Olmesartan Medoxomil

Dosage form: ntsiav tshuaj, zaj duab xis coated
Chav kawm tshuaj: Angiotensin receptor blockers

Ntawm nplooj ntawv no

• Boxed Warning
• Indications thiab siv
• Dosage thiab Administration
• Daim ntawv siv tshuaj thiab muaj zog
• Contraindications
• Ceeb toom thiab ceev faj
• Cov Kev Phem Tsis Zoo/Sib Phem
• Kev Sib Tham Tshuaj
• Siv nyob rau hauv cov neeg tshwj xeeb
• Kev noj ntau dhau
• Kev piav qhia
• Clinical Pharmacology
• Nonclinical Toxicology
• Kev tshawb fawb soj ntsuam
• Yuav Ua Li Cas Muab / Cia thiab tuav
• Cov Ntaub Ntawv Qhia Txog Tus Neeg Mob

• Thaum kuaj pom cev xeeb tub, txiav tawm Olmesartan Medoxomil ntsiav tshuaj sai li sai tau (5.1, 8.1).
• Cov tshuaj uas ua ncaj qha rau ntawm renin-angiotensin system tuaj yeem ua rau raug mob thiab tuag rau tus menyuam hauv plab (5.1, 8.1).

Cov lus qhia thiab kev siv rau Olmesartan Medoxomil

Olmesartan Medoxomil ntsiav tshuaj, USP tau qhia rau kev kho mob ntshav siab hauv cov neeg laus thiab menyuam yaus hnub nyoog 6 xyoo thiab laus dua, txhawm rau txo cov ntshav siab. Txo cov ntshav siab txo qhov kev pheej hmoo ntawm kev tuag thiab tsis tuag ntawm cov hlab plawv, feem ntau mob strokes thiab myocardial infarctions. Cov txiaj ntsig no tau pom nyob rau hauv kev tswj hwm kev sim tshuaj tiv thaiv kab mob los ntawm ntau yam ntawm cov chav kawm pharmacological suav nrog cov chav kawm uas cov tshuaj no koom nrog. Tsis muaj kev tswj xyuas kev sim ua pov thawj txo qis kev pheej hmoo nrog Olmesartan Medoxomil ntsiav tshuaj, USP.

Kev tswj cov ntshav siab yuav tsum yog ib feem ntawm kev tswj hwm kev pheej hmoo ntawm cov hlab plawv, suav nrog, raws li qhov tsim nyog, kev tswj lipid, tswj ntshav qab zib, kev kho tshuaj tiv thaiv, kev haus luam yeeb, kev tawm dag zog, thiab kev siv sodium tsawg. Ntau tus neeg mob yuav xav tau ntau tshaj ib qho tshuaj kom ua tiav cov hom phiaj ntshav siab. Rau cov lus qhia tshwj xeeb ntawm cov hom phiaj thiab kev tswj hwm, saib cov lus qhia tshaj tawm, xws li cov Kev Pabcuam Kev Kawm Ntshav Siab Hauv Lub Tebchaws Lub Koom Haum Koom Tes Hauv Tebchaws ntawm Kev Tiv Thaiv, Kev Tshawb Fawb, Kev Ntsuas, thiab Kev Kho Mob Ntshav Siab (JNC).

Ntau cov tshuaj tiv thaiv kab mob siab, los ntawm ntau yam ntawm cov chav kawm pharmacologic thiab nrog cov txheej txheem sib txawv ntawm kev ua, tau pom nyob rau hauv randomized tswj kev sim los txo cov hlab plawv thiab kev tuag, thiab nws tuaj yeem xaus lus tias nws yog ntshav txo, thiab tsis yog lwm yam khoom siv tshuaj kho mob. cov tshuaj, uas yog lub luag haujlwm loj rau cov txiaj ntsig. Qhov txiaj ntsig zoo tshaj plaws thiab zoo tshaj plaws ntawm cov hlab plawv yog qhov txo qis ntawm kev pheej hmoo ntawm mob stroke, tab sis kev txo qis hauv myocardial infarction thiab cov hlab plawv tuag kuj tau pom tsis tu ncua.

Qhov siab systolic lossis diastolic siab ua rau muaj kev pheej hmoo ntawm cov hlab plawv, thiab qhov kev pheej hmoo ntawm ib mmHg yog ntau dua ntawm cov ntshav siab, yog li txawm tias qhov txo qis ntawm cov ntshav siab tuaj yeem muab txiaj ntsig zoo. Cov txheeb ze kev pheej hmoo txo ​​qis los ntawm kev txo cov ntshav siab yog zoo ib yam nyob rau hauv cov pej xeem uas muaj kev pheej hmoo sib txawv, yog li cov txiaj ntsig zoo yog ntau dua rau cov neeg mob uas muaj kev pheej hmoo siab dua ntawm lawv cov ntshav siab (piv txwv li, cov neeg mob ntshav qab zib lossis hyperlipidemia), thiab cov neeg mob zoo li no yuav xav tau. kom tau txais txiaj ntsig los ntawm kev kho mob hnyav dua mus rau lub hom phiaj txo cov ntshav siab.

Qee cov tshuaj antihypertensive muaj cov teebmeem me me hauv cov ntshav siab (raws li kev kho mob monotherapy) hauv cov neeg mob dub, thiab ntau cov tshuaj tiv thaiv hypertensive muaj kev pom zoo ntxiv thiab cov teebmeem (xws li, ntawm angina, plawv tsis ua haujlwm, lossis mob ntshav qab zib raum). Cov kev txiav txim siab no tuaj yeem coj kev xaiv kev kho mob.

Nws tuaj yeem siv ib leeg lossis ua ke nrog lwm cov tshuaj tiv thaiv hypertensive.

Olmesartan Medoxomil Dosage thiab Kev Tswj Xyuas

Cov neeg laus mob ntshav siab

Kev noj tshuaj yuav tsum yog tus kheej. Qhov ib txwm pom zoo pib koob tshuaj ntawm Olmesartan Medoxomil ntsiav tshuaj yog 20 mg ib hnub ib zaug thaum siv los ua kev kho mob monotherapy hauv cov neeg mob uas tsis ntim cov ntawv cog lus. Rau cov neeg mob xav tau kev txo qis hauv cov ntshav siab ntxiv tom qab 2 lub lis piam ntawm kev kho, koob tshuaj Olmesartan Medoxomil tuaj yeem nce mus txog 40 mg. Cov koob tshuaj ntau dua 40 mg tsis pom tias muaj txiaj ntsig zoo dua. Kev noj ob zaug ib hnub twg tsis muaj txiaj ntsig zoo dua li tib cov koob tshuaj tag nrho ib zaug ib hnub.

Rau cov neeg mob uas muaj peev xwm depletion ntawm intravascular ntim (piv txwv li, cov neeg mob kho nrog diuretics, tshwj xeeb tshaj yog cov neeg uas lub raum tsis ua hauj lwm), pib Olmesartan Medoxomil ntsiav tshuaj nyob rau hauv kev saib xyuas kev kho mob nyob ze thiab muab kev txiav txim siab rau kev siv ntawm ib tug qis pib koob tshuaj.[saib Ceeb toom thiab ceev faj (5.3) ].

Pediatric Hypertension (hnub nyoog 6 xyoos thiab laus dua)

Kev noj tshuaj yuav tsum yog tus kheej. Rau cov menyuam yaus uas nqos tau cov ntsiav tshuaj, ib txwm pom zoo pib noj tshuaj Olmesartan Medoxomil ntsiav tshuaj yog 10 mg ib hnub ib zaug rau cov neeg mob hnyav 20 txog 20.<35 kg (44 to 77 lb), or 20 mg once daily for patients who weigh ≧35 kg. For patients requiring further reduction in blood pressure after 2 weeks of therapy, the dose of Olmesartan Medoxomil tablets may be increased to a maximum of 20 mg once daily for patients who weigh <35 kg or 40 mg once daily for patients who weigh ≧35 kg.

