Peringatan Keamanan

Symptoms of overdose include neurological effects such as ataxia, nystagmus, stupor, sedation, speech difficulties, dizziness, nausea, and vomiting, and may also cause other effects such as hypotension; overdose is not associated with respiratory depression. In case of overdose, symptom-related supportive care up to and including hospitalization is recommended. Ziconotide has no known antidote, but the withdrawal of ziconotide generally allows patients to clear the drug and recover within 24 hours. As ziconotide does not bind to opiate receptors, opioid antagonists are not effective at ameliorating overdose effects.L13389

Ziconotide

DB06283

biotech approved

Deskripsi

Ziconotide (also known as SNX-111) is a neurotoxic peptide derived from the cone snail Conus magus comprising 25 amino acids with three disulphide bonds.A202835, L13389 Other such peptides, collectively termed conotoxins, exist, and some have shown efficacy in binding specific subsets of calcium channels; ziconotide is used in part because it can be synthesized without loss of proper bond formation or structural elements.A202829, A202832 Ziconotide is used to manage severe chronic pain refractory to other methods, through its ability to inhibit N-type calcium channels involved in nociceptive signalling.A202829, A202835, A202838, A202841, A202850, A202859, L13389

Ziconotide was granted FDA approval on December 28, 2004 for marketing by TerSera therapeutics LLC. under the name Prialt.L13389 To date, ziconotide is the only calcium channel blocking peptide approved for use by the FDA.A202835

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) In patients administered 1-10 mcg intrathecal ziconotide over one hour, the elimination half-life was calculated as 4.6 ± 0.9 hr. Although intravenous administration is not indicated, intravenous administration of between 0.3-10 mcg/kg/day ziconotide resulted in an elimination half-life of 1.3 ± 0.3 hr.[L13389]
Volume Distribusi In patients administered 1-10 mcg intrathecal ziconotide over one hour, the apparent volume of distribution was calculated as 155 ± 263 mL; this value is roughly equivalent to the expected CSF volume.[L13389] Although intravenous administration is not indicated, intravenous administration of between 0.3-10 mcg/kg/day ziconotide resulted in an apparent volume of distribution of 30,460 ± 6366 mL.[L13389]
Klirens (Clearance) Ziconotide CSF clearance is 0.38 ± 0.56 mL/min while plasma clearance is 270 ± 44 mL/min.[L13389]

Absorpsi

Ziconotide administered intrathecally over one hour in doses between 1 and 10 mcg produced calculated AUC values between 83.6-608 ng\*h/mL and Cmax between 16.4-132 ng/mL; these values are approximately dose-proportional. Given the intrathecal administration and low membrane permeability due to its size, ziconotide is expected to remain primarily in the CSF; plasma levels, where detected, remain constant up to nine months following administration.L13389

Metabolisme

Ziconotide is expected to be processed by various peptidases upon entering systemic circulation; no detailed information on ziconotide metabolism has been reported.L13389

Rute Eliminasi

A small fraction of intravenous ziconotide (< 1%) is recovered in urine.L13389

Interaksi Makanan

1 Data
  • 1. Avoid excessive or chronic alcohol consumption. Ingesting alcohol may increase the CNS depressive effects of ziconotide.

