Telmista 80 mg - litaelo tsa tšebeliso

Telmista 80 mg - sethethefatsi sa antihypertensive, mohanyetsi ea itseng oa li-receptors tsa angiotensin II (mofuta oa AT1).

Letlapa le le leng la 80 mg:

Motsoako o sebetsang: Telmisartan 80.00 mg

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

Letlapa 80 mg: Capsule e bopehileng joaloka sebopeho, biconvex ea 'mala o mosoeu kapa o batlang o le tšoeu.

Mofumahali

Telmisartan ke "antiantensin II" receptor antagonist e ikhethang (mofuta oa AT1), e sebetsang ha e nkuoa ka molomo. E na le kamano e phahameng bakeng sa li-receptors tsa II1 tsa angiotensin II, tseo ka tsona ketso ea angiotensin II e fumanehang. Displaces angiotensin II ho tloha khokahanong le li-receptor, e se na ts'ebetso ea agonist e amanang le receptor ena. Telmisartan e tlama feela ho li-subtype tsa AT1 tsa li-angiotensin II receptors. Khokahano e ntse e tsoela pele. Ha e na kamano ea li-receptor tse ling, ho kenyelletsa li-receptor tsa AT2 le li-receptor tse ling tse ithutoang tsa angiotensin. Bohlokoa bo sebetsang ba li-receptor tsena, hammoho le phello ea ho tsosa ha tsona ho fetelletseng ka angiotensin II, mohopolo oa eona o eketsehang ka ts'ebeliso ea telmisartan, ha e so ithutoe. E fokotsa bongata ba aldosterone ho plasma ea mali, ha e thibele renin ka har'a plasma ea mali le lits'elo tsa li-ion block. Telmisartan ha e thibele angiotensin e fetolang enzyme (ACE) (kininase II) (enzyme eo hape e theolang bradykinin). Ka hona, keketseho ea litlamorao tse bakoang ke bradykinin ha e lebelloe.

Ho bakuli, telmisartan ka tekanyo ea 80 mg e thibela ka botlalo phello ea khatello ea mali ea angiotensin II. Ho qala ha ts'ebetso ea antihypertensive ho bonoa nakong ea lihora tse 3 kamora ts'ebetso ea pele ea telmisartan. Tšusumetso ea lithethefatsi e tsoela pele lihora tse 24 mme e lula e le bohlokoa ho fihlela lihora tse 48. Phello e phatlalalitsoeng ea antihypertensive hangata e hlaha ka mor'a libeke tse 4 ho8 tsa taolo e tloaelehileng ea telmisartan.

Ho bakuli ba nang le khatello ea mali ea methapo, telmisartan lowers systolic le diastolic khatello ea mali (BP) ntle le ho ama sekhahla sa pelo (HR).

Tabeng ea ho hlakoloa ha telmisartan ka tšohanyetso, butle-butle khatello ea mali e khutlela boemong ba eona ba pele ntle le nts'etsopele ea "ho hula" lefu.

Mofumahali

Ha e nooa ka molomo, e kenella ka potlako ho tsoa mokokotlong oa mpa (GIT). Bioavailability ke 50%. Ho fokotseha ha AUC (sebaka se tlas'a mochini oa nako ea mahloriso) le tšebeliso ea nako e tšoanang ea telmisartan ka lijo ho tloha ho 6% (ka tekanyo ea 40 mg) ho 19% (ka tekanyo ea 160 mg). Lihora tse 3 ka mor'a ho kenella, ho kenella ka bongata plasma ea mali ho lutlisoe ho sa tsotelehe nako ea ho ja. Ho na le phapang lipapisong tsa plasma ho banna le basali. Khatiso e phahameng ka ho fetisisa (Cmax) ho plasma ea mali le AUC ho basali ha e bapisoa le banna e ne e le makhetlo a 3 le a mabeli, ka ho latellana (ntle le phello e kholo ea katleho).

Puisano le liprotheine tsa plasma ea mali - 99,5%, haholo-holo ka albin le alpha-1 glycoprotein.

Boleng bo bohareng ba bophahamo bo bonahalang ba thomello ea mahloriso a lekanang ke lilithara tse 500. E tšelisoa ke khokahano le glucuronic acid. Metabolites ha e sebetse ka mokhoa oa meriana. Half-life (T1 / 2) e feta lihora tse 20. E pepisoa haholo ka popelong ka popelong ka tsela e sa fetoheng le ka liphio - ka tlase ho 2% ea lethal dose e nkuoeng. Tlhahiso e hlakileng ea plasma e phahame (900 ml / min), empa ha e bapisoa le phallo ea mali ea "hepatic" (hoo e ka bang 1500 ml / min).

