Diclonate n

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

Contains the element diclofenac, which helps to reduce the intensity of pain (occurring during movement or at rest), reduce swelling affecting the joints, and reduce morning stiffness that occurs with rheumatic diseases. Like other NSAIDs, the medication exhibits an antiplatelet effect. [ 1 ]

Indications Diclonate n

It is used for intramuscular injections in the following cases:

• inflammations affecting the musculoskeletal system ( arthritis of psoriatic, rheumatoid or chronic juvenile origin, as well as arthritis of gouty origin in the active phase and Bechterew's disease);
• inflammation in the pelvic area, as well as proctitis with adnexitis, colic of biliary or renal nature, and primary algomenorrhea;
• pathologies of the musculoskeletal system that are of a degenerative nature (osteochondrosis or deforming form of osteoarthritis);
• combination therapy in case of inflammatory infections in the throat, ears and nose, which are accompanied by intense pain (tonsillitis or otitis with pharyngitis);
• various pains (rheumatism in the soft tissue area, sciatica, bursitis and lumbago with neuralgia and tendovaginitis, myalgia, headaches, toothaches or migraines, as well as moderate pain of other origins);
• pain associated with injuries, against the background of which inflammation develops;
• postoperative pain;
• febrile syndrome.

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

Release form

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

Diclonate p retard 100

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

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 temperature. [ 2 ]

Pharmacokinetics

When 75 mg of the drug is administered intramuscularly, its plasma Cmax values are equal to 2.5 μg/ml and are recorded after 20 minutes; these values are linearly related to the size of the dose administered.

Intravenous infusion of 75 mg via a drip (lasting more than 2 hours) results in plasma Cmax values equal to 1.9 μg/ml. LS values are inversely dependent on the duration of infusion. [ 3 ]

Protein synthesis of the drug is quite high – 99% (mainly synthesized with albumins). The term of intraplasmic half-life is in the range of 1-2 hours.

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

Participates in intrahepatic metabolic processes: by 50% during the first pass. AUC values are twice as low when the drug is administered orally (compared to parenteral use of a similar dosage). Metabolic processes occur with single or multiple conjugation with hydroxylation. Metabolic processes are implemented using the enzyme structure P450 CYP2C9. The medicinal activity of metabolic components is weaker than that of diclofenac.

Most of Diclonat P is excreted by the kidneys. Total clearance values are 260 ml per minute. 60% is excreted by the kidneys in the form of metabolic elements; less than 1% is unchanged. The remainder of the metabolic components are excreted with bile.

Dosing and administration

The medication is administered intravenously through a drip (infusion) or intramuscularly. Diclonat P should be used for a maximum of 2 days. If therapy needs to be continued, the medication should be administered in the form of suppositories or tablets.

Conducting intramuscular injections: persons with acute pain are given 75 mg of the drug daily. If necessary (during the development of renal or biliary colic), the daily dose is increased to 0.15 g (1 ampoule 2 times a day).

Performing intravenous infusions through a dropper: before using the drug, it is necessary to dissolve 75 mg of the substance (1 ampoule) in 0.1-0.5 l of 5% dextrose or 0.9% NaCl (before this, 8.4% Na bicarbonate (0.5 ml) must be added to the infusion fluid). The finished infusion fluids must be transparent.

During the treatment of postoperative pain (moderate or severe), the drug is used in the period of 0.5-2 hours in a dose of 75 mg. If necessary, it can be used again after a few hours, but the dosage of the drug should not exceed 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. The infusion is then continued at a rate of 5 mg/hour until the daily dosage of 0.15 g is obtained.

• Application for children

Diclonat P is not used in persons under 15 years of age.

Use Diclonate n during pregnancy

Do not use during pregnancy or breastfeeding.

Contraindications

Among the contraindications:

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

Side effects Diclonate n

Main side effects:

• Gastrointestinal tract lesions: NSAID-gastropathy is often observed (epigastric discomfort and gastralgia, bloating, vomiting, belching, severe heartburn, abdominal pain, nausea, gastric fullness and diarrhea), gastrointestinal bleeding (melena or hematemesis), gastrointestinal lesions of an erosive and ulcerative nature (peptic ulcers, stomach or esophageal lesions and multiple gastrointestinal disorders) and intestinal wall perforation (bloody stool, severe cutting pain, melena, burning in the epigastric region and hematemesis), as well as pancreatitis accompanied by bleeding or non-specific colitis, constipation, xerostomia and toxic hepatitis. Sometimes colitis or its exacerbation, anorexia or loss of appetite, vomiting, spasms, pain affecting the oral mucosa, and aphthous stomatitis (ulcers and erosions, as well as white plaque in the oral mucosa) occur;
• disorders associated with the activity of the nervous system: dizziness or headaches often occur. Sometimes depression, drowsiness, convulsions, severe fatigue, nervousness with irritability may be observed, as well as meningitis of aseptic genesis, polyneuropathy (tremor and hypoesthesia, as well as weakness or pain in the muscles of the legs and arms), insomnia, memory impairment, fear and psychotic symptoms;
• problems with the function of the sense organs: often observed are amblyopia of toxic origin, deterioration of visual acuity, diplopia, scotoma, hearing loss and other disorders, as well as tinnitus;
• Epidermal lesions: epidermal hyperemia, itching or rashes (mainly urticarial or erythematous) are often observed. Sometimes erythema multiforme, SJS, TEN and photodermatitis (rashes, severe sunburn and pigmentation disorders) develop. Rarely, with an intramuscular injection, infiltration, burning, necrosis of fatty tissue and aseptic necrosis may occur. Necrosis in the area of the procedure is also possible;
• urogenital disorders: fluid retention often occurs. Sometimes dysmenorrhea, proteinuria, hematuria, recurrent vaginal pain of unknown origin, cystitis, anuria or oliguria develop, as well as pollakiuria, tubulointerstitial nephritis, deterioration of renal function or aggravation of existing disorders, as well as nephrotic syndrome and peripheral edema;
• problems with hematopoietic activity: sometimes anemia (aplastic, hemolytic or caused by endogenous bleeding), agranulocytosis, neutro-, leukopenia- or thrombocytopenia (accompanied by purpura or not) and ecchymosis are observed;
• respiratory dysfunction: dyspnea is sometimes observed;
• damage to the cardiovascular system: blood pressure often increases. Sometimes collapse, arrhythmia or cardialgia occurs. Occasionally, CHF worsens or pain appears in the chest area;
• endocrine disorders: occasional weight loss;
• Allergy symptoms: anaphylactoid symptoms (urticaria, dyspnea, epidermal itching, focal hyperemia, Quincke's edema affecting the tongue and lips, glottis, eyelids or paraorbital tissues, and also wheezing and pressing pain in the sternal area) and anaphylaxis occasionally develop, as well as manifestations of bronchospastic allergy.

Overdose

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

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

Interactions with other drugs

The drug increases 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 within the gastrointestinal tract).

The medication reduces the therapeutic activity of sleeping pills and antihypertensive drugs.

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

Aspirin reduces blood levels of diclofenac.

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

The drug weakens the hypoglycemic activity of antidiabetic drugs.

Cefotetan, plicamycin with valproic acid, and also cefoperazone with cefamandole increase the incidence of hypoprothrombinemia.

Gold substances 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 within the gastrointestinal tract.

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

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

Storage conditions

Diclonat P should be stored in places closed to small children. Temperature – within 15-25°C.

Shelf life

Diclonat P can be used for a period of 5 years from the date of manufacture of the therapeutic agent.

Analogues

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