Leuprolide Schedule (India)

Schedule H

Leuprolide Routes

Subcutaneous (SC), Intramuscular (IM)

Leuprolide Formulations

Injection (SC): 1 mg/0.2 mL (daily formulation)

Depot Injection (IM): 3.75 mg (1-month), 7.5 mg (1-month), 11.25 mg (3-month), 22.5 mg (3-month), 30 mg (4-month)

Leuprolide Adult indications

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

Advanced Hormone-Sensitive Prostate Cancer

Parameter Recommendation

Starting dose 3.75 mg IM depot once monthly OR 7.5 mg IM depot once monthly

Titration Not applicable

Usual maintenance dose 3.75 mg monthly OR 11.25 mg every 3 months OR 22.5 mg every 3 months

Maximum dose As per approved depot formulation selected

Key Clinical Notes:

Initiate anti-androgen therapy (e.g., bicalutamide 50 mg daily) at least 3 days before first leuprolide injection and continue for 2–4 weeks to prevent tumour flare

Monitor serum testosterone — target castrate levels (<50 ng/dL)

Continue until disease progression or intolerable toxicity

Endometriosis

Parameter Recommendation

Starting dose 3.75 mg IM once monthly

Titration Not applicable

Usual maintenance dose 3.75 mg monthly OR 11.25 mg every 3 months

Maximum dose 11.25 mg every 3 months

Key Clinical Notes:

Maximum treatment duration: 6 months (due to bone loss risk)

Add-back therapy recommended: low-dose norethindrone (5 mg daily) or combined estrogen-progestin to reduce hypoestrogenic symptoms and bone loss

May repeat course after reassessment if symptoms recur

Uterine Leiomyomas (Fibroids) — Preoperative Size Reduction

Parameter Recommendation

Starting dose 3.75 mg IM once monthly

Titration Not applicable

Usual maintenance dose 3.75 mg monthly

Maximum dose 3.75 mg monthly for up to 6 months

Key Clinical Notes:

Duration: 3–6 months preoperatively

Reduces uterine and fibroid volume by 30–50%

Corrects preoperative anaemia

Consider add-back therapy if used beyond 3 months

Hormone Receptor-Positive Breast Cancer (Premenopausal Women — Ovarian Suppression)

Parameter Recommendation

Starting dose 3.75 mg IM once monthly

Titration Not applicable

Usual maintenance dose 3.75 mg monthly OR 11.25 mg every 3 months

Maximum dose As per oncology protocol

Key Clinical Notes:

Used in combination with tamoxifen or aromatase inhibitor

Duration: 2–5 years as part of adjuvant endocrine therapy

Specialist only (Medical Oncology)

Confirm ovarian suppression with serum estradiol levels

Central Precocious Puberty (CPP)

See Paediatric Dosing Section

Secondary Indications – Adults Only (Off-label)

Assisted Reproductive Technology (ART) — Pituitary Downregulation — OFF-LABEL

Starting dose: 0.5–1 mg SC daily

Titration: Not applicable

Usual maintenance dose: 0.5–1 mg SC daily

Maximum dose: 1 mg SC daily

Duration: Begin in mid-luteal phase of preceding cycle; continue until adequate downregulation confirmed (typically 10–14 days)

Specialist only (Reproductive Medicine/IVF centres)

Evidence: Indian Fertility Society protocols; established IVF practice

Gender-Affirming Hormone Therapy (Male-to-Female) — OFF-LABEL

Starting dose: 3.75 mg IM monthly

Titration: Not applicable

Usual maintenance dose: 3.75 mg monthly OR 11.25 mg every 3 months

Maximum dose: As per specialist protocol

Duration: Long-term; individualized

Specialist only (Endocrinology with expertise in gender medicine)

Evidence: International guidelines; limited formal Indian guidance — use under specialist supervision only

Leuprolide Paediatric indications

PAEDIATRIC DOSING (Specialist Only)

Primary Indications (Approved / Standard in India)

Central Precocious Puberty (CPP)

Minimum age: ≥2 years

Specialist only (Paediatric Endocrinology)

Weight-Based Dosing (Monthly IM Depot):

Body Weight Dose (IM Monthly)

<25 kg 7.5 mg once monthly

25–37.5 kg 11.25 mg once monthly

37.5 kg 15 mg once monthly

Alternative 3-Month Depot:

11.25 mg IM every 3 months (for appropriate weight categories)

Parameter Recommendation

Starting dose As per weight-based table above

Titration Adjust based on clinical and biochemical response

Usual maintenance dose Same as starting dose

Maximum dose 15 mg monthly

Key Clinical Notes:

Confirm diagnosis with GnRH stimulation test before initiating therapy

Goal: Suppression of pubertal progression and deceleration of bone age advancement

Discontinue when chronological age appropriate for puberty (typically 11 years for girls, 12 years for boys)

Secondary Indications – Paediatric Doses (Off-label)

Not established in Indian guidelines. Off-label use outside CPP is NOT recommended without Paediatric Endocrinologist supervision.

