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167 Cards in this Set

  • Front
  • Back
Definition of Pharmacology
the study of the effect of chemicals on living tissue
Pharmacokinetics is...
the study of absorption, distribution, metabolism, and excretion of drugs

(what the body does to the drug)
Pharmaceutics
formulation and preparation of drugs
Pharmacoeconomics
study of the economic impact of drugs
Toxicology
the study of the harmful effects of chemicals
This is the study of the medicinal uses of naturally occurring compounds (from plants and animals)
pharmacognosy
This is the preparation and dispensing of drugs
pharmacy
Pharmacogenetics
genetic influences by and on drugs
Pharmacodynamics
physiological and biochemical mechanism of action of drugs

(What drugs do to the body)
This identifies discrete genetic differences among individuals that play a critical role in drug response
Pharmacogenomics
This is the study of the use and effects of drugs on large groups of people
Pharmacoepidemiology
_____ is the range of medication dosage that effectively treats the majority of the population
Therapeutic window
How many mg are in 2% lidocaine per mL?
20 mg/mL (just add a zero!)
Chemical substances that bind to a specific receptor (proteins) are referred to as ______.
ligands
Two types of ligands:
agonists (bind to receptor and stimulate its function)

antagonists (bind to receptor and block its function)
_____ binding is reversible, and this is found in most drugs. _____ binding is nonreversible, and an example is aspirin.
competitive, noncompetitive

in noncompetitive binding, in order to get rid of the drug's effects, you must make new cells/receptors -- will aspirin, it takes 5-7 days to make more platelets
What does it mean if a receptor is stereospecific?
receptor has a specific shape, and their ligand must have complementary shape, "lock and key"
ED50 means...
effective dose in 50% of the population
TD50 means...
toxic dose in 50% of the pop. -- does not necessarily mean death, but organ damage
LD50 means...
lethal dose in 50% of the pop.
Therapeutic Index =
LD50/ED50

want this number to be as high as possible for drug to be safe

if therapeutic window is narrow (low #) drug is unsafe!
Therapeutic Window =
TD50/ED50

index for estimation of drug dosage which can treat issue effectively while staying within safety range
The Receptor Theory states:
a drug receptor is a macromolecular complex which acts as the site of action for a drug
usually proteins involved in production of normal cellular function
may include membrane proteins, enzymes, carrier molecules, ion channels, nucleic acids
Endogenous Transmitter
body's own ligand that stimulates a receptor
An allosteric agonist or antagonist binds at one location but...
its effects are felt elsewhere.
This is the study of the medicinal uses of naturally occurring compounds (from plants and animals)
pharmacognosy
This is the preparation and dispensing of drugs
pharmacy
Pharmacogenetics
genetic influences by and on drugs
Pharmacodynamics
physiological and biochemical mechanism of action of drugs

(What drugs do to the body)
This identifies discrete genetic differences among individuals that play a critical role in drug response
Pharmacogenomics
List the types of chemical bonds from strongest to weakest
Covalent, Ionic, Hydrogen, Hydrophobic, Van der waals

Pnemonic: Cobras In Hawaii Have Venom!
_____ is the ability of a drug to bind to a receptor, whereas _____ is the ability of a drug to produce a response.
affinity, efficacy
_____ is governed by affinity, whereas ____ is governed by efficacy.
occupation, activation
What is the shape of a dose response curve and what 4 things does it determine?
sigmoidal, determines what dose produces what effect

1. affinity (potency)
2. efficacy
3. variability
4. slope
ED99 is ...
the actual dose recommended for administration
If the LD 50 of a drug is 400 mg, and the ED 50 of a drug is 100 mg, the therapeutic index tells you...
400/100 = 4

it takes 4 x as much to kill you as is needed to produce desired effect
Receptors are (almost always/never) subject to feedback regulation by their own signaling outputs.
almost always
Continued stimulation of cells with agonists generally results in desensitization referred to as ______. Continued or subsequent exposure to same concentration of drug is diminished
down-regulation

decr. in number of receptors during over-stim.
Chronic administration of an antagonist results in ______. The number and sensitivity of receptors increases as a response to chronic blockade.
up-regulation

