Lurasidone

Các tên gọi khác (2) :

Lurasidona
Lurasidonum

Thuốc Gốc

Small Molecule

CAS: 367514-87-2

ATC: N05AE05

CTHH: C₂₈H₃₆N₄O₂S

PTK: 492.676

Lurasidone is an atypical antipsychotic developed by Dainippon Sumitomo Pharma. It was approved by the U.S. Food and Drug Administration (FDA) for treatment of schizophrenia on October 29, 2010 and is currently pending approval for the treatment of bipolar disorder in the United States. (Wikipedia)

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₂₈H₃₆N₄O₂S

Phân tử khối

492.676

Monoisotopic mass

492.255897106

InChI

InChI=1S/C28H36N4O2S/c33-27-24-18-9-10-19(15-18)25(24)28(34)32(27)17-21-6-2-1-5-20(21)16-30-11-13-31(14-12-30)26-22-7-3-4-8-23(22)35-29-26/h3-4,7-8,18-21,24-25H,1-2,5-6,9-17H2/t18-,19+,20-,21-,24+,25-/m0/s1

InChI Key

InChIKey=PQXKDMSYBGKCJA-CVTJIBDQSA-N

IUPAC Name

(1R,2S,6R,7S)-4-{[(1R,2R)-2-{[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]methyl}cyclohexyl]methyl}-4-azatricyclo[5.2.1.0²,⁶]decane-3,5-dione

Traditional IUPAC Name

lurasidone

SMILES

O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1C[C@@H]1CCCC[C@H]1CN1CCN(CC1)C1=NSC2=CC=CC=C12

Độ hòa tan

7.89e-03 g/l

logP

4.56

logS

-4.8

pKa (Strongest Basic)

8.5

PSA

56.75 Å²

Refractivity

139.33 m³·mol^-1

Polarizability

56.2 Å³

Rotatable Bond Count

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

Rule of Five

true

Dược Lực Học : Lurasidone is a benzothiazol derivative that is an antagonist and binds with high affinity to Dopamine-2 (D2) (Ki = 0.994 nM), 5-HT2A (Ki = 0.47 nM) receptors, and 5-HT7 receptors (Ki = 0.495 nM). It also binds with moderate affinity to alpha-2C adrenergic receptors (Ki = 10.8 nM) and is a partial agonist at 5-HT1A receptors (Ki = 6.38 nM). Its actions on histaminergic and muscarinic receptors are negligible.

Cơ Chế Tác Dụng : Lurasidone is an atypical antipsychotic developed by Dainippon Sumitomo Pharma. It was approved by the U.S. Food and Drug Administration (FDA) for treatment of schizophrenia on October 29, 2010 and is currently pending approval for the treatment of bipolar disorder in the United States. (Wikipedia) Lurasidone is an atypical antipsychotic that is a D2 and 5-HT2A (mixed serotonin and dopamine activity) to improve cognition. It is thought that antagonism of serotonin receptors can improve negative symptoms of psychoses and reduce the extrapyramidal side effects that are often associated with typical antipsychotics.

Dược Động Học :

▧ Absorption :
Lurasidone is readily absorbed and quickly reaches maximal concentrations (Cmax) within 1-4 hours. When taken with food, there is a two-fold increase in exposure and time to maximal concentration is increased by 0.5-1.5 hours. This occurs regardless of fat or caloric content. Bioavailability = 9-19%.
▧ Volume of Distribution :
6173 L
▧ Protein binding :
~99% bound to serum proteins.
▧ Metabolism :
Lurasidone is metabolized by CYP3A4 in which its major active metabolite is referred to as ID-14283 (25% of parent exposure). Its two minor metabolites are referred to as ID14326 and ID11614 which make up 3% and 1% of parent exposure respectively. Its two non-active metabolites are referred to as ID-20219 and ID-20220.
▧ Route of Elimination :
Urine (~9%) and feces (~80%)
▧ Half Life :
40 mg dose= 18 hours 120 mg - 160 mg dose = 29-37 hours
▧ Clearance :
3902 mL/min

Chỉ Định : Treatment of schizophrenia.

