CNS stimulants -- Lichtblau Flashcards
CNS effects of sympathamimetics
increased wakefulness, decreased fatigue, increased motor and speech; OD –> tremor/restlessness
Examples include amphetamine, cocaine, caffeine, modafinil
Peripheral effects of sympathamimetics
increased systolic and diastolic BP; high dose = arhythmias
When you increase the doseing of sympathomimetics, different affects occur in neurotransmission. What are the stages you see?
- increased release of DA and NE – increased [] acting on postsynapitic receptors
- Blocking of NE and DA reuptake – further increasing []
- inhibition of MAO – usually breaks down stuff, so [] increases
What are the toxic effects of amphetamine and treatment for OD?
overstimulation, dizziness, dyskinesia, hallucinations
MOA: increased NE release
Tx: give sedatives such as benzodiazepines, antipsychotics
Therapeutic uses for sympathamimetics?
AD(H)D
narcolepsy
fatigue
analeptic – reduces drug induced depression
weight loss
Cocaine acts on the CNS, PNS, and of course has toxicity. List all three.
CNS = inhibits DA reuptake
PNS = inhibits reuptake of NE (released by postganglionic sympathetics on cardiac and smooth muscle, gland cells (except sweat gland releases ACh), nerve terminals.
Toxic = cardiac arrhythmias, coronary and cerebral thrombosis (local coagulation or clotting of the blood in a part of the circulatory system)
MOA of methylxanthines?
- translocation of intracellular CA++ from sarcoplasmic reticulum
- inibition of phosphodiesterase (increased [cAMP])
- non-selective adenosine receptor antagonist
MDMA vs. other sympathamimetics?
MDMA = ecstasy (meth + -CH3 = increase lipophilic)
MDMA directly stimulates 5-HT2(1a)autoreceptors and stimulates release of serotonin and inhibits its reuptake
sympathamimetics = dose dependent (1) increased release (2) reuptake of NE and DA
What are bath salts? How are they used?
bath salts contain various amphetamine-like chemicals (increasing release of NE and DA)
High abuse and addiction potential
“cocaine substitute”
Theophylline
methylxanthine used for treatment and prophylaxis of bronchial asthma
Amphetamine vs Cocaine in tolerance and dependence
amphetamine = less dependence
cocaine = more dependence
similar tolerance between the two developes to effects on appetite on mood
modafinil
MOA and adverse affects
MOA:
- increases [DA] in striatum and nucleus accumbans
- increases [NE] release in hypothalamus
- increases [5-HT] in amygdala and frontal cortex
Adverse affects: headach, insomnia, anxiety, increased BP, *potential for severe rash!
