Ketorol Express tablets, dispersible in the oral cavity 10 mg, 20 pcs.

Zodak Express allergy remedy tablets No. 28

A country

Czech Republic
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Active substance

Levocetirizine

Compound

Active substance: levocetirizine hydrochloride 5.00 mg.

pharmachologic effect

Pharm acodynamics. Levocetirizine, the (R)-enantiomer of cetirizine, is an inhibitor of peripheral H1 histamine receptors, the affinity of which is 2 times higher than that of cetirizine. After a single dose of levocetirizine, binding of H1-histamine receptors was observed by 90% after 4 hours and by 57% after 24 hours. It has an effect on the histamine-dependent stage of allergic reactions; reduces the migration of eosinophils, reduces vascular permeability, limits the release of inflammatory mediators. Prevents the development and facilitates the course of allergic reactions, has an antiexudative and antipruritic effect; has virtually no anticholinergic and antiserotonin effects. In therapeutic doses it has virtually no sedative effect. Action begins 12 minutes after a single dose in 50% of patients, 1 hour in 95% of patients, and continues for 24 hours. Does not affect the QT interval on the ECG. Pharmacokinetics: Pharmacokinetics are linear, independent of dose and time, and vary slightly among individuals. Absorption: After oral administration, absorption of levocetirizine occurs quickly and in large quantities. The maximum plasma concentration is reached 0.9 hours after taking the drug. Equilibrium concentration is established after 2 days. The maximum plasma concentration after a single dose of 5 mg of levocetirizine is 270 ng/ml, and after a repeated dose of 5 mg - 308 ng/ml. The degree of absorption depends on the dose and is not affected by food intake, but when eating food, the maximum concentration decreases and its achievement slows down. Distribution: Levocetirizine is 90% bound to plasma proteins. The volume of distribution is 0.4 l/kg. There are no data on the distribution of levocetirizine in tissues and its penetration through the blood-brain barrier in humans; Levocetirizine passes into breast milk. Metabolism: In humans, less than 14% of the dose of levocetirizine is metabolized, since the expected differences in the pharmacokinetic profile of levocetirizine due to genetic polymorphism or concomitant use of enzyme inhibitors are insignificant . Metabolic transformations consist of oxidation of the aromatic ring, N- and O-dealkylation and conjugation with taurine. The dealkylation process is mainly carried out by the CYP3A4 isoenzyme, while the oxidation of the aromatic ring occurs through many and/or unidentified CYP isoforms. Levocetirizine, when taken orally at a dose of 5 mg and/or when maximum plasma concentrations are exceeded, does not affect the activity of CYP isoenzymes 1A2, 2C9, 2C19, 2D6, 2E1, 3A4. Due to limited metabolism and the absence of metabolic inhibitory activity, the interaction of levocetirizine at the level of metabolism with other substances is unlikely. Elimination. The half-life in adults is 7.9 ± 1.9 hours. The average observed total clearance is 0.63 ml/min/kg. Levocetirizine is predominantly excreted in the urine, on average, about 85.4% of the dose taken by glomerular filtration and active tubular secretion. Excretion through the intestines (with feces) is only 12.9% of the dose taken. Patients with renal failure. The total clearance of levocetirizine depends on the creatinine clearance (CC). Therefore, patients with moderate and severe renal failure are recommended to increase the intervals between doses of the drug in accordance with the QC. In patients with anuria and end-stage renal disease, the total clearance of levocetirizine is reduced by approximately 80% compared to healthy individuals. The amount of levocetirizine excreted during a standard 4-hour hemodialysis procedure is less than 10%.

Indications for use

Treatment of symptoms of year-round (persistent) and seasonal (intermittent) allergic rhinitis and allergic conjunctivitis, such as itching, sneezing, nasal congestion, rhinorrhea. lacrimation, conjunctival hyperemia. Hay fever (hay fever). Urticaria, including chronic idiopathic urticaria. Quincke's edema (as an auxiliary therapy). Other allergic dermatoses, accompanied by itching and rashes.

