Stimulants Flashcards
Dopamine Stimulants
Substantia Nigra –> VTA
AMPHETAMINES - Adderall
METHAMPHETAMINE
METHYLPHENIDATE - Ritalin
COCAINE
Adrenergic Stimulants
Locus Ceruleus
*NOREPINEPHRINE - can give directly
Ephedrine, Yohimbe
Serotonergic Stimulants
Dorsal Raphe
MDMA - Block SERT and reverses its direction. Also blocks DAT. Increases both Serotonin and Dopamine
FENFLURAMINE - 5HT2B agonist previously used for PTSD, affects heart valves.
SE: Hyperthermia, Arrythmias, Rhabdo
Cholinergic Stimulants
Nucleus Basalis, Septum, Pedunculopontine Nuclei
NICOTINE - agonist at Alpha-7 nicotinic receptors. Increases Dopamine levels.
Both a relaxant and a stimulant
SE: Increased clotting, tachycardia
Norepinephrine Stimulants
Locus Ceruleus
EPHEDRINE (Ma Huang) - nonselective alpha/beta agonist. Asthma and weight reduction
YOHIMBE - alpha-2 antagonist. Arousal from anesthesia, sexual dysfunction, Type II Diabetes
Interactions: Halothane, MAOIs, NDRIs
GABA Stimulants
FLUMAZENIL - competitively block GABA-A receptor from Benzo’s/Alcohol
SE: Seizures
DILSULFIRAM - Acetylaldehyde Dehydrogenase inhibitor
Adenosine Stimulants
Xantines = Blocks Adenosine Receptor
Caffeine Metabolites
- Paraxanthine - lipolysis
- Theobromine - vasodilation
- Theophylline - bronchodilation
Histamine Antagonists
IRDABISANT - blocks H3 receptor (presynaptic) so you increase Histamine release at the synapse
Histamine = Wakefulness, Alertness
Modafinil
Used in Narcolepsy, Shift Work sleep disorder
“Dirty Drug” - many actions
- Inhibits DAT, NET, SERT
- Activates orexin receptors –> Increases Dopamine
- Inhibits GABA transmission
- Increases histamine in the hypothalamus
Amphetamines
Increase Dopamine Release. Interfere with DAT and cause it to leak Dopamine into the synapse
More potent and longer acting than cocaine
D1/D5 Receptors
Gs stimulates AC to increase cAMP
D2, D3, D4 Receptor
Gi inhibits AC and decrease cAMP
Target of many antipsychotics along with 5-HT2A (Gq)
Cocaine/Methylphenidate (Ritalin)
Block reuptake DAT, SERT, NET, and sodium channels
Keep Dopamine in the synapse
Sodium channels responsible for deadly cardiac arrest with Cocaine
Amphetamines more potent and longer acting
Dopaminergic Side Effects
Overstimulation - some cross-talk with adrenergic receptors Na+ Blockade - cardiac Exhaustion of dopamine system Suicidal Ideation Tolerance
Caffeine
Nonselective A2a antagonist (Gs) that ultimately increases cAMP and increases Dopamine
Nicotine decreases half life
Oral contraceptives double (!!)
