Tìm theo
Phendimetrazine
Các tên gọi khác (1) :
  • Phendimetrazine
central nervous system stimulants, appetite depressants
Thuốc Gốc
Small Molecule
CAS: 634-03-7
ĐG : Apotheca Inc.
CTHH: C12H17NO
PTK: 191.2695
Phendimetrazine is a weight loss medication. Phendimetrazine is chemically related to amphetamines and is a Schedule III drug under the Convention on Psychotropic Substances. In the United States, phendimetrazine is a Schedule III controlled substance under the Uniform Controlled Substances Act of 1970.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
191.2695
Monoisotopic mass
191.131014171
InChI
InChI=1S/C12H17NO/c1-10-12(14-9-8-13(10)2)11-6-4-3-5-7-11/h3-7,10,12H,8-9H2,1-2H3
InChI Key
InChIKey=MFOCDFTXLCYLKU-UHFFFAOYSA-N
IUPAC Name
3,4-dimethyl-2-phenylmorpholine
Traditional IUPAC Name
phendimetrazine
SMILES
CC1C(OCCN1C)C1=CC=CC=C1
Độ sôi
134.5 °C at 1.20E+01 mm Hg
Độ hòa tan
2.43e+00 g/l
logP
2.17
logS
-1.9
pKa (Strongest Basic)
7.28
PSA
12.47 Å2
Refractivity
57.76 m3·mol-1
Polarizability
21.99 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Phendimetrazine is a phenylalkylamine sympathomimetic amine with pharmacological 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 has been demonstrated with all drugs of this class in which these phenomena have been looked for. Drugs of this class used in obesity are commonly known as ''anorectics or anorexigenics." It has not been established, however, that the action of such drugs in treating obesity is primarily one of appetite suppression. Other central nervous system actions or metabolic effects, may be involved.
Cơ Chế Tác Dụng : Phendimetrazine is a weight loss medication. Phendimetrazine is chemically related to amphetamines and is a Schedule III drug under the Convention on Psychotropic Substances. In the United States, phendimetrazine is a Schedule III controlled substance under the Uniform Controlled Substances Act of 1970. Phendimetrazine may act in a similar way to amphetamines in that it activates the alpha-adrenergic system to induce an appetite suppressive and metabolic increase effect. The drug also acts as a norepinephrine-dopamine releasing agent (NDRA). It can bind to and reverse the NET.
Dược Động Học :
▧ Absorption :
Peak plasma levels occur within 1 to 3 hours. Absorption is usually complete by 4 to 6 hours.
▧ Metabolism :
Approximately 30% of a given dose of phendimetrazine is metabolized into phenmetrazine, which may account for part of its anorectic effect, and probably also influences abuse potential; individuals who metabolise a greater proportion of phendimetrazine into phenmetrazine are more likely to develop problems with dependence and addiction
▧ Route of Elimination :
The major route of elimination is via the kidneys where most of the drug and metabolites are excreted.
▧ Half Life :
19-24 hours
Độc Tính : Acute overdosage of phendimetrazine may manifest itself by the following signs and symptoms: unusual restlessness, confusion, belligerance, hallucinations, and panic states. Fatigue and depression usually follow the central stimulation. Cardiovascular effects include arrhythmias, hypertension, or hypotension and circulatory collapse. Gastrointestinal symptoms include nausea, vomiting, diarrhea, and abdominal cramps. Poisoning may result in convulsions, coma and death.
Chỉ Định : Used in 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 Decreased anorexic effect, may increases psychotic symptoms
  • Fluoxetine Risk of serotoninergic syndrome
  • Fluphenazine Decreased anorexic effect, may increase psychotic symptoms
  • Fluvoxamine Risk of serotoninergic syndrome
  • Guanethidine Phendimetrazine may decrease the effect of guanethidine.
  • Isocarboxazid Possible hypertensive crisis
  • Mesoridazine 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 pyschotic symptoms
  • Promethazine Decreased anorexic effect, may increase pyschotic symptoms
  • Propericiazine Decreased anorexic effect, may increase pyschotic symptoms
  • Rasagiline Possible hypertensive crisis
  • Thioridazine Decreased anorexic effect, may increase psychotic symptoms
  • Tramadol Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Trandolapril Phendimetrazine may reduce the efficacy of Trandolapril.
  • Tranylcypromine The MAO inhibitor, Tranylcypromine, may increase the vasopressor effect of the amphetamine, Phendimetrazine. Concomitant therapy should be avoided.
  • Trifluoperazine Decreased anorexic effect, may increase psychotic symptoms
  • Triprolidine Triprolidine may reduce the sedative effect of the antihistamine, Phendimetrazine.
Liều Lượng & Cách Dùng : Tablet - Oral
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