PHARMAKO KINETICS > FFect OF body on Pruq PHARMAKO DYNAMES > EFFett OF pruq on Body PHARMACOKINETICS > aka ADME STUDY = Absorption — Distribution orn. — Metaboli sen ROUTE — exerekion ABSORPTION % MOVEMENT OF DRUG FROM SITE OF ADMINISTRATION 10 BLOOD % LIPLD SOLUBLLITY - Single most important Factor in absorpt — LIPLD SOLWBLE DRUGS ARE ABSORBED > FORM OF DRUG Ho === Htt on He te xT ~ Tonined form of Drug is toakr Soluble — Non Tonined form oF Drug is Hiptd soluble — RUG Is ABGORBED IN NON - JONI ZABLE FORM > Mectum ~ WHEN THE MEDLUM TS SAME, THEN THE DRUG WILL CRoss DRVG MeDrum Foam SOLUBELITY | CROSS | Radic Reid Non ionized Lipid Soluble Bagic Basic Non jonized Lipid Soluble Radic Basic tonired Wolter Soluble Basic Bciclic tonined Woker Soluble — Aeidic Drug [ASPIRIN] + moinly absorbed from stomach — Basic Druq [MORPHINE] moinly absorbed from iniestine patBro AVAILABILITY FRACTION OF GIVEN DOSE WHICH REACH SYSTEMIC CERULATION > Bio Availability 7 determines the DOSE High bioavailability % Low dose Low bioawailobilily 7 High close Factors © Absorption + absorpe” 4 Bio availability + absorpt” > 4 Bio availability Bio ouaidebility oF drugs given by TV rou is ‘irst Pass mukobolismn re systumic. ist f | Pre sy muro! + First Pass mitoboligm — J Bio ovoilability {First Pass mitobolism —* 4 Bio availability NTG LU Nitro Glyarine) has high first pass metabolism SUB LINGUAL ROUTE i Prefetred Advontages 7 Fast acting > can be used in No first pass mutobolixe Sele odministot” 12 possible DISTRIBUTION FACTORS. © Uri soLUBILETY -> most important factor Liptd Soluble Drugs > Higher Distribution Wokw Soluble Drugs > Lowes diatribubion @ PtAsmA PROTEIN BINDING 7 PPB > Loto distribution @ Barrters CIRM VENTRICULAR ORGANS [ No Blood Brolin Borie] crz Cowmoreuptor Trigger zone] Vomiting Met caused by > Anti emekics nei Psychotic algo has anti emebic property Arter desizuble atkion , we con spit! ingest Excreted 100% esurgences the extra doze | OtSTRIBUTEONVOLWME OF DISTRIBUTION Vd * i va AMOUNE given by IV > crses Po = 182 = a0maJL 5 Va = is = st > case Po = BD = 10 mgt 5 vg = ie jou 0 > cases Pe 10s a mgiL 3 100 vg = 2 = 5ou 7 a % VOLUME OF DISTRIBUTION Vy % AMOUNT OF DRUG IN TrSSUES more vg + more distribution CHLOROQUINE OACING BOSE brug & maximum vy £>1300LI mosHy distributed in Liver joae But siti OF preferred action 18 RBC ‘moet oop LODING DOSE [LD) — Initial high doze given to Start the preferred action - [lo = Vg % Targer Plasma conantation — WW depends on Vg A Target Plagma Contino” — warwracianal MAINTALNANCE pose — [mp = clearance x Targer Plasma conc — Mp depends on cleorance 6 Target plasma conc.METABOLISM,EXCRETION ELIMINATION > Termination OF atkion of Bq = ELIMINATION 7% Includes Metabolism & Excretion Metabolism Fare OF meTABOLISM ® active — A acive @ active — Petive DIAZEPAM —> OxeZEPAM @ inactive — Arkive TproDRUG] LevopoPAR ACC. OF Parkinsonism] BIM of METABOLISM > To MAKE A DRUG WATER SOLUBLE PHASE 1 REACTIONS > mostly catabolic Reattions > tnaudes PHASE 1 REACIIONS > mMesHy anabolic reatkioné > indudes — oxidation — Glucuronide Cre Phase Reatt”J - Reduction = Glotamione — Hydrolysis — Roky! = Gycbaakion = Metiyl = _Deamination = Sulfa > Purpose of PHASED > makes the drug Waker Soluble > Purpose of PHASE L > makes funcbional Group to atfoth the drug ENZYMES > Divided into Micro somal Enzymes > Inside the microsomes Non Micro Some! > but side the microsomes > Microsome Cendoplasmic reticulum > > only Microsomel enaymes con be induced or inhibitedWARFARIN HEPARIN] case. 100 Breq 100 Breq 5D microsomal 5D non microsomal Emymes — |» =) Enzymes —tT 490) 50 Drug 50 org case Along T RLFAMPICIN Lemyme inducer] - Me — ame — sonme —? SONME 100 oreq 100 Oroq 90 microsomal} '5D non microsomal Enzymes |p 2 Eniymes, or +) to Drug 50 orug = rug dote & be increased — No change required cAseA Along T CLMETLOLNE Lemayme inhibitor] — SME — OME — SoNmE = —? 50 NME 100 Brog 100 Broq 10 microsomal ‘5D non microsomal Enzymes. — | ng Enzymes ——a +490} to Drug 50 prog — rug dose & be derensed — No change required ENZYME INDUCERS ENZYME LNHIBTTORS q GRISEOFULVIN vit VALPROATE P PHENYTOIN k KETOCONAZOLE R RIFAMPICIN Can*t CIMETIDINE s SMOKING Cause CIPROFLOXACIN Cell CARBAMAZAPINE Enayre ERYTHROMYCIN Phone PHENO BARBITONE Tohibit? ISONTAZIDE most of anti epllephics 7 ENZYME INDUCERS most oF anti biotice ENZYME INHIBLTORSEXcRETLON GLOMERULAR FLLTRATLON > Lipid soluble drugs filtered easily Waker soluble drugs also Filtered > Filtration 4, Plame Protein binding > @ GR = RBEMIJmin 7.5 Ur|hr ~ a50 Ler] Days + @ourpur oF urine + arloay TUBULAR REABSORPION > 997 OF GFR ig reabsorbed — Lipid soluble droge reabsorbed — Woker soluble cirugk excreted > or drug & media are some > drug absorbed drug & media are different > druq not absosbed + acidic drug poisoning [Aspirin] , R by NOHCOg [forced Alkaline Divresis] Alkaline drug poisoning Campheramine , R, by NHaci [forced acid pivresis]} TUBULAR SECRETION > dit purmps | trangporters in proximal tubules. 7 These transporters are SaTVRABLE — Penicillin ix short acting — Penicillin + Probenecid 7 Long acting — Probenecid hat higher affinity for Eronspories oy Prevents Penicillin secretion SOME MORE FORMULAS RATE OF ELIMLNATION [R] > incomplete parometer R MOONE OF Dreg Eliminabed Time CLemrance [cul > comple. parameter a > RB Pe = Plasma contenbakionHove ttre Ce),7 too btu. 50 tte as { ts as {tp 6.25 > ky, For most drugs it constane @ tu, = obrs » after 1 day How much drvq remained in body How Much drug eliminated from body, tou ve + pose can't be calculoted DOSING INTERVAL | FREQUENCY Can be known ty, & volume oF distribution Lvq] ty, L Clearance ad eta 0.693 x cu ORDER of KINETICS FIRST ORDER KENETECS ZERO ORDER KINETS + Fraction i¢ constant PERST ORDER 100 ce eva Line 20] [ase 50 4 1 Libr oas | ahs 25 L J {tor 033 | |ishe as JL J bib 0.50 the 6.35 R a ty> Mojority drugs Follow First order Kinetics DRUGS FOLLOWLNG ZERO ORDER KINETICS are REASON LERO > ZERD ORDER KINETICS w > WARFPRRRIN 8 —* ALCOHOL | ASPLRIN T > THEOPHY LLLNE v > TOLGUTAMLDE Power + PHENYTOIN > order OF Kinekics depends on Enayme Sorurakion Te enaymes ore abundant — Follow aSt order Kinekice > a ip emymes are Limiting fackor > Follows ZERD ORDER KINETICS (spruRATION KtNertcs]+ © RERINITY, 7q INTRINSIC. g fertycty’ DRUG, RECEPTOR, AFFINITY > INTRINGTEC ACTLVLTY > CLASSTFLCATION OF DRUGS PGONTET > PARTIAL AGONIST > INVERSE AGONTST PNTAGONIST = REFINETY, + es ROG RECEPTOR, ACTION ability OF a drug FO bind to a receptor ability to produce action after binding to receptor BASED ON INTRUNSLC ACTIVITY Maximum intrinste activity (t2] Submarimum intinsic activity [o to +1) Opposite attion to agonist [—ve] NO atkion [o] bur interrerec T omer atkivity TNNTRENSIC. g ——> acrevery t Signob traduction Mechonism ACTION CLASSTFLCATION OF DRUGS BASED ON STQNAL TRANSDUCT® MECHANESM @ INOTROPIC RECEPTORS 7 Exomples + Rostest atting receptors not g c peeptera Fonotrepic ne 7 GABA, receptors FON receptors > NMDA receptors Nyy receptors AMPA receptors 7 SHTg receptors@ Enzvmarte RECEPTORS aka TYROSINE KINASE RECEPTORS [CmosHy assotiated enayme ig Tyrsine Kinase] eo nee = frame > Examples cytokines P Prolactin L Insulin 4 Growth hormones @4q- PROTEIN coupLeD RECEPTORS LGPCRI cer 4 prin Parenaline Bdrencline Ta me 4 1 2 ton dann tke on B receptor ackt On & receptor aaa ne 4 1 SHmulakes G proiein GHimulates & protein: 4 J Peeve component Petive component 7 cAMP * com — THR — vasoconstrick™ — Bronchodilat” G PROTEIN @ Stands for GoP/ qe binding protein Components. a > GDP binds bere in resting Stabe B ft Girase a = luhen G protein stimulated, phosphorylat"” occurs, GOP converted to GTP 4 components Seperakes B&T components are inactive a CGTP ig active Produce one of Following atk” on 7 came com ack” of ionotropic receptors & component algo hos GTPase activity > converts qtp to qDP + G proiein Stabitiant? occurs > Recyling oF G prokin@ INTRACELLULAR, RECEPTORS @. CYTOPLASMIC RECEPTORS . . b. NDCLEAR RECEPTOR, only Upid Soluble drugs ackt rough these receptors F Stowest acting Teceptors > commony named an NUCLEAR RECEPTOR SUPERFAMILY Nuclear Reaptor c+ Covticosteroide > PPAR e Glueo 7 Gex Hormones &e nainaralo > ira oO 713, DOSE RESPONSE CAVE LoRc] peuperbol 7 HYPERBOLA SHAPE . + Log DOSE RESPONSE curve [ioq PRC] R R Z > 6S Shaped curve [ stqmo1D cuRvE) y > Clinically more oseful thon DRC BS yO © @orency a 2 7 left sided curve ig more povoerful (a) » . > Right Sided curve ig less poweful(8) x R > relates to PoWwER yo tS errccacy > relakes to efeck regardless oF dose > © ig more efficaceous D ig lesc efficaceous cose |® | © © o 5mq | to ° 1K tom | a0 to |-s0 20mq | 35 20 lao oma | 35 30 8 mq | as 440 Potent] EF Ficacy > EFFicoqy 18 more important thon poktney < respect to RSlope telabed to SAFETY + prog t Jecc Slope ig more safer Drug C deep Slope i Bmq tom4 D>PHRRMACO GENETICS @ G-6 PO OEFICIENCY > G-GPp prolects Rac from free radicle ingury > PRIMAQUINE SULFONAMIOES NITRO FURANTOIN FURP20 LLDONE © AceryLATION > emyme + Neat CN Acetyl Tronsferage ] > Frsr INH > no response SLOW TNH > Peripheral newopothy > S > SULFoNAMIDE CoAPsoNE] H > HYORALR ZINE T > Ink P > PROCRINAMIDE 7 SHIP Drugs con comte SIE @ Gch INOUCED APNER Sch [ SUCCENYL CHOLINE] > moccle relaxant > shortest acting [K5min] ~ dit Pseudocholinesierate > uted For Endotrocheal Intubation PTYPLCRL PSEUDO CHOLINESTERASE 7 merabelizes Sch in 30 minutes > couses prolonged APnea THERAPEUTIC DRUG MONITORING £1DM] casa 7% AIM > reduce BP From 160 > IROMM Hg, Presyibed drug @ @ oma For 1 Week, check BP ofter 4 week, Change the dose accordingly case2 > Epilepsy Patient » Prescribed DRUG © @ 100mq, thenrequired plagma concentrot? = 10-20 NIL check plazma Concentrak® & change the dose accordingly hot used commonly > crtreria To use Tom 1 RESPONSE CAN'T MEASURABLE 9. LOW THERAPEDTIC INDEX DRUGS 3. INCONSISTENT PHARMACOKENETIC DRUGS 4 + Tom done For 5 > Antibiotics Drug > DIGOXIN Possecsing > PHENYTOIN Lmost anti epileptic drugs] low > LorHtom Therapeutic > TRICYCLIC ANTE DLPRESSANTS CICA) Index > Immuno SUPPREGANT DRUGS > CYCLOSPORINE > TACROLIMUS CLENTCAL TRALLS = > Testing OF drug in humans PHASE Tt > done in HEALTHY PEOPLE + We cane do Efficacy TESTING 7 mrp LEmaximum tolerable dose] con be found > Phase T cam also be done in Patients for Toxic drugs PHase TL > done in patients [20-200 number] EFFICACY INDICATION con be Known, PHASE «or > done in poients Lupto 5000] > multicentric troilt done Covers different gtnekic make upJ 7 EFFICACY CONFIRMATION can be known PHASE = + Post marketing study done [ mox. no. of patients tested J > RARE SIDE EFFECTS can be studied 7 CHRONIC SIDE EFFECTS Can be Studied Fon APPLLCATIONS INDA > Tnvestigational New org Application 7 Applied Tefore starting clinical trails NDR > New Drug Application, 7 Applied wefore marketing the droqPLASMA CONCENTRATION & TIME GRAPH max + Max plastna conc, can be obtained depends on dosage Chould lie bw MIN EC & Max TC Wb Metllreyeces Concentrakion time in eohich concentrate? becomes max. tellg the RATE OF ARSORPTION Area under the curve tell the EXTENT OF ABSORPTIONTYPES OF DRUG ANTAGONTSM PHYSECAL > physical presence of drug Stops the act” of omer [charcoal] CHEMICAL, chemical reat” stops ine action Crnractos] PHYSTOLOGTCAL, PHARMACOLOGICAL PHYSIOLDGTEAL ANTAGONECTS F ases on different receptors produces opposite efitcts 7 Histamine Adrenaline 4 4 4® Pa® L + Broncho constriction Bronchodilation > Histamine iz physiological antagonist oF Adrenaline PHARMACOLOGICAL ANTAGONEETS 7 acts om same receptors to produce opposié: effects 7 PPRENALINE. Propronolol + tL Bak Pak L 4 Broncho dilation Broncho consteiction + Propronolol i pharmacological antagonist OF adrenaline.ENZYME INHIBITION COMPETLTLVE > Non COMPETITIVE Drug can not bind to enryme swbstrali complex > prog con bind to enzyme| enayme Subsholi. Complex > dreg Mainly binds fb enayme Substrofi Complex ON comPETITLVE conperireve a pos compere [| LINE WEAVER BURKE PLOT | DOUBLE RECILPROCAL PLOT non competitive competitive uncompetitive Normalcyp alc iqg cYPACI9 > CLOPIDOGREL ——* acrtve > PpeL — PPL ackg ag Competitive inhibitor ~ clopidegrel should not qive cyp alc a] Cc + Clotting > WARFARIN 9 7? P > PHENYTOIN PPLECOMBINED EFFECT OF DRUGS 4, ROPITION / SUMM ATION ea ata =a a. SYNERATEM > ata =o 3. POTENTIATION 7 ato #5 4. BNTAGDNICM zy ata 64 ADDITION /SumMMATION —> Shdividual errectk oF a drugs, simply acldad SYNERGTEM > coTrimaxo20L€ > SULPHAMETHOARZ0LE = + TRIMETHOPRIM [Bocteriocidal ] Leackeriostatic) Leackeriostatic) POTENTIATION + LevonoPa + cARBTDOPA Conatkivel > EFFicacy oF Levodopq ses ANTAGONISM 7 combined eFFeck OF tod drugs Will be lesser“SHEAT GLANDS: PAR SYMPA~ THETIC sysrem 7 Preqanglionic Fibres are shorter in Sympathetic System Preqanglionic Fibres are Longer in para sympathetic System 7 Postganglionic Fibres are Longer in Sympathetic 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 Fr ON, 7 NT Geureted by the post ganglionic Fibres of paragym. Sysiey > ACh > NT Secrered by Porasympaimetic system is Ath + CHOLINERGIC SYCTEM 7 NT Secreted by postganglionic Fibres OF Gyrnpamhetic system + NA — aka, ADRENERGIC SYSTEM — EXCEPTION, postganglionic Fibres orsweatglandeseenl > Ach PARASYMPATHETIC eveTem SXMPATHETIC SysTEMm HEART 1 * +++ OTHERS r rE Bronchus > Brontho constrict > Bronthodiloz® qr > Diarrhoea = ConsHperion Bloddar > TF Urim OuEFlow 3 orine ouk Flow Glands >t Sewetiong => Seerebione Pupil > miosis > mydriasis PARASYMPATHETIC SYSTEM ORIGIN, cronial nerves = + -3,9,9,10 Sowral nerves > 2|,3,4ACETYL CHOLINE [Ach] CHOLINE slowest step * uptoke of choline + Paro, sympatictic ackivity HemicHorgaitum> Vesalmico. BOTULINUM TOXIN Ach Esteroge Inhibitor FT Paro sympaletic atkivity 4 PHY6OSTIG@MINE RECEPTORS OF Ach NICOTINIC ® _LocArion: [__Muscartnse ® vocatton N, 7 Gonglio ™, > Stomach Ny Nes Ma > Heart require Optimal Stimulor” ™3 > Bronchus fn both hyper & hypo qu sHrnulat muscle weakness Bladder occurs Glands Popil PARASYMPATHOMIMETICS DIRECTLY ACTING INDIRECTLY ACTENG > directly ackt on receptors Fates byTing Ach AchEsterace F INDICATION PELOCARPINE | Fupti_(M5@) [meiosic | angle closure BETHANECHOL Atonic bladdar METHA CHOLINE) myocardium (M,@] | cardiac Suppression [Tachycardia CARBACHOL — | Common Action Nicotinic® Muscarink ® Emax. nicotinic ackion > CARBACHOLAChE # REVERSIBLE AChE #F UZPED 6OLVBLE PRUgS WATER SOLUBLE ORLgS PHYSOSTLG@MENE NEOSTEGmMINE Lnot lipid Soluble] qr > F orally given qr > X > Ingeckions BeB > ~ > central trfecks tnt Bea > x > no Central cefects Pupil > > used in glaucoma Pupil -* x > no effect on pupil LPED solvBle DRUGS — USES 1. ANGLE CLOSURE GLAUCOMA + by Physostigmine 2. PTROPENE POISONING > prRoPINE, > Muscarinic receptor blocker Cm,,m,,m3] + cross BBB > oc for atropine poisoning > Physostigmine easol_Nucleur oF 3. SENTLE DEMENTIA { PLIHIEMER’S OEMENTIA ee > dit degeneration OF dholinerqic neurone in Acquiring retaining mmo Bozel nucleus oF meynert > TREATMENT PHYSOSTIGMINE — not used > Peripheral action leads to Side errects TACRINE > has only Cental