Atovaquone 750mg/5ml Suspension
It is used to treat or prevent infections caused by Pneumocystis jirovecii.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Antiprotozoal, Antimalarial
Pharmacologic Class
Naphthoquinone
Pregnancy Category
Category C
FDA Approved
Nov 1992
DEA Schedule
Not Controlled
Overview
What is this medicine?
Atovaquone is an anti-infective medicine used to treat or prevent a type of pneumonia called PCP (Pneumocystis pneumonia), which often affects people with weakened immune systems. It works by stopping the growth of the germs that cause the infection. It is very important to take this medicine with food to help your body absorb it properly.
How to Use This Medicine
Taking Your Medication Correctly
To ensure you get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your medication and follow the instructions closely.
Administration Instructions
Shake the medication well before use.
Take your medication with food to help your body absorb it properly. If you have trouble taking it with food, consult your doctor for guidance.
Continue taking your medication as directed by your doctor or healthcare provider, even if you start feeling well.
Unit-Dose Instructions
Open the pouch and take the contents by mouth.
You can place the contents directly into your mouth, or use a dosing spoon or cup to make it easier.
Bottle Instructions
Measure liquid doses carefully using the measuring device provided with the medication.
If a measuring device is not included, ask your pharmacist for one to ensure accurate dosing.
Storage and Disposal
Store your medication at room temperature, away from freezing temperatures.
Keep it in a dry place, avoiding storage in a bathroom.
Store all medications in a safe location, out of the reach of children and pets.
Missed Dose Instructions
If you miss a dose, take it as soon as you remember, with food.
If it's close to the time for your next dose, skip the missed dose and return to your regular schedule.
* Do not take two doses at the same time or take extra doses to make up for a missed one.
To ensure you get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your medication and follow the instructions closely.
Administration Instructions
Shake the medication well before use.
Take your medication with food to help your body absorb it properly. If you have trouble taking it with food, consult your doctor for guidance.
Continue taking your medication as directed by your doctor or healthcare provider, even if you start feeling well.
Unit-Dose Instructions
Open the pouch and take the contents by mouth.
You can place the contents directly into your mouth, or use a dosing spoon or cup to make it easier.
Bottle Instructions
Measure liquid doses carefully using the measuring device provided with the medication.
If a measuring device is not included, ask your pharmacist for one to ensure accurate dosing.
Storage and Disposal
Store your medication at room temperature, away from freezing temperatures.
Keep it in a dry place, avoiding storage in a bathroom.
Store all medications in a safe location, out of the reach of children and pets.
Missed Dose Instructions
If you miss a dose, take it as soon as you remember, with food.
If it's close to the time for your next dose, skip the missed dose and return to your regular schedule.
* Do not take two doses at the same time or take extra doses to make up for a missed one.
Lifestyle & Tips
- Always take Atovaquone suspension with food, preferably a fatty meal (e.g., milk, peanut butter, cheese, or a high-fat supplement) to ensure proper absorption. If you cannot eat, try to take it with a nutritional supplement.
- Shake the bottle well before each use.
- Use the provided measuring spoon or cup to ensure an accurate dose.
- Do not miss doses. If you miss a dose, take it as soon as you remember with food. If it's almost time for your next dose, skip the missed dose and continue your regular schedule. Do not take two doses at once.
- Complete the full course of treatment, even if you start feeling better, to prevent the infection from returning.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Pneumocystis Pneumonia (PCP) Treatment: 750 mg (10 mL) orally twice daily with food for 21 days. PCP Prophylaxis: 1500 mg (20 mL) orally once daily with food.
Dose Range:
750 - 1500 mg
Condition-Specific Dosing:
PCP Treatment:
750 mg BID with food for 21 days
PCP Prophylaxis:
1500 mg QD with food
Pediatric Dosing
Neonatal:
Not established (safety and efficacy not established in infants <1 month of age)
Infant:
PCP Treatment (1-12 months): 30 mg/kg/day divided BID with food for 21 days (max 750 mg/dose). PCP Prophylaxis (1-12 months): 15 mg/kg/day once daily with food (max 1500 mg/day).
Child:
PCP Treatment (1-16 years): 30 mg/kg/day divided BID with food for 21 days (max 750 mg/dose). PCP Prophylaxis (1-16 years): 15 mg/kg/day once daily with food (max 1500 mg/day).
