Finalgon® [Nicoboxyl, Nonivamide]

Pharmacological properties

Finalgon® contains two vasodilating active ingredients that are intense thermal irritants on the skin for a long time.

Nonyl vinylamide (nonivamide) is a synthetic analogue of capsaicin with analgesic properties, which when applied to the skin again leads to a decrease in the amount of substance P in peripheral pain C and A delta nerve fibers. By stimulating afferent nerve endings in the skin, nonivamide has an expanding effect on nearby blood vessels, which is accompanied by an intense, long-lasting sensation of warmth.

Nicotinic acid β-butoxyethyl ester (nicoboxyl). Nicotinic acid is a B-vitamin with vasodilating properties due to prostaglandin. Nicoboxyl causes faster and more intense hyperemia compared to nonivamide.

The combination of nonivamide and nicoboxyl has complementary vasodilating properties, which reduces the time of skin hyperemia during use.

This leads to a local increase in blood circulation. Thanks to this action, Finalgon^® provides a long-lasting soothing sensation of warmth.

Pharmacokinetics Finalgon^® applied topically, the clinical effect is manifested at the site of application of the ointment. Systemic pharmacokinetic data do not affect efficacy. Since the active substances quickly penetrate the skin, erythema and an increase in skin temperature occur several minutes after application.

Indications

For topical treatment for joint and muscle pain.

Application

For application to the skin.

Treatment should begin with a very small amount of Finalgon.^® on a very small area of ​​the skin to test individual sensitivity. In some cases, only a small amount of the drug is required to achieve the desired warming effect.

The drug is applied without difficulty, using the applicator, in an amount of not more than 0.5 cm (pea size) on the pain area (but not more than the size of the palm). When applying even a small amount of ointment, a noticeable warming effect is noted. The action of the ointment develops after a few minutes, the maximum effect appears after 20-30 minutes.

With subsequent applications, in case of good tolerance, the dose of the drug can be increased. Finalgon^® if necessary, apply up to 2-3 times a day. The maximum daily dose should not exceed 3 applications.

Mode of application. The ointment should be applied effortlessly with an applicator to the pain area.

Children. Due to insufficient data, the drug is not recommended for use in children.

Contraindications

Hypersensitivity to nonivamide or nicoboxyl or other components of the drug; very sensitive or inflamed skin; open wounds; dermatitis.

Side effects

Criteria for assessing the incidence of side effects of the drug: very often (≥1 / 10); often (≥1 / 100–1 / 10); infrequently (≥1 / 1000–1 / 100); rarely (≥1 / 10,000–1 / 1000); very rarely (1/10 000); unknown (cannot be estimated from the available data).

According to post-marketing experience as a result of the use of the drug Finalgon^® side effects may occur.

From the side of the immune system: unknown - anaphylactic reactions, hypersensitivity.

From the side of the nervous system: infrequently - paresthesia; unknown - burning sensation of the skin.

Respiratory, thoracic and mediastinal disorders: unknown - cough, dyspnea.

From the skin and subcutaneous tissue: infrequently - blisters at the site of application, local skin reaction, itching; unknown - blisters, rash, swelling of the face, urticaria.

General diseases and changes in the place of use: infrequently - a feeling of heat.

special instructions

Due to local skin hyperemia caused by the use of Finalgon® ointment, redness, sensation of warmth, itching and burning sensation at the site of application are expected.these symptoms can be especially noticeable if the amount of finalgon® used is excessive or the drug is rubbed intensively into the surface of the skin. Excessive use or rubbing of FinalGon® ointment can cause blisters on the skin.

