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Pharm 1 > Pharmacokinetics/Pharmacodynamics > Flashcards

Pharmacokinetics/Pharmacodynamics Flashcards

1
Q

“the drug’s effect on the body”

therapeutic and/or toxic doses

Sensitivity and responsiveness of receptors

Variability from person to person

Mechanism of action

effective dose (ED)

A

Pharmacodynamics

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2
Q

When is a drug considered eliminated?

A

when 95% has been eliminated – usually 4-5 elimination ½ lives

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3
Q

The time for the drug in the plasma to decrease by 50%; affected by volume of distribution and changes in clearance.

A

Elimination ½ life

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4
Q

The time for the plasma drug concentration to decrease by 50% after discontinuing a continuous infusion of a specific duration

A

Context-Sensitive Half-Time (infusion duration)

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5
Q

Which drug has a short context-sensitive half-time?

A

remifentanyl

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6
Q

The half-time of equilibration between drug concentration in the blood and the drug effect*

Accounts for the delay between IV injection into the plasma and the delivery of the drug to its site of action

Important for redosing intervals!

A

Effect-Site Equilibration Time

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7
Q

Number to describe the apparent volumes of compartments that constitute the compartmental model.

Describes the distribution characteristic of a drug in the body.

Calculated – dose of drug given divided by the resulting plasma concentration prior to elimination (at maximal concentration)

A

Volume of Distribution

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8
Q

What is Volume of Distribution effected by?

A

1) Lipid solubility
2) Binding to plasma proteins
3) Molecular size

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9
Q

Large Vd Drug

A

propofol

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10
Q

small Vd drug (MOSTLY IN PLASMA)

A

NMB

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11
Q

Which drug has more effect, bound or unbound?

A

unbound (in the plasma, can cross cell membrane, not bound to the protein)

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12
Q

What is an ionized drug?

A

WATER-soluble

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13
Q

What is a nonionized drug?

A

LIPID-soluble

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14
Q

What 4 areas are lipid soluble?

A

blood-brain barrier
renal tubules
GI endothelium
placental barrier

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15
Q

high vD

A

low protein binding

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16
Q

low vD

A

high protein binding

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17
Q

One effective dose plus another effective dose

1 + 1 = 2

Sebo and nitrous

A

Additive

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18
Q

Given together to create a bigger effect

1 + 1 = 3

fentanyl and midazolam

A

Synergistic

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19
Q

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

1 + 0 = 3

A

Potentiation

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20
Q

Working against each other

1 + 1 = 0

Fentanyl and nalaxone

A

Antagonistic

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21
Q

Having or showing abnormally high sensitivity to stimuli

such as bronchial response to an irritant

A

Hyperreactive

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22
Q

Abnormally susceptible physiologically to a specific agent

can be an immune-mediated response

A

Hypersensitive

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23
Q

Having or showing abnormally low sensitivity to stimuli

A

Hyporeactive

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24
Q

What type of response can occur with a person on an antihypertensive drug given vasodilation?

A

Hypersensitive

hypersensitive to vasodilation, super responsive, extremes of BP lows and highs

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25
Q

What type of response can occur with a person who chronically uses oxy for back pain?

A

Hyporeactive

developed a tolerance, may have low sensitivity to narcotics

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26
Q

The difference between the usual effective/therapeutic dose and the dose that causes severe or life-threatening side effects (toxic)

A

Safety margin

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27
Q

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

A

tolerance

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28
Q

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

less of a response the next times you give it (second dose often needs to be larger)

A

Tachyphylaxis

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29
Q

Example of tachyphylaxis?

A

ephidrine

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30
Q

what is ED50?

A

effective dose in 50% of patients

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31
Q

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

Mimics the action of an endogenous ligand that binds to the same receptor

A

Agonist

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32
Q

Can some drugs be partial agonists and antagonists?

A

Yes

Activates a receptor, but cannot produce a maximum response

May partially block effect of full agonists

Lower efficacy than a full agonist

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33
Q

A drug that has affinity/potency for the receptor, but no efficacy

does NOT activate the receptor to produce a physiologic action.

A

Antagonist

34
Q

Does an antagonist produce a physiologic action?

A

no, it produces a CONSEQUENCE (block of the response)

35
Q

What type of antagonist is reversible?

A

Competitive

36
Q

What type of antagonist is irreversible?

A

non-competitive

37
Q

Two agonist drugs that bind to different receptors – causing opposing responses

A

Physiologic antagonism

38
Q

NO receptor activity is involved – one drug binds with the second drug to inactivate it

A

Chemical antagonism

39
Q

example of chemical antagonism?

A

protamine and heparin

40
Q

example of physiologic antagonism?

A

vasodilation v. vasoconstriction

41
Q

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

A

Receptor

42
Q

What is responsible for the selectivity of drug action?

