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Esmolol hydrochloride has the molecular formula C16H26NO4CI and a molecular weight of 331.8. It has one asymmetric center and exists as an enantiomeric pair.Esmolol Hydrochloride is a white to off-white crystalline powder. It is a relatively hydrophilic compound which is very soluble in water and freely soluble in alcohol. Its partition coefficient (octanol/water) at pH 7.0 is 0.42 compared to 17.0 for propranolol.Esmolol HCl Injection is a clear, colorless to light yellow, sterile, nonpyrogenic solution.Esmolol powder
100 mg, 10 mL Single Dose Vial - Each mL contains 10 mg Esmolol Hydrochloride and Water for Injection; buffered with 2.8 mg Sodium Acetate Trihydrate and 0.546 mg Glacial Acetic Acid. Sodium Hydroxide and/or Hydrochloric Acid added, as necessary, to adjust pH to 4.5 to 5.5.
3CLINICAL PHARMACOLOGY
Esmolol hydrochloride is a beta1-selective (cardioselective) adrenergic receptor blocking agent with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilizing activity at therapeutic dosages. Its elimination half-life after intravenous infusion is approximately 9 minutes. Esmolol inhibits the beta1 receptors located chiefly in cardiac muscle, but this preferential effect is not absolute and at higher doses it begins to inhibit beta2 receptors located chiefly in the bronchial and vascular musculature.
3.1Pharmacokinetics and Metabolism
Esmolol hydrochloride is rapidly metabolized by hydrolysis of the ester linkage, chiefly by the esterases in the cytosol of red blood cells and not by plasma cholinesterases or red cell membrane acetylchoIinesterase. Total body clearance in man was found to be about 20 L/kg/hr, which is greater than cardiac output; thus the metabolism of esmolol is not limited by the rate of blood flow to metabolizing tissues such as the liver or affected by hepatic or renal blood flow. Esmolol has a rapid distribution half-life of about 2 minutes and an elimination half-life of about 9 minutes.
Using an appropriate loading dose, steady-state blood levels of esmolol for dosages from 50 to 300 mcg/kg/min (0.05 to 0.3 mg/kg/min) are obtained within five minutes. (Steady-state is reached in about 30 minutes without the loading dose.) Steady-state blood levels of esmolol increase linearly over this dosage range and elimination kinetics are dose-independent over this range. Steady-state blood levels are maintained during infusion but decrease rapidly after termination of the infusion. Because of its short half-life, blood levels of esmolol can be rapidly altered by increasing or decreasing the infusion rate and rapidly eliminated by discontinuing the infusion.
Consistent with the high rate of blood-based metabolism of esmolol, less than 2% of the drug is excreted unchanged in the urine. Within 24 hours of the end of infusion, approximately 73% to 88% of the dosage has been accounted for in the urine as the acid metabolite of esmolol.
Metabolism of esmolol results in the formation of the corresponding free acid and methanol. The acid metabolite has been shown in animals to have about 1/1500th the activity of esmolol and in normal volunteers its blood levels do not correspond to the level of beta blockade. The acid metabolite has an elimination half-life of about 3.7 hours and is excreted in the urine with a clearance approximately equivalent to the glomerular filtration rate. Excretion of the acid metabolite is significantly decreased in patients with renal disease, with the elimination half-life increased to about ten-fold that of normals, and plasma levels considerably elevated.
Methanol blood levels, monitored in subjects receiving esmolol for up to 6 hours at 300 mcg/kg/min (0.3 mg/kg/min) and 24 hours at 150 mcg/kg/min (0.15 mg/kg/min), approximated endogenous levels and were less than 2% of levels usually associated with methanol toxicity.Esmolol has been shown to be 55% bound to human plasma protein, while the acid metabolite is only 10% bound.
Purpose: The objective of this study was to evaluate the thermal behavior of crystalline and amorphous bisoprolol fumarate and its compatibility with amorphous valsartan. This pharmacologically relevant drug combination is a potential candidate for fixed-dose combination formulation. Methods: DSC and TMDSC were used to examine thermal behavior of bisoprolol fumarate. SSNMR and XRPD were applied to probe the solid state forms. The thermal behavior of physical mixtures with different concentrations of bisoprolol and valsartan were examined by DSC and TMDSC, and the observed interactions were investigated by XRPD, solution- and solid-state NMR. Results: The phase transitions from thermal methods and solid-state NMR spectra of crystalline and amorphous bisoprolol fumarate are reported.Bisoprolol
Strong interactions between bisoprolol fumarate and valsartan were observed above 60 C, resulting in the formation of a new amorphous material. Solution- and solid-state NMR provided insight into the molecular nature of the incompatibility. Conclusions: A combined analysis of thermal methods, solution- and solid-state NMR and XRPD experiments allowed the investigation of the conformational and dynamic properties of bisoprolol fumarate. Since bisoprolol fumarate and valsartan react to form a new amorphous product, formulation of a fixed-dose combination would require separate reservoirs for bisoprolol and valsartan to prevent interactions. Similar problems might be expected with other excipients or APIs containing carboxylic groups.
