Home > Medical Reference > Complementary Medicine

Pentazocine


Pronunciation

 (pen TAZ oh seen)


U.S. Brand Names

 Talwin®; Talwin® NX


Synonyms

 Naloxone Hydrochloride and Pentazocine Hydrochloride; Pentazocine Hydrochloride; Pentazocine Hydrochloride and Naloxone Hydrochloride; Pentazocine Lactate


Generic Available

 Yes: Tablet


Canadian Brand Names

 Talwin®


Use

 Relief of moderate to severe pain; has also been used as a sedative prior to surgery and as a supplement to surgical anesthesia


Restrictions

 C-IV


Pregnancy Risk Factor

 C/D (prolonged use or high doses at term)


Pregnancy Implications

 Pentazocine was not found to be teratogenic in animal studies. Pentazocine and naloxone have 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

 Excretion in breast milk unknown/use caution


Contraindications

 Hypersensitivity to pentazocine, naloxone, or any component of the formulation; increased intracranial pressure (unless the patient is mechanically ventilated); pregnancy (prolonged use or high doses at term)


Warnings/Precautions

 Use with caution in seizure-prone patients, acute myocardial infarction, patients undergoing biliary tract surgery, patients with renal and hepatic dysfunction, head trauma, increased intracranial pressure, and patients with a history of prior opioid dependence or abuse; pentazocine may precipitate opiate withdrawal symptoms in patients who have been receiving opiates regularly; injection contains sulfites which may cause allergic reaction; tolerance or drug dependence may result from extended use. Talwin® NX is intended for oral administration only - severe vascular reactions have resulted from misuse by injection.


Adverse Reactions

 Frequency not defined.

Cardiovascular: Hypotension, circulatory depression, shock, tachycardia, syncope, flushing

Central nervous system: Malaise, headache, nightmares, insomnia, CNS depression, sedation, hallucinations, confusion, disorientation, dizziness, euphoria, drowsiness, lightheadedness, irritability, chills, excitement

Dermatologic: Rash, pruritus, dermatitis, urticaria, Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme

Gastrointestinal: Nausea, vomiting, xerostomia, constipation, anorexia, diarrhea, abdominal distress

Genitourinary: Urinary retention

Hematologic: WBCs decreased, eosinophilia

Local: Tissue damage and irritation with I.M./SubQ use

Neuromuscular & skeletal: Weakness, tremor, paresthesia

Ocular: Blurred vision, miosis

Otic: Tinnitus

Respiratory: Dyspnea, respiratory depression (rare)

Miscellaneous: Physical and psychological dependence, facial edema, diaphoresis, anaphylaxis


Overdosage/Toxicology

 Symptoms of overdose include drowsiness, sedation, respiratory depression, and coma. Naloxone, 2 mg I.V., with repeat administration as necessary up to a total of 10 mg, can also be used to reverse toxic effects of the opiate.


Drug Interactions

May potentiate or reduce analgesic effect of opiate agonist (eg, morphine) depending on patients tolerance to opiates can precipitate withdrawal in narcotic addicts

Increased effect/toxicity with tripelennamine (can be lethal), CNS depressants (phenothiazines, tranquilizers, anxiolytics, sedatives, hypnotics, or alcohol)


Ethanol/Nutrition/Herb Interactions

 Ethanol: Avoid ethanol (may increase CNS depression).


Stability

 Store at room temperature, protect from heat and from freezing; I.V. form is incompatible with aminophylline, amobarbital (and all other I.V. barbiturates), glycopyrrolate (same syringe), heparin (same syringe), nafcillin (Y-site)


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, meperidine with perphenazine, metoclopramide, morphine, perphenazine, prochlorperazine edisylate, promazine, promethazine, propiomazine, ranitidine, scopolamine. 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: Oral, I.M., SubQ: 15-30 minutes; I.V.: 2-3 minutes

Duration: Oral: 4-5 hours; Parenteral: 2-3 hours

Protein binding: 60%

Metabolism: Hepatic via oxidative and glucuronide conjugation pathways; extensive first-pass effect

Bioavailability: Oral: ~20%; increased to 60% to 70% with cirrhosis

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: I.M.:

5-8 years: 15 mg

8-14 years: 30 mg

Children >12 years and Adults: Oral: 50 mg every 3-4 hours; may increase to 100 mg/dose if needed, but should not exceed 600 mg/day

Adults:

I.M., SubQ: 30-60 mg every 3-4 hours, not to exceed total daily dose of 360 mg

I.V.: 30 mg every 3-4 hours (maximum: 360 mg/day)

