Side effects of requip

Ropinirole

Generic Name: ropinirole (oral) (roe PIN i role)
Brand Name: Requip, Requip XL, ReQuip Follow on Pack, ReQuip Starter Pack, Repreve, Requip Starter Kit

Medically reviewed by Drugs.com on Mar 18, 2019 – Written by Cerner Multum

  • Overview
  • Side Effects
  • Dosage
  • Professional
  • Tips
  • Interactions
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What is ropinirole?

Ropinirole has some of the same effects as a chemical called dopamine, which occurs naturally in your body. Low levels of dopamine in the brain are associated with Parkinson’s disease.

Ropinirole is used to treat symptoms of Parkinson’s disease (stiffness, tremors, muscle spasms, and poor muscle control). Ropinirole is also used to treat restless legs syndrome (RLS).

Only immediate-release ropinirole (Requip) is approved to treat either Parkinson symptoms or RLS. Extended-release ropinirole (Requip XL) is approved only to treat Parkinson symptoms.

Parkinson’s and RLS are two separate disorders. Having one of these conditions will not cause you to have the other condition.

Ropinirole may also be used for purposes not listed in this medication guide.

Important Information

Follow all directions on your medicine label and package. Tell each of your healthcare providers about all your medical conditions, allergies, and all medicines you use.

Before taking this medicine

You should not use ropinirole if you are allergic to it.

To make sure ropinirole is safe for you, tell your doctor if you have:

  • high or low blood pressure;

  • kidney disease (or if you are on dialysis);

  • heart disease, heart rhythm problems;

  • a sleep disorder such as narcolepsy, or other conditions that may cause daytime sleepiness; or

  • if you smoke.

People with Parkinson’s disease may have a higher risk of skin cancer (melanoma). Talk to your doctor about this risk and what skin symptoms to watch for.

It is not known whether ropinirole will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant.

It is not known whether ropinirole passes into breast milk or if it could affect the nursing baby. Ropinirole may slow breast milk production. Tell your doctor if you are breast-feeding.

Ropinirole is not approved for use by anyone younger than 18 years old.

How should I take ropinirole?

Follow all directions on your prescription label. Your doctor may occasionally change your dose. Do not take this medicine in larger or smaller amounts or for longer than recommended.

If you are taking immediate-release ropinirole (Requip) you should not take extended-release ropinirole (Requip XL) at the same time.

The dose and timing of ropinirole in treating Parkinson’s disease is different from the dose and timing in treating RLS. Follow the directions on your prescription label. Ask your pharmacist if you have any questions about the kind of ropinirole you receive at the pharmacy.

Ropinirole can be taken with or without food. Take the medicine at the same time each day.

Do not crush, chew, or break an extended-release tablet (Requip XL). Swallow it whole.

Call your doctor if you see part of the ropinirole tablet in your stool. This is a sign that your body may not have absorbed all of the medicine.

If you are taking this medicine for RLS, tell your doctor if your symptoms get worse, if they occur in the morning or earlier than usual in the evening, or if you feel restless symptoms in your hands or arms.

It may take up to several weeks before your symptoms improve. Keep using the medication as directed and tell your doctor if your symptoms do not improve.

Do not stop using ropinirole suddenly, or you could have unpleasant withdrawal symptoms. Follow your doctor’s instructions about tapering your dose.

Store at room temperature away from moisture, heat, and light. Keep the bottle tightly closed when not in use.

What happens if I miss a dose?

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while taking ropinirole?

Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Get up slowly and steady yourself to prevent a fall. Dizziness may impair your thinking or reactions. Avoid driving or operating machinery until you know how ropinirole will affect you.

Drinking alcohol can increase certain side effects of ropinirole.

Ropinirole side effects

Get emergency medical help if you have signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Some people taking ropinirole have fallen asleep during normal daytime activities such as working, talking, eating, or driving. Tell your doctor if you have any problems with daytime sleepiness or drowsiness.

You may have increased sexual urges, unusual urges to gamble, or other intense urges while taking this medicine. Talk with your doctor if this occurs.

Call your doctor at once if you have:

  • extreme drowsiness, falling asleep suddenly (even after feeling alert);

  • worsening or no improvement in your symptoms;

  • a light-headed feeling, like you might pass out;

  • unusual changes in mood or behavior;

  • tremors, twitching uncontrollable muscle movements; or

  • hallucinations (seeing or hearing things that are not real).

Side effects such as confusion or hallucinations may be more likely in older adults.

Common side effects may include:

  • drowsiness, dizziness, weakness;

  • headache, confusion, hallucinations;

  • increased blood pressure (severe headache, pounding in your neck or ears, nosebleed, irregular heartbeats);

  • nausea, vomiting, upset stomach, constipation;

  • flu symptoms (fever, chills, body aches);

  • sudden muscle movements;

  • increased sweating; or

  • swelling in your legs or feet.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect ropinirole?

