Pentazocine and naloxone is available by the brand name of Talwin-NX. It is a combination of Pentazocine which is an opioid analgesic and naloxone. Naloxone is used to reduce the addiction potential of pentazocine.

Indications of Pentazocine and Naloxone (Talwin-NX):

• Pain management:

  • It is used to treat severe pain that needs an opioid analgesic but cannot be adequately managed with other methods.
  • Limitations of use: Reserve for use in patients with alternative treatment alternatives (such as nonopioid analgesics) that are ineffective, poorly tolerated, or would otherwise fall short of managing pain adequately.

Pentazocine and naloxone (Talwin-NX) dose in Adults

Pentazocine and naloxone (Talwin-NX) dose in Pain management:

• Every three to four hours, take one tablet (pentazocine 50 mg/naloxone 0.5 mg); if necessary, increase to two tablets (pentazocine 100 mg/naloxone 1 mg).
• The maximum daily dose is 12 tablets (600 mg of pentazocine and 6 mg of naloxone).

• Discontinuation of therapy:

  • Gradual tapering should be done when discontinuing chronic opioid therapy..
  • Proposed schedules range from slow (eg, 10% reductions per week) to rapid (eg, 25% to 50% reduction every few days).
  • Tapering schedules should be individualized to minimize opioid withdrawal while considering patient-specific goals and concerns as well as the pharmacokinetics of the opioid being tapered.
  • Long term therapy for years needs slower tapering while patients experiencing severe adverse reactions need more rapid tapering.
  • Withdrawal symptoms should be treated with slow tapering that includes adjustments including lengthening the time between dose reductions, reducing daily dose reduction, pausing the taper and restarting it when the patient is ready,
  • During the tapering, non-opioids should be used to control pain and withdrawal symptoms.

Pentazocine and naloxone (Talwin-NX) dose in Children

Refer to adults dosing.

Pregnancy Risk Category: C

• [US Boxed Warning]
• Neonatal opioid withdrawal syndrome, which can be lethal if not adequately managed, can result from long-term opioid medication.
• The patient should be informed about the possibility of neonatal opioid withdrawal syndrome (Neonatal Opioid Withdrawal Syndrome) and the best course of treatment if long-term opioid therapy is necessary during pregnancy.
• For more information, contact individual agents.

Use of pentazocine or naloxone during breastfeeding

• Breast milk contains pentazocine.
• It is not known if breast milk secretes Naloxone.
• The decision of whether to continue breastfeeding or quit breastfeeding during therapy is based on the risks and benefits to the infant as well as the benefits to the mother, according to the manufacturer's instructions.
• Contact individual agentsPentazocineand naloxone)

Dose adjustment in renal disease:

• The manufacturer's labelling does not mention dosage modifications. Take care when using.
   
• Based on the pentazocine component, several practitioners have used the following recommendations:

  • GFR ≥50 mL/minute:

    • No dosage adjustment necessary

  • GFR 10 to 50 mL/minute:

    • Administer 75% of normal dose

  • GFR <10 mL/minute:

    • Administer 50% of normal dose

Dose adjustment in liver disease:

The manufacturer's labelling does not mention dosage modifications. Take care when using.

Side effects of Pentazocine and Naloxone (Talwin-NX):

• Cardiovascular:

  • Circulatory Depression
  • Facial Edema
  • Flushing
  • Hypertension
  • Hypotension
  • Syncope
  • Tachycardia

• Central Nervous System:

  • Central Nervous System Depression
  • Chills
  • Confusion
  • Disorientation
  • Dizziness
  • Drowsiness
  • Drug Dependence
  • Euphoria
  • Excitement
  • Hallucination
  • Headache
  • Increased Intracranial Pressure
  • Insomnia
  • Irritability
  • Nightmares
  • Paresthesia
  • Sedation
  • Seizure
  • Withdrawal Syndrome

• Dermatologic:

  • Dermatitis
  • Diaphoresis
  • Erythema Multiforme
  • Pruritus
  • Skin Rash
  • Stevens-Johnson Syndrome
  • Toxic Epidermal Necrolysis
  • Urticaria

• Gastrointestinal:

  • Abdominal Distress
  • Anorexia
  • Biliary Tract Spasm
  • Constipation
  • Diarrhea
  • Nausea
  • Vomiting
  • Xerostomia

• Genitourinary:

  • Urinary Retention

• Hematologic & Oncologic:

  • Agranulocytosis (Rare)
  • Decreased White Blood Cell Count
  • Eosinophilia

• Hypersensitivity:

  • Anaphylaxis

• Neuromuscular & Skeletal:

  • Tremor
  • Weakness

• Ophthalmic:

  • Blurred Vision
  • Miosis

• Otic:

  • Tinnitus

• Respiratory:

  • Respiratory Depression (Rare)

Contraindications to Pentazocine and naloxone (Talwin-NX):

• Hypersensitivity to pentazocine, Naloxone or any other component of the formulation (eg, anaphylaxis).
• GI obstruction/ paralytic ileus
• Bronchitis, acute or severe
• Grave respiratory depression.

