Carbamazepine Raw material Carbamazepine Powder

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Carbamazepine Powder Usage and Synthesis.

Clinical indications for carbamazepine include psychomotor seizures, trigeminal neuralgia, manic-depressive disorder, central partial urolithiasis, restless leg syndrome, hemifacial spasms, withdrawal syndromes of alcoholism, schizophrenic affective disorders, intractable schizophrenia, loss-of-control syndromes associated with limbic dysfunction, and more.

Uses of Carbamazepine.

Carbazepine is a dibenzazepine antiepileptic drug with antiepileptic effects similar to those of phenytoin sodium. It is most effective against psychomotor seizures, and is also effective against grand mal seizures, limited seizures and mixed seizures.

Carbazepine is superior to phenytoin sodium in its anti-peripheral neuralgia effects and can be used for trigeminal neuralgia and glossopharyngeal neuralgia. It can also be used in the treatment of cardiac arrhythmia and dysuria. The oral LD50 is 3750mg/kg in mice and 4025mg/kg in rats.

Sedative; ligand for the benzodiazepine regulatory site of the GABAA receptor. Sodium channel inhibitor.

Anticonvulsants, used in the treatment of grand mal and psychomotor epilepsy, also for trigeminal neuralgia.

Drug interactions.

Pharmacological Effect of Carbamazepine.

Membrane stabilising effect, can reduce the permeability of the nerve cell membrane to Na+ and Ca2+, thus reducing the excitability of the cell and prolonging the period of inappetence; it may also enhance the synaptic transmission function of GABA.

The anticonvulsant mechanism is similar to phenytoin, the inhibition of tonic late reinforcement of synaptic sites, limiting the spread of abnormal discharges from epileptogenic foci. May also inhibit electrical activity within the anterior ventral nucleus of the thalamus. The mechanism of analgesia is unknown and may attenuate synaptic transmission in the CNS.

FAQ.

Q1: What should I do if I miss a dose?
A: If it is close to the next scheduled dose, skip the missed dose; do not take a double dose.

Q2: Does alcohol consumption affect the medication?
A: Alcohol consumption is strictly prohibited! It may exacerbate drowsiness and liver toxicity.

Q3: What regular check-ups are required?
A: Monthly: Complete blood count, liver function tests

Every 3 months: Blood drug concentration monitoring

Seek medical attention immediately if a rash develops

Q4: What foods should be avoided?
A: Grapefruit juice (inhibits metabolism, leading to toxicity).

Product Method of Bulk Carbamazepine Powder.

10,11-dihydro-5H-dibenzo[b,f]azepine is first prepared from o-nitrotoluene by condensation, reduction and cyclisation, and then the product is prepared by elimination and acylation, or by chloroformylation, bromination, elimination and amination.

1.Preparation of 10,11-dihydro-5H-dibenzo[b,f]azepine A mixture of sodium methanol and petroleum ether was cooled and a mixture of o-nitrotoluene and ethyl formate was added dropwise and adjusted to pH 5-6 with dilute hydrochloric acid.2,2'-Dinitrobiphenyl.

Dissolve it in ethanol and add hydrochloric acid-ethanol dropwise while adding iron powder slowly. It was adjusted to pH 8-9 with sodium hydroxide and filtered, and the filtrate was adjusted to pH 5 with phosphoric acid to precipitate crystals to give 2,2'-diaminobibenzyl phosphate.

The 2,2'diaminobibenzyl phosphate was heated to melt under stirring, and the material was put into water to precipitate crystals to obtain 10,11-dihydro-5H-dibenzo[b,f]azepine crude product. The crude product was recrystallised with petroleum ether to obtain the fine product.

2. Carbazepine preparation method a reaction bed of iron catalyst with hot air activation, control the bed temperature at 400-450 ° C, through the superheated steam, slowly add the molten 10,11-dihydro-5H-dibenzo[b,f]azepine, the reaction product is absorbed through the absorption tower with water spray absorption, collection of solids floating under the tower, suction filtration, drying the crude product.

Recrystallised with ethanol to obtain 5H dibenzo[b,f]azepine fine. Then, using benzene as a solvent, 5H dibenzo[b,f]azepine and isocyanic acid reaction and then adjusted to pH 12-14 with sodium hydroxide solution, reflux, reduce the temperature to below 10 ℃, precipitation of crystals, filtration, washing, drying, to get the crude carbamazepine. The crude product was recrystallised with ethanol and decoloured with activated carbon, i.e. the finished product.

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