Praziquantel

Keep all appointments with your doctor.

Do not let anyone else take your medication. Your prescription is probably not refillable. If you still have symptoms of infection after you finish the praziquantel, call your doctor.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Less serious side effects may include:

• tired feeling;

• headache, dizziness;

• nausea, upset stomach;

• mild fever; or

• mild skin rash.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Administration

Oral Administration

Administer orally with meals.1

Tablets may be halved or quartered to allow administration of individualized doses.1 Swallow the tablets, halves, and/or quarters with a sufficient amount of water during meals.1

Do not chew tablets.1 Retention of the tablets or tablet segments in the mouth may cause gagging or vomiting as a result of the drug's bitter taste.1

Dosage

Pediatric Patients

Children ≥4 years of age: 20 mg/kg 3 times daily for 1 day; space doses 4–6 hours apart.1

Some clinicians recommend 20 mg/kg twice daily for 1 day for schistosomiasis caused by Schistosoma haematobium or S. mansoni.134 Doses of 40 mg/kg given as a single dose or in 2 equally divided doses have been effective in some patients with schistosomiasis caused by any species.3 6 9 12 14 15 16 17 19 20 128 133

Children ≥4 years of age: 25 mg/kg 3 times daily for 1 day; 1 11 25 26 31 43 44 87 88 90 91 92 94 95 96 102 104 105 128 129 130 134 space doses 4–6 hours apart.1

Alternatively, 40–50 mg/kg given as a single dose has been effective in some patients,31 126 131 132 but may be associated with lower cure rates.31

Children ≥4 years of age: 25 mg/kg 3 times daily for 1 day;1 11 25 26 31 43 44 87 88 90 91 92 94 95 96 102 104 105 128 129 130 134 space doses 4–6 hours apart.1

Alternatively, 40–50 mg/kg given as a single dose has been effective in some patients,31 126 131 132 but may be associated with lower cure rates.31

25 mg/kg 3 times daily for 1 day.11 87 88 134

20 mg/kg 3 times daily for 1 day.134 135 136

25 mg/kg 3 times daily for 2 days.71 134

25 mg/kg 3 times daily for 5–8 days has been used,87 but treatment failures have occurred.88 110 134

5–10 mg/kg as a single dose.134

25 mg/kg as a single dose.55 87 134 Eradication may be difficult; retreatment necessary if infection persists.55

50–100 mg/kg given in 3 divided doses daily for 30 days.134

Adults

20 mg/kg 3 times daily for 1 day; space doses 4–6 hours apart.1

Some clinicians recommend 20 mg/kg twice daily for 1 day for treatment of schistosomiasis caused by Schistosoma haematobium or S. mansoni.134 Doses of 40 mg/kg given as a single dose or in 2 equally divided doses have been effective in some patients with schistosomiasis caused by any species.3 6 9 12 14 15 16 17 19 20 128 133

25 mg/kg 3 times daily for 1 day;1 11 25 26 31 43 44 87 88 90 91 92 94 95 96 102 104 105 128 129 130 134 space doses 4–6 hours apart.1

Alternatively, 40–50 mg/kg given as a single dose has been effective in some patients,31 126 131 132 but may be associated with lower cure rates.31

25 mg/kg 3 times daily for 1 day;1 11 25 26 31 43 44 87 88 90 91 92 94 95 96 102 104 105 128 129 130 134 space doses 4–6 hours apart.1

Alternatively, 40–50 mg/kg given as a single dose has been effective in some patients,31 126 131 132 but may be associated with lower cure rates.31

25 mg/kg 3 times daily for 1 day. 11 87 88 134

20 mg/kg 3 times daily for 1 day.134 135 136

25 mg/kg 3 times daily for 2 days.71 134

25 mg/kg 3 times daily for 5–8 days has been used, but treatment failures have occurred.88 110 134 .87

5–10 mg/kg as a single dose.134

25 mg/kg as a single dose; re-treat if infection persists.55 87 134

50–100 mg/kg given in 3 divided doses daily for 30 days.134

50 mg/kg given in 3 equally divided doses daily for 14–21 days.52 53 72 74 88 113 115 116 121 Concomitant corticosteroids (e.g., dexamethasone 6–24 mg daily, prednisone 30–60 mg daily) often administered to reduce adverse nervous system effects.52 65 73 74 76 121

Consider repeating therapy in patients who show only partial resolution of cysts 3 months after a course or whose condition deteriorates.53 121 123

Special Populations

Hepatic Impairment

Use caution if usual dosage is used in patients with hepatosplenic schistosomiasis if they have moderate to severe liver impairment (Child-Pugh class B and C).1 (See Hepatic Impairment under Cautions.)

Renal Impairment

Dosage adjustments not necessary in patients with renal impairment.1 (See Pharmacokinetics.)

