Atovaquone

Do not take it if

Quoted from the official label, section “Contraindications”.

How to take it

These directions are for this exact strength and form. Another one is different.

• Prevention of PCP:
• 1,500 mg (10 mL) once daily with food (2.1) Treatment of PCP:
• 750 mg (5 mL) twice daily with food for 21 days (2.2) Shake gently before use.
• (2.3)
• 2.1 Dosage for the Prevention of P. jirovecii Pneumonia The recommended oral dosage is 1,500 mg (10 mL) once daily administered with food.
• 2.2 Dosage for the Treatment of Mild-to-Moderate P. jirovecii Pneumonia The recommended oral dosage is 750 mg (5 mL) twice daily (total daily dose = 1,500 mg) administered with food for 21 days.
• 2.3 Important Administration Instructions Administer atovaquone oral suspension with food to
• avoid low plasma atovaquone concentrations that may limit response to therapy [see Warnings and Precautions (5.1) , Clinical Pharmacology (12.3) ].
• Atovaquone Oral Suspension Shake gently before administering the recommended dosage.

Quoted from the official label, section “Dosage & Administration”.

Other warnings

Quoted from the official label, section “Warnings”.

Pregnancy and breastfeeding

Quoted from the official label, section “OTC — Pregnancy or Breast Feeding”.

Other medicines

Quoted from the official label, section “Drug Interactions”.

If you take too much

In an emergency, call your local emergency number or a poison control centre.

Quoted from the official label, section “Overdosage”.

Use in children

• Evidence of safety and effectiveness in pediatric patients (aged 12 years and younger) has not been established.
• In a trial of atovaquone oral suspension administered once daily with food for 12 days to 27 HIV-1-infected, asymptomatic infants and children aged between 1 month and 13 years, the pharmacokinetics of atovaquone were age-dependent.
• The average steady-state plasma atovaquone concentrations in the 24 subjects with available concentration data are shown in Table 5.
• Table 5.
• Average Steady-state Plasma Atovaquone Concentrations in Pediatric Subjects Age Dose of Atovaquone Oral Suspension 10 mg/kg 30 mg/kg 45 mg/kg Average C ss in mcg/mL (mean ± SD) 1 to 3 months 5.9 (n = 1) 27.8 ± 5.8 (n = 4) _ >3 to 24 months 5.7 ± 5.1 (n = 4) 9.8 ± 3.2 (n = 4) 15.4 ± 6.6 (n = 4) >2 to 13 years 16.8 ± 6.4 (n = 4) 37.1 ± 10.9 (n = 3) _ C ss = Concentration at steady state.

Quoted from the official label, section “Pediatric Use”.

Use in older people

Clinical trials of atovaquone did not include sufficient numbers of subjects aged 65 years and older to determine whether they respond differently from younger subjects.

Quoted from the official label, section “Geriatric Use”.

