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Pharm Exam 1 > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

ADME acronym

A

Absorption
Distribution
Metabolism
Elimination

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2
Q

Dose-effect relationship for pharmacokinetics

A

Pharmacokinetics: dose - concentration part
Pharmacodynamics: concentration - effect part

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3
Q

The time it takes for a drug to be _____ and
______ mainly accounts for the appearance of its effects: onset of action

A

absorbed and distributed

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4
Q

The time it takes for _____ and _____ accounts for the disappearance of a drug’s effect

A

metabolism; elimination

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5
Q

_____: involves the movement of a drug from the site of application into the bloodstream

A

Absorption

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6
Q

Rate and amount of drug absorbed depend on these factors

A
  • route of administration
  • local blood flow
  • pH, drug ionization
  • water solubility
  • lipid solubility
  • dose
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7
Q

____- the fraction of unchanged drug reaching the systemic circulation by any route

A

Bioavailability

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8
Q

What is the first pass effect?

A

the fraction of drug lost during the process of absorption

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9
Q

____ is a major site of drug metabolism

A

Liver

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10
Q

Pathway of oral drug to reach systemic circulation

A

oral-> gut-> portal circ. -> liver -> IVC -> heart-> lungs-> heart-> systemic circulation

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11
Q

Most drugs are weak _____

A

acids or weak bases

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12
Q

A drug is more readily absorbed and passes through cell membrane if it is uncharged- _____

A

non-ionized

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13
Q

Due to greater blood flow, _____ is often the major site of entry into the bloodstream, rather than stomach (oral route)

A

duodenum

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14
Q

______ - important enzyme for metabolizing endogenous compounds and drug biotransformation in the liver

A

Cytochrome P450

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15
Q

Usually described as the ______; a measure of the apparent space in the body available to\ contain the drug

A

volume of distribution

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16
Q

4 main compartments for drug distribution:

A

-blood (plasma)
-fat
-extracellular fluid
-intracellular fluid

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17
Q

The balance between distribution compartments determined by

A

-permeability of barriers
-pH within the compartment
-binding capacity
-fat solubility of the drug

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18
Q

A protein bound drug cannot do these things:

A

-diffuse through membranes
-be metabolized
-be excreted
-cause effects

19
Q

What is Vd?

A

Volume of distribution
the property of the drug which shows how much drug needs to be within the body to get a certain concentration in the plasma

20
Q

Plasma protein binding greatly _____ the amount of drug free in the plasma

A

reduces

21
Q

Vd formula

A

Vd = total amount of drug in the body /
concentration of drug in plasma

22
Q

T/F - Drugs with very high volumes of distribution have much higher concentrations in extravascular tissue than in the vascular compartment

A

T

23
Q

______: the set of chemical reactions and pathways by which living organisms transform chemical substances

A

Metabolism

24
Q

This process begins as soon as the drug reaches systemic circulation

A

Biotransformation
* One purpose is to eliminate
metabolic wastes
* Drug converted into a metabolite

25
Q

Most common form of drug inactivation

A

Active Drug –> inactive metabolites
-typically metabolite is more water soluble
-enhancing elimination

26
Q

Biotransformation that results in partial loss of activity

A

Active drug –> active metabolites (heroin–> morphine)

27
Q

Biotransformation that promotes absorption and maybe to bypass first pass elimination

A

Inactive drug → active metabolite (aspirin)

28
Q

What is a drug example of this type of biotransformation?
Active drug → toxic metabolite

A

Acetaminophen

29
Q

Metabolism phases

A
  • Phase 1: involves formation of a new or modified
    function group or cleavage
    – Hydroxylation: most common Phase 1 reaction
  • Phase 2: involves conjunction with an
    endogenous substance
    – Glucuronidation: most common Phase 2
    reaction
30
Q

Drugs can act as:

A

– substrates- material upon which the enzyme acts
– inhibitors- results in decreased metabolism of
drugs; selective or non-selective inhibition
– inducers- results in increased synthesis of P450 enzymes and increased metabolism of drugs

31
Q

How does the GI tract play a role in metabolism?

A

enzymes in mucosal cells of intestinal wall
bacteria in large bowel

32
Q

How does plasma play a role in metabolism?

A

not a major site; enzymes that degrade
drugs such as succinylcholine and procaine

33
Q

T/F with elimination drugs removed unchanged or as one or more metabolites

A

T

34
Q

the most important organs for drug removal

A

Kidneys

35
Q

T/F Reduced renal excretion accounts for more adverse drug effects in the elderly than any other pharmacokinetic factor

A

T

36
Q

Clearance equation

A

Cu x Vu / Cp
Cu- concentration of drug in the urine
Vu- rate of urine production
Cp- concentration of drug in the plasma

37
Q

Half life of a drug

A

the amount of time it takes for the blood level (or concentration) of a drug to fall to exactly half of what it was at some previous time

38
Q

Time to reach steady state is____ half lives

A

4 ½ to 5

39
Q

The higher the Cp, the ____ excretion

A

Faster

40
Q

When the Elimination rate is proportional to drug concentration, these drugs are following what

A

first order kinetics

41
Q

When the Elimination rate becomes independent of drug in system, these drugs are following what

A

zero-order kinetics

42
Q

Which drugs are more easily overdosed

A

Zero-order kinetics

43
Q

Elimination of constant amount of drug per unit time with

A

zero-order kinetics

44
Q

Elimination is a constant percentage of drug/unit time with ___

A

First order kinetics

Pharm Exam 1 (7 decks)

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