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151 Cards in this Set
- Front
- Back
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is ethanol lipid or water soluble and why does this matter?
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both lipid and water soluble
when it is ingested it goes everywhere (gets into all cells) uniformly distributed |
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mechanism of action of ethanol
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inhibits glutaminergic (excitatory) pathways so it acts as a depressant
increases GABAergic pathways => depressant net result: CNS inhibition dopaminergic "pleasure center" can be activated |
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sites of action of ethanol
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CNS: bad judgement, slow rxns, decreased motor, slurred speach
Cardiovascular: skin vasodilation and increase heat loss (hypothermia) GI: low doses increase gastric secretions (help digest) but can irritae gi at high levels liver: toxic to liver, do not take tylenol with alcohol kidney: inhibits ADH |
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what should you not take with alcohol
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tylenol (acetaminophen)
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where is alcohol absorbed
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small intestine (NOT the stomach)...so if you keep alcohol in the stomach it wont be absorbed as fast (food slows alcohol absorption)
carbonation increases rate of stomach emtying which increases rate of EtOH absorption |
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distribution of alcohol in body
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equilibrates with all tissues
passes through b.b. barrier and placental barrier |
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what order rxn is the metabolism of alcohol
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zero order (rate is constant regardless of concentration of EtOH...1 oz per 3 hours)
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metabolism of ethanol
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ethanol to acetaldehyde (using alcohol dehydrogenase)
acetaldehyde to acetyl co A (using acetaldehyde dehydrog) acetyl co A to CO2 and H2O |
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symptoms of ethanol withdrawl
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headache, dizziness, sweating (a hangover)
severe: delerium tremors "dt's"...due to REM rebound...drink for entire week then stop then you get dt's |
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ethanol drugs:
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"FAD"
fomepizole: inhibits alcohol dehyd. acamprosate: decr craving in alcoholic disulfiram and tetraethylthiuram disulfide: inhibit acetaldehyde dehydrog (accum. of acetaldehyde) |
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nutritional deficiencies of alcoholics
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poorest nutrition in US b/c of high calories of alcohol
vitamin (thiamin) deficiency |
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what vitamin are alcoholics deficient
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thiamin
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what does the thiamin deficiency of alcoholics cause
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Warnicke's encephalopathy
and polyneuritis |
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to see if you're an alcoholic
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CAGE
Cut down on drinking Annoyed with criticism Guilty Eye opener |
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why is methyl alcohol so dangerous
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its metabolites are toxic (formaldehyde and formic acid)
and can cause metabolic acidosis, blindness treat by giving them ethanol (competes with methanol) |
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what would you give someone who drank methanol
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ethanol or fomepizil
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what kills people when they drink ethanol?
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decreased respiration
vomiting |
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what does acamprosate do?
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decreases the craving of alcohol in an abstained alcoholic
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characteristics of fetal alcohol syndrome
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cns dysfunction
facial abnormalities impaired immune system |
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when do you use general anesthetics?
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only for surgery
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characteristics of an "ideal" anesthetic
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loss of consciousness
amnesia analgesia (no pain) inhib. of reflexes muscle relaxation rapid onset and recovery pleasant for patients no serious side effects |
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classes of anesthetics:
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INHALED:
NO halogenated hydrocarbons (halothane, isoflurane, desflurane, sevoflurane) IV: barbituates (thiopental) propofol ketamine etomidate midazolam |
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how do inhaled general anesthetics work
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decrease membrane sensitivity which decreases neuronal firing
increases GABA decreases Glutamate |
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what makes one inhaled general anesthetic more potent than another
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the more lipid soluble (easier to get into brain) means more potent
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what do you use to measure potency of inhaled general anesthetics
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MAC (minimal alveolar concentration): the conc. at which 50% of patients feel no pain
lower MAC = more potent |
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with inhaled general anesthetics, which is more potent a higher or lower MAC
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lower MAC = more potent
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blood/gas coeff. for inhaled general anesthetics
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speed of inhaled anesthetic induction is inversely proportional to its solubility in blood (high blood solubility means slow induction (onset))
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why does an inhaled general anesthetic that has high blood solubility take longer to get into brain
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b/c the blood must become saturated before the anesthetic will leave the blood and enter the brain
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what about the speed of recovery of inhaled gen. anesth?
