Peringatan Keamanan

Symptoms of overdose include agitation, coma, seizures, lethargy, and precipitation in renal tubules.L7315 These symptoms are more common in patients given high doses without monitoring of fluid and electrolyte balance or reduced kidney function.L7315,A180730,A180775 In the case of an overdose, treat with symptomatic and supportive care.L7321

Acyclovir

DB00787

small molecule approved

Deskripsi

Acyclovir is a deoxynucleoside analog antiviral used to treat herpes simplex, Varicella zoster, herpes zoster, herpes labialis, and acute herpetic keratitis.L7303,L7315,L7318,L7321,L7324,L7327 Acyclovir is generally used first line in the treatment of these viruses and some products are indicated for patients as young as 6 years old.L7321

Acyclovir was granted FDA approval on 29 March 1982.L7318

Struktur Molekul 2D

Berat 225.2046
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The clearance of acyclovir varies from 2.5-3 hours depending on the creatinine clearance of the patient.[A180757] The plasma half life of acyclovir during hemodialysis is approximately 5 hours.[L7315] The mean half life in patients from 7 months to 7 years old is 2.6 hours.[L7315]
Volume Distribusi The volume of distribution of acyclovir is 0.6L/kg.[A180775]
Klirens (Clearance) The renal clearance of acyclovir is 248mL/min/1.73m<sup>2</sup>.[A180787] The total clearance in neonates if 105-122mL/min/1.73m<sup>2</sup>.[A180787]

Absorpsi

The oral bioavailability of acyclovir is 10-20% but decreases with increasing doses.L7315 Acyclovir ointment is <0.02-9.4% absorbed.L7318 Acyclovir buccal tablets and ophthalmic ointment are minimally absorbed.L7324,L7327 The bioavailability of acyclovir is not affected by food.L7315 Acyclovir has a mean Tmax of 1.1±0.4 hours, mean Cmax of 593.7-656.5ng/mL, and mean AUC of 2956.6-3102.5h/*ng/mL.A180793

Metabolisme

Acyclovir is <15% oxidized to 9-carboxymethoxymethylguanine by alcohol dehydrogenase and aldehyde dehydrogenase and 1% 8-hydroxylated to 8-hydroxy-acyclovir by aldehyde oxidase.A180730 Acyclovir is becomes acyclovir monophosphate due to the action of viral thymidine kinase.A180757 Acyclovir monophosphate is converted to the diphosphate form by guanylate kinase.A903 Acyclovir diphosphate is converted to acyclovir triphosphate by nucleoside diphosphate kinase, pyruvate kinase, creatine kinase, phosphoglycerate kinase, succinyl-CoA synthetase, phosphoenolpyruvate carboxykinase and adenylosuccinate synthetase.A903,A180781

Rute Eliminasi

The majority of acyclovir is excreted in the urine as unchanged drug.A180730,L7324 90-92% of the drug can be excreted unchanged through glomerular filtration and tubular secretion.A180757 <2% of the drug is recovered in feces and <0.1% is expired as CO2.A180787

