Loratadin

General characteristics. Structure:

Active ingredient: 10 mg of a loratadin in each tablet.

Excipients: lactoses monohydrate, potato starch, cellulose microcrystallic, stearic acid.

Pharmacological properties:

Pharmacokinetics. It is quickly and completely soaked up in digestive tract. Time of achievement of TCmax - 1,3 - 2,5 h; meal slows down it on 1 h Cmax at elderly people increases for 50%, at alcoholic damage of a liver - with increase in disease severity. Drug intake during food for 30-70% increases its bioavailability.

Communication with proteins of plasma - 97%.

It is metabolized in a liver with formation of an active metabolite of a deskarboetoksiloratadin (дезлоратадин) with the participation of isoenzymes of P450 CYP3A4 cytochrome and to a lesser extent CYP2D6.

Css of a loratadin and metabolite in plasma are reached for the 5th days of introduction. Does not get through a blood-brain barrier. T1/2 of a loratadin - 3 - 20 h (on average 8,4), an active metabolite - 8,8 - 92 h (on average 28 h); elderly patients respectively have 6,7-37 h (on average 18,2 h) and 11-38 h (17,5 h). At alcoholic damage of a liver of T1/2 increases with increase in weight of a disease. It is removed by kidneys and with bile.

At patients with a chronic renal failure and when carrying out a hemodialysis the drug pharmacokinetics practically does not change.

Indications to use:

Seasonal and year-round allergic rhinitis (including pollinosis); allergic conjunctivitis; small tortoiseshell (including chronic idiopathic); allergic pruritic dermatosis (contact allergic dermatitis, chronic eczema); Quincke's disease; the pseudo-allergic reactions caused by release of a histamine; allergic reactions to stings of insects.

Route of administration and doses:

Inside, not less than for 1 h to food. To adults and children 12 years − on 10 mg of 1 times a day are more senior. To children aged from 3 up to 12 years: with a body weight less than 30 kg − 5 mg of 1 times a day, more than 30 kg – 10 mg of 1 times a day, a daily dose - 10 mg.

Against the background of abnormal liver functions an initial dose – 5 mg/days.

Features of use:

Pregnancy and lactation. Safety of use of a loratadin during pregnancy is not established therefore its use is possible only in that case when the estimated advantage for mother exceeds potential risk for a fruit. Loratadin is allocated with breast milk therefore at prescription of medicine in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

Influence on ability to driving of motor transport and control of mechanisms. At the first appointment it is necessary to warn the patient about need to abstain from occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions because of risk of emergence of drowsiness. Further extent of restriction is established individually for each patient.

Use for persons with an abnormal liver function. To patients with heavy abnormal liver functions the initial dose is reduced to 5 mg a day in connection with possible disturbance of clearance of a loratadin.

Medicine contains lactose therefore it should not be applied to patients with exceptional hereditary cases of intolerance of a galactose, a lactose intolerance or glyukozo-galaktozny malabsorption.

It is necessary to stop Loratadin's reception not later, than in 48 hours prior to carrying out skin diagnostic аллергопроб for prevention of wrong results.

Does not cause accustoming.

Side effects:

Loratadin, as a rule, is well had. Side effects depend on individual sensitivity, have short character and completely disappear after drug withdrawal.

From a nervous system: fatigue, uneasiness, excitability (at children), dizziness, a headache, drowsiness, sleeplessness; nictitating spasm, dysphonia, hyperkinesias, paresthesias, tremor, amnesia, depression.

From skin and hypodermic cellulose: rash, alopecia.

From an urinogenital and urinary system: urine discoloration, painful desires on an urination; dysmenorrhea, menorrhagia, vaginitis.

From a metabolism: increase in body weight, perspiration, thirst.

From a musculoskeletal system: spasms of gastrocnemius muscles, arthralgia, mialgiya.

From the alimentary system: nausea, vomiting, dryness in a mouth, taste change, anorexia, a lock or diarrhea, dyspepsia, gastritis, a meteorism, increase in appetite, stomatitis.

From respiratory system: cough, bronchospasm, xeromycteria, sinusitis.

From sense bodys: vision disorder, conjunctivitis, eye and ears pain.

From cardiovascular system: heart consciousness, tachycardia.

Allergic reactions: Quincke's disease, small tortoiseshell, itch, photosensitization.

Interaction with other medicines:

At simultaneous use with ketokonazoly, erythromycin, Cimetidinum note increase in concentration of a loratadin in plasma, however without any clinical manifestations, including electrocardiographic.

Loratadin does not influence effect of ethanol.

Contraindications:

Hypersensitivity to medicine; pregnancy; breastfeeding; children's age up to 2 years.

With care apply at heavy abnormal liver functions.

Overdose:

Symptoms: at adult patients the headache, drowsiness and tachycardia at reception of medicine in doses of 40 - 180 mg considerably exceeding the recommended therapeutic dose of 10 mg were noted. At children with body weight less than 30 kg at reception in a dose more than 10 mg were noted extrapyramidal symptoms and a cardiopalmus.

Treatment: induction of vomiting, gastric lavage, purpose of absorbent carbon, symptomatic and maintenance therapy. Loratadin is not brought from an organism at a hemodialysis.

Storage conditions:

List B. In dry, protected from light, the place, unavailable to children, at a temperature not above 25 °C. A period of validity - 2 years. Drug cannot be used after expiry date.

Issue conditions:

Without recipe

Packaging:

10 tablets in a blister strip packaging, on 1 or 3 packagings in a pack (No. 10 × 1, No. 10 × 3).