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with regards to [2:<1% of the plasma concentration Metabolism Undergoes enterohepatic recirculation Excretion Feces (> 94% as unchanged drug); urine ( <1%) Time to Peak Dual peak serum concentrations at 1 to 8 hours and at 24 to 96 hours after dose due to enterohepatic cycling Half-Life Elimination Children (4 months to 12 years): 60 hours (range: 31-163 hours); Adults: 2.9 days; Adults with AIDS: 2.2 days Protein Binding> 99% Use: Labeled Indications Pneumocystis jirovecii pneumonia (PCP), prophylaxis: Prevention of PCP in adults and adolescents 13 years and older who are intolerant to trimethoprim-sulfamethoxazole (TMP-SMZ) Pneumocystis jirovecii pneumonia (PCP), treatment: Acute oral treatment of mild-to-moderate PCP in adults and adolescents 13 years and older who are intolerant to TMP-SMZ Off Label Uses Babesiosis Data from a prospective, nonblinded, randomized trial in patients with non-life-threatening babesiosis, supports the use of atovaquone (in combination with azithromycin) for the treatment of this condition [Krause 2000] . Clinical experience also suggests the utility of atovaquone (in combination with azithromycin) for the treatment of immunocompetent patients with mild-to-moderate babesiosis [Vannier 2012] . Additional trials may be necessary to further define the role of atovaquone in the treatment of this condition. Based on the Infectious Diseases Society of America (IDSA) guidelines for the clinical assessment, treatment, and prevention of Lyme disease, human granulocytic anaplasmosis, and babesiosis , atovaquone (in combination with azithromycin) is effective and recommended for the treatment of babesiosis. Toxoplasma gondii encephalitis (prophylaxis/treatment/chronic maintenance) in HIV-infected patients (adolescents and adults) Based on the US Department of Health and Human Services (HHS) Guidelines for Prevention and Treatment of Opportunistic Infections in HIV-Infected Adults and Adolescents , atovaquone is an effective and recommended agent for prophylaxis, treatment, or as chronic maintenance therapy for T. gondii encephalitis in adolescent and adult HIV-infected patients. Toxoplasma gondii encephalitis (prophylaxis) in HIV-exposed/infected patients (children) Based on the Centers for Disease Control and Prevention (CDC), the National Institutes of Health (NIH), the HIV Medicine Association (HIVMA) of the Infectious Diseases Society of America (IDSA), the Pediatric Infectious Diseases Society, and the American Academy of Pediatrics (AAP) guidelines for the prevention and treatment of opportunistic infections among HIV-exposed and HIV-Infected children , atovaquone is effective and recommended for the prophylaxis of T. gondii encephalitis in HIV-exposed/-infected children. Contraindications Hypersensitivity to atovaquone or any component of the formulation Dosing: Adult Pneumocystis jirovecii pneumonia (PCP), prevention: Oral: 1,500 mg once daily with food PCP, mild-to-moderate, treatment: Oral: 750 mg twice daily with food for 21 days Babesiosis (off-label use): Oral: 750 mg twice daily with azithromycin for 7 to 10 days; Note: Relapsing infection may require at least 6 weeks of therapy (Krauss 2000; Vannier 2012). Toxoplasma gondii encephalitis in HIV-infected patients (off-label use) (HHS [OI adult 2015]): Oral: Prophylaxis: 1,500 mg once daily with food (either as monotherapy or with pyrimethamine plus leucovorin) Treatment: 1,500 mg twice daily with food (either with pyrimethamine plus leucovorin, or with sulfadiazine, or as monotherapy) for at least 6 weeks (longer if extensive disease or incomplete response) Chronic maintenance: 750 to 1,500 mg twice daily with food (either with pyrimethamine plus leucovorin, or with sulfadiazine, or as monotherapy); may discontinue when asymptomatic and CD4 count >200 cells/mm 3 for 6 months Dosing: Geriatric Refer to adult dosing. Dosing: Pediatric Pneumocystis jirovecii pneumonia (PCP), prevention: Infants and Children <13 years (off-label use) (CDC 2009): Oral: 1 to 3 months: 30 mg/kg once daily with food 4 to 24 months: 45 mg/kg once daily with food> 24 months: 30 mg/kg once daily with food Adolescents 13 years: Refer to adult dosing. PCP, mild-to-moderate, treatment: Infants and Children <13 years (off-label use) (CDC 2009): Oral: Birth to 3 months: 30 to 40 mg/kg/day in 2 divided doses with food (maximum: 1,500 mg daily) 3 to 24 months: 45 mg/kg/day in 2 divided doses with food (maximum: 