Mode of application

The tablet should be taken orally, without chewing and with liquid, regardless of meals. It is recommended to take the daily dose in one dose. Adults, teenagers and children over 6 years old. The recommended daily dose is 5 mg (1 tablet). Elderly patients. In elderly patients with moderate and severe renal failure, dose adjustment is recommended. Patients with impaired renal function. The interval between doses of the drug is determined individually taking into account renal function. In children with impaired function kidney dose is adjusted individually taking into account creatinine clearance and body weight. There are no separate data on use in children with impaired renal function. Patients with impaired liver function. In case of isolated impaired liver function, no dose adjustment is required. In patients with hepatic-renal insufficiency, dose adjustment is recommended. Duration of treatment. Treatment of allergic rhinitis is carried out in accordance with the course of the disease; The drug can be stopped when symptoms disappear and resumed if symptoms recur. In the case of chronic allergic rhinitis, long-term treatment may be prescribed during the period of exposure to allergens. Currently, clinical experience with the use of levocetirizine in the form of 5 mg film-coated tablets is limited to 6 months.

Interaction

There have been no drug interaction studies with levocetirizine, including studies with inducers of the CYP3A4 isoenzyme. The extent of absorption of levocetirizine was not reduced by food, although the rate of absorption was reduced. In sensitive patients, concomitant use of levocetirizine and alcohol or other substances that have a depressant effect on the central nervous system (CNS) ), may enhance the effect on the central nervous system.

Side effect

Immune system disorders. Very rare: hypersensitivity reactions, including anaphylactic reactions. Nervous system disorders. Often: headache; uncommon: drowsiness; very rare: aggression, agitation, hallucinations, depression, convulsions. Visual disorders. Very rare: visual disturbances. Cardiac disorders. Very rare: palpitations, tachycardia. Disorders of the respiratory system, chest and mediastinal organs. Very rare: shortness of breath. Gastrointestinal disorders. Often: dryness of the oral mucosa; uncommon: abdominal pain; very rare: nausea, diarrhea. Liver and biliary tract disorders. Very rare: hepatitis. Skin and subcutaneous tissue disorders. Very rare: angioedema, itching, rash, including drug rash, urticaria. Musculoskeletal disorders and connective tissue. Very rare: myalgia. General disorders. Often: fatigue; uncommon: asthenia. Violations of laboratory and instrumental data. Very rare: abnormal liver function tests, weight gain.

Contraindications

Hypersensitivity to levocetirizine and other piperazine derivatives or to any of the auxiliary components of the drug. Terminal renal failure with CC less than 10 ml/min. Pregnancy. Children under 6 years of age (for this dosage form). Congenital galactose intolerance, lactase deficiency or glucose malabsorption - galactose (due to the lactose content in the preparation).

Overdose

Symptoms: Symptoms of overdose may include drowsiness in adults and agitation and restlessness alternating with drowsiness in children. Treatment: There are no specific antidotes for levocetirizine. In case of overdose, symptomatic or supportive treatment is recommended. If little time has passed after taking the drug, gastric lavage should be performed. Levocetirizine is practically not excreted during hemodialysis.

special instructions

With caution. Caution must be exercised when taken simultaneously with alcohol. Chronic renal failure with CC more than 10 ml/min, but less than 50 ml/min (dosage adjustment required). Older age (possible decrease in glomerular filtration). Use during pregnancy and during pregnancy period of breastfeeding. The use of the drug during pregnancy is contraindicated. Levocetirizine is excreted in breast milk, therefore, if it is necessary to use the drug during lactation, it is recommended to stop breastfeeding. During treatment with the drug, it is not recommended to take ethanol. Impact on the ability to drive vehicles or engage in other potentially hazardous activities Levocetirizine, when taken in recommended doses, does not have a negative effect on attention and speed of psychomotor reactions and the ability to drive vehicles. However, during the period of taking the drug, it is advisable to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Ketorol Express tablets, dispersible in the oral cavity 10 mg, 20 pcs.

