Pronunciation:

(proe klor PER a zeen)

U.S. Brand Names:

Synonyms:

Generic Available:

Canadian Brand Names:

Use:

Use - Unlabeled/Investigational:

Pregnancy Risk Factor:

Pregnancy Implications:

Lactation:

Contraindications:

Warnings/Precautions:

Phenothiazines may cause anticholinergic effects (constipation, xerostomia, blurred vision, urinary retention); therefore, they should be used with caution in patients with decreased gastrointestinal motility, urinary retention, BPH, xerostomia, or visual problems. Conditions which also may be exacerbated by cholinergic blockade include narrow-angle glaucoma (screening is recommended) and worsening of myasthenia gravis. May cause extrapyramidal symptoms, including pseudoparkinsonism, acute dystonic reactions, akathisia and tardive dyskinesia. May be associated with neuroleptic malignant syndrome (NMS).

Adverse Reactions:

Cardiovascular: Hyper-/hypotension, orthostatic hypotension, tachycardia, bradycardia, dizziness, cardiac arrest

Central nervous system: Extrapyramidal symptoms (pseudoparkinsonism, akathisia, dystonias, tardive dyskinesia), dizziness, cerebral edema, seizure, headache, drowsiness, paradoxical excitement, restlessness, hyperactivity, insomnia, neuroleptic malignant syndrome (NMS), impairment of temperature regulation

Dermatologic: Rash, discoloration of skin (blue-gray), photosensitivity

Endocrine & metabolic: Hypoglycemia, hyperglycemia, galactorrhea, lactation, breast enlargement, gynecomastia, menstrual irregularity, amenorrhea, SIADH, libido (changes in)

Gastrointestinal: Constipation, weight gain, vomiting, stomach pain, nausea, xerostomia, salivation, diarrhea, anorexia, ileus

Genitourinary: Difficulty in urination, ejaculatory disturbances, incontinence, polyuria, ejaculating dysfunction, priapism

Hematologic: Agranulocytosis, leukopenia, eosinophilia, hemolytic anemia, thrombocytopenic purpura, pancytopenia

Hepatic: Cholestatic jaundice, hepatotoxicity

Neuromuscular & skeletal: Tremor

Ocular: Pigmentary retinopathy, blurred vision, cornea and lens changes

Respiratory: Nasal congestion

Miscellaneous: Diaphoresis

Overdosage/Toxicology:

Drug Interactions:

Aluminum salts: May decrease the absorption of phenothiazines; monitor

Amphetamines: Efficacy may be diminished by antipsychotics; in addition, amphetamines may increase psychotic symptoms; avoid concurrent use

Anticholinergics: May inhibit the therapeutic response to phenothiazines and excess anticholinergic effects may occur; includes benztropine, trihexyphenidyl, biperiden, and drugs with significant anticholinergic activity (TCAs, antihistamines, disopyramide)

Antihypertensives: Concurrent use of phenothiazines with an antihypertensive may produce additive hypotensive effects (particularly orthostasis)

Bromocriptine: Phenothiazines inhibit the ability of bromocriptine to lower serum prolactin concentrations

CNS depressants: Sedative effects may be additive with phenothiazines; monitor for increased effect; includes barbiturates, benzodiazepines, narcotic analgesics, ethanol and other sedative agents

Epinephrine: Chlorpromazine (and possibly other low potency antipsychotics) may diminish the pressor effects of epinephrine

Guanethidine and guanadrel: Antihypertensive effects may be inhibited by phenothiazines

Levodopa: Phenothiazines may inhibit the antiparkinsonian effect of levodopa; avoid this combination

Lithium: Phenothiazines may produce neurotoxicity with lithium; this is a rare effect

Metoclopramide: May increase extrapyramidal symptoms (EPS) or risk.

Phenytoin: May reduce serum levels of phenothiazines; phenothiazines may increase phenytoin serum levels

Propranolol: Serum concentrations of phenothiazines may be increased; propranolol also increases phenothiazine concentrations

Polypeptide antibiotics: Rare cases of respiratory paralysis have been reported with concurrent use of phenothiazines

QTc-prolonging agents: Effects on QTc interval may be additive with phenothiazines, increasing the risk of malignant arrhythmias; includes type Ia antiarrhythmics, TCAs, and some quinolone antibiotics (sparfloxacin, moxifloxacin, and gatifloxacin)

Sulfadoxine-pyrimethamine: May increase phenothiazine concentrations

Tricyclic antidepressants: Concurrent use may produce increased toxicity or altered therapeutic response

Trazodone: Phenothiazines and trazodone may produce additive hypotensive effects

Valproic acid: Serum levels may be increased by phenothiazines

Ethanol/Nutrition/Herb Interactions:

Ethanol: Avoid ethanol (may increase CNS depression).

Food: Limit caffeine.

Herb/Nutraceutical: Avoid dong quai, St John's wort (may also cause photosensitization). Avoid kava kava, gotu kola, valerian, St John's wort (may increase CNS depression).

Stability:

Injection: Intact vials/ampuls for injection are stable at room temperature; protect from light; clear or slightly yellow solutions may be used.

I.V. infusion: Injection may be diluted in 50-100 mL NS or D5W.

Suppository: May require refrigeration

Tablet: Stable at room temperature.

