Chemical properties
Dextromethorphan, what is it? This chemical compound is an antitussive, an optical levorotatory isomer of methorphan. Despite its similarity to morphine , the drug does not have opiate effects.
Typically, the substance is found in drugs in the form of dextromethorphan hydrobromide . These are white crystals, bitter in taste, without a specific odor. Molecular weight of the compound = 370.3 grams per mole. It dissolves well in chloroform , less so in water and ether . One of the main ways to obtain Dextromethorphan is by methylation of 3-hydroxy-N-methylmorphinan .
The substance is most often used in combination with other medications as a substitute for codeine . a dissociative is also widespread . Also in medicine, the drug is used for diagnostics and treatment of seizures, alcoholism, some neurodegenerative diseases and heroin addiction. Sometimes the medicine is used to treat mental retardation in children, Parkinson's disease , lung cancer and transplantation.
Due to the fact that dextromethorphan in high dosages can have an effect similar to dissociative and psychedelic substances (similar to phencyclidine and ketamine ), it is used for recreational purposes . The substance may cause psychological dependence.
Research is also being conducted on the drug's ability to block NMDA channels in pancreatic cells and lead to blocking the increase in basal insulin . This property can be used to help patients diabetes who were previously forced to take metformin . Perhaps the drug is able to increase the intensity of insulin production without leading to negative consequences, namely hypoglycemia .
On the territory of the Russian Federation, this chemical compound is included in the 3rd list of narcotic drugs, the circulation of which is limited by the state. Most often, the medicine can be seen in cough syrups, oral capsules or tablets.
Duration
Dextromethorphan is available in the form of tablets, pills, syrups and is consumed by mouth.
Rarely, tablets are crushed and dissolved in liquid. In small doses, the drug has an antitussive effect that lasts up to 5 hours. At higher doses it causes dissociation, which lasts up to 8 hours after ingestion. In low doses (about 1.5-2.5 mg per kg of body weight), the drug has a weak stimulating effect: it enhances the pleasant sensations from music or movements. As the dose increases, a psychotropic effect similar to the use of nitrous oxide or marijuana is possible. Due to short-term memory impairments, mild hallucinations sometimes occur.
At a dose of about 7.5-15 mg per kg of body weight, hallucinations, disturbances in thinking, sensory perception of the environment and memory are possible. At doses greater than 15 mg/kg body weight, the effect is similar to a non-anesthetic dose of ketamine, which causes severe dissociation.
At a dose of 20-30 mg/kg body weight, dextromethorphan is toxic to the body - this does not mean that poisoning cannot occur even at lower doses. The drug is not a “dance drug”: the effect is incomparable to “ecstasy” in terms of euphoria and with ketamine in terms of dissociation.
Dextromethorphan is primarily used by adolescents as a recreational psychotropic drug. The most commonly used dosage at rave parties is up to 120 mg, at which euphoria, hallucinations and dissociation occur. Less commonly used is a dose of 120 mg, which is characterized by an “out-of-body” experience.
Pharmacodynamics and pharmacokinetics
Dextromethorphan hydrobromide, after penetration into the systemic bloodstream, acts directly on the cough center located in the medulla oblongata, reducing the center’s sensitivity threshold to external irritants and preventing dry cough . When used in therapeutic doses, the substance does not have analgesic , hypnotic or narcotic effects .
After oral administration, the medicine begins to act within 10 minutes to half an hour. The duration of action is from 5 to 9 hours (children). In the brain, the substance also affects the processes of serotonin and activates sigma receptors. The drug is capable of blocking N-methyl-D-aspartate channels when using dosages greater than 150 mg.
The absolute bioavailability of the product is 11%. Metabolism of the drug occurs in the liver tissues, with the participation of the cytochrome P450 (mainly CYP2D6 , less pronounced CYP3A4 and CYP3A5 ). Metabolites are removed from the blood plasma by the kidneys within 1.4 - 4 hours.
Mechanism of action
This medication was previously classified as an opiate, but is no longer classified as such. It has been proven that dextromethorphan does not bind to opioid receptors. Its mechanism of action is different than that of opioid medications.
This substance binds to NMDA receptors involved in the excitation of nerve cells. Euphoria and other pleasant sensations arise due to the fact that it blocks the reuptake of the neurotransmitters dopamine and serotonin - the so-called “happiness hormones”. This is not unique to dextromethorphan; combination medications containing it have the same effect.
