Bioran

Bioran is a medication from the NSAID subgroup. Its active component is diclofenac Na (a non-steroidal element with a strong anti-inflammatory, antipyretic and analgesic effect).

The main principle of the effect of diclofenac is to slow down the biosynthesis of PG (these elements are important participants in the development of pain, inflammation, and fever). [1]

During rheumatic lesions, the analgesic and anti-inflammatory effects of drugs cause a significant reduction in the intensity of pain that occurs during movement or during a calm state, stiffness in the morning and joint swelling, and in addition, they improve the functioning of the joints.

Indications Bioran

It is used for the following violations:

• rheumatic lesions of a degenerative or inflammatory nature ( rheumatoid type arthritis , osteoarthritis, ankylosing spondylitis and spondyloarthritis);
• pain affecting the spine;
• rheumatic disorders in the soft tissue area outside the joints;
• active phase of a gouty attack;
• pain resulting from surgery or injury (accompanied by swelling and inflammation);
• severe forms of migraine attacks;
• colic of a bilious or renal nature.

Release form

The release of the therapeutic substance is realized in the form of an injection liquid - inside ampoules with a volume of 3 ml / 75 mg. The box contains 5 such ampoules.

Pharmacodynamics

In in vitro tests, diclofenac Na in values similar to those observed during therapy did not suppress the biosynthesis of proteoglycans occurring inside cartilaginous tissues.

In the case of inflammation associated with surgery or injury, the medication quickly relieves pain (spontaneous or occurring during movement) and relieves swelling caused by inflammation or postoperative wound. [2]

The medicine has a significant analgesic effect for severe and moderate pains of a non-rheumatic nature. Bioran can relieve pain and reduce the intensity of blood loss in the case of primary dysmenorrhea.

Along with this, the drug demonstrates high efficiency in the development of migraine attacks.

Pharmacokinetics

Absorption.

With an intramuscular injection of 75 mg of diclofenac, it immediately begins to be absorbed. Cmax values within plasma, with an average level of about 2.5 μg / ml, are recorded after approximately 20 minutes. Immediately after this, the plasma drug value decreases rapidly. The volumes of the absorbed active element have a linear dependence on the size of the dose of the drug.

With repeated use of drugs, the pharmacokinetics remains unchanged. If the prescribed intervals between injections of the substance are observed, its accumulation does not occur.

Distribution processes.

Protein synthesis of the substance is equal to 99.7% and is mainly realized with albumin (by 99.4%). The distribution volume indicator is 0.12-0.17 l / kg.

Also, diclofenac is found inside the synovium (its Cmax values are observed here 2-4 hours later than inside the blood plasma). The imaginary term for synovial half-life is 3-6 hours. After 2 hours from the moment of determining the plasma Cmax, the level of diclofenac inside the synovium exceeds the intraplasmic mark, and these indicators remain higher for another 12 hours.

Exchange processes.

The exchange of diclofenac is partially realized through glucuronization of an unchanged molecule, but mainly through 1-time and multiple methoxylation, which causes the formation of several metabolic elements of the phenolic type (3'-hydroxy-, 4'-, 5'-, and at the same time elements 4 'and 5 dihydroxy - with 3'-hydroxy-4'-methoxydiclofenac), most of which are transformed into conjugates of the glucuronide form. 2 of these phenolic degradation elements have bioactivity, but their expression is much weaker than that of diclofenac.

Excretion.

Systemic indicators of drug clearance are equal to 263 ± 56 ml per minute. The final half-life is 1–2 hours. The term half-life of 4 metabolic elements (including 2 components with therapeutic activity) is also short-term and is equal to 1-3 hours. At the same time, in 3'-hydroxy-4'-methoxydiclofenac, the term of half-life is longer, but it does not have a therapeutic effect at all.

About 60% of a portion of Bioran is excreted together with urine in the form of conjugates (glucuronic type) of an unchanged active element, and at the same time in the form of metabolic components, most of which are also conjugates of a glucuronic nature.

Less than 1% of excreted diclofenac has an unchanged form. The remainder of the drug portion is excreted in the form of decay components along with feces, as well as bile.

Dosing and administration

The medication is prescribed for intramuscular injections - deep inside the muscles of the buttocks. It is forbidden to administer injections for more than 2 days in a row. If necessary, therapy is continued with the use of Bioran tablets.

During the injection, in order to avoid damage to other tissues or nerves in the area of \ u200b \ u200bthe procedure, you must follow these rules. The medication is injected deep into the outer upper quadrant of the buttock muscle. Serving size is usually 75 mg (1 ampoule volume), with 1 dose per day.

In severe disorders (for example, in the case of colic), as an exception, 2 injections can be administered at a dosage of 75 mg, with an interval of several hours (the second injection must be performed in the other buttock).

Alternatively, you can use the following scheme: an injection of the drug (75 mg per day) is interspersed with oral administration of Bioran tablets (the maximum serving volume per day is 0.15 g).

• Application for children

It is forbidden to use the medicine in pediatrics (under the age of 18).

Use Bioran during pregnancy

During pregnancy Bioran is not prescribed.

If you need to use drugs during breastfeeding, you must first make a decision to cancel breastfeeding.

Contraindications

The main contraindications:

• an ulcer that affects the gastrointestinal tract;
• severe intolerance to diclofenac or other elements of the drug (among them sodium metabisulfate);
• persons with an allergic reaction to the use of aspirin or other NSAIDs (among the symptoms of allergy are urticaria, asthma attacks, or the active phase of the common cold).

