ANTIBACTERIAL DRUGS 3 Flashcards
Nyatakan kelas & ubat bagi moa menghalang sintesis protein (jejas scr langsung fungsi ribosom)
(1) 50s - macrolide,clindamycin,chloramphenicol,
oxazolidinones
(2) 30s - aminoglycosides,tetracycline
(3) Miscellaneous antibiotic - fusidic acid
Nyatakan cth ubat bagi Macrolide & MOA
- cth ubat : erythromycin , azithromycin, clarithromycin , roxithromycin
MOA : Macrolide bertindak pd subunit ribosom ke 50s pd bact. - Kemudian, akan menghlg translocation iaitu perpindahan peptidyl tRNA dari tapak A ke tapak P
- Menghlg proses pemanjgn rantaian polipeptida
Macrolide Indication
- Rawatan dan pencegahan jangkitan disebabkan oleh staphlococci and pneumococco dan kalangan individu yang
hypersensitive kepada penicillin. - Intracellular dan atypical bacteria (Azithromycin)
- H. pylori dalam ulser ppetic (Clarithromycin)
- 2nd line untuk rawatan Gonnorhea dan Syphilis.
- Rawatan jangkitan middle ear dan sinus (H. influenza danStrep. Pneumonia)
Macrolide Side Effects , Adverse Effects & Drug Interactions
Side Effects : Nausea Vomiting Tinnitus Cholestasis hepatitis
Adverse effects :
Epigastric distress (Erytromycin) Bacterial resistance (used more than 1 week)
Hypersensitivity
Drug Interactions :
Epigastric distress (Erytromycin) Bacterial resistance (used more than 1 week)
Hypersensitivity
Macrolide Warning & Precaution
- Patients with known QT prolongation ora history of ventricular dysrhythmia.
- Patients on medications that prolong the QT interval: antipsychotic medication including atypical antipsychotics, amiodarone & other antiarrhythmics, some antidepressants.
- Pregnancy, heart disease and electrolyte
disturbances
Terangkan Lincosamides
- Lincomycin
- Clindamycin : semisynthetic of Lincomycin & lebih potent
Terangkan Clindamycin dri segi MOA
MOA : bertindak pd subunit ribosom ke 50s pd bakteria
- menghalang translocation iaitu perpindahan peptidyl tRNA dari tapak A ke tapak P
- halang proses pemanjgn rantaian polipeptida
Clindamycin Indication, Side Effects, Adverse Effects & Drug Interaction
Indication : Digunakan sebagai rawatan alternatif untuk jangkitan akibat anaerobic bakteria. Digunakan secara topikal bagi rawatan jerawat. Digunakan dalam jangkitan tulang dan sendi.
Side Effects :
Diarrhea, Pseudomembranous colitis, Unpleasant/ metallic taste in mouth, Joint pain, Nausea, Vomiting
Adverse Effects :
- Superinfection by resistant clostridia
Drug Interaction :
- Vaccine BCG, Cholera, Tyhpoid
Disease interaction: Colitis, Prematurity,
Liver disease, Renal dysfunction
Clindamycin Warning & Precaution
May cause overgrowth of dangerous bacteria in the large intestine. This may cause mild diarrhea or may cause a life-threatening condition called colitis (inflammation of the large intestine)
diarrhea, myasthenia gravis,Crohn’s disease, ulcerative colitis,severe liver disease, blood in the bowel movement, severe renal impairment, atopic dermatitis
Terangkan Chloramphenicol dri segi MOA & spectrum activity
MOA : - merencat sintesis protein dgn mengikat pd ribosom 50s
- halang pemanjangan rantai protein dgn merencat peptidyl transferase
- peptidyl transferase berfungsi mengikat 2 asid amino dgn ikatan peptide utk hasilkan protein
SPECTRUM ACTIVITY : - broad spectrum
- limited use due to severe toxicity
Chloramphenicol Indication
Digunakan sebagai alternatif kepada Macrolide dan Tetracycline untuk jangkitan disebabkan oleh atypical
bacteria (Mycoplasma, Legionella, Ricketssia, Coxiella)
Digunakan sebagai alternatif kepada Penicliin dan Cephalosporin untuk rawatan meningitis (H. Influenza), Typhoid fever dan jangkitan anaerobic bakteria.
Digunakan sebagai eye drop dan oinment untuk jangkitan pada mata.
Chloramphenicol Adverse Effects & Drug Interaction
Adverse Effects :
Bone marrow suppression
Aplastic anemia
Grey baby syndrome
Drug Interactions :
Merupakan enzim inhibitor kepada CYP450
Chloramphenicol Warning & Precaution
Very bad and sometimes deadly blood problems have happened with chloramphenicol.
This may cause more chance of getting an infection, bleeding problems, or slow healing.
Aplastic anemia that happened with
chloramphenicol has led to a certain kind of cancer (leukemia)
Terangkan Oxazolidinones
- cth ubat : Linezolid (bacteriostatic)
MOA : - mengikat pd bacteriak 23s ribosomal RNA of the 50s subunit - halang pembentukan 70s ribosomal unit lalu merencat sintesis protein
SPECTRUM ACTIVITY : - efektif pd drug resistant gram (+) : vancomycin & MRSA
- limited to serious bacteria infection when other antibiotic fail
Linezolid Indication, Adverse Effects & Drug Interaction
Indication :
-Limited to serious bacteria infection
when other antibiotic fail.
