Tìm theo
Benzphetamine
Các tên gọi khác (19 ) :
  • (+)-benzphetamine
  • (+)-N-Benzyl-N,alpha-dimethylphenethylamine
  • (+)-N-benzyl-N,α-dimethylphenethylamine
  • (+)-N,alpha-Dimethyl-N-(phenylmethyl)-benzeneethanamine
  • (+)-N,α-dimethyl-N-(phenylmethyl)-benzeneethanamine
  • (AlphaS)-N,alpha-dimethylphenethylamine
  • (S)-(+)-benzphetamine
  • (S)-(+)-N-Benzyl-N,alpha-dimethylphenethylamine
  • (S)-(+)-N-benzyl-N,α-dimethylphenethylamine
  • (S)-benzphetamine
  • Benzaphetamine
  • Benzfetamina
  • Benzfetamine
  • Benzfetaminum
  • Benzphetamine
  • Benzylamphetamine
  • D-N-Methyl-N-benzyl-beta-phenylisopropylamine
  • d-N-methyl-N-benzyl-β-phenylisopropylamine
  • N-methyl-1-phenyl-N-(phenylmethyl)propan-2-amine
adrenergic agents, adrenergic uptake inhibitors, central nervous system stimulants, dopamine agents, dop
Thuốc Gốc
Small Molecule
CAS: 156-08-1
ĐG : Aidarex Pharmacuticals LLC , http://www.aidarex.com
CTHH: C17H21N
PTK: 239.3553
A sympathomimetic agent with properties similar to dextroamphetamine. It is used in the treatment of obesity. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1222)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H21N
Phân tử khối
239.3553
Monoisotopic mass
239.167399677
InChI
InChI=1S/C17H21N/c1-15(13-16-9-5-3-6-10-16)18(2)14-17-11-7-4-8-12-17/h3-12,15H,13-14H2,1-2H3/t15-/m0/s1
InChI Key
InChIKey=YXKTVDFXDRQTKV-HNNXBMFYSA-N
IUPAC Name
benzyl(methyl)[(2S)-1-phenylpropan-2-yl]amine
Traditional IUPAC Name
benzphetamine
SMILES
C[C@@H](CC1=CC=CC=C1)N(C)CC1=CC=CC=C1
Độ tan chảy
129-130
Độ hòa tan
Readily soluble
logP
4.1
logS
-4
pKa (Strongest Basic)
9.8
PSA
3.24 Å2
Refractivity
78.39 m3·mol-1
Polarizability
29.03 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
1
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Benzphetamine, a phenylalkylamin, is related to amphetamine both chemically and pharmacologically. It is an anorectic agent indicated in the management of exogenous obesity as a short term adjunct (a few weeks) in a regimen of weight reduction based on caloric restriction. Benzphetamine is a sympathomimetic amine with pharmacologic activity similar to the prototype drugs of this class used in obesity, the amphetamines. Actions include central nervous system stimulation and elevation of blood pressure. Tachyphylaxis and tolerance have been demonstrated with all drugs of this class in which these phenomena have been looked for.
Cơ Chế Tác Dụng : A sympathomimetic agent with properties similar to dextroamphetamine. It is used in the treatment of obesity. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1222) Although the mechanism of action of the sympathomimetic appetite suppressants in the treatment of obesity is not fully known, these medications have pharmacological effects similar to those of amphetamines. Amphetamine and related sympathomimetic medications (such as benzphetamine) are thought to stimulate the release of norepinephrine and/or dopamine from storage sites in nerve terminals in the lateral hypothalamic feeding center, thereby producing a decrease in appetite. This release is mediated by the binding of benzphetamine to centrally located adrenergic receptors.
Dược Động Học :
▧ Absorption :
Readily absorbed from the gastro-intestinal tract and buccal mucosa. It Is resistant to metabolism by monoamine oxidase.
▧ Protein binding :
75-99%
▧ Metabolism :
Hepatic. Benzphetamine's metabolites include amphetamine and methamphetamine.
▧ Half Life :
16 to 31 hours
Độc Tính : LD50=160 mg/kg (orally in rats). Acute overdosage may result in restlessness, tremor, tachypnea, confusion, assaultiveness, and panic states.
Chỉ Định : For the management of exogenous obesity as a short term adjunct (a few weeks) in a regimen of weight reduction based on caloric restriction
Tương Tác Thuốc :
  • Chlorpromazine Antipsychotics may diminish the stimulatory effect of Amphetamines. Monitor effectiveness of amphetamine therapy when altering concurrent antipsychotic therapy as antipsychotic agents may impair the stimulatory effect of amphetamines.
  • Fluoxetine Amphetamines may enhance the adverse/toxic effect of Serotonin Modulators. The risk of serotonin syndrome may be increased. Monitor patients closely for signs and symptoms of serotonin syndrome (e.g., agitation, tremor, tachycardia, etc.) when using amphetamines and serotonin modulators in combination.
