Composition, form of production and packaging
Suppositories rectal white or yellowish-white, conical; on the longitudinal section - a homogeneous wax mass of white or yellowish-white color.
1 supp.
diclofenac sodium 50 mg
Excipients: fat is solid.
5 pieces. - Strips (2) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Diclofenac is a non-steroidal anti-inflammatory drug (NSAID) with analgesic, anti-inflammatory and antipyretic effects.
The main mechanism of its action and associated side effects are indiscriminate inhibition of the activity of the enzyme cyclooxygenase 1 and 2 (COX1 and COX2), which leads to a disruption of the metabolism of arachidonic acid, a decrease in the synthesis of prostaglandins, prostacyclin and thromboxane. The synthesis of prostaglandins in the kidneys, mucous membrane of the stomach and synovial fluid decreases.
The most effective for inflammatory pain. In rheumatic diseases, the anti-inflammatory and analgesic effect of diclofenac significantly reduces the severity of pain, morning stiffness, swelling of the joints, which improves the functional state of the joints. In injuries, in the postoperative period, diclofenac reduces pain and inflammatory edema. Like all NSAIDs, diclofenac has antiaggregant activity. In therapeutic doses, diclofenac has virtually no effect on bleeding time. With prolonged treatment, the analgesic effect of diclofenac does not decrease.
PHARMACOKINETICS
Suction
Diclofenac is rapidly absorbed after rectal administration. C max is reached after 1 hour. With rectal administration, eating does not affect the absorption of diclofenac.
Distribution
99% of the absorbed diclofenac binds to plasma proteins, mainly albumins. Diclofenac actively penetrates into the synovial fluid, where it reaches 60-70% of serum concentrations. After 3-6 hours after the application of the concentration of the active substance and metabolites in the synovial fluid is higher than in the serum.Diclofenac from synovial fluid is excreted more slowly than from serum.
Metabolism and excretion
T 1/2 of diclofenac is 1-2 hours. Diclofenac is almost completely metabolized in the liver, mainly by hydroxylation and methoxylation. The enzyme system P450 CYP2C9 takes part in the metabolism of the drug. The pharmacological activity of metabolites is lower than that of diclofenac.
T 1/2 from the plasma - 2 hours. About 70% of the administered dose is excreted as pharmacologically inactive metabolites by the kidneys; less than 1% is unchanged, the rest of the dose is excreted as metabolites with bile.
Pharmacokinetics in special clinical cases
In patients with severe renal failure (CC less than 10 ml / min), excretion of metabolites with bile is increased, while there is no increase in their concentration in the blood.
In patients with chronic hepatitis or compensated cirrhosis of the liver, as well as in elderly patients, the pharmacokinetic parameters of diclofenac do not change.
INDICATIONS
Diseases that require the achievement of a rapid anti-inflammatory or analgesic effect:
- inflammatory diseases of the musculoskeletal system (rheumatoid arthritis, seronegative spondylitis, juvenile chronic arthritis, arthritis of another etiology);
- degenerative diseases of the musculoskeletal system (osteoarthritis);
- microcrystalline arthritis (gouty arthritis, pseudo-arthritis arthritis);
- rheumatic soft tissue damage;
- periarthritis, bursitis, myositis, tendonitis, synovitis;
- other inflammatory diseases of the musculoskeletal system accompanied by pain syndrome.
As an analgesic, Naklofen is used in soft tissue injuries, in dentistry, after surgical interventions, in severe migraine attacks, primary algodismorrhea, adnexitis, as well as in renal or biliary colic.
Diclofenac is intended for symptomatic therapy and does not affect the progression of the disease.
DOSING MODE
Rectally. If patients with oral diclofenac form are poorly tolerated, Naklofen can be administered rectally in the form of suppositories at appropriate doses. When combining several dosage forms (in addition to oral administration of the drug), it should be borne in mind that the daily dose of diclofenac should not exceed 150 mg.
Adults with an initial dose of 100-150 mg per day (1 suppository 2-3 times a day), depending on the severity of the disease. To adolescents aged 15 years and over , one suppository is recommended no more than 2 times a day. The maintenance dose is usually 100 mg per day (1 suppository 2 times a day).
