Melarsoprol

Melarsoprol is antiprotozoal drug. It is an arsenic-containing medication used for the treatment of sleeping sickness (African trypanosomiasis) with CNS involvement, but it has replaced other arsenicals for this purpose. Melarsoprol has been used medically since 1949. It is on the World Health Organization's List of Essential Medicines.

Melarsoprol is primarily indicated in conditions like Trypanosomiasis.

Melarsoprol is contraindicated in conditions like Viral infection, G6PD, Documented hypersensitivity.

The severe or irreversible adverse effects of Melarsoprol, which give rise to further complications include Liver damage, Jarisch herxheimer reaction, Jaundice, Thrombophlebitis, Erythema, Coma, Albuminuria, Urinary casts. Melarsoprol produces potentially life-threatening effects which include Agranulocytosis, Thrombocytopenia, Aplastic Anemia, Encephalopathy, Exfoliative dermatitis, Peripheral neuropathy. which are responsible for the discontinuation of Melarsoprol therapy. The symptomatic adverse reactions produced by Melarsoprol are more or less tolerable and if they become severe, they can be treated symptomatically, these include Headache, Fever, Abdominal pain, Urticaria, Arthralgia, Nausea and vomiting, Slurred speech, Erythematous rash, Abdominal colic, Convulsions, Limb pain.

