Drug information of Ketoprofen

Ketoprofen


Ketoprofen is one of the propionic acid class of nonsteroidal anti-inflammatory drugs with analgesic and antipyretic effects. It acts by inhibiting the body's production of prostaglandin.

Mechanism of effect

Reversibly inhibits cyclooxygenase-1 and 2 (COX-1 and 2) enzymes, which results in decreased formation of prostaglandin precursors; has antipyretic, analgesic, and anti-inflammatory properties

Other proposed mechanisms not fully elucidated (and possibly contributing to the anti-inflammatory effect to varying degrees), include inhibiting chemotaxis, altering lymphocyte activity, inhibiting neutrophil aggregation/activation, and decreasing proinflammatory cytokine levels.

Pharmacokinetics

Metabolism
Hepatic via glucuronidation; metabolite (inactive) can be converted back to parent compound; may have enterohepatic recirculation
Absorption
Almost complete
Excretion
Urine (~80%, primarily as glucuronide conjugates)
Onset of Action
Regular release: <30 minutes
Time to Peak
Regular release: 0.5 to 2 hours; Extended release capsule: 6 to 7 hours; Extended release tablet [Canadian product]: 5 to 6 hours; Enteric coated tablet [Canadian product]: 1 to 2 hours; Rectal suppository [Canadian product]: ~1 hour
Half life
Regular release: 2 to 4 hours; Renal impairment: Mild: 3 hours; moderate to severe: 5 to 9 hours
Enteric coated tablet [Canadian product]: 2 hours
Extended release: ~3 to 7.5 hours
Rectal suppository [Canadian product]: ~2 to 2.5 hours

Drug indications

Osteoarthritis: Management of the signs and symptoms of osteoarthritis
Pain (immediate release only): Management of pain
Primary dysmenorrhea (immediate release only): Treatment of primary dysmenorrhea
4-Rheumatoid arthritis: Management of the signs and symptoms of rheumatoid arthritis

Dosage

Usual Adult Dose for Osteoarthritis
Immediate Release: 50 mg orally 4 times a day or 75 mg orally 3 times a day
Maximum dose: 300 mg/day
Extended Release: 200 mg orally once a day
Maximum dose: 200 mg/day
Usual Adult Dose for Rheumatoid Arthritis
Immediate Release: 50 mg orally 4 times a day or 75 mg orally 3 times a day
Maximum dose: 300 mg/day
Extended Release: 200 mg orally once a day
Maximum dose: 200 mg/day
Usual Adult Dose for Dysmenorrhea
Immediate Release: 25 mg to 50 mg orally every 6 to 8 hours as needed
Maximum dose: 300 mg/day
Usual Adult Dose for Pain
Immediate Release: 25 mg to 50 mg orally every 6 to 8 hours as needed
Maximum dose: 300 mg/day

Drug contraindications

Hypersensitivity to ketoprofen or any component of the formulation; history of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs; use in the setting of CABG surgery
Canadian labeling: Additional contraindications (not in US labeling): Active peptic ulcer or active inflammatory disease of the GI tract; inflammatory lesions or recent bleeding of the rectum or anus (suppository only

Side effects

>10%
Gastrointestinal: Dyspepsia
Hepatic: Abnormal hepatic function tests
1%
 to 10%
Cardiovascular: Peripheral edema
Central nervous system: Headache, dizziness, abnormal dreams, depression, drowsiness, insomnia, malaise, nervousness
Dermatologic: Skin rash
Gastrointestinal: Abdominal pain, constipation, diarrhea, flatulence, nausea, gastrointestinal hemorrhage, peptic ulcer, anorexia, stomatitis, vomiting
Genitourinary: Urinary tract irritation
Ophthalmic: Visual disturbance
Otic: Tinnitus
Renal: Renal insufficiency
<1%, postmarketing, and/or case reports: Acute renal tubular disease, agranulocytosis, allergic rhinitis, alopecia, anaphylaxis, anemia, angioedema, aseptic meningitis, auditory impairment, blurred vision, bone marrow depression, bronchospasm, buccal necrosis, bullous rash, cardiac arrhythmia, cardiac failure, change in libido, chills, cholestatic hepatitis, confusion, conjunctivitis, cystitis, dysphoria, dyspnea, eczema, edema, epistaxis, erythema multiforme, exacerbation of diabetes mellitus, exfoliative dermatitis, facial edema, fluid retention, gastritis, gastrointestinal perforation, gastrointestinal ulcer, gynecomastia, hallucination, hematemesis, hematuria, hemolytic anemia, hemoptysis, hepatic insufficiency, hepatitis, hepatotoxicity (idiosyncratic; Chalasani 2014), hot flash, hypersensitivity reaction, hypertension, hyponatremia, impotence, infection, interstitial nephritis, jaundice, laryngeal edema, leukopenia, melena, microvesicular steatosis, migraine, myocardial infarction, nephrotic syndrome, occult blood in stools, onycholysis, palpitations, pancreatitis, peripheral neuropathy, peripheral vascular disease, polydipsia, polyuria, pruritus, purpura, purpuric rash, renal failure, renal papillary necrosis, retinal hemorrhage, septicemia, shock, skin photosensitivity, Stevens-Johnson syndrome, tachycardia, thrombocytopenia, toxic amblyopia, toxic epidermal necrolysis, ulcerative bowel lesion, ulcerative colitis, urticaria, vasodilation, xerostomia

