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Beta blocker

Types of drugs that antagonize the excitatory effect of neurotransmitters and catecholamines on beta receptors

This entry is made by Project of Compilation and Application of Scientific Terms in "Popular Science China" Encyclopedia to examine.

Beta receptor Blockers can selectively interact with β - Adrenergic receptor Combine and thus antagonize Neurotransmitter and catecholamine A type of drug that stimulates beta receptors. Adrenaline receptors are distributed in most sympathetic nerve Postganglionic fibre Dominated Effector cell membrane Its receptors are divided into three types, which can excite heart rate and Myocardial contractility Add bronchiectasia 、 Vasodilation , Viscera smooth muscle Relaxation, etc Lipolysis 。 These effects can be blocked and antagonized by beta blockers.

Chinese name: Beta blocker
Foreign name: β-receptor blocker

Features: Selective binding to beta adrenergic receptors
Pharmacodynamics: β receptor activation
Scope of application: Medical Science

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Adrenergic receptor Distributed in most sympathetic nerve Postganglionic fibre Dominated Effector cell membrane Its receptors can be divided into three types, namely, β 1 receptor, β 2 receptor and β 3 receptor. β 1 receptor is mainly distributed in myocardium, which can excite heart rate and Myocardial contractility Increase; β 2 receptor exists in bronchial and vascular smooth muscle and can be induced by activation bronchiectasia 、 Vasodilation Visceral smooth muscle relaxation; β 3 receptor mainly exists in fat cells Yes, it can be excited Lipolysis 。 These effects can be blocked and antagonized by beta blockers.

Beta blockers can be divided into three categories: ① non selective beta blockers that block both beta 1 and beta 2 receptors, such as propranolol; ② Selective beta blockers have little or no effect on beta 2 receptors, such as Bisoprolol Etc.; ③ Block α 1 and β receptors, such as carvedilol.

Pharmacology of beta blockers

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Action mechanism:

β Receptor blocker With cardiovascular Protective effect , the main mechanism is to antagonize catecholamine adrenergic transmitter Toxicity, especially through β 1 receptor mediated Cardiotoxic effects 。 Other mechanisms include antihypertensive and antihypertensive Myocardial ischemia . Play a certain blocking role by inhibiting renin release Renin angiotensin aldosterone system Function and improvement cardiac function And increase Left ventricle Ejection fraction , anti arrhythmia, etc.

Adverse reactions:

β Receptor blocker High dose application may occur Serious adverse reactions ① Cardiovascular system: it can slow down the heart rate and even cause severe bradycardia and atrioventricular block, mainly seen in Sinoatrial node Patients with impaired atrioventricular node function; ② Metabolic system: some vigilance symptoms of hypoglycemia such as tremor and tachycardia can be masked by the use of non selective beta blockers in patients with type 1 diabetes mellitus; ③ Respiratory system: can cause airway resistance Increase, so it is forbidden to use it for asthma or bronchospasm chronic obstructive pulmonary disease; ④ Central nervous system: fatigue, headache, sleep disorder, insomnia abnormal sweating And depression; ⑤ Drug withdrawal syndrome: after long-term treatment, sudden drug withdrawal may occur, with hypertension, arrhythmia, and worsening angina pectoris.

Disable or use with caution

Beta blockers should not be used or should be used cautiously in the following situations: bronchial spastic asthma, symptomatic hypotension, bradycardia or atrioventricular block of more than second degree type II, heart failure with Significance Sodium retention requires extensive diuresis, and Hemodynamics Unstable requires intravenous application Positive inotropic agent Etc. However, for most Cardiovascular disease Patients with chronic obstructive pulmonary disease without bronchospasm or Peripheral vascular disease % of patients with cardiovascular disease could still benefit significantly from beta blocker treatment; Diabetes mellitus and intermittent claudication of lower limbs are not absolute contraindications.

Application in hypertension

Beta blockers via antagonism sympathetic nerve The main antihypertensive mechanism involves reducing cardiac output and improving Baroreceptor It can regulate the blood pressure and regulate the blood pressure, and inhibit the renin angiotensin aldosterone system; It can also prevent the cardiotoxic effect of catecholamine by reducing the sympathetic nerve tension.

