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Protein Synthesis inhibitor PowerPoint Presentation

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Description : Protein Synthesis inhibitor

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Published on : Mar 21, 2018 | Views : 2019 | Downloads : 4

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Protein Synthesis Inhibitors 2/12/2020 1 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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2/12/2020 2 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Protein Synthesis Inhibitor Protein Synthesis Inhibitor are those antibiotics that binds with ribosomal subunit of bacteria and interfere with protein synthesis. Protein is required for the growth and development of the organism The group of antibiotics are divided into 2 group Bacteriostatic : Tetracycline, chloramphenicol, clindamycin Bactericidal : Aminoglycosides, Macrolides 2/12/2020 3 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Macrolides Azithromycin, Erythromycin, Clarithromycin, Roxythromycin. MOA:- Macrolides bind irreversibly to 50s subunit of the bacterial ribosome and inhibit the protein synthesis. So they stop the growth and development of bacteria. Thus they are primarily bacteriostatic but they can be bactericidal at higher dose. 2/12/2020 4 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Erythromycin It was isolated from Streptomyces erythreus in 1952 . Since then it has been widely used, mainly as alternative to penicillin. It is bacteriostatic at low conc. & bactericidal at high conc. MOA: Same as before 2/12/2020 5 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Indications A. As an alternative to penicillin in Pharyngitis, Tonsilitis, Community acquired respiratory infections Diphtheria Syphilis & Gonorrhoea SABE ( Subacute Bacterial Endocarditis) Chancroid B. As a first choice of drug for Atypical pneumonia caused by mycoplasma pneumonia Whooping cough 2/12/2020 6 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Dose: Adult : 250-500 mg QID ( max. 4 gm / day) Children: 30-60 mg/kg/day Side Effects: Mild to severe epigastric pain Reversible hearing loss Rashes, Fever Jaundice C/I: Heapatic dysfunction 2/12/2020 7 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Azithromycin It is a macrolide antibiotics MOA: Same Indications: Legionnaires pneumonia:-500mg OD 3-5 days Urethritis & Genital infections:-1 gm stat Pharyngitis, Tonsilitis, Sinusitis, Otitis media, skin & soft tissue infections: 500 mg OD 3-5 days Children: 10mg/kg/day 2/12/2020 8 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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CI:- Hepatic impairment, pregnancy, below 6 months ADR:- Nausea, vomiting, headache, dizziness, Mild gastric pain, diarrhoea, flatulence, vertigo 2/12/2020 9 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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2/12/2020 10 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Aminoglycosides These are the group of protein syntheis inhibitors effective against Gram –ve bacteria. Streptomycin was the first member of this group discovered in 1944. All the aminoglycosides are isolated from soil actinomycetes & have common properties are not absorbed orally and donot penetrate CSF Excreted unchanged in urine by glomerular filtration Have relatively narrow margin of safety between therapeutic and toxic dose Exhibit ototoxicity and nephrotoxicity. 2/12/2020 11 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Systemic aminoglucosides: Streptomycin, Gentamicin, amikacin, tobramycin, kanamycin Topical aminoglycosides: Neomycin, Framycetin MOA: Aminoglycosides bind to the 30s subunit of bacterial ribosome and inhibit protein synthesis. It is bactericidal in nature. 2/12/2020 12 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Indications Pseudomonal infection ( burn, UTI, Lung abscess) Pneumonia Plague SABE Bacteraemia, Septicaemia Post-op infection Meningitis 2/12/2020 13 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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ADR Ototoxicity Nephrotoxicity Neuromuscualar paralysis Headache Vertigo Ataxia CI: Pregnancy, Renal failure 2/12/2020 14 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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2/12/2020 15 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Streptomycin It is the oldest aminoglycoside antibiotic obtained from streptomyces griseus. It is used extensively in the past but now practically restricted to treatment of Tuberculosis. MOA: bind to the 30s subunit of bacterial ribosome and inhibit protein synthesis 2/12/2020 16 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Indications Tuberculosis SABE Plague 2/12/2020 17 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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ADR Ototoxicity Nephrotoxicity Neuromuscualar paralysis Headache Vertigo Ataxia CI: Pregnancy, Renal failure 2/12/2020 18 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Gentamicin It was obtained from Micromonospra purpurea in 1964. It has become the most commonly used aminoglycoside for acute infection. MOA: bind to the 30s subunit of bacterial ribosome and inhibit protein synthesis 2/12/2020 19 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Indications It is the cheapest & the first line aminoglycoside but because of low therapeutic index its use should be resticted to serious gm-ve bacillary infections like SABE, Meningitis, Otitis media, eye infection Burns, UTI, Pneumonia, Ling abscess, osteomyelitis, ear infection, septicaemia 2/12/2020 20 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Gentamicin is drug of choice for treating respiratory infections in critically ill patients, in those with impaired host defence( receiving anticancer drugs, high dose of corticosteroids, AIDS), post operative pneumonia, In ICU Meningitis caused by gm-ve bacilli 2/12/2020 21 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Route of administration: local & Parenteral Preparation available: Injection & ointment, drop Dose : Adult: 1.5 to 2 mg/kg loading dose, followed by 1 to 1.7 mg/kg IV or IM every 8 hours or 5 to 7 mg/kg IV every 24 hours Duration of therapy: 14 days, depending on the site, nature, and severity Child:- 3 mg/kg IV or IM once every 24 hours or 1 mg/kg every 8 hours 2/12/2020 22 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Gentamicin loss of appetite may occur. Pain/irritation/redness at the injection site may infrequently occur. 