ANTIBIOTICS-Introduction and Classification

Antibiotics

1. 4. ANTIBIOTICS Presented By- Mr. Dattatraya B Thorat M. Pharm. Head of Department PRES, Institute of Pharmacy, Loni.

2. ANTIBIOTICS Defination ÷ Antibiotics are the chemical substance derived from metabolically produced by living organism which are capable of inhibiting a small life process of other micro organism in small concentration NOMENCLATURE OF ANTIBIOTICS: - Previously known antibiotics where named on very subjective basis a) Some antibiotic where named from microbs from which they are derived . E.g : Sterptomycin as it is obtained from streptomyces griseus .

3. B) Some are named after their laborotary E.g : Nystatin as it is produced in New York state board of health laboratory C) some were named after secretary E.g.. Nacimycin as the name of secretary was Nancy . D) some were named after movies E.g. Rifonycin derived from the movie Riffi E) Some are named after patient E.g. Bacitracin because the name of patient was Tracy F) Some are named after culture number E.g. Standing as it was isolated from the culture name eight and so on. To avoid the confusion the committee by American chemical role society of microbiolgy to frame role which are as follows -

4. 1) If chemical structure is known as then name should be based on chemical structure . 2) If chemical structure unknown then germs can be used as a route . a) the suffix mycia is restricted to the antibiotics obtained from Sterptomycin Specis . E.g. Neomycia b) The suffix mycin is restricted to antibiotics which etc derived from micromomospora spp . 3) Failing the use of germ the mode of acting or spectrum of activity should be useful ..

5. Classification :- A)Depending upon system of antimicrobial activity . a) Nature Spectrum antibiotics :- The antibiotics having high degree specific i.e they are selectively effective either on gram positive and negative bacteria or certain fungi or antibiotics e.g.. Benzyl penicillin b) Broad spectrum antibiotics . The Antibiotics which are large number of pathogen not only gram positive or gram negative bacteria but also effect on intracellular microorganism like virus and rickets are called broad spectrum antibiotics e g . Tetracycline Streptomycin

6. B) Depending upon biosynthesis :- a) Antibiotics derived from amino acid 1) from simple amino acid : e.g. Chlorophenol 2) From two amino acid eg : Benzyl penicillin 3) from many amino acid e.g. Bacteria b) Antibiotic derived from sugar e.g. Benzyl penicillin streptomycin neomycin gentamyacin c) Antibiotics derived from acetates and propannuate e.g Tetracycline

7. d ) Miscellaneous. e.g. Griseofulein Rifamcia C) Depending upon on the basis of chemical structure a) B.lactum antibiotics { contain B.lacture beterocycle } E.g. Benzyl penicillin Benzathin , Penicillin phenoxymethyl penicillin ,Ampicillin, cerebencillin , cephalondine , Cepharhin , cephalexin . b) non- lactum antibiotics [does not contain B- lactum ring] 1) antibiotics containing hydraonapthalene ring. Eg Tetracycline 2) amino glycoside antibiotics e.g. Sterptomycin , Neomycin Gentamyacin 3) Macrolide amtibiotics e.g Erythromycin 4 ) Ansmycin e.g Rifampicia

8. 5) Polyene antifungal antibiotics e.g. Nystain hamycin Amphaterenin 6) Anthracyclin 7) petide antibiotics e.g Bacteria 8) Steriodal antibiotics e.g Fruscride acid 9) Necloside Antibiotics e.g Furomycin 10) other hetrocyclic ring containing antibiotics e.g Mitomycin , cycloserine 11) Non classifible antibiotics e.g Griseofulvin , chloromphenical

9. Basic structure of protein BENZYL PENICILLIN :-

10. Amphicillin :- Phenoxy methyl penicillin :-

11. Chemistry of pencillin : Penicillin contain B- lactum ring 4-membered of cyclic amide is fused with Thiozoledin ring so that nitrogen atom Adjucent carbon atom are common to both ring this gives bycyclic hetrocyclic system called phenom .

12. 1) Benzyl penicillin ( penicillin-G) Physical properties:- 1) It is white finely crystalline powder having faint characteristic odour. 2) They are hygroscopic. 3) Very soluble in water.

