Composition and dosage forms
Ortofen contains one active substance - diclofenac, which has a pronounced analgesic, anti-inflammatory and moderate antipyretic effect. The drug has several forms of release for systemic and local use:
- tablets: white, flat-cylindrical, with a dosage of 25 mg, auxiliary components: povidone, starch, magnesium stearate and others;
- gel: a clear, slightly viscous liquid containing 5% diclofenac, packaged in 100 ml bottles, containing water, ethyl alcohol, propylene glycol and other binders;
- Ortofen ointment: 20% preparation in the form of a homogeneous viscous mass, available in tubes of 30 and 50 ml;
- water-based injection solution: liquid in 3 ml ampoules containing 25 mg. diclofenac in 1 ml.
How does Ortofen work?
The mechanism of action of all forms of the drug is determined by the non-steroidal anti-inflammatory active component they contain. The injection solution and tablets have a systemic effect, relieve symptoms of fever and acute pain. Diclofenac indiscriminately inhibits the activity of pain and inflammatory prostaglandins, has an antiplatelet property - it increases blood flow. After administration intramuscularly or orally, the medicine is distributed in all fluids and tissues of the body. The liver and kidneys take part in the transformation and filtration of drug metabolites.
Topical preparations: Ortofen ointment and gel have moderate analgesic properties and are used to reduce pain in muscles and joints. Part of the drug is absorbed orally through the skin. With prolonged use, the active substance may accumulate in the blood and affect the tissues of internal organs.
Ortofen
Ortofen (INN - diclofenac) is a domestic answer to the foreign “branded” voltaren. This non-steroidal anti-inflammatory drug has been used in clinical practice for more than three decades, which was enough for it not only to gain a place in the sun, but also to usurp the actual leadership in the number of medical prescriptions among other NSAIDs. Ortofen has a pronounced anti-inflammatory and analgesic, as well as a moderate antipyretic (antipyretic) effect. The mechanism of action of the drug is due to the suppression of the activity of the enzyme cyclooxygenase (COX), which is involved in the synthesis of mediators of inflammation and pain, prostaglandins. The analgesic effect is associated with the suppression of prostaglandin production in the central nervous system and peripheral nerve fibers. For diseases of a rheumatic nature, ortofen relieves joint pain during movement and at rest, relieves morning stiffness and swelling of the joints, and liberates movements. The drug reduces pain after injuries and operations, reduces swelling of damaged tissue areas. Ortofen has a moderate antiplatelet effect, preventing platelet aggregation.
When administered orally, Orofen is quickly absorbed from the gastrointestinal tract. In this case, food intake inhibits the rate of absorption, but not its completeness. The maximum concentration of the active substance in the blood plasma when taking tablets is observed after 2-4 hours, when administered by injection - after 20 minutes. Ortofen is available in the following dosage forms: tablets, injection solution, ointment and gel. A single dose of tablet form is 25-50 mg for 2-3 doses. The maximum daily dose should not exceed 150 mg. For the treatment of acute conditions or relief of severe pain, a single injection of 75 mg of the substance is allowed. In children over 6 years of age, the daily dose depends on body weight and is 2 mg per 1 kg. Apply 2-4 g of ointment or gel locally (depending on the affected area) 3-4 times a day. A history of allergy to NSAIDs practically excludes the use of ortofen in this patient. When taking the drug, experts recommend constantly monitoring laboratory blood counts, incl. markers of normal functioning of the liver and kidneys. During treatment with Ortofen you should not drink alcohol.
Indications for use of Ortofen
The drug is prescribed for moderate to severe pain of various origins, which accompanies injuries, degenerative processes, and inflammatory pathologies. Main area of application: diseases of the joints and muscular system:
- myositis;
- arthritis, arthrosis deformans, spondyloarthrosis;
- tendinitis, sprains and ligament ruptures;
- neuralgic pain;
- rheumatic symptoms;
- lumbago, sciatica, bursitis.
Ortofen helps eliminate pain in intense infectious pathologies, diseases of internal organs and the central nervous system. Including:
- for migraine, tension headache;
- toothache;
- for gynecological pathologies;
- for renal colic;
- for bruises, dislocations.
The antipyretic effect of Ortofen is less pronounced than the analgesic and anti-inflammatory effect, therefore, at high temperatures it is recommended to use other types of NSAIDs.
Diclofenac (ortofen)
From the gastrointestinal tract:
more often than 1% - abdominal pain or spasm, feeling of bloating, diarrhea, nausea, constipation, flatulence, increased activity of liver transaminases, peptic ulcer with possible complications (bleeding, perforation), gastrointestinal bleeding without ulcer; less than 1% - vomiting, jaundice, melena, blood in the stool, damage to the esophagus, aphthous stomatitis, dry mucous membranes (including the oral cavity), hepatitis (possibly fulminant), liver necrosis, cirrhosis, hepatorenal syndrome, changes in appetite, pancreatitis (including with concomitant hepatitis), cholecystopancreatitis, colitis.
