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53 Cards in this Set
- Front
- Back
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metaraminol (Aramine)
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adrenergic agonist, α1 selective. Vasopressor (reverse hypotension - long acting β1,α1 receptor stimulant)
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methoxamine (Vasoxyl)
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adrenergic agonist, α1 selective. Uses: overcome hypotensive crisis (protect cerebral and coronary blood flow)
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phenylephrine (Neo-Synephrine)
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adrenergic agonist, α1 selective. Synthetic chatecholamine. Uses: nasal decongestant, vasopressor(shock), vasoconstrictor, mydriatic(facilitate eye exam)
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α-methyldopa (Aldomet)
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adrenergic agonist, α2 selective. PNS/CNS. Partial replacement of DOPA, makes MNE -> false NT. Hypotensive activity from stimulation of vasomotor center in brainstem
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clonidine (Catapres)
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adrenergic agonist, α2 selective. Inhibit NE release presynaptically, less NE-> hypotension (low HR, periph.resist., CO). CNS effects
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guanabenz (Wytensin)
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adrenergic agonist, α2 selective. Inhibit NE release presynaptically, less NE-> hypotension (lower HR, periph.resist., CO)
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amphetamine
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adrenergic agonist, mixed αβ, NET - blocks NE reuptake, stimulates release
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ephedrine
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adrenergic agonist, mixed αβ, NET. Uses: vasopressor(chronic hypotension), mydriatic, nasal decongestant, relax bronchi, CNS stimulant, increase mm. contractility, stress incontinence
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epinephrine
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adrenergic agonist, mixed αβ (β1=β2>>α1=α2). Released by adrenal medulla. Uses: anaphylactic shock, relax bronchi, vasoconstriction(hemostasis during surgery), mydriatic(glaucoma)
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norepinephrine
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adrenergic agonist, mixed αβ (β1>>β2,α1=α2). 1° NT of adrenergic fibers. vasopressor (shock)vasoconstriction(α1), increase CO (β1), dilate renal blood vessels (DA1)
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dobutamine
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adrenergic agonist, β1 selective. Uses: increase force of cardiac contraction, increase cardiac output (heart failure)
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isoproterenol (Isuprel)
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adrenergic agonist, β non-selective. Synthetic chatecholamine. Uses: vasodilation, relax bronchi (asthma)(β2), cardiac stimulant (A-V block)(β1)
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albuterol (Proventil)
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adrenergic agonist, β2 selective. Uses: relax bronchi (bronchial asthma)
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metaproterenol (Alupent)
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adrenergic agonist, β2 selective. Uses: relax bronchi (bronchial asthma)
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terbutaline (Brethine)
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adrenergic agonist, β2 selective. Uses: relax bronchi (bronchial asthma), relax pregnant uterus
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bromocriptine (Parlodel)
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dopamine agonist, DA2. Uses: anti-parkinson agent. PNS effects: postural hypotensions initially, dvlpmnt of cardiac arrhythmia
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dopamine
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dopamine agonist, β1,α1,DA1&NET. Released on renal and splanchnic vascular mm. Vasopressor (shock), increase blood flow or pressure after MI
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fenoldopam (Corlopam)
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dopamine agonist. Uses: vasodilation of renal and mesenteric vessels
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doxazosin (Cardura)
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adrenergic antagonist, α1 selective. Uses: relieving urinary symptoms (from BPH)
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prazosin (Minipres)
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adrenergic antagonist, α1 selective. Competitive. Hypertension therapy. No tachy side effect (selective) - expect reflex induced tachy, (-)'ed by unknown site? NOT β1. Oral. Lasts 12hrs
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phenoxybenzamine (Dibenzyline)
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α receptor antagonist. Noncompetitive (irreversible). Alkylates α1andα2, and inhibits NET. Lasts 24hrs. Oral or IV. Used for hypertension caused by pheochromocytoma
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phentolamine (Vasomax)
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α receptor antagonist. Competitive. α1->vasodilation(therapeutic use); α2->NE release (β1 not blocked, NE will elicit tachy and increased CO). Also cross reactive with muscarinic, histamine receptors. Used to help diagnost pheochromocytoma (Regitine Test)
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tamsulosin
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adrenergic antagonist, α1 selective. Uses: relieving urinary symptoms (from BPH)
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terazosin (Hytrin)
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adrenergic antagonist, α1 selective. Uses: relieving urinary symptoms (from BPH)
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labetalol (Trandate)
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adrenergic antagonist, mixed αβ
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atenolol (Tenormin)
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adrenergic antagonist, β1 selective. Use: antihypertensive. 6-9hr½life. Diminished ability to cross BBB
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betaxolol (Betoptic, Kerlone)
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adrenergic antagonist, β1 selective. Use: glaucoma (reduces production of aqueous humor). 14-22hr½life
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metoprolol (Lopressor)
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adrenergic antagonist, β1 selective. Uses: prophylactically for recurrence of MI. antihypertensive, angina pectoris. 3-4hr½
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nadolol (Corgard)
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adrenergic antagonist, β non-selective. Uses: antihypertensive. 14-24hr½life. Diminished ability to cross BBB
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pindolol (Visken)
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adrenergic antagonist, β non-selective. Uses: antihypertensive. 3-4hr½life.
