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PubMedDate not supplied

Ocular hypotensive effect of sublingual administration of timolol.

PURPOSE: A randomized clinical, trial to assess ocular hypotensive effect of sublingual administration of timolol was performed. PATIENTS AND METHODS: Seventeen (9 male, 8 female; age range 45 to 68 years) with bilateral ocular hypertension were selected for the study. Each patient was evaluated with regard to IOP, arterial blood pressure and heart rate before and after each of the following experimental treatment: unilateral ocular administration of 20 microliters of 0.5% timolol solution; sublingual administration of 20 microliters of 0.5% timolol solution; unilateral ocular administration of 20 microliters of saline solution (placebo); sublingual administration of 20 microliters of saline solution (placebo). The sequence of the treatments and the eye topically treated were randomly chosen. At least four weeks wash-out elapsed between each experimental treatment. RESULTS: Our results showed that sublingual administration of timolol was able to induce a bilateral significant reduction of the IOP. This reduction was not statistically different from that obtained in the eye treated with timolol. A significantly greater reduction of the IOP was obtained by sublingual timolol than in the contralateral eye after unilateral topical administration of timolol solution. No significant modification of arterial blood pressure and heart rate were evidenced after the treatment. CONCLUSIONS: Sublingual administration seems to be a new interesting way for reducing the IOP. Long term studies are required in order to test efficacy and safety of this new treatment.

Administration, Sublingual↗
PubMed1999

Comparison of sedative effects of romifidine following intravenous, intramuscular, and sublingual administration to horses.

OBJECTIVE: To compare sedative effects of romifidine following IV, IM, or sublingual (SL) administration in horses. ANIMALS: 30 horses that required sedation for routine tooth rasping. PROCEDURE: Horses (n = 10/group) were given romifidine (120 microg/kg) IV, IM, or SL. Heart rate, respiratory rate, head height, distance between the ear tips, thickness of the upper lip, response to auditory stimulation, response to tactile stimulation, and degree of ataxia were recorded every 15 minutes for 180 minutes. Tooth rasping was performed 60 minutes after administration of romifidine, and overall adequacy of sedation was assessed. RESULTS: IV and IM administration of romifidine induced significant sedation, but SL administration did not induce significant sedative effects. Scores for overall adequacy of sedation after IV and IM sedation were not significantly different from each other but were significantly different from scores for horses given romifidine SL. Sedative and other effects varied among groups during the first 60 minutes after drug administration; thereafter, effects of IV and IM administration were similar. CONCLUSIONS AND CLINICAL RELEVANCE: Onset of action was fastest and degree of sedation was greater after IV, compared with IM, administration of romifidine, but duration of action was longer after IM administration. Sublingual administration did not result in clinically important sedative effects.

Acoustic Stimulation↗
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↗
PubMed1981

Rapid absorption of micronized estradiol-17 beta following sublingual administration.

The effect of sublingual administration of 2 mg of micronized estradiol-17 beta (E2) on circulating concentrations of estrone (E1), E2, luteinizing hormone, and follicle-stimulating hormone was evaluated. Six women were studied during the early follicular phase, along with 3 hypogonadal women. Absorption of E2 was extremely rapid with a respective 9-fold and 41-fold increase over basal serum levels within 30 minutes. However, for most of the 24-hour period studied, E1 rather than E2 was the predominant circulating estrogen. Although physiologic levels of E2 can be maintained, it would appear that the sublingual route is not ideal for E2 replacement, as concomitant superphysiologic elevation of circulating E1 occurs.

Absorption↗
PubMed2005

Comparison of misoprostol plasma concentrations following buccal and sublingual administration.

