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ketoprofen

 
Drug Info:

Ketoprofen

Brand names: Orudis®, Orudis® KT, Oruvail®

Chemical formula:



Ketoprofen tablets or capsules

What do ketoprofen tablets or capsules do?

KETOPROFEN (Orudis® KT™, Oruvail®) is an anti-inflammatory drug. Ketoprofen helps relieve the inflammation and pain associated with rheumatoid arthritis, osteoarthritis, menstrual cramps or premenstrual pain and swelling. Ketoprofen is available in a non-prescription strength to treat minor aches and pains associated with the common cold, backache, muscular aches, toothache and menstrual pain. Generic ketoprofen immediate- and extended-release capsules are available.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• asthma, especially aspirin-sensitive asthma
• bleeding problems
• cigarette smoker
• coronary artery bypass graft (CABG) surgery within the past 2 weeks
• diabetes mellitus
• drink more than 3 alcohol-containing beverages a day
• heart or circulation problems like angina, high blood pressure, heart failure, heart rhythm problems, history of heart attack, history of blood clots, or leg edema (fluid retention)
• kidney disease
• liver disease
• lost a lot of fluid due to continued vomiting or diarrhea
• stomach or duodenal ulcers
• history of stroke
• systemic lupus erythematosus
• ulcerative colitis
• an unusual or allergic reaction to ketoprofen, aspirin, other salicylates, other NSAIDs, foods, dyes or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I take this medicine?

Take ketoprofen tablets or capsules by mouth. Follow the directions on the label. Swallow tablets or capsules whole with a full glass of water; take tablets or capsules in an upright or sitting position. Taking a sip of water first, before taking the tablets or capsules, may help you swallow them. If possible take bedtime doses at least 10 minutes before lying down. Do not crush or chew the extended-release capsules. You can take ketoprofen with food to prevent stomach upset. Take your doses at regular intervals. Do not take your medicine more often or for a longer time than directed.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.

What other medicines can interact with ketoprofen?

• alcohol
alendronate
• anti-inflammatory drugs (other NSAIDs, prednisone)
• aspirin and aspirin-like medicines
cidofovir
cyclosporine
• drospirenone; ethinyl estradiol (Yasmin®)
entecavir
• herbal products that contain feverfew, garlic, ginger, or ginkgo biloba
lithium
• medicines for high blood pressure
• medicines that affect platelets
• medicines that treat or prevent blood clots such as warfarin and other 'blood thinners'
methotrexate
pemetrexed
• water pills (diuretics)

Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What do I need to watch for while I take ketoprofen?

Let your prescriber or health care professional know if your pain continues, do not take with other pain medicines or fever medicine without advice. If you get flu-like symptoms (fever, chills, muscle aches and pains), call your prescriber or health care professional. Do not treat yourself.

To reduce unpleasant effects on your throat and stomach, take ketoprofen with a full glass of water and never just before lying down. Take ketoprofen with food or milk if stomach upset occurs. If you notice black, tarry stools or experience severe stomach pain and vomit blood or what looks like coffee grounds, notify your health care prescriber immediately. If you have stomach pain or an upset stomach that worsens or persists, redness or swelling in a painful area, or any new symptoms, call your health care professional.

If you are taking medicines that affect the clotting of your blood, such as aspirin or blood thinners such as Coumadin®, talk to your health care provider or prescriber before taking this medicine.

You may get dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how ketoprofen affects you. Do not sit or stand up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells.

Do not smoke cigarettes or drink alcohol; these increase irritation to your stomach and can make it more susceptible to damage from ketoprofen.

It is especially important not to use ketoprofen during the last 3 months of pregnancy unless specifically directed to do so by your health care provider. Ketoprofen may cause problems in the unborn child or complications during delivery.

If you are going to have surgery, tell your prescriber or health care professional that you are taking ketoprofen. Problems can arise if you need dental work, and in the day to day care of your teeth. Try to avoid damage to your teeth and gums when you brush or floss your teeth.

