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Pharmacological properties

Prochlorperazine maleate is a phenothiazine derivative.

Prochlorperazine has a wide spectrum of activity due to its inhibitory effect on the central nervous system, blocking of α-adrenergic receptors and its weak antimuscarinic effect. It inhibits dopamine and prolactin-inhibiting factor, thus stimulating the release of prolactin and accelerating the metabolism of dopamine in the brain. There is evidence that the therapeutic effect in mental conditions is due to the antagonistic effect of prochlorperazine on dopaminergic CNS receptors.

Prochlorperazine has a sedative effect, but in most cases tolerance develops quickly. Prochlorperazine exhibits antiemetic and antipruritic effects and blocks the action of serotonin. In addition, prochlorperazine has a slight antihistamine effect and a weak blocking effect on the ganglia. Also, prochlorperazine has an inhibitory effect on the center of thermoregulation, a relaxing effect on smooth muscles, and has membrane-stabilizing and local anesthetic properties. The effect of prochlorperazine on the autonomic nervous system leads to vasodilation, arterial hypotension, tachycardia, hyposalivation and decreased secretion of gastric juice.

Pharmacokinetics Prochlorperazine is well absorbed in the gastrointestinal tract, but undergoes a significant degree of presystemic metabolism in the intestinal wall. It is also actively metabolized in the liver and excreted in urine and bile. After oral administration of prochlorperazine, its concentration in blood plasma is significantly lower than after its administration in / m. There is no direct correlation between the concentration of prochlorperazine and its metabolites in blood plasma and therapeutic effect.

Prochlorperazine can be metabolized by hydroxylation and conjugation with glucuronic acid, N-oxidation, sulfur atom oxidation and dealkylation. T½ from blood plasma is only a few hours, but the excretion of metabolites can be very long. Prochlorperazine largely binds to plasma proteins and is well distributed throughout the body, its metabolites cross the placental barrier and pass into breast milk. The metabolic rate and excretion of prochlorperazine is reduced in elderly patients.

Indications

Dizziness that occurs with Menter syndrome, inflammation of the inner ear.

Nausea and vomiting that occurs for any reason, including migraine.

It can also be used as an additional drug for the short-term treatment of anxiety conditions.

Application

Adults prevention of nausea and vomiting: 1-2 tablets (5-10 mg) 2-3 times a day.

Treatment of nausea and vomiting: 4 tablets (20 mg) immediately after the onset of symptoms, and if necessary 2 more tablets (10 mg) after 2 hours.

Dizziness: 1 tablet (5 mg) 3 times a day. If necessary, the daily dose of the drug can be increased to 6 tablets (30 mg). After a few weeks, the daily dose can be gradually reduced to 1-2 tablets (5-10 mg).

As an additional drug for the short-term treatment of anxiety conditions: 1 tablet (5 mg) 3-4 times a day at the beginning of treatment. If necessary, the daily dose of the drug can be increased to 8 tablets (40 mg) in 3-4 doses.

Elderly patients. Elderly patients are recommended a lower daily dose of prochlorperazine.

Contraindications

Sensitivity to prochlorperazine or other components of the drug.

Side effects

From the immune system: angioedema, urticaria.

On the part of the blood and lymphatic system: leukopenia, agranulocytosis.

From the endocrine system: hyperprolactinemia, which can lead to galactorrhea; gynecomastia; amenorrhea, impotence; glucose intolerance; hyperglycemia.

From the nervous system: acute dystonia or dyskinesia; akathisia; symptoms of parkinsonism (tremor, stiffness, akinesia, or others); insomnia; anxiety arousal.

From the side of the organ of vision: ophthalmic changes.

From the side of the heart: changes on the ECG (lengthening of the Q – T interval, depression of the S – T segment, changes in the U and / or T waves); heart rhythm disturbances (ventricular arrhythmia and atrial arrhythmias, AV block, ventricular tachycardia, which can lead to ventricular fibrillation or cardiac arrest); sudden death.

From the vessels: hypotension, venous thromboembolism (including cases of pulmonary embolism), deep vein thrombosis.

From the digestive tract: dry mouth.

On the part of the respiratory system: respiratory depression, nasal congestion.

From the hepatobiliary system: jaundice.

On the part of the skin and subcutaneous tissue: metallic gray-purple staining of the skin; skin rashes; photosensitization.

