Lezine

Le lezine est un antihistaminique non sédatif de troisième génération indiqué pour le soulagement des symptômes associés à la rhinite allergique saisonnière et pérenne et aux manifestations cutanées non compliquées de l'urticaire idiopathique chronique. Il a été développé à partir de la cétirizine antihistaminique de deuxième génération. Lezine est l'énantiomère R du racémate de cétirizine. La lezine est un agoniste inverse qui diminue l'activité aux récepteurs de l'histamine H1. Cela empêche à son tour la libération d'autres produits chimiques allergiques et l'augmentation de l'apport sanguin dans la région, et soulage les symptômes typiques du rhume des foins. Il n'empêche pas la libération réelle d'histamine des mastocytes. Lezine a été approuvé par la Food and Drug Administration des États-Unis le 25 mai 2007 et est commercialisé sous la marque Lezine® par sanofi-aventis U.S. LLC .

Rhinite allergique saisonnière

Le dichlorhydrate de lezine est indiqué pour le soulagement des symptômes associés à la rhinite allergique saisonnière chez les adultes et les enfants de 2 ans et plus.

Rhinite allergique pérenne

Le dichlorhydrate de lezine est indiqué pour le soulagement des symptômes associés à la rhinite allergique pérenne chez les adultes et les enfants de 6 mois et plus.

Urticaire chronique idiopathique

Le dichlorhydrate de lezine est indiqué pour le traitement des manifestations cutanées non compliquées de l'urticaire chronique idiopathique chez les adultes et les enfants de 6 ans et plus.

Lezine est un antihistaminique qui réduit les effets de l'histamine chimique naturelle dans le corps. L'histamine peut produire des symptômes d'éternuements, de démangeaisons, d'yeux larmoyants et de nez qui coule.

Le lezine est utilisé pour traiter les symptômes de allergies toute l'année (perenniales) chez les adultes et les enfants âgés d'au moins 6 mois. Il est également utilisé pour traiter les symptômes de allergies saisonnières chez les adultes et les enfants âgés d'au moins 2 ans.

Le lezine est également utilisé pour traiter les démangeaisons et les gonflements causés par l'urticaire chronique (urticaire) chez les adultes et les enfants âgés d'au moins 6 mois.

Le lezine peut également être utilisé à des fins non répertoriées dans ce guide de médicaments.

Lezine is available as 2.5 mg/5 mL (0.5 mg/mL) oral solution and as 5 mg breakable (scored) tablets, allowing for the administration of 2.5 mg, if needed. Lezine can be taken without regard to food consumption.

Adults And Children 12 Years Of Age and Older

The recommended dose of Lezine is 5 mg (1 tablet or 2 teaspoons [10 mL] oral solution) once daily in the evening. Some patients may be adequately controlled by 2.5 mg (½ tablet or 1 teaspoon [5 mL] oral solution) once daily in the evening.

Children 6 To 11 Years Of Age

The recommended dose of Lezine is 2.5 mg (½ tablet or 1 teaspoon [5 mL] oral solution) once daily in the evening. The 2.5 mg dose should not be exceeded because the systemic exposure with 5 mg is approximately twice that of adults.

Children 6 Months To 5 Years Of Age

The recommended initial dose of Lezine is 1.25 mg (½ teaspoon oral solution) [2.5mL] once daily in the evening. The 1.25 mg once daily dose should not be exceeded based on comparable exposure to adults receiving 5 mg.

Dose Adjustment For Renal And Hepatic Impairment

In adults and children 12 years of age and older with:

• Mild renal impairment (creatinine clearance [CLCR] = 50-80 mL/min): a dose of 2.5 mg once daily is recommended;
• Moderate renal impairment (CLCR = 30-50 mL/min): a dose of 2.5 mg once every other day is recommended;
• Severe renal impairment (CLCR = 10-30 mL/min): a dose of 2.5 mg twice weekly (administered once every 3-4 days) is recommended;
• End-stage renal disease patients (CLCR < 10 mL/min) and patients undergoing hemodialysis should not receive Lezine.

No dose adjustment is needed in patients with solely hepatic impairment. In patients with both hepatic impairment and renal impairment, adjustment of the dose is recommended.

How supplied

Dosage Forms And Strengths

Lezine oral solution is a clear, colorless liquid containing 0.5 mg of Lezine dihydrochloride per mL.

Lezine tablets are white, film-coated, oval-shaped, scored, imprinted (with the letter Y in red color on both halves of the scored tablet) and contain 5 mg Lezine dihydrochloride.

Storage And Handling

Lezine tablets are white, film-coated, oval-shaped, scored, imprinted (with the letter Y in red color on both halves of the scored tablet) and contain 5 mg Lezine dihydrochloride. They are supplied in unit of use HDPE bottles.

90 Tablets (NDC 50474-920-90)

Lezine oral solution is a clear, colorless liquid containing 0.5 mg of Lezine dihydrochloride per mL.

Oral Solution in 5 oz polypropylene bottles (

Storage

Store at 20 to 25°C (68 to 77°F); excursions permitted to 15 to 30°C (59 to 86°F).

