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MindMap Gallery Drugs that act on the circulation and blood system (4)
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Drugs that act on the circulation and blood system (4)
This is a mind map about four drugs that act on the circulation and blood system, including antihypertensive drugs, drugs that act on the blood system and hematopoietic system, antiarrhythmic drugs, etc.
Edited at 2024-03-09 11:23:02
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Drugs that act on the circulation and blood system (4)
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- Outline
Drugs that act on the circulatory and blood systems
antihypertensive drugs
Hypertension classification standards
Commonly used antihypertensive drugs
Calcium channel blocker CCB
Relaxes vascular smooth muscle by reducing intracellular calcium ion concentration
nifedipine
Pharmacological effects
Dihydropyridines
Lowering blood pressure is accompanied by reflexive acceleration of heart rate, increased cardiac output, and increased plasma renin activity. Combined use of β-receptor antagonists can avoid and enhance the antihypertensive effect.
Clinical application
hypertension
Adverse reactions
Flushing face
ankle edema
Headache
Palpitations
Long-term prone to gum hyperplasia
Niqun Diping
Suitable for all levels of hypertension, especially for elderly patients
Adverse reactions similar to those of nifedipine
People with poor liver function should use with caution or reduce the dosage
amlodipine
Second-generation dihydropyridines, long-acting calcium channel blockers
Reverse vascular hypertrophy and protect target organs
Once a day, 7 a.m. and 3 p.m.
Adverse reactions
Headache, dizziness, palpitations, edema, nausea and diarrhea, etc.
adrenergic receptor antagonists
beta receptor antagonist
Mechanism
Block cardiac β1 receptors, inhibit myocardial contractility, and reduce cardiac output.
Blocks the glomerular β1 receptor, reduces renin secretion, inhibits the activity of the renin-angiotensin system, resulting in reduced vascular tone and blood volume.
Blocks beta receptors in the presynaptic membrane of sympathetic nerve terminals, inhibits positive feedback, and reduces norepinephrine secretion
Block central beta receptors and reduce peripheral sympathetic nerve activity
Clinical application
hypertension
It is more suitable for patients with hypertension accompanied by tachyarrhythmia, angina pectoris, chronic heart failure, and young hypertensive patients with high renin activity and high hemodynamics.
Representative medicine
propranolol
Clinical application
Grade I and II hypertension, especially suitable for young and middle-aged hypertensive patients with fast heart rate and those with angina pectoris
Hypertensive patients with cerebrovascular disease
Adverse reactions
rebound phenomenon
Disable
Hypertensive patients with bronchial asthma, severe atrioventricular block, sinus bradycardia, etc.
Metoprolol
Selective β1-receptor antagonist with no intrinsic sympathomimetic activity
bisoprolol
Good effect on heart failure
α1 receptor antagonist
α1 receptor antagonists can selectively block α1 receptors in the postsynaptic membrane of vascular smooth muscles, relax arteriolar and venous smooth muscles, reduce peripheral resistance, and cause a decrease in blood pressure.
Prazosin
Pharmacological effects
Blocks α1 receptors on blood vessel walls, dilates arterioles and venules, mainly dilates arterioles, and has a blood pressure lowering effect in both standing and supine positions.
Clinical application
Hypertension at all levels, mainly treating patients with grade I and II hypertension and hypertensive patients with renal insufficiency
Elderly patients with high blood pressure and prostatic hypertrophy can reduce the symptoms of dysuria
For patients with severe hypertension, diuretics and beta-receptor antagonists can be combined to increase the efficacy.
Adverse reactions
Severe orthostatic hypotension, palpitations, syncope, etc. may occur after taking the drug for the first time, which is called the "first dose phenomenon". It usually occurs within 1 hour after taking the drug. If the first dose is reduced to 0.5 mg, it can be avoided by taking it in the supine position or before going to bed.
Terazosin
doxazosin
alpha, beta receptor antagonists
labelore
Pharmacological effects
By blocking α1 and β receptors, it reduces peripheral resistance and produces antihypertensive effects.
Clinical application
All levels of hypertension, intravenous injection can treat hypertensive crisis
Hypertension during pregnancy, hypertensive emergency
Angina pectoris
Angiotensin-converting enzyme inhibitor ACEI
antihypertensive mechanism
Inhibits angiotensin I converting enzyme, reduces the production of angiotensin II, and reduces the secretion of aldosterone
Because angiotensin I converting enzyme can hydrolyze bradykinin, by inhibiting angiotensin I converting enzyme, it reduces the hydrolysis of bradykinin and dilates blood vessels.
Clinical application
This type of drug has good target organ protection and cardiovascular endpoint prevention effects in patients with hypertension.
It is suitable for hypertensive patients with chronic heart failure, cardiac insufficiency after myocardial infarction, diabetic nephropathy, non-diabetic nephropathy, metabolic syndrome, proteinuria or microalbuminuria.
Captopril
Pharmacological effects
Lowering blood pressure is not accompanied by a reflex increase in heart rate
Reduce renal vascular resistance and increase renal blood flow
Prevents and reverses myocardial and vascular remodeling
Does not cause electrolyte imbalance and abnormal lipid metabolism
Clinical application
Suitable for all levels of hypertension, especially for patients with hypertension such as chronic cardiac insufficiency, left ventricular hypertrophy, diabetic nephropathy, etc.
Adverse reactions
Irritating dry cough
hypotension
Allergic reactions, loss of taste, smell, hair loss
Hyperkalemia
Fetal underdevelopment during the second and third trimester of pregnancy
Enalapril
Features
Slow onset, long-lasting, powerful
Contains no sulfhydryl group and has fewer adverse reactions than captopril
Lisinopril
Fosinopril
benazepril
perindopril
cilapril
Angiotensin II receptor antagonist ARB
Mechanism
After the angiotensin Ⅱ receptor (AT1 receptor) is blocked, Ang Ⅱ's role in constricting blood vessels and stimulating the adrenal gland to release aldosterone is inhibited, resulting in lower blood pressure. It blocks Ang Ⅱ's effect on promoting cardiovascular cell proliferation and hypertrophy, and can prevent and treat heart disease. The remodeling of blood vessels can also treat congestive heart failure by reducing the afterload of the heart, which is beneficial to improving the therapeutic effect of heart failure and hypertension.
Clinical application
Suitable for patients with ventricular hypertrophy, heart failure, diabetic nephropathy, microalbuminuria or proteinuria, and patients who cannot tolerate ACEI
Losartan
Pharmacological effects
It can effectively block the combination of Ang II and AT1 receptors, reduce peripheral vascular resistance, lower blood pressure, and have a powerful and long-lasting antihypertensive effect.
When lowering blood pressure, it increases renal blood flow and glomerular filtration rate, and reverses ventricular remodeling.
Once a day, it also has the effect of promoting uric acid excretion in the kidneys
Clinical application
Various types of hypertension
Adverse reactions
Potassium-sparing diuretics and potassium supplements should be used with caution during medication
Not suitable for pregnant and lactating women
Valsartan
Long-term administration also reverses ventricular remodeling and vessel wall thickening
Candesartan
Irbesartan
Telmisartan
diuretics
Hydrochlorothiazide
Pharmacological effects
Natriuretic diuresis - reduces the Na concentration in vascular smooth muscle cells, thereby reducing intracellular Ca2 through the Na-Ca2 exchange mechanism, thereby reducing the responsiveness of vascular smooth muscle cells to vasoconstrictor substances, leading to peripheral vasodilation and a decrease in blood pressure.
