AERIUS TABLETS

Israel - English - Ministry of Health

Buy It Now

Active ingredient:
DESLORATADINE
Available from:
MERCK SHARP & DOHME ISRAEL LTD
ATC code:
R06AX27
Pharmaceutical form:
TABLETS
Composition:
DESLORATADINE 5 MG
Administration route:
PER OS
Prescription type:
Required
Manufactured by:
SCHERING-PLOUGH LABO. N.V , BELGIUM
Therapeutic group:
DESLORATADINE
Therapeutic area:
DESLORATADINE
Therapeutic indications:
Aerius tablet is indicated in adults and adolescents aged 12 years and older for the relief of symptoms associated with:- allergic rhinitis - urticaria
Authorization number:
125 49 30441 21
Authorization date:
2017-05-31

Documents in other languages

Patient Information leaflet Patient Information leaflet - Arabic

22-01-2021

Patient Information leaflet Patient Information leaflet - Hebrew

15-03-2018

Page 1 of 1

MULT-1247173-0000

ראורבפ

2018

ה/דבכנ ה/אפור

/חקור

ה/דבכנ

:ןודנה

Aerius syrup 0.5mg/ml and Aerius tablets 5 mg (Desloratadine)

סוירא

פוריס

0.5

מ

"

ג

/

מ

"

ל

או תוילבט סויר

5

ג''מ

)

ןידטרולסד

(

Dosage Form: Tablets/ Syrup

Composition: Tablets: 5 mg desloratadine

Syrup: 0.5 mg/ml desloratadine

לארשי םהודו פראש קרמ תרבח

MSD)

לש ןכרצלו אפורל םינולעה ןוכדע לע עדייל תשקבמ (

syrup

®

Aerius

ו

-

tablets

®

Aerius

היוותהה ןושל ןלהל

רישכתל תרשואמה םי

:

Aerius tablets

Aerius tablet is indicated in adults and adolescents aged 12 years and older for the relief of

symptoms associated with:

- allergic rhinitis

- urticaria

Aerius syrup

Aerius syrup is indicated in adults, adolescents and children over the age of 1 year for the relief of

symptoms associated with :

- allergic rhinitis (AR),

- chronic idiopathic urticaria (CIU).

עדימל

אלמ

תוארוהלו

ןתמ

,תוטרופמ

שי

ןייעל

ןולעב

אפורל

ןכרצל ןולעו

רשואמה

לע

ידי

דרשמ

תואירבה

ל ןולעב םייתוהמ םינוכדע אפור

םירישכתה לש

Aerius tablets and syrup

.

4.8

Undesirable effects

Tabulated list of adverse reaction:

ןכרצל ןולעב םייתוהמ םינוכדע

םירישכתה לש

Aerius tablets and syrup

.

4

.

יאוול תועפות

:םירגובמ

אל םייקה עדימה ךותמ תוחיכשה תא ךירעהל ןתינ אל :עודי

.ןובאתב הילע ,לקשמב הילע

םינולעה

םימסרופמ

רגאמב

תופורתה

רתאבש

טנרטניאה

לש

היינפ ידי לע םיספדומ םלבקל ןתינ .תואירבה דרשמ לעבל

,םושירה תרבח

ןופלטב ,

09-9533333

syrup

®

Aerius

ו

-

tablets

®

Aerius

פומ יצ

.מ"עב גולובונ תרבח י"ע

,הכרבב

לכימ רפרס

הנוממ תחקור

לארשי

References:

Aerius_syrup_SPC_022018

Aerius_syrup_PPI_HEB_022018

Aerius_tablets_SPC_022018

Aarius_tablets_PIL_HEB_022018

System

Organ Class

Frequency

Adverse reactions seen with

Aerius

Metabol

and nutrition

Disorders

Not known

Increased appetite

Investigations

Not known

Weight increased

1.

NAME OF THE MEDICINAL PRODUCT

Aerius

Tablets

2.

QUALITATIVE AND QUANTITATIVE COMPOSITION

Each tablet contains 5 mg desloratadine.

Excipient(s) with known effect:

This medicine contains lactose.

For the full list of excipients, see section 6.1.

3.

