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Psychopharmacolog
y
 Psychopharmacology is the branch of pharmacology that

deals with the study of the actions, effects, and development
of psychoactive drugs.
 In its broadest sense it means the study of all

pharmacological agents that affect mental and emotional
functions.
 Specifically to the study and synthesis of drugs used in the

control of psychiatric illnesses,

 The mentally ill in early communities were generally

cared for by family members, however, in severe cases
they sometimes ended up in almshouses or jails. Because
mental illness was generally thought to be caused by a
moral or spiritual failing, punishment and shame were
often handed down to the mentally ill and sometimes
their families as well.
 The Treatment of Psychiatry disorders in the past has
often constituted of merely institutionalisation (i.e
administration in ansylym or mental hospital)
 with the advent of psychopharmacology in the 6th
decade has brought treatment of Psychiatric disorder
within the realm of scientific medicine
 Antipsychotics
 Antidepressants
 Mood stabilizing drugs
 Anti anxiety and hypno-sedatives
 Anti epileptics

 Alcohol and drug dependence
 Antiparkinsonians
 Miscellaneous drugs-(e.g Stimulants , drug used in

treatment of eating disorder, alcohol dependence,
anaesthetic,dementia,drugs used for child psychiatry,
vitamines calcium channel blocker and other drugs)
OD
PD
(mg/dl) (mg)

Sedatio Hypote
n
n-sion

EPSE

Wt.gain

Increas
e
prolact
in

Chlorpromazi
ne

3001000

50-100

+++

+++

+

++

++

Triflupromazi
ne

100-400

30-60

++

++

++

++

++

100-400

______

++

+

+

++

+

+++

++

+

++

+

Drug

I.Phenothiaz
ines
A. Aliphatic

B.
Piperidines
Mesoridazine
Thioridazine

300-600 ______
OD
PD
(mg/dl) (mg)

Sedati
on

Hypote
n-sion

EPSE

Wt.gai
n

Increase
prolacti
n

Fluphenazi
ne

2-20

_____

+

+

+++

+

+++

Prochlorpe
razine

45-150

40-80
IM

+

+

+++

+

+++

1-5 IM

+

+

+++

+

+++

Drug

C.Piperazi
ne

Trifluopera 15-50
zine
Drug

OD
(mg/dl)

PD
(mg)

Sedatio
n

Hypote
n-sion

EPSE

Wt.
gain

Increas
e
prolacti
n

25-75

+++

++

++

++

++

Thioxanthines
A.Aliphatics
1.Chlorpromazin 75-600
e

B. Piperazines
1.Flupentixol

3-18

_____

+

+

++

++

++

2.Thiothixene

6-60

2-6 IM

+

++

++

++

++

3.Zuclopenthixo
l

25-150

50-600
IM

++

++

++

++

++
OD
(mg/dl)

PD (mg)

Sedatio
n

Hypoten EPSE
-sion

Wt.
gain

Increase
prolacti
n

1.Haloperidol

5-30

5-10 IM

+

+

+++

+

+++

2.Trifluperidol

0.5-8

2.5-5 IM

+/-

+/-

+++

+

++

1.Penfluridol

20-60
mg/w

____

+

+

++

+

++

2.Pimozides

4-20

____

+

+

++

+

+++

50-225

______

++

0

+

+/-

+/-

25-250

_____

++

++

++

+

+++

Drug
III.Butyropheno
ne

IV.Diphenylbutylpiperidines

V. Indolic
Derivatives
1.Molindone

VI.Dibenzopine
1.Lorxapine
OD
PD
(mg/dl) (mg)

Seda
tion

Hypot
ension

EPSE

Wt.gain

Increase
prolactin

1.Iloperidone

4-24

_____

0

+

+

++

0

2.Paliperidone

3-12

_____

+

++

+

++

+++

3.Resperidone

2-8

_____

+

++

+

++

+++

40-160

_____

+/-

+

0

+/-

+/-

5-20

2.5-10
IM

++

+

+/-

+++

+

Drug

C.Benzisoxales

D.Benzisothazolyl
1.Ziprasidone

E.Thienobenzodi
azepine
1.Olanzapine
OD
(mg/dl)

PD
(mg)

Sedatio
n

Hypot
ension

EPS
E

Wt.gain Increase

50-900

____

+++

+++

0

+++

0

1.Amisupride

400-1200

____

+/-

+

+

+

+++

2.Sulpiride(not
called atypical
usually)