Clinical application
Elderly patients with hypertension, simple systolic hypertension or heart failure
Adverse reactions
Long-term heavy use can cause hypokalemia, hyperuricemia, hyperglycemia, elevated plasma cholesterol, etc., and can increase plasma renin activity.
Indapamide
Sulfonamide diuretics
Pharmacological effects
Acts by inhibiting the reabsorption of water and electrocutin in the cortex of the distal renal tubule
Regulates calcium influx into vascular smooth muscle
Stimulates the synthesis of the vasodilatory prostaglandins PGE2 and PGI2
Reduce the sensitivity of blood vessels to vasoconstrictor substances, thereby inhibiting vasoconstriction
Clinical application
Patients with hyperlipidemia or hyperglycemia can use indapamide instead of thiazide diuretics
Adverse reactions
dose dependent
Contraindications
People allergic to sulfa
severe renal insufficiency
hepatic encephalopathy
Severe liver insufficiency
People with hypokalemia
furosemide
Spironolactone
Triamterene
Chlorthalidone
Other antihypertensive drugs
central antihypertensive drugs
Clonidine - central α2 receptor agonist
Pharmacological effects
By activating inhibitory neurons, it reduces the tone of the vasomotor center and reduces the adverse reaction functions of peripheral sympathetic nerves, thereby causing antihypertensive effects.
Clinical application
It is suitable for grade II hypertension, especially for hypertensive patients with ulcer disease and renal hypertension. It is also used to prevent migraine or control the withdrawal symptoms of morphine drugs.
Adverse reactions
Prolonged use can cause water and sodium retention
Sudden discontinuation of the drug may cause sympathetic nerve hyperactivity, headache, sweating, palpitations, and sudden increase in blood pressure due to the downregulation of receptors, which can be treated with the α-receptor antagonist phentolamine.
vasodilators
Features
Arteriolar dilating drugs - hydralazine (commonly used high blood pressure drug during pregnancy), minoxidil (often used topically for male pattern baldness and alopecia areata), diazoxide (preferred for hyperinsulinemia)
It has dilation effect on both arteries and veins-sodium nitroprusside
This class of drugs produces antihypertensive effects by relaxing vascular smooth muscle and reducing peripheral resistance.
Long-term medicinal use leads to increased peripheral resistance and water and sodium retention
sodium nitroprusside
Fast, powerful and short-lived antihypertensive medication
Intravenous drip administration directly dilates arterioles and venules, reduces peripheral vascular resistance and cardiac output, and can quickly reduce systolic and diastolic blood pressure.
It is used for hypertensive crisis, suitable for hypertensive patients with heart failure, and can also be used for acute and chronic cardiac insufficiency.
Long-term use of large amounts of medication can cure thiocyanide accumulation poisoning, causing acute psychosis and hypothyroidism. (sodium thiosulfate to the rescue)
Use with caution in patients with liver and kidney dysfunction and hypothyroidism
Sensitive to light, should be prepared and used immediately, and should be protected from light during intravenous infusion.
Noradrenergic nerve ending blocking drugs
Representative drugs-reserpine, guanethidine
reserpine
Mechanism of action: Inhibits the reuptake of NA by the vesicle membrane amine pump of sympathetic nerve terminals and prevents DA from entering the vesicles, gradually reducing and depleting NA synthesis and storage, thus blocking the transmission of sympathetic nerve impulses, dilating blood vessels and lowering blood pressure.
It is used for grade I and II hypertension. Combination with diuretics can improve the efficacy.
Common adverse reactions include sedation, drowsiness and symptoms of parasympathetic hyperactivity, such as nasal congestion, excessive gastric acid secretion, diarrhea, etc. Long-term use of large doses can cause depression. People with ulcers, those with a history of depression, and lactating women should not use it or use it with caution.
ganglion blocking drugs
Representative drugs-camimefen, mecamylamine
Pharmacological effects: Block ganglion N1 receptors, blocking both sympathetic and parasympathetic nerves
Due to many side effects, it is only used for hypertensive crisis, aortic dissection, aneurysm, controlled blood pressure reduction during surgery, etc.
Application principles
Smoothly control blood pressure
Adhere to long-term treatment
Individualized dosing
Reasonable combination of medications
Focus on protecting target organs
Actively eliminate risk factors for high blood pressure
Focus on improving patients’ quality of life
antiarrhythmic drugs
Basic functions of antiarrhythmic drugs
reduce self-discipline
Change membrane reactivity to improve conductivity
Reduce afterdepolarization and triggering activity
Change ERP and APD
Class I - sodium channel blockers
Class IA
effect
Moderately blocks Na channels, reduces the rising rate of phase 0 poles, and slows down conduction
Reduce the influx of 4-phase Na in ectopic autonomous cells and reduce their autonomy
Prolong the time required for the Na channel to return to the open state after inactivation, thereby prolonging the effective refractory period (ERP) and action potential duration (APD). Prolonging the ERp is more significant, and inhibits the activation of K and Ca2 by the cardiomyocyte membrane to varying degrees. Permeability, obvious membrane stabilization effect
Quinidine
Pharmacological effects
Moderately blocks Na channels, and high concentrations can still inhibit K outflow and Ca2 influx.
Anticholinergic effects and blockade of peripheral alpha receptors
reduce self-discipline
slow down conduction
Extended ERP
Clinical application
Broad spectrum antiarrhythmic drugs
Mainly used for cardioversion of atrial fibrillation or atrial flutter, maintenance of sinus rhythm after cardioversion and treatment of life-threatening ventricular arrhythmias.
Adverse reactions
gastrointestinal reactions
cinchona reaction
Cardiovascular Reactions - Quinidine Syncope
interaction
Combined use with digoxin can reduce the renal clearance rate of the latter and increase its plasma concentration.
Hepatic enzyme inducers such as phenobarbital can accelerate the metabolism of quinidine in the liver
Procainamide
Amide derivatives of local anesthetic procaine
Pharmacological effects
Therapeutic dose can reduce the automaticity of Purkinje fibers, reduce the maximum rate and amplitude of phase 0 rise of fast-response cell action potentials and slow down the conduction speed, turn unidirectional conduction block into bidirectional conduction block and cancel reversal activation.
High concentrations can cause hypotension by blocking ganglia
Clinical application
Broad spectrum antiarrhythmic drugs
Ventricular arrhythmias such as ventricular tachycardia
acute myocardial infarction
Adverse reactions
Oral administration may cause multiple gastrointestinal reactions, and intravenous injection may cause hypotension and intraventricular conduction block.
Anaphylaxis-Lupus Erythematosus Syndrome
Use with caution or prohibition in patients with hepatic and renal insufficiency and existing atrioventricular conduction block
disopyramide
Acts similarly to quinidine
Clinical treatment of premature ventricular contractions, supraventricular and ventricular tachycardia, and arrhythmias caused by myocardial infarction, etc.
Adverse reactions caused by multiple atropine-like effects
Long-term use may aggravate or induce heart failure
Category IB
Mildly blocks Na channels, inhibits 4-phase Na inflow, reduces self-discipline, accelerates the repolarization process by promoting K outflow, shortens ERP and APD, and shortens APD more significantly
lidocaine
Pharmacological effects
Mildly blocks Na channels and promotes K efflux
reduce self-discipline
Improve conductivity
Shortened APD and relatively prolonged ERP
Clinical application
Narrow-spectrum antiarrhythmic drugs are mainly used to treat ventricular arrhythmias. They are particularly effective in treating ventricular arrhythmias complicated by acute myocardial infarction and can be used as the drug of choice.
