Peringatan Keamanan

The oral LD50 in rats is 145 mg/kg.L40273

Baclofen withdrawal symptoms typically occur within hours to days following interruption of either oral or intrathecal drug formulations.A245338 Abrupt discontinuation of baclofen is not advised.L39429 Clinical manifestations of baclofen overdose may include altered mental status, somnolence, seizure, hypothermia, respiratory depression, and coma. Overdose from baclofen oral tablets resulted in vomiting, lightheadedness, drowsiness, muscular hypotonia, accommodation disorders, coma, respiratory depression, and seizures.A245323, L40134 Most overdose symptoms are neurological but uncommon cardiovascular effects such as hypertension, bradycardia, and tachycardia may be observed.A37219 In case of overdose, symptomatic treatment and gastric decontamination should be initiated. When the patient is alert, gastric emptying should be performed by inducing emesis and then performing lavage while maintaining an adequate airway and respiration. Emesis should not be induced in unconscious patients.A245323, L40134

Baclofen

DB00181

small molecule approved

Deskripsi

Baclofen is a gamma-aminobutyric acid (GABA) agonist used as a skeletal muscle relaxant. Although originally designed in 1962 to treat epilepsy, baclofen was not effective in treating this condition but instead was shown to reduce spasticity in selected patients.A245338 Baclofen was reintroduced in 1971 as a treatment for spasticity and was later approved by the FDA in 1977.A245323, A245338 Baclofen is used to manage severe muscle spasms of cerebral or spinal cord origins, including multiple sclerosis and traumatic brain injury.L39429

Baclofen was investigated for use in alcohol dependence and withdrawal; however, evidence is limited and there is inconsistent evidence to suggest its clinical efficacy in managing alcohol dependence or withdrawal symptoms.A173905, A173908, A245338

Struktur Molekul 2D

Berat 213.661
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life is 2-6 hours after oral administration and 1-5 hours following intrathecal administration.[A245338] The apparent elimination half-life of baclofen oral suspension or granules is about 5.6 hours.[L40134]
Volume Distribusi The volume of distribution of baclofen is 0.7 L/kg.[L40278] As baclofen is mainly water-soluble, it does not readily cross the blood-brain barrier.[A245333] Drug concentrations of baclofen in the cerebrospinal fluid are approximately 8.5 times lower than in the plasma.[L40278]
Klirens (Clearance) The systemic clearance (CL/F) was 180 mL/min and the renal clearance was 103 mL/min following oral administration.[A245343]

Absorpsi

Baclofen has an oral bioavailability of 70% to 85%. Following oral administration, it is rapidly absorbed through the gastrointestinal tract with peak plasma concentrations being reached two to three hours after ingestion.A245323 Peak effect is observed about four hours after intrathecal administration.A245338 The absorption is dose-dependent and increases with higher doses.A245323 There is intersubject variation in absorption.L40134 Administration of oral baclofen suspension with a high-fat meal resulted in 9% decrease in AUC and 33% decrease in Cmax compared to the fasted state.L40134

Metabolisme

Approximately 15% of the oral dose is metabolized in the liver, mainly by deamination.A245338 Deamination yields the main metabolite, ?-(p-chlorophenyl)-4-hydroxybutyric acid, which is pharmacologically inactive.L40278

Rute Eliminasi

About 70-80% of baclofen is eliminated in an unchanged form by renal excretion A245323, A245338 within 72 hours of administration. About 5% of the dose is excreted via the kidneys as metabolites.L40278 There is intersubject variation in elimination.L40134

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with food. Take with food or milk to reduce gastric irritation.

Interaksi Obat

1556 Data
Buprenorphine Baclofen 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 Baclofen.
Dronabinol Baclofen may increase the central nervous system depressant (CNS depressant) activities of Dronabinol.
Droperidol Baclofen may increase the central nervous system depressant (CNS depressant) activities of Droperidol.
Hydrocodone Baclofen 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 Baclofen.
Magnesium sulfate The therapeutic efficacy of Baclofen can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
Mirtazapine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Baclofen may increase the central nervous system depressant (CNS depressant) activities of Nabilone.
Orphenadrine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Baclofen may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Baclofen may increase the central nervous system depressant (CNS depressant) activities of Perampanel.
Pramipexole Baclofen may increase the sedative activities of Pramipexole.
Ropinirole Baclofen may increase the sedative activities of Ropinirole.
Rotigotine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Rotigotine.
Rufinamide Baclofen may increase the central nervous system depressant (CNS depressant) activities of Rufinamide.
Sodium oxybate Baclofen may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Baclofen 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 Baclofen.
Thalidomide Baclofen may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Baclofen may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Baclofen.
Ethanol Baclofen may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Brimonidine.
Lacidipine Baclofen may increase the hypotensive activities of Lacidipine.
Fluvoxamine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Fluvoxamine.
Citalopram Baclofen may increase the central nervous system depressant (CNS depressant) activities of Citalopram.
Duloxetine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Duloxetine.
Trazodone Baclofen may increase the central nervous system depressant (CNS depressant) activities of Trazodone.
Paroxetine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Paroxetine.
Sertraline Baclofen may increase the central nervous system depressant (CNS depressant) activities of Sertraline.
Sibutramine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Sibutramine.
Nefazodone Baclofen may increase the central nervous system depressant (CNS depressant) activities of Nefazodone.
Escitalopram Baclofen may increase the central nervous system depressant (CNS depressant) activities of Escitalopram.
Zimelidine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Zimelidine.
Dapoxetine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Dapoxetine.
Milnacipran Baclofen may increase the central nervous system depressant (CNS depressant) activities of Milnacipran.
Desvenlafaxine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Desvenlafaxine.
Seproxetine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Seproxetine.
Levomilnacipran Baclofen may decrease the excretion rate of Levomilnacipran which could result in a higher serum level.
Indalpine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Indalpine.
Ritanserin Baclofen may increase the central nervous system depressant (CNS depressant) activities of Ritanserin.
Alaproclate Baclofen may increase the central nervous system depressant (CNS depressant) activities of Alaproclate.
Benzatropine Baclofen may decrease the excretion rate of Benzatropine which could result in a higher serum level.
Cyproheptadine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
Propiomazine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Propiomazine.
Propantheline Baclofen may decrease the excretion rate of Propantheline which could result in a higher serum level.
Dicyclomine Baclofen may decrease the excretion rate of Dicyclomine which could result in a higher serum level.
Maprotiline Baclofen may increase the central nervous system depressant (CNS depressant) activities of Maprotiline.
Tolterodine Baclofen may decrease the excretion rate of Tolterodine which could result in a higher serum level.
Flavoxate Baclofen may decrease the excretion rate of Flavoxate which could result in a higher serum level.
Tiotropium Baclofen may decrease the excretion rate of Tiotropium which could result in a higher serum level.
Pizotifen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Pizotifen.
Fesoterodine Baclofen may decrease the excretion rate of Fesoterodine which could result in a higher serum level.
Aclidinium Baclofen may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Trimebutine Baclofen may decrease the excretion rate of Trimebutine which could result in a higher serum level.
Imidafenacin Baclofen may decrease the excretion rate of Imidafenacin which could result in a higher serum level.
Propiverine Baclofen may decrease the excretion rate of Propiverine which could result in a higher serum level.
Zopiclone Baclofen may increase the central nervous system depressant (CNS depressant) activities of Zopiclone.
Botulinum toxin type B Baclofen may increase the central nervous system depressant (CNS depressant) activities of Botulinum toxin type B.
Botulinum toxin type A The therapeutic efficacy of Botulinum toxin type A can be increased when used in combination with Baclofen.
Tryptophan Baclofen may increase the central nervous system depressant (CNS depressant) activities of Tryptophan.
Lorazepam Baclofen may increase the central nervous system depressant (CNS depressant) activities of Lorazepam.
Ethchlorvynol Baclofen may increase the central nervous system depressant (CNS depressant) activities of Ethchlorvynol.
Eletriptan Baclofen may increase the central nervous system depressant (CNS depressant) activities of Eletriptan.
Enflurane Baclofen may increase the central nervous system depressant (CNS depressant) activities of Enflurane.
Temazepam Baclofen may increase the central nervous system depressant (CNS depressant) activities of Temazepam.
Reboxetine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Reboxetine.
Butabarbital Baclofen may increase the central nervous system depressant (CNS depressant) activities of Butabarbital.
Butalbital Baclofen may increase the central nervous system depressant (CNS depressant) activities of Butalbital.
Methysergide Baclofen may increase the central nervous system depressant (CNS depressant) activities of Methysergide.
Cabergoline Baclofen may increase the central nervous system depressant (CNS depressant) activities of Cabergoline.
Phenytoin Baclofen may increase the central nervous system depressant (CNS depressant) activities of Phenytoin.
Clemastine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Clemastine.
Venlafaxine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Venlafaxine.
Etomidate Baclofen may increase the central nervous system depressant (CNS depressant) activities of Etomidate.
Morphine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Morphine.
Talbutal Baclofen may increase the central nervous system depressant (CNS depressant) activities of Talbutal.
Pentobarbital Baclofen may increase the central nervous system depressant (CNS depressant) activities of Pentobarbital.
Valproic acid Baclofen may increase the central nervous system depressant (CNS depressant) activities of Valproic acid.
Zolmitriptan Baclofen may increase the central nervous system depressant (CNS depressant) activities of Zolmitriptan.
Dihydroergotamine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Dihydroergotamine.
Tolcapone Baclofen may increase the central nervous system depressant (CNS depressant) activities of Tolcapone.
Hydromorphone Baclofen may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.
Olanzapine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Olanzapine.
Cetirizine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Cetirizine.
Trimethadione Baclofen may increase the central nervous system depressant (CNS depressant) activities of Trimethadione.
Clobazam The risk or severity of sedation, somnolence, and CNS depression can be increased when Clobazam is combined with Baclofen.
Chlorzoxazone Baclofen may increase the central nervous system depressant (CNS depressant) activities of Chlorzoxazone.
Clozapine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Clozapine.
Meprobamate Baclofen may increase the central nervous system depressant (CNS depressant) activities of Meprobamate.
Thiethylperazine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Thiethylperazine.
Sulpiride Baclofen may increase the central nervous system depressant (CNS depressant) activities of Sulpiride.
Alprazolam Baclofen may increase the central nervous system depressant (CNS depressant) activities of Alprazolam.
Dexbrompheniramine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Dexbrompheniramine.
Loxapine Baclofen may increase the central nervous system depressant (CNS depressant) activities of Loxapine.
Remoxipride Baclofen may increase the central nervous system depressant (CNS depressant) activities of Remoxipride.

