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43 Cards in this Set

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Caffeine
found in coffee and tea is a trimethylated xanthine (1,3,7 trimethylxanthine).
theophylline
found in tea, 1,3 dimethylxanthine. Less able to cross into CNS. Used to be used for asthma tx.
theobromine
found in chocolate, 3,7 dimethylxanthine.
Caffeine properties
CNS stimulant, delay onset of drowsiness and fatique, promote concentration, produce keener appreciation for sensory stimuli.//

Constricts cerebral vasculature, antagonist to vasodilatory effects of adenosine.//
Peripheral effects of caffeine
increase HR, increase GFR, acid secretion, and lower bowl irritability.
Caffeine Mech of action
During periods of wakefulness, ATP and cAMP is generated, and upon their breakdown, adenosine is released. Adenosine activates receptors resulting in drowsiness and sleep. Caffeine antagonizes the effects of adenosine.
Adenosine receptors
A1, A2a, A2b, A3.//
Caffeine effects on A1-R
A1: brain, presynaptic, inhibit AC, decrease cAMP, especially in arousal areas. //
Caffeine effects on A2a-R
A2a-R: basal ganglia, postsynaptic. They activate AC and increase cAMP which enhances tonic inhibitory action of basal ganglia. Caffeine release this tonic inhibition resulting in psychomotor stimulation.
Caffeine Toxicity and OD:
rare, overconsumptions may cause headaches (excessive vasocontriction), insomina, anxiety and panic attack.
Caffeine withdrawal and Tolerance.
little tolerance; headache, depression and inablity to concentrate 24-48 hrs after last dose. Headache due to excessive vasodilation.
Xanthine action on Phosphodiesterase (PDE)
PDE removes cAMP, and things like caffeine inhibit it causing increased cellular cAMP. Not seen with typical coffee consumption dose.
Theophylline and muscle
used to be for asthma treatment. At high dose would inhibit PDE, resulting in SM relaxation. NO longer drug of choice for asthma.
Nicotine
agonist at the nAchRn. Peripheral effects include vasocontriction, and bradycardia (ganglionic) and increased perspiration (aortic chemoreceptors). CNS effects involve cortical arousal.//
CNS sympathomimetics
involves global neuromodulation by monoaminergic neurons located in midbrain and the brainstem.
Cocaine
obtained from leaves of Erythroxylon coca.//
Cocain CNS effects
tachycardia, systolic and distolic BP rise, euphoria.... after 40-80 min, followed by depression, dysphoria, and intense craving for more cocaine.
Cocaine effects depending on route of administration
injected, smoked and intranasal result in greater risk of binge use.//

Oral risks of delayed OD and heart attack.//
Cocaine Mech of action
CNS: blockade of reuptake for NE, DA, and serotonin (5HT). >> increased activation of their receptors.//

DA activation: cause reinforcing effects at mesolimbic 'reward' pathways in Nucleus accumbens.
Difference btwn cocaine action and amphetamines?
effects are similar but cocaine has shorter duration and its actions are activity-dependant.
Cocaine's Medical use?
local anesthetic in upper resp. tract.
Cocaine addiction
seems to cause permanent changes in brain, causing less DA release to same stimulus >>> drug craving, depression
Cocaine toxicity
High acute dose: arrhythmias, heartblock, cardiac arrest.

Higher dose: termor, tonic-clonic convulsion, vomiting... followed by depression and respiratory failure.

Tx: symptomatic; beta blocker, diazepam and DA.
Cocaine chronic use:
some degree of tolerance, cardiac damage (enlarged heart), paranoia and psychotic behavior similar to amphetamines, nasal septum damage (from repeated vasoconstriction). //

Withdrawal: ahedonia, more craving, increased appetite, depression, lethargy, sexual dysfuntion.//
What's a 'speed ball'?
polydrug: cocain or amphetamine combined with opitates to reduce anxiety provoking effects.
What's a DA receptor antagonist?
haloperidol
Amphetamines
synthetic benzylethylamine, resembling endogenous catecholamine (NE, DA) and decongestant drugs (ephedrine, pseudoephedrine)
Amphetamines: CNS stimulation
increase alertness, delay fatigue, euphoria, irritability, anxiety.//

DA antagonist (haloperidol) block amphetamine actions.

depresses appetite (weight loss).
High dose amphetamines
stereotypical behavior of DA receptor activation: repetitive lip movement, tongue and extremities, jaw clenching, teeth grinding >>> followed by depression.
Amphetamine Mech of action?
indirect sympathomimetics: release NE, DA from nerve terminals both in CNS and periphery.
compare amphetamine, methamphetamine and tyramine?
Tyramine is the least CNS permissive. methamphetamine due to its extra methyl group enters brain more readily than amphetamine and has a longer half-life.
Describe Amphetamine action?
enters neurone through DA-transporter or by diffusion, inhibits MAO, enters storage vesicles and displaces DA, NE or serotonin. High monoamine result in going through plasma membrane transporter (in reverse), causing receptor activation.
Khat
kathionine (from katha edulis), resemple amphetamine, but less potent. used in horn of Africa and Arabian peninsula.
Amphetamine medical use
restricted to treatment of ADHD and narcolepsy.
Drug for ADHD pts
Methylphenidate (Ritalin). Inhibits NE, DA and 5HT uptake like cocaine; may also induce transmitter release similar to amphetamines. oral administration.//

amphetamine and methylphenidate have same efficacy in treating ADHD.//
Describe Amphetamine action?
enters neurone through DA-transporter or by diffusion, inhibits MAO, enters storage vesicles and displaces DA, NE or serotonin. High monoamine result in going through plasma membrane transporter (in reverse), causing receptor activation.
What's a NE-selective reuptake inhibitor?
atomoxetine, approved for ADHD. This drug is not reinforcing b/c of no DA action? compared to methylphenidate. //

many side effects; sexual dysfunction, less reliable, liver dysfunction (CYP2D6), suicidal thoughts.
Narcolepsy treatment
amphetamines, modanifil
Amphetamine medical use
restricted to treatment of ADHD and narcolepsy.
Modanifil
new drug for narcolepsy, shift-work sleep disorders, military. Does not activate reward pathways, no "high" or "crash" afterwards.
Drug for ADHD pts
Methylphenidate (Ritalin). Inhibits NE, DA and 5HT uptake like cocaine; may also induce transmitter release similar to amphetamines. oral administration.//

amphetamine and methylphenidate have same efficacy in treating ADHD.//
ADHD
deficiency in NE and/or DA leading to less ability to focus.
gamma hydroxybutyrate (GHB)
also 'date rape drug', not a stimulant but a sedative-hypnotic. Used in conjuction with modanifil, given at bedtime to enhance quality of nocturnal sleep in order to reduce daytime sleepyness in narcolepsy pts.