Drugs acting on CNS-Introduction and Classification

Drug acting on CNS-Introduction and classification

1. 10. DrugsActing on Central
Nervous System(CNS)
Presented By-
Mr. Dattatraya B Thorat
M. Pharm.
Head of Department
PRES, Institute of Pharmacy, Loni

2. The CNS drugs are categorisedas:
1.General Anaesthetics e.g. Diethyl ether.
2.Hypnoticsand sedative e.g. Phenobarbitone.
3.Anticonvulsants e.g. Phenytoin.
4.Tranquillizers e.g. Chlorpromazine.
5.CNS Depressant with skeleton muscle relaxent property.
The narcotic analgesics or true analgesics like morphine and phethidine also selectively
depressC.N.S.

3. GeneralAnaesthetics
GeneralAnaestheticsaretheC.N.S.depressantdrugsthatproducea
partialortotallossofthesenceofpain,accompaniedbylossofconsciousness.
GeneralAnaestheticsisthecontrolled,reversibledepressionofthe
functionalactivityofC.N.S.anddepressvitralfunctionsofalltypesofcells,especially
thoseofnervoustissues.

4. The stage of anaesthesiaare:
1.Analgesiawhichisduetodepressionofcorticalcentres.
2.Excitementduetodepressionofhighermotorcentres.
3.SurgicalAnaesthesiawhichincludes
a)lossofspinalreflexes
b)skeletonmusclerelaxation
c)somaticmusclerelaxationanddisappearanceofmuscletone.
Thisstageisessentialtocarryonsurgicaloperation.
4.The4
th
stageismedurallaryparalysiswhichisduetooverdose.inthistheirisrespiratoryfailureand
vasomotorcollapse.

5. Classification
Depending upon the route of administration general anaesthetics are placed
into two major groups
(A)Volatile and gaseousanaesthetics administered byinhalation
1.Gases:
a)Inorganic gases e.g. Nitrous oxide. b)hydrocarbon e.g. Cyclopropane, ethylene.
2. volatile Liquids:
a)Halogenated hydrocarbon e.g. Halothene, trichloroethylene.
b)Ethers e.g. Diethyl ether.

6. (B)fixed anesthetics administered intravenously:
a)Ultra-short acting barbiturates and thiobarbiturates
e.gmethohexital sodium,Thiopental sodium.
a)Miscellaneous compounds e.g. ketamine, Alphaxalone.

7. Thiopental sodium or thiopentone sodium
Chemical Name:
Sodium;5-ethyl-4,6-dioxo-5-pentan-2-yl-1H-pyrimidine-2-thiolate

8. Stability and storage:
It is hygroscopic and is decomposed by atmospheric CO2. hence, it is stored in
tightly-closed containers
Uses:
It is used
1.as an anticonvulsant.
2.for induction of general anesthesia.
3.for preventation and treatment of cerebral ischaemia(Low oxygen supply to
brain).

9. Pharmaceutical formulations:
Thiopentone injection I.P.
Brand names:
Pentothal sodium
Intraval sodium.

10. Ketaminehydrochloride
Chemical name:
2-(2-chlorophenyl)-2-(methylamino) cyclohexan-1-one; hydrochloride.

11. Uses:
It is used as a General anaesthetics agents.
It can also be usedas an inducer of anaesthesia before the administration of
other anaesthesia agents.
storage:
Ketamine hydrochloride should be stored at controlled room temperature
and protected from light.

12. Pharmaceuticalformulations:
i)Ketamine hydrochloride injectionI.P.
ii)Ketamine hydrochloridetablet
iii)ketaminehydrochloride nasal spray bp.
Brandnames:
Ketaler, Anesketin, Ketamax, Ketamil,Ketamine,Radiopharm,
Ketaminolvet.

13. Propofol
Uses:-
1. Propofol is an intravenous (IV) sedative-hypnotic agent that:
i) Can be used for initiation and maintenance of monitored Anastheasia care
(MAC)sedation combined sedation and regional anesthesia.
ii)can be used for induction of general anesthesia.
iii)also used for the maintenance of general anesthesia.
Storage: It should be protected from light under an inert gas.

