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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↗
PubMed1953

The sublingual administration of curare.

A new method of administering d-tubocurarine transmucosally by sublingual pellets (and also by rectal suppository) was used in 100 patients. In therapeutic dosage of 6 to 12 mg., it was found to be non-toxic and very effective in relieving pain due to acute and chronic muscle spasm. The relief was often of long duration or permanent and no unpleasant side effects were noted in any case. The drug was found to be more prompt and more effective in its action than mephenesin. In addition to relief of pain, it was found to be useful in distinguishing between kinds of pain and hence in differential diagnosis.

Acetaminophen↗
PubMedDate not supplied

Quantitative and qualitative modifications of lymphocyte subsets after sublingual administration of isosorbide dinitrate in migraineurs. Preliminary report.

In 22 migraine patients and 5 healthy controls an investigation has been performed on lymphocyte subsets in basal conditions and 90 minutes after sublingual isosorbide dinitrate (IDN) administration. In all patients the drug assumption induced a typical migraine attack with increase in all examined lymphocyte subsets with except of NK cells. A statistically significant increase (p < 0.05) in T lymphocyte subsets we found during the crisis, whereas in healthy controls neither a migraine attack nor any modification in lymphocyte subsets could be observed. These results seem to confirm the immune alteration we have previously found in migraineous patients and suggest the possible role of IDN-stimulated endothelium not only in vasodilatation but also in production of substances responsible of the observed immune modifications.

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↗
PubMed1985

[Dynamics of coronary artery lumina during tests with cold and with intracoronary and sublingual administration of nitroglycerin in patients with different clinical forms of stenocardia].

Cold tests and those using intracoronary or sublingual nitroglycerin administration were applied during coronarography to 50 coronary patients with varying clinical manifestations of angina pectoris. The quantitative assessment of angiographic patterns showed the cold and nitroglycerin tests to change significantly the extent of stenosis in patients with spontaneous angina (by +13.3 and -30.8%, respectively) and those with angina of effort and at rest (by +5.6 and -12.0%, respectively) and have no such effect in patients with angina of effort. The change in the stenosed coronary arterial lumen was more marked in cases of excentric localization of the atherosclerotic patch inside the coronary artery, as compared to the concentric arterial narrowing. The data obtained demonstrate the variability of coronary arterial lumen at the site of atherosclerotic stenosis in a certain population of patients.

Adult↗
PubMed1994

[Are there indications for oral or sublingual administration of morphines?].

During the perioperative period, gastric emptying rate and first pass metabolism limit the use of oral morphine. The bioavailability of sublingual and buccal opioids is better as the uptake of active drug is governed by local blood flow. This way of administration requires patient cooperation. Sublingual buprenorphine is widely used; buccal morphine and oral transmucosal fentanyl deserve further evaluation, especially in children.

Administration, Oral↗
PubMed1979

[Absorption and excretion of g-strophanthin after intravenous or sublingual administration (author's transl)].

Tritiated g-strophanthin was administered to six volunteer patients in a dose of 0.25 mg intravenously and 6.0 mg sublingually 1-3 weeks apart. Radioactivity in plasma and urine was measured afterwards for 48 or 96 hours, respectively. Plasma concentration fell to about a fifth of the maximal concentration within 6 min after intravenous administration, total excretion within three days being about 50%, with a half-time of 11 hours. Measurable plasma concentration after sublingual administration was demonstrable only after 15 min in some and after 2 hours in all the six patients. Radioactivity counts increased up to the 24th hour, in three patients up to the 48th hour. Maximal plasma concentration ranged from 4.7 to 0.7 ng/ml, corresponding to levels reached 15 min or 4 hours, respectively, after intravenous administration. Urinary radioactivity reached its maximum after 24-48 hours and then decreased. Within three days 0.6 and 2.5% of the administered radioactivity was recovered, corresponding to the g-strophanthin doses of 0.072 to 0.3 mg. The findings once again confirm the low and irregular absorption of g-strophanthin when administered sublingually or orally.