Beta blocker is one of the initial and long-term antihypertensive drugs for hypertensive patients, which can be used alone or in combination with other antihypertensive drugs. nothing complication Eighty five percent of young and middle-aged patients with hypertension may consider the use of beta blockers. Hypertension patients with the following conditions should give priority to the use of beta blockers: Rapidity Arrhythmia (e.g Sinus tachycardia 、 Atrial fibrillation )、 Coronary atherosclerotic heart disease (coronary heart disease, such as angina pectoris and myocardial infarction) chronic heart failure , and increased sympathetic nerve activity, such as anxiety, tension and other mental stress, Perioperative period Patients with hypertension and high circulatory status such as hyperthyroidism. It is recommended to use β receptor blockers that have no intrinsic sympathomimetic activity, high selectivity of β 1 receptor, or both α receptor blocking and vasodilating effects, such as Bisoprolol , metoprolol and carvedilol. These drugs have little impact on metabolism and few adverse reactions, and can be safely used for hypertensive patients with diabetes, chronic obstructive pulmonary disease and peripheral vascular disease.

Beta blockers and long-acting Dihydropyridine Calciform Antagonist Combined use is one of the recommended antihypertensive drug combinations; Beta blockers and Angiotensin converting enzyme inhibitor or Angiotensin receptor The combination of antagonists is suitable for patients with hypertension and coronary heart disease.

Application in coronary heart disease

Beta blockers are beneficial to patients with various types of coronary heart disease. First, by reducing Myocardial contractility , heart rate and blood pressure Myocardial oxygen consumption Reduction; Simultaneously lengthen the heart Diastole And increase the Blood supply And perfusion to reduce and alleviate daily activities or motion state Myocardial ischemic attack, improve Quality of life 。 Second, it can reduce the infarct size and fatal arrhythmia, including Sudden cardiac death Inside acute stage Case fatality rate And various cardiovascular event incidence rate 。 Third, long-term application can improve the long-term performance of patients prognosis , improve survival rate It is beneficial to the secondary prevention of coronary heart disease.

All patients with coronary heart disease should be treated with beta blockers for a long time as a secondary prevention. ST segment elevated myocardial infarction or non ST segment elevated myocardial infarction Acute coronary syndrome If patients cannot use it due to contraindications in the acute phase, they should be re evaluated before discharge, and beta blockers should be used as far as possible to improve the prognosis.

Application in heart failure

Beta blockers effectively antagonize the sympathetic nervous system, renin angiotensin aldosterone system and overactive nerves Humoral factor , plays an important role in blocking the vicious cycle chain of cardiovascular disease, thus delaying or reversing Myocardial remodeling , give play to improvement endogenous The "biological effect" of myocardial function.

Application of β - blocker in arrhythmia β - blocker is the only antiarrhythmic drug that can reduce sudden cardiac death and total mortality. The application indications recommended as Class I include: partial sinus tachycardia, perioperative arrhythmia, atrial fibrillation with rapid ventricular response, ventricular tachycardia storm Sympathetic excitation And some types of long QT syndrome.

Application in other cardiovascular diseases

1　 Dilated cardiomyopathy In the early stage, only Cardiomegaly For patients without clinical manifestations of heart failure, beta blockers can be used to reduce myocardial damage It is especially suitable for patients with fast heart rate, ventricular arrhythmia, and β receptor antibody positive. Patients with symptoms and signs of heart failure in the middle and late stages should be treated as chronic heart failure, and beta blockers should also be used.

2. Patients with hypertrophic cardiomyopathy with definite diagnosis, including those with early and mild symptoms, are suitable for beta blockers; The symptoms of patients with obstructive hypertrophic cardiomyopathy can be improved by using larger doses.

3　 Mitral valve prolapse Symptoms apply to symptomatic patients.

Hyperthyroidism beta blocker can rapidly relieve tachycardia, tremor, anxiety and other symptoms caused by hyperthyroidism.

five Aortic dissection

The combination of β - blocker and sodium nitroprusside , reduce blood flow aorta To reduce the contraction rate of the left ventricle to slow down the progress of the disease.

