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At least 19 recordsLinked to original sources
PubMed1990

Assessment of left ventricular function after sublingual administration of nifedipine in patients with moderate to severe hypertension.

To evaluate the left ventricular functional changes induced by acute decreases in blood pressure in 15 patients with systemic hypertension and left ventricular hypertrophy, this study used Doppler and M-mode echocardiographic derived left ventricular indices. After 30 minutes of administration of sublingual nifedipine, both systolic and diastolic blood pressure decreased and heart rates increased. The left ventricular end-systolic dimension decreased but not the end-diastolic dimension, which suggests that sublingual nifedipine may decrease only afterload, not preload. Total peripheral resistance decreased from 2770 to 1960 dyne.sec.cm-5. The M-mode-derived peak rate of dimension changes improved both the systolic and diastolic phase, and Doppler-derived indices of atrial contribution to ventricular filling decreased. Because both the systolic and diastolic phase indices of LV function are sensitive to variations in both preload and afterload, the improvement of myocardial contractility per se cannot necessarily be attributed to the direct effect of the drug to myocardium. Though favorable effects on the myocardial oxygen supply-demand ratio or increased adrenergic tone stimulated by the decline in systemic arterial pressures may contribute to the augmentation of LV systolic and diastolic function observed after nifedipine in the present study, the apparent augmentation of LV function appears to be attributable primarily to afterload reduction.

Administration, Sublingual↗
PubMed1989

Arterial-venous plasma concentration differences of 6-chloro-2-pyridylmethyl nitrate in humans after sublingual administration.

The plasma concentrations of 6-chloro-2-pyridylmethyl nitrate after sublingual administration were determined in six healthy male volunteers (venous plasma) and eleven patients (arterial plasma) with ischemic heart failure. The pharmacokinetics of the compound was investigated in volunteers. Plasma concentration-time data in each volunteer were found to fit a two-compartment open model with zero-order absorption. The pharmacokinetic parameters estimated from curve-fitting the plasma concentration-time data were as follow: Tmax 10 +/- 2.8 min, Cmax 8.16 +/- 2.48 ng/mL and CLP 6.16 +/- 1.79 L/min (means +/- S.D.). The arterial plasma concentrations (11.9 +/- 5.14 ng/mL) 7 min after sublingual administration were significantly higher (p less than 0.05) than those in venous samples (6.86 +/- 2.80 ng/mL). These results support that the arterial-venous gradient exists after administration of 6-chloro-2-pyridylmethyl nitrate in humans.

Administration, Sublingual↗
PubMed1991

[Comparison of the effects of diazepam, nifedipine, propranolol and a combination of nifedipine and propranolol, by sublingual administration, in patients with hypertensive crisis].

PURPOSE: To evaluate the effects of sublingual administration of diazepam, nifedipine, propranolol and the association of nifedipine with propranolol patients with hypertensive crisis. METHODS: Eighty patients with hypertensive crisis, DAP greater than 120 mmHg, and mean age of 54 +/- 7.4 years, 33 women and 47 men, were evaluated. The AP was measured with an aneroid sphygmomanometer, in mmHg, in orthostatic position, before and after 10, 20, 30 and 60 minutes of treatment. The heart rate in one minute was also measured at the same intervals. The patients were divided randomly into four groups and treated, respectively, with 10 mg of diazepam, 10 mg of nifedipine, 40 mg of propranolol and 10 mg of nifedipine associated with 40 mg of propranolol. RESULTS: A significant and gradual reduction of SAP and DAP were observed in all groups of patients. The percentage of reduction, after 60 minutes, for SAP was, respectively, 10.1%, 12.9%, 15.4% and 16%, and for DAP 7.7%, 11.3%, 13.6% and 13% in groups I to IV. The heart rate did not change in groups I and II, but significative reduction was observed in groups III (p = 0.002) and IV (p = 0.009). CONCLUSION: The drugs used were effective for the treatment of hypertensive crisis, and the sublingual administration is an important and easy way for their administration.

Administration, Sublingual↗
PubMed1989

Effects of sublingual administration of nifedipine on arterial pressure, plasma renin activity, and glomerular filtration rate in essential hypertension.

Effects of sublingual administration of nifedipine on systemic arterial pressure (BP), plasma renin activity (PRA), aldosterone level (AL), and serum sodium (Na) and potassium (K) levels, have been determined. A significant decrease was observed in systolic and diastolic blood pressure five minutes after the sublingual administration of nifedipine in 21 patients with mild or moderate essential hypertension. Furthermore, in an observation period of six hours, it was also established that the effect of nifedipine on systolic and diastolic blood pressure continued. An increase was observed in glomerular filtration rate, whereas there were no changes in PRA, AL, or serum Na and K levels.

Administration, Sublingual↗
PubMed1989

[Biological availability of glycerol trinitrate after sublingual administration].

