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.-Alpha 2 Adrenergic Medication for Hypertension .-Adrenergic medications mechanism of actions and their side effects, and ad
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1Q).

Centrally acting sympatholytics block the sympathetic activity within the brain by the activation of alpha 2 (α2)- adrenoceptors. This results in decreased sympathetic outflow to the heart, which decreases the heart rate and force of contraction. Centrally acting sympatholytics also decreases the systemic vascular resistance and causes vasodilatation, which decreases arterial pressure.

These drugs are not generally used as first line drugs in the treatment of hypertension due to their side effects that include sedation, dry mouth, bradycardia, impotence and orthostatic hypotension. They are given in conjugation with diuretics to avoid fluid accumulation and edema.

2Q).

The neurotransmission of noradrenaline occurs through the following adrenergic receptors:

· Alpha 1 receptors

· Alpha 2 receptors

· Beta 1 receptors

· Beta 2 receptors

Alpha 1 receptors are present in the eyes, visceral vessels, skeletal muscles, liver and the intestinal smooth muscles. The stimulation of alpha 1 receptors causes the constriction of peripheral vascular smooth muscles and pupil dilatation. The alpha 1 antagonists (prazosin) are used in the treatment of urinary retention in benign prostatic hypertrophy (BPH).

The alpha 2 receptors are presynaptic receptors, stimulation of alpha 2 receptors prevent the release of norepinephrine. This is an auto-regulatory mechanism of norepinephrine secretion.

Beta 1 receptors are present in the heart. The stimulation of beta 1 receptors causes an increase in rate of contraction and also the force of contraction of the heart. Excess stimulation of beta 1 receptors causes tachycardia. Thus, beta antagonists are used in the treatment of hypertension and cardiac arrhythmias. Atenolol is a selective inhibitor of beta 1 receptors, used in the treatment of hypertension.

The beta 2 receptors are present in the arterioles, bronchial smooth muscles and the liver. The stimulation of beta 2 receptors causes relaxation of bronchial smooth muscle and uterine smooth muscle. Thus, the beta 2 agonists are used in the treatment of bronchoconstriction and to delay the pregnancy or to prevent premature birth. Salbutamol is the selective agonist of the beta 2 receptors, which is used in the treatment of asthma.

3Q).

Beta blockers: Selective β1 blockers are used in the treatment of hypertension.

Beta-blockers inhibit the binding of noradrenaline and adrenaline to the beta adrenoceptors, which blocks the normal sympathetic effects mediated through these receptors.

Blockade of β1 receptors prevent the formation of cAMP through the inhibition of adenylate cyclase (AC). Inhibition of Camp formation further inhibits the protein kinase A, and decreases intracellular calcium levels. Decreased calcium results in decreased heart rate and force of contraction. Postural hypotension is the general adverse effect.

Adrenoceptors of β2 type causes relaxation of bronchial smooth muscle. Non-selective beta blockers produce sides effects, especially are contraindicated in asthma patients. General side effects produced by beta blockers include bradycardia, block of AV nodal conduction, hypotension, etc.

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