6 LQTS

LQTS( genetic QT prolongation syndrome): Unless there are serious contraindications, beta blockers are the first choice for symptomatic LQTS patients today. If there is no absolute contraindication, lifelong use is recommended Maximum tolerable dose β - blocker can significantly reduce the occurrence of cardiovascular events. By 2015, it is believed that beta blockers are also recommended for asymptomatic LQTS patients.

7 Left atrioventricular valve prolapse

For patients with symptomatic left atrioventricular valve prolapse, beta blockers are usually the first choice.^[1]

Common beta blockers

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(1) Atenolol (also known as aminoacyl propranolol) , a cardiac selective beta blocker, has no endogenous inhibition of sympathetic nerve activity, half life 6-9 hours, most clinical research It shows that the blood pressure can be reduced continuously for 24 hours after taking the medicine once, especially for Tachycardia merge hypertension Patients. And Vasodilation Agent Calcium antagonist or diuretic Used together, the effect of reducing blood pressure is better. Someone is used to treat serious Hypertensive crisis After taking 10mg orally, the blood pressure gradually decreased within 12 hours, on average systolic pressure 7.5kPa (56mmHg) drop, diastolic pressure It is considered to be a safe and effective drug with a decrease of 5.3kPa (40mmHg).

(2) metoprolol ( Trade name Betaloc ）, is a selective beta receptor blocker. After it was introduced in 1975 angina pectoris 、 myocardial infarction 、 Arrhythmia And other aspects have achieved certain curative effects. In the treatment of hypertension, 100 mg was taken orally for 4 weeks, and the total effective rate was 82.4%. After 2 weeks of treatment, the blood pressure gradually decreased, but the heart rate did not decline, which could be significantly improved Hypertensive patients Of dizzy 、 palpitation 、 vertigo 、 Chest tightness It is suitable for patients with primary and secondary hypertension. Its side effects include slow heart rate, fatigue Xerostomia , chest tightness, etc., most of which can be relieved or disappeared after a period of treatment, but with bronchial asthma or Bradycardia Disabled by.^[2]

(3) Sotalol hydrochloride

[Trade name] Steicher

[Drug name] Sotalol hydrochloride

【 Indications 】Suitable for life threatening fast Ventricular arrhythmia , if continuous Ventricular tachycardia 。 Due to its proarrhythmic effect, it is generally not recommended for non persistent Ventricular tachycardia And supraventricular arrhythmia.

[Pharmacology] (1) Pharmacodynamics : Existing β of this product Block action And Class III Antiarrhythmic drugs characteristic. This product is Racemate , both isomers have class III effects, but only Left-handed isomer yes Beta receptor Blocking effect, which is non cardiac selective and non intrinsic Parasympathetic effect. Extension of this product action potential Platform phase, slow down sinus rhythm, delay Atrioventricular node Conduction. Make atrium, ventricular muscle and Conduction system (including bypass) Undue period Extension. electrocardiogram produce Dose dependence QTc prolonged, slightly decreased Cardiac output And lowering blood pressure.

(2) Pharmacokinetics ： Bioavailability 90%～ 100% 。 Oral Peak time 2.5~4 hours. 2 to 3 days after oral administration twice a day Steady state concentration 。 In the range of 160~640mg per day Blood concentration Same as the dose. Not with Plasma protein Combination, no Liver metabolism 。 Difficult to pass blood brain barrier 。 All are discharged from the kidney in the original form. t 1/2 β is 12 hours, renal function The half-life of obstacle is prolonged. But Liver dysfunction It has no effect on the metabolism of the product.

【 Adverse reactions 】(1) The most important adverse reaction is the proarrhythmic effect, which causes twisted ventricular tachycardia and new severe ventricular arrhythmia. It can also produce bradycardia syncope 、 hypotension 、 dyspnea 、 Heart failure Exacerbation, edema, etc. (2) nervous system : fatigue dizzy 。 (3) digestive system : Nausea and vomiting. (4) Others: asthma ． rash , limb pain, etc.

