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פבוקסיל 50 FAVOXIL 50 (FLUVOXAMINE MALEATE)

תרופה במרשם תרופה בסל נרקוטיקה ציטוטוקסיקה

צורת מתן:

פומי : PER OS

צורת מינון:

טבליה : TABLETS

Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1    Pharmacodynamic properties
Pharmacotherapeutic group: Antidepressants, Selective serotonin reuptake inhibitors ATC code: N06AB08

The mechanism of action of fluvoxamine is thought to be related to selective serotonin re-uptake inhibition in brain neurones. There is minimum interference with noradrenergic processes. Receptor binding studies have demonstrated that fluvoxamine has negligible binding capacity to alpha adrenergic, beta adrenergic, histaminergic, muscarine cholinergic, dopaminergic or serotonergic receptors.

In a placebo controlled trial in 120 patients with OCD, aged between 8 and 17 years, a statistically significant improvement was seen in the total population in favour of fluvoxamine at 10 weeks. A further subgroup analysis showed improvement on the C- YBOCS rating scale in children whereas no effect was seen in adolescents. The mean dose was respectively 158 mg and 168 mg/day.

Dose response

No formal clinical trials were conducted investigating the dose response of fluvoxamine. However, it is clinical experience that up-titrating the dose might be beneficial for some patients.

Pharmacokinetic Properties

5.2    Pharmacokinetic properties
Absorption

Fluvoxamine is completely absorbed following oral administration. Maximum plasma concentrations occur within 3-8 hours of dosing. The mean absolute bioavailability is 53% due to first-pass metabolism.
The pharmacokinetics of fluvoxamine is not influenced by concomitant food intake.
Distribution

In vitro plasma protein binding of fluvoxamine is 80%. Volume of distribution in humans is 25 l/kg.

Metabolism

Fluvoxamine undergoes extensive metabolism in the liver. Although CYP2D6 is in vitro the main isoenzyme involved in fluvoxamine’s metabolism, plasma concentrations in poor metabolisers for CYP2D6 are not much higher than those in extensive metabolisers.

The mean plasma half-life is approximately 13-15 hours after a single dose and slightly longer (17-22 hours) during repeated dosing,when steady-state plasma levels are usually achieved within 10-14 days.

Fluvoxamine undergoes extensive hepatic transformation, mainly via oxidative demethylation, into at least nine metabolites, which are excreted by the kidneys. The two major metabolites showed negligible pharmacological activity. The other metabolites are not expected to be pharmacologically active. Fluvoxamine is a potent inhibitor of CYP1A2 and CYP2C19. A moderate inhibition was found for CYP2C9, CYP2D6 and CYP3A4.

Fluvoxamine displays linear single-dose pharmacokinetics. Steady-state concentrations are higher than calculated from single-dose data, and this disproportional increase is more pronounced with higher daily doses.

Special Patients groups

The pharmacokinetics of fluvoxamine is similar in healthy adults, elderly patients, and patients with renal insufficiency. The metabolism of fluvoxamine is impaired in patients with liver disease.
Steady-state plasma concentrations of fluvoxamine were twice as high in children (aged 6-11) as in adolescents (aged 12-17). Plasma concentrations in adolescents are similar to those in adults.

שימוש לפי פנקס קופ''ח כללית 1994 Depressive illness. יירשם ע"י רופא פסיכיאטר ורופא עצבים
תאריך הכללה מקורי בסל 01/01/1995
הגבלות תרופה מוגבלת לרישום ע'י רופא מומחה או הגבלה אחרת

רישום

041 92 25727 00

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0 ₪

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פבוקסיל 50

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