Apomorphine

Apomorphine

File:Apomorphine.svg
Clinical data
Routes of administration	sc
ATC code	G04BE07 (WHO) N04BC07 (WHO)
Legal status
Legal status	II (California), non-scheduled (Rest of USA)
Pharmacokinetic data
Bioavailability	100% following sc injection
Protein binding	~50%
Metabolism	hepatic
Elimination half-life	40 minutes (range 30-60 minutes)
Identifiers
IUPAC name 5,6,6a,7-Tetrahydro-6-methyl-4H- dibenzo[de,g]quinolin-10,11-diol (?)
CAS Number	41372-20-7
PubChem CID	6005
DrugBank	APRD00531
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C17H17NO2
Molar mass	267.322 g/mol
See also: data page

WikiDoc Resources for Apomorphine
Articles
Most recent articles on Apomorphine Most cited articles on Apomorphine Review articles on Apomorphine Articles on Apomorphine in N Eng J Med, Lancet, BMJ
Media
Powerpoint slides on Apomorphine Images of Apomorphine Photos of Apomorphine Podcasts & MP3s on Apomorphine Videos on Apomorphine
Evidence Based Medicine
Cochrane Collaboration on Apomorphine Bandolier on Apomorphine TRIP on Apomorphine
Clinical Trials
Ongoing Trials on Apomorphine at Clinical Trials.gov Trial results on Apomorphine Clinical Trials on Apomorphine at Google
Guidelines / Policies / Govt
US National Guidelines Clearinghouse on Apomorphine NICE Guidance on Apomorphine NHS PRODIGY Guidance FDA on Apomorphine CDC on Apomorphine
Books
Books on Apomorphine
News
Apomorphine in the news Be alerted to news on Apomorphine News trends on Apomorphine
Commentary
Blogs on Apomorphine
Definitions
Definitions of Apomorphine
Patient Resources / Community
Patient resources on Apomorphine Discussion groups on Apomorphine Patient Handouts on Apomorphine Directions to Hospitals Treating Apomorphine Risk calculators and risk factors for Apomorphine
Healthcare Provider Resources
Symptoms of Apomorphine Causes & Risk Factors for Apomorphine Diagnostic studies for Apomorphine Treatment of Apomorphine
Continuing Medical Education (CME)
CME Programs on Apomorphine
International
Apomorphine en Espanol Apomorphine en Francais
Business
Apomorphine in the Marketplace Patents on Apomorphine
Experimental / Informatics
List of terms related to Apomorphine

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Please Take Over This Page and Apply to be Editor-In-Chief for this topic: There can be one or more than one Editor-In-Chief. You may also apply to be an Associate Editor-In-Chief of one of the subtopics below. Please mail us [2] to indicate your interest in serving either as an Editor-In-Chief of the entire topic or as an Associate Editor-In-Chief for a subtopic. Please be sure to attach your CV and or biographical sketch.

Overview

Apomorphine is a type of dopaminergic agonist, a morphine derivative (but does not actually contain morphine, or bind to opioid receptors). Apomorphine is a relatively non-selective dopamine receptor agonist, having possible slightly higher affinity for D₂-like dopamine receptors.

Historically, apomorphine has been tried for a variety of uses including psychiatric treatment of homosexuality in the early 20th century. Currently, apomorphine is used in the treatment of Parkinson's disease and (under the name Uprima) erectile dysfunction. It was also successfully used in the treatment of heroin addiction, a purpose for which it was championed by the author William S. Burroughs. It is a potent emetic, meaning that it should not be administered without an antiemetic such as domperidone. The emetic properties of apomorphine are exploited in veterinary medicine to induce therapeutic emesis in canines that have recently ingested toxic or foreign substances.

For treatment of erectile dysfunction, it is believed that dopamine receptors in the hypothalamic region of the brain are the main target, as although dopamine receptors in the penis do facilitate erection, they do so far more weakly than those in the brain.

Apomorphine is clear as a liquid but stains green. Therefore care must be taken to avoid splashes. Apormophine does not remain stable for more than 24 hours in a plastic container, so syringes are discarded if not used within 24 hours.

Use in Parkinson's disease

First mooted as a treatment for Parkinson's disease as early as 1951, its clinical use was first reported in 1970 by Cotzias et al, although its emetic properties and short half-life made oral use impractical. A later study found that combining the drug with the antiemetic domperidone improved results significantly.

Therapeutic use in Parkinson's disease is effective because of the drugs strong dopaminergic action, with a rapid effect (within 3-20 minutes of injection) but a brief duration. Whilst apomorphine can be used in combination with l-dopa, the intention is usually to wean patients off of this, as by this stage they will probably be experiencing a great deal of dopa-induced dyskinesias and "off" periods. Following a successful apomorphine challenge, training of patient and caregiver, and careful dose titration, there is no reason why an apomorphine pump can not be an effective monotherapy.

Erectile dysfunction

Apomorphine hydrochloride (trade name "Uprima") is used in the treatment of erectile dysfunction (male impotence). Its mode of stimulating dopamine in the brain which is believed to enhance the sexual response. It was found to be of poor efficacy in a large scale study by Researchers at the UK's Drug Safety Research Unit and University of Portsmouth and discontinued in the UK in January 2006. Around 65-70% of doctors felt it was ineffective, with 60% of over 11,000 patients (avg age 61) discontinuing in month 1 and a further 23% in month 2. Nonetheless some sources continue to supply the drug claiming it is effective.

External links

• PDSP K_i database
• "Apomorphine - Frequently Asked Questions". Britannia Pharmaceuticals.
• Andrew Lees and Kirsten Turner (2002). "Apomorphine for Parkinson's Disease" (PDF). Practical Neurology. 2: 280–287. doi:10.1046/j.1474-7766.2002.00086.x. - Detailed usage guide for Apomorphine pumps for Parkinson's

Template:WS