Ilomedin is an antiaggregant. This is the concentrate needed to make the infusion solution.
Indications of ilomedine
Indicated for the elimination of such violations:
Buerger's disease, which appeared on the background of the critical degree of ischemia in the limbs, if there are no indications for revascularization;
severe degree obliterating endarteritis shape (especially if there is a possibility of amputation, and in addition, if it is impossible to perform angioplasty or operate vessels);
Reynaud's Syndrome in a hard form (leading to disability) which can not be treated with other drugs.
It is produced in ampoules (No. 5) with a volume of 1 ml.
Iloprost is an artificial analogue of prostacyclin. Its pharmacological properties:
inhibition of adhesion, aggregation, and in addition release of platelets;
expansion of venules with arterioles;
strengthening the capillary density, and at the same time strengthening the weakened walls of the vessels inside the microcirculatory system (with permeability provoked by such conductors as histamine or serotonin);
activation of the internal fibrinolysis process;
anti-inflammatory properties (slowing of adhesion of leukocytes in endothelial injuries, and in addition leukocyte accumulation inside damaged tissues and weakening of tumor necrosis release factor).
The equilibrium level within the plasma drug reaches 10-20 minutes from the beginning of the infusion. This indicator is linear depending on the speed of the infusion (if it is 3 ng / kg / min, then the concentration level of the substance will be approximately 135 ± 24 pg / ml). Upon completion of the infusion, the plasma index of the active component of the drug rapidly decreases (due to the increased intensity of its metabolism process).
The metabolic coefficient of plasma clearance is 20 ± 5 ml / kg / minute. The plasma half-life (terminal phase) is 30 minutes. As a result, after 2 hours after completion of the infusion, the medication will be less than 10% of the equilibrium level.
The drug can not interact with other drugs at the level of protein synthesis, since most of its active component is synthesized with plasma albumin (with protein synthesis is 60%), resulting in a very small amount of free iloprost. Along with this, the likelihood of exposure to iloprost on the processes of bioconversion of other drugs is extremely low (due to the ways of its metabolism and low absolute dosage).
The metabolism of the substance is carried out with the help of the b-oxidation process in the side carboxyl chain. Excretion of the unchanged component does not occur. The main product of decomposition is tetranor-iloprost, which falls into the urine (conjugated, as well as free form) under the guise of 4 diastereoisomers. This metabolite has no pharmacological activity (this has been shown by testing in animals). In vitro tests show that with inhalation or with / in the introduction, the metabolism of the substance inside the lungs is very similar.
In people with healthy renal and hepatic activity, the excretion of iloprost after the infusion procedure often occurs in 2 phases with half-lives of 3-5 or 15-30 minutes, respectively. At the same time, the total clearance of the component is about 20 ml / kg / minute, which demonstrates the presence of extrahepatic metabolic pathway of the substance.
With the participation of volunteers, testing was carried out to identify the mass fraction of the decay products (here, 3H-iloprost was used). After the infusion, the total radioactivity index was 81%, while in the stool with urine, respectively, 12% and 68% were detected. The decay products are excreted in the urine, and also from the plasma in a 2-phase way. In this case, the half-life in the 1-st phase is equal to about 2 hours, and in the second - about 5 hours. Of urine, the half-life lasts 2, and also 18 hours, respectively.
With reduced renal activity (terminal phase of kidney failure). Studies in people with this disorder, who also underwent periodic dialysis, show that after intravenous medications the clearance rate is much lower (on average 5 ± 2 ml / minute / kg) than the similar level in people with kidney failure, not who underwent periodic dialysis procedures (with an average of 18 ± 2 ml / minute / kg).
With decreased hepatic activity. Since most of the active substance of the drug passes the metabolism inside the liver, changes in its work affect the plasma values of drugs. Test results with the participation of 8 people with cirrhosis showed that the average level of clearance of the substance was 10 ml / minute / kg.
