The Experts below are selected from a list of 243 Experts worldwide ranked by ideXlab platform
Pertti J Neuvonen - One of the best experts on this subject based on the ideXlab platform.
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Interactions of Buspirone with itraconazole and rifampicin: effects on the pharmacokinetics of the active 1-(2-pyrimidinyl)-piperazine metabolite of Buspirone.
Pharmacology & toxicology, 1999Co-Authors: Kari T. Kivistö, Tommi Lamberg, Pertti J NeuvonenAbstract:The effects of inhibition and induction of the metabolism of Buspirone on the plasma concentrations of 1-(2-pyrimidinyl)-piperazine (a piperazine metabolite), the principal active metabolite of Buspirone, were investigated. Two separate randomized, placebo-controlled cross-over studies with two phases were carried out in healthy volunteers. In Study I, six subjects took itraconazole 200 mg daily or matched placebo orally for 4 days. On day 4, 10 mg Buspirone was administered orally. In study II, six subjects took rifampicin 600 mg daily or matched placebo orally for 5 days. On day 6, 30 mg Buspirone was administered orally. Buspirone and piperazine metabolite concentrations in plasma were determined by gas chromatography. Itraconazole decreased the mean AUC of the piperazine metabolite by 50% (P
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Lack of effect of terfenadine on the pharmacokinetics of the CYP3A4 substrate Buspirone.
Pharmacology & toxicology, 1999Co-Authors: Tommi Lamberg, Kari T. Kivistö, Pertti J NeuvonenAbstract:The effects of terfenadine, a non-sedating antihistamine on the pharmacokinetics and pharmacodynamics of Buspirone, a CYP3A4 substrate, were investigated in a randomised, placebo-controlled, two-phase cross-over study. Ten healthy volunteers took either 120 mg terfenadine or matched placebo orally once daily for 3 days. On day 3, 10 mg Buspirone was taken orally. Plasma concentrations of Buspirone were measured up to 18 hr and its pharmacodynamic effects up to 8 hr. Terfenadine slightly but not significantly increased plasma concentrations of Buspirone. No psychomotor deterioration was observed during the terfenadine phase. In conclusion, terfenadine did not significantly affect the pharmacokinetics of Buspirone, a CYP3A4 substrate shown to be very susceptible to interactions with CYP3A4 inhibitors. Thus, terfenadine is expected to have little effect on the pharmacokinetics of CYP3A4 substrates in general.
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The effect of fluvoxamine on the pharmacokinetics and pharmacodynamics of Buspirone.
European journal of clinical pharmacology, 1998Co-Authors: Tommi Lamberg, Kari T. Kivistö, J Laitila, K Mårtensson, Pertti J NeuvonenAbstract:The effects of fluvoxamine, a selective serotonin (5-HT) reuptake inhibitor antidepressant, on the pharmacokinetics and pharmacodynamics of Buspirone, a non-benzodiazepine anxiolytic agent, were investigated. In a randomized, placebo-controlled, two-phase cross-over study, ten healthy volunteers took either 100 mg fluvoxamine or matched placebo orally once daily for 5 days. On day 6, 10 mg Buspirone was taken orally. Plasma concentrations of Buspirone and its active metabolite, 1-(2-pyrimidinyl)-piperazine (1-PP), were measured up to 18 h and the pharmacodynamic effects of Buspirone up to 8 h. The total area under the plasma Buspirone concentration-time curve was increased 2.4-fold (P < 0.05) and the peak plasma Buspirone concentration 2.0-fold (P < 0.05) by fluvoxamine, compared with placebo. The half-life of Buspirone was not affected. The ratio of the total area under the plasma concentration-time curve of 1-PP to that of Buspirone was decreased from 7.4 [6.3 (SD)] to 4.4 (3.6) by fluvoxamine (P < 0.05). The results of the six pharmacodynamic tests remained unchanged. Fluvoxamine moderately increased plasma Buspirone concentrations and decreased the production of the active 1-PP metabolite of Buspirone. The mechanism of this interaction is probably inhibition of the CYP3A4-mediated first-pass metabolism of Buspirone by fluvoxamine. However, this pharmacokinetic interaction was not associated with impairment of psychomotor performance and it is probably of limited clinical significance.
