Gabapentin - cov lus qhia rau kev siv thiab tshuaj xyuas

Kev piav qhia cuam tshuam rau 04.02.2015

• Lub npe Latin: Gabapentin
• ATX Code: N03AX12
• Yam tshuaj muaj sia: Gabapentin
• Chaw tsim tshuaj paus: PIK-PHARMA, Canonfarm Ntau Lawm CJSC (Russia), Aurobindo Pharma (Is Nrias teb), Erregierre S.p.A. (Ltalis)

Hauv 1 tshuaj ntsiav - gabapentin 300 mg

Calcium hydrogen phosphate, qos hmoov txhuv nplej siab, macrogol, magnesium stearate - raws li cov neeg tau txais txiaj ntsig.

Kev ntsuas rau siv

• tshuaj mob hlwb focal chua leeg ntawm qaug dab peg rau cov laus thiab menyuam yaus txij 12 xyoos,
• kev kho mob ntxiv focal chua leeg nrog qaug dab peg hauv cov neeg laus,
• kev kho mob ntxiv tiv taus mob vwm nyob rau hauv cov menyuam yaus los ntawm 3 xyoo,
• mob taub hau,
• neuropathic mob (neuralgia postherpetic, mob ntshav qab zib, trigeminal, mob HIV, cawv, nrog mob txha caj qaum),
• qhov txo qis hauv kev siv ntau ntawm kev ntas thaum lub sijhawm lawm.

Cov Yuav Tsum Muaj

• ntse pancreatitis,
• hypersensitivity rau cov tshuaj,
• galactose intolerance lossis malabsorption ntawm qabzib thiab galactose,
• hnub nyoog txog li 3 xyoos nrog rau kev phom sij rau kev puas ntsoog,
• hnub nyoog txog li 12 xyoos nrog kev xaiv tom qab neuralgia,
• cev xeeb tub.

Sab sij huam

• nce HUAB TAIS, tachycardia,
• dyspepsia, xeev siab, mob plab, qhov ncauj qhuav, anorexia, cem quav lossis zawv plab, pancreatitis, flatulence, mob caj dab,
• myalgiarov qab mob
• tsaug zog, kiv taub hau, nystagmusnce nkeesthiab ua kom zoo siab, dysarthria, gtin mob, kev nyuaj siabtsis meej pem hyperkinesia,ntxhov siab, insomnia,
• rhinitis, pharyngitis, hnoos,
• zis tsis tu ncua, tsis hnov ​​qab potency,
• pom kev tsis taus, tinnitus,
• tawv nqaij ua pobexudative erythema,
• hnyav, lub ntsej muag o, o tuaj.

Kev sib txuam

Kev siv lwm cov tshuaj tiv thaiv kev mob ib txhij raug tso cai (Phenobarbital, Carbamazepine, Phenytoin, Valproic Acid) thiab tshuaj tiv thaiv qhov ncauj. Hauv qhov no, pharmacokinetics ntawm gabapentin tsis hloov pauv.

Antacids txo cov bioavailability ntawm cov tshuaj, yog li noj cov tshuaj tseem ceeb thiab antacids kis thaum lub sijhawm.

Myelotoxic tshuaj ntxiv rau hematotoxicity ntawm gabapentin.

Tau nrog morphine morphine pharmacokinetics tsis hloov pauv. Txawm li cas los xij, muaj kev phiv tshuaj los ntawm lub hauv nruab nrab ntawm lub paj hlwb yuav tsum tau saib xyuas.

Haus dej cawv tuaj yeem ua rau muaj kev phiv los ntawm cov hlab ntsha hauv nruab nrab (ataxia, stupor).

Cov lus qhia tshwj xeeb

Yog tias nws yuav tsum tau txiav tawm cov tshuaj, qhov kev txo qhov siab yuav tsum tau nqa tawm maj (hauv 1-2 lub lis piam), txij li kev ncua kev kho mob tuaj yeem ua rau tus mob epistatus. Thaum cev xeeb tub, nws raug tso cai siv raws li cov cim nruj me ntsis, thaum muaj txiaj ntsig rau leej niam tshaj qhov txaus ntshai rau tus me nyuam hauv plab.

Yog tias ataxia, kiv taub hau, hnyav, qaug zog yuav tshwm sim hauv cov neeg laus, thiab tsaug zog thiab ua yeeb ncuab hauv menyuam yaus, kev kho yuav tsum tsis ua ntxiv. Thaum kho, koj yuav tsum caiv tsis txhob tsav tsheb.

Daim ntawv tso tawm thiab cov qauv ntawm cov tshuaj

Gabapentin muaj nyob hauv daim ntawv tshuaj ntsiav rau txoj kev tswj hwm qhov ncauj. Cov tshuaj no tau ntim rau hauv hnab yas ntawm 50 lossis 100 pieces lossis hlwv ntawm 10-15 pieces hauv ib daim ntawv thawv.

Txhua lub tshuaj ntsiav muaj cov tshuaj nquag - gabapentin 300 mg, ntxiv rau tus naj npawb ntawm cov khoom siv pabcuam: calcium stearate, gelatin, titanium dioxide, microcrystalline cellulose.

Siv rau hauv kev xyaum kho mob

Gabapentin tau tsim tawm ntawm Parke-Davis thiab tau piav qhia thawj zaug xyoo 1975. Raws li Neurontin lub npe, nws tau pom zoo thawj zaug thaum Lub Tsib Hlis 1993 rau kev kho mob ntawm kev mob vwm ntawm lub teb chaws Askiv thiab tau muag hauv Tebchaws Asmeskas thaum xyoo 1994. Tom qab ntawd, gabapentin tau pom zoo nyob hauv Tebchaws Meskas los kho tus mob postherpetic neuralgia hauv lub Tsib Hlis 2002. Lub Ib Hlis 2011, Tebchaws Asmeskas pom zoo rau kev tso tshuaj uas tau tsim tawm gabapentin rau kev tswj hwm ib zaug ib hnub nyob rau hauv lub npe npe Gralise. Gabantine anacarbil nyob rau hauv lub npe lag luam Horizant, uas muaj lub cev siab zoo, tau qhia nyob rau hauv Tebchaws Asmeskas rau kev kho mob tsis tuaj yeem mob caj dab nyob rau lub Plaub Hlis 2011 thiab tau pom zoo rau kev kho mob ntawm postherpetic neuralgia thaum Lub Rau Hli 2012.

Siv rau hauv kev xyaum kho mob

Gabapentin tsuas yog siv los kho mob qaug dab peg thiab mob neuropathic. Qhov no tsuas yog tswj hwm los ntawm qhov ncauj, nrog kev tshawb fawb qhia tau tias "kev tswj hwm ntawm lub qhov quav tsis txaus siab." Nws tseem yog feem ntau tau sau tseg rau ntau daim ntawv thov uas tsis muaj cim, xws li kev kho mob ntawm kev ntxhov siab tsis xws luag, insomnia thiab bipolar tsis meej. Txawm li cas los xij, muaj kev txhawj xeeb txog qhov zoo ntawm cov kev ntsuas tau ua thiab cov pov thawj rau qee qhov kev siv, tshwj xeeb tshaj yog thaum siv los ua lub siab ntsws nyob rau hauv kev puas siab puas ntsws bipolar.

Pharmacological cov yam ntxwv ntawm cov tshuaj

Gabapentin yog ib qho tshuaj uas muaj cov nyhuv anticonvulsant. Hauv qab ntawm qhov tshuaj nyob rau hauv cov neeg mob qaug dab peg, nws txo txoj kev pheej hmoo ntawm kev tsim rov qab tawm tsam.

Cov tshuaj no yog siv rau kev kho mob rau cov neeg laus thiab menyuam yaus rau kev kho mob ntawm kev mob vwm thiab mob neuropathic mob tiv thaiv cov keeb kwm yav dhau los ntawm tus mob pob ntseg.

Cov Tshuaj Hauv Tshuaj

Hauv kev teeb tsa, gabapentin zoo ib yam li GABA neurotransmitter (gamma-aminobutyric acid), tab sis nws cov kev ua haujlwm txawv ntawm lwm cov tshuaj uas cuam tshuam nrog GABA receptors (valproic acid, barbiturates, benzodiazepines, GABA uptake inhibitors, GABA transaminase inhibitors, thiab agonists ntawm agonists ntawm agonists ntawm agonists GABA cov ntaub ntawv).

Gabapentin tsis muaj GABAergic lub zog thiab tsis cuam tshuam rau kev coj thiab metabolism ntawm GABA. Raws li kev tshawb fawb ua ntej, cov tshuaj khi rau α₂-δ-subunit ntawm voltage-dependant calcium channel thiab txo qhov khiav ntawm calcium ions, uas ua lub luag haujlwm tseem ceeb hauv kev txhim kho kev mob neuropathic.

Lwm cov kev ua ntawm kev ua rau mob neuropathic:

• nce zog ntawm GABA,
• txo qis hauv glutamate-kev tuag ntawm neurons,
• kev tsuj ntawm kev tso tawm ntawm neurotransmitters ntawm monoamine pawg.

Hauv cov chaw kuaj mob tseem ceeb ntawm gabapentin nrog receptors rau lwm yam tshuaj feem ntau los yog neurotransmitters, suav nrog GABA receptors_HauvGABA_A, glycine, glutamate, N-methyl-D-aspartate, lossis benzodiazepine receptors, tsis khi.

Gabapentin, tsis zoo li carbamazepine thiab phenytoin, tsis cuam tshuam nrog sodium channel hauv vitro. Thaum nyob rau hauv kev kho mob hauv vitro, qee qhov kev kuaj hauv cov vitro qhia pom ib nrab ntawm qhov tshwm sim ntawm glutamate receptor agonist N-methyl-D-aspartate, tab sis tsuas yog nyob rau hauv lub siab ntawm> 100 μmol, uas tsis tiav hauv vivo. Gabapentin me ntsis txo cov kev tso tawm ntawm monoamine neurotransmitters.

Cov Tshuaj Pharmacokinetics

Lub bioavailability ntawm gabapentin tsis yog koob tshuaj-nyob rau hauv qhov thiab txo nrog nce zuj zus. C_max (qhov siab tshaj plaws ntawm cov tshuaj) gabapentin hauv plasma tom qab kev tswj hwm ntawm qhov ncauj tau tiav hauv 2-3 teev. Kev tsis raug cai txog ntawm qhov tsis raug cai yog kwv yees li 60%. Khoom noj khoom haus, suav nrog cov roj ntau hauv lub cev, tsis cuam tshuam rau qhov tsis muaj pharmacokinetic.

Kev tshem tawm cov khoom ntawm cov ntshav tau zoo tshaj plaws yog siv cov qauv kab. T_1/2 (tshem tawm ib nrab-lub neej) los ntawm cov ntshav nruab nrab li 5-7 teev thiab tsis nyob ntawm qhov siab. Nrog kev siv tas li, cov tsis haum pharmacokinetic tsis hloov. Tus nqi ntawm qhov sib luag ntawm cov ntshav plhaws muaj peev xwm kwv yees tau raws li cov txiaj ntsig ntawm ib zaug ntawm cov tshuaj.

Gabapentin xyaum tsis khi rau cov roj ntsha plasma (80 - 900-2400 mg ib hnub,