Drugs online research references
N Z Med J. 1998 Jul 10;111(1069):246-8.
Promethazine overdose: is it a "Goodnight" after all?
Bergman J, Wallman P.
Auckland Hospital.
AIMS: To evaluate and describe the perceived increase in number of promethazine overdoses presenting to Auckland Hospital Emergency Department since Goodnight became available in New Zealand. METHOD: Emergency Department records were reviewed for 19.5 months from 19 December 1994 (when Goodnight became available on the New Zealand market) until 31 July 1996. The Emergency Department database for the preceding years dating back to 1 January 1984 was reviewed. RESULTS: There were a total of 25 patients (18 female; 7 male) with 17 patients being between the ages of 15-25. The first cases presented in April 1995 and 15 cases (60%) presented during the 1996 period of the study. Fifteen patients (60%) ingested one or more full boxes of Goodnight. Twelve patients (48%) were admitted to intensive care, eight of whom were intubated. Fifteen patients were discharged from hospital in under 24 hours, but five (20%) stayed 2-3 days. Records dating back to 1 January 1984 revealed a total of 31 cases of promethazine overdose in just under 11 years, nine being accidental ingestion in children less than 5 years of age. CONCLUSIONS: This review highlights the high morbidity and cost of having promethazine available as an unrestricted, pharmacy--only medication. It suggests that marketing laws should be reviewed and the availability of promethazine be curtailed.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9695759&dopt=Abstract
Pharmacol Res. 1998 Jul;38(1):35-9.
Bioavailability of intranasal promethazine dosage forms in dogs.
Ramanathan R, Geary RS, Bourne DW, Putcha L.
KRUG Life Sciences Inc., Houston, TX, USA.
Intramuscular promethazine (PMZ) is used aboard the US Space Shuttle to ameliorate symptoms of space motion sickness. Bioavailability after an oral dose of PMZ during space flight is thought to be impaired because of gastrointestinal disturbances associated with weightlessness and space motion sickness. In an attempt to find an alternative dosage form for use in space, we evaluated two intranasal (i.n.) dosage forms of PMZ in dogs for absorption and bioavailability relative to that of an equivalent intramuscular dose. Promethazine (5 mg kg-1) was administered as two intranasal dosage forms and as an intramuscular (i.m.) dose to three dogs in a randomised cross-over design. Serial blood samples were taken and analysed for PMZ concentrations and the absorption and bioavailability of PMZ were calculated for the three dosage forms. PMZ absorption from the carboxymethyl cellulose microsphere i.n. dosage form was more rapid and complete than from the myverol cubic gel formulation or from an i.m. injection. Bioavailability of the microsphere formulation was also greater than that of the gel formulation (AUC 3009 vs 1727 ng h ml-1). The bioavailability of the two i.n. dosage forms (relative to that of the i.m. injection) were 94% (microsphere) and 54% (gel). The i.n. microsphere formulation of PMZ offers great promise as an effective non-invasive alternative for treating space motion sickness due to its rapid absorption and bioavailability equivalent to the i.m. dose.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9697152&dopt=Abstract
Anticancer Res. 1998 Jul-Aug;18(4C):3033-8.
Multidrug resistance reversal in mouse lymphoma cells by heterocyclic compounds.
Molnar J, Szabo D, Mandi Y, Mucsi I, Fischer J, Varga A, Konig S, Motohashi N.
Department of Microbiology, Albert Szent-Gyorgyi Medical University, Szeged, Hungary.
Due to the close homology between bacterial and tumor cell transporter proteins, some antiplasmid and anticancer compounds were tested for their ability to reserve the multidrug resistance (mdr) of lymphoma cells. Some known anticancer medicines such as platidiam, novantron, fluorouracil, bleomycin and methotrexate were ineffective/while vinca alkaloids exerted a strong reversal effect on the mdr of lymphoma cells. The structurally related reserpine and yohimbine do not affect the activity of efflux pump. Some selected antitumor phenothiazines and benzo[a]phenothiazines, including trifluoperazine inhibit the P-glycoprotein (pgp) function. This fact is independent from the antiproliferative- or differentiation inducing effects. Since the polylactosamine specific tomato lectin prevents the action of the chemosensitizers tested, it is supposed that the site of action of phenothiazines can be at the 1st loop in the transmembrane glycoprotein. The efflux pump activity of the pgp in brain capillary endothel which is responsible for blood brain barrier (BBB) was also inhibited by some phenothiazines. However, the tomato lectin sensitivity of pgp was different in mouse lymphoma and human brain capillary endothelial cells. The mdr-gene expression of the mouse lymphoma cells (which were transfected with the human mdr-1 gene) could be reduced by phenothiazines such as promethazine and trifluoperazine, when the cells were cultured in the presence of 0.5 microgram/mL phenothiazines. Further synergism was found between two resistance modifiers i.e. verapamil and trifluoperazine on the inhibition of mdr-glycoprotein.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9713505&dopt=Abstract
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