Konvalis: litaelo, litlhahlobo, li-analogues le litheko

Karolo e sebetsang ea sehlahisoa se ts'oana le sebopeho ho gamma-aminobutyric acide leng neurotransmitter. Ntho e tlama hoalpha-2-δ-subunit ea liteishene tsa calciummme e emise ho phalla ha calcium ho tsona. Ke likheo tsena tse fanang ka phetiso ea ts'usumetso ea methapo e bonts'a bohloko.

Hape, sesebelisoa se ea fokotsa glutamate itšetlehalefu la li-neuron, le eketsa synthesis GABAe fokotsa sekhahla sa tokollo li-neurotransmitterssehlopha sa monoamine.

Likarolong tse tloaelehileng tsa kelello ho lero la mali sethethefatsi ha se ame tse ling Li-receptors tsa GABA, benzodiazepine, glutamate le li-receptors tse ling. Ntho ha e sebelisane le liteishene tsa sodium.

Haeba u eketsa litekanyetso tsa moriana, ts'ebetso ea lona ea bioavailability e tla fokotseha ka lehlakoreng le leng. Boholo ba mahloriso a plasma madi e etsahala lihora tse 2-3 kamora tsamaiso. Bioavailability e ka ba 60%. Ho ja, leha ho na le mafura a mangata, ha ho ame likarolo tsa lithethefatsi tsa pharmacokinetic.

Ho felisoa ha halofo ea bophelo ke lihora tse ka bang 6. Ntho e sebetsang ha e na bokhoni ba ho tlama liprotheine tsa plasma.

Moriana ha o bokelle 'meleng, ha o bake tlhahiso ea li-enzyme tsa sebete. Ho ikarola 'meleng ho tsoa liping ka moroto. Leha ho le joalo, ho bakuli ba tsofetseng, batho ba nang le mafu a sebete, tumello ea gabapentin fokotsoe hanyane.

Bakuli ba nang le bothata ba ho renal bo sa sebetseng hantle, haholoholo bo fetang nako le nako hemodialysis, Litekanyetso tsa letsatsi le letsatsi li lokela ho fetoloa.

Matšoao a ho sebelisoa

• ho lefu la sethoathoa batho ba baholo le bana ba lilemo tse 12 e le karolo ea kalafo e felletseng kapa e le sesebelisoa se ikemetseng.
• bakeng sa kalafo bohloko ba neuropathic,
• ho lefu la sethoathoa le kakaretso general.

Contraindication

Likarete ha li khone ho sebelisoa:

• bana ba ka tlase ho lilemo tse 12
• ho pancreatitis e hlobaetsang,
• batho ba nang le mamello lactose, khaello ea lactase le glucose galactose malabsorption,
• hodima phumaneho allergy ka likarolo tsa moriana.

Bakuli ba nang le bothata ba ho hloleha ha remstlhokomelo e lokela ho nkuoa ha o sebelisa moriana.

Litlamorao

Ha u sebelisa meriana ho phekola bohloko ba neuropathic e ka etsahala:

Haeba moriana o laetsoe kalafo ho ts'oaroa ka nakoanaebe litla-morao tse latelang lia hlaha:

• leukopenia, letsolo,
• lability khatello ea mali, vasodilationts'ebetso ea ho ruruha ka hanong (mafu a meno le marenene),
• makhophomakhopho le ho hlohlona letlalong,
• gingivitis, ho sokela, lets'ollophahamisoa takatso ea lijo le ho sithabelaho nyekeloa botlaelabohloko ho tikoloho ea epigastric,
• bohloko ba morao, ho ruruha ha mesifa ea mesifa, arthralgiabrittle bones
• ho tsekelaMathata a na le tendon reflexes, matšoenyeho, khatello ea maikutlokhatello ea maikutlo, nystagmusmathata a ho nahana,
• nko e otlangkhohlela pneumonia,
• nts'etsopele ea ts'oaetso karolo ea liphatsa tsa lefutso,
• hyperkinesis, paresthesia, amnesiapherekano le tšebelisano e mpe ea ts'ebetso, dysarthria, ho hloka boroko, thothomela,
• ho fokotseha libido le ho hloka matla,
• ho senyeha ha pono, diplopiamokhathala, ho ruruha ha sefahleho le periphery, asthenia.

Liphetoho tse fapaneng tse kang ataxia, ho tsekela, nystagmus le ho otsela, ho latela tekanyo e nkuoeng.

Ka ho khaotsa ho tebela matlapa, ho ka ba le matšoao a ho khaotsa: ho nyekeloa ke pelo, bohloko libakeng tse fapaneng, ho fufuleloa, ho tšoenyeha, ho khathatseha boroko.

Litaelo tsa ho sebelisoa Konvalisa (Mokhoa le litekanyetso)

Setlhare se nooa ka molomo ntle le ho hlafuna kapa ho arola letlapa, ho sa tsotelehe lijo.

Litaelo tsa tšebeliso ea Convalis e le moriana oa lefu la sethoathoa

Litekanyetso tsa pele ke 300 mg ka letsatsi. Ebe tekanyetso ea letsatsi le letsatsi e eketsoa ho 900 mg, e ajoa ka linako tsohle. Kamora moo, haeba ho hlokahala le ka khothatso ea ngaka e eang, palo ea lithethefatsi ka letsatsi e ka fihla 1200 mg.

Max Qty gabapentine ka noang letsatsi lohle ke 3600 mg (lihora tse ling le tse ling tse 8). Nako e pakeng tsa tekanyetso ha e fetise lihora tse 12.

Phekolo ea bohloko ea Neuropathic

Ka letsatsi la pele, 300 mg ea moriana o nooa, ka la bobeli - 600 mg ho litekanyetso tse peli tse arohaneng, ka boraro - 300 mg, makhetlo a 3 ka letsatsi. Ho ea pele, litekanyetso tsa letsatsi le letsatsi li ka eketsoa ho 3600 mg.

Ka lefu la liphio:

• haeba tumello ea creatinine e tsoa ho 50 ho isa ho 79 di ml ka motsotso, joale u ka noa 600-1800 mg ea moriana ka letsatsi,
• haeba KK ho tloha ho 30 ho isa ho 49 ml / min - ho fihla ho 900 mg ka letsatsi,
• haeba lengolo la tumello le ka fihla ho 30 ml / min - 600 mg,
• ka tumello ea ka tlase ho 15 ml ka motsotso, litekanyetso tsa 300 mg ka letsatsi li lokela ho lateloa.

Ho bakuli ho hemodialysis, Kamora 'metsotso e mene le e' ngoe ea lihora tse 4, ho nooa moriana o eketsehileng oa 300 mg.

Matsatsing ao lets'ollo ha e etsoe, ho eketsa tekanyetso ea letsatsi le letsatsi ha ho na letho.

Bongata

Haeba o sebelisa sesebelisoa sena hampe o ka hlaha ho tsekela, lets'ollo, diplopia, dysarthria le ho otsela.

E le mehato ea kalafo ea ho felisa litlamorao tse sa batleheng, ho lavage ea ka mpeng ho laetsoe lihora tsa pele kamora ho sebelisa overdose, ho nka hangosorbentsmatšoao a kalafo. E sebetsa hantle hemodialysis.

Tšebelisano

Cimetidine e eketsa nako ea ho felisoa gabapentin kantle ho mmele.

Batho ba amohelang chelete ka nako e le ngoe lithibela-pelehi tsa molomotse nang ethinyl estradiolkapa norethisterone ha e bake tšebelisano ea bona ea lithethefatsi.

Motsoako oa meriana le morphinehaeba morphine e ile ea nkuoa metsotso e 120 pele ho moogabapentine lebisa katolosong Auc chelete ka 50% le ho eketsa bohloko.

Ha u ntse u sebelisa lithethefatsi ka li-anticonvulsants tse ling (Phenobarbital, Valproic Acid, Carbamazepine, Phenytoin) ha ho na ho sebelisana pakeng tsa lithethefatsi.

Li-antacid tse nang aluminiumkapa magnesiumfokotsa bioavailability ea lithethefatsi. Nka chelete ena nako le nako ea lihora tse peli.

Motsoako o kopaneng le lithethefatsi tse nang le ethanol, litlamorao li ka mpefala.

Mokhahlelo oa kopanelo le Naproxen ho lebisa keketseho ea nako ea ho amoheloa ha Convalis.

Litaelo tse khethehileng

Ka nako e 'ngoe ka mor'a ho qala ho sebelisa moriana oa batho ba nang le bothata ba lefu la tsoekereho ka hlokahala phetoho ea litekanyetso hypoglycemic agents.

Ha ho hlahlojoa moroto oa ho sebelisa protheinepampiri ea litmus Liphetho li ka sotha. Ho khothalletsoa ho etsa tlhahlobo u sebelisa mokhoa o mong.

Ha ho khothalletsoe ho khanna kapa ho etsa liketso tse hlokang tlhokomelo e phahameng ea tlhokomelo haeba u ntse u nka Convalis.

Haeba nakong ea kalafo ka kalafo ho amohela a hlobaetsang le pancreatitis, kalafo e tlameha ho kenella.

Ho hlakoloa kapa ho khutlisoa ha matlapa ho lokela ho etsoa butle butle, matsatsing a 7 ka lebaka la kotsi e eketsehileng ea ho ts'oaroa.

Ho boetse ho khothalletsoa ho etsa tlhahlobo ea nako ea kelello ea mokuli. Nakong ea kalafo, kotsi ea ho hola khatello ea maikutloketsahalo menahano ea ho ipolaea le liketso.

Li-analog tsa Convalis

Litšoantšiso tse atileng haholo tsa moriana: Algerica, Gerolamic, Lamiktal, Normeg, Lamitrile, Latrigil, Topiramin, Levetiracetam, Levicit, Lyric, Epimil, Topilex, Neogabin, Topamax, Topilepsin, Epileptal, Epiramat, Epitrizhin, Wimpat, Keppra, Lamitor, Lamitor.