The patient should be advised that:

• after applying Finalgon^® hands should be washed immediately with soap in order to avoid contact with other areas of the skin or transfer to other people;
• Finalgon^® Do not use on the face, eyes, or mucous membrane of the oral cavity. Transient facial edema, facial pain, conjunctival irritation, eye hyperemia, burning eyes, visual disturbances, discomfort in the oral cavity and stomatitis may appear;
• Finalgon^® should not be applied to sensitive areas of the skin (front surface of the neck, lower abdomen, inner thighs);
• the skin of people with fair hair and those with hypersensitivity can usually react more strongly, so a warming effect can be achieved even with very low doses of Finalgon^®;
• patients should not take a hot bath or shower before or after applying Finalgon^®. Redness of the skin and intense sensation of heat for several hours after applying Finalgon^® may be caused by excessive sweating or warming.

Finalgon^®, ointment, contains an auxiliary substance - sorbic acid, which can cause a local skin reaction (for example, contact dermatitis).

Use during pregnancy or lactation. Due to lack of information, do not use the drug during pregnancy or lactation.

The ability to influence the reaction rate when driving vehicles or other mechanisms. Studies have not been conducted on the ability of the drug Finalgon^® influence the management of vehicles and work with mechanisms.

Interactions

Interaction with other drugs used topically or systemically is unknown.

Overdose

Symptoms after excessive use of Finalgon®, hyperemic effects may increase, and the severity of the described side effects may increase. excessive use can be manifested mainly by the appearance of blisters on the affected areas of the skin on which finalgon® has been applied.

Since nicotinic acid ester exhibits high absorption through the skin, excessive use of Finalgon^® can cause systemic reactions, such as hyperemia of the upper body, fever, an attack of fever, hyperemia, accompanied by pain and a decrease in blood pressure.

Treatment. When using excessive amounts of Finalgon^® the severity of its effects can be reduced by lubricating the skin with a swab soaked in oil (preferably olive oil) or a greasy cream. Symptomatic therapy should be used.

Activities for random oral administration: if necessary, take activated charcoal, paraffin oil, analgesics.

Storage conditions

At a temperature not exceeding 30 ° c.

Information for healthcare professionals. Instructions for the medical use of the drug Finalgon^®. Order of the Ministry of Health of Ukraine dated September 20, 2017 No. 1116. P.S. Ministry of Health of Ukraine No. UA / 1909/01/01.

Actual information

Finalgon is an ointment used for topical treatment of joint and muscle pain. finalgon has been known since the 50s of the twentieth century, when it was offered as a warming ointment (geyer f. et al., 1956) and even as a contact gel for ultrasound studies (castellazzo m., 1958). back in the 50s of the twentieth century. the therapeutic effect of finalgon in the form of an ointment for pain syndrome of various origins has been described (geyer f. et al., 1956). the effect of the drug is provided by two substances - nonivamide, an analog of capsaicin, and nicoboxyl (beta-butoxyethyl ester of nicotinic acid).

The therapeutic effect of the active components of the drug Finalgon

Nonivamide

Capsaicinoids have been used for musculoskeletal pain for several decades.Nonivamide is a non-aggressive, antinociceptive capsaicin derivative with anti-inflammatory properties. Its analgesic and anti-inflammatory effect is realized through peripheral nociceptive fibers, inhibition of thromboxane B2, inhibition of platelet aggregation, as well as through tissue macrophages and blood mononuclear cells. In rat experiments, nonivamide inhibited bradykinin-induced pain (Yang J. M. et al., 1996). Nonivamide activates the metabolism and accelerates the rate of enzymatic reactions. Unlike capsaicin, nonivamide has a less pronounced irritant effect (subjectively, this is felt by the patient as a less pronounced burning sensation at the site of application of the drug) (Walker J. et al., 2017).

In recent years, topical drug use has become especially popular. This has been facilitated by extensive research in the field of transdermal drug delivery. As a result, an increasing number of drugs are added to the list of therapeutic agents that can be delivered to the systemic circulation through the skin. Dosage forms for topical use are creams, ointments, gels, plasters, etc. Local use of drugs is limited by the barrier properties of the stratum corneum. Nonivamide, in addition to the properties already mentioned above, has the ability to enhance the permeability of the skin, which means to improve the transdermal penetration of other medicinal substances (Parhi R. et al., 2012).

Nonivamide can be used as a means to relieve itching (Rottke N. et al., 2014).

