Is lamotrigine metabolized by CYP?
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Is lamotrigine metabolized by CYP?
In contrast, valproic acid (a CYP enzyme inhibitor) reduces metabolism of lamotrigine, increasing serum half-life to 60 h or more [102]. Severe renal failure also increases elimination half-life of lamotrigine.
What CYP enzyme metabolizes lamotrigine?
| Enzyme or transporter induction/inhibition* | |
|---|---|
| Lamotrigine | May induce its own metabolism by UGT-glucuronidation (minor) |
| Levetiracetam | None |
| Oxcarbazepine | Induces CYP3A4 (weak) and UGT-glucuronidation but does not induce its own metabolism |
| Perampanel | Appears to induce metabolism of progestin-containing hormonal contraceptives |
What drug inhibits metabolism of lamotrigine?
Valproate is a strong inhibitor of lamotrigine metabolism and may cause an increase in lamotrigine concentrations by 200% (5-9).
How is lamotrigine metabolized?
Lamotrigine is inactivated by glucuronidation in the liver. Lamotrigine is metabolized predominantly by glucuronic acid conjugation. Its major metabolite is an inactive 2-n-glucuronide conjugate.
Is lamotrigine a CYP3A4 inhibitor?
Lamotrigine appears to be a weak inducer of UGTs, whereas induction of CYP3A4 seems improbable as the compound does not change the concentrations of oral contraceptives or the urinary excretion of 6beta-hydroxycortisol.
What gene metabolizes lamotrigine?
Lamotrigine disposition is mediated by UDP‐glucuronosyltransferases, mainly by UGT1A4 and UGT2B7. ABCB1 and SLC22A1 transporters appear to be also involved. Polymorphisms in UGT1A4, UGT2B7, ABCB1 and SLC22A1 genes affect protein activity and expression.
What drugs should not be taken with lamotrigine?
The following medications may decrease the level and effect of lamotrigine:
- Anticonvulsants such as phenytoin (Dilantin®), carbamazepine (Tegretol®/Carbatrol®/Equetro®), phenobarbital, and primidone (Mysoline®)
- Oral contraceptives (birth control pills)
- Rifampin (Rifadin®), ritonavir (Norvir®)
What are the pharmacokinetics of lamotrigine?
Lamotrigine exhibits first-order linear pharmacokinetics. Lamotrigine is well absorbed with bioavailability approaching 100%. The absorption is unaffected by food and there is no first-pass metabolism. The volume of distribution is between 1.25 and 1.47 L/kg and protein binding is about 55%.
Is lamotrigine and enzyme inducer?
Lamotrigine (Lamictal) is a non-enzyme-inducing AED. But unlike other non-enzyme-inducing AEDs, it needs special consideration. There is no evidence that the Pill affects epilepsy directly, but there is evidence that the Pill lowers lamotrigine levels in the blood.
What medications are CYP3A4 inducers?
Inducers of CYP3A4 include phenobarbital, phenytoin, rifampicin, St. John’s Wort and glucocorticoids.
Is Lamotrigine a CYP3A4 inhibitor?
What drugs are inducers of CYP450?
Exampled of drugs that commonly interact with CYP450 enzyme inhibitors and inducers are; Warfarin the Combined Contraceptive Pill, Theophylline, Corticosteroids, Tricyclics, Pethidine, and Statins.
What drugs are metabolized by UGT1A4?
The UGT1A4 enzyme mediates the metabolism of important psychotropic medications, including some tricyclic antidepressants, antipsychotics, and mood stabilizers1–20. Therefore, genetic polymorphisms in this gene may have pharmacological importance.
What does Lamictal interact with?
The following medications may decrease the level and effect of lamotrigine: Anticonvulsants such as phenytoin (Dilantin®), carbamazepine (Tegretol®/Carbatrol®/Equetro®), phenobarbital, and primidone (Mysoline®) Oral contraceptives (birth control pills) Rifampin (Rifadin®), ritonavir (Norvir®)
Can lamotrigine cause heart problems?
FDA Warns of Cardiac Risk With Lamotrigine (Lamictal) and Other Sodium Channel Blockers. Key takeaways: In October 2020, the FDA issued a new warning for the seizure and mental health medication lamotrigine (Lamictal), stating it could raise the risk of heart rhythm problems in people with heart disease.
Is lamotrigine an enzyme inducer?
Non-enzyme inducing antiepileptic drugs include: Ethosuximide. Gabapentin. Lacosamide. Lamotrigine.
