Desloratadine Tablets 5mg Taj Pharma

  1. Name of the medicinal product

Desloratadine  5mg film-coated tablets

  1. Qualitative and quantitative composition

Each film coated tablet contains:
Desloratadine                           5mg
Excipients                                 q.s
Colour: Red oxide of iron, Yellow oxide of iron & Titanium Dioxide USP

For the full list of excipients, see section 6.1.

  1. Pharmaceutical form

Film-coated tablet.

  1. Clinical particulars

4.1 Therapeutic indications

Desloratadine   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 Desloratadine   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 Desloratadine   5mg film-coated tablets in children below the age of 12 years have not been established. No data are available.

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, desloratadine 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, 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.

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, desloratadine 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 desloratadine 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 desloratadine 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

Desloratadine 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 5mg daily, undesirable effects with desloratadine 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 ClassFrequencyAdverse reactions seen with desloratadine
Metabolism and nutrition disordersNot knownIncreased appetite
Psychiatric disordersVery rare

Not known

Hallucinations

Abnormal behaviour, aggression

Nervous system disordersCommon

Very rare

Headache

Dizziness, somnolence, insomnia, psychomotor hyperactivity, seizures

Cardiac disordersVery rare

Not known

Tachycardia, palpitations

QT prolongation

Gastrointestinal disordersCommon

Very rare

Dry mouth

Abdominal pain, nausea, vomiting, dyspepsia, diarrhoea

Hepatobiliary disordersVery rare
Not known
Elevations of liver enzymes, increased bilirubin, hepatitis

Jaundice

Skin and subcutaneous tissue disordersNot knownPhotosensitivity
Musculoskeletal and connective tissue disordersVery rareMyalgia
General disorders and administration site conditionsCommon

Very rare

 

Not known

Fatigue

Hypersensitivity reactions (such as anaphylaxis, angioedema, dyspnoea, pruritus, rash, and urticaria)

Asthenia

InvestigationsNot knownWeight 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.

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.

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 45mg 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.

  1. Pharmacological properties

5.1 Pharmacodynamic properties

Pharmacotherapeutic group: antihistamines – H1 antagonist.

Mechanism of action

Desloratadine is a non-sedating, long-acting histamine antagonist with selective peripheral H1-receptor antagonist activity. After oral administration, desloratadine selectively blocks peripheral histamine H1-receptors because the substance is excluded from entry to the central nervous system.

Desloratadine has demonstrated anti-allergic properties from in vitro studies. These include inhibiting the release of pro-inflammatory 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 20mg 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 45mg 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 5mg daily, there was no excess incidence of somnolence as compared to placebo. Desloratadine given at a single daily dose of 7.5mg did not affect psychomotor performance in clinical trials. In a single dose study performed in adults, desloratadine 5mg 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, desloratadine was effective in relieving symptoms such as sneezing, nasal discharge and itching, as well as ocular itching, tearing and redness, and itching of palate. Desloratadine effectively controlled symptoms for 24 hours.

Paediatric population

The efficacy of desloratadine 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.

Desloratadine 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, desloratadine 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 desloratadine 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 5mg to 20mg.

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 (5mg to 20mg) 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 7.5mg 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 Cmax) 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.

  1. Pharmaceutical particulars

6.1 List of excipients

Tablet core:

Microcrystalline cellulose, Starch, pregelatinised, Mannitol, Talc, Magnesium stearate

Tablet coating:

Hypromellose , Titanium dioxide , Macrogol , Indigo carmine aluminum lake

6.2 Incompatibilities

Not applicable.

6.3 Shelf life

3 years

6.4 Special precautions for storage

Blisters:

This medicinal product does not require any special storage conditions.

Bottles:

This medicinal product does not require any special temperature storage conditions.

Keep the bottle tightly closed in order to protect from light.

6.5 Nature and contents of container

OPA/Aluminium/PVC–Aluminium blisters.

Pack sizes: 7, 10, 14, 20, 21, 30, 50, 90 and 100 tablets.

