Apomorphine hydrochloride for the treatment of Parkinson’s disease

Abstract

Apomorphine (APO) is a potent D1 and D2 dopamine agonist. Plasma maximal concentration is reached in 8-16 min with a plasma half-life of 34-70 min. Bioavailability is close to 100%. It has a rapid antiparkinsonian action after subcutaneous (s.c.) administration with a size effect comparable with that of levodopa. Trials of s.c., oral, sublingual, intravenous, rectal, intranasal and iontophoretic transdermal administration of APO have been attempted in Parkinson's disease (PD), each of these routes have shown some potential for clinical effectiveness but the majority of studies indicate that APO intermittent s.c. administration, on which this review is mainly focused, is an effective therapy for the management of motor symptoms in PD, particularly in advanced phases mainly characterized by motor fluctuations, such as wearing OFF and unpredictable "off". Data on the effect of APO on non-motor symptoms in PD patients are limited but there is strong suggestion of a beneficial effect that warrants further investigation.

Pharmacological Insights into Levodopa‐induced Motor Fluctuations in Patients with Parkinson's Disease

“…A first set of articles is dedicated to new insights into apomorphine therapy. Apomorphine is an “old” dopamine agonist . Based on empirical experience, it is the sole dopamine agonist considered to be as efficacious and potent as l ‐dopa on parkinsonian motor symptoms.…”

“…Apomorphine is an "old" dopamine agonist. 4 Based on empirical experience, it is the sole dopamine agonist considered to be as efficacious and potent as L-dopa on parkinsonian motor symptoms. At the moment, apomorphine is not broadly used in clinical practice, because no orally active formulation exists.…”

Praktische Anwendung der kontinuierlichen Apomorphin-Pumpentherapie

“…Injektor [10] oder kontinuierlich mittels Medikamentenpumpe [11], in neueren Studien auch sublingual [12], angewendet werden (die sublinguale Applikation ist zur Behandlung des idiopathischen Parkinson-Syndroms aktuell jedoch noch nicht zugelassen). Darüber hinaus wurden auch intranasale, rektale und sogar iontophoretische transdermale Applikationen getestet, die sich jedoch bisher nicht etabliert haben [13]. In diesem Artikel soll die klinisch oft durchgeführte Darreichung mittels subkutaner Gabe durch eine Medikamentenpumpe vorgestellt werden.…”

Exploring the global animal biodiversity in the search for new drugs – Spiders, scorpions, horseshoe crabs, sea spiders, centipedes, and millipedes

“…A few examples are the analgesic salicylic acid from the white willow Salix alba L. (Salicaceae) [3]; the chemotherapeutic agent paclitaxel from the American yew Taxus brevifolia Nutt. (Taxaceae) [4]; the antiparkinson medication apomorphine, a semisynthetic compound derived from morphine from the opium poppy Papaver somniferum L. (Papaveraceae) [5]; the bronchodilator tiotropium, a derivative of atropine from the deadly nightshade Atropa belladonna L. (Solanaceae) [6]; the artemisinin-derived antimalarials from the Chinese sweet wormwood Artemisia annua L. (Asteraceae) [7]; and the anti-alzheimer drug galantamine that was first isolated from the Caucasian snowdrop Galanthus caucasicus (Baker) Grossh. (Amaryllidaceae) [8].…”