Diclonat p

Diclonate p is a derivative of α-toluic acid; has analgesic, anti-inflammatory and antipyretic effects.

Contains the element diclofenac, which helps to reduce the intensity of pain (appearing during movement or in a calm state), reduce swelling affecting the joints, and also reduce morning stiffness that occurs in rheumatic diseases. Like other NSAIDs, the drug demonstrates an antiplatelet effect. [1]

Indications Diclonat p

It is used for intramuscular injections in such cases:

• inflammations affecting the ODA area ( arthritis of psoriatic, rheumatoid or chronic juvenile nature, and in addition, arthritis of gouty origin in the active phase and ankylosing spondylitis);
• inflammation in the pelvic area, and in addition, proctitis with adnexitis, colic, having a bilious or renal character, and algomenorrhea of the primary type;
• having a degenerative nature of the pathology of ODA (osteochondrosis or deforming form of osteoarthritis);
• combination therapy in the case of inflammatory infections in the throat, ears and nose, in which there is intense pain (tonsillitis or otitis media with pharyngitis);
• various pains (rheumatism in the soft tissues, sciatica, bursitis and lumbago with neuralgia and tendovaginitis, myalgia, headache, toothache or migraine pain, and at the same time moderate pain of a different origin);
• pain associated with injuries, against the background of which inflammation develops;
• postoperative pain;
• febrile syndrome.

Intravenous infusions through a drip are performed to relieve or prevent postoperative pain.

Release form

The release of the drug element is realized in the form of a liquid for intravenous or intramuscular injections; inside the box contains 5 ampoules with a volume of 3 ml.

Diclonat p retard 100

Diclonat p retard 100 is produced in tablets (volume 0.1 g) - 10 pieces inside a blister pack. The box contains 2 such packs.

Pharmacodynamics

Diclofenac non-selectively inhibits the components of COX-1 and COX-2, thereby destroying the metabolic processes produced with arachidonic acid. In addition, it inhibits the biosynthesis of PGs, which act as inflammatory and pain mediators, and also increase the temperature. [2]

Pharmacokinetics

With intramuscular administration of 75 mg of the drug, its plasma Cmax is 2.5 μg / ml and is recorded after 20 minutes; these indicators are linearly related to the size of the applied portion.

Intravenous infusion of 75 mg through a dropper (lasting more than 2 hours) leads to a plasma Cmax of 1.9 μg / ml. The drug values are inversely related to the duration of the infusion. [3]

The protein synthesis of the drug is quite high - 99% (mainly synthesized with albumin). The term intraplasma half-life is in the range of 1-2 hours.

If the established interval between doses is observed, the drug does not accumulate. It lends itself well to distribution inside fluids along with tissues. It passes into the synovium, reaching the Cmax level after 3-6 hours.

Participates in intrahepatic metabolic processes: by 50% in the 1st passage. AUC values are twice lower in the case of oral administration of drugs (in comparison with parenteral use of a similar dosage). Metabolic processes occur with 1-fold or multiple conjugation with hydroxylation. Metabolic processes are carried out using the P450 CYP2C9 enzyme structure. The medicinal activity of metabolic components is weaker than that of diclofenac.

The excretion of most of the Diclonat is carried out by the kidneys. The total clearance is 260 ml per minute. 60% excreted by the kidneys in the form of metabolic elements; less than 1% has an unchanged shape. The rest of the metabolic components are excreted along with bile.

Dosing and administration

The medication is prescribed intravenously through a dropper (infusion) or intramuscularly. You need to use Diclonat n for a maximum of 2 days. If there is a need to continue therapy, it is necessary to prescribe medication in the form of suppositories or tablets.

Conducting intramuscular injections: people with acute pain are daily used 75 mg of drugs. If necessary (during the development of colic of a renal or biliary nature), the daily portion is increased to 0.15 g (1 ampoule 2 times per day).

Performing intravenous infusions through a dropper: before using the drug, it is necessary to dissolve 75 mg of the substance (1 ampoule) inside 0.1-0.5 liters of 5% dextrose or 0.9% NaCl (before this, you need to add to the infusion fluid 8.4% sodium bicarbonate (0.5 ml)). Finished infusion fluids should be clear.

During the treatment of postoperative pain (moderate or severe), the medication is used for a period of 0.5-2 hours in a portion of 75 mg. If necessary, after a few hours it can be reapplied, but the dosage of the drug should not be more than 0.15 g per day.

To prevent the development of postoperative pain, a 15-60-minute infusion of 25-50 mg of Diclonat p is performed. Further, the infusion continues at a rate of 5 mg / hour until a daily dosage of 0.15 g is obtained.

• Application for children

Diclonat p is not used by persons under 15 years of age.

Use Diclonat p during pregnancy

It is forbidden to prescribe during pregnancy or breastfeeding.

Contraindications

Among the contraindications:

• severe intolerance to NSAIDs (also to aspirin) or if the patient has "aspirin" asthma;
• bleeding or active phases of erosive and ulcerative lesions inside the gastrointestinal tract;
• suppression of hematopoietic processes inside the bone marrow;
• various disorders of hemostasis (including hemophilia);
• conditions associated with a high likelihood of bleeding (also their presence in history).

