Cancer treatment: the search for new drugs continues. There is hope! How to use diclofenac for oncology, does the drug really help against cancer How to inject Diclofenac injections correctly, dosage for oncology

The international project Repurposing Drugs in Oncology (ReDO) found a significant anti-cancer effect in the well-known analgesic and anti-inflammatory drug diclofenac. The results of the work are published in ecancermedical science.

Diclofenac belongs to non-steroidal anti-inflammatory drugs (NSAIDs), which have long interested scientists as potential means of preventing cancer. It turned out that diclofenac can be used in the treatment of already developed tumors.

ReDO staff conducted a meta-analysis of works on the antitumor effect of diclofenac and concluded that this effect can be considered undoubted. Due to the well-studied pharmacokinetics, relatively low toxicity and low cost of the drug, scientists have classified it as a strong candidate for use as a chemotherapy agent.

The first study of the anticancer properties of the drug in an animal model dates back to 1983, when it was tested on rats with implanted fibrosarcoma - a slowdown in tumor growth was recorded. More recent animal and human cell culture studies have shown that diclofenac can inhibit cancer cell division in colon and rectal cancer, neuroblastoma, ovarian cancer, glioma, pancreatic cancer, melanoma, and prostate cancer.

Since diclofenac is used for pain relief in oncological diseases and after operations for them, several retrospective studies have been conducted comparing the results of treatment in patients who received and did not receive diclofenac. It turned out that the administration of the drug statistically significantly reduced the likelihood of distant metastasis and overall mortality in patients with tumors of the breast, lung and kidney; sharply reduced the concentration of CA 19-9 (a biomarker of pancreatic adenocarcinoma) in the blood and slowed down the progression of the disease, and also significantly reduced the size of neoplasms in aggressive fibromatosis.

According to scientists, the antitumor effects of diclofenac are diverse. First of all, they are associated with its direct action as an inhibitor of cyclooxygenase (COX), in particular its second type. This enzyme synthesizes prostaglandins. One of them, prostaglandin E2, is found in a variety of neoplasms, where it maintains chronic inflammation by forming the tumor microenvironment. The effect of different NSAIDs on COX-2 varies greatly, and diclofenac binds to it especially well.

In addition, the antitumor activity of diclofenac may be responsible for its effects such as suppression of the growth of tumor-feeding vessels, immunomodulation, stimulation of apoptosis (natural cell death that is disturbed in cancer), suppression of platelet activity and glucose metabolism, as well as an increase in the sensitivity of cancer cells to radiation and chemotherapy. .

The collected data have aroused serious scientific interest in the anticancer properties of diclofenac, and four clinical trials are currently underway for this indication, with one of them already in phase IIB (in which the effectiveness of the drug at a given dose is being investigated).

ReDO is an international project designed to find anti-cancer properties in drugs that are or have been used for other indications. Preference is given to drugs that are widely available and inexpensive.

Diclofenac is a "classic" analgesic and anti-inflammatory drug developed and brought to market in 1973 by Ciba-Geigy, now part of Novartis. It is widely used for various pains, rheumatoid diseases, lesions of the musculoskeletal system and keratoses. Available in tablets, suppositories, injections, ointments and eye drops, in a number of countries it is available without a prescription.

Cancer Pain Assessment

The level of pain can only be adequately assessed by the one who experiences it. In addition, patients experience different sensations: drilling, cutting, tingling, pulsation, burning, etc. In order for these experiences to be better understood by the doctor, they use a visual scale of pain levels (see Fig.).

Pain scale from 0 to 10

According to the origin of pain in oncology, there are:

Visceral pain. With neoplasms in the abdominal cavity. Sensations of squeezing, fullness, pain aching or dull, not having a clear localization.
Somatic pain. Develop in vessels, joints, bones, nerves. Continuous, dull pain.
neuropathic pain. Occur when the nervous system is damaged: central and peripheral.
Psychogenic pain. They appear against the background of depression, fear, self-hypnosis, without any organic damage, as a rule, painkillers do not help here.

Causes and mechanism of pain in cancer

As the tumor grows and increases in size, it puts pressure on nearby tissues and organs, irritating peripheral nerve receptors. In oncology of the last stage, when the body is affected by metastases, pain can be caused by a malfunction in the brain and all vital organs.

The causes depend on the etiology of pain:

Somatic - formed when blood vessels, tendons and ligaments, nerves are damaged. The pain is dull, muffled, but constant.
Psychogenic - are formed against the background of emotional fading, when a person realizes the inevitability of his situation. Pain of various localization and intensity, which cannot be eliminated with the help of drug therapy.
Visceral - associated with tumors in the sternum and peritoneum. Accompanied by a feeling of fullness, do not have a clear localization (diffuse pain).
Neuropathic - are formed with lesions of the central and peripheral nervous system.

The mechanism of pain development is associated with irritation of nerve receptors and incorrect perception of information, in response to which the brain forms a pain attack.

Cancer patients suffer a lot and suffer. Death does not come from the progression of the cancer itself, but from the inability to endure the torment and exhaustion of the body. Medicines can help relieve this condition.

What to do?

If the oncology is confirmed histologically, there is a diagnosis and the patient is observed by an oncologist:

at the inpatient stage, the department in which the person is operated on or treated is responsible for anesthesia,
if the patient is observed by a therapist in the clinic, and in the oncology clinic by an oncologist or transferred for observation to the doctor of the antitumor office of the clinic, he should, along with all the extracts and medical records, contact an analgist (most often in an oncology clinic). This should be done even if there is no pain. The analgist paints a step-by-step scheme of anesthesia, which the doctor observing the patient will adhere to.

If the cancer has not yet been confirmed - there is no diagnosis confirmed by histology, but there is pain - it is also worth contacting an analgist and getting recommendations fixed in writing in the medical documentation (entry in the outpatient card, extract).

If you have not yet been treated to an analgist, but there is pain, contact your local therapist. It is in his power to prescribe non-narcotic analgesics and concomitant drugs that relieve or relieve pain.
If non-narcotic analgesics were previously used, but their effect is not enough, you should immediately get the recommendations of the analgologist, with which they turn to the therapist at the place of residence, less often - to the doctor of the antitumor office of the polyclinic.

Without a prescription at the pharmacy today, you can only get non-steroidal anti-inflammatory drugs (below there is an instruction on how to get the necessary painkillers for a cancer patient in a timely manner).

Pain levels and drugs

The choice of this or that medicine depends on the degree of discomfort. Each patient has their own pain threshold, which is a purely individual indicator. Therefore, the doctor selects those drugs that can relieve pain in a particular patient.

Analgesics from the NSAID group are prescribed, which cope with pain, fever, swelling. The most effective of them are:

Analgin;
Nimesulide;
Paracetamol.

Nimesulide - one of the types of painkillers for oncology

They are used in the form of tablets, starting with minimal dosages. The course of administration is designed so that the therapeutic effect is achieved with the accumulation in the body of all the substances of the drug. The choice of dose depends on age, body weight and tendency to allergic reactions.

Since the tablets are absorbed from the digestive tract, they are taken after a meal. Metabolism by liver cells dictates the need to take hepatoprotectors in parallel.

