2018年3月現在、アトルバスタチンは約140の国及び地域で発売しており、その主な状況を表に示す。
なお、米国ワーナー・ランバート社(現 米国ファイザー社)は1996年6月にFDAにNDAを提出し、本剤 が家族性高コレステロール血症ホモ接合体患者及び難治性の高コレステロール血症患者に対する有効性 を示したことから、優先審査が認められ、半年後の1996年12月に承認された。
本邦における効能・効果、及び用法・用量は以下のとおりであり、外国での承認状況とは異なる。
【効能・効果】
高コレステロール血症 家族性高コレステロール血症
【用法・用量】
・高コレステロール血症
通常、成人にはアトルバスタチンとして10mgを1日1回経口投与する。
なお、年齢、症状により適宜増減するが、重症の場合は1日20mgまで増量できる。
・家族性高コレステロール血症
通常、成人にはアトルバスタチンとして10mgを1日1回経口投与する。
なお、年齢、症状により適宜増減するが、重症の場合は1日40mgまで増量できる。
主な国及び地域における発売状況(2018年3月現在) 国名及び地域名
アイスランド アイルランド アルゼンチン イタリア インドネシア 英国
エクアドル エジプト エルサルバドル オーストラリア オーストリア オランダ カナダ 韓国 キプロス ギリシャ グアテマラ クウェート コスタリカ
コロンビア サウジアラビア シンガポール スイス スウェーデン スペイン タイ 台湾 中国 チリ デンマーク ドイツ
ドミニカ共和国 トルコ
ニカラグア ニュージーランド ノルウェー パナマ フィリピン
フィンランド ブラジル フランス 米国 ベトナム ペルー ベルギー ポルトガル 香港
ホンジュラス マレーシア 南アフリカ メキシコ モロッコ UAE ヨルダン ルクセンブルグ レバノン
ⅩⅡ．参考資料
米国における承認状況 会社名 Pfizer Inc.
販売名 LIPITOR®
剤形・規格 10, 20, 40, and 80mg tablets 承認年月 1996年12月
効能・効果 LIPITOR is an HMG-CoA reductase inhibitor indicated as an adjunct therapy to diet to:
・Reduce the risk of MI, stroke, revascularization procedures, and angina in adult patients without CHD, but with multiple risk factors.
・Reduce the risk of MI and stroke in adult patients with type 2 diabetes without CHD, but with multiple risk factors.
・Reduce the risk of non-fatal MI, fatal and non-fatal stroke, revascularization procedures, hospitalization for CHF, and angina in adult patients with CHD.
・Reduce elevated total-C, LDL-C, apo B, and TG levels and increase HDL-C in adult patients with primary hyperlipidemia (heterozygous familial and nonfamilial) and mixed dyslipidemia.
・Reduce elevated TG in adult patients with hypertriglyceridemia and primary dysbetalipoproteinemia.
・Reduce total-C and LDL-C in patients with homozygous familial hypercholesterolemia (HoFH).
・Reduce elevated total-C, LDL-C, and apo B levels in pediatric patients, 10 years to 17 years of age, with heterozygous familial hypercholesterolemia (HeFH) after failing an adequate trial of diet therapy.
Limitations of Use:
LIPITOR has not been studied in Fredrickson Types I and V dyslipidemias.
用法・用量 ・Dose range: 10 to 80 mg once daily.
・Recommended start dose: 10 or 20 mg once daily.
・Patients requiring large LDL-C reduction (＞45％) may start at 40 mg once daily.
・Pediatric patients with HeFH: starting dose: 10 mg once daily; dose range: 10 to 20 mg/day for patients 10 years to 17 years of age.
(2018年8月) 英国における承認状況
会社名 Pfizer Limited
販売名 Lipitor™
剤形・規格 Film-coated tablets：10, 20, 40 and 80mg 承認年月 1996年11月
効能・効果 Hypercholesterolaemia
Lipitor is indicated as an adjunct to diet for reduction of elevated total cholesterol (total-C), LDL-cholesterol (LDL-C), apolipoprotein B, and triglycerides in adults, adolescents and children aged 10 years or older with primary hypercholesterolaemia including familial hypercholesterolaemia (heterozygous variant) or combined (mixed) hyperlipidaemia (Corresponding to Types IIa and IIb of the Fredrickson classification) when response to diet and other nonpharmacological measures is inadequate.
Liptor is also indicated to reduce total-C and LDL-C in adults with homozygous familial hypercholesterolaemia as an adjunct to other lipid-lowering treatments (e.g. LDL apheresis) or if such treatments are unavailable.
ⅩⅡ．参考資料
用法・用量 Posology
The patient should be placed on a standard cholesterol-lowering diet before receiving Lipitor and should continue on this diet during treatment with Lipitor.
The dose should be individualised according to baseline LDL-C levels, the goal of therapy, and patient response.
The usual starting dose is 10 mg once a day. Adjustment of dose should be made at intervals of 4 weeks or more. The maximum dose is 80 mg once a day.
Primary hypercholesterolaemia and combined (mixed) hyperlipidaemia
The majority of patients are controlled with Lipitor 10 mg once a day. A therapeutic response is evident within 2 weeks, and the maximum therapeutic response is usually achieved within 4 weeks. The response is maintained during chronic therapy.
Heterozygous familial hypercholesterolaemia
Patients should be started with Lipitor 10 mg daily. Doses should be individualised and adjusted every 4 weeks to 40 mg daily. Thereafter, either the dose may be increased to a maximum of 80 mg daily or a bile acid sequestrant may be combined with 40 mg atorvastatin once daily.
Homozygous familial hypercholesterolaemia Only limited data are available.
The dose of atorvastatin in patients with homozygous familial hypercholesterolemia is 10 to 80 mg daily.
Atorvastatin should be used as an adjunct to other lipid-lowering treatments (e.g. LDL apheresis) in these patients or if such treatments are unavailable.
Prevention of cardiovascular disease
In the primary prevention trials the dose was 10 mg/day. Higher doses may be necessary in order to attain (LDL-) cholesterol levels according to current guidelines.
Renal impairment
No adjustment of dose is required.
Hepatic impairment
Lipitor should be used with caution in patients with hepatic impairment. Lipitor is contraindicated in patients with active liver disease.
Elderly
Efficacy and safety in patients older than 70 using recommended doses are similar to those seen in the general population.
Paediatric population Hypercholesterolaemia
Paediatric use should only be carried out by physicians experienced in the treatment of paediatric hyperlipidaemia and patients should be re-evaluated on a regular basis to assess progress.
For patients with Heterozygous Familial Hypercholesterolemia aged 10 years and above, the recommended starting dose of atorvastatin is 10 mg per day. The dose may be increased to 80 mg daily, according to the response and tolerability. Doses should be individualised according to the recommended goal of therapy. Adjustments should be made at intervals of 4 weeks or more. The dose titration to 80 mg daily is supported by study data in adults and by limited clinical data from studies in children with Heterozygous Familial Hypercholesterolemia.
There are limited safety and efficacy data available in children with Heterozygous Familial Hypercholesterolemia between 6 to 10 years of age derived from open-label studies. Atorvastatin is not indicated in the treatment of patients below the age of 10 years.
Other pharmaceutical forms/strengths may be more appropriate for this population.
Method of administration
Lipitor is for oral administration. Each daily dose of atorvastatin is given all at once and may be given at any time of day with or without food.
Lipitor 10 mg film-coated tablets (2018年5月)
https://www.medicines.org.uk/emc/medicine/1424 (2018/09/19 アクセス)
ⅩⅡ．参考資料