Fluvoxaminum

Fluvoxaminum Uses, Dosage, Side Effects, Food Interaction and all others data.

The mechanism of action of fluvoxamine maleate in obsessive compulsive disorder is presumed to be linked to its specific serotonin reuptake inhibition in brain neurons. Fluvoxaminum has been shown to be a potent inhibitor of the serotonin reuptake transporter in preclinical studies, both in vitro and in vivo.

In in vitro studies, fluvoxamine maleate had no significant affinity for histaminergic, alpha or beta adrenergic, muscarinic, or dopaminergic receptors. Antagonism of some of these receptors is thought to be associated with various sedative, cardiovascular, anticholinergic, and extrapyramidal effects of some psychotropic drugs.

Fluvoxaminum, an aralkylketone-derivative agent , is one of a class of antidepressants known as selective serotonin reuptake inhibitors (SSRIs) that differs structurally from other SSRIs . It is used to treat the depression associated with mood disorders. It is also used on occassion in the treatment of body dysmorphic disorder and anxiety . The antidepressant, antiobsessive-compulsive, and antibulimic actions of Fluvoxaminum are presumed to be linked to its inhibition of CNS neuronal uptake of serotonin . In vitro studies show that Fluvoxaminum is a potent and selective inhibitor of neuronal serotonin reuptake and has only very weak effects on norepinephrine and dopamine neuronal reuptake . Moreover, apart from binding to σ1 receptors , fluvoxamine has no significant affinity for adrenergic (alpha1, alpha2, beta), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine receptors; antagonism of such receptors has been hypothesized to be associated with various anticholinergic, sedative, and cardiovascular effects for other psychotropic drugs . Furthermore, some studies have demonstrated that the chronic administration of Fluvoxaminum was found to downregulate brain norepinephrine receptors (as has been observed with other drugs effective in the treatment of major depressive disorder), while others suggest the opposite .

Fluvoxaminum
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Fluvoxaminum
Availability	Prescription only
Generic	Fluvoxamine
Fluvoxamine Other Names	Fluvoxamina, Fluvoxamine, Fluvoxaminum
Related Drugs	sertraline, fluoxetine, amitriptyline, venlafaxine, Zoloft, citalopram, Prozac, paroxetine, Celexa, Paxil
Type
Formula	C₁₅H₂₁F₃N₂O₂
Weight	Average: 318.34 Monoisotopic: 318.155512413
Protein binding	~77-80% (plasma protein) .
Groups	Approved, Investigational
Therapeutic Class	SSRIs & related anti-depressant drugs
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Obsessive-Compulsive Disorder: Fluvoxaminum Maleate are used for the treatment of obsessions and compulsions in patients with obsessive compulsive disorder (OCD), as defined in DSM-III-R or DSM-IV. The obsessions or compulsions cause marked distress, are time-consuming, or significantly interfere with social or occupational functioning.

Obsessive compulsive disorder is characterized by recurrent and persistent ideas, thoughts, impulses or images (obsessions) that are ego-dystonic and/or repetitive, purposeful, and intentional behaviors (compulsions) that are recognized by the person as excessive or unreasonable.

Fluvoxaminum is also used to associated treatment for these conditions: Bulimia Nervosa, Major Depressive Disorder (MDD), Obsessive Compulsive Disorder (OCD)

How Fluvoxaminum works

The exact mechanism of action of fluvoxamine has not been fully determined, but appears to be linked to its inhibition of CNS neuronal uptake of serotonin . Fluvoxaminum blocks the reuptake of serotonin at the serotonin reuptake pump of the neuronal membrane, enhancing the actions of serotonin on 5HT_1A autoreceptors . Studies have also demonstrated that fluvoxamine has virtually no affinity for α₁- or α₂-adrenergic, β-adrenergic, muscarinic, dopamine D₂, histamine H₁, GABA-benzodiazepine, opiate, 5-HT₁, or 5-HT₂ receptors, despite having an affinity for binding to σ1 receptors .

Dosage

Fluvoxaminum dosage

Adults: The recommended starting dose for Fluvoxaminum Maleate Tablets in adult patients is 50 mg, administered as a single daily dose at bedtime. In the controlled clinical trials establishing the effectiveness of Fluvoxaminum Maleate Tablets in OCD, patients were titrated within a dose range of 100 to 300 mg/day. Consequently, the dose should be increased in 50 mg increments every 4 to 7 days, as tolerated, until maximum therapeutic benefit is achieved, not to exceed 300 mg per day. It is advisable that a total daily dose of more than 100 mg should be given in two divided doses. If the doses are not equal, the larger dose should be given at bedtime.

