Back pain is a common reason for patients to visit a doctor. There are many pathologies characterized by back pain: osteochondrosis, osteoarthritis, rheumatoid arthritis, spinal hernia. Movalis is one of the most effective drugs that can relieve pain.
Active ingredient
The active component of the drug, meloxicam, relieves any inflammation. This has been proven by clinical trials. Meloxicam inhibits the synthesis of prostaglandins (Pg), which are known to be mediators of inflammation. That is, Movalis acts precisely. As for cartilage tissue, it does not experience any negative effects during a course of taking the drug.
The pharmacological market boasts a variety of dosage forms of the drug: tablets, injection solution, rectal suppositories (suppositories), suspensions.
Movalis against arthritis of the fingers
It is worth noting that the injections are intended for the first 2-3 days of therapy, when the inflammatory and pain syndrome is most pronounced. After pain and inflammation are relieved, treatment continues using available dosage forms.
The analgesic effect can be observed after 30 minutes and lasts about a day after taking Movalis.
Indications
What do pills help with?
- symptomatic treatment of aggravated osteoarthritis;
- long-term treatment of infectious nonspecific polyarthritis and rheumatoid spondylitis.
What do injections help with?
- short-term treatment of an acute attack of infectious nonspecific polyarthritis or rheumatoid spondylitis, when the rectal and oral routes of administration of the drug Movalis are impossible.
Why is the suspension prescribed?
- symptomatic treatment of osteoarthritis (including with a pain component), rheumatoid arthritis (including juvenile arthritis), rheumatoid spondylitis
Contraindications
The use of Movalis is prohibited in the following cases:
- active gastrointestinal bleeding, recent cerebrovascular bleeding or established diagnosis of diseases of the blood coagulation system;
- concomitant therapy with anticoagulants, because there is a risk of intramuscular hematoma formation;
- severe liver failure;
- severe heart failure;
- severe renal failure (if hemodialysis is not performed, CC <30 ml/min, and also with confirmed hyperkalemia);
- active liver disease;
- erosive and ulcerative lesions of the stomach and duodenum in the acute phase or recently suffered;
- inflammatory bowel diseases (Crohn's disease or ulcerative colitis in the acute phase);
- therapy of perioperative pain during coronary artery bypass grafting;
- pregnancy;
- lactation period (breastfeeding);
- age under 18 years;
- hypersensitivity to the active substance or auxiliary components of the drug.
- hypersensitivity (including to other NSAIDs), complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses, angioedema or urticaria caused by intolerance to acetylsalicylic acid or other NSAIDs (including a history) due to existing potential for cross-sensitivity.
Movalis should be used with caution in old age
Use with caution if you have:
- history of gastrointestinal diseases (presence of Helicobacter pylori infection);
- congestive heart failure;
- cerebrovascular diseases;
- dyslipidemia/hyperlipidemia;
- diabetes;
- peripheral arterial disease;
- renal failure (creatinine clearance 30-60 ml/min);
- IHD;
- elderly age;
- long-term use of NSAIDs;
- smoking;
- frequent drinking of alcohol;
- concomitant therapy with the following drugs: anticoagulants, oral corticosteroids, antiplatelet agents, selective serotonin reuptake inhibitors.
Contraindications for use in pediatrics:
- tablets - age up to 16 years;
- d/i solution - age up to 18 years;
- candles - age up to 12 years;
- suspension - age up to 12 years (for juvenile arthritis, the restriction for use is age up to 2 years).
Movalis
Use during pregnancy and breastfeeding
The use of Movalis® is contraindicated during pregnancy.
It is known that NSAIDs are excreted in breast milk, therefore the use of Movalis® during breastfeeding is contraindicated.
As a drug that inhibits COX/prostaglandin synthesis, Movalis® may affect fertility and is therefore not recommended for women planning pregnancy. Meloxicam may delay ovulation. In this regard, in women who have problems conceiving and are undergoing examination for such problems, it is recommended to discontinue taking the drug Movalis®.
Use for liver dysfunction
The drug is contraindicated in severe liver failure.
In patients with liver cirrhosis (compensated), no dose adjustment is required.
Use for renal impairment
The drug is contraindicated in severe renal failure (if hemodialysis is not performed, CC <30 ml/min, as well as with confirmed hyperkalemia), progressive kidney disease.
The drug should be prescribed with caution in case of renal failure (creatinine clearance 30-60 ml/min).
In patients with severe renal failure undergoing hemodialysis, the dose should not exceed 7.5 mg/day.
In patients with mild to moderate renal insufficiency (creatinine clearance >25 ml/min), no dose adjustment is required.
Use in children
The use of the drug in children under 12 years of age is contraindicated.
special instructions
Patients with gastrointestinal diseases should be monitored regularly. If ulcerative lesions of the gastrointestinal tract or gastrointestinal bleeding occur, Movalis® should be discontinued.
Gastrointestinal bleeding, ulcers, and perforations may occur at any time during the use of NSAIDs, with or without warning symptoms or a history of serious gastrointestinal complications. The consequences of these complications are generally more serious in older people.
When using Movalis®, serious skin reactions such as exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis may develop. Therefore, special attention should be paid to patients reporting the development of adverse events from the skin and mucous membranes, as well as hypersensitivity reactions to the drug, especially if such reactions were observed during previous courses of treatment. The development of such reactions is observed, as a rule, during the first month of treatment. If the first signs of a skin rash, changes in mucous membranes or other signs of hypersensitivity appear, discontinuation of Movalis® should be considered.
Cases have been described of an increased risk of developing serious cardiovascular thrombosis, myocardial infarction, and an attack of angina, possibly fatal, when taking NSAIDs. This risk increases with long-term use of the drug, as well as in patients with a history of the above diseases and those predisposed to such diseases.
NSAIDs inhibit the synthesis of prostaglandins in the kidneys, which are involved in maintaining renal perfusion. The use of NSAIDs in patients with reduced renal blood flow or reduced volume may lead to decompensation of latent renal failure. After discontinuation of NSAIDs, renal function usually returns to baseline levels. Those most at risk for developing this reaction are elderly patients, patients with dehydration, congestive heart failure, liver cirrhosis, nephrotic syndrome or acute renal impairment, patients concomitantly taking diuretics, ACE inhibitors, angiotensin II receptor antagonists, and also patients who have undergone major surgical interventions that lead to hypovolemia. In such patients, diuresis and renal function should be carefully monitored when initiating therapy.
The use of NSAIDs in combination with diuretics can lead to sodium, potassium and water retention, as well as a decrease in the natriuretic effect of diuretics. As a result, predisposed patients may experience increased signs of heart failure or hypertension. Therefore, careful monitoring of the condition of such patients is necessary, as well as maintaining adequate hydration. Before starting treatment, a kidney function test is necessary.
In case of combination therapy, renal function should also be monitored.
When using the drug Movalis® (as well as most other NSAIDs), episodic increases in transaminase activity or other indicators of liver function in the blood serum have been reported. In most cases, this increase was small and transitory. If the identified changes are significant or do not decrease over time, Movalis® should be discontinued and the identified laboratory changes should be monitored.
Frail or malnourished patients may be less able to tolerate adverse events and should be monitored closely.
Like other NSAIDs, Movalis® can mask the symptoms of an infectious disease.
As a drug that inhibits COX/prostaglandin synthesis, Movalis® may affect fertility and is therefore not recommended for women who have difficulty conceiving. In women undergoing examination for this reason, it is recommended to discontinue taking Movalis®.
In patients with mild to moderate renal insufficiency (creatinine clearance >25 ml/min), no dose adjustment is required.
In patients with liver cirrhosis (compensated), no dose adjustment is required.
Impact on the ability to drive vehicles and operate machinery
No special clinical studies have been conducted on the effect of the drug on the ability to drive a car or use machinery. However, when driving and operating machinery, the possibility of dizziness, drowsiness, visual impairment or other central nervous system disorders should be taken into account. Patients should be careful when driving a car and operating machinery.
Side effects
Side effects - headache
As with therapy with other NSAIDs, while taking Movalis, there is a possibility of adverse reactions from the body:
- From the urinary system: edema, hypercreatininemia, increased urea concentration. In rare cases - interstitial nephritis, glomerulonephritis, renal medullary necrosis, nephrotic syndrome.
- From the digestive system: nausea, vomiting, belching, abdominal pain, constipation or diarrhea, flatulence, increased activity of “liver” transaminases, hyperbilirubinemia, stomatitis, erosive and ulcerative lesions of the gastrointestinal tract, gastrointestinal bleeding (hidden or obvious), perforation of the digestive tract canal, colitis, dyspepsia, gastroduodenal ulcer, esophagitis, gastritis, hepatitis.
