Atorvastatin (40 mg) Atorvastatin

Atorvastatin 40 mg - ọgwụ na-agbada egbugbere ọnụ site na otu nke statins. Uzo ihe eji eme ogwu a bu iji wedata cholesterol di ala

Otu mbadamba ihe mkpuchi na fim nwere:

• ihe na-arụ ọrụ: atorvastatin calcium trihydrate (na usoro nke atorvastatin) - 40.0 mg,
• ndị na - ahụkarị: microcrystalline cellulose - 103.72 mg, lactose monohydrate - 100,00 mg, calcium carbonate - 20.00 mg, crospovidone - 15.00 mg, sodium carboxymethyl stachi (sodium sitashi glycolate) - 9.00 mg, hyprolose (hydroxypropyl cellulose) - 6, .00 mg, magnesium stearate - 3.00 mg,
• mkpuchi ihe nkiri: hypromellose - 4,500 mg, talc - 1,764 mg, hyprolysis (hydroxypropyl cellulose) - 1,746 mg, titanium dioxide - 0,990 mg ma ọ bụ ngwakọta akọrọ maka mkpuchi ihe nkiri nwere hypromellose (50.0%), talc (19.6%), hyprolose (hydroxypropyl cellulose) (19.4%), titanium dioxide (11.0%) - 9,000 mg.

Mpempe okirikiri biconvex gbara agba, ihe mkpuchi na-acha ọcha ma ọ bụ nke na-acha ọcha Pa cross ngalaba nke isi bụ ọcha ma ọ bụ na-acha ọcha.

Mlọ ọgwụ

Atorvastatin bụ ihe na - egbochi asọmpi HMG-CoA reductase, enzyme dị mkpa nke na - agbanwe 3-hydroxy-3-methylglutaryl-CoA ka mevalonate, ihe ga - ebute steroid, gụnyere cholesterol. Onye nnọchi anya mmanu mmanu mmanu.

N'ime ndị ọrịa na-ahụ maka hyzycholesterolemia na homozygous na heterozygous, ụdị na-abụghị nke ezinụlọ na dyslipidemia, atorvastatin na-ebelata oke mkpokọta cholesterol (Ch) na plasma ọbara. lowpo density lipoprotein cholesterol (Chs-LDL) na apolipoprotein B (apo-B), yana obere npoprotein dị ala (Chs-VLDL) na triglycerides (TG), na-akpata mmụba nke lipoprotein cholesterol (Chs-HDL).

Atorvastatin na-ebelata mkpokọta Chs na Chs-LHNP na plasma ọbara, na-egbochi HMG-CoA mbelata na cholesterol njikọta na imeju na ịbawanye ọnụ ọgụgụ ndị na-anabata "LDL" na sel ahụ, nke na-eduga n'ịba ụba na catabolism nke Chs-LDL.

Atorvastatin na-ebelata mmepụta LDL-C yana ọnụ ọgụgụ nke LDL, na-akpata mmụba na nnọgidesi ike na ọrụ nke LDL na-anabata ya na mgbanwe ruru eru na LDL-uruu, ma na-ebelata mkpokọta nke LDL-C n’ebe ndị ọrịa nwere hyzycholesterolemia na -agagide ọgwụ, na -eme ka ọgwụgwọ na-adịgide adịgide pụtara.

Atorvastatin na doses nke 10 ruo 80 mg belata mkpokọta Chs site na 30-46%, Chs-LDL - site na 41-61%, apo-B - site na 34-50% na TG - site na 14-33%. Nsonaazụ ọgwụgwọ dị ka ndị ọrịa nwere heterozygous familial hypercholesterolemia, ụdị na-abụghị nke ezinụlọ nke hypercholesterolemia na hyperlipidemia agwakọta, gụnyere n'ime ndị ọrịa nwere ọrịa shuga 2.

N'ime ndị ọrịa nwere hypertriglyceridemia dịpụrụ adịpụ, atorvastatin na-ebelata mkpokọta cholesterol, Chs-LDL, Chs-VLDL, apo-B na TG ma na-eme ka ịba ụba nke Chs-HDL. N'ime ndị ọrịa nwere dysbetalipoproteinsemia, atorvastatin na-ebelata itinye uche nke cholesterol intermediate-density lipoprotein (Chs-STD).

N'ime ndị ọrịa nwere ụdị IIa na IIb hyperlipoproteinemia dị ka nkewa Fredrickson, ọnụ ahịa nke ịba ụba ịtawanye nke HDL-C n'oge ọgwụgwọ na atorvastatin (10-80 mg) ma e jiri ya tụnyere uru mbido bụ 5.1-8.7% na-adabereghị na dose ahụ. Enwere mbelata ihe dị ukwuu na-adabere na ogo ahụ: kọlestrọl / Chs-HDL na Chs-LDL / Chs-HDL site na 29-44% na 37-55%, n'otu n'otu.

Atorvastatin na ọgwụ nke 80 mg budata belata ihe egwu nke nsogbu ischemic nsogbu na ịnwụ site na 16% mgbe usoro izu 16 gasịrị, na ihe egwu nke ịbanyeghachi n'ụlọ ọgwụ maka angina pectoris tinyere akara nke methicial ischemia site na 26%. N'ime ndị ọrịa nwere ebumnuche mbụ dị iche iche nke LDL-C (na - enweghị ebili mmiri Q na Myocardial infarction na ụmụ nwoke, ụmụ nwanyị, na ndị ọrịa dị obere karịa karịa afọ 65), atorvastatin na-ebute mbelata ihe egwu nke nsogbu ischemic na ọnwụ.

Mbelata plasma nke mkpokọta LDL-C ka mma ijikọtara ọnụ na atorvastatin karịa na ịta ọkwa plasma. Ahoputara dose a na-eburu n'uche usoro ọgwụgwọ (lee ngalaba "Usoro ọgwụgwọ na nchịkwa").