Gabagma, Gabantin, Grimodin, Neuralgin, Tebantin, Gabalept, Gabapentin, Gabalept, Meditan, Newropentin.

Litlhahlobo mabapi le Convalis

Ba arabela hantle ho moriana, haholo-holo nakong ea kalafo lefu la sethoathoa. Litla-morao tse atileng haholo ke ho opeloa ke hlooho, ho nyekeloa le pelo le mathata a ho ja. Hape belaela ka se etsahetseng syndrome ea ho ntša cheleteka ho khaotsa ho matla ha ho nka matlapa.

Maikutlo mabapi le Konvalis ka liforamu:

• “... Setlhare se setle haholo, leha ho le joalo, se tlameha ho nkuoa nako e telele 'me se latele mokhoa o boletsoeng oa kalafo”,
• “... Ke na le bothata ba ho ba le bothata ba mokokotlo oa disc intervertebral disc, ho Konvalis Ke ne ke ikutloa ke le betere haholo, ke khona ho tsamaea haholo, ke le mafolofolo haholoanyane. Empa kamora hore thupelo e felile, bohloko bo ile ba khutla”,
• “... Mahloko a Neuropathic a lula a le joalo. Ke nnete, kamora lihora tse 2x 3 kamora ho nka, ho a khonahala ho robala lihora tse 3-4”.

Sokolla foromo le sebopeho

Mofuta oa litekanyetso tsa lithethefatsi ke li-capsules tse mosehla, tse nang le litaba ka mokhoa oa phofo ea kristale ea 'mala o mosoeu kapa o bosoeu bo bosehla (li-capsules tse 10 ka pakete, lipakete tse 3 kapa tse 5 ka lebokoseng la karete.

Ntho e sebetsang ke gabapentin, 300 mg ho 1 capsule e le 'ngoe.

Lintho tse ling tse eketsoang: stgel ea pele ea poone, lactose monohydrate, magnesium stearate, talc.

Sebopeho sa khase ea gelatin e thata: dae ea tshepe e nang le oxide, gelatin, titanium dioxide.

Tekanyetso le tsamaiso

Setlhare se nooa ka molomo, ho sa tsotelehe lijo tse ngata, ho metsa ka botlalo, ntle le ho hlafuna le ho noa ka metsi.

Ha o etsa monotherapy mme o sebelisa Convalis e le mokhoa oa ho phekola ho ts'oaroa ha sethoathoa sa sethoathoa ho batho ba baholo le bana ba fetang lilemo tse 12, ho khothalletsoa ho qala ka tekanyetso ea letsatsi le letsatsi ea 300 mg mme butle-butle a e eketse ka 900 mg:

• Letsatsi la pele - 300 mg 1 nako,
• Letsatsi la bobeli - 300 mg makhetlo a 2,
• Letsatsi la boraro - 300 mg makhetlo a 3.

Nakong e tlang, tekanyetso ea letsatsi le letsatsi e ka eketsoa. Ka karolelano, e ka ba 900-1200 mg, lethal dose le leholo ka letsatsi ke 3600 mg, e arotsoe ka litekanyetso tse 3 tse lekanang le karohano ea lihora tse 8. Nako e phahameng pakeng tsa litekanyetso ha ea lokela ho ba lihora tse fetang tse 12 (ho qoba ho ts'oaroa hape).

Ha ho phekoloa bohloko ba neuropathic ho batho ba baholo, Convalis o laetsoe ka letsatsi la pele ka tekanyetso ea 300 mg, ka letsatsi la bobeli - 600 mg (300 mg makhetlo a 2), ka letsatsi la boraro - 900 mg (300 mg makhetlo a 3). Maemong a bohloko bo boholo, moriana o ka laetsoa ka letsatsi la pele makhetlo a mararo ho 300 mg. Ho ipapisitse le katleho ea moriana, lethalinyana le ka eketsoa butle-butle, empa eseng hofeta ho feta 3600 mg / ka letsatsi.

Litekanyetso tse latelang tsa letsatsi le letsatsi li fuoe bakuli ba nang le ts'ebetso ea renal e sa sebetseng, ho latela tumellano ea creatinine (QC):

• KK 50-79 ml / metsotso - 600-1800 mg,
• KK 30-49 ml / metsotso - 300-900 mg,
• KK 15-29 ml / metsotso - 300-600 mg,
• CC ka tlase ho 15 ml / min - 300 mg (letsatsi le letsatsi kapa ka letsatsi le leng le le leng).

Ho kenyelletsoa tekanyetso ea pele ea 300 mg bakeng sa bakuli ba ho hemodialysis, ho fanoa ka tekanyetso ea 300 mg ea post-hemodialysis kamora ho qeta karolo e ngoe le e ngoe e nang le lihora tse 4. Matsatsing ao ha dialysis e sa sebetse, setlhare ha se fuoe.

Litlamorao

Litlamorao tse latelang li ka hlaha nakong ea kalafo ea bohloko ba neuropathic:

• Tsamaiso ea methapo e bohareng (CNS): amnesia, pherekano, ataxia, lefu le sa tsitsang, ho otsela, ho tsekela, ts'ebetso ea kelello, ho thothomela, monahano o fosahetseng,
• Sistimi ea tšilo ea lijo: dyspepsia, lets'ollo, ho sokela, ho nyekeloa, ho ruruha, ho hlatsa, molomo o omileng, bohloko ba ka mpeng,
• Sistimi ea maikutlo: pharyngitis, dyspnea,
• Litho tsa letsoalo: amblyopia,
• Letlalo: lekhopho la letlalo,
• Tse ling: lefu le kang la ntaramane, mafu a tšoaetsanoang, asthenic syndrome, hlooho e bohloko, edema ea ho potoloha, bohloko ba ho ferekanya ba fapaneng ba naha, ho nona ka boima.

Phekolo ea ho ts'oaroa ka mokhoa o fapaneng le Convalis, ho ka bonoa tse latelang:

• Sisteme ea mali: leukopenia, purpura (hangata e le ka tsela ea ho longoa ho etsahalang nakong ea khatello ea maikutlo),
• Sistimi ea pelo: ho fokotseha kapa keketseho ea khatello ea mali (BP), matšoao a vasodilation,
• Tsamaiso ea methapo: paresthesia, ho holisa, ho fokolisa matla kapa ho se be teng ha methapo ea kutlo, ho hloka taolo, ho tsitsipana, ho ferekana, ho ferekana, ho ferekana maikutlong, ho otsela, nystagmus, ho hloka boroko, ho nahana ka tsela e sa sebetseng, ho ts'oaroa ke mesifa hyperkinesis
• Sistimi ea tšilo ea lijo: dyspepsia, molomo o ommeng kapa 'metso, bolutu, ho nyekeloa, ho hlatsa, ho sokela, ho nyekeloa, ho nyekeloa ke pelo, ho opeloa ke mpa, ho eketsa takatso ea lijo, lefu la meno.
• Sistimi ea musculoskeletal: myalgia, bohloko ba morao, arthralgia, ho eketseha ha masapo hoa masapo,
• Sistimi ea khatello ea kelello: rhinitis, pharyngitis, khohlela, pneumonia,
• Tsamaiso ea methapo ea kutlo le ho ba le bana: ts'oaetso ea ts'ehetso ea mochine, ho hloka matla,
• Letlalo: ho hlohlona ha letlalo, makhopho, maqeba, letlalo lekhopho,
• Litho tsa kelello: amblyopia, ho senyeha ha pono, diplopia,
• Tse ling: mokhathala, ho opeloa ke hlooho, feberu, edema ea sefahleho, asthenic syndrome, tšoaetso ea vaerase, ho nona ka boima ba mmele, edema ea potoloho.

Ha ho bapisoa mamello ea Convalis ho tekanyetso ea 300 le ea 3600 mg / ka letsatsi, ho ne ho bonoa tekanyo ea tebello ea liketsahalo tse kang ho otsela, ataxia, kizungu, nystagmus le paresthesia.

Boemong ba ho ngolisa ka mor'a ts'ebeliso, ho bile le liketsahalo tsa lefu la tšohanyetso le sa hlalosoang le sa amaneng le kalafo ea gabapentin.

Nakong ea kalafo le lithethefatsi, ho ka ba le litlamorao tse latelang tse sa rateheng: ho se sebetse hantle ha real, ho kula, ho senyeha ha sebete le / kapa manyeme, gynecomastia, keketseho ea bophahamo ba mammary gland, mathata a motor (dystonia, dyskinesia, myoclonus). urination, tinnitus.

Kamora ho khaotsa kalafo ka matla, ketsahalo e atisang ho etsahala khafetsa e kang: ho nyekeloa ke pelo, ho hloka boroko, ho utloisa bohloko bo fapaneng ba lehae, ho tšoenyeha, ho fufuleloa.

Haeba u ba le matšoao a mang a kaholimo kapa litla-morao tse ling, o lokela ho bona ngaka ea hau.

Ka overdose ea Convalis, lets'ollo, khathatso ea lipuo, diplopia, kizungu, dysarthria, ho otsela ho ile ha bonoa. Nakong ea liteko ho litoeba le likhoto, lethal dose e bolaeang ea gabapentin, e nkuoeng ka molomo, e ne e le litekanyetso tsa 8000 mg / kg. Matšoao a chefo e matla liphoofolong a bontšitsoe ho ataxia, ho hema hanyane, ptosis, hypoactivity kapa ho tsofala.

Phekolo ea overdose ke letšoao, hemodialysis e kanna ea fuoa bakuli ba nang le bothata bo matla ba ho lemala.

Sebopeho le mofuta oa tokollo

Sehlopha sa Clinical le pharmacological: lithethefatsi tsa anticonvulsant.

Sebaka se sebetsang sa gabapentin se tšoana ka sebopeho sa neurotransmitter GABA, empa e fapana le eona ka ts'ebetsong ea ts'ebetso, ha e na thepa ea GABAergic, mme ha e ame metabolism le ho ts'oaroa ha GABA. Sesebelisoa se na le phello e sebetsang ea anticonvulsant mme se bonts'a thepa ea mahlahahlaha, e eketsa bokhoni ba mmele ba ho ikamahanya le maemo.

Setlhare se fumaneha ka mokhoa oa li-capsules tsa "yellowatin". Ka hare ho na phofo (e tšoeu). Ntho ea mantlha ea sebopeho ke gabapentin ka tekanyetso ea 300 mg.

Hobaneng ha Convalis a abetsoe?

Joalokaha ho bontšitsoe ka litaelo tsa Convalis, meriana ena ea anticonvulsant e laetsoe kalafo ea:

• ka lefu la sethoathoa ho batho ba baholo le bana ba lilemo tse 12 e le karolo ea kalafo e felletseng kapa e le sesebelisoa se ikemetseng.
• bakeng sa kalafo ea bohloko ba neuropathic,
• ka ho ts'oaroa ha sethoathoa ka kakaretso general.

Ketso ea pharmacological

Ntho e sebetsang ea Convalis e na le phello ea anticonvulsant. Ntle le moo, Konvalis, ho ea ka litaelo, o na le phello ea melemo, e amanang le keketseho ea bokhoni ba mmele ba ho sebetsa. Moriba o na le phello e leka-lekaneng ea ho hlapoloha maemong a polyneuropathies, mme molemo oa ona ho lithethefatsi tse ling ka ts'ebetso e ts'oanang ea ts'ireletso ke polokeho e lekanyelitsoeng.

Bokhachane le pelehi

Ha ho na lintlha tse lekaneng mabapi le ts'ebeliso ea gabapentin ho basali baimana.Setlhare ha sea lokela ho sebelisoa nakong ea kemaro haeba phaello e ka ba teng ho mme e sa fetise kotsi e ka bang teng ho lesea.

Lithethefatsi li fetela lebese la matsoele, hore na phello ea bana nakong ea letsoele ha e tsejoe, ka hona, nakong ea kanyeso, moriana o lokela ho sebelisoa feela haeba phaello e ka ba teng ho mme ho nka moriana ka mokhoa o hlakileng e feta kotsi e ka bang teng ho lesea.

Meetso ea sebopeho (ke., E sebetsang,) ea Convalis ke Gabagamma, Gapentek, Gabapentin, Katena, Lepsitin, Neurontin, Tebantin, Egipentin, Eplirintin.

Theko e tloaelehileng ea CONVALIS lihoebi (Moscow) ke li-ruble tse 450.

Ho sebelisana le lithethefatsi

Ka tšebeliso e kopaneng ea Convalis e nang le lithethefatsi tse ling, litlamorao tse latelang li ka hlaha (AUC - kakaretso ea ntho ka plasma ea mali, C_max - Kakaretso ea ntho e maling.)

• Li-antacid tse nang le aluminium kapa magnesium: bioavailability e fokotsitsoeng ea gabapentin (nako e ka bang bonyane lihora tse 2 lipakeng tsa tekanyetso e lokela ho bonoa),
• Morphine (ha u nka morphine lihora tse 2 pele u nka Convalis): keketseho ea AUC ea gabapentin ka 44% (ha e bapisoa le monotherapy le gabapentin),
• Cimetidine: Ho fokotseha hanyane ho sesupo sa chess ea gabapentin,
• Ethanol le lithethefatsi tse sebetsang tsamaisong ea methapo ea kutlo: litlamorao tse eketsehang tsa gabapentin ho tsoa ho tsamaiso ea methapo e bohareng,
• Naproxen: ho amoheloa ha gabapentin,
• Hydrocodone: AUC ea gabapentin e ile ea fokotsa AUC le C_max hydrocodone.

Convalis analogues ke: Algerica, Gerolamic, Lamictal, Normeg, Lamitril, Latrigil, Topiramin, levetiracetam, Levitsit, Lyric, Epimil, Topilex, Neogabin, Topamax, Topilepsin, Epileptal, Epiramat, Epitrigin, Wimpatin, Lampatin, Lampatin, Lampatin Gabagamma, Gabantin, Grimodin, Neuralgin, Tebantin, Gabalept, Gabapentin, Gabalept, Meditan, Newropentin, Neurontin, Catena.

Sebopeho ka motsotsoana o le mong:

ntho e sebetsang: gabapentin - 300.0 mg
Baeti: lactose monohydrate - 66.0 mg, sehokelo sa poone ea pregelatinized - 30.0 mg, talc - 3.0 mg, magnesium stearate - 1.0 mg.
Boholo ba se kahare sa khase ke 400.0 mg.
Sebopeho sa khetla ea Capsule
Li-capsules tsa gelatin tse thata No. 0 - 96.0 mg.
Bolulo le sekoaelo: titanium dioksidi (E 171) - 2.0000%, dae oxide e sootho (E 172) - 0,6286%, gelatin - ho fihla 100%.
Boima kaofela ba capsule e nang le se ka har'a eona ke 496.0 mg.

Sehlopha sa Pharmacotherapeutic: lithethefatsi antiepileptic.

Khoutu ea ATX: N03AX12.

Melemo ea pharmacological

Mofumahali
Sebopeho sa lik'hemik'hale sa gabapentin se tšoana le sebopeho sa GABA neurotransmitter (gamma-aminobutyric acid), empa ts'ebetso ea ts'ebetso e fapana le lintho tse ling tse sebetsang tse sebetsanang le li-synapses tsa GABA, joalo ka li-valproates, barbiturates, benzodiazepines, GABA transaminase inhibitors, GABA reuptake inhibitors, and GABA agabists and GABA Lihlahisoa tsa meriana ea GABA. Lithutong in vitro Ka radioisotope gabapentin e ngotsoeng, libaka tse ncha tsa ho tlama liprotheine li fumanoe bokong ba rat, ho kenyeletsoa neocortex le hippocampus, tse ka amanang le ts'ebetso ea anticonvulsant le analgesic ea gabapentin le lits'oants'o tsa eona. Ho ile ha fumaneha hore sebaka se kopanyang sa gabapentin ke setsi sa vene-2-δ (alpha-2-delta) se secha sa li-channels tsa calcium-gated calcium.
Likarolong tse kholo tsa kliniki, gabapentin ha e tlamele ho li-receptor tse ling tse tloaelehileng tsa lithethefatsi le li-neurotransmitters tse teng bokong, ho kenyeletsoa le GABA_AGABA_Ho, benzodiazepine, glutamate, glycine le N-methyl-D-aspartate receptors.
Gabapentin maemong in vitro ha e sebelisane le liteishene tsa sodium, e e khethollang ho phenytoin le carbamazepine. Likarolong tse 'maloa tsa liteko in vitro ts'ebeliso ea gabapentin e lebisitse ho fokotseha ho se nang karabelo karabong ea glutamate agonist N-methyl-D-aspartate (NMDA), empa ke feela molemong oa mahloriso o fetang 100 μmol / L, o sa fumaneheng tlasa maemo ho vivo. Maemong in vitro ts'ebeliso ea gabapentin e lebisa ho fokotseha hanyane ha tokollo ea li-neurotransmitters tsa monoamine.
Mokhoa o nepahetseng oa ts'ebetso ea gabapentin ha o tsejoe.

Mofumahali
Suction
Kamora ho tsamaisoa ka molomo, boholo bo phahameng ba gabapentin ka plasma ea mali bo fihlella ka nako ea lihora tse 2-3. The bioavailability ea gabapentin e sekamela ho fokotseha ka tekanyetso e ntseng e eketseha. Boaoavailability e phethahetseng ha u nka li-capsules tsa 300 mg ke hoo e ka bang 60%. Lijo, ho kenyelletsa le tse nang le mafura a mangata, ha li na phello e kholo litabeng tsa pharmacokinetics ea gabapentin.
Pharmacokinetics ea gabapentin ha e fetohe ka ho pheta-pheta ha lithethefatsi.
Tsamaiso
Gabapentin ha e tlamele liprotheine tsa plasma, mme bophahamo ba eona ba tlhahiso ke li-lithane tse 57,7. Ho bakuli ba nang le lefu la ho akheha, mokokotlo oa mokokotlo oa mokokotlo oa mokokotlo oa mokokotlo oa mokokotlo oa mokokotlo oa mokokotlo (CSF) ke hoo e ka bang 20% ​​ea mahlahana a plasma a leka-lekaneng. Gabapentin e epuoa ka lebese la matsoele.
Biotransformation
Ha ho na data ea metabolism ea gabapentin 'meleng oa motho. Gabapentin ha e khothalletse ho kenngoa ha li-oxidase tse sa ikhethang tse ikarabellang bakeng sa metabolism ea lithethefatsi.
Ho tsala
Gabapentin e hlahisoa e sa fetohe feela ka ho hlaba makhopho. Bophelo ba halofo ea gabapentin bo ikemetse ka tekanyetso ea tekanyetso le makhetlo a 5 ho isa ho a 7.
Ho batho ba tsofetseng le bakuli ba nang le ts'ebetso ea renal e holofetseng, tumello ea gabapentin ho plasma ea mali e fokotsehile. Ho felisoa khafetsa, ho hlakisoa ha plasma le ho hlakisoa ha renal ea gabapentin ho tšoana ka kotloloho ho tumellano ea creatinine.
Gabapentin e tlosoa ka plasma ea mali nakong ea hemodialysis. Bakuli ba nang le ts'ebetso ea renal e holofetseng kapa ba nang le hemodialysis ba eletsoa hore ba fetole tekanyetso ea lithethefatsi (bona karolo "Karolo le Tsamaiso").
Linearity / nonlinearity ea paramente ea pharmacokinetics
Tekanyo ea bioavailability ea gabapentin e fokotseha ka tekanyetso e ntseng e eketseha, e kenyang lintlha tse sa amaneng le litekanyetso tsa pharmacokinetic, tse kenyelletsang index ea bioavailability (F), ka mohlala, Ae%, CL / F, Vd / F. Elimination pharmacokinetics (paramente ha e kenyeletse F, joalo ka CLr le T_1/2) e hlalosoa hantle ho latela mohlala. Tekanyetso ea plasma ea equilibrium e lekantsoeng e ka ipapisa le data ea kinetics ka lethal dose e le 'ngoe.

