Limits...
Once-daily pramipexole for the treatment of early and advanced idiopathic Parkinson's disease: implications for patients.

Antonini A, Calandrella D - Neuropsychiatr Dis Treat (2011)

Bottom Line: The introduction of a once-daily formulation of pramipexole poses significant potential advantages for patients and this is reflected by relatively stable plasma levels.The most obvious benefit is convenience of use and better adherence to treatment schedule.Additional advantages may be represented by the opportunity to provide continuous drug delivery in a fashion that could potentially help minimize dyskinesia risk if the drug is used early in the disease course.

View Article: PubMed Central - PubMed

Affiliation: Department for Parkinson's Disease, IRCSS San Camillo, Venice, Italy;

ABSTRACT
Immediate-release (IR) pramipexole is indicated for the symptomatic treatment of idiopathic Parkinson's disease (PD), either alone (without levodopa) or in combination with levodopa, that is, during the entire progress of disease up to the advanced stage. It is also currently indicated for the treatment of moderate-to-severe primary restless legs syndrome (RLS). An extended-release (ER) formulation of pramipexole has been developed to allow a once-daily formulation and to provide more stable dopaminergic stimulation. This review summarized the pharmacokinetic profile of pramipexole for both the IR and ER formulations, and discussed the role of pramipexole in the management of early and advanced PD. The introduction of a once-daily formulation of pramipexole poses significant potential advantages for patients and this is reflected by relatively stable plasma levels. The most obvious benefit is convenience of use and better adherence to treatment schedule. Additional advantages may be represented by the opportunity to provide continuous drug delivery in a fashion that could potentially help minimize dyskinesia risk if the drug is used early in the disease course.

No MeSH data available.


Related in: MedlinePlus

Simulated concentration-time profile of pramipexole ER and pramipexole IR at steady state in Parkinson patients after intake of pramipexole ER 4.5 mg qd or pramipexole IR tid in intervals of 8 hours (8-8-8) or different intervals of 6 and 12 hours (6-6-12).Notes: Reproduced with permission from Eisenreich W, Sommer B, Hartter S, Jost WH. Pramipexole extended release: a novel treatment option in Parkinson’s disease. Parkinsons Dis. 2010;2010:612–619.16Abbreviations: ER, extended release; IR, immediate release; tid, three times daily; qd, once daily.
© Copyright Policy
Related In: Results  -  Collection


getmorefigures.php?uid=PMC3101890&req=5

f1-ndt-7-297: Simulated concentration-time profile of pramipexole ER and pramipexole IR at steady state in Parkinson patients after intake of pramipexole ER 4.5 mg qd or pramipexole IR tid in intervals of 8 hours (8-8-8) or different intervals of 6 and 12 hours (6-6-12).Notes: Reproduced with permission from Eisenreich W, Sommer B, Hartter S, Jost WH. Pramipexole extended release: a novel treatment option in Parkinson’s disease. Parkinsons Dis. 2010;2010:612–619.16Abbreviations: ER, extended release; IR, immediate release; tid, three times daily; qd, once daily.

Mentions: Pramipexole ER is a nonergolinic dopamine receptor agonist available for use as a once-daily oral treatment for the signs and symptoms of early and advanced PD. Continuous dopaminergic stimulation is a therapeutic concept for the development of dopamine agonists with continuous, as opposed to discontinuous or pulsatile, stimulation of striatal dopamine receptors. This concept derived from studies of the normal basal ganglia demonstrating that nigral dopaminergic neurons normally fire continuously and striatal dopamine levels are relatively constant. Once-daily pramipexole ER and three times daily pramipexole IR have similar exposure over 24 hours. In a Phase I trial, where pramipexole IR and ER tablets were assessed in fasted state, the minimum and maximum plasma concentration (Cmin, Cmax) and exposure (AUC) of the same daily dose of pramipexole ER tablets given once daily and pramipexole IR tablets given three times daily were equivalent. Moreover, once-daily administration of pramipexole ER tablets causes a smaller fluctuation in the pramipexole plasma concentration over 24 hours compared to the three times daily administration of pramipexole IR tablets. Maximum plasma concentrations occur at about 6 hours after administration of pramipexole ER tablets (Figure 1) and a steady state of exposure is reached after 5 days of continuous dosing at the latest.13


Once-daily pramipexole for the treatment of early and advanced idiopathic Parkinson's disease: implications for patients.

Antonini A, Calandrella D - Neuropsychiatr Dis Treat (2011)

Simulated concentration-time profile of pramipexole ER and pramipexole IR at steady state in Parkinson patients after intake of pramipexole ER 4.5 mg qd or pramipexole IR tid in intervals of 8 hours (8-8-8) or different intervals of 6 and 12 hours (6-6-12).Notes: Reproduced with permission from Eisenreich W, Sommer B, Hartter S, Jost WH. Pramipexole extended release: a novel treatment option in Parkinson’s disease. Parkinsons Dis. 2010;2010:612–619.16Abbreviations: ER, extended release; IR, immediate release; tid, three times daily; qd, once daily.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3101890&req=5

f1-ndt-7-297: Simulated concentration-time profile of pramipexole ER and pramipexole IR at steady state in Parkinson patients after intake of pramipexole ER 4.5 mg qd or pramipexole IR tid in intervals of 8 hours (8-8-8) or different intervals of 6 and 12 hours (6-6-12).Notes: Reproduced with permission from Eisenreich W, Sommer B, Hartter S, Jost WH. Pramipexole extended release: a novel treatment option in Parkinson’s disease. Parkinsons Dis. 2010;2010:612–619.16Abbreviations: ER, extended release; IR, immediate release; tid, three times daily; qd, once daily.
Mentions: Pramipexole ER is a nonergolinic dopamine receptor agonist available for use as a once-daily oral treatment for the signs and symptoms of early and advanced PD. Continuous dopaminergic stimulation is a therapeutic concept for the development of dopamine agonists with continuous, as opposed to discontinuous or pulsatile, stimulation of striatal dopamine receptors. This concept derived from studies of the normal basal ganglia demonstrating that nigral dopaminergic neurons normally fire continuously and striatal dopamine levels are relatively constant. Once-daily pramipexole ER and three times daily pramipexole IR have similar exposure over 24 hours. In a Phase I trial, where pramipexole IR and ER tablets were assessed in fasted state, the minimum and maximum plasma concentration (Cmin, Cmax) and exposure (AUC) of the same daily dose of pramipexole ER tablets given once daily and pramipexole IR tablets given three times daily were equivalent. Moreover, once-daily administration of pramipexole ER tablets causes a smaller fluctuation in the pramipexole plasma concentration over 24 hours compared to the three times daily administration of pramipexole IR tablets. Maximum plasma concentrations occur at about 6 hours after administration of pramipexole ER tablets (Figure 1) and a steady state of exposure is reached after 5 days of continuous dosing at the latest.13

Bottom Line: The introduction of a once-daily formulation of pramipexole poses significant potential advantages for patients and this is reflected by relatively stable plasma levels.The most obvious benefit is convenience of use and better adherence to treatment schedule.Additional advantages may be represented by the opportunity to provide continuous drug delivery in a fashion that could potentially help minimize dyskinesia risk if the drug is used early in the disease course.

View Article: PubMed Central - PubMed

Affiliation: Department for Parkinson's Disease, IRCSS San Camillo, Venice, Italy;

ABSTRACT
Immediate-release (IR) pramipexole is indicated for the symptomatic treatment of idiopathic Parkinson's disease (PD), either alone (without levodopa) or in combination with levodopa, that is, during the entire progress of disease up to the advanced stage. It is also currently indicated for the treatment of moderate-to-severe primary restless legs syndrome (RLS). An extended-release (ER) formulation of pramipexole has been developed to allow a once-daily formulation and to provide more stable dopaminergic stimulation. This review summarized the pharmacokinetic profile of pramipexole for both the IR and ER formulations, and discussed the role of pramipexole in the management of early and advanced PD. The introduction of a once-daily formulation of pramipexole poses significant potential advantages for patients and this is reflected by relatively stable plasma levels. The most obvious benefit is convenience of use and better adherence to treatment schedule. Additional advantages may be represented by the opportunity to provide continuous drug delivery in a fashion that could potentially help minimize dyskinesia risk if the drug is used early in the disease course.

No MeSH data available.


Related in: MedlinePlus