Invocana® (300 mg) Canagliflozin
Biko tupu ịzụta mbadamba akwụkwọ Invokana. 300 mg 30 pcs., Pack., Lelee ozi banyere ya na ozi dị na weebụsaịtị nke onye na-emepụta ma ọ bụ kọwaa nkọwapụta nke ụdị akọwapụtara ya na onye njikwa ụlọ ọrụ anyị!
Ozi a gosiputara na saịtị ahụ abụghị onyinye ọha. Onye rụpụtara ya nwere ikike ịme mgbanwe n ’okike, imewe na ịkwakọ ngwaahịa. Foto nke ngwongwo na foto nke egosiri na katalọgụ saịtị ahụ nwere ike ịdị iche na mbido mbụ.
Ozi banyere ọnụahịa nke egosiri na katalọgụ saịtị ahụ nwere ike ịdị iche na nke ahụ n'ezie n'oge etinyebere iwu maka ngwaahịa kwekọrọ.
Emeputa
N'ime mbadamba ihe nkiri 300 mg agba agba agba nwere:
306,0 mg nke canagliflozin hemihydrate, nke ya na 300.0 mg nke canagliflozin.
Ndị na - ahụ maka ihe (isi): microcrystalline cellulose 117.78 mg, anhydrous lactose 117.78 mg, croscarmellose sodium 36.00 mg, hyprolose 18.00 mg, magnesium stearate 4.44 mg.
Ndị na-ahụ anya (shei): Opadray II 85F18422 acha ọcha (polyvinyl mmanya, akụkụ mmiri hydrolyzed, 40.00% titanium dioxide 25,00%, macrogol 3350 20,20%, talc 14.80%) - 18.00 mg .
Omume ọgwụ
Egosipụtawo na ndị ọrịa nwere ọrịa mellitus nwere mgbake ume ọhụrụ na-emetụta aha na glucose, nke nwere ike iso na-eme ka mmụba glucose na-aga n'ihu. Sodium glucose transport protein 2 (SGLT2), nke egosipụtara na probual renal tubules, bụ maka ihe ka ọtụtụ nhazigharị nke glucose site na tubule lumen.
Kanagliflozin bụ ihe na-egbochi protein sọdum-glucose na-ebute protein 2. Site na igbochi SGLT2, canagliflozin na-ebelata nhazigharị nke glucose na-edozi ma na -ebelata ụzọ nkwụghachi maka glucose (PPG), si otú a na-abawanye mmamịrị nke urinary, nke na-eduga n'ịbelata mkpụkọ glucose ọbara na insulin- usoro nnwere onwe na ndị ọrịa nwere ụdị shuga 2.
Mmụba nke glucose na urinary excretion site na mgbochi nke SGLT2 na-edugakwa osmotic diuresis, mmetụta diuretic na-eduga na mbelata ọbara mgbagha systolic, mmụba nke urinary excretion na-eduga na mbelata calorie na, n'ihi ya, mbelata nke ahụ.
N'ime usoro ọmụmụ nke III nke a rụrụ ule nnwere onwe ngụkọta nri ụtụtụ, ojiji nke canagliflozin na dose nke 300 mg mere ka mbelata nke ọma na mmụba na ọkwa nke postprandial glycemia karịa na nke 100 mg. Mmetụta a nwere ike ịbụ n'ihi ihe mgbochi mpaghara SGLT1 dị n'ime obodo, na-eburu n'uche ohere dị ukwuu nke canagliflosin na eriri afọ lumen tupu ịnabata ọgwụ (canagliflosin bụ obere ihe mgbochi SGLT1 inhibitor). Na nyocha, achọpụtaghị malabsorption site na iji canagliflozin.
Mmetụta ọgwụ ọgwụ:
N'oge ọnwụnwa nke ụlọ ọgwụ gachara mgbe a na-ejikwa otu ọnụ na ọtụtụ nchịkwa nke canagliflozin site na ndị ọrịa nwere ọrịa shuga 2, a na-eme ka ọnụ ala akwara dị elu nke glucose na-agbadata, ma na-ewepụta glucose na-abawanye elu. Ọnụahịa mbụ nke mbata naalụ nke glucose dị ihe dị ka 13 mmol / L, ọnụego kachasi elu n'ime awa iri abụọ na anọ ana-ahụ maka glucose na-eji ọgwụ nke 300 mg otu ugboro kwa ụbọchị ma malite na 4 ruo 5 mmol / L, nke na-egosi ntakịrị ihe ize ndụ nke hypoglycemia na ndabere usoro ọgwụgwọ. N'ime nyocha ụlọ ọgwụ banyere ojiji nke canagliflozin na doses nke 100 ruo 300 mg otu ugboro kwa ụbọchị site n'aka ndị ọrịa nwere ụdị ọrịa shuga 2 maka ụbọchị 16, mbelata nke ọnụ ụlọ na-emetụta glucose na mmụba nke ikuku urinary excretion bụ mgbe niile. N'okwu a, nchịkọta nke glucose na plasma ọbara belatara nke ukwuu-dabere n’ụbọchị mbụ iji rụọ ọrụ, sochiri nkwụsi ike nke glucose na plasma ọbara n’afọ na-enweghị nri na mgbe i richara nri.
Ojiji nke otu 300 mg nke canagliflozin tupu nri nke calorie agwakọtara na ndị ọrịa nwere ụdị shuga 2 kpatara igbu oge na nnweta glucose na eriri afọ yana mbelata nke glycemia postprandial site na sistemụ akụrụ na extrarenal.
N'ime ule nke ụlọ ọgwụ, ndị ọrụ afọ ofufo 60 nwere ahụike natara otu ọgwụ ọnụ nke 300 mg nke canagliflozin, 1200 mg nke canagliflozin (4 ugboro kachasị atụ aro), moxifloxacin, na placebo. Enweghị mgbanwe mgbanwe dị mkpa na etiti oge QT ka ejiri ya na 300 mg tụrụ aro ya ma ọ bụ na nke 1200 mg. Mgbe ị na-etinye dose nke 1200 mg, ihe nrịba ama nke plasma nke canagliflozin dị ihe dị ka oge 1.4 karịa ogo ịta ahụhụ mgbe ị aụsịrị 300 mg otu ugboro n'ụbọchị.
Na-ebu ọnụ Glycemia:
N'ime ule nke ụlọ ọgwụ, ojiji nke canagliflozin dị ka monotherapy ma ọ bụ dịka njikọta ọgwụgwọ na otu ma ọ bụ ọgwụ ọnụ abụọ nke hypoglycemic dugara ná mgbanwe ọnụ glycemia na-emetụta ma e jiri ya tụnyere ọkwa mbụ dị na placebo site na -1.2 mmol / l ka -1.9 mmol / l mgbe ị na-etinye usoro onunu ogwu nke 100 mg na site -1.9 mmol / l gaa -2.4 mmol / l - mgbe ị na-etinye usoro onunu ogwu nke 300 mg, otu. Mmetụta a dịkarịrị nso mgbe ụbọchị ọgwụgwọ mbụ gachara wee nọgidesie ike n'oge ọgwụgwọ niile.
Postprandial glycemia:
N'ime ule nke ụlọ ọgwụ iji ojiji nke canagliflozin dị ka monotherapy ma ọ bụ ọgwụgwọ njikọ maka otu ma ọ bụ abụọ ọnụ hypoglycemic ndị nnọchi anya, postprandial glycemia ka tụtara mgbe itinye ule nnabata ya na iji nri ụtụtụ agakọla agwakọta. Ojiji nke canagliflozin mere ka mbelata nke ọkwa nke postprandial glycemia ma e jiri ya tụnyere ọkwa mbụ na-akwanyere placebo si -1.5 mmol / L ka -2.7 mmol / L - mgbe ị na-eji usoro ọgwụ nke 100 mg na site na -2.1 mmol / L gaa -3.5 mmol / l - mgbe ị na-a aụ ọgwụ nke 300 mg, karị, n'ihi mbelata mgbanye glucose tupu nri na mbelata nke mgbanwe na ọkwa nke postprandial glycemia.
Isi:
Canagliflozin 100 mg na 300 mg dị ka monotherapy dị ka okpukpu abụọ ma ọ bụ okpukpu atọ usoro ọgwụgwọ ọzọ kpatara mbelata ihe dị ka ogo ahụ karịa izu 26, ma e jiri ya tụnyere placebo. N’ime izu iri abụọ na ise na-arụsi ọrụ ike jisiri ike were atule canagliflozin na glimepiride na sitagliptin, nkwado siri ike ma nwekwaa ọnụego mbelata nke anụ ahụ maka canagliflozin dịka njikọ metformin bụ -4.2% na -4.7% maka canagliflozin 100 mg na 300 mg, otu, jiri ya tụnyere glimepiride na metformin (1.0%) na -2.5% maka canagliflozin 300 mg na mgbakwunye na metformin na sulfonylurea, ma e jiri ya tụnyere sitagliptin na nchịkọta metformin na sulfonylurea (0.3%).
