Evista Clinical Pharmacology

Drug Library
Evista - Clinical Pharmacology [Raloxifene]

Antacids ?

Concurrent administration of calcium carbonate or aluminum and magnesium hydroxide-containing antacids does not affect the systemic exposure of raloxifene.

Corticosteroids ? The chronic administration of raloxifene in postmenopausal women has no effect on the pharmacokinetics of methylprednisolone given as a single oral dose. Cholestyramine ? See PRECAUTIONS.

Cyclosporine ? The co-administration of EVISTA with cyclosporine has not been evaluated. Digoxin ? Raloxifene has no effect on the pharmacokinetics of digoxin.
Warfarin ? See PRECAUTIONS.

ANIMAL PHARMACOLOGY

The skeletal effects of raloxifene treatment were assessed in ovariectomized rats and monkeys.

In rats, raloxifene prevented increased bone resorption and bone loss after ovariectomy. There were positive effects of raloxifene on bone strength, but the effects varied with time. Cynomolgus monkeys were treated with raloxifene or conjugated estrogens for 2 years. In terms of bone cycles, this is equivalent to approximately 6 years in humans. Raloxifene and estrogen suppressed bone turnover, and increased BMD in the lumbar spine and in the central cancellous bone of the proximal tibia.

In this animal model, there was a positive correlation between vertebral compressive breaking force and BMD of the lumbar spine. Histologic examination of bone from rats and monkeys treated with raloxifene showed no evidence of woven bone, marrow fibrosis, or mineralization defects. These results are consistent with data from human studies of radiocalcium kinetics and markers of bone metabolism, and are consistent with the action of EVISTA as a skeletal antiresorptive agent.

CLINICAL STUDIES

In postmenopausal women with osteoporosis, EVISTA reduced the risk of vertebral fractures.

EVISTA also increased BMD of the spine, hip, and total body. Similarly, in early postmenopausal women without osteoporosis (women with normal or low BMD without fracture), EVISTA increased spine, hip, and total body BMD relative to calcium alone at 24 months. The effect on hip bone mass was similar to that for the spine.