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

 Rotate injection site for I.M., SubQ use; avoid intra-arterial injection; avoid SubQ use unless absolutely necessary (may cause tissue damage)


Monitoring Parameters

 Relief of pain, respiratory and mental status, blood pressure


Patient Education

 If self-administered, use exactly as directed; do not increase dose or frequency. Drug 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 (2-3 L/day of fluids) unless instructed to restrict fluid intake. May cause hypotension, dizziness, drowsiness, impaired coordination, or blurred vision (use caution when driving, climbing stairs, or changing position - rising from sitting or lying to standing, or when engaging in tasks requiring alertness until response to drug is known); nausea, vomiting, loss of appetite, or dry mouth (frequent mouth care, small, frequent meals, chewing gum, or sucking lozenges may help); or constipation (increased exercise, fluids, fruit, or fiber may help; if unresolved, consult prescriber about use of stool softeners). Report persistent dizziness or headache; excessive fatigue or sedation; changes in mental status; changes in urinary elimination or pain on urination; weakness or trembling; blurred vision; or shortness of breath. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Consult prescriber if breast-feeding.


Additional Information

 Pentazocine hydrochloride: Talwin® NX tablet (with naloxone); naloxone is used to prevent abuse by dissolving tablets in water and using as injection.


Anesthesia and Critical Care Concerns/Other Considerations

 Naloxone is added to the tablet form of pentazocine to prevent abuse.

Mixed agonist-antagonist: May precipitate psychomimetic effects; may precipitate withdrawal in narcotic-dependent patients.


Dental Health: Effects on Dental Treatment

 No significant effects or complications reported


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


Oncology: Vesicant

 Local effects (stinging, induration, ulceration, thrombosis) have been associated with chronic use of pentazocine. I.M. injections are reported to cause less local tissue damage than SubQ injections.


Dosage Forms

Injection, solution (Talwin®): 30 mg/mL (1 mL, 10 mL) [10 mL size contains sodium bisulfite]

Tablet (Talwin® NX): Pentazocine 50 mg and naloxone 0.5 mg


References

Alexander JI and Spence AA, "Central Nervous Effects of Pentazocine," Br Med J , 1974, 2(912):224-5.

Challoner KR, McCarron MM, and Newton EJ, "Pentazocine (Talwin®) Intoxication: Report of 57 Cases," J Emerg Med , 1990, 8(1):67-74.

De Bard ML and Jagger JA, "T's and B's - Midwestern Heroin Substance," Clin Toxicol , 1981, 18(9):1117-23.

"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.

Martin WR, "Naloxone," Ann Intern Med , 1976, 85(6):765-8.

Mokhlesi B, Leikin JB, Murray P, et al, "Adult Toxicology in Critical Care: Part II: Specific Poisonings," Chest , 2003, 123(3):897-922.

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

 Fortal® (BE, FR, LU); Fortalgesic® [inj.] (CH); Fortalgesic® [Suppos.] (CH); Fortalgesic® [Tab.] (CH); Fortral® (AT, AU, CZ, DE, DK, GB, HR, NL, NZ, PL, RO, RU, SI, YU); Fortralin® [inj.] (NO); Fortralin® (NO); Fortwin® (RU, TH); Forwin® (RO); Ospronim® (ZA); Pangon® (TH); Peltazon® (JP); Pentagin® (JP); Pentavon® (IN); Pentazocina Fides® (ES); Pentazocine® (GB, ZA); Pentazocine-Profarma® (TH); Pentazocinum® (PL); Sosegon® [compr.] (ES, JP); Sosegon® [inj./rect.] (JP); Sosenol® (ZA); Talwin® (CA, HK, IL, IT)


A.D.A.M., Inc. is accredited by URAC, also known as the American Accreditation HealthCare Commission (www.urac.org). URAC's accreditation program is the first of its kind, requiring compliance with 53 standards of quality and accountability, verified by independent audit. A.D.A.M. is among the first to achieve this important distinction for online health information and services. Learn more about A.D.A.M.'s editorial process . A.D.A.M. is also a founding member of Hi-Ethics (www.hiethics.com) and subscribes to the principles of the Health on the Net Foundation (www.hon.ch).

The information provided herein should not be used during any medical emergency or for the diagnosis or treatment of any medical condition. A licensed medical professional should be consulted for diagnosis and treatment of any and all medical conditions. Call 911 for all medical emergencies. Links to other sites are provided for information only -- they do not constitute endorsements of those other sites. © 1997-2007 A.D.A.M., Inc. Any duplication or distribution of the information contained herein is strictly prohibited.
adam.com