Ọbara ọbara:
N'ime ọmụmụ ihe na-achịkwa nsị, ọgwụgwọ na canagliflozin 100 mg na 300 mg mere ka mbelata nke mgbali ọbara systolic nke -3.9 mm Hg. na -5.3 mmHg karị, atụnyere placebo (-0.1 mm), na mmetụta pere mpe na mgbali ọbara diastol na mgbanwe mgbanwe uru maka canagliflozin 100 mg na 300 mg -2.1 mm Hg na -2.5 mmHg n'otu n'otu, jiri ya tụnyere placebo (-0.3 mm).
Onweghi mgbanwe di nkpa n’iru obi.
Ọrụ batrị dị na:
Nnyocha nke ojiji nke canagliflozin na ndị ọrịa nwere ụdị ọrịa shuga 2 nke ọrịa shuga na-egosi mmụba na arụmọrụ beta, dịka nyocha nke usoro homeostasis n'ihe metụtara ọrụ mkpụrụ ndụ ndị a (HOMA2-% B) yana mmụba na ọnụego insulin insulin na iji nnabata ndidi na nri ụtụtụ agwakọta.
Diabetesdị ọrịa shuga 2 n'ime ndị okenye yana nri na mmega iji melite njikwa glycemic na ogo:
- Monotherapy
- Dị ka akụkụ nke ọgwụgwọ njikọta na ọgwụ hypoglycemic ndị ọzọ, gụnyere insulin.
Nsonaazụ
Ihe omuma banyere mmeghachi omume ojoo a chọpụtara n’oge ule 1 nke canagliflozin nwere ugboro ≥2% bụ nke a na-ahazi n’usoro akụkụ ahụ nke ọ bụla dabere na nha nke mere site na iji usoro nke a: ugboro ugboro (≥1 / 10), ugboro ugboro (≥1 / 100,
Ọrịa afọ ime:
Ugboro: afọ ntachi, akpịrị ịkpọ nkụ2, akpịrị ịkpọ nkụ.
Nmebi nke akụrụ na akwara:
Ugboro: polyuria na pollakiuria3, urination peremptory, ọrịa urinary tract4, urosepsis.
Mmebi nke akụkụ anụ ahụ na mammary gland:
Ugboro: balanitis na balanoposthitis 5, vulvovaginal candidiasis 6, ọrịa na-efe efe.
1 Gụnyere monotherapy na mgbakwunye na ọgwụgwọ na usoro metformin, metformin na sulfonylurea, yana metformin na pioglitazone.
Thedị “akpịrị ịkpọ nkụ” gụnyere okwu a “akpịrị ịkpọ nkụ”, okwu ahụ bụ “polydipsia” bụkwa nke a.
3 Otu "polyuria ma ọ bụ pollakiuria" gụnyere okwu "polyuria", okwu ndị "mmụba na oke mmamịrị ahụ" na "nocturia" tinyekwara na udi a.
4 “urinary tract infection” gụnyere okwu “ọrịa urinary tract” yana kwa “okwu ahu” na “ọrịa akụrụ”.
5 Otu “balanitis ma ọ bụ ọrịa balanoposthitis” gụnyere okwu “balanitis” na “balanoposthitis” yana yana okwu “candida balanitis” na “ọrịa fungal”.
6 Atiya “vulvovaginal candidiasis” gụnyere okwu “vulvovaginal candidiasis”, “vulvovaginal fungal infection”, “vulvovaginitis” yana usoro ndị ahụ “na-efe efe na ọrịa nwoke na nwanyị na-efe efe”.
Mmeghachi omume ndị ọzọ na - adịghị mma nke mepụtara n'ọmụmụ ihe ndị na - ejikwa ike nke canagliflozin nwere ọtụtụ
Mmeghachi omume ọjọọ na-emetụta mbelata olu olu intravascular
Ugboro nke mmeghachi omume ọjọọ niile metụtara mbelata olu intravascular (postural dizziness, orthostatic hypotension, hypotension, frize na fainting) sitere na nsonaazụ nyocha emere, na ndị ọrịa natara “akaghị” diuretics, ndị ọrịa nwere obere akwara ezughị oke (GFR si 30 ruo 2) na ndị ọrịa ≥75 afọ, ugboro ugboro ka-ekwupụta ihe ọjọọ ndị a. Mgbe ị na-eduzi ọmụmụ ihe banyere ihe egwu dị na obi, ugboro ugboro nke mmeghachi omume dị njọ jikọtara ya na mbelata olu intravascular adịghị abawanye site na iji canagliflozin, ikpe nke ịkwụsị ọgwụgwọ n'ihi mmepe nke mmeghachi omume ọjọọ nke ụdị a enweghị isi.
Hypoglycemia mgbe ejiri ya mee ihe dịka njikọta insulin ma ọ bụ ihe ndị na-eme ka nzuzo ya dịkwuo elu
Mgbe ị na-eji canagliflozin dị ka njikọ nke ọgwụgwọ na insulin ma ọ bụ ihe dị iche iche nke sulfonylurea, a na-akọpụta mmepe hypoglycemia ugboro ugboro. Nke a kwekọrọ na mmụba a na-atụ anya ya na ugboro ole hypoglycemia na ọnọdụ ebe ọgwụ, nke a na-ejikọtaghị ya na mmepe nke ọnọdụ a, a na-agbakwunye na insulin ma ọ bụ ọgwụ na-eme ka nzuzo ya dịkwuo (dịka ọmụmaatụ, usoro sitere na sulfonylurea).
Mgbanwe ụlọ nyocha
Potassiumba ụba potassium ịta
A chọpụtara ọkwa nke ịba ụba ọka serum (> 5.4 mEq / L na 15% dị elu karịa ịta ahụhụ mbụ) na 4.4% nke ndị ọrịa na-anata canagliflozin na dose nke 100 mg, na 7.0% nke ndị ọrịa na-anata canagliflozin na dose nke 300 mg , na 4.8% nke ndị ọrịa na-anata placebo. N'oge ụfọdụ, a na-ahụkarị mmụba nke ukwuu na mkpokọta ọka potassium na ndị ọrịa nwere nsogbu akụrụngwa arụ ọrụ na-agafe agafe, bụ onye nweburu mmụba na mgbanye potassium na / ma ọ bụ onye natara ọtụtụ ọgwụ na-ebelata ọgwụ excretion (ihe na-eme ka ọnụnọ potassium na angiotensin na-agbanwe enzyme inhibitors (ACE)). Na mkpokọta, mmụba nke ịta ọka potassium dị obere, ọ chọghịkwa ọgwụgwọ pụrụ iche.
Inbawanye ọtụtụ ọbara creatinine na urea
N'ime izu isii mbụ ebidola ọgwụgwọ, enwere ntakịrị mmụba na mkpokọta creatinine (Ọdịmma ndị ọrịa nwere mbelata dị ukwuu na GFR (> 30%) ma e jiri ya tụnyere ọkwa izizi a hụrụ na ọkwa ọ bụla ọgwụgwọ bụ 2.0% - site na iji canagliflozin na dose 100 mg, 4.1% mgbe ị na-eji ọgwụ ahụ na ọgwụ nke 300 mg na 2.1% mgbe ị na-eji placebo Mbelata ndị a na GFR na-abụkarị oge, na njedebe nke ọmụmụ ahụ, a na-ahụta mbelata yiri ya na GFR na ndị ọrịa ole na ole. maka ndị ọrịa nwere obere akwara ezughị oke, oke nke ndị ọrịa nwere mmụba dị ukwuu na GFR (> 30%) ma e jiri ya tụnyere ọkwa izizi a hụrụ na ọkwa ọ bụla ọgwụgwọ bụ 9.3% - iji canagliflozin na dose nke 100 mg, 12.2 % - mgbe ejiri ya na 300 mg, yana 4.9% - mgbe ị na-eji placebo Mgbe ịkwụsịtụ canagliflozin, mgbanwe ndị a na paradaịs nwere ọnọdụ dị mma ma ọ bụ laghachi na ọkwa mbụ ha.
