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Bisoprolol fumarate

Pharmacological effects Indications Method and Dosage Distinguish Content Determine Drug interactions Precautions Side effects Category Toxicity Acute toxicity Flammability hazard characteristics Storage Characteristics Extinguishing agent

CAS No. 104344-23-2
Chemical Name: Bisoprolol fumarate
Synonyms: EMCOR;SOPROL;ZEBETA;ISOTEN;CONCOR;Azopsin;Well-bi;Seafuri;MONOCOR;Bisotate
CBNumber: CB8371980
Molecular Formula: C22H35NO8
Formula Weight: 441.52
MOL File: 104344-23-2.mol
Bisoprolol fumarate Property
Melting point : 100°C
storage temp. : Store at RT
solubility : DMSO: >20 mg/mL
form : solid
color : white
CAS DataBase Reference: 104344-23-2(CAS DataBase Reference)
SAFETY
  • Risk and Safety Statements
  • Hazard and Precautionary Statements (GHS)
Hazard Codes : Xn,Xi
Risk Statements : 22
WGK Germany : 3
RTECS : UB8390000
HazardClass : IRRITANT
Symbol(GHS):
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H302 Harmful if swallowed Acute toxicity,oral Category 4 Warning P264, P270, P301+P312, P330, P501
Precautionary statements:
P264 Wash hands thoroughly after handling.
P264 Wash skin thouroughly after handling.
P270 Do not eat, drink or smoke when using this product.
P330 Rinse mouth.

Bisoprolol fumarate Chemical Properties,Usage,Production

Pharmacological effects
Bisoprolol fumarate is a selective β1-adrenergic receptor blockers. No intrinsic sympathomimetic activity and membrane stabilizing effect. Animal experiments of different models show that affinity for β1-receptor is 11 to 34-fold larger than β2-receptor. The selectivity for β1 receptor is four times of the similar drugs Atenolol. This product plays the role for a long time (24 hours or more), continual application takes good control of symptoms without tolerance phenomenon, with minimal side effects on the respiratory system, no effects on metabolism of fat. it also has a certain degree of block effect for bronchial β2 receptors, but it may only occur at high doses, usually it has no obvious clinical significance.
Indications
Treatment of essential hypertension. As first-line antihypertensive agents, it can be used alone or combined with diuretics and vasodilator drugs.
Angina and myocardial infarction.
Arrhythmias, such as the rapid ventricular arrhythmia, ventricular contraction.
In recent years, bisoprolol fumarate is also tempted used for the treatment of heart failure. It is effective for moderate to severe chronic stable heart failure which previously receiving ACE inhibitors, diuretics and cardiac glycosides medications associated with ventricular systolic dysfunction (ejection fraction ≤35%) .
The above information is edited by the chemicalbook of Tian Ye.
Method and Dosage
Hypertension: The initial dose is 5mg once, 1 times a day. It may be suitable for some patients to start with initial dose of 2.5mg (such as bronchial spasm disease). If the dose of 5 mg one day is not enough for antihypertensive effect , the dose may be increased to 10-20mg one day .
Angina: initial dose of 2.5mg, 1 time a day, the maximum daily dose can not exceed 10mg.
Heart failure: chronic, stable heart failure: it should start from small dose, if it is tolerated, the dose can gradually increasing (doubling the dose every 2-4 weeks) to the maximum tolerated dose or target dose. The maximum recommended target dose is 10mg one day , the starting dose is usually 1/8 of the target dose.
Distinguish
Take appropriate amount of this product powder (about the equivalent of bisoprolol fumarate 20mg), add 4ml water to dissolve, the filtrate is added 1 to 3 drops of potassium permanganate test solution , purple should fade , and brown precipitate forms.
Take right amount of this product powder,it is dissolved in water and form the solution of which 1ml each contains about 0.1mg bisoprolol fumarate,after filtration, take continued filtrate, according to the UV-visible spectrophotometry (Appendix Ⅳ A) measure ,there is the maximum absorption in the 271nm wavelength.
In the chromatogram recorded under the item of content determination ,the test solution peak retention time should be consistent with the reference solution peak retention time.
