Carprofen

Carprofen
Clinical data
AHFS/Drugs.com FDA Professional Drug Information
ATCvet code QM01AE91 (WHO)
Legal status
Legal status
  • US: Veterinary use only. It was Rx-only in humans.
Pharmacokinetic data
Protein binding High (99%)
Biological half-life Approximately 8 h (range 4.5–9.8 h) in dogs
Identifiers
CAS Number 53716-49-7 YesY
PubChem (CID) 2581
IUPHAR/BPS 7141
DrugBank DB00821 YesY
ChemSpider 2483 YesY
UNII FFL0D546HO YesY
KEGG D03410 YesY
ChEBI CHEBI:364453 YesY
ChEMBL CHEMBL1316 YesY
ECHA InfoCard 100.053.357
Chemical and physical data
Formula C15H12ClNO2
Molar mass 273.714 g/mol
3D model (Jmol) Interactive image
Chirality Racemic mixture
  (verify)
A 100 mg Rimadyl pill approximately 19 mm (0.75 in) wide and 8.6 mm (0.34 in) thick, sold in the United States

Carprofen, marketed under many brand names worldwide,[1] is a non-steroidal anti-inflammatory drug that veterinarians prescribe as a supportive treatment for various conditions in animals.[2] It provides day-to-day treatment for pain and inflammation from various kinds of joint pain as well as post-operative pain.[2] Carprofen reduces inflammation by inhibition of COX-1 and COX-2; its specificity for COX-2 varies from species to species.[2]

Health issues

Most dogs respond well to carprofen use, but like all non-steroidal anti-inflammatory (NSAID) medications used in humans and animals, it is capable of causing gastrointestinal, liver and kidney problems in some patients.

After introduction, significant anecdotal reports of sudden animal deaths from its use arose. To date , the FDA has received more than 6,000 adverse reaction reports about the drug (manufactured by Pfizer). As a result, the FDA requested that Pfizer advise consumers in their advertising that death is a possible side effect.[3] Pfizer refused and pulled their advertising; however, they now include death as a possible side effect on the drug label. Plans call for a "Dear Doctor" letter to advise veterinarians, and a safety sheet attached to pill packages.

Pfizer acknowledges a problem with some dog owners, especially a consumer group that mounted a campaign dubbed BARKS, for Be Aware of Rimadyl's Known Side-effects—which include loss of appetite, wobbling, vomiting, seizures, and severe liver malfunction. Reports say the drug company has contacted pet owners who told their stories on the Internet, offering to pay medical and diagnostic expenses for dogs that carprofen may have harmed.

Symptoms to watch for include:

Other symptoms worth discussing with a vet include excessive drinking or urination, blood or dark tar-like material in urine or stools, jaundice (yellowing of eyes), and unusual lethargy.

Other side effects of Rimadyl include:

Excess use of Rimadyl can lead to gastritis and ulcer formation.[6] It is also believed that in some breeds of dogs it may induce kidney and liver damage.

Carprofen should not be administered to animals that are also being given steroids (one of the primary risks of this combination being that it can cause ulcers in the stomach). In dogs, it is recommended that the dog be taken off carprofen for three full days before ingesting a steroid (such as prednisolone).

According to the official Rimadyl website, the drug should not be given at the same time with other types of medications such as other NSAIDs (aspirin, etodolac, deracoxib, meloxicam, tepoxalin) or steroids such as dexamethasone, triamcinolone, cortisone or prednisone. However, dog owners whose pets have been administered Rimadyl and have experienced side effects are highly recommended to contact a veterinarian as soon as they appear and to stop the therapy.

Also, Rimadyl must be used with caution within the supervision of a veterinarian in dogs with liver or kidney disease, dehydration, bleeding deficits, or other health problems. Rimadyl is not recommended for use in dogs with bleeding disorders (such as Von Willebrand's disease), as safety has not been established in dogs with these disorders.[7] Also, it has not yet been established whether Rimadyl can be safely used in pregnant dogs, dogs used for breeding purposes, or in lactating female dogs.

