Active Pharmaceutical Ingredients

Catalog ID80019628

CAS NO.84057-84-1

Purity 98%

MDL NumberMFCD00865333

EINEC281-901-8

Molecular FormulaC9H7Cl2N5

Molecular Weight256.0914

Melting point: 217~222°C

Category	Information
Chemical Properties	– Molecular Formula: C₁₄H₁₂F₃N₃O₂<br>- Molecular Weight: 331.26 g/mol
Mechanism of Action	– Sodium Channel Blockade: Lamotrigine preferentially binds to the fast-inactivated state of voltage-dependent sodium channels, reducing neuronal excitability and decreasing seizure activity.<br>- Calcium Channel Blockade: It reduces calcium currents through N- and L-type calcium channels.<br>- Glutamate Release Inhibition: Lamotrigine inhibits the release of excitatory neurotransmitters like glutamate, contributing to its antiseizure effects.<br>- GABA Modulation: It increases the activity of the inhibitory neurotransmitter GABA, further reducing neuronal excitability.<br>- HCN Channel Modulation: Lamotrigine modulates HCN channels, which are involved in regulating neuronal excitability and pacemaker currents.<br>- Antioxidant Properties: It has antioxidant properties that contribute to its neuroprotective effects.<br>- Anti-inflammatory Effects: Lamotrigine reduces the activation of microglia, the immune cells of the central nervous system, potentially reducing neuroinflammation.
Clinical Uses	– Epilepsy: Effective in treating various types of epilepsy, including partial seizures and generalized seizures.<br>- Bipolar Disorder: Used as a mood stabilizer to prevent manic and depressive episodes.<br>- Neuropathic Pain: Investigated for its potential use in managing neuropathic pain.
Pharmacokinetics	– Absorption: Rapidly and completely absorbed after oral administration with negligible first-pass metabolism.<br>- Bioavailability: Absolute bioavailability is 98%.<br>- Distribution: Volume of distribution ranges from 0.9 to 1.3 L/kg.<br>- Metabolism: Primarily metabolized by glucuronidation in the liver.<br>- Excretion: Excreted by the kidneys.<br>- Half-Life: 15-30 hours.
Adverse Effects	– Common side effects include rash, nausea, dizziness, and headache.<br>- Rare but serious side effects include Stevens-Johnson syndrome and toxic epidermal necrolysis.<br>- Other potential side effects include ataxia, diplopia, tremor, gastrointestinal discomfort, and psychiatric symptoms.
Storage Conditions	Store in a cool, dry place, protected from moisture.
Special Notes	– Drug Interactions: Lamotrigine levels can be affected by other medications, including enzyme-inducing drugs like rifampicin and oral contraceptives.<br>- Gradual Dose Titration: To reduce the risk of rash, gradual dose titration is recommended.<br>- Monitoring: Plasma concentration monitoring is important for achieving therapeutic effects and avoiding adverse reactions.

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