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167 Cards in this Set
- Front
- Back
Definition of Pharmacology
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the study of the effect of chemicals on living tissue
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Pharmacokinetics is...
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the study of absorption, distribution, metabolism, and excretion of drugs
(what the body does to the drug) |
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Pharmaceutics
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formulation and preparation of drugs
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Pharmacoeconomics
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study of the economic impact of drugs
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Toxicology
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the study of the harmful effects of chemicals
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This is the study of the medicinal uses of naturally occurring compounds (from plants and animals)
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pharmacognosy
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This is the preparation and dispensing of drugs
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pharmacy
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Pharmacogenetics
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genetic influences by and on drugs
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Pharmacodynamics
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physiological and biochemical mechanism of action of drugs
(What drugs do to the body) |
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This identifies discrete genetic differences among individuals that play a critical role in drug response
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Pharmacogenomics
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This is the study of the use and effects of drugs on large groups of people
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Pharmacoepidemiology
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_____ is the range of medication dosage that effectively treats the majority of the population
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Therapeutic window
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How many mg are in 2% lidocaine per mL?
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20 mg/mL (just add a zero!)
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Chemical substances that bind to a specific receptor (proteins) are referred to as ______.
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ligands
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Two types of ligands:
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agonists (bind to receptor and stimulate its function)
antagonists (bind to receptor and block its function) |
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_____ binding is reversible, and this is found in most drugs. _____ binding is nonreversible, and an example is aspirin.
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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 |
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What does it mean if a receptor is stereospecific?
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receptor has a specific shape, and their ligand must have complementary shape, "lock and key"
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ED50 means...
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effective dose in 50% of the population
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TD50 means...
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toxic dose in 50% of the pop. -- does not necessarily mean death, but organ damage
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LD50 means...
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lethal dose in 50% of the pop.
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Therapeutic Index =
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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! |
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Therapeutic Window =
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TD50/ED50
index for estimation of drug dosage which can treat issue effectively while staying within safety range |
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The Receptor Theory states:
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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 |
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Endogenous Transmitter
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body's own ligand that stimulates a receptor
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An allosteric agonist or antagonist binds at one location but...
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its effects are felt elsewhere.
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This is the study of the medicinal uses of naturally occurring compounds (from plants and animals)
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pharmacognosy
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This is the preparation and dispensing of drugs
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pharmacy
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Pharmacogenetics
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genetic influences by and on drugs
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Pharmacodynamics
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physiological and biochemical mechanism of action of drugs
(What drugs do to the body) |
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This identifies discrete genetic differences among individuals that play a critical role in drug response
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Pharmacogenomics
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List the types of chemical bonds from strongest to weakest
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Covalent, Ionic, Hydrogen, Hydrophobic, Van der waals
Pnemonic: Cobras In Hawaii Have Venom! |
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_____ is the ability of a drug to bind to a receptor, whereas _____ is the ability of a drug to produce a response.
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affinity, efficacy
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_____ is governed by affinity, whereas ____ is governed by efficacy.
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occupation, activation
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What is the shape of a dose response curve and what 4 things does it determine?
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sigmoidal, determines what dose produces what effect
1. affinity (potency) 2. efficacy 3. variability 4. slope |
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ED99 is ...
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the actual dose recommended for administration
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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...
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400/100 = 4
it takes 4 x as much to kill you as is needed to produce desired effect |
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Receptors are (almost always/never) subject to feedback regulation by their own signaling outputs.
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almost always
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Continued stimulation of cells with agonists generally results in desensitization referred to as ______. Continued or subsequent exposure to same concentration of drug is diminished
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down-regulation
decr. in number of receptors during over-stim. |
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Chronic administration of an antagonist results in ______. The number and sensitivity of receptors increases as a response to chronic blockade.
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up-regulation
incr. in number of receptors during under-stim. |
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Both up-regulation and down-regulation of receptors require:
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higher doses of drugs to achieve desired response.
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Why can't drug companies do good studies on fetal effects of drugs?
