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药品详细

Phenylephrine(福林)

化学结构式图
中文名
福林
英文名
Phenylephrine
分子式
C9H13NO2
化学名
3-[(1R)-1-hydroxy-2-(methylamino)ethyl]phenol
分子量
Average: 167.205
Monoisotopic: 167.094628665
CAS号
59-42-7
ATC分类
C01C 未知;R01A 未知;R01A 未知;R01B 未知;S01F 扩瞳药及睫状肌麻痹药;S01G 解充血药及抗过敏药;C05A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Phenylephrine is a sympathomimetic amine that acts predominantly on α-adrenergic receptors. It is mainly used to treat nasal congestion, but may also be useful in treating hypotension and shock, hypotension during spinal anaesthesia, prolongation of spinal anaesthesia, paroxysmal supraventricular tachycardia, symptomatic relief of external or internal hemorrhoids, and to increase blood pressure as an aid in the diagnosis of heart murmurs.

生产厂家
    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
    • Benzyl Alcohols and Derivatives
    • Phenols and Derivatives
    • Phenethylamines
    Substructures
    • Hydroxy Compounds
    • Benzyl Alcohols and Derivatives
    • Aliphatic and Aryl Amines
    • Phenols and Derivatives
    • Benzene and Derivatives
    • Amino Alcohols
    • Phenethylamines
    • Aromatic compounds
    • Alcohols and Polyols
    • Phenyl Esters
    适应症
    药理
    Indication Phenylephrine is mainly used to treat nasal congestion, but may also be useful in treating hypotension and shock, hypotension during spinal anaesthesia, prolongation of spinal anaesthesia, paroxysmal supraventricular tachycardia, symptomatic relief of external or internal hemorrhoids, and to increase blood pressure as an aid in the diagnosis of heart murmurs.
    Pharmacodynamics Phenylephrine is a powerful vasoconstrictor. It is used as a nasal decongestant and cardiotonic agent. Phenylephrine is a postsynaptic α1-receptor agonist with little effect on β-receptors of the heart. Parenteral administration of phenylephrine causes a rise in systolic and diastolic pressures, a slight decrease in cardiac output, and a considerable increase in peripheral resistance; most vascular beds are constricted, and renal, splanchnic, cutaneous, and limb blood flows are reduced while coronary blood flow is increased. Phenelephrine also causes pulmonary vessel constriction and subsequent increase in pulmonary arterial pressure. Vasoconstriction in the mucosa of the respiratory tract leads to decreased edema and increased drainage of sinus cavities.
    Mechanism of action In general, α1-adrenergic receptors mediate contraction and hypertrophic growth of smooth muscle cells. α1-receptors are 7-transmembrane domain receptors coupled to G proteins, Gq/11. Three α1-receptor subtypes, which share approximately 75% homology in their transmembrane domains, have been identified: α1A (chromosome 8), α1B (chromosome 5), and α1D (chromosome 20). Phenylephrine appears to act similarly on all three receptor subtypes. All three receptor subtypes appear to be involved in maintaining vascular tone. The α1A-receptor maintains basal vascular tone while the α1B-receptor mediates the vasocontrictory effects of exogenous α1-agonists. Activation of the α1-receptor activates Gq-proteins, which results in intracellular stimulation of phospholipases C, A2, and D. This results in mobilization of Ca2+ from intracellular stores, activation of mitogen-activated kinase and PI3 kinase pathways and subsequent vasoconstriction. Phenylephrine produces its local and systemic actions by acting on α1-adrenergic receptors peripheral vascular smooth muscle. Stimulation of the α1-adrenergic receptors results in contraction arteriolar smooth muscle in the periphery. Phenylephrine decreases nasal congestion by acting on α1-adrenergic receptors in the arterioles of the nasal mucosa to produce constriction; this leads to decreased edema and increased drainage of the sinus cavities.
