The range of uses of essential oils in modern medicine using the example of Golden Star balm

Instructions for use

pharmachologic effect

Camphor has a beneficial effect on tissues and organs, improving their trophism . The medication stimulates nervous stimulation. After the first administration, it increases the sensitivity of nerve endings. When applied topically, an anti-inflammatory, antimicrobial, and analgesic effect is achieved.

Parenteral administration stimulates an increase in blood pressure , respiratory rate and heart rate. There is a noticeable vasoconstrictor effect, the contractility of the myocardium increases. The respiratory organs react to the administration of camphor with increased expectoration of secretions and accumulated mucus.

When administered subcutaneously, there is a beneficial effect on the myocardium, it becomes healthier and contracts better. The speed of metabolic processes increases. Camphor ensures the saturation of organs and tissues with oxygen, nutrients, and blood. This improves their function and accelerates the process of cellular renewal.

Release form and composition

The main active ingredient is camphor . Available in several pharmacological forms. It is prescribed taking into account the patient’s diagnosis and tolerability of the active substance.

Below are all the dosage forms of camphor

• Powdered camphor in small sachets
• Racemic camphor
• Oil solution volume 1, 2, 10 ml
• Camphor oil 30 ml
• Anti-inflammatory and antiseptic ointment
• Alcohol tincture 40, 60, 80 ml

Indications for use

The drug is prescribed if the following indications exist::

• emergency care for acute and chronic heart failure;
• collapse and the need to stimulate respiratory function;
• emergency assistance in stimulating blood circulation;

Camphor is a good remedy for heart diseases

• treatment of low blood pressure and breathing problems;
• treatment of infectious blood diseases that cause heart and breathing problems;
• development of purulent pleurisy;
• asphyxia of any type;

Lung pathologies can be treated in combination with the use of camphor inhalations

• muscle pain and fatigue;
• stress and unstable mental state;
• poisoning of the body, most often in the treatment of carbon monoxide intoxication and sedatives;
• treatment of freckles and skin rashes;
• therapy to eliminate peri-wound eczema;
• relieving itching and inflammation of the skin;
• cosmetic procedures.

Camphor solution and ointment are actively used for skin diseases

Directions for use and dosage

When using the medication for subcutaneous administration, it is recommended to warm the Camphor in your hands. The classic dosage of the drug for adult patients is 1-5 ml up to three times a day.

To relieve pain or tension, it is recommended to rub in the active substance, preferably during massage sessions. The dose is 4-5 drops of camphor oil. The active substance is mixed with 15 ml of any massage oil.

For serious heart pathologies and breathing problems, the form of the medication and dose are selected individually. To stimulate breathing, one procedure requires 2 drops of the active substance; it is placed in an aroma lamp.

Attention! For children, the dosage of the active substance is selected according to age and weight. Self-administration under the skin is strictly prohibited for this group of patients, as there is a high risk of an allergic reaction.

Interaction with other drugs

• Use with great caution at the same time as other stimulants, as delirium and excessive nervous excitement may occur.
• The use of Camphor at the same time as heart medications and to stimulate respiratory function requires a more careful selection of the dose so as not to excessively increase blood pressure and prevent respiratory overload.
• When applied externally, it is not recommended to use the drug at the same time as creams, ointments and lotions. Such use may increase irritation and cause rashes and redness.

Video: What does camphor oil help with?

The range of uses of essential oils in modern medicine using the example of Golden Star balm

The necessary therapeutic effect of a drug and its bioavailability are ensured not only by the pharmacological action of the drug, but also by the dosage form (DF) chosen for their creation and use [1]. Official herbal preparations, which have significantly fewer side effects, can be considered as an alternative therapy or used to enhance the effectiveness of prescription drugs. Medicines (medicines) obtained on the basis of medicinal plant raw materials (MPS) are usually called “medicines of plant origin” (MSRP). A fairly common class of drugs obtained on the basis of MP are oils—essential oils (EOs) and vegetable fatty oils. Oils are most often used as a starting or intermediate product for the production of LSRP and are characterized as pharmaceutical substances or pharmaceutical excipients [1].

Separate requirements for the quality of specific names of packaged medicinal products are specified in private pharmacopoeial monographs (FS) for medicinal products included in the State Pharmacopoeia of the USSR X ed. (GF X) [2], State Pharmacopoeia of the USSR XI ed. (GF XI) [3], in the regulatory documentation of manufacturers. LSRP are included in the Register as “drugs of herbal origin” indicating the pharmacological action: “choleretic of herbal origin”, “sedative of herbal origin”, etc. LSRP are available in more than 50 pharmacological groups of the Register, including: expectorants, general tonics , antispasmodic, sedative, laxative, choleretic, diuretic, astringent, etc. The drugs presented in these groups are registered in the form of various dosage forms. In the domestic pharmacopoeia, the characteristics of essential oils are given in article 471 of the State Fund X “Essential oils” (Olea aetherea): “Essential oils are a mixture of volatile fragrant substances belonging to various classes of organic compounds. The main components of essential oils are terpenes and their oxygen-containing derivatives, and less commonly, aromatic and aliphatic compounds. EOs are obtained from various plant organs by distillation with water or steam, extraction with organic solvents, pressing and other methods” [1]. The European Pharmacopoeia (EP) has a general monograph 01/2008:2098 “Essential oils. Aetherolea”; The monograph of the British Pharmacopoeia is identical to the EP. According to this monograph: “Essential oils are odorous drugs, usually of complex composition, obtained from medicinal plants by steam distillation, dry distillation, or suitable mechanical effects without heating” [4]. GF X included three private pharmacopoeial articles for essential oils: eucalyptus, peppermint, purified turpentine oil (turpentine).

