Ibuprofen-Akrikhin (Suspension) Instructions for Use

Marketing Authorization Holder

Polpharma Pharmaceutical Works, Sa (Poland)

Manufactured By

Pharmaceutical Works “Polpharma” SA Medana Branch In Sieradz (Poland)

Contact Information

AKRIKHIN JSC (Russia)

ATC Code

M01AE01 (Ibuprofen)

Active Substance

Ibuprofen (Rec.INN registered by WHO)

Dosage Form

Ibuprofen-Akrikhin

Oral suspension (orange) 100 mg/5 ml: 100 ml or 200 ml bottle

Dosage Form, Packaging, and Composition

Oral suspension (orange) orange in color with an orange odor; separation into a liquid layer and a sediment is allowed, which after mixing form a homogeneous suspension.

Excipients: sodium carmellose – 0.97 g, macrogol glyceryl hydroxystearate – 1.14 g, sucrose – 34.2 g, glycerol – 5.7 g, magnesium aluminum silicate (veegum) – 0.57 g, propylene glycol – 1.71 g, methylparahydroxybenzoate – 0.15 g, propylparahydroxybenzoate – 0.05 g, sodium phosphate dihydrate – 0.46 g, citric acid monohydrate – 0.91 g, sodium saccharin – 0.25 g, crospovidone – 0.14 g, orange flavor – 0.34 g, sunset yellow dye (E110) – 0.02 g, purified water – up to 100 ml.

100 g – dark glass bottles (1) complete with a measuring spoon – cardboard packs.
100 g – plastic bottles (1) complete with a dosing syringe – cardboard packs.

Clinical-Pharmacological Group

NSAID

Pharmacotherapeutic Group

NSAID

Pharmacological Action

NSAID. It has antipyretic, analgesic, and anti-inflammatory effects.

The antipyretic effect is due to the blocking of COX-1 and COX-2 in the arachidonic acid cascade of the CNS, which leads to a decrease in the synthesis of prostaglandins, a decrease in their concentration in the cerebrospinal fluid, and a decrease in the excitation of the thermoregulation center. The temperature-lowering effect in fever begins 30 minutes after taking the drug, its maximum effect is manifested after 3 hours.

The leading mechanism of the analgesic effect is the reduction in the production of prostaglandins of classes E, F, and I, and biogenic amines, which prevents the development of hyperalgesia at the level of nociceptor sensitivity changes. The analgesic effect is most pronounced in pain of an inflammatory nature.

The anti-inflammatory effect is due to the inhibition of COX activity and a decrease in the synthesis of prostaglandins in the foci of inflammation, which leads to a decrease in the secretion of inflammatory mediators and a decrease in the activity of the exudative and proliferative phases of the inflammatory process.

Like other NSAIDs, Ibuprofen exhibits antiplatelet activity.

Pharmacokinetics

Absorption and Distribution

After oral administration, more than 80% of ibuprofen is absorbed from the gastrointestinal tract. C_max in blood plasma when taken on an empty stomach is 45 minutes, when taken after a meal is 1.5-2.5 hours; in synovial fluid – 2-3 hours, where higher concentrations are created than in blood plasma. After absorption, about 60% of the pharmacologically inactive R-form of ibuprofen is slowly transformed into the active S-form.

Binding to plasma proteins (mainly albumin) is 90%.

Ibuprofen does not accumulate in the body.

Metabolism

Ibuprofen is biotransformed mainly in the liver.

It undergoes presystemic and postsystemic metabolism.

Excretion

Ibuprofen has biphasic elimination kinetics with T_1/2 2-2.5 hours. 60-90% of the drug is excreted by the kidneys as metabolites and products of their conjugation with glucuronic acid, to a lesser extent, with bile, and no more than 1% is excreted unchanged. After a single dose, the drug is completely excreted within 24 hours.

Indications

The drug is intended only for the treatment of children.

Elevated body temperature of various origins in

• Common colds;
• Acute respiratory viral infections, including influenza;
• Sore throat (tonsillitis);
• Childhood infections;
• Post-vaccination reactions.

Pain syndrome of various origins of mild to moderate intensity in

• Toothache, painful teething;
• Ear pain with inflammation of the middle ear;
• Headache, migraine;
• Neuralgia;
• Muscle and joint pain due to injuries of the musculoskeletal system.

It is intended for symptomatic therapy, reducing pain and inflammation during the period of use, and does not affect the progression of the disease.

ICD codes

Dosage Regimen

The drug is taken orally, after meals. Before use, the bottle should be shaken well to obtain a homogeneous suspension.

