Different substitution drugs

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Module 3

• Different substitution drugs

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Outline

• Methadone
• Buprenorphine
• LAAM substitute medication
• Diamorphine
• Levo methadone
• Lofexidine
• Naltrexone detox
• Naloxone

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Methadone

• Most prevalent substitute medication 70 of
  patients respond well
• Synthetic opioid agonist
• Half life of 24-36 hours, daily dosage
• Oral dosage in liquid form (1 mg/1ml) or tablets,
  but also injectable form available
• Average dose between 60-120 mg
• Found hard to withdraw from
• High risk of overdose

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Buprenorphine

• Partial agonist antagonist
• Once stabilised, 48-56 hours half-life and 3 to 4
  dosages per week
• Strong attachment to opiate receptors
• Sublingual
• Average dose 8-12 mg
• Found relatively easy to withdraw from
• Prescribed as Subutex
• Ceiling effect

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Diamorphine

• Opioid analgesic, semi synthetic derived from
  morphine
• Illegal in most countries
• 4 hours half-life and 3 to 4 dosages per day
• Expensive form of treatment
• Found hard to withdraw from
• High risk of overdose

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LAAM

• Levo Alpha Acetyl Methadol
• Synthetic agonist and opiate analgesic
• 4872 hours half-life, 3-4 times per week
• Oral doses, 12-24 mg
• Recent problems with accumulation and cardiac
  arrest
• Not available anymore in Europe
• High risk of overdose and found hard to withdraw
  from

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Levo methadone

• Contains the active part of methadone (only levo
  and not dextro)
• Half the dosage
• Expensive
• Only prescribed in Germany Polamidon
• Double blind RCT in Hamburg

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Other medications

• Non substitution
• Detoxification
• Lofexidine
• Naltrexone
• Naloxone

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Lofexidine

• Not an opiate analgesic, inhibits the release of
  noradrenaline
• Does not eliminate withdrawal symptoms but
  reduces craving and anxiety
• Used as detoxification treatment
• Only prescribed in the UK as Britlofex

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Naltrexone

• A pure opiate antagonist or blocking agent
• Used as rapid detoxification or ultra rapid
  detoxification under anaesthesia
• 2-7 times per week
• Average dose 50mg/day or 100mg/2 days or 150mg/3
  days
• No risk of overdose and not difficult to withdraw
• Nalorex, Antaxone, Trexan, Celupan, Revia

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Naloxone

• A pure antagonist
• With very short half-life
• Used in case of overdose or to reverse coma
• Brand name Narcan

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Conclusions

• Important that there is wide range of medications
  available
• Most research available on methadone
• But other medications available and proven
  effective
• Proper assessment of patients and information re.
  different medications is vital