Dexibuprofen

Pharmacological properties

Dexibuprofen is a pharmacologically active isomer of racemic ibuprofen. NSAIDs with antipyretic and analgesic properties. the action of the drug is based on the suppression of prostaglandin synthesis, it is capable of inhibiting the production of leukotrienes, reducing inflammatory edema due to the effect on polymorphonuclear leukocytes and reducing the production of nitric oxide, mitochondrial fatty acid oxidation.

Dexibuprofen is rapidly and completely absorbed in the small intestine. C_max in the blood is reached 2 hours after taking 200 mg of the drug. Excretion from the synovial fluid is slow, due to which a constant concentration is maintained, independent of the concentration of the drug in the blood plasma.

It is metabolized in the liver, after which it is excreted in the form of inactive metabolites, mainly (90%) by the kidneys, the rest with bile.

T_½ - 1.8-3.5 hours, binding to plasma proteins - about 99%. When using dexibuprofen with food, the time to reach C increases_max in the blood from 2.1 to 2.8 hours and decrease C_max in blood plasma from 20.6 to 18.1 μg / ml, but food does not affect the degree of absorption.

Indications

Symptomatic therapy for mild to moderate pain of various origins: toothache, back pain, joints, muscles, rheumatic pain, dysmenorrhea.

Application

The dosage regimen is set individually, taking into account the intensity of the pain syndrome. adults are usually prescribed 1-2 tablets (200-400 mg of dexibuprofen) 3 times a day after meals. the recommended starting dose is 200 mg of dexibuprofen. the recommended daily dose is 600–900 mg of dexibuprofen, divided into 3 doses. the highest daily dose is 1200 mg, the highest single dose is 400 mg. with dysmenorrhea, the highest single dose is 300 mg, the maximum daily dose is 900 mg. preferably taken with food. the drug is intended for symptomatic relief of pain, but if the symptoms of the disease persist for 3 days, accompanied by high body temperature, headache or other phenomena, it is necessary to clarify the diagnosis and additional correction of the treatment regimen.

Use in the elderly. It is recommended to start therapy with low doses. The dose can be increased to the recommended daily dose only after a good tolerability of the drug is established.

Use in patients with impaired liver and kidney function. Patients with moderate impaired liver and kidney function should be wary of starting the use of the drug in a reduced dose. Zotek is contraindicated in patients with severely impaired liver or kidney function.

Contraindications

• Hypersensitivity to dexibuprofen or other NSAIDs and other components of the drug in the form of an asthma attack, bronchospasm, acute rhinitis, or nasal polyps, urticaria, and angioedema in history; ba; gastrointestinal bleeding, other bleeding, or bleeding disorders; hemorrhagic diathesis and other coagulation disorders or anticoagulant therapy; erosive and ulcerative lesions of the gastrointestinal tract in the acute phase, ulcerative colitis in the acute phase, Crohns disease in the acute phase; severe violations of the liver and kidneys; leukopenia, thrombocytopenia; uncontrolled ag, heart failure; diseases of the optic nerve, violation of color perception.

Side effects

From the digestive tract: dyspepsia, diarrhea, nausea, vomiting, abdominal pain, with prolonged use - stomach ulcer and duodenal ulcer, bleeding from the gastrointestinal tract, ulcerative stomatitis, rarely - gastrointestinal perforation, flatulence, constipation, esophagitis, esophageal strick. exacerbation of diverticulitis, nonspecific hemorrhagic colitis, ulcerative colitis or Crohns disease.

From the skin: rash, urticaria, pruritus, purpura (including allergic purpura), polymorphic erythema, epidermal necrolysis, alopecia, photosensitivity, Stevens-Johnson syndrome, acute toxic epidermal necrolysis (Lyells syndrome) and allergic vasculitis.

Hypersensitivity reactions: fever, headache, rhinitis, bronchospasm, asthma, tachycardia, arterial hypotension, shock, anaphylactic reactions, angioedema, systemic lupus erythematosus, and other collagenoses.

From the nervous system: dizziness, fatigue, drowsiness, insomnia, anxiety, visual hallucinations, psychotic reactions, irritability, depression, disorientation, double vision, ringing or tinnitus, aseptic meningitis.

On the part of the blood: prolonged blood coagulation, rarely thrombocytopenia, leukopenia, granulocytopenia, pancytopenia, agranulocytosis, aplastic anemia, hemolytic anemia.

From the cardiovascular system: peripheral edema. An increase in blood pressure and heart failure may occur, especially in the elderly.

In patients with hypertension or impaired renal function, fluid retention is possible.