Prevent and treat various ventricular arrhythmias caused by cardiac glycoside poisoning, post-electroconversion, general anesthesia, etc.
Adverse reactions
central nervous system symptoms
Nystagmus is one of the early signs of lidocaine poisoning
Contraindicated in patients with severe atrioventricular block
Phenytoin
Pharmacological effects
Similar to lidocaine, it reduces Purkinje fiber automaticity and relatively prolongs ERP
It can increase the rate of phase 0 depolarization of the atrioventricular node and accelerate its conduction, so it can improve atrioventricular conduction block caused by cardiac glycoside poisoning.
Competes with cardiac glycosides for Na-K-ATPase, reduces cardiac glycoside poisoning, and inhibits delayed depolarization and triggering activities caused by cardiac glycoside poisoning.
Clinical application
Atrial and ventricular arrhythmias caused by cardiac glycoside poisoning, especially ventricular arrhythmias are more effective
Ventricular arrhythmias due to other causes
Adverse reactions
Intravenous injection too fast may cause hypotension, respiratory depression and cardiac arrhythmia
It is contraindicated in patients with existing sinus bradycardia or severe atrioventricular block and other heart diseases.
Not allowed for pregnant women
Mexiletine
It has similar effects on myocardial electrophysiology as lidocaine
It is effective in treating ventricular arrhythmias, especially acute ventricular arrhythmias after myocardial infarction.
Adverse reactions include gastrointestinal reactions, and long-term use may cause neurological symptoms, such as tremor, ataxia, diplopia, etc.
IC class
Severely blocks the Na channel in the myocardial cell membrane, reduces the rise rate and amplitude of the 0-phase action potential, significantly slows down conduction, and can also inhibit the 4-phase Na inflow and reduce self-discipline.
propafenone
Pharmacological effects
Mainly inhibits Na influx, slows down conduction velocity, reduces the automaticity of Purkinje fibers, and prolongs APD and ERP
It has certain β-receptor antagonism and calcium channel blocking effects, which can inhibit myocardial contractility to a certain extent.
Clinical application
Supraventricular or ventricular premature contractions and tachycardia, etc., have good curative effect on arrhythmias caused by coronary heart disease and hypertension.
Adverse reactions
gastrointestinal reactions
Causes cardiovascular system reactions such as atrioventricular block and orthostatic hypotension, and can also aggravate heart failure
Flecainide
Pharmacological effects
Blocking Na channels has a strong effect, which can significantly slow down the maximum rise rate of phase 0 of myocardial cells and slow down conduction, inhibit the influx of phase 4 Na and reduce automaticity.
Block K channels and prolong APD of atrial and ventricular myocardium
Clinical use
Treatment of refractory or life-threatening arrhythmias
Adverse reactions
Cause fatal arrhythmias, which can lead to ventricular tachycardia or ventricular fibrillation, atrioventricular block, induce reentrant arrhythmias, and increase the mortality rate of patients after myocardial infarction.
Class II-β-adrenoceptor antagonists
Blocking β-receptors antagonizes the influence of noradrenergic nerves on the heart. It can also block Na channels, promote K outflow, relatively or absolutely prolong ERP, and has anti-myocardial ischemia effects.
propranolol
Pharmacological effects
reduce self-discipline
slow down conduction
Clinical application
Treatment of supraventricular and ventricular arrhythmias
Drug of choice for sinus tachycardia
Adverse reactions
Can cause sinus bradycardia, atrioventricular block, hypotension, etc., and can induce heart failure and asthma
Use with caution in patients with hyperlipidemia and diabetes
Category III-drugs that prolong action potential duration
Potassium channel blockers can block voltage-dependent potassium channels, prolong APD and ERP, and have a good preventive and therapeutic effect on ventricular fibrillation.
Amiodarone
Pharmacological effects
Blocking K channels can significantly prolong the APD and ERP of the atrioventricular node, atrial myocardium, and ventricular myocardium, which is beneficial to eliminating discounted excitement.
Blocks Na channels and Ca2 channels to slow down the conduction of the atrioventricular node and reduce the self-discipline of the sinoatrial node.
Block α and β receptors, dilate blood vessels, and reduce myocardial oxygen consumption.
Clinical application
Broad-spectrum antiarrhythmic drug, effective against both supraventricular and ventricular arrhythmias
Adverse reactions
Cardiovascular system reactions such as sinus bradycardia, atrioventricular block, hypotension, Q-T interval prolongation, and even cardiac insufficiency can be seen.
Corneal brown particle deposition
interstitial pneumonia or pulmonary fibrosis
Sotalol
Non-selective β-receptor antagonist and blocks K channels
Reduce automaticity, slow down atrioventricular node conduction, and prolong ERP and APD
It is clinically used to treat various severe ventricular arrhythmias, as well as paroxysmal supraventricular tachycardia and atrial fibrillation.
A small number of patients with prolonged Q-T interval may occasionally develop torsade de pointes during use.
Class IV-calcium channel blockers
Verapamil
Pharmacological effects
Blocks Ca2 channels in myocardial cell membranes, inhibits Ca2 influx, and mainly acts on slow-reacting cells in the sinoatrial node and atrioventricular node, which can reduce automaticity, slow down conduction, prolong ERP, and eliminate reentry.
Clinical application
Drug of choice for paroxysmal supraventricular tachycardia
Used to slow the ventricular rate in atrial fibrillation or atrial flutter
Adverse reactions
Hypotension, severe cases or too fast injection rate can lead to bradycardia, atrioventricular block or even heart failure
It is prohibited to be used in patients with II or III degree atrioventricular block, hypotension, cardiac insufficiency and cardiogenic shock.
diltiazem
It is mainly used for supraventricular arrhythmias, such as paroxysmal supraventricular tachycardia and frequent premature atrial contractions, and is also effective for paroxysmal atrial fibrillation.
There is an obvious first pass effect
Tachyarrhythmic drugs
Sinus tachycardia should be treated with beta-receptor antagonists or verapamil
Amiodarone, sotalol or quinidine should be used to correct atrial fibrillation and maintain sinus rhythm.
Verapamil is the first choice to control paroxysmal supraventricular tachycardia, but propranolol, amiodarone, propafenone, etc. can also be used
If ventricular presystole is caused by acute myocardial infarction, lidocaine should be used, and if it is caused by cardiac glycoside poisoning, phenytoin should be used.
Ventricular tachycardia is often treated with intravenous lidocaine
For ventricular fibrillation, lidocaine, amiodarone, and procainamide should be administered intravenously.
Ventricular tachycardia or ventricular fibrillation caused by acute myocardial infarction or cardiac glycoside poisoning should be treated with phenytoin or lidocaine.
Anti-chronic cardiac insufficiency drugs-congestive heart failure CHF
Drugs with positive inotropic properties
cardiac glycosides
Mainly extracted from digitalis plants
Representative medicine
digoxigenin
Digoxin
Trinoside-Cidilan
Trichoside K
Pharmacological effects
Positive inotropic effect (increase myocardial contractility)
Increase the rate of myocardial contraction
Reduce oxygen consumption in failing heart
Increase output in failing heart
negative frequency effect
Cardiac glycosides increase myocardial contractility, increase cardiac output, reflexively excite the vagus nerve, slow down the heart rate, and reduce myocardial oxygen consumption.
negative conduction
Therapeutic amounts of cardiac glycosides slow down the atrioventricular node and Purkinje fiber conduction by exciting the vagus nerve, prolonging the refractory period, but shortening the refractory period of the atria.