A na-enweta ọgwụgwọ ahụ izu abụọ ka ebidochara usoro ọgwụgwọ, rute oke mgbe izu anọ gachara wee nọgidesie ike na oge ọgwụgwọ niile.

Egwu

Atorvastatin na-abanye ngwa ngwa mgbe nchịkwa ọnụ gasịrị: oge ​​iji ruo ogo ịta ya (TCmax) na plasma ọbara bụ 1-2 awa. N'ime ụmụ nwanyị, mkpokọ atorvastatin (Cmax) kachasị elu bụ 20%, mpaghara dị n'okpuru usoro ntinye uche (AUC) bụ 10% dị ala karịa nke ụmụ nwoke. Ogo nke nnabata na itinye uche na plasma ọbara na-abawanye na oke na nha. Ezigbo bioavailability bụ ihe dịka 14%, na sistemụ bioav adị nke ọrụ inhibitory na-emegide Htr-CoA reductase bụ ihe dịka 30%. Usoro bioavailability dị ala bụ n'ihi metabolism metabolism na akpụkpọ anụ mucous nke eriri afọ na / ma ọ bụ n'oge "isi ụzọ" site na umeji. Iri ura na -ebelata ọnụego na ogo nnabata nke atorvastatin (site na 25% na 9%, otu aka ahụ, dị ka ihe gosiri na nsonaazụ nke mkpebi Cmax na AUC), agbanyeghị, mbelata nke LDL-C yiri nke ahụ mgbe ị na-ewere atorvastatin na afọ efu. N'agbanyeghi eziokwu na mgbe o nwesasịrị atorvastatin na mgbede, mkpokọta plasma ya dị ala (Cmax na AUC ihe dị ka 30%) karịa mgbe iwere ya n'ụtụtụ, mbelata nke ịta LDL-C abụghị dabere n'oge ụbọchị eji ọgwụ ahụ.

Metabolism

Atorvastatin nwere nnukwu metabolized iji mepụta usoro ortho- na para-hydroxylated na ngwaahịa dị iche iche beta-oxidation. Na vitro, ortho- na para-hydroxylated metabolites nwere mmetụta inhibitory na mbelata HMG-CoA, yana nke atorvastatin. Ọrụ mgbochi mgbochi megide HMG-CoA reductase bụ ihe dịka 70% n'ihi ọrụ nke na-ekesa metabolites. Na nyocha nke vitro na-atụ aro na imeju isoenzyme CYP3A4 na-arụ ọrụ dị mkpa na metabolism nke atorvastatin. E gosipụtara nke a site na mmụba nke mkpokọta atorvastatin na plasma ọbara mmadụ mgbe ị na-ewere erythromycin, nke bụ ihe na-egbochi ịdịpụrụiche a.

Nnyocha ọmụmụ vitro egosikwala na atorvastatin bụ onye na - egbochi ike nke CYP3A4 isoenzyme. Atorvastatin enweghị mmetụta ọfụma n'ihe gbasara ịgwọ ọrịa na plasma ọbara nke terfenadine, nke metabolized bụ nke CYP3A4 isoenzyme; yabụ, mmetụta ya dị ukwuu na pharmacokinetics nke ndị ọzọ nọ na CYP3A4 isoenzyme bụ eleghi anya (lee mmekọrịta na ngalaba ọgwụ ndị ọzọ).

Atorvastatin na metabolites ya bụ ihe kachasị nke nwere ọrịa bile mgbe ọrịa ịba ọcha n'anya na / ma ọ bụ extrahepatic metabolism (atorvastatin anaghị ata ahụhụ enterohepatic recirculation). Ọkara ndụ (T1 / 2) bụ ihe dị ka awa iri na anọ, ebe mmetụta nke inorvastatin na-egbochi ngbanwe HMG-CoA bụ ihe dịka 70% kpebisiri ike site na ọrụ nke ịmegharị metabolites ma were ihe dị ka awa 20-30 n'ihi ọnụnọ ha. Mgbe i takingụsịrị ọgwụ ahụ na mmamịrị, ọ bụ ihe na-erughị 2% nke ọgwụ a nabatara.

Ihe ngosi maka ojiji

• dị ka mgbakwunye nri iji belata cholesterol dị elu, LDL-C, apo-B, na triglycerides na ndị okenye, ndị na-eto eto, na ụmụaka gbara afọ 10 ma ọ bụ karịa nwere hypercholesterolemia, gụnyere ezinụlọ hypercholesterolemia (ụdị heterozygous) ma ọ bụ jikọtara (agwakọta) hyperlipidemia ( ụdị IIa na IIb dịka nhazi nke Fredrickson), mgbe mmeghachi omume nri na usoro ọgwụgwọ ndị ọzọ anaghị ezu ezu,
• iji belata oke cholesterol dị elu, LDL-C n'ime ndị okenye nwere hypercholesterolemia na homozygous familial dị ka mgbakwunye na usoro ọgwụgwọ ndị ọzọ na-agbada ume ọkụ (dịka LDL-apheresis) ma ọ bụ na ọgwụgwọ ndị dị otú ahụ adịghị,

Mgbochi ọrịa obi:

• mgbochi nke ihe gbasara obi na ọrịa ndị okenye n’ohere dị elu nke imepe ihe gbasara ọrịa obi, na mgbakwunye na mgbazi nke ihe ndị ọzọ dị ize ndụ,
• mgbochi nke ọrịa obi na ọrịa obi, iji belata ngụgụ ọnwụ, myocardial infarction, ọrịa strok, nwughari n'ụlọ ọgwụ maka angina pectoris na mkpa ịlọ ụwa.

