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Biomedical subjects

F Mailland

Publications and source records attributed to F Mailland.

34 records · Page 2Linked to original sources

The effects of amineptine on the mood and nocturnal sleep of depressed patients.

The effect of amineptine, a new tricyclic antidepressant, was studied on the sleep of 12 depressed patients. A single blind comparative trial vs placebo was carried out and changes in depression symptoms were recorded using Hamilton Rating Scale for Depression (HRSD). The sleep was evaluated according to the Rechtschaffen and Kales criteria to determine various parameters. Amineptine treatment induced statistically significant reduction of HRSD total score after 14 days of treatment. Polysomnographic analysis revealed significant differences between depressed patients and healthy volunteers.

Adult↗

Dihydroergocriptine in management of microprolactinomas.

The effects of dihydroergocriptine (DHECP), a dihydrogenated ergot alkaloid with dopaminergic agonistic and alpha-adrenergic antagonistic properties, were studied in 22 women with PRL-secreting microprolactinomas and compared with those recorded in 36 previously studied patients treated with bromocriptine (BRC). After acute administration of 5 mg DHECP, orally, serum PRL decreased by 61 +/- 18% (+/- SD); only 1 patient was unresponsive. The nadir was reached at 300 min. Long term treatment with increasing DHECP doses caused a progressive PRL fall from 125 +/- 142 (+/- SD) to 81 +/- 159 micrograms/L after 1 week of a 3 mg twice daily regimen, to 64 +/- 88 micrograms/L after 1 week of 5 mg twice daily, 46 +/- 57 micrograms/L after 1 week of 10 mg twice daily, and 28 +/- 34 to 33 +/- 45 micrograms/L throughout 9 months of treatment with 10 mg DHECP 3 times daily. Seventy-seven percent of patients had normal serum PRL levels during chronic treatment. All women, including those with supranormal serum PRL levels, resumed regular menses, and 16 had ovulatory cycles; 1 woman became pregnant. Galactorrhea disappeared in all. During treatment the PRL response to TRH, initially absent in all patients, became positive in 10. In 7 patients, after DHECP treatment for 9 months, high definition computed tomographic scan no longer showed the focal lesions initially seen. After drug withdrawal, serum PRL increased again in all except 1 patient. Two patients had regular menses for 6 months, and 3 still had no adenoma imaged by high definition computed tomography. In BRC-treated patients the serum PRL changes and clinical results were very similar to those in the DHECP-treated patients, except for the persistence of normal serum PRL levels in 4 patients after drug withdrawal. On the other hand, side-effects were negligible during DHECP treatment, but remarkable during BRC. Systolic and diastolic blood pressures decreased by only 5.4 and 3.0 mm Hg, respectively, after acute 5 mg DHECP administration, but decreased by 12.8 and 14 mm Hg after acute 2.5 mg BRC administration. Orthostatic hypotension and peripheral vasomotor phenomena occurred in the long term DHECP treated patients except one, but they occurred in 9 and 3 of those treated with BRC, respectively. Gastric discomfort or mild nausea occurred in 12 DHECP-treated patients, while mild or severe nausea or vomiting were observed in 18, 11, and 2 of those taking BRC, respectively.(ABSTRACT TRUNCATED AT 400 WORDS)

Adult↗

Acute and long-term haemodynamic effects of propranolol and indenolol in hypertension.

The haemodynamic effect of indenolol, a beta-adrenoceptor blocker with intrinsic sympathomimetic activity (ISA) in animals, has been evaluated in a double-blind cross-over randomized trial after acute (3 days) and long-term treatment (28 days), in 12 hypertensive patients in comparison with that of propranolol. Patients were evaluated at rest and during isometric exercise (hand grip). The overall acute effect of both beta-adrenoceptor blocking drugs was to decrease mean blood pressure, heart rate and cardiac output, while total peripheral resistance increased. In the long-term studies the haemodynamic effect of propranolol was still characterized by cardiodepression and unchanged peripheral resistance. Patients on the long-term treatment with indenolol showed normal cardiac output and reduced total peripheral resistance. The data are compatible with a relatively strong ISA of indenolol, which would be responsible for the haemodynamic pattern observed during chronic treatment.

