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RENAL II - Pharm Exam > General principles of pharmacology > Flashcards

General principles of pharmacology Flashcards

1
Q

Pharmacodynamics

A

Mechanism of action, what drug does to your body

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2
Q

Pharmacokinetics

A

Time course, how your body metabolizes drug

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3
Q

Drug action

A

Change at the molecular level, biochemical event

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4
Q

Drug effect

A

**Clinical practitioner more concerned with this

Change in physiological function

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5
Q

MEC

A

Minimum effective concentration: concentration needed to start seeing drug effect

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6
Q

Maximum tolerated concentration

A

Concentration above which toxicity occurs

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7
Q

Effect of drugs is dose dependent

A

Some level before which no effect occurs
Some level above which no extra effect occurs
Ideal range of drug concentration between when drugs begin being effective and cutoff for toxicity

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8
Q

Therapeutic window

A

Between MEC and max tolerated concentration

Depends on absorption, distribution, elimination, and drug action + effect

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9
Q

Percutaneous administration

A

Slow and sustained absorption

Lipid soluble > water soluble

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10
Q

Enteral

A

Via GI

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11
Q

Sublingual administration

A

Rich blood flow

More rapid than oral

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12
Q

Oral administration

A 
Most common but slower
2 barriers to absorption
Intestine > stomach
Absorption highly variable among patients (gastric emptying, pH, food, other drugs)
Drug recall is possible
Lipid > water soluble
Some drugs (PROTEINS) inactivated in GI
First pass metabolism
GI irritation
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13
Q

Rectal administration

A

For vomiting patient

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14
Q

Parenteral

A

Non-oral

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15
Q

IV

A 
No barrier to absorption - easier to control concentration
Rapid but NO recall
Needs to be aqueous solution
No big "chunks" due to possible embolism
Possible infection at injection site
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16
Q

Intra-arterial

A

More diagnostic

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17
Q

Subcutaneous injection

A

Barriers to absorption: Slower absorption and sustained action
Can be poorly water soluble
Allows for depot preparations

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18
Q

Protein drugs

A

Most need to be delivered IV or SQ

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19
Q

Intramuscular injection

A

Only barrier is capillary, high blood flow in muscle
Time is dictated by water solubility (water > lipid)
Can inject oily and particulate matter

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20
Q

Lipid/oily drugs

A

Oral, SQ, IM, percutaneous

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21
Q

Water soluble drugs

A

Better with IV, faster with IM

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22
Q

Particulate drugs

A

IM

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23
Q

Depot preparations

A

Can release effective amounts of drug for weeks or months

SQ or IM

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24
Q

Inhalation

A

Keep localized to minimize systemic effects
Large SA
Particle size important

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25
Q

Intranasal

A

Lots of it swallowed

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26
Q

Absorption

A

Movement of drug into the blood
Rate - how soon effects start
Amount - intensity of effects

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27
Q

Rate of dissolution

A

Dissolved = free in solution, not bound, free to move into cells
Smaller size and liquid are better

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28
Q

Concentration gradient

A

Drug always moves down gradient

Blood flow readily changes gradient

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29
Q

Lipid absorption

A

Faster

Can more easily cross the membrane (hydrophobic)

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30
Q

Charged molecules

A

CANNOT diffuse

31
Q

pH

A

Determine amount of drug that is ionized

32
Q

Tissue condition

A

Damaged tissue less likely to absorb

33
Q

Distribution

A

To all areas perfused with blood

Can move into interstitial fluid or within cells

34
Q

Volume of distribution

A

Hypothetical volume of fluid into which the drug is distributed
May calculate to be larger than 42L if drugs build up in tissues

35
Q

Water compartments

A

Plasma: 4L
Extracellular: 14L
Total: 42L

36
Q

Drug redistribution

A

Drugs are constantly moving along gradient into different compartments

37
Q

Blood brain barrier

A

Lipid soluble, nonpolar, noncharged cross more easily

38
Q

Drug elimination

A

In urine, breath, stool, or sweat

Unchanged or biotransformed (active, inactive, larger or smaller)

39
Q

Major site of biotransformation

A

Liver

40
Q

Major biotransformation pathway

A

Conjugation: larger and more water soluble

41
Q

Metabolites that are too large

A

Secreted into bile

42
Q

Major form of elimination

A

Urine
Involves glomerular filtration of plasma
Drugs may be reabsorbed

43
Q

Free drug

A

Unbound drug in solution

44
Q

Most common type of drug movement into cell

A

Diffusion

Function of lipid solubility, conc. gradient, size, and charge

45
Q

Concentration of drug at site of action (cell) is function of

A

absorption, biotransformation, distribution, and elimination

46
Q

Active transport

A

Special tissues: renal, choroid, hepatocytes

47
Q

Rate of diffusion

A

Directly related to concentration gradient

Nonionized only

48
Q

Maintain steep conc. gradient

A

High blood flow

49
Q

Ionized and polar molecules

A

More water soluble

Harder to cross membrane

50
Q

Nonionized and nonpolar molecules

A

More lipid soluble

Easier to cross membrane

51
Q

Concentration of ionized and nonionized form

A

Influenced by pH

52
Q

High lipid water partition coefficient (above 1)

A

Very lipid soluble

53
Q

Low lipid water partition coefficient (below 1)

A

Very water soluble

54
Q

Weak acid in more acidic environment (pH<pKa)

A

NONIONIZED

55
Q

Weak base in more acidic environment (pH<pKa)

A

IONIZED

56
Q

Strong acids and bases

A

Not effected by pH
Always ionized
Drugs are mostly weak electrolytes

57
Q

Excretion of weak acids increases with

A

Basic urine

Less reabsorbed

58
Q

Excretion of weak bases increases with

A

Acidic urine

Less reabsorbed

59
Q

Plasma concentration at equilibrium of weak acid

A

Higher than intracellular

60
Q

Plasma concentration at equilibrium of weak base

A

Lower than intracellular

61
Q

Ionized with large hydrophobic structure

A

May diffuse easily if hydrophobic enough

62
Q

Why is IV drug so concentrated near stomach?

A

Lots of H+ available to ionize drug and trap in there

63
Q

Acidosis

A

Weak acid more nonionized and moves into tissues

64
Q

Alkalosis

A

Weak base ionized, builds up in plasma, and is then readily excreted

65
Q

Quaternary salts

A

Permanently charged
Does not cross BBB
Quickly excreted if given IV

66
Q

Anion transport

A

Penicillins and related antibiotics

67
Q

Cation transport

A

Quaternary ganglionic blocking drugs

68
Q

Albumin

A

Primary binding protein in plasma

Favors weak acids and lipid soluble drugs

69
Q

Drug bound to protein

A

Cannot be used, cannot be filtered in kidney, and cannot cross membrane

70
Q

Protein binding affects

A

Loading dose, all binding proteins must be saturated before therapeutic concentrations can be achieved
Elimination may be prolonger

71
Q

Drug interactions and protein binding

A

More than one drug may compete for same binding protein

Most problematic when drug binds in excess, has low Vd, is eliminated slowly, and has low therapeutic index

72
Q

Drugs may displace endogenous substances

A

Thyroxine, steroids, billirubin

73
Q

Drugs can be pre-bound to protein

A

Slower release

74
Q

Drug redistribution concerning brain

A

High lipid solubility allows to enter quickly and lots of blood flow changes gradient causing drug to leave quickly as well
Ex. thiopental

RENAL II - Pharm Exam (7 decks)

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