Clinical Pharmacokinetics of Fluvoxamine

  title={Clinical Pharmacokinetics of Fluvoxamine},
  author={Emilio Perucca and Giuliana Gatti and Edoardo Spina},
  journal={Clinical Pharmacokinetics},
SummaryFluvoxamine is a selective inhibitor of serotonin reuptake that is widely used in the management of depression.Following oral administration, the drug is absorbed efficiently from the gastrointestinal tract. Peak plasma concentrations are usually observed within 2 to 8 hours postdose for capsules and film-coated tablets and within 4 to 12 hours for enteric-coated tablets. Despite complete absorption, oral bioavailability may be incomplete probably because of first-pass metabolism… 

Overview of the Pharmacokinetics of Fluvoxamine

Fluvoxamine pharmacokinetics are substantially unaltered by increased age or renal impairment, however, its elimination is prolonged in patients with hepatic cirrhosis, and has the potential for clinically significant drug interactions.

Inhibition of diazepam metabolism by fluvoxamine: A pharmacokinetic study in normal volunteers

Fluvoxamine inhibits the biotransformation of diazepam and its active N‐demethylated metabolite, and the magnitude of this interaction is likely to have considerable clinical significance.

Pharmacokinetic-Pharmacodynamic Relationship of the Selective Serotonin Reuptake Inhibitors

  • P. Baumann
  • Medicine, Biology
    Clinical pharmacokinetics
  • 1996
No clearcut plasma concentration-clinical effectiveness relationship in patients with depression has been shown, nor any threshold which defines toxic concentrations, and SSRIs presently available may be explained by their low toxicity and use at dosages where serious adverse effects do not appear.

Pharmacokinetics of selective serotonin reuptake inhibitors.

Non-linear fluvoxamine disposition.

The present study conclusively demonstrates that fluvoxamine exhibits non-linear kinetics within the therapeutic dose interval, which is not Michaelis-Menten saturation kinetics of a single metabolic pathway, but rather a complex involvement of multiple parallel pathways.

Pharmacokinetics of Fluvoxamine in Relation to CYP2C19 Phenotype and Genotype

FLV disposition and dosing is unlikely to be affected by CYP2C19 polymorphism and AUC, elimination half-life, Cmax and Tmax did not significantly differ between the two groups.

Metabolism and Pharmacokinetics of Selective Serotonin Reuptake Inhibitors

  • C. DeVane
  • Biology, Medicine
    Cellular and Molecular Neurobiology
  • 2004
The metabolism and relevant pharmacokinetic properties of the SSRIs are summarized, appearing to share similar pharmacodynamic properties which translate to efficacy in the treatment of depression and anxiety syndromes.

Effects of Caffeine on the Kinetics of Fluvoxamine and its Major Metabolite in Plasma After a Single Oral Dose of the Drug

Caffeine slightly induces the metabolism of FLV, probably mediated by CYP1A2, and plasma concentration and pharmacokinetic parameters of FLA were not affected by caffeine.

Fluvoxamine. A review of global drug-drug interaction data.

Clinical symptoms were infrequent and varied widely; no symptom clusters were identified; those agents metabolised by cytochrome P450 1A2 isoenzyme appear most likely to be involved in drug-drug interactions with fluvoxamine.

The Differential Effects of Steady‐State Fluvoxamine on the Pharmacokinetics of Olanzapine and Clozapine in Healthy Volunteers

The effects of fluvoxamine on different aspects of pharmacokinetics of the two antipsychotics may have implications for clinical therapeutics.



Pharmacokinetics of Fluvoxamine Maleate in Patients with Liver Cirrhosis after Single-Dose Oral Administration

It is concluded that in patients with signs of active liver disease, e.g. raised bilirubin, it is wise to lower the initial daily dose and to carefully monitor the patient during subsequent upward dose adjustments.

Inhibition of diazepam metabolism by fluvoxamine: A pharmacokinetic study in normal volunteers

Fluvoxamine inhibits the biotransformation of diazepam and its active N‐demethylated metabolite, and the magnitude of this interaction is likely to have considerable clinical significance.

Effect of Fluvoxamine on the Pharmacokinetics of Imipramine and Desipramine in Healthy Subjects

Findings indicate that, at the dosage tested, fluvoxamine markedly inhibits the demethylation of imipramine without affecting significantly the CYP2D6-mediated hydroxylation of desipramines.

Single and Multiple Oral Dose Fluvoxamine Kinetics in Young and Elderly Subjects

The results suggest that it is not necessary to adjust the dosage of fluvoxamine in elderly depressed patients, on the basis of pharma-cokinetic arguments.

Review of the animal pharmacology and pharmacokinetics of fluvoxamine.

  • V. Claassen
  • Biology, Chemistry
    British journal of clinical pharmacology
  • 1983
A highly favourable therapeutic ratio of antidepressant effects vs disturbing side-effects is predicted on the basis of the pharmacological profile of fluvoxamine.

Fluvoxamine. An updated review of its pharmacology, and therapeutic use in depressive illness.

Fluvoxamine may be particularly beneficial in potentially suicidal patients with severe depression, in those with an underlying compulsive personality or cardiovascular disorder, in patients with coexistent anxiety or agitation, and in the elderly.

Fluoxetine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in depressive illness.

Fluoxetine has overall therapeutic efficacy comparable with imipramine, amitriptyline and doxepin in patients with unipolar depression treated for 5 to 6 weeks, although it may be less effective than tricyclic antidepressants in relieving sleep disorders in depressed patients.

Clinical Pharmacokinetics of Selective Serotonin Reuptake Inhibitors

Although many attempts were made, to date no convincing evidence exists of a relationship between plasma concentrations of any of the SSRIs and clinical efficacy, and available data indicate that metabolism ofSSRIs is impaired with reduced liver function.

Chronic Treatment with Fluvoxamine, Clovoxamine, and Placebo: Interaction with Digoxin and Effects on Sleep and Alertness

Clovoxamine and fluvoxamine appear to have differential effects on sleep and alertness in healthy volunteers, however, neither have an important influence on the kinetics of digoxin.