Interaksi Obat

1090 Data
Buprenorphine Ziconotide may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Ziconotide.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Ziconotide.
Hydrocodone Ziconotide may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Ziconotide.
Magnesium sulfate The therapeutic efficacy of Ziconotide can be increased when used in combination with Magnesium sulfate.
Metyrosine Ziconotide may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Ziconotide.
Mirtazapine Ziconotide may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Ziconotide.
Orphenadrine Ziconotide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Pramipexole Ziconotide may increase the sedative activities of Pramipexole.
Ropinirole Ziconotide may increase the sedative activities of Ropinirole.
Rotigotine Ziconotide may increase the sedative activities of Rotigotine.
Sodium oxybate The risk or severity of CNS depression can be increased when Ziconotide is combined with Sodium oxybate.
Suvorexant Ziconotide may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Ziconotide.
Thalidomide Ziconotide may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Ziconotide may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Cimetidine The serum concentration of Ziconotide can be increased when it is combined with Cimetidine.
Clopidogrel The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Ziconotide.
Efavirenz The serum concentration of Ziconotide can be decreased when it is combined with Efavirenz.
Melatonin The therapeutic efficacy of Ziconotide can be decreased when used in combination with Melatonin.
Nafcillin The therapeutic efficacy of Ziconotide can be decreased when used in combination with Nafcillin.
Nitroprusside Ziconotide may increase the hypotensive activities of Nitroprusside.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Ziconotide.
Dantrolene The risk or severity of hyperkalemia can be increased when Dantrolene is combined with Ziconotide.
Lithium citrate The risk or severity of adverse effects can be increased when Ziconotide is combined with Lithium citrate.
Lithium carbonate The risk or severity of adverse effects can be increased when Ziconotide is combined with Lithium carbonate.
Lithium hydroxide The risk or severity of adverse effects can be increased when Ziconotide is combined with Lithium hydroxide.
Ethanol Ziconotide may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Ziconotide may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Ziconotide.
Fluvoxamine The risk or severity of adverse effects can be increased when Ziconotide is combined with Fluvoxamine.
Duloxetine The risk or severity of adverse effects can be increased when Ziconotide is combined with Duloxetine.
Paroxetine The risk or severity of adverse effects can be increased when Ziconotide is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Ziconotide is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Ziconotide is combined with Sibutramine.
Zimelidine The risk or severity of adverse effects can be increased when Ziconotide is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Ziconotide is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Ziconotide is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Ziconotide is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Ziconotide is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Ziconotide is combined with Indalpine.
Alaproclate The risk or severity of adverse effects can be increased when Ziconotide is combined with Alaproclate.
Citalopram The risk or severity of adverse effects can be increased when Ziconotide is combined with Citalopram.
Escitalopram The risk or severity of adverse effects can be increased when Ziconotide is combined with Escitalopram.
Nefazodone The risk or severity of adverse effects can be increased when Ziconotide is combined with Nefazodone.
Trazodone The risk or severity of adverse effects can be increased when Ziconotide is combined with Trazodone.
Tocainide Tocainide may increase the arrhythmogenic activities of Ziconotide.
Aprindine Aprindine may increase the arrhythmogenic activities of Ziconotide.
Carteolol Ziconotide may increase the arrhythmogenic activities of Carteolol.
Metipranolol Ziconotide may increase the arrhythmogenic activities of Metipranolol.
Xylometazoline Ziconotide may increase the arrhythmogenic activities of Xylometazoline.
Sparteine Ziconotide may increase the arrhythmogenic activities of Sparteine.
Fasudil Ziconotide may increase the arrhythmogenic activities of Fasudil.
Tiracizine Ziconotide may increase the arrhythmogenic activities of Tiracizine.
Ethacizine Ziconotide may increase the arrhythmogenic activities of Ethacizine.
Hydroquinine Ziconotide may increase the arrhythmogenic activities of Hydroquinine.
Bioallethrin Ziconotide may increase the arrhythmogenic activities of Bioallethrin.
Fosfructose Ziconotide may increase the arrhythmogenic activities of Fosfructose.
Hydroquinidine Ziconotide may increase the arrhythmogenic activities of Hydroquinidine.
SOR-C13 Ziconotide may increase the arrhythmogenic activities of SOR-C13.
Digoxin Digoxin may increase the arrhythmogenic activities of Ziconotide.
Acetyldigitoxin Acetyldigitoxin may increase the arrhythmogenic activities of Ziconotide.
Deslanoside Deslanoside may increase the arrhythmogenic activities of Ziconotide.
Cymarin Ziconotide may increase the arrhythmogenic activities of Cymarin.
Metildigoxin Ziconotide may increase the arrhythmogenic activities of Metildigoxin.
Acetyldigoxin Ziconotide may increase the arrhythmogenic activities of Acetyldigoxin.
Hyoscyamine Hyoscyamine may increase the arrhythmogenic activities of Ziconotide.
Niguldipine Ziconotide may increase the arrhythmogenic activities of Niguldipine.
Diltiazem Diltiazem may increase the arrhythmogenic activities of Ziconotide.
Nimodipine Nimodipine may increase the arrhythmogenic activities of Ziconotide.
Cinnarizine Cinnarizine may increase the arrhythmogenic activities of Ziconotide.
Atropine Atropine may increase the arrhythmogenic activities of Ziconotide.
Adenosine Adenosine may increase the arrhythmogenic activities of Ziconotide.
Levosimendan Levosimendan may increase the arrhythmogenic activities of Ziconotide.
Nifedipine Nifedipine may increase the arrhythmogenic activities of Ziconotide.
Flecainide Flecainide may increase the arrhythmogenic activities of Ziconotide.
Prenylamine Prenylamine may increase the arrhythmogenic activities of Ziconotide.
Azimilide Azimilide may increase the arrhythmogenic activities of Ziconotide.
Tedisamil Tedisamil may increase the arrhythmogenic activities of Ziconotide.
Nilvadipine Ziconotide may increase the arrhythmogenic activities of Nilvadipine.
Fendiline Ziconotide may increase the arrhythmogenic activities of Fendiline.
Benidipine Ziconotide may increase the arrhythmogenic activities of Benidipine.
Simendan Ziconotide may increase the arrhythmogenic activities of Simendan.
Otilonium Ziconotide may increase the arrhythmogenic activities of Otilonium.
Nizofenone Ziconotide may increase the arrhythmogenic activities of Nizofenone.
Bunaftine Ziconotide may increase the arrhythmogenic activities of Bunaftine.
Lorcainide Ziconotide may increase the arrhythmogenic activities of Lorcainide.
Dexverapamil Ziconotide may increase the arrhythmogenic activities of Dexverapamil.
Disopyramide Disopyramide may increase the arrhythmogenic activities of Ziconotide.
Ibutilide Ibutilide may increase the arrhythmogenic activities of Ziconotide.
Procainamide Procainamide may increase the arrhythmogenic activities of Ziconotide.
Bepridil Bepridil may increase the arrhythmogenic activities of Ziconotide.
Terodiline Ziconotide may increase the arrhythmogenic activities of Terodiline.
Eperisone Ziconotide may increase the arrhythmogenic activities of Eperisone.
Tropisetron Ziconotide may increase the arrhythmogenic activities of Tropisetron.
Isradipine Isradipine may increase the arrhythmogenic activities of Ziconotide.
Amlodipine Amlodipine may increase the arrhythmogenic activities of Ziconotide.