Cardiac glycosides have diuretic and vasodilatory effects on patients with CHF. Its diuretic effect can reduce blood volume and reduce the burden on the heart.
Mechanism
The therapeutic amount of cardiac glycoside inhibits Na-K-ATPase on the myocardial cell membrane, reducing Na-K exchange and increasing Na-Ca2 exchange, thereby increasing Ca2 influx, resulting in an increase in Ca2 in myocardial cells and strengthening myocardial contractility.
Toxic doses of cardiac glycosides severely inhibit Na-K-ATPase, causing intracellular K loss and making the maximum negative value of diastolic potential smaller, resulting in increased myocardial cell automaticity and easily causing arrhythmia.
Clinical application
chronic cardiac insufficiency
Best effect on CHF accompanied by atrial fibrillation and accelerated atrial rate
Ineffective for CHF caused by mechanical obstructive lesions, such as constrictive pericarditis and severe mitral stenosis
certain cardiac arrhythmias
atrial fibrillation
atrial flutter
paroxysmal supraventricular tachycardia
Adverse reactions
Drug safety range is small
gastrointestinal symptoms
Neurological symptoms and visual abnormalities are precursors of cardiac glycoside poisoning
Cardiac reaction, the most serious toxic reaction, a heart rate below 60 beats/min is a precursor to poisoning
Prevention and treatment of poisoning
Various predisposing factors leading to poisoning should be corrected first, such as hypokalemia, hypomagnesemia, hypercalcemia, hypoxia and acidosis, etc.
Identify the signs of poisoning and indications for discontinuation, and if necessary, monitor the blood concentration of cardiac glycosides to avoid poisoning.
① Stop medications promptly, including potassium-depleting diuretics, and switch to potassium-sparing diuretics if necessary
② Appropriate supplementation of potassium. Potassium chloride can compete with cardiac glycosides for Na-K-ATPase and reduce the binding of cardiac glycosides to the enzyme. In mild cases, it can be taken orally. In severe cases, intravenous drip can be used. Potassium salts cannot be used.
③Tachyarrhythmia: Phenytoin is effective in treating tachyarrhythmia caused by cardiac glycoside poisoning. Lidocaine is used to rescue severe ventricular tachycardia and ventricular fibrillation caused by cardiac glycoside poisoning. For severe poisoning, digoxin antibody Fab fragment can be used
④Brady arrhythmia: Patients with bradycardia and atrioventricular block can be treated with atropine
drug administration
First, use the full effective dose to basically control the symptoms of heart failure and then maintain the efficacy. This method causes a high incidence of cardiac glycoside poisoning.
The daily constant dose administration method has a low incidence of poisoning and is suitable for patients with chronic, mild symptoms and those prone to poisoning.
interaction
Glucocorticoids and potassium-depleting diuretics can cause hypokalemia and induce cardiac glycoside poisoning. When combined with cardiac glycosides, attention should be paid to potassium supplementation.
Quinidine can displace digoxin from tissues and double the blood concentration of digoxin. If the two are used together, the dosage of digoxin should be reduced.
Amiodarone, verapamil, propafenone, erythromycin, etc. can also increase the blood concentration of digoxin, so be careful to reduce the dosage when used together.
Calcium and cardiac glycosides have a synergistic effect, and their combined use increases toxicity.
Non-cardiac glycoside inotropes
sympathomimetic drugs
Produces positive inotropic and vasodilatory effects respectively through the β1 receptors in the cardioexcitable heart and the β2 receptors and DA receptors on vascular smooth muscle.
ibopamin
By stimulating dopamine receptors and β-receptors, it relaxes renal blood vessels and increases renal blood flow to produce significant diuretic effects; it has positive inotropic effects and increases cardiac output; it relaxes peripheral blood vessels and reduces cardiac afterload.
Used to treat and relieve symptoms of heart failure and improve exercise tolerance
Dobutamine
Mainly stimulates β1 receptors, can increase myocardial contractility, increase cardiac output, reduce peripheral vascular resistance, increase urine output, and have little impact on heart rate.
For acute myocardial infarction or cardiac surgery complicated by cardiac insufficiency and chronic refractory heart failure
Phosphodiesterase inhibitors
Mechanism
By inhibiting the activity of phosphodiesterase III, reducing cAMP degradation and increasing intracellular cAMP levels
Increased cAMP content in myocardial cells can produce positive inotropic effects, and increased cAMP in vascular smooth muscle cells can relax vascular smooth muscles and dilate blood vessels.
Aminrinone
Non-glycoside, non-catecholamine cardiotonic drug with both positive inotropic and vasodilatory effects
Increase myocardial contractility, increase cardiac output, reduce cardiac pre- and afterload, reduce left ventricular filling pressure, improve left ventricular function, increase cardiac index, but have no significant effect on arterial pressure and heart rate, and generally do not cause arrhythmia
It is suitable for the short-term treatment of acute and chronic refractory congestive heart failure caused by various reasons where digitalis, diuretics, and vasodilators are ineffective or ineffective.
It is now limited to intravenous injection for heart failure that is ineffective in other treatments.
Milrinone
It can significantly improve cardiac systolic and diastolic functions, relieve symptoms, and improve exercise endurance.
For short-term intravenous administration only in patients with severe CHF
It has an adverse effect on the patient's survival, so long-term medication is not recommended.
Renin-angiotensin-aldosterone system inhibitors
angiotensin-converting enzyme inhibition
Pharmacological effects
Inhibiting angiotensin I converting enzyme reduces the production of Ang II and the release of aldosterone, which can reduce the sodium and water retention caused by this.
It can reduce peripheral vascular resistance, dilate coronary arteries, reduce left ventricular filling pressure and ventricular wall tension, and increase renal blood flow, etc., improve cardiac function, and relieve symptoms of CHF.
Inhibit cardiac hypertrophy, vascular proliferation and ventricular remodeling
Representative medicine
Captopril
Enalapril
Ramipril
Lisinopril
perindopril
Angiotensin II receptor antagonists
The effect is similar to that of ACEI, but without the non-reaction of ACEI
Losartan, Irbesartan, etc.
aldosterone antagonists
Spironolactone
A weak diuretic that conserves potassium and eliminates sodium
Antagonizing aldosterone reduces or reverses cardiovascular remodeling in CHF and can reduce the morbidity and mortality of CHF.
It can be used in combination with chlorothiazide, ACEI or Ang II receptor antagonists to treat CHF.
Cardiac load-reducing medicine
diuretics
Promote the excretion of sodium and water, reduce blood volume, reduce the preload and afterload of the heart, eliminate or relieve venous congestion and the pulmonary edema and peripheral edema caused by it
For mild or moderate cardiogenic edema, thiazide diuretics are used. Hydrochlorothiazide is commonly used, and can be combined with potassium-sparing diuretics.
For severe CHF, high-potency diuretics such as furosemide should be administered intravenously.
vasodilators
Produces prescription effect by dilating venules or arterioles, adjuvant drug for CHF
Only for the treatment of refractory CHF that is refractory to cardiac glycoside and diuretic therapy.
