Psychostimulants (for Wakefulness) Flashcards
Psychostimulants (General)
Uses:
-excessive sleepiness and fatigue
-improvement of ADHD
Drugs of Abuse
-can cause euphoria
-used by students for academic benefit
-weight loss
Characteristics:
-increase NE, increase DA, increase 5-HT
—all 3 monoamines are affected to various degrees
Effects of increased Concentration in CNS
-NE (increase arousal, decrease need for sleep)
-DA (euphoria, reward, and potential abuse; abnormal movements; psychosis
-5-HT (hallucinations; decreased appetite)
Amphetamine
Indirect Sympathomimetics - releasing agents
MOA:
-displaces stored catecholamines:
—uptake via NET and VMAT-2 –> replaces DA in vesicles –> DA release via DA (reverse transport) (also increases NE and 5-HT levels)
Use:
-ADHD
-Excessive sleepiness in patients with narcolepsy
AEs:
-increase NE
—Sympathomimetic AES: increased BP, cardiac arrhythmias
-increased DA
—Growth inhibition (DA might suppress growth hormone)
-increased 5-HT
—anorexia (decreased appetite)
Methylphenidate (Ritalin)
Indirect Sympathomimetics - reuptake inhibitors
MOA:
-blocks NET and DAT (NE and DA reuptake) –> increase DA, increase NE
Use:
-ADHD
-Excessive sleepiness in patient with narcolepsy
AEs:
-similar to amphetamine
Modafinil, Armodafinil
Indirect sympathomimetics - reuptake inhibitors
MOA:
-May block NET and DAT (NE and DA reuptake) –> increase DA, increase NE
Use:
-Excessive sleepiness in patients with narcolepsy and other disorders that cause excessive sleepiness
AEs:
-Less than other psychostimulants (eg. less sympathomimetic effects)
Reuptake Inhibitors that are NOT Psychostimulants
Atomoxetine
-inhibits NET
-for ADHD, Anxiety, Neuropathic Pain
TCAs (Amitriptyline)
-inhibits SERT
-for Depression, Anxiety, Neuropathic Pain
SSRIs (Fluoxetine)
-inhibits SERT
-for Depression, Anxiety
SNRIs (Duloxetine)
-inhibits SERT, NET
-for Depression, Anxiety, Neuropathic Pain
NDRIs (Bupropion)
-inhibits NET, DAT
-for Depression, ADHD, Smoking Cessation
