- Raw materials
- Alkalinizing agents
- DL-Methylephedrine
DL-Methylephedrine API Manufacturers & Suppliers
0 verified results
Take control of your API sourcing
Submit a Special Inquiry and have Pharmaoffer activate verified suppliers.
Commercial-scale Suppliers
No suppliers found
Sorry, there are currently no suppliers listed for this ingredient. Hopefully we can help you with other ingredients.
Notify me!
Want to be the first to find out when a supplier for DL-Methylephedrine is listed?
Join our notification list by following this page.
Join our notification list by following this page.
List your company
Are you a supplier of DL-Methylephedrine or other APIs and are you looking to list your company on Pharmaoffer?
Click the button below to find out more
Click the button below to find out more
Find CDMO
Looking for a CDMO/CMO that can help you with your pharmaceutical needs?
Click the button below to switch over to the contract services area of Pharmaoffer.
Click the button below to switch over to the contract services area of Pharmaoffer.
When insight is your advantage
Full data, full access, full negotiation power
Total market transparency
|
Supplier trade data access
|
Buyer / supplier flow comparison
Trusted by 30,000+ registered pharma professionals:
Reach multinationals, SMEs, compounding pharmacies & more!
DL-Methylephedrine | CAS No: 1201-56-5 | GMP-certified suppliers
A medication that serves as an antitussive and nasal decongestant, providing relief in respiratory conditions by reducing cough and nasal congestion.
Therapeutic categories
Adrenergic AgonistsAdrenergic alpha-2 Receptor AgonistsAdrenergic alpha-AgonistsAgents producing tachycardiaAgents that produce hypertensionAlcohols
Generic name
DL-Methylephedrine
Molecule type
small molecule
CAS number
1201-56-5
DrugBank ID
DB11278
Approval status
Approved drug
Primary indications
- Used as an antitussive and decongestant
Product Snapshot
- DL-Methylephedrine is available as oral capsules and liquid formulations for systemic administration
- It is primarily utilized as an antitussive and nasal decongestant agent
- This API is approved for use in the US market
Clinical Overview
DL-Methylephedrine (CAS Number 1201-56-5) is a sympathomimetic amine belonging to the phenylpropane chemical class. It is used primarily as an antitussive and nasal decongestant in various over-the-counter cough and cold remedies worldwide. The compound acts as an adrenergic receptor agonist with pharmacological properties including bronchodilation and central nervous system stimulation.
Pharmacodynamically, DL-Methylephedrine activates both alpha and beta adrenergic receptors. This dual stimulation contributes to its antitussive effects by reducing cough reflex sensitivity and to decongestant effects through vasoconstriction of nasal mucosa. Like other adrenergic amines, it increases systolic and diastolic blood pressure as well as cardiac contractility and output, though heart rate is not typically elevated. Bronchial smooth muscle relaxation is sustained post-administration, facilitating airway expansion. Pupil dilation has also been observed.
The mechanism of action involves mimicking endogenous catecholamines to stimulate the sympathetic nervous system. DL-Methylephedrine is capable of crossing the blood-brain barrier, inducing central stimulation. Its peripheral effects are largely indirect, resulting from norepinephrine release which leads to smooth muscle relaxation in bronchi and contraction of bladder smooth muscle via alpha-adrenoceptors, the latter potentially decreasing urinary output.
Pharmacokinetic and excretion data indicate renal elimination as the primary pathway, consistent with its classification as a drug mainly renally excreted.
Safety concerns primarily arise from its sympathomimetic profile, including potential cardiovascular effects such as increased blood pressure and cardiac workload. Cases of abuse involving methylephedrine-containing products have been documented, notably in Japan. It is not legally marketed in the United States but has appeared in investigations related to drug misuse.
From an API sourcing perspective, quality control should emphasize purity and compliance with regulatory standards due to its pharmacological potency and abuse potential. Reliable suppliers must validate consistent assay, impurity profiling, and adherence to pharmacopeial standards. Documentation supporting legal status and controlled substance monitoring is recommended given its variable regulatory approval internationally.
Pharmacodynamically, DL-Methylephedrine activates both alpha and beta adrenergic receptors. This dual stimulation contributes to its antitussive effects by reducing cough reflex sensitivity and to decongestant effects through vasoconstriction of nasal mucosa. Like other adrenergic amines, it increases systolic and diastolic blood pressure as well as cardiac contractility and output, though heart rate is not typically elevated. Bronchial smooth muscle relaxation is sustained post-administration, facilitating airway expansion. Pupil dilation has also been observed.
The mechanism of action involves mimicking endogenous catecholamines to stimulate the sympathetic nervous system. DL-Methylephedrine is capable of crossing the blood-brain barrier, inducing central stimulation. Its peripheral effects are largely indirect, resulting from norepinephrine release which leads to smooth muscle relaxation in bronchi and contraction of bladder smooth muscle via alpha-adrenoceptors, the latter potentially decreasing urinary output.
