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Pharmacology > Pharmacokinetics and Dynamics > Flashcards

Pharmacokinetics and Dynamics Flashcards

1
Q

Where are water soluble drugs excreted

A

Urine

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2
Q

Where are lipid soluble drugs excreted

A

Can cross the lipid membrane so are reabsorbed in the kidney and are changed to water soluble

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3
Q

Which type of drugs will reach the tissue

A

Free drugs–not bound to protein

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4
Q

CO to lungs

A

100%

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5
Q

CO to liver

A

30%

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6
Q

CO to kidney

A

25%

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7
Q

Bioavailability

A

How much drug will reach the blood

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8
Q

First pass metabolism by liver

A

Until all liver enzymes are saturated by the drug, the drug has no effect

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9
Q

What form of drug bypasses the first pass liver effect

A

Sublingual and IV lidocaine

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10
Q

Fastest route of absorption

A

Inhalation

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11
Q

Ionized drug

A

Water soluble–better excretion

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12
Q

Non-ionized drug

A

Lipid soluble–better diffusion

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13
Q

If pH < Pk

A

Lots of H+; acidic medium; drug is protonated; non-ionized; lipid-soluble

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14
Q

If pH > pK

A

Few H+; basic medium; drug is unprotonated; ionized; water soluble

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15
Q

Acidification of urine causes

A

Increased ionization of weak bases and increased excretion

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16
Q

Alkalization of urine causes

A

Increased ionization of weak acids and increased excretion

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17
Q

How to make urine more acidic

A

Cranberry juice, vitamin C, NH4Cl

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18
Q

How to make urine more alkaline

A

Aspirin

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19
Q

IV administration does not involve

A

Absorption

100% bioavailability

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20
Q

2 phases of elimination

A

Rapid decrease in blood concentration due to tissue distribution
Slower decrease in blood concentration due to metabolism and excretion

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21
Q

MEC

A

Minimum effective concentration

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22
Q

MTC

A

Minimum toxic concentration

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23
Q

To be bioequivalent…

A

2 drugs need to have some bioavailability and rate of absorption

24
Q

Competition between drugs for plasma protein binding sites may

A

Increase free fraction of drug and might increase the effects of the displaced drug

25
Q

Sulfonamides and bilirubin competition

A

Sulfonamides can displace bilirubin from albumin and cause kernicterus in neonates so sulfonamides are contraindicated in newborns

26
Q

What can cross placental barrier and BBB

A

Small, lipid soluble drugs

In pregnancy: water soluble alternatives are safer and drugs with highest plasma protein binding

27
Q

High volume of distribution

A

Indicates large tissue distribution due to low plasma protein binding

28
Q

Low volume of distribution

A

indicates drug primarily found in the blood due to high plasma protein binding

29
Q

Drug metabolism

A

Conversion of drug to more water soluble to be more easily excreted

30
Q

Phases of drug metabolism

A

Phase 1: modify drug by oxidation, reduction, hydrolytic reactions
Phase 2: conjugation of drug molecule with transferase

31
Q

Codeine is prodrug for

A

Morphine

If someone is an ultra-rapid metabolizer they could die

32
Q

Examples of general inducers

A

Anti-seizure drugs, Rifampin, HIV drugs, chronic alcohol, glucocorticoids
Increase gene expression of CYP enzymes resulting in increased metabolism of other drugs

33
Q

Examples of general inhibitors of metabolism

A

Proton pump inhibitors, azoles and macrolides, grapefruit juice, SSRI’s, acute alcohol
Causes decreased metabolism of other drugs and potential toxicity

34
Q

Zero-order elimination

A

Large amount of drugs–toxic level
Saturation kinetics
Body has to eliminate drug at a constant rate regardless of half life
Ex. alcohol, phenytoin, salicylates

35
Q

First order elimination

A

Constant fraction is eliminated per unit time
Half life is constant
Most drugs follow this

36
Q

Clearance

A

How much blood is completely cleared of drug per unit time

If drug is renally cleared, only the free fraction is filtered by glomerulus

37
Q

Clinical steady state is reached at

A

4-5 half lives

38
Q

Steady state

A

Rate in= Rate out

39
Q

Agonist

A

Has an effect

40
Q

Antagonist

A

Has no effect

41
Q

Inverse agonist

A

Has opposite effect

42
Q

Efficacy

A

Maximal effect a drug can achieve, irrespective of dose

43
Q

Higher potency=

A

Less amount of drug needed to reach 100% efficacy

44
Q

Physiologic antagonism

A

2 agonists with opposing action antagonize each other

45
Q

Chemical antagonism

A

2 chemicals bind to each other and cancel each other (antedotes)

46
Q

ED
TD
LD

A

Effective dose
Toxic dose
Lethal dose

47
Q

Therapeutic index

A

TD/ED

48
Q

Phase 1 of FDA oversight

A

Is drug safe for patients?
Involves healthy volunteers usually young males
Works out toxicity and pharmacokinetics of drug

49
Q

Phase 2 of FDA oversight

A

Does the drug work?
Involves patients
Compare to placebo or positive control
Randomized, double-blind

50
Q

Phase 3 of FDA oversight

A

how well does drug work and what are common side effects?

Larger group of patients

51
Q

Phase 4 of FDA oversight

A

Post marketing surveillance

52
Q

Schedule 1 Controlled substances

A

High abuse liability
Low or no medical utility
Heroin, marijuana, LSD, PCP

53
Q

Schedule 2 Controlled substances

A

high potential for abuse
Can be prescribed under restricted conditions
Triplicate prescription and no automatic refills
Ex. Opiates, Amphetamines

54
Q

Schedule 3 Controlled substances

A

Lower risk

Anabolic steroids

55
Q

Schedule 4 controlled substances

A

low potential for abuse

Benzodiazepines

56
Q

Schedule 5 controlled substances

A

Lowest abuse potential

Cough medication with codeine

Pharmacology (56 decks)

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