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'''Foscarnet''' is the [[conjugate base]] of the [[chemical compound]] with the [[chemical formula|formula]] HO<sub>2</sub>CPO<sub>3</sub>H<sub>2</sub>. This [[phosphonic acid]] derivative is (marketed by [[AstraZeneca]] as foscarnet [[sodium]] under the trade name Foscavir®) is an [[antiviral]] [[medication]] used to treat [[herpes viruses]], including [[cytomegalovirus]] (CMV) and [[herpes simplex]] viruses types 1 and 2 (HSV-1 and HSV-2). It is particularly used to treat [[CMV retinitis]]. |
'''Foscarnet''' is the [[conjugate base]] of the [[chemical compound]] with the [[chemical formula|formula]] HO<sub>2</sub>CPO<sub>3</sub>H<sub>2</sub>. This [[phosphonic acid]] derivative is (marketed by [[AstraZeneca]] as foscarnet [[sodium]] under the trade name Foscavir®) is an [[antiviral]] [[medication]] used to treat [[herpes viruses]], including [[cytomegalovirus]] (CMV) and [[herpes simplex]] viruses types 1 and 2 (HSV-1 and HSV-2). It is particularly used to treat [[CMV retinitis]]. Foscarnet can be used to treat highly treatment experienced patients with [[HIV]] as part of [[salvage therapy]].<ref>{{cite journal |author=Canestri A, Ghosn J, Wirden M, ''et al'' |title=Foscarnet salvage therapy for patients with late-stage HIV disease and multiple drug resistance |journal=Antivir. Ther. (Lond.) |volume=11 |issue=5 |pages=561–6 |year=2006 |pmid=16964823 |doi=}}</ref><ref>{{cite journal |author=Mathiesen S, Dam E, Roge B, ''et al'' |title=Long-term foscarnet therapy remodels thymidine analogue mutations and alters resistance to zidovudine and lamivudine in HIV-1 |journal=Antivir. Ther. (Lond.) |volume=12 |issue=3 |pages=335–43 |year=2007 |pmid=17591023 |doi=}}</ref><ref>{{cite journal |author=Meyer PR, Rutvisuttinunt W, Matsuura SE, So AG, Scott WA |title=Stable complexes formed by HIV-1 reverse transcriptase at distinct positions on the primer-template controlled by binding deoxynucleoside triphosphates or foscarnet |journal=J. Mol. Biol. |volume=369 |issue=1 |pages=41–54 |year=2007 |pmid=17400246 |doi=10.1016/j.jmb.2007.03.006 |url=http://linkinghub.elsevier.com/retrieve/pii/S0022-2836(07)00335-X}}</ref> |
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==Mechanism of action== |
==Mechanism of action== |
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[[Category:Antivirals]] |
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[[Category:Antiretroviral drugs]] |
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Revision as of 00:49, 18 December 2007
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| Clinical data | |
|---|---|
| Pregnancy category | |
| Routes of administration | Intravenous |
| ATC code | |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Bioavailability | NA |
| Protein binding | 14-17% |
| Elimination half-life | 3.3-6.8 hours |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| DrugBank | |
| CompTox Dashboard (EPA) | |
| Chemical and physical data | |
| Formula | CH3O5P |
| Molar mass | 126.005 g/mol 300.1 g/mol (foscarnet trisodium hexahydrate) g·mol−1 |
Foscarnet is the conjugate base of the chemical compound with the formula HO2CPO3H2. This phosphonic acid derivative is (marketed by AstraZeneca as foscarnet sodium under the trade name Foscavir®) is an antiviral medication used to treat herpes viruses, including cytomegalovirus (CMV) and herpes simplex viruses types 1 and 2 (HSV-1 and HSV-2). It is particularly used to treat CMV retinitis. Foscarnet can be used to treat highly treatment experienced patients with HIV as part of salvage therapy.[1][2][3]
Mechanism of action
Foscarnet is a structural mimic of the anion pyrophosphate that selectively inhibits the pyrophosphate binding site on viral DNA polymerases at concentrations that do not affect human DNA polymerases. Because foscarnet is not activated by thymidine kinase, it maintains activity in some viruses which have lost thymidine kinase activity to gain resistance to aciclovir or ganciclovir. Therefore, foscarnet is often used in aciclovir- or ganciclovir-resistant disease.
However, acyclovir or ganciclovir resistant mutants with alterations in viral DNA polymerase may be resistant to foscarnet.[4]
Administration
Intravenous only
Side effects
- Nephrotoxicity - Increase in serum creatinine levels occurs on average in 45% of patients receiving foscarnet. Other nephrotoxic drugs should be avoided. Nephrotoxicity is usually reversible and can be reduced by dosage adjustment and adequate hydration.
- Electrolyte disturbances - Changes in calcium, magnesium, potassium and phosphate levels occurs commonly and regular monitoring of electrolytes is necessary to avoid clinical toxicity.
- Genital ulceration - Occurs more commonly in men and usually occurs during induction use of foscarnet. It is most likely a contact dermatitis due to high concentrations of foscarnet in urine. It usually resolves rapidly following discontinuation of the drug.
References
- ^ Canestri A, Ghosn J, Wirden M; et al. (2006). "Foscarnet salvage therapy for patients with late-stage HIV disease and multiple drug resistance". Antivir. Ther. (Lond.). 11 (5): 561–6. PMID 16964823.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: multiple names: authors list (link) - ^ Mathiesen S, Dam E, Roge B; et al. (2007). "Long-term foscarnet therapy remodels thymidine analogue mutations and alters resistance to zidovudine and lamivudine in HIV-1". Antivir. Ther. (Lond.). 12 (3): 335–43. PMID 17591023.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: multiple names: authors list (link) - ^ Meyer PR, Rutvisuttinunt W, Matsuura SE, So AG, Scott WA (2007). "Stable complexes formed by HIV-1 reverse transcriptase at distinct positions on the primer-template controlled by binding deoxynucleoside triphosphates or foscarnet". J. Mol. Biol. 369 (1): 41–54. doi:10.1016/j.jmb.2007.03.006. PMID 17400246.
{{cite journal}}: CS1 maint: multiple names: authors list (link) - ^ Bonnafous P, Naesens L, Petrella S; et al. (2007). "Different mutations in the HHV-6 DNA polymerase gene accounting for resistance to foscarnet". Antivir. Ther. (Lond.). 12 (6): 877–88. PMID 17926642.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: multiple names: authors list (link)