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Product Name: Fluoxetine
Generics: Fluoxetine
Common Brand Names: Prozac; Prozac Weekly; Sarafem
Pharmaceutical Category: Antidepressants / Anti Anxiety
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There is an additional general information about this medication active ingredient fluoxetine:
Pharmacological action
Fluoxetine is an antidepressant, propylamine derivative. The mechanism of action is associated with selective blockade of the inverse of neuronal serotonin reuptake in the CNS. Fluoxetine is a weak antagonist of choline, adrenergic and histamine receptors. Unlike most antidepressants fluoxetine apparently does not cause reduction of functional activity of postsynaptic beta-adrenergic receptors. This medication improves mood, reduces anxiety and stress, eliminates dysphoria. Fluoxetine does not cause sedation. When you receive a medium therapeutic doses of this drug it does not affect the function of cardiovascular and other systems.
Pharmacokinetics
Fluoxetine absorbed from the gastrointestinal tract. This medication is poorly metabolized in the "first pass" through the liver. The ingestion did not affect the extent of absorption, although it may slow its speed. Cmax in plasma is reached after 6-8 hours. Css in plasma is reached only after a continuous reception in a few weeks. The protein binding is 94.5%. Fluoxetine easily penetrates through the BBB.
Fluoxetine metabolized in the liver by demethylation to form the main active metabolite norfluoxetine.
T1/2 of fluoxetine is 2-3 days, norfluoxetine - 7-9 days.
Why is Fluoxetine prescribed?
Depressions of various origins, obsessive-compulsive disorders, bulimic neurosis.
Dosage and administration
The initial dose of Fluoxetine is 20 mg 1 time / day in the morning, if necessary, the dose may be increased in 3-4 weeks. The frequency of reception is 2-3 times / day.
The maximum oral daily dose for adults is 80 mg.
Fluoxetine side effects
CNS: anxiety, tremors, nervousness, drowsiness, headache, sleep disturbances.
Digestive system: diarrhea, nausea.
Metabolism: increased sweating, hypoglycemia, hyponatremia (especially in elderly patients and when hypovolemia).
Reproductive system: decreased libido.
Allergic reactions: skin rash, itching.
Other: pain in joints and muscles, shortness of breath, increased body temperature.
Fluoxetine contraindications
Glaucoma, bladder atony, severe renal dysfunction, benign prostatic hyperplasia, co-administration of MAO inhibitors, convulsions of various origins, epilepsy, pregnancy, lactation, hypersensitivity to fluoxetine.
Using during pregnancy and breastfeeding
Fluoxetine is contraindicated during pregnancy and lactation.
Special instructions
Fluoxetine should be used with caution in patients with impaired liver and kidney, with a history of epileptic seizures, cardio-vascular diseases.
Patients with diabetes may change in blood glucose levels that require correction dosing regimen of hypoglycemic drugs. When applied in debilitated patients with fluoxetine increases the risk of epileptic seizures.
With the simultaneous application of Fluoxetine and electroconvulsive therapy may develop prolonged seizures.
Fluoxetine can be applied not earlier than 14 days after discontinuation of MAO inhibitors. The period after the abolition of fluoxetine before therapy MAO inhibitors should not be less than 5 weeks.
Elderly patients need correction of dosing regimen.
Safety of fluoxetine in children has not been established.
During the period of treatment it needed to avoid use alcohol.
During the period of treatment should refrain from potentially hazardous activities requiring increased attention and rapid psychomotor reactions.
Fluoxetine drug interactions
Simultaneous administration of Fluoxetine with:
drugs providing a depressing effect on the central nervous system and with ethanol it is possibly significantly increased inhibitory action on the CNS, as well as increasing the likelihood of developing seizures;
MAO inhibitors, furazolidone, procarbazine, tryptophan may develop serotonin syndrome (confusion, hypomanic state, motor restlessness, agitation, convulsions, dysarthria, hypertensive crisis, fever, tremor, nausea, vomiting, diarrhea);
fluoxetine inhibits the metabolism of tricyclic and tetracyclic antidepressants, trazodone, carbamazepine, diazepam, metoprolol, terfenadine, phenytoin, thereby increasing their concentration in serum, increase their therapeutic and side effects;
it is possible inhibition of the biotransformation of drugs metabolized with the participation of isoenzyme CYP2D6;
hypoglycemic agents may increase their activities;
haloperidol, fluphenazine, maprotiline, metoclopramide, perphenazine, pyrathiazine, pimozide, risperidone, sulpiride, trifluoperazine there were describes cases of extrapyramidal symptoms and dystonia; with dextromethorphan - described a case of hallucinations; with digoxin - the case of increasing the concentration of digoxin in plasma;
with lithium salts may increase or decrease the concentration of lithium in blood plasma;
may increase the concentration of imipramine and desipramine in plasma is 2-10 times (and may persist for 3 weeks after discontinuation of Fluoxetine);
propofol there was described a case in which spontaneous movements were observed; with phenylpropanolamine - described a case in which were observed dizziness, weight loss, hyperactivity;
may increase the effects of flecainide, mexiletine, propafenone, thioridazine, zuclopenthixol.
There are reports on the strengthening effects of warfarin in its simultaneous application with fluoxetine.
Fluoxetine in case of emergency / overdose
Symptoms: nausea, vomiting, agitation, restlessness, hypomania, seizures, large seizures. There were describes two deaths from acute overdose of fluoxetine (in combination with maprotiline, codeine, temazepam).
Treatment: gastric lavage, taking activated charcoal, sorbitol, ECG monitoring, symptomatic and supportive therapy, when convulsions - diazepam. There is no specific antidote. Forced diuresis, peritoneal dialysis, hemodialysis, blood transfusions are ineffective.
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