Moditen® [Fluphenazine]

Pharmacological properties

Moditen Depot is a prolonged form of the antipsychotic flufenazine. fluphenazine decanoate is gradually hydrolyzed to release active fluphenazine entering the bloodstream. the antipsychotic effect of the drug is approximately 20 times greater than that of chlorpromazine. the use of the drug leads to a reduction in psychopathological symptoms in patients with chronic psychosis and is optimal for outpatient treatment.

Fluphenazine decanoate is slowly absorbed after intramuscular injection and then hydrolyzed in blood plasma with the release of pharmacologically active fluphenazine. The action begins 24–72 hours after the injection. The half-life of flufenazine from blood plasma is from 7 to 10 days. The standard injection of Moditen Depot acts on patients with psychosis from 15 to 35 days, which indicates the importance of individual selection, dose adjustment and the interval between injections for each patient. The intervals between injections are usually from 2 to 4 weeks. It passes through the BBB. It is excreted in the urine and partially with feces.

Indications

Neurosis-like disorders and hallucinations, various forms of schizophrenia, especially in the presence of stupor-catotonic disorders, paranoid conditions accompanied by fear, a sluggish course of the process with a predominance of depressive-hypochondriac syndrome.

Application

Introduced deep in oil. the needle and syringe must be dry. the initial dose is usually 12.5 to 25 mg of moditene depot. subsequent doses and intervals between administrations are determined individually. usually the interval between injections is 15 to 35 days. if a dose above 50 mg is needed, it is gradually increased by 12.5 mg. single dose should not exceed 100 mg. patients who have not previously received treatment with phenothiazine derivatives should first be treated with injections of short-acting forms of the drug or moditin tablets. with good portability of moditene, they can be transferred to moditen depot. the initial dose of 12.5 mg of moditene depot is administered in oil. with good tolerance after 5-10 days, you can prescribe the next dose - 25 mg. further changes in the dose and the interval between injections of the drug depend on the individual response of the patient to the treatment.

If the patient has already taken phenothiazine derivatives, they can be replaced by Moditen Depot without prior treatment with short-acting forms of drugs or Moditen tablets. In this case, the initial IM dose of 12.5 mg is again used to determine the tolerance of the drug, then the dose is individually regulated. Older patients should be prescribed lower doses - from¹/₃ before¹/₄ standard dose. If extrapyramidal disorders occur, antiparkinsonian drugs are prescribed.

Contraindications

Hypersensitivity to fluphenazine. apparent or suspected subcortical cerebral disorders; acute disorders of consciousness, severe cerebral atherosclerosis, pheochromocytoma, severe renal, hepatic or heart failure, hypersensitivity to other phenothiazines; acute intoxication with central nervous system inhibitors (alcohol, antidepressants, antipsychotics, tranquilizers, sedatives, sleeping pills and drugs); children under 12 years old.

Side effects

Most often manifested by extrapyramidal disorders (parkinsonism, dystonia, loss of ability to exhibit an adequate emotional reaction, opistotonus). these symptoms are reversible and disappear after a dose reduction or treatment discontinuation. they can be avoided or reduced by severity with antiparkinsonian drugs. drowsiness, visual impairment, dry mouth, mild disorders of the autonomic nervous system (hypertension, unstable hell) and endocrine glands (amenorrhea, galactorrhea, gynecomastia, impotence), moderate hypotension, epileptic seizures, and skin allergic reactions are sometimes noted. all these symptoms are reversible and disappear after a dose reduction or treatment discontinuation. rarely - significant hypotension may occur.

With prolonged treatment, tardive dyskinesia may occur, manifested by involuntary rhythmic movements of the muscles of the tongue, face, mouth, lips, trunk and extremities. Tardive dyskinesia often occurs in old age, mainly in women and against the background of high doses. It is necessary to stop treatment, since antiparkinsonian drugs are not effective in tardive dyskinesia.

The effect of phenothiazine on the heart is dose dependent. It can lengthen the Q-T interval and the T wave; very rarely leads to ventricular paroxysmal tachycardia and fibrillation. These disorders disappear when the dose is reduced. In exceptional cases, malignant neuroleptic syndrome may occur, characterized by hyperthermia, muscle rigidity, akinesia, hypotension, stupor and coma. The use of the drug must be stopped immediately, prescribe symptomatic treatment in a hospital.

Isolated cases of vein thrombosis of the lower extremities have been reported.

Treatment with Moditen Depot can worsen the course of mental disorders, so patients receiving it should be under medical supervision.

special instructions

Moditen Depot is not intended for short-term use (less than 3 months), it is ineffective in treating behavior disorders in mentally retarded patients. with great caution, the drug is prescribed to patients with convulsive disorders, since it can lower the threshold for seizures or cause them, including a generalized epileptic seizure. prescribed with caution in patients with cardiovascular disease, since a significant decrease in hell is possible. elderly patients and weakened patients are prescribed a modestine depot in the least effective dose, since side effects can occur more often in this category of patients.

As with other phenothiazine derivatives, mute pneumonia may develop with flufenazine.

If the patient takes anti-Parkinsonian drugs during treatment with Moditen Depot and abruptly stops using the latter, he should continue taking the drugs for Parkinsonism for several more weeks.

During pregnancy, the drug can be used only in cases where the potential benefit exceeds the potential risk to the fetus. Fluphenazine passes into breast milk, so you should stop breastfeeding during treatment.

Interactions

The combined use of fluphenazine with antihistamines, sedatives, sleeping pills, drugs, antidepressants, other antipsychotics or alcohol increases their inhibitory effect on the central nervous system.

Barbiturates, sleeping pills of other groups, carbamazepine, griseofulvin, phenylbutazone and rifampicin enhance metabolism, while paracetamol, chloramphenicol, disulfiram, MAO inhibitors, tricyclic antidepressants and antidepressants that inhibit the neuronal uptake of serotonin metabolism, perforum. Phenothiazines can increase blood glucose because they affect carbohydrate metabolism. Accordingly, dose adjustment of hypoglycemic agents in patients with diabetes mellitus is needed.

Fluphenazine weakens the effect of adrenaline and other sympathomimetics. Thanks to the blockade of the dopamine receptor, it reduces the antiparkinsonian effect of levodopa. Moditen Depot can lower the seizure threshold, therefore dose adjustment of antiepileptic drugs is necessary. Fluphenazine can enhance the effect of anticoagulants, so it is recommended to control prothrombin time.

A strong decrease in blood pressure due to Moditen Depot requires immediate iv infusion of norepinephrine. You can not use epinephrine (adrenaline) because in combination with phenothiazine derivatives it does not increase blood pressure, but reduces it.

Avoid co-administration of antiarrhythmic drugs or use them under strict medical supervision.

Overdose

Serious extrapyramidal disorders, a significant decrease in hell, miosis, hypothermia, urinary retention, changes in ecg and cardiac arrhythmias are possible; sedation and disturbances of consciousness up to a coma. the antidote is unknown. symptomatic treatment. careful monitoring of the patients condition is necessary. with arrhythmias, sodium bicarbonate and magnesium sulfate are effective. with extrapyramidal disorders - antiparkinsonian drugs. with severe hypotension, only norepinephrine (norepinephrine) can be prescribed. epinephrine (adrenaline) will lower the pressure even more.

Storage conditions

In the dark place at a temperature of 8-25 ° C.