Taking ropinirole with other drugs that make you sleepy can worsen this effect. Ask your doctor before taking a sleeping pill, narcotic medication, muscle relaxer, or medicine for anxiety, depression, or seizures.

Other drugs may interact with ropinirole, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Copyright 1996-2018 Cerner Multum, Inc. Version: 14.01.

Medical Disclaimer

More about ropinirole

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  • Drug class: dopaminergic antiparkinsonism agents
  • FDA Alerts (1)

Consumer resources

  • Ropinirole Tablets
  • Ropinirole Extended-Release Tablets
  • Ropinirole (Advanced Reading)

Other brands: Requip, Requip XL

Professional resources

  • Ropinirole Hydrochloride (AHFS Monograph)
  • … +3 more

Related treatment guides

  • Restless Legs Syndrome
  • Tardive Dyskinesia
  • Parkinson’s Disease
  • Periodic Limb Movement Disorder

Identification

Are you a new drug developer? Contact us to learn more about our customized products and solutions. Stay in the know! As part of our commitment to providing the most up-to-date drug information, we will be releasing #DrugBankUpdates with our newly added curated drug pages. #DrugBankUpdates Name Ropinirole Accession Number DB00268 (APRD00302) Type Small Molecule Groups Approved, Investigational Description

Ropinirole, also known as ReQuip, is a non-ergoline dopamine agonist used in Parkinson’s disease and restless legs syndrome Label, 3. It is manufactured by GlaxoSmithKline Pharmaceuticals. Ropinirole was initially approved in 1997 by the FDA Label for the management of Parkinson’s disease. In 2005, it was the first drug approved in the US for the management of primary moderate to severe restless legs syndrome 3.

In 2008, the extended-release capsules of ropinirole were approved, allowing for less frequent dosing, therefore increased compliance, and offering a similar side effect profile and efficacy to previous formulations of ropinirole 4.

Structure 3D Download Similar Structures

Structure for Ropinirole (DB00268)

× Close Synonyms

  • Ropinirol
  • Ropinirole
  • Ropinirolum

External IDs SK&F 101468 / SK&F-101468 Product Ingredients

Ingredient UNII CAS InChI Key
Ropinirole Hydrochloride D7ZD41RZI9 91374-20-8 XDXHAEQXIBQUEZ-UHFFFAOYSA-N

Product Images Prescription Products

Name Dosage Strength Route Labeller Marketing Start Marketing End
Unlock Additional Data
Act Ropinirole Tablet Oral TEVA Canada Limited 2009-07-22 Not applicable Canada
Act Ropinirole Tablet Oral TEVA Canada Limited 2009-07-22 Not applicable Canada
Act Ropinirole Tablet Oral TEVA Canada Limited 2009-07-22 Not applicable Canada
Act Ropinirole Tablet Oral TEVA Canada Limited 2009-07-22 Not applicable Canada
Requip Tablet, film coated 2 mg/1 Oral Glaxo Wellcome SA 1997-10-03 2019-02-28 US
Requip Tablet, film coated 5 mg/1 Oral GlaxoSmithKline LLC 1997-10-10 2019-09-30 US
Requip Tablet, film coated 0.5 mg/1 Oral GlaxoSmithKline LLC 1997-10-10 2019-11-30 US
Requip Tablet 1 mg Oral Glaxosmithkline Inc 1997-09-25 2018-03-05 Canada
Requip Tablet, film coated 0.5 mg/1 Oral Physicians Total Care, Inc. 2007-02-27 2008-12-31 US
Requip Tablet, film coated 1 mg/1 Oral Pd Rx Pharmaceuticals, Inc. 1997-10-01 2018-04-27 US

Additional Data Available

  • Application Number Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products

Name Dosage Strength Route Labeller Marketing Start Marketing End
Unlock Additional Data
Apo-ropinirole Tablet Oral Apotex Corporation Not applicable Not applicable Canada
Apo-ropinirole Tablet Oral Apotex Corporation Not applicable Not applicable Canada
Apo-ropinirole Tablet Oral Apotex Corporation Not applicable Not applicable Canada
Apo-ropinirole Tablet Oral Apotex Corporation Not applicable Not applicable Canada
Apo-ropinirole Tablet Oral Apotex Corporation Not applicable Not applicable Canada
Apo-ropinirole Tablet Oral Apotex Corporation Not applicable Not applicable Canada
Apo-ropinirole Tablet Oral Apotex Corporation Not applicable Not applicable Canada
Dom-ropinirole Tablet Oral Dominion Pharmacal Not applicable Not applicable Canada
Dom-ropinirole Tablet Oral Dominion Pharmacal Not applicable Not applicable Canada
Dom-ropinirole Tablet Oral Dominion Pharmacal Not applicable Not applicable Canada

Additional Data Available

  • Application Number Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products