Manufactured for: UCB, Inc., Smyrna, GA 30080. Revised: June 2016

Voir aussi:
Quelles sont les informations les plus importantes que je devrais connaître sur Lezine?

Vous ne devez pas utiliser ce médicament si vous êtes allergique à la lezine ou à la cétirizine (Zyrtec).

Ne prenez pas de lezine si vous avez une maladie rénale terminale ou si vous êtes sous dialyse. Tout enfant de moins de 12 ans atteint d'une maladie rénale ne doit pas prendre de lezine.

Avant de prendre Lezine, informez votre médecin si vous avez une maladie du foie, une maladie rénale ou des problèmes de vésicule biliaire.

Il est très important de ne pas donner à un enfant plus que la dose prescrite de ce médicament. Le corps d'un enfant absorbe deux fois plus de la même dose de Lezine que le corps d'un adulte.

Appelez votre médecin si vos symptômes ne s'améliorent pas, s'ils s'aggravent ou si vous avez également de la fièvre.

Utilisez la solution de lezine selon les directives de votre médecin. Vérifiez l'étiquette sur le médicament pour obtenir des instructions de dosage exactes.

• Prenez la solution de lezine par voie orale avec ou sans nourriture. Prenez-le le soir, sauf indication contraire de votre médecin.
• Utilisez un appareil de mesure marqué pour le dosage des médicaments. Demandez de l'aide à votre pharmacien si vous ne savez pas comment mesurer votre dose.
• Si vous manquez une dose de solution de lezine, prenez-la dès que possible. S'il est presque temps pour votre prochaine dose, sautez la dose oubliée et revenez à votre schéma posologique habituel. Ne prenez pas 2 doses à la fois.

Posez à votre fournisseur de soins de santé toutes vos questions sur la façon d'utiliser la solution Lezine.

La lezine est utilisée pour traiter les symptômes de conditions allergiques telles que la fièvre allergique (rhume des foins), les allergies toute l'année comme la poussière ou les allergies aux animaux de compagnie et les éruptions cutanées chroniques de l'ortie.

Voir aussi:
Quels autres médicaments affecteront Lezine?

Des études d'interaction médicamenteuse ont été réalisées avec la cétirizine racémique.

Antipyrine, azithromycine, cimétidine, érythromycine, kétoconazole, théophylline et pseudoéphédrine : Des études d'interaction pharmacocinétique réalisées avec la cétirizine racémique ont démontré que la cétirizine n'interagissait pas avec l'antipyrine, la pseudoéphédrine, l'érythromycine, l'azithromycine, le kétoconazole et la cimétidine. Il y a eu une petite diminution (environ 16%) de la clairance de la cétirizine causée par la dose de 400 mg de théophylline. Il est possible que des doses de théophylline plus élevées aient un effet plus important.

Interactions avec d'autres médicaments:

Le degré d'absorption de Lezine n'est pas réduit avec les aliments, bien que le taux d'absorption soit diminué.

Chez les patients sensibles, l'administration simultanée de cétirizine ou de lezine et d'alcool ou d'autres dépresseurs du SNC peut avoir des effets sur le système nerveux central, bien qu'il ait été démontré que la cétirizine racémate ne potentialise pas l'effet de l'alcool.

See also:
What are the possible side effects of Lezine?

Use of Lezine has been associated with somnolence, fatigue, asthenia, and urinary retention.

Clinical Trials Experience

The safety data described below reflect exposure to Lezine in 2708 patients with seasonal or perennial allergic rhinitis or chronic idiopathic urticaria in 14 controlled clinical trials of 1 week to 6 months duration.

The short-term (exposure up to 6 weeks) safety data for adults and adolescents are based upon eight clinical trials in which 1896 patients (825 males and 1071 females aged 12 years and older) were treated with Lezine 2.5, 5, or 10 mg once daily in the evening.

The short-term safety data from pediatric patients are based upon two clinical trials in which 243 children with seasonal or perennial allergic rhinitis (162 males and 81 females 6 to 12 years of age) were treated with Lezine 5 mg once daily for 4 to 6 weeks, one clinical trial in which 114 children (65 males and 49 females 1 to 5 years of age) with allergic rhinitis or chronic idiopathic urticaria were treated with Lezine 1.25 mg twice daily for 2 weeks, and one clinical trial in which 45 children (28 males and 17 females 6 to 11 months of age) with symptoms of allergic rhinitis or chronic urticaria were treated with Lezine 1.25 mg once daily for 2 weeks.

The long-term (exposure of 4 or 6 months) safety data in adults and adolescents are based upon two clinical trials in which 428 patients (190 males and 238 females) with allergic rhinitis were exposed to treatment with Lezine 5 mg once daily. Long term safety data are also available from an 18-month trial in 255 Lezine-treated subjects 12-24 months of age.

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trial of another drug and may not reflect the rates observed in practice.

Adults and Adolescents 12 years of Age and Older

In studies up to 6 weeks in duration, the mean age of the adult and adolescent patients was 32 years, 44% of the patients were men and 56% were women, and the large majority (more than 90%) was Caucasian.

