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Dr.Reshmi.T.R
ANTIVIRAL DRUGS
VIRUS
 Structure
 Genome: RNA/DNA/neverBoth
 Capsid: Protein shell
 Envelope: Lipoprotein
Structure of a virus
Envelope
Capsid
DNA/RNA
3
CLASSIFICATION
DNA virus
 Hepatitis B
 Herpes virus
HSV-1,HSV-2
VZV
EBV
CMV
 Poxvirus(Molluscum)
 Parvovirus(Erythema
...
Viral replication
Attachment Entry Uncoating
Synthesis of
viral
RNA/DNA
Synthesis of
structural
proteins
Assembly Release
DNA VIRUS REPLICATION
DNA polymerase
Entry into nucleus
Attachment
Uncoating
Release of virions
Viral
proteins
RNA VIRUS REPLICATION
CLASSIFICATION
Antivirals
DNA Polymerase
inhibitors
mRNA inhibitors
Inhibitors of viral
penetration and uncoating
Release ...
ANTIVIRALS AND
DNA VIRUS
Docosanol (HSV)
1) INHIBITION OF ATTACHMENT
Aliphatic alcohol
Topical – 10% cream
Use – Herpes labialis
IIn
DNAP
Inhibitors
DNA POLYMERASE INHIBITORS
Acyclovir
Valacyclovir
Ganciclovir
Valganciclovir
Famciclovir
Penciclovir
Adefovir
Cidofovir
Entecavir
Vidarabin...
MONOPHOSPHATE
TRIPHOSPHATE
DIPHOSPHATE
ACYCLOVIR
PENCYCLOVIR
GANCICLOVIR
CIDOFOVIR
FOSCARNET
INHIBITION OF VIRAL DNA POLYM...
PK
 BA – 10-30%
 Wide distribution, crosses BBB
 Half life – 2-3hrs
 Renal excretion-dose reduction
ACYCLOVIR &VALACYC...
SPECTRUM AND USE
 HSV-1: Herpes labialis, esophagitis, keratitis ,encephalitis,
Ocular herpes
 HSV-2: Genital herpes,VZV...
ROA
 HSV-1,HSV-2,VZV:Oral
 400mg tds
 Encephalitis:Parenteral
 Genital ,Ocular Herpes:Topical
ADR
 I.V- rash, sweating, emesis, hypotension, CNS effects, renal
insufficiency, phlebitis on extravasation
 Topical-sti...
VALACYCLOVIR
 L-valyl ester prodrug of acyclovir
 BA more than acyclovir
 Less frequent dosing
 No IV preparation
 Us...
Penciclovir
Topical cream
Persist in infected
cell for long time
Half life -8to20 hrs
Use:Herpes
Labialis
Famciclovi...
GANCICLOVIR AND VALGANCICLOVIR
 Selective action to CMV Infections
 Accumulate in vitreous humor
 CMV retinitis
Poor or...
ADVERSE EFFECTS
 Myelosuppression
Anemia,neutropenia,thrombocytopenia
 Fever
 Phlebitis
VALGANCICLOVIR
 Prodrug of Ganciclovir
 Well absorbed orally
 Oral valganciclovirCMV Retinitis:900 mg BD
CIDOFOVIR
 Poor oral bioavailability
Topical, IV
 Phosphorylated by cellular but not viral enzymes
Acyclovir resistant...
 MOA:No phosphorylation required to inhibit DNAP
 Thymidine kinase mutation not a threat
 Use:Mucocutaneous HSV ,CMV re...
Idoxuridine
 Ophthalmic use:HSV
infection
 Trifluridine
 HSV-1 ,HSV-2,CMV
 Ophthalmic use
 AE: Hyperemia
 Adefovir
 Use:chronic HBV
 AE:Nephrotoxicity
 Telbivudine
 Use:Chronic HBV
 AE:Headche,vomiting
mRNA synthesis
inhibitors
MRNA SYNHTHESIS INHIBITORS
Fomivirsen
Selective accumulation in vitreous
Use: CMV retinitis
AE: ...
 InterferonsDefence against viral infections:
Immunomodulator
 Inhibit viral replication at multiple steps:
1 Penetrati...
 Uses:
 Interferon alpha2a:
 Chronic hepatitis B,Kaposi’s sarcoma,Chronic Hepatitis C
 Interferon alpha2b
 HepatitisC...
