Dimercaprol: Difference between revisions

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|authorTag={{SG}}
|authorTag={{SG}}
|genericName=dimercaprol
|genericName=dimercaprol
|aOrAn=a
|drugClass=heavy metal chelator
|drugClass=heavy metal chelator
|indicationType=treatment
|indicationType=treatment
|indication=arsenic, gold and mercury poisoning. It is indicated in acute lead poisoning when used concomitantly with Edetate Calcium Disodium Injection USP
|indication=[[arsenic]], [[gold]] and [[mercury poisoning]]. It is indicated in acute [[lead poisoning]] when used concomitantly with [[Edetate Calcium Disodium]] Injection USP
|adverseReactions=Blepharospasm, conjunctivitis, lacrimation, nasal discharge,
|adverseReactions=[[Blepharospasm]], [[conjunctivitis]], [[lacrimation]], [[nasal discharge]],
tightness sensation, chest, limbs, jaw, abdomen
tightness sensation in [[chest]], [[limbs]], [[jaw]] and [[abdomen]], injection site pain, [[nausea]], [[vomiting]], [[headache]], [[paresthesia]], [[tremor]]
Injection site pain, nausea, vomiting, headache, paresthesia, tremor,
|blackBoxWarningTitle=<b><span style="color:#FF0000;">TITLE</span></b>
|blackBoxWarningTitle=<b><span style="color:#FF0000;">TITLE</span></b>
|blackBoxWarningBody=<i><span style="color:#FF0000;">Condition Name:</span></i> (Content)
|blackBoxWarningBody=<i><span style="color:#FF0000;">Condition Name:</span></i> (Content)
|fdaLIADAdult=====Mild Arsenic or Gold Poisoning====
*2.5 mg/kg of body weight four times daily for two days.
*Two times on the third day.
*Only once daily thereafter for ten days.
====Severe Arsenic or Gold Poisoning====
*3 mg/kg every four hours for two-days
*Four times on the third day
*Twice daily thereafter for ten days.
====Mercury poisoning====
*5 mg/kg initially, followed by 2.5 mg/kg one or two times daily for ten days.
====Acute Lead Encephalopathy====
*4 mg/kg body weight is given alone in the first dose
*Thereafter at four-hour intervals in combination with Edetate Calcium Disodium Injection USP administered at a separate site.
*For less severe poisoning the dose can be reduced to 3 mg/kg after the first dose.
*Treatment is maintained for two to seven days depending on clinical response. *Successful treatment depends on beginning injections at the earliest possible moment and on the use of adequate amounts at frequent intervals
|offLabelAdultGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of Dimercaprol in adult patients.
|offLabelAdultGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of Dimercaprol in adult patients.
|offLabelAdultNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of Dimercaprol in adult patients.
|offLabelAdultNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of Dimercaprol in adult patients.
|fdaLIADPed=====Mild Arsenic or Gold Poisoning====
*2.5 mg/kg of body weight four times daily for two days.
*Two times on the third day.
*Only once daily thereafter for ten days.
====Severe Arsenic or Gold Poisoning====
*3 mg/kg every four hours for two-days
*Four times on the third day
*Twice daily thereafter for ten days.
====Mercury poisoning====
*5 mg/kg initially, followed by 2.5 mg/kg one or two times daily for ten days.
====Acute Lead Encephalopathy====
*4 mg/kg body weight is given alone in the first dose
*Thereafter at four-hour intervals in combination with Edetate Calcium Disodium Injection USP administered at a separate site.
*For less severe poisoning the dose can be reduced to 3 mg/kg after the first dose.
*Treatment is maintained for two to seven days depending on clinical response. *Successful treatment depends on beginning injections at the earliest possible moment and on the use of adequate amounts at frequent intervals
|offLabelPedGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of Dimercaprol in pediatric patients.
|offLabelPedGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of Dimercaprol in pediatric patients.
|offLabelPedNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of Dimercaprol in pediatric patients.
|offLabelPedNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of Dimercaprol in pediatric patients.
|contraindications=BAL in Oil (Dimercaprol Injection USP) is contraindicated in most instances of hepatic insufficiency with the exception of postarsenical jaundice. The drug should be discontinued or used only with extreme caution if acute renal insufficiency develops during therapy.
|contraindications=*Dimercaprol (Dimercaprol Injection USP) is contraindicated in most instances of [[hepatic insufficiency]] with the exception of postarsenical [[jaundice]].  
|warnings=There may be local pain at the site of the injection. A reaction apparently peculiar to children is fever which may persist during therapy. It occurs in approximately 30% of children. A transient reduction of the percentage of polymorphonuclear leukocytes may also be observed.
*The drug should be discontinued or used only with extreme caution if [[acute renal insufficiency]] develops during therapy.
|clinicalTrials=One of the most consistent responses to Dimercaprol Injection USP is a rise in blood pressure accompanied by tachycardia. This rise is roughly proportional to the dose administered. Doses larger than those recommended may cause other transitory signs and symptoms in approximate order of frequency as follows: (1) nausea and, in some instance, vomiting; (2) headache; (3) a burning sensation in the lips, mouth and throat; (4) a feeling of constriction, even pain, in the throat, chest, or hands; (5) conjunctivitis, lacrimation, blepharal spasm, rhinorrhea, and salivation; (6) tingling of the hands; (7) a burning sensation in the penis; (8) sweating of the forehead, hands and other areas; (9) abdominal pain; and (10) occasional appearance of painful sterile abscesses. Many of the above symptoms are accompanied by a feeling of anxiety, weakness, and unrest and often are relieved by administration of antihistamine.
|warnings=*There may be local pain at the site of the injection.  
*A reaction apparently peculiar to children is [[fever]] which may persist during therapy.  
*It occurs in approximately 30% of children.  
*A transient reduction of the percentage of [[polymorphonuclear leukocytes]] may also be observed.
|clinicalTrials=====Cardiovascular====
*Rise in [[blood pressure]] accompanied by [[tachycardia]].  
*This rise is roughly proportional to the dose administered.  
 
