Peringatan Keamanan

Skin, LD50 = 62 mg/kg (rat) MSDS

Pregnancy

Epinephrine is teratogenic in rats when given in doses about 25 times the human doses. It is unknown whether epinephrine can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Epinephrine should be given to a pregnant woman only if clearly required in critical situations/emergencies F2136.

Labor and Delivery
Parenteral administration of epinephrine, if used as support for blood pressure during low or other spinal anesthesia for delivery, can lead to the acceleration of fetal heart rate and should not be used in obstetrics when maternal blood pressure is higher than 130/80. Epinephrine may delay the second stage of labour.

Common and generalized adverse effects:
Transient and minor side effects of anxiety, headache, fear, and palpitations may occur with therapeutic doses of epinephrine, especially in hyperthyroid individuals. Repeated local injections may result in necrosis at sites of injection due to vascular constriction. Cerebral hemorrhage; hemiplegia; subarachnoid hemorrhage; anginal pain in patients with angina pectoris; anxiety; restlessness; throbbing headache; tremor; weakness; dizziness; pallor; respiratory difficulty; palpitation; apprehensiveness; sweating; nausea; vomiting FDA label.

Cardiovascular effects: Inadvertently induced high arterial blood pressure may result in angina pectoris (especially when coronary insufficiency is present), cardiac ischemia, or aortic rupture FDA label, L4825. Epinephrine may cause serious cardiac arrhythmias in patients not suffering from heart disease and patients with organic heart disease receiving drugs that sensitize the cardiac muscle. With the injection of epinephrine 1:1,000, a paradoxical but transient lowering of blood pressure, bradycardia and apnea may occur immediately post-injection FDA label.

Cerebrovascular hemorrhage: Overdosage or accidental I.V. injection of epinephrine may lead to cerebrovascular hemorrhage resulting from the sharp rise in blood pressure FDA label.

Renal vasoconstriction: Parenterally administered epinephrine initially may produce constriction of renal blood vessels and decrease urine formation. High doses may cause complete renal shutdown F2136.

Pulmonary edema: Fatality may also result from pulmonary edema due to the peripheral constriction and cardiac stimulation produced by epinephrine injection FDA label.

Digital vasoconstriction: Since epinephrine is a strong vasoconstrictor, accidental injection into the digits, hands or feet may lead to the loss of blood flow to the affected area. Treatment should be directed at vasodilation in addition to further treatment of anaphylaxis FDA label.

Epinephrine

DB00668

small molecule approved vet_approved

Deskripsi

Epinephrine, also known as adrenaline, is a hormone and neurotransmitter and produced by the adrenal glands that can also be used as a drug due to its various important functions. Though it has long been used in the treatment of hypersensitivity reactions, epinephrine in the auto-injector form (EpiPen) has been available since 1987 in the USA. Many new products/biosimilars and dosage routes have been approved under various names over the last several decades L4355, L4356, L4358. On August 16, 2018, Teva Pharmaceuticals USA gained approval to market its generic epinephrine auto-injector in 0.3 mg and 0.15 mg strengths L4353. Dosage delivery routes for epinephrine include intravenous, inhalation, nebulization, intramuscular injection, and subcutaneous injection.

In general, the most common uses of parenteral epinephrine are to relieve respiratory distress due to bronchospasm, to provide rapid relief of hypersensitivity (anaphylactic or anaphylactoid) reactions to drugs, animal serums and other allergens, and to prolong the action of infiltration anesthetics F2136. In addition to the above functions, epinephrine is the primary drug administered during cardiopulmonary resuscitation (CPR) to reverse cardiac arrest A37697, A37699. It can be used in severe cases of croup L4824.

Struktur Molekul 2D

Berat 183.2044
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The plasma half-life is approximately 2-3 minutes. However, when administered by subcutaneous or intramuscular injection, local vasoconstriction may delay absorption so that epinephrine's effects may last longer than the half-life suggests [L4361].
Volume Distribusi -
Klirens (Clearance) Intravenous injection produces an immediate and intensified response. Following intravenous injection, epinephrine disappears rapidly from the blood stream [F2136].

