2010/06/23

Rapten Rapid

Composition, structure and packing

Tablets are coated with sugar coat red, with small splashes of lighter-colored, round, biconvex.

1 tab. diclofenac potassium 12.5 mg.

Excipients: calcium hydrophosphate, corn starch, karboksimetilkrahmal sodium (Type A), colloidal silicon dioxide (anhydrous), povidone 30, magnesium stearate.

The composition of the shell: sucrose, talc, dye, crimson Ponceau E124, acacia gum, povidone 25, titanium dioxide E171, macrogol 6000.

Tablets, coated in red, with small splashes of lighter-colored, round, biconvex.

1 tab. Diclofenac Potassium 50 mg.

Other ingredients: colloidal silicon dioxide (anhydrous), calcium hydrophosphate (anhydrous), starch maize, povidone K30, magnesium stearate, sodium karboksimetilkrahmal, gum arabic, sucrose, talc, cochineal red lacquer E124, povidone K25, macrogol 6000.

Clinico-pharmacological group: NSAID.

Pharmacological action

NSAIDs. Has a marked anti-inflammatory, analgesic and antipyretic effect.

Indiscriminately inhibiting cyclooxygenase 1 and 2 (COX-1 and COX-2), diclofenac potassium violates the metabolism of arachidonic acid and inhibits the synthesis of prostaglandins (mediators, which play a major role in the pathogenesis of inflammation, pain and fever).

Analgesic and antipyretic effect Rapten Rapida tablets 12.5 mg manifested during the first 30 min after administration, but the effect lasts for 4-6 hours

Pharmacokinetics

Absorption

After oral administration the drug is rapidly and completely absorbed. Absorption of diclofenac is reduced when taking it with food. Absorption begins in the stomach, Cmax of diclofenac in plasma is reached after about 40 minutes after ingestion. The concentration in plasma is in a linear dose-dependent administration. Cmax in blood plasma after administration of 50 mg tablets of 1.3 ug / ml.

Distribution

The binding with plasma proteins (mainly albumin) is high - up to 99%. Rapidly distributed in tissues and body fluids. Penetrates the synovial fluid. At the same time Cmax of diclofenac potassium in the synovial fluid observed by 2-4 h later than in plasma. T1 / 2 of diclofenac potassium from the synovial fluid is 3-6 hours, and its concentration in the synovial fluid within 4-6 hours after taking the drug remain higher than in plasma as early as within 12 hours

Under the recommended interval between meals is no accumulation of the drug.

Metabolism

Diclofenac is metabolized in the liver. 50% of the active substance undergoes metabolism during the "first pass" through the liver. Metabolism occurs by multiple or single-hydroxylation and conjugation. Participates in the metabolism of isoenzyme CYP2C9. Pharmacological activity of metabolites is lower than that of diclofenac potassium.

Withdrawal

T1 / 2 from plasma is 1-2 hours is derived mainly kidneys: about 60% - in the form of metabolites, less than 1% - unchanged. The remainder of the drug is excreted in the bile as metabolites.

Systemic clearance is 260 ml / min.

Pharmacokinetics in special clinical situations

Pharmacokinetics does not change depending on the age of the patient.

In patients with severe renal dysfunction (CC <10 ml / min) during removal of metabolites with bile increases. At the same time increasing their concentration in the blood is not observed.

In patients with chronic hepatitis or compensated cirrhosis pharmacokinetic parameters of diclofenac are the same as that of patients without liver disease.

Changes in the pharmacokinetics of diclofenac on the background of repeated administration does not occur.

Statement

Tablets 12.5 mg pain syndrome of different origin:
sharp pains in muscles and joints (including pain in various parts of the spine);
severe headache;
severe toothache;
Primary tuberculosis,.

Addressing symptoms of colds and flu:
Acute pain in muscles and joints;
headache
sore throat;
sharp rise in body temperature.

Tablets 50 mg are used for short-term treatment (up to 7 days) of pain that accompanies the following conditions:
inflammatory diseases of the musculoskeletal system (including abscess, bursitis, myalgia);
post-traumatic pain syndromes accompanied by inflammation;
postoperative pain;
lumbago;
sciatica;
neuralgia;
toothache;
migraine;
inflammatory disease of the pelvic organs;
Primary tuberculosis,;
proctitis;
renal colic;
biliary colic;
infectious and inflammatory diseases of ENT organs with marked pain syndrome, v.t.ch pharyngitis, tonsillitis, otitis media (in the complex therapy);
fever.

Dosage regimen

12.5 mg Tablets Adults and children over 14 years, the drug is prescribed in an initial dose of 2 tabs. Next to reach the required therapeutic effect recommended to take 1-2 pills. every 4-6 hours maximum daily dose of 6 tab. (75 mg).

