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Kovalenko Svetlana Olegovna 、薬局による医学的評価、 最終更新日:16.03.2022
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Control of tachyarrhythmias, especially supraventricular tachyarrhythmias.
Early intervention with Vasocardin SR I.V. Injection in acute myocardial infarction reduces infarct size and the incidence of ventricular fibrillation. Pain relief may also decrease the need for opiate analgesics.
Vasocardin SR I.V. Injection has been shown to reduce mortality when administered to patients with acute myocardial infarction.
- Hypertension
- Angina pectoris
- Tachyarrhythmias, in particular supraventricular tachycardia
- Maintenance treatment after a myocardial infarction
- Prophylaxis of migraine
Vasocardin SR is indicated in adults.
- Hypertension
- Angina pectoris
- Tachyarrhythmias, in particular supraventricular tachycardia
- Maintenance treatment after a myocardial infarction
- Prophylaxis of migraine
Metoprolol is indicated in adults.
Posology
The dose must always be adjusted to the individual requirements of the patient. The following are guidelines:
Cardiac arrhythmias:
Initially up to 5 mg injected intravenously at a rate of 1-2 mg per minute. The injection can be repeated at 5 minute intervals until a satisfactory response has been obtained. A total dose of 10-15 mg generally proves sufficient.
Because of the risk of a pronounced drop of blood pressure, the I.V. administration of Vasocardin SR I.V. Injection to patients with a systolic blood pressure below 100 mmHg should only be given with special care.
During Anaesthesia:
2-4 mg injected slowly I.V. at induction is usually sufficient to prevent the development of arrhythmias during anaesthesia. The same dosage can also be used to control arrhythmias developing during anaesthesia. Further injections of 2 mg may be given as required to a maximum overall dose of 10 mg.
Myocardial infarction:
Intravenous Vasocardin SR I.V. Injection should be initiated in a coronary care or similar unit when the patient's haemodynamic condition has stabilised. Therapy should commence with 5 mg I.V. every 2 minutes to a maximum of 15 mg total as determined by blood pressure and heart rate. The second or third dose should not be given if the systolic blood pressure is <90 mmHg, the heart rate is <40 beats/min and the P-Q time is >0.26 seconds, or if there is any aggravation of dyspnoea or cold sweating. Oral therapy should commence 15 minutes after the last injection with 50 mg every 6 hours for 48 hours. Patients who fail to tolerate the full intravenous dose should be given half the suggested oral dose.
Renal impairment:
Dose adjustment is generally not needed in patients with impaired renal function.
Hepatic Impairment:
Dose adjustment is normally not needed in patients suffering from liver cirrhosis because metoprolol has a low protein binding (5 - 10 %). However, in patients with severe hepatic dysfunction a reduction in dosage may be necessary.
Elderly:
Several studies indicate that age related physiological changes have negligible effects on the pharmacokinetics of metoprolol. Dose adjustment is not needed in the elderly, but careful dose titration is important in all patients.
Paediatric population:
The safety and efficacy of metoprolol in children has not been established.
Vasocardin SR tartrate tablets should be administered orally.
The tablets should be taken on an empty stomach.
The dose must always be adjusted to the individual requirements of the patient. The following are guidelines:
Posology
Hypertension
The usual dose is 100mg to 200mg daily, given as a single dose in the morning, or in divided doses (morning and evening). Begin with 50mg twice daily or 100mg once daily. Dose increments should be at weekly intervals thereafter according to individual patient responses. Maximum dose, usually 200mg daily. If necessary, it may be taken in combination with other antihypertensive drugs.
Angina pectoris
The usual dose is 100 to 200 mg daily, given in divided doses (morning and evening). Begin with 50mg twice daily. Dose increments should be at weekly intervals thereafter according to individual patient responses. Maximum dose, usually 200mg daily (in divided doses). If necessary, it may be taken in combination with other antianginal drugs.
