Description

Simple

A pain killer medication used to treat arthritis and painful symptoms during the menstrual cycle.

Clinical

A COX-2 inhibitor used to treat osteoarthritis and dysmenorrhoea.

Overview

Valdecoxib was removed from the Canadian, U.S., and E.U. markets in 2005 due to concerns about a possible increased risk of heart attack and stroke.

Pharmacology

Indication

For the treatment of osteoarthritis and dysmenorrhoea

Pharmacodynamic

Valdecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, is classified as a nonsteroidal anti-inflammatory drug (NSAID). Valdecoxib is used for its anti-inflammatory, analgesic, and antipyretic activities in the management of osteoarthritis (OA) and for the treatment of dysmenorrhea or acute pain... Read more

Mechanism of action

Both COX-1 and COX-2 catalyze the conversion of arachidonic acid to prostaglandin (PG) H2, the precursor of PGs and thromboxane. Valdecoxib selectively inhibits the cyclooxygenase-2 (COX-2) enzyme, important for the mediation of inflammation and pain. Unlike non-selective NSAIDs, valdecoxib does not... Read more

Absorption

Oral bioavailability is 83%.

Protein binding

98%

Volume of distribution

86 L

Clearance

oral cl=6 L/h6 – 7 L/h [In patients undergoing hemodialysis]6 – 7 L/h [healthy elderly subjects]

Half life

8-11 hours

Route of elimination

Valdecoxib is eliminated predominantly via hepatic metabolism with less than 5% of the dose excreted unchanged in the urine and feces. About 70% of the dose is excreted in the urine as metabolites, and about 20% as valdecoxib N-glucuronide.

Toxicity

Symptoms following acute NSAID overdoses are usually limited to lethargy, drowsiness, nausea, vomiting, and epigastric pain, which are generally reversible with supportive care. Gastrointestinal bleeding can occur. Hypertension, acute renal failure, respiratory depression and coma may occur, but are... Read more

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Post Operative Pain
      • Drugbank Id: DBCOND0031846
  • Patient Conditions Associated With:
      • Name: Coronary Artery Bypass Graft Surgery Patients
      • Drugbank Id: DBCOND0033212
  • Hypersensitivity:
    • true
    • sulfonamides
  • Regions: US
  • Hypersensitivity:
    • NSAIDs
  • Regions: US

Food Interactions

  • Avoid alcohol. Ingesting alcohol may increase the risk of gastrointestinal bleeding.
  • Take with or without food.

Interactions

Type in a drug name to check for interaction with Valdecoxib
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The risk or severity of bleeding and hemorrhage can be increased when Valdecoxib is combined with (R)-warfarin.
(S)-Warfarin
The risk or severity of bleeding and hemorrhage can be increased when Valdecoxib is combined with (S)-Warfarin.
1-benzylimidazole
The risk or severity of hypertension can be increased when Valdecoxib is combined with 1-benzylimidazole.
2,5-Dimethoxy-4-ethylamphetamine
The risk or severity of hypertension can be increased when Valdecoxib is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of hypertension can be increased when Valdecoxib is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of hypertension can be increased when Valdecoxib is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-hydroxycoumarin
The risk or severity of bleeding and hemorrhage can be increased when Valdecoxib is combined with 4-hydroxycoumarin.
4-Methoxyamphetamine
The risk or severity of hypertension can be increased when Valdecoxib is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of hypertension can be increased when Valdecoxib is combined with 5-methoxy-N,N-dimethyltryptamine.
Abacavir
Valdecoxib may decrease the excretion rate of Abacavir which could result in a higher serum level.
Abatacept
The metabolism of Valdecoxib can be increased when combined with Abatacept.
Abciximab
The risk or severity of bleeding and hemorrhage can be increased when Valdecoxib is combined with Abciximab.
Abediterol
The risk or severity of hypertension can be increased when Valdecoxib is combined with Abediterol.
Abiraterone
The metabolism of Valdecoxib can be decreased when combined with Abiraterone.
Acarbose
Valdecoxib may decrease the excretion rate of Acarbose which could result in a higher serum level.
Acebutolol
Valdecoxib may decrease the antihypertensive activities of Acebutolol.
Aceclofenac
The risk or severity of adverse effects can be increased when Valdecoxib is combined with Aceclofenac.
Acemetacin
The risk or severity of adverse effects can be increased when Valdecoxib is combined with Acemetacin.
Acenocoumarol
The risk or severity of bleeding and hemorrhage can be increased when Valdecoxib is combined with Acenocoumarol.
Acepromazine
The risk or severity of hypertension can be increased when Valdecoxib is combined with Acepromazine.
1 References
  1. 1 . FDA Approved Drug Products: Betra (valdecoxib) oral tablets Link