Exam 3 - Amphetamines and Cocaine

Question 1

What accounted for the rise and fall of meth use?

Answer 1

its changes in potency

Question 2

What are amphetamine and cocaine?

Answer 2

stimulants

Question 3

What are amphetamines structurally similar to?

Answer 3

dopamine

Question 4

Khat/Cathinone

Answer 4

• active components are cathinone and cathine
• stimulant properties similar to amphetamine and cocaine

Question 5

Bath salts

Answer 5

• synthetic cathinone
• 10x more powerful than cocaine
• triggers release of dopamine

Question 6

MDPV

Answer 6

• main ingredient in bath salts, detected in urine of users
• first synthesized in 1968 to counteract chronic fatigue

Question 7

What are the desired effects of bath salts?

Answer 7

• euphoric high with a rush
• appetite suppression
• study aid

Question 8

What are the adverse effects of bath salts?

Answer 8

• combative
• hallucinations
• hyperthermia
• anxious/paranoia

Question 9

Ephedrine

Answer 9

• comes from ephedra
• only use today is anesthesiology to increase BP
• can be toxic/fatal when combined with other stimulants
• pseudoephedrine used in cough and cold medicines

Question 10

Basic pharmacology of amphetamines

Answer 10

• absorption from GI tract is slow, I.V. is rapid
• methamphetamine is more potent than amphetamine
• amphet and metham are metabolized by liver at slow rate

Question 11

What are amphetamines mechanism of action?

Answer 11

• release DA independently of an action potential, and also releases NE and DA
• block reuptake of NE and DA
• addiction comes from the release of DA in the mesolimbic pathway

Question 12

What are the behavioral effects of amphetamines?

Answer 12

• confident
• highly alert/don’t sleep
• low appetite
• improves performance on simple repetitive tasks

Question 13

What are the psychological effects of amphetamines?

Answer 13

• sympathomimetic agents - mimic actions of epinephrine
  
  • sympathetic nervous system (increase HR, BP, RR, dilate pupils)

Question 14

What are the therapeutic uses of amphetamines?

Answer 14

• narcolepsy
• obesity - suppresses appetite
• ADHD - causes release of DA in areas that control attention

Question 15

Tolerance/Dependence of amphetamines

Answer 15

• reverse tolerance of motor effects
• withdrawal symptoms include: increased appetite/weight gain, decreased energy, increased need for sleep (amphets block REM)

Question 16

Amphetamine psychosis

Answer 16

• psychotic reaction occurring in substantial number of high dose users
• resembles paranoid schizophrenia (hallucinations, behavioral disorganization, paranoia, formication - picking at skin)

Question 17

Neurotoxicity of amphetamines

Answer 17

• neuronal death of both dopaminergic and serotonergic neurons in animal models

Question 18

Cocaine

Answer 18

stimulant that comes from the coca plant

Question 19

What were the leaves of E. coca used for historically? When was the active alkaloid isolated? What was this alkaloid named?

Answer 19

• increase endurance/stamina, promote sense of well being, induce euphoria
• 1850’s
• cocaine

Question 20

Coca paste was combined with hydrochloric acid to form:

Answer 20

less potent, water soluble salt cocaine hydrochloride

Question 21

Who typically uses cocaine? Why do they use it?

Answer 21

• young males that are typically dependent on other drugs
• tend to have coexisting psychopathology that they are self-medicating for

Question 22

What are the two ways that cocaine is absorbed?

Answer 22

• snorted, slow absorption, low concentration in blood
• inhalation and IV, rapid absorption, high concentration in blood

Question 23

Distribution of cocaine

Answer 23

• penetrates brain rapidly, initial brain concentrations exceed blood concentrations
• freely crosses the placental barrier

Question 24

Metabolism and excretion of cocaine

Answer 24

• biological half-life of 20-90 minutes
• major metabolite is benzoylecgonine, makes cocaethylene

Question 25

What does cocaine do?

Answer 25

- potent local anesthetic - vasoconstrictor

Question 26

What are the adverse effects of cocaine

Answer 26

- convulsions/seizures - hemorrhagic stroke (vasocontrictor and also a stimulant) - cardiac arrhythmias

Question 27

What are some consequences of use of cocaine during pregnancy?

Answer 27

- everything that can happen to mom can happen to baby - premature birth - respiratory distress - cerebral infarctions - seizures

Question 28

What are the 3 phases of withdrawal of cocaine?

Answer 28

- crash (1-14 days): intense craving, exhaustion, agitation - withdrawal (1-10 weeks): intense craving, mod to severe depression, inability to feel normal pleasure - extinction (months to years): cravings occurs by exposure to environment cues

Question 29

Mechanism of action of cocaine

Answer 29

- blocks reuptake of DA, NE and 5-HT

Question 30

Baseline DA release of reinforcing effects of psychostimulants

Answer 30

- b/c cocaine doesn't cause release of DA, it depends on the baseline levels of DA - body begins to compensate by releasing less and less DA

Question 31

Neurotoxicity of cocaine

Answer 31

- damage axon terminals: change memory function - predisposition to early onset dementia/parkinson's

Question 32

What are some medicinal treatments for cocaine dependency?

Answer 32

- dopaminergic agonists to treat withdrawal symptoms, relapse, and craving (disulfiram, antabuse) - antidepressants (tricyclic like despiramine) - Gamma-vinyl-GABA for anti-craving effects (inhibit endorphin areas that become excited w/ use)

Question 33

What are some new approaches to cocaine dependency treatment?

Answer 33

- dopamine reuptake inhibitors to reduce craving and relapse - cocaine vaccine: antibody that will bind to and inactivate cocaine, slow entry to brain and inhibit euphoria - can be overridden by taking more cocaine