Prochlorperazine


Generic Medicine Info
Indications and Dosage
Intramuscular
Nausea and vomiting
Adult: As prochlorperazine mesilate: 12.5 mg given via deep inj, may give further doses via oral admininistration, if necessary. As prochlorperazine edisylate: Initially. 5-10 mg, if necessary, may repeat dose 3-4 hourly. Max: 40 mg daily.
Elderly: Dose reduction may be necessary.

Intramuscular
Mania, Schizophrenia
Adult: As prochlorperazine mesilate: 12.5-25 mg bid or tid given via deep inj. As prochlorperazine edisylate: Initially, 10-20 mg via deep inj, may repeat dose 2-4 hourly, if necessary.
Elderly: Dose reduction may be necessary.

Intravenous
Nausea and vomiting
Adult: As prochlorperazine edisylate: 2.5-10 mg given via slow IV inj or infused at a rate not exceeding 5 mg per minute. Max: 10 mg per dose; 40 mg per day.
Elderly: Dose reduction may be necessary.

Oral
Vertigo
Adult: As prochlorperazine mesylate/maleate: In patient with Meniere’s syndrome, labyrinthitis: 5 mg tid, may increased up to 30 mg daily. Reduced dose gradually to 5-10 mg after several weeks.
Elderly: Dose reduction may be necessary.

Oral
Nausea and vomiting
Adult: As prochlorperazine mesylate/maleate: Prophylaxis: 5-10 mg bid or tid. Treatment: Initially, 20 mg, followed by 10 mg after 2 hours, if necessary.
Child: >1 year >10 kg: 0.25 mg/kg bid or tid.
Elderly: Dose reduction may be necessary.

Oral
Adjunct in severe anxiety disorder
Adult: As prochlorperazine mesylate/maleate: Initially, 15-20 mg daily in divided doses. May increase to Max 40 mg daily if necessary.
Elderly: Dose reduction may be necessary.

Oral
Mania, Schizophrenia
Adult: As prochlorperazine mesylate/maleate: Initially, 12.5 mg bid for 7 days, increased at 4-7 days interval until satisfactory response is achieved. Usual dose: 75-100 mg daily.
Elderly: Dose reduction may be necessary.

Rectal
Severe nausea and vomiting
Adult: 25 mg bid.
Elderly: Dose reduction may be necessary.
Administration
May be taken with or without food.
Contraindications
Reye’s syndrome, comatose patients. Children <2 years or weighing <9 kg.
Special Precautions
Patient with decreased gastrointestinal motility, paralytic ileus, urinary retention, BPH, xerostomia, visual problems, stroke, cerebrovascular disease, severe CV disease, dementia, Parkinson’s disease, hypothyroidism, cardiac failure, phaeochromocytoma, myasthenia gravis, prostate hyperthrophy, hypovolaemia, epilepsy or history risk of seizures. Children and elderly. Renal and hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Cholinergic effects (e.g. constipation, xerostomia, blurred vision, urinary retention), aspiration of vomit, extrapyramidal symptoms, somnolence, orthostatic hypotension, motor instability, hyperprolactinemia, pigmentary retinopathy, lenticular or corneal deposits, impaired body temperature regulation.
Endocrine disorders: Amenorrhoea.
Gastrointestinal disorders: Nausea, obstipation, intestinal obstruction, vomiting.
Hepatobiliary disorders: Jaundice.
Immune system disorders: Angioedema, urticaria.
Metabolism and nutrition disorders: Hyponatraemia, hyperglycaemia.
Nervous system disorders: Acute dystonia, dyskinesia, parkinsonism, tardive dyskinesia, agitation, convulsion.
Psychiatric disorder: Akathisia, insomnia.
Renal and urinary disorders: Urinary retention.
Reproductive system and breast disorder: Impotence, ejaculatory disorder.
Respiratory, thoracic and mediastinal disorders: Respiratory depression.
Skin and subcutaneous tissue disorders: Contact dermatitis, rash.
Potentially Fatal: Arrhythmias, torsade de pointes, blood dyscrasias (e.g. leucopenia, neutropenia, agranulocytosis), hypotension, neuroleptic malignant syndrome (e.g. hyperpyrexia, muscle rigidity, altered mental status).
Patient Counseling Information
This drug may cause drowsiness, if affected, do not drive or operate machinery. Avoid exposure to extreme heat.
Monitoring Parameters
Monitor for electrolytes, CBC, LFT, fasting plasma glucose level, lipid panel, visual changes. Discontinue treatment if neutrophil count is <1,000/mm3. Monitor for changes in mental status, vital signs, weight, BMI, waist circumference, tardive dyskinesia, changes in menstruation, libido, development of galactorrhoea, erectile and ejaculatory function, fever, muscle rigidity, autonomic instability.
Overdosage
Symptoms: Drowsiness, loss of consciousness, hypotension, tachycardia, EC changes, ventricular arrhythmias, hypothermia, severe extrapyramidal dyskinesias. Management: Symptomatic and supportive treatment. Empty stomach by gastric lavage immediately up to 6 hours after ingestion of toxic dose. May give dopamine to correct circulatory collapse; procyclidine or orphenadrine via IM/IV for severe dystonic reactions; diazepam IV for convulsions. Restore normal body temperature and correct circulatory or metabolic disturbances.
Drug Interactions
Enhanced CNS depression with barbiturates and sedatives. Reduced antipsychotic effect with anticholinergics. May reduce the effect of hypoglycaemic agents. Increased risk of arrhythmias with antidepressants. Increased risk of agranulocytosis with carbamazepine. Increased neurotoxicity with lithium. Diminished therapeutic effect of oral anticoagulant. Decreased absorption with antacids.
Food Interaction
Increased CNS depressant effect with alcohol.
Lab Interference
False-positive result to phenylketonuria and pregnancy test.
Action
Description: Prochlorperazine is a phenothiazine antipsychotic. It blocks the postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain including the chemoreceptor trigger zone. It exhibits a strong α-adrenergic and anticholinergic locking effect. It also depresses the releases of hypothalamic and hypophyseal hormones, reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone and emesis.
Synonym: Chlormeprazine
Onset: 30-40 minutes (oral); 10-20 minutes (IM); approx 60 minutes (rectal).
Duration: 3-4 hours (IM/oral); 3-12 hours (rectal).
Pharmacokinetics:
Absorption: Bioavailability: 12.5%. Time to peak plasma concentration: 1.5-5 hours.
Distribution: Volume of Distribution: 1,400-1,548 L.
Metabolism: Metabolised in the liver to N-desmethyl prochlorperazine active metabolite.
Excretion: Mainly via faeces. Elimination half-life: 6-10 hours.
Chemical Structure

Chemical Structure Image
Prochlorperazine

Source: National Center for Biotechnology Information. PubChem Database. Prochlorperazine, CID=4917, https://pubchem.ncbi.nlm.nih.gov/compound/Prochlorperazine (accessed on Jan. 23, 2020)

Storage
Store between 20-25°C. Protect from light.
ATC Classification
N05AB04 - prochlorperazine ; Belongs to the class of phenothiazine antipsychotics with piperazine structure.
References
Anon. Prochlorperazine (Antiemetic). AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 13/02/2019.

Anon. Prochlorperazine (Antipsychotic). AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 13/02/2019.

Anon. Prochlorperazine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/02/2019.

Buckingham R (ed). Prochlorperazine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/02/2019.

Prochlorperazine Edisylate Injection (Baxter Healthcare Corporation). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 07/02/2019.

Prochlorperazine Suppository (G&W Laboratories, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 01/02/2019.

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