Content Determine
Take 10 tablets of this product , weigh accurately, porphyrize, accurately weigh appropriate amount (about the equivalent of bisoprolol fumarate 5mg), set it into 50ml volumetric flask, add water to make bisoprolol fumarate dissolve and dilute it to the mark , shake, filtrate, according to chromatographic conditions under the item of bisoprolol fumarate related substances,take the precise amount of continued filtrate 20μl into the liquid chromatograph, record the chromatograms; in addition , precisely weigh appropriate amount of the reference bisoprolol fumarate , dissolve it in water and dilute into the solution of which 1ml each contains about 0.1mg,measure in the same method, calculate according to the external standard method bisoprolol peak area ,it is obtained .
Drug interactions
1.when bisoprolol fumarate is used in combination with other anti-hypertensive drugs, the antihypertensive effect is enhanced .
2. when bisoprolol fumarate is used in combination with reserpine, methyldopa, clonidine or guanfacine, the heart rate can be slowed down.
3. when bisoprolol fumarate is used in combination with reserpine, reserpine needs to be stopped a few days after stop of this product .
4. when bisoprolol fumarate is used in combination with nifedipine, the antihypertensive effect of this product can be enhanced .
5. when bisoprolol fumarate is used in combination with verapamil or diltiazem ketones calcium icon antagonists or other antiarrhythmic drugs , there is the need for patient care, because they can cause hypotension, bradycardia and others.
Precautions
Diabetic patients with great blood glucose fluctuations or acidosis patients should be careful in use of it.
Patients with pulmonary insufficiency, severe liver and kidney dysfunction should use with caution.
Interruption of treatment should diminish doses daily ,when it is used in combination with other antihypertensive drugs, the dose often requires reductions.
when drug overdose causes slow heartbeat or low blood pressure , patients must immediately stop taking this product. If necessary, take separate or sequential use of following drugs, atropine 0.5mg~2.0mg intravenously, appropriate amount of metaproterenol slow intravenous injection; glucagon 1mg~5mg (or 1mg~10mg).
Because the antihypertensive effect of bisoprolol fumarate, capacity of the patient to drive or operate the machine may be weakened , particularly at the beginning of taking medication or conversion medication and taking with alcohol at the same time, but the person's ability to respond will not be directly affected .
Side effects
1.In early medication, mild fatigue, chest tightness, dizziness, bradycardia, drowsiness, palpitations, headache and lower limb edema may appear , and all automatically reduce or disappear after continuing taking .
2. In rare cases, there will be gastrointestinal disorders (diarrhea, constipation, nausea, abdominal pain) and skin reactions (eg erythema, itching).
3. Occasionally blood pressure decreases , pulse slow or atrioventricular conduction disorders.
4.Sometimes there will be tingling or cold extremities, in rare cases, it can cause muscle weakness, muscle cramps and less tears.
5.For patients with intermittent claudication or Raynaud's phenomenon,during the initial medication, the condition may worsen, the condition of existing myocardial dysfunction patients will possibly aggravate.
6.Occasionally airway resistance may increase .
7.Elderly patients with diabetes, their glucose tolerance may reduce , which may cover hypoglycemia manifestations (such as rapid heartbeat).
Category
Toxic substances
Toxicity
Moderate poisoning
Acute toxicity
Oral-rat LD50: 940 mg/kg; Oral-Mouse LD50: 678 mg/kg
Flammability hazard characteristics
Combustible; fire decomposition with toxic nitrogen oxide fumes
Storage Characteristics
Treasury temperature, ventilation, dry
Chemical Properties
White Solid
Extinguishing agent
Water, carbon dioxide, dry, sandy soil
Uses
antiinflammatory
Uses
A selective β-adrenergic blocker. Used as an antihypertensive.
Uses
semi-synthetic kanamycin-derived aminoglycoside antibiotic
Uses
Labeled Bisoprolol, intended for use as an internal standard for the quantification of Bisoprolol by GC- or LC-mass spectrometry.
Uses
A selective a-adrenergic blocker. Used as an antihypertensive
Uses
A selective α-adrenergic blocker. Used as an antihypertensive.
Biological Activity
A selective β 1 -adrenergic antagonist. Has a K d of 2-3 nM at the β 1 receptor and a β 1 / β 2 selectivity of approximately 100-fold.
Bisoprolol fumarate Preparation Products And Raw materials
Raw materials
Preparation Products
Bisoprolol fumarate Suppliers      Global( 216)Suppliers     
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Beijing Cooperate Pharmaceutical Co.,Ltd. +86-10-60279497 +86(0)15646567669
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Beijing Lianben Pharm-Chemicals Tech. Co., Ltd +86-10-83386766
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Chongqing Landtower Pharmaceutical Co., Ltd. 023-68980308
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CGeneTech (Suzhou, China) Co., Ltd. 0512-62956963
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Meryer (Shanghai) Chemical Technology Co., Ltd. +86-(0)21-61259100(Shanghai) +86-(0)755-86170099(ShenZhen) +86-(0)10-62670440(Beijing)
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(+-)-1-(p-((2-isopropoxyethoxy)methyl)phenoxy)-3-isopropylamino-2-propanolh (+-)-mino)(e)-2-butenedioate(2:1)(salt) 2-propanol,1-(4-((2-(1-methylethoxy)ethoxy)methyl)phenoxy)-3-((1-methylethyl)a C18H31NO4C4H4O4C22H35NO8 C36H64N2O12 C40H66O12N2 NegativeioncolophonyPolymer 1-[4-[[2-(1-Methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]propan-2-ol hemifumarate C18H31NO412C4H4O4 Intermediates & Fine Chemicals Pharmaceuticals 1-[4-[[2-(1-Methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanol hemifumarate salt C18H31NO45C4H4O4 C36H62N2O8C4H4O4 (±)-1-((alpha-(2-Isopropoxyethoxy)-p-tolyl)oxy)-3-(isopropylamino)-2-propanol fumarate Adrenoceptor Azopsin Bisotate Seafuri Well-bi C18H31NO4C4H4O4C22H Bisoprolol fumarate (±)-1-[4-[[2-(1-Methylethoxy)ethoxy)methyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanolhemifumarate C18H31NO4189C4H4O4 Bisoprolol Fumarate (200 mg) Bisoprolol FuMarate, USP 1-(propan-2-ylaMino)-3-(4-{[2-(propan-2-yloxy)ethoxy]Methyl}phenoxy)propan-2-ol 1-(4-((2-isopropoxyethoxy)Methyl)phenoxy)-3-(isopropylaMino)propan-2-ol fuMarate CELESTOVET eMifuMarate bisoprolol fuMarate bisoprololheMifuMarate (2RS) -1-{4-[(2-isopropoxyethoxy)Methyl]phenoxy}-3-(isopropylaMino)propan-2-ol fuMarate Bisoprolol f 1-[4-[[2-(1-methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanol,(2E)-2-butenedioate (2:1) Bisoprolol for system suitability Bisoprolol for peak identification emd33512 emifumarate MONOCOR SOPROL ZEBETA ISOTEN (+/-)-BISOPROLOL HEMIFUMARATE BISOPROLOL HEMIFUMARATE EURADIAL DETENSIEL EMCOR CONCOR 104344-23-2 1-[4-[[2-(1-METHYLETHOXY)ETHOXY]METHYL]PHENOXY]-3-[(1-METHYLETHYL)AMINO]-2-PROPANOL (+/-)-1-[4-[[(2-(1-METHYLETHOXY)ETHOXY)METHYL]PHENOXY]-3-[(1-METHYLETHYL)AMINO]-2-PROPANOL] HEMIFUMARATE C40H66N2O12 C22H35NO8 1-[4-[[2-(1-Methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanol, Concor, Detensiel, Emcor, Euradial, Isoten, Monocor, Soprol, Zebeta, 2-Propanol, 1-[4-[[2-(1-methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-, (+-)-, (E)-2-butenedioate (2:1) (salt) (8CI) 2-Propanol, 1-[4-[[2-(1-methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-, (2E)-2-butenedioate (2:1) (salt) 2-Propanol, 1-[4-[[2-(1-methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-, (E)-2-butenedioate (2:1) (salt) Emvoncor Eurtadal
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