What side effects may I notice from taking ketoprofen?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• signs of bleeding - black tarry stools, blood in the urine, unusual tiredness or weakness, vomiting blood or vomit that looks like coffee grounds
• signs of an allergic reaction - difficulty breathing, wheezing, skin rash, redness, blistering or peeling skin, hives, itching, swelling of eyelids, throat, lips
• blurred vision
• change in the amount of urine passed
• difficulty swallowing, severe heartburn or burning, pain in throat
• pain or difficulty passing urine
• stomach pain or cramps
• swelling of feet or ankles

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• diarrhea or constipation
• dizziness, drowsiness
• gas or heartburn
• headache
• nausea, vomiting

Where can I keep my medicine?

Keep out of the reach of children in a container that small children cannot open.

Store at room temperature, approximately 25 degrees C (77 degrees F) away from humidity (not in the bathroom or kitchen, if possible). Keep container tightly closed. Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

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An non-steroidal anti-inflammatory drug used for the treatment of pain and mild inflammation in rheumatoid arthritis and other disorders of muscles or joints. It is also used to relieve period pains, acute gout, sciatica, and pain occurring after orthopaedic surgery. It is available, on prescription only, as capsules, modified-release capsules, suppositories, an injection, and a gel for topical application (some gel formulations are also available without a prescription).

Side effects:
see non-steroidal anti-inflammatory drugs. Suppositories may cause local irritation; there may be pain at the site of the injection.

Precautions and interactions with other drugs:
see non-steroidal anti-inflammatory drugs.

Proprietary preparations:
Boots Muscular Pain Relief Gel; Ketocid (modified-release capsules); Ketoprofen continuous release (= modified release) (modified-release capsules); Ketovail (modified-release capsules); Orudis (capsules); Orudis Suppositories; Oruvail (modified-release capsules, gel, and injection); Powergel (gel).

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Columbia Encyclopedia:

ketoprofen

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ketoprofen (kē'təprō'fĭn), nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and fever-reducing effects, used to relieve the symptoms of headaches, arthritis, and painful menstruation. Along with ibuprofen and naproxen, it belongs to the propionic acid class of NSAIDs; it apparently acts by inhibiting the body's production of prostaglandins. Available as a prescription drug for more than 20 years in many countries, it was approved as an over-the-counter painkiller in the United States in 1995 and first marketed as Orudis KT. It is considered more powerful than many other NSAIDs. Side effects may include gastrointestinal disturbances and fluid retention.


Word Tutor:

ketoprofen

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pronunciation

IN BRIEF: n. - Nonsteroidal anti-inflammatory drug (trade names Orudis or Orudis KT or Oruvail).

LearnThatWord.com is a free vocabulary and spelling program where you only pay for results!


2-(3-benzoylphenyl)propionic acid; a nonsteroidal anti-inflammatory agent; it inhibits prostaglandin-endoperoxide synthase (EC 1.14.99.1). See also ibuprofen.





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A propionic acid, nonsteroidal anti-inflammatory agent; used also as an analgesic and antipyretic.


n

trade names: Orudis, Oruvail, Actron; drug class: nonsteroidal antiinflammatory; action: inhibits prostaglandin synthesis by interfering with cyclooxygenase needed for biosynthesis; possesses analgesic, antiinflammatory, antipyretic properties; uses: osteoarthritis, rheumatoid arthritis, dysmenorrhea.

Wikipedia on Answers.com:

Ketoprofen

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Ketoprofen
Systematic (IUPAC) name
(RS)-2-(3-benzoylphenyl)propanoic acid
Clinical data
AHFS/Drugs.com monograph
MedlinePlus a686014
Pregnancy cat. C (D in 3rd trimester)
Legal status Prescription-only medicine
Routes Oral, topical, intravenous (veterinary use)
Pharmacokinetic data
Protein binding 99%
Half-life 2-2.5 hours
Identifiers
CAS number 22071-15-4 YesY
ATC code M01AE03 M01AE17, M02AA10
PubChem CID 3825
DrugBank DB01009
ChemSpider 3693 YesY
UNII 90Y4QC304K YesY
KEGG D00132 YesY
ChEBI CHEBI:6128 N
ChEMBL CHEMBL571 YesY
Chemical data
Formula C16H14O3 
Mol. mass 254.281 g/mol
SMILES eMolecules & PubChem
 N(what is this?)  (verify)

Ketoprofen, (RS)2-(3-benzoylphenyl)-propionic acid (chemical formula C16H14O3) is one of the propionic acid class of non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic effects.[1] It acts by inhibiting the body's production of prostaglandin.