Absorpsi

Following I.V. (intravenous) injection, epinephrine disappears rapidly from the blood stream. Subcutaneously or I.M. (intramuscular) administered epinephrine has a rapid onset and short duration of action. Subcutaneous (SC) administration during asthmatic attacks may produce bronchodilation within 5 to 10 minutes, and maximal effects may occur within 20 minutes. The drug becomes fixed in the tissues rapidly F1247, FDA label.

Metabolisme

Epinephrine is rapidly inactivated mainly by enzymic transformation to metanephrine or normetanephrine, either of which is then conjugated and excreted in the urine in the form of both sulfates and glucuronides. Either sequence results in the formation of 3-methoxy-4- hydroxy-mandelic acid(vanillylmandelic acid, VMA) which is shown to be detectable in the urine F1247. Epinephrine is rapidly inactivated in the body mostly by the enzymes COMT (catechol-O-methyltransferase) and MAO (monoamine oxidase). The liver is abundant in the above enzymes, and is a primary, although not essential, tissue in the degradation process L4361.

Rute Eliminasi

The majority of the dose of epinephrine is seen excreted in the urine L4361, FDA label. About 40% of a parenteral dose of epinephrine is excreted in urine as metanephrine, 40% as VMA, 7% as 3-methoxy-4-hydroxyphenoglycol, 2% as 3,4-dihydroxymandelic acid, and the rest as acetylated derivatives. These metabolites are excreted mainly as the sulfate conjugates and, to a lesser extent, the glucuronide conjugates. Only small amounts of the drug are excreted completely unchanged L4827.

