Schedule H

Oral

• Tablet: 300 mg (as Tenofovir disoproxil fumarate)

• Fixed-Dose Combinations (FDCs):

• TDF 300 mg + Emtricitabine 200 mg

• TDF 300 mg + Lamivudine 300 mg

• TDF 300 mg + Lamivudine 300 mg + Efavirenz 600 mg

• TDF 300 mg + Lamivudine 300 mg + Dolutegravir 50 mg

• TDF 300 mg + Emtricitabine 200 mg + Efavirenz 600 mg

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

1. HIV-1 Infection (Adults) — As part of combination ART

Parameter Details

Starting dose 300 mg orally once daily

Titration Not required

Usual maintenance dose 300 mg orally once daily

Maximum dose 300 mg per day

Key notes Must be used with at least one other active antiretroviral agent; component of NACO first-line regimen (TDF + Lamivudine + Dolutegravir); administer with or without food

1. Chronic Hepatitis B Virus (HBV) Infection

Parameter Details

Starting dose 300 mg orally once daily

Titration Not required

Usual maintenance dose 300 mg orally once daily

Maximum dose 300 mg per day

Duration Long-term; typically continued indefinitely or until HBsAg seroconversion

Key notes First-line agent per ICMR Hepatitis guidelines; high genetic barrier to resistance; monitor HBV DNA levels for response assessment

Secondary Indications — Adults (Off-label, if any)

HIV Pre-Exposure Prophylaxis (PrEP) — OFF-LABEL

Parameter Details

Indication Prevention of HIV-1 acquisition in high-risk individuals

Dose TDF 300 mg + Emtricitabine 200 mg once daily

Duration Continuous use during period of ongoing risk exposure

Notes Specialist only; limited rollout in India outside research/targeted programmes

Evidence basis International RCTs (iPrEx, Partners PrEP); WHO guidelines supportive; Indian practice limited to high-risk key populations under specialist supervision

PAEDIATRIC DOSING (Specialist Only)

Primary Indications (Approved / Standard in India)

1. HIV-1 Infection (Children ≥2 years and weight ≥17 kg)

Weight-Based Dosing Table (WHO/IAP supported):

Body Weight Dose Frequency

17 to <22 kg 150 mg Once daily

22 to <28 kg 200 mg Once daily

28 to <35 kg 250 mg Once daily

≥35 kg 300 mg Once daily

Parameter Details

Starting dose Per weight band above

Titration Adjust dose as child grows and weight changes

Maximum dose 300 mg once daily

Key notes Always use as part of combination ART; dispersible/scored tablets available in paediatric FDCs; baseline renal function and bone health assessment recommended

1. Chronic Hepatitis B (Children ≥12 years and weight ≥35 kg)

Parameter Details

Starting dose 300 mg orally once daily

Titration Not required

Usual maintenance dose 300 mg once daily

Maximum dose 300 mg per day

Key notes Monitor LFTs and HBV DNA regularly; long-term therapy required

Secondary Indications — Paediatrics (Off-label, if any)

• HBV in children <12 years: Not routinely recommended; specialist consultation mandatory if considered

• HIV in children <2 years or weight <17 kg: Expert dosing protocols required; consider alternative NRTIs (abacavir preferred in this age group per NACO/IAP)

• Use below recommended age/weight thresholds only under specialist paediatric infectious disease supervision with enhanced renal and bone monitoring

Additional Notes:

• Avoid use with eGFR <10 mL/min unless on haemodialysis and no alternatives exist

• In paediatric renal impairment: use with extreme caution; consider alternative agents

• Peritoneal dialysis: Limited data; avoid if possible

Special Note for HBV: Discontinuation of tenofovir in HBV-infected patients may cause severe acute exacerbation of hepatitis. If discontinuation necessary, monitor LFTs closely for several months post-cessation; taper under specialist supervision.

• Hypersensitivity to tenofovir disoproxil fumarate or any excipient

• Concurrent administration with adefovir dipivoxil (overlapping nephrotoxicity and no added benefit)

• Severe renal impairment (eGFR <10 mL/min) without dialysis access

• Pre-existing renal impairment or proteinuria — requires baseline assessment and closer monitoring

• Concurrent use of nephrotoxic agents (aminoglycosides, amphotericin B, high-dose NSAIDs, foscarnet)

• Risk of decreased bone mineral density — particularly concerning in growing children, adolescents, postmenopausal women, and elderly

• Prior history of lactic acidosis or hepatic steatosis with nucleoside/nucleotide analogues

• HIV/HBV co-infection — discontinuation may cause HBV flare

• Patients with osteoporosis or history of pathological fractures

Aspect Details

Overall safety Considered safe; extensive human data available

Risk category Preferred NRTI backbone in pregnancy per NACO guidelines

When used Recommended as first-line component of ART in HIV-positive pregnant women; also used for HBV in pregnancy

Preferred regimen TDF + Lamivudine + Dolutegravir (NACO first-line for pregnant women initiating ART)

What to monitor Maternal renal function (serum creatinine, eGFR); serum phosphate levels; routine antenatal monitoring

Aspect Details

Compatibility Compatible with breastfeeding

Drug levels in milk Low (minimal oral bioavailability in infant)

Preferred alternatives Not required; tenofovir is approved component of PMTCT regimens

Infant monitoring Monitor feeding patterns, growth, and development; no specific drug-level monitoring needed

Note: Per NACO and WHO, breastfeeding is supported for HIV-positive mothers on suppressive ART with infant prophylaxis.

