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Block 1 Week 7 > Buxton Block 1 week 7 > Flashcards

Buxton Block 1 week 7 Flashcards

1
Q

What are the physicochemical factors in transfer of drugs across membranes?

A

Lipid-water partition coefficient (ratio of hydrophobicity to pass through membrane)
Size of the molecule
Concentration gradient
pH of the environment for acids and bases
Active versus passivetransport
Paracellular (intercellular) transport

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2
Q

what kind of groups readily cross plasma membranes?

A

nonionizable groups

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3
Q

If you want your drug to be excreted you want to trap it in what form?

A

the ionizable form ( A- + H+)

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4
Q

(blank) are involved in all aspects of drug absorption distribution metabolism and excretion

A

Transporters

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5
Q

(blank) of the genes in the human genome code for transporters or transporter-related proteins.

A

~7%

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6
Q

The functions of membrane transporters may be participate in what two types of transpot?

A

active and facilitated

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7
Q

What are the two big families of transporters? which one is active and which one is facilitated?

A

ABC (ATP binding cassette, Active)

SLC (solute carrier, Facilitated)

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8
Q

ATP binding cassette (ABC transport) hydrolyzes ATP to drive the drug across (blank).

A

Membrane

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9
Q

What is P-glycoprotein and why is it important?

A

It is a ABC transporter and is over expressed in cancer and a multi drug resistant cell (it transports drugs out of the cell)

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10
Q

Serotonin transporter (SERT); dopamine transporter (DAT) are examples of what kind of transporters?

A

solute carrier transporters

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11
Q

Getting drugs to target tissues depends on profusion of (blank).

A

blood flow

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12
Q

What organs will a drug reach first based on profusion of blood flow?

A

1) brain, heart, liver and kidneys
2) skeletal muscle and skin
3) adipose tissue

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13
Q

The primary desired effect of drug metabolism is to accelerate (blank)

A

elimination

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14
Q

Drugs can be transformed into what 2 metabolites?

A

inactive and active metabolites

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15
Q

What are the three metabolizing reactions?

A

oxidative
hydrolytic
conjugative

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16
Q

What are the 2 phases of metabolism?

A

metabolism, conjugation

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17
Q

Prozac can act on what?

A

the SLC transporter to keep serotinin in the synapse to increase feeling good

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18
Q

What are the three ways that drugs act on targets in an adverse way?

A
  • drugs can act on clearance organs by decreasing ability to rid body of drug (kidney liver)
  • drugs can act on toxicological (organs that rid body of toxins) target organs by increasin uptake of drug and decreasing efflux of drug i.e. alcohol
  • drugs can act on target organs by forcing them to not take up necessary endogenous compounds
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19
Q

Why is the blood brain barrier so good at keeping drugs from getting in?

A

because of tight endothelial junctions and P-glycoprotein acting as bouncer

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20
Q

What is a good example of drugs that can act on target organs by forcing them to not take up necessary endogenous compounds?

A

the effects of inhibitors on bile acid.

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21
Q

What are the two secondary active transports?

A

symport and antiport

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22
Q

What are the three processes of passive diffusion?

A

partition
diffusion
repartition

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23
Q

Does facilitated diffusion require energy?

A

No, but it does require a gradient

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24
Q

What kinds of diffusion go down an electrochemical potential gradient?

A

facilitated and passive

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25
Q

What is primary active transport?

What is secondary active transport?

A

using ATP hydrolysis to go against a concentration gradient

Using ATP hydrolysis to create a concentration gradient for another ion to passively diffuse across membrane.

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26
Q

(blank) is important for efficient metabolism because it is an oxidizing agent.

A

cytochrome P450 (CYP)

27
Q

(blank) occur because you want the drug to be soluble and therefore easily eliminated from the body.

A

Oxidation reactions

28
Q

In order to make a drug soluble for excretion, what are the two reactions that need to occur?

A

phase 1: oxygenases

phase 2: transferases

29
Q

What family of genes have about 57 genes and overlapping specificity, can lead to ADR if they are competitively inhibited, polymorphisms and differing expression levels explain individual differences in drug clearance?

A

Cytochrome P450

30
Q

The importance of a CYP450 isoform is not correlated to the concentration of CYP450 isoform in an (blank).

A

organ

31
Q

A poor metabolizer is at risk for (blank), while a ultra-rapid metabolizer isn’t (blank) by drugs.

A

toxicity

affected

32
Q

Where do you find CYP3A?

