Instructions Ibuprofen-Zdorovye ultracap capsules 200 mg blister No. 20
Composition
active ingredient: ibuprofen;
1 soft capsule contains ibuprofen in terms of 100% substance 200 mg or 400 mg;
Excipients: potassium hydroxide; purified water; polyethylene glycol 600; capsule shell containing: gelatin; sorbitol liquid, partially dehydrated; glycerin; methylparaben (E 218); propylparaben (E 216); Ponceau 4R (E 124).
Dosage form
Soft capsules.
Main physicochemical properties: oval transparent soft gelatin capsules from light red to dark red in color, containing a viscous solution.
Pharmacotherapeutic group
Nonsteroidal anti-inflammatory and antirheumatic drugs. Propionic acid derivatives. ATC code M01A E01.
Pharmacological properties
Pharmacodynamics
Ibuprofen is a phenylpropionic acid derivative with analgesic, anti-inflammatory and antipyretic properties. Experimental data suggest that ibuprofen may inhibit the effect of low-dose acetylsalicylic acid on platelet aggregation when administered concomitantly. Some pharmacodynamic studies have shown that a single effect of acetylsalicylic acid on thromboxane formation or platelet aggregation was observed when ibuprofen 400 mg was administered immediately or within 30 minutes of immediate-release acetylsalicylic acid (81 mg). Although there is uncertainty about the extrapolation of these data to the clinical situation, it cannot be excluded that regular long-term use of ibuprofen may reduce the cardioprotective effect of low-dose acetylsalicylic acid. With non-systematic use of ibuprofen, such a clinically significant effect is considered unlikely (see section "Interaction with other medicinal products and other forms of interaction").
Pharmacokinetics
When administered orally, reconstituted ibuprofen (soft capsule) is rapidly absorbed after administration on an empty stomach. The Cmax value is reached in approximately 35 minutes compared to conventional tablets (approximately 90 minutes), i.e. the active substance is absorbed more than twice as fast as with conventional ibuprofen tablets. When taken with food, peak levels occur after 1–2 hours. The analgesic effect persists for 8 hours. These values are obtained only from pharmacokinetic studies. The binding of ibuprofen to plasma proteins is approximately 99%. In the first 24 hours after oral administration, 75–85% of ibuprofen is excreted in the urine (mainly as two inactive metabolites), while the rest is excreted in the intestines after excretion in the bile. The drug is completely excreted within 24 hours. The half-life of ibuprofen is approximately 2 hours.
In limited studies, ibuprofen has been found in breast milk at very low concentrations.
In randomized, double-blind clinical trials, ibuprofen soft capsules at a dosage of 400 mg showed a faster onset of pain relief for episodic tension-type headache and, overall, greater efficacy for dental pain than a single dose of 2×500 mg paracetamol.
In a randomized, double-blind, 6-hour, parallel-group clinical trial, 59 patients with moderate to severe postoperative pain were treated with ibuprofen 400 mg soft capsules. 98% of patients experienced significant analgesic effects, with onset of action within 10.2 (9.0–13.8) minutes.
Indication
The drug has analgesic and anti-inflammatory effects and is recommended for the relief of acute pain of mild to moderate severity in dysmenorrhea, back pain, muscle pain, headache, migraine, toothache, to reduce fever, as well as to relieve symptoms of colds and flu.
The medicine is recommended for adults, adolescents and children aged 12 years and over.
Contraindication
Hypersensitivity to the active substance or any of the excipients.
Hypersensitivity to acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs.
History of bronchospasm, asthma, cold symptoms, or urticaria with other nonsteroidal anti-inflammatory drugs (NSAIDs).
Gastric or duodenal ulcer/bleeding, active or history of, inflammatory bowel disease, gastrointestinal bleeding, cerebrovascular bleeding or other active bleeding; hematological diseases.
Severe hepatic insufficiency, severe renal insufficiency or severe heart failure (NYHA class IV).
