++
Chapter 2: Pharmacodynamics
++
++
++
A 55-year-old man is seen in the clinic with hypertension of 150/95 mm Hg (millimeters of mercury). His personal medical history and physical examination are otherwise unremarkable but his family history is positive for early deaths due to cardiovascular disease. A decision is made to treat his hypertension, starting with a calcium channel blocker. Blocker A in a dose of 5 mg produces the same decrease in blood pressure as 500 mg of blocker B. Which of the following predictions is most accurate?
++
++
++
(A) Blocker A will be more efficacious than blocker B
++
++
(B) Blocker A will be about 100 times more potent than blocker B
++
++
(C) Toxicity of blocker A will be less than that of blocker B
++
++
(D) Blocker A will have a wider therapeutic window than blocker B
++
++
(E) Blocker A will have a longer half-life than blocker B
+
++
No information is given regarding the maximal antihypertensive response to either drug. Similarly, no information about half-life or toxicity is provided. The fact that a given response is achieved with a smaller dose of blocker A indicates only that A is more potent than B in the ratio of 500:5. The answer is B.
++
++
++
Graded and quantal dose-response curves are being used for evaluation of a new analgesic drug in the animal laboratory and in clinical trials. Which of the following statements best describes graded dose-response curves?
++
++
++
(A) More precisely quantitated than quantal dose-response curves
++
++
(B) Obtainable from isolated tissue preparations but not from the study of intact subjects
++
++
(C) Used to determine the maximal efficacy of the drug
++
++
(D) Used to determine the therapeutic index of the drug
++
++
(E) Used to determine the variation in sensitivity of subjects to the drug
+
++
Precise quantitation is possible with both types of dose-response curves. Quantal dose-response curves show the frequency of occurrence of a specified response, which may be therapeutically effective (ED) or toxic (TD). Thus, quantal studies are used to determine the therapeutic index and the variation in sensitivity to the drug in the population studied. Graded (not quantal) dose-response curves are used to determine maximal efficacy (maximal response). The answer is C.
++
++
++
Prior to clinical trials in patients with heart failure, an animal study was carried out to compare two new positive inotropic drugs (A and B) to a current standard agent (C). The results of cardiac output ...