ANTIPRESTIN

Pharmacological action
Antiprestin 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. Antiprestin 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
Antiprestin 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. Antiprestin 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.
Indication
Depressions of various origins, obsessive-compulsive disorders, bulimic neurosis.
Dosage and administration
The initial dose of Antiprestin 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.
Side effects, adverse reactions
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.
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.
Pregnancy and breastfeeding
Antiprestin is contraindicated during pregnancy and lactation.
Special instructions
Antiprestin 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 Antiprestin 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.
Drug interactions
Simultaneous administration of Antiprestin 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
Antiprestin);
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.
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.
Active ingredients
Fluoxetine Hydrochloride

Available forms
Capsules; Oral; Fluoxetine Hydrochloride 10 mg
Capsules; Oral; Fluoxetine Hydrochloride 20 mg
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