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PubMed2002

Sublingual apomorphine for the treatment of erectile dysfunction.

Erectile dysfunction (ED) is a prevalent problem in the world and wreaks havoc on the psychosocial well-being of sufferers as well as partners. First-line treatment for ED is oral therapy, however, the currently available oral erectogenic agent is not uniformly successful and requires approximately 1 h to exert its effect. Apomorphine is a novel, oral erectogenic agent taken sublingually. It exerts its effect on hypothalamic centres involved in the triggering of the erection cascade. It dissolves rapidly and results in an erection in responders in approximately 20 min. By avoiding first pass metabolism through its sublingual administration, apomorphine avoids any significant interaction with food or other drugs. In trials in over 4000 subjects representative of the general ED population, beneficial effects were seen in a significant percentage of men. Its exact position in the market remains to be seen, however, its ability to permit spontaneous sexual relations will prove to be of significant benefit to many men.

Administration, Sublingual↗
PubMed1990

Angiographic response to a vasodilating drug, nicorandil, in patients with coronary artery disease.

To investigate the usefulness of nicorandil as an antianginal drug, we compared the coronary vasodilatory response in nonstenotic coronary artery segments and the hemodynamic response in 26 coronary artery disease patients. Both responses were studied prior to sublingual administration of 10 mg of this drug and 10, 30 and 60 min afterward. The plasma nicorandil concentration was determined up to 120 min after administration. The mean coronary dilating ratio of nicorandil was 117% 30 min after administration (p less than 0.01) and showed a good correlation to the plasma nicorandil concentration. The mean maximum dilating ratio of each patient was 125%. There was no difference between individual coronary arteries or between proximal and distal segments in terms of the coronary artery dilating ratio. The plasma nicorandil concentration required for 120% dilation of the coronary arteries was 26 ng/ml, 89 ng/ml and 142 ng/ml for those cases with variant angina, exertional angina and postinfarction angina, respectively. Hemodynamic changes due to administration of this drug included a decrease in blood pressure, and a reduction in total peripheral resistance, rate-pressure product, pulmonary capillary pressure and stroke-work index. These results indicate that the antianginal effects of nicorandil are derived from its coronary vasodilatory action and an inhibitory effect on myocardial oxygen consumption.

Administration, Sublingual↗
PubMedDate not supplied

Sublingual nifedipine controversy in drug delivery.

Nifedipine, given sublingually, has become increasingly common for treatment of cardiovascular crises. While this may seem an expedient and safe method to reduce blood pressure, controversial issues have surfaced that emphasize the need for cautious drug delivery. Moreover, sublingual administration of nifedipine is not currently approved by the Food and Drug Administration.

Administration, Sublingual↗
PubMed1989

[Prediction of true and false positive responses to exertion by a second exercise under sublingual nitroglycerin. Multivariate analysis].

The authors consider that the diagnostic value of exercise tests could be improved by a multivariate analysis integrating the ergometric data of two exercise tests: a reference test and a test performed under nitroglycerin. 109 patients without previous myocardial infarction who suffered from angina-like chest pain were explored. All had an ischaemic-type ST depression on the CM5 lead during the first exercise test and were tested again after sublingual administration of nitroglycerin. Both tests were continued until the theoretical maximum heart rate was reached or symptoms were no longer bearable. Coronary arteriography showed that 27 patients had normal coronary vessels and 82 had a coronary disease. At univariate analysis, two parameters were significant in predicting coronary disease. These were an in increase, between the two tests, of maximal work performed (from 95 +/- 1578 kpm to 2085 +/- 1662 kpm, p less than 0.001) and of the double product, i.e. maximum heart rate x maximum systolic arterial pressure (from 181 +/- 5289 to 3826 +/- 4245 mmHg.b.min-1, p less than 0.001). Five variables were selected by logistic regression analysis, viz.: change in ST depression between the two tests, double product during the first test, sex, modification of work performed between the two tests and occurrence of chest pain during the first test. By using a threshold analysis (less than 20 p. 100, greater than 80 p. 100), 76 p. 100 of the population was correctly classified; 82.9 p. 100 of coronary disease patients and 53 p. 100 of normal subjects were well classified, whereas 2.7 p. 100 of the population studied (all normal subjects) were erroneously classified.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Sublingual↗
PubMed1989

Correlation between isosorbide dinitrate plasma levels and coronary vasodilation after chewing capsules.

