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Pharmacology Test #6 > CNS Stimulants > Flashcards

Flashcards in CNS Stimulants Deck (56)
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1

Classes of CNS stimulants

1. Catecholamine releasers
2. Catecholamine reuptake blockers
3. Stimulant antidepressants
4. Methylxanthines
5. Nicotinic agents

2

Therapeutic uses of CNS sitmulants

1. ADHD
2. Narcolepsy
3. Obesity
4. Smoking cessation
5. Alcohol use disorder? (varenicline)

3

Historical prototype of catecholamine releasers

D-ephedrine

4

Catecholamine releasers

1. Amphetamine (Adderal)
2. Methamphetamine (Desoxyn)
3. Methylphenidate (Ritalin SR, Concerta, Metadate)
4. Ephedrine

5

MOA of catecholamine releasers in CNS

1. Binds to presynaptive membrane and induces release from vesicles
2. Causes release of DA from vesicles into the intracellular space in terminal
3. Blocks MAO, blocking degradation of DA and causing buildup inside cytoplasm in terminal
4. Induces reverse transport through the DAT to "release" DA into EC space

6

Reuptake blockers

1. Cocaine
2. Modafinil (Provigil)
3. Sibutramine (Meridia)

7

MOA of reuptake blockers

pure block of re-uptake, prolonging lifetime of catecholamine in the synapse and promoting its action on postsynaptic cell

8

Cocaine

abuse potential; short/intense action; NaV activity (locak anesthetic)

9

Modafinil (Provigil)

monoamine reuptake blocker; MOA unclear; less abuse potential than cocaine

10

What are bath salts?

Synthetic cathinones

11

Intoxication from synthetic cathinones

psychosis, hallucinations, agitation, tachycardia, hypertension, hyperthermia, and combative or violent behaviors

12

What is MDPV?

reuptake blocker for DAT and NET; 10-50X cocaine potency

13

Cathinones that are releasers have variable selectivity for

DAT, SERT, and NET

14

Stimulant antidepressants

1. Atomoxetine (Strattera)
2. Bupropion (Zyban, Welbutrin)

15

Atomoxetine (Strattera)

Net activity; alternative to classical stimulants; refractory ADHD, ADD, and adult ADD

16

Bupropion (Zyban, Welbutrin)

Adjunct for depression/anxiety; smoking cessation; lowers seizure threshold

17

MOA of stimulant antidepressants

mixture of antidepressants properties (block NET or SERT) plus some mild CNS activating properties via block of DA reuptake

18

When are stimulant antidepressants used

used as alternative to classical stimulants, likely in situations refractory to first-line drugs

19

How is bupropion often used?

often used as an adjunct mood enhancer along with an SSRI, has NET and DAT blocking activity

20

Methylxanthines

1. Caffeine
2. Theophylline
3. Theobromine

21

Caffeine

short-acting; diuretic; mild DA and NE stimulant

22

Theophylline

found in tea; bronchodilation, used in asthma

23

Where does caffeine act as an antagonist?

at adenosine receptors; in the brain the A2a receptor seems to be most important for the wakefullness-promoting properties of caffeine

24

Describe A2a receptors

Gs-coupled and have high expression in the area of the brain called the striatum, involved in arousal and drug addiction

25

What does specific knock out of A2a receptors in the striatum do?

eliminates the wakefullness property of caffeine

26

Nicotine's action in the DA system

1. Stimulate AP firing
2. Stimulate DA release (direct and indirect)

27

Nicotinic agents

1. Nicotine
2. Varenicline (Chantix)
3. Bupropion (Zyban)

28

Describe nicotinic acetylcholine receptors

acetylcholine-gated cation channels, where activation promotes cellular depolarization and NT release when receptors on presynaptic terminals are activated

29

Brain or neuronal nicotinic receptors have the same secondary structure as

muscle receptors

30

Brain nicotinic receptors have high affinity for

both nicotine and Ach