Active material: Diclofenac
When ATH: M01AB05
CCF: NSAIDs
ICD-10 codes (testimony): G43, H66, J02, J03, J06.9, J10, K08.8, K80, M25.5, M54, M54.3, M54.4, M65, M70, M71, M79.1, M79.2, N23, N70, N71, N72, N94.4, R07, R50, R51, R52.0, R52.2
When CSF: 05.01.01.03.01
Manufacturer: HEMOFARM A.D. (Serbia)
◊ Pills, sugar-coated of red color, with small inclusions of a lighter color, round, lenticular.
| 1 tab. | |
| diclofenac potassium | 12.5 mg |
Excipients: calcium hydrogen phosphate, corn starch, sodium carboxymethyl starch (Type A), Colloidal anhydrous silica, povidone 30, magnesium stearate.
Ingredients sugar shell: sucrose, talc, carmine dye Ponce (E124), acacia gum, povidone 25, Titanium dioxide (E171), macrogol 6000.
10 PC. – блистеры (1) – пачки картонные.
Pills, coated of red color, with small inclusions of a lighter color, round, lenticular.
| 1 tab. | |
| diclofenac potassium | 50 mg |
Excipients: Colloidal anhydrous silica, calcium hydrogen phosphate, anhydrous, corn starch, povidone K30, magnesium stearate, sodium carboxymethyl starch, gummiaraʙik, sucrose , sucrose powder, talc, cochineal red varnish (E124), povidone K25, macrogol 6000.
10 PC. – блистеры (1) – пачки картонные.
NSAIDs. Has a pronounced anti-inflammatory, analgesic and antipyretic effect, which is caused by inhibition of prostaglandin synthesis due to inhibition of the activity of COX-1 and COX-2.
Considering that, that diclofenac potassium is very quickly absorbed from the gastrointestinal tract, Rapten Rapid is most effective in the treatment of acute pain and inflammatory conditions, in which a quick initial effect is most important.
The analgesic and antipyretic effect of Rapten Rapid appears within the first 30 minutes after administration, and the effect continues for 4-6 no.
Absorption
After oral administration, the drug is quickly and completely absorbed. Absorption of diclofenac is reduced when taken with food. Absorption begins in the stomach, Cmax diclofenac in blood plasma is achieved approximately after 40 minutes after administration. Plasma concentration is linearly dependent on the dose of the administered drug.
Distribution
The binding to plasma proteins (mainly with albumins) высокое – до 99 %. Rapidly distributed into tissues and body fluids. It penetrates into synovial fluid. Thus Cmax diclofenac potassium in the synovial fluid is observed on 2-4 hours later, than in plasma. T1/2 diclofenac potassium from synovial fluid is 3-6 no, and its concentration in synovial fluid through 4-6 h after taking the drug remains higher, than in plasma during 12 no.
If the recommended interval between meals is observed, the drug does not accumulate.
Metabolism
Diclofenac is metabolized in the liver. 50% активного вещества подвергается метаболизму во время “первого прохождения” через печень. Metabolism occurs through multiple or single hydroxylation and conjugation. The isoenzyme CYP2C9 is involved in metabolism. Pharmacological activity of metabolites below, than diclofenac potassium.
Deduction
T1/2 from plasma is 1-2 no. Write mainly kidneys: about 60% - As metabolites, less 1% - Unchanged. The rest of the drug is excreted in the bile in the form of metabolites.
Systemic clearance is 260 ml / min.
Pharmacokinetics in special clinical situations
The pharmacokinetics of the drug does not change depending on the age of the patient.
In patients with severe renal impairment (CC<10 ml / min) the time of excretion of metabolites with bile increases. However, no increase in their concentration in the blood is observed..
In patients with chronic hepatitis or compensated liver cirrhosis, the pharmacokinetic parameters of diclofenac are the same, like in patients, without liver disease.
There are no changes in the pharmacokinetics of diclofenac due to repeated administration..
Pain syndrome of various origins:
-pain in muscles and joints (in t. no. pain in various parts of the spine);
- Headache;
- toothache;
- primary algodismenorrhea.
Eliminate symptoms of colds and flu:
- pain in muscles and joints;
- Headache;
- Sore throat;
-increased body temperature.
Adults and children senior 14 years the drug is prescribed in an initial dose 2 tab. Further, to achieve the required therapeutic effect, it is recommended to take 1-2 tab. every 4-6 no. The maximum daily dose is 6 tab. (75 mg).
The patient should be informed, that without consulting a doctor, the drug should not be taken any longer 3 days to reduce body temperature or more 5 days to treat pain. If the required effect is not achieved within the specified time frame, seek medical advice.
Tablets should be taken as a whole, without chewing, drinking water. To achieve maximum therapeutic effect, the drug should be taken before meals..
Determining the frequency of side effects: often (>1/100); sometimes (<1/100, but >1/1000); rarely (<1/1000, but >1/10 000); rarely (<1/10 000).
From the hematopoietic system: очень редко – тромбоцитопения, leukopenia, anemia (incl. hemolytic and aplastic anemia), agranulocytosis.
