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z F1: Pharmacology > Exam 2 > Flashcards

Exam 2 Flashcards

1
Q

Absorption

A

movement of drugs into the bloodstream from the site of delivery
-stomach
-skin
-vein

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2
Q

Factors accepting absorption

A

Drug transport
Physicochemical properties
Routes of Administration

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3
Q

When pH is lower than pKa which form will predominate

A

protonated

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4
Q

pKA - pH
4.2 - 7.4 = (-) what occurs
weak acid

A

unprotonated form predominates, drug can not cross barrier because it has a negative charge

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5
Q

pKa - pH
9.4 - 1.4 = (+) what occurs
weak base

A

protonated form predominates
can’t cross barrier, charge

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6
Q

Fractional extent to which a dosage of drug reaches the systemic circulation is dependent on what 3 factors

A

Route of administration
Absorption
Metabolism

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7
Q

Area under the curve (AUC) indicates what

A

overall amount of drug in blood after a given dose (over time)

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7
Q

Three factors that impact drug distribution

A

Protein binding
Tissue binding
Transporters

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8
Q

oral administration: absorption and limitations

A

absorption: variable, must cross intestinal mucosa
limitations: subject to metabolism

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9
Q

How is uptake governed by pH in oral absorption

A

-weak acids absorbed from stomach and upper intestine
-weak bases absorbed better from upper intestine rather than from stomach

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10
Q

Oral absorption factors

A

-accelerating gastric emptying will increase rate of absorption
-delaying gastric emptying will decrease rate of absorption

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11
Q

Controlled release preparations in oral absorption

A

-designed for slow, uniform absorption of drug
-reduce frequency of administration
-more uniform blood levels

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12
Q

Limitations of controlled release preparations

A

dose dumping increases toxicity
increase stomach acidity with high-fat meal

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13
Q

sublingual administration

A

-venous drainage through superior vena cava
-useful with more lipid soluble drugs

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14
Q

transdermal absorption

A

intact skin provides a lipid barrier for transdermal absorption
oily vehicles (improves permeability)

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15
Q

Rectal administration

A

absorption may be incomplete
used when patient is vomiting or unconscious

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16
Q

Parenteral administration

A

-injections allow for absorption by simple diffusion from frug depot into bloodstream
-avoid first-pass metabolism

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17
Q

IV injection

A

-useful for poor soluble suspensions and depot formulations
-not good for large volumes
-potential pain at injection site

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18
Q

IM injection

A

-self-administration
-precluded during anticoagulant therapy
-many variabilities

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19
Q

Intraarterial injection

A

-circumvented to deliver drug directly to tissue or organ
-used for diagnostic agents and chemo

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20
Q

Intrathecal injection

A

injection into space surrounding spinal cord, useful for drugs that cannot cross the blood brain barrier or limiting effect to spinal cord or meninges

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21
Q

pulmonary absorption

A

absorption through pulmonary epithelium and mucous membranes of the respiratory tract, avoids first pass hepatic metabolism, directs application of drug to target tissue

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22
Q

Pharmaceutical equivalence

A

same active form, concentration, dosage form, and route of administration

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23
Q

Bioequivalence

A

indicated when rates of extent of bioavailability of active pharmaceutical ingredient (API) do not differ significantly

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24
Q

What is drug distribution dependent on

A

cardiac output, blood flow, capillary permeability, tissue volume

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25
Q

Redistribution of drugs

A

Rapid distribution to muscle and liver
Slower distribution to adipose tissue

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26
Q

What carriers help drugs bind to plasma protein

A

albumin for acidic drugs
a1-acid glycoprotein for basic drugs

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27
Q

Tissue binding

A

-Accumulate by active transport
-Lipid soluble drugs stored in body fat

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28
Q

What drugs bind to bone tissue

A

Tetracycline and aminoglycoside antibiotics

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29
Q

Blood brain barrier

A

-composed of capillary endothelial cells
-regulates distribution of chemicals to the brain
membrane transporters (efflux and influx)

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30
Q

What glial cells are located where

A

BBB
(includes astrocytes and microglia)

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31
Q

what cells separate cerebrospinal fluid from blood

A

epithelial cells

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32
Q

Phase 1 functionalization reactions

A

Introduce or expose functional groups
Result in both active and inactive compounds
Net result is water-soluble compounds that can be excreted into urine

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33
Q

Phase 2 biosynthetic (conjugation) reactions

A

-covalent linkage between functional group on drug
-polar conjugates usually inactive and excreted rapidly

34
Q

What is first order kinetics?

A

-constant fraction of drug is eliminated per unit time
-drug metabolism proportional to plasma concentration

35
Q

What is zero order kinetics?

