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level: Level 2

Questions and Answers List

Direct-Acting Cholinergic Agonists

level questions: Level 2

Question	Answer
• a quaternary ammonium compound that cannot penetrate membranes • Effects: – decrease in heart rate and cardiac output – decrease in blood pressure – DUMBELS – 1% solution - for ophthalmic surgery	ACETYLCHOLINE • Miochol-e®
• Actions: Causes increased secretion, smooth muscle contraction (except vascular smooth muscle - relaxes), and changes in heart rate • CA: Postoperative nonobstructive urinary retention, neurogenic ileus and megacolon • S/E: Generalized cholinergic stimulation (sweating, salivation, flushing, decreased blood pressure, nausea, abdominal pain, diarrhea, bronchospasm)	BETANECHOL • Urecholine®
Antidote for Betanechol & Pilocarpine	Atropine
• Actions: similar to betanechol • CA: used topically almost exclusively for GLAUCOMA	Carbachol • Carboptic®, Miostat®, Carbastat®
• Actions: effects are similar to betanechol; produces rapid miosis; potent stimulators of secretions • CA: GLAUCOMA, SJORGEN'S SYNDROME • S/E: blurred vision, night blindness, brow ache, exaggeration of various parasympathetic actions • Antidote: Atropine DRUG OF CHOICE for emergency lowering of INTRAOCULAR PRESSURE	PILOCARPINE • Isopto Carpine®
• Synthetic • Similar to pilocarpine	Cevimeline • Evoxac®
• Activates autonomic postganglionic neurons and skeletal muscle neuromuscular end plates • CA: medical use in smoking cessation • S/E: Nausea & Vomiting, Increased BP, Long term GI and Cardiovascular risk factor • Interaction: Additive to CNS stimulant	Nicotine
Inhibits Acetylcholinesterase for degradation	Indirect-Acting Cholinomimetics
3 Chemical Groups of Cholinesterase Inhibitors	1 Simple alcohols bearing a quaternary ammonium group 2 Carbamic acid esters of alcohols having quaternary or tertiary ammonium groups 3 Organic derivatives of phosphoric acid
ORGANOPHOSPHATES 1 has a clinical value 2 an extremely potent "nerve gas" 3 (sulfur-containing phosphate) prodrugs that are converted to phosphate derivatives in animals and plants and used as insecticide	1 Echothiophate 2 Soman 3 Parathion & Malathion
MOA of ORGANOPHOSPHATE	Increase the concentration of Endogenous Acetylcholine at Cholinoreceptors by inhibiting acetylcholinesterase enzyme
"irreversible" cholinesterase inhibitor	Organophosphates
"reversible" cholinesterase inhibitor	Edrophonium and Carbamates
a disease characterized by increased INTRAOCULAR PRESSURE	Glaucoma
a medical emergency that is frequently treated initially with drugs but usually requires surgery for permanent correction	Acute angle-closure glaucoma
(strabismus caused by hypermetropic accomodative error)	Accomodative esotropia
paralysis of the stomach or bowel following surgical manipulation	Postoperative atony
• Neuromuscular Junction • Curare-induced neuromuscular paralysis	Myasthenia gravis
was used to treat supraventricular tachyarrhythmias	Edrophonium
drug with anticholinesterase and other cholinomimetic actions used for the treatment of mild to moderate Alzheimer's disease (Deficiency of Cholinergic Neurons / Ach)	TACRINE (Cognex)
• MOA: Binds briefly to active site of AChE and prevents access of ACh • Effects: Amplifies all actions of ACh (increases parasympathetic activity and somatic neuromuscular transmission) • CA: Diagnosis and acute treatment of myasthenia gravis • Toxicity: Parasympathomimetic excess	EDROPHONIUM • Tensilon®
• an autoimmune disease affecting skeletal muscle neuromuscular junctions • S/Sx: ptosis, diplopia, difficulty in swallowing and extremity weakness	Myasthenia Gravis
DIAGNOSIS OF Myasthenia Gravis	• 2 mg of Edrophonium given IV after baseline muscle strength is measured • if no reaction occurs after 45 sec, an additional 8 mg may be injected • POSITIVE RESULT = the patient has improvement in muscle strength that lasts for 5 minutes
• Like neostigmine, but longer-acting • also used in myasthenia gravis Short-Acting Cholinesterase Inhibitor	AMBENONIUM • Mytelase®