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Argatroban
Overview
What is Argatroban?
Argatroban is a synthetic direct thrombin inhibitor and the chemical name is 1-[5- [(aminoiminomethyl)amino]-1-oxo-2-[[(1,2,3,4-tetrahydro-3-methyl-8-quinolinyl)sulfonyl]amino]pentyl]-4-methyl-2-piperidinecarboxylic acid, monohydrate. Argatroban has 4 asymmetric carbons. One of the asymmetric carbons has an configuration (stereoisomer Type I) and an configuration (stereoisomer Type II). Argatroban consists of a mixture of and stereoisomers at a ratio of approximately 65:35.
The molecular formula of argatroban is CHNOS•HO. Its molecular weight is 526.66 g/mol. The structural formula is:
Argatroban is a white, or almost white crystalline powder that is sparingly soluble in ethanol, and insoluble in acetone, ethyl acetate, and ether.
Argatroban injection is a sterile clear, colorless to pale yellow, slightly viscous solution in a single-dose amber vial containing 250 mg/2.5 mL of argatroban. Each mL of sterile, nonpyrogenic solution contains 100 mg argatroban, 300 mg D-sorbitol, and 400 mg dehydrated alcohol in water for injection.
What does Argatroban look like?
What are the available doses of Argatroban?
250 mg/2.5 mL single-dose vial ()
What should I talk to my health care provider before I take Argatroban?
How should I use Argatroban?
Argatroban injection is indicated for prophylaxis or treatment of thrombosis in adult patients with heparin-induced thrombocytopenia (HIT).
Argatroban injection must be diluted 100-fold prior to infusion. Argatroban injection should not be mixed with other drugs prior to dilution.
Argatroban injection should be diluted in 0.9% Sodium Chloride Injection, 5% Dextrose Injection, or Lactated Ringer’s Injection to a final concentration of 1 mg/mL. The contents of each 2.5-mL vial should be diluted 100-fold by mixing with 250 mL of diluent. Use 250 mg (2.5 mL) per 250 mL of diluent or 500 mg (5 mL) per 500 mL of diluent.
The constituted solution must be mixed by repeated inversion of the diluent bag for 1 minute. Upon preparation, the solution may show slight but brief haziness due to the formation of microprecipitates that rapidly dissolve upon mixing. Use of diluent at room temperature is recommended. Colder temperatures can slow down the rate of dissolution of precipitates. The final solution must be clear before use. The pH of the intravenous solution prepared as recommended is 3.2 to 7.5. Solutions prepared as recommended are stable at controlled room temperature, 20°C to 25°C (68°F to 77°F) (see USP) in ambient indoor light for 24 hours; therefore, light-resistant measures such as foil protection for intravenous lines are unnecessary. Solutions are physically and chemically stable for up to 96 hours when protected from light and stored at controlled room temperature, 20°C to 25°C (68°F to 77°F) (see USP), or at refrigerated conditions, 5°C ± 3°C (41°F ± 5°F). Prepared solutions should not be exposed to direct sunlight. No significant potency losses have been noted following simulated delivery of the solution through intravenous tubing.
Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit.
What interacts with Argatroban?
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What are the warnings of Argatroban?
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What are the precautions of Argatroban?
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What are the side effects of Argatroban?
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What should I look out for while using Argatroban?
Argatroban is contraindicated in
What might happen if I take too much Argatroban?
Excessive anticoagulation, with or without bleeding, may be controlled by discontinuing argatroban or by decreasing the argatroban dose. In clinical studies, anticoagulation parameters generally returned from therapeutic levels to baseline within 2 to 4 hours after discontinuation of the drug. Reversal of anticoagulant effect may take longer in patients with hepatic impairment.
No specific antidote to argatroban is available; if life-threatening bleeding occurs and excessive plasma levels of argatroban are suspected, discontinue argatroban immediately and measure aPTT and other coagulation parameters. When argatroban was administered as a continuous infusion (2 mcg/kg/min) prior to and during a 4-hour hemodialysis session, approximately 20% of argatroban was cleared through dialysis.
Single intravenous doses of argatroban at 200, 124, 150, and 200 mg/kg were lethal to mice, rats, rabbits, and dogs, respectively. The symptoms of acute toxicity were loss of righting reflex, tremors, clonic convulsions, paralysis of hind limbs, and coma.
How should I store and handle Argatroban?
