Diclac

Diclac belongs to the category of antirheumatic drugs, and is also a substance from the NSAID subgroup.

The composition of the drug contains an active medicinal component - sodium diclofenac. This substance has a pronounced non-sterile structure and is a derivative of α-toluic acid. Among the medicinal properties that this therapeutic component has: pronounced analgesic, antirheumatic, anti-inflammatory, and also antipyretic.

Indications Diclaca

The medication tablets are used for the following disorders:

• having inflammatory and, in addition, degenerative activity of pathologies of rheumatic origin (for example, osteoarthritis or rheumatoid arthritis);
• pain symptoms that occur in the spinal region;
• rheumatism affecting soft tissues (for example, of an extra-articular nature);
• attacks of gouty arthritis in the active phase;
• pain arising in connection with operations or injuries, against the background of which swelling and inflammation appear (including pain developing in connection with dental or orthopedic procedures);
• gynecological diseases during which pain and signs of inflammation appear (for example, primary dysmenorrhea or adnexitis);
• having severe pathologies affecting the ENT organs, against the background of which pain is observed (the drug is used as an auxiliary substance).

The intramuscular solution of the drug is used for the following disorders:

• rheumatic diseases that have an inflammatory or degenerative form (for example, rheumatoid arthritis or osteoarthritis);
• attacks of gouty arthritis (active stage);
• biliary pain;
• colic in the kidney area;
• pain caused by injuries, against the background of which tissue swelling and inflammation are observed;
• pain that occurs after surgery;
• migraine attacks that are severe.

The drug is administered intravenously to prevent or treat pain that develops after surgery.

The tablets are used in the following cases:

• rheumatism;
• elimination of pain after injuries or surgeries;
• painful conditions observed in some gynecological pathologies.

Rectal suppositories are prescribed in case of the following disorders:

• active or common inflammations in rheumatism with degenerative activity (for example, in the case of neuritis, polyarthritis, which has a chronic form, or neuralgia);
• lesions in the soft tissue area that have rheumatic etiology;
• pain associated with injuries or surgeries in which painful tissue swelling and inflammation are observed;
• pain of an inflammatory nature that has a non-rheumatic origin.

The gel is prescribed to eliminate pain symptoms, inflammatory manifestations and tissue edema in the following diseases:

• injuries of various natures that affect layers of soft tissue (including dislocations with muscle or tendon strains, hematomas, etc.);
• localized inflammations of rheumatic origin (for example, periarthropathy or tendinitis);
• localized types of rheumatism in which degenerative processes are recorded (for example, in the case of spinal or peripheral joint osteoarthritis).

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Release form

The medicinal substance is released in the form of:

• enteric-coated tablets (20 pieces each);
• liquids for intramuscular injections (3 ml ampoules, 5 pieces each);
• tablets with modified release of the active element (volume 0.075 and 0.15 g, 20 or 100 pieces);
• 5% gel (inside 50 or 100 g tubes);
• rectal suppositories (50 mg, 10 pieces).

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Pharmacodynamics

Diclofenac has the following therapeutic effects:

• inhibits the activity of the COX enzyme, which is involved in the binding of prostanoids, and also in the cascade of metabolic effects of arachidonic acid;
• inhibits the biosynthesis of PG, which are the main causative agents of developing inflammation, fever and pain;
• strengthens capillary strength;
• stabilizes lysosomal walls;
• inhibits platelet aggregation that develops under the influence of the nucleotide ADP, as well as collagen (fibrillar protein).

The use of diclofenac Na helps to improve the motor activity of joints affected by the disease, increases their range of motion and reduces the severity of pain during movement and at rest.

In vitro tests performed using the active element of the drug in doses similar to those used in the treatment of patients demonstrated that the drug does not lead to the inhibition of proteoglycan biosynthesis within cartilage tissue.

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Pharmacokinetics

After oral administration of enteric-coated tablets, the active component of the drug is fully and rapidly absorbed from the gastrointestinal tract. Food affects the rate of absorption (it slows down), but the volumes of the absorbed element remain the same.

