medicalmeds.eu Medicines The means influencing a musculoskeletal system. Candle diclofenac 0,1 No. 10

Candle diclofenac 0,1 No. 10

Препарат Диклофенак свечи 0,1 №10. ЗАО "Лекхим-Харьков" Украина

Producer: CJSC Lekhim-Kharkiv Ukraine

Code of automatic telephone exchange: M01A B05

Release form: Firm dosage forms. Suppositories rectal.

Indications to use:

General characteristics. Structure:

International and chemical names: diclofenac (diclofenac); sodium salt 2-[(2,6 dichlorophenyl) - amine] phenylacetic acid; Main physical and chemical properties: suppositories from color, white to white with a yellowish or creamy shade, a cigar-shaped form. Existence of a plaque on the surface of suppository is allowed. Structure: 1 suppository contains sodium of diclofenac 100 mg; excipients: solid fat.

Pharmacological properties:

Pharmacodynamics. Antiinflammatory, analgetic, antipyretic. The mechanism of action is caused by suppression of biosynthesis of prostaglandins by cyclooxygenase inhibition, reduction of formation of kinin and other mediators of an inflammation and pain, the stabilizing influence on lizosomalny membranes. At rheumatic diseases reduces hypostasis, a hyperemia and a rest pain and at the movement, morning constraint and a swelling of joints, improving their functional capacity. Facilitates migraine attacks.

Pharmacokinetics. At rectal use diclofenac is well adsorbed in a system blood stream. Linkng with proteins of plasma makes more than 99%. The maximum concentration in blood is reached within 1 hour after introduction, i.e. quicker, than at diclofenac use orally (2-4 hours). The metoksilirovaniya and glyukuronization with formation of several phenolic metabolites is exposed to biotransformation in a liver by a hydroxylation. The elimination half-life makes 1-2 hours. It is removed by kidneys (about 65%) and with bile (about 35%) in the form of inactive connections with glucuronic and sulfuric acids; less than 1% are excreted in not changed form.

Features of pharmacokinetics of diclofenac at patients with the chronic hepatitis compensated by cirrhosis are not observed. At patients with a renal failure, at observance of the recommended mode of dosing, cumulation of diclofenac in an organism is not noted. At clearance of creatinine less than 10 ml/min. of concentration of hydroxymetabolites of diclofenac are about 4 times higher, than at healthy volunteers, at the same time metabolites are removed only with bile.

Indications to use:

The pseudorheumatism ankylosing a spondylarthritis, acute gouty, infectious, psoriasis and traumatic arthritises, osteoarthroses, a bursitis, a tendovaginitis, radiculitises, thrombophlebitises, neuralgia, mialgiya, a posttraumatic inflammation of muscles, joints, sinews and sheaves (stretchings, bruises), a post-operational edematous pain syndrome and also as symptomatic therapy of other diseases which are followed by an inflammation and pain.

Route of administration and doses:

The adult appoint on 1 suppository (100 mg of diclofenac) rektalno 1 time a day. Having exempted suppository from planimetric packaging, it is entered into a rectum after an enema or spontaneous bowel emptying. After introduction it is necessary to be in a prone position within 20–30 minutes.

At inflammatory diseases use of suppositories can be combined with reception of diclofenac in the form of tablets, at the same time the total daily dose of drug should not exceed 150 mg of diclofenac.

Duration of a course of treatment is established individually taking into account efficiency and portability of therapy.

Features of use:

With care appoint the patient with acute inflammatory diseases of a rectum and an anus, diseases of a liver, kidneys, digestive tract in the anamnesis, inborn disturbances of a hemopoiesis, at arterial hypertension, heart failure, to patients of advanced age.

During treatment by diclofenac it is necessary to control the level of transaminases and other enzymes of a liver for the first 4 weeks from the beginning of therapy.

At emergence of by-effects from the central nervous system (drowsiness, etc.) or an organ of sight to patients should refuse control of vehicles or work with mechanisms.