Contraindication

Contraindication ts'ebelisong ea moriana oa Telmista:

Hypersensitivity ho ntho e sebetsang kapa ba fumanang lithethefatsi.
Boimana
Nako ea ho anyesa.
Maloetse a kotsi a pampiri ea biliary.
Tšenyehelo e matla ea hepatic (Karolelano ea bana-Pugh C).
Tšebeliso e kopanetsoeng le aliskiren ho bakuli ba nang le lefu la tsoekere kapa ka mokhoa o leka-lekaneng ho isa ho sebetseng hantle ha renal (tekanyo ea filtration ea glomerular (GFR)

Litlamorao

Maemo a hlokometsoeng a litlamorao a ne a sa tsamaellane le bong, lilemo kapa mofuta oa bakuli.

Maloetse a tšoaetsanoang le a tšoaetsanoang: sepsis, ho kenyelletsa le sepsis e bolaeang, tšoaetso ea pampitšana ea urine (ho kenyelletsa le cystitis), tšoaetso ea pampiri ea phefumoloho e holimo.
Mathata a tsoang tsamaisong ea mali le ea li-lymphatic: anemia, eosinophilia, thrombocytopenia.
Mathata a tsoang tsamaisong ea 'mele ea ho itšireletsa mafung: anaphylactic reaction, hypersensitivity (erythema, urticaria, angioedema), eczema, ho hlohlona, lekhopho la letlalo (ho kenyeletsa le lithethefatsi), angioedema (ka sephetho se bolaeang), hyperhidrosis, lekhopho le kotsi la letlalo.
Ho tlosoa hoa tsamaiso ea methapo: ho tšoenyeha, ho hloka boroko, khatello ea maikutlo, ho akheha, vertigo.
Mathata a amanang le setho sa pono: Ho ferekana hoa pono.
Ho tlosoa ha pelo: bradycardia, tachycardia.
Ho tlotsoa ha methapo ea mali: ho fokotseha hoa khatello ea mali, hypotension ea orthostatic.
Mathata a ts'ebetso ea ho hema, litho tsa ka sefubeng le mediastinum: ho hema hanyane, ho khohlela, lefu la matšoafo a mahareng * (* nakong ea thekiso ea kamora ts'ebeliso, linyeoe tsa lefu la matšoafo la nakoana li hlalositsoe, ka kamano ea nakoana le telmisartan. e kentsoe).
Mathata a amanang le ho ja ka mpeng: bohloko ba ka mpeng, lets'ollo, mucosa o omileng oa molomo, dyspepsia, flatulence, ho hlonama ka mpeng, ho hlatsa, ho kheloha letsoalo (dysgeusia), ts'ebetso ea ho senyeha ha sebete / lefu la sebete: (* ho latela liphetho tsa ho bona kamora ho bapatsa ka bongata linyeoe tsa ho senyeha ha tšebetso ea sebete / lefu la sebete li fumanoe ho baahi ba Japane).
Mathata a tsoang masikeng a masculoskeletal le a hokahaneng: arthralgia, bohloko ba mokokotlo, mesifa ea mesifa (mesifa ea mesifa ea namane), bohloko bo lipheletsong tse tlase, myalgia, tendon pain (matšoao a tšoanang le ponahatso ea tendonitis).
Lits'oaetso tse tsoang lipelong le mochine oa ho ntša metsi: ts'ebetso ea ho hlonepha ha a tsoeroe ke mokokotlo, ho kenyelletsa le ho hloleha ho sa sebetseng hantle ha retso.
Mathata le mathata a fumanehang setsing sa ente: bohloko ba sefuba, lefu la sefuba, bofokoli bo akaretsang.
Lintlha tsa laboratori le tsa ts'ebetso: ho fokotseha ha hemoglobin, keketseho ea bongata ba uric acid, creatinine ho plasma ea mali, keketseho ea ts'ebetso ea li-enzymes tsa "sebete", creatine phosphokinase (CPK) ho plasma ea mali, hyperkalemia, hypoglycemia (ho bakuli ba nang le lefu la tsoekere mellitus).