Name Ingredients Dosage Route Labeller Marketing Start Marketing End
Requip Ropinirole Hydrochloride + Ropinirole Hydrochloride + Ropinirole Hydrochloride Tablet, film coated Oral GlaxoSmithKline 2006-10-06 2006-10-06 US
Requip Ropinirole Hydrochloride + Ropinirole Hydrochloride + Ropinirole Hydrochloride Tablet, film coated Oral GlaxoSmithKline 2006-10-06 2006-10-06 US
Requip Ropinirole Hydrochloride + Ropinirole Hydrochloride + Ropinirole Hydrochloride Tablet, film coated Oral GlaxoSmithKline 2006-10-06 2006-10-06 US

International/Other Brands Adartrel / ReQuip CR (GlaxoSmithKline) / Ronirol Categories UNII 030PYR8953 CAS number 91374-21-9 Weight Average: 260.3746
Monoisotopic: 260.1888634 Chemical Formula C16H24N2O InChI Key UHSKFQJFRQCDBE-UHFFFAOYSA-N InChI InChI=1S/C16H24N2O/c1-3-9-18(10-4-2)11-8-13-6-5-7-15-14(13)12-16(19)17-15/h5-7H,3-4,8-12H2,1-2H3,(H,17,19) IUPAC Name 4–2,3-dihydro-1H-indol-2-one SMILES CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1

Pharmacology

Indication

For the treatment of the signs and symptoms of Parkinson’s disease and for the treatment of primary moderate-severe restless legs syndrome Label.

Associated Conditions

  • Idiopathic Parkinson’s Disease
  • Parkinson’s Disease (PD)
  • Moderate Restless Legs Syndrome
  • Severe Restless Legs Syndrome

Pharmacodynamics

Effects on Parkinson’s and restless leg syndrome

This drug promotes the relief or improvement of symptoms of Parkinson’s or restless leg syndrome by stimulatory actions on dopamine receptors, which regulate movement.

Effects on blood pressure

Clinical experience with dopamine agonists, including ropinirole, suggests an association with impaired abilities in regulating blood pressure with resulting orthostatic hypotension, especially with patients undergoing dose escalation. In some patients in clinical studies, blood pressure changes were associated with orthostatic symptoms, bradycardia, and, in one case in a healthy volunteer, transient sinus arrest accompanied by syncope Label. The mechanism of orthostatic hypotension caused by ropinirole is assumed to be due to a D2-mediated blunting of noradrenergic response to a standing position, followed by a decrease in peripheral vascular resistance. Nausea is also a frequent symptom which accompanies orthostatic signs and symptoms Label.

Effects on prolactin

At oral doses as low as 0.2 mg, ropinirole suppressed serum prolactin concentrations in healthy male volunteers. Ropinirole had no dose-related effect on ECG wave form and rhythm in young, healthy, male volunteers in the range of 0.01 to 2.5 mg Label.

Effects on QT interval

Ropinirole had no dose- or exposure-related effect on average QT intervals in healthy male and female volunteers at doses up to 4 mg/day. The effect of ropinirole on QTc intervals at higher exposures reached either due to drug interactions, hepatic dysfunction, or at higher doses has not been adequately evaluated Label.

Mechanism of action

Ropinirole is a non-ergoline dopamine agonist. Ropinirole has the highest affinity at the D3 receptors, which are concentrated in the limbic areas of the brain and may be responsible for some of the neuropsychiatric effects 4. The exact mechanism of action of ropinirole as a treatment for Parkinson’s disease is unknown, however, it is believed to be related to its ability to selectively stimulate dopamine D2 receptors within the caudate-putamen system in the brain. This system affects body movement. Negligible affinity is seen for ropinirole at α2 adrenoreceptors in the periphery and 5HT-1 receptor. Ropinirole has no affinity at the D1-like receptors, benzodiazepine or GABA receptors 4.

The precise mechanism of action of ropinirole as a treatment for Restless Legs Syndrome is unknown, however, it is believed to be related to its ability to stimulate dopamine receptors Label.

Target Actions Organism
ADopamine D3 receptor agonist Humans
UDopamine D4 receptor agonist Humans
UAlpha adrenergic receptor antagonist Humans
ADopamine D2 receptor agonist Humans

Unlock Additional Data Additional Data Available Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Learn more Absorption

Ropinirole is rapidly absorbed after oral administration, reaching peak concentration in approximately 1 to 2 hours Label, 5.

Absolute bioavailability was 45% to 55%, suggesting approximately 50% hepatic first-pass effect Label. The bioavailability of ropinirole prolonged release compared to the immediate release tablets is about 100% 2.

Ingestion of food does not affect the absorption of ropinirole, although its Tmax was increased by 2.5 hours and its Cmax was reduced by approximately 25% when the drug is taken with a high-fat meal Label.

