Cov kab lus yuav nthuav qhia tus yam ntxwv ntawm imidazoline receptor agonists.
Tshuaj uas ua rau lub hauv paus tsis muaj zog ntawm kev tswj hwm lub plawv thiab cov hlab ntsha nyob hauv qhov chaw tseem ceeb ntawm cov tshuaj tiv thaiv kab mob niaj hnub no.
Tam sim no, qhov teeb meem ntawm kev txhim kho hauv nruab nrab cov tshuaj tiv thaiv kab mob ntshav siab raws li lub tswv yim ntawm imidazoline-type receptors yog tshuaj pleev. Plaub qhov kev xaiv imidazoline receptor agonists twb tau tsim. Cov tshuaj yog tsim nyob rau hauv ntau lub npe lag luam. Cov neeg sawv cev tseem ceeb ntawm pawg no yog moxonidine (Cint, Physiotens) thiab rilmenidine (Tenaxum, Albarel). Cov no yog cov tshuaj nrov tshaj plaws uas nyob rau hauv cov npe ntawm imidazoline receptor agonists.
Kev ua haujlwm tshwj xeeb thiab thaj chaw ntawm receptors
Receptorsimidazoline feem ntau muab faib ua ob pawg loj, hu ua I1 thiab I2.
Kev faib tawm, lawv lub ntsiab lus thiab cov yam ntxwv ua haujlwm ua lub hauv paus ntawm ntau yam kev tshawb fawb.
I1-receptors nyob rau hauv cov ntaub so ntswg neuronal ntawm lub hlwb, ob lub raum, cov hlwb ntawm cov khoom ntawm adrenal medulla, platelets thiab pancreas. Nws yog precisely nrog lub predominant receptor excitation ntawm hom no hais tias lub cawv ntawm niaj hnub antihypertensive tshuaj yog txuam nrog. Hom I2 receptors yog nyob rau hauv cov neurons ntawm cerebral cortex, platelets, daim siab thiab lub raum hlwb. Lawv qhov tseem ceeb raws li ib qho kev iab liam ntawm cov tshuaj pharmacological tau kawm txog qhov tsawg dua.
Cia peb xav txog cov txheej txheem ntawm kev ua ntawm imidazoline receptor agonists.
Mechanism of action
Lub hom phiaj tseem ceeb rau cov tshuaj tiv thaiv ntshav siab yog hom I1 imidazoline central receptors, uas nyob hauv thaj tsam ventrolateral rostral ntawm medulla oblongata. Lawv qhov ua rau ua rau txo qis hauv lub suab ntawm lub cev muaj zog ntawm cov hlab ntsha, txo qis hauv kev ua haujlwm ntawm cov hlab ntsha ntawm lub siab, vim tias muaj qhov tsis muaj zog ntawm kev tso tawm ntawm norepinephrine los ntawm adrenergic neurons. Ntxiv nrog rau cov txheej txheem no, muaj qhov txo qis hauv kev tsim cov adrenaline los ntawm cov qog adrenal, uas kuj muaj imidazoline I1 receptors. Qhov tshwm sim ntawm qhov kev cuam tshuam no yog qhov txo qis hauv cov suab nrov ntawm cov hlab ntsha, qhov nce hauv hluav taws xob ruaj khov ntawm myocardium thiab bradycardia.
Ntawm lwm yam, imidazoline receptors nyob ntawm daim nyias nyiasmitochondria ntawm lub epithelium ntawm cov tubules thiab nyob rau hauv lub raum.
Kev txhawb zog ntawm lawv (feem ntau cov kws tshawb fawb ntseeg tias cov receptors no yog hom I1), uas ua rau muaj kev cuam tshuam ntawm sodium ion reabsorption thiab diuretic nyhuv, kuj tseem koom nrog hauv kev ua kom cov nyhuv hypotensive. Qhov no kuj tseem txhawb nqa los ntawm kev txo qis hauv renin ntau lawm, uas yog vim yog ib feem ntawm qhov txo qis hauv kev sib koom tes.
