CNS Stimulants Flashcards
Name 6 sympathomimetics:
Amphetamine (Benzedrine)
D-Amphetamine (Dexedrine)
Methamphetamine
Methylphenidate (Ritalin, Concerta, Metadate)
Cocaine
MDMA “Ecstasy”
Name three Xanthines:
Theobromine
Theophylline
Caffeine
Low dose sympathomimetics have what general effect on neurotransmission?
Increase release of DA and NE
Medium dose of sympathomimetics have what effect on neurotransmission (generally)?
Blocks NE and DA reuptake
High dose of sympathomimetics have what effect on neurotransmission (generally)?
Inhibit monoamine oxidase (MAO)
Cocaine MOA:
Blocks reuptake of NE–> motor excitation
Blocks reuptake of DA –> euphoria
Local anesthetic properties
Toxicity of cocaine:
cardiac arrhythmias, coronary and cerebral thrombosis
impairs in utero brain development–>significantly decreased brain size and neurological manifestations
High lipophilicity, very rapid entry into the brain:
MDMA (ecstasy)
-stimulates release and reuptake of epinephrine, NE, DA
Difference between MDMA and amphetamines:
MDMA also directly stimulates 5HT(2,1A) autoreceptors and stimulates the release of serotonin and inhibits it’s reuptake
**also affects histamine, GABA, Ach, NE transport proteins, DA receptors
Three Xanthines:
Caffeine
Theobromine
Theophylline
Xanthines’ affects on skeletal and smooth muscle:
Skeletal–increase work capacity
Smooth–relax
Non CNS effects of sympathomimetics: (2)
- Increased systolic and diastolic BP (reflex decrease in HR)
- High doses lead to arrhythmias
Treatments for acute sympathomimetic toxicity: (2)
- antipsychotics (ie. haldol)
2. acidify patients urine —> increase % ionization of drug
Tolerance and dependance of sympathomimetics more psychological or physical?
Psychological–withdrawal results in craving more drug
Physical dependance is debated
Drug that may be an “empathogen”?
MDMA