Diklak

Description overdue on 08/23/2014

• Latin name: Diclac
• ATC code: M01A B05
• Active substance: Diclofenac sodium (Diclofenacum Na)
• Manufacturer: SALUTAS PHARMA, GmbH, Germany

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• Composition
• Product form
• Pharmacological action
• Pharmacodynamics and pharmacokinetics
• Indications
• Contraindications
• Side effects
• Instructions for use Diklaka: Dosing and dose
• Overdose
• Cooperation
• Terms of sale
• Storage conditions
• Shelf life
• Reviews
• Price, where to buy

Composition

One enteric-coated tablet contains 50 mg Diclac diclofenac sodium   and a number of auxiliary ingredients.

One vial of solution for intramuscular injection containing 75 mg Diklak diclofenac sodium   and auxiliary substances:

• n-acetylcysteine;
• benzyl alcohol;
• mannitol (E421);
• sodium hydroxide;
• propylene glycol;
• water for injections.

One tablet Diklak modified release may contain 75 or 150 mg of active substance + number of auxiliary substances.

The structure of 1 gram of gel for external use Diklak includes 50 mg diclofenac sodium And isopropyl alcohol, purified water, macrogol glycerol cocoate 7, hypromellose, flavor oil "Bouquet" WN 4507 as an auxiliary component.

A rectal suppository contains 50 mg Diklak diclofenac sodium And 1, 2-propylene glycol, witepsol and Aerosil as auxiliary components.

Product form

The drug Diklak has several dosage forms:

• enteric-coated tablets №20;
• solution for intramuscular injection, available in ampoules with a capacity of 3 ml, №5;
• The modified-release tablet diclofenac sodium   75 mg, №20 and №100;
• The modified-release tablet diclofenac sodium   150 mg, №20 and №100;
• 5% gel in tubes with capacity of 50 g;
• 5% gel in tubes with capacity of 100 g;
• 50 mg rectal suppositories, №10.

Pharmacological action

Diklak tablets, rectal suppositories and solutions for intramuscular injections belong to the group of non-steroidal antiinflammatory and antirheumatic drugs.

Gel Diklak refers to the pharmacotherapeutic group of drugs that are applied topically to relieve pain in muscles and joints.

Pharmacodynamics and pharmacokinetics

The preparation includes Diklak diclofenac sodium - a drug non-sterile structure, a derivative of phenylacetic (alpha-toluic acid), and having the ability to have expressed:

• antiphlogistic ;
• anesthetic ;
• antirheumatic ;
• antipyretic effect .

Mechanism of action diclofenac   reduces to:

• the suppression of the activity involved in the synthesis of prostanoids   and a cascade of metabolic reactions of arachidonic acid of the enzyme cyclooxygenase (COX);
• the suppression of the biosynthesis prostaglandins Playing a leading role in the development of inflammation, pain, and fever;
• The decline in permeability capillaries ;
• membrane stabilization lysosome ;
• suppression of aggregation Platelet , Which provoked the nucleotide adenosine diphosphate and fibrous proteins Collagen ;

Application diclofenac sodium   It improves the ability of the affected motor pathological process joints , Improves range of motion in them, as well as a decrease in the intensity of pain with rest and in motion.

Conducted in vitro experiments on application diclofenac sodium   in doses equivalent to those used for the treatment of patients showed that the drug does not cause suppression of the biosynthesis proteoglycans   (carbohydrate and protein components) cartilage .

Patients who have pain and inflammation are due to trauma or surgery, Diklak:

• quickly and efficiently relieves pain   (spontaneously occurring, and pain that makes itself felt when driving);
• reduces the severity of edema Induced inflammation;
• reduces symptoms of morning stiffness.

A significant analgesic effect of the drug is also indicated for the treatment of patients with symptoms Diklakom moderately and strongly expressed the nature of non-rheumatic pain   origin.

