Varenicline

DB01273

small molecule approved investigational

Deskripsi

Varenicline is a prescription medication used to treat smoking addiction. This medication is the first approved nicotinic receptor partial agonist. Specifically, varenicline is a partial agonist of the alpha4/beta2 subtype of the nicotinic acetylcholine receptor. In addition it acts on alpha3/beta4 and weakly on alpha3beta2 and alpha6-containing receptors. A full agonism was displayed on alpha7-receptors.

On March 9, 2015, the U.S. Food and Drug Administration warned that Varenicline, in the form of Pfizer Inc's quit-smoking drug, Chantix, has been associated with seizures and that some patients who drink while taking the drug may become aggressive or black out. Pfizer is conducting an additional safety study of the drug, results of which are expected in late 2015. The FDA said it is keeping the black box in place at least until the results of the trial are announced.

Struktur Molekul 2D

Berat 211.268
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of varenicline is approximately 24 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Metabolism is limited (<10%). Most of the active compound is excreted by the kidneys (81%). A minor amount of varenicline is glucuronidated, oxidated, N-formylated, as well as conjugated to form a hexose.

Rute Eliminasi

Varenicline undergoes minimal metabolism, with 92% excreted unchanged in the urine. Renal elimination of varenicline is primarily through glomerular filtration along with active tubular secretion possibly via the organic cation transporter, OCT2.

Interaksi Makanan

1 Data
  • 1. Avoid excessive or chronic alcohol consumption. Varenicline may increase the effects of alcohol; therefore, reduce consumption of alcohol when starting varenicline.

