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PubMed1998

The Effects of Sublingual Administration of Captopril on Parameters of Exercise Test and Neurohormonal Activation in Patients With Stable Angina Pectoris

A prospective randomized, double-blind, and placebo-controlled study was designed to investigate the effects of sublingual administration of captopril on the parameters of exercise test and neurohormonal activation in patients with stable angina pectoris. A total of 31 patients (28 male, 3 female; mean age 55.4 +/- 9.4 years) took part in the study. Coronary angiography and left ventriculography were performed in all cases and the patients were classified according to the ejection fraction (EF). Following sublingual placebo or 25 mg captopril, plasma levels of renin, angiotensin II, norepinephrine, and serum aldosterone levels were measured at rest and maximal exercise. test was performed. Hormone levels were remeasured immediately after the exercise. The same procedure was repeated the next day using captopril or placebo. Sublingual captopril administration increased the time to angina, the time to 1 mm ST depression, maximal exercise capacity, maximal exercise duration and decreased maximal ST depression, maximal systolic blood pressure, and maximal double product (p < 0.001-0.01). After the maximal exercise test following captopril, the % difference of angiotensin II, aldosterone, and norepinephrine levels was found to be significant lower and the % difference of the renin level was found to be significantly higher than those of placebo (p < 0.001). The effects of sublingual captopril on exercise parameters were additionally assessed in different left ventricular systolic function subgroups. The favorable effects were more prominent in cases with left ventricular systolic dysfunction. There were no adverse effects related to sublingual captopril use. As a result, sublingual administration of captopril improved the parameters of maximal exercise test and suppressed the neurohormonal activation during exercise. We suggest that sublingual captopril may be used effectively before planned daily activities in patients with stable angina pectoris.

Journal Article↗

PubMed1987

Left ventricular response to sublingual administration of nitroglycerin.

The aim of this study was to investigate whether the rapid improvement of the clinical condition of patients after administration of nitroglycerin can be documented objectively using the apexcardiogram. The study was performed on 28 male patients with coronary heart disease whose clinical condition allowed us to perform the initial polygraphic examination during an attack of angina pectoris. The heart rate and three apexcardiographic indexes were determined from non-invasive polygraphic tracings. The first index was the a/H (ratio: amplitude of apexcardiographic "a" wave to total amplitude of apexcardiogram). The second and third were the velocity of the anterior left ventricular wall motion during both isovolumic contraction (VwmC) and isovolumic relaxation (VwmR) of the left ventricle. The mean differences from initial values were calculated after 2, 4, 6 and 10 min following administration of nitroglycerin. Significant changes already occurred during the second minute after administration of nitroglycerin. All parameters remained significantly changed up to the 10th minute after this treatment. According to our results, the cardiovascular response to sublingual administration of nitroglycerin can be objectively evaluated by apexcardiography.

Administration, Sublingual↗

PubMed1994

Plasma concentrations of glyceryl trinitrate and its dinitrate metabolites after sublingual administration to volunteers. Simultaneous determination of glyceryl trinitrate and its dinitrate metabolites.

The plasma profiles of nitroglycerin (glyceryl trinitrate, GTN, CAS 55-63-0) and its dinitrate metabolites (1,2-GDN and 1,3-GDN) were estimated after sublingual administration of GTN tablets 0.5 mg (Nitromex) given in single doses to 20 volunteers. Blood samples (totally 20) were collected to 2 h after administration, and the plasma concentrations of GTN, 1,2-GDN, and 1,3-GDN were measured simultaneously by gas chromatography. The pharmacokinetic parameters, Cmax, tmax, t1/2, and the dinitrate ratio (AUC1,2-GDN/AUC1,3-GDN) were determined for each subject. The plasma concentrations of GTN reached a maximum of 1.38 ng/ml (mean) (range: 0.32-3.18 ng/ml) after 4.9 min (mean) (range: 3-8 min). The plasma concentrations of 1,2-GDN and 1,3-GDN reached a maximum of 3.11 ng/ml (mean) (range: 1.14-5.44 ng/ml) and 0.70 ng/ml (mean) (range: 0.33-1.19 ng/ml) after 13.7 min (mean) (range: 8-40 min) and 17.6 min (mean) (range: 8-40 min). The t1/2 values (mean) were 3.3, 35.5, and 38.1 min for GTN, 1,2-GDN, and 1,3-GDN, respectively. The dinitrate ratio was estimated to be 4.1 (mean).

