4. macrolide antibiotics.pptx

INTRODUCTION
Erythromycin is the first member of group, and was isolated from a strain of Streptomyces erythreus in 1952.

Rest drugs are semi-synthetic derivatives of erythromycin known as newer macrolides

Some other drugs are dirithromycin, oleandomycin and troleandomycin.
MECHANISM OF ACTION
Macrolide antibiotics are bacteriostatic agents and inhibit the protein synthesis by binding reversibly to 50s ribosomal subunit of sensitive microorganism and interfere with translocation step in the protein synthesis.

Gram positive bacteria's are 100 times more sensitive than gram negative bacteria's by these drugs.

MECHANISM OF ACTION
It is bacteriostatic at low concentration & bactericidal at high concentration

Bactericidal property depends on the concentration, organism concerned and its rate of multiplication
ANTI MICROBIAL SPECTRUM
It is narrow spectrum antibiotic. These antibiotics are more active against gram positive cocci and inactive against most of the aerobic and enteric gram negative bacilli.

In addition, Campylobacter, Legionella, Branhamella catarrhalis, G. vaginalis and Mycoplasma (which are not affected by pencillin are also highly susceptible to erythromycin)

ANTI MICROBIAL SPECTRUM
Moderately sensitive to H. influenza, B. pertussis, C. trachomatis, N. meningitidis and Rickettsiae

Ineffective against Enterobacteriaceae, other gram negative bacilli.

ERYTHROMYCIN
This drug is acid labile, given as enteric coated tablets. Poorly absorbed when given empty stomach and has poor tissue penetration.

DOSE: 250-500mg QID with half life of 1.5 hrs
Indications: a drug of choice in atypical pneumonia, whooping cough and cancroids and as an alternative to penicillin in streptococcal pharyngitis, tonsillitis, mastoiditis.

SIDE EFFECTS: Epigastric distress causing nausea, vomiting and diarrhea. Allergic reactions such as fever and skin eruption.
CLARITHROMYCIN
These drugs are acid stable, good absorption occurs when given empty stomach and has good tissue penetration.

Dose: 250-500mg BD with half life of 3-6 hrs at low dose and 3-9 hrs at high dose.

Indications: upper and lower RTI, sinusitis, otitis media, atypical pneumonia, skin infections. And H. pylori infection and first line drug in combination regimens in AIDS infection

Side effects: same as erythromycin but better gastric tolerance, reversible hearing loss at high doses.
AZYTHROMYCIN

These drugs are acid stable, good absorption occurs when given empty stomach and has good tissue penetration
Dose: 500mg OD with half life >50 hrs.
Indications: pharyngitis, tonsillitis, sinusitis, otitis media pneumonias, chronic bronchitis. In the prophylaxis and treatment of AIDS infections.
Side effects: nausea vomiting, diarrhea and abdominal pain.

ROXITHROMYCIN
These drugs are acid stable, good absorption occurs when given empty stomach and has good tissue penetration
DOSE: 150mg BD with half life of 12 hrs.
Indications: alternative to erythromycin for respiratory, skin

1. MACROLIDE ANTIBIOTICS NEHA BHARTI M.Sc. N(MEDICAL SURGICAL NURSING) NURSING TUTOR, SMVDCoN

2. INTRODUCTION These drugs contain a many membered lactone ring known as macrocyclic ring to which one or more deoxy -sugars are attached. Erythromycin, clarithromycin, roxythromycin and azithromycin are macrolide antibiotics.

3. INTRODUCTION Erythromycin is the first member of group, and was isolated from a strain of Streptomyces erythreus in 1952 . Rest drugs are semi-synthetic derivatives of erythromycin known as newer macrolides Some other drugs are dirithromycin , oleandomycin and troleandomycin .

4. MECHANISM OF ACTION Macrolide antibiotics are bacteriostatic agents and inhibit the protein synthesis by binding reversibly to 50s ribosomal subunit of sensitive microorganism and interfere with translocation step in the protein synthesis. Gram positive bacteria's are 100 times more sensitive than gram negative bacteria's by these drugs.

5. MECHANISM OF ACTION It is bacteriostatic at low concentration & bactericidal at high concentration Bactericidal property depends on the concentration, organism concerned and its rate of multiplication

6. ANTI MICROBIAL SPECTRUM It is narrow spectrum antibiotic. These antibiotics are more active against gram positive cocci and inactive against most of the aerobic and enteric gram negative bacilli. In addition, Campylobacter, Legionella, Branhamella catarrhalis , G. vaginalis and Mycoplasma (which are not affected by pencillin are also highly susceptible to erythromycin )

7. ANTI MICROBIAL SPECTRUM Moderately sensitive to H. influenza, B. pertussis, C. trachomatis, N. meningitidis and Rickettsiae Ineffective against Enterobacteriaceae , other gram negative bacilli.

8. ERYTHROMYCIN This drug is acid labile, given as enteric coated tablets. Poorly absorbed when given empty stomach and has poor tissue penetration. DOSE: 250-500mg QID with half life of 1.5 hrs Indications: a drug of choice in atypical pneumonia, whooping cough and cancroids and as an alternative to penicillin in streptococcal pharyngitis, tonsillitis, mastoiditis . SIDE EFFECTS: Epigastric distress causing nausea, vomiting and diarrhea. Allergic reactions such as fever and skin eruption.

