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S3.M2.Pharm9&10
Anti-Viral Drugs
45
Pharmacology
Professional
06/25/2010

Additional Pharmacology Flashcards

 


 

Cards

Term
Acyclovir
Definition
-antiherpes agent --> DOC for HSV encephalitis
-poor CNS distribution
Term
Famciclovir
Definition
-antiherpes agent
-prodrug
-less affinity for viral pol. than ACYCLOVIR, but can enter the cell in higher concentrations
Term
Penciclovir
Definition
-treats recurent fever blisters
Term
Trifluridine
Definition
-antiherpes agent
-***can be activated by infected and host cell enzymes***
-can also be incorporated into human DNA and cause damage--> this is why it is administered LOCALLY, not systemically
Term
Ganciclovir
Definition
-anti-cytomegalovirus (CMV)
-can be administered via a drug releasing ocular implant--> treats RETINITIS
-must be phosphorylated by the infected cell first (PHOSPHSOTRANSFERASE UL97) to be activated
-prevents development of KAPOSI SARCOMA in AIDS patients
***MYELOSUPRESSION is a side effect***
Term
Fomivirsen
Definition
-anti CMV agent
-Gene therapy approach to anti-viral therapy (antisense oligonucleotide)
-administered intraocularly-->RETINITIS
-not a first choice, but a "big gun" if other drugs don't work
-can cause cataracts, or intraocular pressure
Term
Foscarnet
Definition
-treats several viruses including HIV
-inhibits viral DNA and RNA polymerase or RT by inhibiting PYROPHOSPHATE binding site of the enzyme
-used with Ganciclovir to treat RETINITIS, ESOPHAGITIS, and COLITIS
**used when resistance to ACYCLOVIR is shown
Term
Cidofovir
Definition
-anti CMV agent along with other viruses
-***given with PROBENECID***
-must be phosphorylated 2x by host cells
-competitively inhibits viral DNA POLYMERASE
Term
***abacavir
Definition
-antiretroviral (anti-HIV)
-causes severe HYPERSENSITIVITY RXNS
Term
***Didanosine
Definition
-POOR ABSORPTION must be taken on empty stomach-->inactivated by gastric acids, contains buffers that can inhibit absorption of other drugs
-can cause pancreatitis, hepatitis, retinal changes
Term
***Emtricitabine
Definition
-inhibits HEP B DNA POL and RT
-hyperpigmentation of soles of hand and palms of feet
Term
***Lamivudine
Definition
-inhibits HEP B and RT
-can cause PANCREATITIS
Term
***Zidovudine
Definition
-FLAGSHIP HIV drug
-3 or more mutations necessary to acquire resistance
-HIV associated dementia
-prevents transfer of HIV from mother to child
-can cause MYELOSUPPRESSION and HEPATOTOXICITY
Term
***Stavudine
Definition
-can cause peripheral neuropathy and ascending muscular weakness
-
Term
Nevirapine
Definition
-used to prevent mother to daughter HIV transmission
like Zidovudine
Term
Delavirdine
Definition
-absorption inhibited by antacids and H2 receptor antagonists
-require no phosphorylation to be activated
-anti-HIV 1 (not against HIV 2)
-target RT
-high rate of resistance development-->use several NNRTIs at once
-
Term
Efavirenz
Definition
Term
Atazanavir
Definition
Term
Indinavir
Definition
Term
Lopinavir
Definition
Term
Ritonavir
Definition
potent inhibitor in cytochrome P450 enzyme-->administered in combination with other protease inhibitor to increase clearance
Term
Saquinavir
Definition
Term
Enfuvirtide
Definition
biologic-peptide
active against HIV 1 only--> bind gp41 and prevents ENTRY form occurring
Term
Maraviroc
Definition
-strong effectiveness against R5HIV1 (specific HIV strain)
-alters CCR5 receptor on HOST CELL, but virus can still develop resistance
Term
Raltegravir
Definition
-inhibits viral INTEGRATION into host genome
Term
Interferon Alpha
Definition
-recombinant protein used to fight HEPATITIS B & C
-works by eliciting immune response just like endogenous IFN alpa
-can unmask autoimmune disorders, MYELOSUPPRESSION
Term
Adefovir
Definition
-specific to HEPATITIS B
-competitively inhibits HEP B DNA Polymerase
Term
Entecavir
Definition
Term
Ribavirin
Definition
-Activated by host cell enzyme phosphorylation
-acts against WEST NILE VIRUS, HEP C
-never administered alone--> always with IFN alpha
-highly CI in pregnancy including 6 months after stopping the drug
Term
Amantadine
Definition
act against INFLUENZA A
Term
Oseltamivir
Definition
act against INFLUENZA A
Term
Rimantadine
Definition
act against INFLUENZA A&B
Term
Zanamivir
Definition
-act against INFLUENZA A&B
-CI in kids under 7
Term
Palivizumab
Definition
-binds RSV virus
-given to high risk infants and children
Term
Imiquimod
Definition
stimulates the host immune system...
Term
Antiherpes agents
Definition
• Activated by viral THYMIDINE KINASE (only in infected cells)
• Inhibits viral DNA polymerase-->incorporates to viral DNA stoping chain elongation
-poor bioavailability
-resistance by mutation to thymidine kinase or DNA pol
-Nephro, neuro toxicities, rashes
Term
Anti-CMV agents
Definition
• Activated by viral thymidine kinase (only in infected cells)
• Inhibits viral DNA polymerase-->incorporates to viral DNA stopping chain elongation
-resistance by mutation to thymidine kinase or DNA pol
-can cause MYELOSUPPRESSION, neutropenia, neurotoxicity
Term
Antihepititis agents
Definition
Term
Anti influenza agents
Definition
Term
NRTIs
Definition
• Activated intracellularly by phosphrylation with cellular kinases
•competatively inhibits RT and can get incorporated into HIV DNA
• Mitochondrial toxicity (anemia, lactic acidosis)
Term
NNRTIs
Definition
• Non-competative (allosteric) inhibitors of RT -->DO NOT REQUIRE PHOSPHORYLATION FOR ACTIVATION
• Active only against HIV-1
• Metabolized by Cyp-450
-cause RASHES
Term
Protease Inhibitors
Definition
• Inhibit HIV PROTEASE which interferes with post-translational processing of precursor-->immature HIV copies
-Substrates and metabolized by the Cyp-450 system
○ Ritonavir = potent inhibitor of Cyp 450, taken in combination with PIs
-can cause CUSHINGOID effects
Term
Entry Inhibitors
Definition
Term
Integrase Inhibitors
Definition
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