Peringatan Keamanan

The oral LD50 in mouse and rat is 205 mg/kg and 245 mg/kg, respectively.MSDS

Fatal cases of overdose of up to 15g of lamotrigine have been reported. Overdose with lamotrigine has been manifested by ataxia, nystagmus, increased seizures, decreased level of consciousness, coma, and intraventricular conduction delay. Though no known antidote exists for lamotrigine, hospitalization and general supportive measures should be employed in the case of a suspected lamotrigine overdose. Gastric lavage and emesis may be warranted with simultaneous protection of the airway. It is uncertain at this time whether hemodialysis is an effective means of removing lamotrigine from the sytemic circulation.L12183,L9404

Lamotrigine

DB00555

small molecule approved investigational

Deskripsi

Lamotrigine is an antiepileptic drug belonging in the phenyltriazine class. It is used in the treatment of both epilepsy and as a mood stabilizer in bipolar disorder. Lamotrigine is the first medication since lithium granted Food and Drug Administration (FDA) approval for the maintenance treatment of bipolar type I. It is approved for use in more than 30 countries.A191350

Lamotrigine has relatively few side-effects and does not require laboratory monitoring. While it is indicated for epilepsy and bipolar disorders, there is evidence that lamotrigine could have some clinical efficacy in certain neuropathic pain states.A849,A850

Struktur Molekul 2D

Berat 256.091
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The average elimination half-life of lamotrigine ranges from approximately 14-59 hours. The value is dependent on the dose administered, concomitant drug therapy, as well as disease status.[A191946,L12183] One pharmacokinetic study revealed a half-life of 22.8 to 37.4 hours in healthy volunteers. It also reported that enzyme-inducing antiepileptic drugs such as pheobarbital, phenytoin, or carbamazepine decrease the half-life of lamotrigine. On the other hand, valproic acid increases the half-life of lamotrigine (in the range of 48-59 hours).[A191946]
Volume Distribusi The mean apparent volume of distribution (Vd/F) of lamotrigine following oral administration ranges from 0.9 to 1.3 L/kg and is independent of dose administered. Lamotrigine accumulated in the kidney of the male rat, and likely behaves in a similar fashion in humans. Lamotrigine also binds to tissues containing melanin, such as the eyes and pigmented skin.[L9404,L12183]
Klirens (Clearance) The mean apparent plasma clearance (Cl/F) ranges from 0.18 to 1.21 mL/min/kg. The values vary depending on dosing regimen, concomitant antiepileptic medications, and disease state of the individual.[L9404] In one study, healthy volunteers on lamictal monotherapy showed a clearance of about 0.44 mL/min/kg after a single dose.[L9404]

Absorpsi

Lamotrigine is rapidly and entirely absorbed with minimal first-pass metabolism effects, with a bioavailability estimated at 98%. Cmax is reached in the range of 1.4 to 4.8 hours post-dose, but this depends on the dose administered, concomitant medications, and epileptic status. The rate and extent of lamictal absorption is considered equivalent between the compressed tablet form taken with water to that of the chewable dispersible tablets, taken with or without water.L9404,L12183

Metabolisme

Lamotrigine is mainly glucuronidated, forming 2-N-glucuronide conjugate, a pharmacologically inactive metabolite.A192027 The total radioactivity detected after a 240mg radiolabeled dose of lamotrigine during clinical trials were as follows: lamotrigine as unchanged drug(10%), a 2-N-glucuronide (76%), a 5-N-glucuronide (10%), a 2-N-methyl metabolite (0.14%), as well as various other minor metabolites (4%).L9404

Rute Eliminasi

Lamotrigine is excreted in both the urine and feces.A192027 Following oral administration of 240 mg radiolabelled lamotrigine, about 94% of total drug and its metabolites administered is recovered in the urine and 2% is recovered in the feces.L9404 One pharmacokinetic study recovered 43 to 87% of a lamotrigine dose in the urine mainly as glucuronidated metabolites.A191946 2-N-glucuronide is mainly excreted in the urine.A192027

