Rivastigmine adverse effects

The recommended starting dose of rivastigmine is 1.5 mg twice a day. If dose is well tolerated, after a minimum of 2 weeks of treatment, the dose may be increased to 3 mg twice a day. Subsequent increases to 4.5 and 6 mg twice/day should be attempted after a minimum of 2 weeks at the previous dose. If adverse effects (eg, nausea, vomiting, abdominal pain, loss of appetite) cause intolerance during treatment, instruct the patient to discontinue treatment for several doses and then restart at the same or next lower dose level. If treatment is interrupted for longer than several days, reinitiate treatment with the lowest daily dose and titrate as described above. The maximum dose is 6 mg twice/day (12 mg/day). 

Rivastigmine (1) was the second drug after donepezil in a class of second-generation acetylcholinesterase inhibitors to become commercially available. It is now marketed in over 60 countries worldwide, including those in Europe and South America and the United Kingdom. It has central selectivity, suggesting fewer peripheral adverse effects. These include nausea, vomiting, abdominal pain, and anorexia (2,3). Daily doses up to 12 mg were tolerated and produced improvement in patients with Alzheimer s disease (4). 

Based on an electrocardiographic analysis of pooled data from four 26-week, phase III, multicenter, double-blind, placebo-controlled trials of rivastigmine (n = 2791), there were no adverse effects on cardiac function (19). Rivastigmine can therefore be safely given to patients with Alzheimer s disease, without the need for cardiac monitoring. 

Of the acetylcholinesterase inhibitors, tacrine, methoxy-tacrine, metrifonate, donepezil hydrochloride, and rivastigmine are used in the treatment of Alzheimer s disease. In 12-30% of patients with Alzheimer s disease, tacrine causes an increase in hepatic transaminase activity. Abdominal adverse effects are very frequent, for example nausea, anorexia, diarrhea. The peripheral cholinomimetic effects of tacrine occur in a very high proportion of patients, probably the majority. The hepatic effects seem to be such that the use of these new (and in some cases still experimental) drugs would not be justified in... 

Fluvoxamine markedly increases the levels of tacrine, and increases its cholinei ic adverse effects, whereas fluoxetine, paroxetine, and sertraline are not expected to interact. Paroxetine and fluoxetine may increase donepezil and galantamine levels. Sertraline does not appear to have a pharmacokinetic interaction with donepezil, and concurrent use seems generally well tolerated however, one report describes hepatotoxicity, possibly as a result of their concurrent use. Rivastigmine and fluoxetine appear not to interact. 

Gi effects Rivastigmine is associated with significant Gl adverse reactions, including nausea and vomiting, anorexia, and weight loss. 

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