Ketoprofen

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Ketoprofen (Brand names: Fastum, Orudis, Oruvail, Profenid...) is a NSAID with analgesic and antipyretic properties indicated for the management of the signs and symptoms of rheumatoid arthritis and osteoarthritis and for the treatment of acute pain.

Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Ketoprofen.jpg

[edit] MECHANISM OF ACTION

Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties.

ketoprofen acts by inhibiting cyclooxygenase-1 and -2 (COX-1 and COX-2) enzymes reversibly, which decreases production of proinflammatory prostaglandin precursors.

Metabolism:
Ketoprofen is biotransformed according to two processes: one minor (hydroxylation), and one major pathway (glucuronic acid conjugation). Plasma elimination half-life is 1.5 to 2 hours for the oral route.

Distribution:

  • Ketoprofen is 99% bound to plasma proteins.
  • Ketoprofen enters the synovial fluid and remains at levels above serum concentrations after the 4th hour following oral intake.
  • It crosses the placental and blood brain barriers.

[edit] INDICATIONS

  • Orally:
    • management of the signs and symptoms (swelling, redness and soreness) of rheumatoid arthritis and osteoarthritis.
    • treatment of acute pain (musculoskeletal pain, dental pain, headache, primary dysmenorrhea (painful periods), nerve pain such as sciatica and postherpetic neuralgia)


  • Topical plasters and gel
    • Treatment of musculoskeletal pain

[edit] DOSAGE

Oral route:

  • Normal oral forms:
    • mild-to-moderate pain and dysmenorrhea: The usual recommended dose is 25 to 50 mg every 6 to 8 hours as necessary
    • Rheumatoid Arthritis And Osteoarthritis: The recommended starting dose in otherwise healthy patients is 75 mg three times or 50 mg four times a day.
  • Slow Release (SR): The usual dose for Rheumatoid Arthritis And Osteoarthritis is 100mg to 200mg taken once a day

[edit] CONTRAINDICATIONS

Ketoprofen is contraindicated in patients with a history of hypersensitivity to ketoprofen or any of the components of the formula as well as in patients with a history of hypersensitivity to aspirin or other NSAIDs, such as attacks of asthma or other allergic reactions. Anaphylactic reactions have been reported serious and rarely fatal in these patients.

Ketoprofen is also contraindicated in the following cases:

  • Active peptic ulcer.
  • Severe liver failure.
  • Severe renal impairment.
  • Severe heart failure, uncontrolled.
  • Third trimester of pregnancy.

[edit] PRECAUTIONS

  • At the start of treatment, careful monitoring of urine volume and kidney function in heart failure, cirrhotic and nephrotic patients, patients treated with diuretics, patients with chronic renal failure and particular elderly subjects.
  • The use of NSAIDs may impair female fertility and is not recommended in women attempting to conceive. In women who have difficulties conceiving or who are undergoing investigation of infertility, withdrawal of the NSAID should be considered.
  • Ketoprofen should be administered with care and closely monitored in patients with history of gastrointestinal disorders (peptic ulcer, ulcerative colitis, Crohn’s disease) as their condition may be axacerbated.
  • Patients with history of photosensitivity or phototoxicity reactions must be closely monitored.

[edit] INTERACTIONS

Coprescriptions to be avoided:

  • Warfarin, aspirin, heparin, Ticlopidine and clopidogrel: increased risk of haemorrhage.
  • Lithium: raised serum lithium levels.
  • Methotrexate at doses greater than 15mg/week: increased haematological toxicity.
  • Other NSAIDs or corticosteroids: Increased risk of ulcer and haemorrhage.

[edit] PREGNANCY AND LACTATION

Pregnancy Category C (US). Because of the known effects of nonsteroidal anti-inflammatory drugs on the fetal cardiovascular system (closure of ductus arteriosus), use during pregnancy (particularly late pregnancy) should be avoided

Nursing Mothers: ketoprofen is not recommended for use in nursing mothers.

[edit] SIDE EFFECTS

Adverse reactions:[1]


Incidence Greater than 1% (Probable Causal Relationship) Less than 1% (Probable Causal Relationship) Less than 1% (Causal Relationship Unknown)
Body as a Whole
  • Chills
  • facial edema
  • infection
  • pain
  • allergic reaction
  • anaphylaxis.
  • Septicemia
  • shock.
Hemic
  • Hypocoagulability
  • agranulocytosis
  • anemia
  • hemolysis
  • purpura
  • thrombocytopenia.