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Effects of verapamil and diltiazem on the pharmacokinetics and pharmacodynamics of Buspirone
Clinical pharmacology and therapeutics, 1998Co-Authors: Tommi Lamberg, Kari T. Kivistö, Pertti J NeuvonenAbstract:Background Buspirone has an extensive first-pass metabolism, which makes it potentially susceptible to drug interactions. The aim of this study was to investigate possible interactions of Buspirone with verapamil and diltiazem. Methods In a randomized, placebo-controlled, three-phase crossover study, nine healthy volunteers received either 80 mg verapamil, 60 mg diltiazem, or placebo orally three times a day. On day 2, after the fifth dose, 10 mg Buspirone was given orally. Plasma concentrations of Buspirone, verapamil, and diltiazem were determined up to 18 hours, and the effects of Buspirone were measured up to 8 hours. Results Verapamil and diltiazem increased the area under the Buspirone plasma concentration-time curve [AUC (0-∞)] 3.4-fold (p < 0.001) and 5.5-fold (p < 0.001), respectively. The peak plasma concentration of Buspirone was increased 3.4-fold (p < 0.001) and 4.1-fold (p < 0.001) by verapamil and diltiazem, respectively. The effect of diltiazem on the AUC(0-∞) of Buspirone was significantly (p < 0.05) greater than that of verapamil. The elimination half-life of Buspirone was not changed by verapamil and diltiazem. Of the six pharmacodynamic variables, only the subjective overall drug effect of Buspirone was significantly increased with verapamil (p < 0.05) and diltiazem (p < 0.05). Side effects of Buspirone occurred more often (p < 0.05) with diltiazem than with placebo. Conclusions Both verapamil and diltiazem considerably increase plasma Buspirone concentrations, probably by inhibiting its CYP3A4-mediated first-pass metabolism. Thus enhanced effects and side effects of Buspirone are possible when it is used with verapamil, diltiazem, or other inhibitors of CYP3A4. Clinical Pharmacology & Therapeutics (1998) 63, 640–645; doi:
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Grapefruit juice substantially increases plasma concentrations of Buspirone
Clinical pharmacology and therapeutics, 1998Co-Authors: Jari J. Lilja, Kari T. Kivistö, Tommi Lamberg, Janne T. Backman, Pertti J NeuvonenAbstract:Background Buspirone has a low oral bioavailability because of extensive first-pass metabolism. The effect of grapefruit juice on the pharmacokinetics and pharmacodynamics of orally administered Buspirone is not known. Methods In a randomized, 2-phase crossover study, 10 healthy volunteers took either 200 mL double-strength grapefruit juice or water 3 times a day for 2 days. On day 3, each subject ingested 10 mg Buspirone with either 200 mL grapefruit juice or water, and an additional 200 mL was ingested ½ hour and 1½ hours after Buspirone administration. Timed blood samples were collected up to 12 hours after ingestion, and the effects of Buspirone were measured with 6 psychomotor tests up to 8 hours after ingestion. Results Grapefruit juice increased the mean peak plasma concentration of Buspirone 4.3-fold (range, 2-fold to 15.6-fold; P < .01) and the mean area under the plasma Buspirone concentration-time curve 9.2-fold (range, 3-fold to 20.4-fold; P < .01). The time of the peak concentration (tmax) of Buspirone increased from 0.75 to 3 hours (P < .01), and the elimination half-life (t½) was slightly increased (P < .01) by grapefruit juice. A significant increase in the pharmacodynamic effects of Buspirone by grapefruit juice was seen only in subjective overall drug effect (P < .01). Conclusions Grapefruit juice considerably increased plasma Buspirone concentrations. The probable mechanism of this interaction is delayed gastric emptying and inhibition of the cytochrome P450 3A4-mediated first-pass metabolism of Buspirone caused by grapefruit juice. Concomitant use of Buspirone and at least large amounts of grapefruit juice should be avoided. Clinical Pharmacology & Therapeutics (1998) 64, 655–660; doi:
Tommi Lamberg - One of the best experts on this subject based on the ideXlab platform.