Pharmacokinetic and excretion data indicate renal elimination as the primary pathway, consistent with its classification as a drug mainly renally excreted.
Safety concerns primarily arise from its sympathomimetic profile, including potential cardiovascular effects such as increased blood pressure and cardiac workload. Cases of abuse involving methylephedrine-containing products have been documented, notably in Japan. It is not legally marketed in the United States but has appeared in investigations related to drug misuse.
From an API sourcing perspective, quality control should emphasize purity and compliance with regulatory standards due to its pharmacological potency and abuse potential. Reliable suppliers must validate consistent assay, impurity profiling, and adherence to pharmacopeial standards. Documentation supporting legal status and controlled substance monitoring is recommended given its variable regulatory approval internationally.
Identification & chemistry
| Generic name | DL-Methylephedrine |
|---|---|
| Molecule type | Small molecule |
| CAS | 1201-56-5 |
| UNII | SHS9PGQ2LS |
| DrugBank ID | DB11278 |
Pharmacology
| Summary | Methylephedrine is a sympathomimetic agent that acts primarily as an agonist at alpha and beta adrenergic receptors, resulting in bronchodilation and central nervous system stimulation. Its pharmacodynamic effects include relaxation of bronchial smooth muscle, alpha-adrenoceptor–mediated reduction of bladder smooth muscle activity, and modulation of cardiovascular parameters such as increased blood pressure and cardiac contractility without a significant increase in heart rate. Therapeutically, it is utilized for its antitussive and decongestant properties. |
|---|---|
| Mechanism of action | 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 . |
| Pharmacodynamics | 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 . |
Targets
| Target | Organism | Actions |
|---|---|---|
| Beta-1 adrenergic receptor | Humans | agonist |
| Alpha-2A adrenergic receptor | Humans | agonist |
| Alpha adrenergic receptor | Humans | agonist |
ADME / PK
| Absorption | 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) . |
| Metabolism | Methylephedrine is metabolized to give ephedrine and norephedrine . |
| Route of elimination | 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 . |
| Volume of distribution | Ephedrine: 2.5-3.0 L/kg . Methylephedrine is a derivative of ephedrine and quickly distributed throughout the body . |
Formulation & handling
- DL-Methylephedrine is a small molecule suitable for oral administration in capsule or liquid form.
- It exhibits moderate water solubility and a logP of 1.7, indicating balanced lipophilicity for oral absorption.
- As a small molecule phenylpropane derivative, it requires standard handling without special peptide or biologic stability considerations.
Regulatory status
| Lifecycle | The API's primary patent protection in the US has expired, allowing for generic competition and established market presence with multiple approved products. Market activity now focuses on lifecycle management and potential formulation improvements. |
|---|
| Markets | US |
|---|
Supply Chain
| Supply chain summary | The manufacturing landscape for DL-Methylephedrine involves multiple originator companies producing branded products primarily marketed in the US. The presence of several branded formulations indicates established market penetration, while patent expirations in this segment suggest existing generic competition in the marketplace. |
|---|
Safety
| 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) . |
|---|
High Level Warnings:
- Acute toxicity: LD50 in mice (intraperitoneal) is 185 mg/kg
- Potential central nervous system effects include seizures, psychosis, and cerebrovascular events with chronic exposure
- Cardiovascular risks encompass hypertension, arrhythmias, and myocarditis
DL-Methylephedrine is a type of Alkalinizing agents
Alkalinizing agents, a pharmaceutical API category, refers to a group of substances used to increase the pH (alkalinity) of a solution or body fluid. These agents play a crucial role in various medical applications, such as the treatment of acidosis, kidney disorders, and certain drug overdoses.
One commonly used alkalinizing agent is sodium bicarbonate, which is highly effective in raising the pH of blood and urine. It works by neutralizing excess acid and restoring the acid-base balance in the body. Sodium bicarbonate is often administered intravenously in emergency situations to rapidly correct severe acidosis.
Another alkalinizing agent, acetazolamide, is frequently employed in the treatment of glaucoma and certain types of epilepsy. By inhibiting carbonic anhydrase, acetazolamide reduces the production of bicarbonate ions, leading to a systemic decrease in pH. This mechanism is particularly useful in lowering the intraocular pressure associated with glaucoma.
Alkalinizing agents are also utilized in the management of certain drug toxicities. For instance, methotrexate, a chemotherapy medication, can cause severe toxicity if its elimination is hindered. Alkalinizing the urine with agents like sodium bicarbonate enhances methotrexate solubility, preventing the formation of toxic crystals in the kidneys.
In conclusion, alkalinizing agents are indispensable pharmaceutical APIs that help correct acid-base imbalances, treat specific medical conditions, and mitigate drug toxicities. Their diverse applications make them valuable tools in modern medicine.
