| Aprotinin Pharmacology |
| Aprotinin |
| About Aprotinin |
| Bovine pancreatic trypsin inhibitor(natural proteinase inhibitor), Hemostatic. |
| Mechanism of Action of Aprotinin |
| Aprotinin is a polypeptide obtained from bovine lung tissues with polyvalent protease inhibitory activity. It inhibits trypsin, chymotrypsin, kallikrein, and plasmin. It inhibits fibrinolysis and turnover of coagulation factors and prevents bleeding. It inhibits serine proteases and preserves platelet function and decrease bleeding time. It inhibits contact face activation and preserves adhesive glycoprotein in the platelet membrane. It increases resistance to damage and preserves adhesive glycoprotein receptors in the platelets which are responsible for platelet adhesion to endothelium. It prevents expression of proinflamatory adhesive glycoprotein and inhibits proinflamatory cytokine release. |
| Pharmacokinets of Aprotinin |
| Absorption: Administered intravenously. Distribution: Distributed extracellularly and accumulates in kidneys. Metabolism: It is degraded by lysosomal enzymes in proximal tubules of kidneys. Excretion: Up to 40% is excreted in urine. |
| Onset of Action for Aprotinin |
| N/A |
| Duration of Action for Aprotinin |
| N/A |
| Half Life of Aprotinin |
| 2 to 5hours |
| Side Effects of Aprotinin |
| 1.Hypersensitivity reactions 2.Anaphylactic shock 3.Local thrombophlebitis 4.Dyspnoea 5.Tachycardia 6.Pallor 7.Cyanosis 8.Nausea 9.Rash 10.Skin eruptions |
| Contra-indications of Aprotinin |
| Hypersensitivity to the drug |
| Special Precautions while taking Aprotinin |
| 1. First give a test dose 10 minutes prior to loading dose to access allergy to the drug. 2. If hypersensitivity reactions appear during loading dose administration stops the drug immediately. |
| Pregnancy Related Information |
| Contraindicated |
| Old Age Related Information |
| May be used. |
| Breast Feeding Related Information |
| Use with caution |
| Children Related Information |
| Use with caution |
| Indications for Aprotinin |
| 1.Cardio pulmonary bypass surgery 2.Haemorrhage |
| Interactions for Aprotinin |
| Fibrinolytic agents: May inhibit the effects of fibrinolytic agents. Heparin: May prolong activated blood clotting time. Dosage may need to be adjusted. Captopril: May block the hypotensive effect of captopril. |
| Typical Dosage for Aprotinin |
| Cardio pulmonary bypass surgery: 2000,000 KIU Aprotinin loading dose, immediately after anaesthetic induction 2000,000KIU added to cardiopulmonary bypass circuit prime, and a continuous infusion of 500000 KIU during surgery until closing chest. Other wise low dose protocol is adopted which use half of full dose as effective as full dose except in anti inflammatory activity. Haemorrhage: 500000 to 1000000 KIU by slow infusion at a rate of 100000KIU/minute. Followed by 200000KIU every hour until bleeding stops. |
| Schedule of Aprotinin |
| C |
| Storage Requirements for Aprotinin |
| Store at a temperature range of 2 to 8degree C. |
| Effects of Missed Dosage of Aprotinin |
| Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose. |
| Effects of Overdose of Aprotinin |
| Treatment is supportive and symptomatic |