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Pharmacology > Pregnancy & Geriatrics > Flashcards

Pregnancy & Geriatrics Flashcards

1
Q

The ______________ is an organ of exchange between the mother and fetus (food, waste, drugs, etc.)

A

Placenta

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2
Q

How do most drugs move from maternal to fetal circulation?

A

By diffusion

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3
Q

What are the main factors affecting the rate of drug transfer across the placenta?

A
  1. Lipid solubility
  2. Molecular weight
  3. Degree of protein binding
  4. pH
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4
Q

What type of drugs cross the placenta more easily based on lipid solubility?

A

Drugs with HIGH lipid solubility

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5
Q

What type of drugs cross the placenta more easily based on molecular weight?

A

Drugs with LOW molecular weight

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6
Q

What type of drugs cross the placenta more easily based on protein binding?

A

Drugs with LOW plasma protein binding

(Read pic if you want to understand why)

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7
Q

What type of drugs cross the placenta more easily based on pH?

A

Weak basic drugs OR drugs with low ionized fraction

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8
Q

True or false

Drugs with molecular weight less than 500 Da readily cross the placenta.

A

True

Low molecular weight drugs (< 500 Da) readily cross the placenta&raquo_space;> larger molecules ( 600-1,000 Da) move more slowly

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9
Q

How do drugs with a molecular weight between 600 and 1,000 Da move across the placenta?

A

They move more slowly compared to smaller molecules.

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10
Q

What happens to drugs with molecular weight over 1,000 Da?

For example: Insulin and Heparin

A

They do NOT cross the placenta in significant amounts

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11
Q

How do changes in maternal and fetal albumin levels during pregnancy affect drug transfer across the placenta?

A

↓ Maternal albumin levels → more free drug available to cross

↑ Fetal albumin levels → more drug binds and accumulates in fetus

= Higher protein-bound drug levels in the fetus

(Read pic if you want to understand)

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12
Q

How does the difference in maternal and fetal pH affect drug transfer across the placenta?

A

Fetal pH is more acidic than maternal ph → weak basic drugs cross more easily

Once inside, drugs become ionized → less likely to diffuse back to maternal circulation

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13
Q

True or false

Water-soluble drugs cross the placenta more easily than lipophilic drugs.

A

False

Lipophilic drugs cross more easily

NOTE: in the slide they added “ (e.g opiates and antibiotics) “
Read the picture to generally understand why.

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14
Q

True or False:

All drugs are teratogens.

A

False

(Note: teratogen is any substance that can cause birth defects or harm a developing fetus during pregnancy)

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15
Q

True or False:

The teratogenicity of different drugs varies.

A

True

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16
Q

True or False:

Every exposure to a teratogen leads to malformations.

A

False

Exposure to a teratogen does not always = malformations

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17
Q

What are some factors that affect teratogenicity?

A
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18
Q

What are the three stages of development during which the fetus can be affected by drugs?

A
  1. Implantation stage
    (17 days after fertilization)
  2. Organogenesis
    (18–55 days after fertilization)
  3. Growth and Development stage
    (56 days to birth, second and third trimesters)
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19
Q

When does the implantation stage occur?

A

17 days after fertilization

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20
Q

When does organogenesis take place?

A

18–55 days after fertilization

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21
Q

What is the time frame for the growth and development stage?

A

From 56 days to birth (includes second and third trimesters)

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22
Q

What is the effect of drugs during the implantation stage (up to 17 days after fertilization)?

A

“All or Nothing” effect — either no effect or pregnancy failure

(e.g. methotrexate)

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23
Q

Which drug example can lead to pregnancy failure during implantation?

A

Methotrexate (anticancer drug)

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24
Q

What is the most sensitive developmental stage for drug-induced teratogenicity?

A

Organogenesis - First trimester
(18–55 days after fertilization)

Is the most sensitive stage to the harmful effects of drugs (teratogenesis most likely)