Papaverine can enhance the effectiveness of NSAID preparations, which stops vasospasm and promotes the active absorption of trace elements of the drug.

As auxiliary drugs that are prescribed to reduce the load on all organs and systems, are:

Corticosteroids - improve appetite and enhance the analgesic effect.
Anticonvulsants - prevent spasm of blood vessels and smooth muscles.
Antipsychotics - stop attacks of nausea and vomiting, enhancing the analgesic effect.
Muscle relaxants of central action - relax the body, normalizing sleep.

The need to use this or that drug is due to the peculiarities of the course of oncological disease.

Non-steroidal anti-inflammatory drugs are not able to anesthetize to the desired state, therefore weak opioid preparations containing narcotic substances are prescribed. Their principle of action is based on the impact on the centers of pain formation in the brain, which causes a complete absence of discomfort in the body.

Recently, Tramadol has been used in the treatment of cancer patients. Now they are inclined to use the medicine Zaldiar, which contains minimal doses of an opioid in combination with Paracetamol, which makes it possible to achieve a complex therapeutic effect.

Tramadol can be administered simultaneously with Diphenhydramine as an injection. This will speed up the pain relief process and reduce the load on the digestive tract.

When the patient is on the verge, it is necessary to normalize the condition as quickly as possible. To do this, use drugs such as:

Pyritramide;
Tramadol;
Fentonyl;
Morphine.

The last drug is the fastest. Its therapeutic efficacy persists for 5-6 hours.

Opioid analgesics are combined with non-opioid analgesics to achieve the maximum analgesic effect.

The key disadvantage of all opioids is addiction. The cells of the body can no longer exist without a medicine that relieves pain. Drug dependence develops, which disappears only after the onset of death.

Standard pain therapy regimens

At each examination of an oncological patient, the attending physician evaluates his subjective sensation of pain and, in prescribing painkillers, moves up a three-step ladder from bottom to top. You don't have to go through the steps sequentially. The presence of severe unbearable pain immediately suggests a transition to stage 3.

Stage 1 - mild pain Stage 2 - severe pain Stage 3 - unbearable pain

Choice of route of drug administration

Tablets for oncology and capsules are almost always convenient, except for cases of difficulty swallowing (for example, with cancer of the stomach, esophagus, tongue).
Skin forms (patches) allow the drug to be gradually absorbed without irritation of the mucous membranes of the gastrointestinal tract and sticking the patch once every few days.
Injections are more often performed intradermally or (when there is a need for rapid pain relief) intravenously (for example, bowel cancer).

For any route of administration, the selection of dosages and frequency of drug administration is carried out individually with regular monitoring of the quality of anesthesia and the presence of an undesirable effect of substances (for this, an examination of the patient is indicated at least once every ten days).

Pain injections are represented by: Tramadol, Trimeperidine, Fentanyl, Buprenorphine, Butorphanol, Nalbufinlm, Morphine.
Combined agent: Codeine Morphine Noscapine Papaverine hydrochloride Thebaine.

Non-injectable options for opioid pain medications:

Tramadol in capsules of 50 mg, tablets of 150, 100, 200 milligrams, rectal suppositories of 100 milligrams, oral drops,
Paracetamol Tramadol capsules 325 mg 37.5 milligrams, coated tablets 325 mg 37.5 middigrams,
Dihydrocodeine extended-release tablets 60, 90, 120 mg,
Propbuccal tablets 20mg
Buprenorphine skin patch 35mcg/hour, 52.5mcg/hour, 70mcg/hour,
Buprenorphine Naloxone sublingual tablets 0.2 mg/0.2 mg,
Oxycodone Naloxone long-acting tablets 5 mg / 2.5 mg; 10 mg / 5 mg; 20 mg / 10 mg; 40 mg / 20 mg,
Extended release tapentadol tablets 250, 200, 150, 100 and 50 milligrams,
trimeperidine tablets,
Fentanyl skin patch 12.5; 25; 50, 75 and 100 mcg/hour, sublingual tablets.
Morphine extended release capsules 10, 30, 60, 100 milligrams, extended release tablets 100, 60, 30 milligrams.

In the case when there are no problems with the gastrointestinal tract and liver, it is recommended to use tablets for oral administration. To reduce irritation of the gastric mucosa, the drug Omeprazole is prescribed in parallel.

Injections can reduce pain in the shortest possible time. The first noticeable results appear 3-5 minutes after administration, which is effective for acute pain attacks.

In some cases, patches with an anesthetic effect may be prescribed. They are attached to the skin, through which the process of slow absorption of the drug takes place. The therapeutic effect is manifested by the accumulative system, when there is enough analgesic in the body.

In the presence of moderate and persistent pain, tablets can be combined with injections to achieve maximum effect. The choice of the most optimal means and method of administration into the body depends on the recommendations of the doctor.

In the event that the opioid drug has ceased to give the desired effect, it can be replaced with an analogue. The initial dose should be slightly lower than that which was used before.

If the therapeutic effect is completely absent, the doctor must be informed about this. Treatment is being adjusted and some medications are being replaced.

First step - mild pain

At the first stage of anesthesia in oncology, there are non-steroidal anti-inflammatory drugs with an analgesic effect (Ibuprofen, Ketoprofen, Diclofenac, Celecoxib, Lornoxicam, Nimesulide, Etoricoxib, Meloxicam) or Paracetamol.

Start with the minimum dose (see table) with a gradual increase if necessary.
Since the effect of painkillers is cumulative, not instantaneous, the initial dose should not be exceeded for several days.
You need to start with tablet forms, then move on to injections. With contraindications to oral administration or the effect of the tablets is low, it is necessary to administer painkillers intramuscularly.
Take tablets after meals, under the cover of Omeprazole and its analogues, you can drink milk, in order to avoid damage to the gastric mucosa.

For all types of cancer pain, except bone:

Ketanov (or more effective Ketorol), in a separate syringe.
Papaverine to enhance efficiency. If the patient smokes, then papaverine will be ineffective.

For bone pain:

Neither papaverine nor Ketanov can be compared in effectiveness with bone pain with Piroxicam, Meloxicam, Xefocam. Choose one of the drugs and inject in a separate syringe.
In case of primary bone tumors or metastases in them, it is advisable to discuss with the doctor the use of bisphosphonates, radiopharmaceuticals, Denosumab. In addition to pain relief, they also have a therapeutic effect.

If the patient does not suffer from low blood pressure and the body temperature is normal, then Relanium, Sibazol are indicated.

anticonvulsants- Carbomazepine, Pregabalin (Lyrica), Lamotrigine,
central muscle relaxants- Gabapentin (Tebantin),
tranquilizers- Clonazepam, Diazepam, Imipramine. They improve sleep, have a sedative effect, enhance the effect of narcotic analgesics.
corticosteroids- Prednisolone, Dexamethasone. They increase appetite, in combination with painkillers they give an effect on pain in the spine, bones, pains of internal organs.
neuroleptics - Galaperidol, Droperidol, enhance analgesics and are antiemetic.
anticonvulsants- Clonazepam, effective for shooting pains, enhances narcotic analgesics.