[Contraindication] This product is prohibited under the following circumstances: bronchial asthma, Sinus bradycardia , II or III degree atrioventricular block (unless there is pacemaker ）, congenital or Acquirability Q-T prolongation syndrome, Cardiogenic shock , uncontrolled heart failure and Allergic history The.

[Precautions] (1) Renal dysfunction may cause accumulation of this product, and the interval of medication should be extended according to creatinine clearance rate. (2) This product can pass through the placenta and secrete milk. Pregnant women and lactating women should use it with caution. (3) Same as other beta blockers. Do not stop taking medicine suddenly. (4) The following cases should be used with caution: heart failure controlled by digitalis Hypokalemia , hypomagnesemia, first degree atrioventricular block. (5) Pay attention to monitoring during application: ① ECG, especially Q-T interval Change; ② Blood pressure; ③ electrolyte ；④ Renal function.

【 Drug interaction 】(1) When used together with other Class Ia, II and III antiarrhythmic drugs Synergy 。 (2) When used together with calcium antagonist, it can add barycenter conduction barrier to further inhibit ventricular function , reduce blood pressure. (3) And catecholamine Drugs (such as reserpine Guanethidine ）When used together, hypotension and severe bradycardia may occur. (4) There is an increase in blood sugar, which needs to be increased insulin and Hypoglycemic drugs Report of.

【 Administration Note] (1) When the QTc of ECG is greater than 500ms, attention should be paid to the proarrhythmic effect, and the drug should be stopped when the QTc exceeds 550ms. (2) If the drug needs to be stopped, it should be gradually reduced and used within 1 to 2 weeks. (3) When switching from other antiarrhythmic drugs to this product, this product should be stopped for 2~3 half lives of the previous drug under strict monitoring before use. from amiodarone When replacing this product, it can be used only after Q-T returns to normal.

[Usage and dosage] (1) Adult Common quantity : Oral administration starts from 80mg twice a day, and the dosage is increased to 120-160mg twice a day within 2-3 days according to the reaction. 640mg per day. (2) Pediatric usage and safety: not yet determined.

[Preparation and specification] Sotalol Hydrochloride Tablets : (1) 80mg * 28 pieces; (2)160mg； (3)240mg。

(4) Propranolol hydrochloride

[Trade name] Peace of mind

[Drug name] Propranolol hydrochloride

[Indications] For: ① hypertension, used alone or in combination with other drugs. ② Angina pectoris (typical angina pectoris, that is, exertional angina pectoris). ③ Arrhythmias, control supraventricular tachyarrhythmias, ventricular arrhythmias, especially those related to catecholamine and caused by digitalis, can be used for those with unsatisfactory efficacy of digitalis Atrial flutter 、 atrial fibrillation Of Ventricular rate Can also be used for stubborn Premature beat Improve the symptoms of patients. ④ Hypertrophic cardiomyopathy , used to reduce outflow tract pressure difference, relieve angina pectoris, heart palpitations and faint And other symptoms. ⑤ pheochromocytoma , matching Alpha receptor blocker It is used to control tachycardia. ⑥ Hyperthyroidism , for control Tachycardia , also used for treatment Thyroid crisis 。⑦ miocardial infarction , as Secondary prevention , decrease mortality 。⑧ Mitral valve prolapse Syndrome. ⑨ Also available for migraine and Primary tremor 。

[Pharmacology] (1) Pharmacodynamics: this product is non selective competitiveness Ground suppression adrenaline β receptor. The contraction force and contraction speed of the heart are reduced by weakening or preventing the excitation of beta receptors conduction velocity Slows down, which weakens the heart's response to exercise or stress. Therefore, it can be used for the treatment of angina pectoris to reduce the heart muscle Oxygen consumption , add Exercise tolerance 。 Because of block Cardiac pacemaker Potential adrenaline can excite, so it is used to treat arrhythmia. This product may pass through the central Adrenergic neuron Blocking and inhibition renin It can release blood and reduce cardiac output, and is suitable for treating hypertension. As this product can antagonize the catecholamine effect, it is also used to treat pheochromocytoma and Hyperthyroidism , so that the activities of β 1 and β 2 receptors are both in Suppression state 。

