 100 Normal Parcinsoniem DOPAMINERGIC DRUGS. 1 Levopopn a ovo v z & aoe rano® oh 28s sean” > LevopopA alone > ig Less porenr > as peripheral vopamine decarboxylaze errective than centro 7 DA causes PERIPHERAL SIDE EFFECTS 7 bd, + 7 Hypotension Blt > arrhytimias d, + 7 Hypertension an + > vomiting > carBroopa Peripheral Dopamine BENSERAZIDE Decarboxylase Inhibitors Ft ErRicngy OF Levoclopa 7 4 Peripheral Sle OF DA > psycHosis [dit excessive DA in brain) > all Partinsonicm drugs can cause Psychosic ou antipsychotic drugs can cause Parkinsonicm 7 Central sie cant be prevented by carbidopa 7 Psychosis > Dystinesia a AMANTADINE % asks by ‘Teleasing 0% From vesicle 7% aleo used as antiviral drug for Influenza virus 79 3 comtT cNHtBrroRS — & MAO INHEBLTORS MAO INHEBITORS MAO A mao & present at all places presenk mainly in Brain mekaboliges all substances metabolises OF SELECTIVE MAO & INHEOLTORS 7 preferred in parkinsonism 7 Includes SELE@rLINe RASAGILINE comT INHEGITORS + Includes ENTACAPONE 7% preferred @Ocapone > GBxic toDiver # 4. DOPAMINE AGONIST T_eRaoT NON ERGOT BROMOCRIPTINE PRAMIPEXOLE PERGOLLDE ROPINTROLE sarer Long _Aeting Ve > Gangrene 7 x Fibrosis - x ANTE CHOLINERGTC DRUGS [central Ach 4] > voc for Drug Induced Parkinsonism > includes BENZHEXOL (TRIHEXIPHENYDILT BENZTROPINE BIPERLDINE PROCYCLIDINE Ipoc FOR PARKINSONTCM > PRAMEPEXOLE | ROPLNTROLE MOST EFFECTEVE DRUG FOR PARKENSONTS( > LEVODOPR + CARBIDOPA OC FOR DRUG INDUCED PARKINSONTSM > BENZHEXOL 80 op une GABA? @ com H qaen pegradat” Transom wor Be k7 CHANNEL OPENERS DRUGS t GABA 1. PREGABALIN GABAPENTIN > prugs ack by releasing GABA > pec Fer Neuropathic pain dit Diabetic newropathy Post Herpetic neuralgia 7 Recent opda > MOA + mainly by ca** channel Ibibition VIGABATRIN visual Field contrace” C sje] t —. INfantile spasm Luse] VY Dona win + GABA TRansaminase INhibitor [MOA] boc for infantile spasm = > ACTH THEGABINE + Transport Inhibitor [GATA) (Reuptake Inhibitor] oF @ABe BARBITURATES + PHENOBARGLTONE 820 > prazepaAm LorazePam CLONAZEPAM cLOBRZAM Phenoborbitone con cause Hyperkinesia in children Doc for Fetnile Seizures + Diarepam Doc for stokus epilepticus —* Lorazepam used For obgence sefaures + clonazepam used in Lennox Gostaue Syndrome > cloba2om 81 a 4 qlurpmare Aertvery NMOR # AMPA H FELBAMATE PERAMPANEL Sie _Bone Marrow Suppression Used in Focal Seiaures 3. T-ca** CHANNEL BLOCKERS ETHOSUXLMLDE > used only for Absence Selaure 4 Nat CHANNEL BLOCKERS ¥ PHENYTOIN CIT in absence & myodonic seizures CARBAMAZEPINE Useful In GTCS & Focal seizures OXCARBAMAZE PINE roranamar |. cae aaa! sone ZONISAMLDE ecco DEoe vsed in Focal seizures RUFINAMLDE TOPIRAMATE. OTHER USES % 4 craving oF Alcohol > obesity 7 migraine prophylaxis > Bipolar disorder CARBAMAZEPINE > voc for Focal seinvres > bec For Trigeminal newalgia > can be ofed for piabstes insipidus [ Doc for ot > DESMOPRESSENT Bipolar Disorder {0c Fer QD -* LaTHtum] PHENYTOIN > Follows Zerm order Kinetics > emyme inducer > Used for Arrhyiimias too > used for @Ics & focal Seimres e cll in Absence & Mypclonic Setaores 82 ROVERSE EFFECTS 4 pane Drie Vee eee tee 5. k* CHANNEL OPENER RETIGABIN [EZOQABLN] + osed for focal seiavres does not ack on @Aer Sobtum VALPROATE Mon Na* channel Blocker co>* channel Blocker T Gee + Givtomate Doc for eres Pbsence also used for Bipolar disorder POVERSE EFFECIS Vomiting Blopecia Liver damage * Pop LAMOTRIGENE MoA + Not channel Blocker > > aren FL Glutamal RIE > STEVEN JOHNSON SYNDROME LevITERACETAM & BRIVACETAM + bind to a protein “sv? Ceynoptic vesicular protetn ) 83 PSYCHOSIS Cano insight) NEOROSES Cinsight presented 2. SCHTZDPHRENTA A. MOOD DrSORDERS a. MANTA b. DEPRESSION Cc. MANIC DEPRESSIVE PSYCHOSTS/| BLPOLAR DISORDER GENERALISED ANXIETY DLGCORDER PHOBLAS. op BuLTMIA POSTTRAUMATIC STRESS DISORDER, epee ScHT2DPHRENTA ANTE PSYCHOTIC DRUGS TYPICAL ANTE PSycHoTCS Lb, #1] AIVPLCAL ANTE PsycHertcs CSHT, HJ 7 most drugs possess bor properties . st SH, 3 > Bo, 5 SHTA a TYPECAL PNTLPSYCHOTECS, 2 STRONG Dg tt Typicol Antipsychotics Atypical Antipsychotics > FRLOPEREDOL [Highest risk oF EPSJ DROPERTDOL FLDPHE NAZINE a WEAK Dy # > CHLOR PROM AZINE THIORIDAZENE 3 INTERMEDIATE O, H > THLOTHIXENE CHLOR PROTHIXENE Ste EFFECTS 2, EXTRA PYRAMEDAL SYmproms CEPSI 2. Dystonias Ceariest] 2 Akathesia (meJ 3. Parkinsonism 4. Tordive dyskinesia ( latest] 5 Least risk of eps] Maliqnant neuroleptic Syndrome F me ala strong da # TREATMENT BENZHEXOL > Dystonias Loocd Partinsonicm Cooc] Pkathisia Malignant neuroleptic syndrome, cit in Tardive dystinesio PROPONOLOL «= Pkathisia Coc] DANTROLENE =~ Malignant neuroleptic syndrome {Doc} VALBENALINE > Tardive dyskinesia @. HYPER PROLACTINEMIA, 7 by FL Prolactin O,H Ft Prolactin F mie alo strong 0, # 3 Bch # + dryness, blurring OF Vision ete AH > vee more common % BH > sedation Weak D, # 6 Seizures DISADVANTAGES OF TYPICAL DRUGS 1 Sie 2. not efreckive against -tve symptoms BTYPLCAL ANTE PSYCHOTECS AOVANTAGES 1. lesser sie 2. EFFective against both Positive & negative symptoms DRvgs > clozapine > RISPEREDONE > OLANZAPINE, > PALIPERTDONE F QUEITAPENE > LLOPERIDONE > ASENAPINE > ZIPRASIDONE 7 20TEPINE > WRASLOONE > prtpreRAZOLe 9 PIMAVANSERIN SUDE EFFCTS Fb qlucose 7 > Lipide UPODYSTROPHY SYNDROME weight qain Chighest risk © clozapine 4 clanzapine J Insulin Resistance 85 CLOZAPINE SIE > Pgranulowtosis [dose indepedant) > Seinwres [dose dependent 1 > myocarditis 7 Sedakion Lmel QUELTAPINE SIE > cokorack ZIPRASIDONE > TOP (t Qt Interval J OSES OF ANTI PsycHOTICs : antr > psy > CHOR yay Tres > GULLE DE LA TOURETTE SYNDROME > chorecterised by Vormt THs [ abusive Sounds] 7k > HatoPeRiDol Conly FDA approved droq] 7 cLontptne 7 @DANAPACLNE, MOOD DESORDERS ACUTE MANIA > R oF Au Episode > SEDATIVES CAnti psychotics /82D] + LITHIUM 7 Prophylaxis > trrtrum — {poe} > LerHtum Lo > Leveonytes pu eybosis > Increase T > Tremors Cmel HF Hypotiyroldismn TL > Increase } polyuria uv > urine m > avoided In momers [ Limlom in pregnancy -> Ebstein anormal] > Plasma concentration Norms Revte mania * 0.8 ~ 1-AMEQqIL Prophylaxis * 05 — 08 meq/L Toxic > yamegiL 86 BIPOLAR DISORDER. > urHtom > poe For bipslar disorders > cARBAMATEPENE. > vaLproare > poe For Rapid cyclers + Toprramare 7 morrrgiNEe @NTE PSYeHoTECS BNE DEPRESSANTS > boc fer bipolar disorders in preqnancy DeFicleney oF monoamines (SHT > NA > DA) cause Depression 7 typicel anti Depressants > aces by TSHT Arypical anti