Side effects

• The following adverse reaction is discussed in another section of the labeling:
• Hepatotoxicity [see Warnings and Precautions (5.2) ].
• PCP Prevention:
• The most frequent adverse reactions (≥25% that required discontinuation) were diarrhea, rash, headache, nausea, and fever.
• (6.1) PCP Treatment:
• The most frequent adverse reactions (≥14% that required discontinuation) were rash (including maculopapular), nausea, diarrhea, headache, vomiting, and fever.
• (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Hetero Labs Limited at 1-866-495-1995 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
• 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice.
• Additionally, because many subjects who participated in clinical trials with atovaquone had complications of advanced human immunodeficiency virus (HIV) disease, it was often difficult to distinguish adverse reactions caused by atovaquone from those caused by underlying medical conditions.
• PCP Prevention Trials In 2 clinical trials, atovaquone oral suspension was compared with dapsone or aerosolized pentamidine in HIV-1-infected adolescent (13 to 18 years) and adult subjects at risk of PCP (CD4 count <200 cells/mm 3 or a prior episode of PCP) and unable to tolerate TMP-SMX.
• Dapsone Comparative Trial:
• In the dapsone comparative trial (n = 1,057), the majority of subjects were white (64%), male (88%), and receiving prophylaxis for PCP at randomization (73%); the mean age was 38 years.
• Subjects received atovaquone oral suspension 1,500 mg once daily (n = 536) or dapsone 100 mg once daily (n = 521); median durations of exposure were 6.7 and 6.5 months, respectively.
• Adverse reaction data were collected only for adverse reactions requiring discontinuation of treatment, which occurred at similar frequencies in subjects treated with atovaquone oral suspension or dapsone (Table 1).
• Among subjects taking neither dapsone nor atovaquone at enrollment (n = 487), adverse reactions requiring discontinuation of treatment occurred in 43% of subjects treated with dapsone and 20% of subjects treated with atovaquone oral suspension.
• Gastrointestinal adverse reactions (nausea, diarrhea, and vomiting) were more frequently reported in subjects treated with atovaquone oral suspension (Table 1).
• Table 1.
• Percentage (>2%) of Subjects with Selected Adverse Reactions Requiring Discontinuation of Treatment in the Dapsone Comparative PCP Prevention Trial Adverse Reaction All Subjects Atovaquone Oral Suspension 1,500 mg/day (n = 536) % Dapsone 100 mg/day (n = 521) % Rash 6.3
• 8.8 Nausea 4.1
• 0.6 Diarrhea 3.2
• 0.2 Vomiting 2.2
• 0.6 Aerosolized Pentamidine Comparative Trial:
• In the aerosolized pentamidine comparative trial (n = 549), the majority of subjects were white (79%), male (92%), and were primary prophylaxis patients at enrollment (58%); the mean age was 38 years.
• Subjects received atovaquone oral suspension once daily at a dose of 750 mg (n = 188) or 1,500 mg (n = 175) or received aerosolized pentamidine 300 mg every 4 weeks (n = 186); the median durations of exposure were 6.2, 6.0, and 7.8 months, respectively.
• Table 2 summarizes the clinical adverse reactions reported by ≥20% of the subjects receiving either the 1,500-mg dose of atovaquone oral suspension or aerosolized pentamidine.
• Rash occurred more often in subjects treated with atovaquone oral suspension (46%) than in subjects treated with aerosolized pentamidine (28%).
• Treatment-limiting adverse reactions occurred in 25% of subjects treated with atovaquone oral suspension 1,500 mg once daily and in 7% of subjects treated with aerosolized pentamidine.
• The most frequent adverse reactions requiring discontinuation of dosing in the group receiving atovaquone oral suspension 1,500 mg once daily were rash (6%), diarrhea (4%), and nausea (3%).
• The most frequent adverse reaction requiring discontinuation of dosing in the group receiving aerosolized pentamidine was bronchospasm (2%).
• Table 2.
• Percentage (≥20%) of Subjects with Selected Adverse Reactions in the Aerosolized Pentamidine Comparative PCP Prevention Trial Adverse Reaction Atovaquone Oral Suspension 1,500 mg/day (n = 175) % Aerosolized Pentamidine (n = 186) % Diarrhea 42 35 Rash 39 28 Headache 28 22 Nausea 26 23 Fever 25 18 Rhinitis 24 17 Other reactions occurring in ≥10% of subjects receiving the recommended dose of atovaquone oral suspension (1,500 mg once daily) included vomiting, sweating, flu syndrome, sinusitis, pruritus, insomnia, depression, and myalgia.
• PCP Treatment Trials Safety information is presented from 2 clinical efficacy trials of the atovaquone tablet formulation:
• 1) a randomized, double-blind trial comparing atovaquone tablets with TMP-SMX in subjects with acquired immunodeficiency syndrome (AIDS) and mild-to-moderate PCP [(A-a)DO 2 ] ≤45 mm Hg and PaO 2 ≥60 mm Hg on room air; 2) a randomized, open-label trial comparing atovaquone tablets with intravenous (IV) pentamidine isethionate in subjects with mild-to-moderate PCP who could not tolerate trimethoprim or sulfa antimicrobials.
• TMP-SMX Comparative Trial:
• In the TMP-SMX comparative trial (n = 408), the majority of subjects were white (66%) and male (95%); the mean age was 36 years.
• Subjects received atovaquone 750 mg (three 250-mg tablets) 3 times daily for 21 days or TMP 320 mg plus SMX 1,600 mg 3 times daily for 21 days; median durations of exposure were 21 and 15 days, respectively.
• Table 3 summarizes all clinical adverse reactions reported by ≥10% of the trial population regardless of attribution.
• Nine percent of subjects who received atovaquone and 24% of subjects who received TMP-SMX discontinued therapy due to an adverse reaction.
• Among the subjects who discontinued, 4% of subjects receiving atovaquone and 8% of subjects in the TMP-SMX group discontinued therapy due to rash.
• The incidence of adverse reactions with atovaquone oral suspension at the recommended dose (750 mg twice daily) was similar to that seen with the tablet formulation.
• Table 3.
• Percentage (≥10%) of Subjects with Selected Adverse Reactions in the TMP-SMX Comparative PCP Treatment Trial Adverse Reaction Atovaquone Tablets (n = 203) % TMP-SMX (n = 205) % Rash (including maculopapular) 23 34 Nausea 21 44 Diarrhea 19 7 Headache 16 22 Vomiting 14 35 Fever 14 25 Insomnia 10 9 Two percent of subjects treated with atovaquone and 7% of subjects treated with TMP-SMX had therapy prematurely discontinued due to elevations in ALT/AST.
• Pentamidine Comparative Trial:
• In the pentamidine comparative trial (n = 174), the majority of subjects in the primary therapy trial population (n = 145) were white (72%) and male (97%); the mean age was 37 years.
• Subjects received atovaquone 750 mg (three 250-mg tablets) 3 times daily for 21 days or a 3-to 4-mg/kg single pentamidine isethionate IV infusion daily for 21 days; the median durations of exposure were 21 and 14 days, respectively.
• Table 4 summarizes the clinical adverse reactions reported by ≥10% of the primary therapy trial population regardless of attribution.
• Fewer subjects who received atovaquone reported adverse reactions than subjects who received pentamidine (63% vs. 72%).
• However, only 7% of subjects discontinued treatment with atovaquone due to adverse reactions, while 41% of subjects who received pentamidine discontinued treatment for this reason.
• Of the 5 subjects who discontinued therapy with atovaquone, 3 reported rash (4%).
• Rash was not severe in any subject.
• The most frequently cited reasons for discontinuation of pentamidine therapy were hypoglycemia (11%) and vomiting (9%).
• Table 4.
• Percentage (≥10%) of Subjects with Selected Adverse Reactions in the Pentamidine Comparative PCP Treatment Trial (Primary Therapy Group) Adverse Reaction Atovaquone Tablets (n = 73) % Pentamidine (n = 71) % Fever 40 25 Nausea 22 37 Rash 22 13 Diarrhea 21 31 Insomnia 19 14 Headache 18 28 Vomiting 14 17 Cough 14 1 Sweat 10 3 Monilia, oral 10 3 Laboratory abnormality was reported as the reason for discontinuation of treatment in 2 of 73 subjects (3%) who received atovaquone, and in 14 of 71 subjects (20%) who received pentamidine.
• One subject (1%) receiving atovaquone had elevated creatinine and BUN levels and 1 subject (1%) had elevated amylase levels.
• In this trial, elevated levels of amylase occurred in subjects (8% versus 4%) receiving atovaquone tablets or pentamidine, respectively.
• 6.2 Postmarketing Experience The following adverse reactions have been identified during post-approval use of atovaquone oral suspension.
• Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
• Blood and Lymphatic System Disorders Methemoglobinemia, thrombocytopenia.
• Immune System Disorders Hypersensitivity reactions including angioedema, bronchospasm, throat tightness, and urticaria.
• Eye Disorders Vortex keratopathy.
• Gastrointestinal Disorders Pancreatitis.
• Hepatobiliary Disorders Hepatitis, fatal liver failure.
• Skin and Subcutaneous Tissue Disorders Erythema multiforme, Stevens-Johnson syndrome, and skin desquamation.
• Renal and Urinary Disorders Acute renal impairment.

