EXAM #3: DRUGS OF ABUSE II Flashcards
What are the two most commonly abused Benzodiazepines?
1) Diazepam (Valium)
2) Alprazolam (Xanax)
What is Flunitrazepam?
Rohypnol i.e. the date rape drug
What is Flumazenil?
Benzodiazepine receptor antagonist
What Barbiturate is commonly abused?
Pentobarbital
How does the abuse of Pentobarbital compare to the Benzodiazepines?
- Not as common
- Lower margin of safety
What is the MOA of reward seen with Benzodiazepine and Barbiturate drugs?
1) Increased frequency/ duration of opening of GABA Cl- channels
2) GABA-A receptors are located on GABAnergic neurons in the VTA
Net result is dis-inhibition and activation of mesolimbic reward pathway.
What is Gamma-Hydroxybutyric Acid (GHB)?
CNS depressant that has been used as a date rape drug
What is the MOA of GHB?
Disinhibition of GABA-B receptors in the VTA
List the five common psychostimulants.
1) Cocaine
2) Amphetamine
3) Methamphetamine
4) Methylphenidate
5) MDMA
What is the trade name of Methylphenidate?
Ritalin
What is the RR of addiction with the psychostimulants?
5
What endogenous chemical do the psychostimulants mimic?
NE
What drug has the strongest psychological dependence of any drug?
Cocaine
What is cocaethylene?
Cocaine and alcohol mixed–this is the metabolite made in the liver
What is cocaethylene associated with?
- Intensification of cocaine’s euphoric effects
- Most common fatal two-drug combination
What amphetamine derivative is most commonly abused? Why?
Methamphetamine
- Can easily be burned/smoked
What are the side effects seen with methamphetamine use?
Sympathomimetic
- Mydriasis
- Tachycardia
- HTN
What is the MOA of MDMA (ecstacy)?
1) Blocks SERT transporters (5-HT)
2) Causes the release of 5-HT from presynaptic neurons
What are the long-term effects of MDMA use in regards to 5-HT?
Can cause permanent 5-HT depletion
What toxicity is associated with MDMA?
Acute hyperthermia and dehydration
What phenotype is produced by long-term abuse of psychostimulants?
Toxic psychosis that cannot be distinguished from paranoid schizophrenia
What is another name for a Psychedelic?
Hallucinogen
List the drugs categorized as Psychedelics.
1) Lysergic acid diethylamide (LSD)
2) Psilocybin
3) Ketamine
4) Phencyclidine
What is the RR of addiction seen with the Psychedelics?
1
What is the MOA of LSD and Psilocybin?
- Glutamate release
- 5-HT2A agonist
Gq–>Ip3–> increased Ca++ that causes glutamate release*
What is correlated with increased hallucinogen potency?
5-HT2 affinity
Do LSD and Psilocybin activate the mesolimbic DA pathway?
NO–thus, low risk for addiction and no withdrawal syndrome
What is the MOA of Ketamine and PCP?
NMDA antagonists that decrease activity of:
- Cortex
- Limbic system
What is the RR of opioid addiction?
4
What are the most commonly abused opioids?
1) Codeine
2) Heroin
3) Morphine
4) Oxycodone
What is the MOA of euphoria seen with opioid use?
1) Activation of mu-opioid receptors
2) Inhibition of GABAergic neurons in the VTA= disinhibition of VTA DA neurons
What is the effect of kappa-opioid receptor agonism?
Dysphoria
What is Naloxone used to treat?
Opioid receptor antagonist used to treat opioid overdose
What drug is used to treat opioid withdrawal and addiction?
Methadone
What drug is used as maintenance therapy in opioid addiction?
Naltrexone
What is the active substance found in marijuana?
THC
What is Dronabinol?
Synthetic THC
What is Dronabinol used for clinically?
Chronic pain
What is the RR of cannabinoid addiction?
2
What is the MOA of THC?
Blocks GABA-A receptors on DA neurons in the VTA
What is the mechanism of nictone addiction?
NAChR activation results in DA release in:
- Nucleus accumbens
- PFC
