LIPO-HEPIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LIPO-HEPIN (LIPO-HEPIN).
LIPO-HEPIN (unfractionated heparin) binds to antithrombin III, accelerating the inactivation of thrombin (factor IIa) and activated factor X (Xa), thereby inhibiting coagulation.
| Metabolism | Primarily cleared by the reticuloendothelial system and undergoes desulfation and depolymerization; partially metabolized in the liver and excreted in urine. |
| Excretion | Renal: 30-60% as unchanged drug; minor biliary/fecal (<10%). Clearance predominantly via hepatic metabolism (desulfation) and reticuloendothelial system uptake. |
| Half-life | 1-2 hours (therapeutic doses); dose-dependent: 30-60 min at low doses, up to 4-6 hours at high doses. Heparin is eliminated by a saturable zero-order process, leading to nonlinear pharmacokinetics. Clinical context: prolonged half-life in renal impairment or hepatic disease. |
| Protein binding | Highly bound to antithrombin III (70-80%), heparin cofactor II, and other plasma proteins (albumin, lipoproteins). Total protein binding >90%. |
| Volume of Distribution | 0.05-0.1 L/kg; restricted to plasma volume. The small Vd reflects high protein binding and limited extravascular distribution. In pregnancy or obesity, Vd may increase due to expanded plasma volume. |
| Bioavailability | SC: 20-30% (due to first-pass hepatic metabolism and binding to endothelial cells). IV: 100%. Intramuscular is avoided due to risk of hematoma. Inhalation: <10% (experimental). |
| Onset of Action | IV: immediate; SC: 20-60 minutes; inhalation: 15-30 minutes. Onset is enhanced by heparin cofactor II activation and antithrombin III binding. |
| Duration of Action | IV: 2-6 hours (dose-dependent); SC: 8-12 hours. Duration is prolonged in hepatic or renal insufficiency. Low-molecular-weight heparin fractions have longer duration due to reduced clearance. |
| Molecular Weight | 12000 |
Initial IV bolus 80 units/kg, then continuous IV infusion 18 units/kg/hr; or subcutaneous 5000 units every 8-12 hours. Dose adjusted based on aPTT.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 30-60 mL/min: reduce infusion by 20%; CrCl 15-29 mL/min: reduce infusion by 30%; CrCl <15 mL/min: reduce infusion by 50% or consider alternative. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 25%; Child-Pugh C: avoid use due to increased bleeding risk. |
| Pediatric use | IV bolus 75-100 units/kg, then continuous IV infusion: infants 28 units/kg/hr, children 20 units/kg/hr, adolescents 18 units/kg/hr; adjust to target aPTT. |
| Geriatric use | Consider lower initial doses (e.g., 60 units/kg IV bolus, 15 units/kg/hr infusion) due to increased bleeding risk; monitor renal function and aPTT closely. |
| 1st trimester | Heparin does not cross the placenta; considered safe in pregnancy. Risk of hemorrhage if used near delivery. |
| 2nd trimester | Safe for use; no known teratogenic effects. Monitor for bleeding. |
| 3rd trimester | Safe but avoid near term due to risk of maternal hemorrhage and epidural hematoma during delivery. |
Clinical note
Comprehensive clinical and safety monograph for LIPO-HEPIN (LIPO-HEPIN).
| Placental transfer | Does not cross placenta due to high molecular weight and negative charge. |
| Breastfeeding | Heparin is not excreted into breast milk due to high molecular weight; considered compatible with breastfeeding. |
| Lactation Rating |
■ FDA Black Box Warning
Heparin can cause heparin-induced thrombocytopenia (HIT), a serious antibody-mediated reaction leading to irreversible thrombosis. Monitor platelet counts closely.
| Serious Effects |
Active major bleedingHistory of heparin-induced thrombocytopeniaSevere uncontrolled hypertensionKnown hypersensitivity to heparinEpidural or spinal anesthesia in progress
| Precautions | Risk of bleeding, especially in patients with renal impairment or concomitant anticoagulants, Heparin-induced thrombocytopenia (HIT) and heparin-induced thrombocytopenia with thrombosis (HITT), Spinal/epidural hematomas in patients receiving neuraxial anesthesia or spinal puncture, Hyperkalemia due to aldosterone suppression |
| Food/Dietary | No known food interactions. LIPO-HEPIN is administered parenterally and does not have dietary restrictions. However, avoid excessive intake of vitamin K-rich foods (e.g., leafy greens, broccoli, liver) as high vitamin K levels may theoretically antagonize heparin's effect if transitioning to warfarin, but heparin's action is independent of vitamin K. No specific food contraindications. |
Loading safety data…
| L1 (Safe) |
| Teratogenic Risk | Heparin does not cross the placenta. No evidence of teratogenicity in first trimester; risk of fetal hemorrhage and maternal osteopenia with prolonged use in second/third trimester. |
| Fetal Monitoring | Monitor activated partial thromboplastin time (aPTT) every 6 hours during initial therapy and daily once stable. Check complete blood count (CBC) including platelets every 2-3 days for heparin-induced thrombocytopenia. Assess for signs of bleeding or thrombosis. |
| Fertility Effects | No direct effects on fertility reported. Use in assisted reproductive technology for thrombophilia is common without impact on conception rates. |
| Clinical Pearls | LIPO-HEPIN (heparin sodium) is an injectable anticoagulant. For weight-based dosing, use actual body weight; in obese patients, consider using ideal body weight to avoid overdosing. Start with an IV bolus of 80 units/kg followed by continuous infusion at 18 units/kg/hr. Monitor aPTT 6 hours after initiation and adjust per nomogram. Use with caution in renal impairment (CrCl <30 mL/min) due to reduced clearance. Protamine sulfate reverses effect, but excessive protamine can paradoxically increase bleeding. Heparin-induced thrombocytopenia (HIT) type II is an immune-mediated reaction typically occurring 5-14 days after start; check platelet count regularly. LIPO-HEPIN is not a low molecular weight heparin. |
| Patient Advice | This medication is given as an injection into a vein or under the skin. Do not rub the injection site. · Avoid taking aspirin, ibuprofen, naproxen, or other NSAIDs unless prescribed, as they increase bleeding risk. · Report any unusual bleeding, bruising, black or tarry stools, blood in urine, or coughing up blood. · Use a soft toothbrush and electric razor to avoid cuts and bleeding. · Inform all healthcare providers that you are taking this anticoagulant. · You may need frequent blood tests (aPTT) to monitor the medication's effect. · Do not stop or change the dose without consulting your healthcare provider. · If you have signs of allergic reaction (rash, hives, difficulty breathing), seek medical help immediately. · Carry medical identification stating you are taking heparin. |