Pramipexole is a research liquid indicated for treating early-stage Parkinson’s disease (PD) and restless legs syndrome (RLS).

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WHAT IS PRAMIPEXOLE?

It is a non-ergot dopamine agonist that is efficacious in treating various Parkinson’s symptoms, such as tremors, rigidity, and bradykinesia (slow movements) in animal test subjects.

Pramipexole exhibits a little affinity to some serotonergic and adrenergic receptors apart from dopaminergic activity.

STRUCTURE OF PRAMIPEXOLE

Molecular Formula: C₁₀H₁₇N₃ S

Molecular weight: 211.33 g/mol

CAS number: 104632-26-0

IUPAC name: (6S)-6-N-propyl-4,5,6,7-tetrahydro-1,3-benzothiazole-2,6-diamine

MECHANISM OF ACTION

Studies performed in animals show that pramipexole is a selective dopaminergic agonist with a minor agonistic activity at other receptors.

It shows specificity and potent activity in the D2 subfamily of dopamine receptors in vitro. It also has an affinity for the dopamine D3 receptor subtype rather than other subtypes.

Pramipexole is quickly absorbed, reaching plasma peak concentrations in approximately 2 hours. Its terminal half-life is between 8 – 12 hours, and it is primarily excreted by the kidneys, with 90% of a pramipexole dose recovered in urine, almost all as an unchanged drug.

PRAMIPEXOLE EFFECTS

Pramipexole’s benefits include the following:

• Relieving the symptoms of Parkinson’s Disease.
• Neuroprotection to dopamine neuron degeneration after ischemia or methamphetamine neurotoxicity.
• Treating cluster headaches, clinical depression, and fibromyalgia.

PRAMIPEXOLE SIDE EFFECTS

The adverse effects of pramipexole result from both peripheral and central dopaminergic stimulation. They include:

• Involuntary muscle movements
• Falling asleep suddenly
• Orthostatic hypotension
• Fainting
• Changes in mental status
• Hallucinations
• Psychosis
• Changes in posture

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References:

1. Mierau J, Schneider FJ, Ensinger HA, Chio CL, Lajiness ME, Huff RM: Pramipexole binding and activation of cloned and expressed dopamine D2, D3 and D4 receptors. Eur J Pharmacol. 1995 Jun 23;290(1):29-36. [PMID:7664822]

2. Massano J, Bhatia KP: Clinical approach to Parkinson’s disease: features, diagnosis, and principles of management. Cold Spring Harb Perspect Med. 2012 Jun;2(6):a008870. doi: 10.1101/cshperspect.a008870. [PMID:22675666]

3. Poewe W, Mahlknecht P: The clinical progression of Parkinson’s disease. Parkinsonism Relat Disord. 2009 Dec;15 Suppl 4:S28-32. doi: 10.1016/S1353-8020(09)70831-4. [PMID:20123553]

4. Authors unspecified: Global, regional, and national burden of Parkinson’s disease, 1990-2016: a systematic analysis for the Global Burden of Disease Study 2016. Lancet Neurol. 2018 Nov;17(11):939-953. doi: 10.1016/S1474-4422(18)30295-3. Epub 2018 Oct 1. [PMID:30287051]

1. Aiken CB: Pramipexole in psychiatry: a systematic review of the literature. J Clin Psychiatry. 2007 Aug;68(8):1230-6. [PMID:17854248]