Patients should be aware that, without consulting a doctor, the drug should not take more than 3 days for fever and more than 5 days to treat pain. If deadlines are not achieved the desired effect, you must consult a doctor.

Tablets should be taken as a whole, without chewing, drinking water. To achieve maximum therapeutic effect of the drug should be taken before meals.

Tablets 50 mg

Dosage is determined individually according to the severity of the disease.

Adults medication prescribed in a daily dose of 100-150 mg, divided into 2-3 reception.

The maximum dose - 200 mg / day.

Adolescents over 15 years of drug administered in a daily dose of 100 mg, divided into 2 admission.

Elderly patients, particularly exhausted and debilitated patients should be prescribed the drug in the lowest effective dose.

Tablets should be taken as a whole, without chewing, drinking water. To achieve maximum therapeutic effect of the drug should be taken before meals.

Side effect

The frequency of side effects: frequent (> 1 / 100), sometimes (<1> 1 / 1000), rarely (<1> 1 / 10 000), very rarely - <1 / 10 000.

12.5 mg Tablets

On the part of the hemopoietic system: very rarely - thrombocytopenia, leukopenia, anemia (including hemolytic and aplastic anemia), agranulocytosis.

From the side of the central nervous system and peripheral nervous systems: common - headache, dizziness, rarely - drowsiness, disorientation, depression, insomnia, nightmares, irritability, psychotic disorders, very rare - paresthesia, memory loss, convulsions, anxiety, tremor, aseptic meningitis , taste disorders, cerebrovascular disorders.

From the sensory organs: often - dizziness, very rarely - tinnitus, hearing impairment, blurred vision, diplopia.

Since the cardiovascular system: very rarely - a feeling the heartbeat, pain behind the sternum, heart failure, myocardial infarction, hypertension, vasculitis.

On the part of the respiratory system: rarely - bronchial asthma (including dyspnoea); very rarely - pneumonia.

On the part of the digestive system: frequent - nausea, vomiting, diarrhea, dyspepsia, abdominal pain, flatulence, anorexia, increase in liver transaminases; rarely - gastritis, gastrointestinal bleeding, vomiting blood, diarrhea, melena, stomach ulcer or intestine (with with or without bleeding or perforation), hepatitis, jaundice, very rarely - colitis (including the blood, worsening of ulcerative colitis or Crohn's disease), constipation, stomatitis, glossitis, pathology of the esophagus, esophageal stricture orifice, pancreatitis, fulminant ( fulminant) hepatitis.

From the urinary system: very rarely - acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.

Dermatological reactions: often - a rash, very rarely - as a blistering rash, eczema, erythroderma (exfoliative dermatitis), alopecia, photosensitivity, purpura.

Allergic reactions: rare - rash, anaphylactic and anaphylactoid reactions (including hypotension and shock) are very rare - erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis syndrome (toxic epidermal necrolysis), allergic purpura, angioedema (including edema person).

Other: rarely - swelling.

Tablets 50 mg

On the part of the digestive system: often - NSAID-gastropathy (gastralgia and discomfort in the epigastric region, nausea, feeling of repletion, regurgitation, heartburn, diarrhea, abdominal pain, flatulence), erosive and ulcerative lesions gastrointestinal tract, perforation of the intestinal wall, bleeding from the gastrointestinal tract , dry mouth, constipation, pancreatitis, toxic hepatitis, sometimes - vomiting, decreased appetite, anorexia, stomatitis, glossitis.

From the side of the central nervous system and peripheral nervous systems: common - headache, dizziness, and sometimes - convulsions, aseptic meningitis, memory decline, depression, psychotic reactions, peripheral polyneuropathy (hypoesthesia, tremor, pain or weakness in the muscles of the arms and legs), lethargy, irritability and nervousness, anxiety, insomnia, weakness and fatigue.

From the senses: sometimes - a toxic lesion of the optic nerve, reduction of visual acuity, diplopia, scotoma, hearing loss, ringing, and tinnitus.

On the part of the urinary system: often - fluid retention, sometimes - hematuria, cystitis, thamuria, proteinuria, interstitial nephritis, nephrotic syndrome, oliguria, anuria, acute renal failure, peripheral edema.

On the part of the reproductive system: dysmenorrhea.

From the side of hematopoiesis: sometimes - agranulocytosis, hemolytic anemia, aplastic anemia, anemia associated with internal bleeding, leukopenia, neutropenia, thrombocytopenia purpura with or without her.

The respiratory system: sometimes - shortness of breath.

Dermatological reactions: often - itching, skin rash (predominantly erythematous and urticaria), ecchymosis, hyperemia of the skin, sometimes - photodermatitis.

Allergic reactions: sometimes - erythema multiforme exudative, including Stevens-Johnson syndrome, Lyell syndrome (toxic epidermal necrolysis).