Adult↗

Prolactin lowering effect of dihydroergokryptine in rat and in man.

The prolactin lowering activity of dihydroergokryptine was investigated both in rats and in humans. The drug was administered orally at the doses of 0.2, 1 and 5 mg/Kg to intact or reserpinized male rats. Nine male adult volunteers were given 300 mg cimetidine iv 90 min after receiving 2, 3 or 4.5 mg of dihydroergokryptine and 3, 4.5 and 6.75 mg of dihydroergocristine or placebo per os in a randomized, cross-over design. Eight young adult males were injected im with 10 mg sulpiride 120 min after randomly receiving dihydroergokryptine 2.5 and 5 mg or placebo in a cross-over manner. Finally, five healthy young women were given dihydroergokryptine 2.5 and 5 mg, bromocriptine 2.5 mg and placebo in a cross-over design. Dihydroergokryptine caused a strong, long-lasting, dose-dependent fall of plasma prolactin concentrations in both rats and humans. Moreover, it inhibited the reserpine-induced rise of plasma prolactin in rats, as well as the cimetidine-or sulpiride-induced hyperprolactinemia in humans. Dihydroergokryptine proved twice as potent as dihydroergocristine and about half as potent as bromocriptine. Effective doses of both dihydrogenated ergot alkaloids were much better tolerated than bromocriptine.

Adult↗

Indenolol kinetics versus pharmacodynamics in hypertension.

A kinetic model has been employed to compare the duration of the antihypertensive activity of indenolol to its plasma half-life both after single administration and at steady-state. After a 14 day run-in period with placebo, 60 or 120 mg indenolol were given to hypertensive patients I or II grade, according to W.H.O. guidelines, once a day for 14 days. Blood samples were drawn and blood pressure recorded at intervals after the first dose, during treatment and after the last dose of the compound. Both plasma concentration and mean arterial pressure difference curves were fitted by a first order input-output model, where plasma half-life was 4 h, while pharmacological half-life was 24 h for both dose-levels tested. Therefore, with once-a-day dose regimen an accumulation of the antihypertensive effect of indenolol was demonstrated, with 99% steady-state of blood pressure reached after 7 days, while the drug did not accumulate in the central compartment.

Adrenergic beta-Antagonists↗

Effect of indenolol treatment on beta-adrenergic receptors of polymorphonucleates in essential hypertension.

Indenolol is a new antihypertensive agent, whose beta 1-adrenoceptor antagonist properties combined with beta 2-adrenoceptor agonist properties have been shown by experimental studies in animals. Our previous work reported that in vivo beta-adrenoceptor blocking drugs markedly increase the beta-adrenoceptor (BAR) number, without increasing BAR affinity. The aim of this study was to evaluate BAR density and affinity before and after indenolol therapy in membranes of polymorphonucleates (PMN) of patients with essential hypertension. Polymorphonuclear binding parameters were studied in 12 hypertensives (WHO stages I and II) after 14 days of placebo and after 21 days of indenolol therapy (120 mg once daily orally). Indenolol did not increase BAR number but significantly decreased (P less than 0.01) BAR affinity. On the basis of these data it is concluded that indenolol does not induce the same changes in PMN's BAR as previously observed with oxprenolol, propranolol and labetalol. This phenomenon may account for the absence of rebound effect after withdrawal of indenolol in hypertensives.

Adrenergic beta-Antagonists↗

Effect of dihydroergokryptine administration on serum prolactin and growth hormone levels in normal, hyperprolactinaemic and acromegalic subjects: evidence of potent and long-lasting pituitary dopamine receptor stimulation.

