Praziquantel
JFDA label: Epiquantel 600mg Tab
Mechanism of Action
Blocker of Voltage-activated calcium channel beta 1 subunit — Voltage-activated calcium channel beta 1 subunit blocker; Blocker of Voltage-activated calcium channel beta 2 subunit — Voltage-activated calcium channel beta 2 subunit blocker
| Target | Action | Gene / class |
|---|---|---|
| Voltage-activated calcium channel beta 1 subunit efficacy | BLOCKER | |
| Voltage-activated calcium channel beta 2 subunit efficacy | BLOCKER |
Indications
Approved
- Helminths
Off-label
- Cysticercosis
- Tapeworms
Antimicrobial Spectrum
Expected / intrinsic spectrum (EUCAST breakpoints & labels) — not local resistance. Source: openfda-label.
Helminths
| Organism | Activity | MIC |
|---|---|---|
| Schistosoma hematobium | Active | — |
| Schistosoma japonicum | Active | — |
| Schistosoma mansoni | Active | — |
| Schistosoma mekongi | Active | — |
Contraindications
Source: Lexicomp
- Hypersensitivity to praziquantel or any component of the formulation Absolute
- concomitant administration with strong cytochrome P450 (CYP450) inducers, such as rifampin Absolute
- ocular cysticercosis Absolute
Adverse Reactions
Nervous system disorders (3)
Not Known Dizziness · headache · malaise
Gastrointestinal disorders (2)
Not Known Abdominal distress · nausea
Skin and subcutaneous tissue disorders (1)
Not Known Urticaria
General disorders and administration site conditions (1)
Not Known Fever
Dosing
Source: Lexicomp
Warnings & Precautions
Source: Lexicomp
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.
Pregnancy & Lactation
Pregnancy
Adverse effects have not been observed in animal reproduction studies. Use in pregnant women only if clearly needed.
Lactation
Appears in breast milk at a concentration of ¼ that of maternal serum. Women should be advised to not breast-feed on the day of treatment and for 72 hours after treatment.
Monitoring
| Clinical pearl | Liver function tests; monitor patients with cardiac irregularities during treatment; monitor for seizures; culture urine or feces for ova prior to instituting therapy |
|---|
Chemistry & Properties
| Formula | C19H24N2O2 |
|---|---|
| Molecular weight | 312.41 g/mol |
| IUPAC name | 2-(cyclohexanecarbonyl)-3,6,7,11b-tetrahydro-1H-pyrazino[2,1-a]isoquinolin-4-one |
| CAS | 55268-74-1 |
| PubChem CID | 4891 |
| InChIKey | FSVJFNAIGNNGKK-UHFFFAOYSA-N |
| logP | 2.53 (XLogP 2.7) |
| Polar surface area | 40.62 Ų |
| H-bond acceptors / donors | 2 / 0 |
| Drug-likeness (QED) | 0.80 |
| Lipinski violations | 0 |
SMILES
O=C(C1CCCCC1)N1CC(=O)N2CCc3ccccc3C2C1Biology & Pharmacokinetics
Pharmacokinetics predicted
| Bioavailability | 70.0% |
|---|---|
| Half-life | 1.404 h |
| Volume of distribution | 0.734 L/kg |
| Protein binding | 81.1% |
| BBB penetrant | Yes |
Enzyme interactions
| Enzyme | Role | Detail |
|---|---|---|
| CYP1A2 | Inhibitor | — |
| CYP1A2 | Substrate | — |
| CYP2B6 | Inhibitor | — |
| CYP2C19 | Inhibitor | — |
| CYP2C19 | Substrate | — |
| CYP2C9 | Inhibitor | — |
| CYP2C9 | Substrate | — |
| CYP2D6 | Substrate | — |
| CYP3A4 | Substrate | — |
Transporters
BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP4 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)
Drug–drug interactions (83, DDInter)
| Interacting drug | Severity | Management |
|---|---|---|
| Apalutamide | major | |
| Carbamazepine | major | |
| Enzalutamide | major | |
| Fosphenytoin | major | |
| Lumacaftor | major | |
| Mitotane | major | |
| Phenobarbital | major | |
| Phenytoin | major | |
| Primidone | major | |
| Rifabutin | major | |
| Rifampicin | major | |
| Rifapentine | major | |
| St. John's Wort | major | |
| Abametapir (topical) | moderate | |
| Aminoglutethimide | moderate | |
| Amobarbital | moderate | |
| Armodafinil | moderate | |
| Bexarotene | moderate | |
| Bosentan | moderate | |
| Brigatinib | moderate | |
| Butabarbital | moderate | |
| Butalbital | moderate | |
| Cenobamate | moderate | |
| Chloroquine | moderate | |
| Dabrafenib | moderate | |
| Darunavir | moderate | |
| Deferasirox | moderate | |
| Dexamethasone | moderate | |
| Doravirine | moderate | |
| Duvelisib | moderate | |
| Echinacea | moderate | |
| Efavirenz | moderate | |
| Elagolix | moderate | |
| Eslicarbazepine | moderate | |
| Etravirine | moderate | |
| Fedratinib | moderate | |
| Felbamate | moderate | |
| Fosnetupitant | moderate | |
| Fostamatinib | moderate | |
| Glycerol phenylbutyrate | moderate |
Showing 40 of 83.
Registered Products (1)
| Brand | Form / strength | Pack | Agent | Citizen (JOD) |
|---|---|---|---|---|
| Epiquantel | Tablet 600 mg | 4 tab | AL-Faiasel Drug Store | 3.400 |