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Antibiotics
- 1. Zephyr’s Strength Prepared by: Dr. Naila Ansari
- 2. Antibiotics Antibiotics are drugs used to treat infections caused by bacteria. What bacteria is? Bacteria are tiny organisms that can cause illness to humans and animals
- 3. Types of Antibiotics • The commonly used antibiotic types are: • Beta-Lactams: 1.Penicillins 2.Cephalosporins • Aminoglycosides • Macrolides • Fluoroquinolones • Tetracyclines
- 4. Uses of Cephalosporin • Cephalosporin's are used to treat 1. Pneumonia 2. Soar throat 3. Tonsillitis 4. Bronchitis 5. Otitis 6. Skin infections 7. Urinary tract infections
- 5. Generations 1st Generation • Cephalothin • Cefazolin • Cephapirin • Cephradine • Cephalaxin • Cefadroxil 2nd Generation • Cefaclor • Cefamandole • Ceforanide • Cefuroxime.
- 6. Generations 3rd Generation • Cefixime • Cefotaxime • Ceftriaxone 4th Genertaion • Cefclidine • Cefepime • Cefluprenam • Cefozopran • Cefquinome
- 7. WIZY (Cefixime) • 3rd Generation Cephalosporin • Effective against rapidly growing organism that synthesizes peptidoglycan
- 8. Mode Of Action • They destroy the cell wall of bacteria. Cefixime has high affinity for Penicillin binding protein.
- 9. Indications • RTI • Typhoid • UTI • Otitis Media • Gonorrhea • Typhoid fever • Post surgical infection • Bone & Joint Infection
- 10. Dosage • Typhoid Fever • Infectious Diarrhea • UTI Indication Dosage Uncomplicated Gonoccoal Infection 400 mg O.D 7 days Bronchitis 400 mg O.D Urinary Tract Infection 400 mg OD Otitis Media 400 mg OD
- 11. Pharmacokinetics Absorption • Bioavailability 40-50% • Hepatic Distribution • Protein binding 50-60% • Half life 3-4hr • 50% excreted in urine Metabolism Elimination
- 12. Adverse Effects Common • Diarrhea • Abdominal Pain • Dizziness • Flatulence • Fever • Vomiting Rare but serious • Prolonged Prothrombin time • Leukopenia • Increased Creatinine
- 13. Contraindications & Interaction Contraindications • Hypersensitivity to cephalosporin antibiotics • Penicillin sensitive patients Interactions • Carbamezapine • Warfarin
- 14. Macrolides • Macrolides just like the other types of antibiotics it interfere with the protein formation of bacteria by binding with bacterial ribosomes. • Macrolides includes: • Azithromycin • Clarithromycin • Erythromycin.
- 15. CLARACIN (Clarithromycin) • Clarithromycin, a semisynthetic macrolide antibiotic derived from erythromycin • Clarithromycin may be bacteriostatic or bactericidal depending on the organism and drug concentration.
