The Experts below are selected from a list of 6309 Experts worldwide ranked by ideXlab platform
Albert J Azzaro - One of the best experts on this subject based on the ideXlab platform.
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Pharmacokinetics and absolute bioavailability of Selegiline following treatment of healthy subjects with the Selegiline transdermal system (6 mg/24 h): a comparison with oral Selegiline capsules.
Journal of clinical pharmacology, 2007Co-Authors: Albert J Azzaro, John Ziemniak, Eva M Kemper, Bryan J Campbell, Chad M VandenbergAbstract:The Selegiline transdermal system is a monoamine oxidase inhibitor that was recently approved by the US Food and Drug Administration for the treatment of major depressive disorder. The current study was conducted during the Selegiline transdermal system development program to characterize the single-dose pharmacokinetics and absolute bioavailability of Selegiline administered by the 6-mg/24-h Selegiline transdermal system in healthy volunteers. Selegiline transdermal system results were compared with those obtained after a single 10-mg oral dose of Selegiline HCl. The Selegiline pharmacokinetics differed greatly between the 2 routes of administration. Transdermal Selegiline administration reduced metabolism and produced a high, sustained plasma Selegiline concentration over the dosing period, with an absolute bioavailability of 73%. By contrast, oral dosing produced a sharp plasma Selegiline peak that occurred within 1 hour and declined rapidly, with an absolute bioavailability of 4%. The data provide the basis for therapeutic advantages of the Selegiline transdermal system in administering antidepressant doses of Selegiline.
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evaluation of the potential for pharmacodynamic and pharmacokinetic drug interactions between Selegiline transdermal system and two sympathomimetic agents pseudoephedrine and phenylpropanolamine in healthy volunteers
The Journal of Clinical Pharmacology, 2007Co-Authors: Albert J Azzaro, Chad M Vandenberg, John Ziemniak, Eva M Kemper, Lawrence F Blob, Bryan J CampbellAbstract:Selegiline transdermal system is a recently approved monoamine oxidase inhibitor antidepressant. Medications that inhibit monoamine oxidase type A can augment the pressor effects of sympathomimetic amines, increasing the potential for hypertensive crisis. This study examined the potential for drug-drug interactions during treatment with Selegiline transdermal system and pseudoephedrine or phenylpropanolamine. Two studies were conducted with 25 healthy volunteers to assess changes in blood pressure and heart rate during administration of pseudoephedrine or phenylpropanolamine alone or together with Selegiline transdermal system. No significant differences in mean maximum changes in vital signs occurred with pseudoephedrine. No significant differences were found in mean maximum changes in systolic heart rate with phenylpropanolamine; however, 4 of 12 subjects each experienced 1 isolated protocol-defined minimal pressor response without concurrent adverse effects (1 with phenylpropanolamine alone; 3 with phenylpropanolamine + Selegiline transdermal system). Pharmacokinetic parameters obtained following Selegiline transdermal system and pseudoephedrine or phenylpropanolamine were unremarkable. The results suggest that Selegiline transdermal system 6 mg/24 h does not significantly alter the pharmacodynamics or pharmacokinetics of either pseudoephedrine or phenylpropanolamine when administered to healthy volunteers; however, it is prudent to avoid coadministration of Selegiline transdermal system and sympathomimetics.
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tyramine pressor sensitivity during treatment with the Selegiline transdermal system 6 mg 24 h in healthy subjects
The Journal of Clinical Pharmacology, 2006Co-Authors: Albert J Azzaro, Chad M Vandenberg, Eva M Kemper, Lawrence F Blob, Melvin Sharoky, Dan A Oren, Bryan J CampbellAbstract:The oral tyramine pressor test was administered to healthy males during treatment with a Selegiline transdermal system (STS; 6 mg/24 h). The tyramine sensitivity factor (TSF) was calculated from the ratio of baseline and on-treatment tyramine pressor doses. The tyramine sensitivity factor value following 9 days of treatment with the Selegiline transdermal system was 1.85 ± 0.10. Extended treatment, 33 days, produced a small, clinically nonmeaningful increase in this value. The tyramine sensitivity factor for the Selegiline transdermal system was similar to that following treatment with 10 mg/d of oral Selegiline capsules but more than 20 times less than observed during tranylcypromine treatment. A larger increase in the tyramine sensitivity factor was observed following extended Selegiline transdermal system treatment at a higher dose (12 mg/24 h), which was significantly decreased following coadministration of tyramine capsules with a meal. These results suggest a wide tyramine safety margin for the Selegiline transdermal system and provide evidence that the 6-mg/24-h Selegiline transdermal system can be administered safely without dietary tyramine restrictions.
