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Pharmacology > Pharmodynamics and kinetics > Flashcards

Pharmodynamics and kinetics Flashcards

1
Q

____ refers to how effective a drug is at producing a response

A

Efficacy

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2
Q

drugs with a ____ first pass effect have ____ bioavailability

A

high, low

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3
Q

what is the primary site of drug elimination

A

the kidney

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4
Q

Rate of renal excretion = ?

A

filtration + secretion - reabsorption

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5
Q

When does steady state occur?

A

occurs after multiple drug doses when the average drug concentration no longer changes, i.e. when the amount of drug going into the body is equivalent to the amount of drug leaving the body over the dosing interval. Approximate by multiplying half-life by 5.

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6
Q

Which phase of drug metabolism is enzymatic, which increases water solubility via conjugation and deactivates active metabolites?

A

phase 2

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7
Q

What is pharmacokinetics

A

what the body does to the drug

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8
Q

Describe phase 2 of drug metabolism

A

enzymatic, increases water solubility via conjugation and deactivates active metabolites

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9
Q

What is the primary site of drug metabolism

A

the liver

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10
Q

which are more easily absorbed: hydrophilic or lipophilic drugs

A

lipophilic

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11
Q

When environmental pH is lower than the drug pH, more of the ______ form predominates

A

un-ionized, protonated

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12
Q

un-ionized drugs are more ____ soluble, and therefore cross cell membranes ____

A

lipid soluble, cross cell membranes readily

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13
Q

What is bioavailability

A

the percentage of a drug dose that reaches systemic circulation

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14
Q

The magnitude and percent of clinical response is called

A

clinical efficacy

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15
Q

What is Tmax

A

the time at which the drug reaches Cmax, the highest measured concentraion in the plasma

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16
Q

What is the consequence of a drug being protein bound?

A

it cannot be filtered through the glomerulus, and it is not typically bioavailable.

17
Q

What is the most important transport protein that moves drugs out of cells

A

P-glycoprotein

18
Q

What is ion-trapping

A

a phenomenon where the drug will accumulate more in the compartment where it is more ionized (aka the compartment that has a pH further from the drug’s pKa)

19
Q

Lipophilic drugs go into ____, hydrophilic drugs go into ____

A

fat, fluid compartmetns

20
Q

What is the Area under the time concentration curve (AUC) a measure of?

A

the animals total exposure to the drug

21
Q

If the environmental pH is higher than the drug pKA, the ____ form predominates

A

ionized (deprotonated) form

22
Q

Which of the four processes of pharmacokinetics is not applicable to IV administration?

A

Absorption, as it is immediately at Cmax in the blood

23
Q

What is Cmax and what does it determine?

A

the highest concentration achieved by the drug in the plasma. This is determined by bioavailability and relative rate of absorption, distribution, metabolism/elimination

24
Q

Rank the drug receptors from fastest to slowest

A

ligand gated
g-protein coupled
enzyme receptors
intracellular receptors

25
Q

What is the first phase of drug metabolism, and what happens

A

Redox reactions, carried out by cytochrome P450

26
Q

What are the phases of drug metabolism

A

redox
Enzymatic

27
Q

What two things does metabolism increase in a drug

A

polarity and water solubility

28
Q

what type of administration can over-come the first pass effect

A

rectal

29
Q

equation for loading dose

A

loading dose= Vd x desired drug concentration

30
Q

what is pharmacological efficacy

A

the inhibition or activation of receptor activity

31
Q

what is potency

A

the concentraiton of a drug required to produce a response

32
Q

speed of absorption depends on ____

A

blood flow. This is why IM injections are more readily absborbed than SQ

33
Q

What is Vd?

A

The theoretical volume that would be needed to contain the total amount of administered drug at the initial concentration (C0) in the plasma after IV administration (or at Cmax after other forms of administration. Higher Vd means more distribution of the drug from the blood into the tissues, but not specific sites

34
Q

What does a higher Vd indicate?

A

more distribution of the drug from the blood into the tissues

35
Q

What is the clearance (Cl) of a drug after a single dose equal to?

A

dose/AUC

36
Q

What is a half life

A

the length of time it takes for the concentration of the drug in plasma to decrease by half (t1/2). When the dose is doubled, the duration of drug action is extended by 1 halflife

37
Q

What are the four physiological responses associated with pharmacokinetics

A

absorption
distribution
metabolism
elimination

Pharmacology (11 decks)

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