- From the cardiovascular system: increased blood pressure, “flushes” of blood to the skin of the face and upper chest, palpitations.
- From the nervous system: dizziness, headache, drowsiness, mood lability, confusion, disorientation..
- From the hematopoietic organs: anemia, leukopenia, thrombocytopenia.
- Allergic reactions: skin rash, itching, blisters, erythema multiforme, Lyell's syndrome, bullous dermatitis, Stevens-Johnson syndrome, angioedema, hypersensitivity to UV radiation, urticaria, anaphylactoid reactions.
- Other: ringing in the ears, blurred vision, conjunctivitis.
Combination use of the drug Movalis and drugs that suppress the functioning of the bone marrow can provoke cytopenia (deficiency of one or more types of blood cells). If gastrointestinal bleeding, perforation or ulcer occurs during treatment with Movalis, this can lead to death.
When using a d/i solution, the following are possible:
- glomerular or interstitial nephritis;
- papillary necrosis;
- nephrotic syndrome;
- swelling and pain at the injection site.
TREATMENT AND PREVENTION OF GOUT: DRUGS OF CHOICE (Part 2)
Preferanskaya Nina Germanovna
Associate Professor, Department of Pharmacology, Faculty of Pharmacy, First Moscow State Medical University named after. THEM. Sechenova, Ph.D.
To increase the effectiveness of treatment and reduce the manifestations of pathology, the patient should be warned that taking anti-inflammatory drugs (
Diclofenac, Indomethacin, Ibuprofen, Ketoprofen, Naproxen, Meloxicam, Celecoxib, Nimesulide, etc. ) should be started at the first sensation of pain.
NON-STEROID drugs
Diclofenac sodium
(
Voltaren
,
Ortofen
) - NSAID, a derivative of phenylacetic acid, has a strong analgesic and anti-inflammatory effect. Indiscriminately inhibits COX-1 and COX-2, disrupts the metabolism of arachidonic acid, and reduces the amount of Pg at the site of inflammation. The anti-inflammatory effect develops after 7–14 days. 50% undergoes presystemic elimination. The half-life is very short, T½ = 1.5–2 hours, so 100 mg extended-release, film-coated retard tablets have been created that provide a high concentration over a long period of time. In acute conditions, to relieve exacerbation, the drug is administered intravenously (once), then 25–50 mg 4 times a day. For inflammatory processes of non-infectious etiology, it is recommended to use 5% gel or 1.2% ointment for external use, which reduces swelling and pain. Apply 2–4 g of ointment or gel to the area of inflamed joints 2–3 times a day.
Indications for use are osteoarthritis; rheumatoid arthritis, articular syndrome with exacerbation of gout, inflammatory and degenerative diseases of the joints.
Important!
When taken, allergic reactions occur: itching, skin rash, hyperemia, angioedema, exudative erythema multiforme, fever, chills, photosensitivity, nausea, vomiting. With long-term use in large doses - ulceration of the gastrointestinal mucosa, bleeding (gastrointestinal, gingival, uterine, hemorrhoidal).
Indomethacin (Metindol retard, Indobene)
- a derivative of indoleacetic acid, an inhibitor of prostaglandin synthesis in the kidneys - prescribed orally after meals at a dose of 75 mg, and then every 6 hours. 50 mg each. Treatment continues until the pain disappears. On the next day, the dose is reduced to 50 mg 3 times. Then switch to a maintenance dose of 25 mg 3 times a day.
Side effects of Indomethacin include gastrointestinal disorders (bloating, colitis, enteritis, ulcers), bleeding in internal organs, sodium retention in the body, allergic reactions, confusion, convulsions, forgetfulness, hallucinations. These doses may cause side effects in up to 60% of patients. However, Indomethacin is easier to tolerate than Colchicine, and in acute gouty arthritis it is often the drug of choice.
Meloxicam
(Movalis, Mirlox)
belongs to the oxicam class;
enolic acid derivative. The mechanism of action is inhibition of Pg synthesis as a result of selective suppression of the enzymatic activity of COX-2. When prescribed in high doses or with prolonged use, the selectivity of the drug decreases. Suppresses Pg synthesis in the area of inflammation to a greater extent than in the gastric mucosa or kidneys, which is associated with relatively selective inhibition of COX-2. Important!
Side effects are common to all NSAIDs. Selective NSAIDs are less likely to cause erosive and ulcerative damage to the gastrointestinal tract. Eating does not affect absorption. Plasma concentration is dose-dependent, TCmax is 5–6 hours. The maximum daily dose is 15 mg. Metabolized in the liver to inactive metabolites. Excreted through the intestines and kidneys (in equal proportions), unchanged - 1.6% of the daily dose.
Nimesulide
(Actasulide
,
Nise
,
Nimulid)
is a non-steroidal anti-inflammatory drug, a sulfonanilide derivative. It has a pronounced anti-inflammatory, antipyretic, analgesic and antiplatelet effect. When prescribed in high doses, long-term use or individual characteristics of the body, selectivity decreases. Selectively inhibits cyclooxygenase-2, reduces the amount of prostaglandins (mainly at the site of inflammation), suppresses the exudative and proliferative phases of inflammation. Reduces capillary permeability; stabilizes lysosomal membranes; inhibits the production of ATP in the processes of oxidative phosphorylation; inhibits the synthesis or inactivates inflammatory mediators (prostaglandins, histamine, bradykinins, lymphokines, complement factors and other nonspecific endogenous damaging factors). Blocks the interaction of bradykinin with tissue receptors, restores impaired microcirculation and reduces pain sensitivity at the site of inflammation.
Important!
Side effects: hepatotoxicity, NSAID gastropathy, dyspepsia, abdominal pain, nausea, vomiting, heartburn, tinnitus, dizziness, allergic reactions: skin rash, itching, urticaria, Quincke's edema, headache, hematuria, agranulocytosis, leukopenia.
Combining NSAIDs with each other is contraindicated, because the risk of developing ulcerative lesions of the gastrointestinal tract increases, the activity of serum transaminases increases and bleeding time prolongs.
GLUCOCORTICOSTEROIDS
In acute gout, especially when NSAIDs are contraindicated or ineffective, systemic or local (intra-articular) administration of glucocorticosteroids is resorted to. For systemic administration (orally or intravenously), moderate doses are prescribed over several days, because the concentration of glucocorticosteroids quickly decreases and the effect decreases. Intra-articular injection of the long-acting (3–4 weeks) steroid drug Triamcinolone hexacetonide
at a dose of 20 or 30 mg can stop an attack of rheumatoid arthritis.
Treatment is especially appropriate when standard drug therapy is ineffective. Triamcinolone hexacetonide (Lederspan)
is available in the form of a suspension of 20 mg/ml per amp.
PHYTOTHERAPY
For gout, the herbal medicine Fulflex
, produced in the form of capsules (pack of 24 pcs.) and in the form of a gel (75 g).
1 capsule contains Martinia fragrant root extract (225 mg), white willow bark extract (75 mg). An extract from the root of Martinia fragrant is especially good for gout, because... The main thing is the ability to bind excess concentrations of uric acid in the blood and remove it out with the help of the kidneys. Fullflex
is used for rheumatism, gout, myalgia, lumbago and especially for arthritis, taking into account its anti-inflammatory, antirheumatic analgesic effect. Adults and children over 14 years old take 1 capsule of dietary supplement. 1 time per day with meals for a month. The gel is applied to the affected joint.
For gout, you can use an infusion of lingonberry leaves.
(20.0–200 ml) 1 tbsp.
l. 3–4 times a day. For preventive purposes, preparations that are indicated for urolithiasis
. The composition of such collections includes: madder root, horsetail herb, parsley fruits, lingonberry leaves, bearberry leaves, etc., which help loosen urinary calculi and have an antispasmodic, anti-inflammatory and diuretic effect.
RECOMMENDATIONS
A generally accepted risk factor for the development of gout is an increased consumption of the following foods:
- containing excessive amounts of purines (meat, especially brains, liver, tongue, kidneys, fish, mushrooms, legumes, peanuts, spinach, chocolate);
- fats and carbohydrates;
- alcohol, especially beer and fortified red wines containing guanosine (a precursor to uric acid);
- tea and coffee containing the purine alkaloid caffeine more than 1%.
