Different substitution drugs Module 3

Outline Methadone Buprenorphine LAAMsubstitute medication Diamorphine Levo methadone Lofexidine Naltrexonedetox Naloxone

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

MedicationFrequencyOptimal dose recommended Route of administr Brand Names OD Risk With- drawal MethadoneEvery 24 hr mg/day Oral (syrup, tablets) Injectable Metasedin  +++ Buprenor- phine Every 24 or 48 or 72 hrs 8 – 16mg/daySublingual Subutex  + (with additional drugs) + Diamorphine2-3 times/24 hrs mg/dayInjectable Smokable NO LAAMEvery hrs mg x 3/wkOral Orlaam  +++ Levo - methadone Every 24 hr40-60mg/dayOral (syrup) Polamidon  +++

Buprenorphine Partial agonist antagonist Once stabilised, 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

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

LAAM Levo Alpha Acetyl Methadol Synthetic agonist and opiate analgesic 48–72 hours half-life, 3-4 times per week Oral doses, mg Recent problems with accumulation and cardiac arrest Not available anymore in Europe High risk of overdose and found hard to withdraw from

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

Other medications Non substitution Detoxification –Lofexidine –Naltrexone –Naloxone

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 ®

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®

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

MedicationFrequencyOptimal dose recommended Route of administration Brand Names OD Risk With- drawal Note Lofexidine Brifolex  n.a. Only available in UK NaltrexoneEvery 24, or 48 or 72 hrs 50 mg/day, or 100 mg/2 days, or 150 mg/3 days Oral Antaxone  Trexan  Celupan  Revia  Nalorex  n.a. Previous to start this treatment subjects have to be detoxified. NaloxoneIn cases of overdose Injectable Narcan  n.a. Only available for distribution in patients in Italy Codeine Oral (syrup, tablets) Injectable DHC  Remedacen  +++++Only in Germany for maintenance treatment

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