Salofalk® 1 g: composition and pharmaceutical form
One suppository contains 1 g of mesalazine, and that is the whole daily dose at once. The medicine has a 500 mg version given three times a day; here the same daily dose is packed into a single suppository, so the regimen comes down to one procedure a day.
The form is a rectal suppository, and it was not chosen for convenience. The indication of the medicine is tied to the rectum, and the suppository delivers mesalazine exactly there, without making it travel through the whole digestive tract. The suppository is recommended to be inserted before sleep: the night is the longest stretch during which the medicine stays in place and does not shift anywhere.
How Salofalk® 1 g works
The main property of mesalazine with this route of administration is locality. On reaching the intestinal lumen it exerts a marked effect on the mucous membrane and the submucosal layer right where it was introduced, and that is what explains how narrow the indication is: what is treated is not «the bowel» in general but the stretch the suppository physically reaches.
The mechanism of the anti-inflammatory action has not been fully explained. Test-tube studies indicate that a certain role belongs to inhibition of lipoxygenase, the enzyme with which the synthesis of some inflammatory substances begins. An effect of mesalazine on prostaglandin concentrations in the intestinal mucosa has also been shown. Besides, 5-aminosalicylic acid, which is mesalazine itself, may work as a scavenger of free radicals — active oxygen compounds that damage cells in the focus of inflammation.
Indications
The leaflet gives one indication and it has two boundaries. The first is anatomical: treatment of ulcerative colitis limited to the rectum, that is, ulcerative proctitis. If the inflammation goes higher, the suppository will not reach it and another form of mesalazine is needed.
The second boundary is severity and phase: the medicine is intended for an acute course of mild to moderate degree. Not for maintenance treatment between flares and not for severe forms. The usual duration of treatment of an acute episode is eight weeks, but the final term is set by the doctor.
Method of use and dosage
Adults and elderly patients are given one suppository once a day rectally, which corresponds to 1 g of mesalazine per day. Age by itself does not change the dose: for older people it is the same as for other adults. Experience of use in children and adolescents is small and the documentation limited, so the decision at that age rests with the doctor.
The suppository is advised to be used before sleep. And there is a condition without which the regimen does not work: treatment is effective only with regular and systematic use. Missed evenings are no trifle in a course planned for eight weeks; a noticeable improvement after a week does not mean the task is done and the medicine can be set aside.
Contraindications
The first prohibition is known hypersensitivity to salicylic acid and its derivatives or to the other components of the medicine. Mesalazine itself belongs to the derivatives of salicylic acid, so a reaction to any substance of that series closes it off too.
The second prohibition concerns organs far from the rectum: the medicine is contraindicated in severe impairment of liver or kidney function. The reason is that even with rectal administration part of the mesalazine still reaches the blood, and it is precisely these organs that have to excrete and process it. In the warnings section the requirement is worded even more strictly: in renal impairment the medicine should not be used, and not only in severe impairment.
Special warnings and precautions
There is a set of symptoms upon which the medicine is stopped at once, without waiting for an appointment: cramping or acute abdominal pain, fever, severe headache and rash. That is what an acute intolerance reaction to the suppositories looks like, and a wait-and-see approach is out of place here. Two groups of patients need separate attention. The first are people with lung diseases, especially asthma: they are monitored very closely throughout the course. The second are those who have had adverse reactions to sulfasalazine products in the past; for them the start of treatment with suppositories proceeds under strict medical observation. If kidney function worsens during treatment, the nephrotoxic action of mesalazine itself must be considered as a possible cause, rather than looking for an explanation only in the underlying disease.
Monitoring of treatment is described in the leaflet not in general words but as a schedule of tests. Before the start and during the course, at the doctor's discretion, blood is checked — a peripheral blood smear, liver function parameters such as ALT or AST, plasma creatinine — and urine, with dipsticks. The first check is recommended 14 days after the start, then two or three times at four-week intervals. If the results are normal, later a check every three months is enough. Any new symptom cancels that schedule: the tests are done straight away. On the ability to drive and operate machinery the medicine has no effect.
