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Lamotrigine
Systematic (IUPAC) name
6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine
Identifiers
CAS number 84057-84-1
ATC code N03AX09
PubChem 3878
DrugBank APRD00570
Chemical data
Formula C9H7Cl2N5 
Mol. mass 256. IUPAC Nomenclature is a system of naming Chemical compounds and of describing the science of Chemistry in general CAS registry numbers are unique numerical identifiers for Chemical compounds Polymers biological sequences mixtures and Alloys They are also referred to The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs It is controlled by the WHO Collaborating Centre for Drug A section of the Anatomical Therapeutic Chemical Classification System. PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component The DrugBank database available at the University of Alberta is a unique Bioinformatics and Cheminformatics resource that combines detailed drug (i A chemical formula is a way of expressing information about the Atoms that constitute a particular Chemical compound, and how the relationship between those atoms changes Carbon (kɑɹbən is a Chemical element with the symbol C and its Atomic number is 6 Hydrogen (ˈhaɪdrədʒən is the Chemical element with Atomic number 1 Chlorine (ˈklɔriːn from the Greek word 'χλωρóς' ( khlôros, meaning 'pale green' is the Chemical element with Atomic number 17 and Nitrogen (ˈnaɪtɹəʤɪn is a Chemical element that has the symbol N and Atomic number 7 and Atomic weight 14 The molecular mass (abbreviated m of a substance, more commonly referred to as molecular weight and abbreviated as MW, is the Mass of one 091 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 98%
Protein binding 55%
Metabolism Hepatic
Half life 24-34 hours (healthy adults)
Excretion Renal
Therapeutic considerations
Pregnancy cat.

C (USA)
Legal status

N/A(USA); POM (UK)
Routes Oral

Lamotrigine (marketed as Lamictal (IPA: /ləˈmɪktəl/) by GlaxoSmithKline, called Lamictin in South Africa, למוג'ין (Lamogine)[1] in Israel, and 라믹탈 in South Korea) is an anticonvulsant drug used in the treatment of epilepsy and bipolar disorder. In Pharmacology, bioavailability is used to describe the fraction of an administered Dose of unchanged drug that reaches the Systemic circulation, one of A drug's efficiency may be affected by the degree to which it binds to the proteins within Blood plasma. Drug metabolism is the Metabolism of drugs, their Biochemical modification or degradation usually through specialized enzymatic systems The biological half-life of a substance is the time it takes for a substance (drug radioactive nuclide or other to lose half of its pharmacologic physiologic or radiologic activity Excretion is the process of eliminating waste products of Metabolism and other non-useful materials The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical if it is used as directed by the mother during The United States of America —commonly referred to as the The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction The United States of America —commonly referred to as the The United Kingdom of Great Britain and Northern Ireland, commonly known as the United Kingdom, the UK or Britain,is a Sovereign state located In Pharmacology and Toxicology, a route GlaxoSmithKline plc () is a United Kingdom -based pharmaceutical, biological and Healthcare Company. The Republic of South Africa (also known by other official names) is a country located at the southern tip of the continent of Africa For a topic outline on this subject see List of basic Israel topics. South Korea, officially the Republic of Korea and often referred to as Korea ( Korean: 대한민국 tɛː The anticonvulsants, also called antiepileptic drugs (abbreviated "AEDs" are a diverse group of pharmaceuticals used in the treatment of epileptic Epilepsy is a common chronic Neurological disorder that is characterized by recurrent unprovoked seizures. For epilepsy it is used to treat partial seizures, primary and secondary tonic-clonic seizures, and seizures associated with Lennox-Gastaut syndrome. Focal seizures (also called partial seizures) are Seizures which affect only a small part of the brain and are split into two main categories Simple partial Tonic-clonic seizures are a type of Generalized seizure affecting the entire brain Lennox-Gastaut syndrome (LGS also known as Lennox syndrome, is a difficult-to-treat form of childhood-onset Epilepsy that most often appears between the second and Lamotrigine also acts as a mood stabilizer. This article refers to the medication For other uses see Stabilizer. It is the first medication since lithium to be granted approval by the U. Lithium in pharmacology refers to use of the Lithium Ion, Li+ as a drug S. Food and Drug Administration (FDA) 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 in monotherapy. The exact way lamotrigine works is unknown. Some think that it is a Na+ (sodium) channel blocker. Sodium channels are Integral membrane proteins that form Ion channels, conducting sodium ions ( Na+) through a cell's Plasma membrane It is inactivated by hepatic glucuronidation. The liver is a vital organ in the human body and is present in Vertebrates and some other animals Glucuronic acid (from Greek γλυκερός - "sweet" is a Carboxylic acid.

