have the option Dimercaprol Class: Heavy Metal Antagonists ATC Class: V03AB09 VA Class: AD300 CAS Number: 59-52-9 Brands: BAL in Oil Overview Side Effects Professional Interactions Reviews More Support Group Q & A Introduction Dithiol heavy metal antagonist; chelates arsenic, lead, mercury, gold, and other heavy metals. a b Slideshow Hives: The What, Where, And Why Of This Bizarre Skin Condition Uses for Dimercaprol Arsenic, Mercury, and Gold Poisoning Antidote of choice in treatment of acute arsenic (except arsine), mercury, or gold poisoning following ingestion of salts of these metals or overdosage of therapeutic agents containing these metals. a b Most effective when administered early in the course of poisoning; administration should be accompanied by appropriate supportive measures. a b For treatment of acute poisoning by mercury salts, most effective if administered within 1 2 hours following ingestion. a b Does not reverse extensive mercury-induced renal damage. a Minimally effective in chronic mercury poisoning. a b Usually of no value in the treatment of hypersensitivity reactions to mercury compounds; however, has been used to treat mercury-induced acrodynia (pink disease) in infants and children. a Usually effective in treatment of chronic poisoning from inorganic or organic arsenicals. a Consult most recent AAP and CDC recommendations for information regarding chelation therapy. a i Ineffective in the treatment of poisoning resulting from arsine gas (AsH 3 ). a May be effective in the treatment of gold-induced dermatitis and gold-induced thrombocytopenia. a Dermatologic or ocular manifestations of arsenic poisoning have been effectively treated with topical dimercaprol ointment or oil solution, respectively. a Lead Poisoning Used as an adjunct to edetate calcium disodium for chelation of lead in the management of acute lead encephalopathy or symptoms suggestive of encephalopathy and symptomatic lead poisoning in patients with severe lead poisoning (blood lead concentration >100 mcg/dL in adults or >70 mcg/dL in pediatric patients). f g h Has been used for managing moderate lead poisoning; however, other agents (e.g., edetate calcium disodium, succimer) preferred for managing most cases of moderate lead poisoning. 102 103 g h Consult specialized references for detailed information on the diagnosis and management of suspected or known lead intoxication and on the decision to employ chelation therapy. 100 101 102 Not useful in acute poisonings resulting from alkyl lead compounds (e.g., tetraethyl lead). a Chemical Warfare Agent Poisoning Has been used to treat lewisite or mustard-lewisite mixture poisoning in chemical warfare or terrorism; 105 reserve for patients with signs of shock or substantial pulmonary injury. 105 Initial management includes respiratory support and immediate decontamination to prevent further absorption by the victim and to prevent contamination of others (e.g., emergency personnel, health-care workers) by direct contact or off-gassing of vapors from contaminated clothing. 105 Other Heavy Metal Poisonings No conclusive evidence regarding efficacy in the treatment of poisonings with other heavy metals (e.g., antimony, bismuth). a b Ineffective in treatment of argyria or acute toxicity from thallium, tellurium, or vanadium. a Should not be used in iron, cadmium, selenium, or uranium poisoning; resulting dimercaprol-metal complexes more toxic than metals alone. a b Dimercaprol Dosage and Administration General Administer at earliest possible time and at adequate doses at frequent intervals for greatest efficacy; a b should always be accompanied by appropriate supportive measures. a b Consult published protocols and specialized references for dosages of chelating agents, the method and sequence of administration, and specific information on precautions associated with chelation therapy. a i Maintain alkaline urine during therapy to prevent dissociation of dimercaprol-metal complex and protect the kidneys. 105 b f h (See Renal Effects under Cautions.) Lead Poisoning Various dosage regimens have been recommended in lead poisoning management; i total dose of chelator depends on patient s response to, and tolerance of, the select agent, i as well as severity of lead toxicity. i When source for lead poisoning has been identified, remove patient from that source. 102 103 104 g Chelation therapy can increase absorption of lead from the GI tract; therefore, administer only to patients who reside in environments free of lead both during and after therapy. 102 104 Administer in hospital setting; monitor cardiovascular and mental status closely. 103 g Subsequent course(s) of therapy may be required based on clinical symptoms and blood lead concentrations. g In patients with severe lead poisoning, allow 2 days without treatment to elapse before a second 5-day course of therapy is considered. 