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symmetrical with speed of induction
so if highly blood soluble...slow onset...slow recovery not blood soluble...fast onset...fast recovery |
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blood gas coeff. of nitrous oxide
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0.5 (not very soluble) do works quickly and can recover quickly
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potency of NO
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low
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characteristics of NO
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not soluble (works fast, recovers fast)
not potent no amnesia bloating and discomfort (because it wants to leave the blood since is is not soluble) repeated exposure...leukopenia (dec. WBC) and megaloblastic anemia (dec. RBC's) fetal abnormalities with repeated use |
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what form are the halogenated hydrocarbons
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liquid
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which is more potent...NO or halogenated hydrocarbons
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halogenated hydrocarbons
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side effect of halogenated hydrocarbons
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malignant hyperthermia (large increase in body temp, musc. rigidity from increased calcium uptake, life threatening)
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a high blood/gas coeff means what
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more soluble in blood (takes longer to act and longer to remove)
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MAC and side effects of halothane (a halogenated hydrocarbon inhaled anesthetic)
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lower MAC (minimal alveolar concentration) than NO so more potent
hepatic necrosis after repeated exposure |
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what is a side effect of halothane
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hepatic necrosis
(also malignant hyperthermia) |
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what is the MAC of NO
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greater than 100% so it is not very potent
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what can you use to treat the malignant hyperthermia caused by halogenated hydrocarbons
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dantrolene which will decrease release of calcium from the sarcoplasmic reticulum
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IV general anesthetics
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Barbituates: thiopental
Propofol Ketamine Etomidate Midazolam |
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acronym for IV general anesthetics:
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Barbara's Thighs
Probably Keep Eating Midas |
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IV general anesthetics have very _____ induction
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rapid
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barbituates are highly ______ soluble meaning....
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highly lipid soluble...rapidly enter brain (rapid onset and recovery)
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what did M.J. die from
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propofol (an IV anesthetic)
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how does thiopental work
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increases GABA receptor activity
rapid onset and recovery because drug will leave brain and be redistributed throughout the body (know that it gets redistributed) also an anti-anxiety med. |
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propofol works exactly the same as _________
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thiopental
small lipid soluble molecule increases GABA rapid onset and recovery redistribution from brain to other tissues (an IV general anesthetic) |
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propofol is what type of drug
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IV general anesthetic
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ketamine is what type of drug
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IV general anesthetic
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how does ketamine work
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blocks glutamate receptors
it is a phencyclidine (angel dust) analog "dissociative anesthesia" HALLUCINATIONS (remember thiopental and propofol increase GABA) |
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what is midazolam used for?
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tranquilizer (it is an IV general anesthetic)
Barbara's Thighs Probably Keep Eating Me |
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what are 2 IV general anesthetics that are no longer used
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diethyl ether
chloroform |
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which IV general anesthetic can cause hallucinations
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ketamine
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how many penises has jonas sucked on in his life?
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17 not counting the one in his mouth right now
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what are the benzodiazapenes?
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"pam's and lam's" plus chlordiazapoxide
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what are the anti anxiety and hypnotic drugs
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B(F)NB
benzodiazapenes: "pam", "lam", chlorodiazepoxide...flumazenil is a benzodiazapene blocker non-benzodiazapenes: "Z.Z. es ram bus" Barbituates: "tal" |
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acronym for non benzodiazapenes
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"Z Z es ram bus" think of some mexican guy named ZZ and he forgets the name of the bang bus so he calls it ram bus...if you dont know what bang bus is, look it up
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barbituate drugs
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"tal"
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what would you give someone who over doses on benzodiazapenes and what does it do
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flumazenil...blocks benzodiazapene receptor
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which drug is a benzodiazapene receptor blocker
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flumazenil
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what type of ion channel is the GABA receptor associate with
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Chloride
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what happens when you stop using benzodiazapenes
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increase CNS activity
seizures |
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side effects of benzodiazapenes
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drowsiness
do NOT drink alcohol with these b/c will depress CNS even more *visual disturbances |
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how would you administer flumazenil and why
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IV because of 1st pass metabolism
to someone who OD'd on benzodiazapenes |
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which non-benzodiazapene drugs work by the same mechanism but only vary by their T1/2
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zolpidem
zaleplon eszopiclone "Z Z es"....look for the Z's |
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how does ramelteon work?
