Acyclovir is Tx for? Mech?

*HSV*Guanosine analogue; Activated by viral thymidine kinase-->INHIBITS DNA synthesis by competing with dGTP
Acyclovir mech of resistance? Resistance develops due to DECREASE in viral thymidine kinase
Acyclovir pros and cons? NO Bone Marrow effect
Very well-tolerated
Will NOT work against CMV
Excreted by Kidney-->Nephrotoxicity with HIGH IV doses
Acyclovir drug interaction & effect of note? Somnolence/lethargy with Zidovudine
Valacyclovir similar to _________? Admin? Acyclovir
ADMIN: Oral
Famciclovir/Penciclovir similar to ________? Acyclovir
Docosanol mech? Use/admin? INHIBITS viral fusion to cell membrane
OTC for
HSV, cold
sores
(topical)
Ganciclovir/Valganciclovir mech? Inhibits Cytomegalovirus (CMV) DNA replication; Activated by viral kinases in cells infected with herpes or CMV
Ganciclovir/Valganciclovir pros and cons? Less selective than Acyclovir- more toxicBone Marrow Toxicity!
Ganciclovir/Valganciclovir drug interaction/effect? Do NOT combine with other Bone Marrow drugs (Zidovudine)
Cidofovir uses? Resistant CMV and herpes
Cidofovir adverse effects? Prevention of these? Renal toxicityUse probenecid & hydrate
Foscarnet mech? Inhibits DNA & RNA polymerase, reverse transcriptase
Foscarnet admin/uses? Adverse? IV, resistant herpes and CMVRenal toxicity
Name the drugs used for Herpes (only).
Name the CMV/Herpes drugs. Note:anything that treats Herpes can end with -ciclovir
Oseltamivir, Zanamivir mech? Uses? Neuraminidase inhibitorsActive against Influenza A and B
Ribavirin mech? Uses/admin? Inhibits viral RNA synthesisPrimary uses are RSV (aerosol) and Hep C (w/IFNs)
Ribavirin adverse effects? Very Teratogenic!!!
Name the Influenza drugs.
Name the RSV drugs. *Ribavirin (Virazole)Palivizumab (SynagisTM)"PAVLOV's dog ate RIBs in his custom RV"
Lamivudine mech? Reverse transcriptase inhibitor used for HIV; Also inhibits HBV polymerase
Lamivudine adverse effects? DOC for? Few side effects, well-toleratedDOC for CHRONIC Hepatitis B
Interferon alpha-2b MAIN use? alpha-2b with ribavirin for HCV
Interferons adverse effects? (3) Flu-like symptomsCNS depression, suicideBone marrow depression
Boceprevir, Toleprevir mech? Uses? Protease inhibitor of HCVFor HCV genotype I
Boceprevir, Toleprevir adverse effects/drug interactions? Strong CYP3A4 INHIBITIONBone marrow depression
Name the Hep B and C drugs *Interferon-alfa2b (Intron-A; PegIntron), Interferon alfa2a (Pegasys)**Boceprevir (Victrelis),Teleprevir (Incivik),Semeprevir (Olysis)**Sofosbuvir (Sovaldi)*Lamivudine (Epivir)*Adefovir (Hepsera), Entacavir (Baraclude)Telbivudine (Tyzeka)"A-DEFening BOSE TELEfone speaker will SEMPRE-PREVent any LAMe HEP B and C INTERFERence"
HIV Reverse Transcriptase Inhibitors mech? Common adverse effect? Mechanism like AcyclovirAll will cause Lactic Acidosis
Name the HIV Reverse Transcriptase Inhibitors (NTRI's). *Zidovudine*Lamivudine (also used for Hep B & C)*Emtracitabine*Tenofovir*DidanosineZalcitabineStavudine*Abacavir"DID you REVERSE that TENOR's LAME ABC's back to "ZID", or EM-i-TRICkIng myself?"
