Adrenergic Antagonists
Drug Actions Receptor Therapeutic Uses Pharmacokinetics Adverse Effects Others
Phenoxybenzamine -irreversibly and non- Nonselective -Chronic -single administration -postural hypotension -administration of
competitively binds to the α-blocker management of can last for 24 hours -nasal stuffiness EPINEHPRINE in the
postsynaptic receptors pheochromocytoma -after administration it -nausea presence of this drug
-prevents vasoconstriction of -Pre-surgical takes a few hours -vomiting causes decrease in
peripheral BV, causing reflex administration for before actions develop -inhibit ejaculation systemic BP
tachycardia pheochromocytoma -induce reflex -actions of NE, are
-blockade of presynaptic to avoid tachycardia diminished, not reversed
inhibitory α2 receptors can hypertensive crisis -has to effect of
cause increased cardiac -Raynaud’s disease ISOPROTERENOL
output -Autonomic -contraindicated in
-reverse the α-agonist actions hyperreflexia patients with decreased
of EPINEPHRINE coronary perfusion
Phentolamine -competitive blocker Nonselective -Short management -single administration -Postural hypotension -contraindicated in
-EPINEPHRINE reversal α-blocker of can last for 4 hours -Reflex cardiac patients with decreased
pheochromocytoma stimulation and coronary perfusion
tachycardia
-Arrhythmias
-Anginal pain
Prazosin -competitive blockers Selective α1 -Prazosin, Terazosin, -Doxazosin excreted in -Dizziness -minimal changes in CO,
Terazosin - Tamsulosin: acts on α1A blockers Doxazosin: feces, and is the -Lack of energy RBF, GFR
Doxazosin receptors on SM of prostate treatment of HTN longest acting of all -Nasal congestion -Tamsulosin has least
Alfuzosin -decrease the peripheral -Tamsulosin, these drugs -Headache effect on BP
vascular resistance and lower Alfuzosin: treatment -Rest of the drugs are -Drowsiness -if used as monotherapy in
Tamsulosin
arterial BP of BPH excreted in urine -Orthostatic HTN, they can cause CHF
-“First-pass” (exaggerated hypotension -Prazosin can be used with
orthostatic hTN, resulting in -Inhibition of a diuretic for
syncope) effect occurs with 1st ejaculation and antihypertensive effect
administration of the drugs, retrograde ejaculation
therefore should be given at
bedtime
Yohimbine -competitive Selective α2 -Sexual stimulant -contraindicated in CNS
-works at the level of the CNS blocker -Raynaud’s disease and CV conditions
to increase sympathetic
outflow to the periphery
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Adrenergic Antagonists
Propranolol -diminishes CO due to Nonselective -Chronic -CIMETIDINE, -Bronchoconstriction -contraindicated in
negative chronotropic and β-antagonist management of FLUOXETINE, (causes death in patients with COPD or
inotropic effect angina PAROXETINE, asthmatics) asthma
-decreased BP leads to reflex -Attenuating RITONAVIR interfere -Arrhythmias -often combined with a
peripheral vasoconstriction supraventricular with metabolism of -impaired sexual activity diuretic to prevent Na+
-reduced BP causes decreased cardiac arrhythmias the drug in some retention
renal perfusion, leading to -HTN (Decreased CO, -BARBITURATES, -Fasting hypoglycaemia -pronounced
sodium retention inhibition of renin PHENYTOIN, hypoglycaemia may occur
-depresses SA and AV activity, release, decreased RIFAMPIN stimulate after insulin injection in a
resulting in bradycardia sympathetic outflow its metabolism Type I diabetic
-causes bronchoconstriction from CNS) -in the presence of these
-decreased glycogenolysis and -Chronic tx of drugs, EPINEPHRINE
glucagon secretion glaucoma doesn’t lower diastolic
-blocks the action of (decreased secretion pressure or stimulate the
ISOPROTERENOL on CVS of aqueous humor heart
by ciliary body) -Protective effect on the
-Prophylactic for myocardium
migraine
-Acute
hyperthyroidism
-Given after MI, it
reduces infarct size
Timolol -Timolol: reduces production Nonselective -Timolol: chronic -Nadolol: very long -more potent than
Nadolol of aqueous humor in the eye β-antagonist open-angle duration of action PROPRANOLOL
glaucoma
-Timolol: systemic tx
of HTN
Acebutolol -antagonize β1 receptors at Selective β1 -Lower BP in HTN -Esmolol: short -cardioselectivity
Atenolol doses 50- to 100- fold less antagonists -Increase exercise lifetime, therefore IV pronounced at low doses,
Metoprolol than those required to block tolerance in angina during surgery or lost at high doses
Esmolol β2 receptors -Useful in diabetic diagnostic procedure -may be used in
HTN pts receiving asthmatics with careful
insulin or oral monitoring
hypoglycaemic
agents
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Adrenergic Antagonists
Pindolol -Intrinsic sympathetomimetic Partial -HTN in pts with -minimize the
Acebutolol activity agonists moderate disturbances of lipid and
-Stimulate the β receptor to (weak bradycardia carbohydrate metabolism
which they are bound, but stimulation -Valuable in the seen with other β-blockers
block stimulation of the of β1 and treatment of
receptor by EPINEPHRINE and β2) diabetics
NE
Labetalol -Produces peripheral α and β -Useful in treating -Labetalol may be -Orthostatic hTN
Carvedilol vasodilation, thereby reducing antagonists HTN pts for whom administetered -Dizziness
BP increased peripheral through IV and can
-Carvedilol: decreases lipid vascular resistance is rapidly lower BP
peroxidation and vascular wall undesirable (elderly,
thickening black ppl)
-Labetalol:
pregnancy-induced
HTN, hypertensive
emergencies
-CHF
Reserpine -Blocks the Mg2+/ATP- -Slow onset
dependent transport of NE, -Long duration of
DA, serotonin from the action
cytoplasm into storage -Effects that persist for
vesicles many days after
-Sympathetic function is discontinuation
impaired
Guanethidine -Blocks the release of stored -Orthostatic
NE and displaces NE from hypotension
storage vesicles -Interferes w/ male
sexual function
-Hypertensive crisis in
pts with
pheochromocytoma
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