Photoleukomelanodermatitis (Kobori) Induced by Afloqualone

We reported a case of photoleukomelanodermatitis (Kobori) type drug eruption due to afloqualone (Arofuto®). The patient was given afloqualone and imipramine hydrochloride (Chrytemin®) for cervical spondylosis from November of 1990. Edematous erythema with slight itching appeared on the sun-exposed areas in December of 1990. As drug eruption was suspected, drugs were ceased, and the cutaneous lesions almost disappeared but pigmentations and depigmentations developed in spots in sun-exposed areas in March of 1991. Photopatch and oral challenge tests were positive.     

Anticonvulsant Activities of 4–Bromobenzaldehyde Semicarbazone

Summary: Some of the properties of 4–bromobenzalde-hyde semicarbazone (compound IV), a prototype molecule of a new class of anticonvulsants, aryl semicarbazones, are described. Compound IV demonstrated activity in the maximal electroshock (MES) and subcutaneous pentylenetetrazol (scPTZ) tests in mice, with low neurotoxicity. When given orally to rats, it displayed high potency in the MES test and very low neurotoxicity, resulting in a high protective index (PI). Compound IV displayed no proconvulsant properties, and development of rapid tolerance was not noted. When administered intraperitoneally (i.p.) at doses of 100, 300, or 600 mg/kg to rats, compound IV had no effect on levels of γ-aminobu-tyric acid (GABA) or on GABA-T activity in whole brain. When tested in vitro, compound IV had no effect on rat brain GABA-T at a drug concentration of 100 μM. Although the activities of certain drug-metabolizing enzymes were increased after oral administration of compound IV to rats, these effects were less prominent than those of phenytoin (PHT) and carbamazepine (CBZ). The principal mode of action of compound IV does not appear to be an interaction with the GABA_A receptor complex, and other mechanisms, involving excitatory amino acid neurotransmission, will have to be considered in future investigations of the anticonvulsant activity of this compound.     

米非司酮作用于兔输卵管收缩活动与Ca^2＋关系的研究

通过“结合化学分离与原子吸收分光光度法”对Ca^2 含量测定和离体输卵管肌条收缩记录方法，研究米非司酮（Ru486)对增加假孕（4d)兔输卵管平滑肌收缩频率，而不改变其收缩张力和振幅时与Ca^2 之间的关系，结果提示：（1）Ru486对输卵管分泌液和组织内Ca^2 的含量分布无明显影响；（2）Ru486具有降低细胞外液高Ca^2 浓度促Ca^2 内流，而使收缩增强的效应，且能协同Ca^2 通道阻断剂（Verapamil)抑制细胞外Ca^2 内流，而致收缩减弱的效应。     

Model Features of a Cardiac lontophoretic Drug Delivery Implant

Pharmaceutical Research -     

Kathon® CG reactivity in 1396 consecutively patch tested patients in the Copenhagen area

In 1396 consecutively patch tested patients 18 (1.3%) reacted to Kathon CG. Relevance was established in 4 of the 18 patients. The frequency of positive reactions to Kathon CG in eczema patients seems to have been stable in Denmark during the period 1983 to 1988.     

Cyclic hormonal replacement therapy after the menopause: Transdermal versus oral treatment

Summary In an open, randomized, comparative, between-patient trial, 45 postmenopausal women were treated for 4 months with cyclical transdermal oestradiol 0.05 mg per day or oral conjugated equine oestrogens 0.625 mg per day, in both cases, plus, medroxyprogesterone acetate 10 mg per day on the last 8 days of each cycle. Similar relief from postmenopausal symptoms was obtained with both treatments. Post-treatment histological evaluation of the endometrium did not reveal neoplastic or hyperplastic change in any patient.Early follicular-phase plasma oestradiol levels were observed only after transdermal oestradiol. There was a significant reduction in serum total cholesterol and LDL cholesterol in both treatment groups, with no difference between treatments, whereas serum triglyceride levels were decreased only by transdermal oestradiol. Plasma calcium and phosphorus fell significantly and serum intact parathyroid hormone rose significantly, with no difference between the therapies. No significant changes were observed in clotting factors.Transdermal oestradiol appears to be an effective and safe hormonal replacement therapy, and this route of administration may be responsible for the more useful action of the drug on serum lipids and plasma oestradiol levels.     

