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Pharm Sci > ADME > Flashcards

ADME Flashcards

1
Q

A scientific discipline that aims to quantitatively characterize the effect of the body on the drug

A

Pharmacokinetics (PK)

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2
Q

ADME

A

Absorption: drug transfer from its site of administration to the general circulation

Distribution: Drug molecules carried by blood to site of action

Metabolism: Transformation from one drug product to another

Excretion: Removal of the drug product (or metabolite) from the body

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3
Q

The drug to travel form its site of administration to its target site at desirable concentrations and at desirable time frame

A

The overall goal in drug therapy

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4
Q

The site of action is localized around the site of administration

A

Local drug administration

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5
Q

The site of action is far from the site of administration and must be transported via the bloodstream

A

Systemic drug administration

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6
Q

A common route of drug administration

A

Extravascular route

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7
Q

Before the drug is absorbed through the GI walls,

A

It should be available as molecules solubilized in the interstitial fluids

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8
Q

Solid must under go ______ and liquid must under go _____

A

Solids must undergo disintegration and dissolution, liquids much undergo dissolution

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9
Q

For most drugs, the optimum site for drug absorption after oral administration is

A

The upper portion of the small intestine or duodenum region

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10
Q

The anatomy of the duodenum provide:

A
  • large surface area for the drug to passively diffuse

- high perfusion through a large network of capillaries

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11
Q

Large particles are delayed for ______ by the presence of food in the stomach

A

3-6 hours

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12
Q

Gastric emptying of solids v. Liquids

A

About 50% of liquids empty in 20 minutes

About 50% of solids remain after 2 hours

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13
Q

Small intestine pH gradient and what it means

A

(6.5-7)
Retention time is about 3-4 hours
Independent of solid particle size or fed status
Gradient bacterial content duodenum (sterile) to ileum (confluent)

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14
Q

Large intestine pH and what it means

A

(7)
Avg, takes 53 hours from ingestion to excretion
Unabsorbed molecules spend ~90% of time in large intestine and rectum (minimum absorption)
Highest bacterial content (anaerobic)

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15
Q

The rate and extent to which an active drug ingredient or therapeutic moiety is absorbed from a drug product and becomes available at the site of action

A

Bioavailability

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16
Q

Fraction of the administered dose which reaches the systemic circulation relative to an intravenous dose (F)

A

Absolute bioavailability

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17
Q

Bioavailability data are used to determine:

A
  • amount of drug absorbed from dosage form
  • rate at which the drug was absorbed
  • duration of the drug’s presence in the biologic fluid or tissue
  • relationship between drug blood levels and clinical efficacy and toxicity
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18
Q

FDA requires bioavailability data for

A

NDA, Abbreviated NDA, supplemental applications (for changes in manufacturing, new indications, and new/additional doses)

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19
Q

The rates of absorption and elimination are equal

A

Peak height concentration (Cmax)

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20
Q

MEC

A

Minimum effective concentration, must be achieved for the patient to exhibit adequate response

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21
Q

MTC

A

Minimum toxic concentration

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22
Q

Relationship between dose and Cmax

A

Cmax (and AUC) increase with increased dose

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23
Q

Reflects the rate of absorption from a formulation, which determines the time needed for the MEC to be reached and to maintain it

A

Time of Peak (Tmax)

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24
Q

Changes in the rate of drug absorption change the

A

Cmax and Tmax

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25
Q

When the rate of abortion is decreased

A

Cmax is lowered and Tmax occurs at a later time

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26
Q

The serum blood concentration over time; measure of the total amount of drug absorbed into the circulation following the administration of a single dose

A

AUC (area under curve)

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27
Q

If equivalent doses of a drug in different formulations provide different AUC values =

A

Differences in the extent of absorption (Graph on Slide 23)

—-Formulation A Delivers much greater amt of drug to circulatory system than other two formulations

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28
Q

Oral dosage strengths are based on considerations of the proportion of the dose

A

That is expected to be aborbed

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29
Q

The absolute bioavailability following oral dosing is compared to

A

IV dosing

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30
Q

When F is less than 1, oral doses

A

Must be larger than IV doses to provide the same concentration of drug in the plasma

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31
Q

As bioavailability worsens,

A

The variability from patient to patient tends to increase

32
Q

What enzyme in the liver is responsible for a lot of drug metabolism?

A

Cytochrome C

33
Q

What does this equation and the components mean?

F = Fa X Fi X Fh

A 
F= bioavailability
Fa= the fraction of the administered dose that is not destroyed in the gut or lost in feces
Fi= the fraction of the dose that escapes metabolism in the intestinal wall
Fh= the fraction of the dose that escapes metabolism on first-pass through the liver
34
Q

Transport without external energy and molecules diffuse randomly in all directions

A

Passive Transport

35
Q

The rate of transfer of diffusion

A

Flux (measured in mass per unit area)

36
Q

Molecules diffuse from a region of high concentration to a region of low concentration

A

Fick’s law of diffusion

37
Q

The location, extent, and degree of distribution are dependent on

A

The drug’s properties and individual patient characteristics

38
Q

Drugs can distribute into these fluids

A
  1. Plasma (3 L)
  2. Intracellular water (27 L)
  3. Interstitial water (12 L)

Where the drug dissolves affects concentration

39
Q

Drugs are present in the body in two states

A

Bound (to protein)

Free (plasma, interstitial fluid and lymph, tissues)

40
Q

What drugs diffuse across the membrane the easiest?

