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Pronunciation
(pen TAZ oh seen)
Generic Available (U.S.)
No
Index Terms
Controlled Substance
C-IV
U.S. Brand Names
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Relief of moderate-to-severe pain; has also been used as a sedative prior to surgery and as a supplement to surgical anesthesia
Pregnancy Risk Factor
C
Pregnancy Considerations
Pentazocine was not found to be teratogenic in animal studies. Pentazocine has been shown to cross the human placenta. Use should be avoided during labor and delivery of premature infants. Abstinence syndromes in the newborn have been reported after long-term use of pentazocine during pregnancy. Other adverse effects in the newborn have been reported following abuse of pentazocine during pregnancy; these effects may be due to pentazocine, other drugs abused, the mother's lifestyle, or a combination of all factors.
Lactation
Enters breast milk/use caution
Breast-Feeding Considerations
Pentazocine is excreted in human breast milk. Treatment of the mother with single doses of pentazocine is not expected to cause detrimental effects in nursing infants.
Contraindications
Hypersensitivity to pentazocine or any component of the formulation
Warnings/Precautions
Concerns related to adverse effects:
• Cardiovascular effects: May increase systemic and pulmonary arterial pressure and systemic vascular resistance; use with caution in patients who may not tolerate these alterations in hemodynamics (eg, heart failure).
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
• Hypotension: May cause hypotension; use with caution in patients with hypovolemia, cardiovascular disease (including acute MI), or drugs which may exaggerate hypotensive effects (including phenothiazines or general anesthetics).
• Injection-site reactions: Severe sclerosis has occurred at the injection-site following multiple injections; avoid SubQ use unless absolutely necessary; rotate sites of injection.
Disease-related concerns:
• Abdominal conditions: May obscure diagnosis or clinical course of patients with acute abdominal conditions.
• Adrenal insufficiency: Use with caution in patients with adrenal insufficiency, including Addison's disease.
• Biliary tract impairment: Use with caution in patients with biliary tract dysfunction; acute pancreatitis may cause constriction of sphincter of Oddi.
• CNS depression/coma: Use with caution in patients with CNS depression or coma.
• Drug abuse: Use with caution in patients with a history of drug abuse or acute alcoholism; potential for drug dependency exists. Tolerance, psychological and physical dependence may occur with prolonged use.
• Head trauma: Use with extreme caution in patients with head injury, intracranial lesions, or elevated intracranial pressure; exaggerated elevation of ICP may occur.
• Hepatic impairment: Use with caution in patients with hepatic dysfunction.
• Obesity: Use with caution in patients who are morbidly obese.
• Prostatic hyperplasia/urinary stricture: Use with caution in patients with prostatic hyperplasia and/or urinary stricture.
• Renal impairment: Use with caution in patients with renal dysfunction.
• Respiratory disease: Use with caution in patients with pre-existing respiratory compromise (hypoxia and/or hypercapnia), COPD or other obstructive pulmonary disease, and kyphoscoliosis or other skeletal disorder which may alter respiratory function; critical respiratory depression may occur, even at therapeutic dosages.
• Seizures: Use with caution in patients with a history of seizure disorders.
• Thyroid dysfunction: Use with caution in patients with thyroid dysfunction.
Concurrent drug therapy issues:
• Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
Special populations:
• Debilitated patients: Use with caution in debilitated patients; there is a greater potential for critical respiratory depression, even at therapeutic dosages.
• Elderly: May be inappropriate in this age group due to increased risk of CNS effects (confusion and hallucinations), in addition to its activity as a mixed opioid agonist and antagonist (Beers Criteria). If used, use lower initial doses.
Dosage form specific issues:
• Sulfites: Injection may contain sulfites which may cause allergic reaction.
Other warnings/precautions:
• Withdrawal: Concurrent use of agonist/antagonist analgesics may precipitate withdrawal symptoms and/or reduced analgesic efficacy in patients following prolonged therapy with mu opioid agonists. Abrupt discontinuation following prolonged use may also lead to withdrawal symptoms; taper dose to decrease risk of withdrawal symptoms.
Adverse Reactions
Frequency not defined.
