Telmista 80 mg - cov lus qhia rau kev siv

Telmista 80 mg - ib qho tshuaj tiv thaiv kev tsis haum tshuaj, ib qho tshwj xeeb kev thaiv ntawm angiotensin II receptors (hom AT1).

1 ntsiav tshuaj 80 mg:

Lub cev nquag ua haujlwm: Telmisartan 80.00 mg

Cov muaj mob: meglumine, sodium hydroxide, povidone-KZO, lactose monohydrate, sorbitol (E420), magnesium stearate.

Ntsiav tshuaj 80 mg: Capsule-puab, biconvex ntsiav tshuaj ntawm cov xim dawb lossis yuav luag xim dawb.

Cov Tshuaj Hauv Tshuaj

Telmisartan yog ib hom tshuaj angiotensin II receptor antagonist (ARA II) (hom AT1), siv tau thaum noj ntawm qhov ncauj. Nws muaj qhov ua tau zoo rau AT1 subtype ntawm angiotensin II receptors, los ntawm qhov kev txiav txim ntawm angiotensin II tau pom. Txom cov tshuaj angiotensin II los ntawm qhov sib txuas nrog cov receptor, tsis muaj cov kev ua ntawm agonist nyob rau hauv kev sib raug zoo nrog cov receptor no. Telmisartan khi nkaus xwb rau AT1 subtype ntawm angiotensin II receptors. Cov kev sib txuas tas mus li. Nws tsis muaj kev sib raug zoo rau lwm tus txais, suav nrog AT2 receptors thiab lwm qhov tsawg kawm angiotensin receptors. Lub luag haujlwm tseem ceeb ntawm cov receptors, nrog rau cov txiaj ntsig ntawm lawv qhov kev xav tau dhau los nrog angiotensin II, qhov kev cia siab ntawm uas nce nrog kev siv telmisartan, tseem tsis tau kawm. Nws txo nws cov concentration ntawm aldosterone hauv ntshav plasma, tsis inhibit renin hauv ntshav ntshav thiab ns block ion channels. Telmisartan tsis inhibit angiotensin hloov enzyme (ACE) (kininase II) (ib qho enzyme uas tseem tsoo bradykinin). Yog li, kev nce qib hauv kev phiv los ntawm bradykinin tsis yog kev cia siab.

Hauv cov neeg mob, telmisartan ntawm ib koob ntawm 80 mg ua rau tag nrho cov kev cuam tshuam ntawm kev mob siab ntawm angiotensin II. Qhov pib ntawm kev tawm tsam qhov kev tiv thaiv tau sau tseg tsis pub dhau 3 teev tom qab thawj thawj coj ntawm telmisartan. Cov nyhuv ntawm cov tshuaj no mob tsawv rau 24 teev thiab tseem ceeb txog li 48 teev. Ib qho kev tawm tsam los tiv thaiv kev tiv thaiv feem ntau txhim kho tom qab 4-8 lub lim tiam ntawm kev tswj hwm tsis tu ncua ntawm telmisartan.

Hauv cov neeg mob uas mob ntshav lub plawv, telmisartan txo qis systolic thiab diastolic ntshav siab (BP) tsis cuam tshuam rau lub plawv dhia (HR).

Nyob rau hauv cov ntaub ntawv ntawm kev tshem tawm sai ntawm telmisartan, ntshav siab maj mam rov qab los rau nws thawj qib tsis muaj kev txhim kho ntawm "tshem tawm" syndrome.

Cov Tshuaj Pharmacokinetics

Thaum noj ntawm qhov ncauj, nws yog nqus tawm sai sai ntawm lub plab zom mov (GIT). Bioavailability yog 50%. Qhov kev txo qis hauv AUC (thaj chaw nyob rau hauv qhov kev xav-lub sijhawm nkhaus) nrog kev siv telmisartan tib lub sijhawm nrog kev noj zaub mov ntau li ntawm 6% (ntawm ib koob 40 mg) txog 19% (ntawm koob tshuaj 160 mg). 3 teev tom qab noj, qhov kev nkag siab hauv cov ntshav ntshav yog qib, tsis hais noj lub sijhawm noj mov. Muaj qhov sib txawv ntawm ntshav ntau nyob rau hauv cov txiv neej thiab poj niam. Qhov siab tshaj plaws (Cmax) hauv ntshav plasma thiab AUC hauv cov poj niam piv nrog txiv neej yog kwv yees li 3 thiab 2 zaug siab dua, ntsig txog (tsis muaj kev cuam tshuam rau lub txiaj ntsig tseem ceeb).

Kev sib txuas lus nrog cov ntshav plasma protein - 99.5%, feem ntau nrog albumin thiab alpha-1 glycoprotein.