Immediately before or after cardiac surgery.
The last trimester of pregnancy.
Age up to 12 years.
Interaction with other medicinal products and other types of interactions
Experimental data suggest that ibuprofen may competitively inhibit the effect of low-dose acetylsalicylic acid on platelet aggregation when used concomitantly. Although there is uncertainty about the extrapolation of these data to the clinical situation, it cannot be excluded that regular long-term use of ibuprofen may reduce the cardioprotective effect of low-dose acetylsalicylic acid. With non-systematic use of ibuprofen, such a clinically significant effect is considered unlikely (see section "Pharmacodynamics").
NSAIDs may enhance the effects of sulfonamides and anticoagulants and reduce the effects of antihypertensives, furosemide, thiazide diuretics and ß-blockers.
Ibuprofen enhances the hyperkalemic effect of potassium salts, other non-steroidal NSAIDs, heparins (low molecular weight heparins or unfractionated heparins), cyclosporine, tacrolimus and trimethoprim.
NSAIDs may reduce the effect of diuretics and other antihypertensive drugs. In some patients with impaired renal function (e.g., dehydrated patients or elderly patients with impaired renal function), the concomitant use of cyclooxygenase inhibitors with ACE inhibitors, beta-blockers or angiotensin II antagonists may lead to further deterioration of renal function, including acute renal failure, which is usually reversible. Therefore, such a combination should be used with caution, especially in elderly patients. Patients should be adequately hydrated and attention should be paid to monitoring renal function after initiation of combination therapy and periodically thereafter.
The increase in serum lithium levels after ibuprofen administration is clinically significant.
Ibuprofen may increase serum digitalis concentrations. Therefore, digitalis and glycoside blood levels should be monitored in patients with impaired renal function or congestive heart failure.
Ibuprofen may increase the plasma concentration of pharmacologically active free phenytoin. Therefore, patients receiving long-term treatment with ibuprofen should be monitored.
Concomitant use of ibuprofen with moderate to high doses of methotrexate may lead to severe and fatal methotrexate toxicity. There is an increased risk of toxicity from this combination in patients with renal insufficiency, even when methotrexate is administered at low doses (≤ 20 mg/week).
Some antacids may increase the absorption of ibuprofen. However, this is only of clinical significance with long-term use of ibuprofen.
When using anticoagulants, it should be taken into account that prolonged use of ibuprofen may increase the risk of bleeding.
Concomitant use with corticosteroids and other NSAIDs increases the risk of gastrointestinal disorders and bleeding.
Ibuprofen should be used with caution with selective serotonin reuptake inhibitors (SSRIs) as there is an increased risk of gastrointestinal bleeding.
The possibility of reduced effectiveness of intrauterine contraceptives is much debated.
Application features
Do not use in combination with other analgesics, e.g. NSAIDs.
Use with caution in patients with bronchial asthma or allergic diseases, including a history of them. In such patients, the drug may cause bronchospasm. If other NSAIDs have caused bronchospasm, the drug should not be used. Ibuprofen may cause a severe allergic reaction (e.g., skin redness, rash, blisters), especially in patients who are hypersensitive to acetylsalicylic acid.
To reduce the risk of side effects, the minimum effective dose should be used for the minimum period necessary to eliminate the symptoms of the disease (see gastrointestinal and cardiovascular risks below).
The drug should be used with caution in patients with kidney and heart disease, cirrhosis or other liver damage, as kidney function may deteriorate. The drug should be used at the lowest effective dose and renal function should be monitored.
The drug should only be used after careful benefit/risk assessment in patients with existing systemic lupus erythematosus or other autoimmune diseases due to the risk of aseptic meningitis or renal failure.
Ibuprofen can relieve fever and inflammation, reducing their diagnostic value as symptoms of another disease that may exist.
