Peringatan Keamanan

Oral LD50 in rat and mouse are 965 mg/kg and 841 mg/kg, respectively. Intraperitoneal LD50 in rat and mouse are 426 mg/kg and 396 mg/kg, respectively MSDS.

Doxofylline

DB09273

small molecule experimental

Deskripsi

Doxofylline is a methylxanthine derivative with the presence of a dioxolane group in position 7. As a drug used in the treatment of asthma, doxofylline has shown similar efficacy to theophylline but with significantly fewer side effects in animal and human studies. In contrast with other xanthine derivatives, doxofylline does not significantly bind to adenosine alpha-1 or alpha-2 receptors and lacks stimulating effects. Decreased affinity for adenosine receptors may account for the better safety profile of doxofylline compared to theophylline L1169. Unlike theophylline, doxofylline does not affect calcium influx and does not antagonize the actions of calcium channel blockers which could explain reduced cardiac adverse reactions associated with the drug A7885. The anti-asthmatic effects of doxophylline are mediated by other mechanisms, primarily through inhibiting the activities of the phosphodiesterase (PDE) enzyme.

Struktur Molekul 2D

Berat 266.257
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following administration of a single intravenous dose of 100 mg over 10 minutes in adults with chronic bronchitis, the elimination half life of doxofylline was 1.83 ± 0.37 hours. Following oral administration of 400 mg twice daily for 5 days in adults with chronic bronchitis, the mean elimination half life was 7.01 ± 0.80 hours [L1169].
Volume Distribusi Doxofylline demonstrates a short distribution phase following intravenous administration of 100 mg given in adults with chronic bronchitis [L1169]. As methylxanthines are distributed to all body compartments, doxofylline may be detected in breast milk and placenta [L1169].
Klirens (Clearance) Following oral administration of 400 mg doxofylline twice daily for 5 days, the total clearance was 555.2 ± 180.6 mL/min [L1169].

Absorpsi

After repeated administrations doxofylline reaches the steady-state in about 4 days. Following oral administration of 400 mg doxofylline twice daily for 5 days in adults with chronic bronchitis, the peak plasma concentrations (Cmax) at steady state ranged from 5.78 to 20.76 mcg/mL. The time to reach maximum concentration (Tmax) was 1.19 ± 0.19 hours L1169. The absolute bioavailability of doxofylline in healthy subjects was 63 ± 25% L1169.

Metabolisme

Doxofylline is thought to undergo hepatic metabolism which accounts for 90% of total drug clearance L1171. ?-hydroxymethyltheophylline was detected in the serum and urine after oral administration of 400 mg given in healthy subjects. The circulating metabolite was devoid of any significant pharmacological activity L1169.

Rute Eliminasi

Less than 4% of an orally administered dose is excreted unchanged in the urine due to extensive hepatic metabolism L1171.

