What it isKappa agonist and mu partial agonist; moderate pain.
Why this oneA ceiling on respiratory depression, and the oral form is combined with naloxone to deter injection.
What limits itDysphoria and hallucinations from kappa agonism, worst in the elderly. It precipitates withdrawal in the opioid-dependent.
FDA-approved for
FDA label
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BOXED WARNING Opioid: risk of addiction, abuse, and misuse; life-threatening respiratory depression; fatal accidental ingestion (esp. children); profound sedation/death with benzodiazepines or CNS depressants; neonatal opioid withdrawal syndrome; REMS.
| FDA dosing | Population | Start | Target | Max |
| Pain | adult | 1 tablet q3-4h PRN | 1-2 tablets q3-4h PRN | 12 tablets/day |
Renal Undefined
Hepatic Undefined
Total daily dose should not exceed 12 tablets.
Instructions
- Use lowest effective dose for shortest duration
- Do not abruptly discontinue in physically dependent patients - taper by no more than 10-25% of daily dose every 2-4 weeks
- Ensure access to an opioid overdose reversal agent
Contraindications
- Significant respiratory depression
- Acute or severe bronchial asthma in an unmonitored setting or without resuscitative equipment
- Known or suspected GI obstruction, including paralytic ileus
Cautions
- Life-threatening respiratory depression
- Addiction, abuse, and misuse
- Serotonin syndrome with concomitant serotonergic drugs
- Adrenal insufficiency
- Severe hypotension
- Seizures; may raise intracranial pressure
- Profound sedation/respiratory depression with benzodiazepines or other CNS depressants
Adverse reactions
- Nausea, vomiting, constipation
- Dizziness, lightheadedness, sedation, euphoria
- Hallucinations (usually visual), disorientation, confusion
- Sweating
- Hypertension, hypotension, tachycardia
- Visual blurring, miosis
Pregnancy Prolonged use can cause neonatal opioid withdrawal syndrome; no adequate human data - advise of potential fetal risk.
Lactation Excreted in human milk; use with caution and monitor infant for excess sedation/respiratory depression.
⚠ BOXED WARNINGS
- Addiction, abuse and misuse
- Life-threatening respiratory depression
- Risk from concomitant use with benzodiazepines
Classes and tags
Clinical profile
Direct muscarinic antagonism0 / 4
Mechanism of action: Pentazocine ballicule
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