In these trials 43% and 42% of the subjects in the Lezine 2.5 mg and 5 mg groups, respectively, had at least one adverse event compared to 43% in the placebo group.

In placebo-controlled trials of 1-6 weeks in duration, the most common adverse reactions were somnolence, nasopharyngitis, fatigue, dry mouth, and pharyngitis, and most were mild to moderate in intensity. Somnolence with Lezine showed dose ordering between tested doses of 2.5, 5 and 10 mg and was the most common adverse reaction leading to discontinuation (0.5%).

Table 1 lists adverse reactions that were reported in greater than or equal to 2% of subjects aged 12 years and older exposed to Lezine 2.5 mg or 5 mg in eight placebo-controlled clinical trials and that were more common with Lezine than placebo.

Table 1 : Adverse Reactions Reported in ≥ 2%* of Subjects Aged 12 Years and Older Exposed to Lezine 2.5 mg or 5 mg Once Daily in Placebo-Controlled Clinical Trials 1-6 Weeks in Duration

Additional adverse reactions of medical significance observed at a higher incidence than in placebo in adults and adolescents aged 12 years and older exposed to Lezine are syncope (0.2%) and weight increased (0.5%).

Pediatric Patients 6 To 12 Years Of Age

A total of 243 pediatric patients 6 to 12 years of age received Lezine 5 mg once daily in two short-term placebo controlled double-blind trials. The mean age of the patients was 9.8 years, 79 (32%) were 6 to 8 years of age, and 50% were Caucasian. Table 2 lists adverse reactions that were reported in greater than or equal to 2% of subjects aged 6 to 12 years exposed to Lezine 5 mg in placebo-controlled clinical trials and that were more common with Lezine than placebo.

Table 2 : Adverse Reactions Reported in ≥ 2%* of Subjects Aged 6-12 Years Exposed to Lezine 5 mg Once Daily in Placebo-Controlled Clinical Trials 4 and 6 Weeks in Duration

Pediatric Patients 1 To 5 Years Of Age

A total of 114 pediatric patients 1 to 5 years of age received Lezine 1.25 mg twice daily in a two week placebo-controlled double-blind safety trial. The mean age of the patients was 3.8 years, 32% were 1 to 2 years of age, 71% were Caucasian and 18% were Black. Table 3 lists adverse reactions that were reported in greater than or equal to 2% of subjects aged 1 to 5 years exposed to Lezine 1.25 mg twice daily in the placebo-controlled safety trial and that were more common with Lezine than placebo.

Table 3 : Adverse Reactions Reported in ≥ 2%* of Subjects Aged 1-5 Years Exposed to Lezine 1.25 mg Twice Daily in a 2-Week Placebo-Controlled Clinical Trial

Pediatric Patients 6 To 11 Months Of Age

A total of 45 pediatric patients 6 to 11 months of age received Lezine 1.25 mg once daily in a two week placebo-controlled double-blind safety trial. The mean age of the patients was 9 months, 51% were Caucasian and 31% were Black. Adverse reactions that were reported in more than 1 subject (i.e. greater than or equal to 3% of subjects) aged 6 to 11 months exposed to Lezine 1.25 mg once daily in the placebo-controlled safety trial and that were more common with Lezine than placebo included diarrhea and constipation which were reported in 6 (13%) and 1 (4%) and 3 (7%) and 1 (4%) children in the Lezine and placebo-treated groups, respectively.

Long-Term Clinical Trials Experience

In two controlled clinical trials, 428 patients (190 males and 238 females) aged 12 years and older were treated with Lezine 5 mg once daily for 4 or 6 months. The patient characteristics and the safety profile were similar to that seen in the short-term studies. Ten (2.3%) patients treated with Lezine discontinued because of somnolence, fatigue or asthenia compared to 2 ( < 1%) in the placebo group.

There are no long term clinical trials in children below 12 years of age with allergic rhinitis or chronic idiopathic urticaria.

Laboratory Test Abnormalities

Elevations of blood bilirubin and transaminases were reported in < 1% of patients in the clinical trials. The elevations were transient and did not lead to discontinuation in any patient.

Post-Marketing Experience

In addition to the adverse reactions reported during clinical trials and listed above, adverse reactions have also been identified during post-approval use of Lezine. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Adverse reactions of hypersensitivity and anaphylaxis, increased appetite, angioedema, fixed drug eruption, pruritus, rash and urticaria, convulsion, paraesthesia, dizziness, tremor, dysgeusia, vertigo, movement disorders (including dystonia and oculogyric crisis), aggression and agitation, hallucinations, depression, insomnia, suicidal ideation, visual disturbances, blurred vision, palpitations, tachycardia, dyspnea, nausea, vomiting, hepatitis, dysuria, urinary retention, myalgia, arthralgia, and edema have been reported.

Besides these reactions reported under treatment with Lezine, other potentially severe adverse events have been reported from the post-marketing experience with cetirizine. Since Lezine is the principal pharmacologically active component of cetirizine, one should take into account the fact that the following adverse events could also potentially occur under treatment with Lezine: orofacial dyskinesia, severe hypotension, cholestasis, glomerulonephritis, still birth, tic, myoclonus, and extrapyramidal symptoms.