III. Pharmacokinetics

  1. Base Weight calculations on Lean Body Mass
  2. Metabolized by Kidney
    1. Decrease interval in renal Impairment to q12-24h
  3. Dialysis: 50-100% dialyzable

IV. Safety: Pregnancy and Lactation

  1. FDA Pregnancy Class C
  2. Safety unclear in Breast Feeding

V. Preparations

  1. Tablets: 200, 400, 800 mg
  2. Suspension: 200 mg/5 ml
  3. Buccal tablet (Sitavig)

VI. Dosing: Orolabial Herpes (Cold Sores)

  1. Primary Herpetic Gingivostomatitis
    1. Adult: 200 mg orally every 4 hours while awake (5x/day)
    2. Ped: 15 mg/kg/day (750 mg/m2/day) divided five times daily for 5 days
  2. Episodic, recurrent Orolabial Herpes
    1. Topicals
      1. Acyclovir cream apply 5 times per day for 4 days
      2. Sitavig buccal one tablet per episode placed in upper gum on same side of mouth as symptoms
        1. Very expensive ($300 for 2 tabs in 2014) and only shortens Cold Sore course by <1 day
        2. (2014) Presc Lett 21(9): 53
    2. Systemic
      1. Child: 15 mg/kg (max: 200 mg) orally 5 times per day for 5 days
      2. Adult: 400 mg orally 3 times daily for 5 days (or 200 mg orally 5 times daily for 5 days)

VII. Dosing: Herpes Neonatorum

  1. HSV Encephalitis or Herpes Neonatorum
    1. Child: 30 mg/kg/day (1500 mg/m2/day) divided every 8 hours IV

VIII. Dosing: Genital Herpes

  1. Initial Genital HSV
    1. Adult: 200 mg orally 5 times per day for 10 days
  2. Episodic Genital HSV
    1. Adult: 200 mg orally 5 times per day for 5 days
    2. Apply topical Acyclovir to affected area 6 times per day for 7 days
  3. Prophylaxis of Genital HSV
    1. Adult: 400 mg orally twice daily for up to 12 months

IX. Dosing: Varicella Zoster

  1. Herpes Zoster (Shingles) or Herpes Ophthalmicus
    1. Adult Oral: 800 mg orally 5 times/day for 7-10 days
    2. Adult IV: 10-12 mg/kg/dose every 8 hours for 7-14 days
  2. Varicella Zoster Virus (Chicken Pox)
    1. Child
      1. Dose: 10-20 mg/kg/dose to 800 mg orally four times daily for 5 days
    2. Adult
      1. Dose: 600-800 mg/dose orally every 4 hours while awake (5x/day)
      2. Dose: 1000 mg/dose orally every 6 hours for 5 days
    3. Intravenous
      1. Dose: 30 mg/kg/day (1500 mg/m2/day) divided q8h IV

X. Adverse Effects

  1. Headache
  2. Gastrointestinal Upset
  3. Impaired Renal Function
  4. CNS depression
    1. Lethargy
    2. Confusion
    3. Coma
  5. Tremors
  6. Agitation

XI. Drug Interactions (prolong Acyclovir half life)

XII. Precautions

  1. Overdose may result in Renal Failure
  2. Maintain adequate urine to flush renal tubules

XIII. Efficacy: Herpes Labialis (Oral Herpes)

  1. Only effective if used at outset of symptoms (first sense of Paresthesias such as burning or tingling)
  2. Shortens Vesicle life and decreases shedding
  3. Prevents recurrence in immunocompromised
  4. Reduction in episodes: 53%
  5. Quicker healing: 4 days instead of 8 for Placebo
  6. Reduction in number of Fever Blisters: 71%

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Cost: Medications

Acyclovir (on 6/18/2017 at Walmart.com)
Acyclovir 200mg #30 capsules for $4.00 $0.13 each
Acyclovir 200mg #90 capsules for $10.00 $0.11 each
acyclovir (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
ACYCLOVIR 200 MG CAPSULE Generic $0.12 each
ACYCLOVIR 200 MG/5 ML SUSP Generic $0.57 per ml
ACYCLOVIR 400 MG TABLET Generic $0.10 each
ACYCLOVIR 5% OINTMENT Generic $13.26 per gram
ACYCLOVIR 800 MG TABLET Generic $0.19 each
zovirax (on 2/22/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
ZOVIRAX 5% CREAM $140.34 per gram

Ontology: Acyclovir (C0001367)