Mmụba Lipoprotein dị ala (LDL)
Mmụba na -adabere na dose nke LDL nwere mkpokọta canagliflozin. Mgbanwe ndị na-agbanwe agbanwe na LDL dịka pasent nke itinye uche mbụ ma e jiri ya tụnyere placebo bụ 0.11 mmol / L (4.5%) na 0.21 mmol / L (8.0%) mgbe ị na-eji canagliflozin na doses nke 100 mg na 300 mg, n'otu n'otu . Nkezi izizi nke LDL bụ 2.76 mmol / L, 2.70 mmol / L na 2.83 mmol / L nwere canagliflozin na usoro nke 100 na 300 mg na placebo, otu isi.
Mmụba haemoglobin mụbara
Mgbe ị na-eji canagliflozin na doses nke 100 mg na 300 mg, ntakịrị mmụba na mgbanwe pasent pasent na mkpokọta hemoglobin site na ọkwa mbụ (3.5% na 3.8%, dị iche iche) hụrụ ka e jiri ya tụnyere ntakịrị ntakịrị na otu placebo (−1.1%). A hụrụ ntakịrị ịrị elu na nkezi mgbanwe pasent nke ọnụọgụ ọbara ọbara na hematocrit site na ntọala. Imirikiti ndị ọrịa gosipụtara mmụba na mkpo haemoglobin (> 20 g / l), nke mere na 6.0% nke ndị ọrịa na-anata canagliflozin na dose nke 100 mg, na 5.5% nke ndị ọrịa na-enweta canagliflozin na dose nke 300 mg, na 1, 0% nke ndị ọrịa na-anata placebo. Ọtụtụ ụkpụrụ ka nwere ike ịbụ etu o kwesịrị.
Mbelata seric uric acid ịta
Site na iji canagliflozin na doses nke 100 mg na 300 mg, a na-ahụta mbelata dị ala na nchịkọta nke uric acid site na ọkwa mbụ (−10.1% na −10.6%, dị iche iche) ma e jiri ya tụnyere placebo, site na iji nke ntakịrị mmụba na nkezi ịta site na mbido mbụ. (1,9%). Mbelata nke nlebara seric uric acid na otu canagliflozin bụ nke kachasị ma ọ bụ nso nso na izu n'izu isii ma nọgidesie ike na usoro ọgwụgwọ. Ihe emere ka ọghara imebi ihe uric acid n’ mmamịrị bụ ama ama. Dabere na nsonaazụ nke nchịkọta jikọtara iji ojiji nke canagliflozin na doses nke 100 mg na 300 mg, egosiri na omume nke nephrolithiasis adịghị elu.
Nchekwa Cardiovaskụla
Enweghị mmụba n'ihe egwu dị na obi yana canagliflozin ma e jiri ya tụnyere otu placebo.
Mmekorita
Mmekọrịta Mmanị Ọgwụ (data in vitro)
Canagliflozin enwetaghị ngosipụta nke CYP450 system isoenzymes (3A4, 2C9, 2C19, 2B6 na 1A2) na ọdịbendị nke hepatocytes mmadụ.O gbochighi cytochrome P450 isoenzymes (1A2, 2A6, 2C19, 2D6 ma ọ bụ 2E1) na enweghi ike inagide CYP2B6, CYP2C8, CYP2C9, CYP3A4, dika nyocha nke ulo ogwu jiri microsomes imeju mmadu. Na nyocha nke vitro egosila na canagliflozin bụ mkpụrụ nke metabolizing enzymes ọgwụ UGT1A9 na UGT2B4 na ndị na-ebu ọgwụ P-glycoprotein (P-gp) na MRP2. Canagliflozin bụ ihe na-adịghị ike nke P-gp.
Canagliflozin na-enwe metabolism dị ala. Ya mere, mmetụta dị egwu nke ọgwụ ndị ọzọ na pharmacokinetics nke canagliflozin site na usoro cytochrome P450 bụ eleghi anya.
Mmetụta nke ọgwụ ndị ọzọ na canagliflozin
Ihe omuma nke ulo ogwu gosiputara na ihe omuma nke nmekorita di egwu ya na ogwu eji abia.
Ọgwụ ọjọọ na-eme ka enzymes nke ezinụlọ transferase nke UDF-glucuronyl (UGT)
Ojiji nke oge a na rifampicin, onye na - abụghị onye na - ahọrọ ọtụtụ enzymes nke ezinụlọ UGT na ndị na - ebu ọgwụ ọjọọ, gụnyere UGT1A9, UGT2B4, P-gp, na MRP2 belatara mkpughe nke canagliflozin. Mbelata ikpughere canagliflozin nwere ike ibute mbelata nke arụmọrụ ya. Ọ bụrụ na ọ dị mkpa ịdepụta onye na - eweta ọgwụ enzyme UGT na ndị na - ebu ọgwụ (dịka ọmụmaatụ, rifampicin, phenytoin, phenobarbital, ritonavir), ọ dị mkpa ijikwa mkpokọta gemo nke glycated НbА1c na ndị ọrịa na-anata canagliflozin na oge nke 100 na nke canagliflozin ruo 300 mg 1 oge / ụbọchị, ma ọ bụrụ na nchịkwa glycemic ọzọ dị mkpa.
Ọgwụ na-egbochi enzymes nke ezinụlọ nke transferases UDF-glucuronyl (UGT)
Probenecid: Nchịkọta ojiji nke canagliflozin na probenecid, ihe na-abụghị nhọrọ na-egbochi ọtụtụ enzymes ezinụlọ UGT na ndị na-ebu ọgwụ, gụnyere UGT1A9 na MRP2, enweghị mmetụta dị ukwuu na ụlọ ọgwụ na canagliflozin ọgwụ. Ebe ọ bụ na enzymes abụọ dị iche iche nke gluola nke gluagronlozin nwere glucuronidation site na nnukwu ọrụ / ịdị ala dị ala, mmepe nke akabeghị ahụike nke ọgwụ ndị ọzọ na pharmacokinetics nke canagliflosin site na glucuronidation bụ eleghi anya.
Cyclosporine: Mkparịta ụka ọgwụ dị mkpa na-emetụta ọgwụ na ọnụnọ nke canagliflozin na cyclosporine, onye na-egbochi P-glycoprotein (P-gp), CYP3A na ọtụtụ ndị na-ebu ọgwụ ọjọọ, gụnyere Ahụghị MRP2. Egosiputala mmepe a na-eteghi aka, obere oge “a na-enwu enwu ọkụ” na oge a na-eji canagliflozin na cyclosporine. Ọ dịghị atụ aro ịgha mkpụrụ nke canagliflozin. Enweghị mmekọrịta dị egwu na ndị ọzọ na-egbochi P-gp inhibitors.
Etu ị ga-esi, usoro nchịkwa na usoro onunu ogwu
A na-atụ aro ka a na -emekarị ọgwụ ọnụ otu ugboro n'ụbọchị, ọkacha mma tupu nri ụtụtụ.
Ndị okenye (≥18 afọ)
Usoro a tụrụ aro nke canagliflozin bụ 100 mg ma ọ bụ 300 mg otu ugboro n'ụbọchị, ọkacha mma iwere tupu nri ụtụtụ.
Mgbe ị na-eji canagliflozin dị ka njikọ nke insulin na-agwọ ọrịa ma ọ bụ site na ịkwalite ihe nzuzo ya (dịka ọmụmaatụ, usoro ọgwụgwọ sulfonylurea), enwere ike ịtụle obere ọgwụ ndị dị n'elu iji belata ihe ize ndụ nke hypoglycemia.
Canagliflozin nwere mmetụta diuretic. Ndị ọrịa mesoro diuretics, ndị ọrịa nwere nsogbu ọrụ akụrụ na-arụ ọrụ nke ike na-agaghị agafe agafe (GFR) nke 30 ruo 2, ma ọ bụ ndị ọrịa gbara afọ ≥75, gosipụtara mmụba na-adịghị ala ala nke mmeghachi omume ọjọọ na-emetụta mbelata olu olu intravaskụla (dịka ọmụmaatụ, dizziness postalli. orthostatic hypotension ma ọ bụ hypotension). Ya mere, n’ime ndị ọrịa a, a na-atụ aro iji canagliflozin na ọgwụ mbụ nke 100 mg otu ugboro n’ụbọchị. N'ime ndị ọrịa nwere akara hypovolemia, a na-atụ aro ka a gbanwee ọnọdụ a tupu ọgwụgwọ na canagliflozin. N'ime ndị ọrịa na-anata canagliflozin na dose nke 100 mg na ntachi obi dị mma, bụ ndị chọrọ njikwa glycemic ọzọ, ọ ga-adị mma ka iwelie ọgwụ ahụ gaa na 300 mg.
