Prochlorperazine Maleate

INDICATIONS AND USAGE For control of severe nausea and vomiting. For the treatment of schizophrenia. Prochlorperazine maleate tablets are effective for the short-term treatment of generalized non-psychotic anxiety. However, prochlorperazine maleate tablets are not the first drug to be used in therapy for most patients with non-psychotic anxiety, because certain risks associated with its use are not shared by common alternative treatments (e.g., benzodiazepines). When used in the treatment of non-psychotic anxiety, prochlorperazine maleate tablets should not be administered at doses of more than 20 mg per day or for longer than 12 weeks, because the use of prochlorperazine maleate tablets at higher doses or for longer intervals may cause persistent tardive dyskinesia that may prove irreversible (see WARNINGS ). The effectiveness of prochlorperazine maleate tablets as treatment for non-psychotic anxiety was established in 4-week clinical studies of outpatients with generalized anxiety disorder. This evidence does not predict that prochlorperazine maleate tablets will be useful in patients with other non-psychotic conditions in which anxiety, or signs that mimic anxiety, are found (e.g., physical illness, organic mental conditions, agitated depression, character pathologies, etc.). Prochlorperazine maleate tablets have not been shown effective in the management of behavioral complications in patients with mental retardation.

DOSAGE AND ADMINISTRATION ADULTS (For children’s dosage and administration, see below). Dosage should be increased more gradually in debilitated or emaciated patients. Elderly Patients: In general, dosages in the lower range are sufficient for most elderly patients. Since they appear to be more susceptible to hypotension and neuromuscular reac‐tions, such patients should be observed closely. Dosage should be tailored to the individual, response carefully moni‐tored, and dosage adjusted accordingly. Dosage should be increased more gradually in elderly patients. 1. To Control Severe Nausea and Vomiting: Adjust dosage to the response of the individual. Begin with the lowest recommended dosage. Oral Dosage-Tablets: Usually one 5 mg or 10 mg tablet, 3 times or 4 times daily. Daily dosages above 40 mg should be used only in resistant cases. 2. In Adult Psychiatric Disorders: Adjust dosage to the response of the individual and according to the severity of the condition. Begin with the lowest recom‐mended dose. Although response ordinarily is seen within a day or 2, longer treatment is usually required before maximal improvement is seen. Oral Dosage: Non-Psychotic-Anxiety -Usual dosage is 5 mg, 3 times or 4 times daily. Do not administer in doses of more than 20 mg per day or for longer than 12 weeks. Psychotic Disorders including Schizophrenia - In relatively mild conditions, as seen in private psychiatric practice or in outpatient clinics, dosage is 5 mg or 10 mg, 3 times or 4 times daily. In moderate to severe conditions, for hospitalized or adequate‐ly supervised patients, usual starting dosage is 10 mg, 3 times or 4 times daily. Increase dosage gradually until symptoms are con‐trolled or side effects become bothersome. When dosage is increased by small increments every 2 days or 3 days, side effects either do not occur or are easily controlled. Some patients respond satisfactorily on 50 mg to 75 mg daily. In more severe dis ‐ turbances, optimum dosage is usually 100 mg to 150 mg daily. DOSAGE AND ADMINISTRATION CHILDREN Do not use in pediatric surgery. Children seem more prone to develop extrapyramidal reac‐tions, even on moderate doses. Therefore, use lowest effec‐tive dosage. Tell parents not to exceed prescribed dosage, since the possibility for adverse reactions increases as dosage rises. Occasionally the patient may react to the drug with signs of restlessness and excitement; if this occurs, do not administer additional doses. Take particular precaution in administering the drug to children with acute illnesses or dehydration (see under Dystonias). 1. Severe Nausea and Vomiting in Children: Prochlorperazine maleate tablets should not be used in pediatric patients under 20 pounds in weight or 2 years of age. It should not be used in conditions for which children’s dosages have not been established. Dosage and frequency of administration should be adjusted according to the severity of the symptoms and the response of the patient. The duration of activity following intra‐muscular administration may last up to 12 hours. Subsequent doses may be given by the same route if necessary. Oral Dosage: More than 1 day’s therapy is seldom necessary. Weight Usual Dosage Not to Exceed under 20 lbs not recommended 20 lbs to 29 lbs 21⁄2 mg, 1 time or 2 times a day 7.5 mg per day 30 lbs to 39 lbs 21⁄2 mg, 2 times or 3 times a day 10 mg per day 40 lbs to 85 lbs 21⁄2 mg, 3 times a day or 5 mg, 2 times a day 15 mg per day 2. Children with Schizophrenia: Oral Dosage: For children 2 years to 12 years, starting dosage is 21⁄2 mg, 2 times or 3 times daily. Do not give more than 10 mg the first day. Then increase dosage according to patient’s response. FOR AGES 2 years to 5 years, total daily dosage usually does not exceed 20 mg. FOR AGES 6 years to 12 years, total daily dosage usually does not exceed 25 mg.

