Yloprost | Ilomedin concentrate d / prig. solution for infusion 20 Ојg / ml 1 ml ampoules 5 pcs.

Release form

Concentrate for the preparation of a solution for infusion.

Packing

5 ampoules of 1 ml.

Pharmacological action of

Iloprost is a synthetic analogue of prostacyclin, inhibits platelet aggregation, adhesion and reaction, dilates arterioles and venules, increases capillary density (restores impaired microcirculation by inducing vasodation, inhibiting platelet activation, restoring platelets, activation of endogenous fibrinolysis and correction of imbalance in the cytokine system) and reduces the increased vascular permeability due to mediators, such as serotonin or histamine, activates endogenous fibrinolysis in the microcirculation system and exerts an anti-inflammatory effect: it inhibits the adhesion and migration of leukocytes after damage to the endothelium, as well as tissue, reduces the production of tumor necrosis factor (TNF alpha).

Indications

thromboangiitis obliterans (Buerger's disease) in the later stages with critical limb ischemia in the absence of indications for

revascularization, severe peripheral arterial occlusion disease, especially in cases of risk of amputation and the impossibility of vascular surgery or angioplasty

severe Raynaud's syndrome, leading to disability, not amenable to therapy with other drugs.

Contraindications

pathological changes in the blood picture of unclear genesis

gastric ulcer and duodenal ulcer disease lactation period (breast-feeding should be abandoned)

children and adolescents under 12 years of age (i / m administration, supp.)

children d about 6 years (tablets, ointment)

hypersensitivity to acetylsalicylic acid or other NSAIDs (including intracranial bleeding)

severe coronary heart disease or unstable angina pectoris myocardial infarction in the last 6 months acute heart failure or chronic congestive heart failure stage II — IV (according to the New York Heart Association) severe heart rhythm disturbances

suspected congestive pulmonary circulation

lactation period

pregnancy

hypersensitivity to iloprost or other components of the drug

by road: in patients with cerebrovascular accident over the past 3 months (e.g. transient ischemic disorder, stroke). Such patients need a thorough assessment of the ratio of benefit and risk of treatment.

With renal failure requiring dialysis, and with cirrhosis, the excretion of iloprost is reduced.

It is necessary to take measures against a further decrease in blood pressure in patients with initially (prior to the initiation of Ilomedin therapy) low blood pressure, patients with severe heart disease should be closely monitored.

The possibility of developing orthostatic hypotension during the transition of patients from horizontal to vertical after the end of Ilomedin administration should be taken into account.

Special instructions

In the hope of the success of conservative iloprost therapy, surgery should not be postponed for patients requiring emergency leg amputation (for example, with infected gas gangrene).

Patients should be strongly advised to stop smoking.

Accidental injection of undiluted Ilomedin solution into nearby tissues can lead to their local change at the injection site (redness, pain, itching, feeling hot).

Avoid taking the drug inside and getting it on the mucous membranes. Once in the skin, iloprost can lead to prolonged, albeit painless, erythema. Therefore, care must be taken to avoid contact with the skin. If iloprost gets on any part of the skin, it should be immediately washed with plenty of water or saline sodium chloride.

Composition

1 ml contains iloprost trometamol 27 Ојg, which corresponds to 20 Ојg.

