Opipramol, sold under the brand name Insidon among others, is an anxiolytic and tricyclic antidepressant that is used throughout Europe.
Medical uses
Opipramol is typically used in the treatment of generalized anxiety disorder (GAD) and somatoform disorders.
Preliminary studies suggest that opipramol shows potential clinical significance in the treatment of severe
Bruxism.
Contraindications
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In patients with hypersensitivity to opipramol or another component of the formulation
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Acute alcohol, sedative, analgesic, and antidepressant intoxications
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Acute urinary retention
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Acute delirium
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Untreated glaucoma
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Benign prostatic hyperplasia with residual urinary retention
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Paralytic ileus
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Pre-existing higher-grade atrioventricular blockages or diffuse supraventricular or ventricular stimulus conduction disturbances
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Combination with monoamine oxidase inhibitor (MAOI)
Pregnancy and lactation
Experimental animal studies did not indicate injurious effects of opipramol on the embryonic development or
fertility. Opipramol should only be prescribed during pregnancy, particularly in the first trimester, for compelling indication.
It should not be used during
lactation and
breastfeeding, since it passes into
breast milk in small quantities.
Side effects
Frequently (≥1% to <10%) reported adverse reactions with opipramol, especially at the beginning of the treatment, include fatigue,
dry mouth, blocked nose,
hypotension, and orthostatic dysregulation.
Adverse reactions reported occasionally (≥0.1% to <1%) include dizziness, stupor, micturition disturbances, vigilance, accommodation disturbances, tremor, weight gain,
Rarely (≥0.01% to <0.1%) reported adverse reactions include excitation, headache, paresthesia especially in elderly patients, restlessness, sweating, sleep disorder, edema, galactorrhea, urine blockage, nausea and vomiting, fever,
Very rarely (<0.01%) reported adverse reactions include seizures, (akathisia, dyskinesia, ataxia), polyneuropathy, glaucoma, anxiety, hair loss, agranulocytosis, severe liver dysfunction after long-term treatment, jaundice, and chronic liver damage.
Overdose
Symptoms of intoxication from
overdose include drowsiness, insomnia, stupor, agitation, coma, transient confusion, increased anxiety, ataxia, convulsions, oliguria, anuria, tachycardia or bradycardia, arrhythmia, AV block, hypotension, shock, respiratory depression, and, rarely, cardiac arrest.
Interactions
While opipramol is not a monoamine reuptake inhibitor, any irreversible MAOIs should still be discontinued at least 14 days before treatment. Opipramol can compete with other tricyclic antidepressants,
, antiarrhythmics (of class 1c), and other drugs for
microsome, which can lead to slower metabolism and higher plasma concentrations of these drugs. Co-administration of
Antipsychotic (e.g.,
haloperidol,
risperidone) can increase the plasma concentration of opipramol.
and
can reduce the plasma concentration of opipramol and thereby weaken its therapeutic effect.
Pharmacology
Pharmacodynamics
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| Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site. |
Opipramol acts as a high affinity sigma receptor agonist, primarily of the σ1 subtype, but also of the σ2 subtype with lower affinity.
Unlike other TCAs, opipramol does not inhibit the reuptake of serotonin or norepinephrine.
Sigma receptors are a set of located in the endoplasmic reticulum.
Pharmacokinetics
Opipramol is rapidly and completely absorbed by the gastrointestinal tract.
The
bioavailability of opipramol amounts to 94%.
After single oral administration of 50 mg, the peak plasma concentration of the drug is reached after 3.3 hours and amounts to 15.6 ng/mL.
After single oral administration of 100 mg the maximum plasma concentration is reached after 3 hours and amounts to 33.2 ng/mL.
Therapeutic concentrations of opipramol range from 140 to 550 nmol/L.
The plasma protein binding amounts to approximately 91% and the volume of distribution is approximately 10 L/kg.
Opipramol is partially
metabolism in the
liver to deshydroxyethylopipramol.
Metabolism occurs through the CYP2D6
isoenzyme.
Its terminal half-life in plasma is 6–11 hours.
About 70% is eliminated in
urine with 10% unaltered.
The remaining portion is eliminated through
feces.
History
Opipramol was developed by
Geigy.
It first appeared in the literature in 1952 and was patented in 1961.
The drug was first introduced for use in medicine in 1961.
Opipramol was one of the first TCAs to be introduced, with
imipramine marketed in the 1950s and
amitriptyline marketed in 1961.
Society and culture
Generic names
Opipramol is the
English language,
German language,
French language, and
Spanish language generic term of the drug and its , , and , while
opipramol hydrochloride is its , , and .
Its generic name in
Italian language and its is
opipramolo and in
Latin language is
opipramolum.
Brand names
Opipramol is marketed under the brand names Deprenil, Dinsidon, Ensidon, Insidon, Insomin, Inzeton, Nisidana, Opipram, Opramol, Oprimol, Pramolan, and Sympramol among others.