Dose kwuo
Ọ bụrụ n’otu ụzọ echere, a ga-ewere ya ozugbo o kwere omume, agbanyeghị nke abụọ, ekwesighi ịbanye ya n’otu ụbọchị.
Otu ndị ọrịa pụrụ iche
Undermụaka na-erubeghị afọ 18
A mụbeghị nchekwa na nrụpụta nke canagliflozin n'ime ụmụaka.
Ndị okenye na-arịa ọrịa
Ekwesịrị inye ndị ọrịa ≥75 afọ ka 100 mg otu ugboro kwa ụbọchị dị ka ọgwụ mbido. Site na nnabata ọ dị mma nke 100 mg, ọ bụ ihe amamihe dị na ndị ọrịa chọrọ njikwa glycemic ọzọ iji mee ka ọgwụ ahụ gaa na 300 mg.
Alrụ ọrụ na-arụ ọrụ na ụlọ
N'ime ndị ọrịa nwere nsogbu izizi obere akụrụ (ọnụego ndọtị glomerular filtration (GFR) site na 60 ruo 2), a chọghị ndozi dose.
N'ime ndị ọrịa nwere nsogbu akụrụngwa arụ ọrụ na-adịghị mma, a na-atụ aro iji ọgwụ eme ihe na ọgwụ mbụ 100 mg otu ugboro n'ụbọchị. Site na nnabata ọ dị mma nke 100 mg, ọ bụ ihe amamihe dị na ndị ọrịa chọrọ njikwa glycemic ọzọ iji mee ka ọgwụ ahụ gaa na 300 mg.
A naghị akwado Kanagliflozin maka ndị ọrịa nwere nsogbu akụrụkasị akwara siri ike (GFR 2), ọdịda akụrụngwa ọgwụgwụ na-adịghị ala ala (CRF), ma ọ bụ n'ọrịa ndị ọrịa na-enwe, ebe a na-atụ anya na canagliflozin enweghị ike na ndị ọrịa a.
Mpempe usoro onunu ogwu
100 mg na 300 mg mbadamba ihe mkpuchi fim
N'ime mbadamba 1, ihe eji ọgwụ mgwo oria 100 mg mee ya:
102 mg nke heaghydlozin hemihydrate bụ 100 mg nke canagliflozin.
Ndi ozo (isi): microcrystalline cellulose, lactose anhydrous, shịum croscarmellose, hydroxypropyl cellulose, magnesium stearate.
Ndị na-eme ihe (shei): Opadry II 85F92209 edo edo: mmanya mmanya polyvinyl, mmiri hydrolyzed, titanium dioxide (E171), macrogol / polyethylene glycol 3350, talc, iron oxide odo (E172).
N'ime mbadamba ihe nkiri 300 mg agba agba agba nwere:
306 mg nke canagliflozin hemihydrate bụ 300 mg nke canagliflozin.
Ndi ozo (isi): microcrystalline lactose anhydrous cellulose, croscarmellose sodium, hydroxypropyl cellulose, magnesium stearate.
Ndị na-eme ihe (shei): Opadry II 85F18422 ọcha: mmanya
polyvinyl, nwere mmiri hydrolyzed, titanium dioxide (E171), macrogol / polyethylene glycol 3350, talc.
Maka onunu ogwu nke 100 mg: mbadamba nkume, odo na-acha odo odo, ekpuchie okpu, nke etinyere ya na "CFZ" n'otu akụkụ yana "100" n'akụkụ nke ọzọ.
Maka onunu ogwu nke 300 mg: Mbadamba ihe eji etinye ihe nkiri site na ọcha ruo ihe fọrọ nke nta ka ọ bụrụ ọcha, nke nwere mkpuchi kapịrị, nke a kanyere na "CFZ" n'otu akụkụ yana "300" n'akụkụ nke ọzọ.
Ngwongwo ogwu
Mlọ ọgwụ
Aclọ ọgwụ ọgwụ nke canagliflozin na ndị nwere ahụike yiri ọgwụ ọgwụ nke canagliflozin na ndị ọrịa nwere ọrịa shuga nke afọ 2. Mgbe otu nchịkwa ọnụ nke 100 mg na 300 mg site na ndị ọrụ afọ ofufo nwere ahụ ike, a na-enweta canagliflozin ngwa ngwa, mkpo plasma kachasị (Tmax median) ruru 1-2 awa mgbe ọgwụ ọgwụ. Oke plasma kachasị nke Cmax na AUC nke canagliflozin mụbara oke site na iji doses site na 50 mg ruo 300 mg. Ogologo ndụ ikpeazu pụtara ìhè (t1 / 2) (nke akọwapụtara dị ka “±toodu ọkọlọtọ) bụ awa 10.6 ± 2.13 na elekere 13.1 ± 3.28 mgbe ị na-eji ọgwụ dị 100 mg na 300 mg, otu isi. Etinyela ndọta ahụ ruru 4-5 ụbọchị ka mmalite nke ọgwụ canagliflozin n’otu ọgwụ nke 100-300 mg otu ugboro n’ụbọchị.
Aclọ ọgwụ ọgwụ nke canagliflozin anaghị adabere n'oge. Nchịkọta ọgwụ na plasma ruru 36% mgbe nchịkwa ugboro ugboro.
Egwu
Ogologo bioavailability nke canagliflozin dị ihe dịka 65%. Iri ahiri riri nne riri oke emetụtaghi ọgwụ nke akpukpoloslos, yabụ, enwere ike iburu nri canagliflosin ma ọ bụ n’enweghi nri. Agbanyeghị, na-eburu n'uche ikike nke canagliflozin iji belata mgbanwe dị na glycemia postprandial n'ihi nkwụsịlata mgbatị glucose na eriri afọ, a na-atụ aro iburu canagliflozin tupu nri mbụ..
Nkesa
Ogologo mkpokọta uche nke canagliflozin na mmekorita mgbe otu nrakọta intravenous na ahụike bụ 119 l, nke na-egosi nkesa zuru oke na anụ ahụ. A na-ejikọ Canagliflosin na protein plasma (99%), ọkachasị ya na albumin. Ntinye protin bụ nnwere onwe na mkpokọta plasma nke canagliflozin. Njikọ protein na Plasma adịghị agbanwe agbanwe nke ukwuu na ndị ọrịa nwere nsogbu akwara.
Metabolism
Routezọ nke metabolic excretion nke canagliflozin bụ O-glucuronidation, nke UGT1A9 na UGT2B4 na-arụ ọrụ metabolites abụọ na-adịghị arụ ọrụ O-glucuronide. A na - eleghara metabolism nke canagliflozin nke CYP3A4 (metabolism oxidative) n'ime ụmụ mmadụ (ihe dịka 7%).
Na ihe omumu n'imevitro canagliflozin egbochighị enzymes nke usoro cytochrome P450 CYP1A2, CYP2A6, CYP2C19, CYP2D6 ma ọ bụ CYP2E1, CYP2B6, CYP2C8, CYP2C9 na etinyeghị CYP1A2, CYP, CYP, CYP, CYP, CYP, CYP, CYP, CYP, CYP, CYP, CYP, CYP, CYP, CYP, CYP, CYP, CYP, CYP, CYP, CYP, CYP Nsonaazụ pụtara ọghọm na ntinye uche nke CYP3A4 n'imevivo Achọpụtaghị (lee mpaghara "Mkparịta ụka ọgwụ ọjọọ").
Ojiji
Mgbe otu nchịkwa ọnụ nke 14C canagliflozin dị na ndị ọrụ afọ ofufo ahụike, 41.5%. 7.0% na 3.2% nke ọgwụ redioaktiinara nabatara ka ekwuputere na feces n'ụdị canagliflozin, hydroxylated metabolite na metabolic nke O-glucuronide, karị. Enterohepatic recirculation nke canagliflozin amachaghị.
Ihe dị ka pacenti iri anọ na asaa (40%) nke ọgwụ redio anabatala ka akpụrụ na mmamịrị, ọkachasị n'ụdị metabolites O-glucuronide (30.5%). Ihe na-erughị 1% nke ọgwụ a na-esepụrụ dị ka canagliflozin na-agbanweghi na mmamịrị. Nwepụ nke akụrụngwa canagliflozin mgbe ejiri ya na ọgwụ nke 100 mg na 300 mg sitere na 1.30 ml / min ruo 1.55 ml / min.
Canagliflozin bụ ihe nwere nhichapu dị ala, ebe nkezi usoro nhazi nke ndị ọrụ afọ ofufo mara mma mgbe nchịkwa intraven dị ihe dị ka 192 ml / min.
