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Pharm > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

Vd equation

A

amount of drug/desired plasma concentration

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2
Q

Volume distribution assumes (2 things)

A

the drug distributes completely all at once, does not undergo any biotransformation or elimination

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3
Q

If a drug is lipophilic/hyrdophilic, it requires a ____/____ amount to achieve a plasma concentration

A

lipophilic=higher

hydrophilic=lower

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4
Q

How do you calculate a loading dose of an IV med

A

IV dose= Vd x plasma concentration/ bioavailability -which is 1

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5
Q

An acid ____ a H+

A

donates

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6
Q

A base ___ a OH+

A

accepts

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7
Q

What is ionization?

A

The process of when a molecule gains a positive or negative charge

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8
Q

Ionized or nonionized is more water soluble?

A

Ionized

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9
Q 
Explain the following for nonionized molecules:
Solubility
Active or nonactive?
Hepatic biotransformation?
Renal elimination?
Diffuses across lipid barrier?
A 
Solubility-lipophilic
Active or nonactive-active
Hepatic biotransformation? yes
Renal elimination? no
Diffuses across lipid barrier? yes
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10
Q 
Explain the following for ionized molecules:
Solubility
Active or nonactive?
Hepatic biotransformation?
Renal elimination?
Diffuses across lipid barrier?
A 
Solubility-hydrophilic
Active or nonactive-nonactive
Hepatic biotransformation? no
Renal elimination? yes
Diffuses across lipid barrier? no
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11
Q

What happens when you put a weak acid into a weak base?

A

It will become ionized. The acid wants to donate it’s protons and the base wants to accept it.

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12
Q

What happens when you put a weak acid into an acid?

A

It will be nonionized. Both acids want to donate their protons so they both retain them.

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13
Q

Name the 3 key plasma proteins

A

Albumin, AAG (alpha-1 acid glycoprotein), beta-globulin

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14
Q

Do the following bind to acid or bases? Albumin, AAG, beta-globulin

A

Albumin-acids, AAG & beta-globulin-bases

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15
Q

Which conditions decrease albumin?

A

Liver disease, renal disease, old age, malnutrition, pregnancy

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16
Q

Which conditions increase a1-acid glycoprotein?

A

surgical stress, MI, Rheumatoid arthritis, chronic pain, advanced age

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17
Q

Which conditions decrease a1-acid glycoprotein?

A

pregnancy, neonate

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18
Q

Are protein binding and plasma concentration inversely or directly proportional?

A

inversely. As protein building increases, plasma concentration decreases.

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19
Q

What are phase 1 reactions?

A

Oxidation, reduction, hydrolysis

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20
Q

What is oxidation?

A

Adds an oxygen molecule to a compound. Involves loss of electrons.

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21
Q

What is reduction?

A

Adds electrons to a compound.

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22
Q

What is hydrolysis?

A

Adds water to a compound to split into 2 parts

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23
Q

What is a phase 2 reaction? What happens?

A

Conjugation, adds an endogenous, highly polar, water substrate to make it inactive and water soluble.

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24
Q

What are CP 450 inducers? What happens?

A

They break down drugs FASTER. Increased clearance, decreased plasma concentration, re-dosing may be needed.
Smoking, barbituates, ethanol, phenytoin, carbamazepine, rifampin

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25
Q

What are CP 450 inhibitors? What happens?

A 
They SLOW metabolism of drugs. Decreased clearance, increased plasma concentration, may have to decrease dose. 
Grapefruit
Cimetidine
Omeprazole
Isoniazid
SSRI's
Erythromycin
Ketoconazole
26
Q

What is pharmacokinetics?

A

What the body does to the drug

27
Q

What is pharmacodynamics?

A

What the drug does to the body

28
Q

What does ADME mean in pharmacokinetics?

