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The plasma half-life is about 35 to 40 hours when carbamazepine is given as single dose, but it is a strong inducer of liver enzymes, and the plasma half-life shortens to about 12 to 17 hours when it is given repeatedly. The half-life can be further shortened to 9–10 hours by other enzyme inducers such as phenytoin or phenobarbital. About 70% ...
Low IC 50 or high pIC 50 values indicate tighter binding (pIC 50 of 8.0 = IC 50 of 10nM, pIC 50 of 9.0 = IC 50 of 1nM, etc.) These are non subtype selective IC 50 values averaged across all GABA A receptor subtypes , so subtype selective compounds with strong binding at one subtype but weak at others will appear unusually weak due to averaging ...
A derivative of carbamazepine that has similar efficacy and is better tolerated and is also available generically. Eslicarbazepine acetate (2009). Photoswitchable analogues of carbamazepine (2024) are research compounds developed to control its pharmacological activity locally and on demand using light, with the purpose to reduce adverse ...
Acute use (1–3 days) yields a potency about 1.5× stronger than that of morphine and chronic use (7 days+) yields a potency about 2.5 to 5× that of morphine. Similarly, the effect of tramadol increases after consecutive dosing due to the accumulation of its active metabolite and an increase of the oral bioavailability in chronic use.
Esketamine (Spravato) – non-competitive NMDA receptor antagonist, other actions [13] Gepirone (Exxua) – 5-HT 1A receptor partial agonist and α 2-adrenergic receptor antagonist; Opipramol (Insidon) — σ 1 receptor agonist, other actions; Tianeptine (Stablon, Coaxil, Tianeurax) – weak and atypical μ-opioid receptor agonist, other actions
The most common ones (more than 10% of patients) are tiredness and dizziness. Other fairly common side effects (1 to 10%) include impaired coordination, gastrointestinal disorders such as diarrhoea, nausea and vomiting, rash (1.1%), and hyponatremia (low sodium blood levels, 1.2%). [3] [9] There may also be an increased risk of suicidal ...
Other side effects include vision loss and dizziness. [3] It is a recommended treatment in pregnancy and appears to be safe for the baby. [4] [5] The World Health Organization; however, recommends waiting until after pregnancy for treatment when feasible. [2] It is made from 4-methyl-piperazine. [6]
Cenobamate, sold under the brand names Xcopri (US) and Ontozry (EU), is a medication used for the treatment of partial-onset seizures, a kind of epilepsy, in adults. [3] [7] [8] It is taken by mouth.