Painkillers for oncology at home

In the event that palliative treatment is carried out at home, it is necessary:

Indicate the person who will give the medicine to the patient in accordance with the doctor's prescription. This person should be adequate and responsible for possible negative manifestations.
Obtain medicines and the recommended dosage according to which the drug should be administered to the patient.
Comply with all rules and regulations regarding patient care.

It is strictly forbidden to leave medicines, especially opioid-type drugs, in close proximity to a cancer patient. Under the influence of panic and addiction, a person can use all the pills at one time, which will provoke the development of a fatal outcome. Medicines are best stored in a locker box, where only one person who is responsible for the patient's health has access.

Medicines are taken according to the doctor's prescription. It is not recommended to change dosages on your own, cancel the medication or replace it with an analogue, as this can adversely affect the patient's health.

Some patients who suffer from psychiatric disorders may mimic medication. This dictates the need to use only the injection method of introducing drugs into the body.

Stage three - severe pain

Because first-line drugs become ineffective Paracetamol (or non-steroidal anti-inflammatory drugs) in combination with weak opioids (codeine-containing or Tramadol) is required.

With such pains, pills are more often prescribed for oncology:

Tramadol - it is prescribed in the first place, just when non-narcotic painkillers are already helping. It is taken either as a tablet (often causing nausea) or as an injection. Together with NSAIDs (Paracetamol, Ketorol). Tramadol should not be taken together with narcotic analgesics and with MAO inhibitors (Fenelzine, Iproniazid, Oklobemide, Selegiline).
Zaldiar is a complex preparation of Tramadol and Paracetamol.

Tramadol Relanium (in different syringes)
Tramadol and Diphenhydramine (in one syringe)
Codeine Paracetamol (max daily intake 4-5 thousand mg).

To achieve an effect and at the same time reduce pain with as few drugs as possible, you need to combine Codeine or Tramadol with other NSAIDs (Paracetamol, Ketorol, etc.).

Further, it is possible to prescribe Paracetamol with small doses of Fentanyl, Oxycodone, Buprenorphine, which are strong opioid analgesics. The combination is reinforced with adjuvant therapy from the first stage.

For severe pain or constant pain, such as stage 4, high doses of Tramadol or Codeine no longer help. A cancer patient needs strong opioids in combination with paracetamol and auxiliary muscle relaxants or tranquilizers.

Morphine is a drug that is prescribed in oncology for unbearable pain. In addition to the analgesic effect, it also has all the side effects of a strong drug (addiction, addiction), after its use there will be nothing to help, there will be no choice of means. Therefore, the transition from weak (Tramadol) to stronger ones should be very carefully considered.

List of narcotic painkillers from weaker to stronger:

Tramadol - according to some sources, it is considered a synthetic analogue of drugs, according to other non-narcotic analgesics.
Trimeperidine - in tablet forms, the effect is 2 times lower than injectables, there are fewer side effects compared to Morphine.
Buprenorphine is slower to develop tolerance and dependence than morphine.
Pyritramide - the action is very fast (1 minute), compatible with neurotropic drugs.
Fentonyl is more convenient, painless and effective to use in a patch, rather than intramuscularly or intravenously.
Morphine - the effect occurs after 5-10 minutes.

The doctor should offer these drugs to the patient, but as a rule, the patient's relatives need to take the initiative and discuss with him the possibility of using less powerful opiates than Morphine after non-narcotic drugs.

How to get painkillers

The appointment of light opioids is signed by the chief medical officer once, then a second discharge can be made by the doctor himself. The re-starter looks at the arguments for changing the dose or switching to another drug (for example, amplification).

Today, if there is a normal recommendation of an alnalgologist (stepwise increase in therapy), then they move along it and no one waits for anything for a long time:

They inject Ketorol, less often Diclofenac, then immediately switch to Tramadol (with increased pain).
Three times taking Tramadol in combination with paracetamol and Gabapentin without effect - they switch to Durgesic (Fentanyl).
After increasing the dosage to the maximum or the impossibility of using patches, they switch to morphine.

Cutaneous options - fentanyl and buprenorphine pain relief patches are the preferred alternative to oral opioids. It is a strong pain reliever with a gradual release of the drug. The question of their appointment rests on the price tag and availability.

If the patient has a disability group, and he is entitled to preferential drug coverage

the issue of extracting the same Fentanyl (Dyurgesic) is carried out at the place of residence by the local therapist or surgeon of the antitumor office (if there are recommendations from the analgologist, filling out the documentation - a preferential prescription and a copy of it signed by the head of the medical institution at the initial discharge of the drug). In the future, the local therapist can prescribe the medication on his own, turning to the help of the chief medical officer only when adjusting dosages.

In the case when a person with a disability has refused drug provision and receives monetary compensation for it

he can start getting the required pills, capsules or patches free of charge. It is necessary to obtain a free-form certificate from the local doctor about the need for expensive therapy indicating the drug, its dose and frequency of use, stamped by the doctor and the medical institution, which must be submitted to the Pension Fund. Preferential drug coverage is restored from the beginning of the month following the submission of the certificate.

Non-steroidal anti-inflammatory drugs are freely available and purchased at a pharmacy. Opioid analgesics are handed out only with the approval of the head of the medical unit of the polyclinic. To do this, the patient or his relatives write a statement in which they ask for the appropriate medicines.

Such a scheme is quite long, therefore, in some cases, they resort to the help of the attending physician, whose actions are based on the gradual use of medications, taking into account the intensity of pain. The prescription of drugs is carried out only once. First, drugs of the NSAID group are administered, after which a small dose of Tramadol is added. The frequency of taking drugs - 3 times a day.

With increased pain, Tramadol is prescribed 2 times a day, supplementing it with Paracetamol. The advanced forms of the oncological process and unbearable pain dictate the need for the introduction of Fentanyl and Morphine.

In the future, the attending physician has the right to independently prescribe the required amount of pain medication, which is controlled by the head of the medical unit. Medicines are handed out only to relatives. Preferential queues for receiving medicines are issued through the Department of Labor and Social Protection of the Population.

Cancer continues to be one of the leading causes of death worldwide. Despite numerous studies in this area, the mechanism leading to the transformation of healthy cells into malignant ones is not yet known to specialists. The search for effective cancer treatments continues. What can modern medicine offer?

Diclofenac as a cure for cancer

Recently, ecancermedicalscience published the results of a study investigating previously unknown properties of a popular pain reliever. The studies were initiated by the International Project Repurposing Drugs in Oncology (ReDO). The data obtained allow us to state: Diclofenac can be used as an effective anticancer drug.

Diclofenac belongs to the group of non-steroidal anti-inflammatory drugs. It was developed in the 70s of the last century and has traditionally been used as an analgesic and anti-inflammatory agent for rheumatoid diseases, problems with the musculoskeletal system, pain syndrome of various etiologies.

Experts became interested in Diclofenac as a means of preventing and treating various types of cancer more than 30 years ago. Studies have been carried out on an animal model. The drug was administered to experimental mice with fibrosarcoma. At the same time, a significant slowdown in tumor growth was recorded. Research has been continued. It turned out that Diclofenac is able to suppress the division of malignant cells also in ovarian cancer, pancreatic cancer, melanoma, glioma, rectal and colon cancer, neuroblastoma.