Definition (CHV) a drug used to treat initial genital herpes infections
Definition (NCI_NCI-GLOSS) A substance used to prevent or treat cytomegalovirus and herpes simplex infections that may occur when the body is immunosuppressed. It belongs to the family of drugs called antivirals.
Definition (NCI) A synthetic analog of the purine nucleoside, guanosine, with potent antiviral activity against herpes simplex viruses type 1 and 2, varicella-zoster virus and other viruses of the herpesvirus family. After conversion in vivo to the active metabolite acyclovir triphosphate by viral thymidine kinase, acyclovir competitively inhibits viral DNA polymerase by incorporating into the growing viral DNA chain and terminating further polymerization.
Definition (MSH) A GUANOSINE analog that acts as an antimetabolite. Viruses are especially susceptible. Used especially against herpes.
Definition (CSP) 9-(2-hydroxyethoxymethyl) guanine; acts against herpesviruses by inhibiting the viral DNA polymerase.
Definition (PDQ) A synthetic analog of the purine nucleoside, guanosine, with potent antiviral activity against herpes simplex viruses type 1 and 2, varicella-zoster virus and other viruses. After conversion in vivo to the active metabolite acyclovir triphosphate, acyclovir competitively inhibits viral DNA polymerase, incorporates into and terminates the growing viral DNA chain, and inactivates viral DNA polymerase. The greater antiviral activity of acyclovir against HSV compared to VZV is due to its more efficient phosphorylation by the thymidine kinase of HSV. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39134&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39134&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C205" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Nucleic Acid, Nucleoside, or Nucleotide (T114)
MSH D000212
SnomedCT 425884003, 372729009, 330282004, 324721009, 333010007, 391710009, 41193000
LNC LP14522-4, MTHU006764
English Aciclovir, Acycloguanosine, 6H-Purin-6-one, 2-amino-1,9-dihydro-9-((2-hydroxyethoxy)methyl)-, Aciclovir [eyes], Aciclovir [skin], Aciclovir [systemic], Acyclovir [eyes], Acyclovir [skin], Acyclovir [systemic], 9-((2-Hydroxyethoxy)methyl)guanine, 2-Amino-1,9-dihydro-9-[(2-hydroxyethoxy)methyl]-6H-purin-6-one, 9-[(2-Hydroxyethoxy)methyl]guanine, acyclovir, ACV, Ophthalmic form aciclovir, Ophthalmic form acyclovir (product), Ophthalmic form acyclovir, acyclovir (medication), ACYCLOVIR, Acyclovir [Chemical/Ingredient], aciclovir, Aciclovir - chemical, Aciclovir - chemical (substance), Aciclovir [systemic] (product), Aciclovir [eyes] (product), Aciclovir [skin] (product), 9-[(2-Hydroxyethoxy)-methyl]guanine, Acyclovir (product), Acyclovir (substance), acycloguanosine, Acyclovir, Aciclovir [eyes] (substance), Aciclovir [skin] (substance), Aciclovir [systemic] (substance)
Swedish Aciklovir
Czech acykloguanosin, acyklovir
Spanish aciclovir, forma oftálmica, aciclovir, forma oftálmica (producto), aciclovir (uso dermatológico), aciclovir [uso oftálmico], aciclovir (uso dermatológico) (producto), aciclovir [uso oftálmico] (producto), aciclovir [uso sistémico], aciclovir [uso sistémico] (producto), acicloguanosina, aciclovir (piel) (producto), aciclovir (piel), aciclovir (producto), aciclovir (sustancia), aciclovir [oftálmico] (producto), aciclovir [oftálmico], aciclovir [sistémico] (producto), aciclovir [sistémico], aciclovir, Acicloguanosina, Aciclovir
Finnish Asykloviiri
Russian ATSIKLOGUANOZIN, ATSIKLOVIR, АЦИКЛОВИР, АЦИКЛОГУАНОЗИН
Japanese アシクロビル, アシクログアノシン
Polish Acyklowir, Acyklognanozyna
French Aciclovir, Acycloguanosine, 9-((2-Hydroxyethoxy)methyl)guanine, Acyclovir
German Aciclovir, Acycloguanosin, Acyclovir, Azyklovir
Italian Acyclovir
Portuguese Acicloguanosina, Aciclovir

Ontology: Zovirax (C0592290)

Concepts Pharmacologic Substance (T121) , Nucleic Acid, Nucleoside, or Nucleotide (T114)
MSH D000212
English zovirax, Glaxo Wellcome Brand of Aciclovir Sodium Salt, Glaxo Wellcome Brand of Aciclovir, Parke Davis Brand of Aciclovir, Warner Wellcome Brand of Aciclovir, Wellcome Brand of Aciclovir Sodium Salt, Wellcome Brand of Aciclovir, Zovirax for Injection, Aciclovir Wellcome Brand, Zovirax