Levocetirizine
Levocetirizine: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Levocetirizine
ATX code: R06AE09
Active ingredient: levocetirizine (levocetirizine)
Producer: ALSI Pharma CJSC (Russia), Hetero Labs Limited (India)
Description and photo updated: 22.11.2018
Levocetirizine is an antiallergic drug, blocker of H 1 -histamine receptors.
Release form and composition
Levocetirizine is available in the form of film-coated tablets: round, biconvex, white, the core is almost white or white (10 pcs. In blisters, in a cardboard box 1, 2 or 3 packs).
1 tablet contains:
- active substance: levocetirizine dihydrochloride - 5 mg;
- auxiliary components: pregelatinized starch, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, colloidal silicon dioxide;
- shell composition: opadry II white - hypromellose, lactose monohydrate, macrogol 3000, titanium dioxide.
Pharmacological properties
Pharmacodynamics
Levocetirizine is an anti-allergic drug that has an antipruritic, anti-exudative effect. Its active ingredient is the R-enantiomer of cetirizine, a competitive histamine antagonist. By blocking H 1 - histamine receptors and influencing the histamine-dependent stage of allergic reactions, the action of levocetirizine reduces vascular permeability, eosinophil migration, and limits the release of inflammatory mediators. Therapeutic doses of the drug almost do not cause anticholinergic, antiserotonin, sedative effect. Taking Levocetirizine allows you to prevent the development of allergic reactions and ease their course.
Pharmacokinetics
The pharmacokinetic parameters of levocetirizine are practically similar to the pharmacokinetics of cetirizine, they are characterized by a linear change depending on the dose.
After oral administration, levocetirizine is rapidly and completely absorbed. Simultaneous food intake reduces the rate of absorption, but does not affect its completeness. Cmax (maximum concentration) in blood plasma is 270 ng / ml after 0.9 hours. After 48 hours, the concentration of the drug in the blood plasma reaches a constant level.
Bioavailability of levocetirizine is 100%. Plasma proteins bind 90% of the dose taken. Vd (volume of distribution) - 0.4 l / kg.
Levocetirizine passes into breast milk.
Less than 14% of the drug is metabolized in the liver by N- and O-dealkylation, forming a pharmacologically inactive metabolite. Since the cytochrome system is minimally involved in the metabolism of levocetirizine, it is assumed that its interaction with other drugs is unlikely.
T 1/2 (half-life) in adults is approximately 7.9 hours, in young children this indicator is reduced. The total clearance in adults is 0.63 ml / min / kg.
About 85.4% is excreted through the kidneys, about 12.9% of the dose taken through the intestines.
In renal failure with creatinine clearance (CC) less than 40 ml / min T 1/2 is lengthened. The indicator of total clearance decreases with hemodialysis - by 80%, during the standard procedure of hemodialysis, up to 10% of levocetirizine is removed.
In children aged 6–11 years (with a body weight of 20–40 kg), with a single oral administration of 5 mg of levocetirizine, the Cmax and AUC values (the area under the concentration-time curve characterizing the total concentration of the drug in the blood plasma) exceed those in adults about 2 times. In children aged from six months to five years, when taking the drug at a dose of 1.25 mg, the plasma concentration reaches a level corresponding to that in adults when taking levocetirizine at a daily dose of 5 mg.
In elderly patients, the dose of the drug is recommended to be adjusted taking into account renal function.
Indications for use
- pollinosis (hay fever);
- seasonal (intermittent) and year-round (persistent) allergic rhinitis and allergic conjunctivitis, accompanied by itching, nasal congestion, sneezing, rhinorrhea, conjunctival hyperemia, lacrimation;
- hives;
- itching and rash with allergic dermatoses.
Contraindications
- syndrome of glucose-galactose malabsorption, lactose intolerance, lactase deficiency;
- end-stage renal failure (CC less than 10 ml / min);
- age up to 6 years;
- hypersensitivity to cetirizine, hydroxyzine and any of the piperazine derivatives;
- individual intolerance to the components of the drug.
Levocetirizine should be taken with caution in chronic renal failure, in the presence of factors predisposing to urinary retention (including prostatic hyperplasia, spinal cord injury), concomitant use of alcohol, during pregnancy, during breastfeeding and in elderly patients.
Instructions for the use of Levocetirizine: method and dosage
The tablets are taken orally, swallowed whole, before meals or during meals, with a sufficient amount of water. The daily dose is taken at a time.
The recommended daily dose, it is also the maximum, for patients over 6 years old is 5 mg.
With renal failure and elderly patients, the dose should be adjusted depending on the CC value.
In case of impaired liver function, dose adjustment of the drug is not required.
Course duration:
- intermittent (seasonal) rhinitis with symptoms up to 4 days a week, with a total duration not exceeding 4 weeks: depending on the duration of the symptoms, treatment can be discontinued when symptoms disappear and resumed as needed;
- persistent (perennial) allergic rhinitis with symptoms 4 days a week or more, with a total duration exceeding 4 weeks: should be continued during the entire period of exposure to allergens, the duration of therapy in adults can be up to 180 days.