Tương Tác Thuốc :

Atazanavir Concomitant therapy with a strong CYP3A4 inhibitor will increase level or effect of lurasidone. Coadministration with lurasidone is contraindicated.
Bicalutamide CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of lurasidone. Limit adult lurasidone dose to 40 mg/day in patients receiving a moderate CYP3A4 inhibitor.
Bosentan Concomitant therapy with a CYP3A4 substrate and inducer will decrease levels of lurasidone. Coadministration with lurasidone is contraindicated.
Carbamazepine Concomitant therapy with a CYP3A4 inducer will decrease levels of lurasidone. Coadministration with lurasidone is contraindicated.
Chloramphenicol Concomitant therapy with a strong CYP3A4 inhibitor will increase level or effect of lurasidone. Coadministration with lurasidone is contraindicated.
Clarithromycin Concomitant therapy with a strong CYP3A4 inhibitor will increase level or effect of lurasidone. Coadministration with lurasidone is contraindicated.
Clotrimazole CYP3A4 Inhibitors (Moderate) such as clotrimazole may increase the serum concentration of lurasidone. Limit adult lurasidone dose to 40 mg/day in patients receiving a moderate CYP3A4 inhibitor.
Conivaptan CYP3A4 Inhibitors (Strong) may increase the serum concentration of Lurasidone. Avoid use of lurasidone in patients receiving strong CYP3A4 inhibitors.
Darunavir Concomitant therapy with a strong CYP3A4 inhibitor will increase level or effect of lurasidone. Coadministration with lurasidone is contraindicated.
Delavirdine Concomitant therapy with a strong CYP3A4 inhibitor will increase level or effect of lurasidone. Coadministration with lurasidone is contraindicated.
Dexamethasone Concomitant therapy with a CYP3A4 inducer will decrease levels of lurasidone. Coadministration with lurasidone is contraindicated. Will decrease Cmax of lurasidone by 85%.
Dopamine Dopamine increases toxicity (enhanced hypotensive effects) of lurasidone.
Epinephrine Epinephrine increases toxicity (enhance hypotensive effects) of lurasidone by pharmacodynamic synergism.
Etravirine Concomitant therapy with a CYP3A4 inducer will decrease levels of lurasidone. Coadministration with lurasidone is contraindicated.
Etravirine Lurasidone, when used concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to avoid concurrent therapy.
Fosamprenavir Concomitant therapy with a strong CYP3A4 inhibitor will increase level or effect of lurasidone. Coadministration with lurasidone is contraindicated.
Fosphenytoin Concomitant therapy with a CYP3A4 inducer will decrease levels of lurasidone. Coadministration with lurasidone is contraindicated.
Imatinib Concomitant therapy with a strong CYP3A4 inhibitor will increase level or effect of lurasidone. Coadministration with lurasidone is contraindicated.
Indinavir Concomitant therapy with a strong CYP3A4 inhibitor will increase level or effect of lurasidone. Coadministration with lurasidone is contraindicated.
Itraconazole Concomitant therapy with a strong CYP3A4 inhibitor will increase level or effect of lurasidone. Coadministration with lurasidone is contraindicated.
Ketoconazole Concomitant therapy with a strong CYP3A4 inhibitor will increase level or effect of lurasidone. Coadministration with lurasidone is contraindicated.
Metoclopramide Increases toxicity and risk of extrapyramidal effects of lurasidone by antidopaminergic effects. Concomitant therapy should be avoided.
Nafcillin Concomitant therapy will decrease levels of lurasidone via effects on CYP 3A4. Concomitant therapy is contraindicated.

Liều Lượng & Cách Dùng : Tablet - Oral - 20 mg, 40 mg, 80 mg, 120 mg

Dữ Kiện Thương Mại

Nhà Sản Xuất

Công ty : Sunovion Pharmaceuticals Inc.

Sản phẩm biệt dược : Latuda

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB08815

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D04820

National Drug Code Directory

http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/63402-312-30

Wikipedia

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

RxList

http://www.rxlist.com/latuda-drug.htm

Drugs.com

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

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