The study of biological activity and the possibility of using essential oils for medicinal purposes was widely carried out in the laboratory of the Crimean Research Institute named after. I. M. Sechenov. In the course of research, it was found that essential oils and their components easily pass through the epithelium of the capillaries, they freely cross the placenta. With the help of transport carrier molecules located in biological membranes, molecules of aromatic substances penetrate cell membranes and interact with receptors of intracellular biological complexes. They interact with the enzyme, endocrine, immune and other systems [5]. Complex mixtures of fragrant substances (essential oils) are most often classified as monoterpenes and sesquiterpenes based on their chemical structure, but they can also be phenolic compounds. By their physical nature, they are mobile oily liquids that evaporate without leaving greasy stains and mix well with alcohols and fatty oils. They do not mix with water, but are capable of distillation with water vapor [6]. The global assortment of major essential oil plants includes about 30–40 species, the most important among them are species of genera that include not only monocyclic monoterpenes, but also their precursors, acyclic monoterpenes: geraniol, linalool, citronellol, etc. [7]. In modern medical practice, medicines based on EOs are used in the treatment of functional disorders of the gastrointestinal tract, inflammatory diseases of the upper respiratory tract, lower urinary tract and as a means of correcting functional disorders of the central nervous system.

In medicine, complex preparations containing essential oils from many medicinal plants are used [9, 10]. Group aromatherapy appears to be a promising method of group therapy and prevention of acute respiratory diseases (ARI) in groups. The term “aromatherapy” (literally, the use of scent as a medicine) was first coined by the French chemist Dr. Rene M. Gattefosse in 1928. [11] Aromatherapy is the inhalation of natural essential oils that have antimicrobial and antiviral properties. Inhaling the vapors of such oils has a bactericidal, anti-inflammatory and antiseptic effect, improves the qualitative composition of the microflora of the upper respiratory tract and their patency, and increases local immunity. We should dwell in more detail on the group of essential oils that are used to treat inflammatory pathologies of the respiratory tract. The significant prevalence of acute respiratory diseases, their adverse effects on the state of the body’s leading systems, and the insufficient effectiveness of prevention and rehabilitation methods determine the importance of the medical aspects of this problem and their social significance [12, 13]. Today, a current trend is the use in medical practice of safe medical technologies that increase the functional reserves of the child’s body in the treatment of respiratory diseases. There is extensive experience in the use of “collective” prevention of respiratory pathology. Thus, in a number of schools and kindergartens, in collaboration with doctors, various methods are used: vaccination, the use of means for elimination therapy [12]. In a number of studies conducted in children's medical institutions, various drugs were prescribed based on a complex of natural essential oils (mint, eucalyptus, cajeput, juniper, clove, wintergreen).

E. Yu. Radzig et al. (2009) [12] conducted an open comparative study to evaluate the effectiveness of the drug (oil for inhalation), which includes a multicomponent composition of essential oils, as a means of preventing colds in organized children's groups. The study was conducted for 90 days at a kindergarten in the North-East Administrative District of Moscow. The main group included children (n = 100) aged 3–7 years who were prescribed the drug EM; In the control group, children (n = 100) had their nasal cavity and nasopharynx washed with saline every day for a month. During inhalation of the drug with EF during the first 20 days, a less pronounced manifestation of symptoms (nasal congestion, mucous discharge from the nose) was observed in comparison with the control group. In the main group of 100 people, 2 children (2%) developed an allergic skin rash after one day of taking the drug and the children dropped out of the study. According to the results of the study, during the observation period of the remaining children (n = 98) it was obtained: 32.6% never got sick; 51% got sick only once; 15.3% got sick twice; 1% - three times. When taking a drug with EOs as a means of preventing the development of respiratory diseases in children in organized children's groups, the number of children who did not get sick increased by 34%; in 98% of cases the drug was well tolerated [12].

In another open comparative study by E. A. Azova et al. (2012) [13] assessed the effectiveness of another drug, which contains natural essential oils (mint, eucalyptus, cajeput, juniper, clove, wintergreen), in the complex therapy of acute respiratory infections. The study was conducted on the basis of a children's clinic in Nizhny Novgorod. We observed 45 children with acute respiratory infections, aged 3–14 years, who had a history of recurrent disease. The main group of children (n = 30) received standard therapy in combination with a preparation based on essential oils, the control group (n = 15) received standard therapy only. In the main group, the drug was prescribed in the form of passive inhalations for 30 days. The dynamics of the condition were assessed by a pediatrician, an ENT doctor, using nasopharyngootoscopy, cytoscopy of a smear from the nasal mucosa, and an allergy test for tolerance to essential oils. In the background: clinical signs of acute respiratory infections with damage to the upper respiratory tract (soreness, dryness and sore throat, rhinorrhea, cough), with pharyngoscopy - signs of an active inflammatory process (hyperemia of the mucous membrane of the pharynx, etc.). Clinically positive dynamics were noted on the 3rd day in the main group, on the 7th day - in the control group; on the 3rd day, an improvement in the rhinoscopic and pharyngoscopic picture was noted in all children (100%) in the main group and in 20% in the control group. No adverse reactions were observed when using the complex of essential oils, including in children with a history of allergies. Based on the results of the study, a conclusion was drawn [13]: the use of a complex of essential oils in addition to standard therapy can reduce the duration of acute respiratory infections by 1.6 times; Can be prescribed to children of different age groups; can be used as a prevention of recurrent respiratory diseases in children both at home and in outpatient settings.

