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40 Cards in this Set
- Front
- Back
Undesirable side effects of drugs that antagonize NE
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1. Postural Hypotension
2. Sedation/Depression 3. Increased GI Motility 4. Sodium Retention 5. Impaired Sexual Function |
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Irreversible antagonist of alpha 1 and 2
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Phenoxybenzamine
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Length of time for irreversible blockade to develop
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60-70 minutes
Lasts 3-4 days |
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Effects of alpha 2 blockade in phenoxybenzamine
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1. enhanced reflex tachycardia
2. Enhanced GI tone and motility 3. Blockade of epi's ability to inhibt insulin secretion |
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Method of delivery for phenyoxybenzamine
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Irritant properties dictate parenteral (however it is lipid soluble and gets into CNS)
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Reversible competitive alpha 1 and 2 antagonist
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Phentolamine
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Addition mechanisms found in Phentolamine over Phenyoxybenzamine
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1. Vasodilation by direct action on vascular smooth muscle
2. More intense cardiac stimulation than reflex 3. Increased GI tone, motility and secretion |
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Phentolamine is primarily used in the OR because?
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Cardiac and GI stimulation are so strong, tolerable doses have incomplete alpha blockade.
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Prototype alpha 1 anatagonist and its half life
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Prazosin
T1/2 = 3 hours |
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differences between prazosin and phenoxybenzamine or phentolamine
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little reflex tachy
little GI stimulation sex side effects are rare CNS effects of drowsiness, dissiness, fatigue |
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This drug may cause postural hypotension with the first dose only
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prazosin
Should be administered lose dose at night the first time |
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Difference between terazosin and prazosin
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Terazosin T1/2 = 12 hours
Prazosin T1/2 = 3 hours |
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Three therapeutic uses for alpha blockers
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Essential hypertension
Urinary Retention Pheochromocytoma |
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Drugs for essential hypertension
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Prazosin and terazosin
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Drugs for urinary retnetion
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terazosin helps void bladder
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Drugs for pheochromocytoma surgery
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Pre-op Oral phenoxybenzamine
Op IV phentolamine Cause vasodilation and increase blood volume prior to surgery |
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Chronic pheyochromocytoma
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oral phenyoxybenzamine
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non selective beta antagonists
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Propranolol
Nadolol Timolol Pindolol Labetalol |
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Cardio effects of propranolol
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slows all aspects of heart
decreases systolic pressure reflexive increases in PR leading to low blood flow low GFR |
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Propranolol effects on exercise tolerance in partient with angina and in normal patients
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increases tolerance with angina, but decrease tolerance in normal patients
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Metabolic effects of propranolol
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block insulin release and metabolism on fat and muscle
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Toxicity of propranolol
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Extreme case of normal actions (heart failure, bronchospasm, Na and water retention, sensitization to hypoglycemia)
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First pass clearance of propranolol
Half life % protein bound |
50%
3 to 40 hours 90% |
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Nadolol
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Propranolol with T1/2 20-24 hours
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2 uses of Timolol
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1. Antihypertensive
2. Reduction of aqueues humor for glaucoma |
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non-selective beta antagonist with partial agonist activity. less withdrawl symptoms
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Pindolol
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a alpha and beta antagonist
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Labetalol
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Metoprolol
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selective beta 1 antagonist
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Effects and toxicities of metoprolol
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Same and propranolol without bronchiol constriction (beta 2 mediated)
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beta 1 blocker with intrinsic sympathomimetic activity. t1/2 = 3 hours
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Acebutolol
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beta 1 blocker with 10 min half life. used IV for critcally ill partients for rapid withdrawl if necessary.
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Esmolol
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beta 1 blocker for opthalmic uses
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Betaxolol
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used for supraventricular tachycardia
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Esmolol
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beta 1 blocker with no intrinsive sympathomimetic activy
half life if 5=8 hours. does not pentetrate CNS |
Atenolol
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Does acebutolol have intrinsic sympathomimetic activity?
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Yes
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Two uses for betaxolol
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opthalmic use in glaucoma
antihypertensive |
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Does atenolol have intrinsice sympathomimetic activity
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No
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half live of Atenolol
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5-8 hours
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Esmolol is approved for treatment of
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Supraventricular tachycardia
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T 1/2 for acebutolol
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3 hours
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