RNA VIRUS
1) ATTACHMENT AND ENTRY
Palivuzumab
Humanized monoclonal antibody
Use: RSV
AE: Fever,Rhinitis,Diarrhoea
2)INHIBITION OF UNCOATING
Uncoating inhibited by
AMANTADINE
RIMANTIDINEResistance:
M2 protein mutation
AMANTADINE ,RIMANTADINE
 Rimantadinealpha methyl ester of amantadine
 Amantadine is excreted in urine ,Rimantidinelive...
MRNA INHIBITORS
RIBAVIRIN
Broad spectrum
Inhibit RNA and DNA virus
Use: Influenza,HCV
AE: Respiratory distress,hypotension...
Release of virions
Viral
proteins
NEURAMINIDASE INHIBITORS
(INHIBITION OF VIRAL RELEASE)
Neuraminidase
inhibitors
Oseltamivir
Zanamivir
Peramivir
NEURAMINIDASE INHIBITORS
Influenza A,B
Oseltamivir Zanamivir
MOA Neuraminidase inhibitor Neuraminidase inhibitor
ROA Oral Intranasal
ROE Renal Renal
AE Gastroint...
 Recent drug
Use:
Emergency treatment of H1N1
Only IV option for swine flu
PERAMIVIR
ANTIHERPES DRUGS
HSV-1 Herpes Labialis
Ocular Herpes ,
Herpes encephalitis
HSV-2
Genital herpes
VZV
Chickenpox
Shingles
AGENTS TO TREAT-HSV...
Drug ROA USE
Acyclovir
Valacyclovir (No IV)
Oral
Topical
IV
Genital herpes
Orolabial herpes
Herpes Encephalitis
Varicella
...
AGENTS TO TREAT CMV
Agent Route Use
Ganciclovir Oral
IV
Intraocular implant
CMV retinitis
Treatment and prophylaxis
Valganciclovir Oral CMV Re...
AGENTS TO TREAT
HEPATITIS
Agent Indication Route
Lamivudine Chronic hepatitis B Oral
Adefovir
Chronic hepatitis B
Oral
Entecavir Chronic hepatitis B...
Agent Indication Route
Lamivudine Chronic hepatitis B Oral
Adefovir
Chronic hepatitis B
Oral
Entecavir Chronic hepatitis B...
ANTIINFLUENZA VIRUS
Agent Route Mechanism Use
Oseltamivir Oral Neuraminidase inhibitor Influenza A ,B
Zanamivir Inhalation Neuraminidase inhib...
Antiviral drugs
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Antiviral drugs

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Antiviral drugs

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Antiviral drugs

  1. 1. Dr.Reshmi.T.R ANTIVIRAL DRUGS
  2. 2. VIRUS  Structure  Genome: RNA/DNA/neverBoth  Capsid: Protein shell  Envelope: Lipoprotein
  3. 3. Structure of a virus Envelope Capsid DNA/RNA 3
  4. 4. CLASSIFICATION DNA virus  Hepatitis B  Herpes virus HSV-1,HSV-2 VZV EBV CMV  Poxvirus(Molluscum)  Parvovirus(Erythema infectiosum)  Papilloma virus(Warts) RNA Virus  Influenza  Hepatitis A,C,D,E  Enterovirus  Mumps  Measles
  5. 5. Viral replication Attachment Entry Uncoating Synthesis of viral RNA/DNA Synthesis of structural proteins Assembly Release
  6. 6. DNA VIRUS REPLICATION DNA polymerase Entry into nucleus Attachment Uncoating
  7. 7. Release of virions Viral proteins RNA VIRUS REPLICATION
  8. 8. CLASSIFICATION Antivirals DNA Polymerase inhibitors mRNA inhibitors Inhibitors of viral penetration and uncoating Release inhibitors Immunomodulators Docosanol, Amantadine Palivizumab Ribavirin, Fomivirsen Neuraminidase inhibitors Interferons Acyclovir, Ganciclovir
  9. 9. ANTIVIRALS AND DNA VIRUS
  10. 10. Docosanol (HSV) 1) INHIBITION OF ATTACHMENT Aliphatic alcohol Topical – 10% cream Use – Herpes labialis
  11. 11. IIn DNAP Inhibitors DNA POLYMERASE INHIBITORS
