Peringatan Keamanan

Symptoms of overdose include seizures, arrhythmias, and GI effects.

Theophylline

DB00277

small molecule approved

Deskripsi

A methylxanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Mechanistically, theophylline acts as a phosphodiesterase inhibitor, adenosine receptor blocker, and histone deacetylase activator. Theophylline is marketed under several brand names such as Uniphyl and Theochron, and it is indicated mainly for asthma, bronchospasm, and COPD.

Struktur Molekul 2D

Berat 180.164
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 8 hours
Volume Distribusi * 0.3 to 0.7 L/kg
Klirens (Clearance) * 0.29 mL/kg/min [Premature neonates, postnatal age 3-15 days] * 0.64 mL/kg/min [Premature neonates, postnatal age 25-57 days] * 1.7 mL/kg/min [Children 1-4 years] * 1.6 mL/kg/min [Children 4-12 years] * 0.9 mL/kg/min [Children 13-15 years] * 1.4 mL/kg/min [Children 16-17 years] * 0.65 mL/kg/min [Adults (16-60 years), otherwise healthy non-smoking asthmatics] * 0.41 mL/kg/min [Elderly (>60 years), non-smokers with normal cardiac, liver, and renal function] * 0.33 mL/kg/min [Acute pulmonary edema] * 0.54 mL/kg/min [COPD >60 years, stable, non-smoker >1 year] * 0.48 mL/kg/min [COPD with cor pulmonale] * 1.25 mL/kg/min [Cystic fibrosis (14-28 years)] * 0.31 mL/kg/min [Liver disease cirrhosis] * 0.35 mL/kg/min [acute hepatitis] * 0.65 mL/kg/min [cholestasis] * 0.47 mL/kg/min [Sepsis with multi-organ failure] * 0.38 mL/kg/min [hypothyroid] * 0.8 mL/kg/min [hyperthyroid]

Absorpsi

Theophylline is rapidly and completely absorbed after oral administration in solution or immediate-release solid oral dosage form.

Metabolisme

Hepatic. Biotransformation takes place through demethylation to 1-methylxanthine and 3-methylxanthine and hydroxylation to 1,3-dimethyluric acid. 1-methylxanthine is further hydroxylated, by xanthine oxidase, to 1-methyluric acid. About 6% of a theophylline dose is N-methylated to caffeine. Caffeine and 3-methylxanthine are the only theophylline metabolites with pharmacologic activity.

Rute Eliminasi

Theophylline does not undergo any appreciable pre-systemic elimination, distributes freely into fat-free tissues and is extensively metabolized in the liver. Renal excretion of unchanged theophylline in neonates amounts to about 50% of the dose, compared to about 10% in children older than three months and in adults.

Farmakogenomik

1 Varian
CYP1A2 (None)

Patients with this genotype have reduced metabolism of theophylline.

Interaksi Makanan

3 Data
  • 1. Avoid excessive or chronic alcohol consumption. Ingesting alcohol may reduce the clearance, and therefore increase the serum concentrations of theophylline.
  • 2. Avoid St. John's Wort.
  • 3. Take with or without food. Take consistently with regard to food.

