Pentazocine/naloxone Tablets
Overview
What is this medicine?
How to Use This Medicine
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.
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.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Condition-Specific Dosing:
Pediatric Dosing
Dose Adjustments
Renal Impairment:
Hepatic Impairment:
Pharmacology
Mechanism of Action
Pharmacokinetics
Absorption:
Distribution:
Elimination:
Pharmacodynamics
Safety & Warnings
BLACK BOX WARNING
Side Effects
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.
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)
Before Using This Medicine
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.
Precautions & 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.
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
Contraindicated Interactions
- Not explicitly contraindicated with specific drugs, but caution with MAOIs due to theoretical risk of serotonin syndrome.
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.
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.
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Rationale: To establish baseline and guide initial dosing.
Timing: Prior to initiation
Rationale: To assess baseline respiratory function, especially important due to risk of respiratory depression.
Timing: Prior to initiation
Rationale: To assess baseline neurological status.
Timing: Prior to initiation
Rationale: To identify potential impairment that may require dose adjustment.
Timing: Prior to initiation, if clinically indicated
Routine Monitoring
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.
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.
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.
Frequency: Regularly
Target: Regular bowel movements
Action Threshold: Constipation requires prophylactic measures or treatment.
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
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:
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.
Pediatric Use
Safety and efficacy have not been established in pediatric patients. Use is generally not recommended.
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
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.
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
Cost & Coverage
General Drug Facts
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.