Ipratropium-aeronativ

General characteristics. Structure:

Active ingredient: 0,021 mg of an ipratropiya of bromide of monohydrate (in terms of 0,02 mg of an ipratropiya of bromide).

Excipients: ethanol (the alcohol absolutized), citric acid monohydrate, triethyl citrate, R 134a propellant (1,1,1,2-tetraftoretan).

Ipratropium-aeronativ is bronkhodilatiruyushchy means.

Pharmacological properties:

Pharmacodynamics. Blocks M-holinoretseptory smooth muscles of a tracheobronchial tree (preferential at the level of large and average bronchial tubes) and suppresses a reflex bronkhokonstriktion. Having structural similarity to acetylcholine molecule, is his competitive antagonist. Effectively prevents the narrowing of bronchial tubes resulting from inhalation of cigarette smoke, cold air, effect of various bronkhospazmiruyushchy substances and also the spasm of bronchial tubes connected with influence of a vagus nerve oppresses. At inhalation use has practically no resorptive effect - development of tachycardia requires inhalation about 500 doses, at the same time only 10% reach small bronchial tubes and alveoluses, and the rest settles in a throat or an oral cavity and is swallowed.

At patients with the bronchospasm connected with chronic obstructive diseases of lungs (chronic bronchitis and emphysema of lungs) improves indicators of function of external respiration: the volume of the forced exhalation for the first second (OFV1) and the maximum sredneekspiratorny flow (% FEF25-75) increases by 15% and more in 15 minutes after administration of drug, the maximum effect is noted in 1-2 hours, and proceeds at most of patients till 6 o'clock.

At patients with bronchial asthma considerable improvement of function of external respiration is noted at 40% of patients (OFV1 increased by 15% and more).
 
Pharmacokinetics. Absorption. At inhalation introduction for an ipratropiya of bromide low absorption from a mucous membrane of respiratory tracts is characteristic. In a GIT it is practically not absorbed. System bioavailability at an inhalation way of introduction low — about 7% in this connection system anticholinergic effects are poorly expressed. Action develops in 5 min. after inhalation and reaches a maximum in 30–60 min. Action duration after inhalation — to 8 h.

Distribution. Less than 20% an ipratropiya of the bromide which came to a system blood stream contact proteins of a blood plasma. It is badly dissolved in fats and poorly gets through biological membranes. Does not get through GEB. Does not kumulirut.

Metabolism. It is metabolized in a liver about education 8 pharmacological of the inactive and poorly active metabolites possessing anticholinergic action.

Removal. At inhalation introduction an ipratropiya bromide is removed preferential through intestines. About 25% of the entered dose are removed in not changed look, other part - in the form of metabolites. A part of metabolites is also removed by kidneys. An elimination half-life — 3–4 h.

Indications to use:

- chronic obstructive pulmonary disease;
- chronic bronchitis;
- emphysema of lungs;
- bronchial asthma (easy and moderate severity), especially with associated diseases of cardiovascular system.

Route of administration and doses:

The drug "Ipratropium-aeronativ" is intended only for inhalation introduction. The mode of dosing is selected individually. If the doctor it is not appointed differently, for adults and children 6 years are more senior the following mode of dosing is recommended: 2 inhalation doses (40 mkg) 4 times a day.

The need for increase in a dose can testify to need of review of the main treatment. The general daily dose should not exceed 12 inhalations (240 mkg) a day.

If inhalations are insufficiently effective, or the condition of the patient worsened, it is necessary to see a doctor for change of treatment planning. In case of sudden developing and bystry progressing of a short wind it is necessary to see a doctor immediately.

Children are younger than 6 years: because information on use of drug in this age group is limited, use of the following dose is recommended (only on condition of medical observation): 1 inhalation dose (20 mkg) 3 times a day.

Instruction for performing inhalations. Ipratropium-aeronativ it is intended only for inhalation use.

Before the first use of an inhaler or if did not use an inhaler week and longer check its work. For this purpose remove a protective cap from an inhaler mouthpiece, well stir up an inhaler and press a cylinder, releasing one stream of drug in air.

Performing inhalation:
Step 1. Remove a protective cap from an inhaler mouthpiece, as shown in the figure 1.

Step 2. Vigorously shake an inhaler.
Step 3. To make a slow, full exhalation.
Step 4. Holding a cylinder as shown in the figure 2, to densely clasp with lips a mouthpiece. The cylinder has to be directed by a bottom up (figure 2).

Step 5. Expedite the deepest breath, at the same time press a cylinder bottom before release of one inhalation dose.
Step 6. For several seconds hold the breath, then take out a mouthpiece from a mouth and slowly exhale through a nose.
Step 7. To put on a protective cap an inhaler mouthpiece. Repeat steps 3-6 for receiving the second inhalation dose if it is necessary.

Cleaning of an inhaler. Regularly (weekly) it is necessary to clear an inhaler mouthpiece, as shown in the figure 3.

 

Take out a metal barrel from a plastic case and rinse a case and a cap warm water. Do not use hot water. Carefully dry up, but do not use for this purpose heating devices. Place a barrel back in a case and put on a cap. Do not dip a metal barrel into water.

PREVENTION: the plastic mouthpiece is developed for a mouth especially for Ipratropium-aeronativ and serves for an exact drug dosing. The mouthpiece should not be used with other dosed aerosols. Also it is impossible to use Ipratropium-aeronativ with any other adapters, except the mouthpiece delivered together with drug.

Contents of a cylinder are under pressure. The cylinder cannot be opened and subjected to heating above 50 °C.

Features of use:

Use at pregnancy and during breastfeeding. Safety of use of Ipratropiuma-aeronativ at pregnancy at the person is not established. Use of drug in the I trimester of pregnancy is contraindicated. Purpose of drug in II and III trimesters of pregnancy is possible only if the estimated advantage of therapy for mother exceeds possible risk for a fruit. In preclinical trials embriotoksichesky and teratogenic effect of drug at inhalation and intranasal appointment in the doses considerably exceeding the recommended therapeutic dose for the person was not revealed. Data on allocation of Ipratropium-aeronativ with breast milk are absent. Though insoluble quarternary cations in lipids get into breast milk, it is improbable that Ipratropium-aeronativ will have significant effect at inhalation use. However as many drugs are removed with breast milk, it is necessary to appoint with care Ipratropium-aeronativ in the period of a lactation (breastfeeding), only if the potential advantage for mother exceeds possible risk for the child.

It is not recommended to appoint drug for the emergency stopping of an attack of bronchial asthma (since the broncholitic effect develops later, than at β-adrenomimetik).

At patients with a mucoviscidosis the risk of development of disturbances of motility of a GIT is increased.

Patients have to be able to use correctly Ipratropium-aeronativ an aerosol for inhalations dosed. The patient should be informed that if inhalations are insufficiently effective or there was an aggravation of symptoms, it is necessary to see a doctor for change of treatment planning. In case of sudden developing and bystry progressing of a short wind the patient also has to see a doctor immediately.

In case of any symptom of an attack of closed-angle glaucoma (eye pain, discomfort, indistinct sight, emergence of an aura and color spots before eyes in combination with a conjunctival and corneal hyperemia) it is necessary to appoint the drops causing narrowing of a pupil and to address immediately the ophthalmologist.

Influence on ability to driving and other vehicles, for work with moving mechanisms. Researches on studying of influence of drug on ability to driving of motor transport and control of mechanisms were not conducted. In cases of development of side effects at use of drug it is necessary to refrain from driving of motor transport and control of mechanisms.

Side effects:

Determination of frequency: very often (> 1/10), it is frequent (from 1/100 to 1/10), infrequently (from 1/1000 to 1/100), is rare (from 1/10000 to 1/1000), is very rare (<1/10000).

Allergic reactions: infrequently - skin rash, an itch, a Quincke's disease of language, lips and the person, a small tortoiseshell, a laryngospasm, a bronchospasm, an exudative mnogoformny erythema, anaphylactic reactions.

The effects connected with anticholinergic effect of drug: seldom - supraventricular tachycardia, a cardiopalmus, accommodation disturbance, reduction of secretion of sweat glands, disturbance of motility of the digestive tract (DT), a lock, an ischuria (these effects have reversible character). At patients with obstructive damage of urinary tract the risk of development of an ischuria increases.

From a nervous system: very often - a headache.

From the alimentary system: very often - nausea, it is frequent - dryness in a mouth, is rare - diarrhea, an abdominal pain, vomiting.

From respiratory system: infrequently - cough; seldom - a paradoxical bronchospasm.

From organs of sight: very seldom - at hit in eyes of an aerosol the mydriasis (mydriasis), increase in intraocular pressure (especially at patients with closed-angle glaucoma), closed-angle glaucoma, eye pain are observed. Eye pain or a sensation of discomfort, indistinct sight, emergence of an aura and color spots before eyes in combination with a conjunctival and corneal hyperemia can be symptoms of an attack of closed-angle glaucoma.

Others: very often - increase in viscosity of a phlegm.

Interaction with other medicines:

At simultaneous use β2-адреномиметики and derivatives of xanthine exponentiate bronkhodilatiruyushchy effect of drug.

The anticholinergic effect amplifies protivoparkinsonichesky means, quinidine, tricyclic antidepressants. At simultaneous use with other anticholinergics the additive action is noted.

Contraindications:

- hypersensitivity to atropine and its derivatives;
- hypersensitivity to an ipratropiya to bromide or to other components of drug;
- pregnancy (I trimester).
 
With care closed-angle glaucoma, obstruction of urinary tract, a prostate hyperplasia, II and the III trimester of pregnancy, breastfeeding, children's age (up to 6 years).

Overdose:

Symptoms: specific symptoms of overdose are not revealed. Considering the width of therapeutic action and a local route of administration of Ipratropiuma-aeronativ, emergence of any serious anticholinergic symptoms is improbable. Insignificant manifestations of systemic anticholinergic action, such as dryness in a mouth, accommodation disturbances, increase in heart rate are possible.

Treatment: performing symptomatic therapy.

Storage conditions:

Aerosol for inhalations dosed, 20 mkg / a dose. On 200 doses of drug in a cylinder from stainless steel with the valve of the dosing action and a raspylitelny nozzle. Each cylinder together with the application instruction in a cardboard pack.

Issue conditions:

According to the recipe

Packaging:

In the place protected from light at a temperature not above 25 °C, far from heating devices. Not to freeze. To store in the place, unavailable to children. A period of validity - 2 years. Not to apply after the period of validity specified on packaging.