ﺑﺎﺯﮔﺸﺖ ﺑﻪ ﺻﻔﺤﻪ ﻗﺒﻠﯽ
خرید پکیج
تعداد آیتم قابل مشاهده باقیمانده : 3 مورد
نسخه الکترونیک
medimedia.ir

Reteplase: Drug information

Reteplase: Drug information
(For additional information see "Reteplase: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Retavase;
  • Retavase Half-Kit
Pharmacologic Category
  • Thrombolytic Agent
Dosing: Adult
ST-elevation myocardial infarction, acute

ST-elevation myocardial infarction (STEMI), acute:

Note: Primary percutaneous coronary intervention (PCI) is the preferred reperfusion strategy. Thrombolytic therapy is an option in centers without PCI capability, followed by transfer to a PCI-capable center. Administer thrombolytic therapy within 30 minutes of first medical contact (in ambulance or emergency department) if primary PCI cannot be performed within 120 minutes; if primary PCI is not available, may still consider thrombolysis in patients who present late (within 12 to 24 hours of symptom onset) and have ongoing ischemia or extensive ST elevation. Administer aspirin, clopidogrel, and anticoagulant therapy (ie, unfractionated heparin, enoxaparin, or fondaparinux) in combination with thrombolytic therapy (ACCF/AHA [O'Gara 2013]; ESC [Ibanez 2018]).

IV: 10 units IV over 2 minutes, followed by a second dose 30 minutes later of 10 units IV over 2 minutes

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling. However, risks of reteplase therapy may be increased.

Hemodialysis: Dialyzable: Unknown, but unlikely (NCS/SCCM [Frontera 2016])

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling. However, risks of reteplase therapy may be increased.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%: Local: Bleeding at injection site (49%)

1% to 10%:

Gastrointestinal: Gastrointestinal hemorrhage (9%)

Hematologic & oncologic: Hemorrhage (genitourinary: 10%), anemia (1%)

<1%, postmarketing, and/or case reports: Anaphylactoid shock, hypersensitivity reaction, intracranial hemorrhage

Contraindications

Active internal bleeding; recent stroke; intracranial or intraspinal surgery or serious head trauma within 3 months; intracranial conditions that increase the risk of bleeding (eg, neoplasm, arteriovenous malformations, or aneurysm); bleeding diathesis; severe uncontrolled hypertension

Additional contraindications (ACCF/AHA [O’Gara 2013]): Ischemic stroke within 3 months; any prior intracranial hemorrhage; active bleeding (excluding menses); suspected aortic dissection; significant closed head or facial trauma within 3 months with radiographic evidence of bony fracture or brain injury

Warnings/Precautions

Concerns related to adverse effects:

• Arrhythmias: Coronary thrombolysis may result in reperfusion arrhythmias (eg, sinus bradycardia, accelerated idioventricular rhythm, ventricular premature depolarizations, ventricular tachycardia). Antiarrhythmic therapy should be available during therapy (Miller 1986).

• Bleeding: Internal bleeding (intracranial, retroperitoneal, gastrointestinal, genitourinary, respiratory) or external bleeding (especially at arterial and noncompressible venous puncture sites) may occur (may be fatal). Monitor all potential bleeding sites. If serious bleeding occurs, the infusion of reteplase and any other concurrent anticoagulants (eg, heparin) should be stopped and the patient should be treated appropriately.

• Cholesterol embolization: Has been reported rarely in patients treated with thrombolytic agents; may present as livedo reticularis, "purple toe" syndrome, acute renal failure, gangrenous digits, hypertension, pancreatitis, myocardial infarction, cerebral infarction, spinal cord infarction, retinal artery occlusion, bowel infarction, or rhabdomyolysis and can be fatal.

• Hypersensitivity reactions: Have been reported, including glossal edema, hypotension, and respiratory distress. If anaphylactoid reaction occurs, withhold second dose of reteplase and initiate appropriate therapy.

• Thromboembolic events: Use may increase risk of thromboembolic events in patients with high probability of left heart thrombus (eg, patients with mitral stenosis or atrial fibrillation).

Disease-related concerns:

• Conditions that increase bleeding risk: For the following conditions the risk of bleeding is higher with use of thrombolytics and should be weighed against the benefits of therapy: History of chronic, severe, poorly controlled hypertension; significant hypertension on presentation (systolic BP >180 mm Hg or diastolic BP >110 mm Hg); history of prior ischemic stroke >3 months; dementia; traumatic or prolonged CPR (>10 minutes); major surgery (<3 weeks); recent internal bleeding (within 2 to 4 weeks); noncompressible vascular punctures; active peptic ulcer; oral anticoagulant therapy (ACC/AHA [O’Gara 2013]); lumbar puncture within 10 days (ASRA [Horlocker 2010]).

