Composition of the injection form of Diclofenac
One milliliter of injection solution contains 25 mg of the active ingredient diclofenac sodium. The structure of the active component of the drug is a derivative of phenylacetic acid. The solution is available in ampoules of 3 milliliters. Its additional components include purified water and benzyl alcohol. Diclofenac for injection is produced in cardboard packages of 5 or 10 ampoules.
Is Diclofenac injection painful?
Diclofenac is considered a painful injection; after injection into the buttock, swelling and hardening often occur. If the technique is incorrect (shallow injection), suppuration and destruction of the subcutaneous tissue are possible.
After your leg hurts: what to do?
If there is only pain in the leg, but no numbness or muscle weakness, then an iodine mesh is prescribed to reduce pain. A medical consultation is required if the body temperature increases or the pain does not decrease by day 3. Based on the examination results, the doctor may prescribe:
- heating UHF, ultrasound;
- antibiotics in tablets;
- applications with Vishnevsky ointment;
- compress with Dimexide solution - add 40 ml of boiled water and 3 ml of Dioxidin solution or 2 ml of Gentamicin to 10 ml.
Compress with Dimexide
If suppuration occurs, surgery is performed.
Pharmacodynamics of the drug
The medicine Diclofenac has the following effects:
- anti-inflammatory;
- analgesic;
- antipyretic.
The explanation for the effectiveness of the active substance lies in the inhibitory effect on cyclooxygenase. In connection with it, the reactions of prostaglandin formation are inhibited, and platelet aggregation reactions are suppressed.
Diclofenac eliminates pain, joint stiffness, and restores their functionality. If necessary, use in cases of post-traumatic and postoperative complications helps relieve spontaneous pain and pain during movements.
Pharmacokinetics of the drug
Features of the pharmacokinetics of the injection form of Diclofenac are presented in the table.
Suction | After entering the muscle tissue, absorption starts immediately. The maximum content in the blood is reached 10-20 minutes after the injection. If the preferred time intervals between injections of the drug are observed, then cumulation does not occur |
Distribution | 99.7% of the active substance binds to blood proteins (99.4% to albumin). The active component of the drug has the ability to penetrate into the joint fluid. Here the maximum value of its content is possible after 2-4 hours. After 2 hours after reaching the peak content of diclofenac in the blood, the content of the drug component in the joint fluid exceeds that in the serum. High concentrations of the active substance in the joint fluid persist for another 12 hours |
Biotransformation | Metabolic transformations of diclofenac consist of glucuronidation of the original molecules (partially), methoxylation and hydroxylation (mainly) of the substance to the formation of intermediate metabolites, which are subsequently converted into glucuronic conjugated molecules |
Removal | The half-life of diclofenac is 1-2 hours. Its metabolites have a slightly longer half-life. 60% of the drug is excreted in the form of glucuronic conjugates in the urine. The remaining amount of the active ingredient after a series of metabolic transformations is excreted in bile and subsequently in feces |
Range of indications for injections
Indications for the use of Diclofenac solution for intramuscular injection:
- joint pathologies of inflammatory origin (gouty, rheumatic, rheumatoid arthritis);
- degenerative-dystrophic joint diseases (osteochondrosis, arthrosis);
- myalgia, neuralgia, sciatica, lumbago;
- pathologies of extra-articular structures (bursitis, tendovaginitis, rheumatic lesions);
- complications after injuries and operations.
What does the drug in injection form help with, besides diseases of the musculoskeletal system? Diclofenac is also prescribed for adnexitis, migraine attacks, hepatic and renal colic, infectious processes of the airways, and pneumonia.
You cannot prescribe this medicine yourself. This can cause serious undesirable consequences from the cardiovascular, nervous, digestive and other systems. The medication can be prescribed by the attending physician if there are indications and there are no restrictions on use.
Most often, Diclofenac enters the body of animals in one of the following ways:
A) The owner left his medications in an accessible place, and the pet ate them (this happens not only with medications, but also with foreign objects that would seem completely unattractive as food).
B) The owner noticed signs of pain in his pet and decided to help cope with this condition by using (by analogy with the human body) an anesthetic drug from his personal first aid kit.
C) It also happens that the pet begins to limp. The owner decides to apply Diclofenac to the sore limb. The pet, in turn, did not tolerate the strange substance on itself and licked it all off.
How to use and dose the medicine
The instructions for use of the injection form of Diclofenac suggest the following dosage regimen: 75 mg of the active substance (one ampoule) once a day. The dosage for adults can be adjusted to a maximum of 150 mg (two ampoules) per day. How many days this drug can be injected is determined by the attending physician, based on the characteristics of the patient’s condition. However, the course of treatment with Diclofenac should not exceed 5 days.
