Pharmacodynamics
Loratadine is a tricyclic compound with a pronounced antihistamine action and is a selective blocker of peripheral H1-histamine receptors. It has a rapid and prolonged antiallergic effect. Onset of action is within 30 minutes after ingestion. Antihistamine effect reaches a maximum after 8-12 hours from the beginning of action and lasts for more than 24 hours.
Loratadine does not penetrate through the blood-brain barrier and has no effect on the central nervous system (CNS). It has no clinically significant anticholinergic or sedative effect, i.e. does not cause drowsiness and does not affect the speed of psychomotor reactions when used in the recommended doses. Administration of loratadine does not lead to prolongation of the QT interval on the electrocardiogram (ECG).
Loratadine has no significant selectivity towards H2-histamine receptors. It does not inhibit norepinephrine reuptake and has almost no effect on the cardiovascular system or rhythm driver function.
No clinically significant changes in vital signs, physical examination data, laboratory findings or electrocardiography were observed during long-term treatment.
Pharmacokinetics
Loratadine is quickly and well absorbed in the gastrointestinal tract. Time to reach maximum concentration (Tmax) of loratadine in blood plasma is 1-1.5 hours, and its active metabolite desloratadine – 1.5-3.7 hours. Food intake increases Tmax of loratadine and desloratadine by about 1 hour, but has no effect on the effectiveness of the drug.
Maximum concentration (Cmax) of loratadine and desloratadine is independent of food intake. In patients with chronic renal disease the maximum concentration (Cmax) and the area under the curve “concentration – time” (AUC) of loratadine and its active metabolite are increased compared to patients with normal renal function.
The half-life (T½) of loratadine and its active metabolite in this case does not differ from that of healthy patients. In patients with alcoholic liver damage Cmax and AUC of loratadine and its active metabolite increased twice in comparison with these figures in patients with normal liver function, while pharmacokinetics of its active metabolite did not change significantly.
Loratadine has a high degree (97-99%) and its active metabolite – a moderate degree (73-76%) of binding to plasma proteins.
Loratadine is metabolized to desloratadine by cytochrome P450 3A4 system and, to a lesser extent, by cytochrome P450 2D6 system. It is excreted through the kidneys (about 40% of the dose taken orally) and through the intestines (about 42% of the dose taken orally) for more than 10 days, mainly as conjugated metabolites.
Approximately 27% of the ingested dose is excreted through the kidneys within 24 hours after drug administration. Less than 1% of the active substance is excreted unchanged through the kidneys within 24 hours after drug intake.
Bioavailability of loratadine and its active metabolite is dose-dependent. Pharmacokinetic profiles of loratadine and its active metabolite in adult and elderly healthy volunteers were comparable.
The half-life (T½) of loratadine is 3 to 20 hours (mean 8.4 hours) and that of desloratadine is 8.8 to 92 hours (mean 28 hours); in elderly patients, 6.7 to 37 hours (mean 18.2 hours) and 11 to 39 hours (mean 17.5 hours) respectively. The half-life (T½) increases with alcoholic liver damage (depending on the severity of the disease) and does not change with chronic renal failure.
Hemodialysis in patients with chronic renal failure has no effect on the pharmacokinetics of loratadine and its active metabolite.
Indications
Diathesis, Edema, Runny nose (rhinitis), Sneezing, Allergic rhinitis, Urticaria, Allergic conjunctivitis, Increased lacrimation, Dermatitis, Conjunctivitis, Skin itching, Dermatosis, Allergies, Insect bites, PollinosisSeasonal (pollinosis) and year-round allergic rhinitis and allergic conjunctivitis – elimination of symptoms associated with these diseases – sneezing, nasal mucosa itching, rhinorrhea, burning and itching sensations in the eyes, lacrimation. Chronic ideopathic urticaria.
Active ingredient
Loratadine
Composition
Active ingredient:
Loratadine -10,0 mg.
Excipients:
lactose monohydrate – 71,3 mg
corn starch – 18,0 mg
magnesium stearate – 0,7 mg
How to take, the dosage
Orally, regardless of the time of meals.
Adults, including elderly ones and teenagers over 12 years old should take loratadine in dose of 10 mg (1 tablet) once a day.
When the preparation is used in elderly patients and patients with chronic renal insufficiency the dose adjustment is not required.