• STEMI: Appropriate use: Follow standard management for STEMI while infusing reteplase.

Special populations:

• Older adult: Use with caution in patients with advanced age (eg, >75 years); increased risk of bleeding.

Dosage form specific issues:

Polysorbate 80: Some dosage forms may contain polysorbate 80 (also known as Tweens). Hypersensitivity reactions, usually a delayed reaction, have been reported following exposure to pharmaceutical products containing polysorbate 80 in certain individuals (Isaksson 2002; Lucente 2000; Shelley 1995). Thrombocytopenia, ascites, pulmonary deterioration, and renal and hepatic failure have been reported in premature neonates after receiving parenteral products containing polysorbate 80 (Alade 1986; CDC 1984). See manufacturer's labeling.

Other warnings/precautions:

• Administration: Intramuscular injections and nonessential handling of the patient should be avoided. Venipunctures should be performed carefully and only when necessary. Avoid internal jugular and subclavian venous punctures. If arterial puncture is necessary, use an upper extremity vessel that can be manually compressed.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Kit, Intravenous [preservative free]:

Retavase: 2 X 10 UNIT [contains polysorbate 80]

Retavase Half-Kit: 1 X 10 UNIT [contains polysorbate 80]

Generic Equivalent Available: US

No

Pricing: US

Kit (Retavase Half-Kit Intravenous)

1 X 10 unit (per each): $4,488.84

Kit (Retavase Intravenous)

2 X 10 unit (per each): $3,625.24

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

IV: For IV use only; do not administer IM. Administer reconstituted dose over 2 minutes; no other medication should be added to the injection solution.

Use: Labeled Indications

ST-elevation myocardial infarction, acute: Use in acute ST-elevation myocardial infarction (STEMI) to reduce the risk of death and heart failure.

Medication Safety Issues
High alert medication:

The Institute for Safe Medication Practices (ISMP) includes this medication (IV) among its list of drugs which have a heightened risk of causing significant patient harm when used in error.

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Agents with Antiplatelet Properties (e.g., P2Y12 inhibitors, NSAIDs, SSRIs, etc.): May enhance the anticoagulant effect of Thrombolytic Agents. Risk C: Monitor therapy

Anticoagulants: Thrombolytic Agents may enhance the anticoagulant effect of Anticoagulants. Management: Monitor for signs and symptoms of bleeding if these agents are combined. For the treatment of acute ischemic stroke, avoidance with anticoagulants is often recommended, see full drug interaction monograph for details. Risk C: Monitor therapy

Aprotinin: May diminish the therapeutic effect of Thrombolytic Agents. Risk C: Monitor therapy

Dabigatran Etexilate: Thrombolytic Agents may enhance the anticoagulant effect of Dabigatran Etexilate. Management: Carefully monitor for bleeding. Dabigatran Canadian labeling recommends avoiding use with thrombolytic agents. Consider avoiding alteplase treatment of acute ischemic stroke in patients receiving dabigatran (see full drug monograph for details). Risk C: Monitor therapy

Defibrotide: May enhance the adverse/toxic effect of Thrombolytic Agents. Specifically, the risk of hemorrhage may be increased. Risk X: Avoid combination

Desirudin: Thrombolytic Agents may enhance the anticoagulant effect of Desirudin. Management: Discontinue treatment with thrombolytic agents prior to desirudin initiation. If concomitant use cannot be avoided, monitor patients receiving these combinations closely for clinical and laboratory evidence of excessive anticoagulation. Risk D: Consider therapy modification

Herbal Products with Anticoagulant/Antiplatelet Effects (eg, Alfalfa, Anise, Bilberry): May enhance the adverse/toxic effect of Thrombolytic Agents. Bleeding may occur. Risk C: Monitor therapy

Lecanemab: May enhance the adverse/toxic effect of Thrombolytic Agents. Specifically, the risk of hemorrhage may be increased. Risk C: Monitor therapy

Limaprost: May enhance the adverse/toxic effect of Thrombolytic Agents. The risk for bleeding may be increased. Risk C: Monitor therapy

Prostacyclin Analogues: Thrombolytic Agents may enhance the adverse/toxic effect of Prostacyclin Analogues. Specifically, the antiplatelet effects of prostacyclin analogues may lead to an increased risk of bleeding when combined with thrombolytic agents. Risk C: Monitor therapy

Protein C Concentrate (Human): May enhance the adverse/toxic effect of Thrombolytic Agents. Specifically, the risk of bleeding may be increased. Risk C: Monitor therapy

Salicylates: May enhance the adverse/toxic effect of Thrombolytic Agents. An increased risk of bleeding may occur. Risk C: Monitor therapy

Tranexamic Acid: May diminish the therapeutic effect of Thrombolytic Agents. Thrombolytic Agents may diminish the therapeutic effect of Tranexamic Acid. Risk X: Avoid combination

Pregnancy Considerations

Adverse events have been observed in some animal reproduction studies. The risk of bleeding may be increased in pregnant women.

