Medchem Adrenergic Antagonists

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    • Prazosin: α1-Blocker (reversible)
    • Tx: Hypertension
    • ADEs: syncope, dizziness, orthostatic hypotension
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    • Terazosin: α1-Blocker (reversible)
    • Tx: Hypertension + BPH nocturia
    • ADEs: syncope, dizziness, orthostatic hypotension
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    • Doxazosin: α1-Blocker (reversible)
    • Tx: Hypertension + BPH nocturia
    • ADEs: syncope, dizziness, orthostatic hypotension
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    • Alfuzosin: α1-Blocker (reversible)
    • Tx: BPH nocturia
    • ADEs: syncope, dizziness, orthostatic hypotension
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    • Silodosin: α1a-Blocker (reversible)
    • Tx: BPH nocturia
    • ADEs: block ejaculation
    • *take with evening meal
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    • Tamsulosin: α1a-Blocker (reversible)
    • Tx: BPH nocturia
    • ADEs: ?
    • *Evening dosing, without meals
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    • Phentolamine:  α1 and α2-Blocker (reversible)
    • Tx: Frostbite, but not used often; and to diagnose adrenal medulla tumor (pheochromocytoma)
    • ADEs: ?
    • *imidazoline antagonist!
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    • Dichloroisoproterenol: β1 and β2 antagonist
    • Tx: Hypertension
    • ADEs: hypotension, bradycardia, fatigue, drowsiness
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    • Pronethalol: β1 and β2 antagonist
    • Tx: Hypertension
    • ADEs: hypotension, bradycardia, fatigue, drowsiness
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    • Labetalol: β1 and β2 AND α1 antagonist
    • Tx: Hypertension
    • ADEs: hypotension, bradycardia, fatigue, drowsiness
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    • Propranolol: β1 and β2 antagonist (ortho-meta)
    • Tx: Hypertension, glaucoma, migraine, hyperthyroidism, angina pectoris, myocardial infarction
    • ADEs: hypotension, bradycardia, fatigue, drowsiness
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    • Nadolol: β1 and β2 antagonist (ortho-meta)
    • Tx: Hypertension
    • ADEs: hypotension, bradycardia, fatigue, drowsiness
    • *Cleared renally, thus not dependent on individual metabolism. Therefore easier to dose.
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    • Alprenolol: βand β2 antagonist (ortho)
    • Tx: Hypertension
    • ADEs: hypotension, bradycardia, fatigue, drowsiness
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    • Timolol: β1 and β2 antagonist (ortho)
    • Tx: Hypertension, Glaucoma
    • ADEs: hypotension, bradycardia, fatigue, drowsiness
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    • Atenolol: β1 antagonist (para)
    • Tx: Hypertension, Open-Angle Glaucoma
    • ADEs: hypotension, bradycardia, fatigue, drowsiness
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    • Metoprolol: β1 antagonist
    • Tx: Hypertension
    • ADEs: hypotension, bradycardia, fatigue, drowsiness
    • *Preferred w/ asthmatics and diabetics
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    • Betaxolol: β1 antagonist
    • Tx: Hypertension
    • ADEs: hypotension, bradycardia, fatigue, drowsiness
    • *Opthalmic preferred w/ asthmatics
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    • Bisoprolol:  β1 antagonist
    • Tx: Hypertension
    • ADEs: hypotension, bradycardia, fatigue, drowsiness
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    • Nebivolol: β1 antagonist (newest)
    • Tx: Hypertension
    • ADEs: hypotension? It is the most β1-specific, so perhaps it doesn't have as many side effects?
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    • Phenoxybenzamine: α1 and α2-Blocker (irreversible; alkylating agent)
    • Tx: Increase blood flow to periphery for post-menopausal women (Raynaund's syndrome); Pheochromocytoma-induced hypertension
    • ADEs: orthostatic hypotension, tachycardia, vertigo, sexual dysfunction
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    • Pindolol: β1 and β2 antagonist (ortho-meta) Intrinsic Sympathomimetic Activity (ISA)
    • Tx: Hypertension
    • ADEs: hypotension, bradycardia, fatigue, but not as bad as the regular β-blockers
    • *recommended for African-American hypertensive patients
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    • Carteolol: β1 and β2 antagonist (ortho-meta) Intrinsic Sympathomimetic Activity (ISA)
    • Tx: Hypertension
    • ADEs: hypotension, bradycardia, fatigue, but not as bad as the regular β-blockers
    • *Opthalmic! contraindicated in asthmatics, hepatically cleared
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    • Celiprolol: β1 antagonist with selective β2-ISA (Intrinsic Sympathomimetic Activity)
    • Tx: Hypertension (via vasodilation)
    • ADEs: hypotension, bradycardia, fatigue, but not as bad as the regular β-blockers
    • *Sold in Europe, NOT USA
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    • Penbutolol: β1 and β2 antagonist (ortho-meta) Intrinsic Sympathomimetic Activity (ISA)
    • Tx: Hypertension
    • ADEs: hypotension, bradycardia, fatigue, but not as bad as the regular β-blockers
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    • Acebutolol: β1-selective antagonist w/ Intrinsic Sympathomimetic Activity (ISA)
    • Tx: Asthmatics' Hypertension
    • ADEs: hypotension, bradycardia, fatigue, but not as bad as the regular β-blockers
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    • Carvedilol: S-enantiomer = β1 and β2 antagonist, R-enantiomer = α1-Blocker (reversibility?) (UNIQUE)
    • Tx: CHF
    • ADEs: ????
    • *If there's an OH on the benzene ring, it is 13x more potent as an agonist, as compared to when it's a naked benzene ring.
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Accelipse
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Card Set:
Medchem Adrenergic Antagonists
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2012-11-04 20:34:39
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Medchem Rutgers Exam2 Drugs Structures
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Rutgers Medicinal Chemistry: Adrenergic Antagonists. From Monday 10/8/12
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