| Pilocarpine| ~~ | Carbachol | Arecoline | Bethanechol |Classification Directly acting Choline esters * Acetylcholine + Bethanechol * Carbachol Reversible Carbamates Alcohol * Physostigmine « Edrophonium + Neostigmine « Pyridostigmine « Rivastigmine Cholinergic agonists Alkaloids * Pilocarpine « Muscarine Others + Donepezil Galantamine ° Tacrine y Indirectly acting (anticholinesterases) vy Irreversible Organophosphorus (OP) Carbamates compounds « Propoxur « Parathion + Carbaryl * Malathion Sarin, soman, tabun (nerve gases) * Dyflos * EchothiophateTable 9.1: Difforenc een @ B B52 NAD: 1. Rank order of potency of agonists “Adr > NA> Iso Iso > Adr > NA ‘ 2. Antagonist (Phentolamine! * Propranolol * 3. Coupling protein Gq/GiGo IO -G Gs 4. Effector pathway | IP{DAGT, cAMP J, K¢channel t___¢AMP?, Ca’ channel t ec ough inherently NA is equipotent to Ar on a receptors, in test aystoms with intact neuronal reuptake, it appears less potent due to faster reuptake. On the basis of relative organ specificity induce thermogenesis. 'S of selective agonists and antagonists, the B been investigated as. receptors were further subdivided into, ind location of B, receptors is on detrusor muscle @) subtypes. Later(B (atypical B) receptors of urinary Bladder; activation causing relaxation, Were described which are more sensitive to A relatively: selec ‘mirabegron NA than to Adr, and have very low affinity been recently found useful in th Symptomatic for the classical B~blockers. The| receptors. treatment of overactive bladder by relaxing the are located on adipocytes, ind detrusor muscle alee BS By 2 @ronchi(bloog> Adipose tissue, (vessels, uterus, liver, Detrusor muscle of i i ‘, urinary tract, eye bladder 1. Location 2. Selective agonist Mirabegron “ 3. Selective antagonist Icl 118551 ‘OGP 20712A (also f,) a-methyl propranolol ICl 118551 (also B,) 4 Relative potency of NA and Adr° Adr2 NA Adr >> NA NA> Adr‘Dastiunctional in brain, pancreatic B cells and ‘extrajunctional in certain blood vessels, platelets GU Smooth muscle-contraction _ Inhibition of transmitter release Location -Postjunctional o ‘Prejunctional on nerve ending (c.,,), also Function subserved Vasoconstriction Vasoconstriction ~ Gland—secretion — Decreased central sympathetic flow {Sut—relaxation Decreased insulin release J eye - py clXorty Platelet aggregation Selective agonist Phenylephrine Clonidine “Selective antagonist Prazosin _ Yohimbine, Rauwolscine Coupling protein Gq : GilGo spholipase A, TPG release channel Ca? channel,t.or t j IPJDAG t \ nNANTICHOLINERGIC DRUGS (Muscarinic antagonists, Atropinic drugs, Parasympatholytics) alkaloids Atropine methonitrate Homatropine Hyoscine butyl bromide Ipratropium bromide Tiotropium bromide Oxybutynin Flavoxate Tolterodine Darifenacin ° Solifenacin Trihexyphenidy! (Benzhexol) Procyclidine Biperiden Cyclopentolate Tropicamide Propantheline | Oxyphenonium | Clidinium | Cimetropium bromide Isopropamide GlycopyrrolateADRENERGIC DRUGS ‘(Sympathomimetics) | Bronchodilators "Noradrenaline | Isoprenaline Amphetamine | (Norepinephrine) | Salbutamol Dexamphetamine | “Tsoxsuprine | Ephedrine : | (Albuterol) Methamphetamine’ | Salbutamol | Dopamine | Terbutaline Methylphenidate | Terbutaline | Phenylephrine | Salmeterol | esreeeereeal Methoxamine | Formoterol Mephentermine Bambuterol "A ‘Ad renaline Isoprenaline Dobutamine Pas Xylometazoline Oxymetazoline Naphazoline Phenylephrine Pseudoephedrine ‘Amphetamine Fenfluramine Sibutramine __& ADRENERGIC BLOCKING DRUGS Nonequilibrium type ium type B-haloalkylamine | Prazosin | Yohimbine Terazosin Doxazosin. Alfuzosin Tamsulosin Silodosin Ergot alkaloids 'Ergotamine ‘Ergotoxine f Dmyaceigoenie EE | | Dihydroergotoxine (Codergocrine)ANTIADRENERGIC DRUGS AND.DRUGS FOR GLAUCOMA aa TOPICAL DRUGS FOR GLAUCOMA | Physostigmine Timolol ‘ Latanoprost Dorzolamide Betaxolol | i Travoprost Brinzolamidé ~~~ Echothiophate Levobunolol i idi Bimatoprost CarteololTable 10.2: Comparati P~BLOCKER Potency (on B,) NONSELECTIVE - 1, Propranciol 1. 