Cardiac arrhythmias
The usual dose is 100 to 150 mg per day, in divided doses (in the morning and in the evening). This dosage may be increased, where necessary.
Myocardial infarctions
Maintenance therapy
The oral treatment can be initiated once the patient is haemodynamically stable. The maintenance dose is 100 mg of Vasocardin SR tartrate twice a day (in the morning and in the evening).
Prophylaxis of migraine
The usual dose is 100 to 200 mg per day, in divided doses, in the morning and evening.
Impaired renal function
The dosage does not need to be adjusted in patients with reduced renal function.
Impaired hepatic function
Usually a dose adjustment in patients suffering from liver cirrhosis is not necessary because Vasocardin SR has a low protein binding (5-10%).However, in patients with severe hepatic dysfunction a reduction in dosage may be necessary.
Elderly patients
No dosage adjustment is required in otherwise healthy elderly patients. However, caution is advised in elderly patients as a fall in blood pressure or excessive bradycardia may have more pronounced effects.
Children
The experience in children is limited, therefore Vasocardin SR tartrate is not recommended in children.
Vasocardin SR tablets should be administered orally.
The tablets should be taken on an empty stomach.
The dose must always be adjusted to the individual requirements of the patient. The following are guidelines:
Posology
Hypertension
The usual dose is 100mg to 200mg daily, given as a single dose in the morning, or in divided doses (morning and evening). Begin with 50mg twice daily or 100mg once daily. Dose increments should be at weekly intervals thereafter according to individual patient responses. Maximum dose, usually 200mg daily. If necessary, it may be taken in combination with other antihypertensive drugs.
Angina pectoris
The usual dose is 100 to 200 mg daily, given in divided doses (morning and evening). Begin with 50mg twice daily. Dose increments should be at weekly intervals thereafter according to individual patient responses. Maximum dose, usually 200mg daily (in divided doses). If necessary, it may be taken in combination with other antianginal drugs.
Cardiac arrhythmias
The usual dose is 100 to 150 mg per day, in divided doses (in the morning and in the evening). This dosage may be increased, where necessary.
Myocardial infarctions
Maintenance therapy
The oral treatment can be initiated once the patient is haemodynamically stable. The maintenance dose is 100 mg of Vasocardin SR twice a day (in the morning and in the evening).
Prophylaxis of migraine
The usual dose is 100 to 200 mg per day, in divided doses, in the morning and evening.
Impaired renal function
The dosage does not need to be adjusted in patients with reduced renal function.
Impaired hepatic function
Usually a dose adjustment in patients suffering from liver cirrhosis is not necessary because Metoprolol has a low protein binding (5-10%).However, in patients with severe hepatic dysfunction a reduction in dosage may be necessary.
Elderly patients
No dosage adjustment is required in otherwise healthy elderly patients. However, caution is advised in elderly patients as a fall in blood pressure or excessive bradycardia may have more pronounced effects.
Children
The experience in children is limited, therefore Vasocardin SR is not recommended in children.
Vasocardin SR I.V. Injection, as with other beta blockers, should not be used in patients with any of the following:
-
- Hypotension.
- AV block of second- or third-degree.
- Decompensated cardiac failure (pulmonary oedema, hypoperfusion or hypotension).
- Continuous or intermittent inotropic therapy acting through beta-receptor agonism.
- Bradycardia (<45 bpm).
- Sick sinus syndrome (unless a permanent pacemaker is in place).
- Cardiogenic shock.
- Severe peripheral arterial circulatory disorder.
- Untreated phaeochromocytoma.
- Metabolic acidosis.
Known hypersensitivity to any component of Vasocardin SR I.V. Injection or other beta-blockers.
Vasocardin SR I.V. Injection is also contra-indicated when suspected acute myocardial infarction is complicated by bradycardia (<45 bpm), first-degree heart block or systolic blood pressure <100 mmHg and/or severe heart failure.
- Hypersensitivity to the active ingredient, other β-blockers or to any of the excipients.
