Gabapentin - litaelo tsa tšebeliso le litlhahlobo

Tlhaloso e amanang le 04.02.2015

• Lebitso la Latin: Gabapentin
• Khoutu ea ATX: N03AX12
• Lintho tse sebetsang: Gabapentin
• Moetsi: PIK-PHARMA, Canonfarm Production CJSC (Russia), Aurobindo Pharma (India), Erregierre S.p.A. (Itali)

Ho 1 capsule gabapentin 300 mg

Calcium hydrogen phosphate, starch ea litapole, macrogol, stearate ea magnesium - joalo ka ba ananelang.

Matšoao a ho sebelisoa

• monotherapy tsepamiso ea maikutlo ho lefu la sethoathoa ho batho ba baholo le ho bana ba lilemo tse 12,
• kalafo e eketsehileng tsepamiso ea maikutlo le lefu la sethoathoa ho batho ba baholo,
• kalafo e eketsehileng lefu la sethoathoa baneng ho tloha lilemong tse 3,
• migraine,
• bohloko ba neuropathic (neuralgia postherpetic, lefu la tsoekere, trigeminal, amanang le HIV, joala bo nang le lesapo la mokokotlo),
• ho fokotseha ha botebo ba maqhubu nakong ea ho khaotsa ho ilela khoeli.

Contraindication

• bohale pancreatitis,
• hypersensitivity ho lithethefatsi,
• galactose mamello kapa malabsorption ea tsoekere le galactose,
• lilemo ho isa ho lilemo tse 3 ka ho ts'oaroa ke sethoathoa,
• lilemo ho isa ho lilemo tse 12 ka postherpetic neuralgia,
• boimana.

Litlamorao

• eketsa HELL, tachycardia,
• dyspepsia, ho nyekeloa ke pelo, bohloko ba ka mpeng, molomo o omileng, ho ipolaisa tlala kapa lets'ollo, pancreatitis, botlaela, gingivitis,
• myalgiabohloko ba morao
• ho otsela, ho tsekela, nystagmuseketsehile mokhathalale thabo, dysarthria, gbohloko ba tin, khatello ea maikutlopherekano hyperkinesia,ho tšoenyeha, ho hloka boroko,
• rhinitis, pharyngitis, khohlela,
• ho robala ka ntle ho moroto, ho senyeha ha potoloho,
• ho senyeha ha pono, tinnitus,
• letlalo makhophoexudative erythema,
• boima ba 'mele, ho ruruha sefahleho, ho ruruha.

Tšebelisano

Tšebeliso e tšoanang ea lithethefatsi tse ling tsa antiepileptic e lumelletsoe (Phenobarbital, Carbamazepine, Phenytoin, Valproic Acid) le lithibela-pelehi tsa molomo. Tabeng ena, li-pharmacokinetics tsa gabapentin ha li fetohe.

Li-antacid li fokotsa bioavailability ea moriana, ka hona ho nka lithethefatsi tse ka sehloohong le li-antacid li hasana nako e telele.

Lithethefatsi tsa Myelotoxic li eketsa ho ata ha hematotoxicity ea gabapentin.

Ka kopanelo le morphine morphine pharmacokinetics ha ea ka ea fetoha. Leha ho le joalo, liphetoho tse ka bang teng tse tsoang tsamaisong ea methapo e kholo li lokela ho beoa leihlo.

Ho nwa joala ho ka eketsa likarohano tse mpe tse tsoang tsamaisong ea methapo e ka hare (ataxia, stupor).

Litaelo tse khethehileng

Haeba ho hlokahala ho khaotsa lithethefatsi, phokotso ea litekanyetso e lokela ho etsoa butle-butle (ka libeke tse 1-2), hobane ho tlohela kalafo ho ka baka epistatus. Nakong ea kemolo, hoa lumelloa ho sebelisa ho latela matšoao a thata, ha molemo ho 'm'a o feta kotsi ho lesea.

Haeba ataxia, ho tsekela, boima ba 'mele, ho otsela ho hlaha ho batho ba baholo,' me ho otsela le ho hloea bana, kalafo e lokela ho khaotsa. Nakong ea kalafo, o hloka ho hana ho khanna.

Khokahano le sebopeho sa moriana

Gabapentin e fumaneha ka foromo ea capsule bakeng sa tsamaiso ea molomo. Setlhare sena se kentsoe ka makotikoting a polasetiki a likotoana tse 50 kapa tse 100 kapa ka matlakala a likotoana tse 10 -15 ka lebokoseng la karete.

K'hapete ka 'ngoe e na le ntho e sebetsang - gabapentin 300 mg, hammoho le likarolo tse' maloa tse thusang: calcium stearate, gelatin, titanium dioxide, cellcose ea microcrystalline.