ackion > Was the boc > disadvantages > very Short acting 7 hepatotoxic tm Some D > DONEPEZEL > Long acting Rg > RIVASTTQGMENE > non hepakotoxic Gobind + GALANTAMENE * Doc for Almzhieme’s disease WATER SOLUBLE DRUGS 1, NEO stTrgm=NE a. PYREDOSTLG MINE 3. EDROPHONTUMWATER SDLUBLE DRUGS - USES | MYSTHENIA GRAVIS 4 Re against N,, Receptor Nyy Receptors under stimuloted 4 MUSCLE WEAKNESS Ny Receptors overstimulaked 1 CHOLINERGIC CRISIS EOROPHONTOM TEST > iw edrophonium given > very short acting L 1F the condition improves for lomin — Mysthenia gravis Tr the Condition worsens for lOmin 7 Cholinergic crisis TREATMENT > NEOSTIGMINE or PYRLDOSTEGMLNE PACH Nj, Reteptors @ ™ receptors 4muscle weakness Side efrecks > Rec > NEOSTIGMINE + ATROPINE 2 COBRA BITE > Nn Ht + Neostigmine + Atropine -* — Ryoc 3. POST OP PARALYTIC ILEUS + by Neostigmine 4. POST OP URINARY RETENTION 7 RF by NeostigmineTRREVERSIBLE AChE #F ORGANO PHOSPHATES 1. MALATHTON 2. PARATHION CARBA MATES 1. CARBORYL @. PROPOXUR, > Highly Lipfd Soluble > can cross intact skin > Ach mR @ > Hed coma, mR @ > bur, + BP M3 R @ > Pinpoint pupi! 1 secretions Diarrhoea Urinary incontinence Bronchoconstriction > Ir Pinpoint pupil ®@L aye y Poisoning + Secretionz © 7 THR, TBP can be seen rarely (dit N® Stirmvlation] Muscle weakness occors usually Cdlt Nm® overstimulation] TREATMENT 1 ATROPINE + doe For OP & corbamake poisoning > by Ww reste, Im every 5 min till signs OF Ptropinizakion Ocors + L seatkions +> most reliable | specific Sign > mydriasis > most commen sign > HR > 100 7 cantt reverse muscle weakness & Ach REACTLVATORS Oxtmes Praupoxtme Cram] DI ACETYL moNoxIME COAM > ret poc > only erfective in OP Poisoning F PAM actz only peripherally 4 DAM has both actionsDRUGS PIRENZEPINE TELENZEPING HEART RYROPINE Coc) BRADY CAROTA BV BLOCK BRONCHUS | IPRATROPIUM ‘TEOTROPLUM) BRONCHIAL ASTHMA copp BLADDER SOLEFENACIN OXYBUTYNIN, FLAVOXATE, TOLTERODENE TROSPIUM bla. DAR FENACIN: ATROPINE, OVERACIIVE BLADDER or DETRUCCOR INSTABILITY, PRE ANESTHETEC MEDICATION orinary Retent™ cL in BHE Dryness Celt in chitdrend + Sweating 4 Fever + Hyper hernia, ATROPENE HomarRoPLNe CYCLOPENTALONE TROPICAMEOE FUNDOSCOPY Citin Angle Closure glaucormn, REFRACTION TESTING Blurred vision dic CICULOPLEGIA doe in + children - Atropine [max cyctoplegic act”, 73 daysd sAduits - Tropicamide (shortest octing] + Loss OF actornmodat™ ditm, # * ciliary muscle contrad” bby MCN Wenpaired HYOSCINE (scopolamine) MOTION SICKNESS PROPHYLAXIS BENZ HEXOL GrmivextPRENY OVO BENZTROPINE BIPERLDIN PARKINSONIS™ (0c For drug induced Parkinsonism > Abe] MOTLON -> VESTBULAR SYSTEM @ 7 cz © > vo+mei Very high altitudes (leh Ladakh] + 4 Po, boc For motion Sicknecc Bec For mountain sickness Ln PARKINSONISM , bolonce blu Ach & DA Sysiemn disturbed 7 AceTAZOLAMIDE > Hypoxia > MOUNTAIN SICENESS| HYOSCINE CENS Deppresant] > MOTEON sicknessNOR ADRENALINE. NA in synopge + sympathetic activi xT yMpal d © me|tyROStNE bora v @ Researine @ _QvANETHIDINE pA os Reuptake Inhibitor 1 sympametic ackivil TYROSINE Trrosine. JN NA RECEPTORS. % ay Location Petion Presynaptic a receptor IBtood vessels wasoconstrick” + acts like brake to sympametic eye Mydriasis Systern (Moin funckion OFX. J Prosthokic urethra |+ OvtFlow Post Synaptic a, receptor = _Praaosine (a#) used for BHP. 7 _indigtinqvishoble from a, © Pa > Acke on Adipose tissues > causes Lipolysis Pa Location Action locakion Action Heart THR POP Lungs Bronchodilokion JG cells Renin secretion [qtr constipar” Glodter 4 Suk FOW Glands 4 Seerekions ueerus Tocolytic Blood vessels vase dilation Skeletalmusclespindies! Tremors ver Sugars > a 7 vasoconstriction & By 7 yasodilation > errecr depends predominance oF type OF receptor 7 feort q Muscles F Baro > vasodilation > skin, Eolernal organs > o,>p, vasoconstriction8m hypoglycemia WARNING SYmproms > By + dle cympaihecic system stimulation Tachycordia Polpitakions + Have to toke sugars > LF sugars are not token , even then P, © > Liver @ Gioconeogenesis @ Giycogenolysis © aiycogenesis if % Sugor 4 Reversal oF hypoglycernia > B Blockers causes 2. masking oF warming Symptoms 2. po reversal oF hypoglycemia B blockers are contraindicated in hypoglycemia Sweaking 1g only reliable syrnptor oF hypogiyermia in diobekics on B Blocker medication SYMPATHOMLMETIC DRUGS > DIRECTLY ACTING DRUGS 7 INDIRECTLY ACTENG DRUGS INDIRECTLY ACTING DRUGS A Reuptake Inhibitors > cocALNE. > ne B. Drugs acking by displacement 4 TYRAMENE > present in cheese Cg) > EPHEDRINE } Nosol decongestants om o 7 Psevoo EPHEDRINE ee 7 AMPHETAMINES > cross BBB 4 Sleep & Pattent” span Uses Narcolepsy Csleep attacks] ADHD In Children Show TACHY|PHYLAXTS Cooc - memylphenican. Fost__ toleranceDIRECTLY ACTING DRUGS carecHolmINES catechol > Di Hydroxy Benzene com > abundant in GIT > catechol ortho memy transferase recognise cakecholamin. > not effective Orally ENDOGENOUS CATECHOLAMINES [Exogenous CATECHOLAMINES ADRENALINE DOBUTAMINE NA TSO PRENALINE DOPAMINE FENOLDO PAM DOPAMENE Rees on max in Ranal BV BR @ Heart aR @ 10 pq 1kq [min > Vasoconstriction uses a. CHE a. SHOCK + oLrqvRtA C doc] DRUG T DOPA in their name atts on D,®@, Omhers do not DOBUTAMINE > do mot atk on Dd, receptors 7 mainly aces on B, receptors > used for CHE FENOLOOPAM > stimula. only, Receptors 7 used in Hypertencive emergencies sep pBP HR Br | 4 Ba] trect EFFEcT ON Yip, | INDIRECTEFFECT On © | FENAL| PORENALINE EPINEPHRINE tT - - - + $144, Pa NORADRENALENE| | TT 7 Ww ¥ NOREPINEPHREN! Gis das Br TSO PRENALING. = + t cS ee Bi» Pa> Blood vessels contains Baroreceptors mainiy sense MBP(DBPI mer = pep +1 PP tose + + BR > PSS > LHR +o0BP + + BRO > SS > tur NA EFFECT ON HR 2. 1p ® person 74 2 Im @ person T transplanted heart > t [Eno Indirede attion] uses ISOPRENALINE > By > cue 7 Ba 7 Asma NA a ay > shock 7 Bp > cHF PDRENALENE > 4,Gp, 7% 2 ANAPHYLACTEC SHOCK > voc 7% Route 4 tm > Sc > conc. > 1 1000 ign in 1000 mI Solution Dose > O.5ml OF 171000 Concentration > re donot improved , repeat the dere tin IO min > IF still mot responded , Iv Adrenaline C1% 10,000] @ CARDIAC ARREST BLS. | no response Ww Adrenaline - 11000 — main veing CJugular veins] are preferred Next preferred route + Intraosseous Still Next preferred route -* endotrachealVASOMOTOR REVERSAL OF DALE a JORENALINE, srronq (24 4 ve BIPHASIC RESPONSE When Adrenaline given fv at high doses ob First BP increases L dit (ay >p,> Stimulotion] then BP will dewean» C dit py stimulation] When Adrenaline given Iv at high dose ta, plocter Exaqqerated Fall of BP occurs > vaSOmOTOR REVERSAL OF DALE 3n Pheochromoaytoma 4 4? adrenaline + pee SF R by & blocker, then vasomotor reversal OF Dole Occurs & deamh con occur. a blockers are CI in pakients OF Phenchromocytoma NON CATE CHOLAMENES sremuuares [| omvgs eto @. PHENYLEPHRINE EYE DROAS Mydriasis tout cycloplegia b METHOXAMINE vasoconstrick® MEPHENTERMINE used in shock MEDODRINE XYLOMETAZOLINE Nasal drops | Nasal decongestants OXYMETAZOLENE Nasal drops NAPHAZOLINE Nasal drops CLONTDENE Break for Gymp. System METHYLDOPA used for HTN ‘SALBUTAMOL Bronchodilation TERGUTALENE, Osed for Asthma by SALMETEROL fnhalabional rouk. FoRMOTEROL, RITODRINE Tocolytics ISOxSUPRINE used for Preterm labourars SYMPATHOLXTIC DRUGS A BIOCKERS 3,4 o, BLOCKERS &, BLOCKERS y BLOCKERS > —YOHIMBINE [no Clinical Use J > Selective & non selective #H used for HIN + Non Selective q #H can couse severe tothycardia Non Seletkive o H used for Severe HTN oo Selective & H used for mild to modurate HTN oy NON SELECTIVE IRREVERSIBLE REVERSIBLE PHENOXY BENZAMINE. PHENTOLAMINE TOLALOLINE uses Uses Pheochrome aytoma Cheese Reattion Clonidine withdrawal CHEESE REACTION Tyramine Tyromine | m0 Break down, mo | PAO INHLBETORS Suddin severe HIN [CHEESE REACTION] > poc Phentolamine . Tolazoline CLONTDENE WETHDRAWAL 7% donidine > 43 agonist > reduces Bp > suddun stoppage after prolonged use > = REBOUND HIN — dit upgradation of receptors 7 pec + Phentolamine s Tolazoline &, BLwckERS PRA LOSLN TERA ZOSIN DoxA Z0SIN ALU Z0s1Nuses 2 HTN + BHP [ooc) FIRST DOSE / POSTURAL HYPOTENSLON > od, H always storted at bed time Types Sin Sia ‘ates on oce8 on Prostakic urethra, Blood vessels TAMBULDEEN SILODOSIN > 70 postural hypotension > pec fer Normotensives t BHP B GLOCKERS Bit pa # Cron selective] ast Generation p 4 BF and Generation BH P, # > BLTEXAMINE Eno clinical Significance] > Bot used for cardiac indications > Non Selective @# have bol cardiac & non cardiac indications Selective B # hove only cardiac Indications Bronchodilak Blood vessel vasodi lak Liver bypoglyamia revercal 2.B, OF CAROIO SELECTIVE Or and GENERATION 6 # New > NEBIVOLOL Beko > BeTAXO LoL Blockers > BISOPRO LoL Be > ACEBUTOLOL Exclusively * ESMOLOL Lehortest acting pi, degrodad by pseudocsolinee J aE 7 RBreNoloL Myo > meroprpLot Cardium > CELLPROLOL > These are relatively Safe in ASiRma » PYD & DmJ2.INTRINSIC SYMPATHOTMEMETIC AcTEVETY CISA] / PARTIAL AGONISTS s ve s wR $ 1 s 4 aI to Ay 8 LEX 0 at ° Jef aye RI Za oe Rs : mn |Z a i a a aoe & a og Ws: @ oo Ss es Jo WOH a el I ie % 8 a 4 Nae an SH 8 @ Ie an 8 RS we ne meet Normal phenomenon 1@® stimulation > HR=10 10 ® stimulation > HR = 10x10 =100 B. Bp blocker Usage in normal person B blocker blocks acy. of M > HR = 10x8B = BO © B blocker usage in p blocker in a Bp blocker sensitive person, 7 Bp blocker blocks @ox OF R + HR = l0xa = 20 > Severe bradycardia manifests > So, Sensitivity Should be checked Z HR monitoring in p blocker prescribed patients + 9n These patients, partial agonigtt ore useful > ess chances OF causing Severe brady cordia (Safer drug] > Bur less erficaceous contain > CELLPROLOL Partial => PINDOLOL. Agonist > ALPRENODLOL Accivicy * ACEBUTOLOL 3 MEMBRANE STABLLEZING | Natchannel H/ LOCAL ANESTHETIC PROPERTY > indicaked in Arrhytimias > Mot indicated (M Gloucoma > cornea is protected by corneal refiex (Protective Reflex] Engony ftnsolt + Seimulat” OF Sensory 9. oF Trigeminal nee 4 Facial m. stimulazed + cortrehion oF orbiedlaris ocuti < eye closure Cooment REFLXD> comeal reflex ig masked T thece drugs 7 pRug@s Possess > PROPRNALOL Cmaximom] Membrane stabilising or METOPROLOL Local > LABETALOL Anesthetic > ACeBUTRLOL Property 7 PINDOLoL WATER SOLUBLE B BLOCKERS > at in renal Failure > prugs A > ATENOLOL N NapoloL Congest acting p 4] S > Soro Lot 3RO GENERATION B BLOCKERS 7 any BH T vasodilation property > vasodilation ig dit & blockage > ExanyPLes: LABETALOL CARVEDILOL USES OF B BLOCKERS Bia uses BIN 2 classical Angina [ cjz in variant angina] 3. ME chronic CHF COT In awh cHe] Arrhythmia BiH Uses 1. Glaucoma, a. Angina 3. Migraine 4 Essentfol tremors 5. Thyrotoxicosis ADVERSE EFFECTS | c/L B® 4 4 Rak > Bradycardia Sick Ginus syndrome 24 Conduckion > By Block 3 4 Contratkitiky > Acute CHEPal 1. ASHmMa a. Peripheral vascular pisease 3. 0m BH contraindicated in A FF ASThma B * Block CAv) c > CHE Lacute] BO DmACTIVE & PASSLYVE MYDRIASIS Erect OF DRUGS ON EYE > Lie Conwackion oF Sphicter pupillar > Active miosis contrackion of Dilaror pupiliac > Active mydriasis Relative overackivity OF Bilator pupilla + Passive mydriasis Active miosis > caused by Cholinerqic drugs Active mydriasis —* Coused by ot, agonists Passive mydriass > caused by Anticholinergic drugsQ@LAUCOMmA = 4 Hoe 4 Aqueos hurmor production + Aqveovs humor drainage > Aqueows Humor produced by Ciliary blood vessels 7 4, > vasoconstriction @© ss meanness } stimula &, receptors DIPIVERTNE APRACLONLDING } Stimulake post synaptic ay receptors BRIMONIOTNE > Bp > vasodilation * B, H canbe used tT Aqueovs outflow 7 Trobeawlar outflow 4 Uveosatral oukFlow a for = ul 1S Major path wou PGF, , | LATANOPROST > prugS + MIOTICS — poc For POAG PLLOCARPINEAoverRse EFFECTS LATANOPROST / PGF. Pigmentok” OF tris > HETERO CHROMIA IREDLS Growth OF eye lashes — HYPERTRECHOSIS Mrorics cararack Stenosis oF Nasolatrimal system BPRACLONE DINE Lid retraction BRIMONIDINE Brain Suppression > CIE in new born babies Tridocyclitis precipitar®CONGESTIVE HEART FAILURE Aum a 4 FLUID > DtURETICS a. Tt PumPINg = > TNOTROPICS DIURETICS LOOP DIURETTCS THIAZIDES > strong > Weak > shore acking F Long acting > used in cHe 7 used in HIN common SIE > + Not ? sugar 2 4 Kt > ? Lipids > 4 Ht > T uric acid + + 4 mg biFFerence. > Loop looses ca + 4 co®* P cor TNOTROPICS, a. py, ABONTETS DA DOBUTAMINE NA TCOPRENALINE. gids 2 2 > 15 camp 2. PHOSPHODIESTERASE INHIBITORS [PEI] AMRINONE MULRINONE also atts on Blood vessels + VASODILATION — ako + INODILATORS 3 pigarALts / CARDIAC GLYCOSTDES > digitalis inhibits Not kt erpase + NCX Inhibition + tea im wytoplaim + 7 com in ER oS + % contractility italig donot THR F no Tin Workload on heart> vagomimensc EFPECT + LHR + Conduction > useful in ATRIAL PLBRILLATLON > HR + oo —500 bpm 7 inefteckive Contrackions > Fibrillakions 7 aim of mx > 4 ventriaar Contraccions Digitalic ses Conduckion from abrium to ventricles DIGOXIN DIGITOXIN Cwithdrown I > mainly excreted by kidney > mainly mekobolised by liver c]t_Renal failure Cit in liver Foilure DIGOXIN: only inotropic drug that can be given ORALLY 7 Ale 1 Nausea, vomiting Cme] a Aithytkmias me_arrhy tenia > ventricular _biqeming most Specific | choratceristic —* NPATT Av Block Cron paroxysmal Atrial Tachycordia CAV Block J not seen > Peril Floher Mobit2 Type heort block 3 Gynaecomastia s J oxaoxan 4A. XANTHOPSIA | YELLOW VESEON SW scseoeuae + cemeroine > oestrogens DIGLTALES TOxtCtTY FACTORS Ting OLGITALIS TOXICITY PATHOLOGICAL RENAL FALLURE LIveR FATLURE METABOLIC a cost + Kt 4 mg QUINIDINE VERAPAMIL AMIODARONE THIAZIDES Mx OF DIGLTALIS TOXICITY a, Correck the cause 2. DOC for Digitalis induced arrhyMmiat > LIQNOCAINE] PHENYTOIN 3. DIGIBIND for Severe poisoningCHRONTC CHF cae: P07 26 cells, J 1 co Renin secretion J J x 4 Syrmpometic Angiotensinogen l J Carwad = | “lo vce Angiotensin “™N pre, Veins Arterties By on heart Angiotensin IT — eradyrinin J 1 L J TPRELWOAD — PAFTERLOAD tco vo #— AT,R — FAINA + LvH — Aldosierone 4 4 Death A Nat & Hao retention Jkt tht AIM OF TREATMENT a. 4 Work ad Fluid 3. 