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Gupta antivirals
see above
| Question | Answer |
|---|---|
| Adamantanamines | Aamantadine and rimantadine; enters cell; inhibits viral uncoating in host cell; Basic = Prohibit acidic environment needed; amantadine excreted unchanged, Rimantadine undergoes hepatic metab |
| Excretion of amantadine is increased in _______urine | Amantadine pKa ~9.0 (acidic urine increases excretion) |
| Neuraminidase inhibitors | oseltamivir and zanamivir; zanamivir is Not taken orally (polar and charged guanidine group) Inhalation powder; prophylaxis and treatment |
| Why zanamivir has much lesser resistance | Guanidino group in zanamavir forms more H-bonds |
| Oseltamivir | ethyl ester prodrug |
| Valacyclovir vs Acyclovir | Valacyclovir is more effective, more bioavailable at equivalent dose of acyclovir; |
| Why avoid 3TC and FTC in combo? | similar N-base (cytidine): compete for phosphorylation; Two “like” nucleoside analogues are generally avoided: too toxic |
| Foscarnate mimics | pyrophosphate; Does not require activation step before attacking viral enzymes (may be good in resistant cases); is not a nucleoside/tide; not a bioprecursor; Reversible; inhibs DNA and RNA IV only For CMV and HSV 1 and 2 Does not require activation |
| Bisphosphonates are used orally, why not foscarnate? | Highly ionized at physiological pH: metabolic abnormalities; High affinity for bones: Sequestration in bones, 10-20% of given dose: May lead to bone abnormalities |
| Nucelotides are | monophosphrylated; only need diphosphorylation |
| Inhibition of viral attachment and entry Anti HIV | Enfuvirtide, maraviroc |
| Inhibition of viral uncoating anti Flu | Amantadine, rimantadine |
| Inhibition of viral release anti flu | Zanamavir, oseltamivir, peramivir |
| Inhibition of viral genome replication Nucleoside/nucleotide analogs Anti-herpesvirus | Acyclovir, valacyclovir, ganciclovir, valganciclovir, penciclovir, femciclovir, vidarabine, trifluridine, idoxuridine, cidofovir |
| Inhibition of viral genome replication Nucleoside/nucleotide analogs Anti CMV | ganciclovir, valganciclovir, cidofovir |
| Inhibition of viral genome replication Nucleoside/nucleotide analogs anti HIV | Zidovudine, stavudine, lamivudine, Emtricitabine, didanosine, abacavir, tenofovir |
| Inhibition of viral genome replication Nucleoside/nucleotide analogs anti Hep B | Adefovir, entecavir, telbivudine, lamivudine, tenofovir |
| Non-nucleoside analogs DNA polymerase inhibitor For CMV, HSV-1 & HSV-2 | Foscarnet |
| Non-nucleoside Reverse transcriptase inhibitors anti HIV | Efavirenz, nevirapine, delaviridine, etravirine |
| Inhibition of viral maturation anti HIV | Saquinavir, ritonavir, amprenavir, fosamprenavir, indinavir, nelfinavir, lopinavir, atazanavir, tipranavir, darunavir |
| Overlapping uses: | Ganciclovir, Valganciclovir, Cidofovir and Foscarnet: Useful as Anti-HSV and as anti-CMV Lamivudine and Tenofovir: Useful as anti-HIV and anti-hepatitis B Interferons are also useful for anti-hepatitis B & C |
| Enfuvirtide (T-20, Fuzeon) | fusion inhib; anti HIV; not PO; SQ inj only; Only approved antiretroviral drug that must be administered parenterally |
| Entry inhib | Maraviroc {Selzentry} Mimics loss of fnx |
| Inhibs neuraminidase; prevents Sialic cleavage; prevents infectious virus release | Zanamivir; oseltamivir |
| Inhibs viral uncoating | Amantadine, Rimantadine |
| _______ and ________ enters cell while ________ and __________ do not | Amantadine; rimantadine. Zanamivir; oseltamivir |