Sebelisa ho tsa bongaka

Gabapentin e qapiloe Parke-Davis mme e hlalositsoe ka lekhetlo la pele ka 1975. Tlas'a lebitso la mabitso la Neurontin, e ile ea amoheloa ka la pele ka Mots'eanong 1993 bakeng sa kalafo ea lefu la sethoathoa UK mme ea rekisoa United States ka 1994. Kamora moo, gabapentin e ile ea amoheloa naheng ea Amerika bakeng sa kalafo ea neuralgia ea postherpetic ka May 2002. Ka Pherekhong 2011, United States e amohetse mofuta oa tekanyetso ea tsoekere e tsoetseng pele ea taolo ea letsatsi le letsatsi tlasa lebitso la brand Gralise. Gabantine anacarbil tlasa lebitso la brand Horizant, e nang le lefu le phahameng la bioavailability, e ile ea hlahisoa United States bakeng sa kalafo ea methapo ea maoto e sa phumoleng ka Mmesa 2011 mme ea amoheloa bakeng sa kalafo ea postalopetic neuralgia ka Phuptjane 2012.

Sebelisa ho tsa bongaka

Gabapentin e sebelisoa haholo ho phekola ho ruruha le bohloko ba neuropathic. Sena se tsamaisoa haholo-holo ka molomo, 'me lipatlisiso li bonts'a hore "tsamaiso ea methapo ha e khotsofatse." E boetse e laeloa hangata bakeng sa lits'ebetso tse ngata tse sa tsejoeng, joalo ka kalafo ea mathata a ho tšoenyeha, ho hloka boroko le lefu la ho ferekana kelellong. Leha ho le joalo, ho na le ho tšoenyeha ka boleng ba liteko tse entsoeng le bopaki ba tse ling tsa lits'ebetso tsena, haholo-holo ha li sebelisoa e le mohopolo oa ho feto-fetoha ha maikutlo ho ferekanyang kelello.

Pharmacological thepa ea lithethefatsi

Gabapentin ke sethethefatsi se nang le phello e bitsoang anticonvulsant. Tlas'a tšusumetso ea lithethefatsi ho bakuli ba nang le lefu la sethoathoa, e fokotsa kotsi ea ho hlaseloa khafetsa.

Motsoako ona o sebelisetsoa ho phekola batho ba baholo le bana bakeng sa kalafo ea lefu la sethoathoa le bohloko ba neuropathic khahlano le semelo sa shingles.

Pharadodynamics

Ka sebopeho, gabapentin e ts'oana le GABA neurotransmitter (gamma-aminobutyric acid), empa ts'ebetso ea ts'ebetso ea eona e fapane le lithethefatsi tse ling tse sebelisanang le li-receptor tsa GABA (valproic acid, barbiturates, benzodiazepines, GABA uptake inhibitors, GABA transaminase inhibitors, le agonists of the gabe transaminase Liforomo tsa GABA).

Gabapentin ha e na thepa ea GABAergic ebile ha e ame ho fumanoa le metabolism ea GABA. Ho latela lithuto tsa pele, ntho ena e tlama ho α₂-δ-subunit ea liteishene tsa calcium tse itšetlehileng ka matla le ho fokotsa ho phalla ha ion ea calcium, e etsang karolo ea bohlokoa ntlafatsong ea bohloko ba neuropathic.

Mekhoa e meng ea ts'ebetso ea bohloko ba neuropathic:

• Kakaretso ea GABA,
• fokotseha hoa lefu le itlhommeng pele la glutamate,
• khatello ea ho ntšoa ha li-neurotransmitters tsa sehlopha sa monoamine.

Litekong tse bohlokoa tsa kliniki ea gabapentin e nang le li-receptor bakeng sa lithethefatsi tse ling kapa li-neurotransmitters tse kenyeletsang GABA receptors_HoGABA_A, glycine, glutamate, N-methyl-D-aspartate, kapa li-receptor tsa benzodiazepine, ha e tlamele.

Gabapentin, ho fapana le carbamazepine le phenytoin, ha e sebelisane le menyetla ea sodium ho vitro. Nakong ea phekolo ea in vitro, liteko tse ling tsa vitro li bonts'a ho lekola ho sa lekanyetsoang ka litlamorao tsa glutamate receptor agonist N-methyl-D-aspartate, empa ke feela pokellong ea> 100 μmol, e sa fihleheng ho vivo. Gabapentin hanyane o fokotsa tokollo ea li-neurotransmitters tsa monoamine.

Mofumahali

The bioavailability ea gabapentin ha ea itšetleha ka litekanyetso ka tlhaho mme e fokotseha ka tekanyetso e ntseng e eketseha. C_max (boholo ba mahloriso a ntho) gabapentin ho plasma kamora hore tsamaiso ea molomo e fihlelloe ka lihora tse 2-3. Boaoavailability e felletseng e ka ba 60%. Lijo, ho kenyelletsa le mafura a mangata, ha li ame maemo a pharmacokinetic.

Ho felisoa ha lintho ho plasma ho hlalosoa hantle ho sebelisoa mohlala. T_1/2 (ho tlosa halofo ea bophelo) ho tloha ka karolelano ea plasma makhetlo a 5-7 mme ha ea its'etleha ka lethal dose. Ha e sebelisoa khafetsa, paramente ea pharmacokinetic ha e fetohe. Boleng ba ho lekana ha plasma ho lekana ho ka boleloa esale pele ho latela liphetho tsa lethal dose le le leng la moriana.

Gabapentin ha e amane le liprotheine tsa plasma (80 - 900-2400 mg ka letsatsi,