4 LH Ccardioe Remodelling] a 4 WORK + vAsopiLATORS ENO DTLATORS PRTERLO OLLATORS JVENO + ARTERLD OILATORS NITRATES HY ORALAZINE NO NITROPRUSSIDE, BCEL PINGIOTENSIN RECEPTOR BLOCKERS. a. + FLUID > Loop prurerrcs 3. + LWH Coardiac Remodetling] 4 These droge 4 morrattrY 1B BLOCKER ACEI PINGIOTENSIN RECEPTOR BLOCKERS . BIDOSTERONE ANTAGONISTS poe B Blockers CARVEDLLDL METOPROLOL BICO PROLOL ALDOSTERONE ANTAGONIGIS / POTASSIUM SPARING DIURETICS SPIRONOLACTONE =~ cause qynaecomostia EPLERONONEAcer C Ace INHIBITORSI > also inhibit Brady Kinin mekaboliam [7 Bradykinins] > sie > ory Cough Fingio edema > peves > carro Pett Ro > ieee. > LteINo Prt. © % captopril > ENALAPatL > EnalopriloE LF _Lisinoprit > RAmZIPRIL > Romiprilar > PERENDOPRIL = Perindoprilat Active Forms > moerr Pret > Moexiprilac > Poverse EFFcrs cough Angloeduma Prodrogs except captopril & Lisinopril Teste alteration [ sysqusea] Orthostakic | Postural hypotens® [max t captopril] Gt tn pregnancy cz im BIL Renal Artery stenosis at in Increased kt Lower the Tsk OF Diabetic Nephropatny rHepvreotvao tebudyoe vue ARBs Taste alteration [ oysqusea] Orihostakic | Postural hypotens™ {t tm preqnanay cit im BIL Renal Artery stenosis at in Increased kt Lower the Hisk Of Diabebic Nephropathy rHevost see cde pres CAnG@rotenstn (AT,] RecePTOR BlocKERS] Lo SARTAN S > Selective VAL SARTAN BF aT, TEL R OISARTAN } Recepror IRBE SARTAN r EPROSARTAN A Antagonists CANDE SARTAN N + TELMESARTAN > also stimulakes PPAR - 1 > used to Reverse Insulin ResistanceNEW DRUGS BNP CBroin Natrioritic Peptide] > cause Natrivnisis (4 at J > cause vasodilation BNP | nee CNeprilysin] begradat® 2. NASIRITIDE > Recombinant BNP + not given orally , qiven fv F Short aking > Used for Otu cases &. NEP INHEBErORS ACUBT SACUBTTREL > cepective orally ECADO TRIL VASOPEPTLDASE INHLBLTORS 3 7 Inhibit bom ACE & NEP > omar&drcL€D Sam PARILED 7 sie > cough AnqioedemaANGINA PECTORIS I CLASSICAL | EXERTIONAL TI VARLANT PRINZMETAL VASOSPASTIC. CLASSICAL ANGINA PATHOLOGY > dit atherosclerosig of small branches oF coronasy, artery » Isthernioa occors IScHEMEA + t EFfeckive Diameter OF artery L No poin ar © activity ° During Exercise /Exertion , % effective diameter oF artery Mok SUFFICE for Compeng akion — PRIN Occurs ALM OF TREATMENT ~ J Work on heortVARIANT PINGINA PATHOLDGY > dit SPASM OF MAIN CARONARY ARTERY > Pain @ rest occurs 7 ptm of TREATMENT + Dilation OF Coronary artery DRUGS I NITRATES D1 CALCLUMm CHANNEL BLOCKERS M =p GLOCKERS IG POTASSIUM CHANNEL OPENERS 1) NITRATES 7 ack by releasing No = tT camp — vasodilokion Neins Y Orteries: > moinly 4 Pretoad > pRogs GLYCERYL TRINITRATE / NrTROTRLGLYCERATE [ GIN|NTG] ISOSORBIOE prNiTRATE [ rONI ISOSORBLOE MononiTrate [imN] PENTA ERYTHRYTAL TETRA NITRATE CPETN] AMYLNTIRITE CAN] > @IN|NTG & ION > bas high 4st pass metabolism 7% Sub linqual route preferred > pec for aculi attack OF angina 7 ImN hag minimum 1st pass metabolism F Longest acting > PETN Shortest acting 7 AN > NITRATE FREE PERLOD > tolerance occur iF nitrokes continuously, present 7 to avoid tolerance, 6-8 hrs of Nitrali free period Should be maintained + NITRATES: L NO ‘SULDENAFIL 1 coun —thosthodiesteree peqraded Vasodilakion NITRATES should not be qiven & STLOENAFEL LRISK OF Severe hypotension]I. CALCIUM CHANNEL BLOCKERS 7 CALCLUM CHANNELS > Lryee > present tn cvs > TTP > Present In CNS 7 L= CALCIUM CHANNEL BLOCKERS BLooD VESSELS HEART RATE prrect | tNorrect| NET VERAPAMTL vasodilation yoer [iat [tT w DILTIAZEM vasodilation + 0BP |e + 4 BHP COLHYDROPYRIDINES] vasodilation 4 dap | * NIFE DIPEN MLD DIPIN NICAROIPIN CLENT DIPLN DIHYDROPYRIDINES Shovld be avoided in ongina CtHRI M = PoTAsslum CHANNEL OPENER NECORANGED + NO Releaser + kt Channel opener W B BwckeRS BA + LHR 4 4 WORK J vseful in classical angina, > B® Blockers ore CjT in vorient angina NEW DRUGS 1) BRADYCARDIAC AGENT > IVABRADINE @® GRAD Ne Not channels in SA Node @ 4 Ip blocker sje > visual Geutty| Funny current Cig] ae) F Brodicardiac agent > wabradin inhibit Not channel C Funny current] > sie > 4 visual auity + recently approved for CHE2. Rho KINASE INHIBITOR +> FASUDIL + Rho Kinase > couses vasoconstriction > Rho kinase > causes vasodilation > indicated in angina 3 METABOLIC MODULATORS > @ivcose +100 0, > Wo ATP Comer ports oF Body Fatty acids + 200 03 +> too ate CHeort] + FR require more 0 for some enerqy production 7 METABOLTC MODULATION = Making heart to otilise qlvcoze ingtead OF Fattyacids DRGs, 1 TRIMETAZLDINE 2 RANOLAZINE 7 also atks by blocking Not channels along t FA metabolism Inhibition Ma > ANGINA > Myocardial Ischemia [Reversible ] ML > Myocerdial infarction ( trreversible ] > NON - STEML > sTEmI Management MANAGEMENT M o> MORPHINE. S > STREPTOKINASE Oo > OXYGEN © > OXYGEN N 7% NITRATES N ? NITRATES A > ASPIRIN B 7 ASPIRIN ™ > MORPHINE.BLOOD PRESSURE > Lateral pressure exerted by roving column of BLOOD 0m WALL OF BLDOD VESSEL ANTI HYPERTENSIVE DRUGS 4, DIDRETICS + 4 BLOOD volume > 4 HARDNESS oF BLWOD vEsseL LY s. Sodium] 2. VASODILATORS 3. SYMPATHETIC SYSTEM BLOCKERS RAAS BLOCKERS I piuretres LOOP BIURETECS > strong > short acting THIAZLOES weak long acting T VASODILATORS 4. NO RELEASERS 7 Na NITROPRUSSIDE > HYORALA ZONE 7 Bom ave Fast acting + Na Nitro prusside > MICROPRIP SET used — 6h drops 7 tong term use 7 metabolised by 7 sie 2. L- CALCIUM CHANNEL BLOCKERS > VERAPAMIL DILTEAZEM DHP 3. KY CHANNEL OPENERS Mo MENOXIDIL Db > DIAZOXIDE H 9% BYDRAWZING Masala tears used in HIN. Emergencies a Leads to CYANEDE POISONING Antidote > HYOROXOCOBALAMINE Peekylation Sie+ > ‘DRUgE Cueine HaRSOTEEM) > PHENYTOIN > used for Alopecia 7 cyclo SPORTNE MENOXIDIL causes hair qrowth M7 Minoo. > avoided in young females DIAZOXIDE 4 Detreases the release of insulin > at in om > vsed in INSULINDMA TL SYMPATHETIC SYSTEM BLOCKERS 1. GANGLION BLOCKERS > ONY Receptor antagonists > TRIMETHOPHAN HEXAMETHONIUM > moinly used os Antidote for NICOTINIC POISONING 2 dy AGONTSTS > CLONIDINE } Bol are Safe in pregnancy METHYLDOPA Bol, con couse dry mow & Sedation + CLONIDINE Sudden stoppage causes REBOUND HTN > MeTHYLDOPA con cause Hemolytic Anaamia 3. A & B BLOCKERS IW RAAS BLOCKERS [ RAAS ~ Renin Angiotensin Aldosterone system] @ Qs ceus OKI L Angiotensinogen Renin cc 4 Angiotensin 1 3 K vce Angiotensin IL Lt vasoconstriction = <—— | PT PTORS| —+ Catecholamines tL ea + Alddsterone, t ONA L 7 nat & HORENIN INHIBITORS + piskD@ED Remi KOREN bonne orvas ENAL KDREN RENIN INHIBITORS > PLISKIREN » REMIKIREN, ENALKIREN RENIN RELEASE INHIBITORS -> B BLOCKERS TREATMENT OF HTN INC — 8 GUIDELINES a. BP Y 140/90 Lany one CSBP] DBP) can be considered J a. START > BP % 140/90 Not controlled inspite OF LIFESTYLE MMODTFLCATION L Low Nat diet & requiar exercise] 3. FIRST LINE ORUGS [IF there are No omer Compelling indications] A > pcet / ARB c > cee Db > prurettcs [ Thiazides] 4 GOAL > 140/90 in all patients >< 150/90 in >60yYrs patients Tout DM Or CKO > Bor SBP & DBP Should be Corrected 5. poc [ INc-8 HARRISON [HTN in Pregnancy => METHYLDOPA =| Oral LABETALOL HTN Emergency in Preqn —> _HYDRALAZINE | Tv LABETALOL HTN > THIAZLDES > THLAZIDES [HTN” Emergency > __NITROPROSSIDE| > NICARDIPLNE: ANTE HTN DRUGS SAFE IN PREGNANCY Better > p# Caserta) Mone > METHYLDOPA core 7 cloNtDINE uring 7 DHPs HYpertensive > HYDRALAZINE > PRegnancy PRAZOSINE Ca #1]Hyperpolarizat” C@ resting phase) + BNot nah kt? RepolarizatC@ depolarised Phase) br e8@ + at Depolortzat” RESTING MEMBRANE POTENTIAL LC - #0 mv] + Relative negative charge inside the membrane dit Natk* ATPase DEPOLAREZATION > dit not entry through Nat channel HNPERPOLARIZATION 7 dit kt entry Through Kt Channel of vesting state JREPOLARTZATION 7 _dit_ktentry through Kt channel at depolasizat” state ACTION POTENTIAL +30 2, NOT CHANNEL BLOCKERS > octe by 4 store (“dt] oF Phase 0 2 kt CHANNEL BLOCKERS on 7 Action Potentiol duration (ArD] > @T INTERVAL + Depolorisat” + repolorasotion > monifecte ag T AT interval On ECG > TORSADES’ DE POINTES [TDP] ~~? 7 QT Interval ars 3 KY CHANNEL OPENERS > 4 Action Potential Curation [ard] NTE ARRHYTHMEC DRUGS VAUGHAN WILLLAMS CLASSIFICATION > Based on predominant methanigm oF action CLASS I > Nat CHANNEL BLOCKERS class I > B e@iockeRS class Tl 7 kt CHANNEL BLOCKERS class TL ~ co™* CHANNEL BLOCKERS: > orners Class 2CLASS 1 > Not CHANNEL BLOCKERS > 4 Slope of phase o * 1 7 block kt channels > Precipitates ‘TDP I, 7 open Kt channels Te nO ef ret on Kt Channels Tg pRUSS QUINLOINE PROCAINAMIDE Th DRUGS LIQNOCALNE PHENY TOLIN TOCALNLDE Te oRvgS ENCAINLDE FLECAINIDE PROPAFENONE cuass D > B Blockers > used in Tochy arrhymmias CLASS M = * Kt CHANNEL BLOCKERS & > BRetYLum > IpuTripe > DOFETELIDE > AMLODARONE > soragod > SoTALOL has both class mM Cmajor] & class a Actions BMIODARONE % tongest acting LEy, * 7 BwKks] anti arrhymmic drug > mon 1, Nat channel Blocker a. B blocker 3. Kt channel Blocker [main atkion] 4. cot channel Blocker 7% Indicated in all arrhythmias except TDP+ AbverRse EFFECTS The > hyper or bypo Thyroidism Periphery oF 7 Peripheral newopaihy My + myocardial deprecsion lung & 7 Lung fibrosis Cornea is > cornea! deposits Photosensitive > Photosensitivity class > L- Cart cHANNEL BLOCKERS VERAPAMLL DLLTIAZEM DHPs Lnot used J > used in Tachyarrhytamias Should not combine & P blocker! Risk oF Severe Cardiac depression] CLASS VW > OTHERS DIGOXIN > vused in Atrial Fibrfllakion ATROPIN > poc Fer bradycardia & Av Block ADENOSINE 7 Shortest Cty, > poe For PSVTANTI - OYSLLPIDEMICS STATLNS MOA 1 Lnhibit HM@—- COA Reductase a. compensatory T oF LDL -®@ 3. Cholestero! ig taken from blood A. L Serum cholesterol RH Ow. Ore Includes ATORVA STATIN Non ANTL DYSLLPLDEMICS ROCUVA STATIN [ Longest acting] ENDS 7 STATIN PRAVASTATIN CILASTATIN SimvaA sTATIN PENTOSTATTN: FLUVASTATIN SOMATOSTATIN CERIVASTATIN PLTAVASTATIN IMPORTANT POLNTS a. Statins have moximum LOL - cholesterol lowering Potential 2. Given @ Lote evening | night7% Atorvastokin | Rosuvastakin are long atking » Con be given of anytine oF the day 3. ADVERSE EFFECTS Myopamy = Risk fuer Td t FIBRATES Hepototoxicity 4 TOM 5. PLELOTROPLC EFFECTS [Beneficial J PL > plaque stobilizer® e 4 Endothelial dysfunction L FL Inelammation ° F L oOxidakive strecs TR ?% 4 Thrombosis Opic. INTESTINAL CHOLESTEROL ABSORPTION INHEBITOR [ ELETIMIBE] > cmmely combined t statins FIBRATES > Includes cLoFT@RATE FENO FIBRATE BEZAFTBRATE GEM FIBROZIL > ack by PPAR j Stimvlation 4 pie. C 4 4 Triglyceridec ipo protein Lipase] > Fibrakes have mox. T@ lowering potential BILE ACID BINDING AGENTS (BABA) > includes CHOLE STYRAMINE coLestrPoL CHOLESEVALAM > mon ENTERD HEPATIC CYCLE =~ Bile Acid carry Substance From Gut & lenses in blood & reabsorbed BABA interupts enterDhepakic cycle & BA excreted Liver Synmesizes BA Gem Cholesierol —> 1 Cholesterol7% oc in children & pregnanw [sare drugs] 7 Cholestyramine € colestipol not easily polatable (Cholesevalamn can be tare orally ) NrACctN C VITAMIN Bz) + has max. HDL - Choleciere| increasing property only drug, trot can 4 Lipoprotein Ca) Leost expensive Not cormmonty used dit Pruritis | Flushing can cause Hyper usicermia , Heparotoxicity NEW DRUGS MOND CLONAL Ab against PCSK -F > PCcSK-3 helps in breakdown of LoL-® 7 {ncludes ALTROCUMAB Evolo cumaBANTI - OYSLLPIDEMICS STATLNS MOA 1 Lnhibit HM@—- COA Reductase a. compensatory T oF LDL -®@ 3. Cholestero! ig taken from blood A. L Serum cholesterol RH Ow. Ore Includes ATORVA STATIN Non ANTL DYSLLPLDEMICS ROCUVA STATIN [ Longest acting] ENDS 7 STATIN PRAVASTATIN CILASTATIN SimvaA sTATIN PENTOSTATTN: FLUVASTATIN SOMATOSTATIN CERIVASTATIN PLTAVASTATIN IMPORTANT POLNTS a. Statins have moximum LOL - cholesterol lowering Potential 2. Given @ Lote evening | night7% Atorvastokin | Rosuvastakin are long atking » Con be given of anytine oF the day 3. ADVERSE EFFECTS Myopamy = Risk fuer Td t FIBRATES Hepototoxicity 4 TOM 5. PLELOTROPLC EFFECTS [Beneficial J PL > plaque stobilizer® e 4 Endothelial dysfunction L FL Inelammation ° F L oOxidakive strecs TR ?% 4 Thrombosis Opic. INTESTINAL CHOLESTEROL ABSORPTION INHEBITOR [ ELETIMIBE] > cmmely combined t statins FIBRATES > Includes cLoFT@RATE FENO FIBRATE BEZAFTBRATE GEM FIBROZIL > ack by PPAR j Stimvlation 4 pie. C 4 4 Triglyceridec ipo protein Lipase] > Fibrakes have mox. T@ lowering potential BILE ACID BINDING AGENTS (BABA) > includes CHOLE STYRAMINE coLestrPoL CHOLESEVALAM > mon ENTERD HEPATIC CYCLE =~ Bile Acid carry Substance From Gut & lenses in blood & reabsorbed BABA interupts enterDhepakic cycle & BA excreted Liver Synmesizes BA Gem Cholesierol —> 1 Cholesterol7% oc in children & pregnanw [sare drugs] 7 Cholestyramine € colestipol not easily polatable (Cholesevalamn can be tare orally ) NrACctN C VITAMIN Bz) + has max. HDL - Choleciere| increasing property only drug, trot can 4 Lipoprotein Ca) Leost expensive Not cormmonty used dit Pruritis | Flushing can cause Hyper usicermia , Heparotoxicity NEW DRUGS MOND CLONAL Ab against PCSK -F > PCcSK-3 helps in breakdown of LoL-® 7 {ncludes ALTROCUMAB Evolo cumaBcee C co*t CHANNEL BLOCKER J Ty VASODTLATOR TESTING > IF positive, Doc + ccB > TP negative, boc > ENDOTHELIN ANTAGONIST BOSENTAN AMBRENTAN MACE ENTAN PDEL [ PHOSPHODIESTERASE INHIBITORS J > STLDENRErL P@ly TLOPROST PGE, TREPROSTINOL > most effective drugs for Pulmonary HTN 7 corre be qiven oralig SELEXTPAG seLe > Selective > Prostacyclin ogonist x} > non Ingeckoble [oral] can be given orally = BSES AQ > Agonist RIOCL GUAT > scirmvlohi Guonylate cyclase = = % camMP ~% vasodilationPHENO > caused by Drugs L dilali small vessels only C ? 7 die & blood supply to ischemic aren ix token towards dilated small vessel > CORONARY STEAL PHENOMENON X\ S > Shown by 7 H 7 HYDRALA ZINE I > LSOFLURLNE D > orpYRIDAMoLE & 7 ENFLORING* shock > 4 Tissue perfusion > corp EXTREMITIES WARM EXIREMITLES cardingenic shock Vasodi latory | digtribukive shock Hypovolumnic Shock > prsrRtBUrrvE SHOCK 21 Septic shock a. Anophytackic chock 3. Newrogenic shock 4. Hypoadrenal Shock TREATMENT tL cam 2. PLUTO REPLACEMENT > evP Should be mointained blo 8-12 mm OF Hg 7 Ns or RL preferred 7 blood given iF required 3. YASOPRESSORS + Septic Shock 2 NB Coocd 2. PHENYL EPHRENE C in case oF 4 risk OF arrhythmias) 3. NB + VASOPRESSIN oso osed > cordiogenic shook = ~=poc + NA > DR 7 Anophylactic Shock + poe + im ADRENALINE 7 GC ADRENALINE 1000 + = 14% 1locom! L img [mi] > SmI oF 12 1000 Concentrat F 1410,000 iv Adrenaline given in mor responsive coses A. SPECIFIC TREATMENT 1) Septic Shock > Broad Spectrum Antibiotics a _Hypoadrenal shoe > _Stervidsprurerics 7 cause loss of Nat & 40 in urine PRVARETIC * cause loss OF Ho only sual CLASSIFICATION based On Site oF ACKION =~ 2. OSMOTIC OIURETICS 7 Includes = MANNITOL > PRoperrtes > Shovid be Freely Filteable + Shovid not be reabsorbed 7 ghovid net react chemically + shovid exert osmetic eFeck > oses CEREBRAL EDEMA 7 beneficial effect oF mannitol in broin + Osmotic effec 7 cit in ActIVE CEREBRAL HAEMORRHAGE 7 oral mannitol causes Osmotic diarrhoea 2. CARGONEC ANHYDRASE INHEBLTORS > Mets on Proximal tubvie went + Inhibits carbonic anhydrase + > causes loss oF Nat HeOS in uFine we - x ut + Hoop tot +H > brorests 1 ca + Heo > ORINARY ALKALDSTS: 4, METABOLIC ACLDOSIS 1,603, Loa co, + #, F hove Self limiting ackion a AP > tndudes ACETA 2ZOLAMLDE BRIN ZOLAMEDE 1 given as eye drops DoRZOLAMEDE 7 AceTAZOLAMEDE > con be given orally | Ingectoble Form * Indications 7 mountoin sickness Looe] 7 glaucoma 7 RE > metobolic Acidosis hypokaleraia Emax. hypokalemia among diuretics] > Poresthesia +3 Loop oruRETICS Loop pluretics| > asks on ascending mb oF loop of Henle wack > Inhibtes Natkt aci” syrmporter =. > includes FuRDSEMIDE ToRSEmLDE BUMETANTDE, ASCENDING LEM® oF LH High ceiling diuretics CHigh oFficacy Divretics } > ap-a57 oF Nat is reabsorbed from ascending Limb of LH urATt0eS 4 THURZLOES > gets on distal tubule not 7 fnhibits Nat ci” symporter a > includes METHTAZEDE POLY THERZEDE weasrany reece CHLORTHTAZIDE INOAPAMIDE Thiaaide like xIPAMIDE Diuretics + Nat * Glucose 4 Kt ® uric Acid + Mgt + Lipids 4 Ht Loop looses co** > 4 ort * cot used in Hypercalcemia used in Osteopornsis © pivretic preferred in Recurrent Rena} stones % eer b. (4 ea™) f tntces oli 8 Loop pivrebics ee a’ Even though Thiazides 7 $.ca™, less cat reaches Kidney Z toop diuretics, more co** reothes Kidney uses 1. Edena a. HTN 3. Diabetes insipidus —> Thianides indicatedDIABETES TNGIPIDUS PDH retains only water + TYPES ETLOLOGY TREATMENT CENTRAL BT Y POF DESMOPRESSIN Coot] NEPHROGENIC DI |Renal cause THIRztDeS > THipatpes + mon in bE > ow + 4 plasma osmolarity 5. K+ GPARING DTURETECS * > * orine [~ 100 -aoot J compensazory mechanisms 3, POH a Thirt centre stimulation > Thianides couse excret® of concentrated urine 4 osmolarity 4 4 Thirst L 4 urine Formotion > acts OF collecting duck moore, nat @ 2. RuDoSsTERDNE © H — a. epithelial Nat channel Hf pe xt SPLRONOLACTONE AMILORIDE E EPLERONONE TRIAMTERENE D> wt COUECTING DUCT LUMEN > These drugs couse 4 Nate Ho + divresis Kt 7 Hyperkalemia wont Metabolic Acidosis > Pp > Potassium sparing D1URETECS A 7 pmttorcDe S 7 SPIRONOLACIONE > cause qynaecomastia T > TRIAMTERENE £ > EAERONONE do not come gqyunaecomastia ALL DUDRETICS WORK FROM LUMILNAL SIDE ExcePT ALDOSTERONE ANTAGONISTS| ALDOSTERDNE ANTAGONISTS WORK FROM BASOLATERAL SIDEcougH BRY COUGH [ PRopucttvE cough by ANTLTUSSIVES Ry by MUCOLYTICS / EXPECTORANTS CODEINE BROMHEXTNE PHOLCODETNE. PMBROXOL DEXTROMETHORPHAN GUANAPHESIN NoSCAPINE KL BRONCHIAL ASTHMA 2, BRONCHODILATORS oN a a, SYMPATHOMIMETICS — Cs E T Ba AGONISTS, saiauramo. short acting cma qiven by | TenguTeuine = used im auute atiacks inhalation | sAlmereRoL | Long acting FORMETERDL } used For prophylaxts + Spimererol > Sia acting > only used For Prophylaxis FORMETEROL * Fast acting 7 also be used for Acute Atos [Doc] > SIE of Bp, AaoNTSTS T > Tachycordia Cme) T > Tremors 1 > Tolerance b. PARASYMMPATHOLYTECS Mg BlocreRs TTPRATROPLUM Troreoptum > given by Inbolationol route > oc for acute attack in pakients on p blocter therapy ¢. PpET C PHOSPHODEESTERASE INHIBITORS] PDE > camp 9 ——————— _ degrada” 7 finclodes THEOPHYLLINE — not effective by inhalational route2. PHOSPHOLIPLDS srerorns @ —[- Phospholipase Ay PRACHEDONEC ACLD cox | ___tox @ FELEUTON PROSTAGLANOINES LELCOTRIENS L Lr REDESTORS zAFTRIDKAST L @ MonteLucast IBRONCHO CONSTRICTION STEROLDS > Bec For prophylaxic 7 alto used in acu amack along & bronchodilators 3. MAST CELL STRBLLIZERS 7 fnmelude SODIUM CHROMOGLYCATE NEDOCROMIL > only used for prophylaxis 4. OMALT2ZUMAB ? menocional antibody against Ig& 7 only used for prophylaxis > given subcubsneousiyPEPTIC ULCER DISEASE 7 dit imbalance between Aggressive & protective fockors Aggressive factors > HC) 4 H- pylori Hoos H pylori Proteckive Factors > mucus & Hos” TREATMENT 2, 4 ACID Hel 7 produced by Poriebal cell oF Stomach > proton Pump CHtKt PUMP] 7% helps in SecrekM oF Acid 7 stimuked by Bch Cm Hictamine [H2J Gastrin Lock] > jnbibited by PGES+ Acto M) BLOCKERS Hy BLOCKERS: PGE PPL PLRENZEPINE CLMETEDINE MISOPROSTOL, OMEPRAZOL JTELENZE PINE RANITIDINE ESOMEPRAZOL PAMOTIDINE, PANTO PRR2DL LORATEOINE LANSO PRAZOL RABEPRAZDL % most Specific drug for NSALD induced! Peptic olceer + misoprostol PPIs [ PROTON PUMP INHEBi10RS) 7 trreversible tmbibitors + Example DF HIT AND RUN DRUGS 7 exerts systemic effect (not work locally) — normally acid lobite Qiven © atid resistant coating + Enteric coating > pec For PUD of any reason Doc for GERD boc For Zollinger Ellison syndrome. > GIE C chronic ose] -— + wm (osteoporosis) — 4 vit By [Megaloblastic anatmia] — fF infections — Carcinoid syndrome Lot noted in humens] 2 RNTACEDS. > Fastest pain relieves oF PUD PAEN 7% imeludes Pi CoH], cause constipat” mgCoH], cause Diorrhoea 3. UWER PROTECTIVES > sucrALeATe COUDTDAL BISMUTH SUB CITRATE 7% SucralFoG ots by Polymerizat”, requires acidic pr L<4] — Shovld not combined t antacids > CBS can cause BISMUTH POISONING — Bone > esteadystrophy — Brain + Ercephalopalhy4. H.PYLORT DRUGS > PMOXYCTLLIN METRONIDAZOLE. CLARITHROMYCIN > TRIPLE CRUG THERAPY > PPL t+ 2 AMA CF CLARETHROMAYCIN Preferred A pROXNCELLLN Pp o> Per PINT EMETIC DRUGS ANTE CHOLINERGIC DRUGS HYOSCINE H, Blockers DOXYLAMENE Looe for morning Sictnesc]) BHT, BLOCKERS ONDENCETRON oc for GRANICETRON Drug induced vomiting TROPI CETRON: Radiomeropy induced vomiting PROLONOCETRON Lmost potent] Post Op. induced vomiting, . NEUROKININ ANTAGONISTS [SUBSTANCE P ANTAGONISTS] APREPITANT boc For NEUPITANT Delayed vomiting by CISPLATIN ROLF PLTANT Dg ANTAGONISTS METOCLOPRAMLOE DOMMPERLDONE cross 88B Do not ass BBB can cause dystonia DO Mot cause dystonia, Doc for Levedopa induced vomiting! SHT3 # NO omer action 5HTy® NTT DIARRHEAL DRUGS a. ORS > centoins Nacl Kel Tri Sodium Citra. > prevent acidoshs Glucose + to aid Nat absorption } Replenishes elechrolytes 2. BNTI MICROBIALS FOR INFECTIONS METRONIDAZOLE for Omeobic infect” } combined usage is CIPROFLOARCIN for bacterial infect irrotional3. NON INFECTIVE DIARRHEA > LOPERRMIDE } 4 Intestinal motility DIPHENOXYLATE 4 SECRETORY OLARRHER, 7 ocTREDTIOE 7% Somakostatin analogue 5 RACECADROTRIL > ENKEPHALINS ‘Enxiphalinase Degradat® endogenous opioid > Enkepholinase inhibitor INFLAMMATORY BOWEL DISEASE ULCERATLVE COLITIS 1. 5S ASA DERIVATIVES > Doc 1. SULFASALAZINE > SASH - SULFRPYRIDINE 2. OLSALAZINE > B5ASA - 5ASA 3. MESALAMINE a. STEROIDS > [F nok responding t 5 ASA clerivakives CROHN'S OISEASE 1 STERDLDS > voc. a2 TNF & BLOCKERS > IF not responding € sterofds ADALTMUMAB CERTOLI ZUMAB ETANERCEPT INFLIXIMAB—E PURGATIVES 7 Laxakive > causes semi Solid Stools Purqabive —* corises wakery stools 7 uses 1. Functional constipation (not for obstructive constipation] > constipakion preferrably Ry by High fibre diek & reqular exercise 2. TO PREVENT STRATNING > Hernia x Piles 7 Aral Fissure. 3. ¥ — RAYS OF KUB 4. RBlong t ANTI HELMINTHIC DRUGS CNICLOsAmIDED2 includes 1. BULK FORMING (Should be given T Plenty of wake] > prerany Frere PsYuLUr METHYL CELLULOSE > at in megacolon 2. OSMOTIC PURGATIVES > SALINE PURGATLVES 7 Mgso, , Mg COD, cit in chronic renal failure ? Lacrutose > POLY ETHYLENE GLYCOL 3. STOOL SOFTNERS > 4 Surfac tension of Fluids in GIT + pocussrTE - Di octyl Sodium sulfosuccinake 4& STIMULANT PURGATIVES > oRGgANTC > BISACODYL No PICOSULPHATE > sie - colonic atony Con longterm usoged > BNTHRAQUINONES > SENNA CASCARA + sie - Melanosis coli > castor or > Stimulant purgakives are cit in Obstuctive Constipakion 5 NEW DRUGS 2, LENACLOTIDE cr channel LUBIPROSTONE Stimulants 2 PLECAN@TIDE 7 CFTR Stimulont 3 OPIOID ANTAGONTSTS CoH] METHYLNALTREAONE ALVIMOPAN NALAXIGOL NALOE MEDLIN:PITUITARY HYPOTHALAMIC SYSTEMS PITUITARY GLAND HORMONES HYPOTHALAMUS CONTROL Groot, Hormone [aH] < Thyroid Stimulating Hormone C1sH] <——— TRH Ethyroid Releasing Hormone] Adreno Corticotropic Hormone (acni] cr C corticotropin Releasing Hornond, Gonadotropins <———— @nkH C@n Releasing Hormone] Prolatkin) «————— Prt C Prolactin In! GHRHL GH Releasing Hormone) GHIH GH Inhibiting Hormone] iting Hormone] GROWTH HORMONE INHEBITING HORMONES [GHIH) / SomATOSTATIN ORGAN RCTION USES @ PLTULTARY > + GH > Pcromegaly @ PANCREAS & cells [Glucagon } > T Blood suger p ceils Cinsulin] > 4° Blocd sugar 6 cells CSomotostatin]| > 4 glucagon > Iletcell tumors + Insulin eart > 4 Seeretions > Geeretory diarrhoea ® BLOOD VESSELS vasoconstriction | -» Oesophageal vorices > Soma to statins S > Secretory diarrohea Oesophageal varices vid ° M 5 Acromegaly Matignoney C tet cell tumors] + Somokostotin > Short atking OuREOTIDE =F Long atking Somakostakin derivative RNY PHYGIOLDGICAL SUBSTANCE ENDING CSN? 15 PEPTIDE > ocrReoTIDE «=> given by SC rou GONADOTROPIN RELEASING HORMONE LC GaRHI They will be degradad when given by Ore! rout POLSATLLE FASHTON t genadotropins 7 Estrogen, T Progesterone ? Testosterone CONTINUOUS FASHTON 4 Gonadotropins + Estrogen, | Progesicrone J TestosteroneINDICATIONS Of GnRH In Pulsatile manner ® typogonadotropic hypogonadiem ® delayed Puberty In continuous Fashion ® cancers > Prostake cancer > Breast concer © Endometriosis @ Precocious puberty GnRH AGONESTS © LevupROLEDE © NAFARELIN ® qosereiin @ BusuRELIN © HTSTARELIN + FLAREUP REACTION > When these drugs given in Continuous manner, Initial 2-3 days there is oggrevation of diseose GnRH ANTAGONESTS CETRO RELIX GANT RELIX ABA RELIX DEGARELEX ®@000 v No Flore up reaction but they do not tse sex hormones + 7 Eimer GnRH Agonists of GnRH antagonists , not effective orally PROLACTIN INHT@ITING HORMONE C pit] Dopamine Cond > DA atk trough D2 Receptors > rugs stimulating og Receptors ack ike PIH > D, RECEPTOR AGONTSTS > BROMOCRIPTINE. 7 CABERGOLINE [ Long acting] > INDICATIONS @ HYPER PROLACTINEMLA > cABERGOLINE > DOC, Can be given only© Pprkinsontsm © acromegaty 7 CABERGOLINE is the preferred drug > 4 aH 7 can be given only PEGVISOMANT [GH RECEPTOR ANTAGONIST) PEGVISOMANT > Somakotropin Antagonist > PEG VE SOMANT > causes Visual Field defect PEG VISOMANT > _PolyEtFyleneclycol > tong ocking ® wre 2 om F% BROMOCRIPTINE > J Insulin resistance THYROID > secrets 13 T} CALETTONTN 3 Tq > short acting > longer acting FP __more active > tess ackive > WOTHYRONINE. > L-THYROXINE — only indicat? > — poe For hypormyroictismm Myxedema coma Cemergenty} Doc For myxedema coma PHYSEOLOGY OF THYROLD HORMONE PRODUCTLON@ iodide (171 enters tnro tyrvid Follicle by Nat t” Symporter @ from follicles Iodidw enters into colloid © In couoro 1 oxidation T orgonificat® t tyrasine MIT T_ coupling > all te 3 reactions catolysed by Thyroid Peroxidase 7 ta,Tq Stored in colloid @ TSH stimuletes myroid © 13,1, released into circulation © Hormone reaches peripheral tissues jorgans [ Liver] 7 tm the blood, Ts if active but less in quantity Ta 1B abundont but ot much active ® Peripheral conversion takes place in peripheral ticsves Jorgans [ Liver] ——___ +. Te Mebobolized 3 HYPERTHYROIDISM — DRUGS @ Nts INHIBITORS @ THYROID PEROKEDASE INHEBITORS @ SecRETION INHIBITORS @ PERIPHERAL CONVERSION INHIBITORS © THYROID DESTROYING DADGS NIS INHIBITORS @ PERCHLORATE @ PERTECHTE NATE @ THrocvanaTe > not used clinically (toxic) 7 cabbage i@ © rich source of Thiocyonate + GorTROGENTHYROID PEROXLDASE INHIBITORS @ carermazole Cinactive] @ PropyeTHrooRActL C Pro] | @_mernrmazoce active) | > more potent > Less potent [> _ more plasma tty, > tess plasma ti, “crosses planta easily less crossing of Placenta > doc im 46t trimester pregnanyy) [7 be action on peripheral convers® > decreages Peripheral conversion 7 Slow acting drugs + en @ person, stored 13,1 Surfice for 1-2 UkS 9n byperthyroidism , they suffice for 3-4 Wks Dose increant OF mete drugs Should be done after A WKS. SECRETION INHIBITORS @ nat ® kt © vugoi's tootNe > Fastest atking ontiMyroid drugs @eRIPHERRL CONVERSION INHIBITORS ® PROPRANOLOL ® peru © prepnisotone THYROID DESTROYING DRUGS [ L'3!] *- e used becouse @ Ndi~ symporter ig gpecific For Iodine intoke > restricte 1181 to thyroid gland @ 113! stored in colloid, emission of radioactive rays confined @® 1 emits p rays , have lece penetrating power > at im pregnonuy > con be given orally 7 Radioackive drugs couse Irreversible hy poryroidism , requires life long thyroid hormone theorapy 7 CIT in < 35 yrs aged patients PII Ome ontimyToid drugs couse Reversible hypothyroidism , discontinuck” oF drug suffice > 18 cy. > 8 days[.””~”~”—~—CRR I Secneres RercON 0se5 a ceils | Glucagon % Blood Sugar hypoglycemia B cells Insolin 4 Blood suger Amylin & celts Somabostoting gLUcAgON oses 2. HYPOGLYCEMIA > Mon > acke by GLYCOGENOLYSIS — Hot oseFul in hypoglycemia caused by + Starvation + Alcohol induced hypoglycemia, 2. PBLWCKER PortsonttNg Looc] INSULIN INDICATIONS & Tyeet om [topm] > AM pakients require insulin a. TYPEAa Dm CNIDDm] * oncontrolied patients 3. GESTATEONAL Dm > poe 4. DIABETIC KETOAcCOOSES 7 doc 5. TIDE STRESS 6 ACUTE HYPERKALEMEA * non dioberic use. PREPARATIONS RAPLD ACTING > LESPRO ASPART @LULESENE SHORT ACTING REGULAR Sem - Lente INTERMEDIATE ACTENG => NPH LENTE LONG ACTING 7 _UUTRA - LENTE ULTRA LONG ACTING FGLARGINE * RIL Insulin preparations ore Given by > Sub wkaneovs roote Requier Insulin also be giver by > Ty route 7 pil insulin preparations ore ak > Neotral PH Glargine is of acidic PH C<4I CNo insulin should be mixed % it]sie HYPOqLYCEMTA ome & most dangerous > Advice to patients for prevent? a, donot stip meals a, Keep Glucose [form] ORAL ANTI OIAGETICS Acts by t Insulin acts by Other mechanisms > sie > bypogiycemia > no hypoglycemia > >307, Functional B cellx > ne such requirement Should present DRUgs Acts BY + INSULIN MEG LLETENEDES NATE GLINEDE REPA GLINIDE SULFONYLUREAS 38 GENERATION CHLORPROPAMI DE TOLBUTAMIDE 204 GENERATION Guprzt0e @UICLAZLDE GLIBENCLAMEDE y Omer than Insulins drogs ending t “Ine” can couse —* hypoglycemia SULPONYLUREAS 7 couse hypoglycemia > conse weight gain +> CHLOPROPAMLOE Sie — Joundice — Disvifiram like reaction — POH Cretains H0) 7 Dilukional hyponatremia also Indicated for Diobetes insipidus MEGLITINIDES + ghort acking L~ thr] + indicated in Post prondial hyperglycemiaDRUGS ACIS BY OTHER MECHANISMS 1. METFORMIN: PHENFORMEN > se 2. Megaloblastic Anoumia > more ald Metformin aL Latkic acidosis > more afi Phenformin not used now] > PHENFORMIN > hag more ajw totkic acidosis (not used now] > METFORMIN 7% hag more ajw Megaloblactic onoamia > Ie con also couse pattic acidosis — contraindicated in Liver diseases Renal diseases Lung dixeases 7 voc for TYPE a om — no risk oF hypoglycemia — max. reduction Hb A\. — can couse weight loss most M Merformin preferred in obese patients ° s Sulphonyloreas preferred in T Thin pokients > Metformin also indicatec!