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Interactions of Buspirone with itraconazole and rifampicin: effects on the pharmacokinetics of the active 1-(2-pyrimidinyl)-piperazine metabolite of Buspirone.
Pharmacology & toxicology, 1999Co-Authors: Kari T. Kivistö, Tommi Lamberg, Pertti J NeuvonenAbstract:The effects of inhibition and induction of the metabolism of Buspirone on the plasma concentrations of 1-(2-pyrimidinyl)-piperazine (a piperazine metabolite), the principal active metabolite of Buspirone, were investigated. Two separate randomized, placebo-controlled cross-over studies with two phases were carried out in healthy volunteers. In Study I, six subjects took itraconazole 200 mg daily or matched placebo orally for 4 days. On day 4, 10 mg Buspirone was administered orally. In study II, six subjects took rifampicin 600 mg daily or matched placebo orally for 5 days. On day 6, 30 mg Buspirone was administered orally. Buspirone and piperazine metabolite concentrations in plasma were determined by gas chromatography. Itraconazole decreased the mean AUC of the piperazine metabolite by 50% (P
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Lack of effect of terfenadine on the pharmacokinetics of the CYP3A4 substrate Buspirone.
Pharmacology & toxicology, 1999Co-Authors: Tommi Lamberg, Kari T. Kivistö, Pertti J NeuvonenAbstract:The effects of terfenadine, a non-sedating antihistamine on the pharmacokinetics and pharmacodynamics of Buspirone, a CYP3A4 substrate, were investigated in a randomised, placebo-controlled, two-phase cross-over study. Ten healthy volunteers took either 120 mg terfenadine or matched placebo orally once daily for 3 days. On day 3, 10 mg Buspirone was taken orally. Plasma concentrations of Buspirone were measured up to 18 hr and its pharmacodynamic effects up to 8 hr. Terfenadine slightly but not significantly increased plasma concentrations of Buspirone. No psychomotor deterioration was observed during the terfenadine phase. In conclusion, terfenadine did not significantly affect the pharmacokinetics of Buspirone, a CYP3A4 substrate shown to be very susceptible to interactions with CYP3A4 inhibitors. Thus, terfenadine is expected to have little effect on the pharmacokinetics of CYP3A4 substrates in general.
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The effect of fluvoxamine on the pharmacokinetics and pharmacodynamics of Buspirone.
European journal of clinical pharmacology, 1998Co-Authors: Tommi Lamberg, Kari T. Kivistö, J Laitila, K Mårtensson, Pertti J NeuvonenAbstract:The effects of fluvoxamine, a selective serotonin (5-HT) reuptake inhibitor antidepressant, on the pharmacokinetics and pharmacodynamics of Buspirone, a non-benzodiazepine anxiolytic agent, were investigated. In a randomized, placebo-controlled, two-phase cross-over study, ten healthy volunteers took either 100 mg fluvoxamine or matched placebo orally once daily for 5 days. On day 6, 10 mg Buspirone was taken orally. Plasma concentrations of Buspirone and its active metabolite, 1-(2-pyrimidinyl)-piperazine (1-PP), were measured up to 18 h and the pharmacodynamic effects of Buspirone up to 8 h. The total area under the plasma Buspirone concentration-time curve was increased 2.4-fold (P < 0.05) and the peak plasma Buspirone concentration 2.0-fold (P < 0.05) by fluvoxamine, compared with placebo. The half-life of Buspirone was not affected. The ratio of the total area under the plasma concentration-time curve of 1-PP to that of Buspirone was decreased from 7.4 [6.3 (SD)] to 4.4 (3.6) by fluvoxamine (P < 0.05). The results of the six pharmacodynamic tests remained unchanged. Fluvoxamine moderately increased plasma Buspirone concentrations and decreased the production of the active 1-PP metabolite of Buspirone. The mechanism of this interaction is probably inhibition of the CYP3A4-mediated first-pass metabolism of Buspirone by fluvoxamine. However, this pharmacokinetic interaction was not associated with impairment of psychomotor performance and it is probably of limited clinical significance.
