CHLORPROMAZINE HYDROCHLORIDE INTENSOL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CHLORPROMAZINE HYDROCHLORIDE INTENSOL (CHLORPROMAZINE HYDROCHLORIDE INTENSOL).
Chlorpromazine is a phenothiazine antipsychotic that blocks postsynaptic dopamine D2 receptors in the central nervous system, particularly in the mesolimbic and mesocortical pathways. It also exhibits antagonism at serotonin 5-HT2, histamine H1, alpha-1 adrenergic, and muscarinic receptors, contributing to its sedative, antiemetic, and hypotensive effects.
| Metabolism | Primarily hepatic via CYP2D6, with minor contributions from CYP1A2 and CYP3A4. Major metabolites include 7-hydroxychlorpromazine, Nor1-chlorpromazine, and chlorpromazine sulfoxide, which are less active. |
| Excretion | Renal (70-80% as metabolites, <1% unchanged); biliary/fecal (~20-30%) |
| Half-life | 15-30 hours; prolonged in elderly and hepatic impairment; active metabolites (e.g., 7-hydroxychlorpromazine) have longer half-lives (up to 12-24 hours) |
| Protein binding | 90-99%; bound to albumin and lipoproteins |
| Volume of Distribution | 10-30 L/kg; large Vd indicates extensive tissue distribution and accumulation |
| Bioavailability | Oral: 20-40% (first-pass metabolism); IM: 50-70% |
| Onset of Action | Oral: 30-60 min; IM: 15-30 min; IV: 5-10 min |
| Duration of Action | Antipsychotic: 4-6 hours; sedative: 6-8 hours; antiemetic: 4-6 hours |
Oral: 25-50 mg 2-3 times daily, up to 1000 mg/day in severe psychosis. IM: 25-50 mg every 1-4 hours until controlled, then switch to oral.
| Dosage form | CONCENTRATE |
| Renal impairment | No adjustment required for mild-moderate renal impairment. Severe impairment (GFR <10 mL/min): use with caution, reduce dose by 50%. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: contraindicated or use with extreme caution at reduced dose (e.g., 50% reduction). |
| Pediatric use | <6 months: not recommended. 6 months-5 years: 0.5-1 mg/kg/dose po/IM every 4-6 hours (max 40 mg/day). 6-12 years: 10-25 mg po/IM every 4-6 hours (max 200 mg/day). >12 years: adult dosing. |
| Geriatric use | Initiate at 10-25 mg daily orally, increase gradually by 10-25 mg per week. Use lowest effective dose; increased risk of hypotension, sedation, and anticholinergic effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CHLORPROMAZINE HYDROCHLORIDE INTENSOL (CHLORPROMAZINE HYDROCHLORIDE INTENSOL).
| Breastfeeding | Chlorpromazine is excreted into breast milk; M/P ratio approximately 0.5-0.7. Potential adverse effects include drowsiness, lethargy, and possibly impaired temperature regulation in the infant. Avoid breastfeeding if possible; if used, monitor infant for sedation and poor feeding. |
| Teratogenic Risk | First trimester: Risk of congenital malformations not clearly established; may be associated with neural tube defects. Second and third trimesters: Risk of extrapyramidal symptoms and withdrawal in neonates. Cases of jaundice and hyperreflexia have been reported. Use only if clearly needed. |
■ FDA Black Box Warning
Increased mortality in elderly patients with dementia-related psychosis. Antipsychotic drugs are not approved for the treatment of dementia-related psychosis.
| Serious Effects |
["Hypersensitivity to chlorpromazine or any phenothiazine","Comatose states, especially with CNS depressants","Bone marrow depression/agranulocytosis","Concurrent use of large doses of other CNS depressants","Pheochromocytoma","Severe hypotension or cardiovascular disease","Parkinson's disease (may worsen symptoms)","Pregnancy: avoid unless clearly needed (teratogenic potential)"]
| Precautions | ["Tardive dyskinesia","Neuroleptic malignant syndrome","Cardiovascular effects: QT prolongation, orthostatic hypotension, tachycardia","Seizure threshold lowering","Leukopenia/neutropenia/agranulocytosis","Hyperglycemia and diabetes mellitus","Hyperprolactinemia","Prolonged QT interval","Increased risk of falls due to sedation and orthostasis","Hepatic effects: cholestatic jaundice, elevated transaminases","Photosensitivity and ocular changes","Avoid abrupt withdrawal"] |
| Food/Dietary |
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| Fetal Monitoring | Monitor maternal blood pressure, liver function, and for signs of extrapyramidal symptoms. Fetal monitoring: assess growth and well-being via ultrasound, especially in third trimester. Neonatal monitoring: observe for extrapyramidal signs, jaundice, and respiratory depression after delivery. |
| Fertility Effects | May cause hyperprolactinemia leading to menstrual irregularities, galactorrhea, and reduced libido. Reversible upon discontinuation. No direct evidence of permanent fertility impairment. |
| Avoid concurrent use with alcohol. May reduce absorption with high-fiber foods and antacids; separate administration by at least 1 hour. Grapefruit juice may increase chlorpromazine levels; avoid excessive consumption. |
| Clinical Pearls | Chlorpromazine intensol is a concentrated oral solution; must be diluted in water, juice, or semisolid food to avoid GI irritation. Use with caution in elderly due to anticholinergic and hypotensive effects. Monitor for extrapyramidal symptoms, especially akathisia and tardive dyskinesia. Avoid concurrent use with other CNS depressants. Can cause photosensitivity; warn patients to use sun protection. May lower seizure threshold; use cautiously in epilepsy. QT prolongation risk; obtain baseline ECG and monitor electrolytes. |
| Patient Advice | Dilute the prescribed dose in at least 60 mL of water, fruit juice, or semisolid food immediately before taking. · Do not drink alcohol while taking this medication, as it increases drowsiness and dizziness. · Avoid prolonged sun exposure and use sunscreen, as this drug increases sensitivity to sunlight. · Rise slowly from sitting or lying positions to prevent dizziness and fainting. · Report any uncontrolled muscle movements, especially of the face, tongue, or jaw, to your healthcare provider. · Do not stop taking abruptly; consult your doctor before discontinuing. · May cause dry mouth; sugarless candy or ice chips can help relieve this symptom. |