Pentazocine/naloxone Tablets

Manufacturer ACTAVIS Active Ingredient Pentazocine and Naloxone(pen TAZ oh seen & nal OKS one) Pronunciation pen-TAZ-oh-seen / nal-OKS-own
WARNING: This drug has an opioid drug in it. Opioid drugs can put you at risk for drug use disorder. Misuse or abuse of this drug can lead to overdose and death. If you have questions, talk with your doctor.Severe breathing problems may happen with this drug. The risk is highest when you first start taking this drug or any time your dose is raised. These breathing problems can be deadly. Call your doctor right away if you have slow, shallow, or trouble breathing.Even one dose of this drug may be deadly if it is taken by someone else or by accident, especially in children. If this drug is taken by someone else or by accident, get medical help right away.Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.Severe side effects have happened when opioid drugs were used with benzodiazepines, alcohol, marijuana, other forms of cannabis, or street drugs. This includes severe drowsiness, breathing problems, and death. Benzodiazepines include drugs like alprazolam, diazepam, and lorazepam. If you have questions, talk with the doctor.Many drugs interact with this drug and can raise the chance of side effects like deadly breathing problems. Talk with your doctor and pharmacist to make sure it is safe to use this drug with all of your drugs.Get medical help right away if you feel very sleepy, very dizzy, or if you pass out. Caregivers or others need to get medical help right away if the patient does not respond, does not answer or react like normal, or will not wake up.If you are pregnant or plan to get pregnant, talk with your doctor right away about the benefits and risks of using this drug during pregnancy. Using this drug for a long time during pregnancy may lead to withdrawal in the newborn baby. Withdrawal in the newborn can be life- threatening if not treated. @ COMMON USES: It is used to manage pain when non- opioid pain drugs do not treat your pain well enough or you cannot take them.
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Drug Class
Opioid analgesic, opioid antagonist combination
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Pharmacologic Class
Opioid agonist-antagonist (Pentazocine), Opioid antagonist (Naloxone)
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Pregnancy Category
Category C
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FDA Approved
Jan 1978
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DEA Schedule
Schedule IV

Overview

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What is this medicine?

This medication is a combination of two drugs used to treat moderate to severe pain. Pentazocine is a pain reliever that works on your brain and nervous system. Naloxone is added to help prevent misuse of the medication, but it doesn't affect the pain relief when taken by mouth as prescribed.
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How to Use This Medicine

Taking Your Medication Correctly

To use this medication safely and effectively, follow your doctor's instructions and read all the information provided. Take your medication with or without food, but if it causes stomach upset, take it with food. Always take this medication by mouth and never inject or snort it, as this can lead to severe side effects, including breathing difficulties and overdose, which can be fatal.

Storing and Disposing of Your Medication

Store your medication at room temperature in a dry place, avoiding bathrooms. Keep it in a secure location where children and others cannot access it, such as a locked box or area. Also, keep all medications away from pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so. Consult your pharmacist for guidance on proper disposal, and consider participating in local drug take-back programs.

Managing Missed Doses

If you take this medication regularly, take a missed dose as soon as you remember. However, if it's close to the time for your next dose, skip the missed dose and resume your regular schedule. Do not take two doses at the same time or take extra doses. If you take this medication as needed, follow your doctor's instructions and do not take it more frequently than recommended.
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Lifestyle & Tips

  • Do not drink alcohol or use other sedating medications (like tranquilizers or sleeping pills) while taking this drug, as it can increase the risk of serious side effects like severe drowsiness and breathing problems.
  • Avoid driving or operating heavy machinery until you know how this medication affects you, as it can cause dizziness or drowsiness.
  • To prevent constipation, drink plenty of fluids, eat fiber-rich foods, and consider a stool softener as advised by your doctor.
  • Store this medication securely away from children and pets to prevent accidental ingestion, which can be fatal.
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Available Forms & Alternatives

Available Strengths:

Dosing & Administration

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Adult Dosing

Standard Dose: 50 mg pentazocine / 0.5 mg naloxone orally every 3 to 4 hours as needed
Dose Range: 50 - 100 mg

Condition-Specific Dosing:

moderate to severe pain: Initial dose 50 mg pentazocine / 0.5 mg naloxone. May be increased to 100 mg pentazocine / 1 mg naloxone per dose if needed. Maximum daily dose is 600 mg pentazocine / 6 mg naloxone.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established
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Dose Adjustments

Renal Impairment:

Mild: Use with caution; consider lower doses and extended dosing intervals.
Moderate: Use with caution; consider lower doses and extended dosing intervals.
Severe: Use with caution; consider lower doses and extended dosing intervals.
Dialysis: Pentazocine is not significantly removed by hemodialysis. Use with caution; monitor for increased effects.

Hepatic Impairment:

Mild: Use with caution; consider lower doses and extended dosing intervals due to reduced metabolism.
Moderate: Use with caution; consider lower doses and extended dosing intervals due to reduced metabolism.
Severe: Use with caution; consider lower doses and extended dosing intervals due to reduced metabolism.

Pharmacology

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Mechanism of Action

Pentazocine is a synthetic opioid agonist-antagonist. It acts as an agonist at kappa (Îē) and sigma (΃) opioid receptors and as a weak antagonist or partial agonist at mu (Îŧ) opioid receptors. Its analgesic effects are primarily mediated through kappa receptor activation. Naloxone is a pure opioid antagonist that competitively binds to mu (Îŧ), kappa (Îē), and delta (δ) opioid receptors. It is included in the tablet formulation to deter intravenous abuse of pentazocine; when taken orally, naloxone has very low bioavailability and does not significantly antagonize the effects of pentazocine, but if injected, it can precipitate withdrawal in opioid-dependent individuals.
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Pharmacokinetics

Absorption:

Bioavailability: Pentazocine: ~20% (oral, due to extensive first-pass metabolism); Naloxone: <2% (oral, due to extensive first-pass metabolism)
Tmax: Pentazocine: 1-3 hours; Naloxone: Rapid (if absorbed)
FoodEffect: Food may slightly delay absorption but does not significantly affect the extent of absorption.

Distribution:

Vd: Pentazocine: ~3-7 L/kg; Naloxone: ~2 L/kg
ProteinBinding: Pentazocine: ~60%; Naloxone: ~45%
CnssPenetration: Pentazocine: Yes; Naloxone: Limited (when taken orally)

Elimination:

HalfLife: Pentazocine: 2-3 hours; Naloxone: 30-81 minutes
Clearance: Not available
ExcretionRoute: Renal (primarily metabolites), Fecal (minor)
Unchanged: Pentazocine: <10%; Naloxone: <5%
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Pharmacodynamics

OnsetOfAction: 15-30 minutes (oral)
PeakEffect: 1-3 hours
DurationOfAction: 3-4 hours

Safety & Warnings

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BLACK BOX WARNING

RISK OF ADDICTION, ABUSE, AND MISUSE; LIFE-THREATENING RESPIRATORY DEPRESSION; ACCIDENTAL INGESTION; NEONATAL OPIOID WITHDRAWAL SYNDROME; and RISKS FROM CONCOMITANT USE WITH BENZODIAZEPINES OR OTHER CNS DEPRESSANTS.
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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:

Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high or low blood pressure, including:
+ Severe headache
+ Dizziness
+ Passing out
+ Changes in eyesight
Signs of low blood sugar, such as:
+ Dizziness
+ Headache
+ Feeling sleepy or weak
+ Shaking
+ Fast heartbeat
+ Confusion
+ Hunger
+ Sweating
Breathing difficulties, including:
+ Trouble breathing
+ Slow or shallow breathing
+ Noisy breathing
+ Sleep apnea (breathing problems during sleep)
Feeling confused
Severe constipation or stomach pain, which may be signs of a severe bowel problem
Feeling extremely tired or weak
Hallucinations (seeing or hearing things that are not there)
Seizures
Chest pain or pressure, or a rapid heartbeat
Changes in eyesight
Trouble passing urine
Mood changes
Fever, chills, or sore throat
Abnormal sensations, such as burning, numbness, or tingling

Serotonin Syndrome: A Potentially Life-Threatening Condition

If you take this medication with certain other drugs, you may be at risk of developing serotonin syndrome, a severe and potentially deadly condition. Seek medical help immediately if you experience:

Agitation
Changes in balance
Confusion
Hallucinations
Fever
Fast or abnormal heartbeat
Flushing
Muscle twitching or stiffness
Seizures
Shivering or shaking
Excessive sweating
Severe diarrhea, upset stomach, or vomiting
Severe headache

Adrenal Gland Problems: A Rare but Serious Condition

Taking an opioid medication like this one may lead to a rare but severe adrenal gland problem. Contact your doctor right away if you experience:

Extreme tiredness or weakness
Passing out
Severe dizziness
Upset stomach
Vomiting
Decreased appetite

Other Possible Side Effects

While many people may not experience any side effects or only minor ones, it's essential to be aware of the following potential side effects:

Constipation
Diarrhea
Stomach pain
Upset stomach
Vomiting
Decreased appetite
Dizziness or drowsiness
Excessive sweating
Headache
Dry mouth

If you're concerned about any side effects or have questions, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Slow, shallow, or difficult breathing
  • Extreme drowsiness or difficulty waking up
  • Severe dizziness or lightheadedness
  • Confusion or disorientation
  • Bluish lips or fingernails
  • Severe constipation or abdominal pain
  • Signs of an allergic reaction (rash, itching, swelling, severe dizziness, trouble breathing)
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including:
+ Respiratory problems like asthma, breathing difficulties, or sleep apnea
+ Elevated carbon dioxide levels in the blood
+ Stomach or bowel blockage or narrowing
Current use of opioid pain medications, such as morphine or oxycodone
Use of specific drugs, including buprenorphine, butorphanol, or nalbuphine

Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, it is crucial to disclose all of your:

Prescription and over-the-counter medications
Natural products
Vitamins
Health problems

Your doctor and pharmacist need this information to determine whether it is safe for you to take this medication with your existing health conditions and medications. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
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Precautions & Cautions

Important Warnings and Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.

Caution with Daily Activities
Avoid driving and engaging in activities that require alertness until you understand how this medication affects you. To minimize the risk of dizziness or fainting, rise slowly from a sitting or lying position, and exercise caution when climbing stairs.

Tolerance and Dependence
Long-term or high-dose use of this medication may lead to tolerance, where the medication becomes less effective, and higher doses may be required to achieve the same effect. If you experience a decrease in the medication's effectiveness, contact your doctor. Do not take more than the prescribed dose.

Additionally, regular use of opioid medications like this one can cause dependence. If you need to reduce the dose or stop taking this medication, consult your doctor first, as sudden changes may increase the risk of withdrawal or other severe problems. Follow your doctor's instructions carefully, and report any adverse effects, such as increased pain, mood changes, suicidal thoughts, or other concerns.

Safe Use and Dosage
Do not exceed the prescribed dose, frequency, or duration of treatment, as this may increase the risk of severe side effects. Avoid taking this medication with other strong pain medications or using a pain patch without consulting your doctor first.

If your pain worsens, you experience increased sensitivity to pain, or you develop new pain, contact your doctor immediately. Do not take more than the prescribed dose.

Special Considerations
If you have an opioid use disorder and are prescribed this medication, you may experience withdrawal symptoms, such as sweating, shaking, fever, chills, diarrhea, nausea, vomiting, stomach cramps, goosebumps, body aches, anxiety, irritability, yawning, or rapid heartbeat.

Do not consume alcohol or products containing alcohol while taking this medication, as this may lead to unsafe and potentially fatal effects.

Long-term Use and Hormonal Effects
Prolonged use of opioid medications like this one may cause a decrease in sex hormone levels. If you experience a decrease in libido, fertility problems, irregular menstrual periods, or ejaculation difficulties, contact your doctor.

Seizure Risk
This medication may increase the risk of seizures, particularly in individuals with a history of seizures. Discuss your risk with your doctor.

Age-Related Precautions
If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects.

Breastfeeding
Inform your doctor if you are breastfeeding, as this medication passes into breast milk and may harm your baby. Seek medical attention immediately if your baby appears excessively sleepy, limp, or has breathing difficulties.
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Overdose Information

Overdose Symptoms:

  • Pinpoint pupils
  • Slowed or stopped breathing
  • Extreme drowsiness or unresponsiveness
  • Limp muscles
  • Cold, clammy skin
  • Slowed heart rate
  • Loss of consciousness

What to Do:

Seek immediate emergency medical attention. Call 911 or Poison Control at 1-800-222-1222. Naloxone (Narcan) may be administered by emergency personnel.

Drug Interactions

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Contraindicated Interactions

  • Not explicitly contraindicated with specific drugs, but caution with MAOIs due to theoretical risk of serotonin syndrome.
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Major Interactions

  • CNS depressants (e.g., alcohol, benzodiazepines, other opioids, sedatives, hypnotics, general anesthetics, phenothiazines, tricyclic antidepressants): Increased risk of respiratory depression, profound sedation, coma, and death.
  • Serotonergic drugs (e.g., SSRIs, SNRIs, TCAs, triptans, MAOIs, St. John's Wort): Risk of serotonin syndrome.
  • Mixed agonist/antagonist opioids (e.g., buprenorphine, butorphanol, nalbuphine): May precipitate withdrawal symptoms due to competitive binding at opioid receptors.
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Moderate Interactions

  • Anticholinergic drugs: Increased risk of urinary retention and severe constipation.
  • CYP2D6 inhibitors (e.g., quinidine, fluoxetine, paroxetine): May increase pentazocine plasma concentrations, leading to increased opioid effects.
  • CYP3A4 inhibitors (e.g., ketoconazole, erythromycin, ritonavir): May increase pentazocine plasma concentrations.
  • CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin): May decrease pentazocine plasma concentrations, leading to reduced efficacy.
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Minor Interactions

  • Not available

Monitoring

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Baseline Monitoring

Pain assessment (intensity, location, quality)

Rationale: To establish baseline and guide initial dosing.

Timing: Prior to initiation

Respiratory rate and depth

Rationale: To assess baseline respiratory function, especially important due to risk of respiratory depression.

Timing: Prior to initiation

Level of consciousness/sedation

Rationale: To assess baseline neurological status.

Timing: Prior to initiation

Renal and hepatic function tests (e.g., BUN, creatinine, ALT, AST)

Rationale: To identify potential impairment that may require dose adjustment.

Timing: Prior to initiation, if clinically indicated

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Routine Monitoring

Pain relief and adverse effects (e.g., sedation, nausea, constipation, dizziness)

Frequency: Regularly during therapy, especially during dose titration

Target: Adequate pain control with tolerable side effects

Action Threshold: Inadequate pain control or intolerable side effects warrant dose adjustment or alternative therapy.

Respiratory rate and depth

Frequency: Periodically, especially after dose changes or with concomitant CNS depressants

Target: >10-12 breaths/min, regular rhythm

Action Threshold: Respiratory rate <10 breaths/min, shallow breathing, or signs of hypoventilation require immediate intervention.

Level of consciousness/sedation

Frequency: Periodically, especially after dose changes or with concomitant CNS depressants

Target: Alert and oriented, or easily aroused

Action Threshold: Excessive sedation, somnolence, or difficulty arousing requires intervention.

Bowel function

Frequency: Regularly

Target: Regular bowel movements

Action Threshold: Constipation requires prophylactic measures or treatment.

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Symptom Monitoring

  • Respiratory depression (slow, shallow breathing)
  • Excessive sedation or somnolence
  • Dizziness or lightheadedness
  • Nausea and vomiting
  • Constipation
  • Urinary retention
  • Confusion or disorientation
  • Signs of serotonin syndrome (agitation, hallucinations, rapid heart rate, fever, sweating, shivering, muscle stiffness, twitching, loss of coordination, nausea, vomiting, diarrhea)
  • Signs of opioid withdrawal (if abruptly discontinued in dependent patients)

Special Patient Groups

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Pregnancy

Use during pregnancy is generally not recommended unless the potential benefit justifies the potential risk to the fetus. Chronic use during pregnancy can lead to neonatal opioid withdrawal syndrome.

Trimester-Specific Risks:

First Trimester: Potential for increased risk of major congenital malformations, though data for pentazocine specifically is limited.
Second Trimester: Risk of fetal growth restriction and other adverse outcomes with prolonged opioid exposure.
Third Trimester: Risk of neonatal opioid withdrawal syndrome (NOWS) if used chronically. Symptoms include irritability, hyperactivity, abnormal sleep pattern, high-pitched cry, tremor, vomiting, diarrhea, and poor feeding.
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Lactation

Pentazocine is excreted into breast milk. Naloxone is poorly absorbed orally by the infant. Monitor breastfed infants for signs of sedation, respiratory depression, or poor feeding. Use with caution, or consider alternative analgesics.

Infant Risk: Moderate risk (L3). Potential for infant sedation, respiratory depression, and withdrawal symptoms if mother discontinues drug abruptly. The amount of naloxone absorbed by the infant is negligible.
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Pediatric Use

Safety and efficacy have not been established in pediatric patients. Use is generally not recommended.

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Geriatric Use

Elderly patients may be more sensitive to the analgesic and adverse effects of pentazocine, particularly respiratory depression and CNS effects. Start with lower doses and titrate slowly, monitoring closely for adverse reactions.

Clinical Information

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Clinical Pearls

  • Pentazocine/naloxone is formulated to discourage IV abuse; the naloxone component is poorly absorbed orally but will precipitate withdrawal if injected in opioid-dependent individuals.
  • Due to its mixed agonist-antagonist properties, pentazocine can precipitate withdrawal symptoms in patients physically dependent on full opioid agonists.
  • Caution is advised when discontinuing therapy, especially after prolonged use, to avoid withdrawal symptoms. Tapering the dose gradually is recommended.
  • Patients should be educated on the risks of respiratory depression and CNS depression, especially when combined with other sedatives or alcohol.
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Alternative Therapies

  • Other opioid analgesics (e.g., oxycodone, hydrocodone, tramadol)
  • NSAIDs (e.g., ibuprofen, naproxen)
  • Acetaminophen
  • Other mixed opioid agonist-antagonists (e.g., buprenorphine, butorphanol, nalbuphine - though these are typically injectables or sublingual)
  • Non-pharmacological pain management strategies
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Cost & Coverage

Average Cost: Varies widely, typically $10-$50 per 30 tablets (generic)
Generic Available: Yes
Insurance Coverage: Tier 1 or Tier 2 (generic), Tier 3 or higher (brand)
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General Drug Facts

If your symptoms or health problems do not improve or worsen over time, it is essential to contact your doctor for further evaluation and guidance. To ensure safe and effective treatment, never share your medication with others or take someone else's medication.

This medication is accompanied by a Medication Guide, which provides crucial information about its safe use. It is essential to read this guide carefully and review it again whenever your prescription is refilled. If you have any questions or concerns about this medication, consult your doctor, pharmacist, or other healthcare provider for clarification.

In some cases, your doctor may prescribe naloxone, a medication used to treat opioid overdose, for you to keep on hand. This precaution is necessary because opioid overdose can occur if you resume taking opioid medications or take too much of this medication. If you are unsure about how to obtain or use naloxone, discuss your concerns with your doctor or pharmacist.

In the event of a suspected opioid overdose, seek immediate medical attention, even if naloxone has been administered. Prompt treatment is critical in such situations, and delaying medical care can have serious consequences.