incr. in number of receptors during under-stim.
Both up-regulation and down-regulation of receptors require:
higher doses of drugs to achieve desired response.
Why can't drug companies do good studies on fetal effects of drugs?
unethical
Most drugs are part of this pregnancy category:
C
Pregnancy Cat A
no risk to fetus, remote possibility of fetal harm
Pregnancy Cat B
no harm shown in animal studies, but no controlled studies done in pregnant women, or animal showed adverse effect not demonstrated in humans
Preg Cat C
studies unavailable, or have shown teratogenic effects, only give if benefit > risk
Why can't drug companies do good studies on fetal effects of drugs?
unethical
Most drugs are part of this pregnancy category:
C
Pregnancy Cat A
no risk to fetus, remote possibility of fetal harm
Pregnancy Cat B
no harm shown in animal studies, but no controlled studies done in pregnant women, or animal showed adverse effect not demonstrated in humans
Preg Cat C
studies unavailable, or have shown teratogenic effects, only give if benefit > risk
Pregnancy Cat D
evidence of human fetal risk, but allowed to use in life-threatening situations and safer drugs cannot be used or are ineffective
Pregnancy Cat X
risk of use in pregnancy clearly outweights benefits, contraindicated in women who are or may become pregnant
The percentage of a drug contained in a drug product that enters systemic circulation in unchanged form after administration is called _____. (includes both amt. of drug and rate of entry)
bioavailability
______ refers to the alteration in the therapeutic action of a drug by concurrent administration of other exogenous chemicals.
interaction
1+1=2
addition: combined effect of 2 drugs acting via same mechanism is equal to that expected by simple addition of each's actions
1+1=3
synergism: the combined effect of 2 drugs together is greater than each's individual effects
1+0=3
potentiation: enhancement of action of one drug by a second drug that has no detectable action of its own
ex: pcn and probenacid -- PCN is antibiotic and probenacid prevents drug from being excreted by kidneys so that its actions stay longer
1+1=0
antagonism: action of one drug opposes that of the other
ex: morphine and narcan
If something is ionized, it is ________ soluble, whereas something that is unionized is ________ soluble.
water soluble, lipid soluble
what is pKa?
the ionization constant of a chemical compound -- the pH at which the drug will exist in olution as 50%ionized and 50% non-ionized
All drugs are salts of a weak ____ or _____.
acid, base
If a drug has a charge and is ionized, it is 100% (water/lipid) soluble, and (will/won't) make it to bloodstream unless given in IV, thus making it easier to eliminate.
water, won't
If a drug has no charge (unionized), it is 100% (water/lipid) soluble and (will/won't) cross the blood brain barrier or placenta, thus making it harder to eliminate.
lipid, will
Can you use regional anesthesia in an acidotic limb?
NO
if pH > pKa,
drug is basic
if pH <pKa,
drug is acidic
If pH-pKa =0
50% will be ionized and 50% will be unionized
If pH-pKa=0.5,
75%/25% ionized/unionized
if pH-pKa=1,
99%/1% ionized, unionized
An acid drug in an acid pH will be (ionized/unionized).
unionized
A base drug in an acid pH will be (ionized/unionized)
ionized
Find solubility: Drug A is an acid compound with pKa 7.1, placed into acid environment pH 6.0....
7.1-6.0=1.1

99/1

99% non-ionized/1% ionizied

lipid soluble!
pKa does not measure acid base status, rather the extent of:
ionization
In bases:
pH>pKa ____ predominates
pH=pKa ____
pH<pKa ____ predominates
nonionized,
nonionized=ionized
ionized
pg 20 workbook
In acids:
pH>pKa ____ predominates
pH=pKa _____
pH<pKa____ predominates
ionized
non-ionized=ionized
non-ionized
pg 20 workbook
For acidic drugs:
pH-pKa<0 means:
pH-pKa>0 means:
nonionized, ionized
For basic drugs:
pKa-pH<0 means:
pKa-pH>0 means:
nonionized, ionized
Lipophilic drugs are metabolized to form more ____ metabolites than parent drugs, making metabolites more easily excreted.
hydrophilic/water-soluble
Grapefruit juice changes the _____ of a drug, whether it is the drug or its metabolites that take action, this value will change what pt was intended to _____.
bioavailability, absorb