It is recommended to exclude the consumption of smoked and spicy foods, concentrated meat broths, meat by-products, canned fish and meat, chocolate and strong coffee, overeating in general and little physical activity. Restriction of movement is effective during an acute attack. Avoiding hypothermia and taking local anesthetics is necessary, especially in patients at high risk of side effects from systemic medications. The current goals of anti-gout therapy are to convince the patient to adhere to the diet, adherence to treatment (increasing compliance) and developing skills to control blood pressure and body weight.
How to take Movalis
General advice for the use of any of the dosage forms of Movalis is that the drug is recommended to be used in the minimum effective dose, and the therapeutic course should last as short as possible. Moreover, during treatment, it is recommended to assess the need for taking the drug and the body’s response. During the day, you can take, regardless of the dosage form of the drug Movalis, only 15 mg/day. This is the maximum for the day.
How to take Movalis medicine correctly?
Movalis tablets and suspension are taken orally during meals with a sufficient amount of water.
- osteoarthritis: 7.5 mg/day. If indicated and the severity of the pain syndrome, it is possible to increase the dose to 15 mg/day;
- rheumatoid arthritis, ankylosing spondylitis: 15 mg/day. (possibly reducing the dose by 2 times);
- Children under 12 years of age are prescribed Movalis in the form of a suspension for the treatment of juvenile rheumatoid arthritis. The dose is calculated based on body weight - 0.125 mg/kg (maximum - 7.5 mg per day).
- children 12-18 years old with juvenile rheumatoid arthritis: 0.25 mg/kg, but not more than 15 mg per day.
It is recommended to use the following dosage regimen (amount of active substance/volume of suspension):
- 12 kg: 1.5 mg/1 ml;
- 24 kg: 3 mg/2 ml;
- 36 kg: 4.5 mg/3 ml;
- 48 kg: 6 mg/4 ml;
- From 60 kg: 7.5 mg/5 ml.
Movalis, Mydocalm and Milgamma: which is better, comparison
Movalis, Mydocalm and Milgamma are drugs used for dysfunction of the musculoskeletal system. Medicines have different compositions, so they have different effects.
To speed up the treatment process, relieve inflammation and pain, replenish vitamin B deficiency, and prevent the development of degenerative processes, Milgamma, Movalis and Mydocalm are included in combination treatment.
Additional composition:
- Water
- Megluminum
- Glycofurol
- Sodium hydroxide
- Poloxamer 188
- Aminoacetic acid
- Sodium chloride.
A transparent solution with a yellow-green tint is placed in glass ampoules with a volume of 1.5 ml. The bottles are packed in cardboard boxes.
Movalis tablets contain 7.5 or 15 mg of meloxicam. Auxiliary components:
- E 572
- Milk sugar
- E 331
- Crospovidone
- Polysorb
- MCC
- Povidone.
Large yellow pills are placed in a blister (10 pieces). The box contains 1-2 blister packs.
The manufacturer of Movalis is Boehringer Ingelheim, Germany. The drug is available with a prescription. The cost of the medicine is from 540 to 820 rubles.
Movalis is a COX-2 inhibitor. The medicine has anti-inflammatory, analgesic and antipyretic properties.
Pills and solution are included in symptomatic therapy for rheumatoid arthritis, osteoarthritis, and ankylosing spondylitis. The drug is also prescribed for other pathologies of the locomotor system, accompanied by degeneration and inflammation (sciatica, dorsopathy, arthropathy).
Contraindications:
- Heart failure
- Pregnancy
- Meloxicam and NSAID intolerance
- Gastrointestinal ulcer or bleeding
- Impaired hemostasis
- Renal dysfunction
- Intestinal inflammation
- Liver diseases
- Respiratory diseases.
The daily dose of Milgamma solution is 15 mg. Duration of use – 3 days. The drug is administered intramuscularly.
In case of renal or hepatic dysfunction, the daily dosage can be reduced to 7.5 mg.
Injections with Movalis: instructions for use
Movalis in ampoules is used exclusively intramuscularly (intravenous use is prohibited). The medicine is administered once in a dose of 15 mg. Typically, injections with Movalis are used in the first 2-3 days of therapy.
The medicine is administered slowly, by deep injection into the gluteus maximus muscle.
The recommended daily dose is 7.5 mg or 15 mg 1 time/day, depending on the intensity of pain and the severity of the inflammatory process.
- Osteoarthritis with pain: 7.5 mg/day. If necessary, the dose can be increased to 15 mg/day;
- Rheumatoid arthritis: 15 mg/day. Depending on the therapeutic effect, the dose can be reduced to 7.5 mg/day;
- Ankylosing spondylitis: 15 mg/day. Depending on the therapeutic effect, the dose can be reduced to 7.5 mg/day.
Movalis suppositories: instructions for use
For adults with osteoarthritis, rheumatoid arthritis or spondylitis, rectal suppositories are administered at a dose of 7.5 mg 1 time / day. If indicated, the dose can be increased to the maximum possible per day - 15 mg.
The effectiveness of movalis in the treatment of acute pain in the lower back
E. G. Filatova A. V. Kondrikov O. I. Istomina
The purpose of the study was to determine the factors influencing the effectiveness of movalis (meloxicam) when used in combination (injection and tablet forms) in patients with acute back pain syndrome (LBP) and to assess the safety of treatment. We observed 30 patients (18 women, 12 men, average age 43.1 years) with primary LBP syndrome. In 83% of patients, its cause was muscular-tonic syndrome, in 17% it was combined with radiculopathy.
Movalis treatment regimen : intramuscular administration at a dose of 15 mg/day for 5 days, followed by oral administration of the drug at 15 mg (1 tablet) per day, treatment duration is 2 weeks. The high efficiency of this mode has been established. In accordance with the patients’ subjective assessment of the results of treatment, its effectiveness was as follows: “satisfactory” - 7%, “good” - 30%, “very good” - 33%, “excellent” - 30%. Side effects in the form of transient abdominal pain were observed in only 2 (6.6%) patients. The main factors influencing the effectiveness of the drug in reducing pain were emotional, namely the severity of depression and anxiety, and the presence or absence of radiculopathy.
Low back pain syndrome (LBP) is pain localized between the 12th pair of ribs and the gluteal folds. Their prevalence in the population is very high - up to 58-84%, and the socio-economic losses associated with this pathology for society are enormous. According to WHO, in the USA in 2000 they amounted to 25-85 billion dollars, in the UK - 6 billion pounds sterling [5].
There are primary and secondary LBP syndrome.
The main causes of primary LBP syndrome, which develops mainly at the age of 20-50 years (peak incidence 35-45 years), are dysfunction of the musculo-ligamentous apparatus, spondylosis, less commonly, intervertebral disc herniation, etc. Secondary LBP syndrome is observed both in older and older adults. and in middle age. It develops as a result of diseases of the visceral organs (cardiovascular, genitourinary systems, lungs, gastrointestinal tract, etc.), endocrine and other diseases.
The syndrome can occur acutely (about 3 weeks), subacutely (3-12 weeks) and chronically (more than 12 weeks - up to 25 episodes per year) [5]. The peculiarity of the pain in question is a combination of reflex muscular-tonic and myofascial syndromes with changes in mental , namely in the emotional sphere. The latter contribute to the chronicity of the condition. In some cases, it is the emotional factors that determine the lack of correlation between the severity of degenerative changes and pain syndrome, the correlation of pain syndrome with the size and localization of the intervertebral hernia, as well as the recurrent course with the relative stability of pathological changes in anatomical structures.
In accordance with WHO recommendations [5], treatment of LBP is carried out taking into account their form and course. The general therapeutic complex usually includes the following activities:
- interventions aimed at eliminating the cause of back pain;
- providing rest for 2-5 days;
- use of a bandage;
- use of non-steroidal anti-inflammatory drugs (NSAIDs) and muscle relaxants; local therapy - injections of anesthetics, glucocorticoids, acupuncture;
- manual therapy; traction (although from the standpoint of evidence-based medicine there is no convincing data on its effectiveness);
- transcutaneous electrical stimulation; physical exercise;
- physiotherapeutic procedures (phonophoresis, sinusoidal modulated currents, ultrasound, laser and magnetic therapy);
- surgical decompression [2, 3].
NSAIDs (diclofenac, etc.) occupy a central place in the treatment of LBP.
Their therapeutic effect is based on inhibition of the enzyme cyclooxygenase, which catalyzes the synthesis of prostaglandins [4]. Today two of its forms are known - 1 and 2.
