Diclofenac sodium: instructions for use, release forms, analogs, reviews
Various diseases of the musculoskeletal system not only have a negative impact on the patient's vital activity, but also cause him a lot of discomfort and inconvenience. Very often, diseases are accompanied by pain and stiffness of movements, which limits the patient's working capacity and affects his communication with others.
In such cases, doctors prescribe a drug such as “Diclofenac Sodium”. Instructions for use of this medication are of interest to many. What is this tool? What explains the effectiveness of its use? How to take the drug to achieve the maximum therapeutic effect? What contraindications and side effects should be remembered when using this remedy in your treatment? And finally, are there analogs of “Diclofenac sodium” with similar pharmacological properties? All this will be discussed in this review.
The most important thing is the active substance.
“Diclofenac sodium” is a non-steroidal anti-inflammatory substance derived from phenylacetic acid. In pharmacology, it is used in the form of sodium salt. The substance is actively used in medicine since 1966. Initially, it was used in the treatment of rheumatological diseases only. However, now preparations based on this component are used in various fields of surgery, gynecology, oncology, ophthalmology, neurology, and so on.
Despite the fact that the use of diclofenac sodium is actively practiced in many areas of medicine, some experts recommend banning drugs based on it. They explain this by the fact that such drugs can cause a heart attack or some other serious cardiovascular disease with long-term use.
Dosage Forms and Composition
“Diclofenac sodium” is available in the form of tablets, capsules, suppositories (or suppositories), solution for injection, gels and ointments. We will understand this in more detail:
- Tablets “Diclofenac sodium”. Each pill contains fifty milligrams of active ingredient.Auxiliary substances are lactose monohydrate, polyvinylpyrrolidone, colloidal silicon dioxide, magnesium stearate, starch, microcrystalline cellulose, gelatin, titanium dioxide, shellac wax, ammonium methacrylate copolymer, dye, PEG-600, purified sugar, propylene glycol, propylene glycol, propylene glycol, methylene glycollate, dye, polyethylene glycol Each tablet is coated with an enteric coating.
- Capsules The amount of active ingredient in this form of the drug is reduced in comparison with tablets and is equal to 25 milligrams. The composition of the capsule shell includes components such as titanium dioxide, gelatin, erythrosine, iron oxide, indigotin. The capsule filler is a light powder, the auxiliary components of which are lactose monohydrate monohydrate and magnesium stearate.
- Injections “Diclofenac sodium”. The instructions for use explains that the injection solution is a clear (with a yellowish tinge) liquid with a slight, specific odor. The drug is packaged in glass ampoules of three milliliters). One milliliter of solution contains 25 milligrams of active ingredient. Additional components include water for injection, sodium metabisulfite, benzyl alcohol, propylene glycol, mannitol, sodium hydroxide.
- Candles “Diclofenac sodium” for rectal use. Each suppository has a torpedo shape. It consists of fifty milligrams of active substance. Additional ingredients include colloidal silicon dioxide, solid fat and propylene glycol.
- Ointment “Diclofenac sodium”. The instructions for use contain information on the composition of this external agent. A thousand milligrams of ointment contains ten milligrams of the active ingredient. Additional components include propylene glycol, macrogol 1500 and 400, dimethyl sulfoxide. The drug is a white ointment with a mild specific smell.
- Gel. According to the annotation to the drug, a thousand milligrams of the drug contains ten milligrams of the active ingredient. Auxiliary substances are propylene glycol, methyl parahydroxybenzoate, carbomer 940, ethanol (96%), glycerin, purified water, ammonia solution 15%. The product is a seemingly transparent jelly-like substance with a low specific odor.
What makes a therapeutic effect from the use of the drug?