Drug interactions
The most important combination involves the bone marrow. In patients who are simultaneously receiving azathioprine, 6-mercaptopurine or thioguanine, the possible enhancement of these drugs' suppressive effect on blood formation must be taken into account. The combination is not forbidden — in inflammatory bowel disease it occurs constantly — but it calls for attention to the blood count, which is part of the monitoring schedule anyway.
The second combination is described more cautiously: there is weak evidence that mesalazine may enhance the anticoagulant effect of warfarin. No specific interaction studies were carried out for this medicine, so the list is short not because there are no interactions but because they were not studied. It is worth telling the doctor about every medicine being taken.
Pregnancy and breastfeeding
One described case sets the tone of the whole section: renal failure was observed in a newborn after the mother had used high doses of mesalazine — 2 to 4 g orally — for a long time during pregnancy. This concerns intake by mouth and doses many times larger than a single suppository, but that case left caution regarding the child's kidneys behind it.
Otherwise, data on use in pregnant women are insufficient. Information from a limited number of women who used mesalazine during pregnancy does not indicate an undesirable effect on its course or on the health of the foetus or newborn; other significant epidemiological data do not yet exist. Studies in animals given mesalazine orally revealed neither direct nor indirect harmful effects on pregnancy, embryonic and foetal development, labour or postnatal development. The leaflet's conclusion: during pregnancy the suppositories are used only when the possible benefit outweighs the risk. The same reservation applies to breastfeeding. It is mainly N-acetyl-5-aminosalicylic acid and, to a lesser extent, mesalazine itself that pass into milk; experience in breastfeeding women is limited and hypersensitivity reactions in the child, diarrhoea in particular, cannot be ruled out. If the child develops diarrhoea, breastfeeding is stopped.
Adverse reactions
Practically all adverse reactions of mesalazine belong to the «rare» and «very rare» categories, but among them there are some that call not for monitoring but for stopping treatment immediately. These are allergic and fibrosing reactions in the lungs — breathlessness, cough, bronchospasm, inflammation of the pulmonary alveoli, pulmonary eosinophilia, pulmonary infiltrates, pneumonia; inflammation of the pericardium and of the heart muscle; acute pancreatitis; disorders of kidney function, including acute and chronic interstitial nephritis and renal failure. Hypersensitivity reactions belong here too: allergic rash, drug fever, lupus erythematosus and spread of the inflammation to the whole large bowel.
The second group is what shows up in tests, and what the monitoring schedule was drawn up for: very rare blood count disorders (aplastic anaemia, agranulocytosis, pancytopenia, neutropenia, leukopenia, thrombocytopenia) and changes in liver function parameters — a rise in aminotransferase activity and signs of cholestasis — as well as hepatitis and cholestatic hepatitis. The third group is what the patient notices and tolerates more easily: rarely headache and dizziness, rarely abdominal pain, diarrhoea, bloating, nausea and vomiting, very rarely peripheral neuropathy, muscle and joint pain, hair loss and a reversible fall in sperm count.
Overdose
Mesalazine has neither a specific antidote nor specific treatment — in case of overdose symptomatic and supportive measures are what remains. This is no reason for panic but a reason not to experiment with the dose on your own: increasing it «to speed things up» is not possible, and such a decision cannot be reversed.
There are few data on overdose, and they come mainly from cases of deliberate intake of high doses of mesalazine with suicidal intent. Those cases did not point to kidney or liver toxicity, but no conclusions about the safety of high doses are drawn from them either.
How to get a prescription for Salofalk® 1 g online
The indication for these suppositories is narrow — a flare of ulcerative colitis limited to the rectum, of mild or moderate degree — so the doctor needs an established diagnosis rather than a description of symptoms. In the questionnaire it is worth stating whether proctitis has been confirmed and by what, which form of mesalazine was used before and at what dose, whether there are kidney, liver or lung diseases and asthma, and whether you take azathioprine, 6-mercaptopurine, thioguanine or warfarin.
The course here runs for weeks and is accompanied by scheduled tests, so an online consultation does not replace monitoring but opens it. The formal side is short: the suppositories are prescription-only, you fill in the questionnaire at e-zdrowie.com yourself, the doctor issues an electronic prescription based on the answers, its code arrives by message, and with that code the medicine is dispensed at any Polish pharmacy.
