Presentation class on Drugs used on central Nervous System for the PCL Nursing first year in Nepal . Content of CNS Drugs and its mechanisam and use

1. DRUGS ACTING ON CNS
DR. SAROJ SUWAL

2. DRUGS
• Anesthetic drugs
• Analgesics
• Sedative and hypnotics
• antipsychotic
• Antiepileptic drugs

3. ANESTHETIC DRUGS
• In the “old days” the following were used for anesthesia.
• – Alcohol
• – Ice for numbing
• – Blow to the head
• – Strangulation
Drugs which cause
• loss of sensation (especially Pain)
• Sleep ( unconsciousness)
• muscular relaxation
• Loss of reflex activity

4. TYPES OF ANESTHESIA DRUGS
• Local Anesthesia Drugs
• General Anesthesia Drugs

5. LOCAL ANESTHETICS
•are drugs that
cause
• reversible loss of
sensory
perception,
especially of pain,
in a restricted
area of the body.
Local
Anesthetics
Blocks
sensory
afferent
Prevent
reflex &
Pain relief

6. LOCAL ANESTHESIATYPES
• Surface/topical Anesthesia
• local injection
• Conduction Anesthesia( nerve blocks)

7. SURFACE ANESTHESIA
• Local application to mucus
surface or wound
• Anesthesia act on Nerve Ending
• Topical application
• Spray application
• Lignocaine, xylocaine, lozenges
With epinephrine → longer time of anesthetic
effect

8. MOA OF LA
Nerve conduction is blocked.
Potassium ions also cannot flow out
Slowing of conduction.
Inhibit Na+ ions in nerve cytoplasm
Local Anesthesia
block generation and conduction of nerve impulse
in all parts of the neuron

9. LIDOCAINE (LIGNOCAINE)
• Most widely used Local anesthetics
• versatile LA→Used plain or with adrenaline
• Duration of action→ intermediate( 1-2 hrs.)
• Onset of action→ 3 mins
• Vasodilatation occurs in the injected area.
• 2%, 4%,
• Better than porcaine
• Duration→ 2%→ 100 mins

10. BUPIVACAINE
• Has long duration of action
• 0.5 % anesthesia occurs in 2-10 mins and duration up
to 7 hrs
• In epidural
• →0.75% with dextrose onset within one min and motor blockade→ 15
min
• Duration 2 hrs
• Complete return average→ 3-5 hrs

11. INDICATION
• surface application,
• infiltration,
• Nerve conduction block,
• Epidural, spinal block
• Intravenous Regional block
anesthesia.
• Used as popular antiarrhythmic

12. ADVERSE EFFECTS
• CNS toxicity
• Systemic absorption→excitement,
tremors, shivering,
• If absorbed in higher amounts →
can lead to depression( coma,
respiratory arrest, death)

13. OVERDOSE
• muscle twitching,
• convulsions,
• cardiac arrhythmias,
• fall in BP,
• Anxiety, restlessness
• Status asthmatics
• coma and
• respiratory arrest
.

14. • Cardiovascular toxicity
• Depression of cardiovascular system
• Hypersensitivity
• Rashes to anaphylaxis
• Local Reactions
• Combination with vasoconstrictors should be
avoided to feet, fingers, toes, pinna, penis

15. CONTRAINDICATION
• Heart block
• Severe sinoatrial block
• Myasthenia gravis
• Serious adverse reaction
• Treatment with quinidine(class I antiarrhythmic
agent)
• Cautions with adrenaline
• to end arteries places
• Hypertensive

16. NURSING CONSIDERATIONS
• Monitor BP and ECG constantly
• Assess respiratory and neurologic status frequently to
avoid potential overdosage and toxicity
• Watch for neurological toxicity( drowsiness, dizziness,
confusion, visual disturbance, excitement, behavioral
changes
• Blood level more than 7mcg/ml are toxic( so w/f iv
lidocaine
• Can interfere swallowing reflex → so ingest food after
60 mins

17. GENERAL ANESTHETICS
• drugs which produce reversible loss
of all sensation and consciousness.
Features:
• Loss of all sensation, especially pain
• Sleep (unconsciousness)
• amnesia
• Immobility and muscle relaxation
• Stoppage of somatic and autonomic reflexes

18. STAGES OF GENERAL ANESTHESIA
• Stage I
• Stage of Analgesia(induction)
• Stage II
• Stage of Delirium and Excitement
• Stage III
• Stage of Surgical Anesthesia
• Stage IV
• Medullary Paralysis

