ANTIVIRAL

AGENTS
Antiviral Agents :
Antiviral agents are drugs approved by the Food and
Drug Administration (FDA) for the treatment or
control of viral infections. Available antiviral agents
mainly target stages in the viral life cycle. The target
stages in the viral life cycle are; viral attachment to
host cell, uncoating, synthesis of viral mRNA,
translation of mRNA, replication of viral RNA and
DNA, maturation of new viral proteins, budding,
release of newly synthesized virus, and free virus in
body fluids. At least half of available antiviral agents
are for the treatment of human immunodeficiency
virus (HIV) infections. The others are used mainly
for the management of herpesviruses, hepatitis B
virus (HBV), hepatitis C virus (HCV), and
respiratory viruses.
Antiviral agents can be used for prophylaxis,
suppression, preemptive therapy, or treatment of
overt disease. Two important factors that can limit
the utility of antiviral drugs are toxicity and the
development of resistance to the antiviral agent by
the virus. In addition, host phenotypic behaviors
toward antiviral drugs because of either genomic or
epigenetic factors could limit the efficacy of an
antiviral agent in an individual.
Life cycle :

The process of viral infection can be sequenced in

seven stages:
1. Adsorption, attachment7 of the virus to specific
receptors on the surface of the host cells, a specific
recognition process.
2. Entry, penetration7 of the virus into the cell.
3. Uncoating, release7 of viral nucleic acid from the
protein coat.
4. Transcription, production of viral mRNA from the
viralgenome.8
5. Translation, synthesis8 of viral proteins (coat
proteins and enzymes for replication) and viral
nucleic acid (i.e., the parental genome or
complimentary strand). This process uses the host
cell processes to express viral genes, resulting in a
few or many viral proteins involved in the
replication process. The viral proteins modify the9
host cell and allow the viral genome to replicate by
using host and viral enzymes. The mechanisms by
which this occurs are complex. This is often the
stage at which the cell is irreversibly modified and
eventually killed.
6. Assembly of the viral particle. New viral coat
proteins assemble into capsids (the protein
envelope that surrounds nucleic acid and associated
molecules in the core) and viral genomes.8
7. Release of the mature virus from the cell by
budding from the cell membrane or rupture of the
cell and repeat of the process, from cell to cell or
individual to individual.8 Enveloped viruses typically
use budding on the plasma membrane,
endoplasmic reticulum, or Golgi membranes. Non
enveloped viruses typically escape by rupture of the
host cell.
Sr no. 1 2
Name of Amantadine Rimantadine
drug
IUPAC Amantan-1-amine 1-(adamantanyl)ethanamine
Name
Generic Amantadine Rimantadine
name
Structur
e

MOA They have two mechanisms : (a) they inhibit an Note : Same as amantadine
early step in viral replication, most likely viral
 uncoating.
(b) in some strains,  they affect the later step
that probably involves viral assembly, possibly
by interfering with hemaglobinin processing.
(c) Additionally by blocking viral
transmembrane ion channel protein (M2) viral
replication may be affected.
(d) The amantadine type drugs inhibit
penetration of the virus into the host cell.
SAR
Synthesi
s

Use
Amantadine oral capsule is used to
treat a variety of movement disorders
caused by Parkinson’s disease. It
can also be used to treat movement
disorders caused by certain drugs
(drug-induced movement disorders).
In addition, this drug is used to
prevent and treat influenza A virus
infection. Amantadine is not a
substitute for annual flu shots.
When used to treat Parkinson’s
disease, this drug may be used as
part of a combination therapy. This
means you may need to take it with
other medications.
Rimantadine is approved in the United
States for prevention and treatment of
influenza type A virus
infections. Seasonal prophylaxis with
either drug is about 70% to 90%
protective27 against influenza type A.
The drugs have no effect on influenza
type B. The primary side effects are
related to the central nervous system
and are dopaminergic. This is not
surprising, because amantadine is used
in the treatment of Parkinson disease.
Rimantadine has significantly fewer
side effects, probably because of its
extensive biotransformation. Less than
50% of a dose of rimantadine is
excreted unchanged, and more than
20% appears in the urine as
metabolites.28 Amantadine is excreted
largely unchanged in the urine.

Adverse CNS effects. Nervousness, insomnia, dizziness, It is reported that the adverse effects
reaction headaches, and fatigue are the most common are much less with rimantadine than
s reported. with amantadine and normal consist of
minor GI effects and dose-related.
 CNS effects. Nervousness, insomnia,
dizziness, headaches, and fatigue are
the most common reported.

Sr. no. 3
Drug Oseltamvir
name
IUPAC ethyl (3R,4R,5S)-5-amino-4 acetamido-3-(pentan-3-yloxy)-cyclohex-1-ene-1-
name carboxylate
Generic Oseltamvir
name
Structure

MOA  Oseltamivir is a neuraminidase inhibitor, a competitive inhibito of

influenza's neraminidase enzyme.
  The enzyme cleaves the sialic cid, which is found on glycoproteins on the
surface of human cells that helps new virions to exit the cell.
 Thus oseltamivir prevents new viral particles from being released.
Synthesi
s

Use It is used to treat symptoms caused by the flu virus (influenza). It helps

make the symptoms (such as stuffy nose, cough, soar throat,
fever/chills, aches, tiredness) less severe and shortens the recovery time
by 1-2 days.
This medication may also be used to prevent the if you have been
exposed to someone who already has the flu (such as a sick household
member) or if there is a flu outbreak in the community.
Talk to your doctor for more details.This medication works by stopping
the flu virus from growing. It is not a substitute for the flu vaccine. (See
also Notes section
Adverse
effects Common oseltamivir side effects may include:

 nausea, vomiting;
 headache; or
 pain.
Sr. No. 4 5
Drug Zanamvir Acyclovir
name
IUPAC (2R,3R,4S)-4-guanidino-3-(prop-1-en-2- 2-Amino-1,9-dihydro-9-((2-
name ylamino)-2-((1R,2R)-1,2,3 hydroxyethoxy)methyl)-3H-purin-6-one
trihydroxypropyl)-3,4-dihydro-2H-pyran-
6-carboxylic acid
Generi Relenza Brand name- Zovirax
c
name
Struct
ure
MOA Zanamivir works by binding to
the active site of
the neuraminidase protein, rendering
the influenza virus unable to escape its
host cell and infect others.
 It is also an inhibitor of influenza virus
replication in vitro and in vivo.
Synthe
sis
Use Zanamivir is used for the treatment of
infections caused by influenza A and
influenza B viruses, but in otherwise-
healthy individuals, benefits overall
appear to be small.
It decreases the risk of one's getting
symptomatic, but not asymptomatic
influenza.
Aciclovir is converted by viral thymidine
kinase to aciclovir monophosphate, which is
then converted by host cell kinases to
aciclovir triphosphate (ACV-TP). ACV-TP, in
turn, competitively inhibits and inactivates
HSV-specified DNA polymerases preventing
further viral DNA synthesis without
affecting the normal cellular processes.
Aciclovir is used for the treatment
of herpes simplex virus (HSV)
and varicella zoster virus infections,
including:[2][14][15]
 Genital herpes simplex (treatment
and prevention)
 Neonatal herpes simplex
 Herpes simplex labialis (cold sores)
 Shingles

Advers Zanamivir is not recommended for use in
e patients with underlying airway disease,
effects which includes asthma or chronic
obstructive pulmonary disease.
Potentially hazardous bronchospasm has
been
reported which may require
hospitalization. Peramivir may cause rare
but serious skin
hypersensitivity reactions.
 Acute chickenpox in immunocompromi
sed patients
 Herpes simplex encephalitis
 Acute mucocutaneous HSV infections
in immunocompromised patients
 Herpes of the eye and herpes
simplex blepharitis (a chronic (long-
term) form of herpes eye infection)
 Prevention of herpes viruses in
immunocompromised people (such as
people undergoing cancer
chemotherapy)[
Acyclovir: renal insufficiency and nephrotoxicity
being the most serious
although reversible and possibly associated
with other complicating conditions.
CNS effects
have also been reported including somnolence.