Symptomatic treatment of rheumatic diseases, including rheumatoid arthritis and osteoarthritis. Symptomatic treatment of acute inflammation of the musculoskeletal system (tendonitis, injuries). Musculo-muscular pain of moderate to moderate intensity, regardless of origin.
Composition:
1 suppository contains 100 mg ketoprofen.
Action:
A non-steroidal anti-inflammatory drug (phenylpropionic acid derivative) with anti-inflammatory, antipyretic and analgesic effects. The mechanism of action is the inhibition of cyclooxygenase, the enzyme responsible for the synthesis of prostaglandins. It also inhibits platelet aggregation. After rectal administration it reaches a maximum concentration in the blood after 45-60 min. It is 99% bound to plasma proteins. It penetrates into the synovial fluid, periarticular space (joint capsule, synovial membrane, tendon tissue), cerebrospinal fluid and through the placental barrier. It is metabolised in the body by conjugation with glucuronic acid and to a small extent by hydroxylation. Excreted mainly in the form of metabolites in the urine and in a small amount with faeces. T0,5 is approximately 2 hours. In the elderly and in patients with renal impairment, the half-life of the drug is prolonged, plasma and renal clearance are reduced. In patients with hepatic impairment, the plasma clearance and the elimination half-life are not changed, the amount of drug not related to plasma proteins increases about 2-fold.
Contraindications:
Hypersensitivity to the active substance or to any of the excipients. Past hypersensitivity reactions such as bronchospasm, asthma attack, rhinitis, urticaria or other allergic reactions caused by Ketoprofen, salicylates (including acetylsalicylic acid) or other NSAIDs. Active or in a history of gastric or duodenal ulcer, perforation or bleeding. Severe heart failure. Severe hepatic failure. Severe renal failure. Hemorrhagic diathesis. Third trimester of pregnancy. Suppositories are contraindicated in patients with anorexia or anal bleeding.
Precautions:
In patients with bronchial asthma, chronic rhinitis, chronic sinusitis, nasal polyposis, there is an increased risk of NSAID allergy. Caution for patients who are at increased risk of gastrointestinal bleeding and perforation (patients with gastrointestinal disorders, also including: gastroenteritis, ulcerative colitis, Crohn's disease, patients with platelet dysfunction, patients taking anticoagulants or antiaggregating agents, elderly people, people with low body mass) - if ulceration or gastrointestinal bleeding occurs, the drug should be discontinued. Carefully observe patients with photosensitivity or phototoxicity. In patients with heart failure, chronic renal impairment, disturbances in water management (eg dehydrated, postoperative hypovolaemia) - detailed monitoring of diuresis, renal function and circulatory system is recommended. In patients with impaired liver function, transaminase levels should be periodically determined. Due to the increased risk of arterial blockages (eg myocardial infarction, stroke), caution should be used in patients with: uncontrolled hypertension, congestive heart failure, ischemic heart disease, peripheral artery disease, cerebrovascular disease and patients with risk factors for systemic diseases circulation (hypertension, hyperlipidemia, diabetes, smoking). Ketoprofen may mask the symptoms of developing infection. In the case of vision disorders, the drug should be discontinued. The use of ketoprofen in children <15 years is not recommended (safety in this group of patients has not been established).
Pregnancy and lactation:
Ketoprofen should not be used during the first and second trimesters of pregnancy unless clearly necessary. The drug is contraindicated in the third trimester of pregnancy.There is an increased risk of miscarriage, heart defects and exaggeration after the use of prostaglandin synthesis inhibitors in early pregnancy; the total risk of developing cardiovascular malformations increases from less than 1% to about 1.5%; the risk increases with the dose and duration of treatment. If ketoprofen is used in women attempting to become pregnant or in women in the first and second trimester of pregnancy, the drug should be administered in the lowest possible dose for the shortest possible time. Prostaglandin inhibitors used during the third trimester may cause renal dysfunction in the fetus (which may lead to kidney failure with olihydramnios), cardiovascular and pulmonary function (premature closure of the ductus arteriosus and pulmonary hypertension) and expose mother and baby to prolonged bleeding time and inhibition of spasms the uterus. Use during breastfeeding is not recommended. The use of ketoprofen may reduce fertility in women and it is not recommended for women who are planning to get pregnant. For women who have difficulty conceiving or who are being tested for infertility, discontinuation should be considered.
Side effects:
Common: indigestion, nausea, abdominal pain, vomiting. Uncommon: headache, dizziness, drowsiness, constipation, diarrhea, bloating, gastritis, rash, redness, itching, swelling, tiredness. Rare: anemia caused by hemorrhage or bleeding, paresthesia, visual disturbances, tinnitus, dyspnea, asthma attacks, oral mucositis, gastric ulcer, colitis, hepatitis, elevated transaminases, increased bilirubin in blood due to impaired function liver, weight gain. Not known: agranulocytosis, thrombocytopenia, bone marrow depression, anaphylactic reactions (including shock), mood disorder, seizures, dysgeusia, heart failure, hypertension, vasodilatation, bronchospasm (especially in patients with known hypersensitivity to Acetylsalicylic acid or other NSAIDs) , rhinitis, exacerbation of colitis and Crohn's disease, gastrointestinal bleeding, perforation, photosensitivity, alopecia, urticaria, angioneurotic edema, Stevens-Johnson syndrome, toxic necrotic decay of the epidermis, acute renal failure (especially in individuals with existing impaired renal or dehydrated function), tubulointerstitial nephritis, nephrotic syndrome, abnormal renal function tests. Flavor disorders may occur. Clinical and epidemiological studies suggest that the intake of certain NSAIDs (especially long-term at high doses) affects a small increase in the risk of arterial blockages (e.g., myocardial infarction or stroke).
Dosage:
Rectally. In symptomatic long-term treatment: 1 to 2 suppositories a day; in symptomatic short-term treatment of acute conditions: 2 cones per day. The maximum daily dose of ketoprofen is 200 mg - a risk-benefit ratio should be carefully considered before starting treatment with a 200-mg dose, and a higher dose is not recommended.Special groups of patients. In patients with renal insufficiency and in the elderly, it is recommended to reduce the starting dose of ketoprofen and to use the lowest effective doses. In patients with hepatic impairment, the lowest effective doses should be used and the patient monitored. Ketoprofen is not recommended for children <15 years.