Zidovudine pros? Maintain CD4 countsDECREASE risk of transmission to newborns
Zidovudine cons? Neutropenia and anemia
When to stop Zidovudine? What drug interactions (why)? Stop if lactic acidosis or hepatotoxicity developDont combine with Ganciclovir (Bone Marrow) or Acyclovir (can get somnolence when in combo)
Tenofovir, Emtractibine combo is DOC for? Adverse FX? Nave HIV patientsGI, flatulence (Tenofovir)
KNOW serious side FX chart...
Didanosine admin (combo w/)?Adverse effect? Combined with ZidovudinePeripheral neuropathy, pancreatitis
Zalcitabine adverse FX? Peripheral neuropathy, Oral ulcers
Stavudine adverse effect? Peripheral neuropathy
Abacavir adverse effect? Significance? Hypersensitivity: do NOT use again!!!
Non-Nucleotide RTIs (NNRTIs) admin? What is preferred drug from this group? When is it NOT preferred and what do you use instead? Use ONLY with nucleoside analoguesEfavirenz= preferred drug, EXCEPT in pregnancy -- Switch to Nevirapine
Adverse effect of Efavirenz and Delavirdine? Adverse FX of Nevirapine? (2) Efavirenz and Delavirdine teratogenic!Nevirapine- hepatitis, Stevens Johnson
Name the NNRTIs (NON-nucleoside Reverse Transcriptase Inhibitors).
Name the Protease inhbiitors. ALL end with "navir!" (Atazenavir, Ritonavir)
Protease inhbiitors drug interactions? Specific effects? (9) Most metabolized by CYP3A4Many drug interactions: (Cushing's-like)Altered body fat distributionBuffalo humpAbdominal fat INCREASESBUT- face is thin (diff from corticosteroids)INCREASE cholesterol/TAGsDM, MI, stroke
Atazanavir uses? DOC for HIV!!!
Ritonavir drug interactions? INHIBITS CYP3A4
Ritonavir typically used how?Typical use?Atypical ingredient? Combined with other Protease Inhibitors to INCREASE their bioavailabilityBooster!Contains alcohol
Indinavir uses? Adverse FX? X-resist with RitonavirKidney stones, HYPERbilirubinemia
Amprenavir/Fosamprenavir (combo drug) atypical ingredient and drug interaxn?Adverse FX? Contains propylene glycol- avoid metronidazole!Stevens-Johnson syndrome/rash
Name the HIV fusion inhibitors. Enfuvirtide (Fuzeon)Maraviroc (SelzentryTM)"MY-RIVA-ROCks an ENFURiating FUSION against HIV"
Enfuviritide mech?Adverse effect? Prevents fusion and entry of HIV into cellInjection sites reactions
Maraviroc mech? Adverse effects?Resistance? CCR5 on HIVRash most commonResistance!
Raltegravir mech? Blocks integrase (ONLY integrase inhibitor)
Bad HIV combos and why? (3) Atazanavir/Indinavir (bilirubin)Didanosine/Stavudine (neuropathy)Zidovudine/Stavudine (antagonize each other)
*HSV*Guanosine analogue; Activated by viral thymidine kinase-->INHIBITS DNA synthesis by competing with dGTP
Resistance develops due to DECREASE in viral thymidine kinase
Inhibits Cytomegalovirus (CMV) DNA replication; Activated by viral kinases in cells infected with herpes or CMV
Less selective than Acyclovir- more toxicBone Marrow Toxicity!
Do NOT combine with other Bone Marrow drugs (Zidovudine)
Neuraminidase inhibitorsActive against Influenza A and B
Inhibits viral RNA synthesisPrimary uses are RSV (aerosol) and Hep C (w/IFNs)
*Ribavirin (Virazole)Palivizumab (SynagisTM)"PAVLOV's dog ate RIBs in his custom RV"
Reverse transcriptase inhibitor used for HIV; Also inhibits HBV polymerase
Few side effects, well-toleratedDOC for CHRONIC Hepatitis B
Flu-like symptomsCNS depression, suicideBone marrow depression
*Interferon-alfa2b (Intron-A; PegIntron), Interferon alfa2a (Pegasys)**Boceprevir (Victrelis),Teleprevir (Incivik),Semeprevir (Olysis)**Sofosbuvir (Sovaldi)*Lamivudine (Epivir)*Adefovir (Hepsera), Entacavir (Baraclude)Telbivudine (Tyzeka)"A-DEFening BOSE TELEfone speaker will SEMPRE-PREVent any LAMe HEP B and C INTERFERence"
*Zidovudine*Lamivudine (also used for Hep B & C)*Emtracitabine*Tenofovir*DidanosineZalcitabineStavudine*Abacavir"DID you REVERSE that TENOR's LAME ABC's back to "ZID", or EM-i-TRICkIng myself?"
