Schedule H

Oral

• Tablets: 60 mg

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

⮞ 1. Prevention and Treatment of Postmenopausal Osteoporosis

Dosing Parameter Recommendation

Starting dose 60 mg once daily orally

Titration Not required

Usual maintenance dose 60 mg once daily

Maximum dose 60 mg once daily

Clinical Notes:

• Administer with or without food

• Ensure adequate daily calcium (1000–1200 mg) and vitamin D (800–1000 IU) supplementation

• Does not alleviate vasomotor symptoms (hot flushes); may actually worsen them

• Continue therapy as long as osteoporosis risk persists and benefits outweigh risks

⮞ 2. Reduction of Risk of Invasive Breast Cancer in Postmenopausal Women with Osteoporosis or at High Risk for Breast Cancer

Dosing Parameter Recommendation

Starting dose 60 mg once daily orally

Titration Not required

Usual maintenance dose 60 mg once daily

Maximum dose 60 mg once daily

Clinical Notes:

• Indicated for risk reduction only; not for treatment of established breast cancer

• Patient selection should involve oncology/gynaecology consultation for risk assessment

• Duration: Long-term; reassess periodically for continued benefit

Secondary Indications – Adults Only (Off-label, if any)

Not established in Indian clinical practice.

PAEDIATRIC DOSING (Specialist Only)

Primary Indications (Approved / Standard in India)

Not applicable.

Secondary Indications – Paediatric Doses (Off-label, if any)

Not applicable.

Safety Statement:

• Raloxifene is contraindicated in children and adolescents (<18 years)

• No paediatric indications exist; safety and efficacy not established

• Not recommended below 18 years of age under any circumstances

Notes:

• Monitor for adverse effects in severe renal impairment

• Drug is highly protein-bound; unlikely to be removed by dialysis

• Active or past history of venous thromboembolic events (deep vein thrombosis, pulmonary embolism, retinal vein thrombosis)

• Pregnancy (confirmed or suspected)

• Premenopausal women

• Breastfeeding

• Severe hepatic impairment (Child-Pugh C)

• Active endometrial cancer or unexplained uterine bleeding

• Known hypersensitivity to raloxifene or any excipients

• Concurrent use with systemic oestrogen therapy

• History of stroke or transient ischaemic attack

• Coronary artery disease or high cardiovascular risk

• Prolonged immobilisation (surgery, prolonged bed rest, long-distance travel) — discontinue at least 72 hours prior and resume only after full mobilisation

• History of oestrogen-induced hypertriglyceridaemia — may exacerbate

• Moderate hepatic impairment

• History of breast cancer (use for osteoporosis requires careful evaluation)

• Unexplained uterine bleeding — investigate before initiating therapy

Parameter Recommendation

Risk category Contraindicated — teratogenic potential demonstrated in animal studies

Preferred alternatives Not applicable (raloxifene indicated only in postmenopausal women)

When may be used Never — ensure pregnancy is excluded before initiation

What to monitor Confirm postmenopausal status or negative pregnancy test before starting

Parameter Recommendation

Compatibility Contraindicated

Preferred alternatives Bisphosphonates (after weaning) for osteoporosis

Expected drug levels in milk Unknown; likely to be excreted

What to monitor in infant Not applicable — drug should not be used during lactation

Parameter Recommendation

Starting dose 60 mg once daily (no dose adjustment for age)

Titration Not required

Extra risks Increased VTE risk, especially with reduced mobility; higher stroke risk in those with cardiovascular risk factors; leg cramps; falls due to musculoskeletal effects

Notes:

• Assess mobility status and thrombotic risk carefully before initiation

• Ensure prophylactic measures during periods of immobilisation

Interacting Drug Effect/Mechanism Clinical Action

Cholestyramine Reduces raloxifene absorption by 60% (interrupts enterohepatic circulation) Avoid concurrent use

Systemic oestrogens Pharmacological antagonism; negates benefit Concurrent use contraindicated

Warfarin Raloxifene may decrease prothrombin time by 10% Monitor INR closely; adjust warfarin dose as needed

Interacting Drug Effect/Mechanism Clinical Action

Levothyroxine Potential reduction in absorption Separate administration by at least 4 hours

Tamoxifen Potential antagonistic SERM effects; unclear clinical benefit Avoid combination

Highly protein-bound drugs (diazepam, diclofenac, ibuprofen) Theoretical displacement from albumin binding sites Clinical significance uncertain; monitor if used in high doses

Ampicillin Reduces peak concentration of raloxifene (not clinically significant in most cases) Monitor; no specific adjustment needed

• Hot flushes (worsening in some patients)

• Leg cramps

• Peripheral oedema

• Flu-like symptoms

• Arthralgia

• Sweating

• Headache

Adverse Effect Clinical Notes

Venous thromboembolism (DVT, PE) Risk highest in first 4 months; discontinue immediately if suspected

Stroke Increased risk in women with cardiovascular risk factors; requires immediate medical attention

Retinal vein thrombosis Rare; discontinue if visual symptoms occur

Severe hypersensitivity reactions Rare; discontinue and provide supportive care

After initiation Monitor for signs of thromboembolism (leg swelling, chest pain, dyspnoea) — especially in first 4 months

Long-term DEXA scan every 1–2 years; periodic assessment of cardiovascular and thrombotic risk; lipid profile annually

• Ralista® (Cipla)

• Bonmax® (Sun Pharma)

• Raloxiheal® (Healing Pharma)

• Ralofen® (Elder)

• Evista® (Eli Lilly — limited availability)

• Ralozest® (Zydus Cadila)

Notes:

• Not currently under NPPA price control (not in NLEM 2022)

• Wide price variation between brands; generic options available

1. Ideal patient profile: Postmenopausal women aged <70 years with osteoporosis or osteopenia and elevated breast cancer risk; not suitable for women with significant vasomotor symptoms

1. VTE prevention: Discontinue raloxifene at least 72 hours before anticipated prolonged immobilisation (elective surgery, long travel) and resume only after full mobilisation

1. Not a hot flush remedy: Raloxifene may worsen vasomotor symptoms in some women; counsel patients accordingly before initiation

1. Calcium and vitamin D are essential: Always co-prescribe adequate supplementation for optimal bone health outcomes

1. Compared to bisphosphonates: Raloxifene offers dual benefit (bone + breast cancer risk reduction) but has lesser antifracture efficacy at hip compared to bisphosphonates; choose based on individual risk profile

1. Lipid effects: Raloxifene favourably affects LDL cholesterol but may raise triglycerides; monitor lipid panel in patients with baseline dyslipidaemia

raloxifene; osteoporosis; postmenopausal; SERM; breast cancer prevention; VTE risk; antiresorptive; bone health; Schedule H

RxIndia v1.0 — 28 May 2025

• CDSCO-approved product information

• National Formulary of India (NFI)

• API Textbook of Medicine, 11th Edition

• Goodman & Gilman's The Pharmacological Basis of Therapeutics

• Indian Menopause Society Guidelines

• AIIMS Geriatric and Endocrinology Prescribing Protocols

• Harrison's Principles of Internal Medicine