Common adverse reactions-sodium and water retention
Main arteriole dilation drugs: hydralazine, nifedipine, amlodipine
Main venous dilation drugs: nitrates
Drugs that dilate arterioles and venules: sodium nitroprusside, prazosin
beta receptor antagonists
Mechanism
Block β1 receptors, reduce sympathetic tension, inhibit the toxic effects of catecholamines on the heart, slow down the heart rate, reduce cardiac load, reduce myocardial oxygen consumption, and increase cardiac output.
Inhibit the renin-angiotensin-aldosterone system, reverse ventricular remodeling, and further improve cardiac function
Long-term use can upregulate myocardial β1 receptors, increase the sensitivity of β1 receptors to catecholamines, and improve myocardial contractility.
Clinical application
Chronic systolic heart failure, patients with NYHA cardiac function class II or III, LVEF <40% and stable condition
Treatment principles
No contraindications to beta-antagonists
Combined with other anticardiac insufficiency drugs
Start with a low dose and gradually increase the dose
If symptoms of cardiac insufficiency worsen, the dose should be reduced
Adverse reactions
It has inhibitory effect on the heart. It is contraindicated in patients with CHF accompanied by bronchial asthma and atrioventricular block.
Antianginal and antiatherosclerotic drugs
anti-angina pectoris
concept
Angina pectoris - a common symptom of ischemic heart disease, is a syndrome of acute, temporary ischemia and hypoxia in the myocardium caused by insufficient coronary blood supply.
Pathophysiological mechanisms of angina pectoris
The balance between myocardial oxygen demand and oxygen supply is imbalanced, resulting in temporary myocardial ischemia and hypoxia. Myocardial anaerobic metabolism increases, producing a large amount of metabolites such as lactic acid, pyruvate, histamine, K, etc., which stimulate nerve endings and cause pain.
Classification
Nitrates
Nitroglycerin
sublingually
Pharmacological effects
Relax smooth muscle, especially vascular smooth muscle, dilate veins, arteries and coronary blood vessels, reduce myocardial oxygen consumption and increase myocardial oxygen supply
Increase blood supply to myocardial ischemic area
Clinical application
Angina pectoris, the drug of choice for stable angina pectoris, is taken sublingually to control acute attacks of angina pectoris. For unstable angina pectoris, intravenous administration should be used, supplemented by aspirin and other other therapeutic drugs.
acute myocardial infarction
cardiac insufficiency
Adverse reactions
It is contraindicated in patients with throbbing headache, elevated intracranial pressure, craniocerebral injury, and intracranial hemorrhage.
Facial flushing, which may cause orthostatic hypotension and syncope in severe cases
Dilation of blood vessels in the eye can increase intraocular pressure, so patients with glaucoma should use with caution
Excessive dosage causes blood vessels to dilate significantly, lowers blood pressure, reflexively causes sympathetic nerve excitement, accelerates heart rate, and strengthens myocardial contractility. On the contrary, it can increase oxygen consumption and aggravate angina pectoris attacks.
Methemoglobinemia
Tolerance
Isosorbide dinitrate
It is mainly used orally for the prevention of angina pectoris and the long-term treatment of heart failure after myocardial infarction.
Isosorbide mononitrate
Prevent angina pectoris, more effective than isosorbide dinitrate
beta receptor antagonist
propranolol
Pharmacological effects
Reduce myocardial oxygen consumption
Increase blood supply to ischemic area
Improve myocardial metabolism
....increase tissue oxygen supply,....improve myocardial blood circulation
Clinical application
stable angina
unstable angina
variant angina
Propranolol combined with nitrates in the treatment of angina pectoris
Nitrates cause accelerated heart rate and enhanced myocardial contractility by dilating blood vessels, and their effect of increasing myocardial oxygen consumption can be weakened by propranolol's effect of slowing down the heart rate and inhibiting myocardial contractility.
The effect of propranolol on increasing ventricular volume leading to increased oxygen consumption may also be offset by the effect of nitrates on reducing ventricular volume.
However, since both types of drugs have antihypertensive effects, if the dose is too high, blood pressure will drop significantly, coronary perfusion pressure will decrease, coronary blood flow will decrease, and angina attacks will be aggravated. Therefore, the dosage should be reduced when used together.
Adverse reactions
cardiac↓inhibition
Inducing and aggravating bronchial asthma
After long-term use, the dose should be gradually reduced and discontinued. If discontinued suddenly, it may aggravate angina or induce myocardial infarction.
calcium channel blockers
Representative medicine
Verapamil
nifedipine
diltiazem
Niqun Diping
amlodipine
Pharmacological effects
Reduce myocardial oxygen consumption
Increase blood supply to myocardium
Protect ischemic cardiomyocytes
Clinical application
Effective for all types of angina pectoris, especially for variant angina pectoris.
Nifedipine has a strong effect on dilating coronary arteries and is the first choice for variant angina pectoris.
Verapamil has a strong inhibitory effect on the heart, a weak dilation effect on blood vessels, and is effective in treating exertional angina.
Anti-atherosclerosis
Lipid-adjusting drugs
LDL↑ TC↑ TG↑
lipoprotein type
density
ChylomicronsCM
very low density lipoprotein vLDL
low density lipoprotein LDL
intermediate density lipoprotein IDL
HDL
Lipoprotein a-Lpa
Element
free cholesterol FC
Cholesterol Ester CE
Triglycerides TG
Phospholipid pL
Combines with apolipoprotein to form lipoprotein
Drugs that affect cholesterol absorption
Bile acid sequestrants
Representative medicine
Cholestyramine
colestipol
Pharmacological effects
It performs ion exchange with cholic acid in the form of chloride ions to form bile acid chelates that are not absorbed and are excreted with the feces, hindering the enterohepatic circulation of cholic acid, thus inhibiting the absorption of cholesterol in the intestine and promoting the conversion of cholesterol into cholic acid. Transformed, lowering blood LDL and cholesterol levels
Clinical application
Mainly used for hypercholesterolemia with elevated total cholesterol and LDL
Effective for heterozygous familial hyperlipidemia
Often used in combination with clofibrate or probucol to produce synergistic effects
Adverse reactions
gastrointestinal reactions
Long-term use may cause steatorrhea and affect the absorption of fat-soluble vitamins and folic acid, so supplementation should be noted.
Mainly drugs that lower triglycerides
Phenoxy acids-fibrates
Clofibrate
Pharmacological effects
Activate lipoprotein lipase to promote the breakdown of very low-density lipoprotein VLDL and triglycerides in the blood
Mildly inhibits the synthesis of cholesterol in the liver, significantly reduces triglycerides and VLDL in the blood, and slightly lowers cholesterol.
Long-term use can also reduce plasma fibrinogen content and platelet adhesion, and can reduce the formation of thrombus.
Clinical application
For the treatment of hyperlipidemia with elevated triglycerides and VLDL
Adverse reactions
gastrointestinal reactions
Skin allergies
Myositis-like syndrome, combined with statins, increases the incidence of myopathy
Abnormal liver function and changes in renal function
Disable
Pregnant and lactating women
People with liver and kidney dysfunction
gemfibrozil
bezafibrate
fenofibrate
Niacin
niacin
Pharmacological effects
Can inhibit liver synthesis of triglycerides and VLDL, thereby reducing LDL levels
Promote cholesterol excretion through bile and prevent cholesterol esterification
Moderately elevated high-density lipoprotein HDL levels
Clinical application
Broad spectrum lipid regulating drug
Anti-atherosclerosis and coronary heart disease
Adverse reactions
Gastrointestinal tract irritation symptoms and aggravation of peptic ulcers
Dilated blood vessels in the skin can cause skin rashes, itching, etc.
