 Hello everyone welcome back to another session at industry and more in pharmacology sessions topic for today is diazepam last session we finished nitrates so the uses of nitrates its side effects and its pharmacokinetics all we learned today we have diazepam diazepam is a medicine of benzo diazepine benzo diazepine family diazepine family which act as angiolytic which is a commonly used angiolytic the benzo diazepine family drug which is commonly used to treat a very range of conditions including anxiety seizures alcohol withdrawal syndrome muscles spasms trouble sleeping all those things so we learned the details of diazepam so it depresses basically all levels of central nervous system okay so it depresses central nervous system through the increased action of GABA okay by increased action of GABA GABA is nothing but the gamma amino butry acid okay so diazepam depresses all levels of CNS activity by increased action of GABA and it helps to treat unbalanced chemicals in the brain cells okay unbalanced chemicals so it is also used to treat status epilepticus and other convulsive disorders okay status epilepticus and other convulsive disorders so before that we need to understand a little bit about epilepsy epilepsy is known as a seizure disorder epilepsy or fits is a seizure disorder in excessive and abnormal brain cell activity caused by excessive and abnormal brain cell activity it can occur at any age and it may vary in etiology okay so this seizures can be basically two type that is one is hereditary and other one is you know acquired so there are two classification for seizures again one can be partial and next will be the generalized one okay so the partial can again be divided as simple and complex simple and complex so we are studying about the seizures whereas a generalized consist of the tonic-clonic seizure and the clonic seizure then the athonic seizure then myoclonic seizure all those things and we have one more thing that is the most serious one that is status epilepticus it is a very serious condition where the seizure activity becomes life-threatening and it is basically which lasts for more than 30 minutes okay more than 30 minutes seizure activity which is lasting more than 30 minutes with two or more consecutive seizures consecutive seizures without any recovery between them that is very difficult to manage two consecutive seizures without recovery so that is status epilepticus so we learned about seizures and status epilepticus all comes under epilepsy so there's a pump he's a drug used to treat epilepsy so the treatment part or the drug response so the primary goals of treating acute seizures are prompt cessation of the seizure and prevention of any type of recurrence so what diazepam does is so when we apply or when we give diazepam to a brain cell so it has anti-convulsant effect by interacting with the receptor molecules that is benzodiazepine receptor okay so benzodiazepine receptor and after that it regulate the efficiency of inhibitory neurotransmitter GABA okay so there is GABA which act on the GABA A receptor okay so this is nothing but inhibitory neurotransmitter so it regulate the efficiency okay it regulate the efficiency of GABA at GABA A receptor that is how it bring out the action of anti-convulsants so this GABA A receptor is a complex one with chloride channels it has got chloride channels and that contains benzodiazepine as an allosteric modulator unit so you know what is allosteric unit because every receptor has a active site so this might be the active site but if the molecule attached to any other part other than the active site and bring out the action it is known as allosteric unit and basically this diazepam crosses the blade brain barrier to elicit the pharmacological effect now we have DREC interaction so what could be the other DREC interact with diazepam okay DREC interaction so the common one is the valproic acid okay valproic acid may also result okay in an increasing inserity effect of diazepam by displacing it from the binding side so this valproic acid act as a competitive antagonist okay so we learned what is DREC antagonism in previous class so this competitive antagonist means this active site where this diazepam supposed to attach instead of that this valproic acid comes and get attached so that is known as competitive antagonism there is a competition between the diazepam and valproic acid okay so that DREC interaction we can expect with respect to the diazepam and valproic acid so what are the side effects of diazepam okay since it is an anti-convulsant effect there could be lots of side effects because it is crossing blade brain barrier so normally it could be the drowsiness vertigo and the decreased respiratory rate and there could be tachycardia chest pain confusion slurred speech on headache so common side effects may include rashes constipation osia vomiting all those things along with menstrual irregularities and blurred vision so sedation is a commonly reported adverse event associated with diazepam in any root that is administered okay so all those things slurred speech confusion attacks here nausea vomiting all those things menstrual irregularities menstrual problems all those things are the side effects so now let's learn the pharmacokinetics so in pharmacokinetics we have the volume distribution equals around 0.8 to 1.9 litre per kg and the percentage bound to plasma protein equals 98 where the t-half equals 44 to 48 hours though it accumulates over time and can take longer with prolonged use okay this may increase and oral bioavailability is greater than 90 percentage and time to reach the peak ranges from 15 minutes so this is minutes to 2.5 hours so if the person is on fasting the peak time can be 1.5 hours and with food it can be 2.5 hours and the metabolism happens inside liver by the oxidation catalysis by the enzyme cytochrome P450 okay so this was about the pharmacokinetics so regarding the binding issues so we learned earlier the valproic acid act as a competitive antagonist okay so it replaces the it replaces valproic acid from the binding sites i mean valproic acid replaces the diazepam from the binding sites and it gets attached to the site this is a mass competitive antagonism so that was about the binding issues now we have the application to practice so patient and caregivers must understand the different types of seizures and understand when they should be prompted to seek medical emergency because overuse and abuse must be avoided with respect to the diazepam drug because they have got so much of side effects and patient might develop tolerance to diazepam so that was about diazepam drug so we learned about pharmacodynamics pharmacokinetics its side effects and its mechanism of action and the antagonist that is the valproic acid how it affects diazepam in a competitive antagonist manner so all those things you need to write when it asked as a short note so it commonly asked as a short note diazepam alone sometimes the centrally acting dricks can be asked as a essay but diazepam alone can be come only as a short note for a small three marks or five marks so all these points will fetch you definitely 80 percentage marks okay so i'll come up with a new topic in pharmacology thank you