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25
What may result from drug exposure during organogenesis? Include examples
Fetal malformations (e.g. cleft palate, short limbs)
26
What teratogenic effect is associated with warfarin?
Nasal hypoplasia
27
What teratogenic effect is associated with phenytoin?
Cleft palate/cleft lip
28
What teratogenic effect is associated with valproic acid?
Neural tube defects
29
What is the effect of drugs during the growth and development stage (2nd and 3rd trimester -- 56 days to birth)?
Teratogenesis is unlikely, but drugs may alter the growth and function of already formed fetal organs and tissues.
30
Which drugs, when used during the growth and development stage of pregnancy, may cross the placenta and affect fetal organ function?
Antithyroid drugs ACE inhibitors.
31
What fetal effect can antithyroid drugs cause during the growth and development stage?
Neonatal hypothyroidism
32
What fetal complication is linked to ACE inhibitors during the 2nd and 3rd trimester?
Serious damage to fetal renal function
33
What are some drugs that are given at the end of pregnancy and could cause harmful effects ?
Aspirin Opiates and benzodiazepines.
34
What can large doses of aspirin cause if given at the end of pregnancy?
Premature closure of ductus arteriosus
35
What are the effects of opiates or benzodiazepines in the baby given before or during delivery?
Respiratory depression Hypotension Hypothermia
36
What three pharmacokinetic processes are affected by pregnancy? ( effect of pregnancy on drugs )
Absorption, Distribution and Elimination.
37
True or false During pregnancy, physiological changes can influence drug pharmacokinetics, including absorption, distribution, and elimination.
True
38
What physiological changes during pregnancy can influence drug pharmacokinetics?
• Maternal plasma albumin concentration is reduced, influencing drug protein binding → increased free fraction of drug. • Cardiac output is increased → increased renal blood flow & glomular filtration rate & increased renal elimination of drugs. • Plasma volume and extracellular fluid increase → altering drug disposition
39
How does reduced maternal plasma albumin concentration affect drug protein binding?
It increases the free fraction of the drug in circulation.
40
How does increased cardiac output during pregnancy affect drug elimination?
It increases renal blood flow and glomerular filtration rate, leading to increased renal elimination of drugs.
41
What is the effect of increased plasma volume and extracellular fluid during pregnancy on drugs?
It alters drug disposition in the body.
42
What are examples of drugs considered safe in pregnancy for common conditions? (Diabetes, Blood clots, Infections, Hypertension, Hyperthyroidism, Pain)
• Diabetes: Insulin • Blood clots: Heparin • Infections: Penicillins, Cephalosporins • Hypertension: Methyldopa • Hyperthyroidism: Propylthiouracil • Pain: Acetaminophen
43
What factors influence the transfer of drugs into breast milk?
• Lipid solubility • Molecular weight (MW) • pH/Ionization • Blood flow (Same factors that control drug distribution)
44
True or False: The factors that influence drug transfer into breast milk are the same as those that control drug distribution in the body.
True
45
True or False: Only small amounts of drugs pass into the milk compartment
True
46
What are some examples of drugs that should be AVOIDED during breastfeeding?
• Narcotic analgesics • Benzodiazepines • Antithyroid drugs • Sulfonylureas • Aspirin (Hint: BAANS) - remember "avoid" = "ban" = "BAANS"
47
What are some examples of drugs considered SAFER for use during breastfeeding?
• Penicillins, Cephalosporins • Theophylline, Salbutamol by inhaler • Carbamazepine • Beta blockers, Methyldopa • Warfarin, Heparin • Tricyclic antidepressants
48
What are key physiological changes in the elderly that affect drug response?
↓ Decreased: - total body water - lean body mass - serum albumin - brain weight & volume ↑ Increased: - body fat - sensitivity to depressant drugs - CNS effects and side effects Numerous other changes
49
True or False: Homeostatic response is reduced in the elderly.
True
50
True or False: Cardiovascular reflexes are impaired in the elderly.
True
51
What is a consequence of impaired cardiovascular reflexes in elderly patients taking antihypertensives?
Orthostatic hypotension is more frequent.
52
What medications are associated with impaired cardiovascular reflexes in the elderly, such as increased risk of orthostatic hypotension?
Antihypertensives and β-blockers ما عجبني السؤال بس ما عرفت اصيغه ، المهم الصوره من السلايدات
53
True or False Postural control and stability are impaired in the elderly.
True
54
What consequence can result from impaired thermoregulation in elderly individuals, especially when using CNS depressants?
Hypothermia
55
What renal changes occur with advanced aging that contribute to reduced glomerular filtration rate (GFR)?
Decreased: • kidney size • renal blood flow • number of functional nephrons • tubular secretion All of which ↓ GFR
56
How does advanced aging affect drug excretion by the kidneys?
↓GFR = reduces renal drug clearance and excretion.
57
The excretion of which drugs is affected by decreased GFR in the elderly?
• Atenolol • Gabapentin • H2 blockers • Digoxin • Allopurinol • Quinolones (Hint: Q-GHADA)
58
True or False: There are major age-related issues with drug absorption in the elderly.