Most often, this medicine is prescribed as an initial therapy. How many injections of Diclofenac can be given depends on whether the injection form of the medication is combined with rectal or tablet form, since the total dose of the active ingredient per day should not exceed 150 mg. If you use suppositories or take tablets at the same time, you can inject the medicine only in the volume of one ampoule (75 mg).
How to give Diclofenac injections? The injection solution is drawn into a syringe and injected intramuscularly into the uppermost gluteal quadrant; You must first disinfect the injection site. The next day, the injection is given in the other buttock.
The attending physician should explain how to inject and how often Diclofenac injections can be given. It is important to follow the recommendations of a specialist.
Diclofenac injections: how to do and where
Diclofenac injections are given intramuscularly (in the buttock) and into a vein (dropper). The main rule for self-administration is maintaining sterility. It is also necessary to immerse the needle deeply and select the correct injection site.
How to inject intramuscularly into the buttock
When injecting Diclofenac into the buttock, you must first find the upper outer quadrant. To do this, the first time it is best to draw two stripes on the skin with iodine - the first divides the buttock in half vertically, and the second horizontally. The injection site should be the part closest to the lower back and side surface. The injection area should not be hard or painful.
Sequence of use of Diclofenac ampoule solution:
- Open the ampoule.
- Draw up all the contents into a 5 ml syringe.
- Release excess air.
- Wipe the injection site with an alcohol swab.
- With a confident and quick movement, pierce the skin so that the syringe is at an angle of 90 degrees and the needle enters 3/4 of the soft tissue.
- Release the solution from the syringe very slowly.
- Remove the needle and cover the injection area with an alcohol swab.
Is it possible to keep up?
Diclofenac can be injected into the leg, but this method can be more painful, since the skin of the thigh contains more nerve fibers and blood vessels. To inject the drug you need:
- Sit on a chair with your leg bent at a 90-degree angle and firmly on the floor.
- Choose a place on the outer lateral surface of the thigh approximately in the middle.
- Wipe the injection area with alcohol.
- Quickly pierce the skin and insert the needle 2 cm.
- Slowly release the solution into the muscle.
- Remove the needle and apply pressure to the injection site with an alcohol swab.
At the next injection, be sure to change sides - the injection is given in the other thigh.
Shoulder injection
Diclofenac is not recommended for injection into the shoulder because:
- compaction and suppuration often occur in this area;
- the accumulation of the drug slowly resolves;
- the injection is very painful.
In exceptional cases, the injection is carried out by a specialist, since it is impossible to perform it correctly on your own. The injection site is chosen at the border of the upper and middle third along the outer surface.
How to inject yourself, dosage
If you have to inject Diclofenac yourself, it is important to adhere to the basic rules of injection:
- dosage for 1 time – 3 ml (75 mg), in case of severe pain, a second injection is allowed after 6-8 hours;
- deep intramuscularly;
- in compliance with sterility - wash your hands with soap, put on sterile gloves, do not touch anything with the needle after drawing the solution;
- If pain and/or hardening occurs, an iodine mesh is applied.
Self-administering Diclofenac is dangerous, as even injections administered by trained nurses can lead to thickening, long-term pain and numbness in the leg.
How to inject - slowly or quickly
Diclofenac is always administered as slowly as possible. This helps it gradually spread through the soft tissues and more quickly absorb the injected substance. For intramuscular injections, to slowly deliver the drug, gently press the piston.
How to open an ampoule
To open an ampoule of Diclofenac with a dot, you need to take it in your left hand (with the dot facing you), and in your right hand - a sterile napkin or cotton pad moistened with alcohol. Cover the tip of the ampoule with an alcohol wipe on top and break it off with a movement away from you. If there is a ring painted on the ampoule, then open it in the same way, but it does not matter which side it is facing.
Opening an ampoule of Diclofenac with a notch
It is extremely rare to find ampoules without a dot and a ring; to open them you need a special file. It is usually included in the package, but if you don’t have it, a stationery knife or metal nail file will do. One of these devices needs to apply a notch using progressive, sawing movements. Then the ampoule is taken with this line towards you and the tip is broken off, as in cases of marking.
What happens if you administer it intravenously?
Diclofenac is also suitable for intravenous administration, but it must be dissolved in 100 ml of saline solution. The drip is placed for at least half an hour. The concentrated drug can cause inflammation of the venous wall.
