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.

Cochrane

People with schizophrenia often hear voices or see things (hallucinations) and have strange beliefs (delusions). The main treatment for these symptoms of schizophrenia is antipsychotic medications (antipsychotics), which can be taken by mouth (pills) or by injection (depot medications). Fluphenazine was one of the first antipsychotics to be produced in a depot form. Depot is produced in two forms (decanoate and enanthate). Depot injections are often used in people who refuse or forget to take pills (showing poor compliance or adherence to therapy). Fluphenazine is an old antipsychotic drug (neuroleptic) that is very effective in treating schizophrenia. However, compared to newer antipsychotic drugs (antipsychotics), fluphenazine has serious side effects (such as involuntary movements, shaking (tremors), muscle rigidity, and the inability to sit still - restlessness) and is known to lower mood.

This review aims to investigate the effects of fluphenazine (decanoate and enanthate) in schizophrenia. A search for relevant randomized controlled trials was conducted in February 2011 and October 16, 2013. The authors were able to include and extract data from 73 studies with a total of 4870 participants. There were more studies on fluphenazine decanoate than on enanthate. The review authors rated the quality of the evidence from the included trials as low or very low. Long-term results from only one clinical trial showed that fluphenazine decanoate reduced relapse rates compared with placebo (a "dummy treatment"). Three studies showed that fluphenazine decanoate caused fewer general movement disorders than oral (oral) antipsychotics. However, other results showed that, overall, the effects and outcomes, including adverse effects of fluphenazine (decanoate and enanthate), are similar to other oral and depot antipsychotics. None of the studies reported important outcomes and information on service use, hospital visits, satisfaction with care and costs.

Depot injections have an advantage over tablets (oral administration of the drug) from the point of view of people taking therapy (compliance and adherence to treatment). However, this must be weighed against the potential for serious side effects such as involuntary movements, shaking (tremors), muscle stiffness, inability to sit still (restlessness) and depressed mood. The results did not provide convincing evidence that fluphenazine depot formulations caused more adverse effects than other antipsychotic agents.

This should be considered in future large-scale, high-quality studies.

This plain language summary was written by consumer representative Ben Gray of Rethink Mental Illness, a UK charity.

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.

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

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.