Peringatan Keamanan

There haven't been reports regarding the LD50 of the parent compound nor the effects of an overdose. However, based on the reports with the derivative that most rapidly transforms into tenofovir, tenofovir disoproxil, it is recommended to monitor overdose patients. As well, it is widely known that tenofovir is efficiently removed by hemodialysis.A178528

Administration of high doses of tenofovir has been reported to produce bone toxicity reported as osteomalacia and reduced bone mineral density and to produce some degree of renal toxicity.L6346

To know more about the carcinogenicity and mutagenic potential of tenofovir, as well as the effect on fertility, please visit the drug entries for the derivatives tenofovir disoproxil and tenofovir alafenamide.

Tenofovir

DB14126

small molecule experimental investigational

Deskripsi

Tenofovir is an acyclic nucleotide diester analog of adenosine monophosphate.A37693 In the most strict sense and due to the fact that it presents a phosphate group bound to the nitrogenous base, it is determined as an actual nucleotide analog.A37693 The antiviral activities of tenofovir were first reported in 1993 and this agent was commercially available since 2008 in the form of tenofovir disoproxil and tenofovir alafenamide in order to obtain oral bioavailability.A18473, A178360

Struktur Molekul 2D

Berat 287.2123
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The reported half-life of tenofovir is of 32 hours.[A178231]
Volume Distribusi Accumulation of tenofovir in plasma is related to the presence of nephrotoxic effects.[A178060] It is reported that tenofovir presents a volume of distribution of 0.813 L/kg.[A16539]
Klirens (Clearance) The clearance of tenofovir is highly dependent on the patient renal stage and hence the clearance rate in patients with renal impairment is reported to be of 134 ml/min while in patients with normal function the clearance rate can be of 210 ml/min.[A178525]

Absorpsi

Tenofovir as the active moiety presents a very low bioavailability when orally administered. Hence, the administration of this active agent is required to be under its two prodrug forms, tenofovir disoproxil and tenofovir alafenamide. This reduced absorption is suggested to be related to the presence of two negative charges among its structure. This negative charge limits its cellular penetration, and its passive diffusion across cellular membranes and intestinal mucosa hindering its availability for oral administration.A178060 Intravenous tenofovir has been shown to produce a maximum plasma concentration of 2500 ng/ml with an AUC of 4800 ng.h/ml.A18473

Metabolisme

Tenofovir activation is performed by a bi-phosphorylation which in order forms the biologically active compound, tenofovir biphosphate.A178060 This metabolic activation has been shown to be performed in hepG2 cells and human hepatocytes.A174640

Rute Eliminasi

Tenofovir is eliminated in the urine by tubular secretion and glomerular filtration. The elimination of this compound is driven by the activity of the human organic anion transporters 1 and 3 and its secretion is mainly ruled by the activity of the multidrug resistance-associated protein 4.A178060

Interaksi Makanan

1 Data
  • 1. Take with food.

Interaksi Obat

989 Data
Ranolazine The serum concentration of Tenofovir can be increased when it is combined with Ranolazine.
Atazanavir The serum concentration of Atazanavir can be decreased when it is combined with Tenofovir.
Cobicistat The serum concentration of Tenofovir can be increased when it is combined with Cobicistat.
Darunavir The serum concentration of Darunavir can be increased when it is combined with Tenofovir.
Didanosine The serum concentration of Didanosine can be increased when it is combined with Tenofovir.
Simeprevir The serum concentration of Simeprevir can be decreased when it is combined with Tenofovir.
Telaprevir The serum concentration of Tenofovir can be increased when it is combined with Telaprevir.
Tipranavir The serum concentration of Tipranavir can be decreased when it is combined with Tenofovir.
Taxifolin Taxifolin may decrease the excretion rate of Tenofovir which could result in a higher serum level.
Licofelone Licofelone may decrease the excretion rate of Tenofovir which could result in a higher serum level.
Polmacoxib Polmacoxib may decrease the excretion rate of Tenofovir which could result in a higher serum level.
Ebselen Ebselen may decrease the excretion rate of Tenofovir which could result in a higher serum level.
Flurbiprofen axetil Flurbiprofen axetil may decrease the excretion rate of Tenofovir which could result in a higher serum level.
Ribavirin Ribavirin may increase the hepatotoxic activities of Tenofovir.
Foscarnet The risk or severity of nephrotoxicity can be increased when Tenofovir is combined with Foscarnet.
Mannitol The risk or severity of nephrotoxicity can be increased when Mannitol is combined with Tenofovir.
Icosapent Icosapent may increase the nephrotoxic activities of Tenofovir.
Cefotiam Cefotiam may increase the nephrotoxic activities of Tenofovir.
Mesalazine The risk or severity of nephrotoxicity can be increased when Mesalazine is combined with Tenofovir.
Cefmenoxime Cefmenoxime may increase the nephrotoxic activities of Tenofovir.
Cefmetazole Cefmetazole may increase the nephrotoxic activities of Tenofovir.
Pamidronic acid Pamidronic acid may increase the nephrotoxic activities of Tenofovir.
Tenofovir disoproxil Tenofovir disoproxil may increase the nephrotoxic activities of Tenofovir.
Indomethacin Indomethacin may increase the nephrotoxic activities of Tenofovir.
Cidofovir Cidofovir may increase the nephrotoxic activities of Tenofovir.
Triamterene Triamterene may increase the nephrotoxic activities of Tenofovir.
Cefpiramide Cefpiramide may increase the nephrotoxic activities of Tenofovir.
Ceftazidime Ceftazidime may increase the nephrotoxic activities of Tenofovir.
Loracarbef Loracarbef may increase the nephrotoxic activities of Tenofovir.
Framycetin Framycetin may increase the nephrotoxic activities of Tenofovir.
Cefalotin Cefalotin may increase the nephrotoxic activities of Tenofovir.
Nabumetone Nabumetone may increase the nephrotoxic activities of Tenofovir.
Ketorolac Ketorolac may increase the nephrotoxic activities of Tenofovir.
Tenoxicam Tenoxicam may increase the nephrotoxic activities of Tenofovir.
Amikacin Amikacin may increase the nephrotoxic activities of Tenofovir.
Celecoxib Celecoxib may increase the nephrotoxic activities of Tenofovir.
Cefotaxime Cefotaxime may increase the nephrotoxic activities of Tenofovir.
Tolmetin Tolmetin may increase the nephrotoxic activities of Tenofovir.
Rofecoxib Rofecoxib may increase the nephrotoxic activities of Tenofovir.
Piroxicam Piroxicam may increase the nephrotoxic activities of Tenofovir.
Methotrexate Methotrexate may increase the nephrotoxic activities of Tenofovir.
Cephalexin Cephalexin may increase the nephrotoxic activities of Tenofovir.
Fenoprofen Fenoprofen may increase the nephrotoxic activities of Tenofovir.
Valaciclovir Valaciclovir may increase the nephrotoxic activities of Tenofovir.
Valdecoxib Valdecoxib may increase the nephrotoxic activities of Tenofovir.
Diclofenac Diclofenac may increase the nephrotoxic activities of Tenofovir.
Sulindac Sulindac may increase the nephrotoxic activities of Tenofovir.
Bacitracin Bacitracin may increase the nephrotoxic activities of Tenofovir.
Amphotericin B Amphotericin B may increase the nephrotoxic activities of Tenofovir.
Tobramycin Tobramycin may increase the nephrotoxic activities of Tenofovir.
Cephaloglycin Cephaloglycin may increase the nephrotoxic activities of Tenofovir.
Furosemide Furosemide may increase the nephrotoxic activities of Tenofovir.
Flurbiprofen Flurbiprofen may increase the nephrotoxic activities of Tenofovir.
Pentamidine Pentamidine may increase the nephrotoxic activities of Tenofovir.
Etodolac Etodolac may increase the nephrotoxic activities of Tenofovir.
Mefenamic acid Mefenamic acid may increase the nephrotoxic activities of Tenofovir.
Acyclovir Acyclovir may increase the nephrotoxic activities of Tenofovir.
Naproxen Naproxen may increase the nephrotoxic activities of Tenofovir.
Sulfasalazine Sulfasalazine may increase the nephrotoxic activities of Tenofovir.
Gentamicin Gentamicin may increase the nephrotoxic activities of Tenofovir.
Phenylbutazone Phenylbutazone may increase the nephrotoxic activities of Tenofovir.
Meloxicam Meloxicam may increase the nephrotoxic activities of Tenofovir.
Carprofen Carprofen may increase the nephrotoxic activities of Tenofovir.
Cefaclor Cefaclor may increase the nephrotoxic activities of Tenofovir.
Diflunisal Diflunisal may increase the nephrotoxic activities of Tenofovir.
Bumetanide Bumetanide may increase the nephrotoxic activities of Tenofovir.
Etacrynic acid Etacrynic acid may increase the nephrotoxic activities of Tenofovir.
Ceforanide Ceforanide may increase the nephrotoxic activities of Tenofovir.
Salicylic acid Salicylic acid may increase the nephrotoxic activities of Tenofovir.
Meclofenamic acid Meclofenamic acid may increase the nephrotoxic activities of Tenofovir.
Acetylsalicylic acid Acetylsalicylic acid may increase the nephrotoxic activities of Tenofovir.
Netilmicin Netilmicin may increase the nephrotoxic activities of Tenofovir.
Carboplatin Carboplatin may increase the nephrotoxic activities of Tenofovir.
Oxaprozin Oxaprozin may increase the nephrotoxic activities of Tenofovir.
Hydrochlorothiazide Hydrochlorothiazide may increase the nephrotoxic activities of Tenofovir.
Ketoprofen Ketoprofen may increase the nephrotoxic activities of Tenofovir.
Balsalazide Balsalazide may increase the nephrotoxic activities of Tenofovir.
Ibuprofen Ibuprofen may increase the nephrotoxic activities of Tenofovir.
Cefditoren Cefditoren may increase the nephrotoxic activities of Tenofovir.
Streptomycin Streptomycin may increase the nephrotoxic activities of Tenofovir.
Colistimethate Colistimethate may increase the nephrotoxic activities of Tenofovir.
Cefuroxime Cefuroxime may increase the nephrotoxic activities of Tenofovir.
Cefapirin Cefapirin may increase the nephrotoxic activities of Tenofovir.
Cefadroxil Cefadroxil may increase the nephrotoxic activities of Tenofovir.
Cefprozil Cefprozil may increase the nephrotoxic activities of Tenofovir.
Kanamycin Kanamycin may increase the nephrotoxic activities of Tenofovir.
Ceftriaxone Ceftriaxone may increase the nephrotoxic activities of Tenofovir.
Olsalazine The risk or severity of nephrotoxicity can be increased when Tenofovir is combined with Olsalazine.
Lumiracoxib Lumiracoxib may increase the nephrotoxic activities of Tenofovir.
Cefamandole Cefamandole may increase the nephrotoxic activities of Tenofovir.
Cefazolin Cefazolin may increase the nephrotoxic activities of Tenofovir.
Cefonicid Cefonicid may increase the nephrotoxic activities of Tenofovir.
Cefoperazone Cefoperazone may increase the nephrotoxic activities of Tenofovir.
Cefotetan Cefotetan may increase the nephrotoxic activities of Tenofovir.
Cefoxitin Cefoxitin may increase the nephrotoxic activities of Tenofovir.
Ceftizoxime Ceftizoxime may increase the nephrotoxic activities of Tenofovir.
Cefradine Cefradine may increase the nephrotoxic activities of Tenofovir.
Magnesium salicylate Magnesium salicylate may increase the nephrotoxic activities of Tenofovir.
Salsalate Salsalate may increase the nephrotoxic activities of Tenofovir.
Choline magnesium trisalicylate Choline magnesium trisalicylate may increase the nephrotoxic activities of Tenofovir.