Watch this video for instructions on how to use Diclofenac injection solution:
Side effects
Side effects from Diclofenac injections can be divided into groups presented in the table below.
Organ system or group of symptoms | Side effects |
Infectious pathologies | In rare situations, a post-injection abscess may develop if the rules for disinfecting the skin before an injection are not followed. |
Hematopoietic system | Leukopenia and agranulocytosis, thrombocytopenia, aplastic and hemolytic variants of anemia |
Immune system | Hypersensitivity, including anaphylactic shock, angioedema |
Nervous system | Headaches and dizziness, deterioration of sleep, memory, sensory impairment, convulsions, aseptic meningitis, strokes |
Mental disorders | Unreasonable attacks of anxiety, irritability, depression, nightmares, disorientation in space |
Visual analyzer | Diplopia, blurred vision |
Hearing analyzer | Tinnitus, hearing loss |
The cardiovascular system | Arrhythmias, symptoms of heart failure, myocardial infarction, pain, increased blood pressure, vasculitis |
Respiratory system | Bronchial asthma, pneumonitis |
Gastrointestinal tract | Abdominal pain, vomiting and nausea, indigestion, bloating, diarrhea, gastritis, peptic ulcer, gastrointestinal bleeding. Rare negative consequences from the gastrointestinal tract include glossitis and stomatitis, dysgeusia (taste disturbance), formation of intestinal diaphragm-like structures, colitis, pancreatitis, constipation |
Liver and bile ducts | Hepatitis, deterioration of the functional state of the liver, a jump in the activity of transaminase enzymes in the blood |
Dermatological pathologies | Rash, dermatitis, erythema, eczema, Lyell and Stevens-Johnson syndromes, purpura, alopecia, photosensitivity |
Excretory system | Nephrotic syndrome, nephritis, proteinuria and hematuria, insufficient renal function |
General symptoms | Soreness and the formation of a compaction at the injection site, less often swelling and necrotic changes at the injection site |
To reduce the risk of negative consequences, it is necessary to use the minimum dose of the drug that can be effective, and the duration of the course should be short. If the duration of the course of use of Diclofenac exceeds the recommended one and/or too high a dosage is used, the risk of negative consequences from the cardiovascular system, including stroke and myocardial infarction, increases significantly.
Any reactions of the body to the administration of the drug must be reported to the doctor immediately. If pathological signs appear, Diclofenac injections should be stopped immediately.
Contraindications
Absolute contraindications to the use of diclofenac solution for intramuscular administration:
- hypersensitivity to the active component and other non-steroidal anti-inflammatory substances;
- dysfunction of the hematopoietic system;
- peptic ulcer;
- intestinal pathologies of destructive-inflammatory origin in the acute stage;
- bronchial asthma;
- age up to 15 years;
- periods of bearing a child and breastfeeding.
During pregnancy, injections of the drug should not be prescribed at any time; if it is necessary to use the drug during breastfeeding, lactation is stopped until the course of therapeutic correction is completed.
Strict medical supervision if it is necessary to administer Diclofenac injections and subject to an analysis of the risk-benefit ratio for the patient is necessary in the following situations:
- systemic connective tissue diseases (lupus erythematosus, collagenosis);
- induced porphyria;
- history of inflammatory and ulcerative pathological conditions of the gastrointestinal tract;
- impaired liver function;
- impaired functionality of the organs of the excretory system;
- hypertonic disease;
- heart failure;
- diabetes;
- lipid metabolism disorders;
- early postoperative period;
- tendency to hypersensitivity reactions;
- chronic obstructive pathologies of the airways;
- chronic infectious and inflammatory diseases of the respiratory system;
- elderly age;
- alcohol abuse.
The drug should be used with caution if concomitant drug treatment is necessary with anticoagulant, antiplatelet drugs, glucocorticosteroids for internal use, antidepressants from the group of selective serotonin reuptake inhibitors.
Since the administration of Diclofenac can provoke dizziness and excessive fatigue, during the course of use of the drug you should refrain from driving vehicles and other complex equipment.
Indications for use of the drug Diclofenac
Rheumatism, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout, lumbago, neuralgia, myalgia, pain due to traumatic injuries of the musculoskeletal system and soft tissues, primary dysmenorrhea, as a symptomatic remedy for infectious and inflammatory diseases of the ENT organs. In ophthalmology: inhibition of miosis during cataract surgery; prevention of the inflammatory process in the postoperative period for cataracts and surgical interventions in the anterior parts of the eye; prevention of cystoid macular edema before and after operations for lens removal and implantation; non-infectious inflammatory processes involving the anterior parts of the eye (chronic non-infectious conjunctivitis, allergic conjunctivitis); post-traumatic inflammatory process with penetrating and non-penetrating wounds of the eyeball (as an addition to local antibacterial therapy); to reduce the severity of eye pain in photophobia.