Aspect Details

Starting dose Standard 300 mg once daily, after confirming adequate renal function

Titration Not applicable; adjust dosing interval based on eGFR

Extra risks Age-related decline in renal function; increased susceptibility to nephrotoxicity; higher risk of bone demineralisation and fractures; potential for lactic acidosis

Monitoring Baseline and periodic renal function (every 3 months); serum phosphate; consider DEXA scan if prolonged use anticipated

Drug Interaction/Mechanism Recommendation

Adefovir dipivoxil Overlapping nephrotoxicity; no therapeutic advantage Contraindicated — avoid combination

Didanosine Tenofovir increases didanosine levels significantly; risk of pancreatitis, lactic acidosis, peripheral neuropathy Avoid combination; if unavoidable, reduce didanosine dose and monitor closely

High-dose or multiple NSAIDs Additive nephrotoxicity Avoid concurrent chronic use; if essential, monitor renal function frequently

Aminoglycosides (gentamicin, amikacin) Additive nephrotoxicity Avoid if possible; if required, close renal monitoring mandatory

Drug/Class Interaction Recommendation

Ritonavir-boosted protease inhibitors (lopinavir/r, atazanavir/r) Increased tenofovir plasma levels Monitor renal function more frequently

Ledipasvir-containing HCV regimens Increased tenofovir levels, especially with boosted PI Enhanced renal monitoring; consider alternative HCV regimen if renal concerns

Antacids (aluminium, magnesium, calcium-based) May reduce tenofovir absorption Administer tenofovir at least 2 hours before or after antacids

Rifampicin No significant interaction No dose adjustment required; safe to co-administer

Amphotericin B Additive nephrotoxicity Use with caution; monitor renal function

Acyclovir, valacyclovir Competition for tubular secretion Monitor renal function when used concurrently

• Nausea

• Diarrhoea

• Vomiting

• Flatulence

• Headache

• Dizziness

• Fatigue and asthenia

• Mild elevation in serum creatinine

• Rash

• Renal tubular dysfunction (Fanconi syndrome) — presents with hypophosphataemia, glycosuria, proteinuria, hypokalaemia; may require discontinuation

• Acute kidney injury — monitor creatinine; discontinue if progressive decline

• Osteomalacia and decreased bone mineral density — particularly concerning in paediatric and elderly populations; may present with bone pain, fractures

• Lactic acidosis with hepatic steatosis — rare but potentially fatal; discontinue immediately if suspected

• Severe acute exacerbation of hepatitis B — may occur upon discontinuation in HBV-infected patients; requires close post-discontinuation monitoring

Baseline (Before Initiation):

• Serum creatinine and eGFR calculation

• Serum phosphate

• Urinalysis (proteinuria, glycosuria)

• HBV serology (HBsAg, anti-HBc) — even in HIV-positive patients

• HIV viral load and CD4 count (if HIV indication)

• HBV DNA (if HBV indication)

• LFTs

• DEXA scan consideration in high-risk patients (children, postmenopausal women, elderly)

After Initiation/Dose Change:

• Serum creatinine and eGFR at 2–4 weeks, then at 3 months

Long-Term Monitoring:

• Renal function (creatinine, eGFR, phosphate) every 3–6 months

• Urinalysis annually or if symptoms develop

• HBV DNA (every 6–12 months in HBV infection)

• HIV viral load and CD4 per NACO protocol

• LFTs every 6 months

• Bone mineral density assessment if prolonged use in high-risk groups

Single-Drug Formulations:

• Tenvir (Cipla)

• Tenofo (Hetero)

• Tenohep (Zydus)

• Tenof (Emcure)

Common Fixed-Dose Combinations:

NACO Supply: Generic FDCs available free at government ART centres

TDF 300 mg tablet (generic/NACO) Free at government ART centres

• NLEM Status: Included in NLEM (price controlled)

• Government supply: Free under NACO for HIV; subsidised HBV programmes in select states

1. NACO first-line backbone: TDF + Lamivudine + Dolutegravir is the preferred first-line ART regimen in India for treatment-naïve adults and adolescents, including pregnant women

1. Renal vigilance: Always calculate eGFR before initiation; even mild pre-existing renal impairment significantly increases nephrotoxicity risk. Avoid concurrent chronic NSAID use

1. HBV flare risk: Never discontinue tenofovir abruptly in HBV-infected patients (including HIV/HBV co-infected); monitor LFTs for at least 6 months post-discontinuation

1. Bone health in children: Consider baseline bone assessment in paediatric patients on long-term therapy; ensure adequate calcium and vitamin D supplementation

1. FDC verification: When switching brands, verify exact FDC components and strengths — multiple combinations exist with different partner drugs

1. HBV vs HIV monotherapy: Tenofovir monotherapy is acceptable for HBV but never for HIV (rapid resistance development); always confirm HIV status before starting monotherapy for HBV

Tenofovir; TDF; HIV; Hepatitis B; HBV; antiretroviral; NRTI; NtRTI; renal-adjustment; nephrotoxicity; bone-toxicity; pregnancy-safe; NACO; NLEM India; PMTCT

RxIndia v1.0 — 15 May 2025

• CDSCO approved product information

• Indian Pharmacopoeia (IP)

• National Formulary of India (NFI)

• NLEM 2022

• NACO National ART Guidelines 2021

• ICMR-NIE Guidelines on Management of Hepatitis B 2021

• AIIMS Paediatric HIV Treatment Protocols

• IAP Guidelines for Paediatric HIV Management

• WHO Consolidated Guidelines on HIV Prevention, Testing, Treatment, and Care (supportive)

• API Textbook of Medicine, 11th Edition

• Goodman & Gilman's The Pharmacological Basis of Therapeutics