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Dextromethorphan hydrobromide

ACTION AND MECHANISM

- Antitussive. Dextromethorphan is a derivative of 3-methoxy-levorphanol, an opiate alkaloid analogue of codeine, which acts at the level of the cough center, depressing it. Although their exact mechanism of action is unknown, opioids could act by inhibiting the production of tachykinins, the main neurotransmitters of C fibers, which constitute this control center.

It has an antitussive effect similar to codeine, but lacks narcotic or depressant effects on the respiratory center.

PHARMACOKINETICS

- Absorption: rapid absorption, with cmax of 5.2-5.8 ng/ml and tmax of 2 h after a 60 mg dose. Its effects appear in 15-30 min and last for 6 h. Its bioavailability is reduced due to an intense hepatic first-pass effect.

Effect of food: do not affect the pharmacokinetics of dextromethorphan.

- Distribution: its Vd is 7.3 l.

- Metabolism: extensive and rapid in the liver by CYP2D6 and CYP3A4, giving rise to several demethylated metabolites. The majority is dextrorphan, partially active, and to a lesser extent 3-methoxy and 3-hydroxy-morphinan, both inactive.

Enzyme inducing/inhibiting capacity: no data available.

- Elimination: in urine (20-86% in 48 h), in the form of free or conjugated metabolites. Minimal amounts in feces (<1%). Its t1/2 is 1.4-3.9 h (dextromethorphan) and 3.4-5.6 h (dextrorphan).

Pharmacokinetics in special situations:

- Genetic polymorphism: dextromethorphan is a substrate of CYP2D6, a cytochrome P450 isozyme for which populations with non-functional alleles have been described, which act as slow metabolizers (up to 6% of the population). These patients could see reduced elimination of dextromethorphan, with cmax and AUC up to 16 and 150 times higher, respectively, and t1/2 prolonged up to 45 h.

- Other situations: there are no specific data in children, the elderly or patients with renal or hepatic insufficiency. However, an increase in its t1/2 is to be expected in patients with liver failure.

INDICATIONS

- Symptomatic treatment of unproductive [DRY COUGH], such as irritative cough or nervous cough.

POSOLOGY

- Adults: 10-20 mg/4 h or 30 mg/6-8 h. Maximum dose 120 mg/24 h.

- Children and adolescents < 18 years:

* Adolescents from 12 years: same as adults.

* Children < 12 years: not adapted to this age.

- Elderly: does not require dose readjustment.

Duration of treatment: it is recommended to use it for the shortest time possible to control the symptoms. If symptoms continue or worsen after 7 days, or are accompanied by high fever, skin rash, or persistent headache, consult a doctor and/or pharmacist.

Forgotten dose: administer the next dose at the usual time. Do not double the next dose.

DOSAGE IN RENAL FAILURE

No specific dosage recommendations have been made. Use with caution.

DOSAGE IN LIVER FAILURE

No specific dosage recommendations have been made. Use with caution.

RULES FOR CORRECT ADMINISTRATION

Administration with food: can be taken with or without food. Avoid grapefruit juice or bitter oranges.

- Lozenges to suck: let the lozenge dissolve in the mouth, without chewing or swallowing. Once dissolved, drink a glass of water.

CONTRAINDICATIONS

- Hypersensitivity to dextromethorphan, [ALLERGY TO OPIOIDS] or any other component of the medication.

- Serious respiratory diseases such as [ASTHMA], [PRODUCTIVE COUGH], [CHRONIC OBSTRUCTIVE PULMONARY DISEASE], [PNEUMONIA], [RESPIRATORY FAILURE] or [RESPIRATORY DEPRESSION].

- Children < 2 years (see Children).

- Treatment with MAOIs, SSRIs, bupropion, linezolid, procarbazine or selegiline in the previous 2 weeks (see Interactions; enzyme inhibitors).

- Breastfeeding (see Breastfeeding).

PRECAUTIONS

- Cough. It should not be used in case of chronic cough or cough due to smoking, since it can impair expectoration and increase the resistance of the respiratory tract.

- Atopic processes. It could worsen the symptoms of diseases such as [ATOPIC DERMATITIS] or [MASTOCYTOSIS] due to the increase in the release of histamine.

- [DRUG DEPENDENCE]. Dextromethorphan can potentially give rise to dependency phenomena (cases of abuse in adolescents have been described, sometimes leading to fatal poisoning), although to a much lesser extent than other opioids such as morphine. It is recommended to take extreme precautions and monitor the patient, especially people with a history of drug addiction, in case symptoms of abuse appear, such as mood swings, changes in habits or the appearance of the person, abuse of large amounts of products for cough or disappearance of medicines from the home medicine cabinet.

- Neurological diseases. Assess the benefit/risk ratio in patients with neurological disorders associated with a decreased cough reflex, such as [Stroke], [DEMENTIA] or [PARKINSON'S DISEASE].

- Slow metabolizers. Dextromethorphan is a CYP2D6 substrate. About 10% of the general population is a poor metabolizer of this isoenzyme, with a risk of dextromethorphan accumulation and toxicity. Lower doses of dextromethorphan may be required.

- Limitations in clinical experience. Its efficacy and safety in patients with [KIDNEY FAILURE] or [HEPATIC FAILURE] have not been evaluated. Use with caution, especially in seriously ill patients.

ADVICE TO THE PATIENT

- Drink plenty of water during treatment.