2/12/2020 23 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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AMIKACIN It is awide spectrum aminoglycoside active against a wide variety of Gm+ve & Gm-ve bacteria. MOA:- Uses: Septicaemia, bacteraemia, RTI, bone & Joint infection, skin & soft tissue infection, post operative infection, UTI Dose: 15-20 mg/kg/day BD or TDS 2/12/2020 24 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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2/12/2020 25 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Tetracycline 2/12/2020 26 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Tetracycline Tetracyclines are group of closely related comound consisting of four fused ring with a system of conjugated double bond. They are the broad spectrum bacteriostatic antibiotic. MOA: They bind reversibly to the 30s subunit of the bacteria and inhibit the protein synthesis. 2/12/2020 27 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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USES: Drug of choice in infection with mycoplasma pneumonia, chlamydiae (genital disease), rickettsiae, spirochetes Used in combination regimens to treat gastric and duodenal ulcer disease cused by Helico Bacter Pylori In treatment of protozoal infection due to histolytica and plasmodium falciparum Acne Upper respiratory infection Vibro cholera Community accquired pneumonia Plague brucellosis 2/12/2020 28 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Adverse reaction Nausea, vomiting diarrhoea Tetracyclines are not completely absorbed so unabsorbed tetracycline in intestine causes super infection by alteration of normal flora. They modify normal with suppression of susceptible coliform organisms and overgrowth of pseudomonas, proteus, staphylococci, candida, clostridia. This can result in intestinal functional disturbances and pruritis, vaginal or oral candidiasis or enterocolitis with shock and death (Irritative diarrhoea) 2/12/2020 29 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Vestibular toxitcity results from high concentratin of drug in vestibular fluid Phototoxicity with doxycycline 2/12/2020 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd 30
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Coloration of bone Tetracycline readily bound to calcium, bound to newly formed bone or teeth in young children cause the discoloration of teeth. They cross placental barriers so during pregnancy tetracycline given to mother may be deposited in foetal teeth leading to discoloration. Similarly in case of bone it may cause deformity or growth inhibition It decreases renal function so except doxycycline and minocycline other are not give in renal impairment 2/12/2020 31 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Chloramphenicol It is a broad spectrum bacteriostatic antibiotic active against wide range of gm-ve & gm+ve organisms. MOA: Chloramphenicol binds to the bacterial 50S ribosomal subunit & inhibit protein synthesis. 2/12/2020 32 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Preparation & administration: Chloramphenicol can be administered orally or intravenously. The common route of administration of chloramphenicol is oral caps. Also available as dry syrup , suspension, opthalmic oint. 2/12/2020 33 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Guidelines for chloramphenicol therapy Because of serious bone marrow toxicity Never use chloramphenicol for minor infections or those of undefined etiology. Do not use chloramphenicol for infections treatable by other safer antimicrobials. Avoid repeated courses. Daily dose not to exceed 2-3g; duration of therapy to be <2 weeks, total dose in a course<28g Combined formulation of chloramphenicol with any drug meant for internal use should be avoided. 2/12/2020 34 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Indications. Enteric fever; chloramphenicol was the first antibiotic & drug of choice for typhoid fever till 1980s. But because of emergence of resistant bacteria, severe toxicity it is replaced by other antibiotics now a days. Pyogenic meningitis. 3rd generation cephalosporin are presently the first line drug for emperical therapy of bacterial meningitis. chloramphenicol in a dose of 50-75 mg/kg/day may be used as a 2nd line drug for H. influenzae &meningococcal meningitis, especially in young children & cephalosporin allergic patients. 2/12/2020 35 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Indications Intraocular infections: chloramphenicol is the preferred drug for endophthalmitis caused by sensitive org. In conjuctivitis, external ear infections. Severe gastroenteritis Anaerobic infections Gas gangrene 2/12/2020 36 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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DOSE Adult dose: 250-500 mg QID Children:25-50mg/kg/day 2/12/2020 37 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Contraindications: pregnancy, breast feeding, blood dyscrasis, prolonged use, minor infections, bone marrow depression 2/12/2020 38 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Adverse effects. Bone marrow depression. It results from binding of chloramphenicol to mitochondrial ribosome(host) becoz of similarity with bacterial ribosome. It occurs mainly in high conc. when serum conc. Reaches above 25mcg/ml. So chloramphenicol is the main cause of aplastic anaemia, agranulocytosis, thrombocytopenia Pancytopenia(reduction in the number of red and white blood cells, as well as platelets) 2/12/2020 39 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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Adverse effects. 2 Gray baby syndrome. It occur when high doses (=100mg/kg) were given to neonates. In neonate, infant renal function is not properly developed. So they cannot adequately metabolize & excrete chloramphenicol. It leads to accumulation of chloramphenicol in the body which in turn interfere with the function of mitochondrial ribosome resulting 2/12/2020 40 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd
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9 Symptons of Gray Baby Syndrome Cardiovascular collapse Gray skin color Abdominal swelling Low blood pressure Low body temperature Irregular breathing Vomiting Refuse to suck liquids Green stools 2/12/2020 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd 41
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Adverse effects. Irritative effects; nausea, vomiting, diarrhoea, Superinfections Hypersensitivity reactions: Rashes, fever, itching Impaired vision, irreversible aplastic anaemia, optic neuritis. 2/12/2020 42 Pabitra Thapa, Pharmacist, Asianpharmaceuticals Pvt. ltd