Peringatan Keamanan

The oral LD50 of cyclobenzaprine in mice and rats is 338 mg/kg and 425 mg/kg, respectively. Signs of overdose may develop rapidly after ingestion and commonly include significant drowsiness and tachycardia, with less common manifestations including tremor, agitation, ataxia, GI upset, and other CNS effects such as confusion and hallucinations. Potentially critical manifestations, though rare, include cardiac arrest or dysrhythmias, severe hypotension, seizures, and neuroleptic malignant syndrome.L8408,L8411

As the management of cyclobenzaprine overdose is complex and ever-changing, it is recommended that a poison control center be consulted prior to treatment. Typical management involves gastrointestinal decontamination, close cardiac monitoring, and monitoring for signs of CNS or respiratory depression. As cyclobenzaprine exists in relatively low concentrations in plasma, monitoring of drug plasma levels should not guide management and dialysis is likely of no value.L8408,L8411

Cyclobenzaprine

DB00924

small molecule approved

Deskripsi

Cyclobenzaprine, a centrally-acting muscle relaxant, was first synthesized in 1961A185039 and has been available for human use since 1977.A184982 It was initially studied for use as antidepressant given its structural similarity to tricyclic antidepressants - it differs from Amitriptyline by only a single double bond.A185039,A184982 Since its approval, it has remained relatively popular as an adjunctive, short-term treatment for acute skeletal muscle spasms secondary to musculoskeletal injury.

Struktur Molekul 2D

Berat 275.3874
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The effective half-life of cyclobenzaprine in young healthy subjects is approximately 18 hours.[A184940,L8408,L8411] These values are extended in the elderly and those with hepatic insufficiency, with a mean effective half-life of 33.4 hours and 46.2 hours in these groups, respectively.[A184940]
Volume Distribusi The volume of distribution of cyclobenzaprine is approximately 146 L.[A185039] The combination of high plasma clearance despite a relatively long half-life observed with cyclobenzaprine is suggestive of extensive tissue distribution.[A185054,A184940]
Klirens (Clearance) The approximate plasma clearance of cyclobenzaprine is 0.7 L/min.[A184940,L8408,L8411]

Absorpsi

The oral bioavailability of cyclobenzaprine has been estimated to be between 0.33 and 0.55.A184940,A185039,L8408 Cmax is between 5-35 ng/mL and is achieved after 4 hours (Tmax).L8408,A184982 AUC over an 8 hour dosing interval was reported to be approximately 177 ng.hr/mL.L8408

Metabolisme

Cyclobenzaprine is extensively metabolized in the liver via both oxidative and conjugative pathways.L8408,A184940,A184982 Oxidative metabolism, mainly N-demethylation, is catalyzed primarily by CYP3A4 and CYP1A2 (with CYP2D6 implicated to a lesser extent) and is responsible for the major metabolite desmethylcyclobenzaprineL8408,A14914,A184982. Cyclobenzaprine also undergoes N-glucuronidation in the liver catalyzed by UGT1A4 and UGT2B10A184916, and has been shown to undergo enterohepatic circulation.L8408,A184940,A184982

Rute Eliminasi

After administration of a radio-labeled dose of cyclobenzaprine, 38-51% of radioactivity was excreted in the urine while 14-15% was excreted in the feces.L8411 Cyclobenzaprine is highly metabolized, with only approximately 1% of this same radio-labeled dose recovered in the urine as unchanged drug. Metabolites excreted in the urine are likely water-soluble glucuronide conjugates.L8411

Interaksi Makanan

1 Data
  • 1. Avoid alcohol. Cyclobenzaprine is a central nervous system depressant which may be potentiated by the co-administration of alcohol.

