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Pharmocology > Pharmacokinetics - Wolff > Flashcards

Pharmacokinetics - Wolff Flashcards

1
Q

4 pharmacokinetics

A

Absorption
Distribution
Metabolism
Excretion

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2
Q

3 Pharmacodynamics types

A
  1. Drug- receptor interactions
  2. Patient’s functional state
  3. Placebo effects
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3
Q

4 things that can cause pharmacokinetics and pharmacodynamics

A

Physiological variables
Pathological variables
Genetics
Drug interactions

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4
Q

Medication error is reported where

A

To the NCCMERP (national coordination council for medical error report ion and prevention

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5
Q

What are the 4 basic pharmacokinetic processes

A

A : absorption (GI, intramuscular)
D : distribution (site of action and other places like liver and kidney)
M : metabolism (liver and kidney)
E : excretion

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6
Q

What effects absorption

A
  • rate of dissolution of tablet
  • SA of tablet
  • BF
  • lipid solubility
  • pH partitioning
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7
Q

Enteral

A

Rectal
Oral
Sublingual

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8
Q

Parenteral

A

Intravenous
Intramuscular
Subcutaneous

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9
Q

Inhalation con

A

Variable distribution

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10
Q

Drug going TO cell mechanisms of transport

A
  1. Simple diffusion (direct penetration of cell membrane)

2. Unimportant carrier / channel (facilitated diffusion)

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11
Q

Drug going OUT of cell mechanisms of transport

A 
Active transport (energy in and drug out)
EX: p-glycoproteins and MDR1
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12
Q

NR4 drug structure , quaternary ammonium

A

Has a net positive charge and can’t cross membrane

COPD

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13
Q

Amino glycecydes

A

Cant cross membrane and positive charge

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14
Q

Weak acid can cross the membrane of cells when

A

In its UNIONIZED form = (In the stomach its very acidic and can cross membrane)
(Cant cross in basic environments)

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15
Q

Weak base can cross the membrane of cells when

A

In its unionized form which happens in more basic environments (not in the stomach)

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16
Q

When you eat a lot f an acidic drug what happens to the urine

A

A lot of the H+ get donated to the NH3, and becomes NH4+, = basic

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17
Q

Ka

A

Rate constant for absorption

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18
Q

S

A

Salt factor , less than or equal to 1 always

Every drug is in salt form, with some parent compound amount in it

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19
Q

F

A

Bioavailability fraction of drug that reaches bloodstream , also less than or equal to 1
= Area under Curve (route used)/ AUC (intravenous route)

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20
Q

Amount absorbed

A

S x F x Dose

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21
Q

Bioavailability is always =

A

< or = to 1

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22
Q

Concentration of drug in plasma is calculated how

A

Cp= (SxFxDose)/Vd
S : 1 * if not given
F : 1 *if not given
Vd : volume of distribution

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23
Q

Vd is calculated how

A

Amount of Drug in Body/ Plasma Concentration

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24
Q

ECV is calculated how (extracellular volume)

A

1/3 x TBW (total body water)= ECV

EVC x 0.25 = plasma volume

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25
Q

TBW is what

A
  • 55% body weight (Kg) in women

- 60% body weight (Kg) in men

26
Q

Some drugs are concentrated and accumulated in the peripheral sites (not EVC, TBW)

A

Like the GI, bones, kidney, or liver and this causes the an APPARENT VOLUME (has a a large Vd muscle larger then TBW)

27
Q

What causes distribution

A

CO
BF
Ability to exit and enter vascular vessels

28
Q

Which drugs cant cross the vascular membranes

A

Drugs bound to plasma proteins
(Only free drugs are bio active (alpha))
- dangerous if another drug is added that displaces the first drug from the plasma proteins and increases in amount

29
Q

What drugs can go to brain

A

Only lipid solvable

Polar an ionized can only if there is a transporter available

30
Q

Drug metabolites must be

A

Polar so they can be trapped in the renal tubular fluids

31
Q

Phase 1 drug biotransformation is

A

Reduction oxidation hydrolysis

*P450

32
Q

Oxidation happens where

A

P450 cytochrome in the smooth ER (microsomes part of liver)

