Ethotoin (Peganone) is an antiepileptic drug that belongs to the class of drugs called hydantoins (like phenytoin). It is used in the treatment of patients with seizures.
Ethotoin (Peganone) Uses:
-
Seizures:
- It is used in the management of generalized tonic-clonic or grand mal and complex-partial or psychomotor seizures.
Ethotoin (Peganone) Dose in Adults
Ethotoin (Peganone) Dose for Seizures:
- Oral: Initial:
- ≤1 g/day, in four or six divided doses;
- The dose may be increased over a period of several days to the usual maintenance dose of 2 to 3 g/day.
Ethotoin (Peganone) Dose in Children
Ethotoin (Peganone) for Seizures:
-
Children ≥1 year and Adolescents:
- Oral: Initial:
- ≤750 mg/day, in four or six divided doses;
- The usual maintenance dose is 0.5 to 1 g/day
- The maximum daily dose is 3 g/day.
- Oral: Initial:
Pregnancy Risk Category: D
- After maternal drug use, adverse drug reactions may occur in the fetus.
- Consuming antiepileptic drugs may lead to neonatal bleeding defects or bleeding within 24 hours after birth.
- Other hydantoins have been used in conjunction with in utero exposure to ethotoin.
Use of Ethotoin while breastfeeding
- Breast milk contains the drug.
- The manufacturer suggests that you stop breastfeeding because of possible adverse reactions in your infant.
Ethotoin (Peganone) Dose in Kidney Disease:
No dosage adjustment has been provided in the manufacturer’s labeling.
Ethotoin (Peganone) Dose in Liver disease:
It is contraindicated in patients with liver disease.
Side effects of Ethotoin (Peganone):
-
Cardiovascular:
- Chest Pain
-
Central Nervous System:
- Ataxia
- Dizziness
- Fatigue
- Headache
- Insomnia
- Numbness
-
Dermatologic:
- Skin Rash
- Stevens-Johnson Syndrome
-
Gastrointestinal:
- Diarrhea
- Gingival Hyperplasia
- Nausea
- Vomiting
-
Hematologic & Oncologic:
- Hematologic Disease
- Lymphadenopathy
-
Neuromuscular & Skeletal:
- Lupus-Like Syndrome
-
Ophthalmic:
- Diplopia
- Nystagmus
-
Miscellaneous:
- Fever
Contraindications to Ethotoin (Peganone):
- Hepatic impairment
- Blood disorders
- Hypersensitivity reactions to any component of the drug or the drug itself.
Warnings and precautions
-
Blood dyscrasias
- It is possible for patients to develop blood dyscrasias and cytopenias after the drug's use.
- Patients who have an underlying hematological condition or suffer from cytopenias may be at greater risk.
- Patients should be monitored for blood-related side effects. Patients might be warned to report fever, sore throats, infections, easybruising, and skin rash (petechiae, purpuric)
- If the patient develops cytopenias, treatment can be stopped.
- Megaloblastic anemia is also possible in individuals who have impaired folic acid metabolism due to the drug.
- Patients with preexisting hematological conditions such as severe anemia and cytopenia should avoid it.
-
Suicidal thoughts:
- Antiepileptics have been shown to increase suicidal thoughts/ideas and suicidal behavior.
- Suicidal ideation can be detected as soon as treatment begins. It is also possible during drug intake.
- Patients must be closely monitored for any changes in behavior, especially if they are displaying suicidal thoughts.
- These patients should be immediately reported to their healthcare providers.
