Protamine sulphates, History, uses and pharmacological effects.

1. Protamine Sulphate
Ms. Snehpreet Sandhu
Dept. of Pharmacology
NIMS&R

4. Mechanism
 It is a highly cationic peptide that binds to either heparin or low molecular
weight heparin (LMWH) to form a stable ion pair, which does not have
anticoagulant activity.
 The ionic complex is then removed and broken down by the
reticuloendothelial system.
 In large doses, protamine sulfate may also have an independent —
however weak — anticoagulant effect.

5. Medical uses
 Protamine sulfate is usually administered to reverse the large dose of heparin
administered during certain surgeries, especially heart surgery where anti-coagulation is
necessary to prevent clot formation within the cardiopulmonary bypass pump
apparatus.
 A dose of protamine is given, by drip administered over several minutes, once the
patient is off-pump, when extracorporeal circulation and anticoagulation are no longer
needed.
 It is also used in gene transfer, protein purification and in tissue cultures as
a crosslinker for viral transduction.
 In gene therapy, protamine sulfate has been studied as a means to increase transduction
rates by both viral and nonviral-mediated delivery mechanisms (e.g. utilizing cationic
liposomes).
 Protamine is used in insulin aspart protamine and NPH insulin.