General disorders: malignant antipsychotic syndrome (hyperthermia, rigidity, autonomic dysfunctions and impaired consciousness).

special instructions

Vertinex should not be used in patients with impaired liver or kidney function, Parkinsons disease, hypothyroidism, heart failure, pheochromocytoma, myasthenia gravis and prostatic hypertrophy. vertinex should not be prescribed to patients with a known hypersensitivity to prochlorperazine, with angle-closure glaucoma or a history of agranulocytosis.

Care should be taken to monitor the condition of patients with a history of epilepsy or seizures, since prochlorperazine may lower the threshold for seizure readiness.

Since there are no data on cases of agranulocytosis during prochlorperazine therapy, regular monitoring of the data of a general detailed blood test is recommended. If a patient develops an infection of an unexplained genesis or fever, the necessary hematological studies should immediately be performed to detect blood dysrasia.

It is necessary to stop treatment with Vertinex if there is a fever of unknown origin, since it can be a sign of the development of a malignant antipsychotic syndrome (pallor, hyperthermia, autonomic dysfunction, impaired consciousness, muscle stiffness). Signs of autonomic dysfunction, such as hyperhidrosis and unstable blood pressure, may precede the onset of hyperthermia and be early signs of malignant antipsychotic syndrome. Although this syndrome may also have an idiosyncratic origin, the factors contributing to its development are dehydration and organic brain diseases.

Since data on the occurrence of acute withdrawal symptoms, including nausea, vomiting, insomnia, extrapyramidal reactions, after a sharp cessation of taking high doses of antipsychotics, a gradual cancellation of Vertinex is advisable.

Prochlorperazine, like other antipsychotics phenothiazines, can potentiate the lengthening of the Q – T interval, which increases the risk of ventricular tachycardia such as pirouette, which is deadly (sudden death). The risk of lengthening the Q – T interval is increased if the patient has bradycardia, hypokalemia, as well as congenital or acquired (drug-induced) lengthening of the Q – T interval. Therefore, before the appointment of Vertinex, it is necessary to fully evaluate the risk-benefit ratio. It is recommended to conduct appropriate clinical and laboratory tests (for example, biochemical analysis of blood and ECG) before treatment with Vertinex and during the initial phase of treatment, and as necessary during treatment, to exclude possible risk factors (such as heart disease, prolongation of the Q – T interval family history, metabolic disorders such as hypokalemia, hypocalcemia or hypomagnesemia, history of starvation, alcohol abuse, other concomitant therapy drugs that extend the Q – T interval) (seeINTERACTION AND ADVERSE REACTIONS).

Concomitant therapy with other antipsychotics should be avoided (see INTERACTION).

Vertinex should be used with caution in patients with risk factors for acute cerebrovascular accident, since data have been obtained on an increased risk of cerebrovascular complications during prochlorperazine therapy.

Like other antipsychotic drugs, Vertinex should not be taken as monotherapy if the patient is dominated by manifestations of depression. However, it can be added to antidepressant therapy for the treatment of manic-depressive psychosis.

Due to the risk of photosensitization, patients who are receiving Vertinex treatment should avoid exposure to direct sunlight.

The drug should be used with caution in elderly patients, especially in very hot or very cold weather, because of the risk of developing hyper- or hypothermia in them. In addition, elderly patients are prone to postural hypotension. Also, patients of this age category have an increased risk of drug parkinsonism, especially after prolonged use of the drug Vertinex. Elderly patients are recommended to prescribe a lower daily dose of prochlorperazine, especially at the beginning of treatment.

An increased mortality rate is observed in elderly patients with dementia.

There is evidence of an increased risk of mortality in elderly patients with dementia treated with antipsychotic drugs. Vertinex is not intended to treat dementia-related behaviors.

Increased risk of venous thromboembolism (VTE). Before and during Vertinex drug therapy, it is necessary to identify all possible risk factors for the development of VTE and, if possible, take the necessary preventive measures.

Hyperglycemia and glucose intolerance. Patients with diabetes mellitus or patients with risk factors for the development of this disease require appropriate glycemic control before and during treatment.

Excipients. The drug contains lactose. Patients with rare inherited diseases, such as galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption, should not take this drug.

Use during pregnancy and lactation. There is insufficient evidence for the safety of prochlorperazine during pregnancy, therefore, the use of the drug Vertinex during this period should be avoided, unless the potential benefit of using the drug exceeds the possible risk. Since antipsychotics can prolong labor activity, the drug should be discontinued during childbirth until the cervix opens 3-4 cm. There is a risk of undesirable effects of prochlorperazine on newborns, which may result in a low assessment of the condition of the newborn on the Apgar scale, lethargy, or on the contrary, paradoxical agitation and tremor.