In 10 patients with coronary artery disease coronary angiograms were performed in identical projections before and 5, 10 and 15 min after sublingual administration of two chewing capsules with 5 mg of isosorbide dinitrate (ISDN) each. Simultaneously, blood samples were taken for gas-chromatographical determination of nitrate plasma levels. The average ISDN plasma levels amounted to 138 +/- 73 ng/ml, 102 +/- 76 ng/ml and 62 +/- 34 ng/ml in the fifth, tenth and fifteenth min, resp. In the fifteenth min significant isosorbide mononitrate plasma levels (greater than 70 ng/ml) were found only in three patients. Mean diameters of angiographically normal coronary segments were measured with the automatic edge detection system CAAS; they increased by an average of 20 +/- 10%, 26 +/- 11%, and 27 +/- 13% (p less than 0.001) in the fifth, tenth and fifteenth min, resp. Due to hysteresis of the coronary dilation in relation to ISDN plasma levels no significant correlation was found between these parameters. The minimal diameters of seven of 10 coronary stenoses analyzed in seven patients reacted with a maximal increase of 23%-98%. Thus, ISDN chewing capsules may be preferable for rapid and prolonged relief of anginal attacks as well as for potent dilation of epicardial coronary arteries as desired during angiography.

Administration, Sublingual↗
PubMedDate not supplied

Bioavailability and pharmacokinetics of nifedipine administered by different routes in healthy volunteers.

Absolute bioavailability (F) of 10 mg nifedipine capsules was studied in six adult healthy male volunteers. The drug was given swallowed and sublingual and the results compared with data obtained when the drug was administered intravenously (0.015 mg/k). The pharmacokinetic profile of nifedipine was performed from venous blood samples obtained over a period of 8 hours, with a specific gas chromatographic assay. Besides bioavailability (F), also were calculated the peak plasma concentration (Cmax), the time to reach Cmax, (tmax), the clearance of the drug (CL), the apparent volume of distribution (V1), the elimination half-life (t1/2 beta), and the area under the curve (AUC). The F value was 44.5 + 7.5% and 48.7 + 8.3% for the swallowed and sublingual routes respectively; however, during the sublingual administration the mean Cmax was larger (92.9 +/- ng/ml), and mean tmax greater (1 h), than the data obtained following the swallowed administration (134.1 +/- 17.7 ng/ml and 0.5 h respectively; p less than 0.05). When nifedipine was administered intravenously the mean t1/2 beta was 2.063 +/- 0.24 h, the mean CL was 0.234 + 0.017 l/h.kg, and the mean V1 was 0.278 + 0.027 l/kg; these data did nat show the great individual variability reported by other authors. Due to the mean AUC, less than 450 ng.h/ml, the group of volunteers of this trial could be classified as rapid metabolizers. Finally, there was a significant linear correlation between nifedipine plasma concentrations and the changes observed in the heart rate blood pressure (r = 0.85; p less than 0.05).

Administration, Oral↗
PubMed1989

Drug plasma levels and coronary vasodilation after isosorbide dinitrate chewing capsules.

Five, ten and fifteen min after sublingual administration of 10mg isosorbide dinitrate (ISDN) in chewing capsules, in 10 patients with coronary artery disease, ISDN plasma levels were correlated with the dilation of epicardial coronary arteries as well as with changes in aortic blood pressure and heart rate. Due to the rapid and extensive drug absorption, maximal ISDN plasma levels averaged 138 +/- 73 ng ml-1 and were already obtained after 5 min; they declined to 102 +/- 76 and 62 +/- 34 ng ml-1 in the 10th and 15th min respectively. In 7 patients isosorbide mononitrate plasma levels were still negligibly low (less than 30 ng ml-1). Mean diameters of 'normal' coronary segments increased by an average of 20 +/- 10%, 26 +/- 11% and 27 +/- 13% (P less than 0.001) at 5, 10 and 15 min respectively compared to control. The maximal drop in systolic aortic pressure (147 +/- 19 to 115 +/- 15 mmHg; P less than 0.01) as well as the maximal increase in heart rate (66 +/- 4 to 80 +/- 11 beats min-1; P less than 0.01) were observed in the 15th min; diastolic aortic pressure and double product remained constant. Due to the long persistence of coronary dilation and haemodynamic changes, none of these drug effects correlated significantly with the ISDN plasma levels. In addition, the minimal diameters of 10 coronary stenoses were measured in 7 patients; with ISDN 7 stenoses showed dilation ranging from 23% to 98%.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Sublingual↗
PubMed1988

A new lormetazepam galenical formulation for sublingual premedication.

