Tìm theo
Epinephrine
Các tên gọi khác (22 ) :
  • (-)-(R)-Epinephrine
  • (-)-3,4-Dihydroxy-alpha-((methylamino)methyl)benzyl alcohol
  • (-)-Adrenaline
  • (−)-adrenaline
  • (R)-(-)-Adnephrine
  • (R)-(-)-Adrenaline
  • (R)-(-)-Epinephrine
  • (R)-(-)-Epirenamine
  • (R)-(−)-adrenaline
  • 4-[(1R)-1-Hydroxy-2-(methylamino)ethyl]-1,2-benzenediol
  • Adrenalin
  • Adrenaline
  • Epinefrin
  • Epinefrina
  • Epinephrin
  • Epinephrine
  • Epinephrinum
  • Epipen
  • Epipen jr
  • L-Adrenaline
  • levoepinephrine
  • Primatene
Thuốc cấp cứu & giải độc
Thuốc Gốc
Small Molecule
CAS: 51-43-4
ATC: A01AD01, B02BC09, C01CA24, R01AA14, R03AA01, S01EA01
ĐG : Adamis Laboratories , http://www.adamispharmaceuticals.com
CTHH: C9H13NO3
PTK: 183.2044
The active sympathomimetic hormone from the adrenal medulla in most species. It stimulates both the alpha- and beta- adrenergic systems, causes systemic vasoconstriction and gastrointestinal relaxation, stimulates the heart, and dilates bronchi and cerebral vessels. It is used in asthma and cardiac failure and to delay absorption of local anesthetics. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C9H13NO3
Phân tử khối
183.2044
Monoisotopic mass
183.089543287
InChI
InChI=1S/C9H13NO3/c1-10-5-9(13)6-2-3-7(11)8(12)4-6/h2-4,9-13H,5H2,1H3/t9-/m0/s1
InChI Key
InChIKey=UCTWMZQNUQWSLP-VIFPVBQESA-N
IUPAC Name
4-[(1R)-1-hydroxy-2-(methylamino)ethyl]benzene-1,2-diol
Traditional IUPAC Name
epinephrine
SMILES
CNC[C@H](O)C1=CC(O)=C(O)C=C1
Độ tan chảy
211.5 °C
Độ hòa tan
180 mg/L (at 20 °C)
logP
-1.37
logS
-0.99
pKa (strongest acidic)
9.69
pKa (Strongest Basic)
8.91
PSA
72.72 Å2
Refractivity
49.23 m3·mol-1
Polarizability
19.04 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
4
H Bond Donor Count
4
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
caco2 Permeability
-6.02
pKa
8.59 (at 25 °C)
Dược Lực Học : Epinephrine is indicated for intravenous injection in treatment of acute hypersensitivity, treatment of acute asthmatic attacks to relieve bronchospasm, and treatment and prophylaxis of cardiac arrest and attacks of transitory atrioventricular heart block with syncopal seizures (Stokes-Adams Syndrome). The actions of epinephrine resemble the effects of stimulation of adrenergic nerves. To a variable degree it acts on both alpha and beta receptor sites of sympathetic effector cells. Its most prominent actions are on the beta receptors of the heart, vascular and other smooth muscle. When given by rapid intravenous injection, it produces a rapid rise in blood pressure, mainly systolic, by (1) direct stimulation of cardiac muscle which increases the strength of ventricular contraction, (2) increasing the heart rate and (3) constriction of the arterioles in the skin, mucosa and splanchnic areas of the circulation. When given by slow intravenous injection, epinephrine usually produces only a moderate rise in systolic and a fall in diastolic pressure. Although some increase in pulse pressure occurs, there is usually no great elevation in mean blood pressure. Accordingly, the compensatory reflex mechanisms that come into play with a pronounced increase in blood pressure do not antagonize the direct cardiac actions of epinephrine as much as with catecholamines that have a predominant action on alpha receptors.
Cơ Chế Tác Dụng : The active sympathomimetic hormone from the adrenal medulla in most species. It stimulates both the alpha- and beta- adrenergic systems, causes systemic vasoconstriction and gastrointestinal relaxation, stimulates the heart, and dilates bronchi and cerebral vessels. It is used in asthma and cardiac failure and to delay absorption of local anesthetics. [PubChem] Epinephrine works via the stimulation of alpha and beta-1 adrenergic receptors, and a moderate activity at beta-2 adrenergic receptors.
Dược Động Học :
▧ Absorption :
Usually this vasodilator effect of the drug on the circulation predominates so that the modest rise in systolic pressure which follows slow injection or absorption is mainly the result of direct cardiac stimulation and increase in cardiac output.
▧ Metabolism :
Epinephrine is rapidly inactivated in the body and is degraded by enzymes in the liver and other tissues. The larger portion of injected doses is excreted in the urine as inactivated compounds and the remainder either partly unchanged or conjugated. The drug becomes fixed in the tissues and is inactivated chiefly by enzymatic transformation to metanephrine or normetanephrine either of which is subsequently conjugated and excreted in the urine in the form of sulfates and glucuronides. Either sequence results in the formation of 3-methoxy-4-hydroxy-mandelic acid which also is detectable in the urine. Main metabolic enzymes include MAO and COMT
▧ Route of Elimination :
Renal
▧ Half Life :
2 minutes
Độc Tính : Skin, LD50 = 62 mg/kg (rat)
Chỉ Định : Used to treat anaphylaxis and sepsis. Also one of the body's main adrenergic neurotransmitters.
Tương Tác Thuốc :
  • Acebutolol Hypertension, then bradycardia
  • Alseroxylon Increased arterial pressure
  • Amitriptyline The tricyclic antidepressant, amitriptyline, may increase the sympathomimetic effect of epinephrine.
