Acyclovir Sodium 50mg/ml Inj, 20ml

Manufacturer FRESENIUS KABI Active Ingredient Acyclovir Injection(ay SYE kloe veer) Pronunciation ay SYE kloe veer
It is used to treat shingles or certain other herpes infections.It is used to treat chickenpox.It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Antiviral
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Pharmacologic Class
Synthetic nucleoside analog; DNA polymerase inhibitor
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Pregnancy Category
Category B
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FDA Approved
Jan 1981
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Acyclovir is an antiviral medicine given by injection into a vein. It works by stopping viruses like herpes simplex (which causes cold sores, genital herpes, and some serious infections) and varicella-zoster (which causes chickenpox and shingles) from growing and spreading in your body. It's used for serious infections or when oral medication isn't suitable.
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How to Use This Medicine

Taking Your Medication Correctly
To ensure safe and effective use, take this medication exactly as directed by your doctor. Carefully read all accompanying information and follow the instructions provided. This medication is administered as an intravenous infusion, which means it is given slowly into a vein over a specified period of time.

Storing and Disposing of Your Medication
If you need to store this medication at home, consult with your doctor, nurse, or pharmacist to determine the proper storage procedure.

Missing a Dose
If you miss a dose, contact your doctor immediately to receive guidance on what to do next.
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Lifestyle & Tips

  • Stay well-hydrated by drinking plenty of fluids, especially during and after the infusion, to help prevent kidney problems.
  • Report any pain, redness, or swelling at the injection site immediately.
  • Report any unusual side effects, especially confusion, drowsiness, or changes in urination.

Dosing & Administration

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Adult Dosing

Standard Dose: Varies by indication and patient status. Examples: Herpes Simplex Encephalitis: 10 mg/kg IV every 8 hours for 10-21 days. Severe Initial Genital Herpes: 5 mg/kg IV every 8 hours for 5-10 days. Varicella Zoster (immunocompromised): 10 mg/kg IV every 8 hours for 7-10 days.
Dose Range: 5 - 10 mg

Condition-Specific Dosing:

Herpes Simplex Encephalitis: 10 mg/kg IV every 8 hours for 10-21 days
Severe Initial Genital Herpes: 5 mg/kg IV every 8 hours for 5-10 days
Mucocutaneous HSV (immunocompromised): 5-10 mg/kg IV every 8 hours for 7-14 days
Varicella Zoster (immunocompromised): 10 mg/kg IV every 8 hours for 7-10 days
Herpes Zoster (normal immune): 10 mg/kg IV every 8 hours for 7 days
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Pediatric Dosing

Neonatal: Neonatal HSV: 20 mg/kg IV every 8 hours for 14-21 days (dose based on postmenstrual age and postnatal age, consult specific guidelines).
Infant: HSV/VZV (3 months to <12 years): 10-20 mg/kg IV every 8 hours (max 500 mg/m2/dose).
Child: HSV/VZV (3 months to <12 years): 10-20 mg/kg IV every 8 hours (max 500 mg/m2/dose).
Adolescent: HSV/VZV (â‰Ĩ12 years): Adult dosing (e.g., 5-10 mg/kg IV every 8 hours).
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Dose Adjustments

Renal Impairment:

Mild: CrCl 25-50 mL/min: Administer recommended dose every 12 hours.
Moderate: CrCl 10-25 mL/min: Administer recommended dose every 24 hours.
Severe: CrCl <10 mL/min: Administer half of the recommended dose every 24 hours.
Dialysis: Hemodialysis: Administer recommended dose after each dialysis session. Peritoneal Dialysis: No specific recommendations, but consider dose adjustment similar to CrCl <10 mL/min.

Hepatic Impairment:

Mild: No adjustment generally needed.
Moderate: No adjustment generally needed.
Severe: No adjustment generally needed.

Pharmacology

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Mechanism of Action

Acyclovir is a synthetic purine nucleoside analog with in vitro and in vivo inhibitory activity against herpes simplex virus types 1 (HSV-1), 2 (HSV-2), and varicella-zoster virus (VZV). It is converted to acyclovir monophosphate by viral thymidine kinase, then to acyclovir triphosphate by cellular enzymes. Acyclovir triphosphate inhibits viral DNA synthesis and replication by competing with deoxyguanosine triphosphate for incorporation into viral DNA, leading to chain termination.
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Pharmacokinetics

Absorption:

Bioavailability: 100% (IV administration)
Tmax: Not applicable (IV)
FoodEffect: Not applicable (IV)

Distribution:

Vd: 0.8 L/kg (adults)
ProteinBinding: 9% to 33%
CnssPenetration: Yes (CSF concentrations are approximately 30-50% of plasma concentrations)

Elimination:

HalfLife: 2.5 to 3.3 hours (in adults with normal renal function)
Clearance: Primarily renal clearance via glomerular filtration and tubular secretion.
ExcretionRoute: Renal (unchanged drug)
Unchanged: 62% to 91% (excreted unchanged in urine)
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Pharmacodynamics

OnsetOfAction: Rapid (IV administration)
PeakEffect: Within minutes of infusion completion
DurationOfAction: Dependent on half-life and viral replication cycle, typically requiring every 8-hour dosing for sustained antiviral effect.

