Antibacterial Drugs Flashcards
Cell wall synthesis inhibitors
Beta lactams
Describe MOA, Side effects of Penicillin
MOA= Bactericidal (because it’s a beta lactam)
Side effects
1. Haematological effects
2. Infectious Mononucleosis
3. Hypersensitivity
4. Bleeding
5. Neurotoxic Effects
Cell wall synthesis inhibitors
Describe the spectrum and of Penicillin G and V
has a NARROW SPECTRUM
Penicillin G
“Goat Step M”
1. Gonorrhea
2. Oropharangeal Infections
3. Abscess
4. Tetanus/Gangrene
5. Syphillis
6. Tonsilitis
7. Enterococci
8. Prophylaxis…of what????
9. Meningitis
Penicillin V
1. USed for less serious infections
2. 2 to 4 times less effective than penicillin G.
Cell wall synthesis inhibitors
Describe penicillin cautions
- ELderly
- Neonates
Cell wall synthesis inhibitors
Describe the spectrum and indications of Ampicillin
Broad Spectrum
Gram positive bacteria and Influenza
Cell wall synthesis inhibitors
Describe the Spectrum, and Indications of Amoxillin
Indications.
1. Listeria and Enterococci
2. Gram negative bacteria (eg, UTIs)
3. Cholecystitis (Gall Bladder Inflammation)
Cell wall synthesis inhibitors
Describe the spectrum of Piperacinllin and Tazobactam
Extended Spectrum
and Gram negative show high resistance.
Describe Spectrum of cephalosporins
note: Enterococci are resistant
Broad spectrum
4 generations
1st gen is most effective against gram positive bacteria and 4th generation is most effective against gram negative bacteria.
Cell wall synthesis inhibitors
Describe A/E and C/I of Cephalosporins
Side Effects
1. Hypersensitivity rections
2. Alcohol Intolerance
3. phlebitis
4. Neurotoxicity
C/I
1. Allergy and Anaphylactic Shock.
Cephalosporins and Aminoglycosides would inactivate each other.
Cell wall synthesis inhibitors
Carbapenems
spectrum
A/E
C/I
Broad Spectrum
Imipenem-used in severe nosocomial Infections
given IV
A/E
1. PAin and Erythema
2. Red urine discolouration is Kids
3. Thrombophlebitis
C/I
1. Allergy
2. CNS disorders
3. Renal Impairment
Cell wall synthesis inhibitors
MONOBACTAMS
Spectrum
Admin
A/E
Narrow Spectrum- good activity against gram negative bacteria.
Admin
IM or IV
A/E
1. INjection Site reactions
2. Rash
3. GIT
4. Gastro-induced Eosinophilia.
Vancomycin
Spectrum
MOA
Admin Route
A/E and Cautions
Narrow Spectrum- Good activity against Gram Positive Bacteria
Prophylaxis for Endocarditis
MOA= Inhibits Transglycosylation.
Only administered IV infusion
A/E
1. Fever and Skin rashes
2. Histamine Release
3. Ototoxic and Nephrotoxic
Cautions
1. Renal Impairment
2. Elderly
3. Neonates
4. Pregnancy
5. Hearing Abnormalities.
Cell wall synthesis inhibitors
Teicoplanin
MOA, A/E/ Route of Admin
Teicoplanin is Vancomycin Twin
Route of Admin= IM
Fosfocymic
Spectrum
Indications
Side Effects
Cautions
Broad Spectrum
Uses- Single dose therapy for sensitive E.coli
Side Effects= GIT disturbances and Skin rashes (this goes together)
