Description
Pharmacological action
Pharmacotherapeutic group:
NSAIDs
ATX:
M.01.AE01 Ibuprofen
Pharmacodynamics:
Mechanism of action of ibuprofen, a derivative of propionic acid from the group of non-steroidal anti-inflammatory drugs (NSAIDs), due to the inhibition of the synthesis of prostaglandins – mediators of pain, inflammation and hyperthermia. It indiscriminately blocks cyclooxygenase 1 (COX-1) and cyclooxygenase 2 (COX-2), as a result of which it inhibits prostaglandin synthesis.
It has a quick directed action against pain (analgesic), antipyretic and anti-inflammatory effect. Ibuprofen inversely inhibits platelet aggregation.
Pharmacokinetics:
Ibuprofen is absorbed from the digestive tract by approximately 80%. Absorption decreases slightly when taking the drug after a meal. The time to reach maximum concentration (TCmax) when taken on an empty stomach is 45 minutes, when taken after meals – 1.5-2 hours, in synovial fluid – 2-3 hours.
Ibuprofen is 90% bound to blood proteins, mainly to albumin. It undergoes a presystem and post-system metabolism in the liver. After absorption, about 60% of the pharmacologically inactive R-form of ibuprofen slowly transforms into the active S-form. The isoenzyme of CYP2C9 takes part in the metabolism of the drug.
Has a two-phase elimination kinetics with a half-life (T1 / 2) of 2-2.5 hours. It is excreted by the kidneys (unchanged no more than 1%) and to a lesser extent with bile.
Indications
Used for headache, migraine, toothache, painful menstruation, neuralgia, back pain, muscle and rheumatic pain in case of fever with flu and colds.
Designed for symptomatic therapy, reduce pain and inflammation at the time of use, does not affect the progression of the disease.
Contraindications
– Hypersensitivity to ibuprofen and other components of the drug
– erosive and peptic ulcer of the gastrointestinal tract (including peptic ulcer of the stomach and duodenum, peptic ulcer, peptic ulcer) complete or incomplete combination of bronchial asthma, triggered by the use of NSAIDs
– severe heart failure
– severe renal failure (CC less than 30 ml / min)
– progressive kidney disease
– severe hepatic failure or active liver disease
– condition after coronary artery bypass grafting srdlkremen .
With caution:
With caution, the drug is used for cirrhosis of the liver with portal hypertension, hyperbilirubinemia, gastric ulcer and duodenal ulcer (history), gastritis, enteritis, colitis of hepatic porphyria, liver and / or renal failure, nephrotic syndrome insufficiency, arterial hypertension coagulation disorders, blood diseases of unknown etiology (leukopenia and anemia), old age, pregnancy (I-II trimester), coronary heart disease, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral artery disease, smoking, chronic renal failure (CC 30-60 ml / min ), the presence of Helicobacter pylory infection, prolonged use of NSAIDs, frequent alcohol consumption, severe somatic diseases, systemic lupus erythematosus or other autoimmune diseases of the connective tissue (increased risk of developing aseptic eningitis), while taking oral GCS (including prednisone), anticoagulants (including warfarin), antiplatelet agents (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine Paroxegin. Sertraline).
Use during pregnancy and lactation
In animal studies, no adverse effect of ibuprofen on the fetus was found. In the absence of a sufficient number of well-controlled observations in humans, the drug should be used in the first and second trimesters of pregnancy only in cases of urgent need, if the potential benefit to the mother outweighs the potential risk to the fetus and baby.
Ibuprofen inhibits uterine muscle contraction. The effect of ibuprofen on the fetus can cause premature closure of the botallal duct, which can lead to the development of pulmonary hypertension in the newborn. Ibuprofen should not be used at the end (third trimester) of pregnancy.
No isolation of ibuprofen with breast milk was detected. However, due to the limited volume of these studies and the possible adverse effect of inhibition of prostaglandin synthesis in a newborn, it is not recommended to use the drug during breastfeeding.
Special instructions
During treatment, monitoring of the picture of peripheral blood and the functional state of the liver and kidneys is necessary.
When symptoms of gastropathy appear, careful monitoring is indicated, including esophagogastroduodenoscopy, a blood test to determine hemoglobin, hematocrit, and feces for occult blood.
