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1. HYPNOTIC, ANTIEPILEPTIC &HYPNOTIC, ANTIEPILEPTIC &
ANTIPARKINSONIAN DRUGSANTIPARKINSONIAN DRUGS

2. HYPNOTICHYPNOTIC DRUGSDRUGS
I.I. Benzodiazepine Receptor 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
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3. II.II. Hypnotics with Narcotic 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
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7. MECHANISM OF ACTION of 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
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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
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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
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11. Pharmacological Effects of BarbituratesPharmacological 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.
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12. Clinical Uses of Barbituretes:
 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
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13. Adverse Effects of Barbiturates:
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
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14. Poisoning with BarbituratesPoisoning with 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 Poisoning with 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% 5 ml,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
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17. Drugs Used to Treat EpilepcyDrugs Used to Treat Epilepcy
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18. ANTIEPILEPTIC DRUGSANTIEPILEPTIC DRUGS
I. Delaying the recovery from inactivating NaI. Delaying the recovery from inactivating Na++
channels:channels:
CarbamazCarbamazepineepine ((FinlepsinFinlepsin))
OxcarbazepineOxcarbazepine
DipheninDiphenin ((PhenytoinPhenytoin))
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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
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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 Effects ofof 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
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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
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24. III.III. Inhibiting Excitatory NeurotransmittersInhibiting 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))
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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
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26. Classification of EpilepsyClassification of 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
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28. Seizure TypeSeizure Type 1st 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
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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))
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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
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32. Adverse effect ofAdverse effect 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
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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.
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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
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35. BromocriptineBromocriptine, an, an ergotamineergotamine 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.
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36. Thank You for AttentionThank You for Attention!!
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