Term
| Oxidation/hydroxylation (bc it adds and OH group) |
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Definition
most common phase 1 reaction
removal of an electron
oxygen molecule needed
OH added to the compound , H2O produced
become more negative, gain a charge and becomes more water soluble. |
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Term
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Definition
decreased protein states might temporarily increase the free drug.
Usually only significant for drugs that are protein bound. If a drug is not highly protein bound if a drug doesnt have high protein binding then a little bit of change doesn't change the free drug.
Usually think of them as needing to be > 90% protein bound before it makes a difference in low protein states. |
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Term
| When do low protein states occur? |
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Definition
sick people in the hospital
liver failure
kidney failure-typically dont have low protein states but uremia interferes with protein binding. So the protein is there but its not effective in accepting the drug and carrying it around. ** |
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Term
| Elderly pt decreased central bucket/less lean mass. what else is an exception to the normal bucket |
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Definition
| Babies-little sacks of water, they have a greater volume of distribution for water soluble compounds. |
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Term
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Definition
enzyme most often involved in metabolizing our drugs. Primary functions are oxidation and reduction.
FOund everywhere, usually in the endo plasmic reticulum in the liver cells. |
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Term
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Definition
addition of an electron
usually under anaerobic conditions
less common |
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Term
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Definition
super family of Heme proteins,
Heme protein is iron containing protein
Primary purpose processing exogenous compound
Lots of function in the human at all times.
Heme is in a lot of enzymes and hg and mb. |
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Term
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Definition
3A45
gets 50% of our meds
women have more than men
CYP 2D6 **
25% of drugs |
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Term
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Definition
Esters
Hydrolysis
can be in the plasma, tissue, lots of esterase, and ester bond likes to get metabalized.
If they are metabolized by this they are metabolized fast, and not organ dependent. |
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Term
Esterases: Things that do not undergo induction
This are metabolized quick and fast |
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Definition
plasma cholinesterase:
succ
atracurium, cisatracurium
ester locals
mivacurium
esmolol |
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Term
| How would someone up regulate their enzymes? |
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Definition
If these patients up regualte their enzymes you don't have to worry about drugs that are metabolized by esterases.
Alcohol
Seizure disorder patients |
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Term
| Would enzyme induction change your induction dose or maintenance dose? |
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Definition
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Term
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Definition
conjugations
all transferases
glucuronosyltransderase
Glutathione S transferase
N acetyl transferase
Sulfotransferase
Going to transfer a compound onto the molecule |
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Term
| Medium/High Hepatic clearance |
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Definition
flow dependent bc the liver can chew up a constant fraction depending on what you bring to it. You bring a lot of drug with normal liver blood flow it will chew it all up. If you change liver blood flow, you change what it can chew up.
Flow and non flow dependent. |
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Term
Low clearance drugs
*know these |
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Definition
only ones that are NOT flow dependent.
Thiopental
diazepam
lorazepam
rocuronium (use all the time)
methadone
theophylline
Liver blood flow:
hepatic artery and portal vein
during surgery hepatic flow is decrease d. |
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Term
| What changes flow through the portal vein? |
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Definition
Constriction, we would constrict it bc you would want to inc blood flow to the heart so you dec splenic flow by constricting
constricting also happens in stressed states and surgery puts the patient in a stress state
in states of low perfusion drugs that are flow dependent could have a decreased metabolism in states that have decreases blood flow to liver. |
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Term
| Bell Curve jump off point |
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Definition
Mac-minimal alveolar concentration at which half the patients will not move on incision.
Where do I get started not what this patient needs.
May have to adjust opiods up to 5 folds |
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Term
Where do most drug complications from?
Where do most critical incidence in anesthesia come from? |
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Definition
wrong amount of drug for the person
during maintenance, do what the patient needs and stay vigilant. |
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Term
| stereo chemistry..whats the big deal? |
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Definition
enantiomers: identical chemical components exist in mirror images
when nature makes drugs it doesnt make both.
Now we have more and more with 2 types
or stereo specific compounds |
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Term
Enantiomers may have:
inhaled agents: |
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Definition
| Different rates of absorbtion, metabolism , excretion, receptor, one could be theraputic the other could contribute to side effects. RAcemic mixtures. Only ones that aren't racemic mixtures are inhaled agents. |
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Term
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Definition
1. tells us efficacy, how much does it work. You can say which are the most efficacious out of the 3 because they are taller.
2. Potency-which is least potent?
3. Tells us Ed 50
4. what does the slope tell us? steeper the slope=more titratable to drug is.
Where is it working when is it working to our advantage when is it not? |
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Term
| what does a dose response curve NOT tell us? |
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Definition
pharmacokenetic or pharmacodynamin differences.
doesnt talked about potency related to dec protein binding.
