Dimercaprol

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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

Dimercaprol
Dimercapril Chemical structure.png
IUPAC name 2,3-Disulfanylpropan-1-ol
Other names 2,3-Dimercaptopropanol
British anti-Lewisite
Identifiers
CAS number 59-52-9
PubChem 3080
EINECS number 200-433-7
DrugBank DB06782
KEGG D00167
MeSH Dimercaprol
RTECS number UB2625000
ATC code V03AB09
SMILES OCC(S)CS
Beilstein Reference 1732058
Properties
Molecular formula C3H8S2O
Molar mass 124.225 g mol-1
Density 1.239 g cm-3
Boiling point

120 °C, 393 K, 248 °F (at 2.0 kPa)

log P 0.627
Acidity (pKa) 8.999
Basicity (pKb) 4.998
Refractive index (nD) 1.573
Hazards
EU classification Harmful Xn
NFPA 704

NFPA 704.svg

1
2
0
 
R-phrases R22, R36/37/38
S-phrases S26, S36
Except where noted otherwise, data are given for
materials in their standard state
(at 25 °C, 100 kPa)

Infobox disclaimer and 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

Dimercaprol.png

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

Package and Label Display Panel

Dimercaprol FDA label.png

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.




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