From the central and peripheral nervous system: often - headache, dizziness; rarely - somnolence; очень редко – парестезии, the loss of orientation, depression, insomnia, nightmares, irritability, psychotic disorders, – ухудшение памяти, convulsions, anxiety, tremor, aseptic meningitis, flavor violation, cerebrovascular disorders.
From the senses: often - dizziness; очень редко – звон в ушах, amblyacousia, blurred vision, diplopia.
Cardio-vascular system: очень редко – ощущение сердцебиения, chest pain, heart failure, myocardial infarction, arterial hypertension, vasculitis.
The respiratory system: редко – бронхиальная астма (including Dyspnea); очень редко – пневмония.
From the digestive system: often - nausea, vomiting, diarrhea, dyspepsia, abdominal pain, flatulence, anorexia, increase in liver transaminases; редко – гастрит, gastrointestinal bleeding, vomiting blood, diarrhea, ground, stomach or intestinal ulcer (with or without bleeding or perforation), hepatitis, jaundice; очень редко – колит (incl. with blood, exacerbation of ulcerative colitis or Crohn's disease), constipation, stomatitis, glossitis, pathology of esophagus, hiatal stricture, pancreatitis, Lightning (ful'minantnyj) hepatitis.
From the urinary system: очень редко – острая почечная недостаточность, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.
Dermatological reactions: часто – сыпь; очень редко – высыпания в виде пузырей, eczema, erythroderma (exfoliative dermatitis), alopecia, photosensitivity, purpura.
Allergic reactions: rarely - urticaria, anaphylactic and anaphylactoid reactions (including arterial hypotension and shock); очень редко – многоформная эритема, Stevens-Johnson syndrome, Lyell's syndrome (toxic epidermal necrolysis), allergic purpura.
Other: редко – отеки.
- attack of bronchial asthma;
- history of urticaria or acute rhinitis in response to taking acetylsalicylic acid or other NSAIDs (eg, ibuprofen);
- The period after coronary artery bypass grafting;
- stomach ulcer;
- inflammatory bowel diseases in the acute phase (NYAK, Crohn's disease);
-ulcerous hemorrhage or perforation;
- III trimester of pregnancy;
- Severe hepatic impairment;
- Severe renal insufficiency (CC less than 30 ml / min);
- Severe heart failure;
- Progressive kidney disease;
- Confirmed hyperkalemia;
- Violation of hematopoiesis;
- various hemostasis disorders;
- bone marrow damage;
- Children up to age 14 years;
- Hypersensitivity to the drug.
FROM caution use in patients with coronary artery disease, cerebrovascular diseases, Congestive heart failure, dyslipidemias/hyperlipidemias, diabetes, Peripheral arterial disease, at least QC 60 ml / min, smokers are patients; with indications in the anamnesis of the development of ulcerative lesions of the gastrointestinal tract, long-term use of NSAIDs, frequent alcohol use, severe somatic diseases; in elderly patients.
In the first and second trimesters of pregnancy, the drug is prescribed only if, when the expected benefit of therapy for the mother outweighs the potential risk for the fetus and child. Use of diclofenac, like other NSAIDS, contraindicated in the third trimester of pregnancy because of the risk of uterine atony and/or premature closure of the ductus arteriosus.
Diclofenac may have a negative effect on female fertility, therefore, the drug is not recommended for use in women, planning pregnancy.
Diclofenac, Like other NSAIDs, in small amounts out of breast milk. Therefore, to prevent unwanted effects in a child, Rapten Rapid is not recommended for use during lactation. (breast-feeding).
When using NSAIDs, there is a risk of gastrointestinal bleeding, as well as gastrointestinal ulcers, sometimes complicated by perforation, without previous symptoms or a history of similar attacks in the patient. These complications can have serious consequences especially for elderly patients. If you experience such symptoms, the drug should immediately cancel.
The risk of gastrointestinal bleeding increases with increasing doses of NSAIDs in patients with a history of peptic ulcer disease, especially in the case of complications of the disease bleeding and perforation, as well as in elderly patients. To reduce the risk of complications, therapy should be started and maintained at the minimum effective dose, taking into account the possibility of using combination therapy and the use of protective agents (eg, protonovogo pump inhibitor or misoprostol). When prescribing diclofenac in patients with existing GASTROINTESTINAL pathology (ulcer, bleeding, perforation) history, Therapy must be carried out under close medical supervision and extreme caution. Caution is recommended when administered concomitantly with medications., which may increase the risk of erosive and ulcerative lesions or bleeding from the gastrointestinal tract (such as systemic corticosteroids, antykoahulyantы, inhibitors of platelet aggregation or selective serotonin reuptake inhibitors).
Patients, suffering from ulcerative colitis or Crohn's disease, therapy should be under careful medical supervision, tk. as a result of taking diclofenac may occur and the exacerbation of these diseases.
Use of diclofenac should be discontinued at the first sign of the emergence of skin rashes, damage to the mucous membranes and if other signs of hypersensitivity to the components of the drug occur.
During treatment, in rare cases, allergies may occur, in t. no. anaphylactic / anaphylactoid reaction, incl. patients, not previously applied diclofenac.
