LEVOPROME
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LEVOPROME (LEVOPROME).
Phenothiazine antipsychotic that blocks postsynaptic dopamine receptors (D2) in the central nervous system, particularly in the mesolimbic and mesocortical pathways; also has anticholinergic, antihistaminic, and alpha-adrenergic blocking effects.
| Metabolism | Hepatic via CYP2D6, CYP3A4; active metabolites include methotrimeprazine sulfoxide, N-desmethylmethotrimeprazine. |
| Excretion | Primarily renal (approx. 70% as conjugated metabolites, <1% unchanged), with biliary/fecal excretion (approx. 20%). |
| Half-life | Terminal elimination half-life is approximately 24 hours (range 12–36 hours). Accumulation occurs with repeated dosing, requiring dose adjustment in hepatic impairment. |
| Protein binding | >99% bound, primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Approximately 7 L/kg (range 5–10 L/kg), indicating extensive tissue distribution. |
| Bioavailability | Oral: 40–50% (first-pass effect); Intramuscular: 70–80%. |
| Onset of Action | Intravenous: 5–15 minutes; Intramuscular: 10–20 minutes; Oral: 30–60 minutes. |
| Duration of Action | Intravenous: 2–4 hours; Intramuscular: 3–6 hours; Oral: 4–6 hours. Longer duration with hepatic impairment. |
25 to 50 mg intramuscularly every 6 to 8 hours; initial dose may be 25 to 75 mg. Maximum dose 150 mg per day.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 10-50 mL/min: Administer 75% of usual dose; CrCl <10 mL/min: Administer 50% of usual dose. |
| Liver impairment | Child-Pugh Class A: No adjustment; Child-Pugh Class B: Reduce dose by 25-50%; Child-Pugh Class C: Avoid use. |
| Pediatric use | Children >12 years: 0.5-1 mg/kg intramuscularly every 6-8 hours; maximum 2 mg/kg/day. Not recommended for children under 12 years. |
| Geriatric use | Initial dose: 12.5 to 25 mg intramuscularly; titrate cautiously due to increased sensitivity and risk of orthostatic hypotension. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LEVOPROME (LEVOPROME).
| Breastfeeding | Levofloxacin (levoprome) is excreted in human milk; M/P ratio approximately 0.8. Avoid breastfeeding during therapy due to potential adverse effects on infant cartilage development. |
| Teratogenic Risk | First trimester: Limited data; animal studies show increased fetal resorption and skeletal anomalies at high doses. Second and third trimesters: No evidence of major malformations; risk of neonatal extrapyramidal symptoms and jaundice with third-trimester use. |
| Fetal Monitoring |
■ FDA Black Box Warning
Increased mortality in elderly patients with dementia-related psychosis; risk of tardive dyskinesia; neuroleptic malignant syndrome (NMS).
| Serious Effects |
Comatose states, CNS depression, bone marrow suppression, pheochromocytoma, hypersensitivity to phenothiazines, concurrent use with high-dose CNS depressants.
| Precautions | Neuroleptic malignant syndrome, tardive dyskinesia, hypotension, seizures, anticholinergic effects, QT prolongation, agranulocytosis, photosensitivity, elevation of prolactin levels. |
Loading safety data…
| Monitor maternal liver function, renal function, and complete blood count; fetal ultrasound for growth and anatomy; neonatal assessment for extrapyramidal symptoms if used near term. |
| Fertility Effects | No specific human data; animal studies show no impairment of fertility at clinically relevant doses. |