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04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006
Drugs affecting bloodDrugs affecting blood
• They are used to tr...
04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006
Con.Con.
-Stimulated coagulation cascade leads to the-Stimulated...
04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006
ChemicalChemical signalssignals that oppose-plateletthat oppose-...
04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006
ChemicalChemical signalssignals that promote-plateletthat promot...
04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006
Platelet aggregation inhibitorsPlatelet aggregation inhibitors
•...
04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006
AnticoagulantsAnticoagulants
• Heparin : It is an injectable,rap...
04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006
Con.Con.
• Therapeutic uses :Therapeutic uses :
-It acts on thro...
04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006
WarfarinWarfarin
• Coumarin anticoagulnt = warfarin +Coumarin an...
04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006
Con.Con.
• Mechanism of action :These vitamin KMechanism of acti...
04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006
Con.Con.
• Pharmacokinetics :Pharmacokinetics :
* Sodium salts o...
04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006
Trombolytic drugsTrombolytic drugs
• Plasminogen is activated sy...
04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006
Con.Con.
• They should be given intracoronary toThey should be g...
04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006
Drugs used to treat bleedingDrugs used to treat bleeding
• In fi...
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Drugs affecting blood

Drugs Affecting Blood

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Drugs affecting blood

  1. 1. 04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006 Drugs affecting bloodDrugs affecting blood • They are used to treat thrombosisThey are used to treat thrombosis bleeding and anaemia.bleeding and anaemia. • Vascular trauma :Vascular trauma : -punctures or cuts lead to the formation-punctures or cuts lead to the formation of a platelets-fibrin plug.of a platelets-fibrin plug. -Clot formation = platelet activation-Clot formation = platelet activation aggregation thrombin fibrinaggregation thrombin fibrin clot .clot . -Inactive platelets respond to vascular-Inactive platelets respond to vascular trauma by adhesion to the site of injury.trauma by adhesion to the site of injury.
  2. 2. 04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006 Con.Con. -Stimulated coagulation cascade leads to the-Stimulated coagulation cascade leads to the increase of thrombin level and hence, fibrinogenincrease of thrombin level and hence, fibrinogen strands forming the hemostatic plug.strands forming the hemostatic plug. - Both thrombi and emboli occlude the bloodBoth thrombi and emboli occlude the blood vessels and decrease oxygen and nutrients invessels and decrease oxygen and nutrients in tissues.tissues. - Arterial thrombosis may lead to atheroscelorosis .Arterial thrombosis may lead to atheroscelorosis . - Defects in normal defense hemostaticDefects in normal defense hemostatic mechanisms may lead to blood stasis or impropermechanisms may lead to blood stasis or improper coagulation cascade and hence ,venouscoagulation cascade and hence ,venous thrombosis.thrombosis.
  3. 3. 04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006 ChemicalChemical signalssignals that oppose-plateletthat oppose-platelet activation:activation: • Increased prostacyclin levels.Increased prostacyclin levels. • Decreased plasma levels of thrombin andDecreased plasma levels of thrombin and thromboxanes .thromboxanes .
  4. 4. 04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006 ChemicalChemical signalssignals that promote-plateletthat promote-platelet aggregation:aggregation: • Decreased prosacyclin levels .Decreased prosacyclin levels . • Exposed collagen may lead to plateletExposed collagen may lead to platelet release reaction.release reaction. • Increased synthesis of thromboxanes .Increased synthesis of thromboxanes . • Both types of signals balance whetherBoth types of signals balance whether platelet are stimulated or stayedplatelet are stimulated or stayed quiescent.quiescent.
  5. 5. 04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006 Platelet aggregation inhibitorsPlatelet aggregation inhibitors • They act by decreasing the formation orThey act by decreasing the formation or the action of signals that promote plateletthe action of signals that promote platelet aggrgation.This is used in the treatment ofaggrgation.This is used in the treatment of cardiovascular diseases , maintenance ofcardiovascular diseases , maintenance of vascular grafts, arterial potency andvascular grafts, arterial potency and adjustment to thrombolytic therapy inadjustment to thrombolytic therapy in myocardial infarction e.g. aspirin.myocardial infarction e.g. aspirin.
  6. 6. 04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006 AnticoagulantsAnticoagulants • Heparin : It is an injectable,rapidly actingHeparin : It is an injectable,rapidly acting macromolecule that is complexed withmacromolecule that is complexed with histamines in mast cells. It is extractedhistamines in mast cells. It is extracted from porcine intestine or bovine lung.from porcine intestine or bovine lung. • Enoxaprin is a low molecular weightEnoxaprin is a low molecular weight heparin .heparin . • Heparin acts by enhancing inactiveHeparin acts by enhancing inactive clotting factorsclotting factors