14. .
Pharmaceuticalformulations:
Propofoltablet, propofol capsule, propofolsyrup, propofolcream
propofolgel, propofolointment, Propofolliquid, propofol injectionI.P.
Brandnames: Celofol, critipol, diprivanneurof

15. HYPNOTICS AND SEDATIVES

16. Introduction
HypnoticsarethedrugswhichdepressC.N.Sandproducesleep,resembling
naturalsleepinnormaldose.Theyareusedtoovercomeinsomnia
(sleeplessness).
SedativesareC.N.Sdepressantsbutdonotinduse(produce)sleepinnormal
dosebutcalmsthenerves.Theyreduceexcitementofnervesandhenceare
usedinthereliefoftension,anxietyandrestlessness.

17. They are also useful
1) In potentiation of analgesic drugs .
2) To control epileptic seizures
3) As an adjunct to anaesthesia.
4) To treat hypertension.
5) In narcoanalysis in psychiatry , emotional strain.

18. Classification
1) Barbiturates : they are further classified depending upon duration of action .
a) Long acting barbiturates ( 6 hours or more)
eg. Barbitone, phenobarbitone
b) Intermediate acting barbiturates ( 3 to 6 hours )
eg. Butobarbitone
c) Short acting barbiturates ( less than 3 hrs. )
e.g. Cyclobarbitone
d) Ultrashortacting ( Intravenous) barbiturates ( ½ to 1 hrs. )
e.g. Methohexitonesodium, Thiopentonesodium

19. 2) Non-barbiturates
a) Benzodiazepine eg. Dazepam , Nitrazepam
b) Other cyclic nitrogen containing compounds amides and imides eg. Glutethimide, methyprylone
c) A cyclic nitrogen contianing compounds eg. Meprobamate, ethinamate
d) Alcohols and their derivatives eg. Triclofos sodium, ethchorvynol
e) Aldehydes and derivatives eg. Paraldehyde
f) Miscellaneous compounds.
e.g. Bromides, Antihistamines

20. 1. Phenobarbitoneor Phenobarbital
Storage :
It is stored in tightly-closed containers.
Uses :
1)Itisusedasasedativeinnervousinsomnia,anxietystates,Dysmenorrhoea(Crampsandpelvicpainwith
menstruation,withcommoncausessuchasheavyflow,passingclots,uterinefibroidsorendometriosis.)
2)Itisanticonvulsantandusedtotreatepilepsy.
3)Itisusedtotreatneonataljaundice(conditioninwhichaninfant'sskinappearsyellowwithinthefirstfewdaysofbirth.)
orgilbertssyndrome(common,harmlessliverconditioninwhichtheliverdoesn'tproperlyprocessbilirubin.)
Pharmaceutical formulation
Phenobarbitonetablets, Phenobarbitoneand theobrominetablets, Phenobarbitonecapsules, Phenobarbitoneelixir,
Phenobarbitonesodium tablets, Phenobarbitonesodium injection
Band Names : Gardenal, Garoin, Phenytal, Luminal

21. Diazepam
Storage :
1) It is degraded by moisture and light. It is stored in tightly closed & light resistant containers .
Uses :
1) For management (control) of anxiety and tension states.
2) For management of acute alcoholic withdrawal.
3) As an adjunct for relief of skeletal muscles spasm.
Pharmaceutical formulation
1.Diazepam tablets
2.Diazepam injection
3.Diazepam capsules
4.Diazepam elixir
Brand Names :Calmpose, Sedanite.

22. Alprazolam
Uses :
1) It is used to treat anxiety disorders and panic disorders.
2) It works by decreasing abnormal excitement in the brain .
Storage :It should be protected from light.
Pharmaceutical formulations
1.Alprazolam tablet
Brand Names : Alzolam, Alzopax, Zonil, Anxil.

23. Nitrazepam
Storage : It is degardedby moisture and sunlight and hence it is stored in
tightly closed light resistant containers.
Uses :
1)It is a hypnotic and sedetiveare used to treat insomnia.
2)It is also used to treat some forms of epilepsy.
Pharmaceutical formulation
1.Nitrazepam tablets
2.Nitrazepam capsules
Brand Names :Somnite, Sedamon, Hypnotex,Nitravet

24. Antipsychotics /Neurolepticsor
tranquillizers or psychotropic

25. Psychosis means mental condition characterized by disturbance
in mental functions.
Psychosis may be:
i)Organic psychosis where there is memory distarbance, cloudings of
consiousness. They may be due to head injuries.
ii)Functional psychosis may be;
a) Manic i.e. depressive psychosis or disturbance of mood.
b) Schizophrenia in which there is disorder of thoughts, emotions, motor
behaviour, perception etc.
c) Halucination.
d) Anxiety where there is feeling of fear, apprehension etc.