Interaksi Obat

1273 Data
Deferasirox The serum concentration of Doxofylline can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Doxofylline can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Doxofylline can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Doxofylline can be decreased when it is combined with Teriflunomide.
Azilsartan medoxomil Doxofylline may decrease the antihypertensive activities of Azilsartan medoxomil.
Levamlodipine Doxofylline may decrease the antihypertensive activities of Levamlodipine.
Regadenoson Doxofylline may decrease effectiveness of Regadenoson as a diagnostic agent.
Alprostadil The risk or severity of hypotension and priapism can be increased when Doxofylline is combined with Alprostadil.
Amyl Nitrite The risk or severity of hypotension can be increased when Doxofylline is combined with Amyl Nitrite.
Dapoxetine The risk or severity of orthostatic hypotension can be increased when Dapoxetine is combined with Doxofylline.
Riociguat Doxofylline may increase the hypotensive activities of Riociguat.
Desmopressin The risk or severity of hypertension can be increased when Desmopressin is combined with Doxofylline.
Cyclosporine The risk or severity of hypertension can be increased when Cyclosporine is combined with Doxofylline.
Icosapent The risk or severity of hypertension can be increased when Icosapent is combined with Doxofylline.
Eletriptan The risk or severity of hypertension can be increased when Eletriptan is combined with Doxofylline.
Mesalazine The risk or severity of hypertension can be increased when Mesalazine is combined with Doxofylline.
Etomidate The risk or severity of hypertension can be increased when Etomidate is combined with Doxofylline.
Indomethacin The risk or severity of hypertension can be increased when Indomethacin is combined with Doxofylline.
Methylphenidate The risk or severity of hypertension can be increased when Methylphenidate is combined with Doxofylline.
Ketorolac The risk or severity of hypertension can be increased when Ketorolac is combined with Doxofylline.
Tenoxicam The risk or severity of hypertension can be increased when Tenoxicam is combined with Doxofylline.
Celecoxib The risk or severity of hypertension can be increased when Celecoxib is combined with Doxofylline.
Buspirone The risk or severity of hypertension can be increased when Buspirone is combined with Doxofylline.
Tolmetin The risk or severity of hypertension can be increased when Tolmetin is combined with Doxofylline.
Piroxicam The risk or severity of hypertension can be increased when Piroxicam is combined with Doxofylline.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Doxofylline.
Atropine The risk or severity of hypertension can be increased when Atropine is combined with Doxofylline.
Fenoprofen The risk or severity of hypertension can be increased when Fenoprofen is combined with Doxofylline.
Valdecoxib The risk or severity of hypertension can be increased when Valdecoxib is combined with Doxofylline.
Sulindac The risk or severity of hypertension can be increased when Sulindac is combined with Doxofylline.
Sumatriptan The risk or severity of hypertension can be increased when Sumatriptan is combined with Doxofylline.
Sufentanil The risk or severity of hypertension can be increased when Sufentanil is combined with Doxofylline.
Flurbiprofen The risk or severity of hypertension can be increased when Flurbiprofen is combined with Doxofylline.
Etodolac The risk or severity of hypertension can be increased when Etodolac is combined with Doxofylline.
Isoflurane The risk or severity of hypertension can be increased when Isoflurane is combined with Doxofylline.
Sulfasalazine The risk or severity of hypertension can be increased when Sulfasalazine is combined with Doxofylline.
Alfentanil The risk or severity of hypertension can be increased when Alfentanil is combined with Doxofylline.
Phenylbutazone The risk or severity of hypertension can be increased when Phenylbutazone is combined with Doxofylline.
Fentanyl The risk or severity of hypertension can be increased when Fentanyl is combined with Doxofylline.
Meloxicam The risk or severity of hypertension can be increased when Meloxicam is combined with Doxofylline.
Carprofen The risk or severity of hypertension can be increased when Carprofen is combined with Doxofylline.
Diflunisal The risk or severity of hypertension can be increased when Diflunisal is combined with Doxofylline.
Remifentanil The risk or severity of hypertension can be increased when Remifentanil is combined with Doxofylline.
Almotriptan The risk or severity of hypertension can be increased when Almotriptan is combined with Doxofylline.
Salicylic acid The risk or severity of hypertension can be increased when Salicylic acid is combined with Doxofylline.
Meclofenamic acid The risk or severity of hypertension can be increased when Meclofenamic acid is combined with Doxofylline.
Acetylsalicylic acid The risk or severity of hypertension can be increased when Acetylsalicylic acid is combined with Doxofylline.
Naratriptan The risk or severity of hypertension can be increased when Naratriptan is combined with Doxofylline.
Rizatriptan The risk or severity of hypertension can be increased when Rizatriptan is combined with Doxofylline.
Oxaprozin The risk or severity of hypertension can be increased when Oxaprozin is combined with Doxofylline.
Ketoprofen The risk or severity of hypertension can be increased when Ketoprofen is combined with Doxofylline.
Balsalazide The risk or severity of hypertension can be increased when Balsalazide is combined with Doxofylline.
