LORATADINE (tablets 0.01 g)

Loratadine

International nonproprietary name (INN)

Loratadine.

Pharmacotherapeuticgroup

Antihistaminiс drug.

Composition

1 tablet contains 10 mg of loratadine.

Pharmacological effect

Pharmacodynamics

Loratadine is of antihistaminis, antiallergic, antiexudative, antipruritic effect. It selectively blocks H₁-histamine receptors and prevents histamine action on smooth muscles and vessels. It reduces capillary permeability, exudation, itch and erythema.

Antiallergic action develops in 30 minutes after oral intake and reaches its max. in 8-12 h. and persists at least 24 h. Loratadine has no effect on CNS, is of no anticholinergic or sedative effect. IthasnoinfluenceonQTintervalsofEKG. Itisoflow bronchodilatory action.

Pharmacokinetics

It is rapidly absorbed after oral intake. Loratadine blood С_махis evidenced in 1.3 h., of its active metabolite (descarboetoxyloratadine) in 2.5 h. food intakes does not influence significantly pharmacokinetics, (Loratadine AUC may increase by 40%, and of its active metabolite by 15%), but delays by 1 h. the time of С_мах(intake after meals is recommended). Plasma concentration 2.5-100 ng/ml: protein binding is 97% (active metabolite 73-77% at concentration 0.5-100 ng/ml). equal concentrations of Loratadine and its metabolite are reached by the 5^th day. It is intensively biotransformed in liver by cytochromуP450 system (mainly by CYP3A4 иand less by CYP2D6) with the formation of active metabolite. Within 24 h. about 30% of total dose is renal excreted as hydroxylated metabolites and/or conjugates. In 10 days about 80% metabolites are renal (40%) and feces (40%) excreted.Т_1/2 for Loratadine is 3-20 h. (average 8.4 h.), its active metabolite 8.8-92 h. (average 28 h.). In alcohol-induced liver injury and elderly patients Т_1/2 is higher. Loratadine is distributed like 119 l/kg,Cl- 142-202ml/min/kg. Within 24 h. 27% of loratadine is renal excreted as hydroxylated metabolites. Loratadine and its active metabolite is easily absorbed to breast milk and through placental barrier with the concentration in milk equal to plasma concentration. After intake of 40 mg, about 0.03% of the drug is found in mother’s milk during 48 h.

Indicationsforusage

Loratadineisadministeredinallergicrhinitis (seasonalandyear-round), allergicconjunctivite, pollinosis, chronicidiopathicutricaria, itching dermatosis (contactallergodermatitis, chroniceczema), angioneuroticedema. The drug is administered also in bronchial asthma (as auxiliary agent), allergic reactions to stings, pseudoallergic reactions to histaminoliberators.

Administration and dosage

The drug is administered for oral intake, in adults and children after 12 10 mg (1 tablet) a day. In children from 2 to 12 years old 5 mg (1/2 tablet) once a day. If the body weigh of a child is more than 30 kg, administer 10 mg once a day.

Specialindications

Loratadine has no effect on psychomotor reactions and does not provoke sedation. Still due to possible side effects (sleepiness, fatigue, concentration disorder, vertigo) avoid driving and other potentially dangerous activities with higher concentration and rapid psychomotor reaction during treatment.

Adverse reaction

The drug is well tolerated. Rare cases: dry mouth, vomit, nausea, gastritis, hyper fatigue, headache, sleepiness, concentration disorder, vertigo, skin eruption, hepatic disorder. In children: irritability, excitation or sedation. In single cases: possible irritation, depression, hyperkinesias, tremor, paresthesia, hypesthesia, visual impairment, lacrimation, conjunctivitis, blepharospasm, eye and ear pain, ear noise, convulsions. In patients with hepatic disorder Loratadine may decrease clearance of creatinine, in single cases jaundice, hepatitis, hepatic necrosis.

Contraindications

Hypersensitivity to the drug.

The drug is not recommended in children under 2.

Loratadine is excreted with breast milk, hence the doctor determines whether to cancel breast feeding under administration of loratadine.

Safety usage of loratadine in pregnancy is not determined, hence administer the drug only if the supposed advantage for mother prevails over the potential risk for the fetus.

Interaction with other drugs

Concurrent administration of the drug with ketoconazole, erythromycin (inhibitors CYP3A4), cimetidine (inhibitor CYP3A4 and CYP2D6): higher concentration of loratadine in blood plasma, still without clinical manifestation. Here the concentration of ketoconazole and cimetidine in blood plasma remains unaltered, and the concentration of erythromycin decreases by 15%.

Concurrent administration of the drug with inducers of microsomal oxidation (ethanol, phenitoin, barbiturate, riphamicine, phenylbutasone, tricyclic antidepressants) reduces loratadine effect. AlcoholactivitydoesnotpotentiateonCNS.

There are no safety data of loratadine administered concurrently with inhibitors of hepatic enzymes (guanidine, phlucosanol, phluoxitine), hence, administer with care.

Overdose

Symptoms: overdosing may cause sleepiness, tachycardia, headache.

Treatment: there is no specific antidote. Bring on vomit using syrup of ipecacuanha with further gastric lavage and/or intake of activated carbon.

Dosage form

Tablets 10 mg. 10 tablets in blister, 2 blisters in a pack.

The drug loratadine is manufactured in collaboration with “CTS Chemical Jndustries Ltd.”, Israel.