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Influenza drugs zanamivir

The Discovery of Zanamivir, the First Potent Designer Anti-Influenza Drug.. 119... [Pg.111]

Much more interesting, in terms of applications, is the case in which the anomeric oxygen is replaced by a double bound. This is the case of Zanamivir (Fig. 3)2 an anti-influenza drug approved by the US Food... [Pg.259]

Fig. 1.4 Hemagglutination assay results from the active fraction of the red alga Gigartina skottsbergii. a Red blood cells (RBCs) hemagglutinate in the presence of influenza virus top row) and with extract A4 -t- virus or extract A4 alone. The bottom two rows present the back titration of the virus used in this experiment, b In contrast to the other anti-influenza drugs (ribavirin, amantadine, rimantadine, and zanamivir) that do not induce hemagglutination of human as well as chicken RBCs, extract A4 does it in a dose-dependent manner... Fig. 1.4 Hemagglutination assay results from the active fraction of the red alga Gigartina skottsbergii. a Red blood cells (RBCs) hemagglutinate in the presence of influenza virus top row) and with extract A4 -t- virus or extract A4 alone. The bottom two rows present the back titration of the virus used in this experiment, b In contrast to the other anti-influenza drugs (ribavirin, amantadine, rimantadine, and zanamivir) that do not induce hemagglutination of human as well as chicken RBCs, extract A4 does it in a dose-dependent manner...
Zanamivir (Relenza, 3.22) is used to fight the viruses that cause influenza A and influenza B (Figure 3.13). Because its oral bioavailability is low at only 2%, an alternative delivery route, inhalation, is required for zanamivir. As a possible demonstration of the public s general preference for oral drugs, oseltamivir (Tamiflu, 3.23), an oral influenza drug, far outsells the inhaled drug zanamivir. [Pg.46]

Compound 28, named zanamivir, was selected for clinical studies for the prophylaxis and treatment of influenza virus. Zanamivir was found to be suitable as a drug because it is highly selective for influenza type A and B viruses, which it inhibits with high potency... [Pg.832]

Figure 20.2 Structure of neuraminidase inhibitors used against type A and B influenza in humans, namely, the drug zanamivir (3) and the prodrug oseltamivir (4) whose active agent is Ro-64-0802 (5) [25, 26],... Figure 20.2 Structure of neuraminidase inhibitors used against type A and B influenza in humans, namely, the drug zanamivir (3) and the prodrug oseltamivir (4) whose active agent is Ro-64-0802 (5) [25, 26],...
Influenza A viruses cause severe infections in the respiratory system and are responsible for seasonal epidemics and sporadic pandemics. The primary method for prevention is through vaccination but vaccine production by current methods cannot be carried out in time to stop the progress of a new strain of the influenza virus. Therefore, effective antiviral agents are used for prophylactic and therapeutic treatments. Among several viral molecular targets for anti-influenza drugs, the surface glycoprotein neuraminidase appears particularly attractive. Selective inhibitors of this enzyme have been developed and two of which, oseltamivir phosphate 18 (Tamiflu ) " and zanamivir 19 (Relenza ), have been approved for human use (Scheme 6). [Pg.146]

Neuraminidase inhibitors are the major class of drugs to treat or to prevent the infection with influenza viruses. Currently, two neuraminidase inhibitors are available, zanamivir and oseltamivir, which block the release of new influenza vims from infected host cells and thereby stop the spread of infection. The enzyme neuraminidase is a surface glycoprotein present on all influenza viruses. There are nine influenza neuraminidase sub-types known of which subtypes N1 and N2 appear to be the most important ones. Neuraminidase inhibitors are effective against all neuraminidase subtypes. The activity of the neuraminidase is required for the newly... [Pg.821]

The discovery of the potent in vitro sialidase inhibitory activity and in vivo efficacy of zanamivir 12, and the increasing availability of 3D structural data for influenza virus sialidases in the 1990s, particularly with Neu5Ac and various inhibitors bound into the active site, provided a platform for further drug discovery efforts targeting... [Pg.123]

A pro-drug approach for improving the pharmacokinetics of zanamivir has recently shown some promise. The alkoxyalkyl ester 23 of zanamivir, with long alkyl chains chosen to counteract the high hydrophUicity of the molecule, was reported to show significant protective effects against influenza (HlNl) infection in mice upon oral or intraperitoneal administration (Liu et al. 2007). [Pg.127]

In the clinical setting, zanamivir 12 and oseltamivir 19 are effective in both the prevention and treatment of influenza A and B infection. Benefit in treatment is restricted to patients treated within 48 h of symptom onset (Fleming 2003). Importantly, the effects of drug treatment are a rednction in the severity of illness, and in the incidence of secondary complications. The term of illness is generally rednced between 1 and 2.5 days. The evalnation of zanamivir (Calfee and Hayden 1998 Oxford 2000 Fleming 2003), oseltamivir (Doncette and Aoki 2001 Oxford 2005) and peramivir (Sidwell and Smee 2002) for the treatment, and prophylaxis, of inflnenza virus infection has been reviewed. The reader is directed to these reviews for further details of drug pharmacodynamics and clinical trial data. [Pg.138]

The two classes of antiviral drugs available for treatment of influenza are the same as those available for prophylaxis and include the adamantanes, amantadine and rimantadine, and the neuraminidase inhibitors, oseltamivir and zanamivir. Because of widespread resistance to the adamantanes among influenza A viruses in the United States, amantadine and rimantadine are not recommended for treatment of influenza until susceptibility can be reestablished. [Pg.468]

Currently, two classes of drugs are available with antiviral activity against influenza viruses inhibitors of the ion channel activity of the M2 membrane protein, amantadine and rimantadine, and the neuraminidase inhibitors oseltamivir, and zanamivir. H5N1 viruses isolated from poultry and humans in Thailand and Viet Nam in 2004 invariably showed an amantadine-resistance indicating that amantadine treatment is not an option during the ongoing outb-treak in South-East Asia. [Pg.544]

Zanamivir is contraindicated in individuals with severe or decompensated chronic obstructive lung disease or asthma because it has not been shown to be effective in these individuals and can cause serious adverse pulmonary reactions. Individuals with mild to moderate asthma may have a decline in lung function when taking zanamivir. The safety and efficacy of this medication have not been determined in individuals with severe renal insufficiency. No clinically significant drug interactions have been reported. Zanamivir does not decrease the effectiveness of the influenza vaccine. [Pg.577]


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See also in sourсe #XX -- [ Pg.10 , Pg.100 , Pg.101 , Pg.117 , Pg.139 , Pg.144 ]




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Anti-influenza Drugs zanamivir

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