HALOPERIDOL INTENSOL
Clinical safety rating: safe
CNS depressants may enhance sedative effects Can cause extrapyramidal symptoms and QT prolongation.
Haloperidol is a typical antipsychotic that primarily antagonizes dopamine D2 receptors in the central nervous system, particularly in the mesolimbic and mesocortical pathways. It also has moderate affinity for alpha-1 adrenergic receptors and low affinity for H1 histamine and muscarinic cholinergic receptors.
| Metabolism | Primarily hepatic via CYP3A4 and CYP2D6; also undergoes glucuronidation. Active metabolite reduced haloperidol is formed. |
| Excretion | Primarily hepatic metabolism with renal elimination of metabolites; about 40% excreted in urine and 15% in feces via bile. |
| Half-life | Terminal elimination half-life is approximately 14-37 hours (average 21 hours) after oral administration; may be longer in elderly or hepatic impairment. |
| Protein binding | Approximately 92% bound to plasma proteins (albumin and alpha-1-acid glycoprotein). |
| Volume of Distribution | Mean Vd is 8-18 L/kg (range 7-27 L/kg), indicating extensive tissue distribution. |
| Bioavailability | Oral: 60-65% due to first-pass metabolism; Intramuscular: 70-80%; Intravenous: 100%. |
| Onset of Action | Oral: 1-2 hours; Intramuscular: 30-45 minutes; Intravenous: 5-10 minutes. |
| Duration of Action | Oral: 12-24 hours; Intramuscular: 12-24 hours; Intravenous: 6-12 hours (duration may be shorter for acute effects). |
Oral (Intensol): 0.5-5 mg twice or three times daily. Maximum: 100 mg/day.
| Dosage form | CONCENTRATE |
| Renal impairment | No dosage adjustment required for renal impairment. Hemodialysis does not remove significant amounts. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose by 50%. Child-Pugh C: Avoid use or use with caution at 25% of normal dose. |
| Pediatric use | Children 3-12 years (weight >15 kg): 0.05-0.15 mg/kg/day orally in 2-3 divided doses. Maximum: 0.15 mg/kg/day for nonpsychotic disorders, up to 0.2 mg/kg/day for psychosis. |
| Geriatric use | Initial dose: 0.5-1 mg orally once or twice daily, with gradual titration. Maximum dose: 5 mg/day. Use lowest effective dose due to increased sensitivity to extrapyramidal effects and anticholinergic adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
CNS depressants may enhance sedative effects Can cause extrapyramidal symptoms and QT prolongation.
| FDA category | Animal |
| Breastfeeding | Haloperidol is excreted into breast milk. M/P ratio not established. Infant exposure estimated to be 2-12% of maternal weight-adjusted dose. Monitor infant for sedation, extrapyramidal symptoms, and developmental milestones. Consider avoiding breastfeeding if high maternal doses required. |
| Teratogenic Risk | First trimester: Limited data; potential risk of congenital malformations, particularly limb defects (case reports). Second trimester: Risk of extrapyramidal symptoms and withdrawal in neonate if used near term. Third trimester: Neonatal withdrawal syndrome, extrapyramidal signs, agitation, hypertonia, hypotonia, tremor, somnolence, respiratory distress, feeding disorder. Use only if benefit outweighs risk. |
■ FDA Black Box Warning
Increased mortality in elderly patients with dementia-related psychosis. Haloperidol is not approved for the treatment of dementia-related psychosis.
| Common Effects | Tourette's syndrome |
| Serious Effects |
["Comatose states","CNS depression (severe alcohol, barbiturate, or narcotic intoxication)","Parkinson's disease (relative)","Known hypersensitivity to haloperidol","QTc interval prolongation (congenital or acquired) (relative)","Concurrent use with drugs that prolong QT interval"]
| Precautions | ["Risk of QT prolongation and torsades de pointes","Neuroleptic malignant syndrome (NMS)","Tardive dyskinesia","Extrapyramidal symptoms (EPS)","Seizure threshold lowering","Use in elderly with dementia-related psychosis (see black box warning)","Hematologic effects (leukopenia, neutropenia)","Hyperprolactinemia"] |
| Food/Dietary |
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| Fetal Monitoring | Monitor maternal blood pressure, ECG (QTc prolongation risk), extrapyramidal symptoms, and serum prolactin. Fetal monitoring: serial growth ultrasound, nonstress test, biophysical profile in third trimester. Neonatal observation for withdrawal and extrapyramidal signs for 24 hours after birth. |
| Fertility Effects | Haloperidol elevates prolactin levels via dopamine D2 blockade, potentially disrupting menstrual cyclicity and ovulation, leading to reversible infertility. May also decrease libido and cause erectile or ejaculatory dysfunction. Effects are dose-dependent and resolve upon discontinuation. |
| Avoid grapefruit juice, as it may inhibit CYP3A4 metabolism and increase haloperidol levels. No specific food restrictions; however, taking with food may reduce gastrointestinal irritation. Do not mix with caffeinated beverages or alcohol due to increased CNS depression. |
| Clinical Pearls | Haloperidol Intensol is a concentrated oral solution (2 mg/mL) that must be diluted in water or juice before administration to ensure accurate dosing. Monitor for QTc prolongation, especially in elderly patients, those with electrolyte imbalances, or those on other QT-prolonging drugs. Tardive dyskinesia risk increases with cumulative dose and duration; use lowest effective dose. For acute agitation, IM haloperidol may be preferred due to faster onset. Avoid concurrent use with other antipsychotics unless cross-titrating. |
| Patient Advice | Dilute the prescribed amount of Haloperidol Intensol in at least 60 mL of water, juice (except grapefruit juice), or milk before taking. Do not take it undiluted. · Avoid grapefruit juice while taking this medication as it may increase side effects. · Do not stop taking this medication suddenly without consulting your doctor. Your doctor may need to gradually reduce the dose. · This medication may cause dizziness or drowsiness. Avoid driving or operating heavy machinery until you know how it affects you. · Report any involuntary muscle movements (e.g., tongue, face, jaw) to your doctor immediately. · Avoid alcohol while taking haloperidol as it may worsen side effects. · If you miss a dose, take it as soon as you remember unless it is near the time of your next dose. Do not double the dose. |