Depressants > acks by ofher mechanisms TYPECAL ANTTDEPRESSANTS, 2 -MAO-A INHIBITORS > Mocte BEmIDE > aka RIMA R > Reversible I Inhibitor oF ™ + mao a> A @ REUPTAKE INHIBTTORS BD OX snr, THES pegradation ad [NON SELECTIVE ‘SELECTIVE > Tnhibit” reuptake oF SHT G Ne | > % Avoided in cardiac poriente > > indicated for Severe depression | > inhibit reuptake oF BAT can be used in cardiac patients indicated for mild to moduraf. _depression NON SeLective TCA Crricqdic antidepressants) > includes TMLPRAMINE DESIPRAMINE CLOPAL PRANALNE AMLTRIPTY LANE NORTRIPTYLINE > SIE Ach # ag HH Seiaures Brthymmios Metabolic acidosis a 87 SNRI (SEROTONIN NORADRENALINE REUPTAKE INHESTIORS] ats SHE eA taeNO > less sie > doc For Severe depression > pRvgs VENELAFAXLNE, DULOXETINE MILANACLPRAN DES VENELAFAXLNE LEvo MLLANACTPRAN SELECTIVE SEROTONIN REUPTAKE INHIBITORS > prugs FLpoxeTINE PEROXETINE FLUOKAMINE SERTRALINE CITALOPRAM Es- CITALOPRAM > pve For mild - moderab. depression depression + voc For all newotic disorders + Sle + celayed Esaulation % used For Premobure Ejaculation ATYPICAL ANTE DEPRESSANTS > paves BUPROPION > pnti- smoking dug AMOINEPTIN: } > reuptake TIANERTIN MERTRZAPINE AmoxAPINE > pv, aso ATOMOXETINE + Used in ADHD MIANSERINE oprotps > obtained from Opium Cerude extract oF Poppy plonts] > oPtpres > drugs derived from opium + mojor opin > MORPHENE > optorns + pia Like gubstances 88 MORPHINE % ate on Hy k,5 Receptors + stimuloth oF H,K,6 Receptors cause —* Anolgesia M. RECEPTOR FuNCTLONS S 4 Sedation > can cause coma B > analgesia > used in Severe pain © 4 constipation + used in diomhea Ro Respiratory depression > awoid in astirna & COPD 0 > Uphoria > Addictive drogs ™m™ > Meiosis ADDICTIVE DRUG PROPERTEES Tolerance > pose has tobe Td to ger Same eFFect > Tolerance donot develop for constipation constrict? oF pupil Dependence > Psychological > cRAVING > physical WITHDRAWAL SynpPTOMS. CLASSIFICATION OPIOLD AGONISTS 7 stimula all s Receptors [u,e,8] OPIOLD PARTIAL @GONLETS > blocks all 3 Receptors OPIOLD AGONEST - ANTAGONISTS > agonist at Hy receptors OPIOLD ANTAGONISTS F agonict on one (4), antagonict on offer (i) Paontsts > paves MORPHINE HEROINE Feo times More addictive than morphine METHADONE > very long acting , used in deaddics” oF opioid PETHTOENE. CODELNE | PHOLCODEINE | DEXTROMETHORPHAN J NOSCAPINE. LOPERAMIDE | DIPHENOXYLATE TRAMADOL / TAPENTADOL FENTANYL PL FENTANYL SUPENTANYL REMLFENTANYL CODELNE | PHOLCODETNE | DEXTROMETHORPHAN | NOSCAPINE cough Suppresants / Anti tussives indicated for dry cough 89 begradat” PETHIDINE an NOR PETHIDINE Lvery fong acking I > si€ + Seiwres Lon chronic usage] cit along t mao - Inbibitors LOPERAMIDE | OTPHENOXYLATE indicated for non - infectious diorthea > at in infectious diarrhea TRAMADOL | TAPENTADOL > mon F Mak, ot } couses analgesia > f SHT in Spinal cord FENTANYL, ALFENTANYL, SUPENTANYL & REMLPENTANYL highly lipid Soluble drugs used For anesthesia couses Post op. muscle rigidity [post op. muscle pain Clb succinyl choline] SUFENTANYL > most potent opioid REMIFENTANYL > Shortest” acting opioid Cdit metabolicry by Pseudo ced beyee A PARTEAL AGONISTS BUPRENORPHINE has cETLING EFFECT On respiratory depression oe es Pp 7] | 23 > ogonise @ K & antagonist @ + sie > hallucinations 4. ANTAGONISTS > oevas NALOXONE 7% Short acting 4 given Iv NALTREXONE 7 Lang acting , given Orally > poe For cule opioid poisoning + Naloxone > poe For maintainance in opioid poisoning * Naltrexone 90 4 4 4 OPIOID DEADOTCTION SHORT TERM ADDICTION TONG TERM ADDICTION Stop opioids REPLACE € METHADONE i Cless addictive & Long acting WITHDRAWAL SYMPTOMS couse less euphoria J =—_I__, 4 Sym. System @ opposste 1 oprorps 4 dose gradually & stop by & by RELAPSE PREVENTION -BH Bx NALTREXONE = CLONIDINE. PLcoHoLs PLCoHOL ETHYL ALCOHOL METHYL ALCOHOL 1 te. dehydroginae 4 L ALOEHYOE Ace aldehyde Formaldehyd Lid. denydroge nase| 4 Reto Acebic Acid Formic pot ETHYL ALCOHOL DrsULerRAM > inhibits Acetoldehyde dehydrogenase 7% used ag PLCOHOL AVERSION THERAPY > fnstead oF euphoria.» unpleasant symptoms occur on consuming alcoho! dit > ocetol ddyydt. DISULFIRAM LIKE RERCIION > paves © > CEPHALOSPORINS Csomed CHLORPROPAMIDE @ > GRISEOFULVIN ™ > METRONIDAZOLE P > PROCARBAZINE METHYL BLCOHOL 7 Both formoldehydt & formic atid can casise retinol damage & blindness > FomEPtz0L + doc for Memnol Poisoning PROGS 4 ALCOHOL CRAVING None _ — oF The Above bude 1 Read and make the notes of following topics from the book “Review of Pharmacology” by Dr. Gobind Rai Garg. Multiple sclerosis Epilepsy in pregnancy Lithium mechanism and toxicity Anti axiety drugs Golden points DRUGS AFFECTING FLOW L | ier ‘<— | Plasenin Paes wise! ee ‘rrembus] Liss Fiat Bleeding prevent” ARTERY VEIN ANTE PLATELET DRUGS 8 sorte” © GPab|Ma Enon sticky} 6 3 Spyefina Lexterioriar” © Plokeleks o Plobelers + © | roca ve eee Blood vessel Sti © © | aovd vesset =| & oxy Boe NORMAL INGURED 2 ASPIRIN 7 aut on TAR, ~ semooweet 1 ae on sop THeIpPIDENE 3. ABCIAEMAG TIROFIGAN, EPTLFLBATIDE ok on GP Tb] Ma 4. DRUGS Aer ON THAR, Phospholipids J Prothidonic Add =——________, Prostaglandins Levcotrienes Pagal Ha ——t———_ TKR. P@I. Pade! G Plotelets Endothelium omer TA, = > cause Aggregation Par, => Inhibit aggregation ASPIRIN > Lrreversible inhi 92 a. DRUGS ACT ON ADP + PDP Receptor =F PAY > prvas cloprnogReL TIOLOPLDENE > ese drugs Wreverstbly inhibit. Pa Yin > Bot are Prodrogs Cinackive] > Awivoted by cYPaci4 > OMEPRAZOLE Inhibit CYPACI9 + should not combine t these drugs 7 REVERSIBLE P,Y,q INHTBITORS CAN GRELOR TLCA GRELOR 3. DRUGS ACTON GP Mb] Uo > strongest ontiplaliler drugs ANTE PLATELET DRUGS ARE PREFERRED IN ARTERZAL THROMBOSIS ANTEFIBREN DRUGS / ANTE COAGULANTS ORAL ANTE CORGULANTS WARFARIN Bae > nbibit the action oF vitamin K > yakes 4-5 days to manifest it's action + as already formed clotting fatkors are tnt > wSed For maintainance thempy > teratogenic, Cit indicated in pregnancy * cause FETAL WARFARIN SYNOROME MONITORING > mainly oFrects extrinsic pomwary monitored by ProTrembin Time of INR 7 clortINg PRTHIOAY Extring{e palhway monitored by Proimrombin Time CPT] Intrinsic pathuwoy Monitored by activated Portial Thromboplestin Time NORMAL VALUES PT + ia-16 Sec Lv 5S) arr > ag~ 3a Sec [~ Sosec] On WARFARIN, Therapy, PT a-3 Limes the control value HEPARIN meinly affeds Inérinsic pathway » Monitored by OPT Wu > vtarrarin Yo > Heparin € > Extrinsic pomhieay, INT > Intrinsic