Use of ilomedine during pregnancy
The medicine is forbidden to be prescribed to pregnant and lactating women. There is no information on the use of drugs during pregnancy.
According to preclinical testing, it was found that the drug has a toxic effect on the fetus of the rat, although, at the same time, it does not affect fetal development in monkeys with rabbits.
Since there is no information about the possible risk of drug use of Ilomedin, women of childbearing age should use reliable contraception during the entire period of therapy with the use of drugs.
There is no information on the passage of the substance into the breast milk, but at the same time, as it passes in small amounts into rat milk, it is not recommended to use the medicine in breastfeeding.
Among the contraindications of drugs:
painful conditions during which, due to the influence of the drug on platelets, the risk of bleeding increases (for example, an active stage of an ulcer, a hemorrhage inside the skull, or trauma);
severe form of ischemic heart disease or unstable type of angina pectoris;
the myocardial infarction transferred in the last half a year;
acute or chronic stage of heart failure in stagnant form (grade 2-4 according to NYHA classification);
suspected development in mild stagnant phenomena;
intolerance to iloprost or other elements of the drug.
Today only a few cases of using drugs in adolescents and children are allowed.
Side effects of ilomedine
Often as a result of the use of drugs during clinical tests such side effects were observed: vomiting, flushing, rash, and nausea, and headaches. Basically they arose at an early stage in the process of titration of therapy for the selection of the optimal dosage for each patient. But these symptoms are usually soon after tapering.
The most severe adverse reactions to the use of drugs were cerebrovascular symptoms, pulmonary embolism, myocardial infarction, lowering blood pressure, heart failure. In addition, also developed asthma, tachycardia, pulmonary edema, angina, and besides there were convulsions or dyspnea.
Another category of unwanted manifestations associated with local reactions at the site of infusion administration. For example, you may experience pain and redness at the site of the procedure. Also, due to expansion of skin vessels at the infusion site erythema appeared occasionally (strip-shaped).
Among the side effects that have been observed in clinical testing and post-marketing observations in patients treated Ilomedinom:
lymph and blood formation system: occasionally developed thrombocytopenia;
organs of the immune system: rarely - intolerance reactions;
metabolic disorders: often decreased appetite;
mental disorders: often there is confusion or a sense of apathy, sometimes develop depression, anxiety, and hallucinations;
NA organs: often headaches often occur vertigo / dizziness, feeling of pulsation / paresthesia / hyperaesthesia; in rare cases - migraines, tremors, seizures, convulsions and loss of consciousness;
visual organs: rarely appears irritation or pain in the eye, and besides deteriorating visual acuity;
balance and hearing organs: single - vestibular disorders;
heart organ system: often develops bradi-, tachy or angina pectoris, heart failure is less common / arrhythmia and myocardial infarction;
cardiovascular system: often there are hot flashes, often raises blood pressure indicator or reduced blood pressure; rarely have cerebrovascular disease, pulmonary embolism, ischaemia golovnomozgovaya and DVT;
diseases of thoracic and mediastinal disorders, respiratory disorders: dyspnea appears frequently, rarely, pulmonary edema or asthma, in a few cases there is a cough;
Gastrointestinal organs: often nausea and vomiting, often also found abdominal pain or discomfort, diarrhea and in addition, in rare cases - dyspeptic symptoms, hemorrhagic form of diarrhea, bleeding from the anus, constipation, tenesmus and belching; sporadically - proctitis;
Digestive system: rarely jaundice;
subcutaneous tissue and skin: often increased sweating, rarely itching;
connective tissue, skeleton and musculature: often develop pain in the joints or muscles, and in addition pain in the jaw and lockjaw; rarely increases muscle tone, there are muscle cramps, tetany, and in addition to this;
Urinary system and kidneys: rarely - renal pain, painful spasms in the urinary organ, urine analysis shows the change in indicators of pathology of the urinary ducts and dysuria;
General disorders and local reactions: often develops a fever, there is heat, the temperature rises, there is pain, there is fatigue, chills, thirst, malaise, asthenia and in addition; also in the area of administration may develop infusion phlebitis, erythema or pain.