  7. 7. 04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006 Con.Con. • Therapeutic uses :Therapeutic uses : -It acts on thrombi by preventing fibrin-It acts on thrombi by preventing fibrin formation.formation. - Enoxaprin prevent deep vein thrombosis- Enoxaprin prevent deep vein thrombosis following hip replacement.following hip replacement. • Phamacokinetics :It is given by deep S/C or I/MPhamacokinetics :It is given by deep S/C or I/M or in a bolus I/V followed by continuousor in a bolus I/V followed by continuous infusion.It binds to plasma proteins andinfusion.It binds to plasma proteins and reticuloendothelial cells and by depolymerizationreticuloendothelial cells and by depolymerization inactivated to be excreted in urine .inactivated to be excreted in urine .
  8. 8. 04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006 WarfarinWarfarin • Coumarin anticoagulnt = warfarin +Coumarin anticoagulnt = warfarin + dicumarol work by their ability todicumarol work by their ability to antagonize the co-factor functions ofantagonize the co-factor functions of vitamin K.vitamin K. • It is a former rodenticide that can not beIt is a former rodenticide that can not be monitored to keep the prothrombin time atmonitored to keep the prothrombin time at 1.5 to 2.5 .1.5 to 2.5 .
  9. 9. 04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006 Con.Con. • Mechanism of action :These vitamin KMechanism of action :These vitamin K cofactors including factors II,VII,IX and X,cofactors including factors II,VII,IX and X, undergo vitamin K-dependant post-undergo vitamin K-dependant post- translational modification. A number oftranslational modification. A number of their glutamine acid residues aretheir glutamine acid residues are carboxylated to formcarboxylated to form γγ--carboxyglutamiccarboxyglutamic acid residues that bind calcium ions andacid residues that bind calcium ions and are essential for interaction with cellare essential for interaction with cell membranes. Warfarin or dicumarol lead tomembranes. Warfarin or dicumarol lead to inactive clotting factors.inactive clotting factors.
  10. 10. 04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006 Con.Con. • Pharmacokinetics :Pharmacokinetics : * Sodium salts of warfarin if given orally* Sodium salts of warfarin if given orally are completely absorbed and bound toare completely absorbed and bound to plasma proteins ,hence they can notplasma proteins ,hence they can not diffuse to cerebrospinal fluid ,urine anddiffuse to cerebrospinal fluid ,urine and breast milk ,but can rapidly cross placentalbreast milk ,but can rapidly cross placental barreir and glucronidate to urine and stool.barreir and glucronidate to urine and stool.
  11. 11. 04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006 Trombolytic drugsTrombolytic drugs • Plasminogen is activated systemically byPlasminogen is activated systemically by streptokinases and urokinases and via tissue-streptokinases and urokinases and via tissue- uptake by alteplase to give plasmin and finallyuptake by alteplase to give plasmin and finally fibrin and fibrin degradation products.fibrin and fibrin degradation products. • They all act to convert plasminogen to plasmin ,They all act to convert plasminogen to plasmin , cleaves fibrin leading to lysed thrombin. This cancleaves fibrin leading to lysed thrombin. This can be achieved if initiated early after the clotbe achieved if initiated early after the clot formation.formation. • To avoid platelet thrombosis and aggregability useTo avoid platelet thrombosis and aggregability use antiplatelet drugs e.g. aspirin or antithromboticsantiplatelet drugs e.g. aspirin or antithrombotics e.g. heparin.e.g. heparin.
  12. 12. 04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006 Con.Con. • They should be given intracoronary toThey should be given intracoronary to treat myocardial infarction .treat myocardial infarction . • They are used to treat deep veinThey are used to treat deep vein thrombosis, serious pulmonary embolism ,thrombosis, serious pulmonary embolism , acute myocardial infarction , peripheralacute myocardial infarction , peripheral arterial thrombosis & emboli and forarterial thrombosis & emboli and for unclotted catherters and shunts.unclotted catherters and shunts. • These agents do not distinguish betweenThese agents do not distinguish between thrombi and fibrin.thrombi and fibrin.
  13. 13. 04/22/1504/22/15 Dr. Medani ,A.B.2006Dr. Medani ,A.B.2006 Drugs used to treat bleedingDrugs used to treat bleeding • In fibrinolytic status use aminocaproic acidIn fibrinolytic status use aminocaproic acid or transexamic acid.or transexamic acid. • Antagonize heparin by protamine sulfate.Antagonize heparin by protamine sulfate. • Stop bleeding problems by vitamin KStop bleeding problems by vitamin K11.. • Anaemia is treated with iron ,folic acidAnaemia is treated with iron ,folic acid ,cyalocobalamin and erythrobiotin.,cyalocobalamin and erythrobiotin. • Sickle cell anaemia is treated withSickle cell anaemia is treated with hydroxyurea .hydroxyurea .

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