From the urinary system: interstitial nephritis, nephrotic syndrome, renal failure cannot be excluded taking into account the experience of using NSAIDs, liver failure.

Other: in very rare cases, there may be an increase in perspiration.

special instructions

Caution should be used in patients with a history of gastrointestinal diseases. persons of this group require careful examination and observation. when prescribing the drug to patients with a violation of the cardiovascular system, ag, renal and liver failure, especially with concomitant treatment with diuretics, it is necessary to take into account the existing risk of fluid retention and impaired renal function. in such patients it is recommended to use the lowest dose and regularly monitor renal function.

With extreme caution, the drug should be used in the elderly.

It should be used with caution in patients with systemic lupus erythematosus and connective tissue diseases, since they may be at risk of disorders from the central nervous system and side effects from the kidneys.

It is necessary to monitor renal and hepatic function in patients using dexibuprofen for a long time.

Use during pregnancy and lactation. The drug is not recommended for use during pregnancy, as well as for women planning a pregnancy.

Dexibuprofen passes into breast milk. During breastfeeding, the use of dexibuprofen is contraindicated. If treatment is necessary, breast-feeding should be discontinued.

Children. The drug is not used in pediatric practice.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. With a single or short-term use, the drug does not affect the reaction rate and the ability to drive vehicles or work with other mechanisms. During prolonged use, the possibility of the appearance of such an undesirable reaction as dizziness is possible, which can affect the reaction rate when driving vehicles or working with other mechanisms.

Interactions

Do not use NSAID combinations, as kidney damage may occur with the risk of an arrester.

NSAIDs should be used with caution with other drugs, which may increase the risk of gastrointestinal bleeding, perforation and impaired renal function.

When using Zotek with any other drug that inhibits COX / prostaglandin synthesis, fertility may be impaired, so this combination is not recommended for women planning a pregnancy.

When dexibuprofen interacts with oral anticoagulants, acetylsalicylic acid, prolonged blood clotting time and inhibition of platelet aggregation may occur.

With the simultaneous administration of methotrexate at a dose of 15 mg / kg kg, blood tests and a study of kidney function are required during the first weeks, especially in the elderly. Methotrexate administered at a dose of ≥15 mg / kg should be used 24 hours after dexibuprofen. Due to the increase in the concentration of methotrexate in blood plasma as a result of a decrease in its excretion by the kidneys, the toxicity of methotrexate increases, therefore, the simultaneous use of dexibuprofen is not recommended.

Lithium: NSAIDs can increase the concentration of lithium in the blood, reducing its excretion by the kidneys. The combination is not recommended.

With extreme caution, you should combine antihypertensive drugs with NSAIDs, since the effectiveness of β-adrenergic blockers decreases.

The simultaneous use of ACE inhibitors or angiotensin II receptor antagonists can reduce the hypotensive effect of angiotensin II receptor antagonists and ACE inhibitors, may increase the risk of acute renal failure, especially in patients with a history of renal function or elderly people.

Cyclosporin, tacrolimus with simultaneous use may increase the risk of nephrotoxicity due to a decrease in the synthesis of prostaglandins in the kidneys. It is necessary to control renal function, especially in the elderly.

Glucocorticoids with simultaneous use can increase the likelihood of gastrointestinal bleeding.

With the combined use of the drug Zotek with digoxin, the concentration of the latter in the blood plasma and toxicity increase.

Zotek can replace phenytoin when bound to proteins, possibly leading to an increase in blood concentration and toxicity. Therefore, monitoring the concentration of phenytoin in the blood is recommended.

Thiazide, thiazide-like, loop and potassium-sparing diuretics with simultaneous use with NSAIDs can increase the risk of developing renal failure and cause a secondary decrease in renal circulation.

Drugs that increase the concentration of potassium while using dexibuprofen, lead to an increase in the concentration of potassium and require determination of the concentration of potassium in the blood.

Thrombolytics, ticlopidine, antiplatelet agents, while used with NSAIDs, can increase the antiplatelet effect.

Overdose

Symptoms: dizziness, stunning, abdominal pain, nausea, vomiting, drowsiness, headache, nystagmus, tinnitus, ataxia, gastrointestinal bleeding, arterial hypotension, hypothermia, metabolic acidosis, impaired renal function, rarely - loss of consciousness.

Treatment: symptomatic, no specific antidote.

You can apply gastric lavage with water (only during the first hour after ingestion). Assign activated carbon. Hemodialysis is ineffective due to the high degree of protein binding.

Storage conditions

In the original packaging at a temperature not exceeding 25 ° C.