The medicine can cause angina, especially in individuals with coronary artery disease. It increases the likelihood of bleeding in people who are treated with the help of heparin, antiplatelet agents or anticoagulants coumarin.
Dosing and administration
Use of drugs is allowed only in conditions of constant monitoring of the patient (in a hospital or an outpatient institution that has the necessary equipment).
Women need to exclude the possibility of pregnancy before starting a therapeutic course.
Diluted medicine should be administered in the form of infusion for 6 hours (the way of administration - through the catheter inside the central vein or without it inside the peripheral vein) every day. The rate of infusion is determined by the individual sensitivity of the patient and is approximately 0.5-2 ng / kg / minute.
Infusion solution must be prepared every day, to ensure the sterility of the drug. The solvent and the substance contained in the ampoule must be thoroughly mixed.
It is required to detect heart rate indicators, and also the level of blood pressure before the start of the course, and then after each increase in the rate of infusion.
During the first 2-3 days, the drug is tolerated (therapy begins with the administration of drugs at a rate of 0.5 ng / kg / minute for half an hour). Further, the dosage gradually increases approximately every half hour by 0.5 ng / kg / minute until a rate of 2 ng / kg / minute is reached. A more accurate speed is selected, taking into account the weight of the person with the maximum tolerated dosage within 0.5-2 ng / kg / minute.
If a patient develops such negative reactions as lowering blood pressure, headaches or nausea, it is required to lower the rate of administration to a level that will be well tolerated by the patient. If severe side effects have occurred, you need to cancel the infusion. Later treatment is resumed (often the infusion lasts for 1 month) with the use of a dosage that has come to the person in the first 2-3 days, when choosing the speed of infusion.
As a result of overdose, hypotensive signs may appear, but in addition to the tides of blood to the skin of the face, headaches, vomiting, diarrhea and nausea. The level of blood pressure may increase, the pain in the back or legs may develop, and in addition tachycardia or bradycardia.
There are no specific antidotes. To eliminate the symptoms, it is necessary to cancel the infusion, monitor the patient's condition, and then treat the manifestations of an overdose.
Interactions with other drugs
Iloprost is able to increase the antihypertensive properties of blockers of the channels of Ca, β-adrenoblockers, as well as vasodilating drugs with ACE inhibitors. In a situation where the level of blood pressure has decreased very significantly, you can correct this violation by lowering the dose of Ilomedin.
Since the drug slows platelet aggregation, combined use with anticoagulants (for example, coumarin derivatives or heparin), and in addition other antiplatelet agents (among such NSAIDs, aspirin, PDE inhibitors or nitro-containing drugs that dilate blood vessels: for example, Molsidomine) is able to increase probability of bleeding. When such a reaction appears, it is necessary to cancel the infusion.
With premedication with aspirin (300 mg tablet), taken daily for 8 days, no effects on the pharmacokinetics of Ilomedin were found.
During the testing on animals, it was found that the drug can lower the equilibrium plasma level of plasminogen (tissue activator).
Data from clinical trials demonstrate that drug infusions do not affect the pharmacokinetics of digoxin (with repeated internal use of the latter), and in addition to the properties of plasminogen administered simultaneously with Ilomedin.
The vasodilating properties of iloprost increase with preliminary glucocorticoids (animal testing), but at the same time, changes in the level of antiaggregation are not observed. To clarify the clinical significance of the above-described information has not yet been possible.
Although clinical tests on this issue have not been carried out, according to in vitro tests that examined the retarding properties of iloprost against the enzyme activity of the hemoprotein P450 system, it was found that this component can not slow down the metabolism of drugs that are metabolized by these enzymes.
The medicine is recommended to be stored in a place where there is no access for young children. Temperature - no more than 30 ° С.
Ilomedin allowed to use for 5 years from the time of manufacture.
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To simplify the perception of information, this instruction for use of the drug "Ilomedin" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.
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