Ho sebelisana le lithethefatsi tse ling

Telmisartan e ka eketsa phello ea antihypertensive ea lithethefatsi tse ling tsa antihypertensive. Mefuta e meng ea litšebelisano tsa bohlokoa ba tliliniki ha e so tsejoe.

Tšebeliso e kopanetsoeng le digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, simvastatin le amlodipine ha e lebise tšebelisanong e kholo ea kliniki. Keketseho e tšoaeang ho karolelano ea kakaretso ea digoxin ho plasma ea mali ka karolelano ea 20% (boemong bo le bong, ka 39%). Ka tšebeliso e tšoanang ea telmisartan le digoxin, ho bohlokoa hore nako le nako ho tsebe hore na digoxin li ka bongata ka plasma ea mali.

Joalo ka lithethefatsi tse ling tse sebelisang lenaneo la renin-angiotensin-aldosterone (RAAS), tšebeliso ea telmisartan e ka baka hyperkalemia (bona karolo ea "Litaelo tse Khethehileng"). Kotsi e ka eketseha maemong a ts'ebeliso e le 'ngoe le lithethefatsi tse ling, tse ka bakang le nts'etsopele ea hyperkalemia (e nang le litsi tsa letsoai tsa potasiamo, li-diuretics tsa potasiamo, li-ACE inhibitors, ARA II, lithethefatsi tse seng tsa antiidalidal NSAIDs, ho kenyelletsa le cycloo oxygenase-2 | TsOGG-2 | li-immunosuppressants cyclosporine kapa tacrolimus le trimethoprim.

Nts'etsopele ea hyperkalemia e ipapisitse le maemo a kotsi a kopaneng. Kotsi e boetse e eketseha ha ho sebelisoa ka nako e le 'ngoe metsoako e kaholimo. Ka ho khetheha, menyetla e kotsing e phahameng haholo ha e sebelisoa ka nako e le 'ngoe le li-diuretics tse nang le potasiamo, hammoho le tse nkiloeng ka letsoai la potasiamo. Mohlala, tšebeliso e kopanetsoeng le li-inhibitors tsa ACE kapa NSAID ha e na kotsi e fokolang haeba ho nkuoa mehato e tiileng ea ho nka mehato. ARA II, joalo ka telmisartan, e fokotsa tahlehelo ea potasiamo nakong ea kalafo ea diuretic. Ts'ebeliso ea diuretics ea potasiamo e sa sebeliseng potoloho, ka mohlala, spironolactone, eplerenone, triamteren kapa amiloride, li-additives tse nang le potasiamo kapa tse ling tsa potasiamo tse nang le potasiamo li ka lebisa keketseho e kholo ea serum potasiamo. Ts'ebeliso e tšoanang ea "hypokalemia" e ngotsoeng e lokela ho sebelisoa ka hloko le ka ho lekola potasiamo ka bongata lero la mali. Ka tšebeliso e tšoanang ea telmisartan le ramipril, keketseho e habeli ho 2 ho AUC0-24 le Cmax ea ramipril le ramipril e hlokometsoe. Bohlokoa ba bongaka ba ketsahalo ena ha bo e-so fumanoe. Ka tšebeliso e tšoanang ea li-inhibitors tsa ACE le litokisetso tsa lithium, keketseho e khutlisetsang ea litaba tsa lithium ea plasma e ile ea bonoa, e tsamaea le litlamorao tse mpe. Maemong a sa tloaelehang, liphetoho tse joalo li tlalehiloe ka ARA II le litokisetso tsa lithium. Ka tšebeliso e tšoanang ea lithium le ARA II, ho khothalletsoa ho tseba se kahare sa lithium ho plasma ea mali. Phekolo ea li-NSAIDs, ho kenyelletsa acetylsalicylic acid, COX-2, le NSAIDs e seng khetho, e ka baka ho hloleha ho matla ha renal ho bakuli ba nang le metsi. Lithethefatsi tse sebelisang RAAS li ka ba le phello ea synergistic. Ho bakuli ba fumanang li-NSAIDs le telmisartan, bcc e lokela ho lefshoa qalong ea kalafo le ts'ebetso ea ho beleha e behiloe leihlo. Tšebeliso e kopanetsoeng le aliskiren ho bakuli ba nang le lefu la tsoekere kapa ka tekanyo e itseng ho isa ho matla ho sebetsaneng ha lere (glomerular filtration rate ea GFR)