Dr Sharon Rees @reesprescribe
Day 1: The discovery of the COX-2 channel in the early 1990s led to two new NSAIDs designed and licensed with COX-2 selective action. The new drug target implied therapeutic and adverse drug effect (ADE) superiority, but only #celecoxib endured, as rofecoxib (Vioxx) was found to have the highest cardiovascular risks.
Dr Sharon Rees @reesprescribe
Day 2: #celecoxib is licensed in adults for pain and inflammation in OA, RA and ankylosing spondylitis. Oral (capsule) use only; adult dose range is 200-400 mg in daily divided doses for the shortest duration possible. Not indicated for use in children and contraindicated in pregnancy.
Dr Sharon Rees @reesprescribe
Day 3: #celecoxib has good oral absorption taken with/without food (no advisory label). Major hepatic metabolism by CYP2C9 leads to inactive metabolites and elimination. Hepatic impairment, elderly and poor metabolisers incur increased drug levels, therefore use with caution. Contraindicated in severe hepatic or renal impairment.
Dr Sharon Rees @reesprescribe
Day 4: #celecoxib mechanism of action: NSAIDs all bind to membrane-bound cyclooxygenase (COX) in the cells' endoplasmic reticulum. #celecoxib blocks the active site of inducible COX-2 enzymes, which lowers prostaglandin production. This reduces pain and inflammation. COX-1 activity is relatively unaffected, so superior gut protection.
Dr Sharon Rees @reesprescribe
Day 5: Common ADEs for #celecoxib include cough, hypersensitivity, rash, insomnia, arthralgia and myocardial infarction. Uncommon ADEs include heart failure, depression, tinnitus and visual disorders, (NOT exhaustive). Overall, there is a lower risk of gastrointestinal (GI) adverse effects, especially in high-risk groups, such as a history of peptic ulcer or GI vulnerability (such as ulcerative colitis). However, caution is still required and #celecoxib is contraindicated if active GI bleeding or ulceration.
Dr Sharon Rees @reesprescribe
Day 6: DDIs. CYP2D6 inhibition by #celecoxib can cause increased levels of antidepressants and more ADEs. Risk of bleeding with all anti-platelets/coagulants and SSRIs. Diuretics can cause acute renal failure and corticosteroids can increase the risk of GI bleeds. Combination with lithium or methotrexate can lead to toxicity (NOT exhaustive).
Dr Sharon Rees @reesprescribe
Day 7: Selective COX-2 inhibition by #celecoxib uncouples vascular cyclooxygenase function. This can lead to loss of antithrombotic protection and more cardiovascular events. Use is contraindicated in cerebrovascular disease, ischaemic heart disease and peripheral arterial disease.
Earn Your Cpd Certificate
With the help of Prescribing and Therapeutics Training Ltd and the Journal of Prescribing Practice, you can earn your 1-hour CPD certificate
In addition to the Tweets, read the BNF treatment summary on ‘Non-steroidal anti-inflammatory drugs and the monograph for Celecoxib, as well as the Celecoxib Summary of Product Characteristics and then answer the ten questions. Please submit the answers to reesprescribe@gmail.com as a numbered list with TRUE/FALSE or the correct A,B,C,D option. If you achieve 8 or more out of ten on the questions, a CPD certificate will be emailed to you.
- The discovery of the enzyme cyclooxygenase 1 (COX-1) and its functions happened before the discovery of COX-2? TRUE or FALSE?
- Which of the following is TRUE?
- Arachidonic acid is the main substrate for all forms of cyclooxygenase (COX) enzymes
- Prostaglandins are the only product of COX enzymatic activity
- COX-2 is only found in white blood cells
- Celecoxib is the only COX-2 inhibitor on the UK formulary
- Rofecoxib (Vioxx) was removed from the market because of the associated increased risk of cardiovascular events TRUE or FALSE?
- Celecoxib is licensed for use in all age groups TRUE or FALSE?
- Celecoxib is associated with significant genetic variations because of its active metabolites TRUE or FALSE?
- Which of the following is FALSE?
- Celecoxib is selective for blocking the COX-2 enzyme
- Celecoxib lowers prostaglandin levels and therefore inflammation
- Celecoxib should be taken with food
- COX-2 selective NSAIDs are associated with an increased risk of cardiovascular events
- Because of its selective effects, celecoxib cannot harm the gastrointestinal tract TRUE or FALSE?
- Cardiovascular events such as angina and myocardial infarction are ‘common’ adverse drug events for celecoxib TRUE or FALSE?
- Which of the following is TRUE?
- Celecoxib and non-selective NSAIDs have the same gastro-intestinal risk
- All diuretics have a ‘severe’ drug-drug interaction with celecoxib
- Visual disorders are common adverse drug events for celecoxib
- Celecoxib is safe to take in pregnancy
- It is a contraindication to take celecoxib if there is ischaemic heart disease TRUE or FALSE?
Further reading on #celecoxib
- Non-steroidal anti-inflammatory drugs: https://bnf.nice.org.uk/treatment-summaries/non-steroidal-anti-inflammatory-drugs/
- Celecoxib: https://bnf.nice.org.uk/drugs/celecoxib/
- Celecoxib 100 mg Capsules, hard: https://www.medicines.org.uk/emc/product/3445/smpc#PRODUCTINFO