PHARMACEUTICAL FORM

Film-coated tablets

4.

CLINICAL PARTICULARS

4.1

Therapeutic indications

Aerius tablet is indicated in adults and adolescents aged 12 years and older for the relief of symptoms

associated with:

allergic rhinitis (see section 5.1)

urticaria (see section 5.1)

4.2

Posology and method of administration

Posology

Adults and adolescents (12 years of age and over)

The recommended dose of Aerius is one tablet once a day.

Intermittent allergic rhinitis (presence of symptoms for less than 4 days per week or for less than

4 weeks) should be managed in accordance with the evaluation of patient’s disease history and the

treatment could be discontinued after symptoms are resolved and reinitiated upon their reappearance.

In persistent allergic rhinitis (presence of symptoms for 4 days or more per week and for more than

4 weeks), continued treatment may be proposed to the patients during the allergen exposure periods.

Paediatric population

There is limited clinical trial efficacy experience with the use of desloratadine in adolescents

12 through 17 years of age (see sections 4.8 and 5.1).

The safety and efficacy of Aerius 5 mg film-coated tablets in children below the age of 12 years have

not been established.

Method of administration

Oral use.

The dose can be taken with or without food.

4.3

Contraindications

Hypersensitivity to the active substance, to any of the excipients

listed in section 6.1, or to loratadine.

4.4

Special warnings and precautions for use

In the case of severe renal insufficiency, Aerius should be used with caution (see section 5.2).

Desloratadine should be administered with caution in patients with medical or familial history of

seizures, and mainly young children (see section 4.8), being more susceptible to develop new

seizures under desloratadine treatment. Healthcare providers may consider discontinuing

desloratadine in patients who experience a seizure while on treatment.

Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or

glucose-galactose malabsorption should not take this medicine.

4.5

Interaction with other medicinal products and other forms of interaction

No clinically relevant interactions were observed in clinical trials with desloratadine tablets in which

erythromycin or ketoconazole were co-administered (see section 5.1).

Paediatric population

Interaction studies have only been performed in adults.

In a clinical pharmacology trial Aerius tablets taken concomitantly with alcohol did not potentiate the

performance impairing effects of alcohol (see section 5.1).

However, cases of alcohol intolerance and

intoxication have been reported during post-marketing use. Therefore, caution is recommended if

alcohol is taken concomitantly.

4.6

Fertility, pregnancy and lactation

Pregnancy

A large amount of data on pregnant women (more than 1,000 pregnancy outcomes) indicate no

malformative nor foeto/ neonatal toxicity of desloratadine. Animal studies do not indicate direct or

indirect harmful effects with respect to reproductive toxicity (see section 5.3). As a precautionary

measure, it is preferable to avoid the use of Aerius during pregnancy.

Breast-feeding

Desloratadine has been identified in breastfed newborns/infants of treated women. The effect of

desloratadine on newborns/infants is unknown. A decision must be made whether to discontinue

breast-feeding or to discontinue/abstain from Aerius therapy taking into account the benefit of breast

feeding for the child and the benefit of therapy for the woman.

Fertility

There are no data available on male and female fertility.

4.7

Effects on ability to drive and use machines

Aerius has no or negligible influence on the ability to drive and use machines based on clinical trials.

Patients should be informed that most people do not experience drowsiness. Nevertheless, as there is

individual variation in response to all medicinal products, it is recommended that patients are advised

not to engage in activities requiring mental alertness, such as driving a car or using machines, until

they have established their own response to the medicinal product.

4.8

Undesirable effects

Summary of the safety profile

In clinical trials in a range of indications including allergic rhinitis and chronic idiopathic urticaria, at the

recommended dose of 5 mg daily, undesirable effects with Aerius were reported in 3 % of patients in

excess of those treated with placebo. The most frequent of adverse reactions reported in excess of

placebo were fatigue (1.2 %), dry mouth (0.8 %) and headache (0.6 %).

Paediatric population

In a clinical trial with 578 adolescent patients, 12 through 17 years of age, the most common adverse

event was headache; this occurred in 5.9 % of patients treated with desloratadine and 6.9 % of

patients receiving placebo.