Administration, Oral↗
PubMed1995

Triazolam pharmacokinetics after intravenous, oral, and sublingual administration.

This study was designed to evaluate the relative and absolute bioavailability of triazolam, 0.25 mg, after the administration of the marketed oral tablet and a sublingual prototype wafer; an intravenous dose was used as a reference. Twelve men were evaluated in a three-way crossover study; study days were separated by 1 week. A single dose was administered to each subject at approximately 8 a.m.; serial blood samples were obtained for the determination of triazolam concentration. The fraction absorbed relative to intravenous was 20% higher in the sublingual than in the oral treatment (p = 0.0128); the difference between treatments was greatest in the first 2 hours as indicated by the area under the curve from 0 to 2 hours (p < 0.05). The extraction ratio ranged from 0.05 to 0.25, and the predicted availability after oral administration was 86% with a range of 75 to 95%. In contrast, the observed mean absolute availability was 44% (oral) and 53% (sublingual). A potential explanation for this discrepancy between predicted and observed bioavailability is that after oral administration, a fraction of triazolam may be metabolized by cytochrome P450IIIA4 in the gut wall, with a separate fraction subject to first-pass metabolism in the liver. Although this study was not designed to identify sites of triazolam metabolism, the proposed explanation is consistent with the occurrence of P450IIIA4 in the stomach, small intestine, and liver. Doses administered sublingually avoid first-pass metabolism, producing earlier and higher peak concentrations than do doses administered orally.

Administration, Oral↗
PubMedDate not supplied

[Pharmacokinetics of glycerin trinitrate (nitroglycerin) after sublingual administration in patients with chronic ischemic heart disease].

Pharmacokinetics of nitroglycerin was studied in 22 patients with ischemic heart disease associated with angina of effort after sublingual intake of 0.5 mg standard granules. The maximal blood plasma concentration of the drug was shown to occur on the average in 4.4 minutes and was 2.56 ng/ml. The half-life in plasma was on the average 6.0 minutes, apparent clearance was 21.9 l/min. The mean retention time of nitroglycerin was 9.5 minutes. Significant fluctuations of pharmacokinetic parameters during repeated examinations in the same patient as well as between the patients were revealed. A sharp asymmetry of distribution of these parameters was observed that makes it necessary to use the mean arithmetical for characterization of the pharmacokinetic parameters.

Administration, Sublingual↗
PubMed2005

Pharmacokinetics and tolerability of different doses of fentanyl following sublingual administration of a rapidly dissolving tablet to cancer patients: a new approach to treatment of incident pain.

AIMS: It is estimated that two-thirds of cancer patients will at some point during their illness experience breakthrough pain. In this study, the pharmacokinetics of a novel sublingual dosage form of fentanyl developed for breakthrough pain was evaluated. METHODS: Eleven Caucasian patients (seven male and 4 female, aged 34-75 years, median 60 years) with metastatic malignant disease were recruited initially, but three patients withdrew. Prior to the study all patients were on continuous nonfentanyl opiate medication. The study was a double-blind, cross-over trial, consisting of three 1-day treatment periods. A new rapidly dissolving preparation of fentanyl, was administered sublingually in single doses of 100, 200 and 400 microg, respectively, on three separate occasions. Plasma fentanyl concentrations were determined using liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS). Pharmacokinetic parameters were calculated by noncompartment analysis. Tolerability and the occurrence of adverse events were monitored throughout the study by patient questionnaire. RESULTS: The data from nine subjects who completed at least two periods were used in the analysis of variance. There were no significant differences between doses (100, 200 and 400 microg) for dose adjusted AUC (F = 0.42, P = 0.6660), dose adjusted C(max) (F = 0.08, P = 0.9206) and Tmax (F = 0.94, P = 0.4107). Thus, these parameters showed dose proportionality. The differences (400-100microg) in dose adjusted AUC from the three-period crossover analysis was -0.016 min.ng/ml (t = 0.71, P = 0.8718). Interindividual variability in systemic exposure to fentanyl was fairly small (25-40%), which may be related to a good in vivo biopharmaceutical performance of the sublingual tablet, and a relatively small fraction of the dose being swallowed. The first detectable plasma concentration of fentanyl was observed between 8 and 11 min after administration. t(max) increased from 39.7 +/- 17.4 to 48.7 +/- 26.3 and 56.7 +/- 24.6 min for the 100, 200 and 400 microg doses, respectively. Adverse events were few and did not increase with increasing dose. CONCLUSION: With this rapidly dissolving fentanyl formulation, the first detectable plasma concentration of fentanyl was observed at 8-11 min after administration. The pharmacokinetics of the drug showed dose proportionately. This formulation of fentanyl seemed to be well tolerated by the patients.