| for PcoD L reverses Insulin Resistonce) 2, TROGLITAZONE ROSE @LtTAZONE PIOGLITAZONE 7 acks by stimulating PPAR-€ > Reversal oF insulin Resistonce > ge a. Hepakotoxic 7 max. hepatotoxicity + Troglitazone Cwitidrowh] 7% Rosiglitazone & Pioglitazone requires LET monitoring NaTG Waker Retention * avoid in CHF & HIN + risk OF m2 by Rosiglitazone t risk OF urinary bladdy corcinoma by PioglitazoneA & GWCOSIDASE INHEBETORS pets by inhibiting the absorpt” of carbohydrates > 2 MagurroL Vogitaose 7 Blakvlence > me side effect > cit in Inflammoetor bowel dieases laxative colitis chron's dixeate. > hypoglycemic prophylaxis in d@L 7 only by Glucose NEw DRUGS 2, INCRETINS 7 releases Insulins GLUCAGON LIke PEPTIOE 1 [Emoct important endogenous Incretin] | pep 4 Coipeptidy! peptidase 4] Degradation a. GLP AGONISTS > Exenarépe>d LIRA@LUTEDE) F alco couse weight loss (Liraglutide indicaked for Obesity] not efFective orally » given Subcotaneously 7 cause hypoglycemia + b DPR ENHTBLTORS > SITAQLIPTIN VELDA GLIPTEN SAKA GLIPTEN ALOGLIPTEN LINAGLIPTIN eFreckive orally only oPPr SaFe in renal failure > Linagliptine me sie 7 Nasopharyngitis do not conse hypoglycemia 4edveg 7 SIE oF INCRETINS —* PancreatitisQ BMYLIN ANALDGE > PRAMLIN TLOE —S=r 7 given by Gubaukaneous rou > causes hypoglycemia > ONLY DRUG INDICATED IN BOTH TYPE 1 & TYPEQ DM 3 SGIT-2 INHIBITORS , > canaG@DEODEN) V Lorine] DAPA GLEFLOZEIN EMPA GLIFLOZIN > se > Infeckions OTL — Genital track infeckions 4 BROMOCRIPINE > Reverses Insulin Resistance 7 Exatk mechanism ot Knownmesviin Teme > Secrets > Secretes Aa GLuco corticoids NA Minercus corticoids DA ALDOSTERONE > Major endoqenovs = Mineralocerticofd ACTIONS a. TNOt, THD a L Kt, +H HYDROCORTISONE > Major endogenous Glucocorticoid ACTIONS 1, CATABOLIC aAcrION Careohydrakes ( CHO] breakdown 0 glucose * avoided in Om Proteins breoxdown 7 myopatles can occur fats breakdown [Ermainiy fromm periphery] = CUSHING SYNDROME co metabolic 7 cassses OStenporosis2. ANTE - INFLAMMATORY ACTION Fo mainiy by inhibition oF Chemotaxis + vsed in inflammatory conditions Citis*] + cause delayed voound healing 3. IMMUNO SUPPRESSANT ACTION 7 Indicated in Troncplantat? g hukoimmynity 7 bur predispose to infections 4. NTE CANCER ACTION > indicated in FHL [Hodgkin Lyrmphornal F NHL LNon Hedgkin tyrnphomal > UW [bymphoeytic levkernial > cit fh kapesi sarcoma GweoeokrecorDs C Anti Inflammatory} MENERALO CORTECOEDS CTNO*, TH0I SHORT ACTENG ALDOSTERONE CORTESONE FLUDROCORTISONE HYORD CORTESONE Boca ILNTERMEDIATE ACTING PREDNISONE PREDNISOLONE TRIAMCINOLONE DEXAMETHACONE BETA ME THASONE PARAMETHASONE max. glucocorticoid activity > _ DEXAMETHASONE Max. glucocorticoid potaney > BETA METHASONE jucocorticoid % Max. mineralpcorticeld ostivity + HYDRO CORTESONE max. mineroto corticoid activity 7 ALDOSTERONE minerolocorticoid Tt max glucocorticoid ackivity —? _ FLUDROCORTISONE: Glucocorticoid T aero mineralocorticoid ackivity TRIAMCINOLE °o + aero DEXAMETHASONE M > minerlocorticoid activity BETA ME THASONE PARAMETHASONE mineralocorticoid % uero glucocorticoid ackivity > DOcA © > aero © F cortisone like activityOSES OF CORTICOSTERDEDS PNTENATAL USES REPLACEMENT OSES [_ orHer uses Dexa | Beamemasone |Reste Adrenal insufFicienty / |INFLArMATIONS. For Fetal lung maturity |peidisonian crisis Loy iv} | ®UTO tryMmUNE DISEASES TRANSPLANTATIONS Crenic Adrenal Insufficienty/ | BNTE CANCER THEARAPY Addison's digeage Cby Orel]) ASTHMA HYPOTHALAMO ~ PITUITARY — ADRENAL Axts [HPA Axis] HYPOTHALAMUS = —> cRH 4 PITULTRRY id ACTH, 1 ©] Entities ADRENAL, — + |Glvecorticoids Mineralo corticoids HPA AXIS SUPPRESSTON 7 occurs When corticosteroids are given continuously for 7 aus. > PREVENTIVE MEASORES 1. STOP UNNECESSARY USE OF Steroids a. If indicated, prescribe them for < auks 3 fe Indicated for long perfods » prescribe them on ALTERNATE DAY — Long acking stervids are ovoidid indicated daily & longer periods % DON'T STOP ABRUPTLY tapering should be cone Lg OTHER USES | NON - REPLACEMENT USES 2. INFLAM mATIONS 2. AUTO LMMMONE DISEASES & TRANSPLANTATLONS: 3. ANTE CANCER THEARAPY 7 HL [Hodgkin Lymphoma > NHL [Non Hedgkin tyrmphomal F tL [bymphoaytic levkemia] > Mm [Multiple myeloma] 4 ASTHMAADVERSE EFFECTS £& CONTRA INDICATIONS OF GLUCOCORTICOLDS Glaucoma Copen angle glaucoma. Cy long term eid usage) Limb muscle abrophy vleer Cpeptic ulcer) coborock [mostly posterior Subcopsular] ( Long term oro! usage] Osteoporosis Cushing syndrome osteoneuvsis CAvasawar necrosis] Reno! failure TB Clleocaecs!J + cy Lnfeckions CHE t clr oedema Impair healing DM > ot Suppre Sion OF HPA axis Cmost dangerous complication] $ELtaedde ta thavaeda q L uv é ° c ° R I e ° L D &VITAMIN D CALCLTONIN PTH [Parathyroid Hormone J VITAMIN D, T Serum coldum by + absorption } % Bone ca®t > used in osteoporosis + Excretion PTH, T Serum calcium by Resorption of Bone ~~ 4 Bone to > causes osteoporosis calcitonin, + Serum calcium by moving co>* to bone > T Bone Co** * Used in osteoporosis OSTEOPOROSIS DRUGS USED a. VITAMIN BD 2. CALCLTONIN 3. THIAZIDES 4. BISPHOSPHONATES > prenGRgnnre) RISE DRONATE OLENDRONATEBrSPHOSPHONATES inhibit osteoclasts Leone eaters] boc For Osteoporosis Lfor any reason J Highly toxic to oesophagus Preventive measures 1. Given on empty stomach a. Given % full glacs OF waker 3. Shovld not Lie down for a min. oF Zomin after taking Alendronali. Risendronal. Zolendronai given IV once yearly t given orally POST MENOPAUSAL OsTEOPOROSTS. ESTROGEN —* responsible for Post Menopausal osteoporosis + Actions BONE Formation BLOOD HDL BREAST carcinoma ENDOMETRIUM carcinoma, LIVER clotting fators > Thromb Embolism > Not preferred for R OF Pm OSteoporosic + Earlier HRT [Estrogen + Progesteron ] given , but not now SERM [ SELECTIVE ESTROGEN RECEPTOR moDULATORS J a, RALOKIFENE > used in Pry osteoporosis 7 additional Benefits > > BOL > + Breast & Endometrial carcinoma visk > Sle = + Thromboembolism 2, TAMOXLFENE DOLOX1FENE TOREMIFENE 7 mese drugs have beneficial efrects on Bone Blood Breast [strong errect] > have decrementol effects on Endometriom = >t Endometrial cA Liver > % Thrombo embolism > beneficiol in Breast cordnoma3 clomiPHENE Hypothalamus > [S0RH Pituitary — [Fenian | Lanier ovary —> | PROGESTERON /EStROGEN 7 estrogen receptor antagonist of pituitory 7% Imdicakion > Anovulatory Infertility NEW DRUGS | TeRL@ARADIDE > @® PTH contain 1-84 amino atid, & activates osteoclasts > Teriparakide contain PTH t I-34 AM & ackivolu Osteoblasts a, STRONTIUM RANELATE. > peat Aerturty * Stimulates osteoblastic activity > hibits osteoclastic activity caeeel RANK 3 venfosumAB) hd fe > monoclonal Ab ogainst RANK C® on asteoclast] L RESORPTION =— [© cxmmveus Mick & hostile f sperm MAIN MECHANISM | Inhibition of Ovulation PROGESTERONE ONLY PILLS | MENTPILS I Cx Mucus thick & hostile Disioging oF implantation com@tned ocP CE +P) EMERGENCY / POST COITAL] MORNING AFTER PILLSCOMBINED ORAL CONTRACEPIVE PILLS + estrogen Progesicrone > ETHINYL ESTRADTOL + LevonorGestRol > posage 7 Leobler daily for a days from Ist day oF menstrual cyde 7 no rable: for next 4 dod 7 To t compilok®, a8 Tablets Strip t 48t Al tablets contains drug next F tablets contains Fe 7 4. TF 2 tablet is missed > Toke @ tablets on Next doy a. LF a tablets missed 7 piscard remaining tablets | Start ofresh and prockice omer memod OF contracept® c tt 7 BREAKTHROUGH BLEEDING 7 bleeding @ 2-al day 7 prevented by PHASIC PILLS gradual OF Progesterone from 1t0 aida POP / MotNTPLLS > contains LNG > Inprcartons 2. Thromoenbolism risk A Lackakion C contraceptive oF choice] EMERGENCY CONTRACEPTIVES. a. COC > atoblets ot Stat + atoblerg fier ahve a. Por (ING) > a2 tablet of Stort + 2 tablet after Rhre or 7% atoblets ot Start 3. MEFEPRISTONE > SspRm - Selective Progesterone Receptor Modularor > uses 2. Emergency contraception 2. Induction OF abortion * Above 3 drugs should be Used Zin con be used Tin i209 hrsADVERSE EFFECTS OF OCP [mus | mom SEVERE os + =~ ss 4 =s Nausea oedema Acne C¥S Cthrombo Embol ism) weight gain CNS CDepreccion) Reaurent headache chloasma cholestasis Mastalgia cancers Abnormal bleeding T/ Breast ca Loss of WitKdranoal T cervical cn bleecling NON CONTRACEPTIVE SENEFITS other GAH am z mg t¥tete yb bud S$eeeeneece Ovarian ayst [doc For Prop] Benign Breoct Direose Endometriosis Neoplacia Cendometriat & Ovorian cancers] Eckopic pregnanuy Fibroid Tron dericiency Syndrom Pre menstrual Tension syndrome Skeletal Digeace [ostenporos! sjMIFEPRLSTONE > SPRM — Seletkive Progecterone Receptor Modularor > ActIONS 1 Progesterone R antagonist in endometrium a Glucocorticoid R antagonist Androgen R antagonists Morning after pill Induction of aboxt” Fibsoid Endometriosis > > = > } Progesterone R +ive cancers uh Breast concer Menin gioma } Cushing Syndrome SteroidsANTE NATAL STEROLDS Poked Oo) terme Ovrak” BETAMETHASONE > im amg per auhrs x a Doses > aymg 4dbr DEXAMETHASONE 7 [m 6mq pu 12 hrs X 4 Doses > au mg abbrPROGESTERONES: KA) POTENCY | ANDROGENIC ACTLVITY ast GENERATION | ESTRANES| + + and Generptzon | GONANES| ++ +t Srd_ GENERATION ttt + Al _ GENERATION ttt Bnti Androgenic ast GENERATION NOR ~ ETHINDRONE NORGESTREL NOR ~ ETHENODREL LEVONORGESTREL [LNG] 3rd_ GENERATION AIS _GENERATZON DESOgESTREL NOMEGESTREL NOR GesttMATE DROSPLRENONE GESTIDONE DRDSPLRENONE (7 alo has anti mineralo corticoid atktvityawa Linbibitory newotransmiter oF Brain] BARBITURATES BENZODIAZEPINES| casti GABA mimekics GABA Facilitatory mae K channel + duration 1 Frequency Re Steep Flat inducers | +++ xx secmcemuaiees Addiction tt+t + L Revaeea| NS ~ Fw mazelnzt Antidote xX FLUMAZENTL [aneidoted BENZODIAZEPINES 7 includes DrnZerAm > oxmrepam Lastive metobolite] FLURAZEPAM NTTRAZEPAM FLUNITRAZEPAM F B20 are LONG AGING dit active metabolites > cause Hangover 7 cit in elderly me ¢j1 tm tiver Fodlure > 82D Not FORMING ACTIVE METABOLITES S > SHORT Acr=ng 82D T 7% TEMAZEPAM Oo FF OxAZEPAM Lo LORAZEPAM — 7 EsTAzoLAm maintained cop Qualtty SLEEP > Sleep architechture L phases OFREM & Non - REM] Borbitwals & BZD + biStort the hormal Sleep architecture Ceuality] 7 also d tatency oF sleep onset 7 t Quantity oF Sleep Z oRVES = DEC For Insomnia. ZOLPLBE m 4 Lokency of sleep onsek ZOPICLONE nok eFfeck Quality ZABLE PLON not eFfect quantity Non addictive> Normally, Golance biw Doparninergic CDAD & cholinergic CAch) neurons > =m Parkinsonisms , this bolance is Lost [Relative cholinergic excess DOPAMINERGIC DRUGS 1 Levopora rrnontwe, > LeVODOPA alone > is Léss porent > as peripheral dopamine decarboxylase errective than central ry ono .| oh SAS p began > DA causes PERIPHERAL SDE EFFECTS > pd, + > Hypotension Bot > ArrhytRmias do, + 7 Hypertension em + > vomiting > CARBIDOPR Peripheral Dopamine BENSERAZIDE Decarboxylase Inhibitors +t EFeicacy oF Levoclopa 7 4 Peripheral SIG OF DA > psycHosis [dit excessive DA in broin] > all Partinsonicm drugs can couse Psychosic a antipsychotic drugs can cause Parkinsonicm + Centrol SIE contr be prevented by carbidopa > Psychosic > dyskinesia 2 AMANTADINE > acts by Teleasing 08 From vesicle * also used as antiviral drug for Influenza virus3 comt INHIBITORS & MAO INHEBrTORS MAO INHEBITORS. MAO A Mao 8 Present at all ploces Present mainly in Brain Mekobolises all substances Mekabolises OP SELECTLVE MAO B INHEBLTORS 7 preterred in parkinsonism + Includes SELEGILINE RASA GILINE ComT INHIBITORS > Includes ENTACAPONE > preferred GOcarone > Oxic toDiver 4. DOPAMINE AGONIST ERGOT NON ERGOT BROMOCATPTENE PRAMIPEXOLE PERGOLEDE, ROPINTROLE saFer tong Acting ve > G@ongrene * Fibrosis x ANTE CHOLINERGIC DRUGS (Central Ach 4J > pec for Drug Induced Parkinsonism > includes BENZHEXOL CTRIHEXIPHENYDIL] BENZ TROPINE BIPERLDINE PROCYCLIDINE DOC FOR, PARKINSONTISM > PRAMEPEXOLE | ROPLNIROLE MOST EFFECTIVE DRUG FOR PARKENSONTSM > LEVODOPA + CARBIDOPA BOC FOR DRUG INDUCED PARKINSONESM > BENZHEXOL,qneat QLUTAMATE 4 © <> s gata com ¥ qaen Tea pegradat’ not &—— k7 CHANNEL OPENERS DRUGS t GABA 1, PREGABALIN GABAPENTIN > prugs act by releasing GABA > doc For Newopamhic pain dit. Diabetic neuropathy Post Heretic neuralgia > Recent upda > MoA + mainly by ca2* channel Inhibition a VE@ABATRIN vtsval oa contrace” C sje] 4 INfantile spasm Cuse] v Denn TRIN ¥ GABA TRansaminase INhibitor CMOAD Doc for Infantile spasrn 7 ACTH 3 TE@GABINE + Transport Inhibitor [GATa] [Reuptake Inhibitor] oF GABA 4 BARBITURATES > PHENOBARBLTONE, 820 > piazerpam LorAZePAm, CLONAZEPAM, CLOBAZAM Phenoborbitone can Cause Hyperkinesia in children oc for febrile Seizures > Diazepam Doc for status epilepticus —* Lorazepam used for obgerce Sef2ures + clonazepam used in Lennox Gastowr Syndrome > clobazoma 4 qwurAMATE Aertvery NMOR # AMPA FELBAMATE PERAMPANEL Bene Merrow Soppression 3. T-co™ CHANNEL BLOCKERS ETHOSUXLMLDE, > used only for Absence Selaure 4 Nat CHANNEL BLOCKERS PHENYTOIN CIt in absence & myoclonic seizures CARBAMAZEPINE Useful in GTCS & focal Seizures OXCARBAIMAZE PINE rormxamar | ete saad stn ‘ZONISAMIDE EXpenietee vsed in Focal seizures RUFLNAMLOE VY qorrramare OTHER USES 4 craving oF Alcohol Obesity migraine prophylaxis Bipolar disorder CARBAMAZEPINE > voc For Focal seizures > poe For Trigeminal newalgia > can be osed for Diabses insipidus [ Doc For DL > DESMOPRESSEN] Bipolar Disorder (poc FerBO -* LiTHtumI PHENYTOIN > Follows 2er order Kinetics Emyme inducer Used for Arrhymrnias too used For GCS & focal seizures CIT in Abgerce & Mypclonic Seiures,ROVERSE EFFECTS 4 Hirsutic¢m , Hypertrophy oF gums. Osteomalaca Teratogenedty [Fetal Hydentoin Syndrome] Megoloblastic anaimia | +Foloke] Arrhythmia Lonly in overdose J Lymph node enlargernent ¥ insulin + vitamin Ataxia, Nystagmus 4 vertigo C cerebellar symptoms] Conly at tdose} PAF DRZ40 beet veuvage 5. kt CHANNEL OPENER, RETIGABIN [EZO@ABINI] > used for focal seiapres > does not act on GABA SobrIum VALPROATE Mon Na** channel Blocker co channel Blocker tT Geer 4+ Glutamate eres Absence Selaures Myoclonic Setaures Atonic Selavres Lennox Gastauk syndrome Doc For tvydud > alco used For Bipolar disorder RDVERSE EFFECTS Vomiting Alopecia Uver domage + Pcon LAMOTRIGENE, Mon > Nat channel Blocker 7 ) @ABA 7 4 Glutamak RIE > STEVEN JOHNSON SYNDROME LEVITERACETAM & BRIVACETAM > bind co a protein “svn” Ceynoptic vesicular protein )PSYCHOSIS Cho insight) NEuROSES C Insight present] 2. SCHTZDPHRENTA a, 2. MOOD DLSORDERS a 0. MPNTA 3 b. DEPRESSION a C. MANIC DEPRESSIVE PSYCHOSIS]! 5, BIPOLAR BrsORDER SCHLLDPHRENTA BNTE PSYCHOTIC DRUGS TYPLCAL ANTE PEYCHOTECS Loa #] RTYPLCAL ANTE PsycHortcS CSHT, 1] 7 most drugs possess bom properties ° pw >2 SHT) 7 > miogy SHT, TYPLCAL PNTLPSYCHOTICS 2 STRONG Dy # GENERALISED ANXIETY DISORDER, PHOBLAS oc BuLtMIA POSTTRAUMATIC STRESS DISORDER, +> Typical Antipsychotics > Atypical Antipsychotics > PLOPERCDOL [Highest risk oF EPS] DRDPERTDOL, FLDPHENAZINE 2 WERK Dy H > CHLOR PROM AZINE THIORLDAZENE 3 INTERMEDIATE 0, # > THLOTHIXENE CHLORPROTHIXENE. SUE EFFECTS a, EXTRAPYRAMIDAL SYmproms CEPS] 4, pystonias [earliest] 2 Akathesia (mel 3. Parkinsonism 4. Tardive dyskinesia ( tarestJ ». Malignant neuroleptic Syndrome ae Me alo Strong Da H Cleast risk of eps]TREATMENT BENZHEXoOL > Dystonias Loocd Parkinsonicm [ooc] Pkathisia Malignant neuroleptic syndrome 7 at in Tordive dyskinesia, PROPONOLOL = AKathisia Coot] DANTROLENE = Malignant neuroleptic syndrome [boc] VALBENAZINE > Tardive dyskinesia a. HYPER PROLACTINEMTA F Dy 4 Prolactin aH > t Prolactin > mic ako strong Oy # 3. Bch # + dryness, blurring OF Vision etc A 4 > ep more common & 5 HH > sedation Weak D, # 6. Seizures DISADVANTAGES OF TYPICAL DRUGS 1 SIE R. not efreckive aquinst —lve symptoms TYPICAL ANTE PSYCHOTECS AOVANTAGES 1. lesser sie a. EFfeckive against bolh Positive & negokive Symptoms DRUGS > clozmerne + RISPEREDONE > OLANZAPINE > PALIPERLDONE 7 QUEITAPINE > ILOPERLDONE > RSENAPINE > ZIPRASIDONE > ZOTEPINE > WRASEDONE 7 pRIPrPRAZOLE 9 PIMAVANSERIN SIDE EFFCTS 7 > qlucose, > > Lipids UPODYSTROPHY SYNDROME 7 wefght gain Chighest risk € clozapine & olanzapine J > Insulin ResistanceCLOZAPINE SIE > Pgranviowytosis [dose indepedant] 7 Sevres [dose dependent 1 > myocarditis > sedation Lmel QUETTAPINE SIE > cobarack ZIPRASIDONE > Top Ct qt interval I OSES OF ANTI PsycHoTics ANTI > Anti emetic Psy > Psychosis cHo = chorea C Huntington chorea ; boc + TETRA BENAZENE] TES > tre disorders GILLE DE LA TOURETTE SYNDROME > charecterised by vocnt Tics [ abusive Sounds) FR > Hetwrertpol Conly FDA approved drug] > ctontptne > @UANAFACENE, MOOD OLSORDERS AeUreE MANTA, 7 R oF Raw Episode > SEDATIVES CANti psychotics/B20] + LITHIUM > Prophylaxis > urtHum — Looe] 7 utrHtum L Leveocytes, Increase Tremors [me hypothyroidism Increase urine avoided in Momers [ Lithium in pregnancy + Ebstein anormakj]) } Leucocytasis } Poly uria pebaudsde Zeonrae > Plasma concentration Norms Revte mania > 0.8 — LQ meQIL