| Buffer to resist change in pH Used for tx/prophylaxis of influenza A, not B or C | Amantadine, Rimantadine |
| Blocks sialic acid cleavage by neuraminidase | Zanamavir; oseltamivir |
| Inhalation powder; polar/charged guanidine group; low resistance | Zanamivir |
| has high resistance w H1N1 | Oseltamivir |
| has low resistance to all flu | Zanamivir |
| have high resistance to flu A (H3N2) and novel flu A (H1N1) | Adamantenes |
| Zanamavir has | Guanidino group; forms more H bonds; less resistance |
| ) is an ethyl ester prodrug Ester hydrolysis leads to active drug Oxidation makes inactive | Oseltamivir (Tamiflu) |
| A nucleoside is phophorylated to a nucleoTIDE By | virus polymerases |
| Mimics normal nucleoside Guanosine | Acyclovir |
| Acyclovir triphosphate mistaken for | deoxyguanosine triphos |
| Extra hydroxymethyl (-CH2OH) in ganci and penci: Why? | More affinity Closer to actual structure |
| Famciclovir is a prodrug for | penciclovir; 6 deoxy diacetyl ester prodrug |
| Famciclovir has ___ step activation to penciclovir | two; Oxidation at 6 position; deacetylation/hydrolysis |
| Idoxuridine | Similarity to uridine; extra iodo Inhibs virus genome; thpx effect or Similarity to thymidine; CH3 replaced w iodide Inhibs mammalian genome Topical only; to toxic for PO; cardiotoxic |
| Trifluridine | Similar to Uridine; extra CF3 Inhibs virus genome; thpx effect Or Similar to thymidine; Hs replaced by Fs Inhibs mammalian genome Topical only; toxic if PO |
| has a cytosine Nucleus; cytosine analouge; Will be diphosphorylated to be active | Cidofovir |
| Nucleotide; doesn’t need initial phosphorylation w viral enzyme Good for acyclovir resist herpes/Ganciclovir resist CMV | Cidofovir |
| Zidovudine | AZT, ZDV |
| Didanosine | ddI |
| Stavudine | d4T |
| Lamivudine | 3TC |
| Abacavir | ABC |
| Tenofovir disoproxil | TDF |
| Emtricitabin | FTC |
| Thymidine analogue | Zidovudine (AZT, ZDV); Stavudine (d4T); Telbivudine; |
| Cytosine analogues | Lamivudine (3TC); Emtricitabine (FTC); Cidofovir |
| Purine analogue | Didanosine (ddI) |
| Guanosine derivative | Abacavir; Entecavir; Acyclovir; ganciclovir; penciclovir |
| Adenosine derivative | Tenofovir (nucleotide); adefovir |
| Desired combinations: Lamivudine (3TC) with | zidovudine (AZT)→ Combivir®; abacavir → Epzicom®; zidovudine and abacavir → Trizivir® |
| Desired combinations Emtricitabine (FTC) with | Tenofovir →Truvada® |
| Foscarnet SEs | Affects Ca2 and phos levels Chelates Divalent metals; Ca2, Mg2 Similar to bisphosphonates; high affinity for bones High ionized at physiological pH |
| NNRTIs | Efavirenz, nevirapine, delaviridine, etravirine |
| 1st gen NNRTIs | Nevirapine {Viramune} (NVP); Delaviridine {Rescriptor} (DLV); Efavirenz {Sustiva} (EFV); Hydrophobic; bind to allosteric site; locks neighbor substrate site into inactive |
| 2nd gen NNRTIs | Etravirine {Intelence} (ETR) |
| Pis | Saquinavir; Ritonavir; Amprenavir/Fosamprenavir; Indinavir; Nelfinavir; Lopinavir; Atazanavir; tipranavir; darunavir;; Inhibs maturation of virus |
| Understand differences between hydroxyethylene and hydroxyethylamine? | -etheylamine has an N |
| Understand difference between statine and norstatine core? | Lack of R group on norstatine |
| PI that isnt a peptidomimetic | Tipranavir |
| Transition state analogue of Phe-Pro cleavage site | Saquinavir (Invirase, SQV) Hydroxyethylamine; the N-CC-OH group; H phobic, H bond interactions |
Created by:
DudeEH
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