Similar data were obtained in the study by L.P. Grebova et al. (2013) [14], which assessed the effectiveness of a drug containing a similar composition of essential oils on the incidence of acute respiratory viral infection (ARVI) in an organized children's group. The study involved 106 children in the first grades of a school in Ryazan; all schoolchildren were vaccinated according to age. All participants were divided into 4 groups: in group 1, children (n = 27) were prescribed a drug with essential oils only in the classroom; in the 2nd (n = 27) - only at home; in the 3rd (n = 23) - both in the classroom and at home; in the 4th, control group (n = 29) - nothing was prescribed. The drug was used in the form of passive inhalations for 30 days. The study revealed: in children who received the drug with essential oils as a means of preventing ARVI, the following was noted: 1) a decrease in the number of cases of ARVI by 3.1 times; 2) milder course of the disease; 3) reducing by 3 times the number of missed school days due to illness [14].

One of the most popular remedies for the treatment of colds is Golden Star balm. The balm was developed by Vietnamese scientists based on ancient recipes and received approval from the Ministry of Health of the Russian Federation [15]; it can be used in the treatment of a wide range of diseases [16]. Today, the Russian pharmaceutical market sells several forms of the drug: pencil for inhalation, liquid balm, solid balm. As a result of the studies, it was proven that the substances included in the balm do not have a negative effect on human skin. The balm contains essential oils: camphor (Camphora) - 0.910 g, peppermint (Mentha piperita) - 0.590 ml, eucalyptus (Eucalyptus) - 0.140 ml, clove (Syzygium aromaticum) - 0.228 ml, cinnamon (Cinnamomum zeylanicum) - 0.053 ml and menthol oil - 0.455 g. The healing and preventive properties of the Golden Star balm are recognized by official medicine. Pharmacological effect of the balm: distracting, antiseptic, local irritant.

It is worth briefly dwelling on the medicinal properties of the essential oils included in the Golden Star balm. Clove essential oil is light, fluid, with a strong spicy odor and pungent taste. Clove oil is obtained from the flower buds of the evergreen clove tree of the myrtle family. Clove oil has a strong antiseptic, antispasmodic, strengthening, stimulating and carminative effect, so it can be used for preventive purposes during epidemics of airborne and intestinal infections [16]. It is used as an antiseptic, due to its high antibacterial and antiviral activity, in the prevention of influenza and ARVI during epidemics of these airborne infections [11]. Clove oil also has antimycotic activity against Aspergillus fungi [17]. Clove oil is a pain reliever that can be used for neuralgia, arthritis and rheumatism, and it also strengthens the immune system and has a warming effect. The use of clove oil in combination with other remedies has a strong healing effect on inflammation of the skin, infection in wounds and long-term non-healing ulcers. Preparations with clove oil eliminate inflammatory processes in the oral cavity during periodontal disease and pulpitis, as well as dental neuralgia [16].

The medicinal properties of peppermint, a perennial herbaceous plant, have been known since ancient times. The medicinal raw material is mint herb, as well as the essential oil obtained from the leaves, which has pronounced antibacterial properties [18]. Mint leaves contain substances such as carotene, hesperidin, betaine, rhamnose, glucose, ursolic, melicic, linoleic and oleanolic acids [16, 18]. From peppermint leaves, EO is obtained, which is actively used in the treatment of respiratory diseases [19], and menthol, which has a mild analgesic and disinfectant effect. Menthol is used in the form of alcohol, ether-alcohol and oil solutions externally (for rubbing) for itching, neuralgia, migraines, used for lubrication, inhalation and as drops (in the nose) for inflammatory diseases of the upper respiratory tract (runny nose, tracheitis, etc.) . Peppermint oil is used for inhalation for laryngitis, to eliminate muscle pain due to overexertion and injuries [16]. Cinnamon tree or cinnamon is a genus of trees and shrubs from the laurel family, from the fruits and leaves of which cinnamon oil is obtained. Cinnamon oil has antiseptic, analgesic, decongestant, warming and antidepressant effects; accelerates the recovery process for nervous and cold diseases, as well as for some disorders of the gastrointestinal tract [16]. According to recent data [20] in experimental models, cinnamon has an inhibitory effect on cholinesterase activity, and an increase in the number of neurons in the hippocampus has been histologically revealed.

The medicinal raw materials are eucalyptus leaves. Substances contained in eucalyptus have an antiseptic (due to the presence of bioflavonoids) [21] and analgesic effect. Eucalyptus EO is used both externally and internally. It is used for diseases of the upper respiratory tract for inhalation, as well as for lumbago [16]. Eucalyptus preparations are used in the treatment of abscesses, cellulitis, infected wounds, pleurisy, mastitis, chronic osteomyelitis, open fractures, gynecological, colds and many other diseases [21]. In addition to extracts and essential oils of medicinal plants, the balm also contains some other components that have a number of medicinal properties. Camphor is one of the powerful medicinal agents and is included in many preparations intended for both external and internal use [16]. Linalool, which is part of camphor, has pronounced insecticidal and repellent effects [22]. Camphor is a powerful stimulant of heart activity and is used in the treatment of acute and chronic heart failure, as well as to restore blood circulation and breathing during collapse. It is used externally for joint diseases (rheumatism, arthritis, arthrosis, radiculitis), as well as for bedsores in severely ill patients.

