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药品详细

Pargyline(优降宁)

化学结构式图
中文名
优降宁
英文名
Pargyline
分子式
C11H13N
化学名
benzyl(methyl)(prop-2-yn-1-yl)amine
分子量
Average: 159.2276
Monoisotopic: 159.104799421
CAS号
555-57-7
ATC分类
C02K Other Antihypertensives;C02L 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A monoamine oxidase inhibitor with antihypertensive properties. [PubChem]

生产厂家
  • Abbott laboratories pharmaceutical products div
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
规格
化合物类型
Type small molecule
Classes
  • Benzene and Derivatives
Substructures
  • Alkynes
  • Benzene and Derivatives
  • Aliphatic and Aryl Amines
  • Aromatic compounds
适应症
药理
Indication For the treatment of moderate to severe hypertension.
Pharmacodynamics Pargyline is a monoamine oxidase B (MAO-B) inhibitor with antihypertensive properties. Patients taking pargyline must avoid concurrent consumption of tyramine-containing foods such as bleu cheese and beer, as this can lead to a hypertensive crisis.
Mechanism of action MAOIs act by inhibiting the activity of monoamine oxidase, thus preventing the breakdown of monoamine neurotransmitters and thereby increasing their availability. There are two isoforms of monoamine oxidase, MAO-A and MAO-B. MAO-A preferentially deaminates serotonin, melatonin, epinephrine and norepinephrine. MAO-B preferentially deaminates phenylethylamine and trace amines. Pargyline functions by inhibiting the metabolism of catecholamines and tyramine within presynaptic nerve terminals. Catecholamines cause general physiological changes that prepare the body for physical activity (fight-or-flight response). Some typical effects are increases in heart rate, blood pressure, blood glucose levels, and a general reaction of the sympathetic nervous system.
Absorption Not Available
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Not Available
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties Not Available
Predicted Properties
Property Value Source
water solubility 9.98e-02 g/l ALOGPS
logP 2.05 ALOGPS
logP 2.14 ChemAxon
logS -3.2 ALOGPS
pKa (strongest basic) 8.13 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 1 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 3.24 ChemAxon
rotatable bond count 3 ChemAxon
refractivity 52.18 ChemAxon
polarizability 18.78 ChemAxon
药物相互作用
Drug Interaction
Epinephrine Increased arterial pressure
Fenoterol Increased arterial pressure
Guanethidine Pargyline may decrease the effect of guanethidine.
Methotrimeprazine Possible severe adverse reaction with this combination
Milnacipran Increase serotonin levels. Combination therapy is contraindicated.
Orciprenaline Increased arterial pressure
Phenylephrine Increased arterial pressure
Phenylpropanolamine Increased arterial pressure
Pseudoephedrine Increased arterial pressure
Terbutaline Increased arterial pressure
食物相互作用
  • Food increases the oral bioavailability by 3-5 fold.

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