Calcium channel blockers yog cov tshuaj siv tau zoo nrog ntau yam tshuaj siv tshuaj. Cov npe ntawm calcium antagonists muaj ntau tshaj nees nkaum yam tshuaj, txhua yam uas cuam tshuam rau lub cev ntawm ib tug neeg nyob rau hauv ib txoj kev sib txawv. Tau ntev, lawv tau siv nyob rau hauv cov tswv yim tshuaj - kev kho mob, neurology, gynecology vim lawv cov nyhuv ntawm cellular cov ntaub so ntswg ntawm lub plawv cov leeg, lub conduction system ntawm lub plawv, myometrium thiab vascular du nqaij. Cov tshuaj ntawm cov pab pawg no ua rau nws nyuaj rau calcium nkag mus rau hauv cov hlwb los ntawm calcium channels, uas yog cov proteins nyob rau hauv lub cell daim nyias nyias thiab kis tau tus kab mob los ntawm tshwj xeeb qhib.
Lub luag haujlwm ntawm calcium hauv lub cev
Cov kab no nyob rau hauv feem pua ntawm cov ntsiab lus yog nyob rau hauv thib tsib ntawm tag nrho cov ntxhia tshuaj muaj nyob rau hauv lub cev ntawm ib tug neeg. Nws yog ib qho tsim nyog rau lub zog ntawm cov pob txha cov ntaub so ntswg thiab cov kev cai ntawm kev ua haujlwm ntawm lub plawv. Ions ntawm cov kab mob, nkag mus rau cov leeg hlwb ntawm lub plawv, tawm mus rau hauv qhov chaw intercellular nrog kev pab los ntawm ionic.twj. Vim lawv nkag mus rau hauv cardiomyocyte, myocardium cog lus, thiab raws li kev tawm, nws so. Yog li, calcium siv lub luag haujlwm tseem ceeb hauv kev ua haujlwm ntawm lub plawv cov leeg thiab koom nrog kev tswj hwm lub plawv dhia. Lub plawv yog lub luag haujlwm rau cov ntshav muab rau tag nrho lub cev thiab lub cev, thiab yog tias ua tsis tau, tag nrho lub cev yuav raug kev txom nyem.
cov ntaub ntawv dav dav
Calcium antagonists tau ua tiav hauv kev kho plawv rau ntau tshaj li tsib caug xyoo. Cov poj koob yawm txwv ntawm pab pawg no ntawm cov tshuaj tiv thaiv ntshav siab yog cov tshuaj "Verapamil", tsim los ntawm German kws tshwj xeeb hauv xyoo 1961. Hauv cov tshuaj siv tau, nws tau ua pov thawj nws tus kheej tsis yog ua cov vasodilator zoo xwb, tab sis kuj yog tus neeg sawv cev nrog cov txiaj ntsig cardiotropic. "Verapamil" tau ntau xyoo tom qab nws tsim tau raug ntaus nqi rau cov pab pawg ntawm beta-blockers, txawm li cas los xij, kev tshawb fawb ntxiv ntawm cov txheej txheem ntawm kev ua ntawm cov tshuaj pom tau hais tias nws muaj peev xwm inhibit transmembrane calcium tam sim no. Nyob rau hauv lub neej yav tom ntej, nws tau npaj kom muab cov tshuaj zoo sib xws hauv kev ua haujlwm nrog Verapamil rau hauv ib pawg hu ua calcium channel blockers. Nyob rau hauv lub lig 60s thiab thaum ntxov 70s, cov tshuaj Nifedipine thiab Diltiazem tau tsim, uas tau los ua lub npe hu ua thawj tiam.
Tshuaj ntawm pab pawg no tau pom lawv siv los ua cov kab mob coronary lytics hauv cov kab mob plawv, thiab tseem siv los ua cov tshuaj tiv thaiv thiab tshuaj kho mob ntshav siab. Qhov kev siv dav dav no yog vim qhov kev txiav txim ntawm calcium antagonists los so cov leeg ntawm phab ntsa vascular thiabnthuav cov hlab ntsha ntawm coronary, cerebral txaj, tsis cuam tshuam rau lub suab ntawm cov leeg. "Diltiazem" thiab "Verapamil" txo qis kev noj cov pa los ntawm myocardium thiab txo nws cov contractility, ntxiv rau, lawv inhibit qhov kev ua ntawm lub sinus node thiab supraventricular arrhythmias, ntxiv rau, lawv tau endowed nrog ib tug antihypertensive nyhuv. "Diltiazem" nyob rau hauv nws cov khoom yog nyob rau hauv ib tug nruab nrab txoj hauj lwm ntawm "Verapamil" thiab "Nifedipine". Qhov kawg, rau qhov tsawg dua, muaj kev cuam tshuam rau myocardial contractility thiab lub plawv conduction system. Nws yog qhia rau peripheral vasospasm thiab arterial hypertension. Tsuas yog pawg kws tshuaj ntawm cov tshuaj calcium antagonist uas sib xyaw tshuaj:
- sib txawv hauv cov qauv tshuaj;
- nrog ntau yam kev ua haujlwm;
- sib txawv hauv kev kho mob, ua haujlwm kho mob;
- sib txawv hauv contraindications thiab phiv.
