What is the mechanism of Acyclovir-induced renal toxicity?

Medical Advisory BoardAll articles are reviewed for accuracy by our Medical Advisory Board
Article Review Status
Submitted
Under Review
Approved

Last updated: February 13, 2025 • View editorial policy

From the Guidelines

Acyclovir-induced renal toxicity is primarily caused by crystalluria, leading to obstructive nephropathy.

Mechanism of Renal Toxicity

The mechanism of Acyclovir-induced renal toxicity is attributed to its excretion by the kidneys, where it can cause renal impairment through crystalluria, resulting in obstructive nephropathy 1. This reversible nephropathy usually manifests after 4 days of intravenous therapy and can affect up to 20% of patients 1, 2.

Risk Factors and Prevention

The risk of nephropathy can be reduced by maintaining adequate hydration and monitoring renal function 2. Additionally, the dose of acyclovir should be reduced in patients with pre-existing renal impairment, as it is excreted via the kidneys 2.

Clinical Considerations

In patients with suspected viral encephalitis, acyclovir treatment is usually started once the initial CSF and/or imaging findings suggest viral encephalitis, without waiting for confirmation of HSV by PCR 1, 2. However, clinicians should be aware of the potential for renal toxicity and take steps to prevent it, such as adequate hydration and monitoring of renal function.

Dosage Adjustments

Dosage adjustments for acyclovir in patients with chronic kidney disease (CKD) or end-stage renal disease (ESRD) are recommended, with reduced doses for patients with creatinine clearance <10 mL/min 3.

From the FDA Drug Label

Precipitation of acyclovir in renal tubules may occur when the solubility (2.5 mg/mL) is exceeded in the intratubular fluid. The mechanism of Acyclovir-induced renal toxicity is precipitation of acyclovir in renal tubules when the solubility is exceeded in the intratubular fluid, leading to potential renal failure 4.

  • Key factors contributing to this mechanism include: + High doses or bolus injections + Inadequate fluid and electrolyte balance + Exceeding the solubility limit of 2.5 mg/mL in the intratubular fluid

From the Research

Mechanism of Acyclovir-Induced Renal Toxicity

The mechanism of acyclovir-induced renal toxicity is complex and involves multiple factors. Some studies suggest that:

  • Acyclovir crystalluria, which leads to an intraparenchymal form of obstructive nephropathy, is a primary cause of nephrotoxicity 5, 6
  • Direct renal tubular toxicity, mediated by the acyclovir aldehyde metabolite, may also play a role in acyclovir-induced nephrotoxicity 7
  • Metabolic changes, including alterations in urinary metabolites such as guanine, 4-guanidinobutyric acid, creatinine, and urea, may be involved in the development of nephrotoxicity 8

Key Factors Contributing to Nephrotoxicity

Several factors have been identified as contributing to the development of acyclovir-induced nephrotoxicity, including:

  • Age: older patients are more susceptible to nephrotoxicity 9
  • Dose: higher doses of acyclovir increase the risk of nephrotoxicity 9
  • Concomitant use of nephrotoxic drugs: increases the risk of nephrotoxicity 9, 6
  • Duration of treatment: longer treatment durations increase the risk of nephrotoxicity 9

Pathological Changes

The pathological changes associated with acyclovir-induced nephrotoxicity include:

  • Acute tubular necrosis: characterized by loss of proximal tubule brush border and dilated proximal and distal tubules with flattening of lining cells and focal nuclear loss 5
  • Crystal deposition: acyclovir crystals may deposit in renal tubules, leading to obstructive nephropathy 5, 6

References

Research

Rapidly progressive acute renal failure due to acyclovir: case report and review of the literature.

American journal of kidney diseases : the official journal of the National Kidney Foundation, 1993

Research

Antiviral drug-induced nephrotoxicity.

American journal of kidney diseases : the official journal of the National Kidney Foundation, 2005

Research

Acyclovir-induced nephrotoxicity: the role of the acyclovir aldehyde metabolite.

Translational research : the journal of laboratory and clinical medicine, 2011

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.