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68 Cards in this Set

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1,3,7 trimethylxanthine
1,3 dimethylxanthine
3,7 dimethylxanthine
caffeine
theophylline
theobromine
At what dose of caffeine are measurable CNS effects seen?
oral ingestions of 150 mg caffeine- giving plasma levels of 10 mg/ml (50uM)
Of the three caffeine drugs, which is the weakest stimulant?
theobomine
What is the mechanism of CNS effects?
disinhibition of forebrain arousal pathways
At high doses of caffeine, what happens to medullary stimulation?
respiratory, vasomotor, and vagal centers stimulated
even inc reflex excitability in spinal cord
Is there a lot of tolerance/dependence with caffeine?
little tolerance but heavy coffee drinkers may get headache and depression in morning upon withdrawal
How can a xanthine be used in smooth muscle relaxation?
theophylline in asthma
What can large amounts of strong coffee do to CV stimulation?
produce cardiac irregularities
What do xanthines do to GFR?
increase rate- caffeine induced diuresis
What do xanthines do to the GI tract?
inc HCl secretion- heartburn; lower bowel irritability
Describe caffeines affect on adenosine receptors
non selective A1 and A2 antagonist at fairly low concentrations (50 uM)
What does A1 do?
inhibits adenylyl cyclase --> dec cAMP
inc adenosine (from ATP brkdwn and cAMP) --> A1 inhibits forebrain cholinergic arousal pathways --> drowsiness and sleep
(caffeine inhibits the adenosine--> delays sleep)
What does A2 do?
stimulate adenylyl cyclase
inc cAMP
What does ethanol do to the adenosine actions at A1 receptors?
potentiates them, regulating ACh release in thalamus
What does caffeine do at >100 uM concentrations
1. inhibits phosphodiesterase --> inc cAMP
2. releases Ca from intracellular stores
What are the two phases of tobacco smoke?
gas phase
and
particulate phase
What does the gas phase of tobacco smoke contain?
CO2, CO, acetaldehyde, acetone, hydrogen cyanide, ammonia, etc
What does the particulate phase of tobacco smoke contain?
nicotine
phenol, cresols, beta-naphthylamine, etc
Through what receptors does nicotine activate the sympathetic nervous system?
nACHn receptors
Through what receptors does nicotine activate the parasympathetic nervous system?
nAChn receptors
How can nicotine cause ganglionic blockade?
through nAChn receptors- only at high doses (not smoking)
What are the effects of chemoreceptor stimulation by nicotine at nAChn receptors?
aortic arch and carotid body- respiratory stimulation
emetic trigger zone (postrema)- nausea, vomitting
hypothalamus (supraoptic nu)- ADH secretion
What is the most obvious effect of motor reflex stimulation/depression in smokers?
depression of knee jerk
*only weak activity at nAChm receptors
differences in motor stimulation with different nicotine doses?
stimulation at low doses
depression at high doses with very rapid tolerance to stimulant
How does nicotine create an effect associated with behavioral reinforcement
increases DA release in nuc Accumbens
How good is nicotine at analgesia?
great, but not used because of other effects
What is the major metabolite of nicotine?
longer or shorter t1/2?
less or more pharmacologic activity?
cotinine
longer (19 hrs)
less
What is green tobacco sickness?
acute intoxication of nicotine- nausea, vomiting, weakness, headache, sweating, salivation
How common are daths due to oral ingestion of nicotine?
rare due to vomiting and first-pass metabolism
What happens with chronic nicotine toxicity?
CV toxicity, hypertension, COPD, low birth weight babies
Name some different nicotine replacement therapies?
NICOTINE skin patches, nasal spray, inhalers, chewing gum
What is the success rate of the patch?
10% at 1 yr
What antidepressant may be used for nicotine cessation?
buproprion- 23% success rate at 1 yr
(tremor 3%, headache 1%, skin rash 1%)
What are some possible therapeutic applications of nicotine?
1. ulcerative colitis- symptoms develop when smokers quit- use of nicotine patches have reduced sx in ex smokers
2. alzheimer's disease- lower incidence of AD and Parkinson's, some symptomatic relief with patch
Is nicotine approved by the FDA for tx of UC or AD?
no
What are amphetamines?