pathway PT > Protrombin Time 93 PROTHROMBIN Time MEASUREMENT [wer LAB 2. LABS BEFORE WARFARIN THERAPY | aosec 15 see a0 sec, AFTER WARFARIN THERAPY | a0 Sec Bo sec 40 see ‘9 prererent tobe gives different control values for the Same sample 7 SowrtoN = Measure bolS Samples in SAME LAB INR C international Normalized Ratio] Ist Ist. > International Sensitivity Inder TNR | PT test: PTcontrol 7 value oF INR Will be some in all labs BLEEOING DLE To WARFARIN Ry by > FRESH FROZEN PLASMA C erp) Ry OF BLEEDING TENDENCY due to Warfarin -* VITAMIN k Rj PROTOCOL FOR BLEEDING Based On INR | | Li INDECTABLE ANTICOAGULANTS / THROMBIN L a] INHTBTTORS 2. INDIRECT Ta INHTZBITORS A. DEREcT Ma INHTBrTORS 2. INDIRECT Da INHTBrTORS C HEPARIN] Heparin + Anti Thrombin Heparin + Anti Thrombin 4+ a + Aneithrombin Activated AS YQ Antithrombin Activaked + man vistas +0 a 7 eens, AT inhibit Thrombin in compLEX Ld AT inhibit’ xa, (Heparin + mr + nad ia 7 LMH [Low Moleculor Heparin] inhibit Xa. > FONDAPRRINOS > smallest portion of heparin al thot ig absolutely necessary for anticoagulant activity X + Inhibit z0 ve FoNDAPARENUX HEPARIN 1, Rovte * sic or iv Inhibit Ba & Da Immediate Action > osefol In aux conditions Anticoagulant oF choice in pregnancy monitoring done by apTt 6. Antidote F PROTAMINE SULPHATE prop a sit oe Bleeding Heparin Induced Thrombocytopenia. inomeos HEPARIN INDUCED THROMBOCYTOPENTA CHIT] on > Trrombocytopenta occors: ontigen |e, THROMBOSIS present ee + poc > DIRECT THROMBIN INHIBITORS var DIRECT THROMBIN ENHEBITORS 7 prRogs wre O@ Leprrupin BEVALURLOIN ungecables ARgA RODE MELRGAGD ED DABTGATRAN > given orally DIRECT XO. INHIBCTORE > paves Waiver > wiversibie AEODSM aoe Aer DO) 8 > Becker wn EDD xA BAN An > _Pmragonist: ANTLCOAQULANTS ARE MORE EFFECTIVE IN VENOUS THROMBOSTS - indicated in pvt & Pulmonary Embolism THROMBOLYTIC DRUGS | TISSUE PLASMINOGEN ACTLVATORS /FIBRINOLYTIC DROGS 4 PLASMIN removes thrombus EPA Plasminogen ———_? Plasmin, > pres STREPTOKENASE Short acking» given iv UROKINASE ALTEPASE RETEPLASE tong acting, given as bolus TENECTEPLASE Tenecteplase -* Longest cicking 95 STREPTOKINASE > derived from Strepto coccus, > can cause ALLERGY + PNTEBODIES against streptokinase produced BLPA CRECOMBLNANT TESSUE PLASMINOGEN ACTIVATORS] + putepase RETEPLASE TENECTEPLASE 7% No allergy 4 NO antibody format occurs DRUGS AFFECTING CELLS ceus GROWTH FACTOR, Rec ERYTHROPOIETIN wec @- CSF am -csF Pupreters [IL - a1 Thrombopoietin ERYTHROPOLETLN, > INoteATIONS 7 Pnaumia dit chronic Kidney disease Anaimia dit BM suppression 7 overdose causes = > Polycyrmemia + DRUG * DARBOPOLETIN C Recombinant Erythropoietin] G-CSF & @m- CSF > INDECATION > Leucopenia dit anticancer rugs > pres @ -csF > PILgRASTIM PEG FILGRASTEM GM-CSF SARGRAMOSTIM MOL@RAMOsTEM TL-11 4 Used for thromboujtopenia dit anticancer drugs. > OPRELVE KIN THROMBOPOLETIN RECEPTOR AGONISTS > Used in ITP > RomLPLostrm ELTROMBO PAG 96 Read and make the notes of following topics from the book “Review of Pharmacology” by Dr. Gobind Rai Garg. Iron Vitamin B,, New antiplatelet drugs Plasma expanders Golden points CLASSTFICATION OF AMA BASED ON 1 CWDAL RUGS L Kills] STATIC DRUGS Linhibits grout] TYPE OF ORGANISMS CHEMICAL STRUCTURE source 7 PNTEBIOTICS & NON ~ ANTEBLOTICS MECHANTSM OF ACTION & Cell Coal! symmesis Inhibitors & Protein synmesis Inhibitors © Metobelizm 4 DNA < Membranes wrap CELL WALL SYNTHESTS INHIBTTORS > orvas Firmly, > Fosromycrn 7 osed for ort Bindt> = > BeTALAcTAMS Bacterial => BactTRACIN toca use only cell > crapsertn > osed in ta vali > vancomyetn BETA LAcTAMS 3. PENECTLLLNS 3 and ring is diffrent in 2 CEPHALOSPORINS eae different B lactams & 3 CARGAPENEME absent in monobactams 4 MONOBACTAMS, 2 PENTCLLLENG PENTCELLIN @ | BENIYL PENICILLEN Lumrrarrons 2 not effective Orally CAcid fabiled Shore acting Cit rapid tubulor secretion] 3 Norrow Spectrum A Resistance 5. Pllergy 97 4. PCED RESTSTANT / ORAL PENTCLLLENS s3[ | | poovo a 2. T DURATION OF ACTION OF PENICILLIN G > PROBENECID compete T Pentillin at tubular pumps > + duration OF ackion of Penecillin + DEPOT PREPARATIONS > BENZATHINE PENICILLIN @ 7% Longest acking Penicillin > PROCRIN PENICLLLEN 6 > pepot preparations ase givery by im Only 3. SPECTRUM OF PENICILLIN G Gram tive Gram —ive cocel Bacillus cocci Bacillus L L L 1 Gtrepto Bositius Neisseria not efFeckive Stophylo clostridium piphiheria Listeria EXTENDED | WIDE SPECTRUM PENTCILUNS A > ORMMPLETLLIN , AMmOxYCLLLEN ct > CARBENICLLLLN Ty Tacnrezuite xr pseuDOMonAL ™ > me2LocruiN: oRvES A > P2tocruLtn P > PLPERACELLIN W Vancomycin ts Nor EFFECTIVE AEAINST PSEUDOMONAS 98 es 4. B LACTAMASE INHIBLIORS encarta CLAVULENTE AGED + AMORYELLLEN *—€) ee GoLBneram ++ Ampreiiitn rersiinase Peaurose TAZOBACTAI + PLPERACLULIN: —s m + PEPERACLU pectling plocaace PRNICELLENACE REGLETANT PENZERELENE foniror eeteceeeas 7 OxAcELLEN N 9 NAFCELLEN D > DLCLOXACELLIN ° M METHICILLEN [most resistant] > marsh [ Memicillin Resistant Stoph. aureus} 7 resistance if dit alterat” in Penicillin Binding Protein 7B lactoms ore tneFreckive except 5m gen. cephalosporins 5. ALLERGY 7% GRIN TESTING done by Intraderna) Injeck of drug 7 CROSS ALLERGY > allergic tO one penicillins , all B lactams are allergic ‘except MONOBAcrAmS PENICILLIN @ INDECATCONS FURST LINE ORUGS IN. Lo Usreate p> AcrtNomyceszs & > syPHtLts T > Tetanus Mm 7 MENTNgococcus 5 } PravHiRax N CEPHALOSPORENS ast_GEn, and Gen. rd GEN am GEN 5h Gen EFFECTIVE AGAINGT am tive @m ive Gram 4ve ‘@ram ve MRSA am ~ive Gram ~ive Anaerobic Iidest specks 99 [ist_Gen. and Gen. Brd_Gen am GEN 5 Gen CEFAZOLIN | CEFOROXLME CEFOPERAZONE CePEPLME Cerrar PROLE, CEFALEXIN |CEFOXITINE CEFTREAXONE cePpraome, CEFTAROLINE CEFALOTHIN |cErmeTAZOLe — | cEFOTAXTINE CEFA LORLDEN|CEFOMANDOLE — [cEFTEZOxIME CEA DROXIL |CEFACLOR. ceFPopoxtmE CerrRarOEME, CERTEBUTEN MOKALACTAMS CEFLXIME, 41 BILE SECRETED CEPHALO SPORENES sore in renal Failure. 7 Indudes CEFOPERAZONE CEFTREAX ONE farce secnereo Gun mucnoatoL REENTS cof in > CEFOPERRZONE ,CEPTALAX ONG| R > uenmercan, fe > enyrHromyern 8 > nempren.un ie > Lencosmmanes ( ctenommretn3| iseage “?_Doxyevettne, ANTI PSEUDOMONAL CEPHALOSPORINS + includes. 