Diklak

Diclac is included in the category of antirheumatic drugs, and in addition is a substance from the NSAID subgroup.

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

Indications Diklaka

Medication tablets are used for such disorders:

• having inflammatory and, in addition, degenerative activity of a pathology of rheumatic origin (for example, osteoarthritis or arthritis of a rheumatoid variety);
• pain symptoms occurring in the vertebral region;
• soft tissue-affecting rheumatism (for example, extra-articular);
• bouts of gouty arthritis in the active phase;
• arises in connection with operations or injuries of pain, against the background of which there are puffiness and inflammation (among them pains that develop in connection with dental or orthopedic procedures);
• gynecological diseases during which pain and signs of inflammation appear (for example, dysmenorrhea with primary form or adnexitis);
• severe pathology, affecting the ENT organs, against which there is pain (the drug is used as an auxiliary substance).

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

• rheumatic diseases with inflammatory or degenerative forms (for example, rheumatoid arthritis or osteoarthritis);
• bouts of gouty arthritis (active stage);
• biliary pain;
• colic in the kidneys;
• pains caused by injuries, against which tissue edemas and inflammations are observed;
• pains arising after operations;
• migraine attacks with severe severity.

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

Tablets are used in such cases:

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

Rectal suppository is prescribed for the following disorders:

• active or normal inflammation in rheumatism with degenerative activity (for example, in the case of neuritis, polyarthritis, which has a chronic form, or neuralgia);
• having a rheumatic etiology of damage in the area of soft tissues;
• pain associated with injuries or surgeries that cause painful tissue swelling and inflammation;
• inflammatory pain having a non-rheumatic genesis.

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

• injuries having a different nature, damaging layers of soft tissues (among these are sprains with muscle or tendon sprains, hematomas, etc.);
• localized inflammations that are of a rheumatic nature (for example, periarthropathy or tendonitis);
• localized types of rheumatism in which degenerative processes are recorded (for example, in the case of vertebral or osteoarthritis affecting the peripheral joints).

[1], [2],

Release form

The release of the drug substance is in the form of:

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

[3]

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 the exchange effects of arachidonic acid;
• inhibits biosynthesis of PG, which are the main causative agents of developing inflammation, fever and pain;
• strengthens capillary strength;
• stabilizes lysosomal walls;
• inhibits platelet aggregation, which develops under the action of the nucleotide ADP, as well as collagen (fibrillar protein).

The use of Diclofenac Na helps to improve the motor activity of the affected joints, increases their motor volume and reduces the painful severity during movements and in a calm state.

In vitro tests performed using the active element of drugs in portions similar to those used in the treatment of patients demonstrated that the drug does not lead to inhibition of proteoglycan biosynthesis inside cartilage tissues.

[4], [5]

Pharmacokinetics

After oral ingestion of enteric tablets, the active component of the drug is fully absorbed from the gastrointestinal tract at high speed. Food affects the rate of absorption (it slows down), but the volume of the absorbed element remains the same.

With a / m injection of a portion equal to 75 mg of a substance, its absorption begins immediately. At the same time, plasma Cmax values equal to 2.5 μg / ml are recorded after 20 minutes from the moment of the procedure.

There is a linearity between the volumes of the absorbed component and the size of the portion of the drug.

AUC values after i / m injection or intravenous injection are approximately twice as high as those observed after rectal or oral drug use. This is due to the fact that with the latter method of introducing approximately 50% of the element, metabolic processes with the 1st intrahepatic passage take part.

With repeated use of the drug, its pharmacokinetic properties do not change. Compliance with the prescribed intervals between injections of drugs allows you to avoid the accumulation of its active element inside the body.

With oral pills, the drug is fully absorbed inside the gastrointestinal tract. It reaches the plasma level Cmax in the interval of 1-16 hours from the moment of drug administration (on average, the drug reaches its peak values after 2-3 hours from the moment of use).

After ingesting the body, the substance is almost completely (99.7%) synthesized with intraplasma protein (most of it with albumin). The distribution volume is in the range of 120-170 ml / kg.

Indicators of diclofenac inside synovia, located in the articular cavity, after oral administration of Diclac tablets are recorded after 3-6 hours; with the introduction of drugs through injection - after 2-4 hours.