Large doses can cause increases in blood sugar and uric acid, and long-term use can cause abnormal liver function.
For long-term use, blood sugar, liver and kidney function should be checked regularly
Disable
peptic ulcer
gout
diabetics
acipimox
Nicotinic acid isomers
Inhibiting the lipolysis of adipose tissue is stronger and more lasting, which can improve fasting blood sugar and glucose tolerance in diabetic patients without causing an increase in uric acid.
Treatment of hyperlipidemia in patients with type 2 diabetes or gout
Hydroxymethylglutarate CoA reductase inhibitor-statins
It is effective if taken with dinner
Lovastatin
Pharmacological effects
Competitively inhibits the activity of HMG-COA reductase, lowers blood cholesterol and LDL, can also reduce the synthesis of VLDL, and can also slightly increase HDL
Clinical application
mixed hyperlipidemia
Treatment of type 2 diabetes accompanied by multiple lipoprotein metabolism abnormalities, especially in patients with excessive serum LDL-cholesterol (LDL-C) and VLDL levels
Protect and improve kidney function to a certain extent
Adverse reactions
Mild gastrointestinal reaction
rhabdomyolysis
Hepatitis and angioedema
Use with caution if you have a history of liver disease, and use with caution if you are pregnant or breastfeeding.
Simvastatin
pravastatin
Antioxidants
Excessive oxidation and oxygen free radicals can promote the formation and development of atherosclerosis
Probucao
Taking medication immediately after a meal can increase absorption
Pharmacological effects
It can reduce total serum cholesterol, LDL-C and HDL-C. As a powerful antioxidant, it can inhibit LDL oxidation and prevent the formation of oxidized LDL and its atherosclerotic effect.
Clinical application
Mainly used in combination with other hypolipidemic drugs to treat hypercholesterolemia and prevent the formation of atherosclerosis.
Adverse reactions
Gastrointestinal inversion, headache, dizziness, abnormal liver function, etc.
It is contraindicated for those with recent myocardial injury.
ECG should be monitored regularly during medication
Not suitable for pregnant women and children
polyene fatty acids
Representative medicine
Vegetable oil has weak lipid-lowering effect
Marine animal fats and oils contain polyunsaturated fatty acids. Long-term use can prevent the formation of atherosclerosis and reduce plaques.
Pharmacological effects
Lowering triglycerides in plasma can slightly increase HDL, but plasma total cholesterol and LDL levels may increase, inhibit platelet aggregation, reduce blood viscosity, reduce the inflammatory response of plaques, stabilize plaques, and make them Less prone to spontaneous rupture, reducing the occurrence of cardiovascular events
Drugs that protect arterial endothelial cells
sulfated polysaccharide
Representative medicine
Heparin, chondroitin sulfate A, dextran sulfate
Pharmacological effects
It has a large amount of negative charge and binds to the surface of vascular endothelium to prevent the adhesion of white blood cells, platelets and harmful factors, protect the vascular endothelium from damage, inhibit the proliferation of vascular smooth muscle cells, and prevent restenosis.
Clinical application
Ischemic cardiovascular and cerebrovascular diseases and restenosis after percutaneous coronary angioplasty (PTCA)
Diuretics and dehydration drugs
diuretics
High potency diuretics
Mainly acts on the thick ascending branch of the medullary loop, reducing Na reabsorption by 15%-25%, and has a strong diuretic effect
Furosemide
Pharmacological effects
diuretic
dilate blood vessels
Clinical application
severe edema
acute pulmonary edema and cerebral edema
acute renal failure
Accelerate the elimination of poisons
hypercalcemia
Adverse reactions
Fluid and electrolyte disorders-hypokalemia-hyperuricemia
Hearing Impairment-Ototoxicity
gastrointestinal reactions
interaction
Epinephrine, mineralocorticoids, adrenocorticotropic hormone and estrogen can reduce the diuretic effect of this drug and increase the chance of hypokalemia.
Nonsteroidal anti-inflammatory drugs can reduce the diuretic effect of this drug and increase the chance of kidney damage.
Combined use with amphotericin B, cephalosporins, aminoglycosides and other antibiotics may increase nephrotoxicity and ototoxicity
Combined use with barbiturates and anesthetics may easily cause orthostatic hypotension
Combined with oral anticoagulants to enhance anticoagulant effect
Increase the heart's sensitivity to cardiac glycosides, easily causing poisoning
bumetanide
The intensity of action is 20-60 times that of furosemide, and is used to treat various types of severe edema and acute pulmonary edema.
Adverse reactions are similar to those of furosemide. Unmarried men occasionally experience spermatorrhea and difficulty in penile erection.
Large doses may cause muscle soreness and chest pain
Torasemi
ethacrynic acid
Azosemi
Piretanide
Medium potency diuretics
Mainly acts on the cortex of the thick ascending branch of the medullary loop and the beginning of the distal convoluted tubule, reducing Na reabsorption by 5% to 10%, and has a moderate diuretic effect.
Hydrochlorothiazide
Pharmacological effects
diuretic
step down
antidiuretic
Clinical application
Edema, good effect on mild and moderate cardiogenic edema
hypertension
diabetes insipidus
Adverse reactions
Electrolyte imbalance-hypokalemia
hyperuricemia
high blood sugar
fat metabolism disorder
Occasionally allergic reactions, gastrointestinal reactions, granulocytopenia, thrombocytopenia, etc.
interaction
Hypokalemia may increase the toxicity of cardiac glycosides, so potassium supplementation is recommended when used in combination with cardiac glycosides.
Combined use with glucocorticoids and amphotericin B may increase the incidence of hypokalemia
Due to increased blood sugar, attention should be paid to adjusting the dosage of hypoglycemic drugs when used in combination with hypoglycemic drugs.
NSAIDs may reduce the diuretic effect of these drugs
Indapamide
Chlorthalidone
low potency diuretics
Mainly acts on the end of the distal convoluted tubule and collecting duct, reducing Na reabsorption by 1% to 3%, and has a weak diuretic effect
Spironolactone
Pharmacological effects
It can compete with aldosterone for aldosterone receptors in distal convoluted tubule and collecting duct cells, antagonize the potassium-excreting and sodium-retaining effect of aldosterone, and promote the excretion of sodium and water.
Clinical application
Refractory edema associated with elevated aldosterone, such as congestive heart failure, cirrhosis, ascites, and nephrotic syndrome
Often combined with potassium-excreting diuretics, it can enhance the diuretic effect and prevent hypokalemia caused by potassium-excreting diuretics.
Adverse reactions
Electrolyte imbalance-hyperkalemia is the most common
hormone imbalance
triamterene, amiloride
Both drugs mainly act on the distal convoluted tubules and collecting ducts, blocking sodium channels, reducing Na reabsorption and K secretion, increasing Na excretion and becoming diuretic.
Long-term use may easily cause hyperkalemia. Use with caution in patients with renal insufficiency. Disabled in patients with hyperkalemia.
Inhibits dihydrofolate reductase, causing folic acid deficiency, and may easily cause megaloblastic anemia in patients with cirrhosis.
Acetazolamide, dichlorphenamide
Both drugs produce weak diuretic effects by inhibiting carbonic anhydrase and are no longer used as diuretics.