Thanks to eucalyptus oil, Golden Star balm stimulates sensitive nerve endings and is indispensable for headaches and colds; peppermint oil has sedative analgesic, antiseptic, antispasmodic and other effects; clove oil has a pronounced anesthetic effect; menthol oil suppresses the development of edema in inflammatory diseases of the upper respiratory tract; cinnamon oil is used as a remedy after bruises and for arthralgia; camphor oil has a warming effect (for myositis, etc.) [9–11, 16]. Balm Golden Star is used externally for colds, runny nose, cough, flu, inflammation and pain in the nasopharynx. It eliminates nasal discomfort and is recommended for headaches and dizziness, as well as for symptoms of seasickness. Thanks to the medicinal plant essential oils it contains, the balm has a strong aromatherapy effect, so it can be used in combination with other remedies in the treatment of psychosomatic conditions. Balm Golden Star can also be used in the treatment of various joint diseases (arthritis and arthrosis), radiculitis, rheumatism, osteochondrosis, as well as minor injuries (bruises and sprains). The drug can also be used for insect bites to relieve skin itching. Contraindications for the use of Golden Star balms are intolerance to the components included in the balm and pustular skin diseases.

Conclusion

This review describes the effects of the most famous natural essential oils (peppermint, eucalyptus, cloves, cinnamon), on the basis of which various medicines have been created. Data from a number of studies using medications containing essential oils are presented, which indicate that the use of a complex of essential oils in addition to standard therapy can reduce the duration and severity of acute viral respiratory diseases.

One of the most famous and popular means for the prevention and treatment of colds during an unfavorable epidemiological situation is still the Golden Star balm.

Literature

1. Sakaeva I.V., Bunyatyan N.D., Sakanyan E.I. et al. Medicines of herbal origin in modern dosage forms: characteristics and classification // Bulletin of the Scientific Center for Expertise of Medicinal Products. 2013; 4:51–58.
2. State Pharmacopoeia of the USSR: X edition. Collection of mandatory national standards and regulations regulating the quality of medicines, ed. Mashkovsky M. D. M.: Medicine. 1968. 1078 p.
3. State Pharmacopoeia of the USSR: Vol. 1. General methods of analysis / USSR Ministry of Health. 11th ed., add. M.: Medicine, 1987. 336 p.
4. State Pharmacopoeia of the USSR: Vol. 2. General methods of analysis. Medicinal plant raw materials / Ministry of Health of the USSR. 11th ed., add. M.: Medicine, 1989. 400 p.
5. European Pharmacopoeia 7.0. Volume 1. M.: Remedium, 2011. 1812 p.
6. Tikhomirov A. A., Yarosh A. M. Features of the use of essential oils for therapeutic and prophylactic purposes. Chasopis // Phytotherapy. 2008; 1:18–21.
7. Rozhdestvensky D. A. Clinical pharmacology of medicines based on essential oils // Medical news. 2015; 10: 16–18.
8. Ponomareva E.I., Molokhova E.I., Kholov A.K. Application of essential oils in pharmacy // Modern problems of science and education. 2015; 4:567–575.
9. Pavlov S. A. Balm “Star”. In the book: Ancient and modern methods of treatment. St. Petersburg: Lenizdat, 2006. 128 p.
10. Pavlov S. A. Balm “Star”. In the book: Ancient and modern methods of treatment. St. Petersburg: Lenizdat, 2011.
11. Zaitseva S.V., Zastrozhina A.K., Belskaya E.A. The place of aromatherapy in the treatment and prevention of acute respiratory diseases // Difficult Patient. 2015: 1–2 (13): 48–54.
12. Radtsig E. Yu., Bogomilsky M. R., Ermilova N. V. Inhalation with essential oils - a method for the prevention of respiratory viral infections in organized children's groups // Treating Doctor. 2009; 9:92–94.
13. Azova E. A., Vorobyova V. A., Kulikov A. G. et al. Experience of inhalation use of “Breathe” oil in the prevention and complex therapy of acute respiratory infections in children // Pediatrician’s Handbook. 2012; 3:55–61.
14. Grebova L.P., Besarab G.A., Lobanova E.I. Prevention and complex therapy of ARVI: the effectiveness of inhalation effects of natural essential oils // Respiratory diseases. 2013; 1:60–63.
15. Instructions for use of the medicinal product for medical use. Balm “Golden Star”. Register. number: P N011814/01–070911.
16. Antonova L.V. “Star”. Unknown healing properties of an old friend. M.: RIPOL classic, 2007. 64 p.
17. Císarová M., Tansinová D., Medo J. et al. The in vitro effect of selected essential oils on the growth and mycotoxin production of Aspergillus species // J Environ Sci Health B. 2021, Jun 20: 1–7.
18. Radaelli M., da Silva B.P., Weidlich L. et al. Antimicrobial activities of six essential oils commonly used as condiments in Brazil against Clostridium perfringens. // Braz J Microbiol. 2016 Apr-Jun; 47(2):424–430. DOI: 10.1016/j.bjm.2015.10.001.
19. Ayrle H., Mevissen M., Kaske M. et al. Medicinal plants — prophylactic and therapeutic options for gastrointestinal and respiratory diseases in calves and piglets? A systematic review // BMC Vet Res. 2021, Jun 6; 12 (1): 89. DOI: 10.1186/s12917–016–0714–8.
20. Madhavadas S., Subramanian S. Cognition enhancing effect of the aqueous extract of Cinnamomum zeylanicum on non-transgenic Alzheimer's disease rat model: Biochemical, histological, and behavioral studies // Nutr Neurosci. 2021, Jun 16: 1–12.
21. Goodger JQD, Senaratne SL, Nicolle D. et al. Foliar Essential Oil Glands of Eucalyptus Subgenus Eucalyptus (Myrtaceae) Are a Rich Source of Flavonoids and Related Non-Volatile Constituents // PLoS ONE. 2016; 11 (3): e0151432. DOI: 10.1371/journal.pone.0151432.
22. Jiang H., Wang J., Song L. et al. GC×GC-TOFMS Analysis of Essential Oils Composition from Leaves, Twigs and Seeds of Cinnamomum camphora L. Presl and Their Insecticidal and Repellent Activities // Molecules. 2021, Mar 28; 21(4). DOI: 10.3390/molecules21040423.