From the nervous system:
more often 1% - headache, dizziness; less than 1% - sleep disturbance, drowsiness, depression, irritability, aseptic meningitis (more often in patients with systemic lupus erythematosus and other systemic connective tissue diseases), convulsions, general weakness, disorientation, nightmares, a feeling of fear.
From the senses:
more often 1% - tinnitus; less than 1% - blurred visual perception, diplopia, taste disturbance, reversible or irreversible hearing loss, scotoma.
From the skin:
more often 1% - skin itching, skin rash; less than 1% - alopecia, urticaria, eczema, toxic dermatitis, exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), increased photosensitivity, pinpoint hemorrhages.
From the genitourinary system:
more often 1% - fluid retention; less than 1% - nephrotic syndrome, proteinuria, oliguria, hematuria, interstitial nephritis, papillary necrosis, acute renal failure, azotemia.
From the hematopoietic organs and immune system:
less than 1% - anemia (including hemolytic and aplastic anemia), leukopenia, thrombocytopenia, eosinophilia, agranulocytosis, thrombocytopenic purpura, worsening of infectious processes (including the development of necrotizing fasciitis).
From the respiratory system:
less than 1% - cough, bronchospasm, laryngeal edema, pneumonitis.
From the cardiovascular system:
less often 1% - increased blood pressure; congestive heart failure, extrasystole, chest pain.
Allergic reactions:
less than 1% - anaphylactoid reactions, anaphylactic shock (usually develops rapidly), swelling of the lips and tongue, allergic vasculitis.
Contraindications and side effects
The drug is not applicable for cases of high sensitivity to salicylates, inflammatory and erosive lesions of the digestive tract mucosa, severe liver and urinary tract diseases. Contraindications also include:
- tendency to internal bleeding, decreased blood clotting;
- Iron-deficiency anemia;
- pregnancy at all stages;
- breastfeeding period.
Ortofen is also prohibited for the treatment of children under 6 years of age. An extensive list of contraindications is explained by high toxicity. Various undesirable reactions are possible against the background of its use:
- loss of appetite, change in taste, pain in the epigastrium, abdominal cavity, exacerbation of gastritis and gastrointestinal pathologies, diarrhea;
- kidney inflammation, impaired diuresis;
- dizziness, asthenic syndrome, insomnia;
- drug hepatosis.
Ortofen should be used with caution in diseases of the heart and blood vessels, bronchial asthma, and diabetes mellitus. Possible signs of a drug overdose: severe headache, vomiting, loss of coordination of movements, deterioration of hearing and vision.
Ortofen ointment for external use 2% 30g
Compound
Active substance: diclofenac sodium - 2 g;
Excipients: benzyl benzoate (medical benzyl benzoate) - 6 g; polysorbate-80 - 1 g; methyl parahydroxybenzoate (methylparaben, nipagin) - 0.08 g; propyl parahydroxybenzoate (propylparaben, nipazole) - 0.02 g; carbomer (carbomer 940) - 0.75 g; trolamine (thermostable triethanolamine) - 0.4 g; purified water - up to 100 g.
Pharmacokinetics
With the recommended method of application of the drug, systemic absorption of diclofenac is no more than 6%. Bonding with plasma proteins is 99.7%. Excreted by the kidneys. Diclofenac is predominantly distributed and retained deep in tissues affected by inflammation. When applying the drug to the area of the affected joint, the concentration of diclofenac in the synovial fluid is higher than in the blood plasma.
Indications for use
The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease.
- Post-traumatic inflammation of soft tissues and joints, for example, as a result of sprains and bruises;
- rheumatic diseases of soft tissues (tenosynovitis, bursitis, damage to periarticular tissues):
- pain and swelling associated with diseases of muscles and joints (rheumatoid arthritis, osteoarthritis, radiculitis, lumbago, sciatica, muscle pain of rheumatic and non-rheumatic origin).
Contraindications
- Hypersensitivity to diclofenac or any of the components included in the drug;
- complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including a history);
- pregnancy (III trimester);
- breastfeeding period;
- age up to 12 years;
- violation of the integrity of the skin at the intended site of application.
With caution: Hepatic porphyria (exacerbation), erosive and ulcerative lesions of the gastrointestinal tract, severe dysfunction of the liver and kidneys, chronic heart failure, bleeding disorders (including hemophilia, prolongation of bleeding time, tendency to bleed), advanced age, bronchial asthma, pregnancy (I and II trimester).