Ndị otu ọrịa pụrụ iche
Ndị ọrịa nwere ọrụ mgbazinye nsogbu
N'ime nyocha otu ụzọ mepere emepe, a gụrụ ọgwụ pharmacokinetics nke canagliflozin mgbe etinyere ya na 200 mg na ndị ọrịa nwere akwara ezughị oke nke ogo dị iche iche (dịka nhazi ọkwa dabere na nhichapụ creatinine nke Cockcroft-Gault formulament) jiri ya tụnyere ndị mmadụ nwere ahụ ike. Ọmụmụ ihe metụtara ndị ọrịa 8 nwere ọrụ gbasara akụrụngwa nkịtị (mwepụ nke in 80 ml / min), ndị ọrịa 8 nwere nsogbu gbasara akwara dị nro (mwepụ nke 50 ml / min -10% na ≤12%
N'ime ọmụmụ metụtara ndị ọrịa nwere ọkwa HbA1c dị ala> 10% na ≤ 12%, mgbe ị na-eji canagliflozin dị ka monotherapy, mbelata nke ụkpụrụ HbA1c ma e jiri ya tụnyere ntọala (na-enweghị mgbazi) site na -2.13% na -2.56% maka canagliflozin na doses nke 100 mg na 300 mg, n'otu n'otu.
Agencylọ ọrụ European maka nnyocha nke ogo ọgwụ nyere ikike ịnye nsonaazụ nke ọmụmụ ọgwụ Invocana® na ngalaba niile nke ụmụaka nwere ụdị ọrịa shuga 2 (ihe banyere etu esi eme ụmụaka nwere bụ nkebipụtara “ofzọ Ojiji na Ngwọta”).
Ihe ngosi maka ojiji
Mmelite njikwa glycemic na ọgwụgwọ nke ụdị shuga 2 na ndị ọrịa okenye:
- nke ihe oriri na mmega ahụ anaghị enye njikwa glycemic zuru oke yana ojiji nke metformin na-ahụta adịghị mma ma ọ bụ contraindicated.
- dị ka ngwa ọzọ na ọgwụ shuga ndị ọzọ dị ala, gụnyere insulin, mgbe ha, yana nri na mmega ahụ, anaghị enye njikwa glycemic zuru ezu.
Usoro onunu ogwu na nhazi
Ekwesịrị iji ọnụ bute invocana® otu ugboro n'ụbọchị, ọkacha mma tupu nri mbụ.
Ndị okenye (≥ afọ 18)
Usoro akwadoro invocan® nke akwadoro bụ 100 mg otu ugboro kwa ụbọchị. Ndị ọrịa na-anabata 100 mg nke ọgwụ ahụ nke ọma otu ugboro kwa ụbọchị, na ọnụego mkpokọta glomerular filtration (rSCF) ≥ 60 ml / min. / 1.73 m2 ma ọ bụ nwechapụ ihe (CRCl) ≥ 60 ml / min. nchịkwa glucose ọbara, enwere ike ịbawanye dose nke ọgwụ ahụ ka 300 mg otu ugboro kwa ụbọchị (lee akụkụ "ntuziaka pụrụ iche").
Ọ dị mkpa inyocha mmụba nke ọgwụ a maka ndị ọrịa afọ ≥ 75, ndị ọrịa na-arịa ọrịa nke usoro akwara obi, ma ọ bụ ndị ọrịa ndị ọzọ nke ihe kpatara ọrịa mbụ site na ị Invụ Invokana® bụ ihe egwu (lee mpaghara “Ntuziaka Pụrụ Iche”). Maka ndị ọrịa nwere akpịrị mmiri, a na-atụ aro idozi ọnọdụ a tupu ị takingụ ọgwụ Invokana® (lee akụkụ "ntuziaka pụrụ iche").
Mgbe ị na-eji ọgwụ ọgwụ Invokana® dị ka njikọta insulin na ọgwụgwọ ma ọ bụ na - eme ka ndị na - eme ihe dịkwuo elu (dịka ọmụmaatụ, nkwadebe sulfonylurea), iji belata ihe ize ndụ nke hypoglycemia, enwere ike ịtụle ohere nke iji usoro ọgwụ ndị dị n'elu (lee akụkụ "Mmekọrịta Ọgwụ" na "Mmetụta Ọkụ") .
Ndị okenye na-arịa ọrịa ≥ Afọ 65
Ekwesịrị iburu ọrụ ọgbụgba yana ihe nwere ike ịmị nke akpịrị ịkpọ nkụ (lee "Ntuziaka Pụrụ Iche").
Ọrịa enweghị akụrụ
Maka ndị ọrịa nwere eGFR nke 60 ml / min / 1.73 m2 ruo 30%) n'oge ọ bụla n'oge ọgwụgwọ bụ 9.3%, 12.2% na 4.9% n'etiti ndị na-ewere 100 mg, 300 mg canagliflozin na placebo, otu. Na ngwụsị nke ọmụmụ ahụ, a chọpụtara mbelata nke uru a na 3.0% nke ndị ọrịa bụ ndị were 100 mg nke canagliflozin, 4.0% n'etiti ndị were 300 mg, yana 3.3% nke placebo (lee akụkụ "Ntuziaka Pụrụ Iche").
Mkparịta ụka ọgwụ ọjọọ
Canagliflozin nwere ike ịkwalite nsonaazụ nke diuretics, yana ịbawanye n'ihe ize ndụ nke akpịrị ịkpọ nkụ na hypotension (lee akụkụ "ntuziaka pụrụ iche").
Inyocha insulin na insulin na-akpali
Mkpali insulin na insulin na-akpali akpali, dị ka sulfonylureas, nwere ike ibute ọrịa hypoglycemia.
Ya mere, iji belata ihe ize ndụ nke hypoglycemia, ọ dị mkpa iji belata ọgwụ insulin ma ọ bụ onye na-akpali insulin na nzuzo mgbe ejikọtara ya na canagliflozin (lee akụkụ "Usoro Ọgwụ na Nchịkwa" na "Mmetụta Akụ").
Mmetụta nke ọgwụ ndị ọzọ na canagliflozin
Ihe metabolism nke canagliflozin bụ isi n'ihi conjugation na glucuronides, nke mgbasa ozi UDP-glucuronyl transferase 1A9 (UGT1A9) na 2B4 (UGT2B4). Cangliflozin bụ nke P-glycoprotein (P-gp) na protein protein na-egbochi ara ure (BCRP).
Enzyme inducers (dịka St John's wort Hypericum perforatum, rifampicin, barbiturates, phenytoin, carbamazepine, ritonavir, efavirenz) nwere ike belata nsonaazụ nke canagliflozin. Mgbe otu oge a na-eji canagliflozin na rifampicin (onye na-ebugharị ndị na-ebugharị ụgbọ na enzymes dị iche iche na-etinye aka na metabolism), mbelata nke usoro canagliflozin site na 51% na 28% (mpaghara akụkụ, AUC) na mkpo kachasị (Cmax). Mbelata dị otú a nwere ike ibute mbelata nke ọma na canagliflozin.
Ọ bụrụ na ọ dị mkpa iji otu inducer nke enzymes UDP ndị a na mbufe protein na canagliflozin, ọ dị mkpa ijikwa ọkwa glucose iji chọpụta nzaghachi nke canagliflozin. Ọ bụrụ na ọ dị mkpa iji inducer nke enzyme UDF ndị a yana canagliflozin, a na-abawanye ọgwụ ahụ ruo 300 mg otu ugboro n'ụbọchị, ọ bụrụ na nnabata ọ dị mma site n'aka ndị ọrịa 100 mg nke canagliflozin otu ugboro n'ụbọchị, uru RSCF ha bụ ≥ 60 ml / min. / 1.73 m2 ma ọ bụ CrCl ≥ 60 ml / min., ha chọkwara njikwa nke glucose dị n'ọbara. Maka ndị ọrịa nwere eGFR nke 45 ml / min / 1.73 m2 ma ọ bụ ihe na-erughị 60 ml / min / 1.73 m2 ma ọ bụ CrCl nke 45 ml / min. ihe na-erughị 60 ml / min., nke na-ewere 100 mg nke canagliflozin, ma na-ejikwa ọgwụ UDF-enzyme na-enweta ọgwụgwọ concoitant, yana ndị chọrọ nchịkwa nke glucose ọbara, ụdị ọgwụgwọ ndị ọzọ kwesịrị ịtụle iji belata ọkwa glucose (lee akụkụ "Usoro onunu ogwu na ochichi" na "ntuziaka puru iche").
