Drugs online research references
medfak.gu.se
OBJECTIVE : To evaluate the pharmacokinetics and safety of esomeprazole (Nexium), the S-isomer of omeprazole, after repeated oral dosing in patients with hepatic impairment. DESIGN : Single-centre, open-label one-way study. METHODS : Twelve patients (aged 40-60 years) with mild to severe hepatic impairment received once-daily oral esomeprazole 40 mg for 5 days. Serial blood samples were drawn up to 24 h post-dose on day 5 to determine plasma levels of esomeprazole and its metabolites. Pharmacokinetic parameters were compared with an historical control group of 36 gastro-oesophageal reflux disease (GORD) patients (aged 29-58 years) with normal hepatic function. RESULTS : Esomeprazole was absorbed rapidly (mean maximum plasma concentration (Cmax) 6.1 micromol/l, mean time to Cmax (tmax) 1.9 h) and eliminated rapidly (mean plasma elimination half-life (t1/2) 2.1 h). Elimination of its pharmacologically inactive sulphone and hydroxy metabolites was more gradual. Patients with mild hepatic impairment had area under the plasma concentration-time curve during the dosage interval (AUCtau) and t1/2 values largely within the range of the control group. In patients with moderate hepatic impairment, t1/2 values were similar and AUCtau was slightly higher than in controls, whereas both parameters were increased in patients with severe hepatic impairment. The mean ratios of esomeprazole AUCtau, Cmax and t1/2 values in patients with and without hepatic impairment were 1.8, 1.3 and 1.3, respectively. CONCLUSIONS : The steady-state pharmacokinetics of esomeprazole were not altered substantially by mild or moderate hepatic impairment; however, plasma levels of esomeprazole were elevated in severe cases. Thus, dose adjustment appears unwarranted in mild or moderate hepatic impairment, but may be required in some severely impaired patients. Esomeprazole was tolerated well across the spectrum of hepatic impairment.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11984146&dopt=Abstract
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Fortschr Med. 1994 Apr 10;112(10):134-6.
[Bouginage of peptic esophageal stenoses. Results of one year with long-term omeprazole medication]
[Article in German]
Jaspersen D, Korner T, Schorr W, Hammar CH, Blaurock M.
Medizinische Klinik II, Stadtisches Klinikum, Fulda.
METHOD: Within the framework of an open prospective study, 47 patients with chronic reflux esophagitis, unresponsive to H2-receptor blockers and complicated by stenosis, underwent endoscopic bougienage. Unsuccessful treatment with H2-receptor blockers was followed in all patients by antisecretion treatment with omeprazole at a dose of 40 mg/day. RESULTS: At the latest after 3 months, stenotic and inflammatory changes had cleared up in all patients and under continued omeprazole over the long-term, remission of at least one year was achieved. CONCLUSION: A combination of endoscopic bougienage and simultaneous treatment with the proton pump blocker, omeprazole, represents effective treatment of chronic reflux disease complicated by stenosis.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8194815&dopt=Abstract
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Dig Dis Sci. 1999 Jan;44(1):125-33.
Healing of severe esophagitis improves esophageal peristaltic dysfunction.
Deprez P, Fiasse R.
Department of Internal Medicine, Cliniques Universitaires Saint-Luc, Catholic University of Louvain, Brussels, Belgium.
Reflux esophagitis is frequently associated with peristaltic dysfunction, which increases with the severity of inflammatory lesions. In order to assess peristaltic dysfunction with more accuracy before and after healing, we used a 24-hr pH and pressure recording method. Nineteen patients (median age: 65, range: 33-77) with stage II and III (Savary-Miller classification) esophagitis and peristaltic dysfunction were treated with 40 mg omeprazole for three to six months until complete endoscopic healing was achieved. Before treatment, median contraction amplitude was significantly lower than median contraction amplitude of a control group of comparable age [31 (21-53) versus 42 (21-77) mm Hg, P < 0.01], as well as median percentage of peristaltic contractions [27 (16-63) versus 44 (11-56), P < 0.01]. At the end of treatment, a statistically significant improvement of esophageal motor functions was observed for both median contraction amplitude [38 (26-55), P = 0.001] and median percentage of peristaltic waves [45 (23-68), P = 0.0001]. The posttreatment values, although still low, were not significantly different from control values. In conclusion, complete healing of grade II and III esophagitis improves peristalsis. Inflammatory processes related to severe esophagitis may be involved in failed peristalsis and low contraction amplitude.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9952233&dopt=Abstract
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