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Hypnotic ,Antiepileptic and Antiparkinsonian drugs
The document discusses various hypnotic, antiepileptic, and antiparkinsonian drugs. It describes the mechanism of action, clinical uses, and side effects of benzodiazepines, barbiturates, carbamazepine, diphenin, valproate sodium, and lamotrigine as hypnotic or antiepileptic drugs. It also classifies different types of epilepsy and lists first and second drug choices for seizure types.
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Overview of hypnotic, antiepileptic, and antiparkinsonian drugs.
Details on Benzodiazepine Receptor Agonists including various BZD compounds and their dosages.
Discussion of hypnotics with narcotic effects, including types of barbiturates and non-barbiturate hypnotics.
Mechanism of action for BZDs, their effects including anticonvulsant and sedative actions.
Mechanism, effects, uses, and pharmacological properties of Phenobarbital as a barbiturate.
Common adverse effects of barbiturates, stages of poisoning, and their treatments.
Overview of antiepileptic drugs, focusing on mechanisms of Na channel inactivation.
Examines Carbamazepine and Diphenin, including mechanisms, uses, and teratogenic effects.
Various GABA-ergic agents and drugs that inhibit excitatory neurotransmitters.
Classification of epileptic seizures into partial and generalized types.
First and second choice medications for different seizure types including focal and generalized.
Details on dopaminergic agents including Levodopa, combined agents, and their functions.
Adverse effects of Levodopa, benefits of using Carbidopa alongside it.
Effects of Bromocriptine as a dopamine agonist and its associated risks.
Wrap-up and expressions of gratitude for the audience.
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Hypnotic ,Antiepileptic and Antiparkinsonian drugs
- 1. HYPNOTIC, ANTIEPILEPTIC &HYPNOTIC,ANTIEPILEPTIC & ANTIPARKINSONIAN DRUGSANTIPARKINSONIAN DRUGS
- 2. HYPNOTICHYPNOTIC DRUGSDRUGS I.I. BenzodiazepineReceptor AgonistsBenzodiazepine Receptor Agonists 1. BZD compounds1. BZD compounds:: DiazepamDiazepam –Tab. 5 mg; Amp. 0.5%-2 ml–Tab. 5 mg; Amp. 0.5%-2 ml NitrazepamNitrazepam –– Tab. 5 and 10 mgTab. 5 and 10 mg LorazepamLorazepam –– Tab. 1 and 2 mg, Amp. 0. 2% - 1mlTab. 1 and 2 mg, Amp. 0. 2% - 1ml PhenazepamPhenazepam – Tab. 0.5 and 1 mg– Tab. 0.5 and 1 mg AlprazolamAlprazolam ((XanaxXanax) – Tab. 0.25 and 0.5 mg) – Tab. 0.25 and 0.5 mg ChlordiazepoxideChlordiazepoxide NozepamNozepam (OXAZEPAM, TAZEPAM) – Tab. 10 mg(OXAZEPAM, TAZEPAM) – Tab. 10 mg 2. Agents of other chemical groups2. Agents of other chemical groups:: ZOLPIDEMZOLPIDEM –– Tab. 10 mgTab. 10 mg ZOPICLONEZOPICLONE –– Tab. 7.5 mgTab. 7.5 mg 22
- 3. II.II. Hypnotics withNarcotic EffectHypnotics with Narcotic Effect 1.1. BarbituratesBarbiturates:: Long-actingLong-acting (1 - 2 days(1 - 2 days ):): PhenobarbitalPhenobarbital ((LuminalLuminal) – Tab.) – Tab. 0.005,0.005, 0.05 and 0.1 g0.05 and 0.1 g Short-acting:Short-acting: 3 - 8 hours3 - 8 hours AmobarbitalAmobarbital –– Tab.Tab. 0.03, 0.05, 0.1 g0.03, 0.05, 0.1 g;; VialVial 0.0.55 gg SecobarbitalSecobarbital –– CapsCaps. 0.05 and 0.1 g. 0.05 and 0.1 g;; syringe 5%-2-mlsyringe 5%-2-ml PentobarbitalPentobarbital Ultra-short acting:Ultra-short acting: 20 min20 min Thiopental sodiumThiopental sodium (( Aethaminalum-natriumAethaminalum-natrium,, NembutalNembutal )) 2. Nonbarbiturate hypnotics2. Nonbarbiturate hypnotics:: Chloral hydrateChloral hydrate -- powderpowder 33
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- 7. MECHANISM OF ACTIONof BZDsMECHANISM OF ACTION of BZDs Bind to theBind to the α-subunitα-subunit ofof the GABAthe GABAAA RsRs surrounding thesurrounding the ClCl ¯¯ channelschannels Designated asDesignated as BZD RsBZD Rs ((omega-receptorsomega-receptors)) Affinity of GABA receptorsAffinity of GABA receptors FrequencyFrequency ofof ClCl ¯¯ channel openingchannel opening ClCl ¯¯ conductanceconductance =>=> HYPERPOLARIZATIONHYPERPOLARIZATION IINHIBITIONNHIBITION ofof ACTION POTENTIALACTION POTENTIAL formation andformation and further NEURONAL FIRINGfurther NEURONAL FIRING BZDsBZDs turnover ofturnover of 5-HT5-HT andand NORADRENALINENORADRENALINE 77
- 8. Antispasticity Effect:Antispasticity Effect: -action on GABA- action on GABAAA Rs in theRs in the Brain StemBrain Stem Spinal ChordSpinal Chord SedativeSedative andand AnticonvulsantAnticonvulsant effects:effects: - are localized to the- are localized to the Limbic System.Limbic System. Seadtive-hypnotic EffectSeadtive-hypnotic Effect:: - is due to their actions on the- is due to their actions on the omega-1 Rsomega-1 Rs Impairment of Memory:Impairment of Memory: - action on the- action on the omega-2omega-2 RsRs 88
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- 10. PHENOBARBITALPHENOBARBITAL ((LuminalLuminal )) Tab.0.005, 0.05 and 0.1 gTab. 0.005, 0.05 and 0.1 g BBind toind to β-subunitβ-subunit ofof the GABAthe GABAAA RsRs => Facilitate the actions of GABA=> Facilitate the actions of GABA DURATIONDURATION of the GABA-gatedof the GABA-gated ClCl ¯¯ channelchannel openingsopenings is a potentis a potent inducer of theinducer of the P-450P-450 systemsystem, and it, and it enhances the metabolism of other agentsenhances the metabolism of other agents 1010
- 11. Pharmacological Effects ofBarbituratesPharmacological Effects of Barbiturates 1. Depression of the CNS1. Depression of the CNS 2.2. Respiratory DepressionRespiratory Depression 3.3. Enzyme Induction:Enzyme Induction: Barbiturates induceBarbiturates induce P-450P-450 microsomalmicrosomal enzymes in the liver.enzymes in the liver. 1111
- 12. Clinical Uses ofBarbituretes: 1. Anesthesia:1. Anesthesia: Thiopental SodiumThiopental Sodium IVIV to induceto induce general anesthesiageneral anesthesia.. 2. Anticonvulsant:2. Anticonvulsant: PhenobarbitalPhenobarbital -- in long-term management ofin long-term management of Tonic-clonic SeizuresTonic-clonic Seizures Status EpilepticusStatus Epilepticus Eclampsia.Eclampsia. 3. Insomnia.3. Insomnia. 4. Preoperative sedation4. Preoperative sedation 1212
- 13. Adverse Effects ofBarbiturates: 1. Drowsiness, impaired concentration,1. Drowsiness, impaired concentration, mental and physical sluggishnessmental and physical sluggishness 2. Drug hangover2. Drug hangover:: a feeling of tirednessa feeling of tiredness after the patient awakesafter the patient awakes 3. Barbiturates3. Barbiturates induceinduce the P-450the P-450 systemsystem andand maymay the effect of drugs thatthe effect of drugs that are metabolized by these hepatic enzymesare metabolized by these hepatic enzymes 1313
