Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Block 1: Pharmacology > Lecture 1 and 2 (Revised) > Flashcards

Lecture 1 and 2 (Revised) Flashcards

1
Q

PK?

A

Absorption, Distribution, and Elimination

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Xenobiotics?

A

Substances that are foreign to the body

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

All drugs at high concentrations are?

A

Toxic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Absorption?

A

Process by which drugs enter systemic circulation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Only way to bypass absorption?

A

Using an IV

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Distribution?

A

Phenomenon by which drugs reach its site of action

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Elimination?

A

Process by which drugs are enzymatically altered (biotransformation) mainly in liver and eventually excreted by the kidneys

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Elimination mainly occurs in?

A

The liver and eventually excreted by the kidneys

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Drugs taken by the Hepatic Portal Vein are?

A

NOT absorbed yet because they have not entered systemic circulation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

If a drug is taken orally and patient has severe diarrhea?

A

It will not enter the systemic system and will not be effective

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

How well a drug can cross cell membrane is correlated with?

A

Physiochemical Characteristics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Absorption, Distribution, and Elimination of a Drug all involve?

A

Its passage across cell membranes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Factors in Transfer of Drugs Across Membranes?

A

1) Molecular size and shape of drug
2) Solubility of drug (lipid:water partition coefficient)
3) Most drugs are weak acids or weak bases

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Only highly lipid soluble drugs can?

A

Cross BBB, water soluble does not

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Only highly lipid soluble drugs can?

A

Cross BBB, water soluble does not

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Ionized?

A

Charge, cannot pass through membrane

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Unionized?

A

No Charge, does cross BBB

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Can readily cross cell membrane?

A

Only non-ionized form of the drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

If there is a charge?

A

It cannot cross membrane

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Henderson-Hasselbalch Equation?

A

Allows for calculation of degree of ionization for weak acids or weak bases

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Henderson-Hasselbalch Equation? (Weak Base)

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Henderson-Hasselbalch Equation? (Weak Acid)

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Lower pH?

A

More Acidic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

pH of Urine?

A

4.0-8.0

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Weak Acid gets trapped on more?

A

Basic Side

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Weak Base gets trapped in more?

A

Acidic Side

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

Processes of Drug Transfer?

A

1) Passive Diffusion
2) Active Transport
3) Facilitated Diffusion
4) Bulk Flow
5) Pinocytosis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

Factors that Influence Drug Absorption?

A

1) Solubility
2) Concentration
3) Circulation
4) Surface Area
5) Time

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

Passive Diffusion?

A

-Most common
-Moves only down concentration gradient
-Not saturable
-Not carrier-mediated

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

Higher the lipid:water partition coefficient?

A

Faster is the passive diffusion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

Ethanol (Alcohol) is an example of?

A

Passive Diffusion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

Which 2 Processes of Drug Transfer are Carrier-Mediated?

A

-Active Transport
-Facilitated Diffusion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

Active Transport?

A

-P-glycoprotein and Multi-drug resistance-associated proteins (MRP) are main transporters of drugs
-Need energy (ATP)
-Drug can move up concentration gradient
-Requires a carrier
-Can be saturated

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

Only process where drugs can go from a lower concentration to a higher concentration?

A

Active Transport

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

Penicillin in Kidney is an example of?

A

Active Transport

36
Q

Facilitated Diffusion?

A

-Drug moves only down concentration gradient
-Involves a carrier (No expenditure of energy)
-Can be saturated

37
Q

Amino Acids transport into Brain are an example of?

A

Facilitated Diffusion

38
Q

Bulk Flow?

A

-Movement of molecules through capillary junction
-Only free drugs can move through fenestration between capillaries, but most drugs are bound to plasma protein (Not with BBB)

39
Q

Fenestrations?

A

Tiny openings, capillaries have fenestrations but Brain does not

40
Q

Pinocytosis?

A

-Formation and movement of vesicles
-It plays a minor role in drug transport across membrane

41
Q

Solubility?

A

-Aqueous solution vs. Oily solution
-pH affect solubility

42
Q

Concentration?

A

High concentration of drug preparations are absorbed more rapidly

43
Q

Circulation?

A

-Increased Circulation, Increased Absorption (local massage or heat application)
-Decreased Circulation, Decreased Absorption (state of shock or disease state)

44
Q

Surface Area?

A

-Increase Surface Area, Increase Absorption

45
Q

First-Pass Effect?

A

-Combined action of bacterial and liver enzyme on drugs BEFORE reaching systemic circulation
-Not 100% of drug will be absorbed

46
Q

Factors that Influence Drug Distribution?

A

1) Blood Flow
2) Lipid Solubility of Drug
3) Molecular Size
4) Protein Binding

47
Q

Blood Flow?

A

-Most highly perfused organs receive most of the drug during the first few minutes after absorption
-Delivery of drug to muscle, viscera, skin and fat is slower

48
Q

Lipid Solubility of Drug?