Interaksi Obat

860 Data
Nicotine The risk or severity of adverse effects can be increased when Varenicline is combined with Nicotine.
Bupropion The excretion of Varenicline can be decreased when combined with Bupropion.
Trimethoprim The serum concentration of Varenicline can be increased when it is combined with Trimethoprim.
Esmolol The risk or severity of adverse effects can be increased when Esmolol is combined with Varenicline.
Betaxolol The risk or severity of adverse effects can be increased when Betaxolol is combined with Varenicline.
Atenolol The risk or severity of adverse effects can be increased when Atenolol is combined with Varenicline.
Sotalol The risk or severity of adverse effects can be increased when Sotalol is combined with Varenicline.
Alprenolol The risk or severity of adverse effects can be increased when Alprenolol is combined with Varenicline.
Carvedilol The risk or severity of adverse effects can be increased when Carvedilol is combined with Varenicline.
Propafenone The risk or severity of adverse effects can be increased when Propafenone is combined with Varenicline.
Acebutolol The risk or severity of adverse effects can be increased when Acebutolol is combined with Varenicline.
Bevantolol The risk or severity of adverse effects can be increased when Bevantolol is combined with Varenicline.
Practolol The risk or severity of adverse effects can be increased when Practolol is combined with Varenicline.
Dexpropranolol The risk or severity of adverse effects can be increased when Dexpropranolol is combined with Varenicline.
Celiprolol The risk or severity of adverse effects can be increased when Celiprolol is combined with Varenicline.
Nebivolol The risk or severity of adverse effects can be increased when Nebivolol is combined with Varenicline.
Bufuralol The risk or severity of adverse effects can be increased when Bufuralol is combined with Varenicline.
Bopindolol The risk or severity of adverse effects can be increased when Bopindolol is combined with Varenicline.
Bupranolol The risk or severity of adverse effects can be increased when Bupranolol is combined with Varenicline.
Indenolol The risk or severity of adverse effects can be increased when Indenolol is combined with Varenicline.
Levobetaxolol The risk or severity of adverse effects can be increased when Levobetaxolol is combined with Varenicline.
Talinolol The risk or severity of adverse effects can be increased when Talinolol is combined with Varenicline.
Anisodamine The risk or severity of adverse effects can be increased when Anisodamine is combined with Varenicline.
Bucindolol The risk or severity of adverse effects can be increased when Bucindolol is combined with Varenicline.
Esatenolol The risk or severity of adverse effects can be increased when Esatenolol is combined with Varenicline.
Cloranolol The risk or severity of adverse effects can be increased when Cloranolol is combined with Varenicline.
Mepindolol The risk or severity of adverse effects can be increased when Mepindolol is combined with Varenicline.
Epanolol The risk or severity of adverse effects can be increased when Epanolol is combined with Varenicline.
Tertatolol The risk or severity of adverse effects can be increased when Tertatolol is combined with Varenicline.
Timolol The risk or severity of adverse effects can be increased when Timolol is combined with Varenicline.
Labetalol The risk or severity of adverse effects can be increased when Labetalol is combined with Varenicline.
Bisoprolol The risk or severity of adverse effects can be increased when Bisoprolol is combined with Varenicline.
Pindolol The risk or severity of adverse effects can be increased when Pindolol is combined with Varenicline.
Nadolol The risk or severity of adverse effects can be increased when Nadolol is combined with Varenicline.
Penbutolol The risk or severity of adverse effects can be increased when Penbutolol is combined with Varenicline.
Arotinolol The risk or severity of adverse effects can be increased when Arotinolol is combined with Varenicline.
Landiolol The risk or severity of adverse effects can be increased when Landiolol is combined with Varenicline.
Cimetropium Varenicline may decrease the anticholinergic activities of Cimetropium.
Ethanol The risk or severity of adverse effects can be increased when Varenicline is combined with Ethanol.
Pegvisomant The risk or severity of adverse effects can be increased when Pegvisomant is combined with Varenicline.
Mefloquine The risk or severity of adverse effects can be increased when Mefloquine is combined with Varenicline.
Tacrine The risk or severity of adverse effects can be increased when Tacrine is combined with Varenicline.
Sulpiride The risk or severity of adverse effects can be increased when Sulpiride is combined with Varenicline.
Profenamine The risk or severity of adverse effects can be increased when Profenamine is combined with Varenicline.
Gallamine triethiodide The risk or severity of adverse effects can be increased when Gallamine triethiodide is combined with Varenicline.
Triflupromazine The risk or severity of adverse effects can be increased when Triflupromazine is combined with Varenicline.
Cinchocaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Varenicline.
Pyridostigmine The risk or severity of adverse effects can be increased when Pyridostigmine is combined with Varenicline.
Nizatidine The risk or severity of adverse effects can be increased when Nizatidine is combined with Varenicline.
Isoflurophate The risk or severity of adverse effects can be increased when Isoflurophate is combined with Varenicline.
Diethylcarbamazine The risk or severity of adverse effects can be increased when Diethylcarbamazine is combined with Varenicline.
Procaine The risk or severity of adverse effects can be increased when Procaine is combined with Varenicline.
Minaprine The risk or severity of adverse effects can be increased when Minaprine is combined with Varenicline.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Varenicline.
Hexafluronium The risk or severity of adverse effects can be increased when Hexafluronium is combined with Varenicline.
Demecarium The risk or severity of adverse effects can be increased when Demecarium is combined with Varenicline.
Physostigmine The risk or severity of adverse effects can be increased when Physostigmine is combined with Varenicline.
Rivastigmine The risk or severity of adverse effects can be increased when Rivastigmine is combined with Varenicline.
Ambenonium The risk or severity of adverse effects can be increased when Ambenonium is combined with Varenicline.
Tubocurarine The risk or severity of adverse effects can be increased when Tubocurarine is combined with Varenicline.
Decamethonium The risk or severity of adverse effects can be increased when Decamethonium is combined with Varenicline.
Pancuronium The risk or severity of adverse effects can be increased when Pancuronium is combined with Varenicline.
Pipecuronium The risk or severity of adverse effects can be increased when Pipecuronium is combined with Varenicline.
Ginkgo biloba The risk or severity of adverse effects can be increased when Ginkgo biloba is combined with Varenicline.
Neostigmine The risk or severity of adverse effects can be increased when Neostigmine is combined with Varenicline.
Bambuterol The risk or severity of adverse effects can be increased when Bambuterol is combined with Varenicline.
1,10-Phenanthroline The risk or severity of adverse effects can be increased when 1,10-Phenanthroline is combined with Varenicline.
Thiotepa The risk or severity of adverse effects can be increased when Thiotepa is combined with Varenicline.
Huperzine A The risk or severity of adverse effects can be increased when Huperzine A is combined with Varenicline.
Phenserine The risk or severity of adverse effects can be increased when Phenserine is combined with Varenicline.
Regramostim The risk or severity of adverse effects can be increased when Regramostim is combined with Varenicline.
Aprotinin The risk or severity of adverse effects can be increased when Aprotinin is combined with Varenicline.
Betaine The risk or severity of adverse effects can be increased when Betaine is combined with Varenicline.
Capsaicin The risk or severity of adverse effects can be increased when Capsaicin is combined with Varenicline.
Coumaphos The risk or severity of adverse effects can be increased when Coumaphos is combined with Varenicline.
Dichlorvos The risk or severity of adverse effects can be increased when Dichlorvos is combined with Varenicline.
Fenthion The risk or severity of adverse effects can be increased when Fenthion is combined with Varenicline.
Metrifonate The risk or severity of adverse effects can be increased when Metrifonate is combined with Varenicline.
Acotiamide The risk or severity of adverse effects can be increased when Acotiamide is combined with Varenicline.
Methanesulfonyl Fluoride The risk or severity of adverse effects can be increased when Methanesulfonyl Fluoride is combined with Varenicline.
Paraoxon The risk or severity of adverse effects can be increased when Paraoxon is combined with Varenicline.
Tyrothricin The risk or severity of adverse effects can be increased when Tyrothricin is combined with Varenicline.
Ipidacrine The risk or severity of adverse effects can be increased when Ipidacrine is combined with Varenicline.
Distigmine The risk or severity of adverse effects can be increased when Distigmine is combined with Varenicline.
Tretamine The risk or severity of adverse effects can be increased when Tretamine is combined with Varenicline.
Posiphen The risk or severity of adverse effects can be increased when Posiphen is combined with Varenicline.
Methylphosphinic Acid The risk or severity of adverse effects can be increased when Methylphosphinic Acid is combined with Varenicline.
Galantamine The risk or severity of adverse effects can be increased when Galantamine is combined with Varenicline.
Tipiracil The excretion of Tipiracil can be decreased when combined with Varenicline.
Choline The excretion of Varenicline can be decreased when combined with Choline.
Thiamine The excretion of Varenicline can be decreased when combined with Thiamine.
Ranolazine The excretion of Varenicline can be decreased when combined with Ranolazine.
Metoprolol The excretion of Varenicline can be decreased when combined with Metoprolol.
Disopyramide The excretion of Varenicline can be decreased when combined with Disopyramide.
Metformin The serum concentration of Metformin can be increased when it is combined with Varenicline.
Aminohippuric acid The excretion of Varenicline can be decreased when combined with Aminohippuric acid.
Grepafloxacin The excretion of Varenicline can be decreased when combined with Grepafloxacin.
Norepinephrine The excretion of Varenicline can be decreased when combined with Norepinephrine.
Progesterone The excretion of Varenicline can be decreased when combined with Progesterone.
Imipramine The excretion of Varenicline can be decreased when combined with Imipramine.

