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Pharmacology - UT Housotn SON Gard School > Exam 1 - Lecture 3 & CNS Drugs > Flashcards

Exam 1 - Lecture 3 & CNS Drugs Flashcards

1
Q

Define FDA Pregnancy Category:

No fetal harm in studies in women

A

A

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2
Q

What drug characteristics make them easier to cross into breast milk?

A
  • Smaller molecular weight
  • Lipid soluble drugs
  • Breast milk more acidic - so accumulates more basic drugs (beta blockers)
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3
Q

What drug metabolism phenotype describes pt who metabolizes prodrugs slowly?

A

Poor/Intermediate Metabolizing Phenotype

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4
Q

FDA Pregnancy Categories for Teratogenic Risk

B

A

No fetal harm in animals; no studies in women

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5
Q

Compared to males, is plasma volume levels higher or lower in females?

A

Plasma volumes are LOWER in females.

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6
Q

Physiologic changes with geriatric pts. affecting drug processing:

A
  • Decreased 1st pass elimination (increased amount of drug entering systemic circulation)
  • Decreased serum albumin (increased concentraiton of unbound drug - more intense effect)
  • Creatinine clearance occurs
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7
Q

Define FDA Pregnancy Category:

Fetal harm in studies in women; Weigh risk vs. benefit

A

D

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8
Q

Pharmacokinetic Differences by Race

American Indian / Alaska Native

A

•Little pharmacokinetic research has been done

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9
Q

What effects on prodrug to poor/intermediate metabolizer phenotypes have?

A
  • Prodrug: metabolized slowly into active drug
  • Prodrug: may lead to prodrug accumulation
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10
Q

Pharmacokinetics not affected by race:

A

•absorption*, (AAs may have difference)

glomerular filtration, &

passive tubular reabsorption

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11
Q

How do pts. w/ ultrarapid metabolizing phenotype metabolize prodrugs?

A
  • Prodrug is rapidly metabolized to active drug
  • No dosage adjustment is needed
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12
Q

Define FDA Pregnancy Category:

Definite fetal harm in studies in women. Contraindicated

A

X

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13
Q

Pharmacokinetic Differences by Race

African American

A
  • Hypertension: Not all AA are salt sensitive
  • Have less renin-dependent HTN- ACEI not 1st line
  • Afr Ams- more sensitive to bradykinin → at risk for ACEI- associated angioedema
  • Higher gastric bicarb secretion-, raises gastric pH → negatively affects absorption of some drugs
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14
Q

How does estrogen affect distribution?

A
  • Estrogen is distributed attached to a serum-binding globulin.
  • Exogenous estrogens INCREASE levels of many serum-binding globulins
  • These serum binding agents will bind to drugs, resulting in less free drug
  • Examples - corticosteroid-binding / thyroxine-binding globulins = less free drug
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15
Q

How do pts. w/ ultrarapid metabolizing phenotype metabolize active drugs?

A
  • They rapidly metabolize active drug to the inactive form.
  • B/c of this - they may have therpetherapeuticre
  • They will require HIGHER doses of active drug
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16
Q

Define FDA Pregnancy Category:

No fetal harm in animals; no studies in women

A

B

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17
Q

Pharmacokinetic Differences by Race

Asian Americans

A
  • East Asians- “Fast acetylators”: faster hepatic metabolism of certain drugs à may require more frequent and higher doses
  • May metabolize antidepressants slower (unless they are a ultra-rapid 2D6 metabolizers- 21%) à may require lower doses
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18
Q

Typcially, pts. who are have poor/intermediate drug metabolizing phenotype require higher or lower doses of medications?

A

LOWER DOSES for poor metabolizers

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19
Q

Pharmacogenetic abnormalities can lead to:

A
  • Unexpected drug toxicity even when low doses of drugs are administered.
  • Unexpected drug-drug interactions.
  • Novel drug effects not seen in the “average” patient.
  • Failure to respond to “therapeutic” doses.

Example:

Individuals who do not produce enough CYP2D6 in the liver to metabolize codeine to morphine and thus may not experience normal pain relief with this drug

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20
Q

Changes in older adult

A

Changes in older adults

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21
Q

What effect on drug metabolism will ultrarapid metabolizers have?

A

FAST METABOLISM

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22
Q

Know this chart!

A

Know this chart!

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23
Q

Because plasma levels are lower in females, how will drug concentration be affected, especially in drugs with high volumes of distribution?

A

Drugs with high volume distributions will be MORE CONCENTRATED in plasma of females.

24
Q

What effects can having lower plasma volumes have on drug levels?

A

Drug levels will be more concentrated.

25
Q

If pregnant, what fetal exam is needed for the patient on paroxetine (paxil)?

