Dicloberl retard: composition and presentation
One hard prolonged-release capsule contains 100 mg of diclofenac sodium. The prolonged release settles everything else: the capsule is taken once a day, but it does not suit every situation.
The capsule is swallowed whole with plenty of liquid. It should not be taken on an empty stomach, and anyone with a sensitive stomach is advised to take it with meals.
How Dicloberl retard works
Diclofenac is a non-steroidal anti-inflammatory drug that inhibits the synthesis of prostaglandins, as shown in the standard experimental models of inflammation in animals. In humans diclofenac reduces inflammation-related pain, swelling and fever.
It has a second property as well, named separately in the leaflet: diclofenac inhibits platelet aggregation induced by ADP and collagen. Hence the warnings about bleeding and the caution when it is taken together with anticoagulants and antiplatelet drugs.
Indications
Symptomatic treatment of pain and inflammation in the conditions listed below. The word "symptomatic" matters here: the medicine relieves the manifestations but does not act on the cause of the disease.
- acute joint inflammation, including gout attacks, as maintenance treatment;
- long-running joint inflammation, first of all rheumatoid arthritis, in which many joints are inflamed at once;
- ankylosing spondylitis — Bechterew's disease — and other inflammatory rheumatic diseases of the spine;
- flares of degenerative disease of the joints and of the spine;
- inflammatory rheumatic diseases of the soft tissues, painful swelling and post-traumatic inflammation.
Because of the delayed release of the active substance the medicine is not suitable for conditions in which an immediate therapeutic effect is required. That is a plain limitation: for acute pain that has to be relieved now, another dosage form is needed.
Method of use and dosage
The dose is chosen according to how severe the manifestations of the disease are. Adults are given one capsule a day, which corresponds to 100 mg of diclofenac sodium. The doctor decides how long the medicine is used: rheumatic diseases may call for long-term treatment. The number of adverse reactions can be limited by using the lowest effective dose and for no longer than is needed to control the symptoms.
| Who it is prescribed to | What happens to the dose |
| Elderly people | no dose change is required, but because adverse reactions are possible such patients are monitored especially closely; for the frail and those of low body weight the lowest effective dose is recommended |
| Mild and moderate renal impairment | the dose need not be reduced |
| Mild and moderate hepatic impairment | the dose need not be reduced, but starting treatment calls for medical supervision: the condition may worsen |
| Children and adolescents under 18 | the medicine must not be used — the capsule holds too much active substance |
The need to continue symptomatic treatment and the response to it are reviewed periodically: cardiovascular risk grows with high doses and long use, hence the requirement to manage with the lowest effective daily dose for the shortest possible time.
Contraindications
The first group of contraindications is intolerance. The medicine must not be used in hypersensitivity to diclofenac or to any excipient, nor in people in whom taking acetylsalicylic acid or other drugs that inhibit prostaglandin synthesis has ever caused an asthma attack, bronchospasm, urticaria or acute inflammation of the nasal mucosa.
The remaining contraindications concern bleeding and severe disease of the internal organs.
- non-specific disorders of blood formation or disorders of blood clotting;
- active or recurrent ulceration or bleeding of the digestive tract — two or more separate confirmed episodes;
- perforation of the wall or bleeding that occurred at some time while taking drugs of this same group;
- active bleeding from the cerebral vessels and any other active bleeding;
- severe failure of the liver, the kidneys or the heart;
- congestive heart failure of NYHA classes II–IV, ischaemic heart disease, involvement of the peripheral and cerebral vessels;
- the third trimester of pregnancy and age under 18.
Special warnings and precautions
The main danger is to the digestive tract. Bleeding, gastric and duodenal ulcers and perforations have been described for every drug in this group; they occur at various times during treatment, sometimes without warning signs. The risk grows with the dose and is higher in those who have already had an ulcer, especially one complicated by bleeding or perforation, and in the elderly — in them such reactions run a more severe course and may lead to death. In such patients treatment is begun with the lowest effective doses, and if the person is also taking a low dose of acetylsalicylic acid or other drugs that raise the risk, medicines that protect the gastric mucosa are considered: misoprostol or proton pump inhibitors.
- concomitant use with other non-steroidal anti-inflammatory drugs, including selective cyclo-oxygenase-2 inhibitors, should be avoided;
- if bleeding of the digestive tract or an ulcer occurs the medicine is withdrawn; with an ulcer, bleeding or perforation in the past, and also in ulcerative colitis and Crohn's disease, it is given cautiously and under strict medical supervision, because a flare is possible;
- clinical and epidemiological data indicate that taking diclofenac, especially in high doses and for a long time, may slightly increase the risk of arterial thrombosis — heart attack or stroke; with significant risk factors such as hypertension, hyperlipidaemia, diabetes and smoking the medicine is used with great caution;
- patients with hypertension or congestive heart failure in the history, with fluid retention and oedema, are watched separately: fluid retention and oedema with this group of drugs have been described.
The skin and the liver call for separate attention. Very rarely, severe skin reactions have been described with this group of drugs, some of them fatal: exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis. The greatest risk falls on the start of treatment, in most cases on the first month, so at the first signs of a rash, of changes on the mucous membranes or of other manifestations of hypersensitivity the medicine is withdrawn. Diclofenac may raise the activity of liver enzymes, and in patients with impaired liver function the condition may worsen, so starting treatment in them requires supervision.
