What Is Bisoprolol Fumarate?

Bisoprolol fumarate is a -receptor blocker, which has a high affinity for 1-receptors in bronchial and vascular smooth muscle, thereby dilating blood vessels and lowering blood pressure. Applicable to hypertension, coronary heart disease, and moderate to severe chronic stable heart failure.

Bisoprolol fumarate

Bisoprolol fumarate is

[Ingredients]

The main ingredient of this product is bisoprolol fumarate

[Character]

This product is a film-coated tablet.

Hypertension, coronary heart disease (angina pectoris).

Moderate to severe chronic stable heart failure with impaired ventricular systolic function (ejection fraction 5% 35%, determined from echocardiogram). Before using this product, you need to receive treatment with ACE inhibitors, diuretics, and selective use of cardiac glycosides.

For all indications:

This product should be taken in the morning and can be taken with meals.

Treatment of hypertension or angina:

Usually 5mg bisoprolol fumarate once daily.

Treatment of chronic stable heart failure:

The use of bisoprolol for chronic stable heart failure should start with a low dose and gradually increase the dose according to the following scheme:

1.25mg once daily for 1 week, if it is well tolerated, increase to

2.5mg once a day, continue medication for 1 week, if tolerated, increase to

3.75mg once a day, continue medication for 1 week, if tolerated, increase to

5mg once daily for 4 weeks, if it is well tolerated, increase to

7.5mg once daily for 4 weeks, if it is well tolerated, increase to

10mg once daily as maintenance treatment

The maximum recommended dose is 10 mg once daily.

Liver and kidney dysfunction:

Patients with mild to moderate liver and kidney dysfunction usually do not need to adjust the dose. For patients with advanced renal failure (creatinine clearance <20ml / min) and severe liver dysfunction, the daily dose should not exceed 10mg.

Bisoprolol is contraindicated in the following patients:

1.

Pharmacology:

Bisoprolol is a highly selective 1-adrenoreceptor antagonist.

Bisoprolol is almost completely absorbed from the gastrointestinal tract (> 90%). Because the first-pass effect of the liver is small (<10%), it exhibits up to about 90% bioavailability. Bisoprolol

Revisions of the 2010 Chinese Pharmacopoeia:

Bisoprolol fumarate (draft for comment)

Fumasuan Bisuoluo'er

Bisoprolol Fumarate

(C18H31NO4) 2 · C4H4O4 766.96

This product is (±) 1- [4-[[2- (1-methylethoxy) ethoxy] methyl] -phenoxy] -3 [(1-methylethyl) amino] -2-propanol fumarate. Calculated on dry basis, containing (C18H31NO4) 2 · C4H4O4 shall not be less than 99.0%.

[Properties] This product is white powder; odorless.

This product is very soluble in water, easily soluble in ethanol, slightly soluble in acetone, and insoluble in ether.

Melting point The melting point of this product (Appendix VI C) is 100 ° C to 104 ° C.

[Identification] (1) Take about 10mg of this product, add 2ml of water to dissolve, add 1 to 3 drops of potassium permanganate test solution, the purple red should fade, and brownish yellow precipitates are formed.

(2) Take this product, dissolve it with water and dilute it separately to make solution A containing 0.1mg per 1ml and solution B containing 0.01mg per 1ml. Solution A had maximum absorption at a wavelength of 271 nm; solution B had maximum absorption at a wavelength of 223 nm.

(3) The infrared light absorption spectrum of this product should be consistent with the control spectrum (spectrum set 859).

[Check] Take 0.50g of this product for acidity, dissolve it by adding 10ml of water, and measure it according to law (Appendix VI H). The pH value should be 6.0 7.0.

The clarity of the solution is 0.50 g of this product. After adding 10 ml of water to dissolve, the solution should be clear (Appendix B).

Take the appropriate amount of this substance, dissolve and dilute with water to make a solution containing about 0.5mg per 1ml as the test solution; take a precise amount and dilute with water to make a solution containing about 5g per 1ml, as the control solution . According to

[Indications]

For the treatment of essential hypertension and angina pectoris. [Chemical composition] The main ingredients and chemical name of this product are: 1- [4-[[2- (1-methylethoxy) ethoxy] methyl] -phenoxy] -3-[(1 -Methylethyl) amino] -2-propanol fumarate.

[Pharmacological action]

This product is a selective 1-adrenergic receptor blocker. There is no intrinsic sympathomimetic activity and membrane stabilization. Experiments in different model animals show that its affinity for 1-receptor is 11-34 times greater than that of 2-receptor, and its selectivity for 1 receptor is 4 times that of similar drug Atenolol. This product has a long acting time (more than 24 hours), continuous taking has good control symptoms and no intolerance, has minimal side effects on the respiratory system, and has no effect on fat catabolism.

medicine interactions

1 The antihypertensive effect of this product is enhanced when used in combination with other antihypertensive drugs.

2 This product can slow down heart rate when used in combination with reserpine, methyldopa, clonidine or chlorphenidamine.

3 When combined with reserpine, reserpine should be discontinued after a few days of discontinuation of this drug.

4 Combined with Xintongding can enhance the antihypertensive effect of this product.

5 When used in combination with cardiac arrest or azathione calcium antagonists or other antiarrhythmic drugs, the patient must be monitored because it can cause hypotension, bradycardia and others.

Adverse reactions

1 Mild fatigue, chest tightness, dizziness, bradycardia, drowsiness, palpitations, headache, and lower extremity swelling may occur at the beginning of medication, and all of them will be relieved or disappeared automatically after continued medication.

2 In rare cases, gastrointestinal disorders (diarrhea, constipation, nausea, abdominal pain) and skin reactions (such as erythema, itching) can occur.

3 Occasionally a significant drop in blood pressure, slow pulse or atrioventricular conduction disorder.

4 Sometimes tingling sensation or cold limbs, in rare cases, can lead to muscle weakness, muscle painful spasms and less tears.

5 For patients with intermittent claudication or Raynaud's phenomenon, the condition may worsen at the beginning of the medication, and the original myocardial dysfunction may also worsen.

6 Occasionally increased airway resistance.

7 Elderly patients with diabetes may have impaired glucose tolerance and mask hypoglycemia (such as faster heartbeat).

Contraindications

1 shock, atrioventricular conduction disorder (second and third degree atrioventricular block), sick sinus syndrome, sinoatrial block, bradycardia (below 50 / min), low blood pressure, bronchial asthma and peripheral circulation disorder Late.

2 Adrenal tumor (pheochromocytoma), this product can only be taken after using -receptor blockers.