A new agent that selectively inhibits cyclooxygenase 2 (which provides better tolerability compared to traditional NSAIDs) is meloxicam (Movalis). Its advantage lies in the presence of an injection form of use. A number of studies [1, 6-8] have shown that movalis effectively relieves LBP, and acts faster than diclofenac and is better tolerated.
The purpose of our study was to identify factors influencing the effectiveness of movalis in combined (injection and tablet forms) treatment of patients with acute LBP, and to assess its safety.
Material and methods
We observed 30 patients (18 women and 12 men) aged 27-64 years (average 43.1 years) with primary LBP syndrome. Inclusion criteria were acute or subacute LBP; stop taking other NSAIDs 3-7 days before the start of the study; stopping taking muscle relaxants, psychotropic and other analgesic drugs that affect the threshold of pain sensitivity.
Exclusion criteria were chronic or chronically relapsing LBP (more than two attacks in the last 6 months); history of spinal injuries; consequences of surgery on the spine; presence of clinical signs of gastric or duodenal ulcer; blood diseases; kidney disease; hypersensitivity to analgesics, antipyretics and NSAIDs. The study was conducted at the neurological department of the Moscow City Clinical Hospital #33. Movalis was administered intramuscularly at a dose of 15 mg/day for 5 days, followed by enteral administration at the same dose (one tablet per day) .
The duration of treatment was 2 weeks. Along with movalis, patients received vascular medications, vitamins, physiotherapy, massage according to indications. The examination was carried out before the start of the course of treatment with movalis (background), on the 1st day of treatment, 1 hour after the injection of movalis, on the 5th day, on the last day of injection therapy and on the 14th day - at the end of the course of treatment. Along with the traditional clinical neurological examination, the intensity of pain at rest and during movement was assessed on a visual analogue scale (VAS), the severity of Lasegue's symptom (in degrees), flexion of the lumbar spine, its lateral mobility to the right and left.
When determining the threshold of pain sensitivity, the pressure threshold at the maximum painful point of the back was measured with an algometer. The device records the pressure (in feet) at the moment pain occurs. The disability index was determined (according to Waddell).
The subjective assessment of the treatment outcome by the patients themselves was also taken into account: “excellent”, “very good”, “good”, “satisfactory”, “bad”. In addition, the level of anxiety was determined psychometrically using the Spielberger test, the level of depression was determined using the Beck scale, and the quality of life of patients was also assessed.
results
A neurological study showed that reflex muscular-tonic syndrome (MTS) - tension and pain on palpation of the paravertebral muscles, and in some cases the piriformis muscle - was present in all patients. At the same time, in 5 (17%) patients, in addition, clinical signs of radiculopathy of the L5 and S1 roots were detected - loss of the knee or Achilles tendon reflex, decreased pain and tactile sensitivity in the area of the corresponding root, paresthesia, weakness of the foot muscles (in 2) .
When analyzing the symptoms of tension in patients with radiculopathy, a true Lasegue symptom was noted, when pain when lifting a straightened limb radiated along the affected root all the way to the foot. In patients with only MTS, Lasegue's pseudo-symptom was observed, when raising the leg caused local pain either in the lower back, or in the hip, or under the knee, or in the lower leg, which was explained by stretching of the spasmodic muscles.
Thus, in 17% of patients, clinical neurological examination revealed signs of radiculopathy in combination with secondary reflex MTS, while in the remaining 83%, acute pain syndrome in the lower back was caused only by MTS.
During an X-ray examination of the spine, degenerative-dystrophic changes of varying severity, i.e. signs of osteochondrosis were determined in all patients. Neuroimaging studies, CT or MRI of the lumbar spine were performed in all patients with radiculopathy and in 5 (20%) patients with MTS only.
All tomograms revealed disc protrusions and/or hernias of varying severity, but in radiculopathy they were larger (7-10 mm), compressed the root or fatty tissue, and in one patient signs of spinal canal stenosis were determined. The intensity of spontaneous pain according to VAS was before treatment 4 points, and with movement more than 7.5 points, already an hour after the first injection of movalis it decreased significantly (p<0.05). A significant decrease in the severity of pain compared to both the background and the previous study was recorded after 5 days of treatment (end of the injection period) and after 14 days (completion of the study).
The reduction in pain was accompanied by a significant improvement in flexion in the lumbar spine when bending forward (decreasing the distance to the floor), an increase in lateral mobility of the spine (total - to the right and left), a decrease in the severity of Lasegue's symptom (increasing the angle of elevation of the straightened leg) and an increase in the pain threshold of pressure in the most painful point of the back (see figure). Before the start of therapy, patients with acute pain syndrome showed a significant decrease in the pain threshold compared to healthy subjects (n=13, 6.95 and 19.02 feet, respectively; p<0.05).
When movalis was prescribed, it increased after the first injection. At the end of the course of therapy (day 14), a significant increase was noted, approaching the values in healthy subjects (see figure). As can be seen from the table. 1, treatment of acute back pain with movalis led in the group as a whole to a significant weakening of secondary anxiety-depressive symptoms, an increase in the ability to work and the quality of life of patients.
Patients' subjective assessment of the results of treatment with movalis was generally positive: there were no cases of poor assessment. The rating “satisfactory” was given by 2 (7%) patients, “good” - 9 (30%), “very good” - 10 (33%), “excellent” - also 9 (30%).
Negative side effects during parenteral and subsequent enteral treatment with Movalis were observed in 2 patients. One patient with duodenal ulcer, without exacerbation, developed epigastric pain while taking movalis, which required corrective therapy with ranitidine, and the patient completed treatment. The second developed an attack of acute cholecystitis for the first time on the 10th day of therapy; the patient was transferred to the therapeutic department, and therefore treatment was interrupted.
In order to clarify the influence of objective and subjective indicators on the effectiveness of movalis, the dynamics of indicators were analyzed depending on gender, the etiological factor - MTS (25 patients), MTS + radiculopathy (5), the severity of depression on the Beck scale - less and more than 15 points (respectively 17 and 13 patients). In addition, we compared clinical and psychophysiological characteristics in patients with a pronounced effect of the drug (ratings “excellent” and “very good” - 19) and with a satisfactory effect (ratings “good” and “satisfactory” - 11).
When analyzing the indicators taking into account gender, no significant differences were noted between men and women, although women had slightly greater mobility in the lumbar spine. In patients with radiculopathy in general, treatment results were worse than in patients with only MTS, although the significance of the differences in this indicator was not determined due to the small number of patients with radiculopathy. Differences between patients with satisfactory and excellent treatment effects were revealed already on the 5th day treatment: in the former, the pain syndrome weakened significantly less, and mobility and flexion in the lumbar region improved to a lesser extent (Table 2).
The psychological characteristics of patients had the greatest impact on treatment results. Thus, in patients with clinically significant depression (more than 15 points on the Beck scale), they were worse than in patients with less pronounced affective disorders. This also affected the quality of life and ability to work (Table 3).
Discussion
The high effectiveness of movalis in relieving LBP syndrome has previously been noted both in multicenter foreign studies and in a recently completed study in Russia involving 767 patients with exacerbation of lumboischialgic syndrome [1]. The corresponding generalized results indicate that patients rated the treatment effect as good in 78.0% of cases, as satisfactory in 20.5% and as unsatisfactory in 1.5%. In our cases, there was no unsatisfactory assessment; only 7% of patients gave a satisfactory assessment, and the rest - good or excellent.
Thus, our study confirmed the high effectiveness of the drug in the treatment of acute LBP. Our obtained better results may be explained by the longer use of the injection form - 5 days (versus 3 days in the multicenter study mentioned above).
This regimen of its administration apparently helps to increase the effect of the course of treatment as a whole, since a significant reduction in pain and improvement in function are determined after the first injection of the drug. The safety of movalis that we noted confirms the results of its other studies [1, 6-8]. Some features are of interest. LBP in men and women.
It is known that women experience pain more often than men. This is due to a number of biological, socio-psychological and cultural factors. We are talking about different activities of pain - nociceptive and antinociceptive systems, lower levels of serotonin - one of the main antinociceptive mediators, more frequent visits by women to the doctor, their greater emotional lability and tendency to anxiety-depressive reactions, as well as rental attitudes in the presence of pain syndrome, etc. In addition, pain for a woman is a socially acceptable form of response to stress.
Movalis, as mentioned above, reduced back pain to the same extent in men and women. At the same time, the functional activity of the spine after treatment was higher in women, which may be due to greater natural flexibility in general, but the influence of the listed socio-psychological factors cannot be excluded.