A

Echocardiogram of fetus

26
Q

Know this:

Metabolism of drugs differences by sex may depend on the differences in the CYP450 enzymes

A

Know this:

Metabolism of drugs differences by sex may depend on the differences in the CYP450 enzymes

27
Q

When prescribing medications, consider all women of reproductive age pregnant unless:

A
  • You have tested them for pregnancy,
  • they give you a history of using a reliable contraceptive method,
  • t​hey are reliable enough to make use of their contraceptive method in a consistent manner.
28
Q

What effect on drug metabolism will poor/intermediate metabolizers have?

A

SLOW METABOLISM

29
Q

What should you be concerned with children and topical medications?

A
  • Children absorb topical medications more readily than adults due to larger body surface area (can lead to toxicity!)
  • There is great concern for the absorption of topical corticosteroids due to HPA axis suppression
  • Look up appropriate topical corticosteroids before prescribing to children
30
Q

FDA Pregnancy Categories for Teratogenic Risk

A

A

No fetal harm in studies in women

31
Q

What effect can having higher levels of free drug in the plasma have on the patient?

A

Higher risk for adverse effects.

32
Q

What effects on active drugs to poor/intermediate metabolizer phenotypes have?

A
  • Metabolizes slowly into active form
  • Potential for accumulation
  • Pts require lower dosages of medications
33
Q

If pregnant, what fetal exam is needed for the patient on SSRI?

A

Detailed fetal anatomy during 2nd trimester.

34
Q

Although drugs can affect fetal formation at all stages, when is the fetus most susceptible to damage?

A

1st trimester

35
Q

In patients with higher body fats proportions, like in female patients - how are absorption and distribution affected with lipophilic drugs?

A

Lipophilic drugs are more readily absorbed.

They have a greater volume of distribution.

36
Q

What are physiologic factors affecting drug prescription?

A

Pregnancy

Children

Infant

Geri

Our bodies change over time - affecting the pharmacokinetics of drugs.

37
Q

FDA Pregnancy Categories for Teratogenic Risk

C

A

Fetal harm in animals; no studies in women

38
Q

Review this chart

A

Review this chart

39
Q

For pts. with ultrarapid metabolizing phenotype, which drug type would need to be adjusted to higher doses: prodrug or active drug?

A

Active Drug (because they metabolize it quickly)

(No dosage change needed for pro-drug)

40
Q

How do pts. w/ poor/intermediate metabolizing phenotype metabolize active drugs?

A

Slowly, leading to potential accumulation

41
Q

FDA Pregnancy Categories for Teratogenic Risk

X

A

Definite fetal harm in studies in women. Contraindicated

42
Q

FDA Pregnancy Categories for Teratogenic Risk

D

A

Fetal harm in studies in women; Weigh risk vs. benefit

43
Q

Define FDA Pregnancy Category:

Fetal harm in animals; no studies in women

A

C

44
Q

What physiological changes during pregnancy directly affect pharmacokinetics?

A
  • Increased CYP450
  • Increased volume of distribution
45
Q

How does estrogen affect drug absorption?

A

Estrogen affects female gastric emptying by making it slower.

Drugs absorbed in the stomach will have longer exposure to absorption sites.

46
Q

Gender differences with pharmacokinetics

A

BMI - has an effect of distribution and excretion of drugs.

Females have higher body fat

47
Q

Which gender has a higher proportion of body fat - males or females?

A

Females have a higher proportion of body fat.

48
Q

Do children metabolize drugs faster or slower than adults?

A

FASTER

49
Q

Why is drug therapy for pregnant women especially difficult? because of the real likelihood of altered drug kinetics and dynamics, the possibility of drug-induced fetal toxicity, and the likelihood that for many drugs, precise estimates of fetal risk are not available.

A
  • Because of the real likelihood of altered drug kinetics and dynamics,
  • The possibility of drug-induced fetal toxicity, and
  • The likelihood that for many drugs, precise estimates of fetal risk are not available.
50
Q

Which gender has lower body weight and BMI - males or females?

A

Females have lower body weights and BMI.

51
Q

What is kernicterus and what drug causes it?

A

(permanent brain damage from severe jaundice) with sulfonamide medications.

52
Q

Are race related pharmacokinetics universal to all members of that race?

A

NO

53
Q

If drug concentration is high in maternal plasma, what is the concentration in breast milk?

A

Higher in breast milk with higher maternal plasma concentration.

54
Q

In women, what issues can happen with tricyclic antidepressants?

A
  • Take longer to achieve steady state
  • Women may experience side effects of drug because after drug saturates fat tissue
  • More free drug is available in the plasma
55
Q

chloramphenicol resulted in which neo-nate condition?

A

Gray baby syndrome (life-threatening characterized by body limpness and ashen gray color, cardiovascular collapse, cyanosis, hypotension, hypothermia, vomiting)

56
Q

What effects on prodrug accumulation will poor/intermediate metabolizer phenotypes have?

A

Accumulation of pro-drug

57
Q

At what age do most children metabolize drugs similar to adults?

A

1 year

Pharmacology - UT Housotn SON Gard School (3 decks)

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