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102 Cards in this Set
- Front
- Back
- 3rd side (hint)
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drug
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bethanechol
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parasympathetic that promotes GI and urinary tract mobility, mAChR agonist
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atropine
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parasympathetic antagonist dilates pupils (locally) or increases heart rate (systemically)
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ipratroprium
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parasympathetic antagonist dilates bronchioles
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pancuronium
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antagonist of neuromuscular junction activity used to induce paralysis in surgery
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edrophonium
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increase NMJ activity used in diagnosis and treatment of myasthenia gravis (if administration mitigates muscle weakness then postive for MG, if it makes the weakness worse then there is a depolarizing antagonist of nAChR present) via inhibition of AChEsterase (simple alcohol, reversible inhibition)
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neostigmine
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increase NMJ activity used in diagnosis and treatment of myasthenia gravis via inhibition of AChEsterase and direct activation of nAChR, quaternary ammonium, also used to increase GI motility
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barbituates
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activate GABA neurons in cortex (sedative and hypnotic)
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benzodiazepenes
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activate GABA neurons in cortex (sedative and hypnotic)
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clonidine
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partail agonist that acts on presynaptic alpha-2 receptors
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tricyclic antidepressants
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block NE and serotonin reuptake
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monoamine oxidase inhibitors
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block NE degradation
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ssri
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block serotonin reuptake (antidepressant)
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carbidopa
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inhibitor of dopamine decarboxylase (Ldopa-->dopamine)
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vesamicol
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inhibits the H+/Ach antiporter into the vesicles
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hemicholinium-3
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inhibits sodium-dependent transport of choline into neurons
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hexamthonium
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selective blockage of presynaptic cholinergic receptor that prevents facilitation and causes rapid tetanic fade
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botulinum toxin
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degrades synaptobrevin and blocks Ach synaptic vesicle fusion; ;used for achalasia, strabismus (eye misalignment due to ocular imbalance, esotropia=cross-eyed, exotropia=wall-eyed), blepharospasm (involuntary closing of the eyelids), cosmetic
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pralidoxime
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strong nucleophile that prevents aging of AChE
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diisopropyl fluorophosphate
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organophosphate that inhibits AChE shows property of aging
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physostigmine
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increase NMJ activity used in diagnosis and treatment of myasthenia gravis via inhibition of AChEsterase, quaternary ammonium
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ambenonium
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treatment of myasthenia gravis via inhibition of AChE
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Meds to treat alzheimers
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tacrine, donepezil, rivastigmine, galantamine
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three uses of AChE inhibitors
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increase transmission at NMJ, increase parasympathetic tone, increase cholinergic activity in CNS in Alzheimer's Dz
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methacholine
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used for diagnosis of asthma (mAChR agonist)
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Carbachol
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mAChR agonist, used as a miotic agent, treatment of glaucoma
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pilocarpine
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alkaloid mAChR agonist used for drymouth secondary to decreased salivary secretion (xerostomia) treatment as it induces saliva
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succinylcholine
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nAChR agonist, used to induce depolarizing paralysis (see fasciculations at onset)
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uses of atropine
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induce mydriasis (pupil dilation), to reverse sinus bradycardia caused by excessive vagal tone in the context of MI or asystole, inhibit excessive salivary and mucus secretion during surgery, to prevent vagal reflexes induced by surgical trauma of visceral organs, counteract the effects of muscarine poisoning from certain mushrooms
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atropine
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alkaloid mAChR antagonist, must be used in high doses
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scopolamine
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mAChR antagonist used for motion sickness (CNS effects)
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pirenzepine
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mAChR antagonist selective for M1 and M4, alternative peptic ulcer treatment to H2 receptor blockers
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ipratropium
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mAChR antagonist. Quaternary ammonium, COPD (better than beta-adrenergic agonists)
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d-tubocurarine
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long lasting nAChR antagonist
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pancuronium
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long lasting nAChR antagonist
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vecuronium
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intermediate lasting nAChR antagonist
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rocuronium
