02 Anticoagulant

8/2/2019 02 Anticoagulant

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1-HEPARIN. 2-Oral anticoagulants.

3-Antithrombin


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Low molecular weight heparin Synthetic pentasaccharide inhibitors of factorXa

Fondaparinux is a synthetic sugar composedof the five sugars (pentasaccharide) inheparin that bind to antithrombin. It is asmaller molecule than low molecular weight

heparin. Idraparinux

Heparin and derivative substances
http://en.wikipedia.org/wiki/Factor_Xahttp://en.wikipedia.org/wiki/Factor_Xahttp://en.wikipedia.org/wiki/Fondaparinuxhttp://en.wikipedia.org/wiki/Idraparinuxhttp://en.wikipedia.org/wiki/Idraparinuxhttp://en.wikipedia.org/wiki/Fondaparinuxhttp://en.wikipedia.org/wiki/Factor_Xahttp://en.wikipedia.org/wiki/Factor_Xa


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is a naturally occurring glycosaminoglycan, that hasimmediate action after its administration(subcutaneous or I.V). Mech. of action:Bind with antithrombin III (At III) ,potentiating its inhibitory action on thrombin, XIIa, XIa and Xa.


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1-Ordinary heparin ( mol.weight 15000-18000)

2-Low molecular weightheparin (mol weight =5000), it has a longer half life than

ordinary heparin


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Low molecular weight heparin is a morehighly processed product that is useful as itdoes not require monitoring of the APTTcoagulation parameter (it has more

predictable plasma levels) and has fewer sideeffects
http://en.wikipedia.org/wiki/Low_molecular_weight_heparinhttp://en.wikipedia.org/wiki/APTThttp://en.wikipedia.org/wiki/Coagulationhttp://en.wikipedia.org/wiki/Coagulationhttp://en.wikipedia.org/wiki/APTThttp://en.wikipedia.org/wiki/Low_molecular_weight_heparin


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Acute thrombosis ,and thrombosis in

pregnancyProphylaxis ofthrombosis in

pregnancy and in highrisk surgery


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Dose: S.c. 5000 u/ 8-12 h or 2000 u oflow MW

Continuous I.V. : 1000 u / 6 hoursMonitoring:

By A.P.T.T.: keep it 1.5 -2.5times that of the control plasma


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Toxicity: Bleeding Osteoperosis Thromocytopenia

Treatment of overdose:By protamine sulphate (1 mg IVneutralize 100 u heparin)


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Ex. Warfarin Action: takes 48 72 hours for full action

Interfere with the action of vitamin k in thehepatic synthesis of factors II, VII, IX and X Inhibit action of protein C and S

Monitoring of its action: By PT (prothrombin time) and INR


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Treatment of deep vein thrombosis(DVT) and pulmonary embolism (INR 2-3) Prophylaxis of DVT in high risk surgery(INR- 2-2.5) Recurrent DVT (INR 3-4.5) A.F (INR 3-4.5) Myocardial infraction (INR 3-4.5) Prosthetic valves and grafts (INR 3-4.5)


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PregnancyPeptic ulcerSevere hypertensionInfective endocarditisRenal damageHepatic diseases


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Potentiation of its action :oral hypoglycemic drugs,aspirin, NSAID , penicillinand alcohol

Reduction of its action :spironoloctone,barbiturates and oralcontraceptive drugs


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Another type of anticoagulant is the directthrombin inhibitor. Current members of thisclass include argatroban, lepirudin,

bivalirudin, and dabigatran.
http://en.wikipedia.org/wiki/Direct_thrombin_inhibitorhttp://en.wikipedia.org/wiki/Direct_thrombin_inhibitorhttp://en.wikipedia.org/wiki/Argatrobanhttp://en.wikipedia.org/wiki/Lepirudinhttp://en.wikipedia.org/wiki/Bivalirudinhttp://en.wikipedia.org/wiki/Dabigatranhttp://en.wikipedia.org/wiki/Dabigatranhttp://en.wikipedia.org/wiki/Bivalirudinhttp://en.wikipedia.org/wiki/Lepirudinhttp://en.wikipedia.org/wiki/Argatrobanhttp://en.wikipedia.org/wiki/Direct_thrombin_inhibitorhttp://en.wikipedia.org/wiki/Direct_thrombin_inhibitor


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Laboratory instruments, test tubes, bloodtransfusion bags, and medical and surgicalequipment will get clogged up and becomenonoperational if blood is allowed to clot.