A

Hydrophobic, small, not bound to plasma protein

40
Q

The pressure gradient between the arterial end of the capillaries entering the tissue and the venous capillaries leaving the tissue

A

Hydrostatic pressure

40
Q

The difference between the capillary hydrostatic pressure and the blood osmotic pressure

A

Net Filtration pressure (NFP)

40
Q

As the blood newly enters the capillary (arterial end) the pressure of the capillary blood is slightly higher than that of tissue causing

A

Fluid to leave the capillary bed and enter the tissues

Also known as: hydrostatic or filtration pressure

40
Q

Venues have lower pressure than tissue fluids allowing the filtered fluid to

A

Return to the venous capillary

Also known as absorptive pressure

41
Q

Partitioning and accumulation of a drug in the tissue or organ

A

Drug affinity

42
Q

The time for the drug distribution is generally measured by the time for 50% distribution

A

Distribution half life

43
Q

Relation to the blood flow to the organ, the volume of the organ, and the partitioning of the drug into the organ tissues

A

Distribution Constant

44
Q

An estimated value used because the true volume a drug is absorbed into (distributed) is not known

A

Volume of Distribution

It is not a physiological volume, it is hypothetical

45
Q

Determined by the same physiological and drug-related factors that control drug distribution

A

Volume of Drug distribution

46
Q

The decline from peak plasma concentrations after drug administration results from drug elimination or removal by the body

A

Metabolism

47
Q

Elimination of most drugs from the body involves both

A

Metabolism (bio transformation) and renal excretion

48
Q

The principle site of metabolism is

A

The liver

49
Q

The enzymes responsible for oxidation and reduction of drugs and certain metabolites are monoxygenase enzymes know as

A

Mixed-Function Oxidases

Constitute ETC enzymes

50
Q

The terminal component of the electron transport chain in the ER and acts as both an oxygen and substrate binding locus for drugs and endogenous substrates

A

Cytochrome P-450

51
Q

Responsible for metabolism >70% of drugs

A

Cytochrome-P450

Families (numbers) and subfamilies (letters)
CYP2c(, 2C19, and 3A4 >50% of oral drugs

52
Q

Inactive and must be biotransformed in the body to metabolites that have pharmacological activity, intentionally designed to improve drug stability, increase systemic absorption, or prolong activity

A

Pro drugs

53
Q

What are the two major groups of reactions for pathways of drug biotransformation

A 
Phase I (asymmetric): oxidation, reduction, hydrolysis
Phase II (synthetic): conjugation
54
Q

Phase I biotransformation reactions usually occur

A

First and introduce or expose a functional group on the drug molecule

55
Q

Once a polar constituent is recreated or placed into the molecule

A

A phase II reaction may occur

56
Q

Derived from biochemical compounds involved in carbohydrate, fate, and protein metabolism

A

Conjugating reagents

57
Q

Refers to the irreversible removal of drug from the body by all routes of elmination

A

Drug elimination

58
Q

Drug elimination is usually divided into two components

A

Excretion and Biotransformation

59
Q

The removal of the intact drug

A

Drug excretion

60
Q

The process by which the drug is chemically converted in the body to a metabolite

A

Biotransformation or drug metabolism

61
Q

The main excretory organ for the removal of metabolic waste products and plays a major role in maintaining the normal fluid volume and electrolyte composition

A

Kidney

62
Q

To maintain salt and water balance, the kidney

A

Excretes excess electrolytes, water, and waste products while conserving solutes necessary for proper body function

63
Q

The two endocrine functions of the kidneys

A
  1. Secretion of renin to regulate BP

2. Secretion of erythropoietin, which stimulates RBC

64
Q

Briefly describe the anatomy of renal filtration

A
  • Kidney is supplied blood via the renal artery
  • Each arterial carries blood into nephrons to Bowman’s capsule to filter the blood in the glomerulus
  • Blood flows out into a second capillary network that surrounds the tubules including the Loop of Henle
65
Q

The volume of blood flowing through the renal vasculature per unit time

A

Renal Blood Flow (RBF) 1.2 L/min or 1700 L/d

66
Q

The renal blood flow minus the volume of RBCs present, important factor in the rate of drug filtration at the glomerulus

A

Renal plasma flow (RPF)

67
Q

About 120 mL/min or 180L/d

A

Glomerular filtration rate (GFR) about 20% of the RPF

68
Q

Ratio of GFR/RPF

A

Filtration fraction

69
Q

The process by which a drug is excreted via the kidneys may include

A

Glomerular filtration, active tubular secretion, and tubular reabsorption

70
Q

The ratio of the sum of the glomerular filtration and active secretion rates less the reabsorption rate divided by the plasma drug concentration

A

Renal clearance

71
Q

May give an indication for the mechanism of renal excretion of the drug

A

Clearance ratio

<1 — drug is partially reabsorbed
=1 — drug is filtered only
>1 — drug is actively secreted

Pharm Sci (5 decks)

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