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Question 1

What is the metabolism and pharmacokinetics?

Answer 1

1. celecoxib (methyl hydroxylation) -> hydrocelecoxib
2. Hydrocelecoxib (Oxidised) -> carboxycelecoxib
   cytosolic alcohol dehydrogenase adh1 + 2
3. conjugated with glucornic acid via UDP with UGT ->1-O-glucuronide

Question 2

What is the enzyme used for the metabolism of the drug?

Answer 2

• CYP2C9

-

Question 3

What is the drug?

Answer 3

analgesic
anti-inflammatory
non steroidal

Question 4

What is the form and dosage of the drug?

Answer 4

• 50mg, 100mg, 200mg and 400mg

- capsule

Question 5

What is the physical appearance of the drug?

Answer 5

white to off white powder

Question 6

Hydrophillic or hydrophobic

Answer 6

hydrophobic

Question 7

What is the drug’s Pka?

Answer 7

11.1

Question 8

SOL OR INSOL

Answer 8

sol

Question 9

What are the indications?

Answer 9

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

Question 10

What are the side effects?

Answer 10

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

Question 11

What is COX2?

Answer 11

enzyme receptor

Question 12

When are steady state conditions reached?

Answer 12

5 days

Question 13

What are symptoms of overdose?

Answer 13

• lethargy
• vomit
• epigastric pain
• drowsiness
• nausea

Question 14

Where is it metabolised?

Answer 14

Liver

Question 15

What happens when 200mg is orally administered?

Answer 15

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

Question 16

when was the drug discovered?

Answer 16

1998

Question 17

What receptor does the drug target?

Answer 17

• cox2 enzyme

- macrophages, leukocytes and fibroblasts

Question 18

What is the FDA’s opinion on the drug?

Answer 18

• warning recommending limited use

Question 19

What is the half life?

Answer 19

11 hours

Peak plasma levels occur 3 hours after the oral dose

Question 20

what is it soluble in?

Answer 20

ethyl acetate

Question 21

What is the molecular weight of the drug?

Answer 21

381.38g

Question 22

What is the empirical formula?

Answer 22

C17H14N3F3O2S

Question 23

What are the contraindications

Answer 23

• asthma

- allergy to NSAIDs or aspirin or sulphonamides

Question 24

What is arthritis?

Answer 24

• joint inflammation

- pain, stiffness, swelling

Question 25

High or low protein distribution?

Answer 25

High binding and distribution

Question 26

What are COX2 Inhibitors?

Answer 26

prevent arachidonic transforming into prostaglandin H2 selectively

Question 27

What are its IR peaks?

Answer 27

amine 3000-3500

benzene rings 1600-2000, 1450-1600

Question 28

What is the mechanism of action?

Answer 28

• inhibits prostaglandin synthesis and prevents release

- decrease in peripheral tissue, prevents inflammation and pain

Question 29

How was the drug discovered?

Answer 29

• cox-2 enzyme identified

- dup-697 was used a building block

Question 30

Who manufactures the drug?

Answer 30

• teva pharmaceutical industry ltd
• activis pln
• myelin

Question 31

What temperature should it be kept at?

Answer 31

room temperature

Question 32

What is its boiling point?

Answer 32

158

Question 33

Why is it not a substitute for aspirin?

Answer 33

no platelet effect

Question 34

What does COX2 inhibition result in?

Answer 34

apoptosis and a reduction in tumor angiogenesis and metastasis.

Question 35

Give one toxicity

Answer 35

decrease the natriuretic effects of diuretics
inhibiting renal prostaglandin synthesis
risk of renal failure is increased