Maintain CD4 countsDECREASE risk of transmission to newborns
Stop if lactic acidosis or hepatotoxicity developDont combine with Ganciclovir (Bone Marrow) or Acyclovir (can get somnolence when in combo)
Combined with ZidovudinePeripheral neuropathy, pancreatitis
Use ONLY with nucleoside analoguesEfavirenz= preferred drug, EXCEPT in pregnancy -- Switch to Nevirapine
Efavirenz and Delavirdine teratogenic!Nevirapine- hepatitis, Stevens Johnson
Most metabolized by CYP3A4Many drug interactions: (Cushing's-like)Altered body fat distributionBuffalo humpAbdominal fat INCREASESBUT- face is thin (diff from corticosteroids)INCREASE cholesterol/TAGsDM, MI, stroke
Combined with other Protease Inhibitors to INCREASE their bioavailabilityBooster!Contains alcohol
Contains propylene glycol- avoid metronidazole!Stevens-Johnson syndrome/rash
Enfuvirtide (Fuzeon)Maraviroc (SelzentryTM)"MY-RIVA-ROCks an ENFURiating FUSION against HIV"
Prevents fusion and entry of HIV into cellInjection sites reactions
Atazanavir/Indinavir (bilirubin)Didanosine/Stavudine (neuropathy)Zidovudine/Stavudine (antagonize each other)
*Interferon-alfa2b (Intron-A; PegIntron), Interferon alfa2a (Pegasys)**Boceprevir (Victrelis),Teleprevir (Incivik),Semeprevir (Olysis)**Sofosbuvir (Sovaldi)*Lamivudine (Epivir)*Adefovir (Hepsera), Entacavir (Baraclude)Telbivudine (Tyzeka)"A-DEFening BOSE TELEfone speaker will SEMPRE-PREVent any LAMe HEP B and C INTERFERence"
*Zidovudine*Lamivudine (also used for Hep B & C)*Emtracitabine*Tenofovir*DidanosineZalcitabineStavudine*Abacavir"DID you REVERSE that TENOR's LAME ABC's back to "ZID", or EM-i-TRICkIng myself?"
Most metabolized by CYP3A4Many drug interactions: (Cushing's-like)Altered body fat distributionBuffalo humpAbdominal fat INCREASESBUT- face is thin (diff from corticosteroids)INCREASE cholesterol/TAGsDM, MI, stroke
*Interferon-alfa2b (Intron-A; PegIntron), Interferon alfa2a (Pegasys)**Boceprevir (Victrelis),Teleprevir (Incivik),Semeprevir (Olysis)**Sofosbuvir (Sovaldi)*Lamivudine (Epivir)*Adefovir (Hepsera), Entacavir (Baraclude)Telbivudine (Tyzeka)"A-DEFening BOSE TELEfone speaker will SEMPRE-PREVent any LAMe HEP B and C INTERFERence"
Acyclovir/Valacyclovir
Acyclovir/Valacyclovir
Acyclovir/Valacyclovir
Famcyclovir
Famcyclovir
Pencyclovir
Trifluridine
Docosanol
Docosanol
Docosanol
Ganciclovir/Valganciclovir
Ganciclovir/Valganciclovir
Ganciclovir/Valganciclovir
Cidofovir
Cidofovir
Cidofovir
Foscarnet
Foscarnet
Foscarnet
Oseltamivir (Tamiflu) and Zanamivir (Relenza)
Oseltamivir SE?
Zanamivir
Amantadine and Rimantidine
Amantadine and Rimantidine
Amantadine SE?
Rimantidine SE?