Pharmacological characteristics of the substance
As mentioned above, “Diclofenac sodium” is a remedy that has anti-inflammatory, analgesic and even antipyretic effect, used most often for rheumatic ailments, less often for blood thinning. Anti-inflammatory result is achieved due to the fact that the substance is able to inhibit the activity of cyclooxygenase. COX is an enzyme that participates in the metabolic processes of arachidonic acid, called the precursor of prostaglandins, which are responsible for the development of inflammation, fever and painful sensations.
The analgesic effect is achieved not only due to inhibition of prostaglandin synthesis, but also due to its inhibition in the nervous system (both central and peripheral).
Anti-inflammatory and analgesic effect of the drug allows its use in various rheumatic pathologies. This eliminates or minimizes such unpleasant symptoms as pain in the joints in motion and rest, morning stiffness, swelling or swelling of the joints, and so on.
Studies in the laboratory have proventhat this substance does not inhibit the synthesis process (or compound) of cartilage proteoglycans, if taken in therapeutically correct dosages.
It is noteworthy that “Diclofenac sodium” is actively used in non-rheumatic pain syndrome. The substance is able to eliminate pain and swelling at the site of the wound. In addition, it lowers platelet aggregation, reduces the severity of blood loss with heavy menstruation, in some cases, is used as an anti-allergic agent, especially with prolonged use.
What effect does the use of Diclofenac Sodium ointment have on the human body? When applied externally, the active ingredient penetrates deep into the joint tissue. Within seven to fourteen days, the necessary therapeutic effect is observed. Pain and swelling decrease, the possibility of movement increases.
Pharmacokinetic features of the drug
How is the active substance absorbed by the drug, getting inside the human body? “Diclofenac sodium” is almost immediately absorbed through the intestinal walls.Meal does not affect the amount of absorption of the substance, but slows down this process a little. If you take fifty milligrams of the active ingredient once, then in two hours its maximum amount will be noted in the blood. If you follow the schedule of taking the drug, it will not accumulate in the human body.
Almost one hundred percent of the component of interest to us is bound to plasma proteins, after which it penetrates into synovial fluids, where its maximum concentration is reached four to six hours after ingestion and can be saved in such quantity for twelve hours. During metabolism, the substance breaks down into several metabolites, two of which retain relative biological activity, while the rest are converted into glucuronic conjugates.
“Diclofenac sodium” is shown with urine as glucuronides and glucuron conjugates (about sixty percent). Only one percent of the substance is displayed in unchanged condition. The remaining forty percent of the drug is excreted through the liver and bile. The half-life process usually does not exceed two hours.
This information refers to the pharmacokinetic features of the tablet and injectable form of the drug. What processes occur when the active substance enters the human body through suppositories? The absorption rate of “Diclofenac sodium” with rectal administration of the drug is slightly lower than with the use of tablets, capsules or solution for injection. However, the maximum concentration of a substance in the blood is reached within an hour after applying candles. Its value is 2/3 less than the figure corresponding to the identical dosage taken orally in the form of tablets. When using rectal suppositories strictly according to a doctor's prescription, the cumulation of the active substance should not be observed.
In the external application of the gel and ointment, the absorption of the active component depends on the area of application of the drug and the individual characteristics of the epidermis. Studies have shown that the absorption of the ointment is six percent, while the gel is absorbed by 3.3 percent. Through the skin, the active substance penetrates into the blood plasma, however, its concentration is one hundred times lower than this indicator in oral administration of the drug.For better absorption of “Diclofenac sodium”, it is recommended to use an occlusive dressing for ten consecutive hours.
Indications for use of the drug
In which cases are prescribed pills and candles “Diclofenac sodium”? First of all, with such conditions and ailments:
- Various inflammatory or degenerative processes occurring in the musculoskeletal system. First of all, these are the types of arthritis such as chronic, rheumatoid, juvenile, as well as osteoarthritis, ankylosing spondylitis, spondylitis, osteoarthritis.
- Diseases of the spine, which are accompanied by severe pain. These diseases include radiculitis, lumbago, neuralgia, sciatica, myalgia, ossalgia, arthralgia.