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unethical
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Most drugs are part of this pregnancy category:
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C
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Pregnancy Cat A
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no risk to fetus, remote possibility of fetal harm
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Pregnancy Cat B
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no harm shown in animal studies, but no controlled studies done in pregnant women, or animal showed adverse effect not demonstrated in humans
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Preg Cat C
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studies unavailable, or have shown teratogenic effects, only give if benefit > risk
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Why can't drug companies do good studies on fetal effects of drugs?
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unethical
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Most drugs are part of this pregnancy category:
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C
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Pregnancy Cat A
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no risk to fetus, remote possibility of fetal harm
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Pregnancy Cat B
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no harm shown in animal studies, but no controlled studies done in pregnant women, or animal showed adverse effect not demonstrated in humans
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Preg Cat C
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studies unavailable, or have shown teratogenic effects, only give if benefit > risk
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Pregnancy Cat D
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evidence of human fetal risk, but allowed to use in life-threatening situations and safer drugs cannot be used or are ineffective
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Pregnancy Cat X
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risk of use in pregnancy clearly outweights benefits, contraindicated in women who are or may become pregnant
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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)
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bioavailability
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______ refers to the alteration in the therapeutic action of a drug by concurrent administration of other exogenous chemicals.
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interaction
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1+1=2
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addition: combined effect of 2 drugs acting via same mechanism is equal to that expected by simple addition of each's actions
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1+1=3
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synergism: the combined effect of 2 drugs together is greater than each's individual effects
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1+0=3
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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 |
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1+1=0
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antagonism: action of one drug opposes that of the other
ex: morphine and narcan |
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If something is ionized, it is ________ soluble, whereas something that is unionized is ________ soluble.
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water soluble, lipid soluble
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what is pKa?
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the ionization constant of a chemical compound -- the pH at which the drug will exist in olution as 50%ionized and 50% non-ionized
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All drugs are salts of a weak ____ or _____.
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acid, base
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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.
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water, won't
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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.
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lipid, will
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Can you use regional anesthesia in an acidotic limb?
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NO
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if pH > pKa,
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drug is basic
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if pH <pKa,
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drug is acidic
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If pH-pKa =0
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50% will be ionized and 50% will be unionized
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If pH-pKa=0.5,
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75%/25% ionized/unionized
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if pH-pKa=1,
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99%/1% ionized, unionized
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An acid drug in an acid pH will be (ionized/unionized).
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unionized
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A base drug in an acid pH will be (ionized/unionized)
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ionized
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Find solubility: Drug A is an acid compound with pKa 7.1, placed into acid environment pH 6.0....
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7.1-6.0=1.1
99/1 99% non-ionized/1% ionizied lipid soluble! |
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pKa does not measure acid base status, rather the extent of:
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ionization
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In bases:
pH>pKa ____ predominates pH=pKa ____ pH<pKa ____ predominates |
nonionized,
nonionized=ionized ionized pg 20 workbook |
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In acids:
pH>pKa ____ predominates pH=pKa _____ pH<pKa____ predominates |
ionized
non-ionized=ionized non-ionized pg 20 workbook |
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For acidic drugs:
pH-pKa<0 means: pH-pKa>0 means: |
nonionized, ionized
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For basic drugs:
pKa-pH<0 means: pKa-pH>0 means: |
nonionized, ionized
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Lipophilic drugs are metabolized to form more ____ metabolites than parent drugs, making metabolites more easily excreted.
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hydrophilic/water-soluble
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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 _____.
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bioavailability, absorb
grapefruit juice selectively inhibits CYP3A in enterocytes |
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_____ refers to when drugs, environmental chemicals, air pollutants, and components or cigarette smoke stimulate synthesis and elevate level of hepatic drug-metabolizing enzymes
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enzyme induction
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Enzyme inhibitions occurs when:
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a substance cause less metabolism of a drug, leading to incr. in their effects
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Because nonionized drug molecules are ____ soluble, they can diffuse across _______ such as the blood-brain, gastric, and placental barriers to reach the effect site.
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lipid, cell membranes
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____ 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.
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Ionized, lipid, ionized
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The (higher/lower) the degree of ionization, the less access the drug has across tissues such as GI tract, blood-brain and placental barriers.
