New Flashcards
What is the metabolism and pharmacokinetics?
- celecoxib (methyl hydroxylation) -> hydrocelecoxib
- Hydrocelecoxib (Oxidised) -> carboxycelecoxib
cytosolic alcohol dehydrogenase adh1 + 2 - conjugated with glucornic acid via UDP with UGT ->1-O-glucuronide
What is the enzyme used for the metabolism of the drug?
- CYP2C9
-
What is the drug?
analgesic
anti-inflammatory
non steroidal
What is the form and dosage of the drug?
- 50mg, 100mg, 200mg and 400mg
- capsule
What is the physical appearance of the drug?
white to off white powder
Hydrophillic or hydrophobic
hydrophobic
What is the drug’s Pka?
11.1
SOL OR INSOL
sol
What are the indications?
200 mg pain, osteoarthritis, 100mg/200mg twice daily rheumatoid arthritis
What are the side effects?
- chest pain
- weight gain
- bloody stools
- less pee or none at all
- nausea
- cough blood
What is COX2?
enzyme receptor
When are steady state conditions reached?
5 days
What are symptoms of overdose?
- lethargy
- vomit
- epigastric pain
- drowsiness
- nausea
Where is it metabolised?
Liver
What happens when 200mg is orally administered?
Exhibits dose proportional increase in exposure after oral admin up to 200 mg twice daily
- Less than proportional increase at higher doses
when was the drug discovered?
1998
What receptor does the drug target?
- cox2 enzyme
- macrophages, leukocytes and fibroblasts
What is the FDA’s opinion on the drug?
- warning recommending limited use
What is the half life?
11 hours
Peak plasma levels occur 3 hours after the oral dose
what is it soluble in?
ethyl acetate
What is the molecular weight of the drug?
381.38g
What is the empirical formula?
C17H14N3F3O2S
What are the contraindications
- asthma
- allergy to NSAIDs or aspirin or sulphonamides
What is arthritis?
- joint inflammation
- pain, stiffness, swelling
High or low protein distribution?
High binding and distribution
What are COX2 Inhibitors?
prevent arachidonic transforming into prostaglandin H2 selectively
What are its IR peaks?
amine 3000-3500
benzene rings 1600-2000, 1450-1600
What is the mechanism of action?
- inhibits prostaglandin synthesis and prevents release
- decrease in peripheral tissue, prevents inflammation and pain
How was the drug discovered?
- cox-2 enzyme identified
- dup-697 was used a building block
Who manufactures the drug?
- teva pharmaceutical industry ltd
- activis pln
- myelin
What temperature should it be kept at?
room temperature
What is its boiling point?
158
Why is it not a substitute for aspirin?
no platelet effect
What does COX2 inhibition result in?
apoptosis and a reduction in tumor angiogenesis and metastasis.
Give one toxicity
decrease the natriuretic effects of diuretics
inhibiting renal prostaglandin synthesis
risk of renal failure is increased