Kev siv cov ntsiav tshuaj Olmesartan Medoxomil hauv cov menyuam yaus<1 year of age is not recommended [saib Ceeb toom thiab ceev faj (5.2) thiab Siv hauv Cov Pej Xeem Tshwj Xeeb (8.4) ].

Rau cov menyuam yaus uas nqos tsis tau cov ntsiav tshuaj, tib koob tuaj yeem muab tau los ntawm kev ncua kev ncua ntev raws li tau piav qhia hauv qab no[saib Clinical Pharmacology (12.3) ].

Ua raws li cov lus qhia txog kev ncua kev ncua hauv qab no los tswj Olmesartan Medoxomil ntsiav tshuaj raws li kev ncua.

Kev npaj ntawm Suspension (rau 200 mL ntawm 2 mg / mL ncua kev kawm)

Ntxiv 50 mL ntawm Purified Dej rau hauv amber polyethylene terephthalate (PET) lub raj mis uas muaj nees nkaum Olmesartan Medoxomil ntsiav tshuaj 20 mg ntsiav tshuaj thiab tso cai rau sawv ntsug li 5 feeb. Co lub thawv rau tsawg kawg yog 1 feeb thiab tso cai rau kev ncua ntev li 1 feeb. Rov ua 1-feeb co thiab 1-feeb sawv ntsug rau plaub zaug ntxiv. Ntxiv 100 mL ntawm ORA-Sweet®thiab 50 mL ntawm ORA-Plus® ib mus rau qhov ncua sij hawm thiab co zoo rau yam tsawg 1 feeb. Qhov kev ncua yuav tsum tau muab tso rau hauv tub yees ntawm 2-8 ° C (36-46 ° F) thiab tuaj yeem khaws cia ntev txog 4 lub lis piam. Co lub ncua kev kawm ntawv zoo ua ntej siv thiab rov qab mus rau lub tub yees kom sai.

ib

ORA-Sweet ® thiab ORA-Plus ® yog cov cim lag luam ntawm Paddock Laboratories, Inc.

Daim ntawv siv tshuaj thiab muaj zog

• 5 mg dawb los yog yuav luag dawb round zaj duab xis-coated ntsiav tshuaj, debossed L20 ntawm ib sab thaum dawb paug ntawm sab nraud.
• 20 mg dawb los yog yuav luag dawb puag ncig zaj duab xis-coated ntsiav tshuaj, debossed L18 ntawm ib sab thaum dawb paug ntawm lwm sab.
• 40 mg dawb los yog yuav luag dawb round zaj duab xis-coated ntsiav tshuaj, debossed L17 ntawm ib sab thaum dawb paug ntawm lwm sab.

Contraindications

Tsis txhob noj aliskiren nrog Olmesartan Medoxomil ntsiav tshuaj hauv cov neeg mob ntshav qab zib[saib Kev sib tham nrog tshuaj (7.3) ].

Ceeb toom thiab ceev faj

Fetal Toxicity

Cov ntsiav tshuaj Olmesartan Medoxomil tuaj yeem ua rau muaj kev phom sij rau menyuam hauv plab thaum siv rau tus poj niam cev xeeb tub. Kev siv cov tshuaj uas ua rau renin-angiotensin system (RAS) thaum lub sij hawm thib ob thiab thib peb lub hlis twg ntawm cev xeeb tub yuav txo tau lub raum ua haujlwm ntawm lub raum thiab ua rau cov fetal thiab neonatal morbidity thiab tuag. Qhov tshwm sim oligohydramnios tuaj yeem cuam tshuam nrog fetal ntsws hypoplasia thiab pob txha deformations. Tej yam tshwm sim tsis zoo ntawm cov menyuam mos muaj xws li pob txha taub hau hypoplasia, anuria, hypotension, lub raum tsis ua haujlwm, thiab tuag. Thaum kuaj pom cev xeeb tub, txiav tawm Olmesartan Medoxomil kom sai li sai tau[saib Siv hauv Cov Pej Xeem Tshwj Xeeb (8.1) ].

Mob ntshav qab zib hauv cov menyuam mos

Kev siv cov ntsiav tshuaj Olmesartan Medoxomil hauv cov menyuam yaus<1 year of age is not recommended. Drugs that act directly on the renin-angiotensin-aldosterone system (RAAS) can have effects on the development of immature kidneys [saib Siv hauv Cov Pej Xeem Tshwj Xeeb (8.4) ].

Hypotension nyob rau hauv Volume- los yog ntsev-Depleted neeg mob

Hauv cov neeg mob uas muaj cov kab mob activated renin-angiotensin-aldosterone, xws li ntim- thiab/los yog cov neeg mob ntsev-depleted (xws li, cov uas tau kho nrog cov tshuaj diuretics siab), cov tsos mob ntawm hypotension yuav xav tau tom qab pib kho nrog Olmesartan Medoxomil. Pib kev kho mob nyob rau hauv kev saib xyuas kev noj qab haus huv nyob ze thiab xav txog pib ntawm koob tshuaj qis dua. Yog tias hypotension tshwm sim, muab tus neeg mob tso rau hauv lub supine txoj hauj lwm thiab, yog tias tsim nyog, muab cov tshuaj infusion ntawm ib txwm saline.[saib Dosage thiab Administration (2.1) ]. Ib qho kev hloov pauv hypotensive tsis yog ib qho contraindication rau kev kho mob ntxiv, uas feem ntau tuaj yeem txuas ntxiv yam tsis muaj teeb meem thaum cov ntshav siab tau ruaj khov.

Lub raum tsis ua haujlwm

Raws li qhov tshwm sim ntawm inhibiting renin-angiotensin-aldosterone system, cov kev hloov hauv lub raum kev ua haujlwm yuav xav tias yuav raug rau cov neeg raug kho nrog Olmesartan Medoxomil. Hauv cov neeg mob uas lub raum ua haujlwm tuaj yeem nyob ntawm kev ua haujlwm ntawm renin-angiotensin-aldosterone system (xws li, cov neeg mob uas muaj lub plawv tsis ua haujlwm hnyav), kev kho mob nrog angiotensin converting enzyme (ACE) inhibitors thiab angiotensin receptor antagonists tau cuam tshuam nrog oliguria thiab / lossis Kev loj hlob azotemia thiab tsis tshua muaj mob raum tsis ua haujlwm thiab / lossis tuag. Cov txiaj ntsig zoo sib xws yuav raug cia siab hauv cov neeg mob kho nrog Olmesartan Medoxomil[saib Dosage thiab Administration (2.1) , Kev sib tham nrog tshuaj (7.3) , Siv hauv Cov Pej Xeem Tshwj Xeeb (8.7) thiab Clinical Pharmacology (12.3) ].

Hauv kev tshawb fawb ntawm ACE inhibitors nyob rau hauv cov neeg mob uas muaj unilateral los yog ob sab lub raum hlab ntsha stenosis, nce nyob rau hauv cov ntshav creatinine los yog ntshav urea nitrogen (BUN) tau tshaj tawm. Tsis tau siv sijhawm ntev ntawm Olmesartan Medoxomil hauv cov neeg mob uas muaj kev sib koom ua ke lossis ob tog lub raum hlab ntsha stenosis, tab sis cov txiaj ntsig zoo sib xws yuav xav tau.

Sprue zoo li Enteropathy

Mob hnyav, mob raws plab nrog qhov hnyav hnyav tau raug tshaj tawm nyob rau hauv cov neeg mob noj olmesartan hli mus rau xyoo tom qab pib siv tshuaj. Txoj hnyuv biopsies ntawm cov neeg mob feem ntau pom tau tias villous atrophy. Yog tias tus neeg mob tsim cov tsos mob no thaum kho nrog olmesartan, tsis suav nrog lwm yam etiologies. Xav txog lwm txoj kev kho mob ntshav siab hauv cov xwm txheej uas tsis muaj lwm yam etiology raug txheeb xyuas.

