Alpha Blockers

ALPHA BLOCKERS
 PHENOXYBENZAMINE
 irreversible blockade Binds alpha1 and 2

receptors
 Dilates veins more than arteries.
 Long duration of action (20-48 hrs)

 Crosses BBB
 Use – Pheochromocytoma- given 1mg /kg

slow iv – surgical manipulation.
 Malignant pheochromocytoma &

inoperable cases- along with metyrosine
prolonged t/t
 Peripheral vascular dz- (10mg tds)
 ADR- Postural hypotension, reflex

tachycardia, salt and water retention,
impotency, sedation, fatigue, nausea.
 PHENTOLAMINE & TOLAZOLINE
 Competitive antagonist of alpha1 & 2 receptors.

 dilates veins more than arteries.
 Poor oral absorption, give i/v- Phentolamine

 Immediate onset of action, shorter duration of action-
Phentolamine.
 Tolazoline – better git absorption but less potent, rarely

used nowadays.
 Diagnosis of pheochromocytoma- 5mg iv- fall in BP by 25-35

mm of Hg- case of pheochromocytoma, if less case of
essential HTN,
 Peripheral vascular dz, to prevent dermal necrosis,

hypertensive crisis ( clonidine withdrawal, cheese
reaction).
 ADR- Postural hypotension, reflex tachycardia, impotency.

SELECTIVE ALPHA1 BLOCKERS
PRAZOSIN
 Selective alpha1 blocker. ( prototypical drug).
 Similar affinity for alpha1 subtypes.
 Block alpha1 receptors on arterioles and veins- fall in PVR & venous
return- fall in BP (dilates arterioles more than veins)
 But less tachycardia- it lacks alpha2 blocking property hence do not

promote NE release (CNS & periphery), also decrease preload and
thus have little tendency to increase CO & HR.
 Also a potent PDEs inhibitor – rise in cAMP- vasodilatation.
 Increase HDL, decrease LDL & TG.
 T1/2= 4hrs
 Uses- HTN, BPH, peripheral vascular disease
 ADR – postural hypotension, impotency, nasal congestion, git upset,
sodium water retention.
 TERAZOSIN AND DOXAZOSIN
CONT….
 Structural analogues of Prazosin, but less potent.
 Alpha1 blockers, longer duration of action.
 Terazosin t1/2= 12hrs
 Doxazosin t1/2= 20hrs
 Better patient compliance – once daily dose.
 Use- HTN, BPH
 Faster action to improve urine flow- adv. in BPH
 There is some evidence that these two drugs promote

apoptosis in prostate – quinazoline moiety- better than
finasteride in t/t of BPH.
CONT…
ALFUZOSIN
 Quinazoline based
alpha1 antagonist.
 t1/2= 4hrs
 It is not approved for

treatment of HTN.
 Primarily used in BPH.

SUBTYPE SPECIFIC
 Tamsulosin – alpha1a & 1d
selective antagonist.
 More efficacious in treating BPH

with little effect on BP.
 Not approved for t/t of HTN.
 T1/2= 8hrs
 side effects- Abnormal

ejaculation.
 Silodosin- longer acting

analogue of tamsulosin.
ALPHA2 BLOCKER
 YOHIMBINE
 Structure resembles that of
Reserpine.
 Lipid soluble, crosses BBB.
 Also has 5HT antagonist activity.
 Promote NE release.
 theoretically used to treat

autonomic insufficiency.
 male sexual dysfunction (in past),

diabetic neuropathy, postural
hypotension- other uses ( studies)
CONT….
 In US it is legally
sold as dietary
supplement.
 Veterinary use –
reversal of xylazine
anaesthesia.
USES
Pheochromocytoma:
Tumor of adrenal medullary
cells.
Excess CA- persistent HTN
Diagnosis : Estimation of
CA metabolites
Phentolamine test- 5mg iv

Treatment: Phenoxybenzamine – definitive
therapy for inoperable/malignant cases, surgical
manipulation.
orally 1-2 wks prior to surgery & iv during surgery
 normalize blood volume and distribution of body

water .
 reduces risk of outpouring of CA during removal
 After removal, risk of marked fall in BP due to

vasodil. & low body volume this will not happen if
volume is restored before hand with alpha
blockers.
HYPERTENSION
 Alpha1 selective drugs- Prazosin
preferred due to less adverse.
 Lowers blood pressure by
blocking Alpha 1 receptors on
the arterioles and veins. This
causes the arterioles and veins
to dilate, which lowers the
blood pressure
 Phentolamine/phenoxybenzamine -
to control BP during clonidine
withdrawal & cheese reaction
 Classical alpha blockers- postural

hypotension, reflex tachycardia limits
its use in essential HTN.
BPH
OTHER USES
 Secondary shock due to blood/fluid loss
counteract vasoconstriction,
shift blood from pulmonary to systemic circulation,
return fluid from extravascular to vascular comp. →
improves CO.
 PVD-----helpful when vasoconstriction is prominent ;

symptomatic relief in Raynaud’s dz & acrocynosis.
 CHF- can be helpful in short term, alpha1 selective

antagonist.
 vasodilatation of both arteries and veins resulting in a
reduction of both preload and after load- increase in CO
& reduction in pulmonary congestion.
ADVERSE EFFECTS
 Orthostatic hypotension
 Reflex tachycardia
 Impotency, abnormalities in ejaculation
 Nasal congestion
 Dizziness
 Headache
THANK YOU

Alpha Blockers

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ALPHA BLOCKERS

 irreversible blockade Binds alpha1 and 2

 Long duration of action (20-48 hrs)

 Use – Pheochromocytoma- given 1mg /kg

 Malignant pheochromocytoma &

 Peripheral vascular dz- (10mg tds)

 ADR- Postural hypotension, reflex

 Competitive antagonist of alpha1 & 2 receptors.

 Poor oral absorption, give i/v- Phentolamine

 Tolazoline – better git absorption but less potent, rarely

 Diagnosis of pheochromocytoma- 5mg iv- fall in BP by 25-35

 Peripheral vascular dz, to prevent dermal necrosis,

 ADR- Postural hypotension, reflex tachycardia, impotency.

 Selective alpha1 blocker. ( prototypical drug).

 Similar affinity for alpha1 subtypes.

 But less tachycardia- it lacks alpha2 blocking property hence do not

 Alpha1 blockers, longer duration of action.

 Terazosin t1/2= 12hrs

 Doxazosin t1/2= 20hrs

 Better patient compliance – once daily dose.

 Use- HTN, BPH

 Faster action to improve urine flow- adv. in BPH

 There is some evidence that these two drugs promote

 It is not approved for

 Primarily used in BPH.

 More efficacious in treating BPH

 Not approved for t/t of HTN.

 side effects- Abnormal

 Silodosin- longer acting

 theoretically used to treat

 male sexual dysfunction (in past),

Excess CA- persistent HTN

Phentolamine test- 5mg iv

orally 1-2 wks prior to surgery & iv during surgery

 normalize blood volume and distribution of body

 reduces risk of outpouring of CA during removal

 After removal, risk of marked fall in BP due to

 Classical alpha blockers- postural

 PVD-----helpful when vasoconstriction is prominent ;

 CHF- can be helpful in short term, alpha1 selective

 Impotency, abnormalities in ejaculation

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