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Transport kinetics of plasma free fatty acid, very low density lipoprotein triglycerides and apoprotein in patients with endogenous hypertriglyceridaemia: effects of 2,2-dimethyl, 5(2, 5-xylyoxy) valeric acid therapy.

The effects of C1-719 on plasma lipid and lipoprotein concentrations have been examined in four patients with endogenous hypertriglyceridaemia maintained on an isocaloric diet for a period of 6 months. During therapy (400 mg/day) the mean plasma triglyceride and cholesterol concentrations were reduced by 35% and 15% respectively, while the administration of 800 mg/day reduced these by 49% and 31%. This hypolipidaemic effect was due to a reduction in the circulating level of very low density lipoproteins (VLDL) without a change in their composition. Before treatment the plasma VLDL triglyceride turnover, and FFA flux, were higher than that of normal subjects maintained on a similar diet. The plasma VLDL B-apoprotein turnover was similarly higher than in the controls. Administration of C1-719 decreased the plasma VLDL triglyceride turnover, FFA flux and VLDL B-approtein turnover. The drug reduced the insulin response following a glucose load with some decrease in glucose levels. The results suggest that the increase in plasma triglyceride concentration in patients with endogenous hypertriglyceridaemia is due to increased production of plasma VLDL triglyceride and its apoptein associated with an enhanced supply of FFA for hepatic triglyceride synthesis. C1-719 exerts a hypolipidaemic effect through a reduction of VLDL production, consequent upon inhibition of lipolysis as well as decreased synthesis of the apoprotein carrier. These effects could in part be explained by an improvement in peripheral tissue responsiveness to insulin and decreased exposure of the liver to high levels of insulin. However, a direct effect of the drug on adipose tissue and liver metabolism has to be considered.

Adult↗

Serum oestrone, oestradiol and oestriol concentrations in castrated women during intramuscular oestradiol valerate and oestradiolbenzoate-oestradiolphenylpropionate therapy.

Serum oestrone, oestradiol and oestriol concentrations were studied during intramuscular Primogyn Depot (10 mg of oestradiolvalerate) and Dimenformon prolongatum (2.5 mg of oestradiolbenzoate + 10 mg of oestradiolphenylpropionate) treatments. The serum oestrone concentrations were markedly elevated in both therapeutic groups 24 h after the injection. After the Primogyn Depot injection the serum oestrone concentration 10 days after the injection was still significantly higher than the pretreatment level. The serum oestradiol concentrations of both groups were markedly elevated 24 h after the injections and were significantly higher than the pretreatment concentration 10 days later. The oestriol values were low during both treatments.

Castration↗

A randomized controlled trial to compare calcipotriol with betamethasone valerate for the treatment of cutaneous lichen planus.

BACKGROUND: Topical calcipotriol is a vitamin D3 analogue which influences keratinocyte proliferation and differentiation. Its efficacy in cutaneous lichen planus has not been well evaluated. METHODS: This is a randomized open-label trial comparing the effectiveness of calcipotriol 50 microg/g versus betamethasone 0.1% ointments twice daily for 12 weeks in patients with cutaneous lichen planus, with respect to thickness, pigmentation, clearance and pruritus. Patient self-assessment was made at 0, 4, 8 and 12 weeks post randomization using visual analogue scales (VAS). Clinical assessment was made at week 12 and adverse events noted. Clinical response was defined as 75% or more for lesion flattening and absent or minimal pigmentation, and 50% or more for clearance. RESULTS: A total of 31 patients were randomized: 15 to calcipotriol and 16 to betamethasone. Clinically assessed lesion flattening occurred in approximately half the patients. With calcipotriol, there were two responses for pigmentation and one for clearance but none with betamethasone. Patient VAS indicated a gradual improvement in all measures but with little difference between the treatments. The largest difference indicated a 12-point disadvantage to calcipotriol for thickness but this was not statistically significant (p=0.09). Side effects reported were erythema (one patient) and increased pruritus (two patients), all with calcipotriol. CONCLUSION: Calcipotriol appears no more effective than betamethasone. The course of the disease appears to be affected in the same way by both treatments.

Administration, Cutaneous↗