1,500 mg daily) 24 months: 30 to 40 mg/kg/day in 2 divided doses with food (maximum: 1,500 mg daily) Adolescents 13 years: Refer to adult dosing Toxoplasma gondii encephalitis in HIV-exposed/infected patients (off-label use): Infants and Children> <13 years: Prophylaxis (either as monotherapy or with pyrimethamine plus leucovorin) (CDC 2009): Oral: 1 to 3 months: 30 mg/kg once daily with food 4 to 24 months: 45 mg/kg once daily with food> 24 months: 30 mg/kg once daily with food Adolescents: Prophylaxis, treatment, and chronic maintenance (HHS [OI adult 2015]): Refer to adult dosing. Babesiosis (off-label use): Children: Oral: 40 mg/kg/day in 2 divided doses with azithromycin for 7 to 10 days (maximum: 1,500 mg daily). Note: Relapsing infection may require at least 6 weeks of therapy (Vannier 2012). Dosing: Renal Impairment There are no dosage adjustments provided in the manufacturer s labeling (has not been studied). However, atovaquone is not appreciably renally excreted. Dosing: Hepatic Impairment There are no dosage adjustments provided in the manufacturer s labeling (has not been studied). Atovaquone undergoes enterohepatic cycling and primarily hepatic excretion. Use caution in patients with severe impairment; monitor closely. Administration Oral: Must administer with food. Shake suspension gently before use. Once opened, a foil pouch can be emptied on a dosing spoon, in a cup, or directly into the mouth. Dietary Considerations Must be taken with food. Storage Store at 15 C to 25 C (59 F to 77 F). Do not freeze. Drug Interactions Efavirenz: May decrease the serum concentration of Atovaquone. Management: Consider alternatives to the use of atovaquone with efavirenz when possible. If this combination must be used, monitor for evidence of reduced atovaquone clinical effectiveness. Consider therapy modification Etoposide: Atovaquone may increase the serum concentration of Etoposide. Management: Consider separating the administration of atovaquone and etoposide by at least 1 to 2 days. Monitor therapy Etoposide Phosphate: Atovaquone may increase the serum concentration of Etoposide Phosphate. Management: Consider separating the administration of atovaquone and etoposide by at least 1 to 2 days. Monitor therapy Indinavir: Atovaquone may decrease the serum concentration of Indinavir. Monitor therapy Metoclopramide: May decrease the serum concentration of Atovaquone. Management: Consider alternatives to metoclopramide when possible; atovaquone should only be used with metoclopramide if no other antiemetics are available. Consider therapy modification Rifamycin Derivatives: May decrease the serum concentration of Atovaquone. Avoid combination Ritonavir: May decrease the serum concentration of Atovaquone. Avoid combination Tetracycline: May decrease the serum concentration of Atovaquone. Monitor therapy Adverse Reactions Frequency not always defined. Adverse reaction statistics have been compiled from studies including patients with advanced HIV disease. Consequently, it is difficult to distinguish reactions attributed to atovaquone from those caused by the underlying disease or a combination thereof. >10%: Central nervous system: Headache (16% to 31%), insomnia (10% to 19%), depression, pain Dermatologic: Skin rash (22% to 46%), pruritus (5% to 10%), diaphoresis Gastrointestinal: Diarrhea (19% to 42%), nausea (21% to 32%), vomiting (14% to 22%), abdominal pain (4% to 21%) Infection: Infection (18% to 22%) Neuromuscular & skeletal: Weakness (8% to 31%), myalgia Respiratory: Cough (14% to 25%), rhinitis (5% to 24%), dyspnea (15% to 21%), sinusitis (7% to 10%), flu-like symptoms Miscellaneous: Fever (14% to 40%) 1% to 10%: Cardiovascular: Hypotension ( 1%) Central nervous system: Dizziness (3% to 8%), anxiety ( 7%) Endocrine & metabolic: Hyponatremia (7% to 10%), hyperglycemia ( 9%), increased amylase (7% to 8%), hypoglycemia ( 1%) Gastrointestinal: Oral candidiasis (5% to 10%), anorexia ( 7%), dyspepsia ( 5%), constipation ( 3%), dysgeusia ( 3%) Hematologic & oncologic: Anemia (4% to 6%), neutropenia (3% to 5%) Hepatic: Increased liver enzymes (4% to 8%) Renal: Increased blood urea nitrogen ( 1%), increased serum creatinine ( 1%) Respiratory: Bronchospasm (2% to 4%) <1% (Limited to important or life-threatening): Acute renal failure, angioedema, constriction of the pharynx, corneal disease (vortex keratopathy), desquamation, erythema multiforme, hepatic failure (rare), hepatitis (rare), hypersensitivity