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carbamazepine

Carbamazepine (CBZ)

Carbamazepine-associated withdrawal reaction (CAWR) is dependent on the pre-operative dosage and the changing rate of pre- and post-operative CBZ blood concentrations 1).

Female patients with epilepsy and an older age, AED polytherapy, and carbamazepine treatment had a higher risk of low fT4. Thyroid function in these patients should be monitored closely. 2).


The goal of a study was to determine if the incorporation of carbamazepine, into a biodegradable microparticle for local sustained perineural release would be an efficacious analgesic following a peripheral injury.

Following induction of the chronic constriction injury model in Sprague-Dawley rats, mechanical allodynia testing was performed using von Frey filaments and thermal allodynia was evaluated using the Hargreaves method. Histology and blood work were performed to evaluate toxicity as well to monitor drug and metabolite presence over time.

A 2-fold increase in hindpaw withdrawal thresholds in animals receiving carbamazepine loaded microparticles relative to controls was observed for up to 14 days after treatment. Drug and metabolite had a peak blood concentration of 54.7ng/mL and dropped off exponentially to less than 5ng/mL over a few days.

This formulation reduced systemic exposure to carbamazepine over 1,000-fold relative to traditional analgesic dosing regimens. This two-component drug-delivery system has been specifically engineered to release a controlled amount of carbamazepine over a 14 day period providing significant pain relief with no toxicological or observable adverse events via behavioral or histochemical analysis 3).

1)
Chen MJ, Zhang WJ, Guo ZL, Zhang WH, Chai Y, Li YW. Withdrawal reaction of carbamazepine after neurovascular decompression for trigeminal neuralgia: A preliminary study. J Neurol Sci. 2013 Dec 11. pii: S0022-510X(13)03084-0. doi: 10.1016/j.jns.2013.12.013. [Epub ahead of print] PubMed PMID: 24387898.
2)
Shih FY, Chuang YC, Chuang MJ, Lu YT, Tsai WC, Fu TY, Tsai MH. Effects of antiepileptic drugs on thyroid hormone function in epilepsy patients. Seizure. 2017 Mar 19;48:7-10. doi: 10.1016/j.seizure.2017.03.011. [Epub ahead of print] PubMed PMID: 28364656.
3)
Dai H, Tilley DM, Mercedes G, Doherty C, Gulati A, Mehta N, Khalil A, Holzhaus K, Reynolds FM. Opiate-free pain therapy using carbamazepine-loaded microparticles provides up to two weeks of pain relief in a neuropathic pain model. Pain Pract. 2018 May 3. doi: 10.1111/papr.12705. [Epub ahead of print] PubMed PMID: 29723917.
carbamazepine.txt · Last modified: 2018/05/04 11:02 by administrador