Store at 20°C to 25°C (68°F to 77°F). Excursion permitted between 15°C to 30°C (59°F to 86°F). See USP controlled room temperature.Discard any unused EMFLAZA Oral Suspension remaining after 1 month of first opening the bottle. Store at 20°C to 25°C (68°F to 77°F). Excursion permitted between 15°C to 30°C (59°F to 86°F). See USP controlled room temperature.Discard any unused EMFLAZA Oral Suspension remaining after 1 month of first opening the bottle. Argatroban injection is a sterile, clear, colorless to pale yellow, slightly viscous solution supplied in 2.5 mL solution in single-dose amber vials at the concentration of . Each vial contains 250 mg of argatroban. 2.5 mL, Single Dose Vial in a Carton: NDC 70121-1037-1 Store the vials in original cartons at 20° to 25°C (68° to 77°F); excursions permitted between 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature]. Do not freeze. Retain in the original carton to protect from light. If the solution is cloudy, or if an insoluble precipitate is noted, the vial should be discarded. Argatroban injection is a sterile, clear, colorless to pale yellow, slightly viscous solution supplied in 2.5 mL solution in single-dose amber vials at the concentration of . Each vial contains 250 mg of argatroban. 2.5 mL, Single Dose Vial in a Carton: NDC 70121-1037-1 Store the vials in original cartons at 20° to 25°C (68° to 77°F); excursions permitted between 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature]. Do not freeze. Retain in the original carton to protect from light. If the solution is cloudy, or if an insoluble precipitate is noted, the vial should be discarded. Argatroban injection is a sterile, clear, colorless to pale yellow, slightly viscous solution supplied in 2.5 mL solution in single-dose amber vials at the concentration of . Each vial contains 250 mg of argatroban. 2.5 mL, Single Dose Vial in a Carton: NDC 70121-1037-1 Store the vials in original cartons at 20° to 25°C (68° to 77°F); excursions permitted between 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature]. Do not freeze. Retain in the original carton to protect from light. If the solution is cloudy, or if an insoluble precipitate is noted, the vial should be discarded.
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
Argatroban is a direct thrombin inhibitor that reversibly binds to the thrombin active site. Argatroban does not require the co-factor antithrombin III for antithrombotic activity. Argatroban exerts its anticoagulant effects by inhibiting thrombin-catalyzed or -induced reactions, including fibrin formation; activation of coagulation factors V, VIII, and XIII; activation of protein C; and platelet aggregation.
Argatroban inhibits thrombin with an inhibition constant (Ki) of 0.04 μM. At therapeutic concentrations, argatroban has little or no effect on related serine proteases (trypsin, factor Xa, plasmin, and kallikrein).
Argatroban is capable of inhibiting the action of both free and clot-associated thrombin.
Non-Clinical Toxicology
Argatroban is contraindicated inEthanol:
Clinical evidence has shown that etretinate can be formed with concurrent ingestion of acitretin and ethanol (see boxed AND and ).
Glyburide:
In a trial of 7 healthy male volunteers, acitretin treatment potentiated the blood glucose-lowering effect of glyburide (a sulfonylurea similar to chlorpropamide) in 3 of the 7 subjects. Repeating the trial with 6 healthy male volunteers in the absence of glyburide did not detect an effect of acitretin on glucose tolerance. Careful supervision of diabetic patients under treatment with acitretin is recommended (see and ).
Hormonal Contraceptives:
It has not been established if there is a pharmacokinetic interaction between acitretin and combined oral contraceptives. However, it has been established that acitretin interferes with the contraceptive effect of microdosed progestin “minipill” preparations. Microdosed “minipill” progestin preparations are not recommended for use with acitretin (see ).
Methotrexate:
An increased risk of hepatitis has been reported to result from combined use of methotrexate and etretinate. Consequently, the combination of methotrexate with acitretin is also contraindicated (see ).
Phenytoin:
Tetracyclines:
Since both acitretin and tetracyclines can cause increased intracranial pressure, their combined use is contraindicated (see and ).
Vitamin A and Oral Retinoids:
Concomitant administration of vitamin A and/or other oral retinoids with acitretin must be avoided because of the risk of hypervitaminosis A.
Other:
There appears to be no pharmacokinetic interaction between acitretin and cimetidine, digoxin, or glyburide. Investigations into the effect of acitretin on the protein binding of anticoagulants of the coumarin type (warfarin) revealed no interaction.
Hemorrhage can occur at any site in the body in patients receiving argatroban. Unexplained fall in hematocrit or blood pressure may indicate hemorrhage. Intracranial and retroperitoneal hemorrhage has been reported. The risk of hemorrhage with argatroban may be increased in severe hypertension, immediately following lumbar puncture, spinal anesthesia, major surgery (especially involving the brain, spinal cord, or eye), hematologic conditions associated with increased bleeding tendencies such as congenital or acquired bleeding disorders, and gastrointestinal lesions such as ulcerations.
Concomitant use of argatroban with antiplatelet agents, thrombolytics, and other anticoagulants may increase the risk of bleeding.
The following adverse reaction is also discussed in other sections of the labeling:
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
While we update our database periodically, we cannot guarantee it is always updated to the latest version.
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