400-2400

____

+/-

+

+

+

+++

Drug

prolactin

A.Dibenzodiaz
epines
1.Clonazipine
B.Substituted
Benzamides
Hypoten
-sion

EPSE

Wt.gain Increas

++

+/-

0

++

0

_____

0

0

0

+/-

0

20

_____

0

0

0

+/-

0

75-300

______ ++

+/-

+

++

++

OD
(mg/dl)

PD
(mg)

Sedation

150-750

____

1.Aripiprazole

5-30

2. Bifeprunox

Drug

e
prolacti
n

E.Dibezodiaze
pine
Quetiapine

F. Partial
Agonist

G.Dibenzothi
epin
1.Zotepine
Drug

OD
(mg/
dl)

PD
(mg)

Sedati
on

Hypot
ension

EPSE

5-10

____

0

+/-

0

Wt.gai Increas
e
n

prolacti
n

H.Dibenzooxe
pinopyrrole
1. Asenapine

+/-

0
 The estimates of the common side effect in the table

mention are roughly given and is an empirical guideline
to the clinical use. The dosage can be change as per the
requirement of the patient, clinical symptoms and
severity.
 EPSE=Extra Pyramidal Side Effect
** 0=Absent, +/- = Probable/Very little
+ = Mild, ++ =Moderate, +++ = Severe
The exact mechanism of action of antipsychotic is unknown
 however one of the major mechanism appears to be anti-dopaminergic activity of
these drugs
 Block D2-receptor which are mainly present in



mesolimbic-mesocortical system (concern with emotion)

nigo-striatal system & tubero-infundibulum system
 Extra Pyramidal side effect (EPSE) are cause due to blockade in
mesolimbic system, & hyperprolactinemia cause by blockade in
tubero-infundibular system.
 Sedation is caused by histaminergic blockade which are usually
highest for drugs such as Chlorpromazine and thioridazine.

 Atypical or 2nd generation Antipsychotic has action only on







mesolimbic system but has no eefect on nigro-striatal or
tubero-infundibular system.
The SGAs and clude Risperidone,Quetiapine,Olanzapine,
Amisulpride,Papiperidone,Zointepine,Ziprasidone and
Aripiprazole.
so it reduce s/e such as Extapyrimidal s/e (EPSE)and
hyperprolatinemia s/e
It mainly act on D4 & 5-HT2 receptor and has weak D2
antagonism
less incidence of tardive dyskinesia & Neuroleptic Malignant
syndrome.
Organic Psychotic
disorder

Non organic
Psychotic disorder

Delirium

Schizophrenia
Schizo-Effective
disorder

Drug induce
psychosis

Acute psychoses

Other:
Organic
hallucination

1.Mania
2.Bipolar

Organic delusion
disorder

Major Depression

Secondary mania

Delusional disorder

Medical Disorder

Severe, intractable &
disabling anxiety
Dementia

Neurotic & other
psychiatric
Disorder

Hungtington Chorea

Rx refractory OCD

Intractable hiccup

Anorexia Nervousa

Nausea & Vomiting
Tic disorder e.g
Gilles de la tourette
syndrom
Autonomic Side effects
Dry Mouth, Constipation,
Cycloplegia,Mydriasis, Urinary Retention
Central Anti Cholinergic Syndrome (Delirium)
Impotence, Impaired Ejaculation.
Extra Pyrimidal Side Effects
Parkinsonian Syndrome (esp tremor),
Akanthisia (Motor restlessness),
Acute Dystonia,
Rabbit Syndrome (Peri oral tremor),
Tardive Dyskinesia (late onset oro-facial dyskinesia),
Neuroleptic Malignant Syndrome(Fever,EPS,High CPK
catotonic symptom and autonomic dysfunction)
Other Central Nervous System Side Effects
Seizure, Sedation Depression or Pseudo
depression
Metabolic And Endocrine side effects
Weight Agin,Diabetes, Galactorrhea with/without
Amenorrhea
Allergic Side effect:
Cholestatic Jaundice, Agranulocytosis
Cardiac Side effect
EKG Changes (e.g QTc Prolongation)

Ocular Side Effect
Granular side effect not know in cornea and
lens,Pigmentatary retinopathy resembling retinitis
pigmentosa.