Breastfeeding Considerations

It is not known if reteplase is present in breast milk.

Monitoring Parameters

CBC, aPTT; signs/symptoms of bleeding; ECG monitoring

Mechanism of Action

Reteplase is a recombinant plasminogen activator which catalyzes the cleavage of endogenous plasminogen to generate plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action.

Pharmacokinetics (Adult Data Unless Noted)

Onset of action: Thrombolysis: 30 to 90 minutes

Half-life elimination: 13 to 16 minutes

Excretion: Feces and urine

Clearance: Plasma: 250 to 450 mL/minute

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AE) United Arab Emirates: Rapilysin;
  • (AT) Austria: Rapilysin;
  • (AU) Australia: Rapilysin;
  • (BE) Belgium: Rapilysin;
  • (BG) Bulgaria: Rapilysin;
  • (CN) China: Pai tong xin;
  • (CO) Colombia: Retelyse;
  • (DE) Germany: Rapilysin;
  • (EE) Estonia: Rapilysin;
  • (EG) Egypt: Rapilysin;
  • (FI) Finland: Rapilysin;
  • (FR) France: Rapilysin;
  • (GB) United Kingdom: Rapilysin;
  • (GR) Greece: Rapilysin;
  • (HU) Hungary: Rapilysin;
  • (IE) Ireland: Rapilysin;
  • (IN) India: Mirel | Vascium;
  • (IT) Italy: Rapilysin;
  • (KE) Kenya: Mirel;
  • (LV) Latvia: Rapilysin;
  • (NL) Netherlands: Rapilysin;
  • (NO) Norway: Rapilysin;
  • (NZ) New Zealand: Rapilysin;
  • (PH) Philippines: Mirel;
  • (PK) Pakistan: Rapilysin;
  • (PR) Puerto Rico: Retavase;
  • (PT) Portugal: Rapilysin;
  • (PY) Paraguay: Mirel;
  • (QA) Qatar: Rapilysin;
  • (RO) Romania: Rapilysin;
  • (SA) Saudi Arabia: Mirel | Rapilysin;
  • (SE) Sweden: Rapilysin;
  • (SI) Slovenia: Rapilysin;
  • (TR) Turkey: Rapilysin
  1. “A Comparison of Reteplase With Alteplase for Acute Myocardial Infarction. The Global Use of Strategies to Open Occluded Coronary Arteries (GUSTO III) Investigators,” N Engl J Med, 1997, 337(16):1118-23. [PubMed 9340503]
  2. Alade SL, Brown RE, Paquet A Jr. Polysorbate 80 and E-Ferol toxicity. Pediatrics. 1986;77(4):593-597. [PubMed 3960626]
  3. Centers for Disease Control (CDC). Unusual syndrome with fatalities among premature infants: association with a new intravenous vitamin E product. MMWR Morb Mortal Wkly Rep. 1984;33(14):198-199. http://www.cdc.gov/mmwr/preview/mmwrhtml/00000319.htm. [PubMed 6423951]
  4. De Luca G, Suryapranata H, Stone GW, et al, “Abciximab as Adjunctive Therapy to Reperfusion in Acute ST-Segment Elevation Myocardial Infarction: A Meta-Analysis of Randomized Trials,” JAMA, 2005, 293(14):1759-65. [PubMed 15827315]
  5. Ellis SG, Tendera M, de Belder MA, et al, “Facilitated PCI in Patients With ST-Elevation Myocardial Infarction,” N Engl J Med, 2008, 358(21):2205-17. [PubMed 18499565]
  6. Frontera JA, Lewin JJ 3rd, Rabinstein AA, et al; Guideline for reversal of antithrombotics in intracranial hemorrhage: a statement for healthcare professionals from the Neurocritical Care Society and Society of Critical Care Medicine. Neurocrit Care. 2016;24(1):6-46. [PubMed 26714677]
  7. Horlocker TT, Wedel DJ, Rowlingson JC, et al. Regional anesthesia in the patient receiving antithrombotic or thrombolytic therapy: American Society of Regional Anesthesia and Pain Medicine Evidence-Based Guidelines (Third Edition). Reg Anesth Pain Med. 2010;35(1):64-101. [PubMed 20052816]
  8. Ibanez B, James S, Agewall S, et al; ESC Scientific Document Group. 2017 ESC Guidelines for the management of acute myocardial infarction in patients presenting with ST-segment elevation: The Task Force for the management of acute myocardial infarction in patients presenting with ST-segment elevation of the European Society of Cardiology (ESC). Eur Heart J. 2018;39(2):119-177. doi:10.1093/eurheartj/ehx393 [PubMed 28886621]
