Anthelmintic

Biltricide

Approved 29 Dec 1982OralTablet

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Indications

Biltricide is indicated in patients aged 1 year and older for the treatment of the following infections:

Schistosomiasis due to all species of schistosoma (for example, Schistosoma mekongi, Schistosoma japonicum, Schistosoma mansoni and Schistosoma hematobium ), and
Clonorchiasis and Opisthorchiasis due to the liver flukes, Clonorchis sinensis/Opisthorchis viverrini (approval of this indication was based on studies in which the two species were not differentiated) Biltricide is an anthelmintic indicated in patients aged one year and older for the treatment of the following infections:
Schistosomiasis due to all species of schistosoma (for example , Schistosoma mekongi , Schistosoma japonicum , Schistosoma mansoni and Schistosoma hematobium ), and,
Clonorchiasis and Opisthorchiasis due to the liver flukes, Clonorchis sinensis and Opisthorchis viverrini

Contraindications

Biltricide is contraindicated in:

Patients who previously have shown hypersensitivity to praziquantel or any of the excipients in Biltricide.
Patients with ocular cysticercosis; since parasite destruction within the eye that occurs because of hypersensitivity reaction to the dead parasite after treatment may cause irreversible lesions, ocular cysticercosis must not be treated with Biltricide.
Patients taking strong Cytochrome P450 3A enzyme (CYP3A) inducers, such as rifampin, [see Warnings and Precautions ( 5.6 ) and Drug Interactions ( 7.1 , 7.2 )] .
Known hypersensitivity to Biltricide or any of its ingredients. ( 4.1 )
Concomitant administration with strong Cytochrome P450 3A enzyme (CYP 3A) inducers such as rifampin. ( 4 , 5.6 7.1)

Warnings and precautions

Clinical Deterioration : Potentially life threatening clinical deterioration can occur in patients treated during the acute phase of schistosomiasis. ( 5.1 )
Central Nervous System (CNS) Effects : Biltricide can exacerbate central nervous system pathology due to schistosomiasis. Consider whether to administer to individuals reporting a history of epilepsy and/or other signs of potential central nervous systems involvement such as subcutaneous nodules suggestive of cysticercosis. ( 5.2)
Potential Lack of Efficacy for Acute Schistosomiasis : This has been reported in observational studies ( 5.3 ).

At a glance

Brand name: Biltricide
Active substance: praziquantel
Pharmacologic class: Anthelmintic
Route: Oral
Dosage form: Tablet
Applicant: Bayer Hlthcare
Status: Discontinued
FDA approval: 29 Dec 1982
Application: NDA018714-001

Indications

Biltricide is indicated in patients aged 1 year and older for the treatment of the following infections:

Schistosomiasis due to all species of schistosoma (for example, Schistosoma mekongi, Schistosoma japonicum, Schistosoma mansoni and Schistosoma hematobium ), and
Clonorchiasis and Opisthorchiasis due to the liver flukes, Clonorchis sinensis/Opisthorchis viverrini (approval of this indication was based on studies in which the two species were not differentiated) Biltricide is an anthelmintic indicated in patients aged one year and older for the treatment of the following infections:
Schistosomiasis due to all species of schistosoma (for example , Schistosoma mekongi , Schistosoma japonicum , Schistosoma mansoni and Schistosoma hematobium ), and,
Clonorchiasis and Opisthorchiasis due to the liver flukes, Clonorchis sinensis and Opisthorchis viverrini

Contraindications

Biltricide is contraindicated in:

Patients who previously have shown hypersensitivity to praziquantel or any of the excipients in Biltricide.
Patients with ocular cysticercosis; since parasite destruction within the eye that occurs because of hypersensitivity reaction to the dead parasite after treatment may cause irreversible lesions, ocular cysticercosis must not be treated with Biltricide.
Patients taking strong Cytochrome P450 3A enzyme (CYP3A) inducers, such as rifampin, [see Warnings and Precautions ( 5.6 ) and Drug Interactions ( 7.1 , 7.2 )] .
Known hypersensitivity to Biltricide or any of its ingredients. ( 4.1 )
Concomitant administration with strong Cytochrome P450 3A enzyme (CYP 3A) inducers such as rifampin. ( 4 , 5.6 7.1)