The results of new studies show that such therapy can be quite effective. The advantages of the drug are its low toxicity, well-studied pharmacokinetics and low cost.

Diclofenac is often used as an analgesic for cancer and after surgery to remove a tumor. The results of the analysis of data from patients who underwent such therapy revealed a number of positive changes in them, including:

Decreased mortality rates and the risk of metastasis in tumors of the breast, kidneys, and lungs.
Reducing the size of the tumor in aggressive fibromatosis.
Slowing the progression of pancreatic adenocarcinoma.

Scientists believe that the anti-cancer properties of Diclofenac are associated with six main factors:

The drug inhibits a special enzyme synthesized by prostaglandins - an inhibitor of cyclooxygenase of the second type. Prostaglandin E2 has been found in a number of tumors. It supports chronic inflammation, thereby forming a tumor microenvironment.
Diclofenac produces an immunomodulatory effect.
The drug inhibits the growth of blood vessels that supply the tumor with nutrients.
It activates apoptosis of cancer cells (regulated process of programmed cell death).
The tool helps to increase the sensitivity of cancer cells to chemotherapy and radiation therapy.

Based on the data obtained, scientists express hope that Diclofenac can be used as a fairly effective anticancer agent in the near future.

The benefits of ionized air in oncological diseases

In the middle of the last century, scientists discovered that air with a high content of air ions inhibits the growth of transplanted tumors in animals. Later, the same effect was found in cancer patients. For example, 10-20 sessions of aerotherapy led to a significant reduction in the size of the tumor or its complete disappearance in women suffering from mastopathy.

Russian scientist A.L. Chizhevsky at one time suggested that there is a definite connection between the development of malignant neoplasms and the systematic lack of air ions in the air. Deficiency of air ions creates a background for disruption of electrical exchange, a decrease in the electrical potential of cells, leads to early aging of the body and the formation of neoplasms.

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Ionizes water.

Improves pH level

Saturates with oxygen.

Structures water for better absorption by the body.

Immunotherapy in the treatment of cancer

Today, experts focus on the search for safe methods of cancer treatment. In addition to the traditional ones (surgery, chemotherapy, radiation therapy), other techniques are also used.

Immunotherapy is one of the most promising areas. Modern medicine offers a number of activities carried out to maintain the functioning of the immune system, strengthen immunity.

Vaccination. Two types of vaccines are used: to prevent disease and to treat an already developed disease. They are produced on the basis of malignant cells removed from the body.
Preparations based on cytokines. Cytokines are special proteins through which information is transmitted from one cell to another.
T cells. These specific cells are highly active in fighting cancer.
Monoclonal antibodies, deoxynate, thymogen. These medicines activate the immune system for the body to fight the disease on its own. In addition, they help to eliminate toxic substances from the body.
5.TIL cells. They are isolated from cancerous tissues and injected into the body after reproduction in the laboratory. The technique is aimed at preventing the recurrence of cancer.
Natural methods of immunotherapy. Scientists advise using natural organic products that help improve the functioning of the immune system. However, they warn of the need to continue conventional treatment. In other words, natural products enriched with vitamins, herbal remedies can only be used as part of adjuvant therapy.

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Attention! Cancer patients should be under mandatory medical supervision. The use of any additional funds is possible only simultaneously with the treatment prescribed by specialists.

Both acute and chronic types of pain require medical assistance. Chronic pain syndrome in oncological diseases has its own characteristics:

It can develop in a short time (due to compression of the nerve trunks by a growing tumor or rapid massive destruction of the organ).
It can exist almost constantly due to overstimulation of the nervous system.
It can persist even after the elimination of its source (due to breakdowns in the system of inhibition of nerve impulses).

Therefore, even at the stage of the absence of any sensations, but the existing proven diagnosis of a malignant neoplasm, a tactic of phased anesthesia should be developed - from weak to strong drugs.

By the time the pain appears or begins to intensify, the doctor and the patient should be armed with a ready-made strategy that can be applied specifically to this cancer patient, observing the necessary timing for increasing drug dosages or enhancing the analgesic effect.

Cancer Pain Assessment

Pain scale from 0 to 10

According to the origin of pain in oncology, there are:

Visceral pain. With neoplasms in the abdominal cavity. Sensations of squeezing, fullness, pain aching or dull, not having a clear localization.
Somatic pain. Develop in vessels, joints, bones, nerves. Continuous, dull pain.
neuropathic pain. Occur when the nervous system is damaged: central and peripheral.
Psychogenic pain. They appear against the background of depression, fear, self-hypnosis, without any organic damage, as a rule, painkillers do not help here.

What to do?

If the oncology is confirmed histologically, there is a diagnosis and the patient is observed by an oncologist:

at the inpatient stage, the department in which the person is operated on or treated is responsible for anesthesia,
if the patient is observed by a therapist in the clinic, and in the oncology clinic by an oncologist or transferred for observation to the doctor of the antitumor office of the clinic, he should, along with all the extracts and medical records, contact an analgist (most often in an oncology clinic). This should be done even if there is no pain. The analgist paints a step-by-step scheme of anesthesia, which the doctor observing the patient will adhere to.

If you have not yet been treated to an analgist, but there is pain, contact your local therapist. It is in his power to prescribe non-narcotic analgesics and concomitant drugs that relieve or relieve pain.
If non-narcotic analgesics were previously used, but their effect is not enough, you should immediately get the recommendations of the analgologist, with which they turn to the therapist at the place of residence, less often - to the doctor of the antitumor office of the polyclinic.

Standard pain therapy regimens

Stage 1 - mild pain Stage 2 - severe pain Stage 3 - unbearable pain

Stage one - mild pain

Cancer pain pills

Injections at the first stage

For all types of cancer pain, except bone:

Ketanov(or more efficient Ketorol) in a separate syringe.
Papaverine to enhance efficiency. If the patient smokes, then papaverine will be ineffective.

For bone pain:

Neither papaverine nor Ketanov can be compared in effectiveness with bone pain with Piroxicam, Meloxicam, Xefocam. Choose one of the drugs and inject in a separate syringe.
In case of primary bone tumors or metastases in them, it is advisable to discuss with the doctor the use of bisphosphonates, radiopharmaceuticals, Denosumab. In addition to pain relief, they also have a therapeutic effect.

If the patient does not suffer from low blood pressure and the body temperature is normal, then Relanium, Sibazol.

The above funds can be supported by auxiliary

anticonvulsants- Carbomazepine, Pregabalin (Lyrica), Lamotrigine,
central muscle relaxants- Gabapentin (Tebantin),
tranquilizers- Clonazepam, Diazepam, Imipramine. They improve sleep, have a sedative effect, enhance the effect of narcotic analgesics.
corticosteroids- Prednisolone, Dexamethasone. They increase appetite, in combination with painkillers they give an effect on pain in the spine, bones, pains of internal organs.
neuroleptics - Galaperidol, Droperidol, enhance analgesics and are antiemetic.
anticonvulsants- Clonazepam, effective for shooting pains, enhances narcotic analgesics.

The second stage - moderate to severe pain

Because first-line drugs become ineffective Paracetamol (or non-steroidal anti-inflammatory drugs) in combination with weak opioids (codeine-containing or Tramadol) is required.