reaction, methemoglobinemia, pancreatitis, Stevens-Johnson syndrome, thrombocytopenia, urticaria Warnings/Precautions Concerns related to adverse effects: Diarrhea/vomiting: Absorption may be decreased in patients who have diarrhea or vomiting; monitor closely and consider use of an antiemetic. If severe, consider use of an alternative antiprotozoal. Hypersensitivity: Hypersensitivity reactions (eg, angioedema, bronchospasm, throat tightness, urticaria) have occurred. Disease-related concerns: Gastrointestinal disorders: Consider parenteral therapy with alternative agents in patients who have difficulty taking atovaquone with food. Gastrointestinal disorders may limit absorption of oral medications; may not achieve adequate plasma levels. Hepatic impairment: Use with caution in patients with severe hepatic impairment; monitor closely; rare cases of cholestatic hepatitis, elevated liver function tests, and fatal liver failure have been reported. Pneumocystis jirovecii pneumonia (PCP): Appropriate use: When used for treatment, has only been indicated in mild-to-moderate PCP; not studied for use in severe PCP; atovaquone has less adverse effects than trimethoprim-sulfamethoxazole (TMP-SMZ) (the treatment of choice for mild-to-moderate PCP), although atovaquone is less effective than TMP-SMZ (HHS [OI adult 2015]). Concurrent drug therapy issues: Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information. Special populations: Elderly: Use with caution in elderly patients. Dosage form specific issues: Benzyl alcohol and derivatives: Some dosage forms may contain benzyl alcohol; large amounts of benzyl alcohol ( 99 mg/kg/day) have been associated with a potentially fatal toxicity ( gasping syndrome ) in neonates; the gasping syndrome consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension and cardiovascular collapse (AAP ["Inactive" 1997]; CDC 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol with caution in neonates. See manufacturer s labeling. Monitoring Parameters Hepatic function at baseline (monitor closely during treatment in patients with severe hepatic impairment), hypersensitivity reactions, CD4 count (for chronic maintenance treatment in toxoplasmosis), patient s food tolerance/ability to take atovaquone, post-dose vomiting, diarrhea Pregnancy Risk Factor C Pregnancy Considerations Adverse events were observed in animal reproduction studies. Diagnosis and treatment of Pneumocystis jirovecii pneumonia (PCP) in pregnant women is the same as in nonpregnant women; however, information specific to the use of atovaquone in pregnancy is limited (HHS [OI adult 2015]). Patient Education Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?) Patient may experience headache, nausea, vomiting, muscle pain, insomnia, sweating a lot, rhinitis, or rhinorrhea. Have patient report immediately to prescriber depression, thrush, cough, flu-like symptoms, or signs of liver problems (dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or jaundice) (HCAHPS). Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions. Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients. Next Interactions Print this page Add to My Med List More about atovaquone Side Effects During Pregnancy or Breastfeeding Dosage Information Drug Interactions Support Group Pricing & Coupons En Español 3 Reviews Add your own review/rating Drug class: miscellaneous antibiotics Consumer resources Atovaquone Atovaquone (Advanced Reading) Professional resources Atovaquone (AHFS Monograph) Atovaquone Suspension (FDA) Other brands: Mepron Related treatment guides Babesiosis Malaria Pneumocystis Pneumonia Prophylaxis Pneumocystis Pneumonia Toxoplasmosis> ]} Drug Status Rx Availability Prescription only C Pregnancy Category Risk cannot be ruled out N/A CSA Schedule Not a controlled drug Approval History Drug history at FDA Atovaquone Rating 3 User Reviews 5.5 /10 3 User Reviews 5.5 Rate it! Manufacturer Amneal Pharmaceuticals LLC Drug Class Miscellaneous antibiotics Related Drugs miscellaneous antibiotics metronidazole , Flagyl , Xifaxan , bacitracin , rifaximin , polymyxin b Babesiosis azithromycin , Zithromax , clindamycin , Cleocin , Mepron , More... Pneumocystis Pneumonia clindamycin , Bactrim , sulfamethoxazole / trimethoprim , Bactrim DS , leucovorin , More... Toxoplasmosis azithromycin , Zithromax , clindamycin , Bactrim , sulfamethoxazole / trimethoprim , More... 2 more conditions...} } special


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