Peringatan Keamanan

Revefenacin does not produce the typical systemic effects associated with anticholinergic therapies.A40025 In carcinogenic studies in animals, there was no evidence of tumorigenicity. As well, there was no evidence of mutagenicity in the Ames test nor genotoxicity in in vitro mouse lymphoma assays and in vivo rat bone marrow micronucleus assays. There is no effect in the fertility.FDA label

In overdose situations, the common signs and symptoms are nausea, vomiting, dizziness, lightheadedness, blurred vision, increased intraocular pressure, obstipation and difficulties in voiding.FDA label

Revefenacin

DB11855

small molecule approved investigational

Deskripsi

Revefenacin is a novel biphenyl carbamate tertiary amine agent that belongs to the family of the long-acting muscarinic antagonists (LAMA). The labile primary amide in the structure produces a "soft-drug" site that allows rapid systemic clearance and minimizing of the systemically mediated adverse reactions. The LAMA group falls into a parent category known as long-acting inhaled bronchodilators and this type of agents are recommended as a maintenance therapy for chronic obstructive pulmonary disease (COPD).A40025 From the LAMA group, revefenacin is the first once-daily nebulized LAMA treatment.A40026 It was developed by Theravance Biopharma and FDA approved on November 9, 2018.L4818

Struktur Molekul 2D

Berat 597.76
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The apparent terminal half-life of a dose of 350 mcg of revefenacin was 22.3-70 hours.[A40025]
Volume Distribusi After intravenous administration of revefenacin, the reported volume of distribution is 218 L which suggests an extensive distribution to the tissues.[FDA label]
Klirens (Clearance) The renal clearance of revefenacin is negligible and thus, the clearance rate is not a major parameter for this drug.

Absorpsi

In pharmacokinetic studies, revefenacin was absorbed very rapidly and presented a linear increase in plasma exposure with Cmax, tmax and AUC that ranged between 0.02-0.15 ng/ml, 0.48-0.51 hours and 0.03-0.36 ng.h/ml, respectively.A40025 The bioaccumulation of revefenacin was very limited and the steady-state was achieved by day 7.L4822

Metabolisme

Revefenacin presents a high metabolic liability producing a rapid metabolic turnover after being distributed from the lung. This metabolic process is done primarily via enzymatic hydrolysis via CYP2D6 to its major hydrolytic metabolite THRX-195518.A40025

Rute Eliminasi

After reaching maximum concentration, revefenacin concentrations decline in a biphasic manner.A40025 This elimination kinetics is observed by a rapid declining plasma concentration followed by a slow apparent bi-exponential elimination. Renal elimination of revefenacin is limited and it presents a mean cumulative amount excreted in urine as the unchanged drug of < 0.2% of the administered dose.A40028 Following intravenous revefenacin administration, 54% of the dose is recovered in feces and 27% was recovered in urine which confirms a high hepatobiliary processing.L4823