IV or IM: Hypotension, which may develop suddenly and may be moderate to severe, can occur. Fatalities due to severe hypotension or cardiac arrhythmias reported. Hypotensive reactions most likely with rapid IV injection or infusion. Oral inhalation via nebulization: Hypotension, hypertension, and cardiac arrhythmias also reported rarely. When administering IM or IV, place patient in a supine position. Monitor BP during and after administration until stable; perform ECG before, during, and after administration. Appropriate equipment for maintenance of an adequate airway and other supportive measures and agents (e.g., IV fluids, vasopressor agents) for management of hypotensive reactions should be readily available. Use with caution in patients with hypertension, hypotension, or ventricular tachycardia. IV: Extravasation may result in ulceration, tissue necrosis, and/or sloughing at injection site; long-term sequelae reported. Properly position and closely observe IV needle and catheter throughout infusion; if extravasation occurs, immediately discontinue infusion and restart in another vein. Phlebitis also reported. IM: Sterile abscess and/or necrosis, pain, erythema, tenderness, and induration at injection site. Hypoglycemia, which may be severe and has been fatal in some cases, reported with IM or IV pentamidine. Has been associated with pancreatic islet cell necrosis and inappropriately high plasma insulin concentrations. Hyperglycemia and insulin-dependent diabetes mellitus (which appears to be permanent in some cases) has occurred with or without preceding hypoglycemia and ketoacidosis in patients receiving parenteral pentamidine. Hypoglycemia, hyperglycemia, and diabetes also have occurred in patients receiving pentamidine by oral inhalation via nebulization. Monitor blood glucose concentrations before, during (daily or every other day), and after IM or IV pentamidine. Use with caution in patients with hypoglycemia or hyperglycemia. Acute pancreatitis (sometimes fatal) reported with IM or IV pentamidine. Acute pancreatitis also reported rarely in patients receiving pentamidine by oral inhalation via nebulization. Use with caution in patients with pancreatitis. Discontinue if acute pancreatitis occurs. Use IM or IV pentamidine for treatment of PCP only in patients in whom the presence of P. jirovecii has been demonstrated. Prior to initiating pentamidine oral inhalation via nebulization for prevention of PCP, evaluate symptomatic patients to rule out P. jirovecii infection. Dosage of orally inhaled pentamidine used for prevention of PCP is insufficient for treatment of PCP. Patients receiving the drug for prevention of PCP may still develop acute PCP. Extrapulmonary and/or disseminated P. jirovecii infection also reported occasionally during PCP prophylaxis, usually in patients with a history of PCP. Monitor patients receiving PCP prophylaxis for signs and symptoms of pulmonary infection (e.g., fever, cough, dyspnea); evaluate those with signs or symptoms to rule out infection caused by P. jirovecii or other opportunistic or nonopportunistic pathogens. If PCP develops, discontinue prophylaxis and initiate treatment with co-trimoxazole, parenteral pentamidine, or another effective regimen. PCP prophylaxis can be reinstituted when treatment is complete. Cough and bronchospasm reported frequently when pentamidine administered by oral inhalation via nebulization, especially in those with a history of smoking or asthma. Bronchospasm also reported after parenteral administration. Cough or bronchospasm in patients receiving pentamidine by oral inhalation can be controlled in most patients by interrupting pentamidine treatment and administering a bronchodilator. Coughing also may be controlled by slowing the delivery or intensity of the pentamidine aerosol stream. Pretreatment with an orally inhaled bronchodilator may minimize occurrence of coughing and bronchospasm. IM or IV: Anaphylaxis, anaphylactoid reactions with shock, Stevens-Johnson syndrome, and toxic epidermal necrolysis reported. Use with caution in patients with Stevens-Johnson syndrome. Oral inhalation via nebulization: Anaphylaxis, allergic reaction, and nonspecific allergy reported. Pruritus, local or generalized urticaria, rash (e.g., maculopapular, pruritic) also reported with IM or IV administration. Rash, including severely pruritic, maculopapular eruption on upper chest and back, also reported in patients receiving the drug by oral inhalation via nebulization. IM or IV: Nephrotoxicity (increase in S cr and/or BUN, azotemia, renal insufficiency, renal failure) reported. Oral inhalation via nebulization: Flank pain, incontinence, increased BUN and S cr , nephritis, renal failure, renal pain, and syndrome of inappropriate antidiuretic hormone secretion (SIADH) reported rarely. Monitor renal function (BUN, S cr ) before, during (daily or every other day), and after therapy. Consider monitoring serum potassium concentrations, particularly in AIDS patients. Ensure that patients are well hydrated; monitor fluid status. (See Renal Impairment under Cautions.) IM or IV: Elevated liver function test results reported. Hepatitis, hepatomegaly, and hepatic dysfunction reported in patients receiving the drug parenterally or by oral inhalation via nebulization. Monitor hepatic function (serum bilirubin, alkaline phosphatase, AST, ALT) before, during, and after therapy. (See Hepatic Impairment