Schedule H

Intravenous (IV)

• IV infusion: 5 mg/100 mL premixed bag

• IV solution: 0.25 mg/mL concentrate (50 mL bolus vial)

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

⮞ Acute Coronary Syndromes (NSTE-ACS) including Unstable Angina and NSTEMI undergoing Percutaneous Coronary Intervention (PCI)

Dosing Component Recommendation

Starting dose (Bolus) 25 mcg/kg IV over 3 minutes

Titration Not applicable — single bolus followed by fixed infusion

Usual maintenance dose 0.15 mcg/kg/min continuous IV infusion

Maximum dose 0.15 mcg/kg/min for maximum 18 hours total infusion duration

Clinical Notes:

• Administer bolus immediately before PCI

• Continue infusion for minimum 12 hours and maximum 18 hours post-PCI

• Co-administer with aspirin (300–325 mg loading) and unfractionated heparin unless contraindicated

• Adjust maintenance infusion for renal impairment (see Renal Adjustment)

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

Not established in Indian practice.

PAEDIATRIC DOSING (Specialist Only)

Primary Indications (Approved / Standard in India)

Not applicable — Tirofiban is not approved for paediatric use in India.

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

Not established.

Safety Statement:

• Safety and efficacy not established for patients <18 years

• Use only in research settings or specialised tertiary care centres under approved study protocols

• Not recommended for any paediatric indication outside specialist supervision

CrCl ≥60 mL/min No adjustment — use standard maintenance dose 0.15 mcg/kg/min

CrCl 30–59 mL/min Reduce maintenance infusion to 0.1 mcg/kg/min

CrCl <30 mL/min Use with extreme caution; consider avoiding

Dialysis-dependent Avoid use; if essential, specialist supervision with close monitoring

Notes:

• Bolus dose remains unchanged in renal impairment

• Monitor platelet count and bleeding risk with increased vigilance

• Drug is partly cleared renally; accumulation increases bleeding risk

• Active internal bleeding or known bleeding diathesis

• History of haemorrhagic stroke or intracranial haemorrhage

• Ischaemic stroke within preceding 30 days

• Major surgery, severe trauma, or organ biopsy within 30 days

• Severe uncontrolled hypertension (systolic >180 mmHg or diastolic >110 mmHg)

• Platelet count <100,000/mm³ (thrombocytopenia)

• Known intracranial neoplasm, arteriovenous malformation, or aneurysm

• Hypersensitivity to tirofiban or any excipient in the formulation

• Age >65 years — inherently higher bleeding risk

• Body weight <60 kg — monitor carefully

• Recent lumbar puncture, epidural catheter, or spinal procedure within 7 days

• Recent ophthalmic surgery

• Concurrent use of anticoagulants or thrombolytics

• Suspected aortic dissection or pericarditis

• Diabetic retinopathy with active bleeding risk

• Uncontrolled hypertension (lower than absolute contraindication threshold)

• Poor vascular access sites or multiple failed puncture attempts

Parameter Recommendation

Risk category Caution advised — limited human safety data

Preferred alternatives Unfractionated heparin; low-dose aspirin (depending on indication and trimester)

When may be used Only if maternal benefit clearly outweighs fetal risk; multidisciplinary input from cardiology and obstetrics essential

What to monitor Maternal bleeding (vaginal, puncture sites); fetal heart rate; signs of placental compromise

Parameter Recommendation

Compatibility Unknown — no human lactation data available

Expected drug levels in milk Likely minimal due to IV-only use, short half-life (~2 hours), and large molecular weight

Preferred alternative Avoid breastfeeding during infusion and for 12–24 hours post-infusion if possible

What to monitor in infant Signs of bleeding (bruising, petechiae), poor feeding, unusual irritability (although significant exposure unlikely)

• Starting dose: Standard bolus (25 mcg/kg) acceptable; however, use renal-adjusted maintenance dose if eGFR <60 mL/min

• Titration: Not applicable

• Extra risks: Increased baseline bleeding risk; higher incidence of renal impairment; frailty and poor vascular access increase complications

• Recommendations:

• Avoid in frail elderly with multiple comorbidities unless high-risk NSTE-ACS with planned PCI

• Intensify monitoring for bleeding at puncture sites, gastrointestinal tract, and retroperitoneum

• Minimise concurrent use of other antiplatelet agents and anticoagulants where clinically feasible

Interacting Drug(s) Effect / Mechanism Clinical Action

Thrombolytics (alteplase, tenecteplase, streptokinase) Markedly increased bleeding risk Avoid concurrent use