Target Protein

Reverse transcriptase/RNaseH pol
Gag-Pol polyprotein gag-pol
Reverse transcriptase rt
DNA polymerase

Referensi & Sumber

Artikel (PubMed)
  • PMID: 27438578
    Aloy B, Tazi I, Bagnis CI, Gauthier M, Janus N, Launay-Vacher V, Deray G, Tourret J: Is Tenofovir Alafenamide Safer than Tenofovir Disoproxil Fumarate for the Kidneys? AIDS Rev. 2016 Oct-Dec;18(4):184-192.
  • PMID: 30460547
    Deeks ED: Bictegravir/Emtricitabine/Tenofovir Alafenamide: A Review in HIV-1 Infection. Drugs. 2018 Nov;78(17):1817-1828. doi: 10.1007/s40265-018-1010-7.
  • PMID: 26640223
    Ray AS, Fordyce MW, Hitchcock MJ: Tenofovir alafenamide: A novel prodrug of tenofovir for the treatment of Human Immunodeficiency Virus. Antiviral Res. 2016 Jan;125:63-70. doi: 10.1016/j.antiviral.2015.11.009. Epub 2015 Nov 27.
  • PMID: 23963694
    Margolis AM, Heverling H, Pham PA, Stolbach A: A review of the toxicity of HIV medications. J Med Toxicol. 2014 Mar;10(1):26-39. doi: 10.1007/s13181-013-0325-8.
  • PMID: 24741339
    McConville C, Boyd P, Major I: Efficacy of Tenofovir 1% Vaginal Gel in Reducing the Risk of HIV-1 and HSV-2 Infection. Clin Med Insights Womens Health. 2014 Feb 13;7:1-8. doi: 10.4137/CMWH.S10353. eCollection 2014.
  • PMID: 24966587
    Ridruejo E: Treatment of chronic hepatitis B in clinical practice with entecavir or tenofovir. World J Gastroenterol. 2014 Jun 21;20(23):7169-80. doi: 10.3748/wjg.v20.i23.7169.
  • PMID: 12462284
    Fung HB, Stone EA, Piacenti FJ: Tenofovir disoproxil fumarate: a nucleotide reverse transcriptase inhibitor for the treatment of HIV infection. Clin Ther. 2002 Oct;24(10):1515-48.
  • PMID: 16801428
    Delaney WE 4th, Ray AS, Yang H, Qi X, Xiong S, Zhu Y, Miller MD: Intracellular metabolism and in vitro activity of tenofovir against hepatitis B virus. Antimicrob Agents Chemother. 2006 Jul;50(7):2471-7. doi: 10.1128/AAC.00138-06.
Menampilkan 8 dari 10 artikel.
Textbook
  • Sivapalasingam S., Steigbigel N. (2015). Mandell, Douglas and Bennett's Principles and practice of infectious diseases (8th ed.). Elsevier.

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