Ethylmorphine Stats - Substance Search

Pharmacology

DrugBank

State Solid

Description

A narcotic analgesic and antitussive. It is metabolized in the liver by ethylmorphine-N-demethylase and used as an indicator of liver function. It is not marketed in the US but is approved for use in various countries around the world. In the US it is a schedule II drug (single-entity) and schedule III drug (in combination products).

Mechanism of Action

Ethylmorphine is metabolized by the liver enzyme cytochrome P450 2D6 to morphine. The precise mechanism of the analgesic action of morphine is unknown. However, specific CNS opiate receptors have been identified and likely play a role in the expression of analgesic effects. Morphine first acts on the mu-opioid receptors. The mechanism of respiratory depression involves a reduction in the responsiveness of the brain stem respiratory centers to increases in carbon dioxide tension and to electrical stimulation. It has been shown that morphine binds to and inhibits GABA inhibitory interneurons. These interneurons normally inhibit the descending pain inhibition pathway. So, without the inhibitory signals, pain modulation can proceed downstream.

Pharmacodynamics

Ethylmorphine is metabolized by the enzyme cytochrome P450 2D6 to morphine. Morphine is a narcotic pain management agent indicated for the relief of pain in patients who require opioid analgesics for more than a few days. Morphine interacts predominantly with the opioid mu-receptor. These mu-binding sites are discretely distributed in the human brain, with high densities in the posterior amygdala, hypothalamus, thalamus, nucleus caudatus, putamen, and certain cortical areas. They are also found on the terminal axons of primary afferents within laminae I and II (substantia gelatinosa) of the spinal cord and in the spinal nucleus of the trigeminal nerve. In clinical settings, morphine exerts its principal pharmacological effect on the central nervous system and gastrointestinal tract. Its primary actions of therapeutic value are analgesia and sedation. Morphine appears to increase the patient's tolerance for pain and to decrease discomfort, although the presence of the pain itself may still be recognized. In addition to analgesia, alterations in mood, euphoria and dysphoria, and drowsiness commonly occur. Opioids also produce respiratory depression by direct action on brain stem respiratory centers.

Metabolism

After ingestion, ethylmorphine is converted to morphine in the human liver by the CYP450-isozyme CYP2D6, similarly to codeine.

Indication

Ethylmorphine is an analgesic used for pain relief.

Receptor Profile

Receptor Actions

Agonists

μ-opioid receptor agonist (via active metabolite morphine)

Other

metabolized by CYP2D6 to morphine and CYP3A4 to norethylmorphine

History & Culture

Ethylmorphine is a semi-synthetic opioid first synthesized by the pharmaceutical company Merck in 1884. It was developed as a weaker alternative to morphine for therapeutic applications. By the early twentieth century, the compound had found a specialized role in ophthalmic medicine under the trade name Dionine, employed to treat inflammatory conditions of the eye. A 1904 publication described an ethylmorphine preparation as "a new ocular analgesic," establishing its early medical utility in this specialized application. Commercial marketing of ethylmorphine began in France in 1953 through the pharmaceutical company Houde, with subsequent introduction to Norwegian and Spanish markets in 1960. The substance has since evolved to become primarily used as an antitussive agent, available in various cough preparation formulations across certain European countries, including syrups such as Cocillana, Cosylan, and Solvipect comp., as well as tablet formulations like Tussipax.

Subjective Effect Notes

physical: The cognitive effects of ethylmorphine can be broken down into several components which progressively intensify proportional to dosage. The general head space of codeine is described by many as one of intense euphoria, relaxation, anxiety suppression and pain relief.

cognitive: The physical effects of ethylmorphine can be broken down into several components which progressively intensify proportional to dosage.

Effect Profile

Curated + 4 Reports

Opioid 7.6

Strong euphoria and pain relief with moderate itching/nausea, mild sedation

Euphoria / Warmth×3

10

Analgesia×2

8

Sedation / Relaxation×1

4

Itching / Nausea×1

7

Based on reports from:

Erowid Experience Reports PsychonautWiki Ethylmorphine

Tolerance & Pharmacokinetics

drugs.wiki

Tolerance Decay

Full tolerance 1d Half tolerance 21d Baseline ~35d

Experience Report Analysis

Erowid

4 Reports

2004–2019 Date Range

3 With Age Data

1 Effects Detected

Demographics

Gender Distribution

Age Distribution

Reports Over Time

Effect Analysis

Erowid

Effects aggregated from 4 experience reports (4 Erowid)

4 Reports

1 Effects Detected

1 Positive

0 Adverse

0 Neutral

Effect Sentiment Distribution

Confidence Distribution

Positive Effects 1

Euphoria 100.0% 70%

Adverse Effects 0

Form / Preparation

Most common forms and preparations reported

Legal Status

Single Convention on Narcotic Drugs 1961 (Schedule III)

Country	Status	Notes
France	Available over-the-counter (in certain preparations)	Preparations combining ethylmorphine (10mg) with codeine (10mg), such as Tussipax tablets, are reportedly available without prescription.
Germany	Anlage II BtMG	Controlled under Anlage II of the Betäubungsmittelgesetz. Manufacturing, importing, possessing, selling, or transferring without license is prohibited. An exception exists for preparations containing up to 2.5% or 100mg per unit, which may be prescribed using narcotic prescription forms.
Norway	Prescription Class B	Cough syrups containing ethylmorphine (such as Cosylan at 1.7mg/mL and Solvipect comp. at 2.5mg/mL) are available by prescription and commonly used for dry cough treatment.
Russia	Schedule II	Classified as a Schedule II controlled substance under Russian drug control legislation.
Sweden	Prescription drug	Available as a prescription medication. Cough preparations containing ethylmorphine (e.g., Cocillana-Etyfin at 2.5mg/mL and Lepheton combination products) require a prescription.
Switzerland	Verzeichnis A (controlled)	Specifically listed as a controlled substance under Verzeichnis A. Medical use is permitted. Certain preparations fall under Verzeichnis C, with some exceptions.
United Kingdom	Class B	Controlled under the Misuse of Drugs Act 1971 as a Class B substance, the same classification as codeine. However, unlike codeine, no legal pharmaceutical preparations containing ethylmorphine are currently available.
United States	Schedule II/III/V (varies by preparation)	Pure ethylmorphine is Schedule II. Combination products containing no more than 3mg/mL (or 15mg per dosage unit with non-narcotic ingredients) are Schedule III. Preparations with 1mg/mL or less are Schedule V. Despite this scheduling structure paralleling codeine, no ethylmorphine preparations are currently marketed for medical use.

Ethylmorphine Stats & Data