Fluphenazine

Pharmacological properties of the drug Fluphenazine

Fluphenazine is a strong, long-acting antipsychotic. It has a pronounced antipsychotic effect, combined with some activating effect, as well as a moderate sedative effect. Has an antiemetic effect. The mechanism of action is due to a blocking effect on central dopaminergic receptors with a moderate effect on noradrenergic receptors. Unlike other phenothiazine derivatives, it is characterized by a stronger effect (25 times greater than chlorpromazine in neuroleptic activity) and less pronounced extrapyramidal and somatic disorders. Particularly effective for malignant nuclear (hebephrenic, catatonic, early paranoid forms) and long-term schizophrenia. In the form of decanoate (oil solution), it has a long-lasting effect due to the gradual release of the active substance; after a single intramuscular injection, it acts, depending on the dose, for 1–2 weeks or more. It is quickly and almost completely absorbed after oral administration. Penetrates the BBB and placental barrier. Excreted in urine and partially in bile.

FLUPHENAZINE DECANOATE

Dosage form:

solution for intramuscular administration [oil]

Pharmachologic effect:

Long-acting antipsychotic (neuroleptic); has a weak antiemetic effect. Eliminates anxiety and irritability, hallucinations and delusions. The antipsychotic effect is due to the blockade of dopamine D2 receptors in the mesolimbic and mesocortical systems. The sedative effect (moderately expressed and observed when used in high doses) is due to the blockade of adrenergic receptors in the reticular formation of the brain stem; antiemetic effect - blockade of dopamine D2 receptors in the trigger zone of the vomiting center; hypothermic effect - blockade of dopamine receptors of the hypothalamus. Unlike other phenothiazine derivatives, it is characterized by greater activity (25 times greater than chlorpromazine in neuroleptic activity) and a less pronounced ability to cause extrapyramidal and somatic disorders. Particularly effective for malignant nuclear (hebephrenic, catatonic, early paranoid forms) and long-term schizophrenia. In the form of decanoate (solution in oil), it has a long-term effect (the release of the drug is gradual) - the effect lasts up to 1-2 weeks or more (depending on the dose).

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Indications:

Paranoid states, hallucinations, fear, aggressiveness; excited state in the weak-minded; agitation, emotional disturbances (in older people). Chronic forms: schizophrenia (all forms), psychosis, depressive-hypochondriacal syndrome, neurotic conditions accompanied by fear, nervous tension.

Contraindications:

Hypersensitivity, severe cardiovascular diseases (decompensated CHF, arterial hypotension), severe depression of central nervous system function and coma of any etiology; brain injuries, progressive systemic diseases of the brain and spinal cord, pregnancy, lactation, childhood (up to 12 years - for fluphenazine decanoate). Caution. Alcoholism (increased susceptibility to hepatotoxic reactions), pathological changes in the blood (impaired hematopoiesis), breast cancer (as a result of phenothiazine-induced prolactin secretion, the risk of disease progression and resistance to treatment with endocrine and cytostatic drugs increases), angle-closure glaucoma, prostatic hyperplasia with clinical manifestations , liver and/or kidney failure, peptic ulcer of the stomach and duodenum (during exacerbation); diseases accompanied by an increased risk of thromboembolic complications; Parkinson's disease (extrapyramidal effects increase); epilepsy, history of epileptic seizures; myxedema; chronic diseases accompanied by breathing problems (especially in children); Reye's syndrome (increased risk of hepatotoxicity in children and adolescents); cachexia, vomiting (the antiemetic effect of phenothiazines can mask vomiting associated with an overdose of other drugs), old age.

Side effects:

Dyskinesia (including tardive dyskinesia), predisposition to epileptiform seizures, neuroleptic malignant syndrome (hyperthermia, akinesia, autonomic lability, clouding of consciousness, coma), tachycardia, decreased blood pressure, urinary retention, constipation, impaired secretory activity of the exocrine glands, increased intraocular pressure, photosensitivity, allergic reactions, galactorrhea, dysmenorrhea, psychomotor retardation; seborrhea; orthostatic hypotension, agranulocytosis, eosinophilia, leukopenia, hemolytic anemia, pancytopenia.

Directions for use and dosage:

IM, s/c, inside. IM or SC, initial dose - 12.5-25 mg, if necessary and taking into account tolerability, the dose is repeated or increased every 1-3 weeks. Maintenance dose - up to 50 mg every 1-4 weeks. If the dose is more than 50 mg, it should be increased with caution by 12.5 mg. The maximum single dose for adults is 100 mg. Children 5-12 years old - IM or SC 3.125-12.5 mg, if necessary and taking into account tolerability, the dose is repeated every 1-3 weeks. Children 12 years of age and older - 6.25-18.75 mg per week, if necessary and taking into account tolerability, the dose is increased to 12.5-25 mg and prescribed every 1-3 weeks. Inside. Adults, initial dose - 2.5-10 mg/day, divided into 3-4 doses; If necessary and taking into account tolerability, the dose can be gradually increased. Maintenance dose - 1-5 mg/day once, or in divided doses. Depleted and weakened patients require a lower initial and maintenance dose - 1-2.5 mg, which is increased if necessary and taking into account tolerability. The maximum dose for adults is 20 mg/day. Children - 0.25-0.75 mg 1-4 times a day.

Special instructions:

If there is a significant decrease in blood pressure while using the drug, norepinephrine should be immediately administered intravenously. If there is a history of epileptic seizures, fluphenazine can be prescribed in combination with antiepileptic drugs. During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Interaction:

Weakens the vasoconstrictor effect of ephedrine. Reduces the effectiveness of antiepileptic drugs. Reduces the antiparkinsonian effect of levodopa (due to the blockade of dopamine receptors), as well as the effects of amphetamines, clonidine and guanethidine. Strengthens the anticholinergic effects of other drugs, while its own antipsychotic effect may decrease. May mask some manifestations of ototoxicity (tinnitus, dizziness) of ototoxic drugs, especially antibiotics. It should not be combined with combination drugs that contain reserpine. Long-term combination with analgesics and antipyretics is undesirable (possible development of hyperthermia). When used simultaneously with other drugs that have a depressant effect on the central nervous system (drugs for general anesthesia, narcotic analgesics, ethanol and drugs containing it, barbiturates, anxiolytic drugs (tranquilizers), etc.), an increase in the depressive effect, as well as respiratory depression, is possible. Prescription together with tricyclic antidepressants, maprotiline or MAO inhibitors increases the risk of developing neuroleptic malignant syndrome; with drugs for the treatment of thyrotoxicosis increases the risk of developing agranulocytosis; with other drugs that cause extrapyramidal reactions, increases the frequency and severity of extrapyramidal disorders; with antihypertensive drugs increases the severity of orthostatic decrease in blood pressure. Antacids, antiparkinsonian drugs, Li+ drugs can interfere with absorption. Dr. hepatotoxic drugs - the risk of developing hepatotoxicity. During treatment, the administration of epinephrine should be avoided (due to the possibility of distorting the effect of epinephrine and further reducing blood pressure).

Special instructions for the use of the drug Fluphenazine

Use with caution for liver diseases, arrhythmia, thyrotoxicosis, epilepsy, Parkinson's disease, angle-closure glaucoma. Fluphenazine should be dosed with particular care when treating patients who work in high temperatures, have contact with fluoride-containing insecticides, and elderly patients. Prescription of fluphenazine during pregnancy is possible only under strict indications. If it is necessary to prescribe during breastfeeding, breastfeeding should be discontinued. During the treatment period, it is necessary to refrain from potentially dangerous activities that require increased attention, speed of mental and motor reactions.

- Due to possible cross-sensitivity, the drug should be prescribed with caution to patients with allergic reactions.

history of phenothiazine derivatives;

- with the development of cholestatic jaundice

If an adverse reaction occurs, treatment with fluphenazine should be discontinued;

- during surgical operations

patients taking high doses of phenothiazine derivatives may experience a sharp decrease in blood pressure;

- it may be necessary to reduce the doses
of anesthetics
or
neuroleptics
in some patients during treatment with the drug; it is possible to potentiate the effect of m-anticholinergic blockers, since fluphenazine has an m-anticholinergic effect;

- Fluphenazine should be prescribed with caution in
very hot weather
or
poisoning with organophosphorus insecticides
, in patients with
of seizures
;

- used with caution in case of mitral valve insufficiency

or other
cardiovascular disorders
or with
pheochromocytoma
;

- the drug should be prescribed with caution for
breast cancer
, since as a result of the secretion of prolactin induced by phenothiazine derivatives, the risk of disease progression and resistance to treatment with endocrine and cytostatic drugs increases;

- cases of venous thromboembolism

were observed when taking antipsychotic drugs. Because patients taking antipsychotic drugs often have risk factors for the development of venous thromboembolism, it is necessary to evaluate these factors before and during treatment and take appropriate preventive measures;

- when prescribed to patients with Parkinson's disease

possible increase in extrapyramidal symptoms;

extrapyramidal symptoms arising as adverse reactions

, as a rule, are reversible, but can also be persistent. The likelihood and severity of such undesirable side reactions depends to a greater extent on individual sensitivity than on other factors, but the dose and age of the patient are important. The patient should be warned in advance about such manifestations and their reversibility. Usually, to eliminate these undesirable effects, it is sufficient to prescribe m-anticholinergic drugs or antiparkinsonian drugs and/or reduce the dose of the drug;

- in elderly patients, sedative and hypotensive effects may be pronounced (see sections “Dosage and Administration” and “Side Effects”).

Neuroleptic malignant syndrome

If this adverse reaction develops, you should immediately stop taking antipsychotics and other medications that do not affect the maintenance of vital functions, and intensive symptomatic treatment, constant monitoring of vital functions and treatment of concomitant diseases are also necessary.

Cerebrovascular accident and increased mortality in elderly patients with dementia

An approximately 3-fold increase in the risk of developing cerebrovascular accidents was observed when taking some atypical antipsychotics in elderly patients with a history of dementia. There was a slight increase in mortality in elderly patients with a history of dementia during treatment with antipsychotic drugs. The extent of the risk and the reasons for this phenomenon are unknown. It should be remembered that fluphenazine is not indicated for the treatment of elderly patients with dementia.

Hypotension

It is rare during treatment with fluphenazine. At the same time, in patients with pheochromocytoma, cerebrovascular, renal and severe heart failure (for example, in patients with mitral valve insufficiency), hypotension develops more often while taking fluphenazine; These patients require careful monitoring.

If severe hypotension develops, rapid intravenous administration of vasoconstrictor drugs is necessary. Norepinephrine injection is best for this. Epinephrine is not recommended because phenothiazine derivatives distort the response to epinephrine, resulting in an even greater decrease in blood pressure.

If diseases of the oral mucosa, gums or throat develop, or an upper respiratory tract infection occurs in combination with a change in the number of leukocytes confirming hematopoietic suppression, fluphenazine therapy should be discontinued and the necessary therapeutic measures should be started immediately.

Patients with seizures

history, phenothiazine derivatives, including fluphenazine, should be prescribed with caution.

It should be borne in mind that the antiemetic effect of phenothiazine derivatives (including fluphenazine) may mask vomiting associated with an overdose of other drugs.

Abrupt withdrawal of the drug

: In general, taking phenothiazine derivatives does not cause mental dependence, but cases of nausea, vomiting, sweating, insomnia, and dizziness have been reported with abrupt withdrawal of high doses of phenothiazine derivatives. These symptoms decreased when antiparkinsonian drugs were taken for several weeks after discontinuation. The dose reduction should be gradual.

The drug contains sesame oil, which in rare cases can cause severe allergic reactions.

Benzyl alcohol contained in the drug can cause severe toxic and anaphylactoid reactions in children over 12 years of age.

Drinking alcohol during treatment with the drug is prohibited.

The drug should not be stored in the refrigerator, as this leads to precipitation of the triglycerides contained in sesame oil. If a precipitate appears, the drug should be heated to 37 ° C, and the precipitate will dissolve without loss of activity of the active substance.

