Dextromethorphan

Декстрометорфан Constitutional formula

The description is actual on 09.02.2016

  • Latin name: Dextromethorphanum
  • ATH code: N07XX59, R05DA09, R05DA59
  • Chemical formula: C18H25NO
  • CAS code: 125-71-3

Chemical name

(+)-3-метокси-17-метил-(9α,13α,14α)-морфинан

Chemical properties

Dextromethorphan, what is it? This chemical compound represents an antibechic, optical left-handed isomer of a metorfan. Despite the similarity to morphine, means has no opiate effects.

Usually as a part of medicines substance is in a type of dextromethorphan of hydrobromide. These are white crystals, bitter on taste, not possessing a specific smell. The molecular mass of connection = 370,3 grams on mol. It is well dissolved in chloroform, it is worse – in water and ether. One of the main ways of receiving Dextromethorphan is methylation 3-oxy-N-metilmorfinana.

Substance is used most often in a combination with other drugs as codeine replacement. The recreational use of drug as a dissotsiativ is also eurysynusic. Also in medicine means is used for carrying out diagnosis, treatment of attacks, alcoholism, some neurodegenerative diseases and dependence on heroin. Sometimes medicine is applied to treatment of a delay of intellectual development in children, by Parkinson's diseases, at lung cancer and transplantation.

Because Dextromethorphan in high dosages can have the effect similar to dissociative and psychodelic substances (similar to phencyclidine and Ketaminum) it apply in the recreational purposes. Substance can cause psychological dependence.

Also researches of ability of medicine to block NMDA channels in cells of a pancreas and to lead to blocking of growth of basal level of insulin are conducted. This property can be used to help a sick diabetes mellitus 2 types which were forced to accept Metforminum earlier. Perhaps, drug is capable to increase intensity of production of insulin, without leading to negative effects, namely – a hypoglycemia.

In the territory of the Russian Federation this chemical compound is included into the list of the 3rd list of drugs which turnover is limited to the state. Most often medicine can be seen as a part of cough syrups, capsules for intake or tablets.

Pharmacological action

Suppresses activity of the tussive center.

Pharmacodynamics and pharmacokinetics

Dextromethorphan hydrobromide after penetration into a system blood stream influences directly the tussive center located in a myelencephalon, reducing a threshold of sensitivity of the center to external irritants and preventing dry cough. When using substance in therapeutic doses, it has no analgeziruyushchy, somnolent or narcotic effects.

After intake medicine begins to work within 10 minutes – half an hour. Duration of action makes from 5 to 9 hours (children). In a head brain substance also exerts impact on processes of the return serotonin reuptake and the sigma activates receptors. Means is capable to block N-methyl-D-aspartate channels when using dosages more than 150 mg.

Absolute biological availability of means makes 11%. The metabolism of medicine proceeds in liver tissues, with participation of system of P450 cytochrome (in the main CYP2D6, it is less expressed to CYP3A4 and CYP3A5). Metabolites are brought out of a blood plasma by means of kidneys within 1,4 — 4 hours.

Indications to use

Dextromethorphan is appointed for treatment of dry cough of various origin in combination with other anti-cold and antibechic drugs.

Contraindications

Medicine is contraindicated:

It is recommended to be careful at a liver failure, to pregnant women in the first 3 months.

Side effects

Usually when using therapeutic dosages of medicine side effects are not shown. Nevertheless, depending on specific features of the patient can be shown: nausea, weakness, drowsiness and dizziness.

Dextromethorphan, application instruction (Way and dosage)

Depending on a dosage form and disease severity drug can be appointed in various dosage.

As a rule, for adults and children of 12 flyings a daily dosage = 60 mg. Medicine is distributed on 4 receptions a day. Correction of a dosage is necessary for children of 6 flyings (30 mg a day on 7,5 mg at one time).

Overdose

Depending on the accepted dose various side reactions can be shown. Are observed: drowsiness or strong psychomotor excitement, ataxy, tachycardia, lowering of arterial pressure, hallucinations, involuntary movements by muscles, nausea.

As treatment it is shown: IVL, symptomatic therapy, introduction of Naloxonum as an antidote.

Interaction

At a drug combination to MAO inhibitors (selegiliny, the collapse, dizziness, adrenergic crisis, growth of arterial pressure, excitement, nausea, bleedings intracranial, a tremor and spasms, up to a lethargy and a coma can arise furasolidone, Procarbazinum).

The concomitant use of means and tricyclic antidepressants is fraught with development of a serotoninovy syndrome and a lethal outcome.

Under the influence of the means inhibiting system of P450 cytochrome (quinidine, Amiodaronum, fluoxetine, etc.) concentration of Dextromethorphan in blood can increase, be extended time of its action for an organism.

Inhalation of a tobacco smoke leads to increase of secretion of glands that is extremely undesirable against oppression of the tussive reflex occurring under the influence of drug.

Terms of sale

According to the recipe.

Storage conditions

Storage conditions are standard, usually depend on a dosage form and the producer.

To children

Children can appoint substance of 6 flyings. At such age it is necessary to correct a drug dosage. For children of 12 flyings the adult dosage is used.

At pregnancy and a lactation

Women need to observe extra care in 1 trimester of pregnancy.

Drugs in which contains (Analogues)

Substance in a combination with paracetamol is a part of drugs: Padeviks, Grippostad Goode Knight, Ferveks for dry cough (+ ascorbic acid), Grippeks (+ pseudoephedrine).

In combination with chlorphenaminum, paracetamol and pseudoephedrine means is in drugs: Taylenol for cold, Taylenol children's for cold, Mulsineks.

Also Dextromethorphan is a part of capsules Toff plus (+ paracetamol + chlorphenaminum + Phenylephrinum), syrup Glikodin (+ left menthol + terpin hydrate), Alex Plus, Kaffetin Kold, Terasil-D, Tussin Plus (gvayfenezin).

Section: Active ingredients
PAY ATTENTION! Information on active ingredients on the website is help generalizing, collected from public sources and can form the basis for making decision on use of these substances it is not aware of treatment. Before substance Dextromethorphan use surely consult with the attending physician.