Leucovorin (injection): Difference between revisions

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{{drugbox
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| IUPAC_name = 2-[4-[(2-amino-5-formyl-4-oxo-5,6,7,8-<br>tetrahydro-1''H''-pteridin-6-yl)methylamino]<br>benzoyl]aminopentanedioic acid
|authorTag=
| image = Folinic acid.svg
 
| width = 300px
 
| CAS_number = 1492-18-8
<!--Overview-->
| ATC_prefix = V03
 
| ATC_suffix = AF03
|genericName=
| PubChem = 54575
 
| DrugBank = APRD00698
 
| C = 20 |H = 23 |N = 7 |O = 7
 
| molecular_weight = 473.44 [[Gram|g]]/[[Mole (unit)|mol]]
|aOrAn=
| bioavailability = Dose dependent:
 
*97% (25mg)
a
*75% (50mg)
 
*37% (100mg)
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| elimination_half-life = 6.2 hours
 
| excretion = Urinary
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* Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.


<!--Brand Names-->


==Overview==
|brandNames=
'''Folinic acid''' ([[International Nonproprietary Name|INN]]) or '''leucovorin''' ([[USAN]]), generally administered as '''calcium folinate''' (or '''leucovorin calcium'''), is an [[adjuvant]] used in [[cancer]] [[chemotherapy]] involving the drug [[methotrexate]]. It is also used in [[synergy|synergistic]] combination with the chemotherapy agent [[5-fluorouracil]].


Folinic acid is ''not'' [[folic acid]].
* ®<ref>{{Cite web | title =  | url =  }}</ref>


==Mechanism of action==
<!--Look-Alike Drug Names-->
Folinic acid is a 5-formyl derivative of [[folic acid|tetrahydrofolic acid]].  It is readily converted to other reduced folic acid derivatives (e.g. tetrahydrofolate), and thus has vitamin activity which is equivalent to folic acid. However, since it does not require the action of [[dihydrofolate reductase]] for its conversion, its function as a vitamin is unaffected by [[enzyme inhibition|inhibition]] of this enzyme by drugs such as methotrexate.


Folinic acid, therefore, allows for some [[purine]]/[[pyrimidine]] synthesis to occur in the presence of dihydrofolate reductase inhibition, so that some normal [[DNA]] replication and [[RNA]] transcription processes can proceed.
|lookAlike=


==Therapeutic use==
* A® — B®<ref name="www.ismp.org">{{Cite web  | last = | first = | title = http://www.ismp.org | url = http://www.ismp.org | publisher =  | date =  }}</ref>
Folinic acid is administered at the appropriate time following [[methotrexate]] as part of a total chemotherapeutic plan, where it may "rescue" [[bone marrow]] and gastrointestinal mucosa cells from methotrexate. There is no apparent effect on preexisting methotrexate-induced [[nephrotoxicity]].<ref>Therapeutic Information Resources Australia (2004). Calcium Folinate (Systemic) in ''AUSDI: Australian Drug Information for the Health Care Professional.'' Castle Hill: Therapeutic Information Resources Australia.</ref>


While not specifically an antidote for methotrexate, folinic acid may also be useful in the treatment of acute methotrexate overdose. Different dosing protocols are used, but folinic acid should be re-dosed until the methotrexate level is less than 5 x 10<sup>-8</sup> M (this can also be re-stated as < 0.05 μM) <ref>www.cancercare.on.ca/pdfdrugs/leucovo.pdf</ref>
<!--Drug Shortage Status-->


Folinic acid is also used in combination with the chemotherapy agent [[5-fluorouracil]] in treating [[colon cancer]].  In this case, folinic acid is not used for "rescue" purposes; rather, it enhances the effect of [[5-fluorouracil]] on inhibiting [[thymidylate synthase]].
|drugShortage=
}}


Folinic acid is also sometimes used to prevent toxic effects of high doses of [[antimicrobial]] dihydrofolate reductase inhibitors such as [[trimethoprim]] and [[pyrimethamine]].
<!--Pill Image-->


==Note on administration==
{{PillImage
Folinic acid should '''not''' be administered [[intrathecal]]ly. This may produce severe adverse effects or even death.<ref>{{cite journal | author= Jardine, LF ''et al''| title= Intrathecal Leucovorin After Intrathecal Methotrexate Overdose | journal= J Pediatr Hematol Oncol | year= 1996| volume= 18| issue= 3| pages= 302&ndash;304 | url=http://www.jpho-online.com/pt/re/jpho/abstract.00043426-199608000-00014.htm | id= PMID 8689347}}</ref>
|fileName=No image.jpg|This image is provided by the National Library of Medicine.
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==References==
<!--Label Display Image-->
{{reflist|2}}
{{Detoxifying agents for antineoplastic treatment}}


