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Block3Pharm
Cholinergics/Adrenergics
| Question | Answer |
|---|---|
| Pralidoxime | Frees acetylcholinesterase to active unit. for treatment of cholinergic overdose |
| Phyrostigmine | AchE inhibitor; glaucoma treatment. can penetrate CNS |
| Neostigmine | AchE inhibitor; Myasthenia Gravis treatment |
| Edrophonium | quaternary alcohol, forms ionic interactions with AchE (competitive inhibitor), diagnose myasthenia gravis |
| Carbamate | Competitive inhibitor of AchE |
| DFP | organophosphate, irreversible cholinesterase inhibitor, glaucoma |
| Bethanechol | muscarinic agonist, resists AchE (treat bladder atony) |
| Carbachol | muscarinic/nicotinic agonist; applied topically to treat glaucoma by opening canals of Schlemm |
| Pilocarpine | muscarinic agonist which is not a substrate for AchE (long lasting); glaucoma |
| Methacholine | muscarinic receptor agonist; resists hydrolysis by AchE, test for bronchial asthma |
| Trimethaphan | hypertensive emergencies, counteracts cholinergic transmission at ganglion (like nicotine), nondepolarizing competitive antagonist at nicotinic receptor |
| scopalomine | anticholinergic, lots of CNS axn; nausea |
| atropine | anticholinergic |
| ipratopium | anticholinergic, used to treat bronchial constriction |
| nicotine | depolarizing noncompetitive cholinergic ganglionic blocker (kind of like trimethaphan) starts excitatory, then depression at ALL ANS ganglion |
| vecuronium | competitive nAchR blocker (at NMJ); no histamine release, short duration of axn |
| hemicholinium-3, triethylcholine | blocks uptake of choline (rate limiting step for acetylcholine release) |
| d tubocurarine | ccompetitve and nondepolarizing nAchR at NMJ blocker, causes some bronchoconstriction due to histamine release |
| atracurium | shorter duration of axn than tubocurarine, some histamine release |
| mivacurium | nAChR blocker at NMJ; low histamine release, really short acting |
| succinylcholine | depolarizing nAchR blocker at NMJ |
| MAO inhibitor | increase serotinin, dopamine levels by blocking metabolism |
| clorgylin | antidepression MAOI |
| selegiline | MAOI, adjuvant to Parkinson's tx |
| tyramine | taken up by NE reuptake vessels preferentially (increases NE in synaptic junction) |
| amphetamine | taken up by NE reuptake vessels preferentially (increases NE in synaptic junction), also adrenergic drug |
| cocaine | competitively inhibits NE/EPI neuronal uptake |
| impramine | tricyclic antidepressant, competitively inhibits NE/EPI neuronal uptake |
| reserpine | irreversibly inhibits vesicular uptake system where DOPA is taken up in storage vesicles and is converted to NE so decreases intraneuronal NE; treats hypertension/psychosis |
| guanethidine | inhibits noradrenergic nerve function by being preferentially taken up in neuronal cellsso have accumulation in sympathetic nerves so decrease NE but mostly block release (exocytosis) of NE |
| alpha 1 selective antagonists | tarazosin, doxazosin, tamsulosin; hypertension tx without blocking alpha 2 so don't get extra NE release (tachycardia) |
| beta 1 selective antagonist | metoprolol, atenolol, esmolol; specifically target cardiac output (not vasodilation), can still use EPI for rescue therapy |
| propanolol | non selective beta blocker, used for hypertensive patients, decrease HR and CO, decrease BP |
| pindolol | nonselective partial Beta agonist |
| carvedilol | 3rd generation beta blocker, antagonist to b1, b2 and a1 receptors, used in CHF to decrease arrhythmias, increase ejection fraction and decrease hypertrophy |
| labetolol | 3rd generation beta blocker, antagonist to b1, b2 partial agonist and a1 receptors,, used in hypertensive emergencies, treat hypertension |
| timolol | glaucoma tx, non selective beta blocker, decrease formation of aq humor |
| dopabutamine | beta receptor agonist, circulatory shock tx, decrease CO without increasing SVR |
| dopamine | weak beta 1 recetpor agonist, increase CO, dopamine receptors on vascular SM lead to vasodilation and increased perfusion of vital organs without increasing bp |
| albuterol, salmeterol | beta 2 agonists, albuterol is used for rescue thereapy, salmeterol with steroid = advair, lipphilic long acting be2 receptor agonist |
| sumatriptan | 5HT1D receptor agonist, used to treat migraines, decresae proinflammatory peptide release, constriction of blood vessels to shunt to ischemic areas |
| dipivefrin | prodrug for epi used to great glaucoma, increase outflow of aqueous humor and decrease formation of aq humor |
| phenylephrine | alpha 1 agonist, treat hypotension, paroxysmal atrial tachycardia, mydriasis: contraction of pupils. |
| epinephrine | inhibits mast cell degranulation |
| isoproterenol | poor alpha agonist, good b2/b1 agonist |
| clonidine | acts in CNS on a2 receptors to decresae sympathetic outflow, good for withdrawal from addiction |