Positive therapeutic effects after injection Diklaka develops in about half an hour (and sometimes after only 15 minutes). In addition, injections Diklaka greatly facilitate the condition of patients suffering from seizures migraine .

Also, the drug is able to stop symptoms of pain   and reduce the severity of blood loss in women with dysmenorrhea   primary type.

In those cases where diclofenac   administered in combination with opoidnymi analgesics to relieve postoperative pain, the need for narcotic analgesics is greatly reduced.

A solution for intramuscular injection is recommended in the initial stages of therapy rheumatic diseases   degenerative and inflammatory disorders, as well as for removal pain Which are accompanied by inflammation non-rheumatic diseases of nature   origin.

Gel Diklak represents the nonsteroidal anti-inflammatory drug for external use from the group of alpha-toluic acid.

The product is characterized by the ability to provide local antirheumatic . analgesic   and anti-inflammatory Which it is due to the ability to being a part of diclofenac sodium   inhibit biosynthesis prostaglandins Which are mediators pain   and inflammation.

Application of ointments Diklak:

• It relieves the intensity of pain in the affected joints   and muscle (both at rest and in motion);
• improves motor activity of the pathological process of affected joints.

After oral administration of the drug in the form of enteric-coated tablets diclofenac sodium   rapidly and fully absorbed from stomach   and gastrointestinal tract . Food affects the absorption rate, slowing, however, the amount of absorbable material remains unchanged.

After intramuscular administration Diklaka at a dose equivalent to 75 mg of diclofenac sodium, the process of absorption of the active substance starts immediately. Maximum plasma concentration of the drug is 2, 5 micrograms / ml (and 8 mol / L) was observed after twenty minutes after the injection.

Between the amount of the absorbed dose of the drug substance and observed a linear relationship.

The pharmacokinetic parameter AUC, area under the curve showing the "active ingredient concentration - time" following injection into muscle, or intravenous Diklaka approximately twice that after the drug orally or rectally.

This is because in the latter case, about 50% of the active substance is exposed metabolization processes already during the first passage through liver .

After re-introduction diclofenac sodium   its pharmacokinetic parameters remain unchanged. Under the recommended dosing intervals instruction accumulation in the body of the active substance is observed.

A characteristic feature of tablets Diklak ID is the fact that one sixth of the members thereof as active component diclofenac sodium   released quickly, and the remaining ⅚ of its total amount released gradually.

Due to the pharmacological effects of this combination in a single two-layer tablet is provided:

• rapid onset of action of the drug;
• continuous circulation diclofenac sodium   in the systemic circulation and, as a consequence, prolonged therapeutic effect which is observed even during the day.

After using the tablet Diklak ID per os diclofenac   completely absorbed from gastrointestinal tract . Maximum observed plasma concentration in the range from 1 to 16 hours after ingestion (on average the figure reaches its maximum value after two or three hours after administration).

Between the amount of the absorbed dose of the drug substance and observed a linear relationship.

Once in the body, diclofenac   almost 100% (and, more precisely, at 99, 7%) binds to the plasma proteins Mainly - with albumin . The volume of distribution material is in the range of from 120 to 170 ml / kg.

Concentration diclofenac   in filling the cavities of joints synovial fluid   after receiving Diklaka inwards in the form of tablets observed after three to six, and after the injection - have two to four hours.

The half-life of the substance synovial fluid   It varies from three to six hours.

Two hours after addition, as an indicator of plasma concentration reaches its maximum rate diclofenac   at synovial fluid   It becomes higher than its plasma levels, and this effect is maintained over the next twelve hours.

After receiving tablets Diklak about 50% of a single dose of diclofenac sodium   metabolization already exposed during the first pass through the tissue liver   and only 35 to 70% of the absorbed substance reaches poslepechenochnoy circulation in an unchanged form.

Diclofenac partially biotransformed by glucuronidation of the parent molecule but, to a greater extent by hydroxylation and methoxylation reaction.