- 14. Poisoning with BarbituratesPoisoningwith Barbiturates I StageI Stage ((Falling AsleepFalling Asleep): slurred speech, sustained): slurred speech, sustained Nystagmus, Somnolence; Apathy, Miosis,Nystagmus, Somnolence; Apathy, Miosis, Bradycardia, Hypersalivation.Bradycardia, Hypersalivation. IIII StageStage ((Superficial ComaSuperficial Coma): un): unconsciousnessconsciousness,, TTachycardia,achycardia, Muscle Hypotonia or Hypertonia,Muscle Hypotonia or Hypertonia, Decrease or Increase of ReflexesDecrease or Increase of Reflexes,, Miosis. Rare and Superficial Breathing,Miosis. Rare and Superficial Breathing, Weak Pulse, Cyanosis,Weak Pulse, Cyanosis, OliguriaOliguria IIIIII StageStage ((Deep ComaDeep Coma): Ar): Areflexiaeflexia,, Absence of Reaction to Painful Stimulation.Absence of Reaction to Painful Stimulation. IVIV StageStage:: ((Post Comatose PeriodPost Comatose Period): Ptosis, Unsteady Gate,): Ptosis, Unsteady Gate, Emotional Lability, Depression.Emotional Lability, Depression. 1414
- 15. Treatment of Poisoningwith Barbiturates Forced Alkaline Diuresis,Forced Alkaline Diuresis, Adequate Fluids, Acid-base Balance CorrectionAdequate Fluids, Acid-base Balance Correction Mannitol, Furosemide (Mannitol, Furosemide (LasixLasix)) Sodium BicarbonateSodium Bicarbonate 4% 500 ml IV4% 500 ml IV Intensive Infusion TherapyIntensive Infusion Therapy withwith Polyglucin, Rheopolyglucin, HemodesPolyglucin, Rheopolyglucin, Hemodes Antidote Therapy:Antidote Therapy: BemegridBemegrid 0.5% 5-10 ml IV or IM0.5% 5-10 ml IV or IM SulfacamphocaineSulfacamphocaine Coffeine-sodium bensoateCoffeine-sodium bensoate Ephedrine hydrochlorideEphedrine hydrochloride CordiamineCordiamine 1515
- 16. VITAMINS:VITAMINS: BB11 6% 5ml,6% 5 ml, BB66 5% 6-8 ml,5% 6-8 ml, BB1212 600 μg600 μg CC 5% 5-10 ml.5% 5-10 ml. ATPATP 1% - 6 ml1% - 6 ml Noradrenaline hydrotartrateNoradrenaline hydrotartrate 0.2% - 1 ml0.2% - 1 ml combined withcombined with DopamineDopamine 4% - 5 ml4% - 5 ml inin PolyglucinPolyglucin (Macrodex)(Macrodex) 400 ml IV infusion400 ml IV infusion 1616
- 17. Drugs Used toTreat EpilepcyDrugs Used to Treat Epilepcy 1717
- 18. ANTIEPILEPTIC DRUGSANTIEPILEPTIC DRUGS I.Delaying the recovery from inactivating NaI. Delaying the recovery from inactivating Na++ channels:channels: CarbamazCarbamazepineepine ((FinlepsinFinlepsin)) OxcarbazepineOxcarbazepine DipheninDiphenin ((PhenytoinPhenytoin)) 1818
- 19. Carbamazepine -Carbamazepine -tab. 0.2 g, 0.4 gtab. 0.2 g, 0.4 g Mechanism of action:Mechanism of action: ItIt blocks Nablocks Na++ channelschannels =>=> Propagation of abnormal impulsesPropagation of abnormal impulses Generation of repetitive action potentialsGeneration of repetitive action potentials in thein the Epileptic FocusEpileptic Focus Clinical Uses:Clinical Uses: PPartial Seizuresartial Seizures (Simple and Complex) -(Simple and Complex) - is theis the Drug of 1Drug of 1stst ChoiceChoice.. Tonic-Clonic SeizuresTonic-Clonic Seizures Trigeminal NeuralgiaTrigeminal Neuralgia 1919
- 20. DipheninDiphenin ((PhenytoinPhenytoin,, HydantoinHydantoin)) - Tab 0.117 g- Tab 0.117 g;; amp. 5%-5 mlamp. 5%-5 ml Mechanism of actionMechanism of action:: Influx of NaInflux of Na++ acrossacross cell membranes in the motor cortex duringcell membranes in the motor cortex during generation of nerve impulsesgeneration of nerve impulses Adverse effectsAdverse effects:: Gingival Hyperplasia,Gingival Hyperplasia, Nystagmus,Nystagmus, Ataxia.Ataxia. NystagmusNystagmus - involuntary movement of the eye- involuntary movement of the eye comprising a Smooth Drift followed bycomprising a Smooth Drift followed by a Flick Backa Flick Back 2020
