Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0016382 (flushing)
 6,387 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Twenty three patients with essential hypertension who were uncontrolled on diuretic and/or beta-receptor antagonist therapy were treated additionally with the vasodilator, pinacidil, in an open study. Significant reduction in mean blood pressure was achieved. Supine and erect systolic and diastolic blood pressure fell by 44/25 mmHg and 37/24 mmHg respectively over the study period of 12 weeks. Side-effects such as dizziness, headache, facial flushing and mild oedema were experienced by 10 patients during the study, all of which were mild and transient and did not require withdrawal from pinacidil therapy. Pinacidil is an effective and well tolerated agent in the treatment of essential hypertension.
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PMID:Pinacidil, a new vasodilator, in the treatment of mild to moderate essential hypertension. 400 40

Preliminary investigation in 3 healthy volunteers suggested that intravenous pinacidil in a dose of 0.2 mg/kg had a potent but well-tolerated hypotensive action in the supine position. Facial flushing, uncomfortable chest sensation and distressing postural hypotension occurred at serum concentrations above 300 ng/ml. Pinacidil, 0.2 mg/kg, was given intravenously over 4 min to 15 healthy volunteers in the supine position. Maximum fall in mean arterial pressure (MAP) was 15.7 +/- 6.0 mmHg. Maximum rise in heart rate was 23.8 +/- 6.6 beats/min. Pinacidil serum distribution half-life (T1/2 alpha) was 13.4 +/- 8.5 min and elimination half-life (T1/2 beta) was 2.13 +/- 0.49 h. The apparent volume of distribution (Vd beta) was 90.3 +/- 13.21 and total body clearance was 31.1 +/- 9.61/h. Pinacidil was approximately 40% bound to plasma protein over the concentration range 40-400 ng/ml. Urinary excretion of unchanged pinacidil accounted for 5.7 +/- 1.3% of the administered dose over 24 hours and urinary excretion of the major metabolite, pinacidil pyridine-N-oxide, was 31.6 +/- 9.2% of the administered dose. It was concluded that intravenous pinacidil is a potent vasodilator hypotensive compound, with a duration of action between 1.5 and 2 h.
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PMID:Pharmacokinetics and hypotensive effect in healthy volunteers of pinacidil, a new potent vasodilator. 646 76