Peringatan Keamanan

Oral TDLO (human female): 100 ug/kg, Oral TDLO (human male): 75 ug/kg, Oral LD50 (rat): 28270 ug/kgMSDS

Digoxin toxicity can occur in cases of supratherapeutic dose ingestion or as a result of chronic overexposure.T607 Digoxin toxicity may be manifested by symptoms of nausea, vomiting, visual changes, in addition to arrhythmia. Older age, lower body weight, and decreased renal function or electrolyte abnormalities lead to an increased risk of digoxin toxicity.L9143

Digoxin

DB00390

small molecule approved

Deskripsi

Digoxin is one of the oldest cardiovascular medications used today.A178225 It is a common agent used to manage atrial fibrillation and the symptoms of heart failure.A178234 Digoxin is classified as a cardiac glycoside and was initially approved by the FDA in 1954.L9143

This drug originates from the foxglove plant, also known as the Digitalis plantT610, studied by William Withering, an English physician and botanist in the 1780s.A178237,A178240 Prior to this, a Welsh family, historically referred to as the Physicians of Myddvai, formulated drugs from this plant. They were one of the first to prescribe cardiac glycosides, according to ancient literature dating as early as the 1250s.A178240

Struktur Molekul 2D

Berat 780.9385
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Digoxin has a half-life of 1.5-2 days in healthy subjects.[L9143] The half-life in patients who do not pass urine, usually due to renal failure, is prolonged to 3.5-5 days. Since most of the drug is distributed extravascularly, dialysis and exchange transfusion are not optimal methods for the removal of digoxin.[L9143]
Volume Distribusi This drug is widely distributed in the body, and is known to cross the blood-brain barrier and the placenta.[L9143,A178228] The apparent volume of distribution of digoxin is 475-500 L.[L9143] A large portion of digoxin is distributed in the skeletal muscle followed by the heart and kidneys.[A178228] It is important to note that the elderly population, generally having a decreased muscle mass, may show a lower volume of digoxin distribution.[L9143]
Klirens (Clearance) The clearance of digoxin closely correlates to creatinine clearance, and does not depend on urinary flow. Individuals with renal impairment or failure may exhibit extensively prolonged half-lives. It is therefore important to titrate the dose accordingly and regularly monitor serum digoxin levels.[L9143] One pharmacokinetic study measured the mean body clearance of intravenous digoxin to be 88 ± 44ml/min/l.73 m².[A178324] Another study provided mean clearance values of 53 ml/min/1.73 m² in men aged 73-81 and 83 ml/min/1.73 m² in men aged 20-33 years old after an intravenous digoxin dose.[A178318]

Absorpsi

Digoxin is approximately 70-80% absorbed in the first part of the small bowel.A178228 The bioavailability of an oral dose varies from 50-90%, however, oral gelatinized capsules of digoxin are reported to have a bioavailability of 100%.A178252 Tmax, or the time to reach the maximum concentration of digoxin was measured to be 1.0 h in one clinical study of healthy patients taking 0.25 mg of digoxin with a placebo.A178369 Cmax, or maximum concentration, was 1.32 ± 0.18 ng/ml?1 in the same study, and AUC (area under the curve) was 12.5 ± 2.38 ng/ml?1.A178369 If digoxin is ingested after a meal, absorption is slowed but this does not change the total amount of absorbed drug. If digoxin is taken with meals that are in fiber, absorption may be decreased.L6274 A note on gut bacteria An oral dose of digoxin may be transformed into pharmacologically inactive products by bacteria in the colon. Studies have indicated that 10% of patients receiving digoxin tablets will experience the degradation of at least 40% of an ingested dose of digoxin by gut bacteria. Several antibiotics may increase the absorption of digoxin in these patients, due to the elimination of gut bacteria, which normally cause digoxin degradation.L9143 A note on malabsorption Patients with malabsorption due to a variety of causes may have a decreased ability to absorb digoxin.L9143 P-glycoprotein, located on cells in the intestine, may interfere with digoxin pharmacokinetics, as it is a substrate of this efflux transporter. P-glycoprotein can be induced by other drugs, therefore reducing the effects of digoxin by increasing its efflux in the intestine.L9143

Metabolisme

About 13% of a digoxin dose is found to be metabolized in healthy subjects. Several urinary metabolites of digoxin exist, including dihydrodigoxin and digoxigenin bisdigitoxoside. Their glucuronidated and sulfated conjugates are thought to be produced through the process of hydrolysis, oxidation, and additionally, conjugation. The cytochrome P-450 system does not play a major role in digoxin metabolism, nor does this drug induce or inhibit the enzymes in this system.L9143

Rute Eliminasi

The elimination of digoxin is proportional to the total dose, following first order kinetics. After intravenous (IV) administration to healthy subjects, 50-70% of the dose is measured excreted as unchanged digoxin in the urine. Approximately 25 to 28% of digoxin is eliminated outside of the kidney. Biliary excretion appears to be of much less importance than renal excretion.A178228 Digoxin is not effectively removed from the body by dialysis, exchange transfusion, or during cardiopulmonary bypass because most of the drug is bound to extravascular tissues.L9143

Interaksi Makanan

4 Data
  • 1. Avoid multivalent ions. Calcium and aluminum containing products (including kaolin-pectin) may interfere with absorption) and digoxin administration must be separated by several hours.
  • 2. Avoid potassium-containing products. They may cause arrhythmias when given with digoxin.
  • 3. Avoid St. John's Wort. This drug can decrease digoxin levels.
  • 4. Do not take with bran and high fiber foods. Separate administration of bran and high fiber foods from medication by at least 2 hours.

