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31 Cards in this Set
- Front
- Back
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Gancyclovir
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Therapeutic use: Treatment of CMV retinitis in immunocompromised patients and prevention of CMV disease in transplant patients.
Toxicity: dose-dependent neutropenia, CNS effects (headache, behavioral changes, convulsions, coma), carcinogenic. Patients present with blurred vision, floaters, loss of central or peripheral vision. |
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T1/2 of acyclovir and ganciclovir
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Acyclovir- Plasma 1/2 life is about 2.5 hr.
Ganciclovir- Plasma 1/2 life is greater than 24 hrs. Ganciclovir triphosphate concentrations are 10X those of acyclovir. |
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Foscarnet
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Therapeutic use: IV treatment for CMV retinitis in HIV-infected patients who are resistant to ganciclovir. Herpes patients who are resistant to acyclovir.
Toxicity: Nephrotoxicity, anemia, nausea, fever, hypocalcemia and hypomagnesemia. |
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Trifluridine
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Blocks DNA synthesis. Therapeutic use: HSV keratoconjunctivitis and keratitis.
Replaced the drug Idoxuridine- still may be used Toxicity: Inflammation of the cornea |
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Fomivirsen
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Antisense oligonucleotide- not first line of treatment. Can be injected into eye
Therapeutic use: CMV retinitis in patients who do not respond to other drugs. Do not give to patients who have taken cidofovir in past month-may increase inflammation of the eye. Toxicity: Iritis, increased intraocular pressure and vision changes |
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Treatment of herpes
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Acyclovir, Trifluidine, fomivirsen
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Treatment for CMV
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Ganciclovir, foscarnet, fomivirsen
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Amantadine and Rimantadine
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No longer recommended for URI, most viruses are resistant
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Neuraminidase Inhibitors
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zanamivir, oseltamivir. Has to present within 48 hrs of exposure, or it won’t work. Shortens the duration and may be used to prevent flu.
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Zanamivir and tamiflu toxicity
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Zanamivir- Toxicity: Nasal and throat discomfort and headaches. Bronchospasm in asthma patients.
Tamiflu- Toxicity: Nausea, vomiting and headaches. When taken with food there is less nausea. It may be used for both influenza A and B. Both for H1N1 |
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Interferons
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Interferons alpha and beta are made in response to viral infection.
MOA: IFNs bind to cellular receptors and activate the JAK-STAT signal transduction pathway. IFNs induce many proteins, including 2'-5'-oligoadenylate synthetase and a kinase, that inhibit protein synthesis. |
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Interferon use
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Therapeutic use: genital warts, chronic hepatitis B and C, Kaposi's sarcoma in HIV-infected patients, multiple melanomas and multiple sclerosis. Peg-interferon 2A with Ribavirin is the treatment of choice is for chronic hepatitis C.
Toxicity: IM or SC injection may produce flu-like symptoms. High dose or chronic therapy may be limited due to bone marrow suppression, fatigue, increased susceptibility to bacterial infections, anorexia, diarrhea and psychiatric syndrome (depression and anxiety). |
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What drug is used in combination with interferon in MS?
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Ribovarin
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Ribovarin
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MOA: Inhibits viral mRNA synthesis
Therapeutic use: Ribavirin with interferon is the standard treatment for hepatitis C. Given to treat infants and young children with Respiratory Syncytial Virus infections that cause bronchiolitis and pneumonia. Influenza A and B, Parainfluenza, Paramyxovirus, Arenaviruses and HIV. RIBAvirin-Rsv, Influenza B, Arenaviruses Toxicity: Aerosol is well tolerated, but systemic doses may cause anemia. Teratogenic therefore do not give to pregnant women. |
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Nucleoside Reverse Transcriptase Inhibitors
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"Ziddy went nuclear and did stab a baby lamb.”
ZIDovudine [NUCLeoside RT inhib.], DIDanosine, STAvudine, A-BAcavir, LAMivudine |
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Zidovudine (AZT)
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Therapeutic use: HIV patients, protects fetuses from becoming infected in HIV-infected pregnant women.
Resistance: Mutated reverse transcriptase that has a lower affinity for the AZT-TP Toxicity: Bone marrow (anemia and leukopenia) and headaches. Probenecid, Acetaminophen Lorazepam (benzodiazepine), Indomethacin (anti-inflammatory), and Cimetidine (H2-receptor antagonist) increase toxicity of AZT. I am a PAL I Care. NEW: Trizivir: Zidovudine, Lamivudine and Abacavir. |
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Didanosine (ddI)
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Therapeutic use: Patients with AZT-resistant HIV infections
Toxicity: Pancreatitis that may be fatal, gastrointestinal disturbances and a dose-limiting peripheral neuropathy. Toxicity increases when combined with Stavudine. In 2010 the FDA changed the warning label on the drug to include non-cirrhotic portal hypertension which is potentially fatal. |
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Zalcitabine (ddC)
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Therapeutic use: Given in conjunction with AZT or alone for those who cannot tolerate AZT- treatment
Toxicity: Peripheral neuropathy, rash and stomatitis on initial treatments |
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Stavudine
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Toxicity: Peripheral neuropathy
Both AZT and Stavudine Treatment: Potentially fatal lactic acidosis, peripheral lipoatrophy, central fat accumulation and hyperlipidemia. |
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Lamivudine (3TC) and Emtricitabine
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Therapeutic use: Patients with HIV in combination with AZT (resistance to AZT develops more slowly when used in combination)
and hepatitis B patients. Toxicity: Pancreatitis often develops in pediatric patients. NEW: Trizivir: Zidovudine, Lamivudine and Abacavir. Also as Lamivudine and Abacavir |
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Abacavir
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Therapeutic use: HIV infected adults and children in combination with AZT and Lamivudine or a protease inhibitor
Toxicity: Hypersensitivity resulting in fever, gastrointestinal distress, malaise and rash |
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Tenofovir
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MOA: Inhibits reverse transcriptase and terminates DNA chain elongation.
Therapeutic use: HIV infected patients and chronic hepatitis B infections. Toxicity: Well tolerated except for flatulence, some renal toxicity. Do not give as didanosine, lamivudin or abacavir combo. |
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Non-nucleoside Reverse Transcriptase Inhibitor
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Efavirenz
Nevirapine Delavirdine |
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Efavirenz
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MOA: alters the conformation of reverse transriptase.
Therapeutic use: Used in combination with AZT and Lamivudine Toxicity: Dizziness, headache, insomnia, rash Drug interactions: Efavirenz decreases concentration of Phenobarbital, Phenytoin, Carbamazepine, Methadone and Rifabutin. Co-administration of Rifampin will reduce levels of Efavirenz. |
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Nevirapine
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MOA: Alters the conformation of reverse transcriptase.
Therapeutic use: Used in combination with Didanosine or Stavudine. Toxicity: Rash, fever, nausea, severe dermatologic effects and fatal hepatotoxicity Drug interaction: Must warn patients not to take St. John's Wort which lowers the concentration of Nevirapine. Nevirapine induces CYP3A4 and therefore it may lower the concentration of drugs metabolized by this enzyme. Nevirapine lowers plasma concentrations of Ethinyl estradiol and therefore patients should be given alternate methods of birth control. |
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Delavirdine
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MOA: Binds and inhibits reverse transcriptase.
Therapeutic use: Used in combination with Zidovudine and Didanosine, least potent NNRTI Drug interactions: Delavirdine inhibits CYP3A4 and may thus alter the metabolism of Rifampin, Rifabutin, Ergot derivatives, Triazolam, Midazolam and Cisapride. Delavirdine also inhibits CYP2C9. Drugs that induce CYP3A4, such as Carbamazepine, Penobarbital, Phenytoin, Rifabutin and Rifampin, may decrease Delavirdine levels. |
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Protease Inhibitors
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Atazanavir, Indinavir, Ritonavir, Lopinavir, Nelfinavir, Amprenavir, Saquinavir- blocks HIV replication
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Atazanavir
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Therapeutic use: HIV patients must take the drugs continuously in combination with AZT and Lamivudine or other nucleoside reverse transcriptase inhibitors.
Toxicity: Well tolerated Sometime- nausea, vomiting, diarrhea, lipodystrophy and hyperglycemia Resistance: Cross-resistance often occurs among the protease inhibitors, but the HIV strains may still be susceptible to Amprenavir. |
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Lopinavir/Ritonavir
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Pharmacokinetics: Lopinavir is metabolized by CYP3A. Ritonavir is an inhibitor of CYP3A4 activity and, therefore, raises the Lopinavir plasma levels.
Therapeutic use: The combination of drugs is used to treat HIV strains that are resistant to multiple protease inhibitors. Toxicity: Well tolerated. Diarrhea, nausea, fatigue, headache, hyperlipidemia, hyperglycemia, and altered body fat. Drug interactions: Inhibit the activity of CYP3A4 and CYP2D6 and therefore may increase or prolong the therapeutic or adverse effects of drugs metabolized by these pathways. |
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Fusion Inhibitors- Enfuvirtide
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Therapeutic use: Injected twice daily in HIV patients. Used with other drugs.
Toxicity: Pain, redness, nodules and cysts formation at the site of injection. |
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Fusion Inhibitors- Maraviroc
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Therapeutic use: HIV patients.
MOA: The drug blocks the CCR5 chemokine receptor. HIV uses CCR5 as a co-receptor to bind and enter macrophages. Toxicity: most common are cough, fever, dizziness, headache, lowered blood pressure, nausea, and bladder irritation. May cause liver problems and cardiac events, an increased risk for some infections, and a slight increase in cholesterol levels |