Warnings and precautions

Clinical Deterioration : Potentially life threatening clinical deterioration can occur in patients treated during the acute phase of schistosomiasis. ( 5.1 )
Central Nervous System (CNS) Effects : Biltricide can exacerbate central nervous system pathology due to schistosomiasis. Consider whether to administer to individuals reporting a history of epilepsy and/or other signs of potential central nervous systems involvement such as subcutaneous nodules suggestive of cysticercosis. ( 5.2)
Potential Lack of Efficacy for Acute Schistosomiasis : This has been reported in observational studies ( 5.3 ).

Pregnancy and breastfeeding

8.1Pregnancy Risk Summary

Published studies have not identified an association with Biltricide use during pregnancy and major birth defects, miscarriage or adverse maternal or fetal outcomes (see Data) . In animal reproduction studies conducted in pregnant rats and rabbits no adverse developmental outcomes were observed with oral administration of praziquantel during organogenesis at approximately 0.65 times (rats) or 1.3 times (rabbits) the highest recommended human daily dose of 75 mg/kg/day, based on body surface area.

The estimated background risk of major birth defects and miscarriage for the indicated population are unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Human Data Two randomized controlled clinical trials have been conducted using praziquantel for the treatment of schistosoma infection in pregnant women.

In one randomized controlled trial in pregnant women with schistosoma ( S. japonicum) infection, 186 pregnant women were treated with praziquantel compared to 184 women who received placebo. Treatment with praziquantel during pregnancy had no effect on birthweight, and there were no differences in rates of miscarriage, fetal death and major birth defects between the praziquantel-treated and control patients. In another randomized controlled trial that included 2507 pregnant women in Uganda, 18% of women were infected with schistosoma infection.

Treatment with praziquantel during pregnancy had no effect on mean birth weight, perinatal mortality or major birth defects. In other published studies, including a retrospective observational study, case series and case reports, there have been no reports of major birth defects, stillbirths or other adverse pregnancy outcomes associated with the use of praziquantel during pregnancy. Animal Data No evidence of fetal harm was observed in rats and rabbits at praziquantel dose levels of 30 to 300 mg/kg body weight given repeatedly by oral administration during the period of organogenesis.

These doses were up to 0.65 times (rats) or 1.3 times (rabbits) the highest recommended human daily dose of 75 mg/kg/day, based on body surface area.

8.2Lactation Risk Summary

Limited data from published literature reports the presence of praziquantel in human milk at low concentrations. There is no information on the effects of praziquantel in the breastfed infant or effects on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for Biltricide and any potential adverse effects on the breastfed infant from Biltricide or from the underlying maternal condition.

8.4Pediatric Use Safety

and dosing recommendations of Biltricide in pediatric patients 1 to 17 years have been established. Safety of Biltricide in pediatric patients younger than 1 year of age has not been established. Post-marketing experience and published literature indicates that pediatric patients 1 to 17 years of age treated with praziquantel experience similar adverse reactions as adults treated with praziquantel [see Adverse Reactions ( 6 )] .

8.5Geriatric Use

Clinical studies of Biltricide did not include a sufficient number of subjects ages 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older patients cannot be ruled out. This drug is known to be substantially excreted by the kidney. Because elderly patients are more likely to have decreased renal function, the risk of toxic reactions to this drug may be greater in these patients [see Clinical Pharmacology ( 12.3 )].