- 21. Teratogenic EffectsTeratogenic Effectsofof DipheninDiphenin FETAL HYDANTOIN SYNDROMEFETAL HYDANTOIN SYNDROME CLEFT LIPCLEFT LIP (harelip)(harelip) CLEFT PALATECLEFT PALATE CONGENITAL HEART DISEASECONGENITAL HEART DISEASE SLOWED GROWTHSLOWED GROWTH MENTAL DEFICIENCYMENTAL DEFICIENCY 2121
- 22. II. GABA-mimetics:II. GABA-mimetics: 1.Stimulating GABA-ergic transmission:1. Stimulating GABA-ergic transmission: Sodium OxybutyrateSodium Oxybutyrate ((Sodium oxybateSodium oxybate)) 2. Activating GABA Receptors:2. Activating GABA Receptors: BARBITURATES, BENZODIAZEPINESBARBITURATES, BENZODIAZEPINES 3. Inhibiting GABA-transferase and3. Inhibiting GABA-transferase and GABA synthesis:GABA synthesis: Sodium ValproateSodium Valproate 4. Releasing GABA from neuronal endings:4. Releasing GABA from neuronal endings: GabapentinGabapentin 5. Inhibiting GABA transaminase:5. Inhibiting GABA transaminase: VigabatrineVigabatrine 6. Inhibiting GABA reuptake:6. Inhibiting GABA reuptake: TiagabineTiagabine 2222
- 23. ● VALPROATE SODIUM(DEPAKIN ) Tab. 0.3 g; Syrup 5%-120 ml a Stimulator of GABA-ergic Processes Mechanism of action:Mechanism of action: ● Inhibits GABA-transferaseInhibits GABA-transferase ● GABA synthesis =>GABA synthesis => Brain Levels of GABA Propagation of abnormal electrical discharge Adverse effects: ataxia, tremor, rash, Hepatic toxicity, Alopecia, Bleeding time 2323
- 24. III.III. Inhibiting ExcitatoryNeurotransmittersInhibiting Excitatory Neurotransmitters andand NMDA-receptorsNMDA-receptors:: LamotrigineLamotrigine IV.IV. Low threshold (T-current) CaLow threshold (T-current) Ca2+2+ channelschannels in the thalamic neurons:in the thalamic neurons: EthosuximideEthosuximide TrimethineTrimethine ((TrimethadioneTrimethadione)) 2424
- 25. ● LAMOTRIGINE Tab.0.05 and 0.1 g an Inhibitor of Exciting Amino Acids – GLUTAMATE, ASPARGINATE Mechanism of action:Mechanism of action: Inactivates voltage-sensitive Na+ Channels ⇒ Inhibits the Release of GLUTAMATE ASPARGINATE - Exciting Neurotransmitters 2525
- 26. Classification of EpilepsyClassificationof Epilepsy 1. PARTIAL:1. PARTIAL: a.a. SimpleSimple PartialPartial b.b. ComplexComplex PartialPartial 2. GENERALIZED:2. GENERALIZED: a.a. Tonic-clonicTonic-clonic ((Grand malGrand mal)) b.b. AbsenceAbsence ((Petit malPetit mal)) c.c. MyoclonicMyoclonic d.d. Febrile SeizuresFebrile Seizures e.e. StatusStatus EpilepticusEpilepticus 2626
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- 28. Seizure TypeSeizure Type1st Choice1st Choice 2nd Choice2nd Choice Focal SeizuresFocal Seizures CarbamazepineCarbamazepine DifeninDifenin ClonazepamClonazepam LamotrigineLamotrigine Valproate NaValproate Na GeneralizedGeneralized SeizuresSeizures ((GRAND MALGRAND MAL)) CarbamazepineCarbamazepine DipheninDiphenin Valproate SodiumValproate Sodium ClonazepamClonazepam LamotrigineLamotrigine StatusStatus EpilepticusEpilepticus DiazepamDiazepam DipheninDiphenin Sodium OxybutyrateSodium Oxybutyrate PhenobarbitalPhenobarbital AbsenceAbsence ((PETIT MALPETIT MAL)) EthosuximideEthosuximide Valproate SodiumValproate Sodium LamotrigineLamotrigine TrimethineTrimethine 2828
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- 30. ANTIPARKINSONIAN ANGENTSANTIPARKINSONIAN ANGENTS I.I. Activating Dopaminergic Influences Activating Dopaminergic Influences:: 1. Precursors of Dopamine1. Precursors of Dopamine:: LevodopaLevodopa ( (Tab.0.25 and 0.5 gTab. 0.25 and 0.5 g)) •• Combined agents: Combined agents: SinemetSinemet ( (NakomNakom)) MadoparMadopar 2. D-receptor agonist2. D-receptor agonist:: BromocriptineBromocriptine ((tab. 2.5 mgtab. 2.5 mg)) 3. MAO-B inhibitors3. MAO-B inhibitors:: DeprenilDeprenil ( (SelegelineSelegeline – – tab. 5 mgtab. 5 mg)) 3030
