Block 9 - Week 3

Question 1

NSAIDS ( Aspirin /ibuprofen /naproxen)

Answer 1

Inhibit COX - COX-1 is constitutionally active and is associated with gastric function. COX-2 is inducible and is associated with inflammation due to the production of prostaglandins (PGs) . This inhibition can be reversible or irreversible dependent on the NSAID

Question 2

Ibuprofen

Answer 2

Reversible inhibitor of the COX enzyme (COX-2 ) which decreases synthesis of PGs involved in mediating inflammation , pain, fever and swelling . The antipyretic effects may be due to action on the hypothalamus. Resulting in increased peripheral blood flow , vasodilation and subsequent heat dissipation

Question 3

Aspirin

Answer 3

Analgesic , antipyretic , anti-inflammatory -

Directly and irreversibly inhibits the activity of both types of COX to decrease formation of precursors of PGs and thromboxanes ( aggregating agent thromboxane A2 in platelets ) from arachidonic acid. platelets cannot produce more COX enzymes and thus the effects of aspirin persist for the life of the exposed platelets (7-10 days )

Question 4

Aciclovir

Answer 4

DNA polymerase inhibitor - antiviral agent activated by viral thymidine kinase . Thymidine kinase converts aciclovir to the aciclovir monophosphate which is then converted to aciclovir diphosphate then triphosphate which competitively inhibits viral DNA polymerase , competes for incorporation into viral DNA and once in acts as a termination signal

Question 5

Amantandine

Answer 5

Viral ion channel disruptor - inhibition of viral protein (M2) which is needed for the viral particle to become uncoated once it is taken inside the cell by endocytosis

Question 6

Diamorphine

Answer 6

Analgesic - opiate receptor agonist

Question 7

Amprenavir

Answer 7

Protease inhibitor - used to treat HIV -1 - inhibits HIV-1 protease which is required for cleavage of viral polyprotein precursors into the functional proteins found in infectious HIV-1 - anti HIV drug

Question 8

Phenoxymethylpencillin

Answer 8

Transpeptidase inhibitor - Pencillin V- treats gram positive organisms I.e strept pneumoniae - narrow spectrum -

Question 9

Zidovudine

Answer 9

Thymidine analogue - nucleoside reverse transcriptase inhibitor (NRTI)