Loratadine: instructions for use, indications,contraindications, dosage

Update: October 2018 Loratadine – a popular antihistamine
2nd generation drug that does not have a sedative effect
when used in therapeutic doses and does not have a negative
effects on the cardiovascular system. After treatment not
developing drug dependence.

It is a histamine H1 receptor blocker and is characterized by
fast and long action. It is effective at various types
allergies, quickly relieves manifestations of an allergic reaction.

Loratadine is used against allergies in the treatment of adults and children and
representative in three dosage forms.

Клинико-фармакологическая группа: противоаллергическое
means.

Composition, physico-chemical properties, price

All dosage forms are for oral administration.
application:

Loratadine tablets Effervescent tablets (loratadine-hemofarm) Syrup
Main substance Loratadine – 10 mg Loratadine – 1 mg in 1 ml of syrup
Auxiliary components Corn starch, magnesium stearate, talc, silica,
microcrystalline cellulose, lactose monohydrate
Sodium carbonate anhydrous, citric acid anhydrous, povidone,
silicon dioxide, lactose monohydrate, macrogol 6000, polysorbate
80
Glycerol, refined sugar, sodium benzoate, citric acid
anhydrous, propylene glycol, food cherry flavoring or
�Apricot 059, purified water
Physicochemical properties Round, white or slightly yellowish flat cylindrical
tablets, biconvex, separated by a line on one side
Round tablets of light yellow or white color Transparent or light yellow, greenish yellow syrup with
specific smell (cherry or apricot flavor)
Packaging

7 or 10 tablets in blister foil blister packs and
polyvinyl chloride. 1-3 blisters per carton

10 tablets in blisters and cardboard packs

Bottles of glass or plastic with a volume of 100 ml. Packaged –
measuring spoon 5 ml.

Price No. 30: 60-80 rubles. № 30: 70-80 rubles. 100 ml: 120-200 rubles.

pharmachologic effect

Provides antiallergic, antiexudative,
antipruritic effect, reduces the permeability of the capillary walls,
relieves puffiness and smooth muscle spasms.

The drug has a selective blocking effect on
peripheral histamine H1 receptors. These receptors
located in smooth muscles, the central nervous system and vessels, are responsible for
development of allergic reactions and allergy symptoms: they are involved
in the production of histamine. The drug, affecting these receptors, reduces
histamine production rate. This leads to
allergic reactions do not develop, and allergy symptoms
(swelling, itching, rash, redness of the skin, and others) disappear.

Among the distinctive advantages of the drug, we note:

  • lack of sedative action. Treatment can be given at
    the need to perform precise work, driving, in
    study time, etc .;
  • no negative effect on cardiovascular function (no
    leads to prolongation of the QT interval on the ECG) and nervous systems (not
    passes through the BBB);
  • does not cause addiction after treatment;
  • accepted only 1 time per day.

Pharmacodynamics and pharmacokinetics

Rapidly absorbed from the gastrointestinal tract: the active substance manifests its
efficiency after 20-30 minutes after oral administration
drug (effervescent tablets – after 15 minutes). Associated with
plasma protein by 97%.

The maximum concentration of the active substance in the blood
observed after 1.3 hours after application, and desloratadine
(active metabolite) – after 2.5 h. Equilibrium concentrations
loratadine and desloratadine in plasma are observed on the 5th day after
reception.

Eating lengthens the period of maximum concentration
blood levels of approximately 1 hour. Blood concentrations are higher in elderly
patients and people with chronic kidney failure
or alcoholic liver damage. Hemodialysis is not
affects the pharmacokinetics of the active substance and its active
metabolite.

Peak therapeutic efficacy occurs after 9-10 hours
reception. The drug acts during the day. Loratadine metabolism
carried out in the liver cells with the participation of cytochrome P450 ZA4 and
cytochrome P450 2D6.

The elimination half-life is 8 hours (it is extended in elderly patients and
in the presence of liver damage). Excreted through the kidneys, bile and
colon.

Indications for use

What helps loratadine:

  • Pollinosis seasonal and year-round;
  • Allergic rhinitis that is accompanied by profuse
    discharge from the nose and disrupt normal breathing;
  • Allergic conjunctivitis;
  • Idiopathic urticaria (chronic course);
  • Allergic skin diseases (including itchy
    dermatitis);
  • Angioedema;
  • Serum sickness;
  • Chronic eczema;
  • Allergic bronchial asthma;
  • Allergic reactions to medications, insect bites, food
    products;
  • Pseudo-allergic reactions.

Contraindications

The instructions for use of loratadine include the following:
contraindications:

  • Individual hypersensitivity to anyone component
    drug;
  • Lactose intolerance;
  • Lactation period;
  • Children’s age up to 2 years (syrup) and up to 3 years (pills);
  • Lactase deficiency;
  • Glucose-galactose malabsorption.