When a dose of 75 mg of the substance is injected intramuscularly, its absorption begins immediately. In this case, plasma Cmax values of 2.5 μg/ml are recorded after 20 minutes from the moment the procedure is performed.

Linearity is observed between the volumes of the absorbed component and the dose size of the drug.

The AUC values after an intramuscular injection or intravenous injection are approximately twice as high as the values observed after rectal or oral administration of the drug. This is due to the fact that with the latter method of administration, approximately 50% of the element is involved in metabolic processes with the first intrahepatic passage.

When the drug is used repeatedly, its pharmacokinetic properties do not change. Compliance with the prescribed intervals between drug administrations allows avoiding the accumulation of its active element inside the body.

When taken orally, the drug is fully absorbed in the gastrointestinal tract. It reaches the plasma level Cmax in the period of 1-16 hours from the moment of administration of the drug (on average, the drug reaches peak values after 2-3 hours from the moment of use).

After entering the body, the substance is almost completely (99.7%) synthesized with intraplasmic protein (mostly with albumins). The distribution volume indicator is in the range of 120-170 ml/kg.

Diclofenac levels inside the synovium located in the joint cavity after oral administration of Diclac tablets are recorded after 3-6 hours; when the drug is administered by injection - after 2-4 hours.

The half-life of the component from the synovium fluctuates in the range of 3-6 hours.

After 2 hours from the moment of reaching plasma Cmax, diclofenac values inside the synovium increase above plasma values and this effect continues to be maintained within the next 12 hours.

After taking a tablet, about 50% of a single dose of the drug is involved in the first intrahepatic passage. Only 35-70% of the absorbed element is unchanged during posthepatic circulation.

Partial biotransformation of the component occurs during glucuronidation of the initial molecule, but mostly during methoxylation and hydroxylation processes.

These processes lead to the formation of several phenolic metabolic elements (only two of them demonstrate bioactivity, but it is still weaker than the effect of the original element).

The half-life of the drug is 1-2 hours, and this indicator is not affected by the functional state of the liver or kidneys.

The plasma level of total clearance of Diclac is in the range of 207-319 ml per minute.

Excretion of the majority of the drug (about 60%) is carried out through the kidneys in the form of metabolic components; less than 1% of the drug is excreted unchanged, and the remainder is excreted with bile in the form of metabolic elements.

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Dosing and administration

In case of using any form of release of the medicine, the dosage is determined individually, using the minimum, having a positive clinical effect. At the same time, the duration of the treatment cycle should also be as short as possible.

Enteric-coated tablets of Diclac.

The drug is used in adolescents from 15 years of age and adults. At first, it is necessary to use 0.1-0.15 g of the medicinal substance per day.

In mild cases of the disease, and in addition to this, if there is a need for long-term therapy, 75-100 mg of the substance should be used per day. This dosage should be divided into 2-3 applications.

If necessary, 75 mg of the drug is used. A maximum of 0.15 g of diclofenac can be consumed per day.

In case of primary dysmenorrhea, a dose of 0.05-0.15 g of the drug is used. In these cases, at the initial stage of therapy, the dosage may fluctuate in the range of 0.05-0.1 g. If there is a need to increase the dose, this procedure is performed during several menstrual cycles, but at the same time, per day it can be a maximum of 0.2 g.

The use of the drug should be started after the development of the first signs of pain syndrome. The duration of the treatment cycle is determined by the intensity of clinical symptoms and is often no more than a few days.

The tablets are taken before meals, without chewing and washed down with plain water (1 glass).

Use of injection fluid.

The portion is selected individually, taking into account the characteristics of the disease. The therapeutic course should last the minimum possible number of days, in the minimum effective portion.

Intramuscular injections are allowed to be carried out for a maximum of 2 days in a row. Then, if pain relief is needed, the therapy is continued using tablets.

