Term
| Name 2 direct acting choline esters. |
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Definition
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Term
| bethanechol, carbachol are which type of drugs? |
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Definition
| direct acting choline esters |
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Term
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Definition
| muscarinic agonist, negligible effect at nicotinic recepts |
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Term
| Which drug is a muscarinic agonist, with negligible effect at nicotinic receptors? |
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Definition
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Term
| What are the effects of bethanechol? |
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Definition
| activates M1 - M3 receptors in all peripheral tissues, increased secretion, smooth muscle contraction (except vascular smooth muscle, which relaxes), and changes in heart rate |
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Term
| clinical applications for bethanechol? |
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Definition
| postop and neurogenic ileus and urinary retention |
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Term
| How is bethanechol given? What is its duration? Does it enter the CNS? |
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Definition
| oral or parenteral, 30 min, no it does not enter the CNS |
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Term
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Definition
| excessive parasympathomimetic effects, especially bronchospasm in asthmatics, interactions - additive with other parasympathomimetics |
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Term
| Name a nonselective muscarinic and nicotonic agonist. What is it used for? |
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Definition
| carbachol, used topically almost exclusively for glaucoma |
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Term
| Name the direct acting muscarinic alkaloids or synthetics |
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Definition
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Term
| What are pilocarpine and cevimeline? |
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Definition
| direct acting muscarinic alkaloid and synthetic |
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Term
| What is the MOA of pilocarpine? |
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Definition
| muscarinic partial agonist |
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Term
| What are the effects of pilocarpine? |
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Definition
| activates M1 - M3 receptors in all peripheral tissues, increased secretion, smooth muscle contraction (except vascular smooth muscle, which relaxes), and changes in heart rate |
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Term
| What are the clinical applications for pilocarpine? |
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Definition
| glaucoma, sjogren's syndrome |
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Term
| Which drug is used for glaucoma and sjogren's syndrome? |
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Definition
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Term
| How is pilocarpine given? Toxicity? |
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Definition
| oral lozenge and topical, excessive parasympathomimetic effects, especially bronchospasm in asthmatics, interactions - additive with other parasympathomimetics |
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Term
| Which drug is used as an oral lozenge and topically? |
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Definition
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Term
| Cevimeline is selective for which receptor? |
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Definition
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Term
| The effects of cevimeline are similar to which other drug? |
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Definition
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Term
| Which M receptors use Gq -> IP3 and the DAG cascade? |
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Definition
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Term
| Which M receptors use Gi -> inhibition of cAMP production, activation of K+ channels? |
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Definition
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Term
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Definition
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Term
| Which M receptor is present only on nerves? |
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Definition
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Term
| Where is the M2 receptor located? |
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Definition
| heart, nerves, smooth muscle |
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Term
| Which M receptor is present on heart, nerves and smooth muscle? |
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Definition
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Term
| Where is the M3 receptor located? |
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Definition
| glands, smooth muscle, endothelium |
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Term
| Which receptor is present on glands, smooth muscle and endothelium? |
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Definition
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Term
| M4 and M5 are present where? |
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Definition
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Term
| Which M receptors are present in the CNS? |
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Definition
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Term
| Name the direct acting nicotinic agonists |
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Definition
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Term
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Definition
| direct acting nicotinic agonist at both Nn and Nm receptors |
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Term
| How do the nicotinic receptors work? |
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Definition
| Na+, K+ depolarizing ion channel |
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Term
| What are the effects of nicotine? |
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Definition
| activates autonomic postganglionic neurons (both sym and parasym) and skeletal muscle neuromuscular end plates, enters CNS and activates Nn receptors |
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Term
| which drug activates autonomic postganglionic neurons (both sym and parasym) and skeletal muscle neuromuscular end plates, enters CNS and activates Nn receptors? |
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Definition
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Term
| clinical applications for nicotine? |
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Definition
| medical use in smoking cessation, nonmedical use in smoking and in insecticides |
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Term
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Definition
| increased GI activity, nausea, vomiting, diarrhea acutely, increased BP, high doses cause seizures, long term GI and CV risk factors, additive with CNS stimulants |
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Term
| Which drug causes increased GI activity, nausea, vomiting, diarrhea acutely, increased BP, high doses cause seizures, long term GI and CV risk factors, and is additive with CNS stimulants? |
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Definition
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Term
| What is the MOA of varencicline? |
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Definition
| selective partial agonist at a4b2 nicotinic recepts, used exclusively for smoking cessation |
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Term
| Name a short acting cholinesterase inhibitor |
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Definition
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Term
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Definition
| a short acting cholinesterase inhibitor |
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Term