Oral anticoagulants (warfarin, acenocoumarol) Additive bleeding risk Avoid concurrent use during infusion; restart oral anticoagulant only after adequate haemostasis

Direct oral anticoagulants (rivaroxaban, apixaban, dabigatran) Increased bleeding risk Avoid concurrent use; if transitioning, ensure appropriate washout period

Unfractionated heparin / LMWH (in high doses beyond standard PCI anticoagulation) Synergistic bleeding Use recommended PCI-level heparin dosing; avoid excessive anticoagulation

Interacting Drug(s) Effect / Mechanism Clinical Action

Aspirin Synergistic antiplatelet effect Standard dual use in ACS/PCI; monitor for mucosal and puncture-site bleeding

P2Y12 inhibitors (clopidogrel, prasugrel, ticagrelor) Additive platelet inhibition Acceptable in ACS/PCI settings; intensify bleeding surveillance

NSAIDs (ibuprofen, diclofenac, naproxen) Increased gastrointestinal and mucosal bleeding risk Avoid unless essential; prefer paracetamol for analgesia

Other GP IIb/IIIa inhibitors (eptifibatide, abciximab) Redundant mechanism; no additional benefit Avoid combination — do not use duplicate agents

SSRIs (fluoxetine, sertraline) Impaired platelet aggregation Use with caution; monitor for bleeding

• Minor bleeding (puncture sites, mucosal surfaces, gingival)

• Thrombocytopenia (mild, usually reversible)

• Nausea

• Headache

• Transient hypotension during infusion

• Fever

• Injection site reactions

Adverse Effect Clinical Notes

Major bleeding Gastrointestinal, retroperitoneal, intracranial — may require transfusion, surgical intervention, or immediate drug discontinuation

Severe thrombocytopenia Can occur within 1–6 hours of initiation; monitor platelet count; discontinue if <90,000/mm³

Haemorrhagic stroke Discontinue immediately if neurological deterioration; obtain urgent imaging

Anaphylaxis / severe allergic reaction Rare; requires immediate supportive care and epinephrine

Timing Parameter

Baseline Complete blood count (including platelet count), serum creatinine, coagulation profile (aPTT, PT/INR), haemoglobin/haematocrit

4–6 hours post-initiation Platelet count (to detect acute thrombocytopenia)

During infusion Puncture sites, signs of bleeding (haematuria, melaena, haemoptysis), haemodynamic stability

Daily (if prolonged infusion) Haemoglobin, haematocrit, platelet count, renal function

Throughout PCI ECG monitoring, activated clotting time (if using heparin)

• Aggribloc® (Lupin)

• Tirobloc® (Samarth)

• Tirofivan® (Abbott)

• Aggrastat® (Correvio — imported)

• Tirofast® (Cadila)

0.25 mg/mL concentrate vial (50 mL) ₹1,800–₹4,000

Notes:

• Not included in NLEM 2022; not under NPPA price control

• Availability primarily in cath-lab equipped tertiary care centres

• Government hospital supply variable; mostly private procurement

1. Always reduce maintenance infusion dose in renal impairment — even moderate CKD (CrCl 30–59) requires reduction to 0.1 mcg/kg/min

1. Monitor platelet count at 4–6 hours post-bolus — acute severe thrombocytopenia can occur rapidly and is a reason to discontinue

1. Use only in PCI-capable centres — avoid initiating tirofiban in facilities without cardiac catheterisation capability; bleeding risk without revascularisation benefit

1. Do not combine with thrombolytics — this combination carries unacceptable bleeding risk

1. Reserve for high-risk NSTE-ACS with planned PCI — low-risk patients may be managed with ischaemia-guided strategy without GP IIb/IIIa inhibitors

1. Prefer radial access for PCI when using tirofiban to minimise access-site bleeding complications

tirofiban; acute coronary syndrome; NSTE-ACS; NSTEMI; unstable angina; PCI; glycoprotein IIb/IIIa antagonist; antiplatelet IV; bleeding risk; renal dosing; cath-lab; interventional cardiology; Schedule H

RxIndia v0.4 — 28 May 2025

• CDSCO-approved product information

• Indian Pharmacopoeia

• AIIMS Emergency Drug Protocols

• API Textbook of Medicine, 2022

• ICMR Guidelines for Management of Ischaemic Heart Disease

• Interventional Cardiology Protocols (AIIMS, PGIMER Chandigarh)

• ACC/AHA Guidelines (referenced for mechanistic understanding only; not primary basis for Indian dosing recommendations)