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Antiviral Drugs 
Harindu Udapitiya. 
Temporary Lecturer, 
Division Of Pharmacology, 
Department of Oral Medicine & Periodontology.
Overview 
• 1.Introduction to virus and replication. 
• 2.Targets of Antivirals. 
• 3.Antiviral Drugs. 
– Mode of Action 
– Pharmacokinetics 
– Clinical Use 
– Adverse effects
1.Introduction to virus and replication.
Structure of a virus
Viral 
Replication
Targets of Antiviral Drugs 
• 1.Inhibition of penetration & attachment 
to host cells. 
• 2.DNA polymarase inhibitors 
• 3.Reverse Transcriptase inhibitors 
• 4.Protease inhibitors 
• 5.Inhibitors of virus release.
Antiviral Drugs 
• 1.Inhibition of penetration & attachment 
to host cells. 
I. Amantidine 
II. Immunoglobulin 
2.DNA polymarase inhibitors. 
I. Aciclovir 
II. Ganciclovir 
III. Tribavirin
• 3.Reverse Transcriptase inhibitors 
I. Zidovudine 
II. Lamivudine 
• 4.Protease inhibitors 
I. Saquinavir 
II. Ritonavir 
• 5.Inhibitors of virus release. 
I. Oseltamivir 
II. Zanamivir
• 6.Interferones(INF)
• 1.Inhibition of penetration & 
attachment to host cells
Amantidine
• Mode of action 
 Blocks M2 receptors 
• Pharmacokinetics 
 Well absorbed orally 
 T1/2=3h 
 Elimination-renally 
• Adverse Effects 
 Anxiety 
 Insomnia 
 Hallucination
Immunoglobulin
• Contains antibodies which are directed 
against the virus envelope and can 
'neutralise' some viruses and prevent 
their attachment to host cells. 
• Use in, 
– Measles 
– infectious hepatitis 
– German measles 
– Rabies 
– poliomyelitis
• 2.DNA polymarase 
inhibitors.
Aciclovir
• Mechanism of action 
Aciclovir viral thiamidine kinase Aciclovir monophosphate 
DNA polymarase Aciclovir triphosphate 
• Pharmacokinetics 
 Oral,IV,Topical 
 oral BA 10-20% 
 Plasma T1/2-2-3h 
 Distribute 50% to CSF 
 Elimination-Renal
• Adverse Effects 
Reversible nephropathy 
Headache,nausea 
Encephalopathy 
• Clinical Use 
 Varicella zoster-shingells,chikenpox 
 Herpes zoster 
 Prophylactically for immunocompramised patients.
Gangcyclovir 
• MOA 
Same as aciclovir 
• Pharmacokinetics 
 IV,oral 
 T1/2=4h 
 Elimination-renal 
• Adverse Effects 
 Bone marrow suppresion 
 Potential carcinogenicity
• Clinical Use 
– CMV infection
3.Reverse Transcriptase 
inhibitors
Zidovudine 
• Necleoside analog 
• Oral,iv,rectal 
• Oral BA=75% 
• T1/2=05-3h 
• Elimination=renal 
• Use in treatement for HIV infection & as 
post exposure prophylactic.
4.Protease inhibitors
Saquinavir 
• Uses with combination of ritonavir. 
• Oral 
• Protein binding 98% 
• T1/2=9-15 h 
• Use in HIV therapy.
5.Inhibitors of virus release.
Oseltamivir 
• Oral BA=75% 
• Oseltamivr hepatic estarase oseltamivir 
carboxylase 
• Widely distributed through body 
• T1/2=6-10h 
• Elimination=renal 
• Use in Influenza A,B 
• Adverse effects 
– Nausea,vomiting,abdominal pain
Zanamivir 
• Oral,inhalation 
• Oral BA=2% 
• T1/2=2.5-5h 
• Elimination-renal 
• Use in infl A & B 
• Adverse effects 
– Broncospasms 
– Cough
Interferones
• Interferons are a family of inducible 
proteins synthesised by mammalian cells 
• They induce, in host cell ribosomes, the 
production of enzymes that inhibit the 
translation of viral mRNA into viral 
proteins, thus halting viral replication. 
• Wide sprectum of use.
• Iv,Im 
• T1/2=2-4h 
• Clinical use 
Hepatitis B & C 
• Adverse effeccts 
Fever 
Myelgia 
BM suppression 
Rashes
Summery 
• 1.Introduction to virus and replication. 
• 2.Targets of Antivirals. 
