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TOPIC; ACYCLOVIR
 PRESENTED BY;
 MR. HAMMAD HASSNAIN
 Class no; 39 (M)- 3RD PROFF
 PRESENTED TO;
 MR. ZAHID RASUL NIAZI
Faculty of Pharmacy,
 Gomal university, Dera ismail khan.
2
ANTIVIRAL DRUGS
 There are four main classes of antiviral drugs;
 1- DNA polymerase inhibitors;
 Acyclovir
 2- Reverse transcriptase inhibitors;
 Abacavir.
 3- Protease inhibitors;
 Ritonavir.
 4- Fusion inhibitors;
 Enfuvirtide. 3
ACYCLOVIR
 INTRODUCTION;
 Prototypic anti-herpetic therapeutic agent.
 Highly efficacious antiviral drug for herpes virus
infections.
 drug of choice for HSV encephalitis.
 Most commonly used in genital herpes infections.
 Used as post transplant immunosuppressive
treatments.
4
CHEMISTRY;
 CATEGORY; anti-viral agent.
 CLASS; imidazolpyrimidines.
 Subclass; Guanine & its derivatives.

5
PHARMACOKINETICS;
 ABSORPTION;
 Administered orally, intravenous or topically.
 Distributes well throughout the body including CSF.
 METABOLISM;
 Partially metabolized to an inactive product.
 BIOAVAILIBILITY;
 Valacyclivir has greater oral bio-availability than acyclovir.
6
SOLUBILITY;
 Poorly water solubility and has poor oral
bioavailability i.e about 15-30%.
HALF LIFE;
 2.5 to 3.3 hours.
EXCRETION;
 Excretion occurs in urine by glomerular filtration and
tubular secretion.
7
MECHANISM OF ACTION;
 Acyclovir is a pro drug, it needs phosphorylation for
its activation.
 Acyclovir is converted into acyclovir monophosphate
by viral thymadine kinase.
 Which is then coverted into acyclovir triphosphate by
host cell kinase, and comparatively inhibits HSV
specified DNA Polymerases.
 Thus in this way it prevent further viral DNA synthesis
without affecting other normal cellular functions.
8
9
SPECTRUM;
Herpes
simplex
virus
(type-1)
Herpes
simplex
virus
(type-2)
Vericella
zoster
virus
(VZV)
Epstain
barr virus.
10
INDICATIONS;
Genital herpes simplex (HSV-2)
• 15mg/kg/day…. For 7-days.
Muco-Cutaneous herpes simplex
(HSV-2)
• 10mg/kg (t.i.d)… for 10 days.
Herpes simplex encephalitis
(type-1)
11
• 3DAYS eye ointment (5 times a day) OR orally.
Herpes simplex keratinitis. (HSV-1)
• 5-10mg/kg (t.i.d.) for 7-days.
Vericella zoster infection.
• 15mg/kg/day … for 7-days.
Chicken pox.
12
ADVERSE EFFECTS;
 Although acyclovir is potent, but there are some dose related
slight adversities, as follows;
 TOPICAL ADMINSTRTION; local irritation, stinging, burning
sensation.
 I/V ADMINISTRATION; hypotension, sweating, rashes, vomiting,
dose dependent decrease in glomerular filtration rate (GFR).
 CNS; Fatigue, reversible neurological reactions, headache.
 GIT; nausea, diarrhea, abdominal pain.
 LIVER; increase in hepatic enzymes.
 BLOOD; slight hyper-uricemia, thrombocytopenia.
13
RESISTANCE;
14
DRUG-DRUG INTERACTIONS;
Promelicin increases the half life
of acyclovir.
Cidofovir is not recommended with
acyclovir because it may damage
kidney.
15
BRANDS IN PAKISTAN;
 ZOVIRAX (Glaxosmithklin)
 CLOVIR (Giltz pharma)
 SUPRAVIRAN (Searle Pakistan. ltd)
 acyclovir (Abott labs)
16
REFRENCES;
 Lippincott’s Pharmacology (5th edition)
 www.Wikipedia.com
 Slideshare.com
 Basic concept of pharmacology. (Mr. Inayatulallah Bhatti)
 Dr. Zahid Rasul Niazi Lectures.
BUNDLE OF THANKS FOR YOUR ATTENTIONS---  
 Compiled BY; Syed Baqir Naqvi.
17