Thaum zoo siab hauv cov hlwb ntawm β-islets ntawm Langerhans ntawm pancreas, I1 receptors ua rau muaj kev tso tawm ntawm insulin ntau ntxiv, uas teb rau cov carbohydrate load thiab ua rau cov nyhuv hypoglycemic.
Cia peb xav txog qhov ua tau zoo tshaj plaws imidazoline receptor agonists.
Moxonidine (Cint, Physiotens)
Cov tshuaj yuav luag tsis muaj kev cuam tshuam rau α-adrenergic receptors thiab xaiv excites I1 imidazoline receptors hauv medulla oblongata. Raws li qhov tshwm sim, lub suab sympathetic innervation txo qis, vim tias tag nrho cov peripheral vascular tsis kam txo thiab, kom tsawg dua, lub zog thiab zaus ntawm lub plawv contractions. Lub ntim ntawm ejection ntawm lub plawv yog xyaum tsis hloov. Txo myocardial oxygen xav tau. Kev sim ua pov thawj xws li kev ua ntawm moxonidine li cardioprotective. Nws smoothly thiab zoo txo diastolic thiab systolic siab, txo cov qib ntawm angiotensin-II, norepinephrine thiab aldosterone nyob rau hauv cov ntshav, renin kev ua si. Ib qho tseem ceeb ntawm moxonidine yog kev tiv thaiv kev txhim kho thiab txo cov myocardial hypertrophy uas twb muaj lawm hauv tus neeg mob.
NrogTsis tas li ntawd, cov tshuaj muaj ib tug concomitant hypoglycemic nyhuv, vim yog excitation ntawm imidazoline pancreatic receptors. Nws muaj nyob rau hauv kev nce cov piam thaj mus rau cov hlwb, muaj zog synthesis ntawm glycogen. Lub lipid-txo cov nyhuv ntawm moxinidin kuj tau tsim.
Cov tom kawg yog nqus tau zoo hauv lub plab thiab cov hnyuv (kwv yees li 90%). Nws raug tso tawm los ntawm ob lub raum feem ntau nyob rau hauv daim ntawv tsis hloov pauv (los ntawm lub siab mus rau qhov tsawg dua), txawm li cas los xij, tsis muaj qhov cuam tshuam loj heev txawm tias lub raum tsis ua haujlwm nruab nrab thiab me me. Cov nyhuv hypotensive ntawm no imidazoline receptor agonist kav ntev txog ib hnub. Kev coj cwj pwm rau moxonidine thiab tshem tawm syndrome tsis tau sau tseg.
Kev qhia ntawm cov cuab yeej no
Symptomatic arterial hypertension thiab kub siab, tshwj xeeb tshaj yog thaum ua ke nrog hom 2 mob ntshav qab zib mellitus thiab rog ("metabolic syndrome"), nrog rau kev tiv thaiv kev kub ntxhov.
Dab tsi yog qhov qhia tau rau tus imidazoline receptor agonist? Yog tias kev kho mob tau npaj, thawj zaug ntawm moxonidine yog 0.2 mg thaum sawv ntxov ib hnub ib hnub (qhov ncauj tom qab lossis thaum noj mov). Nrog kev ua haujlwm tsis txaus tom qab ob lub lis piam, qhov koob tshuaj tau nce mus rau 0.4 mg thaum sawv ntxov lossis 0.2 mg thaum yav tsaus ntuj thiab sawv ntxov. Qhov siab tshaj plaws ib zaug yog 0.4 mg, ib hnub - 0.6 mg. Yog tias lub raum ua haujlwm tsis zoo, ib koob tshuaj yog 0.2 mg, ib hnub (yog tias muab faib ua ob koob) - qhov siab tshaj plaws ntawm 0.4 mg. Cov tshuaj tshwj xeeb tshaj yog tag nrho thiab sai sai absorbed kuj thaum noj nyob rau hauv tus nplaig, ntsemoxonidine yog siv nyob rau hauv hypertensive crises sublingually (ib zaug 0.4 mg nyob rau hauv crushed daim ntawv), ua ke nrog calcium channel blockers los yog ib leeg, tshwj xeeb tshaj yog nrog isradipine.
Data los ntawm Nikitina A. N. qhia tias qhov no, tom qab 20 feeb, muaj qhov txo qis, thiab tom qab ib teev - ploj ntawm lub suab nrov hauv lub taub hau thiab mob taub hau, yaug lub ntsej muag. Systolic siab maj mam txo los ntawm 19-20%, los ntawm 14-15 - diastolic, los ntawm 8-10 - lub plawv dhia.
Thaum kho nrog moxonidine, lub siab yuav tsum tau saib xyuas tas li.
Side tsos mob
Qhov imidazoline receptor agonist tsis tshua ua rau kiv taub hau, orthostatic hypotension. Qhuav nyob rau hauv lub qhov ncauj kab noj hniav yog tsis tseem ceeb, tshwm sim tsuas yog nyob rau hauv 7-12% ntawm cov neeg mob. Muaj tsawg zaus, muaj cov nyhuv sedative me ntsis.
YContraindications
Atrioventricular blockade ntawm qib thib ob lossis thib peb, mob sinus syndrome, bradycardia (qis dua 50 tus neeg ntaus ib feeb), plaub degree circulatory tsis ua haujlwm, lub raum tsis ua haujlwm hnyav, tsis ruaj khov angina, Raynaud's kab mob, hnub nyoog qeb mus txog 16 xyoo (hauv Tam sim no tsis muaj kev paub txog kev siv tshuaj rau kev kho cov tub ntxhais hluas thiab cov menyuam yaus), obliterating endarteritis, lactation, parkinsonism, cev xeeb tub, qaug dab peg, glaucoma thiab kev nyuaj siab.
Qhov kev xaiv hauv nruab nrab imidazoline receptor agonist cuam tshuam nrog lwm tus neeg ua haujlwm li cas?
Kev sib tham nrog lwm yam tshuaj
Ua kom cov nyhuv ntawm lwm cov tshuaj tiv thaiv kab mob siab thiab tuaj yeem ua ke nrog lawv. Thaum noj β-blockers thiab moxonidine tib lub sijhawm, nws yog ntshaw kom tshem tawm thawj cov blocker. Tsawg zaus, clonidine txhim kho cov nyhuv ntawm cov dej cawv, tshuaj tsaug zog thiab sedatives, tab sis nws yog qhov zoo dua kom tsis txhob muaj kev sib xyaw ua ke. Ua haujlwm zoo nrog diuretics. Tej zaum yuav ua rau kom cov nyhuv ntawm cov tshuaj hypoglycemic.
Lwm tus imidazoline I1 receptor agonist tau piav qhia hauv qab no.
Rilmenidine (Tenaxum, Albarel)
Tus neeg sawv cev, uas yog cov txiaj ntsig ntawm oxazosin, muaj kev xaiv ntau dua ntawm kev sib koom ua ke nrog imidazoline I1 receptors ob qho tib si hauv lub hlwb thiab ntawm qhov chaw. Cov qauv hemodynamic ntawm cov nyhuv hypotensive feem ntau cuam tshuam nrog kev txo qis hauv peripheral vascular tsis kam feem ntau. Monotherapy nrog rilmenidine tso cai rau kev tswj kom zoo hauv 70% ntawm cov neeg mob ntshav siab. Feem ntau, cov nyhuv hypotensive tau ua tiav sai thiab du, khaws cia tsis tu ncua nyob rau ib hnub vim lub sijhawm, mus txog hnub.
