PALLADONE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PALLADONE (PALLADONE).
Agonist at mu-opioid receptors, modulating pain perception via central and peripheral pathways.
| Metabolism | Hepatic via CYP3A4 and CYP2D6 to active metabolite hydromorphone; also via glucuronidation. |
| Excretion | Primarily renal (90%) as unchanged drug and glucuronide conjugate; ~10% biliary/fecal. |
| Half-life | Terminal elimination half-life is approximately 18 hours (range 12-24 h); supports extended dosing intervals. |
| Protein binding | Approximately 95-99% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd ~4 L/kg (range 2-6 L/kg). Large Vd indicates extensive tissue distribution. |
| Bioavailability | Oral: ~40% (range 20-60%) due to first-pass metabolism; rectal: similar to oral. |
| Onset of Action | Immediate-release: 15-30 min; extended-release: 1-2 hours. Peak effect at 1-2 h (IR) and 3-6 h (ER). |
| Duration of Action | Immediate-release: 3-6 h; extended-release: 12-24 h. Duration is dose and formulation dependent. |
Immediate-release: 4-8 mg orally every 4-6 hours as needed for pain; extended-release: 8 mg orally every 12 hours, titrated based on response and tolerance.
| Dosage form | CAPSULE, EXTENDED RELEASE |
| Renal impairment | For CrCl 30-59 mL/min: start with 50% of recommended dose and titrate cautiously; for CrCl <30 mL/min: not recommended. |
| Liver impairment | Child-Pugh Class A: no adjustment; Child-Pugh Class B: start at 50% of usual dose and monitor; Child-Pugh Class C: not recommended. |
| Pediatric use | Weight-based dosing: 0.1-0.2 mg/kg orally every 4-6 hours as needed (immediate-release); maximum single dose 5 mg. Extended-release not recommended in children. |
| Geriatric use | Start at the low end of dosing range (e.g., 2-4 mg immediate-release every 4-6 hours) and titrate slowly; monitor for increased sensitivity and respiratory depression. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PALLADONE (PALLADONE).
| Breastfeeding | Hydromorphone is excreted into breast milk. The milk-to-plasma (M/P) ratio is approximately 0.65. The estimated infant dose via breast milk is about 0.5-1% of the maternal weight-adjusted dose. While generally considered compatible with breastfeeding at low maternal doses, caution is advised; monitor infant for excessive drowsiness, respiratory depression, and feeding difficulties. Avoid use in mothers with high-dose or prolonged therapy. |
| Teratogenic Risk | PALLADONE (hydromorphone) is an opioid agonist. Data in pregnancy are limited. First trimester: Use is associated with a small risk of congenital malformations, particularly neural tube defects, based on some epidemiologic studies; however, absolute risk is low. Second and third trimesters: Chronic use may lead to fetal dependence and neonatal opioid withdrawal syndrome (NOWS) after delivery. Additionally, use near term may cause neonatal respiratory depression, and use during labor may prolong labor. |
■ FDA Black Box Warning
Addiction, abuse, and misuse; life-threatening respiratory depression; accidental ingestion; neonatal opioid withdrawal syndrome; interaction with alcohol and CNS depressants.
| Serious Effects |
["Significant respiratory depression","Acute or severe bronchial asthma","Known or suspected gastrointestinal obstruction","Hypersensitivity to hydromorphone or any component","Concurrent use of MAOIs or within 14 days"]
| Precautions | ["Respiratory depression","Addiction and abuse potential","Risks from concomitant use of benzodiazepines or other CNS depressants","Neonatal opioid withdrawal syndrome","Adrenal insufficiency","Severe hypotension","Seizures","Serotonin syndrome with serotonergic drugs"] |
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| Fetal Monitoring | Maternal monitoring: Assess pain control, respiratory rate, sedation level, and bowel function. Fetal/neonatal monitoring: During pregnancy, fetal heart rate monitoring may be indicated with chronic use. Newborns exposed in utero should be monitored for signs of neonatal opioid withdrawal syndrome (e.g., irritability, poor feeding, tremors) for 48-72 hours after birth. Neonatal respiratory monitoring is essential if opioids are used near term. |
| Fertility Effects | PALLADONE may reduce fertility in both males and females due to effects on hormonal regulation (e.g., suppression of gonadotropin-releasing hormone, reduced libido, and menstrual irregularities). In animal studies, hydromorphone caused decreased fertility in males and females. Reversibility upon discontinuation is possible but not well-characterized. |