| What type of chemical is edrophonium? What is the MOA of edrophonium? |
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Definition
| it's an alcohol, binds briefly to active site of AchE, and prevents access of Ach |
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Term
| Which drug binds briefly to active site of AchE, and prevents access of Ach? |
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Definition
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Term
|
Definition
| amplifies all actions of Ach, increases parasympathetic activity and somatic neuromuscular transmission |
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Term
| What is edrophonium used for? |
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Definition
| dx and acute tx of myasthenia gravis |
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Term
| What is used for the dx and acute tx of myasthenia gravis? |
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Definition
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Term
| How is edrophonium given? What kind of molecule is it? Does it enter the CNS? |
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Definition
| parenteral, quaternary amine, does NOT enter CNS |
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Term
| Name 3 quaternary amine drugs. Do they enter the CNS? |
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Definition
| edrophonium, neostigmine, pyridostigmine, NO does NOT enter CNS |
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Term
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Definition
| parasympathomimetic access, additive with other parasympathomimetics |
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Term
| Name an intermediate acting cholinesterase inhibitor |
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Definition
| neostigmine, pyridostigmine (longer acting), physostigmine |
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Term
|
Definition
| an intermediate-acting cholinesterase inhibitor |
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Term
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Definition
| forms covalent bond with AchE, but hydrolyzed and released |
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Term
| Which drug forms a covalent bond with AchE, but it is hydrolyzed and released? |
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Definition
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Term
| What is neostigmine used for? |
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Definition
| MG, postop and neurogenic ileus and urinary retention |
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Term
| Which drug is used for MG, postop and neurogenic ileus and urinary retention? |
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Definition
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Term
| How is neostigmine given? What type of amine is it? Does it enter the CNS? |
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Definition
| oral and parenteral, quaternary amine, NO it does NOT enter the CNS |
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Term
| How long does pyridostigmine act? What is it used for? |
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Definition
| 4-6 hrs, slightly longer than neostigmine, used for MG |
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Term
| What type of drug is physostigmine? What type of molecule is it? Does it enter the CNS? |
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Definition
| intermediate acting AchE inhibitor, natural alkaloid tertiary amine, YES it enters CNS |
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Term
| Name an intermediate acting AchE inhibitor that enters the CNS |
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Definition
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Term
| What is the duration of neostigmine? |
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Definition
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Term
|
Definition
| a long-acting cholinesterase inhibitor |
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Term
| What is the MOA of echothiophate? |
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Definition
| like neostigmine (forms covalent bond) but it is released more slowly |
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Term
| which drug has an MOA like neostigmine (forms covalent bond) but it is released more slowly? |
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Definition
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Term
| clinical applications for echothiophate? |
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Definition
| obsolete, was used in glaucoma |
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Term
| which drug is now obsolete but was used for glaucoma? |
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Definition
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Term
| How is echothiophate given? Toxicity? |
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Definition
| topical only, brow ache, uveitis, blurred vision |
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Term
| Which drug is given topically only and causes brow ache, uveitis, blurred vision? |
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Definition
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Term
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Definition
| an insecticide that is relatively safe for mammals and birds because it's metabolized by other enzymes to inactive products, some medical use as ectoparasiticide |
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Term
| which drug is an insecticide that is relatively safe for mammals and birds because it's metabolized by other enzymes to inactive products, and has some medical use as ectoparasiticide? |
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Definition
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Term
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Definition
| insecticide, dangerous for all animals, toxicity important because of agricultural use and exposure of farm workers? |
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Term
| Which drug is an insecticide, is dangerous for all animals, and has toxicity that's important because of agricultural use and exposure of farm workers? |
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Definition
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Term
|
Definition
| Sarin, a long acting cholinesterase inhibitor |
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Term
| Only direct acting agent that is very lipid soluble and used in glaucoma |
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Definition
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|
Term
| Treatment of atropine overdose and glaucoma (because lipid soluble). Enters the CNS rapidly and has a stimulant effect, which may lead to convulsions |
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Definition
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Term
| Antiglaucoma organophosphate |
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Definition
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|
Term
| Associated with an increased incidence of cataracts in patients treated for glaucoma |
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Definition
| Long acting cholinesterase inhibitors |
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|
Term
| Scabicide organophosphate |
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Definition
|
|
Term
| Organophosphate anthelmintic agent with long DOA |
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Definition
|
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Term
| Toxicity of organophosphate: |
|
Definition
| DUMBELSS (diarrhea, urination, miosis, bronchoconstriction, excitation of skeletal muscle and CNS, lacrimation, salivation, and sweating) |
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|
Term
| The most important cause of acute deaths in cholinesterase inhibitor toxicity |
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Definition
|
|
Term
| The most toxic organophosphate |
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Definition
|
|
Term
| Treatment of choice for organophosphate overdose |
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Definition
|
|
Term
| This agent regenerates active cholinesterase and is a chemical antagonist used to treat organophosphate exposure |
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Definition
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