Interaksi Obat

947 Data
Ranolazine The serum concentration of Revefenacin can be increased when it is combined with Ranolazine.
Aclidinium The risk or severity of adverse effects can be increased when Revefenacin is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Revefenacin.
Mirabegron The risk or severity of urinary retention can be increased when Revefenacin is combined with Mirabegron.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Revefenacin is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Revefenacin.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Revefenacin.
Tiotropium The risk or severity of adverse effects can be increased when Revefenacin is combined with Tiotropium.
Topiramate The risk or severity of hyperthermia and oligohydrosis can be increased when Revefenacin is combined with Topiramate.
Umeclidinium The risk or severity of adverse effects can be increased when Revefenacin is combined with Umeclidinium.
Glycopyrronium The risk or severity of adverse effects can be increased when Revefenacin is combined with Glycopyrronium.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Revefenacin is combined with Botulinum toxin type A.
Glucagon Revefenacin may increase the gastrointestinal motility reducing activities of Glucagon.
Sulpiride Revefenacin may increase the anticholinergic activities of Sulpiride.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Revefenacin is combined with Botulinum toxin type B.
Eluxadoline The risk or severity of constipation can be increased when Revefenacin is combined with Eluxadoline.
Ramosetron The risk or severity of constipation can be increased when Revefenacin is combined with Ramosetron.
Naltrexone The risk or severity of adverse effects can be increased when Revefenacin is combined with Naltrexone.
Bezitramide The risk or severity of adverse effects can be increased when Revefenacin is combined with Bezitramide.
Codeine The risk or severity of adverse effects can be increased when Revefenacin is combined with Codeine.
Hydromorphone The risk or severity of adverse effects can be increased when Revefenacin is combined with Hydromorphone.
Oxycodone The risk or severity of adverse effects can be increased when Revefenacin is combined with Oxycodone.
Butorphanol The risk or severity of adverse effects can be increased when Revefenacin is combined with Butorphanol.
Sufentanil The risk or severity of adverse effects can be increased when Revefenacin is combined with Sufentanil.
Nalbuphine The risk or severity of adverse effects can be increased when Revefenacin is combined with Nalbuphine.
Levorphanol The risk or severity of adverse effects can be increased when Revefenacin is combined with Levorphanol.
Remifentanil The risk or severity of adverse effects can be increased when Revefenacin is combined with Remifentanil.
Hydrocodone The risk or severity of adverse effects can be increased when Revefenacin is combined with Hydrocodone.
Diphenoxylate The risk or severity of adverse effects can be increased when Revefenacin is combined with Diphenoxylate.
Oxymorphone The risk or severity of adverse effects can be increased when Revefenacin is combined with Oxymorphone.
Dezocine The risk or severity of adverse effects can be increased when Revefenacin is combined with Dezocine.
Levacetylmethadol The risk or severity of adverse effects can be increased when Revefenacin is combined with Levacetylmethadol.
Methadyl acetate The risk or severity of adverse effects can be increased when Revefenacin is combined with Methadyl acetate.
Dihydroetorphine The risk or severity of adverse effects can be increased when Revefenacin is combined with Dihydroetorphine.
Diamorphine The risk or severity of adverse effects can be increased when Revefenacin is combined with Diamorphine.
Ethylmorphine The risk or severity of adverse effects can be increased when Revefenacin is combined with Ethylmorphine.
Etorphine The risk or severity of adverse effects can be increased when Revefenacin is combined with Etorphine.
Dextromoramide The risk or severity of adverse effects can be increased when Revefenacin is combined with Dextromoramide.
Desomorphine The risk or severity of adverse effects can be increased when Revefenacin is combined with Desomorphine.
Carfentanil The risk or severity of adverse effects can be increased when Revefenacin is combined with Carfentanil.
Dihydrocodeine The risk or severity of adverse effects can be increased when Revefenacin is combined with Dihydrocodeine.
Alphacetylmethadol The risk or severity of adverse effects can be increased when Revefenacin is combined with Alphacetylmethadol.
Dihydromorphine The risk or severity of adverse effects can be increased when Revefenacin is combined with Dihydromorphine.
Ketobemidone The risk or severity of adverse effects can be increased when Revefenacin is combined with Ketobemidone.
DPDPE The risk or severity of adverse effects can be increased when Revefenacin is combined with DPDPE.
Lofentanil The risk or severity of adverse effects can be increased when Revefenacin is combined with Lofentanil.
Opium The risk or severity of adverse effects can be increased when Revefenacin is combined with Opium.
Normethadone The risk or severity of adverse effects can be increased when Revefenacin is combined with Normethadone.
Piritramide The risk or severity of adverse effects can be increased when Revefenacin is combined with Piritramide.
Alphaprodine The risk or severity of adverse effects can be increased when Revefenacin is combined with Alphaprodine.
Nicomorphine The risk or severity of adverse effects can be increased when Revefenacin is combined with Nicomorphine.
Meptazinol The risk or severity of adverse effects can be increased when Revefenacin is combined with Meptazinol.