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higher
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Oral drugs that are ionized (will/won't) be metabolized by the liver, and are commonly excreted through the _____ system.
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won't, renal
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Acids are proton ____ and bases are proton ____.
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donors, recipients
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When pH and pKa are equal, the drug will be...
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50% ionized/50% unionized
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This equation determines a drug's state of ionization:
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henderson-hasselbach
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A ganglion is:
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a collection of nerve cells outside of CNS
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A parasympathetic receptor for acetylcholine is called _____ and may be ____ at ganglion synapse or _____ at effector organ synapse.
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cholinergic, nicotinic, muscarinic
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A sympathetic receptor for adrenaline (norepinephrine) is called _____ at the effector organ synapse.
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adrenergic
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At the tissue site, sympathomimetic drugs do this:
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mimic norepinephrine and stimulate alpha, beta, or dopamine receptors
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At the tissue site, sympatholytic drugs:
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block adrenergic receptors
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At the tissue site, parasympathomimetic drugs:
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mimic Acetylcholine (Ach)
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At the tissue site, parasympatholytic drugs:
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block muscarinic cholinergic receptors.
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If the effector organ is the heart, sympathetic stimulation ______ whereas parasympathetic stimulation ____.
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speeds up, slows down
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Beta blockers inhibit
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sympathetic adrenergic receptors
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Atropine is a ______, therefore it _____ HR.
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parasympatholytic, anticholinergic, antimuscarinic
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anticholinergic is the same as
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antimuscarinic
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Inhaled anesthetics are great for _____ but poor at _____.
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anesthetia/amnesia, analgesia
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In abdominal surgery, Total muscle relaxation is important for:
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prevention of evisceration
and also "table glue" =) |
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Objective of general anesthesia:
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reduce sensory awareness and suppress reflexes sufficiently to permit surgery
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Stage 1 of anesthesia
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awake to loss of consciousness (hypnosis), "analgesia"
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Stage 2 of anesthesia
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"excitement,"
amnesia, cv instability and excitation, emesis, dysconjugate occular movements |
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Stage 3 of anesthesia
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"surgical anesthesia,"
movement in response to pain is suppressed, 4 planes |
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Stage 4 of anesthesia
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"medullary paralysis, death,"
cessation of spontaneous respiration and medullary cardiac reflexes can lead ot death |
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4 planes of stage 3 anesthesia:
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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. |
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General character and relative duration of stages are same for all IAs, but ____ and _____ differ.
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speed of induction, details of signs
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Stage one ends when....
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pt loses consciousness!
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3 planes of stage 1:
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1. no amnesia/analgesia
2. total amnesia partial analgesia 3. total amnesia and analgesia, skin incision feels like blunt instrument dragged across skin |
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Scary things about stage 2:
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- violent/combative behavior
- struggling - muscle tone increase - jaw sets - breath holding and retching - nystagmus |
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Corneal reflex and laryngeal reflex are lost during this stage, making it a good time for intubation:
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stage 3 plane 2
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Hypotension and tachycardia are seen starting in this stage:
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stage 3, plane 3
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Stage 3 begins with the onset of....
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regular rhythmic respiration
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It's easier to (inhibit/excite) with drugs
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inhibit!
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Disinhibition
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causes intense paranoia and fear, pt psychologically reacts, frequently caused by droperidol
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Greatest danger during stage 2:
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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
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The more complex the brain function, the (Easier/harder) it is to knock it out w a drug
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easier!
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The more simple the brain function, the (easier/harder) it is to knock it out w a drug
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harder!
w/ neuro injury, brain stem function is last to go |
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Sequence for loss of reflexes:
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lips to lungs
oral reflexes go first |
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Children require (lower/higher) MAC than adults, but also go to sleep (slower/faster), this is due to:
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higher MAC, sleep faster, due to incr. metabolism, HR, RR
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This is the plane of stage 3 where corneal reflex is lost:
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stage 3 plane 3
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This is the plane of stage 3 of anesthesia when pupillary light reflex disappears:
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stage 3 plane 4
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These reflexes are the strongest and last to go:
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corina and bronchial
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2 questions when deciding to extubate:
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1. can they breathe without the tube?