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propranolol (Inderal)
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adrenergic antagonist, β non-selective. Uses: prophylactically for recurrence of MI. antihypertensive, anti-arrythmic, angina pectoris, migraine headache. 3-6hr½life
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timolol (Timoptic)
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adrenergic antagonist, β non-selective. Uses: prophylactically for recurrence of MI. antihypertensive, angina pectoris, decrease intraocular pressure. 4-5hr½life
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guanethidine (Isemlin)
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depletes biogenic amine stores in vesicles, reducing NE release - ultimate hypotensive activity. Gets in via NET (inhibited by cocaine and DMI). Also stabilizes neuronal membrane, causing less exocytosis. Does not cross BBB.
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reserpine
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depletes stores of biogenic amines, by blocking transport into storage vesicles. Potent. Oral. Long duration. Adverse effects mostly in CNS, also ulcers from increased GI motility
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cocaine
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amine I transport inhibitor - NE levels rise, further sym. stimulation at target. Also causes hemostasis during surgery
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DMI (desmethylimipramine)
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tricyclic antidepressant, amine I transport inhibitors - NE levels rise, further sym.stimulation at target
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NE releasing agents
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amphetamine, ephedrine, tyramine, psuedoephedrine, dopamine
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Amine I transport
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active transport of catecholamines into sympathetic nerve terminals (NE Transporter)
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tyrosine hydroxylase
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converts tyrosine to DOPA; rate limiting step in catcholamine synthesis; (-) feedback inhibition control via presynaptic receptors
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COMT
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catechol-o-methyltransferase; found in liver (and other tissues) transfers methyl group onto 3' hydroxyl
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MAO
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monoamine oxidase; found in adrenergic nerve terminals, liver, brain (and other tissues) removes amide group
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adrenergic agonists: substitutions on amino group
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larger alkyl moieties increase β activity. Isoproterenol, dobutamine, terbutaline
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adrenergic agonists: substitutions to benzene ring
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loss of -OH decreases potency, but increases duration of action (COMT can't methylate). Metaraminol, phyenylephrine, ephedrine
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adrenergic agonists: substitutions to α-carbon
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block oxidation by MAO, prolonging activity. Better able to displace NE from storage vesicles. Metaraminol, ephedrine
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α1 adrenoceptors
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binds Gq. elicit contraction/constriction reponses (vessels, radial iris mm., ejaculation, piloerection), relax intestines, glycogenolysis
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α2 adrenoceptors
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binds Gi. Presynaptic - autoreceptors that provide negative feedback to decrease NE release from terminals. Antagonists cause further NT release
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β1 adrenoceptors
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binds Gs. Increases heart rate, heart contractile force, cardiac output, lipolysis
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β2 adrenoceptors
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binds Gs. Skeletal mm vasodilation, smooth mm relaxation (vessels, myometrial, bronchi, intestine), decrease intraocular pressure, increased tremor
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β3 adrenoceptors
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increased glycogenolysis in liver and skeletal mm
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D1 adrenoceptors
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binds Gs. Vasodilation of renal and mesenteric organs
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D2 adrenoceptors
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binds Gi. Presynaptic - negative feedback role to decrease dopamine release. Antagonists eliminate (-) feedback and cause further NT release
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tyramine
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releases NE from nerve terminals after being taken up by NET (amino I transport). Found in cheeses, beer, sausage - danger for pts on MAO inhibitors (increase art.pressure)
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esmolol
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adrenergic antagonist, β1 selective. Uses: acute Tx of sinus tachycardia, atrial flutter. 9min½life
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