Exam 3 Review Flashcards

1
Q

Site of administration to blood

A

Absorption

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2
Q

Blood to tissues

A

Distribution

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3
Q

Tissues back to the blood

A

Redistribution

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4
Q

Chemical alteration of drug molecule by cells of the animal

A

Biotransformation (metabolism)

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5
Q

Removal or clearance of drug out of the body

A

Excretion

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6
Q

Downhill movement; no E required

A

Passive diffusion

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7
Q

Downhill movement; no E required; carrier-mediated

A

Facilitated diffusion

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8
Q

Uphill movement; E required; carrier-mediated

A

Active transport

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9
Q

Endocytosis of molecules dissolved in water

A

Pinocytosis

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10
Q

Pinocytosis example:

Aminoglycosides can cause what kind of damage and can act as what?

A

Renal damage; can act as renal toxins

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11
Q

What are these?
Concentration gradient
Lipid solubility
Degree of drug ionization

A

Factors affecting simple diffusion

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12
Q

Lipid solubility

A

Higher lipid solubility of the drug = FASTER crossing cell membranes

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13
Q

Degree of drug ionization

A

Drugs cross biological membranes in NON-IONIZED, LIPID SOLUBLE form

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14
Q

Ionized drugs tells us what?

A

The drugs are trapped

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15
Q

Non-ionized drugs tell us what?

A

The drugs are permeable to the membrane

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16
Q

What ionization equation would you use for a weak acid?

A

pka=pH + log N/I

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17
Q

What are these?
Molecular size, Dissolution in water, Concentration at absorptive site, Route of administration, Lipid solubility, Degree of ionization

A

Factors affecting drug absorption related to the drug

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18
Q

What are these?

Blood flow, absorptive surface area, connective tissue, species, individual

A

Factors affecting drug absorption related to the animal

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19
Q

Molecular size?

A

Smaller molecule = FASTER drug absorption

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20
Q

Lipid solubility?

A

High solubility = FASTER drug absorption

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21
Q

Degree of ionization?

A

High ratio = FASTER drug absorption

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22
Q

Dissolution in water?

A

Liquid drugs = FASTER drug absorption

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23
Q

Concentration at absorptive site?

A

Higher concentration = FASTER drug absorption

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24
Q

Routes of administration in order of fastest absorption?

A
  1. Sublingual and inhalation
  2. IM
  3. SQ
  4. PO
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25
Q

Blood flow?

A

Higher blood flow = FASTER drug absorption

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26
Q

Absorptive surface area?

A

Higher area = FASTER drug absorption

Ex. Fetanyl patch

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27
Q

Dissolution is often the rate limiting step for what kind of absorption?

A

Oral absorption (absorption from the GI tract)

28
Q

What are these?

Lipid solubility, Degree of ionization, Concentration gradient, Plasma protein binding, Affinity for certain tissues

A

Factors affecting drug disposition related to the drug

29
Q

What are these?

Blood flow, Species/individual differences, Plasma protein binding, Tissue barriers

A

Factors affecting drug disposition related to the animal

30
Q

Plasma protein binding?

A

Acids to Albumin
Bases to alpha-glycoproteins and lipoproteins
Unbound, free drugs are biologically active
Prolongs half life

31
Q

Blood Brain Barrier

A

Tight capillary endothelial junctions
Glial cells fill in gaps bt junctions
Younger animals have GREATER drug movement across BBB

32
Q

Affinity of drugs for certain tissues

A

Drugs will accumulate in certain tissues

Ex. Aminoglycosides bind to kidney tissue and can cause renal damage or failure

33
Q

Increased redistribution does what to the half life?

A

Increases the half life

34
Q

Which tissue is the common site of drug redistribution?

A

Adipose tissue

35
Q

What are the main effects of drug biotransformation?

A

Change in physiochemical properties of the drug

Change in pharmacologic activity

36
Q

The metabolite may be more water soluble, more polar, and more ionized

A

Change in physicochemical properties of the drug

37
Q

What are the changes in pharmacologic activity?

A

Bioinactivation and bioactivation

38
Q

Conversion of a parent drug to an inactive metabolite

A

Bioinactivation

39
Q

Conversion of a prodrug to an active drug

A

Bioactivation

40
Q

Conversion of a non-toxic substance to a toxic one

A

Bioactivation (lethal synthesis)

41
Q

Types of metabolic reactions?

A
Phase I (nonsynthetic)
Phase II (synthetic)
42
Q

What are the types of Phase I reactions?

A

Oxidation (most common)
Reduction
Hydrolysis

43
Q

What is the Phase II reaction?

A

Conjugation (cats and neonates are deficient)

44
Q

Species differences:

Deficient in glucuronyl transferases

A

Cats

45
Q

Species differences:

Deficient in acetylating enzymes

A

Dogs

46
Q

Species differences:

Have less plasma pseudocholinesterase

A

Ruminants

47
Q

Species differences:

Have high levels of oxidative enzymes

A

Ruminants and horses

48
Q

Species differences:

Deficient in sulfate conjugating enzymes

A

Pigs

49
Q

Species differences:

Lack oxidative enzymes

A

Birds

50
Q

Drug must go to liver before systemic circulation, so drug is metabolized before distribution is what?

A

First-pass metabolism

51
Q

Drugs that stimulate the liver to produce more metabolic enzymes, is reversible, includes microsomal enzymes, and may lead to tolerance or drug-drug interactions?

A

Enzyme inducers

52
Q

Examples of drug enzyme inducers

A

P- Phenobarbital
P- Phyenylbutazone
G- Griseofulvin
R- Rifampin

53
Q

Drugs that inhibit production of metabolic enzymes

A

Enzyme inhibitors

54
Q

Examples of drug enzyme inhibitors

A

C- Chloramphenicol
C- Cimetidine
K- Ketoconazole

55
Q

Conjugates of lipophilic compounds excreted in bile can be hydrolyzed in the intestines and converted back into lipid soluble free drugs

A
Enterohepatic recirculation
(prolongs half life of a drug)
56
Q

Renal excretion is dependent on which 3 factors?

A

Glomerlular filtration rate (GFR)
Active tubular secretion
Passive tubular reabsorption

57
Q

Volume of distribution equation?

A

Vd (L or L/kg)= Dose (mg or mg/kg) / Cp (mg/L)

58
Q

Renal clearance equation?

A

CLr (mL/min)= Rate of elimination (mg/min) / Cp (mg/mL)

59
Q

Rate of elimination equation?

A

Urine flow (mL/min) x Drug concentration (mg/mL)

60
Q

Half life equation?

A

T1/2= 0.693 x Vd / CLb

61
Q

Steady state plasma concentration equation?

A

DOSEcri= Cpss x CLb

62
Q

Loading dose equation?

A

Dose= Cpss x Vd

63
Q

Maintenance dose equation?

A

Dose = Cpss x CLb x Interval

64
Q

Adjusted dose equation?

A

Normal dose x Patient CLr / Normal CLr

adjusted dose should be SMALLER

65
Q

Adjusted dose interval equation?

A

Normal dose interval x Normal CLr / Patient CLr

adjusted interval should be LARGER (longer)