Some evidence suggests that the use of drugs that inhibit cyclooxygenase, and therefore prostaglandin synthesis, negatively affects female fertility and is therefore not recommended for women attempting to conceive. This effect is reversible and disappears after discontinuation of treatment.
NSAIDs may mask the symptoms of infection and fever, which may delay appropriate treatment and thus complicate the course of the disease. This has been observed in bacterial community-acquired pneumonia and bacterial complications of varicella. When NSAIDs are used for fever or for pain relief in infections, monitoring for infection is recommended. In the outpatient setting, the patient should seek medical attention if symptoms persist or worsen.
Effect on the gastrointestinal tract.
Elderly: Adverse reactions associated with NSAIDs, especially gastrointestinal bleeding and perforation, may be more common in the elderly and may be fatal (see section 4.2).
Gastrointestinal bleeding, ulceration or perforation, which can be fatal, can occur at any time during treatment with any NSAID, with or without warning symptoms, and with or without a history of serious gastrointestinal disease. The risk of gastrointestinal bleeding, ulceration or perforation increases with increasing NSAID dose in patients with a history of ulcer disease, especially complicated by bleeding or perforation (see section 4.3), or in the elderly. In such patients, treatment should be started at the lowest possible dose. In these patients, as well as in patients requiring concomitant use of low doses of acetylsalicylic acid or other medicinal products that may increase the risk of gastrointestinal events, combination therapy with protective agents (e.g. misoprostol or proton pump inhibitors) is recommended (see below and section “Interaction with other medicinal products and other forms of interaction”). Patients with a history of gastrointestinal toxicity, especially elderly patients, should be informed of any unusual gastrointestinal symptoms (especially gastrointestinal bleeding), particularly at the beginning of treatment.
Caution should be exercised when treating patients who are taking concomitant medications that may increase the risk of ulceration or bleeding, such as oral corticosteroids, anticoagulants (e.g. warfarin), selective serotonin reuptake inhibitors or antiplatelet agents (e.g. acetylsalicylic acid) (see section 4.5).
In the event of gastrointestinal bleeding or ulceration in patients receiving ibuprofen, treatment should be discontinued immediately.
Dehydrated teenagers are at risk of kidney damage.
Effects on the cardiovascular and cerebrovascular systems.
Clinical studies have shown that some NSAIDs (including ibuprofen) may slightly increase the risk of arterial thrombotic events (e.g. myocardial infarction, stroke), especially at higher doses (2400 mg/day) over a long period. Overall, epidemiological studies have shown that ibuprofen at low doses (e.g. ≤ 1200 mg/day) is not associated with an increased risk of arterial thrombotic events.
Patients with uncontrolled hypertension, congestive heart failure (NYHA class II-III), ischemic heart disease, peripheral arterial disease and/or cerebrovascular disease should use ibuprofen only after careful clinical assessment and avoid high doses (2400 mg per day).
The clinical picture should also be carefully assessed before starting long-term treatment in patients with risk factors for cardiovascular complications (e.g., hypertension, hyperlipidemia, diabetes mellitus, smoking), especially if high doses of ibuprofen (2400 mg per day) are required.
Severe skin reactions.
Serious (sometimes fatal) skin reactions such as exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis have been reported rarely with NSAIDs (see section 4.8). The risk of these reactions is greatest early in therapy, with most occurring within the first month of treatment. Acute generalised exanthematous pustulosis (AGEP) has been reported with ibuprofen-containing products. Ibuprofen should be discontinued at the first appearance of skin rash, mucosal lesions or any other sign of hypersensitivity.
The medicine contains methylparaben (E 218) and propylparaben (E 216), which may cause allergic reactions (possibly delayed).
The medicine contains ponceau 4R (E 124), which may cause allergic reactions.
This medicinal product contains sorbitol. If you have been told by your doctor that you have an intolerance to some sugars, contact your doctor before taking this medicinal product.
