Overview
11 DESCRIPTION Galantamine hydrobromide extended-release capsules contain galantamine, a reversible, competitive acetylcholinesterase inhibitor, as the hydrobromide salt. Galantamine hydrobromide is known chemically as (4a S ,6 R ,8a S )- 4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-6 H -benzofuro [3a,3,2- ef ][2]benzazepin-6-ol hydrobromide.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Although the etiology of cognitive impairment in Alzheimer's disease (AD) is not fully understood, it has been reported that acetylcholine-producing neurons degenerate in the brains of patients with Alzheimer's disease. The degree of this cholinergic loss has been correlated with degree of cognitive impairment and density of amyloid plaques (a neuropathological hallmark of Alzheimer's disease). Galantamine, a tertiary alkaloid, is a competitive and reversible inhibitor of acetylcholinesterase. While the precise mechanism of galantamine's action is unknown, it is postulated to exert its therapeutic effect by enhancing cholinergic function.
Indications
- 1 INDICATIONS AND USAGE Galantamine hydrobromide extended-release capsules are indicated for the treatment of mild to moderate dementia of the Alzheimer's type. Galantamine hydrobromide is a cholinesterase inhibitor indicated for the treatment of mild to moderate dementia of the Alzheimer’s type ( 1 )
Common Doses
- 8 mg
- 16 mg
- 24 mg
- 59 mL
Dosage
2 DOSAGE AND ADMINISTRATION Recommended starting dosage is 8 mg/day in morning; increase to initial maintenance dose of 16 mg/day after a minimum of 4 weeks. Based on clinical benefit and tolerability, dosage may be increased to 24 mg/day after a minimum of 4 weeks at 16 mg/day. ( 2.1 ) Take with food; ensure adequate fluid intake during treatment ( 2.1 ) Hepatic impairment: should not exceed 16 mg/day for moderate hepatic impairment; do not use in patients with severe hepatic impairment ( 2.
Contraindications
- 4 CONTRAINDICATIONS Galantamine hydrobromide extended-release capsules are contraindicated in patients with known hypersensitivity to galantamine hydrobromide or to any excipients used in the formulation. Known hypersensitivity to galantamine hydrobromide or any excipients ( 4 )
Side Effects
- 6 ADVERSE REACTIONS Serious adverse reactions are discussed in more detail in the following sections of the labeling: Serious Skin Reactions [see Warnings and Precautions ( 5.1 )] Cardiovascular Conditions [see Warnings and Precautions ( 5.3 )] Gastrointestinal Conditions [see Warnings and Precautions ( 5.4 )] Genitourinary Conditions [see Warnings and Precautions ( 5.5 )] Neurological Conditions [see Warnings and Precautions ( 5.6 )] Pulmonary Conditions [see Warnings and Precautions ( 5.7 )] Deaths in Patients with Mild Cognitive Impairment (MCI) [see Warnings and Precautions ( 5.
Interactions
- 7 DRUG INTERACTIONS Potential to interfere with the activity of anticholinergic medications ( 7.1 ) Synergistic effect expected when given concurrently with succinylcholine, other cholinesterase inhibitors, similar neuromuscular blocking agents, or cholinergic agonists ( 7.2 ) 7.1 Use with Anticholinergics Galantamine has the potential to interfere with the activity of anticholinergic medications [see Clinical Pharmacology ( 12.3 )] . 7.