  12. 12. Acyclovir Valacyclovir Ganciclovir Valganciclovir Famciclovir Penciclovir Adefovir Cidofovir Entecavir Vidarabine Idoxuridine Trifluridine Telbivudine Foscarnet DNA POLYMERASE INHIBITORS
  13. 13. MONOPHOSPHATE TRIPHOSPHATE DIPHOSPHATE ACYCLOVIR PENCYCLOVIR GANCICLOVIR CIDOFOVIR FOSCARNET INHIBITION OF VIRAL DNA POLYMERASE INHIBITION OF VIRAL DNA SYNTHESIS VIRAL KINASE HOST KINASES HOST KINASES
  14. 14. PK  BA – 10-30%  Wide distribution, crosses BBB  Half life – 2-3hrs  Renal excretion-dose reduction ACYCLOVIR &VALACYCLOVIR
  15. 15. SPECTRUM AND USE  HSV-1: Herpes labialis, esophagitis, keratitis ,encephalitis, Ocular herpes  HSV-2: Genital herpes,VZV  EBV,CMV: Weak action HSV-1>HSV-2>CMV>EBV
  16. 16. ROA  HSV-1,HSV-2,VZV:Oral  400mg tds  Encephalitis:Parenteral  Genital ,Ocular Herpes:Topical
  17. 17. ADR  I.V- rash, sweating, emesis, hypotension, CNS effects, renal insufficiency, phlebitis on extravasation  Topical-stinging, burning  Oral-head ache, nausea, malaise
  18. 18. VALACYCLOVIR  L-valyl ester prodrug of acyclovir  BA more than acyclovir  Less frequent dosing  No IV preparation  Use:  VZV, Recurrent genital herpes  Dose:1g BD/TDS 7 days
  19. 19. Penciclovir Topical cream Persist in infected cell for long time Half life -8to20 hrs Use:Herpes Labialis Famciclovir Prodrug of penciclovir Excreted in urine Use:VZV
  20. 20. GANCICLOVIR AND VALGANCICLOVIR  Selective action to CMV Infections  Accumulate in vitreous humor  CMV retinitis Poor oral Bioavailability  ROA:  IV  Oral  Intraocular implant
  21. 21. ADVERSE EFFECTS  Myelosuppression Anemia,neutropenia,thrombocytopenia  Fever  Phlebitis
  22. 22. VALGANCICLOVIR  Prodrug of Ganciclovir  Well absorbed orally  Oral valganciclovirCMV Retinitis:900 mg BD
  23. 23. CIDOFOVIR  Poor oral bioavailability Topical, IV  Phosphorylated by cellular but not viral enzymes Acyclovir resistant cases Use:CMV Retinitis,HSV mucocutaneous lesion  AE:Nephrotoxicity,Uveitis
  24. 24.  MOA:No phosphorylation required to inhibit DNAP  Thymidine kinase mutation not a threat  Use:Mucocutaneous HSV ,CMV retinitis  ROA:IV  Dose: Induction:90mg/kg IV Q12h Maintenance:90 mg/kg/day FOSCARNET
  25. 25. Idoxuridine  Ophthalmic use:HSV infection  Trifluridine  HSV-1 ,HSV-2,CMV  Ophthalmic use  AE: Hyperemia
  26. 26.  Adefovir  Use:chronic HBV  AE:Nephrotoxicity  Telbivudine  Use:Chronic HBV  AE:Headche,vomiting
  27. 27. mRNA synthesis inhibitors MRNA SYNHTHESIS INHIBITORS Fomivirsen Selective accumulation in vitreous Use: CMV retinitis AE: Iritis,Vitreitis
  28. 28.  InterferonsDefence against viral infections: Immunomodulator  Inhibit viral replication at multiple steps: 1 Penetration 2 Uncoating 3 mRNA synthesis 4 Assembly 5 Release DNA and RNA viruses are sensitive to interferons 2) INHIBITION OF REPLICATION BY INTERFERONS
  29. 29.  Uses:  Interferon alpha2a:  Chronic hepatitis B,Kaposi’s sarcoma,Chronic Hepatitis C  Interferon alpha2b  HepatitisC,Chronic hepatitis B,Condyloma acuminata  Adverse effects:  Myalgia.fever,rash  Alopecia,Bone marrow suppression(long term) INTERFERONS
  30. 30. RNA VIRUS
  31. 31. 1) ATTACHMENT AND ENTRY Palivuzumab Humanized monoclonal antibody Use: RSV AE: Fever,Rhinitis,Diarrhoea
  32. 32. 2)INHIBITION OF UNCOATING Uncoating inhibited by AMANTADINE RIMANTIDINEResistance: M2 protein mutation
  33. 33. AMANTADINE ,RIMANTADINE  Rimantadinealpha methyl ester of amantadine  Amantadine is excreted in urine ,Rimantidineliver  ROA:Oral,100mg BD  Rapidly absorbed from GIT  Use: Treatment of Influenza  Additional use of Amnatidine:Parkinson’s Disease InfluenzaA >Influenza B
  34. 34. MRNA INHIBITORS RIBAVIRIN Broad spectrum Inhibit RNA and DNA virus Use: Influenza,HCV AE: Respiratory distress,hypotension Resistance: Uncommon
  35. 35. Release of virions Viral proteins NEURAMINIDASE INHIBITORS (INHIBITION OF VIRAL RELEASE) Neuraminidase inhibitors
  36. 36. Oseltamivir Zanamivir Peramivir NEURAMINIDASE INHIBITORS Influenza A,B
  37. 37. Oseltamivir Zanamivir MOA Neuraminidase inhibitor Neuraminidase inhibitor ROA Oral Intranasal ROE Renal Renal AE Gastrointestinal Bronchospasm Dose 75 mg BD for treatment 75mg OD fror prophylaxis 10mg BD inhalation
  38. 38.  Recent drug Use: Emergency treatment of H1N1 Only IV option for swine flu PERAMIVIR
  39. 39. ANTIHERPES DRUGS
  40. 40. HSV-1 Herpes Labialis Ocular Herpes , Herpes encephalitis HSV-2 Genital herpes VZV Chickenpox Shingles AGENTS TO TREAT-HSV,VZV INFECTIONS
  41. 41. Drug ROA USE Acyclovir Valacyclovir (No IV) Oral Topical IV Genital herpes Orolabial herpes Herpes Encephalitis Varicella Zoster Famciclovir Oral Genital herpes Orolabial herpes Zoster Foscarnet IV Acyclovir resistant HSV,VZV Docosanol Topical Recurrent herpes labialis Penciclovir Topical Herpes labialis Herpes Genitalis Trifluridine Topical Acyclovir resistant HSV
  42. 42. AGENTS TO TREAT CMV
  43. 43. Agent Route Use Ganciclovir Oral IV Intraocular implant CMV retinitis Treatment and prophylaxis Valganciclovir Oral CMV Retinitis Treatment and prophylaxis Foscarnet IV CMV retinitis treatment Cidofovir IV CMV retinitis treatment
  44. 44. AGENTS TO TREAT HEPATITIS
  45. 45. Agent Indication Route Lamivudine Chronic hepatitis B Oral Adefovir Chronic hepatitis B Oral Entecavir Chronic hepatitis B Oral Tenofovir Chronic hepatitis B Oral Telbivudine Chronic hepatitis B Oral Interferon alpha Chronic Hepatitis B S/C Interferon alpha +Ribavirin Chronic hepatitis C S/C
  46. 46. Agent Indication Route Lamivudine Chronic hepatitis B Oral Adefovir Chronic hepatitis B Oral Entecavir Chronic hepatitis B Oral Tenofovir Chronic hepatitis B Oral Telbivudine Chronic hepatitis B Oral Interferon alpha Chronic Hepatitis B S/C Interferon alpha +Ribavirin Chronic hepatitis C S/C
  47. 47. ANTIINFLUENZA VIRUS
  48. 48. Agent Route Mechanism Use Oseltamivir Oral Neuraminidase inhibitor Influenza A ,B Zanamivir Inhalation Neuraminidase inhibitor Influenza A,B Peramivir IV Neuraminidase inhibitor H1N1 Amantadine Oral Inhibtor of penetration Influenza A>B Rimantidine oral Inhibitor of penetration Influenza A>B Ribavirin Oral IV Aerosol mRNA inhibitor Influenza A,B RSV

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