Lamotrigine | |
Lamotrigine | |
Lamotrigine | |
Chemical compound | |
IUPAC | 6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine |
Gross formula | C₉H₇Cl₂N₅ |
Molar mass | 256 g/mol |
CAS | 84057-84-1 |
PubChem | 3878 |
DrugBank | 00555 |
Classification | |
Pharmacol. group | Normotimik, Anticonvulsant (antiepileptic drug) |
ATX | N03AX09 |
Pharmacokinetics | |
Bioavailable | 98% |
Plasma protein binding | 55% |
Metabolism | liver (enzyme UGT1A4) |
Half-life | 24-34 hours (in adults) |
Excretion | kidneys |
Dosage forms | |
tablets and chewable tablets of 25, 50 and 100 mg | |
Method of administration | |
inside | |
Other names | |
Konvulsan, Lamictal, Lamitor, Lamolep, Lamotrin, Seizar | |
Lamotrigine on Wikimedia Commons |
Lamotrigine
is an antiepileptic drug used in the treatment of epilepsy and bipolar disorders; also has normothimic activity.
Pharmacodynamics and pharmacokinetics
Glutamic acid is a kind of catalyst for epileptic seizures .
The drug has the ability to influence presynaptic sodium channels in neuronal membranes, inhibiting the release of glutamic acid . Additionally, lamotrigine inhibits the depolarization caused by glutamate .
The medicine is almost completely absorbed from the gastrointestinal tract and enters the bloodstream. Already 2 and a half hours after administration, the active substance reaches its maximum concentration.
About half of the substance binds to blood . The drug undergoes a metabolic in the liver. The half-life ranges from 24 to 35 hours. In children this figure is slightly lower.
Eating does not affect the effectiveness of the product, but can slow down the absorption process.
The drug is excreted through the kidneys, in the form of metabolites , about 10% - in the form of lamotrigine , and a small part - with feces.
About the manufacturers
Lamotrigine was first introduced to the pharmaceutical market by the British company GlaxoSmithKline (GSK) under the brand name Lamictal. Today, this drug is produced in the USA, Europe (UK, Germany, Italy, Canada), India, Israel, Egypt and other countries of the world in the form of generics bearing the same name Lamotrigine or distinctive trade names.
In Germany, the medicine is produced by two well-known pharmaceutical companies:
- 1A Pharma GmbH - engaged in the production of antipsychotics, cardiological, hormonal drugs, analgesics and drugs from some other pharmacological groups;
- Desitin Arzneimittel GmbH - mainly specializes in drugs for the central nervous system.
Side effects
The medicine may cause:
- skin rashes, facial swelling , fever ;
- headaches , dizziness , sleep problems, aggressiveness , decreased performance;
- nausea, tremor , confusion , vomiting , diplopia ;
- vision problems, distorted sense of balance, conjunctivitis ;
- lymphadenopathy , anemia , increased levels enzymes , jaundice ;
- Stevens-Johnson syndrome , Lyell's syndrome .
Customer Reviews
Patients praise Lamotrigine for its high effectiveness and minimal side effects. Among the disadvantages, the high cost of the drug is noted.
Natalya Ivanova, 23 years old : “I tried many medications to treat epilepsy. Several years ago, a doctor suggested switching to Lamotrigine. The first week I had severe headaches and nightmares. Then the symptoms began to subside and by the third week everything returned to normal. I've been taking these pills for three years now. There are no attacks, side effects also no longer bother me. I order medicine online from intermediaries. “I liked the German drug Lamotrigine 100 the most.”
Instructions for use of Lamotrigine (Method and dosage)
The amount of the drug per day is determined by the doctor depending on the disease and its severity, combination with other drugs.
As a rule, 25 to 50 mg of the drug are prescribed at a time. The daily dosage can be about 100-200 mg.
Maximum – 700 mg.
In case of taking the medicine by children from 2 to 12 years old, the maximum amount of the drug per day is 400 mg. The amount of medication per day is calculated: 1-2 mg per kg of weight.
The duration of therapy and treatment regimen are prescribed by the doctor.
Notes
- Gusev E.I., Gurd G.S.
Lamictal in the treatment of patients with epilepsy // Epilepsy. - M.: All-Russian Society of Neurologists, 1994. - Nassir Ghaemi S., Shirzadi A.A., Filkowski M.
Publication bias and the pharmaceutical industry: the case of lamotrigine in bipolar disorder. (English) // Medscape journal of medicine. - 2008. - Vol. 10, no. 9. - P. 211. - PMID 19008973. [correct] - Medford N. (2005). "Understanding and treating depersonalization disorder." Advances in Psychiatric Treatment 11
(2): 92–100. DOI:10.1192/apt.11.2.92. - Sierra M., Baker D., Medford N., Lawrence E., Patel M., Phillips ML et al. (2006). "Lamotrigine as an add-on treatment for depersonalization disorder: a retrospective study of 32 cases." Clin Neuropharmacol 29
(5):253–8. DOI:10.1097/01.WNF.0000228368.17970.DA. PMID 16960469. - Erfurth A., Walden J., Grunze H. (1998). "Lamotrigine in the treatment of schizoaffective disorder." Neuropsychobiology 38
(3): 204–5. DOI:10.1159/000026540. PMID 9778612. - Lieb K., Völlm B., Rücker G., Timmer A., Stoffers J. M. (2009). "Pharmacotherapy for borderline personality disorder: Cochrane systematic review of randomized trials." The British Journal of Psychiatry 196
(1): 4–12. DOI:10.1192/bjp.bp.108.062984. PMID 20044651. - Hermle L., Simon M., Ruchsow M., Geppert M. (2012). "Hallucinogen-persisting perception disorder." Therapeutic Advances in Psychopharmacology 2
(5):199–205. DOI:10.1177/2045125312451270. PMID 23983976. - Hussain A., Dar MA, Wani RA, Shah MS, Jan MM, Malik YA et al. (2015). "Role of lamotrigine augmentation in treatment-resistant obsessive compulsive disorder: a retrospective case review from South Asia." Indian J Psychol Med 37
(2):154–8. DOI:10.4103/0253-7176.155613. PMID 25969599. - Backonja M. (2004). "Neuromodulating drugs for the symptomatic treatment of neuropathic pain." Curr Pain Headache Rep 8
(3):212–6. DOI:10.1007/s11916-004-0054-4. PMID 15115640. - Jensen T. S. (2002). "Anticonvulsants in neuropathic pain: Rationale and clinical evidence." European Journal of Pain 6
: 61–68. DOI:10.1053/eujp.2001.0324. PMID 11888243. - Pappagallo M. (October 2003). "Newer antiepileptic drugs: possible uses in the treatment of neuropathic pain and migraine." Clin Ther 25
(10):2506–38. DOI:10.1016/S0149-2918(03)80314-4. PMID 14667954. - Mashkovsky, 2005, p. 40.
