Inxight Drugs

Search results for "EMA EPAR|DISEASES|NERVOUS SYSTEM DISEASES|CENTRAL NERVOUS SYSTEM DISEASES|BRAIN DISEASES" in comments (approximate match)

Showing 1 - 10 of 28 results

STIRIPENTOL

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R02XOT8V8I

Status:

US Approved Rx (2018)

First approved in 2018

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

Conditions:

Stiripentol is an anticonvulsant drug used in the treatment of epilepsy. It recently proved to increase the GABAergic transmission in vitro in an experimental model of immature rat. Clinical studies were based on the fact that STP also acts as an inh...

Perampanel

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H821664NPK

Status:

US Approved Rx (2016)

First approved in 2012

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Perampanel (trade name Fycompa) is an antiepileptic drug developed by Eisai Co. that acts as a selective non-competitive antagonist of AMPA receptors, the major subtype of ionotropic glutamate receptors. Although the mechanism of action through which...

Lacosamide

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563KS2PQY5

Status:

US Approved Rx (2022)

First approved in 2008

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Lacosamide is an anticonvulsant that is FDA approved for the treatment of partial-onset seizures. The precise mechanism by which lacosamide exerts its antiepileptic effects in humans remains to be fully elucidated. In vitro electrophysiological studi...

RUFINAMIDE

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WFW942PR79

Status:

US Approved Rx (2022)

First approved in 2008

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Rufinamide is an anti-epileptic drug that is FDA approved for the treatment of lennox-gastaut syndrome (LGS). The principal mechanism of action of rufinamide is modulation of the activity of sodium channels and, in particular, prolongation of the ina...

PREGABALIN

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55JG375S6M

Status:

US Approved Rx (2010)

First approved in 2004

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Pregabalin, marketed under the brand name Lyrica among others. LYRICA is indicated for: Neuropathic pain associated with diabetic peripheral neuropathy (DPN) Postherpetic neuralgia (PHN); Adjunctive therapy for adult patients with partial onset seizu...

Miglustat

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ADN3S497AZ

Status:

US Approved Rx (2003)

First approved in 2003

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Miglustat, an N-alkylated imino sugar, is a synthetic analogue of D-glucose. Miglustat is an inhibitor of the enzyme glucosylceramide synthase, which is a glucosyl transferase enzyme responsible for catalyzing the formation of glucosylceramide (gluco...

cerebroside). Glucosylceramide is a substrate for the endogenous glucocerebrosidase, an enzyme that is deficient in Gaucher's disease. The accumulation of glucosylceramide due to the absence of glucocerebrosidase results in the storage of this material in the lysosomes of tissue macrophages, leading to widespread pathology due to infiltration of lipid-engorged macrophages in the viscera, lymph nodes, and bone marrow. This results in secondary hematologic consequences including sever anemia and thrombocytopenia, in addition to the characteristic progressive hepatosplenomegaly, as well as skeletal complications including osteonecrosis and osteopenia with secondary pathological fractures. Miglustat functions as a competitive and reversible inhibitor of the enzyme glucosylceramide synthase, the initial enzyme in a series of reactions which results in the synthesis of most glycosphingolipids. The goal of treatment with miglustat is to reduce the rate of glycosphingolipid biosynthesis so that the amount of glycosphingolipid substrate is reduced to a level which allows the residual activity of the deficient glucocerebrosidase enzyme to be more effective (substrate reduction therapy), reducing the accumulation of glucocerebroside in macrophages. In vitro and in vivo studies have shown that miglustat can reduce the synthesis of glucosylceramide-based glycosphingolipids. In clinical trials, miglustat improved liver and spleen volume, as well as hemoglobin concentration and platelet count. Inhibition of glycosphingolipid synthesis has also shown to reduce intracellular lipid storage, improve fluid-phase endosomal uptake and normalize lipid transport in peripheral blood B lymphocytes of NP-C patients, which results in a decrease in the potentially neurotoxic accumulation of gnagliosides GM2 and GM3, lactosylceramide and glucosylceramide, possibly preventing further neuronal damage. Other studies have also suggested that miglustat may indirectly modulate intracellular calcium homeostasis through its effects on glucosylceramide levels, and evidence has shown that an initiating factor in the pathogenesis of NP-C may be impaired calcium homeostasis related to sphingosine storage. Therefore, the effect that miglustat exerts on intracellular calcium levels may influence an important underlying pathogenic mechanism of NP-C. Miglustat is used for the treatment of adult patients with mild to moderate type 1 (nonneuropathic) Gaucher's disease for whom enzyme replacement therapy is not a therapeutic option (e.g. due to constraints such as allergy, hypersensitivity, or poor venous access). Now approved in some countries for the treatment of progressive neurological symptoms in adult and pediatric patients with Niemann-Pick disease type C (NP-C). Miglustat is marketed under the trade name Zavesca.

