Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C10H15NO.CHNS |
| Molecular Weight | 224.323 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
SC#N.CN[C@@H](C)[C@H](O)C1=CC=CC=C1
InChI
InChIKey=RHPLXTLBWAZINH-GNAZCLTHSA-N
InChI=1S/C10H15NO.CHNS/c1-8(11-2)10(12)9-6-4-3-5-7-9;2-1-3/h3-8,10-12H,1-2H3;3H/t8-,10-;/m0./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 |
|---|---|---|
| Ephedrine-induced complete atrioventricular block with ventricular asystole during rapid concomitant phenytoin infusion: a case report. | 1999 Mar |
|
| The use of oral vasopressors in the management of autonomic dysfunction and orthostatic hypotension. | 1999 May |
|
| The haemodynamic effects of propofol in combination with ephedrine in elderly patients (ASA groups 3 and 4). | 1999 Oct |
|
| Caffeine and exercise: metabolism, endurance and performance. | 2001 |
|
| Recurrent ischaemic colitis associated with pseudoephedrine use. | 2001 Apr |
|
| [Misuse of drugs in recreational sports]. | 2001 Apr |
|
| Chromatographic analysis of phenethylamine-antihistamine combinations using C8, C18 or cyano columns and micellar sodium dodecyl sulfate-pentanol mixtures. | 2001 Apr |
|
| The effects of an increase of central blood volume before spinal anesthesia for cesarean delivery: a qualitative systematic review. | 2001 Apr |
|
| Mass spectrometric quantitation of chiral drugs by the kinetic method. | 2001 Apr 15 |
|
| Phenylpropanolamine and hemorrhagic stroke. | 2001 Apr 5 |
|
| Role of the atrial natriuretic factor in obstetric spinal hypotension. | 2001 Aug |
|
| Comparison of metaraminol and ephedrine infusions for maintaining arterial pressure during spinal anesthesia for elective cesarean section. | 2001 Aug |
|
| Hypokalemic metabolic acidosis attributed to cough mixture abuse. | 2001 Aug |
|
| Application of carboxymethyl-beta-cyclodextrin as a chiral selector in capillary electrophoresis for enantiomer separation of selected neurotransmitters. | 2001 Aug 17 |
|
| Continuous production of (R)-phenylacetylcarbinol in an enzyme-membrane reactor using a potent mutant of pyruvate decarboxylase from Zymomonas mobilis. | 2001 Aug 20 |
|
| The trouble with fat-burner pills. | 2001 Aug 27 |
|
| Successful management of venous air embolism with inotropic support. | 2001 Feb |
|
| 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 |
|
| NCAA study of substance use and abuse habits of college student-athletes. | 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 |
|
| The effect of betahistine on vestibular habituation: comparison of rotatory and sway habituation training. | 2001 Jul |
|
| Pre-filled ephedrine syringes. | 2001 Jul |
|
| It's a rave new world: rave culture and illicit drug use in the young. | 2001 Jun |
|
| Nutritional supplements as a source for positive doping cases? | 2001 Jun |
|
| Stability indicating HPTLC method for the simultaneous determination of pseudoephedrine and cetirizine in pharmaceutical formulations. | 2001 Jun |
|
| 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 |
|
| Asymmetric synthesis of beta-substituted alpha-methyl-beta-amino esters by Mannich reaction of (S,S)-(+)-pseudoephedrine acetamide derived enolate with imines. | 2001 Mar 8 |
|
| Extra-strong graduated compression stocking reduces usage of vasopressor agents during spinal anesthesia for cesarean section. | 2001 May |
|
| Linezolid: pharmacokinetic and pharmacodynamic evaluation of coadministration with pseudoephedrine HCl, phenylpropanolamine HCl, and dextromethorpan HBr. | 2001 May |
|
| Pharmacologic options available to treat symptomatic intradialytic hypotension. | 2001 Oct |
|
| High performance liquid chromatography with UV detection for the simultaneous determination of sympathomimetic amines using 4-(4,5-diphenyl-1H-imidazole-2-yl)benzoyl chloride as a label. | 2001 Oct |
|
| Time-controlled release pseudoephedrine tablets: bioavailability and in vitro/in vivo correlations. | 2001 Sep |
|
| Treatment of erectile dysfunction with sildenafil citrate (Viagra) in parkinsonism due to Parkinson's disease or multiple system atrophy with observations on orthostatic hypotension. | 2001 Sep |
|
| Rapid chiral on-chip separation with simplified amperometric detection. | 2001 Sep 14 |
|
| [Risk management by reporting critical incidents. Vitamin K and ephedrine mix-up at a birthing unit]. | 2001 Sep 24 |
|
| A history of nebulization. | 2001 Spring |
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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44149060
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13900-17-9
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TB6LCS628F
Created by
admin on Sat Dec 16 18:44:09 GMT 2023 , Edited by admin on Sat Dec 16 18:44:09 GMT 2023
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PARENT (SALT/SOLVATE)
SUBSTANCE RECORD