Contraindications

12.5 mg Tablets
bronchial asthma;
urticaria or acute rhinitis in history in response to receiving aspirin or other NSAID (eg ibuprofen);
Since the aorto-coronary bypass surgery;
ulcer;
inflammatory bowel disease exacerbation (UC, Crohn's disease);
ulcer bleeding or perforation;
III trimester of pregnancy;
severe hepatic impairment;
renal failure severe (CC less than 30 ml / min);
heart failure, severe;
progressive renal disease;
confirmed hyperkalaemia;
hemodyscrasia;
various violations of hemostasis;
damage to bone marrow;
Children under 14 years
Hypersensitivity to the drug's components.

Tablets 50 mg
"Aspirin" asthma;
erosive-ulcerative lesions GIT (exacerbation);
bleeding from the gastrointestinal tract;
hemodyscrasia;
Various hemostatic disorders (including hemophilia);
Pregnancy
Lactation (breastfeeding);
childhood and adolescence (15 years);
hypersensitivity to NSAIDs (including aspirin).

Precautions to apply Rapten Rapid patients with severely impaired liver and kidney function in history, with QA <60 ml / min, hepatic porphyria, anemic, suffering from bronchial asthma, hypertension, ischemic heart disease, congestive heart failure, edema, erosions and ulcerative lesions GIT without exacerbation, diverticulitis, dyslipidemia, or hyperlipidemia, diabetes, severe somatic diseases, patients receiving long-term NSAIDs, elderly patients and patients in the postoperative period in chronic alcoholism and smoking.

Pregnancy and lactation

12.5 mg Tablets

In I and II trimesters of pregnancy drug prescribed only when the intended use of therapy to the mother outweighs the potential risk to the fetus and child. The use of diclofenac, like other NSAIDs, is contraindicated in the III trimester of pregnancy because of possible uterine atony and / or premature closure of ductus arteriosus.

As with other NSAIDs, diclofenac in small amounts excreted in breast milk. Therefore, to prevent adverse effects in the child Rapten Rapid is not recommended during lactation (breastfeeding).

Tablets 50 mg

Use during pregnancy and lactation (breastfeeding) is contraindicated.

Diclofenac may have a negative impact on female fertility, and therefore not advisable to appoint Rapten Rapid women planning pregnancy.

Application for violations of liver function

Precautions appoint Rapten Rapid disorders of liver function.

Application for violations of renal function

Precautions appoint Rapten Rapid disorders of kidney function.

Cautions

In the application of NSAIDs is likely the development of gastrointestinal bleeding and ulcers of the digestive tract, sometimes complicating perforation, without prior symptoms or the presence of similar attacks in the history of the patient. These complications can have serious consequences especially for the elderly. If you have similar symptoms the drug should be lifted immediately.

The risk of gastrointestinal bleeding increases with increasing doses of NSAIDs in patients with peptic ulcer history, especially in case of complications of the disease bleeding and perforation, as well as elderly patients. To reduce the risk of complications of therapy should be initiated and maintained at the minimum effective dose for the possibility of combined therapy and the use of protective equipment (eg, proton pump inhibitors or misoprostol). In the appointment of diclofenac in patients with available pathology of the gastrointestinal tract (ulcers, hemorrhage, perforation) history, it is necessary to conduct therapy with careful medical supervision and compliance with particular caution. Caution should be observed while the appointment of drugs that may increase the risk of erosive and ulcerative lesions or bleeding from the gastrointestinal tract (such as systemic corticosteroids, anticoagulants, platelet aggregation inhibitors or selective serotonin reuptake inhibitors).

Patients suffering from ulcerative colitis or Crohn's disease, therapy should be administered under close medical supervision, because as a result of taking diclofenac can occur exacerbation of these diseases.

The use of diclofenac should be discontinued at the first sign of the emergence of skin rashes, lesions of the mucous membranes, and when you have other signs of hypersensitivity to the drug's components.

In patients who previously did not use diclofenac during treatment may occur allergy, including anaphylactic / anaphylactoid reactions.

It should be remembered that in connection with their pharmacological properties diclofenac may mask the symptoms associated with infectious diseases.

Avoid the simultaneous application of diclofenac with systemic NSAID (including a selective inhibitor of COX-2), since there is no evidence of a beneficial effect as a result of synergy, and there are no data on possible side effects.

Caution must be exercised in the appointment of the drug in elderly patients. Debilitated elderly patients and elderly patients with low body weight should appoint a drug in the lowest effective dose.

In patients with bronchial asthma, seasonal allergic rhinitis, swelling of the nasal mucosa (nasal polyps), COPD, or chronic infection of the respiratory tract (especially related to allergic rhinitis-like symptoms), reactions to drugs from the group of NSAIDs in the form of asthma attacks, Quincke's edema or hives develop more often than usual. In the appointment of the drug in such patients should be very careful (readiness for urgent medical intervention).