  9. Isaksson M, Jansson L. Contact allergy to Tween 80 in an inhalation suspension. Contact Dermatitis. 2002;47(5):312-313. [PubMed 12534540]
  10. Kearon C, Akl EA, Comerota AJ, et al. Antithrombotic therapy for VTE disease: Antithrombotic Therapy and Prevention of Thrombosis, 9th ed: American College of Chest Physicians evidence-based clinical practice guidelines [published correction appears in Chest. 2012;142(6):1698-1704]. Chest. 2012;141(2)(suppl):e419S-e496S. doi: 10.1378/chest.11-2301. [PubMed 22315268]
  11. Kearon C, Akl EA, Ornelas J, et al. Antithrombotic Therapy for VTE disease: CHEST guideline and expert panel report. Chest. 2016;149(2):315-352. doi: 10.1016/j.chest.2015.11.026. [PubMed 26867832]
  12. Keeley EC, Boura JA, and Grines CL, "Comparison of Primary and Facilitated Percutaneous Coronary Interventions for ST-Elevation Myocardial Infarction: Quantitative Review of Randomised Trials," Lancet, 2006, 367(9510):579-88. [PubMed 16488801]
  13. King SB 3rd, Smith SC Jr, Hirshfeld JW Jr, et al, “2007 Focused Update of the ACC/AHA/SCAI 2005 Guideline Update for Percutaneous Coronary Intervention: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines,” J Am Coll Cardiol, 2008, 51(2):172-209. [PubMed 18191745]
  14. Lincoff AM, Califf RM, Van de Werf F, et al, “Mortality at 1 Year With Combination Platelet Glycoprotein IIb/IIIa Inhibition and Reduced-Dose Fibrinolytic Therapy vs Conventional Fibrinolytic Therapy for Acute Myocardial Infarction: GUSTO V Randomized Trial,” JAMA, 2002, 288(17):2130-5. [PubMed 12413372]
  15. Lucente P, Iorizzo M, Pazzaglia M. Contact sensitivity to Tween 80 in a child. Contact Dermatitis. 2000;43(3):172. [PubMed 10985636]
  16. Milller FC, Krucoff MW, Satler LF, et al. Ventricular arrhythmias during reperfusion. Am Heart J. 1986;112(5):928-932. [PubMed 3776819]
  17. O'Connor RE, Brady W, Brooks SC, et al, “Part 10: Acute Coronary Syndromes: 2010 American Heart Association Guidelines for Cardiopulmonary Resuscitation and Emergency Cardiovascular Care,” Circulation, 2010, 122(18 Suppl 3):787-817. [PubMed 20956226]
  18. O'Gara PT, Kushner FG, Ascheim DD, et al. 2013 ACCF/AHA guideline for the management of ST-elevation myocardial infarction: a report of the American College of Cardiology Foundation/American Heart Association Task Force on Practice Guidelines [published correction appears in Circulation. 2013;128(25):e481.] Circulation. 2013;127(4):e362-e425. [PubMed 23247304]
  19. Retavase (reteplase) [prescribing information]. Cary, NC: Chiesi USA Inc; April 2022.
  20. Smalling RW, Bode C, Kalbfleisch J, et al, “More Rapid, Complete, and Stable Coronary Thrombolysis With Bolus Administration of Reteplase Compared With Alteplase Infusion in Acute Myocardial Infarction. RAPID Investigators,” Circulation, 1995, 91(11):2725-32. [PubMed 7758177]
  21. Shelley WB, Talanin N, Shelley ED. Polysorbate 80 hypersensitivity. Lancet. 1995;345(8980):1312-1313. [PubMed 7746084]
  22. Topol EJ, GUSTO V Investigators, “Reperfusion Therapy for Acute Myocardial Infarction With Fibrinolytic Therapy or Combination Reduced Fibrinolytic Therapy and Platelet Glycoprotein IIb/IIIa Inhibition: The GUSTO V Randomized Trial,” Lancet, 2001, 357:1905-14. [PubMed 11425410]
Topic 9857 Version 156.0

آیا می خواهید مدیلیب را به صفحه اصلی خود اضافه کنید؟