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stimulate melatonin receptors because during sleep melatonin levels increase
(a non-benzodiazapene hypnotic) |
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what is a side effect of ramelton
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(a non-benzodiazapene hypnotic)
decreased testosterone "Ramel Bradley (a former UK bball player) was such a panzy so he must have had decreased testosterone" |
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how does buspirone work
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stimulates seretonin (5HT) receptors
pupil constriction at high doses (a non-benzodiazapene hypnotic) |
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side effect of buspirone
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pupil constriction
(a non-benzodiazapene hypnotic that is a seretonin agonist) |
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how do the barbituates work
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bind to GABA receptor and increase their activity 20 fold (benzodiazapenes increase GABA receptor activity 2 fold)
work at a site on the GABA different than where GABA or benzodiazapene work |
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what is the cause of death when using too much barbituates
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you stop breathing
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barbituates are ___ efficatious and _____potent than benzodiazapenes
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barbituates are more efficatious and less potent than benzodiazapenes (look at the graph)
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problems with barbituates
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decrease respiration
dont use with kidney problems *strongly induce p450 (induce interaction of other drugs and increase their metabolism) suppress REM sleep (does NOT lead to normal sleep) |
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what are the ways you can treat epilepsy (the different ways anti-epileptic drugs can act)
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inhibit Na or Ca channels
increase GABA decrease glutamate |
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mode of action of phenytoin
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inhibits Na channels (anti-epileptic)
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what does phenytoin treat?
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epilepsy...all forms EXCEPT petit mal
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side effects of phenytoin and what type of drug is it
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drug to treat gran mal and partial seizures
gingival hyperplasia hirutism (hair growth) resp. depression CV collapse messes up fetus messes up vision |
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is phenytoin metabolized by p450
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yes
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how does carbamaepine work
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(anti epileptic) inhibits Na channels
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What drug can cause chronic oral gingival hyperplasia, and excess hair growth
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Phenytonin
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What is the drug is used for all types of seizures
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Sodium Valproate
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What is the drug used for partial seizures?
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carbamazepine
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decreases sodium, can cause severe rash (steven Johnson), diplopia
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A new drug for seizures:
Iamotrigine |
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increases GABA neuron activity and decreases glutamate
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A new drug for seizures:
Topiramate |
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increases GABA, OD can cause nystagmus
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A new drug for seizures:
Gabapentin |
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inhibits GABA reuptake, hallucinations
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A new drug for seizures:
Tiagabine |
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decreases sodium, drowsiness
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A new drug for seizures:
Zonisamide |
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Blocks Ca++ channels, diplopia, ataxia, impaired thinking
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A new drug for seizures:
Pregabalin |
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What drug is used for status epilepticus?
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Diazepam
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Drug of choice to treat Petit mal and mechanism of action
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Succinimides
works by inhibiting Ca channels in thalamus |
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What drug is used for all seizures except petit mal?
What is it's mechanism? |
Phenobarbital
Activates GABA neurons for inhibition causes drowsiness and activates p450 |
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two drugs that inhibit MAO and reuptake of dopamine
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selegiline - metablized into amphetamine, causes insomnia
Resagiline - is more potent that selegiline and not metabolized to amphetamine |
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inhibits DOPA decarboxylase and taken with L-DOPA
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carbidopa
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what kind of drugs are capones?
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COMT inhibitors
used in combo with L DOPA piss orange |
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Ropinirole
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a dopamine agonist used to treat parkinson's(can cause impulsive gambling)
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what class of drugs do you also take modafinil with?
