Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C10H17N3S.2ClH |
Molecular Weight | 284.249 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.Cl.CCCN[C@H]1CCC2=C(C1)SC(N)=N2
InChI
InChIKey=QMNWXHSYPXQFSK-KLXURFKVSA-N
InChI=1S/C10H17N3S.2ClH/c1-2-5-12-7-3-4-8-9(6-7)14-10(11)13-8;;/h7,12H,2-6H2,1H3,(H2,11,13);2*1H/t7-;;/m0../s1
DescriptionSources: http://www.drugbank.ca/drugs/DB00413Curator's Comment: Description was created based on several sources, including
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/020667s014s017s018lbl.pdf
Sources: http://www.drugbank.ca/drugs/DB00413
Curator's Comment: Description was created based on several sources, including
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/020667s014s017s018lbl.pdf
Pramipexole is a nonergot dopamine agonist with high relative in vitro specificity and full intrinsic activity at the D2 subfamily of dopamine receptors, binding with higher affinity to D3 than to D2 or D4 receptor subtypes. The relevance of D3 receptor binding in Parkinson's disease is unknown. The precise mechanism of action of Pramipexole as a treatment for Parkinson's disease is unknown, although it is believed to be related to its ability to stimulate dopamine receptors in the striatum. This conclusion is supported by electrophysiologic studies in animals that have demonstrated that Pramipexole influences striatal neuronal firing rates via activation of dopamine receptors in the striatum and the substantia nigra, the site of neurons that send projections to the striatum.
Pramipexole is used for the treatment of signs and symptoms of idiopathic Parkinson's disease.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL234 Sources: http://www.drugbank.ca/drugs/DB00413 |
1.5 nM [EC50] | ||
Target ID: CHEMBL217 Sources: http://www.drugbank.ca/drugs/DB00413 |
27.0 nM [EC50] | ||
Target ID: CHEMBL219 Sources: http://www.drugbank.ca/drugs/DB00413 |
15.0 nM [EC50] | ||
Target ID: CHEMBL205 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24289818 |
4.81 µM [IC50] | ||
Target ID: CHEMBL261 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24289818 |
5.37 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | MIRAPEX Approved UseMirapex® (pramipexole dihydrochloride) tablets are indicated for the treatment of the signs and symptoms of idiopathic Parkinson's disease.
MIRAPEX tablets are indicated for the treatment of moderate-to-severe primary Restless Legs Syndrome (RLS). Launch Date1997 |
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Primary | MIRAPEX Approved UseMirapex® (pramipexole dihydrochloride) tablets are indicated for the treatment of the signs and symptoms of idiopathic Parkinson's disease.
MIRAPEX tablets are indicated for the treatment of moderate-to-severe primary Restless Legs Syndrome (RLS). Launch Date1997 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
0.268 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/20110012 |
0.375 mg single, oral dose: 0.375 mg route of administration: Oral experiment type: SINGLE co-administered: |
PRAMIPEXOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
5.29 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/20110012 |
0.375 mg single, oral dose: 0.375 mg route of administration: Oral experiment type: SINGLE co-administered: |
PRAMIPEXOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
31.2 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/20110012 |
0.375 mg single, oral dose: 0.375 mg route of administration: Oral experiment type: SINGLE co-administered: |
PRAMIPEXOLE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
1.5 mg 3 times / day multiple, oral (max) Recommended Dose: 1.5 mg, 3 times / day Route: oral Route: multiple Dose: 1.5 mg, 3 times / day Sources: Page: p.740 |
unhealthy, 61.6 n = 391 Health Status: unhealthy Condition: Parkinson's disease Age Group: 61.6 Sex: M+F Population Size: 391 Sources: Page: p.740 |
Disc. AE: Hallucination, Hypotension... AEs leading to discontinuation/dose reduction: Hallucination (1.3%) Sources: Page: p.740Hypotension (0.5%) Peripheral edema (0.5%) |
1.5 mg 3 times / day multiple, oral (max) Recommended Dose: 1.5 mg, 3 times / day Route: oral Route: multiple Dose: 1.5 mg, 3 times / day Sources: Page: p.727 |