A

-limited metabolic capacity
-constant amount of drug metabolized per unit of time

36
Q

some drugs alter metabolism of other drugs through

A

-induction of enzymes (increased expression of drug metabolizing enzymes)
-inhibition of enzymes (blockade of drug metabolizing enzymes)

37
Q

Glomerular filtration

A

only unbound drug filtered into tubular lumen from the blood

38
Q

Active proximal tubular secretion

A

-ATP-binding cassette transporters secrete anions and metabolizes into tubular fluid
-Other ABC transporters are more selective for organic cations or neutral substrates

39
Q

Active distal tubular reabsorption

A

-From tubular lumen to systemic circulation by membrane transporters
-most reabsorption is by nonionic diffusion

40
Q

Renal excretion

A

concomitant reabsorption of non-ionized weak acids and weak bases, depends on pH

41
Q

Biliary excretion

A

potential recycling through reabsorption from GI tract to systemic circulation

42
Q

What is F (bioavailability)

A

fraction of a drug absorbed into the systemic circulation
-depends on route of administration, absorption, metabolism, excretion

43
Q

What is V (volume of distribution)

A

apparent space of body available to contain a drug based on amount given and concentration in systemic circulation
-impact by plasma binding protein, age, gender, body composition

44
Q

What is CL (clearance)

A

measures body efficiency in drug elimination
-use in designing dosing regimens
-can follow either first order or zero order

45
Q

Steady State Concentration (Css)

A

Concentration achieved when intake of drug is in dynamic equilibrium with elimination of drug

46
Q

Km and vm

A

Km is the concentration at which half max rate of elimination is reached
vm is the max rate of elimination

47
Q

Clinical pharmacokinetics parameters can be utilized to design dosing regimens

A

maintain plasma concentrations within therapy window
maintenance doses can be adjusted
loading doses used to achieve rapid onset

48
Q

Maintenance Dose

A

Series of repetitive doses or continuous infusion to maintain steady state

49
Q

What can polymorphisms impact

A

Protein structure
Function
Pattern of expression in

50
Q

SNPs

A

May change coding for proteins or impact expression

51
Q

Insertions or deletions (indels)

A

Like SNPs (change coding)

52
Q

Copy number variations

A

Gene duplications or deletions

53
Q

Non-synonymous (missense)

A

Change impacts protein sequence
Amina acid substitution or stop translation

54
Q

Synonymous (sense)

A

Change does not impact protein structure
May impact expression

55
Q

Non-coding SNPs

A

3’ or 5’ untranslated regions (promoter or enhancer regions)
Intronic/intergenic regions

56
Q

UGT1A1

A

TA repeats (insertions) in promoter impact expression of enzyme
-range is from 4 to 9 repeats
-6 or 7 repeats most common

57
Q

CYP2D6

A

Ultra rapid metabolized phenotype implicated in variable responses to antidepressants therapy

58
Q

CYP2D6

A

20-25% of drugs are metabolized by the enzyme
Can have poor or ultra-rapid metabolism

59
Q

What does poor drug metabolism do in your body

A

Can’t eliminate drugs so they stay in the system and produce toxic effects

60
Q

CYP3A5 expressed in higher percentage of individuals of ________ descent than in caucasians

A

african

61
Q

SNP in intron __ encode stop codon, resulting in truncated protein

A

3

62
Q

What are the two main classes of transporters and what do they do

A

SLC-include both active and non-active transporters
ABC-active transporters needing ATP

63
Q

What are the three adverse effects of membrane transporters

A

decreased uptake in clearance drugs
enhanced uptake or reduced efflux from target organs
decreased efflux of endogenous compounds

64
Q

Passive diffusion

A

electrochemical potential gradient

65
Q

Facilitated diffusion

A

Membrane SLC transporters facilitate diffusion

66
Q

Primary active transport

A

ABC transporters hydrolyze ATP through intrinsic ATPase activity

67
Q

Secondary active transport

A

SLC transporters move one solute against ECG by transporting another solute with ECG

68
Q

Vectorial transport

A

The net flow of drugs from one compartment to another depending opinion the relative orientation and function of multiple transporters

69
Q

ADME transport of vectorial transport

A

Absorption - absorb in small intestine
Distribution - CNS penetration at the BBB
Metabolism - Hepatobiliary transport in the liver
Elimination - tubular secretion in the kidney

70
Q

Role for type 2 nuclear receptors

A

Ligand binding and formation of heterodimers
Binding to specific elements in enhancer regions of target genes
Changes in transcription or transporters and other proteins

71
Q

Altered transporter function has been linked to human disease what receptor is tangier disease

A

ABCA

72
Q

Altered transporter function has been linked to human disease what receptor malfunction results in amyotrophic lateral sclerosis

A

High affinity glutamine and neutral amino acid transporter

73
Q

7 ABC transporters are identified. Which two play important roles in drug transport

A

ABCB1
ABCC
ABCG

74
Q

Induction of ________ can decrease systemic exposure to substrates such as digoxin

A

ABCB1

75
Q

Inhibition can reduced _________ of digoxin

A

Excretion

76
Q

Role:
OATP, OAT
OCT

A

OATP, OAT- transport anions
OCT- transports cations

77
Q

Role of NTCP

A

Transports bile salts

78
Q

Phase 1 bio transformation reactions

A

Increase water solubility by exposing functional groups
CYP 450 enzymes
Epoxied hydrolases
Flavin containing monooxygenases

79
Q

Phase 2 conjugating enzymes

A

Increase hydrophilicity and molecular weight
Inactive compounds
Transferases (UPD, sulfur, glutathione, acetyl, methyl)

80
Q

CYP 3A 4/5 involved with metabolism of _____% of all drugs

A

50

81
Q

UDP UGT1A1 is important for metabolizing drugs and bilirubin what disease can it cause and what is it effects

A

Gilbert’s syndrome
Toxic for patients with low binding levels

82
Q

Induction of drug metabolizing enzymes increase metabolism thereby ________ drug exposure and _________ clearance

A

Decreasing
Enhancing

z F1: Pharmacology (4 decks)

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