{{LabelImage
|fileName={{PAGENAME}}11.png|This image is provided by the National Library of Medicine.
}}


[[Category:Chemotherapeutic adjuvants]]
{{LabelImage
[[Category:Folates]]
|fileName={{PAGENAME}}11.png|This image is provided by the National Library of Medicine.
}}


[[da:Folinsyre]]
<!--Category-->
[[de:Folinsäure]]
[[fr:Acide folinique]]
[[he:חומצה פולינית]]
[[ja:フォリン酸]]


{{WH}}
[[Category:Drug]]
{{WS}}

Revision as of 18:46, 10 February 2015

Leucovorin (injection)
Black Box Warning
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1];

Disclaimer

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Black Box Warning

Title
See full prescribing information for complete Boxed Warning.
ConditionName:
  • Content

Overview

Leucovorin (injection) is a that is FDA approved for the {{{indicationType}}} of . There is a Black Box Warning for this drug as shown here. Common adverse reactions include .

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Condition1
  • Dosing Information
  • Dosage
Condition2
  • Dosing Information
  • Dosage
Condition3
  • Dosing Information
  • Dosage
Condition4
  • Dosing Information
  • Dosage

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

Condition1
  • Developed by:
  • Class of Recommendation:
  • Strength of Evidence:
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Guideline-Supported Use of Leucovorin (injection) in adult patients.

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Leucovorin (injection) in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding FDA-Labeled Use of Leucovorin (injection) in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

Condition1
  • Developed by:
  • Class of Recommendation:
  • Strength of Evidence:
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Guideline-Supported Use of Leucovorin (injection) in pediatric patients.

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Leucovorin (injection) in pediatric patients.

Contraindications

  • Condition1

Warnings

Title
See full prescribing information for complete Boxed Warning.
ConditionName:
  • Content
  • Description

Precautions

  • Description

Adverse Reactions

Clinical Trials Experience

There is limited information regarding Clinical Trial Experience of Leucovorin (injection) in the drug label.

Body as a Whole
Cardiovascular
Digestive
Endocrine
Hematologic and Lymphatic
Metabolic and Nutritional
Musculoskeletal
Neurologic
Respiratory
Skin and Hypersensitivy Reactions
Special Senses
Urogenital
Miscellaneous

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Leucovorin (injection) in the drug label.

Body as a Whole
Cardiovascular
Digestive
Endocrine
Hematologic and Lymphatic
Metabolic and Nutritional
Musculoskeletal
Neurologic
Respiratory
Skin and Hypersensitivy Reactions
Special Senses
Urogenital
Miscellaneous

Drug Interactions

  • Drug
  • Description

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA):

  • Pregnancy Category


Pregnancy Category (AUS):

  • Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Leucovorin (injection) in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Leucovorin (injection) during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Leucovorin (injection) with respect to nursing mothers.

Pediatric Use

There is no FDA guidance on the use of Leucovorin (injection) with respect to pediatric patients.

Geriatic Use

There is no FDA guidance on the use of Leucovorin (injection) with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Leucovorin (injection) with respect to specific gender populations.

Race

There is no FDA guidance on the use of Leucovorin (injection) with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Leucovorin (injection) in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Leucovorin (injection) in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Leucovorin (injection) in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Leucovorin (injection) in patients who are immunocompromised.

Administration and Monitoring

Administration

  • Oral
  • Intravenous

Monitoring

There is limited information regarding Monitoring of Leucovorin (injection) in the drug label.

  • Description

IV Compatibility

There is limited information regarding IV Compatibility of Leucovorin (injection) in the drug label.

Overdosage

Acute Overdose

Signs and Symptoms

  • Description

Management

  • Description

Chronic Overdose

There is limited information regarding Chronic Overdose of Leucovorin (injection) in the drug label.

Pharmacology

There is limited information regarding Leucovorin (injection) Pharmacology in the drug label.

Mechanism of Action

Structure

File:Leucovorin (injection)01.png
This image is provided by the National Library of Medicine.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Leucovorin (injection) in the drug label.

Pharmacokinetics

There is limited information regarding Pharmacokinetics of Leucovorin (injection) in the drug label.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Leucovorin (injection) in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of Leucovorin (injection) in the drug label.

How Supplied

Storage

There is limited information regarding Leucovorin (injection) Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

{{#ask: Label Page::Leucovorin (injection) |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}

Patient Counseling Information

There is limited information regarding Patient Counseling Information of Leucovorin (injection) in the drug label.

Precautions with Alcohol

  • Alcohol-Leucovorin (injection) interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

Look-Alike Drug Names

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

  1. Empty citation (help)
  2. "http://www.ismp.org". External link in |title= (help)


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