Importance of Structural Information in Determining Drug Choice in the Same Pharmacological Class (Structurally Based Therapeutic Evaluations)

Question 1

What class of drugs are Plavix, Effient and Brilinta?

Answer 1

Platelet aggregation inhibitors

Question 2

True or false: Clopidogrel, Prasugrel and Ticagrelor are prodrugs and irreversible inhibitors of P2Y purinergic receptors

Answer 2

False. Ticagrelor is not a prodrug and is a reversible inhibitor

Question 3

Which enzyme is a MAJOR metabolizer of Clopidogrel?

Answer 3

CYP2C19

Question 4

Duration of action of 1,4-Dihydropyridine type CCBs is based on rate of ________ __________

Answer 4

Metabolic inactivation

Question 5

Why does amlodipine have the longest duration of action compared to other CCBs?

Answer 5

Less first pass metabolism due to methoxypropyl amine side chain

Question 6

Two advantages of amlodipine due to its methoxypropyl amine

Answer 6

Increased water solubility

Protects 1,4-DHP ring from being oxidized

Question 7

One disadvantage of amlodipine

Answer 7

Decreased BBB permeability

Question 8

What class of drugs are Sitagliptin (Januvia), Linagliptan (Tradjenta), Saxagliptan (Onglyza) and Vildagliptin (Galvus)?

Answer 8

DPP-4 inhibitors

Question 9

Atracurium is a neuromuscular blocking agent mixture of _____ isomers. _____ of the isomers is active

Answer 9

10, 1

Question 10

Atracurium besylate forms the toxic metabolite __________

Answer 10

Laudanosine

Question 11

Which isomer of atracurium has the least CNS side effects and why?

Answer 11

Cisatracurium besylate because it produces the smallest amount of laudanosine, which is responsible for its toxic effects

Question 12

Which -gliptin would be preferred to other -gliptins in a patient with decreased kidney function and why?

Answer 12

Linagliptin because it is eliminated by the liver, not the kidneys