ANDRENERGIC CHOLINERGIC
Direct Acting Agents
Nonselective Alpha & Beta Nonselective mAChR & nAChR
Agonist Antagonist Agonist Antagonist
Epinephrine ( α) Carvedilol ( 1, 2, α1)* Carbachol
Levophed/NE (not 2s) Labetalol ( 1, 2, α1)
Dopamine (D1 1 α)
Ephedrine/Pseudoephedrine (all)
Nonselective Beta Nonselective mAChR
Nonselective Alpha
1 Gs AC cAMP M1 Gq DAG & IP3 ↑Ca2+
Agonist Antagonist Agonist Antagonist Neuronal CNS & presynaptic ANS
Oxymetazoline Phenoxybenzamine Isoproterenol Propranolol M2 Gi ↓cAMP ↓Ca2+ in, ↑K+ out
(only PNS α2 ) (irreversible) Nadolol, Timolol Heart: ↓Contractility & ↓HR
Phentolamine Pindolol, Carteolol M3 Gq DAG & IP3 ↑Ca2+
(reversible) (partial) ↑Secretions (bronchial, sweat, salivary, gastric acid)
eNOS →↑NO ↑cGMP (SM) vasodilation
Selective Alpha 1 Selective Beta 1 Agonist Antagonist
α1 Gq IP3 & DAG ↑Ca2+ from ER 1 Gs cAMP PKA Troponin I / ↑Ca Bethanechol Atropine, Scopolamine
Smooth Muscle Contraction Heart: ↑Contractility & ↑HR Pilocarpine Glycopyrrolate, Oxybutynin
(vascular, GI, GU, sphincters, pupillary dilator) Kidney: renin release Adipose: ↑lipolysis Cevimeline Ipratropium, Tiotropium (Quaternary)
Agonist
Antagonist
Agonist Ca di Antagonist
Phenylephrine Dobutamine Atenolol Selective ANS Ganglion nAChR
Prazosin
Methoxamine Metoprolol* Agonist Antagonist
Terazosin
Tetrahydrozoline Esmolol, Betaxol Nicotine Trimetaphan
Doxazosin
Naphazoline Acetabutalol (partial) Chantix/Varenicline (partial) Hexamethonium
Tamsulosin
Pseudoephedrine
Selective Alpha 2 Selective Beta 2
α2 Gi ↓cAMP ↑Ca2+ influx from ECF 2 Gs cAMP PKA → MLCK
Smooth Muscle Contraction (vascular) SM relaxation (bronchial, GI, GU, ciliary)
Platelet aggregation Aqueous humor production
↓Insulin secretion, ↓Lipolysis ↑K+ uptake by skeletal m. Selective NMJ nAChR
↓SNS outflow from CNS ↑Insulin, ↑Glucose from liver, ↑Lipolysis
Agonist Antagonist Agonist Antagonist Agonist Antagonist
Clonidine (CNS) Mirtazapine Albuterol Levobunolol Succinylcholine Tubocurarine
Methyldopa Bitolterol Timolol Pancuronium
(partial CNS) Metaproterenol Mivacurium
Terbutaline
Isoetharine
Ritodrine (uterus)
Indirect Acting Agents
Pre-Synaptic Effects on NE
Pre-Synaptic Effects on ACh
Metyrosine - ↓Tyrosine DOPA conversion
Hemicholinium - ↓Choline uptake (Na+ transporter)
Reserpine - ↓ DA NE conversion/vesicular loading
Vesamicol - ↓vesicular Ach transporter (H+ antiporter)
Guanethidine - ↓NE release
Botulinum - ↓ACh release
Cocaine/Amphetamines/TCAs - ↓NE reuptake
α-Latrotoxin (Black Widow Spider) - ↑↑ACh release
Tyramine, (Pseudo)Ephedrine, Amphetamines ↑NE release
AChE Inhibitors
MOA Inhibitors- ↓NE breakdown
Endrophonium short-acting/ noncovalent
Pargyline
Physostigmine (CNS), Neostigmine (PNS), Pyridostigmine (PNS) carbamates/reversible
Tranylcypromine
Malathion/Parathion/Diazinon, Sarin/Soman/Tabun - organophosphates/irreversible
Drug Antidotes
K ha he OD ed a ie i look like
Atropine (mAChR antagonist) Physostigmine (AChE inhibitor than can cross BBB)
Curare-like drugs (NMJ nAChR antagonists) Neostigmine/Pyridostigmine (AChE inhibitors that stay in PNS)
Succinylcholine (NMJ nAChR agonist) Ventilation/Time (ca b ed i h he stigmines b/c i a -competitive agonist)
Carbamate (AChE Inhibitor) Atropine (mAChR agonist) & Curare-like drug (nAChR agonist)
Organophosphate (AChE Inh.) Atropine + Pralidoximine (dephosphoryles/regenerates active AChE) + Diazepam (↓seizures/conclusion) + Respirator
Heparin Protamine Sulfate (binds to inactivate anti-coag ability, limited effectiveness on LMW Heparin)
Warfarin Vitamin K (phytonadione)
Thrombolytics Aminocaproic acid (inhibits conversion of plasminogen to plasmin)
Memory Tricks
-stigmine = reversible AChE inhibitors (carbamate) (Tx for Myasthenia Gravis)
o Oh, it may sting when your car-mate kicks you to the curb but at least you can still walk h e
Endrophonium = short-acting AChE inhibitor Chec i g if M a he ia G a i a ie a e h ie
Me = ganglionic nAChR inhibitors M BP c e ed he I met a gang used for life threatening HTN
C = NMJ nAChR inhibitors U ed a a ea a cure (i.e. in surgery) used with anesthesia to promote muscle relaxation
-i = ACh stuff
Z = α1 acting drugs Z li e = ag i , Z i = a ag i
Ritodrine = 2 agonist for uterine relaxation (prevents premature delivery) Righ he d ai
B a = agonists (Iso = both, Do = 1, Ter = 2)
-erol, -e l = 2 agonist
-blockers = -l l
o Can you, Please Try Not Picking = N e ec i e selective
o A BEAM targets the heart = Cardioselective 1 (good for asthmatics)
o l l ha a e l l =N e ec i e -blockers + α1 blocker (vasodilatory)
o My Top Carvers in remodeling the heart = B-Arrestin signaling (Metoprolol & Carvedilol)
clop = ADP ece a i-platelets (a i e c )
- la e = Di ec ed Th b ic (g a he igh ace a a only site of the thrombi) = Altelplase, Reteplase, Tenecteplase
a a = Vasopressin antagonist
The Queen Proclaims Dis Pyramid = Class IA antiarrythmics (Quinidine, Procainamide, Dispyramide
Phendy Liddle Mexican Tac = Class IB antiarrythmics (Phenytoin, Lidocaine, Mexiletene, Tocainide)
I C the propane flecks = Class IC antiarrythmics (Propafenone, Flecainimide)
Kinky Ami sorta lied about her AIDS = Class III antiarrythmics (K+ channel blockers - Amiodarone, sotalol, dofetilide, ibutilide)
Call Veron for Nifty Dil ic e = Class IV antiarrythmics (Ca2+ channel blockers Verapamil, Nifedipine, Diltiazem, Bepridil)
o N & B = Not Blocking the AV node
Be ha , ca e ac i a e b adde /b e (post-op) = Bethanecol (mAChR agonist)
Carbon copy of Ach = Carbachol (mAChR & nAChR agonist)
Sweat, Cry & Drool on you Pillo = Pilocarpine (mAChR agonist → g a c a, Sj g e )