13. Chemical properties :- In Strongely acidic medium penicillin undergose degradation in which B- lactum and thiorodic ring are open giving penicillinis acid In presence of alkali it is hydrolised to penicilloic acid by opening a B- lactum ring

14. Stability and storage It is store in tightly closed container. Use : It’s used as to treat :- 1) Absence [Formulation of pus ] 2) Cephylis 3) Gonorrhoea [Caused due to Gonocal infection ] 4) Pharyngitis 5) Pneumonia 6) Meningitities 7) Endocarditis Formulation 1) Benzyl penicillin Injection 2) Benzyl penicillin eye drop 3) Benzyl penicillin eye ointment 4) Procaine penicillin Injection Brand name pentides , PAM , Crystopen

15. 2) Benzathin penicillin Physical properties 1) It is white crystalline powder 2) It is odourless 3) It is hygroscopic 4) It is slightly soluble in water Stability and storage It is stored in tightly closed light resistant container at temperature not exceeding 25°C Formulation 1) Benzathine penicillin Tablet 2) Benzathin penicillin oral Suspension 3) Benzathin penicillin static suspension 4) Benzathin penicillin Injection

16. Use: 1) It is used to treat 2) Absence 3) Gonorrhoea 4) Phoroyngitis 5) Pneumonia Brand name : penidure , Longacillin 3) Phenoxy methyl penicillin:

17. Properties : 1) It is white , Crystalline Powder 2) It is odourless 3) It is slightly bitter taste 4) It is very slightly Soluble in water &freely soluble in alcohol . Storage : It is stored in tightly closed container . Use : It is used to treat : 1) Abcesses 2) Cyphylics 3) Gonorrhoea 4) Pneumonia Formulation : 1) Phenoxy methyl penicillin capsule 2) Phenoxy methyl penicillin Tablet 3) Phenoxy Methyl penicillin suspension Brand name Penotried , Depan , Crystapen

18. 4) Ampicillin Properties : 1) It is white crystalline powder 2) It is odourless 3) It is a bitter taste 4) It is slightly soluble in water and very slightly Soluble in alcohol Storage : It is stored in tightly closed container in a cool place

19. Use: 1) Gonorrhoea 2) Menigitits 3) Enteric infection 4) Urinary track infection preparation : Capsule Tablet Suspension Sterile Solution Injection Brand name : Ampicillin

20. 5) Carbanicillin Properties : 1) It is almost hygroscopic powder or white crystalline powder 2) It is odourless 3) It has bitter taste 4) Freely soluble in water , practically insoluble in other and chloroform. Storage : It is stored in tightly closed container in a cool place.

21. Uses: 1) It is used to treat Respiratory track infection. 2) It is used to treat urinary track infection Dosage form: Carbenecillin Injection Brand name: carbepan , Carbalin . 6) Cloxacillin : Properties: 1) It is white crystalline powder 2) It is odourless 3) It has bitter taste 4) It is freely soluble in water, Slightly soluble in chloroform 5) Temp. Is not more than 25°C.

22. Storage : It is stored in tightly closed container. Use : 1) It is used to treat the respiratory track infection 2) It is use to treat the urinary track infection 3) It is use to treat the aritis media meningitis. preparation : Tablet Capsule Suspension Injection Brand name Cloxine , Cloxa -A

23. 7) Cephadospories : Eg . Cephalaxin. Properties : 1) It is cream colour crystalline powder 2) It has characteristic odour 3) It is Sparingly soluble in water slightly Soluble in alcohol and chloroform Chemical properties:- with the mixture of Sulphuric acid and nitric it gives yellow colour Stability & Storage : 1) It is absorbed the moisture it is after by light. 2) It is stored in tightly closed light resistant container at temperature not exceending 30°C.

24. Use : 1) It is used to treat Respiratorytrack infection 2) It is use to skin & soft tissue infection i ) otitis media ii)Urinary track infection iii) Bonel joint infection v) Dental infection Formulation : 1) Cephalaxin Tablet 2) Cephalexin Capsule 3) Cephalexin mixture Brand name : Cephaxine , Neocet cephaxin

25. 8) Cephaloridine Properties: 1) It is white crystalline powder 2) It is odourless. 3) It has slight odour pyridine 4) It has bitter taste , Freely soluble in water discoloured in presence of light. Chemical properties : With mixture of Sulphuric acid and nitric acid it gives permanent bluish green colour . Stability and Storage : It is discoloured on expansion to light hence it is stored resistance container which one sealed to excluide micro organism on kept in cool place

26. Use : 1) It is antimicrobial agent 2) It is used to treat UTI &RTI 3) It is used to treat infection of skin and soft tissue 4) bone and joint infection Formulation : Cephalaridine Injection Brand name : Cephalodin , cephadine 9 ) Cephalondine : Properties : 1) It is white crystalline powder 2) It is odourless 3) It is freely soluble in water and insoluble in alcohol .

