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level: Level 2

Questions and Answers List

Direct-Acting Cholinergic Agonists

level questions: Level 2

QuestionAnswer
• 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 surgeryACETYLCHOLINE • 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 & PilocarpineAtropine
• Actions: similar to betanechol • CA: used topically almost exclusively for GLAUCOMACarbachol • 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 PRESSUREPILOCARPINE • Isopto Carpine®
• Synthetic • Similar to pilocarpineCevimeline • 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 stimulantNicotine
Inhibits Acetylcholinesterase for degradationIndirect-Acting Cholinomimetics
3 Chemical Groups of Cholinesterase Inhibitors1 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 insecticide1 Echothiophate 2 Soman 3 Parathion & Malathion
MOA of ORGANOPHOSPHATEIncrease the concentration of Endogenous Acetylcholine at Cholinoreceptors by inhibiting acetylcholinesterase enzyme
"irreversible" cholinesterase inhibitorOrganophosphates
"reversible" cholinesterase inhibitorEdrophonium and Carbamates
a disease characterized by increased INTRAOCULAR PRESSUREGlaucoma
a medical emergency that is frequently treated initially with drugs but usually requires surgery for permanent correctionAcute angle-closure glaucoma
(strabismus caused by hypermetropic accomodative error)Accomodative esotropia
paralysis of the stomach or bowel following surgical manipulationPostoperative atony
• Neuromuscular Junction • Curare-induced neuromuscular paralysisMyasthenia gravis
was used to treat supraventricular tachyarrhythmiasEdrophonium
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 excessEDROPHONIUM • Tensilon®
• an autoimmune disease affecting skeletal muscle neuromuscular junctions • S/Sx: ptosis, diplopia, difficulty in swallowing and extremity weaknessMyasthenia 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 InhibitorAMBENONIUM • Mytelase®