During the day, 75 mg of diclofenac Na (corresponds to 1 ampoule of the drug) can be administered via intramuscular injections. The needle for injections is inserted deep into the outer upper region of the gluteal muscle.

In extremely severe conditions, during which severe pain is observed, it is allowed to double the daily dose of the medicine. It is necessary to maintain a break of at least several hours between injections. The drug is injected alternately into different muscles of the buttocks (left, then right).

An alternative therapeutic regimen can also be used, when instead of the second injection, diclofenac Na is administered in a different form of release. The dose should be calculated so that in total it does not exceed 0.15 g per day.

In case of migraine attacks, an injection of the drug in a dosage of 75 mg should be given as quickly as possible. In addition, on the same day, it is possible to administer rectal suppositories of Diclac (0.1 g per day). During the first day, with such a scheme, it is necessary to use a maximum of 175 mg of the substance.

Infusion is usually performed by bolus method. Taking into account the duration of the procedure, the liquid from the 1st ampoule of the drug is mixed with 0.9% NaCl or 5% glucose liquid; this combination also includes 8.4% infusion liquid (sodium bicarbonate). The volume of the solvent used is 0.1-0.5 l of the substance. Only transparent solvent liquids can be used.

In case of severe or moderate pain that occurs after operations, the patient requires an injection of 75 mg of the drug. Such an infusion lasts within 0.5-2 hours.

If necessary, the procedure can be repeated after several hours. It should not be forgotten that the patient can be administered no more than 0.15 g of the drug per day.

For prophylaxis after the surgical procedure, after 15-60 minutes, the patient is given 25-50 mg of the drug (loading dose of the drug). Then, a continuous infusion is performed (at a maximum rate of 5 mg/hour) until a volume of 0.15 g of the drug is obtained.

Tablets with modified release form.

At first, patients take 75-150 mg per day (1 or 2 tablets, depending on the severity of pain).

If long-term therapy is required, 75 mg of the drug should be administered per day.

For people whose symptoms of the disease mainly occur in the morning and at night, the medication is prescribed to be taken at night, before bedtime.

A maximum of 0.15 g of Diclac is allowed per day. Such a treatment course should last a maximum of 14 days. The duration of the course should be selected by the attending physician, taking into account the patient's condition and clinical picture.

The tablets must be swallowed whole, without crushing them first; the medicine should be washed down with a glass of plain water. It is recommended to take the medicine with food.

Use of medicinal suppositories.

The drug should be administered to adults. Different treatment regimens are used - once a day in a dose of 0.1 g of the substance, twice a day in a dosage of 50 mg, or 3-4 times a day in a dose of 25 mg.

It is allowed to use no more than 0.15 g of the medication per day.

For children over 12 years of age, suppositories are administered at 0.05-0.1 g in 1 or 2 applications, and also at 75 mg in 2 or 3 applications.

Application of the substance in the form of a gel.

The medicine is applied to the skin 2-3 times a day in the volumes required to treat the inflamed area. For example, 2-4 g of the medicine is enough to treat an epidermis area of 0.4-0.8 m2 ^. The application is carried out in a thin layer, with light rubbing of the substance into the epidermis.

After finishing the treatment procedure, you need to wash your hands thoroughly using soap. The only exception is situations when the substance is applied specifically to this area of the hands.

It is allowed to use the gel in combination with iontophoresis procedures. This method of application ensures deeper penetration of the substance into the epidermis with a more intense medicinal effect. The medicine should be applied under the electrode with a negative charge.

The duration of the treatment cycle is selected taking into account information about the effectiveness of the therapy. Basically, it is 10-14 days. Taking into account the person's health condition, a second course may be prescribed (but it can be carried out at least after 2 weeks from the end of the first one).

In case of damage in the soft tissue area (also of rheumatic origin), the gel is used for a maximum of 14 days. Therapy for people whose pain is caused by the development of arthritis lasts 21 days (unless the attending physician has prescribed a different duration).