Interaction between Diclofenac and other medications
Characteristics of the simultaneous use of the drug and some medications are given in the table.
Medicines | Result of interaction |
Digoxin, phenytoin, lithium-containing drugs | An increase in the concentration of the active components of these drugs in the blood |
Antihypertensive drugs, diuretics | Weakening the effectiveness of drugs |
Potassium-sparing diuretics. | Hyperkalemia |
NSAIDs | Increased risk of adverse reactions from the digestive system |
Cyclosporine | Increased nephrotoxicity of Diclofenac |
Antidiabetic drugs | Sharp fluctuations in blood glucose levels, both upward and downward |
Methotrexate | Increasing the concentration of this drug and enhancing its toxic properties |
Quinolone derivatives | Convulsive conditions |
The patient must notify the doctor about the medications he is already taking. This measure will minimize the risk of possible consequences of drug interactions.
Drug interactions Diclofenac
It should not be used simultaneously with other NSAIDs (including salicylates and pyrazolone drugs), since with such a combination there is a risk of mutual potentiation of toxic effects and a decrease in the effectiveness of one of the drugs. When used simultaneously with anticoagulants, the risk of developing hemorrhagic complications increases significantly. When combined with lithium salts, diclofenac may increase the concentration of lithium in the blood plasma. Co-administration of digoxin with diclofenac after 48–72 hours can lead to a significant increase in the concentration of the glycoside in the blood plasma; after stopping taking diclofenac, digoxin levels return to normal after 48 hours. Diclofenac causes sodium and fluid retention in the body, reducing the effectiveness of antihypertensive and diuretic drugs. When combined with diuretics, potassium levels should be monitored. It is not advisable to prescribe simultaneously with cyclosporines. GCS may potentiate the toxic effects of diclofenac. For patients taking methotrexate, diclofenac is prescribed 24 hours before or after taking methotrexate, since the plasma concentration and toxicity of the latter may increase.
Overdose symptoms
If the dosage regimen for the injectable form of Diclofenac is not observed and the permissible amount of the administered drug is exceeded, the following symptoms may appear:
- clouding of consciousness;
- headaches and dizziness;
- convulsive states of myoclonic type;
- vomiting, nausea, sharp abdominal pain;
- impairment of the functional state of the kidneys and liver.
In case of overdose, it is advisable to carry out symptomatic treatment, the goals of which are to reduce blood pressure, correct impaired renal function, negative reactions from the gastrointestinal tract, depressed breathing, and convulsions. There is no specific antidote substance. Hemodialysis and forced diuresis have low effectiveness and are not used.
Diclofenac analogues and comparative costs of drugs
The price of Diclofenac Akos (manufactured by Sintez OJSC) for injection is not at all high; you can buy it from 16 rubles per package, which contains 5 ampoules of the medicinal solution. The cost of drug analogues can be found in the table:
Analogue | Price in rubles per package with five ampoules |
Voltaren | 269 |
Diklak | 128 |
Diclonate P | 108 |
Naklofen | 128 |
If it is impossible to use Diclofenac in injection form for some reason, then the doctor should select analogue injections that are safer. Only the action should be similar, and not the composition of the solution for intramuscular injection.
What is stronger than Diclofenac in injections?
Drugs based on:
- ketorolac – Ketorol, Ketanov;
- ketoprofen - Ketonal, Flamax, Artrosilene;
- dexketoprofen - Dexalgin, Ketodexal.
Artrosilene Ketanov Ketonal Flamax Dexalgin Ketodexal
Replacing this medication with a more potent one is carried out only by a doctor. If you need to choose a drug that has a better anti-inflammatory effect, the doctor may prescribe Indomethacin or hormonal drugs.
At a doctor's appointment: frequently asked questions from patients
During a consultation with a specialist, the patient can ask questions about the use of the medication. Let's look at some of the most common questions and their answers.
Tablets or injections - which is better?
The specific form of Diclofenac is prescribed depending on the characteristics of the clinical case. It cannot be said that any of them is better. Injections of the drug are effective in the early stages of the development of pathologies, and tablets are prescribed to continue the course of therapy.
Is it possible to combine Diclofenac and Milgamma injections?
Milgamma is a good complex of B vitamins, and prescribing this drug at the same time as Diclofenac is quite acceptable and rational.
Which is better: Diclofenac or Voltaren injections?