Lamotrigine has a wide range of clincal uses. It has been found to be useful to treat neuropathy and also is known to be effective in treating unipolar depression, therefore patients with only these symptoms can derive an optimum benefit from lamotrigine when suffering from only these two symptoms. Neuropathy is a medical term usually short for Peripheral neuropathy. Atypical Depression (AD is a subtype of Dysthymia and Major Depression characterized by mood reactivity — being able to experience improved mood in response to positive events

However, lamotrigine has also been successful in controlling rapid cycling and mixed bipolar states in persons with more serious psychiatric disorders and who have not received what is considered to be adequate relief from lithium, carbamazepine or valproate, because it is deemed to possibly have significantly more antidepressant potency than either carbamazepine or valproate. Carbamazepine ("CBZ" is an Anticonvulsant and mood stabilizing drug used primarily in the treatment of Epilepsy and Bipolar disorder Valproic acid ( VPA) is a Chemical compound that has found clinical use as an Anticonvulsant and mood-stabilizing drug, primarily in

Lamotrigine has recently been reported to be a useful treatment for some people with post-traumatic stress disorder (PTSD) and borderline personality disorder (BPD). Post traumatic stress disorder It is a severe and ongoing emotional reaction to Borderline personality disorder ( BPD) is a psychiatric diagnosis in the Diagnostic and Statistical Manual of Mental Disorders ( DSM-IV Personality A recent study reported beneficial effects on individuals with schizoaffective disorder, bipolar subtype with depression. Schizoaffective disorder is a Psychiatric Diagnosis of neurobiological illness. [2]

Contents

U. S. Food and Drug Administration approval history

Indications and usage

Therapeutic dose is 100-200 mg.

Lamotrigine was approved by the US FDA in 1994, for the treatment of bipolar I disorder and for the treatment of epilepsy. [3] For maintenance treatment of bipolar I disorder, Lamotrigine (Lamictal) is the first FDA-approved therapy since lithium. Lithium (ˈlɪθiəm is a Chemical element with the symbol Li and Atomic number 3 [4]

While traditional anticonvulsant drugs are primarily antimanics, lamotrigine is most effective in the treatment and prophylaxis of bipolar depression. The anticonvulsants, also called antiepileptic drugs (abbreviated "AEDs" are a diverse group of pharmaceuticals used in the treatment of epileptic Prophylaxis ( Greek "προφυλάσσω" to guard or prevent beforehand) is any medical or Public health procedure whose purpose Lamotrigine treats bipolar depression without triggering mania, hypomania, mixed states, or rapid-cycling, and the 2002 American Psychiatric Association guidelines recommended lamotrigine as a first-line treatment for acute depression in bipolar disorder as well as a maintenance therapy. Mania (from Greek μανία and that from μαίνομαι - mainomai, "to rage to be furious" is a severe medical condition This article is an expansion of a section entitled '''Hypomania''' from within the main article Bipolar disorder. This article is an expansion of a section entitled '''Mixed state''' from the main article Bipolar disorder In the context of Mental

However, lamotrigine is not indicated on label for the treatment of acute bipolar symptoms. Because the dosage must be slowly increased from a sub-therapeutic level to the therapeutic level, the drug's utility in the management of acute manic symptoms is debatable; typically benzodiazepines or another anticonvulsant will be used to manage the acute mania until the lamotrigine reaches therapeutic blood concentration. The benzodiazepines (pronounced, often abbreviated to "benzos") are a class of Psychoactive drugs with varying Hypnotic