Dermatological side effect:
Contact dermatitis, Photosensitivities reaction,
Bleu-ray metallic Discoloration


ANTIDEPRESSANT
DRUG

Drug use to treat depressive

disorder
Also know as Mood elevator
and thymoleptic
Sedation

Orthostatic
hypotension

Anticholiner
gic

1.Amitriptylline 75-300

+++

+++

+++

2.Clomipramin
e

75-250

++

++

++

3.Dosulepin

75-300

+++

+++

++

4. Doxepine

75-300

+++

+++

+

5.Imipramine

75-300

++

++

++

6.lofepramine

70-210

+

+

+

7.TriImipramine

75-300

+++

++

++

Drugs

Oral dose

Tricyclic
Tertiary amines
Oral dose

Sedation

Orthostatic
hypotension

Anticholiner
gic

1.Desipramine

75-300

+/-

+

++

2.Nortriptyline

75-200

+

++

+

3.Protriptyline

15-60

0

++

++

1.Amoxapine

150-400

+

+

++

2.Maprotiline

75-225

++

++

++

3..Mianserin

30-120

+++

+/-

+/-

100-300

+/-

+/-

+/-

Drugs

B Ticyclic 2nd

Amine

C. Tricyclic
Antidepressant

D.Bicyclic
Antidepressant

1.Viloxazine
Oral dose

Sedation

Orthostatic
hypotension

Anticholinergi
c

1.Citalopram

20-40

+/-

+/-

0

2.Estitalolopra
m

10-20

+/-

+/-

0

3.Fluoxamine

20-60

+/-

0

0

4.Fluvoxamine

50-300

+/-

+/-

+/-

5.Paroxetine

20-40

+/-

0

+/-

6.Setraline

50-200

+/-

0

Drugs
II. SSRI

IV SNRIs
1.Duloxetine

60

+/-

+/-

+/-

2.Venlafaxine

50-200

+/-

+/-

+/-
Oral dose

Sedation

Orthostatic
hypotension

Anticholinergi
c

37.5

+

0

+/-

15-45

+++

+

+/-

150-450

Activating

0

0

Nefazodone

200-600

++

+

+/-

Trazodone

150-400

+++

+/-

+/-

Drugs
IV.NSREs
Tianeptin
V.NaSSAs
Mirtazapine
VI.NDRI

Bupropion
VII.SARIs
Drugs

Oral dose

Sedation

Orthostatic
hypotension

AntiCh

+/-

+/-

+/-

VIII.NARI
1.Reboxetine
IX.MAOIs
A.Reversible Selective
MAO-B Inhibitor
1.Selegiline

5-10

Use in
Parkinsonis
m

300-600

Activating

0

0

20-50

+

0

0

B.Reversible Selective MAOA inhibitor(RIMAs)
1.Meclobemide
X.Melatonin Receptor
agonist & 5-HT2c antagonist
1.Alomelatin
 It increase catecholamine levels in brain
 TCA:
 1. Blocking the reuptake of norepinephrine,serotonine

and/or Dopamine at the nerve terminal thus increase
NE,5-HT and/or DA level at the reactor site
 2. Down regulation of Beta adenergic receptor
 Depression:
 Depressive Episode (also called Major

depression,endogenous depression)
 Depressive episode with melancholia (with or without
ECTs)
 Depressive Episode with Psychotic feature (with
antipsychotic or ECTs)
 Dysthymia (with Psychotherapy)
 Reactive depression (with Psychotherapy)
 Depressive equivalent and masked depression
 Atypical Depression
 Secondary Depression (e.g in Hypothyroidism, cushing

Syndrome)
 Abnormal Grief Reaction
 Enuresis
 Attention Deficit disorder with Hyperactivity
 School Phobia
 Separation anxiety disorder
 Somnambulism
 Night tremor
 Panic Attack

 Borderline Personality

 Agoraphobia

Disorder
Trichotillomania
Depersonalisation
syndrome
Post traumatic stress
syndrome
Generalise Anxiety
Disorder
Narcotic dependence
Alcohol Dependence

 Obsessive compulsive



disorder with or without
depression
 Cataplexy (associated
with narcolepsy)
 Aggression in Elderly
 Eating Disorder






 Chronic Pain
 Migraine
 These drug are usually effective in treatment of mania

Therefore the words Antimania is often use to
describe them.
 Effective in preventing Mood swing in Bipolar Disorder
 These Drug include

Lithium , Valproate , Carabamazepine and
Lamotrigine
 INDICATION:
 Rx of Acute Mania
 Prophylais of Bipolar mood Disorder
 Rx of Schizo -effective disorder
 Prophylaxis of Unipolar mood disorder
 Rx of cyclothymia
 Rx Of Acute Depression
 Rx Acute Alcoholism