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Acyclovir

  • 1. 1
  • 2. TOPIC; ACYCLOVIR  PRESENTED BY;  MR. HAMMAD HASSNAIN  Class no; 39 (M)- 3RD PROFF  PRESENTED TO;  MR. ZAHID RASUL NIAZI Faculty of Pharmacy,  Gomal university, Dera ismail khan. 2
  • 3. ANTIVIRAL DRUGS  There are four main classes of antiviral drugs;  1- DNA polymerase inhibitors;  Acyclovir  2- Reverse transcriptase inhibitors;  Abacavir.  3- Protease inhibitors;  Ritonavir.  4- Fusion inhibitors;  Enfuvirtide. 3
  • 4. ACYCLOVIR  INTRODUCTION;  Prototypic anti-herpetic therapeutic agent.  Highly efficacious antiviral drug for herpes virus infections.  drug of choice for HSV encephalitis.  Most commonly used in genital herpes infections.  Used as post transplant immunosuppressive treatments. 4
  • 5. CHEMISTRY;  CATEGORY; anti-viral agent.  CLASS; imidazolpyrimidines.  Subclass; Guanine & its derivatives.  5
  • 6. PHARMACOKINETICS;  ABSORPTION;  Administered orally, intravenous or topically.  Distributes well throughout the body including CSF.  METABOLISM;  Partially metabolized to an inactive product.  BIOAVAILIBILITY;  Valacyclivir has greater oral bio-availability than acyclovir. 6
  • 7. SOLUBILITY;  Poorly water solubility and has poor oral bioavailability i.e about 15-30%. HALF LIFE;  2.5 to 3.3 hours. EXCRETION;  Excretion occurs in urine by glomerular filtration and tubular secretion. 7
  • 8. MECHANISM OF ACTION;  Acyclovir is a pro drug, it needs phosphorylation for its activation.  Acyclovir is converted into acyclovir monophosphate by viral thymadine kinase.  Which is then coverted into acyclovir triphosphate by host cell kinase, and comparatively inhibits HSV specified DNA Polymerases.  Thus in this way it prevent further viral DNA synthesis without affecting other normal cellular functions. 8
  • 9. 9
  • 11. INDICATIONS; Genital herpes simplex (HSV-2) • 15mg/kg/day…. For 7-days. Muco-Cutaneous herpes simplex (HSV-2) • 10mg/kg (t.i.d)… for 10 days. Herpes simplex encephalitis (type-1) 11
  • 12. • 3DAYS eye ointment (5 times a day) OR orally. Herpes simplex keratinitis. (HSV-1) • 5-10mg/kg (t.i.d.) for 7-days. Vericella zoster infection. • 15mg/kg/day … for 7-days. Chicken pox. 12
  • 13. ADVERSE EFFECTS;  Although acyclovir is potent, but there are some dose related slight adversities, as follows;  TOPICAL ADMINSTRTION; local irritation, stinging, burning sensation.  I/V ADMINISTRATION; hypotension, sweating, rashes, vomiting, dose dependent decrease in glomerular filtration rate (GFR).  CNS; Fatigue, reversible neurological reactions, headache.  GIT; nausea, diarrhea, abdominal pain.  LIVER; increase in hepatic enzymes.  BLOOD; slight hyper-uricemia, thrombocytopenia. 13
  • 15. DRUG-DRUG INTERACTIONS; Promelicin increases the half life of acyclovir. Cidofovir is not recommended with acyclovir because it may damage kidney. 15
  • 16. BRANDS IN PAKISTAN;  ZOVIRAX (Glaxosmithklin)  CLOVIR (Giltz pharma)  SUPRAVIRAN (Searle Pakistan. ltd)  acyclovir (Abott labs) 16
  • 17. REFRENCES;  Lippincott’s Pharmacology (5th edition)  www.Wikipedia.com  Slideshare.com  Basic concept of pharmacology. (Mr. Inayatulallah Bhatti)  Dr. Zahid Rasul Niazi Lectures. BUNDLE OF THANKS FOR YOUR ATTENTIONS---    Compiled BY; Syed Baqir Naqvi. 17