Microbiology Drugs Flashcards
Antimicrobials drugs that inhibits the folic acid synthesis and reduction ( DNA methylation) ;
- Sulfonamides.
- Trimethoprim
Which type of penicillin use as IV and IM ?
Penicillin G
Which type of penicillin used as oral ?
Penicillin V
Which Antimicrobials drugs contains Beta lactam ring ?
- Penicillin.
- Cephalosporins.
- Carba-penems
- Monobactam (Aztreo-nam).
Mechanism of penicillin:
Penicillin break down of the bacterial cell wall by inhibition of the cross-linking of transpeptidase, therfore, it’s prevent the cell wall formation— lead to increasing the osmotic pressure in the cell —- lyisis of the cell .
Penicillin doesn’t affects the human cell wall due to :
Because the human cell wall consist of L-Ala (not D-Ala like the bacteria )
Cross linking of the bacterial cell wall occurs by :
Transpeptidase( penicillin binding protein )
Clinical use of penicillin :
- Gram + (s.pneumonea, s. Pyogenes {specially for sore throat}, Actinomyces )
- Gram (-) cocci : mainly(N.meningitis)
- Spirochets :( T.pallidum)
- Penicillinase sensitive.
What is penicillinase ?
B-lactamase enzyme present in the periplasm of the gram (-) bacteria .
Mechanism of penicillinase “B-lactamase” ?:
Destruction of beta lactam ring.
Adverse effect of penicillin:
- Hypersinsivity (type1,2,3,4)
- Jaresch-herxeimer reaction
What’s the hypersinsivity reaction of penicillin ?
- Type 1 hypersinsivity
- Type 2 hypersinsivity ( Hemolytic anemia ).
- Type 3 hypersinsivity (Serum sickness).
- Type 4 hypersinsivity (Maculopapular rash).
Hemolytic anemia that cause by penicillin, which typer of hypersinsivity reaction is considered?
Typer 2 hypersensitivity
Maculopapular rash that cause by penicillin, which type of hypersinsivity reaction considered ?
Type 4 hypersinsivity reaction
Resistance of penicillin by :
- Penicillinase(B-lactamase)
- Modification of PBP( changing of penicillin-binding protein )
- Reduced bacterial cell pentration by:
*Gram (-) bacteria “that have outer membrane “.
*decrease number of porins channel ( that responsible for transporting chemical element to outside and inside the bacterial call ).
Which drug increase the duration of penicillin in the blood by decrease the penicillins renal secrtion?
Probencid
B-lactamase inhibitors :
- Clavulanic acid
- Sul-bactam
- Tazo-bactam
- Avi-bactam
Penicillinase-sensitive penicillin (anino-penicillins): oral, IV ..?
- Amoxicillin (oral)
- Ampicillin (IV)
Mechanism of Penicillinase-sensitive penicillin :
The same with penicillin but have more Penetration of porin channels of gram (-) bacteria .
Augmentin it’s :
Amoxicillin + clavulenic acid
Augmentin (Amoxicillin +clavulanic acid) uesed for :
Resistance cases of otitis media
Unasyn (Ampiccillin +sulbactum) uesed for :
Surgical infection
Clinical use of penicillinase-sensitive penicillin :
- HHELPSS :
- H-influenza,
- H-pylori,
- E.coli,
- Listeria
- Proteus
- Salmonella,
- Shigella, ++++ enterococci
Penicillinase- resistance penicillins (antistaphylococcal penicillins ):
- Dicl-oxa-cillin.
- Naf-cillin.
- Oxa-cillin.
- Methi-cillin.
Mechanism of Penicillinase- resistance penicillins (antistaphylococcal penicillins ):
Same with penicillin.
Why Penicillinase- resistance penicillins are resistance to penicillinase ?
Because “bulky side chain R group “ block access of B-lactamase to B-lactamase ring.
Clinical use of Penicillinase- resistance penicillins (antistaphylococcal penicillins ):
S.aureus skin infection{cellulitis and impetigo, folliculitis } (except MRSA resistance)
Adverse effect of Penicillinase- resistance penicillins (antistaphylococcal penicillins ):
- Hypersinsivity
- Acute Interstitial nephritis.
Antipseudomonal penicillins :
- Pi-pera-cillin,
- Ticar-cillin .
