Flu Drug

Use: Bird flu, flu

Mechanism: Neurominidase inhibitor for Flu A and B; Inhibits release of virus from infected cells (inhibit sialic acid cleave)

Oral

Side effects: nausea/vomiting, 

Other drugs: Zanamivir (Relenza) - Intranasal or oral inhaler, may worsen respiratory function in COPD; may cause bronchospasm in asthmatics

Amantadine (Symmetrel®) -  rarely used, Side effects

Rimantadine (Flumadine®) - rarely used, side effects

Herpes Dx; Antiviral

DOC Herpes (all types, including encephalitis)

Uses: Immunocompromised (chronic) pts for all herpes infections; Genital Herpes (reduces shedding, increases healing speed, decreases duration of pain and formation of new lesions), herpes keratitis (topical), herpes encephalitis (IV), prophylactically in organ transplant pt; Hairy cell leukoplakia (AIDS)

Mechanism: guanosine analogue, gets taken into the cell, phosphorylated by viral thymidine kinase, keeping it in the cell; binds to viral DNA inhibiting replication; competes tih dGTP casuing chain termination

Major Side effect: Somnelence and lethargy when combined with zidovudine (AZT); nephrotox in high IV dose; SAFE IN PREGNANCY

Relatively non-toxic because cell that are not infected do not activate the drug

Herpes Dx: Antiviral

Pro drug that has higher oral bioavailability than acyclovir

food does not affect absorption

Mechanism: Same as acyclovir

2/day admin makes the preferred oral for

Herpes Dx: Antiviral

Use: Herpes zoster

Mechanism: similar to acyclovir, converted to penciclovir in vivo

Renal elimination

nausea,headache, diarrhea

Other Dx: Penciclovir (Denavir) - topical for herpes labialis

Herpes Dx: Antiviral

Uses: CMV/Herpes, Resistant herpes/CMV (other drugs); Usually used if pt is resistant to acyclovir or gancyclovir

Mechanism: Inhibits DNA and RNA polymerase, reverse transcriptase (Direct binding?)

IF

Toxicity: Renal tubular necrosis, genital ulcers in men, 

Herpes Dx: Antiviral

Use: cold sores (topical)

Mechanism: inhibits fusion between plasma membrane and the herpes simplex virus (HSV) envelope, virus can't invade cell

Hep B and C antiviral

Use: initail Hep C and chronic hep B (alfa2b) combo w/ ribavirin; Now combied with serine protease inhibitor, much more effective

Mechanism: inhibits viral protein synth, viral replication, inhibits translation/transcription and viral messenger RNA; Effects virus in many ways

Side effects (hep pt): flu like symptoms, aches/pains, GI, depression/suicide, hematologic = neutropenia, anemia-worse when combined with ribavirin, telaprevir, boceprevir; hypotension, edema

Hep C antiviral

Mechanism: Block activity of serine protease required for production and processing of viral proteins essental for viral replication

Improved absorption, especially fat

Tox: strong CYP3A4 inhibition, anemia, fatigue

Hep C antiviral

Mechanism: Block activity of serine protease required for production and processing of viral proteins essental for viral replication

Improved absorption, especially fat

Tox: strong CYP3A4 inhibition, anemia, fatigue

Hep C antiviral

Mechanism: Block activity of serine protease required for production and processing of viral proteins essental for viral replication

Improved absorption, especially fat

Tox:  strong CYP3A4 inhibition, anemia, fatigue

Hep C antiviral; GAME CHANGER

Use: Combo with interferon for Hep C

Mechanism: Nucleotide analogue that inhibits the activity of Hep C through NS5B RNA polymerase

has decreased viral load from millions to 15 (Example)

Hep B and C antiviral

Use: DOC for chronic hep B, HBV, DOC combo zidovudine for HIV

Mechanism: reverse transcriptase competitive inhibitor used for HIV

few side effects, well tolerated

Hep B and C antiviral

Use: DOC HBV

Mechanism: reverse transcripase inhibitor

Renal toxicity, may cause lactic acidosis

Other Drugs: Entacavir (Baraclude)