CONTRAINDICATIONS Do not use in patients with known hypersensitivity to phenothiazines. Do not use in comatose states or in the presence of large amounts of central nervous system depressants (alcohol, barbiturates, narcotics, etc.). Do not use in pediatric surgery. Do not use in pediatric patients under 2 years of age or under 20 lbs. Do not use in children for conditions for which dosage has not been established.

ADVERSE REACTIONS Drowsiness, dizziness, amenorrhea, blurred vision, skin reactions and hypotension may occur. Neuroleptic Malignant Syndrome (NMS) has been reported in association with antipsychotic drugs (see WARNINGS ). Cholestatic jaundice has occurred. If fever with grippe-like symptoms occurs, appropriate liver studies should be conducted. If tests indicate an abnormality, stop treatment. There have been a few observations of fatty changes in the livers of patients who have died while receiving the drug. No causal relationship has been established. Leukopenia and agranulocytosis have occurred. Warn patients to report the sudden appearance of sore throat or other signs of infection. If white blood cell and differential counts indicate leukocyte depression, stop treatment and start antibiotic and other suitable therapy. Neuromuscular (Extrapyramidal) Reactions These symptoms are seen in a significant number of hospitalized mental patients. They may be characterized by motor restlessness, be of the dystonic type, or they may resemble parkinsonism. Depending on the severity of symptoms, dosage should be reduced or discontinued. If therapy is reinstituted, it should be at a lower dosage. Should these symptoms occur in children or pregnant patients, the drug should be stopped and not reinstituted. In most cases barbiturates by suitable route of administration will suffice. (Or, injectable Benadryl ® || may be useful.) In more severe cases, the administration of an anti-parkinsonism agent, except levodopa (see PDR ), usually produces rapid reversal of symptoms. Suitable supportive measures such as maintaining a clear airway and adequate hydration should be employed. Dystonia Class effect: Symptoms of dystonia, prolonged abnormal contractions of muscle groups, may occur in susceptible individuals during the first few days of treatment. Dystonic symptoms include: spasm of the neck muscles, sometimes progressing to tightness of the throat, swallowing difficulty, difficulty breathing, and/or protrusion of the tongue. While these symptoms can occur at low doses, they occur more frequently and with greater severity with high potency and at higher doses of first generation antipsychotic drugs. An elevated risk of acute dystonia is observed in males and younger age groups. These usually subside within a few hours, and almost always within 24 to 48 hours, after the drug has been discontinued. Motor Restlessness: Symptoms may include agitation or jitteriness and sometimes insomnia. These symptoms often disappear spontaneously. At times these symptoms may be similar to the original neurotic or psychotic symptoms. Dosage should not be increased until these side effects have subsided. If these symptoms become too troublesome, they can usually be controlled by a reduction of dosage or change of drug. Treatment with anti-parkinsonian agents, benzodiazepines or propranolol may be helpful. Pseudo-parkinsonism: Symptoms may include: mask-like facies; drooling; tremors; pillrolling motion; cogwheel rigidity; and shuffling gait. Reassurance and sedation are important. In most cases these symptoms are readily controlled when an anti-parkinsonism agent is administered concomitantly. Anti-parkinsonism agents should be used only when required. Generally, therapy of a few weeks to 2 or 3 months will suffice. After this time patients should be evaluated to determine their need for continued treatment. (Note: Levodopa has not been found effective in pseudo-parkinsonism.) Occasionally it is necessary to lower the dosage of prochlorperazine or to discontinue the drug. Tardive Dyskinesia: As with all antipsychotic agents, tardive dyskinesia may appear in some patients on long-term therapy or may appear after drug therapy has been discontinued. The syndrome can also develop, although much less frequently, after relatively brief treatment periods at low doses. This syndrome appears in all age groups. Although its prevalence appears to be highest among elderly …

