Toloxatone

Toloxatone Uses, Dosage, Side Effects, Food Interaction and all others data.

Toloxatone is an antidepressant agent, the first ever use of which was in France, 1984. It acts as a selective and reversible inhibitor of monoamine oxidase-A (MOA) .

This drug has been shown to help manage the symptoms of depression by maintaining neuro-synaptic levels of serotonin and catecholamines while regulating their metabolism, which leads to relief of depressive symptoms .

Trade Name Toloxatone
Generic Toloxatone
Toloxatone Other Names Toloxatone
Type
Formula C11H13NO3
Weight Average: 207.229
Monoisotopic: 207.089543283
Groups Experimental
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Toloxatone
Toloxatone

Uses

For the treatment of major depressive disorder.

How Toloxatone works

This medication is a reversible inhibitor of monoamine oxidase type-A (also known as RIMA).
MAO-A can be found in norepinephrinergic and serotonergic neurons and regulates the metabolism of serotonin and catecholamines, allowing for increased circulation in the synaptic cleft. Traditional monoamine oxidase inhibitors irreversibly inhibit monoamine oxidase and therefore, side effects, drug interactions, and food interactions persist as long as 2-3 weeks after discontinuing toloxatone. The elevation of serotonin and norepinephrine levels occurs rapidly after medication administration. However, the therapeutic relief of depressive symptoms requires weeks of daily treatment to observe results. Selective and reversible MAO-A inhibitors are more effective in treating major depression without several of the drug and food interactions associated with traditional monoamine oxidase inhibitors .

Toxicity

In rare cases, toloxatone toxicity may cause fulminant hepatitis . More common adverse effects include dysuria, nausea, constipation, vertigo, and insomnia. Administration of toloxatone can lead to an increased risk of serotonin syndrome with selective serotonin reuptake inhibitors (SSRI), and tricyclic antidepressants . Increased blood pressure can occur with sympathomimetic medication coadministration. One study showed that when combined with meals, elevated doses of toloxatone may contribute to elevated blood pressure in healthy subjects. This pharmacodynamic interaction could be explained by enhanced tyramine bioavailability in the presence of toloxatone. This tyramine in meals and toloxatone is unlikely to occur in patients after long-term administration of the drug at therapeutic dosages .

Half Life

1-3 h

Clearance

High hepatic excretion rate

Elimination Route

Mainly hepatic 1% of drug is excreted unchanged in the urine

Innovators Monograph

You find simplified version here Toloxatone

*** Taking medicines without doctor's advice can cause long-term problems.
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