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Medically reviewed by Oliinyk Elizabeth Ivanovna, PharmD. Last updated on 09.04.2022
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Roletra 10mg Orodispersible Tablet is indicated for the symptomatic treatment of allergic rhinitis (AR) and chronic idiopathic urticaria (CIU).
Temporarily relieves these symptoms due to hay fever or other upper respiratory allergies:
- runny nose
- sneezing
- itchy, watery eyes
- itching of the nose or throat
Posology
Adults and children over 12 years of age
10 mg once daily (one orodispersible tablet once daily).
Paediatric population
Children 2 to 12 years of age with body weight more than 30 kg: 10 mg once daily (one orodispersible tablet once daily).
The 10 mg strength orodispersible tablet is not appropriate in children with a body weight less than 30 kg.
Efficacy and safety of Roletra in children under 2 years of age has not been established.
Patients with hepatic impairment
Patients with severe hepatic impairment should be administered a lower initial dose because they may have reduced clearance of Roletra. An initial dose of 10 mg every other day is recommended for adults and children weighing more than 30 kg.
Patients with renal impairment
No dosage adjustments are required in patients with renal insufficiency.
Elderly
No dosage adjustments are required in the elderly.
Method of administration
Roletra 10 mg orodispersible tablets should be handled with caution and with dry hands only.
Roletra 10 mg orodispersible tablets are intended for oral use.
The tablet shall be put on the tongue and wait until it is thoroughly disintegrated. Water or other liquid is not needed to swallow the dose.
The orodispersible tablet may be taken without regard to mealtime.
Directions
Use only with enclosed dosing cup
- adults and children 6 years and over: 2 teaspoonfuls (TSP) daily; do not take more than 2 teaspoonfuls (TSP) in 24 hours
- children 2 to under 6 years of age: 1 teaspoonful (TSP) daily; do not take more than 1 teaspoonful (TSP) in 24 hours
- children under 2 years of age: ask a doctor
- consumers with liver or kidney disease: ask a doctor
Roletra 10 mg orodispersible tablets are contraindicated in patients who are hypersensitive to the active substance or to any of the excipients in these formulations.
No information provided.
Roletra should be administered with caution in patients with severe hepatic impairment.
This product contains lactose and sorbitol. Patients with rare hereditary problems of fructose intolerance, galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
This product contains aspartame. Aspartame is a source of phenylalanine, which may be harmful for people with phenylketonuria.
The administration of Roletra should be discontinued at least 48 hours before skin tests since antihistamines may prevent or reduce otherwise positive reactions to dermal reactivity index.
WARNINGS
Included as part of the PRECAUTIONS section.
PRECAUTIONS
Do not use if you have ever had an allergic reaction to this product or any of its ingredients.
Ask a doctor before use if you have liver or kidney disease. Your doctor should determine if you need a different dose.
When using this product do not take more than directed. Taking more than directed may cause drowsiness.
Stop use and ask a doctor if an allergic reaction to this product occurs. Seek medical help right away.
If pregnant or breast-feeding, ask a health professional before use.
Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center right away.
In clinical trials that assessed driving ability, no impairment occurred in patients receiving Roletra. However, patients should be informed that very rarely some people experience drowsiness, which may affect their ability to drive or use machines.
Adverse events which have been associated with Roletra are given below. 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)
Not known (cannot be estimated from the available data).
In clinical trials in a paediatric population, children aged 2 through 12 years, common adverse reactions reported in excess of placebo were headache (2.7%), nervousness (2.3%), and fatigue (1%).
In clinical trials involving adults and adolescents in a range of indications including AR and CIU, at the recommended dose of 10 mg daily, adverse reactions with Roletra were reported in 2 % of patients in excess of those treated with placebo.
The most frequent adverse reactions reported in excess of placebo were somnolence (1.2%), headache (0.6%), increased appetite (0.5%) and insomnia (0.1%).
Other adverse reactions reported during the post-marketing period are listed in the following table.
| Organ | Frequency | Adverse reaction |
| Immune system disorders | Very rare | Hypersensitivity reactions (including angioedema and anaphylaxis) |
| Nervous system disorders | Very rare | Dizziness, convulsion |
| Cardiac disorders | Very rare | Tachycardia, palpitation |
| Gastrointestinal disorders | Very rare | Nausea, dry mouth, gastritis |
| Hepatobiliary disorders | Very rare | Abnormal hepatic function |
| Skin and subcutaneous tissue disorders | Very rare | Rash, alopecia |
| General disorders and administration site conditions | Very rare | Fatigue |
| Investigations | Not known | Weight increased |
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. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme: www.mhra.gov.uk/yellowcard or search for MHRA Yellow Card in the Google Play or Apple App Store.
