Maraviroc

Enfuvirtide (T-20)

HIV

Hepatotoxicity, myocardial infarction/ischemia, immune reconstitution syndrome, risk of infection, rash,m dizziness, upper respiratory infection, fever

Hypersensitivity

-Blocks infection of HIV strains that use CCR5 for attachment and entry, but it is not active against HIV strains that use the CXCR4 receptor

-Used in combination with other anti-HIV drugs in patients who have continued detectable viral loads or who have multidrug-resistant virus

HIV

Guillain-Barre syndrome, renal insufficiency, thrombocytopenia, neutropenia, eosinophillia, peripheral neuropathy, 6th nerve palsy, conjunctivitis 

Hypersensitivity

-Peptide that must be administered parenterally, with twice-daily injections

-Used in combination with other anti-HIV drugs in patients whose HIV has not been controlled on other anti-HIV medications

Amantadine

Rimantadine

Influenza A, Parkinsonism (amantadine)

Neuroleptic malignant syndrome, exacerbation of mental disorder, orthostatic hypotension, peripheral edema, GI disturbance, confusion, dizziness, insomnia, irritability, hallucination

Hypersensitivity

-Rimatadine causes fewer neurological effects than amantadine

-The use of these drugs has been largely supplanted by neuraminidase inhibitors

Acyclovir

Valacyclovir

Penciclovir

Famciclovir

Ganciclovir

Valganciclovir

Cidofovir

Vidarabine

Idoxuridine

Trifluridine

Herpes simplex virus (HSV), Varicella-zoster virus (VZV)

Renal failure (intravenous administration), thrombotic thrombocytopenic purpura in immunocompromised patients, encephalopatic changes, hemolytic uremic syndrome, GI disturbance, agitation, dizziness

Hypersensitivity

-Valacyclovir is prodrug of acyclovir with greater oral bioavaliability

Herpes simplex virus (HSV), Varicella-zoster virus (VZV)

Erythema multiforme, GI disturbance, headache

Hypersensitivity

-Famciclovir is a diacetyl 6-deoxy prodrug analogue of penciclovir, the active form of the drug

Cytomegalovirus (CMV)

Neutropenia, thrombocytopenia, anemia, fever, phlebitis

Severe neutropenia, severe thrombocytopenia

-Valganciclovir is a prodrug of ganciclovir with greater oral bioavailability

Cytomegalovirus (CMV) retinitis

Nephrotoxicity, neutropenia, metabolic acidosis, decreased intraocular pressure, GI disturbance, headache, rash

Renal insufficiency, concomitant nephrotoxic agents

-Must be co-administered with probenecid

-Long half-life, requiring only once weekly dosing

Herpes simplex virus (HSV) keratitis, Rarely vidarabine for severe HSV or Varicella-zoster virus (VZV)

Eye irritation lacrimation, light intolerance

Hypersensitivity

-Early anti-HSV drugs with increased toxicity relative to other agents

-Trifluridine used as ophthalmic preparation

Zidovudine (AZT)

Stavudine (d4t)

Zalcitabine (ddC)

Lamivudine (3TC)

Emtricitabine (FTC)

Didanosine (ddl)

Abacavir

Tenofovir

Adefovir

Entecavir

HIV, Hepatitis B virus (HBV) (lamiudine)

Neutropenia, anemia, pancreatitis, lactic acidosis, hepatomegaly with steatosis, optic neuritis, peripheral neuropathy, fatal hypersensitivity (abacavir)

Hypersensitivity

-Most toxicity is due to inhibition of mitochondrial DNA polymerase by drug triphosphates

-Lamivudine is less toxic, possibly due to L-stereoisomer structure

-Emtricitabine is administered once daily

HIV (tenofovir), Hepatitis B virus (HBV) (Adefovir, Entecavir)

Lactic acidosis, hepatotoxicity (tennofovir), renal toxicity (adefovir)

Hypersensitivity

-Entecavir dose should be adjusted for patients with moderate renal insufficiency

Herpes simplex virus (HSV), Cytomegalovirus (CMV)

Renal impairment, electrolyte imbalance, seizures, anemia, fever, GI disturbance

Concurrent administration of: arsenic trioxide, bepridil, levomethadyl, mesoridazine, pimozide, probucol, thioridazine, ziprasidone, intravenous pentamidine

