Diclofenac – indications, dosage and side effects of suppositories

Proven content

Diclofenac is a drug that has anti-rheumatic, anti-inflammatory, analgesic and antipyretic properties. This preparation is available in the form of rectal suppositories. The active substance is diclofenac, a non-steroidal anti-inflammatory drug. In what cases is it worth using Diclofenac, and when should it be definitely avoided? How to properly dose this preparation? Can its use cause side effects in a patient? What should you know before taking this medication?

Diclofenac – general characteristics of the drug

Diclofenac is a rectal suppository drug that is available from prescription pharmacies. This preparation is used as an anti-rheumatic, anti-inflammatory, analgesic and antipyretic agent. It is a non-steroidal anti-inflammatory drug containing the active substance, sodium diclofenac. 1 suppository contains 50 mg or 100 mg of diclofenac sodium.

Diclofenac is in the form of white to cream suppositories with a characteristic torpedo shape. The package of the drug contains 10 suppositories (2 blisters of 5 pieces), which are packed together with the patient information leaflet in a cardboard box.

The manufacturer and entity responsible for the distribution of Diclofenac is GlaxoSmithKline (GSK) Consumer Healthcare Sp. z o. o., which is a global company in the healthcare sector focused on the progress of scientific knowledge. The company conducts research and develops a wide range of innovative products in three areas: pharmaceuticals, vaccines and healthcare products. GlaxoSmithKline began operations on January 1, 2001 following the merger of Glaxo Wellcome plc and SmithKline Beecham plc, which have a much longer history.

In Poland, thanks to many investments, the company has become one of the largest foreign investors in the Polish pharmaceutical industry cooperating with the medical community to support medical progress and improve the quality of healthcare for patients.

The company provides patients with over 300 drugs, vaccines and health care products. Medicines produced by GSK are used to treat respiratory diseases and HIV infection. In 2017 alone, the GSk concern supplied 3,6 million doses of vaccines. The company is the largest investor in the pharmaceutical industry in Poland. Among others, it was bought by Poznańskie Zakłady Farmaceutyczne Polfa SA.

What are the causes and symptoms of rheumatism? Read on: Rheumatism

Diclofenac – composition and action of the drug

The active ingredient of Diclofenac is diclofenac sodium. This compound is a non-steroidal anti-inflammatory drug from the group of phenylacetic acid derivatives. First of all, it has anti-inflammatory, analgesic, anti-rheumatic and antipyretic properties.

Diclofenac as a drug substance was introduced to the medical market in 1979 and is now considered to be the most prescribed non-steroidal anti-inflammatory drug in the world. For example, on the Polish pharmaceutical market, there are several dozen preparations that contain this substance in their composition.

The basis of the mechanism of action of diclofenac, as well as of other NSAIDs, is the inhibition of the activity of cyclooxygenase, an enzyme involved in the synthesis of prostaglandins from lipids in cell membranes. There are at least 2 isoforms of this enzyme COX-1 and COX-2.

COX-1 is an enzyme that is active under physiological conditions in many tissues, including platelets, kidneys, blood vessels and stomach.

COX-2, on the other hand, is an enzyme whose activity increases rapidly in inflammatory tissues. Diclofenac is active against both COX-1 and COX-2 isoforms.

The inhibition of COX-2 activity underlies the analgesic and anti-inflammatory effects of diclofenac. Diclofenac probably also inhibits the activity of lipoxygenase, the enzyme responsible for the formation of other pro-inflammatory factors. It is also noted that diclofenac is a drug with high analgesic and anti-inflammatory efficacy, it has a stronger effect than acetylsalicylic acid. In contrast, the anti-aggregating effect of diclofenac is weaker and shorter than that of acetylsalicylic acid.

After oral administration, diclofenac is rapidly and completely absorbed. The maximum concentration in the blood is usually obtained within 0,5–3 hours after drug administration.

The excipients of Diclofenac are colloidal anhydrous silica and medium-chain saturated fatty acid triglycerides.

If you want to know more about the substance diclofenac, read on: When to use diclofenac? Characteristics, action, indications and contraindications

Diclofenac – indications for use

Diclofenac is a preparation that is used in cases of inflammation. Your doctor may recommend this medication, especially for the treatment of:

1. inflammatory or degenerative forms of rheumatic disease (rheumatoid arthritis, ankylosing spondylitis), osteoarthritis (painful shoulder syndrome, tendinitis and bursitis), pain syndromes associated with lesions in the spine;
2. acute gout attacks;
3. other pain conditions caused by injuries (fracture, sprain, tearing, displacement, pain in the lumbar region), orthopedic, dental and other minor surgical procedures;
4. primary dysmenorrhea;
5. migraine attacks.

