Mazindol

Các tên gọi khác (4 ) :

Mazindol
Mazindolo
Mazindolum
Sanorex

adrenergic uptake inhibitors, central nervous system stimulants, dopamine uptake inhibitors

Thuốc Gốc

Small Molecule

CAS: 22232-71-9

ATC: A08AA05

CTHH: C₁₆H₁₃ClN₂O

PTK: 284.74

Mazindol is a tricyclic anorexigenic agent unrelated to and less toxic than amphetamine, but with some similar side effects. It inhibits uptake of catecholamines and blocks the binding of cocaine to the dopamine uptake transporter. Mazindol is only approved in the United States for the treatment of Duchenne muscular dystrophy, and is not marketed or available in the United States for use in the treatment of obesity.

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₁₆H₁₃ClN₂O

Phân tử khối

284.74

Monoisotopic mass

284.071640755

InChI

InChI=1S/C16H13ClN2O/c17-12-7-5-11(6-8-12)16(20)14-4-2-1-3-13(14)15-18-9-10-19(15)16/h1-8,20H,9-10H2

InChI Key

InChIKey=ZPXSCAKFGYXMGA-UHFFFAOYSA-N

IUPAC Name

5-(4-chlorophenyl)-2H,3H,5H-imidazo[2,1-a]isoindol-5-ol

Traditional IUPAC Name

mazindol

SMILES

OC1(N2CCN=C2C2=CC=CC=C12)C1=CC=C(Cl)C=C1

Độ tan chảy

198-199

Độ hòa tan

1.39e-01 g/l

logP

3.7

logS

-3.3

pKa (strongest acidic)

11.61

pKa (Strongest Basic)

3.86

PSA

35.83 Å²

Refractivity

79.42 m³·mol^-1

Polarizability

29.42 Å³

Rotatable Bond Count

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

Rule of Five

true

Ghose Filter

true

Dược Lực Học : Mazindol is a sympathomimetic amine, which is similar to an amphetamine. Mazindol stimulates the central nervous system (nerves and brain), which increases your heart rate and blood pressure and decreases your appetite. Sympathomimetic appetite suppressants are used in the short-term treatment of obesity. Their appetite-reducing effect tends to decrease after a few weeks. Because of this, these medicines are useful only during the first few weeks of a weight-loss program.

Cơ Chế Tác Dụng : Mazindol is a tricyclic anorexigenic agent unrelated to and less toxic than amphetamine, but with some similar side effects. It inhibits uptake of catecholamines and blocks the binding of cocaine to the dopamine uptake transporter. Mazindol is only approved in the United States for the treatment of Duchenne muscular dystrophy, and is not marketed or available in the United States for use in the treatment of obesity. Although the mechanism of action of the sympathomimetics in the treatment of obesity is not fully known, these medications have pharmacological effects similar to those of amphetamines. Unlike other sympathomimetic appetite suppressants such as phentermine, mazindol is thought to inhibit the reuptake of norepinephrine rather than to cause its release.

Dược Động Học :

▧ Metabolism :
Hepatic.
▧ Half Life :
10-13 hours

Độc Tính : Symptoms of a mazindol overdose include restlessness, tremor, rapid breathing, confusion, hallucinations, panic, aggressiveness, nausea, vomiting, diarrhea, an irregular heartbeat, and seizures.

Chỉ Định : Used in short-term (a few weeks) treatment of exogenous obesity in conjunction with a regimen of weight reduction based on caloric restriction, exercise, and behavior modification in patients with a body mass index of 30 kg of body weight per height in meters squared (kg/m²) or in patients with a body mass index of 27 kg/m² in the presence of risk factors such as hypertension, diabetes, or hyperlipidemia.

Tương Tác Thuốc :

Acetophenazine Decreased anorexic effect, may increase psychotic symptoms
Alimemazine Decreased anorexic effect, may increase psychotic symptoms
Chlorpromazine Decreased anorexic effect, may increase psychotic symptoms
Ethopropazine Decreased anorexic effect, may increase psychotic symptoms
Fluoxetine Risk of serotoninergic syndrome
Fluphenazine Decreased anorexic effect, may increase psychotic symptoms
Fluvoxamine Risk of serotoninergic syndrome
Guanethidine Mazindol may decrease the effect of guanethidine.
Isocarboxazid Possible hypertensive crisis
Mesoridazine Decreased anorexic effect, may increase psychotic symptoms
Methdilazine Decreased anorexic effect, may increase psychotic symptoms
Methotrimeprazine Decreased anorexic effect, may increase psychotic symptoms
Paroxetine Risk of serotoninergic syndrome
Perphenazine Decreased anorexic effect, may increase psychotic symptoms
Phenelzine Possible hypertensive crisis
Prochlorperazine Decreased anorexic effect, may increase psychotic symptoms.
Promazine Decreased anorexic effect, may increase psychotic symptoms
Promethazine Decreased anorexic effect, may increase psychotic symptoms.
Propericiazine Decreased anorexic effect, may increase psychotic symptoms.
Propiomazine Decreased anorexic effect, may increase psychotic symptoms
Rasagiline Possible hypertensive crisis
Thiethylperazine Decreased anorexic effect, may increase psychotic symptoms
Thioridazine Decreased anorexic effect, may increase psychotic symptoms
Tranylcypromine Possible hypertensive crisis
Trifluoperazine Decreased anorexic effect, may increase psychotic symptoms
Triflupromazine Decreased anorexic effect, may increase psychotic symptoms
Venlafaxine Risk of serotoninergic syndrome

Dữ Kiện Thương Mại

Nhà Sản Xuất

Công ty : Gador

Sản phẩm biệt dược : Dimagrir
Công ty : Cetus

Sản phẩm biệt dược : Fagolip Plus
Công ty : Kwang Dong

Sản phẩm biệt dược : Mazanor
Công ty : Novartis

Sản phẩm biệt dược : Sanorex
Công ty : Novartis

Sản phẩm biệt dược : Teronac

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB00579

PubChem Compound

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4020

PubChem Substance

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46509094

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D00367

ChemSpider

http://www.chemspider.com/Chemical-Structure.3880.html

BindingDB

http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50005536

PharmGKB

http://www.pharmgkb.org/drug/PA450326

Wikipedia

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

Drugs.com

http://www.drugs.com/mtm/mazindol.html

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