Target Protein

Neuronal acetylcholine receptor subunit alpha-4 CHRNA4
Neuronal acetylcholine receptor subunit alpha-7 CHRNA7
Neuronal acetylcholine receptor subunit alpha-3 CHRNA3
Neuronal acetylcholine receptor subunit alpha-6 CHRNA6
Neuronal acetylcholine receptor subunit beta-2 CHRNB2

Referensi & Sumber

Synthesis reference: Vinod Kumar Kansal, Suhail Ahmad, Amit Gupta, "PROCESSES FOR THE PREPARATION OF VARENICLINE AND INTERMEDIATES THEREOF." U.S. Patent US20090318695, issued December 24, 2009.
Artikel (PubMed)
  • PMID: 16820547
    Jorenby DE, Hays JT, Rigotti NA, Azoulay S, Watsky EJ, Williams KE, Billing CB, Gong J, Reeves KR: Efficacy of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: a randomized controlled trial. JAMA. 2006 Jul 5;296(1):56-63.
  • PMID: 16766716
    Mihalak KB, Carroll FI, Luetje CW: Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol Pharmacol. 2006 Sep;70(3):801-5. Epub 2006 Jun 9.
  • PMID: 16221753
    Obach RS, Reed-Hagen AE, Krueger SS, Obach BJ, O'Connell TN, Zandi KS, Miller S, Coe JW: Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitro. Drug Metab Dispos. 2006 Jan;34(1):121-30. Epub 2005 Oct 12.
  • PMID: 15887955
    Coe JW, Brooks PR, Vetelino MG, Wirtz MC, Arnold EP, Huang J, Sands SB, Davis TI, Lebel LA, Fox CB, Shrikhande A, Heym JH, Schaeffer E, Rollema H, Lu Y, Mansbach RS, Chambers LK, Rovetti CC, Schulz DW, Tingley FD 3rd, O'Neill BT: Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation. J Med Chem. 2005 May 19;48(10):3474-7.
  • PMID: 16467225
    Kuehn BM: FDA speeds smoking cessation drug review. JAMA. 2006 Feb 8;295(6):614.

Contoh Produk & Brand

Produk: 167 • International brands: 0
Produk
  • Apo-varenicline
    Kit; Tablet, film coated • - • Oral • US
  • Apo-varenicline
    Kit; Tablet, film coated • - • Oral • US
  • Apo-varenicline
    Tablet, film coated • 0.5 mg/1 • Oral • US
  • Apo-varenicline
    Tablet, film coated • 1 mg/1 • Oral • US
  • Apo-varenicline
    Tablet • 0.5 mg • Oral • Canada • Generic • Approved
  • Apo-varenicline
    Tablet • 1 mg • Oral • Canada • Generic • Approved
  • Apo-varenicline
    Kit; Tablet • - • Oral • Canada • Generic • Approved
  • Apo-varenicline
    Kit; Tablet • - • Oral • Canada • Generic • Approved
Menampilkan 8 dari 167 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul