Chemotherapy notes for B. Sc Nursing students

1. CHEMOTHERAPY
By: Mrs. Kalaivani Sathish M. Pharm
Assistant Professor,
PIMS - Panipat

2. Definition
 The treatment of disease by the use of
chemical substances, especially the
treatment of cancer by cytotoxic and other
drugs.

3. UNIT OVERVIEW
 Penicillin and Sulphonamides
 Broad Spectrum Antibiotics
 Aminoglycosides and Treatment of UTI
 Macrolides and Misc. AMA
 Quinolones
 Anti TB, HIV – AIDS Drugs & Treatment of
AIDS.
 Anti Leprosy Drugs & Treatment of
Anaerobic Infections

4. UNIT OVERVIEW (Cont…)
 Anti Cancer Drugs
 Treatment of Amoebiasis, Helminthic
Infections
 Antifungal Drugs
 Anti Septics and Disinfectants

5. PENICILLIN
•Alexander Fleming
•Pencillin was discovered by
chance in 1928.
•It was the first antibiotic to
be used clinically in 1941.
•It was originally obtained
from the fungus Penicillium
notatum, but the present
source is P. Chrysogenum

6. CLASSIFICATION
A. Natural – Penicillin G
B. Semi Synthetic
1. Acid Resistant Alternative To
Pencillin G {Phenoxy Methyl
Penicillin – Penicillin V}
2. Penicillinase Resistant Penicillin
{Methicillin, Cloxacillin}

7. CLASSIFICATION (Cont..)
3. Extended Spectrum Penicillin {3 Types}
A. Aminopenicillin. E.g., Ampicillin, Bac
Ampicillin, Amoxicillin
B. Carboxypenicillin, E.g., Carbenicillin, Ticarcillin
C. Ureidopenicillin, E.g., Pipercillin, Mezlocillin.
  - Lactamase Inhibitors – Clavulanic acid,
Sulbactam, Tazobactam

9. NATURAL PENICILLIN
 Penicillin G has a narrow antibacterial
spectrum and is effective against gram
positive cocci and bacilli and a few gram
negative cocci.
Resistance
Many organisms like staphylococci produce a
penicillinase which is a  - Lactamat.
It opens the  - Lactam ring and inactivate
penicillin

10.  Penicillin may not bind to the bacteria,
because of changes in the target protein,
this leads to resistance.

11. PHARMACOKINETICS OF
PENICILLIN G
 Penicillin G is destroyed by gastric juice. It could
interfere with its absorption hence it is to be
given 2 hours after food.
 It does not readily cross the BBB in the presence
of inflammation, therapeutic concentration is
attained in the CSF.
 It is excreted by the kidney.

12. PREPARATION & DOSE
 Penicillin G is mainly given parentally, Oral
Penicillin is used only in minor infections.
 Procaine Penicillin G (0.5 to 1 MU) 12 – 24 Hrs.
IM Route.
 Benzaphine Penicillin G (1.2 to 2.4 MU) Every
3 – 4 weeks, Deep IM.

13. ADVERSE EFFECTS
 Hypersensitivity
Other adverse effects includes
Pain at the site of infection, thrombophelebitis on
IV injections.
On CNS Large dose may produce confusion,
muscle twitching, convulsions and coma, supra
infections.

14. USES
 Pneumococcal infections – Pneumonia,
Meningitis, Osteomyelitis.
 Streptococcal infections – pharygitis, sinusitis,
pneumonia, meningitis and endocarditis.
 Meningococcal infection
 Staphylococcal infection
 Syphillis
 Diptheria
 Anerobic infections – pulmonary, dental and brain
abscess.

15. USES
 Actinomycosis
 Tetanus and Gas Gngrene
 Other infections – Anthrax, trench mouth, rat
bite fever and listeria infections.
 Prophylactic Uses Includes
 Rheumatic Fever, Gonorrhea and syphillis
 Valvular heart diseases.

