Tìm theo
Lamotrigine
Các tên gọi khác (5 ) :
  • 3,5-Diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine
  • Lamictal
  • Lamotrigina
  • Lamotrigine
  • Lamotriginum
Thuốc điều trị về tâm thần
Thuốc Gốc
Small Molecule
CAS: 84057-84-1
ATC: N03AX09
ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com
CTHH: C9H7Cl2N5
PTK: 256.091
Lamotrigine is an anticonvulsant drug used in the treatment of epilepsy and bipolar disorder. For epilepsy it is used to treat partial seizures, primary and secondary tonic-clonic seizures, and seizures associated with Lennox-Gastaut syndrome. Lamotrigine also acts as a mood stabilizer. It is the first medication since lithium granted Food and Drug Administration (FDA) approval for the maintenance treatment of bipolar type I. Chemically unrelated to other anticonvulsants, lamotrigine has relatively few side-effects and does not require blood monitoring. The exact way lamotrigine works is unknown. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C9H7Cl2N5
Phân tử khối
256.091
Monoisotopic mass
255.007850663
InChI
InChI=1S/C9H7Cl2N5/c10-5-3-1-2-4(6(5)11)7-8(12)14-9(13)16-15-7/h1-3H,(H4,12,13,14,16)
InChI Key
InChIKey=PYZRQGJRPPTADH-UHFFFAOYSA-N
IUPAC Name
6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine
Traditional IUPAC Name
lamotrigine
SMILES
NC1=NC(N)=C(N=N1)C1=C(Cl)C(Cl)=CC=C1
Độ tan chảy
216-218 °C (uncorr)
Độ hòa tan
4.88e-01 g/l
logP
2.5
logS
-2.7
pKa (strongest acidic)
14.98
pKa (Strongest Basic)
5.87
PSA
90.71 Å2
Refractivity
66.62 m3·mol-1
Polarizability
23.1 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
5
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Lamotrigine, an antiepileptic drug (AED) of the phenyltriazine class, is chemically unrelated to existing antiepileptic drugs. Lamotrigine is also used in the treatment of depression and bipolar disorder. Lamotrigine is thought to exert its anticonvulsant effect by stabilizing presynaptic neuronal membranes. Lamotrigine inhibits sodium currents by selectively binding to the inactivated state of the sodium channel and subsequently suppresses the release of the excilatory amino acid, glutamate.
Cơ Chế Tác Dụng : Lamotrigine is an anticonvulsant drug used in the treatment of epilepsy and bipolar disorder. For epilepsy it is used to treat partial seizures, primary and secondary tonic-clonic seizures, and seizures associated with Lennox-Gastaut syndrome. Lamotrigine also acts as a mood stabilizer. It is the first medication since lithium granted Food and Drug Administration (FDA) approval for the maintenance treatment of bipolar type I. Chemically unrelated to other anticonvulsants, lamotrigine has relatively few side-effects and does not require blood monitoring. The exact way lamotrigine works is unknown. [Wikipedia] One proposed mechanism of action of Lamotrigine, the relevance of which remains to be established in humans, involves an effect on sodium channels. in vitro pharmacological studies suggest that lamotrigine inhibits voltage-sensitive sodium channels and/or calcium channels, thereby stabilizing neuronal membranes and consequently modulating presynaptic transmitter release of excitatory amino acids (e.g., glutamate and aspartate). Studies on lamotrigine show binding to sodium channels similar to local anesthetics.
Dược Động Học :
▧ Absorption :
98%
▧ Volume of Distribution :
* 0.9 to 1.3 L/kg
▧ Protein binding :
55%
▧ Metabolism :
Hepatic
▧ Half Life :
25 +/- 10 hours (healthy individuals); 42.9 hours (chronic renal failure)
▧ Clearance :
* Apparent plasma cl=0.44 mL/min/kg [healthy volunteers taking single-dose LAMICTAL] * Apparent plasma cl=0.58 mL/min/kg [healthy volunteers taking multiple-dose LAMICTAL] * Apparent plasma cl=0.30 mL/min/kg [healthy volunteers taking valproate and single-dose LAMICTAL] * Apparent plasma cl=0.18 mL/min/kg [healthy volunteers taking valproate and multiple-dose LAMICTAL] * Apparent plasma cl=1.1 mL/min/kg [Patients with epilepsy taking carbamazepine, phenytoin, phenobarbital, or primidone plus valproate and single-dose LAMICTAL] * Apparent plasma cl=1.12 mL/min/kg [Patients with epilepsy taking carbamazepine, phenytoin, phenobarbital, or primidone plus valproate and multiple-dose LAMICTAL]
Độc Tính : LD50=250 (mg/kg) (in rat, mice); LD50>640 orally (mg/kg) (in rat, mice) (Sawyer). Symptoms of overdose include decreased level of consciousness, coma, delayed heartbeat, increased seizures, lack of coordination, and rolling eyeballs.
Chỉ Định : For the adjunctive treatment of partial seizures in epilepsy and generalized seizures of Lennox-Gastaut syndrome. Also for the maintenance treatment of bipolar I disorder and depression.