• 3.Antiviral Drugs 
– Amantidine 
– Immunoglobulin 
– Aciclovir 
– Gangcyclovir 
– Zidovudine 
– Saqunavir 
– Oseltamivir 
– Zanamivir
• Interferones
Furthur reading… 
1. Viral vaccines 
2. DNA & RNA Viruses 
3. HIV treatment.
Antiviral drugs

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Antiviral drugs

  • 1. Antiviral Drugs Harindu Udapitiya. Temporary Lecturer, Division Of Pharmacology, Department of Oral Medicine & Periodontology.
  • 2.
  • 3.
  • 4. Overview • 1.Introduction to virus and replication. • 2.Targets of Antivirals. • 3.Antiviral Drugs. – Mode of Action – Pharmacokinetics – Clinical Use – Adverse effects
  • 5. 1.Introduction to virus and replication.
  • 8.
  • 9. Targets of Antiviral Drugs • 1.Inhibition of penetration & attachment to host cells. • 2.DNA polymarase inhibitors • 3.Reverse Transcriptase inhibitors • 4.Protease inhibitors • 5.Inhibitors of virus release.
  • 10. Antiviral Drugs • 1.Inhibition of penetration & attachment to host cells. I. Amantidine II. Immunoglobulin 2.DNA polymarase inhibitors. I. Aciclovir II. Ganciclovir III. Tribavirin
  • 11. • 3.Reverse Transcriptase inhibitors I. Zidovudine II. Lamivudine • 4.Protease inhibitors I. Saquinavir II. Ritonavir • 5.Inhibitors of virus release. I. Oseltamivir II. Zanamivir
  • 13. • 1.Inhibition of penetration & attachment to host cells
  • 15. • Mode of action  Blocks M2 receptors • Pharmacokinetics  Well absorbed orally  T1/2=3h  Elimination-renally • Adverse Effects  Anxiety  Insomnia  Hallucination
  • 17. • Contains antibodies which are directed against the virus envelope and can 'neutralise' some viruses and prevent their attachment to host cells. • Use in, – Measles – infectious hepatitis – German measles – Rabies – poliomyelitis
  • 18. • 2.DNA polymarase inhibitors.
  • 20. • Mechanism of action Aciclovir viral thiamidine kinase Aciclovir monophosphate DNA polymarase Aciclovir triphosphate • Pharmacokinetics  Oral,IV,Topical  oral BA 10-20%  Plasma T1/2-2-3h  Distribute 50% to CSF  Elimination-Renal
  • 21. • Adverse Effects Reversible nephropathy Headache,nausea Encephalopathy • Clinical Use  Varicella zoster-shingells,chikenpox  Herpes zoster  Prophylactically for immunocompramised patients.
  • 22. Gangcyclovir • MOA Same as aciclovir • Pharmacokinetics  IV,oral  T1/2=4h  Elimination-renal • Adverse Effects  Bone marrow suppresion  Potential carcinogenicity
  • 23. • Clinical Use – CMV infection
  • 25. Zidovudine • Necleoside analog • Oral,iv,rectal • Oral BA=75% • T1/2=05-3h • Elimination=renal • Use in treatement for HIV infection & as post exposure prophylactic.
  • 27. Saquinavir • Uses with combination of ritonavir. • Oral • Protein binding 98% • T1/2=9-15 h • Use in HIV therapy.
  • 29. Oseltamivir • Oral BA=75% • Oseltamivr hepatic estarase oseltamivir carboxylase • Widely distributed through body • T1/2=6-10h • Elimination=renal • Use in Influenza A,B • Adverse effects – Nausea,vomiting,abdominal pain
  • 30. Zanamivir • Oral,inhalation • Oral BA=2% • T1/2=2.5-5h • Elimination-renal • Use in infl A & B • Adverse effects – Broncospasms – Cough
  • 32. • Interferons are a family of inducible proteins synthesised by mammalian cells • They induce, in host cell ribosomes, the production of enzymes that inhibit the translation of viral mRNA into viral proteins, thus halting viral replication. • Wide sprectum of use.
  • 33. • Iv,Im • T1/2=2-4h • Clinical use Hepatitis B & C • Adverse effeccts Fever Myelgia BM suppression Rashes
  • 34. Summery • 1.Introduction to virus and replication. • 2.Targets of Antivirals. • 3.Antiviral Drugs – Amantidine – Immunoglobulin – Aciclovir – Gangcyclovir – Zidovudine – Saqunavir – Oseltamivir – Zanamivir
  • 36.
  • 37. Furthur reading… 1. Viral vaccines 2. DNA & RNA Viruses 3. HIV treatment.