- Second-or third-degree AV block
- Patients with unstable or acute decompensated heart failure (pulmonary oedema, hypoperfusion, or hypotension), in which case intravenous inotropic therapy is indicated
- Patients who are receiving, continuously or periodically, inotropic β receptor agonist therapy
- Severe bradycardia (<50 bpm)
- Sick sinus syndrome
- Cardiogenic shock
- Severe peripheral arterial disease
- Asthma or a history of bronchospasm
- Untreated phaeochromocytoma
- Metabolic acidosis
- The concomitant intravenous administration of calcium antagonists of verapamil and Diltiazem, due to the risk of hypotension, AV conduction disturbances, or left ventricular insufficiency occurring
- Hypotension
Vasocardin SR is not indicated for patients with myocardial infarction and a heart rate of <50 beats/minutes, a P-Q interval of >0.24 seconds, or systolic blood pressure of <100 mg Hg and/or severe congestive heart failure.
- Hypersensitivity to the active ingredient, other β-blockers or to any of the excipients.
- Second-or third-degree AV block
- Patients with unstable or acute decompensated heart failure (pulmonary oedema, hypoperfusion, or hypotension), in which case intravenous inotropic therapy is indicated
- Patients who are receiving, continuously or periodically, inotropic β receptor agonist therapy
- Severe bradycardia (<50 bpm)
- Sick sinus syndrome
- Cardiogenic shock
- Severe peripheral arterial disease
- Asthma or a history of bronchospasm
- Untreated phaeochromocytoma
- Metabolic acidosis
- The concomitant intravenous administration of calcium antagonists of verapamil and Diltiazem, due to the risk of hypotension, AV conduction disturbances, or left ventricular insufficiency occurring
- Hypotension
Metoprolol is not indicated for patients with myocardial infarction and a heart rate of <50 beats/minutes, a P-Q interval of >0.24 seconds, or systolic blood pressure of <100 mg Hg and/or severe congestive heart failure.
When treating patients with suspected or definite myocardial infarction the haemodynamic status of the patient should be carefully monitored after each of the three 5 mg intravenous doses. The second or third dose should not be given if the heart rate is <40 beats/min, the systolic blood pressure is <90 mmHg and the P-Q time is >0.26 sec, or if there is any aggravation of dyspnoea or cold sweating.
Vasocardin SR I.V. Injection, as with other beta blockers:
- should not be withdrawn abruptly during oral treatment. When possible, Vasocardin SR I.V. Injection should be withdrawn gradually over a period of 10 - 14 days, in diminishing doses to 25 mg daily for the last 6 days. During its withdrawal patients should be kept under close surveillance, especially those with known ischaemic heart disease. The risk for coronary events, including sudden death, may increase during the withdrawal of beta-blockade.
- must be reported to the anaesthetist prior to general anaesthesia. It is not generally recommended to stop Vasocardin SR I.V. Injection treatment in patients undergoing surgery. If withdrawal of metoprolol is considered desirable, this should, if possible, be completed at least 48 hours before general anaesthesia. Routine initiation of high-dose metoprolol to patients undergoing non-cardiac surgery should be avoided, since it has been associated with bradycardia, hypotension, stroke and increased mortality in patients with cardiovascular risk factors. However in some patients it may be desirable to employ a beta-blocker as premedication. In such cases an anaesthetic with little negative inotropic activity should be selected to minimise the risk of myocardial depression.
- although contra-indicated in severe peripheral arterial circulatory disturbances , may also aggravate less severe peripheral arterial circulatory disorders.
- may be administered when heart failure has been controlled. Digitalisation and/or diuretic therapy should also be considered for patients with a history of heart failure, or patients known to have a poor cardiac reserve. Vasocardin SR I.V. Injection should be used with caution in patients where cardiac reserve is poor.
- may cause patients to develop increasing bradycardia, in such cases the Vasocardin SR I.V. Injection dosage should be reduced or gradually withdrawn.
