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Pramipexole
Systematic (IUPAC) name
(S)-N6-propyl-4,5,6,7-tetrahydro-1,3-benzothiazole-2,6-diamine
Identifiers
CAS number 104632-26-0
ATC code N04BC05
PubChem 59868
DrugBank APRD00156
Chemical data
Formula C 10H17N3S 
Mol. mass 211.324 g/mol
Pharmacokinetic data
Bioavailability >90%
Protein binding 15%
Metabolism Minimal
Half life 8 hours
Excretion Renal (90%) and fecal (2%)
Therapeutic considerations
Licence data

EU EMEA:linkUS FDA:link

Pregnancy cat. B3(AU) C(US)
Legal status Prescription only
Routes Oral
 Yes check.svgY(what is this?)  (verify)

Pramipexole (Mirapex, Mirapexin, Sifrol) is a medication indicated for treating Parkinson's disease and restless legs syndrome (RLS). It is also sometimes used off-label as a treatment for cluster headache and to counteract the problems with sexual dysfunction experienced by some users of the selective serotonin reuptake inhibitor (SSRI) antidepressants.[1] Pramipexole has shown robust effects on pilot studies in a placebo-controlled proof of concept study in bipolar disorder.[2] It is also being investigated for the treatment of clinical depression and fibromyalgia.[3][4][5]

Contents

Pharmacology

Pramipexole acts as a selective non-ergoline D2, D3, and D4 dopamine receptor full agonist (see dopamine agonist) with highest affinity by 5-fold for D3.[6][7]

Parkinson's disease is a neurodegenerative disease affecting the substantia nigra, a component of the basal ganglia. The substantia nigra has a high quantity of dopaminergic neurons, which are nerve cells that release the neurotransmitter known as dopamine. When dopamine is released, it may activate dopamine receptors in the striatum, which is another component of the basal ganglia. When neurons of the substantia nigra deteriorate in Parkinson's disease, the striatum no longer properly receives dopamine signals. As a result, the basal ganglia can no longer regulate body movement effectively and motor function becomes impaired.

By acting as an agonist for the D2, D3, and D4 dopamine receptors, pramipexole may directly stimulate the underfunctioning dopamine receptors in the striatum, thereby restoring the dopamine signals needed for proper functioning of the basal ganglia.

Adverse effects

Some of the more common side effects of pramipexole include:[8][9]

  • Changes in appetite and weight
  • Dizziness, lightheadedness, or fainting, especially when standing up (orthostatic hypotension)
  • Drowsiness
  • Hallucinations (seeing, hearing, or feeling things that are not there)
  • Nausea
  • Insomnia
  • Twitching, twisting, or other unusual body movements
  • Unusual tiredness or weakness

Several unusual adverse effects of pramipexole (and related D3-preferring dopamine agonist medications such as ropinirole) may include compulsive gambling, hypersexuality, and overeating,[10] even in patients without any prior history of these behaviours.[11] Other compulsive behaviors, such as excessive shopping and even cross-dressing, have been reported.[12] These side effects are thought to be linked to the D3 activity of pramipexole, as D3 receptors are heavily expressed in brain regions involved in mood, behavior, and reward.[13]

References

  1. ^ DeBattista C, Solvason HB, Breen JA, Schatzberg AF. (2000). "Pramipexole augmentation of a selective serotonin reuptake inhibitor in the treatment of depression.". J Clin Psychopharmacol. 20 (2): 274–275. PMID 10770475.  
  2. ^ Biol Psychiatry. 2004 Jul 1;56(1):54-60. Pramipexole for bipolar II depression: a placebo-controlled proof of concept study.Zarate CA Jr, Payne JL, Singh J, Quiroz JA, Luckenbaugh DA, Denicoff KD, Charney DS, Manji HK.PMID: 15219473
  3. ^ Lattanzi L, Dell'Osso L, Cassano P, Pini S, Rucci P, Houck PR, Gemignani A, Battistini G, Bassi A, Abelli M, Cassano GB. (2002). "Pramipexole in treatment-resistant depression: a 16-week naturalistic study.". Bipolar Disord. 4 (5): 307–314. PMID 12479663.  
  4. ^ Cassano P, Lattanzi L, Soldani F, Navari S, Battistini G, Gemignani A, Cassano GB. (2004). "Pramipexole in treatment-resistant depression: an extended follow-up.". Depress Anxiety. 20 (3): 131–138. PMID 15549689.  
  5. ^ Holman AJ, Myers RR. (2005). "A randomized, double-blind, placebo-controlled trial of pramipexole, a dopamine agonist, in patients with fibromyalgia receiving concomitant medications.". Arthritis Rheum. 52 (8): 2495–2505. PMID 16052595.  
  6. ^ Piercey MF. (1998). "Pharmacology of pramipexole, a dopamine D3-preferring agonist useful in treating Parkinson's disease.". Clin Neuropharmacol. 21 (3): 141–151. PMID 19213730.  
  7. ^ Mierau J, Schneider F, Ensinger H, Chio C, Lajiness M, Huff R (1995). "Pramipexole binding and activation of cloned and expressed dopamine D2, D3 and D4 receptors.". Eur J Pharmacol 290 (1): 29–36. doi:10.1016/0922-4106(95)90013-6. PMID 7664822.  
  8. ^ "MedlinePlus Drug Information: Pramipexole (Systemic)". United States National Library of Medicine. http://www.nlm.nih.gov/medlineplus/druginfo/uspdi/203739.html. Retrieved 2006-09-27.  
  9. ^ "FDA Prescribing Information: Mirapex® (pramipexole dihydrochloride)". Food and Drug Administration (United States). http://www.accessdata.fda.gov/drugsatfda_docs/label/2008/020667s014s017s018lbl.pdf. Retrieved 2008-12-31.  
  10. ^ Wolters ECh, van der Werf YD, van den Heuvel OA. Parkinson's disease-related disorders in the impulsive-compulsive spectrum. Journal of Neurology. 2008 Sep;255 Suppl 5:48-56. PMID 18787882
  11. ^ Bostwick JM, Hecksel KA, Stevens SR, Bower JH, Ahlskog JE. Frequency of new-onset pathologic compulsive gambling or hypersexuality after drug treatment of idiopathic Parkinson disease. Mayo Clinic Proceedings. 2009 Apr;84(4):310-6. PMID 19339647
  12. ^ USA Today, Not Your Ordinary Side Effects, May 23, 2006
  13. ^ Dodd ML, Klos KJ, Bower JH, Geda YE, Josephs KA, Ahlskog JE (September 2005). "Pathological gambling caused by drugs used to treat Parkinson disease". Arch. Neurol. 62 (9): 1377–81. doi:10.1001/archneur.62.9.noc50009. PMID 16009751.  

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