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Effects of verapamil and diltiazem on the pharmacokinetics and pharmacodynamics of Buspirone
Clinical pharmacology and therapeutics, 1998Co-Authors: Tommi Lamberg, Kari T. Kivistö, Pertti J NeuvonenAbstract:Background Buspirone has an extensive first-pass metabolism, which makes it potentially susceptible to drug interactions. The aim of this study was to investigate possible interactions of Buspirone with verapamil and diltiazem. Methods In a randomized, placebo-controlled, three-phase crossover study, nine healthy volunteers received either 80 mg verapamil, 60 mg diltiazem, or placebo orally three times a day. On day 2, after the fifth dose, 10 mg Buspirone was given orally. Plasma concentrations of Buspirone, verapamil, and diltiazem were determined up to 18 hours, and the effects of Buspirone were measured up to 8 hours. Results Verapamil and diltiazem increased the area under the Buspirone plasma concentration-time curve [AUC (0-∞)] 3.4-fold (p < 0.001) and 5.5-fold (p < 0.001), respectively. The peak plasma concentration of Buspirone was increased 3.4-fold (p < 0.001) and 4.1-fold (p < 0.001) by verapamil and diltiazem, respectively. The effect of diltiazem on the AUC(0-∞) of Buspirone was significantly (p < 0.05) greater than that of verapamil. The elimination half-life of Buspirone was not changed by verapamil and diltiazem. Of the six pharmacodynamic variables, only the subjective overall drug effect of Buspirone was significantly increased with verapamil (p < 0.05) and diltiazem (p < 0.05). Side effects of Buspirone occurred more often (p < 0.05) with diltiazem than with placebo. Conclusions Both verapamil and diltiazem considerably increase plasma Buspirone concentrations, probably by inhibiting its CYP3A4-mediated first-pass metabolism. Thus enhanced effects and side effects of Buspirone are possible when it is used with verapamil, diltiazem, or other inhibitors of CYP3A4. Clinical Pharmacology & Therapeutics (1998) 63, 640–645; doi:
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Grapefruit juice substantially increases plasma concentrations of Buspirone
Clinical pharmacology and therapeutics, 1998Co-Authors: Jari J. Lilja, Kari T. Kivistö, Tommi Lamberg, Janne T. Backman, Pertti J NeuvonenAbstract:Background Buspirone has a low oral bioavailability because of extensive first-pass metabolism. The effect of grapefruit juice on the pharmacokinetics and pharmacodynamics of orally administered Buspirone is not known. Methods In a randomized, 2-phase crossover study, 10 healthy volunteers took either 200 mL double-strength grapefruit juice or water 3 times a day for 2 days. On day 3, each subject ingested 10 mg Buspirone with either 200 mL grapefruit juice or water, and an additional 200 mL was ingested ½ hour and 1½ hours after Buspirone administration. Timed blood samples were collected up to 12 hours after ingestion, and the effects of Buspirone were measured with 6 psychomotor tests up to 8 hours after ingestion. Results Grapefruit juice increased the mean peak plasma concentration of Buspirone 4.3-fold (range, 2-fold to 15.6-fold; P < .01) and the mean area under the plasma Buspirone concentration-time curve 9.2-fold (range, 3-fold to 20.4-fold; P < .01). The time of the peak concentration (tmax) of Buspirone increased from 0.75 to 3 hours (P < .01), and the elimination half-life (t½) was slightly increased (P < .01) by grapefruit juice. A significant increase in the pharmacodynamic effects of Buspirone by grapefruit juice was seen only in subjective overall drug effect (P < .01). Conclusions Grapefruit juice considerably increased plasma Buspirone concentrations. The probable mechanism of this interaction is delayed gastric emptying and inhibition of the cytochrome P450 3A4-mediated first-pass metabolism of Buspirone caused by grapefruit juice. Concomitant use of Buspirone and at least large amounts of grapefruit juice should be avoided. Clinical Pharmacology & Therapeutics (1998) 64, 655–660; doi:
Kari T. Kivistö - One of the best experts on this subject based on the ideXlab platform.
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Interactions of Buspirone with itraconazole and rifampicin: effects on the pharmacokinetics of the active 1-(2-pyrimidinyl)-piperazine metabolite of Buspirone.