Use during pregnancy or breastfeeding
Inhibition of prostaglandin synthesis may adversely affect pregnancy and/or embryonal/fetal development. Based on epidemiological data, there is an increased risk of premature birth and of cardiac malformations and heart failure following the use of prostaglandin synthesis inhibitors in early pregnancy. The absolute risk of cardiovascular malformations increased from less than 1% to approximately 1.5%. The risk is believed to increase with increasing dose and duration of therapy.
In animal studies, the use of prostaglandin synthesis inhibitors has resulted in increased pre- and post-implantation losses and embryo/fetal lethality. In addition, animal studies have reported an increased incidence of various developmental anomalies (e.g. cardiovascular) when a prostaglandin synthesis inhibitor was used during the period of organogenesis.
Ibuprofen should not be used during the first and second trimesters of pregnancy unless clearly necessary. If ibuprofen is used by a woman attempting to conceive, or during the first and second trimesters of pregnancy, the lowest possible dose should be used for the shortest possible period of time.
During the third trimester of pregnancy, prostaglandin synthesis inhibitors may pose the following risks:
for the fetus:
cardiopulmonary toxicity (early closure of the ductus arteriosus and pulmonary hypertension);
impaired kidney function, which can lead to renal failure associated with oligohydramnios;
for the mother and newborn at the end of pregnancy:
possible increase in bleeding time: anti-aggregation effect, which may develop even after the use of very low doses;
suppression of uterine contractions, leading to a delay or increase in the duration of labor.
Therefore, ibuprofen is contraindicated during the third trimester of pregnancy.
Breast-feeding.
Ibuprofen passes into breast milk only in very low concentrations and is unlikely to have any adverse effects on a breastfed infant.
Fertility.
The use of drugs that inhibit cyclooxygenase/prostaglandin synthesis has been shown to negatively affect female fertility through effects on ovulation. This effect is reversible and disappears after discontinuation of treatment (see section 4.4).
Ability to influence reaction speed when driving vehicles or other mechanisms
Patients who experience dizziness, drowsiness or visual disturbances while taking ibuprofen should avoid driving or operating machinery. Single administration or short-term use of ibuprofen usually does not require any special precautions. This mainly applies to the simultaneous use of the drug with alcohol.
When used in accordance with the recommended doses and duration of treatment, the drug does not affect the reaction speed when driving or working with other mechanisms.
Method of administration and doses
To reduce the risk of side effects, the minimum effective dose should be used for the minimum period necessary to eliminate the symptoms of the disease (see section "Special instructions for use").
Dosage.
According to all indications
Adults, adolescents and children over 12 years of age: 1 capsule of 400 mg or 2 capsules of 200 mg.
The dose should not be repeated sooner than 4 hours later.
Maximum daily dose: 1200 mg ibuprofen (3 capsules of 400 mg or 6 capsules of 200 mg).
If symptoms of the disease in children or adolescents aged 12 years and older persist for more than 3 days or if symptoms worsen, a doctor should be consulted.
Method of administration and doses
For oral use only. Capsules should be taken with water.
Children: The drug is contraindicated in children under 12 years of age (see section "Contraindications").
Overdose
Symptoms: dizziness, headache, nausea, vomiting, abdominal pain, drowsiness, hypotension, liver dysfunction, hyperkalemia, vertigo, convulsions, loss of consciousness, renal failure, shortness of breath, respiratory depression. In severe intoxication, metabolic acidosis may occur.
Appropriate supportive therapy, gastric lavage, and correction of severe electrolyte imbalance are required.
Adverse reactions
Adverse reactions are classified according to their frequency of occurrence as follows: very common (≥ 1/10), common (≥ 1/100 to < 1/1000), uncommon (≥ 1/10
In particular, the risk of gastrointestinal bleeding is dose and duration dependent. See section 4.4 for known risk factors.
The adverse reactions listed below, except for some rare cases, occurred with short-term use and with daily doses up to 1200 mg.
Infections and infestations
Very rare: meningitis.
