Name | Carvedilol phosphate hemihydrate |
Synonyms | Carvedilol Phosphate CARVEDILOL PHOSPHATE Carvedilol Phosphate API BM 14190 (phosphate hemihydrate) Carvedilol phosphate hemihydrate 1-9H-(Carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propanolphosphateHemihydrate |
CAS | 610309-89-2 |
EINECS | 642-914-8 |
InChI | InChI=1/2C24H26N2O4.2H3O4P.H2O/c2*1-28-21-10-4-5-11-22(21)29-14-13-25-15-17(27)16-30-23-12-6-9-20-24(23)18-7-2-3-8-19(18)26-20;2*1-5(2,3)4;/h2*2-12,17,25-27H,13-16H2,1H3;2*(H3,1,2,3,4);1H2 |
Molecular Formula | C24H26N2O4.H2O.H3O4P |
Molar Mass | 522.488 |
Boling Point | 655.2°C at 760 mmHg |
Flash Point | 350.1°C |
Vapor Presure | 4.63E-18mmHg at 25°C |
In vitro study | Superoxide generation by activated human neutrophils in vitro is inhibited by Carvedilol with an IC 50 of 28 μM. Carvedilol is shown to scavenge oxygen free radicals in a cell-free system with an IC 50 of 25 μM. |
Pharmacological effects | Carvedilol phosphate is a selective blocking α1-receptor and non-selective β-receptor blocker, no intrinsic Sympathimetic active drugs, bioavailability of 10 ~ 47%, not affected by food, the effect on α1-receptor is significantly lower than β1-and β2-receptor, the intensity ratio of β 1-and β 2-receptor blockade is 1:10~1:100. The effect of β 1-receptor blockade is about 1/2 of labetalol, and its α1 blockade is weaker than prazosin. It can dilate blood vessels, reduce peripheral vascular resistance, dilate coronary and renal vessels, and reduce pulmonary wedge pressure. It has obvious protective effect on myocardial hypoxia and myocardial injury caused by myocardial infarction, which may be related to blocking β-receptor, which can reduce the decrease of myocardial glycogen and the increase of pH, and reduce the infarct size. |
uses | carvedilol phosphate is used to treat mild to moderate hypertension and can be used alone or in combination with other antihypertensive drugs (especially thiazide diuretics). For symptomatic chronic congestive heart failure. |
usage and dosage | tablets: 2.5mg;6.25mg;10mg;20mg. Capsule: 10mg. The dose must be individualized and should be added under the close monitoring of the physician. The initial oral dose of hypertension is 6.25mg each time, 2 times a day. If tolerated, the vertical systolic blood pressure 1 hour after taking the medicine can be used as a guide to maintain the dose for 7 to 14 days, and then according to the valley concentration The blood pressure is increased to 12.5mg each time, 2 times a day if necessary. Similarly, the dose can be increased to 25mg each time, 2 times a day. Generally, complete antihypertensive effect is achieved within 7~14 days. The total amount shall not exceed 50mg per day. This product must be taken with food to slow down absorption and reduce the occurrence of orthostatic hypotension. Adding diuretics on the basis of this product or adding this product on the basis of diuretics is expected to produce cumulative effects and increase the postural effects of this product. |
Biological activity | Carvedilol phosphate hemihydrate (BM 14190 phosphate hemihydrate) is a non-selective β/α-1 receptor blocker. Carvedilol inhibit lipid peroxidation with an IC50 of 5 μM. Carvedilol is a multi-purpose antihypertensive agent with potential for the study of angina pectoris and congestive heart failure. Carvedilol is an autophagy (autophagy) inducer that inhibits NLRP3 inflammasome. |
target | β/α-1 adrenergic receptor IC50: 5 μM (lipid peroxidation) Autophagy |