Quoted from the official label, section “Adverse Reactions”.

What to discuss with your doctor

• Administration Instructions Instruct patients to:
• Ensure the prescribed dose of atovaquone oral suspension is taken as directed.
• Take their daily doses of atovaquone oral suspension with food, as food will significantly improve the absorption of the drug.
• Shake atovaquone oral suspension gently before use each time.
• Lactation Instruct mothers with HIV-1 infection not to breastfeed because HIV-1 can be passed to the baby in the breast milk [see Use in Specific Populations (8.2) ] .
• Trademarks are owned or licensed to the GSK group of companies.

Quoted from the official label, section “Patient Counseling Information”.

Strengths and forms

• FORMS AND STRENGTHS Atovaquone oral suspension, USP is a yellow homogenous suspension containing 750 mg of atovaquone USP per 5 mL. Oral suspension:
• 750 mg per 5 mL (3)

Quoted from the official label, section “Dosage Forms & Strengths”.

What it looks like and how it is packed

• Atovaquone oral suspension, USP is a yellow homogenous suspension containing 750 mg atovaquone USP per 5 mL, supplied in:
• 5 mL unit dose cups:
• 20 cups (2 x 10) NDC 60687-534-36 5 mL unit dose cups:
• 42 cups (7 x 6) NDC 60687-534-78
• Store at 15° to 25°C (59° to 77°F).
• Do not freeze .
• DO NOT USE IF SEAL IS BROKEN.

Quoted from the official label, section “How Supplied”.

What is in it

• Atovaquone oral suspension is a quinone antimicrobial drug.
• The chemical name of atovaquone is 1,4-Naphthalenedione, 2-[4-(4-chlorophenyl)cyclohexyl]-3-hydroxy-, trans.
• Atovaquone USP is a yellow colored powder that is freely soluble in tetrahydrofuran, soluble in chloroform and sparingly soluble in acetone.
• It has a molecular weight of 366.84 and the molecular formula C 22 H 19 ClO 3 .
• The compound has the following structural formula:
• Atovaquone oral suspension, USP is a formulation of micro-fine particles of atovaquone USP.
• Each 5 mL of atovaquone oral suspension, USP contains 750 mg of atovaquone USP and the inactive ingredients benzyl alcohol, flavor, hypromellose, poloxamer, purified water, saccharin sodium, and xanthan gum.
• Structural Formula

Quoted from the official label, section “Description”.

Ingredients people check for

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Same active substance, strength and form in other countries

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Details

Source: NDC Directory · 2026-09-13 · not reviewed by a clinician

Source: US Food and Drug Administration, NDC Directory. Reuse terms: US government work (FDA).

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Other strengths and forms

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Same active substance

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