Manufacturer

Dr. Reddy's, India

Compound

Each tablet, dispersible in the oral cavity, contains: Active ingredient: ketorolac tromethamine (ketorolac trometamol) 10,000 mg; Excipients: microcrystalline cellulose, silicon dioxide, butylated hydroxyanisole, mannitol, crospovidone (type A), sucralose, mint flavor, quinoline yellow dye (E104), magnesium stearate.

pharmachologic effect

NSAIDs have a pronounced analgesic effect, have anti-inflammatory and moderate antipyretic effects. The mechanism of action is associated with non-selective inhibition of the activity of COX - COX-1 and COX-2, which catalyzes the formation of prostaglandins from arachidonic acid, which play an important role in the pathogenesis of inflammation, pain and fever. Ketorolac is a racemic mixture of [-]S- and [+]R-enantiomers, and the analgesic effect is due to the [-]S-form. In terms of the strength of the analgesic effect, ketorolac is comparable to morphine, significantly superior to other NSAIDs. The drug does not affect opioid receptors, does not depress respiration, does not cause drug dependence, and does not have a sedative or anxiolytic effect. After oral administration, the onset of analgesic action is observed after 1 hour, the maximum effect is achieved after 1-2 hours. Pharmacokinetics
Absorption After oral administration, ketorolac is well absorbed from the gastrointestinal tract, Cmax in blood plasma (0.7-1.1 mcg/ml) is achieved 40 minutes after administration on an empty stomach at a dose of 10 mg.
Food rich in fat reduces the Cmax of ketorolac in the blood and delays its achievement by 1 hour. Bioavailability is 80-100%. Distribution Plasma protein binding is 99%; with hypoalbuminemia, the amount of free substance in the blood increases. The time to reach Css (0.39-0.79 mcg/ml) when taking 10 mg ketorolac orally 4 times a day (a dose higher than subtherapeutic) is 24 hours. Vd – 0.15-0.33 l/kg. Penetrates into breast milk: after the mother takes 10 mg of ketorolac, Cmax in breast milk is reached after 2 hours and is 7.3 ng/ml after the first dose and 7.9 ng/ml after the second dose of the drug. Metabolism More than 50% of the administered dose is metabolized in the liver with the formation of pharmacologically inactive metabolites. The main metabolites are glucuronides, which are excreted by the kidneys, and p-hydroxyketorolac. Excretion Excreted by the kidneys (91%) and through the intestines (6%). T1/2 in patients with normal renal function is 2.4-9 hours after oral administration of a dose of 10 mg. When taken orally at a dose of 10 mg, the total clearance is 0.025 l /h/kg. Pharmacokinetics in special clinical situations
In patients with renal failure, the Vd of ketorolac may increase by 2 times, and the Vd of its R-enantiomer by 20%. T1/2 increases in elderly patients and decreases in young ones. Liver dysfunction does not affect T1/2. In patients with impaired renal function, with a plasma creatinine concentration of 19-50 mg/l (168-442 µmol/l), T1/2 is 10.3-10.8 hours, with more severe renal failure - more than 13.6 hours. When taken orally in At a dose of 10 mg, the total clearance in patients with renal failure (with a plasma creatinine concentration of 19-50 mg/l) is 0.016 l/h/kg. Not excreted during hemodialysis.

Indications

Pain syndrome of severe and moderate severity:

• injuries;
• toothache;
• pain in the postoperative period;
• oncological diseases;
• myalgia;
• arthralgia;
• neuralgia;
• radiculitis;
• dislocations, sprains;
• rheumatic diseases.

Intended for symptomatic therapy, reducing the intensity of pain and inflammation at the time of use, does not affect the progression of the disease.

