Rofecoxib is a nonsteroidal antiinflammatory drug (NSAID) that selectively inhibits cyclooxygenase-2 (Cox-2), which was used in the therapy of chronic arthritis and mild-to-moderate musculoskeletal pain. Rofecoxib was withdrawn in 2004 because of an association with an increase in cardiovascular events with its long-term use. Rofecoxib had also been linked transient serum aminotransferase elevations during therapy and too rare instances of idiosyncratic drug-induced liver disease.
Rofecoxib is a synthetic, nonsteroidal derivative of phenyl-furanone with antiinflammatory, antipyretic and analgesic properties and potential antineoplastic properties. Rofecoxib binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in an inhibition of the conversion of arachidonic acid to prostaglandins. COX-related metabolic pathways may represent key regulators of cell proliferation and neo-angiogenesis. Some epithelial tumor cell types overexpress pro-angiogenic COX-2.
Mechanism of Action of Rofecoxib
The anti-inflammatory, analgesic, and antipyretic effects of NSAIDs appear to result from the inhibition of prostaglandin synthesis. Although the exact mechanism of action has not been determined, these effects appear to be mediated through the inhibition of the COX-2 isoenzyme at the sites of inflammation with subsequent reduction in the synthesis of certain prostaglandins from their arachidonic acid precursors. Rofecoxib selectively inhibits the cyclooxygenase-2 (COX-2) enzyme, which is important for the mediation of inflammation and pain. Unlike non-selective NSAIDs, rofecoxib does not inhibit platelet aggregation. It also has little to no affinity for COX-1.
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Rofecoxib is a synthetic, nonsteroidal derivative of phenyl-furanone with antiinflammatory, antipyretic and analgesic properties and potential antineoplastic properties. Rofecoxib binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in an inhibition of the conversion of arachidonic acid to prostaglandins. COX-related metabolic pathways may represent key regulators of cell proliferation and neo-angiogenesis. Some epithelial tumor cell types overexpress pro-angiogenic COX-2. (NCI04)
Indications of Rofecoxib
- Osteoarthritis
- Rheumatoid arthritis
- Ankylosing spondylitis
- Pain due to especially musculoskeletal system
- Lumbago
- Low back pain
- PLID
- Polyarthralgia
- Muscles stiffness in nerve diseases
- Morning stiffness
- For the treatment of osteoarthritis, rheumatoid arthritis, acute pain in adults, and primary dysmenorrhea, as well as acute treatment of migraine attacks with or without auras.
Contra-Indications of Rofecoxib
Allergies to
- Salicylates
- NSAIDs (Non-Steroidal Anti-Inflammatory Drug)
- Cox-2 Inhibitor
- Cox-2 Inhibitor/Nsaid
Side effects of Rofecoxib
- Confusion
- Stomach pain,
- Heartburn,
- GI disorders (e.g. dyspepsia, abdominal pain, nausea, vomiting,diarrheaa, flatulence, constipation, malaena, haematemesis, ulcerative stomatitis, gastritis),indigestion,
Less common
- Acid or sour stomach
- belching
- diarrhea
- heartburn
- indigestion
- nausea
- stomach discomfort, upset, or pain
- vomiting
Rare
- Abdominal or stomach cramping, burning, or tenderness
- back or leg pains
- bleeding gums
- blistering, peeling, or loosening of the skin
- bloody or black, tarry stools
- blue lips and fingernails
- breast enlargement and tenderness
- burning, crawling, itching, numbness, prickling, “pins and needles”, or tingling feelings
- burning upper abdominal or stomach pain
- chest pain, discomfort, or burning
- confusion
- continuing diarrhea
- cough or hoarseness
- coughing that sometimes produces a pink frothy sputum
- cracks in the skin
- dark urine
- decreased appetite
- decreased vision or any change in vision
- depression
- difficult or labored breathing
- dizziness, faintness, or lightheadedness when getting up from a lying or sitting position
- double vision
- dry mouth
- extreme fatigue
- false sense of well-being
- feeling of unreality
- feeling of warmth
- general body swelling
- greatly decreased frequency of urination or amount of urine
- hair loss
- headache
- heavier menstrual periods
- increased hunger
- increased sweating
- jerky movements of the head, face, mouth, and neck
- joint pain
- large, flat, blue or purplish patches in the skin
- large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs
- loss of appetite
- loss of balance control
- loss of bladder control
- loss of consciousness
- loss of hearing
- loss of heat from the body
- lower back or side pain
- mask-like face
- mood swings
- muscle aches, pains, or weakness
- muscle spasm or jerking of all extremities
- numbness or tingling in the hands, feet, or lips
- pain in the ankles or knees
- pain or discomfort in the upper stomach or throat
- pain with swallowing
- painful or difficult urination
- painful, red lumps under the skin, mostly on the legs
- seeing, hearing, or feeling things that are not there
- seizures
- sense of detachment from self or body
- severe constipation
- severe mental changes
- severe or continuing stomach pain
- shuffling walk
- skin rash, hives or welts, itching
- slow, fast, irregular, pounding, or racing heartbeat or pulse
- slowed movements
- slurred speech
- small red or purple spots on the skin
- sore throat
- unexplained weight loss
- unpleasant breath odor
- vaginal bleeding
- vomiting of blood or material that looks like coffee grounds
- weakness in the arms, hands, legs, or feet
- weight gain
- yellow eyes or skin
Symptoms of overdose
- Confusion about identity, place, and time
- severe headache
- unusual drowsiness, dullness, or feeling of sluggishness
More common
- Mild headache
- Continuing ringing or buzzing or other unexplained noise in the ears
- difficulty having a bowel movement (stool)
- discouragement
- feeling sad or empty
- general feeling of discomfort or illness
- hearing loss
- irritability
- loss of interest or pleasure
- sleepiness
- trouble with concentrating
Rare
- Anxiety
- bloated or full feeling
- changes in patterns and rhythms of speech
- excess air or gas in the stomach or intestines
- feeling of constant movement of self or surroundings
- involuntary muscle movements
- lightheadedness
- passing gas
- sensation of spinning
- tiredness
- trouble sleeping
- trouble with speaking
Drug Interactions of Rofecoxib
Rofecoxib may interact with following drugs, suppliments & may change the efficacy of drugs
- aminoglycoside antibiotics (e.g., amikacin, gentamicin, tobramycin)
- angiotensin converting enzyme inhibitors (ACEIs; e.g., captopril, enalapril, ramipril)
- angiotensin receptor blockers (ARBs; e.g., candasartan, irbesartan, losartan)
- beta-adrenergic blockers (e.g., metoprolol, atenolol)
- calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
- celecoxib
- cilostazol
- clopidogrel
- corticosteroids (e.g., dexamethasone, hydrocortisone, prednisone)
- cyclosporine
- diuretics (water pills; e.g., furosemide, hydrochlorothiazide, triamterene)
- 5-ASA medications (e.g., mesalamine, sulfasalazine)
- glucosamine
- haloperidol
- heparin
- methotrexate
- multivitamins
- other non-steroidal anti-inflammatory medications (NSAIDs; e.g., diclofenac, ibuprofen, ketorolac, naproxen)
- Omega-3 fatty acids
- pentoxifylline
- 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., desvenlafaxine, duloxetine, venlafaxine)
- tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
- warfarin
Pregnancy Catagory of Rofecoxib
FDA Pregnancy Catagory C
Pregnancy
In animal studies, pregnant animals were given this medication and had some babies born with problems. No well-controlled studies have been done in humans, though. Therefore, this medication may be used if the potential benefits to the mother outweigh the potential risks to the unborn child.
Lactation
There are no well-controlled studies that have been done in pregnant women. Rofecoxib should be used during pregnancy only if the possible benefit outweighs the possible risk to the unborn baby.
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