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dopamine agonists
bromocryptine, apomorphine, pramipexole, ropinirole |
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anticholinergics used to treat parkinsons
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"3-6 mafia benz"
trihexyphenidyl and benztropine anti dumbells ex. dry mouth |
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which drug is an antiviral but is also used to treat parkinson's?
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amantadine (releases stored dopamine...can cause a transient affect of CNS stimulation)
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what are the typical (first generation) schizophrenia and anti-psychotic drugs
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"TCTH"
Low potency: thioridizine and chloropromazine High potency: trifluoPERazine and haloPERiodol block dopamine receptors mainly (along with other receptors) but cause many side effects like extrapyramidal symptoms (parkinson's like symptoms, dystonias, akathesia) |
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what are the ATYPICAL schizo and anti-psycho drugs
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"CORA"
Clozapine Olanzapine Risperidone Aripiprazole block more seretonin receptors than dopamine receptors so you have fewer extrapyramidal effects |
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in GENERAL how do the anti-psycho and schizo drugs work
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block receptors
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contraindications for taking typical and atypical antipsychotics
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do NOT use for sedatives (sleep)
do NOT use to treat senile dimensia b/c it will decrease lifespan of elderly do NOT use in combo with CNS depressants |
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what are extrapyramidal effects and what drugs do you have to take to get these effects
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get them from TYPICAL antipsychotics: TCTH
parkinson's like symptoms (b/c blocking DA receptors) dystonias (abnormal movements of face, neck, etc) akathesia (need for constant movement) decrease these symptoms by taking anticholinergics (benztropine) to resore the dopamine:Ach balance |
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effects of typical and atypical antipsychotics
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extrapyramidal (parkinson's like, dystonias, akathesia)
sedation (block histamine rec.) hypotension (block alpha 1 rec.) hypersensitivity messed up eyes (glaucoma b/c block Ach rec., dry eyes) endocrine problems (decreased hormones) neuroleptic malignant syndrome (malignant hyperthermia like the anesthetics cause) dysphoria |
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compare sedation effects of the antipsychotics
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low potency typicals (TC) cause more sedation than high potency typicals (TH)
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long term use of the typical antipsychotics (TCTH) can cause what?
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tardive dyskinesias: IRREVERSIBLE damage to motor areas of the brain leading to "choreoform movements" (whole body weird movements)
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what is the biochemical basis of depression?
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there is a decrease in neurotransmitters in the CNS
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in general what are ways to treat depression
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inhibit reuptake of NE or 5HT (or both)
inhibit MAOa inhibit COMT |
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what are the first generation antidepressants
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"I Am"
Imipramine Amitriptyline |
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2nd generation antidepressants
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the SSRI's
"Flu Season Parrots Flock City Excitement"...think of a flock of parrots flying into a NYC party during flu season fluoxetine, sertraline, paroxetine, fluvoxamine, citalopram, escitalopram |
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3rd generation antidepressants
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the SNRI's "DMV"
duloxetine milnacipram venlofaxine |
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how do the 1st generation anti-depressants work?
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they inhibit reuptake of NE
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side effects of 1st gen. anti-depressants
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they inhibit reuptake of NE...(more side effects than the 2nd and 3rd gen.)
size effects are from blocking other receptors like histamine, alpha 1, Ach: sedation (b/c block histamine receptors) anticholinergic (antimuscarinic) effects: anti-dumbbels CV effects: arrhythmias and decreased bp from blocking alpha 1 receptors |
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MAO inhibitors used to treat depression
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"Tranny's Penis Inside"...think of a depressed tranny. "he/she" is drinking wine and eating cheese which have tyramine (indirect acting amine) causing severe hypertension and "he/she" says "meow" which sounds like MAO
Tranylcypromine Phenelzine Isocarboxazid |
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in children and adolescents, ALL antidepressants may cause increased risk of __________
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suicide
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what are the 6 ways to treat bipolar depression?