Tabulated list of adverse reactions

The frequency of the clinical trial adverse reactions reported in excess of placebo and other

undesirable effects reported during the post-marketing period are listed in the following table.

Frequencies are defined as very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1,000

to < 1/100), rare (≥ 1/10,000 to < 1/1,000), very rare (< 1/10,000) and not known (cannot be estimated

from the available data).

System Organ Class

Frequency

Adverse reactions seen with Aerius

Metabolism and nutrition

disorders

Not known

Increased appetite

Psychiatric disorders

Very rare

Not known

Hallucinations

Abnormal behaviour,

aggression

Nervous system disorders

Common

Very rare

Headache

Dizziness, somnolence, insomnia,

psychomotor hyperactivity, seizures

Cardiac disorders

Very rare

Tachycardia, palpitations

Not known

QT prolongation

Gastrointestinal disorders

Common

Very rare

Dry mouth

Abdominal pain, nausea, vomiting,

dyspepsia, diarrhoea

Hepatobiliary disorders

Very rare

Not known

Elevations of liver enzymes, increased

bilirubin, hepatitis

Jaundice

Skin and subcutaneous tissue

disorders

Not known

Photosensitivity

Musculoskeletal and

connective tissue disorders

Very rare

Myalgia

General disorders

and

administration site conditions

Common

Very rare

Not known

Fatigue

Hypersensitivity reactions (such as

anaphylaxis, angioedema, dyspnoea,

pruritus, rash, and urticaria)

Asthenia

Investigations

Not known

Weight increased

Paediatric population

Other undesirable effects reported during the post-marketing period in paediatric patients with an

unknown frequency included QT prolongation, arrhythmia, bradycardia,

abnormal behaviour, and

aggression.

A retrospective observational safety study indicated an increased incidence of new-onset seizure in

patients 0 to 19 years of age when receiving desloratadine compared with periods not receiving

desloratadine. Among children 0-4 years old, the adjusted absolute increase was 37.5 (95%

Confidence Interval (CI) 10.5-64.5) per 100,000 person years (PY) with a background rate of new

onset seizure of 80.3 per 100,000 PY. Among patients 5-19 years of age, the adjusted absolute

increase was 11.3 (95% CI 2.3-20.2) per 100,000 PY with a background rate of 36.4 per 100,000 PY.

(See section 4.4.)

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It

allows continued monitoring of the benefit/risk balance of the medicinal product.

Any suspected adverse events should be reported to the Ministry of Health according to the National

Regulation by using an online form:

https://sideeffects.health.gov.il

4.9

Overdose

The adverse event profile associated with overdosage, as seen during post-marketing use, is similar to

that seen with therapeutic doses, but the magnitude of the effects can be higher.

Treatment

In the event of overdose, consider standard measures to remove unabsorbed active substance.

Symptomatic and supportive treatment is recommended.

Desloratadine is not eliminated by haemodialysis; it is not known if it is eliminated by peritoneal

dialysis.

Symptoms

Based on a multiple dose clinical trial, in which up to 45 mg of desloratadine was administered

(nine times the clinical dose), no clinically relevant effects were observed.

Paediatric population

The adverse event profile associated with overdosage, as seen during post-marketing use, is similar to

that seen with therapeutic doses, but the magnitude of the effects can be higher.

5.

PHARMACOLOGICAL PROPERTIES

5.1

Pharmacodynamic properties

Pharmacotherapeutic group: antihistamines – H

antagonist, ATC code: R06A X27

Mechanism of action

Desloratadine is a non-sedating, long-acting histamine antagonist with selective peripheral H

-receptor

antagonist activity. After oral administration, desloratadine selectively blocks peripheral histamine H

receptors because the substance is excluded from entry to the central nervous system.

Desloratadine has demonstrated antiallergic properties from in vitro studies. These include inhibiting

the release of proinflammatory cytokines such as IL-4, IL-6, IL-8, and IL-13 from human mast

cells/basophils, as well as inhibition of the expression of the adhesion molecule P-selectin on

endothelial cells. The clinical relevance of these observations remains to be confirmed.