unhealthy, 62.7 n = 163 Health Status: unhealthy Condition: Parkinson's disease Age Group: 62.7 Sex: M+F Population Size: 163 Sources: Page: p.727 |
Disc. AE: Hallucinations, Sleepiness... AEs leading to discontinuation/dose reduction: Hallucinations (4.3%) Sources: Page: p.727Sleepiness (3%) Dizziness (2.5%) Memory loss (1.2%) Paranoia (0.6%) |
2 mg 3 times / day multiple, oral Highest studied dose Dose: 2 mg, 3 times / day Route: oral Route: multiple Dose: 2 mg, 3 times / day Sources: Page: p.128 |
unhealthy, 62.8 n = 55 Health Status: unhealthy Condition: Parkinson's disease Age Group: 62.8 Sex: M+F Population Size: 55 Sources: Page: p.128 |
DLT: Drowsiness, Muscle spasms... Dose limiting toxicities: Drowsiness (3.6%) Sources: Page: p.128Muscle spasms (1.8%) Insomnia (1.8%) Vertigo (1.8%) Ankle swelling (1.8%) Hallucination (3.6%) Nausea (1.8%) |
1.5 mg 3 times / day multiple, oral (max) Recommended Dose: 1.5 mg, 3 times / day Route: oral Route: multiple Dose: 1.5 mg, 3 times / day Sources: Page: p.740 |
unhealthy, 63 n = 511 Health Status: unhealthy Condition: Parkinson's disease Age Group: 63 Sex: M+F Population Size: 511 Sources: Page: p.740 |
Disc. AE: Nausea, Hallucination... AEs leading to discontinuation/dose reduction: Nausea (0.6%) Sources: Page: p.740Hallucination (1%) Peripheral edema (0.8%) Abdominal pain upper (0.6%) Myocardial infarction (0.6%) Pneumonia (0.6%) Vomiting (0.6%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Hypotension | 0.5% Disc. AE |
1.5 mg 3 times / day multiple, oral (max) Recommended Dose: 1.5 mg, 3 times / day Route: oral Route: multiple Dose: 1.5 mg, 3 times / day Sources: Page: p.740 |
unhealthy, 61.6 n = 391 Health Status: unhealthy Condition: Parkinson's disease Age Group: 61.6 Sex: M+F Population Size: 391 Sources: Page: p.740 |
Peripheral edema | 0.5% Disc. AE |
1.5 mg 3 times / day multiple, oral (max) Recommended Dose: 1.5 mg, 3 times / day Route: oral Route: multiple Dose: 1.5 mg, 3 times / day Sources: Page: p.740 |
unhealthy, 61.6 n = 391 Health Status: unhealthy Condition: Parkinson's disease Age Group: 61.6 Sex: M+F Population Size: 391 Sources: Page: p.740 |
Hallucination | 1.3% Disc. AE |
1.5 mg 3 times / day multiple, oral (max) Recommended Dose: 1.5 mg, 3 times / day Route: oral Route: multiple Dose: 1.5 mg, 3 times / day Sources: Page: p.740 |
unhealthy, 61.6 n = 391 Health Status: unhealthy Condition: Parkinson's disease Age Group: 61.6 Sex: M+F Population Size: 391 Sources: Page: p.740 |
Paranoia | 0.6% Disc. AE |
1.5 mg 3 times / day multiple, oral (max) Recommended Dose: 1.5 mg, 3 times / day Route: oral Route: multiple Dose: 1.5 mg, 3 times / day Sources: Page: p.727 |
unhealthy, 62.7 n = 163 Health Status: unhealthy Condition: Parkinson's disease Age Group: 62.7 Sex: M+F Population Size: 163 Sources: Page: p.727 |
Memory loss | 1.2% Disc. AE |
1.5 mg 3 times / day multiple, oral (max) Recommended Dose: 1.5 mg, 3 times / day Route: oral Route: multiple Dose: 1.5 mg, 3 times / day Sources: Page: p.727 |
unhealthy, 62.7 n = 163 Health Status: unhealthy Condition: Parkinson's disease Age Group: 62.7 Sex: M+F Population Size: 163 Sources: Page: p.727 |
Dizziness | 2.5% Disc. AE |
1.5 mg 3 times / day multiple, oral (max) Recommended Dose: 1.5 mg, 3 times / day Route: oral Route: multiple Dose: 1.5 mg, 3 times / day Sources: Page: p.727 |
unhealthy, 62.7 n = 163 Health Status: unhealthy Condition: Parkinson's disease Age Group: 62.7 Sex: M+F Population Size: 163 Sources: Page: p.727 |
Sleepiness | 3% Disc. AE |
1.5 mg 3 times / day multiple, oral (max) Recommended Dose: 1.5 mg, 3 times / day Route: oral Route: multiple Dose: 1.5 mg, 3 times / day Sources: Page: p.727 |
unhealthy, 62.7 n = 163 Health Status: unhealthy Condition: Parkinson's disease Age Group: 62.7 Sex: M+F Population Size: 163 Sources: Page: p.727 |
Hallucinations | 4.3% Disc. AE |
1.5 mg 3 times / day multiple, oral (max) Recommended Dose: 1.5 mg, 3 times / day Route: oral Route: multiple Dose: 1.5 mg, 3 times / day Sources: Page: p.727 |
unhealthy, 62.7 n = 163 Health Status: unhealthy Condition: Parkinson's disease Age Group: 62.7 Sex: M+F Population Size: 163 Sources: Page: p.727 |
