Cholestyramine influences the absorption of troglitazone

Troglitazone, 4-thiazolidinedione, is an insulin action enhancing agent under clinical development for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). Administration with, or up to 30 min after, food significantly improves absorption of troglitazone due probably to enhanced bile solubilisation and dissolution time.
Cholestyramine is an anion exchange resin with lipid-lowering properties. Taken orally, it is not [...]

Improvement in the gastrointestinal absorption of troglitazone

Troglitazone, 4-thiazolidinedione, an insulin action enhancing agent, is one of a new class of agents, the thiazolidinediones, currently in clinical development for the treatment of non insulin dependent diabetes (NIDDM). Animal models of NIDDM provide evidence that troglitazone suppresses hepatic gluconeogenesis and improves insulin sensitivity and responsiveness by potentiating insulin-induced peripheral glucose uptake. In vitro [...]

Rifampicin on activity of mephenytoin 4′-hydroxylase

The enzyme (CYP2C19) that 4′-hydroxylates S- mephenytoin (S-MP) is a genetically polymorphic cytochrome P450. Based on the activity of CYP2C19, individuals are phenotyped as extensive metabolizers (EM) and poor metabolizers (PM). S-MP is extensively metabolized in EMs; this results in a lower S/R ratio measured in EMs than that in PMs. The PM phenotype is [...]

Oral matrix metalloproteinase inhibitor marimastat

Marimastat (BB-2516) is an inhibitor of the family of enzymes known as matrix metalloproteinases (MMPs). These enzymes are considered to be primarily responsible for the degradation of extracellular matrix proteins in processes of tissue formation and remodelling. Under normal conditions the activity of MMPs is controlled at several levels, including their secretion as latent proenzymes [...]

Human follicle stimulating hormone in women

Follicle stimulating hormone (FSH) is one of the key hormones regulating reproductive function in both genders. FSH, a heterodimeric glycoprotein, is produced in the anterior pituitary gland and then secreted into the general circulation. In the female it stimulates growth and maturation of ovarian follicles; in males it promotes spermatogenesis. One indication for human FSH [...]

Suppression of tumour development

The notion that the prevention of disease is better than having to cure it is probably as old as the concept of restoration of human health by medical intervention. Many human cancers are preventable because their causes have been identified in the human environment. The finding that regular consumption of certain constituents of fruits and [...]

Endoscopic evaluation of the gastrotolerance of short-term antalgic treatment with low dose k-diclofenac

Nonsteroidal anti-inflammatory drugs (NSAIDS) are widely used at a low dosage as an analgesic treatment. They are very efficient analgesic and anti-inflammatory drugs but may cause gastrointestinal damage by two independent mechanisms: a systemic effect (mediated by cyclo-oxygenase 2 inhibition) and a local effect that is pH and pKa related.
Low dose ibuprofen is the reference [...]

Biotransformation in vitro of the 22R and 22S epimers of budesonide by human liver, bronchus, colonic mucosa and skin

Budesonide is a synthetic glucocorticosteroid used in the topical treatment of diseases such as rhinitis, asthma and psoriasis , which has also been introduced for the treatment of inflammatory bowel disease. This drug is characterized by a high local potency at the site of application with relatively low systemic activity after absorption. This high therapeutic [...]