LIQUAEMIN SODIUM
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LIQUAEMIN SODIUM (LIQUAEMIN SODIUM).
Heparin binds to antithrombin III, accelerating the inactivation of thrombin and factor Xa, thereby inhibiting coagulation cascade.
| Metabolism | Primarily metabolized by the reticuloendothelial system; partially desulfated and depolymerized. Renal excretion of metabolites. |
| Excretion | Primarily renal (heparin is metabolized and excreted as uroheparin and other metabolites; up to 50% of administered dose appears in urine as unchanged heparin, but clearance is dose-dependent and nonlinear). |
| Half-life | Mean 1.5 hours (range 1-2 hours) after IV administration; increases with dose (e.g., 25,000 U IV: ~2.5 h). Clinical context: nonlinear pharmacokinetics; half-life prolonged in hepatic or renal impairment. |
| Protein binding | Very high; primarily binds to antithrombin III, fibrinogen, and other plasma proteins; fraction bound >90%. |
| Volume of Distribution | 0.06-0.1 L/kg (confined to plasma volume; does not distribute widely due to high protein binding and polarity). |
| Bioavailability | SC: variable, ~30% (due to first-pass metabolism and binding; highly dependent on injection site and depth). |
| Onset of Action | IV: immediate; SC: 20-30 minutes (with therapeutic effect at 1-2 hours). |
| Duration of Action | IV: dose-dependent; single dose ~2-6 hours; SC: ~8-12 hours (clinical effect lasts 8-12 hours after a single SC dose). |
| Molecular Weight | 15000 |
Initial adult dose: 5,000 units IV bolus, followed by continuous IV infusion at 1,000–2,000 units/hour; or 10,000–20,000 units subcutaneously every 12 hours. Dose adjusted based on aPTT.
| Dosage form | INJECTABLE |
| Renal impairment | GFR <30 mL/min: reduce dose by 25–50% and monitor aPTT closely. GFR 30–60 mL/min: consider dose reduction of 25%. Hemodialysis: avoid or use with extreme caution. |
| Liver impairment | Child-Pugh class B or C: dose reduction of 25–50% recommended due to increased risk of bleeding; monitor aPTT and anti-Xa levels. |
| Pediatric use | Neonates: 75 units/kg IV bolus, then 20 units/kg/hour. Infants and children: initial bolus 50–100 units/kg, maintenance 15–25 units/kg/hour continuous infusion; titrate to aPTT 1.5–2.5 times control. |
| Geriatric use | Elderly patients: initial dose reduction of 25–50% due to decreased renal function and higher bleeding risk; monitor aPTT and anti-Xa levels frequently. |
| 1st trimester | Avoid due to risk of hemorrhage; may cause maternal bleeding and pregnancy loss. |
| 2nd trimester | Use with caution; increased risk of bleeding and heparin-induced thrombocytopenia. |
| 3rd trimester | Use with caution; risk of maternal hemorrhage and potential for neonatal bleeding (e.g., retroplacental hematoma). |
Clinical note
Comprehensive clinical and safety monograph for LIQUAEMIN SODIUM (LIQUAEMIN SODIUM).
| Placental transfer | Heparin does not cross the placenta due to high molecular weight and negative charge. |
| Breastfeeding | Heparin does not cross into breast milk due to high molecular weight; considered compatible with breastfeeding. Monitor infant for signs of bleeding. |
| Lactation Rating |
■ FDA Black Box Warning
Heparin is not intended for intramuscular use. Risk of spinal/epidural hematoma in patients receiving neuraxial anesthesia or spinal puncture, especially with concomitant use of agents affecting hemostasis.
| Serious Effects |
History of heparin-induced thrombocytopeniaActive major bleedingKnown hypersensitivity to heparinSevere thrombocytopeniaWhen coagulation tests cannot be performed at appropriate intervals
| Precautions | Risk of hemorrhage; heparin-induced thrombocytopenia (HIT); hypersensitivity reactions; hyperkalemia due to aldosterone suppression; osteoporosis with prolonged use; caution in renal/hepatic impairment, obesity, elderly; monitor platelet counts and aPTT. |
| Food/Dietary | No significant food interactions are known. However, foods rich in vitamin K (e.g., leafy greens) may theoretically affect coagulation, but heparin's action is not vitamin K-dependent. Advise consistent intake of vitamin K-rich foods if also on warfarin. No specific dietary restrictions required. |
Loading safety data…
| L1 (Safe) |
| Teratogenic Risk | FDA Pregnancy Category B. Heparin does not cross the placenta and is not associated with teratogenicity. First trimester: No increased risk of major birth defects. Second/third trimester: Risk of maternal bleeding complications, fetal hemorrhage, and preterm labor. Use only if clearly needed. |
| Fetal Monitoring | Monitor maternal CBC (platelets), anti-Xa levels (if using unfractionated heparin), aPTT, signs of bleeding, and fetal growth (ultrasound). During labor, monitor for fetal distress and maternal hemorrhage risk. |
| Fertility Effects | No direct adverse effects on fertility reported. Heparin does not affect ovarian function or spermatogenesis. |
| Clinical Pearls | Heparin (LIQUAEMIN SODIUM) is a parenteral anticoagulant. Monitor aPTT regularly; therapeutic range typically 1.5-2.5 times control. Use cautiously in renal impairment; avoid in severe thrombocytopenia (HIT). Protamine sulfate reverses effect. For subcutaneous administration, use abdominal site to minimize hematoma. Do not use in patients with active bleeding or history of HIT. Check platelet counts frequently. |
| Patient Advice | Report any unusual bleeding, bruising, or dark stools immediately. · Avoid activities that increase injury risk; use electric razor and soft toothbrush. · Take exactly as prescribed; do not skip doses. If a dose is missed, contact your healthcare provider. · Tell all healthcare providers you are taking this medication, including dentists and surgeons. · Do not take over-the-counter medications, supplements, or herbal products without discussing with your doctor. · Store heparin at room temperature, away from light and moisture. |