Desglymidodrine
Desglymidodrine
Desglymidodrine is a pharmacologically active metabolite of the prodrug midodrine, which is used primarily in the treatment of orthostatic hypotension. Desglymidodrine is an alpha-adrenergic agonist, meaning it stimulates alpha-adrenergic receptors, leading to vasoconstriction and an increase in blood pressure.
Pharmacology
Desglymidodrine is formed in the body from midodrine through enzymatic hydrolysis. Once converted, desglymidodrine exerts its effects by selectively activating alpha-1 adrenergic receptors located on the smooth muscle cells of blood vessels. This activation causes the blood vessels to constrict, thereby increasing peripheral vascular resistance and elevating blood pressure.
Mechanism of Action
The primary action of desglymidodrine is its ability to bind to and activate alpha-1 adrenergic receptors. These receptors are part of the sympathetic nervous system and are responsible for mediating vasoconstriction. By activating these receptors, desglymidodrine increases the tone of the vascular smooth muscle, leading to increased blood pressure.
Clinical Use
Desglymidodrine, through its prodrug midodrine, is used in the management of orthostatic hypotension, a condition characterized by a significant drop in blood pressure upon standing. This condition can lead to dizziness, lightheadedness, and even fainting. By increasing blood pressure, desglymidodrine helps to alleviate these symptoms and improve the quality of life for affected individuals.
Side Effects
The use of desglymidodrine can lead to several side effects, primarily due to its vasoconstrictive properties. Common side effects include:
- Hypertension
- Piloerection (goosebumps)
- Urinary retention
- Pruritus (itching)
Patients are advised to monitor their blood pressure regularly to avoid excessive hypertension.
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Contributors: Prab R. Tumpati, MD