3. DISULETRAM LIKE REACTION not to be given t alcoho includes 5 > a 4 PRoTHI cererrme CEFPrROME CEFOPERAZONE CEFTALIDIME [most efreckive antipseudomonal cephalosporin] CEPOPERAZONE MOKALACTAM CEFOTETAN CEFOMANDOLE, ROMBIN includes CEPOPERRZONE MOKALACTAM CEFOTETAN CE FORMANDOLE 100 CARBAPENEMS, IMEPENEM > errective againct Fam tive Gr Wve incl. Pseudomonas > Anaerobic. * Dehydropeptidase by Kidney metabolises Imepenem ropidiy > cUASTATIN 4 Dihydropeptidant Inhibitor + Imepenem + cilastatin must be given for desired action > sie > seires + cit in Epilepsy OTHER CARBAPENEMS 7 includes MEROPENEM DOR PENEMm ERTRPENEM FAROPENEm, 7 Resistant to dihydropeptidase Co cilastakin required] 7 CARBAPENEME are only drugs that ore eFfective oghinst bacteria producing Esallextended Gpettrom Beta Lattamase} CoocJ MoNoBACTAM BITREONAM 7% do not show crese allergy 7 efreckive only against Gm -We batkeria including Pseudomonas VANCOMYCIN 7 Not erreckive orally { nor AgsoRBEDI 7 qiven by fv > releases HtStTAMINE > RED MAN SYNOROME > sie 7 nephrotoxic > ototoxic > not eFrective against Pseudomonas > ose > Marsa [poc] + Pseudo MEMBRANOUS CoLLTES % cormmensal bacteria protect the GIT from infection F by competing Tt nutrition & producing BACTERIOCIN + Bread spectrum ankibiotics KilIg Commensals , which Predisposed CO SUPER INFECTEON 7 WBC forms a membrone > PSEUDO MEMBRANE 101 PSEUDOMEMBRANE COLITES 2 me organism responsible, a me cause 3. Doc > Clostridiom difficile > Srd gen. cephalosporins > clindamycin > oRAL vANcomycrN Lonly oral indicath of vancomycin] GLYCOPEPTIDES VANCOMYCEN TELCO PLANIN TELAVANCEN ORITA VANCEN, Do net couse DALBA VANCLN RED MAN SYNDROME, PROTEIN SYNTHESIS TNHIBETORS 2. TETRACNCLINES > a. CHLORAMPHENICOL => 3M > MACROLEDS @ 7 QurnpREsTIN mhibit the attathmunt OF CRN to A Site Inhibit the gotning oF aan Cpeptide bond formar” ] Inhibit Tranclocat fon 4. AMIND @LYCOSIDES gees by causing Misreading oF mRNA codon + only cidal protein Synihesic inhibi SINOING, Binding 8 BMENOGINCOSTDES. T TETRACYOLIN ES 308 bind @ Bos Ribosome Rest all bind at 50S ribosome 102 2. TETRACYCLINES braves TETRACYCLINE OXY TETRACYCLINE, CHLOR TETRACYCLINE DEMECLOCYCLINE = most phototoxIc y highest risk of pr oxy CYCLINE MENO CYCLINE 7 highest Vestibular dysfunction POVERSE EFFECIS K BT GIRDH [ Demectouycline? R o> Rickettsia Coot] I + Gronvlema tnquinale {oc} Lo tev 5 Atypical pNeumenia Cooc - macroupes ) ot kK > cholera £ oe} BF Luminal Amoebiaci¢ Cooc for amoebiasis > metRonrDAZOLE] 3. CHLORAMPHENICOL Poverse EFFECTS 2. Bone Morrow suppression 2. Grey Baby syndrome [clz in new borns J 3 MBCROLIDES rugs And Line drugs to Penicillins boc For ERYTHROMYCIN eal CLARITHROMYCIN L > Legionella eee 8 > Atypteal pneumonia Po pertussis ALLTHROMYCEN FIDOXOMICIN = Used in mild to moderafl Pseudo Membrane colitis 103 +> couses stirmlakion oF Motilin®@ in att + piorrhea is SIE 7 vsed In Diobetic qastroparesis [AAITHROMYCIN OTHER “THROMYCINS” > very tong acing > Relakively Short acking > non microsomal enrsyme OQ > microsomal enayme inhibitors + Fewer _drvg interoekions > _more drug interactions CLENDAMYCLN > Seureted in Bile > causes Preudy membronous colitis > used in anamobic bacterial Infections QUINPRISTIN + DBLFOPRESIIN + Bom ore streptogramins + indicated in vesm Coc “> DAPrOmYCLNI 4. AIMINOGLYCOSTDES DRUGS GTREPTOMYCIN ] # Not efFedkive orally [Nob obsorbed] GeNTA MYCIN sarkive moinly on Gm —ive C ind. Pseudomonas] TOBRA MYCIN snot efrcbive OM Onawobic batkeria NeTELMYeEN, « cidal drugs NEO MYCIN enephrotoxic. Cmax. by NeomycinI eee ian puditory Crpax. by Amikodnd KANAMYCEN * ototoxre ees ~< vesetvier Cmax. by Streptomycin scause newromvscular blockade [max by Neomycind + capREOMYCLN. is chemically not aminoglycoside STREPTOMYCIN, TB, Plague CAPREO MYCN KANAMYCIN and line drugs for TS. BMIKACIN NEOMNYCEN, Hepatic coma C given orally 104 BACTERICIDAL DRUGS CONCENTRATION DEPENDENT KILLING [CDK] x Teme teas Post & fing concentration above minimum cidal Concentrat”, more bodkeria are kite High & lese frequent: doses required Followed by AmINOGLYcoOsrDES FLUORO QUINOLONES. tong [at min. Cone Eo Kru inhibit DEPENDENT KILLING C1DKI Killing ackivify do not depend on concentration Killing depends on time ak which Concentrakh if above min. Kelling Cone. Small & multiple doses are given Followed by P Lackams Vancomycin ANTrEeroTEC eFrecT [ PAE] Time at which Supression oF bacterial growth occurs even When the concentra” Fallen below the minimum Inhibitory concentrot” PRE + > LBhrs > tong PRE < \Shrs > Short PAE All the drugs inbibiting Protein synthesi¢ or DNA of batteria have tong PAE PIERIOINE + PRGA + GLUTAMATE Suipenarmines —f rotie pced SYNTHASE. Dec ——> fFotte acto rearmervooeim Zeameriorram -$ prayoRe FA REOUCIACE TETRA HYDRDFOLIC AcIO [FOLINIC ACID) J ona 105 SULFONAMIDES /SULFA DRUGS paves ADVERSE EFFECTS GULFA DOXINE, SULFR CYTINE Aplastic anemia Bilirubin displacement > cause Kerniclervs in a> at GuLeR SOKAZOLE © 7 crystalioria eae SULA METHORAZDLE R > Rosh SULFA SALATING RF Reetytotion SuLrA DIAZENE s > se DAPSONE HF Hemolysis in @EPD dericinny + guifenamide T minimum rick OF crystalluria > SulFa Soxodole 7 Guifadoxine Longest acting > Bulfacytine Shortest acting > sulfasalazine > prodroq, 7 uses > olcerakive colitis Coo Rheumatoid Arthritts Dermatitis Herpetiformis > eq sulfadiazine + used for Burn dressing > popsone > Used for Leprosy ComBINATIONS 2 COTREMOXKA ZOLE TREMETHOPREM + SULFAMETHOXAZOLE > rabio for best batkericidal aekivity + ratio in tnblet to attain this rakio > > voc For a. SULPADOXEME + PYRLMETHAMINE + Indicated in Parasitic infections > malaria > Toxoplasmosis 106 DNA GYRASE INHIBITORS > DNA GYRASE introduces negabive Coils § helps In replication 7% DNAqyrose Inhibitors > Inhibit replicarion > chemically these are QUINDLONES QUINOLONES, 1 NALIDEXIC ACLD > used in oT A FLOORD QUINOLONES FLUOROQUTNOLONES prvee NORPLDXACIN: > osed in orr CIPROFLOXACIN oral DOC For Typhoid & BOC for ANRroX OFLOXACIN PE RLOXACIN SPAR PLOXACLN, LeVo FipxA cin PHoXT PLOXACLN + Long acting 5 also atkive ageinst anaerobes Gart PloxpciN > wimdrawnCcomses dysqiycenia] TROVAFLOXACIN + oral dda drogs Wide spectrum Lam tive & Gm -ivel cit in pregnanay & children C induce seiaures Cavoidad in Epilepsy] ch in Renol Failure ExcEPTLON do m7? | + LI > Phototoxiclty Cmax. t Partloxacin] RESPIRATORY FQ © > OFLOXACIN Mo MOxTPLoxAcint GF GATE Ploxaciny LevoPtoxpcin Lisomer oF ofloxacin, Long ocking 7 7 active against respiratory infections caused by am +1ve backeria Gm -Ive bacteria Atypical bockerta Mycobockeriony 78 107 DRUGS ACIENG ON MEMBRANES prugs ANTE PONGAL DRUGS PowrmYyxcn & Powwmyxcn E (coLZSrEN] Dapromycin, > voc