At doses considered sub-therapeutic, lamotrigine is thought to have a mild anti-depressant effect, leading some to question its safety for use in bipolar disorder. If lamotrigine's mechanism of action involves an increase in serotonin levels, this may potentially increase the risk of Serotonin syndrome. Serotonin syndrome is a potentially life-threatening adverse drug reaction that may occur following therapeutic drug use inadvertent interactions between drugs or the recreational

In addition to treating bipolar Lamotrigine is one of a small number of FDA-approved therapies for seizures associated with Lennox-Gastaut syndrome, a severe form of epilepsy. Lennox-Gastaut syndrome (LGS also known as Lennox syndrome, is a difficult-to-treat form of childhood-onset Epilepsy that most often appears between the second and Epilepsy is a common chronic Neurological disorder that is characterized by recurrent unprovoked seizures. Typically developing before four years of age, LGS is associated with developmental delays. There is no cure, treatment is often complicated, and complete recovery is rare. Symptoms include the atonic seizure (also known as a "drop attack"), during which brief loss of muscle tone and consciousness cause abrupt falls. Atonic seizures (also called drop seizures, drop attacks, or akinetic seizures) are a minor type of Seizure. Lamotrigine significantly reduces the frequency of LGS seizures, and is one of two medications known to decrease the severity of drop attacks. [5] Combination with valproate is common, but this increases the risk of lamotrigine-induced rash, and necessitates reduced dosing due to the interaction of these drugs. Valproic acid ( VPA) is a Chemical compound that has found clinical use as an Anticonvulsant and mood-stabilizing drug, primarily in [6]

Off-label uses include the treatment of peripheral neuropathy, trigeminal neuralgia, cluster headaches, migraines, and reducing neuropathic pain [7]. Off-label use is the practice of prescribing drugs for a purpose outside the scope of the drug's approved label most often concerning the drug's indication. Peripheral neuropathy is the term for damage to Nerves of the Peripheral nervous system, which may be caused either by diseases of the Nerve or from the Trigeminal neuralgia (TN, or Tic Doloureux, (also known as prosopalgia is a neuropathic disorder of the Trigeminal nerve that causes episodes of intense Cluster headache is a neurological disease that involves as its most prominent feature an immense degree of pain Migraine is a neurological Syndrome characterized by altered bodily experiences painful headaches and nausea Neuropathy is a medical term usually short for Peripheral neuropathy. Off-label psychiatric usage includes the treatment of bipolar II disorders, schizoaffective disorder, borderline personality disorder, post traumatic stress disorder, and as adjunctive therapy for "treatment-resistant" unipolar depression. Schizoaffective disorder is a Psychiatric Diagnosis of neurobiological illness. Borderline personality disorder ( BPD) is a psychiatric diagnosis in the Diagnostic and Statistical Manual of Mental Disorders ( DSM-IV Personality Major depressive disorder, also known as major depression, unipolar depression, unipolar disorder, clinical depression, or simply depression [8]

Mechanism of action

One proposed mechanism of action for lamotrigine involves an effect on sodium channels, although this remains to be established in humans. In vitro pharmacological studies suggest that lamotrigine inhibits voltage-sensitive sodium channels, thereby stabilizing neuronal membranes and consequently modulating presynaptic transmitter release of excitatory amino acids (for example glutamate and aspartate). Sodium channels are Integral membrane proteins that form Ion channels, conducting sodium ions ( Na+) through a cell's Plasma membrane Glutamic acid (abbreviated as Glu or E) is one of the 20 Alpha Amino acids It is not among the human Essential amino acids Its Aspartic acid (abbreviated as Asp or D; Asx or B represent either aspartic acid or Asparagine) is an α- Amino acid [9]

