13 . December , 2019 - Friday
Check todays hot topics or new products

Find a Drug: Advanced

Please Sign in or Register

All about: Lepirudin

Big Image Pronouncation: (LEP-ih-ruh-din)
Class: Thrombin inhibitor

Trade Names:
Refludan
- Powder for Injection 50 mg

Mechanism of Action

Pharmacology

One molecule of lepirudin (rDNA) binds to 1 molecule of thrombin and blocks the thrombogenic activity of thrombin.

Pharmacokinetics

Distribution

Following IV administration, distribution is confined to extracellular fluids and is characterized by an initial t ½ of approximately 10 min.

Metabolism

Lepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis.

Elimination

Elimination follows first order kinetics and is characterized by a terminal t ½ of approximately 1.3 h. About 48% of the administered dose is excreted in the urine (35% unchanged).

Special Populations

Renal Function Impairment

In patients with marked renal insufficiency (CrCl less than 15 mL/min) and on hemodialysis, the elimination t ½ is prolonged up to 2 days.

Elderly

Systemic Cl is 20% lower in elderly than in younger patients.

Gender

Systemic Cl is about 25% lower in women than men.

Indications and Usage

Anticoagulation in patients with heparin-induced thrombocytopenia and associated thromboembolic disease to prevent further thromboembolic complications.

Unlabeled Uses

Adjunct therapy for treatment of unstable angina; acute MI without ST elevation; prevention of deep vein thrombosis; patients undergoing percutaneous coronary intervention.

Contraindications

Hypersensitivity to hirudins or any component of the product.

Dosage and Administration

Heparin-Induced Thrombocytopenia
Adults

IV 0.4 mg/kg (up to 110 kg body weight) slowly (eg, over 15 to 20 sec) as a bolus followed by 0.15 mg/kg (up to 110 kg/h of body weight) as a continuous IV infusion for 2 to 10 days or longer if clinically needed.

Dose Modification
Adults

IV If the confirmed APTT ratio is below the target range, increase the infusion rate in steps of 20% and determine the APTT ratio again 4 h later. Do not exceed an infusion rate of 0.21 mg/kg/h without checking for coagulation abnormalities that might prevent an appropriate APTT response. If the confirmed APTT ratio is above the target range, stop the infusion for 2 h. At restart, decrease the infusion 50% and determine the APTT ratio again 4 h later.

Renal Function Impairment
Adults

IV Reduce the dose if there is known or suspected renal function impairment (CrCl less than 60 mL/min or serum creatinine above 1.5 mg/dL). In addition to monitoring renal status, APTT monitoring should be used. In all patients with renal function impairment, the bolus dose is to be reduced to 0.2 mg/kg. Reduce the standard initial infusion rate as follows— CrCl 45 to 60 mL/min or serum creatinine 1.6 to 2 mg/dL— Administer at 50% of the standard infusion rate (0.075 mg/kg/h). CrCl 30 to 44 mL/min or serum creatinine 2.1 to 3 mg/dL— Administer at 30% of the standard infusion rate (0.045 mg/kg/h). CrCl 15 to 29 mL/min or serum creatine 3.1 to 6 mg/dL— Administer at 15% of the standard infusion rate (0.0225 mg/kg/h). Less than 15 mL/min or serum creatine greater than 6 mg/dL— Avoid or stop infusion.

Concomitant Use of Thrombolytic Therapy
Adults

IV Initial bolus of 0.2 mg/kg followed by continuous infusion of 0.1 mg/kg/h.

Switching to Oral Anticoagulants
Adults

Gradually reduce the lepirudin dose to reach an APTT ratio just above 1.5 before initiating oral anticoagulation. Initiate coumarin derivatives only when platelet counts are normalizing. Start maintenance dose with no loading dose. To avoid prothrombotic effects when initiating coumarin, continue parenteral anticoagulation for 4 to 5 days.

General Advice

  • For IV administer only. Not for intradermal, IM, or subcutaneous administration.
  • Follow manufacturer's instructions for reconstitution of powder and dilution of reconstituted solution.
  • Use reconstituted solution immediately. Discard any unused infusion solution after 24 h.
  • Refer to manufacturer's insert for compatibility with IV fluids and other medications.
  • Do not administer if solution is cloudy, discolored, or contains particulate matter.
  • Warm solution to room temperature before administration.
  • Ensure that baseline hematocrit or hemoglobin, platelet count, and APTT ratio (patient APTT over APTT reference value) are performed and evaluated prior to starting therapy.
  • Do not initiate therapy if baseline APTT ratio is 2.5 or more.
  • Ensure that APTT ratio is determined 4 h after start of therapy and after every dosage adjustment, and at least every 24 h thereafter during therapy.
  • Ensure that dosage is adjusted to maintain APTT ratio between 1.5 and 2.5 following manufacturer's recommendations for dosage adjustments.

Storage/Stability

Store unopened vials in refrigerator (36° to 46°F) or at controlled room temperature (59° to 77°F). Reconstituted solution remains stable for up to 24 h at room temperature (eg, during infusion).