Compatibility:

Y-site administration: Compatible: Amsacrine, calcium gluconate, cisatracurium, cisplatin, cladribine, clarithromycin, cyclophosphamide, cytarabine, docetaxel, doxorubicin, doxorubicin liposome, fluconazole, gatifloxacin, granisetron, heparin, hydrocortisone sodium succinate, linezolid, melphalan, methotrexate, ondansetron, paclitaxel, potassium chloride, propofol, remifentanil, sargramostim, sufentanil, teniposide, thiotepa, topotecan, vinorelbine, vitamin B complex with C. Incompatible: Aldesleukin, allopurinol, amifostine, amphotericin B cholesteryl sulfate complex, aztreonam, cefepime, etoposide phosphate, fludarabine, foscarnet, filgrastim, gemcitabine, piperacillin/tazobactam

Compatibility in syringe: Compatible: Atropine, butorphanol, chlorpromazine, cimetidine, diamorphine, diphenhydramine, droperidol, fentanyl, glycopyrrolate, hydroxyzine, meperidine, metoclopramide, nalbuphine, pentazocine, perphenazine, promazine, promethazine, ranitidine, scopolamine, sufentanil. Incompatible: Dimenhydrinate, ketorolac, midazolam, morphine tartrate, pentobarbital, thiopental. Variable (consult detailed reference): Hydromorphone, morphine sulfate

Compatibility when admixed: Compatible: Amikacin, ascorbic acid injection, cephalothin, dexamethasone sodium phosphate, dimenhydrinate, erythromycin lactobionate, ethacrynate, lidocaine, nafcillin, sodium bicarbonate, vitamin B complex with C. Incompatible: Aminophylline, amphotericin B, ampicillin, chloramphenicol, chlorothiazide, floxacillin, furosemide, heparin, hydrocortisone sodium succinate, methohexital, penicillin G sodium, phenobarbital, phenytoin, thiopental. Variable (consult detailed reference): Calcium gluconate, penicillin G potassium

Mechanism of Action:

Pharmacodynamics/Kinetics:

Onset of action: Oral: 30-40 minutes; I.M.: 10-20 minutes; Rectal: ~60 minutes

Duration: I.M., oral extended-release: 12 hours; Rectal, immediate release: 3-4 hours

Distribution: Vd: 1400-1548 L; crosses placenta; enters breast milk

Metabolism: Primarily hepatic; N-desmethyl prochlorperazine (major active metabolite)

Bioavailability: Oral: 12.5%

Half-life elimination: Oral: 3-5 hours; I.V.: ~7 hours

Dosage:

Antiemetic: Children (not recommended in children <10 kg or <2 years):

Oral, rectal: >10 kg: 0.4 mg/kg/24 hours in 3-4 divided doses; or

9-14 kg: 2.5 mg every 12-24 hours as needed; maximum: 7.5 mg/day

14-18 kg: 2.5 mg every 8-12 hours as needed; maximum: 10 mg/day

18-39 kg: 2.5 mg every 8 hours or 5 mg every 12 hours as needed; maximum: 15 mg/day

I.M.: 0.1-0.15 mg/kg/dose; usual: 0.13 mg/kg/dose; change to oral as soon as possible

Antiemetic: Adults:

Oral: 5-10 mg 3-4 times/day; usual maximum: 40 mg/day

I.M.: 5-10 mg every 3-4 hours; usual maximum: 40 mg/day

I.V.: 2.5-10 mg; maximum 10 mg/dose or 40 mg/day; may repeat dose every 3-4 hours as needed

Rectal: 25 mg twice daily

Surgical nausea/vomiting: Adults:

I.M.: 5-10 mg 1-2 hours before induction; may repeat once if necessary

I.V.: 5-10 mg 15-30 minutes before induction; may repeat once if necessary

Antipsychotic:

Children 2-12 years (not recommended in children <10 kg or <2 years):

Oral, rectal: 2.5 mg 2-3 times/day; increase dosage as needed to maximum daily dose of 20 mg for 2-5 years and 25 mg for 6-12 years

I.M.: 0.13 mg/kg/dose; change to oral as soon as possible

Adults:

Oral: 5-10 mg 3-4 times/day; doses up to 150 mg/day may be required in some patients for treatment of severe disturbances

I.M.: 10-20 mg every 4-6 hours may be required in some patients for treatment of severe disturbances; change to oral as soon as possible

Nonpsychotic anxiety: Oral: Adults: Usual dose: 15-20 mg/day in divided doses; do not give doses >20 mg/day or for longer than 12 weeks

Elderly: Behavioral symptoms associated with dementia (unlabeled use): Initial: 2.5-5 mg 1-2 times/day; increase dose at 4- to 7-day intervals by 2.5-5 mg/day; increase dosing intervals (twice daily, 3 times/day, etc) as necessary to control response or side effects; maximum daily dose should probably not exceed 75 mg in elderly; gradual increases (titration) may prevent some side effects or decrease their severity

Hemodialysis: Not dialyzable (0% to 5%)

Administration:

Monitoring Parameters:

Test Interactions:

Dietary Considerations:

Patient Education:

Additional Information:

Anesthesia and Critical Care Concerns/Other Considerations:

Dental Health: Effects on Dental Treatment:

Tardive dyskinesia: Prevalence rate may be 40% in elderly; development of the syndrome and the irreversible nature are proportional to duration and total cumulative dose over time. Extrapyramidal reactions are more common in elderly with up to 50% developing these reactions after 60 years of age. Drug-induced Parkinson's syndrome occurs often; akathisia is the most common extrapyramidal reaction in elderly.

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

Oncology: Emetic Potential:

Oncology: Vesicant:

Dosage Forms:

Injection, solution, as edisylate: 5 mg/mL (2 mL, 10 mL) [contains benzyl alcohol]

Suppository, rectal: 2.5 mg (12s), 5 mg (12s), 25 mg (12s) [may contain coconut and palm oil]

Compazine®: 2.5 mg (12s), 5 mg (12s), 25 mg (12s) [contains coconut and palm oils] [DSC]

Compro™: 25 mg (12s) [contains coconut and palm oils]

Tablet, as maleate: 5 mg, 10 mg

International Brand Names: