Nessili

Nesipide Chinese Description

Description Natrecor® (Nexitide) is a novel drug, a sterile preparation of human B-type natriuretic peptide (hBNP), prepared from E. coli using recombinant DNA techniques. The molecular weight of nesiceptin is 3464g / mol, and the empirical formula is C143H244N50O42S4. Nesiritide has the same 32 amino acid sequence as the endogenous peptide, which is produced by the ventricular myocardium. Natrecor is formulated as a citrate salt of rhBNP and is provided in a sterile disposable vial. Each 1.5 mg vial contains a white to off-white lyophilized powder for intravenous (IV) administration after reconstitution. The quantitative composition of each bottle of lyophilized drug was: 1.58 mg of nesiceptin, 20.0 mg of mannitol, 2.1 mg of citric acid monohydrate, and 2.94 mg of sodium citrate dihydrate. The mechanism of action of human BNP binds to the granule guanylate cyclase receptor of vascular smooth muscle and endothelial cells, resulting in increased intracellular concentrations of guanosine 3'5'-cyclic monophosphate (cGMP) and smooth muscle cell relaxation. Circulating GMP acts as a second messenger to dilate veins and arteries. Nesiritide has been shown to relax isolated arterial and venous tissue preparations that pre-contract with endothelin-1 or the alpha-adrenergic agonist phenylephrine. In human studies, nesiritide produced a dose-dependent reduction in pulmonary capillary wedge pressure (PCWP) and systemic arterial pressure in patients with heart failure. In animals, nesiritide has no effect on cardiac contractility or cardiac electrophysiological measurements, such as atrial and ventricular effective refractory time or atrioventricular node conduction. The naturally occurring atrial natriuretic peptide (ANP) is a related peptide that increases vascular permeability in animals and humans and reduces the amount of vascular content. The effect of nesiceptin on vascular permeability has not been studied. Pharmacokinetics In patients with congestive heart failure (CHF), Natrecor administered intravenously by infusion or bolus showed biphasic treatment from plasma. Natrecor's average terminal elimination half-life (t1 / 2) is approximately 18 minutes and is associated with approximately 2/3 of the area under the curve (AUC). The average initial elimination phase is estimated to be approximately 2 minutes. In these patients, the average volume of the Natrecor central chamber (Vc) was estimated to be 0.073 L / kg, the mean steady-state volume (Vss) was 0.19 L / kg, and the mean clearance (CL) was about 9.2 ml / min / kilogram. At steady state, plasma BNP levels increased approximately 3- to 6-fold from baseline endogenous levels, and Natrecor infusion doses ranged from 0.01 to 0.03 μg/kg/min. Elimination of clearance from human BNP by three independent mechanisms, reduced importance: 1) binding to cell surface clearance receptors, followed by cell internalization and lysosomal proteolysis; 2) by endopeptidases (eg neutral endopeptides) Enzyme) proteolytic cleavage of the peptide, the endopeptidase is present on the surface of the vascular lumen; 3) renal filtration. In the special population, although the Natrecor part was eliminated by renal clearance, clinical data indicate that patients with renal insufficiency do not need to adjust the dose. Natrecor's effects on PCWP, cardiac index (CI), and systolic blood pressure (SBP) were not significantly different in patients with chronic renal insufficiency (baseline serum creatinine range of 2 mg/dL to 4.3 mg/dL) and patients. Renal function is normal. Population pharmacokinetic (PK) analysis was performed to determine the effect of demographic and clinical variables on PK parameters, indicating that Natrecor's clearance is proportional to body weight and supports the weight-adjusted dose of Natrecor (ie, in μg/give Medicine) kg / min (basis). Age, gender, race/ethnicity, baseline endogenous hBNP concentration, CHF severity (as indicated by baseline PCWP, baseline C1 or New York Heart Association [NYHA] classification) or concurrent administration of ACE inhibitors had no significant effect on clearance . Concomitant drug effects The co-administration of Natrecor with enalapril had no significant effect on Natrecor's PK. The PK effect of Natrecor in combination with other IV vasodilators such as nitroglycerin, sodium nitroprusside, milrinone or IV ACE inhibitors has not been evaluated. Natrecor is used concurrently with other drugs during clinical studies, including: diuretics, digoxin, oral ACE inhibitors, anticoagulants, oral nitrates, statins, class III antiarrhythmic drugs, beta-receptors Blockers, dobutamine, calcium channel blockers, angiotensin II receptor antagonists, and dopamine. Although there is no specific assessment of PK interactions, there appears to be no evidence of any clinically significant PK interaction. Pharmacodynamics Natrecor's recommended dosing regimen is an intravenous bolus of 2 μg/kg followed by an intravenous infusion of 0.01 μg/ Read more...

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Nebirol Chinese Description

Indications and Usage Hypertension BYSTOLIC is indicated for the treatment of hypertension and lowering blood pressure [see Clinical Studies (14.1)]. BYSTOLIC can be used alone or in combination with other antihypertensive drugs. Lowering blood pressure reduces the risk of fatal and non-fatal cardiovascular events, mainly stroke and myocardial infarction. These benefits have been seen in controlled trials of antihypertensive drugs from a variety of pharmacological classes, including the categories to which the drug primarily belongs. No controlled trials have shown that BYSTOLIC reduces risk. Controlling hypertension should be part of a comprehensive cardiovascular risk management, including proper lipid management, diabetes management, antithrombotic therapy, smoking cessation, exercise, and limited sodium intake. Many patients need more than one drug to reach their blood pressure goals. For specific recommendations on goals and management, please refer to published guidelines such as the United Nations Home Prevention, Testing, Assessment and Hypertension Treatment Committee (JNC) guidelines for the National Hypertension Education Program. Many antihypertensive drugs, from a variety of pharmacological classes, have different mechanisms of action, have been shown in randomized controlled trials to reduce cardiovascular morbidity and mortality, and can conclude that it is a drop in blood pressure, not Some other pharmacological properties. The drug is primarily responsible for these benefits. The greatest and most consistent cardiovascular outcome benefit is reduced stroke risk, but myocardial infarction and cardiovascular mortality are often seen. An increase in systolic or diastolic blood pressure leads to an increase in cardiovascular risk and an increased absolute risk per mmHg when blood pressure rises, so even a modest reduction in severe hypertension can provide substantial benefits. In people with different absolute risks, the relative risk reduction of blood pressure reduction is similar, so the absolute benefit of patients who are at higher risk of hypertension (eg, patients with diabetes or hyperlipidemia) is greater, And such patients will be expected to benefit from more aggressive treatments to lower blood pressure goals. Some antihypertensive drugs have a lower blood pressure effect in black patients (as monotherapy), and many antihypertensive drugs have additional approved indications and effects (eg, for angina, heart failure, or diabetic nephropathy). These considerations can guide the choice of treatment. Dosage and administration of high dose BYSTOLIC must be personalized according to the needs of the patient. For most patients, the recommended starting dose is 5 mg once daily, with or without food, monotherapy or in combination with other drugs. For patients who need to further lower their blood pressure, the dose can be increased to 40 mg at 2 week intervals. More frequent dosing regimens are unlikely to be beneficial. Renal insufficiency In patients with severe renal insufficiency (ClCr less than 30 mL / min), the recommended initial dose is 2.5 mg per day; if necessary, slowly titrate. The BYSTOLIC study has not been performed on patients undergoing dialysis [see Clinical Pharmacology (12.4)]. Hepatic impairment In patients with moderate hepatic impairment, the recommended initial dose is 2.5 mg per day; if necessary, slowly titrate. BYSTOLIC has not been studied in patients with severe liver damage and is therefore not recommended for use in this population [see Clinical Pharmacology (12.4)]. Subgroups of elderly patients do not need to adjust the dose of the elderly [see use in special populations (8.5)]. The CYP2D6 polymorphism does not require dose adjustment for patients with CYP2D6 malnutrition. The clinical effects and safety observed in patients with poor metabolism are similar to those of a wide range of metabolizers [see Clinical Pharmacology (12.3)]. Dosage Form and Strength BYSTOLIC can be used as a tablet for oral administration containing nebivolol hydrochloride equivalent to 2.5, 5, 10 and 20 mg of nebivolol. BYSTOLIC tablets are triangular, biconvex, unnotched, and of different colors, with "FL" engraved on one side and mg (21⁄2, 5, 10 or 20) on the other side. Contraindications BYSTOLIC is contraindicated in the following cases: severe bradycardia, cardiac arrest, greater than one degree of cardiogenic shock, decompensated heart failure, sick sinus syndrome (unless there is a permanent pacemaker), severe liver damage ( Child-Pugh> B) A patient who is allergic to any of the ingredients in this product. Warnings and Precautions Sudden Stop Treatment Do not suddenly stop BYSTOLIC treatment in patients with coronary artery disease. After sudden discontinuation of treatment with beta blockers, patients with coronary artery disease have reported severe exacerbations of angina, myocardial infarction, and ventricular arrhythmias. Myocardial infarction and ventricular arrhythmias can occur with or without prior deterioration of angina. Be careful not to interrupt or suddenly stop treatment in patients without significant coronary artery disease. As with other beta blockers, when planning to discontinue BYSTOLIC, carefully observe and advise patients to minimize physical activity. If possible, gradually reduce BYSTOLIC for 1 to 2 weeks. If angina worsens or acute coronary insufficiency develops, restart BYSTOLIC immediately, at least temporarily. Angina and acute myocardial infarction BYSTOLIC have not been studied in patients with angina or recent myocardial infarction. Bronchospasm In general, patients with bronchospasm should not receive beta-blockers. Anesthesia and major surgery Because the withdrawal of beta blockers is associated with an increased risk of MI and chest pain, patients who have taken beta blockers should generally continue treatment throughout the perioperative period. If BYSTOLIC continues to be used during the perioperative period, patients are closely monitored when using anesthetics that inhibit myocardial function, such as diethyl ether, cyclopropane, and trichloroethylene. If the beta-blocking therapy is withdrawn prior to major surgery, impaired cardiac responsiveness to reflex adrenergic stimulation may increase the risk of general anesthesia and surgery. The beta-blocking effect of BYSTOLIC can be reversed by beta-agonists such as dobutamine or isoproterenol. However, these patients may suffer from persistent severe hypotension. In addition, beta blockers have been reported to be difficult to restart and maintain heartbeat. Read more...

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