Stimulants, Anorexigenics, + Hallucinants

Question 1

Which transporter does cocaine act on and what does it go?

Answer 1

DAT - prevents reuptake into the presynaptic cleft of dopamine, serotonin, and NE

Question 2

What are the two functions of amphetamines?

Answer 2

1) compete with dopamine for uptake

2) compete w/ DA for VMAT -> dopamine released non-vesicularly

Question 3

Which drug mech is the synthetic cathinones most similar to?

Answer 3

Amphetamines - Stimulate monoamine neurotransmitter release and inhibit reuptake

Question 4

What happens if cocaine is administered systemically?

Answer 4

Increase in BP, HR, and heart contractility

coronary artery vasoconstriction

Question 5

How long is the half life for cocaine?

Answer 5

1 hr (less if smoked or IV)

Question 6

What metabolite of cocaine and for how long does it stay in your system after a binge?

Answer 6

Benzoylecogonine - 1 week

Question 7

How does the nucleus accumbens react to the repeated exposure to cocaine and amphetamine-like drugs?

Answer 7

Anticipation - sensitization causes an earlier more intense peak (can even happen with saline)

Question 8

What is the only drug labeled for obesity treatment?

Answer 8

Phentermine

Question 9

What happens in stimulant withdrawal?

Answer 9

‘Crash’ period - depression, anxiety, agitation and craving

Question 10

How long can stimulant craving last and what sets it off?

Answer 10

Craving can last for years after abstinence and can be set off by familiar people, places, or stressful situations (PTSD-like)

Question 11

What happens after the crash period of stimulant withdrawal?

Answer 11

Intermediate period - fatigue, loss of energy and affect

Question 12

What does amphetamines do to heart rate and why?

Answer 12

Induces a bradycardial reflex because it is increases blood pressure

Question 13

How is cocaine metabolized?

Answer 13

Ester hydrolysis

Question 14

How are amphetamines excreted?

Answer 14

Renal - unchanged

Question 15

What is used to treat ADHD?

Answer 15

Amphetamines and methylphenidate

Question 16

What is modafinil used for?

Answer 16

1) Narcolepsy
2) Adjunct for OSA
3) Shift work sleep disorder

Question 17

Which patient population should not take modafinil?

Answer 17

Cardiovascular problems - MI, unstable angina, LVH

Question 18

Modafinil adverse reactions

Answer 18

Headache
Nausea
Hypersensitivity
Drug interactions

Question 19

Caffeine use

Answer 19

idiopathic apnea of prematurity

Acute resp depression (not first line)

Question 20

What mech does caffeine have at high concentrations?

Answer 20

Inhibits phosphodiesterase

Question 21

Does caffeine have substance dependence?

Answer 21

No

Question 22

Effects of nicotine

Answer 22

Arousal 
Relaxation
Attention
Reaction time
Enhances mood

Question 23

Peripheral effects of nicotine

Answer 23

Increases BP
Increase HR
Vasoconstriction
Increases cardiac output

Question 24

What type of learned behavior is precipitated in nicotine replacement therapy?

Answer 24

Positive reinforcement to curtail tobacco use

Question 25

What are the three major groups of hallucinogens?

Answer 25

1) 5HT-2A partial agonists 2) Muscarinic antagonists 3) Glutamate antagonists

Question 26

In which cells are 5HT-2A receptors found mostly?

Answer 26

Cortical pyramidal cells (prefrontal cortex)

Question 27

Which drugs bind at the 5HT-2A receptor?

Answer 27

LSD and MDMA

Question 28

What are some side effects of 5HT-2A partial agonists?

Answer 28

Flashbacks (~4%) and bad trips (anxiety, depression and paranoia)

Question 29

What receptor does PCP act on? What else acts here?

Answer 29

It is an NMDA antagonist. Ketamine also acts here

Question 30

Peripheral effects of LSD and other hallucinogens?

Answer 30

Mydriasis Increased BP Increased HR

Question 31

What happens to serotonergic neurons exposed to MDMA?

Answer 31

Degeneration

Question 32

Adverse effects of PCP

Answer 32

``` Paranoia Hostility (combative behavior) Increased BP, HR, sweating High risk of addiction Numb and loss of pain sensation ```

Question 33

What population is the synthetic cannabinoid used in?

Answer 33

Dronabinol is used to help anorexia in AIDs patients | Nausea in chemotherapy patients

Question 34

What receptors does THC act on and how?

Answer 34

Agonist at CB1 and CB2 at the presynaptic axon

Question 35

How does CB1 work?

Answer 35

Gi/o coupled G protein inhibits adenylyl cyclase

Question 36

What causes the large volume of THC distribution?

Answer 36

HIgh lipid solubility

Question 37

What toxicities are caused by whippets?

Answer 37

``` Bone marrow suppressoin Chemical pneumonitis, coughing, and wheezing renal tubular acidosis arrhythmias cerebellar degeneration ```