under Cautions.) IM or IV: Leukopenia (e.g., neutropenia) and thrombocytopenia, which can be severe (e.g., leukocyte count <1000/mm 3 , platelet count <20,000/mm 3 ), occur occasionally. Anemia, eosinophilia, pancytopenia, and prolonged clotting time reported rarely. Oral inhalation via nebulization: Anemia reported occasionally; eosinophilia, neutropenia, nonspecific cytopenia, pancytopenia, and thrombocytopenia also reported. Monitor CBCs and platelet counts. Use with caution in patients with leukopenia, thrombocytopenia, or anemia. Consider that serious adverse effects reported with parenteral pentamidine also may occur when the drug is administered by oral inhalation via nebulization. Monitor renal function (BUN, S cr ) before, during (daily or every other day), and after IM or IV pentamidine; consider monitoring serum potassium concentrations, particularly in AIDS patients. Also monitor renal function and for hyperkalemia in patients receiving the drug by oral inhalation via nebulization. (See Renal Impairment under Cautions.) Monitor hepatic function (serum bilirubin, alkaline phosphatase, AST, ALT) before, during, and after IM or IV pentamidine. Also monitor hepatic function in patients receiving the drug by oral inhalation via nebulization. (See Hepatic Impairment under Cautions.) Monitor blood glucose concentrations before, during (daily or every other day), and after IM or IV pentamidine. Also monitor for hypoglycemia and hyperglycemia in patients receiving the drug by oral inhalation via nebulization. Because hypocalcemia has been reported, monitor serum calcium concentrations before, during, and after IM or IV pentamidine. Also monitor for hypocalcemia in patients receiving the drug by oral inhalation via nebulization. Potential risks of environmental exposure to aerosolized pentamidine in health-care personnel and visitors or other individuals present when patients are receiving pentamidine by oral inhalation via nebulization not known. Measurable levels of pentamidine can be present in room air when pentamidine is administered by oral inhalation via nebulization. Adverse effects reported in health-care personnel and others exposed to aerosolized pentamidine in the environment include eye irritation (e.g., conjunctivitis); perioral and perinasal paresthesia; burning sensation of the eyes, nose, and throat; sinus irritation; shortness of breath; cough; tightness of the chest; acute bronchospasm; headache; and light-headedness. Cough and bronchospasm frequently occur in patients receiving pentamidine by oral inhalation via nebulization; health-care personnel and other individuals present during administration of the drug may be at risk of exposure to pathogens that can be transmitted when patients cough (e.g., Mycobacterium tuberculosis ). Because of concerns about potential risks of environmental exposure to aerosolized pentamidine and lack of data regarding potential effects of the drug on the fetus or pregnancy, some clinicians suggest that pregnant women and possibly those planning to become pregnant (e.g., within 8 weeks of potential exposure) avoid environmental exposure to aerosolized pentamidine. Health-care personnel administering aerosolized pentamidine should be familiar with the manufacturer's instructions for use of the nebulizer delivery system; improper use potentially could result in release of substantial amounts of pentamidine into the environment. Because potential risks, particularly long-term and cumulative effects, associated with environmental exposure to aerosolized pentamidine not established, health-care facilities should have procedures to minimize environmental exposure to aerosolized pentamidine. Consult specialized sources for recommended procedures. Category C. For treatment of first-stage (hemolymphatic) trypanosomiasis † or treatment of leishmaniasis † in pregnant women, WHO states do not use IM or IV pentamidine during first trimester of pregnancy, but may use after first trimester. Some clinicians suggest that pregnant women and possibly those planning to become pregnant (e.g., within 8 weeks of potential exposure) avoid environmental exposure to aerosolized pentamidine. (See Environmental Exposure of Health-care Personnel and Visitors under Cautions.) Not known whether distributed into milk. Discontinue nursing or the drug. IM or IV: Safety and efficacy established for treatment of PCP in children >4 months of age; no unusual risks identified. Also has been used effectively and apparently without unusual risks in children for treatment of first-stage (hemolymphatic) African trypanosomiasis † and for treatment of leishmaniasis † . Oral inhalation via nebulization: Manufacturer states safety and efficacy not established in children ≤16 years of age. Recommended by CDC, NIH, IDSA, and AAP as an alternative for prevention of PCP in children ≥5 years of age † capable of effectively using the Respirgard II jet nebulizer. IM or IV: Use with caution in patients with hepatic impairment; safety and efficacy of alternative dosage regimens not established in these patients. Oral inhalation via nebulization: Pharmacokinetic data not available. IM or IV: Use with caution in patients with renal impairment; safety and efficacy of alternative dosage regimens not established in these patients. (See Renal Impairment under Dosage and Administration.) Oral inhalation via nebulization: Pharmacokinetic data not available.