O. A. Shavlovskaya, Doctor of Medical Sciences

GBOU VPO First Moscow State Medical University named after. I. M. Sechenova Ministry of Health of the Russian Federation, Moscow

Contact Information

Side effects

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Next fact

When using Camphor, there is a risk of the following side symptoms :

• live embolism, which is characterized by acute blockage of blood vessels with oil;
• skin irritation and redness;
• swelling and swelling of the injection site;
• anaphylactic shock;
• rash resembling scarlet fever;
• severe headache and dizziness;
• convulsive state and delirium;
• a sharp jump in blood pressure and acute excitability.

Attention! If side effects occur, you should immediately consult a doctor to accurately determine the cause of the disorder. In some cases, it is sufficient to reduce the dose of the active substance and conduct a short course of symptomatic treatment.

Overdose

Excessive use of the drug leads to the side symptoms described above . The likelihood of developing a live embolism increases several times. Treatment is symptomatic and carried out under the supervision of a doctor.

Contraindications

Camphor should not be used if the following problems exist::

• 
  Hypersensitivity is a contraindication to the use of camphor-based products. Hypersensitivity to the active substance is usually determined after external use;

• individual intolerance to auxiliary components that may be in ointments and alcohol solutions;
• extensive damage to the skin when used topically;
• tendency to epileptic seizures and excessive psycho-emotional state;
• high blood pressure or a tendency to it;
• It can be used with caution during inflammatory processes in internal organs.

Use during pregnancy and lactation

The drug is usually not prescribed during pregnancy , as there is a risk of an allergic reaction due to hormonal changes. During lactation, you should also consult with your doctor about the possibility of using Camphor, since it can pass through breast milk into the baby’s body.

Terpenes and their use in clinical practice

V.A. Shaderkina1, I.A. Shaderkin2

1Urological information portal Uroweb.ru 2Federal State Autonomous Educational Institution of Higher Education First Moscow State Medical University named after I.M. Sechenov Ministry of Health of Russia (Sechenov University)

CHEMICAL STRUCTURE OF TERPENS

Terpenes are a subclass of unsaturated hydrocarbons with the general formula (C5H8)n, where n>2. The hydrocarbon with the empirical formula C5H8, bearing the official “structural” name 2-methylbuta-1,3-diene, is known as isoprene. Essentially, terpenes are polymers of isoprene with a low degree of polymerization. With an increase in the number of isoprene residues in the molecule (degree of polymerization), the properties of the compound change radically.

However, in living nature, it is not isoprene polymers that are most often found, but their oxygen-substituted derivatives, which are currently called “terpenoids”.

The concept of “oxygen-substituted derivative” from the point of view of organic chemistry is extremely vague. Such a derivative can be an alcohol, both simple and polyhydric, a ketone, an aldehyde, an ether, and an ester. This results in a huge (more than 10,000 known representatives) group of chemical compounds, extremely diverse in their physical, chemical, and pharmacological properties, which are united by two characteristics:

• composition exclusively of carbon, hydrogen and oxygen atoms;
• the presence in the structure of isoprene fragments connected to each other according to the “head to tail” type.

The number of these isoprene fragments largely determines the properties of the molecule.

Two molecules of isoprene make up monoterpenes (monoterpenoids). They are widely distributed in the plant world as a component of essential oils. It is monoterpenes and esters that determine the smell of plants. Classic representatives of monoterpenes are cineole, the main component of eucalyptus oil, and menthol, the main component of peppermint oil. Also classified as monoterpenes is camphor (camphene), a bicyclic ketone containing two isoprene monomers. Monoterpene hydrocarbons (α-pinene, β-pinene, terpinolene, β-terpinene) are very characteristic of phylogenetically more ancient coniferous plants, while oxygen-containing monoterpene aldehydes, ketones and alcohols (citral, linalool, terpineol) are more characteristic of flowering plants , geraniol). The specific smell of coniferous forests is associated with the formation and evaporation of monoterpene hydrocarbons.

The combination of three isoprene molecules is called sesquiterpenes (sesquiterpenoids) - “one and a half” terpenes. They are also found in essential oils. However, the three-membered isomer has a heavier molecule, and, therefore, a priori, is less volatile and gives a less pronounced but more persistent odor. Sequiterpenes are farnesol, which is part of the essential oils of lily of the valley and linden, as well as farnesene isolated from pine resin.

Four-membered isoprene polymers (diterpenes, diperpenoids) are even less volatile; they are part of plant resins. In addition, the diterpene vitol is part of chlorophyll.

Six-membered isoprene polymers (triterpenes) contain 30 carbon atoms. Due to their almost complete lack of volatility, they are not found in essential oils. Triterpenoids are polycyclic acids or alcohols. However, the best known products are their glycosidation products, which already belong to the class of glycosides or saponins. Of the triterpene acids, the most common are ursolic, oleanolic, and crateic acids. Ursolic acid is found in relatively large quantities in the fruits and leaves of cranberries, sea buckthorn, lingonberries, and apple skins. Crateic acid has been identified in hawthorn fruits.

Eight-membered polymers (tetraterpenes, tetraterpenoids) include one single structural group - carotenoids. These are natural pigments of yellow, orange, red colors, synthesized by higher plants, which determines the appropriate coloring of their flowers and fruits.

