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cholinomimeticsdrugs
cholinomimetics drugs
| question | Answer |
|---|---|
| direct acting cholinoceptor stimulants | Acetylcholine, bethanechol, pilocarpine, cevimeline, varenicline |
| Indirect-acting cholinomimetics | neostigmine, physostigmine, pyridostigmine, ambenonium, demecarium, edrophonium, tacrine, donepezil, galantamine, rivastigmine, echothiophate, parathion, malathion, sarin, soman |
| AchE regenerator | Pralidoxime(PAM) |
| Inhibitors of synaptic vesicle function | Botulinum Toxin |
| ACH MOA | Activates Muscarinic and Nicotinic cholinergic receptors. Facilitates both parasympathetic (Muscarinic and Nicotinic) and sympathetic (Nicotinic ganglionic) transmission |
| ACH kinetics | Short half life. Rapidly metabolized by AChE (5-20sec) Poor oral absorption (quaternary amine). Given IV |
| ACH toxicity and uses | toxicity: autonomic excess uses: gluacoma |
| Bethanechol, pilocarpine, cevimeline MOA | Muscarinic receptor specific. Increases parasympathetic activity |
| bethanechol kinetics | quaternary amine, oral or SC |
| Bethanechol clinical uses | Treats various GI disorders postoperative and neurogenic ileus, Urinary retention. Activates bowel and bladder smooth muscle |
| Bethanechol, pilocarpine, cevimeline, carbachol toxicity | Muscarinic excess, so symptoms of sweating, bradycardia, increased bowel activity, urination, blurred vision, miosis, etc. |
| pilocarpine kinetics | tertiary amine |
| pilocarpine clinical use | glaucoma. See explanation with Carbachol, Sjogren's Disease (autonimmune distruction of secretory glands) |
| cevimeline kinetics | oral |
| cevmeline clinical use | Dry mouth from Sjögren syndrome (oral) |
| carbachol MOA | Muscarinic and Nicotinic receptor activation |
| carbachol kinetics | quaternary amine |
| carbachol clinical use | glaucoma (ophthalmic solution and drops). Works by activating ciliary muscle of eye –opens canal of Schlemm (open angle) pupillary sphincter (narrow angle) |
| varenicline MOA | partial agonist to CNS a4,b2 type Nicotinic receptor |
| varenicline kinetics | tertiary amine |
| varenicline clinical use | smoking cessation treatment |
| varenicline toxicity | nausea, headache, sleep disturbances, neuropsychiatric effects (mood changes, suicidal ideations, etc.) |
| neostigmine, physostigmine, pyridostigmine, ambenonium, denecarium, Edrophonium, tacrine, donepezil, galantamine, rivastigmine MOA | Reversible AChE inhibitor, produce increase in synaptic released Ach which can activate its post-synaptic receptors |
| neostigmine kinetics | Oral or parenteral, half life .5-2 hrs, duration of action medium |
| neostigmine clinical uses | Myasthenia Gravis, paralytic ileus, urinary bladder atony |
| neostigmine, physostigmine, pyridostigmine, ambenonium, demecarium, edrophonium, tacrine, donepezil, galantamine, rivastigmine, echothiophate, parathion, malathion, sarin, soman TOXICITY | DUMBBELSS, diarrhea, urination, miosis, bronchospasm, bradycardia, Excitation, lacrimation, sweating, salivation |
| Physostigmine Kinetics | ophthalmic or parenteral, half life .5-2 hrs (medium duration), tertiary amine, distributed throughout body, absorbed through skin |
| Physostigmine clinical uses | atropine poisoning (IM or slow IV), glaucoma (ophthalmic ointment) |
| pyridostigmine kinetics | oral or parenteral, half life 3-6 hours |
| pyridostigmine, Ambenonium clinical uses | Myasthenia Gravis |
| ambenonium kinetics | Oral, half life 4-8 hours, quaternary amine |
| Demecarium Kinetics | ophthalmic, half life 4-6 hours, quaternary amine |
| Demecarium clinical uses | Glaucoma (Opthalmic drop) |
| Edrophonium kinetics | Parenteral, short duration (minutes) quaternary amine |
| Edrophonium clinical uses | test for Myasthenia Gravis |
| Tacrine, Donepezil, Galantamine, Rivastigmine Kinetics | Oral, tertiary amines |
| Tacrine, Donepezil, Galantamine, Rivastigmine Clinical uses | Help with cognitive dysfunction of Alzheimer's |
| Echothiophate, parathion, malathion, sarin, soman MOA | organophosphate, irreversible inhibitor of AChE, Activation of Nicotinic and Muscarinic receptors via Ach increase |
| Echothiphate kinetics | Ophthalmic powder, long duration 100 hours, quaternary amine |
| Echothiophate clinical uses | glaucoma (opthalmic powder) |
| Parathion and malathion kinetics and clinical uses | Insecticide |
| Sarin and soman kinetics and clinical uses | nerve toxin- excitotoxcity and death |
| Pralidoxime (PAM) | MOA:displaces organophosphates from AChE active site, prevents aging kinetics: given withen 48 hours until symptoms abate (days) |
| pralidoxime clinical doses | Clinical uses:severe organophosphate insecticide poisoning in which respiratory depression, muscle weakness, and/or twitching are severe.(given early approx 48 hour window) |
| Pralidoxime toxicity | CV: tachycardia, hypertension, pain on injection, Muscle rigidity, weakness, transient increases in ALT and AST, Rash, nausea, dizziness, headache, decreased renal function |
| Botulinum toxin | MOA:cleaves synaptic vesicle protein synaptobrevin preventing docking and fusion of acetylcholine vesicles kinetics:injected locally clinical uses and toxicity: nerve paralysis |
Created by:
925love
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