Diclofenac 50mg suppositories FIP 10 pc

Description

Composition
Active substance:
1 suppository contains: Sodium diclofenac – 50 mg.
Excipients:
Hard fat (a suppository base) – to obtain a suppository weighing 1.50 g
Description:
Suppositories are white or white with a slightly yellowish white, odorless, torpedo-shaped; on the cut tolerance of air core or funnel-shaped depressions.
Product form:
Diclofenac-FIP rectal suppositories 50 mg; 5 suppositories in blisters of PVC film. Two blisters with instruction for medical application is placed in a pile of cardboard.
Contraindications
Since the aortocoronary bypass surgery; III trimester of pregnancy, lactation;
Uncompensated heart failure;
Hypersensitivity to the active substance or auxiliary components;
A history of an attack bronchial, rhinitis, urticaria, after receiving aspirin or other NSAIDs (complete or incomplete syndrome intolerance of acetylsalicylic acid – rhinosinusitis, urticaria, polyps, nasal mucosa, asthma);
Erosive and ulcerative changes in the mucosa of the stomach or intestine -perstnoy 12, active gastrointestinal bleeding;
Inflammatory bowel disease (ulcerative colitis, Crohn’s disease);
Cerebrovascular bleeding or other bleeding disorders and hemostasis;
Severe hepatic insufficiency or active liver disease;
Renal failure (creatinine clearance less than 30 mL / min), progressive renal disease, including confirmed by hyperkalemia;
Children’s age (18 suppository 100mg, 15 years for the suppositories of 50 mg);
Rectal bleeding, hemorrhoids, trauma, or inflammation of the rectum.
Carefully:
Anemia, asthma, cerebrovascular disease, ischemic heart disease, congestive heart failure, hypertension, peripheral artery disease, edema syndrome, liver or kidney failure, dyslipidemia / hyperlipidemia, diabetes, smoking, inflammatory bowel disease, condition after major surgery, induced porphyria, advanced age, diverticular disease, systemic connective tissue disease, creatinine clearance less than 60 mL / min, pregnant awn (I-II trimester).
A history of the development of ulcerative gastro – intestinal tract, the presence of infection Helicobacter pylori, long-term use of NSAIDs, frequent alcohol consumption, severe somatic diseases.
Simultaneous anticoagulation therapy (e.g. warfarin), antiplatelet agents (e.g., aspirin, clopidogrel), oral corticosteroids (e.g., prednisone), selective serotonin reuptake inhibitors (e.g., citalopram, fluoxetine, paroxetine, sertraline).
Dosage
50 mg
Indications
Symptomatic treatment of diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, ankylosing spondylitis, gouty arthritis, rheumatic soft tissue, osteoarthritis peripheral joints and spine, including radicular syndrome, tenosynovitis, bursitis). Pain syndrome weak or moderate severity: neuralgia, myalgia, sciatica, post-traumatic pain, accompanied by inflammation, postoperative pain, headache, migraine, tuberculosis, adnexitis, proctitis, toothache. In the combined therapy of infectious and inflammatory diseases of the ear, nose and throat with severe pain (pharyngitis, tonsillitis, otitis media).
Interaction with other drugs
Increasing the concentration of digoxin in plasma of methotrexate drugs lithium and cyclosporine. Reduces the effect of diuretics, potassium-sparing diuretics in the background increases the risk of hyperkalemia; against the background of anticoagulants, thrombolytic agents (alteplase, streptokinase, urokinase) – The risk of bleeding (usually from the gastrointestinal tract). Reduces the effect of antihypertensive and hypnotic drugs. It increases the likelihood of side effects of other nonsteroidal anti-inflammatory drugs and glucocorticosteroid means (bleeding in the gastrointestinal tract), the toxicity of methotrexate and cyclosporine nephrotoxicity. Acetylsalicylic acid reduces the concentration of diclofenac in the blood. Simultaneous use of paracetamol with increased risk of nephrotoxic effects of diclofenac. Reduces the effect of hypoglycemic agents. Cefamandole, cefoperazone, cefotetan, valproic acid and increase the incidence plicamycin hypoprothrombinemia. Cyclosporine and preparations of gold increases the effect of diclofenac on the synthesis of prostaglandins in the kidneys, which increases the nephrotoxicity. Simultaneous with the appointment ethanol, colchicine, corticotropin, serotonin reuptake inhibitors and drugs St. John’s wort increases the risk of bleeding in the gastrointestinal tract. Diclofenac enhances the action of drugs that cause photosensitization. Drugs that block tubular secretion, increase the concentration of diclofenac in plasma, thereby increasing its toxicity. Antibacterial drugs from the group of quinolone – the risk of seizures. Effect on lab results: Diclofenac may affect the performance of serum transaminases (if this effect is long-term or if there are complications, treatment should be stopped), and may also cause an increase in potassium concentration.
Overdose
symptoms:
Dizziness, headache, hyperventilation, dizziness, children – myoclonic seizures, nausea, vomiting, abdominal pain, bleeding, abnormal liver function and kidney.
Treatment:
Activated carbon, symptomatic therapy. Forced diuresis, hemodialysis is not effective.
pharmachologic effect
Pharmacological group:
Nonsteroidal anti-inflammatory drug.