Kev faib tawm
Calcium antagonists yog qhov txawv ntawm cov qauv tshuaj:
- YDihydropyridine. Kev npaj ntawm no series nce lub mem tes. Lawv raug sau tseg nyob rau hauv kev kho mob ntawm atherosclerosis ntawm peripheral hlab ntsha, kub siab, sab laug ventricular hypertrophy, angina pectoris. Lawv tsis qhia nyob rau hauv kev kho mob ntawm arrhythmia.
- Nonhydropyridines yog benzodiazepine thiab phenylalkylamine derivatives. Cov tshuaj no tau pom tias muaj txiaj ntsig zoo hauv kev kho mob atherosclerosis ntawm cov hlab ntsha carotid, angina pectoris. Lawv tau txais txiaj ntsig nrog kev hais tawm los tiv thaiv ischemic, hypotensive, antiarrhythmic nyhuv. Yuav txo tau lub plawv dhia.
- Tsis xaiv. Cov no suav nrog derivatives ntawm diphenylpiperazine. Lawv txhim kho cerebral ncig, tsis muaj kev cuam tshuam rau qib siab, tab sis muaj peev xwm ntawm vasodilating nyhuv.
Ntau tiam neeg ntawm calcium antagonists tau ua tiav hauv cov tshuaj:
- Thawj yog Nifedipine, Verapamil, Diltiazem. Qhov tsis zoo ntawm cov tshuaj no suav nrog kev tshem tawm sai ntawm lub cev thiab tsis muaj bioavailability.
- Qhov thib ob yog sawv cev los ntawm kev hloov kho cov ntawv tso tawm - "Nifedipine XL", "Verapamil SR". Cov tshuaj muaj kev kho mob ntev dua. Txawm li cas los xij, qib siab tshaj plaws hauv cov ntshav tau mus txog lub sijhawm sib txawv, thiab yog li nws nyuaj heev los kwv yees lawv cov txiaj ntsig.
- Thib peb - cov no yog cov tshuaj ua haujlwm ntev uas muaj txiaj ntsig zoo bioavailability. Lawv cov neeg sawv cev yog "Amlodipine", "Lercanidipine", uas feem ntau tau sau rau kev kho mob ntshav siab.
Muaj lwm qhov kev faib tawm ntawm calcium antagonists hauv cov ntaub ntawv. Piv txwv li, benzodiazepine thiab phenylalkylamine derivatives tau muab faib ua cov pab pawg sib cais, thiab, nyob ntawm cov lus qhia rau kev siv, cov tshuaj dihydropyridine yog qhov txawv, uas tau sau rau angina pectoris, sab laug ventricular hypertrophy, ntshav siab hauv cov neeg laus, thiab cov tshuaj uas tsis yog dihydropyridine. - rau atherosclerosis ntawm cov hlab ntsha carotid, supraventricular tachycardia.
Nyob rau xyoo tas los no, calcium channel blockers, nyob ntawm seb cov nyhuv ntawm lub plawv dhiamuab faib ua pawg hauv qab no:
- txo cov suab nrov, piv txwv li, "Verapamil", "Diltiazem";
- nce lossis tsis hloov lub suab, piv txwv li, Nifedipine thiab tag nrho cov dihydropyridine derivatives
Lub Sijhawm ntawm kev tiv thaiv kab mob siab
Lub hauv paus ntawm cov nyhuv hypotensive ntawm tag nrho cov calcium channel blockers yog lawv lub peev xwm los nthuav cov hlab ntsha, thaum pab txo qis hauv tag nrho cov peripheral tsis kam. Cov nyhuv vasodilating tshaj plaws yog qhia hauv "Nitrendipine", "Amlodipine", "Isradipine". Cov tshuaj muaj qhov nqus tau siab, tab sis muaj qhov sib txawv (tsis tuaj yeem) bioavailability. Qhov ceev ntawm qhov pib ntawm qhov siab tshaj plaws plasma concentration txawv ntawm ib mus rau kaum ob teev, nyob ntawm seb cov tshuaj tiam twg. Cov npe ntawm cov tshuaj calcium antagonist sib txawv nyob rau lub sijhawm ntawm cov nyhuv hypotensive (hauv teev):
- "Amlodipine" - ntev ntev (24-36).
- Cov tshuaj ntev ntev: Felodipine, Diltiazem, Nifedipine, Verapamil, Isradipine - mus sij hawm ntev (18–24).
- Isradipine, Felodipine - nruab nrab (8-18).
- Nifedipine, Diltiazem, Verapamil - luv (6-8).
Mechanism of action
Lub luag haujlwm ntawm kev ua ntawm calcium antagonists yog qhov sib txawv ntawm cov khoom siv tshuaj. Xav txog lawv qhov cuam tshuam rau cov hlab ntsha thiab lub plawv, nyob ntawm lub hom phiaj kho:
- "Nifedipine" thiab lwm tus neeg sawv cev ntawm dihydropyridine derivatives yog vasoselective agents. Ua kom so ntawm vascular du nqaijntshav ntws, thiab tsis cuam tshuam rau lub plawv ua haujlwm. Nrog rau kev nthuav dav ntawm cov hlab ntsha, ntshav siab thiab myocardial oxygen thov txo qis, spasm ntawm cov hlab ntsha ntawm cov hlab ntsha raug tiv thaiv. Maj mam tso cov ntaub ntawv ntawm cov tshuaj "Nifedipine" yog qhia rau kev kub siab thiab angina pectoris. Kev tso tawm sai - siv tau zoo tshaj plaws thaum muaj kev kub ntxhov.
- "Verapamil" muaj cov nyhuv inhibitory ntawm lub plawv cov leeg thiab cov leeg nqaij ntawm cov hlab ntsha. Cov cuab yeej vasodilating ntawm cov tshuaj no yog me ntsis manifested dua li ntawm dihydropyridine derivatives. Siv "Verapamil" nrog ventricular los yog atrial flutter, kom qeeb lub atherosclerosis thiab tiv thaiv angina tawm tsam, thiab raws li ib tug tshuaj nrog antiarrhythmic zog.
- Diltiazem zoo ib yam hauv nws cov tshuaj tshuaj rau Verapamil. Txawm li cas los xij, cov nyhuv vasodilatory tau tshaj tawm, thiab qhov tsis zoo chrono- thiab cov nyhuv inotropic tsawg dua li Verapamil.
Ntxiv rau kev txhim kho patency ntawm cov hlab ntsha, cov hlab ntsha, nrog rau cov hlab ntsha me me, cov nyhuv ntawm calcium antagonists tau tshwm sim:
- txo platelet aggregation;
- normalize plawv dhia;
- txo qis hauv pulmonary artery siab thiab bronchial dilatation;
- txo qis ntshav siab;
- antianginal, antiischemic thiab antiatherogenic nkaus.
YContraindications
Ib yam rau txhua tus calcium channel blockers:
- tus neeg intolerance, tus kheej yamtshuaj;
- pub mis niam;
- qis dua 18;
- daim siab thiab lub raum tsis zoo;
- ntshav siab;
- lub plawv tsis ua haujlwm nrog qis qis ventricular systolic muaj nuj nqi, tsis suav nrog Felodipine thiab Amlodipine;
- cev xeeb tub: "Verapamil" raug tso cai nyob rau lub sijhawm thib ob thiab thib peb, thiab "Nifedipine" - thoob plaws lub sijhawm, ntxiv rau, nws suav tias yog qhov ua tau zoo tshaj plaws hauv kev kub ntxhov.
Kev mob tshwm sim. Kev cuam tshuam nrog lwm yam tshuaj thiab zaub mov
Cov tshuaj tiv thaiv tsis zoo tom qab noj cov tshuaj no muaj qee qhov sib txawv.
Rau cov uas tsis yog-dihydropyridine calcium antagonists:
- tsis xav tau ib txhij txais tos nrog beta-blockers;
- bradycardia;
- tachycardia;
- atrial flutter syndrome nrog ntu ntawm antidromic tachycardia;
- atrioventricular conduction tsis ua haujlwm;
- mob sinus syndrome.
Rau dihydropyridine - reflex tachycardia.
Rau txhua tus calcium ion antagonists:
- siab siab;
- kev tsis haum;
- drowsy;
- mob plab;
- ntua;
- mob plab;
- tides;
- mob taub hau, kiv taub hau;
- peripheral edema;
- txo qis hauv ventricular systolic muaj nuj nqi tshwj tsis yog rau Felodipine thiab Amlodipine.
Kev sib xyaw ntawm cov tshuaj tiv thaiv kab mob nrog cov antagonists yog qhov txaus ntshaicalcium. Ib qho kev nce ntxiv hauv cov ntsiab lus ntawm qhov kawg yog pom thaum lawv tau koom nrog kev kho mob plawv glycosides, cov tshuaj tsis-steroidal anti-inflammatory, sulfonamides, indirect anticoagulants, nrog rau Lidocaine thiab Diazepam. Tsis tas li ntawd, calcium channel blockers nce cov nyhuv ntawm diuretics thiab ACE inhibitors. Thaum lub sij hawm ntawm kev kho mob nrog pab pawg neeg ntawm cov tshuaj no, nws yog pom zoo kom tsis txhob haus cawv txiv hmab txiv ntoo thiab kua txiv los ntawm nws. Kev haus dej haus cawv ua rau muaj kev phiv loj heev.
Cov lus qhia rau kev siv
Pathological mob uas siv calcium antagonists:
- angina;
- pulmonary hypertension;
- mob ntshav siab;
- Kuv muaj ib qho kev ntseeg siab thiab txoj kev ncig ua si;
- mob plawv ischemic;
- subarachnoid los ntshav;
- Raynaud's syndrome;
- dysmenorrhea;
- hypertrophic cardiomyopathy;
- kiv taub hau;
- mob khaub thuas;
- kev tiv thaiv ntawm migraine tawm tsam;
- myocardial infarction;
- urinary incontinence;
- glaucoma;
- obstructive pulmonary disease;
- preterm yug;
- esophageal spasm.
Calcium antagonist kho
- Arterial hypertension. Cov tshuaj no tau lees paub tias yog ib qho zoo tshaj plaws ntawm cov tshuaj antihypertensive. Los ntawm kev txo qis cov kab mob vascular tsis kam, calcium channel blockers txo cov ntshav siab. Nyob rau hauv lawv lub zog, cov hlab ntsha poob feem ntau, thiab raucov leeg lawv muaj qhov cuam tshuam tsis tseem ceeb.
- Supraventricular arrhythmias. "Diltiazem" thiab "Verapamil" muaj peev xwm rov ua tau zoo li qub ntawm lub plawv los ntawm kev ua ntawm atrioventricular thiab sinus nodes.
- Angina. Ua tsaug rau kev noj cov tshuaj dihydropyridines, ntshav siab poob qis, raws li, kev thauj khoom ntawm lub plawv kuj txo qis thiab, vim li ntawd, qhov xav tau oxygen txo. Tsis tas li ntawd, calcium antagonists tiv thaiv spasm ntawm cov hlab ntsha coronary, ua rau lawv nthuav. Ua tsaug rau qhov no, cov ntshav muab rau myocardium txhim kho.
- Hypertrophic cardiomyopathy. Nrog rau qhov no pathology, thickening ntawm lub plawv phab ntsa tshwm sim. "Verapamil" pab ua kom tsis muaj zog ntawm lub plawv. Nws raug sau tseg rau contraindications nyob rau hauv ib tug neeg rau noj beta-blockers.
- Pulmonary hypertension. Rau kev kho mob ntawm cov kab mob no, Amlodipine, Nifedipine lossis Diltiazem raug pom zoo.
- Raynaud tus kab mob yog tshwm sim los ntawm spastic vasoconstriction, ob txhais taw thiab txhais tes yog feem ntau raug rau qhov no. "Nifedipine" tshem tawm spasm ntawm cov hlab ntsha thiab yog li qhov zaus ntawm kev tawm tsam raug txo. Nws tuaj yeem siv lwm cov tshuaj calcium ion antagonists - tshuaj "Amlodipine", "Diltiazem"
- Tocolysis. Txhawm rau tiv thaiv kev yug ntxov ntxov thaum so cov leeg nqaij ntawm lub tsev menyuam, Nifedipine tau muab tshuaj.
- Subarachnoid hemorrhage. Hauv qhov no, Nimodipine muaj txiaj ntsig zoo rau cov hlab ntsha hauv hlwb. Nws tiv thaiv vasospasm.
- Cluster headache. Kev noj Verapamil yuav pab txo qis qaug dab peg.
Calcium Antagonists Tshuaj List
Cov tshuaj kws tshaj lij yog dihydropyridine derivatives:
- "Nifedipine". Nws muaj ntau yam kev qhia rau kev siv. Cov tshuaj ua haujlwm ntev yog siv los kho angina thiab kub siab.
- "Ispradipine", "Lercanidipine" zoo ib yam li thawj cov tshuaj hais txog cov yam ntxwv. Lawv raug pom zoo tshwj xeeb rau kev kho mob ntawm arterial hypertension.
- "Amlodipine", "Felodipine", "Lomir", "Norvask". Influencing cov hlab ntsha, lawv tsis muaj kev cuam tshuam rau lub contractility ntawm lub plawv. Vim qhov ua tau ntev, nws yooj yim siv rau hauv kev kho mob vasospastic angina thiab kub siab.
- Nicardipine Siv los kho cov ntshav siab, angina pectoris. Lub tshuab ua haujlwm ntawm cov hlab ntsha zoo ib yam li Nifedipine.
- "Nimodipine" muaj kev xaiv rau cov hlab ntsha ntawm lub hlwb. Feem ntau siv nyob rau hauv subarachnoid hemorrhage los txo thiab tiv thaiv kev spasm tom qab ntawm cov hlab ntsha hlwb.
Cov npe ntawm calcium antagonists ntawm lwm pab pawg suav nrog:
- Y Phenylalkylamines - Isoptin, Finoptin, Gallopamil, Anipamil. Hauv cov tshuaj siv tswv yim, Verapamil feem ntau yog siv, uas cuam tshuam rau kev ua haujlwm ntawm atrioventricular node thiab ua rau lub siab ua haujlwm. Siv los kho angina pectoris.
- Benzodiazepines - Altiazem, Dilzem. Ib tus neeg sawv cev paub zoo yog Diltiazem, uas ua rau cov hlab ntsha tawg thiab ua rau tsis zoo rau cov txheej txheem conduction.lub siab. Nws yog tshuaj rau angina pectoris.
Pharmacokinetics thiab pharmacodynamics ntawm calcium channel blockers
Pharmacokinetic zog ntawm cov tshuaj cuam tshuam nws kev siv tshuaj kho mob:
- "Nifedipine" tsis tuaj yeem khaws cia hauv lub cev ntawm tus neeg. Yog li, kev siv cov tshuaj no tas li hauv ib koob tshuaj tsis ua kom nws cov txiaj ntsig.
- Verapamil, thaum noj tsis tu ncua, muaj peev xwm sib sau ua ke, uas ua rau muaj kev nce ntxiv hauv cov txiaj ntsig kho mob thiab ua rau tsis xav tau.
- Diltiazem, zoo li cov tshuaj yav dhau los, accumulates hauv lub cev, tab sis kom tsawg dua.
Nyob ntawm lub hnub nyoog ntawm tus neeg mob, ntau cov tshuaj muaj qhov hloov pauv hauv cov tshuaj pharmacokinetics. Calcium antagonists tsis muaj kev zam. Hauv cov neeg laus, ib nrab lub neej ntawm Nifedipine, Diltiazem thiab Verapamil tau ntev, thiab lawv qhov kev tshem tawm kuj txo qis. Yog li ntawd, qhov tshwm sim ntawm kev phiv tshwm sim nce. Yog li ntawd, pawg neeg mob no yuav tsum xaiv cov tshuaj kho ib tus zuj zus, pib nrog qhov tsawg tshaj plaws.
Lub xub ntiag ntawm lub raum tsis txaus hauv ib tus neeg yuav luag tsis cuam tshuam rau cov tshuaj pharmacokinetics ntawm Diltiazem thiab Verapamil. Thiab thaum noj Nifedipine hauv cov neeg mob zoo li no, nws ib nrab-lub neej nce, uas ua rau muaj kev tshwm sim tshwm sim.
Pharmacodynamic kev sib cuam tshuam kuj tseem ceeb hauv kev kho mob. Kev noj tshuaj beta-blocker nrog Diltiazem lossis Verapamil ua rau tsis ua haujlwm hauvsab laug ventricular muaj nuj nqi raws li qhov tshwm sim ntawm qhov kev suav ntawm qhov tsis zoo inotropic nyhuv ntawm cov tshuaj no. Kev teem sijhawm ntawm beta-blockers thiab "Nifedipine" yuav ua rau cov kev mob tshwm sim ntawm cov tshuaj no.
Kev sib xyaw ntawm nitrates nrog "Nifedipine" tsis pom zoo, vim nws ua rau txo qis hauv cov ntshav siab, vasodilation ntau dhau thiab tsim cov tshuaj tiv thaiv tsis xav tau.
Yog li, calcium channel blockers yog cov tshuaj siv tau zoo, uas tau raug pov thawj los ntawm ntau xyoo ntawm kev paub hauv lawv txoj kev siv. Lub xub ntiag ntawm cov txheej txheem sib txawv ntawm kev ua, kev sib cuam tshuam thiab kev mob tshwm sim yuav tsum muaj kev sib txawv ntawm kev sau tshuaj los ntawm pab pawg no.
