Direct thrombin inhibitors
Thrombin inhibitors, including argatroban,
bivalirudin, and lep-irudin, help prevent the formation of blood clots.
Direct thrombin inhibitors are typically administered by continu-ous
I.V. infusion. They may also be given as an intra-coronary bo-lus during
cardiac catheterization. In that case, the drug begins acting in 2 minutes,
with a peak response of 15 minutes and a du-ration of 2 hours. After subQ
injection, plasma levels peak in 2 hours; after I.V. administration, levels
peak in less than 1 hour.
Effects on PTT become apparent within 4 to 5 hours of admin-istration.
In patients with heparin-induced thrombocytopenia, platelet count recovery
becomes apparent within 3 days.
Argatroban is metabolized by the liver and excreted primarily in stool.
Bivalirudin and lepirudin are metabolized by the liver and kidneys and excreted
in urine
Direct thrombin inhibitors interfere with blood
clotting by directly blocking all thrombin activity. These drugs offer several
advan-tages over heparin: direct thrombin inhibitors act against soluble as
well as clot-bound thrombin (thrombin in clots that have al-ready formed);
their anticoagulant effects are more predictable than those of heparin; and
their actions aren’t inhibited by the platelet release reaction.
The binding of the drug to thrombin is reversible.
Administered by I.V. infusion, argatroban and
lepirudin are used to treat heparin-induced thrombocytopenia (HIT). Argatroban
may also be given with aspirin to patients with HIT who are undergo-ing a
cardiac procedure, such as PTCA, coronary stent placement, or atherectomy.
·
Bivalirudin has been approved for use in patients with unsta-ble angina
undergoing PTCA, and should be used in conjunction with aspirin therapy.
·
Patients with liver dysfunction may require a reduced dose of
argatroban. Also, the dosage of bivalirudin and lepirudin may need to be
reduced in patients with impaired renal function.
·
Use caution when administering a direct thrombin inhibitor to a patient
who has an increased risk of bleeding. Patients at great-est risk for
hemorrhage are those with severe hypertension, gas-tric ulcers, or hematologic
disorders associated with increased bleeding. Patients receiving spinal
anesthesia or those undergoing a lumbar puncture or having major surgery
(especially surgery of the brain, spinal cord, or the eye) also have an
increased risk for bleeding.
·
Hemorrhage can occur as an adverse reaction to direct throm-bin
inhibitors, so avoid giving these drugs with another drug that may also
increase the risk of bleeding.
·
Discontinue all parenteral anticoagulants before administering
argatroban.
·
Administration of argatroban along with warfarin increases the INR.
·
If the patient has received heparin, allow time for heparin’s ef-fect on
PTT to decrease before administering argatroban. (See Adverse reactions to bivalirudin.)
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