- due to the negative effect on conduction time, should only be given with caution to patients with first-degree heart block.
- may increase the number and duration of angina attacks in patients with Prinzmetal's angina, due to unopposed alpha-receptor mediated coronary artery vasoconstriction. Vasocardin SR I.V. Injection is a beta1-selective beta-blocker; consequently, its use may be considered although utmost caution must be exercised.
- may mask the early signs of acute hypoglycaemia, in particular tachycardia. During treatment with Vasocardin SR I.V. Injection, the risk of interfering with carbohydrate metabolism or masking hypoglycaemia is less than with non-selective beta-blockers.
- may mask the symptoms of thyrotoxicosis.
- may increase both the sensitivity towards allergens and the seriousness of anaphylactic reactions.
Although cardioselective beta-blockers may have less effect on lung function than non-selective beta-blockers, as with all beta-blockers, these should be avoided in patients with reversible obstructive airways disease unless there are compelling clinical reasons for their use. When administration is necessary, these patients should be kept under close surveillance. The use of a beta2-bronchodilator (e.g. terbutaline) may be advisable in some patients. The dosage of the beta2-agonist may require an increase when treatment with Vasocardin SR I.V. Injection is commenced.
The label shall state - “Use with caution in patients who have a history of wheezing, asthma or any other breathing difficulties, see enclosed user leaflet.â€
Like all beta-blockers, careful consideration should be given to patients with psoriasis before Vasocardin SR I.V. Injection is administered.
In patients with a phaeochromocytoma, an alpha-blocker should be given concomitantly.
In labile and insulin-dependent diabetes it may be necessary to adjust the hypoglycaemic therapy.
Intravenous administration of calcium antagonists of the verapamil type should not be given to patients treated with beta-blockers.
A sudden discontinuation of beta blockade can be hazardous and should therefore be avoided. If treatment with Vasocardin SR tartrate needs to be discontinued, then this should be effected, as a rule, over at least 2 weeks, by halving the dosage incrementally until the patient is taking 25 mg of Vasocardin SR per dose (half a 50 mg tablet). This lowest dosage should be taken for at least 4 days until treatment is discontinued completely. Throughout this period, above all patients with ischaemic heart disease should be carefully monitored, since the risk of coronary events, including sudden cardiac death, is elevated whilst beta blockade is being discontinued. Hypertension and arrhythmia can also occur.
Even though Vasocardin SR, at the usual dosages, has less of a negative impact on the bronchial musculature than non-selective beta blockers, care should still be taken. In patients with bronchial asthma who are being treated with Vasocardin SR, bronchodilators that selectively stimulate β2 receptors, e.g. terbutaline, may be prescribed concomitantly if necessary. If the patient is already taking a β2 receptor stimulator, it may sometimes be necessary to adjust the dosage thereof.
Since beta blockers can affect the glucose metabolism, vigilance is advisable in patients with diabetes mellitus. The impact on the glucose metabolism and the masking effect on the symptoms of hypoglycaemia are less pronounced in patients treated with Vasocardin SR than in those treated with non-selective beta blockers (in particular tachycardia).
Vasocardin SR Tartrate tablets may not be administered to patients with untreated congestive heart failure. The congestive heart failure needs to be brought under control first of all. If concomitant digoxin treatment is taking place, it must be borne in mind that both medicinal products slow AV conduction and that there is therefore a risk of AV dissociation. In addition, mild cardiovascular complications may occur, manifesting as dizziness, bradycardia, and a tendency to collapse.
When a beta blocker is being taken, a serious, sometimes even life-threatening deterioration in cardiac function can occur, in particular in patients in whom the action of the heart is dependent on the presence of sympathetic system support. This is due less to an excessive beta-blocking effect and more to the fact that patients with marginal heart function tolerate poorly a reduction in sympathetic nervous system activity, even where this reduction is slight. This causes contractility to become weaker and the heart rate to reduce and slows down AV conduction. The consequence of this can be pulmonary oedema, AV block, and shock. Occasionally, an existing AV conduction disturbance can deteriorate, which can lead to AV block.
