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Objectives 
o Understand about each of the antiviral 
o Understand the indications for their use 
o Learn about the virus ...
Now, let’s learn 
about the 
virus life cycle
Ganciclovir 
Synthetic guanosine analogue 
First antiviral approved for CMV treatment
How does it work?
How come it doesn’t work in some 
cases? 
Mutations UL97 – encodes of CMV 
phospotransferase 
.
Which virus does it attack?
In what preparations do they 
exist? 
 Zirgan ointment 0.15% - ophthalmic gel 
 Cytovene 500 mg
What are the effects of the 
body on the drug? 
 Absorption: 
• Oral – very limited 
• t ½ : 2-6 hours 
 Distribution: A...
When do we use Ganciclovir? 
1. Herpes Epithelial Keratitis 
Ganciclovir Gel 0.15% (Zirgan) 
2. CMV Retinitis 
Initial: IV...
What are the side effects? 
 Bone marrow supression 
 Neutropenia 
 Granulocytopenia 
 TOXICITY 
 Potential carcinoge...
Valganciclovir 
Prodrug of Ganciclovir 
Taken orally 
Changed to Ganciclovir by intestinal/hepatic esterase
In what preparations do they 
exist? 
 Valcyte Tablet 450 mg 
 Valcyte Oral Solution 50 mg/mL
What are the effects of the 
body on the drug? 
 Absorption: 
• Well-absorbed especially with fatty meals 
 Distribution...
When do we use Valganciclovir? 
CMV Retinitis 
Initial: Oral 900 mg BD x 21 days 
Maintenance: 
 Oral 900 mg OD
Aciclovir 
Most commonly used antiviral 
Commonly used for HSV and Chickenpox
How does it work?
How come it doesn’t work in 
some cases? 
• Deficient viral thymidine-kinase 
. 
• Mutations to viral thymidine-kinase or ...
Which virus does it attack? 
 Herpes-simplex 1 
 Herpes-simplex 2 
 Varicella-zoster virus 
 Epstein-Barr virus 
 Cyt...
In what preparations do they 
exist? 
 Zovirax ointment 3% 
 Tablet Aciclovir 200 mg / 400 mg
What are the effects of the 
body on the drug? 
 Absorption: 
• Poor water-soluble 
• Poor oral bioavailability 
 Distri...
When do we use Aciclovir? 
Herpes-Zoster Ophthalmicus Herpex Simplex Blepharitis 
Herpes keratitis
What are the side effects? 
 Systemic 
 Nausea, vomiting 
 Encephalopathy  IV 
 Local 
 SPK 
 Allergy
Pharmacology of Ganciclovir, Valganciclovir and Aciclovir
Pharmacology of Ganciclovir, Valganciclovir and Aciclovir
Pharmacology of Ganciclovir, Valganciclovir and Aciclovir
Pharmacology of Ganciclovir, Valganciclovir and Aciclovir
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Pharmacology of Ganciclovir, Valganciclovir and Aciclovir

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Pharmacology of the anti-virals and their use in ophthalmology. Mainly on their principals and mechanism of action.

* This is short presentation as it was a small part of our medical retina team presentation where the topic was on CMV Retinitis.

Published in: Health & Medicine
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Pharmacology of Ganciclovir, Valganciclovir and Aciclovir

  1. 1. Objectives o Understand about each of the antiviral o Understand the indications for their use o Learn about the virus life cycle
  2. 2. Now, let’s learn about the virus life cycle
  3. 3. Ganciclovir Synthetic guanosine analogue First antiviral approved for CMV treatment
  4. 4. How does it work?
  5. 5. How come it doesn’t work in some cases? Mutations UL97 – encodes of CMV phospotransferase .
  6. 6. Which virus does it attack?
  7. 7. In what preparations do they exist?  Zirgan ointment 0.15% - ophthalmic gel  Cytovene 500 mg
  8. 8. What are the effects of the body on the drug?  Absorption: • Oral – very limited • t ½ : 2-6 hours  Distribution: All tissues • Especially CSF and ocular tissue  Excretion: 80-90% unchanged in urine
  9. 9. When do we use Ganciclovir? 1. Herpes Epithelial Keratitis Ganciclovir Gel 0.15% (Zirgan) 2. CMV Retinitis Initial: IV 5mg/kg BD for 14-21 days Maintenance:  IV 5mg/kg OD or  IV 6 mg/kg OD for 5 days/week
  10. 10. What are the side effects?  Bone marrow supression  Neutropenia  Granulocytopenia  TOXICITY  Potential carcinogen  Teratogen  Inhibits spermatogenesis
  11. 11. Valganciclovir Prodrug of Ganciclovir Taken orally Changed to Ganciclovir by intestinal/hepatic esterase
  12. 12. In what preparations do they exist?  Valcyte Tablet 450 mg  Valcyte Oral Solution 50 mg/mL
  13. 13. What are the effects of the body on the drug?  Absorption: • Well-absorbed especially with fatty meals  Distribution: • Well distributed especially CSF and ocular tissues  Metabolism: • In liver & intestine  changed to Ganciclovir  Excretion: 80-90% in urine
  14. 14. When do we use Valganciclovir? CMV Retinitis Initial: Oral 900 mg BD x 21 days Maintenance:  Oral 900 mg OD
  15. 15. Aciclovir Most commonly used antiviral Commonly used for HSV and Chickenpox
  16. 16. How does it work?
  17. 17. How come it doesn’t work in some cases? • Deficient viral thymidine-kinase . • Mutations to viral thymidine-kinase or DNA polymerase
  18. 18. Which virus does it attack?  Herpes-simplex 1  Herpes-simplex 2  Varicella-zoster virus  Epstein-Barr virus  Cytomegalovirus Most activity
  19. 19. In what preparations do they exist?  Zovirax ointment 3%  Tablet Aciclovir 200 mg / 400 mg
  20. 20. What are the effects of the body on the drug?  Absorption: • Poor water-soluble • Poor oral bioavailability  Distribution: High distribution rate • T ½: 3 hours  Metabolism: Small amounts – liver  Excretion: 62-90% unchanged in urine
  21. 21. When do we use Aciclovir? Herpes-Zoster Ophthalmicus Herpex Simplex Blepharitis Herpes keratitis
  22. 22. What are the side effects?  Systemic  Nausea, vomiting  Encephalopathy  IV  Local  SPK  Allergy

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