grapefruit juice selectively inhibits CYP3A in enterocytes
_____ refers to when drugs, environmental chemicals, air pollutants, and components or cigarette smoke stimulate synthesis and elevate level of hepatic drug-metabolizing enzymes
enzyme induction
Enzyme inhibitions occurs when:
a substance cause less metabolism of a drug, leading to incr. in their effects
Because nonionized drug molecules are ____ soluble, they can diffuse across _______ such as the blood-brain, gastric, and placental barriers to reach the effect site.
lipid, cell membranes
____ molecules/drugs are usually unable to penetrate lipid cel membranes easily because of their low ___ solubility. This results from the electric charges exerted by the ______ drug molecules.
Ionized, lipid, ionized
The (higher/lower) the degree of ionization, the less access the drug has across tissues such as GI tract, blood-brain and placental barriers.
higher
Oral drugs that are ionized (will/won't) be metabolized by the liver, and are commonly excreted through the _____ system.
won't, renal
Acids are proton ____ and bases are proton ____.
donors, recipients
When pH and pKa are equal, the drug will be...
50% ionized/50% unionized
This equation determines a drug's state of ionization:
henderson-hasselbach
A ganglion is:
a collection of nerve cells outside of CNS
A parasympathetic receptor for acetylcholine is called _____ and may be ____ at ganglion synapse or _____ at effector organ synapse.
cholinergic, nicotinic, muscarinic
A sympathetic receptor for adrenaline (norepinephrine) is called _____ at the effector organ synapse.
adrenergic
At the tissue site, sympathomimetic drugs do this:
mimic norepinephrine and stimulate alpha, beta, or dopamine receptors
At the tissue site, sympatholytic drugs:
block adrenergic receptors
At the tissue site, parasympathomimetic drugs:
mimic Acetylcholine (Ach)
At the tissue site, parasympatholytic drugs:
block muscarinic cholinergic receptors.
If the effector organ is the heart, sympathetic stimulation ______ whereas parasympathetic stimulation ____.
speeds up, slows down
Beta blockers inhibit
sympathetic adrenergic receptors
Atropine is a ______, therefore it _____ HR.
parasympatholytic, anticholinergic, antimuscarinic
anticholinergic is the same as
antimuscarinic
Inhaled anesthetics are great for _____ but poor at _____.
anesthetia/amnesia, analgesia
In abdominal surgery, Total muscle relaxation is important for:
prevention of evisceration

and also "table glue" =)
Objective of general anesthesia:
reduce sensory awareness and suppress reflexes sufficiently to permit surgery
Stage 1 of anesthesia
awake to loss of consciousness (hypnosis), "analgesia"
Stage 2 of anesthesia
"excitement,"
amnesia, cv instability and excitation, emesis, dysconjugate occular movements
Stage 3 of anesthesia
"surgical anesthesia,"
movement in response to pain is suppressed, 4 planes
Stage 4 of anesthesia
"medullary paralysis, death,"
cessation of spontaneous respiration and medullary cardiac reflexes can lead ot death
4 planes of stage 3 anesthesia:
1. deep respiration, coordinated thoracic and diaphragmatic muscle activity, papillary constriction
2. diminished respiration, fixed midline and dilated pupils
3. continued diaphragmatic mvmt, diminished thoracic mvmt, further papillary dilation
4. thoracic immobility, diminished diaphragmatic mvmt.
General character and relative duration of stages are same for all IAs, but ____ and _____ differ.
speed of induction, details of signs
Stage one ends when....
pt loses consciousness!
3 planes of stage 1:
1. no amnesia/analgesia
2. total amnesia partial analgesia
3. total amnesia and analgesia, skin incision feels like blunt instrument dragged across skin
Scary things about stage 2:
- violent/combative behavior
- struggling
- muscle tone increase
- jaw sets
- breath holding and retching
- nystagmus
Corneal reflex and laryngeal reflex are lost during this stage, making it a good time for intubation:
stage 3 plane 2
Hypotension and tachycardia are seen starting in this stage:
stage 3, plane 3
Stage 3 begins with the onset of....
regular rhythmic respiration
It's easier to (inhibit/excite) with drugs
inhibit!
Disinhibition
causes intense paranoia and fear, pt psychologically reacts, frequently caused by droperidol
Greatest danger during stage 2:
during emergence, pt can suck back against a closed glottis, creating a negative pressure in the lungs --> flash noncardiogenic pulm edema, treat with reintubation and PEEP, common in YOUNG HEALTHY MALES, will see pink frothy sputum
The more complex the brain function, the (Easier/harder) it is to knock it out w a drug
easier!
The more simple the brain function, the (easier/harder) it is to knock it out w a drug
harder!

w/ neuro injury, brain stem function is last to go
Sequence for loss of reflexes:
lips to lungs
oral reflexes go first
Children require (lower/higher) MAC than adults, but also go to sleep (slower/faster), this is due to:
higher MAC, sleep faster, due to incr. metabolism, HR, RR
This is the plane of stage 3 where corneal reflex is lost:
stage 3 plane 3
This is the plane of stage 3 of anesthesia when pupillary light reflex disappears:
stage 3 plane 4
These reflexes are the strongest and last to go:
corina and bronchial
2 questions when deciding to extubate:
1. can they breathe without the tube?
2. will they vomit/aspirate? (swallow and gag, trying to protect airway)
Patients must be deeper for which: intubation or surgical incision?
intubation!
Fi means
inspired gas concentration (%)

determined by FGF, breathing circuit volume, circuit absorption
FA means
alveolar gas concentration

