Suprastinex pills 5 mg 14 pcs
Condition: New product
1000 Items
Rating:
Be the first to write a review!
More info
Active ingredients
Levocetirizine
Release form
Pills
Composition
Levocetirizine dihydrochloride 5 mg, which corresponds to a content of 4.21 mg of levocetirizine. Supplemental agents: microcrystalline silicon cellulose (Prosolv; HD90) - 40.4 mg (microcrystalline cellulose (98%), anhydrous colloidal silicon dioxide (2%), lactose-free anhydrous silicon dioxide (2%), lactose monohydrate (98%), silicon dioxide, colloidal anhydrous (2%), lactose-free anhydrous colloidal silicon dioxide (2%), lactose monohydrate, 98%; Low substituted hyprolosis (L-HPC11) - 10 mg, magnesium stearate - 1.7 mg. The composition of the shell: opadry II 33G28523 white - 5 mg (hypromellose 2910 (40%), titanium dioxide (25%), lactose monohydrate (21%) - 1.05 mg, macrogol 3350 (8%), triacetin (6%)).
Pharmacological effect
Antiallergic means. Levocetirizine - R-enantiomer of cetirizine, which belongs to the group of competitive histamine antagonists, blocks histamine H1 receptors. It has an effect on the histamine-dependent stage of allergic reactions, reduces eosinophil migration, reduces vascular permeability, limits the release of inflammatory mediators. It prevents the development and facilitates the course of allergic reactions, has anti-exudative, antipruritic action. Practically does not have anticholinergic and anti-serotoninergic effects. In therapeutic doses, it has almost no sedative effect. The effect of the drug begins 12 minutes after taking a single dose in 50% of patients, after 1 h in 95% and lasts for 24 hours.
Pharmacokinetics
Absorption The pharmacokinetic parameters of levocetirizine change linearly and are practically the same as those of cytirizine. After ingestion, it is rapidly and completely absorbed from the gastrointestinal tract. Eating does not affect the completeness of absorption, but reduces its speed. In adults, after a single dose of the drug in a therapeutic dose (5 mg), plasma Cmax is reached in 0.9 hours and amounts to 207 ng / ml (for pills) and 270 ng / ml (for drops), after repeated administration at 5 mg - 308 ng / ml Bioavailability reaches 100%. Distribution Levocetirizine is 90% bound to plasma proteins. Vd is 0.4 l / kg. Css is reached after 2 days. Metabolism Less than 14% of the drug is metabolized in the liver by N- and O-dealkylation (unlike other histamine H1 receptor antagonists, which are metabolized in the liver using the CYP system).Because of the insignificant metabolism and metabolic potential, the interaction of levocetirizine with other drugs seems unlikely. Intake of adults T1 / 2 is 7.9 h ± 1.9 h (for drops), 7-10 h (for pills), the total clearance is 0.63 ml / min / kg About 85.4% of the accepted dose of the drug is excreted by the kidneys unchanged by glomerular filtration and tubular secretion; about 12.9% through the intestines. Pharmacokinetics in special groups of patients. In renal failure (CC less than 40 ml / min), the clearance decreases, and T1 / 2 lengthens (for example, in patients on hemodialysis, the total clearance decreases by 80%), which requires appropriate change in dosing regimen. Less than 10% of levocetirizine is removed during a standard 4-hour hemodialysis procedure. In young children, T1 / 2 is shortened.
Indications
Symptomatic treatment: - year-round (persistent) and seasonal (intermittent) allergic rhinitis and conjunctivitis (itching, sneezing, nasal congestion, rhinorrhea, tearing, conjunctival hyperemia); - hay fever (pollinosis); - urticaria, including chronic idiopathic urticaria (for pills); - Quincke edema (for pills); - allergic dermatosis, accompanied by itching and rashes.
Contraindications
- terminal stage of renal failure (QC less than 10 ml / min); - children's age up to 6 years (for pills); - children's age up to 2 years (for drops for oral administration due to the lack of clinical data); - pregnancy; - lactation period; - lactose intolerance, hereditary lactase deficiency or glucose-galactose malabsorption syndrome (for pills); - hypersensitivity to the active substance (including piperazine derivative) or any auxiliary component of the drug. failure (correction of the dosing regimen is necessary), elderly patients (reduction of glomerular filtration is possible), patients with spinal cord injury, prostate gland hyperplasia, and also with other predisposing factors for urinary retention (levocetirizine may increase the risk of urine retention), while drinking with alcohol.
Precautionary measures
Feeding. Application for violations of the liver. When prescribing a drug to patients with isolated liver dysfunction, no dose changes are required. Patients with a combined liver and kidney dysfunction are recommended to adjust the dose. Use for renal dysfunction creatinine clearance (CK). Patients with a combined impaired liver and kidney function are recommended dose adjustment .. Use in children Contraindications: etsky age of 6 years (for pills); children up to 2 years old (for drops for oral administration due to the lack of clinical data). Use in elderly patientsWith caution should be prescribed to elderly patients (may decrease glomerular filtration).
Use during pregnancy and lactation
Preclinical studies did not reveal any direct or indirect adverse effects of levocetirizine on the developing fetus, as well as on the development in the postnatal period; during pregnancy and childbirth also did not change. Adequate and strictly controlled clinical studies on the safety of the drug during pregnancy were not conducted. Use of the drug during pregnancy is contraindicated. Levocetirizine is excreted in breast milk, so if you need to use the drug during lactation, it is recommended to stop breastfeeding.