Hyperkalemia

Serum potassium yuav tsum tau saib xyuas hauv cov neeg mob uas tau txais Olmesartan Medoxomil ntsiav tshuaj. Cov tshuaj uas inhibit renin angiotensin system tuaj yeem ua rau hyperkalemia. Cov xwm txheej txaus ntshai rau kev txhim kho hyperkalemia suav nrog rau lub raum tsis txaus, ntshav qab zib mellitus, thiab kev siv cov tshuaj potassium-sparing diuretics, cov tshuaj potassium thiab / lossis cov tshuaj ntsev uas muaj cov tshuaj potassium.[saib Kev sib tham nrog tshuaj (7.3) ].

Kev Phem Tsis Zoo

Kev sim tshuaj ntsuam xyuas

Vim tias cov kev tshawb fawb soj ntsuam tau ua nyob rau hauv ntau yam sib txawv, cov tshuaj tiv thaiv tsis zoo tau pom nyob rau hauv kev tshawb fawb soj ntsuam ntawm cov tshuaj tsis tuaj yeem ncaj qha piv rau cov nqi hauv kev tshawb fawb soj ntsuam ntawm lwm cov tshuaj thiab tej zaum yuav tsis cuam tshuam cov nqi pom hauv kev xyaum.

Cov neeg laus mob ntshav siab

Olmesartan Medoxomil tau raug soj ntsuam rau kev nyab xeeb hauv ntau dua 3825 tus neeg mob / cov ncauj lus, suav nrog ntau dua 3275 tus neeg mob kho mob ntshav siab hauv kev sim tshuaj. Qhov kev paub no suav nrog txog 900 tus neeg mob tau kho tsawg kawg 6 lub hlis thiab ntau dua 525 rau tsawg kawg 1 xyoos. Cov xwm txheej feem ntau yog mob me, ntuav thiab tsis muaj kev sib raug zoo rau koob tshuaj Olmesartan Medoxomil.

Kev tshuaj xyuas ntawm poj niam txiv neej, hnub nyoog thiab haiv neeg pawg pom tsis muaj qhov sib txawv ntawm Olmesartan Medoxomil thiab cov neeg mob uas siv cov placebo. Tus nqi ntawm kev tshem tawm vim muaj kev cuam tshuam tsis zoo hauv txhua qhov kev sim ntawm cov neeg mob ntshav siab yog 2.4% (piv txwv li, 79/3278) ntawm cov neeg mob kho nrog Olmesartan Medoxomil thiab 2.7% (piv txwv li, 32/1179) ntawm cov neeg mob tswj. Hauv kev sim tshuaj placebo, tsuas yog qhov tshwm sim tsis zoo uas tshwm sim hauv ntau dua 1% ntawm cov neeg mob kho nrog Olmesartan Medoxomil thiab qhov tshwm sim ntau dua piv rau cov placebo yog kiv taub hau (3% vs. 1%).

Lub ntsej muag edema tau tshaj tawm hauv tsib tus neeg mob tau txais Olmesartan Medoxomil. Angioedema tau tshaj tawm nrog angiotensin II antagonists.

Pediatric Hypertension

Tsis muaj qhov sib txawv ntawm qhov sib txawv ntawm qhov tsis zoo ntawm qhov profile rau cov neeg mob menyuam yaus hnub nyoog 1 txog 16 xyoo thiab yav dhau los tau tshaj tawm rau cov neeg laus.

ntev npaum li cas hyoscyamine siv sijhawm ua haujlwm

Tom qab Kev Lag Luam Kev Lag Luam

Cov kev cuam tshuam tsis zoo hauv qab no tau tshaj tawm hauv kev ua lag luam tom qab. Vim tias cov tshuaj tiv thaiv no tau lees paub los ntawm cov pej xeem tsis paub meej qhov loj, nws tsis yog ib txwm ua tau kom ntseeg tau tias lawv cov zaus los yog tsim kom muaj kev sib raug zoo rau kev siv tshuaj.

Lub cev tag nrho:Asthenia, angioedema, anaphylactic cov tshuaj tiv thaiv

plab hnyuv:ntuav, sprue zoo li enteropathy[saib Ceeb toom thiab ceev faj (5.5) ]

Metabolic thiab Nutrition Disorders:Hyperkalemia

Musculoskeletal:Rhabdomyolysis

Urogenital System:Mob raum tsis ua haujlwm, nce ntshav creatinine

Daim tawv nqaij thiab Appendages:Alopecia, pruritus, urticaria

Cov ntaub ntawv los ntawm ib qho kev sim tswj thiab kev tshawb fawb txog kab mob kis tau qhia tias koob tshuaj olmesartan siab tuaj yeem ua rau muaj kev pheej hmoo mob plawv (CV) hauv cov neeg mob ntshav qab zib, tab sis cov ntaub ntawv tag nrho tsis muaj tseeb. Kev sim randomized, placebo-tswj, ob-dig muag ROADMAP sim (Randomized Olmesartan Thiab Diabetes MicroAlbuminuria Prevention trial, n=4447) tshuaj xyuas kev siv olmesartan, 40 mg txhua hnub, vs. placebo hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus, normoalbuminuria. tsawg kawg yog ib qho kev pheej hmoo ntxiv rau tus kab mob CV. Qhov kev sim tau ntsib nws thawj qhov kawg, ncua qhov pib ntawm microalbuminuria, tab sis olmesartan tsis muaj txiaj ntsig zoo rau kev poob qis hauv glomerular filtration rate (GFR). Muaj kev tshawb pom ntawm CV mortality (adjudicated sudden cardiac death, fatal myocardial infarction, fatal stroke, revascularization death) nyob rau hauv pawg olmesartan piv rau cov placebo pawg (15 olmesartan vs. 3 placebo, HR 4.9, 95% kev ntseeg siab interval [CI ], 1.4, 17), tab sis qhov kev pheej hmoo ntawm kev tsis tuag myocardial infarction yog qis dua nrog olmesartan (HR 0.64, 95% CI 0.35, 1.18).

Txoj kev tshawb nrhiav kab mob kis tau suav nrog cov neeg mob hnub nyoog 65 xyoo thiab laus dua nrog rau tag nrho cov kis ntawm> 300,000 tus neeg mob-xyoo. Hauv pab pawg neeg mob ntshav qab zib uas tau txais koob tshuaj olmesartan (40 mg / d) rau > 6 lub hlis, pom tias muaj kev pheej hmoo tuag ntau ntxiv (HR 2.0, 95% CI 1.1, 3.8) piv rau cov neeg mob zoo sib xws noj lwm yam. Cov tshuaj angiotensin receptor blockers. Hauv qhov sib piv, kev siv cov tshuaj olmesartan siab hauv cov neeg mob uas tsis muaj ntshav qab zib tau tshwm sim los cuam tshuam nrog kev pheej hmoo ntawm kev tuag (HR 0.46, 95% CI 0.24, 0.86) piv rau cov neeg mob zoo sib xws uas noj lwm cov tshuaj angiotensin receptor blockers. Tsis muaj qhov sib txawv ntawm cov pab pawg tau txais koob tshuaj qis dua ntawm olmesartan piv rau lwm cov tshuaj angiotensin blockers lossis cov neeg tau txais kev kho mob.<6 months.

Zuag qhia tag nrho, cov ntaub ntawv no ua rau muaj kev txhawj xeeb ntawm qhov muaj peev xwm nce CV uas cuam tshuam nrog kev siv cov koob tshuaj olmesartan hauv cov neeg mob ntshav qab zib. Txawm li cas los xij, muaj kev txhawj xeeb nrog kev ntseeg siab ntawm kev tshawb nrhiav qhov kev pheej hmoo ntawm CV, tshwj xeeb tshaj yog kev soj ntsuam hauv kev tshawb fawb kab mob loj heev rau kev muaj sia nyob hauv cov neeg tsis muaj ntshav qab zib ntawm qhov loj me zoo ib yam li qhov tsis zoo hauv cov neeg mob ntshav qab zib.