Diclofenac is also used as an adjunct to infections and inflammatory diseases of the ear, nose or throat with severe pain (pharyngitis, tonsillitis, ear inflammation).

It is worth remembering that the indication for the use of Diclofenac suppositories is the difficulty in administering the drug in the oral form.

What diagnostics should be performed if a patient is suspected of having rheumatic diseases? Check: Rheumatic profile, i.e. what tests will help detect rheumatic diseases

Diclofenac – contraindications to use

Diclofenac, despite its effectiveness in the treatment of inflammation, pain or rheumatic conditions, cannot be used by every patient struggling with this type of ailments.

Contraindications to the use of the drug Diclofenac are:

1. hypersensitivity to diclofenac or any of the other ingredients of the drug;
2. an active stomach ulcer or intestinal ulceration, gastrointestinal bleeding or perforation;
3. have ever had gastrointestinal bleeding or perforation related to the use of non-steroidal anti-inflammatory drugs;
4. active or recurrent gastric ulcer, bleeding;
5. heart disease and / or cerebrovascular disease, e.g. following a heart attack, stroke, mini-stroke, or embolism of the blood vessels of the heart or the brain, or a blood vessel restoration or bypass surgery;
6. existing circulatory disorders;
7. XNUMXrd trimester of pregnancy;
8. liver or kidney failure;
9. inflammation of the rectum or anus.

Diclofenac should also not be used if the patient has developed symptoms such as asthma, angioedema, urticaria or acute rhinitis after taking acetylsalicylic acid (aspirin) or other non-steroidal anti-inflammatory drugs.

What should you know about drug hypersensitivity? Check: Drugs are also allergenic

Diclofenac – precautions

Before and during the use of Diclofenac, follow the precautions contained in the package leaflet.

Precautions to keep in mind include:

1. in order to minimize the risk of side effects, it is recommended to use the drug in the lowest effective dose for the shortest period necessary to eliminate the symptoms;
2. the drug may mask the symptoms of an existing infection and make it difficult to diagnose the disease properly. During medical examinations, tell your doctor that you are using this medicine;
3. Diclofenac can cause allergic reactions, even if it has not been used before;
4. the drug should be discontinued immediately after the appearance of skin rash, mucosal lesions, or any other signs of hypersensitivity;
5. the drug should be taken under close medical supervision, if the patient has symptoms suggesting gastrointestinal disorders or there is a suspicion that the patient has gastric and duodenal ulcer disease, ulcerative colitis, Crohn’s disease (manifested, among others, with chronic diarrhea) or liver dysfunction.

It is also worth remembering that Diclofenac should be used with caution in the following situations:

1. the patient has hepatic porphyria;
2. you have heart or kidney problems, high blood pressure;
3. the patient is elderly; 
4. you are also receiving diuretics or medicines that affect your kidney function; 
5. you are going to have major surgery or are having surgery;
6. the patient is taking the drug for a long time;
7. the patient has asthma, allergic rhinitis, swelling of the nasal mucosa (e.g. due to nasal polyps), chronic obstructive pulmonary disease – manifested by shortness of breath, persistent cough without sputum production, wheezing, chronic respiratory infection or allergic to other substances that cause skin reactions, itching or hives
8. you suffer from systemic lupus erythematosus or mixed connective tissue disease.

It is also worth remembering that Diclofenac should not be used after the expiry date which is stated on the box. The expiry date refers to the last day of that month. The drug should not be disposed of via wastewater or household waste. It’s best to ask your pharmacist how to dispose of medicines you no longer use.

What should you know about proper drug storage? Check: Medications that are stored wrongly are poisonous

Diclofenac – dosage

Always use Diclofenac exactly as described in the package leaflet or as directed by your doctor or pharmacist. It is the doctor who determines the correct doses of the drug and determines how long the treatment will take. However, it should be remembered that treatment with this preparation should not exceed 7 days.

The drug must not be used orally, suppositories are applied rectally. When applying a single suppository, remember that suppositories must not be divided. The suppository should be removed from the blister and inserted into the anus. It is recommended to use suppositories after defecation.

Initial dose of Diclofenac for adults it ranges from 100 mg to 150 mg. For mild conditions and for chronic treatment, a daily dose of 100 mg is usually used. The total daily dose should not exceed 150 mg. Ideally, it should be divided into 2 to 3 doses.

For relief at night and morning stiffness, daytime tablet treatment may be supplemented by administering a suppository at bedtime (however, not exceeding the total maximum daily dose of 150 mg).

In the case of patients over 65 years of age, the drug should be used with particular caution. First of all, remember about the lowest effective dose of Diclofenac. Due to the risk of gastrointestinal bleeding, elderly patients should be under medical supervision for 4 weeks after starting treatment.