Pediatric Population (children and adolescents): The recommended starting dose for Fluvoxaminum Maleate Tablets in pediatric populations (ages 8-17 years) is 25 mg, administered as a single daily dose at bedtime. In a controlled clinical trial establishing the effectiveness of Fluvoxaminum Maleate Tablets in OCD, pediatric patients (ages 8-17) were titrated within a dose range of 50 to 200 mg/day. Physicians should consider age and gender differences when dosing pediatric patients. The maximum dose in children up to age 11 should not exceed 200 mg/day. Therapeutic effect in female children may be achieved with lower doses. Dose adjustment in adolescents (up to the adult maximum dose of 300 mg) may be indicated to achieve therapeutic benefit. The dose should be increased in 25 mg increments every 4 to 7 days, as tolerated, until maximum therapeutic benefit is achieved. It is advisable that a total daily dose of more than 50 mg should be given in two divided doses. If the two divided doses are not equal, the larger dose should be given at bedtime.

Elderly Or Hepatically Impaired Patients: Elderly patients and those with hepatic impairment have been observed to have a decreased clearance of fluvoxamine maleate. Consequently, it may be appropriate to modify the initial dose and the subsequent dose titration for these patient groups.

Side Effects

Nausea, vomiting, asthenia, headache, malaise, palpitations/tachycardia, abdominal pain, anorexia, constipation, diarrhoea, dry mouth, dyspepsia, agitation, anxiety, dizziness, insomnia, nervousness, somnolence, tremor, sweating.

Toxicity

Fluvoxaminum is a member of antidepressants that possess an increased risk compared to placebo of suicidal thinking and behaviour (suicidality) in children, adolescents, and young adults (ages including and and below 24) in short-term studies of major depressive disorder and other psychiatric disorders .

Fluvoxaminum maleate tablets are not approved for use in pediatric patients except for patients with obsessive compulsive disorder (OCD) .

Side effects include anorexia, constipation, dry mouth, headache, nausea, nervousness, skin rash, sleep problems, somnolence, liver toxicity, mania, increase urination, seizures, sweating increase, tremors, or Tourette's syndrome .

Precaution

History of mania or seizures; liver dysfunction; presence of depressive symptoms; smokers. Treatment with MAOI should only be started at least 2 wk after stopping fluvoxamine treatment. Increased risk of suicidal ideation and behaviour when used in children, adolescents and young adults <24 yr. Pregnancy, elderly; operating hazardous machinery; withdraw gradually. Monitor prothrombin time in patients who are taking oral anticoagulants concurrently.

Interaction

Co-admin with fluvoxamine may increase carbamazepine toxicity and serum levels of theophylline. Lithium enhances the serotonergic effects of fluvoxamine. Anticoagulants may require dosage adjustments. Diltiazem with fluvoxamine may lead to bradycardia. Avoid alcohol.

Potentially Fatal: Fluvoxaminum should not be used in combination with MAOIs, or within 14 days of discontinuing treatment with MAOIs.

Food Interaction

Avoid alcohol.
Avoid grapefruit products.
Limit caffeine intake.
Take with or without food. The absorption is unaffected by food.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Fluvoxaminum Drug Interaction

Major: amphetamine / dextroamphetamine, amphetamine / dextroamphetamine, lisdexamfetamine, lisdexamfetamineModerate: aripiprazole, aripiprazole, lamotrigine, lamotrigine, quetiapine, quetiapine, alprazolam, alprazolamUnknown: omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol

Fluvoxaminum Disease Interaction

Major: depressionModerate: hyponatremia, liver disease, mania, platelet function, seizure disorders, SIADHMinor: smoking, weight loss

Volume of Distribution

25 L/kg .

Elimination Route

Well absorbed, bioavailability of fluvoxamine maleate is 53% .

Half Life

15.6 hours .

Elimination Route

Nine metabolites were identified following a 5 mg radio labelled dose of fluvoxamine maleate, constituting approximately 85% of the urinary excretion products of fluvoxamine . The main human metabolite was fluvoxamine acid which, together with its N-acetylated analog, accounted for about 60% of the urinary excretion products . Approximately 2% of fluvoxamine was excreted in urine unchanged . Following a 14C-labelled oral dose of fluvoxamine maleate (5 mg), an average of 94% of drug-related products was recovered in the urine within 71 hours .

Pregnancy & Breastfeeding use

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Contraindication

Hypersensitivity. Not to be used with thioridazine, terfenadine, astemizole, cisapride, pimozide, aloestron, tizanidine. Lactation.

Special Warning

Pregnant Women During The Third Trimester: Neonates exposed to Fluvoxaminum Maleate Tablets and other SSRIs or SNRIs late in the third trimester have developed complications requiring prolonged hospitalization, respiratory support, and tube feeding and may be at risk for persistent pulmonary hypertension of the newborn (PPHN). When treating pregnant women with Fluvoxaminum Maleate Tablets during the third trimester, the physician should carefully consider the potential risks and benefits of treatment.