Xanthines, Nootropics and NERI

Question 1

Name the Xanthines

Answer 1

Theobromine, Theophylline, Caffeine

Question 2

Uses of Xanthines

Answer 2

Cardio Stimulation in CHF, Paroxysmal dyspnea assoc w/left hrt failure (relaxes hrt vessels)
Bronchial asthma w/ergot for migraine (constricts cerebral
vessels)

Question 3

Mechanism of Xanthines

Answer 3

Translocates Ca++ from sarc reticulum, Inhibits phosphodiesterase (elevates cAMP), adenosine receptor antagonist (wakefulness)
Relaxes smooth muscle in bronchioles

Question 4

CNS affects/tolerance of Xanthines

Answer 4

Stimulates cortex – clear thought flow, less fatigue, better dexterity, better rxn time
Stimulates medulla resp center – inc resp
Stimulates SC – hyperreflexia

Tolerance: some to sleep-disruption
Withdrawal: headache, irritable, can’t concentrate, drowsy, insomnia, GI pain, joint pain

Question 5

Adverse effects of Xanthines

Answer 5

Stimulates CV (theophylline), diuretic, stimulates skeletal muscle & smooth muscle 
In Toxic doses near 1gram:CNS: insomnia, excitement, delirium, tinnitus, light flashes, convulsions (can lead to death)

CV: inc HR, systoles, inc. resp rate, dec. clot time
Gastric: inc secretions

Question 6

What are the Nootropics?

Answer 6

Modafinil and Armodafinil (R stereotype only of Modafinil)

Question 7

Uses for Modafinil and Armodafinil

Answer 7

Narcolepsy (Most common), Shift work Sleep Disorder, Obstructive Sleep Apnea, ADHD in Adults

Question 8

Mechanism of Modafinil and Armodafinil

Answer 8

Only R-Modafinil is active:
Inc DA, NE, 5HT release, may block reuptake

Inc histamine levels, activates GLUT circuits, Inhibits GABA

Question 9

Adverse effects of Modafinil and Armodafinil

Answer 9

Headache, nausea, insomnia, lack of appetite, dizzy, agitated, anxiety, inc BP

Severe: Modafinil can cause SJS rxn (maybe due to L-modafinil?)

Question 10

CNS/tolerance of Modafinil and armodafinil

Answer 10

Wakefulness-promoting Agent

Off label uses: mood disorders, Parkinson, schizo, fatigue, athlete’s use to “dope”

Question 11

NE reuptake inhibitor

Answer 11

Atomoxetine,

Question 12

Use of Atomoxetine

Answer 12

ADHD - especially in adults

Question 13

Mechanism of Atomoxetine

Answer 13

Blocks NE transporter

Question 14

CNS affects of Atomoxetine

Answer 14

Stimulates cortex, improved working memory by Combined rise in NE, DA, & ACh levels

Question 15

Abuse potential of Atomoxetine

Answer 15

DA not elevated in nuc. accumbens = NO ABUSE POTENTIAL