ADDICTION: MOM - Agonist & Agonistic Substitution Flashcards
Agonist Meaning
A chemical that binds to and activates a response from a postsynaptic receptor
- With reference to medication; they are designed to imitate the action of other drugs e.g. Heroin
- E.g. Methadone
Antagonist Meaning
A chemical that binds to and blocks the function of a particular substance
- Typically used in the abstinence stage of addiction recovery
- Blocks euphoric and pleasurable feelings associated with opioids - makes them less desirable
- E.g. Naltrexone
Methadone as a treatment for addiction
- Aims to reduce cravings for and withdrawal symptoms of heroin
- Has some of the same effects as heroin but does not give users the same ‘high’
- The dosage should be reduced over time (detoxification) until it is no longer needed (abstinence)
- It is recommended that methadone treatment is given alongside psychological treatment
- Doctor / nurse / pharmacist sees patients daily for the first 3 months of methadone treatment
- Supervision is required to ensure the patient does not take multiple doses at once or sell their methadone to other users
- Usually given orally as a green liquid though can be given in different forms (tablet / injection)
- Giving methadone orally helps reduce the risk associated with needle and injection use
Methadone Dosage
UK NICE guidelines recommend an initial dosage of 10-40mg daily; increased by up to 10mg daily until withdrawal and toxification symptoms are not seen (National Institute for Health and Care Excellence)
- Individual receives a maintenance dose of 60-120mg daily
Methadone: What is it?
Agonist Substitution
Used as a part of maintenance treatment
Naltrexone: What is it?
Antagonist Substitution
Oral medication - available as an implant / depot injection (only approved in USA and Russia)
Naltrexone as a treatment for addiction
- Can be offered as a therapy for opioid addiction and alcohol addiction
- It is recommended that naltrexone treatment is given alongside psychological treatment
- Can be used up to a 6 month period
- Users should be supervised to ensure they have not started drinking again
- Has been suggested by NHMRC in Australia that it could be used for problem gamblers though more research is needed
Naltrexone Use
UK NICE guidelines recommend naltrexone is given to those who are opioid free and demonstrate high motivation to sustain abstinence from drugs (National Institute for Health and Care Excellence)
Addiction: Agonist & Antagonist Substitution :)
Methadone’s Effectiveness: NICE / Van Den Brink & Haasen
Methadone & Criminality: National Treatment Agency Report
Addiction: Agonist & Antagonist Substitution :(
Comparing Methadone to buprenorphine: Marteau et al.
Effectiveness of Naltrexone: NICE / Lahti et al.
Ethical criticisms of Methadone
Side effects of Naltrexone
Addiction Agonist & Antagonist Substitution :) Methadone’s Effectiveness
NICE assessed 31 reviews of methadone’s effectiveness including 27 randomised controlled trials as a part of their guidance on its use
- Higher levels of retention for methadone users than placebo or no treatment
- Lower rates of illicit opioid use
Van Den Brink & Haasen - Meta-analysis of studies into the effectiveness of a range of treatments concluded that as long as the dosage is adequate then methadone is effective as a maintenance treatment
Addiction Agonist & Antagonist Substitution :) Methadone & Criminality
National Treatment Agency Report - Treating heroin users with methadone reduces criminality (🙂 4 society)
- Suggest that rates of offending are reduced by half when addicts are in treatment
Centre for Policy Studies Report - Claimed that drug-related offending has continued to rise despite the availability of drug treatments such as methadone
Addiction Agonist & Antagonist Substitution :( Comparing Methadone to Buprenorphine
Buprenorphine - a milder alternative to methadone
- Agonist & antagonist properties
- Activates opioid receptors to produce an opiate effect (agonist) but also blocks the euphoria (antagonist)
:) - Less risk of overdose due to ‘ceiling effect’
- After a certain amount has been taken any more will not increase the effect of the drug
Marteau et al. - Analysed data over a 5 year period; concluded that buprenorphine was 6x safer than methadone
Addiction Agonist & Antagonist Substitution :( Effectiveness of Naltrexone
A NICE research review of 17 studies shows conflicting results on the effectiveness of naltrexone on the treatment of heroin addiction
- No significant difference found between naltrexone and control treatment for retention
- When results were pooled, naltrexone was associated with reduced relapse rates
Addiction Agonist & Antagonist Substitution :( Ethical Criticisms of Methadone
- Side effects of methadone
- Methadone may interact with other drugs ( alcohol / antidepressants) to cause respiratory issues
- Danger of overdose when combined with other drugs
- ONS reports that methadone was responsible for 429 deaths in the UK
- Critics highlight that all methadone achieves is creating a new addiction
- Many individuals remain on methadone treatment for prolonged periods of time
- Without the right support users will struggle to make it to the detoxification and abstinence stage