With such pains, pills are more often prescribed for oncology:

Tramadol - it is prescribed in the first place, just when non-narcotic painkillers are already helping. It is taken either as a tablet (often causing nausea) or as an injection. Together with NSAIDs (Paracetamol, Ketorol). Tramadol should not be taken together with narcotic analgesics and with MAO inhibitors (Fenelzine, Iproniazid, Oklobemide, Selegiline).
Zaldiar is a complex preparation of Tramadol and Paracetamol.

Tramadol + Relanium (in different syringes)
Tramadol and Diphenhydramine (in one syringe)
Codeine + Paracetamol (max daily intake 4-5 thousand mg.).

To achieve an effect and at the same time reduce pain with as few drugs as possible, you need to combine Codeine or Tramadol with other NSAIDs (Paracetamol, Ketorol, etc.).

Further, it is possible to prescribe Paracetamol with small doses of Fentanyl, Oxycodone, Buprenorphine, which are strong opioid analgesics. The combination is reinforced with adjuvant therapy from the first stage.

Stage three - severe pain

List of analgesics that are desirable to use before Morphine:

List of narcotic painkillers from weaker to stronger:

Tramadol - according to some sources, it is considered a synthetic analogue of drugs, according to other non-narcotic analgesics.
Trimeperidine - in tablet forms, the effect is 2 times lower than injectables, there are fewer side effects compared to Morphine.
Buprenorphine is slower to develop tolerance and dependence than morphine.
Pyritramide - the action is very fast (1 minute), compatible with neurotropic drugs.
Fentonyl is more convenient, painless and effective to use in a patch, rather than intramuscularly or intravenously.
Morphine - the effect occurs after 5-10 minutes.

The doctor should offer these drugs to the patient, but as a rule, the patient's relatives need to take the initiative and discuss with him the possibility of using less powerful opiates than Morphine after non-narcotic drugs.

Choice of route of drug administration

Tablets for oncology and capsules are almost always convenient, except for cases of difficulty swallowing (for example, with cancer of the stomach, esophagus, tongue).
Skin forms (patches) allow the drug to be gradually absorbed without irritation of the mucous membranes of the gastrointestinal tract and sticking the patch once every few days.
Injections are more often performed intradermally or (when there is a need for rapid pain relief) intravenously (for example, bowel cancer).

injections

Pain injections are represented by: Tramadol, Trimeperidine, Fentanyl, Buprenorphine, Butorphanol, Nalbufinlm, Morphine.
Combined agent: Codeine + Morphine + Noscapine + Papaverine hydrochloride + Thebaine.

Tablets, capsules, drops, patches

Non-injectable options for opioid pain medications:

Tramadol in capsules of 50 mg, tablets of 150, 100, 200 milligrams, rectal suppositories of 100 milligrams, oral drops,
Paracetamol + Tramadol capsules 325 mg + 37.5 milligrams, coated tablets 325 mg + 37.5 middigrams,
Dihydrocodeine extended-release tablets 60, 90, 120 mg,
Propbuccal tablets 20mg
Buprenorphine skin patch 35mcg/hour, 52.5mcg/hour, 70mcg/hour,
Buprenorphine + Naloxone sublingual tablets 0.2 mg/0.2 mg,
Oxycodone + Naloxone long-acting tablets 5 mg / 2.5 mg; 10 mg / 5 mg; 20 mg / 10 mg; 40 mg / 20 mg,
Extended release tapentadol tablets 250, 200, 150, 100 and 50 milligrams,
trimeperidine tablets,
Fentanyl skin patch 12.5; 25; 50, 75 and 100 mcg/hour, sublingual tablets.
Morphine extended release capsules 10, 30, 60, 100 milligrams, extended release tablets 100, 60, 30 milligrams.

How to get painkillers

Today, if there is a normal recommendation of an alnalgologist (stepwise increase in therapy), then they move along it and no one waits for anything for a long time:

They inject Ketorol, less often Diclofenac, then immediately switch to Tramadol (with increased pain).
Three times taking Tramadol in combination with paracetamol and Gabapentin without effect - they switch to Durgesic (Fentanyl).
After increasing the dosage to the maximum or the impossibility of using patches, they switch to morphine.

If the patient has a disability group, and he is entitled to preferential drug coverage

In the case when a person with a disability has refused drug provision and receives monetary compensation for it

To receive Fentanyl in a patch, the patient must:

Contact the pharmacy in person or fill out a power of attorney in the name of a relative in a medical institution.
As before initiating other therapy, the individual is asked to complete informed consent before initiating therapy.
The patient is given instructions on how to use the skin patch.
Disability in oncological pathology should be started from the moment the diagnosis is verified and the results of histology are received. This will make it possible to use all the possibilities of pain therapy by the time the chronic pain syndrome appears and its progression.
In the absence of opportunities to get a skin patch for pain relief for free or buy it for one's own money, a person is offered morphine in one of the dosage forms. Injectable forms of Morphine are also prescribed if it is impossible to provide the patient with non-parenteral forms of opioids. Injections are performed by SPs or hospice workers in the patient's area of residence.
All cases of undesirable effects of the drugs received or incomplete pain suppression should be reported to your therapist. He will be able to correct the treatment, change the treatment regimen or dosage forms.
When switching from one opioid to another (due to inefficiency, side effects), the initial dosage of the new drug is chosen slightly lower than that shown in order to avoid dose summation and overdose phenomena.

Thus, adequate analgesic therapy for cancer patients in the Russian Federation is not only possible, but also available. It is only necessary to know the procedure and not to waste precious time, showing forethought.

Since ancient times, the relationship between pain and inflammation has been known. And today, the most common drugs for pain relief are drugs that have both anti-inflammatory and analgesic effects - non-steroidal anti-inflammatory drugs (NSAIDs).

The history of the creation of diclofenac

The prototype of modern NSAIDs was acetylsalicylic acid, which was first synthesized by a young scientist Felix Hoffman at the end of the 19th century. The chemical structure and properties of acetylsalicylic acid became the guidelines by which new representatives of this class of medicines were created (at first they were usually referred to as "aspirin-like"). Not so much the lack of effectiveness as the toxicity of high doses of acetylsalicylic acid served as a powerful incentive for the development of new, "non-salicylate" NSAIDs. In 1966, during the implementation of the program for the development of an anti-inflammatory drug with improved biological properties in the Geigy research laboratory, more than 200 analogs of 0-aminoacetic acid were synthesized to create a molecule with the necessary parameters, among which the most interesting results were shown by diclofenac sodium - sodium salt 0 -[(2,6 dichlorophenyl)-amino]-phenyl-acetic acid.

Initially, diclofenac was used mainly in the treatment of rheumatological diseases, where both components are important: a pronounced anti-inflammatory and powerful analgesic effect, but, subsequently, the scope of diclofenac has expanded significantly. Currently, diclofenac is used in surgery, traumatology and sports medicine (for lesions of the musculoskeletal system, soft tissue damage (bruises, sprains), for postoperative pain relief), in neurology (for the treatment of back pain, tunnel syndromes, migraine), in gynecology in dysmenorrhea, adnexitis, in oncology as a means of the first stage of anesthesia of the WHO ladder. Intramuscular administration of diclofenac sodium is an effective method of combating renal and hepatic colic. A special dosage form of diclofenac in the form of drops has found application in ophthalmology. General practitioners also prescribe diclofenac for various pain syndromes (Table 1).