Administration, Sublingual↗

PubMed1995

Changes in blood velocities of fetal circulation in association with fetal heart rate abnormalities: effect of sublingual administration of nifedipine.

Nifedipine has been used to treat hypertension in pregnancy, and does not influence fetal or uteroplacental circulations in patients with preeclampsia. A 29-year-old multi-gravid woman presented at 32 weeks' gestation with significant elevation of her blood pressure. After sublingual administration of nifedipine, the blood pressure decreased from 208/122 to 136/96 mm Hg at 30 minutes. In her growth-retarded fetus with abnormal flow velocity waveforms, pulsatility index values for middle cerebral artery and umbilical artery did not change; however, peak systolic velocities, end-diastolic velocities, and time-averaged mean peak velocities for these arteries became significantly elevated. Simultaneously, severe variable decelerations and late decelerations occurred. The adverse effect of nifedipine on fetal circulation might occur in a growth-retarded fetus with abnormal flow velocity waveforms.

Administration, Sublingual↗

PubMed1983

Raynaud's syndrome. Treatment with sublingual administration of nitroglycerin, swinging arm maneuver, and biofeedback training.

Sublingual (SL) administration of nitroglycerin, a swinging arm maneuver, and biofeedback were evaluated for their effectiveness in decreasing hand rewarming time after ice immersion in six patients with Raynaud's disease and four patients with Raynaud's phenomenon. After ice immersion of their hands, ten normal patients showed rewarming to baseline temperatures in less than six minutes, while in nine of ten patients with Raynaud's syndrome, rewarming took more than 40 minutes. Two of ten patients with Raynaud's syndrome showed rewarming in less than six minutes after SL administration of nitroglycerin, while eight of ten patients with Raynaud's syndrome showed rewarming in less than 20 minutes after biofeedback training sessions. Six of the ten still showed rewarming in 20 minutes or less eight weeks after the sessions were over. A swinging arm maneuver provided no objective improvement. Sublingual administration of nitroglycerin provides a new alternative therapy for certain individuals. Effective biofeedback training can be learned in a relatively short time but should be reserved for the well-motivated patient.

Adult↗

PubMed1997

Central 5-HT2A and D2 dopamine receptor occupancy after sublingual administration of ORG 5222 in healthy men.

It has been suggested that a combined blockade of 5-HT2A and D2-dopamine receptors improves efficacy and reduces the risk for extrapyramidal symptoms when treating schizophrenic patients with antipsychotic drugs. ORG 5222 is a new potential antipsychotic drug which has high affinity for 5-HT2A, D2-dopamine and alpha 1 adrenergic receptors in vitro. The objective of this study was to examine if ORG 5222 occupies 5-HT2A and D2-dopamine receptors in human subjects in vivo. Central receptor occupancy was measured by positron emission tomography (PET) in three healthy subjects after sublingual administration of 100 micrograms ORG 5222. [11C]N-methylspiperone ([11C] NMSP) was the radioligand used to measure 5-HT2A receptor binding in the neocortex and [11C]raclopride to measure D2-dopamine receptor binding in the striatum. The 5-HT2A occupancy was 15-30% and the D2-dopamine receptor occupancy was 12-23%. The study confirms that ORG 5222 binds to 5-HT2A and D2-dopamine receptors in human brain. Since receptor occupancy of ORG 5222 is rather low, doses higher than 100 micrograms are suggested in future clinical trials to evaluate the antipsychotic drug effect of ORG 5222.

Administration, Sublingual↗

PubMedDate not supplied

Rush immunotherapy with sublingual administration of grass allergen extract.

A study of RUSH specific immunotherapy by sublingual route has been performed. Twenty patients have been studied suffering from rhinoconjunctivitis a/o allergic asthma to grass pollen, divided in two homogeneous groups. The first group was treated with immunotherapy, the other was used as a comparison in open. The level of specific IgG4, specific IgE, drug consumption and the symptom score were monitored. The symptom and drug scores recorded by the patients during the pollen season were significantly reduced in the group undergoing sublingual allergen administration, thus proving the clinical efficacy of this treatment. There has not been, however, a significant reduction of specific IgE, nor a significant increase of specific IgG4 towards grasses, in the treated group, monitored before and at the end of the immunotherapy.