Bisoprolol fumarate has a molecular weight of 766.97. It is a white crystalline powder which is approximately equally hydrophilic and lipophilic, and is readily soluble in water, methanol, ethanol, and chloroform.
Bisoprolol Fumarate Tablets, USP is available as 5 and 10 mg tablets for oral administration.
Inactive ingredients include colloidal silicon dioxide, partially pregelatinized starch, crospovidone, anhydrous dibasic calcium phosphate, hypromellose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, titanium dioxide and talc.
Bisoprolol fumarate is a beta1-selective (cardioselective) adrenoceptor blocking agent without significant membrane stabilizing activity or intrinsic sympathomimetic activity in its therapeutic dosage range. Cardioselectivity is not absolute, however, and at higher doses ( 20 mg) Bisoprolol fumarate also inhibits beta2-adrenoceptors, chiefly located in the bronchial and vascular musculature; to retain selectivity it is therefore important to use the lowest effective dose.
Pharmacokinetics and Metabolism
The absolute bioavailability after a 10 mg oral dose of Bisoprolol fumarate is about 80%. Absorption is not affected by the presence of food. The first pass metabolism of Bisoprolol fumarate is about 20%.
Binding to serum proteins is approximately 30%. Peak plasma concentrations occur within 2 to 4 hours of dosing with 5 to 20 mg, and mean peak values range from 16 ng/mL at 5 mg to 70 ng/mL at 20 mg. Once daily dosing with Bisoprolol fumarate results in less than twofold intersubject variation in peak plasma levels. The plasma elimination half-life is 9 to 12 hours and is slightly longer in elderly patients, in part because of decreased renal function in that population. Steady state is attained within 5 days of once daily dosing. In both young and elderly populations, plasma accumulation is low; the accumulation factor ranges from 1.1 to 1.3, and is what would be expected from the first order kinetics and once daily dosing. Plasma concentrations are proportional to the administered dose in the range of 5 to 20 mg. Pharmacokinetic characteristics of the two enantiomers are similar.
Bisoprolol fumarate is eliminated equally by renal and non-renal pathways with about 50% of the dose appearing unchanged in the urine and the remainder appearing in the form of inactive metabolites. In humans, the known metabolites are labile or have no known pharmacologic activity. Less than 2% of the dose is excreted in the feces. Bisoprolol fumarate is not metabolized by cytochrome P450 II D6 (debrisoquin hydroxylase).
In subjects with creatinine clearance less than 40 mL/min, the plasma half-life is increased approximately threefold compared to healthy subjects. In patients with cirrhosis of the liver, the elimination of Bisoprolol fumarate is more variable in rate and significantly slower than that in healthy subjects, with plasma half-life ranging from 8.3 to 21.7 hours.
How should I give it?
Furosemide and bumetanide come in liquid and tablet form. It is usually given 1 to 3 times a day. Your child should be awake and alert when taking any medicine. Follow the checked instructions below:β-agonist Powder
___ If using the liquid form, draw up the correct amount of medicine in the medicine dropper or a syringe. Give a small squirt of the medicine inside the cheek. To avoid choking, let your child swallow each squirt before giving more.
___ For babies, you may want to mix the medicine with a small amount of formula or breast milk and give it with a bottle nipple before a feeding. Do not add medicine to a whole bottle because if your baby does not finish it, you will not know how much of the medicine was taken.
___ For children who cannot swallow pills:
Crush it between 2 spoons, inside a plastic bag, or in folded paper.
Mix the powder with a very small amount (about 1 teaspoon) of soft food, such as applesauce, chocolate syrup, ice cream, jelly, or yogurt.Furosemide and bumetanide can be given with or without food or milk. These medicines can decrease the potassium level in the blood, so your child may need to have potassium blood tests.
Cas No.: 72956-09-3
Molecular Formula: C24H26N2O4
Molecular Weight: 406.48
Melting point: 113-117ºC
Density:1.25 g/cm3
Boiling Point: 655.2 °C at 760 mmHg
Flash Point: 350.1 °C
Appearance: white or almost white crystalline powder
Assay:98%min
Usage: Carvedilol powder is a non-selective beta blocker/alpha-1 blocker indicated in the treatment of mild to moderate congestive heart failure (CHF).
Carvedilol is a AR (α1 and β-adrenergic receptor) antagonist with antioxidant properties. Studies show that the receptors α1D-AR and α1B-AR have a greater affinity for Carvedilol in comparison to the receptor β1-AR subtype. Carvedilol has been observed to block the oscillatory intracellular calcium changes induced by α1D-AR and α1B-AR, and shown to have a higher oxidative effect than Atenolol (sc-204895). The S(-) enantiomer of Carvedilol acts as a β-blocker, and the R(+) and S (-) enantionmers both block the α1. Carvedilol is an inhibitor of α1B-AR, β1-AR, β2-AR and α1D-AR.
Celiprolol powder General Description Celiprolol powder is a medication in the class of beta blockers, used in the treatment of high blood pressure. It has a unique pharmacology: it is a selective β1 receptor antagonist, but a β2 receptor partial agonist. It is also a weak α2 receptor antagonist. Celiprolol powder is believed to provide clinical benefit for people with vascular Ehlers–Danlos syndrome by promoting normal collagen synthesis in the blood vessels, and by shifting the pressure load away from the vessels most prone to dissection and rupture. In 2019, a new drug application (NDA) for celiprolol was denied by the Food an the U.S. Food and Drug Administration (FDA), instead calling for an “adequate and well-controlled” trial to determine whether celiprolol reduced the risk of clinical events in patients with vEDS. Celiprolol is a vasoactive beta-1 selective adrenoceptor antagonist with partial beta-2 agonist activity. The beta-2 agonist activity is thought to account for its mild vasodilating properties. It lowers blood pressure in hypertensive patients at rest and on exercise. The effects on heart rate and cardiac output are dependent on the pre-existing background level of sympathetic tone. Under conditions of stress such as exercise, celiprolol attenuates chronotropic and inotropic responses to sympathetic stimulation. However, at rest minimal impairment of cardiac function is seen. Before you start the treatment, read the manufacturer’s printed information leaflet from inside the pack. It will give you more information about celiprolol and will provide you with a full list of the side-effects which you may experience from taking it. Take celiprolol exactly as your doctor tells you to. There are two strengths of tablet – 200 mg and 400 mg. It is usual to start by taking one 200 mg tablet daily, although your doctor may later increase this to the 400 mg strength tablet. You should take the tablet first thing in the morning, preferably ‘on an empty stomach’. This means that you should take the tablet at least 30 minutes before you have breakfast, or wait until two hours after you have eaten. Swallow the Celiprolol: A Unique Selective Adrenoceptor Modulator. Celiprolol is a β-blocker with a unique pharmacologic profile: it is a β1-andrenoceptor antagonist with partial β2 agonist activity. Given this combination of effects, celiprolol may be better described as a selective adrenoreceptor modulator. It has antihypertensive and antianginal properties and is indicated for those uses in various countries around the world. In the United States, however, the proposed indication for this drug will be for the treatment of vascular type Ehlers-Danlos syndrome, a rare connective tissue disorder characterized by fragile arterial structure and an increased risk of life-threatening vascular complications. By reducing heart rate and pulsatile pressure, celiprolol may reduce the mechanical stress on collagen fibers within the arterial wall and be of benefit in patients with vascular type Ehlers-Danlos syndrome. The largest investigation of celiprolol in vascular Ehlers-Danlos syndrome was prematurely terminated due to significant benefit with celiprolol in reducing arterial events in patients with this condition. Celiprolol, therefore, represents a β-blocker that is unique from others in its class in both its pharmacology and clinical applications.
The Most Powerful Health Care Product Antiaging Tomato Extract Lycopene Powder Tomatoes are rich in vitamins A and C and fibre , and are cholesterol free. An average size tomato (148 gram, or 5 oz) boasts only 35 calories. Furthermore, new medical research suggests that the consumption of lycopene - the stuff that makes tomatoes red - may prevent cancer. Lycopene is part of the family of pigments called carotenoids, which are natural compounds that create the colours of fruits and vegetables. For example, beta carotene is the orange pigment in carrots.As with essential amino acids, they are not produced by the human body. Lycopene is the most powerful antioxidant in the carotenoid family and, with vitamins C and E, protect us from the free radicals that degrade many parts of the body.Antiaging Powder Lycopene is a bright red carotene and carotenoid pigment and phytochemical found in tomatoes and other red fruits & vegetables, such as,GAC, red carrots, watermelons and papayas (but not strawberries or cherries). Although lycopene is chemically a carotene, it has no vitamin A activity. In plants, algae, and other photosynthetic organisms, lycopene is an important intermediate in the biosynthesis of many carotenoids, including beta carotene, responsible for yellow, orange or red pigmentation, photosynthesis, and photo-protection. Structurally, it is a tetraterpene assembled from eight isoprene units, composed entirely of carbon and hydrogen, and is insoluble in water. Lycopene is not an essential nutrient for humans, but is commonly found in the diet, mainly from dishes prepared with tomato sauce. When absorbed from the stomach, lycopene is transported in the blood by various lipoproteins and accumulates in the liver, adrenal glands, and testes. The related carotenoid antioxidant, beta-carotene, has been shown to increase the number of prostate cancer cases in a subset of patients, although this area of research remains controversial and ongoing. 1) Prevention and suppression of cancer; 2) Protection of the cardiovascular; 3) Anti-ultraviolet radiation; 4) Suppression mutagenesis; 5) Anti-aging and enhancing immunity; 6) Improving skin allergies; 7) Improving a variety of body tissues 8)With a strong hangover effect; 9) With the prevention of osteoporosis, lower blood pressure,reducing the exercise induced asthma, and other physiological functions; 10) Without any side effects, ideal for taking long-term care; 11) Preventing and improving prostatic hyperplasia; prostatitis and other urological diseases; 12) Helping to improve sperm quality, reduce the risk of infertility.
Nootropic Powder J147 Pharmaceutical Intermediate J147 powder was discovered based upon efficacy in multiple cell culture models of age-associated pathologies rather than exclusively amyloid metabolism. It is an exceptionally potent, orally active and broadly neuroprotective compound has the ability to enhance memory in normal animals as well as to prevent memory deficits in Alzheimer's disease (AD) transgenic mice. The neurotrophic and memory-enhancing activities of J147 are associated with an increase in brain derived neurotrophic factor (BDNF) levels and the expression of BDNF responsive proteins, the enhancement of LTP, the preservation of synaptic protein, the reduction of amyloid plaques, etc. These pleiotrophic effects of a single molecule suggest that J147 has potential for the treatment of AD. J 147 is a novel neurotrophic drug for cognitive enhancement and Alzheimer's disease. J 147 is an exceptionally potent, orally active and broadly neuroprotective compound has the ability to enhance memory in normal animals as well as to prevent memory deficits in Alzheimer's disease (AD) transgenic mice. The neurotrophic and memory-enhancing activities of J147 are associated with an increase in brain derived neurotrophic factor (BDNF) levels and the expression of BDNF responsive proteins, the enhancement of LTP, the preservation of synaptic protein, the reduction of amyloid plaques. Function: Enhance mental intelligence; Boost memory and leaning capabilities;Improve brain power to solve problems and protect it from any chemical or physical injury;Enhance motivation level;Enhance the control of cortical/subcortical brain mechanism;Improve sensory perception.
Pharmaceutical Grade Alpha Lipoic Acid Lipoic Acid CAS No.: 1077-28-7 EINECS No.: 200-534-6 Type: Vitamins, Antioxidant, Nutrition Enhancers Appearance: Slightly yellow crystal powder Application: 1.Alpha lipoic acid is a vitamin drugs, limited physical activity in its dextral, basically no physical activity in its Lipoic acid , and no side effects. 2.Alpha lipoic acid always used for acute and chronic hepatitis, liver cirrhosis, hepatic coma, fatty liver, diabetes, Alzheimer's disease ,and applies as an antioxidant health products. Packaging & Delivery Packaging Details: 25kg/carton Delivery Time: within 7 days after payment Product Description Alpha lipoic acid is a vitamin drugs, limited physical activity in its dextral, basically no physical activity in its Lipoic acid, and no side effects. It is always used for acute and chronic hepatitis, liver cirrhosis, hepatic coma, fatty liver, diabetes, Alzheimer's disease ,and applies as an antioxidant health products.Alpha-lipoic Acid powder 1.Alpha lipoic acid is a fatty acid found naturally inside every cell in the body. 2.Alpha lipoic acid is needed by the body to produce the energy for our body's normal functions. 3.Alpha lipoic acid converts glucose(blood sugar) into energy. 4.Alpha lipoic acid is also an antioxidant, a substance that neutralizes potentially harmful chemicals called free radicals. What makes alpha lipoic acid unique is that it functions in water and fat. 5. Alpha lipoic acid appears to be able to recycle antioxidants such as vitamin C and glutathione after they have been used up. Alpha lipoic acid increases the formation of glutathione.