Target Protein

Voltage-dependent N-type calcium channel subunit alpha-1B CACNA1B
Voltage-dependent P/Q-type calcium channel subunit alpha-1A CACNA1A

Referensi & Sumber

Synthesis reference: Avi Tovi, Chaim Eidelman, Shimon Shushan, Shai Elster, Alon Hagi, Alexander Ivchenko, Gabriel-Marcus Butilca, Gil Zaoui, Eleonora Alterman, Leah Bar-Oz, Tehila Gadi. "Methods for the production of peptide having a c-terminal amide." Patent WO2006119388A2, issued November 09, 2006.
Artikel (PubMed)
  • PMID: 17963128
    Skov MJ, Beck JC, de Kater AW, Shopp GM: Nonclinical safety of ziconotide: an intrathecal analgesic of a new pharmaceutical class. Int J Toxicol. 2007 Sep-Oct;26(5):411-21.
  • PMID: 15578997
    Miljanich GP: Ziconotide: neuronal calcium channel blocker for treating severe chronic pain. Curr Med Chem. 2004 Dec;11(23):3029-40.
  • PMID: 19300539
    McGivern JG: Ziconotide: a review of its pharmacology and use in the treatment of pain. Neuropsychiatr Dis Treat. 2007 Feb;3(1):69-85.
  • PMID: 4071055
    Olivera BM, Gray WR, Zeikus R, McIntosh JM, Varga J, Rivier J, de Santos V, Cruz LJ: Peptide neurotoxins from fish-hunting cone snails. Science. 1985 Dec 20;230(4732):1338-43. doi: 10.1126/science.4071055.
  • PMID: 2441741
    Olivera BM, Cruz LJ, de Santos V, LeCheminant GW, Griffin D, Zeikus R, McIntosh JM, Galyean R, Varga J, Gray WR, et al.: Neuronal calcium channel antagonists. Discrimination between calcium channel subtypes using omega-conotoxin from Conus magus venom. Biochemistry. 1987 Apr 21;26(8):2086-90. doi: 10.1021/bi00382a004.
  • PMID: 8102803
    Valentino K, Newcomb R, Gadbois T, Singh T, Bowersox S, Bitner S, Justice A, Yamashiro D, Hoffman BB, Ciaranello R, et al.: A selective N-type calcium channel antagonist protects against neuronal loss after global cerebral ischemia. Proc Natl Acad Sci U S A. 1993 Aug 15;90(16):7894-7. doi: 10.1073/pnas.90.16.7894.
  • PMID: 27756538
    Bourinet E, Zamponi GW: Block of voltage-gated calcium channels by peptide toxins. Neuropharmacology. 2017 Dec;127:109-115. doi: 10.1016/j.neuropharm.2016.10.016. Epub 2016 Oct 15.
  • PMID: 21150297
    Park J, Luo ZD: Calcium channel functions in pain processing. Channels (Austin). 2010 Nov-Dec;4(6):510-7. doi: 10.4161/chan.4.6.12869. Epub 2010 Nov 1.
Menampilkan 8 dari 17 artikel.

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