Revision

Question 1

What happens when 200mg is orally administered?

Answer 1

Exhibits dose proportional increase in exposure after oral admin up to 200 mg twice daily
- Less than proportional increase at higher doses

Question 2

High or low protein distribution?

Answer 2

High binding and distribution

Question 3

What is the half life?

Answer 3

11 hours

Peak plasma levels occur 3 hours after the oral dose

Question 4

When are steady state conditions reached?

Answer 4

On or before 5 days

Question 5

Where is it metabolised?

Answer 5

Liver

Question 6

What are COX2 Inhibitors?

Answer 6

prevent blocking of arachidonic transforming into prostaglandin H2 selectively

Question 7

How was the drug discovered?

Answer 7

• cox-2 enzyme identified

- dup-697 was used a building block

Question 8

Who manufactures the drug?

Answer 8

• teva pharmaceutical industry ltd
• activis pln
• myelin

Question 9

What is the mechanism of action?

Answer 9

• inhibits prostaglandin synthesis and prevents release

- decrease in peripheral tissue, prevents inflammation and pain

Question 10

What is the drug?

Answer 10

• non- steroidal, anti-inflammatory drug

- analgesic

Question 11

What is the form and dosage of the drug?

Answer 11

• 50mg, 100mg, 200mg and 400mg

- capsule

Question 12

What is the molecular weight of the drug?

Answer 12

381.38g

Question 13

What is the physical appearance of the drug?

Answer 13

white to off white powder

Question 14

Is the drug hydrophobic or hydrophilic?

Answer 14

hydrophobic

Question 15

What is the drug’s pKa?

Answer 15

11.1

Question 16

Sol or insol?

Answer 16

sol

Question 17

What are the indications?

Answer 17

• 200 mg osteoarthritis
• 200 mg/100mg twice daily rheumatoid arthritis
• 200 mg pain

Question 18

What are the side effects?

Answer 18

• chest pain
• weight gain
• bloody stools
• less pee or none at all
• nausea
• cough blood

Question 19

What are symptoms of an overdose?

Answer 19

• lethargy
• vomit
• epigastric pain
• drowsiness
• nausea

Question 20

What are the contraindications

Answer 20

• asthma

- allergy to NSAIDs or aspirin or sulphonamides

Question 21

What is COX2?

Answer 21

enzyme receptor

Question 22

When was the drug discovered?

Answer 22

December 1998

Question 23

What receptor does the drug target?

Answer 23

• cox2 enzyme

- macrophages, leukocytes and fibroblasts

Question 24

What is arthritis?

Answer 24

• joint inflammation

- pain, stiffness, swelling

Question 25

What is the FDA’s opinion on the drug?

Answer 25

• warning recommending limited use

Question 26

What is its empirical formula?

Answer 26

C17H14F3N3O2S

Question 27

what is it soluble in?

Answer 27

ethyl acetate

Question 28

What are its IR peaks?

Answer 28

• amine - 3300-3500

- benzene rings- 1600-2000, 1450-1600

Question 29

What is the enzyme for the metabolism of the drug?

Answer 29

CYP2C9

has direct impact on polymorphisms

Question 30

What is the metabolism and pharmacokinetics?

Answer 30

1. Celecoxib (methyl hydroxylation) -> hydrocelecoxib
2. hydrocelecoxib (oxidised) -> carboxycelecoxib
   - cytosolic alcohol dehydrogenases ADH1 and 2
3. Conjugated with glucornic acid via UDP with UGTs -> 1-O-glucuronide