DOPRAM
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DOPRAM (DOPRAM).
Doxapram (DOPRAM) is a respiratory stimulant that acts primarily by stimulating peripheral chemoreceptors in the carotid body, leading to increased respiratory drive. It also has central effects at higher doses by activating the medullary respiratory center.
| Metabolism | Hepatic metabolism primarily via CYP3A4 and CYP2E1 to active metabolites (keto-doxapram). |
| Excretion | Renal (unchanged drug and metabolites; approximately 20-30% as unchanged doxapram). |
| Half-life | 2-4 hours in adults; prolonged in hepatic impairment or neonates. |
| Protein binding | Approximately 50% (primarily to albumin). |
| Volume of Distribution | 1.5 L/kg (highly distributed into tissues). |
| Bioavailability | Oral: approximately 60% (significant first-pass metabolism). |
| Onset of Action | IV: 20-40 seconds; oral: 30-60 minutes. |
| Duration of Action | IV: 5-12 minutes (respiratory stimulation); oral: 2-4 hours. |
1-3 mg/kg intravenous bolus over 30-60 seconds, may repeat in 15 minutes up to a total of 3 mg/kg; for respiratory stimulation, continuous IV infusion at 1-5 mg/kg/hour.
| Dosage form | INJECTABLE |
| Renal impairment | No specific GFR-based dose adjustment; use with caution in severe renal impairment due to risk of accumulation of metabolite. |
| Liver impairment | No specific Child-Pugh based adjustment; use with caution in severe hepatic impairment as metabolism may be reduced. |
| Pediatric use | Neonates: 1.5-2.5 mg/kg IV, may repeat in 15 minutes; Children: 1-3 mg/kg IV, may repeat in 15 minutes up to 3 mg/kg total; continuous IV infusion: 1-5 mg/kg/hour. |
| Geriatric use | No specific dose adjustment; monitor closely for adverse effects, especially hypertension and arrhythmias due to potential increased sensitivity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DOPRAM (DOPRAM).
| Breastfeeding | Compatibility: probably compatible. Excretion into breast milk is unknown; however, due to low oral bioavailability, infant exposure is likely minimal. M/P ratio: not available. Use caution in preterm infants or those with apnea. |
| Teratogenic Risk | Pregnancy Category B. No evidence of teratogenicity in animal studies, but no adequate human studies. Use only if clearly needed. First trimester: potential risk cannot be excluded. Second/third trimester: possible risk of neonatal respiratory depression if used near term. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to doxapram","Seizure disorders","Severe hypertension","Cerebrovascular accident","Coronary artery disease or arrhythmias","Head injury or respiratory failure due to neuromuscular disease"]
| Precautions | ["Hypertension and tachycardia due to sympathomimetic effects","May cause seizures, especially in patients with seizure disorders","Risk of pulmonary vasoconstriction and increased pulmonary artery pressure","Use with caution in patients with hyperthyroidism, pheochromocytoma, or coronary artery disease"] |
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| Fetal Monitoring |
| Monitor maternal respiratory rate, heart rate, blood pressure, and oxygen saturation. Fetal monitoring for heart rate variability and signs of distress. Neonatal monitoring for respiratory depression if administered near delivery. |
| Fertility Effects | No known adverse effects on fertility based on animal studies; human data limited. |