Piperacillin, ticarcillin used for :
1.Pseudomonas
2. Most gram (+) bacteria
Ticarcillin + clavulonate =
Time-nitin
Piperacillin+ tazobactam =
Zosyn
Penicillin is bactericidal or bacteriostatic
Bacteriocidal
Cephalosporins is bactericidal or bacteriostatic
Bactericidal
Mechanism of cephalosporins ?
B-lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinase .
Which organism not covered (not effected ) by 1st-4th generation of cephalosporins ?
LAME
1. Listeria
2. Atypical {mycobacterium, chlamydia}
3. MRSA
4. Enterococci
1st generation of cephalosporin:
- Cefa-zolin,
- Ceph-alexin.
2nd generation of cephalosporin:”
- Cefa-clor,
- Cefo-xitin,
- Cefu-roxime.
3rd generation of cephalosporin :
- Cef-triaxone,
- Cef-tazidime
- Cef-podoxime,
- Cefo-taxime
4th generation of cephalosporin:
Cefepime
5th generation of cephalosporin:
Cefta-roline
Clinical use of 1st generation of cephalosporin:
** KEP:-
1. Proteus
2. E.coli
3. Klebsiella pneumonia
Which drug used prior to surgery to prevent s.aureus wound infection ?
Cefazolin
Clinical use of 2nd generation of cephalosporin
KEP +SHEN
1. H-influnza
2. Enterobacter
3. Niesseria
4. Serratia
Which drug from 3rd generation of cephalosporin used for meningitis and gonorrhoea and disseminated Lyme disease ?
Ceftriaxone
Which drug from 3rd generation of cephalosporin used for pseudomonas?
Ceftazidime
Which generation of cephalosporins covered the listeria and MRSA and enterococcus but not covered the pseudomonas ?
5th genereation(ceftraoline)
Which drugs have this adverse effects: hypersinsivity reaction, autoimmune hemolytic anemia, disulfiram-like reaction, vit K deficiency , hypoprothombinemia, increasing of neurotoxicity of aminoglycosides ?
Cephalosporins
Carba-penems drugs :
- Imi-penem.
- Mero-penem.
- Erta-penem.
- Dori-penem.
Which drugs that inhibitor of renal dehydropeptidase 1?
Cilastatin
Why the 5th generation of cephalosporins covers the listeria and enterococcus and MRSA ?
Because it’s bind on another site that the fist 4 generation bind to it, it bind to PBP2a
Which drug of carbapenems inhibit by renal dehydropeptidase ?
Imipenem
Which drug of carbapenems have CNS toxicity side effect (seizures)?
Imipneme
Why the meropneme bitter than imipneme ?
- Because the imipneme break down by renal dehydropeptidase-1
- Because the imipneme have CNS toxicity side effect (siezures)
Monobactams (aztreonam) mechanism of action:
- Prevent the peptidoglycan cross-linking by binding to PBP-3 (only in G-negative).
- Synergistic with aminoglycosides .1+1=3
Clinical use of monobactams :
- For penicillin allergic.
- Patient those with renal insufficiency who can’t tolerate aminoglycosides
- Gram (-) rod only
Which drug that have the highly resistance to B-lactamase ?
Carbapenems
Which drug that have highly sensitive to B-lactamase ?
Penicillins
Penicillin binding protein :
1. PBP-3 :?
2. PBP-2a ?
- PBP-3: aztreonam
- PBP-2a: ceftaroline.
اقوى سلاح لل: gram - bacteria
B-lactamase
Mechanism of vancomycin :
Inhibit cell wall peptidoglycan formation by binding D-ala D-ala portion of cell wall precursor .
Why Vancomycin can’t affects the gram (-) bacteria ?
Because it has too large molecule that can’t pentrate the outer membrane of the gram (-) bacteria
Which drugs cause red man syndrome as adverse effects?
Vancomycin
Which drug can cause nephrotoxicity , ototoxicity, thrombophlebitis?
Vancomycin
Which syndrome characterised by diffuse flushing of the whole body, and non specific mast cell degranulation “histamin release” ?
Red man syndrome
Treatment of red man syndrome. :
- Stop the drug
- Give Anti-Histamines
- Restart the medication
Mechanism of resistance of vancomycin ?
