Tìm theo
Rasagiline
Các tên gọi khác (4 ) :
  • (1R)-N-Propargylindan-1-amine
  • (R)-Indan-1-yl-prop-2-ynyl-amine
  • (R)-N-2-Propynyl-1-indanamine
  • RAS
neuroprotective agents, monoamine oxidase inhibitors
Thuốc Gốc
Small Molecule
CAS: 136236-51-6
ATC: N04BD02
ĐG : Murfreesboro Pharmaceutical Nursing Supply , http://www.unitdosesupply.com
CTHH: C12H13N
PTK: 171.2383
Rasagiline is an irreversible inhibitor of monoamine oxidase and is used as a monotherapy in early Parkinson's disease or as an adjunct therapy in more advanced cases.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
171.2383
Monoisotopic mass
171.104799421
InChI
InChI=1S/C12H13N/c1-2-9-13-12-8-7-10-5-3-4-6-11(10)12/h1,3-6,12-13H,7-9H2/t12-/m1/s1
InChI Key
InChIKey=RUOKEQAAGRXIBM-GFCCVEGCSA-N
IUPAC Name
(1R)-N-(prop-2-yn-1-yl)-2,3-dihydro-1H-inden-1-amine
Traditional IUPAC Name
rasagiline
SMILES
C#CCN[C@@H]1CCC2=CC=CC=C12
Độ hòa tan
2.49e-02 g/l
logP
2.3
logS
-3.8
pKa (Strongest Basic)
8.69
PSA
12.03 Å2
Refractivity
54.47 m3·mol-1
Polarizability
20.25 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
1
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Rasagiline is a propargylamine and an irreversible inhibitor of monoamine oxidase (MAO). MAO, a flavin-containing enzyme, regulates the metabolic degradation of catecholamines and serotonin in the CNS and peripheral tissues. It is classified into two major molecular species, A and B, and is localized in mitochondrial membranes throughout the body in nerve terminals, brain, liver and intestinal mucosa. MAO-A is found predominantly in the GI tract and liver, and regulates the metabolic degradation of circulating catecholamines and dietary amines. MAO-B is the major form in the human brain and is responsible for the regulation of the metabolic degradation of dopamine and phenylethylamine. In ex vivo animal studies in brain, liver and intestinal tissues rasagiline was shown to be a potent,selective, and irreversible monoamine oxidase type B (MAO-B) inhibitor. At the recommended therapeutic doses, Rasagiline was also shown to be a potent and irreversible inhibitor of MAO-B in platelets. The selectivity of rasagiline for inhibiting only MAO-B (and not MAO-A) in humans and the sensitivity to tyramine during rasagiline treatment at any dose has not been sufficiently characterized to avoid restriction of dietary tyramine and amines contained in medications.
Cơ Chế Tác Dụng : Rasagiline is an irreversible inhibitor of monoamine oxidase and is used as a monotherapy in early Parkinson's disease or as an adjunct therapy in more advanced cases. The precise mechanisms of action of rasagiline is unknown. One mechanism is believed to be related to its MAO-B inhibitory activity, which causes an increase in extracellular levels of dopamine in the striatum. The elevated dopamine level and subsequent increased dopaminergic activity are likely to mediate rasagiline's beneficial effects seen in models of dopaminergic motor dysfunction.
Dược Động Học :
▧ Absorption :
Rasagiline is rapidly absorbed following oral administration. The absolute bioavailability of rasagiline is about 36%.
▧ Volume of Distribution :
* 87 L
▧ Protein binding :
Plasma protein binding ranges from 88-94% with mean extent of binding of 61-63% to human albumin over the concentration range of 1-100 ng/ml.
▧ Metabolism :
Rasagiline undergoes almost complete biotransformation in the liver prior to excretion. In vitro experiments indicate that both routes of rasagiline metabolism are dependent on the cytochrome P450 (CYP) system, with CYP 1A2 being the major isoenzyme involved in rasagiline metabolism.
▧ Route of Elimination :
Rasagiline undergoes almost complete biotransformation in the liver prior to excretion. Glucuronide conjugation of rasagiline and its metabolites, with subsequent urinary excretion, is the major elimination pathway. After oral administration of 14C-labeled rasagiline, elimination occurred primarily via urine and secondarily via feces (62% of total dose in urine and 7% of total dose in feces over 7 days), with a total calculated recovery of 84% of the dose over a period of 38 days. Less than 1% of rasagiline was excreted as unchanged drug in urine.
▧ Half Life :
Rasagiline has a mean steady-state half life of 3 hours but there is no correlation of pharmacokinetics with its pharmacological effect because of its irreversible inhibition of MAO-B.
Độc Tính : Signs and symptoms of overdosage may include, alone or in combination, any of the following: drowsiness, dizziness, faintness, irritability, hyperactivity, agitation, severe headache, hallucinations, trismus, opisthotonos, convulsions, and coma; rapid and irregular pulse, hypertension, hypotension and vascular collapse; precordial pain, respiratory depression and failure, hyperpyrexia, diaphoresis, and cool, clammy skin.
Chỉ Định : For the treatment of the signs and symptoms of idiopathic Parkinsons disease as initial monotherapy and as adjunct therapy to levodopa.
Tương Tác Thuốc :
  • Altretamine Risk of severe hypotension
  • Amitriptyline Possibility of severe adverse effects
  • Amoxapine Possibility of severe adverse effects
  • Amphetamine Possible hypertensive crisis
  • Atomoxetine Possible severe adverse reaction with this combination
  • Benzphetamine 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.
