18.104.22.168 Mechanism of action
Prolepsi is the keto-derivative of carbamazepine and was developed by introducing minimal changes in the structure of carbamazepine to change the metabolism to avoid the epoxide metabolite. At least part of the antiepileptic effect of Prolepsi seems to be based on interactions with sodium and potassium channels .
Serious side effects
Call your doctor right away if you have serious side effects. Call 911 if your symptoms feel life-threatening or if you think you’re having a medical emergency. Serious side effects and their symptoms can include the following:
- Low sodium levels in your blood. Symptoms can include:
- lack of energy
- more frequent or more severe seizures
- fever, swollen glands, or sore throat that don’t go away or that come and go
- skin rash
- swelling of your face, eyes, lips, or tongue
- trouble swallowing or breathing
- painful sores in your mouth or around your eyes
- yellowing of your skin or the whites of your eyes
- unusual bruising or bleeding
- severe tiredness or weakness
- severe muscle pain
- frequent infections or infections that don’t go away
Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs affect each person differently, we cannot guarantee that this information includes all possible side effects. This information is not a substitute for medical advice. Always discuss possible side effects with a healthcare provider who knows your medical history.
Prolepsi oral tablet can interact with other medications, vitamins, or herbs you may be taking. An interaction is when a substance changes the way a drug works. This can be harmful or prevent the drug from working well.
To help avoid interactions, your doctor should manage all of your medications carefully. Be sure to tell your doctor about all medications, vitamins, or herbs you’re taking. To find out how this drug might interact with something else you’re taking, talk to your doctor or pharmacist.
Examples of drugs that can cause interactions with Prolepsi are listed below.
Prolepsi , the keto-analogue of carbamazepine, was developed to preserve carbamazepine’s membrane-stabilizing effects while minimizing minor adverse effects, such as sedation and serious or life-threatening reactions. A major advantage of Prolepsi is that monitoring of drug plasma levels and hematologic profiles is generally not necessary. Similar to carbamazepine, Prolepsi blocks sodium channels; it does not affect gamma-aminobutyric acid (GABA) receptors.
Significant hyponatremia (sodium 14 They were treated with 300 mg/day that was titrated to a maximum of 1800 mg/day. Prolepsi-treated patients reported less pain on VAS, global improvement, and less sleep disturbances due to pain.
The superior side-effect profile of Prolepsi compared with carbamazepine has led to its increased use. Although it is better tolerated, there is still a significant incidence of adverse effects. In a retrospective review of 100 patients successfully treated for trigeminal neuralgia with oxycarbazepine, there was an 18% discontinuation rate secondary to adverse effects. 13 In several countries Prolepsi is now the drug of choice for trigeminal neuralgia. Although a case series reported its efficacy in the treatment of neuropathic pain, 13 prospective randomized controlled studies are lacking at this time.
Dosage Considerations – Should be Given as Follows:
Adjunctive treatment, Adult
- Trileptal: 300 mg orally every 12 hours initially; may increase at weekly intervals by 600 mg/day up to 1200 mg/day
- Oxtellar XR: 600 mg orally once/day initially; may increase at weekly intervals by 600 mg/day increments to target dosage range of 1200-2400 mg once/day
Trileptal (age 2-4 years)
- Node positive (adjuvant chemotherapy): 175 mg/m² intravenously (IV) over 3 hours every 3 weeks 4 times (with doxorubicin-containing regimen)
- Metastatic Disease (failure of initial chemotherapy or relapse within 6 months following adjuvant chemotherapy): 175 mg/m² IV over 3 hours every 3 weeks
Trileptal (age 4-16 years)
- Initial: 8-10 mg/kg/day orally divided every 12 hours; not to exceed 600 mg/day
- Target maintenance dose: May titrate to higher dose over 2 weeks to reach the following dosage ranges
- 20-29 kg: 450 mg orally every 12 hours
- 29.1-39 kg: 600 mg orally every 12 hours
- Greater than 39 kg: 900 mg orally every 12 hours
Oxtellar XR (age 6-17 years)
- Initial: 8-10 mg/kg orally once/day; not to exceed 600 mg/day in the first week
- Target maintenance dose: May titrate to higher dose at weekly intervals in 8-10 mg/kg/day increments (not to exceed 600 mg) to reach the following target maintenance dosage ranges over a 2-3 week period
- 20-29 kg: 900 mg orally once/day
- 29.1-39 kg: 1200 mg orally once/day
- Greater than 39 kg: 1800 mg orally once/day
Monotherapy (if converting from other antiepileptic drug ), Adult
- Initial: 300 mg orally every 12 hours; increase by 600 mg/day once/week up to 2400 mg/day
- Reduce and withdraw concomitant antiepileptic drugs (AEDs) over 3-6 weeks while reaching maximum Prolepsi dose in 2-4 weeks
Monotherapy (if antiepileptic drug naive), Adult
- Initial: 300 mg orally every 12 hours; increase by 300 mg/day every 3 days to 1200 mg/day divided every 12 hours
Trileptal (age 4-16 years)
- Antiepileptic drug (AED) conversion: Initial, 8-10 mg/kg/day orally divided every 12 hours; may increase once/week by maximum increment of 10 mg/kg/day
- Antiepileptic drug (AED)-naive: Initial 8-10 mg/kg/day orally divided every 12 hours; may increase every 3 days by 5 mg/kg/day
- Target maintenance: Weight-based dosing may be as high as 2100 mg/day for greater than 60 kg
- 20-24.99 kg: 600-900 mg/day
- 25-34.99 kg: 900-1200 mg/day
- 35-44.99 kg: 900-1500 mg/day
- 45-49.99 kg: 1200-1500 mg/day
- 50-59.99 kg: 1200-1800 mg/day
- 60-69.99 kg: 1200-2100 mg/day
- 70 kg: 1500-2100 mg/day
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Why it's used
Prolepsi is used to treat partial seizures in people with epilepsy.