Cholinergic Drugs

nohewipo's version from 2015-12-15 00:37


Question Answer
BethanecholDIRECT cholinomimetic, activates bowel and bladder, is resistand to AChE, indication is for post-op and neurogenic ileus and urinary retention
CarbacholDIRECT cholinomimetic, lowers intraoccular pressure in treatment of glaucoma by binding M3 Receptor and causing miosis
PilocarpineDIRECT cholinomimetic; binds M3 R to contract the ciliary muscle (open angle to allow fluid draining through the canal a Schlemn); contracts pupillary constrictor (miosis), and stimulates tears and salive; used to tx glaucoma and xerostomia (dry mouth) as the result of radiotherapy, resistant to AChE
MethacholineDIRECT cholinomimetic, used for the Methacholing Asthma Challange test (for airway hyperreactivity), stimulates M3 R to cause bronchorestriction
Direct Cholinomimetic AgentsBCPM, Bethanechol-Carbachol-Pilocarpine-Methacholine
Indirect Cholinomimetic AgentsNPEPE, Neostigmine-Pyridostigmine-Edrophonium-Physostigmine-Echotiophate; all are Cholinesterase Inhibitors = increases endogenous ACh, none penetrate the Blood/Brain Barrier except Physostigmine
NeostigmineINDIRECT cholinomimetic; tx of Myasthenia Gravis, post-op bladder and bowel retention, and NMJ blockade after surgery; inhibits AChE
PyridostigmineINDIRECT cholinomimetic; long acting TX of Myasthenia Gravis; inhibits AChE
EdrophoniumINDIRECT cholinomimetic; DIAGNOSIS Myasthenia Gravis (it is extremely short acting); inhibits AChE
PhysostigmineINDIRECT cholinomimetic; CROSSES THE BLOOD/BRAIN BARRIER; used for tx of Glaucoma and Atropine/Diphenhydramine/belladonna overdoses/poisoning
EchothiophateINDIRECT cholinomimetic; tx of glaucoma
Hemicholiniumblocks Choline reuptake by inhibiting the Na+-dependent Choline Transporter at cholinergic presynaptic nerve terminal
Vesamicolblocks ACh sequestration into vesicles by inhibiting the ATP-dependant Vesicular Transporter
Botulinuminhibits ACh release by degrading membrane proteins (VAMPs and SNAPs) that are required for Vesicle/Membrane fusion
M1 Receptorworks through Gq subunit of G-protein to signal in the CNS and Enteric Nervous Systems
M2 Receptorworks through the Gi subunit of G-protein to decrease heart rate and contractility of Atra
M3 Receptorworks through the Gq subunit of G-protein (adenylate cyclase-->cAMP-->protein kinase A) to cause bronchoconstriction, pupillary sphincter contraction, ciliary muscle contraction during accomodation, gut peristalsis, bladder contraction, exocrine gland secretion
Acetylcholinesterase Inhibitor poisoningDUMBLESS (Defication Urination Miosis Bronchospasm Lacrimation Excitation--skeletal muscle + CNS-- Salivation Sweating) poisoning could be caused by excess AChE meds, pesticides/chemical weapons (commonly of the Organophosphare class--ex. Parathion) Tx = Atropine + Pralidoxime (reverses muscle paralysis and SLUD/DUMBLESS sx of organophosphate/AChE-I poisoning by attaching to the AChE-I and removing it from AChE--this is the regeneration of the inactive enzyme)
Pralidoximereverses muscle paralysis and SLUD/DUMBLESS sx of organophosphate/AChE-I poisoning by attaching to the AChE-I and removing it from AChE--this is the regeneration of the inactive enzyme; used in conjunction with Atropine
Cholinergic AntagonistsMUSCARINIC (Eye-atropine, homotropine, tropicamide; CNS- benztropine, scopolamine; Resp- ipratropium; GU- oxybutynin, glycopryyolate; GI- methscopolamine, pirenzepine, propantheline) NICOTINIC (Hexamethonium)
Cholinergic AgonistsDIRECT (Bethanechol, Carbachol, Pilocarpine, Methacholine) INDIRECT aka AChE-Is (Neostigmine, Pyridostigmine, Edrophonium, Physostigmine, Echothiophate)
AtropineMuscarinic Antagonist, used in Tx of AChE-I toxicity Organophosphate poisoning, Tox = hyperthermia in infants, acute angle-closure glaucoma in elderly, urinary retention in men with BPH (increase temp, rapid pulse, dry mouth, flushing, constipation, disorientation, cycloplegia--paralysis of ciliary muscle and loss of accomodation)
Homatropine/TropicamineMuscarinic Antagonist that works in the EYE, produces Mydriasis and cycloplegia
BenztropineMuscarinic Antagonist that works in the CNS, Tx of Parkinson's Dz by decreasing the excess ACh seen in the dz to reduce tremor and rigidity
ScopolamineMuscarinic Antagonist that works in the CNS, tx of motion sickness by inducing drowsiness/CNS depression/fatigue
IpratropiumMuscarinic Antagonist that works in the Resp. System, Tx of Asthma and COPD by inhibiting the bronchospasm caused by binding of M3 Rs/causing bronchodilation ORAL INHALERFORM...relief of rhinorrhea by inhibiting M3 R stimulation of mucous secreting glands NASAL SPRAY FORM
OxybutyninMuscarinic Antagonist that works in the GU system, reduces urgency caused my mild cyctitis and inhibits bladder spasm (alt. drug Glycopyrrolate)
MethscopolamineMuscarinic Antagonist that works in the GI system, tx or Peptic Ulcer Disease by reducing the amount of HCl in gastric secretions (alt. drugs Pirenzepine/Propanthelin)
HexamethoniumNICOTINIC antagonist, used in pharmacologic and physiologic research/experimental models as a GANGLIONIC BLOCKER (nicotinic ACh Rs are found in preganglionic synapses and in the NMJ) to inhibit ALL AUTONOMIC OUTFLOW