Clinical efficacy and safety

In a multiple dose clinical trial, in which up to 20 mg of desloratadine was administered daily for

14 days, no statistically or clinically relevant cardiovascular effect was observed. In a clinical

pharmacology trial, in which desloratadine was administered at a dose of 45 mg daily (nine times the

clinical dose) for ten days, no prolongation of QTc interval was seen.

No clinically relevant changes in desloratadine plasma concentrations were observed in multiple-dose

ketoconazole and erythromycin interaction trials.

Desloratadine does not readily penetrate the central nervous system. In controlled clinical trials, at the

recommended dose of 5 mg daily, there was no excess incidence of somnolence as compared to

placebo. Aerius given at a single daily dose of 7.5 mg did not affect psychomotor performance in

clinical trials. In a single dose study performed in adults, desloratadine 5 mg did not affect standard

measures of flight performance including exacerbation of subjective sleepiness or tasks related to

flying.

In clinical pharmacology trials, co-administration with alcohol did not increase the alcohol-induced

impairment in performance or increase in sleepiness. No significant differences were found in the

psychomotor test results between desloratadine and placebo groups, whether administered alone or

with alcohol.

In patients with allergic rhinitis, Aerius was effective in relieving symptoms such as sneezing, nasal

discharge and itching, as well as ocular itching, tearing and redness, and itching of palate. Aerius

effectively controlled symptoms for 24 hours.

Paediatric population

The efficacy of Aerius tablets has not been clearly demonstrated in trials with adolescent patients

12 through 17 years of age.

In addition to the established classifications of seasonal and perennial, allergic rhinitis can alternatively

be classified as intermittent allergic rhinitis and persistent allergic rhinitis according to the duration of

symptoms. Intermittent allergic rhinitis is defined as the presence of symptoms for less than 4 days per

week or for less than 4 weeks. Persistent allergic rhinitis is defined as the presence of symptoms for 4

days or more per week and for more than 4 weeks.

Aerius was effective in alleviating the burden of seasonal allergic rhinitis as shown by the total score of

the rhino-conjunctivitis quality of life questionnaire. The greatest amelioration was seen in the domains

of practical problems and daily activities limited by symptoms.

Chronic idiopathic urticaria was studied as a clinical model for urticarial conditions, since the

underlying pathophysiology is similar, regardless of etiology, and because chronic patients can be

more easily recruited prospectively. Since histamine release is a causal factor in all urticarial diseases,

desloratadine is expected to be effective in providing symptomatic relief for other urticarial conditions,

in addition to chronic idiopathic urticaria, as advised in clinical guidelines.

In two placebo-controlled six week trials in patients with chronic idiopathic urticaria, Aerius was

effective in relieving pruritus and decreasing the size and number of hives by the end of the first

dosing interval. In each trial, the effects were sustained over the 24 hour dosing interval. As with other

antihistamine trials in chronic idiopathic urticaria, the minority of patients who were identified as non-

responsive to antihistamines was excluded. An improvement in pruritus of more than 50 % was

observed in 55 % of patients treated with desloratadine compared with 19 % of patients treated with

placebo. Treatment with Aerius also significantly reduced interference with sleep and daytime function,

as measured by a four-point scale used to assess these variables.

5.2

Pharmacokinetic properties

Absorption

Desloratadine plasma concentrations can be detected within 30 minutes of administration.

Desloratadine is well absorbed with maximum concentration achieved after approximately 3 hours; the

terminal phase half-life is approximately 27 hours. The degree of accumulation of desloratadine was

consistent with its half-life (approximately 27 hours) and a once daily dosing frequency. The

bioavailability of desloratadine was dose proportional over the range of 5 mg to 20 mg.

In a pharmacokinetic trial in which patient demographics were comparable to those of the general

seasonal allergic rhinitis population, 4 % of the subjects achieved a higher concentration of

desloratadine. This percentage may vary according to ethnic background. Maximum desloratadine

concentration was about 3-fold higher at approximately 7 hours with a terminal phase half-life of

approximately 89 hours. The safety profile of these subjects was not different from that of the general

population.

Distribution

Desloratadine is moderately bound (83 % - 87 %) to plasma proteins. There is no evidence of clinically

relevant medicine accumulation following once daily dosing of desloratadine (5 mg to 20 mg) for

14 days.

