:= ltem_7of7
Question Id: 139
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Nitrates, beta blockers, and calcium channel blockers are the mainstay of therapy for patients with chronic stable
angina. Sublingual nitroglycerin is the therapy of choice in acute episodes for immediate relief of angina and for
prevention of angina prior to engaging in strenuous physical activity. Chronic nitrate therapy with long-acting oral
formulations (isosorbide dinitrate or mononitrate) is used to prevent recurrent anginal episodes in patients with
chronic stable angina.
Sublingual nitroglycerin is absorbed rapidly from oral mucosa directly into the venous circulation and has a rapid
onset of action within 2-5 minutes. Long-acting isosorbide dinitrate is absorbed via the gastrointestinal tract and
undergoes extensive first-pass metabolism in the liver prior to release in the systemic circulation . This leads to
low bioavailability and the need for much higher doses of oral formulations as compared to sublingual
nitroglycerin.
(Choice A) Chronic nitrate therapy on a regular basis leads to nitrate tolerance, w ith attenuation of blood pressure
response and anti-anginal effects. Higher doses do not prevent nitrate tolerance. On the contrary, use of
sublingual nitroglycerin on an intermittent, as-needed basis (nitrate-free intervals) prevents the development of
nitrate tolerance.
(Choices C and D) The oral nitrate preparations do not have high serum protein binding or volume of distribution.
(Choice E) lsosorbide dinitrate has rapid and nearly complete intestinal absorption. Its low bioavailability is due to
considerable first-pass hepatic metabolism.
Educational objective:
lsosorbide dinitrate has a low bioavailability due to extensive first-pass hepatic metabolism prior to release in
,:= ltem_7of7
Question Id: 139
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A 71-year-old man with chronic stable angina comes to the office for routine follow-up.
PDF Compressor He has occasional
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episodes of chest pain that improve after taking sublingual nitroglycerin . The patient also has a history of
hypertension and hypercholesterolemia and takes multiple medications for his conditions. Blood pressure is
140/80 mm Hg and pulse is 68/min and regular. Examination reveals normal heart sounds. While discussing a
plan to start isosorbide dinitrate therapy, the patient becomes concerned about the high dose of oral isosorbide
dinitrate compared to sublingual nitroglycerin . Which of the following is the most likely reason for using a high
dose of oral nitrate?
0 A . Drug tolerance prevention (6%>)
✓ (!) B. High first-pass metabolism (77%)
0 C. High serum protein binding (2%)
0 D. High volume of distribution (4%>)
0 E. Low intestinal absorption (8°/o)
Correct I 1,1 77% (i"\ 03 secs 2023
~ Answered correctly \..::,; Time Spent Version
Explanation
Nitrates, beta blockers, and calcium channel blockers are the mainstay of therapy for patients with chronic stable
,:= ltem_7of7
Question Id: 139
■ t7' Mark <:::
Previous
C>
Next
A 71-year-old man with chronic stable angina comes to the office for routine follow-up.
PDF Compressor He has occasional
Free Version
episodes of chest pain that improve after taking sublingual nitroglycerin. The patient also has a history of
hypertension and hypercholesterolemia and takes multiple medications for his conditions. Blood pressure is
140/80 mm Hg and pulse is 68/min and regular. Examination reveals normal heart sounds. While discussing a
plan to start isosorbide dinitrate therapy, the patient becomes concerned about the high dose of oral isosorbide
dinitrate compared to sublingual nitroglycerin . Which of the following is the most likely reason for using a high
dose of oral nitrate?
0 A . Drug tolerance prevention
0 B. High first-pass metabolism
0 C. High serum protein binding
0 D. High volume of distribution
0 E. Low intestinal absorption
Submit
, PDF Compressor Free Version
Type 1 hypersensitivity reaction
Initial exposure Repeat exposure
Early phase
•
Allergen Late phas
(immediate) (hours lat
Antigen
( presenting
cell
Typ
exp
anti Eosinophil • v,~,u..;or
recruitment Eos
exp
to s
~
i l i i 'Histamine
infla Leukotrienes
lgE
whe cross-linking Neutrophil
(Ch B-cell activation & Mast cell
lgE production priming :·
clea
adv ©UWor1d
Question Id: 139
■ t7' Mark <:::
Previous
C>
Next
PDF Compressor Free Version
Nitrates, beta blockers, and calcium channel blockers are the mainstay of therapy for patients with chronic stable
angina. Sublingual nitroglycerin is the therapy of choice in acute episodes for immediate relief of angina and for
prevention of angina prior to engaging in strenuous physical activity. Chronic nitrate therapy with long-acting oral
formulations (isosorbide dinitrate or mononitrate) is used to prevent recurrent anginal episodes in patients with
chronic stable angina.