In our study, reflex MTS was detected in all patients, and the pain was nociceptive in nature in 83% of cases, and in only 17% of patients muscle-tonic disorders were combined with root pain, i.e. there was mixed nociceptive and neuropathic pain. It was noted that patients with radiculopathy generally assessed the results of treatment with Movalis worse.
Unfortunately, we were unable to conduct a statistical assessment of such differences due to the small number of patients. The role of depression and anxiety-depressive disorders in the pathogenesis of chronic pain is widely discussed in the literature. Their presence is the main argument in favor of prescribing antidepressants to patients with chronic pain syndromes. Our research confirms this. A more pronounced positive effect of treatment with movalis was recorded in patients without depression.
Thus, emotional disorders of the depressive and anxiety spectrum not only play a significant role in the pathogenesis of chronic pain syndromes, but also significantly influence the results of treatment. With a high severity of emotional disturbances, chronicity of the disease is possible. All this determines the relevance of developing optimal regimens for the use of NSAIDs in combination with antidepressant and anti-anxiety drugs.
Literature
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- Voznesenskaya T.G., Vein A.M. In the book: A.M. Wayne, M.Ya. Avrutsky. Pain and pain relief. M: Medicine 1997; 98-126.
- Nasonov E.L. Non-steroidal anti-inflammatory drugs: problems of treatment safety. Consilium medicum 1999; 1:4:41-46.
- Nasonova V.A. The role of cyclooxygenase-2 in the development of pain. Ter Arch 2001; 5: 56-57.
- Shostak N.A., Nasonova V.A., Shemetov D.A., Arinina E.N. Low back pain as a multidisciplinary problem (review). Ter Arch 2000; 10: 57-60.
- Auvinet V., Ziller R., Appelboom T., Velicitat P. Comparison of onset and intensity of action of intramuscular meloxicam and oral meloxicam in patients with acute sciatica. Clin Therapeutics 1995; 6: 17: 1078-1090.7. Colberg K., Hettich M., Sigmund R. et al. The efficacy and tolerability of an 8-day administration of intravenous and oral meloxicam: a comparison with intramuscular and oral diclofenac in patients with acute lumbago. Curr Med Res Opin 1996; 13: 7: 363-377.8. Dreiser RL, Parc JM, Velicitat P., Leu PL Oral meloxicam is effective in acute sciatica: two randomized, double-blind trials versus placebo or diclofenac. Inflammation Res 2001; 50: Suppl 1: 17-23. Received 03/10/05
Source Journal of Neurology and Psychiatry named after. S.S. Korsakov No. 7 | 2005
Special instructions for the use of the drug Movalis:
- for patients with an increased risk of adverse reactions (history of gastrointestinal diseases, presence of risk factors for cardiovascular diseases), the recommended initial daily dose is 7.5 mg;
- For patients with severe renal failure on hemodialysis and the elderly, a dose of 7.5 mg/day is recommended, which should not be exceeded;
- patients with insufficient renal function in which Clcr exceeds 25 ml/min., patients with mild/moderate liver failure, as well as clinically stable cirrhosis do not require dose adjustment.
Important! The required dosage and course duration are determined by the attending physician.
Movalis during pregnancy and breastfeeding
As with other Pg (prostaglandin) inhibitors, meloxicam may have a negative effect on fertility. Therefore, when planning pregnancy, it is recommended to discontinue therapy with this drug.
Movalis during pregnancy
Suppression of prostaglandin synthesis has a negative impact on the development of pregnancy and/or the fetus. In particular, clinical data suggest that Movalis in the first and second trimesters of pregnancy increases the risk of miscarriages, as well as the chance of gastroschisis and heart defects in the fetus. Therefore, during this period, Movalis is prescribed by a doctor only if there is a real threat to the mother’s life.
As for the third trimester, taking the drug at this time can lead to abnormalities in fetal development:
- cardiorespiratory toxicity;
- renal dysfunction, which can develop into renal failure with oligohydramnios.
In addition, taking Movalis in the last weeks of pregnancy can provoke an increase in bleeding time, the development of an antiaggregation effect, inhibition of the ability of the smooth muscles of the uterus to contract, and this leads to a delay or disruption of the birth process.
The active component of Movalis easily passes into mother's breast milk, so it should not be taken during breastfeeding (breastfeeding).
Movalis and alcohol
Is it possible to combine Movalis with alcohol?
There is no clear prohibition on the simultaneous use of Movalis and alcohol in the instructions for use. True, this does not mean that such a combination will not cause harm. Thus, drinking alcohol during therapeutic treatment with the drug can lead to acute renal failure. This occurs due to dehydration, which is caused by alcohol.
Is it possible to take Milgamma, Movalis and Mydocalm at the same time?
If the pain is severe, causes discomfort, cannot be tolerated, and affects the usual rhythm of life, then the doctor may prescribe a combined treatment system. Milgamma and Mydocalm are often prescribed along with Movalis, which have shown good results in the treatment of certain diseases (intervertebral hernia, osteochondrosis). But before injecting Movalis, Milgamma and Mydocalm, you need to visit a doctor, since these drugs in any case have contraindications and the risk of developing negative reactions in the patient’s body.
- Movalis is a non-steroidal anti-inflammatory drug. Its use is indicated in the treatment of diseases of the musculoskeletal system to relieve inflammation, pain and lower temperature.
- Milgamma is a combined multivitamin product consisting of B vitamins. When diagnosing diseases of the musculoskeletal system, Milgamma injections are prescribed to improve blood circulation, nourish cartilage and bone tissue, and strengthen the nervous system.
- Mydocalm is a muscle relaxant. The drug relieves muscle spasms, reduces muscle tension, reduces compression of nerve endings and eliminates pain.
The classic treatment regimen with Movalis, Milgamma and Mydocalm looks like this: during the first three days, Movalis injections are administered once a day, then the patient is transferred to the tablet form of the drug. Milgamma is administered 2 ml IM once a day. Then injections are given two to three times a week, or the tablet form of Milgamma is prescribed.
Mydocalm injections (100 mg) are indicated 2 times a day, the dosage is 100 mg. To enhance the effect, injections can be given on the same day.
Thus, Movalis, Milgamma and Mydocalm are prescribed to eliminate the symptoms of the disease. Despite the fact that the drugs belong to different pharmacological groups, when used together they give positive dynamics during therapy.
It is worth remembering that for patients who are sensitive or intolerant to lidocaine, this treatment regimen is contraindicated.