Contraindications

• Hypersensitivity (including to other NSAIDs);
• complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including a history);
• erosive and ulcerative lesions of the gastrointestinal tract;
• active gastrointestinal bleeding;
• inflammatory bowel diseases (including ulcerative colitis, Crohn's disease);
• diseases of the bone marrow and blood (leukopenia, including history; thrombocytopenia; hypocoagulation, including hemophilia),
• myelosuppression;
• bleeding or a high risk of developing it;
• severe renal failure (creatinine clearance less than 30 ml/min);
• confirmed hyperkalemia;
• severe liver failure or active liver disease;
• condition after coronary artery bypass surgery;
• preventive pain relief before and during major surgical interventions due to the high risk of bleeding;
• active cerebrovascular diseases (including intracranial hemorrhage or suspicion of it);
• pregnancy;
• period of childbirth;
• breastfeeding period;
• children under 16 years of age (safety and effectiveness of use have not been established);
• simultaneous use with probenecid;
• simultaneous use with pentoxifylline;
• simultaneous use of acetylsalicylic acid with other NSAIDs (including selective COX-2 inhibitors);
• simultaneous use with lithium salts;
• simultaneous use with anticoagulants (including warfarin and heparin).

Carefully

Bronchial asthma; the presence of factors that increase gastrointestinal toxicity: alcoholism, smoking and cholecystitis; postoperative period; chronic heart failure; edema syndrome; arterial hypertension; moderate renal failure (creatinine clearance 30-60 ml/min); cholestasis; active hepatitis; sepsis; systemic lupus erythematosus; IHD; cerebrovascular diseases; dyslipidemia/hyperlipidemia; diabetes; peripheral artery disease; history of ulcerative lesions of the gastrointestinal tract; presence of Helicobacter pylori infection; long-term use of NSAIDs; severe somatic diseases; thyroid diseases; tuberculosis; simultaneous use of oral corticosteroids (including prednisolone), antiplatelet agents (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline); old age (over 65 years).

Side effects

Determination of the frequency of side effects: often (1-10%), uncommon (0.1-1%), rare (0.01-0.1%), very rare (<0.01%) and frequency unknown, including isolated reports. From the digestive system: often (especially in elderly patients over 65 years of age with a history of erosive and ulcerative lesions of the gastrointestinal tract) - gastralgia, diarrhea; infrequently – stomatitis, flatulence, constipation, vomiting, feeling of fullness of the stomach; rarely - nausea, erosive and ulcerative lesions of the gastrointestinal tract (including with perforation and/or bleeding - abdominal pain, spasm or burning in the epigastric region, melena, vomiting like “coffee grounds”, nausea, heartburn), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis. From the urinary system: rarely - acute renal failure, lower back pain, hematuria, azotemia, hemolytic-uremic syndrome (hemolytic anemia, renal failure, thrombocytopenia, purpura), frequent urination, oliguria, polyuria, interstitial nephritis, edema of renal origin; frequency unknown – urinary retention. From the senses: rarely - hearing loss, ringing in the ears, visual impairment (including blurred visual perception); frequency unknown – taste disturbance. From the respiratory system: rarely - bronchospasm or dyspnea, rhinitis, laryngeal edema (shortness of breath, difficulty breathing). From the side of the central nervous system: often – headache, dizziness, drowsiness; rarely - aseptic meningitis (fever, severe headache, convulsions, stiffness of the neck and/or back muscles), hyperactivity (mood changes, anxiety), hallucinations, depression, psychosis. From the cardiovascular system: infrequently - increased blood pressure; rarely – pulmonary edema, fainting. From the hematopoietic organs: rarely - anemia, eosinophilia, leukopenia. From the hemostasis system: rarely - bleeding from a postoperative wound, nosebleeds, rectal bleeding. From the skin: infrequently - skin rash (including maculopapular rash), purpura; rarely - exfoliative dermatitis (fever with or without chills, redness, thickening or flaking of the skin, swelling and/or tenderness of the tonsils), urticaria, Stevens-Johnson syndrome, Lyell's syndrome. Allergic reactions: rarely - anaphylaxis or anaphylactoid reactions (change in facial skin color, skin rash, urticaria, itching, tachypnea or dyspnea, swelling of the eyelids, swelling of the tongue, periorbital edema, shortness of breath, difficulty breathing, heaviness in the chest, wheezing). Other: often - swelling (face, legs, ankles, fingers, feet, weight gain); uncommon – increased sweating; rarely – fever; frequency unknown - hyperkalemia, hyponatremia.