DESCRIPTION Prochlorperazine is a phenothiazine derivative, present in prochlorperazine maleate tablets, USP as the maleate. Its chemical name is 2-chloro-10-[3-(4-methyl-1-piperazinyl)propyl]-10 H -phenothiazine ( Z )-2-butenedioate (1:2). Prochlorperazine maleate, USP Prochlorperazine maleate, USP is classified as an anti-emetic and antipsychotic agent. Prochlorperazine maleate, USP, has the molecular formula C 20 H 24 ClN 3 S•2C 4 H 4 O 4 , and the molecular weight is 606.09 g/mol. Prochlorperazine maleate, USP, is a white or pale-yellow crystalline powder. It is slightly soluble in warm chloroform and practically insoluble in water and alcohol. Each film-coated tablet for oral administration contains prochlorperazine maleate, USP equivalent to 5 mg or 10 mg of prochlorperazine. In addition, each film-coated tablet contains the following inactive ingredients consist of colloidal silicon dioxide, corn starch, D&C yellow no. 10 aluminum lake, FD&C yellow no. 6, FD&C blue no. 2, hypromellose, lactose monohydrate, magnesium stearate, polyethylene glycol, polysorbate 80, and titanium dioxide. Structure of Prochlorperazine

OVERDOSAGE (See also ADVERSE REACTIONS . ) SYMPTOMS –Primarily involvement of the extrapyramidal mechanism producing some of the dystonic reactions described above. Symptoms of central nervous system depression to the point of somnolence or coma. Agitation and restlessness may also occur. Other possible manifestations include convulsions, EKG changes and cardiac arrhythmias, fever and autonomic reactions such as hypotension, dry mouth and ileus. TREATMENT–It is important to determine other medications taken by the patient since multiple-dose therapy is common in overdosage situations. Treatment is essentially symptomatic and supportive. Early gastric lavage is helpful. Keep patient under observation and maintain an open airway, since involvement of the extrapyramidal mechanism may produce dysphagia and respiratory difficulty in severe overdosage. Do not attempt to induce emesis because a dystonic reaction of the head or neck may develop that could result in aspiration of vomitus. Extrapyramidal symptoms may be treated with anti-parkinsonism drugs, barbiturates or Benadryl . See prescribing information for these products. Care should be taken to avoid increasing respiratory depression. If administration of a stimulant is desirable, amphetamine, dextroamphetamine or caffeine with sodium benzoate is recommended. Stimulants that may cause convulsions (e.g., picrotoxin or pentylenetetrazol) should be avoided. If hypotension occurs, the standard measures for managing circulatory shock should be initiated. If it is desirable to administer a vasoconstrictor, Levophed and Neo-Synephrine are most suitable. Other pressor agents, including epinephrine, are not recommended because phenothiazine derivatives may reverse the usual elevating action of these agents and cause a further lowering of blood pressure. Limited experience indicates that phenothiazines are not dialyzable.

HOW SUPPLIED Prochlorperazine Maleate Tablets USP, 5 mg are supplied as yellow, round, film-coated tablet debossed with “J” on the top and “5” on the bottom of the score line on one side and plain on the other side. They are available as follows: Bottles of 100 with child-resistant closure: NDC 60219-2038-1 Bottles of 1,000: NDC 60219-2038-7 Prochlorperazine Maleate Tablets USP, 10 mg are supplied as yellow, round, film-coated tablet debossed with “J” on the top and “7” on the bottom of the score line on one side and plain on the other side. They are available as follows: Bottles of 100 with child-resistant closure: NDC 60219-2039-1 Bottles of 1,000: NDC 60219-2039-7 Store at 20° to 25°C (68° to 77°F) ; excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature]. Protect from light. Keep container tightly closed. Important: Use safety closure when dispensing this product unless otherwise directed by physician or requested by purchaser. Dispense in tight, light-resistant container. Keep this and all medications out of the reach of children. To report SUSPECTED ADVERSE REACTIONS, contact Amneal Pharmaceuticals at 1-877-835-5472 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . All trademarks are the property of their respective owners. Manufactured by: Amneal Pharmaceuticals Pvt. Ltd. Oral Solid Dosage Unit Ahmedabad 382213, INDIA Distributed by: Amneal Pharmaceuticals LLC Bridgewater, NJ 08807 Rev. 11-2024-04