Organic nitrates tau nkag mus rau hauv kev kho mob hauv xyoo 19th. Xyoo 1879 ib tsab xov xwm tau luam tawm los ntawm Dr. Murrel, uas tau hais txog kev siv nitroglycerin txhawm rau tshem tawm angina tawm tsam.
Muab qhov tseem ceeb ntawm cov kab mob coronary, qhov cuam tshuam ntawm cov tshuaj suav hais tias yog siab heev niaj hnub no. Txog tam sim no, nitroglycerin thiab lwm yam tshuaj tsim los ntawm nws lub hauv paus, nrog rau cov tshuaj ze rau lawv, isosorbide mono- thiab dinitrate, suav tias yog cov tshuaj tiv thaiv kab mob zoo tshaj plaws.
Cov nyhuv antianginal ntawm cov organic nitrates yog txuam nrog kev nce hauv cov pa oxygen rau cov leeg plawv thiab, tib lub sijhawm, nrog kev txo qis hauv nws qhov kev xav tau.
Mechanism of action
Txawm hais tias muaj kev paub ntev ntawm kev siv, lub tshuab ntawm antianginal thiabCov nyhuv vasodilating ntawm nitrates tau tsim tsis ntev los no. Nws muaj nyob rau hauv cov teebmeem myotropic thiab neurotropic ntawm lub ntsiab Cheebtsam.
Thaum noj, NO pawg tau sib cais los ntawm nitrate molecule, zoo ib yam li endothelial relaxing yam. Nws activates guanylate cyclase, uas ua rau kom nce qib ntawm cyclic guanosine monophosphate, tsub zuj zuj ntawm cov uas ua rau kev loj hlob ntawm myosin dephosphorylation thiab txo qhov kev nkag mus ntawm calcium ions mus rau hauv lub hlwb, ua rau kom cov leeg du ntawm cov leeg. phab ntsa vascular. Qhov no tuaj yeem raug sau tseg hauv cov zis, ua pa, plab hnyuv. Los ntawm kev ua ntawm cov qauv ntawm lub paj hlwb, nitrates pab txhawb rau kev thaiv ntawm lub hauv paus seem ntawm coronary reflexes, thiab tsis muaj zog ntawm kev saib xyuas ntawm cov hlab plawv system.
Nws paub tias hmoov txhuv nplej siab yog cov organic. Cov dej txiv qaub thiab nyiaj nitrate tsis yog.
Antianginal ua tau zoo ntawm nitrates
Rau qhov ua tau zoo ntawm cov tshuaj tiv thaiv kab mob, tsis yog tsuas yog lub sijhawm luv luv thiab ncua sijhawm nthuav dav ntawm cov hlab ntsha thiab cov ntshav ntws los ntawm lawv yog qhov tseem ceeb, tab sis kuj tseem muaj hemodynamic tshem tawm ntawm lub plawv cov leeg, uas ua rau lub plawv tsis muaj zog thiab nws cov pa oxygen xav tau.. Raws li qhov tshwm sim ntawm kev nthuav dav ntawm cov hlab ntsha, qhov rov qab ntawm cov ntshav venous mus rau hauv lub cev yog txwv (qis qis hauv preload, siab nyob rau hauv lub ventricles, nro nyob rau hauv lawv cov phab ntsa), thiab expansion ntawm cov hlab ntsha txo cov theem ntawm tsis kam mus rau lub plawv tso zis. (txo qis tom qab load, tsis kam mus rau lub plawv tso zis, ntwszog thiab myocardial oxygen noj).
Cov txiaj ntsig zoo ntawm myocardial trophism
Ntxiv rau, cov organic nitrates muaj txiaj ntsig zoo rau myocardial trophism, kev ua haujlwm ntawm cov pa enzymes, electrolyte metabolism, ua kom cov hluav taws xob ruaj khov ntawm cov leeg plawv, tiv thaiv kev txhim kho ntawm arrhythmias. Qhov tseem ceeb tseem ceeb kuj yog cov cuab yeej ntawm cov tshuaj no kom txo qis, vim tias lawv siv rau sab laug ventricular tsis ua haujlwm.
Tshuaj
tshuaj kho mob ze rau cov organic nitrates (sodium nitroprusside, nitrites, molsidomine) kuj muaj cov nyhuv nitrooxidergic.
Lawv muaj qhov sib txawv ntawm cov tshuaj pharmacokinetic thiab cov lus qhia rau kev siv (nitroglycerin feem ntau yog siv los tshem tawm angina tawm tsam, lwm yam tshuaj los tiv thaiv lawv txoj kev loj hlob). Kev phiv tshuaj ntawm tus kheej cov khoom siv kho mob feem ntau yog los ntawm cov txheej txheem ntawm kev ua haujlwm rau tag nrho pawg ntawm cov tshuaj no, thiab yog li ntawd zoo sib xws.
Kev faib tawm ntawm cov organic nitrates
Txhua yam tshuaj no poob rau plaub yam tseem ceeb:
- nitroglycerin npaj;
- tshuaj raws li isosorbide dinitrate;
- tshuaj ntawm isosorbide mononitrate;
- tshuaj zoo li nitrate.
Tshuaj raws li nitroglycerin muaj lub sijhawm ua haujlwm ntev. Cov no suav nrog:"Sustonit", "Sustak", "Nitrong", "Trinitrolong", "Nitroderm"
Tshuaj raws li isosorbide dinitrate muaj lub sijhawm luv ntawm kev ua.
Pab pawg ntawm cov organic nitrates suav nrog cov tshuaj xws li Iso-Mik, Nitrosorbide thiab Isodinit.
Cov tshuaj raws li isosorbide mononitrate muaj txiaj ntsig ntev, thiab lawv cov npe suav nrog cov tshuaj xws li Monocinque Retard, Mono Mac Depot.
Nitrate zoo li tshuaj suav nrog Molsidomin, Amyl nitrite thiab sodium nitroprusside.
Yuav ua li cas cov organic nitrate siv rau kev kub siab?
Kev kho mob ntawm arterial hypotension
Kev txo cov ntshav siab ntau dua 15 mmHg yog qhov tseem ceeb hauv kev kho mob. Art. los ntawm qib nkag. Tus kab mob no yog vim hais tias vasodilating nyhuv ntawm nitrates. Nrog rau qhov txo qis hauv cov ntshav siab, nws tuaj yeem txo cov ntshav mus rau txhua lub cev, suav nrog lub plawv. Txhawm rau tiv thaiv kev loj hlob ntawm hypotension hnyav, kev siv nitroglycerin nyob rau hauv ib qho chaw zaum lossis pw nrog ob txhais ceg siab yog pom zoo.
Kev noj cov tshuaj no nyob rau hauv ib qho chaw sawv ntsug tuaj yeem ua rau qaug zog thiab ua rau cov nyhuv antianginal tsis muaj zog, vim tias qhov txo qis hauv cov ntshav ua rau txo qis hauv cov ntshav coronary. Nyob rau hauv xws li mob, nyiag syndrome yuav tshwm sim, uas yog ib tug nce nyob rau hauv ischemia ntawm lub plawv cov leeg, tshwj xeeb tshaj yog nyob rau hauvCov neeg mob stenosing thoob plaws atherosclerosis ntawm cov hlab ntsha coronary.
Kev poob qis hauv siab tuaj yeem ua rau muaj kev npaj cov organic nitrate raws li sodium nitroprusside, uas yog siv rau hauv cov hlab ntsha hauv kev loj hlob ntawm kev kub ntxhov, pulmonary edema, preeclampsia, dissecting aortic aneurysm, eclampsia, nrog rau kev tswj cov ntshav siab thaum phais. kev cuam tshuam.
YContraindications
Cov tshuaj tiv thaiv tsis zoo no ua rau muaj qhov tsis zoo rau kev siv nitroglycerin thiab lwm cov organic nitrates li arterial hypotension nrog systolic siab tsawg dua 90 mm Hg. Art., thiab diastolic - tsawg dua 60 mm Hg. Art.; poob siab, tawg.
Kev Sib Tham Tshuaj
Lub peev xwm ntawm cov organic nitrates kom txo cov ntshav siab yog txhim kho thaum ua ke nrog lwm cov tshuaj vasodilating, cawv, tshuaj tua kab mob. Cais, nws yog ib qho tsim nyog yuav tsum nco ntsoov lawv qhov tsis sib haum xeeb nrog sildenafil ("Viagra"). Cov tshuaj no kuj ua los ntawm nitric oxide thiab potentiates vasodilating teebmeem nrog rau cov ntshav siab thiab txawm tuag.
Cov teebmeem ntawm cov organic nitrates
Nitrates tuaj yeem ua rau muaj qhov tsis zoo hauv qab no:
- Orthostatic collapse. Feem ntau, qhov kev phiv tshuaj no provokes nitroglycerin. Cov txheej txheem ntawm cov kab mob pathological no cuam tshuam nrog kev txo qis hauv venous rov qab mus rau lub plawv, uas txo cov ntshav mus rau lub hlwb.lub hlwb thaum coj txoj hauj lwm ntsug. Yog li ntawd, tom qab noj tshuaj, tus neeg mob yuav tsum ua kom maj mam thiab ua tib zoo.
- Tachycardia, uas yog cov kev mob tshwm sim tseem ceeb ntawm cov organic nitrates thiab muaj cov teebmeem baroreflex, uas yog los txo cov parasympathetic tswj lub plawv contractions teb rau qhov so ntawm cov phab ntsa vascular. tachycardia qee zaum tshwj xeeb tshaj tawm nrog kev kho tus kheej nrog nitrates. Nyob rau hauv cov ntaub ntawv ntawm lawv ib txhij siv nrog cov tshuaj uas ua rau bradycardia: calcium channel blockers los ntawm qeb ntawm phenylalkylamines ("Verapamil"), β-blockers thiab dihydropyridines ("Amlodipine", "Nicardipine", thiab lwm yam) - cov tsos mob ntawm sab no yog leveled.
- Bradycardia, uas yog qhov tsis tshua muaj tshwm sim uas qee zaum tshwm sim nrog kev txhaj tshuaj nitroglycerin rau hauv cov keeb kwm yav dhau los ntawm kev txo qis hauv siab. Lub ntsiab yog vim li cas rau qhov no pathological mob yog ua kom lub suab ntawm lub vagus paj. Atropine tuaj yeem siv los kho qhov tshwm sim no.
- mob taub hau yog cov tsos mob uas feem ntau tshwm sim tom qab noj cov organic nitrates. Cov tshuaj tiv thaiv no tuaj yeem nyob ntev li ntawm 20 feeb mus rau ob peb teev, nrog rau kiv taub hau, muaj tus cwj pwm pulsating, tshwj xeeb tshaj yog rau cov neeg mob cerebral atherosclerosis. Cephalgia yog txuam nrog qhov tsis zoo ntawm cov organic nitrates ntawm cerebral hemodynamics. Qhov tshwm sim ntawm qhov no yog qhov txo qis hauv cov ntshav khiav hauv lub hlwb, oxygen tshaib plab ntawm lub hlwb, nce hauv intracranial siab, nthuav ntawm phab ntsa ntawm cov leeg hauv pob txha taub hau,uas ua rau mob.
- Nruam intraocular siab, uas yog cov tsos mob tsis tu ncua ntawm nitrates. Hauv qhov no, glaucoma yog suav tias yog ib qho kev txwv rau lawv siv.
tshuaj noj tshuaj
"Nitroglycerin" yog siv raws li hauv qab no:
- capsules nrog 1% roj tov ntawm ib koob ntawm 0.001 thiab 0.0005 g;
- tablets 0.0005 g;
- aerosol rau kev siv sublingual - 0.0004g;
- dej cawv - 1-2 tee ib suab thaj.
Txhawm rau tiv thaiv angina tawm tsam, siv cov ntsiav tshuaj qhov ncauj ntev - Nitrong, Nitrogranu-ntev, Sustak forte. Cov npe ntawm cov organic nitrates yog qhov dav heev. Tom qab noj cov tshuaj no, qhov kev ua ntawm lub ntsiab lus pib tom qab 120 feeb thiab kav li 6 teev. Cov nyiaj no kuj tseem siv tau raws li kev kho mob ntawm cov kab mob transdermal - tshwj xeeb thaj ua rau thaj ("Deponit"), uas yog glued rau ntawm daim tawv nqaij rau 12 teev (patch tso tawm 0.0005 g ntawm cov khoom ib hnub twg).
Isosorbide dinitrate yog tswj hwm sublingually, nws cov nyhuv tshwm sim tom qab 3-5 feeb, thaum noj qhov ncauj - tom qab 15-30 feeb. Qhov ntau npaum li cas yog ib ntsiav tshuaj ib zaug, kev siv ntxiv yog txiav txim siab los ntawm txoj kev kho mob uas tsim los ntawm tus kws kho mob tshwj xeeb. Txawm hais tias siv cov tshuaj no dav dav hauv kev kho mob niaj hnub no, nws yog qhov zoo tshaj plaws los tswj hwm nws cov kev tswj hwm nrog tus kws kho mob, hauvnrog rau cov txiaj ntsig kho mob tau hais tawm thiab muaj peev xwm tshwm sim tsis zoo.