8.6Hepatic Impairment

Following oral administration of Biltricide to patients with liver impairment, reduced hepatic metabolism of praziquantel results in higher and sustained plasma concentrations of unmetabolized praziquantel [see Clinical Pharmacology ( 12.3 )]. Monitor patients for adverse reactions when administering the recommended dose of Biltricide to hepatosplenic schistosomiasis patients with moderate or severe liver impairment (Child-Pugh Class B or C).

8.7Renal Impairment

No dosage adjustment of Biltricide is necessary in patients with renal impairment. Nephrotoxic effects of Biltricide or its metabolites are not known [see Clinical Pharmacology ( 12.3 )] .

Adverse reactions

The following serious or otherwise important adverse reactions are discussed elsewhere in the labeling:

Clinical Deterioration [see Warnings and Precautions ( 5.1 )]
Central Nervous System (CNS) Effects [see Warnings and Precautions ( 5.2 )]
Potential Lack of Efficacy During the Acute Phase of Schistosomiasis [see Warnings and Precautions ( 5.3 )]
Cardiac Arrhythmias [see Warnings and Precautions ( 5.4 )]
Hepatic Impairment in Hepatosplenic Schistosomiasis Patients [see Warnings and Precautions ( 5.5 )]
Concomitant Administration with Strong Cytochrome P450 Inducers [see Warnings and Precautions ( 5.6 )] The following adverse reactions associated with the use of Biltricide were identified in clinical studies, published literature or postmarketing reports. Because some of these reactions were 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. The following adverse reactions were observed in both adults and pediatric patients: General disorders and administration site conditions: malaise, pyrexia Nervous system disorders: headache , dizziness Gastrointestinal disorders: abdominal discomfort, nausea Skin and subcutaneous tissue disorders: urticaria Such adverse reactions may be more frequent and/or serious in patients with a heavy worm burden. Additional adverse reactions reported from worldwide post marketing experience and from publications with Biltricide and various formulations of praziquantel include: Blood and lymphatic system disorders: eosinophilia Cardiac disorders: arrhythmia (including bradycardia, ectopic rhythms, ventricular fibrillation, AV blocks) Ear and labyrinth disorders: vertigo, tinnitus Eye disorders: visual disturbance Gastrointestinal disorders: abdominal pain, bloody diarrhea, vomiting General disorders and administration site conditions: polyserositis, asthenia, fatigue, gait disturbance Hepatobiliary disorders: hepatitis Immune system disorders: allergic reaction, generalized hypersensitivity, anaphylactic reaction Metabolism and nutrition disorders: anorexia Musculoskeletal and connective tissue disorders: myalgia Nervous system disorders: convulsion, somnolence, intention tremor Respiratory, thoracic and mediastinal disorders: pneumonitis, dyspnea, wheezing Skin and subcutaneous tissue disorders: pruritus, rash, Stevens-Johnson syndrome Pediatric patients 1 to 17 years of age treated with Biltricide and various formulations of praziquantel experienced similar adverse reactions as those observed in adult patients. The adverse reactions reported were malaise, headache, dizziness, abdominal discomfort (with or without nausea), pyrexia and urticaria. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Bayer HealthCare Pharmaceuticals Inc. at 1-888-842-2937 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Biltricide

Indications

Contraindications

Warnings and precautions

At a glance

Two medicines in one question?

Biltricide

Indications

Contraindications

Warnings and precautions

At a glance

Two medicines in one question?

5.1Clinical Deterioration

5.2Central Nervous System (CNS) Effects

5.3Potential Lack of Efficacy During the Acute Phase of Schistosomiasis Data

5.4Cardiac Arrhythmias

5.5Hepatic Impairment in Hepatosplenic Schistosomiasis Patients

Interactions

7.1CYP 3A Inducers Strong and Moderate CYP 3A Inducers

Pregnancy and breastfeeding

8.1Pregnancy Risk Summary

8.2Lactation Risk Summary

8.4Pediatric Use Safety

8.5Geriatric Use

8.6Hepatic Impairment

8.7Renal Impairment

Adverse reactions

Composition

Official product information