DALGAN
Clinical safety rating
cautionComprehensive clinical and safety monograph for DALGAN (DALGAN).
Dalgan (generic: dezocine) is a mixed opioid agonist-antagonist that acts as a partial agonist at mu-opioid receptors and a full agonist at kappa-opioid receptors, producing analgesia through modulation of pain signaling in the central nervous system. It also exhibits antagonist activity at mu receptors at higher doses, limiting its abuse potential and respiratory depression compared to full agonists.
| Metabolism | Primarily hepatic via glucuronidation and N-demethylation. Involves UDP-glucuronosyltransferase (UGT) enzymes and possibly cytochrome P450 (CYP) 3A4 contributes to minor metabolism to inactive metabolites. |
| Excretion | Renal: ~90% as unchanged drug and glucuronide conjugates; biliary/fecal: ~10%. |
| Half-life | Terminal half-life: 2–3 hours; clinically may be prolonged in renal impairment. |
| Protein binding | ~20% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 3–5 L/kg; suggests extensive tissue distribution. |
| Bioavailability | Oral: 40–60% (first-pass metabolism); IM: ~70%; rectal: ~50%. |
| Onset of Action | Oral: 30–60 minutes; IM: 15–30 minutes; IV: 5–10 minutes. |
| Duration of Action | Analgesic duration: 4–6 hours after oral/IM; 3–4 hours after IV; extended-release formulations provide up to 12 hours. |
| Molecular Weight | 327.45 |
Oral: 50-100 mg every 6-8 hours; maximum 400 mg/day. IV: 25-50 mg every 6 hours; maximum 200 mg/day.
| Dosage form | INJECTABLE |
| Renal impairment | GFR 10-50 mL/min: administer 50-75% of usual dose every 8-12 hours. GFR <10 mL/min: administer 50% of usual dose every 12 hours. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50% and extend interval to every 8-12 hours. Child-Pugh C: reduce dose by 75% and extend interval to every 12 hours. |
| Pediatric use | Oral: 0.5-1 mg/kg every 4-6 hours; maximum 4 mg/kg/day. IV: 0.3-0.5 mg/kg every 6 hours; maximum 2 mg/kg/day. |
| Geriatric use | Initiate at 50% of adult dose; titrate slowly to response; maximum 300 mg/day. Avoid in patients with creatinine clearance <30 mL/min. |
| 1st trimester | Avoid in first trimester due to potential teratogenic effects based on animal studies; human data limited. |
| 2nd trimester | Use only if clearly needed; may cause fetal respiratory depression and dependence with prolonged use. |
| 3rd trimester | Avoid near term; risk of neonatal respiratory depression, withdrawal syndrome, and meconium aspiration. |
Clinical note
Comprehensive clinical and safety monograph for DALGAN (DALGAN).
| Placental transfer | Crosses placenta; detected in fetal plasma at concentrations 50-80% of maternal levels. |
| Breastfeeding | DALGAN is excreted into breast milk in low concentrations. Use with caution; monitor infant for signs of respiratory depression or sedation. Consider alternative analgesics if prolonged use. |
| Lactation Rating | L3 - Moderately Safe |
| Teratogenic Risk | FDA Pregnancy Category C: First trimester risk of major malformations unknown; animal studies show fetal toxicity at high doses. Second/third trimester: risk of neonatal withdrawal syndrome if prolonged use near term. Avoid unless benefit outweighs risk. |
| Fetal Monitoring | Maternal: vital signs, pain scores, respiratory rate, sedation level, bowel function. Fetal/neonatal: heart rate monitoring during labor, observe for neonatal respiratory depression and withdrawal symptoms (irritability, poor feeding, tremors). |
| Fertility Effects | May impair female fertility by altering gonadotropin secretion; reversible upon discontinuation. No known male fertility effects. |
■ FDA Black Box Warning
WARNING: ADDICTION, ABUSE, AND MISUSE; LIFE-THREATENING RESPIRATORY DEPRESSION; NEONATAL OPIOID WITHDRAWAL SYNDROME; and RISKS FROM CONCOMITANT USE WITH BENZODIAZEPINES OR OTHER CNS DEPRESSANTS. Dalgan exposes users to risks of opioid addiction, abuse, and misuse, which can lead to overdose and death. Serious, life-threatening, or fatal respiratory depression may occur. Prolonged use during pregnancy can result in neonatal opioid withdrawal syndrome. Concomitant use with benzodiazepines or other CNS depressants may cause profound sedation, respiratory depression, coma, and death.
| Serious Effects |
Hypersensitivity to DALGAN or any componentSevere respiratory depressionAcute or severe bronchial asthmaParalytic ileusConcurrent use of MAO inhibitors or within 14 daysPostoperative pain management in children after tonsillectomy/adenoidectomy
| Precautions | Life-threatening respiratory depression: monitor closely, especially during initiation or dose escalation, Opioid-induced hyperalgesia: paradoxical increase in pain sensitivity, Adrenal insufficiency: monitor for symptoms of hypocortisolism, Severe hypotension: risk in hypovolemic patients or those with compromised blood pressure, Seizures: may exacerbate seizure disorders, Risks of use in patients with head injury or increased intracranial pressure, Avoid abrupt discontinuation: taper dose to prevent withdrawal syndrome, May precipitate withdrawal in opioid-dependent patients due to antagonist activity at mu receptors |
| Food/Dietary | Avoid grapefruit juice as it may increase dezocine levels via CYP3A4 inhibition. No other significant food interactions reported; take with or without food. Limit alcohol to prevent additive CNS depression. |
| Clinical Pearls | Dalgan (dezocine) is a mixed agonist-antagonist opioid with ceiling effect for respiratory depression; use caution in opioid-tolerant patients due to risk of precipitating withdrawal. Not recommended for prolonged use due to potential for dependence. Monitor for hypotension and bradycardia, especially in elderly or volume-depleted patients. |
| Patient Advice | Take exactly as prescribed; do not increase dose or frequency without consulting your doctor. · Avoid driving or operating heavy machinery until you know how this medication affects you. · Do not consume alcohol or other central nervous system depressants while taking this drug. · Report any signs of withdrawal (e.g., anxiety, sweating, cramping) or allergic reaction (rash, difficulty breathing) immediately. · Store at room temperature away from moisture and heat; keep out of reach of children. |
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