prochlorperazine (Compazine, Compazine Spansules, prochlorperazine edisylate, prochlorperazine mesylate)
Dosing and uses of Compazine, Compazine Spansules (prochlorperazine)
Adult dosage forms and strengths
tablet
- 5mg
- 10mg
suppository
- 25mg
injectable solution
- 5mg/mL
Severe Nausea & Vomiting
PO: Immediate-release, 5-10 mg q6-8hr; extended-release, 10 mg q12hr or 15 mg every morning
Suppository: 25 mg q12hr
IM: 5-10 mg q3-4hr; not to exceed 40 mg/day
IV: 2.5-10 mg q3-4hr; not to exceed 10 mg/dose or 40 mg/day
Severe Intraoperative Nausea & Vomiting
Prophylaxis
IM: 5-10 mg administered 1-2 hours before induction of anesthesia; may be repeated once 30 minutes after initial dose
IV: 5-10 mg administered 15-30 minutes before induction of anesthesia, repeated once before procedure if desired, or 20 mg/L administered 15-30 minutes before induction; not to exceed 30 mg/day
Psychosis
5-10 mg PO q6-8hr; slowly titrate dose q2-3days; not to exceed 150 mg/day
10-20 mg IM q2-4hr to gain control; 3-4 doses rarely needed
Pediatric dosage forms and strengths
tablet
- 5mg
- 10mg
suppository
- 2.5mg
- 5mg
- 25mg
injectable solution
- 5mg/mL
Psychotic Disorder
<2 years: Not recommended
2-6 years: 2.5 mg PO/PR q8-12hr initially; not to exceed 20 mg/day; not to exceed 10 mg on the first day
6-12 years: 2.5 mg PO/PR q8-12hr initially; not to exceed 25 mg/day; not to exceed 10 mg on the first day
Severe Nausea & Vomiting
<2 years: Not recommended
≥2 years (9-13 kg): 2.5 mg PO daily or q12hr; not to exceed 7.5 mg/day
≥2 years (13.1-18 kg): 2.5 mg PO q8-12hr; not to exceed 10 mg/day
≥2 years (18.1-37 kg): 2.5 mg PO q8hr or 5 mg PO q12hr; not to exceed 15 mg/day
Geriatric dosage forms and strengths
Not drug of choice in elderly, because of extrapyramidal symptoms
Nonpsychotic Dementia Behavior (Off-label)
Lower initial dose and adjust gradually; 2.5-5 mg/day PO; dosing interval may be increased to q8-12hr PRN; not to exceed 75 mg/day
Compazine, Compazine Spansules (prochlorperazine) adverse (side) effects
<1%
Insomnia
Restlessness (immediate restlessness or agitation may be treated with diphenhydramine 25 mg IV push)
Dizziness
Anxiety
Euphoria
Agitation
Depression
Weakness
Headache
Cerebral edema
Poikilothermia
Orthostatic hypotension (after IM injection)
Tachycardia
ECG changes
Anorexia
Dyspepsia
Constipation
Diarrhea
Ileus
Blood dyscrasia
Galactorrhea
Gynecomastia
Ejaculatory disorder
Lens opacities (with prolonged use)
Photosensitivity
Pruritus
Frequency not defined
Akathisia
Sedation
Anticholinergic effects
Weight gain
Oligomenorrhea or amenorrhea
Erectile dysfunction
Extrapyramidal symptoms (muscle stiffness, dystonia, parkinsonism, tardive dyskinesia)
Neuroleptic malignant syndrome (infrequent but serious)
Seizure
Decreased gag reflex
Confusion
Hypotension
Hypertension
Leukopenia
Agranulocytosis
Cholestatic jaundice
Photosensitivity reaction
Priapism
Hepatotoxicity
Warnings
Black box warnings
Patients with dementia-related psychosis who are treated with antipsychotic drugs are at an increased risk of death, as shown in short-term controlled trials; the deaths appeared to be either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature
This drug is not approved for treatment of patients with dementia-related psychosis
Contraindications
Documented hypersensitivity to phenothiazines
Coma, severe CNS depression, concurrent use of large amounts of CNS depressants, poorly controlled seizure disorder, subcortical brain damage
Postoperative management of nausea/vomiting following pediatric surgery
Children <2 years or weighing <9 kg
Cautions
Avoid using in children with suspected Reye syndrome
Use caution in evere hypertension, severe cardiovascular disease
Use with caution in glaucoma, prostatic hypertrophy, stenosing peptic ulcer disease, history of neuroleptic malignant syndrome, Parkinson disease, hypocalcemia, renal/hepatic impairment, history of severe reactions to insulin or electroconvulsive therapy, history of seizures, asthma, respiratory tract infections, cardiovascular disease, myelosuppression