Warnings and precautions

• Cardiovascular effects

  • Because it can raise systemic and/or pulmonary arterial pressures and systemic resistance, pentazocine shouldn't be administered in MI.

• CNS effects

  • CNS depression can cause impairments in mental and physical abilities. It is important to warn patients not to drive or operate machinery.
  • Some patients have experienced confusion, disorientation and visual hallucinations. However, it usually resolves in a matter of hours.

• Constipation

  • With post-myocardial damage or unstable angina, constipation can happen. Consequently, preventative measures like increased fibre and stool softener are advised.

• Respiratory depression [US Boxed Warning]

  • Respiratory depression is a serious condition that requires close monitoring. Carbon dioxide retention can increase the sedating effects associated with opioids.

• Conditions abdominales:

  • Patients with acute abdominal conditions may not be diagnosed or treated appropriately.

• Insufficiency of the adrenal glands:

  • Patients with adrenal insufficiency (Addison disease) should be cautious.
  • Long-term therapy can help with mood disorder, osteoporosis and sexual dysfunction caused by secondary hypogonadism.

• Insufficiency of the biliary tract:

  • Patients with biliary dysfunction (including acute pancreatitis) should be cautious. It may cause constriction to the sphincter.

• Bowel disease

  • Patients with inflammatory or obstructional bowel disease should be cautious.

• CNS depression/coma:

  • It should be avoided in patients suffering from CNS or come depression.

• Delirium tremens:

  • Patients with delirium-tremens should be taken with caution

• Use of ethanol:

  • Be aware that there is a greater risk of CNS depressant side effects.

• Head trauma

  • It should not be used if there is a head injury, intracranial lesion, or elevated intracranial Pressure.

• Hepatic impairment

  • Patients with hepatic impairment should be cautious.

• Mental health conditions

  • Due to the increased risk of opioid abuse disorder, regular monitoring is required for depressive, anxiety, and post-traumatic stress disorders (OPD).

• Obesity:

  • Patients who are severely obese should be taken with caution

• Porphyria

  • Patients with a history porphyria should be cautious as it may worsen the condition.

• Prostatic hyperplasia/urinary restriction:

  • Patients with prostatic hyperplasia or urinary stricture should be cautious.

• Psychosis:

  • Patients with toxic psychosis should be treated with caution.

• Renal impairment

  • Patients with impaired renal function should be cautious.

• Respiratory disease

  • It is not recommended to be used in COPD, cor pulmonale, patients with reduced respiratory reserve, hypoxia or hypercapnia, as well as those who have preexisting respiratory depression.
  • These patients may prefer nonopioid analgesics.

• Seizures:

  • Preexisting seizures may be exacerbated or caused by therapy. Therefore, it is important to use it with caution.

• Sleep-disordered breathing

  • This should be avoided in severe or moderate sleep-disordered sleeping and used sparingly with other risk factors, such as obesity and heart failure.

• Thyroid dysfunction:

  • Patients with thyroid dysfunction should be cautious.

Pentazocine and naloxone: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Monitoring parameters:

• BP
• Mental and respiratory health
• Bowel function
• Pain relief
• Signs and symptoms of abuse, misuse, or addiction
• Signs and symptoms of hypogonadism/hypoadrenalism

Alternate suggestions:

• Before treatment, and once per year, urine drug testing

• Chronic pain (end-of life or palliative care), active cancer treatment, sickle cells disease or medication-assisted opioid use disorder treatment):

  • Within one month of beginning treatment, evaluate the risks and benefits of opioid therapy. 
  • You should evaluate the risks and benefits of opioid therapy every three months, or more often if there is a higher risk of overdose.
• Clinicians should review the state prescription drug monitoring program data (PDMP) before initiation and every so often during therapy.

How to Administer Pentazocine and naloxone (Talwin-NX):

See Pentazocine (Talwin)

Mechanism of action of Pentazocine and naloxone:

Pentazocine:

• In the Brain, it functions as an agonist for the kappa and a partial agonist for the mu opiate receptors.
• It modifies how pain is perceived, how the body reacts to pain, and it blocks the ascending pain pathways.
• Similar to opioids, this causes analgesia, respiratory depression, and drowsiness.

Naloxone:

• By vying for opioids and displacing them at opioid receptor sites in the central nervous system (CNS), it functions as a pure opioid antagonist.
• Due to its weak systemic absorption, it has little pharmacologic effect following oral administration (low dose: 0.25 mg).
• Pentazocine's effects are inhibited when it is taken parenterally.

See individual agents.

Pentazocine and naloxone Brand Names (International):

Talwin-NX

Pentazocine and naloxone Brand Names in Pakistan:

No Brands Available in Pakistan.