Therapeutic Interventions for Bacterial Infections Flashcards
Structure of bacterial cell walls
- peptidoglycan molecules in their cell walls that protect them from the environment
- peptidoglycan molecules form a set of chains called penicillin-binding proteins because penicillins and related antibiotics bind to them
Penicillins
- beta-lactam ring structure of penicillin binds PBPs causing lysis of growing bacteria by damaging cell walls
Resistance to penicillin
- mutate so they lack the PBPs that are the target of penicillins
- secrete an enzyme (penicillinase or beta-lactamase) that splits penicillin;s beta-lactam ring, often in response to penicillin
Penicillin Generalization
- mainly active against gram-positive bacteria
- most have narrow spectrum of antimicrobial activity
- widely distributed to tissues
- nearly all are rapidly excreted by kidneys
- short half-lives so it has to be given more often
Prototype Drug: Penicillin G Potassium
- therapeutic effects and uses
- mechanism of action
- Adverse effects
- mostly gram-positive bacteria/ bacterial endocarditis and prosthetic heart valves, rheumatic fever, congenital heart disease
2/ inhibits bacteral cell wall synthesis by binding to PBPs - urticaria/allergies/anaphylaxis
Cephalosporins - 20 types in 5 generations
- first - gram positive and some gram negative
- second - broader spectrum than first
- third - broader spectrum than second and longer duration of action
- fourth - effective against bacteria that are resistant to earlier generations
- fifth - extended gram-positive effectiveness, including MRSA infections
Cephalosporins Generalizations
- generally safe
- most common side effects (allergy/rash/GI complaints)
- elimination in kidneys
- use with caution in nursing mothers and patients with renal impairment
Cephalosporin prototype Drug: Cefotaxime
- therapeutic effects and uses
- mechanism of action
- adverse effects
1 . third generation cephalosporin with broad spectrum activity against both gram + and gram - / infections of the respiratory tract, urinary tract, genital infections, septicemia, meningitis, endocarditis, bone and joint infections
/infection prophylaxis in surgical patients
2. inhibits bacterial wall synthesis by binding to specific PBPs
3. rash, diarrhea, allergic response, potential superinfection, pain, phlebitis and IM injection sites, anaphylaxis, seizures
Carbapenems
broad-spectrum antibiotics with similar properties to other beta-lactams
- provide better activity against serious gram - and multidrug resistant infections than most cephalosporins or penicillins
- low incidence of adverse effects
Tetracyclines
- active against both gram negative and gram positive bacterial.
- drug of choice for typhus, cholera, rocky mountain spotted fever, lyme disease, H. pylori, ulcers and chlamydia
- bacteriostatic - prevents formation of proteins from amino acids. prevents making of bacterial cell wall.
- wide spread resistant to tetracycline has developed.
- take on empty stomach
- incompletely absorbed in intestine, thus can alter flora, causes super-infection
- if given parenterally, can be hepatotoxic and cause photosensitivity
Prototype Drug Tetracycline
- therapeutic effects and uses
- mechanism of action
- Adverse effects
- Serious Adverse effects
- susceptible gram + and gram - bacterial including: chlamydia, rickettsia, mycoplasmas, certain protozoa, H. pylori
- inhibits bacterial protein synthesis. Terminates the growing amino acid chain prematurely
- super infections/nausea vomiting epigastric burning diarrhea/discoloration of teeth/photosensitivity/
- hepatotoxicity/anaphylaxis/exfoliative dermatitis
Macrolides
- most effective against gram-positive
- alternative drugs for patients allergic to penicillin
- generally well tolerated and safe
- decreased hepatic metabolism of other drugs thus drug interactions are possible
- bacteriostatic in low doses, can be bactericidal in high doses
- suffix - thromycin
Macrolide prototype drug: Erythromycin
- therapeutic effect
- mechanism of action
- adverse effects
- serious adverse effects
- prophylaxis and treatment of susceptible bacterial infections including legionella, chlamydia, listeria, campylobacter, as well as upper and lower respiratory tract infections and skin infections
- inhibits protein synthesis/kills of bacteria/considered bacteriostatic, but may be bactericidal in high doses
- N&V/abdominal cramping/phlebitis
- Cholestatic hepatitis/ototoxicity (hearing loss, vertigo, dizziness)/cardiotoxicity - palpitations, chest pain, arrhythmias
Aminoglycosides
- effective against aerobic gram-negative bacteria including pseudomonas, enterobacteriaceae family, also used for TB
- prevention of protein synthesis
- bacteriostatic
- reserved for serious systemic infections, must be given parenterally
- associated with post-anitbiotic effect (activity of drug continues even as serum levels drop)
- may serious adverse effects including nephrotoxicity, ototoxicity, and neuromuscular blockade, thus these drugs are only used when other drugs are not effective
Aminoglycosides: Prototype Drug - Gentamicin
- therapeutic effects and uses
- Mechanism of action
- adverse effects
- serious adverse effects
- serious infections caused by aerobic, gram-negative bacilli/a few gram-positive bacteria, including some strains of MRSA
- inhibits protein synthesis
- N&V/rash and fatigue
- ototoxicity/nephrotoxicity/neurmuscular blockage/neurotoxicity