Methylephedrine
Methylephedrine Uses, Dosage, Side Effects, Food Interaction and all others data.
Methylephedrine is a sympathomimetic amine that appears in various over-the-counter cough and cold medications throughout the world , , . The abuse of methylephedrine-containing medications has been reported in Japan. Methylephedrine is not legally available in the United States, but has been identified in cases of drug abuse .
This drugs acts as an antitussive, bronchodilator, and adrenergic receptor agonist . It stimulates the alpha and beta adrenergic receptors, relieving cough and congestion .
As with other adrenomimetic amines, the drugs in this class are much less potent than norepinephrine itself. Members of this class of drugs increase both systolic and diastolic blood pressure, cardiac contractility, and cardiac output; in general, however, they do not increase heart rate. Bronchial smooth muscle relaxation of prolonged duration occurs, and pupils dilate .
| Trade Name | Methylephedrine |
| Generic | DL-Methylephedrine |
| DL-Methylephedrine Other Names | (+/-)-Methylephedrine, Methylephedrine, (+/-)-, Methylephedrine, DL-, N-methylephedrine DL-form |
| Type | |
| Formula | C11H17NO |
| Weight | Average: 179.263 Monoisotopic: 179.131014171 |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Used as an antitussive and decongestant .
Methylephedrine is also used to associated treatment for these conditions: Fever, Generalised muscle aches, Headache, Irritative cough, Nasal Congestion, Pain, Sinus Congestion, Sore Throat, Postnasal drip
How Methylephedrine works
The pharmacology of methylephedrine is similar to that of other members of the ephedra alkaloid class of drugs. These compounds are sympathomimetic amines because they mimic the effects of the catecholamines on the sympathetic nervous system. These alkaloids permeate the blood-brain barrier and have a direct central nervous system stimulant effect with peripheral effects; the peripheral effects are indirect and primarily mediated by norepinephrine release .
Methylephedrine expands the bronchia by relaxing the bronchial muscles .
The decrease in urination with sympathomimetic use is increased through activation of the alpha-adrenoceptors of the smooth muscles of the bladder .
Toxicity
Ld50 mouse (intraperitoneal): 185mg/kg .
Sympathomimetic drugs, such as DL-methylphedrine, can lead to an increase in catecholamines, resulting in a variety of effects , :
Nervous System/CNS/Psychiatric
Insomnia, Headaches, Seizure, Cerebrovascular Accident, Nervousness, Tremor or other motor disturbance, Psychosis with long-term, chronic use
Cardiovascular System Hypertension, Cardiac arrhythmia, Myocardial Infarction, Hypersensitivity Myocarditis
Renal System Nephrolithiasis
General Predisposition to Heat Exhaustion and Heat Stroke, Hyperglycemia, Glaucoma
The Japanese Ministry of Health made a statement in July 2017 that preparations containing this drug should not be used in children younger than 12 years old (who are highly susceptible to respiratory depression. Overseas, there have been reports that the risk of serious respiratory depression, including death, is high in children younger than 12 years old) .
Food Interaction
No interactions found.Volume of Distribution
Ephedrine: 2.5-3.0 L/kg . Methylephedrine is a derivative of ephedrine and quickly distributed throughout the body .
Elimination Route
Methylephedrine is rapidly absorbed following oral administration . Peak plasma concentrations of ephedrine (from which methylephedrine is derived) occur 2-3h after administration . Due to the fact that methylephedrine is a derivative of ephedrine , peak plasma concentrations are likely similar.
Half Life
3-6 hours (Ephedrine) .
Elimination Route
The primary compound excreted in urine is unchanged methylephedrine (33-40% of dose), followed by the metabolite methylephedrine-N-oxide (15% of dose), and approximately 8% of the dose excreted as ephedrine after 24 hours. About 70% of the dose is excreted in the urine as metabolites over 72 hours .
Alkaline urine reduces elimination to 20-35% of the dose .
Innovators Monograph
You find simplified version here Methylephedrine