Interactions with other medicines
Diclofenac has many interactions and almost all of them come down to two consequences: an increased risk of bleeding from the digestive tract and a change in the concentration of other medicines in the blood. Taking it together with other drugs of the same group increases, through summation of effects, the risk of ulceration and bleeding, and is therefore not recommended.
- plasma concentration may rise for digoxin, phenytoin and lithium; the serum concentration of lithium has to be monitored;
- the effect of diuretics and of blood-pressure-lowering drugs — beta-blockers, angiotensin-converting enzyme inhibitors, angiotensin II antagonists — may weaken, so blood pressure is measured periodically;
- in patients with impaired renal function, dehydrated or elderly, combining an ACE inhibitor or an angiotensin II antagonist with a drug that inhibits cyclo-oxygenase may worsen renal function up to severe, usually reversible failure; they are reminded to drink enough and their kidneys are monitored regularly;
- with potassium-sparing diuretics hyperkalaemia is possible — the potassium concentration is monitored;
- glucocorticoids and selective serotonin reuptake inhibitors increase the risk of ulceration and bleeding;
- diclofenac may inhibit the renal clearance of methotrexate and raise its blood concentration, so caution is needed within 24 hours before and after methotrexate is given; the nephrotoxic effect of ciclosporin diclofenac can intensify, while probenecid delays the elimination of diclofenac itself; with oral antidiabetic drugs it combines without affecting their action.
Anticoagulants are a separate matter. Clinical studies do not show that diclofenac changes the action of these drugs, but an increased risk of haemorrhage with concomitant use has been reported, and such patients are monitored carefully.
Pregnancy and breastfeeding
Inhibition of prostaglandin synthesis can have an unfavourable effect on the course of pregnancy and on the development of the embryo or fetus. Pharmacoepidemiological data point to an increased risk of miscarriage and of cardiac malformations after such a substance is taken early in pregnancy, and the risk grows with the dose and the duration of treatment. In animals such substances caused death of the embryo before and after implantation and, during organogenesis, a rise in various malformations, including cardiovascular ones.
In the first and second trimesters diclofenac sodium is prescribed only when clearly necessary, and for women planning a pregnancy and in those two trimesters the lowest possible dose is used for the shortest possible time. In the third trimester the medicine is contraindicated: such substances may exert a toxic effect in the fetus on the heart, the vessels and the lungs, with premature closure of the ductus arteriosus and pulmonary hypertension, may impair renal function up to failure with oligohydramnios and, at the end of pregnancy, may prolong bleeding time even at low doses; inhibition of uterine contractions may delay or prolong labour. Like other drugs of this group, diclofenac passes into breast milk in small amounts, so it is not prescribed to breastfeeding women.
Adverse reactions
The commonest are disturbances of the stomach and bowel. Gastric or duodenal ulcer, perforation and bleeding of the digestive tract are possible, sometimes fatal, especially in the elderly.
- digestive: nausea, vomiting, diarrhoea, bloating, constipation, indigestion, abdominal pain, tarry stools, bloody vomit, ulcerative inflammation of the mouth, flares of colitis and Crohn's disease; less often gastritis;
- heart and vessels: very rarely palpitations, oedema, heart failure, heart attack; with this group of drugs oedema, a rise in blood pressure and heart failure have also been described;
- blood: very rarely suppression of blood formation — anaemia, a fall in white cells and platelets, the aplastic form, agranulocytosis — and haemolytic anaemia as well;
- nervous system: commonly disturbances of the central nervous system, for example headache and dizziness.
The first signs of disorders of blood formation may be fever, sore throat, erosions in the mouth, flu-like complaints, marked fatigue, nosebleeds and bleeding into the skin. That is exactly why, during long-term use of the medicine, blood counts are checked at regular intervals.
Overdose
There are no characteristic clinical signs of diclofenac overdose. Disturbances of the central nervous system are possible — headache, dizziness, a dazed feeling and loss of consciousness, in children also myoclonic convulsions — as well as abdominal pain, nausea and vomiting, bleeding of the digestive tract, impaired liver and kidney function, a sudden fall in blood pressure, respiratory depression and cyanosis.
There is no specific antidote. Treatment of acute poisoning comes down to supporting the function of the vital organs and relieving symptoms — a marked fall in blood pressure, renal failure, convulsions, gastrointestinal and respiratory disturbances. Forced diuresis, dialysis and haemoperfusion are most probably useless for eliminating diclofenac, because of its strong binding to plasma proteins and extensive metabolism. If a potentially toxic dose has been taken, activated charcoal and emptying the stomach — inducing vomiting or gastric lavage — may be considered.
How to get a Dicloberl retard prescription online
The medicine is available on prescription, and the conversation with the doctor turns on two questions: whether this form is suitable at all, and whether there are contraindications. The prolonged-release form is designed for long treatment of rheumatic disease, not for taking pain away quickly, so it is worth telling the doctor straight away what hurts and for how long.
For the online consultation prepare information about gastric or duodenal ulcer, bleeding and perforations in the past, about ulcerative colitis and Crohn's disease, about liver and kidney disease, heart failure, ischaemic heart disease, heart attack and stroke, about hypertension, diabetes, lipid disorders and smoking, and also about reactions to acetylsalicylic acid and other painkillers — asthma, urticaria, a runny nose. List separately the medicines you take: anticoagulants, antiplatelet drugs, corticosteroids, antidepressants of the serotonin reuptake inhibitor group, diuretics and blood-pressure drugs, lithium, methotrexate, ciclosporin. The doctor will assess these circumstances and, if there are no contraindications, will issue an electronic prescription.