 Rx of Impulsive Aggression
 It effect the Na+ K+ ATPase and accumulates intracellularly as









substitute of Na+
It inhibit the adenyle Cyclase and thus decrease cAMP (II
Messenger) intracellularly
It accelarate the presynaptic reuptake and destruction of
catecholamine,like norepinephrine
It inhibit the release of the catecholamine in synapse
It decrease the post synaptic serotonin 5-HT2 receptor
sensitivity
It stabilizes the membrane, along with Ca++ and Mg++
It decreases the Ca++ mobilisation from the intracellular pools
by ITP(inositol-triphophate)- dependent Ca++ channels (II
Messenger system)
 Lithium Carbonate (300mg tablets;400mg sustained

release tablet)
 Lithium citrate (300MG/5ML liqiud)
 Before starting treatment,it is essential to ensure
normal functioning of kidney, thyroid, heart and CNS
 Routine and general systemic physical examination
 Routine blood count(Hb,TC,DC)
 Urine:R/E and Microscopic
 ECG
 RFT (blood urea,serum creatinine)24hours urine

volume, urine specific gravity).
 TFT (T3,T4,TSH)
 Doses:
 Initial starting dose for lithium is 900-1200mg/dl given in 1-3







doses.
During Rx it is essential to estimate blood level of lithium
Therapeutic levels=0.6-1.2 mEq/L (for Rx of Acute Mania)
Prophylactic levels=0.6-1.0 mEq/L (for relapse prevention in
Bipolar)
Toxic lithium levels >2.0mEq/L
When stopping lithium Rx it is essential to taper the dose
over several days / weeks in order to minimise the risk of
relapse on discontinuation
Side effects:Lithium
I. Neurologic:
Tremor, Muscular weakness,Cogwheel
rigidity,Seizure,Neurotoxicity(Delirium,cerebellar sign,abnormal involuntary
movement seizure & later coma)
II.Renal:
Polyuria, polydipsia, Tubular changes,Nephrogenic diabetes insipidus,
Nephrotic syndrome
III. Cardiovascular:
similar to those of Hypokalemia (T-wave depression)
IV. Endocrine
Goitre,Hypothyroidism,Wt.Gain,Abnormal TFT
V.Gastrointestinal:
Nausea,Vomiting,Diarrhoea,metallic taste, and abdominal pain
VI.Dermatological:
Acneiform eruption, Papular eruption and exacerbation of Psoriasis
VII. S/E during pregnancy:
Teratogenic,Ebstein anomaly,secretion in milk 30-100 % of maternal Lithium
level therefore cause toxicity in Infant
 Valproate Dosage- 1000-3000mg/day oral dose in divided

dose
 Therapautic blood level is 50-125mg/ml
 Bipolar Disorder
 Neurological Disorder- Migraine and pain

Syndrome,Trigeminal Neuralgia, and Neuropathic
pain,Seizure(Absence seizure,complex partial
seizure,myoclonic seizures and generalise tonic clonic
seizure)
 Other: Behavoural agitation in dementia,severe symptom in
mental retardation,ADHD and conduction
disorder,Schizoaffective disorder (bipolar type),alcohol
withdrawal,tadive dyskinesia,impulse control disorder,panic
disorder and borderline personality disorder.
 Side effect: Valproate

 Adverse effect is more common with valproate

concentration above 100mg/dl
 Common side effect are nausea , sedation , tremor,
flushing, weight gain thrombocytopenia , menstrual
disturbance, n hair loss
 Other most serious, though relatively uncommon include
Hepatic toxicity , Acute hemorrhagic pancreatitis and
Steven-Johnson Syndrome.
 SEIZURES
 Complex partial seizure (CPS)
 Generalised tonic clonic seizures
 Alcohol withdrawal seizures (rum fits)
 PSYCHIATRIC DISORDERS:
 Bipolar mood disorder
 Impulse control disorder and aggression
 Psychosis with epilepsy
 Borderline personality disorder
 Cocaine withdrawal syndrome
 PAROXYSMAL PAIN SYNDROME
 Trigeminal neuralgia
 Phantom limb pain
 Diplopia,drowsiness,dizziness,nausea,vomiting ataxia,
 Skin rash, Steven-johnson syndrome(erythema multiforme

major),photophobia,
 cholestatic jaudice ,acute oliguria with
hypertension,leucopenia and thrombocytopenia purpura.
 The most dangerous side effect include bone marrow
depression (causing aplastic anemia) agranulocytosis and
cardiovascular collapse.
ANTI ANXIETY
&
HYPNOSEDATIVES
WHAT IS ANXIETY??
It

is an emotional state,
unpleasant in nature, associated
with uneasiness, discomfort and
concern or fear about some
re
-defined or undefined future
threat.
Anxiety is being in a state of
stress, which is brought upon by
many stressors.
It

is the normal human
response.
Anxiety is regarded as a
disorder only when it occurs in
the absence of appreciable
degree, or kind, of threat or
danger.
CLINICAL
PRESENTATIONS
Palpitations.

