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MindMap Gallery Drugs that act on the blood and hematopoietic system_backup_1708de
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Drugs that act on the blood and hematopoietic system_backup_1708de
Anticoagulants, heparin, low molecular weight heparin, enoxaparin, vitamin K, hirudin, thrombin inhibitors, vitamin K antagonists, dicoumarol, warfarin, hepatic enzyme inducers, rheumatism, antibiotics Platelets, aspirin, cAMP, dipyridamole, ADP, clopidogrel, fibrinolytic drugs, streptokinase, urokinase, alteplase, t-PA, procoagulant drugs, vitamin B12, iron deficiency anemia, folic acid , amino acid interconversion, dextran, blood volume expansion drugs.
Edited at 2022-11-17 16:34:48
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Drugs that act on the blood and hematopoietic system_backup_1708de
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Drugs that act on the blood and hematopoietic system
Overview
blood
blood cells
red blood cells
leukocyte
platelets
plasma
An important component of the internal environment that blood cells rely on to survive
hematopoietic system
hematopoietic organs
yolk sac
Liver, spleen, kidney, thymus, etc.
marrow
hematopoietic cells
bone marrow hematopoietic stem cells
Physiological hemostatic process
blood clotting process
blood clotting factors
Features
①Except factor III, all are in plasma
②Except for factor IV, all are globulin
③Except for factor IV, none is active under normal circumstances
④ Coagulation factors exist in the form of zymogens. When they are activated in a certain sequence, A waterfall-like coagulation reaction can occur
⑤Factors II, VII, IX, and X are synthesized by the liver and require the participation of vitamin K
fibrinolysis
Under the action of a series of hydrolases, the poorly soluble fibrin The process of degradation into soluble fibrin degradation products.
Section 1 Anticoagulant Drugs
Drugs that prevent blood from clotting by affecting clotting factors. used for Prevention and treatment of thromboembolic disease.
Classification
Indirect thrombin inhibitor: heparin
Originally named after its discovery in the liver, medicinal heparin is mainly derived from Extracted from porcine small intestinal mucosa and bovine lung. 5 ~ 30kD.
[Anticoagulant effect of heparin]
Anticoagulant characteristics
1
) has anticoagulant effects both in vivo and in vitro
2
) is powerful and rapid
Anticoagulation mechanism
1. Enhance the activity of antithrombin III
➢ATIII (containing arginine residue) is the coagulation factor IIa, IXa, Xa, XIa, XIIa (containing serine residues) through sperm-silk peptide bonds Combine to form an inactive complex that produces anticoagulation.
Heparin can accelerate this reaction >1000 times
The effect of heparin on inhibiting thrombin activity is related to the length of the molecule. The longer the molecule, the stronger the inhibitory effect.
2. Activate heparin cofactor II
At high concentrations, it activates HCⅡ and increases its inhibition rate on thrombin.
3. Promote activation of fibrinolytic system
Vascular endothelial cells release t-PA
[Other pharmacological effects of heparin]
Lower blood lipids;
anti-inflammatory;
Inhibit vascular smooth muscle proliferation;
Inhibit platelet aggregation
【In vivo process】
1. Not absorbed after oral administration; subcutaneous and intramuscular injection
Causes hematoma, often administered intravenously
2. Liver metabolism
3.
t 1/2 is related to the dose
【Clinical application】
1. Thromboembolic diseases
Prevent blood clots form and expand
2. Disseminated intravascular coagulation (DIC)
Early days
3. Extracorporeal anticoagulation
【Adverse reactions】
1,
Bleeding Protamine Sulfate (Rescue)
2,
Thrombocytopenia: 1-4 days, transiently causing platelet aggregation;
7-10 days
, related to immune response
3.
Allergic Reaction: Asthma
4.
Osteoporosis, spontaneous fracture: long-term
【Contraindications】
Liver and renal insufficiency Bleeding tendencies, peptic ulcer, severe high blood pressure, hemophilia, active tuberculosis, Visceral tumors, post-surgery, pregnant women
low molecular weight heparin
Isolated from unfractionated heparin or after degradation, molecular weight < 7 kD
Anticoagulation mechanism is the same as that of heparin
Route of administration: subcutaneous injection
Commonly used preparations: enoxaparin
Low molecular weight heparin vs. heparin
Selectively inhibits the activity of coagulation factor Xa
➢Anticoagulant factor Xa/Ⅱa activity ratio↑, less bleeding
➢High bioavailability, long tl/2
➢Less likely to induce thrombocytopenia
thrombin inhibitors
1.
