pramipexole
American Heritage Dictionary:
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pram·i·pex·ole
(prăm'ə-pĕk'sōl') 
n.
A dopamine agonist used in the treatment of Parkinson's disease.
n.
A dopamine agonist used in the treatment of Parkinson's disease.
[PR(OPYL) + AMI(NO) + pex-, of unknown meaning + (THIAZ)OLE.]
Drug Info:
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Pramipexole
Brand names: Mirapex®
Chemical formula:
- Drug Forms:
- Pramipexole Dihydrochloride Oral tablet (below)
- Pramipexole Dihydrochloride Oral tablet, extended-release
- Espa�ol:
- Pramipexol Diclorhidrato, Tableta oral
- Pramipexol Diclorhidrato, Tableta oral de liberación prolongada
Pramipexole Dihydrochloride Oral tablet
What is this medicine?
PRAMIPEXOLE (pra mi PEX ole) is used to treat symptoms of Parkinson's disease. It is also used to treat Restless Legs Syndrome.
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
•dizzy or fainting spells
•heart disease
•kidney disease
•low blood pressure
•sleeping problems
•an unusual or allergic reaction to pramipexole, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding
How should I use this medicine?
Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. Take with food. Take your doses at regular intervals. Do not take your medicine more often than directed. Do not stop taking except on the advice of your doctor or health care professional.
Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.
What if I miss a dose?
If you miss a dose, take it as soon as you can. If it is almost time for your next dose (within 2 hours), take only that dose. Do not take double or extra doses.What may interact with this medicine?
•amantadine
•cimetidine
•diltiazem
•medicines for mental problems or psychotic disturbances
•medicines for sleep
•metoclopramide
•quinidine or quinine
•ranitidine
•triamterene
•verapamil
This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.
What should I watch for while using this medicine?
Visit your doctor or health care professional for regular checks on your progress. It may be several weeks or months before you feel the full effect of this medicine. Continue to take your medicine on a regular schedule.
You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this drug affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. If you find that you have sudden feelings of wanting to sleep during normal activities, like cooking, watching television, or while driving or riding in a car, you should contact your health care professional.
Your mouth may get dry. Chewing sugarless gum or sucking hard candy, and drinking plenty of water may help. Contact your doctor if the problem does not go away or is severe.
There have been reports of increased sexual urges or other strong urges such as gambling while taking some medicines for Parkinson's disease. If you experience any of these urges while taking this medicine, you should report it to your health care provider as soon as possible.
You should check your skin often for changes to moles and new growths while taking this medicine. Call your doctor if you notice any of these changes.
What side effects may I notice from receiving this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
•confusion
•double vision or other vision problems
•fainting spells
•falling asleep during normal activities like driving
•hallucination, loss of contact with reality
•mental changes
•muscle pain or severe muscle weakness
•uncontrollable movements of the arms, face, hands, head, mouth, shoulders, or upper body
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•constipation
•frequent urination
•mild weakness
•nausea
This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Where should I keep my medicine?
Keep out of the reach of children.
Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Protect from light. Throw away any unused medicine after the expiration date.
Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
Oxford A-Z of Medicinal Drugs:
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pramipexole
A dopamine receptor agonist used alone or as an adjunct to levodopa in the treatment of Parkinson's disease (see antiparkinsonian drugs). It is also licensed for use in restless legs syndrome. Pramipexole is available as tablets on prescription only.
Side effects:
include visual hallucinations, movement disorders, impulsive behaviour, somnolence and suddenly falling asleep, a fall in blood pressure, nausea, and constipation.
Precautions:
pramipexole should not be taken by women who are pregnant or breastfeeding. It should be used with caution in people with psychotic disorders, kidney disease, or severe cardiovascular disease. People taking pramipexole should avoid driving and operating machinary. Dosage should be reduced gradually at the end of treatment.
Interactions with other drugs:
Antipsychotics: antagonize the effect of pramipexole.
Cimetidine increases the plasma concentration of pramipexole.
Methyldopa antagonizes the effect of pramipexole.