Chest

pain.
Breathlessness.
Sweating, chills, nausea.
Trembling, fear of dying or
losing control.
Numbness, feeling of
detachment.
ANTI-ANXIETY DRUGS
Benzodiazepines.

Azapirones.
Sedative

anti-histaminic.
β-blocker.
Newer drugs
BENZODIAZEPINES
Mode of action
Modulates the gamma-amino
butyric acid(GABA),the main
inhibitory neuro- transmitter of
CNS,by influencing the GABAa
receptor complex.
The GABAa receptor complex includes binding sites
for BZD,barbiturates and steroids. the chlorine ion
channel is controlled by the GABA binding
site.When the neuro transmitter GABA binds with
the receptor it triggers a conformational change in
the pore, allowing more chlorine to enter the cell.
 Resulting in hyperpolarisation of cell membrane,
increasing the firing threshold and producing an
inhibition of action potential firing.
 Upon binding,BZDs lock the GABAa receptor into a
conformation that increases the binding of GABA.
 Increased GABA binding increases the frequency of
opening the chlorine channel and amplifying the
inhibitory effect.

Class of
drug

Eliminatio
n T1/2

(hr)

Oral
Dosage
Mg/day

Very

short

acting

1.Triazolam

2-5

0.125-0.25

2.Midazolam

Parenter
al dose
(mg)

Active
Comment
metabol s
ites
α-hydroxy
triazolam.

2-5

Short

acting

1.Oxazepam

5-15

15-120

2.Lorazepam

10-20

2-6

3.Temazepa
m
4.Alprazolam
5.Estazolam

10-20

15-30

6-20

0.5-6

8-24

1-2

Rapid oral
absorption,
marked as
hypnotic, used
as anesthesia

1-2 iv or im

Oxazepa
m
α-hyroxy
alprazola
m

Slow oral
absorption,
high
dependenc
e potential
Class of
drug

Eliminatio

n T1/2

(hr)

Oral
Dosage
Mg/day

Parenteral
dose
(mg)

Active
Comment
metabolite s
s

50-100 iv
slowly
2-20 iv or im

Desmethyldemoxypam

Long

acting

1.Chlordiaze
poxide
2.Diazepam

25-48

15 -100

14-90

2 – 60

3.Flurazepa
m
4.Chlorazep
ate
5.Nitrazepa
m
6.Prazepam

30-100

15-60

Desmethyhydroxy-ethylflurazepam

30-100

7.5-60

Nordiazeapam
Nordiazepam

20-60

5-20

30-60

20-60

7.Halazepa
m
8.Clonazepa
m
9.Quazepa
m

30-60

Nordiazepam,
diazepam
Nordiazepam

40-160

2-5 im
20-40

0.5-20

40-160

7.5-15

Nordiazepam

Erratically
absorbed after
IM injection,
Marked as
hypotic,
Hydrolyzed to
active form in
stomach
Marked as
hypnotic
Slow oral
absorption
Also used in
mania
.probably
selective for
BZD receptor l
and may
cause less
cognitive and
motor
disturbances
INDICATIONS OF ANTI-ANXIETY
DRUGS
Triazolam and midazolam:- For Generalized
anxiety, panic attacks.
 Oxazepam,Lorazepam,Temazepam,Alprazolam,
Estazolam—For Insomnia,nightmares,muscle
relaxation, drug withdrawal, acute mania attacks
 Chlordiazepoxide,Diazepam,Flurazepam,Chlorazep
ate,Nitrazepam,Prazepam,Halazepam,Clonazepam
,Quazepam—For Minor surgery, acute
psychosis,narcoanalysis,anti
convulsant,somnambulism,agitation depression
attacks.

AZAPIRONES
Class of
drug

Elimination
T½

Dose

Mode of
action

Adverse
effects

Buspirone

2-3.5 hrs

15-30mg/day

5-HT1a partial
agonist and a
selective DA
autoreceptor
antagonist

Dizziness.hea
dache,lighthe
adedness and
diarrhoea.