Ihe ngbanwe

Ihe mgbochi megide iji atorvastatin bu:

• hypersensitivity na atorvastatin na / ma ọ bụ akụkụ ọ bụla nke ọgwụ ahụ,
• ọrịa imeju na-arụ ọrụ ma ọ bụ ihe na-arụ ọrụ nke “transpeases transminates” na ọbara plasma nke ọbara na-amataghị ihe karịrị ugboro atọ ma e jiri ya tụnyere oke nke usoro ahụ.
• cirrhosis nke imeju nke etiology ọ bụla,
• jiri ụmụ nwanyị toruworo ogo ịmụ nwa na-ejighị ụzọ dị mma nke igbochi egbochi,
• ojiji a na-eji jikọrọ ọnụ fusidic acid,
• ruo afọ 10 - maka ndị ọrịa nwere heterozygous familial hypercholesterolemia,
• afọ ruo afọ 18 mgbe ejiri ya dịka njiri mara ndị ọzọ (anaghị edozi ike na nchekwa nke iji),
• afọ ime, na-enye nwa ara
• enweghị lactose, ụkọ lactase, glucose-galactose malabsorption.

Enwere ike ịgwa Atorvastatin nwanyi nke afọ omumu naanị ma ọ bụrụ na amata nke ọma na ọ dịrịghị ime ma gwa ya ihe egwu dị n ’ọgwụ ahụ nye nwa ebu n’afọ.

Iji nlezianya: ị alcoholụbiga mmanya ókè, akụkọ ihe mere eme nke ọrịa imeju, na ndị ọrịa nwere ihe ndị dị ize ndụ maka rhabdomyolysis (arụ ọrụ ezumike nká, hypothyroidism, nkwarụ akwara nke ihe nketa) na ndị ọrịa nwere akụkọ ntolite ma ọ bụ akụkọ ezinụlọ, mmerụ ahụ nke HMG reductase inhibitors ma ọ bụ fibrates na akwara adịlarị. anụ ahụ, afọ karịrị afọ 70, iji ọgwụ ndị ọzọ na-eme ka nsogbu nke myopathy na rhabdomyolysis dịkwuo elu.

Usoro onunu ogwu na nhazi

N'ime. Were oge ọ bụla n'ụbọchị, n'agbanyeghị nri ị na-eri.

Tupu ịmalite ọgwụgwọ na Atorvastatin, ịkwesịrị ịgbalị ịchịkwa hypercholesterolemia site na iji nri, mmega ahụ na oke ibu na ndị ọrịa na-ebu oke ibu, yana ọgwụgwọ nke ọrịa na-akpata.

Mgbe ị na-ede ọgwụ ahụ, onye ọrịa ahụ kwesịrị ikwu ezigbo usoro hypocholesterolemic, nke ọ ga-agbaso n'oge oge ọgwụgwọ niile.

Ọgwụ nke ọgwụ ahụ dịgasị site na 10 mg ruo 80 mg otu ugboro kwa ụbọchị, ana - aha ya bụ iburu n'uche ntinye uche nke LDL-Xc, ebumnuche nke ọgwụgwọ ahụ na nsonaazụ otu onye na ọgwụgwọ ahụ. Oke kachasị kwa ụbọchị nke ọgwụ bụ 80 mg.

Na nmalite ọgwụgwọ na / ma ọ bụ n'oge mmụba nke dose nke Atorvastatin, ọ dị mkpa iji nyochaa mmụba nke lipids na plasma ọbara kwa izu 2-4 ma dozie dose ahụ dabere.

Heterozygous familial hypercholesterolemia

Ọgwụ izizi bụ 10 mg kwa ụbọchị. Ekwesịrị ịhọrọ dose ahụ n'otu n'otu ma nyochaa mkpa ọ dị kwa izu anọ na mmelite ọ bụla nwere ike iru 40 mg kwa ụbọchị. Mgbe ahụ enwere ike ịbawanye dose ahụ ruo ogo 80 mg kwa ụbọchị, ma ọ bụ ngwakọta nke usoro bile acid na iji atorvastatin na dose 40 mg kwa ụbọchị ga-ekwe omume.

Jiri n'ime ụmụaka na ndị nọ n'afọ iri na asatọ ruo afọ iri na isii na ọrịa hypercholesterolemia.

Usoro akwadoro ịmalite bụ 10 mg otu ugboro n'ụbọchị. Enwere ike ịbawanye ọgwụ ahụ ruo 20 mg kwa ụbọchị, dabere na nsonaazụ ụlọ ọgwụ. Ahụmịhe nwere ihe karịrị 20 mg (nke kwekọrọ na dose 0,5 mg / n'arọ) nwere mmachi. Ọ dị mkpa titate dose nke ọgwụ dabere na ebumnuche nke ọgwụgwọ lipid-wedering. Ekwesịrị imeghari dose na oge nke oge 1 n'ime izu anọ ma ọ bụ karịa.

Jiri na ọgwụ ndị ọzọ

Ọ bụrụ na ọ dị mkpa, iji ya eme ihe na cyclosporine, telaprevir ma ọ bụ ngwakọta nke tipranavir / ritonavir, ọgwụ Atorvastatin nke ọgwụ ahụ agaghị agafe 10 mg kwa ụbọchị.

Ekwesịrị iji nlezianya mee ihe yana iji ọgwụ atorvastatin dị ala kachasị mma mgbe ejiri ya na ndị na - egbochi nje HIV, hepatitis C virusase inhibitors (boceprevir), clarithromycin na itraconazole.