Several laboratory studies and clinical trials have been conducted to establish the safety of using Rimadyl. Clinical studies were conducted in nearly 300 dogs, coming from different breeds. These dogs have been treated with Rimadyl at the recommended dose for 2 weeks. According to these studies, the drug was clinically well tolerated and dogs treated with Rimadyl did not have a greater incidence of adverse reactions when compared to the control group.[8]

There are however a number of factors that may contribute to the high incidence of adverse reports received for Rimadyl by the Center for Veterinary Medicine in the late 1990s. These include:

Human use

Carprofen was used in humans for almost 10 years, starting in 1988. It was used for the same conditions as in dogs, viz., joint pain and inflammation. The human body accepted the drug well and side effects tended to be mild, usually consisting of nausea or gastro-intestinal pain and diarrhea. For human use, Rimadyl was available only by prescription in 150 to 600 mg doses. Dosage over 250 mg was only for relieving pain after severe trauma, such as post-surgery inflammation.[9] 150 mg doses were commonly used to relieve the pain of arthritis, while 200 mg doses were commonly prescribed in cases of severe arthritis or severe inflammation pain.[9] The drug was taken orally. Pfizer voluntarily pulled it from the market for human use on commercial grounds.[9]

Equine use

Carprofen is given intravenously to horses at a dose of 0.7 mg/kg once daily.[10] A single dose has been shown to reduce prostaglandin E2 production and inflammatory exudate for up to 15 hours,[11] although there was less effect on eicosanoid production when compared to the effects produced by NSAIDs such as phenylbutazone or flunixin.[12] Prostaglandin E2 and inflammatory exudate are better reduced at a dose of 4 mg/kg IV, with the added benefit of inhibition of leukotriene B4. Carprofen can also be given orally, but intramuscular use may produce muscle damage.[13]

Brands and dosage forms

It is marketed under many brand names including:[1]

Veterinary dosage forms include 25 mg, 75 mg, and 100 mg tablets, and 50 mg per mL injectable form.[14]

References

  1. 1 2 Drugs.com International brand names for Carprofen Page accessed Aug 17, 2016
  2. 1 2 3 Carprofen/Rimadyl (Carprofen) prescribing instructions
  3. ↑ "Update On Rimadyl, FDA's Center for Veterinary Medicine, December 1, 1999".
  4. ↑ "A Review of Signs of a Potentially Life-threatening Reaction to Rimadyl". Retrieved 2010-05-20.
  5. ↑ "Dog Owner Information About Rimadyl (carprofen)". Retrieved 2010-05-20.
  6. ↑ "Generic Dog Rimadyl Online". Retrieved 2010-05-20.
  7. ↑ "Rimadyl (Carprofen)". Retrieved 2010-05-20.
  8. ↑ "Rimadyl [package insert]. New York, NY: Pfizer Animal Health, 2007." (PDF). Retrieved 2014-08-13.
  9. 1 2 3 Committee for Veterinary Medicinal Products: Carprofen, European Agency for the Evaluation of Medicinal Products
  10. ↑ McIlwraith CW, Frisbie DD, Kawcak CE. Nonsteroidal Anti-Inflammatory Drugs. Proc. AAEP 2001 (47): 182-187.
  11. ↑ Lees P, McKellar Q, May SA, Ludwig B. Pharmacodynam- ics and pharmacokinetics of carprofen in the horse. Equine Vet J 1994;26:203–208.
  12. ↑ Lees P, Ewins CP, Taylor JBO, Sedgwick AD. Serum thromboxane in the horse and its inhibition by aspirin, phe- nylbutazone and flunixin. Brit Vet J 1987;143:462–476.
  13. ↑ McKellar QA, Bogan JA, Fellenberg RL, et al. Pharmacoki- netic, biochemical and tolerance studies on carprofen in the horse. Equine Vet J 1991;23:280–284.
  14. ↑ Carprofen (Veterinary—Systemic) The United States Pharmacopeial Convention, 2007


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