Gepirone

Ispapirone
SEDATIVE ANTIHISTAMINES
Mode of action
Selective anxiolytic action with
sedation.
Seldom used nowadays.
Diphenhydramine,
Hydroxyzine and
Promithazine.
ΒETA-BLOCKERS
Example

is propranolol
effective in peripheral
manifestations of anxiety.
C/I in asthmatics and cardiac
conditions.
Dose is 40-240mg/day.
NEWER DRUGS
 Buspirone-non

BZD anti-anxiety drug. its is
a 5-HT1a partial agonist and a selective DA
auto-receptor antagonist. also inhibits the
auto-firing of neurons.
 It does not seem to act on BZD receptor. It
is anxio-selective with no sedative action,
and no anti-anticonvulsant or muscle
relaxant properties.
 Dose is 15-30mg/day, in a thrice daily
schedule due to short half-life.not useful in
t/t of panic disorders.
 Zopiclone—belongs

to a new class of group,
the cyclopyrrolone.They act on GABA
receptors but at a site different from that of
BZDs.Has a short duration of action as well
as shorter onset.Elemination t½ is 4-6hrs.
 Usual dose is 3.75-7.5 mg at bed time.
 Side effects include bitter taste, dry
mouth,drowsiness,nausea and headache
 Clinically superior to BZDs in subjective
awakening quality, well being and attention
span in morning.
Zolpidem—it is an imidazopyridine derivative which
is marketed as a hypnotic.
 It is administered in a dose of 5-10 mg for hypnotic
use. It has a half life of 2-3 hrs; therefore it is useful
in treatment of difficulty in initiation of sleep(initial
insomnia).
 Side effects include
drowsiness,dizziness,headache,depression,nausea
,dry mouth and myalgia.
 It should not be used for more than two weeks at
one time.
 Safety in children, in pregnancy and lactation is not
proven.

 Zolpelon-it

is a pyrazolo-pyrimidine
derivative, marked as a hypnotic. It acts on
omega-1 benzodiazepine receptor located
on the alpha sub-unit of the GABA-A
receptor complex, with a very little effect on
omega-2 and omega-3 receptors.
 Given in a dose of 5-10 mg for hypnotic
use.T½ being of 1 hr with a rapid onset of
effect.
 Side effects include
headache,drowsiness,dizziness,nausea and
myalgia.It should not be used for more than
2 weeks at one time.
Other drugs—these include suriclone(a
cyclopyrrolone derivative; a hypnotic), bretazenil
and imidazenil(partial benzodiazepine agonists;
anxiolytic without sedation; rapid onset of
action),abecarnil(β-carboline partial agonist at
benzodiazepine receptor; anxiolytic and anticonvulsant),tiagabine,riluzole,and
alpidem(anxiolytic).
 Pregabalin is licensed for treatment of anxiety in
some countries. Cognitive behavior therapy with or
without medication is helpful in treatment of several
anxiety disorders.

ANTI-EPILEPTICS
WHAT IS EPILEPSY
It

is a brief recurrent disorder
of cerebral function that is
usually associated with
disturbance of consciousness
and accompanied by a
sudden, excessive electrical
discharge of cerebral neurons.
ANTI-EPILEPTICS
Barbiturates

Deoxybarbiturates
Hydantoin

Iminostilbene
Succinimide
Aliphatic

carboxylic acid
benzodiazepines
Phenyltriazine

Cyclic

GABA analogue
Newer drugs
Class of
drug

Eliminat Dose
ion T½

Phenobarb 80- 120
itone
hrs

60- 180 mg
/day

Primidone

250-500mg
BD

6-14 hrs
Phenytoin

12-24
hrs

200-400
mg/day as
single dose.

Indications Mode of
action

Adverse
effects

Primary
generalized
tonic
clonic,partia
l seizures.

GABAa
receptor
mediated
synaptic
inhibition

Hangover
Idiosyncrasy
Hypersensitivit
y
Dependence.

Generalized
T-C,simple
and
complex
partial,
status
epilepticus,t
rigeminal
neuralgia

Prolongatio
n of
sodium
channel
inactivation
.

Gum
hypertrophy
Hirsutism
Hypersensitivit
y
Megaloblastic
anemia
Osteomalacia
Hyperglycemia
Class of
drug

Eliminati
on T½

Dose

Indications Mode of
action

Adverse
effects

Carbamaze
pine

20-40hrs

6001800mg/day in
2-3 divided
doses

Primary
generalized
tonic
clonic,partia
l seizures.