A

A-absorption, D-distribution, M-metabolism, E-elimination

29
Q

Conditions that affect site of absorption

A

Blood flow, surface area, membrane thickness, metabolism, GI motility, pH, presence of other substance

30
Q

Rate of diffusion equation

A

Concentraion gradient x SA x diffusion coefficient/ membrane thickness

31
Q

The rate of diffusion is directly proportional to what?

A

Concentration gradient and SA

32
Q

The rate of diffusion is inversely related proportionally to what?

A

Membrane thickness

33
Q

What is the definition of bioavailability?

A

Fraction of unchanged drug that reaches the systemic circulation following administration

34
Q

Aqueous Diffusion: Flow (with or against) a concentration gradient.

A

concentration, with

35
Q

Lipid Diffusion: goes from (greater/less) to (greater/less) concentration.

A

greater to less

36
Q

Active transport diffusion

A

uses ATP (Na/K pump)

37
Q

Facilitated Diffusion

A

Passive action without the use of ATP, (glucose and insulin)

38
Q

Endocytosis diffusion

A

the wall of the membrane engulfs the molecule. (Phagocytosis, Pinocytosis)

39
Q

Protein binding can affect:

A

Distribution of drugs, potency, elimination

40
Q

Hepatic microsomal enzymes are mainly found in the ______ of the _____. Examples:

A

endoplasmic reticulum, liver. Ex: Cytochrome P-450, Acetyl CoA, Transferases

41
Q

CYP-2D6 inducers.

A

Phenytoin, Carbamazepine, dexamethasone

42
Q

CYP-2D6 Inhibitors

A

Isoniazid, SSRI’s, Quinidine

43
Q

What is absolute bioavailability?

A

the amount of drug that reaches the systemic circulation from an IV dose

44
Q

What is relative bioavailability?

A

the amount of drug that reaches the systemic circulation from a non-IV form

45
Q

Name fastest to slowest routes to reach peak plasma concentration:

A

(I) (T)hink (I) (C)an (P)lease (E)veryone (B)ut (S)usie & (S)ally
IV, tracheal, Intercostal, Caudal, Paracervical, Epidural, Brachial Plexus, Sciatic/Subarachnoid, Subcutaneous

46
Q

Ion trapping is:

A

a build-up of a higher concentration across a cell membrane due to the pKa value and difference in pH across the membrane.

47
Q

Define clearance

A

volume of plasma that is cleared of drug per unit time

48
Q

What are the major clearing organs

A

liver, kidney

49
Q

Define steady state

A

occurs when the amount of drug entering the body is equivalent to the amount of drug being eliminated from the body.

50
Q

Clearance is directly proportional to:

A

blood flow to clearing organ, extraction ratio, drug dose

51
Q

Clearance is inversely proportional to:

A

half life, drug concentration in the central compartment

52
Q

How many half-times must elapse to achieve steady state?

A

5

53
Q

Renal excretion of drugs involves__ (3 things)

A

glomerular filtration, active tubular secretion, passive tubular secretion

54
Q

Renal clearance is inversely correlated with:

A

age and creatinine clearance

55
Q

The distribution phase of elimination or the ___ phase is:

A

alpha; redistribution of drug from the plasma and vessel rich group to the less perfused tissues of the peripheral compartment

56
Q

The elimination phase or ____ phase:

A

after distribution slows, get slow continuous elimination from the central compartment

57
Q

Weak acids combine with salts to make ____ charged ions

A

positively. Ex sodium thiopental, sodium nitroprusside

58
Q

Weak bases combine with salts to make ____ charged ions

A

negatively. Ex: morphine sulfate, lidocaine hydrochloride

59
Q

The higher the pka, the _____ the amount of drug in the nonionized form

A

greater

60
Q

What is the drug class that doesn’t fall into an acid or base?

A

NMBDs

61
Q

CYP-2D6 deficient individuals have less response to ____

A

codeine

62
Q

CYP-2D6 inducer individuals have decreased response to ____

A

Zofran

Pharm (12 decks)

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