Drug interactions Fluphenazine

It should not be combined with drugs that contain reserpine. When used simultaneously with other drugs that have a depressant effect on the central nervous system (anesthetics, narcotic analgesics, ethanol and drugs containing it, barbiturates, tranquilizers, etc.), the depressive effect, as well as respiratory depression, may be enhanced. Prescription together with tricyclic antidepressants, maprotiline or MAO inhibitors increases the risk of developing neuroleptic malignant syndrome; with drugs for the treatment of hyperthyroidism - increases the risk of developing agranulocytosis; with other drugs that cause extrapyramidal reactions - increases the frequency and severity of extrapyramidal disorders; with antihypertensive drugs - increases the severity of orthostatic reactions. Weakens the vasoconstrictor effect of ephedrine. Antacids, antiparkinsonian drugs, lithium preparations may interfere with the absorption of fluphenazine. Hepatotoxic drugs increase the risk of developing hepatotoxic effects. May mask some manifestations of ototoxicity (tinnitus, dizziness) of ototoxic drugs, especially antibiotics. During treatment, the administration of epinephrine should be avoided (due to the possibility of changing the effect of epinephrine and further reducing blood pressure). Reduces the effectiveness of antiepileptic drugs, the antiparkinsonian effect of levodopa (due to the blockade of dopamine receptors), as well as the effects of amphetamines, clonidine and guanethidine. Increases the effectiveness of anticholinergic drugs, while the severity of its own antipsychotic effect may decrease.

List of pharmacies where you can buy Fluphenazine:

Moscow
Saint Petersburg

FLUPHENAZINE

Pharmacological properties

Fluphenazine is a strong, long-acting antipsychotic.
It has a pronounced antipsychotic effect, combined with some activating effect, as well as a moderate sedative effect. Has an antiemetic effect. The mechanism of action is due to a blocking effect on central dopaminergic receptors with a moderate effect on noradrenergic receptors. Unlike other phenothiazine derivatives, it is characterized by a stronger effect (25 times greater than chlorpromazine in neuroleptic activity) and less pronounced extrapyramidal and somatic disorders. Particularly effective for malignant nuclear (hebephrenic, catatonic, early paranoid forms) and long-term schizophrenia. In the form of decanoate (oil solution), it has a long-lasting effect due to the gradual release of the active substance; after a single intramuscular injection, it acts, depending on the dose, for 1–2 weeks or more.

It is quickly and almost completely absorbed after oral administration. Penetrates the BBB and placental barrier. Excreted in urine and partially in bile.

Indications

Neurosis-like and hallucinatory disorders, various forms of schizophrenia, especially in the presence of soporotic-catatonic disorders, paranoid states occurring with an affect of fear, with a sluggish course of the process with a predominance of depressive-apathetic states.

Application

The solution is injected deeply intramuscularly. The recommended dose is 12.5–25 mg once every 2–4 weeks. It is possible to increase the single dose to 50 mg, in some cases - up to 100 mg.

Contraindications

Coma; severe cerebral atherosclerosis, organic brain lesions; severe dysfunction of the liver and kidneys; pheochromocytoma; blood diseases; prostatic hypertrophy; severe depression; hypersensitivity to phenothiazines.

Side effects

Possible extrapyramidal disorders, tardive dyskinesia, hyperkinesia of the facial muscles, increased fatigue, dizziness, impaired intellectual function, convulsive reactions, dry mouth, nausea, constipation, cardiac arrhythmias, galactorrhea, menstrual irregularities, photosensitivity, leukopenia, thrombocytopenia, dysfunction liver, allergic reactions.

special instructions

Use with caution for liver diseases, arrhythmia, thyrotoxicosis, epilepsy, Parkinson's disease, angle-closure glaucoma.

Fluphenazine should be dosed with particular care when treating patients who work in high temperatures, have contact with fluoride-containing insecticides, and elderly patients.

Prescription of fluphenazine during pregnancy is possible only under strict indications. If it is necessary to prescribe during breastfeeding, breastfeeding should be discontinued.

During the treatment period, it is necessary to refrain from potentially dangerous activities that require increased attention, speed of mental and motor reactions.