Proprietary preparation:
Mirapexin.
| povidone–iodine, povidone, potassium-sparing diuretics | |
| pramocaine hydrochloride, prasugrel hydrochloride, pravastatin |
Wikipedia on Answers.com:
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Pramipexole
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|---|---|
| Systematic (IUPAC) name | |
| (S)-N6-propyl-4,5,6,7-tetrahydro-1,3-benzothiazole-2,6-diamine | |
| Clinical data | |
| Trade names | Mirapex |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a697029 |
| Pregnancy cat. | B3 (AU) C (US) |
| Legal status | ℞ Prescription only |
| Routes | Oral |
| Pharmacokinetic data | |
| Bioavailability | >90% |
| Protein binding | 15% |
| Half-life | 8-12 hours |
| Excretion | Urine (90%), Feces (2%) |
| Identifiers | |
| CAS number | 104632-26-0  |
| ATC code | N04BC05 |
| PubChem | CID 119570 |
| IUPHAR ligand | 953 |
| DrugBank | DB00413 |
| ChemSpider | 106770 |
| UNII | 83619PEU5T |
| KEGG | D05575 |
| ChEBI | CHEBI:8356 |
| ChEMBL | CHEMBL301265 |
| Chemical data | |
| Formula | C10H17N3S |
| Mol. mass | 211.324 g/mol |
| SMILES | eMolecules & PubChem |
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Pramipexole (Mirapex, Mirapexin, Sifrol) is a non-ergoline dopamine agonist indicated for treating early-stage Parkinson's disease (PD) and restless legs syndrome (RLS).[1] It is also sometimes used off-label as a treatment for cluster headache and to counteract problems with sexual dysfunction experienced by some users of selective serotonin reuptake inhibitor (SSRI) antidepressants.[2] Pramipexole has shown robust effects on pilot studies in a placebo-controlled proof of concept study in bipolar disorder.[3] It is also being investigated for the treatment of clinical depression and fibromyalgia.[4][5][6]
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Contents
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Pharmacology
Pramipexole acts as a partial/full agonist at the following receptors:[7][8]
- D2S receptor (Ki = 3.9 nM; IA = 130%)
- D2L receptor (Ki = 2.2 nM; IA = 70%)
- D3 receptor (Ki = 0.5 nM; IA = 70%)
- D4 receptor (Ki = 5.1 nM; IA = 42%)
Pramipexole also possesses low/insignificant affinity (500-10,000 nM) for the 5-HT1A, 5-HT1B, 5-HT1D, and α2-adrenergic receptors.[7][9] It has negligible affinity (>10,000 nM) for the D1, D5, 5-HT2, α1-adrenergic, β-adrenergic, H1, and mACh receptors.[7][9] All sites assayed were done using human tissues.[7][8]
While pramipexole is used clinically (see below), its D3-preferring receptor binding profile has made it a popular tool compound for preclinical research. For example, pramipexole has been used (in combination with D2- and or D3- preferring antagonists) to interrogate the role of D3-receptor function in rodent models and tasks for neuropsychiatric disorders.[10] Of note, it appears that pramipexole, in addition to having effects on dopamine D3 receptors, may also affect mitochondrial function via a mechanism that remains less understood. A pharmacological approach to separate dopaminergic from non-dopaminergic (e.g. mitochondrial) effects of pramipexole has been to study the effects of the R-stereoisomer of pramipexole (which has much lower affinity to the dopamine receptors when compared to the S-isormer) side-by-side with the effects of the S-isomer. [11]
Parkinson's disease is a neurodegenerative disease affecting the substantia nigra, 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.
Bipolar depression
In a single controlled study of twenty one patients, pramipexole was found to be highly effective in the treatment of bipolar depression. Treatment was initiated at 0.125mg t.i.d. and increased at a rate of 0.125mg t.i.d. to a limit of 4.5mg qd until the patients' condition satisfactorily responded to the medication or they could not abide the side effects. The final average dosage was 1.7mg ± .90mg qd. The incidence of hypomania in the treatment group was no greater than in the control group.[3]
Unipolar depression
In one controlled study, pramipexole was shown be efficacious in the treatment of unipolar depression.[12]cited in[3]
Side effects
Common side effects of pramipexole may include:[13][14]
- Headache
- Hyperalgesia (body aches and pains)
- Nausea and vomiting
- Sedation and somnolence
- Decreased appetite and subsequent weight loss
- Orthostatic hypotension (resulting in dizziness, lightheadedness, and possibly fainting, especially when standing up)
- Insomnia
- Hallucinations (seeing, hearing, smelling, tasting or feeling things that are not there)
- 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,[15] even in patients without any prior history of these behaviours.[16] These behaviors have been reported to manifest in almost 14% of patients on DA agonist therapies. Other compulsive behaviors, such as excessive shopping and compulsive cross-dressing, have been reported.[17] L-DOPA is an indirect acting DA agonist with no specificity for any receptor subtypes. As it is the precursor for dopamine it is rarely associated with these disorders. 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.[18]
Chemistry
Pramiprexole can be synthesized from a cyclohexanone derivative by the following route:[19] 
See also
- Dexpramipexole, the enantiomer of pramiprexole
- Piribedil
- Ropinirole
- Rotigotine
References
- ^ National Prescribing Service (2009). "Pramipexole for Parkinson's Disease". Medicines Update. Available at http://www.nps.org.au/consumers/publications/medicine_update/issues/Pramipexole_for_Parkinsons_disease
- ^ 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. doi:10.1097/00004714-200004000-00029. PMID 10770475.
- ^ a b c Zarate CA, Payne JL, Singh J, et al. (July 2004). "Pramipexole for bipolar II depression: a placebo-controlled proof of concept study". Biol. Psychiatry 56 (1): 54–60. doi:10.1016/j.biopsych.2004.03.013. PMID 15219473.
- ^ 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. doi:10.1034/j.1399-5618.2002.01171.x. PMID 12479663.
- ^ Cassano P, Lattanzi L, Soldani F, Navari S, Battistini G, Gemignani A, Cassano GB. (2004). "Pramipexole in treatment-resistant depression: an extended follow-up.". Depression and Anxiety 20 (3): 131–138. doi:10.1002/da.20038. PMID 15549689.
- ^ 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. doi:10.1002/art.21191. PMID 16052595.
- ^ a b c d Kvernmo T, Härtter S, Burger E (August 2006). "A review of the receptor-binding and pharmacokinetic properties of dopamine agonists". Clinical Therapeutics 28 (8): 1065–78. doi:10.1016/j.clinthera.2006.08.004. PMID 16982285. http://linkinghub.elsevier.com/retrieve/pii/S0149-2918(06)00184-6.
- ^ a b Newman-Tancredi A, Cussac D, Audinot V, et al. (November 2002). "Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor". The Journal of Pharmacology and Experimental Therapeutics 303 (2): 805–14. doi:10.1124/jpet.102.039875. PMID 12388667. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=12388667.
- ^ a b Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A (November 2002). "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". The Journal of Pharmacology and Experimental Therapeutics 303 (2): 791–804. doi:10.1124/jpet.102.039867. PMID 12388666. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=12388666.
- ^ Weber, M; Chang W, Breier M, Ko D, Swerdlow NR (December 2008). "Heritable strain differences in sensitivity to the startle gating-disruptive effects of D2 but not D3 receptor stimulation". Behav Pharmacol 19 (8): 786-795. doi:10.1097/FBP.0b013e32831c3b2b. http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3255557/?tool=pubmed.
- ^ Chang, W; Weber M, Breier MR, Saint Marie RL, Hines SR, Swerdlow NR (February 2012). "Stereochemical and neuroanatomical selectivity of pramipexole effects on sensorimotor gating in rats". Brain Res. doi:10.1016/j.brainres.2011.12.007. PMID 22227455. http://www.sciencedirect.com/science/article/pii/S0006899311021834.
- ^ Corrigan MH, Denahan AQ, Wright CE, Ragual RJ, Evans DL (2000): Comparison of pramipexole, fluoxetine, and placebo in patients with major depression. Depress Anxiety 11:58 –65.
- ^ "MedlinePlus Drug Information: Pramipexole (Systemic)". United States National Library of Medicine. Archived from the original on 2006-09-26. http://web.archive.org/web/20060926023858/http://www.nlm.nih.gov/medlineplus/druginfo/uspdi/203739.html. Retrieved 2006-09-27.
- ^ "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.
- ^ Wolters ECh, van der Werf YD, van den Heuvel OA (September 2008). "Parkinson's disease-related disorders in the impulsive-compulsive spectrum". J. Neurol. 255 Suppl 5: 48–56. doi:10.1007/s00415-008-5010-5. PMID 18787882.
- ^ Bostwick JM, Hecksel KA, Stevens SR, Bower JH, Ahlskog JE (April 2009). "Frequency of new-onset pathologic compulsive gambling or hypersexuality after drug treatment of idiopathic Parkinson disease". Mayo Clin. Proc. 84 (4): 310–6. doi:10.4065/84.4.310. PMC 2665974. PMID 19339647. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2665974.
- ^ USA Today, Not Your Ordinary Side Effects, May 23, 2006
- ^ 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.
- ^ Schneider, Claus S.; Mierau, Joachim (1987). "Dopamine autoreceptor agonists: resolution and pharmacological activity of 2,6-diaminotetrahydrobenzothiazole and an aminothiazole analog of apomorphine". Journal of Medicinal Chemistry 30 (3): 494–8. doi:10.1021/jm00386a009. PMID 3820220.
External links
- Mirapex.com - Manufacturer's website
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Copyrights:
American Heritage Dictionary
The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2009. Published by Houghton Mifflin Company. All rights reserved.
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Oxford A-Z of Medicinal Drugs
Market University Press. © 2000, 2003, 2010 An A-Z of Medicinal Drugs. All rights reserved.
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