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House Pharmacology > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

Pharmacokinetics describes the fate of a drug within the body
-It simple refers to “what the body does to the drug”
-These fate includes

_____
______
_____
______

A

ABSORPTION
DISTRIBUTION
METABOLISM
EXCRETION

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2
Q

Administration of a drug
-is the initial introduction of a drug into the body
-Drugs are introduced into the body either
______ or ______

A

Enterally or Parenterally

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3
Q

ENTERAL means of administering drugs

____

A

Oral

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4
Q

PARENTERAL means of administering drugs

Mention 7

A

Intravenous
Intramuscular
Subcutaneous
Inhalational
Topical
Transdermal
Intrathecal/Intraventricular

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5
Q

Absorption
-is the transfer of drug from the _____ to ____

A

site of administration to the bloodstream

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6
Q

MEASURE OF DRUG ABSORPTION

Bioavailability
- is the ______

A

relative amount of the administered drug that reach the systemic circulation

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7
Q

Drugs administered through Intravenous (IV) route have ____% bioavailability

A

100

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8
Q

Formula for bioavailability of drugs:

Absolute bioavailability = _____/ ____ × —-

Relative bioavailability =_____/ ______ × 100

A

AUC Oral

AUC IV

100

AUC (test)

AUC (standard)

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9
Q

Bioequivalence
Two drug formulations with _________ as well as the _______ are bioequivalent

A

the same bioavailability

same rate of absorption

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10
Q

Distribution
is the delivery of a drug from the _____ to ______

A

systemic circulation to tissues

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11
Q

MEASURE OF DRUG DISTRIBUTION
Volume of distribution (Vd)
-It is the _______

Formula:
Vd = _____/Co
Co is the _______

A

fluid volume in the body into which the drug is contained

Dose

concentration of the drug in the plasma at time 0

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12
Q

Tissues that store large concentration of drugs are
____
_____

A

Fat
Bones

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13
Q

Metabolism Of drugs

-Characterized by the conversion of drugs from its ___PHILIC nature to execrable ___PHILIC products, through specialized enzymatic systems

A

LIPO

HYDRO

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14
Q

SITES OF DRUG METABOLISM

Mention 4

A

Liver
Kidney
Small Intestine
Lungs

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15
Q

PRODUCTS OF DRUG METABOLISM

Mention 4 scenarios

A

Inactive to active
Active to inactive
Active to active
Active to toxic

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16
Q

PHASES OF DRUG METABOLISM

Phase I
FUNCTIONALIZATION REACTION
-A ___ is introduced into the drug to make it ____

-Enzymes involved a special enzymes called _____ enzymes found in the ____

A

functional group

more polar

CYTOCHROME P-450

SER

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17
Q

Examples of Phase I reaction includes:

____
_____
_____

A

Oxidation
Reduction
Hydrolysis

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18
Q

Enzymes involved in phase 1 oxidation reactions

A

CytochromeP450 Oxidase

dehydrogenase

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19
Q

Enzymes involved in phase 1 reduction reactions

A

Cytochrome p450 reductase

Decarboxylase

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20
Q

Enzymes involved in phase 1 hydrolysis reactions

A

Estarase

Amidase

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21
Q

Phase II
CONJUGATION REACTION
-An _____ substance is added to the drug to make it hydrophilic
-Examples of Phase II reaction

Mention 5

A

endogenous

Glucuronidation
*Sulfation
*Methylation
*Acetylation
*Glutathione conjugation

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22
Q

Glucuronidation
Sulfation
Methylation
Acetylation
Glutathione conjugation
Glycine conjugation

Mention the enzymes involved in the reactions

A

Glucoronyl Transferase

N-acetyl Transferase

Sulfo Transferase

Methyl Transferase

Glutathione conjugation

Glycine conjugase

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23
Q

Enzyme Induction
-Induces Microsomal Cytochrome P-450 enzyme
-___eases metabolism of co-administered drugs
-May lead to _____

A

Incr

therapeutic failure

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24
Q

Enzyme Inhibition
Inhibitors of Cytochrome P-450
___eases metabolism of co-administered drugs
May lead to ____