Pharmacological properties:
Nonsteroidal anti-inflammatory drug, a derivative of phenylacetic acid; anti-inflammatory, analgesic and antipyretic effect. Non-selectively inhibiting cyclooxygenase 1 and cyclooxygenase 2 gives the metabolism of arachidonic acid, reduces the amount of prostaglandins in inflammation. Most effective for pain of inflammatory nature. Like all non-steroidal anti-inflammatory drugs, the drug has antiplatelet activity.
Pharmacokinetics:
Maximum concentration in plasma is created within 30 – 40 minutes and stored in a linear dependence on the dose used. Changes in the pharmacokinetics of diclofenac on the background of multiple doses is not marked, not accumulates. Relationship to plasma proteins – more than 99% (most associated with albumin). Penetrates into the synovial fluid. The maximum concentration observed in the synovial fluid for 2 – 4 hours later than in plasma. The half-life of synovial fluid 3 – 6 hours (concentration of the active agent in the synovial fluid after 4 – 6 h after administration is higher than in the plasma, and remains higher for a further 12 hours). The relationship of drug concentration in synovial fluid from the clinical efficacy of the drug is not clear. Metabolism occurs as a result of single or multiple hydroxylation and conjugation with glucuronic acid. The metabolism of the drug is involved enzyme system P450 CYP2C9. The pharmacological activity of the metabolites is lower than diclofenac.
Systemic clearance is 350 ml / min, the volume of – 550 ml / kg. . The half-life of plasma-WE-2 hr 65% of the administered dose excreted by the kidneys as metabolites; less than 1% is excreted in unaltered form, the remainder of the dose excreted in bile as metabolites.
In patients with renal failure (less than 10 ml / min creatinine clearance) increases the excretion of metabolites in the bile, thus increasing their concentration in the blood is not observed. In patients with chronic hepatitis or compensated cirrhosis pharmacokinetic parameters of diclofenac are not changed. Diclofenac passes into breast milk.
Conditions of supply of pharmacies
By prescription.
side effects
Often – 1 – 10%; sometimes – 0.1 – 1%; rarely – 0.01 – 0.1%; very rarely – less than 0.001%, including some cases.
From the digestive system: often – epigastric pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, increased transaminases; rare-gastritis, proctitis, bleeding from the gastrointestinal (vomiting blood, melena, bloody diarrhea), gastrointestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, liver dysfunction; rarely, stomatitis, glossitis, esophageal injuries, bowel diafragmopodobnye stiktury (nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn’s disease), constipation, pancreatitis, fulminant hepatitis, exacerbation of hemorrhoids.
From the nervous system: often – headache, dizziness; rarely, drowsiness; very rarely – a violation of the sensitivity, including paresthesia, memory disturbances, tremors, convulsions, anxiety, cerebrovascular disorders, aseptic meningitis, confusion, depression, insomnia, night “nightmares”, irritability, personality disorders.
From the senses: common – vertigo; very rarely – blurred vision (blurred vision, diplopia), impaired hearing, tinnitus, taste disturbance.
From the urinary system: very rarely – acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.
From the side of hematopoiesis: rarely – thrombocytopenia, leukopenia, hemolytic and aplastic anemia, agranulocytosis.
Allergic reactions: anaphylactic / anaphylactoid reactions including marked decrease in blood pressure and shock; rarely, angioneurotic edema (including face).
With the cardiovascular system: very rarely – palpitations, chest pain, high blood pressure, vasculitis, heart failure, myocardial infarction.
The respiratory system: rarely – bronchial asthma (including shortness of breath); very rarely – pneumonitis.
For the skin: often – skin rash; rarely – urticaria; very rare – bullous rash, eczema, including multiforme and Stevens-Johnson syndrome, Lyell syndrome, exfoliative dermatitis, itching, loss of hair, photosensitivity, purpura, including allergic.
Local reactions at the rectal: mucosal irritation rectal mucus mixed with blood, painful defecation, rectal bleeding.
special instructions
Due to the importance of prostaglandins in maintaining renal blood flow should be particularly careful when administered to patients with cardiac or renal insufficiency as well as in the treatment of elderly patients taking diuretics, and patients who for some – any reason reduction of circulating blood volume is observed (eg after major surgery). If in such cases, prescribe diclofenac, is recommended as a precautionary measure to monitor renal function. In patients with hepatic impairment (chronic hepatitis, compensated cirrhosis), the kinetics and metabolism did not differ from similar processes in patients with normal liver function. During long-term therapy is necessary to monitor liver function, peripheral blood picture, analysis of fecal occult blood.
The treatment period may reduce the rate of mental and motor reactions, so you must refrain from driving vehicles and occupation of other potentially hazardous activities that require high concentration and psychomotor speed reactions.
Storage conditions
Store at a temperature not higher than +20 ° C. Keep out of the reach of children.
Dosing and Administration
Rectally, adult starting dose of 100 mg / day divided in 2 doses; in mild cases and in long-term therapy – 50 mg / day; In addition to ingestion, the total daily dose (orally and rectally) should not exceed 150 mg.
When algodismenoree (when the first symptoms), the initial dose of 50 – 100 mg / day which, if necessary, increase for several menstrual cycles to 150 mg.
Migraine – 100 mg at the first sign of attack. If necessary – re 100mg. If necessary, further treatment in the next days the daily dose should not exceed 150 mg for several administrations. Adolescents over 15 years – no more than 1 suppository.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist