Index of drugs

In order to improve exercise capacity and reduce symptoms in adult patients with primary pulmonary hypertension, classified into functional class III according to the NYHA classification.

1 ml of solution contains 10 μg iloprost (as iloprost trometamol). Excipient: ethanol 96%, 0.81 mg / ml.

Platelet aggregation inhibitor, synthetic prostacyclin analogue. In researchin vitro the following pharmacological effects were observed: inhibition of platelet aggregation, platelet adhesion and release reactions; extension of arterioles and veins; increasing the density of capillaries and reducing the increased vascular permeability induced by mediators, such as serotonin or histamine in circulation in the smallest vessels; stimulation of endogenous potential fibrinolytic activity. After administration of iloprost in inhalation direct expansion of arterial pulmonary vasculature was observed with a simultaneous significant improvement in pulmonary artery pressure, decreased pulmonary vascular resistance, increased cardiac output and improved venation saturation of venous blood. Lung expansion after each inhalation is stabilized within 1-2 hours. There are no data available regarding the comparison of patients during acute haemodynamic response following intravenous administration with iloprost and after inhalation. The observed hemodynamic properties suggest an acute response with the preferential effect of inhalation treatment on lung vessels. When administering iloprost in inhalation to patients with pulmonary arterial hypertension (dose of iloprost in the mouthpiece: 5 μg, inhalation time 4.6-10.6 min), the highest concentration of drug in the blood serum occurred at the end of inhalation. The values ​​of these concentrations decrease with T_0,5 approximately 5 to 25 min. Within 30 minutes to 1 hour after completing inhalation, iloprost is not detectable in the central compartment.

Hypersensitivity to iloprost or to any of the excipients. Conditions in which the effect of the preparation on platelets may increase the risk of hemorrhage (eg active peptic ulcers, trauma, intracranial haemorrhage). Severe ischemic heart disease or unstable angina. Myocardial infarction over the last 6 months. Uncompensated heart failure uncontrolled by a doctor. Severe heart rhythm disturbances. Cerebrovascular disorders (eg transient cerebral ischemia, stroke) over the past 3 months. Pulmonary hypertension due to obliterative venous disease. Congenital or acquired valvular defects with clinically significant myocardial dysfunctions not associated with pulmonary hypertension.

It is not recommended for patients with unstable pulmonary hypertension with advanced right heart failure. In the event of worsening or worsening of right heart failure, treatment should be considered. When initiating the preparation, the blood pressure should be checked. Caution should be exercised when administering to patients with low blood pressure and patients with orthostatic hypotension or those receiving antihypertensive medications to prevent further hypotension. Do not start the treatment with patients with systolic blood pressure below 85 mmHg. Consider co-morbidities or concomitant medications that could increase the risk of hypotension and syncope. Patients who experience syncope due to pulmonary hypertension should avoid excessive exercise, for example during physical exercise. Physical inhalation may be beneficial before exercise. An increased occurrence of syncope may indicate therapeutic abnormalities, insufficient efficacy and / or severity of the disease. One should then consider adjusting and / or changing the therapy. Inhalation of the preparation may involve the risk of bronchospasm in patients with bronchial hypersensitivity. In addition, the benefits of the preparation in patients with co-morbid COPD and severe asthma have not been established.Patients with co-existing acute pulmonary infections, COPD and severe asthma should be closely monitored. If pulmonary edema symptoms occur during administration of iloprost in inhalation in patients with pulmonary hypertension, the possibility of pulmonary veno-occlusive disease should be considered. The drug should then be discontinued. Pulmonary vasodilators can significantly worsen cardiovascular status in patients with pulmonary veno-occlusive disease. If symptoms of pulmonary edema occur, it may indicate pulmonary veno-occlusive disease. In this situation, treatment with the preparation should be discontinued. If the treatment is discontinued, the risk of relapse is not excluded. After discontinuing therapy, the patient should be closely monitored and an alternative treatment option should be considered for seriously ill patients. In patients with impaired liver function and in patients with renal failure requiring dialysis, careful adjustment of the initial dose is recommended. It can not be ruled out that during a long-term treatment with the product there will be a slight increase in fasting blood glucose. To minimize the possibility of unintentional exposure to the drug, it is recommended to administer the product in inhalation using nebulizers with a drug release system released by the patient's inspiration (such as HaloLite / Prodose, I-Neb) and ensure adequate ventilation of the room. Newborns, infants and pregnant women should not be exposed to a dispersed medicine in the air. The preparation should not come into contact with the skin and eyes. Avoid ingestion of the oral solution. During the nebulization, the face mask must not be used and only the mouthpiece should be used. The product contains small amounts of ethanol (less than 100 mg / dose).

Taking into account the potential benefits for the mother, the use of the preparation during pregnancy may be considered in those women who decide to continue pregnancy despite the risk of pulmonary hypertension. It is not known whether iloprost / metabolites are excreted in human milk. A potential risk for a breastfed child can not be excluded and it is recommended to avoid breastfeeding during treatment with the preparation.

Very common: bleeding episodes (the risk may be increased in patients using platelet aggregation inhibitors or anticoagulants, fatal cases include cerebral and intracranial haemorrhage), headache, vasodilatation, flushing, chest discomfort or chest pain chest pain, cough, nausea, jaw / maxillofacial pain, peripheral edema. Common: dizziness, tachycardia, palpitations, fainting, hypotension, shortness of breath, sore throat and larynx, irritation of the throat, diarrhea, vomiting, irritation of the mouth and tongue (including pain), rash.

Preparation for inhalation from a nebulizer. Treatment with the product should only be started and monitored by a doctor who has experience in the treatment of pulmonary hypertension. Adults. When starting treatment, the first dose of iloprost given in inhalation should be 2.5 μg (administered through the mouthpiece of the nebulizer). In the case of good tolerability, the dose should be increased to 5 μg and maintain this dosage. In the case of a poor dose tolerance of 5 μg, this dose should be reduced to 2.5 μg. The dose for one inhalation should be given 6-9 times a day, according to individual needs and patient tolerance. The duration of treatment depends on the clinical condition of the patient and the doctor's assessment. In case of deterioration of patients' health while using this treatment, intravenous prostacyclin treatment should be considered. In patients with impaired hepatic function, to avoid undue accumulation of the drug during the day, special care should be taken during the initial dose adjustment. Initially, a dose of 2.5 μg should be administered, taking a 3-4-hour break between successive applications of the drug (this corresponds to a maximum of 6 times a day). Thereafter, dosing intervals may be carefully shortened based on individual patient tolerance. If a dose of up to 5 μg is indicated, 3-4-hour intervals should be used again, and then shortened depending on the patient's individual tolerability. Accumulation of iloprost following a few-day treatment is unlikely due to night interruptions in drug administration. No dose adjustment is required in patients with renal impairment with a creatinine clearance> 30 ml / min.Patients with creatinine clearance ≤ 30 ml / min were not evaluated in clinical trials. Elimination of iloprost is slowed in patients with renal failure requiring dialysis - the same dosing recommendations should be used as in patients with hepatic impairment. The preparation is administered using a suitable inhaler (nebulizer): HaloLite and Prodose - at a dose in the mouthpiece 2.5 μg - estimated inhalation time (15 breaths / min) - 4-5 min; Venta-Neb - at the dose in the mouthpiece 2.5 μg - estimated time of inhalation - 4 min; I-Neb AAD - at a dose in the mouthpiece 2.5 μg - estimated time of inhalation - 3.2 min. Patients treated with one type of nebulizer should not change the type without the supervision of the attending physician.