(2) Pharmacokinetics: after oral administration Gastrointestinal absorption Relatively complete (90%), the blood drug concentration reaches the peak value in 1~1.5 hours, but before entering the systemic circulation Immediate It is metabolized by the liver Inactivation And the bioavailability is 30%. The binding rate with plasma protein was very high, 93%. t 1/2 2-3 hours. through Renal excretion , mainly Metabolites , a small part (<1%) is the prototype. It cannot be discharged through dialysis. [Adverse reactions] (1) Dizziness or dizziness (caused by hypotension) and slow heart rate (<50 times/minute) are common. (2) Less common are Bronchospasm And dyspnea Congestive heart failure Mental confusion (especially in the elderly), mental depression, Unresponsive 。 (3) Less common are fever and Pharyngalgia ( Agranulocytosis ）, rash（ Anaphylactic reaction )、 Bleeding tendency ( Thrombocytopenia )。

(4) When adverse reactions persist, the following should be paid special attention: Raynaud disease Like cold limbs, diarrhea, fatigue, eyes, mouth or xerosis cutis , nausea, numbness of fingers and toes, abnormal fatigue, etc.

[Contraindications] ① Bronchus asthma ；② Cardiogenic shock; ③ heart Conduction block (II to III degrees Atrioventricular block )；④ Severe or Acute heart failure ；⑤ Sinus bradycardia; ⑥ People who are allergic to this product.

[Precautions] (1) This product can enter the fetus through the placenta. It is reported that Pregnancy hypertension After use, it can be sent into the uterus Fetal growth retardation , caused by weakness during delivery dystocia , newborn babies can produce hypotension hypoglycemia 、 Respiratory depression Although there are reports that it has no effect on the mother and fetus, it must be used with caution and should not be used as the first-line treatment drug for pregnant women. (2) It can secrete a small amount from milk, so Lactating women Use with caution. (3) The elderly have low capacity of metabolism and excretion of this product, so appropriate dosage should be taken. (4) Interference to diagnosis: when using this product, measure the blood Urea nitrogen 、 Lipoprotein 、 creatinine , potassium triglyceride 、 uric acid And so on may increase; Blood sugar is reduced, but diabetes Patients sometimes grow taller. Renal insufficiency Hour Propranolol The metabolites of can accumulate in the blood and interfere with the determination of serum bilirubin Diazo reaction , can appear false positive 。 (5) The following cases should be used with caution: ① allergy history; ② congestive heart failure ；③ Diabetes mellitus; ④ emphysema Or not Allergic bronchitis ；⑤ Hepatic insufficiency ；⑥ Hypothyroidism ；⑦ Raynaud's disease or others Peripheral vascular disease ；⑧ Decreased renal function. (6) During the application of this product Regular inspection routine blood test , blood pressure, cardiac function liver function Kidney function. Diabetic patients should check blood sugar regularly. (7) The dosage must be individualized. The dosage varies from person to person and from disease to disease. The dosage for patients with liver and kidney dysfunction is small; (8) Note that the blood concentration cannot be completely predicted Pharmacological effect , so it should also be based on heart rate, blood pressure and other clinical sign Guide clinical medication; (9) coronary heart disease Patients should not stop suddenly when using this product, otherwise angina pectoris, myocardial infarction or Ventricular tachycardia ； (10) hyperthyroidism The patient should not stop suddenly when using this product, otherwise it will aggravate the symptoms of hyperthyroidism; (11) Long term use can cause heart failure in a few patients. If it occurs, digitalis and (or) diuretics can be used to correct it. (12) Overtreatment: bradycardia atropine or Isoproterenol , install if necessary pacemaker ， Ventricular premature beat to lidocaine or Phenytoin sodium 。 Heart failure oxygenation, digitalis or Diuretic 。 Infusion and administration in case of hypotension Pressor 。 Twitch diazepam Or phenytoin sodium. Give isoproterenol aminophylline 。