Interaksi Obat

1043 Data
Deferasirox The serum concentration of Cyclobenzaprine can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Cyclobenzaprine can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Cyclobenzaprine can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Cyclobenzaprine can be decreased when it is combined with Teriflunomide.
Buprenorphine Cyclobenzaprine 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 Cyclobenzaprine.
Hydrocodone Cyclobenzaprine 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 Cyclobenzaprine.
Magnesium sulfate The therapeutic efficacy of Cyclobenzaprine can be increased when used in combination with Magnesium sulfate.
Metyrosine Cyclobenzaprine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Cyclobenzaprine.
Pramipexole Cyclobenzaprine may increase the sedative activities of Pramipexole.
Ropinirole Cyclobenzaprine may increase the sedative activities of Ropinirole.
Suvorexant Cyclobenzaprine 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 Cyclobenzaprine.
Thalidomide Cyclobenzaprine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Cyclobenzaprine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Tramadol The risk or severity of serotonin syndrome and seizure can be increased when Cyclobenzaprine is combined with Tramadol.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Cyclobenzaprine.
Tranylcypromine Cyclobenzaprine may increase the serotonergic activities of Tranylcypromine.
Phenelzine Cyclobenzaprine may increase the serotonergic activities of Phenelzine.
Selegiline Cyclobenzaprine may increase the serotonergic activities of Selegiline.
Moclobemide Cyclobenzaprine may increase the serotonergic activities of Moclobemide.
Isocarboxazid Cyclobenzaprine may increase the serotonergic activities of Isocarboxazid.
Rasagiline Cyclobenzaprine may increase the serotonergic activities of Rasagiline.
Pargyline Cyclobenzaprine may increase the serotonergic activities of Pargyline.
Minaprine Cyclobenzaprine may increase the serotonergic activities of Minaprine.
Iproniazid Cyclobenzaprine may increase the serotonergic activities of Iproniazid.
Nialamide Cyclobenzaprine may increase the serotonergic activities of Nialamide.
Pirlindole Cyclobenzaprine may increase the serotonergic activities of Pirlindole.
Toloxatone Cyclobenzaprine may increase the serotonergic activities of Toloxatone.
Hydracarbazine Cyclobenzaprine may increase the serotonergic activities of Hydracarbazine.
Benmoxin Cyclobenzaprine may increase the serotonergic activities of Benmoxin.
Mebanazine Cyclobenzaprine may increase the serotonergic activities of Mebanazine.
Octamoxin Cyclobenzaprine may increase the serotonergic activities of Octamoxin.
Pheniprazine Cyclobenzaprine may increase the serotonergic activities of Pheniprazine.
Phenoxypropazine Cyclobenzaprine may increase the serotonergic activities of Phenoxypropazine.
Pivhydrazine Cyclobenzaprine may increase the serotonergic activities of Pivhydrazine.
Safrazine Cyclobenzaprine may increase the serotonergic activities of Safrazine.
Caroxazone Cyclobenzaprine may increase the serotonergic activities of Caroxazone.
Furazolidone Cyclobenzaprine may increase the serotonergic activities of Furazolidone.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline Cyclobenzaprine may increase the serotonergic activities of 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
Harmaline Cyclobenzaprine may increase the serotonergic activities of Harmaline.
Brofaromine Cyclobenzaprine may increase the serotonergic activities of Brofaromine.
Procaine Cyclobenzaprine may increase the serotonergic activities of Procaine.
Procarbazine Cyclobenzaprine may increase the serotonergic activities of Procarbazine.
Safinamide Cyclobenzaprine may increase the serotonergic activities of Safinamide.
Clorgiline Cyclobenzaprine may increase the serotonergic activities of Clorgiline.
Linezolid Cyclobenzaprine may increase the serotonergic activities of Linezolid.
Dicoumarol The risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Dicoumarol.
Phenindione The risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Phenindione.
Phenprocoumon The risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Phenprocoumon.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Coumarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Fluindione.
Clorindione The risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Diphenadione.
Tioclomarol The risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Tioclomarol.
(S)-Warfarin The risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with (S)-Warfarin.
Abiraterone The serum concentration of Cyclobenzaprine can be increased when it is combined with Abiraterone.
Mirtazapine The risk or severity of CNS depression can be increased when Cyclobenzaprine is combined with Mirtazapine.
Cyproterone acetate The metabolism of Cyclobenzaprine can be increased when combined with Cyproterone acetate.
Ethanol Cyclobenzaprine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Cyclobenzaprine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Methylene blue Cyclobenzaprine may increase the serotonergic activities of Methylene blue.
Cocaine The risk or severity of serotonin syndrome can be increased when Cocaine is combined with Cyclobenzaprine.
Nicardipine The metabolism of Cyclobenzaprine can be decreased when combined with Nicardipine.
Rifampin The metabolism of Cyclobenzaprine can be increased when combined with Rifampicin.
Albendazole The metabolism of Cyclobenzaprine can be increased when combined with Albendazole.
Caffeine The metabolism of Cyclobenzaprine can be decreased when combined with Caffeine.
Moxifloxacin The metabolism of Cyclobenzaprine can be decreased when combined with Moxifloxacin.
Mexiletine The metabolism of Cyclobenzaprine can be decreased when combined with Mexiletine.
Gatifloxacin The metabolism of Cyclobenzaprine can be decreased when combined with Gatifloxacin.
Simeprevir The metabolism of Cyclobenzaprine can be decreased when combined with Simeprevir.
Lobeglitazone The metabolism of Cyclobenzaprine can be decreased when combined with Lobeglitazone.
Pazufloxacin The metabolism of Cyclobenzaprine can be decreased when combined with Pazufloxacin.
Osilodrostat The metabolism of Cyclobenzaprine can be decreased when combined with Osilodrostat.
Osimertinib The serum concentration of Cyclobenzaprine can be decreased when it is combined with Osimertinib.
Pregabalin The therapeutic efficacy of Cyclobenzaprine can be increased when used in combination with Pregabalin.
Vemurafenib The serum concentration of Cyclobenzaprine can be increased when it is combined with Vemurafenib.
Pitolisant The serum concentration of Cyclobenzaprine can be decreased when it is combined with Pitolisant.
Lofexidine The therapeutic efficacy of Cyclobenzaprine can be increased when used in combination with Lofexidine.
Metreleptin The metabolism of Cyclobenzaprine can be increased when combined with Metreleptin.
Nevirapine The metabolism of Cyclobenzaprine can be decreased when combined with Nevirapine.
Cimetidine The metabolism of Cyclobenzaprine can be decreased when combined with Cimetidine.
Trovafloxacin The metabolism of Cyclobenzaprine can be decreased when combined with Trovafloxacin.
Famotidine The metabolism of Cyclobenzaprine can be decreased when combined with Famotidine.
Pipemidic acid The metabolism of Cyclobenzaprine can be decreased when combined with Pipemidic acid.
Ethambutol The metabolism of Cyclobenzaprine can be decreased when combined with Ethambutol.
Belinostat The metabolism of Cyclobenzaprine can be increased when combined with Belinostat.
Rucaparib The metabolism of Cyclobenzaprine can be increased when combined with Rucaparib.
Insulin pork The metabolism of Cyclobenzaprine can be increased when combined with Insulin pork.
Phenylephrine The metabolism of Cyclobenzaprine can be increased when combined with Phenylephrine.
Nafcillin The metabolism of Cyclobenzaprine can be increased when combined with Nafcillin.
Primaquine The metabolism of Cyclobenzaprine can be decreased when combined with Primaquine.
NN344 The metabolism of Cyclobenzaprine can be increased when combined with NN344.
Dovitinib The metabolism of Cyclobenzaprine can be increased when combined with Dovitinib.
Armodafinil The metabolism of Cyclobenzaprine can be increased when combined with Armodafinil.
beta-Naphthoflavone The metabolism of Cyclobenzaprine can be increased when combined with beta-Naphthoflavone.