Absorption↗

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↗

PubMed1982

[Pharmacokinetics and pharmacodynamics of verapamil in healthy volunteers after single oral and sublingual administration].

5-[3,4-Dimethoxyphenethyl)-methylamino]-2-(3,4-dimethoxyphenyl)-2- isopropylvaleronitril (verapamil, Isoptin) was administered p.o. (80 mg) and via the sublingual route (20 mg as the hydrochloride) in 6 healthy volunteers. After p.o. administration the mean peak serum concentration of 125.6 ng/ml was attained on average 80 min later. The half-life for the distribution phase (t1/2a) was 0.95 h and for the elimination phase (t1/2 beta) 6.08 h. After sublingual administration the mean peak serum concentration of verapamil was 26 ng/ml attained on average after 71.7 min. The mean t1/2a was 0.73 h and the mean T1/2 beta 4.39 h. There was an 18.4 min delay after oral administration and 0.8 min delay after sublingual administration before verapamil was detected in the serum. The relative bioavailability of verapamil sublingually was 2.7 (p.o. = 1.0). There were close correlations between the verapamil concentration in serum and the prolongation of the PQ-interval (0.725 sublingually; 0.853 p.o.). Approximately three times higher concentrations of verapamil were required when given by the oral route to produce the same prolongation of the PQ-interval obtained with sublingual administration. The variability of several important pharmacokinetic parameters of verapamil was reduced by sublingual application in comparison to the oral route. The coefficient of variation for the peak concentration, time to peak and t1/2 beta were 49.7%, 25.0% and 26.4%, respectively, after sublingual administration in comparison to 120.6%, 54.7% and 68.9%, respectively, when given p.o.

Administration, Oral↗

PubMedDate not supplied

Sublingual administration of micronized estradiol and progesterone, with and without micronized testosterone: effect on biochemical markers of bone metabolism and bone mineral density.

OBJECTIVES: The purpose of this investigation was to evaluate the relative efficacy of the sublingual administration of micronized estradiol (E2), progesterone (P4), and testosterone (T) on bone mineral density and biochemical markers of bone metabolism. DESIGN: In this double-blind, prospective study, postmenopausal women were randomly assigned to one of four treatment groups: hysterectomized women were assigned to either 1) micronized E2 (0.5 mg) or 2) micronized E2 (0.5 mg) + micronized T (1.25 mg). Women with intact uteri were assigned to either 3) micronized E2 (0.5 mg) + micronized P4 (100 mg) or 4) micronized E2 (0.5 mg) + micronized P4 (100 mcg) + micronized T (1.25 mg). For the purpose of this study, the four treatment groups were combined into two groups for all comparisons. The E2 and E2+P4 groups were combined into the HRT alone group (n=30), and the E2+T and E2+P4+T groups were combined into the HRT + T group (n=27). Hormones were administered sublingually as a single tablet twice a day for 12 months. Bone mineral density was measured in the anterior-posterior lumbar spine and total left hip via dual energy x-ray absorptiometry. Bone metabolism was assessed via serum bone-specific alkaline phosphatase and urinary deoxypyridinoline and cross-linked N-telopeptide of type I collagen, both normalized to creatinine. Data were analyzed via a repeated measures analysis of variance and a Student's t test (alpha=0.05). RESULTS: The subjects were of similar age (54.0 +/- 0.8 years), height (64.0 +/- 0.3 in), weight (157.6 +/- 4.2 lb), and had similar baseline follicle-stimulating hormone (66.4 +/- 3.2 mIU/L), E2 (26.4 +/- 1.5 pg/ml), P4 (0.3 +/- 0.1 ng/ml), total T (19.0 +/- 1.5 ng/dL), and bioavailable T (3.7 +/- 0.3 ng/dL) levels. During therapy, serum levels increased (p < 0.05) for each hormone. Bone mineral density and bone markers at baseline were similar for each treatment group. Bone-specific alkaline phosphatase decreased (p < 0.05) by -14.3 +/- 4.1% in the HRT alone group and by -8.2 +/- 4.6% in the HRT + T group. Deoxypyridinoline levels decreased significantly in the HRT alone and HRT + T groups, - 14.4 +/- 6.8% and -26.9 +/- 7.6%, respectively. Significant reductions (p < 0.05) in cross-linked N-telopeptide of type I collagen were also observed in both groups, -24.4 +/- 6.5% and -39.5 +/- 8.6%, respectively. Bone mineral density in the lumbar spine increased (p < 0.05) by +2.2 +/- 0.5% the HRT alone group and by + 1.8 +/- 0.6% in the HRT + T group. Total hip bone mineral density was maintained in the HRT alone group (+0.4 +/- 0.4%) and increased (p < 0.05) in the HRT + T group (+ 1.8 +/- 0.5%). CONCLUSIONS: Sublingual micronized HRT favorably decreases serum and urine markers of bone metabolism, prevents bone loss, and results in a slight increase in spine and hip bone mineral density. Although the addition of testosterone to HRT for 1 year did not result in added benefit to the spine bone mineral density, it did result in a significant increase in hip bone mineral density. Longer duration of therapy may have further improved these outcomes.