Interaksi Obat

1293 Data
Ramipril Epinephrine may decrease the antihypertensive activities of Ramipril.
Remikiren Epinephrine may decrease the antihypertensive activities of Remikiren.
Olmesartan Epinephrine may decrease the antihypertensive activities of Olmesartan.
Nitroprusside Epinephrine may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Epinephrine may decrease the antihypertensive activities of Minoxidil.
Fosinopril Epinephrine may decrease the antihypertensive activities of Fosinopril.
Trandolapril Epinephrine may decrease the antihypertensive activities of Trandolapril.
Benazepril Epinephrine may decrease the antihypertensive activities of Benazepril.
Candoxatril Epinephrine may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Epinephrine may decrease the antihypertensive activities of Mecamylamine.
Moexipril Epinephrine may decrease the antihypertensive activities of Moexipril.
Lisinopril Epinephrine may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Epinephrine may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Epinephrine may decrease the antihypertensive activities of Metyrosine.
Cryptenamine Epinephrine may decrease the antihypertensive activities of Cryptenamine.
Perindopril Epinephrine may decrease the antihypertensive activities of Perindopril.
Fenoldopam Epinephrine may decrease the antihypertensive activities of Fenoldopam.
Eprosartan Epinephrine may decrease the antihypertensive activities of Eprosartan.
Quinapril Epinephrine may decrease the antihypertensive activities of Quinapril.
Telmisartan Epinephrine may decrease the antihypertensive activities of Telmisartan.
Methyldopa Epinephrine may decrease the antihypertensive activities of Methyldopa.
Deserpidine Epinephrine may decrease the antihypertensive activities of Deserpidine.
Pentolinium Epinephrine may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Epinephrine may decrease the antihypertensive activities of Trimethaphan.
Captopril Epinephrine may decrease the antihypertensive activities of Captopril.
Epoprostenol Epinephrine may decrease the antihypertensive activities of Epoprostenol.
Hydralazine Epinephrine may decrease the antihypertensive activities of Hydralazine.
Cilazapril Epinephrine may decrease the antihypertensive activities of Cilazapril.
Saprisartan Epinephrine may decrease the antihypertensive activities of Saprisartan.
Spirapril Epinephrine may decrease the antihypertensive activities of Spirapril.
Debrisoquine Epinephrine may decrease the antihypertensive activities of Debrisoquine.
Diethylnorspermine Epinephrine may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Epinephrine may decrease the antihypertensive activities of Temocapril.
Hexamethonium Epinephrine may decrease the antihypertensive activities of Hexamethonium.
Nicorandil Epinephrine may decrease the antihypertensive activities of Nicorandil.
Rauwolfia serpentina root Epinephrine may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Epinephrine may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Epinephrine may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Epinephrine may decrease the antihypertensive activities of Imidapril.
BQ-123 Epinephrine may decrease the antihypertensive activities of BQ-123.
Dihydralazine Epinephrine may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Epinephrine may decrease the antihypertensive activities of Zofenopril.
Guanoxan Epinephrine may decrease the antihypertensive activities of Guanoxan.
Delapril Epinephrine may decrease the antihypertensive activities of Delapril.
Vincamine Epinephrine may decrease the antihypertensive activities of Vincamine.
Linsidomine Epinephrine may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Epinephrine may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Epinephrine may decrease the antihypertensive activities of Tolonidine.
Endralazine Epinephrine may decrease the antihypertensive activities of Endralazine.
Cadralazine Epinephrine may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Epinephrine may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Epinephrine may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Epinephrine may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Epinephrine may decrease the antihypertensive activities of Guanoclor.
Tocopherylquinone Epinephrine may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Epinephrine may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Epinephrine may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Epinephrine may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Epinephrine may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Epinephrine may decrease the antihypertensive activities of Quinaprilat.
Enalapril Epinephrine may decrease the antihypertensive activities of Enalapril.
Isradipine Epinephrine may decrease the antihypertensive activities of Isradipine.
Amlodipine Epinephrine may decrease the antihypertensive activities of Amlodipine.
Nimodipine Epinephrine may decrease the antihypertensive activities of Nimodipine.
Lercanidipine Epinephrine may decrease the antihypertensive activities of Lercanidipine.
Nitrendipine Epinephrine may decrease the antihypertensive activities of Nitrendipine.
Bepridil Epinephrine may decrease the antihypertensive activities of Bepridil.
Mibefradil Epinephrine may decrease the antihypertensive activities of Mibefradil.
Ambrisentan Epinephrine may decrease the antihypertensive activities of Ambrisentan.
Nilvadipine Epinephrine may decrease the antihypertensive activities of Nilvadipine.
Pinacidil Epinephrine may decrease the antihypertensive activities of Pinacidil.
Riociguat Epinephrine may decrease the antihypertensive activities of Riociguat.
Macitentan Epinephrine may decrease the antihypertensive activities of Macitentan.
Aliskiren Epinephrine may decrease the antihypertensive activities of Aliskiren.
Lacidipine Epinephrine may decrease the antihypertensive activities of Lacidipine.
Manidipine Epinephrine may decrease the antihypertensive activities of Manidipine.
Selexipag Epinephrine may decrease the antihypertensive activities of Selexipag.
Tetrahydropalmatine Epinephrine may decrease the antihypertensive activities of Tetrahydropalmatine.
Dexniguldipine Epinephrine may decrease the antihypertensive activities of Dexniguldipine.
Tadalafil Epinephrine may decrease the antihypertensive activities of Tadalafil.
Nisoldipine Epinephrine may decrease the antihypertensive activities of Nisoldipine.
Felodipine Epinephrine may decrease the antihypertensive activities of Felodipine.
Azilsartan medoxomil Epinephrine may decrease the antihypertensive activities of Azilsartan medoxomil.
Diazoxide Epinephrine may decrease the antihypertensive activities of Diazoxide.
Linezolid The risk or severity of hypertension can be increased when Linezolid is combined with Epinephrine.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Epinephrine.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Epinephrine.
Benzylpenicilloyl polylysine Epinephrine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Desmopressin The risk or severity of hypertension can be increased when Desmopressin is combined with Epinephrine.
Icosapent The risk or severity of hypertension can be increased when Icosapent is combined with Epinephrine.
Bethanidine Epinephrine may decrease the antihypertensive activities of Bethanidine.
Mesalazine The risk or severity of hypertension can be increased when Mesalazine is combined with Epinephrine.
Etomidate The risk or severity of hypertension can be increased when Etomidate is combined with Epinephrine.
Zolmitriptan The risk or severity of hypertension can be increased when Zolmitriptan is combined with Epinephrine.
Methylphenidate The risk or severity of hypertension can be increased when Methylphenidate is combined with Epinephrine.
Tolmetin The risk or severity of hypertension can be increased when Tolmetin is combined with Epinephrine.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Epinephrine.
Atropine The risk or severity of hypertension can be increased when Atropine is combined with Epinephrine.
Fenoprofen The risk or severity of hypertension can be increased when Fenoprofen is combined with Epinephrine.
Sulindac The risk or severity of hypertension can be increased when Sulindac is combined with Epinephrine.