9. CLARITHROMYCIN These drugs are acid stable, good absorption occurs when given empty stomach and has good tissue penetration. Dose: 250-500mg BD with half life of 3-6 hrs at low dose and 3-9 hrs at high dose. Indications: upper and lower RTI, sinusitis, otitis media, atypical pneumonia, skin infections. And H. pylori infection and first line drug in combination regimens in AIDS infection Side effects: same as erythromycin but better gastric tolerance, reversible hearing loss at high doses.

10. AZYTHROMYCIN These drugs are acid stable, good absorption occurs when given empty stomach and has good tissue penetration Dose: 500mg OD with half life >50 hrs. Indications: pharyngitis, tonsillitis, sinusitis, otitis media pneumonias, chronic bronchitis. In the prophylaxis and treatment of AIDS infections. Side effects : nausea vomiting, diarrhea and abdominal pain.

11. ROXITHROMYCIN These drugs are acid stable, good absorption occurs when given empty stomach and has good tissue penetration DOSE: 150mg BD with half life of 12 hrs. Indications: alternative to erythromycin for respiratory, skin and soft tissue and genital tract infections. Side effects: nausea, vomitting , diarrhea and abdominal pain.

12. TELITHROMYCIN It is a semi-synthetic derivatives of erythromycin and also called as ketolide , due to a keto group in its structure. Due to this changed structure, it is more active against the macrolide resistant gram positive micro-organisms.

13. It given orally as once daily dosage schedule in a dose of 400mg OD. Half life is 10 hrs. Used for the treatment of RTIs , sinusitis. Major side effects are reversible hepatic dysfunction.

14. DRUG INTERACTIONS Erythromycin inhibits hepatic metabolism of many drugs.

15. NURSING IMPLICATIONS Azythromycin and clarythromycin should be given in empty stomach due to its acid stability and better absorption. These agents should be avoided during pregnancy The hepatic functions should be regularly monitored. Patients should be regularly enquired about any side effects.

16. BROAD SPECTRUM ANTIBIOTICS

17. INTRODUCTION Tetracycline & Chloramphenicol are broad spectrum antibiotics. They are called so because of there effectiveness against a wide range of microorganism such as Gram positive & Gram negative bacteria Eg . Rikettsia , M pneumonia, Chlamydia, anaerobes, sirochetes , H. pylori and some protozoa ( eg . Malerial parasites & Entamoeba )

18. 1. Tetracycline Introduction: Broad-Spectrum Bacteriostatic Antibiotics Active against many gram-positive and gram-negative bacteria, including Anaerobes, Rickettsiae , Chlamydiae , Mycoplasmas, Protozoa, e.g. amoebas Mechanism of Action: It inhibit bacterial protein synthesis by binding to and interfering with ribosomes.

19. Indication & Uses Chlamydial infections, including sexually transmitted diseases, In combination with an aminoglycoside, I ndicated for plague, tularemia , and brucellosis, Treatment of acne, bronchitis , Community-acquired pneumonia

20. Classification of Tetracycline

21. Contraindication & Precautions: Hypersensitivity to tetracycline drugs. Take precaution in Renal disease, Hepatic disease. Drug interactions: Milk and dairy products, Magnesium containing laxatives, antacids, calcium supplements, iron supplements reduce absorption of tetracycline's. Tetracycline's decrease the effect of penicillins & Hormonal contraceptives drugs.

22. Nursing Responsibilities They should not be used during pregnancy, lactation and childhood. They should not be given when renal functions are impaired. Instruct the patient not to take antacids calcium supplements, iron supplements & Magnesium containing laxatives. Do not take Milk or dairy products within 2- 3hrs of taking tetracycline's.

23. 2. Chloramphenicol Introduction: Broad spectrum (aerobic, anaerobic, gram +, gram -, Rickettsiae ) they closely resembles in the action to the tetracycline’s Bacteriostatic (H. influenzae , Neisseria meningitidis ) Mechanism of Action: They inhibit protein synthesis in susceptible bacteria, in presence of these drug, organism cannot multiply thus it acts as bacteriostatic drug.

24. Indication & Uses Mainly used in typhoid fever. UTI , Rickettsial , Cholera, Bacterial meningitis, Eye, Ear infections . Drug Examples & Doses: Adult & Child: O/IV 50 to 100mg/kg/day in divided doses of Q6h not exceed to 100mg/kg/day.

25. Contraindication & Precautions: History of hypersensitivity or toxic reactions, Pregnancy & Lactation, spl . precaution for renal impaired and hepatic patients.

26. Drug interactions Chemical inhibits metabolism of tobutamide chorpropamide , warfarin, cyclophosphamide, and phenytoin.

27. NURSING RESPONSIBILITIES Assess signs of infection, Anemia, before therapy. Administer I/V after diluting 1gm/10ml, provide oral dose with adequate water .