The dose is set depending on the age and body weight of the child.

For accurate dosing of the suspension, a dispenser (spoon or syringe) is included with the bottle.

A single dose is 5-10 mg/kg of body weight 3-4 times/day.

The maximum daily dose is 20-30 mg/kg of body weight.

The drug can be repeated in a single dose every 6-8 hours. The maximum daily dose should not be exceeded.

For infants from 3 to 6 months (5-7.6 kg)with post-vaccination reactions: 2.5 ml of the drug, if necessary – a repeated dose of 2.5 ml after 6 hours.

The daily dose of the drug for children from 3 to 6 months should not exceed 5 ml.

In children from 3 to 6 months, the drug can be used only after consultation with the attending physician.

Ibuprofen-Akrikhin can be used for no more than 3 days as an antipyretic and no more than 5 days as an analgesic.

If fever persists for more than 3 days, you should consult a doctor.

If the pain syndrome persists for more than 5 days, you should consult a doctor.

Using the syringe dispenser

1. Unscrew the bottle cap (press down and turn counterclockwise).
2. Firmly insert the dispenser into the bottle neck opening.
3. Shake the bottle contents vigorously.
4. To fill the dispenser, turn the bottle upside down, then gently move the dispenser plunger down to draw the contents up to the desired mark on the scale.
5. Return the bottle to its original position and carefully remove the dispenser with a twisting motion.
6. Place the dispenser tip in the child’s mouth, then slowly press the plunger to administer the dispenser contents.
7. After use, close the bottle by screwing on the cap, and rinse the dispenser with drinking water and dry it.

Adverse Reactions

From the digestive system: NSAID-gastropathy (nausea, vomiting, decreased appetite, heartburn, abdominal pain, diarrhea, flatulence, pain and discomfort in the epigastric region); ulceration of the gum mucosa and gastrointestinal mucosa (in some cases complicated by perforation and bleeding); dry oral mucosa, aphthous stomatitis, pancreatitis, constipation, hepatitis.

From the respiratory system: shortness of breath, bronchospasm.

From the nervous system: headache, dizziness, sleep disturbance, anxiety, drowsiness, depression, psychomotor agitation, irritability, confusion, hallucinations; rarely – aseptic meningitis (more often in patients with autoimmune diseases).

From the sensory organs: hearing loss, ringing or noise in the ears, reversible toxic optic neuritis, blurred vision or diplopia, color vision impairment, dry and irritated eyes, conjunctival and eyelid edema (of allergic origin), scotoma, amblyopia.

From the hematopoietic organs: anemia (including hemolytic, aplastic), thrombocytopenia and thrombocytopenic purpura, agranulocytosis, leukopenia.

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.

Allergic reactions: skin itching, skin rash (erythematous or urticaria), angioedema, anaphylactoid reactions, anaphylactic shock, bronchospasm, fever, multiforme exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), eosinophilia, allergic rhinitis.

Other: increased sweating.

If any of the listed side effects occur, it is necessary to stop taking the drug and consult a doctor.

Contraindications

• Hypersensitivity to ibuprofen or other NSAIDs (including acetylsalicylic acid), as well as to the auxiliary components of the drug;
• Complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in history);
• Erosive and ulcerative diseases of the gastrointestinal tract (including peptic ulcer of the stomach and duodenum in the acute phase, ulcerative colitis, peptic ulcer, Crohn’s disease – ulcerative colitis);
• Severe renal failure (creatinine clearance < 30 ml/min), progressive kidney disease;
• Severe hepatic failure, active liver disease;
• Confirmed hyperkalemia;
• Inflammatory bowel disease;
• Sucrase/isomaltase deficiency;
• Fructose intolerance, glucose-galactose malabsorption;
• Blood clotting disorders (including hemophilia, prolonged bleeding time, tendency to bleed, hemorrhagic diathesis);
• Children under 3 months of age.

With caution: liver cirrhosis with portal hypertension; hepatic and/or renal failure; arterial hypertension, chronic heart failure; nephrotic syndrome; hyperbilirubinemia; presence of Helicobacter pylori infection; peptic ulcer of the stomach and duodenum (in history); gastritis; enteritis; colitis; blood diseases of unclear etiology (leukopenia and anemia); long-term use of NSAIDs; severe somatic diseases; simultaneous use of oral glucocorticosteroids (including prednisolone); anticoagulants (including warfarin); antiplatelet agents (including clopidogrel). Ibuprofen-Akrikhin contains sugar in its composition, so it should be used with caution in patients with diabetes mellitus.