5-Aminosalicylic Acid Derivatives, Acalabrutinib, Acemetacin, Agents with Antiplatelet Properties (e.g., P2Y12 inhibitors, NSAIDs, SSRIs, etc.), Alcohol (Ethyl), Aliskiren, Bemiparin,
Aminoglycosides, Aminolevulinic Acid (Systemic), Aminolevulinic Acid (Topical), Apixaban,
Angiotensin II Receptor Blockers, Angiotensin-Converting Enzyme Inhibitors, Anticoagulants,
Beta-Blockers, Bile Acid Sequestrants, Bisphosphonate Derivatives, Cephalothin, Collagenase (Systemic), Corticosteroids (Systemic), CycloSPORINE (Systemic), Dabigatran Etexilate, Dasatinib, Deferasirox, Deoxycholic Acid, Desmopressin, Dexibuprofen, Dexketoprofen,
Dichlorphenamide, Diclofenac (Systemic), Digoxin, Drospirenone, Edoxaban, Enoxaparin,
Eplerenone, Fat Emulsion (Fish Oil Based), Felbinac, Floctafenine, Glucosamine, Haloperidol,
Heparin, Herbs (Anticoagulant/Antiplatelet Properties) (eg, Alfalfa, Anise, Bilberry), Herbs (Anticoagulant/Antiplatelet Properties) (eg, Alfalfa, Anise, Bilberry), HydrALAZINE, Ibritumomab Tiuxetan, Ibrutinib, Inotersen, Ketorolac (Nasal), Ketorolac (Systemic), Limaprost, Lithium, Loop Diuretics, Macimorelin, MetFORMIN, Methotrexate, Mifamurtide, Morniflumate, Multivitamins/Fluoride (with ADE), Multivitamins/Minerals (with ADEK, Folate, Iron), Multivitamins/Minerals (with AE, No Iron), Naftazone, Nitisinone, Nonsteroidal Anti-Inflammatory Agents (COX-2 Selective), Obinutuzumab, Omacetaxine, Omega-3 Fatty Acids, Pelubiprofen, Pentosan Polysulfate Sodium, Pentoxifylline, Phenylbutazone, Porfimer, Potassium-Sparing Diuretics, PRALAtrexate, Pretomanid, Probenecid, Prostacyclin Analogues, Prostaglandins (Ophthalmic), Quinolones, Rivaroxaban, Salicylates, Selective Serotonin Reuptake Inhibitors, Serotonin/Norepinephrine Reuptake Inhibitors, Sincalide,
Sodium Phosphates, Tacrolimus (Systemic), Talniflumate, Tenofovir Products, Tenoxicam,
Teriflunomide, Thiazide and Thiazide-Like Diuretics, Thrombolytic Agents, Tipranavir, Tolperisone, Tolvaptan, Tricyclic Antidepressants (Tertiary Amine), Triflusal, Urokinase,
Vancomycin, Verteporfin, Vitamin E (Systemic), Vitamin K Antagonists (eg, warfarin),
Zaltoprofen, Zanubrutinib

Alerts

This medicine may raise the risk of heart and blood vessel problems like heart attack and stroke. These effects can be deadly. The risk may be greater if you have heart disease or risks for heart disease. However, it can also be raised even if you do not have heart disease or risks for heart disease. The risk can happen within the first weeks of using this medicine (ketoprofen capsules) and may be greater with higher doses or long-term use. Do not use this medicine (ketoprofen capsules) right before or after bypass heart surgery

This medicine may raise the chance of severe and sometimes deadly stomach or bowel problems like ulcers or bleeding. The risk is greater in older people, and in people who have had stomach or bowel ulcers or bleeding before. These problems may occur without warning signs


Points of recommendation

What do I need to tell my doctor BEFORE I take Ketoprofen Capsules
If you have an allergy to ketoprofen or any other part of this medicine (ketoprofen capsules
If you have an allergy to aspirin or NSAIDs
If you are allergic to this medicine (ketoprofen capsules); any part of this medicine (ketoprofen capsules); or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had
If you have ever had asthma caused by a salicylate drug like aspirin or a drug like this one like NSAIDs
If you have any of these health problems: GI (gastrointestinal) bleeding or kidney problems
If you have had a recent heart attack
If you are taking any other NSAID, a salicylate drug like aspirin, or pemetrexed
If you are taking probenecid
If you are having trouble getting pregnant or you are having your fertility checked
If you are pregnant or may be pregnant. Do not take this medicine (ketoprofen capsules) if you are in the third trimester of pregnancy. You may also need to avoid this medicine (ketoprofen capsules) at other times during pregnancy. Talk with your doctor to see when you need to avoid taking this medicine (ketoprofen capsules) during pregnancy
If you are breast-feeding. Do not breast-feed while you take this medicine (ketoprofen capsules

High blood pressure has happened with drugs like this one. Have your blood pressure checked as you have been told by your doctor

Very bad and sometimes deadly allergic reactions have rarely happened

Liver problems have happened with drugs like this one. Sometimes, this has been deadly. Call your doctor right away if you have signs of liver problems like dark urine, feeling tired, not hungry, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes

If you are 65 or older, use this medicine (ketoprofen capsules) with care. You could have more side effects

NSAIDs like this medicine (ketoprofen capsules) may affect egg release (ovulation) in women. This may cause you to not be able to get pregnant. This goes back to normal when this medicine (ketoprofen capsules) is stopped

Pregnancy level

B

B; D in late pregnancy because of inhibition of ductus arteriosus closure

Breast feeding warning

unknown whether excreted in breast milk, not recommended.

Drug forms

Orudis

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