Prochlorperazine Information
Prochlorperazine () Warning
Prochlorperazine () Description
Prochlorperazine () , a phenothiazine derivative is designated chemically as 2-Chloro -10- [3-(4-methyl-1-piperazinyl)propyl]phenothiazine with the following structural formula:
Each rectal suppository contains 25 mg Prochlorperazine () with glycerin, glyceryl monostearate, hydrogenated coconut oil fatty acids, hydrogenated palm kernel oil fatty acids.
Prochlorperazine () Clinical Pharmacology
Prochlorperazine () is a propylpiperazine derivative of phenothiazine. Like other phenothiazines, it exerts an antiemetic effect through a depressant action on the chemoreceptor trigger zone.
Prochlorperazine () Indications And Usage
Prochlorperazine () 25 mg suppositories are indicated in the control of severe nausea and vomiting in adults.
Prochlorperazine () Contraindications
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 children under 2 years of age or under 20 lbs. Do not use in children for conditions for which dosage has not been established.
Prochlorperazine () Warnings
Both the risk of developing the syndrome and the likelihood that it will become irreversible are believed to increase as the duration of treatment and the total cumulative dose of neuroleptic drugs administered to the patient increase. However, the syndrome can develop, although much less commonly, after relatively brief treatment periods at low doses.
There is no known treatment for established cases of tardive dyskinesia, although the syndrome may remit, partially or completely, if neuroleptic treatment is withdrawn. Neuroleptic treatment itself, however, may suppress (or partially suppress) the signs and symptoms of the syndrome and thereby may possibly mask the underlying disease process.
The effect that symptomatic suppression has upon the long-term course of the syndrome is unknown.
Given these considerations, neuroleptics should be prescribed in a manner that is most likely to minimize the occurrence of tardive dyskinesia. Chronic neuroleptic treatment should generally be reserved for patients who suffer from a chronic illness that, 1) is known to respond to neuroleptic drugs, and, 2) for whom alternative, equally effective, but potentially less harmful treatments are available or appropriate. In patients who do require chronic treatment, the smallest dose and the shortest duration of treatment producing a satisfactory clinical response should be sought. The need for continued treatment should be reassessed periodically.
If signs and symptoms of tardive dyskinesia appear in a patient on neuroleptics, drug discontinuation should be considered. However, some patients may require treatment despite the presence of the syndrome.
For further information about the description of tardive dyskinesia and its clinical detection, please refer to the sections on and .
The diagnostic evaluation of patients with this syndrome is complicated. In arriving at a diagnosis, it is important to identify cases where the clinical presentation includes both serious medical illness (e.g., pneumonia, systemic infection, etc.) and untreated or inadequately treated extrapyramidal signs and symptoms (EPS). Other important considerations in the differential diagnosis include central anticholinergic toxicity, heat stroke, drug fever and primary central nervous system (CNS) pathology.
The management of NMS should include 1) immediate discontinuation of antipsychotic drugs and other drugs not essential to concurrent therapy, 2) intensive symptomatic treatment and medical monitoring, and 3) treatment of any concomitant serious medical problems for which specific treatments are available. There is no general agreement about specific pharmacological treatment regimens for uncomplicated NMS.
If a patient requires antipsychotic drug treatment after recovery from NMS, the potential reintroduction of drug therapy should be carefully considered. The patient should be carefully monitored, since recurrences of NMS have been reported.
Patients with bone marrow depression or who have previously demonstrated a hypersensitivity reaction (e.g., blood dyscrasias, jaundice) with a phenothiazine should not receive any phenothiazine, including Prochlorperazine () unless in the judgment of the physician the potential benefits of treatment outweigh the possible hazards.
Prochlorperazine () may impair mental and/or physical abilities, especially during the first few days of therapy. Therefore, caution patients about activities requiring alertness (e.g., operating vehicles or machinery).
Phenothiazines may intensify or prolong the action of central nervous system depressants (e.g., alcohol, anesthetics, narcotics).
There have been reported instances of prolonged jaundice, extrapyramidal signs, hyperreflexia or hyporeflexia in newborn infants whose mothers received phenothiazines.
