Monoamine-depleting agent

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A class of drugs that deplete monoamines in the brain


Overview

A monoamine-depleting agent is a type of pharmacological agent that reduces the levels of monoamines in the central nervous system. Monoamines are a group of neurotransmitters that include serotonin, dopamine, and norepinephrine. These neurotransmitters play a crucial role in regulating mood, arousal, and cognition.

Mechanism of Action

Monoamine-depleting agents work by interfering with the storage and release of monoamines in the synaptic vesicles of neurons. One of the primary mechanisms is the inhibition of the vesicular monoamine transporter (VMAT), which is responsible for transporting monoamines into synaptic vesicles. By inhibiting VMAT, these agents prevent the accumulation of monoamines in the vesicles, leading to their depletion in the synaptic cleft.

Clinical Uses

Monoamine-depleting agents are used in the treatment of various psychiatric and neurological disorders. They are particularly effective in managing conditions such as hypertension, schizophrenia, and Huntington's disease.

Hypertension

In the treatment of hypertension, monoamine-depleting agents help lower blood pressure by reducing the levels of norepinephrine, which decreases sympathetic nervous system activity.

Schizophrenia

For patients with schizophrenia, these agents can help alleviate symptoms by reducing dopamine levels, which are often elevated in this condition.

Huntington's Disease

In Huntington's disease, monoamine-depleting agents can help manage chorea, a movement disorder associated with the disease, by depleting dopamine.

Side Effects

The use of monoamine-depleting agents can lead to several side effects due to the reduction of monoamines. Common side effects include depression, sedation, and gastrointestinal disturbances.

Examples

One of the most well-known monoamine-depleting agents is reserpine. Reserpine is derived from the Rauwolfia serpentina plant and has been used historically in the treatment of hypertension and psychotic disorders.

Chemical structure of Reserpine

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Contributors: Prab R. Tumpati, MD