There are studies of the properties of nonivamide that do not relate to its anti-inflammatory and analgesic effects. In an in vitro study, Austrian scientists demonstrated that nonivamide increases the release of dopamine and serotonin in SH-SY5Y cells via the TRPV1-independent pathway. The property of this substance is proposed to be used in the treatment of obesity to reduce body weight (Rohm B. et al., 2013). A recent study by a group of German and Austrian scientists found that nonivamide can contribute to weight loss when taken orally as a dietary supplement (Hochkogler C. M. et al., 2017). This effect is achieved because nonivamide stimulates Ca²⁺-dependent release of serotonin and dopamine in SH-SY5Y cells (human neuroblastoma cell line used for experimental studies).

Nonivamide is also recommended for improving blood collection for immunological studies in patients with needle phobia or for whom venous blood collection is not possible. In this case, nonivamide can be used locally before capillary blood collection to cause vasodilation and facilitate the collection of the right amount of blood. A recent study showed that the use of nonivamide does not affect the composition of immune cells contained in a capillary blood sample obtained after topical application. There were no significant differences between the experimental and control samples in the content of subpopulations of lymphocytes, monocytes or granulocytes or in the average fluorescence intensity of individual surface markers expressed on these leukocytes (Moro C. et al., 2017).

Nicoboxyl

Nicoboxyl is a derivative of nicotinic acid. It has a vasodilating effect. Also, due to its action, a significant proportion of the warming effect of the ointment is provided Finalgon (its warming effect is stronger than that of nonivamide). The therapeutic effects of nicoboxyl and nonivamide in the composition of the drug Finalgon complement and mutually reinforce each other.

Studies on topical use of a combination of nonivamide and nicoboxyl

The combination of nonivamide and nicoboxyl when applied topically causes hyperemia and increases skin blood flow and temperature. These properties were studied by a group of German researchers.In an experiment on healthy calves, optical blood spectrometry was used to determine the blood flow of the skin and muscle tissue before and after topical use of nicoboxyl with nonivamide. Optical spectroscopy was used in the visible (VIS) and near infrared (NIR) wavelengths. The study determined the effect of the cream on changes in oxygenated (ΔoxyHb) and deoxygenated (ΔdeoxyHb) hemoglobin in the skin and muscles, as well as on the oxygenation of tissues in the skin of 14 healthy calves. Topical use of nonivamide-nicoboxil cream increased capillary blood flow and increased oxygenated hemoglobin in the skin and underlying muscle tissue (Warnecke J.M. et al., 2013).

The therapeutic effects arising from the use of a combination of nonivamide with nicoboxyl have also aroused interest in plastic surgery. Studies have shown the effectiveness of postoperative treatment with this combination of transplanted skin flap preparations in order to increase its viability. Experiments were performed on rats. Topical use of nicoboxyl ointment and nonivamide ointment had a significant effect: in rats in which the transplanted skin flap was treated topically with ointment containing nicoboxyl and nonivamide as active substances, a significantly better viability of the transplanted flap and a lower frequency of ischemic necrosis in the distal portions of the transplanted skin flap were observed. Due to its simplicity and safety in use, ointment Finalgon may be clinically useful in plastic surgery, especially in combination with additional postoperative treatment (Huemer G.M. et al., 2003; Huemer G. M. et al., 2009).

The combination of nonivamide with nicoboxyl for topical use has also been investigated in sports medicine. In studies, it was found that topical application of nonivamide-nicoboxil cream to the skin of the legs in a state of rest after 15 minutes increases the content of hemoglobin saturated with oxygen (due to an increase in local blood flow in the leg muscles). This result led to the suggestion that the use of nonivamide-nicoboxil cream may increase the physical performance of athletes. However, further studies showed that the external application of nonivamide and nicoboxyl cream on the thighs of cyclists participating in the 4-km test does not improve muscle oxygen saturation (determined by infrared spectroscopy) and subjective exercise tolerance (Zinner C. et al ., 2016).