Contents

Available forms

Ketoprofen was available over-the-counter in the United States in the form of 12.5 mg coated tablets (Orudis KT & Actron), but this form has been discontinued. It is available by prescription as 50, 75, 100, 150, and 200 mg capsules.

Ketoprofen is available also as a 2.5% gel for topical application.

Brand names in the US are Orudis and Oruvail. It is available in the UK as Ketoflam and Oruvail, in Finland as Ketorin, Keto, Ketomex, and Orudis'; in France as Profénid, Bi-Profénid and Ketum, in Italy as Ketodol, Fastum Gel, Lasonil, Orudis or Oki, in Poland, Serbia, Slovenia and Croatia as Knavon or Ketonal, in Mexico as Arthril, in Norway as Zon or Orudis, in Russia as ОКИ (OKI) and Ketonal, in Spain as Actron and in Venezuela as Ketoprofeno under an injectable solution of 100 mg and 150 mg capsules.

In Lithuania, ketoprofen is called Ketoprofenum and/or Ketoprofenas. For topical application: the name brands are Fastum with 2.5% (gel) which is over the counter and Ketospray with 10% (liquid spray) which must be prescribed. In Switzerland, an innovative ketoprofen formulation based on Transfersome technology for direct application on the skin above the site to be treated has been approved.

In some countries, the optically pure (S)-enantiomer (dexketoprofen) is available; its trometamol salt is said to be particularly rapidly reabsorbed from the gastrointestinal tract, having a rapid onset of effects.

Indication

Ketoprofen is generally prescribed for arthritis-related inflammatory pains or severe toothaches that result in the inflammation of the gums.

Ketoprofen topical patches are being extensively used for treatment of musculoskeletal pain.[2][3][4] The patches have been shown to provide rapid and sustained delivery to underlying tissues without significantly increasing levels of drug concentration in the blood when compared to the traditional oral administration.[4][5] Ketoprofen undergoes metabolism in the liver via conjugation with glucoronic acid, CYP3A4 and CYP2C9 hydroxylation of the benzoyl ring, and reduction of its keto function.[6][7] Ketoprofen is used for its antipyretic, analgesic, and anti-inflammatory properties by inhibiting cyclooxygenase-1 and -2 (COX-1 and COX-2) enzymes reversibly, which decreases production of pro-inflammatory prostaglandin precursors.[6][8]

Ketoprofen can also be used for treatment of some pain, especially nerve pain like sciatica, post-herpetic neuralgia and referred pain for radiculopathy, in the form of a cream, ointment, liquid, spray, or gel which also contains ketamine and lidocaine, along with other agents which may be useful such as cyclobenzaprine, amitryptiline, acyclovir, gabapentin, orphenadrine and other drugs used as NSAIDs or adjuvant, atypical or potentiators for pain treatment.

Efficacy

The results vary in each case, with varying degrees of the attenuation of the burning, tingling, and/or shooting component of neuralgic pain being quite frequent, along with a modest reduction in overall pain level in some cases. In severe cases and those involving multiple conditions in addition to the cause of the neuralgia, there is no substitute for comprehensive palliative therapy including systemic NSAIDs, opioids, muscle relaxants, intermittent corticosteroids and other agents if needed and adjuncts & potentiators to increase the power of the analgesics in addition to the topical preparation and physical and alternative modalities such as physiotherapy, acupuncture, biofeedback & related modalities, nutritional approaches and many others relevant to each case. Even the addition of the opioid tramadol to topical preparations is not known to be an adequate replacement for systemic opioids in cases where they can be useful and efficacious.