Administration, Sublingual↗
PubMed1986

Plasma concentrations of flunitrazepam (Rohypnol) following oral and sublingual administration.

Flunitrazepam (Rohypnol) 2.0 mg was given as a single dose by the oral or sublingual route to ten volunteers using a cross-over design. Plasma concentrations of the drug were measured by gas-liquid chromatography for up to 6 hours after administration. The highest mean concentration occurred 45 min after administration irrespective of route. No significant differences were found between the two treatments at any time. Since the sublingual route compares favorably with other routes of administration, these findings suggest that sublingual flunitrazepam is valuable for premedication.

Administration, Oral↗
PubMed1991

Sublingual administration of captopril in patients with acute myocardial ischemia.

To investigate the anti-ischemic capability of the angiotensin-converting enzyme inhibitor captopril, 10 patients with acute myocardial ischemia (angina pectoris less than 1 h, ST-segment depression greater than or equal to 0.1 mV, no rise in creatine phosphokinase) received 25 mg captopril sublingually after being treated with an intravenous infusion of nitroglycerin (3 mg/h) and heparin (1200 IU/h) for 1 hour. A control group of 10 patients received placebo instead of captopril. Results showed a decrease of the initial ST-segment depression from 0.25 +/- 0.04 to 0.2 +/- 0.03 mV (p less than 0.01) with nitroglycerin for the captopril group and from 0.26 +/- 0.05 to 0.21 +/- 0.05 mV (p less than 0.01) for the control group. An additional decrease to 0.13 +/- 0.03 mV (p less than 0.001) was measured after sublingual captopril, while no significant change was found in the placebo group (0.19 +/- 0.04 mV). In both groups, 3 patients had no incidents of angina after 1-h nitroglycerin infusion. An additional 6 patients resolved their complaints after captopril administration in contrast to only 1 after placebo. Two patients in the placebo group required increased doses of nitroglycerin because of impairment of anginal complaints. Hemodynamic measurements documented a significant drop of pulmonary vascular resistance after a 1-h infusion of nitroglycerin (-12.9% and -13.1%, respectively, p less than 0.05), while all other parameters remained unchanged.(ABSTRACT TRUNCATED AT 250 WORDS)

Acute Disease↗
PubMed1997

Haemodynamic correlates of early and delayed responses to sublingual administration of isosorbide dinitrate in migraine patients: a transcranial Doppler study.

In normal subjects or migraine patients, nitrates induce a non-specific early headache caused by vasodilation of intracranial arteries. In migraineurs a delayed headache response to nitrates may have a typical clinical profile of a spontaneous migraine attack. The cerebral vasomotor changes of this delayed response require further study. Isosorbide dinitrate (IDN), an exogenous nitric oxide (NO) donor, was given at a dose of 5 mg sublingually and a bilateral transcranial Doppler device was used to monitor bilateral mean velocity (Vm) changes at the middle cerebral artery (MCA) after IDN administration and until delayed headache occurred. Spontaneous migraine-like headache occurred only in migraine patients during the delayed phase after IDN and was accompanied by a prolonged arterial vasodilation compared to normal subjects. This vasomotor response was more evident on the customary side of the head pain of a spontaneous migraine attack. Our findings suggest a particular vasomotor response to nitrates in migraine patients. This response is associated with the nitrate-induced headache and it is not evident in healthy pain-free controls during the delayed phase after administration of an NO donor. Owing to the short half-life of NO, the neurotransmitter released by IDN, and because of the late onset of headache, we believe the mechanism is unlikely to be vascular in origin, but may have a neurogenic component.

