Corvalol

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT CORVALOL® (Corvalol®)

Composition:

Active substances: ethyl ether of α-bromoisovaleric acid, phenobarbital, peppermint oil;

1 tablet contains ethyl ether of α-bromoisovaleric acid, calculated as 100% substance – 12.42 mg, phenobarbital calculated as 100% dry substance – 11.34 mg, peppermint oil – 0.88 mg;

Excipients: lactose monohydrate, magnesium stearate, β-cyclodextrin, potassium acesulfame.

Pharmaceutical form. Tablets.

Main physicochemical properties: white tablets with a biconvex surface.

Pharmacotherapeutic group.

Sedatives and hypnotics. Barbiturates in combination with other components.

ATC code N05C B02.

Pharmacological properties.

Pharmacodynamics.

Corvalol® is a sedative and spasmolytic agent, whose effects are determined by its constituent components.

The ethyl ether of α-bromoisovaleric acid exerts a reflex sedative and spasmolytic effect caused by stimulation primarily of oral and nasopharyngeal receptors, reduction of reflex excitability in central nervous system centers, enhancement of inhibitory processes in cortical and subcortical neurons of the brain, as well as reduction of activity in central vasomotor centers and direct local spasmolytic action on vascular smooth muscle.

Phenobarbital suppresses activating influences from the reticular formation centers of the midbrain and medulla oblongata on the cerebral cortex, thereby reducing excitatory impulses to the cerebral cortex and subcortical structures. Reduction of activating influences results in sedative, tranquilizing, or hypnotic effects, depending on the dose. Corvalol® reduces excitatory influences on vasomotor centers and on coronary and peripheral blood vessels, thereby lowering overall arterial pressure, relieving, and preventing vascular spasms, especially in the heart.

Peppermint oil contains a large amount of essential oils, including approximately 50% menthol and 4–9% menthol esters. These components can stimulate oral "cold" receptors and reflexively dilate primarily coronary and cerebral blood vessels, relieve spasms of smooth muscle, and produce sedative and mild cholagogue effects. Peppermint oil exerts antiseptic and spasmolytic actions and is capable of reducing symptoms of meteorism.

Pharmacokinetics.

When administered sublingually, absorption begins in the sublingual area, and bioavailability of active substances is high (approximately 60–80%). Effects appear rapidly (within 5–10 minutes). When administered orally, onset of action occurs within 15–45 minutes and lasts for 3–6 hours. In patients previously treated with barbituric acid derivatives, duration of action is reduced due to accelerated hepatic metabolism of phenobarbital, as barbiturates induce liver enzymes. In elderly patients and in patients with liver cirrhosis, Corvalol® metabolism is reduced, resulting in prolonged elimination half-life, which necessitates dose reduction and prolonged dosing intervals.

Clinical characteristics.

Indications.

• Neuroses with increased irritability;
• insomnia;
• as part of combination therapy for hypertension and vegetative-vascular dystonia;
• mild spasms of coronary vessels, tachycardia;
• intestinal spasms caused by neurovegetative disorders (as a spasmolytic agent).

Contraindications.

• Hypersensitivity to the components of the drug, bromine;
• severe impairment of liver and/or kidney function;
• hepatic porphyria;
• severe heart failure;
• pronounced arterial hypotension;
• acute myocardial infarction;
• diabetes mellitus;
• depression;
• myasthenia gravis;
• alcoholism;
• drug or medication dependence;
• respiratory diseases with dyspnea and obstructive syndrome.

Interaction with other medicinal products and other types of interactions.

Central nervous system depressants enhance the effect of Corvalol®.

The presence of phenobarbital in the formulation may induce liver enzymes and thus accelerate the metabolism of certain drugs metabolized by these enzymes (including indirect anticoagulants, cardiac glycosides, antimicrobial, antiviral, antifungal, antiepileptic, anticonvulsant, psychotropic, oral hypoglycemic, hormonal, immunosuppressive, cytostatic, antiarrhythmic, antihypertensive agents, griseofulvin, glucocorticoids, oral contraceptives), resulting in reduced efficacy due to increased metabolic rate.

Corvalol® enhances the effect of analgesics, local anesthetics, and other agents that depress the central nervous system.