Chemicals can be added to stop bloodclotting. Apart from heparin, most of thesechemicals work by bindingcalcium ions,preventing the coagulation proteins fromusing them.
http://en.wikipedia.org/wiki/Medical_laboratoryhttp://en.wikipedia.org/wiki/Chelationhttp://en.wikipedia.org/wiki/Calciumhttp://en.wikipedia.org/wiki/Coagulationhttp://en.wikipedia.org/wiki/Coagulationhttp://en.wikipedia.org/wiki/Calciumhttp://en.wikipedia.org/wiki/Chelationhttp://en.wikipedia.org/wiki/Medical_laboratory


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EDTA is denoted by mauve or purple caps onVacutainer brand test tubes. This chemical stronglyand irreversibly binds calcium. It is in a powderedform.

Citrate is usually in blue Vacutainer tube. It is in

liquid form in the tube and is used for coagulationtests, as well as in blood transfusion bags. It gets ridof the calcium, but not as strongly as EDTA. Correctproportion of this anticoagulant to blood is crucialbecause of the dilution. It can be in the form of

sodium citrate or ACD. Oxalate has a mechanism similar to that of citrate. It

is the anticoagulant used in fluoride (grey top) tubes.
http://en.wikipedia.org/wiki/EDTAhttp://en.wikipedia.org/wiki/Citratehttp://en.wikipedia.org/wiki/Sodium_citratehttp://en.wikipedia.org/wiki/Acid-citrate-dextrosehttp://en.wikipedia.org/wiki/Sodium_citratehttp://en.wikipedia.org/wiki/Acid-citrate-dextrosehttp://en.wikipedia.org/wiki/Oxalatehttp://en.wikipedia.org/wiki/Fluoridehttp://en.wikipedia.org/wiki/Fluoridehttp://en.wikipedia.org/wiki/Fluoridehttp://en.wikipedia.org/wiki/Oxalatehttp://en.wikipedia.org/wiki/Acid-citrate-dextrosehttp://en.wikipedia.org/wiki/Sodium_citratehttp://en.wikipedia.org/wiki/Citratehttp://en.wikipedia.org/wiki/EDTA


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Drugs that are able tolyses fresh thrombin


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Direct or indirectactivation of plasminogen, with stimulation offibrinolytic pathway

Lyses of intravascularclots

Lyses of fibrinogen


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a.Can be used systemically

as in :Acute pulmonary embolismIleofemoral thrombosis

b.Or locally as in peripheralarterial diseases


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First generation agents e.g.,streptokinase and urokinaseSecond generation agents:Tissue plasminogen activatorsSingle chain uorkinaseplasminogen activatorsAcylated plasminogenstreptokinase activators


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Severe hypertensionPeptic ulcerRecent streptococcalinfection


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1- Aspirin.2-Dipyridamole(persantin)3-Sulphinpyrazone .


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Action: In low dose (75 mg/d)irreversibly inhibit the plateletcyclo-oxygenase activity , henseinhibiting the generation ofthrombokinase A2 (TXA2) thusinhibiting platelets aggregationand the release reaction ofplatelets


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In standard dose itreversibly inhibit theendothelial cell cyclo-oxygenase thus preventsynthesis of prostacyclineswhich is anti aggregator


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Gastrointestinal:Aspirin use has been shown toincrease the risk ofgastrointestinal bleeding

Central effects:tinnitus. Reye's syndrome: a severe illness characterized

by acute encephalopathy and fatty liver, canoccur when children or adolescents are givenaspirin for a fever or other illnesses orinfectionFood and Drug Administration now

recommends that aspirin (or aspirin-containingproducts) should not be given to anyone underthe age of 12 who has a fever.
http://en.wikipedia.org/wiki/Gastrointestinal_bleedinghttp://en.wikipedia.org/wiki/Tinnitushttp://en.wikipedia.org/wiki/Encephalopathyhttp://en.wikipedia.org/wiki/Fatty_liverhttp://en.wikipedia.org/wiki/Food_and_Drug_Administration_(United_States)http://en.wikipedia.org/wiki/Food_and_Drug_Administration_(United_States)http://en.wikipedia.org/wiki/Food_and_Drug_Administration_(United_States)http://en.wikipedia.org/wiki/Food_and_Drug_Administration_(United_States)http://en.wikipedia.org/wiki/Fatty_liverhttp://en.wikipedia.org/wiki/Encephalopathyhttp://en.wikipedia.org/wiki/Tinnitushttp://en.wikipedia.org/wiki/Gastrointestinal_bleeding


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is a phosphodiesteraseinhibitor , that increase thelevel of C-AMP in platelets ,it also has a synergisticaction with low dose aspirin


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interfere with plateletfunction by unknownmechanism

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02 Anticoagulant