To know the differences in dynamics, we need comparison at steady state.
When you compare at steady state you are looking at dynamics and not kinetics. |
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Term
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Definition
works great
l
l
l____________________________not strong strong
not working |
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Term
| nmb and reversals with a dose response curve. |
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Definition
competitive inhibitors
in order to re paralyze your patient after giving a reversal you need to give a whole lot more drug, its going to be all the way out on the line and not as potent, you can still get to same efficacy but it will take a lot more of the dose.
receptor affinity gives you slope of the line and titratablity of the drug, the curve in this case wouldnt change, the only thing that changes is the dose. |
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Term
Line for a drug in the presences of the non competitive inhibitor.
Pt in the emergency room with organophosphate OD, its a non competitive inhibitor, perminantly binds..what will it look like if we give a drug to try and reverse the poisoning. |
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Definition
not as strong and will not reach efficacy. You cant get the drug off its receptor, there to stay so all you can do is give a MUCH larger dose of the new drug and hope receptors are open.
Cant fight the other drug that is already there to reach max efficacy. |
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Term
| Why is dose response curve S shaped instead of linear? |
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Definition
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Term
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Definition
| sits on receptor and doesn't create an action or blocks an action |
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Term
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Definition
| agonist could win if it was stronger |
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Term
| Non competitive antagonist |
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Definition
| agonist cant win, sit on receptor site and stay there, dont have many of these |
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Term
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Definition
binding site is the same,
Ex-narcan and morphine (opiate and narcan) competitive direct antagonist |
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Term
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Definition
binding site is different
alcohol and coffee
nmb and neostygmine. Neostygmine goes to enzyme that breaks down Ach. Direct antagonist is Ach indirect is neostygmine. |
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Term
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Definition
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Term
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Definition
|
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Term
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Definition
| 2 drugs you give together that potentiate each other, more than the sum of the parts. Give drugs from 2 different classes=synergistic |
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Term
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Definition
| decrease effect over time, drugs this happens with opiods..so we have to give more drug |
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Term
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Definition
| rapidly occurring tolerance |
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Term
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Definition
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Term
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Definition
restful sleep, parasympathetic system is dominate
most hormones are cyclic and reach their peaks during sleep.
brain can be more active
motor activity is suppressed if not you could do damage.
inhibits motor movement and sensory responses.
happens 3-4 times a night, brain waves change
Thalamic branch is active and brain patterns can approach normal activity.
Need for restorative cognitive function
pt aren't resting when they don't get this. |
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Term
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Definition
low brain activity levels
m |
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Term
| What turns away from asleep |
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Definition
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Term
| Reticular activating system RAS) |
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Definition
Between upper pons and lower mid brain that is part of the switch to go to sleep.
thalamic and hypothalamic
both are active when you are awake.
both are suppresed in non REM sleep.
In REM sleep thalamic branch is active
2 pathways of sleep and arousal |
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Term
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Definition
includes
locus ceruleus-can suppress the GABA output going to the thalamic branch during REM so could be part of switch that allows thalamic branch to be active when everything else is asleep.
Raphe nucleus
tuberomammillary nucleus
-nor epi, serotonin and histamine
these all include mono amininergice nuerotransmitters
when these are active you get diffuse arousal in the cortex. |
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Term
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Definition
pedunculopontine
laterodorsal tegmental
both produce acetylcholine, which stimulates arousal awake brain patterns |
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Term
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Definition
| monoaminergic hypothalamic branch inhibits VLPO |
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Term
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Definition
| ventrolateral preoptic nucleus (GABA+ Galanin)-->they are active and supress the arousal centers. |
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Term
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Definition
| suppress all wakeful centers |
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Term
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Definition
produce non rem sleep bc they suppress all arousal centers
work on the TMN and VLPO |
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Term
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Definition
| works all the way down at the locus ceruleus, and will allow the brakes to come off the thalamic branch and pt still gets REM sleep |
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Term
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Definition
quiet wakefulness/resting
higher frequency but not as high as beta
8-13 |
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Term
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Definition
highest frequency
wild and crazy, kids look like when they are asleep
Rem sleep jumps right back up here
entropy-chaotic
14-80 |
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Term
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Definition
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Term
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Definition
|
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Term
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Definition
want to decrease as much activity in the brain as possible because they may need to interrupt blood supply to a portion of the brain.
give a bolus dose and see nerve to nerve communication
goal is to stop brain cells from talking to each other, and for a few moments make cells require less oxygen to do their job.
getting the brain down to the lowest possible level for requirement for oxygen with a chemical.
we are stopping nerve to nerve communication |
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