Adolescent:
PCP Treatment (13-16 years): 30 mg/kg/day divided BID with food for 21 days (max 750 mg/dose). PCP Prophylaxis (13-16 years): 15 mg/kg/day once daily with food (max 1500 mg/day). For adolescents >16 years, adult dosing applies.
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No adjustment needed
Dialysis:
Not significantly removed by dialysis; no specific recommendations, but monitor clinical response.
Hepatic Impairment:
Mild:
No specific adjustment needed
Moderate:
No specific adjustment needed
Severe:
Use with caution; no specific dose adjustment recommendations available, but monitor for increased adverse effects due to potential for higher drug exposure.
Pharmacology
Mechanism of Action
Atovaquone is a naphthoquinone antimicrobial agent that inhibits the mitochondrial electron transport chain in susceptible organisms, including *Pneumocystis jirovecii* and *Plasmodium falciparum*. It selectively inhibits dihydroorotate dehydrogenase, an enzyme essential for pyrimidine synthesis, thereby disrupting nucleic acid and ATP synthesis.
Pharmacokinetics
Absorption:
Bioavailability:
23% (increased significantly with food)
Tmax:
1-8 hours
FoodEffect:
Absorption is significantly increased (2-3 fold) when taken with a fatty meal. Taking with food is critical for optimal absorption.
Distribution:
Vd:
0.6 L/kg
ProteinBinding:
>99.9% (primarily to albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
62-77 hours (2-3 days)
Clearance:
Not available (primarily eliminated unchanged)
ExcretionRoute:
Primarily fecal (>94% as unchanged drug)
Unchanged:
>94%
Pharmacodynamics
OnsetOfAction:
Not precisely defined for clinical effect; therapeutic levels achieved within hours of first dose with food.
PeakEffect:
Not precisely defined for clinical effect.
DurationOfAction:
Due to long half-life, sustained levels are maintained with daily or twice-daily dosing.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Depression
Fever
White patches in the mouth
Cough
Liver problems, which can be rare but potentially deadly. Be aware of signs such as:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
Headache
Diarrhea
Upset stomach or vomiting
Muscle pain
Trouble sleeping
Excessive sweating
Runny or stuffy nose
Flu-like symptoms
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Depression
Fever
White patches in the mouth
Cough
Liver problems, which can be rare but potentially deadly. Be aware of signs such as:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
Headache
Diarrhea
Upset stomach or vomiting
Muscle pain
Trouble sleeping
Excessive sweating
Runny or stuffy nose
Flu-like symptoms
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe allergic reaction (rash, hives, itching, difficulty breathing, swelling of face/lips/tongue/throat)
- Severe skin reactions (e.g., Stevens-Johnson syndrome, toxic epidermal necrolysis) - look for widespread rash, blistering, peeling skin, fever, flu-like symptoms
- Persistent or severe nausea, vomiting, or diarrhea (especially if it prevents you from taking the medication with food)
- Unusual bleeding or bruising (if taking warfarin concurrently)
- Signs of liver problems (yellowing of skin or eyes, dark urine, severe stomach pain, unusual tiredness)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you are currently taking rifabutin or rifampin, as these medications may interact with this drug.
This list is not exhaustive, and it is crucial to disclose all your medications, including:
Prescription and over-the-counter (OTC) drugs
Natural products
* Vitamins
Additionally, share any existing health problems with your doctor. This information will help your doctor determine if it is safe for you to take this medication in conjunction with your other medications and health conditions.
Remember, do not start, stop, or modify the dosage of any medication without first consulting your doctor to ensure your safety.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you are currently taking rifabutin or rifampin, as these medications may interact with this drug.
This list is not exhaustive, and it is crucial to disclose all your medications, including:
Prescription and over-the-counter (OTC) drugs
Natural products
* Vitamins
Additionally, share any existing health problems with your doctor. This information will help your doctor determine if it is safe for you to take this medication in conjunction with your other medications and health conditions.
Remember, do not start, stop, or modify the dosage of any medication without first consulting your doctor to ensure your safety.
Precautions & Cautions
It is essential to inform all of your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. If you are pregnant, planning to become pregnant, or are breast-feeding, be sure to discuss this with your doctor. You and your doctor will need to carefully weigh the benefits and risks of using this medication to ensure the best possible outcome for both you and your baby.
Overdose Information
Overdose Symptoms:
- Exaggerated side effects such as severe nausea, vomiting, diarrhea, rash, or headache.