- Rheumatic ailments occurring in extraarticular tissues. These can be various inflammatory processes in soft tissues, such as ligaments, tendons, muscles, nerves, and even joint bags.
- Attacks of gout, accompanied by a strong pain syndrome.
- Severe pain that occurs on the background of injuries or surgery and manifested in the form of swelling and inflammation.These may be surgical, orthopedic and even dental interventions.
- Some gynecological pathologies, such as adnexitis or severe pain during menstruation.
In some cases, the attending physician may consider it expedient to prescribe tablets in combination with other drugs in case of severe such ENT diseases as otitis, tonsillitis, pharyngitis. “Diclofenac sodium” in the form of suppositories can be prescribed for severe migraine attacks.
In what cases does a specialist recommend parenteral administration of the active substance, that is, in the form of injections? “Diclofenac sodium” in ampoules can be administered either intramuscularly or intravenously. Most often, the introduction of the drug into the muscle is carried out with various types of rheumatism, rheumatoid arthritis, spondylitis, gout attacks, severe migraine attacks, postoperative or post-traumatic pain syndromes, renal or hepatic colic. For pronounced pain after various surgical interventions, the analgesic solution can be administered as intravenous infusions.
Very often, “Diclofenac sodium” is prescribed for topical administration. The use of ointment or gel is possible with various soft tissue injuries (dislocations, sprains, hematomas, back pain with fatigue). It is also possible to apply a local drug with tendinitis, bursitis, periatropathy, algo-dystrophic syndrome, osteoarthritis (joints of the fingers, knee), arthrosis, and so on.
In what cases it is impossible to use “Diclofenac sodium”? Let's find out.
Regardless of the form of release, “Diclofenac sodium” cannot be taken with individual intolerance of both the active substance and auxiliary components, as well as when carrying a child (especially during the third trimester) and breastfeeding. In addition, if a patient has a history of attacks of bronchial asthma, acute rhinitis, or urticaria, the attending physician will not prescribe drugs that include the component of interest to us.
According to the instructions for use, the “Diclofenac sodium” tablet form cannot be recommended in the case of such conditions:
- Exacerbation of peptic ulcer of the gastrointestinal tract.
- Pathology of blood formation of unexplained etiology.
- Severe abnormalities in the liver or kidneys.
- The age of patients under six years.
- Galactose intolerance, glucose-galactose malabsorption, severe lactase deficiency.
- Blood clotting disorders of various etiologies.
The pills will be used with caution in patients suffering from systemic lupus erythematosus, moderately severe liver and kidney dysfunctions, high blood pressure, heart failure, chronic obstructive or infectious diseases of the respiratory system, as well as elderly people.
Contraindications to the use of “Diclofenac sodium” capsules are such conditions and ailments as gastric ulcers, gastrointestinal bleeding, renal or hepatic insufficiency, ischemic disease accompanied by angina pectoris or a stroke, galactose intolerance, glucose-galactose malabsorption, lactation deficiency lactate lactate lactate lactate, stroke deficiency, lactose deficiency, gastrointestinal heart failure, diseases associated with peripheral arteries, children up to the age of fourteen (in some cases, admission is allowed after eight years).In addition, the drug is not recommended for painful sensations after coronary artery bypass grafting, or when used in the treatment of a cardiopulmonary bypass.
Are there any contraindications for use of the drug in the form of injection solution? Yes, the above mentioned conditions are among the main warnings. Also, the doctor will not prescribe intramuscular or intravenous injections based on diclofenac for children under eighteen years of age, patients suffering from severe dehydration, and also in situations where there is an increased risk of various bleeding.
The main contraindications for the introduction of suppositories are ulcers of the gastrointestinal tract, proctitis, impaired blood formation, hepatic or renal failure, the patient is under fifteen years old. Relative contraindications of candles based on diclofenac include arterial hypertension, heart failure, nasal polyposis, hay fever, obstructive respiratory diseases. Suppositories for older people are also carefully prescribed.