NITISINONE

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K5BN214699

Status:

US Approved Rx (2019)

First approved in 2002

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Nitisinone, 2-(2-nitro-4-trifluoromethylbenzoyl)-1,3-cyclohexanedione (NTBC) is a triketone with herbicidal activity. Orfadin® capsules contain nitisinone used in the treatment of hereditary tyrosinemia type 1 (HT-1). Nitisinone is a competitive inhi...

ZONISAMIDE

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459384H98V

Status:

US Approved Rx (2005)

First approved in 2000

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Zonisamide is an antiseizure drug chemically classified as a sulfonamide and unrelated to other antiseizure agents. The precise mechanism by which zonisamide exerts its antiseizure effect is unknown, although it is believed that the drug blocks sodiu...

LEVETIRACETAM

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44YRR34555

Status:

US Approved Rx (2009)

First approved in 1999

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Levetiracetam is an anticonvulsant medication used to treat epilepsy. Levetiracetam may selectively prevent hypersynchronization of epileptiform burst firing and propagation of seizure activity. The precise mechanism(s) by which levetiracetam exerts ...

its antiepileptic effect is unknown. The antiepileptic activity of levetiracetam was assessed in a number of animal models of epileptic seizures. Levetiracetam did not inhibit single seizures induced by maximal stimulation with electrical current or different chemoconvulsants and showed only minimal activity in submaximal stimulation and in threshold tests. Levetiracetam also displayed inhibitory properties in the kindling model in rats, another model of human complex partial seizures, both during kindling development and in the fully kindled state. The predictive value of these animal models for specific types of human epilepsy is uncertain. In vitro and in vivo recordings of epileptiform activity from the hippocampus have shown that levetiracetam inhibits burst firing without affecting normal neuronal excitability, suggesting that levetiracetam may selectively prevent hypersynchronization of epileptiform burst firing and propagation of seizure activity. Levetiracetam at concentrations of up to 10 µM did not demonstrate binding affinity for a variety of known receptors, such as those associated with benzodiazepines, GABA (gamma-aminobutyric acid), glycine, NMDA (Nmethyl-D-aspartate), re-uptake sites, and second messenger systems. Furthermore, in vitro studies have failed to find an effect of levetiracetam on neuronal voltage-gated sodium or T-type calcium currents and levetiracetam does not appear to directly facilitate GABAergic neurotransmission. However, in vitro studies have demonstrated that levetiracetam opposes the activity of negative modulators of GABA- and glycine-gated currents and partially inhibits N-type calcium currents in neuronal cells. A saturable and stereoselective neuronal binding site in rat brain tissue has been described for levetiracetam. Experimental data indicate that this binding site is the synaptic vesicle protein SV2A, thought to be involved in the regulation of vesicle exocytosis. Interaction of levetiracetam with the SV2A protein may contribute to the antiepileptic mechanism of action of the drug. Levetiracetam, along with other anti-epileptic drugs, can increase the risk of suicide behavior or thoughts. People taking levetiracetam should be monitored closely for signs of worsening depression, suicidal thoughts or tendencies, or any altered emotional or behavioral states.

EZOGABINE

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12G01I6BBU

Status:

US Previously Marketed

First approved in 2011

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Ezogabine (U.S. adopted name) or retigabine (international nonproprietary name) is one of a family of aminopyrroles with anticonvulsant activity. It is used as an adjunctive treatment for partial epilepsies in treatment-experienced adult patients. Th...

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Condition

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Substance Form

Search results for "EMA EPAR|DISEASES|NERVOUS SYSTEM DISEASES|CENTRAL NERVOUS SYSTEM DISEASES|BRAIN DISEASES" in comments (approximate match)

STIRIPENTOL

R02XOT8V8I

Perampanel

H821664NPK

Lacosamide

563KS2PQY5

RUFINAMIDE

WFW942PR79

PREGABALIN

55JG375S6M

Miglustat

ADN3S497AZ

NITISINONE

K5BN214699

ZONISAMIDE

459384H98V

LEVETIRACETAM

44YRR34555

EZOGABINE

12G01I6BBU