Relation between clinical efficacy and pharmacokinetic parameters after sublingual apomorphine in Parkinson's disease
| Autor: | Dordain G, A. Eschalier, Lavarenne J, F Durif, M Tournilhac, Paire M, D Deffond |
|---|---|
| Rok vydání: | 1993 |
| Předmět: |
Adult
Male medicine.medical_specialty Parkinson's disease Apomorphine Cmax Administration Sublingual Dopamine agonist Sublingual administration Pharmacokinetics Internal medicine medicine Humans Pharmacology (medical) Clinical efficacy Chromatography High Pressure Liquid Aged Pharmacology business.industry Therapeutic effect Parkinson Disease Middle Aged medicine.disease Endocrinology Female Neurology (clinical) business medicine.drug |
| Zdroj: | Clinical neuropharmacology. 16(2) |
| ISSN: | 0362-5664 |
| Popis: | Apomorphine was administered sublingually in two single doses (0.3 and 0.6 mg/kg) to seven patients with idiopathic Parkinson's disease (PD) to assess the relation between clinical efficacy, dosage, and pharmacokinetic parameters of apomorphine. On day 1 and day 3, patients were given 0.3 mg/kg and 0.6 mg/kg of apomorphine, respectively (3 mg tablets). Before apomorphine administration and during the following 4 h, motor score was assessed by measuring tremor, akinesia scores, rising from a chair, and walking speed. The delay to turn on was not different between the two doses but after the 0.3 mg/kg dose, only three patients turned on, whereas all the patients treated with 0.6 mg/kg turned on. Apomorphine (0.3 mg/kg) induced a shorter duration of the "on" period than 0.6 mg/kg (0.3 mg/kg: 24.2 +/- 14.6 min; 0.6 mg/kg: 86.7 +/- 14.9 min). The time to obtain the peak plasma concentration (tmax) obtained with the two doses were not different (0.3 mg/kg: 31.5 +/- 3.4 min; 0.6 mg/kg: 38.3 +/- 2.8 min). Peak plasma concentrations (Cmax) and areas under the curve (AUC) were significantly higher after 0.6 mg/kg than 0.3 mg/kg (Cmax: 0.3 mg/kg: 7.5 +/- 3.2 ng/ml; 0.6 mg/kg: 22.7 +/- 3.6 ng/ml; p < 0.01; AUC: 0.3 mg/kg: 929 +/- 109 ng/ml/min; 0.6 mg/kg; 2,277 +/- 209 ng/ml/min; p < 0.01). There was a significant linear correlation between the duration of therapeutic effect, AUC, and Cmax (r = 0.86, p < 0.01 for AUC; r = 0.63, p < 0.05 for Cmax). These results show that sublingual apomorphine could be of interest in the treatment of "off" phases in parkinsonian patients with motor fluctuations. |
| Databáze: | OpenAIRE |
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