Higher molecular weight isoprene compounds, called polyterpenes and polyterpenoids, are known as gutta-percha and natural rubber.

APPLICATION OF TERPENS IN MEDICINE

All monoterpenes, to one degree or another, have antiseptic, anti-inflammatory and antispasmodic effects. Some representatives may have a sedative, analeptic, expectorant, and diuretic effect. This leads to their use in clinical practice for a wide variety of indications.

Well-known and long-used preparations based on terpenes include: validol (active ingredient - menthol), camphor (active ingredient - camphene), turpentine (a mixture of terpene hydrocarbons in which α- and β-pinenes predominate).

In addition, terpenoids and their derivatives are: retinol (vitamin A), cholecalciferol and alfacalcidol (vitamin D and its active metabolites), tocopherol (vitamin E).

Due to the wide variety of pharmacological effects combined with low toxicity, the interest of researchers in terpenes and their derivatives continues to this day. Moreover, the most exotic areas of pharmacological application of these chemical compounds are sometimes considered. Let's look at the most interesting results of recent research.

There are publications on the potentiation of the antimicrobial effect when combined with antibacterial agents and terpene-based drugs. In particular, this effect is shown in relation to anti-tuberculosis therapy and the treatment of leishmaniasis [1,2].

Saito A. et al. in an experiment on mice showed the antimalarial activity of the sequiterpene nerolidol [3].

A. Kudryavtseva et al. note that a large number of terpenes and terpenoids “have potential geroprotective and anticancer properties.” The authors studied the properties of fir extract and identified these effects in vitro on normal and tumor cell lines [4]. The potential antitumor activity of terpenoids and flavonoids is also indicated in their review by JN Nwodo et al. [5].

The anti-inflammatory and analgesic effect of terpenes is widely used. In one of the early studies presented by Y. Han, terpenes isolated from ginkgobiloba, in an experiment on mice, were found to have anti-inflammatory activity comparable to indomethacin. Acute arthritis provoked by C. albicans antigens was chosen as a model [6].

Recently, most researchers have been inclined to use terpenes as an additional component of anti-inflammatory therapy, which makes it possible to reduce the dose of non-steroidal anti-inflammatory drugs and, therefore, increase the safety of therapy. The creation of transdermal systems based on terpenes and anti-inflammatory agents is considered promising.

In 2006, an original study was published on the resorptive effect of terpenes when applied topically [7]. In general, terpenes penetrate very poorly through intact skin, especially α-pinene. However, when exposed to a weak electric current, the situation changes. According to publications by B. Nokhodchi et al., C. Arunkumar et al. terpenes, in particular geraniol, menthol and thymol, can enhance iontophoresis of diclofenac sodium, which can be used in the practice of physiotherapy for inflammatory diseases of the musculoskeletal system [8,9].

USE OF TERPENS IN UROLOGICAL PRACTICE

A whole layer of research is devoted to the use of terpene-based drugs for the treatment of diseases of the genitourinary system.

In 2013, a meta-analysis was published demonstrating the striking lithokinetic effect of terpene-based drugs [10]. And it is this effect of terpenes that is considered the most popular in modern urology.

In domestic urological practice, until now, the only drug based on terpenes was known, for which two randomized placebo-controlled studies were conducted in 1992 and 2010. A high lithokinetic effect of this drug against ureteral stones was demonstrated - 78% and 67.9%, which significantly exceeds the probability of spontaneous passage of similar stones in the control groups - 52% and 50% in groups receiving placebo [11,12]. The above studies differed in that one of them administered terpenes to patients undergoing external shock wave lithotripsy for a kidney stone.

The likelihood of a stone passing on its own is inversely related to its size. According to the results of a prospective study conducted by G. Faragi et al., in the presence of a small stone (no more than 3.3 mm) in the lower third of the ureter, the effectiveness of lithokinetic therapy using terpene-based drugs reaches 96% [13].

According to the Research Institute of Urology, the probability of spontaneous passage of a ureteral stone, regardless of its location, while taking terpenes is 73%. When a calculus is localized in the lower third of the ureter, the probability of its spontaneous passage against the background of complex therapy, including terpene-based drugs, increases to 83%. With traditional therapy, including drotaverine and a non-narcotic analgesic, 32% of ureteral stones and 51% of stones when localized in the lower third pass away on their own. The use of terpene-based drugs is especially advisable after extracorporeal lithotripsy. When localized in the lower third of the ureter, against the background of complex therapy, 80% of the stone paths recede independently [14].

During the above study, against the background of a three-week course of lithokinetic therapy, diuresis increased significantly and, accordingly, the relative density of urine decreased (from 1015.9 ± 3.0 to 1012 ± 6.9), however, the urine reaction and renal excretion of salts did not undergo significant changes. changes [14]. This property is an important feature that distinguishes the diuretic effect of terpenes from other diuretics, both herbal and synthetic.

The ability to maintain low urine density for a long time without the risk of developing electrolyte disturbances and disorders of phosphorus-calcium metabolism allows us to consider terpene-based drugs as a means for metaphylaxis of all forms of nephrolithiasis.

The lithokinetic effect of terpenes is realized quite quickly. In 72.3% of patients who underwent extracorporeal shock wave lithotripsy of a kidney stone, complete clearance of the urinary tract from fragments of destroyed stones occurred within the first 5 days of the postoperative period. And after 14 days of therapy, complete passage of stone fragments was observed in 84.6% of patients. In the control group, the process of spontaneous removal of fragments of destroyed stone turned out to be longer. During the first 5 days, only 40.8% of patients got rid of fragments of destroyed stone, and within 14 days - 51.0% of patients [15].