Tus nqi nruab nrab ntawm pom meej qhov ntim ntawm kev faib tawm hauv qhov sib npaug ntawm cov tshuaj siab yog 500 litres. Nws yog metabolized los ntawm kev sib txuas nrog glucuronic acid. Metabolites yog tus tsis muaj tshuaj nyob hauv tsev muag tshuaj. Ib nrab-lub neej (T1 / 2) ntau dua 20 teev. Nws yog tawm hauv feem ntau los ntawm txoj hnyuv hauv daim ntawv tsis hloov pauv thiab los ntawm lub raum - tsawg dua 2% ntawm qhov muab noj. Tag nrho cov ntshav hauv lub plasma yog qhov siab (900 ml / min), tab sis piv nrog "ntshav siab" ntshav txaus (li 1500 ml / min).

Cov Yuav Tsum Muaj

Txoj kev txwv tsis pub siv Telmista tshuaj:

• Hypersensitivity rau cov tshuaj nquag lossis excipients ntawm cov tshuaj.
• Cev xeeb tub
• Lub sijhawm pub mis.
• Obstructive kab mob ntawm biliary ib ntsuj av.
• Hepatic cuam tshuam loj heev (Me Nyuam Pugh chav C).
• Siv cov kev tsis haum xeeb nrog aliskiren hauv cov neeg mob ntshav qab zib mellitus lossis mob me mus rau lub raum tsis ua haujlwm (glomerular filtration rate (GFR)

Sab sij huam

Cov kev soj ntsuam txog qhov tshwm sim tsis cuam tshuam nrog tus tub los ntxhais, hnub nyoog lossis haiv neeg ntawm cov neeg mob.

• Cov kab mob sib kis thiab cov kab mob parasitic: mob sepsis, nrog rau kev mob tuag tes tuag taw, mob txeeb zig (nrog rau mob cystitis), mob ua pa sab saud.
• Kev mob tsis txaus siab los ntawm cov ntshav thiab cov kab mob lymphatic: ntshav liab, eosinophilia, thrombocytopenia.
• Kev tiv thaiv kab mob hauv lub cev: mob anaphylactic, kev tiv thaiv tsis haum (erythema, urticaria, angioedema), eczema, khaus, tawv nqaij pob khaus (suav nrog tshuaj), mob hlwb (nrog rau kev tuag taus), hyperhidrosis, ua pob tawv nqaij lom.
• Kev ua txhaum ntawm lub paj hlwb: ntxhov siab, insomnia, kev nyuaj siab, tsaus muag, kiv taub hau.
• Kev tsis sib haum xeeb ntawm cov khoom hauv nruab nrog ntawm qhov muag: pom kev tab kaum.
• Kev ua txhaum ntawm lub siab: bradycardia, tachycardia.
• Kev ua txhaum ntawm cov hlab ntshav: ib qho cim txo qis hauv cov ntshav siab, orthostatic hypotension.
• Kev ua txhaum ntawm lub tshuab ua pa, lub hauv siab thiab mediastinum: ua pa luv, hnoos, mob ntsws interstitial mob * (* hauv lub sijhawm tom qab kev tshaj tawm ntawm kev siv, cov mob ntawm mob ntsws interstitial tau piav qhia, muaj kev txuas ib ntus nrog telmisartan. Txawm li cas los xij, tsis muaj kev sib raug zoo nrog kev siv telmisartan. tau ntsia lawm).
• Kev mob plab zom mov: mob plab, mob plab zom mov, lub qhov ncauj qhuav ntawm lub plab, dyspepsia, pom lub cev, mob plab, ntuav, saj tsis meej (tsis nco qab), ua rau lub siab ua haujlwm / mob siab rau daim siab * (* raws li kev soj ntsuam tom qab kev tshaj tawm hauv feem ntau cov teeb meem ntawm cov neeg muaj mob lub siab ua haujlwm / mob siab rau lub siab tau qhia hauv cov neeg nyob hauv Nyij Pooj).
• Kev mob xiam oob qhab los ntawm cov leeg nqaij thiab pob qij txha txuas: mob pob txha caj qaum, mob nraub qaum, mob pob txha (mob plab ntawm cov leeg), mob hauv qab qis dua, mob myalgia, mob leeg (cov tsos mob zoo ib yam li cov tsos mob txha caj qaum).
• Kev tsis haum xeeb los ntawm lub raum thiab lub raum: tso rau lub raum khiav tsis zoo, suav nrog mob raum tsis ua haujlwm.
• Kev cuam tshuam dav dav thiab cuam tshuam ntawm qhov chaw txhaj tshuaj: mob hauv siab, mob khaub thuas zoo li mob, tsis muaj zog.
• Cov ntaub ntawv kuaj thiab cov khoom siv: txo qis ntawm hemoglobin, kev nce siab ntawm uric acid, creatinine hauv ntshav ntshav, nce ntxiv hauv kev ua haujlwm ntawm "daim siab" enzymes, creatine phosphokinase (CPK) hauv ntshav plasma, hyperkalemia, hypoglycemia (hauv cov neeg mob ntshav qab zib mellitus).

Kev cuam tshuam nrog lwm yam tshuaj

Telmisartan yuav nce ntxiv cov txiaj ntsig antihypertensive ntawm lwm cov tshuaj tiv thaiv antihypertensive. Lwm hom kev sib txuam ntawm cov tseem ceeb hauv chaw kho mob tsis tau txheeb xyuas.

Siv cov tshuaj yooj yim nrog digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, simvastatin thiab amlodipine tsis ua rau muaj kev sib txuam hauv chaw kho mob. Ib qho kev nce siab hauv nruab nrab cov concentration ntawm digoxin hauv ntshav ntshav los ntawm qhov nruab nrab ntawm 20% (hauv ib kis, los ntawm 39%). Nrog rau kev siv tib lub sijhawm ntawm telmisartan thiab digoxin, nws raug nquahu kom qee lub sijhawm txiav txim siab qhov concentration ntawm digoxin hauv cov ntshav ntshav.

Zoo li lwm cov tshuaj ua rau ntawm renin-angiotensin-aldosterone system (RAAS), kev siv cov tshuaj telmisartan tuaj yeem ua rau hyperkalemia (saib ntu "Cov lus qhia tshwj xeeb"). Txoj kev pheej hmoo yuav nce ntxiv yog siv ib txhij nrog lwm cov tshuaj, uas tuaj yeem ua rau kev loj hlob ntawm hyperkalemia (muaj cov ntsev hloov pauv, potassium-sparing diuretics, ACE inhibitors, ARA II, tsis siv tshuaj tiv thaiv tsis haum tshuaj NSAIDs, suav nrog kev xaiv cyclooxygenase-2 inhibitors | COX-2 | txhaj tshuaj tiv thaiv cyclosporine lossis tacrolimus thiab trimethoprim.

Kev txhim kho ntawm hyperkalemia nyob ntawm concomitant txaus ntshai yam. Txoj kev pheej hmoo kuj nce ntxiv nyob rau thaum muaj kev sib txig siv cov kev sib txuas saum toj saud. Hauv tshwj xeeb, qhov kev pheej hmoo yog tshwj xeeb tshaj yog thaum siv tib lub sijhawm nrog cov tshuaj potassium-sparing diuretics, zoo li nrog rau cov ntsev ntxiv ntsev uas muaj ntsev hloov. Piv txwv li, siv cov tshuaj tsis haum nrog ACE inhibitors lossis NSAIDs yuav muaj kev pheej hmoo tsawg yog tias ceev faj txog kev ceev faj. ARA II, xws li telmisartan, txo cov poov tshuaj tsis qab thaum siv tshuaj kho. Kev siv cov tshuaj potassium-sparing diuretics, piv txwv li, spironolactone, eplerenone, triamteren lossis amiloride, cov tshuaj ntxiv los yog cov ntsev ntxiv ntsev tuaj yeem ua rau muaj qhov nce ntxiv ntawm cov poov tshuaj potassium. Kev siv tib txhij ntawm cov ntawv sau tseg hypokalemia yuav tsum tau siv nrog ceev faj thiab nrog kev saib xyuas cov poov tshuaj hauv ntshav ntshav. Nrog kev siv tib lub sijhawm ntawm telmisartan thiab ramipril, qhov nce 2.5-qhov nce ntawm AUC0-24 thiab Cmax ntawm ramipril thiab ramipril tau pom. Cov kab mob tseem ceeb hauv qhov tshwm sim no tsis tau teeb tsa. Nrog kev siv ACE inhibitors thiab lithium npaj txhij, qhov kev cuam tshuam thim rov qab ntawm cov ntsiab lus lithium hauv ntshav tau pom, nrog cov tshuaj lom. Tsis tshua muaj xwm txheej, cov kev hloov pauv no tau tshaj tawm nrog ARA II thiab lithium npaj. Nrog tib lub sijhawm siv cov roj ntsha lithium thiab ARA II, nws raug nquahu kom txiav txim siab cov ntsiab lus ntawm lithium hauv cov ntshav ntshav. Kev kho mob ntawm NSAIDs, suav nrog acetylsalicylic acid, COX-2, thiab tsis xaiv tshuaj NSAIDs, tuaj yeem ua rau mob raum tsis ua haujlwm hauv cov neeg mob lub cev qhuav dej. Cov yeeb yaj kiab ua yeeb yam ntawm RAAS yuav muaj qhov tshwm sim synergistic. Hauv cov neeg mob uas tau txais NSAIDs thiab telmisartan, bcc yuav tsum tau them nyiaj rau thaum pib kho thiab lub raum rov qab saib xyuas. Siv ib qho tsis haum nrog aliskiren hauv cov neeg mob ntshav qab zib mellitus lossis mob me mus rau lub raum tsis ua haujlwm (glomerular pom GFR