Prophylaxis => 0.5 — 0.8 meq/L TORIC > > ameqiLBIPOLAR DISORDER. > urHtum > voc For bipolar disorders > CARBAMAZEPINE > VALPROATE > poe For Rapid cyclers F TOPLRAMATE > tamorerqgtne > eNTEPSYcHorics = boc For bipolar disorders in preqnancy PNTE DEPRESSANTS Deficitnay of Monoomines (SHT > NA > DA) cause Depression 7 Typical antidepressants + acts by TSHT Arypical Anti Depressants > acts by ofher mechanisms TYPICAL ANTIDEPRESSANTS 2 MAO-A INHIBITORS > MocLeBEmIDE > aka RIMA GD, R > Reversible © Le TUBS Searadation IF Inhibitor oF ee ™ > mao * 7*- A a REUPTAKE INHIBTTORS INON SELECTIVE [__ Sétective > Inhibit reuptake oF 5HT GNA | > inhibit feuptake oF 5HT > Avoided in cardiac parients > can be used in cardiac patients dicaked for mild to moduroh depression > indicated for Severe depression | > NON SELECTIVE TcA [tricyclic antidepressants] > includes IMLPRAMLNE DESIPRAMINE CLOPAL PRATYLNE AMLTRIPTY LINE NORTRIPTYLINE > sie Pech a8 ce Seizures Prthyrimias Metabolic acidosis ted eueSNRI [SEROTONIN NORADRENALTNE REUPTAKE INHEGTTORS J 7 4 5H & TNA less ge Doc For Severe depression Drugs VENELAFAXLNE DULOXETINE MLLANACLPRAN DES VENELAFAXLNE. LEVO MILANACLPRAN dud SELECTIVE SEROTONIN REUPTAKE INHIBITORS > prugs FUWOXETINE PEROXETINE FLUOKAMMINE SERTRALINE CITALOPRAM, ES- CTTALDPRAM > dee For mild - modera depression depression + voc For all neurotic disorders 7% Sle + delayed Ejaculation 7 used for Pre Mature Ezaculation ATYPICAL ANTL DEPRESSANTS > prvgs BUPROPION 7 Anti- smoring dug PMRINEPTIN } > reuptake TIANERTIN, MERTRZAPINE AMOXAPINE > vc, H also ATOMOXETINE + ULSed in ADHD MIBNSERINE.OPTOLDS > Obtained from Opium [Ccrude extract oF Poppy plonts] > opipres + drugs derived from opium 7 mojor opiait — MoRPHENE 7 OPLotps > Opio& Like substancesMORPHINE > actz on M,yK,S Receptors > Stimuloth oF M,K,& Receptors couse — Analgesia H RECEPTOR FuNCTLONS Ss > Sedation > can couse coma BF Analgesia 7 used in Severe poln © 7 constipation > used in diorthea R > Respiratory depression > avoid in asthma & Copp 0 > ophoria > Addictive drugs mm > Meiosis ADOLC TIVE DRUG PROPERTIES Tolerance > pose has to be Td to ger Same efrect > Tolerance donot develop for constipation Constrick? oF pupil Dependence > Psychological —% cRAVING > Physical 7 WITHDRAWAL symptoms. CLASSIFICATION OPIOLD AGONTETS > stimula all 3 Receptors Cy, K,8] OPLOLD PARTIAL AGONISTS > blocks aM 3 Receptors OPIOLD AGONLST - ANTAGONISTS > agonist at Ni receptors + OPLOLD ANTAGONISTS agonist on one (], antagonist on offer[y] PgoNTSTS > rugs MORPHINE HERDINE 7 eo times More addictive than morphine METHADONE > very long acting , used in deaddick” OF Opioid PETHTOINE. CODEENE | PHOLCODEINE | DEXTROMETHORPHAN | NOSCAPINE LOPERS MIDE | OITPHENOXYLATE TRAMADOL | TAPENTADOL FENTANYL PLFENTANYL SUPENTANYL REMLFENTANYL CODEINE | PHOLCODEINE | DEXTROMETHORPHAN J NOSCAPINE % cough Suppresants / Anti tussives: + indicoted for dry coughmno~a Degrodat’ 997. <3 PETHIDINE a% NOR PETHIDINE Lvery tong acting} > SIE + Seiawres Lon chronic usage] > elt along t mao - Inhibitors LOPERS MIDE | DLPHENOXYLATE. 7 indicated for non - infectious diarrhea > qt im infeurious diarrhea TRAMADOL / TAPENTADOL > mon > MK, B+ } couses analgesia. > % SHT in Spinol cord FENTANYL, ALFENTANYL, SUFENTANYL € REMLFENTANYL highly lipid Soluble drugs used Fer anesthesia Couses Post op. muscle rigidity Cpost op. muscle pain Clb Succiny! choline) SUFENTANYL + most potent opioid REMIFENTANYL =~ Shortest acting opioid Edit metabolism by Pseudo che] teguve 2 PARTIAL AGONISTS F BUPRENORPHINE — hos cEILING EFFECT On respiratory depression 3. AGONTST ANTAGONICT > pruas p> Penta zosin No NALQUPHTNE B > BUTORPHANOL > agonist @ K & antagoniss @ M 7 sié > hallucinations 4. ANTAGONISTS > oRVeS NALOXONE > Short acting 4 given fv NALTREXONE 7 tong acting » given Orally > voc For acul. opioid poisoning + Naloxone > poe for maintainance in Oplofd poisoning + NaltrexoneOPIOLD DEADOTCTION SHORT TERM ADDICTION TONG TERM ADDICTION REPLACE T METHADONE, Stop opioids Cless addictive & Long acting L WITHDRAWAL SYMPTOMS cause less euphorio 1 —_— 4 J doce gradually & STOP Sym. System @ oppostre 1 oprorps R by % by RELAPSE PREVENTION -pH NALTREXONE — CLONIDINE —BzD PLcoHOLs ALCOHOL, ETHYL ALCOHOL, METHYL ALCOHOL L pic. dehydrogenase BLOEHYDE brid. denydroge nose| 4 eED Acetic Acid 4 L Acebal dehyde Formaldehyde 1 formic acid ETHYL ALCOHOL DESULFTRAM > Inbibite Acetal dehyde. dehydrogenase > sed ag ALCOHOL AVERSION THERAPY + Instead oF euphoria, unpleasant symptoms occur on consuming alcohel dic acetal deydt DICULFIRAM LIKE REACTION > paves © > CEPHALOSPORINS [some] CHLORPROPAMLDE GRISEOFULVIN METRONIDAZOLE PRDCARBAZINE, METHYL ALCOHOL 7 BoTh formaldehyde & formic atid con cause retinol damage & blindness > FoMEPTZOL + doc for Memnol Poisoning DRUGS + ALCOHOL CRAVING None NALTREXONE oF ONDANSETRON: The TOPE RAMATE ACAMPROSATEDRUGS AFFECTING FLOW J L fein <— | Plasmin J, | ates te eor Bleeding prevent” ANTE PLATELET DRUGS So GPob|Ma Lnen sticky] 6 36 GegeTmo Lexteriorizak” 3 Plakelexs Ore | Plotetees # Blood vessel Sticky ©0e © © | ic vesse ue So INQURED ASPIRIN, > ack on TxAg, eomsoetst 1 ge on pop TICLOPIDINE RBCLALMAB. TLROFIGAN EPTLFLGATIDE ar on 4 Tb| Ma DRUGS ACT ON TAD Phospholipids 4 Rrochidonic. Add —_L________, Prostaglandins Leyeotrienes Pagal Ha ——_ -—_— TKR PGIa, PaD,/E! 6 Platelets Endothelium omer TAR > couse aggregation Par, = > Imbibit agqreqation ASPIRIN > Lrreversible inhibitor oF coxa. DRUgE ACT ON ADP + PDP Receptor Pag. 7 prves CLOPLDOgREL TICLOPLDENE > mese drugs irreversibly inhibit Pa Vig > Bom ase Prodrugs Cinackive] > Adivated by CYPACIa > OMEPRAZOLE Inhibit cyYPAcIg > shovid mot combine t these drugs > REVERSIBLE P.Y,. INHTOITORS CAN GRELOR TLCA GRELOR 3. DRUGS ACTON GP Mb] 00 > strongest antiplaiiler drugs ANTE PLATELET DRUGS ARE PREFERRED IN ARTERLAL THROMBOSIS PNTEFIBRIN DRUGS / ANTE COAGULANTS ORAL ANTI COAGULANTS WAREARIN > Inhibit te action oF vitamin 7 takes 4-5 days to manifest it's action > as already formed clotting Fatkors are tnt > vSed For maintainonce therapy + Terakogenic, Cli indicated im pregnancy > cause FETAL WARFARIN SYNDROME > monrroRIng > molnly aFrecks extrinsic pamway > monitored by Pro Thrombin Time or INR ClorTINg PATHWAY Extrinsic palway monitored by Proimrombin Time LPT] Intrinsic pathway monitored by activated Partial Thromboplastin Time NORMAL VALUES PT + ta-16 sec Lv '5s) aPTt > ae-3a Sec [~ dosec] On WARFARIN Therapy, PT * -3 times the contro! value HEPARIN mainly affects Intrinsic pathway» Monitored by oPIT Vou > Werratin Vo Heparin € > Extrinsic pathway ANT Intrinsic pathway PT > ProtRrembin TimePROTHROMBIN Time MEASUREMENT | [wea taB2 laps BEFORE WARFARIN THERAPY | 10sec. 15 See. ao sec AFTER WARFARIN THERAPY | an Sec Bo sec yo Sec. > ptFrerent tabs gives different control values for the Same somple > Sowrton + Measure bol Sampkt in SAME LAB INR C tnternational Normalized Ratio] TNR 5 | PT test PT control 7 valve oF INR Will be same in all labs 3st Ist + Internakionel Sensitivity Inder BLEEDING DUE TD WARFARIN Ry by > FRESH FROZEN PLASMA [FFP] Ry OF BLEEDING TENDENCY due to Warfarin + VITAMIN K Rj PROTOCOL FOR BLEEDING Based On INR <5 > ND 5-20 VITAMIN kK yao > FFP INJECTABLE ANTICOAGULANTS / THROMBIN [ Ta] INHTBLIORS 2, INDIRECT To INHTBITORS 2. prRect Da INHTBrTORS 2. INDIRECT Da INHTBrTORS [ HEPARIN] Heparin + Anti Thrombin Heparin + Anti Thrombin 4 GSS + Aneimrombin Activaked wee SS Antithrombin Activated 4 er ienarn, + a, a, 4 i—_ AT inhibit Thrombin in Complex Creparin + at + Da) 7 LMH [lew Molecules Heparin] inhibit Za. > FONDAPARINOK > smaliest portion of heparin thot if absolulely necessary for anti coagulant ockivity + fohibit: za AT inhibit Ka S \ FoNOAPARINGXHEPARIN 1, Route * Sic or tv Inhibit Za & Da Immediate Action ~ oseful In Qu conditions Anticoagulant of choice in pregnancy monitoring done by apTT Antidote + PROTAMINE SULPHATE sie 7 Bleeding Heparin Induced Thrombocytopenia Hoorpop THROMBUS HEPARIN INDUCED THROMBOCYTOPENIA CHIT] + Trrombouytopenia occurs ? THRomBosrS present. ron oc % DIRECT THROMBIN INHIBITORS HIT DIRECT THROMBIN INHIBITORS > progs HtRv OGD LEPIRUDIN BEVALUREDIN Ingectables ARGACRODEN MELAGAGD ED DABTGATRAN > given orally DIRECT XQ INHIBCTORE > prugs RVAPOLAGAD a Aer GDOEN) 8 EDO XA BAN aiversible corey Blocker en pxtagonist vedas 3 ANTL COAGULANTS ARE MORE EFFECTIVE LN VENOUS THROMBOSIS — Indicated in pvt & Pulmonary Embolism THROMBOLYTLC DRUGS | TISSUE PLASMINOGEN ACTLVATORS /FIBRINOLYTIC DRUGS 7 PLASMIN removes thrombus EPA Plasminogen ————?_ Plasmin > pres STREPTOKINASE Short acking, given iv ORDKINASE — ALTEPASE RETEPLASE } long ackings given as bolus TENECTEPLASE Tenecteplase -> Longest ackingSTREPTOKENASE > derived from strepto coceus 7 con couse ALLERGY + PNTEBODIES agoinst Streptokinase produced BEPA [RECOMBINANT TISSUE PLASMINOGEN ACTIVATORS 1 > ALTEPASE RETEPLASE TENECTEPLASE > No allergy . NO antibody format” occurs, DRUGS AFFECTING CELLS caus GROWTH FACTOR RBC ERYTHROPOLETIN wee @- csr am -csF PUTELens [IL - a2 Thrombopoietin ERYTHROPOLETIN > INOLCATIONS > Pnamia dit chronic Kidney disease Pnowmia dit BM suppression 7 overdose canses > Polycytemia +> prog + DARBOPOLETIN C Recombinant Erythropotetin] G-CSF & @m- CSF > TNOECATION > Leucopenia dit anticancer drugs > prvgs @- CSF > FLLGRASTIM PEG FILGRASTIM M-CSF > SARGRAMOSTIM MOL@RAMOsTEM TL-11 7 Used for thrombouytopenia dit anticancer drugs > OPRELVE KIN THROMBOPOLETIN RECEPTOR AGONISTS > used In ITP > RomLPLostIm ELTROMBO PAG,CLASSTPICATION OF AMA BASED ON 4 CtOAL pruss L kills] STATLC DRUGS Linhibits growth] TYPE OF ORGANISMS CHEMICAL STRUCTURE Source 7 PNTIBIOTICS & NON - ANTIBLOTICS MeCHANTSMm OF ACTION 0. Cell Wall symmesis Inhibitors ype b Protein Syntesis Inhibitors © Metoboligm 4 DNA Membranes CEU WALL SYNTHESIS INHIGLTORS > prvas Firraly > Fosromyctn + osed for Tt Bind to > BETA Lacrams Bacterial > BACITRACIN > tocol use only cel > crcosertn > osed in TB voll > VANCOMYCIN: BETA LAcTAMS 2. PENTCILLINS 4 and ring is difRrent in 2 CEPHALOSPORINS Bla different B lattoms & absent in monobactams 3. CARGAPENEMS 4A MONOBACTAMS PENTCILLEINS, PENTCELLIN 4 | BENZYL PENICILLIN Limtrarrons 2 not eFFtckive Orally CAcid fabiled Short acking Cdit ropid tubular secretion) Narrow spedum Resistance Pllergy wrpopa. PCED RESESTANT / ORAL PENTCLLLENS PENICELLIN V OxACTLLIN, DICLOXACILLIN CLOKACELLEN AmPICCLLEN AMNOKYCLLLIN, v beads ° D c a A. 1 DURATION OF ACTION OF PENICILLIN G > PROBENECLD compete t Pentillin at tubular pumps > + duration oF ackion of Penecillin > DEPOT PREPARATIONS % BENRATHINE PENTCILLIN G F Longest acting Penicillin > PROCAIN PENICILLIN > pepot preparations ase given by im Only 3. SPECTRUM OF PENECELLIN G soe Gram -Ive cocci Bacillus cocel Bacillus. L 4 4 1 Gtrepto Bacilius Neisseria not eFFeckive Stophylo clostridium diphtheria Listeria EXTENDED J WIDE SPECTRUM PENICELULNS A > PMPECTLLENs AmoxYCLLLIN ci - CARBENTCILUN Ty TICARCLLLIN nant PSEUDORENAL ™ > ME2LOCTUIN oRvES A > petoecuctn P > PLPERACELLIN VY vancomycrn £6 NoT EFRECTEVE ASAINST PSEUDOMONAS4. B LACTAMASE INHIBITORS cuavutinte AesD + AMOHVESLLEN *—€) a GuLBAcTam + AmpxCLLLaN renin Piscamase TaaoeAcram ‘+ PrPERACLUI sonal Bloctarmase PENICCULENACE RESISTANT PENICILLINS inbibitor c > CLOXACILLIN: ° F oxAcELitN NF NAFCELLEN BD * DILCLOXACCLLEN ° M % METHICTLLEN Cmost resistant J > mrs [ memicillin Resistant Stoph. ourevs] > resistance ig dit alterak” in Penicillin Binding Pron > pp lactams are IneFFeckive except 51% gen. Cephalosporins 5. ALLERGY 7 GRIN TESTING done by Intradermal Inject) oF drug > CROSS ALLERGY > allergic EO one penicillins 5 all p lackams are allergic except MONOBACrAmS PENICILLIN G INDICATEONS FIRST LINE ORUGS IN Loo Uererte, p> AcrENomycosts & > syPHtits T > Tetanus M 7 MEeNntNgococcus a I PTHRAX N CEPHALOSPORINS ‘ast _GEN, and GEN. Srd_ GEN. afi GEN 51 Gen EFFECTIVE AGAINST am tive arm tive Grom 4ve @ram ve MRSA qm ~ive Grom “ve Anaerobicdst GEN. Jand Gen. Srd_ GEN. AGEN CEFAZOLIN | CEFOROXLME CEFR LEXIN |CEFOXITINE CEFA LOTHIN |CEFMETAZOLE CEFA LORLDEN| CEFOMANDOLE CEFA DROXIL |CEFACLOR 1 BILE SECRETED CEPHALO SPORLNES > SoFe in renal failure 7 includes CEFOPERAZONE CEFTREAX ONE CEFOPERAZONE CEFTREAKONE. (CEFOTAXLME CEFIEZOXEME CEFPODOXIME, CEFTAZTDIME CEFTEBUTEN MOKALACTAM CEFIXIME CePEPLME CeFPrROME, [BtLe SecneTeO purr micnoarAl AGENTS eeF in PoE eS Dicence daaugaga CEFOPERAZONE ,CEFTRIAX OnE RLeRMmPLEIN, ERYTHROMYCIN NAPCLLLEN AmPrerLUN LINcosAmnoes C cliNoRMmYCLN| DoKYeYCLENE A BNTL PSEUDDMONAL CEPHALOSPORINS, > includes CerePrme CEFPLROME CEFOPERAZONE CEFTAZIDIME 3 DISULFTRAM LIKE REACTION F nok to be given t oleoho 7 includes CEFOPERAZONE: MOXALACTAM, CEFOTETAN CEFOMANDOLE A 4 PROTHROMBIN includes CEFOPERRZONE MOXALACTA CEFOTETAN CEFOMAN DOLE Limost effective anti pseudomonal cephalosporin]CARBAPENEmS ImePENEM + eerective against > am tive =~ Gm —We incl. Pseudomonas > Anaerobic > dehydropeptidese > CLLASTATIN > Imepenem > sie Kidney metabolises Imepenem rapidiy Dihydropeptidart Inhibitor Cilastaktn must be given for desired atkion Setwres elt in Epilepsy +4 4 OTHER CARBAPENEMS 7% includes MEROPENEM DORE PENEMm ERTAPENEM® PAROPENEM > Resistant to dibydropeptidase (no cilastakin required] 7 CARBAPENEMS are only drugs that are eFreckive against bacteria producing ESBLCEntended Epettrum Beta Lattamase] Cooc] MONOBACTAM ALTREONAM > do not chow cross allergy 7 efteckive only against Gm -ive batteria induding Pseudomonas VANCOMYCIN > Not erfective Orally [ NeT AsoRBED) > given by iv > releases HISTAMINE -* RED MAN SYNDROME > sie 7? nephrotoxic > ototoxic > not eFrective against Pseudomonas > use > Masa Looc) > PSEUDO MEMBRANOUS COLTTES > cormmensal bockeria protect the GIT from infection + by competing T nutrition & producing BACTERIOCIN > Broad spectrum antibiotics Killg Commensals , Which Predisposed tO SUPER INFECTEON 7 WBC forms a membrone + PSEUDO MEMBRANEPSEUDOMEMBRANE COLITLS a mc organism responsible 2 MC couse 3. Doc Clostridium difficile Srd gen. cephalosporins > Clindamycdn ORAL VANCOMYCIN Conty oral indicat of vancomycin] GLYCOPEPTIDES VANCOmMYCEN TELCO PLANIN ORITA VANCEN DALBA VANCLN TELAVANCLIN BO not conse RED MAN SYNDROMEPROTEIN SYNTHESIS TNHIBETORS a. TETRACYCLINES ES 2. CHLORAMPHENLCOL > 3. M 7 Macrottos } Inhibit the gotning oF aAR Cpeptide bond formar” J ‘bit Trangloceeion c¢ > CLENOATAYCIN Angibie: i @ 7 qurnpRrIsTIN 4. AMINO GLYCOSIDES 7 acke by causing Misreading of MRNA codon F only cided protein Synthesic inhibitor BINOING, Binding ® BIOLNOGINCO SIDES T TETRACYCLEN ES 308 bind @ gos Ribosomne Rest all bind ak 50S ribosome2. TETRACYCLINES DRUGS TETRACYCLINE OXY TETRA CYCLINE CHLOR TETRACYCLINE DEMECLOCYCLINE > most phototoxic 4 highest risk oF Dr DOKY CYCLINE MINO CYCLINE + highest vestibular dysfunction AOVERSE EFFECTS kK kidney Foilure > clr except Doxycycline Anti anabolic Phototoxic tnsipidus diobetes Liver Failure elt Denkition & Bone CCL in pregnancy & children) por be given ofter Expiry L riskoF Fanconi syndrome) Vestibular dysfunc? emork#vD hed eday uses GIRDH C pemectowycline] Rickettsia