Cardiovascular: Circulatory depression, facial edema, flushing, hyper-/hypotension, shock, syncope, systemic vascular resistance increased, tachycardia
Central nervous system: Chills, CNS depression, confusion, disorientation, dizziness, drowsiness, euphoria, excitement, hallucinations, headache, insomnia, irritability, lightheadedness, malaise, nightmares, sedation
Dermatologic: Dermatitis, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Gastrointestinal: Abdominal distress, anorexia, constipation, diarrhea, nausea, taste alteration, vomiting, xerostomia
Genitourinary: Urinary retention
Hematologic: Agranulocytosis (rare), eosinophilia, WBCs decreased
Local: Injection site reaction (tissue damage and irritation)
Neuromuscular & skeletal: Paresthesia, tremor, weakness
Ocular: Blurred vision, diplopia, miosis, nystagmus
Otic: Tinnitus
Respiratory: Dyspnea, respiratory depression (rare)
Miscellaneous: Anaphylaxis, diaphoresis, physical and psychological dependence
Drug Interactions
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Alvimopan: Analgesics (Opioid) may enhance the adverse/toxic effect of Alvimopan. This is most notable for patients receiving long-term (i.e., more than 7 days) opiates prior to alvimopan initiation. Management: Alvimopan is contraindicated in patients receiving therapeutic doses of opioids for more than 7 consecutive days immediately prior to alvimopan initiation. Risk D: Consider therapy modification
Ammonium Chloride: May increase the excretion of Analgesics (Opioid). Risk C: Monitor therapy
Amphetamines: May enhance the analgesic effect of Analgesics (Opioid). Risk C: Monitor therapy
Analgesics (Opioid): Mixed Agonist / Antagonist Opioids may diminish the analgesic effect of Analgesics (Opioid). Management: Seek alternatives to mixed agonist/antagonist opioids in patients receiving pure opioid agonists, and monitor for symptoms of therapeutic failure/high dose requirements (or withdrawal in opioid-dependent patients) if patients receive these combinations. Risk D: Consider therapy modification
Antipsychotic Agents (Phenothiazines): May enhance the hypotensive effect of Analgesics (Opioid). Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Exceptions: Levocabastine (Nasal). Risk C: Monitor therapy
Desmopressin: Analgesics (Opioid) may enhance the adverse/toxic effect of Desmopressin. Risk C: Monitor therapy
Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Management: For patients being treated with hydroxyzine, a reduction in the dose of any other CNS depressants that are to be used in combination is recommended. With concurrent use, monitor patients closely for excessive response to the combination. Risk D: Consider therapy modification
Pegvisomant: Analgesics (Opioid) may diminish the therapeutic effect of Pegvisomant. Risk C: Monitor therapy
Selective Serotonin Reuptake Inhibitors: Analgesics (Opioid) may enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Risk C: Monitor therapy
Succinylcholine: May enhance the bradycardic effect of Analgesics (Opioid). Risk C: Monitor therapy
Thiazide Diuretics: Analgesics (Opioid) may enhance the orthostatic hypotensive effect of Thiazide Diuretics. Risk C: Monitor therapy
Storage
Store at 20°C to 25°C (68°F to 77°F).
Compatibility
Y-site administration: Compatible: Heparin, hydrocortisone sodium succinate, potassium chloride, vitamin B complex with C. Incompatible: Nafcillin.
Compatibility in syringe: Compatible: Atropine, butorphanol, chlorpromazine, cimetidine, dimenhydrinate, diphenhydramine, droperidol, fentanyl, hydromorphone, hydroxyzine, meperidine, metoclopramide, morphine, prochlorperazine edisylate, promethazine, ranitidine. Incompatible: Glycopyrrolate, heparin, pentobarbital.
Compatibility when admixed: Incompatible: Aminophylline, amobarbital, pentobarbital, phenobarbital, sodium bicarbonate.
Mechanism of Action
Binds to opiate receptors in the CNS, causing inhibition of ascending pain pathways, altering the perception of and response to pain; produces generalized CNS depression; partial agonist-antagonist
Pharmacodynamics/Kinetics
Onset of action: I.M., SubQ: 15-20 minutes; I.V.: 2-3 minutes
Duration: 2-3 hours
Protein binding: 60%
Metabolism: Hepatic via oxidative and glucuronide conjugation pathways; extensive first-pass effect
Half-life elimination: 2-3 hours; prolonged with hepatic impairment
Excretion: Urine (small amounts as unchanged drug)
Dosage
Preoperative/preanesthetic: Children 1-16 years: I.M.: 0.5 mg/kg
Analgesia:
Children (unlabeled use): I.M.:
5-8 years: 15 mg
9-14 years: 30 mg
Adults:
I.M., SubQ: 30-60 mg every 3-4 hours; do not exceed 60 mg/dose (maximum: 360 mg/day)
I.V.: 30 mg every 3-4 hours; do not exceed 30 mg/dose (maximum: 360 mg/day)
Labor pain: Adults:
I.M.: 30 mg once
I.V.: 20 mg every 2-3 hours as needed (maximum total dose: 60 mg)
Elderly: Elderly patients may be more sensitive to the analgesic and sedating effects. The elderly may also have impaired renal function. If needed, dosing should be started at the lower end of dosing range and adjust dose for renal function.