Administration, Sublingual↗

PubMed1988

Plasma concentrations following oral and sublingual administration of lorazepam.

Lorazepam 2.5 mg was given as premedication either orally or sublingually to 20 patients undergoing minor gynaecological surgery. Plasma concentrations were followed for up to 8 h after administration. The time for the maximal plasma concentration (tmax) occurred 40 min after oral administration and 60 min after sublingual administration. No significant differences were found between the two treatments at any time. The plasma concentration after 8 h was high compared to the maximal plasma concentration.

Administration, Oral↗

PubMed1998

Pain scoring--a method for assessing acute antianginal therapy comparison of the response to acute sublingual administration of an isosorbide dinitrate tablet, isosorbide dinitrate spray and nitroglycerin spray in unstable angina.

It is difficult to assess acute therapeutic intervention therapy, particularly in patients with unstable angina. Our aim was to evaluate the feasibility of a pain-scoring method and to compare the response to sublingual administration of an isosorbide dinitrate (ISDN) tablet, ISDN spray or nitroglycerin (NTG) spray. Pain scoring was assessed by the subjective grading of the patients' pain severity from 1 to 10. We studied 205 patients (mean age 66 +/- 13 years). Pain attenuation, defined as at least 50% reduction in pain intensity, occurred in the ISDN tablet, ISDN spray and NTG spray groups after 360 +/- 290, 318 +/- 289 and 233 +/- 271 s, respectively (p = 0.0005). In conclusion, pain scoring is a feasible and useful clinical method to assess antianginal therapy in unstable angina patients. Sublingual nitrate sprays, particularly NTG, seem to alleviate anginal pain faster than ISDN tablets in this patient population.

Administration, Inhalation↗

PubMed1983

[Relations between ventricle function, myocardial oxygen consumption and coronary circulation following sublingual administration of nitroglycerin].

The relationships between ventricular function, coronary blood flow, and myocardial oxygen consumption after sublingual administration of 1.6 mg nitroglycerin (TNG) were investigated in 12 patients. Left ventricular volumes, determined from cineventriculograms (enddiastolic volume index and endsystolic volume index), decreased (p less than 0.005) after TNG, as did left ventricular peak pressure (p less than 0.01), left ventricular enddiastolic pressure (p less than 0.005), mean aortic pressure (p less than 0.005), and mean pulmonary artery pressure (p less than 0.001). Due to the decrease in enddiastolic volume and the insignificant change in stroke volume, ejection fraction increased (p less than 0.05). Heart rate did not change significantly. In spite of an increase in the vessel diameter (13%, p less than 0.005), systolic and diastolic coronary blood flow, measured by means of a photodensitometric technique, decreased insignificantly by an average of approx. 15%. Similarly the change in myocardial oxygen consumption, calculated according to Bretschneider, decreased insignificantly by an average of approx. 10%. The correlation of changes in coronary blood flow and myocardial oxygen consumption was evaluated statistically by the use of the 2 X 2 contingency table in conjunction with the chi 2 McNamar test: patients with a decrease in myocardial oxygen consumption also showed a decrease in coronary blood flow (p less than 0.05). This implies that coronary blood flow is determined by myocardial oxygen consumption, which is altered by the systemic effects of TNG.

Adult↗

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↗

PubMed1998

Pharmacokinetics and pharmacodynamics of propranolol in hypertensive patients after sublingual administration: systemic availability.