Voltaren contains the same active ingredient as the classic Diclofenac, so these drugs are equivalent in action.
How to replace Diclofenac in injections?
If the risk of developing negative consequences from the gastrointestinal tract increases, it is rational to prescribe selective inhibitors of type 2 cyclooxygenase instead of Diclofenac, which affects both isoforms of this enzyme. Movalis is one of these medications, so in a number of situations the answer to the question of which is better, Movalis or Diclofenac, will be in favor of the first medication.
And the answers to questions about which injections are better than Diclofenac than replacing Diclofenac in injections can only be given by the attending physician.
Reviews from patients about the injection form of the drug Diclofenac indicate that use for pain allows you to get rid of discomfort and speed up recovery. However, injections for back and joint pain should be done only as prescribed by a specialist and in strict accordance with his recommendations.
Diclofenac solution for injection: does it need to be diluted?
According to the instructions, Diclofenac solution for injection is a completely finished drug that does not need to be diluted before injection into the muscle. For severe pain, the doctor may recommend adding 1 ml of 2% Lidocaine to 3 ml of the drug.
If intravenous injections are prescribed, then dilution is strictly necessary. For one ampoule of the drug, take 100-500 ml of saline solution or 5% glucose. Add 1 ml of 4.2% sodium bicarbonate to the dropper to neutralize the acidity of the solution.
How long does it take for Diclofenac to be removed from the body in injections?
After administering 75 mg of Diclofenac in injections, it is eliminated from the body in 4-6 hours from the blood, and it can remain in the joint cavity for up to 8-10 hours.
How long does it take for it to start working?
Diclofenac infection acts quickly, you can expect pain relief to begin within 8-10 minutes, and maximum pain relief occurs by 20 minutes. The injection allows you to relieve moderate and intense pain already in the first day, but for the anti-inflammatory effect of the drug to manifest itself, it takes at least 3 days.
Mechanism of action of Diclofenac
How long does it last?
One injection of the medication lasts for at least 6 hours, but for many patients, administering an ampoule for a day is enough.
Studies on the effectiveness of the injectable form
Diclofenac is considered the “gold standard” among all non-steroidal anti-inflammatory drugs in terms of effectiveness, since it has been the leader in this group of drugs for 30 years. During this time, a large number of clinical studies were carried out, on the basis of which important conclusions were drawn.
According to the general recommendations of the Manual of Internal Medicine, parenteral administration of Diclofenac is a temporary method of therapy that should be used either to obtain a quick effect or to reduce the negative effect on the digestive system.
The Russian Medicines Register and formulary system indicate that the course of administering the injection form of Diclofenac intramuscularly should not exceed two days . Exceeding the duration of use of the injectable form of the drug may lead to adverse effects.
According to numerous observations, a long course of Diclofenac injections leads to the appearance of post-injection abscesses, the development of necrotizing fasciitis, aseptic necrosis and other complications.
The drug in question cannot be prescribed for a long course, and it cannot be used without medical advice. If you need to inject the medication, you should read the instructions. If there are any relative restrictions on use, the course of treatment with Diclofenac should be carried out under strict medical supervision.
Use of the drug Diclofenac
Orally, adults and adolescents over 14 years of age are prescribed 50–75 mg 2–3 times a day or 25 mg 4 times a day for acute conditions; for chronic diseases and for maintenance therapy - 25 mg 2-3 times a day or in retard form (100 mg) 1 time a day. The duration of treatment is 5–6 weeks. The maximum daily dose is 300 mg. Also used rectally. 75 mg is administered intramuscularly (deep into the gluteal muscle) 1–2 times a day. It is not recommended to prescribe a long course of injections (more than 4–5 days). For the symptomatic treatment of primary dysmenorrhea, the dose of diclofenac can be 50–200 mg/day. The duration of treatment is determined by its effectiveness and usually does not exceed 2–3 days. The gel is applied in a thin layer to painful areas 2-3 times a day. The duration of treatment is 10–14 days. Eye drops 0.1%: before surgery - 1 drop into the conjunctival sac 5 times within 3 hours before surgery; in the postoperative period - immediately after surgery - 1 drop 3 times (at 15, 30 and 45 minutes after surgery), and then - 1 drop 3-5 times a day for the time required for treatment; to eliminate pain - 1 drop immediately after surgery, then - 1 drop 4-6 times a day, if necessary for up to 6 days; for inflammatory processes - 1 drop 4-5 times a day, depending on the severity of the condition. Long-term treatment should be carried out only after a thorough assessment of the indications and ophthalmological examination. As a rule, use no more than 1–2 weeks.