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daily transdermal administration of Selegiline to guinea pigs preferentially inhibits monoamine oxidase activity in brain when compared with intestinal and hepatic tissues
Journal of Pharmacy and Pharmacology, 2003Co-Authors: Michael G Mawhinney, Dennis Cole, Albert J AzzaroAbstract:Selegiline has been formulated in an acrylic polymer adhesive mixture to be employed as a constant release topical patch for daily transdermal administration. Application of this Selegiline transdermal system (STS) to guinea-pigs resulted in an average delivery of 1.185 mg Selegiline/cm(2) patch/24 h. STS dose-response curves were generated by altering patch size (cm(2)). A transdermal dose range was identified which inhibited guinea-pig brain monoamine oxidase-B (MAO-B) by greater than 95% yet provided for a dose-dependent inhibition of monoamine oxidase-A (MAO-A) activity. The ID50 for inhibition of MAO-A activity in response to a 21-day daily regimen with transdermal Selegiline was approximately 7.5-fold lower for cortical and striatal brain regions compared with that obtained for duodenum; hepatic MAO-A was unaffected following the same dosing regimen. By contrast, orally administered Selegiline inhibited brain and duodenal MAO-A to the same extent, and generated a shallower dose-inhibition curve for brain MAO-A inhibition. In addition, transdermal delivery was approximately 6-8-times more potent than oral Selegiline for the inhibition of brain MAO-A activity. It is concluded that daily transdermal Selegiline administration may provide therapeutic advantages over oral treatment, based on its preferential, dose-dependent inhibition of brain vs peripheral MAO-A activity.
Bryan J Campbell - One of the best experts on this subject based on the ideXlab platform.
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Pharmacokinetics and absolute bioavailability of Selegiline following treatment of healthy subjects with the Selegiline transdermal system (6 mg/24 h): a comparison with oral Selegiline capsules.
Journal of clinical pharmacology, 2007Co-Authors: Albert J Azzaro, John Ziemniak, Eva M Kemper, Bryan J Campbell, Chad M VandenbergAbstract:The Selegiline transdermal system is a monoamine oxidase inhibitor that was recently approved by the US Food and Drug Administration for the treatment of major depressive disorder. The current study was conducted during the Selegiline transdermal system development program to characterize the single-dose pharmacokinetics and absolute bioavailability of Selegiline administered by the 6-mg/24-h Selegiline transdermal system in healthy volunteers. Selegiline transdermal system results were compared with those obtained after a single 10-mg oral dose of Selegiline HCl. The Selegiline pharmacokinetics differed greatly between the 2 routes of administration. Transdermal Selegiline administration reduced metabolism and produced a high, sustained plasma Selegiline concentration over the dosing period, with an absolute bioavailability of 73%. By contrast, oral dosing produced a sharp plasma Selegiline peak that occurred within 1 hour and declined rapidly, with an absolute bioavailability of 4%. The data provide the basis for therapeutic advantages of the Selegiline transdermal system in administering antidepressant doses of Selegiline.
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evaluation of the potential for pharmacodynamic and pharmacokinetic drug interactions between Selegiline transdermal system and two sympathomimetic agents pseudoephedrine and phenylpropanolamine in healthy volunteers
The Journal of Clinical Pharmacology, 2007Co-Authors: Albert J Azzaro, Chad M Vandenberg, John Ziemniak, Eva M Kemper, Lawrence F Blob, Bryan J CampbellAbstract:Selegiline transdermal system is a recently approved monoamine oxidase inhibitor antidepressant. Medications that inhibit monoamine oxidase type A can augment the pressor effects of sympathomimetic amines, increasing the potential for hypertensive crisis. This study examined the potential for drug-drug interactions during treatment with Selegiline transdermal system and pseudoephedrine or phenylpropanolamine. Two studies were conducted with 25 healthy volunteers to assess changes in blood pressure and heart rate during administration of pseudoephedrine or phenylpropanolamine alone or together with Selegiline transdermal system. No significant differences in mean maximum changes in vital signs occurred with pseudoephedrine. No significant differences were found in mean maximum changes in systolic heart rate with phenylpropanolamine; however, 4 of 12 subjects each experienced 1 isolated protocol-defined minimal pressor response without concurrent adverse effects (1 with phenylpropanolamine alone; 3 with phenylpropanolamine + Selegiline transdermal system). Pharmacokinetic parameters obtained following Selegiline transdermal system and pseudoephedrine or phenylpropanolamine were unremarkable. The results suggest that Selegiline transdermal system 6 mg/24 h does not significantly alter the pharmacodynamics or pharmacokinetics of either pseudoephedrine or phenylpropanolamine when administered to healthy volunteers; however, it is prudent to avoid coadministration of Selegiline transdermal system and sympathomimetics.