Nervous System
  • Headache
  • Dizziness
  • CNS inhibition (i.e. pooled reports of somnolence malaise)
  • CNS excitation (i.e. insomnia nervousness dreams etc.)
  • Amnesia
  • confusion
  • impotence
  • migraine
  • paresthesia
  • vertigo.
  • Dysphoria
  • hallucination
  • libido disturbance
  • nightmares
  • personality disorder
  • aseptic meningitis.
Skin and Appendages
  • Rash
  • Alopecia
  • eczema
  • pruritus
  • purpuric rash
  • sweating
  • urticaria
  • bullous rash
  • exfoliative dermatitis
  • photosensitivity
  • skin discoloration
  • onycholysis
  • toxic epidermal necrolysis
  • erythema multiforme
  • Stevens-Johnson Syndrome.
Urogenital
  • Impairment of renal function (edema increased BUN)
  • Signs or symptoms of urinary-tract irritation.


  • Menometrorrhagia
  • hematuria
  • renal failure
  • interstitial nephritis
  • nephrotic syndrome.
  • Acute tubulopathy
  • gynecomastia.
Endocrine
  • Diabetes mellitus (aggravated).
Cardiovascular
  • Hypertension
  • palpitation
  • tachycardia
  • congestive heart failure
  • peripheral vascular disease
  • vasodilation.
  • Arrhythmias
  • myocardial infarction.
Special Senses
  • Tinnitus
  • Visual disturbance.
  • Conjunctivitis
  • conjunctivitis sicca
  • eye pain
  • hearing impairment
  • retinal hemorrhage and pigmentation change
  • taste perversion.


Metabolic and Nutritional
  • Thirst
  • weight gain
  • weight loss
  • hyponatremia.

Musculoskeletal
  • Myalgia

Respiratory
  • Dyspnea
  • hemoptysis
  • epistaxis
  • pharyngitis
  • rhinitis
  • bronchospasm
  • laryngeal edema.


Digestive
  • Dyspepsia (11%)
  • Nausea (3% to 9%)
  • Abdominal pain (3% to 9%)
  • Vomiting
  • Diarrhea (3% to 9%)
  • Constipation (3% to 9%)
  • Flatulence (3% to 9%)
  • Anorexia
  • Stomatitis
  • Appetite increased
  • dry mouth
  • eructation
  • gastritis
  • rectal hemorrhage
  • melena
  • fecal occult blood
  • salivation
  • peptic ulcer
  • gastrointestinal perforation
  • hematemesis
  • intestinal ulceration
  • hepatic dysfunction
  • hepatitis
  • cholestatic hepatitis
  • jaundice.
  • Buccal necrosis
  • ulcerative colitis
  • microvesicular steatosis
  • pancreatitis.

[edit] RELATED LINKS

NSAIDs: MOAs and Clinical Considerations

[edit] BIBLIOGRAPHY

[edit] REFERENCES

  1. http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9bc31f67-cfce-4ad6-9c07-3845ead3542c
Non-steroidal anti-inflammatory drugs (NSAIDs)
Non-selective (COX-1 and COX-2 inhibitors) Aceclofenac   Acetylsalicylic acid   Benzydamine   Diclofenac   Flurbiprofen   Ibuprofen   Indometacin   Ketoprofen   Ketorolac   Ketorolac   Lornoxicam   Mefenamic acid   Morniflumate   Nabumetone   Naproxen   Niflumic acid   Piroxicam   Tenoxicam
Relatively COX-2 selective Meloxicam   Nimesulide
COX-2 selective inhibitors (Coxibs) Celecoxib   Etoricoxib   Parecoxib
Ophthalmic NSAIDs Bromfenac (ophthalmic)   Diclofenac (ophthalmic)   Flurbiprofen (ophthalmic)   Ketorolac (ophthalmic)   Nepafenac (ophthalmic)
Veterinary use Carprofen   Deracoxib   Firocoxib   Mavacoxib   Robenacoxib