Флувоксамин химические свойства, назначение, производство
Химические свойства
Colourless Oil
Общее описание
The E-isomer of fluvoxamine (Luvox) can fold after protonation to the β-arylamine–like grouping. Here,the “extra” hydrophobic group is aliphatic.
Опасность
A poison.
Механизм действия
Fluvoxamine is a highly selective inhibitor of 5-HT reuptake at the presynaptic membrane. Potency data from
in vitro affinity studies suggest that fluvoxamine is less potent than the other SSRIs (e.g., paroxetine,
sertraline, and citalopram). Its mechanism of action is similar to that of the other SSRIs. Fluvoxamine appears
to have little or no effect on the reuptake of NE or dopamine. In vitro studies have demonstrated that
fluvoxamine possesses virtually no affinity for other neuroreceptors. Its onset of action is similar to the other
SSRIs (2–4 weeks).
Фармакокине?тика
Fluvoxamine is well absorbed, with a bioavailability of approximately 50%, probably because of first-pass
metabolism. At steady-state doses, fluvoxamine demonstrates nonlinear pharmacokinetics over a
dosage range of 100 to 300 mg/day, which results in higher plasma concentrations at higher doses than
would be predicted by lower-dose kinetics (single dose, 15 hours; multiple dosing, 22 hours). Food does not
significantly affect oral bioavailability. The mean apparent volume of distribution for fluvoxamine reflects its
lipophilic nature, extensive tissue distribution, and protein binding. Fluvoxamine is distributed into breast
milk. Fluvoxamine is preferentially metabolized by CYP2D6 in the liver by O-demethylation to its alcohol
metabolite, which subsequently is oxidized to a carboxylic acid. Oxidative deamination and nine other
metabolites have been identified, none of which shows significant pharmacological activity.
Клиническое использование
Fluvoxamine is approved for use in obsessive-compulsive disorders.
Побочные эффекты
The adverse effects for fluvoxamine include symptoms of drowsiness, nausea or vomiting, abdominal pain,
tremors, sinus bradycardia, and mild anticholinergic symptoms. Toxic doses could produce seizures and
severe bradycardia.
взаимодействия лекарств
In vitro studies have shown fluvoxamine to be a potent inhibitor of CYP1A2, to inhibit CYP3A4 and CYP2C19,
and to weakly inhibit CYP2D6. The bioavailability of fluvoxamine is significantly decreased in smokers
compared with nonsmokers, possibly because of induction of CYP1A metabolism of fluvoxamine. Therefore,
interactions with drugs that inhibit CYP1A2 also should be considered (e.g., theophylline and caffeine).
Флувоксамин препаратная продукция и сырье
сырьё
препарат