In order to ascertain if pirenzepine (Pz), an antimuscarinic drug, could inhibit GH secretion in acromegaly, 8 patients were submitted to 3 successive treatment courses of 9 days each: Pz, bromocriptine (BRC) and Pz plus BRC. No change in basal levels of GH after Pz administration was seen, but its reduction (p < 0.05) by BRC was observed. Pz plus BRC did not improve this response. None of these drugs abolished the paradoxical GH response to TRH. In 7 normal controls, Pz suppressed the GH responsiveness to GHRH (p < 0.001), but not in acromegalic patients. BRC, instead, blunted this response. In conclusion, cholinergic control of GH secretion is altered in acromegaly. Pz, either when administered alone or associated with BRC, is not useful for the treatment of this disease.