Diclovit

Diclovit exhibits analgesic, anti-inflammatory, antiplatelet, and antipyretic activity.

The main principle of the drug's action is the suppression of COX-1 and COX-2 activity. As a result, a disorder of arachidonic acid metabolism occurs. At the same time, the binding of PG in the inflammation zone is weakened. This causes a decrease in pain during movement or at rest. In addition, swelling and stiffness of joints in the morning go away. The drug increases the joint range of motion.

Indications Diclovita

It is used to treat the following disorders:

• lumbago and lumbodynia;
• lesions of the musculoskeletal system that have degenerative or inflammatory activity;
• periarthritis of the shoulder-scapular nature;
• neuralgia or bursitis;
• trismus, swelling, inflammation or pain associated with gynecological, dental, orthopedic and other procedures;
• synovitis or myalgia;
• pain associated with injuries or operations;
• tendovaginitis;
• migraine attacks;
• colic.

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

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Release form

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

Pharmacodynamics

The medication reduces pain that occurs after operations or injuries, and along with this, the intensity of inflammation. Reduces pain and bleeding that develop in the case of primary algomenorrhea.

Pharmacokinetics

Absorption.

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

Bioavailability.

As with oral administration of the drug, after using suppositories, the AUC values are approximately half of the level when administering a parenteral portion. With repeated use of the drug, the pharmacokinetic characteristics do not change. If the prescribed dosages are observed, the drug does not accumulate.

Distribution processes.

Intraplasmic protein synthesis is 99.7%; the substance mainly binds to albumins – 99.4%.

Diclofenac penetrates into the synovium, reaching Cmax values later than in the blood plasma (by 2-4 hours). The imaginary half-life from the synovium is 3-6 hours. After 2 hours from reaching the plasma Cmax level, diclofenac values in the synovium remain higher than in the blood plasma; this indicator is maintained for 12 hours.

Small amounts of the drug (100 ng/ml) are found in breast milk. The estimated volume of the substance entering the body of a breastfed child with milk is equivalent to a portion of 0.03 mg/kg per day.

Exchange processes.

Metabolism of Diclovit is partly realized through glucuronidation of the original molecule, but mainly develops with multiple and single methoxylation with hydroxylation, resulting in the formation of several metabolic elements of the phenolic type, most of which create conjugates that are combined with glucuronic acid. Bioactivity has 2 metabolic components, but it is significantly lower than that of diclofenac.

Excretion.

Systemic plasma clearance of the drug is 263±56 ml per minute (mean level±SD). The terminal intraplasmic half-life is 1-2 hours. The half-life of the 4 metabolic components, including 2 pharmacoactive ones, is also short and is 1-3 hours.

Approximately 60% of the dose is 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 the drug is excreted unchanged. The remainder of the dose is excreted in the feces in the form of metabolic elements.

Dosing and administration

Schemes for using suppositories.

The medication can be used by teenagers over 15 years of age and adults. Suppositories are inserted into the rectum after defecation or a cleansing enema. After inserting the suppository, you need to lie down for 20-30 minutes. The procedure must be performed twice a day. No more than 3 rectal suppositories can be inserted per day.

The duration of the treatment cycle is selected individually, taking into account the patient’s tolerance of the medication, as well as the nature of the disease.

Application of gel.

The gel is used for external treatment - a strip of 1-2 cm should be applied to the inflamed area 2-3 times a day. The substance is rubbed in with gentle movements until the gel is completely absorbed. The entire treatment cycle should last a maximum of 14 days. The duration of therapy can only be increased with a doctor's prescription. After the procedure, it is necessary to wash your hands.

Mode of use of capsules.

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

Children over 6 years of age can be administered no more than 2-3 mg/kg of Diclovit.

The duration of taking the capsules is selected individually by the attending physician.

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Use Diclovita during pregnancy

It is prohibited to prescribe Diclovit during pregnancy.