Interaction

The simultaneous use of ketorolac with acetylsalicylic acid or other NSAIDs, calcium preparations, glucocorticosteroids, ethanol, corticotropin can lead to a significant increase in the risk of adverse reactions, including the formation of gastrointestinal ulcers and the development of gastrointestinal bleeding. When ketorolac is used simultaneously with other NSAIDs (including COX-2 inhibitors), fluid retention, cardiac decompensation, and increased blood pressure may occur. Concomitant use of ketorolac with indirect anticoagulants, thrombolytics, antiplatelet agents, cefoperazone, cefotetan and pentoxifylline increases the risk of bleeding. Probenecid reduces the plasma clearance and volume of distribution of ketorolac, increases its concentration in the blood plasma and increases its T1/2. The combined use of ketorolac with valproate causes a disorder of platelet aggregation. When using ketorolac with other nephrotoxic drugs (including gold preparations) the risk of developing nephrotoxicity increases. Combined use with paracetamol increases the nephrotoxicity of ketorolac. Drugs that block tubular secretion reduce the clearance of ketorolac and increase its concentration in the blood plasma. The combined use of ketorolac with methotrexate increases the hepato- and nephrotoxicity of methotrexate. The combined use of ketorolac and methotrexate is possible only when using low doses of the latter. The clearance of methotrexate may be reduced (it is necessary to monitor the concentration of methotrexate in the blood plasma). With the use of ketorolac, the clearance of lithium may decrease, its concentration in the blood plasma may increase, and the toxic effect of lithium may increase. Simultaneous use with lithium salts is contraindicated. Ketorolac reduces the effect of antihypertensive and diuretic drugs (the synthesis of prostaglandins in the kidneys is reduced). Ketorolac enhances the effect of narcotic analgesics. When combined with opioid analgesics, the doses of the latter can be significantly reduced. Ketorolac enhances the hypoglycemic effect of insulin and oral hypoglycemic drugs, and therefore it is necessary to recalculate the dose of these drugs. Ketorolac increases the plasma concentrations of verapamil and nifedipine. Concomitant use of NSAIDs and mifepristone may reduce the effectiveness of mifepristone. NSAIDs are not recommended for use within 8-12 days after using mifepristone. The simultaneous use of NSAIDs and cyclosporine increases the risk of nephrotoxicity. The simultaneous use of NSAIDs and quinolone antibiotics increases the risk of seizures. The simultaneous use of NSAIDs and tacrolimus increases the risk of developing nephrotoxicity. The simultaneous use of NSAIDs and zidovudine increases the risk of developing hematological toxicity. When used simultaneously with digoxin, ketorolac does not interfere with the binding of digoxin to plasma proteins. Therapeutic concentrations of digoxin do not affect the binding of ketorolac to plasma proteins. Antacids do not affect the absorption of ketorolac. Myelotoxic drugs increase the manifestations of hematotoxicity of ketorolac.

How to take, course of administration and dosage

Place the tablet on your tongue, where it will immediately begin to dissolve. Keep it in your mouth for a few seconds until completely dissolved; if desired, you can wash it down with liquid. Taking tablets dispersible in the oral cavity does not necessarily require drinking water, does not affect the increase in saliva production, and allows the drug to be taken by patients with deviations in the act of swallowing and behavioral and neurological disorders. Ketorol® Express is used orally once or repeatedly depending on the severity of the pain syndrome. Single dose – 10 mg, when repeated, it is recommended to take 10 mg up to 4 times a day, depending on the severity of pain; the maximum daily dose should not exceed 40 mg. When taken orally, the duration of the course should not exceed 5 days. To reduce the risk of adverse events, the minimum effective dose of ketorolac should be used for the shortest possible short course. When switching from parenteral administration of the drug to oral administration, the total daily dose of both dosage forms on the day of transfer should not exceed 90 mg for patients from 16 to 65 years of age and 60 mg for patients over 65 years of age or with impaired renal function. In this case, the dose of the drug in tablets on the day of transition should not exceed 30 mg.

