Okey docs

Treatment of allergies.Review of antihistamines of the third generation

loratadine

CLARITINE

cetirizine

ZYRTEC

ebastine

KESTINE

comparative
efficiency

Efficiency

+++

+++

+++


duration of action

24 hours

24 hours

48 h.


time of onset of effect

0,5 hours

1 hour

1 hour

dosing frequency

1 r / d

1 r / d

1 r / d

unwanted
phenomenon

Elongation
interval QT

no

no

No

Sedative
action

no

RARE

no

Strengthening
effects of alcohol

no

YES

no


side effects when combined with ketoconazole and erythromycin

no

no

YES

Dovelichenie
weight

no

no

no

application
in specific patient populations

Ability
use in children

& gt;2 years

& gt;2 years

& gt;12 years

Application
in pregnant

possible

not
recommended

contraindicated

Application
lactation

contraindicated

contraindicated

is contraindicated

Need for
dose reduction in the elderly

no

no

no


Need for dose reduction in patients with renal insufficiency

no

YES

YES

Necessity
dose reduction with abnormal liver

function is not

no

contraindicated

cost
treatment

cost
1 day of treatment, У.е.

0,57

0,70

0,57

The cost of the
monthly course of treatment, USD.

17,1

21

17,1

0,37

astemizole

HISMANAL

terfenadine

TREXYL

fexofenadine

TELFAST

comparative
efficiency

Efficiency

+++

+++

+++


duration of action

24 hours

18 - 24 hours

24 hourand


time of onset of effect

1 hour

1 hour

1 hour

frequency
dosing

1 r / d

1-2 p / d

1 r / d


comparative effectiveness

Elongation
interval QT

YES

YES

na

Sedative
action

no

no

no

Strengthening
effects of alcohol

no

no

no


side effects when combined with ketoconazole and erythromycin

YES

YES

no

Increase
weight

YES

no

no

application
in specific patient populations

Possibility
use in children

& Gt;1
of the year

& gt;3 years

& gt;12 years

Application
in pregnant

possible

contraindicated

possible

Application
lactation

contraindicated

contraindicated

is contraindicated

The need for dose reduction
in the elderly

no

no

no


Need for dose reduction in patients with renal insufficiency

no

no

YES

Necessity
dose reduction with abnormal liver

function contraindicated

contraindicated

no

cost
treatment

cost
1 day of treatment, У.е.

The cost of the
monthly course of treatment, cu

11.1

-

16,2

Allergia Spring.Nature awakens. .. Primrose blossoms. .. Birch, alder, poplar, hazel let out coquettish earrings;Buzzing bees, bumblebees, collecting pollen. .. The season of pollinosis begins( from the Latin pollinis of pollen) or hay fever - allergic reactions to pollen of plants.Summer comes.Blossom of cereals, tart sage, fragrant lavender. .. Then comes autumn and "mistress" is ragweed, the pollen of which is the most dangerous allergen.During flowering weed, up to 20% of the population suffers from lacrimation, coughing, allergic rhinitis.And the long-awaited Available winter.But there's a lot waiting for cold allergy.Again spring. .. And so all year round.

Contents: Generations of antihistamines The benefits of antihistamines 3 generations Antihistamines 3 generations: names and dosages Antihistamines of the third generation: side effects Antihistamines for children Purpose of antihistamines in pregnancy Antihistamines: from dimedrol to eryusis Antihistamines 4 generations:Myths and reality

And yet off-season allergy to animal hair, cosmetics, homelinessand so on.Plus, drug allergy, food.In addition, in recent years, the diagnosis of "allergies" is raised more often, and manifestations of the disease are more pronounced.

Facilitate the condition of patients with drugs that relieve the symptoms of allergic reactions, and above all - antihistamines( AHP).Histamine, stimulating H1-receptors, can be called the main culprit of the disease.He participates in the mechanism of the emergence of the main manifestations of allergies.Therefore, antihistamines are always prescribed as antiallergic drugs.

Antihistamines - blockers of H1 histamine receptors: properties, mechanism of action

Mediator( biologically active mediator) histamine affects:

  • Skin, causing itching, flushing.
  • Respiratory tract, provoking edema, bronchospasm.
  • Cardiovascular system, causing increased vascular permeability, cardiac rhythm disturbance, hypotension.
  • Gastrointestinal tract, stimulating gastric secretion.

Antihistamines relieve symptoms caused by endogenous release of histamine.They interfere with the development of hyperreactivity, but do not affect the sensitizing effect( hypersensitivity) of allergens, nor on the infiltration of mucous eosinophils( the type of leukocytes: their content in the blood increases with allergies).

Antihistamines:

  • Allergia significantly reduces the histamine-induced increase in capillary permeability;
  • relieves spasms of smooth muscles;
  • prevents tissue edema formation;
  • reduces the toxicity of histamine;
  • reduces the hypotensive effect of histamine;
  • alleviate the condition with allergies.

It should be borne in mind that not only histamine belongs to mediators involved in the pathogenesis( mechanism of occurrence) of allergic reactions.Besides him, acetylcholine, serotonin and other substances are "guilty" of inflammatory and allergic processes.Therefore, drugs that have only antihistamine activity, stop only acute manifestations of allergies.Systematic treatment requires complex desensitizing therapy.

Generations of antihistamines

We recommend to read:

Three groups( generations) of antihistamines are distinguished according to the current classification:
H1, first generation histamine blockers( tavegil, dimedrol, suprastin) - penetrate through a special filter - blood-brain barrierGEB), act on the central nervous system, providing a sedative effect;
H1 second-generation histamine blockers( fenkarol, loratadine, ebastin) - do not cause sedation( in therapeutic doses);
H1 histaminoblockers of the third generation( telphast, erius, zirtek) are pharmacologically active metabolites.Do not pass through the BBB, the CNS is minimal, so do not cause sedation.