16. DISADVANTAGE OF
NATURAL PENICILLIN
 Narrow spectrum of activity
 Not effective orally
 Susceptible to pencillinases
 Risk of hypersensitivity.

17. SEMI SYNTHETIC
PENICILLIN
 These are produced by chemically combining specific
side chain or by incorporating specific precursors in the
mould cultures.
 It has overcome the short comings of the Penicillin G,
which are as below
 Poor Oral Efficacy
 Susceptibility to Penicillinase
 Narow Spectrum activity
 Hypersensitivity reactions.

18. . Acid Resistant Alternative To
Pencillin G
 {Phenoxy Methyl Penicillin – Penicillin V}
 It differs from PnG. Only in that it is acid
stable and oral absorption is better , Peak
blood level is reached in 1 Hr & Plasma T –
½ is 30 to 60 minutes.
 The antibacterial spectrum of PnV is
identical to PnG.
 It is used only for streptococcal Pharyngitis,
Sinusitis, Ottitis media.

19. . Acid Resistant Alternative To
Pencillin G
 Prophylaxis of Rheumatic fever, less
serious Pneumococcal infections and
Trench Mouth.
 Dose – 250 – 500 mg for adults and for
infants 60 mg, children 125 – 250 mg given
6th Hourly.

20. Penicillinase Resistant Penicillin
{Methicillin, Cloxacillin}
 They are resistant to hydrolysis by
penicillinase produced by bacteria.
 They are less effective than PnG.
Methicillin
 It is highly penicillinase resistant but not acid
resistant.
 It is also an inducer of penicillinase production.
 MRSA (Methicillin Resistant Staph Aureus ) also
called as Super Bug Bacteria.

21.  MRSA have altered PBPs (Penicillin-binding
proteins)
Adverse Effects – Hematuria, Albuminuria,
Reversible interstitial Nephritis.
Adverse effects has been replaced by Cloxacillin.
Cloxacillin
It is less active against PnG sensitive organisms,
should not been used as its substitute. It is more
active than Methicillin against penicillinase
producing Staph, but not against MRSA.

22.  Cloxacilline is incompletely but dependably
absorbed from oral route especially when
taken in empty stomach.
 It is > 90 % plasma protein bound.
 It is eliminated by kidney primarily and
also partially by liver.
 Plasma T – ½ is about 1 Hour.
 Dose – 0.25 – 0.5 gram orally every 6 Hrs
for severe infection 0.25 to 1 gram may be
injected.

23. Extended Spectrum
Penicillin
 Aminopenicillin
 These agents cover a wider
antibacterial spectrum including many
gram –ve bacilli. They are orally
effective.
 1. Ampicillin
 It is active against all organisms sensitive to PnG
for Strepto. Viridens and Enterococci, equally
active for Pneumococci, Gonococci and
Meningococci.

24.  But less active against other gram
positive cocci.
 Pharmacokinetics
 Ampicillin is not degraded by gastric acid.
 Oral absorption is incomplete but
adequate.
 It is partially excreted in bile and
reabsorbed in entero hepatic circulation .
 Primarily excreted through kidney
 T – ½ Period is 1 Hour
 Dose – 0.5 to 2 gram Oral / IM & IV
every 6th Hour.

25.  Children Dose is 25 to 50 mg / Kg /
Day.
 Uses
 Drug of choice for Acute UTI.
 RTI including broncitis, Sinusitis,
Otitis.
 Meningitis
 Gonorrhoea – First line drug of choice
for oral treatment of non penicillinase
producing Gonococcal infection.
 Typhoid Fever

26.  Bacillary dysentery
 Cholecystitis (Inflammation of Gall
bladder)
 Sub acute bacterial endocarditis
 Septicemia
 Adverse Effects
 Diarrhoea is frequently common after
oral administration.
 Rashes especially in AIDS, EB
infected Patients.