Use in Pregnancy and Lactation

Prescription of the drug Ibuprofen-Akrikhin during pregnancy is possible only if the potential benefit to the mother outweighs the possible risk to the fetus.

If it is necessary to prescribe the drug Ibuprofen-Akrikhin during lactation, the issue of stopping breastfeeding should be decided.

Use in Hepatic Impairment

The drug is contraindicated in severe liver dysfunction.

Use in Renal Impairment

The drug is contraindicated in severe renal dysfunction.

Pediatric Use

In children from 3 to 6 months, the drug can be used only after consultation with the attending physician.

Contraindicated in children under 3 months of age.

Special Precautions

In patients with bronchial asthma or other diseases occurring with bronchospasm, Ibuprofen may increase the risk of bronchospasm. The use of the drug in these patients is permissible only with great caution, and in case of breathing difficulties, you should immediately consult a doctor.

During long-term treatment with NSAIDs, monitoring of the peripheral blood picture and the functional state of the liver and kidneys is necessary.

To prevent the development of NSAID-gastropathy, it is recommended to combine with prostaglandin E drugs (misoprostol). If symptoms of NSAID-gastropathy appear, careful monitoring is indicated, including esophagogastroduodenoscopy, blood test with determination of hemoglobin, hematocrit, stool test for occult blood.

If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the study.

During treatment, it is not recommended to take drugs containing ethanol.

To reduce the risk of adverse events from the gastrointestinal tract, Ibuprofen-Akrikhin should be used in the minimum effective dose for the shortest possible course.

1 ml of Ibuprofen-Akrikhin suspension contains about 0.34 g of sucrose, which corresponds to approximately 0.03 XE. Thus, the minimum single dose of the drug, equal to 2.5 ml, contains 0.85 g of sucrose (corresponds to 0.075 XE); the maximum single dose of the drug, equal to 15 ml, contains 5.13 g of sucrose (corresponds to 0.45 XE).

Effect on the ability to drive vehicles and mechanisms

Given the possibility of developing significant side effects, during treatment, caution should be exercised when driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms: abdominal pain, nausea, vomiting, lethargy, headache, tinnitus, depression, drowsiness, metabolic acidosis, coma, hemorrhagic diathesis, decreased blood pressure, convulsions, respiratory arrest, acute renal failure, impaired liver function, tachycardia, bradycardia, atrial fibrillation. Children under 5 years of age are especially prone to apnea, coma, and convulsions.

Serious consequences associated with the toxic effect of the drug usually appear after taking a dose exceeding 400 mg/kg of body weight. In case of overdose, it is necessary to immediately consult a doctor.

Treatment: gastric lavage (only within an hour after taking the drug), activated charcoal, alkaline drinking, symptomatic therapy (correction of acid-base status, blood pressure).

Drug Interactions

Ibuprofen should not be used simultaneously with other NSAIDs. For example, acetylsalicylic acid reduces the anti-inflammatory effect of ibuprofen and enhances the side effect.

If possible, simultaneous use of ibuprofen and diuretics should be avoided, due to the weakening of the diuretic effect and the risk of developing renal failure.

Ibuprofen reduces the hypotensive activity of vasodilators (including ACE inhibitors).

Ibuprofen enhances the effect of oral hypoglycemic agents (especially sulfonylurea derivatives) and insulin.

Inducers of microsomal oxidation (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites, increasing the risk of severe hepatotoxic reactions.

Antacids and cholestyramine reduce the absorption of ibuprofen.

Cefamandole, cefoperazone, cefotetan, valproic acid, plicamycin increase the incidence of hypoprothrombinemia.

Agents with myelotoxic action enhance the manifestations of the hematotoxicity of the drug.

Cyclosporines, 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 cyclosporine and the likelihood of developing its hepatotoxic effects.

Drugs that block tubular secretion reduce the excretion and increase the plasma concentration of ibuprofen.

Enhances the effect of indirect anticoagulants, antiplatelet agents, fibrinolytics (increasing the risk of hemorrhagic complications).

Increases the concentration in the blood of digoxin, methotrexate and lithium preparations.

Caffeine enhances the analgesic effect of ibuprofen.

Storage Conditions

The drug should be stored out of the reach of children, protected from light, at a temperature not exceeding 25°C (77°F).

Shelf Life

The shelf life is 3 years.

An opened bottle should be used within 6 months.

Dispensing Status

The drug is approved for use as an over-the-counter product.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.