carprofen - wikipedia, the free encyclopedia

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Systematic (IUPAC) name (RS)-2-(6-Chloro-9H-carbazol-2-yl)propanoic acid Clinical data AHFS/Drugs.com FDA Professional Drug Information Pregnancy cat. ? Legal status ? Pharmacokinetic data Protein binding High (99%) Half-life Approximately 8 h (range 4.5–9.8 h) in dogs Identifiers CAS number 53716-49-7 ATCvet code QM01AE91 PubChem CID 2581 DrugBank DB00821 ChemSpider 2483 UNII FFL0D546HO KEGG D03410 ChEBI CHEBI:364453 ChEMBL CHEMBL1316 Chemical data Formula C 15 H 12 ClNO 2 Mol. mass 273.714 g/mol (what is this?) (verify) Carprofen Carprofen From Wikipedia, the free encyclopedia Carprofen (marketed as Rimadyl, Imadyl, Novox, Imafen and Rovera, [1] ) is a non-steroidal anti-inflammatory drug that veterinarians prescribe as a supportive treatment for various conditions. It provides day-to-day treatment for pain and inflammation from arthritic in geriatric dogs, joint pain, osteoarthritis, hip dysplasia, and other forms of joint deterioration. It is also used to relieve short-term post-operative pain, inflammation, and swelling after spaying, neutering, and other procedures. Carprofen reduces inflammation by inhibition of COX-2 and other sources of inflammatory prostaglandins. This is targeted protection, in that it does not interfere with COX-1 activity. Contents 1 Administration 2 Health issues 3 Human use 4 References 5 External links Administration Carprofen is available in the USA in 25, 75 and 100 mg tablets (given with food or fed directly to the animal), and in injectable form. [2] In the UK, it is available in 20, 50 and 100 mg tablets. The usual dosage is 4.4 mg per kilogram (2.0 mg/lb) daily. [3] In Australia, carprofen is marketed as Norocarp or Tergive Injection. Norocarp is available in 20 mg and 50 mg tablets or Norophen in injectable liquid at 5.0% w/v, for cattle and canines. [4] Carprofen is also marketed in many Latin- American (and some Asian and African countries) as Carprodyl in 25 mg and 100 mg tablets for canines and Carprobay in 20 mg and 50 mg tablets for dogs. [5] Carprofen is sometimes divided between morning and evening doses. It is administered two hours before surgery for post-operative pain. SMILES InChI Carprofen - Wikipedia, the free encyclopedia http://en.wikipedia.org/wiki/Carprofen 1 of 4 06-07-2013 23:19

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Page 1: Carprofen - Wikipedia, The Free Encyclopedia

Systematic (IUPAC) name

(RS)-2-(6-Chloro-9H-carbazol-2-yl)propanoic acid

Clinical data

AHFS/Drugs.com FDA Professional Drug

Information

Pregnancy cat. ?

Legal status ?

Pharmacokinetic data

Protein binding High (99%)

Half-life Approximately 8 h (range

4.5–9.8 h) in dogs

Identifiers

CAS number 53716-49-7

ATCvet code QM01AE91

PubChem CID 2581

DrugBank DB00821

ChemSpider 2483

UNII FFL0D546HO

KEGG D03410

ChEBI CHEBI:364453

ChEMBL CHEMBL1316

Chemical data

Formula C15H12ClNO

2

Mol. mass 273.714 g/mol

(what is this?) (verify)

Carprofen

CarprofenFrom Wikipedia, the free encyclopedia

Carprofen (marketed as Rimadyl, Imadyl, Novox, Imafen

and Rovera,[1]) is a non-steroidal anti-inflammatory drug

that veterinarians prescribe as a supportive treatment for

various conditions. It provides day-to-day treatment for pain

and inflammation from arthritic in geriatric dogs, joint pain,

osteoarthritis, hip dysplasia, and other forms of joint

deterioration.

It is also used to relieve short-term post-operative pain,

inflammation, and swelling after spaying, neutering, and

other procedures. Carprofen reduces inflammation by

inhibition of COX-2 and other sources of inflammatory

prostaglandins. This is targeted protection, in that it does not

interfere with COX-1 activity.

Contents

1 Administration

2 Health issues

3 Human use

4 References

5 External links

Administration

Carprofen is available in the USA in 25, 75 and 100 mg

tablets (given with food or fed directly to the animal), and in

injectable form.[2] In the UK, it is available in 20, 50 and

100 mg tablets. The usual dosage is 4.4 mg per kilogram

(2.0 mg/lb) daily.[3]

In Australia, carprofen is marketed as Norocarp or Tergive

Injection. Norocarp is available in 20 mg and 50 mg tablets

or Norophen in injectable liquid at 5.0% w/v, for cattle and

canines.[4] Carprofen is also marketed in many Latin-

American (and some Asian and African countries) as

Carprodyl in 25 mg and 100 mg tablets for canines and

Carprobay in 20 mg and 50 mg tablets for dogs.[5]

Carprofen is sometimes divided between morning and

evening doses. It is administered two hours before surgery for post-operative pain.

