CALCIPARINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CALCIPARINE (CALCIPARINE).
Unfractionated heparin (UFH) potentiates antithrombin III (ATIII) activity, leading to inhibition of factor Xa and thrombin (factor IIa). It also binds to heparin cofactor II, inhibits platelet aggregation, and increases vascular permeability.
| Metabolism | Hepatic and reticuloendothelial system metabolism via desulfation and depolymerization; partially metabolized by heparinase. Clearance is dose-dependent and involves both saturable (cellular) and non-saturable (renal) mechanisms. |
| Excretion | Primarily renal, with 40-60% of the dose excreted unchanged in urine. Minor biliary/fecal elimination (<10%). |
| Half-life | Terminal elimination half-life is approximately 1.5 hours (subcutaneous) after a 5000 IU dose. With therapeutic doses (e.g., 15,000 IU/24h), half-life may prolong to 2-3 hours. Clinical context: Half-life is dose-dependent and increases with heparin clearance saturation. |
| Protein binding | Highly bound to antithrombin III (ATIII) and other proteins; essentially 100% bound to ATIII when active, but non-specific protein binding is low (<10% to albumin). |
| Volume of Distribution | Vd approximately 0.06-0.1 L/kg (6-10 L in adults), indicating distribution primarily within the plasma volume. |
| Bioavailability | Subcutaneous: Approximately 20-30% after 5000 IU; bioavailability is dose-dependent and inversely related to dose (lower at higher doses due to limited absorption). |
| Onset of Action | Subcutaneous: Anticoagulant effect (APTT prolongation) begins within 20-30 minutes. Intravenous: Immediate (APTT prolonged within minutes of bolus). |
| Duration of Action | Subcutaneous: Anticoagulant effect lasts for approximately 8-12 hours after a single 5000 IU dose. Clinical note: Duration is dose-dependent and may be prolonged with higher doses or in renal impairment. |
5000 IU subcutaneously twice daily for prophylaxis; 5000 IU intravenous bolus followed by 800-1000 IU/hour continuous intravenous infusion for treatment.
| Dosage form | INJECTABLE |
| Renal impairment | GFR 30-50 mL/min: reduce dose by 25%; GFR 15-29 mL/min: reduce dose by 50%; GFR <15 mL/min: avoid use or monitor anti-Xa levels closely. |
| Liver impairment | No specific Child-Pugh based guidelines; use with caution in severe hepatic impairment due to increased bleeding risk. |
| Pediatric use | Weight-based: 50 IU/kg subcutaneously twice daily for prophylaxis; for treatment, 75 IU/kg intravenous bolus followed by 20 IU/kg/hour continuous infusion, adjusted to target anti-Xa 0.3-0.7 IU/mL. |
| Geriatric use | Consider lower initial doses due to age-related renal impairment; monitor anti-Xa levels and renal function frequently. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CALCIPARINE (CALCIPARINE).
| Breastfeeding | Dalteparin is not expected to be excreted in breast milk due to high molecular weight and protein binding. M/P ratio not established. Considered compatible with breastfeeding. |
| Teratogenic Risk | Calcifarine (dalteparin) is a low molecular weight heparin. It does not cross the placenta. No evidence of teratogenicity in first trimester. Risk of fetal bleeding and placental complications in second/third trimester if maternal coagulation is severely altered; use is generally considered safe when indicated. |
■ FDA Black Box Warning
Higher risk of spinal/epidural hematomas in patients receiving neuraxial anesthesia or spinal puncture, especially with concomitant use of antiplatelet agents or other anticoagulants, leading to long-term or permanent paralysis. Monitor for signs of neurological impairment.
| Serious Effects |
["Active major bleeding","Hypersensitivity to heparin or pork products","History of HIT or heparin-associated thrombocytopenia","Severe thrombocytopenia","Inability to perform adequate coagulation monitoring","Suspected intracranial hemorrhage","Uncontrolled severe hypertension","Retroperitoneal bleeding","Spinal puncture or epidural anesthesia (relative; see black box warning)"]
| Precautions | ["Hemorrhage: major bleeding risk; monitor aPTT, platelet counts, and signs of bleeding","Heparin-induced thrombocytopenia (HIT): monitor platelets; discontinue if HIT suspected","Hypersensitivity reactions","Osteoporosis with long-term use ( > 6 months)","Hyperkalemia due to aldosterone suppression","Use with caution in renal impairment, hepatic disease, and elderly"] |
| Food/Dietary |
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| Fetal Monitoring |
| Monitor platelet count, anti-Xa levels if needed, signs of bleeding, and fetal growth and well-being via ultrasound if used long-term. Assess for heparin-induced thrombocytopenia (HIT) with platelet counts. |
| Fertility Effects | No known adverse effects on fertility. Used in management of recurrent pregnancy loss associated with thrombophilia. |
| No significant food interactions. Avoid excessive alcohol consumption due to increased bleeding risk. |
| Clinical Pearls | CALCIPARINE (unfractionated heparin) is used for anticoagulation. Monitor aPTT to maintain 1.5-2.5 times control. Protamine sulfate reverses effect. Avoid in heparin-induced thrombocytopenia (HIT). Check platelet counts regularly. |
| Patient Advice | Report any unusual bleeding or bruising immediately. · Avoid aspirin and NSAIDs unless prescribed by your doctor. · Use a soft toothbrush and electric razor to prevent injury. · Inform all healthcare providers that you are taking this medication. · Do not stop taking this medication suddenly. |