19. GENERAL ANESTHESIA CLASSIFICATION
Inhalational
Gas: Nitrous Oxide,
Volatile Liquid: Ether, Halothane, Enflurane
Injectable
Induction:Thiopentone sod. , Methohexitone sod., Propofol
Maintenance: Benzodiazepines, Diazepam, Lorazepam,
Midazolam
Dissociative Anaesthetic
Ketamine, Opioid analgesia, Fentanyl

20. NITROUS OXIDE:LAUGHING GAS
• low potency, therefore must be combined with other
agents
• rapid induction and recovery
• – good analgesic,WEAK anesthetic properties
• – risk of bone marrow depression with prolonged
administration.
• Can retard O2 uptake during recovery( diffusion
hypoxia), thus 20% of O2 is always needed

21. DIETHYL ETHER
• Ethyl ether or sulfuric ether
• Highly volatile inflammable so not so used now a days
MOA
• Output of nerve ending decrease → Produce good anesthesia and muscle
relaxation
Adverse effect
• Acidosis, dehydration,
• Has narcotic effect→ so psychological addiction
• Post marked → anesthetic nausea, vomiting,retching

22. HALOTHANE
• volatile liquid with sweet odor,
nonirritant and noninflammable.
• Highly potent
• Recovery is rapid
• Used for induction and
maintenance during major
surgery

23. MECHANISM OF ACTION:
HALOTHENE
potentiates
GABA action
on GABAA
receptors
opens K+
channels
reduce
neuronal
activity,
especially in
cerebral
cortex,
thalamus and
hippocampus.

24. DISADVANTAGES
• Expensive
• Cause respiratory and cardiac depression
• Crossed placental barrier and depress fetal respiration
• hepatotoxic

25. ISOFLURANE
• Does NOT induce cardiac arrhythmias
• Stable molecule
• Induction dose is 1.5 – 3%
• maintenance dose is 1 – 2%
• Disadvantages:
• – More pungent odor than halothane
• – Progressive respiratory depression & hypotension

26. DESFLURANE AND SEVOFLURANE
• – similar to isoflurane
• – have faster onset and recovery
• – lack of respiratory irritation
• – commonly used clinically

27. IV ANESTHETICS
•Intravenous:
• Inducing agents:
• Thiopentone, Methohexitone sodium, propofol
and etomidate – Benzodiazepines (slower acting):
Diazepam, Lorazepam, Midazolam
• Dissociative anaesthesia: Ketamine
• Neurolept analgesia: Fentanyl

28. DIAZEPAM
• Long acting benzodizepam
• Sedative, hypnotic and
anxiolytic anti-convulsant and
muscle relaxant
• MOA
• depresses all levels of the Central
Nervous System through the
increased action of gamma-
aminobutyric acid (GABA)

29. DOSE AND USES
• Anxiety and muscle relax
• 2-10 mg orally 2-3 times daily
• Insomnia
• 5-10mg orally at bed time
• Alcohol withdrawal, panic attack, sever anxiety
• 10mg IM slowly or IV 4 hrly
• Child→ sedation, muscle relax, anxiety→ 0.1-0.3 mg/day
TDS
• Status epilecticus
• 0.15-0.25mg/kg dose

30. CONTRA INDICATIONS
•Acute pulmonary insufficiency
•Respiratory depression
•Chronic psychosis
•Precaution
• Pregnancy, lactation, elder ppl,
• respiratory disease
• Muscle weakness

31. THIOPENTONE SODIUM
• Ultra short acting barbiturate→Sedation and
hypnosis
• highlyWater soluble –
• Use for induction→ Consciousness lost in 10-20 sec
and retunes in 10-20 mins
• MOA: inhibitory of neurotransmitter GABA and
GABAa
• Cause dose related respiratory depression
• Uses for
• Induction of GA
• Anesthesia for Short duration
• seizure

32. • Hepatic metabolism (elimination half-life 7-12 hrs)
• - CNS depression persists for long (>12 hr)
• Side effects of Thiopentone:
• • Pre-anaesthetic course – laryngospasm
• • Noncompatibility - succinylcholine
• • Tissue necrosis--gangrene
• • Post-anaesthetic course - analgesic

33. KETAMINE
• Dissociative anesthesia,
• Rapidly acting
• Somnolent effect→ awake but no pain
• HAS short-term amnesia.
• Cause transient depression of respirator center
• Cause increase in systolic and diastolic bp and heart
rate
• Dose: 5-10mg/kg im or 1-2mg i.v.