This study reports a double-blind evaluation of a new formulation of lormetazepam for sublingual administration, given as a premedicant in 48 female patients undergoing minor gynecological procedures. Both patient's and nurse's assessments for anxiety and sedation were recorded at different times. Anxiolysis and sedation were present 30 minutes after administration of the drug as reported by the patient with a peak effect at 45 minutes. Nurses reported significant differences in sedation only, but already present at 30 minutes after premedication. The memory test showed no persistent effect of the benzodiazepine one day after surgery.

Administration, Sublingual↗
PubMed1994

[Fast-dissolving sublingual tablets of piroxicam versus naproxen in the treatment of recurrent acute osteoarthrosis. Multicenter clinical trial].

An open comparative study was carried out to evaluate the efficacy and safety of piroxicam FDDF, for sublingual administration, versus naproxen in the treatment of osteoarthritis. Sixty-one patients with acute-phase osteoarthritis involving various joints are reported. They were treated with 20 mg/day piroxicam FDDF or with 1000 mg/day naproxen for a total of 4 weeks. Drug efficacy was evaluated on the base of the variation of spontaneous pain, pain on motion, functional limitation and capacity to perform a specific activity. The intensity of spontaneous pain on the first day showed a statistically significant improvement with both drugs, but the onset of analgesia was only after 15 minutes with piroxicam and after 1 hour with naproxen. The improvement in pain intensity increased on the first day and until the 7th day with both drugs, but the comparative analysis between the analgesic efficacy of the two treatments proved to be favourable to piroxicam. On the 7th day, pain on motion and the capacity to perform a specific activity showed a statistically significant improvement with both drugs, but the comparative analysis between the two treatments proved to be favourable to piroxicam. The two drugs showed the same efficacy in functional restriction. The local and systemic tolerability of piroxicam was good. Only 5 patients experienced 6 systemic side-effects, and 1 patients showed local side-effects, but 11 patients of the naproxen group showed 12 systemic side-effects. Thus piroxicam showed a better analgesic and anti-inflammatory efficacy than naproxen. Piroxicam proved to have a better systemic tolerability than naproxen. The local tolerability of piroxicam FDDF was good.

Acute Disease↗
PubMedDate not supplied

[Severe bradycardia and arterial hypotension following the administration of sublingual nitroglycerin].

Two patients with coronary artery disease who developed severe bradycardia (less than 40 beats/min) and hypotension (less than 65/...mmHg) in supine position following the administration of sublingual nitroglycerin in the course of an anginal pain are reported. The administration of intravenous atropine sulfate (1-1.5 mg) readily reverted both hypotension and bradycardia. In one patient this complication was observed three times; in this patient sublingual nifedipine (10 mg) was successfully used to treat subsequent anginal crisis.

Administration, Sublingual↗
PubMed1987

Buccal versus sublingual nitroglycerin administration in the treatment of angina pectoris: a multicentre study.

