LIPO-HEPIN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for LIPO-HEPIN (LIPO-HEPIN).

How it works

LIPO-HEPIN (unfractionated heparin) binds to antithrombin III, accelerating the inactivation of thrombin (factor IIa) and activated factor X (Xa), thereby inhibiting coagulation.

What the body does with it

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.

Classification & Brands

Dosing & administration

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.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for LIPO-HEPIN (LIPO-HEPIN).

Breastfeeding	Heparin is not excreted into breast milk due to high molecular weight. Considered compatible with breastfeeding; M/P ratio not applicable (no transfer).
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

Warnings & precautions

■ FDA Black Box Warning

Heparin can cause heparin-induced thrombocytopenia (HIT), a serious antibody-mediated reaction leading to irreversible thrombosis. Monitor platelet counts closely.

Side Effect Profile

Serious Effects

Absolute Contraindications

["History of heparin-induced thrombocytopenia (HIT)","Active major bleeding or high bleeding risk (e.g., hemophilia, recent surgery)","Severe thrombocytopenia","Uncontrolled severe hypertension","Hypersensitivity to heparin or pork products"]

Clinical Precautions

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"]

Clinical Tips & Counseling

Drug interactions

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LIPO-HEPIN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for LIPO-HEPIN (LIPO-HEPIN).

How it works

LIPO-HEPIN (unfractionated heparin) binds to antithrombin III, accelerating the inactivation of thrombin (factor IIa) and activated factor X (Xa), thereby inhibiting coagulation.

What the body does with it

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.

Classification & Brands

Dosing & administration

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.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for LIPO-HEPIN (LIPO-HEPIN).

Breastfeeding	Heparin is not excreted into breast milk due to high molecular weight. Considered compatible with breastfeeding; M/P ratio not applicable (no transfer).
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

Warnings & precautions

■ FDA Black Box Warning

Heparin can cause heparin-induced thrombocytopenia (HIT), a serious antibody-mediated reaction leading to irreversible thrombosis. Monitor platelet counts closely.