What type is more effective
synthetic benzylethylamine derivates- the D-isomer (dexamphetamine) is ore active than the l-isomer in CNS
What is the amphetamine MOA?
indirectly acting sympathomimetic amines- release NE, DA (and 5-HT) in periphery and CNS (like tyramine)
Down to the details, how does amphetamine do its thing?
enters neurons through DA transporter (DAT) and inhibits MAO --> displaces monoamines by getting into vesicles with help of VMAT --> elevated monoamines go into extracellular space via reversal of plasma membrane transporter --> inc local monoamine receptor activation
Where are the critical places for the euphoriant and motor effects of amphetamines?
effects on DA receptors in nuc Accumbens and caudate-putamen
What happens with chronic amphetamine use?
tolerance
tendency to inc dose, compulsive use,
severe pranoia
psychotic behavior
skin crawling delusions
Even though there are "no good reasons for using amphetamines becuase of there abuse potential" why does the military use them? What about athletes?
military- delay onset of fatigue in military personnel (e.g., pilots)
athletes- enhance physical performance
How do you tx acute amphetamine intoxication?
symptomatically
lorazepam for agitation, irritability
antipsychotic
What comes from the leaves of Erythroxylon coca
cocaine (the hydrochloride salt)
powder
snow
What is the "free base" form of cocaine?
crack- more rapidly absorbed across mucous membranes
Cocaine MOA?
local anesthetic and indirectly acting sympathomimetic amine- blocks re-uptake of NE, DA, 5-HT
How much cocaine administered intranasally incresaes heart rate and raises BP?
25-100 mg
How does smoking crack differ from oral ingestion?
smoking can induce very intese effects; oral ingestion gives prolonged intesnse stimulation and high risk of CV and CNS toxicity
What happens after the euphoria induced by cocaine?
it declines before the drug plasma levels do --> 40-80 minutes of depression, dysphoria, and intense craving for more
What antagonizes cocaine euphoria?
DA antagonists
What may explain the depression and drug-craving of drug-free cocaine addicts?
DA neurons of striatum in detoxified human cocaine users release less DA in response to stimulus than drug-naive subjects
What can high doses of cocaine do?
tremor, tonic-clonic convulsions, vasomotor stimulation, vomiting, cardiac arrhythmias, heart block ,sudden death, or death from respiratory depression
what causes nasal septum damage associated iwth cocaine?
repeated local vasoconstriction
What can chronic use cause?
permanent cardiac damage, paranoia, psychotic behavior
What are the withdrawal sx associated with cocaine?
increased appetite, lethargy, depression
What is a speedball?
opiate comibined with amphetamine to reduce anxiety provoking effects
Is cocaine an aphrodesiac?
reportedly, but is definitely associated with sexual dysfunction
How would you tx acute cocaine toxicity causing CV complications and anxiety attacks?
psychosis?
seizures?
beta blocker
laoperidol (DA antagonist)
diazepam
What drugs may be used to treat chronic cocaine use?
bromocryptine- DA agonist
or
desipramine- NE uptake inhibitor
this drug is chemically similar to amphetamines but has fewer CNS affects; used as appetite supressant; may deplete 5-HT stores and lead to cell death
fenfluramine
What is fen/phen
combo of fenfluramine and amphetamine like drug (phenteramine)- was sold for wt. loss; --> valvular heart disease
This drug was approved to tx daytime sleepiness associated with narcolepsy, obstructive sleep apnea/hypopnea, shift work sleep disorder; and is used by military to maintain alertness
modafinil (provigil)
What is the MOA of modafinil?
involves inhibition of NE uptake by neurons in sleep promoting areas of ventrolateral pre-optic area
What does modafinil do to CYP3A4 and CYP2C19
induces
inhibits
this drug inhibits NE, DA, and 5HT like cocaine, but is less reinforcing?
methylphenidate (ritalin)
What is methylphenidate used for?
tx of ADD/ADHD
What is the MOA of methylphenidate?
deficiency of central MOAs leads to reduced ability to forcus attention --> blocking re-uptake reverses this effect
What was the first NE-selective re-uptake inhibitor approved for ADHD?
atomoxetine
Why might atomoxetine be a choice for children who can't take stimulants?
it has non-stimulant action