Ethotoin: Drug Interaction
Note: Drug Interaction Categories:
- Risk Factor C: Monitor When Using Combination
- Risk Factor D: Consider Treatment Modification
- Risk Factor X: Avoid Concomitant Use
Risk Factor C (Monitor therapy) |
|
| Alcohol (Ethyl) | CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). |
| Alizapride | May enhance the CNS depressant effect of CNS Depressants. |
| Brexanolone | CNS Depressants may enhance the CNS depressant effect of Brexanolone. |
| Brimonidine (Topical) | May enhance the CNS depressant effect of CNS Depressants. |
| Bromopride | May enhance the CNS depressant effect of CNS Depressants. |
| Cannabidiol | May enhance the CNS depressant effect of CNS Depressants. |
| Cannabis | May enhance the CNS depressant effect of CNS Depressants. |
| Chlorphenesin Carbamate | May enhance the adverse/toxic effect of CNS Depressants. |
| CNS Depressants | May enhance the adverse/toxic effect of other CNS Depressants. |
| Dimethindene (Topical) | May enhance the CNS depressant effect of CNS Depressants. |
| Doxylamine | May enhance the CNS depressant effect of CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended. |
| Dronabinol | May enhance the CNS depressant effect of CNS Depressants. |
| Esketamine | May enhance the CNS depressant effect of CNS Depressants. |
| HydrOXYzine | May enhance the CNS depressant effect of CNS Depressants. |
| Kava Kava | May enhance the adverse/toxic effect of CNS Depressants. |
| Lofexidine | May enhance the CNS depressant effect of CNS Depressants. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
| Magnesium Sulfate | May enhance the CNS depressant effect of CNS Depressants. |
| MetyroSINE | CNS Depressants may enhance the sedative effect of MetyroSINE. |
| Mianserin | May diminish the therapeutic effect of Anticonvulsants. |
| Minocycline | May enhance the CNS depressant effect of CNS Depressants. |
| Mirtazapine | CNS Depressants may enhance the CNS depressant effect of Mirtazapine. |
| Nabilone | May enhance the CNS depressant effect of CNS Depressants. |
| Orlistat | May decrease the serum concentration of Anticonvulsants. |
| Piribedil | CNS Depressants may enhance the CNS depressant effect of Piribedil. |
| Pramipexole | CNS Depressants may enhance the sedative effect of Pramipexole. |
| ROPINIRole | CNS Depressants may enhance the sedative effect of ROPINIRole. |
| Rotigotine | CNS Depressants may enhance the sedative effect of Rotigotine. |
| Rufinamide | May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. |
| Selective Serotonin Reuptake Inhibitors | CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. |
| Tetrahydrocannabinol | May enhance the CNS depressant effect of CNS Depressants. |
| Tetrahydrocannabinol and Cannabidiol | May enhance the CNS depressant effect of CNS Depressants. |
| Trimeprazine | May enhance the CNS depressant effect of CNS Depressants. |
Risk Factor D (Consider therapy modification) |
|
| Blonanserin | CNS Depressants may enhance the CNS depressant effect of Blonanserin. |
| Buprenorphine | CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine patches (Butrans brand) at 5 mcg/hr in adults when used with other CNS depressants. |
| Chlormethiazole | May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. |
| Droperidol | May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
| Flunitrazepam | CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. |
| HYDROcodone | CNS Depressants may enhance the CNS depressant effect of HYDROcodone. Management: Avoid concomitant use of hydrocodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. |
| Mefloquine | May diminish the therapeutic effect of Anticonvulsants. Mefloquine may decrease the serum concentration of Anticonvulsants. Management: Mefloquine is contraindicated for malaria prophylaxis in persons with a history of convulsions. Monitor anticonvulsant concentrations and treatment response closely with concurrent use. |
| Methotrimeprazine | CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. |
| Opioid Agonists | CNS Depressants may enhance the CNS depressant effect of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. |
| OxyCODONE | CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. |
| Perampanel | May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. |
| Sodium Oxybate | May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to combined use. When combined use is needed, consider minimizing doses of one or more drugs. Use of sodium oxybate with alcohol or sedative hypnotics is contraindicated. |
| Suvorexant | CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. |
| Tapentadol | May enhance the CNS depressant effect of CNS Depressants. Management: Avoid concomitant use of tapentadol and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. |
| Vitamin K Antagonists (eg, warfarin) | Ethotoin may enhance the anticoagulant effect of Vitamin K Antagonists. Vitamin K Antagonists may increase the serum concentration of Ethotoin. Management: Anticoagulant dose adjustment will likely be necessary when ethotoin is initiated or discontinued. Monitor patients extra closely (INR and signs/symptoms of bleeding) when using this combination. |
| Zolpidem | CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. |
Risk Factor X (Avoid combination) |
|
| Azelastine (Nasal) | CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal). |
| Bromperidol | May enhance the CNS depressant effect of CNS Depressants. |
| Orphenadrine | CNS Depressants may enhance the CNS depressant effect of Orphenadrine. |
| Oxomemazine | May enhance the CNS depressant effect of CNS Depressants. |
| Paraldehyde | CNS Depressants may enhance the CNS depressant effect of Paraldehyde. |
| Thalidomide | CNS Depressants may enhance the CNS depressant effect of Thalidomide. |
Monitoring parameters:
- Monitor CBC and urinalysis before treatment initiation and every month thereafter for several months.
- Monitor liver function tests especially if there are clinical signs of hepatic dysfunction;
- Observe for suicidal behavior such as suicidal thoughts, depression, and behavioral changes.
How to administer Ethotoin (Peganone)?
It may be administered after meals to reduce the gastrointestinal side effects.
Mechanism of action of Ethotoin (Peganone):
It stops seizure activity from spreading and progressing by stabilizing the neuronal membrane (stabilizing seizure threshold).
Absorption:
- Rapid
Metabolism:
- It is metabolized in the liver to its metabolites. The enzymes are saturable therefore the relationship between the dose and concentration of the metabolites is not linear.
Half-life elimination:
- 3 to 9 hours
Excretion:
- Urine.
International Brand Names of Ethotoin:
- Peganone
Ethotoin Brand Names in Pakistan:
No Brands Available in Pakistan.