For vRsA cause Myppatiy CsIe] used for Pseudomonan ANTE TUBERCULAR DRUGS FIRcT LINE ORvAS HF teoNtA2to R > RIFAMPICIN CREEND 2 > PYRAZENAMIDE £ > EriamevToL Ss > sthEPtOmYCEN RerLVETY] BACTERLA _[HEPATOTOXTC [PREGNANCY #_[eidat [om ¥ sare. R leicdal [Bom 3 care, z_|edet_te er [avoided _[ecatic [som x care seid ete x leads to Peripheral neuropathy, Hepakotonic Wu ingure metabolize by Acetylation N nerves couce GLE Ho Hepatotonte Should give on empty stomach Secrcked in Bile > Safe in RE Emayme Inducer INTERACTIONS Warfarin Replace’, Heparin oce Replace, omer contraceptive method pnki Mtv drugs = + RCIN replaced © RIFABUTIN 108 REFABUTEN, REFAMPECEN Enzyme inducer + ttt OTE oF ack? Longer acting Short acting Errective on ptypical mywbavteria ™.T8 SIE ho hepatotoxic, Hepakotoxic Peeudojaundice oveitis 4 OTHER USES OF RECN 7 Leprosy F meningococcal meningitis Prophylaxis Cast line drug] MENINGDCOCEAL MENINGETIS PROPHYLAMS ‘CEPROFLOKACIN REIN CEFTREAXONE: > Brucellosis Looe > coxyeyclin + ReINT MRSA, Pseudomonas t+ PyeaziNAmmDe C1] 7 errective only on jc bacteria > most hepakoboxic > caure hyperuricemia ETHAMBUTOL > prfeck Eye + Red qreen colour blindness Coptic neuritis] + Initially reversible , later irreversible > avoid in <6yr age children STREPTOMYCIN > net efeerktve orally Caivey by im) 7 vephrotexic 7 okotoxic > couse neuro muscular blockade, and LINE DRUGS 2 FQ © Floxodn Moxifioxacin, GakiFloxacin LevoFloxacin 109 a. INSECTABLE CAPREDMYCIN KANAMYCIN, AMLKACIN 3 LINE TOLIDE > used for vRSA CLOFAZIMLNE > used for moltibacillary leprosy A CYCLOSERINE =~ camse Nevropsychiakric SIE ETHIONAMLDE > —-hepakotoxic., hypomyroidicm DAS + hyporyroidism 5 NEW ORUGS DELAMINED } TOP Char Intervet] BEDAGUTLINE TS TREATMENT Rurce => OTS [ert cara INTENSIVE PHASE @ HRZE a ARZEs + | HRIE + CONTENUATEON PHASE | 4 HRE 5 HRE > pally therapy given mor - 18 > resistant to bom oH + R. > 1p > 6 monms » 6 drugs given cP > 1B monmS + 4 drugs given MULTE BACTLLARY LEPROSY CIN oom Once monly } el CLOFAZAMINE 300 mg once montily x 1a. ments CPAZAMINE 50M once daily x28 nsuperviset DAPSONE, toomg once daily x28d PAUCEBACELLARY LEPROSY Rctn DAPSONE soomq, too mg > Supervised > _unsupervised once monthly once daily x38d HEB imycobacteriom avivm comple] > alo HEV TREATMENT > REFABUTIN + ETHAMBUTOL + CLARITHROMYCIN PROPHYLAXES > AZITHROMYCIN Cweekiy) | CLARLTHROMYCIN ( Daily] 10 ANTE MALARIAL DRUGS + Plasmedium Kknowlesi Pre Erymrocytic Stage sporozoite osquIto 21 @ a mosquico | TREATMENT MODALLTEES core cLINtCAL, RADICAL L 4 B Erymroaytic EXO-Erymrocytic Stage stage PRIMAQUINE, > pers oN PRE ERYTHROCYTEC srAgE > Exo ERYTHROCITIC rage > > GAMETOGENTC STAGE > car ar on ERYrHROCYTIC SME > > cam couce HEmomsts In GEPD 7 dt in Pregnancy & infants DRUGS ACTENG ON ERYTHROCYTIC STAGE FAST ACTING ™ a a © 4 a R can also couse rmdlaria Exp Erymrouytic ctage Chypnezoite] ~ responsible for relapse erytmroagtic Stage Gametocytic stage PROPHYLAXIS 1 SUPPREGSIVE CABEAL, 1 + Ry Erymrocybic. Ry Pre Eryipocytic. stage stage, used for casual Prophylaxis used for Rodical core used to prevent trangmisston MOE Useful EO RY OF prevent moloria Deficiency Slow ACTING PROGUANINE PYREIMETHAMINE SULFA DOxINE, DOXYCYCLINE CLINDARYCIN 111 CHLOROQUINE + causes BULL'S EVE macuLoPATHY Lon prolonged usage for a-B yrs] uses R Rheumakoid Brinrltis € > Extra intestinal Ameobiasic ° > ve t > Lepra reactions 1 > rnfedcious Mononucleosis Pe > Photogenic Reackions Mahatma = = Malaria gandhi > Giardiasis PRIEMTSENENS aves ARTE SUNATE PRTETHER RIE METHER, DEHYORO ARTE MLSININS Fastest acting antimalortale effective against MDR short acting GL In 16t trimester bots ARIEMMESININ COMBINATION THERAPY LACT] > prtimisinin + Leng acting droq > poe for Chloroquine resistance > comernArtoNs LOMEFANTRENE + ARFEMETHER = > boc in Norih Estern Stobes BRTESUNATE + SULFROOXIME - PYRIMETHAMINE FOC For rer oF Indio TREATMENT OF MALARIA UNDER NVBDCP TREATMENT OF UNCOMPLICATED MALARIA ise Trimester P. vivax matoria Chloroquine Chloroquine P. faldparam malaria ACT Quinine mixed infection ACT Quinine complicated or jw Artesunale Severe or Cerebral , Molaria, act, 12 poe HERPES VIRUS nev = 2. Hsv -2, cmv INFLUENZA, He eRrirts Hey Reore cHRONTC Hey } ACYCLOVER, S GANCYCLOVER AMANTADINE > acke by Inhi osettamiver ANA miveR acts by inhibiting Newrominidase PERAMIVIR biting Unceaking Symmptomabic Ry ENTECAVER | TENDFovER LFirst line drugs} Lamzyoorn EmrRtctinGINE, Ten Earlier INP RIBAVIRIN Linholational] Present my Coral] 1. PROTERSE tNHTBrTORS 2. NS5A TNHOrTORS LEDLPAcuzR DecLaTacviR, NSS®& INHIBITORS SorospuutR, DASA BOVIR 113 co,cell 2. FUSION TNHEBETORS a. RTANHTeZTORS 3. TNFEGRASE INHIBITORS A. PROTEASE INHEBETORS PROTEINS Cenockived 2 FUSION TNHIBTTORS ENEQVIRTEDE MARAYEROE 7 bindg t Gp 4i > binds T CCR-B > not given orally > given orally + can't bind E CO, celIs T_CKCRy A REVERE TRANSCRIPTASE INHIBITORS comPrtirtve [Non comerretve, NATE LNucleotide (side) RT tohibitors) —|NNRTE (Non NRT I Nucleoside RIT INucteortDe ATE 1st GEN and Gen REDOVUOTNE TENOFOVER. le FAvEREN2 ETRAVIRINE LAM tVUDINE NEVERAPENE, RELPLVIRINE STAVUDINE IDEtAvrRDINE DEDANOSINE ZALCITABINE EMIRECLTABINE BRACAVER, SIE OF NRITS Peripheral neuropathy f Pancreatitis [max Tek oF Periphual Hewopaty > STAVUDENE| Jmax risk OF Pancreatitis > pIDANastNE otn. wish OF Peripheral natropamy —F WmtvuSINE Csarest NATE] JBone morro Suppression by > auewworne, lot predtepasit™ by, = _ppncaute, NRTES Used for Hep. 8 LF LamtvuonNe E> EMTRECLTABINE T > TeNoFovER. 