Direct thrombin inhibitor: hirudin
➢Anticoagulant components in leech saliva
➢Powerful and specific thrombin inhibitor
1:1 directly binds to thrombin and inhibits its activity
➢Genetically recombinant hirudin (r-hirudin) has the same effect as natural hirudin.
2.
VitK antagonist coumarins
Basic structure: 4-hydroxycoumarin
Representative medicine:
Warfarin (benzyl acetone coumarin, warfalin)☆
dicoumarol
Acenocoumarol (new anticoagulant)
【Pharmacological effects】
Coumarins are vitamin K antagonists that inhibit the production of vitamin K The epoxy type is converted to the hydroquinone type, preventing the recycling of vitamin K. Keep coagulation factors II, VII, IX, and X in the inactive precursor stage segment, thus affecting the coagulation process.
No effect on activated coagulation factors
Anticoagulant characteristics:
1
, slow-acting, long-lasting
2
, anticoagulation in vivo, ineffective in vitro
【In vivo process】
1. Oral anticoagulants, which take effect slowly (12 to 24 hours) and last for 2 to 5 days.
2. Warfarin is completely absorbed after oral administration Dicoumarol is absorbed slowly and irregularly
3
, high plasma protein binding rate (>99%
4
, liver metabolism, kidney excretion
【Clinical Use】
1. Prevent and treat thromboembolic diseases (Atrial fibrillation, valvular heart disease)
2. Prevent postoperative venous thrombosis
Advantages: Effective when taken orally, long-lasting effects Disadvantages: Slow onset of action, difficult to control dosage Sequential therapy: first heparin and then coumarins
【Adverse reactions】
Spontaneous bleeding: VitK fights, fresh blood Not allowed for pregnant women
[Coumarin drug interactions]
① Aspirin, phenylbutazone, etc. replace plasma proteins to enhance their effects
② Broad-spectrum antibiotics reduce the production of VitK and enhance its effect
③ Barbiturates, phenytoin, etc. induce liver drug enzymes and weaken their effects;
Amiodarone, metronidazole, etc. inhibit liver drug enzymes and enhance their effects.
④ Contraceptive pills increase coagulation and weaken their effect
3.
New oral anticoagulant: dabigatran etexilate
Section 2 Antiplatelet Drugs
Drugs that inhibit platelet adhesion, aggregation, and release.
Classification
Inhibits platelet arachidonic acid metabolism
Cyclooxygenase inhibitor - aspirin☆ (aspirin, acetylsalicylic acid)
【Mechanism】
small dose
Irreversibly inhibit platelet cyclooxygenase (COX-1) activity
Inhibits arachidonic acid metabolism
Reduce the production of thromboxane A2 (TXA2)
Inhibit platelet aggregation and thrombosis
【Clinical Use】
Low-dose aspirin (75 to 150 mg) widely For the prevention and treatment of cardiovascular and cerebrovascular embolism diseases
【Adverse reactions】
Gastrointestinal bleeding and gastrointestinal ulcers
Increase cAMP content in platelets
Dipyridamole (Dipyridamole, dipyridamole)
【Mechanism】
1. Inhibit phosphodiesterase, ↑cAMP content
2. Activate adenylyl cyclase, ↑cAMP content
3. Promote the production of PGI2 by vascular endothelial cells
4. Inhibit platelet COX-1 and reduce TXA2 production
Inhibit platelet aggregation
【Clinical application】
Prevention and treatment of thromboembolic diseases. Often used in combination with coumarins.
Inhibits ADP activation of platelets
Clopidogrel
Prodrugs, metabolites are active.
mechanism:
Powerful platelet aggregation inhibitor (inhibits ADP and blood coagulation board combination).
clinical
Arterial embolism in the heart and brain caused by high platelet aggregation
Adverse reactions:
Gastrointestinal bleeding, neutropenia, etc.