Clinical conditions in which it may be used Finalgon

According to instructions Finalgon indicated for use in muscle or joint pain. In practice, this means that it can be effective in rheumatic diseases affecting the joints (Furtenbach W., 1954), arthritis, myositis, sprains and sports injuries. Frequent indication for appointment Finalgon is pain in the lower back.

Pain in the lower back (lower back pain) is one of the most common conditions in which it is used Finalgon. Low back pain is an extremely common complaint, which is observed at least once in more than 80% of people, it affects people of all age groups. There is still no single approach to treatment. At the same time, the goals of treatment can be formulated - this is a decrease in pain intensity, improved functionality and mobility, increased physical activity (Rauck R. L. et al., 2017). Currently, there are recommendations to start therapy for pain in the lower back with the simplest and safest drugs and only if they are ineffective, go to the next stage of treatment. It is believed that there is an abuse of NSAIDs, opioid analgesics, and surgical interventions (Maher C. et al., 1998). Based on these recommendations, Finalgon is one of the drugs that can be used at the beginning of the treatment of a disease characterized by acute pain, or with an exacerbation of a disease with chronic pain.

At the same time, other researchers emphasize that the treatment of a disease characterized by an attack of acute pain should be comprehensive. Typically, therapy for lower back diseases, characterized by acute pain in the lower back, includes a change in regimen (rest is recommended), NSAIDs administered orally or as an injection, physiotherapy, and the use of topical agents in the form of ointments, gels and plasters. Among them and Finalgon. Unfortunately, people who once suffered an attack of acute back pain are at risk of recurrence of such episodes in the future. Back pain lasting more than 6 months is considered chronic. This condition leads to limited activity, psychosocial disorders, temporary disability and even disability. Examination for chronic nonspecific pain in the lower back should be aimed at identifying its pathological causes, but the latter is not always possible. Local therapy for chronic lower back pain involves an interdisciplinary approach and is aimed at maintaining function and preventing disability. It may include the use of local and systemic drugs and even surgical intervention (Golob A.L., Wipf J.E., 2014). In this case, a maintenance treatment aimed at reducing the severity of back pain and improving motor function may be prescribed for the period of remission (Patrick N. et al., 2014). Finalgon can be included in the complex therapy not only for acute, but also for chronic pain in the lower back.

Efficiency and safety Finalgon with nonspecific pain in the lower back has been shown in many studies. Let us dwell on some of them. The fact that the combination of nicoboxyl with nonivamide effectively and safely reduces the severity of acute nonspecific lower back pain was confirmed by a randomized study involving 138 patients aged 21–68 years. Topical application of Nicoboxyl / Nonivamide Cream (Finalgon) not only significantly reduced the intensity of pain compared with placebo, but also an improvement in mobility with good tolerability of the drug (Blahova Z. et al., 2016). In 2016, a group of European scientists conducted a study of the efficacy, tolerability and safety of the use of nicoboxyl and nonivamide in the form of an ointment in patients with pain in the lumbar region. The intensity of pain was chosen as the primary endpoint in the study, namely the difference between the initial level and 8 hours after the first use of the ointment containing nicoboxyl 2.5% and nonivamide 0.4% as active substances. The study involved 804 patients aged 18–74 years. According to the results of the study, conclusions were made about the high efficiency of the use of ointments containing nicoboxyl and nonivamide, compared with placebo. During treatment, patients received not only a pronounced decrease in the severity of pain, but also a noticeable improvement in mobility in the lower back. Patients subjective assessment of treatment efficacy was also higher in patients in the group of ointment containing nicoboxyl and nonivamide than in the placebo group. The drug was well tolerated. No serious side effects associated with treatment have been reported (M. Gaubitz et al., 2016).

findings

Finalgon - An effective and safe warming and analgesic for topical use. A large number of studies have been devoted to the study of its action and tolerability, as well as to the study of the action of its components. As with any drug, there are contraindications, as well as the occurrence of side effects. Therefore, before starting therapy, a doctor’s consultation is necessary.