Pharm Flashcards Midterm

Front 1

Simvastatin (Zocor)

Back 1

inhibits HMG-CoA reductase

SE: muscle breakdown

Front 2

Niacin (Niacor)

Back 2

inhibits diacylglycerol acyl-transferase 2

SE: flushing/rashes

Front 3

Clofibrate (N/A)

Back 3

PPAR-alpha agonist

SE: myopathy, arrhythmias

Front 4

Fenofibrate (tricor)

Back 4

PPAR-alpha agonist

SE: myopathy, arrhythmias

Front 5

colestipol (colestid)

Back 5

bind bile acids

SE: GI effects

Front 6

Ezetimibe (Zetia)

Back 6

inhibits cholesterol transporter NPC1L1

SE: GI effects

used with statins as last resort Tx

Front 7

Betahistine (Serc)

Back 7

activates HI receptors

use: vertigo
SE: headache/nausea

Front 8

Dimenhydrinate (Dramamine)

Back 8

inhibits H1 receptors

use: allergy generally
SE: sedation

Front 9

Diphenhydramine (Benadryl)

Back 9

inhibits H1 receptors

use: allergy generally
SE: sedation

Front 10

Hydroxyzine (Atarax)

Back 10

inhibits H1 receptors

use: allergy generally
SE: sedation

Front 11

Bromopheniramine (Dimatapp)

Back 11

inhibits H1 receptors

use: allergy generally
SE: sedation

Front 12

Fexofenadine (Allegra)

Back 12

inhibits H1 receptors

use: allergy generally
SE: sedation

Front 13

Bicarbonates (Alka-Seltzer)

Back 13

neutralizes gastric acid

use: GERD, s/a
SE: metabolic alkalosis

Front 14

aluminum hydroxides (Gaviscon)

Back 14

neutralizes gastric acid

use: GERD, s/a
SE: GI

Front 15

Ranitidine (Zantac)

Back 15

blocks H2-receptors

use: GERD, peptic ulcer, h/b
SE: GI

Front 16

Famotidine (Pepcid)

Back 16

blocks H2-receptors

use: GERD, peptic ulcer, h/b
SE: GI

Front 17

Omeprazol (Prilosec)

Back 17

blocks H/K ATPase pump

use: GERD, peptic ulcer, h/b
SE: GI

Front 18

Pantoprazole (Protium)

Back 18

blocks H/K ATPase pump

use: GERD, peptic ulcer, h/b
SE: GI

Front 19

Sucralfate (Carafate)

Back 19

forms protective barrier

use: ulcers, GI bleeding
SE: GI

Front 20

Misoprostol (Cytotec)

Back 20

prostaglandin receptor agonist

use: NSAID-induced ulcers
SE: GI

Front 21

Bismuth subsalicylate (Pepto Bismol)

Back 21

forms protective barrier

use: ulcers, diarrhea
SE: Reye's syndrome

Front 22

weak bases are ionized, T/F?

Back 22

True, thus more polar and more water soluble

Front 23

weak acids are ionized, T/F?

Back 23

False. Weak acids are not ionized and so are less water soluble when they are protonated

Front 24

RNH3+ <-> RNH2 + H+
Which is more water soluble?

Back 24

RNH3+; it is a protonated weak base and it is charged; RNH2 is an unprotonated weak base that is uncharged and more lipid soluble

Front 25

RCOOH <-> RCOO- + H+
Which is more water soluble?

Back 25

RCOO- because it is an unprotonated weak acid and charged; RCOOH is a protonated weak acid that is uncharged and thsu more lipid soluble

Front 26

permeation

Back 26

movement of drug molecules into biologic environment
-aqueous diffusion
-lipid diffusion
-transport by special carriers
-endocytosis/pinocytosis

Front 27

the smaller the EC50 the greater the potency of the drug, T/F

Back 27

T

Front 28

What is the Kd?

Back 28

the concentration of the drug required to bind 50% of the receptor sites; measures affinity of drug for its binding site on receptor

Front 29

The smaller the Kd the greater the affinity of the drug for its receptor; T/F?