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1963 Data
Desmopressin The risk or severity of adverse effects can be increased when Lamotrigine is combined with Desmopressin.
Ceritinib Lamotrigine may increase the bradycardic activities of Ceritinib.
Ivabradine Lamotrigine may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Lamotrigine.
Buprenorphine Lamotrigine 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 Lamotrigine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Lamotrigine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Lamotrigine.
Hydrocodone Lamotrigine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Lamotrigine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Lamotrigine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Lamotrigine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Lamotrigine.
Mirtazapine Lamotrigine 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 Lamotrigine.
Orphenadrine Lamotrigine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Lamotrigine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Lamotrigine.
Pramipexole Lamotrigine may increase the sedative activities of Pramipexole.
Ropinirole Lamotrigine may increase the sedative activities of Ropinirole.
Rotigotine Lamotrigine may increase the sedative activities of Rotigotine.
Sodium oxybate Lamotrigine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Lamotrigine 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 Lamotrigine.
Thalidomide Lamotrigine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Lamotrigine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Dofetilide The serum concentration of Dofetilide can be increased when it is combined with Lamotrigine.
Aclidinium Lamotrigine may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Mirabegron The risk or severity of QTc prolongation can be increased when Lamotrigine is combined with Mirabegron.
Potassium chloride Potassium chloride may increase the hyperkalemic activities of Lamotrigine.
Tiotropium Lamotrigine may decrease the excretion rate of Tiotropium which could result in a higher serum level.
Topiramate The risk or severity of CNS depression can be increased when Topiramate is combined with Lamotrigine.
Umeclidinium The risk or severity of Tachycardia can be increased when Lamotrigine is combined with Umeclidinium.
Mefloquine The therapeutic efficacy of Lamotrigine can be decreased when used in combination with Mefloquine.
Mianserin The therapeutic efficacy of Lamotrigine can be decreased when used in combination with Mianserin.
Orlistat Orlistat can cause a decrease in the absorption of Lamotrigine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Butalbital The serum concentration of Lamotrigine can be decreased when it is combined with Butalbital.
Pentobarbital The serum concentration of Lamotrigine can be decreased when it is combined with Pentobarbital.
Secobarbital The serum concentration of Lamotrigine can be decreased when it is combined with Secobarbital.
Methohexital The serum concentration of Lamotrigine can be decreased when it is combined with Methohexital.
Thiopental The serum concentration of Lamotrigine can be decreased when it is combined with Thiopental.
Thiamylal The serum concentration of Lamotrigine can be decreased when it is combined with Thiamylal.
Amobarbital The serum concentration of Lamotrigine can be decreased when it is combined with Amobarbital.
Hexobarbital The serum concentration of Lamotrigine can be decreased when it is combined with Hexobarbital.
Barbital The serum concentration of Lamotrigine can be decreased when it is combined with Barbital.
Barbexaclone The serum concentration of Lamotrigine can be decreased when it is combined with Barbexaclone.
Butabarbital The serum concentration of Lamotrigine can be decreased when it is combined with Butabarbital.
Phenytoin The serum concentration of Lamotrigine can be decreased when it is combined with Phenytoin.
Fosphenytoin The serum concentration of Lamotrigine can be decreased when it is combined with Fosphenytoin.
Rufinamide The serum concentration of Lamotrigine can be increased when it is combined with Rufinamide.
Topotecan Lamotrigine may increase the excretion rate of Topotecan which could result in a lower serum level and potentially a reduction in efficacy.
Valproic acid Valproic acid may decrease the excretion rate of Lamotrigine which could result in a higher serum level.
Metformin The serum concentration of Metformin can be increased when it is combined with Lamotrigine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Lamotrigine.
