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Titolo:
Dose-related effects of controlled release dihydrocodeine on oro-cecal transit and pupillary light reflex - A study in human volunteers
Autore:
Freye, E; Baranowski, J; Latasch, L;
Indirizzi:
Univ Dusseldorf, Clin Vasc Surg, D-4000 Dusseldorf, Germany Univ Dusseldorf Dusseldorf Germany D-4000 rg, D-4000 Dusseldorf, Germany Ctr Pain Therapy, Dusseldorf, Germany Ctr Pain Therapy Dusseldorf Germany r Pain Therapy, Dusseldorf, Germany Nordwest Hosp, Dept Anaesthesia, Frankfurt, Germany Nordwest Hosp Frankfurt Germany p, Dept Anaesthesia, Frankfurt, Germany
Titolo Testata:
ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH
fascicolo: 1, volume: 51, anno: 2001,
pagine: 60 - 66
SICI:
0004-4172(2001)51:1<60:DEOCRD>2.0.ZU;2-7
Fonte:
ISI
Lingua:
ENG
Soggetto:
OPIATE RECEPTOR-BINDING; GASTROINTESTINAL TRANSIT; CARBOHYDRATE MALABSORPTION; BREATH TEST; CONSTIPATION; ABSORPTION; MECHANISM; MORPHINE; TIME;
Keywords:
CAS 125-28-0; dihydrocodeine, controlled release formulation, by orocecal transit, pupillary light reflex, volunteers;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
55
Recensione:
Indirizzi per estratti:
Indirizzo: Freye, E Hamannstr 37, D-40882 Ratingen, Germany Hamannstr 37 Ratingen Germany D-40882 D-40882 Ratingen, Germany
Citazione:
E. Freye et al., "Dose-related effects of controlled release dihydrocodeine on oro-cecal transit and pupillary light reflex - A study in human volunteers", ARZNEI-FOR, 51(1), 2001, pp. 60-66

Abstract

It is well accepted that long-term administration of opioids results in a dose-related constipation. No data so far have demonstrated conclusively whether such constipation is also seen after intake of a controlled release formulation. It was therefore of interest to evaluate whether increasing doses of a controlled release formulation of dihydrocodeine (DHC, CAS 125-28-0) after oral administration also Induces a dose-related increase in constipation. Additionally, it was of interest to study whether such a peripheral opioid-related side effect is also seen in another, central receptor-mediated effect, the constriction of the pupil, at clinically relevant doses. Twelve volunteers were given controlled release DHC (60 and 120 mg, respectively) or placebo orally within a randomized, double-blind cross-over study. In order to determine the degree of constipation, oro-cecal transit time wasmeasured using the H-2-exhalation test. Additionally, In order to evaluatea centrally mediated effect, the response of the pupil to light was quantified using the pupillary light reflex technique. Both, peripherally and centrally mediated effects were compared to placebo. DHC at both dosages induced a significant (p < 0.01) prolongation of oro-cecal transit time when compared to placebo. However, prolongation of oro-cecal transit was not significantly longer when comparing the lower (60 mg) with the higher dose (120 mg). DHC also induced a significant (p < 0.005) depression of the pupillary light reflex from 53.9 mm (control) to 8.3 and 7.4 mm, respectively. Similar to intestinal transit, the pupillary light reflex was not significantly different among the two doses of DHC. Also, both dosages induced a similar amount of side effects. Tiredness anddry mouth were reported in 80 % after both doses while vertigo was reported In 5 % and 1 % complained of headache. None of the volunteers reported nausea or emesis. It is concluded that opioid receptor sites, which are located in the plexus myentericus of the intestinal wall, are responsible for the delay in propulsion. Because of the controlled release of a fixed amount of DHC over time there is constant binding of the ligand followed by a constant conformational change of peripheral and central receptor sites. Thus constant release Induces no dose-related increase in oro-cecal transit and inhibition of the pupillary light reflex.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 30/03/20 alle ore 00:06:57