The mechanism of action of diclofenac

The analgesic effect of diclofenac is due to several mechanisms. The main mechanism of action of diclofenac is the suppression of cyclooxygenase (COX) - an enzyme that regulates the conversion of arachidonic acid into prostaglandins - mediators of inflammation, pain, fever.

Diclofenac and COX selectivity

In the early 1990s, two isoforms of the COX enzyme, COX-1 and COX-2, were discovered. Most of the positive effects of NSAIDs (suppression of inflammation, pain, fever) are associated with COX-2 inhibition, and the development of adverse reactions (mainly in the form of damage to the gastrointestinal tract) is associated with suppression of COX-1 synthesis.

However, there are a number of exceptions to this rule. It has been shown that COX-1 may also play a role in the development of the inflammatory process. COX-1, together with COX-2, is produced by the synovium of patients with rheumatoid arthritis (RA). This is probably associated with the lower efficiency of selective COX-2 in some pain syndromes. Recent studies have found an increased risk of cardiovascular complications with the use of highly selective COX-2 inhibitors.

Diclofenac inhibits both COX isoenzymes, to a greater extent COX-2. Inhibition of COX-1 in diclofenac is less compared with ibuprofen and naproxen, and therefore diclofenac rarely causes damage to the gastrointestinal tract. At the same time, inhibition of COX-1 (although less pronounced than in non-selective NSAIDs) may explain the greater effectiveness of diclofenac compared to selective COX-2 inhibitors (meloxicam, celecoxib) in a situation where COX-1 is also involved in the pathogenesis of the disease ( e.g. RA). Inhibition of COX-2 in diclofenac is less than that of etoricoxib and rofecoxib, which leads to a decrease in the risk of cardiovascular complications. Such a balanced effect of diclofenac provides high therapeutic activity with good tolerability of treatment.

Other mechanisms of analgesic action of diclofenac

In addition to inhibition of prostaglandins, other mechanisms of action of diclofenac have been identified. In an experimental study, it was shown that diclofenac sodium can significantly inhibit the migration of leukocytes to the site of inflammation. To a certain extent, diclofenac sodium can also affect the balance of cytokines, reducing the concentration of interleukin-6 and increasing the content of interleukin-10. Such a change in the ratio of these products favors the slowing down of the secretion of anti-inflammatory factors. The decrease in the production of free oxygen radicals, which occurs under the influence of sodium diclofenac, can also help reduce the activity of the inflammatory process and limit its damaging effect on tissues.

In addition to the pronounced anti-inflammatory activity, diclofenac sodium also has a powerful analgesic potential, not associated with its effect on inflammation. It has a complex effect on various mechanisms of pain perception, providing effective suppression of pain syndrome of various etiologies. The drug has both central and peripheral antinociceptive effects.

The central analgesic activity of diclofenac sodium is mediated by opioid receptors, as evidenced by the fact that this effect is blocked by naloxone. It appears to be related to the effect of sodium diclofenac on tryptophan metabolism. After the introduction of the drug in the brain, the concentration of tryptophan metabolites, which can reduce the intensity of pain, increases significantly.

The local antinociceptive effect of diclofenac sodium, apparently, is associated not only with the suppression of prostaglandin synthesis, since in several experimental models of pain syndrome, local use of prostaglandin synthesis inhibitors such as indomethacin and celecoxib, unlike diclofenac sodium, did not allow to achieve a significant analgesic effect. The peripheral analgesic effect of diclofenac sodium is not associated with an opioid effect, since it is not eliminated by naloxone. At the same time, the use of compounds that block the formation of NO and the activation of guanylate cyclase suppressed the analgesic effect of sodium diclofenac. A similar effect was also given by inhibitors of various types of potassium channels. In cultured rat cerebellum cells, diclofenac sodium increased the activity of potassium channels, increasing the release of potassium from the cell. These results suggest that the peripheral antinociceptive effect of diclofenac sodium may be associated with the activation of several types of potassium channels, which occurs with the participation of NO and guanosine cyclomonophosphate (cyclo-GMP).

Thus, the analgesic effect of diclofenac may be due to its effect on various levels and links in the pathogenesis of pain. In addition to the analgesic effect associated with a decrease in inflammation in the area of damage due to inhibition of prostaglandins (COX-1 and COX-2), diclofenac can reduce pain by reducing inflammation and through other mechanisms (restraining the migration of leukocytes to the site of inflammation, affecting the balance of cytokines) acting on potassium channels at the peripheral level, as well as reduce the perception of pain through the central mechanisms (by increasing the synthesis of the precursor of serotonin (tryptophan) in the brain tissue).

Indications for the use of diclofenac

Despite the wide range of currently available NSAIDs and the creation in recent years of a new class of symptomatic anti-inflammatory drugs (selective COX-2 inhibitors), diclofenac sodium remains the most popular drug among NSAIDs.

The use of diclofenac in rheumatology

From the very beginning of its appearance, diclofenac has found wide application in rheumatology. An important feature that allowed diclofenac to displace other drugs from the NSAID group used before was its high analgesic and analgesic activity, along with good tolerability.

The action of diclofenac is manifested by a decrease in the duration of morning stiffness, a decrease in pain (at rest and during movement), a decrease in swelling, swelling of the joints, as well as an improvement in the functional ability of the joints, which contributes to an increase in range of motion. Diclofenac is the drug of choice for most rheumatological diseases, it is used to treat inflammatory and degenerative rheumatic diseases (arthritis, arthrosis, etc.).

The use of diclofenac in general medical practice, orthopedics, traumatology, sports medicine

The most common in general medical practice are violations of the musculoskeletal system. The pathology of the musculoskeletal system is diverse in etiology and pathogenesis. Pain in this group of lesions can be caused by trauma, degenerative processes, inflammation, dysplasia, trophic changes (osteoporosis). The mechanisms of the development of the disease can be inflammatory, mechanical, neurogenic, etc. The pronounced analgesic effect of diclofenac in moderate and severe pain, inflammatory processes that occur after operations and injuries, rapid relief of spontaneous pain and pain on movement, and a decrease in inflammatory edema at the wound site made this drug one of the most necessary for the treatment of disorders of the musculoskeletal system, which are found in general medical practice, orthopedics, traumatology, sports medicine, neurology.

In the treatment of orthopedic and traumatic injuries, the form of release of the drug also matters. The possibility of combining local and general forms of diclofenac allows you to achieve maximum efficiency while minimizing possible side effects. Local forms of diclofenac are most widely used for diseases of extra-articular tissues (tendovaginitis, bursitis, rheumatic soft tissue lesions), injuries of tendons, ligaments, muscles and joints. The general forms, such as tablets, suppositories, solutions for injections, are for massive injuries (combined and combined injuries, postoperative conditions, head injuries, fractures of large bones, etc.).

The use of diclofenac in neurology

Diclofenac has found wide application for relief of pain syndromes in neurological practice. Diclofenac is indicated for the treatment of acute back pain, with tunnel syndromes (carpal tunnel syndrome, cubital tunnel syndrome, etc.), with migraine.