The minimum effective dose should be used as little as possible.
SIDE EFFECT
Classification of the incidence of adverse events (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 - from <1/10000, including individual messages.
From the digestive system: often - epigastric pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, increased activity of aminotransferases; rarely gastritis, proctitis, exacerbation of hemorrhoids, bleeding from the gastrointestinal tract (vomiting with blood, melena, diarrhea with a trace of blood), gastrointestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, dysfunction of the liver; very rarely - stomatitis, glossitis, dryness of the mucous membranes (including the mouth), damage to the esophagus, diaphragm-like bowel strains (nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease), constipation, pancreatitis, fulminant hepatitis. When using suppositories, local irritation and inflammation are possible.
From the nervous system: often - headache, dizziness; rarely - drowsiness; very rarely - a violation of sensitivity, incl. paresthesia, memory disorders, tremors, convulsions, anxiety, cerebrovascular disorders, aseptic meningitis, disorientation, depression, insomnia, nightmares, irritability, mental disorders.
From the senses: often - vertigo; very rarely - visual impairment (blurred vision, diplopia), hearing impairment, tinnitus, a violation of taste sensations.
From the urinary system: very rarely - acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.
On the part of the organs of hematopoiesis: very rarely - thrombocytopenia, leukopenia, eosinophilia, hemolytic and aplastic anemia, agranulocytosis.
Allergic reactions: anaphylactic / anaphylactoid reactions, including a marked decrease in blood pressure and shock; very rarely angioedema (including facial).
From the cardiovascular system: very rarely - palpitations, extrasystole, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction.
On the part of the respiratory system: rarely - cough, bronchial asthma (including dyspnea); very rarely - pneumonitis, laryngeal edema.
On the part of the skin: often - skin rash; rarely - hives; very rarely, bulbar eruptions, eczema, incl. multiform and Stevens-Johnson syndrome, Lyell's syndrome, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, incl. allergic.
CONTRAINDICATIONS
- period after aortocoronary shunting;
- erosive and ulcerative changes in the mucosa of the stomach or duodenum, active gastrointestinal bleeding;
- Inflammatory bowel disease (NNC, Crohn's disease) in the phase of exacerbation;
- rectal bleeding, hemorrhoids, trauma or inflammation of the rectum;
- cerebrovascular bleeding;
- hemophilia and other coagulation disorders;
- severe hepatic impairment or active liver disease;
- severe renal failure (QC less than 30 ml / min), including confirmed hyperkalemia, progressive kidney disease;
Decompensated heart failure;
- oppression of bone marrow hematopoiesis;
- III trimester of pregnancy, the period of breastfeeding;
- Children's age (up to 15 years);
- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including in anamnesis);
hypersensitivity to diclofenac.
With caution: IHD, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, CC less than 60 ml / min;anamnestic data on the development of gastric ulcerative lesions, the presence of Helicobacter pylori infection, old age, prolonged use of NSAIDs, frequent alcohol use, severe somatic diseases, pregnancy I-II trimester, concomitant therapy with anticoagulants (eg warfarin), antiplatelet agents (eg, acetylsalicylic acid, clopidogrel), fibrinolytics, oral glucocorticoids (eg, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxet in, sertraline).
PREGNANCY AND LACTATION
The use of diclofenac in pregnant women is possible only when the expected benefit for the mother exceeds the potential risk to the fetus. Diclofenac should not be used during the last trimester of pregnancy.
Despite the fact that diclofenac is found in breast milk in small amounts, its use during breast-feeding is not recommended.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated use of the drug in severe renal failure (QC less than 30 ml / min), including confirmed hyperkalemia, a progressive kidney disease.
With caution for CK less than 60 ml / min
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated use of the drug in severe hepatic insufficiency or active liver disease
APPLICATION FOR CHILDREN
Contraindicated for children under 15 years.
APPLICATION IN ELDERLY PATIENTS
With caution in elderly patients.