Is it safe to use “Diclofenac Sodium” for external use? Doctors do not recommend applying gel or ointment to damaged or inflamed areas of the epidermis. Also, caution is prescribed external means for adolescents, elderly people and patients with a history of gastrointestinal ulcers, heart failure, bronchial asthma, kidney or liver dysfunction.
How should drugs based on diclofenac be used to achieve the desired therapeutic effect?
Recommendations for use
For tablets, the doctor may recommend one to three pills for adults (50-150 milligrams of active ingredient) per day. Children from six to fourteen years old daily dosage is calculated according to the body weight of the child (one to two milligrams per kilogram of weight). Tablets should be taken two to three times a day with or after meals.
Capsules should be consumed before meals, also twice or thrice a day. Patients older than fourteen years are prescribed four to six capsules (100-150 milligrams of the active ingredient) for pronounced ailments and three to four capsules (75-100 milligrams) for a moderate course of the disease.For children from eight years of age, the dosage is calculated on the basis of the weight of the small patient (0.5-2 milligrams of the active substance per kilogram of the child’s body weight). With painful menstruation, women can take from two to six capsules per day.
And what about injection solution? According to the instructions for use, parenteral administration of diclofenac should not last more than two days. Intramuscularly should be administered 75 milligrams of the drug (or three milliliters of solution) once a day. With a pronounced pain syndrome (for example, with colic), two hours after the first injection, you can enter another dose of diclofenac, but already into another buttock. In most cases, the use of injections and oral (or rectal) administration of the drug is practiced. With such treatment, care must be taken not to exceed the daily dosage of “Diclofenac sodium” in 150 (less often in 175) milligrams.
How to administer medication intravenously? This is done using infusions. The drug is diluted in 100-500 milliliters of the prepared liquid (0.9 percent NaCl solution or 5 percent glucose solution, previously buffered with edible soda solution).The dosage regimen for severe pain syndrome involves the use of a single vial of “Diclofenac sodium” (75 milligrams). The duration of continuous infusion varies between half an hour and two hours. For the prevention of postoperative pain, a dosage of 25-50 milligrams of the active substance is prescribed. The drug should be administered fifteen to sixty minutes after surgery.
How to apply for the treatment of candles? Usually, one suppository is administered twice a day for two weeks. Less commonly, the doctor recommends injecting the drug three times a day.
How to use diclofenac based gel? Depending on the affected area, apply the required amount of the drug three or four times a day for two to three weeks. The ointment is used twice or three times a day. Rinse hands thoroughly after application.
According to reviews, “Diclofenac sodium” can cause unpleasant side effects in the form of allergic reactions (edema, urticaria, itching of the skin) and mental disorders (depression, insomnia, nightmares).Dizziness, vomiting or nausea, development of anemia, tinnitus, asthmatic symptoms and many other unpleasant conditions are also possible.
Interactions with other medicines
“Diclofenac sodium” is not recommended for use with anticoagulants and antithrombotic agents because of the increased risk of bleeding. Also, the drug is better not to use in conjunction with diuretic and antidiabetic agents, cardiac glycosides, and so on.
Do I need a prescription for Diclofenac Sodium? According to the instructions for use, the gel and ointment will be sold to you at the pharmacy without permission from the doctor. But to buy tablets, candles and capsules should bring a prescription.
Analogs of the drug
Medications such as Olfen, Voltaren, Naproxen, Diklak and others can be considered substitutes for this drug. It is noteworthy that these drugs are presented on the pharmacological market in the form of tablets, solutions for injections, suppositories and means for external use.
What people say
Patients are satisfied with the use of “Diclofenac sodium” as an analgesic and anti-inflammatory agent.Many say that the best pain syndrome eliminates the solution for injection. Other patients praise the ointment based on the active ingredient. For others, a convenient form of release is a suppository for rectal use.