determined by uptake, ventillation, concentration effect, second gas effect
Fa means
arterial gas concentration

affected by V/Q mismatching
Due to shunting in the lungs during anesthesia, minimum fi02 must always be
30%
MAC means
minimum alveolar concentration required to achieve surgical anesthesia (Stage 3)
lung (Alveolar) concentration =
brain concentration
This makes an anesthetic faster:
low blood gas coefficient
Machine factors:
1. liter flow (the higher the gas flow, faster the pt sleeps)
2. absorption into plastic
Lung Factors:
1. ventilation
2. concentration
3. blood gas solubility
4. v/q problems
5. second gas effect
6. n20 diffusions into closed spaces
Blood Factors:
Cardiac output

central compartment/vessel-rich/vital organs go to sleep first because they receive 75% of c.o., (Then muscle, then fat)

increases in CO sow speed of induction

CO affects slow-acting IAs more
Tissue Factors:
1. oil/gas solubility
2. metabolism
3. diffusion hypoxia
4. pediatrics (go to sleep faster even though MAC is higher, peaks at 6 mo.)
5. obesity (induction time is the same but longer for emergence -- depot/reservoir effect)
6. hypothermia (slower elimination of anesthetics, slower emergence)
Ventilation: The faster you breathe, the (Faster/slower) you go to sleep
faster
Concentration: as you increase dose, the drug works (faster/slower)
faster
Blood gas solubility: the (lower/higher) the b.g. coefficient, the faster the drug works
lower
V/Q problems: bad lungs/one lung/CLD (slows/speeds) delivery of anesthetics, and therefore (slows/speeds) drugs
slows, slows

faster drugs have a more pronounced slowing effect
second gas effect: if you give 2 gases together (1 fast and 1 slow), the slow drug will go in (Faster/same speed) than normally, and occurs during this part of case _____.
faster, occurs during beginning (First 5 min) of case
N20 diffusions into closed spaces: N20 (contracts/expands) more than air, which will (increase/decrease) pressure in a closed space.
expands, increase

incr. size of air emboli, pneumothorax, etc
oil/gas solubility indicates this:
potency

increased number means increased potency
all IA metabolism is trace except for this drug:
sevoflurane/ultane
5-7%
diffusion hypoxia means...
high concentration used for n20 causes high exiting concentration through lungs, requiring 3-5 min of 100% fi02 at end of case to prevent hypoxia
MAC 50 is used for _____, and is the minimum alveolar concentration required to achieve surgical anesthesia/immobility in 50% of pts
maintenance
Relationship between MAC and dose:
inversely proportional -- higher # of mac means lower dose is required
MAC awake:
alveolar concentration of anesthetic that inhibits responses to command in half of pts (open eyes)
MAC bar:
alveolar concentration wher autonomic responses are blocked, 1.6x higher tan MAC 50
Partition coefficient: Sevoflurane
MAC 2
b/g 0.6
oil/gas 50
Partition coefficient:
Isoflurane
MAC 1.15
b/g 1.4
o/g 99
Partition coefficient:
N20
MAC 105
B/G 0.47
O/G 1.4
Partition coefficient:
Desflurane (suprane)
MAC 5.8
b/g 0.42
o/g 18.7
this is the number 1 trigger for malignant hyperthermia:
inhaled anesthetics/volatile gases!
oil gas coefficient indicates:
potency
increased # means increased potency!
low solubility means:
fast in fast out
high solubility means:
slow in slow out
this IA cant be used for mask induction because it causes coughing and tastes caustic
desflurane

use sevoflurane instead!
blood gas coefficient means the number of molecules of a drug stay in the blood for every 1 molecule that...
leaves the blood
the (higher/lower) the b/g coefficient, the (Faster/slower) the rise of anesthetic in the lungs
lower, faster
n20 is faster than desflurane in spite of a higher b/g coefficient due to:
the concentration effect
N20 expansion in closed spaces can be deleterious when:
pneumothorax
bowel obstruction
inner ear sx
neurosurg procedures w air injection
air embolism
within 4 wks of use of sulfur hexafluoride gas injection in occural sx
laparoscopy

can lead to expansion of PA cath balloon or ETT cuff volume
(Increases/decreases) in CO slow the onset of all anesthetics; (highest/lowest) blood gas agents are affected the most.
increases, highest
If blood is moving slowly during decreased CO, it has this effect:
more time to exchange gas and higher alveolar levels
max fiN20 used during anesthesia:
70%
What is the effect of pregnancy on anesthesia?
both CO and Minute ventilation are increased in pregnant women --> offset each other and rate of rise of IA is similar to nonpregnant people