Dopamine agonist
| Dopamine Receptor agonist | |
|---|---|
| Drug class | |
| Class identifiers | |
| Use | Parkinson's disease, Attention deficit/hyperactivity disorder(ADHD), restless legs syndrome, clinical depression, etc. |
| ATC code | N04 |
| Biological target | Dopamine receptors |
| External links | |
| MeSH | D010300 |
A dopamine agonist is a compound that activates dopamine receptors in the absence of that receptor's physiological ligand, the neurotransmitter dopamine. Dopamine agonists activate signaling pathways through the dopamine receptor and trimeric G-proteins, ultimately leading to changes in gene transcription.
Contents
Uses
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Some medical drugs act as dopamine agonists and can treat hypodopaminergic (low dopamine) conditions; they are typically used for treating Parkinson's disease, attention deficit/hyperactivity disorder (in the form of stimulants) and certain pituitary tumors (prolactinoma), and may be useful for restless legs syndrome (RLS). Both Requip (Ropinirole) and Mirapex (Pramipexole) are FDA-approved for the treatment of RLS. There is also an ongoing clinical trial to test the effectiveness of the dopamine agonist Requip (ropinirole) in reversing the symptoms of SSRI-induced sexual dysfunction.[1] Additionally, a systematic review and meta-analysis concluded that prophylactic treatment with cabergoline reduces the incidence, but not the severity, of ovarian hyperstimulation syndrome (OHSS), without compromising pregnancy outcomes, in females undergoing stimulated cycles of in vitro fertilization (IVF).[2]
Side-effects
Some of the common side effects of dopamine agonists include:[3][4]
- Euphoria
- Pericardial effusion
- Fibrous thickening of lining that covers some of the internal organs including the heart or the lungs (fibrotic reaction)
- Hallucinations
- Causing or worsening psychosis
- Orthostatic hypotension
- Increased orgasmic intensity
- Weight loss
- Anorexia (symptom)
- Nausea and possible vomiting
- Insomnia
- Unusual tiredness or weakness
- Dizziness
- Drowsiness
- Possible Narcolepsy manifestations (Sleep attacks)[5]
- Lightheadedness
- Raynaud's phenomenon (common side effect of ergot derivatives)
- Syncope
- Twitching, twisting, or other unusual body movements
- Pathological addiction (gambling, shopping, internet pornography, hyper-sexuality) – specifically D3-preferring agonists
Examples
Examples of dopamine agonists include:
Partial agonist
- Aripiprazole (Partial agonist of the D2 family receptors - Trade name "Abilify" in the United States; atypical antipsychotic)
- Phencyclidine (a.k.a. PCP; partial agonist. Psychoactivity mainly due to NMDA antagonism)
- Quinpirole (Partial agonist of the D2 and D3 family of receptors)
- Salvinorin A (chief active constituent of the psychedelic herb salvia divinorum, the psychoactivity of which is mainly due to Kappa-opioid receptor agonism; partial agonist at the D2 with an Intrinsic activity of 40-60%, binding affinity of Ki=5-10nM and EC50=50-90nM)[6]
Agonists of full/unknown efficacy
- Apomorphine (Apokyn) (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Bromocriptine (Parlodel) (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Cabergoline (Dostinex) (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Ciladopa (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Dihydrexidine (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Dinapsoline (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Doxanthrine (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Epicriptine (Similar to those of Bromocriptine) (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Lisuride (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Pergolide (Dopamine Agonist for Parkinson's disease/Restless leg syndrome) (Permax) - Removed from the market in the USA March 29, 2007.[7]
- Piribedil (Dopamine Agonist for Parkinson's disease/Restless leg syndrome) (Pronoran and Trivastal)
- Pramipexole (Dopamine Agonist for Parkinson's disease/Restless leg syndrome) (Mirapex and Sifrol)
- Propylnorapomorphine (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Quinagolide (Norprolac) (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Ropinirole (Dopamine Agonist for Parkinson's disease/Restless leg syndrome) (Requip)
- Rotigotine (Dopamine Agonist for Parkinson's disease/Restless leg syndrome) (Neupro)
- Roxindole (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Sumanirole (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
Some, such as fenoldopam, are selective for dopamine receptor D1.[8]
See also
- Dopamine antagonist
- Receptor agonist
- GABA receptor agonist
- Dopaminergic
- Serotonin agonist
- Adrenergic agonist (Sympathomimetic)
- Parasympathomimetic drug (acetylcholine agonist)
- Histamine agonist
References
- ↑ Clinical trial number NCT00334048 at ClinicalTrials.gov - "Treating Sexual Dysfunction From SSRI Medication: a Study Comparing Requip CR to Placebo"
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- ↑ Seeman P, Guan HC, Hirbec H (2009). "Dopamine D2High receptors stimulated by phencyclidines, lysergic acid diethylamide, salvinorin A, and modafinil". Synapse 63 (8): 698–704. doi:10.1002/syn.20647. PMID 19391150.
- ↑ FDA Announces Voluntary Withdrawal of Pergolide Products
- ↑ Lua error in package.lua at line 80: module 'strict' not found.
6. Avanzi M, Uber E, Bonfa F. Pathological gambling in two patients on dopamine replacement therapy for Parkinson’s disease. Neurol Sci 2004; 25:98–101[Medline]
External links
- Dopamine Agonists at the US National Library of Medicine Medical Subject Headings (MeSH)
- http://www.abc.net.au/news/stories/2008/01/22/2143502.htm
- http://neuro.psychiatryonline.org/cgi/content/full/19/4/473