34. • Route
• I.v. or i.m. admin.
• Rapid onset and short duration
of action following i.v. dosing.
• Short surgical procedures
• burn dressing, forceps delivery, breech
extraction manual removal of placenta
and dentistry
• Combination with diazepam -
angiography,
• cardiac catheterization
• OPD surgical procedures

35. SIDE EFFECT
• Delirium
• Hallucination
• Increased salivation
• Contraindications
• Epilepsy
• Htn
• Inscrease intracranial pressure
• Gloucoma
• alocholism

36. PROPOFOL
– rapidly metabolized
– very rapid recovery; no cumulative effect
– useful for day-case surgery
– causes more respiratory and cardiovascular depression
than barbiturates
– Lowers intracranial pressure

37. FENTANYL
• Neuroleptic agent or anypsychotics or tranquilizers
• Dosage Forms
• IV
• patch (Duragesic)
• Used extensively for open-heart surgery due to lack of
cardiac depression
• Opioid analgesic
• Suppression of vomiting and coughing
• • Duration of action: 30-50 min.

38. • USES:
• - in combination with diazepam
• used in diagnostic, endoscopic and angiographic
procedures
• - Adjunct to spinal and nerve block anaesthesia

39. ADVERSE EFFECTS:
• Increased heart rate and blood pressure (by activation
of sympathetic system).
• Involuntary muscle movement.
• Hallucinations, delerium and dysphoria during recovery.
• Respiratory depression in overdose.
• Nausea vomiting in wake up

40. COMPLICATIONS OF GENERAL ANAESTHESIA
A. During anaesthesia
1. Respiratory depression and hypercarbia.
2. Salivation, respiratory secretions—
3. Cardiac arrhythmias, asystole.
4. Fall in BP
5. Aspiration of gastric contents: acid pneumonitis.
6. Laryngospasm and asphyxia.
7. Awareness: dreadful perception and recall of events during
surgery—by use of light anaesthesia + analgesics and muscle
relaxants.
8. Delirium, convulsions and other excitatory effects are generally
seen with i.v. anaesthetics.

41. ANALGESICS AND ANTI INFLAMMATORY
DRUGS
• Analgesics
• Durgs used to treat pain or relief pain
• Anti-inflammatory Drug
• Drugs used to decrease inflammation
Types of analgesics
• opioid analgesic
• Opioids are substances that act on opioid receptors to produce morphine-l
effects
• Non opioid analgesic

42. OPIOID ANALGESICS
❑Narcotic analgesics
❑Are pain reliever that act on CNS
MOA
Opioids produce analgesia by binding to
specific G protein coupled receptors in brain
& spinal cord

43. OPIOID CLASSIFICATION
A.Strong agonist:
a. Morphine
b. Meperidine
c. Methadone
d. Heroin
e. Fentanyl
B. Moderate agonist:
a. Propoxyphene
b. Codeine
C.Antagonist:
a. Naloxane, Nalrexone.

44. EFFECTS
• • Analgesia
• • Most powerful analgesics,
• • Morphine, methadone, meperidine, fentanyl, heroin
• • Sedation and euphoria
• • Respiratory depression
Action at medulla lead to respiratory depression.
• • Antitussive effects
Suppression of the cough reflex
• • Nausea & vomiting
• • Activation of chemoreceptor trigger zone

45. CLINICAL USES
• • Analgesia- Fentanyl, morphine
• • Cough Supression- Codeine, Dextromethorphan.
• • Antidiarrheal- Diphenoxylate, Loperamide
• • Acute Pulmonary edema- Morphine
• • Anesthesia- Fentanyl
• • Opioid Dependence- Methadone

46. SIDE EFFECTS
• • GI effects
• Constipation with decreased intestinal peristalsis.
• • Smoot muscle
• Cause contraction of billiary billiary tract SM, inc. ureter and bladder
tone, red. Uterine tone (prolong labor)
• • Miosis
• •Tolerance
• • Dependence

47. CONTRAINDICATIONSTO USE
• Respiratory depression
• Chronic lung disease
• Chronic liver or kidney disease
• Increased intracranial pressure
• Hypersensitivity reactions

