Buprenorphine

1. Introduction

Buprenorphine, marketed under brand names such as Subutex, Suboxone, and Butrans, is a partial opioid agonist-antagonist. It is primarily used in the management of opioid dependence and moderate to severe pain. Its unique pharmacological profile allows it to reduce withdrawal symptoms in opioid dependence while minimising the risk of misuse.

2. Indications

  • Approved Indications:
    • Management of moderate to severe pain (transdermal patches, injections).
    • Opioid dependence treatment (sublingual tablets, films, or implants).
  • Off-Label Uses:
    • Chronic pain in patients intolerant to other opioids.

3. Dosage

  • For Opioid Dependence:
    • Sublingual Tablets/Films: Initial dose: 2–4 mg once daily, titrated to a maintenance dose of 8–16 mg daily. Maximum: 24 mg/day.
  • For Pain Management:
    • Transdermal Patches: Apply one patch every 7 days. Dosages range from 5 mcg/hour to 20 mcg/hour.
    • Injection: 0.3 mg intramuscularly (IM) or intravenously (IV) every 6–8 hours as needed.

Dosage should be individualised based on the condition, severity of symptoms, and patient response.

4. Administration

  • Sublingual Tablets/Films: Place under the tongue and allow to dissolve completely. Do not chew or swallow.
  • Transdermal Patches: Apply to a clean, dry, hairless area of skin on the upper torso or outer arm. Rotate application sites to avoid skin irritation.
  • Injection: Administer IM or IV as directed by a healthcare provider.

5. Forms Available

  • Sublingual Tablets: 2 mg, 8 mg.
  • Sublingual Films: 2 mg/0.5 mg, 8 mg/2 mg (buprenorphine/naloxone).
  • Transdermal Patches: 5 mcg/hour, 10 mcg/hour, 20 mcg/hour.
  • Injectable Solution: 0.3 mg/mL.

6. Side Effects

6.1. Common Side Effects

  • Nausea.
  • Constipation.
  • Drowsiness.
  • Headache.

6.2. Less Common Side Effects

  • Sweating.
  • Dizziness.
  • Dry mouth.

6.3. Rare but Serious Side Effects

  • Respiratory depression (especially with misuse or in combination with other CNS depressants).
  • Hypotension.
  • Hepatotoxicity.

7. Warnings

  • Risk of life-threatening respiratory depression, particularly during initiation or dose escalation.
  • Avoid in patients with severe respiratory impairment, acute asthma, or gastrointestinal obstruction.
  • Prolonged use may lead to dependence, although the risk is lower than with full opioid agonists.

8. Precautions

  • Use with caution in patients with a history of liver disease, as it is metabolised by the liver.
  • Avoid alcohol or sedative drugs, as they can enhance the risk of respiratory depression.
  • Monitor for signs of misuse, abuse, or diversion in opioid dependence treatment.

9. Interactions

  • Drug-Drug Interactions:
    • Benzodiazepines and other CNS depressants: Increased risk of respiratory depression.
    • CYP3A4 inhibitors (e.g., ketoconazole, erythromycin): Increased buprenorphine levels.
    • CYP3A4 inducers (e.g., rifampin, carbamazepine): Reduced buprenorphine efficacy.
  • Drug-Food Interactions:
    • Avoid alcohol consumption during treatment.

10. Monitoring Parameters

  • Signs of respiratory depression, particularly during initiation or dose escalation.
  • Liver function tests periodically in long-term use.
  • Monitor for signs of misuse or dependence.

11. Use in Children

  • Not recommended for use in children under 16 years for opioid dependence.
  • Use in pain management may be considered in select cases with weight-adjusted dosing.

12. Use in Pregnancy

  • Category C: Limited data in pregnancy; use only if the potential benefit outweighs the risk.
  • Often preferred over methadone for opioid dependence treatment in pregnancy due to lower neonatal abstinence syndrome (NAS) severity.

13. Use in Elderly

  • Use with caution, as elderly patients may be more sensitive to the effects, including respiratory depression and hypotension.

14. Use in Kidney Disease

  • No dose adjustment required in mild-to-moderate renal impairment.
  • Use cautiously in severe renal impairment.

15. Use in Liver Disease

  • Use with caution in moderate to severe hepatic impairment, as buprenorphine metabolism may be affected.

16. Patient Counselling Points

  • Explain the importance of proper administration (e.g., dissolve sublingual tablets fully, apply patches to intact skin).
  • Advise patients to avoid alcohol or sedative medications during treatment.
  • Warn about potential drowsiness and to avoid driving or operating heavy machinery until they know how the medication affects them.
  • Inform patients about the risk of withdrawal symptoms if the medication is stopped abruptly.
  • Encourage patients to keep regular follow-up appointments for monitoring.

17. Table of Brand Names, Manufacturers, and Prices

Brand NameManufacturerPrice (USD)
SubutexIndivior$200–300 (30 tablets, 8 mg)
SuboxoneIndivior$250–400 (30 films, 8 mg/2 mg)
ButransPurdue Pharma$250–350 (4 patches, 10 mcg/hour)
Generic OptionsVarious$100–200 (30 tablets, 8 mg)

18. FAQs (15 Questions)

  1. What is buprenorphine used for?
    Buprenorphine is used to treat opioid dependence and manage moderate to severe pain.
  2. How does buprenorphine work?
    It is a partial opioid agonist, reducing withdrawal symptoms and cravings in opioid dependence while minimising misuse risk.
  3. Is buprenorphine addictive?
    While it has a lower risk of addiction compared to full opioid agonists, misuse and dependence are still possible.
  4. How should buprenorphine sublingual tablets be taken?
    Place the tablet under the tongue and let it dissolve completely; do not chew or swallow it.
  5. Can buprenorphine cause respiratory depression?
    Yes, especially if combined with other CNS depressants like benzodiazepines or alcohol.
  6. Can pregnant women use buprenorphine?
    Yes, it may be used in opioid dependence treatment during pregnancy under medical supervision.
  7. What are the common side effects of buprenorphine?
    Nausea, constipation, drowsiness, and headache.
  8. How long does a buprenorphine patch last?
    A single patch provides continuous pain relief for 7 days.
  9. Can I drink alcohol while taking buprenorphine?
    No, alcohol increases the risk of respiratory depression and other side effects.
  10. Can children use buprenorphine?
    It is not recommended for opioid dependence treatment in children under 16 years.
  11. Does buprenorphine interact with other medications?
    Yes, especially with CNS depressants and CYP3A4 inhibitors or inducers.
  12. How should buprenorphine be stored?
    Store at room temperature, away from moisture and heat.
  13. What happens if I miss a dose?
    Take the missed dose as soon as you remember, but do not double the dose.
  14. How does buprenorphine compare to methadone?
    Buprenorphine has a lower risk of misuse and respiratory depression compared to methadone.
  15. Can buprenorphine be used long-term?
    Yes, it can be used long-term under medical supervision for opioid dependence or chronic pain management.