Cholestyramine nwere ike belata mkpụkọ ihu canagliflozin. Ekwesịrị iwere Canagliflozin dịkarịa ala otu elekere tupu awa isii ma ọ bụ awa isii na isii gachaa ọgwụ bile acid iji belata nsonaazụ ha.
Nnyocha ndakọrịta egosila na metformin, hydrochlorothiazide, mgbochi mgbochi a na-ekwu (ethinyl estradiol na levonorgestrol), cyclosporine na / ma ọ bụ probenecid anaghị emetụta ọgwụ pharmokokinetics nke canagliflozin.
Mmetụta nke canagliflozin na ọgwụ ndị ọzọ
Digoxin: ojiji nke canagliflozin n’otu oge kwa 300 mg otu ugboro maka ụbọchị 7 na otu ngwa nke 0,5 mg nke digoxin sochiri 0.25 mg kwa ụbọchị maka ụbọchị 6 mere ka mmụba na AUC nke digoxin site na 20% na mmụba na Cmax 36%, ikekwe n'ihi mgbochi nke P-gp. Achọpụtala Canagliflozin na-egbochi P-gp in vitro. Ekwesịrị inyocha ndị ọrịa na-a digụ digoxin na ihe ndị ọzọ gbasara obi (wdg., Digitoxin).
Dabigatran: Agụbeghị ojiji nke canagliflozin (ihe na-adịghị ike P-gp) na dabigatran etexilate (mkpụrụ nke P-gp). Ebe ọ bụ na itinye uche nke dabigatran nwere ike ịbawanye na ọnụnọ nke canagliflozin, site na iji otu oge dabigatran na canagliflozin, ọ dị mkpa iji nyochaa ọnọdụ onye ọrịa (iji kpochapụ ihe ịrịba ama nke ọbara ọgbụgba ma ọ bụ anaemia).
Simvastatin: jikọtara 300 mg nke canagliflozin otu ugboro kwa ụbọchị maka ụbọchị 6 yana otu ngwa nke 40 mg nke simvastatin (mkpụrụ CYP3A4) butere mmụba na AUC nke simvastatin site na 12% na mmụba na Cmax site 9%, yana mmụba na AUC nke simvastatin acid na 18% na mmụba na Cmax nke simvastatinic acid na 26%. A na-atụle ụdị mmụba ahụ na ihe ndọta simvastatin na simvastatin acid dị ka ọgwụ dị mkpa.
Enweghi ike iwepu mgbochi nke protein cancer ara ure (BCRP) n'okpuru ike canagliflozin na ọkwa nke eriri afọ, yabụ ọ ga - ekwe omume iwelie mmụba nke ọgwụ ndị BCRP na-ebugharị, dịka ọmụmaatụ, ụfọdụ akpụ, dị ka rosuvastatin na ụfọdụ ọgwụ anticancer.
N'ime ihe omumu banyere mmekorita nke canagliflozin na ogha ndi mmadu, enweghi ogwu di egwu banyere ọgwụ nke metformin, ogwu mgbochi (ethinyl estradiol na levonorgestrol), glibenclamide, paracetamol, hydrochlorothiazide na warfarin.
Njikọ Ọgwụ / Mmetụta na Nsonaazụ Laboratory
Ntughari nke 1,5-AG
Rebawanye ume na urinary gluction mgbe ị na-eji canagliflozin nwere ike ibute ntọala nke atụmanya 1,5 (an -rogroglucite) (1,5-AH), n'ihi ihe ọmụmụ 1,5-AH tụfuru ntụkwasị obi ha na ịtụle njikwa glycemic. N'akụkụ a, ekwesighi iji mkpebi siri ike nke 1,5-AH dị ka usoro iji nyochaa njikwa glycemia na ndị ọrịa na-anata Invokana®. Maka ozi zuru ezu karị, a na-atụ aro ịkpọtụrụ ndị nrụpụta nke sistemụ nyocha iji chọpụta 1,5-AH.
Ntụziaka pụrụ iche
Amabeghị ojiji nke canagliflozin na ndị ọrịa nwere ọrịa shuga 1, ya mere akwadoghị ịkọ ya na ụdị ndị ọrịa.
Enweghi ike iji ọgwụ ahụ agwọ ọrịa ketoacidosis nke na-arịa ọrịa shuga, ebe ọ bụ na ọgwụgwọ dị otú ahụ agaghị adị irè n'ọnọdụ ọnọdụ ụlọ ọgwụ a.
Jiri na ndị ọrịa nwere ezigbo ọrụ gbasara akụrụngwa
Candị arụmọrụ canagliflozin na-adabere na ọrụ ndị na-arụ ọrụ na sistemụ, yana arụ ọrụ na-agbada na ndị ọrịa nwere obere akwara na-anaghị ala ala, ọ yikarịrị ka ọ na-anọghị na ndị ọrịa nwere nnukwu akụrụ oke (lee akụkụ "Usoro Ọgwụ na Ọchịchị").
N'ime ndị ọrịa nwere ọnụego mgbazigharị ọnụego 30%), mana emesịa, eGFR mụbara ma wepụta nkwụpụ canniflosin nwa oge n'ọnọdụ ndị adịkarịghị (lee mpaghara “Side side”).
Ekwesịrị ịgwa ndị ọrịa ka ha mata mgbaàmà nke akpịrị. A naghị akwado Canagliflozin maka ndị ọrịa na-a looụ ọgwụ akwara (lee akụkụ “Mmekọrịta Ọgwụ”), ma ọ bụ na-arịa oke mmiri, dịka ọmụmaatụ, na-arịa ọrịa na-arịa oke ọrịa (dịka ọrịa eriri afọ).
A naghị atụ aro iji canagliflozin na ndị ọrịa na-anata ọgwụ akwara (lee akụkụ "Mmekọrịta Ọgwụ") ma ọ bụ na ndị mmadụ nwere mmiri akpịrị, dịka ọmụmaatụ, n'ihe metụtara ọrịa na-arịa ọrịa (dịka ọmụmaatụ, eriri afọ).
Maka ndị ọrịa na-a Invụ ọgwụ Invokana®, na ọnọdụ nke intercurrent ọnọdụ nke nwere ike ibute akpọnwụ (dịka ọmụmaatụ, ọrịa nke eriri afọ), ọ dị mkpa iji nlezianya nyochaa ogo nke akpịrị (dịka ọmụmaatụ, nyocha anụ ahụ, njikwa ọbara mgbali, nyocha ụlọ nyocha, gụnyere ntule nke ọrụ gbasara akụrụ) yana ọkwa ọbara electrolyte. N'ime ndị ọrịa nwetasịrị akpịrị mgbe ị na-arịa Invocana®, ekwesịrị ichebara ịkwụsị Invocana® nwa oge ruo mgbe ọnọdụ ahụ ga-alaghachi na nkịtị. N'ihe banyere iwere ọgwụ, a na-atụ aro ka ị nyochaa ọkwa glucose ugboro ugboro.
N ’ọmụmụ banyere ụlọ ọgwụ na ịre ahịa na ndị ọrịa na-ewere SGLT2 inhibitors, gụnyere canagliflozin, okwu banyere mmepe nke ketoacidosis ọrịa mamịrị (DKA), tinyere okwu gbasara DKA na-egbu ndụ. N'ọtụtụ ọnọdụ, akọwaala ọnọdụ atypical, na mmụba dị ala na mgbanye glucose ọbara erughi 14 mmol / L (250 mg dl). Ọnụọgụ nke DKA nwere ọnụọgụ dị elu nke canagliflozin amabeghị.
E kwesịrị ịtụle ihe ize ndụ nke ịmalite ọrịa ketoacidosis ọrịa shuga dị ka ọgbụgbọ, ọgbụgbọ, ọgbụgbọ, mgbu afọ, akpịrị ịkpọ nkụ, iku ume, ọgba aghara, ike ọgwụgwụ pụrụ iche ma ọ bụ ụra. Ọ bụrụ na ihe mgbaàmà ndị a pụtara, a ga-enyocha ndị ọrịa ozugbo maka ketoacidosis, n'agbanyeghị ogo glucose dị n'ọbara.
N'ọnọdụ enyo enyo maka mmepe nke DKA, yana n'ihe banyere njirimara ya, ndị ọrịa kwesịrị ịkwụsị ọgwụ ozugbo na Invocana®.
