Drug Abuse Flashcards
1
Q
self-administration and tolerance
A
- self-administration is the end of drug-seeking behavior
- tolerance occurs when the effect of a specific dosage decreases with repeated administration, or a higher dosage is needed to produce the same effect with repeated administration
2
Q
Mechanisms for the development of tolerance
A
- dispositional tolerance – due to changes in the pharmacokinetic properties of the drug (absorption, distribution, metabolism and/or elimination)
- pharmacodynamic tolerance – due to adaptive changes in the affected systems (e.g., down-regulation of receptors or compensatory physiological changes)
- behavioral tolerance – an individual alters their behavior in order to adapt or compensate for the presence of drug
3
Q
Cross tolerance
A
If you are tolerant to one opioid, then you are tolerant to every other mu opioid receptor with the same mechanism of action
4
Q
Dependence
A
- physical dependence – is defined by the presence of a “withdrawal” or abstinence syndrome, which is characterized by signs and symptoms usually opposite to those produced by the acute administration of the drug.
- behavioral/psychological dependence – is the enduring problem with drug abuse and can occur independently of physical dependence.
-cross dependence: If you become dependent on a drug, every drug that works by same mechanism of action will alleviate the withdrawal
This is why can use a benzo to treat alcohol withdrawal and treat heroin withdrawal with methadone (agonist of the mu opioid receptor)
5
Q
Cannabinoids
THC, hashish
A
- MOA: binds to 2 receptors: CB1-Brain & CB2-Periphery
- Endogenous substance: anantamide (involved in cholesterol cascade)
- Exogenous-THC, JWH compounds
- Develop tolerance
- Mild physical dependence
- Behavioral dependence
- No overdose, withdrawal, or tx for dependence
6
Q
CNS Stimulants
(cocaine, methamphetamine, amphetamine)
Others listed: d,l-amphetamine (Benzedrine) d-amphetamine (Dexedrine) diethylpropion (Tenuate) methamphetamine (Methadrine) methylphenidate (Ritalin) phenmetrazine (Preludin) phentermine (Ionamin) caffeine cocaine ephedrine
A
- MOA: indirect acting sympathomimetics that enhance release or block reuptake
- Differential tolerance: i.e. Rapidly develop tolerance to anoretic effects, but not alertness
- Mild physical dependence: brain is depressed, changes in mood and sleep; biggest problem is depression
- Behavioral dependence
- OD is possible resulting in psychosis, angina or MI
- Tx: Give antiarrhythmic for CV, Haldol (1st gen antipsych.) for psychosis;
- Tx: for withdrawal/dependence Give SNRI for depression, or a second generation tricyclic
7
Q
Dissociative anesthetics
ketamine [special K], phenylcyclidine [PCP]
A
- MOA: glutamate receptor antagonist (glutamate receptors is major excitatory receptor)
- Develop a tolerance
- Physical dependence due to life threatening CNS excitability(seizures) when in withdrawal
- behavioral dependence
- Tx: life support for overdose
- Tx: Dilantin for withdrawal
8
Q
Hallucinogens
(serotonergic and anticholinergic drugs)
Others listed: dimethyltryptamine (DMT) harmine lysergic acid (LSD) psilocin psilocybin methylenedioxyamphetamine (MDA) methylenedioxymethampehtamine (MDMA: Ecstasy) dimethoxymethylamphetamine (DOM) mescaline (peyote)
anticholinergics:
a. atropine
b. ditran
c. scopolamine
A
MOA: Serotonergic (5HT2a) and Anticholinergic (atropine, scopolamine and angels trumpet)
- Tolerance
- No physical dependence
- Behavioral dependence
- Tx: For overdose of 5HT2A agonist give 5HT2A antagonist (risperidone, ziprasidone)
- Tx: For anticholinergic overdose give physostigmine
- No withdrawal
- No cross tolerance between scopolamine (anticholinergic) and LSD (serotonergic)
- There is cross tolerance among the same type (i.e. cross tolerance among the serotonins)
9
Q
Opiates
A
codeine dihydrocodeine heroin hydrocodone (Vicodin, Dicodid, Hycodan) hydromorphone (Dilaudid) morphine oxycodone (Percodan, Percoset, Oxycontin) oxymorphone (Numorphan)
10
Q
Synthetic Opioids
A
alphaprodine (Nisentil) anileridine (Laritine) butorphanol (Stadol) levorphanol (Levo-Dromoran) meperidine (Demerol) methadone (Dolophin) methadyl acetate (acetylmethadol) nalbuphine (Nubain) pentazocine (Talwin)
11
Q
Opioids
A
- MOA: bind to mu receptors
- Develop tolerance
- Physical dependence not life threatening (dilated pupils, vasoconstriction, cramps
- Behavioral dependence
- Tx: for overdose give narcan (short half life so readminster)
- Tx: for withdrawal give methadone (24hr 1/2life) or buprenorphine (48hr 1/2 life)
12
Q
Sedative hypnotics
Barbiturates and Benzodiazepines
A
Sedative-Hypnotics:
- Barbiturates
a. amobarbital (Amytal)
b. butabarbital (Butisol)
c. pentobarbital (Nembutal)
d. phenobarbital (Luminal)
e. secobarbital (Seconal) - Benzodiazepines
a. alprazolam (Xanax)
b. chlordiazepoxide (Librium)
c. clonazepam (Klonopin)
d. clorazepate (Tranxene)
e. diazepam (Valium)
f. flunitrazepam (Rohypnol)
g. flurazepam (Dalmane)
h. lorazepam (Ativan)
i. midazolam (Versed)
j. oxazepam (Serax)
k. temazepam (Restoril)
l. triazolam (Halcion)
13
Q
Sedative hypnotics
A
- Others
a. chloral hydrate
b. ethinamate (Valmid)
c. ethyl alcohol
d. gammahydroxybutyrate (GHB)??
e. glutethimide (Doriden)
f. meprobamate (Miltown)
g. paraldehyde
14
Q
Sedative hypnotics
A
- MOA: +allosteric modulators of GABA (Barbs, benzos, and alcohol)
- Develop Tolerance
- Physical dependence; withdrawal can be life threatening (excitatory effects)
- Behavioral dependence
- Tx: For overdose of ETOH and barbiturates provide life support
- Tx: For overdose of benzo, give an antagonist (flumazenil)
- Tx: For ETOH withdrawal, give benzo (lorazepam)
15
Q
Treatment for dependence on sedative hypnotics
A
- Tx: For dependence, give disulfram(antabuse) which blocks aldehyde dehydrogenase from breaking down acetylaldehyde=hungover/sick
- Tx: give Naltraxone (opiod antagonist) which blocks positive effects of drinking. Side effect is anhedonia (no pleasure)
- Tx: Acamprosate is an anticonvulsant that blocks the excitatory effects by neuronal dampening. Blocks interest in doing the drug and alleviates withdrawal.