The term elimination half-life of a component from a synovia fluctuates in a range of 3-6 hours.

After 2 hours from reaching the plasma Cmax, the values of diclofenac inside synovia increase above the plasma values and this effect continues to persist for the next 12 hours.

After consuming the tablet, about 50% of the 1-fold portion of the drug is involved in the 1st intrahepatic passage. Only 35-70% of the absorbed element during the post-hepatic circulation has an unchanged state.

Partial biotransformation of the component occurs during the glucuronization of the initial molecule, but mostly during the 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 influence of the original element).

The term half-life of drugs is 1-2 hours, while this indicator does not affect the functional state of the liver or kidneys.

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

Excretion of most of the drug (about 60%) is done through the kidneys in the form of metabolic components; less than 1% of the drug is excreted unchanged, and the rest - with bile in the form of metabolic elements.

[6], [7],

Dosing and administration

In the case of using any form of release of the medication, the dosage is determined personally, 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 Diclac tablets.

The drug is used in adolescents from 15 years of age and adults. Initially, the day required to use 0.1-0.15 g of the drug substance.

With a mild course of the disease, and in addition, if you need long-term therapy, you should use 75-100 mg of the substance per day. Separate this dosage to 2-3 applications.

If required, apply 75 mg of medication. During the day, you can use a maximum of 0.15 g of diclofenac.

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

Begin to use the drug should be after the development of the first signs of pain. The duration of the treatment cycle is determined by the intensity of the clinical symptoms and often does not exceed several days.

Tablets are consumed before eating, without chewing and washing down with plain water (1 cup).

The use of injection fluid.

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

Intramuscular injections are allowed to spend a maximum of 2 days in a row. Further, with the need to eliminate pain, therapy is continued with the use of tablets.

During the day, injections of 75 mg of diclofenac Na (corresponding to the 1st ampoule of the drug) are allowed to be given through the injections. The needle for injections is inserted deep inside the outer upper region of the muscles of the buttocks.

In extremely severe conditions, during which severe pains are noted, it is allowed to double the daily dose of the medicine. It is required to maintain a break between injections for at least several hours. The drug is injected into the different muscles of the buttocks (left, and 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. A portion should be calculated so that in total it is not more than 0.15 g per day.

In the case of migraine attacks, the injection of the drug at a dosage of 75 mg should be done as quickly as possible. In addition, on the same day, it is possible to administer Diclac rectal suppositories (0.1 g per day). For the first day with a similar scheme requires a maximum of 175 mg of the substance.

Infusion is usually performed in a bolus manner. 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; 8.4% infusion fluid (sodium bicarbonate) is also involved in this combination. The volume of solvent used - 0.1-0.5 liters of the substance. It is possible to apply only transparent liquids solvents.

For severe or moderate pain that occurs after surgery, the patient requires the introduction of 75 mg of medication. This infusion lasts within 0.5-2 hours.

If necessary, the procedure can be repeated after several hours. We should not forget that in a day the patient can be administered no more than 0.15 g of the drug.

For prophylaxis after the procedure of the operation, after 15-60 minutes, 25-50 mg of the drug is administered to the patient (load portion of the drug). Then a continuous infusion is performed (at a rate of maximum 5 mg / hour) to obtain a volume of 0.15 g of the drug.

Tablets having a modified release form.

First, patients take 75-150 mg per day (1 or 2 tablets, taking into account the severity of pain).

When the need for long-term therapy is necessary to enter 75 mg of the drug per day.

For people whose manifestations of the disease mainly occur in the morning and at night, the medication is prescribed for reception at night, before bedtime.

Per day is allowed to consume a maximum of 0.15 g Diklaka. This treatment course should last a maximum of 14 days. The course doctor should select the course duration, taking into account the patient's condition and the clinical picture.

It is necessary to swallow tablets completely, without their preliminary crushing; should be washed down with a glass of ordinary water. It is recommended to use the medication with food.

Use of medicinal candles.

To introduce the drug to adults. Different treatment regimens are used - 1 time a day in a dose of 0.1 g of the substance, 2 times a day at a dosage of 50 mg, or 3-4 times a day at a dose of 25 mg.