Diclofenac should not be used in children and adolescents under 18 years of age.

How to take medication correctly? Check: How to take medications effectively?

Diclofenac – side effects

Diclofenac, like any other drug, may cause side effects in patients. It is important to report any suspected adverse reactions after authorization of the medicinal product so that the benefit / risk balance of the medicinal product can be monitored.

The frequency classification of adverse body reactions (ADRs) is based on the following principles: very common (≥1 / 10), common (≥1 / 100 to <1/10), uncommon (≥1 / 1 to <000/1), rare (≥ 100 / 1 to <10 / 000), very rare (<1 / 1), not known (cannot be estimated from the available data).

Given frequency of side effects after taking Diclofenac you can point to:

1. common side effects (may affect up to 1 in 10 patients): headache, dizziness, nausea, vomiting, diarrhea, indigestion, abdominal pain, flatulence, lack of appetite, increased levels of transaminases (liver function test abnormalities shown in a laboratory test), rash;
2. uncommon side effects (may affect up to 1 in 100 patients): palpitations (uneven, fast heartbeat), heart failure, chest pain, myocardial infarction;
3. rare side effects (may affect up to 1 in 1000 patients): hypersensitivity, anaphylactic or anaphylactoid reaction, sleepiness, fatigue, asthma (wheezing, coughing, difficulty breathing), gastritis, gastrointestinal bleeding, vomiting blood, bloody diarrhea, tarry stools, peptic ulcer in the stomach and / or duodenum (with or without bleeding and perforation of the stomach or duodenal wall), proctitis, hepatitis, jaundice, liver dysfunction, hives (pale pink, itchy blisters on the skin), swelling, irritation of the anus;
4. very rare side effects (may affect up to 1 in 10 patients): severely reduced total blood cell counts causing flu-like symptoms, severe exhaustion, increased bleeding and bruising; confusion (disturbance of the orientation of time, place, situation or oneself), depression, insomnia, nightmares, irritability, psychotic disorders, paraesthesia (feeling of tingling or numbness in the hands or feet), memory impairment, seizures, anxiety, tremors, aseptic meningitis (neck stiffness, headache, nausea, vomiting, fever, disorientation disorder), taste disturbance, cerebrovascular accident, visual disturbances, blurred vision, double vision, tinnitus, hearing impairment, palpitations (uneven, rapid heartbeat), heart failure heart, chest pain, myocardial infarction, hypertension, hypotension, vasculitis, pneumonia, colitis (including haemorrhagic and worsening symptoms of ulcerative colitis, Crohn’s disease – manifested, among others, by chronic diarrhea), constipation, inflammation oral mucosa (including ulcerative stomatitis), glossitis, esophagus, membranous stenosis, pancreatitis, exacerbation of haemorrhoids, fulminant hepatitis, liver necrosis, liver failure, bullous rash, eczema, erythema (local reddening of the skin), erythema multiforme (reddish blue spots on the skin and / or membranes) mucous membranes, sometimes with blisters, fever and joint pain), Stevens-Johnson syndrome, toxic epidermal necrolysis (peeling of large areas of the epidermis and necrosis), exfoliative dermatitis, alopecia, photosensitivity reactions, purpura, Schönlein-Henoch disease – known as allergic purpura, it manifests itself among others bloody rash and joint pain and swelling, itching, renal dysfunction (acute renal failure, proteinuria (protein in the urine), haematuria, nephrotic syndrome, interstitial nephritis, papillary necrosis), angioedema, impotence;
5. unknown frequency of side effects: confusional state (disorientation), hallucinations, sensory disturbance, malaise, inflammation of the optic nerve, inflammation of the colon caused by insufficient blood supply.

Apart from drug poisoning, what else causes vomiting? Check: Vomiting – what is it caused and how to deal with it?

Diclofenac – pregnancy and breastfeeding

The use of any medications or dietary supplements during pregnancy requires consultation with the attending physician. If you are pregnant or breastfeeding, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before taking Diclofenac.

Diclofenac GSK may adversely affect the unborn child. Therefore, it is not recommended to use the drug in the first and second trimesters of pregnancy, unless the doctor considers it absolutely necessary. In this case, you should use the lowest dose for the shortest possible duration. Importantly, the third, i.e. the last trimester of pregnancy is a contraindication to the use of this preparation.

This preparation should also not be used during breastfeeding.

What is worth knowing about proper supplementation during pregnancy? Check: Conscious choices. Diet and supplementation in pregnancy

Diclofenac – interactions with other drugs

Before starting treatment with Diclofenac, please inform your doctor or pharmacist about all the medicines you are taking or have taken recently. You should also inform what medications the patient plans to take in the near future.