Pharmacokinetics

Lamictal (lamotrigine) Scored tablets
Lamictal (lamotrigine) Scored tablets

The pharmacokinetics of lamotrigine are quite complicated, with highly varying half-life and blood plasma levels. Pharmacokinetics (in Greek: “pharmacon” meaning drug and “kinetikos” meaning putting in motion the study of time dependency sometimes abbreviated as “PK” is a Half-Life (computer-game page here It's already listed in the disambiguation page Blood plasma is the Liquid component of Blood, in which the Blood cells are suspended Lamotrigine has fewer drug interactions than many anticonvulsant drugs, although pharmacokinetic interactions with Sodium Valproate in particular is an indication for blood monitoring. The anticonvulsants, also called antiepileptic drugs (abbreviated "AEDs" are a diverse group of pharmaceuticals used in the treatment of epileptic See also Valproic acid Sodium valproate ( INN) or valproate sodium ( USAN) is the sodium salt of Valproic acid and is an

Side effects

Lamotrigine prescribing information has a black box warning about life threatening skin reactions, including Stevens-Johnson Syndrome and Toxic Epidermal Necrolysis. Stevens-Johnson syndrome (SJS is a life-threatening Condition affecting the Skin in which Cell death causes the epidermis to separate from the Toxic epidermal necrolysis (TEN also known as Lyell's syndrome, is a life-threatening dermatological condition that is frequently induced by a reaction to medications [9] The manufacturer states that nearly all cases appear in the first 2 to 8 weeks of therapy and if medication is suddenly stopped then resumed at the normal dosage. Patients should seek medical attention for any unexpected skin rash as its presence is an indication of a possible serious or even deadly side effect of the drug. Not all rashes that occur while taking lamotrigine progress to Stevens-Johnson Syndrome or Toxic Epidermal Necrolysis

Cognitive side effects are common with doses over 50mg qid (quater in die - four times daily), as shown in the 2001-2003 Glaxo-sponsored Clinical Trials comparing quality of life between Topiramate and Lamotrigine in healthy volunteers (unpublished). Stevens-Johnson syndrome (SJS is a life-threatening Condition affecting the Skin in which Cell death causes the epidermis to separate from the Toxic epidermal necrolysis (TEN also known as Lyell's syndrome, is a life-threatening dermatological condition that is frequently induced by a reaction to medications This is the overview for the medical abbreviations series This list is far from complete you can help by expanding it Topiramate (brand name Topamax) is an Anticonvulsant drug produced by Ortho-McNeil Neurologics and Noramco Inc Common side effects include headaches, dizziness and insomnia. A headache ( cephalalgia in medical terminology is a condition of pain in the Head; sometimes Neck or upper back pain may also be interpreted Many different terms are often used to describe what is collectively known as dizziness. Insomnia is a symptom of a sleeping disorder characterized by persistent difficulty falling asleep or staying asleep despite the opportunity Other side effects may include acne and skin irritation, vivid dreams or nightmares, night sweats, body aches and cramps, muscle aches, dry mouth, fatigue, memory and cognitive problems, irritability, weight changes, hair loss, changes in libido, frequent urination, nausea, and other side effects. Acne vulgaris (commonly called acne) is a Skin disease caused by changes in the Pilosebaceous units (skin structures consisting of a Hair follicle A nightmare is a Dream which causes a strong unpleasant emotional response from the sleeper typically fear or horror being in situations of extreme danger or the sensations Sleep hyperhidrosis, more commonly known as the night sweats, is the occurrence of excessive sweating ( Hyperhidrosis) during Sleep. Myalgia means " Muscle Pain " and is a symptom of many diseases and disorders Xerostomia is the medical term for a dry mouth due to a lack of Saliva. In Psychology, memory is an organism's ability to store retain and subsequently retrieve information Irritability is an excessive response to stimuli. Irritability takes many forms from the Contraction of a Unicellular organism when touched to complex Baldness involves the state of lacking hair where it often grows especially on the head Libido in its common usage means Sexual desire however more technical definitions such as those found in the work of Carl Jung, are more general referring to libido In Medicine, polyuria is a condition characterized by the passage of large volumes of urine (at least 2 Nausea ( Latin: Nausea, Greek:, " Sea-sickness " also called wamble) is the sensation of unease and discomfort In very rare cases, Lamotrigine has been known to cause the development of a dangerous rash called Stevens-Johnson syndrome (or SJS). A rash is a change of the Skin which affects its color appearance or Texture. Stevens-Johnson syndrome (SJS is a life-threatening Condition affecting the Skin in which Cell death causes the epidermis to separate from the The rash is more common in children, so this medication is often reserved for adults. There is also an increased incidence of this rash in patients who are currently on, or recently discontinued a valproate-type anticonvulsant drug, as these medications interact in such a way that the clearance of both is decreased and the effective dose of lamotrigine is increased. Valproic acid ( VPA) is a Chemical compound that has found clinical use as an Anticonvulsant and mood-stabilizing drug, primarily in .