SPECIAL INSTRUCTIONS
Patients should inform the physician of any chronic illness, metabolic disorder, or sensitivity of the reaction in the history.
When treating the drug Naklofen should carefully monitor patients who have a history of which there are diseases of the upper gastrointestinal tract.
With caution should use the drug with NNC and Crohn's disease because of the possible exacerbation of the disease.
If there are signs of liver damage (skin itching, yellowing of the skin, nausea, vomiting, abdominal pain, darkening of the urine, increasing the level of "liver" transaminases), stop taking the drug and consult a doctor.
With long-term use (more than 2 weeks) of diclofenac, it is necessary to monitor the indicators of liver function (the level of "liver" transaminases).
With caution, diclofenac should be prescribed to patients with severe renal or hepatic insufficiency, heart failure, blood clotting disorders, porphyria, epilepsy, and patients receiving anticoagulants or fibrinolytics.
Do not use the drug simultaneously with other NSAIDs.
The drug can change the properties of platelets, but does not replace the preventive effect of acetylsalicylic acid in cardiovascular diseases.
The use of the drug may adversely affect female fertility and is not recommended for women planning pregnancy.
In infectious diseases, the anti-inflammatory and antipyretic effects of diclofenac sodium can mask the symptoms of these diseases.
In elderly patients, as with other drugs, Naklofen should be used in the lowest effective dose.
Influence on ability to manage motor transport and other complex mechanisms
During the treatment period, it is possible to reduce the speed of mental and motor reactions, so it is necessary to refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
OVERDOSE
When using suppositories, an overdose is unlikely.
Symptoms: vomiting, nausea, abdominal pain, bleeding from the gastrointestinal tract, diarrhea, headache, dizziness, tinnitus, increased excitability, hyperventilation with increased convulsive readiness, convulsions, with a significant overdose of acute renal failure, hepatotoxic effect.
Treatment: symptomatic therapy aimed at the elimination of high blood pressure (BP), violations of kidney function, seizures, irritation of the gastrointestinal tract, respiratory depression. Forced diuresis and hemodialysis are ineffective (significant association with proteins and intensive metabolism).
DRUG INTERACTION
Increases the concentration in the plasma digoxin, methotrexate, lithium and cyclosporine.
Reduces the effect of diuretics, against the background of potassium-sparing diuretics increases the risk of hyperkalemia; against the background of anticoagulants, antiplatelet agents and trombolytic drugs (alteplase, streptokinase, urokinase), the risk of developing bleeding (bowl - gastrointestinal tract) increases.
Reduces the effect of hypotensive and hypnotic drugs. Increases the likelihood of side effects of other NSAIDs and GCS (bleeding from the gastrointestinal tract), toxicity of methotrexate and nephrotoxicity of cyclosporine.
Acetylsalicylic acid reduces the concentration of diclofenac in the blood. Simultaneous use with paracetamol increases the risk of developing nephrotoxic effects of diclofenac.
With simultaneous administration with giglikemicheskimi means can be observed hypo or giperglicemia. With this combination of funds, it is necessary to monitor the concentration of glucose in the blood.
Cefamandol, cefoperazone, cefotetan, valproic acid and plikamycin increase the incidence of hypoprothrombinemia.
Cyclosporine and gold preparations increase the effect of diclofenac on the synthesis of prostaglandins in the kidneys, which is manifested by increased nephrotoxicity.
Selective serotonin reuptake inhibitors increase the risk of bleeding from the digestive tract.
Simultaneous administration with ethanol, colchicine, corticotropin and preparations of St. John's wort increases the risk of bleeding in the digestive tract.
Medicines that cause photosensitivity, increase the sensitizing effect of diclofenac to ultraviolet radiation.
Drugs that block tubular secretion, increase the concentration in the plasma of diclofenac, thereby increasing its toxicity.
Antibacterial drugs from the quinolone group increase the risk of seizures.
TERMS OF RELEASE FROM PHARMACY
On prescription.
TERMS AND CONDITIONS OF STORAGE
List B. At a temperature of no higher than 25 В° C. Keep out of the reach of children. Shelf life - 4 years.
