LYCOS RETRIEVER 
Carbamazepine
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Carbamazepine is used to treat simple and complex partial and generalized seizures, as a specific analgesic for trigeminal neuralgia, and to treat bipolar disorder. It is used alone or in combination with other antiepileptic drugs. While its exact mechanism is not totally understood, it is thought that carbamazepine blocks polysynaptic responses in nerve cells of the brain. Carbamazepine (CBZ) is a widely used drug in neurology and psychiatry. CBZ was originally introduced as an anticonvulsant and nowadays is used as a first-line drug in patients with localization-related epilepsies. There is good evidence that CBZ is effective in the management of acute mania and prophylaxis of bipolar disorder, and it might have some benefit in the treatment of drug-resistant depression.
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Carbamazepine is metabolized in the liver by oxidation to an active metabolite, carbamazepine 10,11-epoxide, which undergoes further metabolism. Carbamazepine is a potent enzyme inducer and can induce its own metabolism. Onset of enzyme induction is at about 3 days, with maximum effect at about 30 days. There is high interindividual variability in the extent to which induction occurs. The plasma half-life is 25÷65 hours initially and 12÷17 hours after repeated dosing. Induction of microsomal enzymes ... affects the metabolism of other concomitantly used drugs via induction of the cytochrome P-450 2D6 enzyme system.
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Carbamazepine may cause birth defects and should be avoided in women who are pregnant. In addition, women sometimes develop hypersensitivity reactions to carbamazepine during pregnancy. An appropriate contraceptive method should be used while on carbamazepine. Carbamazepine can cross into breast milk and should be avoided in women who are breastfeeding. Carbamazepine may ... cause rash or sensitivity to the sun.
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Carbamazepine and its derivatives' mechanism of action is relatively well understood. Voltage gated sodium channels are the molecular pores that allow brain cells (neurons) to generate action potentials, the electrical event that allows neurons to communicate over long distances. After the sodium channels open, to start the action potential, they inactivate, essentially closing the channel. Carbamazepine stabilizes the inactivated state of sodium channels, meaning that fewer sodium channels are available to open, making brain cells less excitable.
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Carbamazepine is bound to serum proteins to the extent of 70 to 80%. The concentration of unchanged substance in cerebrospinal fluid and saliva reflects the non-protein bound portion in the plasma (20 to 30%). Concentrations in breast milk were found to be equivalent to 25 to 60% of the corresponding plasma levels.
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Carbamazepine prevents epileptic fits by preventing the excessive electrical activity in the brain. It is thought to achieve this by preventing sodium from entering nerve cells when they begin to fire rapid and repetitive electrical signals. A build up of sodium in the nerve cells is necessary for the electrical signal to build up and be passed on to other nerve cells. As carbamazepine prevents this, it helps stabilise the electrical activity in the brain.
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Carbamazepine