  • Fluphenazine Antipsychotics may diminish the stimulatory effect of Amphetamines. Monitor effectiveness of amphetamine therapy when altering concurrent antipsychotic therapy as antipsychotic agents may impair the stimulatory effect of amphetamines.
  • Fluvoxamine Amphetamines may enhance the adverse/toxic effect of Serotonin Modulators. The risk of serotonin syndrome may be increased. Monitor patients closely for signs and symptoms of serotonin syndrome (e.g., agitation, tremor, tachycardia, etc.) when using amphetamines and serotonin modulators in combination.
  • Guanethidine Benzphetamine may decrease the effect of guanethidine.
  • Isocarboxazid MAO Inhibitors may enhance the hypertensive effect of Amphetamines. Concomitant use of amphetamines and monoamine oxidase inhibitors (MAOI) should be avoided. If used concomitantly, careful monitoring of blood pressure must occur. It may take up to 2 weeks after the discontinuation of an MAOI for the effects to dissipate enough to afford safety to the administration of interacting agents.
  • Mesoridazine Antipsychotics may diminish the stimulatory effect of Amphetamines. Monitor effectiveness of amphetamine therapy when altering concurrent antipsychotic therapy as antipsychotic agents may impair the stimulatory effect of amphetamines.
  • Methotrimeprazine Antipsychotics may diminish the stimulatory effect of Amphetamines. Monitor effectiveness of amphetamine therapy when altering concurrent antipsychotic therapy as antipsychotic agents may impair the stimulatory effect of amphetamines.
  • Paroxetine Amphetamines may enhance the adverse/toxic effect of Serotonin Modulators. The risk of serotonin syndrome may be increased. Monitor patients closely for signs and symptoms of serotonin syndrome (e.g., agitation, tremor, tachycardia, etc.) when using amphetamines and serotonin modulators in combination.
  • Perphenazine Antipsychotics may diminish the stimulatory effect of Amphetamines. Monitor effectiveness of amphetamine therapy when altering concurrent antipsychotic therapy as antipsychotic agents may impair the stimulatory effect of amphetamines.
  • Phenelzine MAO Inhibitors may enhance the hypertensive effect of Amphetamines. Concomitant use of amphetamines and monoamine oxidase inhibitors (MAOI) should be avoided. If used concomitantly, careful monitoring of blood pressure must occur. It may take up to 2 weeks after the discontinuation of an MAOI for the effects to dissipate enough to afford safety to the administration of interacting agents.
  • Prochlorperazine Antipsychotics may diminish the stimulatory effect of Amphetamines. Monitor effectiveness of amphetamine therapy when altering concurrent antipsychotic therapy as antipsychotic agents may impair the stimulatory effect of amphetamines.
  • Promethazine Antipsychotics may diminish the stimulatory effect of Amphetamines. Monitor effectiveness of amphetamine therapy when altering concurrent antipsychotic therapy as antipsychotic agents may impair the stimulatory effect of amphetamines.
  • Propericiazine Antipsychotics may diminish the stimulatory effect of Amphetamines. Monitor effectiveness of amphetamine therapy when altering concurrent antipsychotic therapy as antipsychotic agents may impair the stimulatory effect of amphetamines.
  • Rasagiline MAO Inhibitors may enhance the hypertensive effect of Amphetamines. Concomitant use of amphetamines and monoamine oxidase inhibitors (MAOI) should be avoided. If used concomitantly, careful monitoring of blood pressure must occur. It may take up to 2 weeks after the discontinuation of an MAOI for the effects to dissipate enough to afford safety to the administration of interacting agents.
  • Sodium bicarbonate Alkalinizing agents such as sodium bicarbonate may decrease the excretion of amphetamines like benzphetamine. Increased clinical effects and/or toxicity may occur. Therapy modification should be considered.
  • Telithromycin Telithromycin may reduce clearance of Benzphetamine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Benzphetamine if Telithromycin is initiated, discontinued or dose changed.
  • Thioridazine Antipsychotics may diminish the stimulatory effect of Amphetamines. Monitor effectiveness of amphetamine therapy when altering concurrent antipsychotic therapy as antipsychotic agents may impair the stimulatory effect of amphetamines.
  • Tramadol Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Trandolapril Benzphetamine may reduce the efficacy of Trandolapril.
  • Tranylcypromine The MAO inhibitor, Tranylcypromine, may increase the vasopressor effect of the amphetamine, Benzphetamine. Concomitant therapy should be avoided.
  • Trifluoperazine Antipsychotics may diminish the stimulatory effect of Amphetamines. Monitor effectiveness of amphetamine therapy when altering concurrent antipsychotic therapy as antipsychotic agents may impair the stimulatory effect of amphetamines.
  • Triprolidine Triprolidine may reduce the sedative effect of the antihistamine, Benzphetamine.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of benzphetamine by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of benzphetamine if voriconazole is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Tablet - Oral
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