Ekwesịrị ka a kwụsịtụrụ ọgwụgwọ ruo nwa oge na ndị ọrịa ụlọ ọgwụ maka ịwa ahụ ma ọ bụ daa ọrịa nke nnukwu ọrịa. N'ọnọdụ abụọ a, mgbe agbatịchara ọnọdụ onye ọrịa, enwere ike ịmaliteghachi ọgwụgwọ na Invocana®.
Tupu ịmalite ọgwụgwọ na Invocana®, ihe niile edepụtara n'akụkọ onye ọrịa nwere ike iduga mmepe nke ketoacidosis kwesịrị ịtụle.
Ihe ndị a gụnyere:
Belata ihe nchekwa beta-cell (dịka ọmụmaatụ, ndị ọrịa nwere ọrịa shuga nke 2 nwere obere C-peptide ma ọ bụ ọrịa shuga autoimmune latent na ndị okenye (LADA) ma ọ bụ ndị ọrịa nwere ọria nke ọrịa pancreatitis)
Conditions ọnọdụ mmachi nri ma ọ bụ akpịrị ịkpọ nkụ
● ndị ọrịa belatara ọgwụ insulin
● ndị ọrịa gosipụtara mmụba na insulin n'ihi mmepe nke ọrịa pathology, ịwa ahụ ma ọ bụ ị alcoholụbiga mmanya ókè
A na-adụ ọdụ iji chekwaa SGLT2 inhibitors na ndị ọrịa a.
A naghị atụ aro ka ịmaliteghachi ọgwụgwọ na onye na - egbochi SGLT2 n'ihe banyere mmepe mbụ nke DKA site na iji ndị na - egbochi SGLT2 ruo mgbe njirimara na iwepu ihe niile doro anya na - akpata nkụda mmụọ.
Onwebeghi nchekwa na ike nke canagliflozin na ndị ọrịa nwere ọrịa shuga nke 1 emebeghị ka akwadoghị ọgwụ Invokana® n'ime ndị ọrịa nwere ụdị shuga 1. Ihe nyocha a na-enyocha ụlọ ọgwụ na-akparaghị ókè na-egosi na DKA yikarịrị ịzụlite na ndị ọrịa nwere ọrịa shuga 1 nke na-ewere ndị na-egbochi SGLT2.
Mgbe ị na-eji canagliflozin, a hụrụ mmụba na hematocrit (lee mpaghara “Side side”), yabụ, n’ime ndị ọrịa nwere oke ebuli ọbara elu, ekwesịrị ịkpachara anya.
Okenye (≥ afọ 65)
Ndị okenye nwere ike nọrọ n'ihe egwu dị elu nke akpịrị ịkpọ nkụ, o yikarịrị ka ha ga-enweta ọrịa afọ, ha nwekwara ike ịrụ ọrụ na-arụ ọrụ ọfụma. N'ime ndị ọrịa ≥ afọ 75, ojiji nke canagliflozin yikarịrị ka ọ ga-akọ mmeghachi omume ndị metụtara mmiri akpịrị ịkpọ nkụ (dịka ọmụmaatụ, postural dizziness, orthostatic hypotension, hypotension). Na mgbakwunye, na ndị ọrịa dị otú ahụ, a kọpụtara mmụba dị ukwuu na eGFR (lee akụkụ "Usoro Ọgwụ na Nchịkwa" na "Mmetụta Akụ").
Fungal ọrịa nke akụkụ ahụ
N'ihi usoro nke canagliflozin onye mgbasa ozi sodium na-adabere na glucose 2 (SGLT2), mgbochi nke ịba ụba ọkwa ịba ọcha n'anya B na ule nyocha n'ụlọ ọgwụ site na iji canagliflozin bụ ndị ụmụ nwanyị nwere ọrịa candvoasis na balantiasis na balanitis ma ọ bụ balanoposthitis na ụmụ nwoke (lee akụkụ “Side Side”) ) Andmụ nwoke na ụmụ nwanyị nwere ọrịa fungal nke akụkụ ọmụmụ ahụ na-enwekarị ọrịa. A na-ahụta ọrịa Balanitis ma ọ bụ ọrịa balanoposthitis n'ime ụmụ nwoke na-anabataghị ibi úgwù. N'ọnọdụ ndị a na-adịghị ahụkebe, a na-akọpụta ọdịdị nke phimosis ma na-emezi ngosipụta nke apịresị. Imirikiti ndị ọrịa nwere ọrịa fungal nke akụkụ ahụ nwa nwoke natara ọgwụ antifungal mpaghara dịka onye nlekọta ahụike nyere ha ma ọ bụ jiri ha mee ihe na-akwụsịghị ọgwụ Invokana®.
Ahụmahụ nke iji ọgwụ ọjọọ eme ihe na ndị nwere nkụda obi obi klas III dị ka nhazi ọkwa nke New York Heart Association (NYHA) bụ nke a kpaara ókè, na emebeghị nnyocha ọmụmụ banyere canagliflozin na NYHA klas obi obi ike IV.
Nnyocha nyocha
Na njikọta usoro nke canagliflozin, n'ime ndị ọrịa na-a Invụ ọgwụ Invokana®, a ga-ekpebi glucose dị na mmamịrị.
Mbadamba ahụ nwere lactose. Ndị ọrịa nwere ọrịa galactose ekweghị ibe nọrọ, ụkọ lactase, ma ọ bụ glucose na ọrịa galactose malabsorption ekwesịghị ị thisụ ọgwụ a.
Enweghị data maka ojiji nke canagliflozin n'ime ụmụ nwanyị dị ime.
Ọmụmụ anụmanụ egosila na o nwere nsí ọmụmụ. Ekwesighi iji Invokana® n'oge di ime. Mgbe etinyere ime, ekwesịrị ịkwụsị ọgwụ na Invocana®.
Amabeghị ma canagliflozin na / ma ọ bụ metabolites ya na mmiri ara ara.
Ihe omuma di na ogwu a ghaputara na anumanu na egosi na canagliflozin / metabolites diri na mmiri ara ehi na ahu ka ana ahuta ihe ndi n’eme ka ogwu ghaputa n’ime umu ahu ndi ara nyere aka na azurughi oke. Ihe ize ndụ a mụrụ ụmụ / ụmụ ọhụrụ agaghị apụ apụ. Ekwesighi iji Invokana® n'oge ara.
A mụbeghị uto nke canagliflozin n’ọrụ ịmụmụ mmadụ.
N'ime ọmụmụ anụmanụ, enweghị mmetụta ọ bụla nke canagliflozin na ọmụmụ.
Akụkụ nke nsonaazụ ọgwụ ahụ nwere ike ịnya ụgbọ ma ọ bụ usoro nwere ike ibute
Invokana® enweghị ma ọ bụ nwee obere mmetụta na ịkwọ ụgbọala ma rụọ igwe.
Agbanyeghị, a ga-eme ka ndị ọrịa mara ihe nwere ike ibute ọrịa hypoglycemia mgbe ha na-eji Invokana® dịka ọgwụ ọgwụgwọ njikọta na insulin ma ọ bụ insulin na-eme ka mkpụrụ ndụ, yana ohere dịwanye ukwuu nke mmeghachi omume ọjọọ metụtara mmiri akpịrị, dị ka nkụchi ọbara (lee akụkụ " Usoro onunu ogwu na ochichi "," ntuziaka puru iche "na" mmetụta ndi ozo ").
Dodoụbiga ya ókè
Ojiji nke canagliflozin na onunu ihe ruru 1600 mg na ndị mmadụ nwere ahụike yana ojiji nke canagliflozin na dose nke 300 mg ugboro abụọ maka izu iri na abụọ n'ime ndị ọrịa nwere ụdị shuga 2 na-anabata nke ọma.
N'ihe banyere ọgwụ ịdoụbiga mmanya ókè, ọ bụ ihe amamihe dị na ya ịme usoro nlekọta mmezi ahụ, dịka ọmụmaatụ, ịme usoro nke iwepu ihe na - adịghị etinye obi ya na eriri afọ, nyochaa ọnọdụ ụlọ ọgwụ ma nye nlekọta ahụike dabere n'ọnọdụ ọrịa. Thezọ kachasị dị irè iji kpochapụ lactate na metformin bụ hemodialysis. Canagliflozin bụ naanị ntakịrị ihe ka m ga-enwe n’oge nnọkọ anọ ọ na-adị n’ọbara. A naghị atụ anya ka Canagliflozin bụrụ nke a na-ahụ maka usoro ịhapụ ọrịa.
Ntụziaka pụrụ iche
Emebeghị ojiji nke canagliflozin na ndị ọrịa nwere ụdị ọrịa shuga 1, ya mere, ejiri ya na contraindicated na otu ndị ọrịa.
