desirudin

Action and Spectrum

Actions and Spectrum: 

Actions: 

desirudin works by directly inhibiting the activity of thrombin, a key enzyme in the clotting process. Thrombin plays a crucial role in converting fibrinogen into fibrin, the protein that forms the structural framework of blood clots. By inhibiting thrombin, desirudin prevents the formation of new blood clots and helps break down existing clots. 

Spectrum: 

desirudin primarily targets preventing and treating blood clots associated with heparin-induced thrombocytopenia (HIT). HIT is an immune-mediated condition where heparin, a commonly used anticoagulant, leads to a drop in platelet count and an increased risk of blood clot formation. desirudin is specifically indicated for patients with HIT who require anticoagulation. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10%  

Hemorrhage (1-3%) 

Severe hemorrhage (3%) 

Anemia (3%) 

Injection site mass (4%) 

Wound secretion (4%) 

Deep thrombophlebitis (2%) 

Allergic reaction (2%) 

Nausea (2%) 

<1% 

Leg edema 

Fever 

Decreased hemoglobin 

Major hemorrhage 

Hypotension 

Hematuria 

Vomiting 

Impaired healing 

Dizziness 

Epistaxis 

Cerebrovascular disorder 

Hematuria 

Leg edema 

Leg pain 

Hematemesis 

Black Box Warning

Black Box Warning: 

Spinal or epidural hematomas occur after taking neuraxial anesthesia with spinal puncture. 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• Hypersensitivity 
• Active bleeding  
• Irreversible coagulation disorders 

Cautions: 

• Renal impairment 
• Advanced age 
• Other medical conditions

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category C 

Breastfeeding warnings:  

Not indicated for lactating women. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies do not show fetal risks in the first or later trimester.        
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.       
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.        
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.        
• Category N: No data for the drug under this category is available. 

Pharmacology

Pharmacology: 

desirudin specifically inhibits the activity of thrombin, a key enzyme in the blood clotting cascade. Thrombin converts soluble fibrinogen into insoluble fibrin, leading to the formation of blood clots. By directly binding to the active site of thrombin, desirudin prevents it from converting fibrinogen to fibrin. This inhibition of thrombin activity helps to prevent the formation of new blood clots and promotes the breakdown of existing clots.  

Pharmacodynamics: 

desirudin directly inhibits thrombin, a key enzyme in the blood coagulation cascade. Thrombin is crucial in converting fibrinogen into fibrin, which is necessary to form blood clots. By inhibiting thrombin, desirudin prevents fibrin formation and inhibits blood clot formation. 

desirudin has a specific binding site on thrombin, allowing it to competitively inhibit the enzyme’s activity. It forms a stable complex with thrombin and prevents its interaction with other substrates. As a result, the clotting process is disrupted, reducing the risk of thrombus formation. 

Pharmacokinetics: 

Absorption 

The half-life of the drug is 2-4 hours 

Distribution 

The volume of distribution is 25L/kg 

The peak plasma concentration is achieved in 1-3 hours 

Metabolism 

desirudin undergoes metabolism primarily in the liver. The metabolism of desirudin involves enzymatic processes that lead to its breakdown and elimination from the body. 

Elimination and Excretion 

The drug is 40-50% unchanged in the urine.

Adminstartion

Administration: 

desirudin is administered subcutaneously and injected into the fatty tissue beneath the skin. The injection is usually given in the abdomen, approximately two inches from the belly button. However, the healthcare provider may recommend alternative injection sites like the thigh or upper arm. 

Patient Information Leaflet

Patient information leaflet 

Generic Name:  desirudin 

Pronounced as: DES-i-ROO-din 

Why do we use desirudin? 

desirudin is used to prevent and treat deep vein thrombosis (DVT), that is regarded as the formation of blood clots deep into the veins, typically in the legs. It can also treat pulmonary embolism (PE), in which a blood clot transfers to the lungs from other body parts.