Cooc) Gronvloma Inquinale [boc] Lev Atypical pNeumonia Cooc + macroupes) cholera L oped Luminal Amocbiacic [doc For amoebiasis — MeTRoNTDAZOLE] Berza¢%8 teoudaee 2. CHLORAMPHENTCOL POvERSE EFFECTS 4. Bone Marrovo Supprescion a. Grey Boby Syndrome ([clz in new borns } 3 MACROLIDES DRUGS 2nd Line drugs to Penicillins ERNTHROMYCIN BOGIES c > Chancroid CLARITHROMYCIN L > Legionetia ROXT THRO MYCEN A > Atypical pneumonia Po pertussis AZLTHROMYCEN FIDOXOMICIN + USed im mild CO Moder Pseudo Membrane colitis+ causes stimulakion of Motilin® in arr + diorrbea is SlE 7 used in Diobetic qastroparesis [PUITHROMYCIN OTHER ®THROMYCINS” > very tong acting + Relatively short acting 7 non mivosormal enayme © > microsomal enayme inhibitors. + Fewer drug interactions > _more drug interactions CLINDAMYCIN, > Sewreted in Bile > couses Pseudo membranous colitis > vsed In anamobic backerfal Infecions QUINPRISTIN + DPLFOPRESTIN > Bom ore Gtreptogramins > indicated in yeasp Coo; + DaPromYCLN] 4. BMINOGLYCOSTOES DRUGS STREPTOMYCIN Not eFFeckive orally Coot absorbed GENTA MYCIN es ackive mainly on Gm ive Cincl. Pseudomonas] TOBRA MYCIN eMok -eFRchive ON Onayobic batteria NETEL MYCIN + cidal drugs NEO MYCELN, *Mephrotoxic Cmax. by Neomycind SAEREGETSEA Puditory Cmax. by Amikacin] KANAMYCEN * oboto Arc arneenere ie CKemox. by Streptomycin] "cause newromuccular blockade [max by Neomycind > cAPREOMYCIN is chemically not aminoglycoside STREPTOMYCIN TB, Plague CAPREOMYCIN, KANAMYCIN and tine drugs for TS PMEKACTN NEomycEN Hepatic coma C given orally]BACTERICIDAL DRUGS CONCENTRATION DEPENDENT KILLING [CDK] ob. > > TIME a Post t fing concentration above minimum cidal Concentrak”, More bockerio are Killed High & lesc Frequent doses required Followed by AMINOGLYCOSIDES FLUORO QULNOLONES: tong [dt min. Conc to Kitt) inhibit, OPEN DENT KILLING [TDK] Killing activity do not depend on concentration Killing depends on tirne at which Concentrakh ig above min. Killing Cone. Small &| multiple doses axe given Followed by B lactams, Vanco raycin: PNTreroTcEC EFrecT [ PRE) Time ak which Supression of bacterial qrowlh . occurs even When the Concentrak” fallen long ist Sahin belows the Minimony inhibitory concentrak” — PRE > > LB hrs > Long PRE < l5 hrs > Short PRE All the drugs inhibiting Protein synthesis or DNA OF bosteria have long PAEMETABO PTERIDINE + PABA + GLUTAMATE SULFONAMIDES —- Foise werd SYNTHASE Dlec ——> oltre actD TREMETHOPRIM PYRIMETHAMINE a DLHYDRO FA REDUCTASE TETRA HYDRDFOLIc ACLD [FOLINIC AID] t DNASULFONAMIDES / SULFA DRUGS Drugs SULFA DOXINE SULFA CYTINE SuLFA SOXAZDLE ADVERSE EFFECTS crystalioria. To ,pPOCoOD tbe lures SULFAMETHORAZOLE Rosh SULFA SALAZING poetylaion SuLeA OTAZENE. sie DAPSONE. > sulfonamide t minimom risk oF crystalluria, 7 SviFadoxine F tongest acting > GuiFacytine > Shortest acting, 1 Sulfasalazine > prodrog 7 uses 7 olcerative colitis Coo) Rheumatoid Artiritts Aplastic onemia Bilirubin displacement > cause Kemictrus in Mew bors. Hemolysis in G6PD deFicienry + Sulfa So xoanle Dermatitis Herpetiformis > Aq Sulfadiazine + Used for Burn dressing > vapsone > Used for Leprosy ComBINATLONS CorREMORA ZOLE TREMETHOPREM + SOLFAMETHOXAZOLE rabio for best botkericidal activity + 12a0 ratio in table to attoin this robin = 135 oc For P > Pheumoaystts giroveci N 7 Nocardia B > Burkholderia cepacia @ SULPADOXLME + PYRIMETHAMINE. * Indicated in Parasitic. infections > malaria > ToxoplasmosisDNA GYRASE INHIBITORS > DNA GNRASE = introduces negabive Coils G helps In replication F DNA qyrase Inhibitors > fhibit replication + Chemically these are QUINDLONES QUTNOLONES a) NALIDEXIC ACD > used in ort © FLOORD QUINOLONES FLUDROQUTNOLONES prv|as NORPLOXACLN > used in ort CIPROFLOXACIN: > oral Doc For Typhoid & Doc for AnRrOX OFLOXACIN PE FLDXACLN, ‘SPAR PLOXACLN. LEVo PLOXA CLN, MoXT PLOXACLN + Long acting 5 ofs0 active agoinst anaerobes GATE PLOXACLN, F Withdrawn C causes dusqlycenial TROVAFLOXACIN + oral Gdad drogs > Wide spectrum [am tive & Sm -ive] > cit in pregnancy & Children C induce seinures Covoidad in Epilepsy] > 2 in Renal Fajlure EXCEPTION Poo PRLOXCLN ™ *% MOXTFLoxACLN 3 TROVAPLOXACIN > phototoxicity Cmax. t Pasfloxadn] + RESPLRATORY FQ © > GFLOXACLN M 7% MOXITPLoxACIN @ 7% GATE PtoxAcin LEVOFLDxAcIN Lisomer OF ofloxacin, Long acking 7 7 ackive aqainst respiratory Infections caused by Gm tive bacteria mm -Ive backeria Aeypical bacteria, Mycobacterium TBDRUGS ACTING ON MEMBRANES. DRUGS ANTE FUNGAL DRUGS POLYMYXIN B PoLYm YxtN E [coLEsTEN] DAPTOMYCLN i used for Pseodomonan —> boc For vRsw Cause Myopathy Csi]ANTE TUBERCULAR DRUGS FIRGT LINE DRUGS H > IsontAzZto R > REFAMPLCLN CRcENI 2 > PYRAZENAMmDE —& > EMAMBUTOL S > stasPiomyctn JACTLVITY|BACTEREA | HEPATOTOXIC | PREGNANCY tt _[eiciat [om R cidol Bor 2 [cided _|tie & _|scatic |eom s_|eidat [ec MYCOBACTERTA Locarton. Errecttve org | Pact @ROwENG wal 4 | INTERMEDIATE @RowiNg | Spurters Leasseous neamsis) | _R SLOLD_ GROWING, ite 2 Isontazrp CINK) 1 camge Pyridonine Cvit®¢] deficiency > tends to Peripheral neuropathy 2 Hepakotoxic i } ‘ingure 2 metabotine by Acetylation N nerves A couse GLE 7 Hepatotoxie. RCIN J. Shovid give on empty stomach a. Seercted in Bile > Safe in RE 3. Enayme Inducer INTERACTIONS Warfarin ocP Anti HIV drugs Replace’, Heparin Replace’, omer contraceptive memod _—____, RCIN replaced & RIPABUTINREFABUTIN REFARNPLCLN Enzyme inducer + tt +t Durak oF ack? Longer acting Short acting Errective on Atypical mycobarteria m.Te sie no hepakotoxic Hepakotoxic Pseudojoundice coveitis 4 OTHER USES OF RCCN > Leprosy, meningococcal meningitis Prophylaxis Cast line dreqa MENINGOCOCCAL MENINGETTS PROPHYLATS CIPROFLOXACIN: REIN CEPTRLAXONE, Brucellosis Looe > cexyeyclin + REIN] MRoA Pseudomonas PYRAZINAMIDE [7] > errective only on jie backena. > moxe hepatotoxic > cate hyperoricemia ETHAMBUTOL, > PFreck Eye + Red green colovr blindness Coptic neuritis] > Initially reversible , later irreversible > avoid in <6yr aqe children STREPTOMYCIN, > not efreckive orally Cgivey by im] Dephrotoxic ototoxic couse Neuro muscular blockade. And LINE DRDGS 1 FQ 0 Floxadn Moxifloxacin, GabiFioxocin Levofloxacina. INDECTABLE CAPREOMCLN KANAMYCIN AMLKACEN + 3 LINEZOLIDE used for vRSA CLOFAZIMLNE > used for moltibacillary leprosy 4 CYCLOSERINE 7 cause Nevropsychiatric Sie ETHIONAMLDE =F hepakotoxic , hypormyroidicm PAS + hypotyroidism 5 NEW DRUGS PEE t couse TDP Cf @r inervo!] BEDAQUILINE TS TREATMENT RNTCP > bors cara cara INTENSIVE PHASE @ HRZE 2 HRZES + | HRIE + + CONTENVATEON PHASE | 4 HRE 5 HRE > Baily therapy given MOR - TR > resictont to bom OH + R > IP + 6 monms 2 6 dregs given cP > 1B MonmS » 4 drugs given PR MOUTE BACTLLARY LEPROSY RCEN 00mg Once moNTBly } sunerveat CLOFAZAMINE 300 mq Once monly ® TUmOORE CloFAZAMINE —5Omq once daily x2Bd } nsupervised DAPSONE loomg once dolly x28d PAUCEBACELLARY LEPROSY > is RCEN Goomq once monthly Supervised 2 Ee DAPSONE tooma once doily x28d > unsupervised FB imycobacteriom aviv complex] > alo HU TREATMENT > RIFABUTIN: + ETHAMBUTOL + CLARITHROMYCIN PROPHYLAXIS “> ALITHROMMYCEN Cweekly | CLARITHROMYCIN [ BailyJANTE MALARIAL DRUGS > Plasmediom Knowlesi can also couse malaria arf Chyprezcite] — responsible for relapse Eryirouytic stage Gamebocytic stage TREATMENT MODALITEES cure PROPHYLAXIS. aS ———— CLINECAL RADICAL SUPPRESSIVE CAUSAL, L 4 4 + Erymroagtic % EBxo-Erywrocytic = Ry ErylRrouytic Ry Pre Erymocytic Stage stage stage stage PRIMAQUINE, > RCTS ON PRE ERYTHROCYTEC SAGE 7% used for casual Prophylaxis Exp ERXTHROCYTLC STAGE > used for Radice! cure GAMETOGENLC STAGE > used to prevenE transmissfon > cork act on ERYTHROCYTIC SIME + not useful tO Ry Or prevent moloaria > com couse HEMOLYSIS In GEPD Deficiency > aL in Preqnana & infants DRUGS ACTENG ON ERYTHROCYTIC STAGE FAST ACTING Slow ACTING M > MEFLOQUINE PROGUANINE ® > RTOVAQUONE PYRIMETHAMINE © 7% CHLOROQUINE SULFA DOxINE H 7 HALOFANTRINE DOXYCYCLINE 8 > PRTEM\ISENINS CLINDARYCIN: Ro Res - @ CQqutntne]CHLOROQUINE + causes BULL'S EYE macuLoPATHY Lon prolonged usage for a-3 yrs] USES R > Rheumatoid Artaritic e 7? Extraintestinal Ameobiasis o > pe L > Lepra reactions ¥ 7% rnFectious Mononucleosis P > Photogenic Reackions Mahatma * Malaria gondhi 7 Giordiasis PRTEMISENENS. DRUGS RTE SUNATE ARTETHER RTE METHER DEHYORO ARTEMISININS Fostest acting antimolariale erretkive against MOR short acting Ci in 1st trimester boeed ARIEMESININ COMBINATION THERAPY LACT] > prtimisinin + Long acting droq 7 voc for Chloroquine resistance > comernArions LOMEFANTRENE + ARTEMETHER, > oc in Norih Estern stoies. BRTESUNATE + SULFADOXEME — PYRIMETHAMINE > DOC For rer OF India TREATMENT OF MALARIA ONDER NVBDCP TREATMENT OF UNCOMPLICATED MALARLA [ Tee Trimester P. vivax malaria | chloroquine Chloroquine P. faldperam malaria Act Quinine mixed infection ACT Quinine complicated or Ww Artesonale Severe or Cerebral * Motori AcTboc HERPES VIRUS nev -2 Hsv -2. cmv INFLWENZA, #ePpTETTS Hey Reve CHRONTC Hey } ACYCLOVIR me GANCYCLOVER AMANTADINE > atke by Inhihibiting Uunceaking osetrAmiVvER ZANA mivER acts by inhibiting Newrominidase PERAMIVIR Symptomatic ENTECAVER | TENOFovER Lfirst line drugs LamiyuoINn EmrRicttTABINE TEN Earlier INP RUBAVERIN Cinholational] Present my Coral] 2. PROTERSE ENHEB@LTORS TELAPREVLR BOCE PREVIR: STMPREVER, PPALTA PREUER 2. NSSA TNHTBITORS LEDIPASVIR DECLATASVER, 3. NSS®& TNHEGITORS SOFOSBUVER DASABUVIR,2, FUSTON INHEBETORS a. RTINHTerTORS 3. TNTEGRASE INHTBETORE A. PROTEASE INHEBrTORS 4 FUSION TNHIBITORS ENEQVIRTEDE MARAUEROG 7 bindg T Gpal > binds T CCR-5 > not given orally > given orally + con't bind © cO,cells T cxcRy A REVERSE TRANSCRIPTASE LNHEGETORS [comPrTireve NON ComPrttttve INRTL C Nucleotide (side} RT tnhibitors) NNRTE_ {Non NRTE I Nucleoside RIT 1st GEN ALOOVUDINE EFAVIRENZ ETRAVIRINE LAMEVUDENE, NEVIRAPINE RILPLVIRINE STAVUDINE DELAVERDINE DLOANOSINE ZALCLTABLNE EMTRECLIAGINE ABACAVER. SIE OF NRIIC > Peripheral neuropathy & Pancreatiti: maX FISK OF PeriphUal neuro pamy STAVUDINE max risk OF Pancreatitis DIDANOSINE min. Fick OF Peripheral neuro pay UmtvonENe (sorest eT) Bone marrow Suppression by, ‘TWDOWWDENE, Mt predispesit™ py BACAR, NRTLS Used for Hep. B Lo LamtvuprNe E 7 EMTRICIrABINE T + TENOFOVER.3 INTEGRASE INHIBITORS DROGS RALTEGRAVER ELVITE GRAVIR DOLUTEGRA VIR: 4 PROTEASE INHTBITORS DRUGS RUONAVER LOPENAVER AMPRENAVER, FOS- AMPRENAVIR, BTAZANAVIR, > Lowest risk OF Lipodystrophy syn. SAQULNAVER buk con couse hyper bilirubinemia NELFLNAVER 1 metabolized by CYPZA4 a CYP3A4 Inhibitors themselves > Gerongest > © RITONAVIR. > RUMNAVER BOOSTING F boost the Ofer Inhibitors 3 couse LIPODYSTROPHY SYNDROME Loalso caused by Atypical Antipsychotics] * Glucose 7 Lipids, ANSulin Resistance we. gain vive HAART > Highly Active Anti Retro Viral Therapy 2. WHEN To Ry > All patients irrespective OF cD, Count a. HOW LONG => LiFe. tong 3. WHeT Minimum 3 Drugs from minimum a groups > aNRTL + INNRIT / IL zie +n T4+uU4FITT 4. PMMPHOTERICEN B Armehotericin 8 HV Ya ergosterot Tnpocellulor contents 7% cldol drug > not eFteckive orally C given tv] oc for Severe Fungal infeckions > Infusion related reactions me] 7 Renol Tubular acidosis t 4 kt Cine dose dependent I > Anemia LIPOSOMAL AMG, 7 4 nephrotoxicity > costiy > poe for Kala Azar a A20LEs DRvgs KETOCONAZOLE: FLUCONAZOLE > woe For Crypococcus & Candida infections TRA CONATOLE VoRICONAZDLE = POL For Asperqillosis POSACONATOLE 7 Fungi static drugs > KETOCONAZOLE > enzyme inducer > cause qynecomastia 3 @RISEOFULVIN = Fungi stakic high affinity for KERRIIN — used only For Dermokophytosis [not preferred now) > Food t absorpt” > con couse Ddisvlfiram like reac” + _Relapses are common4 TERBINAFINE > Fungicidal > has high aFFinity for KERATIN = poe For Dermatophytoses 5, ECHINOCANOTNS CASPO FUNGIN > used For Condida Cooc ~ Fluconazole 3 Asp ergillosis C pot ~ voriconazole I 1. Ameostasts > boc Lominal aAmeobiasis 7 DILOXANTDE FUROATE tnrestinal /hepakic Ameobiasis > — METRONEDAZDLE TENEDAZOLE SECNTORZOLE ORNDAZOLE SPTRA NEDAZLOLE > pisulfiram Like rxm can be caused by metronidorole group > METRONIDAZOLE 4 Giordiasis Cove) v Peptic ulcer Component of TRIPLE DRUG THERAPY] Pp PMc Looe) 7 Trichomoniasis Cooc) a Anaerobic bacteria Coe] A@rmeobiasis Loocd, a. LETSHMANIA KALAAZAR | VISCERAL LELSHMANTASTS > poc + Single iv infusion OF LIPOSOMAL AMPHOTERESIN B 7 Na STEBOGLUCONATE > used For mucocutaneous Leishmaniasis [poc) kalo Aaor > given im > MILIEFOSINE = only oral drug for Kala caor 3 TRYPANOSD MA PFRICAN TRYPANDSOMIASLC/ SOUTH AMERICAN TRYPANOSOMIASIS | SLEEPING SICENESS CHAGAYS DISEASE early stages > SURAMEN Cooc} BEN2NTDAZDLE LOoC] loke Stoges > MELARSOPROL [poc]PLATYHELMHENTHES Tape Worms > poc > PRAZLQUANTEL except §Echinococcus granulosus Cd0q Tapeworm) 7 poe for Echinococcus gronulosss > ALGENDATOLE Flokes > pec > PRALLQUANTEL except For Liver Fluke C Fosiola hepatica] > Doc for Liver Fluke — TRICLABENDAZOLE NEMATODES 7 poc for all Nematode incl. larvae + ~=RLBENDAZOLE > Except Fllaria > pec CDi Emy) Corbamazine J Strongyloides 7 wermecine OnchocercaAROVERSE EFFECTS BM Depression Plopecia Mocositis — diarrhea Hyper eri cena a 2 3 4 ceu cCNCLE SYNTHETIC PHASE [s] 7 DNA Doubled Merortc PHASE CMJ > DNA reduced to half GAP PHASES (4, & G,] Non Selective Drugs + bind to DNA S phase Specific Prugs > inhibit ONA symmesis Mm Phase Gpecific Drugs —~* inhibit mitosis a, Sa o1 ALKYLATING AGENTS Mon, me site oF cukyloEn Bm) Fg or vente oot ADVERSE EFFECTS 2 BM Depression Plopecia Mucositis > diarrhea Hyper uricenia Bo Leukemia Sterility aura DRUGS MELPHALAN MECHLORETHAMINE CXCLOPHOS PHOMEDE ‘IsoseAmMtoE BUSULFAN CHLORAM BuCLL PROCARBAZINE, NITROSOUREAS Hemornnagrte — | Prevented by RBCROLETN eNSTETES |e cause Lung Fibrosis used for Chronic Lymphoid Leukemia couse Disulfiram like Rxn i ds NETROSOUREAS RUGS cARMUSTIN Lomosrtn can cross BBB => Used in Gliomas SemustiN a, PLATENUM COMPOUNDS Druas CESPLATEN CARBOPLATIN OXALLPLATIN > used for COLORECTAL CARCINOMA, Mon = Atkylating Agents BIE = ArKYfabing Agents (CLSPLATIN F most emitogenic anticancer dq [noc > SHT, 1 Condansetron)] > nephrotoxic > oxotoxicCOLORECTAL CARCINOMA REGIMES FOLFOX REGIME FOLFIRL REGIME Fottntc ActD + FoLtntc ActO + 5-FU = 5-FO cd OXALL PLATIN IRINOTECAN 5. PNTEMETABOLITES + 5 Phase specific 0. Drugs affecting FOLIC ACLD MerAGoLTSm b. Drugs affecting PURINE meETAGOLtSm ©. prugs affetting PYRAMIDINE rmeTmBOLTSM . DRUGS AFFECTING FA meTABOLTSM FOLLC ActD SYNTHESIS PTERLDLNE + PABA + GLUTAMATE J pice = DIHYORO FOLtC ActO [FH,I Colic Acid] MeTHORERTE + pHeRase TETRA HYDRD FOLLC ACrD LFHyJ Leplinic eid] + DNA METHOTREXATE > Metmotrexate Poisoning Ry by FOLENTC ACTED | LEUCOVORIN] CIROVORUM F con couse megoioblastic anemia > hepatotoxic F poe For Choriocartinoma 7 me osed oMmARD PURINES PYRAMMEDENE Paenine cytosine @yanine Thymine b, DRUGS AFFECTING PURINE meTABOLISM Daves 6 - MERCAPIO PURINE 5 hepatotoxic 6 — THIOGUANINE CLAORE BENE > pec For Hoiry cell Leukemia PLUDARABINE 7 poe for cu6 ~ MERCAPTOPURINE © ~ MERCAPTOPURINE xanTKIne L xanmine oxi Degradation orie Acid TL ALLOPURENOL combinakion, 6 MP close Should be reduced T ALLOPURENOL combination, AZATHIOPRINE dose should be reduced > 6MP if the ackive metabolite OF Azathioprine © DRUGS AFFECTING PYRAMEDINE METABOLISM pres 5 — Fluor opactt (5-FUT > couse Hand € Foot syndrome CAPECETA BIN > given orally, metabolized to 5- FU GEMCITABIN > voc for Pancreatic carcinoma CYTARABIN > causes cerebellar side effects > mic sic OF 5-FU > diorrhea 4. DRUGS ACTING ON MITOTIC SPINDLE SPINDLE FORMATION + Polymeriaakion oF TORULIN ~ Spindle Formation centriole Spindle, > Specific for M-Phase of cell oye SPINDLE FORMAT” LNHIBTTORS SPINDLE BREAKDOWN ENHTBETORS VINERISTENE PACLETAXEL VIN RLASTINE, SIE > Peripheral newopany SIE > Alergy stAot VENCRIGTINE > Morrow Sporing anticancer drug 5. TOPOISOMERASE INHIBITORS > Topoisomerase introduces negative collings & aid in replication TOPOLSOMERASE T INHIBITORS JOPOLSOMERASE T INHEBITORS TRLINOTECAN ETOPOSTDE > used For colorectal carcinorna BNTHRACYCLINES % cardiotoxic boxoRverctn DoNoORUBICINETOPO SLDE 7 con couse a° Leukemia [Early in onseéI ANTHRACYCLENES * Cause cardiotoxidty > prevented by DEXRAZOXANE 6. Mrsc DRUGS BLEOMYCIN + Marrow Sparing > cause pulmonory ffbrosic L- ASPARAGINASE a > marrow Sposing 7 used For AU > couse Allergy * couse Acute Pancreatitis wes RETLNOLC ACID > vsed in Acute Promyelocytic leuremia Cm, - Ami) 7? acks as maturation agents THALLDOMIEDE 7? used For mpukiple myeloma > cit in pregnancy > Conse Peripheral newropotny > Caonuce constipationSMALL MOLECULES MONOCLONAL ANTI BODIES Can be given Orally Ingeckables SMALL MOLECULES a. TYROSINE KINASE INHTFBITORS ber eI Ob! ber > TIRDSINE =———? CML KINASE Chr. gd ch.2a, t 9,23. PHILADELPHLA CHROMOSOME TmMATENEIG > Doc for chronic Myeloid Leukemia —? IMATINIBGENERAL PROPERTIES 2. Pit end t Enib? a. orally cFRctive 3. metabolised by microsomal enrymes a2 emt I > ImMATINES (boc) N > NCLOTENES D > DASATENTB. a. LUNG CARCLNOmA, Aeter > AFATINIG gE * ERLOTINTS, c os CERITINIG, q - SEFTENIB 3 RENAL CELL CARCINOMA Poo PAZTENTA ® * AXITE NIB S 7 SORAFINER S 7 SontrEnre. 