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Ropinirole
 
 
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Ropinirole (marketed under the brand names Requip and Ropark, in extended release form as Requip XL) is a non-ergoline
Ergoline

Ergoline is a chemical Chemical compound whose structural skeleton is contained in a diverse range of alkaloids and a few psychedelic Psychoactive drug ....
 dopamine agonist
Dopamine agonist

A dopamine agonist is a compound that activates dopamine receptors, stimulating the brain to make more of the dopamine neurotransmitter....
. It is manufactured by GlaxoSmithKline
GlaxoSmithKline

GlaxoSmithKline plc is a United Kingdom-based pharmaceutical industry, biological, and healthcare company. GSK is the world's second largest pharmaceutical company and a research-based company with a wide portfolio of pharmaceutical products covering anti-infectives, central nervous system, respiratory, gastro-intestinal/metabolic,...
 and Sun Pharmaceuticals. It is used in the treatment of Parkinson's disease
Parkinson's disease

Parkinson's disease is a degenerative disorder of the central nervous system that often impairs the sufferer's motor skills and speech, as well as other functions....
. Ropinirole is also one of two medications in the United States
United States

The United States of America is a Federal government constitutional republic comprising U.S. state and a federal district. The country is situated mostly in central North America, where its Contiguous United States and Washington, D.C., the Capital districts and territories, lie between the Pacific Ocean and Atlantic Oceans, Borders of the U...
 with an FDA
Food and Drug Administration

The U.S. Food and Drug Administration is an Government agency of the United States Department of Health and Human Services and is responsible for regulating and supervising the safety of foods, dietary supplements, Medications, vaccines, Biopharmaceutical, blood transfusion, medical devices, Electromagnetic radiation-emitting devices, veteri...
-approved indication for the treatment of restless legs syndrome
Restless legs syndrome

Restless legs syndrome is a condition that is characterized by an irresistible urge to move one's body to stop uncomfortable or odd sensations....
 (RLS), the other being pramipexole
Pramipexole

Pramipexole is a medication indicated for treating Parkinson's disease and restless legs syndrome . It is also sometimes used Off-label use as a treatment for cluster headache or to counteract the problems with low libido experienced by some users of SSRI antidepressant drugs....
. The discovery of the drug's utility in RLS has been used as a successful example of drug repurposing.

Ropinirole's patent expired in May 2008, and the drug is now available in generic
Generic drug

A generic drug is a medication which isproduced and distributed without patent protection. The generic drug may still have a patent on the formulation but not on the active ingredient....
 form.

Dosing
Requip (it is marketed as Adartrel in Europe for the restless legs syndrome indication and as Requip for the anti-Parkinson indication) is available in various preparations, ranging from the .25 mg tablet to the 5 mg tablet.






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Encyclopedia


Ropinirole (marketed under the brand names Requip and Ropark, in extended release form as Requip XL) is a non-ergoline
Ergoline

Ergoline is a chemical Chemical compound whose structural skeleton is contained in a diverse range of alkaloids and a few psychedelic Psychoactive drug ....
 dopamine agonist
Dopamine agonist

A dopamine agonist is a compound that activates dopamine receptors, stimulating the brain to make more of the dopamine neurotransmitter....
. It is manufactured by GlaxoSmithKline
GlaxoSmithKline

GlaxoSmithKline plc is a United Kingdom-based pharmaceutical industry, biological, and healthcare company. GSK is the world's second largest pharmaceutical company and a research-based company with a wide portfolio of pharmaceutical products covering anti-infectives, central nervous system, respiratory, gastro-intestinal/metabolic,...
 and Sun Pharmaceuticals. It is used in the treatment of Parkinson's disease
Parkinson's disease

Parkinson's disease is a degenerative disorder of the central nervous system that often impairs the sufferer's motor skills and speech, as well as other functions....
. Ropinirole is also one of two medications in the United States
United States

The United States of America is a Federal government constitutional republic comprising U.S. state and a federal district. The country is situated mostly in central North America, where its Contiguous United States and Washington, D.C., the Capital districts and territories, lie between the Pacific Ocean and Atlantic Oceans, Borders of the U...
 with an FDA
Food and Drug Administration

The U.S. Food and Drug Administration is an Government agency of the United States Department of Health and Human Services and is responsible for regulating and supervising the safety of foods, dietary supplements, Medications, vaccines, Biopharmaceutical, blood transfusion, medical devices, Electromagnetic radiation-emitting devices, veteri...
-approved indication for the treatment of restless legs syndrome
Restless legs syndrome

Restless legs syndrome is a condition that is characterized by an irresistible urge to move one's body to stop uncomfortable or odd sensations....
 (RLS), the other being pramipexole
Pramipexole

Pramipexole is a medication indicated for treating Parkinson's disease and restless legs syndrome . It is also sometimes used Off-label use as a treatment for cluster headache or to counteract the problems with low libido experienced by some users of SSRI antidepressant drugs....
. The discovery of the drug's utility in RLS has been used as a successful example of drug repurposing.

Ropinirole's patent expired in May 2008, and the drug is now available in generic
Generic drug

A generic drug is a medication which isproduced and distributed without patent protection. The generic drug may still have a patent on the formulation but not on the active ingredient....
 form.

Dosing


Requip (it is marketed as Adartrel in Europe for the restless legs syndrome indication and as Requip for the anti-Parkinson indication) is available in various preparations, ranging from the .25 mg tablet to the 5 mg tablet. The primary reason for such is dose titration. This implies that the person taking Requip has to closely interact and communicate with the primary care physician with regard to how much should actually be taken by the patient.

For restless legs Syndrome (RLS), the maximum recommended dose is 4 mg per day, taken 1 to 3 hours before bedtime. A 52-week open label study had a mean dosage of 1.90mg, once daily 1-3 hours before bedtime.

For Parkinson's disease (PD), the maximum recommended dose is 24 mg per day, taken in three separate doses spread throughout the day.

Mechanism


Ropinirole acts as an agonist at the D2
Dopamine receptor D2

Dopamine receptor D2, also known as DRD2, is a protein that is a receptor.The human protein is coded by the DRD2 gene.This gene encodes the D2 subtype of the dopamine receptor....
 and D3
Dopamine receptor D3

Dopamine receptor D3, also known as DRD3, is a human gene.This gene encodes the D3 subtype of the dopamine receptor....
 dopamine receptor subtypes, binding with higher affinity to D3 than to D2 or D4 and it has no affinity for D1
Dopamine receptor D1

Dopamine receptor D1, also known as DRD1, is a human gene.This gene encodes the D1 subtype of the dopamine receptor....
 receptors. It has medium in vitro
In vitro

In vitro refers to the technique of performing a given procedure in a controlled environment outside of a living organism. Some may argue that in vitro refers to a process that is created in a "test tube"; however, Robert Kail and John Cavanaugh on page 58 in the 4th edition of Human Development: A Life-Span View cite that in fact th...
 affinity to opioid receptor
Opioid receptor

Opioid receptors are a group of G-protein coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin....
s. Ropinirole is weakly active at the 5-HT2
5-HT2 receptor

5-HT2 receptors are a family of 5-HT receptors, with the following members:*5-HT2A receptors*5-HT2B receptors*5-HT2C receptorsMultiple receptor subtypes of serotonin neurotransmitters with multiple physiologic functions have been recognized....
, and a2
Alpha-2 adrenergic receptor

The a2 receptor is a type of adrenergic receptor....
 receptors and is said to have virtually no affinity to 5-HT1
5-HT1 receptor

In the field of neurochemistry, 5-HT1 receptors are a subfamily of 5-HT receptors which bind the neurotransmitter and Peripheral nervous system signal mediator serotonin, also known as 5-hydroxytryptamine ....
, benzodiazepine, GABA
GABA receptor

The GABA receptors are a class of Receptor that respond to the neurotransmitter Gamma-aminobutyric acid , the chief inhibitory neurotransmitter in the vertebrate central nervous system....
, muscarinic
Muscarinic acetylcholine receptor

Muscarinic receptors, or mAChRs, are G protein-coupled receptor acetylcholine receptors found in the plasma membranes of certain neurons and other Cell s....
, a1
Alpha-1 adrenergic receptor

The alpha-1 adrenergic receptor is an adrenergic receptor with the primary effect of vasoconstriction....
, and ß-adrenoreceptors.

Ropinirole is metabolized primarily by cytochrome P450 CYP1A2
CYP1A2

Cytochrome P450 1A2 , a member of the cytochrome P450 mixed-function oxidase system, is involved in the metabolism of xenobiotics in the body....
, and at doses higher than clinical, is also metabolized by CYP3A4
CYP3A4

Cytochrome P450 3A4 , a member of the cytochrome P450 mixed-function oxidase system, is one of the most important enzymes involved in the metabolism of xenobiotics in the body....
. At doses greater than 24mg, CYP2D6
CYP2D6

Cytochrome P450 2D6 , a member of the cytochrome P450 mixed-function oxidase system, is one of the most important enzymes involved in the metabolism of xenobiotics in the body....
 may be inhibited, although this has only been tested in vitro
In vitro

In vitro refers to the technique of performing a given procedure in a controlled environment outside of a living organism. Some may argue that in vitro refers to a process that is created in a "test tube"; however, Robert Kail and John Cavanaugh on page 58 in the 4th edition of Human Development: A Life-Span View cite that in fact th...
.

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