Peringatan Keamanan

EMBRYO-FETAL TOXICITY
Do not administer Riociguat to a pregnant female because it may cause fetal harm.
Females of reproductive potential: Exclude pregnancy before the start of treatment, monthly during treatment, and 1 month after stopping treatment. Prevent pregnancy during treatment and for one month after stopping treatment by using acceptable methods of contraception.
For all female patients, Riociguat is available only through a restricted program called the Adempas Risk Evaluation and Mitigation Strategy.

Riociguat

DB08931

small molecule approved

Deskripsi

Riociguat is a soluble guanylate cyclase (sGC) agonist approved in the USA, Europe and several other regions for patients with group I PAH (pulmonary arterial hypertension) in WHO FC II or III; and for the treatment of patients with inoperable CTEPH (chronic thromboembolic pulmonary hypertension), or persistent/recurrent PH (pulmonary hypertension) after pulmonary endarterectomy in WHO FC II or III. Riociguat is marketed under the brand Adempas® by Bayer HealthCare Pharmaceuticals. Treatment with riociguat costs USD $7,500 for 30 days of treatment.

Struktur Molekul 2D

Berat 422.4157
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) About 12 hours in patients and 7 hours in healthy subjects.
Volume Distribusi Volume of distribution at steady state = 30 L
Klirens (Clearance) -

Absorpsi

The pharmacokinetics of riociguant are dose proportional from 0.5 mg to 2.5 mg. The absolute bioavailability is approximately 94%. After oral administration, peak plasma concentrations were achieved within 1.5 hours. Food does not affect the bioavailability of riociguat.

Metabolisme

The active metabolite (M1) of riociguat is 1/3 to 1/10 as potent as riociguat.

Rute Eliminasi

Riociguat is eliminated in the urine (40%) and feces (53%), largely as metabolites.

Interaksi Makanan

3 Data
  • 1. Avoid St. John's Wort. This herb induces the CYP3A4 metabolism of riociguat and may reduce its serum concentration.
  • 2. Take separate from antacids. Take at least 1 hour before or after antacids. Aluminum or magnesium hydroxide antacids may reduce riociguat absorption.
  • 3. Take with or without food.

Interaksi Obat

1146 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Riociguat is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Riociguat is combined with Levodopa.
Risperidone Riociguat may increase the hypotensive activities of Risperidone.
Alfuzosin Alfuzosin may increase the hypotensive activities of Riociguat.
Amifostine Riociguat may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Riociguat.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Riociguat.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Riociguat.
Obinutuzumab Riociguat may increase the hypotensive activities of Obinutuzumab.
Rituximab Riociguat may increase the hypotensive activities of Rituximab.
Desmopressin Desmopressin may decrease the antihypertensive activities of Riociguat.
Midodrine Midodrine may decrease the antihypertensive activities of Riociguat.
Isoetharine Isoetharine may decrease the antihypertensive activities of Riociguat.
Atomoxetine Atomoxetine may decrease the antihypertensive activities of Riociguat.
Etomidate Etomidate may decrease the antihypertensive activities of Riociguat.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Riociguat.
Protriptyline Protriptyline may decrease the antihypertensive activities of Riociguat.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Riociguat.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Riociguat.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Riociguat.
Droperidol Droperidol may decrease the antihypertensive activities of Riociguat.
Amoxapine Amoxapine may decrease the antihypertensive activities of Riociguat.
Doxapram Doxapram may decrease the antihypertensive activities of Riociguat.
Atropine Atropine may decrease the antihypertensive activities of Riociguat.
Metaraminol Metaraminol may decrease the antihypertensive activities of Riociguat.
Sumatriptan Sumatriptan may decrease the antihypertensive activities of Riociguat.
Nicergoline Nicergoline may decrease the antihypertensive activities of Riociguat.
Methoxamine Methoxamine may decrease the antihypertensive activities of Riociguat.
Propiomazine Propiomazine may decrease the antihypertensive activities of Riociguat.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Riociguat.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Riociguat.
Trifluoperazine Trifluoperazine may decrease the antihypertensive activities of Riociguat.
Dobutamine Dobutamine may decrease the antihypertensive activities of Riociguat.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Riociguat.
Ritodrine Ritodrine may decrease the antihypertensive activities of Riociguat.
Terbutaline Terbutaline may decrease the antihypertensive activities of Riociguat.
Flupentixol Flupentixol may decrease the antihypertensive activities of Riociguat.
Bitolterol Bitolterol may decrease the antihypertensive activities of Riociguat.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Riociguat.
Naratriptan Naratriptan may decrease the antihypertensive activities of Riociguat.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Riociguat.
Formoterol Formoterol may decrease the antihypertensive activities of Riociguat.
Dopamine Dopamine may decrease the antihypertensive activities of Riociguat.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Riociguat.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Riociguat.
Arbutamine Arbutamine may decrease the antihypertensive activities of Riociguat.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Riociguat.
Arformoterol Arformoterol may decrease the antihypertensive activities of Riociguat.
Fenoterol Fenoterol may decrease the antihypertensive activities of Riociguat.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Riociguat.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Riociguat.
Ephedrine Ephedrine may decrease the antihypertensive activities of Riociguat.
Mephentermine Mephentermine may decrease the antihypertensive activities of Riociguat.
Procaterol Procaterol may decrease the antihypertensive activities of Riociguat.
Methotrimeprazine Methotrimeprazine may decrease the antihypertensive activities of Riociguat.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Riociguat.
Bambuterol Bambuterol may decrease the antihypertensive activities of Riociguat.
MMDA MMDA may decrease the antihypertensive activities of Riociguat.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Riociguat.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Riociguat.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Riociguat.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Riociguat.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Riociguat.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Riociguat.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Riociguat.
Metamfetamine Metamfetamine may decrease the antihypertensive activities of Riociguat.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Riociguat.
Periciazine Periciazine may decrease the antihypertensive activities of Riociguat.
Acepromazine Acepromazine may decrease the antihypertensive activities of Riociguat.
Thioproperazine Thioproperazine may decrease the antihypertensive activities of Riociguat.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Riociguat.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Riociguat.
Amineptine Amineptine may decrease the antihypertensive activities of Riociguat.
Amibegron Amibegron may decrease the antihypertensive activities of Riociguat.
Naluzotan Naluzotan may decrease the antihypertensive activities of Riociguat.
Pizotifen Pizotifen may decrease the antihypertensive activities of Riociguat.
Solabegron Solabegron may decrease the antihypertensive activities of Riociguat.
Droxidopa Droxidopa may decrease the antihypertensive activities of Riociguat.
Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Riociguat.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Riociguat.
Xylometazoline Xylometazoline may decrease the antihypertensive activities of Riociguat.
Isometheptene Isometheptene may decrease the antihypertensive activities of Riociguat.
Levonordefrin Levonordefrin may decrease the antihypertensive activities of Riociguat.
Naphazoline Naphazoline may decrease the antihypertensive activities of Riociguat.
Saralasin Saralasin may decrease the antihypertensive activities of Riociguat.
Tetryzoline Tetryzoline may decrease the antihypertensive activities of Riociguat.
Cinitapride Cinitapride may decrease the antihypertensive activities of Riociguat.
Tyramine Tyramine may decrease the antihypertensive activities of Riociguat.
Adrafinil Adrafinil may decrease the antihypertensive activities of Riociguat.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Riociguat.
Hexoprenaline Hexoprenaline may decrease the antihypertensive activities of Riociguat.
Etilefrine Etilefrine may decrease the antihypertensive activities of Riociguat.
Dimetacrine Dimetacrine may decrease the antihypertensive activities of Riociguat.
Butriptyline Butriptyline may decrease the antihypertensive activities of Riociguat.
Dosulepin Dosulepin may decrease the antihypertensive activities of Riociguat.
Cirazoline Cirazoline may decrease the antihypertensive activities of Riociguat.
Synephrine Synephrine may decrease the antihypertensive activities of Riociguat.
Moxisylyte Moxisylyte may decrease the antihypertensive activities of Riociguat.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Riociguat.
Iofetamine I-123 Iofetamine I-123 may decrease the antihypertensive activities of Riociguat.