26. The drugs which are used to treat psychoses (psychiatric disorders)
are called psychotropic or antipsychotic or neuroleptics or
tranquillizers.
Classification of antipsychotics
1. PhenothiazineDerivatives and related tricycliccompounds:
a) Phenothiazinederivatives: Chlorpromazine, Prochlorperazine, trifluoperazine
b) Thioxanthines: Chlorprothixene, Flupenthixol
2. Butyrophenes: Haloperidol,Trifluperidol,Penfulridol
3. Dibenzodiazepines: Clozapine
4. Benzamidesand salicylamidese.g. sulpiride.
5. Diphenylbutylpiperidinederivatives e.g. Pimozide
6. Miscellaneous e.g. Reserpine ( alkaloid).

27. Chlorpromazinehydrochloride
1.Chemical Name:-
2-chloro,10-(3-dimethyl Amino propyl) Phenothiazine
2.Molecular weight:-355.3
3.Physical properties:-
Hydrochloride salt is white or cream colouredpowder.
It is very soluble in alcohol.
It becoming yellow to pink and finally violet.
4.Storage:-
It is stored in well closed container
Protected from moisture.

28. Uses:-
It is used to treat.
1.Schizophrenia.
2.Mania and hypomania.
3.Agitation associated with functional or organic psychosis.
It is used to control nausea and vomiting
It is also reduces salivary and gastric secretion
It has local anaesthetic property.
It is a vasodilator and brings about a reduction in blood pressure.

29. Pharmaceutical Formulation:-
1.Chloropromazine elixir.
2.Chloropromazine injection IP
3.Chloropromazine tablet IP
4.Chlorpromazine suppositories.
Brand name:-Largactil, chlorozine,copamide.

30. Haloperidol
1.Chemical:-
4-[4-(-chlorophenyl),4-hydroxy piperidine]4’-fluoro butyrophenone.
2.Molecular Weight:-375.9
3.Physical properties:-
It is white to faint yellowish.
It is odourlessand tasteless.
4.Uses:-
It is used to treat intractable hiccoughs.
It is antiemetic.
Used to treat acute schizophrenia
Used to treat mania and hypomania.

31. Pharmaceutical Formulation:-
1.Haloperiodol tablet IP
2.Haloperiodol injection IP
3.Haloperidol oral solution IP
4.Haloperidol elixir.
Brand name:-Halidol, Trancodol, Seranace.

32. Risperidone
1.Chemical Name:-
3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl) piperidin-1-yl]ethyl]-2-methyl-6,7,8,9
tetrahedropyrido[1,2-a] pyrimidin-4-one.
2.Uses:-
Risperidone is used to treat certain mental mood disorder.
Irritability associated with autistic disorder.(A serious developmental disorder that
impairs the ability to communicate and interact.)
3.Storage:-
preserve in tight light resistant containers
Store at control room temperature.

33. Pharmaceutical formulation:-
Risperidone tablet IP.
Risperidone Injection IP
Brand names:-respidon, sizodon and Risperdal.

34. Sulpiride
Chemical Name:-
RS-5-(Aminosulphony),N-[(1-ethyl,2-pyrrolidinyl)methyl]2-methoxy benzamide.
Storage:-
Store in cool, dry place in tightly closed container.
Keep container in a well ventilated place.
Uses:-
It is used in constipation.
It used to treat diyspepsia.(indigestion)
It is used in meniers diseases.(a disorder of the inner ear that can lead to dizzy spells (vertigo) and
hearing loss)
it is used to prevention of nauseas and vomiting

35. Pharmaceutical formulation:-
1.Sulpiride tablet
2.Sulpiride Capsule
3.Sulpiride Syrup
4.Sulpiride injection solution
Brand Names:-Sulpitac,Amipride and Zonapride.

