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Flashcards in PDA CNS Stim Deck (32):
1

What is the structure of caffeine?

methylxanthinem=, similar to purines

2

What is hte mechanism of action of caffeine?

competitive antagonist of adenosine receptors produce IPSPs; presynaptic adenosine receptors inhibit glutamate;
caffeine inhibits these inhibitory effects

3

At higher doses what does caffeine do?

inhibits cAMP phosphodiesterase; results in increase of cAMP

4

How does caffeine work as a CNS stimulant?

increased alertness
decrease fatigue and drowsiness
can cause nervousness, restlesness and tremors
high doses can stim medullary respiratory and CV centers; can get tachycardia

5

What are the peripheral effects of caffeine?

positive ionotropic and chronotropic effects
dilates coronary and systemic blood vessels; constricts cerebral blood vessels
diuressis
increase gastric secretion
modest bronchodilation

6

What are the toxicity and consequences of chronic use?

tolerance, overdose results in excess CNS stim
physical dependence
withdrawal symptoms

7

What are the sympathomimetic stimulants; act through enhancement of catecholaminergic

amphetamines, cocaine, etc

8

Mechanism of action of cocaine?

potent inhibitor of the reuptake of norepi, dopamine, and serotonin
binds to transporter itself
increase activity of tyrosine and tryptophan hydroxylases
local anesthetic and vasoconstrictor

9

Cocaine causes waht in addicts?

profound psychological dependence as well as physical dependence

10

What is the structure of amphetamine and metamphetamine?

weak bases, absorbed orally, metabolized to benzoic acid
long half life
similar structurally to norepi

11

What is the mech of action of amphetamine?

relase NE, DA and 5HT
block reuptake of those
partial agonist of alpha receptors
MAO inhibitor at high doses

12

What are the clinical uses of amphetamine?

tx narcolepsy and ADHD

13

Side effects of amphetamine?

insomnia, abdominal pain, anorexia, suppression of growth, facial tic, high body temperature

14

What are the toxic effects of amphetamines and mehtylphenidates?

restlessness, dizziness, tremor
psychosis
neurtoxicity
meth mouth
abuse liability

15

What is the mechanism of action of nicotine?

agonist of nicotinic cholinergic recpetors
neuromuscular junction; initally activates muscle contraction
autonomic ganglia
parasympathetic GI effects

16

How quickly does tolerance ot nictonie occur?

very rapidly within a few hours

17

Nicotine withdrawal symptoms include what?

irritability
anxiety
depression
difficulty concentration
incresased appetite

18

What is unique about alcohol?

not potent at all; one dose is about 14 grams

19

How is alcohol metabolized?

ADH, CYP2E1 and aldehyde dehydrogenase

20

How many molecules of NADH do you use per consumption of one molecule of ETOH?

2 molecules of NADH

21

Mixed function oxidase system metabolizes alcohol in who?

chronic alcoholics

22

What drug blocks aldehyde dehydrogenase?

disulfiram

23

What are some consequences of alcohl metabolism?

increased NADH, inhibiton of TCA cycle, reduced fatty acid oxidation
increased acetaldehyde
depletion of glutathione

24

Metabolic changes in alcoholics results in what?

fatty liver
hepatic inflammation
induction of CYP2E1

25

What are the CNS effects of ethanol?

several ion channels are sensitivie to the presence of ethanol
GABAa receptor-ligand chloride channel
disturbs balance between excitatory and inhibitory

26

Chronic ethanol liver and GI effects are what?

Hep C often co-morbid
steatosis: fatty liver
cirrhosis
gastritis, pancreatitis, malabsorption
chronic diarrhea
cancers

27

Chronic ethanol on CNS system is what?

tolerance occurs; adaptive neruonal changes
Up regulates the excitatory transmission to compensate
both psychological and physical dependence occurs

28

How frequently does alcohol addiction occur?

5-10% of men and 3-5% of women

29

What is the neurtoxicity of alchol?

neuralgia
memory impairment
thiamine deficiency associated with chronic alchol use can produce
cerebellar/cerbral atrophy
wericke's encephalopathy
korsakoffs syndrom

30

What are the tetraogenic effects?

Associated with chronic maternal alcohol abuse
FAS

31

What is the general lethal level of ethanol?

400 mg/dl=12 liters

32

How does one treat alcohol withdrawal?

prevent seizures, deliurium and arrythmias
subsititues for alcohol