Telbivudine (Tyzeka) - similar to lamivudine

Reverse Transcriptase Inhibitor: HIV antiviral

Uses: HAART HIV, (early) prevent opportunistic infections/Kaposi sarcoma, Pregnant pts decrease transmission to newborn, AIDS dementia, psoriasis and adult T cell leukemia (retroviruses)

Mechanism: deoxythymidine analogue, conveted intracellularly to active triphosphate which becomes incorporated into DNA; inhibits viral reverse transcriptase and cause chain termination

Tox: Myelosuppression-anemia (2-6 weeks), neutropenia,  STOP if lactic acidosis or hepatotoxicity develops, CNS, GI

Dx interactions: Increases tox of drugs that are neurotoxic, nephrotoxic, or that affect bone marrow, probenecid decreases elimination

increase risk for granulocytopenia with acetaminophen and ganciclovir

Reverse Transcriptase Inhibitor: HIV antiviral

Uses: HIV combined with zidovudine, pts resistant to zidovudine

Mechanism: Inhibits mitochondrial DNA synth (possible peripheral neuropathy)

Toxicity: Peripheral neuropathy, pancreatitis, anemia, granulocytopenia, hyperuricemia, discontinue if lactic acidosis or hepatotoxicity

used if all else fails

Other Drugs: Zalcitabine (Hivid®) - above info and oral ulcers; peripheral neuropathy

Reverse Transcriptase Inhibitor: HIV antiviral

Uses: DOC HEP B

Toxicity: Lactic Acidosis

Other drugs: Stavudine (Zerit®) - peripheral neuropathy

Reverse Transcriptase Inhibitor: HIV antiviral

Uses: HIV

Toxicity: SERIOUS HYPERSENSITIVITY (never take again), Lactic acidosis nausea, vomiting, diarrhea

Reverse Transcriptase Inhibitor: HIV antiviral

Uses: DOC for HIV in naive pts (combo emtricitabine)

Toxicity: Lactic Acidosis, Nausea, vomiting, abdominal pain and flatulence

Reverse Transcriptase Inhibitor: HIV antiviral

Uses: HIV

Toxicity: Lactic Acidosis

Non-Nucleotide Reverse Transcriptase Inhibitor: HIV antiviral

Efavirenz (Sustiva) - DOC except in pregnancy

Uses: HIV ALWAYS WITH nucleoside analogues (rapid resistance alone)

Mechanism: Binds directly to reverse transcripase and prevents conversion of RNA to ds, not phosphorylation

Toxicity: Induces CYP3A4, dizziness, drowsiness, insomnia, headache, stevens-johnson syndrom, hepatitis; Ketoconazole inhibits metabolism

Can't be used when...

Other Drugs: Delavirdine (Rescriptor®) - antacids decrease absorption, inhibits CYP3A

Integrase Inhibitor

Use: Tx resistant pts where other drugs no longer work

Mech: blocks the integrase enzyme needed for replication, inhibiting transfer of viral DNA to host cell DNA

Side effects: nausea, vomiting, diarrhea, HA

RSV Dx

Uses: Respiratory Syncytial Virus (RSV) and hep C, hospitalizied infants and children with severe lower respiratory tract infections

Mechanism: purine analogue, inhibits RNA polymerase and synthesis of GTP (inhibits viral RNA synth)

Route of admin and why: -aerosol for children; - oral for hep C with interferon; -IV for lassa fever and SARS

Side effects: highly teratogenic; pulmonary, dyspnea, hypotension, anemia, depresion, GI, lethargy

Other Drugs: Palivizumab (Synagis) - RSV Ab, prophylaxis, 1/month admin

CMV/Herpes Dx; Antiviral

Uses: CMV and Herpes; CMV retinitis; Tx or prophylaxis of CMV/herpes in immunocompromised/transplant pts

Mechanism: Activated by viral kinases i.e. thymidine kinase (herpes) or viral protein kinase phosphotransferase (CMV) in cells infected with herpes or CMV; builds up in cell, like acyclovir

IV

Side effects: neutropenia, thrombocytopenia, nausea, fever, rash, phlebitis, headache, confusion, seizures, abnormal LFTs

