ZCP311 Chem Diuretics Revision June/July Exam PDF

Revision of chemistry of diuretics in preparation for June/July examination 1. Which of the following is NOT a disadvantage of the use of organomercurials as diuretic agents: A. Require parenteral administration B. Tolerance can develop C. Toxicit...

Revision of chemistry of diuretics in preparation for June/July examination 1. Which of the following is NOT a disadvantage of the use of organomercurials as diuretic agents: A. Require parenteral administration B. Tolerance can develop C. Toxicity D. Can result in hyperkalemia 2. Select the structure from A-D below that represents a carbonic anhydrase inhibitor diuretic A. B. C. D. 3. Carbonic anhydrase catalyses the following chemical reaction: A. H2CO3 ⇌ H2O + CO2 B. H2CO3 →H2O + CO2 C. H2O + CO2 → H2CO3 D. H2CO3 ⇌ H+ + HCO3– 4. Which one of the following factors is affected by the acidic nature of the thiazide diuretics? A. The formation of water-soluble salts B. A longer duration of action C. Enhanced membrane permeability D. All of the options supplied are affected by the acidic nature of the thiazide diuretics 5. Which of the following modifications would lead to a decrease in the activity of the thiazide diuretics? A. The addition of an electron donating group to position 6 B. The retention of the double bond between position 3 and 4 C. Increasing the lipophilicity of the molecule D. All of the above will lead to a decreased activity 6. Select the true statement regarding the chemical activity of spironolactone: A. It decreases the reabsorption of Na+ and Cl– ions along with accompanying water B. It prevents the conversion of the receptor to its inactive form C. It enhances the binding of aldosterone to the receptor D. It decreases the reabsorption of K+ ions along with accompanying water 7. Use the thiazide skeleton provided to develop your own theoretical diuretic agent that meets the requirements for increased activity and potency. Select five of the groups or modifications from those provided in the list below and provide an explanation for WHY you selected each group or modification, as well as the POSITION on the skeleton where these must be made. A: Sulfone group B: -CH2Cl C: -CH3 D: Retain double bond E: Remove sulfonamide group F: Saturate double bond G: -CH2CH2CH3 H: -CF3 I: -OH J: Acidic functional group (10 x 0.5 = 5) MEMO 1D 2D 3A 4A 5D 6A 7. G: Position 2 - Reason: Incr DoA due to incr lipophilicity B: Position 6 - Reason: incr lipophilicity F: Between 3&4 - Reason: incr potency A: Position 1 - Reason: enhance acidity