48. MORPHINE
• CNS DEPRESSANTS CAUSING
ANALGESIA AND HYPNOSIS
• Peak occurs in
• 50-90 mins in S/C, 30-60 mins in I/M and 20 Mins in
IV
• MOA
• Raises the Pain threshold
• Modify emotional reaction to pain
• Inhibit pain impulse across pain pathway in CNS

49. INDICATIONS
• Sever acute or chronic pain
• Pre anesthetic medicine
• Acute pulmonary edema/LVF
• Drug of choice for pain in Myocardial infraction

50. DOSE AND PREPARATION
• s/c or i/m10 mg for adult (repeated 4 hrs. if required)
• IV→ 2.5 to 10 mg slowly at rate of 2mg/min
• Contraindications
• Respiratory depression
• Head injury
• Increased intracranial pressure
• Severe hepatic impairment
• Convulsive disorders

51. ADVERSE EFFECTS
• Drowsiness
• Nausea vomiting
• Constipation
• Respiratory depression
• Hypotension
• Urinary retention
• Rashes
• Mood changes
• Hallucination
• dependence

52. NURSING INDICATIONS
• Count respiration rate before giving drug( if ,12 <
notify)
• Avoid prolong use → drug dependence occurs
• Sudden position change cause postural hypotension→
change position slowly

53. PENTAZOCIINE
• Analgesic and
• very weak opiate antagonistic effects
• Oral, im, sc
• Peak occurs at 1-3 hours in oral , 1 hrs in im,
• Onset → 2-3 mins
• Inidication
• Moderate to severe pain
• Dose→ 25-100 mg after meal ( 4 hrly if need)

54. • Vomiting more frequent than morphine
• Contraindications
• Head injury
• Raised ICP

55. PETHIDINE
• Usually I/M
• If IV → slowly or via infusion
• More rapid onset and shorter duration of action than
morphine
• Indication
• Moderate to severe pain
• Dose
• Adult→ i/m→ 25-100mg ( rpeated after 4 hrs if required)
• Child→0.5-2mg/kg IM

56. ADVERSE EFFECT
• Nausea
• Hypotension
• Constipation
• Urinary retentions
• Respiratory depression

57. CODEINE PHOSPHATE
• less potent than morphine
• degree of analgesia is comparable to aspirin
• (60 mg codeine ~ 600 mg aspirin);
• can relieve mild to moderate pain only.
• more selective cough suppressant

58. USE
• Mild to moderate pain
• Cough suppressant ( for non productive cough
• Codeine has been used to control diarrhea.
• Constipation is a prominent side effect when it is used
as analgesic.

59. DOSE
•For analgesia
• 30-60mg every 4-6 hrly
• Children→0.5-1mg/kg every 4-6 hourly
•Antitussive
• Adult→ 10 -20mg 4-6 hrs
• Child(6-11 yrs)→ 5-10mg/kg every 4-6 hrly
• Child(2-5 yrs)→ 2.5-5mg/kg every 4-6 hrly

60. SIDE EFFECT
• Constipation
• Drowsiness
• Nausea
• Vomiting
• Decrease urination
• Facial flushing
• Blurred vision
• Dry mouth
• hypotension

61. PROPOXYPHENE HYDOROCHOLROIDE
• Opoids agonist come with combination with
acetaminophen
• Use for muscle pain( mild to moderate pain)

62. NON OPIATE ANALGESIC/ANTIPYRETICS
• Paracetamol
• Ibuprofen
• Aspirin
• indomethacin,
• Piroxicam
• Ketorolac
• Nimusline

63. PARACETAMOL
• Analgesic and anti pyretic agent
• Has very less antiinflamatory effect
• PCM>10 gm → cause toxicity
• MOA
• Reduce temperature by resetting the temperature regulating center to
normal in brain
• Blocks pain center in thalamus
• Inhibit the synthesis of prostaglandings
• Doesn’t affect platelet function
• increase blood clotting time

64. INDICATIONS PREPARATION AND DOSE
• Fever
• Mild to mod. Pain
• Preparations
• 500mg tabs, liquid 125mg/5ml and drops →150ml/1ml
• Dose
• 500mg to 1 grm PO 3-4 times daily
• Child :15mg/kg/day x 6 hourly

65. CONTRAINDICATION AND ADVERSE EFFECTS
•Hepatic and renal dysfunction, anemia
•Adverse effect
• Skin rash and allergic reaction
• Rarely blood disorder
• Nephropathy
• Liver damage on prolong used

