The mechanism of action of Luvox is associated with selective inhibition of serotonin reuptake by neurons of the brain and is characterized by a minimal effect on the noradrenergic system. Proprionate has a poor ability to bind to a-adrenergic, b-adrenergic, histaminergic, m-cholinergic receptors, dopaminergic or serotonergic receptors.
After oral administration, fluvoxamine completely absorbed from the gastrointestinal tract. Maximum plasma concentrations of the drug observed after 3-8 hours after administration. The absolute bioavailability is 53% following primary metabolism in the liver. Simultaneous administration of fluvoxamine with food does not affect the pharmacokinetics.
fluvoxamine protein binding . The volume of distribution – 25 l / kg.
Metabolism fluvoxamine occurs mainly in the liver. Although isoenzyme of cytochrome metabolism in the main fluvoxamine, drug concentration in the blood plasma of persons with impaired function of this isoenzyme is not much higher than those with normal metabolism. The average from the blood plasma component for a single dose of 13-15 hours increases with repeated several reception (17-22 hours), and the equilibrium concentration in plasma is usually reached within 10-14 days. Fluvoxamine biotransformation in the liver (mainly by oxidative demethylation) at least nine to metabolites that are excreted through the kidneys. Two main metabolites have negligible pharmacological activity. Other metabolites may pharmacologically inactive. Fluvoxamine significantly inhibit cytochrome proprionate, moderately inhibit cytochromes proprionate, and slightly. The pharmacokinetics of a single dose of fluvoxamine is linear. Fluvoxamine equilibrium concentration higher than that of a single dose, and disproportionately higher at higher daily doses.
Special groups of patients:
The pharmacokinetics of fluvoxamine is the same in healthy people, the elderly and patients with renal insufficiency. The metabolism of fluvoxamine is reduced in patients with liver disease. The equilibrium plasma fluvoxamine concentration twice as high in children (aged 6-11 years) than in children (aged 12-17 years). Concentrations of drug in plasma are similar in adolescents with concentrations in adults.
Use during pregnancy and lactation
data of a small number of observations do not indicate any adverse effects of fluvoxamine during pregnancy. To date, no other epidemiological data are not available.
The potential risk for humans is unknown. The drug should be administered to pregnant women with caution.
some cases have been described of withdrawal symptoms in the newborn after use of fluvoxamine in late pregnancy.
Some infants after exposure to selective serotonin reuptake inhibitors in the third trimester of pregnancy occurred feeding difficulties and / or breathing, seizure disorders, unstable body temperature, hypoglycemia, tremor, disorders of muscle tone, increased neuro-reflex excitability syndrome, continuous crying, which could require longer hospitalization. Fluvoxamine passes into breast milk. In this regard, the preparation should not be used during lactation.
Dosage and administration
of fluvoxamine tablets should be taken orally, without chewing, drinking water.
The recommended starting dose for adults is 50 or 100 mg (once in the evening). Recommended doses of a gradual increase to a level effective.
The effective daily dose is usually 100 mg, selected individually depending on the patient’s response to treatment . The daily dose may reach 300 mg. Daily doses greater than 150 mg should be distributed on several stages.
In accordance with the official testosterone propionate recommendations antidepressant treatment should continue for at least 6 months after remission of depressive episodes.
For the prevention of depression recurrence recommended once a day, daily.
Due to lack of clinical experience Luvox is not recommended for the treatment of depression in children up to 18 years.
The recommended starting dose for adults sostavyaet be increased gradually until the effective daily dose should not exceed 300 mg in adults. Doses up to 150 mg can be taken once a day, preferably at night. Daily doses greater than 150 mg is recommended to distribute on 2 or 3 doses.
Children over 8 years and adolescents
The starting dose is 25 mg / day for one reception. Maintenance dose 50 – 200 mg / day. In the treatment of OCD in children aged 8 to 18 years, the daily dose should not exceed 200 mg. Daily doses of 100 mg is recommended to distribute on 2 or 3 doses.
If a good therapeutic response to a drug treatment can be continued with the help of individualized daily dose. If no improvement is achieved after 10 weeks, treatment with fluvoxamine should be reconsidered. So far, no systemic studies were organized, which could answer the question of how long can be carried out treatment with fluvoxamine, but obsessive-compulsive disorders are chronic, and proprionate therefore can be considered expedient to prolong the treatment of fluvoxamine over 10 weeks in patients with a good response for this drug. Selection of the minimum effective maintenance dose should be administered with caution individually. Periodically re-evaluate the need for treatment. Some clinicians recommend carrying out concomitant therapy in patients who respond well to drug therapy.