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Rapid dev. Of tolerance

  • Tolerance dev. To the euphoric and analgetsic effects as well

  • Need more and more in order to get that feeling (change in areas in brain where they need it)

  • Withdrawal is extremely uncomfy (flu-like symptoms) 

  • avoid the withdrawl and need the drug to fix it

  • Gives med. Like clonidine to help w/withdrawl

Synthetic opiiods (fentanyl) were the leading cause

Potency- amount of drug needed to produce the effect

  • 100x than morphine

  • 50x than heroin

Efficacy-  the ability of a pharmacsutical drug to produce a desired theraputic effec ts when administered under controlled condirions


Affinity: Ability of drug to to bind to the receptor 


We have endogenous opioids, small pain killing peptides our bodies naturally produce

  • Endorphins

  • Enkephalins

  • Dynorphins

    • Bind and activate the receptor

    • Distributed to brain, spinal cord


Research 

  • Increase in dopamine

  • Gives feeling of pleasure 


Acute withdrawal syndrome

  • Gastrointestinal distress

  • Insomnia

  • Thermoregulation disturbances 

  • Dysphoria

  • Restlessness

  • Anxiety

  • Joint and muscle pain/cramps


Post acute withdrawal syndrome (PAWS)

  • Mood disturbances 

  • Anxiety

  • Depression

  • Sleep problems

  • Fatigue  








COWS

  • Clinical opiate withdrawal scale



  • Where are they in terms of withdrawal? 

  • 11 item scale

  • Used inpatient & outpatient

  • Rate symptoms of opiate withdrawal & monitor over time (know stage & severity)

  • disturb medical treatment if you give suboxone

  • score helps determine stage and severity inform use of suboxone 


Detoxification

  • Drug free is first step

  • Being dependent

  • Methadone & bupropion treatment is a better method for maintaining abstinence from heroin

  • CBT, vocational or employment counseling & support groups 


Med-assisted treatments for OUD (MATs)

Use FDA approved meds with counseling & behavioral thewrap\jes to help w/substance use disorder

  • 20% treated w/ buprenorphine,naltrexone and methadone

  • They are effective in treating OUDs

Harm Reduction

  • Needle distribution programs that distribute sterile needles 

  • MAT’s substitution therapies that substitute illegal heroin with legal, non injection methadone or other prescribed opioids 

  • Naloxone programs that provide training to use an antidote to opioids to reverse an overdose therby preventing brain injury

Agonist -  replacement or substitution - binds the receptor and produces biological response 

Partial agonists- bind to receptors but elicit partial functional responses regardless of drug administered

Antagonist- binds to receptors but produce no functional response but prevent agionist from getting to the receptors 






Methadone 

  • Synthetic agonist: binds Mu opioid receptors ( turns on receptors)

  • For heroin addicts., less addictive 

  • Long acting. Replacement med to opiate addict. (heroin needed every hour)

  • Keeps cravings & withdrawal under control

  • IV use will cross blood brain barrier quickly and will produce euphoria

Issues:

  • Takes practice (need good doctor for right dose)

  • Absorbed into fat tissue

  • Change dose until finding right one

  • Must go somewhere every morning to get medication, very inconvenient

  • You can overdose but its full agonist

  • Very high dose can produce euphoria

  • high/similar effect to heroin when mixed w/benzo

  • Cardiac disturbances. Tachycardia can cause heart attacks.

  • Takes a long time to dose down and stop (even years, or entire lives)

  • Copayments are sometimes very high 

Benefits

  • Decreases crime

  • Decreases Relapse 

  • Increases functioning

  • Maintains job

  • Decrease HIV and hep

Suboxone

  • Partial agonist: buprenorphine. + antagonist (naloxone)

  • delivers very diminished opioid doses to the patient who is addicted to a stronger opioid

  • Partly turns on the receptor


No liquid handcuffs (clinic every morning)


Naltrexone

Antagonist

  • Used for AUD and OUD

  • Blockseuphirc and seditaive effects of opioids

  • No potential for abuse

  • Prevents feeling or getting high

  • If stopped and patient usesd again, increase in ocer dose




Why MATs?

  • Dec. in # of overdoses from heroin 

Resistance to MATs

Lack of understanding- belief that MAT involves “substituting one drug for another”

Diverting the meds/ abuse- 

Cost 


In criminal justice settings

  • Resistance to helping people w/OUD

  • Get arrested and go through withdrawal and need them to prevent it

  • Loose rights in prison and they aren't able to access the meds

  • People released get a higher risk of overdose or death

    • Leading cause is an overdose 

  • Getting meds has less lower risk


Supervised injection/consumption site

  • Facility cannot be arrested, bring own drugs no fear of being arrested 

  • Whatever they need to shoot

  • Nurses there to save them if overdose 

  • Patients bring their own drugs, they arent given them, they are protected 

Supplies

  • Syringes

  • Turnicates

  • Sterile cookers

  • Don't use the IVs to give drugs

  • Pipes

Secure environment

  • Open booths keep clients in view of clinicians

  • Legal

  • Exempt from protection