Apomorphine drug data and news

Apomorphine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Apomorphine
Brand Names/Synonyms Apokyn; Apomorfin; Apomorphine Hydrochloride Hemihydrate; Apomorphinium Chloride Hemihydrate; Apormorphine; L-Apomorphine; Uprima
Indication For the acute, intermittent treatment of hypomobility, off episodes (end-of-dose wearing off and unpredictable on/off episodes) associated with advanced Parkinson's disease.
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Description Not Available
Pharmacology Apomorphine is a non-ergoline dopamine agonist.
Mechanism Of Action The precise mechanism of action of apomorphine as a treatment for Parkinson's disease is unknown, although it is believed to be due to stimulation of post-synaptic dopamine D2-type receptors within the brain. Apomorphine has been shown to improve motor function in an animal model of Parkinson's disease. In particular, apomorphine attenuates the motor deficits induced by lesions in the ascending nigrostriatal dopaminergic pathway with the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) in primates.
Apomorphine News
(When available)

Kyowa Hakko Kogyo to Introduce Self-Injectable Drug for Treating ...  Feb 22, 2006
...announced on February 22 that it has concluded a licensing agreement with UK company Britannia Pharmaceuticals for a self-injectable formulation of apomorphine ... - Japan Corporate News (press release),

Race on to develop women’s yes-yes-yes pill  Feb 11, 2006
Several other companies, including Vectura, a British firm, are preparing drugs based on the chemical apomorphine, which works by mimicking dopamine, the brain ... - Times Online,

Interest aroused in a female love drug  Feb 12, 2006
Several other companies are preparing drugs based on the chemical apomorphine, which mimics dopamine, the brain's "signalling" chemical. ... - Australian,

Dosage Forms Subcutaneous soluion, not for IV
Drug_Category Antiparkinson Agents; Dopamine Agonists; Antidyskinetics; ATC:G04BE07; ATC:N04BC07
Absorption 100% subcutaneous administration
Interactions -->Interactions for Apomorphine:

5HT3 Antagonists

Based on reports of profound hypotension and loss of consciousness when apomorphine was administered with ondansetron, the concomitant use of apomorphine with drugs of the 5HT3 antagonist class (including, for example, ondansetron, granisetron, dolasetron, palonosetron, and alosetron) is contraindicated .

Antihypertensive Medications and Vasodilators

The following adverse events were experienced more commonly in patients receiving concomitant antihypertensive medications or vasodilators (n = 94) compared to patients not receiving these concomitant drugs (n = 456): hypotension 10% vs 4%, myocardial infarction 3% vs 1%, serious pneumonia 5% vs 3%, serious falls 9% vs 3%, and bone and joint injuries 6% vs 2%. The mechanism underlying many of these events is unknown, but may represent increased hypotension . Dopamine Antagonists

Since apomorphine is a dopamine agonist, it is possible that dopamine antagonists, such as the neuroleptics (phenoth-iazines, butyrophenones, thioxanthenes) or metoclopramide, may diminish the effectiveness of APOKYN. Patients with major psychotic disorders, treated with neuroleptics, should be treated with dopamine agonists only if the potential benefits outweigh the risks.

Drugs Prolonging the QT/QTc Interval

Caution should be exercised when prescribing apomorphine concomitantly with drugs that prolong the QT/QTc interval.

Drug/Laboratory Test Interactions

There are no known interactions between APOKYN and laboratory tests.

Toxicity LD50=0.6 mmoles/kg (mice, intraperitoneal)
Organisms Affected Humans and other mammals
Chemical IUPAC Name Not Available
Chemical Formula C17H17NO2
Molecular Weight 267.322 g/mol
Smiles String CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O
Melting Point Not Available
Water Solubility 1.66E+004 mg/L
State Solid
LogP/Hphobicity 3.03
Isoelectric Point 8.92
Biotransformation Hepatic
Half Life 40 minutes (range 30 - 60 minutes)
Protein Binding [%] ~50%-albumin
RxList Link RXlist
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Drug Reference http://www.rxlist.com/cgi/generic3/apokyn.htm
Drug Type Approved Drug
Accession No APRD00531
CAS Registry Number 41372-20-7
KEGG Compound ID Not Available
PubChem ID SID:148852
PharmGKB ID Not Available
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] Not Available

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