CMV/Herpes antiviral

Uses: CMV and Herpes; CMV retinitis; Tx or prophylaxis of CMV/herpes in immunocompromised/transplant pts

Mechanism: Activated by viral kinases i.e. thymidine kinase (herpes) or viral protein kinase phosphotransferase (CMV) in cells infected with herpes or CMV; Builds up in cell like acyclovir

Oral

Side effects: neutropenia, thrombocytopenia (more Gancyclovir IV), nausea, fever, rash, phlebitis, headache, confusion, seizures, abnormal LFTs

Other Dx: Fomvirsen (Vitravene®) - antisense compound complementry to mRNA in CMV; IntraVit; SE = ocular inflammation and visual impairment

Cidofovir (Vistide) = resistant CMV/herpes, renal tubular necrosis

Protease Inhibitor antiviral

Mechanism: Inhibit protease which cleaves the long precursors into the proteins needed for viral core ; ALWAYS used in combo with reverse transcriptase inhibitors

Side effects: diarrhea, stomach discomfort, nausea, rhinitis; hyperglycemia, lipodystrophy (cushinoid), Dx interactions from CYP 450 inhibition

Levels increased if taken with grapefruit juice

Protease Inhibitor; antiviral

Use: improves bioavailability of other protease inhibitors by inhibiting CYP3A4

Mechanism: Inhibits metabolism of many other protease inhibitors

Side effects: nausea, vomiting, weakness, diarrhea, burning or tingling around the mouth and in periphery, eleveted liver enzymes; hyperglycemia, lipodystrophy (cushinoid), Dx interactions from CYP 450 inhibition

Protease Inhibitor/antiviral

Mechanism: Inhibit protease which cleaves the long precursors into the proteins needed for viral core; ALWAY used in combo with reverse transcriptase inhibitors

Side effects: nephrolithiasis, asymptomatic hyperbilirubinemia; hyperglycemia, lipodystrophy (cushinoid), Dx interactions from CYP 450 inhibition

Other Drugs: Nelfinavir (Viracept)

Protease Inhibitor/antiviral

Use: DOC HIV

Mechanism: Inhibit protease which cleaves the long precursors into the proteins needed for viral core; ALWAY used in combo with reverse transcriptase inhibitors

Side effects: "buffalo hump", abdominal fat increase with THIN FACE! (different from corticosteroids); cholesterol/TAG increase, atherosclerosis, CV incidents, MI, DM, depression, abdominal pain; hyperglycemia, lipodystrophy (cushinoid), Dx interactions from CYP 450 inhibition

Protease Inhibitor/antiviral

Use: HIV

Mechanism: Inhibit protease which cleaves the long precursors into the proteins needed for viral core; ALWAY used in combo with reverse transcriptase inhibitors

Side effects: "buffalo hump", abdominal fat increase with THIN FACE! (different from corticosteroids); cholesterol/TAG increase, atherosclerosis, CV incidents, MI, DM, depression, abdominal pain; hyperglycemia, lipodystrophy (cushinoid), Dx interactions from CYP 450 inhibition

Non-peptidic Protease Inhibitor/antiviral

Use: HIV with Ritonavir

Mechanism: Inhibit protease which cleaves the long precursors into the proteins needed for viral core; ALWAY used in combo with reverse transcriptase inhibitors

Side effects: "buffalo hump", abdominal fat increase with THIN FACE! (different from corticosteroids); cholesterol/TAG increase, atherosclerosis, CV incidents, MI, DM, depression, abdominal pain; hyperglycemia, lipodystrophy (cushinoid), Dx interactions from CYP 450 inhibition

Other drugs: Darunavir (PrezistaTM)

Fusion Inhibitor/antiviral

Uses: Advanced HIV when other drugs beggin to fail (resistance)

Mechanism: binds to viral envelop glycoprotein and prevents fusion of virus and entry into cell; no cross resistance with other drugs

Side effects: Injection site reactions/swelling common, pneumonia more likely

Other Drugs: Maraviroc (Selzentry) - Pts with CCR-5-tropic HIV infection and other treatment not effective