A

receptor

43
Q

the degree of drug receptor interaction for a given drug

A

affinity/potency

44
Q

drug’s ability to produce desired response (maximum effect)

A

efficacy/intrinsic activity

45
Q

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

A

Spare receptor concept

46
Q

Is the relationship between the number of receptors stimulated and the response usually:

linear OR nonlinear?

A

NONlinear

Example: muscle receptors and antagonists – takes 70% of receptors blocked before reduction in muscle response – only 30% of receptors activated by ACh produces maximal response

47
Q

occurs with continued stimulation of cells with agonists – the effect is diminished

A

Down-regulation/Desensitization

Example: beta agonist bronchodilators – tolerance develops from repeated use – increased dose required for same effect

48
Q

chronic exposure to antagonists cause receptor number and sensitivity to increase

A

Up-regulation

Example: Beta-blockers cause up regulation of receptors
if taking beta blocker on regular basis, have them continue on morning of surgery
if level is too low, there will be increase of beta 1 receptors, so there is going to be exaggerated response (greater tachycardia, etc.)

49
Q

what type of drug binds to circulating protein receptors?

A

drugs affecting components of the coagulation cascade

50
Q

AGE
Variability of Pharmacologic Response

A

neonates (not ready yet, not good enzymes, large water content, there response to water soluble vs lipid soluble)

80s age (dehydrated, malnourished, things are starting to fail)

51
Q

SEX
Variability of Pharmacologic Response

A

NMBs (guys have a higher muscle content than men, could possibly impact duration)

52
Q

Pathological State (PS)
Variability of Pharmacologic Response

A

muscular dystrophy, myasthenia gravis

53
Q

Variability of Pharmacologic Response

A

Age
Sex
Body weight
Body surface area
Basal metabolic rate
Pathologic state
Genetic profile

54
Q

the actions of the body on the drug

Absorption
Distribution
Metabolism
Elimination of drugs and metabolites

A

Pharmacokinetics

55
Q

What is another word for absorption?

A

bioavailability

56
Q

What types of routes are effected by first-pass effect?

A

PO, rectal

57
Q

circulation through the liver

A

first-pass effect

58
Q

where does sublingual go?

A

superior vena cava

59
Q

where does fentanyl and sufentanyl go first?

A

lungs

60
Q

What are the components of the Two Compartment Model

A

distribution (alpha)
elimination (beta)

61
Q

what is elimination phase?

A

metabolism and excretion

62
Q

what is distribution phase?

A

central (vessel rich group, then muscle, then fat, than redistributed) to peripheral

63
Q

% for Fat Group

A

”im fat and 26”
6% CO and 20% body mass

64
Q

% for Muscle Group

A

“People are more muscley at 19 than 50”
19% CO, 50% body mass

65
Q

% for VRG

A

“wise with the brain at age 75”
75% CO, body mass 10%

66
Q

what is the VRG (5 places)

A

brain
heart
liver
kidney
endocrine

67
Q

does metabolism always create inactive metabolites?

A

no

Morphine-6-glucuronide is more potent than morphine itself

Prodrug – metabolized to an active drug – codeine to morphine

68
Q

what are 5 sites for metabolism?

A

MOSTLY Hepatic microsomal enzymes
Plasma – Hofmann elimination
Lungs
Kidneys
Gastrointestinal tract

69
Q

what effects Hoffman elimination?

A

temperature and pH

70
Q

Does enzyme induction impact inner patient variability?

A

yes

taking certain medications can increase metabolism of drugs

71
Q

Hepatic microsomal enzymes mostly

Oxidative metabolism of most drugs

A

Cytochrome P-450 Enzymes

72
Q

The ability of drugs or chemicals to stimulate activity of the cytochrome P450 system.

A

Enzyme induction

73
Q

Non-microsomal enzymes

Metabolism by conjugation, hydrolysis, and some oxidation and reduction

Present largely in the liver, but also found in the plasma and GI tract

A

NON-cytochrome P-450 Enzymes (Esters)

plasma cholinESTERase, plasma ESTERases

74
Q

Are NON-cytochrome P-450 Enzymes (Esters) inducible?

A

NO

75
Q

Can NON-cytochrome P-450 Enzymes (Esters) be altered by genetics?

A

YES

76
Q

what are phase I enzymes?

A

Cytochrome P-450 Enzymes
NON-cytochrome P-450 Enzymes (Esters)

77
Q

are FAST or SLOW acetylators are at greater risk for side-effects?

A

SLOW

78
Q

What are the 2 major sites of elimination?

A

kidneys and the liver

79
Q

ED50 is an example of what*

A

pharmacodynamics (drug effecting the body)

80
Q

CSHT is effected by what 3 things*

A

distribution, metabolism, duration

Pharm 1 (9 decks)

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