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). |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LIQUAEMIN SODIUM (LIQUAEMIN SODIUM).
| Breastfeeding | Heparin is not excreted into breast milk due to high molecular weight and protein binding. Considered compatible with breastfeeding. M/P ratio: Not applicable (no transfer). |
| 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 |
■ 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 |
Hypersensitivity to heparin; uncontrolled bleeding; history of HIT; severe thrombocytopenia; suspected intracranial hemorrhage; inability to perform adequate coagulation monitoring.
| 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. |
Loading safety data…
| 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. |