MAO inhibitors prolong the effect of phenobarbital. Rifampicin may reduce the effect of phenobarbital.

Concomitant use of phenobarbital with gold-containing preparations increases the risk of kidney damage.

Long-term concomitant use of phenobarbital with nonsteroidal anti-inflammatory drugs increases the risk of gastric ulceration and bleeding.

Simultaneous use of phenobarbital and zidovudine enhances the toxicity of both agents.

Concomitant use with valproic acid enhances its effect.

Concomitant use with methotrexate increases the latter's toxicity.

Alcohol enhances the effect of the drug and also increases its toxicity. Consumption of alcoholic beverages should be avoided during treatment.

Special precautions for use.

The risk of developing Stevens-Johnson syndrome and Lyell's syndrome is highest during the first weeks of treatment. Prolonged use is not recommended due to the danger of developing drug dependence, possible accumulation of bromine in the body, and bromine poisoning. In cases where chest pain does not resolve after taking the medication, medical advice must be sought to rule out acute coronary syndrome. The drug should be prescribed with caution in patients with hyperkinesia, hyperthyroidism, adrenal insufficiency, decompensated heart failure, acute and persistent pain, and acute intoxication with medicinal products.

Concomitant use of alcoholic beverages should be avoided.

The drug should be prescribed cautiously in patients with arterial hypotension.

The product contains lactose monohydrate; therefore, if you have been diagnosed with intolerance to certain sugars, consult your doctor before taking this medication.

Use during pregnancy or breastfeeding.

Do not use during pregnancy and while breastfeeding.

Ability to influence reaction rate when driving or operating machinery.

This medication should not be taken by individuals who operate machinery, drivers, or others whose activities require high attention and quick reactions.

Dosage and Administration.

Corvalol® is administered sublingually (under the tongue) or orally to adults, 1 tablet 2–3 times daily.

If necessary (pronounced tachycardia and coronary vessel spasm), the single dose may be increased to 3 tablets.

The duration of treatment is determined by the physician depending on the clinical response and tolerability of the drug.

Children.

There is no experience with the use of the drug for the treatment of children.

Overdose.

Overdose is possible with frequent or prolonged use of the drug, associated with accumulation of its components. Long-term and continuous use may lead to dependence, withdrawal syndrome, psychomotor agitation. Sudden discontinuation of the drug may cause withdrawal syndrome.

Overdose symptoms: respiratory depression, up to respiratory arrest; central nervous system depression, confusion, dizziness, ataxia, drowsiness, up to coma; cardiovascular depression, including arrhythmias, tachycardia, decreased arterial blood pressure, up to collapse; nausea, weakness, decreased body temperature, reduced diuresis.

Treatment: symptomatic.

Adverse reactions.

Corvalolum® is generally well tolerated. In individual cases, the following adverse effects may occur:

Gastrointestinal tract: constipation, feeling of heaviness in the epigastric region, with prolonged use – liver function disturbances, nausea, discomfort in the stomach and intestine;

Nervous system: weakness, ataxia, impaired motor coordination, nystagmus, hallucinations, paradoxical excitement, decreased attention concentration, fatigue, slowed reaction time, headache, cognitive disorders, confusion, drowsiness, mild dizziness;

Hematopoietic system: anemia, thrombocytopenia, agranulocytosis;

Immune system: hypersensitivity reactions, including angioneurotic edema;

Cardiovascular system: arterial hypotension, bradycardia; slowed heart rate;

Skin and mucous membranes: allergic reactions, including skin rash, pruritus, urticaria, Stevens-Johnson syndrome, toxic epidermal necrolysis;

Other: dyspnea.

Prolonged use of drugs containing bromide may lead to bromism, characterized by the following symptoms: central nervous system depression, depressed mood, depression, confusion, ataxia, apathy, conjunctivitis, rhinitis, lacrimation, acne, or purpura.

Shelf life.

2 years.

Do not use the medication after the expiry date stated on the package.

Storage conditions.

Store in a place protected from light at a temperature not exceeding 25 °C. Keep out of reach of children.

Packaging. 10 tablets per blister. 1, 3, or 5 blisters per carton.

Availability. Over-the-counter.

Manufacturer.

JSC "Farmak".

Manufacturer's address.

74, Kyrylivska Street, Kyiv, 04080, Ukraine.