Do not allow taking a double dose in order to compensate for a missed one.
If the use of the drug does not give a therapeutic effect or new symptoms appear during treatment, you should consult your doctor.
Side effects
During clinical trials, the following undesirable effects have been recorded:
- often: adults (12 years and older) - dry mouth, fatigue; in all age categories - drowsiness, headache;
- infrequently: asthenia, abdominal pain.
As a result of post-registration studies, the following side effects of Levocetirizine were established:
- from the immune system: anaphylaxis, other hypersensitivity reactions;
- on the part of the cardiovascular system: palpitations, angina pectoris, tachycardia, jugular vein thrombosis;
- from the side of the psyche: insomnia, anxiety, aggression, hallucinations, agitation, depression, suicidal thoughts;
- from the nervous system: dizziness, convulsions, paresthesia, sinus thrombosis of the dura mater, tremor, fainting, dysgeusia;
- on the part of the organ of vision: blurred vision, visual impairment, manifestations of inflammatory processes;
- from the organ of hearing: vertigo;
- from the respiratory system: increased symptoms of rhinitis, shortness of breath;
- from the side of metabolism: increased appetite;
- from the digestive system: diarrhea, nausea, vomiting;
- from the hepatobiliary system: hepatitis, impaired liver function tests;
- from the urinary system: urinary retention, dysuria;
- dermatological reactions: itching, rash, urticaria, angioedema, photosensitization, skin cracks, persistent drug erythema, hypotrichosis;
- from the musculoskeletal system: muscle pain, arthralgia;
- general disorders: increased body weight, peripheral edema;
- other: cross-reactivity.
Overdose
Symptoms: drowsiness; in children - anxiety, agitation, turning into drowsiness.
Treatment: there is no specific antidote. Immediate gastric lavage or artificial vomiting. Appointment of supportive and symptomatic therapy. Hemodialysis is ineffective.
special instructions
The possibility of using the drug must be agreed with the doctor.
When deciding on the use of levocetirizine, one should take into account its ability to increase the risk of urinary retention.
Alcohol consumption is contraindicated during therapy. Simultaneous administration of levocetirizine with alcohol can cause lethargy and impairment of performance.
Influence on the ability to drive vehicles and complex mechanisms
Since the drug causes drowsiness, during the entire period of treatment, patients are advised to refrain from performing potentially hazardous activities (including driving vehicles), the performance of which depends on increased concentration of attention and high speed of psychomotor reactions.
Application during pregnancy and lactation
During gestation and breastfeeding, Levocetirizine should be used with caution and only as directed by a doctor.
Pediatric use
According to the instructions, Levocetirizine in the form of tablets cannot be used for the treatment of children under the age of 6 years due to limited information about their effectiveness and safety.
A liquid dosage form is recommended for children under 6 years of age.
With impaired renal function
The use of the drug is contraindicated in patients with end-stage chronic renal failure (CC less than 10 ml / min).
In renal failure, the dose should be adjusted depending on the CC value. For men, its value is calculated based on the concentration of serum creatinine as follows: subtract the patient's age from 140 and multiply by his weight, the result obtained is divided by the serum creatinine (mg / dl), multiplied by 72. For women, the result should be multiplied by a factor 0.85.
Patients with renal insufficiency are advised to use the following dosage regimen, which depends on QC:
- 50–79 ml / min and above: 5 mg per day;
- 30–49 ml / min: 5 mg once every 2 days;
- less than 30 ml / min: 5 mg once every 3 days.
- less than 10 ml / min, patients on dialysis: use is contraindicated.
For violations of liver function
In case of impaired liver function, dose adjustment of the drug is not required.
Use in the elderly
Levocetirizine should be taken with caution in old age. When prescribing, the state of renal function should be taken into account, since the active substance is excreted from the body by the kidneys. Correction of the dosage regimen is carried out taking into account the value of the patient's CC.
Drug interactions
Clinically significant undesirable effects from the interaction of levocetirizine with other drugs have not been established.
Analogs
Analogues of Levocetirizine are: Levocetirizine-Teva, Levocetirizine Sandoz, Allertek, Allercetin, Amertil, Alerza, Aleron, Allerset-L, Glenset, Zestra, Zyrtec, Zodak, Zenaro, Zetrinal, Zincet, Letizetino, Parlazin, R-Retinet, Zodak Express, Suprastinex, Tsesera, Cetirizine, Tsetrin, Tsetrilev.
Terms and conditions of storage
Keep out of the reach of children. Store at temperatures up to 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Available without a prescription.
Reviews about Levocetirizine
The few reviews about Levocetirizine are positive. Patients, pointing out its effectiveness, note a quick action, good tolerance of the drug and a relatively low cost.
Price for Levocetirizine in pharmacies
The price of Levocetirizine film-coated tablets can be: for 10 pcs. in the package ~ 113 rubles; for 30 pcs. in a package 178-225 rubles.
Anna Aksenova Medical journalist About the author
Education: 2004-2007 "First Kiev Medical College" specialty "Laboratory Diagnostics".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