Interaksi Makanan

2 Data
  • 1. Drink plenty of fluids. Dehydration with acyclovir predisposes patients to nephrotoxicity.
  • 2. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1103 Data
Deferasirox The serum concentration of Acyclovir can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Acyclovir can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Acyclovir can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Acyclovir can be decreased when it is combined with Teriflunomide.
Foscarnet The risk or severity of nephrotoxicity can be increased when Acyclovir is combined with Foscarnet.
Mannitol The risk or severity of nephrotoxicity can be increased when Mannitol is combined with Acyclovir.
Tenofovir disoproxil Acyclovir may increase the nephrotoxic activities of Tenofovir disoproxil.
Tenofovir alafenamide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Acyclovir.
Tenofovir Acyclovir may increase the nephrotoxic activities of Tenofovir.
Aspartame The excretion of Acyclovir can be decreased when combined with Aspartame.
Pravastatin The excretion of Acyclovir can be decreased when combined with Pravastatin.
Aminohippuric acid The excretion of Acyclovir can be decreased when combined with Aminohippuric acid.
Lansoprazole The excretion of Acyclovir can be decreased when combined with Lansoprazole.
Enalapril The excretion of Acyclovir can be decreased when combined with Enalapril.
Oxytetracycline The excretion of Acyclovir can be decreased when combined with Oxytetracycline.
Leucovorin The excretion of Acyclovir can be decreased when combined with Leucovorin.
Esomeprazole The excretion of Acyclovir can be decreased when combined with Esomeprazole.
Succinic acid The excretion of Succinic acid can be decreased when combined with Acyclovir.
Citrulline The excretion of Citrulline can be decreased when combined with Acyclovir.
Cefdinir The excretion of Cefdinir can be decreased when combined with Acyclovir.
Fluorescein The excretion of Fluorescein can be decreased when combined with Acyclovir.
Hydrocortisone The excretion of Hydrocortisone can be decreased when combined with Acyclovir.
Quinapril The excretion of Quinapril can be decreased when combined with Acyclovir.
Famotidine The excretion of Famotidine can be decreased when combined with Acyclovir.
Fexofenadine The excretion of Fexofenadine can be decreased when combined with Acyclovir.
Benzylpenicillin The excretion of Benzylpenicillin can be decreased when combined with Acyclovir.
Rosuvastatin The excretion of Rosuvastatin can be decreased when combined with Acyclovir.
Captopril The excretion of Captopril can be decreased when combined with Acyclovir.
Tazobactam The excretion of Tazobactam can be decreased when combined with Acyclovir.
Cyclic adenosine monophosphate The excretion of Cyclic adenosine monophosphate can be decreased when combined with Acyclovir.
Cholic Acid The excretion of Cholic Acid can be decreased when combined with Acyclovir.
Glutaric Acid The excretion of Glutaric Acid can be decreased when combined with Acyclovir.
Oxalic Acid The excretion of Oxalic Acid can be decreased when combined with Acyclovir.
Taurocholic acid The excretion of Taurocholic acid can be decreased when combined with Acyclovir.
Ellagic acid The excretion of Ellagic acid can be decreased when combined with Acyclovir.
Avibactam The excretion of Avibactam can be decreased when combined with Acyclovir.
Eluxadoline The excretion of Eluxadoline can be decreased when combined with Acyclovir.
Silibinin The excretion of Silibinin can be decreased when combined with Acyclovir.
Relebactam The excretion of Relebactam can be decreased when combined with Acyclovir.
Minocycline The excretion of Acyclovir can be decreased when combined with Minocycline.
Novobiocin The excretion of Acyclovir can be decreased when combined with Novobiocin.
Ouabain The excretion of Acyclovir can be decreased when combined with Ouabain.
Liotrix The excretion of Acyclovir can be decreased when combined with Liotrix.
Cilastatin The excretion of Acyclovir can be decreased when combined with Cilastatin.
trans-2-hydroxycinnamic acid The excretion of Acyclovir can be decreased when combined with trans-2-hydroxycinnamic acid.
Benzoic acid The excretion of Acyclovir can be decreased when combined with Benzoic acid.
Caprylic acid The excretion of Acyclovir can be decreased when combined with Caprylic acid.
Ataluren The excretion of Acyclovir can be decreased when combined with Ataluren.
Dabrafenib The excretion of Acyclovir can be decreased when combined with Dabrafenib.
Dolutegravir The excretion of Acyclovir can be decreased when combined with Dolutegravir.
Cabotegravir The excretion of Acyclovir can be decreased when combined with Cabotegravir.
Pradigastat The excretion of Acyclovir can be decreased when combined with Pradigastat.
Cefotiam The excretion of Acyclovir can be decreased when combined with Cefotiam.
Indomethacin The excretion of Acyclovir can be decreased when combined with Indomethacin.
Cefalotin The excretion of Acyclovir can be decreased when combined with Cefalotin.
Tenoxicam The excretion of Acyclovir can be decreased when combined with Tenoxicam.
Cefotaxime The excretion of Acyclovir can be decreased when combined with Cefotaxime.
Piroxicam The excretion of Acyclovir can be decreased when combined with Piroxicam.
Methotrexate The excretion of Acyclovir can be decreased when combined with Methotrexate.
Cephalexin The excretion of Acyclovir can be decreased when combined with Cephalexin.
Valaciclovir The excretion of Valaciclovir can be decreased when combined with Acyclovir.
Diclofenac The excretion of Acyclovir can be decreased when combined with Diclofenac.
Furosemide The excretion of Acyclovir can be decreased when combined with Furosemide.
Oseltamivir The excretion of Oseltamivir can be decreased when combined with Acyclovir.
Pantoprazole The excretion of Acyclovir can be decreased when combined with Pantoprazole.
Liothyronine The excretion of Acyclovir can be decreased when combined with Liothyronine.
Conjugated estrogens The excretion of Acyclovir can be decreased when combined with Conjugated estrogens.
Piperacillin The excretion of Piperacillin can be decreased when combined with Acyclovir.
Trifluridine The excretion of Trifluridine can be decreased when combined with Acyclovir.
Allopurinol The excretion of Allopurinol can be decreased when combined with Acyclovir.
Cimetidine The excretion of Acyclovir can be decreased when combined with Cimetidine.
Levocarnitine The excretion of Levocarnitine can be decreased when combined with Acyclovir.
Tetracycline The excretion of Acyclovir can be decreased when combined with Tetracycline.
Estradiol The excretion of Estradiol can be decreased when combined with Acyclovir.
Cefaclor The excretion of Cefaclor can be decreased when combined with Acyclovir.
Ranitidine The excretion of Ranitidine can be decreased when combined with Acyclovir.
Bumetanide The excretion of Bumetanide can be decreased when combined with Acyclovir.
Acetylsalicylic acid The excretion of Acyclovir can be decreased when combined with Acetylsalicylic acid.
Ganciclovir The excretion of Acyclovir can be decreased when combined with Ganciclovir.
Ketoprofen The excretion of Acyclovir can be decreased when combined with Ketoprofen.
Ibuprofen The excretion of Acyclovir can be decreased when combined with Ibuprofen.
Cefadroxil The excretion of Acyclovir can be decreased when combined with Cefadroxil.
Ceftriaxone The excretion of Acyclovir can be decreased when combined with Ceftriaxone.
Gemfibrozil The excretion of Acyclovir can be decreased when combined with Gemfibrozil.
Sitagliptin The excretion of Sitagliptin can be decreased when combined with Acyclovir.
Ceftibuten The excretion of Ceftibuten can be decreased when combined with Acyclovir.
Topiroxostat The excretion of Acyclovir can be decreased when combined with Topiroxostat.
Doripenem The excretion of Doripenem can be decreased when combined with Acyclovir.
Saxagliptin The excretion of Saxagliptin can be decreased when combined with Acyclovir.
Apalutamide The excretion of Acyclovir can be decreased when combined with Apalutamide.
Phenylbutazone The excretion of Acyclovir can be decreased when combined with Phenylbutazone.
Salicylic acid The excretion of Acyclovir can be decreased when combined with Salicylic acid.
Cefamandole The excretion of Acyclovir can be decreased when combined with Cefamandole.
Cefazolin The excretion of Cefazolin can be decreased when combined with Acyclovir.
Cefoperazone The excretion of Acyclovir can be decreased when combined with Cefoperazone.
Ceftizoxime The excretion of Ceftizoxime can be decreased when combined with Acyclovir.
Cefacetrile The excretion of Cefacetrile can be decreased when combined with Acyclovir.
Cefaloridine The excretion of Cefaloridine can be decreased when combined with Acyclovir.
Dronedarone The excretion of Acyclovir can be decreased when combined with Dronedarone.
Dexamethasone The excretion of Dexamethasone can be decreased when combined with Acyclovir.