Prochlorperazine () Precautions
The antiemetic action of Prochlorperazine () may mask the signs and symptoms of overdosage of other drugs and may obscure the diagnosis and treatment of other conditions such as intestinal obstruction, brain tumor and Reye's syndrome (see ).
When Prochlorperazine () is used with cancer chemotherapeutic drugs, vomiting as a sign of the toxicity of these agents may be obscured by the antiemetic effect of Prochlorperazine () .
Because hypotension may occur, large doses and parenteral administration should be used cautiously in patients with impaired cardiovascular systems. If hypotension occurs after parenteral or oral dosing, place patient in head-low position with legs raised. If a vasoconstrictor is required, norepinephrine bitartrate and phenylephrine hydrochloride are suitable. Other pressor agents, including epinephrine, should not be used because they may cause a paradoxical further lowering of blood pressure.
Aspiration of vomitus has occurred in a few post-surgical patients who have received Prochlorperazine () as an antiemetic. Although no causal relationship has been established, this possibility should be borne in mind during surgical aftercare.
Deep sleep, from which patients can be aroused, and coma have been reported, usually with overdosage.
Neuroleptic drugs elevate prolactin levels; the elevation persists during chronic administration. Tissue culture experiments indicate that approximately one-third of human breast cancers are prolactin dependent , a factor of potential importance if the prescribing of these drugs in contemplated in a patient with a previously detected breast cancer. Although disturbances such as galactorrhea, amenorrhea, gynecomastia and impotence have been reported, the clinical significance of elevated serum prolactin levels is unknown for most patients. An increase in mammary neoplasms has been found in rodents after chronic administration of neuroleptic drugs. Neither clinical nor epidemiologic studies conducted to date, however, have shown an association between chronic administration of these drugs and mammary tumorigenesis; the available evidence is considered too limited to be conclusive at this time.
Chromosomal aberrations in spermatocytes and abnormal sperm have been demonstrated in rodents treated with certain neuroleptics.
As with all drugs which exert an anticholinergic effect and/or cause mydriasis, Prochlorperazine () should be used with caution in patients with glaucoma.
Because phenothiazines may interfere with thermoregulatory mechanisms, use with caution in persons who will be exposed to extreme heat.
Phenothiazines can diminish the effect of oral anticoagulants.
Phenothiazines can produce alpha-adrenergic blockade.
Thiazide diuretics may accentuate the orthostatic hypotension that may occur with phenothiazines.
Antihypertensive effects of guanethidine and related compounds may be counteracted when phenothiazines are used concomitantly.
Concomitant administration of propranolol with phenothiazines results in increased plasma levels of both drugs.
Phenothiazines may lower the convulsive threshold; dosage adjustments of anticonvulsants may be necessary. Potentiation of anticonvulsant effects does not occur. However, it has been reported that phenothiazines may interfere with the metabolism of phenytoin and thus precipitate phenytoin toxicity.
The presence of phenothiazines may produce false positive phenyketonuria (PKU) test results.
Drugs which lower the seizure threshold, including phenothiazine derivatives, should not be used with metrizamide. As with other phenothiazine derivates, Prochlorperazine () should be discontinued at least 48 hours before myelography, should not be resumed for at least 24 hours postprocedure, and should not be used for the control of nausea and vomiting occurring either prior to myelography with metrizamide or postprocedure.
Prochlorperazine () Adverse Reactions
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.
Prochlorperazine () Overdosage
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 diphenhydramine. 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, norepinephrine bitartrate and phenylephrine hydrochloride 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.
Prochlorperazine () How Supplied
For Adults, Prochlorperazine () Suppositories, USP 25 mg in boxes of 12 and 1000 as follows:Box of 12 NDC 0713-0135-12Box of 1000 NDC 0713-0135-10
Prochlorperazine () Package Label
G&W Labs® NDC 0713-0135-12 SUPPOSITORIES USP 25 mg Each suppository contains 25 mg Prochlorperazine () and the following inactive ingredients: glycerin, glyceryl monostearate, hydrogenated coconut oil fatty acids, hydrogenated palm kernel oil fatty acids. Remove foil wrapper and insert one suppository into rectum as directed by a physician. 1 to 2 suppositories daily. See accompanying insert for complete prescribing information.Store at 20-25°C (68-77°F) [See USP Controlled Room Temperature].Do not remove from foil until ready to use.
