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This ppt covers the classification, structures and IUPAC names, Mechanism of action and uses of individual drugs...under anticonvulsants topic..Side effects/metabolism are also given for few
This ppt covers the classification of anti psychotics with structures and IUPAC names, MOA, uses, metabolism and side effects. Dopaminergic pathways also given
Unit iii heterocyclic compounds as per PCI Syllabus of POC-IIIGanesh Mote
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This slide discusses about fused heterocyclic compound Acridine..the structural analogue of anthracene with one carbon group is replaced with nitrogen atom.
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THIS SLIDE HAVE GOOD CONTENT. THIS SLIDE CONTAIN INTRODUCTION, STRUCTURE, RESONANCE, AROMATICITY, PHYSICAL AND CHEMICAL PROPERTIES, SYNTHESIS AND APPLICATION OF QUINOLINE.
This PPT on hypnotics and sedatives covers the Introduction, SAR classification and mechanism of action of drugs listed as per PCI syllabus for in medicinal chemistry for B. Pharmacy
THIS SLIDE HAVE GOOD CONTENT. THIS SLIDE CONTAIN INTRODUCTION, STRUCTURE, RESONANCE, AROMATICITY, PHYSICAL AND CHEMICAL PROPERTIES, SYNTHESIS AND APPLICATION OF QUINOLINE.
POLYNUCLEAR HYDROCARBON : STRUCTURE AND USES OF NAPHTHELENE, ANTHRACENE,DI-PH...RishikaBehere1
Hello everyone, we the students of Gurunanak College of Pharmacy, Nagpur have created a presentation of subject pharmaceutical organic chemistry -2 of third semester, Unit 4 : polynuclear hydrocarbons . This presentation was made for the purpose of better understanding of the topic structure and medicinal uses of naphthelene , anthracene, diphenylmethane , triphenylmethane , phenanthrene and their derivatives . This portion covers topics like structure, properties , and medicinal uses of polynuclear hydrocarbons such as naphthelene , anthracene , di-phenylmethane, tri-phenylmethane , phenanthrene and their respective derivatives.
This presentation explain the knowledge about sedative and hypnotics drugs also its physical properties, storage ,uses,dose, brand name and marketed formulations.
ANALEPTICS Mrs Namrata Sanjay Mane Department of Pharmaceutical Chemistry...NAMRATAMANE8
ANALEPTICS
Mrs Namrata Sanjay Mane
Department of Pharmaceutical Chemistry
Nagpur College of Pharmacy, Wanadongri, Hingna Road, Nagpur-441110,Maharashtra, India.
This topic covers drugs of Sedative & Hypnotic especially from Benzodiazepine class including drugs such as Diazepam , Nitrazepam, Lorazepam, Oxazepam etc also deals with drugs of alcohol class.
reference should be take from Med Chem by Algarswamy , Organic Chemistry by Robert Neilson Boyd and Robert Thornton Morrison or any other suitable reference book.
It contains classification, SAR, MOA, metabolism and usd of hypnotics and sedatives. Barbiturates and benzodiazepines were discussed as per PCI syllabus. This helps B.Pharm students to learn with focus
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Sedatives and Hypnotics
1. TOPIC: SEDATIVE AND HYPNOTIC:
MAHATMA GANDHI INSTITUE OF PHARMACY,
LUCKNOW
Presented by:-
MOHHAMAD AFAQUE
Assistant Professor
Department Of Pharmaceutical Chemistry
( M. Pharm
Medicinal Chemistry)
2. Sedatives and Hypnotics:-
Sedatives:-
➢ Sedatives are central nervous system drugs that reduce
excitement, tension and produce relaxation.
Lower concentration of drugs act as sedatives.
Hypnotics:-
➢ Hypnotics are those drugs that depress the CNS and produce
sleep similar to natural sleep.
➢ Higher concentration of the same drugs may act as hypnotic.
Classification of sedatives and hypnotics:-
Sedatives and hypnotics are classified on the basis of their chemical
structure:-
3. 1. Barbiturates:- Barbiturates are further subdivided into three types a)
long acting b) short-acting c) ultra-short acting.
2. Example of barbiturates:
a) Phenobarbitone
b) Butabarbitone
c) Cyclobarbitone
Benzodiazepines: e.g.
a) Nitazepam
b) Diazepam
c) Oxazepam
d) Alprazola
4. 3. Alcohol and Aldehyde:- e.g. Paraldehyde
4. Miscellaneous:- e.g. 1.Methyprylone, 2. Glutethimide, 3. Triclofos sodium
1. Barbiturates are further subdivided into three types:-
A ) Long acting b) short-acting c) ultra-short acting.
