Microbio - antiviral drugs Flashcards
Do not give aspirin in children for fever,. You give what?
Acetaminophen
Chemical treatment for genital warts
Podophyllin
Host-coded proteins that are member of cytokines and which inhibits viral replication.
Interferon (IFN)
type II or immune interferon
IFN Gamma
T or F: IFN does not protect virus-infected cell and not itself the antiviral agent
True
Neuraminidase inhibitors that can shorten course of influenza A and B infection
Zanamivir (inhaled)
Oseltamivir (oral)
Rimantadine and amantadine action
Prevents viral un coating in influenza A
Inhibits early replication of influenza A (not B)
Prevents in coating by binding to M2 (matrix protein)
Amantadine
Other name for amantadine
Alpha-adamantanamine
Symmetrel
Resistant strains of influenza A to amantadine
H3N2 virus
H1N1 strains
Has longer half life than amantadine
Require no dosage adjustment in renal failure
Rimantadine
Other name for rimantadine
Flumadine
Drugs that inhibits NA synthesis
Acyclovir Ganciclovir Vidarabine Fomivirsen Foscarnet
Drug of choice for HSV-1 encephalitis
Acyclovir
Treatment fro HSV 1&2 and VZV
Acyclovir
Phsphorylated acyclovir is converted by thymidine kinase into…. which interferes with viral synthesis by acting as competitive substrate for DNA polymerase and chain termination
Acyclovir triphosphate
Acyclovir triphosphate inhibits DNA synthesis by (2)
Competitive substrate for DNA polymerase
Chain termination
Involved in the initial viral-specific phosphorylation of acyclovir
Thymidine kinase
Prodrug and oral prep of ganciclovir
Valgancyclovir
Prodrug of acyclovir?
Valacyclovir.
It has longer duration
Another guanosine analog that does not cause chain termination
Penciclovir
Major route of elimination of acyclovir
Renal excretion
Mode of action of ganciclovir
Inhibits DNA polymerase of cmv and HSV
Chain termination
Treatment for CMV infection
Ganciclovir
Dihydroxypropoxymethylguanine (DHPG)
Gancyclovir
Drug of choice for CMV retinitis
Gancyclovir
Adverse effect of ganciclovir
MaLTHuS Mucositis Leukopenia Thrombocytopenia Hepatic dysfunction Seizure
Adenine arabinose, ara-A
Vidarabine
Nucleoside analog of arabinose, instead of ribose.
Teratogenic.
Vidarabine
Topical herpes keratitis but no effect on genital lesions
Vidarabine
Adverse effect of vidarabine
GiPiTCH Gi irritation Paresthesia Tremor Convulsion Hepatic dysfunction
Antisense oligonucleotide that binds to mRNA of CMV
Fomivirsen
Trisodium phosphonoformate, foscavir
Foscarnet
Injected intravitreally for treatment of CMV retinitis
Fomivirsen
Does not require phosphorylation
Inhibits DNA and RNA polymerase and reverse transcriptase
Pyrophosphate analog
Foscarnet
Prophylaxis and treatment for ganciclovir-resistant strains
Foscarnet
Adverse effects of foscarnet
Nephrotoxicity
Hypocalcemia
Hallucination
Seizures
Structural difference between nucleoside and nucelotide
Nucleotide has an attached phosphate group
It has an ability to persist in cells for long period of time increasing their potency
NNRTI or NRTI
Do not need phosphorylation
Binds directly and incompetitively to reverse transcriptase
NNRTI
NRTI or NNRTI:
Competitive inhibition of HIV-1 reverse transcriptase
Requires intracytoplasmic activation via phosphorylation
Activity against HIV-1 and HIV-2
NRTI
NRTI or NNRTI :
Binds directly to HIV-1 reverse transcriptase resulting in allosteric inhibition of RNA and DNA-dependent DNA polymerase.
Neither competes with nucleoside triphosphate s nor require phosphorylation to be active
No activity against HIV-2
NNRTI
NRTIs
Azidothymidine (zidovudine, AZT) Dideoxyinosine (didanosine, ddI) Dideoxycytidine (zalcitabine, ddC) Didehydro-dideoxythymidine (stavudine, d4T) Ribavirin (Virazole) Emtricitabine Methisazone (N-methylisatin B-thiosemocarbazone) Tenofivir Lamivudine (3TC)
Confers resistance to NRTIs
Pol genes
Zidovudine, retrovir, AZT
Azidothymidine
Drug of choice for patients with AIDS
Azidothymidine
Increase plasma levels of azidothymidine by…
Antifungals
This drug increases the clearance of azidothymidine
Rifampin
Primary adverse effect of azidothymidine
Bm suppression
Treatment for AIDS patients resistant to azidothymidine
Dideoxyinosine
Primary adverse effect of dideoxyinosine
Pancreatitis
Peripheral neuropathy
Didanosine, videx, ddl
Dideoxyinosine
Drug is metabolized into ddATP to be active
Dideoxyinosine
Drug is metabolized to ddCTP to be active
Dideoxycytidine
Zalcitabine, hivid, ddc
Dideoxycytidine
Main adverse effect of dideoxycytidine
Peripheral neuropathy
Stavudine, zerit, d4T
Didehydro-dideoxythymidine
Treatment for advance AIDS patients
Didehydro-dideoxythymidine
Main adverse effect of Didehydro-dideoxythymidine
Peripheral neuropathy
Lactose acidosis
Hepatic steatosis
Ddl, ddc, d4T all cause this adverse effect
All Ds cause peripheral neuropathy
Thiazole-carboxamide moiety is substituted by aminoimidazole-carboxamide
Ribavirin
Virazole
Ribavirin
Inhibits synthesis of guanine nucleotides
For RSV infection in children
Ribavirin
Contains propylene glycol
Contraindications for pregnancy and young children
Adverse effects of renal or hepatic dysfunction
Emtricitabine
1st protease inhibitor to be approved for treatment of HIV
Saquinavir
Inhibitor of protease encoded by HIV
Saquinavir
Indanivir
N-methylisatin - B-thiosemicarbozone
Methisazone
Inhibits pox protein synthesis
Blocks translation of late mRNA
Methisazone
Has activity against HBV
Asso with fanconi’s syndrome
Tenofovir
Included in HAART regimen
Effective against HBV infection by inhibiting DNA polymerase
Safely administered to patients with decompensated liver disease
Lamivudine (3TC)
Highly active anti-retroviral therapy (HAART)
1st line standard care
2 NRTI + 1 PI
NNRTI
Delavirdine
Efavirenz
Efavirine
Nevirapine
NNRTI that are teratogenic
Delavirdine
Efavirenz
Frequent adverse effects of NNRTI
Rash (ulceration, SJS)
1st NNRTI to be approved for treating HIV infection
Nevirapine
Blood levels decreased by antacids, phenytoin and rifampin
Increased by azole antifungals and macrolides
Teratogenic
Delavirdine
Has an adverse effect of nightmare and nausea
Efavirenz
Blood level of delavirdine is increased by …
Azole, antifungal and macrolides
Blood level of delavirdine is decreased by
Antacids, phenytoin and rifampin
Enhance bioavailability by fatty foods
Metabolized by cytochrome p450
Teratogenic
Efavirenz
Newest NNRTI
Efavirine
For treatment-experienced HIV
Effective against HIV strains resistant to other drugs
Induced CYP3A4
Inhibits CYP2C9 and CYP2C19
Efavirine
Efavirine inhibits ..
CYP2C9 and CYP2C19
NNRTI that penetrates most tissue including CNS and placenta
Metabolized by CYP3A4
Effective in preventing HI vertical transmission
Nevirapine