Via amino acid modification of D-Ala D-Ala to D-Ala D-Lac
Treatment of MRSA by:
.6 ادويه
Treatment of VRSA by :
- Quinu-pristin
- Dalfo-pristin
All protein synthesis inhibitor are bacteriostatic except :
Aminoglycosides
Amino glycoside is bactericidal due to
Miss reading of mRNA
Which of protein synthesis inhibitor are variable( bacteriostatic + bacteriocaidal) ?
- Dlafo- pristin.
- Quinu-pristin.
Protein synthesis inhibitor divided into : 30s inhibitor and 50s inhibitor, which drug are the 30s inhibitors ?
- Aminoglycosides
- Tetracycline
Protein synthesis inhibitor divided into : 30s inhibitor and 50s inhibitor, which drug are the 50s inhibitors ?
- Chloramphenicol
- Clindamycin
- Marcrolides
- Linezolides
- Strepto-gramins
Aminoglycosides drugs:
- “GNATS “
1. Genta-mycin
2. neo-mycin
3. Amikacin
4. Tobra-mycin
5. Strepto-mycin
Mechanism of aminoglycosides :
- Irreversible inhibtion of initiation complex though binding to 30s subunit causing missreading of mRNA
- Block translocation
Why aminoglycosides ineffective aginst anaerobes ?
Because it require O2 for uptake
Which drugs use for severe gram (-) rod infection , and also can be synergistic with B-lactam antibiotics ؟
aminoglycosides
Which aminoglycosides used for bowel surgery and hepatic encephalopathy ?
Neomycin
Aminoglycoside it synergistic with B-lactam antibiotics , it’s rare to used alone. Which aminoglycoside drug that use with vancomycin to treatment the endocarditis ?
Vancomycin + gentamycin
Aminoglycoside it synergistic with B-lactam antibiotics , it’s rare to used alone. Which aminoglycoside drug that use with ampicillin to treatment the neonatal meningitis ?
Ampicillin +gentamycin
Advers effects of aminoglycosides :
NNOT
1. Nephrotoxicity,
2. Neuromuscular blockage (⬇️ Ach) ,
3. Ototoxicity (specially when used with loop diuretics,
4. Teratogen
Which drug have this adverse effects: Nephrotoxicity, neuromascular blockage (⬇️ Ach) , ototoxicity (specially when used with loop diuretics, teratogen
Aminoglycoside
Mechanism of resistance of aminoglycosides :
- Bacterial transferase enzyme inactivate the drug by :
- Acetylation
- Phosphorylation
- Adenylation
Bacterial transferase enzyme inactivate the aminoglycoside by :
1.acetylation
2. Phosphorylation
3. Adenylation
Tetracycline drugs :
- Tetra-cycline
- Doxy-cycline
- Mino-cycline
Mechanism of tetracycline :
Bind to 30s and prevent attachment of aminoacyl-tRNA
Don’t take tetracycline with milk (calcium) antacid or iron due to :
The milk , antacids and irons decrease the absorption of the tetracycline in the gut.
Which drug have ability to accumulate intracellularly and make them very effective aginst rickettsia and chlamydia ?
Tetracycline
Which drug can use for borrelia burgdorferi and. M.pneumoniae, rickettsia and chlamydia and also used for treat acne ?
Tetracycline
Which drug can used in patient with renal faliure and have effect aginst MRSA?
Doxycycline
Which type of tetracycline not used as antibiotics, used as ADH antagonist, so it’s given for SIADH?
Demeclocycline
Which drugs have this adverse effects :
GI distress, discoloration of teeth, inhibition of bone growth in children , photosensivity, contraindicated in pregnance ?
Tetracycline
Which drug have this mechanism of resistance : ⬇️ Uptake or ⬆️ efflux out of bacterial cell by plasmid -encode transport pumps ?
Tetracycline
Clinical uses for tetracycline :
- Zoonosis : borrelia, M.pneumonea.
- Intracellular orgasnism : chlamydia, rickettsia
- Acne: prpprionecacterium
- Doxycycline : 1. Can use in case-of bacterial infection in patient with renal failure because it does not effect on kidney 2. MRSA
Drugs with photo-sensivity :
- Aminoglycosides
- Tetracycline
- Sulfonamides
Gly-cyl-cycline: drug
Tige-cycline.