66. NURSING CONSIDERATION
• Urine may be dark, reddish color→ infrom others
• Poisioning may occur if taken more than 10gm
• Keep medicine above children
• Tell pt not to take PCM with other NSAIDS on regular
basis
• Drug not use more than 10 days

67. IBUPROFEN
• Commonly used NSAID
• Has
• Weaker than other NSAID but usually beter tolerated
than aspirin
• Indiciations
• RA, Osteoarthritis
• ENT disease,
• And all other moderate type of pain

68. COMBINATION AND DOSE
• Combination :
• Ibuprofen 400mg +PCM 500mg
Usual dose
• Orally after food→1200 to 1800 mg per day in 3 or 4
divided dose
• Daily dose of 600 to 1200 mg may be adequate for
maintainance
• Child→ not recommended under 7 kg
• 20mg/kg /day in divided dose

69. ASPIRIN( ACETYL SALICYLIC ACID
•Analgesic, antipyretics and antiinflaatory
•MOA
• Analgesics→ blocks pain center in thalamus
• Inhibit synthesis of prostaglandin
• Inhibits pain mediators
• Antiinflamatory :
• Anti pyeretic→ reduce temperature by decrease
temperature set point
• Anti platelates→ inhibit platelet aggregration,
inhibit PG and thromboxane A2

70. INDICATION
• Analgesic,
• Joint pain
• Myalgia
• Toothache
• Neuralgia
• Dysmenorrhea
• Acute rheumatic fever

71. PREPARATION AND DOSE
•Tablet→ tablet 300mg, 50 mg, 75 mg,
150mg
•Dose
• 300 to 1gm for adult (4-6 hourly)
• Chidl → orally after food
• 30-100mg/kg /day 6 hrly
• Shouldn’t’ given under 12 yrs

72. CONTRAINDICATION
• Children <12

73. ADVERSE EFFECT
• Nausea
• Dyspepsia
• Gi bleed
• Tinnitus
• Vertigo
• thromocytopenia

74. SEDATIVES AND HYPNOTICS DRUGS

75. • Drugs used to reduce tension and
anxiety
• Induce calm
❖In larger doses →produce hypnosis
❖Site of action → limbic system which
regulate thought and mental function
SEDATIVES DRUGS

76. HYPNOTICS
❖drug that induces and maintains sleep,
❖Reduce tension and anxiety
❖Used for initiation and maintenance of
sleep
❖In higher doses produce general
anesthesia
❖Site of action is
❖midbrain and ascending RAS which maintain
wakefulness

77. INSOMNIA & SLEEP. → SEDATIVE AND
HYPNOTICS
Sleep Pattern
• REM Sleep:
• Rapid eye movement
• NON-REM sleep:
• Non Rapid Eye Movement Sleep

78. NREM AND REM
➢Is dreamless sleep
➢Brainwaves in EEG→
➢Slow and High voltage,
➢breathing and
➢heart rare slow
➢Blood pressure low
➢This sleep occurs when dream
occurs
➢Characterized by :
➢Rapid and low brain waves
➢Irregular breathing and
heart rate
➢ Involuntary muscle jerks
➢We have 3 to 5 REM sleep per night
➢Occurs at interval of 1-2 hrs
➢Variable in length of time

79. STAGES OF SLEEP

80. CLASSIFICATIONS

81. BARBITURATES
• derivative of barbituric acid
• non selective CNS depressants

82. PHENOBARBITONE
• Commonly used barbiturates
• Have sedative, hypnotic and
anticonvulsant action
• Dangerous toxic effect if overrode
used in the emergency
treatment of convulsions
as in status epilepticus.

83. MECHANISM OF ACTION
Inhibit neuronal uptake
of GABA
Stimulate GABA
Depress
CNS

84. MECHANISM OF ACTIONS

85. •REM sleep is suppressed
•Depress respiration by neurogenic,
chemical or hypoxic drive
•Cause hypotension
• Due to direct myocardial andVMC depression
• Hypoxia
• Sympathetic blockade

86. USED FOR
• Sedation
• Relief of anxiety
• Amnesia
• Hypnosis
• Anaesthesia
• Coma
• Seizure
❑drug of choice → young children with
recurrent febrile seizures.
❑can depress cognitive performance in children

87. PREPARATION AND DOSE
• 10mg, 30mg, 60 mg tablets
• 100mg, 200mg/ml in 2 ml ampoule
• Usual Dose
• 60-180mg per day PO at HS
• Child→ 3-6mg/kg/day Po in BD or OD

88. ADVERSE EFFECT
➢ drowsiness, impaired concentration
➢ Hangover, confusion
➢ Hypersensitivity
➢ Restless
➢ osteomalacia
➢ Tolerance and Dependence
Physical dependence:
➢ withdrawal cause tremors, anxiety, weakness,
restlessness, nausea and vomiting, seizures, delirium,
and cardiac arrest.

