Dicklovit

Diklovit demonstrates analgesic, anti-inflammatory, anti-aggregation, as well as anti-pyretic activity.

The main principle of the effect of the drug is the suppression of COX-1 and COX-2 activities. As a result, arachidonic acid metabolism is disturbed. At the same time, the weakening of PG binding in the area of inflammation is also carried out. This causes a weakening of the pain when moving or at rest. In addition, swelling, as well as stiffness of the joints in the morning, goes away. The drug increases motor articular volume.

Indications Dicklovita

It is used to treat such disorders:

• lumbago and lumbodynia;
• ODA lesions with degenerative or inflammatory activity;
• periarthritis of the humeroscapular character;
• neuralgia or bursitis;
• Trisms, puffiness, inflammation or pain associated with gynecological, dental, orthopedic, and other procedures;
• synovitis or myalgia ;
• pain related to injuries or surgeries;
• tendovaginitis;
• migraine attacks;
• colic.

In gynecology, suppositories are used - with adnexitis, primary dysmenorrhea and perimetric. At the same time, the drug can be used as an additional component of complex therapy for pathologies affecting the ENT system (with inflammatory and infectious activity), accompanied by severe pain.

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Release form

The release of the therapeutic substance is in the form of a gel, suppositories and capsules.

Pharmacodynamics

The drug alleviates pains that occur after surgery or injury, and with it the intensity of inflammation. Reduces pain and bleeding that develop in the case of primary algomenorrhea.

Pharmacokinetics

Absorption.

Suppository absorption occurs at high speed, but more slowly than when taking enteric tablets. When using suppositories in a 50 mg dose, plasma Cmax values are noted after 60 minutes, but the maximum values per unit dose are approximately 2/3 of the concentration obtained using enteric tablets (1.95 ± 0.8 μg / ml)

Bioavailability.

As with the administration of the drug inside, after the use of suppositories, the AUC values are equal to about half of the level when the parenteral dose is administered. With repeated use of drugs pharmacokinetic characteristics do not change. At observance of the appointed dosages the medicine does not accumulate.

Distribution processes.

Intlasma protein synthesis equals 99.7%; mainly substance is associated with albumin - by 99.4%.

Diclofenac passes inside synovia, reaching Cmax values later than inside blood plasma (2-4 hours). The imaginary term half-life of synovia is 3-6 hours. After 2 hours after reaching the plasma Cmax level, the values of diclofenac inside the synovium remain higher than inside the blood plasma; This indicator persists for 12 hours.

Small amounts of drugs (100 ng / ml) are noted inside the mother's milk. The estimated volume of a substance that enters the body of an infant with milk is equivalent to a portion of 0.03 mg / kg per day.

Exchange processes.

Diclovit metabolism is partly realized through the glucuronidation of the original molecule, but mainly develops with reusable and 1-time methoxylation with hydroxylation, resulting in several metabolic elements of the phenolic type, most of which create conjugates connected with glucuronic acid. Two metabolic components have bioactivity, but it is significantly lower than that of diclofenac.

Excretion.

Systemic indicators of plasma clearance of drugs are equal to 263 ± 56 ml per minute (mean level ± WITH). The final term of intra plasma half-life is equal to 1-2 hours. The term half-life of 4 metabolic components, among which 2 are pharmacoactive, is also short and equals 1-3 hours.

Approximately 60% of the portions are excreted in the urine in the form of conjugates, together with glucuronic acid of the intact molecule, and also in the form of metabolic components, most of which are transformed into glucuronide-type conjugates. Less than 1% of drugs excreted unchanged. The remainder of the portion is excreted with the faeces in the form of metabolic elements.

Dosing and administration

Suppository use schemes.

The drug is allowed to use in adolescents over 15 years of age and adults. Suppositories are inserted into the rectum after a bowel movement or a cleansing enema. After the introduction of the suppository, you need to lie down for 20-30 minutes. The procedure must be carried out twice a day. For the day, you can enter no more than 3 rectal candles.

The duration of the treatment cycle is selected individually, taking into account the patient's portability of the drug, as well as the nature of the disease.

The use of the gel.

The gel is used for external processing - a strip of 1-2 cm in size should be applied to the inflamed area 2-3 times per day. The substance is rubbed with weak movements until the gel is completely absorbed. The entire treatment cycle should last a maximum of 14 days. Increase the duration of therapy is possible only with the appointment of a doctor. After the procedure, you need to wash your hands.

Capsule mode

Capsules should be taken with food, washed down with plain water; the medicine is swallowed whole, without chewing. Usually use 1-na capsule of drugs 1-3 times a day, every day. An adult at the beginning of a cycle is usually prescribed 3 times daily. The size of the maintenance portion per day - 1 capsule 1-2 times.

