Isotretinoin

Các tên gọi khác (13 ) :

(7e,9e,11e,13Z)-Retinoic acid
13-cis-Retinoic acid
13-cis-Vitamin a acid
13-RA
Accutane
Amnesteem
cis-RA
Claravis
Isotretinoina
Isotretinoine
Isotretinoino
Isotretinoinum
Neovitamin a acid

Thuốc điều trị bệnh da liễu

Thuốc Gốc

Small Molecule

CAS: 4759-48-2

ĐG : Barr Pharmaceuticals

CTHH: C₂₀H₂₈O₂

PTK: 300.4351

Isotretinoin is a medication used for the treatment of severe acne. It is sometimes used in prevention of certain skin cancers. It is a retinoid, meaning it derives from vitamin A and is found in small quantities naturally in the body. Isotretinoin binds to and activates nuclear retinoic acid receptors (RAR), thereby regulating cell proliferation and differentiation. This agent also exhibits immunomodulatory and anti-inflammatory responses and inhibits ornithine decarboxylase, thereby decreasing polyamine synthesis and keratinization.

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₂₀H₂₈O₂

Phân tử khối

300.4351

Monoisotopic mass

300.20893014

InChI

InChI=1S/C20H28O2/c1-15(8-6-9-16(2)14-19(21)22)11-12-18-17(3)10-7-13-20(18,4)5/h6,8-9,11-12,14H,7,10,13H2,1-5H3,(H,21,22)/b9-6+,12-11+,15-8+,16-14-

InChI Key

InChIKey=SHGAZHPCJJPHSC-XFYACQKRSA-N

IUPAC Name

(2Z,4E,6E,8E)-3,7-dimethyl-9-(2,6,6-trimethylcyclohex-1-en-1-yl)nona-2,4,6,8-tetraenoic acid

Traditional IUPAC Name

accutane

SMILES

C\C(\C=C\C1=C(C)CCCC1(C)C)=C/C=C/C(/C)=C\C(O)=O

Độ hòa tan

4.77e-03 g/l

logP

4.2

logS

-4.8

pKa (strongest acidic)

PSA

37.3 Å²

Refractivity

97.79 m³·mol^-1

Polarizability

36.15 Å³

Rotatable Bond Count

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

-1

Number of Rings

Bioavailability

Ghose Filter

true

Dược Lực Học : Isotretinoin, a retinoid, is indicated in the treatment of severe recalcitrant nodular acne. Nodules are inflammatory lesions with a diameter of 5 mm or greater. The nodules may become suppurative or hemorrhagic. "Severe," by definition, means "many" as opposed to "few or several" nodules. Clinical improvement in nodular acne patients occurs in association with a reduction in sebum secretion. The decrease in sebum secretion is temporary and is related to the dose and duration of treatment with Accutane, and reflects a reduction in sebaceous gland size and an inhibition of sebaceous gland differentiation.

Cơ Chế Tác Dụng : Isotretinoin is a medication used for the treatment of severe acne. It is sometimes used in prevention of certain skin cancers. It is a retinoid, meaning it derives from vitamin A and is found in small quantities naturally in the body. Isotretinoin binds to and activates nuclear retinoic acid receptors (RAR), thereby regulating cell proliferation and differentiation. This agent also exhibits immunomodulatory and anti-inflammatory responses and inhibits ornithine decarboxylase, thereby decreasing polyamine synthesis and keratinization. Isotretinoin noticeably reduces the production of sebum and shrinks the sebaceous glands. It stabilises keratinization and prevents comedones from forming. It also reduces inflammation in moderate-severe inflammatory acne. The exact mechanism of action is unknown, however it is known that it alters DNA transcription.

Dược Động Học :

▧ Protein binding :
99.9%
▧ Route of Elimination :
Isotretinoin and its metabolites are further metabolized into conjugates, which are then excreted in urine and feces. The metabolites of isotretinoin and any conjugates are ultimately excreted in the feces and urine in relatively equal amounts (total of 65% to 83%).
▧ Half Life :
17-50 hours
▧ Clearance :
* 96 +/- 6.27 L/hr [severe recalcitrant nodular acne pediatric Patients, 12 to 15 Years]

Độc Tính : Isotretinoin is teratogenic. It also causes mucocutaneous side effects suck as cheilitis, dry skin, and dry eyes.