Geriatric Patients

No specific dosage recommendations at this time.1 (See Geriatric Use under Cautions.)

Metabolized by CYP isoenzymes (e.g., CYP3A).d

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

Inhibitors of CYP isoenzymes: May increase plasma concentrations of praziquantel.1

Inducers of CYP isoenzymes: May reduce plasma concentrations of praziquantel.1

Specific Drugs and Food

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For praziquantel, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to praziquantel or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of praziquantel in children. However, safety and efficacy have not been established in children younger than 4 years of age.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of praziquantel in the elderly. However, elderly patients are more likely to have age-related kidney problems, which may require caution and an adjustment in the dose for patients receiving praziquantel.

Pregnancy

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking praziquantel, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using praziquantel with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

• Carbamazepine
• Dexamethasone
• Fosphenytoin
• Phenytoin
• Rifampin

Using praziquantel with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Chloroquine
• Ketoconazole

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of praziquantel. Make sure you tell your doctor if you have any other medical problems, especially:

• Heart disease or
• Heart rhythm problems—Patients with these conditions should be monitored during treatment with praziquantel.

• Kidney disease or
• Liver disease, moderate to severe—Use with caution. The effects may be increased by slower removal of the medicine from the body.

• Seizures, history of or
• Worm cysts in the eye—Should not be used in patients with these conditions.

• Worm cysts in the brain—Your doctor may want you in the hospital to treat this infection.

• It is used to treat infections caused by worms.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Dizziness.
• Headache.
• Upset stomach.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch.

Children ≥4 years and Adolescents: Refer to adult dosing.

Store below 30°C (86°F).

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with cardiac abnormalities.

• Cerebral cysticercosis: It is recommended to hospitalize patients with cerebral cysticercosis for the duration of treatment.

• Hepatic impairment: Use with caution in patients with moderate-to-severe hepatic impairment; reduced liver drug metabolism may result in higher and longer lasting plasma concentrations of unmetabolized praziquantel.

• Schistosomiasis: Praziquantel may not be effective against migrating shistosomulae; observational data indicate that praziquantel treatment in the acute phase of the infection may not prevent progression from asymptomatic to acute shistosomiasis, or from asymptomatic/acute disease to chronic disease. In addition, use in patients with shistosomiasis may be associated with clinical deterioration such as paradoxical reactions or serum sickness Jarisch-Herxheimer-like reactions, which is a sudden inflammatory immune response likely caused by the release of shistosomal antigens. Such reactions typically occur during the acute disease phase, and may lead to life-threatening events such as respiratory failure, encephalopathy, and/or cerebral vasculitis.

• Seizures: Use not recommended in patients with a history of seizures or signs of central nervous system involvement (eg, subcutaneous nodules suggestive of cysticercosis); may exacerbate condition.

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. Therapeutic levels of praziquantel may not be achieved with concurrent administration of strong inducers of cytochrome P450 (eg, rifampin); concurrent use is contraindicated.

Other warnings/precautions:

• Patient information: Patients should be instructed to not drive or operate machinery on the day of treatment and the day after treatment.

Liver function tests; monitor patients with cardiac irregularities during treatment; monitor for seizures; culture urine or feces for ova prior to instituting therapy

75 mg/kg/day orally in 3 divided doses
Duration of therapy: 1 to 2 days

Comments:
-Considered the drug of choice

5 to 10 mg/kg orally once

Comments:
-For the intestinal (adult) stage
-Considered the drug of choice

4 years or older: 5 to 10 mg/kg orally once

Comments:
-For the intestinal (adult) stage
-Considered the drug of choice

Data not available

Praziquantel is a trematodicide provided in tablet form for the oral treatment of schistosome infections and infections due to liver fluke.

Praziquantel is 2-(cyclohexylcarbonyl)-1,2,3,6,7, 11b-hexahydro-4H-pyrazino [2, 1-a] isoquinolin-4-one with the molecular formula; C19H24N2O2. The structural formula is as follows:

Praziquantel is a white to nearly white crystalline powder of bitter taste. The compound is stable under normal conditions and melts at 136°C to 140°C with decomposition. The active substance is hygroscopic. Praziquantel is easily soluble in chloroform and dimethylsulfoxide, soluble in ethanol and very slightly soluble in water.

Praziquantel tablets, USP contain 600 mg of Praziquantel. Inactive ingredients: corn starch, croscarmellose sodium, magnesium stearate, microcrystalline cellulose, povidone, sodium lauryl sulfate, polyethylene glycol, titanium dioxide and hypromellose.

Therapeutically effective levels of Praziquantel may not be achieved when administered concomitantly with strong P450 inducers, such as rifampin (seeCONTRAINDICATIONS).