103 Assess blood lead concentrations 10 14 days after completion of chelation therapy to allow reequilibration. 103 g Administration Administer by deep IM injection. a b Has also been administered topically as a 5% ointment for dermatologic manifestations of arsenic poisoning or as a 5 10% oil solution for ocular manifestations of arsenic poisoning. a IM Administration Administer by deep IM injection. a b Consider prophylactic or therapeutic administration of antihistamines to prevent or relieve mild adverse effects. 103 a b Dosage Pediatric Patients Arsenic or Gold Poisoning Mild Arsenicor Gold Poisoning IM 2.5 mg/kg 4 times daily for 2 days; then 2.5 mg/kg twice daily on the third day; then 2.5 mg/kg once daily thereafter for 10 days. a b Severe Arsenicor Gold Poisoning IM 3 mg/kg every 4 hours for 2 days; then 3 mg/kg 4 times daily on the third day; then 3 mg/kg twice daily thereafter for 10 days a b or until recovery is complete. a Severe Gold Dermatitis IM 2.5 mg/kg every 4 hours for 2 days, then 2.5 mg/kg twice daily for about 1 week. a Mercury Poisoning IM Initially, 5 mg/kg. a b Then 2.5 mg/kg once or twice daily for 10 days. a b Mercury-induced Acrodynia IM Infants and children: 3 mg/kg every 4 hours for 2 days, then 3 mg/kg every 6 hours for 1 day, then 3 mg/kg every 12 hours for 7 8 days. a Lead Poisoning Consult most recent published protocols, including those from AAP and CDC, and specialized references for combination therapy dosage recommendations. i Lead Encephalopathy IM Initially, 4 mg/kg a b g or 75 mg/m 2 . f g Then, at least 4 hours later a (and when adequate urine flow established) begin 4 mg/kg a b or 75 mg/m 2 f g every 4 hours (i.e., 450 mg/m 2 daily), g in conjunction with edetate calcium disodium (administered at separate injection sites), a b for at least 3 days (usual duration is 5 days). a f g Decision to repeat dual therapy should be based on clinical symptoms and blood lead concentrations. g Symptoms Suggestive of Encephalopathy or Blood Lead Concentration >70 mcg/dL IM Initially, 3 4 mg/kg g or 50 75 mg/m 2 . a Then, at least 4 hours later a (and when adequate urine flow established) begin 3 4 mg/kg b g or 50 75 mg/m 2 g every 4 hours (i.e., 300 450 mg/m 2 daily), g in conjunction with edetate calcium disodium (administered at separate injection sites), a b for 3 5 days. a f g Decision to repeat dual therapy should be based on clinical symptoms and blood lead concentrations. g Chemical Warfare Agent Poisoning Lewisite or Mustard-lewisite Mixture Poisoning IM 3 5 mg/kg every 4 hours for 4 doses. 105 Adjust dosage regimen based on extent of exposure and severity of symptoms. 105 Adults Consult most recent published protocols, including those from AAP and CDC, and specialized references for combination therapy dosage recommendations. a i Arsenic or Gold Poisoning Mild Arsenic or Gold Poisoning IM 2.5 mg/kg 4 times daily for 2 days; then 2.5 mg/kg twice daily on the third day; then 2.5 mg/kg once daily thereafter for 10 days. a b Severe Arsenic or Gold Poisoning IM 3 mg/kg every 4 hours for 2 days; then 3 mg/kg 4 times daily on the third day; then 3 mg/kg twice daily thereafter for 10 days a b or until recovery is complete. a Alternatively, for severe arsenic poisoning, 3 mg/kg every 4 hours for 2 days and then 3 mg/kg twice daily thereafter for 7 10 days f or 3 5 mg/kg every 4 6 hours for 1 day and then taper dose and frequency, depending on patient s symptoms. f Severe Gold Dermatitis IM 2.5 mg/kg every 4 hours for 2 days, then 2.5 mg/kg twice daily for about 1 week. a Gold-induced Thrombocytopenia IM 100 mg twice daily for 15 days. a Mercury Poisoning IM Initially, 5 mg/kg. a b Then 2.5 mg/kg once or twice daily for 10 days. a b Alternatively, 5 mg/kg initially and then 2.5 mg/kg every 8 12 hours for 1 day, followed by 2.5 mg/kg every 12 24 hours until patient improves, up to a total of 10 days; f or 5 mg/kg every 4 hours for 48 hours, then 2.5 mg/kg every 6 hours for 48 hours, then 2.5 mg/kg every 12 hours for 7 days (total of 10 days). j Lead Poisoning Consult most recent published protocols, including those from AAP and CDC, and specialized references for combination therapy dosage recommendations. a Lead Encephalopathy IM Initially, 4 mg/kg a b g or 75 mg/m 2 . g Then, at least 4 hours later (and when adequate urine flow established) begin 4 mg/kg a b or 75 mg/m 2 g every 4 hours (i.e., 450 mg/m 2 daily), g in conjunction with edetate calcium disodium (administered at separate injection sites), a b for at least 3 days (usual duration is 5 days). a Decision to repeat dual therapy should be based on clinical symptoms and blood lead concentrations. g Symptoms Suggestive of Encephalopathy or Blood Lead Concentration >100 mcg/dL IM Initially, 3 4 mg/kg g or 50 75 mg/m 2 . a Then, at least 4 hours later (and when adequate urine flow established) begin 3 4 mg/kg b g or 50 75 mg/m 2 g every 4 hours (i.e., 300 450 mg/m 2 daily), g in conjunction with edetate calcium disodium (administered at separate injection sites), a b for at least 3 5 days. a f g Decision to repeat dual therapy should be based on clinical symptoms and blood lead concentrations. g Chemical Warfare Agent Poisoning Lewisite or Mustard-lewisite Mixture Poisoning IM 3 5 mg/kg every 4 hours for 4 doses. 