Buccal (Suscard) was compared with sublingual nitroglycerin (Nitromex) in 126 patients with stable angina pectoris. Following a dose adjustment period they were randomized to cross-over treatment, two weeks on sublingual and buccal nitroglycerin, respectively. The dosage of buccal nitroglycerin was 2.5 mg in 49% and 5.0 mg in 51%. The total number of treated acute anginal attacks was 31% less during the buccal compared to the sublingual nitroglycerin period (P less than 0.001) despite a reported physical activity level which was significantly higher during the buccal nitroglycerin period. The use of sublingual nitroglycerin and buccal nitroglycerin was considered equally simple by 67%, sublingual nitroglycerin easier by 19% and buccal nitroglycerin easier by 14% of the patients. Sublingual nitroglycerin was used prophylactically on 806 occasions and buccal nitroglycerin on 929 occasions (P less than 0.05) with success in 66% of the sublingual nitroglycerin-attempts and 74% of the buccal nitroglycerin-attempts (P less than 0.05). Considering only prophylactic use, buccal nitroglycerin was preferred by 81% and sublingual nitroglycerin by 4% (P less than 0.05). When given the opportunity only to select one of the two nitroglycerin formulations, 65% (P less than 0.05) preferred buccal nitroglycerin and 19% sublingual nitroglycerin. In conclusion, buccal nitroglycerin seems to be more efficacious than sublingual nitroglycerin. The explanation is probably that the two formulations are comparable in the treatment of acute anginal attacks, while buccal nitroglycerin has a more pronounced prophylactic effect due to its longer duration of action.

Administration, Buccal↗
PubMed1981

Syndrome of severe bradycardia and hypotension following sublingual nitroglycerin administration.

Severe bradycardia associated with profound systemic arterial hypotension was observed in 3 patients following sublingual nitroglycerin administration. All patients had clinical evidence of active ischemic heart disease. In 1 patient, third-degree heart block was observed several hours later, requiring pacemaker therapy. Radionuclide ventriculography in 1 patient during the bradycardia revealed no significant change in regional wall motion or in left or right ventricular ejection fraction. Review of the literature shows no consistent predictors as to which patients are at risk for developing this syndrome. Possible pathophysiologic mechanisms are discussed. These case reports illustrate an unpredictable and serious complication of nitroglycerin administration, and emphasize the need for caution in use of this drug for ischemic heart disease.

Aged↗
PubMed2002

Characterization of nifedipine solid dispersions.

The sublingual administration of nifedipine (NIF) is currently used in clinical practice. The sublingual administration of NIF solid dispersions (SD), by using a suitable dispenser, appears an interesting approach in the treatment of moderate and severe hypertensive emergencies. With this aim nine SD made of NIF and a low viscosity hydroxypropylmethylcellulose (HPMC) in different ratio were prepared by means of spray-drying technique and their structure was studied. Moreover, the drug dissolution properties from SD were verified. The characteristic peaks of crystalline NIF were not detectable by using the X-ray analysis when the NIF/HPMC ratios were lower than 50/50 w/w. In thermograms obtained from SD, the NIF melting endothermic peak disappeared when NIF/HPMC ratios were lower than 30/70 w/w; the experimental Tg values of SD were lower than the Tg values predicted by Gordon Taylor equation suggesting some type of non-ideality of mixing. In the SD FTIR spectra the NH stretching vibrations and the C=O stretch in esteric groups of NIF shift to free NH and C=O regions indicating the rupture of intermolecular hydrogen bond in the crystalline structure of NIF. The prepared SD improved the NIF dissolution rate in comparison with that of commercial NIF or NIF/HPMC physical mixtures. Moreover, the concentration of NIF in the dissolution medium increased decreasing the NIF content.

Administration, Sublingual↗
PubMed1983

Acute changes in infranodal conduction time following left ventriculography and sublingual nitroglycerin administration in man.

During diagnostic cardiac catheterization for the evaluation of chest pain, His bundle electrograms were obtained in 32 male patients before and 2 to 5 minutes after each of two interventions known to acutely affect left ventricular volume and left ventricular end-diastolic pressure (the injection of 40 to 60 cc of contrast medium during left ventriculography and the administration of 0.4 mg of sublingual nitroglycerin). Changes in left ventricular end-diastolic pressure (18 +/- 6 vs 30 +/- 7 mm Hg, p less than 0.001 following ventriculography and 32 +/- 8 vs 19 +/- 8 mm Hg, p less than 0.005 following nitroglycerin administration) were accompanied by parallel alterations in HQ (48 +/- 8 vs 54 +/- 10 msec, p less than 0.005 following ventriculography and 57 +/- 10 vs 53 +/- msec, p less than 0.005 following nitroglycerin administration), but there were no significant changes in atrioventricular (AV) nodal conduction (AH). Significantly greater changes in HQ were seen in patients with triple-vessel coronary artery disease than in the remainder of the population, although there was clinical and/or ECG evidence of ischemia in only one patient. We conclude that factors other than progression of intrinsic conduction system disease may affect infranodal conduction. HQ should be interpreted cautiously in situations with rapidly changing hemodynamics, especially in patients with severe coronary artery disease.