In clinical trials women were more likely than men to have side effects. This is the opposite of most other anticonvulsants and antipsychotics. The anticonvulsants, also called antiepileptic drugs (abbreviated "AEDs" are a diverse group of pharmaceuticals used in the treatment of epileptic Antipsychotics are a group of Psychoactive drugs commonly but not exclusively used to treat Psychosis, which is typified by Schizophrenia. It has been suggested that genetic background makes a difference in dosages, with those of non-Caucasian background typically needing lower doses. The Caucasian race, sometimes the Caucasoid race, is a term of Racial classification, coined around 1800 by Johann Friedrich Blumenbach for the "

Lamotrigine binds to melanin-containing tissues such as the iris of the eye. Melanin is a class of compounds found in the Plant, Animal and Protista kingdoms, where it serves predominantly as a Pigment. The long-term consequences of this are unknown. [10]

Use during pregnancy is recommended only if benefits outweigh potential risks. It was also reported on CNN in September 2006 that taking Lamictal during the first trimester of pregnancy can lead to a cleft palate in babies. Cable News Network, usually referred to by its Initialism CNN, is a major English language Television network founded in 1980 by Ted Turner Cleft lip (cheiloschisis and cleft palate (palatoschisis which can also occur together as cleft lip and palate are variations of a type of clefting Congenital Lamotrigine is found in breast milk; breastfeeding is not recommended during treatment. Breast milk refers to the Milk produced by a mother to feed her baby Breastfeeding is the feeding of an Infant or young Child with Breast milk directly from human Breasts, not from a Baby bottle or other

Some patients have reported experiencing a loss of concentration, even with very small doses, while some others have actually reported an increase in alertness and concentration. In general, however, it tends to have less of an impact on concentration relative to other mood stabilizers. GlaxoSmithKline investigated lamotrigine for the treatment of ADHD. GlaxoSmithKline plc () is a United Kingdom -based pharmaceutical, biological and Healthcare Company. Attention-Deficit Hyperactivity Disorder (ADHD is a neurobehavioral developmental disorder affecting about 3-5% of the world's population The results were inconclusive. No detrimental effects on cognitive function were observed, however, the only statistical improvement in core ADHD symptoms was an improvement on a test, PASAT (Paced Auditory Serial Addition Test), that measures auditory processing speed and calculation ability. [11]

Availability

Lamictal 200 mg tablets
Lamictal 200 mg tablets

GlaxoSmithKline's trademarked brand of Lamotrigine, Lamictal, is manufactured in scored tablets (25 mg, 100 mg, 150 mg and 200 mg) and chewable dispersible tablets (2 mg, 5 mg and 25 mg). Five-week sample kits are also available; these include titration instructions and scored tablets (25 mg for patients taking valproate, 25 mg and 100 mg for patients not taking valproate). Titration is a common laboratory method of Quantitative chemical analysis that is used to determine the unknown Concentration of a known Reactant Lamotrigine is also available in un-scored tablet form. In 2005, Teva Pharmaceutical Industries Ltd. began selling generic Lamotrigine in the United States, but only in 5 mg and 25 mg chewable dispersible tablets. Teva Pharmaceutical Industries Ltd (טבע תעשיות פרמצבטיות בע"מ is an international Pharmaceutical company headquartered in Petah Tikva [12] Lamotrigine is also available in generic form[13] in the United Kingdom and Canada. The United Kingdom of Great Britain and Northern Ireland, commonly known as the United Kingdom, the UK or Britain,is a Sovereign state located

