Dr.U.P.

Rathnakar
MD.DIH.PGDHM
Chemotherapy -General
 Definitions
 Classification
 Problems from the use of AMAs
 Combined use of AMAs
 Prophylactic use of AMAs
Chemotherapy-Definitions
• Chemotherapy -Treatment of infectious
diseases using chemical substances –
(chemo: chemical agents, therapy:
treatment)
• Antibiotic -Substance obtained from
microorganisms and acts against
microorganisms
• AntiMicrobial Agent -Synthetic
substances act against microorganisms.
• Bacteriocidal- Kills microorganisms
• Bacteriostatic- Stops multiplication
• Broad spectrum- Act Against variety of
micro organisms
• Narrow spectrum- Act against limited
Classification
 Bacteriocidal-Penicillin,
Cephalosporin
OR
 Bacteriostatic- Tetracyclines,
Sulfa

Broad spectrum-
Tetracyclines
OR
Classification[MOA]….
 Inhibit cell wall synthesis- Penicillin,
Cephalosporins
 Affect cell membrane function-
Amphoterecin B
 Inhibit protein synthesis-
Chloramphenicol, Tetracycline,
Erythromycin, Aminoglycosides
 Antibiotics that inhibit nucleic acid
synthesis:
Rifampicin, fluoroquinolones, nalidixic
acid, anticancer agents, anti-HIV drugs
 Problems from the use of AMA
[Complications]
• Hypersensitivity[Allergy]- Urticaria [skin
rashes] to anaphylaxis
• Direct toxicity;
• Local- Pain. Eg. Penicillin injection or
gastritis by erythromycin
• Systemic toxicity- Hearing
impairment[oto toxicity] or affect kidneys
[Nephro toxicity]- Eg.Aminoglycosides
• Drug resistance: AMA not effective after
being initially effective
• Natural or acquired
 Problems from the use of AMA
[Complications]
• Super infection [Suprainfection]- New
infection because of use of AMAs
o Why?
o Normally Normal flora compete with
pathogens for food and also produce
substances called bacteriocins which inhibit
microorganisms- AMAs kill these flora-
o Predisposing conditions- Diabetes ,
Cortecosteroid therapy
o Organism-Candida
• Nutritional defeciencies- Intestinal flora
synthsize Vit K and B complex vitamins.
AMAs kill them
•
Combined use of AMAs
 Reduces - Bacterial resistance
 Increases - Efficacy and cure rate
 Increases the - spectrum of activity
 Reduce - duration of treatment
 Reduce the toxicity
 To achieve synergism
 Rifampicin
Amoxicillin

Benzathene pen Zidovudine

Prophylactic use
of AMAs
Cefazoline
[Chemoprophylaxis]
Co-Trimoxazole
 Cotrimoxazole is a mixture of two drugs
 Trimethoprim and
Sulphamethoxazole.[1:5]
 Combination increases the antibacterial
activity
 MOA-
 Prevent synthesis of folic acid in
bacteria.
 Bacteriocidal
 Each component inhibit different
enzymes[Sequential blockade]
 PABA[T→T]Dihydrofolate[S→S]Tetrahyd
Co-Trimoxazole….
Uses Adverse
2.Urinary tract effects[Toxicity]
infections 2. Hypersensitivity
[Allergic reactions]
3.Respiratory 3. Stevens-Johnson's
tract infections: syndrome
4.Typhoid fever 4. Jaundice,
5. Hemolytic anaemia,
5. Bacterial
6. Crystalluria
dysentery
Contra indicationsI-
8. Allergic to
sulphonamides.
9. Avoided during
pregnancy.
10.Hepatic and Renal
failure
Penicillins-[Beta lactam group]