Doses larger than those recommended may cause other transitory signs and symptoms in approximate order of frequency as follows:  
 
====Gastrointestinal====
*[[Nausea]]
*abdominal pain
*in some instance, [[vomiting]]
====Nervous System====
*[[Headache]]
*Tingling of the hands
*Burning sensation in the penis
 
====Ophtalmology====
*[[Conjunctivitis]]
*[[Lacrimation]]
*Blepharal spasm
 
====Other====
*[[Rhinorrhea]]
*[[Salivation]]
*[[Sweating]] of the forehead, hands and other area
*Occasional appearance of painful sterile abscesses.
*Burning sensation in the lips, mouth and throat
*A feeling of constriction, even pain, in the throat, chest, or hands
 
Many of the above symptoms are accompanied by a feeling of [[anxiety]], [[weakness]], and unrest and often are relieved by administration of [[antihistamine]].
|FDAPregCat=C
|FDAPregCat=C
|useInPregnancyFDA=Animal reproduction studies have not been conducted with BAL in Oil. It is also not known whether BAL in Oil can cause fetal harm when administered to a pregnant woman, or can affect reproduction capacity. BAL in Oil should be given to a pregnant woman only if clearly needed.
|useInPregnancyFDA=Animal reproduction studies have not been conducted with dimercaprol. It is also not known whether dimercaprol can cause fetal harm when administered to a pregnant woman, or can affect reproduction capacity. dimercaprol should be given to a pregnant woman only if clearly needed.