Dosing adjustment in renal impairment:
Clcr 10-50 mL/minute: Administer 75% of normal dose
Clcr <10 mL/minute: Administer 50% of normal dose
Dosing adjustment in hepatic impairment: Reduce dose or avoid use in patients with liver disease
Administration: I.M.
Rotate injection site; avoid intra-arterial injection
Administration: Other
Rotate injection site; avoid SubQ use unless absolutely necessary (may cause tissue damage); avoid intra-arterial injection
Administration: I.V. Detail
pH: 4-5 (adjusted with lactic acid or sodium hydroxide)
Monitoring Parameters
Relief of pain, respiratory and mental status, blood pressure
Patient Education
May cause physical and/or psychological dependence. While using this medication, do not use alcohol and other prescription or OTC medications (especially sedatives, tranquilizers, antihistamines, or pain medications) without consulting prescriber. Maintain adequate hydration, unless instructed to restrict fluid intake. May cause hypotension, dizziness, drowsiness, impaired coordination, or blurred vision; nausea, vomiting, loss of appetite, or dry mouth; or constipation. Report persistent dizziness or headache, excessive fatigue or sedation, changes in mental status, weakness or trembling, or shortness of breath.
Geriatric Considerations
Pentazocine is not recommended for use in the elderly because of its propensity to cause delirium and agitation. If pentazocine must be used, be sure to adjust dose for renal function.
This medication is considered to be potentially inappropriate in this patient population (Beers Criteria severity: High).
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation).
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
Drowsiness and euphoria are common; may cause restlessness or nightmares; may rarely cause confusion, depression, or hallucinations
Mental Health: Effects on Psychiatric Treatment
Concurrent use with psychotropics may produce additive effects or toxicity; may cause withdrawal in patients currently dependent on narcotics
Nursing: Physical Assessment/Monitoring
Assess patient's physical and/or psychological dependence. For inpatients, implement safety measures to prevent falls. Discontinue slowly after prolonged use
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution:
Talwin®: 30 mg/mL (1 mL)
Talwin®: 30 mg/mL (10 mL) [contains sodium bisulfite]
Pricing: U.S. (www.drugstore.com)
Solution (Talwin)
30 mg/mL (10): $74.42
References
Aronoff GR, Bennett WM, Berns JS, et al, Drug Prescribing in Renal Failure: Dosing Guidelines for Adults and Children, 5th ed. Philadelphia, PA: American College of Physicians; 2007, 19.
Challoner KR, McCarron MM, and Newton EJ, “Pentazocine (Talwin®) Intoxication: Report of 57 Cases,” J Emerg Med, 1990, 8(1):67-74.
“Drugs for Pain,” Med Lett Drugs Ther, 2000, 42(1085):73-8.
Hanunen K, Olkkola KT, Seppala T, et al, “Pharmacokinetics and Pharmacodynamics of Pentazocine in Children,” Pharmacol Toxicol, 1993, 73(2):120-3.
“Principles of Analgesic Use in the Treatment of Acute Pain and Cancer Pain,” 6th ed, Glenview, IL: American Pain Society, 2008.
Ray AD and Gupta M, “Clinical Trial of Pentazocine as Analgesic in Pediatric Cases,” J Indian Med Assoc, 1994, 92(3):77-9.
Reed DA and Schnoll SH, “Abuse of Pentazocine-Naloxone Combination,” JAMA, 1986, 256(18):2562-4.
Rita L, Seleny FL, and Levin RM, “A Comparison of Pentazocine and Morphine for Pediatric Premedication,” Anesth Analg, 1970, 49(3):377-82.
Waterworth TA, “Pentazocine (Fortal) as Postoperative Analgesic in Children,” Arch Dis Child, 1974, 49(6):488-90.
International Brand Names
Lexi-Comp.com
Last full review/revision May 2011
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