IV or IM: Hypotension, which may develop suddenly and may be moderate to severe, can occur. Fatalities due to severe hypotension or cardiac arrhythmias reported. Hypotensive reactions most likely with rapid IV injection or infusion. Oral inhalation via nebulization: Hypotension, hypertension, and cardiac arrhythmias also reported rarely. When administering IM or IV, place patient in a supine position. Monitor BP during and after administration until stable; perform ECG before, during, and after administration. Appropriate equipment for maintenance of an adequate airway and other supportive measures and agents (e.g., IV fluids, vasopressor agents) for management of hypotensive reactions should be readily available. Use with caution in patients with hypertension, hypotension, or ventricular tachycardia. IV: Extravasation may result in ulceration, tissue necrosis, and/or sloughing at injection site; long-term sequelae reported. Properly position and closely observe IV needle and catheter throughout infusion; if extravasation occurs, immediately discontinue infusion and restart in another vein. Phlebitis also reported. IM: Sterile abscess and/or necrosis, pain, erythema, tenderness, and induration at injection site. Hypoglycemia, which may be severe and has been fatal in some cases, reported with IM or IV pentamidine. Has been associated with pancreatic islet cell necrosis and inappropriately high plasma insulin concentrations. Hyperglycemia and insulin-dependent diabetes mellitus (which appears to be permanent in some cases) has occurred with or without preceding hypoglycemia and ketoacidosis in patients receiving parenteral pentamidine. Hypoglycemia, hyperglycemia, and diabetes also have occurred in patients receiving pentamidine by oral inhalation via nebulization. Monitor blood glucose concentrations before, during (daily or every other day), and after IM or IV pentamidine. Use with caution in patients with hypoglycemia or hyperglycemia. Acute pancreatitis (sometimes fatal) reported with IM or IV pentamidine. Acute pancreatitis also reported rarely in patients receiving pentamidine by oral inhalation via nebulization. Use with caution in patients with pancreatitis. Discontinue if acute pancreatitis occurs. Use IM or IV pentamidine for treatment of PCP only in patients in whom the presence of P. jirovecii has been demonstrated. Prior to initiating pentamidine oral inhalation via nebulization for prevention of PCP, evaluate symptomatic patients to rule out P. jirovecii infection. Dosage of orally inhaled pentamidine used for prevention of PCP is insufficient for treatment of PCP. Patients receiving the drug for prevention of PCP may still develop acute PCP. Extrapulmonary and/or disseminated P. jirovecii infection also reported occasionally during PCP prophylaxis, usually in patients with a history of PCP. Monitor patients receiving PCP prophylaxis for signs and symptoms of pulmonary infection (e.g., fever, cough, dyspnea); evaluate those with signs or symptoms to rule out infection caused by P. jirovecii or other opportunistic or nonopportunistic pathogens. If PCP develops, discontinue prophylaxis and initiate treatment with co-trimoxazole, parenteral pentamidine, or another effective regimen. PCP prophylaxis can be reinstituted when treatment is complete. Cough and bronchospasm reported frequently when pentamidine administered by oral inhalation via nebulization, especially in those with a history of smoking or asthma. Bronchospasm also reported after parenteral administration. Cough or bronchospasm in patients receiving pentamidine by oral inhalation can be controlled in most patients by interrupting pentamidine treatment and administering a bronchodilator. Coughing also may be controlled by slowing the delivery or intensity of the pentamidine aerosol stream. Pretreatment with an orally inhaled bronchodilator may minimize occurrence of coughing and bronchospasm. IM or IV: Anaphylaxis, anaphylactoid reactions with shock, Stevens-Johnson syndrome, and toxic epidermal necrolysis reported. Use with caution in patients with Stevens-Johnson syndrome. Oral inhalation via nebulization: Anaphylaxis, allergic reaction, and nonspecific allergy reported. Pruritus, local or generalized urticaria, rash (e.g., maculopapular, pruritic) also reported with IM or IV administration. Rash, including severely pruritic, maculopapular eruption on upper chest and back, also reported in patients receiving the drug by oral inhalation via nebulization. IM or IV: Nephrotoxicity (increase in S cr and/or BUN, azotemia, renal insufficiency, renal failure) reported. Oral inhalation via nebulization: Flank pain, incontinence, increased BUN and S cr , nephritis, renal failure, renal pain, and syndrome of inappropriate antidiuretic hormone secretion (SIADH) reported rarely. Monitor renal function (BUN, S cr ) before, during (daily or every other day), and after therapy. Consider monitoring serum potassium concentrations, particularly in AIDS patients. Ensure that patients are well hydrated; monitor fluid status. (See Renal Impairment under Cautions.) IM or IV: Elevated liver function test results reported. Hepatitis, hepatomegaly, and hepatic dysfunction reported in patients receiving the drug parenterally or by oral inhalation via nebulization. Monitor hepatic function (serum bilirubin, alkaline phosphatase, AST, ALT) before, during, and after therapy. (See Hepatic Impairment under Cautions.) IM or IV: Leukopenia (e.g., neutropenia) and thrombocytopenia, which can be severe (e.g., leukocyte count <1000/mm 3 , platelet count <20,000/mm 3 ), occur