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24 Cards in this Set

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Phenoxybenzamine

Dibenzyline(R)

MOA: Non- selective, non- competitive α-antagonist/blocker with slightly greater affinity for the α1 receptor


Blocks histamine, ACh & serotonin receptors as well.


Indications: pheochromocytoma (↓HTN & sweating), Raynaud’s disease & frostbite

Phentolamine

Regitine®

Indications: short term management of pheochromocytoma, prevention of dermal necrosis following administration of IV NE, impotence (along with papaverine), hypertensive crisis following abrupt withdrawal of clonidine or following combination of tyramine & MAOIs, hypertension due to overdose of amphetamines & cocaine, rebound hypertension due to abrupt clonidine withdrawal



MOA: Non- selective, competitive α-antagonist/blocker with effects lasting for about 4 hours after injectionα1 blockage: ↓ PR  ↓ BP, relaxation of the trigone & sphincter muscles of the bladder increased urination. Reflex stimulation of the heart due to the baroreceptor effect.α2 blockage: Leads to cardiac stimulation & reflex tachycardia

Prazosin

Minipress®

Indications: 2nd line treatment of systemic HTN, urinary hesitancy in BPH, CHF & pheochromocytoma



MOA: Selective, competitive α1-antagonist/blocker. 1000x more potent at α1 receptor vs α2 receptor

Tamsulosin

Flomax®

Indications: BPH



Modestly selective α1A receptor antagonist which acts on the receptors in the prostrate.

Yohimbine

Aphrodyse®

Indications: treatment of erectile dysfunction, orthostatic hypotension



MOA: Selective, competitive α2 blocker

β- adrenergic Blockers

1. Non-selective β-antagonists e.g. Propranolol 2. Non-selective β-antagonists with action as α1-antagonists e.g. Carvedilol3. β-adrenergic partial agonists: partial activation of the receptor e.g. Pindolol4. β1-selective /cardioselective antagonists e.g. Atenolol

Propranolol

Inderal®

Indications: chronic angina, arrhythmia, 1st line agents for HTN, cardiomyopathy, vascular headache, tremors, physical symptoms of anxiety, mitral valve prolapse, thyrotoxicosis, prophylaxis against myocardial re-infarction and subsequent arrhythmia, adjunct for pheochromocytoma



non-selective β blocker with equal affinity for both subtypes of β receptors. It posses membrane stabilising activity

Nadolol

Corgard®

Used to treat bleeding from esophageal varices in patients with cirrhosis



Non-selective β blockers

Timolol

Blocarden® Timoptic®, Timoptic XE®

used to diminish intraocular pressure in persons with chronic glaucoma.



Non-selective β blockers

Carteolol

Ocupress®

used topically to treat glaucoma



Non-selective β blockers

Levobunolol

Betagan®

used topically to treat glaucoma



Non-selective β blockers

Pindolol

Visken®

Indications: HTN with bradycardia ( less pronounced reduction in HR with this drug



non-selective β blocker with ISA and membrane stabilising activity

Sotalol

Betapace®

used mainly to treat arrhythmias



non-selective β blocker

Penbutalol

Levatol®

used mainly to treat HTN



non-selective β blocker

Metoprolol

Lopressor®, Toprol XL®

Used to manage angina, HTN, arrhythmia, cardiomyopathy, prophylaxis for MI,stable CHF, pheochromocytoma, vascular headache, tremors & anxiety



membrane stabilising effects .



β1 Selective Antagonists

Atenolol

Tenormin®

used to manage HTN. Hydrophillic with limited penetration to the CNS due to its low lipophicity



β1 Selective Antagonists

Acebutolol

Sectral®

used to manage HTN


has ISA



β1 Selective Antagonists

Nebivolol

Bystolic®

most selective blocker


β1 Selective Antagonists


Esmolol

Brevibloc®

Used in critically ill patients when β blocking activity needed for a short period of time with little side effects - β1 Selective Antagonists


Indications: IV for control of supraventricular arrhythmias, arrhythmias associated with thyrotoxicosis, perioperative HTN, & myocardial ischemia in acutely ill patients.



β1 Selective Antagonists


Bisoprolol

Zebeta®

no ISA and is used for stable CHF - β1 Selective Antagonists

Betaxolol

Betoptic®

no ISA and is used topically to treat glaucoma - β1 Selective Antagonists

Labetalol

Trandate®

Indications: treating hypertensive patients for whom increased PVR is undesirable


Mixed α-β Antagonists



alternative to methyldopa in pregnancy induced HTN, IV for hypertensive emergencies. ISA at the β2receptor only

Carvedilol

Coreg®

useful in stable CHF with decreased systolic function.


Mixed α-β Antagonists

Mixed α-β Antagonists

Order of activity : β1 = β2 > α1. In addition β –blocking effects they lead to peripheral vasodilation due to α1 blockade→ ↓ PR