ANTI-COAGULANTS - cardiovascular drugs (part 6A/7)
Inhibit the co-agulation by inhibiting Thrombin or Vit K anatagonists
Complexed with Histamine in Mast cells…Low molecular weigh heparin(LMWH)<6000
MOA=interact with AntiThrombin lll…speed up process of anti-coagulant ofn Antithrombin LMWH complex with Antithrombin & Inactivate Factor Xa…Prothrombin not convert into Thrombin…no formation of fibrin
T.E= used in Deep Vein Thrombosis…pulmonary embolism...Prophylactically in Pt. to avoid Postoperative thrombus during Elective surgery
Do not cross placenta...used in Pregnant women with Prosthetic heart valve
P.K=i.v administer...I/M inj leads to Hematoma formation…1-2hr t1/2…4hr of LMWH..
Titrate the infusion forr7-10 days so aPTT (activated Partial Thromboplastin time) b/w 1.5-2.5…. .taken up by Monocyte/Macrophage Sys for metabolismS.E= Hemorrhage...used Protamine sulphate, 1mg for 100 unit, weak antagonist….
Hypersensitivity reactions…risk of Thrombosis…Thrombocytopenia (abnormal Platelet) Osteoporosis...Contraindicated in surgery of brain,eye,spinal cord, in bleeding disorder
Lepirudin= Polypeptide...Similar to HIRUDIN derived from Leech Saliva..Produced in Yeast cell by Recombinant DNA technology…
Inhibit thrombin...diminish coagulation…bleeding major side effect
Argatroban= Directly inhibit Thrombin...used Prophylactically in Thrombosis in Pt with HIT
Fondaparinux=Pentasaccharides...FDA approved Prophylaxis of Deep Vein
Thrombosis in Hip or Knee surgery...long t1/2 17-21hr…contra in Renal Patients
Vitamin K Antagonists
Co-agulation factor needs Vit K as a Co-factor for Coagulation… these factors undergo into Vit K residue of Glutamic acid… which Carboxylated into γ-CarboxyGlutamic acid… it bind to Ca++ ions… essential for Coagulation factor & platelet aggregation….. Vit K dependent Carboxylase fix CO2 to form COOH on Glutamic acid…… Reduced Vit K converted into Vit K Epoxide by Vit K Epoxide Reductase…
Warfarin=Coumarin anticoagulant...initially Rodenticide…
MOA= inhibit Vit K Epoxide Reductase which convert Reduced Vit K into Vit K Epoxide.... convert Glutamic acid residue into γ-CarboxyGlutamic acid….. 40hr t1/2
T.E= used in Deep vein thrombosis & pulmonary embolism …prevention of thromboembolism in orthopedic surgery or Gynecologic
S.E=Skin lesion & necrosis…Black Boxwarning for Bleeding risk..Teratogenic cuase Abortion as well as Birth defects
Thrombolytic drugs
Streptokinase causes Systematic Fibrinolytic State...lead to bleeding problems Alteplase act locally on Thrombotic Fibrin to produce Fibrinolysis…
Urokinase produce in Kidney naturally, directly convert Plasminogen into Plasmin
MOA= Directly or indirectly Convert Plasminogen into Plasmin..Cleave Fibrin, lysing thrombus….Clot dissolution & Reperfusion occur
T.E= used to dissolve clots in Stroke
S.E= Hemorrhage …Contraindicated in Healing wound, Pregnancy, Head trauma,
Brain tumor, Intracranial bleeding, Metastatic Cancer
Alteplase= known as Tissue Plasminogen Activator(tPA)…derived from Human Melanoma cell…product of Recombinant DNA..Called “Fibrin Selective”…used for M.I…Eteplase can be used as Alternative
S.E= GIT & Cerebral Hemorrhage occur Streptokinase=extracellular protein obtained from Group C β-Heemolytic Streptococci used for M.I within 4hr…t1/2 is 1hr…high Antigenicity
MOA= form complex with Plasminogen...this enzymatically active complex convert Plasminogen into Plasmin …Plasmin catalyze degradation of Fibrin, factor V &VII
S.E=bleeding, hypersensitivity
Anistreplase=complex of Plasminogen & Streptokinase Activator …..prodrug
Urokinase=in kidney …low antigenicity…
MOA= directly cleave Arginine-Valine bond of Plasminogen to yield plasmin
T.E=lysis of pulmonary emboli….off-label use is treatment of M.I, arterial thromboembolism, coornonry artery thrombus
S.E= anaphylactic reaction
DRUGS USED TO TREAT BLEEDING
Hemophilia=deficiency of plasma coagulation factor esp. VII & IX
Aminocaproic acid & Tranxamic acid= inhibit Plasminogen activation...Tranxamic acid 10 time more potent…intravascular thrombosis is side effect
Protamine Sulphate=Antagonize anticoagulant effect of Heparin...obtain from fish sperm/Testes…high in Arginine..+Ve charge…basic...S.E: Hypersensitivity reaction
Vitamin K= Vit K1 (Phytonadione)…used in immediate Homeostatsis...Fresh frozen plasma infusion…require 24 hr
Aprotinin=Serine Protease inhibitor...block plasmin...inhibit Streptokinase…used in patients at risk of blood loss during Coronort Artery Bypass…cause Renal Dysfunction
AGENTS USED TO TREAT ANEMIA
Anemia=below normal Plaasma Hb resulting from decreasing no. of RBCs or Abnormally low Total Hb
Iron=known as Ferritin in Intestinal muscles...deficiency due to chronic blood loss, insufficient intake of iron during Accelerated growth in Childern & in heavily menstruating women…
Supplementation with Ferritin Sulphate….GIT disturbance reported
Folic Acid= used in Megaloblastic Anemia...Folinic acid/Leucovorin is reduced/active form of Vitamin B12
Cyanocobolamine (Vit B12) =deficiency due to loss of Intrinsic Factor (GP produced by Parietal cells of stomach) OR loss of receptor in intestine
Used in Pernicious Anemia….i.v or I/M,S/C used
Erythropoietin & Darbepoetin= Erythropoietin produce in Kidney regulate RBS proliferation & Differentiation in Bone marrow….
Darbepoetin is long active form of erythropoietin…
Used in Anemia due to End-stage renal disease, HIV infection, Cancer Patient….HB level not> 12g/dl & dose not > 1g/dl
AGENTS USED IN SICKLE CELL ANEMIA
Hydroxyurea=used to treat Chronic Myelogenous Leukemia, Polycythemia Vera….in Sickle cell Anemia drug increase Fetal HB level, diluting Abnormal HbS….
S.E= Bone marrow depression, Cutaneous Vasculitis
Pentoxyfylline=methylxanthine derivative…called “Rheologic modifier”….improves RBC flexibility & reduce Viscosity…decrease total Peripheral Resistance…increase O2
..Controlled or sustain release tab with food
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