It is not known whether this drug is excreted in human milk. However, because many drugs are excreted in human milk, caution should be exercised when BAL in Oil is administered to a nursing woman.
It is not known whether this drug is excreted in human milk. However, because many drugs are excreted in human milk, caution should be exercised when dimercaprol is administered to a nursing woman.
|administration=*Intramuscular
|administration=*Intramuscular
|overdose=*Dosage exceeding 5 mg/kg will usually be followed by [[vomiting]], [[convulsions]] and [[stupor]], beginning within 30 minutes and subsiding within 6 hours following injection.
|overdose=*Dosage exceeding 5 mg/kg will usually be followed by [[vomiting]], [[convulsions]] and [[stupor]], beginning within 30 minutes and subsiding within 6 hours following injection.
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|packLabel=[[File:Dimercaprol FDA label.png|none|450px]]
|packLabel=[[File:Dimercaprol FDA label.png|none|450px]]
|alcohol=Alcohol-Dimercaprol interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
|alcohol=Alcohol-Dimercaprol interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
|brandNames=*Bal In Oil
|brandNames=*Bal In Oil<ref>{{cite web|url=http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=bee9a137-160f-47e8-a551-ca461ae4f51e|title=BAL- dimercaprol injection}} </ref>
}}
}}
{{LabelImage
{{LabelImage
Line 116: Line 184:
|fileName=Dimercaprol package 2.png
|fileName=Dimercaprol package 2.png
}}
}}
{{Drugbox
| name = Dimercaprol
| image = Dimercaprol.svg
| IUPAC_name = 2,3-Dimercaptopropanol
| CAS_number= 59-52-9
| ATC_prefix = V03
| ATC_suffix = AB09
| PubChem=3080
| DrugBank=
| C=3 | H=8 | O=1 | S=2
| smiles = OCC(S)CS
| molecular_weight = 124.227
| NFPA Rating = Health - 2;Flammability - 1;Reactivity - 0
| Boiling point = 120 °C
| Liquid density = 1.243 g/cm³
| Appearance = Colorless oily liquid.
| Alternate names = 1,2-dithioglycerol<br />mercaprol<br />dicaptol<br />sulfactin
}}
{{nfpa-float|2|1|0}}
'''Dimercaprol''' ([[International Nonproprietary Name|INN]]) or '''British anti-Lewisite''' (abbreviated '''[[BAL]]'''), is a compound developed by British biochemists at [[Oxford University]] during [[World War II]]. It was developed secretly as an antidote for [[Lewisite]], the now-obsolete [[arsenic]]-based [[chemical warfare agent]]. Today, it is used medically in treatment of [[arsenic]], [[Mercury (element)|mercury]] and [[lead]], and other [[heavy metals|heavy metal poisoning]]. In addition, it is used for the treatment of [[Wilson's disease]], a genetic disorder in which the body tends to retain [[copper]].
== Biochemical function ==
Heavy metals act by chemically reacting with adjacent [[sulfhydryl]] residues on metabolic enzymes, creating a [[chelate]] complex that inhibits the affected enzyme's activity. Dimercaprol competes with the sulfhydryl groups for binding the metal ion, which is then excreted in the urine.
Dimercaprol is itself toxic, with a narrow [[therapeutic index|therapeutic range]] and a tendency to concentrate arsenic in some organs. Other drawbacks include the need to administer it by painful [[intramuscular injection]].
BAL has been found to form stable chelates in vivo with many toxic metals including inorganic mercury, antimony, bismuth, cadmium, chromium, cobalt, gold, and nickel.  However, it is not necessarily the treatment of choice for toxicity to these metals.  BAL has been used as an adjunct in the treatment of the acute encephalopathy of lead toxicity. It is a potentially toxic drug, and its use may be accompanied by multiple side effects.  Although treatment with BAL will increase the excretion of cadmium, there is a concomitant increase in renal cadmium concentration, so that its use in case of cadmium toxicity is to be avoided.  It does, however, remove inorganic mercury from the kidneys; but is not useful in the treatment of alkylmercury or phenyl mercury toxicity. BAL also enhances the toxicity of selenium and tellurium, so it is not to be used to remove these metals from the body.
==See also==
* [[Chelation therapy]]
==References==
*[http://www.chm.bris.ac.uk/motm/bal/index.html British anti-Lewisite] ''Molecule of the Month'', University of Bristol School of Chemistry
* Casarett and Doull's Toxicology, the basic science of poisons
{{Antidotes}}
[[Category:Alcohols]]
[[Category:Antidotes]]
[[Category:Chelating agents]]
[[Category:Thiols]]
[[nl:dimercaprol]]
[[ja:ジメルカプロール]]
[[pl:Dimerkaprol]]