Side effects Bioran

Among the side signs:

• disorders affecting the function of the gastrointestinal tract: sometimes nausea, dyspepsia, flatulence, pain in the epigastric zone and anorexia appear, and in addition, abdominal cramps, diarrhea and vomiting. Occasionally, there are ulcers in the gastrointestinal tract (may or may not be accompanied by perforation / bleeding) and bleeding from the gastrointestinal tract (melena, vomiting, or bloody diarrhea). Possible development of glossitis, stomatitis, disorders associated with the lower intestine (this includes pancreatitis, constipation, nonspecific hemorrhagic colitis and the active phase of transmural ileitis or ulcerative colitis), and changes in the work of the esophagus, as well as the appearance of diaphragm-like strictures inside the intestine;
• lesions associated with the work of the central nervous system: sometimes dizziness (at times severe) or headaches appear. Drowsiness is occasionally noted. Perhaps the development of memory impairment, insomnia, tremor, disorientation, sensitivity disorders (for example, paresthesias), depression and nightmares, and in addition to this convulsions, anxiety, irritability, psychotic symptoms and meningitis of aseptic nature;
• disorders of the activity of the sensory organs: possible auditory disorders, tinnitus, visual disturbances (diplopia or blurred vision) and taste disorders;
• signs of allergies: epidermal rashes are sometimes noted. Urticaria rarely develops. You may experience eczema or a blistering rash;
• renal dysfunction: rarely, swelling occurs. There may be acute renal failure, tubulointerstitial nephritis, changes in urinary sediment (proteinuria or hematuria), nephrotic syndrome or necrotizing papillitis;
• hepatic dysfunction: sometimes serum aminotransferase values increase. Occasionally, hepatitis develops (with or without jaundice). The appearance of fulminant hepatitis is possible;
• hematopoietic disorders: anemia (aplastic or hemolytic), leuko- or thrombocytopenia and agranulocytosis may develop;
• symptoms of intolerance: occasionally asthma appears or general anaphylactoid or anaphylactic manifestations (among them a decrease in blood pressure values). Development of pneumonia or vasculitis is possible;
• damage to the function of the CVS: pain in the sternum, tachycardia and CHF may appear, or an increase in blood pressure;
• Others: Sometimes there are symptoms in the area of the injection (induration or pain). The occurrence of local necrosis or abscesses in the area of drug administration is possible.

Overdose

There is no information that describes the typical clinical symptoms that develop in case of poisoning with Bioran.

In case of acute intoxication with an NSAID substance, symptomatic and supportive actions should be taken. For example, they are carried out in case of failure of the kidneys, suppression of respiration, a decrease in blood pressure and disorders of the gastrointestinal tract. The likelihood that hemoperfusion, forced diuresis or hemodialysis will help excrete NSAIDs is very low, because the active elements of these drugs are essentially synthesized with protein and are involved in intensive metabolic processes.

Interactions with other drugs

Digoxin and lithium substances.

The drug may increase the plasma values of digoxin or lithium.

Diuretics.

Like other NSAIDs, Bioran is able to weaken the intensity of the diuretic effect. Administration together with potassium-sparing diuretic drugs can increase serum K values (with such a combination of drugs, this indicator must be constantly monitored).

NSAID medications.

Systemic use with NSAIDs may increase the incidence of negative signs.

Anticoagulants.

Although the effect of drugs on anticoagulants has not been recorded in clinical tests, there is some information indicating an increase in the likelihood of bleeding in people using such combinations. Because of this, with such a combination, you need to constantly and very carefully monitor the patient.

Hypoglycemic substances.

In clinical tests, it was determined that Bioran can be combined with hypoglycemic drugs without changing the therapeutic effect of the latter. But there is some data on the appearance with such a combination of hyper- or hypoglycemia, which is why, when administered with a drug, it was required to change the dosage of antidiabetic agents.

Methotrexate.

It is necessary to use NSAIDs with caution if they are administered less than 24 hours before or after the administration of methotrexate, because this can increase its blood counts and potentiate its toxic activity.

Cyclosporine.

NSAIDs affect the processes of PG binding within the kidneys, which can potentiate the nephrotoxic properties of cyclosporine.

Antibacterial agents (quinolone derivatives).

There is separate information on the occurrence of seizures in people who have combined NSAIDs with quinolone derivatives.

Often, it is forbidden to mix liquid from Bioran ampoules with injection solutions of other medicines.

Storage conditions

Bioran must be kept out of the reach of children, sunlight and moisture. Do not freeze ampoules. Temperature values - maximum 25 ° С.

Shelf life

Bioran is allowed to be used within a 3-year period from the date of manufacture of the medicinal substance.

Analogs

Analogues of drugs are the medicines Diclomelan, Difen, Artrex and Diclofenac with Diclorium, and in addition Veral, Diclonac and Dorosan with Voltaren, Diclofenacol and Diclak with Diclogen, as well as Diclo-F and Diclofenaclong. In addition, the list includes Diclobene, Dicloran with Diklovit, Ortofen and Diklomax with Sodium diclofenac, Penceid and Diclofen, as well as Remetan and Naklofen with Sanfinac, Naklof and Flector, Ortofer, Uniclofen and Ortoflex with Tabak, Feloran and Ortoflex with Tabak, Feloran and Ortoflex with Tabak, Feloran and Diclofen.