Caution
1. Renal Failure
2. Pregnancy and Lactation.
Bacterial Metabolism Inhibitors
Describe the MOA of Antimetabolites
Inhibit DNA synthesis by blocking *Folate Pathway
Antimetabolite
Describe Spectrum, Formulation, Indications, of Cotrixomizole
Spectrum= BROAD
Formalation:
1:5 of Trimethoprim:Sulphamethoxazole
Indications
1.Use in HIV patients in prophylaxis for PJP
2.Treatment of Nocardiosis
3.Prophylaxis of Toxoplasmosis and Isospora Belli Diarrhoea
Describe the Moa of Trimethoprim and Sulfamethoxazole
Trimethoprim
moa= Inhibits the bacteria dihydroFOLATE reductase enzyme
Sulfamethoxazole
moa= Inhibits the dihydroPTEROATE Synthetase
Cotrimoxazole
Side effects of Trimethoprim
- Skin Rashes
- Bone marrow depression
- Folate shortage
- reduced efficacy of combined contraceptive pill
- Teratogenic (developmental Malformations)
Cotrimoxazole
Describe the A/E of Sulfamethoxazole
- Kernicterus
- Precipitations in urine
- Allergy…eg Steve Johnson’s Syndrome
- Reduces the efficscy of contraceptive pill
Describe the D/I of Cotrimoxazole
D/I- Inhbit Pheenytoin Metabolism
C/I
1. Pregancy
2. Porphyria
3. G6PD deficiency - Bleeding
4. Allergy
Inhibitors of protein synthsis
Describe the mech. of action, causes of resistance, Pharmacokinetics of Tobramycin, Gentamycin, Amikamycin, Kanamycvin, Framycetin, Neomycin, Netilmycin
These are AMINOGLYCOSIDES
Mech.Of Action=30S: prevent Initiation complex
Causes of Resistance
1. Mutation of bidning site on 30S
2. Inactivation of enzymes
3. Inhibition of transport into cell.
Pharmacokinetics
1. Excreted Unaltered in Urine.
2. Once daily dosage.
3. not absorbed after ORAL ingestion.
Describe the cautions and Indications **Tobramycin, Gentamycin, Amikamycin, Kanamycvin, Framycetin, Neomycin, Netilmycin. **
Indications
1. Pseudomonas Auregenosa
2. Aerobic Gram Negative Infections
3. Used allong with penicillins against Staphylococci, Streptococci and Enterococci
4. Topically for Eye infections, Otitis media and Infection of the Nasal Vestibuli
Protein Inhibitors- MACROLIDES
Describe the Uses, MOA, D/I and for Erythromycin, Roxithromycin, Azithromycin and Clarithromycin(collectively)
MACROLIDES ARE BACTERIOSTATIC BUT BACTERICIDAL AT HIGH DOSES.
INDICATIONS
1. Respiratory infections
2. chlamydia infections
3. Community acquired Pneumonia
4. Legionella Pneumonia
5. Whooping cough (Bordetella Pertussis)
6. Mycoplasma Pneumonia
7. Corynebacterium Infections (treated with Erthromycin)
8. Prophylaxis agaisnt Infective Endocarditis during dental procedures
MOA
1. Attaches to 50S ribosomal unit
2. Binds close to sites for chloramphenicol and clindamycin…can lead to competitive binding if administered together.
3. Inhibits translocation.
D/I
Oral Contraceptive
Protein Inhbitors- MACROLIDES
Describe the A/E and Cautions of Erythromycin, Roxithromycin, Azithromycin and Clarithromycin(collectively)
A/E
1. GIT intolerance
2. Hepatotoxicity
Cautions
1. Heart Disease.
2. Liver Disease.
3. Impaired Biliary Infection.
4. Porphyria.
Protein Inhibitors-Macrolides
Describe the uses of Erythromycin
- Treats acne
- treats C. diphtheria
Macrolides-P/Is
Describe uses of combination of Clarithromycin and Omeprezole
Peptic Ulcers
P/I- Macrolides
Describe the use of combination of Azithromycin and Clarithromycin
Rickkettsial Infections
Protein Inhibitors
Describe the characteristics, indications and MOA of Chloramphenicol.
Characteristics- Bacteriostatic and Broad spectrum
Indications
1. Typhoid fever
2. Eye infections
3. Rickettsial infections
4. Meningitis
5. not used long term
Mech. of Action
Attaches reversibly to 50S ribosomal subunit. Interrferes with Peptidyltransferase.
protein Inhbitors
Describe the cause of resistance, Side effects and C/I of Chloramphenicol
Resistance- Production of acetyltransferase.