The active substance of Diclofenac may interact with other drugs or substances contained in medicinal products.

Drugs that may increase the risk of gastrointestinal bleeding with concomitant use of Diclofenac:

1. other non-steroidal anti-inflammatory drugs – e.g. acetylsalicylic acid, ibuprofen;
2. selective cyclooxygenase-2 (COX-2) inhibitors – drugs used in the treatment of rheumatic disease;
3. corticosteroids – anti-inflammatory drugs;
4. antiplatelet drugs – used to prevent blood clots;
5. anticoagulants – used to reduce blood clotting;
6. selective serotonin reuptake inhibitors – used to treat depression.

In addition, the use of Diclofenac can significantly increase the effect of:

1. lithium – a drug used to treat depression;
2. cardiac glycosides – medicines used to treat heart failure and heart problems;
3. methotrexate – a medicine used to treat certain types of cancer.

However, particular caution should be exercised if it is planned to use Diclofenac together with:

1. ciclosporin – a medicine used in organ transplant patients;
2. drugs that lower blood pressure – e.g. beta-adrenergic blockers, ACE inhibitors, diuretics. Diclofenac can reduce their effect, so blood pressure should be monitored regularly;
3. diuretics that increase urine production – Diclofenac reduces their effect;
4. oral antidiabetic drugs used to treat diabetes;
5. quinolones, which are antibiotics used to treat infections;
6. phenytoin, which is a medicine to treat epilepsy;
7. colestipol and cholestyramine, which are medicines that lower blood cholesterol. They can reduce the absorption of diclofenac. The drug should be used at least 1 hour before or 4 to 6 hours after taking colestipol or cholestyramine;
8. strong inhibitors of CYP2C9, such as sulfinpyrazone – used to treat gout, voriconazole – an antifungal medicine;
9. tacrolimus, which is a medicine used in patients after organ transplants and in dermatology;
10. mifepristone, i.e. a preparation used in gynecology;
11. medicines that can cause too much potassium in your blood.

Which drugs should never be combined with each other? Check: Dangerous interactions

Diclofenac — cena

Cena leku Diclofenac may differ depending on the city in which the preparation will be purchased or the pharmacy chosen by the patient. The price of the product also depends on the content of the active substance:

1. 10 rectal suppositories of 100 mg cost about PLN 10-12;
2. 10 rectal suppositories 50 mg cost about PLN 8-10.

How much money does the average Pole spend on treatment? Check: The Pole is not expected to see a doctor

Diclofenac – substitutes

Products that have the same international name and exist in the same form do not have to be substitutes, because the use of a given drug is determined by the content of the active substance, i.e. the dose of the drug.

It should be remembered that even when the dose of the active substance is similar, the patient may not always use the substitute, because he may be allergic to any of the other excipients of the drug.

Therefore, before using a substitute for Diclofenac, read the package leaflet or consult your doctor or pharmacist.

The preparations containing the same ingredients as Diclofenac and showing similar properties include:

1. Cataflam in the form of coated tablets
2. Diclac in the form of an injection solution, suppositories, enteric-coated tablets, modified release tablets or a gel;
3. Dicloabak in the form of a solution and eye drops;
4. Dicloberl in the form of suppositories, solution for injection, hard capsules with prolonged release;
5. DicloDuo – in the form of capsules with a modified release;
6. Diclofenac APTEO MED – in the form of a gel;
7. Diclofenacum Fastum – in the form of a gel;
8. Diclomax – in the form of coated tablets;
9. Dicloratio retard – in the form of extended-release capsules;
10. Dicloreum – in the form of a solution for injection, coated gastro-resistant tablets and prolonged-release tablets;
11. Diclotica – in the form of a gel;
12. Dicloziaja – in the form of a gel
13. Difadol 0,1% – in the form of a solution and eye drops;
14. Diclofenac Perrigo – in the form of a gel;
15. Diky 4% – in the form of a solution and spray for the skin;
16. Felogel Neo – in the form of a gel;
17. Glimbax – in the form of a solution for rinsing the mouth and throat;
18. Itami – in the form of a healing plaster;
19. Majamil – in the form of gastro-resistant tablets and an extended-release coated tablet;
20. Naclof – in the form of a solution and eye drops;
21. Naklofen – in the form of a solution for injection, capsules with modified release and gel;
22. Olfen – in the form of coated tablets, prolonged-release tablets, prolonged-release capsules, gel, medicated plaster, modified-release tablets;
23. Solacutan – in the form of a gel;
24. Veral – in the form of a gel;
25. Voltaren – in the form of a solution for injection or solution for infusion, gastro-resistant tablets, coated tablets, gel, soft capsules, prolonged-release tablets.

When is it worth asking the pharmacy about drug substitutes? Check: Swap when you can