What is tigecycline ?
tetracycline derivative bind to 30s and inhibit protein synthesis
Clinical use of tigecycline :
For multidrug-resistance (MRSA,VRE)
Mechanism of action of chloramphenicol :
Bind to 50s and inhibit peptidyltransferase
Clinical use for chloramphenicol:
- Meningitis,
- Rocky moutain spotted fever (in case of pregnancy for the 1st and 2nd trimester only )
Which drug if used it the pregnant women in the first and seconde trimester does not have side effect, but if she used it in the 3d trimester can lead to gray baby syndrome ?
Chloramphenicol
Gray baby syndrome cause by which enzyme lack in liver ?
Liver UDP-glucu-rony-ltransferase.
Which drug have this mechanism of resistance: plasmid-encoded acetyltransferase inactivates the drug
Chloramphenicol
Which syndrome characterised by : vomiting, ashen grey color of the skin, poor muscle tone, cyanosis, CV collapse ?
Gray baby syndrome
- Gray baby syndrome cause by :
- Gray man syndrome cause by :
- Red man syndrome cause by:
- Gray baby syndrome cause by :chloramphenicol
- Gray man syndrome cause by :amidarone
- Red man syndrome cause by: vancomycin
Macrolides:
- Az-thromycin
- Clari-thromycin
- Erthromycin
Mechanism of macrolides:
Inhibition of protein synrthesis by blocking translocation , bind to the 23S rRNA of the 50s subunit
Mechanism of clindamycin :
Block peptide transfer (translocation) at 50s ribosoma subunit “ same as macrolides
Which drug Block peptide transfer (translocation) at 50s ribosoma subunit “ same as macrolides
Clindamycin
Clinical uses of clindamycin :
- Anaerobic infection
- Group A strep infection
- MRSA
Which drugs cause pseudomembranous colitis as side effects ?
- Clindamycin
- Streptogramin
Mechanism of resistance of clindamycin :
As macrolides “methylation”
Oxazolidinones drug:
Linezolid
Mechanism of linezolid:
Inhibit protein synthesis by binding to 50s subunit- prevent formation of initial complex
Clinical uses of linezolid:
Last line for bacterial resistance (MRSA,VRE)
Which drug have thius adverse effects: bone marrow supression especially thrombocytpnea), peripheral neuropathy, serotonin syndrome when given with SSRIs (selictive serotonin reuptake inhibitors)
Linezolid
How linezolid lead to serotonin syndrome ?
When giver the linezolid with SSRIs , the linezolid is weak MAOIs (increase serotonin)+ SSRIs also increase the sertonin, taking the twice togther lead to serotonin syndrome
Which drug have point mutation of ribosomal RNA as mechanism of resistance ?
Linezolid
Which drugs can cause prephral neuropathy ?
- Linezolid
- isoniazid
Azithromycin, larithromycin, erthromycin, for which group of drug belongs?
Microlides
Which drug have this mechanism of action: ihibit protein synthesis by blocking translocation, bind to the 23s rRNA of the 50s ribosomal subuint?
Macrolides
How the macrolides effect aginst intracellular organisms?
By concentration inside the macrophage and other cells
Clinical use of macrolides :
- Atypical pneumonias ( Mycoplasma,chlamydia , legionella)
- Upper respiratory infection :( str. Pneumonia, str. Pyogenes, proteussis ).
- Streptococcal infection in patient allergic to penicillin.
Which drug of microlides can used in motility disoreder of GIT ( eg, gastroparesis) ?
Erthromycin
Erthromycin bind to which receptor in GIT, that leade to smooth muscle contraction ?
Motilin receptor
adverse effects of macrolide
GAARE
1. Gastrointistinal motility issues,
2. Arrhythmia
3. Acute cholestatic hepatitis
4. Rash
5. Esinophilia
Which macrolides inhibit cytochrome p-450 that lead to increase serum concentration of theophyline, oral anticoagulants ?
Erthromycin and clarithromycin
Mechanism of resistance of macrolides:
Methylation of 23s rRNA-binding site ,prevent binding of drugs.
Sulfonamides drugs :
- Sulfa-methoxazole (SMX)
- Sulfa-soxazole
- Sulfa-diazine
Which drug have this mechanism : inhibit dihydropteroate synthesis ?
1.Sulfonamide
2. Dapsone
Which bacteriostatic drug converts to bacteriocidal when combined with trimethoprim ?
