Phenoxypropazine
Overview
Phenoxypropazine is a monoamine oxidase inhibitor (MAOI) that was used as an antidepressant in the treatment of major depressive disorder. It belongs to the class of non-selective and irreversible MAOIs, which work by inhibiting the activity of the enzyme monoamine oxidase, thereby increasing the levels of neurotransmitters such as serotonin, norepinephrine, and dopamine in the brain.
Mechanism of Action
Phenoxypropazine functions by binding to the active site of the monoamine oxidase enzyme, preventing it from breaking down monoamine neurotransmitters. This leads to an increase in the availability of these neurotransmitters in the synaptic cleft, which is thought to contribute to its antidepressant effects. The inhibition of monoamine oxidase by phenoxypropazine is irreversible, meaning that the enzyme is permanently deactivated and new enzyme synthesis is required to restore its activity.
Clinical Use
Phenoxypropazine was primarily used in the treatment of major depressive disorder, particularly in patients who did not respond to other types of antidepressants. However, due to the risk of serious side effects and dietary restrictions associated with MAOIs, its use has declined with the development of newer antidepressants with more favorable safety profiles.
Side Effects
The use of phenoxypropazine, like other MAOIs, is associated with a range of side effects. Common side effects include orthostatic hypotension, insomnia, and weight gain. More serious side effects can occur, such as hypertensive crisis when foods containing tyramine are consumed. Patients taking phenoxypropazine must adhere to dietary restrictions to avoid these potentially life-threatening reactions.
Interactions
Phenoxypropazine can interact with a variety of other medications, leading to serious adverse effects. It should not be used in combination with other antidepressants, particularly selective serotonin reuptake inhibitors (SSRIs) or tricyclic antidepressants (TCAs), due to the risk of serotonin syndrome. Additionally, it can interact with certain over-the-counter medications, such as decongestants, which can also lead to hypertensive crises.
Discontinuation
Due to the development of newer antidepressants with improved safety profiles and fewer dietary restrictions, the use of phenoxypropazine has largely been discontinued. It is no longer commonly prescribed, and its use is limited to specific cases where other treatments have failed.
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Contributors: Prab R. Tumpati, MD