The endocrine effects of a relatively potent dopaminergic agent, dihydroergokryptine, have been studied in normal subjects, and in hyperprolactinaemic and acromegalic patients. A single 6 mg oral dose of the drug caused a marked, long lasting fall in prolactin (PRL) plasma levels in healthy subjects, in hyperprolactinaemic patients and in normoprolactinaemic acromegalics. Growth hormone (GH) levels decreased in 1-DOPA - responder, acromegalic patients, but dihydroergokryptine did not affect GH levels in normal volunteers or in 1-DOPA non-responder, acromegalic patients. The PRL- and GH- lowering activity of 6 mg dihydroergokryptine was significantly greater than that of 6 mg dihydroergocristine, and was similar to that of an oral dose of 500 mg 1-DOPA.

Acromegaly↗

Amineptine in the management of the depressive syndromes.

The antidepressant activity of amineptine was evaluated in 34 patients in a double-blind study vs clomipramine. Clinical results, assessed using the Hamilton rating scale for depression, failed to show any significant difference in the activity of the two drugs. Amineptine was however much better tolerated than clomipramine. The antidepressant activity of amineptine was further investigated in an open multicenter study carried out in 351 depressed patients. The significant reductions in the scores of the Hamilton rating scale for depression and the final clinical evaluations (87% favorable results, 69% of which excellent or good) confirmed the therapeutic efficacy of amineptine. Tolerance was excellent also in elderly, at risk patients.

Adult↗

Measuring the inhibition of TRH-stimulated prolactin by dihydroergocristine (DEC) in man: an indirect assessment of bioavailability.

An indirect method to assess bioavailability of dihydroergocristine-methansulfonate (DEC) is described. The method uses the inhibitory effect of DEC on TRH stimulated prolactin production. By means of this method it was possible to investigate the relative bioavailability of DEC tablets versus Diertina liquid. The results show that the relative bioavailability is complete.

Adult↗

Indenolol in hypertension.

After a complete washout 14 hypertensive inpatients were given placebo for 3 days. Undistinguishable 30- or 60-mg indenolol tablets were then given twice daily for 14 days in a double-blind, randomized manner. Supine and standing arterial pressure and heart rate were measured at rest three times a day. Indenolol decreased systolic and diastolic arterial pressure as well as heart rate in subjects in supine and standing positions. Placebo had no effect. The effect of indenolol on systolic arterial pressure was dose and time related, but independent of the intensity of hypertension. No dose-effect relationship was found on diastolic arterial pressure. Decrease of heart rate was dose and time related, although bradycardia was never noted. Indenolol was well tolerated.

Adult↗

Indenolol pharmacokinetics and pharmacodynamics after single and repeated daily doses.

The relationship between indenolol (an investigational agent) plasma levels and the drug's effect on blood pressure and heart rate was investigated after single and repeated once daily administration at two dosage levels (60 mg and 120 mg) in two different groups of patients with first or second stage hypertension, according to the World Health Organization classification. The pharmacokinetic data were indicative of a first order absorption-elimination curve; time of maximum plasma levels was 1.5 to two hours, and elimination half-life was four hours. The drug did not accumulate in the central compartment after repeated administrations. A long-lasting decrease of both resting and isometric exercise systolic pressure values was recorded after acute indenolol administration. Diastolic pressure was affected only by repeated administrations. The lower dose (60 mg daily) of indenolol did not affect heart rate, whereas the higher dose (120 mg daily) decreased this parameter. A steady state of pressure values and heart rate was reached after 14 days of once daily treatment.

Adult↗

[Nutrition of the very low birth weight newborn infant (less than 1500 g). Experience with a formula for the premature infant].

After a short review on the topic of nutrition of very low-birth-weight infants, particularly the very small preterms, results are reported on a trial with an adapted milk for prematures. Subjects involved had a gestational age of 28-34 weeks and weighed less than 1500 g thus representing a sample of very low birth weight babies. By using levels of MCT in the milk, a protein quota of 3, 15 g/Kg/day with 40/60 casein whey-protein ratio, an electrolyte content slightly higher than in most adapted formulas (for fullterm babies) and low osmolarity, good results were obtained for body weight growth, length, head circumference and subcutaneous fat. Growth indices were similar to those typical of the terminal months of intrauterine development as well as a satisfactory overall portrayal of biochemical indices of the nutritional status of VLBW babies.

Body Height↗