Safety & Warnings

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Side Effects

Serious Side Effects: Seek Medical Help Immediately

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention right away:

Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Behavioral problems
Mood changes
Feeling confused
Hallucinations (seeing or hearing things that are not there)
Seizures
Shakiness
Feeling dizzy or sleepy
Burning, numbness, or tingling sensations that are not normal
Changes in speech

Kidney Problems

Severe and potentially life-threatening kidney problems have been reported with this medication. Contact your doctor immediately if you experience:

Inability to pass urine
Blood in the urine
Changes in the amount of urine passed
Unexpected weight gain

Blood Problems

Rare but serious blood problems, such as thrombotic thrombocytopenic purpura/hemolytic uremic syndrome (TTP/HUS), have been reported with this medication. Seek medical attention right away if you experience:

Feeling very tired or weak
Bruising or bleeding
Dark urine or yellow skin or eyes
Pale skin
Changes in the amount of urine passed
Changes in eyesight
Changes in strength on one side of the body
Trouble speaking or thinking
Changes in balance
Fever

Other Side Effects

Like all medications, this drug can cause side effects. Many people may not experience any side effects or may only have mild ones. If you notice any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical attention:

Upset stomach or vomiting
Feeling tired or weak
* Irritation at the injection site

Reporting Side Effects

This is not a comprehensive list of all possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Severe dizziness or lightheadedness
  • Confusion, hallucinations, or unusual thoughts/behavior
  • Seizures
  • Difficulty urinating or significant decrease in urine output
  • Severe rash or hives
  • Swelling of the face, lips, tongue, or throat (signs of allergic reaction)
  • Pain, redness, or swelling at the injection site that worsens
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about any allergies you have, including:
- An allergy to this medication or any of its components
- An allergy to other medications, foods, or substances
Please describe the allergy and the symptoms you experienced.

This medication may interact with other medications or health conditions. To ensure safe use, disclose all of the following to your doctor and pharmacist:
- All prescription and over-the-counter (OTC) medications you are taking
- Any natural products or vitamins you are using
- Any existing health problems

Before starting, stopping, or changing the dose of any medication, including this one, consult with your doctor to confirm it is safe to do so with your current medications and health conditions.
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Precautions & Cautions

Important Warnings and Precautions

When taking this medication, it is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are using this drug.

To stay hydrated, drink plenty of non-caffeinated liquids every day, unless your doctor advises you to limit your fluid intake.

If you are 65 years or older, exercise caution when using this medication, as you may be more susceptible to side effects.

If you are pregnant, planning to become pregnant, or breastfeeding, consult your doctor to discuss the potential benefits and risks to you and your baby.

Herpes Infection Considerations

This medication does not cure herpes infections; consult your doctor to discuss treatment options.

If you have genital herpes, note that this medication will not prevent the spread of the infection. Avoid any sexual activity when you have active sores or symptoms of genital herpes. Additionally, genital herpes can still be transmitted even when you do not exhibit any symptoms. To minimize the risk of transmission, use a latex or polyurethane condom during sexual activity and consult your doctor for guidance.
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Overdose Information

Overdose Symptoms:

  • Increased serum creatinine and BUN (indicating renal dysfunction)
  • Renal failure (due to precipitation of acyclovir in renal tubules)
  • Neurological symptoms (lethargy, confusion, agitation, hallucinations, seizures, coma)

What to Do:

Seek immediate medical attention. Hemodialysis is effective in removing acyclovir from the blood. Maintain adequate hydration to prevent renal tubular crystallization. Symptomatic and supportive care should be provided. Call 1-800-222-1222 (Poison Control) for further guidance.

Drug Interactions

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Major Interactions

  • Foscarnet (increased risk of renal impairment)
  • Mycophenolate mofetil (increased concentrations of both drugs)
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Moderate Interactions

  • Probenecid (increases acyclovir AUC and decreases renal clearance)
  • Zidovudine (potential for increased neurotoxicity, though clinical significance is debated)
  • Nephrotoxic agents (e.g., aminoglycosides, NSAIDs, cyclosporine, tacrolimus - increased risk of renal dysfunction)

Monitoring

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Baseline Monitoring

Renal function (Serum Creatinine, BUN, CrCl)

Rationale: Acyclovir is primarily renally eliminated; dose adjustments are necessary in renal impairment.

Timing: Prior to initiation of therapy.

Hydration status

Rationale: Adequate hydration is crucial to prevent renal tubular crystallization.

Timing: Prior to and during therapy.