Block platelet membrane glycoprotein IIb /IIIa receptor
abciximab
Relatively new antiplatelet drugs, monoclonal antibodies.
mechanism:
Block GPIIb/IIIa receptors (this receptor is responsible for thrombocytopenia) specific recognition and binding sites for plate-aggregated adhesion proteins), thereby Inhibits platelet aggregation.
clinical:
Myocardial infarction, unstable angina
Section 3 Fibrinolytic Drugs
Convert plasminogen into plasmin and promote fibrinolysis, Drugs that dissolve blood clots are also called thrombolytic drugs.
For the treatment of acute thromboembolic diseases, organized thrombus Cannot be restored.
Commonly used drugs
Streptokinase (
SK)
Initial: Extracted from β-hemolytic streptococci culture fluid
Now: Genetic recombination technology preparation
【Pharmacological effects】
Indirect activation requires the formation of streptokinase-plasminogen complex. In order to promote plasminogen to become plasmin and degrade fibrin, Dissolve blood clots.
It is difficult to work on organized thrombi. It should be applied as early as possible.
【Clinical application】
For acute thromboembolic disease. Early medication is required, and thrombosis is preferably < 6 hours.
【Adverse reactions】
1. Spontaneous bleeding: not only activates plasminogen in the clot, Simultaneously activates plasminogen in plasma. In severe cases, use antifibrinolytic drugs (aminotoluic acid).
2. Allergic reaction
Urokinase (
UK
Produced by the kidneys, extracted from healthy human urine, non-antigenic
mechanism:
Directly activate plasminogen to become plasmin, Dissolve fibrin.
clinical:
Myocardial infarction and other thromboembolic diseases
Adverse reactions:
Bleeding, lighter than streptokinase; No allergic reactions.
Alteplase (
t-PA
Tissue plasminogen activator, a second-generation thrombolytic drug.
Binds to the fibrin in the blood clot, causing it to bind to the fibrin White-bound plasminogen becomes plasmin, which degrades fibrin, Dissolve blood clots.
Used for acute myocardial infarction, stroke, etc.
High selectivity and relatively low bleeding incidence
anistreplase
Staphylokinase
Section 4 Procoagulant Drugs
Can promote blood coagulation, inhibit fibrinolysis, reduce Drugs that reduce capillary permeability, thereby stopping bleeding.
vitamins
K
Overview
Basic structure: menaquinone
K1: Plants K2: Gut bacteria K3: Artificial synthesis, sodium bisulfite menadione K4: Artificial synthesis, acetyl menadione
【Pharmacological effects】
Vitamin K is a coenzyme of γ-carboxylase and participates in coagulation factors Synthesis of II, VII, IX and X.
These factors have glutamic acid residues on their precursors, which are involved in γ-carboxylation Under the action of enzyme, γ-carboxyglutamic acid is formed, which has the ability to interact with Ca2 , Platelet membrane phospholipid binding ability
【Clinical application】
1. Bleeding caused by Vit K deficiency
Chronic diarrhea, lack of bile; Hemorrhage in neonates and premature infants; Long-term use of broad-spectrum antibiotics.
2. Overdose of anticoagulants
(Coumarins, Salicylan Bleeding caused by acids)
【Adverse reactions】
1. Vit K1 is injected intravenously too quickly (face flushing, difficulty breathing, Collapse); use intramuscular injection;
2. Gastrointestinal reactions;
3. Large doses of Vit K3 can make newborns, premature infants, and glucose-6- Hemolysis in patients with phosphate dehydrogenase deficiency
coagulation factor preparations
Prothrombin complex:
Contains coagulation factors II, VII, IX, and X, Used to treat hemophilia B, severe liver disease, coumarin overdose Bleeding caused by amount.
Antihemophilic globulin:
Contains coagulation factor VIII and a small amount of fibrin White Plains, used to treat hemophilia A.
fibrinolysis inhibitors
Tranexamic acid, tranexamic acid
【Pharmacological effects】
Competitively inhibits plasminogen activator, causing fibrin Lysinogen cannot be converted to plasmin, thereby stopping bleeding
【Clinical application】
Bleeding caused by hyperfibrinolysis (liver, spleen, lungs, anterior prostate surgery). Bleeding due to overdose of streptokinase and urokinase
【Adverse reactions】
Not obvious, overdose can cause blood clots and induce myocardial infarction
Section 5 Anti-anemia drugs and hematopoietic cell growth factors
anemia
Number of red blood cells or hemoglobin content in circulating blood Pathological phenomena that are lower than normal
type
iron deficiency anemia
megaloblastic anemia
aplastic anemia
Anti-anemia drugs: Treat the cause.