A day is allowed to use no more than 0.15 g of the drug.

For children from 12 years old, suppositories are administered in 0.05-0.1 g for 1 or 2 applications, as well as 75 mg for 2 or 3 administrations.

The use of substances in the form of a gel.

The drug is applied to the skin 2-3 times per day in the amount required for the treatment of the inflamed area. For example, 2-4 g of medicine is enough to treat the area of the epidermis, which has an area of 0.4-0.8 m ². Application is carried out with a thin layer, with a slight rubbing of the substance into the epidermis.

After finishing the treatment, wash your hands thoroughly using soap. The only exceptions are situations when the substance is applied to this particular area of the hands.

It is allowed to use the gel in combination with iontophoresis procedures. This method of application provides a deeper passage of the substance into the epidermis with a more intense medical effect. Apply the medicine you need under the electrode with a negative charge.

The duration of the treatment cycle is selected taking into account information on the effectiveness of the therapy. Basically it is 10-14 days. Taking into account the state of human health, a second course can be prescribed (but it can be held at least after 2 weeks from the moment of completion of the first).

In the case of lesions in the area of soft tissues (also having a rheumatic nature), the gel is used for a maximum of 14 days. Therapy in people whose pain is caused by the development of arthritis lasts 21 days (unless the treating doctor has prescribed a different duration).

When using a medicine without medical prescription, if there is no improvement in a person after 7 days of therapy, a doctor should be consulted.

[14], [15]

Use Diklaka during pregnancy

It is forbidden to use the drug during breastfeeding and on the 3rd trimester.

[8], [9], [10], [11], [12]

Contraindications

The main contraindications of the solution, tablets and suppositories:

• strong personal sensitivity with respect to diclofenac or other drug components;
• ulcer affecting the gastrointestinal tract in the active phase;
• bleeding that develops in the gastrointestinal tract;
• gastric or intestinal perforation;
• severe failure of the heart, kidneys, or liver;
• hematopoietic disorder with unexplained etiology.

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

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

The gel is not used in such cases:

• increased personal intolerance regarding diclofenac or auxiliary components of the drug;
• the presence in the history of the patient's urticaria, attacks of asthma, as well as the acute form of rhinitis;
• polyps inside the nose (also available in history);
• a history of angioedema;
• severe intolerance associated with analgesic substances (among them antirheumatic drugs).

[13]

Side effects Diklaka

Forms of the drug, used orally, can cause such side effects:

• disorders associated with the work of the circulatory system and lymph: a single occurrence of anemia of a different nature (hemolytic or aplastic) or decreases in the volume of platelets, leukocytes or granulocytes of neutrophilic nature;
• immune lesions: occasionally symptoms of intolerance, anaphylactoid manifestations, or Quincke edema;
• mental disorders: rarely, nightmares, states of depression, spatial disorientation, increased irritability, and various psychotic problems;
• problems in the work of the National Assembly: dizziness or headaches often occur. Occasionally, severe drowsiness. A single development is a violation of taste or sensitivity, memory disorders, tremor, aseptic meningitis, nightmares, disorders of cerebral blood flow and severe irritability;
• visual manifestations: occasionally double vision, blurred vision or his disorder;
• auditory lesions: vertigo often appears. Auditory impairment and ear ringing are singly observed;
• problems with cardiac activity: pains affecting the sternum, increased heart rate, myocardial infarction, or signs of CH;
• disorders affecting the work of blood vessels: single vasculitis or an increase in blood pressure indicators;
• symptoms associated with respiratory organs: asthma attacks (among them also dyspnea) and manifestations of the bronchospastic syndrome are rarely observed. Unity develops lesions of the interstitial lung tissue or the walls of the alveoli, against which fibrosis is noted;
• lesions in the gastrointestinal tract and digestive system: abdominal pain, anorexia symptoms, dyspeptic disorders, vomiting, increased swelling and nausea are often observed. Occasionally, bleeding occurs in the gastrointestinal tract, gastritis, bloody diarrhea or vomiting of blood, ulcers in the gastrointestinal tract (this can develop bleeding or perforation) and melena. The colitis (its hemorrhagic or ulcerative variety), stomatitis, constipation, pancreatitis, a variety of disorders related to the esophagus, and intestinal diaphragm-like strictures develop spontaneously;
• problems in the hepatobiliary system: an increase in intracellular enzymes of ALT, along with AST (transaminases). Occasionally, manifestations of hepatic impairment or hepatitis are noted. Hepatitis of lightning character, insufficiency of the liver function or hepatonecrosis is singularly observed;
• urinary disorders: signs of acute renal failure, necrotizing papillitis, the appearance of blood in the urine, an increase in protein indicators inside the urine, signs of nephrotic syndrome, and tubulointerstitial nephritis;
• Symptoms in the area of drug administration: abscesses appear in the injection area. Often there may be pain or hardening at the site of administration of the drug. Occasionally, tissue necrosis and edema develop at the injection site;
• other disorders: occasionally the use of medication may cause the development of edemas. Some patients may experience signs of aseptic meningitis (fever, cervical tension, and consciousness suppression among them). Most of these disorders are observed in people with autoimmune pathologies.