Interaction
Combination with hormonal contraceptives (containing levonorgestrel and ethinyl estradiol to a decrease in the effectiveness of the drug and AUC .
Valproates block liver enzymes, slow down the metabolism of the drug, and the drug is excreted from the body almost twice as long.
Medicines that induce liver enzymes , on the contrary, have the ability to accelerate the metabolism of Lamotrigine up to two times. These drugs include: Phenytoin, Phenobarbital, Carbamazepine, Primidone, Paracetamol . Also, when these drugs were taken in combination, ataxia , nausea , dizziness , and diplopia .
The drug does not have the ability to displace other drugs for epilepsy blood plasma proteins .
When the drug is combined with Rifampicin, the clearance of is stimulated and elimination from the body is accelerated.
How to spot a fake
When purchasing Lamotrigine, you should ask the seller for documents confirming the authenticity of the goods (certificates, checks or other payment documents). You cannot buy such drugs in small pharmacy kiosks, tempted by the low price. Licensed medicines are expensive and are practically not sold in Russia. They can be found only in large pharmacy chains, or ordered from intermediaries via the Internet.
The most reliable sellers in this regard are those who work with European countries. They purchase medications from pharmacies and then deliver them to the buyer along with receipts confirming the authenticity of the goods.
special instructions
If the patient has kidney disease, drug therapy should be carried out with caution. The daily dosage should be reduced by at least half. For people suffering from liver disease, it is recommended to reduce the dosage by 70%.
Lamotrigine is not recommended for use in the elderly.
With an abrupt cessation of therapy, withdrawal syndrome and an increase in the frequency of attacks may develop, so withdrawal must be done slowly, over 14 days.
During treatment, it is not recommended to drive a car or perform any high-precision operations.
If, after taking the pills, the patient develops severe allergic reactions , including toxic epidermal necrolysis , it is better to stop taking the medication as soon as possible.
For persons undergoing hemodialysis , it is necessary to take into account that during a four-hour procedure, about 20% of the active substance is removed from the body.
Reviews from doctors
Sergey Tikhonov, neurologist : “I have been recommending Lamotrigine to my patients suffering from epilepsy for many years. This drug, unlike similar drugs, has a wider spectrum of action than Carbamazepine or Phenytoin. It is effective even for the treatment of severe epilepsy, which makes it a priority. The medicine is well tolerated by patients and is guaranteed to lengthen the period of remission. Among the various generics, it is best to choose medications manufactured in Europe or the USA.”
Analogues of Lamotrigine
Level 4 ATC code matches:
Gabagamma
Neurontin
Pagluferal
Algerica
Topiramate
Convalis
Lamictal
Gabapentin
Topamax
Keppra
Pregabalin Richter
Tebantin
The following analogues of Lamotrigine exist: Algerica, Carbamazepine, Vimpat, Lyrica, Neuralgin, Gabagamma (various dosages), Gabantin, levetiracetam, Grimodin, Levicitam, Meditan, Neogabine, Topilex, Tebantin, Topilepsin, Epiramat, Topamax, Keppra, Gabapentin.
Impact on women
During clinical trials of the drug, it was noticed that side effects developed more often in women than in male volunteers. This was unusual, since other medications from the same pharmacological group do not have such a relationship.
While studying this phenomenon, scientists discovered that lamotrigine interacts with female sex hormones. When taken simultaneously with medications containing estrogen, the level of the active substance in the blood fell, and after discontinuation of AEDs, the side effects intensified.
In another study, experts found that drug interactions increased the production of luteinizing and follicle-stimulating hormones. Despite this, the ability of contraceptives to suppress ovulation was preserved.
Lamotrigine price, where to buy
At the moment it is difficult to indicate the price of Lamotrigine.
- Online pharmacies in RussiaRussia
ZdravCity
- Lamotrigine Canon tab.
25 mg No. 30 ZAO Kanonpharma Production 326 rub. order - Lamotrigine Canon tablets 100 mg 30 pcs. Canonpharma Production JSC
640 rub. order
Terms of sale in pharmacies
Lamotrigine is sold in pharmacies by prescription. But this medicine is difficult to find, especially in small Russian cities. Under no circumstances should you buy the drug at pharmacy kiosks, as you may receive counterfeit medicine. It is easier and safer to purchase high-quality medicine from intermediaries in Germany.
No prescription form is required when ordering online. The seller only needs to know the name of the drug, dosage and number of packages. All medications are purchased directly from German pharmacies, which is confirmed by the relevant payment documentation.