Pharmacology & toxicology, 1999Co-Authors: Kari T. Kivistö, Tommi Lamberg, Pertti J NeuvonenAbstract:The effects of inhibition and induction of the metabolism of Buspirone on the plasma concentrations of 1-(2-pyrimidinyl)-piperazine (a piperazine metabolite), the principal active metabolite of Buspirone, were investigated. Two separate randomized, placebo-controlled cross-over studies with two phases were carried out in healthy volunteers. In Study I, six subjects took itraconazole 200 mg daily or matched placebo orally for 4 days. On day 4, 10 mg Buspirone was administered orally. In study II, six subjects took rifampicin 600 mg daily or matched placebo orally for 5 days. On day 6, 30 mg Buspirone was administered orally. Buspirone and piperazine metabolite concentrations in plasma were determined by gas chromatography. Itraconazole decreased the mean AUC of the piperazine metabolite by 50% (P
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Lack of effect of terfenadine on the pharmacokinetics of the CYP3A4 substrate Buspirone.
Pharmacology & toxicology, 1999Co-Authors: Tommi Lamberg, Kari T. Kivistö, Pertti J NeuvonenAbstract:The effects of terfenadine, a non-sedating antihistamine on the pharmacokinetics and pharmacodynamics of Buspirone, a CYP3A4 substrate, were investigated in a randomised, placebo-controlled, two-phase cross-over study. Ten healthy volunteers took either 120 mg terfenadine or matched placebo orally once daily for 3 days. On day 3, 10 mg Buspirone was taken orally. Plasma concentrations of Buspirone were measured up to 18 hr and its pharmacodynamic effects up to 8 hr. Terfenadine slightly but not significantly increased plasma concentrations of Buspirone. No psychomotor deterioration was observed during the terfenadine phase. In conclusion, terfenadine did not significantly affect the pharmacokinetics of Buspirone, a CYP3A4 substrate shown to be very susceptible to interactions with CYP3A4 inhibitors. Thus, terfenadine is expected to have little effect on the pharmacokinetics of CYP3A4 substrates in general.
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The effect of fluvoxamine on the pharmacokinetics and pharmacodynamics of Buspirone.
European journal of clinical pharmacology, 1998Co-Authors: Tommi Lamberg, Kari T. Kivistö, J Laitila, K Mårtensson, Pertti J NeuvonenAbstract:The effects of fluvoxamine, a selective serotonin (5-HT) reuptake inhibitor antidepressant, on the pharmacokinetics and pharmacodynamics of Buspirone, a non-benzodiazepine anxiolytic agent, were investigated. In a randomized, placebo-controlled, two-phase cross-over study, ten healthy volunteers took either 100 mg fluvoxamine or matched placebo orally once daily for 5 days. On day 6, 10 mg Buspirone was taken orally. Plasma concentrations of Buspirone and its active metabolite, 1-(2-pyrimidinyl)-piperazine (1-PP), were measured up to 18 h and the pharmacodynamic effects of Buspirone up to 8 h. The total area under the plasma Buspirone concentration-time curve was increased 2.4-fold (P < 0.05) and the peak plasma Buspirone concentration 2.0-fold (P < 0.05) by fluvoxamine, compared with placebo. The half-life of Buspirone was not affected. The ratio of the total area under the plasma concentration-time curve of 1-PP to that of Buspirone was decreased from 7.4 [6.3 (SD)] to 4.4 (3.6) by fluvoxamine (P < 0.05). The results of the six pharmacodynamic tests remained unchanged. Fluvoxamine moderately increased plasma Buspirone concentrations and decreased the production of the active 1-PP metabolite of Buspirone. The mechanism of this interaction is probably inhibition of the CYP3A4-mediated first-pass metabolism of Buspirone by fluvoxamine. However, this pharmacokinetic interaction was not associated with impairment of psychomotor performance and it is probably of limited clinical significance.
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Effects of verapamil and diltiazem on the pharmacokinetics and pharmacodynamics of Buspirone
Clinical pharmacology and therapeutics, 1998Co-Authors: Tommi Lamberg, Kari T. Kivistö, Pertti J NeuvonenAbstract:Background Buspirone has an extensive first-pass metabolism, which makes it potentially susceptible to drug interactions. The aim of this study was to investigate possible interactions of Buspirone with verapamil and diltiazem. Methods In a randomized, placebo-controlled, three-phase crossover study, nine healthy volunteers received either 80 mg verapamil, 60 mg diltiazem, or placebo orally three times a day. On day 2, after the fifth dose, 10 mg Buspirone was given orally. Plasma concentrations of Buspirone, verapamil, and diltiazem were determined up to 18 hours, and the effects of Buspirone were measured up to 8 hours. Results Verapamil and diltiazem increased the area under the Buspirone plasma concentration-time curve [AUC (0-∞)] 3.4-fold (p < 0.001) and 5.5-fold (p < 0.001), respectively. The peak plasma concentration of Buspirone was increased 3.4-fold (p < 0.001) and 4.1-fold (p < 0.001) by verapamil and diltiazem, respectively. The effect of diltiazem on the AUC(0-∞) of Buspirone was significantly (p < 0.05) greater than that of verapamil. The elimination half-life of Buspirone was not changed by verapamil and diltiazem. Of the six pharmacodynamic variables, only the subjective overall drug effect of Buspirone was significantly increased with verapamil (p < 0.05) and diltiazem (p < 0.05). Side effects of Buspirone occurred more often (p < 0.05) with diltiazem than with placebo. Conclusions Both verapamil and diltiazem considerably increase plasma Buspirone concentrations, probably by inhibiting its CYP3A4-mediated first-pass metabolism. Thus enhanced effects and side effects of Buspirone are possible when it is used with verapamil, diltiazem, or other inhibitors of CYP3A4. Clinical Pharmacology & Therapeutics (1998) 63, 640–645; doi:
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Grapefruit juice substantially increases plasma concentrations of Buspirone
Clinical pharmacology and therapeutics, 1998Co-Authors: Jari J. Lilja, Kari T. Kivistö, Tommi Lamberg, Janne T. Backman, Pertti J NeuvonenAbstract:Background Buspirone has a low oral bioavailability because of extensive first-pass metabolism. The effect of grapefruit juice on the pharmacokinetics and pharmacodynamics of orally administered Buspirone is not known. Methods In a randomized, 2-phase crossover study, 10 healthy volunteers took either 200 mL double-strength grapefruit juice or water 3 times a day for 2 days. On day 3, each subject ingested 10 mg Buspirone with either 200 mL grapefruit juice or water, and an additional 200 mL was ingested ½ hour and 1½ hours after Buspirone administration. Timed blood samples were collected up to 12 hours after ingestion, and the effects of Buspirone were measured with 6 psychomotor tests up to 8 hours after ingestion. Results Grapefruit juice increased the mean peak plasma concentration of Buspirone 4.3-fold (range, 2-fold to 15.6-fold; P < .01) and the mean area under the plasma Buspirone concentration-time curve 9.2-fold (range, 3-fold to 20.4-fold; P < .01). The time of the peak concentration (tmax) of Buspirone increased from 0.75 to 3 hours (P < .01), and the elimination half-life (t½) was slightly increased (P < .01) by grapefruit juice. A significant increase in the pharmacodynamic effects of Buspirone by grapefruit juice was seen only in subjective overall drug effect (P < .01). Conclusions Grapefruit juice considerably increased plasma Buspirone concentrations. The probable mechanism of this interaction is delayed gastric emptying and inhibition of the cytochrome P450 3A4-mediated first-pass metabolism of Buspirone caused by grapefruit juice. Concomitant use of Buspirone and at least large amounts of grapefruit juice should be avoided. Clinical Pharmacology & Therapeutics (1998) 64, 655–660; doi:
David N. Johnson - One of the best experts on this subject based on the ideXlab platform.