Ankle swelling | 1.8% DLT |
2 mg 3 times / day multiple, oral Highest studied dose Dose: 2 mg, 3 times / day Route: oral Route: multiple Dose: 2 mg, 3 times / day Sources: Page: p.128 |
unhealthy, 62.8 n = 55 Health Status: unhealthy Condition: Parkinson's disease Age Group: 62.8 Sex: M+F Population Size: 55 Sources: Page: p.128 |
Insomnia | 1.8% DLT |
2 mg 3 times / day multiple, oral Highest studied dose Dose: 2 mg, 3 times / day Route: oral Route: multiple Dose: 2 mg, 3 times / day Sources: Page: p.128 |
unhealthy, 62.8 n = 55 Health Status: unhealthy Condition: Parkinson's disease Age Group: 62.8 Sex: M+F Population Size: 55 Sources: Page: p.128 |
Muscle spasms | 1.8% DLT |
2 mg 3 times / day multiple, oral Highest studied dose Dose: 2 mg, 3 times / day Route: oral Route: multiple Dose: 2 mg, 3 times / day Sources: Page: p.128 |
unhealthy, 62.8 n = 55 Health Status: unhealthy Condition: Parkinson's disease Age Group: 62.8 Sex: M+F Population Size: 55 Sources: Page: p.128 |
Nausea | 1.8% DLT |
2 mg 3 times / day multiple, oral Highest studied dose Dose: 2 mg, 3 times / day Route: oral Route: multiple Dose: 2 mg, 3 times / day Sources: Page: p.128 |
unhealthy, 62.8 n = 55 Health Status: unhealthy Condition: Parkinson's disease Age Group: 62.8 Sex: M+F Population Size: 55 Sources: Page: p.128 |
Vertigo | 1.8% DLT |
2 mg 3 times / day multiple, oral Highest studied dose Dose: 2 mg, 3 times / day Route: oral Route: multiple Dose: 2 mg, 3 times / day Sources: Page: p.128 |
unhealthy, 62.8 n = 55 Health Status: unhealthy Condition: Parkinson's disease Age Group: 62.8 Sex: M+F Population Size: 55 Sources: Page: p.128 |
Drowsiness | 3.6% DLT |
2 mg 3 times / day multiple, oral Highest studied dose Dose: 2 mg, 3 times / day Route: oral Route: multiple Dose: 2 mg, 3 times / day Sources: Page: p.128 |
unhealthy, 62.8 n = 55 Health Status: unhealthy Condition: Parkinson's disease Age Group: 62.8 Sex: M+F Population Size: 55 Sources: Page: p.128 |
Hallucination | 3.6% DLT |
2 mg 3 times / day multiple, oral Highest studied dose Dose: 2 mg, 3 times / day Route: oral Route: multiple Dose: 2 mg, 3 times / day Sources: Page: p.128 |
unhealthy, 62.8 n = 55 Health Status: unhealthy Condition: Parkinson's disease Age Group: 62.8 Sex: M+F Population Size: 55 Sources: Page: p.128 |
Abdominal pain upper | 0.6% Disc. AE |
1.5 mg 3 times / day multiple, oral (max) Recommended Dose: 1.5 mg, 3 times / day Route: oral Route: multiple Dose: 1.5 mg, 3 times / day Sources: Page: p.740 |
unhealthy, 63 n = 511 Health Status: unhealthy Condition: Parkinson's disease Age Group: 63 Sex: M+F Population Size: 511 Sources: Page: p.740 |
Myocardial infarction | 0.6% Disc. AE |
1.5 mg 3 times / day multiple, oral (max) Recommended Dose: 1.5 mg, 3 times / day Route: oral Route: multiple Dose: 1.5 mg, 3 times / day Sources: Page: p.740 |
unhealthy, 63 n = 511 Health Status: unhealthy Condition: Parkinson's disease Age Group: 63 Sex: M+F Population Size: 511 Sources: Page: p.740 |
Nausea | 0.6% Disc. AE |
1.5 mg 3 times / day multiple, oral (max) Recommended Dose: 1.5 mg, 3 times / day Route: oral Route: multiple Dose: 1.5 mg, 3 times / day Sources: Page: p.740 |
unhealthy, 63 n = 511 Health Status: unhealthy Condition: Parkinson's disease Age Group: 63 Sex: M+F Population Size: 511 Sources: Page: p.740 |
Pneumonia | 0.6% Disc. AE |
1.5 mg 3 times / day multiple, oral (max) Recommended Dose: 1.5 mg, 3 times / day Route: oral Route: multiple Dose: 1.5 mg, 3 times / day Sources: Page: p.740 |
unhealthy, 63 n = 511 Health Status: unhealthy Condition: Parkinson's disease Age Group: 63 Sex: M+F Population Size: 511 Sources: Page: p.740 |
Vomiting | 0.6% Disc. AE |
1.5 mg 3 times / day multiple, oral (max) Recommended Dose: 1.5 mg, 3 times / day Route: oral Route: multiple Dose: 1.5 mg, 3 times / day Sources: Page: p.740 |
unhealthy, 63 n = 511 Health Status: unhealthy Condition: Parkinson's disease Age Group: 63 Sex: M+F Population Size: 511 Sources: Page: p.740 |
Peripheral edema | 0.8% Disc. AE |
1.5 mg 3 times / day multiple, oral (max) Recommended Dose: 1.5 mg, 3 times / day Route: oral Route: multiple Dose: 1.5 mg, 3 times / day Sources: Page: p.740 |
unhealthy, 63 n = 511 Health Status: unhealthy Condition: Parkinson's disease Age Group: 63 Sex: M+F Population Size: 511 Sources: Page: p.740 |
Hallucination | 1% Disc. AE |
1.5 mg 3 times / day multiple, oral (max) Recommended Dose: 1.5 mg, 3 times / day Route: oral Route: multiple Dose: 1.5 mg, 3 times / day Sources: Page: p.740 |
unhealthy, 63 n = 511 Health Status: unhealthy Condition: Parkinson's disease Age Group: 63 Sex: M+F Population Size: 511 Sources: Page: p.740 |
PubMed
Title | Date | PubMed |
---|---|---|
Are dopamine receptor agonists neuroprotective in Parkinson's disease? | 2001 |
|
Switching from pergolide to pramipexole in patients with Parkinson's disease. | 2001 |
|
Release and aggregation of cytochrome c and alpha-synuclein are inhibited by the antiparkinsonian drugs, talipexole and pramipexole. | 2001 Apr 6 |
|
Influence of L-dopa and pramipexole on striatal dopamine transporter in early PD. | 2001 Jun 12 |
|
Antagonism of the discriminative stimulus effects of (+)-7-OH-DPAT by remoxipride but not PNU-99194A. | 2001 Mar |
|
Sleep disorders in Parkinson's disease: epidemiology and management. | 2002 |
|
'Sleep attacks' or 'unintended sleep episodes' occur with dopamine agonists: is this a class effect? | 2002 |
|
Dopamine transporter brain imaging to assess the effects of pramipexole vs levodopa on Parkinson disease progression. | 2002 Apr 3 |
|
[Rhabdomyolysis as a complication of Parkinson's disease]. | 2002 Jan-Feb |
|
Pramipexole ameliorates neurologic and psychiatric symptoms in a Westphal variant of Huntington's disease. | 2002 Jan-Feb |
|
Pramipexole in patients with Parkinson's disease and marked drug resistant tremor: a randomised, double blind, placebo controlled multicentre study. | 2002 Jun |
|
Sleep attacks in patients taking dopamine agonists: review. | 2002 Jun 22 |
|
A case of Parkinsonism due to lithium intoxication: treatment with Pramipexole. | 2002 May |
|
Restless legs syndrome augmentation and pramipexole treatment. | 2002 Nov |
|
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. | 2002 Nov |
|
Neuroprotection in idiopathic Parkinson's disease. | 2002 Oct |
|
Pramipexole in Parkinson's disease. A short-term study using the combined levodopa-dopamine agonist test. | 2002 Oct-Dec |
|
Pramipexole in routine clinical practice: a prospective observational trial in Parkinson's disease. | 2003 |
|
Cabergoline, pramipexole and ropinirole used as monotherapy in early Parkinson's disease: an evidence-based comparison. | 2003 |
|
Comparison of the risk of adverse events with pramipexole and ropinirole in patients with Parkinson's disease: a meta-analysis. | 2003 |
|
Dopamine agonists induce episodes of irresistible daytime sleepiness. | 2003 |
|
Pramipexole in comparison to l-dopa: a neuropsychological study. | 2003 Apr |
|
Piribedil-induced sleep attacks in Parkinson's disease. | 2003 Feb |
|
Sleepwalking and sleep terrors in prepubertal children: what triggers them? | 2003 Jan |
|
Dual dopamine agonist treatment in Parkinson's disease. | 2003 Jul |
|
Dopamine receptor agonists in current clinical use: comparative dopamine receptor binding profiles defined in the human striatum. | 2003 Oct |
|
Current treatment options for restless legs syndrome. | 2003 Oct |
Sample Use Guides
Dosages should be increased gradually from a starting dose of 0.375 mg/day given in three divided doses and should not be increased more frequently than every 5 to 7 days.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26213307
Pramipexole suppressed H2O2-induced ARPE-19 cell death in vitro at concentrations of 10(-6) M or higher.
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DTXSID90146623
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119569
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100000089409
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SUB25210
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4R2HD0M28N
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104632-25-9
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m9095
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ACTIVE MOIETY
SUBSTANCE RECORD