When using the medicine without a doctor's prescription, if a person does not experience improvement after 7 days of therapy, it is necessary to consult a doctor.

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Use Diclaca during pregnancy

It is prohibited to use the drug during breastfeeding and in the 3rd trimester.

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Contraindications

The main contraindications for the solution, tablets and suppositories:

• strong personal sensitivity to diclofenac or other components of the drug;
• an ulcer affecting the gastrointestinal tract in the active phase;
• bleeding developing in the gastrointestinal tract;
• gastric or intestinal perforation;
• severe failure of the heart, kidneys or liver;
• a disorder of hematopoiesis processes with an unknown etiology.

It is prohibited to use Diclac to people who develop signs of urticaria and acute rhinitis, as well as asthma attacks when using aspirin or other NSAIDs.

Rectal suppositories should not be used in individuals with manifestations of proctitis (inflammation in the rectum).

The gel is not used in the following cases:

• increased personal intolerance to diclofenac or auxiliary components of the drug;
• the presence in the patient's medical history of urticaria, asthma attacks, and acute rhinitis;
• polyps inside the nose (also present in the anamnesis);
• history of Quincke's edema;
• severe intolerance associated with analgesic substances (including antirheumatic drugs).

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Side effects Diclaca

Forms of the drug taken orally may cause the following side effects:

• disorders associated with the functioning of the circulatory system and lymph: anemia of various types (hemolytic or aplastic) occurs sporadically, or the volume of platelets, leukocytes, or neutrophilic granulocytes decreases;
• immune disorders: occasionally, symptoms of intolerance, anaphylactoid manifestations or Quincke's edema appear;
• mental disorders: nightmares, depression, spatial disorientation, increased irritability and various psychotic problems are occasionally observed;
• problems with the functioning of the nervous system: dizziness or headaches often occur. Occasionally, severe drowsiness appears. Disturbances of taste or sensitivity, memory disorders, tremors, aseptic meningitis, nightmares, cerebral blood flow disorders and severe irritability develop sporadically;
• visual manifestations: occasionally double vision, blurred vision or visual disturbances occur;
• auditory impairment: vertigo often appears. Hearing impairment and tinnitus are observed sporadically;
• problems with cardiac activity: occasional pain affecting the sternum, increased heart rate, myocardial infarction or signs of developing heart failure;
• disorders affecting the functioning of blood vessels: vasculitis or increased blood pressure are observed occasionally;
• symptoms related to the respiratory organs: asthma attacks (including dyspnea) and manifestations of bronchospastic syndrome are occasionally observed. Lesions of the interstitial lung tissue or alveolar walls develop sporadically, against the background of which fibrosis is observed;
• Gastrointestinal and digestive system lesions: abdominal pain, anorexia symptoms, dyspeptic disorders, vomiting, increased bloating and nausea are often observed. Rarely, gastrointestinal bleeding, gastritis, bloody diarrhea or vomiting with blood, gastrointestinal ulcers (in which case bleeding or perforation may develop) and melena occur. Colitis (its hemorrhagic or ulcerative variety), stomatitis, constipation, pancreatitis, various disorders associated with the esophagus, and diaphragmatic intestinal strictures develop occasionally;
• problems with the hepatobiliary system: increased levels of intracellular enzymes ALT together with AST (transaminases). Occasionally, manifestations of liver disorders or hepatitis are observed. Fulminant hepatitis, liver failure or hepatonecrosis are observed isolated cases;
• urinary disorders: signs of acute renal failure, necrotic papillitis, the appearance of blood in the urine, an increase in protein levels in the urine, the appearance of signs of nephrotic syndrome, as well as tubulointerstitial nephritis are observed sporadically;
• symptoms in the area of drug administration: abscesses in the injection area appear sporadically. Pain or hardening in the area of drug administration may often occur. Occasionally, tissue necrosis and swelling develop in the injection area;
• other disorders: rarely, the use of the drug may cause the development of edema. Some patients may experience signs of aseptic meningitis (including fever, tension in the neck muscles, and decreased consciousness). Such disorders are mainly observed in people with autoimmune pathologies.