In the appointment of diclofenac in patients with impaired liver function should involve careful monitoring, because the state of such patients may deteriorate. During the application Rapten Rapida can increase the activity of one or more liver enzymes. Therefore, long-term therapy the drug showed regular study of indicators of liver function. If violations of the functional parameters of liver persist or intensify, or if you develop complaints or symptoms suggestive of liver disease, and if there are other side effects (eg, eosinophilia, rash etc.), the drug should be cancel. It must be borne in mind that hepatitis on a background of taking diclofenac can occur without prodrome. Caution must be exercised in the appointment of the drug to patients with hepatic porphyria, since receiving diclofenac can provoke attacks.

As has been reported that during treatment with NSAIDs may be fluid retention and edema should be very careful when appointing Rapten Rapida patients with impaired renal function and heart failure, arterial hypertension, a history of elderly patients, while taking diuretics or drugs that have a significant impact on renal function, as well as patients that have a significant decrease in BCC of any etiology, eg, in the period before or after major surgery. In such cases, the use of diclofenac as a precaution it is recommended to monitor kidney function. After the cessation of therapy is usually restored the original settings. Rapten Rapid recommended for use within a few days.

In the appointment of the drug for a long time shows a systematic pattern control peripheral blood, liver, kidneys, study stool test for blood.

Rapten Rapid may temporarily inhibit platelet aggregation. Therefore, in patients with disorders of hemostasis requires careful control of the laboratory parameters.

During the reception Rapten Rapid should avoid alcohol.

Effects on ability to drive vehicles and management mechanisms

In the period of treatment there may be some reduction of speed of psychomotor reactions. Therefore, patients taking the drug, must refrain from activities requiring attention and rapid psychomotor reactions.

Overdose

Symptoms: disorders of the digestive system, hypotension, nephrotoxicity (up to acute renal failure), dizziness, headache, hyperventilation lungs, clouding of consciousness in children - Myoclonic seizures, nausea, vomiting, abdominal pain, bleeding, abnormal liver function and kidney.

Treatment: gastric lavage, followed by the appointment of activated charcoal, symptomatic therapy. Forced diuresis, hemodialysis ineffective.

Drug Interactions

Tablets 12.5 mg and 50 mg tablets

With simultaneous application of diclofenac may increase the concentration of lithium and digoxin in the blood plasma.

At the same time taking a diuretic or other antihypertensive drugs (eg, beta-blockers, ACE inhibitors), diclofenac can reduce the severity of antihypertensive action.

The simultaneous use potassium-sparing diuretics may increase potassium levels in blood serum.

Simultaneous use of diclofenac and other systemic NSAIDs or corticosteroids may increase the incidence of adverse events from the gastrointestinal tract.

Take special care is required when a joint appointment with anticoagulants or platelet aggregation inhibitor, because, while taking diclofenac with these drugs increases the risk of bleeding.

In clinical studies revealed that the simultaneous application of diclofenac and oral hypoglycemic agents is possible and thus the effectiveness of the latter does not change. However, we know of individual cases, as hypoglycemia and hyperglycemia, which required dose change hypoglycemic drugs during the application of diclofenac.

Caution must be exercised in the appointment of NSAIDs for less than 24 hours before or after taking methotrexate, as in such cases may increase the concentration of methotrexate in blood and increase its toxic effects.

Effect of NSAIDs on the synthesis of prostaglandins in the kidney may increase the nephrotoxicity of cyclosporine.

There are some reports on the development of seizures in patients treated with both antibacterial drugs quinolone derivatives and NSAIDs.

Antacids, such as aluminum hydroxide and magnesium hydroxide, can slow the absorption of diclofenac, but not affect the total amount of absorbed drug.

Concomitant therapy selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline) accompanied by increased risk of gastrointestinal bleeding.

Tablets 50 mg

The drug reduces the effectiveness of hypnotic drugs.

Acetylsalicylic acid reduces the concentration of diclofenac in the blood.

At simultaneous application with paracetamol increases the risk of nephrotoxic effects of diclofenac.

Tsefamandol, cefoperazone, tsefotetan, valproic acid and plikamitsin increase the incidence of gipoprotrombinemii.

Preparation of gold increases the influence of diclofenac on the synthesis of prostaglandins in the kidneys that increases the nephrotoxicity.

Simultaneous with the appointment of ethanol, colchicine, corticotrophin, and St. John's wort preparations increases the risk of bleeding from the gastrointestinal tract.

Diclofenac increases the effects of drugs causing photosensitivity.

Drugs that block tubular secretion, increase plasma concentration of diclofenac, thereby increasing its toxicity.

Terms and Conditions of storage

The product should be stored out of reach of children, dry, dark place at a temperature of 15 ° to 25 ° C.

Expiration pills 12.5 mg - 2 years.

Expiration tablets 50 mg - 3 years.