Corvalol

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Corvalol

Corvalol (Корвалол, Corvalolum, Korvalol) is a mild tranquilizer based on valerian (herb) root and phenobarbital, popular in Eastern Europe and the former Soviet Union as a heart medication. It is available as a transparent liquid with a characteristic strong aroma, and as white bi-concave scored tablets. While not available for sale in the Western countries, Corvalol is sometimes brought over from Eastern Europe for self-administration to other countries of residence. Corvalol contains documented amounts of psychoactive chemicals, and may interact with other prescription medications that a person is taking.[1]

Medical uses[edit]

Corvalol is labeled by the manufacturer for use in

  • Neuroses with heightened irritability
  • Insomnia
  • As a part of complex treatment of hypertension
  • Non-acute spasm of coronary vessels
  • Tachycardia
  • Gastrointestinal cramping (as a spasmolytic agent)

Valerian Extract[edit]

Valerian (herb) extract (a component of corvalol) has been historically used for insomnia and conditions associated with anxiety. It has also been used for mood disorders such as depression, infantile convulsions, mild tremors, epilepsy, attention deficit-hyperactivity disorder (ADHD), and chronic fatigue syndrome (CFS). Additional historical uses include to help alleviate muscle and joint pain, nervous asthma, hysterical states, excitability, hypochondria, headaches, migraine, menstrual cramps and symptoms associated with menopause, including hot flashes and anxiety. However, few of these indications are supported by clinical trials in humans.[2] Taking a combination product containing valerian extract plus hops extract has been shown to modestly improve subjective sleep measures including subjective sleep latency compared to placebo after 28 days of treatment.[3] There is evidence in limited animal trials that valerian root may reduce coronary vessel spasm, such as one that may occur in an attack of vasospastic angina or angina pectoris. The same study demonstrated that valerian may reduce bronchospasm in animals after administration of bronchospastic agents. These studies justify the traditional use of this plant in the treatment of some respiratory and cardiovascular disorders.

Phenobarbital[edit]

Phenobarbital is a barbiturate anticonvulsant used in epilepsy and to induce sedation. Currently there is no evidence to support the use of phenobarbital in cardiovascular or bronchospastic disease states.

Safety[edit]

Due to lack of scientific evidence supported by randomized clinical trials in humans, Corvalol and its components should be used with caution in patients with serious cardiovascular conditions, such as hypertension, angina, or respiratory conditions such as asthma. Prescription medications that have been scientifically proved to be effective in these disease states should be preferred due to evidence supporting their clinical use.

According to the American Geriatrics Society, phenobarbital should not be used in the elderly population due to high rate of physical dependence, tolerance to sleep benefits, and the risk of overdose at low dosages.[4]

According to the manufacturer, overdose is possible due to accumulation of the ingredients when Corvalol is used frequently and in large doses. Symptoms of overdose include central nervous system depression, confusion, dizziness, ataxia, and somnolence. In serious cases overdose may result in breathing depression, tachycardia, arrhythmia, hypotension (low blood pressure), cardiovascular collapse, and coma.

Drug interactions[edit]

Phenobarbital is a strong inducer (activator) of several hepatic cytochrome P450 enzymes, including CYP1A2, CYP2C9, CYP3A4 and others.[5] One of the functions of these enzymes is to change the molecular structure of medications and other substances taken in by the human body. Taking phenobarbital-containing products, such as Corvalol, while taking other medications may reduce their effectiveness. Some of the medications that may have decreased effectiveness when used with Corvalol are apixaban, rivaroxaban, clozapine, itraconazole, nifedipine, biologics, and many others. Corvalol may increase CNS depressant effect of other sedatives and hypnotics.

Pharmaceutical category[edit]

Corvalol belongs to the sedative-hypnotic category.[6] Valerianate component of the preparation is purported to offer mild spasmolytic effects on the vasculature. Phenobarbital is a central nervous system depressant.

Composition[edit]

Ethyl ester of α-bromoisovaleric acid

According to the Farmak product label of Colvalol oral solution, the composition per 1 mL (26 drops) is as follows:[7]

Inactive ingredients: stabilizer, ethanol 96%, purified water.

According to the Farmak product label, the composition of 1 tablet is as follows:[8]

  • Ethyl ester of α-bromoisovaleric acid — 12.42 mg
  • Phenobarbital — 11.34 mg
  • Peppermint oil — 0.88 mg

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

Legal status[edit]

Phenobarbital, one of the principal ingredients in Corvalol, is a DEA Schedule IV substance in the United States. Schedule IV substances have a low potential for abuse relative to substances in Schedules I–III. Examples of Schedule IV substances are alprazolam (Xanax), carisoprodol (Soma), clonazepam (Klonopin), diazepam (Valium) and others.[9] It is illegal to import Corvalol into United States (see Health Hazard with Unapproved Imported Drug from Russia )

In some countries of Eastern Europe, Corvalol is believed to be safe enough to use in recommended doses without prescription. It is widely used to treat elevated blood pressure and as a general-purpose tranquilizer/sedative. Despite the -lol suffix, the drug is not a beta-blocker. Corvalol is so common in Eastern Europe that, in 1996, the Ministry of Health of the Russian Federation included it in the list of mandatory items in all Russian passenger vehicle first aid kits, alongside such drugs as aspirin, metamizole sodium (branded Analgin), nitroglycerin, and activated charcoal.

Manufacturer[edit]

Corvalol was produced by Kiev Chemical and Pharmaceutical Plant in Kiev, Ukraine in 1960-1991, and by its successor, the Joint Stock Company "Farmak", from 1991 onward. Farmak currently owns the exclusive trade mark to the drug name in Ukraine and a number of countries of Eastern Europe and the former Soviet Union, but not in Russia, where Corvalol is available from a number of different drug companies.[10]

Similar Products[edit]

The manufacturer Farmak produces another similar product, Corvaldin, which is similar in composition to Corvalol, but also contains 0.2 mg hops oil per 1mL on tincture.[11]

References[edit]

  1. ^ Wikipedia.ru. "Корвалол".[better source needed]
  2. ^ Natural Standard. The Authority on Integrative Medicine. "Valerian". https://naturalmedicines.therapeuticresearch.com/databases/food,-herbs-supplements/professional.aspx?productid=870
  3. ^ Morin, CM; et al. "Valerian-hops combination and diphenhydramine for treating insomnia: a randomized placebo-controlled clinical trial". Sleep. 2005 (11): 1465–71. 
  4. ^ American Geriatrics Society updated Beers Criteria for Potentially Inappropriate Medication Use in Older Adults. The American Geriatrics Society 2012 Beers Criteria Update Expert Panel.
  5. ^ Czekaj, P (2000). "Phenobarbital-induced expression of cytochrome P450 genes". Acta Biochim. Pol. 47: 1093–105. PMID 11996099. 
  6. ^ Фармак. "Корвалол (таблетки)". http://farmak.ua/ru/drugs/182
  7. ^ "Corvalol (oral solution) Prescribing Information" (PDF) (in Russian). PAO "Farmak". Retrieved 14 December 2015. 
  8. ^ "Corvalol (tablets) Prescribing Information" (PDF) (in Russian). PAO "Farmak". Retrieved 14 December 2015. 
  9. ^ U/S/ Department of Justice. Drug Enforcement Administration. Office of Diversion Control. "Controlled Substances Schedules" http://www.deadiversion.usdoj.gov/schedules/
  10. ^ "[Russian] State Register of Medicines: Corvalol" (in Russian). Retrieved 14 December 2015. 
  11. ^ Фармак. "Корвалдин" http://farmak.ua/ru/drugs/135