2. will they vomit/aspirate? (swallow and gag, trying to protect airway) |
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Patients must be deeper for which: intubation or surgical incision?
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intubation!
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Fi means
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inspired gas concentration (%)
determined by FGF, breathing circuit volume, circuit absorption |
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FA means
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alveolar gas concentration
determined by uptake, ventillation, concentration effect, second gas effect |
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Fa means
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arterial gas concentration
affected by V/Q mismatching |
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Due to shunting in the lungs during anesthesia, minimum fi02 must always be
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30%
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MAC means
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minimum alveolar concentration required to achieve surgical anesthesia (Stage 3)
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lung (Alveolar) concentration =
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brain concentration
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This makes an anesthetic faster:
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low blood gas coefficient
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Machine factors:
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1. liter flow (the higher the gas flow, faster the pt sleeps)
2. absorption into plastic |
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Lung Factors:
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1. ventilation
2. concentration 3. blood gas solubility 4. v/q problems 5. second gas effect 6. n20 diffusions into closed spaces |
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Blood Factors:
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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 |
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Tissue Factors:
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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) |
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Ventilation: The faster you breathe, the (Faster/slower) you go to sleep
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faster
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Concentration: as you increase dose, the drug works (faster/slower)
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faster
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Blood gas solubility: the (lower/higher) the b.g. coefficient, the faster the drug works
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lower
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V/Q problems: bad lungs/one lung/CLD (slows/speeds) delivery of anesthetics, and therefore (slows/speeds) drugs
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slows, slows
faster drugs have a more pronounced slowing effect |
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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 _____.
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faster, occurs during beginning (First 5 min) of case
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N20 diffusions into closed spaces: N20 (contracts/expands) more than air, which will (increase/decrease) pressure in a closed space.
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expands, increase
incr. size of air emboli, pneumothorax, etc |
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oil/gas solubility indicates this:
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potency
increased number means increased potency |
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all IA metabolism is trace except for this drug:
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sevoflurane/ultane
5-7% |
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diffusion hypoxia means...
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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
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MAC 50 is used for _____, and is the minimum alveolar concentration required to achieve surgical anesthesia/immobility in 50% of pts
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maintenance
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Relationship between MAC and dose:
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inversely proportional -- higher # of mac means lower dose is required
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MAC awake:
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alveolar concentration of anesthetic that inhibits responses to command in half of pts (open eyes)
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MAC bar:
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alveolar concentration wher autonomic responses are blocked, 1.6x higher tan MAC 50
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Partition coefficient: Sevoflurane
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MAC 2
b/g 0.6 oil/gas 50 |
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Partition coefficient:
Isoflurane |
MAC 1.15
b/g 1.4 o/g 99 |
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Partition coefficient:
N20 |
MAC 105
B/G 0.47 O/G 1.4 |
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Partition coefficient:
Desflurane (suprane) |
MAC 5.8
b/g 0.42 o/g 18.7 |
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this is the number 1 trigger for malignant hyperthermia:
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inhaled anesthetics/volatile gases!
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oil gas coefficient indicates:
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potency
increased # means increased potency! |
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low solubility means:
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fast in fast out
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high solubility means:
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slow in slow out
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this IA cant be used for mask induction because it causes coughing and tastes caustic
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desflurane
use sevoflurane instead! |
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blood gas coefficient means the number of molecules of a drug stay in the blood for every 1 molecule that...
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leaves the blood
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the (higher/lower) the b/g coefficient, the (Faster/slower) the rise of anesthetic in the lungs
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lower, faster
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n20 is faster than desflurane in spite of a higher b/g coefficient due to:
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the concentration effect
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N20 expansion in closed spaces can be deleterious when:
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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 |
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(Increases/decreases) in CO slow the onset of all anesthetics; (highest/lowest) blood gas agents are affected the most.
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increases, highest
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If blood is moving slowly during decreased CO, it has this effect:
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more time to exchange gas and higher alveolar levels
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max fiN20 used during anesthesia:
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70%
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What is the effect of pregnancy on anesthesia?
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both CO and Minute ventilation are increased in pregnant women --> offset each other and rate of rise of IA is similar to nonpregnant people
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