Antibacterial Drugs Flashcards by Nkanyiso Zulu

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

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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.

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Cell wall synthesis inhibitors

Describe penicillin cautions

ELderly
Neonates

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Cell wall synthesis inhibitors

Describe the spectrum and indications of Ampicillin

Broad Spectrum

Gram positive bacteria and Influenza

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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)

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Cell wall synthesis inhibitors

Describe the spectrum of Piperacinllin and Tazobactam

Extended Spectrum

and Gram negative show high resistance.

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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.

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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.

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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

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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.

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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.

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Cell wall synthesis inhibitors

Teicoplanin
MOA, A/E/ Route of Admin

Teicoplanin is Vancomycin Twin

Route of Admin= IM

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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.

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Bacterial Metabolism Inhibitors

Describe the MOA of Antimetabolites

Inhibit DNA synthesis by blocking *Folate Pathway

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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

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Describe the Moa of Trimethoprim and Sulfamethoxazole

Trimethoprim
moa= Inhibits the bacteria dihydroFOLATE reductase enzyme

Sulfamethoxazole
moa= Inhibits the dihydroPTEROATE Synthetase

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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

1. Vestibular Toxicity 2. Blue-Grey pigmentation of the skin 3. 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

1. Pseudomembrane Colitis 2. reduce efficacy of Oral Contraceptives 3. **Diarrohoea** 4. **Nausea** 5. **Skin Lesions** 6. Transient Leukopenia 7. Transient Thrombocytopenia 8. Transient Agrunolocytosis

Inhibitors of protein synthesis describe the cautions made in Clindamycin

1. Porphyria 2. GIT disease 3. ELderly 4. Pregnancy 5. 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

# ``` ``` 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**