Phenoperidine The risk or severity of adverse effects can be increased when Revefenacin is combined with Phenoperidine.
Phenazocine The risk or severity of adverse effects can be increased when Revefenacin is combined with Phenazocine.
Tilidine The risk or severity of adverse effects can be increased when Revefenacin is combined with Tilidine.
Carfentanil, C-11 The risk or severity of adverse effects can be increased when Revefenacin is combined with Carfentanil, C-11.
Buprenorphine The risk or severity of adverse effects can be increased when Revefenacin is combined with Buprenorphine.
Methadone The risk or severity of adverse effects can be increased when Revefenacin is combined with Methadone.
Pentazocine The risk or severity of adverse effects can be increased when Revefenacin is combined with Pentazocine.
Alfentanil The risk or severity of adverse effects can be increased when Revefenacin is combined with Alfentanil.
Fentanyl The risk or severity of adverse effects can be increased when Revefenacin is combined with Fentanyl.
Tramadol The risk or severity of adverse effects can be increased when Revefenacin is combined with Tramadol.
Morphine The risk or severity of adverse effects can be increased when Revefenacin is combined with Morphine.
Dextropropoxyphene The risk or severity of adverse effects can be increased when Revefenacin is combined with Dextropropoxyphene.
Tapentadol The risk or severity of urinary retention and constipation can be increased when Revefenacin is combined with Tapentadol.
Meperidine The risk or severity of adverse effects can be increased when Revefenacin is combined with Meperidine.
Benzhydrocodone The risk or severity of adverse effects can be increased when Revefenacin is combined with Benzhydrocodone.
Naloxegol The risk or severity of adverse effects can be increased when Revefenacin is combined with Naloxegol.
Oxyphenonium The risk or severity of adverse effects can be increased when Oxyphenonium is combined with Revefenacin.
Disopyramide The risk or severity of adverse effects can be increased when Disopyramide is combined with Revefenacin.
Metixene The risk or severity of adverse effects can be increased when Metixene is combined with Revefenacin.
Buclizine The risk or severity of adverse effects can be increased when Buclizine is combined with Revefenacin.
Trihexyphenidyl The risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Revefenacin.
Oxyphencyclimine The risk or severity of adverse effects can be increased when Oxyphencyclimine is combined with Revefenacin.
Procyclidine The risk or severity of adverse effects can be increased when Procyclidine is combined with Revefenacin.
Hyoscyamine The risk or severity of adverse effects can be increased when Hyoscyamine is combined with Revefenacin.
Methscopolamine bromide The risk or severity of adverse effects can be increased when Methscopolamine bromide is combined with Revefenacin.
Tridihexethyl The risk or severity of adverse effects can be increased when Tridihexethyl is combined with Revefenacin.
Anisotropine methylbromide The risk or severity of adverse effects can be increased when Anisotropine methylbromide is combined with Revefenacin.
Atropine The risk or severity of adverse effects can be increased when Atropine is combined with Revefenacin.
Mecamylamine The risk or severity of adverse effects can be increased when Mecamylamine is combined with Revefenacin.
Pirenzepine The risk or severity of adverse effects can be increased when Pirenzepine is combined with Revefenacin.
Homatropine methylbromide The risk or severity of adverse effects can be increased when Homatropine methylbromide is combined with Revefenacin.
Propantheline The risk or severity of adverse effects can be increased when Propantheline is combined with Revefenacin.
Dicyclomine The risk or severity of adverse effects can be increased when Dicyclomine is combined with Revefenacin.
Tropicamide The risk or severity of adverse effects can be increased when Tropicamide is combined with Revefenacin.
Amantadine The risk or severity of adverse effects can be increased when Amantadine is combined with Revefenacin.
Methantheline The risk or severity of adverse effects can be increased when Methantheline is combined with Revefenacin.
Cycrimine The risk or severity of adverse effects can be increased when Cycrimine is combined with Revefenacin.
Cyclopentolate The risk or severity of adverse effects can be increased when Cyclopentolate is combined with Revefenacin.
Pentolinium The risk or severity of adverse effects can be increased when Pentolinium is combined with Revefenacin.
Trimethaphan The risk or severity of adverse effects can be increased when Trimethaphan is combined with Revefenacin.
Flavoxate The risk or severity of adverse effects can be increased when Flavoxate is combined with Revefenacin.
Diphenidol The risk or severity of adverse effects can be increased when Diphenidol is combined with Revefenacin.
Fenoterol The risk or severity of adverse effects can be increased when Fenoterol is combined with Revefenacin.
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione The risk or severity of adverse effects can be increased when Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione is combined with Revefenacin.
Solifenacin The risk or severity of adverse effects can be increased when Solifenacin is combined with Revefenacin.
Isopropamide The risk or severity of adverse effects can be increased when Isopropamide is combined with Revefenacin.
Mepenzolate The risk or severity of adverse effects can be increased when Mepenzolate is combined with Revefenacin.
Hexocyclium The risk or severity of adverse effects can be increased when Hexocyclium is combined with Revefenacin.