A

Decr

drug toxicity

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25
Q

MECHANISM OF HEPATIC EXCRETION

_______
_______

A

Hepatic secretion
Enterohepatic circulation

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26
Q

Enterohepatic circulation
-from ______ to ____ to ___ to ____ to ____

A

duodenum to ileum

capillary bed to portal vein to liver

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27
Q

__% bile salts is excreted into faeces

A

5

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28
Q

a charged drug can cross the plasma membranes

T/F

A

F

can’t

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29
Q

for absorption, acidic drug wants ____ environment. Basic drugs wants ____

for excretion, acidic drugs wants ___ environment, basic drugs wants ____ environment

A

acidic

basic

basic

acidic

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30
Q

MEASURE OF DRUG EXCRETION

Half-life (t1/2)
-It is the time taken for ______

Elimination rate (Kel)
-It is the ________

Clearance (CL)
-It is the _______

A

the concentration of drug in the blood to fall by half its original value.

fraction of drug that is eliminated at a given time

volume of blood or plasma cleared of a drug in unit time

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31
Q

ELIMINATION KINETICS

Zero-order kinetics
-Elimination of ________ per unit time
-Rate of elimination is (dependent or independent?) of drug concentration

-Half-life is ( dependent or independent?) to the drug concentration

A

constant amount of a drug

independent

dependent

32
Q

Zero-order kinetics Examples

Mention 4

A

Ethanol
Heparin
Phenytoin
Aspirin

33
Q

First-order kinetics
-Elimination of ____ of a drug per time
-Rate of elimination is (dependent or independent?) of the drug concentration
-Half-life is (dependent or independent?) of drug concentration

Examples
____

A

constant percentage

Dependent

independent

MOST DRUGS

34
Q

PARACETAMOL

Administration-

Bioavailability-

Metabolism in the liver - phase 1:
phase 2:

Half-life-

Elimination kinetics- zero or first

Excretion is by??

A

Oral

63-89%

Oxidation
Sulphation and glucoronidation

1.9-2.5 hours

First order

Kidney

35
Q

Enteral administration is administering a drug by ______

A

mouth

36
Q

______ administration is the safest and most common, convenient, and economical method of drug
administration.

A

Enteral

37
Q

The drug may be swallowed, allowing oral delivery, or it may be placed _________ (sublingual), or _____ (buccal), facilitating direct absorption into the bloodstream

A

under the tongue

between the gums and cheek

38
Q

A wide range of oral preparations is available for drugs that can’t withstand the low ph of the stomach including
______ and ______ preparations.

A

enteric-coated and extended-release

39
Q

Enteric coating is useful for
certain drugs (for example, ______) that are acid unstable.
Drugs that are irritating to the stomach, such as _______, can
be formulated with an enteric coating that only dissolves in the
small intestine, thereby protecting the stomach.

A

omeprazole

aspirin

40
Q

the half-life of oral morphine is ___

A

2 to 4 hours

41
Q

Example of a drug poorly absorbed in the GIT

A

Heparin

42
Q

Example of a drug that is unstable in the GIT

A

Insulin, omeprazole

43
Q

________ is the most common parenteral
route

A

IV injection

44
Q

Injected drugs can be recalled by activated charcoal
T/F

A

F

45
Q

Subcutaneous injection route should not be used with drugs that cause
_______, because ______ and ______ may occur.

A

tissue irritation

severe pain and necrosis

46
Q

Drugs commonly administered via the subcutaneous route include
______ and ______

A

insulin and heparin.

47
Q

Examples of drugs administered via Oral inhalation include bronchodilators, such as ______, and corticosteroids, such as _____.

A

albuterol

fluticasone

48
Q

Desmopressin is administered ______
in the treatment of _________

A

intranasally

diabetes insipidus.

49
Q

Topical application is used when _____________

A

a local effect of the drug
is desired.

50
Q

Transdermal: This route of administration achieves systemic
effects by application of drugs to ______, usually via a ______

A

the skin

transdermal patch

51
Q

Rectal: Because 50% of the drainage of the rectal region ________, the ___________ is minimized with rectal administration.

