PSIKOTROPIKA

- Antipsychotics
- Antineurotics
- Antidepressants
- Psychotomimetics

ANTIPSYCHOTICS and TRANGUILIZERS

Major tranquilizer

Anti-psychotics -- neuroleptics
(chlorpromazine, haloperidol, clozapin)

Minor tranqulizers

Anxiolytics
(diazepam, clobazepam, nitazepam)

Neuroleptics

Calming effects on
hyperactive, labile, aggressive patients

Large dose
does not cause coma or anaesthesia

May cause extrapyramidal symptoms

(parkinsonism, ataxia, choreoathetoid etc.)

May not cause any dependency

NEUROLEPTICS
Block the r-D2 (dopaminergic-2 receptors)
r-D subtyping :
- r-D1 postsynaptic
- r-D2 pre and postsynaptic
- r-D3 (homolog D2)

Limbic D5

- r-D4 (homolog D1)

cortex frontal D4

- r-D5 (homolog D1)

ventral striatum D3
amigdala D4
hypocampus D4

D1, D2, D4

Ngatidjan, ANTIPSIKOTICS

8/5/16

1. Transmitter synthesis
2. Transmitter release
3. Postsynaptic receptor

G : guanine nucleotide protein

4 GTP
G-GTP and G-GDP :G-protein which is boundDto
(guanosinetriphosphate) or GDP (guanosine diphosphate)
Ngatidjan, ANTIPSIKOTICS

8/5/16

Neuroleptics
- Phenothiazine derivative: chlorpromazine
- Diphenylbutylpiperidine : pimozide
- Thioxanthene

: thiothixene

- Dibenzoxazepine : loxapine
- Dihydroindole : malindone
- Butyrophenone : haloperidol
- Dibenzodiazepine : clozapine

NEUROLEPTICS
-

Lipophylic, and bound to the protein

tends to be accumulated in the SNC

Gastrointestinal absorption often irratics

much better result if be given by i.m. injection

Long half life

the dose once a day
(flufenazine : once every 2 weeks)

NEUROLEPTICS
* Block r-D

- in mesolombics antipsychotic effects

- in basal ganglia parkinsonism, chorea
* Block peripheral r-M

- dry mouth etc.

* Block r-

- hypotension

Side effects of

NEUROLEPTICS

Parkinsonism, chorea athetoid

Type A

(caused by blockade of r-D in basal ganglia)

dry mouth
cycloplegia

r-M blockage

constipation
hypotension, tachycardia

r-blockage

Side effects of NEUROLEPTICS

Type B
- bone marrow depression
- hepatic malfunction
* jaundice
* steatosis
- renal malfunction

Side effects of some antipsycotics

ANTINEUROTICS
Anxiolytics
Minor tranquilizer
Ngatidjan, ANTIPSIKOTICS

8/5/16

NEUROSIS
Neurosis Anxiety
- Physiological anxiety
(easy go / to be forgotten, still realistic)

- Pathological anxiety
(persistent, unforgettable, unrealistic)

ANXIETY,

neurosis, psychoautonomic disorders

and psychotics

psychological
stress

anxiety

- unsatisfaction
(easy go / to be forgotten, realistic)

- somatic complain
(skeletal muscle ache & cramp, headache)

- excessive anxiety
(permanent, unrealistic & irrational)
may lead to

psychotic

ANXIETY and NEUROSIS

- Generalized anxiety disorders
an ongoing state of excessive anxiety lacking any clear reason or focus

- Panic disorders
attack of overwhelming fear occurring in association with marked
somatic symptoms : sweating, tachycardia, chest pains, trembling, etc.

- Phobia
strong fear of specific things or situation e.g. worm, snake, flying, dark.

- Post traumatic stress disorders

anxiety triggered by insistent recall of past stressful experiences

ANXIOLYTICS Hypnotics

Benzodiazepines
diazepam, triazolam, midazolam, zolpidem
lorazepam, oxazepam, temazepam, lormetazepam
alprazolam, nitrazepam
diazepam, chlordiazepoxide,

Buspiron

-blockers (propranolol)
Barbiturates (lack of anxiolytic effects)

Others (lack of anxiolytic effects chloral hydrate,

meprobamat, diphenhydramine etc.)

Benzodiazepines
(diazepam, lorazepam, nitrazepam, clobazepam etc.)

Ngatidjan, ANTIPSIKOTICS

8/5/16

Benzodiazepine

stimulate BDZ-receptors
chloride ion channel opening
Cl- influx
hyperpolarisation
nerve cell activity
anxiety
Ngatidjan, ANTIPSIKOTICS

8/5/16

r-BDZ
- intercorrelate with r-GABA
- 2 type : r-BDZ1 and BDZ2
- located at subunit- r-GABA
-

frequency of ion channel opening

- endazepin (bezodiazepin like substance)

r-GABA
- r-GABAA and r-GABAB
- r-GABAA consists of
subunit- (6), - (4)
and - (3)
- GABA interact D
with
subunit- and 4
Ngatidjan, ANTIPSIKOTICS

8/5/16

r-N

r-BDZ

D4
Ngatidjan, ANTIPSIKOTICS

8/5/16

the effects of benzodiazepines

sedation

hypnosis

anxiolysis

anticonvulsive muscle relaxation

Sedation BDZ
* spontaneous response
* large dose dysinhibition euphoria,
difficulty in decision making,
lost of self control
* amnesia

Anticonvulsive / muscle relaxants

* inhibits polysynaptic reflex (spinal)

EPSP
IPSP

: exitatory postsynaptic potential

: inhibitory postsynaptic potential
Ngatidjan, ANTIPSIKOTICS

8/5/16

Anxiolytics
1. Benzodiazepines
- Diazepam
- Flurazepam
- Temazepam
- Midazolam
- Clobazepam
- Lorazepam
- etc.

2. Propanediol
- Meprobamate
- Chlordiazepoxide

3. Azaspirodecanedione
- Buspiron

T1/2 BENZODIAZEPINES
- Chlordiazepoxide
- Diazepam

: 24 hrs

: 72 hrs

- Flurazepam

: 75 hrs

- Loprazolam

: 9 hrs

- Lorazepam

: 12 hrs

- Nitrazepam

: 24 hrs

- Oxazepam

: 12 hrs

Anxiolytics
1. Benzodiazepines stimulate r-BDZ
-

diazepam, flurazepam, temazepam, midazolam,

clobazepam, lorazepam, nitrazepam, etc.

2. Propanediol stimulate r-BDZ

-

Meprobamate, chlordiazepoxide

3. Azaspirodecanedione 5-HT agonist

-

Buspiron

-blockers reduce physical symptoms of anxiety

-

Propranolol