AUTONOMIC DRUGS (Adrenergic and Antiadrenergic Drugs) Presented by Sasan Zaeri (PharmD, PhD)

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AUTONOMIC DRUGS(Adrenergic and Antiadrenergic
Drugs)Presented by Sasan Zaeri (PharmD, PhD)
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Adrenergic Agonists
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Direct acting adrenergic drugs
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Location Receptor type Effect
Heart ?1, ß2 ? heart rate ? force of contraction
Vascular Smooth Muscle
Skin and splanchnic vessels a1 constriction
Skeletal muscle vessels ß2 dilation
Other smooth muscle
Bronchiole ß2 dilation
Uterine ß2 relaxation
GI tract a and ß relaxation
Eye
Radial pupillary dilator a1 contraction (mydriasis)
Ciliary epithelium ß ? secretion of aqueous humor
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Beta I Receptor Activation

• Beta 1 receptors are located in the heart
• Therapeutic uses
• Cardiac arrest
• Heart failure
• Shock
• Atrioventricular (AV) block

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Beta II Receptor Activation

• Beta 2 receptors are located in the lung and
  uterine
• Therapeutic uses
• Asthma
• Delaying of preterm labor

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Alpha I Receptor Activation

• Alpha 1 response Constriction of blood vessels
  mydriasis
• Therapeutic uses
• Vasoconstriction
• Mydriasis
• Nasal or ophthalmic decongestion

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Alpha II Receptor Activation

• Alpha 2 receptors are located pre-synaptically
• Activation inhibits NE release
• Activation of alpha2 receptors in CNS is very
  important causes reduction of sympathetic
  response in heart and blood vessels

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Indications for use of adrenergic drugs

• Cardiac arrest
• Cardiac stimulant (ß1)
• Hypotension and shock
• Increase blood pressure (a1)
• Asthma
• Bronchodilators (ß2)
• Ophthalmic or nasal congestion
• Decongestant (a1) (oral or topical decongestant)
• Prevention of preterm labor
• Tocolytic (ß2)

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Properties of Representative Adrenergic Agonists

• Epinephrine
• Therapeutic uses
• To cause vasoconstriction
• Treatment of sever asthma
• Treatment of anaphylactic shock

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Phenylephrine

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• Salbutamol
• Selective ß2 agonist
• Dilates bronchial smooth muscle
• Clinical use
• Antiasthmatic

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• dobutamine ? isoproterenol
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• Antiadrenergic Drugs

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ADRENERGIC BLOCKING DRUGS

• Also called sympatholytic drugs
• Classified according to their site of action
• a adrenergic antagonists
• ß adrenergic antagonists
• a2 adrenergic agonists

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a antagonists

• Phenoxybenzamine
• Irreversible antagonist
• Used to treat pheochromocytoma (catecholamine-secr
  eting tumour of the chromaffin tissue)
• Prazocin
• Relaxes the smooth muscle in the blood vessels
  increases dilation of blood vessels and
  decreases blood pressure
• Caution orthostatic hypotention

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ß-Adrenergic Blockers

• Are selective or nonselective
• Nonselective beta-blockers affect beta1 receptor
  sites located mainly in the heart and beta2
  receptor sites located in the bronchi, blood
  vessels, and uterine
• Propanolol

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ß-Adrenergic Blockers

• Selective beta-blockers primarily affect beta1
  receptor
• Atenolol and metoprolol

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ß-Adrenergic Blockers

• Effects on the heart include
• decreased heart rate
• decreased force of heart contractions
• decreased blood pressure

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ß-Adrenergic Blockers

• Clinical uses
• Ischemic heart disease
• ? HR and force of contraction
• Lessens work of heart
• Hypertension
• Arrhythmias

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ß-Adrenergic Blockers

• Also used to treat
• Tremor
• Stage fright
• Cardiovascular symptoms associated with
  thyrotoxicosis
• Migraine headaches
• Glaucoma

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ß-Adrenergic Blockers

• Caution for diabetics
• ß antagonists will suppress glycogenolysis and
  delay recovery during hypoglycemic episodes
• Any ß antagonist will mask tachycardia a
  warning sign of hypoglycemic events
• ß1 selective antagonist is better choice

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ß-Adrenergic Blockers

• Adverse effects
• Bradycardia and heart block
• Bronchospasm
• Drug interactions
• Other antihypertensive agents
• Insulin and oral hypoglycemic agents