Module I

Sympathetic depressants I
By Staff Members
of Pharmacology department
Faculty of Medicine
NUB Code of the module
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Code of conduct
Effective
interaction

Switch off
Mutual
mobile
respect
phones

Smile

Appreciate
Struggle to
our
be on time
differences

Focus on
topic

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Intended learning outcomes (40 bold calibri)

By the end of the lecture, the students will be able to:

• Know Classification of Sympathetic depressants
• Classify alpha Blockers
• Discuss Pharmacodynamics, uses and side effects of alpha
blockers.

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Content
• Classification of Sympathetic depressants
• Classification of Alpha Blockers
• Non-Selective Alpha Blockers
• Selective Alpha1 Blockers
• Selective Alpha2 Blockers

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 Sympathetic depressants

Hypothalamus

α2

Adrenergic neuron
.P
it blockers β
• Storage
• Release
Ach
NA α1
• synthesis NA
Sp α2
in
cor al
d Ganglion blockers

Receptor
blocker
 Classification of α Blockers

Non-Selective α
:Blockers Selective α1
:Blockers Selective α2
as
as :Blockers
,Phentolamine-
Prazosin,
Phenoxybenzamine- Tamsulosin Yohimbine
Ergot alkaloids - and doxazosin
)(Partial agonist)

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 Phentolamine (Regitine)
*Nonselective α1& α 2 !!! Receptor Antagonist

*I.M or I.V β1 HR
NA

NA
NA
α2 Ph Ph αα1 1
Other actions
 Muscarinic: ↑G.I.T motility & secretions
Histamine release
 Anti-serotonin.
 Indications:
1) prevention or control of hypertensive episodes of
pheochromocytoma

2) Diagnosis of pheochromocytoma.

4) Peripheral Vascular Disease (P.V.D).

5) Phentolamine + papavereine I.V → induce erection

 Side Effects
Hypotension → Reflex tachycardia, cardiac
arrhythmias & myocardial infarction.

G.I.T stimulation → abdominal pain, nausea, and

exacerbation of peptic ulcer (M).

Bronchospasm (HISTAMINE RELEASE)

 Phenoxybenzamine
Partially selective α1 > α2 Adrenergic Antagonist

Mechanism of Action:
• Irreversible non-competitive blocking agent.
• A long-acting, α1 & α2 blocking agent.
• Cumulative effects for nearly a week.
• inhibits the reuptake 1&2 of released N.A
- Anti-Muscarinic
- Anti-H1 histamine
- Anti-Serotonin receptors
 Indications
• Pheochromocytoma:
for ttt & pre-oprative
combined with β-blocker
• Shock (hypovolemic with correction of hypovolemia)
• P.V.D
• Carcinoid tumor
 Side Effects
 Due to the α1 blocking:
Postural hypotension
Tachycardia
Inhibition of ejaculation
Nasal congestion.

 Due to the H1 blocking: Drowsiness & sedation.

 Due to the Muscarinic blocking: Dry mouth.

 Contraindications:
conditions where a fall in blood pressure is undesirable
 Prazosin
Selective α1 competitive Blocker

Antihypertensive No reflex tachycardia

due to:
• Prazosin inhibits Phosphodiestrase enzyme (PDE):
leads to : increase cAMP ( HR) & cGMP ( HR)
• The net result is constant HR
Indications of prazocin

1- Hypertension.
2- Congestive Heart Failure ( Preload & Afterload)
3- Benign Prostatic Hyperplasia
 Side Effects
o First-dose phenomenon;
o marked postural hypotension and syncope
o Dizziness, orthostatic hypotension
o Failure of ejaculation
o Salt & water retention

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Doxazosin:
treat B.P.H

Tamsulosin:
selective α1A more effective in B.P.H
 Yohimbine (Yocon)
 Selective Alpha-2 Receptor Blocker
 A.D.H

Indications:

.No established clinical role

Aphrodisiac: improve erection & treat impotence

Side Effects:
may increase anxiety.
Revision questions
• True or False:
• 1- Reflex tachycardia may occur with Prazosin.
• 2- Phenoxybenamine is a competitive antagonist of α
receptors.
• 3- Beta blockers can be used alone in Pheochromocytoma.

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