Monday 27 February 2012

the introduction of Oseltamivir

Oseltamivir


Oseltamivir INN is an antiviral drug.Oseltamivir INN slows the spread of influenza virus between cells in the body by stopping the virus from chemically cutting ties with its host cell. Oseltamivir has been used to treat and prevent influenza A virus and influenza B virus infection in over 50 million people since 1999.

Oseltamivir is a (relatively) inactive chemical which is converted into its active form by metabolic process after it is taken into the body. Oseltamivir was the first orally active neuraminidase inhibitor commercially developed.It is marketed by Chugai Pharmaceutical Co.

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Friday 24 February 2012

the description of Clofarabine

Clofarabine


Cytosine can be found as part of DNA, as part of RNA, or as a part of a nucleotide. As cytidine triphosphate (CTP), Cytosine can act as a co-factor to enzymes.In addition,Cytosine can transfer a phosphate to convert adenosine diphosphate (ADP) to adenosine triphosphate (ATP).

In DNA and RNA, Cytosine is paired with guanine. However, Cytosine is inherently unstable.Cytosine can change into uracil ,which can result in a point mutation if not repaired by the DNA repair enzymes such as uracil glycosylase, which cleaves a uracil in DNA.

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Wednesday 22 February 2012

the does of Ceftobiprole

Ceftobiprole


Ceftobiprole cannot be given by mouth. Consequentlyceftobiprole is given intravenously. Ceftobiprole is not FDA approved for use in children.Ceftobiprole has been permited for use in Canada and Switzerland, and ceftobiprole is under review by regulatory authorities in the United States, the European Union, Australia, Russia and South Africa.

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Monday 20 February 2012

Recommended Dosing of Nilotinib in Europe

Nilotinib

In Europe ,the dose of nilotinib is recommended 400 mg twice a day.  As long as the patient continues to benefit,treatment should be continued. Nilotinib should be taken twice daily approximately 12 hours apart. What's more,nilotinib is not allowed to be taken with food. The capsules should be swallowed whole with water. No food should be consumed for 2 hours before the dose is taken and no food should be consumed for at least one hour after the dose is taken. Nilotinib may be given in combination with haematopoietic growth factors such as erythropoietin or granulocyte colony-stimulating factor (G-CSF) if clinically indicated. Nilotinib may be given with hydroxyurea or anagrelide if clinically indicated.
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Wednesday 15 February 2012

A new standard of care: Voriconazole

Voriconazole
Voriconazole is a crystalline solid, the melting point is 130 ° C.It from 127, and can be used to ergosterol biosynthesis inhibitors as well as antifungal agents.
Voriconazole, has become a new standard of care in the treatment of invasive aspergillosis can occur in immunocompromised patients, including allogeneic BMT, other blood cancers, solid organ transplantation. This is voriconazole .The important thing is based on the results of large randomized trial has proved superior to amphotericin B compared with 32% of amphotericin B, with a partial response or complete 53% , is 71% of patients with voriconazole over amphotericin B provides a survival benefit of 22 percent or more, still alive at 12 weeks in the voriconazole. The longer the duration of treatment significantly fewer severe side effects and the first 13 percent of patients who received initial treatment with voriconazole, amphotericin B, voriconazole also, tolerability was excellent better than amphotericin B compared with 29% of patients who received, was killed in invasive aspergillosis. Design of these studies is called into question, and some consider the (liposomal) amphotericin B as first-line drug yet. Combination therapy with voriconazole and caspofungin against central nervous system aspergillosis site or multiple note is inadequate response or intolerance for must be less considered.With, and other that are Patients with early switch to voriconazole than amphotericin B or lipid formulation that the limited effect of salvage therapy and antifungal agents license, the importance of effective initial treatment has been demonstrated.

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Monday 13 February 2012

The konwledge of Cytosine

Cytosine
Cytosine (C) is one of the four main bases found in DNA and RNA, along with adenine, guanine, and thymine (uracil in RNA). It is a pyrimidine derivative, with a heterocyclic aromatic ring and two substituents attached (an amine group at position 4 and a keto group at position 2). The nucleoside of cytosine is cytidine. In Watson-Crick base pairing, it forms three hydrogen bonds with guanine.
cytosine (sī'tōsēn'), organic base of the pyrimidine family. It was isolated from the nucleic acid of calf thymus tissue in 1894. A suggested structure for cytosine, published in 1903, was confirmed in the same year when that base was synthesized in the laboratory. Combined with the sugar ribose in glycosidic linkage, cytosine forms a derivative called cytidine (a nucleoside), which in turn can be phosphorylated with from one to three phosphoric acid groups, yielding the three nucleotides CMP (cytidine monophosphate), CDP (cytidine diphosphate), and CTP (cytidine triphosphate). Analogous nucleosides and nucleotides are formed from cytosine and deoxyribose. The nucleoside derivatives of cytosine perform important functions in cellular metabolism. CTP acts as a coenzyme in both carbohydrate and lipid metabolism; it can readily donate one of its phosphate groups to adenosine diphosphate (ADP) to form adenosine triphosphate (ATP), an extremely important intermediate in the transfer of chemical energy in living systems. CTP is the source of the cytidine found in ribonucleic acid (RNA) and deoxycytidine triphosphate (dCTP) is the source of the deoxycytidine in deoxyribonucleic acid (DNA). Thus cytosine is intimately involved in the preservation and transfer of genetic information.
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The Chemical reaction on Tri-o-tolylphosphine

Tri-o-tolylphosphine
To a solution of magnesuim turnings (3.11 g, 128 mmol, 3.5 equiv) in THF (50 ml), a small amount of 2-bromotoluene (1 ml) and a iodine crystal was added. The reaction vessel was heated until initiation occurred when a solution of the remaining 2-bromotoluene (20 g, 117 mmol, 3.2 equiv total) in THF (100 mL) was added. The reaction was was refluxed for 2 hours (color change to black solution), after which it to 0 ° C and a solution of phosphorus trichloride (5.01 g, 36.5 mmol, 1 equiv) in THF (30 ml) was cooled adjusted dropwise. Upon addition completion of the reaction was adjusted under reflux for 18 hours. The reaction was were allowed to cool to room temperature, whereupon NH4Cl solution was added cautiously. The resulting solution was washed with ether (3 × 100 ml), dried over MgSO 4, filtered and concentrated in vacuo. The resulting white solid was recrystalised from ethanol to give Tri-o-tolylphosphine was obtained as a white solid. (6.8 g, 62%)

Although Tri-o-tolylphosphine is commercially available, it is relatively expensive because it is so easy to prepare. The Grignard reaction is a bit temperamental and may need a little encouragement to initiate. A word of warning, do not add all the bromotoluene in one portion, as this will flood the magnesium and the reaction will never work. Furthermore, if you find that the iodine is not sufficient to initiate the reaction, we have found that a micro spatula of mercury chloride and other Grignard reactions help for this. This reaction was carried out at different scales and has shown that about 60% of the desired product in all cases.
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