Anticonvulsant Drugs (Arabic PDF)

‫كلية الطب – جامعة العميد‬ ‫الحملة التوعوية حول الحصول‬ ‫ا‪8‬عتمادية‬ ‫على‬  ‫الرؤية‬ ‫التميز الفعال من اجل رفد ا‪P‬جتمع بأطباء اكفاء في الخدمة الطبية والبحث‬ ‫العلمي‬ ‫الرسالة‬ ‫توفير بيئة ج...

‫كلية الطب – جامعة العميد‬ ‫الحملة التوعوية حول الحصول‬ ‫ا‪8‬عتمادية‬ ‫على‬  ‫الرؤية‬ ‫التميز الفعال من اجل رفد ا‪P‬جتمع بأطباء اكفاء في الخدمة الطبية والبحث‬ ‫العلمي‬ ‫الرسالة‬ ‫توفير بيئة جامعية تعمل بمنهج تعليمي مواكب للتطور‬ ‫اطباء ذوي كفاءة ومستوى علمي قادرين على تقديم الخدمة ا‪P‬تميزة‬ ‫ا‪8‬هداف‬ ‫اعداد اطباء بكفاءة عالية ‬ ‫التأكيد على مبادئ ا‪8‬خ‪D‬ق ‬ ‫الطبية‬ ‫نشر مفاهيم العمل كفريق ‬ ‫واحد‬ ‫العمل على حل ا‪P‬شك‪D‬ت ‬ ‫الصحية‬ ‫تطبيق مخرجات البحوث ‬  ‫تقدمة‬P‫ا‬ University of Al-Ameed College of Medicine Department of Dharmacology Loading… Anti-depressant drugs Assist. Professor Dr. Kamal Al-Yassiry Pharmacologist Loading… Vortioxetine is a newer agent that acts as an antagonist of the 5-HT3, 5-HT7, and 5-HT1D receptors, a partial agonist of the 5-HT1B receptor, and an agonist of the 5HT1A receptor. ‫ترك‬ Loading… ‫كلية الطب – جامعة العميد‬ ‫الحملة التوعوية حول الحصول عىل‬ ‫االعتمادية‬  ‫الرؤية‬ ‫التمي الفعال من اجل رفد المجتمع بأطباء اكفاء يف الخدمة الطبية والبحث ال ي‬ ‫علم‬ ‫الرسالة‬ ‫تعليم مواكب للتطور‬ ‫ي‬ ‫توفي بيئة جامعية تعمل بمنهج‬ ‫علم قادرين عىل تقديم الخدمة المتمية‬ ‫ي‬ ‫اطباء ذوي كفاءة ومستوى‬ ‫االهداف‬ ‫اعداد اطباء بكفاءة عالية‬ ‫ ‬ ‫التأكيد عىل مبادئ االخالق الطبية‬ ‫ ‬ ‫نش مفاهيم العمل كفريق واحد‬ ‫ر‬ ‫ ‬ ‫العمل عىل حل المشكالت الصحية‬ ‫ ‬ ‫تطبيق مخرجات البحوث المتقدمة‬ ‫ ‬ ‫العلم‬ ‫ي‬ ‫تعزيز عملية البحث‬ ‫ ‬ ‫المهن المستمر‬ ‫ي‬ ‫تبن مفاهيم التعلم‬ ‫ي‬ ‫ ‬  University of Al-Ameed College of Medicine Department of Dharmacology Anti- Psychotic drugs Assist. Professor Dr. Kamal Al-Yassiry Pharmacologist Special considerations regarding anti-psychotics  Pharmacokinetics They are readily but incompletely absorbed They undergo significant 1st pass metabolism, e.g. the oral dose of Chlorpromazine & Thioridazine have systemic availability 25-35%. Most antipsychotics highly lipid soluble & protein bound They tend to have a large volume of distribution Very little of theses drugs are excreted unchanged.  University of Al-Ameed College of Medicine Department of Dharmacology Assist. Professor Dr. Kamal Al-Yassiry Pharmacologist  Epilepsy is a very common disorder, characterized by abnormal neuronal discharge, causes seizure. Epilepsy affects 0.5–1% of population 75% of cases can be controlled by medications Sodium channel blocking agents Phenytoin Used for generalized tonic clonic seizures and for the treatment of partial seizures with complex symptoms. Phenytoin is highly bound (about 90%) to plasma proteins. Phenytoin displays zero-order (saturable) kinetics.  Side effects Nystagmus, ataxia, vertigo, and diplopia, skin rashes, exfoliative dermatitis, blood dyscrasias and hepatic necrosis. The most common side effect in children receiving long-term therapy is gingival hyperplasia, hirsutism, peripheral neuropathy, teratogenicity (folate deficiency).  Carbamazepine It has high efficacy, is well tolerated by most patients, and exhibits fewer long-term side effects than other drugs. Carbamazepine is metabolized in the liver, its hepatic enzyme inducer. 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.  Side effects Drowsiness, nausea, headache, dizziness, vertigo, and diplopia, rashes, hepatosplenomegaly, and lymphadenopathy. Carbamazepine can induce its own metabolism (auto induction) after prolonged administration and also can induce the enzymes that metabolize other anticonvulsant drug.  