The bioavailability of propranolol depends on the degree of liver metabolism. Orally but not intravenously administered propranolol is heavily metabolized. In the present study we assessed the pharmacokinetics and pharmacodynamics of sublingual propranolol. Fourteen severely hypertensive patients (diastolic blood pressure (DBP) > or = 115 mmHg), aged 40 to 66 years, were randomly chosen to receive a single dose of 40 mg propranolol hydrochloride by sublingual or peroral administration. Systolic (SBP) and diastolic (DBP) blood pressures, heart rate (HR) for pharmacodynamics and blood samples for noncompartmental pharmacokinetics were obtained at baseline and at 10, 20, 30, 60 and 120 min after the single dose. Significant reductions in BP and HR were obtained, but differences in these parameters were not observed when sublingual and peroral administrations were compared as follows: SBP (17 vs 18%, P = NS), DBP (14 vs 8%, P = NS) and HR (22 vs 28%, P = NS), respectively. The pharmacokinetic parameters obtained after sublingual or peroral drug administration were: peak plasma concentration (CMAX): 147 +/- 72 vs 41 +/- 12 ng/ml, P < 0.05; time to reach CMAX (TMAX): 34 +/- 18 vs 52 +/- 11 min, P < 0.05; biological half-life (t1/2b): 0.91 +/- 0.54 vs 2.41 +/- 1.16 h, P < 0.05; area under the curve (AUCT): 245 +/- 134 vs 79 +/- 54 ng h-1 ml-1, P < 0.05; total body clearance (CLT/F): 44 +/- 23 vs 26 +/- 12 ml min-1 kg-1, P = NS. Systemic availability measured by the AUCT ratio indicates that extension of bioavailability was increased 3 times by the sublingual route. Mouth paresthesia was the main adverse effect observed after sublingual administration. Sublingual propranolol administration showed a better pharmacokinetic profile and this route of administration may be an alternative for intravenous or oral administration.

Administration, Sublingual↗

PubMed1999

Increased bioavailability of clomipramine after sublingual administration in rats.

This study examined the absorption and disposition of clomipramine in rats after sublingual (5 and 50 mg/kg), oral (50 mg/kg), and iv (5 mg/kg) administration. The mean oral bioavailability of clomipramine was 24.8% and 29.7%, respectively, in conscious rats and in rats anesthetized with ketamine/xylazine (30/3 mg/kg). When given sublingually in isotonic saline at a dose of 50 mg/kg, clomipramine was rapidly absorbed, and the mean absolute bioavailability (36.2%) was increased over oral dosing. The mean AUC values of clomipramine were 2258 +/- 1762 ng.h/mL and 1891 +/- 867 ng.h/mL after oral administration to conscious and anesthetized rats, respectively, and 3303 +/- 1576 ng.h/mL after sublingual administration to anesthetized rats. Sublingual administration (5 mg/kg doses) of clomipramine formulated with a permeation enhancer, 2-hydroxypropyl beta-cyclodextrin, further increased the sublingual bioavailability to 57.1%. The sublingual route may be an alternative route of administration of clomipramine, providing enhanced bioavailability.

2-Hydroxypropyl-beta-cyclodextrin↗

PubMed1981

Relation of time course of plasma nitroglycerin levels to echocardiographic, arterial pressure and heart rate changes after sublingual administration of nitroglycerin.

Despite the widespread use of nitroglycerin, a relation between plasma nitroglycerin concentrations and the associated cardiovascular effects has not been well established. It was hypothesized that nitroglycerin levels may help predict the hemodynamic responses. With use of a recently developed nitroglycerin assay technique, the relation between the time course of plasma nitroglycerin levels and echocardiographic changes after sublingual administration of 0.6 mg of the drug was evaluated in 12 normal volunteers. Mean plasma nitroglycerin levels were maximal at 2 (1.1 +/- 0.3 ng/ml) and 5 (1.4 +/- 0.6 ng/ml) minutes, when the changes in mean heart rate (+17 +/- 7 and +12 +/- 3 min-1) and decreases in echocardiographic left ventricular diastolic (-4.2 +/- 0.8 mm at 5 minutes) and systolic (-3.1 +/- 0.6 mm at 5 minutes) dimensions were also maximal. Parallel changes were noted in left atrial dimension, ventricular velocity of circumferential fiber shortening and systolic blood pressure, but not in diastolic blood pressure. These findings demonstrate the existence of a close relation between plasma nitroglycerin levels and variables that reflect the known responses to this drug.

Administration, Oral↗