Revision Flashcards
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
High or low protein distribution?
High binding and distribution
What is the half life?
11 hours
Peak plasma levels occur 3 hours after the oral dose
When are steady state conditions reached?
On or before 5 days
Where is it metabolised?
Liver
What are COX2 Inhibitors?
prevent blocking of arachidonic transforming into prostaglandin H2 selectively
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 is the mechanism of action?
- inhibits prostaglandin synthesis and prevents release
- decrease in peripheral tissue, prevents inflammation and pain
What is the drug?
- non- steroidal, anti-inflammatory drug
- analgesic
What is the form and dosage of the drug?
- 50mg, 100mg, 200mg and 400mg
- capsule
What is the molecular weight of the drug?
381.38g
What is the physical appearance of the drug?
white to off white powder
Is the drug hydrophobic or hydrophilic?
hydrophobic
What is the drug’s pKa?
11.1
Sol or insol?
sol
What are the indications?
- 200 mg osteoarthritis
- 200 mg/100mg twice daily rheumatoid arthritis
- 200 mg pain
What are the side effects?
- chest pain
- weight gain
- bloody stools
- less pee or none at all
- nausea
- cough blood
What are symptoms of an overdose?
- lethargy
- vomit
- epigastric pain
- drowsiness
- nausea
What are the contraindications
- asthma
- allergy to NSAIDs or aspirin or sulphonamides
What is COX2?
enzyme receptor
When was the drug discovered?
December 1998
What receptor does the drug target?
- cox2 enzyme
- macrophages, leukocytes and fibroblasts
What is arthritis?
- joint inflammation
- pain, stiffness, swelling
What is the FDA’s opinion on the drug?
- warning recommending limited use
What is its empirical formula?
C17H14F3N3O2S
what is it soluble in?
ethyl acetate
What are its IR peaks?
- amine - 3300-3500
- benzene rings- 1600-2000, 1450-1600
What is the enzyme for the metabolism of the drug?
CYP2C9
has direct impact on polymorphisms
What is the metabolism and pharmacokinetics?
- Celecoxib (methyl hydroxylation) -> hydrocelecoxib
- hydrocelecoxib (oxidised) -> carboxycelecoxib
- cytosolic alcohol dehydrogenases ADH1 and 2 - Conjugated with glucornic acid via UDP with UGTs -> 1-O-glucuronide