Safety Monitoring (Paediatric Use):

Serum LH, FSH, and sex steroids (estradiol or testosterone) at baseline, 1–2 months, then every 6 months

Bone age assessment (X-ray left wrist) at baseline and every 6–12 months

Growth velocity monitoring

Pubertal staging (Tanner) at each visit

Height prediction assessment annually

NOT recommended below 2 years of age.

Leuprolide Renal Adjustments

No dosage adjustment required in mild, moderate, or severe renal impairment

Depot formulation is not significantly dialyzable

Haemodialysis/peritoneal dialysis: No supplemental dosing required

Leuprolide Hepatic adjustment

Mild impairment: No dosage adjustment required

Moderate impairment: Use with caution; no specific dose reduction established but monitor for adverse effects

Severe impairment: Limited data available; use with caution under specialist supervision

Leuprolide Contraindications

Known hypersensitivity to leuprolide, other GnRH agonists, or any excipients

Pregnancy (confirmed or suspected)

Undiagnosed abnormal vaginal bleeding

Hormone-independent (castration-resistant) prostate cancer

Women with hormone receptor-negative breast cancer (no benefit expected)

Leuprolide Cautions

Tumour flare phenomenon: Initial rise in testosterone/estrogen may worsen symptoms in first 1–2 weeks (bone pain, urinary obstruction in prostate cancer; bleeding in fibroids) — always provide anti-androgen cover in prostate cancer

Osteoporosis or risk factors for bone loss — baseline BMD assessment recommended for therapy >6 months

Pre-existing cardiovascular disease — monitor for metabolic effects

Diabetes mellitus — may affect glycaemic control

Depression or psychiatric history — monitor for mood changes

Seizure disorders — rare reports of convulsions

Prolonged QT interval — use with caution with QT-prolonging medications

Vertebral metastases with risk of spinal cord compression (prostate cancer) — close monitoring during initiation

Leuprolide Pregnancy

Parameter Recommendation

Risk category Contraindicated (Category X equivalent)

Teratogenic risk Known teratogenicity in animal studies; fetal harm expected

Preferred alternatives Not applicable — drug must be avoided

When may be used Never during confirmed or suspected pregnancy

Monitoring Confirm negative pregnancy test before initiating therapy; ensure reliable contraception during treatment and for at least 1–2 months after discontinuation

Leuprolide Lactation

Parameter Recommendation

Compatibility Not compatible with breastfeeding

Expected drug levels in milk Unknown; potential for hormonal effects on infant

Preferred alternatives Discontinue breastfeeding if leuprolide therapy essential

Infant monitoring Not applicable — avoid use during lactation

Leuprolide Elderly

Starting dose: Same as adult dosing (3.75 mg depot monthly or equivalent)

Titration: Not applicable

Depot formulations preferred for improved adherence

Extra risks:

Increased susceptibility to bone loss — baseline and periodic BMD assessment

Cardiovascular risk — monitor lipid profile, blood glucose, blood pressure

Falls risk due to potential musculoskeletal effects

In prostate cancer: Regular PSA and testosterone monitoring essential

Leuprolide Major drug interactions

Interacting Drug Effect Mechanism Management

QT-prolonging drugs (amiodarone, sotalol, haloperidol, ondansetron, fluoroquinolones) Additive QT prolongation risk Pharmacodynamic interaction Avoid combination if possible; if essential, obtain baseline ECG and monitor QT interval

Leuprolide Moderate drug interactions

Interacting Drug Effect Management

Antidiabetic agents (metformin, sulfonylureas, insulin) Altered glucose tolerance due to hormonal changes Monitor blood glucose more frequently; adjust antidiabetic doses as needed

SSRIs/SNRIs May exacerbate mood disturbances and hot flushes Monitor for worsening depression or mood changes

Corticosteroids Additive risk of bone loss with prolonged use Consider BMD monitoring; ensure calcium and vitamin D supplementation

Tamoxifen Used together therapeutically in breast cancer Monitor for additive hot flushes and bone health; no dose adjustment needed