occasionally. Anemia, eosinophilia, pancytopenia, and prolonged clotting time reported rarely. Oral inhalation via nebulization: Anemia reported occasionally; eosinophilia, neutropenia, nonspecific cytopenia, pancytopenia, and thrombocytopenia also reported. Monitor CBCs and platelet counts. Use with caution in patients with leukopenia, thrombocytopenia, or anemia. Consider that serious adverse effects reported with parenteral pentamidine also may occur when the drug is administered by oral inhalation via nebulization. Monitor renal function (BUN, S cr ) before, during (daily or every other day), and after IM or IV pentamidine; consider monitoring serum potassium concentrations, particularly in AIDS patients. Also monitor renal function and for hyperkalemia in patients receiving the drug by oral inhalation via nebulization. (See Renal Impairment under Cautions.) Monitor hepatic function (serum bilirubin, alkaline phosphatase, AST, ALT) before, during, and after IM or IV pentamidine. Also monitor hepatic function in patients receiving the drug by oral inhalation via nebulization. (See Hepatic Impairment under Cautions.) Monitor blood glucose concentrations before, during (daily or every other day), and after IM or IV pentamidine. Also monitor for hypoglycemia and hyperglycemia in patients receiving the drug by oral inhalation via nebulization. Because hypocalcemia has been reported, monitor serum calcium concentrations before, during, and after IM or IV pentamidine. Also monitor for hypocalcemia in patients receiving the drug by oral inhalation via nebulization. Potential risks of environmental exposure to aerosolized pentamidine in health-care personnel and visitors or other individuals present when patients are receiving pentamidine by oral inhalation via nebulization not known. Measurable levels of pentamidine can be present in room air when pentamidine is administered by oral inhalation via nebulization. Adverse effects reported in health-care personnel and others exposed to aerosolized pentamidine in the environment include eye irritation (e.g., conjunctivitis); perioral and perinasal paresthesia; burning sensation of the eyes, nose, and throat; sinus irritation; shortness of breath; cough; tightness of the chest; acute bronchospasm; headache; and light-headedness. Cough and bronchospasm frequently occur in patients receiving pentamidine by oral inhalation via nebulization; health-care personnel and other individuals present during administration of the drug may be at risk of exposure to pathogens that can be transmitted when patients cough (e.g., Mycobacterium tuberculosis ). Because of concerns about potential risks of environmental exposure to aerosolized pentamidine and lack of data regarding potential effects of the drug on the fetus or pregnancy, some clinicians suggest that pregnant women and possibly those planning to become pregnant (e.g., within 8 weeks of potential exposure) avoid environmental exposure to aerosolized pentamidine. Health-care personnel administering aerosolized pentamidine should be familiar with the manufacturer's instructions for use of the nebulizer delivery system; improper use potentially could result in release of substantial amounts of pentamidine into the environment. Because potential risks, particularly long-term and cumulative effects, associated with environmental exposure to aerosolized pentamidine not established, health-care facilities should have procedures to minimize environmental exposure to aerosolized pentamidine. Consult specialized sources for recommended procedures. Category C. For treatment of first-stage (hemolymphatic) trypanosomiasis † or treatment of leishmaniasis † in pregnant women, WHO states do not use IM or IV pentamidine during first trimester of pregnancy, but may use after first trimester. Some clinicians suggest that pregnant women and possibly those planning to become pregnant (e.g., within 8 weeks of potential exposure) avoid environmental exposure to aerosolized pentamidine. (See Environmental Exposure of Health-care Personnel and Visitors under Cautions.) Not known whether distributed into milk. Discontinue nursing or the drug. IM or IV: Safety and efficacy established for treatment of PCP in children >4 months of age; no unusual risks identified. Also has been used effectively and apparently without unusual risks in children for treatment of first-stage (hemolymphatic) African trypanosomiasis † and for treatment of leishmaniasis † . Oral inhalation via nebulization: Manufacturer states safety and efficacy not established in children ≤16 years of age. Recommended by CDC, NIH, IDSA, and AAP as an alternative for prevention of PCP in children ≥5 years of age † capable of effectively using the Respirgard II jet nebulizer. IM or IV: Use with caution in patients with hepatic impairment; safety and efficacy of alternative dosage regimens not established in these patients. Oral inhalation via nebulization: Pharmacokinetic data not available. IM or IV: Use with caution in patients with renal impairment; safety and efficacy of alternative dosage regimens not established in these patients. (See Renal Impairment under Dosage and Administration.) Oral inhalation via nebulization: Pharmacokinetic data not available.

3.6 mg/kg (3.6 (3.6)) As recommended. IM — Once in 3 days 3.6 mg/kg (3.6 (3.6)) As recommended. IV — Once in 3 days

No child dosage information is recorded for this medicine yet.

No neonatal dosage information is recorded for this medicine yet.

No data regarding the interactions of Melarsoprol was found.

No storage information is recorded for this medicine yet.