14 3 TNTEGRASE INHIBITORS prvgs RALTEGRAVER ELVETEGRAVIR, DOLUTEGRA VIR 4 PROTEAGE INHTBITORS DRUGS RUTONAVTR LOPENAVER, AMPRENAVER FOS- AMPRENAVIR BTAZANAVER > Lowest risk OF Lipodystrophy syn. SAQUINAVER but can cause hyper bilirtbinemia NELFLNAVER 2 metabolized by CYP3A4 BR CYPZA4 Inhibitors themselves + Gtrongest > RITONAVIR- > RITONAVER BOOSTING + boost the offer inhibitors cause LIPODYSTROPHY SYNDROME Lalso caused by Atypical Antipsychotics] > ralcose > 1 Gpids F ansolin Resistance > we. gain HARRT > Highly Active Anti Retro Viral Therapy 1 WHEN TOR BI pakients irrespective OF co, Count a. HOW LONG =F Life. tong 3. WHer > Minimum 3 dregs from minimom a groups. > ANRIL + 2NNRTE / It 2tL +N T+L HF 115 1. AMPHOTERICIN B Amphotericin B u NB ES eee Tnpocelilor contents 7 cidal drug + not errective orally C given vi poe fer Severe fungal infections 4 infusion relaked reactions Cme} 7 Renal Tubutos ocidosis tT 4 kt Conc dose dependent J > Anemio LLPOSOMAL AMG, 7 4 nephrotoxicity + costiy +> poe for kala Agor a proves brves, KETOCONAZOLE FLUCONAZOLE > poe For Crypococcus & Candida infecions TITRA CONAZDLE VORECONAZDLE BOE For Aspergillosis POSACONAZDLE > Fungi static drugs > KETOCONAZDIE > enzyme inducer + cause gynecomastia 3 GRISEOFULVIN > bung! stakic high agFinity for KERettn = used only For Dermatophytosis (not preferred ow] > Food t absorpt? > com cause pisulfirom like react” > Relapses are common, 116 4 TERSINAFINE > Fungi cidol + bas high aFFinity for KERATIN — bee For Dermabophytoses 5. ECHENOCANOENS CASPO FUNGIN > used for Candida [oc - Fluconarole I Asp ergillosis £ boc ~ voriconarole I sia Meceanre 1. Bmeostasrs ‘}_rneestinel cats > boc i Lumina] Ameobiasis —% ~DELOXANTDE FoROATE Intestinal /hepakic. Ameoblasis > METRONIDAZOLE, fl TENEOAZOLE eon SECNEDAZOLE ORNEDAZOLE SPTRA NEOAZOLE % bisulFiram Like rxn can be caused by metronidercle group > METRONIDAZOLE @ > Giardiasts Looe) > Peptic olcer Component OF TRIPLE ORDG THERAPY] Po PMc Cooc3 T > Trichomoniasis Cooc) A + Anaerobic backeria Coot] Pmeobiasis Loocd a. LETSHMANIA KALAAZAR | VISCERAL LeLSHMANTASTS > poe + gle IV Infusion OF LLPOSOMAL AMPHOTERISIN B > Na sTEeDqLLCONATE > sed For mucocutaneous Leishmaniasis [poc} kalo paar > given im % MILIEFOSINE > only oral drug for Kala coor 2 TRYPANOSD mA, PFRICAN TRYPANOSOMLASLS/ SOUTH AMERICAN TRYPANOSOMEASTS | SLEEPING SICENESS CHAGAYS DISEASE early stages > SURAMEN Coed BENANEDAZDLE Loo] lake stages “7 _MELARSOPROL Looe] 117 PLATYHELMENTHES. Tapenorms + voc > PRAZTQUANTEL except Echinococcus granvlosus (D06 Topetoorm > poe for Echinococus granvloss + piBennarote Flukes > pec > PRAZTQUANTEL except for Liver Fluke C fasiola hepakical > poc for Liver Fluke > TRICLABENDAZOLE NEMATODES 7 poc for all nematode incl. larvae —* ~~ RLBENDALOLE > Except Fflaria + pee COI Emy) Carbamasine I Strongyloides } wermecrnn onchocerca 18 Read and make the notes of following topics from the book “Review of Pharmacology” by Dr. Gobind Rai Garg. Drug resistance CDK &TDK Factors affecting the choice of AMA. Glycopeptides Urinary antiseptics Drug of choice for different bacteria Drug resistance TB Antifungal mechanisms DOC for specific organisms Golden points POVERSE EFFECTS 2 a 3 4 ceu BM Depression Plopecia Mucositis + diorrhea Hyperaricemia excle SYNTHETIC PHASE [s] 7 DNA Doubled Merorre PHAsé (MJ DNA reduced to half GaP PHASES (6, & 6,7 Non Selective Drugs > bind to DNA S phase specific, Prugs > inhibit ONA synmesis mPhase Specific Drugs inhibit: mitosis a) n9 aii 2 ALKYLATING AGENTS Mom — © oer on ADVERSE EFRECIS 2 BM Depression Plopecia Mucositis > Hyperuricemra 3° Levkemio. Sterility, Diorrhea aosue Rugs. MELPHALAN MECHLORETHAMINE CrcLOPHOS PHOMEDE TSOsFArntOE, USULPAN CHLORAMmBUCLL PROCARBAZINE, NITRDSOUREAS, cause Lung used for cl te tun NITRDSOUREAS Rugs a, cARTOUSIIN Lomucrtn SemustENn can cross BBB > PLATINUM COMPOUNDS pru@s CISPLATIN CARGOPLATIN OXALIPLATIN > Mon 2 Alkylating Agents BIE tkytazing Agents cESPLATIN most emitogenic anticancer drug [poe > nephrotoxic. > oxotoxic ACROLEIN > me site of alkylarh 7% ONy OF Guanine, memonnunate [prevented oy ] verre MENA Fibrosis, chronic Lymphoid Levkemfa cause Disuifiram like Rxn used in Gliomas Used for COLORECTAL CARCINOMA, > Burs # Condansetron)] 120 COLORECTAL CARCINOMA REGIMES. FOLFOX REGIME FOLFTRE REGIME FoLINtc ACD + FoLiNtc ActO + 6-Fo * S-ro + OKALLPLATIN IRENOTECAN. 3, ONTE METABOLITES > § Phase specific o. Drugs affecting FOLIC ACLD METABOLISM b. DrUAS affecking PURINE merAoLtsm ©. Drugs afFesking PYRAMLDINE MmerRBOLESD G. DRUGS AFFECTING FA meTABOLISM FOLIC ACEO SYNTHESIS PTERIDINE + PABA + GLUTAMATE 4 pic > DIHYORO FoLte ACO [FHI CFolic Aci 2 mernoTRenTet pye Rose TETRA HYDRO FOLLC ACD CF, Levlinic Acid) 4 DNA MerHOTRERATE, + Methotrexate Poisoning by FOLINEC Act | LEUCOVORIN CtROVORUM con couse megaloblastic anemia hepatotoxic Doc For Chorio cortinoma me osed omARD +ud PURINES PYRAOEDENE Adenine exytosine euonine Thymine b. DRUGS AFFECTING PURINE METABOLISM Daves. 6 MERCAPTO PORINE } hepatotoxic 6 - THIOQUANINE CLADRI BENE PLODARABENE, 5 pec For Hairy cell Leukemia boc For CLL. 6 ~ MERCAPTOPURINE @ ~ MERCAPTO PURINE xantaine 4 xanmine oxidase 4 degradation oric Acid TZ ALLOPURINOL combinakion , T ALLOPURENOL combinakion & MP dose should be reduced PUATHEOPRINE close should be reduced > GMP ig the atkive metabolite of Azamioprine © DRUGS AFFECTING PYRAMEDINE MErAgOLISM orvas, 5 ~ Fluor opactL C5-Fu] > CAPECETR BIN > GemeirABIN > CYTARABIN > > mie sic oF 5-FU > 4. DRUGS ACTING ON rmITOTEC SPENDLE SPINDLE FORMATION centriole spindle couse Hand & foot syndrome given orally, metoboltged bo 5-FU Boe for Pancreatic carcinoma causes cerebellar side effects biorrheo Polymeriaation oF ToRULIN > Spindle Formation Specific for M- Phase of cell cyce. SPINDLE FORMAT? INHIBITORS SPINOLE BRERKDOWN ENHEBETORS VINCRISTENE VIN RUASTINE, PACLITAXEL SIE > Peripheral newropaisy stpoH se > Allergy 5. TOPOLSOMERASE INHTBITORS + NINCRIGTENE > Morrow Sposing anticancer drug Topoisomerase introduces neghtive cwilingS & aid in replication 4 Pl HTOPOLSOMERACE T_INHEBLTORS TOPOLSOMERACE T INHIBITORS TRINOTECAN, ETOPOSIDE 7% used for colorectal carcinoma | ANTHRACYCLINES % cordiotonic boOXORvBTCIN DonoRUsrCIN 122 con cause 2° Leukemia, cause cardiotoxicity prevented by DEXRAZOKANE ETOPOSEDE au BNTHRACYCLENES > 6. mrse DAVES BLEOMYCIN > marrow sparing > cause pulmonary Atbrosis L~ ASPRRAGINACE marrow sparing vsed For BL anergy, cause Aevte Pancreatitis couse | S303 ReTENOTC ACID Cearly in onset > used in Acute Promyelocytic leucemia Cm — Ami] > ats as maturation agents THALLDOMMEDE > used For multiple myeloma > cit Im pregnancy > couse Peripheral newropotny > couse constipation SMALL moOLECULES can be given orally Ingeckables SMALL MOLECULES 2, TYROSINE KINASE INHEBITORS obi le@| erle @| on ® epee chr. 8 chao, tajaa PHILADELPHLA cxRorMOsOME > pec For chronic Myeloid Leukemiq 7 IMATINIB 123 MONOCLONAL ANTS BODIES TERDSINE ———? CML KINASE, IMATENES GENERAL PROPERTIES 2. Bil end t fnib? A orally eFretive 3, metabolised by Microsomal enarymnes 2 emt 1 > trmartnt® Coocd N > NELOTENTS D> DASATINIB. @. WUNG CARCLNOMmA ater + oe « > | | 3 RENAL CELL CARCTNOMA Poo PAZeTINTS, OF AXETE NIB S 7 SORARINES. S > sontrtn16, 4 HEPATOCELLULAR CARCINOMA = SORA FENES. 