Ihe ọmụma
Pregabalin ntụ ntụ, ọgwụ siri ike nke a na-ejikarị agwọ ọrịa neuropathic mgbu, Akwụkwụ na-adọ, na nsogbu nchekasị zuru oke, enwetala nlebara anya dị ukwuu na mpaghara ahụike n'ihi usoro pụrụ iche nke ime ihe n'ime usoro ụjọ ahụ. Edemede a na-abanye n'ime ọrụ mgbagwoju anya nke pregabalin ntụ ntụ, na-enyocha mmetụta ya na ndị na-ahụ maka ndị na-ahụ maka ndị na-ahụ maka ụbụrụ, ọwa calcium, na ọrụ ụbụrụ zuru ezu iji nye nghọta zuru oke banyere uru ọgwụgwọ ya.
Kedu ihe bụ isi ojiji pregabalin ntụ ntụ?
Pregabalin ntụ ntụ, nke a na-ere n'okpuru aha aha dị iche iche gụnyere Lyrica, egosila na ọ bụ ọgwụ dịgasị iche iche nwere ọtụtụ ngwa ụlọ ọgwụ. Ojiji ya bụ isi gụnyere akụkụ atọ bụ isi: njikwa mgbu neuropathic, ọgwụgwọ epilepsy, na ọgwụgwọ nchekasị.
N'akụkụ nchịkwa mgbu neuropathic, pregabalin egosila ịdị irè dị ịrịba ama n'ibelata ahụ erughị ala metụtara ọnọdụ ndị dị ka ọrịa neuropathy mamịrị, postherpetic neuralgia, na fibromyalgia. Ikike ya iji gbanwee ihe mgbaàmà mgbu n'ime usoro ụjọ ahụ na-eme ka ọ bụrụ ngwá ọrụ bara uru maka ndị ọrịa na-alụ ọgụ na-adịghị ala ala nke na-eguzogidekarị ọgwụ analgesics.
Maka ọgwụgwọ akwụkwụ, pregabalin na-eje ozi dị ka ọgwụgwọ mgbakwunye maka ọdịdọ akụkụ akụkụ na ndị okenye. Ngwongwo ya na-egbochi convulsant na-enyere aka ibelata ugboro na ike nke ọdịdọ, na-enye ndụ ka mma maka ndị nwere ọrịa Akwụkwụ. Ikike nke ọgwụ ahụ iji kwụsie ike nke neuronal excitability na-atụnye aka na ịdị irè ya na njikwa ọdịdọ.
N'ihe gbasara nsogbu nchekasị, pregabalin egosipụtala uru dị ukwuu na ijikwa nsogbu nchekasị zuru oke (GAD). Mmetụta anxiolytic ya sitere na mmetụta ya na sistemụ neurotransmitter na-etinye aka na nhazi nchekasị. Site n'ịgbanwe usoro ndị a, pregabalin na-enyere aka belata oke nchekasị, enweghị nchekasị, na mgbaàmà ndị ọzọ metụtara GAD.
E wezụga ihe ngosi ndị a bụ isi, pregabalin egosila nkwa na ojiji a na-ejighị n'aka, gụnyere ọgwụgwọ mmanya na iwepụ benzodiazepine, ọrịa ụkwụ na-adịghị ike, na ụfọdụ ụdị mgbu na-adịghị ala ala na-ejikọtaghị ya na neuropathy. Agbanyeghị, ọ dị mkpa iburu n'obi na ojiji ndị a na-enweghị akara ga-atụle naanị n'okpuru nduzi nke ọkachamara ahụike.
The versatility nke pregabalin ntụ ntụ n'ịgbasa ọtụtụ ọrịa akwara ozi na ọnọdụ uche na-egosi mkpa ọ dị na ọgwụ ọgbara ọhụrụ. Usoro ihe omume ya pụrụ iche, nke anyị ga-enyocha n'ụzọ zuru ezu na ngalaba ndị a, na-enye ya ohere ilekwasị anya n'ọtụtụ akụkụ nke ọrụ akwara ozi, na-eme ka ọ bụrụ ngwá ọrụ bara uru n'ịgwọ ọrịa nhụjuanya dị mgbagwoju anya.
Kedu ka pregabalin si emetụta ntọhapụ neurotransmitter?
Mmetụta Pregabalin na ntọhapụ neurotransmitter bụ akụkụ dị mkpa nke usoro ya n'ime usoro ụjọ ahụ. Ọ bụ ezie na ọ naghị ejikọta ya na ndị na-anabata GABA ma ọ bụ gbanwee mkpokọta GABA, mmetụta ya na ntọhapụ neurotransmitter dị ịrịba ama na ọtụtụ akụkụ.
Usoro izizi nke pregabalin na-emetụta ntọhapụ neurotransmitter bụ site na njikọ ya na mpaghara α2δ nke chanel calcium voltaji. Ọwa ndị a na-arụ ọrụ dị oke egwu na ntọhapụ nke neurotransmitters na synapses na usoro ụjọ ahụ dum. Site na ijikọ na subunit α2δ, pregabalin na-ebelata ntinye nke calcium n'ime neurons, nke na-eduga n'ịbelata ntọhapụ nke ọtụtụ neurotransmitters na-akpali akpali.