Side Effects
1. GIT effects
2. Hypersensitivity- Allergy
3. Irreversible Bone marrow Suppression
4. Inhbits Liver enzymes
5. Optic Neuritis
Contraindications
1. Allergy
2. Porphiria
3. 3rd trimester of Pregnancy
4. Neonates
5. Lactation.
**ORALLY INGESTED*
Describe the characteristics, Indications, MOA of Tetracycline, Doxycycline and Minocycline (Tetracyclines)
Characteristics- Bacteriostatic
MOA
1. Binds to 30S Bacterial Ribosomal Subunit.
2. Inhibits Codon-Anticodon interaction
Indiacations
1. Acne (has good skin penetration)
2. Chronic Bronchitis
Describe pharmacokinetics, A/E and cause of resistance of Tetracycline, Doxycycline and Minocycline (Tetracyclines)
Resistance
1. Enzymatic inactivation.
2. Decreased Intracellular Interaction.
3. Interaction with Drug Interaction.
Pharmacokinetics
1. Must be taken with adequate amount of fluid
2. Milk/Antacids prevent absoprtion
Side Effects
1. Hepatotoxic Effects
2. GIT Disruptions
3. Infection with Candida
4. Decreased bone growth in children
5. Infection with Clostridium Difficile.
6. Nephrotoxic
7. Reduced efficacxy of Combined Ora;l Contraceptive Pill.
8. Discolouration of Nails and Teeth(become darker)
describe side effects of Minocycline
- Vestibular Toxicity
- Blue-Grey pigmentation of the skin
- Pigmentation of acne scars
Tetracyclines- describe cautions
. Children less than 12 years.
2. Elderly
3. Porphiria
4. Pregnacy
5. Hepatic Impairement
Clindamycin
Indications
Mech. Of Action.
Cause of Resistance
Indications
1. Soft tissue infections
2. Gram Positive infections
3. Patients allergic to Penicillin
4. Lung Abscess
5. Not used against Enterococci.
Mech. Of Action
1. BInds 50S
2. Bacteriostatic but bactericidal at higher concs. (like Macrolides).
Cause of Resistance
Mutation of ribosomal sub-unit.
enzymatic inactivation.
Describe the side effects of Clindamycin
- Pseudomembrane Colitis
- reduce efficacy of Oral Contraceptives
- Diarrohoea
- Nausea
- Skin Lesions
- Transient Leukopenia
- Transient Thrombocytopenia
- Transient Agrunolocytosis
Inhibitors of protein synthesis
describe the cautions made in Clindamycin
- Porphyria
- GIT disease
- ELderly
- Pregnancy
- Hepatic Impairement
Describe the Indications and Side effects of Fusic Acid
Indications
1. Severe Staphylococci Infections
2. MOA similar to macrolides
Side Effects
1. Hepatotoxicity
2. GIT effects
3. Avoid In pregnancy
4. Kernicterus
describe the drug interactions and Contraindications of Fusic Acid
*Drug Interactions
1. Hydrocortisone
2. Statins~increasing risk of rhabdomyolysis
Contraindications
1. Hepatic Dysfunction.
Mupirocin
Indications
Pharmacokinetics
Side effects
Indications.
1. Gram Positive Bacteria
2. Effective agaisnt Methicillin-Resistant Staphylococcus Aereus
pk- only TOPICAL
Side Effects
1. Midl stigning and burning and itching at site of application.
Ketolides-includes Telithromycin
Discuss PK, Indications and Side effects of Ketolides(Inc. Telithromycin)
Broad spectrum
PK
dose=once daily for 5 days
Indications
1. Erythromycin-Resistant strains of Pneumococcus
*Side Effects
1. Inhibits Liver Enzymes
2. Visual Disturbances
3. Loss of Consciousness
4. Respiratory Failure
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Describe the Indications, MOA, Side effects of Oxazolidones(Linezolid)
Indications-bacteriostatic
1. Gram negative bacteria
2. M.Tuberculosis
3. Cloxacillin-Resistant staaphylococci and Vancomycin-resistant enterococci.
A/E
1. Haemolytic toxicity
2. headaxhe
3. fungal infection
4. GIT effects
Describe indications and A/E of Lipopeptides (Daptomycin)
Indications
1. Multi-resistant bacteria
2. active against Gram positive bacteria ONLY
Side Effects- Myopathy
*GIVEN IV
