opipramol opipramol opipramol, sold under the brand name insidon among others, is an anxiolytic and tricyclic antidepressant that is used throughout europe. despite chemically being a tricyclic dibenzazepine (iminostilbene) derivative similar to imipramine, opipramol is not a monoamine reuptake inhibitor like most other tricyclic antidepressants, and instead, uniquely among antidepressants, acts primarily as a sigma receptor agonist. it was developed by schindler and blattner in 1961. opipramolclinical datatrade namesinsidon, othersother namesg-33040; rp-8307ahfs/drugs.cominternational drug namesroutes ofadministrationoralatc coden06aa05 (who) legal statuslegal status in general: ℞ (prescription only) pharmacokinetic databioavailability94%protein binding91%metabolismcyp2d6-mediatedelimination half-life6–11 hoursexcretionurine (70%), feces (10%)identifiers iupac name 4-azepin- 5-yl)propyl]-1-piperazinethanol cas number315-72-0 n 909-39-7 (dihydrochloride)pubchem cid9417chemspider9046 yuniid23zxo613ckeggd08297 ychemblchembl370753 ycomptox dashboard (epa)dtxsid3023394 echa infocard100.005.687 chemical and physical dataformulac23h29n3omolar mass363.505 g·mol−13d model (jsmol)interactive image smiles occn1ccn(cc1)cccn4c2ccccc2\c=c/c3ccccc34 inchi inchi=1s/c23h29n3o/c27-19-18-25-16-14-24(15-17-25)12-5-13-26-22-8-3-1-6-20(22)10-11-21-7-2-4-9-23(21)26/h1-4,6-11,27h,5,12-19h2 ykey:ynzfuwzugrbmhl-uhfffaoysa-n y ny (what is this?) (verify) 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 sleep bruxism. contraindications in patients with hypersensitivity to opipramol or another component of the formulation acute alcohol, sedative, analgesic, and antidepressant intoxications acute urinary retention acute delirium untreated narrow-angle glaucoma benign prostatic hyperplasia with residual urinary retention paralytic ileus pre-existing higher-grade atrioventricular blockages or diffuse supraventricular or ventricular stimulus conduction disturbances 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, thirst, allergic skin reactions (rash, urticaria), abnormal ejaculation, erectile impotence, constipation, transient increases in liver enzymes, tachycardia, and palpitations. rarely (≥0.01% to <0.1%) reported adverse reactions include excitation, headache, paresthesia especially in elderly patients, restlessness, sweating, sleep disturbances, edema, galactorrhea, urine blockage, nausea and vomiting, fever, collapse conditions, stimulation conducting disturbances, intensification of present heart insufficiency, blood profile changes particularly leukopenia, confusion, delirium, stomach complaints, taste disturbance, and paralytic ileus especially with sudden discontinuation of a longer-term high-dose therapy. very rarely (<0.01%) reported adverse reactions include seizures, motor disorders (akathisia, dyskinesia, ataxia), polyneuropathy, glaucoma, anxiety, hair loss, agranulocytosis, severe liver dysfunction after long-term treatment, jaundice, and chronic liver damage. overdose main article: tricyclic antidepressant 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. since no antidote for tricyclic antidepressant overdose is known, its treatment remains largely supportive. removal of the drug should be facilitated by vomiting or gastric lavage. cardiovascular function should be monitored continuously for at least 48 hours. arrhythmias should be treated on a case-by-case basis with an appropriate pacemaker and correction of metabolic irregularities, particularly electrolyte imbalances. respiratory failure should be managed by intubation and artificial respiration. convulsions should be managed with anticonvulsants (typically diazepam), while monitoring for any worsening in cns depression. hypotension can be treated by assuming the corresponding recovery position, by increasing plasma volume with saline infusions, or by pressors, such as adrenaline or dobutamine. interactions opipramol can be co-prescribed with other psychiatric drugs, such as antidepressants, anxiolytics and antipsychotics, in which case it can interact with them. most problematic interactions are generally additive or synergistic, such that, when drugs are combined, their effects intensify, which usually manifests as an increase in side effects, but can also be dangerous, depending on the drugs involved. 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 tcas, beta blockers, antiarrhythmics (of class 1c) and other drugs for microsomal enzymes, which can lead to slower metabolism and higher plasma concentrations of these drugs. co-administration of antipsychotics (e.g., haloperidol, risperidone) can increase the plasma concentration of opipramol. barbiturates and anticonvulsants, on the other hand, can reduce the plasma concentration of opipramol and thereby weaken its therapeutic effect. pharmacology pharmacodynamics