Since newborns whose mothers took prochlorperazine in the third trimester of pregnancy have a risk of undesirable effects, including extrapyramidal symptoms and / or withdrawal symptoms (agitation, hypertension, hypotension, tremor, drowsiness, respiratory or nutritional disorders), these children should be carefully monitored .

Since prochlorperazine can pass into breast milk, breast-feeding should be discontinued during treatment.

The ability to influence the reaction rate when driving vehicles or other mechanisms. Patients should be warned of drowsiness in the early days of treatment. It is not recommended to drive or operate machinery.

Children.There is not enough data regarding the use of prochlorperazine in children, therefore, Vertinex should not be prescribed in this age group of patients.

Interactions

In case of overdose with vertinex, epinephrine should not be used (see overdose).

The inhibitory effect of the drug Vertinex on the central nervous system can enhance (additive) alcohol, barbiturates and other sedatives. Possible respiratory depression.

Anticholinergics may decrease the antipsychotic effect of Vertinex.

The mild anticholinergic action of Vertinex can be enhanced by other anticholinergic drugs, which can lead to constipation, heat stroke, etc.

Parkinson’s antacids, drugs, and lithium preparations may impair the absorption of Vertinex.

If treatment with extrapyramidal symptoms caused by the action of antipsychotics is necessary, anticholinergic antiparkinsonian drugs should be preferred over levodopa, since antipsychotics counteract the antiparkinsonian effect of dopaminergic drugs.

High doses of antipsychotics reduce the hypoglycemic effect of antidiabetic drugs, so it may be necessary to adjust their dose.

Neuroleptic drugs can enhance the hypotensive effect of most antihypertensive drugs, especially α-adrenergic blockers.

The drug Vertinex, like other phenothiazine antipsychotics, can suppress the effect of certain drugs: amphetamine, levodopa, clonidine, gunatedine and adrenaline.

There is evidence of a change in the concentration of certain drugs in the blood plasma (e.g. propranolol, phenobarbital), which does not have clinical significance.

With the simultaneous use of prochlorperazine and desferoxamine, transient metabolic encephalopathy was observed, which was characterized by a loss of consciousness for 48–72 hours.

There is an increased risk of arrhythmia with the simultaneous use of prochlorperazine and drugs that extend the Q – T interval (including some antiarrhythmic drugs, antidepressants and other antipsychotic drugs), and drugs that disrupt the electrolyte balance.

An increased risk of agranulocytosis with the simultaneous use of prochlorperazine and drugs that have a myelosuppressive effect (carbamazepine, some antibiotics and cytotoxic drugs) was identified.

Occasionally, neurotoxic effects have been reported with the simultaneous administration of antipsychotics and lithium preparations.

Overdose

Overdose symptoms: drowsiness or loss of consciousness, arterial hypotension, tachycardia, ECG changes, ventricular arrhythmias, hypothermia, extrapyramidal dyskinesia.

Treatment. First aid. If no more than 4 hours have elapsed since the intake of the toxic dose of the drug, gastric lavage should be performed. Activated carbon must be given. There is no specific antidote. Supportive and symptomatic treatment is recommended.

Arterial hypotension. In mild cases, raising the patient’s upper limbs is a sufficient measure. In severe cases, there may be a need for infusion therapy to correct the total volume of fluid. If fluid replacement is insufficient to correct arterial hypotension, agents with a positive inotropic effect, such as dopamine, can be used.

It is not recommended to use peripheral vasoconstrictors and adrenaline.

Ventricular and supraventricular tachyarrhythmias. Generally, maintaining a normal body temperature, correcting general BCC and / or metabolic disorders are effective measures for treating tachyarrhythmias.If the above measures are ineffective or if tachyarrhythmia is life threatening, the necessary antiarrhythmic therapy should be carried out. It is not recommended to use lidocaine or long-acting antiarrhythmic drugs.

Oppression of the central nervous system. It is necessary to use means aimed at supporting breathing, including mechanical ventilation if necessary.

Dystonia. In severe cases, the manifestations of dystonia can be corrected with procyclidine (5–10 mg) or orphenadrine (20–40 mg) iv or v / m.

Convulsive syndrome. Diazepam must be used.

Malignant antipsychotic syndrome. Physical cooling methods must be applied. Dantrolene sodium may also be used.

Storage conditions

At a temperature not exceeding 25 ° C.