CNS Stimulants

Question 1

Examples of Catecholamine releasers

Answer 1

Amphetamine (Adderal)
Methamphetamine (better CNS access than amphetamine)
Methylphenidate (Ritalin)
Ephedrine (decong. + alpha nad beta ag)

Question 2

Four ways that a catacholamine releaser may work

Answer 2

1. Binds to presynaptic membrane and induces vasicle release
2. Causes DA release from vesicles into the intracellular space/terminal (VMAT)
3. Blocks MAO, blocking degradation of DA, causing buildup inside cytoplasm in terminal
4. Induces reverse transport thrrouh DAT to release DA into EC space

Question 3

Effects of Cocaine

Answer 3

Pure block of reuptake, prolonging lifetime catecholaine in the synapse, promoting action on post-synaptic cell

NaV Activity

Question 4

Important details on Modafinil

Answer 4

Monamine reuptake blocker
MOA unclear
Less abuse potetial

Question 5

What are bath salts?

Answer 5

Cathinones – naturally occuring psychostimulants. commonly abused.

• Mechanisms differ
• Intox: psychosis, agitation/violence, tachy, HTN, hyperthermia
• Schedule 1 drugs

Question 6

Effects of MDPV

Answer 6

Reuptake blocker for DAT and NET (10-50x cocaine potency)

Question 7

Important details on Atomoxetine

Answer 7

NET activity

Alternate treatment for refractory ADHD/ADD, Adult ADD

Question 8

Importnat details on buproprion

Answer 8

Mild NET and DAT blocker + nAChR antagonist

Treats depression + nicotine cessation

Question 9

Main methylxanthines

Answer 9

Caffeine
Theophylline (asthma)
Theobromine

Question 10

Theory for how caffeine works

Answer 10

Antagonist of adenosine receptor

Adensine triggers inhibition of NT release and blocks post synatptic effects

Question 11

Details on Nicotinic acetylcholine recepotrs

Answer 11

ACh gated cation channels where activation promotes cellular depolarization and neurotransmitter release hen receptors on presynaptic terminals are activated

Question 12

Effects of Nicotine in DA system

Answer 12

Stimulate AP firing

Stimulate DA release (direct and indirect)

Question 13

Difference btw Nicotine and ACh

Answer 13

ACh is endogenous. Nicotine is also very similar to local anesthetics. ACh doesn’t get protenated, doesn’t get into membrane very easily. Natural presence of actylcholinesterase to keep ACh under control.

Question 14

Difference between free base and singly protenated nicotine

Answer 14

free is a membrane crosser

singly can activate

Question 15

structural similarities with ACh and Nicotine

Answer 15

Nitrogens that are protenated at physiological pH

Hydrogen bond acceptors

Question 16

Important details on Varenacline

Answer 16

Partial agonist of nAChRs (a4b2)

effects on a3b4 nAChRs may cause periphera side effects

Question 17

Toxicities of Amphetamines

Answer 17

CV – HTN, tachy

Psych – psychosis

Question 18

Toxicities of Cocaine

Answer 18

CV - MI, stroke, arrythmias
CNS - Seizures
Respiratory Depression

Question 19

Toxicities of Nicotinics

Answer 19

GI upset

Odd dreams + suicidal ideations

Question 20

Stimulants used to treat ADHD

Answer 20

Amphetamine (Adderall)

Methylphenidate (Ritalin)

Question 21

Adcerse effects of amphetamine/methylphenidate treatment

Answer 21

Insomnia
Ab. Pian
Anorexia/Weight Loss
Growth Suppression in Kids

Question 22

Describe Narcolepsy

Answer 22

Refreshing sleep attacks
Cataplexy
REM sleep intrusions

Question 23

What is cataplexy

Answer 23

Sudden loss of muscle tone (bilateral) often associated with intense emotional engagement

Question 24

Tx for narcolepsy

Answer 24

TCAs and MAOIs
Methylphenidate, Amphetamine
Modafinil (less dependence)

Question 25

How do stimulants help with obesity

Answer 25

Appetite Suppression

can increase energy expenditure

Question 26

Problems with using CNS stimulants to control obesity

Answer 26

Wright regained after discontinuation
Exacerbated HTN
Tolerance
Abuse

Question 27

CNS stimulants used to treat obesity

Answer 27

Amphetamine
Benzphetamine
Phentermine