oritavancin, sold under the brand name orbactiv, is a novel semisynthetic glycopeptide antibiotic medication for the treatment of serious gram-positive bacterial infections. its chemical structure as a lipoglycopeptide is similar to vancomycin.

the u.s. food and drug administration (fda) and the european medicines agency (ema) have approved oritavancin for treatment of acute bacterial skin and skin structure infections.

in vitro activity
oritavancin shares certain properties with other members of the glycopeptide class of antibiotics, which includes vancomycin, the current standard of care for serious gram-positive infections in the united states and europe. it possesses potent and rapid bactericidal activity in vitro against a broad spectrum of both resistant and susceptible gram-positive bacteria, including staphylococcus aureus, mrsa, enterococci, and streptococci. oritavancin was more active than either metronidazole or vancomycin against strains of clostridium difficile tested.

oritavancin has potential use as a therapy for exposure to bacillus anthracis, the gram-positive bacterium that causes anthrax, having demonstrated efficacy in a mouse model both before and after exposure to the bacterium.

mechanism
the 4'-chlorobiphenylmethyl group disrupts the cell membrane of gram-positive bacteria. it also acts by inhibition of transglycosylation and inhibition of transpeptidation.

ciclosporin, also spelled cyclosporine and cyclosporin, is a calcineurin inhibitor, used as an immunosuppressant medication. it is a natural product. it is taken by mouth or by injection into a vein for rheumatoid arthritis, psoriasis, crohn's disease, nephrotic syndrome, and in organ transplants to prevent rejection. it is also used as eye drops for keratoconjunctivitis sicca (dry eyes).

common side effects include high blood pressure, headache, kidney problems, increased hair growth, and vomiting. other severe side effects include an increased risk of infection, liver problems, and an increased risk of lymphoma. blood levels of the medication should be checked to decrease the risk of side effects. use during pregnancy may result in preterm birth; however, ciclosporin does not appear to cause birth defects.

ciclosporin is believed to work by decreasing the function of lymphocytes. it does this by forming a complex with cyclophilin to block the phosphatase activity of calcineurin, which in turn decreases the production of inflammatory cytokines by t-lymphocytes.

ciclosporin was isolated in 1971 from the fungus tolypocladium inflatum and came into medical use in 1983. it is on the world health organization's list of essential medicines, the safest and most effective medicines needed in a health system. in 2017, it was the 248th most commonly prescribed medication in the united states, with more than one million prescriptions that year.

medical uses
ciclosporin is approved by the fda to treat and prevent graft-versus-host disease in bone marrow transplantation and to prevent rejection of kidney, heart, and liver transplants. it is also approved in the us for treating of rheumatoid arthritis and psoriasis, persistent nummular keratitis following adenoviral keratoconjunctivitis, and as eye drops for treating dry eyes caused by sj?gren's syndrome and meibomian gland dysfunction.

in addition to these indications, ciclosporin is also used in severe atopic dermatitis, kimura disease, pyoderma gangrenosum, chronic hives, acute systemic mastocytosis, and posterior or intermediate uveitis with noninfective cause.[citation needed] it is also used, albeit infrequently, in severe rheumatoid arthritis and related diseases.[citation needed]

ciclosporin has also been used in people with acute severe ulcerative colitis and hives that do not respond to treatment with steroids.

carmustine (bis-chloroethylnitrosourea, bcnu, bicnu) is a medication used mainly for chemotherapy. it is a nitrogen mustard ß-chloro-nitrosourea compound used as an alkylating agent.

description
carmustine is an orange-yellow solid medication used mainly for chemotherapy. it is a nitrogen mustard ß-chloro-nitrosourea compound.

mechanism of action
as an alkylating agent, carmustine can form interstrand crosslinks in dna, which prevents dna replication and dna transcription.[citation needed]

uses
carmustine is used as an alkylating agent to treat several types of brain cancer including glioma, glioblastoma multiforme, medulloblastoma and astrocytoma), multiple myeloma, and lymphoma (hodgkin's and non-hodgkin).

bcnu is sometimes used in conjunction with alkyl guanine transferase (agt) inhibitors, such as o6-benzylguanine. the agt-inhibitors increase the efficacy of carmustine by inhibiting the direct reversal pathway of dna repair, which will prevent formation of the interstrand crosslink between the n1 of guanine and the n3 of cytosine.

it is also used as part of a chemotherapeutic protocol in preparation for hematological stem cell transplantation, a type of bone marrow transplant, in order to reduce the white blood cell count in the recipient. use under this protocol, usually with fludarabine and melphalan, was developed by oncologists at the university of texas md anderson cancer center.[citation needed]

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