Kipengele K,

Bpharm

Basic Pharmacology
NTA Level 4 Semester 2

2020
1
Description of Penicillin and
Cephalosporins

Session 4
 Description of Penicillin and
Cephalosporins
By the end of this session you should be able to:
• List indications of penicillins and cephalosporins
• List contraindications of penicillin and
cephalosporins
• Describe dose, dosage and course of penicillins
and cephalosporins
• List side effects and adverse effects of penicillins
and cephalosporins
• Describe interactions and precautions of
penicillins and cephalosporins
 Indications for Penicillins
They:
• Have greatest activity against gram-positive organisms,
gram-negative cocci, and non-lactamase-producing
anaerobes.
• However, they have little activity against gram-negative
rods.
• They are active against staphylococci, streptococci and
enterococcus faecalis but not against anaerobic bacteria,
enterococcus faecium and gram-negative cocci and rods.
• Extended-spectrum penicillins (ampicillin and the
antipseudomonal penicillins) retain the antibacterial
spectrum of penicillin and have improved activity
against gram-negative organisms
 Penicillins
Commonly used Penicillins include:
• Amoxicillin
• Flucloxacillin
• Benzyl penicillin
• Procaine penicillin
• Ampicillin
Dose, Dosage and Course of Penicillins

Orally:
• Amoxicillin 250-500mg every 8hourly for
5-7 days
• Ampicillin 250-500mg every 6hourly for 5-
7 days
Intramuscular(I.M):
• Penicillin G up to 2.4mU/dose I.M
 Adverse effects and side effects:
• The penicillins are remarkably nontoxic
• Most of the serious adverse effects are due to
hypersensitivity.
• All penicillins are cross-sensitizing and cross-reacting
• Allergic reactions include anaphylactic shock (serum
sickness-type reactions, urticaria, fever, joint swelling,
angioneurotic edema, intense pruritus, and respiratory
embarrassment variety of skin rashes
• Oral lesions, fever, interstitial nephritis vasculitis may
also occur.
• Most patients allergic to penicillins can be treated with
alternative drugs.
 Contraindications, Interactions and
Precautions of Penicillins.
Contraindication:
• In patients with renal failure
• In patients with penicillin hypersensitivity
Interactions:
• Reduce excretion of cytotoxic like methotrexate
• Allopurinol increases risk of rash when used with
amoxicillin or ampicillin
• Effects of anticoagulants are altered by penicillin
Precautions:
• History of allergy
• Most patients allergic to penicillins can be treated with
alternative drugs.
 Indications for Cephalosporins
They are:
• Similar to penicillins
• But more stable to many bacterial lactamases .
• Therefore have a broader spectrum of activity.
• However, strains of E coli and Klebsiella species
expressing extended-spectrum lactamases that can
hydrolyze most cephalosporins are becoming a
problem.
• Cephalosporins are not active against enterococci
and L monocytogenes.
 Commonly used Cephalosporins
include:
• Cefuroxime
• Cefotaxime
• Ceftriaxone
• Cefalexin
• Cefradoxil
• Cefixime
• Cefadroxil
 Dose, Dosage and Course of
Cephalosporins:
Orally
• Cephalexin is given orally in dosage of 0.25-
0.5 g every 6 hours (15-30 mg/kg/d)
• Cefadroxil in dosages of 0.5-1 g twice daily.
Parenterally
• The usual intravenous dosage for adults is
0.5-2 g intravenously every 8 hours.
• Can also be administered intramuscularly
 Adverse effects and side effects:
• Cephalosporins are sensitizing and may elicit a
variety of hypersensitivity reactions that are
identical to those of penicillins
• These include anaphylaxis, fever, skin rashes,
nephritis, granulocytopenia, and hemolytic anemia
• Local irritation can produce severe pain after
intramuscular injection and thrombophlebitis after
intravenous injection
• Renal toxicity, including interstitial nephritis and
even tubular necrosis.
 Contraindications, Interactions and
Precautions of Cephalosporins:
Contraindication:
• In patients with cephalosporin hypersensitivity
• In patients with a history of anaphylaxis to penicillins
Interactions:
• Drugs with the methylthiotetrazole ring can also cause
severe disulfiram-like reactions.
• Consequently, alcohol and alcohol-containing medications
must be avoided
Precautions:
• History of allergy
• Most patients allergic to cephalosporins can be treated with
alternative drugs.
 Key Points
• Penicillins have greatest activity against;
– gram-positive organisms
– gram-negative cocci
– non- beta-lactamase-producing anaerobes
• Cephalosporins are similar to penicillins
– But more stable to many bacterial
lactamases
– Therefore have a broader spectrum of
activity
 Key Points .....
• Penicillins and Cephalosporins are
contraindicated in patients with
hypersensitivity reactions
• Penicillins and Cephalosporins can be given
orally or by injection
• Common side effects of Penicillins and
Cephalosporins fever, skin rashes, nephritis
 Self Evaluation
• What are the indications of Penicillins and
Cephalosporin Drugs?
• What are the Contraindication of Penicillins
and Cephalosporin Drugs?
• What are the dose, dosage and course of
Penicillins and Cephalosporin Drugs?
• What are side effects and adverse effects of
Penicillins and Cephalosporin Drugs?