Diklofenak-Altfarm

General characteristics. Structure:

Active ingredient: diclofenac of sodium of 25 mg, 50 mg, 100 mg.
Excipients: Vitepsol of N of 15 - 0,975 g; 1,95 g; 1,9 g.

Description: Suppositories from white to white with a creamy or yellowish shade of a torpedo-shaped form, without visible impregnations on longitudinal section.

Pharmacological properties:

Renders antiinflammatory, analgetic, febrifugal and anti-aggregation action.
Pharmacodynamics. Oppressing TsOG, breaks metabolism of arachidonic acid, reduces quantity of Pg both in the inflammation center, and in healthy fabrics, suppresses exudative and proliferative phases of an inflammation.
Reduces permeability of capillaries; stabilizes lizosomalny membranes; slows down production of ATP in processes of oxidizing phosphorylation; slows down synthesis or inactivates inflammation mediators (Pg, a histamine, bradykinins, limfokinina, complement factors, etc. nonspecific endogenous "disturbing factors"). Blocks interaction of bradikinin with fabric receptors, recovers the broken microcirculation and reduces painful sensitivity in the inflammation center. Causes delay of formation of proteoglycan in cartilaginous tissue. Analgetic action is caused by decrease in concentration of the biogenic amines having algogenny properties and increase in a threshold of painful sensitivity of the receptor device. Causes easing or disappearance of a pain syndrome of rheumatic and not rheumatic character (including at joint pains at rest and at the movement, reduction of morning constraint and a swelling of joints, promotes increase in volume of movements; at the inflammatory processes arising after operations and injuries quickly facilitates both spontaneous pain, and an oxycinesia, reduces inflammatory hypostasis on site of a wound; at primary algodismenorea weakens pain). At prolonged use has the disensibilizing effect. The antiinflammatory effect occurs by the end of the first week of treatment. Surpasses acetylsalicylic acid, Butadionum, an ibuprofen in antiinflammatory activity; at rheumatism and Bekhterev's disease it is equivalent to Prednisolonum and indometacin.

Pharmacokinetics. Absorption - bystry and full, food slows down absorotion speed. At rectal administration the maximum concentration of drug is reached in 30 min. Concentration in plasma is in linear dependence on size of the entered dose. Change of pharmacokinetics of diclofenac against the background of repeated introduction is not noted. Does not kumulirut at observance of the recommended interval between meals. Bioavailability - 50%. Communication with proteins of plasma - 95-98% (the most part contacts albumine). Gets into synovial fluid; the maximum concentration in synovial fluid is observed on 2-4 h later, than in plasma. Time of semi-removal from synovial fluid 3-6 of h (concentration of active agent in synovial fluid in 4-6 h after administration of drug is higher, than in plasma and remains higher during 12 h). Metabolism: 50% of active agent are exposed to metabolism during "the first passing" through a liver. Metabolism results from a repeated or single hydroxylation and a konyyugirovaniye with glucuronic acid. Pharmacological activity of metabolites - is less, than diclofenac. The system clearance makes 260 ml/min. of T1/2 of plasma - 1-2 h 60% of the entered dose vvyvoditsya in the form of metabolites through kidneys; less than 1% are removed in not changed look, other part of a dose is removed in the form of metabolites with bile. At patients with the expressed renal failures (glomerular filtering less than 10 ml/min.) removal of metabolites with bile increases, at the same time increase in their concentration in blood is not observed. At patients with chronic hepatitis or the compensated cirrhosis pharmacokinetic parameters of diclofenac same, as well as at patients without liver diseases.

Indications to use:

Inflammatory diseases of a musculoskeletal system (a pseudorheumatism, the psoriasis, juvenile and chronic arthritis ankylosing a spondylitis; gouty arthritis).
Degenartivny diseases of a musculoskeletal system (the deforming osteoarthrosis, osteochondrosis).
Lumbago, sciatica, neuralgia, mialgiya.
Diseases of extraarticular fabrics (tendovaginitis, bursitis, rheumatic defeat of soft tissues).
The posttraumatic pain syndromes which are followed by an inflammation, postoperative pains, migraine, renal or bilious colic; primary альгодисменорея, adnexitis, proctitis.
Infectious and inflammatory diseases of ENT organs with the expressed pain syndrome (pharyngitis, tonsillitis, otitis), the residual phenomena of pneumonia.
Feverish syndrome.