Use in horses and other animals

Ketoprofen is a common NSAID, antipyretic, and analgesic used in horses and other equines.[9] It is also used as a mild painkiller in smaller animals, generally following surgical procedures. It is most commonly used for musculoskeletal pain, joint problems, and soft tissue injury, as well as laminitis. It does not treat the underlying problem, nor does it speed the healing process. It is also used to control fevers and prevent endotoxemia. However, they may mask the symptoms of the underlying problem, and therefore make diagnosis more difficult for a veterinarian.

Uses with other drugs

Ketoprofen should not be used in with other NSAIDs or corticosteroids, as this increases the risk of GI ulceration. It should also be used with caution with other anticoagulants. It is commonly used with omeprazole, sucralfate, and cimetidine to help protect the GI tract.

Administration

Ketoprofen, when administered intravenously, is recommended for a maximum of five days of use. Its analgesic and antipyretic effects begin to occur 1–2 hours following administration. The most common dosage is 1 mg/ lb, once per day, although this dosage may be lowered for ponies, who are most susceptible to NSAID side effects. It is also available as a capsule dosage form and a tablet.

Ecological problems

Recent studies have found that Ketoprofen, like Diclofenac is a veterinary drug causing lethal effects in Red-headed Vultures. Vultures feeding on the carcasses of recently-treated livestock suffer acute kidney failure within days of exposure.[10]

According to research, the vulture population has undergone a sharp decline on the Indian subcontinent, 95% decline in 2004, 99.9% decline as of 2008 due to the use of Diclofenac in animals.[11]

The loss of vultures has had a social impact on the Indian Zoroastrian Parsi community, who traditionally use vultures to dispose of human corpses in a Tower of Silence, but are now compelled to seek alternate methods of disposal.

References

  1. ^ Kantor, T. G. (1986). "Ketoprofen: a review of its pharmacologic and clinical properties". Pharmacotherapy 6 (3): 93–103. PMID 3526298. 
  2. ^ Mazières, B; Rouanet, S; Guillon, Y; Scarsi, C; Reiner, V (2005). "Topical ketoprofen patch in the treatment of tendinitis: a randomized, double blind, placebo controlled study.". The Journal of rheumatology 32 (8): 1563–70. PMID 16078335. 
  3. ^ Mazières, B (2005). "Topical ketoprofen patch.". Drugs in R&D 6 (6): 337–44. doi:10.2165/00126839-200506060-00003. PMID 16274258. 
  4. ^ a b Sekiya, I; Morito, T; Hara, K; Yamazaki, J; Ju, YJ; Yagishita, K; Mochizuki, T; Tsuji, K et al. (2010). "Ketoprofen Absorption by Muscle and Tendon after Topical or Oral Administration in Patients Undergoing Anterior Cruciate Ligament Reconstruction". AAPS PharmSciTech 11 (1): 154–8. doi:10.1208/s12249-009-9367-2. PMC 2850498. PMID 20087696. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2850498. 
  5. ^ Gayman, MD; Turner, RJ; Cui, M (2008). "Physical Limitations and Depressive Symptoms: Exploring the Nature of the Association". The journals of gerontology. Series B, Psychological sciences and social sciences 63 (4): S219–S228. PMC 2844725. PMID 18689771. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2844725. 
  6. ^ a b Ketoprofen. (n.d.). Millennium Web Catalog. Retrieved February 1, 2010, from http://0-online.lexi.com.library.touro.edu
  7. ^ Lemke TL, Williams DA, Roche VF, Zito SW. Foyes Principles of Medical Chemistry. 6th ed. Philadelphia: Lippincott Williams and Wilkins; 2008.
  8. ^ Ketoprofen. (n.d.). Micromedex. Retrieved February 1, 2010, from https://bb-tuc.touro.edu/webapps/portal/frameset.jsp?tab_id=_102_1
  9. ^ Forney, Barbara C, MS, VMD. Equine Medications, Revised Edition. Blood Horse Publications. Lexington, KY. Copyright 2007.
  10. ^ http://www.birdlife.org/news/news/2009/12/vultures.html
  11. ^ http://www.nature.com/nature/journal/v427/n6975/full/nature02317.html

 
 
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