Iron supplement
Iron constitutes hemoglobin, myoglobin, heme enzyme, etc.
Iron deficiency causes microcytic hypochromic anemia, that is, iron deficiency anemia, In severe cases, it affects children's behavior and learning ability.
The internal processes of iron supplements
Factors that promote iron absorption: gastric acid, vitamins C. Fructose, glutathione, etc.;
Factors that are not conducive to iron absorption: achlorhydria, High phosphorus, high calcium, tetracycline, etc.
【Clinical application】
iron deficiency anemia
4 - 5d; 4 - 8w; halved to continue 2 - 3m
【Adverse reactions】
1
, gastrointestinal irritation
2
,constipate
3
, Acute poisoning: NaHCO 3 , deferoxamine
folic acid☆
【Pharmacological effects】
Tetrahydrofolate serves as a coenzyme for one-carbon unit transferase, transferring one-carbon unit, involved in various biochemical metabolisms in the body.
① De novo synthesis of purine nucleotides
DNA synthesis
② dUMP→ dTMP
DNA synthesis
③Interconversion of amino acids: Ser →Gly, Cys→ Met
【Clinical application】
1. Megaloblastic anemia (nutritional): mainly folic acid
2. Megaloblastic anemia (drug-induced): methotrexate, ethylamine Pyrimidine inhibits dihydrofolate reductase, directly using calcium leucovorin
3. Pernicious anemia: folic acid as supplement
Replenish
Low-dose folic acid may prevent fetal neural tube defects
Vitamin B12 ☆
Overview
Cobalamin (containing cobalt), rich in animal offal, milk, eggs Huang Zhong.
Vitamin B12 in the body: methylcobalamin, 5-deoxyadenosylcobalamin
Medicinal vitamin B12: cyanocobalamin, hydroxocobalamin.
Coenzyme necessary for cell division and maintaining the integrity of the myelin sheath of nervous tissue.
【Pharmacological effects】
2. Methylmalonyl CoA → succinyl CoA tricarboxylic acid cycle MethylmalonylCoA ∽ MalonylCoA (fatty acid synthesis)
【In vivo process】
Combined with intrinsic factor (gastric-parietal cells), Easily absorbed by the small intestine
【Clinical application】
1. Pernicious anemia
Vit B 12 mainly
2. Megaloblastic anemia
: Folic acid
3. Nervous system diseases
: neuritis, god
menstrual atrophy
4. Hyperhomocysteinemia
Hematopoietic cell growth factor—
—Erythropoietin EPO (erythropoietin, erythropoietin)
The peritubular cells of the renal proximal tubule secrete glycoproteins.
Clinical: Recombinant human EPO
①Promote the proliferation, differentiation and maturation of erythroid stem cells
②Promote the release of reticulocytes into the blood.
clinical:
Anemia due to various causes, especially chronic renal failure.
Adverse reactions: few, high blood pressure, headache, etc.
—Leukocyte production-stimulating drugs
Human granulocyte colony-stimulating factor (filgrastim)
Promote the proliferation, differentiation, maturation and release of neutrophils, Enhance its chemotactic and phagocytic functions.
Clinical: Neutropenia
Human granulocyte-macrophage colony-stimulating factor (sargramostim)
Promote the proliferation and differentiation of granulocytes, monocytes and macrophages , mature, and improve its phagocytic and immune activities.
Clinical: Leukopenia
Section 6 Blood Volume Expansion Drugs
Plasma substitutes, by increasing plasma colloid osmotic pressure, expand Effective circulating blood volume.
Starch/polysaccharides:
Dextran, hydroxyethyl starch
【Pharmacological effects】
1
, expand blood volume
2
, anti-thrombotic, improve microcirculation
Inhibit platelet and red blood cell aggregation
Inhibits the activity of coagulation factor II
3. Osmotic diuresis
【Clinical application】
1. Hypovolemic shock (blood loss, burns)
2. Prevent DIC
3. Thromboembolic diseases
【Adverse reactions】
1. Allergic reactions: urticaria, asthma, etc.
2. Bleeding: epistaxis, etc.
【Contraindications】
1
, congestive heart failure
2
, bleeding disorders
3
, liver and kidney insufficiency
Egg whites/gelatins:
Human albumin, succinylated gelatin
other kind:
Povidone