Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
149.120449485
InChI
InChI=1S/C10H15N/c1-9(11-2)8-10-6-4-3-5-7-10/h3-7,9,11H,8H2,1-2H3/t9-/m0/s1
InChI Key
InChIKey=MYWUZJCMWCOHBA-VIFPVBQESA-N
IUPAC Name
methyl[(2S)-1-phenylpropan-2-yl]amine
Traditional IUPAC Name
methamphetamine
SMILES
CN[C@@H](C)CC1=CC=CC=C1
pKa (Strongest Basic)
10.21
Refractivity
48.48 m3·mol-1
Dược Lực Học :
Methamphetamine is a potent central nervous system stimulant which affects neurochemical mechanisms responsible for regulating heart rate, body temperature, blood pressure, appetite, attention, mood and responses associated with alertness or alarm conditions. The acute effects of the drug closely resemble the physiological and psychological effects of an epinephrine-provoked fight-or-flight response, including increased heart rate and blood pressure, vasoconstriction (constriction of the arterial walls), bronchodilation, and hyperglycemia (increased blood sugar). Users experience an increase in focus, increased mental alertness, and the elimination of fatigue, as well as a decrease in appetite.
Cơ Chế Tác Dụng :
Methamphetamine is a psychostimulant and sympathomimetic drug. It is a member of the amphetamine group of sympathomimetic amines. Methamphetamine can induce effects such as euphoria, increased alertness and energy, and enhanced self-esteem. It is a scheduled drug in most countries due to its high potential for addiction and abuse.
Methamphetamine enters the brain and triggers a cascading release of norepinephrine, dopamine and serotonin. To a lesser extent methamphetamine acts as a dopaminergic and adrenergic reuptake inhibitor and in high concentrations as a monamine oxidase inhibitor (MAOI). The mechanism of action involved in producing the beneficial behavioral changes seen in hyperkinetic children receiving methamphetamine is unknown.
Dược Động Học :
▧ Absorption :
Methamphetamine is rapidly absorbed from the gastrointestinal tract with peak methamphetamine concentrations occurring in 3.13 to 6.3 hours post ingestion. Methamphetamine is also well absorbed following inhalation and following intranasal administration. It is distributed to most parts of the body. Because methamphetamine has a high lipophilicity it is distributed across the blood brain barrier and crosses the placenta.
▧ Metabolism :
Hepatic. The primary site of metabolism is in the liver by aromatic hydroxylation, N-dealkylation and deamination. At least seven metabolites have been identified in the urine, with the main metabolites being amphetamine (active) and 4-hydroxymethamphetamine. Other minor metabolites include 4-hydroxyamphetamine, norephedrine, and 4-hydroxynorephedrine.
▧ Route of Elimination :
Excretion occurs primarily in the urine, the rate of which is dependent on urine pH. Between 30-54% of an oral dose is excreted in urine as unchanged methamphetamine and 10-23% as unchanged amphetamine. Following an intravenous dose, 45% is excreted as unchanged parent drug and 7% amphetamine.
▧ Half Life :
The biological half-life has been reported in the range of 4 to 5 hours.
Độc Tính :
Manifestations of acute overdosage with methamphetamine include restlessness, tremor, hyperreflexia, rapid respiration, confusion, assaultiveness, hallucinations, panic states, hyperpyrexia, and rhabdomyolysis. 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. Fatal poisoning usually terminates in convulsions and coma.
Chỉ Định :
For the treatment of Attention Deficit Disorder with Hyperactivity (ADHD) and exogenous obesity.
Tương Tác Thuốc :
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Chlorpromazine
Decreased anorexic effect, may increases psychotic symptoms
-
Fluoxetine
Risk of serotoninergic syndrome
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Fluphenazine
Decreased anorexic effect, may increase psychotic symptoms
-
Fluvoxamine
Risk of serotoninergic syndrome
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Guanethidine
Methamphetamine may decrease the effect of guanethidine.
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Isocarboxazid
Possible hypertensive crisis
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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
-
Terbinafine
Terbinafine may reduce the metabolism and clearance of Methamphetamine. Consider alternate therapy or monitor for therapeutic/adverse effects of Methamphetamine if Terbinafine is initiated, discontinued or dose changed.
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Thioridazine
Decreased anorexic effect, may increase psychotic symptoms
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Tramadol
Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
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Trandolapril
Methamphetamine may reduce the efficacy of Trandolapril.
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Tranylcypromine
The MAO inhibitor, Tranylcypromine, may increase the vasopressor effect of the amphetamine, Methamphetamine. Concomitant therapy should be avoided.
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Trifluoperazine
Decreased anorexic effect, may increase psychotic symptoms
-
Triprolidine
Triprolidine may reduce the sedative effect of the antihistamine, Methamphetamine.
Liều Lượng & Cách Dùng :
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
-
Giá bán buôn : USD >3.6
Đơn vị tính : tablet
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Giá bán buôn : USD >5.1
Đơn vị tính : tablet
Tài Liệu Tham Khảo Thêm
National Drug Code Directory