89. CONTRAINDICATIONS
• Severe respiratory depression
• Severe renal or hepatic dysfunction
• Severe myocardial disease

90. NURSING MANAGEMENT
• Watch for overdose
• Take care for the physical dependence and tolerance
• Patient should be informed that drugs shouldn’t be
stopped suddenly and need tapering
• Sudden withdrawal → status epilepticus(seizure ) occur
• Patient informed that alcohol and barbiturate enhance
each other
• Deep IM in large muscle
• Long term therapy cause→ folic acid or vitamin D
deficiency

91. BENZODIAZEPINES
▪ produce Dose dependent action of sedation, hypnotic, and tranquilizer
▪ Hypnotic doses do not affect respiration or cardiovascular functions.
▪ They have lower abuse liability:
▪ tolerance is mild, psychological and physical dependence and withdrawal
syndrome are less marked.
▪ Antagonist→ flumazenil

93. MOA
Benzodiazepine
act very selectively on
GABAA receptors,
fast inhibitory synaptic
response
sedative, hypnotic (sleep-inducing),
anxiolytic (anti-anxiety),
anticonvulsant, muscle relaxant

94. USES
1. Reduction of anxiety and aggression :
• affects the hippocampus and nucleus amygdalae
2. Sedation and induction of sleep
3. Anticonvulsant and antiseizure
4. Muscle relaxation
• relax contracted muscle in joint disease or muscle spasm.
5. Other effects
• lead to temporary amnesia
• depress respiratory and cardiovascular function

96. ADR
❑On hypnotic doses
❑ dizziness, vertigo, ataxia, disorientation, amnesia, prolongation of reaction time—
impairment of psychomotor skills
❑Hangover is less common,
❑Weakness, blurring of vision, dry mouth and urinary incontinence
❑Tolerance gradually
❑Cross tolerance to alcohol and other CNS depressants occurs.
❑Anxiety, insomnia, restlessness, malaise, loss of appetite, bad dreams is all that occurs in
most cases.
❑ Panic reaction, tremors and delirium are occasional

97. BENZODIAZEPINE ANTAGONIST:
FLUMAZENIL
▪ Reverses depressant or stimulant effects
▪ IV INFUSION
▪ 1 mg flumazenil OVER 1-3 minutes
▪ usually is sufficient to abolish the effects of therapeutic doses of
benzodiazepines.
▪ If Overdose
▪ cumulative dose of 1-5 mg given over 2-10 minutes;
▪ If no Response on 5 mg flumazenil
▪ strongly suggests that a benzodiazepine is not the major cause of
sedation.

98. ANTIPSYCHOTICS DRUGS
• Neuroleptics drugs
• drug reduce nervous tension by depressing nerve functions
• Major tranquilizer
• drug used to reduce mental disturbance
• Classifications
• Phenothiazines
• Chlorpromazine
• Non Phenothiazines
• haloperidol

100. CHLORPROMAZINE
• Major tranquilizer
• Cause more sedation
• Used in mental deteriorations in older patients
• Depress emesis
• control intractable hiccups

101. MOA
• Reduce incoming sensory stimuli by
acting on brain stem reticular
formation
• Blocks →Nor adrenaline, dopamine
and 5HT
• Decrease sympathetic activity in
hypothalamus

102. INDICATIONS
• Schizophrenia
• Aggressive behavioral disorder
• Anti emetic
• Anti hiccup
• Muscle relaxant in tetanus
• Senile psychosis
• Manic depressive psychosis

103. PREPARATIONS AND DOSE
• 10mg, 25mg, 50mg, 100mg
• Syrup→ 25mg/5ml, 5mg/5ml
• Injections→ 25mg/ml in 2 ml ampule
Dose
• Adult
• Initial dose→75mg/day inTDS or single dose at night time
• Maintenance dose→ 75-300mg/day
• IM dose→ 25-50mg deep IM 6-8 hourly
• Child
• 2-4mg/kg/day PO
• IM→ 3 divided dose

