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[Sublingual administration of apomorphine in the treatment of motor fluctuations in Parkinson disease].

Apomorphine, a mixed dopaminergic agonist was given sublingually to 12 patients with Parkinson's disease disabled by severe on-off fluctuations. The patient's mean age was 57 years and the duration of Parkinson's disease was 12 years. All patients were also given domperidone (60 mg/day). Apomorphine was administered as soon as the off periods appeared. On periods were observed in 11 patients, with a mean apomorphine dose of 40 mg for each administration (extremes values: 20-60 mg). One patient had no motor benefit after an apomorphine dose of 120 mg. The mean duration of daily off periods was reduced by 64 per cent in 11 patients, for a mean duration of 8 months (extremes values: 2-12 months). Four patients developed stomatitis or gingival edema and stopped treatment. This pilot study shows that sublingual apomorphine, during a mean period of 8 months, significantly decreases off periods in parkinsonian patients. Others studies are necessary to confirm these results.

Administration, Sublingual↗

Studies on the bioavailability of glyceryl trinitrate after sublingual administration of spray and tablet.

The plasma profiles of nitroglycerin (glyceryl trinitrate, GTN, CAS 55-63-0) were estimated after two sublingual puffs of 0.4 mg GTN from a fluorochlorohydrocarbon (FCH)-free oral spray and one sublingual tablet of 0.5 mg GTN (Nitromex). The study was carried out in an open, randomized, two-phase, cross-over design with 24 volunteers. Eighteen blood samples were taken within 30 minutes after administration, and the plasma concentrations of GTN were determined by a specific gas chromatographic method with electron capture detection. The pharmacokinetic parameters, Cmax, tmax, and AUC, were determined for each volunteer. After correction of the AUC and Cmax values of the oral spray by dividing by two, the ratios (spray/tablet) of the AUC and Cmax and the 90% confidence intervals were estimated. The plasma concentrations of GTN (mean) after the spray (dose: 0.8 mg GTN) reached a maximum of 3.96 ng/ml (range: 0.99-10.86) at 3.5 minutes (range: 2-5). The plasma concentrations of GTN (mean) after the tablet (dose: 0.5 mg GTN) reached a maximum of 1.97 ng/ml (range: 0.57-4.33) at 4.9 minutes (range: 3-7). The corrected ratios (spray/tablet) of AUC and Cmax were 1.02 and 0.97 with the 90% confidence intervals (0.80, 1.30), respectively (0.77, 1.24). The results indicate that the oral spray in a dose of 0.4 mg is equivalent to the sublingual tablet in a dose of 0.5 mg.

Administration, Sublingual↗

[Treatment of arterial hypertension after surgery of the abdominal aorta: comparison of captopril and nifedipine administrated sublingually].

Treatment of high blood pressure after abdominal aortic surgery requires, because of adynamic ileus, the use of intravenously or sublingually (SL) administered drugs. The hemodynamic responses to captopril 25 mg SL (n = 10) and to nifedipine 10 mg SL (n = 10) were studied for 2 hours in patients (mean age 66 years) with arterial hypertension (mean blood pressure, Pa > or = 115 mmHg) the day after abdominal aortic surgery. Patients with bilateral renal artery stenoses, identified with the preoperative angiogram, were excluded. Systemic arterial pressure and pulmonary vascular pressures were measured using a femoral catheter and a pulmonary artery catheter respectively. Cardiac output (Q) was determined by thermodilution. [table: see text] Captopril and nifedipine significantly decreased pulmonary artery pressure, pulmonary artery occlusion pressure and right atrial pressure. No deterioration of renal function was observed. In conclusion, captopril and nifedipine SL are effective and well tolerated for the treatment of high blood pressure after abdominal aortic surgery.

Administration, Sublingual↗

Sublingual administration of desmopressin. Effectiveness in an infant with holoprosencephaly and central diabetes insipidus.

A 3-month-old child with bilateral cleft lip and palate and holoprosencephaly was hospitalized after he developed diabetes insipidus presumably due to hypothalamic dysfunction. He was initially treated with subcutaneous vasopressin injection but was switched to therapy with desmopressin acetate (DDAVP) before discharge. Because of his abnormal nasopharyngeal anatomy, we decided to administer the desmopressin acetate sublingually, and this was effective. A single daily dose of 2 micrograms (0.4 microgram/kg) resulted in a prompt antidiuresis, and the effect gradually lessened over a 24-hour period. Serum electrolyte values were restored to normal and have remained normal after three months of treatment. After additional study, the sublingual route might be considered for the administration of small-polypeptide therapeutic agents when other routes are impractical.

Abnormalities, Multiple↗

Antihypertensive effect of fractionated sublingual administration of nifedipine in moderate essential hypertension.

The magnitude and duration of the antihypertensive effect of nifedipine were studied in 7 cases of moderate essential hypertension. In a double-blind crossover study, nifedipine 10 mg or a placebo were administered sublingually 4 times a day for 2 days, and the results were compared. Each dose of nifedipine reduced systolic and diastolic blood pressure by 14% both in the supine and upright positions. The antihypertensive action lasted for about 3 h and it was not cumulative. The reduction in blood pressure was associated with a temporary increase in heart rate. Administration of nifedipine 10 mg did not significantly raise plasma renin activity or plasma aldosterone. The drug was well tolerated and no side effects were detected.

Administration, Oral↗

[Effect of long-term sublingual administration of nitroglycerin on the indicators of hemodynamics and changes of total ST segment shift in 35 precordial leads in acute myocardial infarct].

Limitation of the final dimensions of a myocardial infarct is a new trend in the treatment of this disease. Nitroglycerin is considered to be one of the most active agents in this respect. The effect of 4-hour sublingual medication with nitroglycerin on changes in the values of precordial cartogram and central hemodynamics was studied. A significantly more rapid dynamics of the overall ST segment displacement under the effect of treatment and favourable shifts in the hemodynamic values were demonstrated. The dynamics of the latter under the effect of nitroglycerin medication varied in its trend and depended on the initial parameters.

Adult↗

Increase of plasma atrial natriuretic peptide levels after sublingual administration of nifedipine in essentially hypertensive patients.

To see whether the acute natriuretic effect of nifedipine is accompanied by changes in atrial natriuretic peptide levels, a group of eight hypertensive patients were studied. After at least a week of constant sodium intake, placebo or nifedipine (10 mg s.I.) were administered and blood pressure, heart rate, plasma renin activity, plasma aldosterone and atrial natriuretic peptide plasma levels, urinary sodium, urinary volume and creatinine clearance were monitored for 2 hours. While placebo did not induce changes in any of the above parameters, nifedipine administration was followed by a significant decrease in blood pressure and an increase in urinary sodium, urinary volume and creatinine clearance; these changes were accompanied by a significant rise in atrial natriuretic peptide levels from 19.4 +/- 2.8 pg/ml to a maximum of 23.9 +/- 2.5 pg/ml and 24.1 +/- 2.2 pg/ml (P less than 0.05) at 60 and 90 minutes, respectively. In conclusion, our data do not rule out the possibility that atrial natriuretic peptide participates in the nifedipine-induced increase in sodium and water excretion.

Adult↗

[Regional ventricular function before and after sublingual administration of nitroglycerin in patients with recent myocardial infarction in the subacute and chronic stage].

Seven patients with a recent myocardial infarction and mostly normal left ventricular end-diastolic pressure were investigated by radionuclide ventriculography after 3-4 days and three weeks before and after 1.6 mg nitroglycerin. Between day 3-4 and the third week global ejection fraction (EF) rose insignificantly (p greater than 0.05) from 31 +/- 4 to 37 +/- 6 percent. The regional EF in the non infarcted area remained nearly stable (74 +/- 5 to 85 +/- 13 relative percent, p greater than 0.05). However, the EF in the infarcted area rose from 22 +/- 9 to 38 +/- 11 relative percent (p less than 0.05 percent). On day 3-4 nitroglycerin induced a clear increase of the EF in the infarcted area from 22 +/- 9 to 35 +/- 11 relative percent (p less than 0.05). The global EF and the EF in the non infarcted area remained nearly constant (global EF from 31 +/- 4 to 34 +/- 5 percent, EF in the non infarcted area from 74 +/- 5 to 77 +/- 7 relative percent; p greater than 0.05). Three weeks after myocardial infarction 1.6 mg nitroglycerin did not produce a significant alteration of the ejection fraction (slight increase of the global EF from 37 +/- 6 to 40 +/- 6, the regional EF in the infarcted area from 38 +/- 11 to 48 +/- 11 relative percent and from 85 +/- 13 to 90 +/- 11 relative percent in the non infarcted area; p greater than 0.05).(ABSTRACT TRUNCATED AT 250 WORDS)

Cardiac Output↗