Drugs online research references
Br J Clin Pharmacol. 1984 Nov;18(5):773-8.
Indobufen interacts with the sulphonylurea, glipizide, but not with the beta-adrenergic receptor antagonists, propranolol and atenolol.
Elvander-Stahl E, Melander A, Wahlin-Boll E.
This study assessed the possible interactions of the cyclooxygenase inhibitor indobufen with one sulphonylurea, glipizide, and with two beta-adrenoceptor antagonists, one of which is extensively metabolised already in the first passage through the liver (propranolol) while the other essentially escapes biotransformation (atenolol). Indobufen was first given as a single 200 mg dose and then for a 5 day period in a dosage of 200 mg twice daily, to six healthy volunteers. Glipizide (5 mg), propranolol (80 mg) and atenolol (100 mg) were given as single doses before and during indobufen medication. The drug concentrations were measured by selective and sensitive h.p.l.c. methods. The findings suggest that the lipophilic acid indobufen can inhibit the metabolic inactivation of another lipophilic acid, glipizide, but does not interfere with the disposal of the two basic drugs, propranolol and atenolol. The increased glipizide concentrations following indobufen were associated with an enhanced blood glucose reduction. Hence, this interaction may be clinically relevant.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6508985&dopt=Abstract
helix.nih.gov
Incubation of PC 12 cells with the sulfonylurea drug, glipizide (1-100 microM), increased intracellular levels of the acidic metabolites of dopamine, 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA). The levels of these acids in the medium were decreased, indicating the presence of a sulfonylurea-sensitive organic anion transporter. In the present study, we demonstrate that the sulfonylurea-sensitive transport of acidic dopamine metabolites is unidirectional, ATP dependent, unaffected by ouabain or by tetrodotoxin and blocked by drugs that interact with the multidrug-resistance protein-1 (MRP1). However, over-expression of MRP1 did not affect transport of the acid metabolites. The pharmacological profile and ion dependence of the transporter also differs from that of known ATP-binding cassette (ABC) family members. Using microdialysis, we also demonstrated a sulfonylurea-sensitive transport process in the striatum of freely moving rats. These results show that acidic dopamine metabolites are actively secreted from dopaminergic cells into surrounding extracellular fluid by a previously undescribed transporter.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10882041&dopt=Abstract
Ann Clin Res. 1983;15 Suppl 37:12-5.
Clinical pharmacokinetics of sulfonylureas: a brief review.
Melander A, Wahlin-Boll E.
All sulfonylureas seem to have similar mechanisms of action. Nevertheless, they may differ in their clinical effects because of differences in their pharmacokinetics and intrinsic activities. Second generation sulfonylureas, such as glibenclamide and glipizide, are much more potent than first generation sulfonylureas, such as tolbutamide and chlorpropamide. The former are, in fact, active at concentrations of the order of nmol/l, while the latter are active in the range of mumol/l. Accordingly, glibenclamide and glipizide are more efficient, and probably also less prone to cause pharmacokinetic interactions with other drugs, and with ethanol. In addition, glipizide and glibenclamide (new formulations) are completely bioavailable, which is a further advantage. Glipizide has a more rapid absorption and onset of action as well as a shorter half-life and duration of effect than glibenclamide. Accordingly, glibenclamide has a better effect on nocturnal and fasting blood glucose levels, but its use may also involve a greater risk of long-lasting hypoglycemia. At daily dosages of 5 mg or more, divided dosage seems unnecessary with glipizide, since effective concentrations will prevail throughout most of a 24 hour period. Efficacy may be improved if either drug is administered before, rather than together with, breakfast. High doses of glipizide may impair, rather than improve, glucose balance.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6679185&dopt=Abstract
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