False
59
What age-related physiological changes may affect drug absorption in the elderly?
• ↑ Higher gastric pH = ↓ absorption of some drugs • Slowed motility and delayed gastric emptying • Intestinal blood flow is reduced by 50% • Absorptive surface reduced
60
How does aging-related change in body composition affect the distribution of certain drugs? Provide an example
Increased volume of distribution (Vd) for lipid-soluble drugs due to: • Decreased lean body mass • Decreased total body water (by 10–15%) • Increased total body fat (by 15–30%) Example : Diazepam has an increased half-life (t½)
61
How does aging affect plasma protein binding and dosing of weak acidic drugs in the elderly?
1. ↑ α₁-acid glycoprotein: slightly increased in the elderly 2. ↓ Serum albumin: decreased This leads to: • Decreased binding of weak acidic drugs • Increased free (active) drug in plasma • Therefore, loading doses of highly bound acidic drugs (e.g. warfarin) should be reduced
62
True or False: In elderly patients, the loading dose of highly protein-bound acidic drugs like WARFARIN should be reduced due to decreased serum albumin levels.
True Lower serum albumin leads to less binding of acidic drugs like warfarin, increasing the free (active) drug fraction in plasma, which can enhance drug effects and toxicity.
63
Recap question: What age-related changes affect drug distribution in the elderly, and how do they impact drug levels in the body?
Body composition changes: • ↓ Lean body mass • ↓ Total body water • ↑ Total body fat = ↑ Volume of distribution (Vd) for fat-soluble drugs (e.g. diazepam) Plasma protein binding changes: • ↓ Serum albumin → ↓ binding of weak acidic drugs → ↑ free (active) drug levels • ↑ α₁-acid glycoprotein → may ↑ binding of basic drugs Overall effect: Altered drug distribution and potentially increased sensitivity/toxicity due to more free drug in plasma.
64
True or False Liver size and hepatic blood flow are reduced in the elderly, impairing first-pass metabolism.
True (Read pic to understand first pass metabolism)
65
What are the consequences of impaired first-pass metabolism in the elderly?
• Reduced clearance of highly extracted drugs • Increased bioavailability of drugs that undergo extensive first-pass metabolism
66
What age-related hepatic change can reduce the hepatic clearance of drugs in the elderly
A decrease in hepatic microsomal enzyme activity.
67
Is there a consistent change in the liver’s ability to metabolize all drugs in the elderly?
No
68
In the elderly, which metabolic reactions are affected more: Phase I or Phase II?
Phase I reactions are more affected than Phase II reactions.
69
Which enzymatic system shows the greatest change in Phase I reactions in the elderly?
mixed function oxidase system.
70
What happens to hepatic clearance of diazepam in the elderly, and what is the pharmacokinetic result?
Hepatic clearance of diazepam is reduced, leading to an increased half-life (t½).
71
How does an increased volume of distribution affect the half-life of drugs like diazepam in the elderly?
Increased volume of distribution leads to an increased half-life (t½).
72
What other conditions in the elderly can influence drug metabolism besides liver function changes?
Congestive heart failure and nutritional deficiencies.
73
True or False: Renal function remains stable with age.
False Renal function declines with age, although the rate of decline can vary.
74
Which two renal processes are reduced in the elderly, affecting drug excretion?
↓ Glomerular filtration rate (GFR) ↓ Active tubular secretion.
75
By how much can GFR decline in the elderly ?
GFR may fall by 50%, (For ex: reaching around 60–70 mL/min at age 80)
76
What happens to renal blood flow in the elderly?
It is reduced
77
What are the consequences of reduced glomerular filtration rate (GFR) and renal blood flow in the elderly on drug elimination?
They lead to ↓ renal clearance, causing drug accumulation (NOTE : increasing risk of toxicity, particularly for drugs primarily eliminated by the kidneys)
78
What is a major cause of drug accumulation in the elderly?
Reduced renal elimination. ( ↓ GFR and ↓ Renal blood flow )
79
What happens to clearance and half-life of drugs that are highly excreted by the kidneys in the elderly?
Clearance decreases, and the half-life (t½) increases.
80
Name two drugs that are significantly affected by reduced renal clearance in the elderly.
Aminoglycosides Digoxin.
81
Why is dosage adjustment often necessary in elderly patients, especially in drugs with a low therapeutic index ?
Because reduced clearance can lead to toxicity
82
What parameter is used to guide dosage adjustment in the elderly?
Creatinine clearance
83
What happens to specific receptors and target sites with aging?
They undergo age-related changes, with some becoming more sensitive and others less sensitive.
84
Which drug types show increased sensitivity in the elderly, and how is the response to narcotics affected?
Increased sensitivity to: • CNS drugs like diazepam • Anti-cholinergic agents For narcotics: • Increased level of pain relief • Prolonged duration of pain relief
85
What is the effect of aging on β₁ receptor affinity?
There is reduced affinity to β₁ agonists and β blockers due to decreased β-receptor response. (Reduced sensitivity)

Pharmacology (9 decks)

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