Action And Clinical Pharmacology: Thioproperazine is a potent neuroleptic with antipsychotic properties.
Thioproperazine has a marked cataleptic and antiapomorphine activity associated with relatively slight sedative, hypothermic and spasmolytic effects. It is virtually without antiserotonin and hypotensive action and has no antihistaminic property.
Indications And Clinical Uses: All types of acute and chronic schizophrenia, including those which did not respond to the usual neuroleptics; manic syndromes.
Contra-Indications: Comatose or depressive states including those induced by CNS depressants; Parkinson’s disease; blood dyscrasias; in patients with spastic diseases and in senile patients with pre-existing Parkinson-like symptoms; in children under 3 years of age and in patients generally sensitive to phenothiazines.
Precautions: Before starting treatment with thioproperazine, it is recommended to ascertain that the cardiovascular system and the liver and kidney functions are unimpaired.
Treatment should be initiated preferably by the oral route with a low initial dosage, increased progressively.
Since thioproperazine may potentiate the action of general anesthetics, morphine-like analgesics, barbiturates, alcohol, and other CNS depressants, care should be exercised when these agents are given with it.
The antiemetic effect of thioproperazine may obscure symptoms such as vomiting and nausea, normally associated with some types of organic disease (intestinal obstruction and brain tumor).
Thiproperazine should be used cautiously in patients with a history of seizures.
Pregnancy: The safety of thioproperazine in pregnant women has not been clearly established, therefore it should not be used during the first trimester of pregnancy.
Manufacturers’ Warnings In Clinical States: Treatment should be discontinued if a severe neurologic syndrome is observed, especially when hypertonia is accompanied by dysphagia and/or marked autonomic disturbances.
Adverse Reactions: Neuromuscular (extrapyramidal) reactions are the most frequently observed. They are usually dose-related and generally subside when the dose is reduced or when the drug is temporarily discontinued. Administration of an antiparkinsonian agent is usually, but not always, effective in reversing the neuromuscular reactions associated with this and other phenothiazines.
Anxiety or apathy, elation or depression, drowsiness and/or insomnia are not infrequently observed.
Occasional disturbances of accommodation, rare cases of headache and exceptionally, cases of nausea and vomiting, constipation or diarrhea have been reported. Lacrimation, sialorrhea and profuse sweating are more frequent. Oliguria may occur.
Symptoms And Treatment Of Overdose: Symptoms: Overdosage may result in severe extrapyramidal symptoms with dysphagia, marked sialorrhea, persistent and rapidly increasing hyperthermia, pulmonary syndrome, state of shock with pallor and profuse sweating, which may be followed by collapse and coma. tag_Treatment
Treatment: There is no specific antidote. When mild symptoms are present (e.g., in regular therapy) corrective measures are usually sufficient:
Administration of thioproperazine should be discontinued.
Against Dyskinetic Manifestations: An antiparkinsonian or chloral hydrate, but the latter should be used with caution, as it may further depress the respiration.
In the presence of severe symptoms (e.g., in cases of overdosage) in addition to the above corrective measures, the following supportive treatment should be carried out:
Gastric Lavage: Because of the antiemetic effect of thioproperazine, centrally acting emetics will remain ineffective.
In cases of severe hypotension or collapse: norepinephrine and adrenocortical hormones to restore blood pressure. Since phenothiazines are known to reverse the pressor action of epinephrine, the latter should not be used as it may further lower blood pressure.
Against Respiratory Depression: oxygen inhalation and, if necessary, tracheal intubation.
Against Dehydration: i.v. infusion of dextrose in normal saline.
Against Respiratory Infection: broad spectrum antibiotics.
Dosage And Administration: Initial Treatment: Adults: Oral route (usual route of administration): It is recommended to start treatment at a low dosage of about 5 mg per day in a single dose or in divided doses. This initial dosage is gradually increased by the same amount every 2 to 3 days until the usual effective dosage of 30 to 40 mg per day is reached. In some cases higher dosages of 90 mg or more per day, are necessary to control the psychotic manifestations.
Children: Oral Route: In children over 10 years: Start treatment with a daily dosage of 1 to 3 mg following the method of treatment described for adults.
Maintenance Therapy: Adults and Children: Dosage should be reduced gradually to the lowest effective level, which may be as low as a few mg per day and maintained as long as necessary.
Other Method of Treatment: Occasionally, thioproperazine is prescribed in the form of discontinuous treatment at 5 or 10 mg, 3 times a day, until the onset of severe extrapyramidal symptoms. Then, treatment is discontinued until spontaneous full recovery from these symptoms. The same course of therapy is repeated for at least 3 consecutive treatments. Discontinuous treatment should be reserved for resistant cases, and performed in hospitalized patients, under close medical supervision.
Availability And Storage: Each scored orange tablet contains: thioproperazine base (as the mesylate) 10 mg. Nonmedicinal ingredients: acetic anhydride, calcium phosphate, carnauba wax, cellulose, colloidal silicon dioxide, diethyl phthalate, FD&C Yellow No 6 aluminum lake, magnesium stearate, polacrilin potassium, sodium oleate, titane oxide and zein. Tartrazine-free. Bottles of 100 and 500.
MAJEPTIL® Rhône-Poulenc Rorer Thioproperazine Mesylate Neuroleptic