AnTicoagulant drugs 1. Pharmacological effects (1)Anticoagulation 1)Heparin increase the activity of AT Il The aT Il may inhibit the activity of the activatedⅡa、Ⅺa、Ⅸa、Ⅹa、Ⅻa. to cause anticoagulation 2)Characteristics of anticoagulation OIt is effective in vitro and in vivo @Its effects are rapid (iv)( < 10min)and short(3-4 h): activated partial thromboplastin time(APTT)↑
1. Pharmacological effects (1)Anticoagulation: 1)Heparin increase the activity of AT Ⅲ The AT Ⅲ may inhibit the activity of the activated Ⅱa、Ⅺa、Ⅸa、Ⅹa、Ⅻa, to cause anticoagulation. 2)Characteristics of anticoagulation ①It is effective in vitro and in vivo ; ②Its effects are rapid(iv) (<10min)and short(3～4 h): activated partial thromboplastin time(APTT) ↑ Anticoagulant drugs
ANTICOGO山crcr山c (2)Anti-atherosclerosis: rEgulating blood li ipds: VLDLL 2)Protecting endothelial cells; 3)Inhibiting the proliferation of smooth muscle cells 4)Inhibits platelet aggregation (3other effects Anti-complement, anti-inflammation and↓ blood viscosity(血液粘度)
(2)Anti-atherosclerosis: 1)Regulating blood lipids: VLDL 2)Protecting endothelial cells; 3)Inhibiting the proliferation of smooth muscle cells. 4)Inhibits platelet aggregation (3)Other effects: Anti-complement, anti-inflammation, and blood viscosity（血液粘度）. Anticoagulant drugs
AaTiCoac山 ani drug 2. Pharmacokinetics Heparin and LMWH are mostly (1)Heparin is not absorbed confined to the vascularsystem by GI t need iv. or sc Partially degraded Heparin heparin and IV, deep sc (2)pl asma proTein binding LMWHs LMWHs: SC rate: 80% appear in the urine (3)t1/2:1~2hr It's metabolised in liver, and partially degraded heparin appears n the urine Heparin and LMWHs
2. Pharmacokinetics (1)Heparin is not absorbed by GI. It need iv. or sc. (2)plasma protein binding rate: 80% (3)t1/2: 1～2 hr. It’s metabolised in liver, and partially degraded heparin appears in the urine. Anticoagulant drugs
ATICOaCI山cruc 3. Clinical uses (1)Anticoagulation Such as: pulmonary emboli; deep vein thrombosis cardiac infarction, etc (2)Heart ischemia Prevent emboli in coronary artery early use (DIC(disseminated intravascular coagulation,弥散性血管内凝血) Such as: certain surgical procedures hemodialysis, cardiac catheterization, etc 4)Prevent coagulation in vitro
Anticoagulant drugs 3. Clinical uses (1)Anticoagulation Such as: pulmonary emboli; deep vein thrombosis; cardiac infarction, etc. (2)Heart ischemia Prevent emboli in coronary artery—— early use. (3)DIC(disseminated intravascular coagulation, 弥散性血管内凝血) Such as: certain surgical procedures, hemodialysis, cardiac catheterization, etc. (4)Prevent coagulation in vitro
AnTICoagu山 r drugs 4. Adverse effects (1) Bleeding(5%~10%) Protamine sulfate(硫酸鱼精蛋白) is the antagonist of heparin. 1 mg protamine=100U heparin. (2) Heparin- induced thrombocytopenia(血小板减 少症)(HIT) 5%6%, Warfarin should be substi-tuted if the platelet count fall ()Others Allergy(过敏反应) Local necrosis((局部坏死), when sc Increased loss of hair and reversible alopecia(B2) Osteoporosis(骨质疏松) (4)Contraindicated in patients with bleeding risk
4. Adverse effects (1)Bleeding(5%～10%) Protamine sulfate（硫酸鱼精蛋白）is the antagonist of heparin. 1mg protamine=100U heparin. (2) Heparin-induced thrombocytopenia(血小板减 少症) (HIT) 5%～6%, Warfarin should be substi-tuted if the platelet count falls. (3)Others Allergy(过敏反应); Local necrosis(局部坏死), when sc; Increased loss of hair and reversible alopecia(脱发); Osteoporosis(骨质疏松). (4) Contraindicated in patients with bleeding risk Anticoagulant drugs