Noonotropics Flashcards
Short-acting amphetamine
dextro-isomer of d,l-amphetamine sulfate
Immediate release formulation -> 30 min
1-2 hr peak and 4-6 hr duration of action
Dextroamphetamine sulfate (Dexedrine, Dextrostat)
Short-acting amphetamine
Amphetamine salt; dextro-isomer of d,l-amphetamine (3:1)
Immediate release formulation -> 45 min
1-2 hr peak and 4-6 hr duration of action
*Significant CYP2D6 interactions; also flavin-containing monooxygenase
Adderall
Short-acting amphetamine
Dextro-isomer of d,l-amphetamine
Immediate release formulations -> 45 min
2-3 hr peak and 4-5 hr duration of action
Methamphetamine HCl (Desoxyn)
Long-acting amphetamine
Contains both immediate and extended release
>10 hr duration of action
Dextroamphetamine Spansule
Long-acting amphetamine
Contains both immediate and extended release
Initial effects about 2 hrs; >7 hrs duration
Extended Amphetamine salt (Adderall XR)
Short-acting Methylphenidate
1/5-2 hr peak; 4 hr duration of action
***dextro-isomer only; 2x as potent as methylphenidate
Dexmythylphenidate (Focalin)
Mechanism of action of methylphenidates
NET & DAT inhibition
Intermediate-acting methylphenidate
6-8 hr duration of action
Due to ER formation cannot be divided, crushed, or chewed
Ritalin, Methylin ER, and Metadate ER
Long-acting methylphenidates
8-12 hr duration
Medadate, Ritalin LA, Concerta, Focalin XR, Daytrana
Nonstimulant drug for ADHD Selective NET inhibitor dosed per body weight *initial effects may take up to a week *CI in pts with reduced CYP2D6 activity
SE?
Atomoxetine
SE: insomnia, increased BP; suicidal tendencies
Nonstimulant drug for ADHD
Tricyclic antidepressant
Reuptake inhibitor of dopamine, 5HT, and NE
Not FDA approved for ADHD (but still used)
SE?
Bupropion (Wellbutrin)
SE: irritability, insomnia, decreased appetite and suicidal tendencies
Sudden death is related to what in tricyclic antidepressants?
CYP2D6
Used as second line treatment/monotherapy for ADHD
alpha agonists
alpha 2 agonist in the brain
Used to treat HTN in adults and ADHD
Onset <1 hr and 3-6 hr duration
Clonidine (Catapres)
selective alpha 2A agonist used for ADHD
onset 1-4 hr and 6-8 hr duration
Guanfacine (Tenex)
SE of alpha agonists for ADHD
sedation, depression, dry mouth, hypotension, rebound hypertension; deaths in combo with stimulants
first FDA approved reversible ChE inhibitor for probable AD
limited use due to hepatotoxicity
Tacrine (Cognex)
Reversible ChE inhibitor approved for mild and moderate AD
100% bioavailability and 70 hr half-life
Donepezil (Aricept)
ChE inhibitor; slow dissociation constant; butyrylcholinesterase
Greater activity but with higher incidence of side effects
Rivastigamine (Exelon)
alkaloid-based ChE inhibitor; nicotinic rc activity
80-100% bioavailability and 7 hr half-life
Galantamine (Reminyl and Razadyne)
NMDA rc; 5HT rc; can be combine with ChE inhibitor
100% bioavailability and 60-80 hr half-life
SE?
Memantine (Namenda and Ebixa)
SE: HA, fatigue, dizziness, vomiting, confusion, hallucination, cough, back pain, and dyspnea
Tx of motor sxs in PD
Levadopa
Tx of psychosis (advanced AD)
Haloperidol
Tx of depression
5HT reuptake inhibitors; tricyclic antidepressants
Tx of insomnia
melatonin