Chỉ Định : For the treatment of severe recalcitrant nodular acne

Tương Tác Thuốc :

Carbamazepine Isotretinoine decreases the effect of carbamazepine
Demeclocycline Increased risk of intracranial hypertension
Doxycycline Increased risk of intracranial hypertension
Methacycline Increased risk of intracranial hypertension
Minocycline Increased risk of intracranial hypertension
Oxytetracycline Increased risk of intracranial hypertension
Rolitetracycline Increased risk of intracranial hypertension
Tetracycline Increased risk of intracranial hypertension
Vitamin A Isotretinoin increases the risk of vitamin A toxicity. Avoid vitamin A supplementation while taking isotretinoin.

Liều Lượng & Cách Dùng : Capsule - Oral

Dữ Kiện Thương Mại

Giá thị trường

Biệt dược thương mại : Clarus 10 mg Capsule

Giá bán buôn : USD >1.05

Đơn vị tính : capsule
Biệt dược thương mại : Clarus 40 mg Capsule

Giá bán buôn : USD >2.14

Đơn vị tính : capsule
Biệt dược thương mại : Sotret 10 mg capsule

Giá bán buôn : USD >7.31

Đơn vị tính : capsule
Biệt dược thương mại : Sotret 30 mg capsule

Giá bán buôn : USD >8.44

Đơn vị tính : capsule
Biệt dược thương mại : Sotret 20 mg capsule

Giá bán buôn : USD >8.67

Đơn vị tính : capsule
Biệt dược thương mại : Sotret 40 mg capsule

Giá bán buôn : USD >10.08

Đơn vị tính : capsule
Biệt dược thương mại : Accutane 10 mg capsule

Giá bán buôn : USD >10.55

Đơn vị tính : capsule
Biệt dược thương mại : Accutane 40 mg capsule

Giá bán buôn : USD >14.88

Đơn vị tính : capsule
Biệt dược thương mại : Claravis 10 mg capsule

Giá bán buôn : USD >15.77

Đơn vị tính : capsule
Biệt dược thương mại : Amnesteem 10 mg capsule

Giá bán buôn : USD >16.4

Đơn vị tính : capsule
Biệt dược thương mại : Claravis 30 mg capsule

Giá bán buôn : USD >16.45

Đơn vị tính : capsule
Biệt dược thương mại : Claravis 20 mg capsule

Giá bán buôn : USD >18.7

Đơn vị tính : capsule
Biệt dược thương mại : Amnesteem 20 mg capsule

Giá bán buôn : USD >19.45

Đơn vị tính : capsule
Biệt dược thương mại : Amnesteem 40 mg capsule

Giá bán buôn : USD >22.6

Đơn vị tính : capsule
Biệt dược thương mại : Claravis 40 mg capsule

Giá bán buôn : USD >22.6

Đơn vị tính : capsule
Biệt dược thương mại : Accutane 20 mg capsule

Giá bán buôn : USD >23.77

Đơn vị tính : capsule

Nhà Sản Xuất

Công ty :

Sản phẩm biệt dược : Absorica
Công ty :

Sản phẩm biệt dược : Accutane Roche
Công ty :

Sản phẩm biệt dược : Myorisan
Công ty :

Sản phẩm biệt dược : ZENATANE

Đóng gói

Công ty : Barr Pharmaceuticals
Công ty : Catalent Pharma Solutions

Website : http://www.catalent.com
Công ty : F Hoffmann-La Roche Ltd.

Website : http://www.roche.com
Công ty : Mylan

Website : http://www.mylan.com
Công ty : Pharmaceutical Utilization Management Program VA Inc.
Công ty : Physicians Total Care Inc.

Website : http://www.physicianstotalcare.com
Công ty : Ranbaxy Laboratories

Website : http://www.ranbaxy.com

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB00982

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D00348

National Drug Code Directory

http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0004-0155-49

PharmGKB

http://www.pharmgkb.org/drug/PA450128

Wikipedia

http://en.wikipedia.org/wiki/Isotretinoin

RxList

http://www.rxlist.com/cgi/generic/isotret.htm

Drugs.com

http://www.drugs.com/cdi/isotretinoin.html

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