  • Amoxapine The tricyclic antidepressant, amoxapine, increases the sympathomimetic effect of epinephrine.
  • Atenolol Hypertension, then bradycardia
  • Betaxolol Beta-Blockers such as betaxolol may enhance the vasopressor effect of epinephrine. Monitor for increases in pressor effects of alpha-/beta-agonists if used in patients receiving beta-blocker therapy (including ophthalmic products). Beta1-selective (i.e., “cardioselective”) agents may confer a more limited risk if used in low enough doses to allow them to retain their selectivity. The amount of epinephrine used in dental procedures as part of local anesthetic administration is not likely to be of clinical concern. Infiltrating larger volumes of local anesthetics for other surgical procedures (e.g., more than 0.06mg epinephrine) may cause clinically-relevant problems. Patients with allergies that require carrying and periodically using subcutaneous epinephrine (e.g., bee sting kits) should probably avoid the use of beta blockers.
  • Bevantolol Hypertension, then bradycardia
  • Bisoprolol Hypertension, then bradycardia
  • Carteolol Hypertension, then bradycardia
  • Carvedilol Hypertension, then bradycardia
  • Clomipramine The tricyclic antidepressant, clomipramine, increases the sympathomimetic effect of epinephrine.
  • Deserpidine Increased arterial pressure
  • Desipramine Trimipramine may increase the vasopressor effect of the direct-acting alpha-/beta-agonist, Epinephrine. Avoid combination if possible. Monitor sympathetic response to therapy if used concomitantly.
  • Desvenlafaxine Desvenlafaxine may increase the tachycardic and vasopressor effects of epinephrine. Consider alternate therapy or monitor for increased sympathomimetic effects, such as increased blood pressure, chest pain and headache.
  • Doxepin The tricyclic antidepressant, doxepin, increases the sympathomimetic effect of epinephrine.
  • Entacapone Entacapone may increase the effect and toxicity of the sympathomimetic, epinephrine.
  • Ergonovine Possible marked increase of arterial pressure
  • Esmolol Hypertension, then bradycardia
  • Guanethidine Epinephrine may decrease the effect of guanethidine.
  • Imipramine The tricyclic antidepressant, imipramine, increases the sympathomimetic effect of epinephrine.
  • Insulin Lispro Concomitant therapy with sympathomimetic agents may reduce the blood-glucose-lowering effect of insulin lispro.
  • Isocarboxazid Increased arterial pressure
  • Labetalol Hypertension, then bradycardia
  • Linezolid Possible increase of arterial pressure
  • Lurasidone Epinephrine increases toxicity (enhance hypotensive effects) of lurasidone by pharmacodynamic synergism.
  • Methyldopa Increased arterial pressure
  • Methylergometrine Possible marked increase of arterial pressure
  • Metoprolol Hypertension, then bradycardia
  • Midodrine Increased arterial pressure
  • Moclobemide Moclobemide increases the sympathomimetic effect of epinephrine.
  • Nadolol Hypertension, then bradycardia
  • Nortriptyline The tricyclic antidepressant, nortriptyline, increases the sympathomimetic effect of epinephrine.
  • Oxprenolol Hypertension, then bradycardia
  • Oxytocin Possible marked increase of arterial pressure
  • Pargyline Increased arterial pressure
  • Penbutolol Hypertension, then bradycardia
  • Phenelzine Increased arterial pressure
  • Pindolol Hypertension, then bradycardia
  • Practolol Hypertension, then bradycardia
  • Propranolol Hypertension, then bradycardia
  • Protriptyline The tricyclic antidepressant, protriptyline, increases the sympathomimetic effect of epinephrine.
  • Rasagiline Increased arterial pressure
  • Reserpine Increased arterial pressure
  • Sotalol Hypertension, then bradycardia
  • Timolol Hypertension, then bradycardia
  • Tranylcypromine Increased arterial pressure
  • Trimipramine Trimipramine may increase the vasopressor effect of the direct-acting alpha-/beta-agonist, Epinephrine. Avoid combination if possible. Monitor sympathetic response to therapy if used concomitantly.
  • Venlafaxine Venlafaxine may increase the tachycardic and vasopressor effects of epinephrine. Consider alternate therapy or monitor for increased sympathomimetic effects, such as increased blood pressure, chest pain and headache.
Liều Lượng & Cách Dùng : Liquid - Intramuscular
Liquid - Oral
Solution - Intramuscular
Solution - Intravenous
Solution - Nasal
Solution - Respiratory (inhalation)
Solution / drops - Ophthalmic
Solution / drops - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Adrenaclick
  • Công ty :
    Sản phẩm biệt dược : Adrenalin
  • Công ty :
    Sản phẩm biệt dược : Anapen
  • Công ty :
    Sản phẩm biệt dược : Auvi-q
  • Công ty :
    Sản phẩm biệt dược : Epi EZ Pen JR
  • Công ty :
    Sản phẩm biệt dược : EpiPen
  • Công ty :
    Sản phẩm biệt dược : Medihaler-Epi
  • Công ty :
    Sản phẩm biệt dược : Primatene
  • Công ty :
    Sản phẩm biệt dược : Twinject
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00668
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5816
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46509097
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C00788
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00095
ChemSpider
http://www.chemspider.com/Chemical-Structure.5611.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/59630-803-01
PharmGKB
http://www.pharmgkb.org/drug/PA449470
Wikipedia
http://en.wikipedia.org/wiki/Epinephrine
RxList
http://www.rxlist.com/cgi/generic/epi.htm
Drugs.com
http://www.drugs.com/mtm/epinephrine-ophthalmic.html
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