[Drug interaction] (1) and hypotensor Interaction: with clonidine If the drug needs to be stopped for the same use, stop using this product first, and then gradually reduce clonidine after a few days to avoid blood pressure fluctuation. And Monoamine oxidase inhibitor It can cause extreme hypotension when used together, so it is forbidden. And reserpine Use the same. When the two effects are added together, the blocking effect of β receptor is enhanced, and bradycardia and hypotension may occur. (2) Same as digitalis glycoside. Atrial rate block may occur and lead to slow heart rate, so close observation is required. (3) Used with calcium antagonists, especially intravenously Verapami We should be very alert to the inhibition of myocardium and conduction system. (4) With adrenaline Phenylephrine Or sympathomimetic amines can cause significant hypertension, slow heart rate, and atrioventricular block, so close observation is required. (5) Can make Non depolarizing muscle relaxants as Tubocurarine chloride 、 Galla ammonium iodide And so on. (6) This product can cause hypoglycemia in diabetic patients, so when used with hypoglycemic drugs, the dosage of the latter must be adjusted. (7) With isoproterenol or xanthine If used together, the effect of the latter can be weakened. (8) And chlorpromazine When used together, the blood drug concentration of both can be increased. (9) Phenytoin sodium Phenobarbital 、 Li Fuping Accelerate the removal of the product. (1O) Antipyrine , lidocaine theophylline Class II slows the removal of the product.

[Description of administration] (1) Oral administration can be performed on an empty stomach or with food, which can slow the metabolism of the product in the liver and increase its bioavailability. (2) Long term users of this product should gradually reduce the dosage after at least 3 days, usually 2 weeks. Gradually decrease the product, and finally stop using it.

[Usage and dosage] (1) Angina pectoris, myocardial infarction: Take 10mg orally, 3-4 times a day, and increase 10~20mg every 3 days, and gradually increase to 200mg a day. (2) Hypertension: Take 10mg orally, 3-4 times a day, and gradually adjust it according to the needs and tolerance until the blood pressure is controlled. (3) Anti arrhythmias: oral, 10~30mg once, 3~4 times a day, dosage should be adjusted according to needs and tolerance. Severe arrhythmia In case of emergency intravenous injection 1~3mg, injected at a rate of no more than 1mg per minute, repeated once every 2 minutes if necessary, and once every 4 hours thereafter. (4) Hypertrophic cardiomyopathy : oral administration, 10-20mg once, 3-4 times a day, adjusted according to needs and tolerance. (5) Pheochromocytoma: oral administration, 10~20mg once, 3~4 times a day, 3 days before operation, often used with alpha receptor blocker, generally alpha receptor blocker should be used first, and this product should be added after the drug effect appears and becomes stable. (6) Sustained release tablets Take 40mg early or late a day for the treatment of hypertension and angina pectoris. If necessary, it can be increased to 80mg. Prevention after myocardial infarction can be up to 160 mg per day. (7) The dosage for children has not yet been determined. Generally, it is taken orally at 0.5~1.0mg/kg per day, in batches; For intravenous injection, the weight shall be 0.0l~0.1mg/kg, and the amount shall not exceed lmg at a time.

[Preparation and specification] Propranolol Hydrochloride Tablets : 1Omg * 100 tablets.

Propranolol hydrochloride sustained-release tablets ：40mg。 Propranolol Hydrochloride Sustained Release Capsules ：40mg。^[3]

(5) Carvedilo

[Trade name] Daliquan Lord

[Name of drug] Carvedilo

[Indications] ① essential hypertension , used alone or in combination with other antihypertensive drugs such as diuretics. ② Symptomatic chronic congestive heart failure.