    Absorption Completely absorbed after oral administration. It has a reduced bioavailability (compared to pseudoephedrine) following oral administration due to significant first-pass metabolism in the intestinal wall. Compared to IV administration, bioavailability is approximately 38%. Peak serum concentrations are achieved approximately 0.75-2 hours following oral administration. Phenylephrine should be administered parenterally to achieve cardiovascular effects. Occasionally, systemic effects are observed following oral inhalation.
    Volume of distribution Not Available
    Protein binding 95% binding-plasma proteins
    Metabolism
    Undergoes extensive first-pass metabolism in the intestinal wall and extensive metabolism in the liver. Sulfate conjugation, primarily in the intestinal wall, and oxidative metabolism by monoamine oxidase (MAO) represent the principle routes of metabolism. Glucuronidation occurs to a lesser extent. Phenylephrine and its metabolites are mainly excreted in urine/ .
    Route of elimination Not Available
    Half life 2.1 to 3.4 hours
    Clearance Not Available
    Toxicity Not Available
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 140-145 °C Not Available
    water solubility Freely soluble in water Not Available
    logP -0.31 HANSCH,C ET AL. (1995)
    pKa 8.97 SANGSTER (1994)
    Predicted Properties
    Property Value Source
    water solubility 2.20e+01 g/l ALOGPS
    logP -0.69 ALOGPS
    logP -0.07 ChemAxon
    logS -0.88 ALOGPS
    pKa (strongest acidic) 9.07 ChemAxon
    pKa (strongest basic) 9.69 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 3 ChemAxon
    hydrogen donor count 3 ChemAxon
    polar surface area 52.49 ChemAxon
    rotatable bond count 3 ChemAxon
    refractivity 47.25 ChemAxon
    polarizability 18.2 ChemAxon
    药物相互作用
    Drug Interaction
    Alseroxylon Increased arterial pressure
    Amitriptyline The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of phenylephrine.
    Amoxapine The tricyclic antidepressant, amoxapine, increases the sympathomimetic effect of phenylephrine.
    Clomipramine The tricyclic antidepressant, clomipramine, increases the sympathomimetic effect of phenylephrine.
    Deserpidine Increased arterial pressure
    Desipramine The tricyclic antidepressant, desipramine, increases the sympathomimetic effect of phenylephrine.
    Doxepin The tricyclic antidepressant, doxepin, increases the sympathomimetic effect of phenylephrine.
    Ergonovine Possible marked increase of arterial pressure
    Guanethidine Phenylephrine may decrease the effect of guanethidine.
    Imipramine The tricyclic antidepressant, imipramine, increases the sympathomimetic effect of phenylephrine.
    Iobenguane Sympathomimetic that increase chances of producing a false negative imaging result
    Isocarboxazid Increased arterial pressure
    Linezolid Possible increase of arterial pressure
    Methyldopa Increased arterial pressure
    Methylergonovine Possible marked increase of arterial pressure
    Midodrine Increased arterial pressure
    Moclobemide Moclobemide increases the sympathomimetic effect of phenylephrine.
    Nortriptyline The tricyclic antidepressant, nortriptyline, increases the sympathomimetic effect of phenylephrine.
    Oxytocin Possible marked increase of arterial pressure
    Pargyline Increased arterial pressure
    Phenelzine Increased arterial pressure
    Protriptyline The tricyclic antidepressant, protriptyline, increases the sympathomimetic effect of phenylephrine.
    Rasagiline Increased arterial pressure
    Reserpine Increased arterial pressure
    Tranylcypromine The MAO inhibitor, Tranylcypromine, may increase the vasopressor effect of the alpha1-agonist, Phenylephrine. Concomitant therapy should be avoided.
    Trimipramine Trimipramine may increase the vasopressor effect of the alpha1-agonist, Phenylephrine. Avoid combination if possible. Monitor sympathetic response to therapy if used concomitantly.
    食物相互作用
    • Take without regard to meals.

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