1 / 14

Chapter 2.2. Antiepileptics

Chapter 2.2. Antiepileptics. Phenobartibal, diazepam, cloazepam are widely used antilepileptics Others: Phenytoin and carbamazeoine. Structure and Nomenclature. Phenytoin Chemical name: 5,5-diphenylhydantoin Brand name: Dilantin.

leroy
Download Presentation

Chapter 2.2. Antiepileptics

An Image/Link below is provided (as is) to download presentation Download Policy: Content on the Website is provided to you AS IS for your information and personal use and may not be sold / licensed / shared on other websites without getting consent from its author. Content is provided to you AS IS for your information and personal use only. Download presentation by click this link. While downloading, if for some reason you are not able to download a presentation, the publisher may have deleted the file from their server. During download, if you can't get a presentation, the file might be deleted by the publisher.

E N D

Presentation Transcript

  1. Chapter 2.2. Antiepileptics

  2. Phenobartibal, diazepam, cloazepam are widely used antilepileptics Others: Phenytoin and carbamazeoine

  3. Structure and Nomenclature Phenytoin Chemical name: 5,5-diphenylhydantoin Brand name: Dilantin

  4. Phenytoin sodium (marketed as Dilantin® in the USA and as Epanutin® in the UK, was approved by the US FDA in 1953 for use in seizures. Phenytoin was first synthesized by a German physician named Heinrich Biltz in 1908. Biltz sold his discovery to Parke-Davis, which did not find an immediate use for it. In 1938, outside scientists including H. Houston Merrt and Tracy Putnam discovered phenytoin's usefulness for controlling seizures, without the sedation effects associated with phenobarbital. There are some indications that phenytoin has other effects, including anxiety control and mood stabilization. Jack Dreyfus, founder of the Dreyfus Fund, became a major proponent of phenytoin as a means to control nervousness and depression when he received a prescription for Dilantin in 1966. Dreyfus' book about his experience with phenytoin, A Remarkable Medicine Has Been Overlooked, sits on the shelves of many physicians courtesy of the work of his foundation. Despite more than $70 million in personal financing, his push to see phenytoin evaluated for alternative uses has had little lasting effect on the medical community.

  5. Chemical synthesis of Phenytoin

  6. Hygroscopicity and acidity • Its sodium salt displays the property of hygroscopicity • When exposes in the air, it absorbs CO2, and precipitate • Phenytoin • Aqueous solution is basic • The pKa value is equal to 8.3

  7. Glucose combo It’s metabolism proceeds by p-hydroxylation by liver enzymes followed by conjugation. Mechanism of action is not well understood.

  8. Chemical Synthesis

  9. Carbamazepine is an anticonvulsant and mood stabilizing drug, used primarily in the treatment of epilepsy. Mechanisms of action 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.

  10. Properties of Carbamazepine • Stability • More stable under room temperature and • dried status • Its tablet when store in humid atmosphere, medical • effect will drop down.

  11. Metabolize • Mainly in liver • Metabolite is mainly vented via urine • Part of metabolite is vented via excrement • The primary metabolite, which expoxidation • occurs at site 10 and 11, also have antiepileptic • activity

  12. Metabolization inside the body

  13. Action • Absorb via stomach and intestines • Because the aqueous solubility is not so good, • absorbance is slow and irregular. • Treatment for grand epilepsy and integrity focal epilepsy. • Mechanism of action is similar to that of phenytoin • sodium

More Related