Prolongati
on of
sodium
channel
inactivatio
n.

Sedation,dizz
iness,vertigo,
diplopia,ataxi
a.

Ethosuximi
de

48 hrs

7501250mg/day
as single
dose

Absence
seizures

Inhibition
of T type
calcium
current

G-I
intolerance,
Mood
changes,hea
dache,drowsi
ness.
Class of
drug

Eliminati Dose
on T½

Indications

Mode of
action

Adverse
effects

Valproic
acid

10-15
hrs

4003000mg
/day in
2-3
divided
doses

Absence
seizures,GTCS
,SPS and CPS

Prolongation
of Na
channel
inactivation.
Attenuation
of Ca
mediated T
current.

Rise in
serum
transaminas
e,alopecia,c
urling of
hair,inc.
blood
ammonia,ful
minant
hepatitis

Clonazepa 24 hrs
m

1-12
mg/day
1060mg/d
ay
0.20.5mg/k
g

Myoclonic szrs

Facilitation of
GABA
mediated Cl
channel
opening.

Sedation,dul
lness
Thrombophl
ebitis,respira
tory
depression,
fall in BP.

Clobazam

35 hrs

Diazepam

30-60
hrs

GTCS,SPS,CP
S
Insomnia,anxiet
y,night b4
surgery
Class of
drug

Elimin
ation
T½

Dose

Indication
s

Mode of action

Adverse
effects

Lamotrigine 24hrs

50mgday- Add on
300mg/da therapy in
y
refractory
partial and
GTCS

Modifies maximal
electroshock and
decreases
electrically
evoked afterdischarge
duration.

Sleeplessn
ess,dizzine
ss,diplopia,
ataxia and
vomiting

Gabapentin 6-8 hrs

300mg/da Absence
y
seizures,G
TCS,SPS
and CPS

Enhances GABA
release and
inhibits PTZ
induced clonic
seizures.

Mild
sedation,tir
deness,dizz
iness and
unsteadine
ss
ALCOHOL AND DRUG
DEPENDENCE
WHAT IS DEPENDENCE??
According

to ICD-10 the
dependence syndrome is a
cluster of physiological ,
behavioral and cognitive
phenomena in which the use of a
substance or a class takes much
higher priority for a given
individual than other behaviors
that once had great value.
PSYCHOACTIVE SUBSTANCE
ABUSE
Drug

Route of
administration

Physical
Psychic
dependen dependenc
ce
e

Tolerance

Alcohol

Oral

++

++

+

Opioids

Oral,IV,smoking

+++

+++

+++

+,--

++

+

Cocaine

Inhalation,oral,sm +,-oking parental

++

Ampheta
mines

Oral,parentral

++

Cannabis Smoking,oral
(Marihuan
a)

++

+++
Drug

Route of
Physical
administrat dependenc
ion
e

Psychic
dependenc
e

Tolerance

Lysergic acid
diethyl
amide(LSD)

Oral

+

+

Barbiturates

Oral,parentr
al

++

++

+++

Benzodiazepines

Oral,parentr
al

+

+

+

Volatile solvents

Inhalation

+,-

++

+

Phencyclidine
(PCP)

Smoking,inh +,alation,pare
ntral,oral

+

+

Caffeine

Oral

+

++

+

Nicotine

Oral,smokin
g

+

++

+
TREATMENT
 Addiction

is a complex but treatable
disease that affects brain function and
behavior.
 No single treatment is appropriate for
everyone.
 Treatment needs to be readily available.
 Remaining in treatment for an adequate
period of time is critical.
 Effective

treatment approaches
include—
Detoxification
Treatment
Relapse prevention
DETOXIFICATION
 Symptoms

produced by the removal of
the toxin(alcohol).
 The aim of detoxification is
symptomatic management of
emergent withdrawal symptoms.
 Drug of choice are usually
benzodiazepines.
 Chlordiazepoxide(80-200mg/day)
 Diazepam (40-80mg/day)
TREATMENT
 Behavior

therapy-aversion therapy, using
either a sub-threshold electric shock or an
emetic such as apomorphine.
 Other methods like(covert
sensatisation,relaxation techniques,
assertiveness training, self control training
and positive reinforcement) has been used
along with aversion therapy.
 Considered unethical in treatment of alcohol
dependence.
 Psycho-therapy—both

group and
individual. patient is educated about
the risks of continuing alcohol use.
 Motivational enhancement therapy
with or without cognitive behaviour
therapy and life style modification.
 The