Administration, Sublingual↗
PubMed1991

Sublingual administration of testosterone-hydroxypropyl-beta-cyclodextrin inclusion complex simulates episodic androgen release in hypogonadal men.

In search of a more physiological testosterone (T) replacement therapy for hypogonadal states, we evaluated an inclusion complex of T with 2-hydroxypropyl-beta-cyclodextrin (HPBCD). HPBCD enhances T solubility and absorption, but HPBCD is not absorbed. Five hypogonadal men (mean age, 32.4 +/- 2.3 yr) with serum T levels below the normal range were treated in two separate experimental phases with either a 2.5- or 5.0-mg tablet of sublingual (SL) T-HPBCD three times daily for 7 days. Acute pharmacodynamic changes were monitored at baseline and 10, 20, and 40 min and 1, 1.5, 2, 3, 4, and 8 h after administration of the first dose. At the 5-mg dose, a maximal concentration (Cmax) of T (85.4 +/- 11.0 nmol/L) was achieved in 20 min (63 +/- 24-fold increase), followed by a rapid decline to below the normal range (less than 12 nmol/L) at 2 h, with an estimated half-life of decline of 1.87 +/- 0.19 h. The dihydrotestosterone (DHT) Cmax (4.1 +/- 0.5 nmol/L) occurred at 32 +/- 5 min (8.9 +/- 1.3-fold increase) and declined to below the normal range (less than 1.2 nmol/L) after 3 h. The integrated 8 h value for the ratio of T/DHT was 10.0 +/- 1.1, which fell within the normal range. The increment in androstenedione paralleled that in T, and the Cmax (6.8 +/- 0.9 nmol/L) was reached in 24 +/- 4 min (2.3 +/- 0.6-fold increase). Compared to baseline, the Cmax was significantly greater for T (P less than 0.005), DHT (P less than 0.0005), and androstenedione (P less than 0.005). Both estradiol (E2) and estrone (E1) remained in the normal range (less than 200 pmol/L), although the Cmax for E1 was significantly greater than baseline (P less than 0.05). Serum LH levels were suppressed (19.0 +/- 2.6%) at 2 h (P less than 0.05), without a significant change in FSH. During 7 days of treatment, there was no cumulative increase in basal T, DHT, and E2 levels or further decline in LH or FSH levels. There was no change in sex hormone-binding globulin levels. Similar results were observed with the 2.5-mg dose, suggesting that the capacity of SL absorption may be limited to a certain dose of T-HPBCD. The fluctuations in T after SL administration of T-HPBCD resemble endogenous episodic secretion. We conclude that T, complexed with HPBCD, is rapidly absorbed by the SL route and quickly metabolized without sustained elevations of DHT or E2.

2-Hydroxypropyl-beta-cyclodextrin↗
PubMed1988

Liquid chromatographic assay and pharmacokinetics of quazepam and its metabolites following sublingual administration of quazepam.

A reverse-phase liquid chromatographic method is described for simultaneous quantification of quazepam, and two of its metabolites, 2-oxoquazepam and N-desaklyl-2-oxoquazepam. The method uses a solid-phase extraction procedure to prepare plasma samples. After extraction, the methanolic extract is evaporated; the residue is then reconstituted in a small volume of mobile phase and chromatographed. The total chromatography time for a single sample is about 20 min. A sensitivity of 1 ng/ml for quazepam and its metabolites is attained when 1 ml of plasma is extracted. Analytical recovery of quazepam and its metabolites added to plasma ranged from 87 to 96%. The maximum within-day and day-to-day coefficients of variation for each compound at concentrations of 20 and 60 ng/ml were 7.6 and 11.2%, respectively. The method was applied to sublingual pharmacokinetic studies of quazepam in healthy volunteers.

Administration, Sublingual↗