pramipexole

[PR(OPYL) + AMI(NO) + pex-, of unknown meaning + (THIAZ)OLE.]

Brand names: Mirapex®

Chemical formula:

Español:
• Pramipexol Diclorhidrato, Tableta oral

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?

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
•dream disturbances or trouble with sleeping
•fainting spells
•hallucinations
•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.

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	C10H17N3S
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:link, US FDA:link
Pregnancy cat.	B3(AU) C(US)
Legal status	℞ Prescription only
Routes	Oral
Y(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 1 Pharmacology 2 Adverse effects 3 References 4 External links

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. 

External links

• Mirapex.com - Manufacturer's website

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