Notes

  1. ^ anonymous (2007). LAMOTRIGINE. www. drug. co. il. Retrieved on 2008-04-14. 2008 ( MMVIII) is the current year in accordance with the Gregorian calendar, a Leap year that started on Tuesday of the Common Events 43 BC - Battle of Forum Gallorum: Mark Antony, besieging Julius Caesar 's assassin Decimus Junius Brutus in
  2. ^ Goldberg, M. D. , Ivan K (3/27/06). FAQ: Psychiatric Uses of Lamotrigine (Lamictal).. psycom. net. Retrieved on 2008-04-09. 2008 ( MMVIII) is the current year in accordance with the Gregorian calendar, a Leap year that started on Tuesday of the Common Events 193 - Septimius Severus is proclaimed Roman Emperor by the army in Illyricum (in the Balkans)
  3. ^ anonymous (19 March 2004). EFFICACY SUPPLEMENTS APPROVED IN CALENDAR YEAR 2003. FDA/Center for Drug Evaluation and Research. Retrieved on 2008-04-09. 2008 ( MMVIII) is the current year in accordance with the Gregorian calendar, a Leap year that started on Tuesday of the Common Events 193 - Septimius Severus is proclaimed Roman Emperor by the army in Illyricum (in the Balkans)
  4. ^ GlaxoSmithKline, 2003
  5. ^ French et al. , 2004
  6. ^ Pellock, 1999
  7. ^ Backonja, 2004; Jensen 2002; Pappagallo, 2003
  8. ^ Barbosa, Berk & Vorster, 2003
  9. ^ a b anonymous (May 2007). LAMICTAL PRESCRIBING INFORMATION. GlaxoSmithKline. . Retrieved on 2008-04-09. 2008 ( MMVIII) is the current year in accordance with the Gregorian calendar, a Leap year that started on Tuesday of the Common Events 193 - Septimius Severus is proclaimed Roman Emperor by the army in Illyricum (in the Balkans)
  10. ^ anonymous. Lamictal, Warnings & Precautions. RxList Inc. . Retrieved on 2008-04-09. 2008 ( MMVIII) is the current year in accordance with the Gregorian calendar, a Leap year that started on Tuesday of the Common Events 193 - Septimius Severus is proclaimed Roman Emperor by the army in Illyricum (in the Balkans)
  11. ^ anonymous. lamotrigine studies. GlaxoSmithKline. Retrieved on 2008-04-09. 2008 ( MMVIII) is the current year in accordance with the Gregorian calendar, a Leap year that started on Tuesday of the Common Events 193 - Septimius Severus is proclaimed Roman Emperor by the army in Illyricum (in the Balkans)
  12. ^ anonymous (17 February 2005). Press Release, Teva Announces Settlement Of Lamictal® Litigation With Glaxosmithkline. Teva Pharmaceutical Industries Ltd. . Retrieved on 2008-04-09. 2008 ( MMVIII) is the current year in accordance with the Gregorian calendar, a Leap year that started on Tuesday of the Common Events 193 - Septimius Severus is proclaimed Roman Emperor by the army in Illyricum (in the Balkans)
  13. ^ anonymous (2 March 2005). Treatment for epilepsy: generic lamotrigine. Department of Health (UK). Retrieved on 2008-04-09. 2008 ( MMVIII) is the current year in accordance with the Gregorian calendar, a Leap year that started on Tuesday of the Common Events 193 - Septimius Severus is proclaimed Roman Emperor by the army in Illyricum (in the Balkans)

References

External links

Dictionary

lamotrigine

-noun

  1. An anticonvulsant drug used in the treatment of epilepsy
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