Biotransformation

The enzyme responsible for the metabolism of desloratadine has not been identified yet, and

therefore, some interactions with other medicinal products cannot be fully excluded. Desloratadine

does not inhibit CYP3A4 in vivo, and in vitro studies have shown that the medicinal product does not

inhibit CYP2D6 and is neither a substrate nor an inhibitor of P-glycoprotein.

Elimination

In a single dose trial using a 7.5 mg dose of desloratadine, there was no effect of food (high-fat, high

caloric breakfast) on the disposition of desloratadine. In another study, grapefruit juice had no effect on

the disposition of desloratadine.

Renally impaired patients

The pharmacokinetics of desloratadine in patients with chronic renal insufficiency (CRI) was compared

with that of healthy subjects in one single-dose study and one multiple dose study. In the single-dose

study, the exposure to desloratadine was approximately 2 and 2.5-fold greater in subjects with mild to

moderate and severe CRI, respectively, than in healthy subjects. In the multiple-dose study, steady

state was reached after Day 11, and compared to healthy subjects the exposure to desloratadine was

~1.5-fold greater in subjects with mild to moderate CRI and ~2.5-fold greater in subjects with severe

CRI. In both studies, changes in exposure (AUC and C

) of desloratadine and

3-hydroxydesloratadine were not clinically relevant.

5.3

Preclinical safety data

Desloratadine is the primary active metabolite of loratadine. Non-clinical studies conducted with

desloratadine and loratadine demonstrated that there are no qualitative or quantitative differences in

the toxicity profile of desloratadine and loratadine at comparable levels of exposure to desloratadine.

Non-clinical data reveal no special hazard for humans based on conventional studies of safety

pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, toxicity to reproduction and

development. The lack of carcinogenic potential was demonstrated in studies conducted with

desloratadine and loratadine.

6.

PHARMACEUTICAL PARTICULARS

6.1

List of excipients

Tablet core: Dibasic calcium phosphate dihydrate, microcrystalline cellulose, corn starch, talc,

carnauba wax, white wax.

Tablet coating: blue color film coat (contains lactose monohydrate, hydroxypropyl methycellulose,

titanium dioxide,

polyethylene glycol, indigotin (E132)), clear coat (contains, hydroxypropyl

methycellulose, polyethylene glycol).

6.2

Incompatibilities

Not applicable.

6.3

Shelf life

2 years

6.4

Special precautions for storage

Store below 30°C.

Store in the original package.

6.5

Nature and contents of container

Aerius is supplied in blisters comprised of laminate blister film with foil lidding.

The materials of the blister consist of a polychlorotrifluoroethylene (PCTFE)/Polyvinyl Chloride (PVC)

film (product contact surface) with an aluminium foil lidding coated with a vinyl heat seal coat (product

contact surface) which is heat sealed.

Packs of 2, 5, 7, 10, 14, 15, 20, 30

tablets.

Not all pack sizes may be marketed.

6.6

Special precautions for disposal

No special requirements.

7.

Manufacturer:

Schering-Plough Labo N.V., Heist-op-den-berg, Belgium

8.

License holder:

Merck Sharp & Dohme (Israel-1996) Company Ltd., P.O.Box 7121, Petah-Tikva 49170.

9.

Licence No.:

Aerius tablets: 125.49.30441

Revised in May 2020.

רשוא

11.11

_ ךיראת

__

92

,ץרמ

9111

___

רישכת םש תילגנאב

AERIUS

םושירה רפסמ

125 49 30441 21

םושירה לעב םש

.

1996) Company Ltd

Merck Sharp & Dohme (Israel

ה טורפל דעוימ הז ספוט דבלב תורמחה

תושקובמה תורמחהה

ןולעב קרפ

טסקט

יחכונ

שדח טסקט

4.5 Interaction

with other

medicinal

products and

other forms of

interaction

In a clinical pharmacology trial Aerius tablets

taken concomitantly with alcohol did not potentiate

the performance impairing effects of alcohol (see

section 5.1). However, cases of alcohol

intolerance and intoxication have been reported

during post-marketing use. Therefore, caution is

recommended if alcohol is taken concomitantly.