36. Olanzapine
Storage:
It should be protected from light and moisture, stored at a temperature not exceeding 30°
Uses:-
1.Olanzapine was initially used orally and intramuscularly for the chronic treatment of
schizophrenia
2.In combination with lithium or valproate for the short term treatment of acute manic or mixed
episode associate it with bipolar I disorder in adult.
3.In combination with fluoxetine for the treatment of episode of depression
Pharmaceutical formulation:-
Olanzapine tablet IP
Olanzapine orally disintegrated tablet
Olanzapine and fluoxetine tablet IP
Brand Names:-Olazax,symbyax,zalasta

37. QUETIAPINE OR QUETIAPINE
FUMARATE
Storage:
It should be protected from light and moisture, stored at a temperature not exceeding 30°
Uses:-
1.Acute depression.
2.Anxiety disorder, generalized anxiety disorder
3.Major depresive disorder (MDD)
4.Mixed manic depressive episode
5.Post traumatic stress disorder (PTSD)(A disorder characterised by failure to recover after
experiencing or witnessing a terrifying event.)
6.Psychosis schizophrenia
Brand Name:-Quel, Socalm, seroquin and Seroquel.

38. Uses:
1.It is used for acute treatment of schizophrenia in adult.
2.Used in acute depressive episode.
Storage:
It should be protected from light and moisture, stored at a temperature not
exceeding 30°
Pharmaceutical formulation:-
Lurasidone tablet
Brand Names :-Latuda
LURASIDONE

39. Antidepressants

40. Antidepressants
Symptoms:
Feelings of sadness and moodiness are experienced.
Fatigue(tiredness),
headache,
insomnia,
G.I Disturbance,
anorexia(Loss of appetite),
Skeletal muscular complaint,
loss of sexual desire etc.
If this is left untreated, it can lead to suicide.
The drugs which are used to elevate the mood are called Anti –Depressants.

41. Classification
1. Typical tricyclic antidepressant
a) Iminodibenzyl derivative E.g. Imipramine
b) Dibenzoxepines E.g. Doxepine
c) Benzocycloheptanes and related compound E.g. Amitriptyline, Nor-triptyline
2. M.A.O. inhibitor
a) Hydrazide E.g. Phenelzine
b)Non-hydrazide
i) Cyclopropylamines e.g. Tranylcypromine
ii) sympathomimetics e.g. Dextramphetamine
3. A typical antidepressante.g. Dibenzepine iprindole
4. Miscellaneous
i) B-adrenoreceptor agonist e.g. Salbutamol
ii) Thyrotropin-Releasing Hormone(TRH)

42. Imipramine hydrochloride
Chemical name:
10,11-dihydro-5-(3-dimethyl aminopropyle) 5-H dibenzo(b,f) azepinehydrochloride
Stability and storage
It is Affected by moist air and light. Hence it is stored in tightly-closed light resistant
container protected from the moisture.
Uses:
It is used to treat
1.Depressive illness
2.Anxiety disorders
3.Anorexia nervosa (abnormally low body weight)
4.Pain
5.Phobias
Pharmaceutical formulations
Imipramine tables IP, Imipraminecapsules, Imipramineinjection, Imipraminemixture
Brand names :
Impratab, Depsonil, Antidep.

43. Amitriptyline Hydrochloride
Chemical name
3-(10,11 dyhydro,5H-dibenzo[a,d] cyclohept, 5-ylidine) propyl dimethyl amine,
Hydrochloride
Pharmaceutical formulations
1) amitriptyline injections
2) Amitriptyline tablets IP
3) Amitriptyline and perphenazinecapsules
Uses:
1. It is an anti Depressants:
2. It is used to treat
1.endogenous depression
2.Anxiety
3.Nocturnal enuresis in children
4.Chronic tension headache
5.chronic pain
3. It is also used for prophylaxis of migraine pain.
4. It is anticholinergic and has sedative property.
Brand name:
Amitrip, tryptinolamline, tryptomer, sarotena.
Stability & storage
It is oxidized by air in the presence of moisture and this reaction is catalyzed
by metal ions.
It is also affected in light hence.it is stored in tightly closed light resistant
containers.