A

bypasses the portal circulation

biotransformation of drugs by
the liver

52
Q

The vast majority of drugs
are absorbed by ____ mechanism

A

Passive diffusion

53
Q

_____-soluble drugs penetrate the cell membrane through aqueous channels or pores, whereas ____-soluble drugs readily move across most biologic
membranes

A

Water

lipid

54
Q

Mechanisms of absorption of drugs from the GI tract

Passive diffusion can be saturated
Facilitated diffusion can be saturated
Active transport can be saturated

T/F

A

F
T
T

55
Q

The lower the pKa of a drug, the more _____ it is

A

acidic

56
Q

Which has more blood flow and hence better for absorption?

Stomach or small intestine?

A

Small intestine

57
Q

First-pass hepatic metabolism: When a drug is absorbed from the GI tract, it enters the _____ before entering the _____

A

portal circulation

systemic circulation

58
Q

more than 90% of _______ is cleared during first-pass metabolism.

A

nitroglycerin

59
Q

rocuronium, a _________ is administered by ______ route

A

Neuromuscular blocker

IV

60
Q

if the medication is delivered too rapidly and high concentrations are reached too quickly , It may also ______, induce ______, or cause other adverse reactions

A

precipitate blood constituents

hemolysis

61
Q

Drugs administered IM can be in ______, which are absorbed rapidly, or in specialized ______, which are absorbed slowly.

A

aqueous solutions

depot preparations

62
Q

Depot preparations often consist of a _____ of the drug in a ______
vehicle such as polyethylene glycol.

As the vehicle diffuses out of the muscle, the drug ______ at the site of injection. The drug then _______, providing a ________ over an extended period of time.

A

suspension; nonaqueous

Precipitates ; dissolves slowly

sustained dose

63
Q

Subcutaneous administration route should not be used with drugs that cause _______, because ________ and _______ may occur.

Drugs commonly administered via the subcutaneous route include ______ and _____

A

tissue irritation

severe pain and necrosis

insulin and heparin.

64
Q

The _____ typically delays or prevents the absorption of drugs into the central nervous system (CNS). When local, rapid effects are needed, it is necessary to introduce drugs directly into the _________

A

blood–brain barrier

cerebrospinal fluid.

65
Q

A drug passes through membranes more readily if it is (charged or uncharged ?)

A

Uncharged

66
Q

Factors that affect route of administration

______ of Drug
________ of treatment
_____ of action
Desired _______
_________

A

Nature

Duration

Site

onset of action

Consciousness

67
Q

FACTORS AFFECTING DRUG ABSORPTION
_______ of Administration
_________ of drug
_______
______
_____ flow
_______ of absorption site
_________ at absorption site
Presence of ______

A

Route

Solubility

Concentration

pH

Blood

Surface area

Contact time

P-glycoprotein

68
Q

Out of AADME, which ones do age affect

A

Distribution
Metabolism

69
Q

Out of AADME, which ones do PH affect

A

Absorption
Distribution
Excretion

70
Q

Arrange in terms of decreasing absorption rate

Skin; gut; muscle

A

Muscle, skin, gut

71
Q

FACTORS AFFECTING DRUG DISTRIBUTION
______ of drug
____
Binding to ______
Binding to _____
Organ or tissue size and perfusion
_____
______
____
_______
______ state
Drug ______

A

Lipophilicity
pH

plasma proteins
Tissues

Age
Pregnancy

Obesity
Diet
Disease

interaction

72
Q

MEASURE OF DRUG DISTRIBUTION
__________

A

Volume of distribution (Vd)

73
Q

Levodopa is converted from _____ to _____

A

Inactive to active

74
Q

Epinephrine is from active to _____

Panadol is from active to_____

A

Inactive
Toxic

75
Q

Salivary excretion is by _______
Pulmonary excretion is by _______________
Tears excretion is by _________
Sweat excretion is by ________
Hair excretion is by _________
Breast excretion is by __________

A

Passive diffusion

Passive diffusion and expiration

Passive diffusion

Passive diffusion

Unknown…maybe deposition from the capillaries

Passive diffusion

76
Q

Codeine

Weak acid or weak base?

A

Weak base

77
Q

Most rapid route of absorption is IV
T or F

A

F

Inhalational

House Pharmacology (50 decks)

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