Agonist ntawm imidazoline receptors nyob rau hauv cov nyhuv antihypertensive tsis yog phem dua li thiazide diuretics, angiotensin-hloov enzyme inhibitors, β-blockers, thaum sib txawv nyob rau hauv zoo heev tolerability thiab ib tug me me ntawm cov kev mob tshwm sim. Kev siv yog pom zoo nyob rau hauv cov ntaub ntawv tsis txaus ntawm cov nyiaj saum toj no. Nws yuav tsum tau hais txog cov metabolic neutrality ntawm rilmenidine - muaj txiaj ntsig zoo rauLub raum ua haujlwm, txo qis hauv microalbuminaria, tsis muaj kev hloov pauv hauv lipid thiab carbohydrate metabolism.
Ua tiav thiab sai sai absorbed thaum noj qhov ncauj, tsis muaj kev cuam tshuam ntawm thawj zaug ntawm cov tshuaj los ntawm lub siab. Rilmenidine yog metabolized tsis zoo, feem ntau tawm hauv cov zis, nws cov concentration hauv cov neeg mob siv cov tshuaj ntau tshaj ib xyoos yog yuav luag ruaj khov.
Thaum pom?
Hypertension arterial, suav nrog cov neeg laus laus, lub raum tsis ua haujlwm, ntshav qab zib mellitus, creatinine tshem tawm tsawg kawg 15 ml ib feeb.
Cov tshuaj feem ntau muab ib ntsiav tshuaj (1 mg) ib hnub ua ntej noj mov. Yog tias cov nyhuv hypotensive tsis txaus nyob rau hauv ib lub hlis ntawm kev kho mob, nws raug nquahu kom nce qhov koob tshuaj rau ob ntsiav tshuaj ib hnub (tag kis thiab yav tsaus ntuj). Kev kho mob tuaj yeem ntev, txog li ob peb lub hlis. Tib lub sijhawm, kev tshem tawm yuav tsum maj mam.
Tsis tshua muaj, vim yog rilmenidine, lub siab xav txo qis, pw tsaug zog thiab lub plawv dhia raug cuam tshuam, epigastric tsis xis nyob thiab asthenia tshwm. Hauv cov xwm txheej sib cais, raws plab lossis cem quav, khaus, khaus ntawm daim tawv nqaij, mob khaub thuas thiab txhais tes raug kaw. Qhov ncauj qhuav yuav luag tsis muaj.
Contraindications rau kev siv rilmenidine
Kev cev xeeb tub, lub raum tsis ua haujlwm hnyav, lactation, kev nyuaj siab loj. Kev saib xyuas tshwj xeeb yuav tsum tau noj thaum muab tshuaj rau cov neeg mob uas nyuam qhuav muaj myocardial infarction lossis mob hlab ntsha tawg.
Kev sib tham nrog lwm tustshuaj
Nws tsis tuaj yeem ua ke rilmenidine nrog cov tshuaj tiv thaiv kev ntxhov siab nrog cov txheej txheem sib txawv ntawm kev ua - tricyclic thiab MAO inhibitors (hauv thawj rooj plaub, cov nyhuv hypotensive tsis muaj zog). Tsis txhob muab tshuaj nrog cawv.
Nyob rau hauv xaus, nws yuav tsum tau hais tias muaj qhov sib txawv tseem ceeb ntawm kev xaiv agonists sib txawv ntawm imidazoline I1 receptors, txawm tias qhov zoo sib xws ntawm pharmacodynamics. Xav txog qhov kev paub ntawm kev siv cov tshuaj no, lawv cov kev qhia dav dav rau hauv kev xyaum yog qhov tshwj xeeb rau kev txhim kho kev nyab xeeb thiab kev ua tau zoo ntawm kev kho mob ntshav siab, tshwj xeeb tshaj yog thaum nrog ntshav qab zib mellitus.
Peb tau saib seb cov tshuaj imidazoline receptor agonist ua haujlwm li cas.
