Antiviral

Drugs

DR MUHAMMAD SADIQ GUL

Virus
 Smallest living unit
 Nutrition from host
 Difficult to diagnose
 Difficult to treat
 Types of Viruses
DNA Viruses RNA Viruses
 He r p e s group Picorna viruses
Herpes Simplex Virus
Measles
Herpes Zoster Virus
Cytomegalo Virus Mumps
 Ad e n o v i r u s e s Rubella
Va r i o l a & Va c c i n i a
Human papilloma virus
Life Cycle
 Adsorption
 Entry
 Uncoating
 Transcription
 Virus component synthesis
 Antiviral Drugs
• Antiviral drugs are a class of medication used
specifically for treating viral infections.
• Like antibiotics for bacteria, specific antivirals
are used for specific viruses.
• Unlike most antibiotics, antiviral drugs do not
destroy their target pathogen; instead they
inhibit their development.
 Anti Viral drugs

1 st Generation Drugs 2 n d Generation Drugs

 Acyclovir
 Idoxuridine  Famciclovir
 Vidarabine  Ganciclovir
 Cytarabine  Vabaciclovir
 Trifluorothymidine
 Foscarnet
 Bromo vinyl deoxyuridine
 Interferon
ACTION SITE
 ANTIVIRAL DRUGS
• These are more often used locally in the eye.
• Currently available antiviral agents are virostatic.
• They are active against DNA viruses; especially herpes simplex virus.
Antiviral drugs used in ophthalmology can be grouped as below:

For herpes simplex For Cytomegalo Virus For herpes zoster

virus infection retinitis virus infection
• Idoxuridine • Ganciclovir
• Foscarnet
• Acyclovir
• Vidarabine
• Zidovudin • Famciclovir
• Trifluridine
• Non selective • Valaciclovir
• Acyclovir
• Interferons • Vidarabine
• Famciclovir • Immunoglobulins • Sorvudine
 Idoxuridine
It is a halogenated pyrimidine resembling thymidine.
Mechanism of action. It inhibits viral metabolism by substituting for
thymidine in DNA synthesis and thus prevents replication of virus.
Preparations. It is available as 0.1% eye drops and 0.5% eye
ointment.
Indications and doses: Since the intraocular penetration of topically
applied IDU is very poor, it is not of much value in the treatment of
chronic stromal herpetic keratitis.
It is mainly used in acute epithelial herpetic keratitis.
IDU drops are used one hourly during day and two hourly during
night and has to be continued till microscopic staining disappears.
 Idoxuridine
Side-effects
follicular conjunctivitis,
lacrimal punctal stenosis and
irritation with photophobia.
Contraindications. It is known to inhibit corneal stromal healing,
hence its use is not advisable during first few weeks after
keratoplasty.
 Adenine Arobinoside
It is a purine nucleoside.
Uses: It has antiviral activity against herpes simplex, cytomegalo,
vaccinia and zoster viruses.
It is more potent and less toxic than IDU and is also effective in IDU
resistant cases.
It has no cross allergenicity with IDU or TF3 and thus can be used
with IDU.
Mechanism of action: It is metabolized to triphosphate form which
inhibits DNA polymerase and thus the growth of viral DNA is
arrested.
 Adenine Arobinoside

Preparations: It is available as 3% ophthalmic ointment.

Dose: It is used 5 times a day till epithelization occurs and then

reduced to once or twice daily for 4-5 days to prevent recurrences.

Side-effects are superificial punctate keratitis and irritation on

prolonged application.
 Triflurothymidine (TF3)
• It is a pyrimidine nucleoside.
• It has the advantage over IDU of higher solubility, greater
potency, lack of toxicity and allergic reactions. It is also effective
in IDU-resistant cases.
• Mechanism of action: It is a DNA inhibitor with same mechanism
as IDU.
Preparation: It is available as 1% eye drops.
• Dose: One drop is instilled 4 hourly. If no improvement occurs in 14
days, it is better to change to some other antiviral drug.
• Toxicity: It is least toxic.
• It may cause mild superficial punctate keratitis on prolonged use.
 Acyclovir (Acycloguanosine)
It has proved to be an extremely safe and effective agent and
is effective in most forms of herpes simplex and herpes zoster
infections.
Mechanism of action: It inhibits viral DNA, preferentially
entering the infected cells, with little effect on normal cells.
It penetrates into deeper layers and thus is very effective in
stromal keratitis.
Preparation. It is available as 3 % ophthalmic ointment and
also as tablet for oral use and injection for intravenous use.
 Acyclovir (Acycloguanosine)
Indications and doses: (a) Topical 3 % ointment is used 5
times a day for epithelial as well as stromal herpes simplex
keratitis
(b) Oral acyclovir 4 tablets of 200 mg each, 5 times a day for
5-7 days, may be considered in following situations:
(i) After penetrating keratoplasty in patients suffering from herpes
simplex keratitis. (ii) Recalcitrant stromal or uveal disease caused by
HSV. (iii) To reduce ocular complications of keratitis and uveitis in
herpes zoster ophthalmicus.
Side-effects: A few cases show slight punctate epithelial
keratopathy which ceases once the drug is stopped.
Valaciclovir
It is used for treatment of herpes zoster
ophthalmicus in a dose of 500-700 mg TDS for 7
days.
It is as effective as acyclovir in acute disease and
is more effective in reducing late neuralgia.
Famciclovir. Its use, dose and affectivity is similar
to valaciclovir.
Interferon--(Glycoproteins) These are non-toxic,
species-specific proteins possessing broad-
spectrum antiviral activity.
INDICATIONS DOSE
Herpes Zoster 30 – 400 million/ml once or
AIDS related Kaposi’s sarcoma twice a day for 2 weeks

Immunoglobulins. These preparations may be useful

in the treatment or prophylaxis of certain viral
diseases especially in patients with immune
deficiencies.
Uses of Anti viral drugs
• Viral Conjunctivitis

• Herpetic keratitis

• Dendritic keratitis

• Superficial punctate
keratitis
Antiviral Agents for Ophthalmic Use
GENERIC ROUTE OF ADMINISTRATION OCULAR INDICATIONS FOR USE
NAME TOXICITY

Trifluridine Topical (1% solution) PK, H -Herpes simplex keratitis

- Keratoconjuctivitis
Acyclovir Oral (200 mg capsules, -Herpes zoster ophthalmicus
800 mg tablets) - Herpes simplex iridocyclitis
Intravenous

Valacyclovir Oral (500- & 1000 mg) -Herpes simplex keratitis

-Herpes zoster ophthalmicus
Famciclovir Oral (125-,250 mg tablets) -Herpes simplex keratitis
-Herpes zoster ophthalmicus

PK – Punctate Keratopathy ; H - Hypersensitivity

Antiviral Agents for Ophthalmic Use…
GENERIC NAME ROUTE OF OCULAR INDICATIONS FOR
ADMINISTRATION TOXICITY USE
Foscarnet Intravenous ----- Cytomegalovirus
Intravitreal Retinitis
Ganciclovir Intravenous, Oral ----- Cytomegalovirus
Intravitreal implant Retinitis

Valganciclovir Oral ------- Cytomegalovirus

Retinitis

Cidofovir Intravenous ------ Cytomegalovirus

Retinitis
Thank you