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Antiviral Agents
(Antiherpes Agents, Anti-influenza agents)
-Prajwal Waman Ghatol
Prajwal Ghatol
01.
02.
Viruses are the ultimate expression of
obligate intracellular parasitism. They not
only take nutrition from the host cell but
also direct its metabolic machinery to
synthesize new virus particles. Viral
chemotherapy, therefore was considered
impossible, as it would require interference
with cellular metabolism in the host.
Introduction
However, in the past 50 years virus
directed enzymes have been identified in
the infected cell and some viruses have
few enzymes of their own which may have
higher affinities for some antimetabolites
or inhibitors than the regular cellular
enzymes.
Prajwal Ghatol
In addition, drugs have been developed
which target virus specific steps like cell
penetration, uncoating, reverse
transcription, virus assembly or maturation
and release from host cell, etc.
Introduction
Another stumbling block is that
in majority of acute infections viral
replication is already at its peak when
symptoms appear. To be effective,
therefore, therapy has to be started in the
incubation period, i.e. has to be
prophylactic or preemptive.
03.
04.
Prajwal Ghatol
Classification
Prajwal Ghatol
Antiherpes Agents
They are used for treatment of various herpetic infections.
Prajwal Ghatol
MOA
This deoxiguanosine analogue requires a virus specific
enzyme for conversion to the active metabolite that
inhibits DNA synthesis and viral replication.
Acyclovir is preferentially taken up by the virus infected
cells. Because of selective generation of the active
inhibitor in the virus infected cell and its greater
inhibitory effect on viral DNA synthesis, acyclovir has low
toxicity for host cells: a several hundred-fold
chemotherapeutic index has been noted.
It is a synthetic, purine nucleoside analogue that has antiherpes
activity. It is more effective against HSV-1 and HSV-2 than
varicella zoster virus (VZV) infections.
Acyclovir
Prajwal Ghatol
Pharmacokinetics of Acyclovir
Only about 20% of an oral dose of acyclovir is absorbed. It is little plasma
protein bound and is widely distributed attaining CSF concentration that
is 50% of plasma concentration. After topical application systemic
absorption is negligible, but it penetrates cornea well. Acyclovir is
primarily excreted unchanged in urine, both by glomerular filtration and
tubular secretion; plasma t1⁄2 is 2- 3 hours.
Renal impairment necessitates dose reduction.
It is a highly potent antiherpes drug. It has high therapeutic index with
low toxicity to host cells.
Prajwal Ghatol
Therapeutic Uses of Acyclovir
1. GENITAL HERPES: Oral/intravenous/topical acyclovir is effective in
genital herpes simplex infections. It is used for primary and recurrent
infections; high doses of acyclovir are needed for recurrent infections.
It reduces the frequency and severity of herpetic lesions.
2. HERPETIC ENCEPHALITIS: Intravenous acyclovir is the drug of
choice for encephalitis caused by HSV.
3. Herpes simplex keratitis: Acyclovir is used topically in herpetic
keratoconjunctivitis.
Prajwal Ghatol
4. Mucocutaneous HSV: Acyclovir is used orally or topically in the
treatment of stomatitis, herpes labialis and ulcers in mouth. It is used
intravenously in immunocompromised patients.
5. Herpetic whitlow (nail-bed infection): Oral acyclovir is useful for the
prevention and treatment of whitlow.
6. CHICKENPOX: Acyclovir reduces the duration of illness if started early
in patients at risk of severe illness and immunocompromised
individuals.
7. Herpes zoster: Acyclovir (oral/topical/i.v.) and valacyclovir (oral) are
effective.
Therapeutic Uses of Acyclovir
Prajwal Ghatol
Adverse Effects of
Acyclovir
Acyclovir is usually well tolerated. Nausea, vomiting,
diarrhoea and headache are the other side effects.
High doses may cause neurotoxicity with tremor,
confusion, disorientation and convulsions. On topical
use, it can cause irritation and burning.
Prajwal Ghatol
Prajwal Ghatol
Idoxuridine
Idoxuridine is a thymidine analogue that acts against DNA viruses. It
inhibits viral replication. Idoxuridine is used topically for HSV
keratoconjunctivitis. The adverse effects are local irritation, itching,
pain and swelling of lids.
Valganciclovir
It is a prodrug of ganciclovir. It has better bioavailability than
ganciclovir.
Prajwal Ghatol
The important features of
some of the antiherpetic
agents are given in the
table.
Prajwal Ghatol
Anti-influenza Agents
Prajwal Ghatol
Anti-influenza Agents
Prajwal Ghatol
Anti-influenza Agents
Prajwal Ghatol
Thank you!

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antiviral agents (Antiherpes Agents, Anti-influenza agents) .pptx

  • 1. Antiviral Agents (Antiherpes Agents, Anti-influenza agents) -Prajwal Waman Ghatol Prajwal Ghatol
  • 2. 01. 02. Viruses are the ultimate expression of obligate intracellular parasitism. They not only take nutrition from the host cell but also direct its metabolic machinery to synthesize new virus particles. Viral chemotherapy, therefore was considered impossible, as it would require interference with cellular metabolism in the host. Introduction However, in the past 50 years virus directed enzymes have been identified in the infected cell and some viruses have few enzymes of their own which may have higher affinities for some antimetabolites or inhibitors than the regular cellular enzymes. Prajwal Ghatol
  • 3. In addition, drugs have been developed which target virus specific steps like cell penetration, uncoating, reverse transcription, virus assembly or maturation and release from host cell, etc. Introduction Another stumbling block is that in majority of acute infections viral replication is already at its peak when symptoms appear. To be effective, therefore, therapy has to be started in the incubation period, i.e. has to be prophylactic or preemptive. 03. 04. Prajwal Ghatol
  • 5. Antiherpes Agents They are used for treatment of various herpetic infections. Prajwal Ghatol
  • 6. MOA This deoxiguanosine analogue requires a virus specific enzyme for conversion to the active metabolite that inhibits DNA synthesis and viral replication. Acyclovir is preferentially taken up by the virus infected cells. Because of selective generation of the active inhibitor in the virus infected cell and its greater inhibitory effect on viral DNA synthesis, acyclovir has low toxicity for host cells: a several hundred-fold chemotherapeutic index has been noted. It is a synthetic, purine nucleoside analogue that has antiherpes activity. It is more effective against HSV-1 and HSV-2 than varicella zoster virus (VZV) infections. Acyclovir Prajwal Ghatol
  • 7. Pharmacokinetics of Acyclovir Only about 20% of an oral dose of acyclovir is absorbed. It is little plasma protein bound and is widely distributed attaining CSF concentration that is 50% of plasma concentration. After topical application systemic absorption is negligible, but it penetrates cornea well. Acyclovir is primarily excreted unchanged in urine, both by glomerular filtration and tubular secretion; plasma t1⁄2 is 2- 3 hours. Renal impairment necessitates dose reduction. It is a highly potent antiherpes drug. It has high therapeutic index with low toxicity to host cells. Prajwal Ghatol
  • 8. Therapeutic Uses of Acyclovir 1. GENITAL HERPES: Oral/intravenous/topical acyclovir is effective in genital herpes simplex infections. It is used for primary and recurrent infections; high doses of acyclovir are needed for recurrent infections. It reduces the frequency and severity of herpetic lesions. 2. HERPETIC ENCEPHALITIS: Intravenous acyclovir is the drug of choice for encephalitis caused by HSV. 3. Herpes simplex keratitis: Acyclovir is used topically in herpetic keratoconjunctivitis. Prajwal Ghatol
  • 9. 4. Mucocutaneous HSV: Acyclovir is used orally or topically in the treatment of stomatitis, herpes labialis and ulcers in mouth. It is used intravenously in immunocompromised patients. 5. Herpetic whitlow (nail-bed infection): Oral acyclovir is useful for the prevention and treatment of whitlow. 6. CHICKENPOX: Acyclovir reduces the duration of illness if started early in patients at risk of severe illness and immunocompromised individuals. 7. Herpes zoster: Acyclovir (oral/topical/i.v.) and valacyclovir (oral) are effective. Therapeutic Uses of Acyclovir Prajwal Ghatol
  • 10. Adverse Effects of Acyclovir Acyclovir is usually well tolerated. Nausea, vomiting, diarrhoea and headache are the other side effects. High doses may cause neurotoxicity with tremor, confusion, disorientation and convulsions. On topical use, it can cause irritation and burning. Prajwal Ghatol
  • 12. Idoxuridine Idoxuridine is a thymidine analogue that acts against DNA viruses. It inhibits viral replication. Idoxuridine is used topically for HSV keratoconjunctivitis. The adverse effects are local irritation, itching, pain and swelling of lids. Valganciclovir It is a prodrug of ganciclovir. It has better bioavailability than ganciclovir. Prajwal Ghatol
  • 13. The important features of some of the antiherpetic agents are given in the table. Prajwal Ghatol