Target Protein

Alpha-1A adrenergic receptor ADRA1A
Alpha-1B adrenergic receptor ADRA1B
Beta-1 adrenergic receptor ADRB1
Beta-2 adrenergic receptor ADRB2
Alpha-2A adrenergic receptor ADRA2A
Alpha-2B adrenergic receptor ADRA2B
Alpha-1D adrenergic receptor ADRA1D
Tumor necrosis factor TNF

Referensi & Sumber

Synthesis reference: Pamela Albaugh, "Pharmaceutical epinephrine-pilocarpine compounds and process of preparation thereof." U.S. Patent US5198545, issued October, 1988.
Artikel (PubMed)
  • PMID: 12717538
    Yamashima T: Jokichi Takamine (1854-1922), the samurai chemist, and his work on adrenalin. J Med Biogr. 2003 May;11(2):95-102.
  • PMID: 10454061
    Bennett MR: One hundred years of adrenaline: the discovery of autoreceptors. Clin Auton Res. 1999 Jun;9(3):145-59.
  • PMID: 7214942
    Otto CW, Yakaitis RW, Blitt CD: Mechanism of action of epinephrine in resuscitation from asphyxial arrest. Crit Care Med. 1981 Apr;9(4):321-4.
  • PMID: 23196774
    Callaway CW: Epinephrine for cardiac arrest. Curr Opin Cardiol. 2013 Jan;28(1):36-42. doi: 10.1097/HCO.0b013e32835b0979.
  • PMID: 28836556
    Shao H, Li CS: Epinephrine in Out-of-hospital Cardiac Arrest: Helpful or Harmful? Chin Med J (Engl). 2017 Sep 5;130(17):2112-2116. doi: 10.4103/0366-6999.213429.
  • PMID: 8609227
    van der Poll T, Coyle SM, Barbosa K, Braxton CC, Lowry SF: Epinephrine inhibits tumor necrosis factor-alpha and potentiates interleukin 10 production during human endotoxemia. J Clin Invest. 1996 Feb 1;97(3):713-9.
  • PMID: 24114291
    Bjornson C, Russell K, Vandermeer B, Klassen TP, Johnson DW: Nebulized epinephrine for croup in children. Cochrane Database Syst Rev. 2013 Oct 10;(10):CD006619. doi: 10.1002/14651858.CD006619.pub3.

Contoh Produk & Brand

Produk: 525 • International brands: 1
Produk
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  • 4% Astracaine Dental With Epinephrine Forte 1:100,000 (0.01mg/ml)
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  • 4% Astracaine Dental With Epinephrine Forte 1:100,000 (0.01mg/ml)
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  • Adrenaclick
    Injection • 1 mg/1mL • Intramuscular; Subcutaneous • US • Approved
  • Adrenaclick
    Injection • 1 mg/1mL • Intramuscular; Subcutaneous • US • Approved
Menampilkan 8 dari 525 produk.
International Brands
  • Epi EZ Pen JR

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