27.  Drug Interactions – Hydrocortisone
inactivates ampicillin if mixed with IV
Solution.
 It interferes with oral contraceptives, failure
of oral contraception.
 Bac Ampicillin
 It is an ester of ampicillin.
 It is a pro drug i.e., better absorbed and
longer acting than ampicillin.
 Dose – 400 – 800 mg bd.

28.  AMOXICILLIN
 It differs from ampicillin in the following:
1. Amoxicillin is better absorbed orally
2. Food does not interfere with its absorption
3. Diarrhoea is rare
4. Amoxicillin is given thrice daily but
ampicillin is given 4 times a day.
USES
It is used in respiratory infection, UTI, Salmonella
gastroenteritis

29.  Doses
 0.25 to 1 gram Tds. Oral – IM
Carboxypenicillin
 In adittion to activity against gram +ve
and gram –ve organism is also
effective against P. Aeruginosa and
Proteas Infections.
 DOSE – 1 – 5 gram IV every 4 to 5th
Hour.

30.  Ticarcillin
 It is more potent than carbencillin but
properties are similar to each.
 Ureidopenicillins
 Piperapacillin – this anti pseudomonal
penicillin is about 8 times more active than
carbenicillin
 It has good activity against klebsiella and
used mainly in neutropenic.
 T – ½ IS 1 Hour. Dose : 100 – 150 mg / kg/
day

31.  Meziotilline
 It has activity similar to Ticarcilline.
 It is given parentally primarily for
infections caused by Enteric bacilli.

32.  - Lactamase Inhibitors
  - Lactamase are enzyme produced
by bacteria, that open up the  -
Lactam ring and inactive the  -
Lactam antibiotics.
  - Lactamase Inhibitors bind to
inactivate  - Lactamase, thus
preventing the destruction of  -
Lactam antibiotics.

33. CLAVULANIC ACID
INHIBITORS
  - Lactamases and is combined with
Amoxycillin for both oral and parentral
administration.
 The combination of Amoxycillin and
Clavulanic acid used for mixed
aerobic, anaerobic and Nosocomical
infections.
 Clavulanic acid is also combined with
Ticarcilline for Parentral use,

34. PHARMACOKINETICS OF
CLAVULANIC ACID
 It has rapid oral absorption and bio
availability of 60 % can also be injected.
 T – ½ is One Hour. It is eliminated mainly
glomerular filteration.

35. USES
 Skin and Soft tissue infection.
 Intra abdominal and gynaecological
sepsis.
 Urinary and RTI
 Nosocomical Infections (Hospital
Acquired Infections)
 Gonnorrhea – Single dose Amoxycilline 3
g. + Clavulanic acid 0.5 g + Probenecid 1
g.

36. ADVERSE EFFECTS
 Tolerance is poor especially in
children.
 Other side effects are Candida
stomatitis.
 Vaginitis and Rashes
 Hepatic Injury causes in combinations
of Clavulanic acids.

37. SULBACTAM
 It is a semi synthetic  - Lactamase Inhibitors.
 Related chemically and as well as in activity to
clavulanic acid.
 It is 2 – 3 times less potent time than clavulanic
acid.
 It does not induce chromosomal  - Lactamases.
 Preferably administered Parenterally

38. SULBACTAM
INDICATIONS
 Penicillinase-producing Neisseria gonorrhoeae
(PPNG).
 N. Gonorrhoeae.
 Mixed aerobic and anaerobic infections.
 Intra abdominal Gynaecological , surgical and
skin soft tissue infections, especially those
acquired in hospitals.

39. SULBACTAM ADVERSE
EFFECTS
 Pain at site of injections
 Thrombophlebitis
 Rashes and Diarrhoea.

40. TAZOBACTUM
 It is another  - Lactamase inhibitor
similar to sulbactam.
 Its pharmacokinetics mataches with
Piperacillin.
 It is used in severe infections like
Peritonits, Pelvic, Urinary, RI caused
by  - Lactamase producing bacilli

41. TAZOBACTUM (Cont)
 Dose – 0.5 combined with Piperacilline,
4 g IV, 30 Minutes for 8th Hourly.