A 45-year-old man with a history of hypertension and resting heart rate consistently above 90 beats per minute is enrolled in a phase 1 clinical trial evaluating a novel antihypertensive agent. At baseline, his blood pressure is 158/96 mmHg and his ECG shows sinus tachycardia. He receives a single dose of the investigational drug, which binds to an allosteric site on a receptor and prevents downstream signaling even when high concentrations of agonist are present. Subsequent dose-response studies demonstrate that the maximal response to the agonist is reduced, but the receptor's affinity for the agonist remains unchanged, and the rightward shift of the dose-response curve cannot be overcome by increasing agonist concentration. Which of the following best describes this investigational drug?
- A)Physiologic antagonist
- B)Full agonist
- C)Partial agonist
- D)Competitive antagonist
- E)Noncompetitive antagonistGABARITO
Explicação
A noncompetitive antagonist decreases efficacy because it cannot be overcome by simply increasing agonist concentration. The maximal response falls, which is the key pharmacodynamic finding in the stem. Ver explicação completa e trilha adaptativa →