LVI Absorption from Nasal Mucous Membrane: Systemic Effect of Hyoscine following Intranasal Administration

Tonndorf, Juergen; Hyde, Reed W.; Chinn, Herman I.; Lett, James E.

doi:10.1177/000348945306200302

Cited by 21 publications

(8 citation statements)

References 4 publications

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“…Our results agree with those of Tonndorf et al, 9 who found that absorption of IN scopolamine fell between that of oral and subcutaneous administration. Our results agree with those of Tonndorf et al, 9 who found that absorption of IN scopolamine fell between that of oral and subcutaneous administration.…”

Section: Discussionsupporting

confidence: 93%

Bioavailability of Intranasal Scopolamine in Normal Subjects**Portions of this work were presented at the 92nd annual meeting of the American Society for Clinical Pharmacology and Therapeutics, March 13, 1991, San Antonio, TX.

Putcha

Tietze

Bourne

et al. 1996

Journal of Pharmaceutical Sciences

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The bioavailability of scopolamine in three dosage forms was compared in 12 healthy nonsmoking male volunteers. Subjects received 0.4-mg doses of scopolamine bromide in intravenous (i.v.), intranasal (i.n.), or oral (p.o.) dosage forms on three occasions, with at least 2 weeks separating the doses. Scopolamine concentrations in plasma were determined with a combined reverse-phase liquid chromatographic-radioreceptor binding assay. Saliva volume and flow rate and percent suppression of control flow rate were determined from each sample. Absorption after i.n. and po scopolamine administration was rapid; plasma concentrations [1680 (i.n.) and 164 pg/mL (p.o.)] peaked within 1 h of dosing [0.37 (i.n.) and 0.78 h (p.o.)], respectively. i.n. and i.v. scopolamine suppressed salivary flow rate to similar extents (95% and 99.7%), respectively. Times to reach maximum effect were 1.05 and 0.27 h after i.n. and i.v. dosage, respectively. Absolute intranasal bioavailability, calculated from the area under the drug concentration vs time curve, was found to be significantly greater than that of p.o. scopolamine (83% vs 3.7%, p < 0.05). The i.n. route may provide a noninvasive, reliable, fast, and effective route for administering scopolamine.

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Section: Discussionsupporting

confidence: 93%

Bioavailability of Intranasal Scopolamine in Normal Subjects**Portions of this work were presented at the 92nd annual meeting of the American Society for Clinical Pharmacology and Therapeutics, March 13, 1991, San Antonio, TX.

Putcha

Tietze

Bourne

et al. 1996

Journal of Pharmaceutical Sciences

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“…A search of the literature reveals very little accurate or detailed information about the measurable effects of (-)-hyoscine after parenteral administration at various dose levels and related to time after dose. Tonndorf, Hyde, Chinn & Lett (1953), however, examined the effects on salivation of 0.65 mg of the hydrobromide given subcutaneously for up to 2 hr after dose, and reported a time course of action similar to that observed after the 0.4 mg dose given in the present experiment. These effects may be compared with those seen when the drug is given by mouth, when, as might be expected, the rate of absorption is somewhat slower and a peak effect does not appear until 2-3 hr after dose and is followed by a rapid decline to baseline levels (Brand et al, 1968).…”

Section: Discussionsupporting

confidence: 66%

The time course of action of (—)‐hyoscine after intramuscular injection

Brand

1969

British J Pharmacology

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Although (–)‐hyoscine has been in clinical use for many years, there is little detailed information concerning the speed of absorption or duration of action of the drug after single intramuscular doses. The time course of action of the drug was therefore examined using biological methods, and measurements were made of saliva flow, pulse rate, pupil diameter and mental alertness for up to 8 hr after doses of 0.4, 0.2, 0.1 and 0.05 mg of the hydrobromide. These techniques gave comparable results and peak activity was achieved at 1–2 hr after dose and followed by a gradual decline over the 8 hr period. The results are compared with those of earlier experiments of a similar kind, and discussed in relation to their bearing on both therapeutics and experimental design.

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“…Understanding the limitations of oral and injected medications in an operational environment, early military research involving scopolamine explored intranasal instillation in the form of drops and spray (Chinn, et al, 1955;Chinn, Milch & Dugi, 1953;Tonndorf, Hyde, Chinn & Lett, 1953). The study conducted by Tonndorf, et al, (1953) compared subcutaneous, oral, and intranasal scopolamine and found the absorption of intranasal scopolamine to be comparable to subcutaneous in rate and "completeness."…”

Section: Early Intranasal Scopolamine Researchmentioning

confidence: 99%

“…The study conducted by Tonndorf, et al, (1953) compared subcutaneous, oral, and intranasal scopolamine and found the absorption of intranasal scopolamine to be comparable to subcutaneous in rate and "completeness." 1955) and Hyde et al, (1953), found analogous absorption results for intranasal scopolamine, however, they also reported a decrease in dose required to reach therapeutic levels, leading to a significant reduction in side effects.…”

Section: Early Intranasal Scopolamine Researchmentioning

confidence: 99%

A Comparison of Intranasal and Oral Scopolamine for Motion Sickness Prevention in Military Personnel

Simmons¹,

Phillips²,

Lojewski³

et al. 2008

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Executive SummaryMotion sickness in astronauts, aviators, and military personnel often leads to decrements in operational performance. The anti-motion sickness medication, scopolamine, is effective; however, oral and transdermal administrations have proven problematic due to slow absorption, low bioavailability, unpredictable therapeutic effect, potential medication loss due to emesis, and side effects. Although efficacy and side-effect characteristics of intranasally administered scopolamine have not been established, results from preliminary studies indicate intranasal scopolamine has faster absorption, higher bioavailability, and a more reliable therapeutic index than equivalent oral or transdermal forms. The purpose of this study was to compare the efficacy, side-effect profile, and pharmacotherapeutics of a 0.4 mg dose of intranasal scopolamine gel and a 0.8 mg dose of oral scopolamine. It was hypothesized that intranasal delivery of scopolamine would rapidly achieve therapeutic concentrations at lower doses compared to oral scopolamine while minimizing medication-induced performance impairment. To test these hypotheses, 54 aviation candidates, 50 male and 4 female, were recruited and randomized to one of three treatment groups [intranasal scopolamine gel (IN SCOP); oral scopolamine (PO SCOP); or placebo] and then exposed to passive Coriolis cross-coupling for 40 minutes or until moderate nausea was reported. Medication efficacy was determined by number of head movements tolerated among groups and pharmacotherapeutics for IN SCOP and PO SCOP were determined by salivary assay. Side-effect profiles for all groups were derived from performance on a cognitive battery, measurements of near-focus visual accommodation (VA), scores on the Karolinska Sleepiness Scale (KSS) and motion sickness questionnaires. Analysis detected no significant differences in the number of head movements tolerated among groups, p > 0.05. Pharmacotherapeutic data show increased scopolamine absorption and decreased time to reach maximum salivary concentration with intranasal administration (T max = 1.463 ± 0.98 hr, C max = 54.857± 103.739 ng/mL, AUC = 51.732 ± 93.802 ng*h/mL). No treatment effects were detected over time on the cognitive battery, VA, or KSS, p > 0.05. An ANOVA revealed a significant decrease in heart rate over time for IN SCOP and PO SCOP versus placebo at several time points post-dose, while no clinically significant differences were found for systolic or diastolic blood pressures. A negative linear relationship was found between Motion Sickness Susceptibility Questionnaire (MSSQ) scores and number of head movements (r = -.24, p < .05). The present study lacked sufficient power to draw definitive conclusions regarding efficacy or to make adequate comparisons between the two medications, F (2, 50) = 0.743, p > .05, observed power = 17 %, however; medication absorption was significantly greater for IN SCOP at onehalf the dose (0.4 mg v. 0.8 mg) with no side effects or detrimental impact to performance. 3 Introduction Impac...

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LVI Absorption from Nasal Mucous Membrane: Systemic Effect of Hyoscine following Intranasal Administration

Cited by 21 publications

References 4 publications

Bioavailability of Intranasal Scopolamine in Normal Subjects**Portions of this work were presented at the 92nd annual meeting of the American Society for Clinical Pharmacology and Therapeutics, March 13, 1991, San Antonio, TX.

Bioavailability of Intranasal Scopolamine in Normal Subjects**Portions of this work were presented at the 92nd annual meeting of the American Society for Clinical Pharmacology and Therapeutics, March 13, 1991, San Antonio, TX.

The time course of action of (—)‐hyoscine after intramuscular injection

A Comparison of Intranasal and Oral Scopolamine for Motion Sickness Prevention in Military Personnel

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