Interaction
When combining the drug with MAO inhibitors ( selegiline , furazolidone , procarbazine collapse , dizziness, adrenergic crisis , increased blood pressure, agitation, nausea, intracranial bleeding, tremor and spasms, up to lethargy and coma may occur .
The simultaneous use of the drug and tricyclic antidepressants is fraught with the development of serotonin syndrome and death.
Under the influence of agents that inhibit the cytochrome P450 ( quinidine , amiodarone , fluoxetine , etc.), the concentration of Dextromethorphan in the blood may increase and the time of its action on the body may be extended.
Inhalation of tobacco smoke leads to increased secretion of the glands, which is extremely undesirable given the suppression of the cough reflex that occurs under the influence of the drug.
Long-term consequences
The drug causes predominantly mental dependence. Dizziness, high blood pressure, nausea and headache occur within two weeks of taking higher doses.
Because dextromethorphan is never sold in its pure form, overdoses cause other unpleasant and long-term effects that depend on the substances added. Like all medicines, it is not recommended to combine the substance with other medicines, as serious side effects, including death, are possible.
Drugs containing (Analogs)
Level 4 ATC code matches:
Trigamma
Riluzole
Huato Boluses
Vitagamma
Vitaxon
Hypoxene
Glycine
Mexiprim
Mexidol
Neurox
Glitsed
Cytoflavin
The substance in combination with paracetamol is part of the drugs: Padevix , Grippostad Good Knight , Fervex for dry cough (+ ascorbic acid ), Grippex (+ pseudoephedrine ).
In combination with chlorphenamine , paracetamol and pseudoephedrine, the drug is found in the following medications: Tylenol for colds, Tylenol for children for colds, Mulsinex .
Dextromethorphan is also included in Toff Plus (+ paracetamol + chlorphenamine + phenylephrine Glycodin syrup (+ levomenthol + terpinhydrate ), Alex Plus , Caffetin Cold , Terasil-D , Tussin Plus ( guaifenesin ).
Dextromethorphan: what medications it contains, how it works
If it is used in a therapeutic dosage, then the following are observed:
- cough suppression;
- mild sedation (calming effect).
When using the product, coughing urges of any origin are stopped. This occurs due to the fact that it inhibits the functioning of the cough center. The effect when taking an average therapeutic dose is observed for about 5 hours. A similar effect is exhibited by drugs containing dextromethorphan - those that contain paracetamol, terpin hydrate, levomenthol and some others.
The drug does not have a direct hypnotic effect, but its use can improve sleep if it has been disturbed due to emotional arousal, stress and the like. The product also has an obstipating effect: it helps to bind feces in the large intestine, preventing the occurrence of diarrhea (diarrhea). But it is not used as an antiperspirant.
Dextromethorphan: effects
Psychedelic phenomena occur at dosages that exceed the therapeutic level. Moreover, they are caused not by the described substance itself, but by its metabolite dextrophan.
The main signs of drug intoxication are:
- drowsiness;
- dizziness;
- disorientation in time;
- hallucinations.
Please note: Addicts take this drug for the sake of “separation” into a certain spiritual substance and a physical body, which it “leaves” when consuming a large amount of the psychotropic. The sensations are similar to those described by patients who have experienced clinical death. There is no fear - curiosity and a desire to experiment with phenomena that do not normally exist arise. This is how dextromethorphan works, no matter what medicine it is in.
The psychotropic phenomena that develop when using the described substance are similar to those that appear when taken in small quantities:
- hallucinogenic drug LSD;
- ketamine.
Dextromethorphan is a drug that can cause addiction and overdose.
Mental dependence means that a person, having used this drug and felt positive emotions, wants to repeat the pleasant experience. But physical cravings were not noticed among drug addicts. Since it does not develop, there is no withdrawal associated with it (syndrome o) - a deterioration in the condition upon abrupt cessation of taking this psychotropic.
An overdose may occur. Its main reasons are:
- juvenile drug addicts do not know how to correctly calculate the dose that, on the one hand, would cause a psychedelic effect, and on the other, would not provoke violations;
- Over time, addicts want to experience more intense euphoria.
In case of overdose, concern:
- anxiety;
- irritability;
- hallucinations.
Breathing disturbances may also be observed (it becomes more superficial, the frequency of respiratory acts decreases), and increased heart rate. The addict develops nystagmus (involuntary oscillatory movements of the eyeballs), and there is a “fog” before the eyes. Pain in the abdominal cavity, manifested as intestinal colic, is often disturbing. It’s not just dextromethorphan that acts this way—drugs that contain it cause the same clinical symptoms.