Oxcarbazepine: is related to carbamazepine, but it has much less capacity of enzyme induction. Lamotrigine: Lamotrigine has a broad spectrum of action and is effective in generalized and partial and absence seizures. Unlike most drugs, Lamotrigine is metabolized primarily by glucuronidation. Side effects: Severe skin rashes, dizziness, diplopia, ataxia, and blurred vision. Topiramate: used for generalized tonic–clonic seizures and those with partial complex seizures. Topiramate causes a higher incidence of CNS related side effects.  Valproic Acid (Sodium Valproate) It is absorbed orally, it can increase in brain GABA with evidence that valproate may also inhibit T-calcium channels. It is highly bound (~90%) to plasma protein. It is highly effective against absence seizures and myoclonic seizures, generalized tonic– clonic epilepsy and for partial seizures with complex symptoms. Adverse effect: fatal hepatic failure. which is idiosyncratic reaction; increased incidence of neural tube defects in the fetus, hair loss, transient gastrointestinal effects are common, hyperglycemia, increase in body weight.  Drugs that primarily enhance the action of GABA Benzodiazepines A limiting side effect of the benzodiazepines is the rapid development of tolerance to their anti- convulsant effects. Lorazepam is the benzodiazepine of choice for emergency treatment of status epilepticus Tiagabine: It blocks the reuptake of GABA. It is primarily used in the treatment of partial complex seizures. Adverse effects: dizziness, somnolence, nervousness, nausea, and confusion Vigabatrin: It is irreversible inhibitor of GABA-transaminase (GABA-T), the major enzyme responsible for the metabolism of GABA. It is well absorbed orally, contraindicated in absence epilepsy or myoclonic seizures. Phenobarbital and Primidone: They acting by binding to an allosteric site on the GABA-benzodiazepine receptor, hence by prolonging the opening of the chloride channels The untoward effect: sedation, disturbance in cognitive function.  Drugs that primarily block calcium channels Ethosuximide: It used for against absence epilepsy. Side-effects: nausea, blood dyscrasias, gastrointestinal irritation, drowsiness, and anorexia.  Other unclassified drugs Felbamate ❑It blocks voltage-dependent sodium channels, competing with the glycine-binding site on the Nmethyl-D-aspartate (NMDA) glutamate receptor, blocking of calcium channels, and potentiating GABA action. ❑Reserved for refractory cases ❑Metabolized by cytochrome P-system ❑Side effect: aplastic anemia Gabapentin It is an analog of GABA enhance the effect of endogenous GABA on its receptor Has Calcium- channel blocking effect Lacosamide Approved for adjunctive treatment of focal seizures Lamotrigine Blocks both sodium and calcium channels. Used , in addition for variety of epileptic forms, for bipolar disease. Levetiracetam and Perampanel They approved as adjunct therapy  Anticonvulsant drugs and pregnancy Withdrawal of medication from an epileptic pregnant woman has a very hazardous effect on both the mother and the fetus. Safest drug in pregnancy is carbamazepine which must be kept at a lower therapeutic level. TREATMENT OF FEBRILE SEIZURES Phenobarbital is the usual drug I.V Diazepam is also effective I.V.  TREATMENT OF STATUS EPILEPTICUS All the following drugs should be administered slowly to avoid respiratory depression and apnea. Fosphenytoin: is a pro-drug that is converted to phenytoin following parenteral administration. It is very effective in terminating seizures and will stop most status epilepticus episodes and provide long-term control without any decreased level of consciousness. Guidelines for treating status epilepticus