V.V. Badokin
Russian Medical Academy of Postgraduate Education, Moscow
Nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most common medications used in clinical practice. They are a class of pharmacological agents that are associated with preventing the development or reducing the intensity of inflammation. In addition, they also have direct analgesic and antipyritic effects. NSAIDs are most widely used in rheumatology in the treatment of inflammatory and degenerative diseases of the joints and spine, microcrystalline arthropathy, diffuse connective tissue diseases, diseases of extra-articular soft tissues, a large group of diseases accompanied by pain in the lower back and bone diseases that are in the field of view of a rheumatologist . As is known, NSAIDs occupy a central place among symptom-modifying drugs in the treatment of rheumatoid arthritis, ankylosing spondylitis and other seronegative spondyloarthritis, osteoarthritis and many other diseases. They are first-line drugs and an obligate component of combination therapy for acute and chronic inflammatory and degenerative diseases of the joints and spine. Symptom-modifying drugs include, in addition to NSAIDs, glucocorticoids, simple analgesics and muscle relaxants. Their share in the treatment of the above diseases is far from equal, but NSAIDs are undoubtedly the leaders in this group of medications. NSAIDs are believed to have only symptomatic effects. They reduce the intensity of joint pain, the duration and severity of morning stiffness, and also improve the functional ability of the musculoskeletal system, without affecting the rate of development of structural changes in those diseases that are in the field of vision of rheumatologists. However, over the past 2 years, works have appeared where NSAIDs are considered as drugs that can actively interfere with the intimate mechanisms of the pathological process and influence the rate of radiological progression. This point of view has found its evidence in ankylosing spondylitis (H. Mielants, BV Cruyssen, 2006). As for rheumatoid arthritis, NSAIDs inhibit the hyperplasia of synoviocyte cells, which occupy one of the leading positions in the pathology of this disease, and in this regard they can also be considered not only as symptomatic agents. The main mechanism of action of NSAIDs is the suppression of prostaglandin biosynthesis. As is known, prostaglandins are characterized by a wide range of biological actions. They are mediators of inflammatory reactions, promote local vasodilation, the development of edema and exudation, sensitize receptors to pain mediators (histamine and bradykinin), lower the threshold of pain sensitivity and increase the sensitivity of the hypothalamic centers to the action of pyrogens. In addition, they regulate a large number of physiological processes in the body, including the secretion of gastric juice, trophism of the gastric mucosa and intestinal motility, take an active part in the functioning of the kidneys, microcirculation and vascular tone, regulate ovulation and promote the initiation of labor, participate in the metabolism of bone tissue, and control blood clotting, take part in the growth and development of nerves, wound healing, etc. [1, 2]. The pharmacological activity of NSAIDs is not limited only to the suppression of prostaglandin synthesis. In addition, they inhibit the synthesis of leukotrienes, the formation of superoxide radicals and the release of lysosomal enzymes, affect the activation of cell membranes, aggregation and adhesion of neutrophils, and the function of lymphocytes. This makes it clear why NSAIDs not only have positive (therapeutic) effects, but also have a wide range of undesirable side effects. The most common gastrointestinal disorders are observed, which can manifest as dyspepsia, the development of erosive gastritis and duodenitis, the formation of ulcers and their perforation, and gastric bleeding. In addition, NSAIDs have nephro- and hepatotoxicity, promote fluid retention and the development of heart failure, arterial hypertension, have a dystrophogenic effect on the myocardium, and affect the metabolism of brain cells. Hematological disorders are possible, including severe cytopenias, inhibition of platelet aggregation, allergic reactions and broncho-obstructive syndrome (“aspirin” asthma), which is associated with their effect on the production of leukotrienes. The main undesirable effects of NSAIDs:
• gastrointestinal (gastric and intestinal dyspepsia, erosive gastritis, enteropathy, ulcers, bleeding, perforation); • cardiac (arterial hypertension, myocardial dystrophy, circulatory failure, acute coronary insufficiency); • renal (decreased glomerular filtration rate, peripheral edema, interstitial nephritis); • hepatic (toxic hepatitis with cytolysis syndrome and protein synthesis deficiency); • cerebral disorders; • allergic (skin rashes, broncho-obstructive syndrome, “aspirin” bronchial asthma); • hematological (leukopenia, hypo- and aplastic anemia); • platelet (inhibition of platelet aggregation, increased risk of bleeding).
When choosing an NSAID and its daily dose, one should take into account the activity of the inflammatory process, the effectiveness and tolerability of specific drugs, the possibility of their combination with other types of therapy, and the presence of concomitant diseases. NSAIDs, as a class of pharmacological agents, are characterized by both general (group) and individual characteristics associated with the characteristics of their metabolism in the body, pharmacokinetics, COX (cyclooxygenase) selectivity, as well as various anti-inflammatory activities. Great importance should be given to identifying risk factors for adverse effects of NSAIDs, which include not only old age, a history of gastrointestinal pathology and concomitant diseases (arterial hypertension, heart failure, liver and kidney diseases), but also taking high doses of NSAIDs, combined NSAID therapy with glucocorticoids, low-dose aspirin or indirect anticoagulants. A significant reduction in the adverse effects of NSAIDs became possible with the advent of drugs that predominantly act on one of the COX isoforms - COX-2. These drugs include meloxicam (Movalis), which is a derivative of enoliconic acid. It, like all other NSAIDs, has anti-inflammatory, analgesic and antipyritic activity. More than 99.5% of movalis is protein bound. In synovial fluid, its concentration is 2 times less than in blood plasma, which helps suppress the inflammatory process in joint tissues. Its half-life is 20 hours, so it should be used once every day. The drug has cumulative properties and its maximum concentration occurs on days 3-5 of administration. To more quickly obtain a therapeutic effect, it is advisable to carry out the so-called “stepped” therapy, which consists of intramuscular administration of 15 mg of movalis in the first three days of treatment, and then transferring the patient to oral administration of the drug [3]. When carrying out combination therapy, movalis does not interact with other medications, including cytostatics, antihypertensives, diuretics, cardiac glycosides and beta blockers, which is of great importance in the treatment of patients with concomitant diseases. Quite high clinical effectiveness of movalis has been demonstrated in patients with rheumatoid arthritis, ankylosing spondylitis, osteoarthritis and diseases the main manifestation of which is pain in the lower back. According to a European multicenter placebo-controlled study, meloxicam in patients with rheumatoid arthritis showed higher anti-inflammatory efficacy compared to placebo [4]. A similar result was obtained during long-term randomized controlled studies, in which the effectiveness of various doses of movalis, diclofenac, naproxen and placebo was studied in a comparative aspect [5, 6]. Significant improvement occurred after 2 weeks. from the start of therapy with movalis, it remained throughout the entire period of treatment with this drug, i.e. for 18 months. Thus, the intensity of joint pain by the end of the second week decreased by 2 times and after 1.5 years from the start of therapy remained at the same level. When taking 7.5 and 15 mg of movalis, the positive dynamics of all studied parameters were more pronounced than with placebo, while with diclofenac a similar result was found in only three out of five parameters. In terms of its effectiveness, movalis was not inferior to such traditional NSAIDs as diclofenac, naproxen and piroxicam. Good results from treatment with movalis were also obtained in patients with ankylosing spondylitis in a long-term 12-month study. In terms of its therapeutic activity, 15 mg of movalis had the same effect as 20 mg of piroxicam. Increasing the dose to 22.5 mg/day was not accompanied by an increase in the anti-inflammatory and analgesic effect of this drug. Movalis, unlike piroxicam, improved the Dougados functional index [7, 8]. The largest number of studies on the clinical effectiveness and safety of movalis has been carried out in osteoarthritis. The prescription of NSAIDs for this disease is justified by the fact that, although osteoarthritis is a degenerative disease, the inflammatory process with localization in the synovium persists - secondary (reactive) synovitis, cartilage (chondritis), periarticular soft tissues (periarthritis) and subchondral bone tissue ( osteitis), which justifies the term “osteoarthritis,” which is widely used abroad. The inflammatory process in patients with osteoarthritis aggravates the progression of this disease. All this explains the need to use anti-inflammatory therapy for this disease, in particular NSAIDs. The positive effect of NSAIDs in osteoarthritis is determined not only by their anti-inflammatory effect, but also by a clear analgesic effect, especially since pain in this disease is one of its main manifestations. Reducing the intensity of pain or its complete relief leads not only to the subjective improvement of patients, but also to an increase in the mobility of the affected joints. NSAIDs are able to reduce the severity of joint pain, promote the resolution of exudative phenomena and restore range of motion in the affected joints, i.e., affect the main subjective and objective symptoms of osteoarthritis. Most patients with osteoarthritis take NSAIDs almost constantly, since they are drugs that have a rapid and pronounced therapeutic effect. Many of the studies conducted to evaluate meloxicam in osteoarthritis met modern requirements for testing medications, were multicenter, prospective, double-blind, and were performed according to a single protocol [9, 10, 11]. These studies comparatively analyzed the effectiveness and safety of meloxicam, diclofenac and piroxicam, both in short-term and relatively long-term trials. It turned out that all NSAIDs were comparable in their effectiveness. In a 12-week study, movalis 7.5 and 15 mg/day was as effective as diclofenac 100 mg. In this controlled trial, some patients took 3.75 mg/day of meloxicam. Such a small dose was superior in its therapeutic potential to placebo, although the difference was not statistically significant. The results of this study convincingly demonstrated the dose-dependent effect of the drug. The effectiveness of meloxicam was studied in the MELISSA (Meloxicam Large Scale International Study Safety Assessment) and SELECT (Safety and Efficacy Large scale Evaluation of COX inhibiting Therapies) studies. The therapeutic activity of movalis (7.5 mg/day) was compared with diclofenac (100 mg/day) or piroxicam (20 mg/day) [11, 12]. These two trials involved approximately 20,000 patients. Meloxicam was equivalent in its effectiveness to diclofenac and piroxicam, with a decrease in the intensity of joint pain, an improvement in general condition and objective signs of joint damage. Discontinuation of the drug due to its low effectiveness in all three groups was low and did not exceed 1.7%. A large randomized controlled trial was conducted in the USA to study the comparative effectiveness of NSAIDs [13]. 