Latest revision as of 04:04, 26 January 2015

Dimercaprol
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]; Associate Editor(s)-in-Chief: Stefano Giannoni [2]

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Overview

Dimercaprol is a heavy metal chelator that is FDA approved for the treatment of arsenic, gold and mercury poisoning. It is indicated in acute lead poisoning when used concomitantly with Edetate Calcium Disodium Injection USP. Common adverse reactions include Blepharospasm, conjunctivitis, lacrimation, nasal discharge, tightness sensation in chest, limbs, jaw and abdomen, injection site pain, nausea, vomiting, headache, paresthesia, tremor.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Mild Arsenic or Gold Poisoning

  • 2.5 mg/kg of body weight four times daily for two days.
  • Two times on the third day.
  • Only once daily thereafter for ten days.

Severe Arsenic or Gold Poisoning

  • 3 mg/kg every four hours for two-days
  • Four times on the third day
  • Twice daily thereafter for ten days.

Mercury poisoning

  • 5 mg/kg initially, followed by 2.5 mg/kg one or two times daily for ten days.

Acute Lead Encephalopathy

  • 4 mg/kg body weight is given alone in the first dose
  • Thereafter at four-hour intervals in combination with Edetate Calcium Disodium Injection USP administered at a separate site.
  • For less severe poisoning the dose can be reduced to 3 mg/kg after the first dose.
  • Treatment is maintained for two to seven days depending on clinical response. *Successful treatment depends on beginning injections at the earliest possible moment and on the use of adequate amounts at frequent intervals

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Dimercaprol in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Dimercaprol in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Mild Arsenic or Gold Poisoning

  • 2.5 mg/kg of body weight four times daily for two days.
  • Two times on the third day.
  • Only once daily thereafter for ten days.

Severe Arsenic or Gold Poisoning

  • 3 mg/kg every four hours for two-days
  • Four times on the third day
  • Twice daily thereafter for ten days.

Mercury poisoning

  • 5 mg/kg initially, followed by 2.5 mg/kg one or two times daily for ten days.

Acute Lead Encephalopathy

  • 4 mg/kg body weight is given alone in the first dose
  • Thereafter at four-hour intervals in combination with Edetate Calcium Disodium Injection USP administered at a separate site.
  • For less severe poisoning the dose can be reduced to 3 mg/kg after the first dose.
  • Treatment is maintained for two to seven days depending on clinical response. *Successful treatment depends on beginning injections at the earliest possible moment and on the use of adequate amounts at frequent intervals

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Dimercaprol in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Dimercaprol in pediatric patients.

Contraindications

Warnings

  • There may be local pain at the site of the injection.
  • A reaction apparently peculiar to children is fever which may persist during therapy.
  • It occurs in approximately 30% of children.
  • A transient reduction of the percentage of polymorphonuclear leukocytes may also be observed.

Adverse Reactions

Clinical Trials Experience

Cardiovascular

Doses larger than those recommended may cause other transitory signs and symptoms in approximate order of frequency as follows:

Gastrointestinal

Nervous System

  • Headache
  • Tingling of the hands
  • Burning sensation in the penis

Ophtalmology

Other

  • Rhinorrhea
  • Salivation
  • Sweating of the forehead, hands and other area
  • Occasional appearance of painful sterile abscesses.
  • Burning sensation in the lips, mouth and throat
  • A feeling of constriction, even pain, in the throat, chest, or hands

Many of the above symptoms are accompanied by a feeling of anxiety, weakness, and unrest and often are relieved by administration of antihistamine.

Postmarketing Experience

There is limited information regarding Dimercaprol Postmarketing Experience in the drug label.