Kev Sib Tham Tshuaj

Tus neeg sawv cev nce ntxiv cov tshuaj poov tshuaj

Kev siv olmesartan nrog rau lwm cov tshuaj uas thaiv cov kab mob renin-angiotensin, potassium-sparing diuretics (piv txwv li, spironolactone, triamterene, amiloride), potassium ntxiv, ntsev hloov pauv uas muaj cov poov tshuaj lossis lwm yam tshuaj uas tuaj yeem nce cov poov tshuaj (piv txwv li, heparin) tuaj yeem ua rau muaj kev phom sij. ua rau kom nce hauv cov poov tshuaj hauv cov ntshav. Yog tias kev siv tshuaj sib xyaw ua ke pom tau tias tsim nyog, kev saib xyuas cov ntshav cov poov tshuaj yog pom zoo.

Non-steroidal Anti-Inflammatory Agents xws li Selective Cyclooxygenase-2 Inhibitors (COX-2 Inhibitors)

Hauv cov neeg mob uas muaj hnub nyoog laus, ntim-depleted (nrog rau cov kev kho diuretic), lossis nrog rau lub raum tsis ua haujlwm, kev sib koom ua haujlwm ntawm NSAIDs, suav nrog kev xaiv COX-2 inhibitors, nrog angiotensin II receptor antagonists, suav nrog Olmesartan Medoxomil, tuaj yeem ua rau tsis zoo. ntawm lub raum ua haujlwm, suav nrog kev mob raum tsis ua haujlwm. Cov teebmeem no feem ntau yog thim rov qab. Saib xyuas lub raum ua haujlwm ib ntus hauv cov neeg mob uas tau txais Olmesartan Medoxomil thiab NSAID txoj kev kho.

Cov nyhuv antihypertensive ntawm angiotensin II receptor antagonists, suav nrog Olmesartan Medoxomil, tuaj yeem txo qis los ntawm NSAIDs suav nrog cov tshuaj COX-2 inhibitors.

Dual Blockade ntawm Renin-Angiotensin System (RAS)

Dual blockade ntawm RAS nrog angiotensin receptor blockers, ACE inhibitors, lossis aliskiren yog txuam nrog kev pheej hmoo ntawm hypotension, hyperkalemia, thiab kev hloov hauv lub raum ua haujlwm (xws li mob raum tsis ua haujlwm) piv rau monotherapy. Feem ntau cov neeg mob tau txais kev sib xyaw ntawm ob RAS inhibitors tsis tau txais txiaj ntsig ntxiv piv rau monotherapy. Feem ntau, zam kev siv RAS inhibitors ua ke. Ua tib zoo saib xyuas cov ntshav siab, lub raum ua haujlwm thiab cov electrolytes hauv cov neeg mob ntawm Olmesartan Medoxomil thiab lwm yam tshuaj uas cuam tshuam rau RAS.

Tsis txhob noj aliskiren nrog Olmesartan Medoxomil hauv cov neeg mob ntshav qab zib[saib Contraindications (4) ].Tsis txhob siv aliskiren nrog Olmesartan Medoxomil hauv cov neeg mob lub raum tsis zoo (GFR<60 ml/min).

Lithium

Kev nce hauv cov ntshav lithium concentrations thiab lithium toxicity tau tshaj tawm thaum lub sijhawm tswj hwm ntawm lithium nrog angiotensin II receptor antagonists, suav nrog Olmesartan Medoxomil ntsiav tshuaj. Saib xyuas cov ntshav lithium qib thaum siv sib xyaw.

Colesevelam Hydrochloride

Concurrent kev tswj hwm ntawm cov kua tsib kua qaub sequestering tus neeg sawv cev colesevelam hydrochloride txo qhov kev raug mob thiab ncov plasma concentration ntawm olmesartan. Kev tswj hwm ntawm olmesartan tsawg kawg yog 4 teev ua ntej colesevelam hydrochloride txo cov tshuaj cuam tshuam nrog cov tshuaj. Xav txog kev tswj hwm olmesartan tsawg kawg 4 teev ua ntej koob tshuaj colesevelam hydrochloride[saib Clinical Pharmacology (12.3) ].

Siv rau hauv cov neeg tshwj xeeb

Kev xeeb tub

Risk Summary

Cov ntsiav tshuaj Olmesartan Medoxomil tuaj yeem ua rau muaj kev phom sij rau menyuam hauv plab thaum siv rau tus poj niam cev xeeb tub. Kev siv cov tshuaj uas ua rau renin-angiotensin system thaum lub sij hawm thib ob thiab thib peb lub hlis twg ntawm cev xeeb tub yuav txo tau lub raum ua haujlwm ntawm lub raum thiab ua rau tus menyuam mos thiab cov menyuam mos thiab tuag. Feem ntau cov kev tshawb fawb txog kab mob kis tau tshuaj xyuas qhov txawv txav ntawm fetal tom qab raug siv los tiv thaiv kev mob ntshav siab hauv thawj peb lub hlis twg tsis tau txheeb xyuas cov tshuaj cuam tshuam rau renin-angiotensin system los ntawm lwm cov tshuaj tiv thaiv kab mob. Hauv kev tshawb fawb txog tsiaj yug me nyuam, Olmesartan Medoxomil ntsiav tshuaj kho thaum lub sij hawm organogenesis ua rau muaj zog embryofetal toxicity nyob rau hauv nas ntawm cov koob tshuaj tsawg dua li cov tshuaj lom niam txiv.

Thaum kuaj pom cev xeeb tub, txiav tawm Olmesartan Medoxomil ntsiav tshuaj sai li sai tau. Xav txog lwm txoj kev kho antihypertensive thaum cev xeeb tub.

Kev kwv yees keeb kwm yav dhau los ntawm kev yug me nyuam loj thiab nchuav menyuam rau cov pej xeem tsis paub. Txhua lub cev xeeb tub muaj keeb kwm muaj feem cuam tshuam txog kev yug menyuam, poob lossis lwm yam tshwm sim tsis zoo. Hauv Teb Chaws Asmeskas cov pej xeem, kwv yees keeb kwm kev pheej hmoo ntawm kev yug me nyuam loj thiab nchuav menyuam hauv kev kuaj mob pom zoo yog 2% -4% thiab 15% -20%, feem.

Kev txiav txim siab kho mob

Kab Mob-Associated Niam thiab/lossis Embryo/Fetal Risk

Kev kub ntxhov hauv cev xeeb tub ua rau muaj kev pheej hmoo rau leej niam rau pre-eclampsia, ntshav qab zib gestational, kev yug ntxov ntxov, thiab kev xeeb tub (xws li, xav tau kev phais thiab tom qab yug me nyuam). Kev kub siab ua rau muaj kev pheej hmoo ntawm fetal rau kev txwv kev loj hlob ntawm intrauterine thiab intrauterine tuag. Cov poj niam cev xeeb tub uas muaj ntshav siab yuav tsum tau ua tib zoo saib xyuas thiab tswj kom haum.

Fetal/Neonatal Adverse Reactions

Oligohydramnios hauv cov poj niam cev xeeb tub uas siv tshuaj cuam tshuam rau renin-angiotensin system hauv lub thib ob thiab peb lub hlis twg ntawm cev xeeb tub tuaj yeem ua rau cov hauv qab no: txo qis hauv lub raum ua haujlwm ua rau anuria thiab lub raum tsis ua haujlwm, fetal ntsws hypoplasia, skeletal deformations, nrog rau pob txha taub hau hypoplasia, hypotension. thiab tuag.