Side effects Diclonat p

The main side effects:

• lesions in the digestive tract: NSAID gastropathy is often noted (epigastric discomfort and gastralgia, bloating, vomiting, belching, severe heartburn, abdominal pain, nausea, gastric overcrowding and diarrhea), bleeding in the gastrointestinal tract (melena or hematemesis), lesions in the gastrointestinal tract, having an erosive-ulcerative nature (peptic ulcers, lesions of the stomach or esophagus and multiple disorders in the gastrointestinal tract) and perforation of the intestinal wall (stools with blood, severe pain with a cutting shape, melena, burning in the epigastric zone and hematemesis), and besides this pancreatitis, accompanied by bleeding or colitis of a nonspecific type, constipation, xerostomia and hepatitis of a toxic nature. Sometimes colitis or exacerbation of its course, anorexia or loss of appetite, vomiting, spasms, pain affecting the mucous membrane in the mouth, and aphthous stomatitis (ulcers and erosion, as well as white plaque in the oral mucosa);
• disorders associated with the activity of the National Assembly: dizziness or headaches often occur. Sometimes there may be depression, drowsiness, convulsions, severe fatigue, nervousness with irritability, and in addition, meningitis of aseptic genesis, polyneuropathy (tremor and hyposthesia, as well as weakness or pain in the muscles of the legs and arms), insomnia, memory impairment, fear and psychotic signs;
• problems with sensory function: toxic amblyopia, deterioration of visual acuity, diplopia, scotoma, hearing impairment and other hearing disorders, as well as ear ringing are often noted;
• epidermal lesions: often there is epidermal hyperemia, itching or rashes (mostly urticarial or erythematous). Sometimes erythema polyform, SS, TEN, and photodermatitis (rashes, severe sunburns and pigmentation disorders) develop. Occasionally, with an intramuscular injection, infiltration, burning, necrosis of adipose tissue and necrosis of an aseptic nature may appear. It is also possible necrosis in the area of the procedure;
• disorders of urogenital function: often there is a delay in fluid secretion. Sometimes dysmenorrhea, proteinuria, hematuria, recurrent vaginal pains of an unknown nature, cystitis, anuria or oliguria develop, and in addition, pollakiuria, tubulointerstitial nephritis, deterioration of renal activity or aggravation of existing disorders, as well as nephrotic syndrome and peripheral edema;
• problems with hematopoietic activity: sometimes there is anemia (aplastic, hemolytic or caused by endogenous bleeding), agranulocytosis, neutro-, leuko- or thrombocytopenia (accompanied by purpura or not) and ecchymosis;
• respiratory dysfunction: dyspnea is sometimes observed;
• lesions in the work of the CVS: the level of blood pressure often increases. Collapse, arrhythmia, or cardialgia sometimes occurs. Occasionally, CHF worsens or chest pain appears;
• endocrine disorders: occasionally weight loss; 
• allergy symptoms: rarely develop anaphylactoid signs (urticaria, dyspnoea, epidermal itching, hyperemia having a focal shape, Quincke's edema affecting the tongue with lips, glottis, eyelids or paraorbital tissues, and besides this wheezing and pressing pain in the chest area) and anaphylaxis, and at the same time manifestations of bronchospastic allergy.

Overdose

In case of poisoning, signs associated with the function of the gastrointestinal tract develop, disorders of the central nervous system (from drowsiness with lethargy to the development of seizures with a coma), nephrotoxicity (can reach acute renal failure) and hypotension.

Symptomatic and supportive measures are taken to help remove signs of disorders. Hemodialysis or forced diuresis procedures will be ineffective.

Interactions with other drugs

The drug increases the plasma levels of methotrexate, cyclosporine with lithium substances and digoxin.

Weakens the effect of diuretic drugs.

When used with potassium-sparing diuretics, the likelihood of hyperkalemia increases.

Administration with thrombolytics (streptokinase and alteplase with urokinase) and anticoagulants increases the likelihood of bleeding (mainly inside the gastrointestinal tract).

The medication reduces the therapeutic activity of hypnotics and antihypertensive drugs.

The combination with Diclonat p increases the risk of developing negative symptoms of other NSAIDs and GCS (bleeding inside the gastrointestinal tract), the nephrotoxic properties of cyclosporine and the toxic activity of methotrexate.

Aspirin reduces the blood counts of diclofenac.

When combined with paracetamol, the likelihood of the nephrotoxic properties of diclofenac increases.

The medicine weakens the hypoglycemic activity of antidiabetic medicines.

Cefotetan, plikamycin with valproic acid, and in addition cefaperazone with cefamandole increase the incidence of hypoprothrombinemia.

The substances gold and cyclosporine increase the effect of diclofenac on intrarenal PG binding, resulting in increased nephrotoxicity.

The combination of Diclonat p with colchicine, ethyl alcohol, St. John's wort or corticotropin increases the likelihood of bleeding inside the gastrointestinal tract.

Medicines that provoke the development of photosensitivity increase the sensitizing effect of diclofenac relative to UV radiation.

Substances that block the processes of tubular secretion increase the plasma level of diclofenac, which enhances its toxicity and therapeutic activity.

Storage conditions

Diclonat n must be kept out of the reach of small children. Temperature - within 15-25 ° С.

Shelf life

Diclonat p can be used within a 5-year period from the date of manufacture of the therapeutic agent.

Analogs

Analogues of drugs are drugs Diclobene with Voltaren Emulgel, as well as Dicloran with Diclofenac Sandoz.