Ojiji nke canagliflozin na-egbochi ọrịa ketoacidosis nke ọrịa mamịrị, n'ime ndị ọrịa nwere ọdịda ọdịda na-adịghị ala ala (CRF) ma ọ bụ na ndị ọrịa na-arịa ọrịa akwara, ebe ọgwụgwọ dị otú ahụ agaghị adị irè n'ọnọdụ ndị a.
Carcinogenicity na mutagenicity
Ihe omimi preclinical egosighi ihe obula di egwu nye mmadu, dika ihe omimi nke ihe omimi nke ogwu si di, mmuo nke otutu ogwu, ihe omumu, na omumu aru.
Ọmụmụ
Amabeghị nsonaazụ nke canagliflozin na ọmụmụ mmadụ. Achọpụtaghị mmetụta na ọmụmụ nri n'ọmụmụ anụmanụ.
Hypoglycemia na-eji otu oge eji ọgwụ hypoglycemic ọzọ
Egosiputara ya na ojiji nke canagliflozin dika monotherapy ma obu dika njikọta nke ndi anakpo hypoglycemic (ihe nke ejikọtara ya na mmepe nke hypoglycemia), adịkarịghị eduga na mmepe nke hypoglycemia. A maara nke ọma na insulin na hypoglycemic na-eme ka ihe nzuzo ya dịkwuo elu (dịka ọmụmaatụ, usoro sulfonylurea) na-akpata mmepe nke hypoglycemia. Mgbe ị na-eji canagliflozin dị ka njikọ nke insulin na-agwọ ọrịa ma ọ bụ site na ịkwalite nzuzo ya (dịka ọmụmaatụ, usoro sulfonylurea), nnabata nke hypoglycemia dị elu karịa na placebo.
Ya mere, iji belata ihe eji egbochi hypoglycemia, a na-atụ aro ka ọ belata insulin ma ọ bụ ndị na-eme ka ihe nzuzo ya dị elu.
Mbelata na olu intravascular
Canagliflozin nwere mmetụta diuretic site na ịbawanye ụba nke glucose site na akụrụ, na-akpata osmotic diuresis, nke nwere ike ibute mbelata olu.Na omumu ihe omumu nke canagliflozin, mmụba nke ugboro nke mmeghachi omume ojoo jikọtara ya na mbelata olu intravascular (dịka ọmụmaatụ, postal dizziness, hyperension orthostatic, ma ọ bụ hypotension) na-ahụkarị karịa ọnwa atọ mbụ mgbe eji 300 mg nke canagliflozin. Ndị ọrịa nwere ike ịnwe mmeghachi omume na-emetụta ọnụọgụ nke metụtara intravascular gụnyere ndị ọrịa na-anata "akaghị" diuretics, ndị ọrịa nwere ọrụ ezigharị arụmọrụ nke oke nfe, yana ndị ọrịa afọ 75.
Ndị ọrịa kwesịrị ịkọ akụkọ mgbaàmà nke ogo mbelata intravascular. Mmeghachi omume ọjọọ ndị a na-edugakarị nkwụsị nke ojiji nke canagliflozin ma na-ejikarị ojiji nke canagliflozin na-agbazi mgbanwe site na usoro nke ị drugsụ ọgwụ antihypertensive (gụnyere ọgwụ mgbarụ). N'ime ndị ọrịa nwere mbelata olu intravascular, ọnọdụ a kwesịrị idozigharị tupu ọgwụgwọ ya na canagliflozin.
N'ime izu isii izizi nke ọgwụgwọ canagliflozin, enwere ọnọdụ nke mbelata ntakịrị na ọnụego mkpokọ nke ụwa (GFR) n'ihi mbelata olu olu intravascular. N'ime ndị ọrịa na-atụ aro ka mbelata nke ukwuu na intravascular olu, dị ka egosiri n’elu, enwere mgbe ụfọdụ mgbadata dị ukwuu na GFR (> 30%), nke mechara gbasaa ma oge ụfọdụ chọrọ nkwụsị na ọgwụgwọ canagliflozin.
Fungal ọrịa nke akụkụ ahụ
N'ime ihe omumu ihe omumu, ihe banyere ndi oria ojoo a na akpo aru ike (dika vulvovaginitis na ndi oria vulvovaginal fungal) kariri umunwanyi ndi natara canagliflozin ma e jiri ha na otu placebo. Ndị ọrịa nwere akụkọ ịba ọcha n'anya nke natara ọgwụgwọ canagliflozin nwere ike ịmalite ịmalite ọrịa a. N'ime ndị ọrịa gwọchara canagliflozin, 2.3% nwere ihe karịrị otu ugboro nke ọrịa. Ọtụtụ akụkọ banyere candidiasis vulvovaginal metụtara ọnwa anọ mbụ mgbe ịmalitere ọgwụgwọ canagliflozin. 0.7% nke ndị ọrịa niile kwụsịrị ị canụ ọgwụ canagliflozin n'ihi ọgwụ ọjọọ vulvovaginitis. Nchọpụta nchoputa nke vulvovaginitis, dịka iwu, bụ nke emere na ntọala nke ihe mgbaàmà. Na omumu ihe omumu ihe banyere ulo ogwu, achoputara odi nma nke ogwugwo ogwu nke mpaghara ma obu site n’onu onye dibia doputara ma obu nke anaputara n’adabereghi na usoro ogwu a na-aga n’ihu na canagliflozin.
N'ime ọmụmụ ụlọ ọgwụ, a hụrụ candida balanitis ma ọ bụ balanoposthitis ugboro ugboro na ndị ọrịa a na-emeso canagliflozin na doses nke 100 mg na 300 mg, ma e jiri ya tụnyere ìgwè placebo. Ọrịa Balanitis ma ọ bụ ọrịa balanoposthitis bidoro bụ nke ụmụ nwoke ndị na-anaghị ebi úgwù, ha na-etolitekarị n'ime ụmụ nwoke nwere ọrịa na-arịa balan balanisis. N'ime 0.9% nke ndị ọrịa na-agwọ ọrịa canagliflozin, a chọpụtara ihe karịrị otu ihe ọrịa butere. 0,5% ndị ọrịa niile kwụsịrị ịgwọ canagliflozin n'ihi candida balanitis ma ọ bụ balanoposthitis. N'ime ule nke ụlọ ọgwụ, n'ọtụtụ oge, ndị ọrịa ọgwụ mpaghara jiri dọkịta gwọọ ọrịa ahụ ma ọ bụ were aka ha wee gbasoo usoro ọgwụgwọ na canagliflozin. Akpaala ikpe nke phimosis, mgbe ụfọdụ a na-ebi ugwu.
Ọkpụkpụ ọkpọ
N'ime nyocha nke nsonaazụ obi na 4327 ndị nwere ọrịa ọria obi ma ọ bụ ọrịa obi mgbawa dị elu, ọnya ọnya anụ ahụ bụ 16.3, 16.4, na 10.8 kwa afọ 1,000 nke iji Invocana® mee ihe na afọ nke 100 mg na 300 mg na placebo, n’otu n’otu. Ihe akpachaghị anya ọ nwere banyere mmebi ahụ mere na izu iri abụọ na isii izizi.
Na nchịkọta nyocha nke ọmụmụ ndị ọzọ nke Invokana®, nke gụnyere ihe dị ka ndị ọrịa 5800 na-arịa ọrịa shuga site na ọha mmadụ, ihe kpatara ọnya ọkpụkpụ bụ 10.8, 12.0, na 14.1 n'ime afọ 1,000 onye ọrịa na-eji Invokana® na onunu ogwu nke 100 mg na 300 mg na placebo, n’otu n’otu.
N'ime izu 104 nke ọgwụgwọ, canagliflozin emetụtaghị ịdị nkọ nke ọkpụkpụ.
Mmetụta ikike ịkwọ ụgbọala na usoro
Achọpụtaghị na canagliflozin nwere ike imetụta ikike ịkwọ ụgbọ ala ma jiri usoro rụọ ọrụ. Agbanyeghị, ndị ọrịa kwesiri ịmapụta ihe egwu hypoglycemia mgbe ha na-eji canagliflozin dị ka njikọta insulin na-agwọ ọrịa ma ọ bụ ọgwụ na-eme ka ihe nzuzo ya dịkwuo elu, nke ihe ize ndụ dịwanye elu nke ịmalite mmeghachi omume ọjọọ metụtara ogo intravaskụla dị ala (ọnya ọgbụgba) na ikike na-enweghị ike iji jikwaa ugbo ala na usoro maka mmepe nke mmeghachi omume ọjọọ.
