Drugs of Abuse Flashcards
What are some of the criteria for substance abuse disorders?
- Tolerance
- Withdrawal
- Usage of large amounts
- Normal activities are given up
- Continued use despite knowledge of problems
Withdrawal
Signs that emerge when the use of the drug is stopped which will go away when the drug is resumed
Tolerance
Decreased effect with repeated use of drug and increased need for larger doses for the same effect
What pathway is activated by all drugs of dependence?
Ventral Tegemental Area of nucleus accumbens which results in the release of dopamine
Besides lack of the agonist, what is another mechanism that can cause withdrawal?
Antagonism of the receptor that the drug normally binds to
What are the psychostimulants?
Cocaine and amphetamines
Cocaine Uses
Powerful CNS stimulant and appetite suppressant as well as a topical anesthetic.
Cocaine MOA
Inhibits the action of dopamine transporters in the presynaptic terminals - the levels of DOPA in the presynaptic cleft will increase
Amphetamines MOA
Inhibit the action of VMAT2 so DOPA cannot be placed in the vesicles leading to a high level of “free” DOPA that can reverse the DOPA transporter - increased DOPA in the presynaptic cleft
What are the effects of psychostimulants?
- Increased energy
- Decreased fatigue
- Decreased appetite
What is the fastest mechanism to feel “high” from cocaine?
IV
Where is cocaine metabolized?
Hepatic metabolism
What is the problem of combining cocaine with ethanol?
Forms cocaethylene which leads to a longer duration of action and an increased cardiotoxic effect
What is a unique risk of psychostimulant abuse?
Increased risk of rare autoimmune disorders like lupus and Stevens Johnson
Cocaine OD Signs
- Cardiac Arrhythmia
- Tachycardia
- Dilated pupils
- HTN
What is the treatment for cocaine withdrawal?
- Bromocriptine
- Lorazapam
Opioid MOA
Inhibition of GABA interneurons leading to the disinhibition of the mesolimbic DOPA system - increased DOPA in the nucleus accumbens is ultimate result
Opioid OD Signs
- Unconsciousness
- Respiratory depression
- Pulmonary edema
Is there cross tolerance to opioids?
Yes. Tolerance to one will cause tolerance to another opoid.
What is the metabolism of heroin?
Heroin -> 6-monoacetylmorphine -> morphine