To prevent the development of NSAIDs, gastropathy is recommended to be combined with prostaglandin E (misoprostol) preparations.
If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the study.
Before starting therapy, patients with a history of arterial hypertension and / or with heart failure should be careful and consult a specialist, since in such patients fluid retention, arterial hypertension, and edema associated with NSAIDs were noted.
Prolonged use may increase the risk of acute coronary disease or stroke.
In patients with a history of bronchial asthma or allergic diseases, the drug may cause an attack or bronchospasm.
Ethanol is not recommended during treatment.
Ibuprofen has an antiplatelet effect (weaker compared with acetylsalicylic acid), which requires caution in the appointment of patients with blood clotting disorders, as well as taking anticoagulants.
It is recommended that you take the drug as soon as possible and at the minimum effective dose necessary to eliminate the symptoms.
Drugs that suppress cyclooxygenase and prostaglandin synthesis can affect ovulation, disrupting female reproductive function (reversible after discontinuation of treatment).
Impact on the ability to drive transp. Wed and fur .:
During the treatment period, it is necessary to refrain from those types of activities where increased attention and speed of mental and motor reaction is required.
Composition
1 capsule contains:
Active ingredient:
ibuprofen – 200,000 mg.
Excipients:
-tocopherol acetate – 0.372 mg,
povidone 17 PF – 30,000 mg,
macrogol 600 – 414.628 mg.
Gelatin capsule shell composition:
gelatin,
sorbitol non-crystallizing solution,
glycerol,
methyl parahydroxybenzoate,
purified water,
dye red charming E-129.
Description:
Soft gelatin capsules oval in shape, with a seam, transparent, red.
The contents of the capsules is a colorless or pinkish clear liquid.
Dosage and administration
Next ® Uno Express is prescribed for adults and children over 12 years old by mouth after meals, 200 mg (1 capsule) 3-4 times a day. Capsules should be washed down with a glass of water.
To achieve a quick therapeutic effect, the dose can be increased to 400 mg (2 capsules) 3 times a day. When the therapeutic effect is achieved, the daily dose of the drug is reduced to 600-800 mg.
The maximum daily dose for adults is 1200 mg (do not take more than 6 capsules in 24 hours).
The maximum daily dose for children 12-18 years old is 800 mg.
A repeated dose should be taken no earlier than 4 hours later.
If, after using the drug for 5 days, the pain syndrome or for 3 days, the increased body temperature persists or intensifies, you should stop taking it and consult your doctor.
Side effects
When using the drug Next® Uno Express for 2-3 days, side effects are practically not observed.
In case of prolonged use, the following side effects may occur:
– from the gastrointestinal tract (GIT): NSAID gastropathy (abdominal pain, heartburn, diarrhea, flatulence, pain and discomfort in the epigastric region), ulceration of the gastrointestinal mucosa (in some cases complicated by perforation and bleeding) irritation dry mouth or mouth pain, ulceration of the gums, aphthous stomatitis, pancreatitis, constipation, indigestion, nausea, loss of appetite, vomiting, hepatitis
– from the respiratory system: shortness of breath, bronchospasm, exacerbation of bronchospasm ialnoy
asthma – hearing impairment: hearing loss, ringing or noise in the ears
– on the part of the central and peripheral nervous system: insomnia, anxiety, nervousness and irritability, agitation, depression, confusion, hallucinations, rarely aseptic meningitis (more often in patients with autoimmune diseases), headache, dizziness, drowsiness
from the cardiovascular system: development or worsening of heart failure, tachycardia, increased blood pressure
from the urinary system: acute renal failure, allergic nephritis , nephrotic syndrome (edema), polyuria,
cystitis – from the hemopoietic organs: hemolytic anemia, aplastic anemia, thrombocytopenia and thrombocytopenic purpura, agranulocytosis, leu accumulation, pancytopenia
– from the side of the organs of vision: reversible toxic amblyopia, blurred vision or double vision, dryness and irritation of the eyes, swelling of the conjunctiva and eyelids (allergic genesis). scotoma.
color vision disorders – allergic reactions: skin rash (usually erythematous, urticaria), pruritus, Quincke’s edema, anaphylactoid reactions, anaphylactic shock, bronchospasm, fever, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), eosinophilia, allergic rhinitis: .