2. Sotalol se Stock 6. 4. Pindoll 6 CARDIOSELECTIVE 1. Metoprolol 1 | 2. Atenolol - A 3.-Acebutolol — 1/3B ADRENERGIC BLOCKING DRUGS Gaeieeucn() Metoprolol Atenolol Acebutolol Bisoprolol Esmolol Betaxolol Celiprolol Nebivolol ....- Tabetalol Carvedilol sympathomimetic activity GENERATION-WISE CLASSIFICATION B ADRENERGIC BLOCKING DRUGS | Metoprolol Timolol | Atenolol Sotalol Acebutolol Carvedilol Pindolol _ | Bisoprolol Celiprolol : Esmolol Nebivolol BetaxololDIURETICS High ceiling Medium efficacy (Inhibitors of (Inhibitors of E Weak/adjunctive diuretics Bumetanide | Torasemide ‘Other high ceiling diuretics, viz. ethacrynic acid and organomercurials (mersalyl) are ‘only historical. Metolazone Xipamide Indapamide ClopamideANTIDIURETICS Thiazides _ Vasopressin (ADH) Amiloride | Chlorpropamide _Desmopressin Indomethacin _ Lypressin seni _ TerlipressinCOAGULANTS ee, Adrenochrome mono- semicarbazone | Ethamsylate RutinANTICOAGULANTS Oral anticoagulants Parenteral anticoagulants Heparin (unfractionated) - Rivaroxaban | | Dabigatran- Low molecular weight Bivalirudin (dicumarol) ~~ Apixaban etexilate heparins Argatroban | | Warfarin sod. ~ (Enoxaparin, Reviparin, Acenocoumarol Y Nadroparin, Dalteparin, (Nicoumalone) Parnaparin, Ardeparin) Ethyl-biscoum- Fondaparinux acetate | DanaparoidANTIPLATELET DRUGS (Antithrombotic drugs) Ticlopidine Clopidogrel Eptifibatide Prasugrel Tirofiban TicagrelorSummary of mechanism of action of anticoagulants Anticoagulant S| Mechanism of action Clotting factors affected | Heparin (parenteral) Activates AT Ill and forms Inactivates factors lla, Xa, sl heparin—AT Ill complex Xa, Xla, Xlla, Xllla et LMWH (parenteral) LMWH-AT III complex Inactivates factor Xa Fondaparinux (parenteral) Fondaparinux-AT III Inactivates factor Xa : complex Bivalirudin, argatroban itors of Thrombin (parenteral) thrombin Dabigatran (oral) Direct inhibitor of thrombin Thrombin Rivaroxaban, apixaban (oral) | Direct inh n of Xa Xa Warfarin (oral) Inhibits vitamin K epoxide reductase Inhibits synthesis of clotting factors Il, Vl, IX, X AT Ill, antithrombin II LMWH, Jow-molecular-weight heparin.HYPOLIPIDAEMIC DRUGS Lovastatin gonists Gemfibrozil | Simvastatin Pravastatin Bezafibrate Atorvastatin Fenofibrate _ Rosuvastatin Pitavastatin Cholestyramine _ Colestipol | Colesevelam Nicotinic acidANTIHYPERTENSIVE DRUGS (1) Pees ReaIeantseen en SMe system inhibitors Haine ears Hydrochlorothiazide | Chlorthalidone Furosemide Propranolol Metoprolol Atenolol (others) Labetalol Carvedilol | Captopril | Enalapril LB Tried e de - ot | Laer Valances Prazosin Clonidine Ramipril Telmisartan nee baled Fosinopril Irbesartan Phentolamnine | Quinapril ‘Olmesartan Trandolapril > ANTIHYPERTENSIVE DRUGS (2) ARs Calcium channel blockers Verapamil Felodipine Amlodipine Nitroprusside sod.ANTIANGINAL DRUGS Other antianginal drugs Nicorandil | | Trimetazidine | Ranolazine Ivabradine Dipyridamole Pot. channel opener. Calcium channel blockers Nitrates B-blockers Verapamil Diltiazem Amlodipine (others) Propranolol Metoprolol Atenolol (others) | dinitrate | (oral) | Isosorbide mononitrate Erythrityl tetranitrate Pentaerythritol tetranitrate Jsosorbide | dinitrate | (sublingual) th \ My Cop") | |Antiarrhythmic drugs Class | Membrane stabilizing agents teri eat blockers | Lidocaine Propafenone | Mexiletine Flecainide | Procainamide Disopyramide | y 1 Agents widening action potential ooo X | Amiodarone ut at fee |Dronedarone agents |Sotalol (class II | | as welt) lit Propranolol |Dofetilide Esmolol \Ibutilide PSVT: Paroxysmal supraventricular tachycardia