Children older than 6 years old, you can enter no more than 2-3 mg / kg Diklovit.

The duration of the capsules is chosen personally by the attending doctor.

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Use Dicklovita during pregnancy

It is forbidden to appoint Diklovit during pregnancy.

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Contraindications

The main contraindications:

• severe intolerance to the elements of the drug or other NSAIDs;
• hematopoietic disorders of unidentified nature;
• asthma "aspirinovogo" type;
• ulcer in the gastrointestinal tract in the active phase;
• active stage of development of lesions of the gastrointestinal tract, having an erosive-ulcerative form;
• "Aspirin" triad.

Caution is required when using during the induced porphyria of the liver in the active phase, and in addition, when renal impairment or hepatic function is impaired.

Side effects Dicklovita

Main adverse events:

• lesions of the digestive activity: gastralgia, constipation, vomiting, ulcerative colitis in the active phase, stomach pain, bleeding in the gastrointestinal tract and anorexia. In addition, nausea, bloating, ultrafast hepatitis, dyspepsia, non-specific colitis, accompanied by bleeding, pancreatitis, the active phase of regional enteritis, hepatitis and increased liver transaminase activity;
• urinary function disorders: OPN, proteinuria, nephrotic syndrome, hematuria, as well as necrotic papillitis and tubulo-interstitial nephritis;
• epidermis infections: eczema, bullous rash, exfoliative type of dermatitis, rash, alopecia, photosensitivity, purpura and erythema multiforme;
• Disorders affecting NA: paresthesia, diplopia, nightmares, headaches, depression and increased fatigue, but also ear noise, loss of orientation, dizziness, insomnia and irritability. In addition, confusion, psychotic symptoms, convulsions, taste disorder, memory loss, anxiety, weakening of auditory and visual acuity, as well as tremor;
• problems with hematopoietic work: agranulocytosis, leuko- or thrombocytopenia, as well as anemia of a hemolytic or aplastic nature;
• allergic signs: urticaria, TEN, SSD, bronchial spasms, allergic purpura of nature and anaphylactic symptoms;
• others: pain in the sternum, impotence, swelling, increased blood pressure values and a feeling of heartbeat;
• local signs: irritation in the mucous membrane of the large intestine, bloody mucous discharge, and pain during bowel movements.

Adverse symptoms depend on the personal characteristics of the patient, the size of the portions and the duration of therapy.

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Overdose

Intoxication with the introduction of candles is unlikely. Use of too high portions of the medication can lead to dizziness, clouding of consciousness, hyperventilation, headaches and negative manifestations associated with the work of the gastrointestinal tract. A child may develop nausea, abdominal pain, vomiting, seizures of myoclonic type and impaired renal or hepatic function.

In case of unintentional intake of drugs inside, it is necessary to perform gastric lavage and give the patient activated carbon. After that, various symptomatic measures are carried out.

Interactions with other drugs

The drug increases plasma indicators of lithium substances and digoxin with phenytoin. It also slows down the activity of antihypertensive and diuretic drugs. Combination with diuretic substances of potassium-sparing type can lead to the appearance of hyperkalemia.

Combination with the GCS or other NSAIDs increases the risk of developing negative symptoms in the GI tract. Use together with aspirin causes a decrease in serum indicators of the active component Diklovit.

Combination with cyclosporine leads to increased toxic effects on the kidneys. Hypoglycemic drugs, when used concomitantly with the medication, can cause hyper- or hypoglycemia. Because of this, with such therapy, it is necessary to regularly monitor blood sugar values.

Drug administration with methotrexate (within 24 hours before or after its use) can lead to an increase in the values of the latter and to the potentiation of its toxic activity.

Use with anticoagulants requires constant monitoring of blood coagulation processes.

Storage conditions

Diklovit is required to be kept at temperature values not higher than the mark of 25 ° С.

Shelf life

Diklovit in the form of suppositories can be used throughout the 24-month term from the moment of drug implementation. Shelf life of capsules and gel - 36 months.

Application for children

The drug is not used in persons younger than 6 years.

Analogs

Analogues of drugs are the substances Ortofen, Dicloran, Almiral with Diclofenac sodium, Rapten with Dicloberl, and besides this Diclogen, Diklak, Naklofen, Diklo-F with Voltaren and Olfen.

Reviews

Diklovit usually receives good reviews from patients. People who used it in different dosage forms talk about the quick and effective effects of the drug. Of the merits of the note that the drug can simultaneously have several effects - eliminate inflammation and swelling, reduce pain and so on.

But in the comments on the suppositories used in gynecology, there are occasionally reports regarding personal sensitivity to the drug, but the negative symptoms quickly disappear after the reduction of the portion.

Of the disadvantages of the gel emit only the need for a long rubbing it - until it is fully absorbed.