Bundle of His↗
PubMed2003

Pharmacokinetics of high-dose buprenorphine following single administration of sublingual tablet formulations in opioid naïve healthy male volunteers under a naltrexone block.

Sublingual buprenorphine formulations have been developed as treatments for opioid dependence. In three studies, opioid naïve healthy male subjects received Subutex tablets (buprenorphine 2 and 8 mg [N=27] or 12 and 16 mg [N=27]) or Suboxone (two formulations) tablets (buprenorphine 8 mg/naloxone 2 mg [N=36]) sublingually, under a naltrexone block for assessment of buprenorphine pharmacokinetics and tablet disintegration times. Plasma buprenorphine was quantified up to 72 h post-dose using a sensitive LC-MS/MS assay. Mean Cmax values ranged from 1.6 to 6.4 ng/ml and tmax from 0.5 to 3 h. Concentrations declined bi-exponentially and fluctuations after a meal suggested enterohepatic recirculation of buprenorphine. The terminal half-life was approximately 26 h (range 9-69). Cmax and AUC appeared to increase in proportion to Subutex dose over 8-16 mg. The Suboxone formulations were bioequivalent. The least squares mean (90% CI) treatment ratio for Cmax was 1.00 (0.92-1.10) and AUC was 1.00 (0.95-1.06). Median times of disintegration were similar for all doses and formulations (range 6-12 min). Sublingual buprenorphine, up to 40 times the 400 microg analgesic dose, was well tolerated in these opioid naïve subjects, as administration of naltrexone 50-150 mg was sufficient to attenuate anticipated adverse effects in this population of subjects.

Administration, Sublingual↗
PubMed1993

Comparative evaluation of ulcer prevention efficacy of orally, rectally and sublingually administered omeprazole in three acute gastric ulcer models in rats.

Ulcer prevention efficacy of orally, rectally and sublingually administered omeprazole was evaluated and compared using ulcer index and percentage inhibition of ulcerogenicity in three different acute gastric ulcer models viz, indomethacin, 0.6N HCl and aspirin (after pylorus ligation) induced ulcers in rats. The ulcer prevention efficacy after oral, rectal and sublingual administration were statistically significant (P < 0.01) in all the models. The differences in ulcer index and percentage inhibition of ulcerogenicity for rectal and sublingual administration were insignificant (P < 0.05) in indomethacin and HCl induced ulcers and were significant (P < 0.05) in aspirin induced ulcers. The ulcer prevention activity was significantly higher (P < 0.05) after rectal and sublingual routes when compared to oral administration in all three models evaluated. Results revealed a faster onset and higher extent of pharmacodynamic activity of omeprazole after rectal and sublingual administration.

Administration, Oral↗
PubMed2003

Pharmacokinetics of prostaglandins.

Naturally occurring prostaglandins (PGs) are rapidly metabolized in the human circulation. For clinical use a number of PG analogues have therefore been developed which are resistant to rapid inactivation. Among these are carboprost, gemeprost and misoprostol. Following intramuscular injection of carboprost, plasma levels peaked after 20 minutes and declined slowly thereafter. In amniotic fluid the half-life was between 31 and 37 hours. Gemeprost is administered vaginally, and maximum plasma levels were reached after 2-3 hours, with detectable levels for at least 6-8 hours. Pharmacokinetic data on misoprostol are available following oral, vaginal and sublingual administration. Following oral treatment, plasma levels peaked at about 30 minutes, while after vaginal administration of the tablets the levels increased gradually and reached maximum levels after 70-80 minutes, but remained detectable for a significantly longer time. After sublingual administration the peak concentration was the same as for oral treatment but declined significantly more slowly. Endocervical administration of PGE(2) might be regarded as a local therapy, while following vaginal administration increased plasma levels of metabolites can generally be found. The plasma profile varies with the vehicle used.

Abortifacient Agents, Nonsteroidal↗