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Uses

Alzheimer’s Disease

Management of mild to moderate dementia of the Alzheimer’s type.

Dosage and Administration

Administration

Oral Administration

Administer orally twice daily (morning and evening) with food. (See Absorption under Pharmacokinetics.)

Administer oral solution using the oral dosing syringe provided; follow the patient instructions provided by the manufacturer. Oral solution may be mixed in a small glass of compatible fluids (see Compatibility under Stability); mix completely and drink the entire contents.

Oral solution and tablets may be interchanged at equal doses.

Dosage

Available as rivastigmine tartrate; dosage is expressed in terms of rivastigmine.

Adults

Alzheimer’s Disease

Oral

Initially, 1.5 mg twice daily.

If well tolerated, increase dosage after ≥2 weeks to 3 mg twice daily; attempt to increase dosage to 4.5 mg twice daily and 6 mg twice daily after ≥2 weeks of treatment at the previous dosage.

If adverse effects intolerable, discontinue for several doses and then resume at the same or the immediately preceding (lower) dosage in the titration regimen. However, if therapy is interrupted for more than several days, restart drug using the recommended initial dosage (i.e., 1.5 mg twice daily) and titration schedule until the previous maintenance dosage is reached (to decrease the risk of severe vomiting and related sequelae [e.g., spontaneous esophageal rupture].) (see GI Effects under Cautions.)

Prescribing Limits

Adults

Alzheimer’s Disease

Oral

Maximum 6 mg twice daily.

Special Populations

Dosage in Hepatic Impairment

Decreased clearance; however, dosage adjustment may not be necessary since dosage is titrated to adverse effect tolerability.

Dosage in Renal Impairment

Clearance decreased with moderate impairment and increased with severe impairment; however, dosage adjustment may not be necessary since dosage is titrated to adverse effect tolerability.

Cautions

Contraindications

• Known hypersensitivity to rivastigmine, other carbamates, or any ingredient in the formulation.

Warnings/Precautions

Warnings

GI Effects

Possible occurrence of clinically important adverse GI effects, including nausea, vomiting, anorexia, and weight loss.

Severe vomiting and spontaneous rupture of the esophagus were reported in a patient who resumed therapy by taking a single 4.5-mg dose after therapy had been interrupted for 8 weeks. Therefore, manufacturer recommends strict adherence to prescribed initial dosages and titration schedules (see Alzheimer’s Disease under Dosage and Administration), particularly when reinitiating therapy following temporary interruption lasting longer than several days.

Possible increased gastric acid secretion. Monitor closely for manifestations of active or occult GI bleeding, especially in patients at increased risk (e.g., history of ulcer disease, concomitant NSAIA therapy).

Cardiovascular Effects

Possible bradycardia or other vagotonic effects on the heart. Use with caution in patients with sick sinus syndrome or other supraventricular cardiac conduction abnormalities.

Genitourinary Effects

Potential urinary obstruction secondary to cholinergic activity.

Nervous System Effects

Possible increased risk of seizures secondary to cholinergic activity or possibly as a manifestation of Alzheimer’s disease.

Respiratory Effects

Use with caution in patients with a history of asthma or obstructive pulmonary disease.

Specific Populations

Pregnancy

Category B.

Lactation

Not known whether rivastigmine is distributed into milk. Use is not recommended.

Pediatric Use

Safety and efficacy not established in children.

Geriatric Use

Decreased clearance; however, clinical outcome of therapy not predicted by age.

Common Adverse Effects

Nausea, vomiting, anorexia, dyspepsia, asthenia.

Drug Interactions

Minimally metabolized by CYP isoenzymes. Pharmacokinetic interaction unlikely with drugs metabolized by CYP isoenzymes or with CYP enzyme inducers or inhibitors.

Protein-bound Drugs

Pharmacokinetic interaction unlikely.

Specific Drugs