104. CONTRAINDICATIONS
• Bone marrow depression
• Coma
• Severe liver or kidney disease
• Cardiac failure
• Parkinsonism
• Epilepsy
• BPH
• Hypothyroidism

105. ADVERSE EFFECT
• Marked sedation
• Extrapyramidal syndrome
• Tardive dyskinesia
• Antimuscarinic effects
• Psychological disturbance
• Convulsion
• hypothermia
stiff, jerky movements of your
face and body that you can't
control

108. NURSING MANAGEMENTS
• Avoid direct sunlight
• IM deeply and slowly
• Should remain in supine at least 1 hours to prevent
orthostatic hypotension
• Watch for constipationa nd urinary retension
• Watch for GI problems
• Urine color may be pink to red-brown
• Caution patient not to stop medicine abruptly
• No driving and working in machinery area which acquire
mental alertness

109. HALOPERIDOL
• Used to treat psychotic disorder
• Alters the effects of dopamine in
CNS
• So has
• anti cholinergic effects
• alpha adergenic blocking activity

111. INDICATIONS AND CONTRAINDICATIONS
• iNDICATIONS
• Acute and chronic psychotic disorder
• Schizophrenia, manic state, drug induced psychosis
• Managing aggressive and agitated patients
• Severe behavioral problem in children
• Short term treatment of hyperactive children
• CONTRAINDICATIONS
• Parkinsonisam
• Lactation
• Narrow angle glaucoma
• Bone marrow depression

112. DOSE AND PREPRATIONS
Preprations
• Tablets 0.5mg, 1mg, 2mg, 5mg, 10 mg
• Injections (haloperidol deconate):50mg/ml, 100mg/ml
Dose
• 0.5mg-5mg BD or TDS with severe symptomea
• May up to 100mg
• IV→ 0.5 to 5mg repetead every 30 min

113. SIDE EFFECTS
• CNS
• Extrapyramidal reaction
• Confustion
• Drowsiness
• Tardive dyskinesia
• EYE
• Blurred vision
• Dry eyes
• Respiratory
• Respiratory depression
• CVS
• Hypotension
• tachycardia
• GI
• Constipation, dry mouth, anorexia
• Others
• Urinary retetnions
• Anemia
• Hypersensitivity reaction

114. EXTRA PYRAMIDAL EFFECTS

115. ANTI DEPRESSANTS
• Drugs used for depressive disorders which are caused
by emotional or environmental disorders
• Commonly used drugs
• Imipramine,
• nortriptyline,
• amitryptiline
• doxepin,
• fluoxetine
• duloxetine

117. IMIPRAMINE
• TCA antidepressants
• also reduce symptoms of agitation and anxiety
• MOA
• Potentiate the effects of serotonin and nor epinephrine
• Has significant anticholinergic effects
• Contraindication
• Hypersensitivity
• Pregnancy and lactation
• Narrow angle glaucoma

119. • Anticholinergic effects: Dry mouth, bad taste, constipaton,
urinary retention etc.
• 2. Dysphoric state or mania – suicide
• 3. CVS:
• Postural hypotension – older patient and overdose
• Arrhythmia – with IHD
• 1.Weight gain – not with bupropion and SSRI
• 2. Seizure – in children
• 3. Sedation, mental confusion etc. – more with amitriptyline
• 4. Sweating and fine tremor

120. ANTIEPILEPTIC DRUGS
• Anti convulsant drugs
• Used for prevention od
seizure
• Status epilepticus and febrile
seizures

122. MECHANISM OF ACTION
•Prevent or reduce excessive discharge of
neuron
•Decrease spread of exciation
•Exact mechanism not know but may be
• Supressing sodium influx
• Supressing calcium influx
• Inscreasing action of GABA that inhibit
neurotransmitters in brain

123. DRUGS CLASSIFICATIONS

124. MECHANISM OF ACTION
MOA of Phenytoin, Carbamazepine, felbamate,
lamotrigine, valproic acid
• •Block voltage-dependent sodium channels
Mechanism of action of Barbiturates
• Prolong GABA-mediated chloride channel openings
• Benzodiazepines
• Increase frequency of GABA mediated chloride channel openings