➢ The first two are used as sedatives and hypnotics and last one used as general
anaesthesia (e.g. thiopentone)
➢ The sodium salts of barbiturates are freely soluble in water.
Structure of barbiturates:-
N
N
O
O
O
H
R1
R5
R5'
5. a) Long-acting barbiturates:-
Phenobarbitone:-
➢ Phenobarbitone is the derivatives of barbituric acid derivatives.
➢ Phenobarbitone is a long-acting barbiturates derivative.
Structure of Phenobarbitone
N
N
O
O
O
H
H
CH2CH3
1
2
3
4
5
6
Phenobarbitone
R5= CH2CH3
R5'= -C6H5
Pyrimidine
Ethyl
Phenyl group
6. IUPAC Name:- 5-ethyl-5-phenyl-2,4,6[1H,3H]-pyrimidine-trione.
Physical properties:-
➢ It is a colourless white crystalline powder.
➢ It has no odour.
➢ It is very slightly soluble in water.
➢ It is soluble in alcohol and ether and sparingly soluble in chloroform.
Chemical properties:-
➢ When phenobarbitone is dissolved in ethanol and one drop of cobalt
chloride solution and one drop of dil. Ammonia solution are added, a violet
colour is produced.
7. ➢ If phenobarbitone is dissolved in methanol and a mixture of cobalt chloride and
calcium chloride solution is added to this solution and then after mixing and
shaking, dilute sodium hydroxide solution is added, a violet-blue colour and a ppt
are produced.
Stability and storage:-
➢ It can be affected by carbon dioxide of the atmosphere store in tightly closed
containers.
Official:
1. Phenobarbitone, I.P, B.P, 2. Phenobarbitone sodium, I.P, B.P, 3.
Phenobarbitone tablets I.P, B.P
8. Brand name:-
1. Gardenal
2. Luminal
3. Somonal
4. Dormiral
Uses:-
1. It is used in the treatment of sedatives and hypnotics.
2. It is also used in the treatment of anticonvulsant.
Butobarbitone:-
➢ This compound has the same structure as barbitone but differs from it is
having a n-butyl group at 5th position.
9. Structure:-
Physical Properties:-
➢ It is a colourless or white crystalline powder.
➢ It is practically odourless
➢ It is slightly soluble in water.
➢ It is soluble in ether and freely soluble in ethanol and in chloroform.
N
N
O
O
O
H
H
CH2CH2CH2CH3
CH2CH3
5-Butyl-5-ethyl-pyrimidine-2,4,6-trione
n-butyl group at 5th position
10. Chemical properties:-
➢ If butobarbitone is dissolved in methanol and a mixture of cobalt chloride and
calcium chloride solutions is added to the solution and then after mixing and
shaking, dilute sodium hydroxide solution is added, a violet-blue colour and a
precipitate are produced.
Stability and storage:-
➢ It should be store in well closed containers.
Official:-
1. Butobarbitone, B.P
Brand Name:- 1. Neonal, 2. Butabarbital, 3. Etoval
11. Uses:-
1. It is used in sedative and hypnotic.
Cyclobarbitone:-
➢ Cyclobarbitone also known as cyclobarbital.
➢ It is a barbituric acid derivative.
Physical Properties:-`
1. Cyclobarbitone is shiny crystalline powder
2. It has bitter taste
3. It has melting point 171-174℃.
4. It is very slightly soluble in cold water, more soluble in hot water and alcohol.
12. 5. It is insoluble in chloroform and ether.
Chemical Properties:-
➢ If a small amount of the cyclobarbitone calcium is added to a mixture of
vanillin in alcohol, sulphuric acid and water, shake and allowed to stand for 5
mint, a greenish-yellow colour is formed slowly. It become dark red when it is
heated on a water bath for ten mints.
Stability and storage:-
➢ It should be store in air tight container.
Official:- 1. Cyclobarbitone calcium, B.P
Brand name
1. Sonaform, 2. Hexemal,3. Phanodorm
13. Uses:
➢ It is used as a sedative and hypnotic.
Benzodiazepine:-
➢ Benzodiazepines are a class of sedative drug, also known as tranquillizers.
➢ Benzodiazepine is a heterocyclic compounds containing two nitrogen atoms.
➢ Benzodiazepine drugs are diazepam, Nitrazepam, Alprazolam etc.
Structure of Benzodiazepine:-
N
N
R1
O
R2
benzene ring
Diazepine ring
phenyl
ring
7-membrer ring conating 2 hetero atoms name as
(diazapine)
Nitrazepam:- R1= NO2, R2= H
Diazepam:- R1= Cl, R2= CH3
14. Nitrazepam:-
➢ Nitrazepam is a benzodiazepine derivative.