The characteristics of the most popular antihistamines are given in the Table:

The benefits of antihistamines 3 generations

This group combines pharmacologically active metabolites of some drugs of previous generations:

  • fexofenadine( telphast, fexofast) is an active metabolite of terfenadine;
  • levocetirizine( xisal) - a derivative of cetirizine;
  • desloratadine( erius, desal) is an active metabolite of loratadine.

The latest generation of drugs is characterized by a significant selectivity( selectivity), they act solely on peripheral H1 receptors. Hence the advantages of :

  1. Efficacy: rapid absorption plus high bioavailability determine the rate of removal of allergic reactions.
  2. Practicality: does not affect performance;The absence of a sedative effect plus cardiotoxicity cancels the need to adjust the dose to elderly patients.
  3. Safety: do not become addictive - it allows you to prescribe long courses of therapy.Practically there is no interaction with concurrently taken drugs;Absorption is not dependent on food intake;The active substance is output "as is"( unchanged), i.e., the target organs( kidneys, liver) do not suffer.

Assign medicines for seasonal and chronic rhinitis, conjunctivitis, dermatitis, bronchospasm of an allergic nature.

Antihistamines 3 generations: names and dosages

Please note: dosages are indicated for adults.

Fexadine, telphast, fexofast take 120-180 mg x once a day.Indication: symptoms of hay fever( sneezing, itching, rhinitis), idiopathic urticaria( redness, itching).

Levocetirizine-teva, xizal take 5 mg x 1 time per day.Indications: chronic allergic rhinitis, idiopathic urticaria.

Desloratadine-teva, erius, dezal take 5 mg x 1 time per day.Indications: seasonal pollinosis, chronic idiopathic urticaria.

Third-generation antihistamines: side effects

With its relative safety, the third-generation histamine receptor blockers H1 can cause: agitation, convulsions, dyspepsia, abdominal pain, myalgia, dry mouth, insomnia, headache, asthenic syndrome, nausea, drowsiness, Dyspnoea, tachycardia, visual impairment, weight gain, paronymy( unusual dreams).

Antihistamines for children

Xylol in drops prescribed for children: over 6 years in a daily dose of 5 mg( = 20 drops);From 2 to 6 years in a daily dose of 2.5 mg( = 10 drops), more often by 1.25 mg( = 5 drops) x 2 times a day.
Levocetirizine-teva - dose for children over 6 years: 5 mg x 1 time per day.

Eryus syrup is allowed for children aged 1 to 6 years: 1.25 mg( = 2.5 ml syrup) x once a day;From 6 to 11 years: 2.5 mg( = 5 ml of syrup) x once a day;
adolescents from 12 years: 5 mg each( = 10 ml syrup) x once a day.

Erius is able to inhibit the development of the first phase of an allergic reaction and inflammation.In the case of chronic urticaria, reverse development of the disease occurs.The therapeutic efficacy of erius in the treatment of chronic urticaria is confirmed in a placebo-controlled( blind) multicenter study.Therefore, erius is recommended for use in children from one year old.

Important : a study of the effectiveness of the eryus in the form of tablets for resorption in the children's group was not carried out.But the pharmacokinetic data revealed in the study of the determination of drug doses with the participation of patients-children, indicate the possibility of using pastilles of 2.5 mg in the age group 6-11 years.

Fexofenadine 10 mg is given to adolescents from 12 years of age.

Allergy medications and their application in pediatrics are told by the doctor:

Prescribing antihistamines during pregnancy

Pregnant antihistamines of the third generation are not prescribed.In exceptional cases, the use of telphast or fexofast is allowed.

Important : information on the use of fexofenadine( telphast) drugs by pregnant women is not enough.Since studies conducted on experimental animals have not revealed signs of adverse effect of telphast on the general course of pregnancy and intrauterine development, the drug is considered conditionally safe for pregnant women.

Antihistamines: from dimedrol to erysus

The first generation of antihistamines, many allergy sufferers are obliged to improve their health."Side" drowsiness was perceived as a reality: but it does not flow from the nose and does not itch.Yes, the quality of life suffered, but what to do - a disease.The latest generation of antihistamines has enabled a large cohort of allergy sufferers to not only get rid of the allergy symptoms, but also to live a normal life: driving a car, playing sports, without risking "falling asleep".

4-generation antihistamines: myths and reality

Allergia Often, the term "anti-histamine drug of the new generation", "antihistamine drug of the fourth generation" slips in advertising of allergy treatment drugs.And this non-existent group is often considered not only the antiallergic drugs of the last generation, but also medicines under new trademarks relating to the second generation.This is nothing more than a marketing gimmick.In the official classification, only two groups of antihistamines are indicated: the first generation and the second.The third group is pharmacologically active metabolites, followed by the term "H1 histamine blockers of the third generation".

Clinical pharmacologist, doctor of the highest category Nazarova Marina Sergeevna


Treatment of allergy with folk remedies

Treatment of allergy with folk remedies

Allergic reaction of the body to any external or internal stimulus can appear at any age.This c...

Read More

Atopic dermatitis in children

Atopic dermatitis in children

Atopic dermatitis in children is a cutaneous, allergic disease that is caused by allergens, a...

Read More

Allergic vasculitis

Allergic vasculitis

Allergic vasculitis - pathological damage and inflammation of the blood vessels of the skin o...

Read More