Dosage and administration
The drug should be taken orally during meals or on an empty stomach. Tablets are taken without chewing, with a small amount of water. To take the drug in the form of drops, use a teaspoon. If necessary, the dose of the drug can be diluted in a small amount of water immediately before use. The recommended dose for adults and children over 6 years old, elderly patients (provided normal kidney function) is 5 mg (1 tab. Or 1 ml of drops or 20 drops from the dropper) / days The maximum daily dose is 5 mg. For children aged 2 to 6 years, the drug is prescribed in the form of drops for oral administration of 1.25 mg (5 drops) 2 times / day; daily dose - 2.5 mg (10 drops). The duration of treatment depends on the disease. When treating year-round (persistent) allergic rhinitis (symptoms more than 4 days a week and their totalduration more than 4 weeks) treatment may continue for the entire period of exposure to allergens. When treating seasonal (intermittent) allergic rhinitis, symptoms less than 4 days per week or their total duration is less than 4 weeks) the duration of treatment depends on the nature of the disease; treatment can be stopped when symptoms disappear and resumed when symptoms appear. The course of treatment of pollinosis is on average 1-6 weeks. In chronic diseases (including chronic idiopathic urticaria), the course of treatment may be longer if agreed with the doctor. There is a clinical experience of continuous use of the drug in adult patients with a duration of up to 6 months. Since levocetirizine is excreted by the kidneys, when the drug is prescribed to patients with renal insufficiency and patients The dose should be adjusted depending on the amount of creatinine clearance (CC). CK for men can be calculated based on the concentration of serum creatinine using the following formula: CC (ml / min) = [140 - age (years)] × body weight ( kg) / 72 × QC of serum (mg / dL) QC for women can be calculated by multiplying the value obtained by a factor of 0.85. For patients with combined renal and hepatic insufficiency, dosing is carried out according to the following table. Kidney failure QC (ml / min) Dosing regimenNorma> 80 5 mg / day Light 50-79 5 mg / s SET 30-49 5 mg / day × 1 time in 2 days Severe <30 5 mg / day × 1 time in 3 daysTerminal stage - patients on dialysis <10 The drug is contraindicated In patients with impaired liver function, dosing regimen adjustment is not required.
Side effects
During clinical trials, the following adverse events were often observed (≥1 / 100, <1/10) in males and females aged 12 years to 71 years: headache, drowsiness, dry mouth, fatigue; infrequently (≥1 / 1000, <1/100) - asthenia and abdominal pain. In children aged 6 to 12, headache and drowsiness often occurred (≥1 / 100, <1/10). During the period of post-registration use of the drug, the following side effects were observed, the frequency of which is unknown due to insufficient data. On the part of the immune system : hypersensitivity reactions,including anaphylaxis. On the mental side: anxiety, aggression, agitation, insomnia, hallucinations, depression, suicidal thoughts. On the nervous system: convulsions, thrombosis of the dura mater sinuses, paresthesia, dizziness, syncope, tremor, dysgeusia. On the side of hearing: vertigo On the part of the organ of vision: visual impairment, blurred vision, inflammatory manifestations. On the part of the cardiovascular system: palpitations, tachycardia, jugular vein thrombosis. On the part of the respiratory system: shortness of breath, increased with rhinitis. From the digestive system: increased appetite, nausea, vomiting. From the hepatobiliary system: hepatitis, changes in liver function tests. From the urinary system: dysuria, urinary retention. From the skin and soft tissues: rash, pruritus, hypotriasis, cracks. Allergic reactions: angioedema, persistent erythema, urticaria, photosensitivity. From the musculoskeletal system: muscle pain. Others: peripheral edema, weight gain, cross-reactivity. The side effects indicated in the instructions are aggravated, or other side effects not mentioned in the instructions are noted, the patient should be informed about this by the doctor.
Overdose
Symptoms: in adults - drowsiness, in children - agitation, anxiety, which are replaced by drowsiness. Treatment: gastric lavage or taking activated carbon, if not enough time has passed after taking the drug. Symptomatic and maintenance therapy is recommended. There is no specific antidote. Hemodialysis is ineffective.
Interaction with other drugs
The study of the interaction of levocetirizine with other drugs was not carried out. When studying the drug interaction of the racemate cetirizine with phenazone, pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam, there was no clinically significant undesirable interaction. With simultaneous use with theophylline (400 mg / day), the total clearance of cetirizine is reduced by 16% (the kinetics of theophylline does not change). In the study, while taking ritanovir (600 mg 2 times / day) and cetirizine (10 mg / day), it was shownthat cetirizine exposure increased by 40%, ritanovir exposure varied (-10%). In some cases, simultaneous use of levocetirizine with ethanol or drugs that have a suppressive effect on the central nervous system may increase their effect on the central nervous system, although it is not proven that cetirizine racemate potentiates the effect of ethanol. The degree of absorption of levocetirizine does not decrease with simultaneous ingestion of food, but the rate of absorption decreases.
special instructions
The drug should be used with caution in patients with spinal cord injury, prostatic hyperplasia, as well as in the presence of other predisposing factors for urinary retention, since levocetirizine may increase the risk of urinary retention. Suprastinex pills; contain lactose, so you should not assign this dosage form to patients with lactose intolerance, hereditary lactase deficiency or glucose-galactose malabsorption syndrome. Drops Suprastinex; can cause allergic reactions (sometimes late), because contain methyl parahydroxybenzoate and propyl parahydroxybenzoate. The drug Suprastinex; in drops is contraindicated in children under 2 years of age due to lack of clinical data. The drug should be prescribed with caution in chronic renal failure, the elderly, while the use of ethanol. Effect on the ability to drive vehicles and control mechanismsLevocetirizin can lead to increased drowsiness, and, therefore, can affect the ability to drive a car or work with equipment. During the period of treatment, it is necessary to refrain from engaging in potentially hazardous activities that require high concentration of attention and quickness of psychomotor reactions.