Side effects:

From digestive tract: pains in epigastric area, nausea, vomiting, diarrhea, spasms in a stomach, dyspepsia, a meteorism, anorexia; seldom – the latent or macroscopically visible gastrointestinal bleeding, digestive tract erosive cankers, increase in level of hepatic transaminases, hepatitis; in some cases – aphthous stomatitis, a glossitis, injuries of a gullet, emergence of diafragmopodobny strictures in intestines, perforation of intestines, fulminant hepatitis, frustration from distal department of a large intestine: nonspecific hemorrhagic colitis, exacerbation of ulcer colitis or disease Krone, locks, pancreatitis.

From the central and peripheral nervous system: a headache, dizziness, it is rare - drowsiness; very seldom – sensitivity disturbances, including paresthesias, dysmnesias, a disorientation, sleeplessness, irritability, spasms, a depression, feeling of alarm, a tremor, psychotic reactions, aseptic meningitis.

From sense bodys: very seldom – vision disorders (sight misting, a diplopia), a hearing disorder, a sonitus, disturbance of flavoring feelings.

From cardiovascular system: seldom – hypostases, in some cases - a heart consciousness, pains in heart, increase in arterial pressure, aggravation of congestive heart failure.

From an urinary system: very seldom – an acute renal failure, a hamaturia, a proteinuria, intersticial nephrite, a nephrotic syndrome, a papillary necrosis.

From system of a hemopoiesis: seldom – thrombocytopenia, a leukopenia, hemolitic anemia, aplastic anemia, an agranulocytosis.

Dermatological reactions: itch, rash; seldom – a small tortoiseshell; in some cases – violent reactions, eczema, a multimorfny erythema, Stephens-Johnson's syndrome, a toxic epidermal necrolysis (Lyell's disease), an erythrosis, a hair loss, a photosensitization, a purpura, including allergic.

Allergic reactions: reactions of local irritation are possible (burning, an itch in anorectal area), it is rare - a bronchospasm, reactions of immediate hypersensitivity (including anaphylactic and anaphylactoid, including hypotension), in some cases – a vasculitis, a pneumonitis.

Interaction with other medicines:

At simultaneous use of drugs of lithium, digoxin and Phenytoinum increase in concentration of the last in plasma is possible. Acetylsalicylic acid can reduce concentration of diclofenac in a blood plasma.

Diclofenac can weaken action of anti-hypertensive means and diuretics. The accompanying use of kaliysberegayushchy diuretics can lead to increase in level of serumal potassium. At purpose of a similar combination therapy it is necessary to control potassium level in blood.

At simultaneous use of diclofenac with other non-steroidal anti-inflammatory drugs or corticosteroids the risk of development of erosive cankers and bleedings in digestive tract increases.

It is necessary to avoid the combined use of drug with anticoagulants, fibrinolitika, antiagregant in connection with increase in risk of development of bleedings.

At simultaneous use of diclofenac and peroral hypoglycemic means separate cases of development of a hypoglycemia and a hyperglycemia at which dose adjustment of hypoglycemic drugs was required are described.

At simultaneous use diclofenac can increase toxicity of cyclosporine and a methotrexate.

The patients accepting at the same time non-steroidal anti-inflammatory drugs and hinolonovy antibacterial drugs have single messages on developing of spasms.

Contraindications:

Inflammatory diseases of a rectum, hemorrhagic colitis, exacerbation of hemorrhoids, rectal or proctal bleeding (including in the anamnesis), a peptic ulcer of a stomach or intestines, disturbance of a hemopoiesis of not clear etiology, bronchial asthma, including in the anamnesis, pregnancy, the breastfeeding period, age up to 18 years, the increased individual sensitivity to diclofenac and other non-steroidal anti-inflammatory drugs and/or components of drug.

Overdose:

At exceeding of the recommended doses frustration from TsNS are possible (the headache, dizziness, a loss of consciousness, are also possible abdominal pains, nausea, vomiting, bleedings of a digestive tract, a renal failure, a liver). Treatment: drug withdrawal, washing of a rectum, symptomatic therapy. There is no specific antidote.

Storage conditions:

In the place protected from light, at ^{a temperature from +8 ° C} to + 15 ^{° C}. To store in the place, unavailable to children. A period of validity – 2 years.