-Renal impairment is the major dose-limiting toxicity

Efavirenz

Nevirapine

Delavirdine

Etravirine

HIV

Rash, psychiatric effects (depression, suicidal ideation), dizziness, insomnia

Concurrent administration of drugs metabolized by P450 3A4 is contraindicated for all of the NNRTIs--must verify metabolism of concurrent medications before prescribing NNRTIs

-Resistance develops rapidly, requiring the use of these drugs in combination with other anti-HIV drugs

HIV

Suicidal risk, renal failure, rhabdomyolysis, insomnia, nausea, asthenia, dizziness, headache, fatigue

Hypersensitivity

-Approved for use only in combination with other anti-HIV drugs

Inhibit HIV protease required for viral maturation; HIV virions replicate and bud from the cell, but these particles are noninfectious

Saquinavir

Ritonavir

Amprenavir

Fosamprenavir

Indinavir

Nelfinavir

Lopinavir

Atazanavir

Tipranavir

Darunavir

HIV

Dyslipidemia (increases in cholestrerol and triglycerides), lipodystrophy, hyperglycemia

Severe hepatic impairment, Concurrent administration of P450 3A4 substrates with narrow therapeutic indices, including ergot derivatives, pimozide, midazolam, triazolam

-Lopinavir is administered in combination with ritonavir; ritonavir inhibits P450 3A4, thus increasing plasma levels of lopinavir

-Many protease inhibitors are inducers and/or inhibitors of P450 enzymes, especially P450 3A4, with numerous pharmacokinetic drug interactions

-Fosamprenavir is a prodrug form of amprenavir with greater oral bioavailability 

Inhibit influenza virus neuraminidase, causing newly synthesized virions to remain attached to host cell

Zanamivir

Oseltamivir

Influenza A and B

Bronchospasm, respiratory depression, GI disturbance, headache, nasal symtoms

Hypersensitivity

-Inhibit both influenza A and B

-Zanamivir is administered by inhaler

-Oseltamivir is approved for both prophylaxis and treatment; zanamivir is indicated only for treatment

-Oseltamivir is used to treat serious human disease due to H5N1 (avian flu) and H1N1 (swine flu)

Cytomegalovirus (CMV) retinitis (2nd-line)

Inflammatory disorders of the eye, transiently elevated intraocular pressure

IV or intravitreal cidofovir therapy within 2-4 weeks, due to risk for exaggerated ocular inflammation

-Was designed as an antisense nucleotide, but the actual mechanism of action is uncertain

-Administered intravitreally

Respiratory syncytial virus (RSV), Hepatitis C virus (in combination with interferon-alpha)

Bradyarrhythmia, hypotension, pancreatitis, hemolytic anemia, thrombotic thrombocytopenic purpura, hepatotoxicity, bacterial infection, suicide, rash, GI disturbance, headache, conjunctivitis, fatigue

Pregnancy or women of child-bearing potential (inhalation), Creatinine clearance less than 50 mL/min (oral), Significant cardiac disease (oral), Hemoglobinopathies (oral), Autoimmune hepatitis (oral, in combination with peginterferon alfa-2a), severe hepatic decompensation

-May inhibit inosine monophosphate dehydrogenase, leading to lower GTP levels; may also inhibit viral RNA polymerases or make the polymerases more error-prone

-Administered in aerosol form for treatment of RSV

Herpes simplex virus (HSV)

Headache, application site reaction

Hypersensitivity

-Lacks significant cytotoxicity

-Exact mechanism of action is unknown

Interferons activate signaling cascades that lead to p[roduction of antiviral proteins, including protein kinase R, which turn off hos translational machinery in virus-infected cells. Imiquimod interacts with Toll-like receptors to boost innate immunity, including the secretion of interferons.

Interferon-alpha

Imiquimod

Hepatitis C virus (HCV), Hepatitis B virus (HBV), Kaposi's sarcoma, Chronic myelogenous leukemia, Hairy cell leukemia, malignant melanoma, renal cell carcinoma

GI hemorrhage, aplastic anemia, neutropenia, thrombocytopenia, increased liver enzymes, autoimmune diseases, psychotic disorder, depression, altered mental status, influenza-like symptoms

Hypersensitivity

-Modified with polyethylene glycol (pegylated to improve pharmacokinetic profile

Human papilloma virus (HPV), Basal cell carcinoma, Actinic keratosis

Skin irritation including erythema, superficial erosin and crusting, burning sensation

Hypersensitivity

-Wash hands before and after application