44. Fluoxetine
Chemical name
Fluxotine hydrochloride is (RS)-N-mithyle-3-phenyle-3-[4-
trifluorimethyl)phenoxy]propylarnine hydrochloride.
Storage
It should be stored at room temperature protected from light.
Uses-
Fluoxetine is used to treat:
Depression, Obsessive compulsive disorder, Alcohol dependency
Anorexia nervosa, Bulimia nervosa, Cataplexy, Major depressive disorder
Myoclonus(Hiccups), Panic disorder, Premenstrual dysphoric disorder(PMDD)

45. Pharmaceutical formulations
1.Fluoxetine capsules I.P.
2.Fluoxetine oral solution IP
3.Fluoxetine tablet IP
4.Fluoxetine injection.
Brand names :Act fluoxetine, prozac, fludac, flunil, flupar
Sarafem, symbyax

46. Venlafaxine
Pharmaceutical formulations:
Venlafaxine Tablet
Venlafaxine capsule
Brand names :
Effexor,effexor-XR, venlor, Sentosa and veniz-XR.
Uses
1.Venlafaxine is used to treat depression.
2.Venlafaxine is indicated in the management of major depressive disorder.
3.Generalized anxiety disorder, social anxiety disorder,
4.Panic disorder with or without Agoraphobia (Fear of places and situations that might cause panic,
helplessness or embarrassment.)
5.Venlafaxine is also used for prophylaxix of migraine headache.
6.For reduction of vasomotors symptoms associated with menopause
7.For management of neuropathic pain.
8.It is also considered as line option for management of obsessive compulsive disorder(Excessive thoughts
(obsessions) that lead to repetitive behaviours (compulsions)

47. Duloxetine
Storage condition :
keep in a cool, dry place away from direct sunlight and moisture.
Uses
Indicated for :
1.Management of major depressive disorder.
2.Management of generalized and anxiety disorder
3.Management of diabetic peripheral neuropathy.
4.Management of chronic musculoskeletal pain.
5.Management of fibromyalgia.(Fibromyalgia is often accompanied by fatigue and altered sleep, memory
and mood.)
6.Management of osteoarthritis of the knee i.nadults.
7.Management of chronic lower back pain in adults
8.Management of stress urinary incontinence in adult human.
Pharmaceutical formulations:
Duoxetinegastro resistant tablet I P.
Brand names :
Cymbalta, DrIzalma, Irenka, yentreve

48. Sertraline
Uses :
It is used in the treatment of:
1.Anxiety disorder
2.Binge eating disorder.
3.Bulimia nervosa.
4.Major depressive disorder.
5.Obsessive compulsive disorder.
6.Panic disorder.
Brand names: Zoloft, Sereneta, Serline, Sertel
Pharmaceutical formulations-SertralineCapsule, SertralineTablet

49. Citalopram
Storage:
Stored at a temperature not exceeding 30°C and protected from moisture.
Uses :
Citalopram is used to treat :
1.Depression
2.Anorexia nervosa
3.Bulimia nervosa
4.Diabetic neuropathneuropathies.
5.Major depressive disorder
6. Obsessive compulsive disorder.
7 . Panic disorder
8. Post traumatic strees disorder.
Pharmaceutical formulations :
Citalopram tablet
Citalopram solution.
Brand names
Celexa ,Ctp, Feliz, Citadep, Celica

50. Escitalopram
Storage condition:
Store protected from moisture.
Uses:-
It is used to treat depression.
It is sometime used for anxiety.
It is also used in obsessive compulsive disorder or panic attacks.
Pharmaceutical formulations :
Escitalopram oxalate tablets
Brand names:
Lexapro , cipralex, esdep, feliz-s, nextid.

51. Fluvoxamine
Uses :
i) a selective serotonin reuptake inhibitors (SSRI) is used as an antidepressant.
ii) used in the management of bulimia nervosa.
Pharmaceutical formulations : Fluvoxaminetablet IP.
Brand name: Luvox, floxyfral,fluvoxin, sorest.

52. Storage condition :
store protected from moisture at a temperature not exceeding 30°C.
Uses:
1. It is used in the management of major depressive disorder.
2. To treat major depressive disorder.
3. To treat social phobia generalized anxiety disorder.
4. To treat the vehicle motor symptoms of manopause.
5. To treat premenstrual dysphoric disorder.
Pharmaceutical formulations :
Paroxetine Tablet I.P.
Paroxetine prolong-release tablet IP.
Paroxetine capsule
Brand names : Brisdlle, Paxil, Pexeva, Xet, Paxidep-CR
Paroxetine

53. Thank You…..