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QuickView for apomorphine (compound)


PubChem
Name: Apomorphine
PubChem Compound ID: 107882
Description: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.
Molecular formula: C34H38Cl2N2O5
Molecular weight: 625.581 g/mol
Synonyms:
(6aR)-5,6,6a,7-Tetrahydro-6-methyl-4H-dibenzo(de,g)chinolin-10,11-diol hydrochlorid; 4H-Dibenzo(de,g)quinoline-10,11-diol, 5,6,6a,7-tetrahydro-6-methyl-, hydrochloride, hemihydrate, (R)-; Uprima (TN); Apmorphine hydrochloride hemihydrate; D02004; Uprima; 4H-Dibenzo(de,g)quinoline-10,11-diol, 5,6,6a,7-tetrahydro-6-methyl-, hydrochloride, hydrate (2:1), (6aR)-; 6abeta-Aporphine-10,11-diol hydrochloride hemihydrate; Apomorphine hydrochloride; Apomorphin hydrochlorid wasser (2/1).
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DrugBank
Identification
Name: Apomorphine
Name (isomeric): DB00714
Drug Type: small molecule
Description: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.
Synonyms:
Apomorphinium Chloride Hemihydrate; L-Apomorphine; Apomorfin; VR-040; Apomorphine Hydrochloride; Apormorphine; VR004; VR-400; Apomorphine Hydrochloride Hemihydrate
Brand: Uprima, Ixense, Apokyn
Brand name mixture: Homeopathic Remedy Thc No. 48 Dps(Antimony Trisulfide + Apomorphine + Ipecac + Phosphorus + Pulsatilla)
Category: Antidyskinetics, Antiparkinson Agents, Dopamine Agonists
CAS number: 41372-20-7
Pharmacology
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.
Pharmacology: Apomorphine is a type of dopaminergic agonist, a morphine derivative which primarily affects the hypothalamic region of the brain. Drugs containing this substance are sometimes used in the treatment of Parkinson's disease or erectile dysfunction. In higher doses it is a highly effective emetic.
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 mot...
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Absorption: 100% following subcutaneous administration
Protein binding: ~50%-albumin
Biotransformation: Hepatic
Half Life: 40 minutes (range 30 - 60 minutes)
Clearance: 223 L/hr
Toxicity: LD50=0.6 mmoles/kg (mice, intraperitoneal)
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
TacrolimusAdditive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
LumefantrineAdditive QTc-prolongation may occur. Concomitant therapy should be avoided.
VorinostatAdditive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
ToremifeneAdditive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
ZuclopenthixolAdditive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). Antagonism may also occur between zuclopenthixol, a dopamine D2 receptor antagonist, and apomorphine, a dopamine agonist. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of both agents if concurrent therapy is initiated, discontinued or dose(s) changed.
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Targets