In the case of increasing bradycardia, the dosage should be reduced, or treatment, gradually discontinued.
Although contra-indicated in severe peripheral arterial circulatory disturbances , in the case of peripheral circulatory disorders, such as Raynaud's disease or peripheral arterial disease, the clinical picture may deteriorate, principally due to the medicinal product's hypotensive effect. Beta blockers should be administered with great caution if a deterioration in the clinical picture occurs.
If Vasocardin SR tartrate is prescribed to a patient with a phaeochromocytoma, an alpha blocker also needs to be administered.
Before a patient undergoes an operation, the anaesthetist must be informed that Vasocardin SR is being taken. In patients who have to undergo an operation, it is not recommended that beta blocker treatment be discontinued. Acute initiation of high-dose Vasocardin SR to patients undergoing non-cardiac surgery should be avoided, since it has been associated with bradycardia, hypotension and stroke including fatal outcome in patients with cardiovascular risk factors.
In patients who are taking a beta blocker, the occurrence of an anaphylactic shock is more serious.
Beta-blockers mask some of the clinical signs of thyrotoxicosis. Therefore, Vasocardin SR should be administered with caution to patients having, or suspected of developing, thyrotoxicosis, and both thyroid and cardiac function should be monitored closely
The administration of adrenaline to patients undergoing beta-blockade can result in an increase in blood pressure and bradycardia although this is less likely to occur with β 1-selective drugs
Beta-blockers may increase the number and duration of angina attacks in patients with Prinzmetal's angina (variant angina pectoris). However, relatively selective β1-receptor blockers, such as Vasocardin SR, can be used in such patients, but only with the utmost care.
Patients with anamnestically known psoriasis should take beta-blockers only after careful consideration.
In the presence of liver cirrhosis the bioavailability of Vasocardin SR may be increased.
In labile and insulin-dependent diabetes it may be necessary to adjust the hypoglycaemic therapy.
Intravenous administration of calcium antagonists of the verapamil-type should not be given to patients treated with beta-blockers.
The initial treatment of severe malignant hypertension should be so designed as to avoid sudden reduction in diastolic blood pressure with impairment of autoregulatory mechanisms.
Dry eyes either alone or, occasionally, with skin rashes has occurred. In most cases the symptoms cleared when Vasocardin SR treatment was withdrawn. Patients should be observed carefully for potential ocular effects. If such effects occur, discontinuation of Vasocardin SR should be considered.
A sudden discontinuation of beta blockade can be hazardous and should therefore be avoided. If treatment with Vasocardin SR needs to be discontinued, then this should be effected, as a rule, over at least 2 weeks, by halving the dosage incrementally until the patient is taking 25 mg of metoprolol per dose (half a 50 mg tablet). This lowest dosage should be taken for at least 4 days until treatment is discontinued completely. Throughout this period, above all patients with ischaemic heart disease should be carefully monitored, since the risk of coronary events, including sudden cardiac death, is elevated whilst beta blockade is being discontinued. Hypertension and arrhythmia can also occur.
Even though metoprolol, at the usual dosages, has less of a negative impact on the bronchial musculature than non-selective beta blockers, care should still be taken. In patients with bronchial asthma who are being treated with Metoprolol, bronchodilators that selectively stimulate β2 receptors, e.g. terbutaline, may be prescribed concomitantly if necessary. If the patient is already taking a β2 receptor stimulator, it may sometimes be necessary to adjust the dosage thereof.
Since beta blockers can affect the glucose metabolism, vigilance is advisable in patients with diabetes mellitus. The impact on the glucose metabolism and the masking effect on the symptoms of hypoglycaemia are less pronounced in patients treated with metoprolol than in those treated with non-selective beta blockers (in particular tachycardia).