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intermediate lasting nAChR antagonist
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mivacurium
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short lasting nAChR antagonist
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mecamylamine
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nAChR antagonist used to treat HTN in patients with acute dissecting aortic aneurysms (lower BP and blunt sympathtic reflexes that would normally cause rise in BP)
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trimethaphan
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nAChR antagonist used to treat HTN in patients with acute dissecting aortic aneurysms (lower BP and blunt sympathtic reflexes that would normally cause rise in BP)
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alpha-1 receptor antagonists
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hypertension and prostatic hypertrophy therapies
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alpha-2 receptor agonists
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act at CNS sites to decreases sympathetic outflow to perifery and decrease SMC contraction, tx for hypertension
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beta-1 receptor antagonists
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decrease heart rate, AV-nodal conduction velocity, and contractility, used to treat MI, hypertension, supraventricular tachycardia, and mild-moderate CHF
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beta-2 receptor agonists
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vasodilate, decrease bronchiolar constriction (asthma tx), act on kidney to catabolize glycogen (increase blood sugar)
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systemic dopamine treatment
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for shock (high doses [>10ug/kg per min]activates alpha 1 adrenergic receptor to induce vasoconstriction)
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alpha-methyltyrosine
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treatment of HTN associated with pheochromocytomas, analogue of tyrosine that blocks catecholamine synthesis
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reserpine
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irreversible inhibits VMAT (uptake 2) which prevents formation of catecholamine vesicles, was used for HTN tx, no longer really used
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indirect sympathomimetics
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act to displace NE from vesicles
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mixed sympathomimetics
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displace NE from vesicles and direct effect on adrenoreceptors
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tyramine
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dietary amine that when taken with MAOI can get into vesicles and cause an acute displacement of NE out of the vesicles --> HTN crisis (wine has a high concentration of tyramine)
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guanethidine
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displaces NE from vesicles, used for uncontrolled HTN
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guanadrel
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displaces NE from vesicles, used for HTN, not used much anymore.
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amphetamine
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displaces endogenous catecholamines, inhibits MAO, acts as an agonist to peripheral Beta and Alpha-receptors, potent adrenoceptor agonist in the CNS, increased alertness, decreased fatigue, depressed appetite, insomnia; side fx: fatigue and depression
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ephedrine
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similar yet less potent than amphetamine
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pseudoephedrine
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similar yet less potent than amphetamine
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phenylpropanolamine
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similar yet less potent than amphetamine
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methamphetamine
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similar and more potent than amphetamine, also known as crystal meth or crank
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cocaine
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inhibits NET (type 1 Uptake) of catecholamines nearly completely, significant risk of abuse
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imipramine
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tricyclic antidepressent that inhibits NET mediated reuptake of NE, also inhibit seratonin and block serotonergic, alpha-adrenergic, histaminergic, and muscarinic receptors; lots of side effects; used for depression (NE and serotonin reuptake inhibition); latency period of several weeks
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None
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amitriptyline
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tricyclic antidepressent that inhibits NEW mediated reuptake of NE, also inhibit seratonin and block serotonergic, alpha-adrenergic, histaminergic, and muscarinic receptors; lots of side effects; used for depression (NE and serotonin reuptake inhibition); latency period of several weeks
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phenelzine
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nonselective MAOI (MOA-A and MOA-B)
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iproniazid
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nonselective MAOI (MOA-A and MOA-B)
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tranylcypromine
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nonselective MAOI (MOA-A and MOA-B)
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clorgyline
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selective MOA-A inhibition
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selegiline
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selective MOA-B inhibition
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brofaromine
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reversible MOA-A inhibitor
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befloxatone
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reversible MOA-A inhibitor
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moclobemide
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reversible MOA-A inhibitor
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uses of MOAIs
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depression, parkinson's dz (selegiline), avoid eating fermented foods with lots of tyramine, do not take with SSRI - can precipitate "serotonin syndrome" (restlessness, tremors, seizures, possibly coma and death)
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"serotonin syndrome"
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concommitant use of SSRIs and MOAIs; restlessness, tremors, seizures, possibly coma and death
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methoxamine
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alpha-1 agonist for hyptotension or shock treatment