Sublingual nitroglycerin is absorbed rapidly from oral mucosa directly into the venous circulation and has a rapid
onset of action within 2-5 minutes. Long-acting isosorbide dinitrate is absorbed via the gastrointestinal tract and
undergoes extensive first-pass metabolism in the liver prior to release in the systemic circulation . This leads to
low bioavailability and the need for much higher doses of oral formulations as compared to sublingual
nitroglycerin.
(Choice A) Chronic nitrate therapy on a regular basis leads to nitrate tolerance, w ith attenuation of blood pressure
response and anti-anginal effects. Higher doses do not prevent nitrate tolerance. On the contrary, use of
sublingual nitroglycerin on an intermittent, as-needed basis (nitrate-free intervals) prevents the development of
nitrate tolerance.
(Choices C and D) The oral nitrate preparations do not have high serum protein binding or volume of distribution.
(Choice E) lsosorbide dinitrate has rapid and nearly complete intestinal absorption. Its low bioavailability is due to
considerable first-pass hepatic metabolism.
Educational objective:
lsosorbide dinitrate has a low bioavailability due to extensive first-pass hepatic metabolism prior to release in
,:= ltem_7of7
Question Id: 139
■ t7' Mark <:::
Previous
C>
Next
A 71-year-old man with chronic stable angina comes to the office for routine follow-up.
PDF Compressor He has occasional
Free Version
episodes of chest pain that improve after taking sublingual nitroglycerin . The patient also has a history of
hypertension and hypercholesterolemia and takes multiple medications for his conditions. Blood pressure is
140/80 mm Hg and pulse is 68/min and regular. Examination reveals normal heart sounds. While discussing a
plan to start isosorbide dinitrate therapy, the patient becomes concerned about the high dose of oral isosorbide
dinitrate compared to sublingual nitroglycerin . Which of the following is the most likely reason for using a high
dose of oral nitrate?
0 A . Drug tolerance prevention (6%>)
✓ (!) B. High first-pass metabolism (77%)
0 C. High serum protein binding (2%)
0 D. High volume of distribution (4%>)
0 E. Low intestinal absorption (8°/o)
Correct I 1,1 77% (i"\ 03 secs 2023
~ Answered correctly \..::,; Time Spent Version
Explanation
Nitrates, beta blockers, and calcium channel blockers are the mainstay of therapy for patients with chronic stable
,:= ltem_7of7
Question Id: 139
■ t7' Mark <:::
Previous
C>
Next
A 71-year-old man with chronic stable angina comes to the office for routine follow-up.
PDF Compressor He has occasional
Free Version
episodes of chest pain that improve after taking sublingual nitroglycerin. The patient also has a history of
hypertension and hypercholesterolemia and takes multiple medications for his conditions. Blood pressure is
140/80 mm Hg and pulse is 68/min and regular. Examination reveals normal heart sounds. While discussing a
plan to start isosorbide dinitrate therapy, the patient becomes concerned about the high dose of oral isosorbide
dinitrate compared to sublingual nitroglycerin . Which of the following is the most likely reason for using a high
dose of oral nitrate?
0 A . Drug tolerance prevention
0 B. High first-pass metabolism
0 C. High serum protein binding
0 D. High volume of distribution
0 E. Low intestinal absorption
Submit
, PDF Compressor Free Version
Type 1 hypersensitivity reaction
Initial exposure Repeat exposure
Early phase
•
Allergen Late phas
(immediate) (hours lat
Antigen
( presenting
cell
Typ
exp
anti Eosinophil • v,~,u..;or
recruitment Eos
exp
to s
~
i l i i 'Histamine
infla Leukotrienes
lgE
whe cross-linking Neutrophil
(Ch B-cell activation & Mast cell
lgE production priming :·
clea
adv ©UWor1d