Blood and lymphatic system disorders
Very rare: haematopoietic disorders (anaemia, aplastic anaemia, haemolytic anaemia, leukopenia, thrombocytopenia, pancytopenia, agranulocytosis). Early symptoms of these disorders may include fever, sore throat, superficial mouth ulcers, flu-like symptoms, severe fatigue, epistaxis and skin bleeding. Occasionally, a decrease in haematocrit and haemoglobin may occur.
Very rare: Aseptic meningitis has been reported in some cases during treatment with ibuprofen in patients with autoimmune diseases (systemic lupus erythematosus, mixed connective tissue disease). Symptoms: neck stiffness, headache, nausea, vomiting, fever, confusion.
From the nervous system
Uncommon: headache, dizziness, stroke.
Very rare: irritability.
From the organs of vision
Uncommon: visual disturbances.
Rare: toxic amblyopia.
From the side of the organs of hearing and labyrinth
Rare: tinnitus, dizziness.
From the heart
Very rare: arrhythmias, myocardial infarction, angina pectoris. Oedema, hypertension and heart failure have been reported with the use of NSAIDs.
Respiratory and mediastinal disorders
Patients who have or have had bronchial asthma or allergic diseases may experience bronchospasm.
Gastrointestinal tract
Uncommon: gastrointestinal disorders, e.g. dyspepsia, abdominal pain, nausea.
Rare: diarrhea, flatulence, constipation, bloating, vomiting, gastrointestinal ulcer, gastritis.
Very rare: gastrointestinal ulcers, overt gastrointestinal bleeding or perforation, abdominal pain, Crohn's disease, exacerbation of colitis, hematemesis, melena, ulcerative stomatitis.
Hepatobiliary system
Very rare: liver function abnormalities, including increased serum transaminase levels, especially with prolonged use; hepatic failure, hepatitis, jaundice.
Skin and subcutaneous tissue disorders
Rare: angioedema.
Very rare: severe skin lesions (e.g. erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, bullous dermatitis), alopecia, purpura. Not known: drug hypersensitivity syndrome with eosinophilia and systemic symptoms (DRESS syndrome), acute generalized exanthematous pustulosis (AGEP), photosensitivity reactions.
Renal and urinary disorders
Very rare: haematuria, interstitial nephritis, proteinuria, urinary retention, fluid retention (e.g. peripheral oedema), nephrotic syndrome. These symptoms may be manifestations of renal disease or even renal failure. High creatinine and urea levels have been reported. Papillary necrosis may develop, especially with long-term treatment.
General disorders and administration site conditions
Uncommon: hypersensitivity reactions (skin redness, rash, maculopapular rash, itching, urticaria), exacerbation of asthma (sometimes with hypotension), bronchospasm, asthmatic breathing (wheezing).
Very rare: severe hypersensitivity reactions (anaphylaxis). Symptoms: facial swelling, swelling of the tongue and larynx, shortness of breath, tachycardia, severe hypotension or shock.
Clinical and epidemiological data suggest that ibuprofen may slightly increase the risk of arterial thrombotic events (e.g. myocardial infarction, stroke), especially when used at high doses (2400 mg/day) for long periods (see section 4.4).
Adverse reactions associated with ibuprofen can be minimized by using the lowest effective dose necessary to treat symptoms for the shortest period of time.
Elderly people are at increased risk of developing adverse reactions with serious consequences.
Expiration date
3 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
Capsules No. 10 (10×1), No. 20 (10×2), No. 60 (10×6) in blisters in a box.
Vacation category
Without a prescription.
Producer
Limited Liability Company "Pharmaceutical Company "Zdorovya".
Location of the manufacturer and address of its place of business.
Ukraine, 61013, Kharkiv region, Kharkiv city, Shevchenko street, building 22
(quality control, series release).
Ukraine, 08301, Kyiv region, Boryspil city, Shevchenko st., building 100, letter B-II (building 4)
(all stages of production, series production).