As a result of these processes produce few phenolic metabolites, only two of which have biological activity, which, however, is less active starting materials.

The half-life diclofenac   from the body it is between one and two hours, and it is not affected by the functional activity kidney   and / or liver .

Indicator systemic clearance substance plasma   It is in the range of 207 to 319 ml / min.

Most got the body diclofenac   (about 60%) excreted kidney   in the form of metabolites, slightly less than 1% excreted unchanged in substance form the residue - as metabolites with bile .

When assigning Diklak solution for treating patients of special groups differences in pharmacokinetic characteristics of the drug have been identified (including any differences in the age dependence of absorption, metabolism and excretion of the active substance from the body).

For some elderly patients after a 15-minute time introducing a solution into a vein rate, plasma concentrations diclofenac sodium   It increased by about 50% compared with young healthy individuals.

Patients with impaired functional activity kidney   Under the recommended dosing regimen of the drug instructions were observed accumulation in the body diclofenac sodium .

In the treatment of patients with Diklakom cirrhosis of the liver   or hepatitis   chronic form pharmacokinetic characteristics diclofenac   It was the same as in the case when dealing with the treatment of patients with a healthy liver .

After application of the gel in the form Diklaka diclofenac sodium   slowly and only partially absorbed on the surface of the skin. Outside the plasma concentration reaches its maximum after six to nine hours.

The average retention time of the active substance in the systemic circulation - about nine hours, which is significantly higher than after the internal use of the drug, which is one to two hours.

After topical processes metabolization and excretion diclofenac   identical to those of the body after systemic administration of the drug. Indicator binding diclofenac   from plasma proteins   is 99%.

After a quick metabolization in   liver   by hydroxylation and binding to glucuronic acid approximately ⅔ substance excreted kidney And the rest - with bile .

Indications

Indications for enteric-coated tablets Diklak are:

• degenerative rheumatic disease and inflammatory (e.g. rheumatoid arthritis or osteoarthritis );
• symptoms pain   localization in the spine;
• rheumatic soft tissue ( articular rheumatism );
• acute attacks gouty arthritis ;
• accompanied by inflammation and swelling of tissues pain syndrome   after trauma or surgery (including pain syndrome That develops after orthopedic or dental treatment);
• gynecological diseases accompanied by inflammation and symptoms pain   (eg, adnexitis   or dysmenorrhea   primary type);
• be severe ENT diseases Accompanied by pain (the drug is prescribed as an adjunct).

The solution Diklak prescribed for intramuscular injection in patients with:

• rheumatic diseases of degenerative and inflammatory (eg   rheumatoid arthritis   or osteoarthritis );
• acute attacks gouty arthritis ;
• biliary pain ;
• renal colic ;
• accompanied by inflammation and swelling of tissues post-traumatic pain ;
• pain We are developing in the postoperative period;
• protekayuschmi severe attacks migraine .

Intravenous drug appropriate to prescribe for treatment and prevention postoperative pain .

Tablets prescribed Diklak ID:

• at rheumatism ;
• to relieve symptoms postoperative   and post-traumatic pain ;
• in disease states, which are accompanied by certain gynecological diseases.

Rectal suppositories are recommended for appointment:

• inflammatory and degenerative processes activated by inflammatory forms rheumatism   (for example, in polyarthritis   chronic form,   neuritis   or neuralgia );
• when soft tissue lesions rheumatic genesis ;
• at posttraumatic   or postoperative pain Which is accompanied by a painful swelling of the tissues and the development of the inflammatory process;
• inflammatory pain states of nature non-rheumatic origin.

Diklak gel is used for the symptomatic treatment of pain, withdrawal symptoms of inflammation and swelling of tissue elimination:

• various types of traumatic injuries of soft tissues ( sprain . muscle . dislocation . hematomas   etc.);
• Localized forms of inflammatory rheumatic diseases (for example, tendinitis   or periartropatii );
• in localized forms rheumatism Accompanied by the development of degenerative processes (for example, osteoarthritis of peripheral joints or osteoarthritis of the spine ).