Target Protein

Gamma-aminobutyric acid type B receptor subunit 2 GABBR2
C-X-C chemokine receptor type 4 CXCR4
Gamma-aminobutyric acid type B receptor subunit 1 GABBR1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 23869179
    Brennan JL, Leung JG, Gagliardi JP, Rivelli SK, Muzyk AJ: Clinical effectiveness of baclofen for the treatment of alcohol dependence: a review. Clin Pharmacol. 2013 Jul 3;5:99-107. doi: 10.2147/CPAA.S32434. Print 2013.
  • PMID: 28822350
    Liu J, Wang LN: Baclofen for alcohol withdrawal. Cochrane Database Syst Rev. 2017 Aug 20;8:CD008502. doi: 10.1002/14651858.CD008502.pub5.
  • PMID: 16182939
    Chen K, Li HZ, Ye N, Zhang J, Wang JJ: Role of GABAB receptors in GABA and baclofen-induced inhibition of adult rat cerebellar interpositus nucleus neurons in vitro. Brain Res Bull. 2005 Oct 30;67(4):310-8. doi: 10.1016/j.brainresbull.2005.07.004.
  • PMID: 22559224
    Fu Z, Yang H, Xiao Y, Zhao G, Huang H: The gamma-aminobutyric acid type B (GABAB) receptor agonist baclofen inhibits morphine sensitization by decreasing the dopamine level in rat nucleus accumbens. Behav Brain Funct. 2012 Jul 10;8:20. doi: 10.1186/1744-9081-8-20.
  • PMID: 30459646
    de Beaurepaire R: A Review of the Potential Mechanisms of Action of Baclofen in Alcohol Use Disorder. Front Psychiatry. 2018 Oct 17;9:506. doi: 10.3389/fpsyt.2018.00506. eCollection 2018.
  • PMID: 30252293
    Ghanavatian S, Derian A: Baclofen .
  • PMID: 28233010
    Ertzgaard P, Campo C, Calabrese A: Efficacy and safety of oral baclofen in the management of spasticity: A rationale for intrathecal baclofen. J Rehabil Med. 2017 Mar 6;49(3):193-203. doi: 10.2340/16501977-2211.
  • PMID: 34158937
    Romito JW, Turner ER, Rosener JA, Coldiron L, Udipi A, Nohrn L, Tausiani J, Romito BT: Baclofen therapeutics, toxicity, and withdrawal: A narrative review. SAGE Open Med. 2021 Jun 3;9:20503121211022197. doi: 10.1177/20503121211022197. eCollection 2021.
Menampilkan 8 dari 10 artikel.

Contoh Produk & Brand

Produk: 468 • International brands: 3
Produk
  • Apo-baclofen
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Apo-baclofen
    Tablet • 20 mg • Oral • Canada • Generic • Approved
  • Ava-baclofen
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Ava-baclofen
    Tablet • 20 mg • Oral • Canada • Generic • Approved
  • Baclofen
    Tablet • 10 mg/1 • Oral • US • Approved
  • Baclofen
    Tablet • 20 mg/1 • Oral • US • Approved
  • Baclofen
    Tablet • 10 mg/1 • Oral • US • Generic • Approved
  • Baclofen
    Tablet • 20 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 468 produk.
International Brands
  • Baclon — Uniao Quimica (Brazil)
  • Lioresal Intrathecal — Novartis Pharmaceuticals
  • Nu-Baclofen — Nu-Pharm

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