In children at the age of 3 – 12 years with body mass more than 30 kg – 10 mg (1 tablet) once a day.
In adults and children with body mass more than 30 kg with severe liver dysfunction the initial dose should be 10 mg (1 tablet) once a day.
Interaction
Food intake has no effect on the effectiveness of Loratadine. Loratadine does not increase the effect of alcohol on the central nervous system. Potential interaction with all known CYP3A4 or CYP2D6 inhibitors may occur, which leads to increased plasma levels of loratadine and an increased risk of side effects.
Co-administration of loratadine with ketoconazole, erythromycin (CYP3A4 isoenzyme inhibitor) or cimetidine (CYP3A4 and CYP2D6 isoenzyme inhibitor) increased loratadine plasma concentration was noted, but this increase was not clinically significant, including according to electrocardiography. Caution should be exercised when concomitant use with drugs that inhibit hepatic metabolism.
Special Instructions
Administration of loratadine should be stopped 48 hours before the skin test because antihistamines may distort the results of diagnostic studies.
Effect on the ability to drive vehicles, mechanisms
No adverse effect of loratadine on the ability to drive a car or perform other activities requiring increased concentration has been identified. However, in very rare cases, some patients experience drowsiness while taking loratadine, which may affect their ability to drive vehicles and operate mechanisms.
Contraindications
Hypersensitivity to loratadine and other components of the drug; lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome; breastfeeding period; children under 3 years of age and body weight less than 30 kg.
With caution
Severe liver function abnormalities; pregnancy (see section “Administration during pregnancy and breast-feeding”).
Side effects
In clinical trials with the participation of children aged from 2 to 12 years who took loratadine more often than the placebo group (“pacifiers”), headache (2.7%), nervousness (2.3%), fatigue (1%) were observed. In clinical trials with adults, adverse events observed more often than when using placebo occurred in 2% of patients taking loratadine. Headache (0,6%), somnolence (1,2%), appetite increase (0,5%) and insomnia (0,1%) were noted in adults while using loratadine more often than in placebo group.
According to the World Health Organization (WHO) side effects are classified according to their frequency of development as follows: Very common (≥ 1/10), common (≥ 1/100 to < 1/10), infrequent (≥ 1/1000 to < 1/100), rare (≥ 1/10000 to < 1/1000), very rare (< 1/10000), frequency unknown – the incidence could not be determined from available data.
Information concerning side effects is given according to the results of observations within the post-registration period.
Immune system disorders: very rarely – allergic reactions (including angioedema, anaphylaxis).
Nervous system disorders: very rarely – dizziness, seizures.
Cardio-vascular system: very rarely – tachycardia, palpitations.
Digestive system: very rare – dry mouth, nausea, gastritis.
Liver and biliary tract: very rarely – liver function abnormalities.
Skin and subcutaneous tissue: very rare – rash, allopecia.
General disorders: very rare – fatigue.
Laboratory and instrumental data: the frequency is unknown – weight gain.
If any of these side effects worsen or you notice any other side effects not specified in the instructions, inform the doctor.
Overdose
Symptoms: headache, drowsiness, tachycardia. In case of overdose seek immediate medical attention.
Treatment: symptomatic and supportive therapy. Possible gastric lavage, taking adsorbents (crushed activated carbon with water).
Loratadine is not excreted by hemodialysis. After emergency treatment, the patient’s condition should be monitored further.
Pregnancy use
A large amount of data on the use of loratadine in pregnant women (more than 1000 cases analyzed) indicate that there is no effect of the drug on the occurrence of malformations or feto- and neonatal toxicity of loratadine.
No reproductive toxicity has been observed in animal studies. As a precautionary measure, it is recommended to avoid using the drug during pregnancy. Loratadine and its active metabolite are excreted into the breast milk, so if the drug is prescribed during breastfeeding, the question of stopping breastfeeding should be addressed.
Similarities
Claritin, Lomilan, Clarisense, Loragesal, Loratadine, Loratadine Teva, Loratavel
Weight | 0.016 kg |
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Shelf life | 4 years. |
Conditions of storage | At a temperature not exceeding 25 ºC. Keep out of reach of children. |
Manufacturer | Update PFC AO, Russia |
Medication form | pills |
Brand | Update PFC AO |
Other forms…
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