Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | 2C10H15NO.H2O4S |
| Molecular Weight | 428.543 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OS(O)(=O)=O.CN[C@@H](C)[C@H](O)C1=CC=CC=C1.CN[C@@H](C)[C@H](O)C2=CC=CC=C2
InChI
InChIKey=CAVQBDOACNULDN-KHFUBBAMSA-N
InChI=1S/2C10H15NO.H2O4S/c2*1-8(11-2)10(12)9-6-4-3-5-7-9;1-5(2,3)4/h2*3-8,10-12H,1-2H3;(H2,1,2,3,4)/t2*8-,10-;/m00./s1
Ephedrine (l-form) is an alkaloid, which was initially purified from Ephedra plant. The extract form Ephedra has been used in China for medicinal purposes for several thousand years. Ephedrine acts as an agonist at alpha- and beta-adrenergic receptors and indirectly causes the release of norepinephrine from sympathetic neurons. The drug crosses the blood brain barrier and stimulates the central nervous system. Ephedrine products are now banned in many countries, as they are a major source for the production of the addictive compound methamphetamine. FDA has approved ephedrine only for the treatment of clinically important hypotension occurring in the setting of anesthesia.
CNS Activity
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: P07550|||Q53GA6|||Q9UCZ3 Gene ID: 154.0 Gene Symbol: ADRB2 Target Organism: Homo sapiens (Human) |
0.36 µM [EC50] | ||
Target ID: CHEMBL2094251 |
4.95 null [pKi] | ||
Target ID: P08588 Gene ID: 153.0 Gene Symbol: ADRB1 Target Organism: Homo sapiens (Human) |
0.5 µM [EC50] | ||
Target ID: CHEMBL2095158 |
4.83 null [pKi] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | AKOVAZ Approved UseAKOVAZ injection is an alpha- and beta- adrenergic agonist and a norepinephrine-releasing agent that is indicated for the treatment of clinically important hypotension occurring in the setting of anesthesia. Launch Date2016 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
79.4 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/973934/ |
22 mg single, oral dose: 22 mg route of administration: Oral experiment type: SINGLE co-administered: |
EPHEDRINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
87.4 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/973934/ |
11 mg 3 times / day multiple, oral dose: 11 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
EPHEDRINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
6.75 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/973934/ |
22 mg single, oral dose: 22 mg route of administration: Oral experiment type: SINGLE co-administered: |
EPHEDRINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
6.69 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/973934/ |
11 mg 3 times / day multiple, oral dose: 11 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
EPHEDRINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Caffeine and exercise: metabolism, endurance and performance. | 2001 |
|
| Chromatographic analysis of phenethylamine-antihistamine combinations using C8, C18 or cyano columns and micellar sodium dodecyl sulfate-pentanol mixtures. | 2001 Apr |
|
| Mass spectrometric quantitation of chiral drugs by the kinetic method. | 2001 Apr 15 |
|
| Study on the chiral recognition of the enantiomers of ephedrine derivatives with neutral and sulfated heptakis(2,3-O-diacetyl)-beta-cyclodextrins using capillary electrophoresis, UV, nuclear magnetic resonance spectroscopy and mass spectrometry. | 2001 Apr 20 |
|
| Dietary supplements containing ephedra alkaloids. | 2001 Apr 5 |
|
| Intrathecal anaesthesia for the elderly patient: the influence of the induction position on perioperative haemodynamic stability and patient comfort. | 2001 Aug |
|
| Comparison of effects of remifentanil and alfentanil on cardiovascular response to tracheal intubation in hypertensive patients. | 2001 Jan |
|
| [Refractory hypotension sustained during general anesthesia due to chronic treatment with angiotensin-converting enzyme inhibitors]. | 2001 Jan |
|
| Suspected caffeine and ephedrine toxicosis resulting from ingestion of an herbal supplement containing guarana and ma huang in dogs: 47 cases (1997-1999). | 2001 Jan 15 |
|
| Combined spinal and epidural anesthesia with low doses of intrathecal bupivacaine in women with severe preeclampsia: a preliminary report. | 2001 Jan-Feb |
|
| Effect of organic cations on the renal tubular secretion of pseudoephedrine in the rat. | 2001 Jan-Feb |
|
| The effect of betahistine on vestibular habituation: comparison of rotatory and sway habituation training. | 2001 Jul |
|
| A stable gas chromatography-mass spectrometry analysis system to characterize Ma Huang products found in health foods and supplements. | 2001 Jul |
|
| Reduced myocardial carbon-11 hydroxyephedrine retention is associated with poor prognosis in chronic heart failure. | 2001 Mar |
|
| Venlafaxine occupation at the noradrenaline reuptake site: in-vivo determination in healthy volunteers. | 2001 Mar |
|
| High-performance liquid chromatographic method development and validation for the simultaneous quantitation of naproxen sodium and pseudoephedrine hydrochloride impurities. | 2001 Mar |
|
| Neuropeptide Y in obese women during treatment with adrenergic modulation drugs. | 2001 May-Jun |
|
| Kinetic spectrophotometric methods for the quantitation of triprolidine in bulk and in drug formulations. | 2001 Sep |
|
| [Risk management by reporting critical incidents. Vitamin K and ephedrine mix-up at a birthing unit]. | 2001 Sep 24 |
Sample Use Guides
The recommended dosages for the treatment of clinically important hypotension in the setting of
anesthesia is an initial dose of 5 to 10 mg administered by intravenous bolus. Administer additional boluses as needed, not to exceed a total dosage of 50 mg.
Route of Administration:
Intravenous
Segments of guinea-pig ileum were treated with 10(-6)-10(-3) M ephedrine. Ephedrine inhibited the ileal responses to transmural stimulation in the terminal and the proximal ileum with EC50 values of 57.2 and 85.5 uM, respectively. In the proximal part of the ileum, more than 70% of preparations were relaxed by ephedrine.
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NCI_THESAURUS |
C319
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CFR |
21 CFR 346.12
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CFR |
21 CFR 341.16
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21 CFR 341.20
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NCI_THESAURUS |
C87053
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SUB13688MIG
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EPHEDRINE SULFATE
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PRIMARY | Description: Colourless crystals or a white, crystalline powder; odourless.Solubility: Freely soluble in water; sparingly soluble in ethanol (~750 g/l) TS.Category: Antiasthmatic drug.Storage: Ephedrine sulfate should be kept in a well-closed container, protected from light.Additional information: Ephedrine sulfate darkens on exposure to light. Even in the absence of light, it is gradually degraded onexposure to a humid atmosphere, the decomposition being faster at higher temperatures.RequirementsDefinition: Ephedrine sulfate contains not less than 98.0% and not more than 101.0% of (C10H15NO)2,H2SO4, calculated withreference to the dried substance. | ||
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100000078927
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91166
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DTXSID6020565
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U6X61U5ZEG
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DBSALT001503
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CHEMBL211456
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134-72-5
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C72765
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1236007
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m4933
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205-154-4
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U6X61U5ZEG
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5359318
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ACTIVE MOIETY
SUBSTANCE RECORD