deterrent agents—disulfiram(tetraethyl
thiuram disulfide)
 When alcoholics ingested by a person who
is on disulfiram,alcohol-derived
acetaldehyde cannot be oxidised to acetate
and this leads to accumulation of
acetaldehyde in blood.
 This causes the disulfiram ethanol
reaction(DER) characterized by
 flushing,tachycardia,hypotension,tachypnoe

a,palpitation,headache,sweating,nausea,vo
miting,giddiness and a sense of impending
doom.
 Onset of reaction occurs within 30minutes
becomes full blown within 1 hr and subsides
within 2 hrs of ingestion of alcohol.
 The usual dose is 250-500mg/day.
Parkinsonism
WHAT IS
PARKINSONISM??
Extrapyramidal

motor disorder
characterized by rigidity,
tremor and hypokynesia with
secondary manifestations like
defective posture and gait,
mask like face
sialorrhoea,dementia may
accompany.
ANTI-PARKINSONISM'S
Drugs affecting brain
dopaminergic system
Dopamine precursorLevodopa(L-dopa).
Peripheral decarboxylase
inhibitor-carbidopa,benserazide.
Dopaminergic agonistbromocriptine,pergolide,piribedil,r
opinirole,pramipexole
MAO-B

inhibitors-Selegiline
COMT inhibitorsentacapone,tolcapone
Dopamine facilitatorAmantadine.
DRUGS AFFECTING BRAIN
CHOLINERGIC SYSTEM
Central

anticholinergicstrihexyphenidyl(benhexol),proc
yclidine,biperidine.
Anti-histaminicsorphanadrine,promithazine.
LEVODOPA (L-DOPA)
Mode
 Orally

of action-

administered L-dopa after
absorption crosses blood brain barrier
and gets metabolized to dopamine.
 Dopamine cannot cross BBB so,a
peripheral decarboxylase inhibitor is
given such as carbidopa or benserazide.
DOSAGE AND T1/2
 Started

with a low dose of 50mg/dose.
Full therapeutic effect may take 4-8
weeks. Maximum dose is 8001000mg/day.
 Plasma t1/2 of levodopa is 1-2 hrs.
ADVERSE EFFECTS
 At

initiation of therapynausea,vomiting,postural hypotension,
cardiac arrhythmias, exacerbation of
angina, alteration of taste sensation.
 After prolonged therapy-abnormal
movements, fluctuation in motor
performance.
PERIPHERAL DECARBOXYLASE
INHIBITORS
Carbidopa

and benserazide are
given along with levodopa to
increase the t1/2 in periphery and
make more of it available to cross
BBB and to reach its site of action.
Maintenance dose is 0.4-0.8g of
levodopa with 75-100mg carbidopa
or 100-200mg of benserazide given
in 3-4 divided doses.
DEMENTIA
WHAT IS DEMENTIA??
Refers

to acquired global
impairment of intellect,
memory and
personality(cognitive function)
in the absence of gross
clouding of consciousness or
motor involvement.
COGNITION ENHANCERS
 Nootropic

(cognition enhancer)-piracetam
 Metabolic enhancerdihydroergotoxine(codergocrine),nicergoline
,piribedil
 Cholinergic activatorstacrine,rivastigmine,donepezil,galantamine
 Vasoactive cerebral protector-pyritinol(pyrithyoxine) ,ginkgo biloba
INDICATIONS
 Senile

dementia and confusional states of
old age.
 Mental retardation and learning problems in
children.
 Cerebrovasular accidents-to hasten
recovery of neuronal function.
 To reduce impairment of consciousness
following brain surgery, memory impairment
after ECT,and central vertigo.
Class of drug

Dose

Mode of action

Adverse effects

Piracetam

0.8-1 g TDS

Enhances
learning and
memory.
Facilitates inter
hemisphere
information
transfer.
Increased tonic
cortical control
on subcortical
areas.

Gastric
discomfort,excite
ment,insomnia,di
zziness and skin
rash.

Dihydroergotoxin 1-1.5mg TDS
e(Codergocrine)
Nicergoline

30mg OD

Piribedil

50mg OD
What we have
learned so far…
 The

drug groups can be chosen according
to the pattern and severity of the disorders.
Accordingly the dosage of the drugs can be
managed.
 Pyscho-pharmacology is one of the
important measures in the management of
the mental disorders.
Thank
Psycho pharmacology
Psycho pharmacology

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