The use of gel can lead to the appearance of such violations:

• epidermal signs: sometimes papules and vesicles with pustules appear, burning and itching, symptoms of contact dermatitis in the treatment area of the gel, and peeling and an increase in dryness of the epidermis occurs. Occasionally there are manifestations of bullous dermatitis. Eczema, severe photophobia and generalized epidermal rash are rarely reported;
• immune disorders: rarely occurrence of symptoms of intolerance (for example, angioedema) and dyspnea. The bouts of asthma rarely develop.

The use of the gel in large portions or its application to large areas of the body can 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 a medication, stool disorders (eg, diarrhea), vomiting, bleeding in the gastrointestinal area, seizures, convulsions, headaches, involuntary twitching and muscle contractions (myoclonic type cramps, mostly 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 category of NSAIDs, therapy for diclofenac intoxication involves the conduct of symptomatic and supportive medical procedures.

Such measures are required in situations where a person has pronounced signs of kidney failure, a decrease in blood pressure values, a variety of disorders associated with the gastrointestinal tract, and a decrease in respiratory activity.

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

If any amount of drug gel is accidentally swallowed, symptomatic procedures are required - gastric lavage, use of sorbents, and the implementation of measures that are carried out in case of treatment of signs of intoxication with NSAIDs.

[16], [17]

Interactions with other drugs

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

Using Diclak along with diuretic drugs lowers the drug effectiveness of these substances.

The use of diclofenac in combination with diuretic drugs of potassium-sparing nature can provoke signs of hyperkalemia.

Using together with aspirin leads to a decrease in plasma indicators of diclofenac. In addition, this combination significantly increases the likelihood of negative side effects.

The effect of diclofenac potentiates the toxic activity against the kidneys exerted by cyclosporin.

Diclofenac-containing products can cause the development of signs of hyper- or hypoglycemia, which, when combined with antidiabetic drugs, requires regular monitoring of blood sugar levels.

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

If you need the combined use of medication and anticoagulants, during therapy you will need to constantly monitor changes in the blood clotting values.

[18], [19], [20], [21]

Storage conditions

Diklak contain in a dark, closed from the penetration of small children, dry place. Tablets and suppositories are stored at temperatures of no more than 25 ° C, and the gel (which is forbidden to freeze) can be stored at a temperature in the range of marks 8-15 ° C.

Shelf life

Diklak allowed to use for a 3-year term from the date of manufacture of the drug.

[22]

Application for children

Tablets should not be administered to persons under the age of 15. The solution is unacceptable to introduce people whose age is less than 18 years. Rectal suppositories are not used in children younger than 12 years of age.

[23], [24], [25], [26]

Analogs

Analogues of drugs are substances Ortofen, Diclo-F, Olfen with Voltaren, and in addition Diclofenac sodium, Diklogen, Almiral with Dikloberlo, Rapten with Naklofen, Diklovit and Dikloran.

[27], [28], [29], [30], [31]

Reviews

Diclac usually receives good reviews from patients - when it is used, there is a rapid improvement in the condition. But it should be borne in mind that after the end of the therapeutic cycle, the symptoms of the disease often appear again. Because of this, the drug is usually used as a substance for symptomatic procedures.

[32]