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29 Cards in this Set
- Front
- Back
Bethanechol
clinical uses, treatment |
CU: Clinical uses: decreased parasympathetic tone
TX: Treatment of bladder and GI hypotonia |
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Direct acting cholinergic agonist.
Name them, their categories, The side effects and contraindications. |
N: Bethanechol (choline esterases), pilocarpine (natural alkaloids), cevimeline (new M3 specific agonists
SE:Side effects: diarrhea, diaphoresis, miosis, nausea, salivation, urinary urgency, CNS if BBB CI: Contraindications: 1) pts with asthma (increasing bronchoconstriction + secretions), 2) pts with heart disease- slow condution of cardiac action = causing arrhythmias. |
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Cevimeline
Clinical Uses, Tx, MOA |
CU: xerostomia
TX: Treatment of dry mouth in patients with Sjogren's syndrome MOA: more selective and potent at salivary glands. Fewer side effects than Pilocarpine. |
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indirectly acting ie: acetyl cholinesterase inhibitors
MOA, potential sites of action, categories, drugs |
MOA: inhibit acetylcholinesterase and prolong actions of acetylcholine.
Potential sites of action: Parasympathetic system (eye, gi, urinary bladder), NMJ, and all autonomic ganglia short (reversible): endrophonium Intermediate (reversible): Physostigmine Neostigmine pyridostigmine rivastigmine galatamine ambenonium donepezil tacrine Long (irreversible): synthetic organophosphate (ecothiophate and isofluorophate) and nerve gases (sarin and soman) |
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endrophonium
clinical use |
clinical use: diagnostic test for myasthenia gravis
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Drugs used to treat myasthenia Gravis
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Neostigmine
pyridostigmine ambenonium |
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Neostigmine
clinical use, what it is, adverse effects |
CU: to treat myasthenia gravis
WIS: synthetic compound that cannot enter the brain. affect nmj greater than physostigmine adverse effects: generalized cholinergic stimulation and a drop in blood pressure. overdose: cholinergic crisis (too much ACH residing in the NMJ) and muscle paralysis |
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drug(s) used to treat hypotonia of the bladder and GI
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physostigmine and bethanechol
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physostigmine
clinical use, what it is, MOA, adverse effects |
clinical uses: antidote for overdoses of atropine and other anticholinergic drugs. reduces IOP. Treat hypotonia of the bladder and GI and glaucoma
WIS: Plant alkaloid and tertiary amine that can cross the BBB MOA:causes ACH effects at muscarinic and nicotinic receptors of the ANS and NMJ (nicotinic) AE: adverse effects: diarrhea, nausea, sweating, miosis, urinary urgency, (high) convulsions, bradycardia, hypotension |
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drugs used to treat glaucoma
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physostigmine and ecothiophate
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drugs used to treat alzheimers
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donepezil, rivastigmine, tacrine, galantamine
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symptoms of poisoning by organophosphates
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symptoms of poisoning:
S: salivation L: Lacrimation U: urination D: defecation |
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How do you treat Organophosphate poisoning? what about prophylactically?
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tx: high doses of atropine or scopolamine followed by an injection of Pralidoxine (Pralidoxine: ineffective once aging has occured)
prophylactically: pyridostigmine |
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what does the "aging process" cause?
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inactivates AChE permanently causing ACh to accumulate in the junction without anything being able to break it down.
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what two categories of drugs cause the "aging process"?
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synthetic organophosphate and nerve gases
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muscarinic antagonists contraindications?
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glaucoma, BPH, myasthenia gravis
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cholinergic antagonists contraindications
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contraindications: slows voiding: no good for peps with urinary retention ie; BPH
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two categories of muscarinic antagonists, and their associated drugs.
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bella dona alkaloids (atropine and scopolamine)
synthetic and semi-synthetic derivatives (iprotropium, tiotropium, tolterodine) |
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atropine
MOA, clinical uses, Side effects, oddity |
MOA: tertiary amine- cross BBB. (competitive antagonist)= blocks all para symp
clinical uses: Reversal of severe bradycardia, produce mydriasis and cycloplegia atinspasmodtic, tx: for poisoning. side effects: xerostomia, blurred vision, hot, dry flushed skin, fever, CNS disturbances. Oddity: causes initial decrease in HR (.5) due to the presynpatic terminal response to an increase in ACh release. |
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scopolamine
MOA, CU, side effects |
MOA: crosses the BBB much more than atropine
Clinical uses: prophylactic for motion sickness side effects: same as atropine but the CNS effects are more prominent: DROWSINESS |
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ipratropium
Clinical uses and MOA |
clinical uses: asthma and COPD to cause bronchodilation as an adjunct to albuterol for pts who have cardiac issues
MOA: blocks muscarinic receptors specific to bronchiole; less CNS effects |
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tiotropium
clinical uses |
clinical uses: COPD and asthma. much more selective action at bronchioles
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tolterodine
Clinical uses, MOA, similar drugs, |
Clinical uses: tx of overactive bladder; inappropriate activation of parasymp innveration
MOA: blocks M3 receptors on detrusor muscle relaxing the muscle and diminishing urge during initial stages of filing. blocks parasym to sphincter too. similar drugs: fesoterodine, solifenacin (10 fold specificity), darifenacin, oxybutynin |
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what are the two categories of nicotinic antagonists?
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ganglionic blockers and NMJ blockers
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ganglionic blockers
MOA, drugs |
MOA: block Nn receptor
drugs: hexamethonium bromide, trimethopham, Mecamylamine (tx: mod to severe hypertension |
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NMJ blocker
Clinical use and two subcategories |
clinical use: skeletal muscle relaxants
Non-depolarizing blockers and depolarizing blockers |
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Non-depolarizing blockers
drugs, MOA |
Atracurium
cistracurium vecuronium rocuronium pancuronium tubocurarine MOA: cannot initiate depolarization; overcome by increasing amounts of ACh. competitive antagonist |
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succinyl choline
what is it, MOA, side effects |
WIS: two acetylcholine molecules linked end to end. metabolized by pseudocholinesterase. rapid onset, short duration.
MOA: initial: depolarization causing fasciculations. second: membrane repolarized. Ca2+ is removed but the drug is still occuping the space of ACh, so Na can't influx to depolarize. side effects: muscle damage, hyperkalemia, decrease HR, increase IOP... serious side effect: malignant hyperthermia |
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what are the two categories of cholinergic drugs?
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cholinomimetics/ parasympathomimetics and cholinergic antagonists/ parasympatholytics
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