Methoxyflurane The risk or severity of hypertension can be increased when Methoxyflurane is combined with Doxofylline.
Ibuprofen The risk or severity of hypertension can be increased when Ibuprofen is combined with Doxofylline.
Dutasteride The risk or severity of hypertension can be increased when Dutasteride is combined with Doxofylline.
Halothane The risk or severity of hypertension can be increased when Halothane is combined with Doxofylline.
Desflurane The risk or severity of hypertension can be increased when Desflurane is combined with Doxofylline.
Finasteride The risk or severity of hypertension can be increased when Finasteride is combined with Doxofylline.
Sevoflurane The risk or severity of hypertension can be increased when Sevoflurane is combined with Doxofylline.
Lumiracoxib The risk or severity of hypertension can be increased when Lumiracoxib is combined with Doxofylline.
Yohimbine The risk or severity of hypertension can be increased when Yohimbine is combined with Doxofylline.
Magnesium salicylate The risk or severity of hypertension can be increased when Magnesium salicylate is combined with Doxofylline.
Salsalate The risk or severity of hypertension can be increased when Salsalate is combined with Doxofylline.
Choline magnesium trisalicylate The risk or severity of hypertension can be increased when Choline magnesium trisalicylate is combined with Doxofylline.
Antrafenine The risk or severity of hypertension can be increased when Antrafenine is combined with Doxofylline.
4-Methoxyamphetamine The risk or severity of hypertension can be increased when 4-Methoxyamphetamine is combined with Doxofylline.
Phendimetrazine The risk or severity of hypertension can be increased when Phendimetrazine is combined with Doxofylline.
Solifenacin The risk or severity of hypertension can be increased when Solifenacin is combined with Doxofylline.
Tiaprofenic acid The risk or severity of hypertension can be increased when Tiaprofenic acid is combined with Doxofylline.
Epicaptopril The risk or severity of hypertension can be increased when Epicaptopril is combined with Doxofylline.
Taxifolin The risk or severity of hypertension can be increased when Taxifolin is combined with Doxofylline.
Oxyphenbutazone The risk or severity of hypertension can be increased when Oxyphenbutazone is combined with Doxofylline.
1-benzylimidazole The risk or severity of hypertension can be increased when 1-benzylimidazole is combined with Doxofylline.
Nimesulide The risk or severity of hypertension can be increased when Nimesulide is combined with Doxofylline.
Benoxaprofen The risk or severity of hypertension can be increased when Benoxaprofen is combined with Doxofylline.
Metamizole The risk or severity of hypertension can be increased when Metamizole is combined with Doxofylline.
Zomepirac The risk or severity of hypertension can be increased when Zomepirac is combined with Doxofylline.
Flibanserin The risk or severity of hypertension can be increased when Flibanserin is combined with Doxofylline.
Cimicoxib The risk or severity of hypertension can be increased when Cimicoxib is combined with Doxofylline.
Rotigotine The risk or severity of hypertension can be increased when Rotigotine is combined with Doxofylline.
Amibegron The risk or severity of hypertension can be increased when Amibegron is combined with Doxofylline.
Naluzotan The risk or severity of hypertension can be increased when Naluzotan is combined with Doxofylline.
Cariprazine The risk or severity of hypertension can be increased when Cariprazine is combined with Doxofylline.
Solabegron The risk or severity of hypertension can be increased when Solabegron is combined with Doxofylline.
Esmirtazapine The risk or severity of hypertension can be increased when Esmirtazapine is combined with Doxofylline.
Vilazodone The risk or severity of hypertension can be increased when Vilazodone is combined with Doxofylline.
Nitrous oxide The risk or severity of hypertension can be increased when Nitrous oxide is combined with Doxofylline.
Xylometazoline The risk or severity of hypertension can be increased when Xylometazoline is combined with Doxofylline.
Dexmethylphenidate The risk or severity of hypertension can be increased when Dexmethylphenidate is combined with Doxofylline.
Isometheptene The risk or severity of hypertension can be increased when Isometheptene is combined with Doxofylline.
Levonordefrin The risk or severity of adverse effects can be increased when Levonordefrin is combined with Doxofylline.
Naphazoline The risk or severity of adverse effects can be increased when Naphazoline is combined with Doxofylline.
Lornoxicam The risk or severity of hypertension can be increased when Lornoxicam is combined with Doxofylline.
Aceclofenac The risk or severity of hypertension can be increased when Aceclofenac is combined with Doxofylline.
Zaltoprofen The risk or severity of hypertension can be increased when Zaltoprofen is combined with Doxofylline.
Saralasin The risk or severity of hypertension can be increased when Saralasin is combined with Doxofylline.
Azapropazone The risk or severity of hypertension can be increased when Azapropazone is combined with Doxofylline.
Parecoxib The risk or severity of hypertension can be increased when Parecoxib is combined with Doxofylline.
Salicylamide The risk or severity of hypertension can be increased when Salicylamide is combined with Doxofylline.
Cinitapride The risk or severity of hypertension can be increased when Cinitapride is combined with Doxofylline.