A

-More lipid solution, better at crossing BBB
-Lipid insoluble drugs, that crosses membrane poorly, are restricted in their distribution and hence in their site of action

49
Q

Molecular Size?

A

Extremely large drugs are mainly confined to the plasma compartment

50
Q

Protein Binding?

A

-Distribution may be limited to drug binding to plasma proteins, only unbound drugs cross cell membrane

51
Q

Acidic drugs bind?

A

Serum Albumin

52
Q

Basic drugs bind?

A

Alpha-one Glycoprotein

53
Q

Drug Reservoirs?

A

1) Plasma Proteins
2) Fat
3) Bone
4) Cellular Reservoirs

54
Q

Plasma Proteins?

A

Many drugs bind to plasma proteins, this binding is predominantly reversible

55
Q

Fat can act as?

A

Drug Reservoir for highly lipophilic drugs

56
Q

Bone?

A

Drug may accumulate in bone by absorption onto bone-crystal surface and eventual incorporation into crystal lattice

57
Q

Cellular Reservoirs?

A

Some drugs may accumulate in muscle or other cells at higher concentrations than in extracellular fluids

58
Q

Blood-Brain Barrier?

A

-Adaptive
-Barrier is not absolute
-Protects against Xenobiotics

59
Q

Placenta?

A

-Cellular Barrier
-Not a barrier to drugs
-Fetus is to at least some extent exposed to essentially all drugs taken by mother

60
Q

Elimination is?

A

-Combination of Biotransformation and Excretion
-Process by which drugs are enzymatically altered mainly in liver and eventually excreted by kidneys

61
Q

Increases water solubility of drugs?

A

Biotransformation

62
Q

Most important for Biotransformation?

A

Liver, but can occur in other Organs too

63
Q

Biotransformation can Result in?

A

1) Inactive Metabolite
2) Metabolite that retain similar activity
3) Metabolite with altered activity
4) Bioactivated metabolites

64
Q

Inactive Metabolite?

A

Hydrolysis of Procaine to p-aminobenzoic acid results in loss of anesthetic activity

65
Q

Metabolite that retain similar activity?

A

-Codeine is demethylated to the more active analgesic morphine
-Like a “pro drug” needs to get converted to morphine via P450 enzymes (C2D6) which is polymorphic

66
Q

Metabolite with altered activity?

A

-Vitamin retinoid acid (Vitamin A) is isomerzied to anti acne agent, isoretinoic acid

67
Q

Bioactivated Metabolites?

A

-Prodrug, drug administered in inactive form
-Prodrug enalapril is hydrolyzed (by biotransformation enzymes) to enalaprilat, a powerful antihypertensive

68
Q

2 Main Reactions of Biotransformation?

A

-Phase I (Oxidation, Reduction and Hydrolysis)
-Phase II (Conjugation (via transferases))

69
Q

Phase I (Biotransformation)?

A

-Mainly degradative resulting in:
1) Inactivation
2) Change in activity, or
3) Conversion of a pharmacologically inactive compound (prodrug) to active drugs

70
Q

Main Phase I reactions?

A

Oxidation, Reduction and Hydrolysis

71
Q

Enzyme system most responsible for oxidation reactions?

A

Cytochrome P450 system (CTP)

72
Q

Phase II?

A

-Mainly involved in coupling of drug or frequently its polar metabolite from Phase I reaction to an endogenous substrate

73
Q

Phase II reaction?

A

Conjugation (via transferases)

74
Q

Oxidation is the most important?

A

Phase I reaction

75
Q

Oxidation Enzyme System is found in?

A

Microsomal Fraction (sER) of cells, mainly in liver and then in lung and kidney

76
Q

Oxidation Enzyme System is found in?

A

Microsomal Fraction (sER) of cells, mainly in liver and then in lung and kidney

77
Q

Cytochrome P450 system consists of 2 components?

A

-Cytochrome P450 oxidoreductase
-Cytochrome P450

78
Q

Cytochrome P450 requires?

A

Molecular oxygen and NADPH

79
Q

Is a family of isoenzymes with overlapping specificities?

A

Cytochrome P450

80
Q

Key Step in Oxidation?

A

Insertion of oxygen atom producing a non-stable intermediate which breaks down to yield final product

80
Q

Key Step in Oxidation?

A

Insertion of oxygen atom producing a non-stable intermediate which breaks down to yield final product

81
Q

Main Reactions Catalyzed by Oxidation?

A

-Dealkylation
-Hydroxylation
-Sulfoxide formation
-N-Oxidation
-Deamination of primary and secondary amines

82
Q

Non-Microsomal Oxidation System, most important enzymes of this class are?

A

-Alcohol Dehydrogenase
-Aldehyde Dehydrogenase
(Both located in cytosol)

83
Q

Hydrolysis?

A

-Carried out by enzymes known as:
-Esterases
-Amidases
-Peptidases

84
Q
A

Block 1: Pharmacology (9 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions