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Titolo:
PHARMACOKINETICS AND PHARMACODYNAMICS OF TUCARESOL, AN ANTISICKLING AGENT, IN HEALTHY-VOLUNTEERS
Autore:
ROLAN PE; MERCER AJ; WOOTTON R; POSNER J;
Indirizzi:
MEDEVAL MANCHESTER M15 6SH LANCS ENGLAND WELLCOME RES LABS,DEPT CLIN PHARMACOL BECKENHAM BR3 3BS KENT ENGLAND
Titolo Testata:
British journal of clinical pharmacology
fascicolo: 4, volume: 39, anno: 1995,
pagine: 375 - 380
SICI:
0306-5251(1995)39:4<375:PAPOTA>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
SICKLE-CELL DISEASE; OXYGEN-AFFINITY; HEMOGLOBIN; BW12C; ERYTHROCYTES; ANEMIA; BASES; DRUG;
Keywords:
TUCARESOL; ANTI-SICKLING AGENT; SICKLE CELL DISEASE; PHARMACOKINETICS; PHARMACODYNAMICS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
24
Recensione:
Indirizzi per estratti:
Citazione:
P.E. Rolan et al., "PHARMACOKINETICS AND PHARMACODYNAMICS OF TUCARESOL, AN ANTISICKLING AGENT, IN HEALTHY-VOLUNTEERS", British journal of clinical pharmacology, 39(4), 1995, pp. 375-380

Abstract

1 Tucaresol is an orally administered antisickling agent which increases the oxygen affinity of haemoglobin. 2 The pharmacokinetics, effects on moderate graded exercise and psychometric performance of tucaresol were examined in a double-blind, placebo-controlled, parallel groupsstudy in 12 healthy men. 3 Three doses of tucaresol were given at 48 h intervals intended to modify 15, 25 and 32.5% of a subject's haemoglobin to a high affinity form (%MOD). 4 Mean peak %MOD was 34%. Mean C-max values in plasma and erythrocytes were 81.4 and 1459 mu g ml(-1), respectively. 5 Heart rate, compared with baseline, increased in the tucaresol group with the greatest changes at the highest %MOD and workload. There were no differences between groups in psychometric test performance. 6 Three volunteers on active drug developed fever, rash and tender cervical lymphadenopathy with onset 7-10 days from the start ofdosing, suggesting an immune mechanism. 7 The acute increase in oxygen affinity with tucaresol is physiologically well-tolerated, but the utility of tucaresol in the management of sickle cell disease will depend on the identification of a dosing regimen with a lower incidence ofdrug allergy.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 30/11/20 alle ore 00:47:24