Classification MOA
1. Natural penicillins:
Eg.Penicillin-G,  Inhibits
Benzathine penicillin
2. Semi synthetic bacterial
penicillins:
1.Acid resistant: cell wall
Eg.Penicillin V
2.Amino penicillins: Eg. synthesis
Amoxycillin,
Ampicillin  Bacterioci
3.Carboxy penicillins:
Carbenicillin dal
Penicillins
Adverse Uses
effects[toxicity]
• Penicillin -a safe  Tonsillitis
Natural Penicillin
antibiotic  Meningitis
• Hypersensitivity[Aller  Prophylactic use-
gy] reactions- Rheumatic fever
Anaphylaxis
Skin rashes  Typhoid fever Semi synthetic
• Bleeding  UTI Penicillins
abnormalities
• Convulsions

Precaution: Test dose

Cephalosporins [Betalactam
group]
Classificati MOA
on  Inhibits
 First generation
bacterial
Cefazolin, cefalexin
 Second cell wall
generation synthesis
Cefamandole,
 Third generation
 Bacterioci
Ceftriaxone, dal
 Fourth
generation
Cephalosporins…
Adverse Uses
effects[Toxicity] 1 Osteomyelitis
 Hypersensitivity 1 Surgical
[Allergy]. Skin prophylaxis
rash, 2 Orbital cellulites
 Anaemia, 2 Otitis media
 Jaundice, 3 Typhoid
 Superinfection 3 Gonnorrhoea
4 Severe hospital
infections[IV
Generation]
Aminogycosides
Parenteral[Injectio MOA
n]  Inhibit bacterial
 Amikacin protein synthesis.
 Gentamicin  Bactericidal.
 Streptomycin  Post antibiotic
 Kanamycin effect
[Act even after blood
concn is very low]
Topical
 Framycetin
 Neomycin
Aminogycosides….
Uses Adverse effects
 Urinary tract  Ototoxicity
infection [hearing]
 Endocarditis  Nephro
 Skin infections and toxicity[Kidney]
Intestinal  Motor end plate
antiseptic blockade[Muscle
[Neomycin] paralysis]
 Tuberculosis Contra indications
[Streptomycin]  Renal failure
 Hearing loss
 Caution with
muscle relaxants
Tetracyclines
Classification MOA
 Short acting  Tetracyclines
Tetracycline arrest bacterial
 Intermediate protein
acting synthesis[bind to
30S ribosome
Demeclocycline,
and ]
 Long acting
 Broad spectrum
Doxycycline,
 Bacteriostatic
minocycline
Tetracyclines
Uses Adverse effects
 Cholera  Superinfection
 Severe acne [Diarrhoea],
 Syphilis  Permanent
 Neonatal discolouration of
gonococcal teeth and bone.
conjunctivitis  Phototoxicity,
 Rickettsial  Hepatotoxicity,
infections Contra indications
 Trachoma  Pregnancy
 Periodontal  Children below 6
diseases: years
Chloramphenicol
MOA Uses
 Inhibits bacterial  Typhoid fever
protein synthesis.  Bacterial
[binds to 50S meningitis
ribosome]
 Anaerobic
 Bacteriostatic
infections – B.
 Broad spectrum fragilis
[Like tetracycline]  Rickettsiae
Chloramphenicol
Uses Adverse effects
 Aplastic anemia
 Typhoid fever [Bone marrow
 Bacterial depression]
meningitis  Grey baby
 Anaerobic syndrome in
infections – B. premature and
fragilis infants
 Rickettsiae  Allergy
Contrandicatiojns
 Neonates and
infants
 Fluoroquinolones
Classification MOA
First  Inhibit bacterial
Gen.Fluoroquinolone DNA gyrase
s andDNA synthesis
 Norfloxacin  Bactericidal
 Ciprofloxacin
 Ofloxacin
 Pefloxacin
Second
Gen.Fluoroquinolones
 Lomefloxacin
 Levofloxacin

