Carbamazepin Chemische Eigenschaften,Einsatz,Produktion Methoden
R-S?tze Betriebsanweisung:
R42/43:Sensibilisierung durch Einatmen und Hautkontakt m?glich.
R22:Gesundheitssch?dlich beim Verschlucken.
R20/21/22:Gesundheitssch?dlich beim Einatmen,Verschlucken und Berührung mit der Haut.
S-S?tze Betriebsanweisung:
S37:Geeignete Schutzhandschuhe tragen.
S24:Berührung mit der Haut vermeiden.
S22:Staub nicht einatmen.
S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
Carbamazepine is a synthetic iminostilbene derivative structurally
similar to imipramine, a tricyclic antidepressant. While
unrelated structurally, carbamazepine shares a similar therapeutic
action with phenytoin. Carbamazepine was first discovered
in 1953 by Swiss chemist Walter Schindler. Throughout the
1960s, antimuscarinic was used and marketed for trigeminal
neuralgia and as an anticonvulsant. By the 1970s, it was being
used as a mood stabilizer for patients with bipolar disorder.
Chemische Eigenschaften
White or off-white crystalline powder. Soluble in ethanol, acetone, propylene glycol, insoluble in water. Odorless and tasteless.
Verwenden
Carbamazepine (CBZ) is a first generation anticonvulsant and mood stabilizing compound that has been used as a therapeutic in the context of neuropathic pain, epilepsy, and affective disorders. It exerts its effects by blocking voltage-gated sodium channels (IC50 = 640 μM), making fewer of these channels available to subsequently open, which leads to decreased high-frequency repetitive firing of action potentials. The estimated IC50 values for inhibition of Nav1.7-, Nav1.3-, and Nav1.8-type channels by CBZ following prolonged inactivation have been reported as 406, 900, and 138 μM, respectively. CBZ can also inhibit L-type Ca2+ channels (IC50 = 974 μM) and has been shown to potentiate GABAA receptors (IC50 >3 mM).
Definition
ChEBI: Carbamazepine is a dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant. It has a role as an anticonvulsant, an EC 3.5.1.98 (histone deacetylase) inhibitor, a mitogen, a glutamate transporter activator, an antimanic drug, an analgesic, a non-narcotic analgesic, an environmental contaminant, a xenobiotic, a drug allergen and a sodium channel blocker. It is a dibenzoazepine and a member of ureas.
Biologische Funktion
Carbamazepine has become a major drug in the treatment
of seizure disorders. It has high efficacy, is well tolerated
by most patients, and exhibits fewer long-term
side effects than other drugs.
Oral absorption of carbamazepine is quite slow and
often erratic. Its half-life is reported to vary from 12 to
60 hours in humans.The development of blood level assays
has markedly improved the success of therapy with
this drug, since serum concentration is only partially
dose related. Carbamazepine is metabolized in the liver,
and there is evidence that its continued administration
leads to hepatic enzyme induction. Carbamazepine-
10,11-epoxide is a pharmacologically active metabolite with significant anticonvulsant effects of its own.
Allgemeine Beschreibung
Certified pharmaceutical secondary standards for application in quality control provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to pharmacopeia primary standards.
Carbamazepine is a tricyclic lipophilic compound, with mild anticholinergic activity. It is widely used as an antiepileptic drug for the treatment of simple and complex partial tonic-clonic seizures.
Mechanism of action
In animals, the profile of antiseizure properties for CBZ is similar to that of phenytoin. CBZ is effective in the maximal
electroshock (MES) test (electrically induced seizure test) but is ineffective against pentylenetetrazole-induced seizures. It is
not effective for absence or myoclonic seizures and, indeed, may exacerbate their onset. Like phenytoin, CBZ acts on
voltage-dependent sodium channels to prevent the spread of seizures. CBZ depresses synaptic transmission in the reticular
activating system, thalamus, and limbic structures. In a double-blind, crossover study in patients whose seizures were not
controlled completely by combinations of AED, CBZ was equal in efficacy to phenobarbital and phenytoin in controlling seizure
frequency, and side effects were minimal.
Clinical Use
Carbamazepine is an effective agent for the treatment
of partial seizures and generalized tonic–clonic
seizures; its use is contraindicated in absence epilepsy.
Carbamazepine is also useful in the treatment of
trigeminal neuralgia and is an effective agent for the
treatment of bipolar disorders.
Arzneimittelwechselwirkung
Carbamazepine may be affected by other medicines, such as blood clot preventers and antibiotics. It may also interact with medications used to treat bipolar disorder. Some medications can decrease carbamazepine levels and others can increase carbamazepine levels. Valproate may increase carbamazepine-10,11-epoxide levels, while carbamazepine may decrease the levels of various medications including corticosteroids, clozapine, and lamotrigine. It is important to inform your doctor if you are taking any of these medicines to avoid potential interactions and to ensure carbamazepine works effectively.
Taking carbamazepine with other medicines and herbal supplementsWhat drug-drug interactions should you be vigilant for when someone is prescribed carbamazepinehttps://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c13bc0b8-7900-4ef4-98ed-e1315a08d95d
Environmental Fate
Carbamazepine is both an important anticonvulsant in therapeutic
doses and a powerful proconvulsant in overdose. The
therapeutic anticonvulsant mechanism is primarily related to
blockade of presynaptic voltage-gated sodium channels.
Blockade of the sodium channels is believed to inhibit the
release of synaptic glutamate and possibly other neurotransmitters.
Carbamazepine is also a powerful inhibitor of the
muscarinic and nicotinic acetylcholine receptors, N-methyl-Daspartate
(NMDA) receptors, and the central nervous system
(CNS) adenosine receptors. In addition, carbamazepine is
structurally related to the cyclic antidepressant imipramine
and in massive overdose, it may affect cardiac sodium
channels.
Carbamazepin Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