Blood dyscrasias including neutropenia, agranulocytosis, and leukopenia reported with use; discontinue therapy at first sign of blood dyscrasias
Risk of extrapyramidal symptoms, neuroleptic malignant syndrome, hypotension (may be particularly severe in patients with pheochromocytoma or mitral insufficiency)
Esophageal dysmotility/aspiration may occur; use with caution in patients at risk of pneumonia
Depresses hypothalamic thermoregulatory mechanism; exposure to extreme temperatures may cause hypo- or hyperthermia
May alter cardiac conduction; life-threatening arrhythmias reported with therapeutic doses
May cause anticholinergic effects (constipation, xerostomia, urinary retention, blurred vision); use caution in patients with decreased gastrointestinal motility, paralytic ileus, urinary retention, BPH, xerostomia, visual problems
May cause pigmentary retinopathy and lenticular and corneal deposits, espcially in prolonged therapy
May cause sedation and impair ability to perform tasks which require mental alertness, including operating heavy machinery
Use associated with increased prolactin levels
In case of severe hypotension, use norepinephrine or phenylepinephrine; do not use epinephrine or dopamine
Do not crush extended-release product
Avoid SC administration (may cause irritation)
Antiemetic effect may obscure toxicity of chemotherapeutic drugs
Use may be associated with neuroleptic malignant syndrome; monitor muscle ritidity, mental status changes, fever, autonomic instability
May need anticholinergic antiparkinsonian agent to counter extrapyramidal symptoms
May impair core body temperature regulation
FDA warning regarding off-label use for dementia in elderly
Pregnancy and lactation
Pregnancy category: C
Lactation: Phenothiazines may be excreted in breast milk; do not nurse
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Compazine, Compazine Spansules (prochlorperazine)
Mechanism of action
Antiemetic: Antidopaminergic effect, blocking dopamine receptors in the brain, blocking vagus nerve in GI tract
Antipsychotic: Blocking mesolimbic dopamine receptors, and blocking alpha-adrenergic receptors (D1 and D2) in brain
Absorption
Bioavailability: 12.5%
Onset: 10-20 min (IM); 30-40 min (PO); 60 min (PR)
Duration: 3-4 hr (PO); 3-12hr (PR); extended-release, 10-12 hr
Distribution
Vd: 1400-1548 L
Metabolism
Metabolized by liver
Metabolites: N-desmethyl prochlorperazine (active)
Elimination
Half-life: 6.8-9 hr (PO); 6-10 hr (IV)
Dialyzable: No
Excretion: Feces (primarily)
Administration
IV Compatibilities
Solution: Compatible with most common solvents
Additive: Amikacin, ascorbic acid injection, dexamethasone, dimenhydrinate, erythromycin, ethacrynate, lidocaine, nafcillin, penicillin G potassium (incompatible at higher concentrations), sodium bicarbonate, vitamins B and C
Syringe (partial list): Atropine, chlorpromazine, cimetidine, diphenhydramine, fentanyl, glycopyrrolate, hydroxyzine, meperidine, metoclopramide, morphine sulfate (incompatible if phenol present)(?)
Y-site (partial list): Calcium gluconate, cisplatin, cladribine, clarithromycin, cyclophosphamide, cytarabine, docetaxel, doxorubicin, doxorubicin liposomal, heparin, linezolid, melphalan, methotrexate, potassium chloride, propofol, teniposide, thiotepa, topotecan, vitamins B and C
IV Incompatibilities
Additive: Aminophylline, amphotericin B, ampicillin, calcium gluconate(?), chloramphenicol, chlorothiazide, floxacillin, furosemide, hydrocortisone, methohexital, penicillin G sodium, phenobarbital, thiopentaL
Syringe: Dimenhydrinate, hydromorphone(?), ketorolac, midazolam, morphine tartate, pentobarbital, thiopentaL
Y-site: Aldesleukin, allopurinol, amifostine, amphotericin B, aztreonam, bivalirudin, cefepime, etoposide phosphate, fenoldopam, filgrastim, fludarabine, foscarnet, gemcitabine, piperacillin/tazobactam
IV Administration
Avoid bolus
IV push rate should not exceed 5 mg/min
For infusion, dilute 20 mg in 1 L of compatible solution; may infuse over 30 minutes
Storage
Store at room temperature, and protect from light
Solution is clear or slightly yellow