Sublingual apomorphine in Parkinson's disease: a clinical and pharmacokinetic study.
The clinical response and the pharmacokinetic parameters of 3 mg subcutaneous (SC) and 30 mg sublingual (SL) apomorphine were compared in nine patients with Parkinson's disease. The magnitude of the motor responses (evaluated by tapping and walking tests and the Webster scale) was similar for SC and SL apomorphine. However, the onset to action was delayed after SL when compared with SC apomorphine. No significant difference was found in bioavailability (area under the curve: AUC) or peak plasma concentration (Cmax) between SC and SL apomorphine, whereas time to peak plasma concentration (Tmax) was shorter after SC apomorphine. Eight other patients were treated for a mean time of 4 months with SL apomorphine with a significant reduction in daily "off" hours. However, four of these eight patients developed stomatitis after some weeks of treatment. These results indicated that (a) pharmacokinetics parallel the clinical response to SL apomorphine, (b) SL apomorphine can reduce severe off periods in parkinsonian patients when used chronically, and (c) its long-term use is limited by a severe side effect (stomatitis).
Montastruc
J L
JL
Department of Medical and Clinical Pharmacology INSERM U317, Centre Hospitalier Universitaire and Faculté de Médecine de Toulouse, France.
Rascol
O
O
Senard
J M
JM
Gualano
V
V
Bagheri
H
H
Houin
G
G
Lees
A
A
Rascol
A
A
D000286:Administration, Sublingual; D000368:Aged; D001058:Apomorphine / Q000008:administration & dosage* / Q000493:pharmacokinetics; D006801:Humans; D007279:Injections, Subcutaneous; D008875:Middle Aged; D010300:Parkinson Disease / Q000188:drug therapy*
D001058:Apomorphine