Sulfonamides
Which drug have the following adverse effects : hypersensivity reaction, hemolysis if G6PD deficient, bind to albumin ?
Sulfonamides
Which drug have the following mechanism of resistance :
1. Altered enzyme ( bacterial dihydropteroate synthase)
2. ⬇️ uptake
3. ⬆️PABA synthesis
Sulfonamides
Which drug have similar mechanism to sulfonamides but structurally distinct agent, and use for leprosy and pneumocystis jivovecii prophylaxis ?
Dapsone
Which drug inhibit bacterial dihydrofolate reductase, and may cause megaloblastic anemia leukopenia, granulocytopenia?
Trimethoprim
Trimethoprim side effects :
Bone marrow supression:
1. Megaoblastic anemia
2. Leukopnia
3. Granulocytopenia
Which drug causing sequential block of folate synthesis in case of used in combination with sulfonamides ?
Trimethoprim
How the trimethoprim lead to megaloblastic anemia ?
By effect on human dihydrofolate reductase
Which drugs are vairable (static\sidal) and synthesized by the streptomycess virginia ?
Strepto-gramins:- quinupristin, dalfopristin
Strepto gramins used for:
- MRSA
- VRE
- Staph
- Strept skin infection
Fluroquinolones drugs :
- Cipro-floxacin
- Nor-floxacin
- Levo-floxacin
- Oflo-floxacin
- Moxi-floxacin
- Gemi-floxacin
- Eno-xacin
Which drugs inhibit prokaryotic enzymes topoisomerase 2 gyrse and topoisomerase 4 ?
Floroquinolones
Which drugs use for gram (-) rods of urinary and GI tract and some gram(+) organsims and otitis externa “ ?
Fluroquinolones
“Cipro drops “ ( fluroquinolones derivatives) used for :
Otitis externa
Which drugs have this adverse effects:, tendonitis or tendon rapture in people > 60 or patient taking prednisalon, cartilage damage in children, leg cramps and myalgias ,and may cause prolong QT interval ?
Fluroquinolones
Fluroquinolones contraindicated in :
- Old age -tendonitis
- Children <18 - cause cartilage damage
3 . Pregnant women - Nursing mother
Which fluroquinolon derivatives inhibit cytochrome p-450 ?
Ciprofloxacin
Which drugs have this mechanism of resistance: chromosome-encoded mutation in DNA gyrase, plasmid- mediated resistance efflux pumps ?
Fluroquinolones
Lipopeptide drug that disrupts cell membrane of gram (-) cocci by creating transmembrane channels ?
Depatomycin
Which drug have the following adverse effects :myopathy, rhabdo-myolysis ?
Depato-mycin
Which drug form toxic free radical metabolites in the bacterial cell that damage DNA that lead to cell death .
Metronidazole
What’s meaning of metronidazole prodrug ?
It’s inactive form of metronidazole
Activation of metronidazole (from prodrug to active drug) occurs by reduction, which organisms cand reducing it ?
Anaerobic bacteria
Why metronidazole work as antiprotozoa ?
Because it effects on the anaerobes, protozoa doesn’t have mitochondria so it’s anaerobes
Clinical uses of metronidazole :
1.Antiprotozoa “GGET” : giardia, entamobea, trichomonas, gradnerella vaginalis,
2. Anaerobic bacteria( bacteroides, c.difficile).
3. Can use in place of amoxicillin in triple therapy of H.pylori
4. Anaerobic infection below the diaphragm
Which drug has the following adverse effects: disulfram-like reaction( severe flushing, tachycardia, hypotension), metallic state .
Metronidazole
Prophylaxis of tuberculosis :
Isoniazid
Prophylaxis of M.avium-intracellulare :
Azithromycin, rifabutin
Treatment of tuberculosis:
- Rifampin
- Isoniazide
- Pyrazimaide
- Ethambutol
Treatment of M.avium-intracellulare :
- Azithromycin + ethambtul ( can also add rifabultin or ciprofluxacin )
- Clarithromycin + ethambtul ( can also add rifabultin or ciprofluxacin )
Treatment of M.leprae:
1. For tuberculoid form :
2. For lepromatous form :
- For tuberculoid form :dapsone and rifampin.