[Pharmacology] (1) Pharmacodynamics: This product is an adrenergic α - and β - receptor blocker with strong β - receptor blocking effect Rabelor 33 times of Propranolol 3 times. This product is blocked by Postsynaptic membrane Alpha receptor , expand blood vessels, reduce Peripheral vascular resistance 。 At the same time, it blocks beta receptor, inhibits renin secretion, and blocks renin angiotensin- aldosterone The system can reduce the pressure. None of this product Intrinsic sympathomimetic activity , with membrane stability. This product pair Cardiac output And heart rate, rarely Retention of water and sodium 。 Animal test and in vitro variety Human cells Test confirmation This medicine It also has antioxidant properties. This medicine is used in high concentration fashion Antagonism 。

(2) Pharmacokinetics: The drug is easy to be absorbed after oral administration, First pass effect About 60%~75%. The bioavailability is 25%. When taken with food, absorption slows down, but there is no significant impact on bioavailability. In plasma and Plasma protein binding rate 98%. This drug is completely metabolized, Metabolic half-life About 2 hours, metabolite Main meridians bile It is excreted by feces, and about 16% is excreted by kidneys. This medicine Lipophilicity High, Distribution volume About 2L/kg, so it may be secreted with milk. Elimination half-life About 6~10 hours Hemodialysis eliminate.

[Adverse reactions] (1) central nervous system : occasional mild dizziness headache , fatigue, especially in the early stage of treatment. Rare depression Sleep disorders 、 Paresthesia 。 (2) cardiovascular system : occasional bradycardia Orthostatic hypotension , few cases of syncope; Peripheral Circulatory disorder (limbs are cold) Not common , can make the original Intermittent claudication Contingent Reynolds phenomenon Symptoms worsened in 30% of patients. Edema and angina were uncommon. A few patients had atrioventricular block and heart failure aggravated. (3) respiratory system : Even inducible asthma Or patients with dyspnea tendency. rare nasal congestion 。 (4) Digestive system: occasional gastrointestinal discomfort (such as abdominal pain , diarrhea, nausea, etc.), constipation and vomiting are uncommon. (5) Urogenital system : dysuria Sexual function Decline; Heart failure and Diffuse Patients with vascular disease or renal insufficiency may further aggravate renal function damage, which may occur in individual cases renal failure 。 (6) Skin: rare Allergy Rashes, which may occur in some patients Urticaria 、 itch 、 lichen planus kind Skin reaction 。 Silver shavings may occur Skin damage Or aggravate the original condition. (7) Eye: available Xerophthalmia symptom; rare Visual impairment And eye irritation. (8) Others: occasionally Limb pain Dry mouth.

[Contraindication] (1) People who are allergic to this product. (2) Pregnant and lactating women. (3) Low liver function. (4) Bronchospasm or asthma 、 Chronic obstructive pulmonary disease patient. (5) Severe bradycardia (heart rate<50 beats/minute) Sick sinus syndrome (including sinoatrial block), Ⅱ~Ⅲ degree atrioventricular block. (6) Cardiogenic shock. (7) Severe hypotension (systolic blood pressure<85mmHg). (8) Grade IV decompensated heart failure requires intravenous Positive muscle strength Patients with drugs.

[Precautions] (1) Caution: ① Surgical patients. ② Hyperthyroidism. ③ Patients with peripheral vascular diseases (such as intermittent claudication). ④ Patients with pheochromocytoma ⑤ Postural hypotension. ⑥ Unstable or Secondary hypertension Patients. ⑦ Variant angina pectoris 。⑧ diabetic. (2) Impact of the drug on children: no patient under 18 years old has ever used this drug for safety and efficacy research data 。 (3) Influence of drugs on test value or diagnosis: occasional serum Aminotransferase Elevated, thrombocytopenia, Leukopenia 。 (4) This medicine may affect the ability to drive and operate the machine. It is more obvious at the beginning of medication, dose change or drinking. (5) anaesthesia During this period, patients should closely observe the negative Myodynamia And hypotension. (6) Accept digoxin , diuretics, vascular tension Converting enzyme Patients treated with inhibitor drugs must first use these drugs to stabilize their condition, and then use carvedilol. (7) If it occurs during the use of this product Transitory The dosage of diuretics must be increased when heart failure is aggravated or water sodium retention occurs. Sometimes it is necessary to reduce or terminate the treatment of this drug. (8) Treatment of drug overdose: patients should adopt Supine position , keep observing and take measures when necessary Special care treatment. Gastric lavage or drugs can be used to induce vomiting shortly after taking the drugs, and atropine 2mg can be injected intravenously for patients with excessive bradycardia. (9) Since the half-life of the drug is 7 to 10 hours, the detoxification treatment must last long enough in case of severe poisoning (shock symptoms).^[1]