Glycopyrronium The risk or severity of Tachycardia can be increased when Lamotrigine is combined with Glycopyrronium.
Deferasirox The metabolism of Deferasirox can be increased when combined with Lamotrigine.
Ritonavir The serum concentration of Lamotrigine can be decreased when it is combined with Ritonavir.
Atazanavir The serum concentration of Lamotrigine can be decreased when it is combined with Atazanavir.
Ezogabine The serum concentration of Lamotrigine can be decreased when it is combined with Ezogabine.
Primidone Primidone may increase the excretion rate of Lamotrigine which could result in a lower serum level and potentially a reduction in efficacy.
Methylphenobarbital Methylphenobarbital may increase the excretion rate of Lamotrigine which could result in a lower serum level and potentially a reduction in efficacy.
Phenobarbital Phenobarbital may increase the excretion rate of Lamotrigine which could result in a lower serum level and potentially a reduction in efficacy.
Nelfinavir The metabolism of Lamotrigine can be increased when combined with Nelfinavir.
Zidovudine The metabolism of Lamotrigine can be increased when combined with Zidovudine.
Troglitazone The metabolism of Troglitazone can be increased when combined with Lamotrigine.
Acetaminophen The metabolism of Acetaminophen can be increased when combined with Lamotrigine.
Indomethacin The metabolism of Indomethacin can be increased when combined with Lamotrigine.
Minoxidil The metabolism of Minoxidil can be increased when combined with Lamotrigine.
Cerivastatin The metabolism of Cerivastatin can be increased when combined with Lamotrigine.
Raloxifene The metabolism of Raloxifene can be increased when combined with Lamotrigine.
Diclofenac The metabolism of Diclofenac can be increased when combined with Lamotrigine.
Simvastatin The metabolism of Simvastatin can be increased when combined with Lamotrigine.
Mycophenolate mofetil The metabolism of Mycophenolate mofetil can be increased when combined with Lamotrigine.
Furosemide The metabolism of Furosemide can be increased when combined with Lamotrigine.
Flurbiprofen The metabolism of Flurbiprofen can be increased when combined with Lamotrigine.
Naproxen The metabolism of Naproxen can be increased when combined with Lamotrigine.
Propofol The metabolism of Propofol can be increased when combined with Lamotrigine.
Tiagabine The metabolism of Tiagabine can be increased when combined with Lamotrigine.
Metronidazole The metabolism of Metronidazole can be increased when combined with Lamotrigine.
Fulvestrant The metabolism of Fulvestrant can be increased when combined with Lamotrigine.
Ezetimibe The metabolism of Ezetimibe can be increased when combined with Lamotrigine.
Ketoprofen The metabolism of Ketoprofen can be increased when combined with Lamotrigine.
Abacavir The metabolism of Abacavir can be increased when combined with Lamotrigine.
Ibuprofen The metabolism of Ibuprofen can be increased when combined with Lamotrigine.
Glipizide The metabolism of Glipizide can be increased when combined with Lamotrigine.
Atorvastatin The metabolism of Atorvastatin can be increased when combined with Lamotrigine.
Fluvastatin The metabolism of Fluvastatin can be increased when combined with Lamotrigine.
Naloxone The metabolism of Naloxone can be increased when combined with Lamotrigine.
Gemfibrozil The metabolism of Gemfibrozil can be increased when combined with Lamotrigine.
Fusidic acid The metabolism of Fusidic acid can be increased when combined with Lamotrigine.
Alvocidib The metabolism of Alvocidib can be increased when combined with Lamotrigine.
Migalastat Lamotrigine may decrease the excretion rate of Migalastat which could result in a higher serum level.
Indacaterol The metabolism of Indacaterol can be increased when combined with Lamotrigine.
Eltrombopag The metabolism of Eltrombopag can be increased when combined with Lamotrigine.
Bazedoxifene The metabolism of Bazedoxifene can be increased when combined with Lamotrigine.
Muraglitazar The metabolism of Muraglitazar can be increased when combined with Lamotrigine.
Gavestinel The metabolism of Gavestinel can be increased when combined with Lamotrigine.
Raltegravir The metabolism of Raltegravir can be increased when combined with Lamotrigine.
Dolutegravir The metabolism of Dolutegravir can be increased when combined with Lamotrigine.
Elvitegravir The metabolism of Elvitegravir can be increased when combined with Lamotrigine.