Volume of distribution

Ropinirole is found to be widely distributed throughout the body, with an apparent volume of distribution of 7.5 L/kg Label.

Protein binding

40% bound to plasma proteins with a blood-to-plasma ratio of 1:1 Label.

Metabolism

Ropinirole is heavily metabolized by the liver. The most important metabolic pathways are N­ despropylation and hydroxylation to form the N-despropyl metabolite and hydroxy metabolites Label, both of which are inactive 4.

The N-despropyl metabolite is then converted to carbamyl glucuronide, carboxylic acid, and N-despropyl hydroxy metabolites. Following this process, the hydroxy metabolite of ropinirole is glucuronidated at a rapid rate Label.

In vitro studies show that the major cytochrome P450 enzyme involved in the metabolism of ropinirole is CYP1A2 Label, 5.

  • Ropinirole N-despropyl ropinirole, N-despropyl hydroxy metabolites, and carboxylic acid

Route of elimination

The majority of the absorbed dose is cleared by the liver 4.

In clinical trials, more than 88% of a radiolabeled dose was recovered in urine Label. Less than 10% of the administered dose is excreted as unchanged drug in urine. N-despropyl ropinirole is the major metabolite found in the urine (40%), followed by the carboxylic acid metabolite (10%), and the glucuronide of the hydroxy metabolite (10%) Label.

Half life

Approximately 6 hours Label, 5.

Clearance

The clearance of ropinirole after oral administration is 47 L/h Label.

Toxicity

Overdose

Symptoms of overdose include agitation, chest pain, confusion, drowsiness, facial muscle movements, grogginess, increased jerkiness of movement, symptoms of low blood pressure (dizziness, light-headedness)upon standing, nausea, and vomiting Label.

Carcinogenicity

Two-year carcinogenicity studies of ropinirole were performed on animal models at oral doses of 5, 15, and 50 mg/kg/day and in rats at oral doses of 1.5, 15, and 50 mg/kg/day. There was an increase in testicular Leydig cell adenomas at all doses tested in rats. The hormonal mechanisms thought to be involved in the development of these tumors in rats are not considered relevant to humans. In mice, there was an increase in benign uterine endometrial polyps at a dose of 50 mg/kg/day. The highest dose not associated with this observation (15 mg/kg/day) is three times the maximum recommended human dose on a mg/m2 basis Label.

Mutagenesis

Ropinirole was not found to be mutagenic or clastogenic during in vitro assays, or in the in vivo mouse micronucleus test Label.

Effects on reproduction

When given to female rats prior to and during mating and throughout pregnancy, ropinirole led to disruption of implantation at oral doses of 20 mg/kg/day (8 times the MRHD on a mg/m2 basis) or higher. This effect in rats is believed to be due to the prolactin-lowering effects of ropinirole.

Use in Pregnancy

Pregnancy Category C. There are no sufficient and well-controlled studies done in pregnant women. In animal reproduction studies, ropinirole has demonstrated adverse effects on embryo-fetal development, including teratogenicity Label.

Affected organisms

  • Humans and other mammals

Pathways Not Available Pharmacogenomic Effects/ADRs Not Available

Interactions

Drug Interactions This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

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  • Vet approved
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Drug Interaction
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(R)-warfarin The risk or severity of adverse effects can be increased when Ropinirole is combined with (R)-warfarin.
(S)-Warfarin The risk or severity of adverse effects can be increased when Ropinirole is combined with (S)-Warfarin.
2,5-Dimethoxy-4-ethylthioamphetamine 2,5-Dimethoxy-4-ethylthioamphetamine may increase the sedative activities of Ropinirole.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may increase the sedative activities of Ropinirole.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Ropinirole is combined with 4-hydroxycoumarin.
4-Methoxyamphetamine 4-Methoxyamphetamine may increase the sedative activities of Ropinirole.
5-methoxy-N,N-dimethyltryptamine 5-methoxy-N,N-dimethyltryptamine may increase the sedative activities of Ropinirole.
7-Nitroindazole 7-Nitroindazole may increase the sedative activities of Ropinirole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the sedative activities of Ropinirole.
Abatacept The metabolism of Ropinirole can be increased when combined with Abatacept.

Additional Data Available

  • Extended Description Extended Description

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  • Severity Severity

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  • Evidence Level Evidence Level

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  • Action Action

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Food Interactions Not Available Synthesis Reference US4452808 General References External Links Human Metabolome Database HMDB0014413 KEGG Drug D08489 KEGG Compound C07564 PubChem Compound 5095 PubChem Substance 46507918 ChemSpider 4916 BindingDB 50020680 ChEBI 8888 ChEMBL CHEMBL589 Therapeutic Targets Database DAP001515 PharmGKB PA164749035 RxList RxList Drug Page Drugs.com Drugs.com Drug Page PDRhealth PDRhealth Drug Page Wikipedia Ropinirole ATC Codes N04BC04 — Ropinirole

  • N04BC — Dopamine agonists
  • N04B — DOPAMINERGIC AGENTS
  • N04 — ANTI-PARKINSON DRUGS
  • N — NERVOUS SYSTEM

AHFS Codes

  • 28:36.20.08 — Nonergot-derivative Dopamine Receptor Agonists

FDA label (796 KB) MSDS (29.6 KB)

Clinical Trials

Clinical Trials

Phase Status Purpose Conditions Count
1 Completed Not Available Healthy Volunteers 2
1 Completed Not Available Pharmacokinetic Study 3
1 Completed Diagnostic End Stage Renal Disease (ESRD) / Restless Legs Syndrome (RLS) 1
1 Completed Other Parkinson’s Disease (PD) 1
1 Completed Treatment Healthy Volunteers 2
1 Completed Treatment Parkinson’s Disease (PD) 1
1 Completed Treatment Restless Legs Syndrome (RLS) 2
1, 2 Recruiting Treatment Parkinson’s Disease (PD) 1
1, 2 Recruiting Treatment Idiopathic hyperprolactinemic disorder / Prolactinoma 1
2 Completed Treatment Cerebrovascular Accident / Hemiparesis 1
2 Completed Treatment Dependence, Cocaine 1
2 Completed Treatment Fibromyalgia Syndrome, Primary 1
2 Completed Treatment Parkinson’s Disease (PD) 2
2 Completed Treatment Restless Legs Syndrome (RLS) 1
2 Recruiting Treatment End Stage Renal Disease (ESRD) / Restless Legs Syndrome (RLS) 1
2 Terminated Treatment Restless Legs Syndrome (RLS) 1
2 Unknown Status Treatment Unverricht-Lundborg Syndrome 1
3 Completed Treatment Dyskinesia / Parkinson’s Disease (PD) 1
3 Completed Treatment Idiopathic Parkinson’s Disease 2
3 Completed Treatment Moderate to Severe Idiopathic Restless Legs Syndrome (RLS) / Restless Legs Syndrome (RLS) 1
3 Completed Treatment Parkinson’s Disease (PD) 10
3 Completed Treatment Restless Legs Syndrome (RLS) 7
3 Recruiting Treatment End Stage Renal Disease (ESRD) / Restless Legs Syndrome (RLS) 1
3 Terminated Treatment Parkinson’s Disease (PD) 1
3 Unknown Status Treatment Parkinson’s Disease (PD) 1
4 Completed Diagnostic Parkinson’s Disease (PD) 1
4 Completed Treatment Bipolar Disorder (BD) 1
4 Completed Treatment Parkinson’s Disease (PD) 4
4 Completed Treatment Restless Legs Syndrome (RLS) 2
4 Completed Treatment Sexual Dysfunctions 1
4 Enrolling by Invitation Supportive Care Liver Cirrhosis / Muscle Cramps 1
4 Unknown Status Treatment Bipolar Disorder (BD) / Major Depressive Disorder (MDD) 1
Not Available Completed Not Available Restless Legs Syndrome (RLS) 1
Not Available Completed Treatment Major Depressive Disorder (MDD) 1
Not Available Completed Treatment Parkinson’s Disease (PD) / Restless Legs Syndrome (RLS) 2
Not Available Recruiting Not Available Atypical Parkinson Disease / Corticobasal Degeneration / Gait, Frontal / Huntington’s Disease (HD) / Multiple System Atrophy (MSA) / Parkinson’s Disease (PD) / Parkinsonian Disorders / Progressive Supranuclear Palsy (PSP) 1

Pharmacoeconomics

Manufacturers

  • Smithkline beecham corp dba glaxosmithkline
  • Glaxosmithkline
  • Alembic ltd
  • Corepharma llc
  • Glenmark generics ltd
  • Huahai us inc
  • Mylan pharmaceuticals inc
  • Roxane laboratories inc
  • Teva pharmaceuticals usa inc
  • Wockhardt ltd
  • Zydus pharmaceuticals usa inc

Packagers

  • Amerisource Health Services Corp.
  • A-S Medication Solutions LLC
  • Atlantic Biologicals Corporation
  • Bryant Ranch Prepack
  • Cadila Healthcare Ltd.
  • Cardinal Health
  • Corepharma LLC
  • GlaxoSmithKline Inc.
  • Glenmark Generics Ltd.
  • Heartland Repack Services LLC
  • Heritage Pharmaceuticals
  • Innoviant Pharmacy Inc.
  • Kaiser Foundation Hospital
  • Lake Erie Medical and Surgical Supply
  • Major Pharmaceuticals
  • Mckesson Corp.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Nucare Pharmaceuticals Inc.
  • PD-Rx Pharmaceuticals Inc.
  • Physicians Total Care Inc.
  • Rebel Distributors Corp.
  • Resource Optimization and Innovation LLC
  • Roxane Labs
  • Stat Rx Usa
  • Teva Pharmaceutical Industries Ltd.
  • Vangard Labs Inc.
  • Wockhardt Ltd.
  • Zydus Pharmaceuticals

Dosage forms

Form Route Strength
Tablet Oral
Tablet, film coated Oral
Tablet, film coated Oral 0.25 mg/1
Tablet, film coated Oral 0.5 mg/1
Tablet, film coated Oral 1 mg/1
Tablet, film coated Oral 2 mg/1
Tablet, film coated Oral 3 mg/1
Tablet, film coated Oral 4 mg/1
Tablet, film coated, extended release Oral 2 mg/1
Tablet Oral 0.25 mg
Tablet Oral 1 mg
Tablet Oral 2 mg
Tablet Oral 4 mg/1
Tablet Oral 5 mg/1
Tablet Oral 5 mg
Tablet Oral 0.25 mg/1
Tablet Oral 0.5 mg/1
Tablet Oral 1 mg/1
Tablet Oral 2 mg/1
Tablet Oral 3 mg/1
Tablet, coated Oral 0.25 mg/1
Tablet, coated Oral 0.5 mg/1
Tablet, coated Oral 1 mg/1
Tablet, coated Oral 2 mg/1
Tablet, coated Oral 3 mg/1
Tablet, coated Oral 4 mg/1
Tablet, coated Oral 5 mg/1
Tablet, film coated Oral 5 mg/1
Tablet, film coated, extended release Oral 12 mg/1
Tablet, film coated, extended release Oral 3 mg/1
Tablet, film coated, extended release Oral 4 mg/1
Tablet, film coated, extended release Oral 6 mg/1
Tablet, film coated, extended release Oral 8 mg/1

Prices

Unit description Cost Unit
Requip XL 12 mg 24 Hour tablet 14.92USD tablet
Requip xl 12 mg tablet 14.35USD tablet
Requip XL 8 mg 24 Hour tablet 8.96USD tablet
Requip xl 6 mg tablet 8.61USD tablet
Requip xl 8 mg tablet 8.61USD tablet
Requip XL 4 mg 24 Hour tablet 5.97USD tablet
Requip xl 4 mg tablet 5.74USD tablet
Requip 5 mg Tablet 3.87USD tablet
Requip 3 mg tablet 3.41USD tablet
Requip 4 mg tablet 3.41USD tablet
Requip 5 mg tablet 3.41USD tablet
Requip 0.25 mg tablet 3.29USD tablet
Requip 0.5 mg tablet 3.29USD tablet
Requip 1 mg tablet 3.29USD tablet
Requip 2 mg tablet 3.29USD tablet
Requip xl 2 mg tablet 2.87USD tablet
Ropinirole hcl 3 mg tablet 2.65USD tablet
Ropinirole hcl 4 mg tablet 2.65USD tablet
Ropinirole hcl 5 mg tablet 2.65USD tablet
Ropinirole hcl 0.25 mg tablet 2.55USD tablet
Ropinirole hcl 0.5 mg tablet 2.55USD tablet
Ropinirole hcl 1 mg tablet 2.55USD tablet
Ropinirole hcl 2 mg tablet 2.55USD tablet
Co Ropinirole 5 mg Tablet 1.8USD tablet
Pms-Ropinirole 5 mg Tablet 1.8USD tablet
Ran-Ropinirole 5 mg Tablet 1.8USD tablet
Ropinirole 5 mg Tablet 1.8USD tablet
Requip 2 mg Tablet 1.41USD tablet
Requip 1 mg Tablet 1.28USD tablet
Co Ropinirole 2 mg Tablet 0.65USD tablet
Pms-Ropinirole 2 mg Tablet 0.65USD tablet
Ran-Ropinirole 2 mg Tablet 0.65USD tablet
Ropinirole 2 mg Tablet 0.65USD tablet
Co Ropinirole 1 mg Tablet 0.59USD tablet
Pms-Ropinirole 1 mg Tablet 0.59USD tablet
Ran-Ropinirole 1 mg Tablet 0.59USD tablet
Ropinirole 1 mg Tablet 0.59USD tablet
Requip 0.25 mg Tablet 0.32USD tablet
Co Ropinirole 0.25 mg Tablet 0.15USD tablet
Pms-Ropinirole 0.25 mg Tablet 0.15USD tablet
Ran-Ropinirole 0.25 mg Tablet 0.15USD tablet
Ropinirole 0.25 mg Tablet 0.15USD tablet

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only. Patents

Patent Number Pediatric Extension Approved Expires (estimated)
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US5422123 No 1995-06-06 2012-06-06 US
US7927624 No 2011-04-19 2021-12-02 US
US8303986 No 2012-11-06 2021-04-12 US

Additional Data Available

  • Filed On Filed On

    The date on which a patent was filed with the relevant government.

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Properties

State Solid Experimental Properties Predicted Properties

Property Value Source
Water Solubility 0.353 mg/mL ALOGPS
logP 3.16 ALOGPS
logP 3.06 ChemAxon
logS -2.9 ALOGPS
pKa (Strongest Acidic) 13.24 ChemAxon
pKa (Strongest Basic) 10.17 ChemAxon
Physiological Charge 1 ChemAxon
Hydrogen Acceptor Count 2 ChemAxon
Hydrogen Donor Count 1 ChemAxon
Polar Surface Area 32.34 Å2 ChemAxon
Rotatable Bond Count 7 ChemAxon
Refractivity 81.43 m3·mol-1 ChemAxon
Polarizability 31.19 Å3 ChemAxon
Number of Rings 2 ChemAxon
Bioavailability 1 ChemAxon
Rule of Five Yes ChemAxon
Ghose Filter Yes ChemAxon
Veber’s Rule Yes ChemAxon
MDDR-like Rule No ChemAxon

Predicted ADMET features

Property Value Probability
Human Intestinal Absorption + 1.0
Blood Brain Barrier + 0.9971
Caco-2 permeable + 0.6087
P-glycoprotein substrate Substrate 0.7604
P-glycoprotein inhibitor I Inhibitor 0.5458
P-glycoprotein inhibitor II Non-inhibitor 0.8641
Renal organic cation transporter Non-inhibitor 0.602
CYP450 2C9 substrate Non-substrate 0.8593
CYP450 2D6 substrate Non-substrate 0.9116
CYP450 3A4 substrate Substrate 0.6903
CYP450 1A2 substrate Non-inhibitor 0.9045
CYP450 2C9 inhibitor Non-inhibitor 0.9071
CYP450 2D6 inhibitor Inhibitor 0.8932
CYP450 2C19 inhibitor Non-inhibitor 0.9025
CYP450 3A4 inhibitor Non-inhibitor 0.8309
CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.6959
Ames test Non AMES toxic 0.7302
Carcinogenicity Non-carcinogens 0.905
Biodegradation Not ready biodegradable 0.9966
Rat acute toxicity 2.6400 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.8959
hERG inhibition (predictor II) Non-inhibitor 0.7066

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST) Not Available Spectra

Spectrum Spectrum Type Splash Key
Predicted GC-MS Spectrum – GC-MS Predicted GC-MS Not Available
Predicted MS/MS Spectrum – 10V, Positive (Annotated) Predicted LC-MS/MS splash10-03di-0190000000-7e072cf65f341641938c
Predicted MS/MS Spectrum – 20V, Positive (Annotated) Predicted LC-MS/MS splash10-03di-3960000000-47d2311adfeeacf4062d
Predicted MS/MS Spectrum – 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0006-7900000000-0891c66db163729a5360
Predicted MS/MS Spectrum – 10V, Negative (Annotated) Predicted LC-MS/MS splash10-0a4i-0090000000-88c0fa3d93090a0d06c6
Predicted MS/MS Spectrum – 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0pb9-3590000000-8fb5fc766313ee6bbd9e
Predicted MS/MS Spectrum – 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0k96-9400000000-f1b50dacd59a9bfe90b7

Taxonomy

Description This compound belongs to the class of organic compounds known as indolines. These are compounds containing an indole moiety, which consists of pyrrolidine ring fused to benzene to form 2,3-dihydroindole. Kingdom Organic compounds Super Class Organoheterocyclic compounds Class Indoles and derivatives Sub Class Indolines Direct Parent Indolines Alternative Parents Phenethylamines / Aralkylamines / Trialkylamines / Secondary carboxylic acid amides / Lactams / Amino acids and derivatives / Azacyclic compounds / Organopnictogen compounds / Organic oxides / Hydrocarbon derivativesCarbonyl compounds show 1 more Substituents Dihydroindole / Phenethylamine / Aralkylamine / Benzenoid / Amino acid or derivatives / Carboxamide group / Lactam / Secondary carboxylic acid amide / Tertiary aliphatic amine / Tertiary amineCarboxylic acid derivative / Azacycle / Organooxygen compound / Organonitrogen compound / Organic oxide / Organopnictogen compound / Amine / Organic oxygen compound / Carbonyl group / Hydrocarbon derivative / Organic nitrogen compound / Aromatic heteropolycyclic compound show 12 more Molecular Framework Aromatic heteropolycyclic compounds External Descriptors tertiary amine, indolones (CHEBI:8888)

Targets

Binding Properties

× Details Binding Properties1. Dopamine D3 receptor Kind Protein Organism Humans Pharmacological action Yes Actions Agonist General Function G-protein coupled amine receptor activity Specific Function Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation. Gene Name DRD3 Uniprot ID P35462 Uniprot Name D(3) dopamine receptor Molecular Weight 44224.335 Da Kind Protein Organism Humans Pharmacological action Unknown Actions Agonist General Function Sh3 domain binding Specific Function Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins … Gene Name DRD4 Uniprot ID P21917 Uniprot Name D(4) dopamine receptor Molecular Weight 48359.86 Da Kind Protein group Organism Humans Pharmacological action Unknown Actions Antagonist General Function Protein heterodimerization activity Specific Function This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot…

Components:

× Details Binding Properties4. Dopamine D2 receptor Kind Protein Organism Humans Pharmacological action Yes Actions Agonist General Function Potassium channel regulator activity Specific Function Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Gene Name DRD2 Uniprot ID P14416 Uniprot Name D(2) dopamine receptor Molecular Weight 50618.91 Da

Enzymes

Kind Protein Organism Humans Pharmacological action Unknown Actions Substrate General Function Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen Specific Function Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un… Gene Name CYP1A2 Uniprot ID P05177 Uniprot Name Cytochrome P450 1A2 Molecular Weight 58293.76 Da ×Unlock Data

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Drug created on June 13, 2005 07:24 / Updated on February 02, 2020 04:07

PMC

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According to the Food and Drug Administration (FDA), some physicians and pharmacists are experiencing some confusion over the similarity of the names of an antidepressant and a blood-thinning medication. Although the FDA claims it is unaware of anyone who consumed the wrong medication, the agency said it received 50 reports of medication errors, including instances where physicians gave the incorrect medication or pharmacists dispensed the wrong drug.

The medications are Brintellix, which is an antidepressant, and Brilinta, which is a blood-thinner medication used to aid in the prevention of death following a heart attack or serious chest pain or to avert a second heart attack. The agency claims it has been the recipient of reports of errors since the approval of Brintellix in September 2013. Each medication is a tablet with the letter T imprinted on it, and each is yellow. In order to avoid any more confusion, the FDA recommends that physicians write out the generic name of the drug in addition to the brand name, and the illness for which it is being prescribed.

Brintellix is an antidepressant that is intended to be taken once a day, and is also known by another name, vortioxetine. Brilinta is a blood thinner that is to be ingested two times a day, and is also referred to as ticagrelor.

Prior to the approval of drugs, companies suggest names for their drugs. The FDA’s Division of Medication Error Prevention and Analysis (DMEPA) reviews those names, and then compares them to drugs that are on the market, and those that are still being reviewed by the FDA.

There have rarely been warnings over confusion of the names of medications. However, they do occur. For example, in 2011, the FDA said it had discovered over 200 medication errors in which the drugs Risperdal and Requip, were involved. Risperdal is an antipsychotic, and Requip is a drug that treats symptoms of Parkinson’s disease and restless legs syndrome. According to the FDA, five patients were hospitalized when they were administered the incorrect drug.

There were similarities between the brand names and generic names of each drug. The generic name for Risperdal is risperidone, and the generic name for Requip is ropinirole. The FDA requested that drug manufacturers Johnson & Johnson and GlaxoSmithKline PLCD modify their packaging to help differentiate one drug from the other. The FDA also advises patients to always check their prescriptions to make certain that they are receiving the correct medication.

DISCUSSION

Smoking induces cytochrome P450 isozyme CYP1A2. Since ropinirole is a CYP1A2 substrate, the plasma concentrations of ropinirole may be decreased in smokers compared with nonsmokers taking similar doses. In a study of patients with restless legs syndrome, smokers compared with nonsmokers had a lower area under the concentration curve (AUC) and lower maximal concentration of ropinirole of about one third when adjusted for dose.2

If a person smokes, he or she may require higher doses of ropinirole to reach clinical response. Conversely, as in this case, if a person is on a stable dose of ropinirole and stops smoking, a dose reduction of ropinirole may be required. By stopping a CYP1A2 inducer (smoking nicotine), the metabolism of ropinirole slows with smoking cessation. This decrease in dose would allow the patients to reach the same blood concentration as they had at the higher dose when they were smoking.

Nicotine replacement therapy (patch, gum, inhaler) is commonly used for a few weeks after a person stops smoking. This nicotine would be expected to induce CYP1A2 in the same way as nicotine from smoking. Therefore, the increase in ropinirole blood concentrations and corresponding symptom would occur only after all forms of nicotine are discontinued.

The adverse reaction described in this case occurred while on ropinirole. There are other dopaminergic agents commonly used to treat RLS, including pramipexole and carbidopa/levodopa. These would not be expected to show elevated blood concentrations with smoking cessation as they are not metabolized by the CYP1A2 route.

Sweating and hyperhidrosis have been reported in clinical trials and in overdose of ropinirole.2,3

This case highlights the importance of a thorough review of medications when any drug, including nicotine, is going to be started or stopped. Patients with RLS who are on ropinirole therapy should be warned, and assessed for symptoms that may require dose adjustments when they start or stop the use of nicotine.

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