- Do not take dextromethorphan if you have been treated with antidepressants in the previous 14 days. Consult your doctor and/or pharmacist.

- Warn your doctor and/or pharmacist if you develop symptoms such as persistent cough for more than 7 days despite treatment, or if it is accompanied by severe headache, fever or rash.

SPECIAL WARNINGS

- Watch for the appearance of possible symptoms of dextromethorphan abuse, such as mood swings, changes in the person's habits or appearance, or abuse of large amounts of cough products.

- Risk of serious interactions when associated with antidepressants such as MAOIs or SSRIs, as well as drugs with MAOI activity such as linezolid.

INTERACTIONS

- Expectorants and mucolytics. Inhibition of the cough reflex could lead to pulmonary obstruction in the event of increased volume or fluidity of bronchial secretions.

- Hypnotics. Risk of potentiation of the sedative effect when associated with alcohol or drugs such as barbiturates, benzodiazepines, H1 antihistamines, other opioid analgesics or antipsychotics.

- Enzyme inhibitors. Dextromethorphan is a CYP2D6 substrate, so its effects and toxicity could be increased when associated with drugs such as abiraterone, antiarrhythmics (amiodarone, flecainide), bupropion, coxibs, imatinib, or terbinafine. Reduce the dose of dextromethorphan if the association is necessary.

Avoid consumption of grapefruit juice or bitter oranges, which can inhibit CYP2D6 and 3A4.

The association of dextromethorphan with certain CYP2D6 inhibitors such as MAOIs, drugs with MAOI activity (eg linezolid, procarbazine) or SSRIs (eg paroxetine) has been associated with the development of severe serotonergic syndrome. The association is contraindicated, and these medications must be distanced for at least 14 days.

Combine with caution other serotonergic drugs such as tricyclic antidepressants.

- Memantine. Dextromethorphan could potentiate the toxicity of memantine. Avoid association.

PREGNANCY

Animal Safety : Dextromethorphan is not teratogenic in animals.

Safety in humans : Adequate and well-controlled studies in humans are not available. Based on data from retrospective studies of women who used dextromethorphan during early gestation (weeks 4-14), use of this opioid was not associated with an increased risk of birth defects, miscarriage, or low birth weight.

High doses of dextromethorphan can cause respiratory depression in newborns even if it is only given for a short time. Therefore, dextromethorphan should only be used during pregnancy after careful consideration of the benefits and risks and only in exceptional cases and under medical supervision.

Effects on fertility: No side effects have been observed in animals. No specific studies have been conducted in humans.

LACTATION

Safety in animals: no data available.

Safety in humans: it is unknown if it is excreted in milk, and the consequences it could have for the nursing infant. Given the risks of respiratory depression in infants, its use is contraindicated.

CHILDREN

Dextromethorphan could be used in children from 2 years of age, with the corresponding dosage readjustments based on age. It is recommended to select those presentations especially indicated in children between 2-12 years (see Dosage).

Children can be especially sensitive to the adverse effects of opioids.

Its use in < 2 years is contraindicated. Serious adverse reactions, some fatal, have been reported with the use of OTC flu medications in these children.

SENIORS

Although no specific dosage recommendations have been made, use with caution is advised. It may be necessary to decrease the dose per administration or increase the interval between doses.

EFFECTS ON DRIVING

Dextromethorphan does not appear to have significant central depressant effects, unlike other opioids. However, the appearance of dizziness is frequent.

ADVERSE REACTIONS

Adverse reactions are described according to each frequency interval, being considered very common (>10%), common (1-10%), uncommon (0.1-1%), rare (0.01-0.1%). , very rare (<0.01%) or frequency unknown (cannot be estimated from the available data).

- Immune system disorders: unknown frequency [HYPERSENSITIVITY REACTIONS] including [ANAPHYLAXIA], [ANGIOEDEMA], [URTICARIA], [PRURITUS], rash and [ERYTHEMA].

- Psychiatric disorders: very rare [HALLUCINATIONS], [OPIOID DEPENDENCE].

- Nervous system disorders: common [DIZZINES]; very rare [SLEEP]; unknown frequency [HEADACHE], [CONFUSION].

- Gastrointestinal disorders: frequent [NAUSEA], [VOMITING], and intestinal discomfort; frequency unknown [CONSTIPATION].

- Skin and subcutaneous tissue disorders: frequency unknown [DRUG ERUPTION].

- General disorders and alterations at the administration site: frequent [FATIGUE].

OVERDOSE

Symptoms: Adverse reactions are usually especially important in children and adolescents or in case of abuse. Among the symptoms described are nausea, vomiting and gastrointestinal disorders, dizziness, fatigue, drowsiness, hallucinations, restlessness and excitability. In more serious cases, symptoms such as decreased concentration and consciousness to the point of coma, dysphoria and euphoria, psychotic disorders such as disorientation and delusions up to confusion or paranoid states, increased muscle tone, ataxia, dysarthria, nystagmus and visual disturbances can occur. , as well as respiratory depression, changes in blood pressure and tachycardia may occur.

Finally, there is a risk of serotonergic syndrome.

Measures to take:

- Antidote: in case of severe poisoning, the administration of naloxone (0.01 mg/kg in children) could be considered.

- General elimination measures: gastric lavage with aspiration, followed by the administration of activated charcoal.

- Monitoring: respiratory and cardiovascular functionality.

- Treatment: keep the airways open, establishing assisted respiration if necessary. symptomatic treatment.

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