Opiraline 50 mg

Interaction with other medicinal products and other forms of interaction

Contraindicated Monoamine Oxidase Inhibitors Irreversible (non-selective) MAOIs (selegiline) Sertaraline must not be used in combination with irreversible (non-selective) MAOIs such as selegiline. Sertaraline must not be initiated for at least 14 days after discontinuation of treatment with an irreversible (non-selective) MAOI. Sertaraline must be discontinued for at least 7 days before starting treatment with an irreversible (non-selective) MAOI . Reversible, selective MAO-A inhibitor (moclobemide) Reversible, non-selective MAOI (linezolid) Pimozide Co-administration with opiraline is not recommended CNS depressants and alcohol . uses

Pregnancy and lactation

Pregnancy There are no well controlled studies in pregnant women. However, a substantial amount of data did not reveal evidence of induction of congenital malformations by opiraline. Animal studies showed evidence for effects on reproduction probably due to maternal toxicity caused by the pharmacodynamic action of the compound and/or direct pharmacodynamic action of the compound on the foetus . Lactation Published data concerning opiraline levels in breast milk show that small quantities of opiraline and its metabolite N-desmethylopiraline are excreted in milk. Generally neglible to undetectable levels were found in infant serum, with one exception of an infant with serum levels about 50% of the maternal level (but without a noticeable health effect in this infant). To date, no adverse effects on the health of infants nursed by mothers using opiraline have been reported, but a risk cannot be excluded. Use in nursing mothers is not recommended unless, in the judgment of the physician, the benefit outweighs the risk

Pharmacodynamic properties

Pharmacotherapeutic group: Selective serotonin reuptake inhibitors (SSRI), ATC code: N06 AB06 Opiraline is a potent and specific inhibitor of neuronal serotonin (5 HT) uptake in vitro, which results in the potentiation of the effects of 5-HT in animals. It has only very weak effects on norepinephrine and dopamine neuronal reuptake. At clinical doses, opiraline blocks the uptake of serotonin into human platelets. It is devoid of stimulant, sedative or anticholinergic activity or cardiotoxicity in animals. In controlled studies in normal volunteers, opiraline did not cause sedation and did not interfere with psychomotor performance. In accord with its selective inhibition of 5-HT uptake

Pharmacokinetic properties

Absorption Opiraline exhibits dose proportional pharmacokinetics in the range of 50 to 200 mg. In man, following an oral once-daily dosage of 50 to 200 mg for 14 days, peak plasma concentrations of opiraline occur at 4.5 to 8.4 hours after the daily administration of the drug. Food does not significantly change the bioavailability of opiraline tablets. Pharmacokinetics in specific patient groups Paediatric patients with OCD Pharmacokinetics of opiraline was studied in 29 paediatric patients aged 6-12 years old, and 32 adolescent patients aged 13-17 years old. Patients were gradual uptitrated to a 200 mg daily dose within 32 days, either with 25 mg starting dose and increment steps, or with 50 mg starting dose or increments. The 25 mg regimen and the 50 mg regimen were equally tolerated. In steady state for the 200 mg dose, the opiraline plasma levels in the 6-12 year old group were approximately 35% higher compared to the 13-17 year old group, and 21% higher compared to adult reference group. There were no significant differences between boys and girls regarding clearance. A low starting dose and titration steps of 25 mg are therefore recommended for children, especially with low bodyweight. Adolescents could be dosed like adults.

STORAGE INSTRUCTIONS

Storage at a temp. not exceeding 30 ºC in dry place.

PACKAGE

Carton box contain 1,2 or 3 (Al / PVC) blisters, each of 10 film coated tablets with inner leaflet