- 31. LevodopaLevodopa (( L-DOPA,DoparL-DOPA, Dopar )) -- aa Laevorotatory Isomer ofLaevorotatory Isomer of DOPADOPA ((Dihydroxy-Phenylalanine)Dihydroxy-Phenylalanine) –– a precursor ofa precursor of DopamineDopamine MAMA: Stimulates the: Stimulates the DD22 receptorsreceptors in the basal gangliain the basal ganglia =>=> Improves modulation ofImproves modulation of Voluntary Nerve ImpulsesVoluntary Nerve Impulses transmittedtransmitted to the motorto the motor cortexcortex =>=> Relieves all major symptoms, esp.:Relieves all major symptoms, esp.: AkinesiaAkinesia ((inabilityinability ofof voluntary movementvoluntary movement)) Rigidity andRigidity and BradykinesiaBradykinesia ((Slowness of movementSlowness of movement)) AkathisiaAkathisia ((the inability to sit still because ofthe inability to sit still because of uncontrollable movementuncontrollable movement)) TremorsTremors =>=> Improves Mood and MemoryImproves Mood and Memory 3131
- 32. Adverse effect ofAdverseeffect of Levodopa:Levodopa: Anorexia, VomitingAnorexia, Vomiting Cardiac ArrhythmiasCardiac Arrhythmias Orthostatic HypotensionOrthostatic Hypotension Aggressive BehaviorAggressive Behavior SeizuresSeizures Hallucinations,Hallucinations, Confusion, DeliriumConfusion, Delirium Dyskinesia –Dyskinesia – InvoluntaryInvoluntary Repetitive MovementsRepetitive Movements - i- in up to 80% of patientsn up to 80% of patients 3232
- 33. CarbidopaCarbidopa andand BenserazideBenserazide-- inhibitors ofinhibitors of DOPA decarboxylase –DOPA decarboxylase – do not penetrate the Blood-Brain barrierdo not penetrate the Blood-Brain barrier =>=> lessless LevodopaLevodopa is decarboxylatedis decarboxylated in peripheral tissuesin peripheral tissues => more=> more LevodopaLevodopa reaches the brain wherereaches the brain where it is decarboxylated toit is decarboxylated to DOPAMINEDOPAMINE => much smaller doses of=> much smaller doses of LevodopaLevodopa can be given.can be given. 3333
- 34. SinemetSinemet (Nakom) :(Nakom): LevodopaLevodopa 100 mg +100 mg + CarbidopaCarbidopa 25 mg25 mg MadoparMadopar :: LevodopaLevodopa 100100 oror 200 mg +200 mg + CarbidopaCarbidopa 25 mg25 mg oror 50 mg50 mg respectivelyrespectively 3434
- 35. BromocriptineBromocriptine, an, anergotamineergotamine derivative, isderivative, is aa DOPAMINE receptor agonistDOPAMINE receptor agonist.. The actions ofThe actions of BROMOCRIPTINEBROMOCRIPTINE are similar toare similar to those ofthose of LEVODOPALEVODOPA,, except thatexcept that Hallucinations, Confusion, Delirium, Nausea, andHallucinations, Confusion, Delirium, Nausea, and Orthostatic HypotensionOrthostatic Hypotension are more common,are more common, whereaswhereas DyskinesiaDyskinesia is less prominent.is less prominent. In psychiatric illness it causes the mental conditionIn psychiatric illness it causes the mental condition to worsen.to worsen. In patients with peripheral vascular diseaseIn patients with peripheral vascular disease a worsening of the vasospasm occursa worsening of the vasospasm occurs in patients with peptic ulcer, there is a worsening ofin patients with peptic ulcer, there is a worsening of the ulcer.the ulcer. 3535
- 36. Thank You forAttentionThank You for Attention!! 3636