BACKGROUND: New indications for misoprostol include medical abortion, cervical softening, induction of labor and treatment of postpartum hemorrhage. Various routes of misoprostol administration under study include oral, vaginal, buccal, sublingual and rectal. MATERIALS AND METHODS: This was an open-label, randomized, cross-over study of the pharmacokinetic differences of buccal vs. sublingual misoprostol 800 mug in 10 healthy women. RESULTS: Of the 10 women enrolled, 2 withdrew after experiencing excessive cramping from the sublingual route of misoprostol. The mean misoprostol plasma concentration-time curves at 4 h [area under the curve (AUC)0-4)] and the maximum concentration (C(max)) showed that levels were significantly higher for sublingual administration than the buccal route. Buccal misoprostol administration resulted in fewer symptoms and was found to be more acceptable. CONCLUSIONS: Sublingual administration of misoprostol had a higher AUC and C(max) compared with buccal administration. The pharmacokinetics may help to determine the best application of misoprostol depending on the indication.

Abortifacient Agents, Nonsteroidal↗
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↗
PubMed2006

Plasma pharmacokinetics of desmopressin following sublingual administration: an exploratory dose-escalation study in healthy male volunteers.

OBJECTIVE: Desmopressin is usually administered intranasally in the treatment of central diabetes insipidus or nocturnal enuresis. The sublingual administration of desmopressin is expected to be an alternative to the intranasal route with advantages to children and to patients with allergic rhinitis or chronic rhinosinusitis. Therefore, the present study was carried out to explore the time-versus-concentration profile of desmopressin in plasma after sublingual administration to healthy volunteers. SUBJECTS AND METHODS: A total of 16 healthy male volunteers were enrolled in this open, exploratory, 1-period, randomized, dose-escalation study. Volunteers received a single sublingual dose of either 20, 40, 80, 160, 240 or 320 microg of desmopressin acetate. Desmopressin plasma concentrations were measured over a 12-hour period using a validated radioimmunoassay method. Safety and tolerability were assessed simultaneously. RESULTS: Plasma concentrations of desmopressin were below the lower limit of quantification (LLOQ) of 5 pg/ml for doses lower than 80 microg. For the doses of 160 - 320 microg the time-versus-concentration profiles were higher than the LLOQ. The area under the curve from 0 - 12 h (AUC0-12h) was 54.66 +/- 25.92 pg x h/ml after the 160 microg dose, 104.38 +/- 79.10 pg x h/ml following the 240 microg dose and 133.18 +/- 181.84 pg x h/ml following the 320 microg dose. Given the data from previous experiments, the time-versus-concentration profile of desmopressin in plasma after a sublingual dose of 240 microg appeared to be in the range of previously published data on an intranasal dose of 20 microg. Sublingual administration of desmopressin proved to be safe and was well tolerated by all volunteers. CONCLUSION: A very high inter-individual variability in desmopressin plasma concentrations was detected after sublingual administration. A sublingual dose of 240 microg of desmopressin appeared to result in a pharmacokinetic profile comparable to 20 microg administered intranasally. These data, however, need to be verified in a separate well-designed prospective clinical study.

Administration, Oral↗
PubMed2005

Sublingual administration of Delta9-tetrahydrocannabinol/beta-cyclodextrin complex increases the bioavailability of Delta9-tetrahydrocannabinol in rabbits.

The bioavailability of Delta(9)-tetrahydrocannabinol (THC) was determined after its sublingual administration as solid THC/beta-cyclodextrin (THC/beta-CD) complex, and was compared to oral administration of ethanolic THC, in rabbits. The absolute bioavailability of THC after sublingual administration of solid THC/beta-CD complex powder (16.0 +/- 7.5%; mean +/- SD; n = 4) is higher than the bioavailability of THC after oral administration of ethanolic THC solution (1.3 +/- 1.4%; mean +/- SD; n = 4). The results suggest that sublingual administration of THC/beta-CD complex is a useful tool in improving absolute bioavailability of THC.

Administration, Oral↗
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↗
PubMed1987

gamma-Cyclodextrin:testosterone complex suitable for sublingual administration.