Women in position often ask if loratadine can be
of pregnancy. The answer is unequivocal – the use of the drug in the period
pregnancy is contraindicated.

Despite the absence of a negative and depressing effect on
CNS activity, during treatment is not recommended (but not
It is forbidden) to drive a car, operate complex machinery and
engage in work requiring high concentration.

special instructions

During treatment, it is impossible to exclude 100% the likelihood of development.
судорог, особенно у  пациентов с предрасположенностью.

Patients with renal or liver dysfunction should receive
adjusted dose of the drug (most often the dose is reduced by 50
%).

Dosage

All dosage forms should be taken at the same time.
days, 5-10 minutes before meals.

Pills:

  • Adults and children from 12 years old (and weighing more than 30 kg): once per
    day 10 mg (1 tablet);
  • Loratadine for children 3-12 years old (and weighing up to 30 kg): once per
    day 5 mg (half a tablet).

Effervescent tablets:

Before taking the tablet is dissolved in 200 ml of pure water. It is impossible
dissolve or chew the pill!

  • Adults and children from 12 years old (and weighing more than 30 kg): once per
    day 10 mg (1 dissolved tablet);
  • Loratadine children 2-12 years old (and weighing up to 30 kg): once per
    day 5 mg (half a tablet dissolved in water).

Syrup лоратадин:

Accept in pure form, if necessary drink down with water.

  • Adults and children over 12 years old, as well as children weighing more than
    30 kg: once a day 10 mg;
  • Children 2-12 years old and children weighing less than 30 kg: once a day 5
    mg.

The duration of loratadine is determined individually,
average rate: 7-14 days. Many are interested if assigned
loratadine, how much can you take as much as possible? In some cases
The drug is prescribed for a period of up to 30 days. Since getting used to it
does not cause, then to achieve the proper therapeutic effect
You can take the medicine for a long time. In any case, the duration
Admission is determined only by a doctor!

Overdose

Excess therapeutic dose leads to the development of weakness,
drowsiness, tachycardia, migraine. In case of accidental or intentional
exceeding the dose should be flushed stomach, take absorbent
drugs (polysorb, activated carbon). If necessary
more serious events are held in the medical environment
institutions.

Side effects

The most common cause of adverse reactions is
hypersensitivity to primary or secondary
components of the drug. All side effects disappear quickly after
cancellation of treatment.

  • On the part of the digestive system rarely nausea, vomiting,
    dry mouth, gastritis, flatulence. In some cases, possible
    abnormal liver function.
  • From the side of the central nervous system sometimes develops headache, insomnia,
    decreased concentration, dizziness, anxiety,
    nervousness, fatigue, irritability (more often in
    children).
  • On the part of the heart in rare cases may occur
    tachycardia.
  • From the musculoskeletal system: arthralgia, myalgia,
    back pain, cramps of the calf muscles.
  • On the part of the respiratory system: sneezing, nasal congestion, cough,
    laryngitis, shortness of breath.
  • From the urinary organs: discomfort when
    urination, vaginitis, change in urine color, menorrhagia.
  • Allergic reactions: skin rash. In isolated cases
    anaphylactic reactions are noted.
  • Skin reactions: alopecia (rare).
  • Other reactions: visual disturbances, fever, chills,
    ear pain.

Drug interactions

When administered simultaneously with drugs that inhibit
CYP3A4 and CYP2D6 isoenzymes or that are metabolized by
participation of these enzymes (including cimetidine, erythromycin, quinidine,
ketoconazole, fluoxetine, fluconazole), it is possible to change the plasma
concentrations of loratadine and / or these drugs.

Inductors of microsomal oxidation (ethanol, barbiturates,
Phenytoin, rifampicin, zixorin, phenylbutazone, tricyclic
antidepressants) reduce the effectiveness of loratadine.

What is better: loratadine or suprastin

Suprastin is one of the most popular antiallergic
drugs, which is widely known and probably in each
home first aid kit. Suprastin refers to antihistamine drugs
first generation, a shorter period of time (up to 8 hours),
taken several times a day. The drug penetrates through
the blood-brain barrier and may cause the following side effects
reactions: drowsiness, headache, reduced concentration
attention, fatigue, dizziness that imposes
certain restrictions on its use. However which drug
Better in each case, only the treating person can tell
doctor.

Analogs

Analogs лоратадина по действующему веществу:

Clarincens, tablets: 100-200 rubles; Claritin, tablets: 200-230 rubles; Claridol, tablets: 50-100 rubles;
Loragexal tablets: 20-50 rubles; Loratadin-Teva, tablets: 250-300 rubles; Loratadin-Stad, tablets: 60-80 rubles.

Автор: врач-гигиенист, эпидемиолог

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