Adverse Effects :
- Thrombocytopenia
Drug Interactions :
Makanan tinggi tyramine kerana boleh menyebabkan hypertensive crisis.
Alkohol
Disease interaction:
Collitis
Bone marrow suppression
Linezolid Warning & Precaution
- Diarrhea from an infection with Clostridium difficile bacteria.
- Pheochromocytoma, Thyrotoxicosis, Carcinoid syndrome, pancytopenia
- Increased blood acidity due to high levels of lactic acid.
Nyatakan cth ubat bg 30s ribosome inhibitor
(1) Aminoglycosides : amikacin , gentamicin , neomycin , kanamycin , streptomycin
(2) Tetracycline : tetracycline , chlortetracycline , oxytetracycline , minocycline
Terangkan MOA Aminoglycosides
- bertindak pd subunit ribosom yg ke 30s pd RNA bakteria
- menganggu translation hingga menyebbkn pentafsiran genetik kod yg salah pd rantaian ribosom bact & menghasilkan sintesis protein yg abnormal
- ganggu translocation tRNA dari tapak A ke tapak P dan menyebabkan pemanjgn rantai polipeptida terhlg & tiada pembentukan rantai polipeptida yg lengkap
Terangkan Aminoglycosides dri segi spectrum activity & lain2
SPECTRUM ACTIVITY :
- narrow spectum , efektfi pd gram (-) bacilli & sedikit gram (+) cocci & mycobacteria TB
LAIN2 :
- concentration dependent : keupayaan membunuh bact meningkat sbaik shj kepekatan antibiotik meningkat
- post antibiotic effect : masih berupaya membunuh bakteria walaupun kepekatan antibiotik dibawah MIC
Aminoglycoside Indication
Plaque, brucellosis dan 1st line untuk
tuberculosis.(Streptomycin)
Jangkitan disebabkan gram negative
(Gentamicin, Tobramycin)
Dalam gram negative septicemia secara
kombinasi dengan Penicillin dan
metronidazole.
Pseudomonas infections secara kombinasi dengan antipseudomonal penicillin.
Enterococcal endocarditis secara kombinasi
dengan Vancomycin dan Gentamicin.
Hepatic encephalopathy (Neomycin)
Sterilization of intestine before surgery and bacillary dysentery (Neomycin)
Secara topical untuk kulit dan mata secara kombinasi dengan Polymixin B atau Bacitracin
Aminoglycosides Adverse Effects & Drug Interaction
Adverse Effects :
- Nephrotoxicity, Ototoxicity, Neuromuscular block, Malabsorption
Drug Interactions :
- Antibiotics, Skeletal muscle relaxants, Anticoagulants, Diuretics
Aminoglycosides Warning & Precaution
- Avoid aminoglycosides if you’re allergic to them or any inactive ingredients these drugs may contain.
- Are allergic to sulfites (often found in
certain wines and dried fruits) - Have kidney or hearing problems, including problems with balance and uncontrollable eye movements
- Have a disorder affecting the nerves and
muscles, like multiple sclerosis or
myasthenia gravis. - Are 65 years of age or older
- You have a newborn or very young baby
who might be treated for a serious infection using aminoglycosides
Terangkan Tetracycline dri segi MOA & Spectrum Activity
Cth : Tetracycline, Chlortetracycline, Oxytetracycline, Minocycline, Demeclocycline (not in FUKKM)
MOA : - tetracycline bertindk pd subunit ribosom ke 30s bacteria
- halang kemasukan amino acyl-tRNA ke mRNA ribosom complex di tapak penerima (A)
- menyebabkan sintesis protein bacteria terencat
SPECTRUM ACTIVITY : broad spectrum
Tetracycline Indication & Adverse Effects
Indication :
- Sebagai alternatif pada Macrolide dalam jangkitan disebabkan Chlamydia, Mycoplasma dan Legionella. (Doxycycline)
- Lyme disease, Typhus dan Rocky Moutain spotted fever, Acne vulgaris, Cholera
Adverse Effects :
- Epigastric distress, Yellow staining, Cholestatic hepatitis, Phototoxicity, Superinfection
Tetracyline Drug Interaction & Warning & Precaution
Drug Interaction : - Calcium channel blockers is of clinical significance because when these agents are given concurrently during the perioperative period they may lead to respiratory depression or prolonged apnoea.
Warning & Precaution
- Severe hepatic disease and renal disease, Peptic ulser, Kanak kanak bawah 8 tahun, Pregnancy and lactation
Terangkan Miscellaneous Antibiotik (Fusidic Acid) dari segi MOA & Spectrum Activity
MOA : - merencat sintesis protein dgn halang pengikatan tRNA pd ribosom
SPECTRUM ACTIVITY : narrow spectrum
- efektif pd gram (+) bacteria
Fusidic Acid Indication , Side Effects & Adverse Effects
Indication : Digunakan secara kombinasi dengan agen antistaphylococcal dalam staphylococcal sepsis. Digunakan secara topical dalam eye infection
Side Effects :
- Skin rashes, Skin itching, Pain, stinging, burning sensation or redness of skin on application, Contact dermatitis
Adverse Effects :
- Jaundice, Skin eruption
Fusidic Acid Drug Interaction, Warning & Precaution
Interactions :
Ritonavir and Saquinavir: inhibition of
metabolism and increased fusidic acid
levels.
Cholestyramine: binds fusidic acid and
decreases bioavailability.
Warning & Precaution
- Use caution in patients with jaundice/
hepatic dysfunction.