Pramipexole

Structural formula
General
Non-proprietary name	Pramipexole
other names	( S ) -2-Amino-6- (propylamino) -4,5,6,7-tetrahydrobenzothiazole ( IUPAC )
Molecular formula	C 10 H 17 N 3 S
External identifiers / databases
CAS number 104632-26-0 (free base) 104632-25-9 (di hydrochloride ) 191217-81-9 (dihydrochloride monohydrate ) ECHA InfoCard 100.124.761 PubChem 119570 DrugBank DB00413 Wikidata Q421304
Drug information
ATC code	N04 BC05
Drug class	Parkinson's medication
Mechanism of action	Dopamine D 2/3 receptor agonist
properties
Molar mass	211.33 g · mol -1
Physical state	firmly
Melting point	296–301 ° C (dihydrochloride monohydrate)
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed GHS labeling of hazardous substances Caution H and P phrases H: 302-317-412 P: ?
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Pramipexole is a dopamine agonist and is used to treat Parkinson's disease , either in monotherapy or in combination with L- DOPA . Another indication is the symptomatic treatment of moderate to severe idiopathic Restless Legs Syndrome . Studies have also shown that pramipexole is effective in treating bipolar disorder .

Mode of action

Pramipexole is a dopamine agonist with high selectivity and specificity at D _2/3 - dopamine receptors . In the early stages of Parkinson's disease, pramipexole stimulates the presynaptic D2 autoreceptors and thereby inhibits excessive dopamine synthesis and release. In the late stage, pramipexole increases the dwindling dopamine synthesis by stimulating and modulating postsynaptic D ₂ and D ₃ receptors.

therapy

Pramipexole is recommended as standard therapy in the guidelines of the German Society for Neurology for patients with Parkinson's disease who are younger than 70 years. Pramipexole may relieve symptoms of depression in early-stage Parkinson's disease patients.

Risks and Side Effects

Since it has no ergoline structure, unlike the ergot alkaloids , there are no pleuropulmonary and retroperitoneal fibroses or peripheral vascular side effects to be feared.

Due to the occurrence of possible "sleep attacks", driving a vehicle or carrying out work with a potential risk of injury under nonergoline dopamine agonists (pramipexole, ropinirole ) is prohibited .

The term "sleep attack" denotes an increased need for sleep with, however, also reduced vigilance and increased sleepiness and is not identical with the term actual sleep attack in narcolepsy . It should also be taken into account that sleep disorders occur as a result of Parkinson's disease and that "sleep attacks" can also occur in healthy people. However, since treatment with pramipexole and ropinirole leads to increased indications of the above If you have had sleep attacks, driving a car is not recommended. A pathophysiological connection with the activation of D ₃ receptors is discussed.

Frequently, the occurrence of impulse control disorders (eg. B. gambling, shopping addiction).

Treatment of restless legs syndrome with pramipexole can worsen the symptoms (so-called rebound or augmentation effects ). Similar interfering effects are known from L- DOPA and other dopamine agonists.

Trade names

Monopreparations

Daquiran (A), Mirapexin (USA), Oprymea (A), Oprymea prolonged-release tablets (D, A), Sifrol (D, A, CH), Vasiprax (A), numerous generic drugs (A), Pexola (TR and some other countries ); numerous generics (D, since Dec. 2010)

Individual evidence

1. ^ The Merck Index . An Encyclopaedia of Chemicals, Drugs and Biologicals. 14th edition, 2006, p. 1323, ISBN 978-0-911910-00-1 .
2. ↑ There is not yet a harmonized classification for this substance . A labeling of (S) -2-amino-6-propylamino-4,5,6,7-tetrahydrobenzothiazole in the Classification and Labeling Inventory of the European Chemicals Agency (ECHA), accessed on July 11, 2020, is reproduced from a self-classification by the distributor .
3. ↑ Brin Dani F, F Vitetta, Gemignani Q: Restless legs syndrome: differential diagnosis and management with pramipexole . In: Clinical Interventions in Aging . 4, 2009, pp. 305-313. PMID 19750232 . PMC 2739631 (free full text).
4. ↑ Ferini-Strambi L, Aarskog D, Partinen M, et al. : Effect of pramipexole on RLS symptoms and sleep: a randomized, double-blind, placebo-controlled trial . In: Sleep Medicine . 9, No. 8, December 2008, pp. 874-881. doi : 10.1016 / j.sleep.2008.09.001 . PMID 18952497 .
5. ^ Zarate CA, Payne JL, Singh J, et al. : Pramipexole for bipolar II depression: a placebo-controlled proof of concept study . In: Biol. Psychiatry . 56, No. 1, July 2004, pp. 54-60. doi : 10.1016 / j.biopsych.2004.03.013 . PMID 15219473 .
6. ↑ Goldberg JF, Burdick KE, Endick CJ: Preliminary, randomized, double-blind, placebo-controlled trial of pramipexole added to mood stabilizers for treatment resistant bipolar depression. . In: American Journal of Psychiatry . 161, No. 3, March 2004, pp. 161: 564-566. PMID 14992985 .
7. ↑ Guy M. Goodwina, A. Martinez-Aranb, David C. Glahn c, Eduard Vieta b: Cognitive impairment in bipolar disorder: Neurodevelopment or neurodegeneration? An ECNP expert meeting report . In: European Neuropsychopharmacology . 18, No. 11, November 2008, pp. 787-793. PMID 18725178 .
8. ↑ Holloway RG, Shoulson I, Fahn S, et al. : Pramipexole vs levodopa as initial treatment for Parkinson disease: a 4-year randomized controlled trial . In: Archives of Neurology . 61, No. 7, July 2004, pp. 1044-1053. PMID 15262734 .
9. ↑ servant, HC Putzki, N. guidelines for diagnosis and therapy in neurology . Georg Thieme Verlag, 4th revised. Edition 2008. Short version online, page 20 , (PDF document; 241 kB).
10. ↑ Barone P., et al. Pramipexole for the treatment of depressive symptoms in patients with Parkinson's disease: a randomized, double-blind, placebo-controlled trial. In: The Lancet Neurology 2010 Jun; 9 (6): 573-580, PMID 20452823 .
11. ↑ Möller, JC et al. (2000): Sleep attacks in Parkinson's patients - a side effect of nonergoline dopamine agonists or a class effect of dopamimetics? In: The neurologist. (71): 670-676. doi : 10.1007 / s001150050645 .

This article is about a health issue. It is not used for self-diagnosis and does not replace a diagnosis by a doctor. Please note the information on health issues !