Drug Interactions

There is limited information regarding Dimercaprol Drug Interactions in the drug label.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): C Animal reproduction studies have not been conducted with dimercaprol. It is also not known whether dimercaprol can cause fetal harm when administered to a pregnant woman, or can affect reproduction capacity. dimercaprol should be given to a pregnant woman only if clearly needed.

It is not known whether this drug is excreted in human milk. However, because many drugs are excreted in human milk, caution should be exercised when dimercaprol is administered to a nursing woman.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Dimercaprol in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Dimercaprol during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Dimercaprol in women who are nursing.

Pediatric Use

There is no FDA guidance on the use of Dimercaprol in pediatric settings.

Geriatic Use

There is no FDA guidance on the use of Dimercaprol in geriatric settings.

Gender

There is no FDA guidance on the use of Dimercaprol with respect to specific gender populations.

Race

There is no FDA guidance on the use of Dimercaprol with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Dimercaprol in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Dimercaprol in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Dimercaprol in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Dimercaprol in patients who are immunocompromised.

Administration and Monitoring

Administration

  • Intramuscular

Monitoring

There is limited information regarding Dimercaprol Monitoring in the drug label.

IV Compatibility

There is limited information regarding the compatibility of Dimercaprol and IV administrations.

Overdosage

  • Dosage exceeding 5 mg/kg will usually be followed by vomiting, convulsions and stupor, beginning within 30 minutes and subsiding within 6 hours following injection.

Pharmacology

Template:Chembox BeilsteinTemplate:Chembox ECNumberTemplate:Chembox E numberTemplate:Chembox RTECSTemplate:Chembox UNNumberTemplate:Chembox DensityTemplate:Chembox BoilingPtTemplate:Chembox LogPTemplate:Chembox pKaTemplate:Chembox pKbTemplate:Chembox RefractIndexTemplate:Chembox GHSPictogramsTemplate:Chembox GHSSignalWordTemplate:Chembox HPhrasesTemplate:Chembox PPhrasesTemplate:Chembox NFPATemplate:Chembox FlashPt
Dimercaprol
Names
IUPAC name
2,3-Disulfanylpropan-1-ol
Other names
2,3-Dimercaptopropanol
British anti-Lewisite
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
DrugBank
ECHA InfoCard Lua error in Module:Wikidata at line 879: attempt to index field 'wikibase' (a nil value). Lua error in Module:Wikidata at line 879: attempt to index field 'wikibase' (a nil value).
KEGG
MeSH Dimercaprol
UNII
Properties
C
3H
8S
2O
Molar mass 124.225 g mol-1
Hazards
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references

Mechanism of Action

  • The sulfhydryl groups of dimercaprol form complexes with certain heavy metals thus preventing or reversing the metallic binding of sulfhydryl-containing enzymes.
  • The complex is excreted.
  • The sustained presence of dimercaprol promotes continued excretion of the metallic poisons - arsenic, gold and mercury.
  • It is also used in combination with Edetate Calcium Disodium Injection USP to promote the excretion of lead.

Structure

Pharmacodynamics

There is limited information regarding Dimercaprol Pharmacodynamics in the drug label.

Pharmacokinetics

There is limited information regarding Dimercaprol Pharmacokinetics in the drug label.

Nonclinical Toxicology

There is limited information regarding Dimercaprol Nonclinical Toxicology in the drug label.

Clinical Studies

There is limited information regarding Dimercaprol Clinical Studies in the drug label.

How Supplied

  • 3 mL (100 mg/mL) ampules, box of 10 (NDC 17478-526-03).

Storage

  • Store at 20° to 25°C (68° to 77°F)

Images

Drug Images

{{#ask: Page Name::Dimercaprol |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}

Package and Label Display Panel

{{#ask: Label Page::Dimercaprol |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}

Patient Counseling Information

There is limited information regarding Dimercaprol Patient Counseling Information in the drug label.

Precautions with Alcohol

Alcohol-Dimercaprol interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

Look-Alike Drug Names

There is limited information regarding Dimercaprol Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

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

  1. ↑ "BAL- dimercaprol injection".

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