Lecture 44: Stimulants Flashcards Preview

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Flashcards in Lecture 44: Stimulants Deck (34):
1

On and off label indications for stimulants (6)

Exogenous obesity, ADHD, narcolepsy, fatigue, cessation of tobacco use, local anesthesia

2

Broadly, cocaine and amphetamine do what?

Increase synaptic levels of DA, NE, and 5HT

3

What is the mechanism of cocaine?

Inhibits DA reuptake

4

What is the dual effect of amphetamines? How does this increase DA in the synapse?

Compete w/ DA for reuptake and for vesicular packaging; leads to nonvesicular release of DA

5

What is the only FDA-approved use of cocaine?

Topical anesthetic

6

What are the peripheral effects of cocaine and the underlying mechanism

Potent vasoconstrictor because it increases NE at sympathetic synapses

7

Cocaine is eliminated where? (2) One important metabolite is useful for what function?

Plasma and hepatic esterases; metabolite can be detected in urine for up to a week after binge use

8

Name the four key amphetamines in order of increasing half-lives. Where are they eliminated?

Methylphenidate, amphetamine, methamphetamine, phentermine; kidney

9

Broadly, amphetamines are prescribe for two things...

ADHD and narcolepsy

10

Which two amphetamine can also be prescribed for exogenous obesity?

Methamphetamine and phentermine

11

Off-label, methylphenidate has been used...

To treat depression in medically ill older adults

12

The D amphetamine isomer is active where? What about L? Relevance for methamphetamine? How about amphetamine?

D = CNS, L = ANS; D-meth = prescribed form, L-meth = decongestant; amph = mix (75% D)

13

What are the cardio effects of amphetamines as they compare to cocaine?

Increase BP but variable effect on HR (can even see reflex bradycardia)

14

Describe two phases of amphetamine withdrawal

"Crash" (anxiety, craving) then withdrawal (fatigue)

15

Modafinil is prescribed for (3)...off label (2)...

Narcolepsy, shift disorder, sleep apnea; ADHD, fatigue in MS

16

How is Modafinil similar and different compared to the amphetamines?

Stimulant, but structurally unrelated (mechanism not well understood), low risk of addiction

17

Caffeine is a what at what receptor?

Adenosine receptor antagonist

18

Nicotine is a what at what receptor?

Full agnoist at nAChRs

19

CNS effects

Arousal, relaxation, enhanced mood, attention

20

PNS effects

Increase BP, HR, CO, vasoconstriction

21

At very high doses, what does nicotine cause?

Hypotension and bradycardia

22

What are synthetic cathinones derived from? Where are they found (on the streets) and what is their mechanism similar to?

Khat; bath salts; amphetamines

23

Hallucinogens do what at what receptor? (2 categories, name relevant drugs)

LSD, MDMA: partial agonist at 5HT2A receptor; PCP: NMDA glutamate receptor antagonist

24

Are there tolerance or withdrawal symptoms for LSD/MDMA?

Tolerance, yes; withdrawal, no

25

PCP comes with a high risk of...

Addiction

26

Besides hallucinations, PCP intoxication can cause...What are some peripheral symptoms?

Hostile behavior, numbness, nystagmus; tachycardia, hypertension, sweating

27

Toxic effects of PCP present as...(3)

Anesthesia, coma, cataonia

28

Cannabinoids are all what at what receptors? These are normally activated how?

Agonists at cannabinoid receptors (mainly CB1); endocannabinoids are synthesized from cell bodies and diffuse retrograde onto afferent nerve terminals

29

What is the most potent cannbindoid in marijuana?

THC

30

Why can cannabinoids be detected in the urine for other a month?

Despite quick hepatoic metabolism, very lipid soluble and store in tissues

31

Are there tolerance or withdrawal symptoms for marijuana?

Tolerance yes, withdrawal has been difficult to observe

32

What is dronabinol prescribed for?

Anorexia in AIDS and antiemetic for patients who are undergoing chemotherapy

33

Acutely, inhalants can cause? (4)

Euphoria, ataxia, hallucinations, seizures

34

What are some of the toxicities of inhalants? (2 CNS and 4 affected organs)

Cerebellar degeneration, cognitive decline, kidney/heart/lung and bone marrow malfunction

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