Inhibits leg carbonic anhydrase, reduces the production of HCO3-, thereby reducing the production of aqueous humor and lowering intraocular pressure. It is mainly used clinically to treat glaucoma.
There may be drowsiness, numbness in the face and limbs, and long-term use may cause hypokalemia, metabolic acidosis, etc.
dehydration medicine
Also known as osmotic diuretics
Mechanism
Most of them are not easily metabolized in the body. After intravenous injection, they can increase plasma osmotic pressure and cause tissue dehydration.
It is not easily reabsorbed when passing through the kidneys, and can increase the excretion of water and some ions, resulting in osmotic diuresis.
Mannitol
Pharmacological effects
After intravenous administration, it can rapidly increase plasma osmotic pressure, causing inter-tissue water to transfer to the plasma, causing tissue dehydration. Injecting 100g of mannitol can transfer water in 2000ml of cells to the outside of the cells.
After filtration from the glomerulus, it is not reabsorbed by the renal tubules and forms hypertonicity in the renal tubular lumen, reducing the reabsorption of Na and water.
It can also dilate renal blood vessels, increase renal blood flow, and increase glomerular filtration rate.
Clinical application
acute renal failure
Cerebral edema and glaucoma
Adverse reactions
Drug leakage, local tissue necrosis, swelling and pain
Injecting too quickly can cause one-time headaches, dizziness, blurred vision, etc.
Use with caution in patients with cardiac insufficiency, and contraindicated in patients with active intracranial hemorrhage.
Sorbitol
Mannitol isomers
It can be used as a 25% hypertonic solution, which is weaker than mannitol.
glucose
Intravenous injection of hypertonic sugar can produce dehydration and osmotic diuresis
When used alone for cerebral edema, there may be a "rebound" phenomenon, and it can generally be used interchangeably with mannitol.
Other drugs that act on the urinary system
sodium bicarbonate
Can accelerate the excretion of weakly acidic drugs such as barbiturates and salicylates from the kidneys
Can increase the solubility of sulfa drugs and reduce their toxicity to the kidneys
Can enhance the effectiveness of antibiotics such as gentamicin on urinary tract infections.
It can directly increase the body's alkali reserve, increase the concentration of HCO3- in the plasma, and neutralize H, thus correcting acidosis.
By alkalinizing the extracellular fluid, K in the serum can be transferred into the cells, thereby reducing serum potassium and used to treat hyperkalemia.
antidiuretic hormone-vasopressin
By increasing the permeability of collecting duct epithelial cells, it increases water reabsorption, reduces urine output, increases urine osmotic pressure, and produces significant antidiuretic effects. It is used for central diabetes insipidus, head surgery or trauma. Treatment of temporary diabetes insipidus
For the treatment of esophageal variceal bleeding and hemoptysis
Drugs that act on the blood system and hematopoietic system
anti-anemia drugs
Anemia classification
iron deficiency anemia
megaloblastic anemia
aplastic anemia
iron supplement
Representative medicine
ferrous sulfate
Ferrous fumarate
Ferric ammonium citrate
Ferrous gluconate
iron dextran
Pharmacological mechanism
Iron is absorbed in the form of Fe2, and the absorption sites are in the duodenum and upper jejunum.
After iron is absorbed into the bone marrow, it enters the bone marrow young red blood cells, combines with protoporphyrin in the mitochondria to form heme, and then combines with globin to form hemoglobin, thereby promoting the maturation of red blood cells.
Clinical application
iron deficiency anemia
Patients with severe anemia need to take medication continuously for several months
After gastrectomy
Chronic nephritis requires taking ferrous sulfate
Adverse reactions
Gastrointestinal irritation
Long-term use may cause constipation and black stools
Acute Poisoning-Desferrioxamine Detoxification
Vitamins
folic acid
Pharmacological effects
After absorption, it is first reduced to dihydrofolate by folate reductase, and then reduced to tetrahydrofolate by dihydrofolate reductase to participate in metabolism.
Clinical application
Megaloblastic anemia caused by folic acid deficiency due to various causes
It has good effect on nutritional, pregnancy and infancy megaloblastic anemia, and can prevent neural tube defects.
Supplementing with VB12, VB6, and VC can improve the efficacy
Adverse reactions
Occasionally, allergic reactions may occur, and gastrointestinal symptoms may occur during long-term use.
Can cause yellow urine when taken in large amounts
VB12
Pharmacological effects
Promote recycling of tetrahydrofolate
Maintains functional integrity of sheathed nerve fibers
Clinical application
Pernicious anemia, also assists in the treatment of megaloblastic anemia
Adjuvant treatment for neurological diseases such as neuritis, nerve atrophy, trigeminal neuralgia, sciatica - can reduce the production of toxic substances
Adverse reactions
Rarely, anaphylactic shock occurs
Hemostatic drugs
Hemostatic drugs that promote the production of clotting factors
Drugs that promote coagulation factor activity
VK
Pharmacological effects
Procoagulant effect
Relieves smooth muscle spasm
Clinical application
For the treatment of bleeding caused by vk deficiency
Relieves pain caused by smooth muscles in the gastrointestinal tract
Adverse reactions
Intramuscular injection can cause local redness, swelling and pain
VK3 is prone to hyperbilirubinemia and hemolysis in newborns, especially premature infants
coagulation factor preparations
thrombin
It is suitable for bleeding of small blood vessels, capillaries and solid organs that are difficult to ligate. It can also be used to stop bleeding in trauma surgery, oral cavity, urinary tract and digestive tract.
Gastrointestinal hemostatic drugs should be taken orally or by infusion. It is strictly prohibited to give them by injection, otherwise they may lead to thrombosis, local necrosis and life-threatening consequences.
prothrombin complex
Treatment of bleeding caused by hemophilia B, severe liver disease, overdose of oral coumarin anticoagulants, and deficiency of VK-dependent coagulation factors
antihemophilic globulin
Mainly used for the treatment of hemophilia A, but also for acquired coagulation VIII deficiency caused by severe liver disease, DIC and systemic lupus erythematosus.
antifibrinolytic drugs
benzoic acid
Pharmacological effects
Competitively inhibits the action of plasminogen activator, preventing plasminogen from being activated into plasmin, thus inhibiting fibrinolysis and achieving hemostatic effect.
Clinical application
Prevent and treat bleeding caused by hyperfibrinolysis, such as abnormal bleeding after surgery on the uterus, thyroid, prostate, liver, spleen and other organs.
Adverse reactions
Excessive dosage can cause thrombosis and induce myocardial infarction, so it is forbidden or used with caution in those who have a tendency to form thrombosis or have a history of vascular embolism.
tranexamic acid
It has the same effect as tranzoic acid and has strong hemostatic effect, but has many adverse reactions.
Procoagulant drugs that act on blood vessels
Hemostasis is achieved by constricting arterioles, venules and capillaries to slow blood flow.
Pituitaryin
Contains oxytocin and vasopressin
Drugs that promote platelet production
phenolsulfonethylamine
It is used to prevent bleeding caused by increased capillary fragility, insufficient platelet function and other reasons. It can also prevent and treat excessive bleeding during surgery.
Can be used together with VK and aminotoluic acid
anticoagulants
Internal and external anticoagulants
heparin
Pharmacological effects
Enhance the anticoagulant effect of antithrombin III
Anti-atherosclerotic effect
Anti-infection, reduce blood viscosity
Clinical application
Prevention and treatment of thromboembolic diseases
Treatment of disseminated intravascular coagulation DLC
Can be used for cardiac catheterization, cardiovascular surgery, extracorporeal circulation, hemodialysis, organ transplantation, etc. to prevent blood coagulation
Adverse reactions
Spontaneous bleeding and severe bleeding require slow intravenous injection of protamine sulfate to counteract it. 1mg of protamine can neutralize 100u of heparin, and the dosage at one time cannot exceed 50mg.