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comparison of routes of administration and time course effects of zacopride and Buspirone in mice using an automated light dark test
Pharmacology Biochemistry and Behavior, 1991Co-Authors: Richard Young, David N. JohnsonAbstract:Abstract The behavioral effects of zacopride and Buspirone were assessed in mice in a fully automated 2-compartment light/dark test. A significant increase in time mice spent in the lit area was used as an indication of anxiolytic-like action. Doses of zacopride from 0.0001 to 17.8 mg/kg, IP, and Buspirone from 3.16 to 17.8 mg/kg, IP, produced significant increases in time mice spent in the lit area of the chamber. In addition, zacopride and Buspirone were compared for oral potency and for duration of action after IP and PO administration. Zacopride and Buspirone produced anxiolytic-like activity between doses of 0.001 to 100.0 mg/kg, PO, and 10.0 to 56.2 mg/kg, PO, respectively. The duration of effect of Buspirone was 2 to 4 h after IP or PO administration, while that for zacopride was ≥16 h by either route of administration. Thus, when compared for anxiolytic-like effects in this test, zacopride is a more potent and longer acting agent than Buspirone.
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Comparison of routes of administration and time course effects of zacopride and Buspirone in mice using an automated light/dark test
Pharmacology biochemistry and behavior, 1991Co-Authors: Richard Young, David N. JohnsonAbstract:Abstract The behavioral effects of zacopride and Buspirone were assessed in mice in a fully automated 2-compartment light/dark test. A significant increase in time mice spent in the lit area was used as an indication of anxiolytic-like action. Doses of zacopride from 0.0001 to 17.8 mg/kg, IP, and Buspirone from 3.16 to 17.8 mg/kg, IP, produced significant increases in time mice spent in the lit area of the chamber. In addition, zacopride and Buspirone were compared for oral potency and for duration of action after IP and PO administration. Zacopride and Buspirone produced anxiolytic-like activity between doses of 0.001 to 100.0 mg/kg, PO, and 10.0 to 56.2 mg/kg, PO, respectively. The duration of effect of Buspirone was 2 to 4 h after IP or PO administration, while that for zacopride was ≥16 h by either route of administration. Thus, when compared for anxiolytic-like effects in this test, zacopride is a more potent and longer acting agent than Buspirone.
Richard Young - One of the best experts on this subject based on the ideXlab platform.
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comparison of routes of administration and time course effects of zacopride and Buspirone in mice using an automated light dark test
Pharmacology Biochemistry and Behavior, 1991Co-Authors: Richard Young, David N. JohnsonAbstract:Abstract The behavioral effects of zacopride and Buspirone were assessed in mice in a fully automated 2-compartment light/dark test. A significant increase in time mice spent in the lit area was used as an indication of anxiolytic-like action. Doses of zacopride from 0.0001 to 17.8 mg/kg, IP, and Buspirone from 3.16 to 17.8 mg/kg, IP, produced significant increases in time mice spent in the lit area of the chamber. In addition, zacopride and Buspirone were compared for oral potency and for duration of action after IP and PO administration. Zacopride and Buspirone produced anxiolytic-like activity between doses of 0.001 to 100.0 mg/kg, PO, and 10.0 to 56.2 mg/kg, PO, respectively. The duration of effect of Buspirone was 2 to 4 h after IP or PO administration, while that for zacopride was ≥16 h by either route of administration. Thus, when compared for anxiolytic-like effects in this test, zacopride is a more potent and longer acting agent than Buspirone.
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Comparison of routes of administration and time course effects of zacopride and Buspirone in mice using an automated light/dark test
Pharmacology biochemistry and behavior, 1991Co-Authors: Richard Young, David N. JohnsonAbstract:Abstract The behavioral effects of zacopride and Buspirone were assessed in mice in a fully automated 2-compartment light/dark test. A significant increase in time mice spent in the lit area was used as an indication of anxiolytic-like action. Doses of zacopride from 0.0001 to 17.8 mg/kg, IP, and Buspirone from 3.16 to 17.8 mg/kg, IP, produced significant increases in time mice spent in the lit area of the chamber. In addition, zacopride and Buspirone were compared for oral potency and for duration of action after IP and PO administration. Zacopride and Buspirone produced anxiolytic-like activity between doses of 0.001 to 100.0 mg/kg, PO, and 10.0 to 56.2 mg/kg, PO, respectively. The duration of effect of Buspirone was 2 to 4 h after IP or PO administration, while that for zacopride was ≥16 h by either route of administration. Thus, when compared for anxiolytic-like effects in this test, zacopride is a more potent and longer acting agent than Buspirone.