Target Protein

Alpha-2C adrenergic receptor ADRA2C
5-hydroxytryptamine receptor 2A HTR2A
5-hydroxytryptamine receptor 2B HTR2B
5-hydroxytryptamine receptor 2C HTR2C
5-hydroxytryptamine receptor 6 HTR6
Sodium-dependent serotonin transporter SLC6A4
Sodium-dependent noradrenaline transporter SLC6A2
5-hydroxytryptamine receptor 7 HTR7
Toll-like receptor 4 TLR4
Aldehyde oxidase AOX1

Referensi & Sumber

Synthesis reference: Villani, F.J.; US. Patent 3,409,640; November 5,1968; assigned to Schering Corporation.
Artikel (PubMed)
  • PMID: 8818577
    Wang RW, Liu L, Cheng H: Identification of human liver cytochrome P450 isoforms involved in the in vitro metabolism of cyclobenzaprine. Drug Metab Dispos. 1996 Jul;24(7):786-91.
  • PMID: 28803208
    Lu D, Xie Q, Wu B: N-glucuronidation catalyzed by UGT1A4 and UGT2B10 in human liver microsomes: Assay optimization and substrate identification. J Pharm Biomed Anal. 2017 Oct 25;145:692-703. doi: 10.1016/j.jpba.2017.07.037. Epub 2017 Aug 4.
  • PMID: 8884233
    Kobayashi H, Hasegawa Y, Ono H: Cyclobenzaprine, a centrally acting muscle relaxant, acts on descending serotonergic systems. Eur J Pharmacol. 1996 Sep 5;311(1):29-35.
  • PMID: 12498911
    Honda M, Nishida T, Ono H: Tricyclic analogs cyclobenzaprine, amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-HT(2) receptors. Eur J Pharmacol. 2003 Jan 1;458(1-2):91-9.
  • PMID: 21975349
    Mestres J, Seifert SA, Oprea TI: Linking pharmacology to clinical reports: cyclobenzaprine and its possible association with serotonin syndrome. Clin Pharmacol Ther. 2011 Nov;90(5):662-5. doi: 10.1038/clpt.2011.177. Epub 2011 Oct 5.
  • PMID: 20381591
    Hutchinson MR, Loram LC, Zhang Y, Shridhar M, Rezvani N, Berkelhammer D, Phipps S, Foster PS, Landgraf K, Falke JJ, Rice KC, Maier SF, Yin H, Watkins LR: Evidence that tricyclic small molecules may possess toll-like receptor and myeloid differentiation protein 2 activity. Neuroscience. 2010 Jun 30;168(2):551-63. doi: 10.1016/j.neuroscience.2010.03.067. Epub 2010 Apr 8.
  • PMID: 14681337
    Obach RS, Huynh P, Allen MC, Beedham C: Human liver aldehyde oxidase: inhibition by 239 drugs. J Clin Pharmacol. 2004 Jan;44(1):7-19.
  • PMID: 11808825
    Winchell GA, King JD, Chavez-Eng CM, Constanzer ML, Korn SH: Cyclobenzaprine pharmacokinetics, including the effects of age, gender, and hepatic insufficiency. J Clin Pharmacol. 2002 Jan;42(1):61-9. doi: 10.1177/0091270002042001007.
Menampilkan 8 dari 13 artikel.

Contoh Produk & Brand

Produk: 597 • International brands: 1
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International Brands
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