Fluvoxamine

When ATH: N06AB08

Characteristic.

Selective serotonin reuptake inhibitor. Fluvoxamine maleate - white or almost white, crystalline powder;. It is soluble in ethanol and chloroform, poorly soluble in water, almost insoluble in diethyl ether. Lipophilic.

Pharmacological action.
Antidepressant.

Application.

Depression different genesis, obsessive compulsive disorder.

Contraindications.

Hypersensitivity, hepatic failure, simultaneous reception of astemizole, cisapride, Terfenadine, means, inhibit MAO (incl. furazolidona, procarbazine, selegiline), breast-feeding, Children up to age 8 years.

Restrictions apply.

Epilepsy, pregnancy; drug dependence, craze, hypomania, convulsive conditions or myocardial infarction.

Pregnancy and breast-feeding.

Be wary of during pregnancy, comparing the expected benefit to the mother and the potential risk to the fetus.

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

At the time of treatment should stop breastfeeding.

Side effects.

From 1087 Patients with obsessive-compulsive disorder and depression, receiving fluvoxamine controlled clinical trials in North America, 22% of patients discontinued due to side effects developed,. Among them were noted (in parenthesis indicates the percentage of occurrence in the placebo group):

From the nervous system and sensory organs: headache 3% (1%), dizziness 2% (less 1%), asthenia 2% (less 1%), insomnia 4% (1%), drowsiness 4% (less 1%), nervousness 2% (less 1%), anxiety 1% (less 1%), ažitaciâ 2% (less 1%).

On the part of the digestive tract: nausea 9% (1%), anorexia 1% (less 1%), dry mouth 1% (less 1%) dyspepsia 1% (less 1%), vomiting 2% (less 1%), diarrhea 1% (less 1%), abdominal pain 1% (0%).

In the placebo-controlled trials in patients with obsessive-compulsive disorder, treated with fluvoxamine in the dose of 100-300 mg/day for 10 Sun, and depression, fluvoxamine-treated at the same dose for 6 Sun, with a frequency of more than 1% The following side effects observed (in parenthesis indicates the percentage of occurrence in the placebo group):

From the nervous system and sensory organs: headache 22% (20%), dizziness 11% (6%), asthenia 14% (6%), drowsiness 22% (8%), insomnia 21% (10%), nervousness 12% (5%), anxiety 5% (3%), ažitaciâ 2% (1%), depression 2% (1%), CNS stimulation 2% (1%), tremor 5% (1%), change in taste 3% (1%), amblyopia 3%(2%).

Cardio-vascular system and blood (hematopoiesis, hemostasis): heartbeat 3% (2%), vasodilation 3% (1%), arterial hypertension 2% (1%).

From the respiratory system: upper respiratory tract infection 9% (5%), dyspnoea 2% (1%), zevota 2% (0%).

From the digestive tract: anorexia 6% (2%), dry mouth 14% (10%), damage to teeth 3% (1%), dysphagia 2% (1%), dyspepsia 10% (5%), nausea 40% (14%), flatulence 4% (3%), diarrhea 11% (7%), constipation 10% (8%), vomiting 5% (2%).

With the genitourinary system: abnormal ejaculation 8% (1%), decreased libido 2%(1%), impotence 2% (1%), anorgazmija 2% (0%), frequent urination 3% (2%), urinary retention 1% (0%).

Other: flu-like symptoms 3% (2%), chills 2% (1%), Sweating 7% (3%).

Cooperation.

Incompatible with means, inhibit MAO, incl. furazolidonom, procarbazine, and selegiline (the risk of serotonin syndrome and death). The development of serotonin syndrome (chills, hyperthermia, muscle stiffness, myoclonus, vegetative lability, hypertensive crisis, excitation, tremor, restlessness, convulsions, diarrhea, elated state) possibly in patients receiving drugs with serotonergic activity (tryptophan, lithium compounds). Increases concentration in plasma propranolol (in 5 time), metoprolol and other beta-blockers, anticoagulants, incl. varfarina (on 98%), karʙamazepina, clozapine (in 3 times), tricyclic antidepressants (amitriptillin, clomipramine, imipramine). Fluvoxamine Simultaneity with antipsychotics group butirofenona, including haloperidol, It leads to an increase of plasma concentrations or 2-10-fold increase in the content of fluvoxamine. Is able to inhibit the biotransformation of drugs, метаболизирующихся при участии изоферментов CYP1A2, CYP3A4, CYP2C9, CYP2D6 цитохрома P450 (phenytoin, quinidine, theophylline, caffeine and other.), increasing the risk of adverse reactions. Fluvoxamine on the background of astemizole, cisapride or terfenadine may lead to a marked prolongation of the QT interval and the appearance of arrhythmias such as "pirouette" (possible death). When concomitantly with diltiazem may develop bradycardia, with sumatriptanom-weakness, hyperreflexia and poor coordination of movements. It reduces the excretion of benzodiazepines (alprazolam, bromazepam, diazepam, midazolam, triazolam), causing them to cumulation; It does not affect the removal Lorazepam, oxazepam and temazepam. Enhances the side effects of alcohol.

Overdose.

Symptoms: dizziness, drowsiness, dry mouth, nausea, vomiting, diarrhea, Beards- or tachycardia, hypotension, ECG changes, abnormal liver function, midriaz, tremor, myoclonus, seizures, oligurija, coma. Described deaths.

Treatment: stimulation of vomiting or gastric lavage, administration of activated charcoal, ECG monitoring, maintaining vital functions, simptomaticheskaya therapy. No specific antidote. Dialysis and forced diuresis are not effective (due to the large volume of distribution).

Dosing and Administration.

Inside, adult, without chewing, with a little water. The initial dose of 50-100 mg/day one (in the evening), with good endurance dose increase to 150-200 mg/day 2-3 reception. The maximum daily dose - 300 mg.

Precautions.

The interval between the cancellation of MAO inhibitors and start taking fluvoxamine or its cancellation and the start of reception of MAO inhibitors should not be less than 14 days. Careful monitoring of patients with suicidal tendencies, especially at the beginning of treatment. Elderly patients fluvoxamine should be given at a reduced dosage. Be wary of the drivers of vehicles and people, activities which require high concentration and speed of psychomotor reactions. During treatment should avoid alcohol.

Animal studies have not revealed the development of drug dependence. Similar studies on humans has not been. It should be used with caution in patients, with a history of drug dependence or abuse.

Cooperation

Active substanceDescription of interaction
AmitriptylineFKV. Against the backdrop of slowing biotransformation and fluvoxamine increases plasma concentration.
WarfarinFKV. Against the backdrop of slowing fluvoxamine and biotransformation 2 times increased plasma concentration.
DiltiazemFMR. Against the background of fluvoxamine, the influence on heart rate (bradycardia).
ImipramineFKV. Against the backdrop of slowing biotransformation and fluvoxamine increases plasma concentration.
CarbamazepineFKV. Against the backdrop of slowing biotransformation and fluvoxamine increases plasma concentration.
KlozapynFKV. Increases (mutually) concentration in the blood.
ClomipramineFKV. Against the backdrop of slowing biotransformation and fluvoxamine increases plasma concentration.
LinezolidFMR. Inhibits MAO and increases the risk of serotonin syndrome.
MetoprololFKV. Amid fluvoxamine concentration increases in blood.
PropranololFKV. Against the background of fluvoxamine increases (in 5 time) plasma levels.
SelegilineFMR: synergism. Inhibits MAO and increases the risk of serotonin syndrome (hyperthermia, rigidity, myoclonus, autonomic disorders, extreme agitation, progressing to delirium and to whom); simultaneous and / or sequential use is not recommended.
SumatriptanFMR. Against the background of fluvoxamine may cause weakness, hyperreflexia and poor coordination of movements.
TheophyllineFKV. Against the background of fluvoxamine significantly increases plasma concentration; combined use is not recommended.
PhenytoinFKV. Against the background of fluvoxamine increases the concentration of phenytoin in the blood.
EthanolFMR. Against the backdrop of intensified fluvoxamine deprimatsiya; at the time of treatment should abandon spirits.

Back to top button