Interaksi Obat

1675 Data
Cyclosporine The serum concentration of Digoxin can be increased when it is combined with Cyclosporine.
Ceritinib Digoxin may increase the bradycardic activities of Ceritinib.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Digoxin.
Acarbose The serum concentration of Digoxin can be decreased when it is combined with Acarbose.
Icosapent Icosapent may decrease the excretion rate of Digoxin which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Digoxin which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Digoxin which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Digoxin which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Digoxin which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Digoxin which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Digoxin which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Digoxin which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Digoxin which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Digoxin which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Digoxin which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Digoxin which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Digoxin which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Digoxin which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Digoxin which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Digoxin which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Digoxin which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Digoxin which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Digoxin which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Digoxin which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Digoxin which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Digoxin which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Digoxin which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Digoxin which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Digoxin which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Digoxin which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Digoxin which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Digoxin which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Digoxin which could result in a higher serum level.
Antrafenine Antrafenine may decrease the excretion rate of Digoxin which could result in a higher serum level.
Aminophenazone Aminophenazone may decrease the excretion rate of Digoxin which could result in a higher serum level.
Antipyrine Antipyrine may decrease the excretion rate of Digoxin which could result in a higher serum level.
Tiaprofenic acid Tiaprofenic acid may decrease the excretion rate of Digoxin which could result in a higher serum level.
Etoricoxib Etoricoxib may decrease the excretion rate of Digoxin which could result in a higher serum level.
Taxifolin Taxifolin may decrease the excretion rate of Digoxin which could result in a higher serum level.
Oxyphenbutazone Oxyphenbutazone may decrease the excretion rate of Digoxin which could result in a higher serum level.
Licofelone Licofelone may decrease the excretion rate of Digoxin which could result in a higher serum level.
Nimesulide Nimesulide may decrease the excretion rate of Digoxin which could result in a higher serum level.
Benoxaprofen Benoxaprofen may decrease the excretion rate of Digoxin which could result in a higher serum level.
Metamizole Metamizole may decrease the excretion rate of Digoxin which could result in a higher serum level.
Zomepirac Zomepirac may decrease the excretion rate of Digoxin which could result in a higher serum level.
Cimicoxib Cimicoxib may decrease the excretion rate of Digoxin which could result in a higher serum level.
Lornoxicam Lornoxicam may decrease the excretion rate of Digoxin which could result in a higher serum level.
Aceclofenac Aceclofenac may decrease the excretion rate of Digoxin which could result in a higher serum level.
Zaltoprofen Zaltoprofen may decrease the excretion rate of Digoxin which could result in a higher serum level.
Azapropazone Azapropazone may decrease the excretion rate of Digoxin which could result in a higher serum level.
Parecoxib Parecoxib may decrease the excretion rate of Digoxin which could result in a higher serum level.
Salicylamide Salicylamide may decrease the excretion rate of Digoxin which could result in a higher serum level.
Kebuzone Kebuzone may decrease the excretion rate of Digoxin which could result in a higher serum level.
Isoxicam Isoxicam may decrease the excretion rate of Digoxin which could result in a higher serum level.
Indoprofen Indoprofen may decrease the excretion rate of Digoxin which could result in a higher serum level.
Ibuproxam Ibuproxam may decrease the excretion rate of Digoxin which could result in a higher serum level.
Floctafenine Floctafenine may decrease the excretion rate of Digoxin which could result in a higher serum level.
Fenbufen Fenbufen may decrease the excretion rate of Digoxin which could result in a higher serum level.
Etofenamate Etofenamate may decrease the excretion rate of Digoxin which could result in a higher serum level.
Epirizole Epirizole may decrease the excretion rate of Digoxin which could result in a higher serum level.
Benzydamine Benzydamine may decrease the excretion rate of Digoxin which could result in a higher serum level.
Dexibuprofen Dexibuprofen may decrease the excretion rate of Digoxin which could result in a higher serum level.
Dexketoprofen Dexketoprofen may decrease the excretion rate of Digoxin which could result in a higher serum level.
Droxicam Droxicam may decrease the excretion rate of Digoxin which could result in a higher serum level.
Tolfenamic acid Tolfenamic acid may decrease the excretion rate of Digoxin which could result in a higher serum level.
Firocoxib Firocoxib may decrease the excretion rate of Digoxin which could result in a higher serum level.
Clonixin Clonixin may decrease the excretion rate of Digoxin which could result in a higher serum level.
Morniflumate Morniflumate may decrease the excretion rate of Digoxin which could result in a higher serum level.
Propacetamol Propacetamol may decrease the excretion rate of Digoxin which could result in a higher serum level.
Talniflumate Talniflumate may decrease the excretion rate of Digoxin which could result in a higher serum level.
Robenacoxib Robenacoxib may decrease the excretion rate of Digoxin which could result in a higher serum level.
Tepoxalin Tepoxalin may decrease the excretion rate of Digoxin which could result in a higher serum level.
Flunixin Flunixin may decrease the excretion rate of Digoxin which could result in a higher serum level.
Polmacoxib Polmacoxib may decrease the excretion rate of Digoxin which could result in a higher serum level.
Nitroaspirin Nitroaspirin may decrease the excretion rate of Digoxin which could result in a higher serum level.
Indobufen Indobufen may decrease the excretion rate of Digoxin which could result in a higher serum level.
Ebselen Ebselen may decrease the excretion rate of Digoxin which could result in a higher serum level.
Tinoridine Tinoridine may decrease the excretion rate of Digoxin which could result in a higher serum level.
Alclofenac Alclofenac may decrease the excretion rate of Digoxin which could result in a higher serum level.
Fentiazac Fentiazac may decrease the excretion rate of Digoxin which could result in a higher serum level.
Suxibuzone Suxibuzone may decrease the excretion rate of Digoxin which could result in a higher serum level.
Bumadizone Bumadizone may decrease the excretion rate of Digoxin which could result in a higher serum level.
Alminoprofen Alminoprofen may decrease the excretion rate of Digoxin which could result in a higher serum level.
Difenpiramide Difenpiramide may decrease the excretion rate of Digoxin which could result in a higher serum level.
Nifenazone Nifenazone may decrease the excretion rate of Digoxin which could result in a higher serum level.
Lonazolac Lonazolac may decrease the excretion rate of Digoxin which could result in a higher serum level.
Tenidap Tenidap may decrease the excretion rate of Digoxin which could result in a higher serum level.
Propyphenazone Propyphenazone may decrease the excretion rate of Digoxin which could result in a higher serum level.
Proglumetacin Proglumetacin may decrease the excretion rate of Digoxin which could result in a higher serum level.
Guacetisal Guacetisal may decrease the excretion rate of Digoxin which could result in a higher serum level.
Ethenzamide Ethenzamide may decrease the excretion rate of Digoxin which could result in a higher serum level.
Carbaspirin calcium Carbaspirin calcium may decrease the excretion rate of Digoxin which could result in a higher serum level.
Mofebutazone Mofebutazone may decrease the excretion rate of Digoxin which could result in a higher serum level.
Proquazone Proquazone may decrease the excretion rate of Digoxin which could result in a higher serum level.
Benorilate Benorilate may decrease the excretion rate of Digoxin which could result in a higher serum level.
Pirprofen Pirprofen may decrease the excretion rate of Digoxin which could result in a higher serum level.
Acemetacin Acemetacin may decrease the excretion rate of Digoxin which could result in a higher serum level.
Imidazole salicylate Imidazole salicylate may decrease the excretion rate of Digoxin which could result in a higher serum level.
SC-236 SC-236 may decrease the excretion rate of Digoxin which could result in a higher serum level.
NS-398 NS-398 may decrease the excretion rate of Digoxin which could result in a higher serum level.

Target Protein

Sodium/potassium-transporting ATPase subunit alpha-2 ATP1A2
Sodium/potassium-transporting ATPase subunit alpha-3 ATP1A3
Sodium/potassium-transporting ATPase subunit beta-1 ATP1B1
Sodium/potassium-transporting ATPase subunit beta-2 ATP1B2
Sodium/potassium-transporting ATPase subunit beta-3 ATP1B3
Solute carrier organic anion transporter family member 4C1 SLCO4C1
Sodium/potassium-transporting ATPase subunit alpha-1 ATP1A1

Referensi & Sumber

Synthesis reference: Wolfgang Voigtlander, Fritz Kaiser, Wolfgang Schaumann, Kurt Stach, "Preparation of C22-alkyl derivative of digoxin." U.S. Patent US3981862, issued October, 1972.
Artikel (PubMed)
Menampilkan 8 dari 19 artikel.
Textbook
  • Rameez Rehman; Ofek Hai. (2018). Digitalis Toxicity. StatPearls Publishing.
  • IARC Working Group on the Evaluation of Carcinogenic Risk to Humans. Lyon (FR) (2016). Some Drugs and Herbal Products. International Agency for Research on Cancer.
  • A Kosaraju (2019). Left Ventricular Ejection Fraction. StatPearls.

Contoh Produk & Brand

Produk: 232 • International brands: 17
Produk
  • Apo-digoxin
    Tablet • 0.25 mg • Oral • Canada • Generic • Approved
  • Apo-digoxin
    Tablet • 0.125 mg • Oral • Canada • Generic • Approved
  • Apo-digoxin
    Tablet • 0.0625 mg • Oral • Canada • Generic • Approved
  • Digitek
    Tablet • 0.125 mg/1 • Oral • US • Generic • Approved
  • Digitek
    Tablet • 0.25 mg/1 • Oral • US • Generic • Approved
  • Digitek
    Tablet • 0.125 mg/1 • Oral • US • Generic • Approved
  • Digitek
    Tablet • 0.25 mg/1 • Oral • US • Generic • Approved
  • Digox
    Tablet • 250 ug/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 232 produk.
International Brands
  • Agoxin — Aristopharma
  • Cardiacin — Center
  • Cardiogoxin — Medipharma
  • Cardioxin — Oboi
  • Cardoxin
  • Celoxin — Celon
  • Centoxin — Opsonin
  • Digacin — mibe
  • Digazolan
  • Digocard-G — Klonal

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