Nsonaazụ

Mgbe ị na-ewere Atorvastatin, nsonaazụ ndị a nwere ike ime:

• Site na usoro ụjọ ahụ: ehighị ụra nke ọma, isi ọwụwa, ọrịa asthenic, malaise, dizzness, neuropathy na-efe efe, amnesia, paresthesia, hypesthesia, ịda mba.
• Site na usoro nri: ọgbụgbọ, afọ ọsịsa, mgbu nke afọ, dyspepsia, flatulence, afọ ntachi, vomiting, anorexia, ịba ọcha n'anya, pancreatitis, cholestatic jaundice.
• Site na usoro akwara: myalgia, azụ mgbu, ogbu na nkwonkwo, ọnya afọ, myositis, myopathy, rhabdomyolysis.
• Mmeghachi omume Allergic: urticaria, pruritus, anụ ahụ na-akpata, ihe na-efe efe, anaphylaxis, polymorphic exudative erythema (gụnyere ọrịa Stevens-Johnson syndrome), ọrịa Laille.
• Site na akụkụ ahụ na hemopoietic: thrombocytopenia.
• Site n'akụkụ nke metabolism: hypo- ma ọ bụ hyperglycemia, ụba ọrụ serum CPK.
• Site na usoro endocrine: mellitus ọrịa shuga - ugboro ole mmepe ga-adabere na ọnụnọ ma ọ bụ enweghị ihe ndị dị ize ndụ (glucose ≥ 5.6, nchịkọta anụ ahụ> 30 n'arọ / m2, mmụba nke triglycerides, akụkọ ihe mere eme nke ọbara mgbali).
• Ndị ọzọ: tinnitus, ike ọgwụgwụ, mmekọahụ dysfunction, akụkụ akụkụ, oke ibu, obi mgbu, alopecia, ikpe nke mmepe nke ọrịa interstitial, karịsịa na-eji ogologo oge, ọbara ọgbụgba (mgbe ewere ya na oke onunu na ya na CYP3A4 inhibitors), Secondal renal odida.

Doụbiga nrịba ama

Edebebeghị ihe ịrịba ama nke ịdoụbiga mmanya ókè. Mgbaàmà nwere ike ịgụnye mgbu na imeju, nnukwu akụrụ akwara, iji myopathy na rhabdomyolysis ruo ogologo oge.

N'ihe banyere ịdoụbiga mmanya ókè, ọ dị mkpa usoro ndị a dị mkpa: nleba anya na idobe ọrụ dị mkpa, yana igbochi ọzọ ị ofụ ọgwụ (eriri afọ, ị ,ụ ya ma ọ bụ ọgwụ mgbu).

Site na mmepe nke myopathy, nke rhabdomyolysis na nnukwu akụrụ gbasara ọdịda, a ga-akagbu ọgwụ ahụ ozugbo na infusion nke diuretic na sodium bicarbonate malitere. Rhabdomyolysis nwere ike iduga hyperkalemia, nke chọrọ nchịkwa intravenous nke ihe ngwọta nke calcium chloride ma ọ bụ ihe ngwọta nke calcium gluconate, infusion nke 5% ngwọta nke égbè mmiri (glucose) na insulin, yana iji resins potassium.

Ebe ọgwụ a na - eme ka protein ndị dị na plasma na - arụ ọrụ, akụrụngwa ọria adịghị arụ ọrụ.

Mpempe usoro onunu ogwu

Mbadamba ụrọ ekpuchi 10 mg, 20 mg na 40 mg

Otu mbadamba ihe nwere:

ike - atorvastatin (dị ka nnu nnu nke trihydrate) 10 mg, 20 mg na 40 mg (10.85 mg, 21.70 mg na 43.40 mg),

ndị mbụ: carbon dioxide, crospovidone, sodium lauryl sulfate, sịlịkọn dioxide, colloidal anhydrous, talc, cellulose microcrystalline,

ihe mejupụtara shei: Opadry II pink (talc, polyethylene glycol, titanium dioxide (E171), polyvinyl mmanya, iron (III) oxide edo edo (E172), iron (III) oxide na-acha uhie uhie (E172), iron (III) oxide ojii (E172).

Mbadamba ụrọ a na-acha odo odo nwere agba biconvex

Ngwongwo ogwu

Mlọ ọgwụ

Atorvastatin na-agbakarị ngwa ngwa mgbe nchịkwa ọnụ gasịrị, plasma ịta ya ruru ogo kachasị elu ruo awa 1 - Oge bioavailability nke atorvastatin bụ 95-99%, zuru oke - 12-14%, systemic (na-enye mgbochi nke HMG-CoA mbelata) - ihe dị ka 30 % A na-akọwa bioavailability usoro dị ala site na mkpocha usoro na mucous akpụkpọ ahụ nke eriri afọ na / ma ọ bụ metabolism n'oge akụkụ mbụ site na umeji. Mwepu na ịta Plasma na-abawanye na oke nke ọgwụ a. N'agbanyeghi eziokwu na mgbe ejiri nri, nnabata nke ọgwụ na-ebelata (ịta ahụ kachasị na AUC bụ ihe dị ka 25 na 9%, dị iche iche), mbelata LDL cholesterol na-adabere na atorvastatin ewere na nri ma ọ bụ. Mgbe ị na-ewere atorvastatin na mgbede, plasma ịta ya dị ala (ihe dịka 30% maka ịta kachasị na AUC) karịa mgbe ị na-ewere ya n'ụtụtụ. Agbanyeghị, mbelata ogo LDL cholesterol na-adabere na oge ị theụ ọgwụ.

Ihe karịrị 98% nke ọgwụ ahụ na-egbochi protein ndị dị na plasma. Ogo nke erythrocyte / plasma ruru ihe dị ka 0.25, nke na-egosi itinye ọgwụ na-esighi ike n'ime sel ọbara.

Atorvastatin bụ metabolized ka ortho- na para-hydroxylatederi na ngwaahịa dị iche iche beta-oxidized. Mmetụta inhibitory ọgwụ a na-emetụta HMG-CoA reductase bụ ihe dịka 70% rụpụtara n'ihi ọrụ nke na-ekesa metabolites. Achọtara Atorvastatin ka ọ bụrụ onye na - egbochi cytochrome P450 ZA4 nke adịghị ike.

