Drug reference

Raloxifene

Selective oestrogen receptor modulator (benzothiophene SERM) · Treatment and prevention of postmenopausal osteoporosis

Also known as Raloxifene hydrochloride

START

60 mg PO once daily; with calcium/vitamin D as needed

TYPICAL MAX

60 mg/day (fixed)

STOP IF

VTE event, prolonged immobilisation (stop ≥72 h before/during), stroke

WATCH

VTE risk/symptoms, stop before prolonged immobilisation, bone density, stroke risk in CV disease

CDSCO approvedSchedule HATC G03XC01

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 6h · absorption (effect over months)
PEAK: 6h · Cmax
t½: 1.2d · plasma t½
DURATION: 1d · once-daily

EXCRETION

Glucuronidation; mainly faecal, minimal renal

route + CYP

INTERACTIONS

7 major

SEVERE in our sources

PREGNANCY

Contraindicated — not for premenopausal/pregnant women; potential fetal harm

FDA category + note

Top interactionssee all 9 →

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Available in India

14 branded formulations. Look up specific brands in the Drugs workspace.

Mechanism

Oestrogen-receptor agonist in bone (reduces resorption, increases BMD) and lipids, antagonist in breast and (neutral/antagonist) endometrium → osteoporosis treatment and breast-cancer risk reduction without endometrial stimulation.

Indications

Postmenopausal osteoporosis (prevention and treatment)Risk reduction of invasive breast cancer in postmenopausal women at high risk / with osteoporosis

Dosing

Adult: 60 mg PO once daily (with or without food).
Pediatric: Not indicated.
Renal adjustment: Caution in moderate–severe renal impairment (limited data).
Hepatic adjustment: Use with caution (limited data; raised levels in hepatic impairment).
Geriatric: No specific adjustment.
Max dose: 60 mg/day (fixed)

Pharmacokinetics

Onset

BMD/marker effect over months

Peak effect

Bone effect months; Cmax ~6 h (extensive first-pass)

Duration

Once daily

Half-life

~27.7 h

Bioavailability

~2% (extensive first-pass glucuronidation; high absorption)

Protein binding

>95%

Metabolism

Glucuronide conjugation (no CYP); enterohepatic recycling

Excretion

Mainly faecal (metabolites); minimal renal

Contraindications

Active or past venous thromboembolism (DVT/PE/retinal vein thrombosis)
Pregnancy / women of childbearing potential / breastfeeding
Hepatic impairment (caution/avoid)
Hypersensitivity to raloxifene

Side effects

Common

Hot flushesLeg cramps/muscle spasmPeripheral oedemaFlu-like symptomsArthralgia

Serious

Venous thromboembolism (DVT/PE) — incl. boxed warning
Increased risk of fatal stroke in women with/at risk of coronary disease (boxed)
Hepatic dysfunction (rare)