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Pharmacology 680 > Pharmacokinetics and Pharmacology Review > Flashcards

Pharmacokinetics and Pharmacology Review Flashcards

1
Q

pharmacodynamics

A

the drug’s effect on the body, therapeutic and toxic

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2
Q

agonist

A

substance that binds to a specific receptor and triggers a response in the cell.

mimics the actin of an endogenous ligand that binds to the same receptor

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3
Q

Full agonist

A

maximal activation of all receptors

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4
Q

partial agonist

A

can block some receptors while effecting other receptors
agonist-antagonist - have both agonist and antagonist effects
activates a receptor but cant produce a maximum response

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5
Q

antagonist

A
  • drug that has affinity for the receptor but no efficacy
  • combination with receptor may block a response
  • higher affinity for receptor
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6
Q

physiologic antagonism

A

two agonists drugs that bind to different receptors causing opposing responses

ex: phenylephrine vs cardene

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7
Q

chemical antagonism

A

no receptor activity is involved. One drug binds with the second drug to inactivate it

ex: protamine and heparin

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8
Q

receptor

A

the component of a cell that interacts with a drug and initiates the chain of events leading to the drug’s effect

-may be membrane bound, intracellular proteins (caffeine, insulin, steroids, theophylline, milrinone), or circulating proteins (coag cascade)

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9
Q

affinity

A

the degree of drug receptor interaction for a given drug - potency -

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10
Q

efficacy

A

-intrinsic activity- a drug’s ability to produce the desired response expected by stimulation of a given receptor, the max effect that can be achieved with the drug

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11
Q

spare receptor concept

A

not all receptors have to be covered to work

-maximal or nearly maximal response can often be produced by activations of only a fraction of the receptors present

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12
Q

down regulation

A

desensitization - occurs with continued stimulation of cells with agonists - the effect is diminished

ex: beta agonist bronchodilators - tolerance develops from repeated use, increased dose will be required

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13
Q

up regulation

A

chronic exposure to antagonists cause receptor number and sensitivity to increase

ex: beta blockers

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14
Q

drugs that don’t act on proteins

A

sodium citrate
chelating drugs
iodine
sodium bicarb

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15
Q

What causes variability of pharmacologic response

A 
age
sex
body weight - kg and ideal body weight
body surface area
basal metabolic rate - temp affects
pathologic state
genetic profile
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16
Q

pharmicokinetics

A

the actions of the body on the drug

absorption, distribution, metabolism, elimination

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17
Q

absorption

A

Route - PO, IM, IV, rectal

first pass effect - PO and rectal pass through liver first which extracts and/or metabolizes some of the drug

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18
Q

bioavailability

A

the extent to which a drug reaches it effect site after its introduction into the circulatory system
affected by lipid solubility, solubility in aqueous and organic solvents, molecular weight, pH, pKa, and blood flow

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19
Q

distribution

A

(alpha phase) the plasma concentration of the drug declines

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20
Q

two compartment model

A

distribution phase – decrease in plasma level – elimination phase

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21
Q

redistribution

A

termination of effect
plasma level decreases to the point that the drug moves out of the vessel rich central group and is then taken into the peripheral group

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22
Q

elimination

A

beta phase

involves metabolism and excretion, clearance of drug

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23
Q

Vessel rich

A

brain, heart, liver, kidney, endocrine

receives 75% of cardiac output (only 10% body mass)

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24
Q

lean muscle

A

muscle and skin

receives 19% of cardiac output (50% body mass)

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25
Q

fat

A

receives 6% of cardiac output (20% body mass)

26
Q

vessel poor

A

bone ligament and cartilage

receives 0% of cardiac output (20% body mass)

27
Q

metabolism pathways

A

oxidation
reduction
hydrolysis
conjugation

28
Q

Phase 1 metabolism

A

oxidation, reduction, hydrolysis

increases the drugs polarity

29
Q

phase 2 metabolism

A

conjugation
drug or metabolites are covalently linked to a highly ionized molecule
the resulting conjugate is more water soluble for excretion

30
Q

sites of metabolism

A 
hepatic microsomal enzymes
plasma - hoffmann elimination
lungs
kidneys
GI tract
31
Q

cytochrome P450 enzymes

A

hepatic microsomal enzymes mostly

oxidative metabolism of most drugs

32
Q

enzyme induction

A

the ability of drugs or chemicals to stimulate activity of the cytochrome p450 system
may be due to increased synthesis of cytochrome p450 and cyt p450 reductase
can be revved up

33
Q

noncytochrome p450 enzymes (esters)

A

nonmicrosomal enzymes
metabolism by conjugation, hydrolysis, and some oxidation and reduction
largely in liver and some GI
not inducable, genetically determined.