Ndị neurotransmitters kacha emetụta ihe omume pregabalin na-agụnye glutamate, norepinephrine, na ihe P. Glutamate, bụ isi ihe na-akpali akpali neurotransmitter na usoro nhụjuanya nke etiti, dị mkpa karịsịa n'ihe gbasara mgbaàmà mgbu na nhụjuanya neuronal. Site na ibelata ntọhapụ glutamate, pregabalin na-enyere aka belata oke ọgbụgba neuronal metụtara mgbu na ọdịdọ neuropathic.
Norepinephrine, neurotransmitter ọzọ nke pregabalin na-emetụta, na-arụ ọrụ dị mkpa na nzaghachi nrụgide nke ahụ yana ọ na-etinye aka na nsogbu nchekasị. Mbelata ntọhapụ norepinephrine na-enye aka na mmetụta anxiolytic nke pregabalin, na-enyere aka belata mgbaàmà nke nsogbu nchekasị zuru oke.
Ihe P, neuropeptide na-etinye aka na mgbaàmà mgbu, na-emetụtakwa ihe omume pregabalin na ọwa calcium. Mbelata ntọhapụ nke ihe P na-enye aka na mmetụta analgesic nke ọgwụ ahụ, karịsịa n'ihe gbasara mgbu neuropathic.
Ọ dị mkpa ịmara na mgbe ahụ Pregabalin ntụ ntụ na-ebelata ntọhapụ nke ndị neurotransmitters na-akpali akpali, ọ naghị egbochi ntọhapụ ha kpamkpam. Kama nke ahụ, ọ na-emezi ntọhapụ ha, na-enyere aka iweghachi ọnọdụ nguzozi nke ọrụ neuronal. Mgbanwe a, kama igbochi mmechi zuru oke, bụ akụkụ nke ihe na-eme ka pregabalin dị irè ma na-ebelata mmetụta ndị nwere ike ime na njedebe neurotransmitter zuru oke.
Ọzọkwa, mmetụta pregabalin na mwepụta neurotransmitter abụghị otu n'ofe sekit akwara niile. Ọgwụ ahụ na-egosi na ọ na-enwe mmetụta dị ukwuu na neurons hyperexcited, dị ka ndị na-etinye aka na ọnọdụ mgbu na-adịghị ala ala ma ọ bụ Akwụkwụ na-adọ, ebe ọ na-enwe mmetụta dị nta na ọrụ ụbụrụ nkịtị. Nhọrọ a na-enye aka na ọgwụgwọ ọgwụgwọ ya na profaịlụ mmetụta dị mma ma e jiri ya tụnyere ụfọdụ ọgwụ ndị ọzọ ejiri maka ọnọdụ ndị yiri ya.
Mkparịta ụka dị mgbagwoju anya n'etiti njikọ pregabalin na ọwa calcium na mmetụta ya na-esote na mwepụta neurotransmitter na-adabere na ngwa ọgwụgwọ ya dị iche iche. Site n'ịgbanwe ntọhapụ nke isi ihe na-akpali akpali neurotransmitters, pregabalin na-enyere aka iweghachi nguzozi na sekit akwara mebiri site na ọnọdụ ndị dị ka mgbu neuropathic mgbu, Akwụkwụ na-adọ, na nsogbu nchekasị.
Kedu ọrụ ọwa calcium na-arụ na usoro pregabalin si arụ ọrụ?
Ọwa Calcium na-arụ ọrụ dị mkpa na usoro pregabalin si eme ihe, na-eje ozi dị ka ebumnuche izizi nke ọgwụ na-egosipụta mmetụta ọgwụgwọ ya. Ịghọta mmekọrịta dị n'etiti pregabalin na ọwa ndị a dị oke mkpa iji ghọta otú ọgwụ ahụ si emetụta ọrụ akwara ma na-enye ahụ efe maka ọnọdụ ahụike dị iche iche na ọrịa uche.
Ọwa calcium voltaji-gated bụ protein akpụkpọ anụ nke na-enye ohere ntinye nke ion calcium n'ime sel na nzaghachi maka mgbanwe nke ike akpụkpọ ahụ. Na neurons, ọwa ndị a dị mkpa karịsịa maka ọtụtụ usoro, gụnyere ntọhapụ neurotransmitter, okwu mkpụrụ ndụ ihe nketa, na nhazi nke excitability neuronal. Akụkụ α2δ, nke pregabalin na-ejikọta, bụ protein inyeaka jikọtara ya na ọwa ndị a ma na-arụ ọrụ dị mkpa na ọrụ ha na ịzụ ahịa na akpụkpọ ahụ.