No information provided.
Overdosage with Roletra increased the occurrence of anticholinergic symptoms. Somnolence, tachycardia, and headache have been reported with overdoses.
In the event of overdose, general symptomatic and supportive measures are to be instituted and maintained for as long as necessary. Administration of activated charcoal as a slurry with water may be attempted. Gastric lavage may be considered. Roletra is not removed by haemodialysis and it is not known if Roletra is removed by peritoneal dialysis. Medical monitoring of the patient is to be continued after emergency treatment.
No information provided.
Pharmacotherapeutic group: antihistamines - H1 antagonist, ATC code: R06A X13.
Mechanism of action
Roletra, the active ingredient in the medicinal product, is a tricyclic antihistamine with selective, peripheral Hl-receptor activity.
Pharmacodynamic effects
Roletra has no clinically significant sedative or anticholinergic properties in the majority of the population and when used at the recommended dosage.
During long-term treatment there were no clinically significant changes in vital signs, laboratory test values, physical examinations or electrocardiograms.
Roletra has no significant H2-receptor activity. It does not inhibit norepinephrine uptake and has practically no influence on cardiovascular function or on intrinsic cardiac pacemaker activity.
Absorption
Roletra is rapidly and well absorbed. Concomitant ingestion of food can delay slightly the absorption of Roletra but without influencing the clinical effect.
Distribution
Roletra is highly bound (97 % to 99 %) and its active metabolite moderately bound (73 % to 76 %) to plasma proteins.
In healthy subjects, plasma distribution half-lives of Roletra and its active metabolite are approximately 1 and 2 hours, respectively.
Biotransformation
After oral administration, Roletra is rapidly and well absorbed and undergoes an extensive first pass metabolism, mainly by CYP3A4 and CYP2D6. The major metabolite -desRoletra (DL)- is pharmacologically active and responsible for a large part of the clinical effect. Roletra and DL achieve maximum plasma concentrations (Tmax) between 1-1.5 hours and 1.5-3.7 hours after administration, respectively.
Increase in plasma concentrations of Roletra has been reported after concomitant use with ketoconazole, erythromycin, and cimetidine in controlled trials, but without clinically significant changes (including electrocardiographic).
Elimination
The mean elimination half-lives in healthy adult subjects were 8.4 hours (range = 3 to 20 hours) for Roletra and 28 hours (range = 8.8 to 92 hours) for the major active metabolite.
Approximately 40 % of the dose is excreted in the urine and 42 % in the faeces over a 10 day period and mainly in the form of conjugated metabolites. Approximately 27 % of the dose is eliminated in the urine during the first 24 hours. Less than 1 % of the active substance is excreted unchanged in active form, as Roletra or DL.
Linearity
The bioavailability parameters of Roletra and of the active metabolite are dose proportional.
Elderly
The pharmacokinetic profile of Roletra and its metabolites is comparable in healthy adult volunteers and in healthy geriatric volunteers.
Renal impairment
In patients with chronic renal impairment, both the AUC and peak plasma levels (Cmax) increased for Roletra and its metabolite as compared to the AUCs and peak plasma levels (Cmax) of patients with normal renal function. The mean elimination half-lives of Roletra and its metabolite were not significantly different from that observed in normal subjects. Haemodialysis does not have an effect on the pharmacokinetics of Roletra or its active metabolite in subjects with chronic renal impairment.
Hepatic impairment
In patients with chronic alcoholic liver disease, the AUC and peak plasma levels (Cmax) of Roletra were double while the pharmacokinetic profile of the active metabolite was not significantly changed from that in patients with normal liver function. The elimination half-lives for Roletra and its metabolite were 24 hours and 37 hours, respectively, and increased with increasing severity of liver disease.
Roletra and its active metabolite are excreted in the breast milk of lactating women.
Preclinical data reveal no special hazard based on conventional studies of safety, pharmacology, repeated dose toxicity, genotoxicity and carcinogenic potential.
In reproductive toxicity studies, no teratogenic effects were observed. However, prolonged parturition and reduced viability of offspring were observed in rats at plasma levels (AUC) 10 times higher than those achieved with clinical doses.
No evidence of mucous membrane irritation was observed after daily administration of up to 12 tablets (120 mg) of oral lyophilisates into the hamster cheek pouch for five days.
Not applicable.
No special requirements.
However, we will provide data for each active ingredient