5 GIST [Gastro Intestinal Stromal Tumors] S * SUNETINIB Lt > Imarrnre [oocd R > REGORAFENLE + also ored for colorectal carcinoma 6 MALIGNANT MELANOMA D > oABREFENTS. vo VEMmURAFENTB T > TRAMELTENTS MEDULLARY CA OF THYROLD. > VaNDEeTANTS 2 PROTEASOME TNHIBrTDRS Bore zorm8 W tomar rugs CARFILZOMIB Ixazomi8, + Used for Multiple Myeloma 124 3 PARP INHIBITORS OLAPARIG. > ¥ D2r>DrFO RIB 4 CYCLIN DEPENDENT [Poly ADP Ribose Polymerase Inhibitor] used ip ovarion carcinoma > ovarian carinorea. fuse] > Poly > Ape > Ribose Polymerase KENASE TNHEBETOR CCDKL] Pargoctc.te > W caw 8 > ° > crcl gN > MONO CLONAL PNITBODLES > end c tmag? > ingeckables pRves CETUXEMAB PANLTUMUMAB RITUAT MUMAB TRASTUZUMAB PeRrozUMAB DARATOMUMAB OLARATUMUMAB bee beg oral drug For Greast Cartinome acke ON CDK-4» CDK 6 Breast can Cuse} oral Cydliy dependent Kinase inhibitor used for colorectal ca used For colorectal or used For NHL uted For Breast cA 3 SIE - cardiotoxicity sed For Breast CA vsed For multiple myeloma used For Soft tigsve Sorcomo 125 Read and make the notes of following topics from the book “Review of Pharmacology” by Dr. Gobind Rai Garg. Hormonal anti-cancer drugs Other anti-cancer drugs Drugs used to prevent toxicity on anti-cancer drugs Golden points 1. STEROTDS 2. DRUGS TARGETING THE CALCINEURIN PATHWAY NFAT} Pog, @© F catcinenrin Nept- Nuclear Factor oF Neat Coctive] Activated T cells L CxeDERO RINE] rhe racnoumes J lb. onctszomnes Ou astm 4 Ic. staoLtms © wyeR 7 TMMUNtTY evenasinus 126 . CNCLOSPORINE & TACROLIMUS > nephrotoxic 4 hepatotoxic, newrotoxie 6p sugor Kt Lipids a) > Hirsutiem > caused by cyclosporine © SEROLIMLS & EVEROLImus > cause BM suppression 3 ANTE MeTAsoLITES METHOTREXATE, BZATHLOPRING MYCOPHENOLATE. MOPETIL Leeunomrne 4 MONOCLONAL ANTI BODLES % monecional Ab and t ‘mag’ MAB + Fusion proteins end t © CEPT? > —— MAB. ? SOURCE > Animal Thigh risk oF atiergy > Mixture ~ chimeric > end z ‘kt mab” — Homanized = > end t © ZU mab? > Homan > end tT So mab” INFLEXIMAB ee FP crimeric Chigh risk oF tery] TRANSTUZOMAB => Humanized PANTTUMUMAB, + Human Lleost Hck oF allergy) ee ol CETOREMAR » RUTUXEMAB, TARGET > TH + Tumor TRANSTUZUMAB PERTUZUMAB 127 ee mob) > TARGET Tu > Tumor vE > virus > PALIVE LUMA * cr > Cireylak® % RBCIXEMAS + BEVACE ZUMAB > os > BONE > DENOSUMAB > oc 7 over > ALEROCUMAB. a Cholecterol = EVOLOCUMAB. Lz > 4immo- F A ADALTMUMAB a nity © CERTOLEZDMAB, E BTANERCEPT Tn INFLEXEMAB. oli GOLImMUMAB. For RSV Antiplatelee drog inhibit angiogenesis ‘osed for osteoporosis osed for hypercholesteremia MAB agolnst INF a used For RB erohn’s Disease Dac LE 2UMAB > mao against 1-2 ® BASTLEXEMAB used for transplant? EFALTZUMAB > Used For Psoriasis NATALEZUMAB > used for multiple sclerosis ECULE 2UMAS mab against Cy Used for PNH OMALEZUMAB, > mab ogainst 198 used For Bronchial astima INF-4 uel > ANAKINRA UL-6 H > TOCTLTZUMAB GARILUMAB —-_—osed For RA CO- STEMULATEON INHEBITORS > perrrcerr > sed For RA THALIDOMIDE > used for ENL 128 ut Zp > have autocrine erfecks (1ocal erretcs] > Based on chemical structure Q. PEPTIDE AuTOCOLDS > ANGLOTENSIN > BRADYEENIN & AMINE AUTOcOrDS + HISTAMINE > 6-H © LEPID AUTOCOLDS § > —PROSTAGLANOTNS > Leucorrtenes, THROMBOXANE i E RECEPTORS LOCATEON Betton BLOCKERS a. RUETQy Inflammation a, Stimulates RAS Promote worsfulness Ha [stomachs ig. [Pre synaptic | @RaKe tg H OF INVERSE AGoNTcT [TTPROLESANT C PLroLtsANT] used for NARCOLERSY Hg [Se Ha gtockers, set GENERATION 2nd GENERATION cress BOB, cause Sedok do not ass BBB, no Fedor ACh tf + _Anticholinergie sie occur RO Ach # Useful For Motion sictness Drug induced Partinsonism Muscolar dystoniag Useful only For allergy allergy PROMETHAZINE Cmax att™d TERFINADINE > hot used (TDR DIPHEN HY DRATHINE, FEXOFENADINE 4 TerFinadine metabolite DIPHENHY DRINATE AsremeZOlE ot used [1DPI PHENERAMINE LoRATIDENE CHLORPHENTRAMINE DES ~ LoRATIOLNE CXCLEZINE CETRIZINE , LEVO CETREZINE CINNARELINE AZELASTINE , OLOPATADENE + Topical 129 BANNED DAVES dit AT PROLDNGAT? [TDP] SEROTONIN RECEPTORS > F Receptors » 5-HT, - SHT, > S-HTg,g5 7 Present in Groin TOCATEON [AION [AGONTSTIANTAS. | ORUG oses [se snr | za Agonist BUSPIRONE Anxiety fr6/10 | evor erain | ve Agonist GUMATREPTAN [acute severe NARATRIPIAN | migraine Croc) ELETRIPTAN RETATREPIAN ng Blockers CLBEAPENE atypical Los prac] olanzapine _ | antipsychotics BHTac Agonist | LORCASERIN ‘obesity fea SATa| ore emesis | Blockers ONDANSETRON | DOC For GQRANTSETRON | chemomerapy | TROPESETRON —_ | Radromherapyy In- PALONOSETRON | ducech vomiting Post op vorniting Sar,| eer rFreri-| Agonists] CESAPREDE @eRd stali- | proinetics MOSAPRIDE Looe - Ppre] sis le > UPodystrophy Syndrome LUPLD AvTOCOLDS CFTC] 130 Phospholipids L pip ra Prochidonic Add cox Lox Prostaglandins Leveotrienes PaGal Ha JL + Ly Te PGIn Pan,iei® <™N Platelets Endothelium omer 8, uc, 1 ud, + LYEg. LTB, mojor Fund” chemotaxis Lreq Dy , LE, > Bronehoconstrictors + © Sronchial Asinma EFFECTS a Fever Poin Inflarmmations a Plrreters TAPy > Paqreqakion PEt, F Inhibition oF aggregation 3 Henrt DucTUs ARTERIOGUS > connects pulmonory trunk bo ada > Present ty 2UL > ie Kept open by PAE, PDA (patent ductus Arteriosus J TREBTM ENT ASPIRIN INDOMETHACEN, TeUPROFEN TRANSPOSIT™ OF GREAT VESSELS ALEROSTADTL [Faey analogue] indicated to Keep open the Om 131 4 Bi0D VESCELS 7 PaEy } cause Vasodilekion Par, > Tioprost (PGrg] > Used For Pulmonary HTN 5 UTERUS + PGE, POR > Pae, > Relores Lover segment OF uterus t Contracts Upper Seqment oF uterus > mrsoprostol CPGE, analogue] uses * Roortion > cervical Tipening in induction oF Labour > capBoprosT used For PPH Coc ~ oxyToCIN] 6 stomach Poe, + Inhibit. Proton Pump + TF mucovs | bicorbonake > vasodilation Prokecks for PUD > cox Inhibitors [NSAIDS] couse PUD > NSATD INDUCED PEPTIC ULER my by MesoPRosroL Cooc + PPrst + EXE Parag > Tt oven sacral outriow > LaranopRosr > d0C For Primary Open Angle Gloucoma > sie e Pigmentakion oF 2ris CHeberodwomia iridis] g growth oF eyelathes C Hypertrichosis] Fas Phospholipids STEROERS kidney Endofelium cns NSAIDs NON GELECTIVE COK INHEBETORS + risk oF PUD SELECTIVE COX-2 INHIBITORS lees vick oF PUD NON SELECTIVE COK INHEBETORS bavgs PSPERIN PARACETAMOL [ ACETAMENOPHENT IBUPROFEN, > NSAED oF choice in children DICLOFENAC, INDOMETHACIN > Gedakive. MEFENAMIC ACT PIROXICAM PHENYL BUTAZONE > Long acting USES Fever Poin inFlameot™ sie Pup PARACETAMOL / ACETAMENOPHEN 7 only NSAID Z 70 anti - inflammatory activity PEROXIDE