Vasocardin SR tablets may not be administered to patients with untreated congestive heart failure. The congestive heart failure needs to be brought under control first of all. If concomitant digoxin treatment is taking place, it must be borne in mind that both medicinal products slow AV conduction and that there is therefore a risk of AV dissociation. In addition, mild cardiovascular complications may occur, manifesting as dizziness, bradycardia, and a tendency to collapse.
When a beta blocker is being taken, a serious, sometimes even life-threatening deterioration in cardiac function can occur, in particular in patients in whom the action of the heart is dependent on the presence of sympathetic system support. This is due less to an excessive beta-blocking effect and more to the fact that patients with marginal heart function tolerate poorly a reduction in sympathetic nervous system activity, even where this reduction is slight. This causes contractility to become weaker and the heart rate to reduce and slows down AV conduction. The consequence of this can be pulmonary oedema, AV block, and shock. Occasionally, an existing AV conduction disturbance can deteriorate, which can lead to AV block.
In the case of increasing bradycardia, the dosage should be reduced, or treatment, gradually discontinued.
Although contra-indicated in severe peripheral arterial circulatory disturbances , in the case of peripheral circulatory disorders, such as Raynaud's disease or peripheral arterial disease, the clinical picture may deteriorate, principally due to the medicinal product's hypotensive effect. Beta blockers should be administered with great caution if a deterioration in the clinical picture occurs.
If Vasocardin SR is prescribed to a patient with a phaeochromocytoma, an alpha blocker also needs to be administered.
Before a patient undergoes an operation, the anaesthetist must be informed that metoprolol is being taken. In patients who have to undergo an operation, it is not recommended that beta blocker treatment be discontinued. Acute initiation of high-dose metoprolol to patients undergoing non-cardiac surgery should be avoided, since it has been associated with bradycardia, hypotension and stroke including fatal outcome in patients with cardiovascular risk factors.
In patients who are taking a beta blocker, the occurrence of an anaphylactic shock is more serious.
Beta-blockers mask some of the clinical signs of thyrotoxicosis. Therefore, Metoprolol should be administered with caution to patients having, or suspected of developing, thyrotoxicosis, and both thyroid and cardiac function should be monitored closely
The administration of adrenaline to patients undergoing beta-blockade can result in an increase in blood pressure and bradycardia although this is less likely to occur with β 1-selective drugs
Beta-blockers may increase the number and duration of angina attacks in patients with Prinzmetal's angina (variant angina pectoris). However, relatively selective β1-receptor blockers, such as metoprolol, can be used in such patients, but only with the utmost care.
Patients with anamnestically known psoriasis should take beta-blockers only after careful consideration.
In the presence of liver cirrhosis the bioavailability of metoprolol may be increased.
In labile and insulin-dependent diabetes it may be necessary to adjust the hypoglycaemic therapy.
Intravenous administration of calcium antagonists of the verapamil-type should not be given to patients treated with beta-blockers.
The initial treatment of severe malignant hypertension should be so designed as to avoid sudden reduction in diastolic blood pressure with impairment of autoregulatory mechanisms.
Dry eyes either alone or, occasionally, with skin rashes has occurred. In most cases the symptoms cleared when metoprolol treatment was withdrawn. Patients should be observed carefully for potential ocular effects. If such effects occur, discontinuation of metoprolol should be considered.
Vasocardin SR I.V. Injection has minor influence on the ability to drive and use machines. It should be taken into account that occasionally dizziness or fatigue may occur.
As with all beta-blockers, Vasocardin SR has influence on the ability to drive and use machines because of dizziness and fatigue. This applies to a greater extent at the beginning of treatment. Patient should be warned accordingly.
As with all beta-blockers, metoprolol has influence on the ability to drive and use machines because of dizziness and fatigue. This applies to a greater extent at the beginning of treatment. Patient should be warned accordingly.
However, we will provide data for each active ingredient