Atorvastatin na metabolites ya bụ ihe kachasị nke bile na mgbe ọrịa ịba ọcha n'anya na / ma ọ bụ extrahepatic metabolism. Ka osila dị, ọgwụ ahụ enweghị ike ịnagide ọnụnọ ọrịa dị ukwuu. Ogologo ndụ ọkara nke atorvastatin fọrọ nke nta ka ọ bụrụ awa iri na anọ, mana oge nke inhibitory mmegide megide HMG-CoA reductase n'ihi ịgbanye metabolites na-arụ ọrụ bụ awa 20-30. Ihe na-erughị 2% nke onorvastatin ọnụ na-apụta na mmamịrị.

Ngwakọta plasma nke atorvastatin na ndị agadi nwere ahụike (karịa 65) dị elu (ihe dị ka 40% maka ịta kachasị na 30% maka AUC) karịa ndị na-eto eto. Enweghị ọdịiche na ịdị irè nke ọgwụgwọ na atorvastatin na ndị ọrịa agadi na ndị ọrịa nke ndị ọgbọ ọzọ.

Ntinye uche nke atorvastatin na plasma ọbara n'ime ụmụ nwanyị dị iche na njupụta nke plasma ọbara n'ime ụmụ nwoke (n'ime ụmụ nwanyị, ntinye uche kachasị bụ ihe dịka 20% dị elu, yana AUC - 10% dị ala). Agbanyeghị, enweghị ọdịiche pụtara ìhè dị n'etiti ahụike achọpụtara na nsonazụ nke ogo nwoke na ụmụ nwanyị.

Ọrịa akụrụ anaghị emetụta mkpokọta ọgwụ na plasma ma ọ bụ nsonaazụ nke atorvastatin na ọkwa nke lipid, yabụ ọ dịghị mkpa nhazigharị dose na ndị ọrịa nwere ọdịda akụrụ. Ọmụmụ ihe ahụ ekpuchighị ndị ọrịa nwere nsogbu akwara dị n'ọgwụgwụ; ikekwe, hemodialysis anaghị agbanwe oke mkpochapu nke atorvastatin, ebe ọ bụ na ọgwụ fọrọ obere ka ọ bụrụ ihe niile metụtara protein plasma.

Ntinye uche nke atorvastatin na plasma ọbara na-abawanye nke ukwuu (ịta kachasị - ihe dịka ugboro 16, AUC - ugboro 11) na ndị ọrịa nwere ọrịa imeju nke etiology na-egbu egbu.

Mlọ ọgwụ

Atorvastatin bụ ihe na - egbochi mpịakọta nke HMG-CoA reductase-enzyme, nke na - ahazi ọnụego ntụgharị nke HMG-CoA na mevalonate - ihe ntụgharị nke sterols (gụnyere kọlesterol (cholesterol)). N'ime ndị ọrịa na-ahụ maka hyzycholesterolemia na ụdị ọrịa hyzycholesterolemia, ụdị ekesa hypercholesterolemia na dyslipidemia, atorvastatin na-ebelata mkpokọta cholesterol, obere lipoproteins dị ala (LDL) na apolipoprotein B (Apo B). Atorvastatin na --ebelata mkpụkọ nke lipoproteins dị obere (VLDL) na triglycerides (TG), na - emekwa ka ọdịnaya nke cholesterol dị elu nke lipoproteins dị elu (HDL) dị ala.

Atorvastatin belatara ọkwa cholesterol na lipoproteins na plasma ọbara site na igbochi HMG-CoA reductase, njikọ nke cholesterol na imeju na ịba ụba nke ndị na-anabata LDL n'elu hepatocytes, nke a na-esonyere na mmụba na catabolism nke LDL. Atorvastatin na-ebelata mmepụta LDL, na-akpata mmụba ọnụ na-adịgide adịgide na ọrụ nnabata LDL. Atorvastatin na-agbadata ọkwa LDL n'ụzọ dị irè na ndị ọrịa nwere hypercholesterolemia homozygous familial, nke a na-agaghị enwe ike ịgwọ ọrịa ọgwụgwọ ọkọlọtọ.

Ebe izi ezi nke atorvastatin bụ imeju, bụ nke na-arụ nnukwu ọrụ na njikọta cholesterol na mkpochapu nke LDL. Mbelata ogo LDL cholesterol na-agbaso na oke ọgwụ ahụ yana itinye uche ya na ahụ.

Atorvastatin na dose nke 1080 mg belatara ọkwa cholesterol zuru oke (site na 30- 46%), LDL kọlesterol (site na 41-61%), Apo B (site na 34-50%) na TG (site na 14-33%). Nsonaazụ a kwụsiri ike na ndị ọrịa nwere hypercholesterolemia heterozygous, ụdị hypercholesterolemia na ụdị hyperlipidemia, gụnyere ndị ọrịa nwere ọrịa mellitus na-abụghị insulin.

N'ime ndị ọrịa nwere hypertriglyceridemia dịpụrụ adịpụ, atorvastatin na-ebelata ọkwa nke cholesterol ngụkọta, LDL cholesterol, VLDL cholesterol, Apo B, TG ma nwetakwuo ọkwa HDL cholesterol. N'ime ndị ọrịa nwere dysbetalipoproteinemia, atorvastatin na-ebelata ọkwa nke imeju cholesterol na-ebelata.