It should be remembered, that due to its pharmacological properties, diclofenac can mask symptoms, characteristic of infectious diseases.
Avoid the simultaneous application of diclofenac with systemic NSAIDS (incl. selective Cox-2 inhibitors), Since no data, confirming the favorable effect as a result of synergies, and the absence of data on possible side effects.
Caution is required when prescribing the drug to elderly patients. Weakened elderly patients and elderly patients with low body weight are recommended to prescribe the drug in the minimum effective dose.
In patients with bronchial asthma, seasonal allergic rhinitis, swelling of the nasal mucosa (nasal polyps), COPD or chronic respiratory tract infection (particularly associated with allergic rinitopodobnymi symptoms), reactions to drugs from the Group of NSAIDS in the form of asthma attacks, Quincke's edema or urticaria develop more often than usual. When prescribing the drug to such patients, special caution is recommended. (preparedness for urgent medical interventions).
When prescribing diclofenac in patients with impaired liver function, it is necessary to carry out careful monitoring, Since these patients may deteriorate. During the use of the drug Rapten Rapid, the activity of one or more liver enzymes may increase. Therefore, during long-term drug therapy, regular testing of liver function indicators is indicated.. If a breach of the liver functional parameters are saved or amplified, or, If a complaint or develop symptoms, indicating liver disease, as well as in the case of, if other side effects occur (eg, eozinofilija, rash, etc.), the drug should be discontinued. It must be borne in mind, that hepatitis against the backdrop of the admission of diclofenac may arise without prodromal'nyh phenomena. Caution should be exercised when prescribing the drug to patients with hepatic porphyria., Since receiving diclofenac may trigger heart attack.
Since there are reports that, that with the use of NSAIDs, fluid retention and edema may occur, It is recommended to exercise special caution when prescribing Rapten Rapid to patients with impaired renal and cardiac function., with arterial hypertension in history, elderly patients, while receiving diuretics or medication, have a significant effect on kidney function, as well as patients, who have a significant decrease in blood volume of any etiology, eg, during the period before or after major surgical interventions. In such cases, monitoring of renal function is recommended as a precaution when using diclofenac.. After the cessation of therapy usually restores the original settings.
Rapten Rapid is recommended to be used for several days. When prescribing the drug for a long time, systematic monitoring of peripheral blood patterns is indicated., liver function, kidney, study of fecal blood.
Rapten Rapid may temporarily inhibit platelet aggregation. Therefore, in patients with impaired hemostasis requires careful monitoring of relevant laboratory values.
Avoid drinking alcohol while taking Rapten Rapid.
The drug is not recommended to be taken during or immediately after meals.
Effects on ability to drive vehicles and management mechanisms
During treatment, there may be some slowdown in the rate of psychomotor reactions. Concerning, patients, receiving the drug, You must refrain from activities, requiring attention and quick emotional reactions.
Symptoms: disorders of the digestive system, hypotension, nephrotoxicity (up to acute renal failure), dizziness, headache, hyperventilation, dizziness; children-mioclauniceskie convulsions, nausea, vomiting, abdominal pain, bleeding, the liver and kidneys.
Treatment: gastric lavage, followed by the appointment of activated charcoal, symptomatic and supportive therapy. Forced diuresis, hemodialysis maloeffyektivny.
When used concomitantly, diclofenac may increase plasma concentrations of lithium and digoxin..
When taken simultaneously with diuretic or antihypertensive drugs (eg, beta-blockers, ACE inhibitors) diclofenac may reduce the antihypertensive effect.
Simultaneous application of kalisberegath dioretikov can lead to increased levels of potassium in the blood serum.
Concomitant use of diclofenac and other systemic NSAIDs or corticosteroids may increase the incidence of gastrointestinal adverse events.
Special caution is required when co-administered with anticoagulants or platelet aggregation inhibitors, since when diclofenac is taken simultaneously with these drugs, the risk of bleeding increases.
In clinical studies found, that the simultaneous use of diclofenac and oral hypoglycemic drugs is possible and the effectiveness of the latter does not change. However, isolated cases of development are known, like hypoglycemia, and hyperglycemia, which required changing the dose of hypoglycemic drugs during the use of diclofenac.
Caution is required when prescribing NSAIDs less than, than 24 hours before or after taking methotrexate, tk. in such cases, the concentration of methotrexate in the blood may increase and its toxic effect may increase.
The effect of NSAIDs on the synthesis of prostaglandins in the kidneys may increase the nephrotoxicity of cyclosporine.
There are isolated reports of the development of seizures in patients, who simultaneously received antibacterial drugs quinolone derivatives and NSAIDs.
Antacids, such as aluminum hydroxide and magnesium hydroxide, may slow down the absorption of diclofenac, but do not affect the total amount of drug absorbed.
With concomitant therapy with selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline) may be accompanied by an increased risk of gastrointestinal bleeding.
The drug is resolved to application as an agent Valium holidays.
List B. The drug should be stored out of reach of children, dry, dark place at a temperature of 15 ° to 25 ° C. Shelf life - 2 year.
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