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Pentazocine is available in the following formulations:
- Pentazocine 30mg/ml Injectable Solution: For intramuscular, subcutaneous, or intravenous administration
- Pentazocine 50mg Tablets: For oral administration (often combined with naloxone to prevent misuse)
Pentazocine is a synthetic benzomorphan derivative with mixed agonist-antagonist opioid properties. It acts primarily as a kappa opioid receptor agonist and a weak mu opioid receptor antagonist, providing analgesia while limiting some of the adverse effects associated with pure mu agonists.
Pentazocine is primarily used for:
- Management of moderate to severe pain
- Preoperative or preanesthetic medication
- Supplement to surgical anesthesia
- Obstetrical analgesia during labor
- Relief of pain in patients with myocardial infarction
Dosing is individualized based on the specific medical indication, patient characteristics, and concurrent medications. Typical dosage ranges include:
- For injectable form: 30mg to 60mg every 3-4 hours as needed, not to exceed 360mg daily
- For oral tablets: 50mg to 100mg every 3-4 hours as needed, not to exceed 600mg daily
Important Safety Information
Pentazocine is a Schedule IV controlled substance with potential for dependence, though this risk is lower compared to pure mu agonists. It should be administered by or under the supervision of healthcare professionals familiar with its use.
Due to its partial antagonist properties, Pentazocine may precipitate withdrawal symptoms in patients physically dependent on pure opioid agonists. It should not be administered to patients who are dependent on opioids or are in opioid withdrawal.
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Common side effects include sedation, dizziness, nausea, vomiting, and sweating. Serious adverse effects requiring immediate intervention include respiratory depression, hypotension, and allergic reactions. Pentazocine may cause psychotomimetic effects in some patients, including hallucinations, dysphoria, and confusion.
Pentazocine should be used with caution in patients with respiratory impairment, head injury, increased intracranial pressure, impaired hepatic or renal function, and in elderly or debilitated patients.
For more information about pain management medications and opioid safety, please visit these authoritative resources:
- American Society of Anesthesiologists
- FDA Drug Safety Information
- MedlinePlus Pentazocine Information
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Pentazocine is a synthetic opioid analgesic with the following characteristics:
- Chemical Name: (2R*,6R*,11R*)-1,2,3,4,5,6-Hexahydro-6,11-dimethyl-3-(3-methyl-2-butenyl)-2,6-methano-3-benzazocin-8-ol
- Mechanism of Action: Kappa opioid receptor agonist and weak mu opioid receptor antagonist
- Onset of Action: 15-30 minutes when administered intramuscularly, 2-3 minutes when administered intravenously
- Duration of Action: 2-3 hours
- Metabolism: Primarily hepatic
- Elimination Half-life: 2-3 hours
- Potency Comparison: Approximately 1/3 to 1/2 the potency of morphine for analgesia
Pentazocine offers several clinical advantages in specific scenarios:
- Less respiratory depression than pure mu agonists at equianalgesic doses
- Lower potential for physical dependence compared to Schedule II opioids
- Minimal effect on cardiovascular parameters at therapeutic doses
- Available in both injectable and oral formulations for versatile administration
- Classified as Schedule IV controlled substance, indicating lower abuse potential
- May cause less constipation than morphine and other pure mu agonists
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