125. • Valproate
• May enhance GABA transmission in specific circuits
• Blocks voltage-dependent sodium channels
• BlocksT-type calcium currents

126. PHENYOTION-ADVERSE EFFECT
• • Gum hypertrophy:
• • Hirsutism:
• • Hypersensitivity reactions:
• • Megaloblastic anaemia:
• • Osteomalacia:
• • Hyper-glycaemia.
• Nystagmus

127. CARBAMAZEPINE • ADVERSE EFFECTS
• – Dose related neurotoxicity
• sedation, dizziness, vertigo, diplopia and ataxia.
• Vomiting, diarrhea
• Acute intoxication
• coma, convulsions and cardiovascular collapse.
• Hypersensitivity reactions:
• rashes,photosensitivity hepatitis, lupus like syndrome
• Antidiuretics actions
• Water retention and hyponatremia in the elderly as it enhances ADH action. –
• Teratogenic

128. SODIUMVALPROATE
❑Mechanism of action:
❑ Increases the inhibitory neurotransmitters (GABA) and decreasing the
excitatory transmission,
❑Due to increase in GABA content of the brain by inhibiting GABA
transaminase and succinic semialdehyde dehydrogenase.
❑Pharmacokinetics:
❑ Well absorbed orally,
❑Inhibits metabolism of several drugs such as carbamazepine, phenytoin,
topiramate and phenobarbital.
❑ Excreted in urine.
❑Plasma half life of 15 hours.

129. ❑Side effects:
❑ Nausea,
❑vomiting,
❑GIT disturbances,
❑transient hair loss,
❑Hepatotoxicity,
❑Thrombocytopenia.

130. GABAPENTIN
❑Structural analogue of GABA.
❑May increase the activity of GABA
❑or inhibits its re-uptake.
❑Pharmacokinetics:
❑ Orally absorbed,
❑ not bound to any proteins,
❑ and does not get metabolized and
❑ excreted mainly in urine.
❑ Plasma half life to 5 to 7 hours

131. ❑Side effects:
❑Somnolence,
❑dizziness,
❑ataxia,
❑fatigue and
❑ nystagmus
Long acting Barbiturates:
inhibit GABA

132. ANTI MANIC DRUGS
• Mania is characterized by excessive desire & too
much of euphoria
• mood stabilizers or drugs for Bipolar disorders
Bipolar disorder:
• also known as manic-depressive illness,
• is a brain disorder that causes unusual
shifts in mood, energy, activity levels, and the
ability to carry out day-to-day tasks

135. • Lithium
• Carbamazepine
• Valproic acid
• Lamotrigine
• Olanzapine

136. LITHIUM MOA
• inhibits several important enzyme in conversion of IP 2
to IP 1 & conversion of IP to inositol
• Act on secondary messanger

137. •Preparation – 300mgtab, 400mg SR tab.
• Dose –
• started at 600mg /day & increased up to
therapeutic plasma level in dose of 600 -1200
mg/day

138. PARKINSONISM
• shaking palsy
• Extrapyramidal motor function
disorder characterized by
• Rigidity
• Tremor
• Hypokinesia/Bradykinesia
• Impairment of postural
balance - falling

139. • Normal condition
• Parkinson disease

140. HOW IT OCCURS?
• Degeneration of dopamine-producing neurons in the
substantia nigra of the midbrain
• Disrupts the balance of:
• dopamine (DA) – neurotransmitter for normal functioning of the
extrapyramidal motor system (control of posture, support, and
voluntary motion)
• Acetylcholine (Ach)
• and the basal ganglia
• Symptoms do not occur until 80% of the neurons in the
substantia nigra are lost

143. ANTI PARKINSONISM DRUGS-LEVODOPA
• Dopamine
precursor drug

145. SIDE EFFECTS
At the initiation of therapy
1 – Nausea and vomiting
2 – Postural hypotension
3 –Cardiac arrhythmias
4 – Exacerbation of angina
5 – Alteration of taste sensation

146. PERIPHERAL DECARBOXYLASE INHIBITORS
Carbidopa
• Do not cross BBB
• Half life of L-Dopa increased
• Systemic side effects less
• Pyridoxine reversal does not occur
• ON/OFF phenomenon is minimized
• Degree of improvement higher
• Smooth control of symptoms
• Less diurnal fluctuations
LEVODOPA + CARBIDPOA

147. • Thanks