4 HEPATOCELLULAR CARCINOMA =) SORA FENES 5 GtsT [Gastro Intestinal Stromal Tumors] S > SuNtrenrB 1 > imattnsB Loocd R => REGORAFENIS: * also ured For colotettal carcinoma © MALIGNANT MELANOMA. D > OABREFENTB vo VEMURAFENIB T 9% TRAMELTENTB J MEDULLARY CA OF THYROLD > VANDETANTB A PROTEASOME TNHTBrTUAS ‘ Bore zom168 tomer prugs CARFILZOMIB, TxazOmIB > used for Multiple Myeloma3 PARP INHIBITORS [Poly ADP Ribose Polymerase Inhibitor] OLAPARIG > used in ovarian carcinoma g >wr>?Pro > Poly > ADP ate > Ribose Polymerase > ovarian carcinorea. Cuse] 4 CYCLIN DEPENDENT KINASE INHEBETOR [CCDKI] PALBOCICLE > oral droq For Grenst carcinoma =. PALA 8 > ° > CICLLBN > MONO CLONAL ANTEBODLES > end ce tmag? > ingeckablec Progs CETUXEMAB PANLrUMUMAB RITUXS MUMAB TRASTUZUMAB PERrOZUMAB DARATOMUMAB OLARATUMUMAB beeboge acks on CDK-a» CDK 6 Breast cana Cuse} oral Cyclin dependent Kinase inhibitor used For coloretkal ca used For colorectal oy used For sed For sed For vsed For used For NHL Breost CA 5 SIE - casdiotoxic Breast cA Multiple myelonna. Soft tissve Sarcomo. 1, STEROTDS DRUGS TARGETING THE CALCINEURIN PATHWAY NFAT POg. © $ colcinewrin Neat Cackive] L ra. L 6 ure 4 © wxeR — mmmontry NeAT- Nuclear Factor of Ackivaked T cells &. SELOSFORINE] TacRoLmos bh pacurzomns, BASLE mAs, strouimes evenoumusQ. CYCLOSPORINE & TACRDLEMUS > nephrotoxic hepatotoxic. NeusoeoRie BP sugor Kt Lipids ed > Hirsutism > caused by Cyclosporine © stRoLImus & EVEROLIMUs > cause BM suppression 3 ®ANTI METABOLITES METHOTREXATE, PZATHTOPRINE. MXCOPHENOLATE MOPETIL LEFLWNOmrDE 4 MONOCLONAL ANTE BOOLES > monocional Ab end t 'mas? MAB + Fusion proteins end t © CEPT? > _— MAB p SOURCE > Animal Chigh risk oF allergy] > mixture - chimeric > end ¢ ‘xt mob" — Humanized = + end t © ZU mab? > Homan > end t fo mob? Ree t chimeric high risk oF allergy? TRANSTU LUMAR > Humanized PANTTUMUMAB + Humon Lleast risk oF allergy) + ~_ ~~ mob ceTuxtmas, * RETUXEMAB TARGET > TS > Tumor TRANSTUZUMAB PERTUZUMABTARGET Tj > Tumor vt > virus > PALEVE Zuma > For RSV cr > Circular? % RARCIXEMAS. > Antiploteler drug BEVACEZUMAB + Inhibit angiogenesis os * BONE DENODSUMAB > osed For osteoporosis oc > over +> ALTROCUMAB 7 vsed for hypercholesieremia Cholesterol = EVOLDCUMAB. tt > 4immo- * A ADALTMUMAB MAB agoinst TNF & nity © CERTOLEZUMAB vsed For —& GrANERCEPT RA In INFLEXTMAB crohns Disease oli GOLIMUMAR Dac Lt 2UMAB > mae against 11-a® BASILIXIMAB used For transplont® EFALIZUMAB, > used For Psoriasis NATALCZUMAS + used for multiple cclerosis ECULT 2UMAB > mob against C5 Used for PNH OMALEZUMAB > mab against 1g& used for Bronchial astima| 5. INF-4 4 at + ANAKINRA ¥ 1lL-6 4 > TOCLLEZUMAB GARILUMAB => _—Osed For RA & CO- STEMULATION INHIBITORS > peprncerr > used for RA @ THALIDOMIDE. > used for ENL7 Based on Chemica} Structure [CRT > hove autocrine eFfecks (Local eFFetcs} 0 PEPTIDE AuTocOLns + ANGIOTENSIN > BRADYEENIN b PMINE AUrocorDS + HISTAMINE a: © LEPED AUTOCOERS > PROSTAGLANDINS > Levcorrienes, > THROMBOXANE RECEPTORS LOCATEON Betton BWCKERS H, 2. BUergy Inflammation a. Stimulates RAS Promote wakefulness Hy _| Stomach Hg [Pre synoptic | BRAKE lig # OF INVERSE AGonTET [TLPROLESANT C PLroLtsAanT) used for NARCOLEPSY Hig | Wee Ha BWWCKERS ist_ GENERATION. Rind GENERATION crocs BOB, cause Cedar? do net cross BBB, No fedath Beh + anticholinergic Sie occur no Ach H useful For motion sictness brug induced Partingonism Musculor dystoniag Useful only for allergy alley PROMETHALINE Emax. ost®I TERFINADINE > Mot used CTDFI DIPHEN HYDRATING FEKOFENADINE 4 TerFinadine membolite, DIPHENHYDRINATE Acremez0lE > ~—not used L1pPd PHENTRAMINE LoRATIDINE CHLOR PHENTRAMINE DES — LORATEDINE CXCLEZINE, CETREZINE , LEVO CETREZENE CLNNARIZINE PYZELASTINE , OLOPATADLNE ~TOpicolBANNED DAVES dit AT PROLONGAS® [TDPI c oF CISAPREDE A 7% ASTEmAZOLE 1 7% TERFENADINE SEROTONIN RECEPTORS 7 F Receptors , 5-HT, - SHT, 7 S-HTs,64 7% Present in Broin ‘BUSPIRONE, Anxiety GUMMATREPTAN | acute Severe NARATRIPTAN | migraine Cooc) ELETREPTAN RETATREPTAN Blockers CLOZAPENE Btypical OLANZAPINE. antipsychotics LORCASERIN | Obesity ONDANSETRON | DOC For GRANTSETRON | Chemomernpy | TROPESETRON —_| Radiofherapty in- PALONOSETRON | duced vomiting Post op vomiting ‘Agonists | CISAPRIDE GERD Prokinetics MOSAPRIDE Looe - pprs]) tos > Podystrophy Syndrome LIPLD AUTOCOLDS CFTC)Phospholipids L purrs Prothidonic. Add cox Lox Prostaglandins Leucotrienes PagslHa hi ——_+—_ Rg, TKAy | PGIg. PGDAIEI 6, <—™ PloKelets Endofelium — omer UB, LTcy, 4 Ud, + LE, LTB, mojor Fund.” > Chemotaxis L1cq UDay , LEY > Bronchoconstrickors -* Bronchial Astkma EFPEcTS a Fever Poin Inflommakions a PuATELETS. Tap, > Pagreqation PGI, Inhibition oF aggregation 3 Heart buctus ARTERTOSUS > Connecks pulmonary trunk Eo adta > Present in TUL it Kept open by PGE PDA [patent ductus Arteriosot J TREATMENT ASPLRIN INOOMETHACEN, TOUPROFEN TRANSPOSIT™ OF GREAT VESSELS ALPROSTADIL (PGE, analogue] indicated to Keep open the DA4 Gio vesseLs > Poe, } cause Vosodilation Paty > tioprost C(par,] > Used for Pulmonary Hin, 5 UTERUS > Pee. a } Contracts Upper segment oF uterus. POF ay > PGE, Relaxer Lower segment oF uterus > wrsopRosto CPGE, analogue] uses > Abortion > cervical ripening in induction oF Labour > cARBOPROST Used For PPH Cooc ~ oxyTOCIN] 6 sTomacH Par, > inhibit Proton Pump > 1 mucous g| bicorbonate > vasodilotion Protecke for PUD 7% COX Inhibitors [NSAIDS] cause PUD -* NSATD INDUCED PEPTIC ULER Ry by MESOPROSrOL Looe + PPrsd # ENE Parag = > T Uveo sacral outFiow 7 LaATANOPROST > BOC for Primary Open Angle Gloucoma 7 sie e Pigmentation of iris CHekerodyromia iridis] gq Grow oF eyelaghes C Hypertrichosis J F. ‘nehPhospholipids STEROrDS + pip Ag Rrothidonic acd NSAT Deg Lox Prostaglandins Leucotrienes Pa galHa 41 TKAg = PG@Ig Panel § Plakelets Endomelium omerconn cox -a constitutive Enayme Inducible enzyme Inducible ak site oF inflammak™ @ sites > kidney Endothelium NS NSAIDS NON GELECTIVE COX LNHEBLTORS SELECTIVE COX-2 INHIBITORS * risk oF PUD lece wick oF PUD NON GELECTIVE COK TNHEBETORS brogs PSPERIN, PARACETAMOL [ ACETAMENDPHEN] IBUPROFEN. > NSAED oF choice in children, DreLoeENAC. INDOMETHACIN + Gedakive MEFENAMIC ACED PIROXECAm + beng a PHENYL BUTAZONE USES Fever Pain inflammot” SIE Pup PARACETAMOL / ACETATTNOPHEN > only NSATD T 90 anti - inFflammekbory activity PEROAIDE THEORY > PEM is Imackive in preence OF HO. > Less visk OF PUD COX 3 INHTBIT THEORY - Pm inhibits Cox-3 In cNS Approved in children for fever & poin > 7 NAPAt (N-Acebyl Para- amino ben26 @uinone Imine] Pom a ane Inackive, NAPQL + ONAPar bas high aFRinity for — SH qroup > Glutathione produced by Liver binds & NAPOT & Nevtrolises i> PCM Toxictry 7 occurs dit 4 overdosage 2 Liver digeare 3 chronic Alcoholic 7% pnttpore > N-ACETYL cysTerNE [Doc] ASPLRIN > only Irreversible cox inhibitor + ontiplotlet drug > cL in child T Viral infect LRisk OF Reye's syndrome] * can cause Hyperuricemia of therapeutic doses > avoid im govt SALICYLTSM Respirakory centre ® Hyperventilabion 4 + Coy 4 Respirakory Alkoloss 7 Reversible 4 Heoy tacle aad Aspirin Metabolic Acidosis > irreversible > TREATMENT NOHO > reverses mekobolic acidosis > helps in aspirin Excretion SELECTIVE COK 2 INHIBITORS Dava@s CELE Cont 4 Gt Toxicity RoFE COXIB ” Mr not ist line dregs VALOECOXIB 1 stroke, } ETORECORIB PARECOKIB LomiRAcoxtB > Etoricorib + longest acting > RoFeconib § valdecoxio i¢ wimdrawnAcuTE Gout 2. NsAtps Looe) a. STEROLDS 3. COLCHECINE [most effective] Sle > myopathy Severe diarrhea, CHRONTC GOUT OREC ACLD PRODUETTON, Proteins | Purines t xon mine @ — } xonmine oxidose oric Acid > Excrekion © @ in birds { 4 vricase @ AUANTOEN Formak” of uric Acid Excret of uric Add Lortcosurtc Drugs) LLOPURINOL PROBENECID > inhibit xanmmine oxidase SULFENPYRAZONE + boc for chronic gout BEN2 BROMARONE LESTNURAD PEBUXOSTAT > inhibit xanmine oxtdace 7 Plenty oF Fluids should be token ric Acid Metabolism @asOGRLeas=> > Recombinant PEGLOTECASE NSALDS DMAROS or STEROIDS SAARDS 4 Poin & inflammation nO efFett on disease progression | Slows down the digease progression Fast _ocking Slow acking DMARDS 7 Disease Modifying Anti Rheumatoid Orugs SAARDS —* Slow Acking Anti Rheumatoid DrugsDMARDS CONVENTIONAL cote > CHLDROQUENE > PENTCELLAMINE A > ALATHTOPRINE gq > goin sAUs L > LeFLUNOmIDE 1 > Lmmnonio SUPPRESANTS Mallika, > METHOTREXATE Sherawat > SULFASALAZINE CHLOROQUENE > used in maloria PENLCLLLAMINE 7 antidote for copper poisoning Cwilson's Disease] ALATHTO PRINE GOLD SALTS LEFLUNOMIDE LMMUNO SUPPRESANTS: METHOTREXATE, > me vsed » DOC SULFASALAZINE > voc For vicerative colitis BLOLOGICAL OmaARDS Co- srEmyLnT? INHIBITOR BDALLMUMAB: CERTOLE ZyMAB ETANERCEPT INFLIXIMAB, Geli GoLEMuMAB ANAKINRARECENT ADVANCES ETLOLOGY Of MLGRAINE VASO DILATION INFLAMMATION > major inflammebory mediator > calcitonin Gene Relared Peptide [carp] TREATMENT a NSAID a TRIPTANS ERGOTRIMINS Stimulo& SHI gj ® 7% Vasoconstrict? & + tnflammot” TRIPTANS > poc ERGOTAMENE % More emetogenic» Mot preferred> Triptons can Canse Coronary vasospasm % Cir in CAD DLTANS | 5HT;~ AGONTSTS +> do not couse coronary vasospasm (LAcmrprran] CQRP ANTAGONIST ERTUNUMAB * monoclonal Ab againsc CgRP + approved for prophylaxis of migraineCOLCHIC i, aA MECHANTSM qranuloays PG Gensomol > inhibit granulouyte migrak® ws wemeer > inhibit the releoce of Glycoprotein From neutrophils SOC? Ged) synovial ceil 90: > Inhibit mitotic spindle in neutrophils eeLOCAL ANAESTHETIC AGENTS eEsTeR AMCDE Not COCAINE. LIGNOCAINE “at PROCAENE BUPLVACAINE CHUDRCAENE PRILDCALNE Nabe p ae Ron TETRA CAINE ETLDOCALNE BENZO CAINE ROPLVACATNE DIBU CAINE 7 only LA causing vatoconstrice —~% COCATNE me used LA > LrqnocetNe Shortest acking LA > chlorprocaine LA causing Metmamoglobin > Prilocaine max. Cordiotoxic > Bupivacaine INFILTRATION ANESTHESTA = Shoxk jacking 5 dIE entry into blood + systemic adverse effet 7 Adrenaline | Epinephrine added for Long actionSKELETAL MUSCLE RELAXANTS CENTRAL > depress ens ABA, @® 7% dbIAZEPAm GABAR® > BECLOFEN 4O > TLZANLDINE PEREPHERAL DIRECTLY ACTING DANTROLENE Rynodine R # used For malignant hypermermia Neuroleptic malignant Syndrome Hepatotoxic NEURO MUSCULAR BLOCKER, [NMI 4] / INDIRECTLY ACTING DEPOLARTZENG MR sch > Shortest atking MR (<5 min? > cit in nerve & muscle inyories [ can corse Severe byperkalemia } > Hypermermia [predpttare molignont hyperthermia] lp FASCICULATLONS 7 responsible for post operative muscle pain Crost operotive muscle rigidity covSed by feNTANYL] Non! DEPOLARIZING / COMPETITIVE DETUBOCURARINE > do not cause post op. muscle poin > releaze Hictamtne > cause bronchocenstrickion 4+ep cuRLOM Crelease_lese histamine] CURONIUM [no histamine released] TRA CURLUM PAN CORONEUM cle -ATRA CURLUM, PPE, Miva cuRLUM [shortest acting] ve Ro RAPA HOFFMAN'S ELLMINATLON + Shown by Ptracurium §& Cis atracurium > MR oF choice in liver & Renal diseaseGENERAL ANAESTHETICS Iv / INDUCLNG AGENTS INHALATIONAL | MAINTAINANCE AGENTS Iv [ INDUCING AGENTS THLOPEN TONE PROPOFOL KeTAMINE ETOMLDATE THIOPENTONE, + highly lipid sotoble > very fast acting > very Short acking dit RentsrREBUTLON PROPOFOL, > poe for Day core bx > ongect® if poinfel DRDGS USED IN DAY CARE Sx Dr > pesrlpRANE. Manmohan 7? MIDAZOLAM singh > SEVOFLURANE 1s > LSOFLURANE a > ALFENTANIL Prime > PROPOFOL. Minister > mrvacurtom ETOMLDATE > couse Adrenal Supprestion KETAMINE, Kida Liv anossthetic agent of choice in children] Emergence reaction Thalamo - cortical gunckion Csite oF action] — brssoctarive ANESTHESIA analgesic Meals CFoll stomach] 7 BP] TOP/ ICP Civ anoxsthetic agent oF choice in Shock] NODA # Lovoided in Glaucoma & head ingury] Ercellent Bronchodilakor mz2"394m5% bhbubuagINHALATLONAL | MAINTAINANCE AGENTS ETHER inFla- CHLORO FORT mmable “) CNCLOPROPANE, TRILENE NETROVS OALDE, HALOTHANE, Non ~ ENFLURANE inFla- SEVOFLURANE mmable | so PLURANE DESFLURANE. METHOXY FLURANE, XENON, Mac [minimum Alveolar Concertratton) > min. conc. In alveoli to produce anaectiecia > mac 'Ja POTENCY Highest MAC > Nad Llogx) Lowest. MAC > METHOXYFLURANE Binod SOLDETLLTY > Inversly proportional to Speed oF anaxcmesia > measured by Blood + Gas Partition co -eFFicient > highest 3 memoxy Florane > Lowest > xenone > DesFlurane BOYLE%s MACHINE > 4 pressure oF anausthesio machine > sneery measures 4. Colour CODING Nad > ble NeELA cydo propane > orange SANTRE Oa > Entonox CHO+0,] > 507. 507. 2. PIN TNDEX SYSTEM air 245 Or aes Ngo 355 Coy > 457. 1:6 Coy < 7-57. a. ‘cyclopropane 36 Entonox xXENON > closest to IDEAL ANESTHETIC AGENT ~ Bnecthetic — Bnalgesic - MR Fastest acting SoFe SmMoOOT induct” & recovery > costiyCHELATING RENTS > UGed For heavy metol polsoning BAL CBritish Anti Lewisite] | OLMERCAPROL vses 8 > Bismorj poisoning 8 > Presence polsoning L > Least portoning ct cadmium poisoning Fe — poitoning Ca Na, EoTA vses M 7% Manganese poisoning 1 Lron poisoning L > Lead poisoning K 7 Cadmium poisoning d - PENTCELLAMINE vses > Cu poisoning [wilson digease J Fe chelating agents DESFERIOKAMINE > ingeckable , Used for atule Sron poisoning DE FERT PLRONE, 7% oral » used for Chronic Sron overload