Hauv cov neeg mob noj cov ntsiav tshuaj Olmesartan Medoxomil thaum cev xeeb tub, ua qhov kev kuaj xyuas ultrasound los ntsuas qhov chaw nyob hauv lub cev. Kev kuaj fetal tej zaum yuav tsim nyog, raws li lub lim tiam ntawm cev xeeb tub. Cov neeg mob thiab cov kws kho mob yuav tsum paub, txawm li cas los xij, tias oligohydramnios yuav tsis tshwm sim kom txog thaum tom qab tus me nyuam hauv plab tau raug mob irreversible.

pregabalin siv rau dab tsi

Ua tib zoo saib cov menyuam mos nrog keeb kwm ntawmhauv uteroraug rau Olmesartan Medoxomil ntsiav tshuaj rau hypotension, oliguria, thiab hyperkalemia. Nyob rau hauv neonates nrog keeb kwm ntawmhauv uteroraug rau cov ntsiav tshuaj Olmesartan Medoxomil, yog tias oliguria lossis hypotension tshwm sim, siv cov kev ntsuas los tswj cov ntshav txaus thiab lub raum perfusion. Kev hloov pauv lossis lim ntshav tuaj yeem xav tau los ua ib txoj hauv kev rov qab hypotension thiab txhawb lub raum ua haujlwm.

Cov ntaub ntawv

Cov ntaub ntawv tsiaj

Tsis muaj qhov cuam tshuam teratogenic tau pom thaum Olmesartan Medoxomil tau muab rau cov nas cev xeeb tub ntawm qhov ncauj ntau txog 1000 mg / kg / hnub (240 npaug ntawm qhov siab tshaj plaws pom zoo tib neeg koob tshuaj (MRHD) ntawm mg / m.obhauv paus) lossis cev xeeb tub ntawm qhov ncauj koob tshuaj txog li 1 mg / kg / hnub (ib nrab ntawm MRHD ntawm mg / mobhauv paus; Cov koob tshuaj ntau dua tsis tuaj yeem ntsuas qhov cuam tshuam rau kev loj hlob ntawm fetal raws li lawv ua rau tuag taus). Hauv cov nas, qhov txo qis hauv cov menyuam yug menyuam thiab qhov hnyav nce tau pom ntawm koob tshuaj ≧1.6 mg / kg / hnub, thiab qeeb hauv kev loj hlob tseem ceeb (kev sib cais ntawm pob ntseg auricula, tawg ntawm qis incisors, tsos ntawm cov plaub hau hauv plab, qhovntsej thiaj tsis mob ntawm cov noob qes, thiab kev sib cais ntawm daim tawv muag) thiab koob tshuaj nce ntxiv nyob rau hauv qhov tshwm sim ntawm dilation ntawm lub raum pelvis tau pom ntawm koob tshuaj ≧ 8 mg / kg / hnub. Qhov tsis pom muaj txiaj ntsig zoo rau kev loj hlob toxicity hauv nas yog 0.3 mg / kg / hnub, txog ib feem kaum ntawm MRHD ntawm 40 mg / hnub.

lactation

Risk Summary

Tsis muaj cov ntaub ntawv hais txog qhov muaj olmesartan hauv tib neeg cov kua mis, cov teebmeem ntawm tus menyuam mos noj mis, lossis cov teebmeem ntawm cov kua mis. Olmesartan yog secreted ntawm tsawg concentration nyob rau hauv cov kua mis ntawm lactating nas(saib Cov ntaub ntawv ). Vim tias muaj peev xwm ua rau muaj kev cuam tshuam tsis zoo rau tus menyuam mos, yuav tsum txiav txim siab seb puas yuav tsum tsis tu ncua lossis txiav cov tshuaj, suav nrog qhov tseem ceeb ntawm cov tshuaj rau leej niam.

Cov ntaub ntawv

Kev pom muaj olmesartan hauv cov mis nyuj tau pom tom qab kev tswj hwm qhov ncauj ntawm 5 mg / kg [14C] Olmesartan Medoxomil rau lactating nas.

Kev siv menyuam yaus

Cov teebmeem antihypertensive ntawm Olmesartan Medoxomil tau raug soj ntsuam hauv ib qho kev tshawb fawb, ob qhov muag tsis pom kev kho mob hauv cov neeg mob hnub nyoog 1 txog 16 xyoo.[saib Kev Kawm Kho Mob (14.2) ]. Cov tshuaj pharmacokinetics ntawm Olmesartan Medoxomil tau soj ntsuam hauv cov neeg mob menyuam yaus hnub nyoog 1 txog 16 xyoo.[saib Clinical Pharmacology (12.3) ]. Olmesartan Medoxomil feem ntau tau txais txiaj ntsig zoo hauv cov neeg mob menyuam yaus, thiab qhov kev tsis zoo ntawm qhov profile zoo ib yam li tau piav qhia rau cov neeg laus.

Olmesartan Medoxomil tsis tau pom tias muaj txiaj ntsig zoo rau ntshav siab hauv cov menyuam yaus<6 years of age.

Kev siv cov ntsiav tshuaj Olmesartan Medoxomil hauv cov menyuam yaus<1 year of age is not recommended [saib Ceeb toom thiab ceev faj (5.2) ]. renin-angiotensin-aldosterone system (RAAS) ua lub luag haujlwm tseem ceeb hauv kev loj hlob ntawm lub raum. RAAS blockade tau pom tias ua rau lub raum tsis zoo hauv cov nas me me. Kev tswj xyuas cov tshuaj uas ua ncaj qha rau ntawm renin-angiotensin aldosterone system (RAAS) tuaj yeem hloov kho lub raum tsis zoo.

Kev siv Geriatric

Ntawm tag nrho cov neeg mob ntshav siab tau txais Olmesartan Medoxomil hauv kev tshawb fawb soj ntsuam, ntau dua 20% yog hnub nyoog 65 xyoo thiab tshaj, thaum ntau dua 5% yog 75 xyoo thiab laus dua. Tsis muaj qhov sib txawv ntawm qhov ua tau zoo lossis kev nyab xeeb ntawm cov neeg mob laus thiab cov neeg mob hluas. Lwm qhov kev paub txog kev kho mob tsis tau txheeb xyuas qhov sib txawv ntawm cov lus teb ntawm cov neeg laus thiab cov neeg mob hluas, tab sis kev nkag siab ntau dua ntawm qee cov neeg laus tsis tuaj yeem txiav tawm.[saib Clinical Pharmacology (12.3) ].

Hepatic Impairment

Nce hauv AUC0-∞thiab Cmaxtau pom nyob rau hauv cov neeg mob uas muaj kev puas siab puas ntsws nruab nrab piv rau cov kev tswj hwm, nrog kev nce hauv AUC txog li 60%. Tsis muaj kev hloov kho thawj zaug tau pom zoo rau cov neeg mob uas muaj qhov tsis txaus siab rau lub siab ua haujlwm tsis zoo[saib Clinical Pharmacology (12.3) ].

Lub raum Impairment

Cov neeg mob lub raum tsis ua haujlwm tau ua kom cov ntshav siab ntau ntawm olmesartan piv rau cov neeg mob uas lub raum ua haujlwm. Tom qab siv ntau zaus, AUC tau kwv yees li peb npaug ntawm cov neeg mob lub raum tsis zoo (creatinine tshem tawm.<20 mL/min). No initial dosage adjustment is recommended for patients with moderate to marked renal impairment (creatinine clearance <40 mL/min) [saib Dosage thiab Administration (2.1) , Ceeb toom thiab ceev faj (5.4) thiab Clinical Pharmacology (12.3) ].

Cov Neeg Mob Dub

Cov nyhuv antihypertensive ntawm Olmesartan Medoxomil yog me dua hauv cov neeg mob dub (feem ntau yog cov neeg tsawg-renin), raws li tau pom nrog ACE inhibitors, beta-blockers thiab lwm yam angiotensin receptor blockers.

Kev noj ntau dhau

Cov ntaub ntawv txwv tsis pub muaj cuam tshuam txog kev noj ntau dhau hauv tib neeg. Qhov feem ntau tshwm sim ntawm overdosage yuav yog hypotension thiab tachycardia; bradycardia tuaj yeem ntsib yog tias parasympathetic (vagal) stimulation tshwm sim. Yog tias cov tsos mob hypotension tshwm sim, pib kho kev txhawb nqa. Lub dialyzability ntawm olmesartan tsis paub.