1309 patients were analyzed, 67% of whom were women. The average age was 64 g, and the average duration of the disease was 9 years. 662 patients took meloxicam 7.5 mg/day and 647 took other NSAIDs, including diclofenac, naproxen, ibuprofen, etodolac, piroxicam, sulindac, celecoxib, rofecoxib, etc. While taking meloxicam, treatment success was observed in 66.8% of patients and only in 45% - when taking other NSAIDs. The advisability of introducing movalis into the complex therapy of patients with osteoarthritis is dictated not only by its anti-inflammatory and analgesic activity, but also by the good tolerability of the drug. Interesting and important from a practical point of view are the data on the effect of movalis on the metabolism of hyaline (articular) cartilage, which is of paramount importance for the rational therapy of osteoarthritis. As is known, hyaline cartilage is, along with subchondral bone, the primary and main springboard for the development of the pathological process in this disease [14]. The effect of NSAIDs on cartilage metabolism appears to be multifaceted. There is a group of drugs that have a chondroneutral effect. However, most NSAIDs have a negative effect on the synthesis of the cartilage matrix and thereby contribute to the progression of osteoarthritis. They inhibit the metabolic activity of chondroblasts, reduce the synthesis of proteoglycans, type II collagen and hyaluronic acid, promote premature death of chondrocytes, increase cartilage degeneration and lead to the progression of osteoarthritis. Thus, indomethacin inhibits the synthesis of proteoglycans, type II collagen and hyaluronic acid by chondrocytes, and also promotes premature death of chondrocytes [15]. EC Huskisson et al. in a randomized controlled trial, joint space width was assessed in 812 patients with knee osteoarthritis [16]. While taking indomethacin, narrowing of the gap was observed in 47% of patients and only in 22% of patients on placebo. There are observations that the use of indomethacin in patients with osteoarthritis leads to rapid and significant impairment of the function of the hip joint and its subsequent replacement compared to those patients who were treated only with simple analgesics. It has previously been shown that salicylates, indomethacin, phenylbutazone, naproxen, ibuprofen and dexamethasone, administered intra-articularly, contributed to a more rapid development of articular cartilage and subchondral bone degeneration in rats and chickens, as evidenced by histology, stereoelectron microscopy, biochemical test studies and x-ray data. . However, not all NSAIDs contribute to the progression of osteoarthritis. It has been shown that some of them stimulate the metabolic activity of chondrocytes to synthesize a complete cartilage matrix. Stimulation of anabolic processes in cartilage tissue occurs through their inhibitory effect on the production of interleukin-1 and the expression of the receptor for this cytokine, as well as by intensifying the synthesis of growth factors, including transforming growth factor-b, inhibiting aggrecan degradation, neutralizing the damaging effects of metalloproteinases, and reducing the intensity of chondrocyte apoptosis [15, 17]. The chondrotropic effect of movalis has been actively studied both experimentally and in the clinic. Numerous in vitro studies have shown that it increases the synthesis of proteoglycans in explants of osteoarthritis cartilage obtained from patients with varying degrees of severity of degenerative disease, and also inhibits chondrocyte apoptosis [15, 18]. In addition, it does not express pro-inflammatory cytokines and, above all, IL-1. These data allow us to consider movalis not as a chondroneutral agent, as was previously thought, but as an NSAID with a distinct chondroprotective effect. The presented properties of meloxicam have also been proven in clinical studies. Long-term (for 18 months) treatment of patients with osteoarthritis with paracetamol, chondroitin sulfate, glycosamine sulfate and meloxicam showed that significant progression of the disease, according to X-ray examination and magnetic resonance imaging (MRI), was observed in those patients who took paracetamol. Further narrowing of the joint space was also observed in patients treated with structural analogues of cartilage, although significantly to a lesser extent than during treatment with paracetamol. As for movalis, its effectiveness, determined both by clinical indicators (WOMAC and Lequesne indices), and, more importantly, by the results of a dynamic study of X-ray and MRI data, turned out to be almost the same as when treated with chondroprotective drugs [19 ]. It seems that the positive effect of therapy with so-called chondroprotectors is primarily due to their anti-inflammatory properties. There is no doubt that this point of view requires additional evidence. When prescribing NSAIDs, gastrotoxicity is the most common problem. NSAID gastropathy is largely associated with the duration of action of individual drugs, differences in their systemic absorption, the basic pH value of gastric juice, but, above all, with the severity of suppression of prostaglandin synthesis. Adverse events that develop when taking COX-nonselective drugs are manifested in 30% of patients by gastric and intestinal intolerance, in 15% by endoscopically confirmed gastric ulcers, and in 1.7% by perforations or hemorrhages. Such severe gastroenterological complications as bleeding, perforation and ulcers in most cases occur without pain, which makes their timely diagnosis difficult and in some patients leads to death. The European pharmacoepidemiological multicenter prospective study assessed the tolerability and safety of movalis in comparison with other NSAIDs in patients with rheumatic diseases [20]. 2530 patients took Movalis, 1996 patients took other NSAIDs. The duration of therapy was 6 months. When taking movalis, adverse events such as abdominal pain (23 and 38, respectively), gastritis (2 and 12), dyspepsia (2 and 7) and gastrointestinal bleeding (2 and 10) were significantly less common compared to other NSAIDs. Interesting data were obtained in the 4-week MELISSA study, in which the tolerability of meloxicam 7.5 mg/day and diclofenac 100 mg/day was studied in 9323 patients with osteoarthritis. 27 countries took part in this study, including Russia [10, 21]. The overall frequency of gastrointestinal adverse events when prescribing diclofenac was significantly higher than when treating with movalis (19 and 13%, respectively), and according to E.S. Tsvetkova [21] – in 22.2 and 6.8%, respectively. The following were observed significantly less frequently: gastric dyspepsia, abdominal pain, nausea and vomiting, diarrhea. Due to the development of adverse gastroenterological events, diclofenac was discontinued 2 times more often than meloxicam. The overall tolerability of meloxicam, as assessed by doctors, was good in 91% and satisfactory in 9%, and the tolerability of diclofenac was good (84%), satisfactory (9%) and unsatisfactory (7%). Results similar to those described above were obtained in the SELECT study, in which meloxicam 7.5 mg/day was compared with piroxicam 20 mg/day in 8227 patients with osteoarthritis. The total number of gastrointestinal adverse events was detected in 10.2% of patients receiving therapy with movalis, and in 15.2% with piroxicam [12]. It is interesting to note that when using movalis, the risk of developing gastrointestinal complications was also lower in individuals taking aspirin simultaneously to prevent thromboembolic complications (10.3 and 15.4%). A meta-analysis of a large number of studies showed that movalis, compared with traditional NSAIDs (diclofenac, piroxicam and naproxen), reduces the risk of drug withdrawal due to the development of gastrointestinal complications by 41%, the risk of serious adverse reactions (perforation, ulceration, bleeding) - by 48% and the risk of intestinal dyspepsia by 27%. Movalis has not only a more favorable gastrointestinal safety profile compared to traditional NSAIDs, but also hepato- and nephrotoxicity [12, 21]. It significantly less frequently causes an increase in serum aminotransferase levels compared to diclofenac. Thus, when taking meloxicam, an increase in AST was registered in 3% of patients and ALT in 2%, and diclofenac in 9 and 2%, respectively. Increases in creatinine and urea levels were observed only during treatment with diclofenac. Recently, interest in NSAIDs with COX-2 selectivity has especially increased, which is associated with the possibility of their inducing thrombotic complications [9, 22]. It is now clear that the higher the selectivity of NSAIDs, the more likely the development of cardiovascular and cerebral thrombotic complications. This primarily applies to specific COX-2 inhibitors – coxibs. According to Layton (2003), cardiovascular thrombotic complications during long-term treatment with movalis are observed in 0.1% of patients, with Celebrex in 0.16% and rofecoxib in 0.14%, and cerebrovascular complications in 0.27; 0.39 and 0.48% respectively. These data served as the basis for limiting the widespread use of coxibs. According to the FDA and the European Medicines Agency, a contraindication to the use of specific COX-2 inhibitors is coronary heart disease (CHD) or a history of stroke. They should be used with caution in persons with risk factors for coronary artery disease. How can one explain the different effects of movalis and coxibs on platelet aggregation? First, movalis is structurally different from coxibs. In particular, it binds to the upper part of the COX-2 channel. Secondly, it has a balanced profile of COX-2 selectivity. As is known, highly selective coxibs associated with the side pocket of the COX-2 channel inhibit thromboxane less, and this explains the increased risk of thromboembolic complications, since thromboxane takes an active part in platelet aggregation. As for meloxicam, it not only does not have cardiotoxicity, but, on the contrary, in RA patients with coronary artery disease it contributes to a less frequent occurrence of arrhythmias and a reduction in the duration of myocardial ischemia compared to similar indicators in patients treated with non-selective COX inhibitors [23]. Thus, movalis has a distinct anti-inflammatory and analgesic effect, as well as good tolerability. These properties contributed to its introduction into complex therapy for the vast majority of inflammatory diseases of the joints and spine. In osteoarthritis, it affects the main subjective and objective symptoms. Particularly interesting is the effect of movalis on hyaline cartilage, which allows it to be considered as a potential chondroprotective drug, in contrast to most NSAIDs, which contribute to the inhibition of the synthesis of the intercellular cartilage matrix and, accordingly, the progression of osteoarthritis.
