[Prolonged use of moxisylyte chlorhydrate (Icavex) by intracavernous self-injections in the treatment of impotence. Evaluation of long-term tolerance]. / Utilisation prolongée de chlorhydrate de moxisylyte (Icavex) en auto-injections intra-caverneuses dans le traitement de l'impuissance. Evaluation de la tolérance à long terme.

Moxisylyte chlorhydrate is a selective alpha-blocker of the post-synaptic alpha 1-adrenoreceptors. It has been used since 1992 for self-injections to induce erection. Tolerance has been studied in open trials in 143 men using 20 mg per intracavernous injection. Among these subjects, 104 were followed for 11 months. Self-administration was performed 7,509 times, i.e. 49.1 injections per subject over a mean period of 307 days. No severe side effects were observed. A total of 1,041 undesirable effects were reported by 90 subjects (75.1%), including mechanical disorders (28.2%) such as pain and burning sensation at injection, hematomas and ecchymoses. Nodules developed in 0.08% of these cases but always regressed. In 71.8% of the cases, the undesirable events was imputable to moxisylyte: dry mouth (2.73%), somnolence (1.9%), sinus congestion (0.71%). No case of priapism was reported. Long-term evaluation showed a reduction in the main undesirable effects with time. This fall off in the mechanical events could be explained by the subjects become for familiar with the technique. Pharmacological effects remain to be analysed. Added to the good tolerance, this result suggests that self-injection can be proposed as a first intention treatment for impotency.

Stabilization of phospho-intermediates of rat liver plasma membrane alkaline phosphatase by uncompetitive inhibition. Relation with phosphate uptake into hepatocytes.

Rat liver plasma membrane alkaline phosphatase (ALP) phospho-intermediates, which have molecular masses of 151 and 135 kDa bands, were labelled at physiological pH with either (gamma-32P) ATP or 32Pi. This labeling was stabilized by a potent enzyme inhibitor, bromolevamisole (BL), and not by bromodexamisole (BD). BL augmented the rate and extent of autophosphorylation and slowed down the rate of autodephosphorylation of ALP. The phospho-intermediates labeling presented nearly the same kinetic behaviour with either (gamma-32P) ATP or 32Pi. In the presence of BL a marked decrease of the phosphorylation state of many proteins was observed in hepatocytes. BL also produced a decrease of the 32Pi uptake into hepatocytes and a decrease of the specific radioactivity of cellular ATP. BD had nearly the same effect as BL on protein phosphorylation and 32Pi uptake. These results argued against a direct involvement of ALP in Pi transport across hepatocyte plasma membrane.