(+/-)-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 .

(+/-)-Methylephedrine
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

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 .