Polyethylene bottles containing a desiccant and closed with a polyethylene cap.

Pack sizes: 30 and 100 tablets.

Not all pack sizes may be marketed.

6.6 Special precautions for disposal and other handling

No special requirements.

Manufactured By:
Taj Pharmaceuticals Ltd.
at: Plot. No. 220, Mahagujarat
Industrial Estate, At & Post-Moraiya,
Tal-Sanand, Dist- Ahmedabad Gujarat (India)

Desloratadine Tablets 5mg Taj Pharma

Package leaflet: Information for the patient

Desloratadine 5mg film-coated tablets

desloratadine

Read all of this leaflet carefully before you start taking this medicine because it contains important information for you.
  • Keep this leaflet. You may need to read it
  • If you have any further questions, ask your doctor or
  • This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as
  • If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. See section

 

 

What is in this leaflet
  1. What Desloratadine is and what it is used for
  2. What you need to know before you take Desloratadine
  3. How to take Desloratadine
  4. Possible side effects
  5. How to store Desloratadine
  6. Contents of the pack and other information
1. What Desloratadine is and what it is used for

Desloratadine is an antiallergy medicine that does not make you drowsy. It helps control your allergic reaction and its symptoms.

Desloratadine is indicated for adults and adolescents (12 years of age and older) to:

relieve symptoms associated with allergic rhinitis (inflammation of the nasal passages caused by an allergy, for example, hay fever or allergy to dust mites). These symptoms include sneezing, runny or itchy nose, itchy palate, and itchy, red or watery eyes.

Desloratadine is also used to relieve the symptoms associated with urticaria (a skin condition caused by an allergy). These symptoms include itching and hives.

Relief of these symptoms lasts a full day and helps you to resume your normal daily activities and sleep.

You must talk to a doctor if you do not feel better or if you feel worse.

2. What you need to know before you take Desloratadine Do not take Desloratadine:

–     if you are allergic to desloratadine, to any of the other ingredients of this medicine (listed in section 6) or to loratadine.

Warnings and precautions

Talk to your doctor or pharmacist before taking Desloratadine if you:

  • have medical or familial history of
  • have poor kidney

If this applies to you, or if you are not sure, please check with your doctor or pharmacist.

Children

Desloratadine tablets are not suitable for children under 12 years of age.

Other medicines and Desloratadine

Tell your doctor or pharmacist if you are taking, have recently taken or might take any other medicines.

Desloratadine with alcohol

Caution is advised when taking desloratadine with alcohol.

Pregnancy and breast-feeding

If you are pregnant or breast-feeding, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before taking this medicine.

If you are pregnant or breast-feeding a baby, taking Desloratadine is not recommended.

Driving and using machines

At the recommended dose, Desloratadine is not expected to cause you to be drowsy or less alert. However, very rarely some people experience drowsiness, which may affect their ability to drive or use machines.

Desloratadine contains Sunset Yellow Aluminium Lake (E110), which may cause allergic reactions.

3. How to take Desloratadine

Always take this medicine exactly as your doctor or pharmacist has told you. Check with your doctor or pharmacist if you are not sure.

The recommended dose for adults and adolescents (12 years of age and older) is one tablet once a day. Swallow the tablet whole with water, with or without food.

Regarding the duration of treatment, your doctor will determine the type of allergic rhinitis you are suffering from and will determine for how long you should take Desloratadine.

If your allergic rhinitis is intermittent (presence of symptoms for less than 4 days per week or for less than 4 weeks), your doctor will recommend you a treatment schedule that will depend on the evaluation of the history of your disease.

If your allergic rhinitis is persistent (presence of symptoms for 4 days or more per week and for more than 4 weeks), your doctor may recommend you a longer term treatment.

For urticaria, the duration of treatment may be variable from patient to patient and therefore you should follow the instructions of your doctor.

If you take more Desloratadine than you should

Take Desloratadine only as it is prescribed for you. No serious problems are expected with accidental overdose. However, if you take more Desloratadine than you were told to, contact your doctor or pharmacist.

If you forget to take Desloratadine

If you forget to take your dose on time, take it as soon as possible, then go back to your regular dosing schedule. Do not take a double dose to make up for a forgotten dose.

If you have any further questions on the use of this medicine, ask your doctor or pharmacist.

4. Possible side effects

Like all medicines, this medicine can cause side effects, although not everybody gets them. In adults, side effects were about the same as with a dummy tablet. However, fatigue, dry mouth and headache were reported more often than with a dummy tablet. In adolescents, headache was the most commonly reported side effect.

If you notice any of the following side effects, stop taking this medicine and contact your doctor or go to the nearest hospital casualty department straight away:

Very rare: (may affect up to 1 in 10,000 people):

  • Severe allergic reactions such as difficulty in breathing, shortness of breath, wheezing, itching, hives and swelling of the face, lips, tongue or other parts of the body and rash
  • Fits (seizures)
  • Liver disease (nausea, vomiting, loss of appetite, feeling generally unwell, fever, itching, yellowing of the skin and eyes, light coloured bowel motions, dark coloured urine)
Not known: (frequency cannot be estimated from available data):
  • A change in the way the heart beats, which may make you feel dizzy or faint. This may be seen in tests of the electrical activity of the heart (‘electrocardiogram’ or ECG)

In clinical studies with desloratadine, the following side effects were reported as:

Common: (may affect up to 1 in 10 people):
  • Fatigue
  • Dry mouth
  • Headache

During the marketing of desloratadine, the following side effects were reported in adults, as:

Very rare: (may affect up to 1 in 10,000 people):
  • Fast heartbeat
  • Being sick (vomiting)
  • Dizziness
  • Muscle pain
  • Restlessness with increased body movement
  • Stomach ache
  • Upset stomach
  • Drowsiness
  • Seeing, feeling or hearing things that are not there (Hallucinations)
  • Pounding or irregular heartbeat
  • Feeling sick (nausea)
  • Diarrhoea
  • Inability to sleep
  • Abnormal liver function tests

 

Not known: (frequency cannot be estimated from available data):
  • Abnormal behavior
  • Aggression
  • Unusual weakness
  • Increased sensitivity of the skin to the sun, even in the case of hazy sun, and to UV light, for instance to UV lights of a solarium
  • Weight increased, increased appetite

 

Additional side effects in children and adolescents

Not known: (frequency cannot be estimated from available data):

  • Slow heart beat
Reporting of side effects

If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet.

5.  How to store Desloratadine

Keep this medicine out of the sight and reach of children. This medicine does not require any special storage conditions.

Do not use this medicine after the expiry date, which is stated on the carton and blister after EXP. The expiry date refers to the last day of that month.

Do not throw away any medicines via wastewater or household waste. Ask your pharmacist how to throw away medicines you no longer use. These measures will help protect the environment.

6. Contents of the pack and other information

What Desloratadine contains

Each film coated tablet contains:
Desloratadine                           5mg
Excipients                                 q.s
Colour: Red oxide of iron, Yellow oxide of iron & Titanium Dioxide USP

The other ingredients of the tablet are magnesium stearate, sodium lauril sulfate, silica colloidal anhydrous, microcrystalline cellulose and pregelatinised maize starch.

The tablet film coating contains: poly (vinyl alcohol), indigo carmine aluminium lake, sunset yellow aluminium lake section 2 Desloratadine contains sunset yellow), macrogol, talc and titanium dioxide.

What Desloratadine looks like and contents of the pack

Desloratadine 5mg film-coated tablets are packed in blisters in packs of 2, 3, 5, 7, 10, 15, 20, 30, 50,60, 90 and 100 tablets.

Not all pack sizes may be marketed.

Manufactured By:
Taj Pharmaceuticals Ltd.
at: Plot. No. 220, Mahagujarat
Industrial Estate, At & Post-Moraiya,
Tal-Sanand, Dist- Ahmedabad Gujarat (India)