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tyramine pressor sensitivity during treatment with the Selegiline transdermal system 6 mg 24 h in healthy subjects
The Journal of Clinical Pharmacology, 2006Co-Authors: Albert J Azzaro, Chad M Vandenberg, Eva M Kemper, Lawrence F Blob, Melvin Sharoky, Dan A Oren, Bryan J CampbellAbstract:The oral tyramine pressor test was administered to healthy males during treatment with a Selegiline transdermal system (STS; 6 mg/24 h). The tyramine sensitivity factor (TSF) was calculated from the ratio of baseline and on-treatment tyramine pressor doses. The tyramine sensitivity factor value following 9 days of treatment with the Selegiline transdermal system was 1.85 ± 0.10. Extended treatment, 33 days, produced a small, clinically nonmeaningful increase in this value. The tyramine sensitivity factor for the Selegiline transdermal system was similar to that following treatment with 10 mg/d of oral Selegiline capsules but more than 20 times less than observed during tranylcypromine treatment. A larger increase in the tyramine sensitivity factor was observed following extended Selegiline transdermal system treatment at a higher dose (12 mg/24 h), which was significantly decreased following coadministration of tyramine capsules with a meal. These results suggest a wide tyramine safety margin for the Selegiline transdermal system and provide evidence that the 6-mg/24-h Selegiline transdermal system can be administered safely without dietary tyramine restrictions.
Chad M Vandenberg - One of the best experts on this subject based on the ideXlab platform.
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Pharmacokinetics and absolute bioavailability of Selegiline following treatment of healthy subjects with the Selegiline transdermal system (6 mg/24 h): a comparison with oral Selegiline capsules.
Journal of clinical pharmacology, 2007Co-Authors: Albert J Azzaro, John Ziemniak, Eva M Kemper, Bryan J Campbell, Chad M VandenbergAbstract:The Selegiline transdermal system is a monoamine oxidase inhibitor that was recently approved by the US Food and Drug Administration for the treatment of major depressive disorder. The current study was conducted during the Selegiline transdermal system development program to characterize the single-dose pharmacokinetics and absolute bioavailability of Selegiline administered by the 6-mg/24-h Selegiline transdermal system in healthy volunteers. Selegiline transdermal system results were compared with those obtained after a single 10-mg oral dose of Selegiline HCl. The Selegiline pharmacokinetics differed greatly between the 2 routes of administration. Transdermal Selegiline administration reduced metabolism and produced a high, sustained plasma Selegiline concentration over the dosing period, with an absolute bioavailability of 73%. By contrast, oral dosing produced a sharp plasma Selegiline peak that occurred within 1 hour and declined rapidly, with an absolute bioavailability of 4%. The data provide the basis for therapeutic advantages of the Selegiline transdermal system in administering antidepressant doses of Selegiline.
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evaluation of the potential for pharmacodynamic and pharmacokinetic drug interactions between Selegiline transdermal system and two sympathomimetic agents pseudoephedrine and phenylpropanolamine in healthy volunteers
The Journal of Clinical Pharmacology, 2007Co-Authors: Albert J Azzaro, Chad M Vandenberg, John Ziemniak, Eva M Kemper, Lawrence F Blob, Bryan J CampbellAbstract:Selegiline transdermal system is a recently approved monoamine oxidase inhibitor antidepressant. Medications that inhibit monoamine oxidase type A can augment the pressor effects of sympathomimetic amines, increasing the potential for hypertensive crisis. This study examined the potential for drug-drug interactions during treatment with Selegiline transdermal system and pseudoephedrine or phenylpropanolamine. Two studies were conducted with 25 healthy volunteers to assess changes in blood pressure and heart rate during administration of pseudoephedrine or phenylpropanolamine alone or together with Selegiline transdermal system. No significant differences in mean maximum changes in vital signs occurred with pseudoephedrine. No significant differences were found in mean maximum changes in systolic heart rate with phenylpropanolamine; however, 4 of 12 subjects each experienced 1 isolated protocol-defined minimal pressor response without concurrent adverse effects (1 with phenylpropanolamine alone; 3 with phenylpropanolamine + Selegiline transdermal system). Pharmacokinetic parameters obtained following Selegiline transdermal system and pseudoephedrine or phenylpropanolamine were unremarkable. The results suggest that Selegiline transdermal system 6 mg/24 h does not significantly alter the pharmacodynamics or pharmacokinetics of either pseudoephedrine or phenylpropanolamine when administered to healthy volunteers; however, it is prudent to avoid coadministration of Selegiline transdermal system and sympathomimetics.
