Etoperidone
Etoperidone Uses, Dosage, Side Effects, Food Interaction and all others data.
Etoperidone is an atypical antidepressant introduced in Europe in 1977. It is a phenylpiperazine-substituted triazole derivative with a composition that classifies it as an analog of tradozone and presents a similar pharmacological profile. Etoperidone was developed by Angelini Francesco ACRAF and even nowadays, there is uncertanty if this drug ever reached the market.
Etoperidone has a biphasic effect on the central transmission of serotonin. It presents the capacity to inhibit serotonin receptor but also to inhibit the reuptake of serotonin, norepinephrine and dopamine. As part of its actions, etoperidone also inhibits the α-adrenergic receptors which directly corresponds to the sedative and cardiovascular effects. The presence of both effects caused that the effective dose of etoperidone was poorly tolerated thus, efforts have been made to separate the serotonergic and adrenergic functions in order to generate etoperidone-derivatives like nefazodone.
| Trade Name | Etoperidone |
| Generic | Etoperidone |
| Etoperidone Other Names | Etoperidone |
| Type | |
| Formula | C19H28ClN5O |
| Weight | Average: 377.92 Monoisotopic: 377.1982382 |
| Protein binding | Etoperidone presents an extensive plasma protein binding. |
| Groups | Withdrawn |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Etoperidone has been studied for the treatment of depression, tremors in Parkinson, extrapyramidal symptoms and male impotence. It is not certain if it was ever approved and marketed but its current status is withdrawn.
How Etoperidone works
The activity of etoperidone is made mainly by its major metabolite 1-(3'-chlorophenyl)piperazine (mCPP). mCPP binds with different affinity to most of the serotonergic receptors and adrenergic receptors. This metabolite is an agonist of 5-HT2c and an antagonist of 5-HT2a. Part of etoperidone structure contibutes to the activity in the α-adrenergic receptors.
Toxicity
Etoperidone presented major cardiovascular effects recorded as abnormal electrocardiogram, changes in blood pressure and even cardiac arrest. From the changes in blood pressure hypotension was the primary effect. These cardiovascular reactions are consistent with its effect to catecholamines.
Volume of Distribution
The high protein binding presented in etoperidone modulates its volume of distribution to a range of 0.23 to 0.69 L/kg.
Elimination Route
The absorption and bioavailability is highly variable between individuals and can be as low as 12%. The lower bioavailability is explained due to its high metabolism. The mean time to peak plasma concentration is ranged from 1.4-4.8 hours.
Half Life
After oral administration of etoperidone the terminal half-life was 21.7 hours.
Clearance
The apparent clearance of etoperidone was 1.01 ml/min.
Elimination Route
The elimination of an oral dose of etoperidone presents a division of 78.8% found in urine and 9.6% found in faeces. On the elimination route, less than 0.01% of the etoperidone dose is represented by the unchanged drug while the rest is formed by 21 different metabolites.
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