N'ime ndị ọrịa nwere ụdị IIa na hyblipoproteinemia (dị ka nhazi Fredrikon), ogo nke mmụba nke cholesterol HDL mgbe ị na-eji atorvastatin na ọgwụ 10-80 mg bụ 5.1-8.7%, n'agbanyeghị agbanyeghị. Na mgbakwunye, enwere mbelata nke ukwuu dabere na oke nke cholesterol / HDL cholesterol na HDL cholesterol. Ojiji nke atorvastatin na-ebelata ihe ize ndụ nke ischemia na ọnwụ n'ime ndị ọrịa nwere infarction myocardial na-enweghị ebili mmiri na angina na-akwụghị chịm (n'agbanyeghị agbụrụ na nwoke na nwanyị) bụ nha anya na ọkwa LDL cholesterol.

Heterozygous metụtara hypercholesterolemia na ọrịa ụmụaka. N'ime ụmụ nwoke na ụmụ nwanyị gbara afọ iri na 10 ruo afọ na heterozygous familial hypercholesterolemia ma ọ bụ hypercholesterolemia siri ike, atorvastatin na 10-20 mg otu ugboro kwa ụbọchị belata ọkwa cholesterol zuru oke, LDL cholesterol, TG na Apo B na plasma ọbara. Agbanyeghị, enweghi mmetụta pụtara ìhè na uto na uto nwoke na ụmụ nwoke ma ọ bụ oge oge nwoke gafere na nwata. A mụbeghị nchekwa na arụmọrụ nke onyunyo karịa 20 mg maka ọgwụgwọ ụmụaka. Emebeghi mmetụta nke oge ọgwụgwọ atorvastatin na nwata na mbelata ọrịa na ọnwụ na-eto eto.

Usoro onunu ogwu na nhazi

Tupu ịmalite Atorvastatin ọgwụ, ọ dị mkpa iji chọpụta ọkwa cholesterol dị n'ọbara megide usoro nri kwesịrị ekwesị, dezie mmega ahụ ma mee ihe iji belata oke ahụ n'ahụ ndị ọrịa nwere oke ibu, yana ịme ọgwụgwọ maka ọrịa ndị kpatara ọrịa. N'oge ọgwụgwọ na atorvastatin, ndị ọrịa kwesịrị ịgbaso usoro hypocholesterolemic nke ọkọlọtọ. Edere ọgwụ ahụ na ọgwụ nke 1080 mg otu ugboro kwa ụbọchị, n'oge ọ bụla, mana n'otu oge nke ụbọchị, n'agbanyeghị nri. Enwere ike ịhazi usoro mmalite na mmezi dịka ọkwa mbu nke cholesterol LDL, ebumnuche na arụmọrụ nke ọgwụgwọ. Ka izu 2-4 gachara site na mbido ọgwụgwọ na / ma ọ bụ ndozigharị ya na Atorvastatin, ekwesịrị ịhapụ profaịlụ egbugbere ọnụ ya ma dozie ọgwụ ahụ otu ya.

Hypercholesterolemia nke mbu yana agwakọta hyperlipidemia. N'ọnọdụ ka ukwuu, iji zuo ọgwụ na ọgwụ 10 mg otu ugboro kwa ụbọchị. Mmetụta ọgwụgwọ na-etolite mgbe izu abụọ gasị, nsonaazụ kachasị - mgbe izu anọ gachara. A na-akwado mgbanwe dị mma site na iji ọgwụ ogologo oge.

Homozygous familial hypercholesterolemia. Edere ọgwụ ahụ na ọgwụ nke 10 ruo 80 mg otu ugboro kwa ụbọchị, n'oge ọ bụla, n'agbanyeghị nri oriri. Mbido na usoro ịchekwa usoro atọrọ ahọpụtara n’otu n’otu. N'ọtụtụ oge, n'ime ndị ọrịa nwere hypercholesterolemia homozygous, a na-enweta nsonaazụ ya site na iji Atorvastatin na dose 80 mg otu ugboro n'ụbọchị.

Heterozygous familial hypercholesterolemia na pediatrics (ndị ọrịa dị afọ 10-17). Atorvastatin na-atụ aro na usoro ọgwụgwọ mbụ.

10 mg otu ugboro kwa ụbọchị. Ogwu a tụrụ aro ya kacha ukwuu bụ milimita iri abụọ n'otu ụbọchị kwa ụbọchị (a gụrụbeghị ọgwụ ndị o mere ihe karịrị 20 mg na ndị ọrịa ọgbọ a). A na-edobe dose ahụ n’otu n’otu, na-eburu n’uche ebumnuche ọgwụgwọ, enwere ike idozi ọnụọgụ ahụ n’etiti nkeji anọ ma ọ bụ karịa.

Jiri na ndị ọrịa nwere akụrụ na akụrụ odida. Ọrịa akụrụ anaghị emetụta mkpokọta atorvastatin ma ọ bụ mbelata cholesterol plasma LDL, yabụ enweghị mkpa maka idozi dose.

Jiri ndị ọrịa agadi. Enweghị ọdịiche dị iche iche na nchekwa na ịdị irè nke ọgwụ na ọgwụgwọ hypercholesterolemia na ndị ọrịa agadi na ndị ọrịa okenye mgbe afọ 60 gasịrị.

Ndị ọrịa nwere ọria imeju Edere ọgwụ ahụ na ịdọ aka na ntị n'ihe metụtara nkwụsịlata mkpocha ọgwụ ahụ ahụ. Egosiputara parampat na ulo ogwu ka egosiputara, ma oburu na achoputara mgbanwe di omimi, ikwesiri ibelata ogwu ma obu ogwu ya.

Ọ bụrụ na emere mkpebi na njikọta nke Atorvastatin na CYP3A4 inhibitors, mgbe ahụ:

Gbalịa ịmalite oge ọgwụgwọ na obere opekata mpe (10 mg), ijide n'aka na ị ga-elezi mkpụrụ egbugbere ọnụ tupu ị na-enye ya oke.

