 Carprofen molecule | |
| Clinical data | |
|---|---|
| Trade names | Rimadyl, others |
| AHFS/Drugs.com | FDA Professional Drug Information |
| License data | |
| Routes of administration | By mouth, injection |
| ATCvet code | |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Protein binding | High (99%) |
| Eliminationhalf-life | Approximately 8 h (range 4.5–9.8 h) in dogs |
| Identifiers | |
| |
| CAS Number | |
| PubChemCID | |
| IUPHAR/BPS | |
| DrugBank |
|
| ChemSpider |
|
| UNII | |
| KEGG |
|
| ChEBI | |
| ChEMBL | |
| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.053.357 |
| Chemical and physical data | |
| Formula | C15H12ClNO2 |
| Molar mass | 273.72 g·mol−1 |
| 3D model (JSmol) | |
| Chirality | Racemic mixture |
| |
| |
| (verify) | |
Carprofen is anonsteroidal anti-inflammatory drug (NSAID) of thecarbazole andpropionic acid class that was previously for use in humans and animals but is now only available toveterinarians for prescribing as asupportive treatment for various conditions in animals.[1] Carprofen reducesinflammation by inhibition ofCOX-1 andCOX-2; its specificity for COX-2 varies from species to species.[1] Marketed under manybrand names worldwide,[5] carprofen is used as a treatment for inflammation andpain, includingjoint pain andpostoperative pain.[1]
Carprofen was used in humans for almost ten years, starting in 1988, for the same conditions as in dogs; namely, joint pain and inflammation. Side effects tended to be mild, usually consisting ofnausea orgastrointestinal pain anddiarrhoea. It was available byprescription in 150 mg to 600 mg doses.[6] Dosages over 250 mg were reserved for pain caused by severetrauma, such as postoperative inflammation; 150 mg doses were commonly used to relievearthritis pain, while 200 mg doses were commonly prescribed for severe arthritis or inflammatory pain. The drug was taken orally.
Pfizer voluntarily removed the medication from the market for human use on commercial grounds.[6]
Carprofen is the most commonly used NSAID in dogs.[7] It aids in the relief of inflammation, pain, andfever. Carprofen can be administered inpill,chewable tablet, orinjection form.[8]
Carprofen can be used for long-termpain management of conditions such asosteoarthritis, which is common in canine patients, and after injury orsurgical procedures for relief ofacute pain and inflammation.[8][1]
Most dogs respond well to carprofen use, but like all NSAIDs, it can cause gastrointestinal, liver, and kidney problems.[9]
In 1999, theFood and Drug Administration (FDA) received more than six thousand anecdotal reports of sudden animal death after usage ofPfizer's Rimadyl brand of carprofen. In response, the FDA requested that Pfizer advise consumers in their advertising that death is a possibleside effect;[10] Pfizer refused and pulled their advertising, later including death as a possible side effect on theprescribing information.[11]
Adverse effects can include:
Effects of overdose includegastritis and ulcer formation.[1]
In healthy dogs given carprofen, no perioperative adverse effects on the cardiovascular system have been reported at recommended dosages.[14][15] Perioperative administration of carprofen to cats affected neither postoperative respiratory rate nor heart rate.[16]
Laboratory studies andclinical trials have been conducted to assess the safety of carprofen. These clinical studies involved nearly 300 dogs of various breeds, which were treated with carprofen at the recommended dosage for two weeks. The findings indicated that the drug was well tolerated, and the treated dogs did not experience a higher rate of adverse reactions compared to the control group.[1][medical citation needed]
A number of factors may have contributed to the high incidence of adverse reports received for carprofen by the FDA'sCenter for Veterinary Medicine in the late 1990s. These include:
Carprofen may be administeredintravenously to horses.[18] A single dose has been shown to reduceprostaglandin E2 production and inflammatoryexudate for up to 15 hours,[19] albeit with an inferior effect oneicosanoid production relative tophenylbutazone andflunixin.[20]Leukotriene B4 release is inhibited, as well. Carprofen can be given orally; intramuscular use may produce muscle damage.[21]
Carprofen is used as an analgesic for mouse surgical procedures.[22] Carprofen may also be used in adult fish.[23]
It is marketed under many brand names including: Acticarp, Artriofin, Austiofen, Bomazeal, Canidryl, Carporal, Carprieve, Carprocow, Carprodolor, Carprodyl, Carprofelican, Carprofen, Carprofène, Carprofeno, Carprofenum, Carprogesic, Carprosol, Carprotab, Carprox, Comforion, Dolagis, Dolocarp, Dolox, Eurofen, Kelaprofen, Librevia, Norocarp, Norodyl, Novocox, Ostifen, Prolet, Quellin, Reproval, Rimadyl, Rimifin, Rofeniflex, Rovera, Rycarfa, Scanodyl, Tergive, Vetprofen, and Xelcor.[5]
Media related toCarprofen at Wikimedia Commons
| pyrazolones / pyrazolidines | |
|---|---|
| salicylates | |
| acetic acid derivatives and related substances | |
| oxicams | |
| propionic acid derivatives (profens) |
|
| n-arylanthranilic acids (fenamates) | |
| COX-2 inhibitors (coxibs) | |
| other | |
| NSAID combinations | |
Key:underline indicates initially developed first-in-class compound of specific group;#WHO-Essential Medicines;†withdrawn drugs;‡veterinary use. | |
.jpg)
