Iloprost (Iloprostum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Antiaggregants

Included in the formulation
  • Ventavis
    solution d / inhal. 
    Bayer Pharma AG     Germany
  • Ilomedin®
    concentrate d / infusion 
    Bayer Pharma AG     Germany
    • АТХ:

    B.01.A.C.11   Iloprost

    Pharmacodynamics:

    Dose-dependent, inhibits platelet aggregation and releases some platelet factors, prolongs bleeding time.

    As a result of inhibition of ADP-dependent binding of fibrinogen to platelet membranes inhibits their aggregation. Does not inhibit cyclooxygenase. It causes dilatation of arterioles and venules, reduces the increased vascular permeability, activates fibrinolysis, suppresses adhesion and migration of leukocytes after endothelial damage, reduces the formation of free oxygen radicals.

    Pharmacokinetics:

    After intravenous administration, the maximum concentration in the blood plasma is reached after 10-15 minutes. The connection with plasma proteins is 60%.

    Therapeutic effect develops after the reception. Metabolism in the liver by β-oxidation of the side carboxyl chain and the formation of an inactive metabolite of tetranoriloprost.

    Half-life is 1-2 hours. Elimination by the kidneys.

    Indications:

    It is used to treat obliterating thromboangiitis, obliterating endarteritis, diabetic angiopathies, with Reynaud's syndrome.

    ICD-10

    IX.I70-I79.I73.0   Raynaud's syndrome

    IX.I70-I79.I73.1   Obliterating thromboangitis [Berger's disease]

    IX.I70-I79.I73.9   Peripheral vascular disease, unspecified

    IX.I70-I79.I79.2 *   Peripheral angiopathy in diseases classified elsewhere

    Contraindications:

    Severe ischemic heart disease, peptic ulcer of the stomach or duodenum, hemorrhagic stroke, severe arrhythmia, heart failure, individual intolerance, children under 18 years.

    Carefully:

    Dysfunction of the liver, renal failure, surgical intervention, trauma and other pathological conditions with the risk of bleeding.

    Pregnancy and lactation:

    Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Intravenously drip daily, for 6 hours.

    When inhaled in the appropriate dosage form, a single dose is 2.5-5 μg.

    The highest daily dose: 1 g.

    The highest single dose: 250 mg.

    Side effects:

    Central and peripheral nervous system: asthenia, dizziness, headache, tinnitus, inhibition, drowsiness, depression, hallucinations.

    The system of hematopoiesis: leukopenia, bone marrow aplasia, pancytopenia, thrombocytopenia, aplastic anemia, rarely - thrombocytopenic purpura.

    Respiratory system: relatively often - bronchial asthma, rarely - cough.

    The cardiovascular system: Arterial hypotension, bradycardia, hot flushes and sensation of fever, arrhythmia, myocardial ischemia, myocardial infarction, deep vein thrombosis, pulmonary embolism, single cases (in elderly patients with severe atherosclerosis) - pulmonary edema.

    Digestive system: anorexia, nausea, vomiting, diarrhea, discomfort and abdominal pain, change in taste, dry mouth, constipation, tenesmus, regurgitation, dysphagia, diarrhea, rectal bleeding, melena, rarely - jaundice.

    Musculoskeletal system: arthralgia, myalgia, pain in the masticatory muscles, trismus, muscle weakness, rarely - tetany, jerking muscle hypertonicity.

    Dermatological reactions: polymorphous skin rashes, rarely - erythema multiforme.

    Urinary system: pain in the lower back, renal colic, dysuria, changes in the cellular composition of urine.

    Allergic reactions.

    Overdose:

    Severe headache, marked blood flow to the face, pain in the legs and back, hyperhidrosis, vomiting, diarrhea, bradycardia or tachycardia.

    Treatment is symptomatic, after cessation of infusion.

    Interaction:

    Increases the hypotensive effect of blockers of β-adrenoreceptors, vasodilators, calcium antagonists, ACE inhibitors.

    Antiaggregant effect is strengthened by other inhibitors of platelet aggregation: acetylsalicylic acid and other non-steroidal anti-inflammatory drugs, inhibitors phosphodiesterase, molsidomine and nitrates.

    Special instructions:

    Iloprost is used only in conditions of careful monitoring. Before starting treatment, women should be excluded from pregnancy.

    Constant infusion over several days is not recommended because of the possibility of developing tachyphylaxis, manifested in a weakened effect on platelets and the possibility of a "rebound" syndrome, manifested in an increase in the propensity to aggregate platelets at the conclusion of the course of therapy.

    Patients receiving iloprost treatment are prohibited from driving and working with moving mechanisms.

    Instructions
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