Olmesartan Medoxomil Cov lus piav qhia

Olmesartan Medoxomil, ib qho tshuaj, yog hydrolyzed rau olmesartan thaum nqus los ntawm txoj hnyuv. Olmesartan yog xaiv ATibsubtype angiotensin II receptor antagonist.

Olmesartan Medoxomil tau piav qhia txog tshuaj raws li 2,3-dihydroxy-2-butenyl 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[p-(Cov-ibH-tetrazol-5-ylphenyl)benzyl]imidazole-5-carboxylate, cyclic 2,3-carbonate.

Nws cov qauv empirical yog C29H30N6LUB6thiab nws cov qauv qauv yog:

Olmesartan Medoxomil yog xim dawb rau lub teeb daj-dawb hmoov lossis crystalline hmoov nrog ib qho hnyav ntawm 558.59. Nws yog xyaum insoluble nyob rau hauv dej thiab sparingly soluble nyob rau hauv methanol. Olmesartan Medoxomil ntsiav tshuaj, USP muaj nyob rau hauv qhov ncauj siv raws li film-coated ntsiav tshuaj uas muaj 5 mg, 20 mg, los yog 40 mg ntawm Olmesartan Medoxomil thiab cov nram qab no inactive cov khoom xyaw: hydroxypropyl cellulose, hypromellose, lactose monohydrate, tsawg-substituted hydroxypropylear cellulose, magnesium. , microcrystalline cellulose, titanium dioxide, polyethylene glycol.

FDA pom zoo dissolution method txawv ntawm USP dissolution method.

Olmesartan Medoxomil - Chaw Kho Mob Pharmacology

Mechanism ntawm Action

Angiotensin II yog tsim los ntawm angiotensin I hauv cov tshuaj tiv thaiv catalyzed los ntawm angiotensin converting enzyme (ACE, kininase II). Angiotensin II yog tus neeg sawv cev tseem ceeb ntawm renin-angiotensin system, nrog rau cov teebmeem vasoconstriction, stimulation ntawm synthesis thiab tso tawm ntawm aldosterone, plawv stimulation thiab lub raum reabsorption ntawm sodium. Olmesartan thaiv cov vasoconstrictor teebmeem ntawm angiotensin II los ntawm kev xaiv thaiv kev khi ntawm angiotensin II rau AT.ibreceptor nyob rau hauv vascular smooth nqaij. Nws qhov kev txiav txim yog, yog li ntawd, ywj siab ntawm txoj hauv kev rau angiotensin II synthesis.

Ib ATobreceptor kuj pom muaj nyob hauv ntau cov ntaub so ntswg, tab sis qhov receptor no tsis paub tias muaj feem cuam tshuam nrog kev mob plawv homeostasis. Olmesartan muaj ntau dua 12,500-fold ntau dua affinity rau ATibreceptor tshaj rau ATobtus neeg txais kev pab.

Blockade ntawm renin-angiotensin system nrog ACE inhibitors, uas inhibit biosynthesis ntawm angiotensin II los ntawm angiotensin I, yog ib tug txheej txheem ntawm ntau yam tshuaj siv los kho ntshav siab. ACE inhibitors kuj inhibit qhov degradation ntawm bradykinin, cov tshuaj tiv thaiv kuj catalyzed los ntawm ACE. Vim tias Olmesartan Medoxomil tsis inhibit ACE (kininase II), nws tsis cuam tshuam cov lus teb rau bradykinin. Txawm hais tias qhov sib txawv no muaj qhov cuam tshuam rau kev kho mob tseem tsis tau paub.

Blockade ntawm angiotensin II receptor inhibits qhov kev tswj tsis zoo ntawm angiotensin II ntawm renin secretion, tab sis qhov ua rau muaj zog plasma renin kev ua thiab circulating angiotensin II theem tsis kov yeej cov nyhuv ntawm olmesartan ntawm cov ntshav siab.

s903 ua

Pharmacodynamics

Olmesartan Medoxomil koob tshuaj ntawm 2.5 mg rau 40 mg inhibits pressor teebmeem ntawm angiotensin I infusion. Lub sijhawm ntawm cov nyhuv inhibitory yog cuam tshuam nrog koob tshuaj, nrog rau koob tshuaj Olmesartan Medoxomil> 40 mg muab> 90% inhibition ntawm 24 teev.

Plasma concentrations ntawm angiotensin I thiab angiotensin II thiab plasma renin kev ua haujlwm (PRA) nce tom qab ib zaug thiab rov ua haujlwm ntawm Olmesartan Medoxomil rau cov neeg noj qab haus huv thiab cov neeg mob ntshav siab. Rov ua dua kev tswj hwm txog li 80 mg Olmesartan Medoxomil muaj kev cuam tshuam tsawg kawg nkaus ntawm cov qib aldosterone thiab tsis muaj kev cuam tshuam rau cov poov tshuaj hauv cov ntshav.

Pharmacokinetics

Kev nqus

Olmesartan Medoxomil yog sai thiab ua tiav bioactivated los ntawm ester hydrolysis rau olmesartan thaum nqus los ntawm txoj hnyuv.

Cov ntsiav tshuaj Olmesartan Medoxomil thiab cov tshuaj ncua kev kawm npaj los ntawm Olmesartan Medoxomil ntsiav tshuaj yog bioequivalent[saib Dosage thiab Administration (2.2) ].

Qhov tseeb bioavailability ntawm olmesartan yog kwv yees li 26%. Tom qab kev tswj hwm qhov ncauj, qhov siab tshaj plaws plasma concentration (Cmax) ntawm olmesartan tau mus txog tom qab 1 mus rau 2 teev. Cov zaub mov tsis cuam tshuam rau bioavailability ntawm olmesartan. Cov ntsiav tshuaj Olmesartan Medoxomil tuaj yeem siv nrog lossis tsis muaj zaub mov.

Kev faib tawm

Qhov ntim ntawm kev faib tawm ntawm olmesartan yog kwv yees li 17 L. Olmesartan yog khi rau cov plasma proteins (99%) thiab tsis nkag mus rau cov qe ntshav liab. Kev sib txuas ntawm cov protein yog qhov tsis tu ncua ntawm plasma olmesartan concentrations zoo tshaj qhov ua tiav nrog cov koob tshuaj pom zoo.

Hauv cov nas, olmesartan hla cov ntshav-hlwb tsis zoo, yog tias tag nrho. Olmesartan hla dhau lub placental barrier nyob rau hauv nas thiab muab faib rau fetus. Olmesartan tau muab faib rau cov mis nyuj ntawm cov nas qis.

Metabolism thiab excretion

Tom qab kev hloov pauv sai thiab ua tiav ntawm Olmesartan Medoxomil rau olmesartan thaum lub sijhawm nqus, tsis muaj cov metabolism ntxiv ntawm olmesartan. Tag nrho cov ntshav plasma tshem tawm ntawm olmesartan yog 1.3 L / h, nrog rau lub raum tshem tawm ntawm 0.6 L / h. Kwv yees li ntawm 35% mus rau 50% ntawm cov koob tshuaj absorbed tau zoo nyob rau hauv cov zis thaum cov khoom seem raug tshem tawm hauv cov quav los ntawm cov kua tsib.

Olmesartan zoo li yuav raug tshem tawm hauv biphasic yam nrog lub davhlau ya nyob twg tshem tawm ib nrab-lub neej ntawm kwv yees li 13 teev. Olmesartan qhia tawm cov tshuaj pharmacokinetics tom qab ib koob tshuaj ntawm qhov ncauj txog li 320 mg thiab ntau qhov ncauj qhov ncauj txog li 80 mg. Cov theem tsis tu ncua ntawm olmesartan tau ua tiav hauv 3 mus rau 5 hnub thiab tsis muaj kev txuam nrog hauv cov ntshav tshwm sim nrog kev noj ib zaug ib hnub.