Back 29

T

Front 30

What is EC50?

Back 30

in graded dose response curves, the concentration or dose required that produces 50% of max

Front 31

competitive antagonist

Back 31

binds the receptor in a reversible way without activating the effector system of that receptor (curve will shift to the right-more drug needed to reach max); Effect can be overcome by adding more agonist; competitive antagonists increase the ED50 (agonist appears less potent)

Front 32

irreversible antagonist

Back 32

causes a downward shift of the max with no shift to the curve on the dose axis unless spare receptors are present (reduces max)

Front 33

physiological antagonist

Back 33

drug that binds to a different receptor producing an effect opposite to that produced by drug its antagonizing

Front 34

what if you find that the EC50 of a drug is smaller than the Kd?

Back 34

you have spare receptors

Front 35

Pharmacokinetics is the study of the actions of the body on drugs.

What are the 4 main concepts of pharmacokinetics?

Back 35

MADE
M: metabolism
A: absorbtion
D: distribution
E: excretion

Front 36

What is bioavailibitliy?

how is it measured?

Back 36

bioavailability is the measure of drug in the systemic circulation.

measured by area under the curve (AUC) of blood concentration of drug over time.

Front 37

What is first pass metabolism? (aka presystemic elimination)

Back 37

The elimination of drug that occures before it reaches systemic circulation. (Eg. oral meds in gut/liver)

Front 38

What are the 5 general ways drugs pass cell membranes? (2 passive and 2 active)

Back 38

Passive
1) simple diffusion
2) facilitated diffusion (through specific/nonspecific transporters)

Active
1) pumps
2) pinocytosis

Front 39

What form of the drug penetrates cell membranes best (protonated/unprotonated)?

1) weak bases
2) weak acids

Back 39

Penetrate cell walls best
1) weak bases : unprotonated
2) weak acids : protonated

Front 40

At a LOW pH environment like the stomach, what type of drug (weak acid or weak base) is more able to absorb into cells?

Back 40

At LOW ph : weak acids become protonated and are more able to absorb into cells

weak bases become protonated and are LESS able to be absorbed.

Front 41

In a relatively neutral pH (like blood or the body's aqueous humor), which type of drug is able to be absorbed into cells more readily, weak acid or weak base?

Back 41

WEAK ACID drugs are able to absorb more readily than weak base drugs in neutral pH becasue at pH 7:

weak acids become unprotonated (become uncharged)

weak bases become protonated (become charged)

Front 42

Tissue distribution of a drug depends on what two factors?

Back 42

1) blood perfusion of the tissue
2) the tissue/blood partition ratio (Kp). Kp= Ctissue/Cven-blood (at equilibrium)

Front 43

Rank the following tissues in order of most partition ratio to least partition ractio: Fat, Kidney, Brain

Back 43

MOST to LEAST partition ratio:
1) Kidney
2) Brain
3) Fat

Front 44

What are 5 unique characteristics of CNS capillary endothelia that make it different than most capillary endothelia?

Back 44

1) Tight intercellular junctions
2) Lacks fenestrations
3) minimal pinocytosis
4) drug metabolizing enzymes
5) endothelial drug transporters (efflux into the blood)
6) abundant mitochondria (power efflux pumps)

Front 45

What is VOLUME OF DISTRIBUTION (Vd)?

Back 45

Given a set quantity of drug:
the volume of fluid the drug would need to be dissolved in to match the concentration of the drug in given volume of plasma.

Front 46

How do you experimentally measure (calculate) the Vd for a drug?

Back 46

1) Inject someone with a measured dose of a drug
2) plot plasma concentratio of drug
3) extrapolate time-zero plasma concentration
4) divide the dose by time-zero pasma concentration

Front 47

There are two phases of drug metabolism. what happens in phase 1?

Back 47

Drugs are FUNCTIONALIZED, commonly by oxidaiton, reduction or hydrolysis

Front 48

There are two phases of drug metabolism. What happens in phase 2?