Overdose

Symptoms: abdominal pain, nausea, vomiting, erosive and ulcerative lesions of the gastrointestinal tract, impaired renal function, metabolic acidosis. Treatment: gastric lavage, administration of adsorbents (activated carbon) and symptomatic therapy (maintaining vital body functions). Hemodialysis is ineffective.

Special instructions

The choice of dosage form of the drug depends on the severity of the pain syndrome and the patient’s condition. The drug Ketorol® is available in the following dosage forms: gel for external use; film-coated tablets; tablets, dispersible in the oral cavity; solution for intravenous and intramuscular administration. Before using the drug, it is necessary to find out whether there is a previous allergy to the drug or other NSAIDs. Due to the risk of allergic reactions, the first dose is taken under close medical supervision. Ketorolac inhibits platelet aggregation and increases blood clotting time. The effect on platelet aggregation ceases 24-48 hours after taking the drug. Patients with bleeding disorders are prescribed the drug only with constant monitoring of the platelet count, which is especially important in the postoperative period when careful control of hemostasis is required. Hypovolemia increases the risk of developing nephrotoxic adverse reactions. If necessary, can be used in combination with narcotic analgesics. Do not use with paracetamol for more than 2 days. The risk of adverse reactions increases with lengthening the course of treatment and increasing the oral dose of ketorolac to more than 40 mg/day. Concomitant use of ketorolac with probenecid, pentoxifylline, acetylsalicylic acid and other NSAIDs (including COX-2 inhibitors), lithium salts, anticoagulants (including warfarin and heparin) is contraindicated. The use of ketorolac for prophylactic pain relief before and during major surgical interventions is contraindicated due to the high risk of bleeding. Ketorolac is not recommended for use as a premedication or maintenance anesthesia. Cases of fluid retention, increased blood pressure and edema have been reported with the use of ketorolac. Caution must be exercised when prescribing to patients with heart failure and arterial hypertension. Concomitant use of ketorolac with other NSAIDs can lead to disorders such as decompensated heart failure and increased blood pressure. According to clinical studies, the use of certain NSAIDs in high doses may lead to an increased risk of arterial thrombotic complications (eg, myocardial infarction, stroke). Although such complications have not been reported with ketorolac, existing data are insufficient to exclude the risk of such complications. To reduce the risk of developing NSAID-induced gastropathy, the use of antacid drugs, misoprostol, as well as drugs that reduce gastric secretion (histamine H2 receptor blockers, proton pump inhibitors) is recommended. To reduce the risk of adverse events, the minimum effective dose of ketorolac should be used for the shortest possible short course. Effect on the ability to drive vehicles and machinery
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Storage conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C.

Best before date

2 years.

Active substance

Ketorolac

Conditions for dispensing from pharmacies

On prescription

Dosage form

pills

Barcode and weight

Barcode: 8901148246591, 8901148308722 Weight: 0.013 kg

Pharmacodynamics

Levocetirizine - the active ingredient of the drug Allerway Express - (R)-enantiomer of cetirizine, a powerful and selective histamine antagonist that blocks H1 histamine receptors.
Levocetirizine has an effect on the histamine-dependent stage of allergic reactions, and also reduces the migration of eosinophils, reduces vascular permeability, and limits the release of inflammatory mediators.

Levocetirizine prevents the development and facilitates the course of allergic reactions, has antiexudative and antipruritic effects, and has virtually no anticholinergic and antiserotonin effects. In therapeutic doses it does not have a sedative effect.

With a single dose of levocetirizine, receptor binding is 90% after 4 hours and 57% after 24 hours.

The use of levocetirizine at a dose of 5 mg significantly reduces the formation of urticarial elements (blisters) in the first 12 hours, this effect lasts up to 24 hours, compared with placebo and desloratadine.

Pharmacokinetics

The pharmacokinetic parameters of levocetirizine change linearly.

Suction

After oral administration, the drug is quickly and completely absorbed from the gastrointestinal tract. Eating does not affect the completeness of absorption, although it reduces its speed. The maximum concentration (Cmax) in blood plasma is reached after 0.9 hours and is 270 ng/ml, the equilibrium concentration is achieved after 2 days.

After taking 5 mg Allerway Express tablets by healthy volunteers on an empty stomach, levocetirizine was detected in the blood after 24 hours at a concentration exceeding 10% of Cmax.

Distribution

Levocetirizine is 90% bound to plasma proteins. The volume of distribution (Vd) is 0.4 l/kg. Bioavailability reaches 100%.

Metabolism

In small quantities (less than 14%), levocetirizine is metabolized in the body by N- and O-dealkylation (unlike other H1-histamine receptor antagonists, which are metabolized in the liver using the cytochrome system) to form a pharmacologically inactive metabolite. Due to negligible metabolism and lack of metabolic potential, interaction of levocetirizine with other drugs is unlikely.

Removal

The half-life (T1/2) in adults is 7.9±1.9 hours. In young children, T1/2 is shorter. In adults, the total clearance is 0.63 ml/min/kg.

About 85.4% of the administered dose of the drug is excreted unchanged by the kidneys through glomerular filtration and tubular secretion; about 12.9% - through the intestines.

Selected patient groups

Patients with kidney failure

In patients with renal failure (creatinine clearance (CC)

Less than 10% of levocetirizine is removed during a standard 4-hour hemodialysis procedure.

Patients with liver failure

The pharmacokinetics of levocetirizine in patients with hepatic impairment have not been studied. In patients with chronic liver diseases (hepatocellular, cholestatic and biliary cirrhosis) receiving the racemic compound cetirizine at a dose of 10 mg or 20 mg once, there was an increase in T1/2 by 50% and a decrease in drug clearance by 40%, compared with healthy people.

Children

Data from a study of the pharmacokinetics of the drug in 14 children aged 6 to 11 years with a body weight of 20 to 40 kg with a single oral dose of 5 mg of levocetirizine showed that Cmax values ​​​​and the area under the pharmacokinetic concentration-time curve (AUC) were approximately twice as high as those in healthy adults when cross-checked. The average Cmax was 450 ng/ml, the maximum concentration was reached on average after 1.2 hours, the total clearance taking into account body weight was 30% higher, and T1/2 was 24% shorter in children than the corresponding values ​​in adults. Specific pharmacokinetic studies have not been conducted in children under 6 years of age. A retrospective pharmacokinetic analysis was conducted in 323 patients (181 children aged 1 to 5 years, 18 children aged 6 to 11 years, and 124 adults aged 18 to 55 years) who received one or more doses of levocetirizine 1.25 mg. up to 30 mg. Data obtained during the analysis showed that taking the drug at a dose of 1.25 mg in children aged 6 months to 5 years leads to plasma concentrations similar to those in adults when taking 5 mg of the drug once a day.

Elderly patients

Pharmacokinetic data in elderly patients is limited. When repeated dosing of levocetirizine 30 mg once daily for 6 days in 9 elderly patients (ages 65 to 74 years) total clearance was approximately 33% lower than that in younger adults. The distribution of cetirizine racemate has been shown to be more dependent on renal function than on age. This statement may also apply to levocetirizine, since both drugs - levocetirizine and cetirizine - are eliminated primarily by the kidneys.

Therefore, in elderly patients, the dose of levocetirizine should be adjusted depending on renal function.