Target Protein

Beta-2 adrenergic receptor ADRB2
cGMP-dependent 3',5'-cyclic phosphodiesterase PDE2A
Adenosine receptor A2a ADORA2A

Referensi & Sumber

Artikel (PubMed)
  • PMID: 3245738
    Cirillo R, Barone D, Franzone JS: Doxofylline, an antiasthmatic drug lacking affinity for adenosine receptors. Arch Int Pharmacodyn Ther. 1988 Sep-Oct;295:221-37.
  • PMID: 2791671
    Poggi R, Brandolese R, Bernasconi M, Manzin E, Rossi A: Doxofylline and respiratory mechanics. Short-term effects in mechanically ventilated patients with airflow obstruction and respiratory failure. Chest. 1989 Oct;96(4):772-8.
  • PMID: 11268710
    Dini FL, Cogo R: Doxofylline: a new generation xanthine bronchodilator devoid of major cardiovascular adverse effects. Curr Med Res Opin. 2001;16(4):258-68.
  • PMID: 18376093
    Sankar J, Lodha R, Kabra SK: Doxofylline: The next generation methylxanthine. Indian J Pediatr. 2008 Mar;75(3):251-4.
  • PMID: 19678793
    Shukla D, Chakraborty S, Singh S, Mishra B: Doxofylline: a promising methylxanthine derivative for the treatment of asthma and chronic obstructive pulmonary disease. Expert Opin Pharmacother. 2009 Oct;10(14):2343-56. doi: 10.1517/14656560903200667.
  • PMID: 29255355
    Matera MG, Page C, Cazzola M: Doxofylline is not just another theophylline! Int J Chron Obstruct Pulmon Dis. 2017 Dec 5;12:3487-3493. doi: 10.2147/COPD.S150887. eCollection 2017.
  • PMID: 22138191
    van Mastbergen J, Jolas T, Allegra L, Page CP: The mechanism of action of doxofylline is unrelated to HDAC inhibition, PDE inhibition or adenosine receptor antagonism. Pulm Pharmacol Ther. 2012 Feb;25(1):55-61. doi: 10.1016/j.pupt.2011.10.007. Epub 2011 Nov 25.
  • PMID: 27173639
    Zhang Y, Zeng K, Wang J, Gao H, Nan Y, Zheng X: Identifying the antiasthmatic target of doxofylline using immobilized beta2 -adrenoceptor based high-performance affinity chromatography and site-directed molecular docking. J Mol Recognit. 2016 Oct;29(10):492-8. doi: 10.1002/jmr.2549. Epub 2016 May 12.

Contoh Produk & Brand

Produk: 0 • International brands: 2
International Brands
  • Ansimar — ABC Farmaceutici S.P.A
  • Maxivent — Ajanta Pharma

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