Lamotrigine

• 3,5-diamino- 6-( 2,3- dichlorophenyl) - 1,2,4 -triazine (IUPAC)
• Lamotriginum (Latin )

N03AX09

Anticonvulsant

Sodium and calcium channel blockers

216-218 ° C

Risk

205 mg · kg -1 ( LD50, rat, oral)

Template: Infobox chemical / molecular formula search available

Lamotrigine is a Certified since 1993 drug from the group of anti-epileptic drugs, which is approved for patients 12 years of age. In addition to the treatment of epilepsy it is also used in mood disorders. Was developed and erstvertrieben Lamotrigine by GlaxoSmithKline. Since June 2005, it is available as a generic.

Pharmacology

Pharmacodynamics ( mechanism of action )

Lamotrigine blocked sodium and voltage-dependent calcium channels of nerve cells, and prevents the release of the excitatory neurotransmitters glutamate and aspartate. Thus, stimuli can only be reduced from one nerve cell to another spread. The inhibition caused by lamotrigine neuronal α4β2 - nACh receptors - probably via blockade lumens - could contribute to the antiepileptic effect. In the depression model values ​​of BDNF and VEGF by lamotrigine are favorably influenced.

Areas of application

In the treatment of epilepsy, it leads at 40-60 % of patients to seizure freedom. However, experience shows that the effectiveness may be decreased in myoclonus.

In addition to the treatment of epilepsy, it is mainly used for the prophylaxis of recurrent depression and depressive states in bipolar disorder. In the treatment of mania, it shows, however, rather small effects. Lamotrigine affects mood stabilizing ( "mood - stabilizer" ) and thus takes its place among the mood stabilizers.

It was also a reduction in pain observed in a study of stroke patients in 30% of participants. Also highly effective in HIV-associated polyneuropathy is described. Although the efficacy of lamotrigine is to provide for neuropathic pain in question, the BfArM plans to recommend the off- label use of lamotrigine in neuropathic pain.

More recently, the means of neurologists is also used to treat migraines - but not against the headache, but in cases where the migraine aura ( neurological problems, paralysis, visual field defects due to the migraine) is in the foreground.

Although a published study showed a good effect of lamotrigine in the treatment of depersonalization and derealization symptoms, these could but not in another, randomized, placebo-controlled study to be confirmed. In clinical practice seems the positive effect in the treatment of depersonalization and derealization symptoms, especially in combination with serotonin reuptake inhibitors, however, to confirm.

Compatibility, known side effects

Lamotrigine is well tolerated in general. As a result of too rapid titration but it can cause dangerous skin and mucosal reactions ( rash, exfoliative dermatitis, Stevens- Johnson syndrome ) can occur.

In rare cases, as side effects double vision, dizziness, headache, nausea, disturbances in movement (ataxia ), muscle trembling ( tremor), Lyell 's syndrome ( scalded skin syndrome ), agranulocytosis, sleep or even described behavioral disorders.

In 3% of cases there may be a paradoxical seizure clustering come ( rebound seizures ).

Liver damage at the beginning of the treatment can not be excluded. Therefore should be monitored especially at the beginning of drug therapy liver function.

If after eight weeks of treatment, none of the side effects have occurred, may be assumed that the drug is well tolerated. Exceptions are switching from another medication, concomitant medications, and mildly symptomatic shortly after a titration.

Interactions

The pain reliever acetaminophen may increase lamotrigine breakdown in the body. An alternative is to provide pain medication containing the active ingredient ibuprofen.

Also, a malaria treatment or prophylaxis may lead to a reduction of the effectiveness of lamotrigine or the anti -malarial drug.

In a therapy with lamotrigine and other antiepileptic drugs may cause increased side effects. In a Carbamazepintherapie lamotrigine is degraded faster because carbamazepine is an enzyme inducer. It is therefore more substance taken werden.Ebenso it behaves with medicines containing the active ingredients phenytoin, phenobarbital, primidone and. In a Valproinsäuretherapie (inhibitor ) Lamotrigine is degraded more slowly. To avoid side effects, lamotrigine must be titrated more slowly in combination with valproic acid.

The Lamotriginkonzentration in plasma is disturbed by the intake of birth control pills. Taking the pill reduces lamotrigine levels by up to 50 %. It can be propagated seizures. Stopping the pill results in a level increase, so that the rate of side effects increases. Lamotrigine can be reversed may also interfere with the effectiveness of hormonal contraceptives, since levonorgestrel is degraded faster. Therefore, patients should be encouraged, through changes in their menstrual pattern, ie breakthrough bleeding, to report immediately. For other progestins are no data.

Trade names

Elmendos (D), Gerolamic (A), Lamictal (D, A, CH), Lamotribene (A ), numerous generics (D, A, CH)