Ribavirin
Ribavirin
Ribavirin
Palivizumab
Lamivudine
IFN-2b (Interferon alfa-
2b)
IFN-2b (Interferon alfa-
2b)
IFN-2b (Interferon alfa-
2b)
Boceprevir, Telaprevir,
Simeprevir
Boceprevir, Telaprevir,
Simeprevir
Boceprevir, Telaprevir,
Simeprevir
Mech: Taken in cell phosphorylated by viral thymidine kinase concentrates in infected
herpes cell (30-300x) competes w/ dGTP inhibits viral DNA pol chain termination
a. Works during the viral synthesis phase
Use: DOC Herpes (wide range of uses), esp. genital
( viral shedding, pain, formation of new lesions, speed of healing,)
SE:
a. Non-toxic to normal cells at therapeutic doses = minimal side-effects
b. high IV doses renal toxicity (only done in severe infx)
c. Prego ok!
Mech: Converted in vitro to Pencyclovir
(just like Acyclovir) Phosphorylated by viral thymidine kinase competitively inhibits DNA
pol
Kidney excreted
IV form of Famcyclovir
not used (too toxic) visual haze
Mech: inhibits fusion (plasma membrane + HSV envelope)
Use: Topical tx of cold sores
SE: skin irritation, headache
Mech: Similar to acyclovir (synthetic analog of guanosine)
a. Herpes = phosphorylated by viral thymidine kinase
b. CMV = phosphorylated by kinase phosphotransferase
Use: Broader coverage (hence CMV/Herpes coverage) > more side effects
a. valganciclovir = oral CMV prophylaxis (esp. transplant pts)
b. ocular implant = tx CMV retinitis
SE: Less specific = side-effects
a. Neutropenia (esp. w/ other drugs that cause neutropenia)
(ex. IFN, Boceprevir, telaprevir, simeprevir, zidovudine)
Mech: Cytosine analog (inhibits viral DNA pol)
Use: kills resistant resistant strains = No enzyme needed for activation intracellularly
SE : kidney eliminated = renal tubular necrosis nephrotoxicity & renal insufficiency
Mech: Antisense compound (binds to mRNA in CMV = cant make protein)
Use : CMV/herpes
SE : Eyes (ocular inflammation, visual impairment)
Mech: Viral neuraminidase inhibitors for influenza A and B virus cant get out of the cell
GI (nausea, vomiting)
Respiratory
Mech: Block uncoating of virus (cloaking inhibitors)
Use: Rarely used due to SE nausea (tx influenza A only )
Hallutionations (increased dopamine)
Doesn't cross BBB, no CNS Sx
Mech : uncertain (inhibits viral mRNA synthesis)
Use: RSV, hepatitis C (used in almost all protocols), herpes simplex, and influenza
a. Combined w/ IFN to tx of Hep C
SE:
a. TERATOGENIC!!!
b. aerosol = pulmonary issues (eg dyspnea)
c. oral = anemia, depression
d. IFN/Ribavirin combo. = anemia and depression SE = watch out!
(ABCDE = A, anemia; B, breathing (SOB,); C, chest sore, cardiac; D, depression); E, embryo
dmg)
Monoclonal ab. confers passive immunity to RSV (not commonly used)
Mech:inhibits HBV DNA polymerase and reverse transcriptase
Use: DOC Hep B, also used in HIV (not IFN, old DOC)
Mech: Affects the virus at many different stages
(synthesis, replication, translation, transcription, processing, penetration,release)
Use:
a. most common for Hep C
b. Chronic Hep B too
c. Combo tx = (IFN-2b + Ribavirin ) SE
(+ serine protease inhibitor) if still not effective
SE:
a. Flu-like sx (fever, ,malaise, headache, fatigue, chills tx w/ acetaminophen)
b. Musculoskeletal (myalgia, arthralgia)
c. Depression suicide
d. Hematologic (anemia, neutropenia, thrombocytopenia)
e. Tx w/ ribavirin > increased suicidal and anemia effects
Mech: Viral serine protease inhibitors
Use: Combo with interferons and ribavirin
SE: Strong inhibitors of CYP3A4 drug interactions
a. anemia, neutropenia, fatigue