Sebelisa nakong ea bokhachane le nakong ea ho anyesa

Kotsi e akaretsang ka lebaka la lefu la sethoathoa le lithethefatsi tsa antiepileptic
Kotsi ea ho ba le bana ba nang le anomalies ea tlhaho ea tlhaho ho bo-mme ba tšoaroang ka li-anticonvulsants bakeng sa lefu la sethoathoa bo eketseha ka makhetlo a 2-3. Hangata ho ba le leruarua la molomo o holimo le mahalapa, ho se sebetse hantle ha tsamaiso ea pelo le methapo ea methapo ea methapo ea methapo. Ho feta moo, ho nka li-anticonvulsants tse 'maloa ho ka amahanngoa le kotsi e kholo ea ho ba le bofokoli ho feta tabeng ea monotherapy. Ka hona, haeba ho khonahala, e 'ngoe ea li-anticonvulsants e lokela ho sebelisoa. Basali ba lilemo tsa ho ba le bana, hammoho le basali bohle bao e ka bang baimana, ba lokela ho botsa setsebi se tšoanelehang. Haeba mosali a rera ho ima, tlhoko ea ho tsoela pele ka kalafo ea anticonvulsant e lokela ho hlahlojoa hape. Ka nako e ts'oanang, li-anticonvulsants ha lia lokela ho felisoa ka tšohanyetso, kaha sena se ka lebisa ho qalella ho ts'oaroa ka litlamorao tse mpe ho mme le ngoana. Maemong a sa tloaelehang, ho bana bao bo-'mè ba nang le lefu la sethoathoa, ho lieha ha nts'etsopele ho ile ha bonoa. Leha ho le joalo, ho ke ke ha khoneha ho tseba hore na ho lieha ho hola ho amana le liphatsa tsa lefutso kapa tsa sechaba, bokuli ba bo-mme kapa kalafo ea anticonvulsant.

Kotsi ea Gabapentin
Ha ho na data ea ts'ebeliso ea lithethefatsi ho basali baimana. Litekong tsa liphoofolo, ho pepesetsoa ha chefo ea motsoako ho "fetus". Mabapi le kotsi e ka bang teng, batho ha ba na datha. Ka hona, gabapentin e lokela ho sebelisoa nakong ea kemolo ha feela phaello e reriloeng ho mme e lokafatsa kotsi e ka bang teng ho lesea.
Maemong a tlalehiloeng, ho ke ke ha khoneha ho bolela ka mokhoa o hlakileng hore na ts'ebeliso ea gabapentin nakong ea kemolo e tsamaea le kotsi e kholo ea ho se sebetse hantle, pele, ka lebaka la ho ba teng ha lefu la sethoathoa ka bo bona, 'me ea bobeli, ka lebaka la ts'ebeliso ea li-anticonvulsants tse ling. .
Ho anyesa
Gabapentin e pepesitsoe lebese la matsoele, hore na phello ea eona ho lesea e anyesang ha e tsejoe, ka hona, nakong ea ho anyesa Convalis ® e lokela ho fuoa feela haeba melemo ho mme e pepesa kotsi ea lesea.
Lithuto tsa liphoofolo ha lia ka tsa hlokomela litlamorao tsa gabapentin ho tsoalo.