105 Adjust dosage regimen based on extent of exposure and severity of symptoms. 105 Special Populations No special population dosage recommendations at this time. b Cautions for Dimercaprol Contraindications Hepatic insufficiency (except for cases of postarsenical jaundice). a b Known hypersensitivity to peanuts. 103 (See Peanut Sensitivity under Sensitivity Reactions.) Warnings/Precautions Warnings Local Effects Possible injection site pain or sterile abscesses at injection site. a b Fever Children may experience fever usually starting after second or third dose; a b may persist throughout therapy b until drug discontinued. a Hematologic Effects Possible transient reduction of the percentage of polymorphonuclear leukocytes. a b Sensitivity Reactions Peanut Sensitivity Dimercaprol injection contains 700 mg of peanut oil per 1 mL of injection solution, which may cause allergic-type reactions in susceptible individuals. b Use with caution in patients with peanut sensitivities; drugs and equipment necessary to treat allergic reactions should be readily available. b General Precautions Renal Effects Potentially nephrotoxic. a Chelate rapidly dissociates in acid medium; alkalinization of urine during therapy may prevent dissociation and protect the kidneys. a b Use with caution and/or reduce dosage in patients with oliguria. a If acute renal failure develops during therapy, discontinue drug or use very cautiously as serum concentrations of dimercaprol may reach toxic levels. a b Rheumatoid Arthritis When used in the treatment of severe reactions to gold therapy, may terminate the gold-induced remission of rheumatoid arthritis. a Cardiovascular Effects Potential dose-related rise in SBP and DBP; may be accompanied by tachycardia. a May appear 15 30 minutes following the injection; BP usually returns to normal within 2 hours. a Use with caution in patients with hypertension. a Repeated high doses may cause capillary damage and loss of protein from the circulation leading to vascular collapse. a Extremely high doses may produce coma and/or seizures. a Oral Effects Drug has a strong odor and may impart an unpleasant mercaptan-like odor to patient s breath. a Possible burning sensation of lips or mouth. a Dermatologic Effects Erythema and edema usually occur when applied topically. a Glucose-6-Phosphate Dehydrogenase Deficiency May induce hemolysis, including severe forms, in patients with glucose-6-phosphate dehydrogenase deficiency. a Screen high-risk individuals for this deficiency and monitor susceptible patients for hemolysis during therapy. a Specific Populations Pregnancy Category C. b e Lactation Not known whether dimercaprol is distributed into human milk; b however, breast-feeding is contraindicated in women receiving dimercaprol for treatment of maternal arsenic, gold, mercury, or lead poisoning because of the risk of exposing nursing infant to the toxic heavy metals. e Pediatric Use Fever may occur in 30% of children; usually starts after second or third dose and may persist throughout therapy. a b Possible transient reduction of the percentage of polymorphonuclear leukocytes. a b Hepatic Impairment Contraindicated in patients with impaired hepatic function, except postarsenical jaundice. a b (See Contraindications under Cautions.) Renal Impairment Use with extreme caution or discontinue therapy if renal impairment develops during therapy. a b (See Renal Effects under Cautions.) Common Adverse Effects Dose-related nausea/vomiting, a b BP elevation, tachycardia, a b injection site pain, fever (in children). a Interactions for Dimercaprol Specific Drugs Drug Interaction Comments Iron-containing preparations Dimercaprol forms a toxic complex with iron 103 a Do not give iron concurrently with dimercaprol; defer iron therapy 24 hours after last dimercaprol dose a b Dimercaprol Pharmacokinetics Absorption Bioavailability Peak plasma concentrations attained 30 60 minutes following IM injection. a Slowly absorbed through the skin following topical application. a Distribution Extent Distributed into all tissues (mainly in the intracellular space) including the brain, with the highest concentrations in the liver and kidneys. a Elimination Metabolism Dimercaprol (not excreted as the dimercaprol-metal complex) is rapidly metabolized to inactive products. a Some drug may be excreted as a glucuronide