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phenylephrine
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topical alpha-1 agonist, also used for shock
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oxymetazoline
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topical alpha-1 agonist
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tetrahydrazoline
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topical alpha-1 agonist
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clonidine
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alpha-2 agonist used for HTN and drug withdrawal symptoms, acts on presynaptic receptors to decrease sympathetic outflow, common side fx include bradycardia (decreased sympathetic activity and increased parasympathetic activity) and dry mouth
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guanabenz
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similar to clonidine more selective for alpha-2 receptors, less side effects
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guanfacine
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similar to clonidine
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methyldopa
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precursor to methylnorepinephrine, alpha-2 receptor agonist, decreases sympathetic outflow by activating presynaptic receptors, used for hypertension, especially in pregnant women (safer in pregnancy), has potential rare side effects of hepatotoxicity and autoimmune hemolytic anemia
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dobutamine
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beta-1 receptor agonist, used for acute management of decompensated heart failure (really a racemic mixture that has different effects depending on the stereoisomer)
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isoproterenol
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beta-1 and beta-2 receptor agonist, good for asthma but has cardiac side effect (beta-1 mediated), supplanted by newer selective drugs
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metaproterenol
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beta-2 selective agonist, used to treat obstructive airway disease and acute asthma via beta-2 receptor-mediated bronchodilation
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terbutaline
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beta-2 selective agonist, used to treat obstructive airway disease and acute asthma via beta-2 receptor-mediated bronchodilation
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albuterol
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beta-2 selective agonist, used to treat obstructive airway disease and acute asthma via beta-2 receptor-mediated bronchodilation
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salmeterol
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long-acting (12hr) beta-2 receptor agonist, bad for acute bronchoconstriction, may be good for prophylaxis
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phenoxybenzamine
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alpha-1 and alpha-2 receptor antagonist, used predominantly for pheochromocytomas and benign prostatic obstruction and HTN, many potential side effects and inductions of compensatory responses
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phentolamine
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reversibe, nonselective alpha-adrenoceptor antagonist, used for preoperative management of pheochromocytomas and HTN; many potential side effects and inductions of compensatory responses
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prazosin
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alpha-1 receptor antagonist, decreases peripheral resistance and preload, used to treat HTN and CHF; may have marked hypotension so first dose is given in small quantities
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terazpsom
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alpha-1 receptor antagonist, decreases peripheral resistance and preload, used to treat HTN and CHF; may have marked hypotension so first dose is given in small quantities, longer halflife than prazosin
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doxazosin
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alpha-1 receptor antagonist, decreases peripheral resistance and preload, used to treat HTN and CHF; may have marked hypotension so first dose is given in small quantities, longer halflife than prazosin
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tamsulosin
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alpha-1A receptor antagonist (found on prostate), used to treat BPH
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yohimbine
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alpha2 receptor antagonist, was used for ED, not used really anymore
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propanolol
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beta1 and beta2 antagonist, used to treat HTN and angina, may have decreased libido side effect (CNS effect)
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nadolol
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beta1 and beta2 antagonist, used to treat HTN and angina, may have decreased libido side effect (CNS effect)
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timolol
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beta1 and beta2 antagonist, used to treat HTN and angina, may have decreased libido side effect (CNS effect), ocular formulation used to treat glaucoma
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labetalol
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blocks alpha1 beta1 and beta2 receptors, used for HTN treatment, potential hepatoxicity requires close monitoring
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carvedilol
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blocks alpha1 beta1 and beta2 receptors, used for HTN treatment,
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pindolol
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partial agonist at beta1 and beta2, blocks action of NE at beta1 receptor, useful for hypertension but agonistic effect on beta1 causes less of a decrease in HR, therefore better to be used in people with bradycardia and HTN
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acebutolol
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partial agonist of beta-1 adrenoceptors, no effect on beta2, used for HTN
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esmolol
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beta1 selective antagonist, 3-4 minute halflife, used for emergency beta-blockade (as in thyroid storm)
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metoprolol
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beta1 selective antagonist, 4-8 hour halflife, prolongs life expectancy in people with moderate to mild CHF and patients who have survived a first MI
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atenolol
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beta1 selective antagonist, 4-8 hour halflife
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celiprolol
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beta1 selective antagonist and beta2 selective agonist
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