Usual Adult Dose for Pain

1 tablet = pentazocine 50 mg/naloxone 0.5 mg

Initial dose: 1 tablet orally every 3 to 4 hours as needed

• May increase dose to 2 tablets orally every 3 to 4 hours as needed

• It is safer to underestimate a patient's 24-hour dosage than overestimate and manage an adverse reaction due to overdose.

• Doses should be initiated individually according to the severity of the pain, patient response, prior analgesic treatment experience, risk factors for addiction, abuse, and misuse.
• Monitor closely for respiratory depression especially on initiation and with each dose increase.
• Because of the risks of addiction, abuse, and misuse, even at recommended doses, this drug should be reserved for use in patients for whom alternative treatment options have not or are not expected to be tolerated or have not or are not expected to provide adequate analgesia.

• For the management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate.

Usual Pediatric Dose for Pain

1 tablet = pentazocine 50 mg/naloxone 0.5 mg

Age: 12 years or older:
Initial dose: 1 tablet orally every 3 to 4 hours as needed

• May increase dose to 2 tablets orally every 3 to 4 hours as needed

• It is safer to underestimate a patient's 24-hour dosage than overestimate and manage an adverse reaction due to overdose.

• Doses should be initiated individually according to the severity of the pain, patient response, prior analgesic treatment experience, risk factors for addiction, abuse, and misuse.
• Monitor closely for respiratory depression especially on initiation and with each dose increase.
• Because of the risks of addiction, abuse, and misuse, even at recommended doses, this drug should be reserved for use in patients for whom alternative treatment options have not or are not expected to be tolerated or have not or are not expected to provide adequate analgesia.

• For the management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate.

Renal Dose Adjustments

Use with caution

Liver Dose Adjustments

Use with caution

Dose Adjustments

Elderly: Generally, start at the low end of the dosing range; titrate slowly and monitor closely for signs of central nervous system and respiratory depression; may be useful to monitor renal function.

Elderly, cachectic, or debilitated: Consider nonopioid analgesic agents; if used, follow guidance for elderly patients.

Discontinuation in Physically Dependent Patients:

• Taper dose gradually by 25% to 50% every 2 to 4 days
• If signs and symptoms of withdrawal appear, may raise the dose to the previous level and taper more slowly (either by increasing the interval between doses, decreasing the dose, or both)
• Do not abruptly discontinue in the physically-dependent patient

Precautions

The US FDA requires a Risk Evaluation and Mitigation Strategy (REMS) for all opioids intended for outpatient use. The new FDA Opioid Analgesic REMS is a designed to assist in communicating the serious risks of opioid pain medications to patients and health care professionals. It includes a medication guide and elements to assure safe use. For additional information: www.accessdata.fda.gov/scripts/cder/rems/index.cfm

US BOXED WARNINGS:

• ADDICTION, ABUSE, AND MISUSE: This drug exposes patients and other users to the risks of opioid addiction, abuse, and misuse, which can lead to overdose and death. Assess each patient's risk prior to prescribing this drug and monitor all patients regularly for the development of these behaviors or conditions.
• RISK EVALUATION AND MITIGATION STRATEGY (REMS): To ensure that the benefits of opioid analgesics outweigh the risks of addiction, abuse, and misuse, a REMS is required for these products. Under the requirements of the REMS, drug companies with approved opioid analgesic products must make REMS-compliant education programs available to healthcare providers. Healthcare providers are strongly encouraged to complete a REMS-compliant education program; counsel patients and/or their caregivers, with every prescription on safe use, serious risks, storage, and disposal of these products; emphasize to patients and their caregivers the importance of reading the Medication Guide every time it is provided by their pharmacist, and consider other tools to improve patient, household, and community safety.
• LIFE-THREATENING RESPIRATORY DEPRESSION: Serious, life-threatening, or fatal respiratory depression may occur with use. Monitor for respiratory depression, especially during initiation of therapy or following a dose increase.
• ACCIDENTAL INGESTION of even one dose, especially by children, can result in a fatal overdose of pentazocine
• NEONATAL OPIOID WITHDRAWAL SYNDROME: Prolonged use during pregnancy can result in neonatal opioid withdrawal syndrome, which may be life-threatening if not recognized and treated, and requires management according to protocols developed by neonatology experts. If opioid use is required for a prolonged period in a pregnant woman, advise the patient of the risk of neonatal opioid withdrawal syndrome and ensure that appropriate treatment will be available.
• RISKS FROM CONCOMITANT USE WITH BENZODIAZEPINES OR OTHER CNS DEPRESSANTS: Concomitant use of opioids with benzodiazepines or other central nervous system (CNS) depressants, including alcohol, may result in profound sedation, respiratory depression, coma, and death. Reserve concomitant use for patients for whom alternative treatment options are inadequate. Limit dosages and durations to the minimum required, and follow patients for signs and symptoms of respiratory depression.

• Significant respiratory depression
• Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment
• Known or suspected gastrointestinal obstruction, including paralytic ileus
• Hypersensitivity to either pentazocine, naloxone, or any of the formulation excipients (e.g., anaphylaxis)

Dialysis

Data not available

Other Comments

Administration Advice:

• Take orally; may be taken with food or milk to decrease gastrointestinal side effects

• Protect from light

• Due to the risk of addiction, abuse, and misuse with opioids, even at recommended doses, this drug is reserved for use in patients for whom alternative treatment options (non-opioid analgesics) are ineffective, not tolerated, or would be otherwise be inadequate to provide sufficient pain management; the lowest effective dose should be used for the shortest duration consistent with individual patient treatment goals.
• Proper dosing and titration of this drug are essential to reduce the risk of respiratory depression, for patients receiving other opioid analgesics and switching to this drug, it is safer to underestimate a patient's 24-hour oral requirement and provide rescue medication than overestimate and manage an adverse reaction; there is substantial inter-patient variation in the relative potency of different opioid drugs that conversion tables are not able to capture.

• Cardiovascular: Monitor for signs of hypotension upon initiating therapy and following dose increases, especially those whose blood pressure is compromised
• Respiratory: Monitor for respiratory depression, especially within the first 24 to 72 hours of initiation and with dose increases.
• Gastrointestinal: Monitor for constipation and decreased bowel motility in post-operative patients.
• General: Monitor routinely for maintenance of pain control and incidence of adverse reactions.
• Psychiatric: Patients should be monitored for the development of addiction, abuse, or misuse.

• Patients should be instructed to read the US FDA-approved Medication Guide each time this drug is dispensed; they should understand the safe use, serious risks, and proper storage and disposal of this drug.
• Advise patients to store this drug safely out of the sight and reach of children; accidental use by a child is a medical emergency and can result in death.
• Patients should understand that this drug, even when taken as recommended can result in addiction, abuse, and misuse; instruct patients not to share their drug with others and protect from theft or misuse.
• Patients should understand the risks of life-threatening respiratory depression, and be informed as to when this risk is greatest; patients should be advised to avoid alcoholic beverages, or respiratory depressant medications while on treatment.
• This drug may cause drowsiness, dizziness, or impair thinking or motor skills; patients should avoid driving or operating machinery during therapy.
• Women of child bearing potential should understand that prolonged use during pregnancy can result in neonatal opioid withdrawal syndrome and that prompt recognition and treatment will be necessary.