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Antiparasitics
Antiprotozoals
Antimicrobials Antibacterials
Chemotherapy
Antifungals
Antineoplastics Antivirals
Chemotherapy Compiled by Birhanu G. 5
Use of Anti-infective Agents
✍ Prophylactic therapy
✍ Empiric therapy
test
☞ Can be:
Bactericidal:
Aminocyclitoles, sulphonamides
Can be innate/acquired
Transduction: phages
☞ Predisposing factors
Compromised → cidal
Site of infection
Antimicrobial allergies
Spectrum of activity
Appropriate dose
Cost
Indication
Mixed infection
Prevention of resistance
Decreased toxicity
Increased cost
-lactams
Cephalosporins
Carbapenems
Glycopeptides: Vancomycin
Chemotherapy Compiled by Birhanu G. 19
BETA-LACTAM ANTIBIOTICS
consists of 3 components:
contains:
MOA:
pentapeptides
microorganisms
Active against:
Anthrax by B. anthracis
Prophylactic applications;
Bacterial endocarditis
fever; GABHS
They have bulky side chains that protect the -lactam ring
Nafcillin
AMINOPENICILLINS
Chlamydial
Chemotherapy infection inCompiled
pregnant:
by Birhanu G. off-label 36
Amoxicillin
Carbenicillin
Use:
Transduction: phages
bacteria
Aminoglycosides: synergism
Type-III:
membranous colitis)
carbencillin
Neutropenia
Pharmacodynamics:
Bactericidal
Cefixime, Ceftizoxime.
Broad spectrum
Active against:
P. aeruginosa,
Acinetobacter baumannii.
Allergic reactions
Probenecid
– -lactamase resistant
Imipenem (IV)
CNS: Seizure
Hypersensitivity reaction
Therapeutic use
MOA:
transporter systems
epithelial cells
H.influenzae
Chemotherapy Compiled by Birhanu G. 70
Has oral & parenteral forms
Dose:
D-4-amino-3-isoxazolidone
alanine-D-alanine
inhibiting;
together
Chemotherapy Compiled by Birhanu G. 73
Spectrum: both G-ve & G+ve
BPP transports NAM & NAG across the cell membrane during
the synthesis of peptidoglycan, by flipping the repeating
monomer units from the cytoplasm to the periplasm
Adverse Effects:
orientalis
MOA:
colitis
Bactericidal: Aminoglycosides
Bacteriostatic:
Aminocyclitols
proteins, like;
Initiation
Termination
General properties:
formation;
Breakup
Chemotherapy of polysomes Compiled
into bynon
Birhanufunctional
G. monosomes 88
Effects of aminoglycosides on protein synthesis
Pharmacokinetics
Ototoxicity
Skin rash
Side effects:
Glycylcyclines (Tigecycline):
Super infection
Hypoplasia of enamel
fair-skinned persons
MOA:
Pharmacokinetics
Longer t1/2
Are expensive
GI effects: ANVD
Drug Interaction
Usually bacteriostatic
Therapeutic use:
Adverse effects:
Nausea,
Diarrhea &
Skin rashes
cytoplasmic)
oxidative
Chemotherapy
stress (mitochondrial toxicity)
Compiled by Birhanu G. 122
MOA:…
marrow suppression
aplastic anemia
Indications:
GI disturbance: NVD
Superinfection
Chemotherapy Compiled by Birhanu G. 127
Drug Interactions:
oxidases
drugs)
Drug interaction
Bacteria;
Trachoma: Sulfacetamide
Sulphadiazine/Sulfadoxine + Pyrimethamine OR
toxoplasmosis
Hematologic effect
crosses the BBB; avoid in 3rd trimester & < 2 months age
Trimethoprim or pyrimethamine:
Other infections;
Adverse effects
Dermatologic
MOA:
Block DNA replication by inhibit the ligase domains of;
Distribution: Vd is high
Elimination
GIT infection:
Peritonitis
RTIs:
woman
MISCELLANEOUS: Metronidazole
Location in host;
Pyrazinamide: 25 mg/kg/d
Bedaquiline
Capreomycin
Clofazimine
Cycloserine
Macrolides
Dapsone
Therapeutic Uses
Direct toxicities:
Peripheral neuropathy:
inhibitor of CYP2D6
H induces CYP2E1
RIFAMPICIN/RIFAMPIN: R
Pharmacokinetics
Mycobacterial infection:
In TB prevention as an alternative to H
Leprosy
Atypical mycobacteria
disease (meningitis)
Chemotherapy Compiled by Birhanu G. 171
Therapeutic uses…
Osteomyelitis
Hepatitis
Hypersensitivity reactions
Thrombocytopenia
Interstitial nephritis
GI upset
MOA:
bacteriostatic
Chemotherapy Compiled by Birhanu G. 174
Therapeutic use: TB
Adverse effects
GI intolerance
Largely bacteriostatic,
Proposed MCZs:
bacteria
M. tuberculosis
Adverse effects
GI intolerance,
Hyperuricemia
Ethambutol 400mg,
Isoniazid 300mg,
Consists of 2 or 3 drugs
Duration is 4 – 6 months
Alternatives:
Recommendation: 2HRZE(S)/1HRZE/5HRE
TB and Leprosy
Give 2RHZ/4RH
anti-TB drug
ketomycolate
Chemotherapy Compiled by Birhanu G. 192
2nd, in NRPB, it generates reactive nitrogen species such
system
synthase
A congener of thioisonicotinamide
then to 2-ethyl-4-aminopyridine
antibiotic
capreolus
times a week
regimen
1. Lepromatous Leprosy
Marked ulceration
Mild infection
Enterohepatic recycling
Adverse effects
Rashes, GI disturbance
Membrane disruption
Adverse effects
GI intolerance (occasionally)
Immuno-pharmacology