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"EALVAC"
ECT (electroconvulsive therapy) antipsychotic drugs (TCTH, CORA) Lithium valproic acid acetazolamide carbamazepine |
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how does lithium work to prevent bipolar disorder
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may block inositol phosphate pathway in CNS
may stabilize a glutamate "setpoint" (with bipolar they have way too much glutamate) |
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people on opiates have _______ pupils
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pin point
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what can opioids TREAT?
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pain, diarrhea, cough
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contraindications to opioids
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undiagnosed pain
head injury convulsive disorder |
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what are side effects of opioids
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pin point pupils
constipation itching can pass through placenta increased CSF pressure |
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do you develop tolerance to opioids?
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only to the anti-pain and euphoria (need to take more of the drug to get these)
but you never develop tolerance to the pin point pupils or constipation (will ALWAYS get these when taking opioids) |
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symptoms of cold turkey withdrawl from opioids
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vasoconstriction
piloerection diarrhea dysphoria restless twitching (can't sit still) dilated pupils insomnia |
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which opioid is 80-100x more potent than morphine?
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fentanyl (or any analog of this like sufentanil)
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which drug is given in a liquid form and used for someone who is trying to get off of heroin?
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methadone
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what are the opioid antagonists
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"Nal" ... "you are NAL free from opioids"
naloxone naltrexone |
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indications for taking opioids
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pain: won't get addicted if used for pain control
diarrhea: loperamide cough: codeine or dextromethorphan (mucinex) |
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which opioid is used to treat diarrhea
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loperamide
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loperamide is used to treat what
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diarrhea (it is an opioid...causes constipation)
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which opioids are used to treat cough
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codeine
dextromethorphan (mucinex) |
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can you get addicted to opioids if you use them for pain control only
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no
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mode of action of caffeine (methylxanthines)
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increase cAMP by inhibiting the enzyme that breaks it down (phosphodiesterase)
INHIBITS ENZYME may act on adenosine receptor |
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what methylxanthine is found in tea
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theophylline
Phil likes tea (the "bros" like cocoa) |
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what methylxanthine is found in cocoa
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theobromine
the bros like cocoa phil likes tea |
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overuse of caffeine can cause what
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chronic poisoning:
sleeplessness tachycardia restlessness GI upset |
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withdrawl from caffeine
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headache
irritation lethargy |
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places caffeine works
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cns: stimulation
cvs: incr. hr sm musc: relaxation (bronchial) kidney: diuretic striated musc: incr. contractility |
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is cocaine an acid or a base
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base
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how is cocaine made to be absorbed easier
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turned into crack by adding bicarbonate which makes the cocaine be in a neutral form which is more readily absorbed
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how can you make sure you piss out the cocaine when you want to get rid of it
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make urine more ACIDIC (by taking vitamin C ...citric acid)
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mechanism of action of cocaine
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reuptake inhibitor of NE, 5HT, DA
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side effects of cocaine
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*hallucinations!
insomnia anxiety nose ulcers urticaria: itching arrythmias |
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what happens if you overuse cocaine
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you decrease the neurotransmitters in the CNS leading to a "crash"
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mode of action of meth (and amphetamine)
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increase release of NE and DA in CNS
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how does the mechanism of action differ between caffeine, cocaine, meth, cannabinoids, and nicotine
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caffeine: increase cAMP by inhibiting phosphodiesterase
cocaine: reuptake inhibitor of NE, 5HT, DA meth: increases release of NE and DA cannabinoids: activate recepor which decreases cAMP nicotine: stimulate nicotinic cholinergic receptors |
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what drug is a partial nicotinic agoinist
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varenicline
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when should you take cannabinoids
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in cancer patients to stimulate hunger and as an anti-emetic also for patients to relieve glaucoma
on saturday nights |
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effects of cannabinoids
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decreases motivation
gets into breast milk causes hunger euphoria anti-emetic (anti-puke) decreases eye pressure bronchodilator dilates bv's in eye (red eyes) anticholinergic effects (like dry mouth) |
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what are the cannabinoid drugs
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"NAB"
dronabinol nabilone |
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what is another name for crack
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free base cocaine...because it puts it in neutral form and makes it absorb more readily
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can cocaine cause hallucinations?
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yes
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