Along with the lithokinetic effect, terpene-based drugs demonstrated a nephroprotective effect in diabetic nephropathy [16], as well as a pronounced analgesic effect in pelvic pain syndrome, comparable to the average therapeutic dose of indomethacin [17].

RENOTINEX®: COMPOSITION AND PROPERTIES

Currently, a new product based on terpenes has appeared on the domestic pharmacological market - Renotinex®,. The drug contains six types of terpenes: pinene, camphene, borneol, anethole, fenchone, cineole. All these active ingredients are in a strictly defined quantitative ratio, which is generally not typical for classical phytotherapeutic agents. The certainty and stability of the chemical composition makes it possible to combine the positive qualities inherent in synthetic drugs, in particular, the predictability and controllability of the effect, with the positive properties of herbal medicines, such as the versatility of the effect and a favorable safety profile. Renotinex® additionally contains alpha-tocopherol acetate (vitamin E).

The main mechanisms of action of vitamin E are cell membrane stabilization and antioxidant effects. These effects determine its nephroprotective effect in dysmetabolic nephropathies and urolithiasis. In addition, tocopherol showed a moderate but clinically significant hypocalcemic effect, which is required for calcium oxalate and calcium phosphate nephrolithiasis.

According to modern concepts, complex therapy for oxalate nephrolithiasis, along with surgical methods for removing or destroying stones, includes a hypooxalate diet, drinking plenty of fluids, sometimes in combination with herbal diuretics, as well as the use of membrane stabilizers and antioxidants.

CONCLUSIONS

Thus, the new domestic product Renotinex® can be recommended for ureteral stones of any location and any chemical composition, if their size allows hope for spontaneous passage, as well as after lithotripsy to facilitate the passage of fragments of destroyed stones. The metabolic effects of Renotinex® allow us to recommend it for long-term metaphylaxis of phosphate, urate and, especially, calcium oxalate nephrolithiasis.

Key words: herbal remedies, terpenes, chemical structure, anti-inflammatory effect, antispasmodic effect, urolithiasis, Renotinex®.

LITERATURE

1. Sieniawska E, Swatko-Ossor M, Sawicki R, Skalicka-Wozniak K, Ginalska G. Natural Terpenes Influence the Activity of Antibiotics against Isolated Mycobacterium tuberculosis. Med Princ Pract 2017;26(2): 108-112. doi: 10.1159/000454680.

2. Camargos HS, Moreira RA, Mendanha SA, Fernandes KS, Dorta ML, Alonso A. Terpenes increase the lipid dynamics in the Leishmania plasma membrane at concentrations similar to their IC50 values. PLoS One 2014;9(8):e104429. doi: 10.1371/journal.pone.0104429. eCollection 2014.

3. Saito AY, Marin Rodriguez AA, Menchaca Vega DS, Sussmann RA, Kimura EA, Katzin AM Antimalarial activity of the terpene nerolidol. Int J Antimicrob Agents 2016;48(6):641-646. doi: 10.1016/j.ijantimicag.2016.08.017.

4. Kudryavtseva A, Krasnov G, Lipatova A, Alekseev B, Maganova F, Shaposhnikov M, Fedorova M, et al. Effects of Abies sibirica

terpenes on cancer- and aging-associated pathways in human cells. Oncotarget 2017(50):83744-83754. doi: 10.18632/onco-target.13467.

5. Nwodo JN, Ibezim A, Simoben CV, Ntie-Kang F. Exploring Cancer Therapeutics with Natural Products from African Medicinal Plants, Part II: Alkaloids, Terpenoids and Flavonoids. Anticancer Agents Med Chem 2016;16(1):108-27.

6. Han Y. Ginkgo terpene component has an anti-inflammatory effect on Candida albicans-caused arthritic inflammation. Int Immunopharmacol. 2005;5(6):1049-56.

7. Cal K. Skin penetration of terpenes from essential oils and topical vehicles. Planta Med 2006;72(4):311-6.

8. Nokhodchi A, Sharabiani K, Rashidi MR, Ghafourian T. The effect of terpene concentrations on the skin penetration of diclofenac sodium. Int J Pharm 2007;335(1-2):97-105.

9. Arunkumar S, Shivakumar HN, Narasimha Murthy S. Effect of terpenes on transdermal iontophoretic delivery of diclofenac potassium under constant voltage. Pharm Dev Technol 2018;23(8):806-814. doi: 10.1080/10837450.2017.1369110. Epub 2017 Aug 31.

10. Chua ME, Park JH, Castillo JC, Morales ML. Terpene compound drug as medical expulsive therapy for ureterolithiasis: a meta-analysis. Urolithiasis 2013;41(2):143-51. doi:10.1007/s00240-012-0538-3.

11. Mukamel E, Engelstein D, Simon D. The value of Rowatinex in the treatment of ureterolithiasis. J Urol 1992;98(1):31-33.

12. Romics I, Siller G, Kohnen R. A special terpene combination (Rowatinex) improves stone clearance after extracorporeal shockwave lithotripsy in urolithiasis patients: a results of a placebo-controlled randomized trial. Urol Int 2010;86(1):102-109.

13. Faragi G, Mulerad M, Rub R. Prospective comparative study of Rowatinex and Alfuzosin in the treatment of urolithiasis in the lower segment of the ureter. Eur Urol Suppl. 2008;7(8):149.

14. Sivkov A.V., Cherepanova E.V., Shaderkina V.A. The use of herbal remedies based on terpenes for urolithiasis. Experimental and clinical urology. 2011;(1):69-72.