The relative bioavailability of a glyceryl trinitrate (GTN) spray (Nitro-Corangin Spray) compared to that of another GTN Spray was evaluated in 12 healthy male volunteers using an open, randomized cross-over design with two treatment phases. The parameters Cmax, tmax and AUC0-1 showed no statistically significant differences between the two treatments. It is concluded that the two GTN-Sprays may be considered bioequivalent.

Administration, Sublingual↗
PubMed1991

Effect of the acute sublingual administration of ketanserin in hypertensive patients.

The purpose of this study has been to compare the acute antihypertensive effect of a dose of 20 mg of ketanserin in 18 patients after sublingual administration and in 19 after oral administration. In three patients ketanserin and ketanserin-ol plasma levels were measured after both sublingual and oral administration. The results showed a more rapid, considerable antihypertensive effect after sublingual administration. In addition, the high plasma levels of ketanserin-ol, the metabolite produced by hepatic reduction of ketanserin, reached after sublingual administration, rather than transmucosal absorption, indicate that the clinical effect observed is due to more rapid dissolution of the tablet formulation and liberation of the active drug.

Administration, Oral↗
PubMedDate not supplied

Pharmacokinetic aspects of the sublingual administration of vincamine.

The sublingual absorption of vincamine used as tracer occurs in two successive absorption steps: true sublingual absorption and absorption in the gastrointestinal tract of the drug dissolved in the saliva and not absorbed through the buccal mucosa. This is confirmed by a pharmacokinetic study and simulation. These two successive absorptions can explain the increase in the amounts of drug absorbed.

Administration, Oral↗
PubMed1990

Sublingual administration of captopril versus nitroglycerin in patients with severe congestive heart failure.

Angiotensin-converting enzyme inhibition has proven to be a successful approach for the long-term treatment of patients with congestive heart failure. This investigation compared the acute hemodynamic changes after sublingual administration of the angiotensin-converting enzyme inhibitor captopril with those after nitroglycerin. A total of 24 patients with severe left heart failure (New York Heart Association classes III and IV) were given 25 mg captopril and 0.8 mg nitroglycerin sublingually in this randomized, cross-over study. Hemodynamic monitoring revealed a clear improvement in pre- and afterload parameters for both drugs (P less than 0.01 and P less than 0.001), while captopril induced a higher increase in cardiac index (+49.2% vs. +25%), stroke volume index (+53.5% vs. +25.7%), and stroke work index (+55% vs. +28%) than nitroglycerin (P less than 0.001). Although not statistically significant, the onset of change for most hemodynamic parameters was measured earlier after nitroglycerin (after 12-19 vs. 16-22 minutes). Captopril revealed later peak effects (after 47-84 vs. 25-55 minutes, P less than 0.001) and a longer sustained improvement in hemodynamic values (return to baseline values after 117-162 vs. 68-120 minutes, P less than 0.001). No side effects occurred after either captopril or nitroglycerin in this study. Thus, these results indicate there is an early improvement in hemodynamic parameters after the sublingual administration of both drugs in patients with severe congestive heart failure, and that captopril induces a more pronounced and prolonged improvement than nitroglycerin.

Administration, Sublingual↗
PubMed1975

Regional left ventricular wall dynamics before and after sublingual administration of nitroglycerin.

Regional wall dynamics of the left ventricle before and after sublingual administration of 0.6 mg of nitroglycerin were determined from left ventricular angiograms in 27 patients undergoing coronary arteriography. Regional wall dynamics were quantitatively measured from 60/sec determinations of wall thickness and derived peak rate of systolic wall thickening (peak dTw/dt) in selected sites of the left ventricle. A total of 70 regions were studied. Analysis of the same segment before and after administration of nitroglycerin revealed that the mean change in peak dTw/dt was +1.97 cm/sec in segments with an initial peak dTw/dt of less than 5 cm/sec, in contrast to a change of +0.66 cm/sec in segments with an initial control value of 5 cm/sec or greater. Akinetic or dyskinetic areas did not show improvements after nitroglycerin. In 11 left ventriculograms, an area that was initially hypokinetic manifested an increase in rate of wall thickening after nitroglycerin. The mean increase in peak dTw/dt in anterior segments with electrocardiographic evidence of myocardial infarction was 0.18 cm/sec (P less than 0.05) after nitroglycerin, compared with a mean change of 1.33 cm/sec in anterior segments without such evidence. This study presents evidence for a regional myocardial response to nitroglycerin with differing responses within the same ventricle apparently depending upon the functional state of the underlying myocardium.

Aged↗
PubMed1990

The effect of captopril on peripheral hemodynamics in patients with essential hypertension: comparison between oral and sublingual administration.

A comparative study of the effects of oral and sublingual captopril on the hemodynamics of the peripheral musculocutaneous vasculature was carried out on ten patients with essential hypertension. Both routes of administration of captopril lead to lower blood pressure and decreased regional resistance, and to an increased arterial blood flow at rest. The first measurable effect and the peak effect on blood pressure and peripheral hemodynamics appear slightly earlier with sublingual administration. The data provided in this study support the usefulness of the sublingual route in clinical situations in which oral administration of captopril is not feasible.

Administration, Oral↗
PubMed1990

Myocardial infarction following sublingual administration of isosorbide dinitrate.

A 78-year-old with healed septal necrosis suffered a recurrent myocardial infarction of the anterior wall following the administration of isosorbide dinitrate 5 mg sublingually. After detailing the course of events, we discuss the role of paradoxical coronary spasm and hypotension-mediated myocardial ischemia occurring downstream to significant coronary arterial stenosis in the pathophysiology of acute coronary insufficiency.

Administration, Sublingual↗
PubMed1989

The pharmacokinetics of clotiazepam after oral and sublingual administration to volunteers.

We have studied the single dose pharmacokinetics of 5 mg clotiazepam drops, oral tablets, and sublingual tablets in a cross-over study in 6 healthy volunteers (median age 28 years). The formulations had similar systemic availability. Compared with oral tablets the sublingual route gave a lower peak concentration and a delayed peak time, while drops gave a greater maximum concentration with a similar peak time. The use of drops is suggested for a more marked initial effect and the sublingual route for easier administration, especially in the elderly.

Administration, Oral↗
PubMed1989

[Nifedipine level in the blood and its immediate hypotensive effect after its sublingual administration to aged patients].

In 28 aged patients (means = 73.1 years) with arterial hypertension nifedipine has been administered sublingually in a single dose of 20 mg and the hypotensive effect of that drug under the control of its concentration in the blood serum was evaluated. The nifedipine concentration was determined by the use of gas chromatography with electron capture detector. The mean drug concentration increased from 38.1 ng/ml to 82.3 ng/l during the 2nd hour of observation. After 3 hours the lowering of the nifedipine concentration and the decrease of its hypotensive effect was observed. After 15 min from the drug application the systolic pressure lowered by the average 22.1 mmHg whereas the diastolic pressure was 7.0 mmHg lower. The most significant pressure decrease (mean of systolic pressure 52.7 mmHg) 7.03 kPa and that of diastolic pressure 23.2 mmHg (3.1 kPa) occurred after 2 and 1.5 hours. The decrease of pressures after nifedipine correlated with the start-point value of systolic pressure. The frequency of the heart action in the whole group did not altered significantly, however, in individual cases both the acceleration of that action (34 per min) or acceleration (42 systoles per min) was noted. Slight typical side-effects were noted in 5 treated patients. A single-dose sublingual 20 mg nifedipine (Cordafen--Polfa) administration enabled in all the subjects the obtaining of therapeutic drug level in the blood and in the aged patients with hypertension may be regarded as efficacious antihypertensive treatment.

Administration, Sublingual↗
PubMed1992

Role of sublingual administration of tablet buprenorphine hydrochloride on relief of labour pain.

Tablet buprenorphine hydrochloride when administered to 34 primigravida women sublingually in a dose of 6 micrograms/kg body weight during the first stage of labour, the analgesic action started 30 minutes after administration of drug and the analgesic action increased gradually and reached its peak level 3 hours after administration of drug. Analgesic action continued throughout the first stage of labour when the duration after administration of drug was 9 hours. In one case maximum analgesic action did not persist after 9 hours. The average time of delivery was 5.88 hours having cervical dilatation of 3.1 (+/- 0.13) cm and the progress of labour was not delayed by the drug. There was no cardiorespiratory depression of the subjects. None complained of nausea or vomiting. There was no change in foetal heart rate and Apgar scoring of neonates revealed the average value of 9.71 at 1 minute and 9.94 at 5 minutes.

Administration, Sublingual↗
PubMed1989

[Hemodynamics after sublingual administration of captopril in severe heart failure. A pilot study].

In a preliminary trial, 23 patients in severe left-heart failure and, in some instances, also right-heart failure (NYHA classes III and IV) received a single sublingual dose of 25 mg captopril. Invasive measurement of various haemodynamic parameters indicated (1) an increase in cardiac index and stroke-volume index of 34% and 38%, respectively (P less than 0.001 for each); (2) decrease in pulmonary artery and systemic pressures by an average of 7% and 11.4% (P less than 0.01 and less than 0.001, respectively); (3) no significant change in heart rate and mean right atrial pressure; (4) decrease in systemic and pulmonary artery resistance by 33% and 29% (P less than 0.001 for both); (5) an increase in left ventricular stroke work index by 18% (P less than 0.001); and (6) a fall in heart rate x pressure product by 10% (P less than 0.005). These haemodynamic changes started within 12 to 23 minutes after captopril administration, the peak effect occurring between 40 and 90 minutes. Baseline values were reached after three hours. Reproducibility measurements revealed a close quantitative and temporal correlation (r for all greater than 0.8). To obtain similar changes of cardiac function 1.65 micrograms/min.kg sodium nitroprusside were needed. The results indicate that sublingual administration of captopril in severe heart failure will achieve early and significant improvement in cardiac function.

Administration, Sublingual↗