Ropinirolum

Ropinirolum Uses, Dosage, Side Effects, Food Interaction and all others data.

Ropinirolum binds the dopamine receptors D3 and D2. Although the precise mechanism of action of ropinirole as a treatment for Parkinson's disease is unknown, it is believed to be related to its ability to stimulate these receptors in the striatum. This conclusion is supported by electrophysiologic studies in animals that have demonstrated that ropinirole 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.

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

Trade Name Ropinirolum
Availability Prescription only
Generic Ropinirole
Ropinirole Other Names Ropinirol, Ropinirole, Ropinirolum
Related Drugs Gocovri, Rytary, Sinemet, Sinemet CR, pramipexole, benztropine, carbidopa / levodopa, amantadine, Requip, Mirapex
Type
Formula C16H24N2O
Weight Average: 260.3746
Monoisotopic: 260.1888634
Protein binding

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

Groups Approved, Investigational
Therapeutic Class Antiparkinson drugs
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Ropinirolum
Ropinirolum

Uses

Ropinirolum is used alone or with other medicines to treat Parkinson’s disease. It helps to improve muscle control and movement difficulties. Thus, is also used to treat a condition called Restless Legs Syndrome (RLS). This condition is an overwhelming feeling of wanting to move the legs to make them comfortable from unpleasant sensations in the legs.

Ropinirolum is also used to associated treatment for these conditions: Idiopathic Parkinson's Disease, Parkinson's Disease (PD), Moderate Restless Legs Syndrome, Severe Restless Legs Syndrome

How Ropinirolum works

Ropinirolum is a non-ergoline dopamine agonist. Ropinirolum 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 . 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. Ropinirolum has no affinity at the D1-like receptors, benzodiazepine or GABA receptors .

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 .

Dosage

Ropinirolum dosage

In all clinical studies, dosage was initiated at a sub therapeutic level and gradually titrated to therapeutic response. The dosage should be increased to achieve a maximum therapeutic effect, balanced against the principal side effects of nausea, dizziness, somnolence and dyskinesia.

The recommended starting dose is 0.25 mg three times daily with or without food. Based on individual patient response, dosage should then be titrated with weekly increments as described in the table below. After week 4, if necessary, daily dosage may be increased by 1.5 mg per day on a weekly basis up to a dose of 9 mg per day, and then by up to 3 mg per day weekly to a total dose of 24 mg per day.

Ascending-Dose Schedule of Ropinirolum:

  • First week:0.25 mg three times daily.Total Daily Dose:0.75 mg
  • Second week:0.5 mg three times daily.Total Daily Dose:1.5 mg
  • Third week:0.75 mg three times daily.Total Daily Dose:2.25 mg
  • Fourth week:1.0 mg three times daily.Total Daily Dose:3.0 mg

Dosage greater than 24 mg/day have not been tested in clinical trials. Ropinirolum should be discontinued gradually over a 7 day period. The frequency of administration should be reduced from three times daily to twice daily for 4 days. For the remaining 3 days, the frequency should be reduced to once daily prior to complete withdrawal of Ropinirolum.

Side Effects

Some of the side effects that are known to be associated with Ropinirolum are abdominal pain, swelling of the legs and ankles due to excess fluid retention (peripheral oedema), confusion, difficulty performing voluntary movements, resulting in jerky or involuntary movements or muscle twitches (dyskinesia), false perceptions of things that are not really there (hallucinations), nausea and vomiting, sleepiness (somnolence), fainting (syncope), slower than normal heart beat (bradycardia), profound drop in blood pressure (hypotension).

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 .

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 .

Mutagenesis

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

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 .

Precaution

If a patient develops significant daytime sleepiness or episodes of falling asleep during activities that require active participation (e.g. conversations, eating, etc.), Riponirole should ordinarily be discontinued. If a decision is made to continue Ropinirolum, patients should be advised to no drive and to avoid other potentially dangerous activities.

Interaction

Co-administration of Ropinirolum with carbidopa or L-dopa or digoxin or theophylline did not show any interaction between them to hamper pharmacological effect. Co administration of ciprofloxacin (500 b.i.d.), an inhibitor of CYP1A2 ( enzyme responsible for Ropinirolum metabolism), with Ropinirolum (2 mg t.i.d.) increased Ropinirolum AUC by 84%. Since ropinirole is a dopamine agonist, it is possible that dopamine antagonists, such as neuroleptics (phenothiazines, butyrophenones, thioxanthenes) or metoclopramide, may diminish the effectiveness of Ropinirolum.

Food Interaction

  • Take with or without food. May take with food to reduce nausea.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Volume of Distribution

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

Elimination Route

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

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

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 .

Half Life

Approximately 6 hours , .

Clearance

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

Elimination Route

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

In clinical trials, more than 88% of a radiolabeled dose was recovered in urine . 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%) .

Pregnancy & Breastfeeding use

Pregnancy: Pregnancy category C. There are no adequate and well-controlled studies using Ropinirolum in pregnant women. Ropinirolum should be used during pregnancy only if the potential benefit outweighs the potential risk of the fetus.

Nursing Mothers: Ropinirolum inhibits prolactin secretion in humans and could potentially inhibit lactation. Because of the potential for serious adverse reactions in nursing infants from Ropinirolum, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother

Contraindication

Ropinirolum is contraindicated for patients known to have hypersensitivity to the product.

Special Warning

Pediatric Use: Safety and effectiveness of Ropinirolum in the pediatric population have not been established.

Acute Overdose

Symptoms include nausea, vomiting, visual hallucinations, hyperhidrosis, asthenia and nightmares. General supportive measures and monitoring of vital signs are recommended. May consider gastric lavage.

Storage Condition

Store in a cool and dry place, away from light. Keep out of reach of children.

Innovators Monograph

You find simplified version here Ropinirolum

Ropinirolum contains Ropinirole see full prescribing information from innovator Ropinirolum Monograph, Ropinirolum MSDS, Ropinirolum FDA label

FAQ

What is Ropinirolum used for?

Ropinirolum is used alone or with other medications to treat the symptoms of Parkinson's disease (a disorder of the nervous system that causes difficulties with movement, muscle control, and balance) including shaking of parts of the body, stiffness, slowed movements, and problems with balance.

How safe is Ropinirolum?

It has not been confirmed that Ropinirolum is safe and effective for use in children younger than 18 years. This drug should not be used in children in this age group. Older adults may not be able to eliminate Ropinirolum from their bodies as well as they used to. This can cause your body to process drugs more slowly.

How does Ropinirolum work?

Ropinirolum works by copying natural dopamine in the brain.

What are the common side effects of Ropinirolum?

Common side effects of Ropinirolum are include:

  • Confusion
  • dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
  • drowsiness
  • falling
  • nausea
  • seeing, hearing, or feeling things that are not there (hallucinations)
  • sleepiness or unusual drowsiness
  • swelling of the legs
  • twisting, twitching, or other unusual body movements
  • unusual tiredness or weakness
  • worsening of parkinsonism

Is Ropinirolum safe during pregnancy?

Ropinirolum should be used during pregnancy only if the benefit outweighs the risk to the fetus. In animal studies, this drug was shown to be teratogenic causing adverse effects on embryo-fetal development.

Is Ropinirolum safe during breastfeeding?

No information is available on the use of Ropinirolum during breastfeeding, but it suppresses serum prolactin and may interfere with breastfeeding. An alternate drug may be preferred, especially while nursing a newborn or preterm infant.

Can I drink alcohol with Ropinirolum?

Alcohol can increase the nervous system side effects of Ropinirolum such as dizziness, drowsiness, and difficulty concentrating You should avoid or limit the use of alcohol while being treated with Ropinirolum.

When is the best time to take Ropinirolum?

Ropinirolum should be taken once a day before bedtime. Ropinirolum may be taken with a meal or snack to reduce any stomach upsets.

How long does it take for Ropinirolum to work?

Peak concentrations of Ropinirolum are achieved within one to two hours, but it takes approximately two days of regular dosing to reach stable blood levels in the body.

Does Ropinirolum help with anxiety?

In addition to controlling motor symptoms, Ropinirolum improved both anxiety and depressive symptoms in PD patients with motor fluctuations and/or dyskinesias.

Does Ropinirolum make me feel good?

Ropinirolum works by copying natural dopamine in the brain. This helps improve movement symptoms related to low dopamine levels in the body, such as in Parkinson's and restless legs syndrome. You may notice an improvement after taking your first dose.

Is Ropinirolum a muscle relaxer?

Ropinirolum is a non-ergoline dopamine agonist used to treat symptoms of Parkinson's disease, such as stiffness, tremors, muscle spasms, and poor muscle control. Requip is also used to treat restless legs syndrome.

Is Ropinirolum safe long-term?

Ropinirolum was highly effective and well tolerated in the long-term management of RLS, with pharmacological effect over 36 weeks.

Is Ropinirolum bad for kidneys?

No dosage adjustment is recommended by the manufacturer for people with kidney or liver disease, but the dosage should be titrated carefully. Has not been studied in severe renal impairment.

Can Ropinirolum cause liver damage?

Thus, Ropinirolum can cause acute, clinically apparent liver injury with jaundice, but it is rare.

How much Ropinirolum is safe?


Adults at first, 2 milligrams (mg) once a day for 1 to 2 weeks. Your doctor may adjust your dose as needed and tolerated. However, the dose is usually not more than 24 mg per day. Children use and dose must be determined by your doctor.

Who should not take Ropinirolum?

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.

What happens if I miss a dose of Ropinirolum?

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 should I avoid while taking Ropinirolum?

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 Ropinirolum.

What happen if I take too much Ropinirolum?

If you take too much, You could have dangerous levels of the drug in your body. Symptoms of an overdose of this drug can include: nausea or vomiting. hallucinations.

*** Taking medicines without doctor's advice can cause long-term problems.
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