What to Do:
There is no specific antidote for atovaquone overdose. Treatment should be supportive and symptomatic. Contact a poison control center immediately or seek emergency medical attention. Call 1-800-222-1222.
Drug Interactions
Major Interactions
- Rifampin
- Rifabutin
Moderate Interactions
- Tetracycline
- Metoclopramide
- Warfarin
- Indinavir
- Efavirenz
Monitoring
Baseline Monitoring
Baseline liver function tests (LFTs)
Rationale: To assess hepatic function, especially in patients with pre-existing hepatic impairment, as atovaquone is primarily eliminated unchanged via bile.
Timing: Prior to initiation of therapy
Renal function (SCr, BUN)
Rationale: Although not renally cleared, to establish baseline for overall patient assessment.
Timing: Prior to initiation of therapy
Routine Monitoring
Clinical response to therapy
Frequency: Daily during acute treatment, periodically during prophylaxis
Target: Resolution of symptoms (e.g., fever, cough, dyspnea for PCP)
Action Threshold: Lack of improvement or worsening symptoms may indicate treatment failure or need for alternative therapy.
Adverse effects monitoring (e.g., rash, GI upset, headache, fever)
Frequency: Daily during acute treatment, periodically during prophylaxis
Target: Absence or mild, tolerable side effects
Action Threshold: Severe or persistent adverse effects may require dose reduction or discontinuation.
INR (if on warfarin)
Frequency: More frequently upon initiation and discontinuation of atovaquone, and with dose changes
Target: Therapeutic range for warfarin
Action Threshold: INR outside target range requires warfarin dose adjustment.
Symptom Monitoring
- Rash
- Nausea
- Vomiting
- Diarrhea
- Abdominal pain
- Headache
- Fever
- Insomnia
- Cough
- Dyspnea
- Fatigue
- Changes in vision (rare)
Special Patient Groups
Pregnancy
Atovaquone is classified as Pregnancy Category C. Studies in animals have shown adverse effects on the fetus, but there are no adequate and well-controlled studies in pregnant women. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Limited human data; animal studies show developmental toxicity at high doses.
Second Trimester:
Limited human data; use only if clearly needed.
Third Trimester:
Limited human data; use only if clearly needed.
Lactation
Atovaquone is excreted into breast milk in animals. It is unknown whether atovaquone is excreted in human milk. Due to the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
Risk to infant is unknown but potential for adverse effects exists. Monitor for gastrointestinal upset (diarrhea, vomiting) or rash in the infant.
Pediatric Use
Safety and efficacy have been established for the treatment and prophylaxis of PCP in children aged 1 month to 16 years. Dosing is weight-based. Not recommended for infants younger than 1 month.
Geriatric Use
Clinical studies of atovaquone did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Clinical Information
Clinical Pearls
- Atovaquone suspension MUST be taken with food, especially a fatty meal, to maximize absorption and achieve therapeutic drug levels. Failure to do so can lead to sub-therapeutic levels and treatment failure.
- Shake the suspension bottle well before each dose to ensure uniform distribution of the active ingredient.
- This formulation (750mg/5ml suspension) is primarily used for PCP treatment and prophylaxis. For malaria, a fixed-dose combination with proguanil (Malarone) is typically used.
- Patients who experience significant nausea, vomiting, or diarrhea may have reduced absorption of atovaquone, potentially leading to treatment failure. Monitor these patients closely and consider alternative therapies if absorption is compromised.
- Atovaquone has a long half-life, allowing for once or twice daily dosing, but also means it takes several days to reach steady-state concentrations.
Alternative Therapies
- For PCP Treatment: Trimethoprim/sulfamethoxazole (TMP/SMX), Pentamidine, Clindamycin + Primaquine, Dapsone + Trimethoprim.
- For PCP Prophylaxis: Trimethoprim/sulfamethoxazole (TMP/SMX), Dapsone, Pentamidine (aerosolized).
- For Malaria (uncomplicated P. falciparum, if Atovaquone/Proguanil is not used): Artemisinin-based combination therapies (ACTs), Chloroquine (if susceptible), Mefloquine, Quinine.
Cost & Coverage
Average Cost:
Varies widely, typically $500-$1500 per 210 mL bottle (750mg/5mL)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (for generic), Tier 3 or 4 (for brand)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to help healthcare professionals provide the best possible care.