Drugs for ADHD ->indirect sympathomimetics

Question 1

Stimulants to increase the level of NE and DA in the prefrontal cortex, increasing attention and focus
-D1 activation by dopamine in PFC decreases “noise”
-NE activation of alpha2 receptors in PFC increases the signal -> attention regulation & behavior inhibition
*Indirect sympathomimetic
MOA: NE and DA reuptake blockers

Answer 1

methylphenidate (Ritalin)
dexmethylphenidate (Focalin)

Interaction: MAOIs

*note dexmethylphenidate is only d-enantiomer so can give half dose ->only advantage

Question 2

Stimulants to increase the level of NE and DA in the prefrontal cortex, increasing attention and focus
-D1 activation by dopamine in PFC decreases “noise”
-NE activation of alpha2 receptors in PFC increases the signal -> attention regulation & behavior inhibition
*Indirect sympathomimetic
MOA: reverse transport of NE and DA

Answer 2

dextroamphetamine (Dexedrine)
amphetamine salts (Adderall)
lisdexamfetamine (Vyvanse)

Interaction: MAOIs

Question 3

Side effects of stimulants

Answer 3

worsens tic disorders, stomach pain, anxiety, irritability, insomnia, tachycardia, cardiac arrhythmias, palpitations, HTN, psychotic disorders, seizure disorders
Most limiting aspect of their use: dependence (not at the dose for ADHD)

Question 4

nonstimulant drug used for ADHD

MOA: selective inhibition of presynaptic NE transporter
-No abuse potential because it does not induce DA release in nucleus accumbens
-does not increase alertness
Side effect: nausea, growth inhibition, sedation

Answer 4

Atomoxetine (Strattera)

Int: Do NOT take within 2 weeks of MAOI (fatal hypertensive crisis)
paroxetine & fluoxetine increase its half-life

Question 5

OTC appetite suppressant that was removed from the market because of hemorrhagic strokes in women
-atomoxetine is derived from this compound

Answer 5

phenylpropanolamine

Question 6

Indirect sympathomimetic
MOA: inhibition of NET transporter & therefore reuptake of dopamine in the pleasure centers of the brain
-readily enters CNS for short duration amphetamine-like psychological effects

Answer 6

cocaine

Question 7

Mixed-acting sympathomimetic that is the precursor for methamphetamine
Use: decongestant

Answer 7

pseudoephedrine

Question 8

psychostimulant used to treat narcolepsy
MOA: inhibits NE and DA transporters, increasing NE, DA, 5-HT, glutamate while decreasing GABA

Side effect: mild increase in bp & HR, appetite suppression

Answer 8

modafinil (Provigil)

Question 9

normal byproduct of tyrosine metabolism in the body
-Can be produced in high concentrations in protein-rich foods by decarboxylation of tyrosine during fermentation
-Metabolized by MAO in the liver and inactive if taken orally due to high first-pass effect
-If given parenterally (infusion, injection or implantation), causes INDIRECT SYMPATHOMIMETIC action by release of stored catecholamines with spectrum of action similar to NE
MAOIs greatly increase its effects - increased bp

Answer 9

tyramine

Question 10

like amphetamine but with higher ratio of central to peripheral actions

Answer 10

methamphetamine