 Fluoroquinolones…
Uses ADE[Toxicity]
 UTI  Tendonitis,
 Typhoid fever  Tendon rupture
 Gonorrhoea
 Superinfection
 Gastrenteritis
 Hypersensitivity[Alle
rgy]
CI
 Pregnancy.
 Children,
 Adolescents and
 Nursing mothers
 Macrolides
Classification MOA
 Erythromycin,  Inhibiting bacterial
 Azithromycin, protein synthesis
 Clarithromycin, PK
 Roxithromycin,  Emycin enzyme
inhibitor
 Hence produces
toxicity if given with
some drugs
 Azithromycin is not-
hence safer
 Azithromycin long
 Macrolides
Uses ADE[Toxicity]
 As an alternative for  Epigastric distress,
penicillin allergic nausea, vomiting
individuals and diarrhoea
 Bronchitis  Jaundice
 Chancroid Drug interactions
 Diphtheria  Inhibits
 Legionella infections enzymes[EMycin]
 Pertussis (Whooping  Hence produces
cough) cardiac toxicity with
Terfanadine
Anti viral drugs
MOA
viruses are merely
genetic information
surrounded by a
protein coat.
3. Fusion inhibition
4. Reverse
transcriptase
inhibition
5. Protease inhibition
6. Inhibit DNA
synthesis
 Anti viral drugs……
Uses ADE[Toxicity]
2. Herpes  Local stinging
3. AIDS sensation
4. Influenza  Nausea , vomiting
 Anemia
 Neutropenia
Drug interactions
 Common with PIs
Anti viral drugs
MOA
viruses are merely
genetic information
surrounded by a
protein coat.
3. Fusion inhibition
4. Reverse
transcriptase
inhibition
5. Protease inhibition
6. Inhibit DNA
synthesis
 Antifungal drugs
Classification MOA
Anti biotics:  Differs with
Amphoterecin-B[AMB], compound
Griseofulvin
Azoles:  Amph B-Makes cell
Clotrimazole wall
Econozole porous[Micropore]
Miconozole  Griseofulvin inhibits
Flucanozole mitosis[Cell
3. Others:
division]
Flucytosine[5-FC]
Terbinafine
 Azoles inhibit
4. Topical: enzymes required to
Tolnaftate synthesize cell wall
Whitfield’s ointment
Antifungal drugs…..
Uses Adverse effects
1. Systemic and 2. AMB is nephro toxic
topical fungal 3. Some azoles inhibit
infections synthesis of
androgens
2. Taenia
4. Hair loss,
versicolor
Gynecomastia
3.T.Cruris
4. Candidiasis DI
5.Histoplasmosis • Ketoconazole may
produce serious dru
interactions with
Anticancer drugs
Classification MOA
Alkylating agents  Varies with different
Cyclophosphamide, agents
Cisplatin  Inhibit cell division
at different phases
 Inhibit cell
Antimetabolites metabolism[Eg.Folic
Methotrexate, acid]
Antibiotics:
Doxorubicin,
Daunaorubicin
Natural products
Vincristine,
Vinblastine
Hormones and
antagonists
 Anticancer drugs
Uses Adverse effects
1. Different types of 2. The acute -nausea,
vomiting,
malignancy
3. Irritants, extravasation
3.Some are used as 4. Bonemarrow
immunomodulato suppression
rs 5. Alopecia
4.Methotrexate is 6. Immunosuppression
7. Terratogenic
also used in
AE: Specific treatment
rhematoid
• Cisplatin-Vomiting-
arthritis Ondansetron
5.Mostly used in • Cyclophosfamide-
combinations Cystitis-MESNA
• Methotrexate-
 Immunomodulators
Immunity Classification
• Advantages- • Immuno
 Required to fight suppressants
against foreign 3. Specific T-cell
bodies-INFECTION inhibitors
 When immunity is Cyclosporine
decreased[Eg.AIDS] 2. Cytotoxic drugs
IMMUNOSTIMULANTS
Methotrexate,
are used
Cyclophosphamide
• Disadvantages
3. Glucocorticoids-
