ANTIVIRUS

Novika Pristiwati
• ANTIVIRUS  agent that kill virus by suppresing and

inhibiting its replication

• According its nucleic acid  RNA & DNA virus

• Intracelluler obligat Paracyte

• To treat  need good understanding of viral cycle cell

ATTACHMENT

PENETRATION HOST
UNCOATING FUNCTIONS

Transcription
Translation
REPLICATION

VIRAL LIFE
ASSEMBLY
CYCLE (MATURATION)

RELEASE

Replication
09/10/2020 5
TOPICAL ANTIVIRAL DRUGS
Idoxurideine, Trifluridine, Vidarabine
Have been used to treat HSV

Structural analogues of Thymidine

Vidarabine is Adenin analogue

Trifluridine  more soluble  can be used in drop form

 good for herpetic keratitis

• Acyclovir is activated by HSV thymidine kinase to inhibit

viral DNA polymerase

• Gancyclovir  activated by triphosphorylation to inhibit

viral DNA polymerase

• Effective for CMV corneal endothelitis and anterior uveitis
SISTEMIC ANTIVIRAL DRUGS
• ACYCLOVIR
• VALACYCLOVIR
• FAMCYCLOVIR
• GANCICLOVIR
• VALGANCICLOVIR
• FOSCARNET
• CIDOFOVIR
• ZIDOVUDINE
ACYCLOVIR
• Synthetic guanosine analogue  requires

phosphorylation by viral thymidinase to become active

• Acyclovir monophosphate  acyclovir triphosphate 

cant not cross cell membranes and accumulate further

• Resistent in HIV patients that already have multiple

therapy
 Vidarabine & Foscarnet
• Oral  bioavailibility: 15-30%

• Food doesn’t affect absorption

• Well distributed  CSF, HA

• Concentration of acyclovir in Zooster vesicle fluid = in

plasma
• Effective in preventing the recurrence of HSV epithelial

and stromal keratitis

• IV  renal toxicity & neurotoxicity
VALACYCLOVIR
• HZV infection in immunocompetent patient

• Bioavalibility  >> acyclovir

• in immunocompromise patient  nephrotoxic and

trombocytopenia
FAMCYCLOVIR
• Prodrug of pencyclovir

• Uncomplicated acute HZV

• Relieving acute Zooster signs and symptomps , reducing

the duration of postherpetic neuralgia when administered

during acute phase
GANCYCLOVIR
• Synthetic guanosine analogue

• Herpesvirus, CMV retinitis and CMV prophylaxis in

patients with advanced HIV infection & transplant patient

• Become active through Phosphorilation  inhibit viral

DNA polymerase
• CMV retintis  implant intraoculer
• Primarily used as IV, ,5% absorbed in oral

• Half life  3-4 hours ; eksretion  urin

• Adverse effect  bone marrow suppresion

• Oral regiment can be given after CMV retinitis is

undercontrolled with IV
• Intravitreal  sustained released introcular device
VALGANCYCLOVIR
• Prodrug Gancyclovir
• Converted to Gancyclovir by intestinal and hepatic
esterase
FOSCARNET
• Phosphonormic acid

• Inhibit DNA, RNA polymerase and reverse trancriptase

• Treatment of CMV retinitis in HIV and mucocutaneous

HSV that resistent with acyclovir in immunocompromised

patient
• Inhibit Pyrophosphate in CMV DNA polymerase
• Inhibits herpesviruses that esistent to acyclovir

/gancyclovir
• IV  renal impairment !!  adequate hydration

• Bioavailibility 20% ; binding with Ca

• Deposited in bone  detectable after months

• Eksretion  urin

• Adverse effect  Hypocalcemia, Nephrotoxic

CIDOFOVIR
• Cytidine nucleoside analogue

• Herpsvirus, poxvirus, polyomavirus, papillomavirus and

adenovirus
• Mechanism of action  inhibit DNA synthesis

• Prolonged half life  1x/week

• Renal toxic  adequate hydration and probenecid hig dose

( pre and post treatment )

• Adverse effect  uveitis and irreversible hypotony

• CMV retinitis  intravitreal

• 2nd line therapy for complication after smallpox vaccination

ZIDOVUDINE
• Thymidine nucleoside analogue

• Used in HIV

• Zidovudine phosphorylated to phosphat forms by celluler kinase

in inefcted? Uninfected cells

• 2 primary method of action

- Triphosphate acts as competitive inhibitor of viral reverse

transcriptase

- Azido groups prevents further chain elongation  acts as

DNA chain terminator
BIBLIOGRAPHY
• American Academy od Ophtalmology.BCSC

Fundamentals and Principles of Ophtalmology.San

Fransisco: American Academy of Ophtalmology, 2014-
2015. 356-361p
TERIMAKASIH
MOHON BIMBINAN DAN SARAN