- For lepromatous form :dapsone + rifampin + clofazimine
Which drug used for treatment of tuberculosis by this mechanism :inhibit of bacterial DNA-dependent RNA polymerase .
Rifampin
Which drug used for treatment of tuberculosis by this mechanism : inhibit mycolic acid synthesis
Isoniazid
Which drug used for treatment of tuberculosis by this mechanism : inhibition of arabinosyl transferase ?
Ethambutol
Which drug used for treatment of tuberculosis and have this side effects : hepatotoxicity ,optic neuropathy?
Ethambutol
Which drug used for treatment of tuberculosis and have this side effects : hepatotoxicity red-orange body fluids, cytopnia , increase cyt p-450 :
Rifampin
Which drug used for treatment of tuberculosis and have this side effects : neurotoxicity, hepatoxicity, vit B6 deficiency , decrease cyt p-450
Isoniazid
Which drug used for treatment of tuberculosis and have this side effects : hepatotoxicity and hyperuricemia?
Pyrazinamide
Rifamycins drugs:
- Rifa-mpin.
- Rifa-butin
Which tuberculosis drug inhibit cytochrome P-450
, isoniazid
Isoniazid (inactive) converts to isoniazid( active) by:
Catalase peroxidase( that release from bacteria )
Which gene encoded the catalase peroxidase enzyme ?
KatG
Reisistance of isoniazide by mutation of which gene ?
KatG
Which tuberculosis drug increase cytochrome P-450
Rifampin
Which drugs block translocation?
- Macrolides
- Clindamycin
- Aminoglycosides
Dehydrofolate reductase :
1. In human inhibit by :
2. In baceria inhibit by :
- In human inhibit by : methotrexate
- In baceria inhibit by : trimethoprim, pyrimehamine
Mechanism of rifampin ?
Inhibition of DNA dependent RNA polymerase
Which drug used for tuberculosis as 2nd line and cause tinnitus, vertigo, ataxia, nephrotoxicity ?
Streptomycin
Which antimicrobial prophylaxis used in case of high risk for endocarditis and undergoing surgical or dental procedures ?
Amoxicillin
Which antimicrobial prophylaxis used in case of exposure to gonorrhea ?
Ceftriaxone + azithromycin
Which antimicrobial prophylaxis used in case of history of recurrent UTI
TMP-SMX
Which antimicrobial prophylaxis used in case of exposure to meningiococcal infection :
Ceftriaxone , ciproflocxacin, rifampin.
Which antimicrobial prophylaxis used in case of pregnant women carrying group B strep?
Intrapartum penicillin G or ampicillin
Which antimicrobial prophylaxis used in order to prevention of gonococcal conjunctivitis in newborn ?
Erthromycin ointment on eyes
Which antimicrobial prophylaxis used to prevention postsurgical infectioon due to s.aureus ?
Cefazolin
Which antimicrobial prophylaxis used to strep pharyngitis in child with prior rheymatic fever?
Benzathine penicillin G or oral penicillin V
Which antimicrobial prophylaxis used in case off exposure to syphilis
Benzathine penicillin G
Prophylaxis of HIV patients in case of CD4<200, with pneumocystis pneumonea ,
TMP-SMX
Prophylaxis of HIV patients in case of CD4< 100, with pneumocystis pneumonea ,toxoplasmosis :
TMP-SMX
Prophylaxis of HIV patients in case of CD4<50, with mycobacterium avium complex infection :
Azithromycin or clarithromycin
Treatment of MRSA:
- Vanco-mycin
- Dapto-mycin
- Linezolid
- Tige-cycline
- Cefta-roline
- Doxy-cycline
Treatment of VRE :
- Linezolid,
- Streptogramins (quinupristin, dalfopristin)
Different between amphotericin B and nyastatin in the clinical used:
Amphotericin uesd in systemic mycosis, but nyastatin used only in topical mycosis
Why Amphotericin B used only in case of severe fungal infection ?
Because it “amphoterrible” (have severe side effects )
Antifungal therapy that work on cell membrane integrity “ form membrane pores “
Polyenes :
1. Amphotericin B
2. Nyastatin
Antifungal therapy that inhibit nucleic acid synthesis :
Flu-cyto-sine
Antifungal therapy that inhibit cell wall synthesis :
Echino-candins:
1. Anidul-fungin
2. Caspo-fungin
3. Muca-fungin
Antifungal therapy that inhibit lanosterol synthesis :
Ter-bina-fine
Antifungal therapy that inhibit ergosterol synthesis :
Azoles :
1.clotrim-azole.