34
Q

phase 1 enzymes

A

cytochrome p450
nonmicrosomal enzymes
noncytochrome p450 enzymes (esters)

35
Q

phase 2 enzymes

A

glucoronosyltransferases
gluthathione-s-transferases
n-acetyl-transferases
sulfotransferases

36
Q

what meds metabolized by glucoronosyltransferase

A

morphine, propofol, and midalozam

37
Q

n-acetyl-transferases

A

have fast and slow acetylators

slow acetylators are at greater risk for side effects because you dont metabolize drugs as fast

38
Q

gluthione-s-transferases

A

a defensive system for detoxification and protection against oxidative stress

39
Q

elimination 1/2 life

A

the time for the drug in the plasma to decrease by 50%

affected by volume of distribution and changes in clearance

40
Q

context sensitive half time

A

the time for the plasma drug concentration to decrease 50% after discontinuing a continuous infusion of a specific duration
(the longer the infusion the longer the half time)

41
Q

effect-site equilibration time

A

the time between IV injection into the plasma and the delivery of the drug to its site of action
important to consider for redosing, don’t want to redose if drug hasn’t made it to site of side effect

42
Q

volume of distribution

A

number to describe the apparent volumes of compartments that constitute the compartmental model.
Dose of drug given divided by the amount in plasma prior to elimination.

43
Q

volume of distribution (Vd) effected by

A

lipid solubility
binding to plasma proteins
molecular size

44
Q

ionized

A

water soluble, poorly lipid soluble

ex: Neuromuscular blockers

45
Q

non-ionized

A

lipid soluble, diffuses easily across lipid barriers like blood-brain barrier, GI endothelium, hepatocytes, renal tubular epithelium, placenta

46
Q

protein binding

A

effects distribution of drugs as only unbound drug can cross cell membranes

47
Q

agonist + agonist

A

1+1=2

ex nitrous and sevo

48
Q

synergistic

A

1+1=3

ex: fentanyl and benzos (increases impact of resp depression, sedation)

49
Q

potentiation

A

1+0=3

enhancement of one drug action by second drug with no action of its own

50
Q

antagonistic

A

1+1=0

ex: fentanyl + narcan

51
Q

hyperreactive

A

having or showing abnormally high sensitivity to stimuli

ex: vasodilators and dehydration

52
Q

hypersensitive

A

abnormally susceptible physiologically to a specific agent

typically immune mediated response

53
Q

hyporeactive

A

having or showing abnormally low sensitivity to stimuli

54
Q

safety margin

A

therapeutic vs lethal dose

55
Q

tolerance

A

the capacity of the body to endure or become less responsive to a substance (as a drug) or a physiological insult especially with repeated use or exposure

56
Q

tachyphylaxis

A

diminished response to later increments in a sequence of applications of a physiologically active substance [med]

57
Q

Inverse agonist

A

A drug or endogenous chemical that binds to a receptor, resulting in the opposite action of an agonist. May have a theoretical advantage over antagonists in situations in which a disease state is partly due to an up regulation of receptor activity,

58
Q

Ligand

A

Molecule that is able to bind and form a complex with a receptor to produce a biological response. Are endogenous chemicals

59
Q

Quantal drug response

A

Using dose response curves, the actions of a drug can be quantified and expressed as the effective dose ED50, toxic dose TD50, and lethal dose LD50. The therapeutic index is LD50/ED50

60
Q

Ceiling effect

A

Refers to the dose beyond which there is no increase in effect. Additional dosing often leads to adverse effects.

Pharmacology 680 (19 decks)

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