clinical pharmacology of medicines influencing on hemostasia

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$tema lektsii: kardiotonicheskie sredstva (ks) clinical pharmacology of medicines, influencing on hemostasia classification of medicines influencing on hemostasia i. direct anticoagulants: 1. dependant from antythrombinum iii a) usual unfractionated heparin b) low molecular weight heparin: - enoxaparin (clexane) - nadroparin (fraxiparin) - daltepparin (fragmin) - reviparin (clivarin) - tinzaparin (logiparin) 2. independent of an antithrombin iii a) hirudin, girugen ii. indirect anticoagulants: 1. coumarin derivatives: - warfarin (coumadin) - bishydroxicoumarol (dicumarin) – ethylbiscumacetate (neodicumarun, pelentan) - acenocoumarol (syncumar) 2. derivatives of an indandion. - phenyndion (phenylin) - omephyn iii. thrombolitics (fibrinolytics): 1. activated in vitro plasminogen - fibrinolysine 2. endogenic plasminogen activators a) first generation - streptokinase - streptodecase - urokinase b) second generation - recombinant prourokinase - recombinant tissue-type plasminogen activator (alteplase) v) third generation - reteplase - tenecteplase iv. antiaggregants: 1. cox 1 ingibitors – acetylsalicylic acid (thrombo ass, thrombopol, cardiomagnyl) 2. phosphodiesterase ingibitors – pentoxyphyllin (trental, agapurin) …$

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transition of prothrombin to the thrombin, reduces aggregation of thrombocyts and moderately increases fibrinolitic properties of a blood. at bond with a heparin the antithrombin-3 activity increases to 700 times. activated antithrombin-3 supresses serinproteases to which xii a, xia, xa, viia, iia coagulation factors belong. other effects of heparin: - antiatherosclerotic - analgesic - anti-inflammatory - antiallergic - diuretic - immunosuppressive - hypoglycemic - potassium-sparing main indications to heparin prescription acute pulmonary embolism acute myocardial infarction instable stenocardia lower extremity deep venous thrombosis balloon coronary angioplasty cerebral circulation transient attack other arterial or venous thrombosis contraindications: acute internal hemorrhage (gastrointestinal tract or urinary tracts) hemorrhagic stroke (or if was in the anamnesis) brain and spinal injury or surgery arterial hypertension (abp higher than 180/120) inducted by heparin thrombocytopenia suspicion on aorta dissecting aneurysm or acute pancreatitis heparin’s side effects bleeding thrombocytopenia transaminase activity increasing allergic reaction withdrawal syndrome osteoporosis, alopecia, …

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prevents formation of 50 un of thrombin. 2. action duration (1-2 times per day). 3. high (90%) bioavailability. at heparin -15-20%. 4. low communication with plasma proteins (activity remains at small doses) 5. low frequency of thrombocytopenia and hemorrhagic complications 6. lack of daily control indications to lmwh prescription: ami, instable stenocardia, pulmonary embolism. prophylaxis and treatment of venous and arterial thrombosis. initial stage of dic syndrome at patients with heart valves prostheses side effects of lmwh and contraindications the same as at heparin. are prescribed to kg/weight. 0,1 ml on 10 kg of weight. indirect anticoagulums break the formation in hepar of k-vitamin’s active form, necessary for synthesis of prothrombin precursors and other coagulation factors (vii, ix, x). they are competitive antagonists of k-vitamin indications: - 1. primary prophylaxis of thrombosis of lower extremities deep veins and thromboembolism at patients with continued ciliary arrhythmia, congestive snf, left ventricular thrombus. …

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t often causes bleedings, often an allerg. reac. up to anaphylactic shock. and at its repeated introduction the efficiency of preparation decreases due to blocking the preparation by antibodies. streptodecase: it it is long circulates in a blood, having long thrombolitic action urokinase – received from the culture of human renal tissue cells, is deprived of allergenic properties, but causes frequent bleedings alteplase – works mainly in thrombus and less often causes allergy. reactions and bleedings. indications: acs, pulmonary embolism. contraindications: continuing bleeding, recent bleeding, brain tumor, the first 3 months after hemorrhagic stroke, hemorrhagic diathesis, aorta dissecting aneurysm. safe control: thrombine time (enlarged twice) thromboplastin time (enlarged by 1,5- 2 times) fibrinogen (concentration decreases by 2-3 times) at overdosage: aprotinin – inhibitor proteinase plasmai. e-aminocapronic acid. aprotinin (kontrikalum, gordox) – suppresses the activity of blood plasma proteinas (tripsin, plasmin, kallikrein), thats lead to depression of activity of hageman's factor …

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t remains during 5-7 days). high doses suppress the formation of prostacyclin. prescribe in a dose of 75-375 mg/day. side effects: irritant action at gastrointestinal tract bleeding at ud allergic reactions up to anaphylactic shock bronchiospasm at p-s with aspirin ba. seldom thrombocytopenia , agranulocytosis 2. phosphodiesterase inhibitors: trental, agapurin) – blocks a phosphodiesterase in thrombocytes, enlarges in them concentration of camp, thats lead to inhibition of thrombocytes and erythrocytes aggregation. and also improves blood microcirculation. moderately strengthens blood flow in kidneys, thats lead to insignificant augmentation of diuresis and natriuresis improves a circulation in extremities and cns. slightly dilates the coronary vessels. the dose is 600-1200 mg/day or i.v. side effects: - dyspepsic disorders high doses can lead to bleedings at i.v. delicacy, giddiness, baresthesia and flash to heard integument hyperemia . 3. adenosine deaminase blockers – dipiridamolum (curantylum). competitive inhibitor of phosphodiesterase and adenosine deaminase. increases concentration of …

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tema lektsii: kardiotonicheskie sredstva (ks) clinical pharmacology of medicines, influencing on hemostasia classification of medicines influencing on hemostasia i. direct anticoagulants: 1. dependant from antythrombinum iii a) usual unfractionated heparin b) low molecular weight heparin: - enoxaparin (clexane) - nadroparin (fraxiparin) - daltepparin (fragmin) - reviparin (clivarin) - tinzaparin (logiparin) 2. independent of an antithrombin iii a) hirudin, girugen ii. indirect anticoagulants: 1. coumarin derivatives: - warfarin (coumadin) - bishydroxicoumarol (dicumarin) – ethylbiscumacetate (neodicumarun, pelentan) - acenocoumarol (syncumar) 2. derivatives of an indandion. - phenyndion (phenylin) - omephyn iii. thrombolitics (fibrinolytics): 1. activated in vitro plasminogen - fibrinolysi...

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