Desacetylmetipranolol
Desacetylmetipranolol
Desacetylmetipranolol is a pharmacologically active metabolite of the beta-blocker metipranolol. It is primarily used in the treatment of glaucoma and other conditions where reduction of intraocular pressure is desired. As a beta-adrenergic antagonist, desacetylmetipranolol works by blocking beta-adrenergic receptors, which are part of the sympathetic nervous system.
Pharmacology
Desacetylmetipranolol is a non-selective beta-adrenergic receptor blocker. This means it can inhibit both beta-1 and beta-2 adrenergic receptors. The blockade of these receptors leads to a decrease in the production of aqueous humor in the eye, thereby reducing intraocular pressure. This mechanism is beneficial in the management of glaucoma, a condition characterized by increased pressure within the eye that can lead to optic nerve damage and loss of vision.
Mechanism of Action
The primary action of desacetylmetipranolol is the competitive inhibition of beta-adrenergic receptors. By blocking these receptors, desacetylmetipranolol reduces the effects of endogenous catecholamines like epinephrine and norepinephrine. This results in decreased heart rate, myocardial contractility, and blood pressure, as well as reduced aqueous humor production in the eye.
Clinical Use
Desacetylmetipranolol is used in the management of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. It is often administered in the form of eye drops, allowing for direct application to the affected area and minimizing systemic absorption and side effects.
Side Effects
Common side effects of desacetylmetipranolol include local irritation, burning sensation in the eyes, and temporary blurred vision. Systemic side effects are rare due to the localized application but can include symptoms associated with beta-blockade such as bradycardia, hypotension, and bronchospasm, especially in patients with pre-existing respiratory conditions like asthma.
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Contributors: Prab R. Tumpati, MD