- 16. Mode Of Action • Inhibits bacterial protein synthesis by binding to the bacterial 50S ribosomal subunit. • Binding inhibits peptidyl transferase activity and interferes with amino acid translocation during the translation and protein assembly process
- 17. Indications • Acute Exacerbation of Chronic bronchitis • Acute Maxillary sinusitis • Mycobacterial Infection • Peptic Ulcer • Pharyngititis • CAP • Endocarditis • Crohn Disease
- 18. Dosage Disease • Typhoid Fever • Infectious Diarrhea • UTI • Intra-abdominal Infection • Pneumonia DoseIndication Dosage Duration AECB 250-500mg BD 7-14 days Acute Maxillary Sinusitis 500 mg BD 14 days Mycobacterial Infection 500 mg BD 7 – 14 days Peptic Ulcer (With PPI) 500 mg BD 10 – 14 days CAP 250 mg BD 7 – 14 days Pharyngititis 250 mg BD 10 days
- 19. Pharmacokinetics Absorption • Bioavailability 50% • Partially metabolized • Metabolite 14-OH clarithromycin active Distribution • 42-50% protein binding • Renal • Half life- 3-7hr Metabolism Elimination
- 20. Adverse Effects Common • Diarrhea (3-6%) • Nausea (adults, 3-6%) • Vomiting (adults, 1%; children, 6%) • Elevated blood urea nitrogen (BUN; 4%) • Abdominal pain (adults, 2%; children, 3%) • Rash (children, 3%) • Dyspepsia (2%) • Heartburn (adults, 2%) • Headache Rare But Serious • Jaundice • Leukopenia • Manic behavior • Neuromuscular blockade • Neutropenia • QT Prolongation • Seizures
- 21. Warnings & Interaction Warnings • Severe renal impairment • Exacerbation of Mysthaneia Gravis • Ventricular Cardiac Arrhythmia Interaction • Quinidine • Cisapride
- 22. Flouroquinolone This is the latest class of antibiotics comprises 1. Ciprofloxacin 2. Enoxacin 3. levofloxacin, 4. Norfloxacin 5. Ofloxacin 6. Gatifloxacin 7. Moxifloxacin These antibiotics are mostly used to treat urinary tract infections.
- 23. Mode of Action • Quinolones inhibit bacterial growth by blocking DNA replication.DNA is the genetic material of the cells, and is responsible for proper functioning of the cell.
- 24. ANACIN ( Ciprofloxacin) • Bacterial DNA Gyrase Inhibitor • Activity gram-negative and gram-positive bacteria. •Its excellent bioavailability permits its use for treatment of variety of serious bacterial infections.
- 25. MOA • Inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV No bacterial DNA replication, transcription, repair and recombination No bacterial cell division
- 26. Indications • UTI • Infectious Diarrhea • Typhoid • Acute Sinusitis • Pneumonia • Intra-abdominal infection • Bone & Joint Infection • Soft Tissue & Skin Infection
- 27. Dosage Disease • Typhoid Fever • Infectious Diarrhea • UTI • Intra-abdominal Infection • Pneumonia Dose Indication Dosage Duration Typhoid Fever 500 mg BD 10 days Infectious Diarrhea 500 mg BD 5 – 7 days Urinary Tract Infection 500 mg BD 7 – 14 days Acute Intra-Abdominal Infection 500 mg BD 7 – 14 days Pneumonia 500 mg BD 7 – 14 days Acute Sinusitis 500 mg BD 10 days Bone & Joint Infection 500 mg BD 7 – 14 days Skin & Soft Tissue Infection 500 mg BD 7 – 14 days
- 28. Pharmacokinetics Absorption • Bioavailability 70% • Hepatic Distribution • 20-40% protein binding • Renal • Half life-4hr Metabolism Elimination
- 29. Adverse Effect Common • Nausea (2.5%) • Vomiting (1%) • Diarrhea (1.6%) • Abnormal LFT (1.3%) • Rash (1%) Rare • Peripheral neuropathy • Acute liver failure • Hepatitis • QT Prolongation • Torsades de pointes • Phototoxicity • Toxic epidermal necrolysis (TEN) • Stevens–Johnson syndrome
- 30. Warnings & Interaction Warnings • Increased risk of Tendinitis & Tendon Rupture in: – Patients over 60 years of age – Rheumatoid Arthritis – Taking corticosteroids – Kidney, Heart or Lung transplants • Muscle weakness in persons with myasthenia gravis Interaction Antacids • Reduces bioavailability by 90% Metronidazole • No change in Cip-Care’s serum concentration • Can be given concomitantly Theophylline • Cip-Care decreases theophylline’s serum clearance – Chances of CNS adverse reactions increases
- 31. CROCUS (Levofloxacin) • It is a synthetic broad spectrum antibacterial agent for oral and intravenous administration
