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Pharmocology > Pharmacokinetics - Wolff > Flashcards

Pharmacokinetics - Wolff Flashcards

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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
TBW is what
- 55% body weight (Kg) in women | - 60% body weight (Kg) in men
26
Some drugs are concentrated and accumulated in the peripheral sites (not EVC, TBW)
Like the GI, bones, kidney, or liver and this causes the an APPARENT VOLUME (has a a large Vd muscle larger then TBW)
27
What causes distribution
CO BF Ability to exit and enter vascular vessels
28
Which drugs cant cross the vascular membranes
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
What drugs can go to brain
Only lipid solvable | Polar an ionized can only if there is a transporter available
30
Drug metabolites must be
Polar so they can be trapped in the renal tubular fluids
31
Phase 1 drug biotransformation is
Reduction oxidation hydrolysis | *P450
32
Oxidation happens where
P450 cytochrome in the smooth ER (microsomes part of liver)
33
Which are the most common Cytochrome P450 enzymes in drug metabolism
1. CYP3A 2. CYP2D6 3. CYP2C
34
CYPs do what when drug binds
Increases metabolism or slows down the metabolism and all other drugs that bind to this
35
What is a common CYP inhibitor
metronidazole, grapefruit juice | So if you drink grapefruit ice with metronidazole it slows down the CYP metabolism of the drug
36
Phase 2 biotransformation
Conjugation bu making drug polar like water 1. Glucuronidation 2. Sulfation
37
Areas drug can go from oral route
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
Filtered by glomerular filtration
YES Small molecule drugs | NO Protein bound drugs
39
Passive tubular reabsorption
Lipid solvable drugs | Unionized weak acid and weal bases
40
Active tubular secretion
Protein bound drugs
41
First order kinetics: 1. Excretion rate 2. Clearance rate
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
Renal clearance is calculated as
C = (U x V) / (P) U- urine concentration V- flow rate P- plasma concentration
43
eGFR is calculated as
[((140-age) x (BW)) / (72 x Scr) ] x [0.85] | If its a woman
44
Genetic Basis : Plasma Esterase
Succinylcholine : Apnea for long time
45
Genetic Basis : X NADH methemoglobin reductase
Nitrites, sulfonamides, primaquine.... : Hereditary methemoglobinemia
46
Genetic Basis : Low amount of liver acetyl transferase
Isoniazid + others : increase drug toxicity
47
Genetic Basis : X G6PD
= low GSH | Primaquine + others : Drug induced hemolytic anemia
48
Genetic Basis : X porphobilinogen deaminase
Barbiturates, estrogens, sulfonamides, chloroquine : acute intermittent porphyria
49
which drug can cause liver failure
acetominophen, lipid lowering drugs, antifungals, immunosuppressants, TB drugs, antiseizure drugs, antiretroviral drugs
50
which drugs can give long QT interval
causing Vfib, Terfenadine (Seldane) interacts with antifungals and causes Vfib
51
diethylstilbestrol (DES) drug
prevents spontaneous abortion in high risk pregnancies | - daughters have high risk to get vaginal or uterine cancers
52
Neonates and drugs
Have more TBW Not well developed BBB Low albumin (plasma proteins)
53
Children > 1 and drugs
ADE = similar to adults | M (metabolize) = faster then adults
54
Elderly and drugs
``` No absorption changes - lower albumin - Lower metabolism - lower excretion = adverse effects more common (B-blockers less effective, oral anticoagulants more effective) ```
55
Pregnancy and drugs
- lower GI motility and bowel tone = higher time of absorption - higher hepatic metabolism - higher RBF= higher GFR
56
Drugs that pass placenta most easily
Lipid solvable
57
Zero order kinetics | Means
Constant amount eliminated per time - elimination is saturated - amount eliminated is independent of drug concentration
58
Zero order kinetics equation + example
dCp/dt = k | Ethanol
59
First order kinetics means
Constant fraction is eliminated per unit time - not saturated during elimination - amount eliminated is directly dependent on concentration
60
First order kinetics equation
dCp/dt= kCp
61
First order and concentration during each half-life
Each half-life backwards doubles the concentration (97% is eliminated after 5 half-lives)

Pharmocology (3 decks)

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