Directions for use and doses
For external use only. For adults and children over 12 years of age, the drug is applied 2 times a day (every 12 hours, preferably morning and evening), lightly rubbing into the skin. The required amount of the drug depends on the size of the painful area. A single dose of the drug is 2-4 g (in volume comparable to the size of a cherry or hazelnut, respectively), which is enough to treat an area of 400-800 cm2. If the hands are not the area where pain is localized, then after applying the drug they must be washed. The maximum daily dose of the drug is 8 g.
The duration of treatment depends on the indications and the observed effect. The drug should not be changed for more than 14 days for post-traumatic inflammation and rheumatic diseases of soft tissues without a doctor’s recommendation. If after 7 days of use the therapeutic effect is not observed or the condition worsens, you should consult a doctor.
Storage conditions
At a temperature not higher than 25 °C. Keep out of the reach of children.
Best before date
2 years 6 months Do not use after expiration date.
special instructions
The drug should be applied only to intact skin, avoiding contact with open wounds. The drug should not come into contact with the mouth, eyes or mucous membranes. After applying the drug, a bandage may be applied, but airtight occlusive dressings should not be applied. Avoid excessive exposure to sunlight on the area of application of the drug. If side effects occur, you should stop using the drug and consult a doctor.
Description
Non-steroidal anti-inflammatory drug (NSAID).
Pharmacodynamics
Non-steroidal anti-inflammatory drug for external use. Diclofenac has a pronounced analgesic and anti-inflammatory effect. Indiscriminately inhibiting cyclooxygenase types 1 and 2 (COX-1 and COX-2), it disrupts the metabolism of arachidonic acid and the synthesis of prostaglandins, which are the main link in the development of inflammation.
Diclofenac is used to eliminate pain and reduce swelling associated with the inflammatory process.
Side effects
Classification of the frequency of side effects according to the recommendations of the World Health Organization (WHO): very often >1/10; often from > 1/100 to < 1/10; infrequently from > 1/1000 to < 1/100; rarely from > 1/10000 to < 1/1000; very rarely <1/10000, including isolated reports; frequency unknown - based on available data, it is not possible to determine the frequency of occurrence.
From the immune system: very rarely - generalized skin rash, allergic reactions (urticaria, hypersensitivity: angioedema).
From the respiratory system and organs of the chest and mediastinum: very rarely - attacks of suffocation, bronchospastic reactions.
From the skin: often - erythema, dermatitis, including contact dermatitis (symptoms: eczema, itching, swelling of the treated skin area, rash, papules, vesicles, peeling); rarely - bullous dermatitis; very rarely - photosensitivity reactions, pustular rashes.
Use during pregnancy and breastfeeding
The use of the drug during the first and second trimesters of pregnancy is recommended only as prescribed by a doctor, weighing the benefits for the mother and the risk for the fetus. The drug is contraindicated in the third trimester of pregnancy due to the possibility of decreased uterine tone and/or premature closure of the fetal ductus arteriosus. Due to the lack of data on the penetration of diclofenac into breast milk, the drug is not recommended for use during breastfeeding.
Interaction
Diclofenac may enhance the effect of drugs that cause photosensitivity. Clinically significant interactions with other drugs have not been described.
Overdose
Symptoms
Due to low systemic absorption when used externally, overdose is unlikely. In case of accidental ingestion, systemic adverse reactions may develop.
Treatment
In case of accidental ingestion - gastric lavage (only within an hour after accidental ingestion), induction of vomiting, intake of activated charcoal, symptomatic therapy. Dialysis and forced diuresis are not effective due to the high degree of binding of diclofenac to plasma proteins (about 99%).
Impact on the ability to drive vehicles and operate machinery
The drug does not affect the ability to drive vehicles and machinery.
Application: instructions
Ortofen tablets are taken in one or several doses per day:
- 1 tablet once and up to 3-4 times a day, after eating food or simultaneously with it, the maximum amount of the product is 150 mg;
- in case of severe pain, from the second day of therapy it is recommended to reduce the number of tablets to 2-3 pieces in order to avoid undesirable consequences for the body;
- It is not recommended to take tablets for more than 5 days in a row.
Ortofen injections are indicated intramuscularly. They are administered once, in a dose of no more than 75 mg. active substance. After a single injection, therapy should be continued by taking the drug in tablets.
Gel and ointment are used externally, treating the surface of the skin in the area of damage or inflammation of the joint. The product in an amount of 2–3 g is applied to clean surfaces, rubbing until the medicine is completely absorbed. If necessary, wrap part of the body in warmth. It is recommended to use Ortofen ointment at night or at rest. It is allowed to use up to 8 g of a topical drug per day without health consequences.
Important: when using both systemic and external forms of the medication, you must take into account its total amount when discussing it with your doctor.
When using injections and tablets, you must avoid other NSAIDs and carefully check the dosage of anticoagulants and glucocorticoids, as they increase the toxicity of Ortofen.