Njikọ dị elu nke Pregabalin na-ejikọta ya na mpaghara α2δ, kpọmkwem α2δ-1 na α2δ-2 isoforms, na-ebute mbelata nke calcium na-abanye na neurons. Mbelata a na-esite na usoro abụọ bụ isi:
1. Mbelata ịzụ ahịa ọwa: Pregabalin ntụ ntụ na-egbochi ịzụ ahịa nkịtị nke ọwa calcium n'elu cell. Site na ijikọ na mpaghara α2δ, ọ na-ebelata ọnụ ọgụgụ ọwa calcium na-arụ ọrụ dị na ọdụ synapti.
2. Kinetics ọwa gbanwere: Njikọ nke pregabalin na α2δ subunit nwekwara ike imetụta mmeghe na mmechi kinetics nke ọwa calcium, na-ebelata ntinye nke calcium.
Nsonaazụ nke mbelata calcium ntuba nke a na-erute ma na-ebute ọtụtụ n'ime mmetụta ọgwụgwọ pregabalin:
1. Mbelata ntọhapụ neurotransmitter: Dị ka a tụlere na ngalaba nke gara aga, mbelata nrịba nke calcium na-eduga na mbelata ntọhapụ nke neurotransmitters na-akpali akpali dị ka glutamate, norepinephrine, na ihe P.
2. Mbelata nke neuronal excitability: Site n'ịkwụsị ntinye calcium, pregabalin na-enyere aka mee ka njedebe nke neurons zuru ezu, bụ nke bara uru karịsịa na ọnọdụ nke hyperexcitability, dị ka epilepsy na neuropathic mgbu.
3. Mgbanwe nke synapti plasticity: Calcium na-arụ ọrụ dị mkpa na synapti plasticity, ikike nke synapses iji wusie ma ọ bụ daa mbà ka oge na-aga. Site n'ịgbanwe mmụba nke calcium, pregabalin nwere ike imetụta mgbanwe ogologo oge na sekit akwara, nwere ike inye aka na mmetụta ọgwụgwọ ya na-adịgide adịgide.
4. Neuroprotection: Mbubata calcium nke ukwuu nwere ike ịbụ neurotoxic. Site na ịmachi ntinye calcium, pregabalin nwere ike inye ụfọdụ mmetụta neuroprotective, ọ bụ ezie na akụkụ a chọrọ nyocha ọzọ.
Ọ dị mkpa iburu n'obi na mmetụta pregabalin na ọwa calcium na-adabere na steeti, nke pụtara na a na-akpọkarị ha na neurons hyperexcited. Nhọrọ a na-enye aka na nrụpụta ya n'ịgwọ ọnọdụ ndị e ji mara hyperexcitability neuronal ma na-ebelata mmetụta na ọrụ ụbụrụ nkịtị.
Ọrụ nke ọwa calcium na usoro pregabalin si eme ihe na-agafe karịa ntọhapụ neurotransmitter. Mgbanwe nke ọwa ndị a na-emetụta akụkụ dị iche iche nke ọrụ neuronal, site na nnyefe mgbaàmà na mgbanwe ogologo oge na sekit akwara. Mmetụta a sara mbara na physiology neuronal na-akọwa nrụpụta pregabalin n'ofe ọnọdụ akwara ozi na ọnọdụ uche, site na mgbu neuropathic ruo nsogbu nchekasị.
Ọzọkwa, ebumnuche akọwapụtara nke subunit α2δ site na pregabalin na-anọchite anya ụzọ pụrụ iche na ọgwụ ọgwụ. N'adịghị ka ọgwụ ndị na-elekwasị anya na sistemu neurotransmitter ozugbo, mgbanwe pregabalin nke ọwa calcium na-enye ohere maka usoro nhazi nke ọrụ akwara. Usoro a na-ebutekarị nguzozi dị mma n'etiti nrụpụta na mmetụta ndị dị na ya, na-eme ka pregabalin bụrụ nhọrọ bara uru n'ịgwọ ọrịa dị iche iche nke akwara ozi.
Na mmechi, mkparịta ụka dị mgbagwoju anya dị n'etiti pregabalin na ọwa calcium voltaji, nke etinyere na mpaghara α2δ, bụ isi nkuku nke usoro ọgwụgwọ ya. Site n'ịgbanwe ọwa ndị a, Na-aga n'ihu Powuru na-emetụta ọtụtụ akụkụ nke ọrụ akwara ozi, na-enye ahụ efe maka ọnọdụ dị iche iche nke akwara ozi na ọnọdụ uche. Ka nyocha na-aga n'ihu, nghọta anyị nwere maka usoro a nwere ike iduga n'ụzọ ndị ọzọ nụchara anụcha maka ịgwọ nsogbu nke sistem ụjọ.
Ọ bụrụ na ị nwekwara mmasị na ngwaahịa a ma chọọ ịmatakwu nkọwa ngwaahịa, ma ọ bụ chọọ ịmata maka ngwaahịa ndị ọzọ metụtara, biko nweere onwe gị ịkpọtụrụ. iceyqiang@aliyun.com.
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