THEORY > PEM is Inackive in presence OF HO, > Lese wick of PUD COX S INHTBIT THEORY + Pam inhibits CoK-3 in CNS. > Approved in children for fuer & pain A NaPAr (N-Acetyl Para-amino beni avinone Imine] bem oy Nee Inactive, NAPAL + NAPat haa high affinity for — SH qrovp * Glutathione produced by Liver binds 7 NAPOT & neutralises it 133 > Pom Toxcrry > cceurs dit 4 overdosage 2 Liver digeate 3 chronic Alcoholic + pnrtpote > N-ACETYL CYSTEINE [ood] ASPLRIN 7 only Irreversible cox inhibitor + antiplatter drug + cit in child t Virol infect? Lrisk oF Reye's syndrome] > can cause Hyperuricemia at theropeukic clotes > avoid in gout saicyLIsm Respiratory centre © L Hyperventila&ion L + cog 4 Respirakory Aikaloss —% Reversible 4 Hoos + tacete add repirin Metabolic Acidosis > irreversible > TrearmenT NOHO, + reverses metobolic acidosis > helps in aspirin Exeretion SELECTIVE Cox 2 INHIBITORS pros CELE cont8 4 Gi Toxicity ROFE COnIB * ME t not Ast line dregs VALDE COnTB 7 sroke ErORECOKIB PARECORTB WMERACORTB > Etoricoxib + longest acting > RoFeconib & valdecoxid i¢ wimdrawn 134 eure GOUT a. Nsatps [ooc) a. STEROTDS 3. COLCHECINE [most effective] Sle > myopathy severe diarrhea CHRONEC GOUT ORE ACID PRODUCTTON Proteins | Purines 4 xanthine @ | xonmine oxdase uric Acid > excretion © @ in birds { PULPNTOEN 4 vricase @ [L Formak” of uric Acid excret” of uric Acid LORtcoSURte DRvGS) LLOPURINOL > inhibie xanmine oxtdace Foc For chronic our PeBUXOSTAT > inhibi xanmine oxidase PROBENECID SULFENPYRAZONE, BENZ BROMARONE LESENURAD > Plenty oF Fluids should be token ft Uric Acid Metabolism @asGGatcnse> 7 Recombinant oricace PEGLOTECASE, NEntDs DMBROS oF ISTEROIDS SAARDS Y Pain & inflammation nO 2fFett on disease progression Fast_ocking Slouss down the diteose progrestion Slow acting pMaros 7 SAARDS > Disease Modifying Anti Rheumatoid Drags slow Acting Anti Rheumatoid Drogs 135 DMARDs CONVENTEONAL coke A g u I Mallika, Sherawat | Lbbbbude CHLOROQUENE > ved in moloria PENTCELLAMINE antidote for copper poisoning Cwilson's Disease] BLATHTO PRINE GOLD SALTS LEFLONOMMEDE TMmnuNo SUPPRESANTS METHOTREXATE > me vsed » DOC SULFASALAZINE > doe For ulcerative colitis BIOLOGICAL OmaAROS NF a ii-1@4 |u-e x CO- STEMULATY INHIBITOR A ADALIMUMAB | ANAKEN: roctttzumas [Renracert , c CERTOLEZDmAB SBRILUMAB © feu nc © ETANERCEPr pees oo L INFLEXIMAG a) vee te Goli__ goltmumag a RECENT ADVANCES ETIOLOGY OF MMERFINE VASODILATION INFLAMMATION > major inftommetory mediator + calcitonin Gene Related Peptide [carr] TREATINENT 2 NSAID a TRLPTANS Stimula SHT gin ® F Vasoconstrice? & + tnFlommot” ERGoTAMHINS TAIPrANS Doe ERGOTAMINE 4 more emetogtnic » not preferred 136 > Triptans can cause Coronary vasospasm > Inhibit the release of Glycoprotein From neutrophils SOC? Ged) synoviol cei 8o- eee 7 Inbibie mitotic spindle iq neutrophils ° ae 137 Read and make the notes of following topics from the book “Review of Pharmacology” by Dr. Gobind Rai Garg. - ErgotAlkaloids - Golden points LOCAL ANAESTHETIC AGENTS esTer AMEDE ba cocAINE, LI@NOCATNE, Sat PROCAENE BUPLVACAINE CHUDR.CAENE PRILDCAENE cs anaes ane TEFRA CALNE, ETIDOCATNE BEN70 CAINE ROPLVACATNE, DIBU CAINE, 7 only LA causing vasoconstrice? > COCALNE me used LA > Lrenocetne Shortest acting LA > chiorprocaine LA causing memaamoglobin + Prilocaine Max, cordiotoxic > Bupivacaine INFILTRATION ANESTHESTA es oe ood IE entry into blood 7 systemic adverse effec Adrenaline | Epinephrine added for long action 138 SKELETAL MUSCLE RELAXANTS CENTRAL > deprese CNS gana, ® 7 vtAZEPAm GABAR® > BECLOFEN 2,® > TEZANTDENE PERLPHERAL DIRECTLY ACTING DANTROLENE Rynodine R # wsed For malignant hypermermia Neuroleptic malignant syndrome Hepatotoxte NEURO MUSCULAR BLOCKER [NMI HJ / TNDIRECTLY ACTING DEPOLARTZENG MR sch > Shortest acting MR (<5 mini > cl in nerve & muscle inguries [ con coutle Severe byperkalemia) > lypermermia Cpredpitare malignant hypertmermial > FASCICULATIONS 4 responsible for post operative muscle pain [post operative muscle rigidity cavsed by FENTANYL] NON DEPOLARI2ING [COMPETITIVE DETUBOCURARINE, do not comse post op. muscle pain > release Histamine > cause bronchoconstrickion Lap CuRLUM® Creiease lest histamine] CURONIUM [no histamine releosedd BTRA cURLUM PAN CURDNEOM cic -Arep curcom Pree mvacurtum (shortest acting] ve RD RAPA HOFFMAN'S ELLMINATION + shown bY REracUriUN & Cis otra corium > MR OF choice in liver & Renal dikeose 139 GENERAL ANAESTHETICS Iv [ INDUCING AGENTS INHALATLONAL | MALNTAINANCE AGENTS Iv [ INDUCING AGENTS. THIOPENTONE, PROPOFOL KeTAMINE. ETOMLDATE, THIOPENTONE + highly lipid Sotoble very Fast acting Very Short acking dit REDtsrREBUTEON PROPOFOL > poe for Day care Sx > gngeck™ If painful DRDGS USED IN DAY CARE Sx Dr at ‘ Menmohen | i | singh > | | is 7 8 =o | Prime 2 | | 3 Minister : i | | Eromtpare > couse Adrenal Suppression | 4 KeTAMINE 4 kK Kids Liv anasstietic agent of choice in children] 4 & > Emergence reaction + 2% Thalamo - cortical junction [site of action A > analgesic m 7 Meals Céull stomach] 1 > P BP} IOP} ICP [fv anossthetic agent of choice in Shock. N > nmpn # Lovoided in Glancomea & head ingurys € 7 Encellenk Bronchodilaror 140 DISSOCIATIVE, ANESTHESIA INHALATIONAL | MAINTAINANCE AGENTS erHer InFIa- CHLOROFORM mmoble “) CNeLoPROPANE TRILENE, NETROVE OALDE HALOTHANE, Non - ENFLURANE infla- 2 Sevorwrane. mmotle | 160 FLURANE DEC FIDRANE METHORY FLURANE XENON, Mac Lminimum Alveolar Concentration] > min. conc. In alveols to produce anaecthecia > mac ‘fa PoreNcy Highest mac > Ngo [loan] Lowest MAC > METHOXYFLURANE, BLOOD sowALLtTY > Inversly proportional to speed of ancscmecia > measured by Blood 2 Gas Partition co -eFFicient > highest = 3 memoxyflurane > Lowest > kenone y desflurane BOYLE’ MACHINE 7 4 pressure oF anaxswiesio. machine > sneery measures 3. colour CODING Nap cyclo propane, Om Entonox (no +053 07. 507. blue NEELA orange SANTRI Blace & white Blue & white teed @. PIN INDEX SYSTEM alr o oa, No co, > #57. Coy, < 3-87. cyclopropane Entonox pepe raat ao 141 XENON F closest to DEAL ANESTHETIC AGENT Pnesmetic Pnalgesic mR Fastest acting sore Smoomh Induct” & recovery > costly Read and make the notes of following topics from the book “Review of Pharmacology” by Dr. Gobind Rai Garg. LA-important points Spinal and epidural anaesthesia Suggamadex Halothane Anaesthetics of choice for various conditions Golden points 142

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