Can nwere ike ịkwụsị ị Atụ Atorvastatin nwa oge ma ọ bụrụ na etinyere ndị na - egbochi CYP3A4 na usoro dị mkpirikpi (dịka ọmụmaatụ, obere usoro nke ọgwụ nje dịka clarithromycin).

Ndụmọdụ gbasara ọnụọgụ Atorvastatin kachasị mgbe ị na-eji:

ya na cyclosporine - ọ̀gaghị kwesịrị gafere 10 mg,

ya na clarithromycin - dose ahụ agaghị akarị 20 mg,

ya na itraconazole - ogwu a gha apughi ibu 40 mg.

Mkparịta ụka ọgwụ ọjọọ

Ewu nke myopathy na-abawanye n'oge a na-eji ọgwụ ndị ọzọ na klaasị agwọ ọrịa mgbe iji cyclosporine, ọgwụ nke fibric acid, erythromycin, antifungals metụtara azoles, na nicotinic acid..

Antacids: n'otu oge nkwusioru nke nwere magnesium na aluminom hydroxide belatara mkpokọta atorvastatin na plasma ọbara site na 35%, agbanyeghị, ogo nke Mbelata LDL cholesterol agbanwebeghị.

Antipyrine: Atorvastatin anaghị emetụta ọgwụ ọgwụ nke antipyrine, yabụ, mmekọrịta na ọgwụ ndị ọzọ metabolized site na otu cytochrome isoenzymes anaghị atụ anya.

Amlodipine: Na nyocha nke mmekorita ọgwụ ọgwụ na mmadụ dị iche iche, nchịkwa nke atorvastatin n’otu oge na 80 mg na amlodipine na dose 10 mg dugara na mmụba nke atorvastatin site na 18%, nke abụghị ihe gbasara ọgwụgwọ.

Gemfibrozil: n'ihi ịba ụba nke ịmalite myopathy / rhabdomyolysis na ojiji nke HMG-CoA reductase inhibitors na gemfibrozil, nchịkwa oge a ga-ezere.

Ndị ọzọ fibrates: n'ihi ịba ụba nke myopathy / rhabdomyolysis na ojiji nke oge HMG-CoA reductase inhibitors na fibrates, atorvastatin kwesịrị iji nlezianya depụta ya mgbe ị na-etinye fibrates.

Nicotinic acid (niacin): enwere ike ịbawanye myopathy / rhabdomyolysis mgbe ị na-eji atorvastatin yana nicotinic acid, yabụ, n'ọnọdụ a, ekwesịrị ịtụle iji belata usoro onorvastatin.

Colestipol: n'iji colestipol n'otu oge, ntinye uche nke atorvastatin na plasma ọbara belatara ihe ruru 25%. Agbanyeghị, mmetụta dị ala nke njikọta nke atorvastatin na colestipol karịrị nke ọgwụ ọ bụla n’otu n’otu.

Nchikota: site na iji atorvastatin na oge nke cochicine, a kọọrọ ihe banyere myopathy, gụnyere rhabdomyolysis, ya mere a ga-eji kpachara anya mgbe ị na-ede akwụkwọ atorvastatin na colchicine.

Digoxin: site na nchịkwa digoxin na atorvastatin ugboro ugboro na 10 mg, nchikota nke digoxin na plasma ọbara agbanweghị. Ka osi di, mgbe eji digoxin na atorvastatin na onwa 80 mg / ubochi, ntughari nke digoxin riri elu dika 20%. Ndị ọrịa na-anata digoxin na mgbakwunye na atorvastatin chọrọ nlebara anya kwesịrị ekwesị.

Erythromycin / clarithromycin: n'iji atorvastatin na erythromycin (500 mg ugboro anọ n'ụbọchị) ma ọ bụ clarithromycin (500 mg ugboro abụọ n'ụbọchị), nke na-egbochi cytochrome P450 ZA4, mmụba na mkpokọta nke atorvastatin na plasma ọbara.

Azithromycin: n'iji atorvastatin eme ihe n'otu oge (10 mg otu ugboro n'ụbọchị) yana azithromycin (500 mg / otu ugboro n'ụbọchị), itinye uche nke atorvastatin na plasma agbanweghị.

Terfenadine: n'iji atorvastatin na terfenadine na-emekọ ihe, achọpụtaghị mgbanwe dị ukwuu na ụlọ ọgwụ ọgwụ nke terfenadine.

Ogwu ogwu mgbochi: ka ị na-eji atorvastatin na ọgwụ mgbochi nwere noareindrone na ethinyl estradiol, a na-ahụwanye mmụba na AUC nke norethindrone na ethinyl estradiol ihe dịka 30% na 20%, n'otu n'otu. E kwesịrị ịtụle mmetụta a mgbe ị na-ahọrọ ọgwụ mgbochi nwanyị maka nwanyị na-ewere atorvastatin.

Warfarin: mgbe a na-amụ nmekorita nke atorvastatin na warfarin, enweghị akara nke mmekọrịta dị oke mkpa nke ụlọ ọgwụ.

Cimetidine: mgbe ị na-amụ mmekọrịta nke atorvastatin na cimetidine, enweghị akara nke mmekọrịta dị oke mkpa nke ụlọ ọgwụ.

Ndị Na - egbochi Ahụhụ: n'otu oge eji atorvastatin nwere ndị na-egbochi nchebe nke a maara cytochrome P450 ZA4 inhibitors tinyere mmụba nke mkpokọta plasma nke atorvastatin.

Aro maka iji juputara atorvastatin yana ndị na - egbochi nje HIV:

Mwepụta wepụtara ya na ihe mejupụtara

A na-enye ndị na-emepụta ọgwụ ọgwụ n'ụdị mbadamba na ọgwụ. Ihe na - arụ ọrụ nke ọgwụ ahụ bụ atorvastatin calcium trihydrate (40 mg na mbadamba ọ bụla).

