Drug Action
Rivastigmine is a reversible non- competitive inhibitor of acetylcholinesterases.
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Drug reference
Rivastigmine is a reversible non- competitive inhibitor of acetylcholinesterases.
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Mild to moderate dementia in Alzheimer’s disease ▶BY MOUTH ▶Adult: Initially 1.5 mg twice daily, increased in steps of 1.5 mg twice daily, dose to be increased at intervals of at least 2 weeks according to response and tolerance; usual dose 3–6 mg twice daily (max. per dose 6 mg twice daily), if treatment interrupted for more than several days, retitrate from 1.5 mg twice daily ▶BY TRANSDERMAL APPLICATION USING PATCHES ▶Adult: Apply 4.6 mg/24 hours daily for at least 4 weeks, increased if tolerated to 9.5 mg/24 hours daily for a further 6 months, then increased if necessary to 13.3 mg/24 hours daily, increase to 13.3 mg/24 hours patch if well tolerated and cognitive deterioration or functional decline demonstrated; use caution in patients with body-weight less than 50 kg, if treatment interrupted for more than 3 days, retitrate from 4.6 mg/24 hours patch Mild to moderate dementia in Parkinson’s disease ▶BY MOUTH ▶Adult: Initially 1.5 mg twice daily, increased in steps of 1.5 mg twice daily, dose to be increased at intervals of at least 2 weeks according to response and tolerance; usual dose 3–6 mg twice daily (max. per dose 6 mg twice daily), if treatment interrupted for more than several days, retitrate from 1.5 mg twice daily DOSE EQUIVALENCE AND CONVERSION ▶When switching from oral to transdermal therapy, patients taking 3–6 mg by mouth daily should initially switch to 4.6 mg/24 hours patch, then titrate as above. Patients taking 9 mg by mouth daily should switch to 9.5 mg/24 hours patch if oral dose stable and well tolerated; if oral dose not stable or well tolerated, patients should switch to 4.6 mg/24 hours patch, then titrate as above. Patients taking 12 mg by mouth daily should switch to 9.5 mg/24 hours patch. The first patch should be applied on the day following the last oral dose
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Bladder outflow obstruction. conduction abnormalities. duodenal ulcers. gastric ulcers. history of asthma. history of chronic obstructive pulmonary disease. history of seizures. risk of fatal overdose with patch administration errors. sick sinus syndrome. susceptibility to ulcers CAUTIONS, FURTHER INFORMATION ▶Elderly For acetylcholinesterase inhibitors, prescription potentially inappropriate (STOPP criteria) in patients with a known history of persistent bradycardia (heart rate less than 60 beats per minute), heart block, recurrent unexplained syncope or concurrent treatment with drugs that reduce heart rate (risk of cardiac conduction failure, syncope and injury). See also Prescribing in the elderly p. 33.
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NICE decisions ▶Donepezil, galantamine, rivastigmine, and memantine for the treatment of Alzheimer’s disease (updated June 2018) NICE TA217 The three acetylcholinesterase (AChE) inhibitors donepezil, galantamine, and rivastigmine as monotherapies are recommended as options for managing mild to moderate Alzheimer’s disease under all of the conditions specified below and in recommendation 1.5.5 of the NICE guideline on dementia. If prescribing an AChE inhibitor (donepezil, galantamine, or rivastigmine), treatment should normally be started with the drug with the lowest acquisition cost (taking into account required daily dose and the price per dose once shared care has started). However, an alternative AChE inhibitor could be prescribed if it is considered appropriate when taking into account adverse event profile, expectations about adherence, medical comorbidity, possibility of drug interactions and dosing profiles. Healthcare professionals should not rely solely on assessment scales to determine the severity of Alzheimer’s disease when the patient has learning or other disabilities, or other communication difficulties. Nervous system www.nice.org.uk/guidance/ta217 EXELON ® PATCHES Scottish Medicines Consortium (SMC) decisions The Scottish Medicines Consortium has advised (November 2007) that Exelon ® patches should be restricted for use in patients with moderately severe Alzheimer’s disease under the conditions of the NICE guidance (September 2007) and when a transdermal patch is an appropriate choice of formulation.
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→Appendix 1: anticholinesterases, centrally acting
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GENERAL SIDE-EFFECTS ▶Common or very common Anxiety. appetite decreased. arrhythmias. asthenia. dehydration. depression. diarrhoea. dizziness. drowsiness. fall. gastrointestinal discomfort. headache. hyperhidrosis. hypersalivation. hypertension. movement disorders. nausea. skin reactions. syncope. tremor. urinary incontinence. urinary tract infection. vomiting. weight decreased ▶Uncommon Aggression. atrioventricular block ▶Rare or very rare Pancreatitis. seizure ▶Frequency not known Hepatitis SPECIFIC SIDE-EFFECTS ▶Common or very common ▶With oral use Confusion. gait abnormal. hallucinations. malaise. parkinsonism. sleep disorders ▶Uncommon ▶With oral use Hypotension ▶With transdermal use Gastric ulcer ▶Rare or very rare ▶With oral use Angina pectoris. gastrointestinal disorders. gastrointestinal haemorrhage ▶Frequency not known ▶With transdermal use Hallucination. nightmare SIDE-EFFECTS, FURTHER INFORMATION Dose should be started low and increased according to response if tolerated. Treatment should be interrupted if dehydration resulting from prolonged vomiting or diarrhoea occurs and withheld until resolution—retitrate dose if necessary. Transdermal administration is less likely to cause side-effects.
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Manufacturer advises caution (risk of increased exposure; no information available in severe impairment). Dose adjustments Manufacturer advises cautious dose titration according to individual tolerability.
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Dose adjustments Titrate according to individual tolerability.
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Monitor body-weight.
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▶With transdermal use Apply patches to clean, dry, non-hairy, non-irritated skin on back, upper arm, or chest, removing after 24 hours and siting a replacement patch on a different area (avoid using the same area for 14 days).
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There can be variation in the licensing of different medicines containing the same drug. Oral solution CAUTIONARY AND ADVISORY LABELS 21 ▶Rivastigmine (Non-proprietary) Rivastigmine (as Rivastigmine hydrogen tartrate) 2 mg per 1 ml Rivastigmine 2mg/ml oral solution sugar free sugar-free | 120 ml P £96.82 DT = £96.82 Capsule CAUTIONARY AND ADVISORY LABELS 21, 25 ▶Rivastigmine (Non-proprietary) Rivastigmine (as Rivastigmine hydrogen tartrate) 1.5 mg Rivastigmine 1.5mg capsules | 28 capsule P £28.26 DT = £3.22 | 56 capsule P £3.82 Rivastigmine (as Rivastigmine hydrogen tartrate) 3 mg Rivastigmine 3mg capsules | 28 capsule P £33.25 DT = £3.69 | 56 capsule P £4.88–£5.22 Rivastigmine (as Rivastigmine hydrogen tartrate) 4.5 mg Rivastigmine 4.5mg capsules | 28 capsule P £33.25 DT = £32.09 | 56 capsule P £47.02–£66.51 Rivastigmine (as Rivastigmine hydrogen tartrate) 6 mg Rivastigmine 6mg capsules | 28 capsule P £32.78 DT = £32.78 | 56 capsule P £54.34–£66.51 ▶Nimvastid (Consilient Health Ltd) Rivastigmine (as Rivastigmine hydrogen tartrate) 1.5 mg Nimvastid 1.5mg capsules | 28 capsule P £28.26 DT = £3.22 Rivastigmine (as Rivastigmine hydrogen tartrate) 3 mg Nimvastid 3mg capsules | 28 capsule P £28.26 DT = £3.69 Rivastigmine (as Rivastigmine hydrogen tartrate) 4.5 mg Nimvastid 4.5mg capsules | 28 capsule P £28.26 DT = £32.09 Rivastigmine (as Rivastigmine hydrogen tartrate) 6 mg Nimvastid 6mg capsules | 28 capsule P £28.26 DT = £32.78 Transdermal patch ▶Almuriva (Sandoz Ltd) Rivastigmine 4.6 mg per 24 hour Almuriva 4.6mg/24hours transdermal patches | 30 patch P £77.97 DT = £77.97 Rivastigmine 9.5 mg per 24 hour Almuriva 9.5mg/24hours transdermal patches | 30 patch P £77.97 DT = £19.97 ▶Alzest (Dr Reddy’s Laboratories (UK) Ltd) Rivastigmine 4.6 mg per 24 hour Alzest 4.6mg/24hours transdermal patches | 30 patch P £35.10 DT = £77.97 Rivastigmine 9.5 mg per 24 hour Alzest 9.5mg/24hours transdermal patches | 30 patch P £19.97 DT = £19.97 ▶Exelon (Novartis Pharmaceuticals UK Ltd) Rivastigmine 4.6 mg per 24 hour Exelon 4.6mg/24hours transdermal patches | 30 patch P £77.97 DT = £77.97 Rivastigmine 9.5 mg per 24 hour Exelon 9.5mg/24hours transdermal patches | 30 patch P £77.97 DT = £19.97 Rivastigmine 13.3 mg per 24 hour Exelon 13.3mg/24hours transdermal patches | 30 patch P £77.97 DT = £77.97 ▶Rivatev (Teva UK Ltd) Rivastigmine 13.3 mg per 24 hour Erastig 13.3mg/24hours transdermal patches | 30 patch P £73.90 DT = £77.97 ▶Voleze (Advanz Pharma) Rivastigmine 4.6 mg per 24 hour Voleze 4.6mg/24hours transdermal patches | 30 patch P £77.97 DT = £77.97 Rivastigmine 13.3 mg per 24 hour Voleze 13.3mg/24hours transdermal patches | 30 patch P £77.97 DT = £77.97 DOPAMINERGIC DRUGS › NMDA RECEPTOR ANTAGONISTS
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EXELON ® PATCHES Advise patients and carers of patch administration instructions, particularly to remove the previous day’s patch before applying the new patch— consult product literature.
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Initially 1.5 mg twice daily, increased in steps of
First-line fragment. Read the complete Indications and Dose section above.
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Apply 4.6 mg/24 hours daily for at least 4 weeks,
First-line fragment. Read the complete Indications and Dose section above.
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Initially 1.5 mg twice daily, increased in steps of
First-line fragment. Read the complete Indications and Dose section above.
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