From Wikipedia, the free encyclopedia
|Dopamine Receptor agonist|
|Use||Parkinson's disease, restless legs syndrome, clinical depression, etc.|
|Biological target||Dopamine receptors|
A dopamine agonist is a compound that activates dopamine receptors in the absence of dopamine. Dopamine agonists activate signaling pathways through the dopamine receptor and trimeric G-proteins, ultimately leading to changes in gene transcription.
Some medical drugs act as dopamine agonists and can treat hypodopaminergic (low dopamine) conditions; they are typically used for treating Parkinson's disease 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 and Post-SSRI sexual dysfunction (PSSD). 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). Inverse agonists, such as haloperidol, or antagonists, such as risperidone, of dopaminergic receptors can also be used as an antidote for overdose of antipsychotic.
- Pericardial effusion
- Fibrous thickening of lining that covers some of the internal organs including the heart or the lungs (fibrotic reaction)
- Causing or worsening psychosis
- Orthostatic hypotension
- Increased orgasmic intensity
- Weight loss
- Anorexia (symptom)
- Unusual tiredness or weakness
- Twitching, twisting, or other unusual body movements
- Pathological addiction (gambling, shopping, internet pornography, hyper-sexuality) – specifically D3-preferring agonists
Examples of dopamine agonists include:
- 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) 
Agonists of full/unknown efficacy
- Apomorphine (Apokyn)
- Bromocriptine (Parlodel)
- Cabergoline (Dostinex)
- Epicriptine (Similar to those of Bromocriptine)
- Pergolide (Permax) - Removed from the market in the USA March 29, 2007.
- Pramipexole (Mirapex and Sifrol)
- Quinagolide (Norprolac)
- Ropinirole (Requip)
- Rotigotine (Neupro)
- Dopamine antagonist
- Receptor agonist
- Serotonin agonist
- Adrenergic agonist
- Histamine agonist
- Acetylcholine agonist
- GABA agonist
- ClinicalTrials.gov NCT00334048 - "Treating Sexual Dysfunction From SSRI Medication: a Study Comparing Requip CR to Placebo"
- Youssef MA, van Wely M, Hassan MA, et al. (March 2010). "Can dopamine agonists reduce the incidence and severity of OHSS in IVF/ICSI treatment cycles? A systematic review and meta-analysis". Hum Reprod Update 16 (5): 459–66. doi:10.1093/humupd/dmq006. PMID 20354100.
- "MedlinePlus Drug Information: Pramipexole (Systemic)". United States National Library of Medicine. Archived from the original on 2006-09-26. Retrieved 2006-09-27.
- Boyd, Alan (1995). "Bromocriptine and psychosis: A literature review". Psychiatric Quarterly 66 (1): 87–95. doi:10.1007/BF02238717. PMID 7701022. Retrieved 2008-09-06.
- 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
- Ng SS, Pang CC (March 2000). "In vivo venodilator action of fenoldopam, a dopamine D(1)-receptor agonist". Br. J. Pharmacol. 129 (5): 853–8. doi:10.1038/sj.bjp.0703119. PMC 1571905. PMID 10696081.
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]
- Dopamine Agonists at the US National Library of Medicine Medical Subject Headings (MeSH)