Two deaths from intravenous nifedipine abuse

Summary An incident is reported in which 2 intravenous drug abusers died as the result of uncontrolled experimentation with intravenous injection of the common anti-hypertensive and anti-anginal drug Nifedipine (Adalatt.m. Bayer), probably in mistake for the commonly abused short-acting benzodiazepine drug Temazepam. Large quantities of Nifedipine were identified in the blood of both deceased men by gas chromatography. Apart from intense gastric mucosal congestion, pulmonary oedema and general visceral congestion, the autopsy findings were entirely nonspecific. The similarity in colour, shape and texture between capsules of Nifedipine and those of Temazepam is likely to have prompted the mistake.     

The pitfalls of the dexamethasone suppression test: A biological marker of endogenous depression?

In the past few years there have been numerous publications which have stressed the value of the dexamethasone suppression test (DST) as a diagnostic marker of endogenous depression. Our own studies in 333 psychiatric inpatients and 121 healthy subjects did not reveal a differential diagnostic use for the DST. This result is in good agreement with other results in the literature. Our data demonstrate that intervening variables such as severity of illness, weight loss, sleep disturbances, situational stress, drug and alcohol withdrawal, and the pharmacokinetics of dexamethasone have an important influence on DST results, regardless of the diagnostic classification.     

Water imbibition in the rat prostate during castration-induced regression

The present study was conducted to examine changes in water concentration in the ventral prostate of adult rats at different intervals following castration. The prostatic dry weight was obtained by drying the fresh prostate at 70 degrees C for at least 110 hr and the prostatic water content was calculated from its wet and dry weight. Under normal conditions, the prostatic water concentration ranges from 81.9 to 82.7% in uncastrated rats. The prostatic water concentration started to increase at 8 hr postcastration (83.1%) but this increase was not statistically significant. By 16 hr postcastration, the prostatic water concentration (83.8%) became significantly higher than that of the uncastrated animals. In rats of day 1 to day 10 postcastration, the prostate contained significantly more water (84.4%-84.7%) than those in uncastrated animals. By day 21 postcastration, the prostatic water concentration (81.5%) was not significantly different from that of uncastrated rats. Unlike the prostate, the skeletal muscle did not significantly change the water concentration following castration. The 51Cr-EDTA space in the prostate was not significantly different in rats before and after castration. These results indicate that water imbibition in the rat prostate is associated with an active period of prostatic regression and that the change in the 51Cr-EDTA space during prostatic regression is not the major cause of water imbibition in the tissue. Therefore, the present findings suggest that castration-induced water imbibition in the rat prostate is caused by an increase in the intracellular water space.     

Regulation of fluid intake in dogs following water deprivation

Whereas water loss in land living animals occurs continuously, water intake takes place discontinuously. At the normal operating set point of plasma osmolality, urine is more concentrated than plasma due to secretion of vasopressin. Thus animals operate around a state of mild dehydration. As water loss occurs, the severity of dehydration and thirst increase in intensity and at some point water intake occurs. Sufficient water is consumed to return plasma osmolality to the normal operating set point. Food intake and water balance are interdependent as food provides the osmoles which determine obligatory renal solute excretion. When dry food with the same osmotic content was substituted for canned food (water content 74%), dogs increased water intake from 24.2 +/- 4.3 to 62.2 +/- 8.8 ml/kg. Urine output and urine osmolality were unchanged, as under conditions of normal hydration, near maximal urine concentration is achieved. Changing water intake is the only available variable to maintain water balance. During water deprivation, the major renal mechanism appears to be natriuresis. In rehydration, satiety mechanisms ensure appropriate water intake and renal sodium conservation restores sodium balance.