Tương Tác Thuốc :
  • Butabarbital Barbiturates like butabarbital may decrease the serum concentration of lamotrigine. There are separate patient management guidelines for patients age 12 and under and for patients older than 12 years of age. Monitor for decreased serum concentrations/therapeutic effects of lamotrigine if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased.
  • Butalbital Barbiturates such as butalbital may decrease the serum concentration of lamotrigine. There are separate management guidelines for patients age 12 and under and for patients older than 12 years of age. Please refer to the current approved prescribing information for additional information. Monitor for decreased serum concentrations/therapeutic effects of lamotrigine if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased.
  • Carbamazepine Lamotrigine may increase the adverse effects of carbamazepine by increasing the concentration of its active metabolite, carbamazepine-epoxide. Carbamazepine may decrease the therapeutic effect of lamotrigine by increasing its metabolism. Lamotrigine doses should be adjusted accordingly. Monitor for changes in the therapeutic and adverse effects of both agents if concomitant therapy is initiated, discontinue or doses are changed.
  • Clozapine Lamotrigine increases the effect and toxicity of clozapine
  • Desogestrel The oral contraceptive decreases the effect of lamotrigine
  • Ethinyl Estradiol The oral contraceptive decreases the effect of lamotrigine
  • Ethotoin Phenytoin may reduce levels of lamotrigine
  • Ezogabine In healthy adults, the AUCs of lamotrigine and ezogabine were both increased. The clinical significance of this is still unknown. Multiple doses of ezogabine also increase the clearance and decrease the terminal half-life of lamotrigine.
  • Fosphenytoin Phenytoin may reduce levels of lamotrigine
  • Mephenytoin Phenytoin may reduce levels of lamotrigine
  • Mestranol The oral contraceptive decreases the effect of lamotrigine
  • Methsuximide Methsuximide decreases the effect of lamotrigine
  • Norethindrone The oral contraceptive decreases the effect of lamotrigine
  • Phenytoin Phenytoin may reduce levels of lamotrigine
  • Rifampicin Rifampin decreases levels of lamotrigine
  • Thiopental Thiopental may increase the metabolism and clearance of Lamotrigine. Monitor for decreased therapeutic effect of Lamotrigine if Thiopental is initiated.
  • Triprolidine The CNS depressants, Triprolidine and Lamotrigine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Valproic Acid Valproic acid may increase the adverse effects of Lamotrigine by increasing Lamotrigine serum concentration. The Lamotrigine dose should be reduced by 50% during concomitant therapy. Monitor for changes in Lamotrigine therapeutic and adverse effects if Valproic acid is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Actavis
    Sản phẩm biệt dược : Convulsan
  • Công ty : Juste
    Sản phẩm biệt dược : Crisomet
  • Công ty : Phoenix
    Sản phẩm biệt dược : Dafex
  • Công ty : Pharmavita
    Sản phẩm biệt dược : Daksol
  • Công ty : Pliva
    Sản phẩm biệt dược : Danoptin
  • Công ty : Rafarm
    Sản phẩm biệt dược : Dezepil
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Elmendos
  • Công ty : Ivax
    Sản phẩm biệt dược : Epilepax
  • Công ty : Ivax
    Sản phẩm biệt dược : Epimil
  • Công ty : Zentiva
    Sản phẩm biệt dược : Epiral
  • Công ty : Cipla Medpro
    Sản phẩm biệt dược : Epitec
  • Công ty : Actavis
    Sản phẩm biệt dược : Epitrigine
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Labileno
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Lambipol
  • Công ty : PharmaSwiss
    Sản phẩm biệt dược : Lamect
  • Công ty : Sandoz
    Sản phẩm biệt dược : Lameptil
  • Công ty : Sandoz
    Sản phẩm biệt dược : Lameptil S
  • Công ty : Vitalchem
    Sản phẩm biệt dược : Lametec
  • Công ty : Intas
    Sản phẩm biệt dược : Lamez
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Lamictal
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Lamictal CD
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Lamictal XR
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Lamictin
  • Công ty : Glenmark
    Sản phẩm biệt dược : Lamotrix
  • Công ty : Rowex
    Sản phẩm biệt dược : Larig
  • Công ty : Medochemie
    Sản phẩm biệt dược : Medotrigin
  • Công ty : Douglas
    Sản phẩm biệt dược : Mogine
  • Công ty : Psicofarma
    Sản phẩm biệt dược : Trimolep
  • Công ty : Ranbaxy
    Sản phẩm biệt dược : Trogine
  • Công ty : Dr Reddys
    Sản phẩm biệt dược : Xebarin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00555
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3878
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505408
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00354
ChemSpider
http://www.chemspider.com/Chemical-Structure.3741.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50031299
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0173-0633-02
PharmGKB
http://www.pharmgkb.org/drug/PA450164
Wikipedia
http://en.wikipedia.org/wiki/Lamotrigine
RxList
http://www.rxlist.com/cgi/generic/lamotrigine.htm
Drugs.com
http://www.drugs.com/cdi/lamotrigine.html
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