Target Protein

Muscarinic acetylcholine receptor CHRM1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 29096627
    Pudi KK, Barnes CN, Moran EJ, Haumann B, Kerwin E: A 28-day, randomized, double-blind, placebo-controlled, parallel group study of nebulized revefenacin in patients with chronic obstructive pulmonary disease. Respir Res. 2017 Nov 2;18(1):182. doi: 10.1186/s12931-017-0647-1.
  • PMID: 27799757
    Tashkin DP: A review of nebulized drug delivery in COPD. Int J Chron Obstruct Pulmon Dis. 2016 Oct 18;11:2585-2596. doi: 10.2147/COPD.S114034. eCollection 2016.
  • PMID: 28128970
    Vogelmeier CF, Criner GJ, Martinez FJ, Anzueto A, Barnes PJ, Bourbeau J, Celli BR, Chen R, Decramer M, Fabbri LM, Frith P, Halpin DM, Lopez Varela MV, Nishimura M, Roche N, Rodriguez-Roisin R, Sin DD, Singh D, Stockley R, Vestbo J, Wedzicha JA, Agusti A: Global Strategy for the Diagnosis, Management, and Prevention of Chronic Obstructive Lung Disease 2017 Report. GOLD Executive Summary. Am J Respir Crit Care Med. 2017 Mar 1;195(5):557-582. doi: 10.1164/rccm.201701-0218PP.
  • PMID: 28987804
    Quinn D, Barnes CN, Yates W, Bourdet DL, Moran EJ, Potgieter P, Nicholls A, Haumann B, Singh D: Pharmacodynamics, pharmacokinetics and safety of revefenacin (TD-4208), a long-acting muscarinic antagonist, in patients with chronic obstructive pulmonary disease (COPD): Results of two randomized, double-blind, phase 2 studies. Pulm Pharmacol Ther. 2018 Feb;48:71-79. doi: 10.1016/j.pupt.2017.10.003. Epub 2017 Oct 4.
  • PMID: 29736245
    Hegde SS, Pulido-Rios MT, Luttmann MA, Foley JJ, Hunsberger GE, Steinfeld T, Lee T, Ji Y, Mammen MM, Jasper JR: Pharmacological properties of revefenacin (TD-4208), a novel, nebulized long-acting, and lung selective muscarinic antagonist, at human recombinant muscarinic receptors and in rat, guinea pig, and human isolated airway tissues. Pharmacol Res Perspect. 2018 Apr 30;6(3):e00400. doi: 10.1002/prp2.400. eCollection 2018 Jun.
  • PMID: 26109098
    Melani AS: Long-acting muscarinic antagonists. Expert Rev Clin Pharmacol. 2015;8(4):479-501. doi: 10.1586/17512433.2015.1058154.
  • PMID: 8441331
    Barnes PJ: Muscarinic receptor subtypes in airways. Life Sci. 1993;52(5-6):521-7.

Contoh Produk & Brand

Produk: 2 • International brands: 0
Produk
  • Yupelri
    Solution • 175 ug/3mL • Respiratory (inhalation) • US • Approved
  • Yupelri
    Solution • 175 ug/3mL • Respiratory (inhalation) • US • Approved

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