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Atovaquone
Pronunciation
U.S. Brand Names
Generic Available
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(a TOE va kwone)

U.S. Brand Names
Mepron™

Generic Available

No


Pharmacological Index

Antiprotozoal


Use

Acute oral treatment of mild to moderate Pneumocystis carinii pneumonia (PCP) in patients who are intolerant to co-trimoxazole; prophylaxis of PCP in patients intolerant to co-trimoxazole; treatment/suppression of Toxoplasma gondii encephalitis, primary prophylaxis of HIV-infected persons at high risk for developing Toxoplasma gondii encephalitis


Pregnancy Risk Factor

C


Contraindications

Life-threatening allergic reaction to the drug or formulation


Warnings/Precautions

Has only been indicated in mild to moderate PCP; use with caution in elderly patients due to potentially impaired renal, hepatic, and cardiac function


Adverse Reactions

Note: 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.

Central nervous system: Headache, fever, insomnia, anxiety

Dermatologic: Rash

Gastrointestinal: Nausea, diarrhea, vomiting

Respiratory: Cough

1% to 10%:

Central nervous system: Dizziness

Dermatologic: Pruritus

Endocrine & metabolic: Hypoglycemia, hyponatremia

Gastrointestinal: Abdominal pain, constipation, anorexia, dyspepsia, increased amylase

Hematologic: Anemia, neutropenia, leukopenia

Hepatic: Elevated liver enzymes

Neuromuscular & skeletal: Weakness

Renal: Elevated BUN/creatinine

Miscellaneous: Oral moniliasis


Drug Interactions

Decreased effect: Rifamycins used concurrently decrease the steady-state plasma concentrations of atovaquone

Note: Possible increased toxicity with other highly protein bound drugs


Stability

Do not freeze


Mechanism of Action

Has not been fully elucidated; may inhibit electron transport in mitochondria inhibiting metabolic enzymes


Pharmacodynamics/Kinetics

Absorption: Decreased significantly in single doses >750 mg; increased threefold when administered with a high-fat meal

Distribution: Enterohepatically recirculated

Protein binding: >99.9%

Bioavailability: ~30%

Half-life: 2.9 days

Elimination: In feces


Usual Dosage

Adults: Oral: 750 mg twice daily with food for 21 days


Dietary Considerations

Administer with a high-fat meal


Mental Health: Effects on Mental Status

May cause anxiety


Mental Health: Effects on Psychiatric Treatment

May cause anemia and neutropenia; use caution with clozapine and carbamazepine


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

Take as directed. Take with high-fat meals. You may experience dizziness or lightheadedness; use caution when driving or engaging in tasks that require alertness until response to drug is known. Small meals may help reduce nausea. Report unresolved diarrhea, fever, mouth sores (use good mouth care), unresolved headache or vomiting. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Consult prescriber if breast-feeding.


Nursing Implications

Notify physician if patient is unable to eat significant amounts of food on an ongoing basis


Dosage Forms

Suspension, oral (citrus flavor): 750 mg/5 mL (210 mL)


References

Artymowicz RJ and James VE, "Atovaquone: A New Antipneumocystis Agent," Clin Pharm, 1993, 12(8):563-70.

El-Sadr WM, Murphy RL, Yurik TM, et al, "Atovaquone Compared With Dapsone for the Prevention of Pneumocystis carinii in Patients With HIV Infection Who Cannot Tolerate Trimethoprim, Sulfonamides, or Both," N Engl J Med, 1998, 339(26):1889-95.

Haile LG and Flaherty JF, "Atovaquone: A Review," Ann Pharmacother, 1993, 27(12):1488-94.

Hughes W, Leoung G, Kramer F, et al, "Comparison of Atovaquone (566C80) With Trimethoprim-Sulfamethoxazole to Treat Pneumocystis carinii Pneumonia in Patients With AIDS," N Engl J Med, 1993, 328(21):1521-7.

Pagano G, Kennedy W, Weller S, et al, "The Safety and Pharmacokinetics of Atovaquone in Immunocompromised Children," Abstracts of the IX International Conference on AIDS in Affiliation With the IV STD World Congress: Berlin, 1993, June 6-11; Abs No PO-B10-1455.

Spencer CM and Goa KL, "Atovaquone. A Review of Its Pharmacological Properties and Therapeutic Efficacy in Opportunistic Infections," Drugs, 1995, 50(1):176-96.


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