15. Rudenko V.I., Innoyatov Zh.Sh., Perekalina A.N. Herbal preparation "Rovatinex" in the treatment of patients with urolithiasis. Materials of the XIV Congress of the Russian Society of Urologists. Saratov. year 2014. pp. 110-111.

16. Chen J, Hou XF, Wang G, Zhong QX, Liu Y, Qiu HH, et al. Terpene glycoside component from Moutan Cortex ameliorates diabetic nephropathy by regulating endoplasmic reticulum stress-related inflammatory responses. J Ethnopharmacol 2016;193:433-444. doi: 10.1016/j.jep.2016.09.043.

17. Lee CB, Ha US, Lee SJ, Kim SW, Cho YH. Preliminary experience with a terpene mixture versus ibuprofen for treatment of category III chronic prostatitis/chronic pelvic pain syndrome. World J Urol 2006;24(1):55-60.

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Renotinex

Magazine

Journal "Experimental and Clinical Urology" Issue No. 1, 2019

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special instructions

When using Camphor, several mandatory factors must be taken into account:

• if there are wounds on the skin and abrasions, you should consult a doctor before using the drug, since contact with an open wound can cause severe inflammation and irritation;
• in childhood, Camphor causes side symptoms several times more often, which is due to the special sensitivity of their body;
• the drug does not affect the ability to drive vehicles and complex mechanisms, except in cases where the active substance provoked headaches, dizziness and delirium.

Video: “Use of camphor alcohol”

Camphor alcohol

2%

10%

Registration number: Р N003092/01

Trade name: Camphor alcohol.

International nonproprietary or generic name: Camphor.

Dosage form: Alcohol solution for external use.

Composition per 100 ml: Active substance:

• Camphor (synthetic camphor) 2 g or 10 g

Excipient:

• Ethanol (ethyl alcohol) 70% up to 100 ml

Description: Transparent, colorless liquid with a characteristic camphor odor. Pharmacotherapeutic group: local anesthetic of natural origin.

ATX code: M02AX10

Pharmacological action: A drug of natural origin, it has a local irritant, antiseptic, anti-inflammatory and analgesic effect. Stimulates sensitive nerve endings, reflexively improves trophism of organs and tissues.

Pharmacokinetics: When applied to the surface of the skin, it is partially absorbed and undergoes oxidation. Oxidation products combine with glucuronic acid and are excreted by the kidneys. Part of the camphor is excreted unchanged by the lungs and bile.

Indications: Myalgia, myositis, arthralgia, sciatica, prevention of bedsores.

Contraindications: Hypersensitivity to any of the components of the drug, damage to the integrity of the skin or inflammatory skin diseases at the site of intended application (including dermatitis, eczema), pregnancy, lactation, childhood (due to lack of data).

Directions for use: Externally. Myalgia, myositis, arthralgia, sciatica: applied to the skin over the affected area 2 - 3 times a day. Duration of treatment is 7 - 10 days.

Prevention of bedsores: Treat the skin 2 - 3 times a day.

Side effects: Allergic reactions (urticaria), skin irritation, headache, dizziness.

Overdose: Symptoms: Excitement, tachycardia, convulsions.

Treatment: Symptomatic.

Release form: Alcohol solution for external use 2%, 10%. 40 ml in orange glass bottles, sealed with polymer stoppers and screw caps. Each bottle with instructions for use is placed in a cardboard pack. It is allowed to pack bottles with an equal number of instructions for medical use in a group package. 4 kg, 8 kg in polyethylene canisters; 18 kg in polyethylene canisters or glass bottles (for hospitals).

Storage conditions: Protected from light at a temperature of 15 to 25°C. Keep out of the reach of children.

Shelf life: 3 years. Do not use after expiration date.

Conditions for dispensing from pharmacies: Without a prescription.

Storage conditions and periods

Camphor should be stored taking into account the form of its release away from direct sunlight. The maximum storage temperature is +25 degrees; it cannot be stored at negative temperatures.

• The shelf life of the ointment is 4 years.
• The granules should be used within 24 months.
• The alcohol tincture can be stored for 12 months.
• Camphor powder is used for 6 years.
• Oil solution for external use has a shelf life of 2 years.

Camphor analogs

The drug has no analogues. Taking into account the diagnosis, the patient can be replaced with forms of Camphor, if possible. When treating heart failure, intoxication, infectious blood lesions and purulent processes in the respiratory system, only the subcutaneous method of therapy can be used.

To enhance the effect, you can try replacing Camphor with Viprosal B. An expensive substitute for the drug, since it additionally contains viper venom and turpentine. It is used only externally in the treatment of muscle diseases, radiculitis and neuralgia.

Reviews about the use of Camphor

Camphor has gained great popularity in cosmetology. Today, the drug is more often used in cosmetology , as more modern and powerful drugs have appeared for the treatment of heart and respiratory dysfunction. Camphor is also often prescribed to treat low blood pressure and apathy.

With this use, patients note a real stimulating effect, more often it is short-term in nature and requires the complex use of other medications.

When administered subcutaneously for the treatment of heart failure, breathing problems and intoxications, positive dynamics were achieved only with a combined course of therapy.

As a separate means to stabilize the patient's condition, Camphor helped only in emergency cases, after which the prescription of stronger medications was required.

Of the side effects, patients most often complained of itching and swelling at the injection site. Sometimes headaches and dizziness were noted.

Disorders such as convulsions, delirium, and live embolism are exceptional and do not have a high risk of occurrence.

Attention! If you have experience using any form of Camphor externally or internally, please share your opinion on the treatment in the comments. Report side effects. How vividly the symptoms manifested themselves, how quickly they stopped. This information is required to correctly design a course of treatment.