The duration of use and the method of administration of the drug depend on the intensity of the pain syndrome. With moderate pain syndromes that do not limit the patient's motor capabilities, it is possible to apply gels and ointments containing diclofenac sodium to painful areas (spastic muscle) for 7-10 days. With intense pain, which significantly limits the patient's movement within the premises, injection routes of administration of diclofenac sodium are used for 3-7 days, with a transition to oral forms in the future. There are reports of a higher efficiency of phonophoresis with diclofenac compared to the use of ointment forms of the drug.

The use of diclofenac in gynecology

The ability to eliminate pain and reduce the severity of blood loss in primary dysmenorrhea made it possible to use diclofenac in gynecological practice. In primary dysmenorrhea, the daily dose is selected individually; usually it is 50-150 mg. The initial dose should be 50-100 mg; if necessary, for several menstrual cycles, it can be increased to 150 mg / day. Diclofenac should be started as soon as the first symptoms appear. Depending on the dynamics of clinical symptoms, treatment can be continued for several days. Diclofenac can also be used for inflammatory diseases of the small pelvis, including adnexitis.

Method of application and doses: what dosage form to choose?

The undoubted advantage of diclofenac is the variety of dosage forms, including tablets (rapid and retarded action), solution for parenteral administration, suppositories, as well as forms used for local therapy: ointments, creams, gels, spray, which creates convenience when choosing an individual dose and method. use of the drug in different patients. The ability to combine different routes of administration in the same patient reduces the risk of adverse reactions.

diclofenac tablets

Tableted forms of diclofenac are available in various dosages (Table 2). The dose and route of administration of the drug for each patient is set individually, taking into account the severity of the disease. The average recommended dose for adults is 100-150 mg / day. The maximum daily dose of diclofenac is 200 mg. In relatively mild cases of the disease, as well as for long-term therapy, a daily dose of 75-100 mg is sufficient. The daily dose should be divided into several single doses. If necessary, to influence night pain or morning stiffness, in addition to taking the drug during the day, you can prescribe diclofenac in the form of suppositories before bedtime; while the daily dose should not exceed 150 mg. Upon reaching the clinical effect, the dose is reduced to the minimum maintenance dose.

Children aged 6 to 15 years (inclusive) are prescribed only 25 mg tablets. The daily dose is 0.5-2 mg / kg of body weight (in 2-3 doses, depending on the severity of the disease).

Adolescents aged 16 to 18 years can be prescribed 50 mg tablets. Tablets should be taken with plenty of liquid, preferably before meals. Tablets should not be divided or chewed.

Diclofenac delayed action tablets

A special form of the drug is diclofenac in the form of prolonged-release tablets. As a result of the delayed release of the active substance when taking retarded forms of diclofenac sodium, the effect occurs later, but lasts longer. These features of pharmacokinetics make it possible to achieve a reduction in the number of doses of the drug by patients (1-2 times a day instead of 3-4 times a day) while maintaining a stable high concentration of the drug in the focus of inflammation. This makes it preferable to use diclofenac in retarded form if long-term use of the drug is necessary (for chronic pain syndromes, mainly in rheumatological practice).

The recommended starting dose for adults is 75 mg, i.e. 1 retard tablet per day. The same dose is used in relatively mild cases of the disease, as well as for long-term therapy. In cases where the symptoms of the disease are most pronounced at night or in the morning, it is advisable to prescribe retard tablets at night.

The tablets should be swallowed whole, preferably with a meal. If it is necessary to increase the dose, an additional 1-2 tablets of diclofenac 25 mg each are used. The maximum daily dose is 200 mg.

Currently, the Swiss pharmaceutical company Sandoz produces 75 mg bilayer tablets, which are unique in that each tablet consists of two layers and includes 12.5 mg of immediate release diclofenac sodium and 62.5 mg of sustained release diclofenac sodium, which provides both rapid onset of action and prolonged action of the drug.

Children and adolescents under 18 years of age should not be prescribed retard tablets.

Diclofenac in the form of rectal suppositories

The dosage form of diclofenac in the form of suppositories has a number of advantages. Candles do not cause the complications that are possible with parenteral administration of drugs (development of muscle necrosis, infiltrates and suppuration at the injection site). It is advisable to prescribe suppositories if it is impossible to take drugs through the mouth (in debilitated patients, in the presence of strictures of the esophagus, etc.). When taken per os, there is a direct damaging effect of diclofenac on the cells of the gastric mucosa. With other methods of drug administration (suppositories, ointments), the risk of damage to the gastrointestinal tract remains, but it is significantly lower. That is why, in the presence of signs of damage to the stomach and duodenum, suppository forms of diclofenac are preferred.

Very often, suppositories are used in combination therapy: during the day, the patient receives either injections or tablets, and suppositories at night, which creates a better therapeutic effect due to a more uniform and prolonged maintenance of the concentration of the drug in the blood. In this case, the total daily dose of diclofenac should not exceed 150 mg.

Children aged 6 to 15 years (inclusive) are prescribed only 25 mg suppositories. The daily dose is 0.5-2 mg / kg of body weight (daily dose, depending on the severity of the manifestations of the disease, should be divided into 2-3 single doses). For the treatment of RA, the daily dose may be increased to a maximum of 3 mg/kg (in multiple doses). Adolescents aged 16 to 18 years can also be prescribed suppositories of 50 mg.

The suppository is injected into the rectum, as deep as possible, preferably after a preliminary bowel cleansing. Suppositories should not be cut into pieces, since such a change in the storage conditions of the drug may further lead to a violation of the distribution of diclofenac.

Diclofenac solution for injection

Diclofenac in the form of injections is preferably used when a faster analgesic effect is needed, usually with more severe acute pain (with renal or hepatic colic, with acute pain associated with soft tissue injuries (bruise, sprain), with acute back pain, postoperative pain Usually prescribed 1 ampoule per day, but in severe cases, you can prescribe 2 injections per day with an interval of several hours, changing the direction of injection.The use of injections can be combined with other dosage forms of diclofenac.Duration of parenteral use should not exceed two days; if necessary, treatment continue with the same diclofenac, but in the form of tablets or rectal suppositories.When used intramuscularly, the drug is injected deep into the upper outer quadrant of the buttock; during the day, no more than 2 ampoules (150 mg) of the drug are used.In renal and hepatic colic, the administration of diclofenac is usually combined with the use antispasmodics.With a pronounced muscular component of back pain, the administration of diclofenac is combined with the use of muscle relaxants.

The combination of two or more NSAIDs should be avoided as their effectiveness remains unchanged and the risk of side effects increases.

Diclofenac in the form of agents for external (local) use

The undesirable effect of NSAIDs on the body is sharply limited if they are used in the form of local applications. The dosage form for such therapy is a mixture of the active drug with a base that provides absorption under the skin. This method of treatment allows you to inject the drug directly into the lesion. At the same time, the impact on other organs and tissues is minimal.

Abroad, there are dosage forms in the form of plates for gluing to the skin, containing 1.3% diclofenac epolamine. For the first time, diclofenac in the form of plates appeared in Switzerland in 1993; currently, diclofenac in the form of plates is registered in 43 countries of the world. Diclofenac plates are intended primarily for those who cannot take the oral form of diclofenac due to contraindications. They are used for damage to soft tissues (bruise, sprain, compression, osteoarthritis), provided that the integrity of the skin is preserved 2 times a day. Plates are convenient to use, but are more expensive than other dosage forms.