Target Protein

Voltage-dependent R-type calcium channel subunit alpha-1E CACNA1E
Sodium channel protein type 11 subunit alpha SCN11A
Voltage-gated sodium channel alpha subunit SCN1A
Adenosine receptor A1 ADORA1
Adenosine receptor A2a ADORA2A
Alpha-1A adrenergic receptor ADRA1A
Alpha-2A adrenergic receptor ADRA2A
Beta-1 adrenergic receptor ADRB1
D(1) dopamine receptor DRD1
D(2) dopamine receptor DRD2
GABA(A) Receptor GABRA1
GABA(A) Receptor Benzodiazepine Binding Site GABRA1
Histamine H1 receptor HRH1
Kappa-type opioid receptor OPRK1
Acetylcholine receptor subunit alpha CHRNA1
5-hydroxytryptamine receptor 2A HTR2A
5-hydroxytryptamine receptor 3A HTR3A
Glutamate receptor 1 GRIA1

Referensi & Sumber

Synthesis reference: Grahame Roy Lee, "Process for the preparation of lamotrigine." U.S. Patent US5925755, issued January, 1981.
Artikel (PubMed)
  • PMID: 15115640
    Backonja M: Neuromodulating drugs for the symptomatic treatment of neuropathic pain. Curr Pain Headache Rep. 2004 Jun;8(3):212-6.
  • PMID: 12716240
    Barbosa L, Berk M, Vorster M: A double-blind, randomized, placebo-controlled trial of augmentation with lamotrigine or placebo in patients concomitantly treated with fluoxetine for resistant major depressive episodes. J Clin Psychiatry. 2003 Apr;64(4):403-7.
  • PMID: 11888243
    Jensen TS: Anticonvulsants in neuropathic pain: rationale and clinical evidence. Eur J Pain. 2002;6 Suppl A:61-8.
  • PMID: 14667954
    Pappagallo M: Newer antiepileptic drugs: possible uses in the treatment of neuropathic pain and migraine. Clin Ther. 2003 Oct;25(10):2506-38.
  • PMID: 19579915
    Tehrani SP, Daryaafzoon M, Bakhtiarian A, Ejtemaeemehr S, Sahraei H: The effects of lamotrigine on the acquisition and expression of morphine-induced place preference in mice. Pak J Biol Sci. 2009 Jan 1;12(1):33-9.
  • PMID: 29176325
    Dibue-Adjei M, Kamp MA, Alpdogan S, Tevoufouet EE, Neiss WF, Hescheler J, Schneider T: Cav2.3 (R-Type) Calcium Channels are Critical for Mediating Anticonvulsive and Neuroprotective Properties of Lamotrigine In Vivo. Cell Physiol Biochem. 2017;44(3):935-947. doi: 10.1159/000485361. Epub 2017 Nov 24.
  • PMID: 7691504
    Goa KL, Ross SR, Chrisp P: Lamotrigine. A review of its pharmacological properties and clinical efficacy in epilepsy. Drugs. 1993 Jul;46(1):152-76. doi: 10.2165/00003495-199346010-00009.
  • PMID: 9429124
    Garnett WR: Lamotrigine: pharmacokinetics. J Child Neurol. 1997 Nov;12 Suppl 1:S10-5. doi: 10.1177/0883073897012001041.
Menampilkan 8 dari 12 artikel.
Textbook
  • ISBN: 978-0-7020-3471-8
    44. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 544, 549). Edinburgh: Elsevier/Churchill Livingstone.

Contoh Produk & Brand

Produk: 637 • International brands: 28
Produk
  • Ag-lamotrigine
    Tablet • 25 mg • Oral • Canada • Generic • Approved
  • Ag-lamotrigine
    Tablet • 100 mg • Oral • Canada • Generic • Approved
  • Ag-lamotrigine
    Tablet • 150 mg • Oral • Canada • Generic • Approved
  • Apo-lamotrigine
    Tablet • 25 mg • Oral • Canada • Generic • Approved
  • Apo-lamotrigine
    Tablet • 150 mg • Oral • Canada • Generic • Approved
  • Apo-lamotrigine
    Tablet • 100 mg • Oral • Canada • Generic • Approved
  • Auro-lamotrigine
    Tablet • 25 mg • Oral • Canada • Generic • Approved
  • Auro-lamotrigine
    Tablet • 100 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 637 produk.
International Brands
  • Convulsan — Actavis
  • Crisomet — Juste
  • Dafex — Phoenix
  • Daksol — Pharmavita
  • Danoptin — Pliva
  • Dezepil — Rafarm
  • Elmendos — GlaxoSmithKline
  • Epilepax — Ivax
  • Epimil — Ivax
  • Epiral — Zentiva

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