Cov pejxeem tshwj xeeb

Cov neeg mob Geriatric

Cov tshuaj pharmacokinetics ntawm olmesartan tau kawm hauv cov neeg laus (≧ 65 xyoo). Zuag qhia tag nrho, qhov siab tshaj plaws plasma concentration ntawm olmesartan zoo sib xws hauv cov tub ntxhais hluas thiab cov neeg laus. Kev sib xyaw me me ntawm olmesartan tau pom nyob rau hauv cov neeg laus nrog rov ua dua; AUCss,τyog 33% siab dua hauv cov neeg mob laus, sib xws rau kwv yees li 30% txo qis hauv CLR [saib Dosage thiab Administration (2.1) thiab Siv hauv Cov Pej Xeem Tshwj Xeeb (8.5) ].

Cov neeg mob menyuam yaus

Cov tshuaj pharmacokinetics ntawm olmesartan tau kawm hauv cov neeg mob ntshav siab rau menyuam yaus hnub nyoog 1 txog 16 xyoo. Kev tshem tawm ntawm olmesartan hauv cov neeg mob me nyuam yaus zoo ib yam li cov neeg laus thaum hloov kho lub cev hnyav.[saib Siv hauv Cov Pej Xeem Tshwj Xeeb (8.4) ].

Olmesartan pharmacokinetics tsis tau tshawb xyuas hauv cov neeg mob me dua 1 xyoos[saib Ceeb toom thiab ceev faj (5.2) thiab Siv hauv Cov Pej Xeem Tshwj Xeeb (8.4) ].

Txiv neej thiab poj niam cov neeg mob

Qhov sib txawv me me tau pom nyob rau hauv pharmacokinetics ntawm olmesartan hauv cov poj niam piv rau cov txiv neej. AUC thiab Cmaxyog 10-15% siab dua ntawm cov poj niam dua li cov txiv neej.

Cov neeg mob Hepatic Impairment

Nce hauv AUC0-∞thiab Cmaxtau pom nyob rau hauv cov neeg mob uas muaj kev puas siab puas ntsws nruab nrab piv rau cov hauv kev tswj kev sib tw, nrog kev nce hauv AUC txog li 60%[saib Dosage thiab Administration (2.1) thiab Siv hauv Cov Pej Xeem Tshwj Xeeb (8.6) ].

Cov neeg mob raum tsis zoo

Hauv cov neeg mob lub raum tsis ua haujlwm, cov ntshav qab zib ntau ntawm olmesartan tau nce siab piv rau cov neeg mob uas lub raum ua haujlwm. Tom qab siv ntau zaus, AUC tau kwv yees li peb npaug ntawm cov neeg mob lub raum tsis zoo (creatinine tshem tawm.<20 mL/min). The pharmacokinetics of olmesartan in patients undergoing hemodialysis has not been studied [saib Dosage thiab Administration (2.1) , Ceeb toom thiab ceev faj (5.4) thiab Siv hauv Cov Pej Xeem Tshwj Xeeb (8.7) ].

Kev Tshawb Fawb Kev Sib Tham Txog Tshuaj

Bile Acid Sequestering Agent Colesevelam

Kev tswj hwm ntawm 40 mg Olmesartan Medoxomil thiab 3750 mg colesevelam hydrochloride hauv cov neeg noj qab haus huv tau ua rau 28% txo qis hauv C.maxthiab 39% txo qis hauv AUC ntawm olmesartan. Cov teebmeem tsawg dua, 4% thiab 15% txo qis hauv Cmaxthiab AUC raws li, tau pom thaum Olmesartan Medoxomil tau tswj hwm 4 teev ua ntej colesevelam hydrochloride.[saib Kev sib tham nrog tshuaj (7.5) ].

Lwm Txoj Kev Kawm

Tsis muaj kev cuam tshuam tshuaj tseem ceeb hauv kev tshawb fawb uas Olmesartan Medoxomil tau koom nrog digoxin lossis warfarin hauv cov neeg ua haujlwm noj qab haus huv.

Lub bioavailability ntawm olmesartan tsis tau hloov pauv los ntawm kev sib koom ua ke ntawm cov tshuaj antacids [Al(OH)]3/Mg (OH)ob].

Olmesartan Medoxomil tsis metabolized los ntawm cytochrome P450 system thiab tsis muaj teebmeem rau P450 enzymes; Yog li, kev sib cuam tshuam nrog cov tshuaj uas inhibit, induce, lossis metabolized los ntawm cov enzymes no tsis xav tau.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

Olmesartan Medoxomil tsis yog carcinogenic thaum noj zaub mov noj rau nas mus txog 2 xyoos. Qhov koob tshuaj ntau tshaj plaws (2000 mg / kg / hnub) yog, ntawm mg / mobHauv paus, kwv yees li 480 npaug ntawm qhov siab tshaj plaws pom zoo tib neeg koob tshuaj (MRHD) ntawm 40 mg / hnub. Ob txoj kev tshawb fawb carcinogenicity ua nyob rau hauv nas, 6-hli gavage kawm nyob rau hauv p53 knockout nas thiab 6-hli kev noj zaub mov kev kawm nyob rau hauv Hras2 transgenic nas, ntawm koob mus txog 1000 mg / kg / hnub (kwv yees li 120 npaug ntawm MRHD) , qhia tsis muaj pov thawj ntawm cov nyhuv carcinogenic ntawm Olmesartan Medoxomil.

Ob leeg Olmesartan Medoxomil thiab olmesartan tau kuaj pom tsis zoo nyob rau hauvhauv vitroSyrian hamster embryo cell transformation assay thiab tsis pom muaj pov thawj ntawm genetic toxicity hauv Ames (cov kab mob mutagenicity) kuaj. Txawm li cas los xij, ob qho tib si tau pom tias ua rau muaj kev cuam tshuam ntawm chromosomal aberrations hauv cov kab lis kev caihauv vitro(Suav lub ntsws hamster) thiab kuaj pom qhov zoo rau thymidine kinase kev hloov hauv lubhauv vitronas lymphoma assay. Olmesartan Medoxomil kuaj tsis zoonyobrau kev hloov pauv hauv MutaMouse txoj hnyuv thiab lub raum thiab rau clastogenicity hauv cov pob txha nas (micronucleus test) ntawm qhov ncauj ntau txog 2000 mg / kg (olmesartan tsis kuaj).

Fertility ntawm nas tsis cuam tshuam los ntawm kev tswj hwm ntawm Olmesartan Medoxomil ntawm koob tshuaj ntau npaum li 1000 mg / kg / hnub (240 npaug ntawm MRHD) hauv txoj kev tshawb fawb uas tau pib koob tshuaj 2 (poj niam) lossis 9 (txiv neej) lub lis piam ua ntej mating.

Kev tshawb fawb soj ntsuam

Cov neeg laus mob ntshav siab

Cov teebmeem ntawm kev mob ntshav siab ntawm Olmesartan Medoxomil tau pom nyob rau hauv xya qhov kev tshawb fawb uas tswj tau cov placebo ntawm cov koob tshuaj xws li 2.5 mg txog 80 mg rau 6 mus rau 12 lub lis piam, txhua qhov qhia txog kev txo qis hauv qhov ncov thiab cov ntshav siab. Tag nrho ntawm 2693 tus neeg mob (2145 Olmesartan Medoxomil; 548 placebo) nrog qhov tseem ceeb kub siab tau kawm. Olmesartan Medoxomil ib hnub ib zaug txo qis diastolic thiab systolic ntshav siab. Cov lus teb tau hais txog koob tshuaj, raws li qhia hauv daim duab hauv qab no. Ib koob tshuaj Olmesartan Medoxomil ntawm 20 mg txhua hnub ua rau txo qis ntshav siab (BP) txo qis dua cov placebo txog li 10/6 mmHg thiab ib koob tshuaj 40 mg txhua hnub ua rau muaj qhov txo qis BP ntau dua li cov placebo txog 12/7 mmHg. Olmesartan Medoxomil koob tshuaj ntau dua 40 mg tsis muaj kev cuam tshuam ntxiv me ntsis. Qhov pib ntawm cov nyhuv antihypertensive tshwm sim hauv 1 lub lis piam thiab tau tshwm sim ntau tom qab 2 lub lis piam.