SMILES

InChI

Carprofen - Wikipedia, the free encyclopedia http://en.wikipedia.org/wiki/Carprofen

1 of 4 06-07-2013 23:19

Page 2: Carprofen - Wikipedia, The Free Encyclopedia

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

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.[6] 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.[citation needed]

Symptoms to watch for include:

Loss of appetite

Vomiting

Diarrhea

Increase in thirst

Increase in urination

Fatigue and/or Lethargy

Loss of coordination

Seizures

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:

Black, tarry stools or flecks of blood in the vomit

Drowsiness

Staggering, stumbling, weakness or partial paralysis, full paralysis, dizziness, loss of balance.[7]

Change in urination habits (frequency, color, or smell)

Change in skin (redness, scabs, or scratching)

Change in behavior (such as decreased or increased activity level, seizure or aggression).[8]

Excess use of Rimadyl can lead to gastritis and ulcer formation.[9] 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).

Carprofen - Wikipedia, the free encyclopedia http://en.wikipedia.org/wiki/Carprofen

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Page 3: Carprofen - Wikipedia, The Free Encyclopedia

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 and within the closely monitoring 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.[10] Also, it has been not yet established if 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 placebo-treated animals.[citation needed]

There are a number of factors that might however contribute to the high incidence of adverse drug experience

reports received for Rimadyl by the Center for Veterinary Medicine in the late 1990s. These include:

The type of drug;

Wide use;

Duration of use. While the side effects from Rimadyl are known to occur within a short period of time

after administration, it is believed that long-term use may actually result in a higher risk for adverse

reactions;

Senior dog use. Older dogs are generally more prone to side effects caused by carprofen.

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. 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. The

drug was taken orally. Pfizer voluntarily pulled it from the market for human use on commercial grounds.[11]

References

^ Pfizer Animal Health-Rimadyl (http://www.rimadyl.com/display.asp?country=US&lang=EN&drug=RC&

species=CN&sec=000)

1.

^ http://www.srdogs.com/Pages/rimadyl.html2.

^ Rimadyl Dosage Chart (https://www.rimadyl.com/content/RIM016007.pdf) Retrieved 2011-10-11.3.

^ Norbrook Pharmaceuticals Worldwide - Australia (http://www.norbrook.com.au)4.

^ Agrovet Market Animal Health - Peru (http://www.agrovetmarket.com)5.

^ "Update On Rimadyl, FDA's Center for Veterinary Medicine, December 1, 1999" (http://www.fda.gov

/AnimalVeterinary/NewsEvents/CVMUpdates/ucm129408.htm).

6.

^ "A Review of Signs of a Potentially Life-threatening Reaction to Rimadyl" (http://www.srdogs.com/Pages7.

Carprofen - Wikipedia, the free encyclopedia http://en.wikipedia.org/wiki/Carprofen

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Page 4: Carprofen - Wikipedia, The Free Encyclopedia

/rimadyl.ade.steps.html). Retrieved 2010-05-20.

^ "Dog Owner Information About Rimadyl (carprofen)" (https://www.rimadyl.com/display.aspx?drug=RC&

species=CN&sec=610). Retrieved 2010-05-20.

8.

^ "Generic Dog Rimadyl Online" (http://www.rimadylonline.com/). Retrieved 2010-05-20.9.

^ "Rimadyl (Carprofen)" (http://www.vetdepot.com/Rimadyl-Carprofen-25mg-60-Caplets.html). Retrieved

2010-05-20.

10.

^ Committee for Veterinary Medicinal Products: Carprofen (http://www.emea.europa.eu/pdfs/vet

/mrls/004295en.pdf), European Agency for the Evaluation of Medicinal Products

11.

External links

Rimadyl warning (http://www.pgaa.com/canine/health/rimadylwarning.html)

Pfizer product website PDS (http://www.rimadyl.com/display.asp?country=US&lang=EN&drug=RC&

species=CN&sec=660)

Senior dogs and Rimadyl (http://www.srdogs.com/Pages/rimadylfr.html)

Retrieved from "http://en.wikipedia.org/w/index.php?title=Carprofen&oldid=555985841"

Categories: Non-steroidal anti-inflammatory drugs Dog health Carbazoles Organochlorides

Veterinary drugs

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Carprofen - Wikipedia, the free encyclopedia http://en.wikipedia.org/wiki/Carprofen

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