Dangerous Drug: Pentazocine(pen taz’ oh seen)
Pentazocine Hydrochloride with Naloxone Hydrochloride, 0.5 mg Pentazocine Lactate
Parenteral: Talwin
PREGNANCY CATEGORY C
CONTROLLED SUBSTANCE C-IV
Drug Class
Opioid agonist-antagonist analgesic
Therapeutic Actions
Pentazocine acts as an agonist at specific (kappa) opioid receptors in the CNS to produce analgesia, sedation; acts as an agonist
at sigma opioid receptors to cause dysphoria, hallucinations; acts at mu opioid receptors to antagonize the analgesic and euphoric activities of some other opioid analgesics. Has lower abuse potential than morphine, other pure opioid agonists; the oral preparation contains the opioid antagonist naloxone, which has poor bioavailability when given orally and does not interfere with the analgesic effects of pentazocine but serves as a deterrent to the unintended IV injection of solutions made from the oral tablets.
at sigma opioid receptors to cause dysphoria, hallucinations; acts at mu opioid receptors to antagonize the analgesic and euphoric activities of some other opioid analgesics. Has lower abuse potential than morphine, other pure opioid agonists; the oral preparation contains the opioid antagonist naloxone, which has poor bioavailability when given orally and does not interfere with the analgesic effects of pentazocine but serves as a deterrent to the unintended IV injection of solutions made from the oral tablets.
Indications
Relief of moderate to severe pain
Preanesthetic medication and as supplement to surgical anesthesia
Contraindications and Cautions
Contraindicated with hypersensitivity to opioids, sulfites (oral and parenteral), naloxone (oral form); pregnancy (neonatal withdrawal); lactation.
Use cautiously with physical dependence on an opioid analgesic (can precipitate a withdrawal syndrome); alcoholism; bronchial asthma, COPD, cor pulmonale, respiratory depression, anoxia, increased intracranial pressure; acute MI with hypertension, left ventricular failure or nausea and vomiting; renal or hepatic impairment; labor or delivery (opioids given to the mother can cause neonatal respiratory depression; premature infants are especially at risk; may prolong labor).
Available Forms
Injection—30 mg/mL; tablets—50 mg with naloxane 0.5 mg
Dosages
Adults
Oral
Initially, 50 mg PO every 3–4 hr. Increase to 100 mg if needed. Do not exceed a total dose of 600 mg/24 hr.
Parenteral
30 mg IM, subcutaneously, or IV. May repeat every 3–4 hr. Doses exceeding 30 mg IV or 60 mg IM or subcutaneously are not recommended. Do not exceed 360 mg/24 hr. Give subcutaneously only when necessary; repeat injections should be given IM.
Patients in labor: A single 30-mg IM dose is most common. A 20-mg IV dose given 2–3 times at 2- to 3-hr intervals relieves pain when contractions become regular.
Pediatric patients younger than 12 yr
Not recommended.
Geriatric patients or impaired adults
Use caution; respiratory depression may occur in the very ill, and those with respiratory problems. Dosage may need to be reduced. Avoid long-term use for pain due to risk of falls, fractures, confusion, dependency, and withdrawal.
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