Dr. Masserano: ADHD/Narcolepsy/Stimulants Flashcards
(33 cards)
Catecholamine Analogs
- Longer acting
- Lipid soluble
1) Removal of 3-OH group protects from COMT metabolism
2) Alpha methyl group protects from MAO metabolism
3) Removal of all OH groups increases lipid solubility and CNS entry
Uses of Stimulants
1) ADHD
2) Short term treatment of obesity
3) Narcolepsy
Xyrem (GHB)
- Used for Narcolepsy with cataplexy
- Schedule 3 when used medically
- Schedule 1 when abused
Which drugs can be used for ADHD
- Amphetamines
- Methamphetamine
- Lisdexamphetamines
- Methylphenadine
- Atomoxetine
- Clonidine
- Guanfacine
Which drugs can be used for Narcolepsy
- Amphetamines
- Methylphenadate
- Solriamfetol
- Modafinil
Which Drugs can be used for Obesity
- Methamphetamine
- Phentermine
- Osymia
- Diethylpropion
- Lorcaserin
- Victoza
- Saxenda
- Contrave
Amphetamines MoA
- Stimulate the release of NE and DA
- Inhibit the reuptake of NE and DA
Adderall
-FDA warning: Cardiac abnormalities and serious cardiac problems in children
Methamphetamine (Desoxyn, Methampex) MoA
-Used for ADHD and Obesity
Lisdexamfetamine (Vyvanse) MoA
- Treatment of ADHD and Eating Disorder
- Inactive prodrug
- Limits abuse potential
Methylphenidate (Ritalin) MoA
- Treatment of ADHD, Narcolepsy, Major Depression
- Daytrana: once daily patch, useful for children who cannot swallow pills
Concerta (Methylphenidate ER)
- Contains polyethylene oxide
1) Insoluble in alcohols
2) Viscous gel when mixed with water
Phentermine (Adipex-P, Fastin, Ionamin)
- Increases NE and DA release
- Inhibits NE and DA reuptake
- Short term treatment of obesity
- BMI > 30
- BMI >27 with risk factors
Osymia (Phentermine and Topiramate)
- Short term treatment of obesity
1) prolongs inactivation period of Na+ channels
2) AMPA/Kainate antagonist - Do NOT use in pregnancy
Diethylpropion (Tenuate)
- Stimulates the release of NE and DA
- Short term management of obesity
Phenylpropanolamine
- OTC drug
- Used for nasal decongestant
- And treatment of obesity???
- Women are at a 15x higher risk of stroke
Ephedrine MoA
- Releases andogenous NE
- Effects on beta receptors
- FDA prohibits dietary supplements containing ephedrine
Therapeutic uses of Ephedrine
1) Acute bronchospasm
2) Hypotension
3) Orthostatic hypotension
4) Nasal congestion
5) Nighttime enuresis
Pseudophedrine (Sudafed)
- OTC drug
- Mostly effects alpha receptors
Therapeutic uses for pseudoephedrine
1) Nasal congestion
2) Otalgia prophylaxis
3) Urinary incontinence
Lorcaserin (Belviq)
- Antiobestity drug
- BMI >30 or >27 with other factors
- Serotonin syndrome, suicidal thoughts, heart disease
Nexafed
- Pseudoephedrine tablet designed to help curb methamphetamine production
- Turns into thick gel when dissolved
- Makes it harder to make meth
Contraindications for all amphetamine type stimulant drugs
1) Cardiac disease
2) Hyperthyroidism
3) Closed angle glaucoma
4) Psychosis
Drug interactions with All amphetamine type stimulant drugs
1) Enhance the effects of sympathomimetics
2) Do NOT use with MAOIs
3) May counteract the effects of some antihypertensive agents
4) Antipsychotics may lower the efficacy of these drugs