Tekanyetso le tsamaiso

Convalis ® e laetsoe ka molomo ho sa tsotelehe takatso ea lijo. Haeba ho hlokahala ho fokotsa tekanyetso, hlakola sethethefatsi sena kapa u se emise ka moemeli ea mong, sena se lokela ho etsoa butle butle ka nako e fetang beke.
Mahlaba a neuropathic ho batho ba baholo
Motsoako oa pele ke 900 mg / ka letsatsi ho litekanyetso tse tharo tse arohaneng, haeba ho hlokahala, ho latela phello, lethalinyana le eketseha hanyane ka hanyane ho isa ho 3600 mg / ka letsatsi. Phekolo e ka qala hanghang ka tekanyetso ea 900 mg / ka letsatsi (makhetlo a 300 mg makhetlo a 3 ka letsatsi) kapa lethal dose le ka eketseha butle butle ho isa ho 900 mg ka letsatsi bakeng sa matsatsi a 3 a pele ho latela morero o latelang:
Letsatsi la 1: 300 mg ea moriana nako e le ngoe ka letsatsi,
Letsatsi la bobeli: 300 mg ea moriana makhetlo a 2 ka letsatsi,
Letsatsi la 3: 300 mg ea moriana makhetlo a 3 ka letsatsi.
Metsoako e meng
Ka lefu la sethoathoa, hangata ho hlokahala kalafo e telele. Tekanyetso ea moriana e khethoa ke ngaka e eang ho latela ho mamella le katleho ea moriana ka mong.
Batho ba baholo le bana ba ka holimo ho lilemo tse 12: tekanyetso e sebetsang - ho tloha 900 ho isa ho 3600 mg / ka letsatsi. Phekolo e ka qala ka lethal dose ea makhetlo a 300 mg makhetlo a 3 ka letsatsi ka letsatsi la pele kapa butle-butle ea eketseha ho ea ho 900 mg ho latela sesebelisoa se hlalositsoeng ka holimo (bona karolana "Leuropathic pain ho batho ba baholo"). Kamora moo, lethalinyana le ka eketsoa ho fihla ho 3600 mg / ka letsatsi (le arotsoe ka litekanyetso tse 3 tse lekanang). Mamello e ntle ea lithethefatsi ho tekanyetso ho fihlela ho 4800 mg / ka letsatsi e ile ea bonoa. Nako e phahameng lipakeng tsa litekanyetso ka tekanyetso ea makhetlo a mararo ea lithethefatsi ha ea lokela ho feta lihora tse 12 ho qoba ho ts'oaroa hape.
Bakuli ba matla
Ho bakuli ba maemong a tebileng, ho etsa mohlala, haeba ho fokotsoa boima ba 'mele, kamora ho fetisoa ha litho, joalo-joalo, lethal dose le lokela ho eketseha butle butle, ekaba ho sebelisa litekanyetso tse tlase kapa ka ho etsa nako e telele pele o eketsa tekanyetso.
Sebelisa ho bakuli ba tsofetseng (ba fetang lilemo tse 65)
Ka lebaka la ho fokotseha ho amanang le lilemo tsa ts'ebetso ea liphio, bakuli ba tsofetseng ba ka hloka phetoho ea litekanyetso (ho fumana lintlha tse ling, bona Lethathamo 1). Ho otsela, edema ea asipia le asthenia ho bakuli ba tsofetseng li ka hlaha khafetsa.
Khetho ea moriana bakeng sa ho hloleha ha liphio
Bakeng sa bakuli ba nang le ho se sebetse hantle ke mokokotlo, ho khothaletsoa ho fokotsa tekanyo ea gabapentin ho latela tafole ea 1:

A - tekanyetso ea letsatsi le letsatsi e lokela ho fuoa meriana e meraro,
B - khetha 300 mg letsatsi le leng le le leng,
B - ho bakuli ba nang le tumello ea creatinine ®. Ho tseba protheine ka har'a morara, ho kgothaletswa ho sebelisa mokhoa o ikhethang oa ho chona le sulfosalicylic acid.
Phello ea CNS
Nakong ea kalafo ea gabapentin, ho bile le maemo a ho tsekela le ho otsela, tse ka eketsang monyetla oa ho lemala ka phoso (haeba o akhehile). Nakong ea ho ngolisoa ka mor'a moo, linyeoe tsa pherekano, ho lahleheloa ke tsebo le ts'ebetso ea kelello e sa sebetseng le tsona li tlalehiloe. Ka hona, bakuli ba lokela ho eletsoa ho ba hlokolosi ho fihlela ba tseba ka litlamorao tsa lithethefatsi tsena.
Ka tšebeliso e le 'ngoe le li-analgesics tsa opioid, ho ka bonoa keketseho ea khatello ea "gabapentin" ka plasma ea mali. Mabapi le sena, mokuli o hloka ho hlahlojoa ka hloko bakeng sa nts'etsopele ea matšoao a khatello ea methapo ea methapo, joalo ka ho otsela, ho tetebela le khatello ea maikutlo. Litekanyetso tsa gabapentin kapa opioid analgesics li lokela ho fokotsoa.
Ts'ebetso ea kopanelo le li-antacid
Gabapentin e khothalletsoa hore e nkuoe kamora lihora tse peli kamora ho nka antacid.

Tšusumetso ho bokhoni ba ho khanna makoloi le mekhoa

Ha u ntse u sebelisa lithethefatsi, bakuli ha ba khothaletsoe ho khanna makoloi kapa ho sebelisa lisebelisoa tse ka bang kotsi ho fihlela ho ba le phello e mpe ea lithethefatsi ts'ebetsong ea mesebetsi ena.
Gabapentin e ama tsamaiso ea methapo e bohareng mme e ka baka tsitsipano, ho otsela, pherekano, ho felloa ke kelello, kapa matšoao a mang a tsamaiso ea methapo e kholo. Le ha e le ka botebo kapa ka tekano e fokolang, litlamorao tsena tse sa rateheng li ka ba kotsi ho bakuli ba khannang likoloi kapa mechini e meng. Monyetla ona o hantle haholo qalong ea kalafo kapa kamora ho eketsa tekanyetso ea gabapentin.