Allergic reactions are occasionally seen, and long-term use can cause hair loss, osteoporosis and spontaneous fractures.
Contraindications
It should not be used by those who are allergic to heparin, have liver and kidney dysfunction, gastroduodenal ulcers, cerebral hemorrhage, severe hypertension, threatened abortion, hemophilia, subacute bacterial endocarditis, and after surgery.
interaction
Combined use with alkaline drugs will lose anticoagulant activity
The combined use of aspirin, NSAIDs, dextran, and dipyridamole may increase the risk of bleeding.
Combined use with adrenocortical hormones and ethacrynic acid may cause gastrointestinal bleeding
Concomitant use with insulin or sulfonylureas may result in hypoglycemia
low molecular weight heparin
Features
Strong inhibitory effect on Xa, weak inhibitory effect on IIa
Strong antithrombotic effect, weak anticoagulant effect
once a day
less bleeding
Treats venous thrombosis and prevents thrombosis after surgery in high-risk patients. It is also effective in unstable angina and acute myocardial infarction.
enoxaparin
ultra low molecular weight heparin
Anticoagulants in the body
Coumarins
Pharmacological effects
It can competitively antagonize the effect of VK and inhibit the synthesis of coagulation factors such as II, VII, IX, and X, thereby producing anticoagulant effects.
Clinical application
Prevention and treatment of thromboembolic diseases, such as venous thromboembolism, pulmonary embolism, etc.
Adverse reactions
Oral overdose can easily cause spontaneous bleeding, which can be counteracted by vk. If necessary, fresh plasma or whole blood can be transfused.
It has teratogenic effects and is contraindicated in early pregnant women.
interaction
Liver enzyme inhibitors, drugs with high plasma protein binding rates, and broad-spectrum antibiotics can increase the anticoagulant effect of coumarins
Hepatic enzyme inducers and oral contraceptives may reduce the anticoagulant effect of coumarins
extracorporeal anticoagulants
sodium citrate
For extracorporeal anticoagulation only
When used to preserve fresh blood, 10ml of 2.5% sodium citrate is generally added to every 100ml of blood.
Excessive or rapid transfusion of blood containing this drug may cause hypocalcemia, leading to cardiac insufficiency, which should be corrected by intravenous injection of calcium chloride if necessary.
Thrombolytic drugs
antiplatelet drugs
dipyridamole
By inhibiting the activity of platelet phosphodiesterase, reducing the hydrolysis of cAMP into 5-AMP, increasing adenosine content, activating adenosine cyclase, and increasing the cAMP content in platelets
Use with aspirin to prevent thrombotic diseases and with warfarin to prevent thrombosis after cardiac surgery
prostacyclin
Used for extracorporeal circulation to prevent thrombosis and requires intravenous drip
Ticlopidine
For use in arterial thromboembolic disease, especially in patients who are not suitable for aspirin treatment
Adverse reactions - gastrointestinal reactions
abciximab
Used to treat unstable angina, acute myocardial infarction and other serious patients
Risk of bleeding
Fibrinolytic drugs-thrombolytic drugs
Streptokinase
Can combine with plasminogen to form a complex, activate plasminogen to convert into plasmin, and promote fibrinolysis
Mainly used for acute thromboembolic diseases, such as acute pulmonary thrombosis, deep vein thrombosis and early treatment of myocardial infarction.
The best effect is achieved when thrombosis does not occur for more than 6 hours.
Adverse reactions include allergic reactions and bleeding (can be stopped by tranzoic acid)
Contraindicated in bleeding disorders, gastroduodenal ulcers, severe hypertension, post-surgery or childbirth, streptococcal infections, etc.
Urokinase
Can directly activate plasminogen to convert into plasmin, resulting in thrombolytic effect
anistreplase
Used for acute myocardial infarction, it can improve symptoms and reduce mortality
Adverse reactions include injection site and gastrointestinal bleeding, transient hypotension, and allergic reactions
reteplase
It has high thrombolytic efficacy, good results, good tolerance, low production cost and simple administration method.
For patients with acute myocardial infarction
Common adverse reactions include bleeding
Snake venom thrombolytic agent
It has obvious anticoagulant, inhibiting thrombosis and dissolving thrombosis effects
Effective in treating cerebral thrombosis
A small number of patients may experience adverse reactions such as bleeding and allergies.
leukocyte proliferative drugs
Gene recombination
granulocyte colony stimulating factor
Promote neutrophil maturation and release, enhance neutrophil chemotaxis and phagocytic function
It is mainly used to prevent bone marrow suppression caused by radiotherapy and chemotherapy for malignant tumors. It can also be used for autologous bone marrow transplantation to promote the recovery of reduced neutrophils.
Slightly mild bone marrow pain, long-term intravenous infusion can cause phlebitis
To avoid increased sensitivity of bone marrow to chemotherapy drugs, chemotherapy drugs should be applied 24 hours before or after
granulocyte/macrophage colony-stimulating factor
Mainly used to prevent leukopenia and complications of infection caused by chemotherapy and radiotherapy of malignant tumors
During the first intravenous infusion, flushing, hypotension, etc. may occur
Other leukocytosis-stimulating drugs
VB4
Used for leukopenia caused by various reasons, such as tumor radiotherapy, chemotherapy, antithyroid drugs, chloramphenicol, antipyretic analgesics, benzene poisoning, etc.
Shartol
It has an antagonistic effect on bone marrow suppression caused by tumor radiotherapy and chemotherapy, and it also has a certain effect on leukopenia caused by benzene poisoning.
For leukopenia caused by radiation and other causes
Li Kejun
It can enhance the metabolism of the hematopoietic system and is clinically used to prevent and treat leukopenia, thrombocytopenia and aplastic anemia caused by various causes.
Inosine
Participates in nucleic acid metabolism, protein synthesis and energy metabolism in the body, improves the activity of various enzymes, thereby allowing cells to perform normal metabolism under hypoxic conditions, and contributes to the recovery of damaged cell functions. It is used as an auxiliary medication and has the effect of improving the body's metabolism.
It can be used clinically for auxiliary treatment of leukopenia and thrombocytopenia, heart failure, angina pectoris, hepatitis, etc. caused by various reasons.
blood volume expansion drugs
Dextran
Pharmacological effects
Expand blood volume
Improve microcirculation
Anticoagulation
diuresis
clinical effects
Medium and low molecular weight dextran is used for hypovolemic shock, such as acute blood loss, trauma and burn shock
Treatment of septic shock
Treatment of thrombotic diseases, such as myocardial infarction, cerebral thrombosis, retinal arteriovenous thrombosis and disseminated intravascular coagulation, etc.
Prevent and treat acute renal failure
Adverse reactions
Occasionally allergic reactions - skin test is required for medication
Intravenous infusion should be slow
Contraindicated in patients with thrombocytopenia and bleeding disorders
Hydroxyethyl starch
After intravenous injection, it expands blood volume and improves hemodynamics. The effect can last for 24 hours or more.
Used for hypovolemia caused by various reasons
Patients may experience allergic reactions, manifested as facial eyelid edema, urticaria, asthma, etc.