A

in the GI tract and liver

33
Q 
Most calcium channel blockers 
Most benzodiazepines 
Most HIV protease inhibitors 
Most HMG-CoA-reductase inhibitors 
Cyclosporine 
Most non-sedating antihistamines 
Cisapride
A

What is CYP3A responponsible for metabolism of?

34
Q

CYP3A is inhibited by what?

A

antifungals(-zole) and grapefruit juice (competitively antagonist)

35
Q

What can create all of these problems?
Excessive sedation (benzodiazepines), increased Risk of rhabdomyolyis (statins)
Hypotension
Qt interval prolongation

A

Grapefruit juice because it inhibits cytochrome P450 3A

36
Q

What is the active ingredient in grapefruit juice that binds to cyp3A?

A

Bergamottin

37
Q

What are some common CYP3A inducers?

A

carbamezepine
Rifampin
Rifabutin
St. Johns Wort

38
Q

What is the active ingredient in st. johns wort that inducers CYP3A

A

hyperforin

39
Q

CYP 2D6 main job is to metabolize (blank)

and is inhibited by (blank)

A

Codeine
Many beta-blockers
Many tricyclic antidepressants

Fluoxetine (Prozac)
Haloperidol
Paroxetine (Paxil)
Quinidine

40
Q

What CYP is hyper active in East africans and absent in some caucasians?

A

CYP 2D6

41
Q 
What is this?
Absent in 1% Caucasians and African-Americans 
Primary metabolism of: 
Most NSAIDs (including COX-2) 
S-warfarin (the active form) 
Phenytoin 
Inhibited by: 
Fluconazole
A

CYP 2C9

42
Q

What is CYP2C19 inhibited by, but also metabolizes?

A

omeprazole

43
Q

What CYP is this?
What Absent in 20–30% of Asians, 3–5% Caucasians

Primary metabolism of:
Diazepam
Phenytoin
Omeprazole

Inhibited by:
Omeprazole
Isoniazid
Ketoconazole

A

CYP 2C19

44
Q 
What CYP is this?
Induced by smoking tobacco 
Catalyzes primary metabolism of: 
Theophylline 
Imipramine 
Propranolol 
Clozapine 
Inhibited by: 
Many fluoroquinolone antibiotics 
Fluvoxamine 
Cimetidine
A

CYP 1A2

45
Q

What causes arrhythmia (QT interval elongation) and was removed from the market? Why is it dangerous to couple that drug with ketoconazole, a CYP3A inhibitor.

A

terfenadine

CYP3A get inhibited by ketoconazole so it is unable to metabolize terfenadine which will lead to toxicity

46
Q

What are the four common routs of drug admin and list them fastest to slowest.

A

intravenous
subcutaneous
intramuscular
oral ingestion

47
Q

What measure the result of liberation as well as absorption? What is the equation?

A

bioavailability, F(bioavailability)= Area under curve/dose

48
Q

drug distribution and elimination can be modeled assuming two compartments (blood stream and tissues) and what will the graph look like?

A

It will reach a peak and slowly decline

49
Q

What are the two phases of drug kinetics?

What will the graph look like?

A

distribution and elimination
It will have a steep declining slope and then a less steep declining slope. The derivative will be the continuation of the beginning slope.

50
Q

Different compartments have different (blank) rates

A

clearance

51
Q

The minumim to maximum effective concentration of a drug effect is called the (blank).

A

therapeutic window

52
Q

How do you find the volume of distribution?

A

Vd=dose/ amount in blood

53
Q

Clearance is the exact reverse of what equation?

A

bioavailability

54
Q

What is the equation for clearance?

What is the equation for elimination rate?

A

Cl=dose/AUC

ER= Cl x Cp

55
Q

Since elimination is not saturated for drugs used clinically, (blank) do not change in a given patient.

A

clearance rates

56
Q

Note that (blank) does not indicate how much drug is being removed, but rather the volume of biological fluid such as blood or plasma from which drug would have to be completely removed to account for the clearance per unit of body weight (e.g., mL/min per kg

A

clearance

57
Q

Most drugs are eliminated in a (blank)-order way.

A

first

58
Q

The rate of (blank) is directly proportional to the concentration of the drug in the blood stream.

A

elimination

59
Q

(blank) is an example of a zero order elimination reaction

A

alcohol

60
Q

For a first order reaction, clearance rate will be graphed in what fashion?

A

Linearly

61
Q

On a linear graph how does a first order reaction appear?

A

as a curve

62
Q

On a linear graph how does a zero order reaction appear?

A

a linear line

63
Q

On a log graph, how does a first order reaction appear?

A

A linear line

64
Q

On a log graph, how does a zero order reaction appear?

A

A curve

Block 1 Week 7 (10 decks)

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