These drugs are convenient to use and easy to dose. After applying the drug to the skin, the active compound accumulates in the regional soft tissues and no more than 6% of the active substance enters the bloodstream. At the same time, the content of the drug in the muscles in the area of application is approximately three times higher than its level in the distant muscle tissue. This makes the use of gel forms of diclofenac preferable for a wide range of disorders of the musculoskeletal system. Gel forms of diclofenac are over-the-counter drugs and are very popular.

Diclak gel is the only diclofenac drug on the Russian market with a maximum concentration of 5% of the active substance, which allows you to reduce the dose of the drug taken orally, and in some cases even replace the tablets. Approved for use by children from 6 years of age.

Diclofenac as part of combination drugs for the treatment of pain

There are also dosage forms (ointments, gels) in which diclofenac is one of the main components. The combination of several drugs with different mechanisms of action can improve the effectiveness of treatment.

Safety

Diclofenac has an optimal combination of analgesic and anti-inflammatory effects and is well tolerated. Therefore, in the absence of contraindications, it can be used even for a long time. Studies have confirmed that treatment with diclofenac at sufficiently high doses (150 mg) with long-term use (up to 8 months or more) was well tolerated by patients. Of course, diclofenac, like any NSAID, may have side effects and contraindications. However, it should be noted that side effects, among which ulceration of the mucosa of the gastrointestinal tract (GIT) should be feared in the first place, develop more often in individuals with risk factors.

Risk factors for gastrointestinal damage include:

age over 65;
peptic ulcer in history;
food intake that increases gastric secretion (spicy, fatty, salty foods);
large doses or concomitant use of several NSAIDs;
concomitant therapy with glucocorticoids;
female, as an increased sensitivity of women to this group of drugs was found;
smoking;
alcohol intake;
Availability Helicobacter pylori.

In this regard, treatment should be started with the lowest recommended dose, especially in risk groups. In persons at risk, the daily dose of diclofenac should not exceed 100 mg, preference should be given to short-lived dosage forms of diclofenac and prescribe it either 50 mg 2 times a day or 25 mg 4 times a day. Diclofenac should be taken after meals. With prolonged use of the drug, you should refrain from drinking alcohol, since diclofenac, like alcohol, is metabolized in the liver. If there are complaints from the gastrointestinal tract, it is necessary to carry out esophagogastroduodenoscopy (EGDS), and with the systematic use of diclofenac, this procedure should be prescribed every 4-6 months, since NSAID gastropathy is often asymptomatic - “silent”.

If it is necessary to use diclofenac for a long time, which is especially important in rheumatology, it is advisable to prescribe diclofenac together with misoprostol, which protects the gastric mucosa from damage.

In patients with hypertension, it is necessary to control the level of blood pressure; in patients with bronchial asthma, an exacerbation may occur while taking diclofenac. In patients with chronic diseases of the liver and kidneys, small doses of the drug should be used, controlling the level of liver enzymes.

Before prescribing diclofenac, the doctor should clarify whether the patient is taking any other medications due to concomitant diseases in order to avoid possible complications when using diclofenac in combination with other drugs. It is known that diclofenac increases the plasma concentration of digoxin, lithium, cyclosporine A, including increasing its nephrotoxicity; enhances the toxicity of methotrexate. Against the background of potassium-sparing diuretics, diclofenac increases the risk of hyperkalemia, and against the background of anticoagulants - the risk of bleeding. Diclofenac reduces the effect of diuretics, antihypertensives and hypnotics. Simultaneous administration of antidiabetic agents can lead to both hypo- and hyperkalemia.

More than 30 years have passed since the introduction of diclofenac into clinical practice. During this time, many new NSAIDs have appeared. This greatly expanded the possibilities of providing effective care to patients, since the individual response to treatment is very variable. However, diclofenac occupies a special place in this therapeutic arsenal. The combination of high efficiency, good tolerability and a variety of dosage forms of the drug allow you to choose the optimal therapy for a wide range of pain syndromes.

For literature inquiries, please contact the editor.

A. B. Danilov, Doctor of Medical Sciences

FPPOV them. I. M. Sechenov, Moscow

Table 1. Indications for the use of diclofenac

Preparations for systemic use (tablets, injections, suppositories)

Rheumatology:

rheumatism;
RA, juvenile RA;
extra-articular forms of rheumatism, soft tissue rheumatism - periarthritis, bursitis, tendovaginitis, fibrositis, myositis;
ankylosing spondylitis - Bechterew's disease;
osteoarthritis;
spondyloarthritis;
other mono- and polyarthritis;
degenerative diseases of the joints - arthrosis (coxarthrosis, spondyloarthrosis);
back pain associated with degenerative changes in the spine;
acute attack of gout

Neurology, traumatology, orthopedics, sports medicine, general medical practice:

dorsalgia (lumbago, sciatica, myofascial and muscular-tonic pain);
migraine and other types of headache;
tunnel syndromes, other diseases accompanied by inflammation of non-rheumatic origin (neuralgia, neuritis, lumboischialgia, bursitis, capsulitis, synovitis, tendonitis or tendosynovitis);
traumatic bruises, sprains, muscles and tendons; inflammatory swelling of soft tissues, muscle soreness (myalgia) and joints caused by heavy physical exertion

Oncology:

WHO step 1 remedy for cancer pain

General medical practice:

renal and biliary colic

Gynecology:

gynecological diseases accompanied by pain and inflammation (primary dysmenorrhea, adnexitis, etc.)

Traumatology, surgery, dentistry:

post-traumatic and postoperative pain syndromes;
obstetric-gynecological, dental or other surgical interventions

Otorhinolaryngology:

with severe inflammatory diseases of the ear, throat and nose, occurring with severe pain, for example, with pharyngitis, tonsillitis, otitis media. Treatment of the underlying disease is carried out in accordance with generally accepted principles, including the use of etiotropic therapy.

Preparations for external and local use

Traumatology, sports medicine:

post-traumatic inflammation of soft tissues and the musculoskeletal system (tendons, ligaments, muscles and joints);
musculoskeletal injuries typical for sports medicine and sports: sprains, dislocations, bruises, contusions, overloads, etc.

Rheumatology:

local treatment of inflammatory and degenerative joint diseases: RA, osteochondrosis of peripheral joints and spine, periarthropathy, etc.

Rheumatology, neurology:

local treatment of inflammatory and degenerative diseases of soft tissues and periarticular tissues: tendovaginitis, shoulder-hand syndrome, bursitis, osteochondrosis, osteoarthritis, periarthropathies, etc.;
arthralgia;
dorsalgia;
myalgia

Traumatology, surgery:

soreness and inflammation of the soft tissues

Ophthalmology:

non-infectious conjunctivitis, post-traumatic inflammation after penetrating and non-penetrating injuries of the eyeball, pain syndrome when using an excimer laser, during the operation of removal and implantation of the lens (pre- and postoperative prevention of miosis, cystoid edema of the optic nerve)