Lecture 54: Prescription Drug Abuse Flashcards
What is the most commonly abused sedative?
Benzodiazepines
What are benzodiazepines?
Enhance GABA at GABA receptor to induce sedation, anti-anxiety, anti convulsant
Example: Xanax
What are types of benzodiazepines?
High potency: i. short half life Alprazolam (Xanax) Lorazepam (Ativan) Triazolam (Halcion) ii. Long half-life Clonazepam (Klonopin) Low potency i. Short half-life oxazepam (serax) temazepam (Restoril ii. Long half-life Librium
What benzos are most addictive?
High potency, short half life
Example: Xanax (alprazolam)
What is valium?
A low potency, long acting benzodiazepine
What is the MOA of benzodiazepines?
Binds to GABA-A receptor and increases overall conductance of inhibitory channels
-BZ POTENTIATE effects of GABA and do NOT activate receptors by themselves
DISINHIBITS dopamine by inhibiting interneuron in ventral tegmental area
-interneuron controls dopaminergic VTA projection, so inhibiting this guy by benzos leads to disinhibition and euphoria feeling
-nicotine and alcohol act at same channels
What else binds GABA-A receptors besides benzos?
Alcohol
Barbiturates
What are the three substances that bind to GABA-A receptors? Significance?
- Benzos
- Barbiturates
- Alcohol
The three accounts for the cross tolerance of the sedatives
-allows one to use benzos for alcohol withdrawal treatment
What happens over time when benzos are continually bound to GABA-A? Significance?
Compensatory changes in GABA-A receptor in presence of benzos renders them less efficient resulting in tolerance or less effect with the same dose
This compensatory change leads to withdrawal symptoms…when off benzos, GABA-A receptor does not function as well leading to agitation, etc.
What does BZ withdrawal look like?
Due to the fact that it is harder to activate GABA receptor so you get more monoamine release and you get 1. Anxiety 2. Agitation 3. Increased sensitivity to lights, sound 4. paresthesias, strange sensations 5. Muscle cramps 6. Myoclonic jerks 7. Insomnia 8. Dizziness 9. Seizures, delirium Similar to alcohol withdrawal but the TIME OF ONSET is different Short half-life drugs = 2-3 days Long half life drugs = 4-7 days
How long do you have to take benzos to see withdrawal results?
4 months
In what patients are benzos most indicated for?
Non drug abusing patients
Extremely useful but can lead to DEPENDENCE and WITHDRAWAL
-also has street value
When are benzos abused?
Abused by opiate patients who take benzos to AUGMENT euphoria or treat withdrawal
What are BZ used for?
- Treat anxiety
- Promote sleep
- alleviate alcohol withdrawal
- Treat seizures
- Perioperative amnesia
What are the downsides of prescribing benzodiazepine?
After four months, BZ leads to dependence
Easily sold…have street value
So DON’T PRESCRIBE shit load of benzos
What BZ has the least street value?
Oxazepam
What are examples of stimulants?
- Amphetamines
- Diet pills
Example: Phentermine - Methylphenidate
-used in California
What are sources of narcotics?
HOARDERS…parents who hoard pain meds and kids who take them
Genuine pain patients that sell their medications
Deceived and dishonest physicians
Internet
The world is AWASH in opiates
What is the ideal medication?
- stops withdrawal
- reduces craving
- blocks the high from abuse
Example: Methadone
Naltrexone
Buprenorphine
How do you treat opiate withdrawal and opiate abuse?
- methadone
- naltrexone
- Buprenorphine
Ideal medications
What is Percocet?
Contains a combination of Acetaminophen and oxycodone
So it is opioid pain reliever
What is the suburban slide?
Start with Percocet and oxycondone
Progresses heroin use
-snorting
-IV
How many 12th graders use pain relievers?
10% !!!!!!
What is pseudo-addiction?
Focus on obtaining opioids for pain relief Looks like addiction -manipulation -doctor shopping -multiple ED visits But it disappears with adequate meds
What do you need to do with methadone to prevent high associated with opiates?
Give patient enough methadone so that you have TOLERANCE and there is less euphoria
How do we deter opiate addiction?
- combining opioids with naloxone
- Physical barriers
- decrease ease with which drug can be taken
- educate the public
- make opioids less abusable
