Ketoprofen; Uses, Dosage, Side Effects, Interactions

Ketoprofen is a propionic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic and antipyretic effects. Ketoprofeninhibits the activity of the enzymes cyclo-oxygenase I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes. The resulting decrease in prostaglandin synthesis, by prostaglandin synthase, is responsible for the therapeutic effects of ibuprofen. Ketoprofen also causes a decrease in the formation of thromboxane A2 synthesis, by thromboxane synthase, thereby inhibiting platelet aggregation.

Ketoprofen is a nonsteroidal anti-inflammatory agent (NSAID) with analgesic and antipyretic properties. Ketoprofen has pharmacologic actions similar to those of other prototypical NSAIDs, which inhibit prostaglandin synthesis. Ketoprofen is used to treat rheumatoid arthritis, osteoarthritis, dysmenorrhea, and alleviate moderate pain.

Mechanism of action of Ketoprofen

The anti-inflammatory effects of ketoprofen are believed to be due to inhibition cyclooxygenase-2 (COX-2), an enzyme involved in prostaglandin synthesis via the arachidonic acid pathway. This results in decreased levels of prostaglandins that mediate pain, fever, and inflammation. Ketoprofen is a non-specific cyclooxygenase inhibitor and inhibition of COX-1 is thought to confer some of its side effects, such as GI upset and ulceration. Ketoprofen is thought to have anti-bradykinin activity, as well as lysosomal membrane-stabilizing action. Antipyretic effects may be due to action on the hypothalamus, resulting in increased peripheral blood flow, vasodilation, and subsequent heat dissipation.

Indications of Ketoprofen

• Ankylosing Spondylitis
• Migraines
• Rheumatoid arthritis
• Osteoarthritis
• Acute and chronic rheumatoid arthritis,
• Primary dysmenorrhea
• Mild to moderate pain associated with musculotendinous trauma (sprains and strains),
• Postoperative (including dental surgery)
• Postpartum pain.
• Treatment of some pain, especially nerve pain such as
• Sciatica,
• Postherpetic neuralgia
• Referred pain for radiculopathy.

Contra-Indications of Ketoprofen

• Systemic mastocytosis
• Increased risk of bleeding due to clotting disorder
• Alcoholism
• High blood pressure
• Chronic heart failure
• Disease of the heart and blood vessels
• Stroke
• Ulcer from stomach acid
• Stomach or intestinal ulcer
• Liver problems
• Bleeding of the stomach or intestines
• Kidney stone
• Systemic lupus erythematosus
• Visible water retention
• A mother who is producing milk and breastfeeding
• A rupture in the wall of the stomach or intestine
• Increased cardiovascular event risk
• The time immediately after coronary bypass surgery
• chronic kidney disease stage 4 (severe)

Dosages of Ketoprofen

Strengths: 12.5 mg; 25 mg; 50 mg; 75 mg;  100 mg; 150 mg; 200 mg;

 Osteoarthritis

• Adults—At first, 75 milligrams (mg) three times a day or 50 mg four times a day. Your doctor may increase your dose, if necessary, up to a total of 300 mg a day.
• Children—Use and dose must be determined by your doctor.

Mild to moderate pain or menstrual cramps

• Adults—25 to 50 mg every six to eight hours as needed. Some people may need to take as much as 75 mg every six to eight hours. Doses larger than 75 mg are not likely to give better relief.

Osteoarthritis and rheumatoid arthritis

• For oral dosage form (extended-release capsules):
• Adults—200 mg once a day, in the morning or evening. Take the medicine at the same time every day.

Dysmenorrhea

• Immediate Release: 25 mg to 50 mg orally every 6 to 8 hours as needed
• Maximum dose: 300 mg/day

Side Effects of Ketoprofen

The common

• stomach pain
• abdominal or stomach pain, cramping, or burning (severe)
• bloody or black, tarry stools
• blurred vision or any change in vision
• chest pain
• convulsions (seizures)
• fast or irregular breathing
• fast, irregular heartbeat or pulse
• indigestion
• nausea, vomiting
• diarrhea

More common

• Acid or sour stomach
• constipation
• headache
• heartburn
• nausea or vomiting
• skin rash
• stomach pain
• constipation
• gas
• rash

Less common

• Excess air or gas in the stomach or intestines
• itching skin
• passing gas
• stomach cramps
• swelling
• weight loss
• diarrhea
• indigestion or heartburn
• nausea
• dizziness
• headache
• itching or rash

Rare

• Anxiety
• change in vision
• seizures
• abnormal or fast heart rate
• weight loss
• chest pain or tightness
• confusion
• cough
• Agitation
• arm, back, or jaw pain
• blurred vision
• chest pain or discomfort
• convulsions
• extra heartbeats
• hallucinations
• headache
• irritability
• muscle pain or cramps
• pale or yellowed skin, dark colored urine, fever, confusion or weakness;
• jaundice (yellowing of the skin or eyes);
• sore throat, and headache with a severe blistering, peeling, and red skin rash;
• swelling, rapid weight gain, feeling short of breath (even with mild exertion); or
• increased thirst, loss of appetite, urinating less than usual or not at all.

Drug Interactions of Ketoprofen 

Ketoprofen may interact with following drugs, supplements & may change the efficacy of drugs

• aminoglycoside antibiotics (e.g., amikacin, gentamicin, tobramycin)
• angiotensin-converting enzyme (ACE) inhibitors (e.g., ramipril, enalapril, captopril, quinapril)
• angiotensin receptor blockers (ARBs; e.g., candesartan, irbesartan, losartan)
• “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
• beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
• bisphosphonates (e.g., alendronate, etidronate)
• carbamazepine
• celecoxib
• cilostazol
• clopidogrel
• cyclosporine
• dabigatran
• dasatinib
• diuretics (water pills; e.g., furosemide, hydrochlorothiazide, triamterene)
• fluvastatin
• haloperidol
• heparin
• ibrutinib
• methotrexate
• multivitamins (with vitamins A, E) with or without minerals
• nilotinib
• non-steroidal anti-inflammatory medications (NSAIDs; e.g., diclofenac, ibuprofen, naproxen)
• omega-3 fatty acids
• omeprazole
• oral corticosteroids (e.g., dexamethasone, hydrocortisone, prednisone)
• pentoxifylline
• phenobarbital
• phenytoin
• quinolone antibiotics (e.g., ciprofloxacin, norfloxacin, ofloxacin)
• selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine, paroxetine, sertraline)
• serotonin/norepinephrine reuptake inhibitors (SNRIs; e.g.,  duloxetine, venlafaxine)
• sulfasalazine
• tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)

Pregnancy & Lactation of Ketoprofen 

FDA  Pregnancy Category C

Pregnancy

This medication should not be used during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding

This medication should not be used by women who are breast-feeding

References