Literature 1. Nasonov E.L. Modern teaching on selective COX-2 inhibitors: new aspects of the use of meloxicam (Movalis) // Scientific and practical rheumatol. 2001; 1:58-62. 2. Schwartz G.Ya. Modern non-steroidal anti-inflammatory drugs. M: Reaform, 2004. 3. Tsvetkova EC Evaluation of the effectiveness of movalis in osteoarthritis and rheumatoid arthritis (data from a multicenter Russian study) // Scientific and practical rheumatol. 2005; 2:29-31. 4. Lemmel E.M., Bolten W., Burgos-Vargas R. et al. Efficacy and safety of meloхicam in patients with rheumatoid arthritis // J Rheumatol. 1997; 24: 282-90. 5. Huskinsson EC, Ghozlan R., Kurthen R. et al. A long-term study to evaluate the safety and efficacy of meloхicam therapy in patients with rheumatoid arthritis // Br J Rheumatol. 1996; 35: Suppl 1: 29-34. 6. Wojtulewsky JA, Schattenkirchner M., Barselo P. et al. A six-month double-blend trial to compare the efficacy and safety of meloхicam 7.5 and naproхen 750 mg daily in patients with rheumatoid arthritis // Br J Rheumatol. 1996; 35: Suppl 1: 22-8. 7. Dougados M., Guerguen A., Nakasche JP et al. Ankylosing spondylitis: what is the optimal duration of the clinical study? A one year versus a 6 weeks non-steroidal anti-inflammatory drug trial // Rheumatology (Oxford). 1999; 38: 235-44. 8. Engelhardt G., Homma D., Schlegel K. et al. Anti-inflammatory, analgesic, antipyretic and related properties of meloхicam, a new non-steroidal anti-inflammatory agent with favorable gastrointestinal tolerance // Inflamm Res. 1995; 44: 423-33. 9. Ushkalova E.A. Cardiotoxicity is a group property of coxibs // Farmateka 2005; 7: 71-78. 10. Hawkey C., Kahan A., Steinbruck K. et al. Gastrointestinal tolerance of meloхicam compared to diclofenac in osteoarthritis patients. International MELISSA Study Group. Melochicam Large Scale International Study Safety Assessment // Br J Rheumatol. 1988; 37: 937-45. 11. Hosie J., Distel M., Bluhmki E. Melochicam in osteoarthritis: a 6-month, double-blind comparison with diclofenac sodium // Br J Rheumatol. 1996; 35: Suppl: 39-43. 12. Dequeker J., Hawkey C., Kahan A. et al. Improvement in gastrointestinal tolerability on the selective cyclooхygenase (COX)-2 inhibitor meloхicam, compared with piroхicam: results of the Safety and Efficacy Large scale Evaluation of COX inhibiting Therapies (SELECT) trial in osteoarthritis // Br J Rheumatol. 1998; 37: 946-51. 13. Gagnier P., Singh G., Reed JI et al. The effect of meloхicam versus usual care NSAIDS for the treatment of osteoarthritis in usual care setting. The results of the IMPROVE trial // Ann Rheum Dis. 2001; 60: Suppl 1: 235. 14. Nasonova V.A. Meloxicam (movalis) – a selective COX-2 inhibitor in clinical practice // Scientific and practical rheumatol. 2000; 4: 16-21. 15. Ding C. Do NSAIDs affect the progression of osteoarthritis? Inflammation 2002; 26: 139-42. 16. Huskinsson EC, Berry P, Gishen P. Effects of antiinflammatory drugs on the progression of osteoarthritis of the knee // J Rheumatol 1995; 22: 1941-46. 17. HenrotinY., Reginster T. In vitro difference among nonasteroidal antiinflammatory drugs in their activities related to osteoarthritis pathophysiology // Osteoarthritis Cartilage 1999; 7: 355-7. 18. Blot L., Marcelis A., Devogelaer JP, Manicourt DH Effects of diclofenac, aceclofenac and meloхicam of proteoglycans and hyaluronan in osteoarthritic human cartilage // Br J Pharmacol. 2000; 131: 1413-21. 19. Ionichenok N.G., Tsvetkova E.S., Karusinov P.S. and others. The influence of modern therapy on the progression of osteoarthritis of the knee joints // Scientific and practical rheumatol. 2005; 3: 51. 20. Degner F., Lanes S., van Ryn J., Sigmund R. Pharmacological and clinical profile of meloхicam. Therapeutic roles of selective COX-2 inhibitors / Eds Vane JR, Botting RM. William Harvey Press, London, 2001. 21. Tsvetkova E.S. Movalis in the treatment of osteoarthritis // Scientific and practical rheumatol. 2001; 1: 67-71. 22. Nasonov E.L. Cardiovascular effects of anti-inflammatory drugs // Scientific and practical rheumatol / 2003; 3:28-31. 23. Mazurov V.I. Use of meloxicam (Movalis) in patients with rheumatic diseases with concomitant coronary heart disease // Klin Med. 2004; 12:54-9.
Analogs
Analogues of Movalis on the pharmaceutical market are the following drugs: Mirlox, Artrosan, Melox, Meloxicam, Mataren.
As for Movalis injections, the doctor can replace them with medications containing the same active ingredient: Amelotex, Arthrozan, Meloxicam, Melbek, Liberum, Bi-xicam, Movasin, Mesipol.
Analogues of the drug Movalis
Movalis/Meloxicam
The drugs are based on the same active substance, so their therapeutic effect is identical. The only difference is the price.
Movalis/Voltaren
The active substance of Voltaren is diclofenac. Frequent development of side effects is noted. Unlike Voltaren, Movalis has a positive effect on cartilage metabolism. Therefore, both drugs are effective for pain relief, but for osteoarthritis, Movalis is better.
Movalis/Nise
The active substance of Nise is nimesulide. Both drugs are characterized by effectiveness in treating heat, inflammation and pain.
But nimesulide is toxic to the liver, but Movalis is not and does not have a similar effect.
Movalis relieves pain more slowly, but its effect is prolonged, while Nise is good for quickly relieving pain.
Mechanism of action of meloxicam
Any inflammation cannot develop on its own. We need special mediators, or carriers. They are called prostaglandins and are produced by the metabolism of arachidonic acid. It is prostaglandins that trigger the release of biologically active substances from mast cells, which initiate inflammation, pain and dysfunction. These substances include, for example, histamine. For this cascade of reactions to work, the work of cyclooxygenase, COX, is needed, a special enzyme that plays a critical role in the development of inflammation. It is with COX that non-steroidal anti-inflammatory compounds work, including Movalis.
It is very important to understand that this enzyme has two varieties, which are abbreviated as cyclooxygenase type 1 and 2, COX-1 and COX-2. It is COX-2 that causes specific inflammation in any tissue, and type 1 enzyme (COX-1) is necessary to maintain the normal mucous membrane of the stomach and duodenum. And if you block COX-1 and COX-2 at once, then as a side effect you will develop stomach ulcers, erosive gastritis and other diseases that are well known as complications from taking NSAIDs. More precisely, not all NSAIDs, but only first-generation drugs. This is the well-known Diclofenac, ibuprofen and other drugs.
They really help, they are highly active, relieve pain well, but at the same time they block both types of cyclooxygenase, and the most common side effect is heartburn, and with long-term use - exacerbation of stomach ulcers, even bleeding. Since these first-generation drugs did not make any difference between the two types of COX enzymes and blocked both types, these drugs were called non-selective COX inhibitors. Movalis is a selective COX-2 inhibitor that leaves type 1 enzyme alone, does not damage the stomach, and at the same time works only with type 2 cyclooxygenase.
Of course, meloxicam and Movalis still have a slight effect on type 1 cyclooxygenase, but tens and hundreds of times weaker than older, non-selective drugs. This means that Meloxicam (Movalis) is much safer than the same Diclofenac. Therefore, side effects such as heartburn and exacerbation of peptic ulcers occur much less frequently when using Movalis.