Contraindications

Contraindication to Diklaka in the form of tablets, solutions and suppositories are:

• Increased individual sensitivity to diclofenac   or any of the components contained in each of these forms of the drug;
• occur in acute form stomach ulcer   or bowel ;
• gastrointestinal bleeding ;
• perforation of the stomach   or bowel ;
• renal . heart   or hepatic failure   severe;
• violation of hematopoiesis   uncertain nature of origin;
• last trimester pregnancy ;
• lactation .

Diklak not indicated for patients who in response to treatment acetylsalicylic acid   or other non-steroidal anti-inflammatory drugs are developed seizures asthma , Symptoms of acute rhinitis   and hives .

Contraindication to tablets Diklak age is 15 years. Diklak solution is contraindicated in patients less than age 18 years. Rectal suppositories prohibits instruction given to children up to 12 years, and patients with symptoms of proctitis ( inflammation of the rectum ).

Contraindication to gel Diklak are:

• Individual hypersensitivity to diclofenac or any of the excipients of the formulation;
• if the patient has a history of seizures asthma . hives   or rhinitis   acute form;
• nasal polyps   (including history);
• angioneurotic angioedema   history;
• heightened individual sensitivity to analgesic drugs, and, in particular, to antirheumatic drugs;
• last trimester pregnancy .

Side effects

Diklaka dosage forms intended for oral administration, can trigger:

• Violations of the circulatory   and lymphatic systems Which are expressed in various forms anemia Including aplastic and hemolytic, reducing the number of leukocytes .   Platelet   and neutrophilic granulocytes (all these phenomena belong to the category of very rare).
• Disorders immune system , Expressed in the form of hypersensitivity reactions, anaphylactoid reactions . angioedema   (rarely).
• In very rare cases - mental disorders Expressed as disorientation   in space occurs depression . nightmares . increased irritability , Various types of psychotic disorders.
• Violations of the Nervous System : Often - headache . dizziness ; in rare cases - increased drowsiness ; in very rare cases - sensitivity disorders, taste disorders, memory disorders, aseptic meningitis Appearance tremor , Violations Cerebral blood flow , The emergence of nightmares, irritability.
• In rare cases - visual impairment , him blurred . ghosting items .
• Hearing impaired Which are expressed: often - in the form of vertigo ; very rarely - in the form of hearing disorders, ringing in the ears .
• Violations of the hearts : heart palpitations , Pain in the chest, symptoms Heart Failure , Development myocardial infarction   (All of these phenomena are very rare).
• Violations by   vascular system : arterial hypertension . vasculitis (rarely).
• Violations of the Respiratory System : rarely - asthmatic attacks   (including dyspnoea) and the emergence of symptoms b ronhospasticheskogo syndrome ; very rare - the defeat of the alveolar walls and / or interstitial tissue light Accompanied by fibrosis .
• Violations by Digestive System . stomach   and gastrointestinal tract : The most frequently - attacks nausea . vomiting . dyspeptic disorders , Abdominal pain, gain flatulence , Signs of anorexia ; in rare cases - gastritis . . stomach ulcer   and / or     and . constipation   stomatitis pancreatitis .
• hepatobiliary system ); hepatitis   liver ; hepatitis hepatic insufficiency .
• renal failure . . .

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• . vesicle .   and pustules   ; eczema .
• immune system shortness of breath  
• asthma  

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  or dyspnea .

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kidney   and / or liver

 

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migraine   .  

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Arthritis

Overdose

 

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  renal failure   liver .

 

• Blood Pressure ;
• renal failure ;
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  or hemosorbtion  

 

 

Cooperation

 

    hyperkalemia .

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  - Or   .

     

  blood clotting .

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