Route of administration and doses:

Apply rektalno (enter into a rectum). Wash up hands, exempt suppositories from planimetric packaging, having cut packaging by means of baskets on a contour, and enter into an anus the pointed end, whenever possible deeply. For more convenient administration of suppository it is recommended to bend down or sit down on hunkers.
Candles on 100 mg: the adult 1 candle of 1 times a day.
Candles on 50 mg: the adult 1 candle 2 times a day; to children 12 years 1-2 times a day are more senior.
Candles on 25 mg: the adult 1 candle 3-4 times a day; to children 12 years 1 candle 2-3 times a day are more senior.

Features of use:

At patients with a renal failure at KK less than 10 mg/min., Css of metabolites in plasma has to be theoretically much higher, than at patients with normal function of kidneys, however it really is not observed as in this situation removal of metabolites with bile amplifies.
At patients with a liver failure (chronic hepatitis, the compensated cirrhosis) the kinetics and metabolism do not differ from similar processes at patients with normal function of a liver. When performing long therapy it is necessary to control function of a liver, a picture of peripheral blood, the analysis a calla on the occult blood.
During treatment reduction of speed of mental and motor reactions therefore patients have to abstain from all types of activity requiring special attention, bystry mental and motor reaction is possible.

Side effects:

From the alimentary system: a gastralgia, nausea, vomiting, diarrhea, gastric colic, dyspepsia, a meteorism, anorexia, increase in activity of "hepatic" transaminases, gastrointestinal bleeding, a hematemesis, a melena, hepatitis with jaundice or without jaundice, fulminant hepatitis, pancreatitis, nonspecific colitis with bleeding, an exacerbation of ulcer colitis or disease Krone, aphthous stomatitis, a glossitis, an erosive esophagitis, a lock.
From a nervous system: headache, dizziness, increased fatigue, disturbances of perception, paresthesia, decrease in memory, loss of feeling of orientation, decrease in visual acuity, diplopia, decrease in hearing, sonitus, sleeplessness, irritability, spasms, depression, uneasiness, "dreadful" dreams, tremor, psychosomatic reactions, disturbance of flavoring feelings.
From skin: enanthesis, violent rashes, eczema, polymorphic erythema, erythrosis (exfoliative dermatitis), alopecia, photosensitization, purpura.
From an urinary system: acute renal failure, hamaturia, proteinuria, intersticial nephrite, nephrotic syndrome, papillary necrosis.
From bodies of a hemopoiesis: thrombocytopenia, leukopenia, agranulocytosis, hemolitic anemia, aplastic anemia.
Allergic reactions: a bronchospasm, a small tortoiseshell, Stephens-Johnson's syndrome, a toxic epidermal necrolysis (Layvll's syndrome), an allergic purpura, system anaphylactic reactions (including shock).
Others: hypostases, impotence, heartbeat, a stethalgia, increase in arterial pressure, Local irritation, mucous allocations with impurity of blood, pain at defecation.

Interaction with other medicines:

Increases concentration in plasma of digoxin, Li + and cyclosporine. Against the background of kaliysberegayushchy diuretics the risk of a hyperpotassemia, against the background of anticoagulants - risk of bleedings amplifies.
Reduces effects diuretic, hypotensive and hypnagogues.
Increases probability of emergence of side effects of NPVP and glucocorticoids (bleeding from digestive tract), toxicity of a methotrexate and nephrotoxicity of cyclosporine.
Acetylsalicylic acid reduces concentration of diclofenac in blood.
At simultaneous use with peroral antidiabetic drugs are possible both hypo - and a hyperglycemia.

Contraindications:

Hypersensitivity (including to other NPVP), GIT erosive cankers (in an aggravation phase), "aspirinovy" asthma, hemopoiesis disturbances, pregnancy, age up to 12 years, the lactation period, hemorrhoids, a proctitis.
With care - the induced acute hepatic porphyrias, heavy abnormal liver functions and kidneys, heart failure.

Overdose:

Symptoms: dizziness, a headache, a hyperventilation of lungs, consciousness opacification, children have myoclonic spasms, nausea, vomiting, pains in a stomach, bleedings, an abnormal liver function and kidneys.

Treatment: the symptomatic therapy directed to elimination of increase in the ABP, a renal failure, spasms, irritations of digestive tract, respiratory depression. The artificial diuresis, a hemodialysis are ineffective.

Storage conditions:

List B. In the place protected from light at a temperature not above 25 °C. To store in places unavailable to children. Period of validity: 2 years. Not to apply after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Suppositories on 5 pieces in a blister strip packaging, 2 planimetric packagings in a cardboard pack.