Protamine sulfate

Identification

Name
Protamine sulfate
Accession Number
DB09141
Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Blood factors
Description

Protamine sulfate is a drug that reverses the anticoagulant effects of heparin by binding to it. It was originally isolated from the sperm of salmon and other species of fish but is now produced primarily through recombinant biotechnology. Protamine sulfate was approved for medical use in the United States in 1969. Protamine sulfate (protamine (protamines) s) occurs as fine white or off-white amorphous or crystalline powder. It is sparingly soluble in water. The pH is between 6 and 7. The cationic hydrogenated protamine at a pH of 6.8 to 7.1 reacts with anionic heparin at a pH of 5.0 to 7.5 to form an inactive complex.

Protein chemical formula
Not Available
Protein average weight
Not Available
Sequences
Not Available
Synonyms
Not Available
Active Moieties
NameKindUNIICASInChI Key
Protamineunknown72G3UY6T4N9012-00-4Not applicable
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Protamine Sulfate Inj 10mg/ml USPLiquid10 mgIntravenousLyphomed, Division Of Fujisawa Canada Inc.1989-12-311996-09-10Canada
Protamine Sulfate Injection USPLiquid10 mgIntravenousOmega Laboratories Ltd2000-01-26Not applicableCanada
Protamine Sulfate Injection USPSolution10 mgIntravenousSandoz Canada Incorporated1998-03-03Not applicableCanada
Protamine Sulfate Injection, USPSolution10 mgIntravenousFresenius Kabi1989-12-31Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Protamine SulfateInjection, solution10 mg/1mLIntravenousCardinal Health2000-10-182016-03-31Us
Protamine SulfateInjection, solution10 mg/1mLIntravenousFresenius Kabi2000-10-18Not applicableUs
Categories
UNII
0DE9724IHC
CAS number
9009-65-8

Pharmacology

Indication

Protamine sulfate is usually administered to reverse the large dose of heparin administered during certain surgeries, especially heart surgery.

Associated Conditions
Pharmacodynamics

Protamine sulphate 1% demonstrates activity neutralising anticoagulant properties of heparin, creating the complex heparin/protamine. Activity of protamine (towards heparin) takes place within five minutes after intravenous injection of the preparation.

Mechanism of action

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.

Absorption

After IV adminsteration, protamine sulfate takes less than 5 min. to neutralize heparin.

Volume of distribution

12.3 L

Protein binding
Not Available
Metabolism

Metabolic fate of the protamine-heparin complex has not been elucidated; however, protamine-heparin complex may be partially metabolized or attacked by fibrinolysin, freeing heparin.

Route of elimination

The mechanism of elimination/excerection has not been discovered yet.

Half life

Without heparin in healthy individuals: Median 7.4 minutes. With heparin: Median 4.5 minutes.

Clearance

Clearance is: 2.2 L/min

Toxicity

Administration of protamine sulfate intravenously could result in severe drop in blood pressure, dyspnea, bradycardia, pulmonary hypertension and anaphylaxis. Systemic hypertension, nausea, vomiting and lassitude were also reported. Overdosage of this drug may theoretically result in hemorrhage.

Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
Not Available
Food Interactions
Not Available

References

General References
  1. Product info [Link]
  2. product info [Link]
External Links
KEGG Drug
D02224
PubChem Substance
347910415
Wikipedia
Protamine_sulfate
AHFS Codes
  • 20:28.08 — Antiheparin Agents

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentCatheter Ablation / Nonvalvular Atrial Fibrillation1
4RecruitingPreventionAortic Valve Stenosis1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Injection, solutionIntravenous10 mg/1mL
LiquidIntravenous10 mg
SolutionIntravenous10 mg
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Taxonomy

Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available

Drug created on September 30, 2015 12:50 / Updated on October 16, 2018 08:41