Target Protein

Retinal guanylyl cyclase 1 GUCY2D
Guanylate cyclase soluble subunit alpha-2 GUCY1A2

Referensi & Sumber

Synthesis reference: "Patent Link":http://www.google.com/patents/US7173037
Artikel (PubMed)
  • PMID: 22044316
    Soeiro-Pereira PV, Falcai A, Kubo CA, Oliveira-Junior EB, Marques OC, Antunes E, Condino-Neto A: BAY 41-2272, a soluble guanylate cyclase agonist, activates human mononuclear phagocytes. Br J Pharmacol. 2012 Jul;166(5):1617-30. doi: 10.1111/j.1476-5381.2011.01764.x.
  • PMID: 26599488
    Hambly N, Granton J: Riociguat for the treatment of pulmonary hypertension. Expert Rev Respir Med. 2015;9(6):679-95. doi: 10.1586/17476348.2015.1106316. Epub 2015 Nov 24.
  • PMID: 26219978
    Humbert M, Ghofrani HA: The molecular targets of approved treatments for pulmonary arterial hypertension. Thorax. 2016 Jan;71(1):73-83. doi: 10.1136/thoraxjnl-2015-207170. Epub 2015 Jul 28.
  • PMID: 24218053
    Conole D, Scott LJ: Riociguat: first global approval. Drugs. 2013 Nov;73(17):1967-75. doi: 10.1007/s40265-013-0149-5.
  • PMID: 25395817
    Khaybullina D, Patel A, Zerilli T: Riociguat (adempas): a novel agent for the treatment of pulmonary arterial hypertension and chronic thromboembolic pulmonary hypertension. P T. 2014 Nov;39(11):749-58.

Contoh Produk & Brand

Produk: 35 • International brands: 0
Produk
  • Adempas
    Tablet, film coated • .5 mg/1 • Oral • US • Approved
  • Adempas
    Tablet, film coated • 1 mg/1 • Oral • US • Approved
  • Adempas
    Tablet, film coated • 1.5 mg/1 • Oral • US • Approved
  • Adempas
    Tablet, film coated • 2 mg/1 • Oral • US • Approved
  • Adempas
    Tablet, film coated • 2.5 mg/1 • Oral • US • Approved
  • Adempas
    Tablet, film coated • 0.5 mg • Oral • EU • Approved
  • Adempas
    Tablet, film coated • 0.5 mg • Oral • EU • Approved
  • Adempas
    Tablet, film coated • 0.5 mg • Oral • EU • Approved
Menampilkan 8 dari 35 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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