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In vitro dissolution profiles of three controlled-release mesalazine formulations were determined at pH 1.0, 6.0 and 7.5. A closed-column type dissolution apparatus was used. A reproducible gradual dissolution profile was seen for Pentasa at all pH values. Dissolution starts immediately and is complete after 20 h. Dissolution profiles at pH 1 and pH 7.5 are much alike and dissolution is faster than at pH 6. The behaviour of Asacol at different pH values corresponds with the expectations: no release at pH 6 and pH 1, fast release at pH 7.5. Dissolution starts after 1 h and is complete after 3 h. Mesalazine release from Salofalk tablets at pH 7.5 and pH 6.0 starts after 2 and 3 h, respectively, and is complete after 5 and 10 h. However, after a long lag-time (10 h) mesalazine is also released from Salofalksu tablets at pH 1 and dissolution is complete after 23 h. [ABSTRACT FROM AUTHOR]

A 73-year-old woman with endocarditis was treated with flucloxacillin and rifampicin. She already used the anticoagulant acenocoumarol because of a recent heart valve replacement. After starting rifampicin therapy the sensitivity for the acenocoumarol was reduced. The international normalised ratio (INR) did not exceed 2.0, while values of 2.5-3.5 were required. Increase of the daily dose of acenocoumarol with a factor 6 compared to the dose which resulted in a therapeutic INR before hospitalisation, proved insufficient to obtain a therapeutic INR during long-term rifampicin therapy. 21 days after rifampicin discontinuation the INR finally responded to high coumarin dosages. The breakdown of coumarins in the liver is increased by rifampicin due to induction of several isoenzymes of the cytochrome P450-system. This case illustrates that sensitivity to coumarins can be decreased profoundly even after discontinuation of rifampicin therapy. INR should be monitored closely not only at the start and discontinuation of rifampicin therapy, but also during the weeks after discontinuation of rifampicin treatment.

An important task of pharmacists is medication control by screening the medication of an individual patient. Many computerized drug interaction screening programs are available, but they all have their drawbacks. Screening without a computerized program is possible, but very time-consuming. In contrast to daily living at home, the patient in a hospital setting is carefully monitored and relevant biochemical parameters are regularly checked. Many potential drug interactions are countered immediately by changing (dosage of) medication. The aim of our study was to determine the number of drug-drug interactions and (pseudo)double medications on the internal, pulmonary and cardiological ward in order to discuss them with the physicians. During this discussion the clinical relevance of interactions was determined. We conclude that the number of clinically relevant interactions and (pseudo)double medication is limited, but that the role of the pharmacist is an important one, especially with regard to medication, that is not regularly used on a ward. Potential drug interactions should be predicted and dealt with by close teamwork of physician and pharmacist at the moment medication is prescribed.

1. There is a limited number of antiviral drugs available for therapy. Many investigations and new analytical techniques have unraveled the development and progression of a viral infection. Nowadays there is a good understanding of the multiplication cycle of viruses, including the human immunodeficiency virus. 2. In this article the currently available antiviral drugs are presented arranged by their mode of action that can be understood by the multiplication cycle of the virus. 3. Clinical use and side-effects are discussed as well as place in current therapy. Some attention is paid on promising investigational antivirals.

In order to investigate the retrograde spread in the colon and its relationship to the extent of the diseased area, the authors evaluated a 100ml enema of mesalazine (5-aminosalicylic acid, Pentasa') lg in a consecutive series of 30 patients with ulcerative colitis. The enema was labelled with 10 MBq 99mtechnetium-human serum albumin microcolloid. Sequential scintigraphic imaging was performed in all patients, and the results compared with the extension of the disease as found by colonoscopy. If the enema reached the entire affected area it was interpreted as 'topically adequate'. In 80% of the patients there was retrograde spread of the enema beyond the rectosigmoid, thus reaching the affected area in ulcerative colitis. No relationship was found between the extent of dispersion of the enema and the time of defecation prior to scintigraphy. The authors conclude that a 100ml 'Pentasa' enema may be adequate for treatment of ulcerative colitis extending up to the splenic flexure.

Twenty-three patients with attacks of distal ulcerative colitis were treated randomly with either 2 or 3 mg of topically administered beclomethasone dipropionate (BDP) or 30 mg of prednisolone sodium phosphate (PP). The effect of the steroid enemas on adrenocortical function was assessed by ACTH tests, which were performed before and after treatment. Endoscopic, clinical and histological scores were comparable in the three treatment groups in this pilot trial. Fasting cortisol in the PP group decreased significantly from 0.47 +/- 0.12 mumol/l before to 0.22 +/- 0.14 mumol/l (P less than 0.05) after therapy; in the BDP group no significant changes were found. Urinary cortisol excretion in the PP group was not detectable after therapy; in the BDP group no changes were found. It is concluded that in the topical treatment of ulcerative colitis, BDP may be preferable to PP because it exerts a promising anti-inflammatory action without affecting adrenocortical function.

Little is known about the factors that determine the extent of dispersion of enema solutions in the colon. To unravel some of the determinants we evaluated a consecutive series of patients with left-sided colitis. 40 ml enema solutions, viscosity 0.062 Pa.s (62 cP) at 37 degrees C were labelled with 10 MBq 99m-technetium human serum albumin microcolloid. Scintigraphic imaging was performed in 35 patients until 2 hours after administration of the enema. In 8 of the 16 patients with limited retrograde spread the study was repeated after doubling the volume (80 ml). We conclude that the extent of dispersion of an enema 0.062 Pa.s solution is highly variable. The basic fluid component for therapeutic 40 ml enemas (viscosity 0.062 Pa.s) reaches the affected area in patients with left sided colitis only in 40% of the cases. Increasing the volume of the enema can be an effective way to increase the retrograde spread up to the affected area in patients with limited retrograde spread. Scintigraphic imaging is a simple and reliable method of checking whether an enema conforms to the requirements of medical treatment. Scintigraphic imaging lasting for 1 hour after administration of the enema appears to suffice.