CNS Stimulants Flashcards Preview

Pharmacology Block 3 > CNS Stimulants > Flashcards

Flashcards in CNS Stimulants Deck (16):
1

Caffeine MOA:

1. Blocks adenosine receptors (post-synaptic receptors produce IPSPs, pre-synaptic receptors inhibit glutamate release – blocks both of those inhibitor effects).
2. At higher doses, blocks PDE – results in an increase in cAMP, beneficial for asthma.

2

Caffeine effects:

CNS: increased alertness, decreased fatigue.

Peripheral: -positive chronotropic, inotropic effects.
-Dilates coronary and general systemic blood vessels but constricts cerebral blood vessels.

3

Caffeine SEs:

-Nervousness, tremors.
-High doses can stimulate medullary respiratory, vasomotor and vagal centers.
-Tolerance, withdrawal.

4

Methylphenidate MOA:

Releases NE, DA, 5HT, blocks transmitter uptake into presynaptic terminals, direct partial agonist of alpha-adrenergic receptors, MAO inhibition (at high doses).

5

Methylphenidate use:

ADHD

6

Cocaine MOA:

-Potent inhibitor of the reuptake of NE, DA, 5HT.
--Increasing DA produces feelings of euphoria, feelings of elation.
-Increasing NE causes vasoconstriction, tachycardia, increased alertness.

7

Cocaine SEs:

-Neurotoxic effects due to damage to DA systems. OD can cause seizures and/or CV effects.
-Fetal effects – low birth weight, learning and emotional problems, attachment disorder, addiction.

8

Amphetamine MOA:

-Releases NE, DA, 5HT, blocks transmitter uptake into presynaptic terminals, direct partial agonist of alpha-adrenergic receptors, MAO inhibition (at high doses).
-Metabolized and excreted unchanged.
Produces wakefulness, alertness, decreased fatigue, increased intellectual performance. Peripheral sympathomimetic effects.

9

Amphetamine uses:

Narcolepsy, ADHD

10

Amphetamine SEs:

-Insomnia, abdominal pain, anorexia.
-Toxicity: sympathomimetic effects, restlessness, dizziness, tremor.
-Abuse liability.

11

Methamphetamine MOA:

Same as amphetamines, but better CNS bioavailability.

12

Nicotine MOA:

-Agonist of nicotinic cholinergic receptors.
-Sympathetic ganglia activation results in release of epinephrine.
-Parasympathetic effects result in GI motility.
-CNS effects: increased alertness, activates DA signaling.
-Is reinforcing: activates neuronal symptoms designed to maintain behaviors that are important for survival. Each puff of a cigarette is reinforcing – reason why it is so addicting.

13

Bupropion MOA:

Seems to enhance noradrenergic and dopaminergic signaling.

14

Bupropion uses:

Reduces craving and nicotine withdrawal symptoms.

15

Verenicline MOA:

Partial agonist of CNS nicotinic receptors. Effect is twofold: activates nicotinic receptors enough to reduce craving and withdrawal, reduces the effects of the full agonist (nicotine).

16

Verenicline SEs:

Depression, constipation, headache.