4.7 Effects on

ability to drive

and use

machines

In clinical trials that

assessed the driving

ability, no impairment

occurred in patients

receiving

desloratadine. However,

patients should be

informed that very rarely

some people experience

drowsiness, which may

affect their ability to drive

or use machines.

Aerius has no or negligible influence on the ability

to drive and use machines based on clinical trials.

Patients should be informed that most people do

not experience drowsiness. Nevertheless, as

there is individual variation in response to all

medicinal products, it is recommended that

patients are advised not to engage in activities

requiring mental alertness, such as driving a car

or using machines, until they have established

their own response to the medicinal product.

4.8 Undesirable

effects

Paediatric population

In a clinical trial with 578 adolescent patients,

12 through 17 years of age, the most common

adverse event was headache; this occurred in

5.9 % of patients treated with desloratadine and

6.9 % of patients receiving placebo.

Tabulated list of adverse reactions

Cardiac disorders - Not known - QT prolongation

Hepatobiliary disorders - Not known – Jaundice

Skin and subcutaneous tissue disorders - Not

known – Photosensitivity

General disorders

and administration site

conditions - Not known - Asthenia

Paediatric population

Other undesirable effects reported during the

post-marketing period in paediatric patients with

an unknown frequency included QT prolongation,

arrhythmia, and bradycardia.

תושקובמה תורמחהה

ןולעב קרפ

טסקט

יחכונ

שדח טסקט

4.2

תליטנ

סוירא ןוזמ םע

,

היתש

ו

לוהוכלא

םילטונ רשאכ רהזיהל שי סוירא

לוהוכלא םע

4.2

שומישו הגיהנ תונוכמב

סוירא ,ץלמומה ןונימב

ךל םורגל היופצ אל ג"מ הדיריל וא םונמנל .תונריעב

םירידנ םירקמב ,םלוא ,דואמ שומיש

רישכתב

לולע

םורגל

תשוחתל

םונמנ

הלולעש

עיפשהל

לע

תלוכי

הגיהנה

שומישו

תונוכמב

,ץלמומה ןונימב סוירא

הניא

היופצ

וא גוהנל ךלש תלוכיה לע עיפשהל תונוכמב שמתשהל

קוסעל אל ץלמומ ,םונמנ םיווח םניא םישנאה תיברמש תורמל דע ,תונוכמ תלעפה וא תינוכמב הגיהנ ןוגכ ,תונריע תושרודה תויוליעפב .הפורתל ךלש הבוגתה תא ססבתש

3

.

שמתשת דציכ :הפורתב

סוירא רתוי תלטנ םא

ךירצ תייהש יפכמ

לוטיל שי סוירא

.ךל םשרנש יפכ קר תויעב תויופצ אל םא תויניצר .רתי תנמ תועטב תלטנ

רתוי תלטנ םא ,םלוא סוירא

,ךל רמאנש יפכמ .חקורל וא ךלש אפורל דימ ךכ לע רפס

2

.

יאוול תועפות

לש קווישה ךלהמב סוירא

לש םירקמ לע דואמ תורידנ םיתיעל חווד תדפרס ,דרג ,םיפוצפצ ,המישנב ישוק( תורומח תויגרלא תובוגת .)תוחיפנו ,וללה תורומחה יאוולה תועפותמ תחא לכב ןיחבמ התא םא .הפוחד תיאופר הרזע תלבקל תידיימ הנפו הפורתה תא לוטיל קספה

םירגובמ

לש קווישה ךלהמב סוירא :כ וחווד תואבה יאוולה תועפות ,

םייקה עדימה ךותמ תוחיכשה תא ךירעהל ןתינ אל :עודי אל

ןפוד תאצוי השלוח

וא/ו רועה לש הבהצה

םייניעה

הסוכמ שמשה רשאכ וליפא ,שמשל רועה לש תרבגומ תושיגר רואלו ,םיננע

תורואל אמגודל ,

ןוכמ( םוירלוס לש )ףוזיש

בלה תמיעפ ןפואב םייוניש

םידלי

םייקה עדימה ךותמ תוחיכשה תא ךירעהל ןתינ אל :עודי אל

יטיא קפוד

בלה תמיעפ ןפואב םייוניש

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