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tyramine pressor sensitivity during treatment with the Selegiline transdermal system 6 mg 24 h in healthy subjects
The Journal of Clinical Pharmacology, 2006Co-Authors: Albert J Azzaro, Chad M Vandenberg, Eva M Kemper, Lawrence F Blob, Melvin Sharoky, Dan A Oren, Bryan J CampbellAbstract:The oral tyramine pressor test was administered to healthy males during treatment with a Selegiline transdermal system (STS; 6 mg/24 h). The tyramine sensitivity factor (TSF) was calculated from the ratio of baseline and on-treatment tyramine pressor doses. The tyramine sensitivity factor value following 9 days of treatment with the Selegiline transdermal system was 1.85 ± 0.10. Extended treatment, 33 days, produced a small, clinically nonmeaningful increase in this value. The tyramine sensitivity factor for the Selegiline transdermal system was similar to that following treatment with 10 mg/d of oral Selegiline capsules but more than 20 times less than observed during tranylcypromine treatment. A larger increase in the tyramine sensitivity factor was observed following extended Selegiline transdermal system treatment at a higher dose (12 mg/24 h), which was significantly decreased following coadministration of tyramine capsules with a meal. These results suggest a wide tyramine safety margin for the Selegiline transdermal system and provide evidence that the 6-mg/24-h Selegiline transdermal system can be administered safely without dietary tyramine restrictions.
Eva M Kemper - One of the best experts on this subject based on the ideXlab platform.
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Pharmacokinetics and absolute bioavailability of Selegiline following treatment of healthy subjects with the Selegiline transdermal system (6 mg/24 h): a comparison with oral Selegiline capsules.
Journal of clinical pharmacology, 2007Co-Authors: Albert J Azzaro, John Ziemniak, Eva M Kemper, Bryan J Campbell, Chad M VandenbergAbstract:The Selegiline transdermal system is a monoamine oxidase inhibitor that was recently approved by the US Food and Drug Administration for the treatment of major depressive disorder. The current study was conducted during the Selegiline transdermal system development program to characterize the single-dose pharmacokinetics and absolute bioavailability of Selegiline administered by the 6-mg/24-h Selegiline transdermal system in healthy volunteers. Selegiline transdermal system results were compared with those obtained after a single 10-mg oral dose of Selegiline HCl. The Selegiline pharmacokinetics differed greatly between the 2 routes of administration. Transdermal Selegiline administration reduced metabolism and produced a high, sustained plasma Selegiline concentration over the dosing period, with an absolute bioavailability of 73%. By contrast, oral dosing produced a sharp plasma Selegiline peak that occurred within 1 hour and declined rapidly, with an absolute bioavailability of 4%. The data provide the basis for therapeutic advantages of the Selegiline transdermal system in administering antidepressant doses of Selegiline.
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evaluation of the potential for pharmacodynamic and pharmacokinetic drug interactions between Selegiline transdermal system and two sympathomimetic agents pseudoephedrine and phenylpropanolamine in healthy volunteers
The Journal of Clinical Pharmacology, 2007Co-Authors: Albert J Azzaro, Chad M Vandenberg, John Ziemniak, Eva M Kemper, Lawrence F Blob, Bryan J CampbellAbstract:Selegiline transdermal system is a recently approved monoamine oxidase inhibitor antidepressant. Medications that inhibit monoamine oxidase type A can augment the pressor effects of sympathomimetic amines, increasing the potential for hypertensive crisis. This study examined the potential for drug-drug interactions during treatment with Selegiline transdermal system and pseudoephedrine or phenylpropanolamine. Two studies were conducted with 25 healthy volunteers to assess changes in blood pressure and heart rate during administration of pseudoephedrine or phenylpropanolamine alone or together with Selegiline transdermal system. No significant differences in mean maximum changes in vital signs occurred with pseudoephedrine. No significant differences were found in mean maximum changes in systolic heart rate with phenylpropanolamine; however, 4 of 12 subjects each experienced 1 isolated protocol-defined minimal pressor response without concurrent adverse effects (1 with phenylpropanolamine alone; 3 with phenylpropanolamine + Selegiline transdermal system). Pharmacokinetic parameters obtained following Selegiline transdermal system and pseudoephedrine or phenylpropanolamine were unremarkable. The results suggest that Selegiline transdermal system 6 mg/24 h does not significantly alter the pharmacodynamics or pharmacokinetics of either pseudoephedrine or phenylpropanolamine when administered to healthy volunteers; however, it is prudent to avoid coadministration of Selegiline transdermal system and sympathomimetics.
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tyramine pressor sensitivity during treatment with the Selegiline transdermal system 6 mg 24 h in healthy subjects
The Journal of Clinical Pharmacology, 2006Co-Authors: Albert J Azzaro, Chad M Vandenberg, Eva M Kemper, Lawrence F Blob, Melvin Sharoky, Dan A Oren, Bryan J CampbellAbstract:The oral tyramine pressor test was administered to healthy males during treatment with a Selegiline transdermal system (STS; 6 mg/24 h). The tyramine sensitivity factor (TSF) was calculated from the ratio of baseline and on-treatment tyramine pressor doses. The tyramine sensitivity factor value following 9 days of treatment with the Selegiline transdermal system was 1.85 ± 0.10. Extended treatment, 33 days, produced a small, clinically nonmeaningful increase in this value. The tyramine sensitivity factor for the Selegiline transdermal system was similar to that following treatment with 10 mg/d of oral Selegiline capsules but more than 20 times less than observed during tranylcypromine treatment. A larger increase in the tyramine sensitivity factor was observed following extended Selegiline transdermal system treatment at a higher dose (12 mg/24 h), which was significantly decreased following coadministration of tyramine capsules with a meal. These results suggest a wide tyramine safety margin for the Selegiline transdermal system and provide evidence that the 6-mg/24-h Selegiline transdermal system can be administered safely without dietary tyramine restrictions.
Lawrence F Blob - One of the best experts on this subject based on the ideXlab platform.
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evaluation of the potential for pharmacodynamic and pharmacokinetic drug interactions between Selegiline transdermal system and two sympathomimetic agents pseudoephedrine and phenylpropanolamine in healthy volunteers
The Journal of Clinical Pharmacology, 2007Co-Authors: Albert J Azzaro, Chad M Vandenberg, John Ziemniak, Eva M Kemper, Lawrence F Blob, Bryan J CampbellAbstract:Selegiline transdermal system is a recently approved monoamine oxidase inhibitor antidepressant. Medications that inhibit monoamine oxidase type A can augment the pressor effects of sympathomimetic amines, increasing the potential for hypertensive crisis. This study examined the potential for drug-drug interactions during treatment with Selegiline transdermal system and pseudoephedrine or phenylpropanolamine. Two studies were conducted with 25 healthy volunteers to assess changes in blood pressure and heart rate during administration of pseudoephedrine or phenylpropanolamine alone or together with Selegiline transdermal system. No significant differences in mean maximum changes in vital signs occurred with pseudoephedrine. No significant differences were found in mean maximum changes in systolic heart rate with phenylpropanolamine; however, 4 of 12 subjects each experienced 1 isolated protocol-defined minimal pressor response without concurrent adverse effects (1 with phenylpropanolamine alone; 3 with phenylpropanolamine + Selegiline transdermal system). Pharmacokinetic parameters obtained following Selegiline transdermal system and pseudoephedrine or phenylpropanolamine were unremarkable. The results suggest that Selegiline transdermal system 6 mg/24 h does not significantly alter the pharmacodynamics or pharmacokinetics of either pseudoephedrine or phenylpropanolamine when administered to healthy volunteers; however, it is prudent to avoid coadministration of Selegiline transdermal system and sympathomimetics.
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tyramine pressor sensitivity during treatment with the Selegiline transdermal system 6 mg 24 h in healthy subjects
The Journal of Clinical Pharmacology, 2006Co-Authors: Albert J Azzaro, Chad M Vandenberg, Eva M Kemper, Lawrence F Blob, Melvin Sharoky, Dan A Oren, Bryan J CampbellAbstract:The oral tyramine pressor test was administered to healthy males during treatment with a Selegiline transdermal system (STS; 6 mg/24 h). The tyramine sensitivity factor (TSF) was calculated from the ratio of baseline and on-treatment tyramine pressor doses. The tyramine sensitivity factor value following 9 days of treatment with the Selegiline transdermal system was 1.85 ± 0.10. Extended treatment, 33 days, produced a small, clinically nonmeaningful increase in this value. The tyramine sensitivity factor for the Selegiline transdermal system was similar to that following treatment with 10 mg/d of oral Selegiline capsules but more than 20 times less than observed during tranylcypromine treatment. A larger increase in the tyramine sensitivity factor was observed following extended Selegiline transdermal system treatment at a higher dose (12 mg/24 h), which was significantly decreased following coadministration of tyramine capsules with a meal. These results suggest a wide tyramine safety margin for the Selegiline transdermal system and provide evidence that the 6-mg/24-h Selegiline transdermal system can be administered safely without dietary tyramine restrictions.
