Almitrine, a peripheral chemoreceptor stimulating drug, was given 100 mg orally to six patients with advanced chronic obstructive pulmonary disease (COPD), and its effects on hemodynamics, blood gases, lung mechanics, and the distribution of ventilation/perfusion ratios (VA/Q), determined by the inert gas elimination technique, were investigated. Arterial Po2 increased from 52 +/- 4 to 59 +/- 3 mm Hg, mean +/- SEM, p less than 0.01, arterial Pco2 decreased from 46 +/- 3 to 43 +/- 3 mm Hg, p less than 0.05, and venous admixture from 30 +/- 6 to 19 +/- 3 percent, p less than 0.02. No change occurred in ventilation, variables of lung mechanics, systemic and pulmonary hemodynamics, except an increase in pulmonary vascular resistance (from 364 +/- 103 to 438 +/- 99 dyne.s.cm-5, p less than 0.05). A reduction in VA/Q inequality could be demonstrated with a redistribution of blood flow into the lungs by a diversion of 15 percent of total blood flow from units with low VA/Q (between 0.08 and 0.4) to units with normal VA/Q (between 0.5 and 1.8). These changes might be explained by an enhancement of hypoxic pulmonary vasoconstriction. Pharmacologic peripheral chemoreceptor stimulation, at an infra-ventilatory analeptic dosage, might be of therapeutic interest to patients with respiratory insufficiency due to VA/Q inequality.