conjugate. a In humans, metabolism and excretion is probably complete within 4 hours. a Elimination Route Excreted in urine and feces via bile. a Stability Storage Parenteral Solution for IM Injection 20 25 C. b Actions Contains sulfhydryl groups that form heterocyclic ring complexes with heavy metals (particularly arsenic, mercury, and gold). a b These complexes prevent or reverse the binding of metallic cations to body ligands such as essential sulfhydryl-dependent enzymes. a b Does not protect sulfhydryl enzymes from metals, such as selenium, that inhibit such enzymes by an oxidation process. a If the affinity of the metal for dimercaprol is greater than that for enzymes, a mercaptide is formed, which can be excreted from the body. Dimercaprol-metal complex can dissociate (particularly in an acid medium or as the level of dimercaprol declines) or be oxidized, thus releasing the metal to exert its toxic effects again. a Has little affinity for the essential trace metals of the body (except copper); does not usually produce trace metal depletion syndromes. a However, may interfere with normal accumulation of iodine by the thyroid. a Advice to Patients When used for lead poisoning, importance of identifying source of lead poisoning and then removing patient from that source. 102 103 104 Importance of patient residing in an environment free of lead both during and after therapy. 102 104 Importance of informing clinician of allergy to peanuts. a Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. b Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs. b Importance of informing patients of other important precautionary information. (See Cautions.) Preparations Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details. Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations. Dimercaprol Routes Dosage Forms Strengths Brand Names Manufacturer Parenteral Injection, for IM use only 100 mg/mL BAL in Oil Akorn AHFS DI Essentials. Copyright 2017, Selected Revisions October 1, 2009. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814. Use is not currently included in the labeling approved by the US Food and Drug Administration. References Only references cited for selected revisions after 1984 are available electronically. 100. Piomelli S, Rosen JF, Chisolm JJ Jr et al. Management of childhood lead poisoning. J Pediatr . 1984; 105:523-32. [PubMed 6481529] 101. Pincus D, Saccar CV. Lead poisoning. Am Fam Physician . 1979; 19:120-4. [PubMed 110123] 102. US Department of Health and Human Services. Preventing lead poisoning in young children: a statement by the Centers for Disease Control October 1991. Atlanta, GA: Centers for Disease Control, National Center for Environmental Health and Injury Control 1991-537-304. Available at CDC website. 103. Committee on Drugs, American Academy of Pediatrics. Treatment guidelines for lead exposure in children. Pediatrics . 1995; 96:155-60. [PubMed 7596706] 104. Committee on Environmental Health, American Academy of Pediatrics. Lead poisoning: from screening to primary prevention. Pediatrics . 1993; 92:176-83. [PubMed 8516071] 105. Agency for Toxic Substances and Disease Registry. Medical Management Guidelines for Blister Agents: Lewisite (L) and Mustard-Lewisite Mixture (HL). From the CDC website. Accessed Nov 12, 2001. a. AHFS Drug Information 2007. McEvoy GK, ed. Dimercaprol. Bethesda, MD: American Society of Health-System Pharmacists; 2007. From AHFS website. b. Akorn, Inc. BAL in Oil (dimercaprol) injection prescribing information. Decatur, IL; Oct 2006. c. FDA Public Health Advisory: Edetate disodium (marketed as Endrate and generic products); 2008. From FDA website. d. MMWR. Deaths associated with hypocalcemia from chelation therapy - Texas, Pennsylvania, and Oregon, 2003-2005. March 2006: 55(08): 204-207. Centers for Disease Control. From CDC website. e. Briggs GC, Freeman RK, Yaffe SJ. Drugs in pregnancy and lactation.7th ed. Philadelphia, PA: Lippincott Williams & Wilkins; 2005: 489 491. f. Howland, MA. Dimercaprol (British Anti-Lewisite or BAL). In: Flomenbaum NE, Goldfrank LR, Hoffman RS et al, eds. Goldfrank s toxicologic ermergencies. 8th ed. New York: McGraw-Hill; 2006:1265-8. g. Henretig FM. Lead. In: Flomenbaum NE, Goldfrank LR, Hoffman RS et al, eds. Goldfrank s toxicologic emergencies. 8th ed. New York: McGraw-Hill; 2006:1308-24. h. Gracia R, Snodgrass W. Lead toxicity and chelation therapy. Am J Health-Syst Pharm . 2007; 64:45-53. [PubMed 17189579] i. AHFS Drug Information 2008. McEvoy GK, ed. Edetate Calcium Disodium. Bethesda, MD: American Society of Health-System Pharmacists; 2008. From AHFS website. j. Young-Jin, S. Mercury. In: Flomenbaum NE, Goldfrank LR, Hoffman RS et al, eds. Goldfrank s toxicologic emergencies. 8t ed. New York: McGraw-Hill, 2006:1334-44. 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