Pharmacological action
Uphaxicam is a NSAID, refers to a group oxicams. This medication has anti-inflammatory, analgesic and antipyretic effect.
The mechanism of action associated with inhibition of the enzyme COX, which leads to inhibition of prostaglandin synthesis from arachidonic acid.
Piroxicam inhibits the aggregation of platelets. For systemic use this medicine reduces the pain syndrome.
When Uphaxicam used externally it weakens or suppresses inflammation and joint pain at rest and in motion, reduces morning stiffness and swelling of the joints, increases range of motion.
The analgesic effect occurs within 30 minutes after oral taking. Anti-inflammatory effect manifested by the end of the first week of treatment. After a single dose the effect lasts for 24 hours.
Pharmacokinetics
After oral administration Uphaxicam is well absorbed from the gastrointestinal tract. Cmax in plasma is reached within 3-5 hours.
The proteins plasma binding is 99%. Piroxicam penetrating the placental barrier, excrets in breast milk.
Metabolized in the liver by hydrolysis and conjugation. Piroxicam is excreted unchanged (5%) and in the form of metabolites, which are displayed in the kidneys and in small amounts in feces. T1/2 is approximately 50 hours.
In patients with liver diseases T1/2 may increases.
Why is Uphaxicam prescribed?
For systemic and topical use: articular syndrome (rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout), back pain, neuralgia, myalgia, traumatic inflammation of the soft tissue and musculoskeletal system.
For systemic use: dysmenorrhea in patients older than 12 years, acute infectious-inflammatory diseases of upper respiratory tract.
Dosage and administration
For oral administration the dosage is 10-30 mg 1 time / day. Rectal - 20-40 mg 1-2 times / day. In acute gout, the initial dose is 40 mg 1 time / day in the first 2 days, then 40 mg 1 time per day or 20 mg 2 times / day for 4-6 days. In acute conditions or exacerbation of a chronic process you can enter IM at a dose of 20-40 mg 1 time / day. After the relief of acute process of switching to maintenance therapy with oral forms.
Externally this medicine is applied 3-4 times / day.
Uphaxicam side effects, adverse reactions
Digestive system: common - nausea, anorexia, stomatitis, epigastric pain, diarrhea or constipation, bloating, bleeding gums (due to the inhibition of platelet aggregation); in rare cases - erosive and ulcerative lesions of the gastrointestinal tract, with possible bleeding and perforation, transient elevation of liver enzymes, jaundice and hepatic necrosis with fatal consequences. Typically these side effects develop with chronic administration at doses exceeding 30 mg / day.
Hematopoietic system: anemia (rarely aplastic anemia or hemolytic anemia), thrombocytopenia, leukopenia, eosinophilia.
CNS and peripheral nervous system: possible dizziness, headache, drowsiness, sleep disturbances, depression, anxiety, hallucinations, mood changes, weakness, disturbances of sensitivity, swelling of the eyes, blurred vision, and signs of eye irritation.
Metabolism: rarely - hyperkalemia, hypo- or hyperglycemia, changes in body weight, in some cases - a transient increase of residual nitrogen and creatinine, uremia with hyperkalemia.
Urinary system: acute renal failure (with symptoms of hemorrhagic vasculitis), acute interstitial nephritis.
Allergic reactions: possible itching, redness, rash, pemphigus vulgaris, allergic swelling of face and hands; in some cases - Stevens-Johnson syndrome, Lyell's syndrome; in rare cases - anaphylactic reactions, bronchospasm, urticaria, angioedema, vasculitis, serum sickness.
Dermatological reactions: rarely - photosensitivity, rarely - onycholysis, alopecia.
Other: possible nosebleeds.
Local reaction: possible irritation of the rectum, tenesmus.
For external use: rarely - erythema and itching at the site of application.
Uphaxicam contraindications
Erosive and ulcerative lesions of the gastrointestinal tract in acute phase, indications in a history to bronchial asthma in connection with the use of NSAIDs, violations of porphyrin metabolism, expressed by human liver and kidney failure, pregnancy, lactation, children under the age of 14 years, proctitis (rectal use), increased sensitivity to piroxicam.
Using during pregnancy and breastfeeding
Uphaxicam is contraindicated for use in the III trimester of pregnancy. If necessary to use this drug in the I and II trimesters of pregnancy should be related to the expected benefit to the mother and the potential risk to the fetus, due to lack of reliable clinical evidence supporting the safety of piroxicam in this period.
Piroxicam is excreted in breast milk. If necessary to use this medication during lactation should solve the issue of termination of breastfeeding. Category effects on the fetus by FDA - C.
Special instructions
With caution use Uphaxicam if erosive and ulcerative lesions and bleeding from the gastrointestinal tract in history, dyspeptic symptoms of chronic heart failure, hepatic dysfunction and kidney failure, asthma, coagulation disorders, and concomitant administration of oral anticoagulants, allergic reactions to acetylsalicylic acid and other NSAIDs in history.
In the course of treatment is necessary to monitor the functional state of the liver and peripheral blood picture. This medicine should not be used topically in violation of the integrity of the skin.
Must avoid contact with eyes or mucous membranes.
Not recommended for use while piroxicam and acetylsalicylic acid and other NSAIDs.
Uphaxicam drug interactions
This medication Displaces from its association with blood proteins other drugs; reduces the effectiveness of antihypertensive drugs. Compared to other NSAIDs and corticosteroids Uphaxicam increases the risk of ulcerogenic action. This drug increases the risk of hyperkalemia when combined with potassium-sparing potassium-based diuretics and other drugs; increases the concentration of phenytoin and lithium in the blood. Anticoagulants increase the risk of bleeding. Aspirin reduces the concentration of piroxicam in the blood up to 80% of the original.
Uphaxicam in case of emergency / overdose
Symptoms: drowsiness, blurred vision, at very high doses - loss of consciousness, coma.
Treatment: gastric lavage, taking activated charcoal, antacids (to reduce the intake), symptomatic therapy.
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