DALGAN
Clinical safety rating: caution
Comprehensive 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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DALGAN (DALGAN).
| Breastfeeding | Excreted in breast milk; M/P ratio not established. Limited human data; potential for infant sedation and withdrawal. Use only if essential, monitor infant for drowsiness and poor feeding. |
| 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 |
■ 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 dezocine or any component of the formulation","Significant respiratory depression","Acute or severe bronchial asthma in an unmonitored setting or without resuscitative equipment","Known or suspected gastrointestinal obstruction, including paralytic ileus","Concurrent use of monoamine oxidase inhibitors (MAOIs) or within 14 days of such therapy"]
| 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"] |
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| 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. |