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Contraindications

Main contraindications:

• severe intolerance to the components of the drug or other NSAIDs;
• hematopoietic disorders of unknown origin;
• aspirin-type asthma;
• ulcer in the gastrointestinal tract in the active phase;
• active stage of development of lesions of the gastrointestinal tract, which have an erosive-ulcerative form;
• "aspirin" triad.

Caution is required when used during active phase of induced liver porphyria, and also in case of renal or hepatic dysfunction.

Side effects Diclovita

Main side effects:

• gastrointestinal disorders: gastralgia, constipation, vomiting, ulcerative colitis in the active phase, stomach pain, bleeding in the gastrointestinal tract and anorexia. In addition, nausea, bloating, acute hepatitis, dyspepsia, non-specific colitis accompanied by bleeding, pancreatitis, active phase of regional enteritis, hepatitis and increased activity of liver transaminases;
• urinary dysfunction: acute renal failure, proteinuria, nephrotic syndrome, hematuria, as well as necrotic papillitis and tubulointerstitial nephritis;
• Epidermal infections: eczema, bullous rash, exfoliative dermatitis, rashes, alopecia, photosensitivity, purpura and erythema multiforme;
• disorders affecting the nervous system: paresthesia, diplopia, nightmares, headaches, depression and increased fatigue, as well as tinnitus, disorientation, dizziness, insomnia and irritability. In addition, confusion, psychotic symptoms, seizures, taste disorders, memory loss, anxiety, decreased auditory and visual acuity, and tremor;
• problems with hematopoiesis: agranulocytosis, leukopenia or thrombocytopenia, as well as hemolytic or aplastic anemia;
• allergic symptoms: urticaria, TEN, SJS, bronchial spasms, allergic purpura and anaphylactic symptoms;
• others: pain in the chest area, impotence, swelling, increased blood pressure and palpitations;
• local symptoms: irritation in the area of the colon mucosa, bloody mucous discharge, and pain during defecation.

Side effects depend on the individual characteristics of the patient, portion sizes and duration of therapy.

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Overdose

Intoxication when administering suppositories is unlikely. Using too much of the drug can lead to dizziness, clouding of consciousness, hyperventilation, headaches and negative manifestations associated with the gastrointestinal tract. The child may develop nausea, abdominal pain, vomiting, myoclonic seizures and renal or hepatic dysfunction.

In case of accidental ingestion of the drug, it is necessary to perform gastric lavage and give the patient activated carbon. After this, various symptomatic measures are carried out.

Interactions with other drugs

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

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

Combination with cyclosporine leads to an increase in its toxic effect on the kidneys. Hypoglycemic drugs, when used simultaneously with the drug, can lead to hyper- or hypoglycemia. Because of this, with such therapy, it is necessary to regularly monitor blood sugar levels.

Administration of the drug together with methotrexate (within 24 hours before or after its use) may lead to an increase in the latter's values and potentiation of its toxic activity.

Use together with anticoagulants requires constant monitoring of blood clotting processes.

Storage conditions

Diclovit must be stored at temperatures no higher than 25°C.

Shelf life

Diclovit in the form of suppositories can be used for a 24-month period from the date of sale of the drug. The shelf life of capsules and gel is 36 months.

Application for children

The medication is not used in persons under 6 years of age.

Analogues

The analogs of the drug are Ortofen, Dicloran, Almiral with sodium diclofenac, Rapten with Dicloberl, and in addition Diclogen, Diclac, Naklofen, Diclo-F with Voltaren and Olfen.

Reviews

Diclovit usually receives good reviews from patients. People who have used it in different dosage forms talk about the fast and effective effect of the medicine. Among the advantages, they note that the drug is capable of simultaneously having several effects - eliminating inflammation and swelling, relieving pain, etc.

But in the comments regarding suppositories used in gynecology, there are sometimes reports of personal sensitivity to the drug, but the negative symptoms quickly disappear after reducing the dose.

The only drawback of the gel is the need to rub it in for a long time until it is completely absorbed.