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Routine Monitoring

Renal function (Serum Creatinine, BUN)

Frequency: Daily or every 2-3 days, especially in patients with pre-existing renal impairment, dehydration, or receiving concomitant nephrotoxic drugs.

Target: Within patient's baseline or acceptable limits.

Action Threshold: Significant increase in creatinine or BUN; consider dose adjustment or discontinuation.

Urine output

Frequency: Daily

Target: Adequate for hydration status.

Action Threshold: Decreased urine output; assess hydration and renal function.

Infusion site

Frequency: Prior to and during infusion

Target: No signs of phlebitis or extravasation.

Action Threshold: Redness, swelling, pain; discontinue infusion and manage extravasation.

Neurological status (especially in high doses or renal impairment)

Frequency: Daily

Target: Normal mental status.

Action Threshold: Confusion, lethargy, seizures; investigate and consider drug-induced neurotoxicity.

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Symptom Monitoring

  • Signs of renal dysfunction (decreased urine output, edema)
  • Neurological changes (lethargy, confusion, hallucinations, seizures, tremors)
  • Infusion site reactions (pain, redness, swelling, phlebitis)
  • Gastrointestinal disturbances (nausea, vomiting, diarrhea)
  • Headache
  • Rash

Special Patient Groups

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Pregnancy

Category B. Acyclovir is generally considered safe for use during pregnancy when indicated for severe or life-threatening herpesvirus infections. The Acyclovir in Pregnancy Registry did not show an increased risk of birth defects.

Trimester-Specific Risks:

First Trimester: No increased risk of birth defects observed in human studies.
Second Trimester: Considered safe when indicated.
Third Trimester: Considered safe when indicated; may be used for suppression near term to prevent neonatal HSV transmission.
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Lactation

Acyclovir is excreted into breast milk. However, the amount transferred to the infant is low, and adverse effects in breastfed infants are not commonly reported. Generally considered compatible with breastfeeding (Lactation Risk Category L2).

Infant Risk: Low risk; monitor infant for diarrhea or rash.
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Pediatric Use

Dosing is weight-based and varies significantly by age group (neonates, infants, children, adolescents) and indication. Neonates require careful dosing based on postmenstrual and postnatal age due to immature renal function. Close monitoring of renal function and hydration is essential.

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Geriatric Use

Elderly patients are more likely to have decreased renal function, which necessitates dose adjustment based on creatinine clearance. They are also at increased risk for neurological adverse effects (e.g., confusion, lethargy) due to higher systemic concentrations and potential for dehydration. Close monitoring of renal function and neurological status is crucial.

Clinical Information

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Clinical Pearls

  • Administer IV acyclovir by slow intravenous infusion over at least 1 hour to prevent renal tubular damage and local irritation.
  • Ensure adequate hydration before, during, and after infusion to minimize the risk of renal toxicity due to acyclovir crystallization in the renal tubules.
  • Do not administer acyclovir by rapid intravenous injection or bolus infusion.
  • Acyclovir IV is a vesicant; ensure proper IV access and monitor for extravasation. If extravasation occurs, discontinue infusion immediately and manage according to institutional guidelines.
  • Dose adjustments are critical in patients with renal impairment; always calculate creatinine clearance before initiating therapy and monitor renal function throughout treatment.
  • Neurological adverse effects (e.g., lethargy, confusion, seizures) are more common in patients with renal impairment or those receiving high doses; monitor closely.
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Alternative Therapies

  • Valacyclovir (oral prodrug of acyclovir)
  • Famciclovir (oral prodrug of penciclovir)
  • Ganciclovir (for CMV, not typically HSV/VZV unless resistant)
  • Foscarnet (for resistant HSV/VZV or in immunocompromised patients with renal impairment where acyclovir is contraindicated)
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Cost & Coverage

Average Cost: Highly variable, typically $50 - $200+ per 500 mg vial
Generic Available: Yes
Insurance Coverage: Tier 1 or 2 (generic), Tier 3 (brand) for most insurance plans, often covered for indicated uses.
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General Drug Facts

If your symptoms or health problems do not improve or worsen over time, it is essential to contact your doctor for further guidance. To ensure your safety and the safety of others, never share your prescription medications with anyone, and do not take medications that have been prescribed to someone else.

All medications should be stored in a secure location, out of the reach of children and pets, to prevent accidental ingestion. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless specifically instructed to do so by a healthcare professional or pharmacist. Instead, consult with your pharmacist to determine the best method for disposal, as some communities may have designated drug take-back programs.

Additionally, some medications may come with a separate patient information leaflet; if you have questions or concerns, your pharmacist can provide more information. If you have any questions or concerns about your medication, it is crucial to discuss them with your doctor, nurse, pharmacist, or other healthcare provider.

In the event of a suspected overdose, immediately contact your local poison control center or seek emergency medical attention. Be prepared to provide detailed information about the medication, including the amount taken, the time it was taken, and any other relevant details.