Dosage and administration of

IV, in the form of infusions, daily as a 6-hour infusion into a peripheral vein or a catheter installed in a central vein. The rate of administration (dose) depends on individual tolerance and is 0.5-2 ng / kg / min. During the first 2-3 days, individual tolerance of the drug is determined under the control of heart rate and blood pressure (should be determined at the beginning of the infusion and after each increase in dose): treatment is started at a rate of administration of 0.5 ng / kg / min for 30 minutes, then the dose is increased stepwise by 0.5 ng / kg / min every 30 minutes The exact rate of infusion is calculated based on their body weight and maximum tolerated dose, within 0.5-2 ng / kg / min. Determination of the infusion rate (ml / h) when using an infusion pump (for example Infusomat): the contents of the ampoule are dissolved in sterile 0.9% NaCl solution or 5% dextrose solution and the final volume of the solution is adjusted for the contents of the ampoule (2.5 ml) 50 ?g to 250 ml, for an ampoule (1 ml) 20 ?g - up to 100 ml. A solution is obtained at a concentration of 0.2 ?g / ml, its infusion rate is determined in accordance with the dose and body weight (within 0.5-2 ng / kg / min) scheme: with a body weight of 40 kg and a dose of 0.5 ng / kg / min infusion - 6 ml / h, 1 ng / kg / min - 12 ml / h, 1.5 ng / ml / min - 18 ml / h, 2 ng / ml / min - 24 ml / h with a body weight of 50 kg and a dose of .5 ng / kg / min - 7.5 ml / h, 1 ng / kg / min - 15 ml / h, 1.5 ng / kg / min - 22.5 ml / h, 2 ng / kg / min - 30 ml / h body 60 kg and a dose of 0.5 ng / kg / min - 9 ml / h, 1 ng / kg / min - 18 ml / h, 1. 5 ng / kg / min - 27 ml / h, 2 ng / kg / min - 36 ml / h with a body weight of 70 kg and a dose of 0.5 ng / kg / min - 10.5 ml / h, 1 ng / kg / min - 21 ml / h, 1.5 ng / kg / min - 31.5 ml / h, 2 ng / kg / min - 42 ml / h with a body weight of 80 kg and a dose of 0.5 ng / kg / min - 12 ml / h, 1 ng / kg / min - 24 ml / h, 1.5 ng / kg / min - 36 ml / h, 2 ng / kg / min - 48 ml / h with a body weight of 90 kg and a dose of 0.5 ng / kg / min - 13.5 ml / h, 1 ng / kg / min - 27 ml / h, 1.5 ng / kg / min - 40.5 ml / h, 2 ng / kg / min - 54 ml / h with a body weight of 100 kg and a dose of 0.5 ng / kg / min - 16 ml / h, 1 ng / kg / min - 30 ml / h, 1.5 ng / kg / min 45 ml / h, 2 ng / kg / min - 60 ml / h with a body weight of 110 kg and a dose of 0.5 ng / kg / min - 16.5 ml / h, 1 ng / kg / min - 33 ml / h, 1.5 ng / kg / min - 49.5 ml / h, 2 ng / kg / min - 66 ml / h. Determination of infusion rate (ml / h) using an automatic syringe (e.g. Perfusor): the contents of the ampoules are diluted in sterile 0. A 9% NaCl solution or 5% dextrose solution and the final volume of the solution are adjusted for the contents of the ampoule (2.5 ml) 50 ?g to 25 ml, for the ampoule (1 ml) 20 ?g to 10 ml. A solution is obtained at a concentration of 2 ?g / ml, its infusion rate is determined in accordance with the dose and body weight dependence scheme (within 0.5-2.0 ng / kg / min): at a body weight of 40 kg and a dose of 0.5 ng / kg / min infusion - 0.6 ml / h, 1 ng / kg / min - 1.2 ml / h, 1.5 ng / kg / min - 1.8 ml / h, 2 ng / kg / min - 2.4 ml / h with a body weight of 50 kg and a dose of 0.5 ng / kg / min - 0.75 ml / h, 1.5 ng / kg / min - 1.5 ml / h, 1.5 ng / kg / min - 2.25 ml / h, 2 ng / kg / min - 3 ml / h with a body weight of 60 kg and a dose of 0.5 ng / kg / min - 0.9 ml / h, 1 ng / kg / min - 1.8 ml / h, 1.5 ng / kg / min - 2.7 ml / h, 2 ng / kg / min - 3.6 ml / h with a body weight of 70 kg and a dose of 0.5 ng / kg / min - 1.05 ml / min, 1 ng / kg / min - 2.1 ml / 1.5 ng / kg / min - 3.15 ml / hr of 2 ng / kg / min - 4. 2 ml / h with a body weight of 80 kg and a dose of 0.5 ng / kg / min - 1.2 ml / h, 1 ng / kg / min - 2.4 ml / h, 1.5 ng / kg / min - 3.6 ml / h, 2 ng / kg / min - 4.8 ml / h with a body weight of 90 kg and a dose of 0.5 ng / kg / min - 1.35 ml / h, 1 ng / kg / min - 2.7 ml / h, 1.5 ng / kg / min - 4.05 ml / h , 2 ng / kg / min - 5.4 ml / h with a body weight of 100 kg and a dose of 0.5 ng / kg / min - 1.5 ml / h, 1 ng / kg / min - 3 ml / h, 1.5 ng / kg / min - 1.5 ml / h, 2 ng / kg / min - 6 ml / h with a body weight of 110 kg and a dose of 0.5 ng / kg / min - 1.65 ml / h, 1 ng / kg / min - 3.3 ml / h, 1.5 ng / kg / min - 4.95 ml / h, 2 ng / kg / min - 6.6 ml / h. The duration of treatment is up to 4 weeks. In patients with Raynaud's syndrome, shorter courses of treatment - 3-5 days are often enough to achieve a short remission (several weeks). In case of side effects such as headache, nausea or decreased blood pressure, infusion rate should be reduced to the maximum tolerated. With the development of severe side effects, the infusion must be interrupted. Treatment is usually resumed after 4 weeks in doses that the patient tolerated well in the first 2-3 days of the previous course of treatment. With renal failure requiring dialysis, and with cirrhosis of the liver, the recommended dose is reduced by 2 times.

