Pharmacopeia

Canonical comparison

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Field ACICLOVIR
Anti-infectives · Anti-infectives · Level 3
NEURAMINIDASE INHIBITORS
Anti-infectives · Anti-infectives · Level 3
AMPHOTERICIN B
Anti-infectives · Anti-infectives · Level 3
GANCICLOVIR
Anti-infectives · Anti-infectives · Level 3
CASPOFUNGIN
Anti-infectives · Anti-infectives · Level 3
Mechanism of action

- Inhibits nucleic acid synthesis
- Cells infected with HSV or VZV contain virally encoded thymidine kinase that converts acyclovir to acyclovir monophosphate. This is then converted to an active triphosphate that inhibits viral DNA polymerase and acts as a chain terminator
- Thymidine kinase in non-infected cells has a low affinity for acyclovir
- Whilst useful for HSV and VZV, it does not eradicate them and is only useful if given at the start of an infection

inhibit neurominidase resulting in impaired viral release from infected cells. Neurominidase cleaves the sialic acid on the cell membrane allowing viral budding.

Polyenes specifically target fungal membranes. They bind ergosterol, which is the principal sterol in fungal membranes as opposed to cholesterol found in host membranes. This interference creates a transmembrane channel and the resultant change in permeability allows leakage of intracellular components

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Absorption

Erratic intestinal absorption and low bioavailability (25%). Oral valine-esterified prodrug valacyclovir improves absorption

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only administered IV

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Distribution

Widely distributed

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Poor tissue penetration. Negligable CSF or urine penetration.

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Protein binding — —

Highly protein bound

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Metabolism

Oral valine-esterified prodrug valacyclovir is rapidly hydrolyzed in the blood

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Metabolised by the liver

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Excretion

actively excreted in the kidneys unchanged (blocked by probenecid)

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poorly characterized but does not accumulate in renal failure

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Adverse Effects Toxicity

Renal
- Rapid IV administration may precipitate renal failure
Thrombophlebitis
- Highly irritating to veins and extravasation may lead to ulcers
CNS
- Tremors, confusion, seizures and coma in rapid infusion

1. Psychiatric symptoms
2. N/V/D
3. Bronchospasm

Dose related nephrotoxicity
Infusion related reactions (hypotension, fever, rigors)

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Antimicrobial Spectrum

Herpes Simplex (1 and 2) and Varicella Zoster.
Lacks CMV cover

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Broad antifungal cover including candida, Cryptococcus, aspergillus and zygomyces

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Class Group

Antiviral

Antiviral

Antifungal

Antiviral

Antifungal

Introduction

Synthetic nucleoside analogue

Oseltamivir and Zanamivir

Polyene

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Legacy Cicm Level

Level 3

Level 3

Level 3

Level 3

Level 3