33
Q

Which are the most common Cytochrome P450 enzymes in drug metabolism

A
  1. CYP3A
  2. CYP2D6
  3. CYP2C
34
Q

CYPs do what when drug binds

A

Increases metabolism or slows down the metabolism and all other drugs that bind to this

35
Q

What is a common CYP inhibitor

A

metronidazole, grapefruit juice

So if you drink grapefruit ice with metronidazole it slows down the CYP metabolism of the drug

36
Q

Phase 2 biotransformation

A

Conjugation bu making drug polar like water

  1. Glucuronidation
  2. Sulfation
37
Q

Areas drug can go from oral route

A

From the GI it can got to:

  1. Portal vein ——> liver
  2. Liver —> bile in to GI OR IVC to heart
  3. Heart to general circulation unless excreted as bile
38
Q

Filtered by glomerular filtration

A

YES Small molecule drugs

NO Protein bound drugs

39
Q

Passive tubular reabsorption

A

Lipid solvable drugs

Unionized weak acid and weal bases

40
Q

Active tubular secretion

A

Protein bound drugs

41
Q

First order kinetics:

  1. Excretion rate
  2. Clearance rate
A
  1. Mass eliminated per unit time (as concentration increases, it increases)
  2. volume needed to remove all depending on flow rate (as concentration changes it remains constant)
42
Q

Renal clearance is calculated as

A

C = (U x V) / (P)
U- urine concentration
V- flow rate
P- plasma concentration

43
Q

eGFR is calculated as

A

[((140-age) x (BW)) / (72 x Scr) ] x [0.85]

If its a woman

44
Q

Genetic Basis : Plasma Esterase

A

Succinylcholine : Apnea for long time

45
Q

Genetic Basis : X NADH methemoglobin reductase

A

Nitrites, sulfonamides, primaquine…. : Hereditary methemoglobinemia

46
Q

Genetic Basis : Low amount of liver acetyl transferase

A

Isoniazid + others : increase drug toxicity

47
Q

Genetic Basis : X G6PD

A

= low GSH

Primaquine + others : Drug induced hemolytic anemia

48
Q

Genetic Basis : X porphobilinogen deaminase

A

Barbiturates, estrogens, sulfonamides, chloroquine : acute intermittent porphyria

49
Q

which drug can cause liver failure

A

acetominophen, lipid lowering drugs, antifungals, immunosuppressants, TB drugs, antiseizure drugs, antiretroviral drugs

50
Q

which drugs can give long QT interval

A

causing Vfib, Terfenadine (Seldane) interacts with antifungals and causes Vfib

51
Q

diethylstilbestrol (DES) drug

A

prevents spontaneous abortion in high risk pregnancies

- daughters have high risk to get vaginal or uterine cancers

52
Q

Neonates and drugs

A

Have more TBW
Not well developed BBB
Low albumin (plasma proteins)

53
Q

Children > 1 and drugs

A

ADE = similar to adults

M (metabolize) = faster then adults

54
Q

Elderly and drugs

A 
No absorption changes
- lower albumin 
- Lower metabolism
- lower excretion 
= adverse effects more common
(B-blockers less effective, oral anticoagulants more effective)
55
Q

Pregnancy and drugs

A
  • lower GI motility and bowel tone = higher time of absorption
  • higher hepatic metabolism
  • higher RBF= higher GFR
56
Q

Drugs that pass placenta most easily

A

Lipid solvable

57
Q

Zero order kinetics

Means

A

Constant amount eliminated per time

  • elimination is saturated
  • amount eliminated is independent of drug concentration
58
Q

Zero order kinetics equation + example

A

dCp/dt = k

Ethanol

59
Q

First order kinetics means

A

Constant fraction is eliminated per unit time

  • not saturated during elimination
  • amount eliminated is directly dependent on concentration
60
Q

First order kinetics equation

A

dCp/dt= kCp

61
Q

First order and concentration during each half-life

A

Each half-life backwards doubles the concentration (97% is eliminated after 5 half-lives)

Pharmocology (3 decks)

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