Interaksi Obat

1201 Data
Modafinil The metabolism of Theophylline can be increased when combined with Modafinil.
Armodafinil The metabolism of Theophylline can be increased when combined with Armodafinil.
Deferasirox The serum concentration of Theophylline can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Theophylline can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Theophylline can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Theophylline can be decreased when it is combined with Teriflunomide.
Regadenoson Theophylline may decrease effectiveness of Regadenoson as a diagnostic agent.
Adalimumab The serum concentration of Theophylline can be decreased when it is combined with Adalimumab.
Adenosine The therapeutic efficacy of Adenosine can be decreased when used in combination with Theophylline.
Allopurinol The serum concentration of Theophylline can be increased when it is combined with Allopurinol.
Carbamazepine The serum concentration of Theophylline can be decreased when it is combined with Carbamazepine.
Cimetidine The metabolism of Theophylline can be decreased when combined with Cimetidine.
Disulfiram The serum concentration of Theophylline can be increased when it is combined with Disulfiram.
Febuxostat The serum concentration of the active metabolites of Theophylline can be increased when Theophylline is used in combination with Febuxostat.
Fluvoxamine The metabolism of Theophylline can be decreased when combined with Fluvoxamine.
Formoterol The risk or severity of hypokalemia can be increased when Theophylline is combined with Formoterol.
Indacaterol The risk or severity of adverse effects can be increased when Theophylline is combined with Indacaterol.
Isoniazid The serum concentration of Theophylline can be increased when it is combined with Isoniazid.
Lithium citrate The serum concentration of Lithium citrate can be decreased when it is combined with Theophylline.
Lithium carbonate The serum concentration of Lithium carbonate can be decreased when it is combined with Theophylline.
Lithium hydroxide The serum concentration of Lithium hydroxide can be decreased when it is combined with Theophylline.
Methotrexate The serum concentration of Theophylline can be increased when it is combined with Methotrexate.
Mexiletine The metabolism of Theophylline can be decreased when combined with Mexiletine.
Olodaterol Theophylline may increase the hyperkalemic activities of Olodaterol.
Pancuronium The therapeutic efficacy of Pancuronium can be decreased when used in combination with Theophylline.
Pentoxifylline The serum concentration of Theophylline can be increased when it is combined with Pentoxifylline.
Propafenone The serum concentration of Theophylline can be increased when it is combined with Propafenone.
Quinine The serum concentration of Theophylline can be increased when it is combined with Quinine.
Quinidine The serum concentration of Theophylline can be increased when it is combined with Quinidine.
Riociguat Theophylline may increase the hypotensive activities of Riociguat.
Thiabendazole The metabolism of Theophylline can be decreased when combined with Thiabendazole.
Ticlopidine The metabolism of Theophylline can be decreased when combined with Ticlopidine.
Zafirlukast The serum concentration of Zafirlukast can be decreased when it is combined with Theophylline.
Zileuton The serum concentration of Theophylline can be increased when it is combined with Zileuton.
Metreleptin The metabolism of Theophylline can be increased when combined with Metreleptin.
Mifepristone The serum concentration of Theophylline can be increased when it is combined with Mifepristone.
Probenecid The serum concentration of Theophylline can be increased when it is combined with Probenecid.
Crizotinib The metabolism of Theophylline can be decreased when combined with Crizotinib.
Mirabegron The serum concentration of Theophylline can be increased when it is combined with Mirabegron.
Abiraterone The metabolism of Theophylline can be decreased when combined with Abiraterone.
Isoprenaline The serum concentration of Theophylline can be decreased when it is combined with Isoprenaline.
Norepinephrine The risk or severity of adverse effects can be increased when Norepinephrine is combined with Theophylline.
Phenylpropanolamine The risk or severity of adverse effects can be increased when Phenylpropanolamine is combined with Theophylline.
Metaraminol The risk or severity of adverse effects can be increased when Metaraminol is combined with Theophylline.
Methoxamine The risk or severity of adverse effects can be increased when Methoxamine is combined with Theophylline.
Orciprenaline The risk or severity of adverse effects can be increased when Orciprenaline is combined with Theophylline.
Phenmetrazine The risk or severity of adverse effects can be increased when Phenmetrazine is combined with Theophylline.
Dobutamine The risk or severity of adverse effects can be increased when Dobutamine is combined with Theophylline.
Pseudoephedrine The risk or severity of adverse effects can be increased when Pseudoephedrine is combined with Theophylline.
Ritodrine The risk or severity of adverse effects can be increased when Ritodrine is combined with Theophylline.
Terbutaline The risk or severity of adverse effects can be increased when Terbutaline is combined with Theophylline.
Oxymetazoline The risk or severity of adverse effects can be increased when Oxymetazoline is combined with Theophylline.
Diethylpropion The risk or severity of adverse effects can be increased when Diethylpropion is combined with Theophylline.
Dopamine The risk or severity of adverse effects can be increased when Dopamine is combined with Theophylline.
Fenoterol The risk or severity of adverse effects can be increased when Fenoterol is combined with Theophylline.
Mephentermine The risk or severity of adverse effects can be increased when Mephentermine is combined with Theophylline.
Procaterol The risk or severity of adverse effects can be increased when Procaterol is combined with Theophylline.
Clenbuterol The risk or severity of adverse effects can be increased when Clenbuterol is combined with Theophylline.
MMDA The risk or severity of adverse effects can be increased when MMDA is combined with Theophylline.
2,5-Dimethoxy-4-ethylamphetamine The risk or severity of adverse effects can be increased when 2,5-Dimethoxy-4-ethylamphetamine is combined with Theophylline.
4-Bromo-2,5-dimethoxyamphetamine The risk or severity of adverse effects can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Theophylline.
Tenamfetamine The risk or severity of adverse effects can be increased when Tenamfetamine is combined with Theophylline.
Chlorphentermine The risk or severity of adverse effects can be increased when Chlorphentermine is combined with Theophylline.
Methylenedioxyethamphetamine The risk or severity of adverse effects can be increased when Methylenedioxyethamphetamine is combined with Theophylline.
Tetryzoline The risk or severity of adverse effects can be increased when Tetryzoline is combined with Theophylline.
Tyramine The risk or severity of adverse effects can be increased when Tyramine is combined with Theophylline.
Isoxsuprine The risk or severity of adverse effects can be increased when Isoxsuprine is combined with Theophylline.
Etilefrine The risk or severity of adverse effects can be increased when Etilefrine is combined with Theophylline.
Synephrine The risk or severity of adverse effects can be increased when Synephrine is combined with Theophylline.
Hydroxyamphetamine The risk or severity of adverse effects can be increased when Hydroxyamphetamine is combined with Theophylline.
Iofetamine I-123 The risk or severity of adverse effects can be increased when Iofetamine I-123 is combined with Theophylline.
Racepinephrine The risk or severity of adverse effects can be increased when Racepinephrine is combined with Theophylline.
Ritobegron The risk or severity of adverse effects can be increased when Ritobegron is combined with Theophylline.
Tramazoline The risk or severity of adverse effects can be increased when Tramazoline is combined with Theophylline.
Mephedrone The risk or severity of adverse effects can be increased when Mephedrone is combined with Theophylline.
Fenozolone The risk or severity of adverse effects can be increased when Fenozolone is combined with Theophylline.
Methoxyphenamine The risk or severity of adverse effects can be increased when Methoxyphenamine is combined with Theophylline.
Tretoquinol The risk or severity of adverse effects can be increased when Tretoquinol is combined with Theophylline.
Gepefrine The risk or severity of adverse effects can be increased when Gepefrine is combined with Theophylline.
Prenalterol The risk or severity of adverse effects can be increased when Prenalterol is combined with Theophylline.
Mefenorex The risk or severity of adverse effects can be increased when Mefenorex is combined with Theophylline.
2,5-Dimethoxy-4-ethylthioamphetamine The risk or severity of adverse effects can be increased when 2,5-Dimethoxy-4-ethylthioamphetamine is combined with Theophylline.
Midodrine The risk or severity of adverse effects can be increased when Midodrine is combined with Theophylline.
Benzphetamine The risk or severity of adverse effects can be increased when Benzphetamine is combined with Theophylline.
Nylidrin The risk or severity of adverse effects can be increased when Nylidrin is combined with Theophylline.
Phentermine The risk or severity of adverse effects can be increased when Phentermine is combined with Theophylline.
Bisoprolol The risk or severity of adverse effects can be increased when Bisoprolol is combined with Theophylline.
Dexpropranolol The risk or severity of adverse effects can be increased when Dexpropranolol is combined with Theophylline.
Doxofylline The risk or severity of adverse effects can be increased when Theophylline is combined with Doxofylline.
Human interferon beta The metabolism of Theophylline can be decreased when combined with Human interferon beta.
Peginterferon beta-1a The metabolism of Theophylline can be decreased when combined with Peginterferon beta-1a.
Interferon Kappa The metabolism of Theophylline can be decreased when combined with Interferon Kappa.
Interferon Gamma The metabolism of Theophylline can be decreased when combined with Interferon Gamma.
Butabarbital The serum concentration of Theophylline can be decreased when it is combined with Butabarbital.
Methohexital The serum concentration of Theophylline can be decreased when it is combined with Methohexital.
Thiopental The serum concentration of Theophylline can be decreased when it is combined with Thiopental.
Halazepam The therapeutic efficacy of Halazepam can be decreased when used in combination with Theophylline.
Camazepam The therapeutic efficacy of Camazepam can be decreased when used in combination with Theophylline.
Delorazepam The therapeutic efficacy of Delorazepam can be decreased when used in combination with Theophylline.
Ethyl loflazepate The therapeutic efficacy of Ethyl loflazepate can be decreased when used in combination with Theophylline.

