Eight young adult male volunteers with a basic (alimentary) plasma boric acid concentration of less than 0.10 - 0.46 mg/l were given a single dose of boric acid (562-611 mg) by 20 min IV infusion. The plasma concentration curves, followed for 3 days, best fitted a three-compartment open model, although two subjects had to be left out due to inconstant basal plasma concentration values or failure to fit to the three-compartment model. The 120 h urinary excretion was 98.7 +/- 9.1% of dose, Cltot 54.6 +/- 8.0 ml/min/1.73 m2, t1/2 beta 21.0 +/- 4.9 h and distribution volumes V1, V2, and V3: 0.251 +/- 0.099, 0.456 +/- 0.067 and 0.340 +/- 0.128 l/kg.
The reporting rate of withdrawal reactions for paroxetine was found to be higher than that for sertraline and fluoxetine in each of the countries selected for detailed analyses (US, UK and Australia), as well as for all 16 countries combined. Moreover, using the WHO system of organ classification, the ratio of central nervous system to psychiatric withdrawal symptoms was 1.9 and 2.1 for paroxetine and sertraline, respectively, whereas that for fluoxetine was 0.48, indicating a possible qualitative difference between the SSRIs with respect to the nature of the withdrawal syndrome.
Using an in vitro technique it has been demonstrated that water-emulsifying and hydrophobic ointments containing boric acid liberate only minute amounts (1-6%) within 24 h compared with the nearly total liberation from a jelly. When an amount of boric acid containing ointment is swallowed, the absorption is only slightly delayed compared with a similar intake when dissolved in water, and in both cases nearly total excretion is found in the urine within 96 h. The halflife (t1l2/3) is 21 h (mean, 7 adult men). The pharmacokinetics rule out the risk of cumulative poisoning with topical preparations containing low amounts of boric acid. The use of water-emulsifying ointments containing up to 3% boric acid should be safe, even for repeated daily use in the napkin region.
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