Cov ntaub ntawv saum toj no yog los ntawm xya qhov kev tshawb fawb tshuaj placebo (2145 Olmesartan Medoxomil cov neeg mob, 548 cov neeg mob placebo). Cov nyhuv txo qis ntshav siab tau tswj hwm thoob plaws lub sijhawm 24-teev nrog Olmesartan Medoxomil ib hnub ib zaug, nrog qhov sib piv-rau-peak piv rau systolic thiab diastolic teb ntawm 60 thiab 80%.

Kev txo cov ntshav siab ntawm Olmesartan Medoxomil, nrog thiab tsis muaj hydrochlorothiazide, tau khaws cia rau hauv cov neeg mob kho txog li 1 xyoos. Tsis muaj pov thawj ntawm tachyphylaxis thaum lub sij hawm kev kho mob mus sij hawm ntev nrog Olmesartan Medoxomil los yog rebound nyhuv tom qab tshem tawm sai sai ntawm Olmesartan Medoxomil tom qab 1 xyoo ntawm kev kho mob.

Cov nyhuv antihypertensive ntawm Olmesartan Medoxomil zoo ib yam li cov txiv neej thiab poj niam thiab cov neeg mob laus thiab hluas dua 65 xyoo. Cov nyhuv me me hauv cov neeg mob dub (feem ntau yog cov neeg tsawg-renin), raws li tau pom nrog ACE inhibitors, beta-blockers thiab lwm yam angiotensin receptor blockers. Olmesartan Medoxomil tau ntxiv cov ntshav siab txo qis thaum ntxiv rau hydrochlorothiazide.

Tsis muaj kev sim ntawm Olmesartan Medoxomil ua kom pom qhov txo qis hauv plawv plawv hauv cov neeg mob ntshav siab, tab sis tsawg kawg yog ib qho tshuaj uas zoo sib xws tau pom cov txiaj ntsig zoo li no.

Pediatric Hypertension

Cov teebmeem antihypertensive ntawm Olmesartan Medoxomil hauv cov menyuam yaus raug soj ntsuam hauv kev tshawb fawb randomized, ob qhov muag tsis pom kev nrog 302 cov neeg mob ntshav siab hnub nyoog 6 txog 16 xyoo. Cov pej xeem txoj kev tshawb no muaj tag nrho-dub pawg ntawm 112 tus neeg mob thiab sib xyaw haiv neeg ntawm 190 tus neeg mob, suav nrog 38 tus neeg mob dub. Lub etiology ntawm kev kub siab yog qhov tseem ceeb tshaj plaws kub siab (87% ntawm pawg neeg dub thiab 67% ntawm pawg sib xyaw). Cov neeg mob uas hnyav 20 rau<35 kg were randomized to 2.5 or 20 mg of Olmesartan Medoxomil once daily and patients who weighed ≧35 kg were randomized to 5 or 40 mg of Olmesartan Medoxomil once daily. At the end of 3 weeks, patients were re-randomized to continuing Olmesartan Medoxomil or to taking placebo for up to 2 weeks. During the initial dose-response phase, Olmesartan Medoxomil significantly reduced both systolic and diastolic blood pressure in a weight-adjusted, dose-dependent manner. Overall, the two dose levels of Olmesartan Medoxomil (low and high) significantly reduced systolic blood pressure by 6.6 and 11.9 mmHg from the baseline, respectively. These reductions in systolic blood pressure included both drug and placebo effect. During the randomized withdrawal to placebo phase, mean systolic blood pressure at trough was 3.2 mmHg lower and mean diastolic blood pressure at trough was 2.8 mmHg lower in patients continuing Olmesartan Medoxomil than in patients withdrawn to placebo. These differences were statistically different. As observed in adult populations, the blood pressure reductions were smaller in black patients.

Hauv tib txoj kev tshawb no, 59 tus neeg mob hnub nyoog 1 txog 5 xyoos uas hnyav ≧5 kg tau txais 0.3 mg / kg ntawm Olmesartan Medoxomil ib hnub ib zaug rau peb lub lis piam hauv lub sijhawm qhib thiab tom qab ntawd tau randomized kom tau txais Olmesartan Medoxomil lossis placebo hauv ob zaug. qhov muag tsis pom kev. Thaum kawg ntawm lub lim tiam thib ob ntawm kev tshem tawm, qhov txhais tau tias systolic / diastolic ntshav siab ntawm trough yog 3/3 mmHg qis hauv pab pawg randomized rau Olmesartan Medoxomil; Qhov sib txawv ntawm cov ntshav siab no tsis yog qhov tseem ceeb (95% C.I. -2 txog 7/-1 txog 7).

Yuav Ua Li Cas Muab / Cia thiab tuav

Olmesartan Medoxomil ntsiav tshuaj, USP tau muab los ua cov ntsiav tshuaj dawb lossis yuav luag dawb puag ncig zaj duab xis-coated ntsiav tshuaj, debossed 'L17', 'L18' thiab 'L20' ntawm ib sab rau 40mg, 20mg thiab 5mg lub zog, raws li, thaum nyob rau sab nraud.

Cov ntsiav tshuaj tau muab raws li hauv qab no:

Cia
Khaws ntawm 20-25 ° C (68-77 ° F); Excursions tso cai rau 15 ° C thiab 30 ° C (59 ° F-86 ° F)[saib USP Controlled Room Temperature].

Cov Ntaub Ntawv Qhia Txog Tus Neeg Mob

cev xeeb tub:Qhia cov poj niam cov neeg mob uas muaj hnub nyoog yug me nyuam txog qhov tshwm sim ntawm kev raug rau Olmesartan Medoxomil ntsiav tshuaj thaum cev xeeb tub. Sib tham txog kev kho mob nrog cov poj niam npaj yuav xeeb tub. Qhia cov neeg mob kom ceeb toom cev xeeb tub rau lawv tus kws kho mob sai li sai tau[saib Ceeb toom thiab ceev faj (5.1) thiab Siv hauv Cov Pej Xeem Tshwj Xeeb (8.1) ].

lactation: Qhia cov poj niam laus kom tsis txhob pub niam mis thaum kho nrog Olmesartan Medoxomil ntsiav tshuaj[saib Siv hauv Cov Pej Xeem Tshwj Xeeb (8.2) ].

Kuv puas tuaj yeem siv monistat 1 thaum cev xeeb tub

Hyperkalemia:Qhia rau cov neeg mob kom tsis txhob siv cov tshuaj potassium los yog ntsev hloov uas muaj cov poov tshuaj yam tsis tau sab laj nrog lawv tus kws kho mob[saib Kev Sib Tham Txog Tshuaj (7.1) ].

* Txhua lub npe lag luam yog cov cuab yeej ntawm lawv cov tswv.

Tsim los ntawm:

Sunshine Lake Pharma Co., Ltd.

Northern Industry Road 1#,

Song Shan Lake, Dongguan,

GuangDong xeev, 523808,

P.R. Suav

Muab faib los ntawm:

Lannett Co., Ltd.

13200 Townsend Txoj Kev,

Philadelphia, PA 19154

Kho tshiab: 06/2021

Pob ntawv Label - Thawj Tswj Hwm Vaj Huam Sib Luag - 5 mg 30 ct Lub raj mis Label

Package Label - Principal Display Panel – 20 mg 30 ct Bottle Label

Pob ntawv Label - Thawj Tswj Hwm Vaj Huam Sib Luag - 40 mg 30 ct Lub raj mis Label