➢ Benzodiazepine is obtained by the fusion of one benzene ring and one
diazepine ring which is a 7-membered ring containing two nitrogen atoms.
➢ It contains also one phenyl ring and a nitro group is substituent.
Structure of nitrazepam:-
IUPAC Name:
N
N
O2N
O
H
7-Nitro-5-phenyl-1,3-dihydro-benzo[e][1,4]diazepin-2-one
15. Physical properties:-
➢ Nitrazepam is a yellow, crystalline powder.
➢ It has no odour.
➢ It is melt at about 226℃ with decomposition.
➢ It is practically insoluble in water, slightly soluble in ethanol and ether.
Chemical Properties:-
➢ If nitrazepam is dissolved in methanol and dilute sodium hydroxide solution
is added, an intense yellow colour is produced.
➢ Nitazepam conatins a nitro group on the benzene ring, it can be reduced to
amino group and diazotized by adding HCl and sodium nitrite. After adding
sulphuric acid, it can be coupled with N-(1-naphthyl) ethylenediamine
hydrochloride to give a red colour.
16. Stability and storage:-
➢ It should be store in well closed containers.
Official:-
1. Nitrazepam, I.P, B.P
2. Nitrazepam tablets, I.P, B.P
3. Nitrazepam capsules, B.P.
Brand name:-
1. Sedamas
2. Hypnotex
3. Nirven
Uses:- 1. It is a long-acting hypnotic with good sedation.
17. Paraldehyde:-
➢ Paraldehyde is a polymer of acetaldehyde.
➢ It is a trimer and consists of three molecules of acetaldehyde.
➢ When concentrated HCl or sulphuric acid is added to acetaldehyde,
polymerization of acetaldehyde to paraldehyde formed.
Structure:-
IUPAC Name:- 2,4,6-Trimethyl-1,3,5-trioxane
O
O
O
CH3
CH3
H3C
18. Physical properties:-
➢ Paraldehyde is a transparent, colourless or pale yellow liquid.
➢ It has strong and characteristic odour.
➢ It solidified at low temperature to give a crystalline mass.
➢ It is soluble in water but less soluble in boiling water.
➢ It is miscible with ethanol, ether, chloroform and volatile oils.
Chemical properties:-
➢ If ammonical silver nitrate is added to a solution of paraldehyde and heated
on water a bath, silver is deposited as a mirror on the side of the test tube.
➢ It can be decomposed by boiling water with sulphuric acid.
19. Storage and condition:-
➢ It is easily oxidized to acetic acid, it should be store in a small, well-filled,
airtight container.
➢ It should be protected from light and store at a low temperature.
Official:-
1. Paraldehyde, I.P, B.P
2. Paraldehyde injection, B.P.
Brand name:-
1. Paraldehyde
2. Paracetaldehyde
20. Uses:-
1. It is used as a hypnotics
2. It has no analgesic and anticonvulsant action.
Glutethimide
➢ Glutethimide is a derivative of 2,6-piperidinedione.
➢ In glutethimide one ethyl group and one phenyl group are present at the third
carbon atom to give glutethimide.
Structure:-
IUPACName: 3-ethyl-3-phenyl-2,6-piperidinedione.
H
N
O
O
C6H5
C2H5
21. Physical Properties:-
➢ Glutethimide is a white powder
➢ It has colourless crystals.
➢ It melts at 86 to 89℃.
➢ It is practically insoluble in water, freely soluble in alcohol, soluble in ether
and very soluble in DCM. (Dichloromethane).
Chemical properties:-
➢ When glutethimide is dissolved in methanol and a cooled mixture of formalin
and conc. Sulphuric acid is added and heated on a water bath, the solution
becomes red and produced.
22. Stability and storage:-
➢ It should be store in well close containers and protected from light.
Official:-
1. Glutethime, B.P
Brand Name:-
1. Doriden, Elrodorm
Uses:- 1. It is used as a hypnotics.
Methyprylone:-
➢ Methyprylone is a derivative of 2, 4-piperidinedione.
Physical Properties:-
➢ It is a white, crystalline powder.
23. ➢ It has a bitter taste and a slight characteristic odour.
➢ It melts at about 76-77℃.
➢ It is soluble in water.
➢ It is soluble in alcohol, ether, benzene and chloroform.
Storage and Stability:-
➢ It should be store in well-closed containers, and protected from light.
Brand Names:-
1. Noludar
2. Noctan, 3. Dimerin.
Uses:- 1. It is used as hypnotic.