- 32. Mode of Action • Levofloxacin inhibits bacterial type II topoisomerases, topoisomerase IV and DNA gyrase. • This results in strand breakage on a bacterial chromosome, super coiling, and resealing; DNA replication and transcription is inhibited
- 33. Indications • Sinusitis • Conjuctivitis • Bronchitis • Community acquired Pneumonia • Complicated UTI • Pyelonephritis
- 34. Dosage Disease • Typhoid Fever • Infectious Diarrhea • UTI • Intra-abdominal Infection • Pneumonia DoseIndication Dosage Duration CAPneumonia 500 mg OD 7-14 days Nosocomial Pneumonia 750 mg OD 7-14 Days Acute bacterial Sinusitis 500 mg OD 10-14days Acute bacterial exacerbation of chronic bronchitis 500 mg OD >7 days Uncomplicated UTI 250mg OD 3days Complicated UTI 250mg OD 10 days
- 35. Pharmacokinetics Absorption • Bioavailabity 62 % • Limited hepatic metabolism • 87% remain unchanged Distribution • 24-38 % protein binding • Half life 6-8hr • Renal excretion Metabolism Elimination
- 36. Adverse effects Common • Disorientation • Dizziness • Drowsiness • hot and cold flashes • Nausea • slurring of speech • swelling and numbness in the face Rare but serious • Cardiac Arrest • Tremor • Anxiety • Abnormal Hepatic function
- 37. M-FLOX (Moxifloxacin) • Bacterial DNA Gyrase and Topo-isomerase IV Inhibitor •Activity gram-negative and gram-positive bacteria. •Its excellent bioavailability permits its use for treatment of variety of serious bacterial infections.
- 38. Mode of Action • Inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV No bacterial DNA replication, transcription, repair and recombination No bacterial cell division
- 39. Indications • Community Acquired Pneumonia • Acute Exacerbation of Chronic Bronchitis Indication Dosage Duration CAP OD 7 days AECB OD 5 days
- 40. Pharmacokinetics Absorption • Bioavailability 71% • Hepatic • 10% of metabolite formation Distribution • Serum Protein Binding 60- 70% • Half life 7±2 hr • Excretion Renal (36%) and Fecal (61%) Metabolism Elimination
- 41. Adverse Effects Common • Nausea (0.3%) • Vomiting (0.2%) • Diarrhea (0.3%) • Urticaria (0.2%) • Rash (0.8%) Rare But Serious • Hemorrhage • Increased (INR) • Retinal Hemorrhage • Peripheral Edema • Renal Failure •QT Prolongation •Supraventricular Tachycardia •Syncope •Transient Ischemic Attack •Antibiotic-associated colitis •Tendon rupture
- 42. Warnings & Interaction Warnings • Increased risk of Tendinitis & Tendon Rupture in: – Patients over 60 years of age – Rheumatoid Arthritis – Taking corticosteroids – Kidney, Heart or Lung transplants • Muscle weakness in persons with myasthenia gravis • QT Prolongation Interaction Probenecid • Increases systemic exposure of Gemo up to 45% Antacids • Decreases absorption of Gemo Warfarin • Increase in the INR, or PT, and/or clinical episodes of bleeding
- 43. Antibiotics In Pregnancy • Category A – Controlled studies in women fail to demonstrate a risk to the fetus in the first trimester (and there is no evidence of a risk in later trimesters), and the possibility of fetal harm appears remote. • Category B – Either animal-reproduction studies have not demonstrated a fetal risk but there are no controlled studies in pregnant women, or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the first trimester (and there is no evidence of a risk in later trimesters). • Category C – Either studies in animals have revealed adverse effects on the fetus (teratogenic or embryocidal or other) and there are no controlled studies in women, or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the fetus. •
- 44. Antibiotics In Pregnancy • Category D – There is positive evidence of human fetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective). • Category X – Studies in animals or human beings have demonstrated fetal abnormalities, or there is evidence of fetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated
- 45. Antibiotic Classification In Pregnancy Category A • Quinolones, • Clarithromycin • Ribavarin Category B • Penicillins • Cephalosporins • Tetracyclines (Doxy, Tige, Mino) • Voriconazole • Aminoglycoside Category C Category D Category X