Clinical Pharmacology Details


FLUVOXAMINE


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Indications & Dose:

Depressive illness



Adult: Initially 50–100 mg daily, dose to be taken in the evening, dose to be increased gradually, increased if necessary up to 300 mg daily, doses over 150mg daily are given in divided doses; maintenance 100 mg daily


Obsessive-compulsive disorder



Adult: Initially 50 mg daily, dose to be taken in the evening, dose is increased gradually if necessary after several weeks, increased if necessary up to 300 mg daily; maintenance 100–300 mg daily, doses over 150mg daily are given in divided doses, if no improvement in obsessive-compulsive disorder within 10 weeks, treatment should be reconsidered 

Contraindications:

Administration within 14 days of discontinuing MAOI therapy. 

Side Effects:

Cautions:

Precautions:

History of mania, seizure disorder, liver dysfunction, suicidal ideation, children 

Interaction:

Drugs


Antihistamines, nonsedating (astemizole, terfenadine): Fluvoxamine inhibits metabolism (CYP3YA4) for detoxifying these antihistamines; cardiac rhythm disturbances


Benzodiazepines (alprazolam, diazepam): Probable inhibition of metabolism (CYP3A4) leading to accumulation of diazepam and alprazolam


Beta-blockers (metoprolol, propranolol, sotalol): Inhibition of metabolism (CYP2Db) leads to increased plasma concentrations of selective beta blockers and potential cardiac toxicity; atenolol may be safer choice Buspirone: Reduced therapeutic effect of both drugs; possible seizures


Carbamazepine: Inhibition of hepatic metabolism of carbamazepine, but the formation of carbamazepine epoxide is not inhibited, contributing to increased toxicity


Clozapine: Fluvoxamine markedly increases clozapine concentrations as a potent inhibitor of CYP1A2


Cyclic antidepressants (ctomipramine, desipramine, doxepin, imipramine, wortriptylline, trazadone): Inhibition of metabolism (CYP1A2 arid CYP3A4) leading to accumulation of cyclic antidepressants; dosage adjustments necessary


Cyproheptadine: Serotonin antagonist may partially reverse antidepressant and other effects


Dexfenfluramine: Duplicate effects on inhibition of serotonin reuptake; inhibition of dexfenfluramine metabolism (CYP2D6) ex-aggerates effect; both mechanisms increase risk of serotonin syndrome


Fenfluramine: Duplicate effects on inhtbition of serotonin reuptake; inhibition of dexfenfluramine metabolism (CYP2Dr6) exaggerates effect; both mechanisms increase risk of serotonin syndrome


HMG-Co A reductase inhibitors (atorvastatin, lovastatin, simvastatin): inhibition of statin metabolism (CYP3A4), by fluoxetine, may lead to rhabdomyolysis


Lithium: Neurotoxicity (tremor, confusion, ataxia, dizziness, dysarthria, and abscence seizures) reported in patients receiving this combination; mechanism unknown


MAOIs (isocarboxazid, phenelzine, tranylcyprotmine): Increased CNS serotonergic effects have been associated with severe or fatal reactions with this combination


Phenytoin: Inhibition of metabolism and phenytoin toxicity


Selegiline: Sporadic cases of mania and hypertension


Theophylline: Theophylline toxicity increased via accumulation due to inhibition of metabolism (CYP1A2) by fluvoxamine


Tryptophan: Additive serotonergic effects


Warfarin: Increased hypothrombinemic response 

Warnings:

Adverse Effects:

Lactations:

Excreted into breast milk; use caution in nursing mothers

Special Precautions:

Counselling:

Side Effects Or Adverse Reactions:

CNS: Agitation, anxiety, decreased libido, depression, dizziness, headache, insomnia, nervousness, somnolence, tremor


CV: Hypertension, hypotension, orthostatic, palpitations, syncope, tachycardia


EENT: Amblyopia, taste perversion/change


GI: Anorexia, constipation, diarrhea, dry mouth, dyspepsia, flatulence, nausea, vomiting


GU: Abnormal ejaculation, sexual dysfunction, urinary frequency


RESP: Dyspnea


SKIN: Sweating 

Patient And Carer Advice: