現在位置 : 藥物 > 帕金森病用藥 Requip 力必平 (Ropinirole)
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REQUIP PD 4MG
中文名 : 力必平 持續性藥效膜衣錠 健保局藥理類別 : 120804 抗巴金森症藥物 學名 : Ropinirole 類別 : PHR 劑量 : TAB 仿單 REQUIP PD 4MG 用藥指導單張 ATC7藥理類別 : N04BC04 ropinirole 孕婦用藥分級 C 級：在對照的動物研究試驗中顯示該藥學物對胚胎有不良反應（致畸胎性或殺胚胎性或其他），但未進行人體懷孕婦女研究；或者尚無對照的人體懷孕婦女或動物研究試驗。只有在可能的利益大於潛在的危險，才可使用此藥物。 結構式 : 4-[2-(dipropylamino)ethyl]-1,3-dihydro-2H-indol-2-one 藥理作用 : Ropinirole是一種強效的非ergoline類 D2/D3多巴胺致效劑。 帕金森氏症的特徵是黑質紋狀體系統明顯缺乏多巴胺。Ropinirole可藉由刺激紋狀體之多巴胺接受體的作用來減輕這種多巴胺缺乏的現象。 適應症 : 治療帕金森氏症。 用法用量 : 每日一次於同一時間服用。此錠劑必須整粒吞服，切勿咀嚼、壓碎或撥半使用。此錠劑可與食物併服，亦可空腹服用。 藥動力學 吸收：達到Cmax中位數時間為六小時。Ropinirole PR口服的生體可用率在飽食或禁食的狀態中是相似的。 分佈：具有高脂溶性，因此其分佈體積極廣（約為7L/kg） 代謝：Ropinirole的廓清主要是透過CYP1A2的代謝作用，且其代謝物大部分都是經由尿液排出體外。 排除：Ropinirole是自全身循環中廓清的，其平均排除半衰期約為6小時。 副作用 : 腹痛、噁心、消化不良、便秘。 交互作用 : CNS depressants (eg, alcohol) Use with caution because of additive CNS effects. CYP1A2 inducers (eg, cigarette smoking, rifampin) May increase metabolic Cl of ropinirole. CYP1A2 inhibitors (eg, ciprofloxacin, erythromycin, fluvoxamine) May decrease metabolic Cl of ropinirole. Dopamine antagonists (eg, butyrophenones, metoclopramide, phenothiazines, thioxanthenes) May reduce effectiveness of ropinirole. Estrogen May reduce Cl of ropinirole. Levodopa Ropinirole mat potentiate dopaminergic adverse reactions of levodopa, and may cause or exacerbate preexisting dyskinesias. Warfarin An increase in INR was reported in a patient stabilized on warfarin 9 days after starting ropinirole. 禁忌 : 對ropinirole或賦形劑過敏者。 給付規定 1.3.4.帕金森氏症治療藥品：(91/11/1、93/2/1、95/9/1、96/9/1、97/7/1、100/6/1、101/6/1) 1.如病人開始出現功能障礙，在使用levodopa之前或同時，得使用一種dopamine agonist（ropinirole、pramipexole、pergolide、lisuride及rotigotine），或amantadine，或是levodopa併用 COMT抑制劑（entacapone：如Comtan film-coated tab.） 2.Levodopa＋carbidopa＋entacapone三合一製劑（如Stalevo Film-Coated Tablets 150/37.5/200mg等3品項）： 限用於表現藥效終期運動功能波動現象，以左多巴/多巴脫羧基脢抑制劑無法達到穩定治療效果之巴金森氏症病人。（95/9/1） 3.若已同時使用上述藥物且達高劑量，仍無法達到滿意的 "on" state，或出現運動併發症（如異動症或肌強直），需合併使用多類藥物治療時，應於病歷上詳細記載理由。 4.Rasagiline：(101/6/1) (1)可單獨使用，每日最高劑量為1 mg；或與levodopa併用，rasagiline每日最高劑量為0.5 mg。 (2)本品不得與levodopa 以外之其他帕金森氏症治療藥品併用。 5.Pramipexole及ropinirole用於治療原發性腿部躁動症時需先排除腎衰竭、鐵缺乏症及多發性神經病變，且不得與dopamine agonist及levodopa併用。（96/9/1、97/7/1） (1)pramipexole每日最大劑量為0.75mg。（96/9/1） (2)ropinirole每日最大劑量為4mg。（97/7/1） 注意事項 : 有遺傳性galactose耐受性、the Lapp Lactose Deficiency 或glucose-galactose malabsorption 的病人不可使用此藥。 警語 : 由於ropinirole的藥理學作用，對併有嚴重心血管疾病的患者應小心治療。 過量處理 : 一般認為，ropinirole使用過量的症狀應該會和其多巴胺致效性作用有關。這些症狀或可使用適當的多巴胺拮抗劑來加以緩解，如抗精神病藥劑或metoclopramide。 藥品保存方式 : 儲存於25℃以下。 |
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Ropinirole
Why is this medication prescribed? Ropinirole is used alone or with other medications to treat the symptoms of Parkinson's disease (PD; 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. Ropinirole is also used to treat restless legs syndrome (RLS or Ekbom syndrome; a condition that causes discomfort in the legs and a strong urge to move the legs, especially at night and when sitting or lying down). Ropinirole is in a class of medications called dopamine agonists. It works by acting in place of dopamine, a natural substance in the brain that is needed to control movement. How should this medicine be used? Ropinirole comes as a tablet and an extended-release (long-acting) tablet to take by mouth. Ropinirole may be taken with food to prevent stomach upset. When ropinirole is used to treat Parkinson's disease, the regular tablet is usually taken three times a day and the extended-release tablet is taken once daily. When ropinirole is used to treat Restless Legs Syndrome, the regular tablet is usually taken once a day, 1 to 3 hours before bedtime. Ropinirole extended-release tablets are not used to treat Restless Legs Syndrome. Take ropinirole at around the same time(s) every day. Follow the directions on your prescription label carefully and ask your doctor or pharmacist to explain any part you do not understand. Take ropinirole exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor. There are other medications that have names similar to the brand name for ropinirole. You should be sure that you receive ropinirole and not one of the similar medications each time you fill your prescription. Be sure that the prescription your doctor gives you is clear and easy to read. You should know the name of your medication and why you are taking it. If you think you were given the wrong medication, talk to your pharmacist. Do not take any medication unless you are certain it is the medication that your doctor prescribed. Swallow the extended-release tablets whole; do not split, chew, or crush them. Your doctor will start you on a low dose of ropinirole and gradually increase your dose to help control your symptoms. If you are taking ropinirole to treat Parkinson's disease, your doctor will probably not increase your dose more often than once a week. If you are taking ropinirole to treat Restless Legs Syndrome, your doctor will probably increase your dose after 2 days, again at the end of the first week, and then not more often than once a week. It may take several weeks before you reach a dose that works for you. If you are taking ropinirole to treat Restless Legs Syndrome, you may receive a starter kit that contains tablets of increasing doses to be taken during the first 2 weeks of your treatment. The dose of medication you will need depends on how well your body responds to the medication, and may be different than the doses contained in the kit. Your doctor will tell you how to use the kit and whether you should take all the tablets it contains. Follow your doctor's directions carefully. Ropinirole controls the symptoms of Parkinson's disease and Restless Legs Syndrome but does not cure these conditions. Continue to take ropinirole even if you feel well. Do not stop taking ropinirole without talking to your doctor. If you are taking ropinirole and you suddenly stop taking the medication, you may experience fever, fast heartbeat, muscle stiffness, sweating, confusion, and other symptoms. If your doctor asks you to stop taking ropinirole, your doctor will probably decrease your dose gradually, over 7 days. If you stop taking ropinirole for any reason, do not start to take the medication again without talking to your doctor. Your doctor will probably want to increase your dose again gradually. Ask your pharmacist or doctor for a copy of the manufacturer's information for the patient. Other uses for this medicine This medication may be prescribed for other uses; ask your doctor or pharmacist for more information. What special precautions should I follow? Before taking ropinirole, ● tell your doctor and pharmacist if you are allergic to ropinirole, any other medications, or any of the ingredients in ropinirole tablets or extended-release tablets. Ask your doctor or pharmacist for a list of ingredients in ropinirole regular or extended-release tablets. ● tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: antidepressants ('mood elevators'); antipsychotics (medications for mental illness); cimetidine (Tagamet, Tagamet HB); fluoroquinolone antibiotics such as ciprofloxacin (Cipro), and norfloxacin (Noroxin); fluvoxamine (Luvox); hormone replacement therapy and hormonal contraceptives (birth control pill, patches, rings, and injections); insulin; lansoprazole (Prevacid); levodopa (in Sinemet, in Stalevo); medications for anxiety and seizures; medications that cause drowsiness; metoclopramide (Reglan); mexiletine (Mexitil); modafanil (Provigil); nafcillin; omeprazole (Prilosec, Zegerid); sedatives; sleeping pills; and tranquilizers. Your doctor may need to change the doses of your medications or monitor you carefully for side effects. Be sure to tell your doctor or pharmacist if you stop taking any medications while you are taking ropinirole. ● tell your doctor if you have ever had an urge to gamble that was difficult to control and if you have or have ever had unexpected daytime sleepiness or a sleep disorder other than restless legs syndrome; high or low blood pressure; a psychotic disorder (mental illness that causes abnormal thinking or perceptions); or heart, liver, or kidney disease. ● tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking ropinirole, call your doctor. ● you should know that ropinirole may make you drowsy or may cause you to suddenly fall asleep during your regular daily activities. You might not feel drowsy or have any other warning signs before you suddenly fall asleep. Do not drive a car,operate machinery, work at heights, or participate in potentially dangerous activities at the beginning of your treatment until you know how the medication affects you. If you suddenly fall asleep while you are doing something such as watching television, talking, eating, or riding in a car, or if you become very drowsy, especially during the daytime, call your doctor. Do not drive, work in high places, or operate machinery until you talk to your doctor. ● remember that alcohol can add to the drowsiness caused by this medication. Tell your doctor if you regularly drink alcoholic drinks. ● tell your doctor if you use tobacco products. Call your doctor if you start or stop smoking during your treatment with ropinirole. Smoking may decrease the effectiveness of this medication. ● you should know that some people who took medications such as ropinirole developed gambling problems or other intense urges or behaviors that were compulsive or unusual for them, such as increased sexual urges or behaviors. There is not enough information to tell whether the people developed these problems because they took the medication or for other reasons. Call your doctor if you have an urge to gamble that is difficult to control, you have intense urges, or you are unable to control your behavior. Tell your family members about this risk so that they can call the doctor even if you do not realize that your gambling or any other intense urges or unusual behaviors have become a problem. ● you should know that ropinirole may cause dizziness, lightheadedness, nausea, or sweating when you get up too quickly from a sitting or lying position. This is more common when you first start taking ropinirole or with an increase in the dose of ropinirole. To avoid this problem, get out of the chair or bed slowly, resting your feet on the floor for a few minutes before standing up. What special dietary instructions should I follow? Unless your doctor tells you otherwise, continue your normal diet. What should I do if I forget a dose? If you are taking regular ropinirole tablets to treat Parkinson's disease and you miss a dose, take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. If you are taking regular ropinirole tablets to treat Restless Legs Syndrome and you miss a dose, skip the missed dose. Take your regular dose 1 to 3 hours before your next bedtime. Do not double the next dose to make up for the missed dose. If you are taking extended-release ropinirole tablets to treat Parkinson's disease and you miss a dose, take the missed dose as soon as you remember it. Return to your regular dosing schedule the next day. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one. What side effects can this medication cause? Ropinirole may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away: ● nausea ● vomiting ● stomach pain ● heartburn or gas ● diarrhea ● constipation ● decrease in appetite ● weight loss ● dizziness ● drowsiness ● tiredness ● weakness ● headache ● sweating or flushing ● confusion ● difficulty remembering or concentrating ● anxiety ● uncontrolled, sudden body movements ● shaking of a part of your body that you cannot control ● decreased sensitivity (response) to touch ● frequent or urgent need to urinate ● difficulty urinating or pain when urinating ● in men, difficulty achieving or maintaining an erection ● back, muscle, or joint pain ● pain, burning, numbness, or tingling in the hands or feet ● swelling of the hands, arms, feet, ankles, or lower legs ● dry mouth Some side effects can be serious. If you experience any of the following symptoms, call your doctor immediately: ● hallucinations (seeing things or hearing voices that do not exist) ● fainting ● chest pain ● slow, fast, or irregular heartbeat ● shortness of breath ● difficulty swallowing ● double vision or other changes in vision People who have Parkinson's disease may have a greater risk of developing melanoma (a type of skin cancer) than people who do not have Parkinson's disease. There is not enough information to tell whether medications used to treat Parkinson's disease such as ropinirole increase the risk of developing skin cancer. You should have regular skin examinations to check for melanoma while you are taking ropinirole even if you do not have Parkinson's disease. Talk to your doctor about the risk of taking ropinirole. Some people taking ropinirole and other similar medications have developed fibrotic changes (scarring or thickening) in their lungs and heart valves. It is not yet known whether this problem is caused by ropinirole. Talk to your doctor about the risk of taking this medication. Ropinirole may cause other side effects. Call your doctor if you have any unusual problems while you are taking this medication. If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting program online [at http://www.fda.gov/Safety/MedWatch] or by phone [1-800-332-1088]. What should I know about storage and disposal of this medication? Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from direct sunlight, excess heat, and moisture (not in the bathroom). Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the proper disposal of your medication. In case of emergency/overdose In case of overdose, call your local poison control center at 1-800-222-1222. If the victim has collapsed or is not breathing, call local emergency services at 911. Symptoms of overdose may include: ● nausea ● vomiting ● dizziness ● fainting ● hallucinations (seeing things or hearing voices that do not exist) ● nightmares ● drowsiness ● confusion ● sweating ● fear when in a small or closed space ● body movements that are difficult to control ● fast, irregular, or pounding heartbeat ● chest pain ● weakness ● cough ● agitation What other information should I know? Keep all appointments with your doctor. Do not let anyone else take your medication.Ask your pharmacist any questions you have about refilling your prescription. It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies. Brand names ● Requip® ● Requip® XL |
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Requip Side Effects
Generic Name: ropinirole It is possible that some side effects of Requip may not have been reported. These can be reported to the FDA here. Always consult a healthcare professional for medical advice. For the Consumer Applies to ropinirole: oral tablet, oral tablet extended release As well as its needed effects, ropinirole (the active ingredient contained in Requip) may cause unwanted side effects that require medical attention. If any of the following side effects occur while taking ropinirole, check with your doctor immediately: More common ● Confusion ● dizziness, faintness, or lightheadedness when getting up from a lying or sitting position suddenly ● 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 Less common ● Abdominal or stomach pain ● bloating or swelling of the face, arms, hands, lower legs, or feet ● blood in the urine ● blurred vision ● burning, pain, or difficulty in urinating ● chest pain ● chills ● cold sweats ● cough ● double vision or other eye or vision problems ● fainting ● fear or nervousness ● feeling of constant movement of self or surroundings ● high or low blood pressure ● irregular or pounding heartbeat ● loss of memory ● mental depression ● pain ● pain in the arms or legs ● pounding in the ears ● rapid weight gain ● sensation of spinning ● slow or fast heartbeat ● sore throat ● sweating ● tightness in chest ● tingling of hands or feet ● tingling, numbness, or prickly feelings ● trouble in concentrating ● troubled breathing ● unusual weight gain or loss ● vomiting Rare ● Anxiety ● buzzing or ringing in the ears ● changes in vision ● fever ● headache ● joint pain ● loss of bladder control ● muscle cramps, pain, or spasms ● nasal congestion ● runny nose ● sneezing ● trouble with swallowing ● unusual urges If any of the following symptoms of overdose occur while taking ropinirole, get emergency help immediately: Symptoms of overdose ● Agitation ● grogginess ● increase in unusual body movements, especially of the face or mouth ● increased coughing ● increased sweating ● lack or loss of strength ● nightmares Some ropinirole side effects may not need any medical attention. As your body gets used to the medicine these side effects may disappear. Your health care professional may be able to help you prevent or reduce these side effects, but do check with them if any of the following side effects continue, or if you are concerned about them: Less common ● Abnormal dreams ● acid or sour stomach ● back pain ● belching ● decrease in sexual desire or performance ● difficulty having a bowel movement (stool) ● dryness of mouth ● flushing ● general feeling of discomfort or illness ● heartburn or gas ● hot flashes ● indigestion ● loss of appetite ● tremor ● weight loss ● yawning For Healthcare Professionals
Applies to ropinirole: oral kit, oral tablet, oral tablet extended release Gastrointestinal Parkinson's disease: Very common (10% or more): Nausea (up to 60%), vomiting (up to 12%) Common (1% to 10%): Dry mouth, abdominal pain, anorexia, dyspepsia, flatulence, constipation, diarrhea, dysphagia, increased saliva, heartburn Restless Leg Syndrome: Very common (10% or more): Nausea (up to 40%), vomiting (up to 12.9%) Common (1% to 10%): Diarrhea, dyspepsia, dry mouth, abdominal pain upper Uncommon (0.1% to 1%) Nervous system Parkinson's disease Very common (10% or more): Dizziness (40%), somnolence (40%), dyskinesia (34%), headache (17%) Common (1% to 10%): Hyperkinesia, hypesthesia, hypokinesia, paresis, paresthesia, tremor Uncommon (0.1% to 1%): Sudden onset of sleep, excessive daytime somnolence Restless Leg Syndrome: Very common (10% or more): Headache (up to 22.3%), somnolence (12%), dizziness (up to 12.9%) Common (1% to 10%): Paresthesia, migraine, paradoxical augmentation and rebound of restless leg syndrome Psychiatric Parkinson's disease Very common (10% or more): Hallucination (10%) Common (1% to 10%): Amnesia, impaired concentration, confusion, amnesia, anxiety, abnormal dreaming, nervousness Uncommon (0.1% to 1%): Psychotic reactions other than hallucinations, included delirium, delusions, paranoia Frequency not reported: Aggression Postmarketing reports: Impulse control disorders included pathological gambling and hypersexuality and increased libido Restless Leg Syndrome: Common (1% to 10%): Nervousness Postmarketing reports: Impulse control disorders included pathological gambling and hypersexuality and increased libido Cardiovascular Parkinson's disease: Very common (10% or more): Syncope (up to 12%) Common (1% to 10%): Hypertension, hypotension, orthostatic symptoms, chest pain, dependent edema, leg edema, flushing, extrasystoles, atrial fibrillation, palpitation, tachycardia, peripheral ischemia Restless Leg Syndrome: Common (1% to 10%): Syncope Uncommon (0.1% to 1%): Orthostatic hypotension, peripheral edema Frequency not reported: Hypotension Immunologic Common (1% to 10%): Influenza, viral infection General The most commonly reported adverse reaction reported in patients with early Parkinson's disease included nausea, somnolence, dizziness, syncope, asthenic conditions, viral infection, leg edema, vomiting, and dyspepsia. Among patients with advance Parkinson's disease, the more commonly reported adverse reactions included dyskinesia, somnolence, nausea, dizziness, confusion, hallucinations, sweating, and headache. The most commonly reported adverse reactions in patients with restless legs syndrome included nausea, vomiting, somnolence, dizziness, and a asthenic condition. Respiratory Parkinson's disease Common (1% to 10%): Yawning, upper respiratory tract infection, dyspnea, bronchitis, pharyngitis, rhinitis, sinusitis Restless Leg Syndrome: Very common (10% or more): Upper respiratory infection (10.7%) Common (1% to 10%): Nasopharyngitis, cough, nasal congestion, rhinitis, sinusitis Ocular Parkinson's disease: Common (1% to 10%): Eye abnormality, abnormal vision, xerophthalmia, diplopia Metabolic Parkinson's disease Common (1% to 10%): Decreased weight Genitourinary Common (1% to 10%): Impotence, urinary tract infection, pyuria, urinary incontinence, urinary tract infection Other Asthenic conditions include asthenia, fatigue, and/or malaise Parkinson's disease Very common (10% or more): Asthenic condition (16%) Common (1% to 10%): Pain, vertigo Restless Leg Syndrome: Very common (10% or more): Fatigue (10.4%) Common (1% to 10%): Asthenic condition, vertigo Postmarketing reports: Musculoskeletal Common (1% to 10%): Arthralgia, arthritis, extremity pain, back pain, injury, myalgia[Ref] Dermatologic Common (1% to 10%): Increased sweating Hematologic Parkinson's disease Common (1% to 10%): Anemia Hepatic Parkinson's disease Common (1% to 10%): Increased alkaline phosphatase Frequency not reported: Increased liver enzymes Hypersensitivity Frequency not reported: Hypersensitivity reactions including urticarial, angioedema, rash, pruritus References 1. "Product Information. Requip (ropinirole)." SmithKline Beecham, Philadelphia, PA. 2. Cerner Multum, Inc. "Australian Product Information." O 0 3. Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0 |
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NON-ERGOLINE DOPAMINE AGONISTS
These new dopamine agonists include ropinirole and pramipexole. Ropinirole Ropinirole is a potent and selective dopamine D2-type receptor agonist and was the first available non-ergoline orally active dopamine agonist. Studies have shown that ropinirole is effective when used as monotherapy in early Parkinson's disease, providing symptomatic relief for up to 5 years. It is also effective as adjunct therapy in patients with motor fluctuations: 65% of patients taking ropinirole with levodopa had a 30% increase in “on” time compared with 39% in the placebo group (p<0.077). A recent 6 month study in patients with motor fluctuations showed that the use of ropinirole permits a >20% reduction in levodopa dose, while significantly reducing the time spent “off” compared with placebo (35% v13%; p=0.003). The results of a 5 year, double blind, randomised trial comparing ropinirole with levodopa plus benserazide in the treatment of 268 patients with early Parkinson's disease have been recently presented.21 22 Forty seven per cent of ropinirole patients and 51% of levodopa patients completed the 5 year study; of these, 34% of patients on ropinirole did so on monotherapy. In those patients on ropinirole who were given levodopa supplements, a lower dose of levodopa was required compared with patients on levodopa alone (427 mg/day v 753 mg/day respectively). Similar clinical efficacy of treatment in the ropinirole and levodopa groups was demonstrated throughout the study (assessed by change in ADL score). Ropinirole monotherapy was also found to be associated with a significantly lower incidence of dyskinesia than levodopa monotherapy (5% v 36% respectively; p<0.0001). In the intention to treat ropinirole arm of the study (including levodopa rescued patients), the incidence of dyskinesia was still significantly reduced (20% for ropinirole v 46% for levodopa; p<0.001). Adverse experiences, typical for dopaminergic agents, caused 27% of ropinirole patients and 29% of levodopa patients to withdraw from the study prematurely (not significantly different). A 3 year, randomised, double blind study comparing the actions of ropinirole and bromocriptine in 335 patients with early Parkinson's disease has also just been completed.18 Patients initially received either ropinirole (n=168), or bromocriptine (n=167) as monotherapy. Where insufficient relief from symptoms was achieved, supplementary levodopa was added and the study allowed to continue. In patients completing the study, both agonists were found to be effective for giving symptomatic relief; however, patients maintained a significantly better functional status on ropinirole than on bromocriptine. This suggested an increased efficacy of the non-ergoline agonist for treatment of early Parkinson's disease over this 3 year period. Pramipexole In vitro electrophysiological studies suggest that pramipexole has greater potency for stimulating dopamine receptors than the ergoline agonists.49 Pramipexole stimulates D2-like receptors, with highest affinity for D3 receptors. The efficacy of pramipexole in patients with Parkinson's disease has been demonstrated in some short term, placebo controlled trials. Use of pramipexole as adjunct therapy to levodopa has been investigated in advanced Parkinson's disease. A three times daily regime has generally been employed. In one study, 12 patients with motor fluctuations received adjunct pramipexole in an 11 week prospective, single blind, parallel group, placebo controlled trial. In this trial pramipexole significantly improved ADL assessed with UPDRS (p<0.05). Use of pramipexole allowed a reduction in levodopa dose of up to 30% (p<0.05). In another trial conducted in 26 centres across the United States and Canada, 181 patients with advanced Parkinson's disease treated with levodopa were randomly scheduled to receive adjunctive therapy with either pramipexole or placebo for 32 weeks.52 This trial found that pramipexole decreased time in “off“ by 31% (p=0.0006) and permitted a 27% decrease in levodopa dose (p=0.0001). A double blind, placebo controlled study of adjunct use of pramipexole and bromocriptine in 247 patients showed a trend towards pramipexole being more effective than bromocriptine in patients with advanced Parkinson's disease and motor fluctuations.51 Adjunct use of pramipexole improved the ADL and motor sections of the UPDRS by 27% and 34% although at the expense of increased dyskinesias and nausea. The efficacy, safety, and tolerability of pramipexole as an add on drug has also been examined in an 11 week, double blind, placebo controlled, randomised trial in 78 patients with advanced disease and motor fluctuations.53 Pramipexole or placebo was given, as add on therapy, to patients who had been previously stabilised on antiparkinsonian medication. The mean UPDRS total score was reduced by 37.3% under pramipexole compared with 12.2% under placebo (p<0.001). Patients who received pramipexole also reported a 12% reduction in “off” periods compared with a 2% increase with placebo. The efficacy of pramipexole has been assessed over 9 weeks in 55 patients with de novo Parkinson's disease.54 Compared with placebo, those patients receiving pramipexole showed a 40% improvement in ADL (p=0.002) and a 44% improvement in the motor score of the UPDRS (p=0.10). In a follow up study by the Parkinson Study Group, 264 patients with early Parkinson's disease were randomised to either pramipexole or placebo for 10 weeks. Pramipexole led to a 20% improvement in total UPDRS score and was well tolerated. Nausea and somnolence were the most common adverse events. Side effects of non-ergoline dopamine agonists The non-ergoline dopamine agonists ropinirole and pramipexole seem to be well tolerated although they are still associated with the usual dopaminergic side effects; nausea, hypotension, somnolence, and exacerbation of dyskinesias. Disappointingly, both can cause confusion and hallucinations when used as adjunct medication. To date, ropinirole and pramipexole do not seem to cause side effects specific to ergots such as skin inflammation, digital vasospasm, and paraesthesias, pleural effusion, pulmonary infiltrates, or erythromelalgia. |