Ihe ndi ozo: microcrystalline cellulose, calcium carbonate, StarKap 1500 complex (pregelatinized stachi na ọka stachi), aerosil, magnesium stearate, titanium dioxide, talc, macrogol, acha uhie uhie, iron oxide, odo odo, ihe omucha iron, mmanya na-egbu polyvinyl).

Ihe ngwugwu ahụ nwere 1.2 ma ọ bụ 3 blisters nke 10.15 ma ọ bụ mbadamba 30.

Mkparịta ụka ọgwụ ọjọọ

Ojiji nke oge ahụ na ndị na-egbochi nje bacteria (erythromycin, clarithromycin), ọgwụ antifungal (fluconazole, ketoconazole, itraconazole), cyclosporine, ihe dị na fibroic acid na-eme ka mkpokọta atorvastitis na ihe ize ndụ nke ịmalite myalgia.

Ojiji nke oge a na mgbochi, nke gụnyere magnesium na aluminom, nyere aka na mbelata mkpokọta atorvastatin. Nke a emetụtaghị ọkwa nke iwetulata cholesterol na obere lipoproteins dị ala.

Womenmụ nwanyị na-a takeụ ọgwụ mgbochi ọnụ kwesịrị iburu n'uche na atorvastatin nwere ike ịbawanye ụba nke ethinyl estradiol na norethindrone.

Nchikota choro nlezianya: nchikota nke atorvastatin yana ogwu nke n’enye aka belata mkpoko homonụ steroid (spironolactone, ketoconazole).

Achọpụtaghị mmekọrịta ndị na-adịghị mma nke atorvastatin na ọgwụ antihypertensive.

Emeghachi ọgwụ ọgwụ nke atorvastatin 40

Ihe na-arụ ọrụ nke ọgwụ ahụ nwere ọrụ akpọlata egbugbere ọnụ yana nke otu statins. Akụkụ ahụ na-egbochi HMG-CoA reductase, enzyme pụrụ iche nke na-agbanwe ụdị A hydroxymethylglutaryl coenzyme na mevalonic acid.

Ọgwụ na-ebelata nguzobe nke LDL (lipoproteins dị ala) ma na-eme ka ọrụ nke ndị na-anabata LDL dịkwuo ala. Na mgbakwunye, na ndị ọrịa nwere hypercholesterolemia, ọgwụ ahụ na-ebelata LDL.

Ọzọkwa, ọgwụ ahụ na-agbada ọkwa nke Ho (ngụkọta cholesterol ma na-abawanye cholesterol nke nnukwu lipoproteins (HDL)).

Atorvastatin nwere mmetụ miri emi. Plasma statin nwetara ntinye uche kachasị na nkeji 60-120. Nri ura na -ebelata oge iwere ogwu a.

Ihe nwere bioav adị nke 12%. Ihe mejupụtara ya bụ mejupụtara na akwara nke imeju. A na-ewepụ ọgwụ ahụ na bile. Ọkara ọkara nke atorvastatin bụ awa 14. Ihe dị ka 2% nke ọgwụ ọgwụ ahụ bụ akụrụ. Usoro ọgwụgwọ emetụtaghị profaịlụ ọgwụ nke ọgwụ ahụ.

Ntụziaka pụrụ iche

Atorvastatin nwere ike ibute mmụba na CPK serum, nke ekwesiri iburu n'uche na nchọpụta ọdịiche nke mgbu obi. Okwesiri iburu n’uche na mmụba na CPK ugboro 10 ma e jiri ya tụnyere usoro, yana myalgia na adịghị ike nwere ike jikọta myopathy, a ga-akwụsị ịgwọ ya.

Site na iji atorvastatin na-eme n'otu oge na cytochrome CYP3A4 protease inhibitors (cyclosporine, clarithromycin, itraconazole), ekwesịrị ịmalite mkpụrụ mbụ na 10 mg, yana obere usoro ọgwụgwọ ọgwụ, atorvastatin kwesịrị ịkwụsị.

Ọ dị mkpa iji oge niile na-eleba anya n'ihe ndị na-egosi ọrụ imeju tupu ọgwụgwọ, 6 na izu iri na abụọ mgbe mmalite nke ọgwụ ma ọ bụ mgbe ịbawanye ọgwụ, na oge kwa oge (ọnwa 6 ọ bụla) n'oge oge niile eji eme ihe (ruo mgbe nhazi nke ọnọdụ ndị ọrịa nke ọkwa transaminase ya gafere. ) A na-ahụ mmụba nke transpekere “hepatic” tumadi n'ime ọnwa atọ mbụ nke nchịkwa ọgwụ. Ọ na-atụ aro ịkagbu ọgwụ ma ọ bụ belata dose ahụ na mmụba na AST na ALT karịa ugboro atọ. Ojiji nke atorvastatin kwesịrị ịkwụsị ruo nwa oge ma ọ bụrụ na mmepe nke mgbaàmà nke ọrịa na-atụ aro ọnụnọ nke nnukwu myopathy, ma ọ bụ na ọnụnọ nke na-ebute mmepe nke nnukwu akwara ọdịda n'ihi rhabdomyolysis (ọrịa siri ike, mbelata ọbara mgbali, nnukwu ịwa ahụ, trauma, metabolic, endocrine ma ọ bụ ọgba aghara electrolyte) . E kwesịrị ịdọ ndị ọrịa ọdụ na ha kwesịrị ịgakwuru dọkịta ozugbo ma ọ bụrụ na mgbu na-enweghị nkọwa ma ọ bụ adịghị ike nwere ahụ, ọ bụrụ na ọnya ma ọ bụ ahụ ọkụ na-eso ya.