  • Bezafibrate MAO Inhibitors may enhance the adverse/toxic effect of Bezafibrate. Avoid concomitant use of bezafibrate with monoamine oxidase inhibitors (MAOIs) rasagiline.
  • Brimonidine MAO Inhibitors like rasagiline may enhance the hypertensive effect of Alpha2-Agonists (Ophthalmic). The concomitant use of monoamine oxidase inhibitors and ophthalmic alpha2 agonists is contraindicated.
  • Buprenorphine Buprenorphine may enhance the adverse/toxic effect of MAO Inhibitors like rasagiline. When possible, avoid use of buprenorphine in patients who have used a monoamine oxidase inhibitor within the past 14 days due to possible severe adverse effects.
  • Bupropion Possible severe adverse reaction with this combination
  • Buspirone Possible blood pressure elevation
  • Ciprofloxacin Ciprofloxacin, a strong CYP1A2 inhibitor, may decrease the metabolism of rasagiline. Monitor for changes in the therapeutic and adverse effects of rasagiline if ciprofloxacin is initiated or discontinued.
  • Citalopram Possible severe adverse reaction with this combination
  • Clomipramine Possibility of severe adverse effects
  • Cyclobenzaprine Increased risk of toxicity with this association
  • Desipramine Possibility of severe adverse effects
  • Desvenlafaxine Increased risk of serotonin syndrome. Ensure adequate washout period between therapies to avoid toxicity. Concurrent therapy should be avoided.
  • Dexfenfluramine Possible hypertensive crisis
  • Dextroamphetamine Possible hypertensive crisis
  • Dextromethorphan Possible severe adverse reaction
  • Diethylpropion Possible hypertensive crisis
  • Dobutamine Increased arterial pressure
  • Dopamine Increased arterial pressure
  • Doxepin Possibility of severe adverse effects
  • Duloxetine Possible severe adverse reaction with this combination
  • Ephedra Increased arterial pressure
  • Ephedrine Increased arterial pressure
  • Epinephrine Increased arterial pressure
  • Escitalopram Possible severe adverse reaction with this combination
  • Fenfluramine Possible hypertensive crisis
  • Fenoterol Increased arterial pressure
  • Fluoxetine Possible severe adverse reaction with this combination
  • Fluvoxamine Possible severe adverse reaction with this combination
  • Imipramine Possibility of severe adverse effects
  • Isoprenaline Increased arterial pressure
  • Mazindol Possible hypertensive crisis
  • Mephentermine Increased arterial pressure
  • Metaraminol Increased arterial pressure
  • Methamphetamine Possible hypertensive crisis
  • Methoxamine Increased arterial pressure
  • Methylphenidate Possible hypertensive crisis with this combination.
  • Midodrine Risk of hypertensive crisis.
  • Milnacipran Increase serotonin levels. Combination therapy is contraindicated.
  • Mirtazapine Possible severe adverse reaction with this combination
  • Nefazodone Possible severe adverse reaction with this combination
  • Norepinephrine Increased arterial pressure
  • Nortriptyline Possibility of severe adverse effects
  • Orciprenaline Increased arterial pressure
  • Paroxetine Possible severe adverse reaction with this combination
  • Pethidine Increased risk of serotonin syndrome. Concomitant use should be avoided.
  • Phendimetrazine Possible hypertensive crisis
  • Phenmetrazine Possible hypertensive crisis
  • Phentermine Possible hypertensive crisis
  • Phenylephrine Increased arterial pressure
  • Phenylpropanolamine Increased arterial pressure
  • Pirbuterol Increased arterial pressure
  • Procaterol Increased arterial pressure
  • Protriptyline Possibility of severe adverse effects
  • Pseudoephedrine Increased arterial pressure
  • Salbutamol Increased arterial pressure
  • Sertraline Possible severe adverse reaction with this combination
  • Sibutramine Possible serotoninergic syndrome with this combination
  • St. John's Wort Increased risk of toxicity with this association
  • Tapentadol Increases the toxicity of tapentadol by unknown mechanism. Discontinue rasagiline at least 14 days prior to tapentadol administration.
  • Terbutaline Increased arterial pressure
  • Tetrabenazine Tetrabenazine may increase the adverse/toxic effects of Rasagiline. Concomitant therapy is contraindicated.
  • Tolcapone Tolcapone and Rasagiline decrease the metabolism of endogenous catecholamines. Concomitant therapy may result in increased catecholamine effects. Consider alternate therapy or use cautiously and monitor for increased catecholamine effects.
  • Tramadol Tramadol may increase the risk of serotonin syndrome and seizure induction by the MAO inhibitor, rasagiline.
  • Tranylcypromine Increased risk of serotonin syndrome. Use caution during concomitant therapy and monitor for symptoms of serotonin syndrome.
  • Trazodone Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Trimipramine Increased risk of serotonin syndrome. Ensure adequate washout period between therapies to avoid toxicity. Avoid combination or monitor for symptoms of serotonin syndrome and/or hypertensive crisis.
  • Venlafaxine Increased risk of serotonin syndrome. Ensure adequate washout period between therapies to avoid toxicity. Concurrent therapy should be avoided.
  • Zolmitriptan The MAO inhibitor, rasagiline, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing rasagiline are contraindicated.
Liều Lượng & Cách Dùng : Tablet - Oral
Tablet - Oral - 0.5 mg
Tablet - Oral - 1 mg
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Azilect 0.5 mg tablet
    Giá bán buôn : USD >12.11
    Đơn vị tính : tablet
  • Biệt dược thương mại : Azilect 1 mg tablet
    Giá bán buôn : USD >12.11
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Azilect
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