A crystalline complex of testosterone with gamma-cyclodextrin was evaluated for solubility and dissolution rate. Whereas these parameters were at least an order of magnitude lower than those of testosterone complexes with amorphous derivatives of cyclodextrins, the properties of the crystalline complex enabled the preparation of a suitable pharmaceutical form for the sublingual administration of hormone to humans. This is in contrast to the situation with similar beta-cyclodextrin complexes, in which such administration was ineffective. Sublingual administration of the gamma-cyclodextrin complex, as shown in previous work using amorphous complexes, avoided rapid first-pass loss of hormone and directed it effectively into the circulation; administration of the complex into the stomach resulted in much lower circulatory hormone levels.

Administration, Sublingual↗
PubMed2003

The start of pharmacological activity after sublingual administration of sildenafil citrate in 30 patients affected by erectile dysfunction.

INTRODUCTION AND OBJECTIVES: Sildnenafil citrate is a powerful phosphodiesterase type 5 isoenzyme; it is the first oral treatment to have had a significant success in treatment of erectile dysfunction (ED). After oral dosing on an empty stomach the pharmacological activity starts within 30 to 120 minutes (average 60 minutes) whereas the effect of this medication after a meal could be notably delayed. We evaluated the start of pharmacological activity in 30 patients affected by non-psychogenic ED after sublingual administration of Sildenafil citrate. METHODS: Patients participating in our study were all affected by ED whose etiology was assessed as vasculogenetic or diabetic. The study lasted 6 months. For the first 3 months patients were asked to take Sildenafil (50-100 mg) for oral administration, under normal everyday conditions, 30 minutes before planned sexual relations. During the second 3 months the patients were asked to take Sildenafil for sublingual administration (crushing the pill in the mouth and dissolving the drug under the tongue) 15 minutes before planned sexual relations. The patients did not know the purpose of the study. RESULTS: An appreciable reduction in the start of pharmacological activity was reported during the time of sublingual administration. In fact, while throughout the first 3 months the average pharmacological onset was 62.8 minutes (DS +/- 16.8), during the second 3 months it was 29.3 minutes (DS +/- 8.1), the mean difference in the start of pharmacological activity was 35.3 (DS +/- 12.4). The results of T-student test for paired observation were T (29) = 15.629; p-value 0.00001. During the two modalities of administration no differences were noted in the efficacy or in the frequency of adverse events. All the patients declared they preferred the sublingual way because of faster onset. CONCLUSIONS: Even though ours is a limited study, our clinical data points out that the sublingual administration of Sildenafil is useful because of the rapid onset unrelated to meals. All the patients were reported to appreciate this method of administration, particularly in the case of unplanned sexual relations.

Administration, Oral↗
PubMed2007

Precipitation complexation method produces cannabidiol/beta-cyclodextrin inclusion complex suitable for sublingual administration of cannabidiol.

In the present study, the precipitation complexation method was used to prepare a complex of cannabidiol (CBD) with beta-CD. The effect of beta-CD-complexation on the sublingual absorption of CBD was studied in rabbits. A solid CBD/beta-CD inclusion complex was prepared by precipitation and the effect of complex formation on the dissolution rate of CBD was studied. The absorption of CBD (a 250 microg/kg dose of CBD in all formulations) after sublingual administration of solid CBD/beta-CD complex and ethanolic CBD solution, and after oral administration of ethanolic CBD solution, was studied in vivo in rabbits. The dissolution rate of solid CBD/beta-CD complex in vitro was significantly (p<0.05) higher than that of plain CBD. The absorption of CBD (AUC0-300 min) decreased in the following order: sublingual ethanolic CBD solution (420+/-120 ngxmin/mL; mean+/-SD; n=4)>sublingual solid CBD/beta-CD complex (270+/-120 ngxmin/mL)>oral ethanolic CBD solution (concentrations in plasma below the quantitation limit). The results demonstrate that sublingual administration of a solid CBD/beta-CD complex enhances the absorption of CBD in rabbits when compared to oral administration of ethanolic CBD. Furthermore, the solid CBD/beta-CD complex may provide an alternative formulation for sublingual administration of CBD.

Absorption↗
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↗