The risk of ulceration of the mucous membrane of the gastrointestinal tract, bleeding (gastrointestinal, gingival, uterine, hemorrhoidal), visual impairment (color vision disorders, scotomas, amblyopia) increases with prolonged use in large doses.
If side effects occur, you should stop taking the drug and consult a doctor.
Lab performance:
– bleeding time (may increase)
– serum glucose concentration (may decrease)
– creatinine clearance (may decrease)
– hematocrit or hemoglobin (may decrease)
– serum creatinine concentration (may increase)
– hepatic activity may increase).
Drug Interactions
Microsomal oxidation inducers (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active ibuprofen metabolites, increasing the risk of severe hepatotoxic reactions.
Microsomal oxidation inhibitors reduce the risk of hepatotoxic effects of ibuprofen.
Ibuprofen reduces the antihypertensive effect of antihypertensive drugs (ACE inhibitors, slow calcium channel blockers, etc.), the natriuretic and diuretic effectiveness of furosemide and hydrochlorothiazide reduces the effectiveness of uricosuric drugs, enhances the ulcerogenic effect of glucocorticosteroids, colchicine, ethanol enhances the effect of oral hypoglycemic agents and insulin increases the concentration in the blood of digoxin, lithium preparations and methotrexate.
Ibuprofen enhances the undesirable effects of estrogen when used together.
Antacids and colestyramine decrease ibuprofen absorption.
Caffeine enhances the analgesic effect of ibuprofen.
With the simultaneous administration of ibuprofen, it reduces the anti-inflammatory and antiplatelet effect of acetylsalicylic acid (it is possible to increase the incidence of acute coronary insufficiency in patients receiving small doses of acetylsalicylic acid as an antiplatelet agent after starting ibuprofen).
When prescribed with anticoagulant and thrombolytic drugs (alteplase, streptokinase, urokinase), the risk of bleeding increases at the same time.
With the combined use of ibuprofen and cefamandol, cefoperazone, cefotetan. valproic acid increases the incidence of hypoprothrombinemia.
Myelotoxic drugs enhance the hematotoxicity of the drug.
Cyclosporine and gold preparations enhance the effect of ibuprofen on the synthesis of prostaglandins in the kidneys, which is manifested by an increase in nephrotoxicity.
Ibuprofen increases the plasma concentration of cyclosporin and the likelihood of its hepatotoxic effects.
Medicines that block tubular secretion reduce excretion and increase the plasma concentration of ibuprofen.
Ibuprofen may decrease the effectiveness of mifepristone, so ibuprofen should be started no earlier than 8-12 days after taking mifepristone.
With the simultaneous administration of ibuprofen and tacrolimus, an increased risk of nephrotoxicity is possible.
The simultaneous use of ibuprofen and zidovudine may lead to increased hematological toxicity.
There is evidence of an increased risk of hemarthrosis and hematomas in HIV-positive hemophilia patients treated with zidovudine and ibuprofen.
Patients receiving co-treatment with ibuprofen and the quinolone antibiotics may increase the risk of seizures.
Overdose
Symptoms: abdominal pain, nausea, vomiting, lethargy, drowsiness, depression, headache, tinnitus, metabolic acidosis, coma, acute renal failure, lowering blood pressure, bradycardia, tachycardia, fibrillation, pre-pulmonary fibrillation.
Treatment: gastric lavage (only within an hour after ingestion), activated charcoal, alkaline drink, forced diuresis, symptomatic therapy.
Storage conditions
In the dark place at a temperature of no higher than 25 ° C.
Keep out of the reach of children.
Expiration
2 years.
Do not use after the expiry date stated on the packaging.
pharmacy dispensing terms without a prescription
Form of Treatment
tablets
Appointment
Pregnant I and II tr Maistre to doctor appointments, For Adults, For children 12 years and older
Indications
Dislocations and sprains, From lumbago, Swelling after injuries and operations, From neuritis, From arthrosis and arthritis, Grippa, Grippa, migraines, Injuries, From myositis, From rheumatoid arthritis, From osteoarthritis, Cold Cold
Possible product names
Next Uno Express capsules 200 mg 20 pcs.