Target Protein

DNA polymerase catalytic subunit
DNA polymerase catalytic subunit

Referensi & Sumber

Artikel (PubMed)
  • PMID: 2653790
    O'Brien JJ, Campoli-Richards DM: Acyclovir. An updated review of its antiviral activity, pharmacokinetic properties and therapeutic efficacy. Drugs. 1989 Mar;37(3):233-309.
  • PMID: 22005269
    Gunness P, Aleksa K, Bend J, Koren G: Acyclovir-induced nephrotoxicity: the role of the acyclovir aldehyde metabolite. Transl Res. 2011 Nov;158(5):290-301. doi: 10.1016/j.trsl.2011.07.002. Epub 2011 Aug 3.
  • PMID: 16838235
    Morrel EM, Spruance SL, Goldberg DI: Topical iontophoretic administration of acyclovir for the episodic treatment of herpes labialis: a randomized, double-blind, placebo-controlled, clinic-initiated trial. Clin Infect Dis. 2006 Aug 15;43(4):460-7. Epub 2006 Jul 3.
  • PMID: 20038622
    Smith JP, Weller S, Johnson B, Nicotera J, Luther JM, Haas DW: Pharmacokinetics of acyclovir and its metabolites in cerebrospinal fluid and systemic circulation after administration of high-dose valacyclovir in subjects with normal and impaired renal function. Antimicrob Agents Chemother. 2010 Mar;54(3):1146-51. doi: 10.1128/AAC.00729-09. Epub 2009 Dec 28.
  • PMID: 2828440
    King DH: History, pharmacokinetics, and pharmacology of acyclovir. J Am Acad Dermatol. 1988 Jan;18(1 Pt 2):176-9. doi: 10.1016/s0190-9622(88)70022-5.
  • PMID: 30531673
    Sadjadi SA, Regmi S, Chau T: Acyclovir Neurotoxicity in a Peritoneal Dialysis Patient: Report of a Case and Review of the Pharmacokinetics of Acyclovir. Am J Case Rep. 2018 Dec 9;19:1459-1462. doi: 10.12659/AJCR.911520.
  • PMID: 7159465
    Miller WH, Miller RL: Phosphorylation of acyclovir diphosphate by cellular enzymes. Biochem Pharmacol. 1982 Dec 1;31(23):3879-84. doi: 10.1016/0006-2952(82)90305-7.
  • PMID: 6342900
    Laskin OL: Clinical pharmacokinetics of acyclovir. Clin Pharmacokinet. 1983 May-Jun;8(3):187-201. doi: 10.2165/00003088-198308030-00001.
Menampilkan 8 dari 9 artikel.

Contoh Produk & Brand

Produk: 595 • International brands: 1
Produk
  • Acyclovir
    Capsule • 200 mg/1 • Oral • US • Generic • Approved
  • Acyclovir
    Tablet • 400 mg/1 • Oral • US • Generic • Approved
  • Acyclovir
    Tablet • 800 mg/1 • Oral • US • Generic • Approved
  • Acyclovir
    Suspension • 200 mg/5mL • Oral • US • Generic • Approved
  • Acyclovir
    Capsule • 200 mg/1 • Oral • US • Generic • Approved
  • Acyclovir
    Tablet • 400.00 mg/1 • Oral • US • Generic • Approved
  • Acyclovir
    Tablet • 800.00 mg/1 • Oral • US • Generic • Approved
  • Acyclovir
    Tablet • 800 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 595 produk.
International Brands
  • Zovir

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