 Rejects foreign Prednisolone
bodies.Eg. Kidney
4. Monoclonal
transplants
antibodies
 In such cases IMMUNO
• Immuno stimulants
SUPPRESSANTS are
 Immunomodulators
Immuno Immuno stimulants
suppressants  MOA:
 MOA: Non-specific
In general inhibit T stimulation of
cell proliferation immune system
which is required for  BCG Vaccine-
development of Bladder cancer
immunity  Some times used
 USES: non specifically in
As anti-rejection various infections,
drug in organ cancers
transplantation
 ADE
 Anti-tubercular drugs
Classification DRUG MOA ADE
• Mycobacterium INH [-]Cell Periphera
tuberculosis wall l Neuritis
Mycolic [Prevente
• First line drugs:[Less acid d by
toxic synthesis Pyridoxin
• More efficient] Rifampici [-] e]
Red
• Isoniazid, n Nucleic urine,
Rifampicin, acid Liver
Ethambutol, synthesis toxicity
Pyrazinamide, Pyrazinami [-] Liver
Streptomycin de Mycolic toxicity
• Second line drugs: Ethambut acid
[-] cell EYE-optic
Ofloxacin, ol wall neuritis
synthesis in
Ciprofloxacin,
Levofloxacin, Streptomy [-]Protein children
Nephro,
cin synthesis vestibula
Ethionamide,
r
TB Drug regimens-DOTS
 TB is curable
 Short course treatment- DOTS-Directly
Observed Treatment Short course
 Depending upon seriousness[Category}
treatment lasts 6 months to 8 months
 3 or 4 drugs for 2 months-INITIAL PHASE
 2 or 3 drugs for 4 to 6 months-
Continuation phase
 Treatment of Multi Drug Resistant [MDR]
requires longer duration
Anti-Leprosy drugs
• Mycobacteria
Drug MOA ADE
Leprae •Anemia,
• Drugs •Nausea
Dapsone [-]F.Acid • vomiting
Dapsone
Rifampici [-] •Red
Rifampicin n Nucleic urine,
acid • Liver
Clofazamine synthesis toxicity
Ofloxacin, Minocycline, Clofazami [-]DNA •Skin
Clarithromycin ne function discolour
ation
•Nausea,
Vomiting
Anti-Leprosy drugs
 Leprosy curable
 Rifampicin-
 Treatment
 Pauci bacillary 6 Once a
Months month-
 Multi Bacillary 12 Suprevised
months-12 months
 Clofazamina
and Dapsone
-Daily
 Malaria
• Falciparum and Drugs Adverse
vivax malaria Effects
Chloroqui •Nausea,
• Falciparum ne vomiting
malaria-No •Retinal
recurrence damage
• Vivax malaria-
Quinine •Nausea,
Recurs
vomiting
• Classification •Cinchonism
5.Used for clinical Primaquin •Anemia in
cure- e G6PD
• Mild- defeciency
Chloroquine, pts.
 Anti –Amoebic Drugs
Classification Drugs Adverse
Effects
Luminal-Diloxanide Metronidazol •Nausea,
furoate e •Vomiting
Extra intestinal •Interaction
only-Chloroquine with alcohol
Intestinal and
extra intestinal-
Metronidazole,
Emitine
A] Intestinal and
extra intestina
Anthemintic drugs
Classification
Round worm
Hook worm
Thread worm
Albendazole
Mebendazole
Pyrantel
Filaria-Diethyl
carbamazine
Tape worm-
Praziquintal,
Albendazole
Hydatid-Albendazole
Albendazole
Mebendazole
Pyrantel ROUND WORM
Albendazole
Mebendazole
Pyrantel HOOK WORMS
Albendazole
Mebendazole
Pyrantel HOOK WORMS
ariasis
rmectin and Diethyl Carbamazine
Tape Worm
Praziquintal, Albendazole
Individual agents
• Classification
• MOA
• ADE
• Uses
• Contra indications
 Penicillins. Cephalosporins.Co-trimoxazole
 Aminoglycosides.Tetracyclines.
Chloramphenicol
 Quinolones.Macrolides
 Antifungal, Antiviral
 Anti-cancer
 Immunomodulators
 TB, leprosy, amoebiasis, antihelminthics