Drug Interactions

Coumarin derivatives (eg, vitamin K antagonists), thrombolytics (eg, alteplase, streptokinase)

Risk of bleeding may be increased.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Heart failure (2%).

Dermatologic

Bleeding from puncture sites and wounds (11%); allergic skin reactions (4%).

EENT

Epistaxis (4%).

GI

GI and rectal bleeding (5%).

Genitourinary

Hematuria (4%); vaginal bleeding (2%).

Hematologic

Anemia or isolated drop in hemoglobin (12%); sepsis (4%).

Hepatic

Abnormal liver function (5%).

Renal

Abnormal renal function (2%).

Respiratory

Pneumonia (4%).

Miscellaneous

Hematoma or unclassified bleeding (11%); fever, multiorgan failure (4%); unspecified infections (2%); intracranial bleeding; allergic reactions (including cough, bronchospasm, stridor, dyspnea [1% to less than 10%]); anaphylactic reactions (postmarketing).

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Hypersensitivity

Allergic and hypersensitivity reactions, including anaphylaxis (resulting in shock or death), can occur.

Renal Function

Adjust the dose as indicated.

Hepatic Function

May enhance the anticoagulant effect.

Hemorrhagic events

Hemorrhagic events may occur at any site. Monitor patient for signs of bleeding throughout therapy. If bleeding develops (eg, epistaxis; hematuria; hematemesis; bloody or black, tarry stools) or is suspected (eg, unexplained fall in hematocrit or BP or any unexplained symptoms), notify health care provider immediately.

Intracranial bleeding

Life-threatening intracranial bleeding may occur with coadministration of thrombolytic therapy (eg, alteplase, streptokinase).

Overdosage

Symptoms

Bleeding.

Patient Information

  • Advise patient, family, or caregiver that medication will be prepared and administered by a health care professional in a hospital setting.
  • Instruct patient, family member, or caregiver to report any signs of bleeding or allergic reaction immediately.

Recent Drug Updates at DrugIndexOnline:





Alavert Alavert
Some commonly used brand names are: In the U.S.— Alavert 14 Allegra 12 Aller-Chlor 4 AllerMax Caplets 10 Aller-med 10 Atarax 13 Banophen 10 Banophen Caplets 10 Benadryl 10 Benadryl Allergy 10 Bromphen 2 Calm X 9 Chlo-Amine 4 Chlorate 4 Chlor-Trimeton 4 Chlor-Trimeton Allergy 4 Chlor-Trime more...

Allercon Allercon
Generic Name: triprolidine and pseudoephedrine (try PROE li deen and soo doe e FED rin) Brand Names: Actifed, Allercon, Allerfrim, Allerfrin, Histafed What is Allercon (triprolidine and pseudoephedrine)? Triprolidine is an antihistamine that reduces the natural chemical histamine in the more...

Auranofin Auranofin
Generic name: Auranofin Brand names: Ridaura Why is Auranofin prescribed? Ridaura, a gold preparation, is given to help treat rheumatoid arthritis. Ridaura is taken by mouth, unlike other gold compounds, which are given by injection. It is recommended only for people who have not been helped suf more...

Fiorinal with Codeine Fiorinal with Codeine
Generic Name: aspirin, butalbital, caffeine, and codeine (AS pir in, bue TAL bi tal, KAF een, and KOE deen) Brand Names: Fiorinal with Codeine What is Fiorinal with Codeine (aspirin, butalbital, caffeine, and codeine)? Aspirin is in a group of drugs called salicylates (sa-LIS-il-ates). more...

Fleet Enema for Children Rectal Fleet Enema for Children Rectal
Some commonly used brand names are: In the U.S.— Bisco-Lax 1 Ceo-Two 5 Dacodyl 1 Deficol 1 Dulcolax 1 Fleet Babylax 3 Fleet Bisacodyl 1 Fleet Enema 7 Fleet Enema for Children 7 Fleet Enema Mineral Oil 4 Fleet Glycerin Laxative 3 Fleet Laxative 1 Sani-Supp 3 Senokot 6 Theralax 1 Therevac P more...

Insulin Detemir Cartridges Insulin Detemir Cartridges
Generic Name: Insulin Detemir Cartridges and Prefilled Syringes (IN-su-lin DE-te-meer) Brand Name: LevemirInsulin Detemir Cartridges is used for:Treating diabetes mellitus. Insulin Detemir Cartridges is a hormone that is produced by the pancreas and is necessary for the body's correct use of foo more...

Nasop Dissolving Tablets Nasop Dissolving Tablets
Generic Name: Phenylephrine Orally Dissolving Tablets (FEN-il-EF-rin) Brand Name: NasopNasop Dissolving Tablets is used for:Relieving congestion due to colds, flu, hay fever, and other allergies. It may also be used for other conditions as determined by your doctor. Nasop Dissolving Tablets is a more...

Pro-Fast SA Pro-Fast SA
Generic Name: Phentermine Capsules and Tablets (FEN-ter-meen) Brand Name: Examples include Adipex P and Pro-Fast SAPro-Fast SA is used for:Reducing weight in obese patients when used short-term and combined with exercise, diet, and behavioral modification. Pro-Fast SA is an appetite suppressa more...