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Biopharm - Midterm

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Anti-viral drugs: classification, pharmacokinetics, drug action, clinical

use, toxicity, side effects.


Classifications:
2 categories :
- Non-retroviral drugs
+ Anti-herpes virus agent
Acylovir, Idoxuridine, Foscamet , Valgancyclovir…
+ Anti-influenza virus agent
Amantadine, Oseltamivir, Peramivir,Zanamivir…
+ Anti-hepatitis virus agent
For hepatitis B: Lamivudine,Tenofovir
For hepatitis C : Ribavirin, Interferon
-Anti-retroviral drug
+ Nucleoside reverse transcriptase inhibitors(NRTls
+ Non-nucseotide reverse transcriptase inhibitors ( NNRTIs)
+ Protea

https://www.encyclopedia.com/medicine/drugs/pharmacology/
antiviral-drug
https://www.slideshare.net/lukelightning/introduction-to-
pharmacology-and-drug-metabolism
https://www.slideshare.net/arijabuhaniyeh/pharmacology-antivirals
https://www.hiv.uw.edu/go/antiretroviral-therapy/drug-drug-
interactions/core-concept/all
https://nurseslabs.com/antiviral-drugs/#Pharmacokinetics
https://slideplayer.com/slide/7468786/
https://www.slideshare.net/drdhriti/antiviral-drugs-drdhriti
https://slideplayer.com/slide/9835964/
http://tmedweb.tulane.edu/pharmwiki/lib/exe/fetch.php/mondalanti-
viral_drugs_f09.pdf

What is anti-viral?
Definition:
Viral:
 the smallest of all the microbes
only alive and able to multiply inside the cells of other living things
made up of a core of genetic material, either DNA or RNA, surrounded by a
protective coat called a capsid which is made up of protein
uses the host cell’s machinery to replicate its own genetic material

CƠ chế virus
stages during viral infection : sldie 16
•Attachment
•Penetration and uncoating
reverse transcription of viral RNA into
DNA
Integration of the viral DNA into the host cell
genome
Synthesis and assembly of nucleocapsids
Virion release
Anitiviral:
Antivirals complement vaccines in combating virus infection.
They may have a role in prophylaxis (in addition to vaccines) to prevent infection as well
as therapeutically to treat disease.
Antivirals are usually selective inhibitors of virus-specific processes which interfere with
virus replication and either prevent or reduce infection.
They include a spectrum of agents, from small molecules (e.g. amantadine), to peptides,
to antibodies (e.g. palivizumab).
https://isirv.org/site/index.php/antiviral-overview
Strategies for Antiviral Drug Development
• inhibition of virus adsorption
• inhibition of virus-cell fusion
• inhibition of the HIV integrase (HIV)
• inhibition of viral DNA or RNA synthesis
– inhibitors of viral DNA polymerase
– inhibitors of the reverse transcriptase
– acyclic nucleoside phosphonates
• viral protease inhibition
• viral neuraminidase inhibition (influenza)
• inhibition of IMP dehydrogenase
• inhibition of S-adenosylhomocysteine hydrolase
Non-nucleoside reverse transcriptase inhibitors
•must be hydrophobic
•bind to an allosteric binding site that is adjacent to the
substrate (nucleoside)
binding site.
•binding locks the adjacent substrate binding site into an
inactive conformation.
•improved specificity for reverse transcriptase over DNA
polymerases resulting in
less toxicity
•unfortunately, rapid resistance is developed
Inhibitors of viral DNA or
RNA synthesis
DNA viruses: First step is
replication of viral DNA. Inhibitors
of the latter are nucleoside
analogues. These are sufficiently
similar to the “normal”
nucleosides, so that they can
serve as substrates for the viral
DNA polymerases. Since the
sugar lacks the 3’ hydroxyl group
they act as chain terminators:
he drugs are prodrugs, that can only be
converted into the
phosphorylated forms by the viral thymidine kinase
and hence do
not interfere with DNA synthesis in non-infected
cells:

https://vnras.com/thuoc-khang-virus/
http://library.um.edu.mo/ebooks/b28113421.pdf
https://www.virology.ws/wp-content/uploads/
2012/03/020_W3310_16.pdf
http://tmedweb.tulane.edu/pharmwiki/lib/exe/fetch.php/mondalanti-
viral_drugs_f09.pdf
https://pubs.rsc.org/en/content/articlehtml/2015/np/c4np00085d
Non‐nucleoside reverse transcriptase inhibitors
• Bind directly to a site on the viral reverse transcriptase that
is near to but distinct from the binding site of the NRTIs. • Neither
compete with nucleoside triphosphates nor require phosphorylation to
be active. • The binding to the enzyme’s active site results in
blockade of RNA‐ and DNA‐dependent DNA polymerase activities.
https://www.sciencedirect.com/topics/neuroscience/non-nucleoside-
reverse-transcriptase-inhibitors
NRTI
https://www.drugs.com/drug-class/nrtis.html

Side effect
https://www.nhsborders.scot.nhs.uk/media/209209/Antiviral-
medication-June-2014.pdf
https://www.slideshare.net/saminathankayarohanam/7antiviral-
drugs-51480845
https://gmch.gov.in/e-study/e%20lectures/pharmacology/ANTI
%20VIRAL%20DRUGS.pdf

http://www.columbia.edu/itc/hs/medical/pathophys/id/2005/MID40-
HammerAntiviralsColor.pdf
http://library.um.edu.mo/ebooks/b28113421.pdf
https://www.virology.ws/wp-content/uploads/
2012/03/020_W3310_16.pdf
http://tmedweb.tulane.edu/pharmwiki/lib/exe/fetch.php/mondalanti-
viral_drugs_f09.pdf
https://www.drugs.com/drug-class/nrtis.html
toxicity
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC375312/
https://gmch.gov.in/e-study/e%20lectures/pharmacology/ANTI
%20VIRAL%20DRUGS.pdf
https://www.epizone-eu.net/en/Home/show/FAQ-Antivirals.htm
https://www.sciencedirect.com/topics/neuroscience/antivirals

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