[Drug interaction] (1) This product can strengthen other antihypertensive drugs (such as: reserpine 、 Methyldopa 、 clonidine 、 Calcium antagonist 、 Alpha receptor Antagonists, etc.) and drugs with side effects of lowering blood pressure（ Barbiturate )、 Phenothiazine , Erhuan antidepressant And the corresponding side effects are also increased. (2) Cimetidine etc. Hepatase Inhibitors can keep the drug in the body Decomposition It may increase the blood concentration of the drug. (3) When this drug is used together with amiodarone, its effect on the heart is enhanced, and hypotension, bradycardia or Cardiac arrest 。 (4) Heart block may occur when this drug is used together with diltiazem or verapamil. (5) This medicine may enhance the effect of insulin or oral hypoglycemic drugs. (6) This medicine and Methacholine acetate When used together, it can produce synergistic shrinkage a bronchial tube smooth muscle Function of Shrinkage time Extension. (7) This medicine can inhibit Cyclosporine The metabolism of the latter increases the toxicity of the latter. (8) This medicine can increase the bioavailability and Valley concentration To enhance its effect on the heart, cause atrioventricular block and toxic symptoms of digoxin. The clinical measurement of digoxin blood concentration should be strengthened. (9) Non steroidal anti-inflammatory drugs can reduce the antihypertensive effect of this drug. (10) Rifampicin Riff pudding Other liver drug enzyme inducers can induce the metabolism of the drug, thus weakening the effect of the drug. (11) This medicine can block adrenal gland β effect of adrenergic acid, thus causing bradycardia and antagonizing the allergic reaction of adrenaline. (12) And fentanyl In combination, it can produce severe hypotension. The mechanism is unknown. (13) Moxonidine May occur when used in combination with this drug Rebound hypertension The mechanism of action is still unclear.^[2]

[Instruction for administration] (1) This drug generally needs to be used for a long time, and sudden drug withdrawal should be avoided. It should be gradually stopped for more than 1 to 2 weeks. It should be reduced as much as possible within 2-3 weeks after drug withdrawal physical activity To avoid worsening angina pectoris or other serious Cardiovascular disease 。 (2) When terminating the combined use of this drug and clonidine, this drug should be stopped first, and then the dosage of clonidine should be gradually reduced after a few days. (3) Before taking carvedilol, patients with pheochromocytoma should first use alpha receptor blocker. (4) Carvedilol must be reduced for bradycardia with heart rate<55 beats/minute. (5) Although the time of taking this medicine has nothing to do with meals, it must be taken with meals for patients with congestive heart failure to slow absorption and reduce the occurrence of postural hypotension.

【 Usage and dosage 】(1) Common dosage for adults: oral, ① essential hypertension and angina pectoris , the initial dose is 12.5 mg, once a day, oral; Take 25mg orally once a day after two days, and then gradually increase the dosage to 50mg a day as required, taking it 1-2 times. ② For chronic congestive heart failure, the dose must be individualized, and close observation is required to increase the dose. The recommended dose is 3.125mg twice a day for the first two weeks. If well tolerated, the dose can be increased to 6.25mg twice a day after an interval of at least two weeks, then 12.5mg twice a day, then 25mg twice a day. The dose must be increased to the maximum level that the patient can tolerate. For those whose weight is less than 85 kg, the maximum recommended dose is 25 mg, twice a day; For those whose weight is>85 kg, the maximum recommended dose is 50 mg, twice a day. When carvedilol is stopped for more than 2 weeks, it should be reapplied with 3.125mg once, twice a day, and then the dosage should be increased according to the above recommended method. (2) Dose for the elderly: the initial dose for patients with primary hypertension is 12.5 mg once a day. If the effect is not good, the dose can be increased to the recommended maximum dose of 50mg a day after an interval of at least 2 weeks, once a day or in batches.

[Preparation specification] Carvedilol tablet : Daliquan (1) 6.25mg * 10 tablets; (2) 25mg * 10 tablets. Lode (3) 10mg * 20 tablets;^[3-4]

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