HEPARIN SODIUM 10,000 UNITS AND DEXTROSE 5% IN PLASTIC CONTAINER
Clinical safety rating: safe
Other drugs that affect hemostasis increase bleeding risk Can cause heparin-induced thrombocytopenia (HIT) and bleeding.
Heparin binds to antithrombin III, accelerating its inhibition of thrombin (factor IIa) and factor Xa, thereby preventing thrombus formation and propagation.
| Metabolism | Heparin is partially metabolized by desulfation via heparin-degrading enzymes (heparinases) in the liver and reticuloendothelial system; a portion is excreted unchanged by the kidneys. |
| Excretion | Primarily renal; metabolism by hepatic and reticuloendothelial system desulfation yields uroheparin, which is excreted in urine. Unchanged heparin is also excreted renally, with elimination proportional to dose and molecular weight. Biliary/fecal excretion is negligible (<5%). |
| Half-life | 30-60 minutes at therapeutic doses, dose-dependent (e.g., 100 U/kg yields t½ ~56 min; 400 U/kg yields ~152 min). At lower doses (e.g., 25 U/kg), t½ is ~30 min. Prolonged in hepatic or renal impairment. |
| Protein binding | Very high; >99% bound primarily to antithrombin III (ATIII) and other plasma proteins (e.g., heparin cofactor II, platelet factor 4, histidine-rich glycoprotein). Binding to ATIII is critical for anticoagulant effect. |
| Volume of Distribution | 0.05-0.07 L/kg (approximately 5-7% of body weight). Reflects limited distribution primarily to plasma volume; does not readily cross placenta or breast milk in significant amounts. |
| Bioavailability | Subcutaneous: 30-50% (dose-dependent; lower absolute bioavailability with higher doses due to binding at injection site). IV: 100%. |
| Onset of Action | IV: immediate (within 1-2 minutes). Subcutaneous: 20-60 minutes (dose-dependent; 20-30 min with 15,000-20,000 U). |
| Duration of Action | IV: 2-6 hours (dose-dependent; lower doses ~2h, higher doses ~6h). Subcutaneous: 12-24 hours (with weight-adjusted dosing; sustained effect). Note: anticoagulant effect lasts longer than measurable heparin levels due to factor Xa inhibition. |
IV: Initial bolus of 5000 units followed by continuous infusion at 1300 units/hour, adjusted based on aPTT. Typical infusion range 1000-2000 units/hour.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment recommended for heparin itself. Monitor aPTT closely in renal impairment due to potential accumulation of antithrombin III levels. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B/C: Consider dose reduction (by 25-50%) and monitor aPTT closely due to decreased synthesis of coagulation factors. |
| Pediatric use | IV: Initial bolus 75-100 units/kg, then continuous infusion 20-25 units/kg/hour adjusted to target aPTT 60-85 seconds. For infants <1 year, may need higher doses. |
| Geriatric use | Consider lower initial bolus (2500-5000 units) and infusion rates (1000 units/hour) due to increased bleeding risk and altered pharmacokinetics. Monitor aPTT and adjust accordingly. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Other drugs that affect hemostasis increase bleeding risk Can cause heparin-induced thrombocytopenia (HIT) and bleeding.
| FDA category | Human |
| Breastfeeding | Heparin is not excreted into breast milk due to high molecular weight; considered compatible with breastfeeding. M/P ratio not applicable. |
| Teratogenic Risk | Heparin does not cross the placenta; no fetal risk established in any trimester. No evidence of teratogenicity. |
■ FDA Black Box Warning
Spinal or epidural hematomas can occur in patients receiving anticoagulants, including heparin, who undergo neuraxial anesthesia or spinal puncture, resulting in long-term or permanent paralysis.
| Common Effects | bleeding |
| Serious Effects |
Known hypersensitivity to heparin or pork products; active major bleeding; history of heparin-induced thrombocytopenia (HIT) or heparin-induced thrombocytopenia with thrombosis (HITT); severe thrombocytopenia; inability to perform appropriate monitoring (e.g., aPTT).
| Precautions | Risk of bleeding; monitor platelets for heparin-induced thrombocytopenia (HIT); risk of osteoporosis with prolonged use; caution in patients with hepatic or renal impairment; hypersensitivity reactions; use with caution in patients with increased bleeding risk. |
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| Fetal Monitoring | Monitor activated partial thromboplastin time (aPTT) to maintain therapeutic range. Assess maternal bleeding, signs of hemorrhage, and platelet count for heparin-induced thrombocytopenia (HIT). Fetal heart rate monitoring per standard obstetric care. |
| Fertility Effects | No known adverse effects on fertility. Heparin does not affect reproductive hormones or gametogenesis. |