|
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. |
|
Copyright © 1978-2000 Lexi-Comp Inc. All Rights Reserved
|