Rivastigmine

Registered South African indications:

• Dementia

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients 
• Hypersensitivity to other carbamate derivatives
• Previous history of application site reactions with rivastigmine patch

Cautions

• Breastfeeding 
• Pregnancy
• Severe hepatic impairment 
• High doses
• Risk factors for torsades de pointes or QT prolongation 
• Active gastric or duodenal ulcers
• Asthma 
• Chronic obstructive pulmonary disease
• Seizure disorders 
• Urinary obstruction 
• Severe dementia 
• Dementia associated with Parkinson's disease
• Age-related cognitive decline
• Low body weight (< 50kg)

Forms avail. in SA and covered in this monograph: cap 

Alzheimer's dementia - mild to moderate
Dementia in patients with idiopathic Parkinson's disease - mild to moderate

• Oral (cap): Initial: 1.5mg, 12hrly; Titrate by 1.5mg, 12hrly at intervals of 2 weeks; Maintenance: 3-6mg, 12hrly; Max: 12mg/24hrs 

If treatment is interrupted for more than three days, it should be re-initiated at 1.5mg twice daily and titrated as above

Treatment should be reassessed at regular intervals

Discontinue treatment if the rate of decline in dementia symptoms is not altered favourably after 3 months of maintenance dose treatment or when evidence of a therapeutic effect is no longer present

Not established for use in children

Pregnancy 

• Caution; not recommended 
• In pregnant animals, rivastigmine and/or metabolites crossed the placenta. It is not known if this occurs in humans
• No clinical data on exposed pregnancies are available
• In peri/postnatal studies in rats, an increased gestation time was observed
• Rivastigmine should not be used during pregnancy unless clearly necessary

Breastfeeding 

• Caution; not recommended
• In animals, rivastigmine is excreted into human milk
• Therefore, women on rivastigmine should not breastfeed

Fertility 

• No adverse effects of rivastigmine were observed on fertility or reproductive performance in rats 
• Effects of rivastigmine on human fertility are not known

Renal Impairment

• No dose adjustment recommended

 Hepatic Impairment 

• Severe: Caution; no information available

Elderly 

• No dose adjustment recommended

Porphyria Information

• Probably not porphyrinogenic (PNP)

Central Nervous System Disorders

• Restlessness
• Fatigue 
• Visual hallucinations 
• Depression
• Tremor
• Dizziness
• Headache
• Bradykinesia
• Dyskinesia
• Hypokinesia
• Cogwheel rigidity
• Dystonia
• Gait disturbance 
• Nightmares 
• Agitation
• Confusion
• Anxiety
• Insomnia
• Aggression
• Restlessness
• Dizziness
• Headache
• Somnolence
• Tremor
• Syncope
• Seizures
• Extrapyramidal symptoms

Cardiovascular Disorders

• Angina pectoris
• Cardiac arrhythmia
• Sick sinus syndrome
• Hypertension
• Hypotension

Gastrointestinal Disorders

• Nausea and vomiting
• Diarrhoea
• Abdominal pain
• Dyspepsia
• Gastric and duodenal ulcers
• Gastrointestinal haemorrhage
• Oesophageal rupture
• Salivary hypersecretion 

Hepatobiliary Disorders

• Pancreatitis 
• Hepatitis 
• Elevated hepatic function test

Genitourinary Disorders 

• Urinary tract infection 

Endocrine and Metabolic Disorders 

• Weight loss
• Decreased appetite
• Dehydration
• Anorexia 

Skin and Subcutaneous Tissue Disorders

• Hyperhydrosis
• Allergic dermatitis
• Rash 
• Pruritis

• Succinylcholine-type muscle relaxants
• Anticholinergic agents 
• Beta blockers 
• Class III antiarrhythmic agents
• Calcium channel blockers 
• Digitalis glycoside
• Pilocarpine
• Chlorpromazine
• Levomepromazine
• Sulpiride
• Sultopride
• Amisulpride
• Tiapride
• Veralipride
• Pimozide
• Haloperidol
• Droperidol
• Cisapride
• Citalopram
• Diphemanil
• Erythromycin (IV)
• Halofantrine
• Mizolastine
• Methadone
• Pentamidine
• Moxifloxacin

None routine. Specific cases may require

• ECG
• Weight

Rivastigmine increases acetylcholine in the central nervous system through reversible inhibition of its hydrolysis by cholinesterase. This leads to an increased concentration of acetylcholine at cholinergic synapses.

Capsule 3mg

• Exelon (Novartis) originator

Capsule 4.5mg

• Exelon (Novartis) originator