Dicloberl 100: composition and presentation
The active substance is diclofenac sodium, and the dosage form here is a suppository — a rectal one. In the dosing section the leaflet describes two strengths, 50 mg and 100 mg, and for Dicloberl 100 the daily dose is reached with a single suppository.
The suppository is inserted deep into the rectum, and it is better to do so after a bowel movement. The leaflet states the point of this form plainly: diclofenac as suppositories makes it possible to use a different route of administration in patients who cannot be given the medicine by mouth.
How Dicloberl 100 works
The action depends on the substance, not on the form. Diclofenac belongs to the non-steroidal anti-inflammatory drugs and inhibits the formation of prostaglandins — this has been demonstrated in the standard experimental models of inflammation in animals. In humans the result is weaker inflammation-related pain, less swelling and a lower temperature.
Beyond that, diclofenac suppresses the clumping of platelets when it is caused by ADP or collagen. With the rectal route that property does not go away, so all the warnings about bleeding, including gastrointestinal bleeding, apply to suppositories just as much as to tablets.
Indications
Symptomatic treatment of pain and inflammation; the medicine is intended for adults, and that is stated in the indication itself. The conditions it is prescribed for fall into three groups. The first is the joints: acute inflammation, including gout, and long-running inflammation, above all rheumatoid, when many joints are affected at once.
The second group is the spine: ankylosing inflammation of its joints, known as Bechterew's disease, other inflammatory rheumatic conditions of the spine, and degenerative disease of both the spine and the joints. The third group is the soft tissues: inflammatory rheumatic diseases, painful swelling and inflammation after an injury. The set of conditions is the same as for the other forms of diclofenac, and that is no accident: the choice between suppository, capsule and injection is made not by diagnosis but by which route is more convenient — or simply possible — for the person right now.
Method of use and dosage
The dose is set according to the severity and type of the disease. The recommended daily dose for adults is 50 to 150 mg of diclofenac sodium, and the whole daily dose is split into one to three administrations. For the 100 mg strength that means one suppository a day; with the 50 mg strength a single dose is one suppository and the daily dose is one to three.
| Circumstance | What it changes |
| Duration of treatment | decided by the treating doctor; in rheumatic disorders long-term use may be needed |
| Limiting the frequency of adverse reactions | achieved with the lowest effective dose and for no longer than is needed to control the symptoms |
| Old age | the dose is not changed, but the patient is monitored especially closely because of possible adverse reactions |
| Mild and moderate renal impairment | the dose need not be reduced |
| Mild and moderate hepatic impairment | the dose need not be reduced |
| Age under 18 | the medicine is not used |
The technique is worth remembering separately: the suppository goes in deep and preferably after a bowel movement — otherwise the urge to defecate can undo the whole point of giving it. This looks like a trifle, but it is precisely what most often explains why a suppository "did not work".
Contraindications
The rectal form has a contraindication that tablets and capsules do not: inflammation of the rectum or of the anus. Proctitis rules the medicine out completely here, because the suppository is inserted exactly where the inflammation is.
The remaining prohibitions are common to diclofenac as a whole.
- hypersensitivity to diclofenac or to any excipient;
- bronchospasm, asthma, rhinitis or urticaria experienced after taking acetylsalicylic acid or another drug of the same group;
- disorders of blood formation of unknown origin;
- peptic ulcer of the stomach or duodenum — current or recurrent — and bleeding as well, if there were two or more confirmed episodes;
- gastrointestinal bleeding or perforations that occurred in connection with earlier treatment with drugs of this group;
- bleeding from the cerebral vessels or any other ongoing bleeding;
- severe liver or kidney failure, severe heart failure, the third trimester of pregnancy.
Special warnings and precautions
The medicine should not be combined with other non-steroidal anti-inflammatory drugs, including selective cyclo-oxygenase-2 inhibitors. There is one general safety rule here: the lowest working dose for the shortest time needed to ease the symptoms — that is what lowers the frequency of adverse reactions. In elderly people these reactions, above all gastrointestinal bleeding and perforations, are more common and may end in death.
- bleeding, peptic ulcer and perforations have been described with every drug of this group: they arise at various times during treatment, with warning symptoms and without them, and regardless of whether severe gastrointestinal reactions occurred before;
- their likelihood grows with the dose, and also in those who have already had an ulcer, especially one complicated by bleeding or perforation, and in the elderly; in such people treatment starts with the lowest effective doses;
- if the person is also receiving a low dose of acetylsalicylic acid or other drugs that raise gastrointestinal risk, medicines protecting the gastric mucosa are considered — misoprostol or proton pump inhibitors;
- patients with gastrointestinal reactions in their history, especially the elderly, are advised to report any unusual sensations in the abdomen, above all at the start of treatment and particularly any signs of bleeding.
From the point of view of the heart and the vessels diclofenac has the same reputation as the whole group: long use of high doses is linked to a small rise in the likelihood of arterial thrombosis, so with hypertension, lipid disorders, diabetes and smoking it is prescribed with particular caution, and the need to continue treatment is reviewed periodically. Very rare severe skin reactions are noted separately, among them Stevens-Johnson syndrome and toxic epidermal necrolysis: they fall more often in the first month of treatment, so a rash or changes on the mucous membranes are grounds for stopping the medicine at once.
Interactions with other medicines
Diclofenac's list of interactions is long, and it is easier to keep in mind not a roll of names but what exactly has to be done with each combination.
- measure blood pressure: diuretics and blood-pressure-lowering drugs, including beta-blockers, angiotensin-converting enzyme inhibitors and angiotensin II antagonists, may work more weakly under the effect of diclofenac;
- watch the kidneys and remind about drinking: in dehydrated or elderly people and in those who already have renal impairment, the combination with an ACE inhibitor or an angiotensin II antagonist can take matters as far as renal failure, usually reversible;
- monitor tests: the serum concentration of lithium without fail, the potassium concentration when potassium-sparing diuretics are used at the same time, because of the risk of hyperkalaemia; plasma concentrations of digoxin and phenytoin may rise too;
- keep an interval: within a day before methotrexate is given and a day after, diclofenac can slow its renal elimination and raise its concentration in the blood;
- expect intensification: diclofenac intensifies the nephrotoxicity of ciclosporin, while probenecid delays the elimination of diclofenac itself; glucocorticoids and antidepressants from among the selective serotonin reuptake inhibitors raise the risk of ulceration and bleeding;
- watch for a tendency to bleed: although studies have not shown that diclofenac affects the action of anticoagulants, cases of increased bleeding with their joint use have been reported.
The combination with other drugs of the same group stands apart: their effects add up, so the risk of ulceration and bleeding rises and such a combination is not recommended. With oral antidiabetic drugs diclofenac gets along, according to clinical studies, without mutual influence.
Pregnancy and breastfeeding
Suppression of prostaglandin synthesis can tell on the course of pregnancy and on the development of the embryo or fetus. Pharmacoepidemiological data speak of a raised likelihood of miscarriage and of heart defects when such substances are used early on, and that likelihood is the greater the higher the dose and the longer the treatment. In animals such substances led to death of the embryo before and after implantation, and use during the period when the organs are forming went along with more frequent malformations, including cardiovascular ones.
Hence the rule for the first two trimesters: prescribe only when clearly necessary, at the minimum dose and for as short a time as possible, and the same goes for women planning a pregnancy. The third trimester is a direct contraindication, and there are several reasons: a possible toxic effect on the fetal heart, vessels and lungs with premature closure of the ductus arteriosus and pulmonary hypertension; impairment of the fetal kidneys up to failure with a reduced volume of amniotic fluid; a longer bleeding time in mother and child even at low doses; and inhibition of uterine contractions, because of which labour may be delayed or drawn out. Diclofenac passes into breast milk in a small amount, and it is not prescribed to breastfeeding women.
Adverse reactions
Most reports concern the stomach and the bowel: peptic ulcer, perforation and bleeding of the digestive tract are possible, sometimes fatal and more often in older people.
- digestion: nausea and vomiting, diarrhoea, bloating, constipation, indigestion, abdominal pain, black stools, vomiting of blood, sores in the mouth, flares of inflammatory bowel disease and, less often, inflammation of the gastric lining;
- circulation: very rarely a rapid heartbeat, oedema, heart failure and infarction; for the group as a whole oedema and a rise in blood pressure have also been described;
- blood and nervous system: very rarely blood formation suffers — from anaemia and a shortage of white cells and platelets to the aplastic form, agranulocytosis and haemolytic anaemia; complaints relating to the central nervous system, for example headache or dizziness, are common.
It is worth knowing about disorders of blood formation in advance, because they begin non-specifically: fever, sore throat, sores in the mouth, a flu-like feeling, severe tiredness, nosebleeds and bruises on the skin. With long treatment blood counts are checked at regular intervals.
Overdose
An overdose of diclofenac gives no distinctive clinical picture. From the central nervous system headache, dizziness, a dazed state and loss of consciousness are possible, and in children myoclonic convulsions; besides that there may be abdominal pain, nausea, diarrhoea, ringing in the ears and vomiting, as well as bleeding of the digestive tract, impaired liver and kidney function, a sharp fall in blood pressure, respiratory depression and cyanosis.
There is no specific antidote, and treatment remains symptomatic. In acute poisoning by drugs of this group the function of the vital organs is supported and the complications are dealt with — a marked fall in blood pressure, renal failure, convulsions, gastrointestinal and respiratory disturbances. Forced diuresis, dialysis and haemoperfusion are most likely useless for eliminating diclofenac: the substance binds strongly to plasma proteins and is extensively processed in the body.
How to get a Dicloberl 100 prescription online
The medicine is available on prescription. What matters to the doctor is understanding why the rectal form has been chosen: the leaflet presents it as an alternative for those who cannot take the medicine by mouth, so it is worth explaining straight away whether there is nausea, vomiting, difficulty swallowing or some other reason to give up on tablets.
The second set of questions is about safety. Prepare in advance information about gastric and duodenal ulcer, bleeding and perforations in the past, about inflammatory bowel disease, about haemorrhoids and inflammation of the rectum — for suppositories this matters — about liver, kidney and heart disease, about a previous heart attack and stroke, hypertension, diabetes, smoking, and also about reactions to acetylsalicylic acid and other painkillers. List the medicines you take: anticoagulants and antiplatelet drugs, corticosteroids, antidepressants, 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.