Leuprolide Common Adverse effects

Hot flushes (50–80%)

Injection site reactions (pain, erythema, induration)

Decreased libido

Erectile dysfunction (males)

Vaginal dryness and dyspareunia (females)

Headache

Fatigue

Mood changes (irritability, emotional lability)

Weight gain

Arthralgia and myalgia

Gynecomastia (males)

Peripheral oedema

Leuprolide Serious Adverse effects

Tumour flare: Worsening of symptoms (bone pain, urinary obstruction, spinal cord compression) in first 1–2 weeks — requires anti-androgen cover in prostate cancer; may require hospitalisation if severe

Pituitary apoplexy: Rare; presents with sudden headache, visual changes, altered mental status — requires immediate neurosurgical evaluation

Osteoporotic fractures: With prolonged therapy (>6 months)

Cardiovascular events: Myocardial infarction, stroke — rare; monitor in high-risk patients

QT prolongation: Rare; obtain baseline ECG in patients with cardiac history

Severe depression/suicidal ideation: Rare; screen for psychiatric history before initiation

Anaphylactic/hypersensitivity reactions: Rare

Interstitial lung disease: Very rare

Leuprolide Monitoring requirements

Baseline:

Serum testosterone (males) or estradiol (females)

PSA (prostate cancer)

LH, FSH (especially in CPP)

Liver function tests

Renal function tests

Bone mineral density (DEXA) if therapy anticipated >6 months

Blood glucose/HbA1c (diabetic patients)

ECG (if cardiac history or QT-prolonging drug use)

Pregnancy test (females of reproductive age)

After Initiation:

Monitor for tumour flare symptoms during first 2–4 weeks (prostate cancer)

Serum testosterone/estradiol at 1 month to confirm suppression

PSA at 3–6 months (prostate cancer)

Clinical assessment for injection site reactions

Long-term (>6 months):

BMD assessment annually

Blood glucose/HbA1c annually

Lipid profile annually

PSA every 3–6 months (prostate cancer)

MRI pituitary if pituitary adenoma history

In CPP: Bone age, growth velocity, and pubertal staging every 6–12 months

Leuprolide Brands in India

Lupride (Sun Pharma)

Lupride Depot (Sun Pharma)

Eligard (Astellas/Tolmar)

Leuprogen (Bharat Serums)

Leupromer (Emcure)

Luprodex (Bharat Serums)

Luperel (Reliance Life Sciences)

Leuprolide Price range (INR)

1 mg SC injection (daily): ₹1,200–₹1,500 per vial

3.75 mg IM depot (1-month): ₹2,500–₹3,500

7.5 mg IM depot (1-month): ₹4,000–₹5,500

11.25 mg IM depot (3-month): ₹6,500–₹9,000

22.5 mg IM depot (3-month): ₹12,000–₹15,000

Included in NLEM for CPP and oncology indications

Available under government oncology programs for prostate and breast cancer

Leuprolide Clinical pearls

Always initiate anti-androgen therapy (bicalutamide or flutamide) before first leuprolide dose in prostate cancer to prevent tumour flare — continue for at least 2–4 weeks

In endometriosis and fibroids, add-back therapy with low-dose norethindrone or estrogen-progestin minimizes bone loss and hypoestrogenic symptoms without reducing efficacy — initiate from the start of treatment

Depot formulations are not interchangeable — ensure correct formulation selected for intended dosing interval (1-month vs 3-month)

Symptoms during first 2 weeks may mimic disease progression due to initial hormone surge — counsel patients appropriately to prevent unnecessary alarm or treatment changes

For any therapy duration exceeding 6 months, baseline and annual BMD assessment is essential — consider bisphosphonates if significant bone loss occurs

In CPP, discontinue treatment when chronological age is appropriate for puberty to allow normal pubertal progression

Leuprolide Tags

leuprolide; GnRH agonist; prostate cancer; endometriosis; uterine fibroids; central precocious puberty; hormonal therapy; depot injection; tumour flare; NLEM India

Leuprolide Version

RxIndia v1.0 — 06 Apr 2025

Leuprolide Reference

CDSCO approved prescribing information

Indian Pharmacopoeia

National List of Essential Medicines (NLEM) India 2022

API Textbook of Medicine

AIIMS Paediatric Endocrinology Protocols

Indian Fertility Society Guidelines (ART protocols)

Tata Memorial Centre Oncology Protocols

Goodman & Gilman's The Pharmacological Basis of Therapeutics

WHO Essential Medicines List (supportive — CPP indication)

RxIndia

The Drug Registry

Leuprolide