27. Storage : It is store in tightly closed container and temperature not exceeding 25°C Use : 1) It is used to treat U.T.J 2) R.T.I 3) Skin and soft tissue 4) Bone and Joint infection . Preparation : Injection Brand name : keflin , Seffine

28. Non lactum antibiotics :- 1 ) Neomycin : Properties : 1) It is white or yellowish white powder 2) It is a hygroscopic 3) It is freely soluble in water slightly Soluble in alcohol Chemical Properties : Solution of substances in pyridine when heated on water bath with Ninhydrin between 65°C to 70°C for 10 min Deep violet colour produced Uses : 1) It is used broad spectrum antibodies 2) It is used to treat Staphylococal infection of skin , eye and also GIT infection on oral administration 3) In hepatic coma

29. Formulation :- 1) Neomycin cream 2) Neomycin eye drop 3) Neomycin eye ointment 4) Hydracortison and neomycin cream 5) hydrocortion and neomycin eye drop 6) neomycin , bacteria , polymixin eye drop Brand name : Dexbr -N , Dexacoart –N , Ne- Ba - Suif . Neospeorin 2 ) Gentamicn : 1) It is white to cream coloured powder 2) It is soluble in water and insoluble in Chloroform

30. Storage : It is stored in tightly closed container in a cool place. Uses : 1) It is used in broad spectrum antibiotics 2) It is used in treatment of septicemia 3) It is used in surgical infection 4) It is used to treatment of endocarditis . Formulation : 1) Gentamicin injection 2) Gentamicin cream 3) Gentamicin eye drop 4) Gentamicin ointment Brand name : Gentamicin , G- Mycin , Gentapor

31. 3) Tetracycline : Properties : 1) It is yellow crystalline powder 2) It is odourless 3) It has bitter taste 4) It is slightly soluble in water and soluble dil. Acid Uses : It is used to treat Bronchitis : a) Urinary track infection b) Syphilis c) Gonorrhoea d) Rat bite fever e) Acne f) Plague g) Malaria h) Amoebic dysentery i ) infection of eye

32. Formulation : 1) Tetracycline capsule 2) Tetracycline Tablet 3) Tetracycline Injection 4) Tetracycline eye ointment 5)Tetracycline Infusion Brand name: Furomycin , Enterocycline Enterocycline , Cadicydine 4 ) Erythromycin : Properties : 1) It is white or yellowish white crystal 2) It is odourless 3) It has bitter taste . 4) It is hygroscopic and soluble in water but soluble in dil.HCL

33. Stability : It is affected by light , moisture hence it is stored in tightly closed light resistant container at temperature below 30°C. Uses : 1) It is used to treat 2) Gonorrhoea 3) Pneomonia 4) pelvic inflammation 5) Urethritis 6) Amoebic dysentry 7) Wound and burn infection Formulation : 1) Erythromycin Tablet 2) Erythromycin Injection

34. 3) Erythromycin soluble Tablet 4) Erythromycin capsule Brand name : Erythrocin , Althrocin 5 ) Chlorophenical Properties 1) It is white greenish powder or yellowish white crystaline powder or needle or dongated plate 2) It is odourless and has bitter taste 3) It is slightly soluble in water freely soluble in alcohol Uses : 1) It is used to treat a) Thyphoid b) Parathyphoid

35. c) Menigitis d) Urinary track infection e) Ricket infection f) Infection of eye and eye e) skin infection Formulation 1) Chlorophenical capsule 2) Chlorophenical eye drop 3) Chlorophenical eye ointment 4) Chlorophenical injection suspension Brand name : chlorostrep , Enterostrep . Enteromycin ,o- mycin

36. Structure of 6) Griseoflavin : 1) It is white or pale cream coloured powder 2) It is tasteless 3) It is odourless 4) It is slightly soluble in water. Soluble in acetone , Freely soluble in tetrachloraethane

37. Chemical Properties: when it is treated with potassium dichromate in presence of Sulphuric acid white red coloured produced . Storage : It is a stored in tightly closed container. Uses : i ) It is used in antifungal agent against wide range dermatophytose it get deposited keratin of skin hair, Nails thus it prevent fungal infection of newly from sepsis. ii) Therefore, it is used in treatment of infectiyon caused by ringwarm , Trychophyton species epidermophytone Species.

38. Properties : 1) Griseoflavin Tablet 2) Griseoflavin Capsule 3) Griseoflavin oral Suspension Brand name : Grisovin , Fungivin , Bifulvin .

39. Thank You..