Target Protein

Adenosine receptor A1 ADORA1
5'-nucleotidase NT5E
Adenosine receptor A2a ADORA2A
Adenosine receptor A2b ADORA2B
3',5'-cyclic-AMP phosphodiesterase 4B PDE4B
cGMP-specific 3',5'-cyclic phosphodiesterase PDE5A
3',5'-cyclic-AMP phosphodiesterase 4A PDE4A
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A PDE3A
Histone deacetylase 2 HDAC2
Copine-1 CPNE1
Minor histocompatibility antigen H13 HM13
BOS complex subunit NOMO1 NOMO1
Poly [ADP-ribose] polymerase 1 PARP1
Protein RIC-3 RIC3
Tubulin monoglycylase TTLL3 TTLL3

Referensi & Sumber

Synthesis reference: Nicolae S. Bodor, Kenneth B. Sloan, Yu-Neng Kuo, "Method for synthesizing certain selected pro-drug forms of theophylline." U.S. Patent US4000132, issued January, 1956.

Contoh Produk & Brand

Produk: 186 • International brands: 5
Produk
  • Aa-theo LA
    Tablet, extended release • 300 mg • Oral • Canada • Generic • Approved
  • Aa-theo LA
    Tablet, extended release • 200 mg • Oral • Canada • Generic • Approved
  • Aa-theo LA
    Tablet, extended release • 100 mg • Oral • Canada • Generic • Approved
  • Apo-theo ER
    Tablet, extended release • 400 mg • Oral • Canada • Generic • Approved
  • Apo-theo ER
    Tablet, extended release • 600 mg • Oral • Canada • Generic • Approved
  • Elixir De Theophylline
    Elixir • 80 mg / 15 mL • Oral • Canada • Approved
  • Elixophyllin
    Liquid • 80 mg/15mL • Oral • US • Generic • Approved
  • Elixophyllin
    Liquid • 80 mg/15mL • Oral • US • Generic • Approved
Menampilkan 8 dari 186 produk.
International Brands
  • Respbid
  • Slo-Bid
  • Theo 24
  • Theo-Dur
  • Theodur G

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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