Using the gel can lead to the following disorders:

• Epidermal signs: sometimes papules and vesicles with pustules, burning and itching, symptoms of contact dermatitis in the area of gel treatment, and in addition, peeling and increased dryness of the epidermis occur. Occasionally, manifestations of bullous dermatitis occur. Eczema, severe photophobia and generalized epidermal rash are noted isolatedly;
• immune disorders: symptoms of intolerance (e.g. Quincke's edema) and dyspnea are occasionally observed. Attacks of bronchial asthma develop sporadically.

The use of the gel in large portions or its application to large areas of the body may cause the development of systemic side effects and manifestations of intolerance in the form of shortness of breath or angioedema.

Overdose

In case of intoxication with the drug, bowel disorders (for example, diarrhea), vomiting, bleeding in the gastrointestinal tract, seizures, headaches with involuntary twitching and muscle contractions (myoclonic seizures, mainly observed in children), as well as dizziness may occur.

Diclofenac poisoning can cause liver damage and the development of manifestations of acute renal failure.

As with overdose of other substances from the NSAID category, therapy for diclofenac intoxication involves symptomatic and supportive treatment procedures.

Such measures are required in situations where a person has pronounced signs of renal failure, decreased blood pressure, various gastrointestinal disorders, and weakened respiratory function.

Specific procedures used as detoxification measures (for example, hemosorption or forced diuresis) are ineffective because the active elements of NSAIDs can be synthesized in large quantities with intraplasmic protein and participate in intensive metabolic processes.

In case of accidental ingestion of any amount of medicinal gel, symptomatic procedures must be carried out - gastric lavage, use of sorbents and implementation of measures that are carried out in the case of treatment of signs of NSAID intoxication.

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Interactions with other drugs

The combination of the drug with the anticonvulsant phenytoin, digoxin and lithium medications may lead to an increase in plasma levels of these therapeutic drugs.

The use of Diclac together with diuretic drugs reduces the medicinal effectiveness of these substances.

The use of diclofenac in combination with potassium-sparing diuretics may provoke signs of hyperkalemia.

Use with aspirin results in decreased plasma levels of diclofenac. In addition, this combination significantly increases the likelihood of negative side effects.

The effect of diclofenac potentiates the renal toxicity of cyclosporine.

Medicines containing diclofenac can cause the development of signs of hyper- or hypoglycemia, which is why when they are combined with antidiabetic drugs, it is necessary to regularly monitor blood sugar levels.

The cytostatic substance methotrexate, when used one day before or after diclofenac, can provoke an increase in plasma levels of methotrexate and potentiation of the intensity of its toxic effects.

If the combined use of the drug and anticoagulants is required, changes in blood coagulation values will need to be constantly monitored during therapy.

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Storage conditions

Diclac is stored in a dark, dry place, out of the reach of small children. Tablets and suppositories are stored at temperatures no higher than 25°C, and the gel (which is prohibited from freezing) can be stored at a temperature in the range of 8-15°C.

Shelf life

Diclac is allowed to be used for a 3-year period from the date of manufacture of the medicine.

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Application for children

Tablets should not be administered to persons under 15 years of age. The solution should not be administered to persons under 18 years of age. Rectal suppositories should not be used in children under 12 years of age.

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Analogues

The analogs of the drug are the substances Ortofen, Diklo-F, Olfen with Voltaren, as well as sodium Diclofenac, Diclogen, Almiral with Dicloberl, Rapten with Naklofen, Diclovit and Dicloran.

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Reviews

Diclac usually receives good feedback from patients - its use leads to a rapid improvement in the condition. But it is important to take into account that after the end of the therapeutic cycle, the signs of the disease often reappear. Because of this, the drug is usually used as a substance for symptomatic procedures.

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