Introduction to Antiviral
1
Drugs
Learning Outcomes
Be able to describe stages of viral replication
targeted by antivirals
Analyze the mechanism of action of antivirals
Examine the treatment of viral infections
N NYOLOKA
04/13/2025
VIRUSES…
2
04/13/2025
VIRUSES…
3
04/13/2025
VIRUSES…
4
04/13/2025
VIRUSES…
5
04/13/2025
Viral infections
6
The main problem with viral infections is that most
of them are asymptomatic and enormous
variations in:
Viral structure, their epidemiology, pathogenesis
Viral infections can involve any organ of the body
At the stage of producing symptoms, mostly it
means the disease has established itself
Examples common cold, HIV infection, hepatitis C
Most antiviral therapy would target steps in viral
replication
04/13/2025
Viruses…
7
04/13/2025
Check point…
8
How did SARS-CoV-2 evolve?
What’s the treatment for SARS-CoV-2?
04/13/2025
9
Should we say we need treatment for Herpes
viruses, Influenza A & B viruses, Hepatitis B and C,
Papilloma, HIV 1 & 2???
If we do not have drugs for the above, how safe
are we???
04/13/2025
Antivirals mainly three
10
types
Virucidal agents
directly inactivate intact viruses
topical treatment of warts with podophyllin, which
destroys both virus and host tissues
most virucides have no demonstrated therapeutic
value
Antiviral agents
Immunomodulators
04/13/2025
ANTIVIRALS…Anti-
11
Retrovirus???
Classification Anti-
Anti- Herpes
virus
Retrovi
rus HIV Virus
HIV???
gfsssssgfes
PRO 542
PRO 140
CCR5
Anti-Hepatitis Anti-
virus/Nonsele Influenza
ctive antiviral virus
drugs
04/13/2025
Check point…
12
Can you be able to explain the whole replication
process of viruses??
Why are retroviruses unique???
04/13/2025
Major sites of antiviral drug
13
action
04/13/2025
Case study…
14
A 35-year-old woman who recently tested
seropositive for both HIV and hepatitis B virus
surface antigen is referred for evaluation.
She is feeling well overall but reports a 25-pack-
year smoking history. She drinks 3–4 beers per
week and has no known medication allergies.
Only that three days ago she was involved in a
road accident, she sustained several bruises and
some head injuries
04/13/2025
15
Physical examination reveals normal vital signs and
no abnormalities. White blood cell count is 5800
cells/mm 3 with a normal differential, hemoglobin
is 11.8 g/dL, all liver function tests are within
normal limits, CD4 cell count is 278 cells/mm 3 ,
and viral load (HIV RNA) is 110,000 copies/mL.
What other laboratory tests should be ordered?
Which antiretroviral medications would you
recommend?
04/13/2025
Agents to treat Herpes
16
Mainly used are acyclovir, valacyclovir and
famciclovir
Others are penciclovir, foscarnet, brivudin
Valacyclovir and famciclovir have not been fully
evaluated in pediatric patients
04/13/2025
Acyclovir
17
Has clinical activity against HSV 1&2, VZV
Activation is required for it to work
phosphorylation
The first step is done by viral enzymes-thymidine
kinase hence selective activation
Mode of action; inhibition of viral DNA sythesis
Competitive inhibition of herpesvirus DNA polymerase
Binding to viral DNA template as an irreversible complex
Viral DNA chain termination
Incorporation into the viral DNA
04/13/2025
Pharmacokinetics of
18
Acyclovir
Available as topical preparations, oral tablets and
intravenous injection
Oral bioavailability is 15-20%, incomplete
absorption
Widely distributed in tissues and body fluid
CSF concentrations 50% of serum values
Almost 80% would be excreted unchanged in urine
Well tolerated, very few side effects
Nausea, diarrhea and headache
04/13/2025
Comparative
19
Pharmacokinetics
Parameter Acyclovi Valacyclov Penciclovir Famciclo
r ir vir
Bioavalability (%) 13-21 54 5 77
Vd (L/1.73M2) 47 47 112 112
Renal Clearance 250-280 250-280 415-530 415-530
(ml/min/1.73m2)
t1/2 (mean, hours) 3 3 2.2 2.2
Urinary excretion (%) 80 80 50-60 50-60
unchanged
04/13/2025
CMV
20
Cytomegarovirus would be treated using
antiherpes agents even though others are specific
to it
Ganciclovir has become the drug of choice
Recall CMV are common in immunosupression
situations due to activation of latent infection
04/13/2025
CMV
21
Disseminated infection causes end-organ disease;
retinitis, colitis, esophagitis, CNS conditions,
pneumonitis
Foscarnet, valganciclovir and cidofovir can also be
used
04/13/2025
Anti-influenza agents
22
Include Amantadine, Rimantadine, Oseltamivir,
Zanamivir
Selection of the agent above depends on the strain
of the causative agent
For example Amantadine inhibits replication of
influenza A while B is not affected
Resistance seen among the strains is also affecting
the use of these agents
04/13/2025
23
Amantadine might also be used in parkinson’s
disease
The usual dose of amantadine for treatment is
100mg bd 5-7 days, orally
Oseltamivir is one of new agents used for influenza
Its indicated both for prophylaxis, as well as
treatment of influenza A, swine flu, bird flu and
influenza B.
04/13/2025
24
Started at the onset of symptoms, it is the most
effective drug; reduces the severity, duration and
complications of the illness.
Prophylactic use for 5–10 days prevents illness in
contacts of influenza patients.
Dose: therapeutic 75 mg oral BD for 5 days;
prophylactic 75 mg OD
04/13/2025
25
Side effects are nausea and abdominal pain due to
gastric irritation (reduced by taking the drug with
food), headache, weakness, sadness, diarrhoea,
cough and insomnia.
Skin reactions have been reported
04/13/2025
ANTI-HEPATITIS VIRUS
26
Although agents are available now, but Malawi is
still moving at its own pace
In this infection most of the available treatment is
suppressive rather than curative
Interferon alfa (injectable forms) are used
Interferons inhibit many RNA and DNA viruses, but
they are host specific: those produced by another
species have poor activity in man
Lamivudine is also applied
04/13/2025
27
Interferons would also be used in treatment for
hepatitis C
Ribavirin has established its use in HCV
PI’s are being investigated for the use
04/13/2025
Conclusion…
28
Therapies sometimes are imperfect
Regimen complexities
Toxicities
Drug resistance
Viral type
We still need effective anti-HIV therapy
Several possible targets are being studied and tested
The area of anti-HIV drugs has more room for growth
and the future for the discovery of new effective drugs is
promising, coming to an end,,, when???-may be
vaccine?
04/13/2025
29
Any questions about antivirals???
THE END!!!
04/13/2025