Back 48

The products of phase 1 are CONJUGATED, commonly with endogenous molecules like glucuronic acid.

Front 49

What is metabolic inactivation?

Back 49

converting a pharmacologically active, lipophilic drug to an inactive hydrophilic metabolite (conjugate) which is readily excreted.

Front 50

volume of distribution

Back 50

the ratio of the amount of a drug in the body to its concentration in the plasma or blood

Vd= amt of drug (body)/plasma drug concent.

Front 51

What is metabolic bioactivation?

Back 51

changing a "prodrug" into its pharmacoliogically active form through a metabolic reation

Front 52

clearance

Back 52

the ratio of the rate of elimination of a drug to its concentration in plasma or blood

CL=rate of el of drug/plasma drug concent.

Front 53

half-life

Back 53

time it takes for the amount or concentration of a drug to fall to 50% of an earlier measurement. For drugs eliminated by first order kinetics, this number is a constant regardless of concentration. Half life is not a constant and therefore not particularly useful for drugs eliminated by zero order kinetics (ethanol)

t1/2= 0.693xVd/CL

Front 54

what is metabolic toxicity?

example?

Back 54

Toxic products of drug metabolism.

eg. acetaminophen through CYP2E1 metabolism in liver

Front 55

bioavailaibility

Back 55

the fraction (or %) of the administered dose of a drug that reaches the systemic circulation.

Front 56

AUC

Back 56

the graphic area under a plot of drug concentration in plasma versus time after a single dose of a drug or during a single dosing interval; the AUC is imp for calculating the bioavailability of a drug given by any route other than IV

Front 57

Peak and trough concentration

Back 57

the max and min drug concentrations in plasma or blood measured during cycles of repeated dosing

Front 58

minimum effective concentrations (MEC)

Back 58

the plasma concentration below which a patient's response is too small for therapeutic benefit

Front 59

first pass effect

Back 59

the elimination of drug that occurs after administration but before it reaches the systemic circ

Front 60

steady state

Back 60

in pharmacokinetics the condition in which the average total amount of drug in the body does not change over multiple dosing intervals (rate of drug input equals the rate of elimination)

Front 61

extraction

Back 61

the fraction of adrug in the plasma that is removed by an organ as it passes through that organ

Front 62

bioequivalence

Back 62

the equivalence of blood concentrations of two preparations of the same drug measured over time; if the concentration time plots for hte two preparations are nearly superimposable (within certain statistical limits) teh preparations are said to be bioequivalent; one preparation may be safely substituted for the other. this parameter is used in determining the safety and efficacy of generic drugs

Front 63

biodisposition

Back 63

often used as a synonym for pharmacokinetics; the processes of drug absorption, distribution and elimination

Front 64

What families of P450 enzyme (CYP gene) are responsible for a major portion of drug metabolism?

Back 64

CYP1-3

Front 65

What are three major human liver P450s that metabolize....
1) weakly acidic drugs
2) weakly basic drugs
3) practically everything else

Back 65

1) CYP2C2 : weakly acidic drugs
2) CYP2D6 : weakly basic drugs
3) CYP3A4 : practically everything else

Front 66

What are three major reaction types that occure during phase 1 metabolism?

Back 66

1) oxidation at C, N, S ceneters
2) Reductive Rxns at C, N, S centers
3)Hydrolysis Rxns (of esters and amines)

Front 67

What is enzyme induction?

example?

Back 67

Inc. in steady-state concentrations of an enzyme due to stimulus.

eg (1) inc. in CYP2E1 concentration due to alcoholism (2) Rifampicin induction of P450 -> inc. metabolism (lowers efficacy) of oral contraceptives/warfarin

Front 68

What is enzyme inhibition?

eg?

Back 68

Inhibition is loss or dec. of drug-metabolizing enzyme due to stimulus

eg. grapefruit juice degrades CYP3A4, inhibiting metabolic activation of Felodipine (dihydropyridine Ca channel antagonist) preventing its uptake (higher plasma concentrations)