Side effects of

From the nervous system and sensory organs: often (more than 1%, but less than 10%) - dizziness, headache, paresthesia, hyperesthesia, tinnitus, anxiety, agitation, lethargy, apathy, drowsiness less often ( more than 0.1%, but less than 1%) - tremors, cerebrovascular disorders, depression, hallucinations, migraines, fainting, prolonged loss of consciousness, impaired vision, irritation and pain in the eyes rarely (more than 0.01%, but less than 0.1%) - vestibular violations frequency unknown - confusion consciousness. From the CCC: often (more than 1%, but less than 10%) - decreased blood pressure, bradycardia, flushing of the skin and a sensation of heat less often (more than 0.1%, but less than 1%) - arrhythmia (including extrasystole) myocardial ischemia myocardial infarction, deep vein thrombosis, pulmonary embolism, frequency is unknown - increased blood pressure, tachycardia in isolated cases (in elderly patients with severe atherosclerosis) - pulmonary edema. From the respiratory system: less often (more than 0.1%, but less than 1%) - rarely bronchial asthma (more than 0.01%, but less than 0.1%) - cough in isolated cases (in elderly patients with severe atherosclerosis) - heart failure. From the digestive system: more often (more than 10%) - nausea, vomiting often (more than 1%, but less than 10%) - anorexia, diarrhea, abdominal discomfort, abdominal pain less often (more than 0.1%, but less than 1%) - dry mouth, taste change, tenesmus, constipation, belching, dysphagia, diarrhea, melena, rectal bleeding, jaundice. From the musculoskeletal system: often (more than 1%, but less than 10%) - pain in the masticatory muscles, trismus, myalgia, arthralgia, muscle weakness less often (more than 0.1%, but less than 1%) - tetany, convulsive muscle twitching, hypertonicity. From the urinary system: lower back pain, renal colic, changes in the cellular composition of urine, dysuria. Local reactions: often (more than 1%, but less than 10%) - flushing of the skin, pain, phlebitis at the injection site. Other: more often (more than 10%) - sweating often (more than 1%, but less than 10%) - local pain, generalized pain, hyperthermia, skin itching, fatigue, thirst frequency is unknown - allergic reactions.

Drug interactions

Due to possible interactions, Ilomedin should not be mixed with other medicines in the same solution.

Iloprost enhances the antihypertensive effect of? -adrenoblockers, slow calcium channel blockers and all vasodilators, as well as ACE inhibitors. If significant arterial hypotension occurs, blood pressure can be corrected by reducing the dose of iloprost.

Since iloprost inhibits platelet function, its use in combination with heparin or indirect anticoagulants (coumarin derivatives) or other platelet aggregation inhibitors (acetylsalicylic acid, NSAIDs, phosphodiesterase inhibitors and nitrates, for example, for example molsidomine), may increase the risk of bleeding. In this case, the infusion of Ilomedin should be discontinued. The use of acetylsalicylic acid in a dose of up to 300 mg / course of 8 days, prior to the use of Ilomedin, had no effect on the pharmacokinetics of iloprost.

In an animal study, it was found that iloprost can cause a decrease in the equilibrium concentration of tissue plasminogen activator (TAP) preparations in plasma. The results of studies in humans show that iloprost infusions do not affect the pharmacokinetics of multiple oral doses of digoxin in patients, and that when used simultaneously with TAP, iloprost does not affect its pharmacokinetics.

In animal experiments, the vasodilating effect of iloprost weakened, if the experimental animals previously received glucocorticosteroids, however, the inhibitory effect on platelet aggregation did not change. The value of this data for the clinic has not yet been established.

Although no clinical studies have been conducted, in vitro studies that examined the inhibitory potential of iloprost in relation to the activity of enzymes of the cytochrome P450 system revealed that a significant suppression of drug metabolism by these enzymes as a result of exposure to iloprost is unlikely.

Overdose

Symptoms: possibly a decrease or increase in blood pressure, as well as headache, blood flow to the face, nausea, vomiting and diarrhea, bradycardia or tachycardia, pain in the legs or back.

Treatment: recommended interruption of infusion, further monitoring of patients and symptomatic therapy. Specific antidotes are unknown.

Storage Conditions

Keep out of the reach and sight of children at temperatures not exceeding 30 РC.

The active substance

Iloprost

Berlimed SA, Germany