2. Flu-con-azole
3. Itra-con-azole
4. Keto-con-azole
5. Mi-con-azole
6. Vori-con-azole
Which drugs bind to ergosterol and forms membrane pores that allow leakage of elctrolytes?
Polyenes: amphotricin, nyastatin
Which antifungal drugs have the following side effects :fever, chills (shake and bake), hypotension, nephrotoxicity, arrhythmias, anemia , IV phelebitis (amphoterrible)?
Amphotericin B
The nephrotoxicity that cause by amphotricin can decrease it by :
Hydration
Which antifungal drugs inhibit DNA and RNA biosynthesis by conversion to 5-fluorouracil by cytosine deaminase ?
Flucytosine
Which antifungal drug used with combination with amphotricin to treat the systemic mycosis ?
Flucytosine
Side effect of flucytosine:
Bone marrow supression
Which antifungal drugs inhibit fungal stgerol(ergosterol) synthesis, by inhibition of the cytochrome P-450 enzyme that converet lanosterol to ergosterol
Azoles
Azoles inhibit fungal ergosterol synthesis by :
Inhibition of cytochrome P-450 that converts lanosterol to ergosterol
Which enzyme convert lanosterol to ergosterol in fungi?
14-alpha-demethylase (Cytochrome P-450)
Which azoles drug used for : chronic suppression of cryptococcal meningitis in AIDS patients?
Fluco-nazole
Which azoles drug used for : blastomyces, coccidioides, histoplasma?
Itra-con-azoles
Which azoles drug used for : atypical fungal infection?
- Clotrim-azoles,
- Mi-con-azoles
Which azoles drug used for : aspergillus and candida?
Voriconazole
Which azoles drug used for :aspergillus and mucorales infections?
Isavu-con-azole
Which antifungal dugs that can cause testesterone synthesis inhibition , gynecomastia
Azoles: specially”ketoconazoles”.
Azoles side effects:
- Testosterone synthesis inhibition ,
- Gynecomastia,
- Liver dysfunction (by inhibition of cytochrome P-450
Azoles can cause liver dysfunction by :
by inhibition of cytochrome P-450
Which antifungal drug inhibit the fungal enzyme squalene epoxide ?
Ter-bina-fine
Clinical uses of terbinafne :
Dermato-phytoses (especially onychomycosis -fungal infection of finger or toe nails)
What’s onychomycosis -
Type of dermatophytoses that characterized by fungal infection of finger or toe nails
Which antifungal drugs inhibit cell wall synthesis by inhibition synthesis of B-glucan ?
Echinocandins
Clinical uses of echinocandins :
Invasive aspergillus and candida
Which anti-fungal drug can cause GI upset and flushing ( by histamine release )?
Echinocandines
Which antifungal therapy interferes with microtubule function, disrupts mitosis. Deposites in keratin containing tissue ?
Griseo-fulvin
anti-malaria therapy
Chloro-quine
What happen when chloroquine block detoxification of heme into hemozin ?
Heme accumulates and it is toxic to plasmodia
Clinical uses of chloroqine :
Treatment of plasmodial species (except P.falciparum)
Artemether\lumefantrine or atovaquone\ proguani used for :
P.falciparum
For long treatment of malaria use :
- Quinidine
- Arte-sunate.
Side effects of chlorquine :
Retinopathy
Antihelminthic theapy that act as microtubule inhibitor :
Mebendazole
Infection by HIV occurs by fusion, fusion of HIV consist of two mechanisms :
1. Attachment.
2. Penetration
Which drgus inhibit this mechanism?>
- Attachment : mara-viroc
- Penetration: Enfu-virtide
HIV converts from RNA to DNA by reverse transcriptase to pentrate the nuceleus of the cell, we can prevent this pentration by :
reverse transcriptase inhibitors
reverse transcriptase inhibitors: two types
- NRTI “nucleotide reverse transcriptase inhibitors”
- NNRTI “ Non nucleotide reverse transcriptase inhibitors”
Integrase enzyme responsible for intigration of the HIV DNA with the Cell DNA , (After converting the HIV RNA to DNA ),whcih drug can prevent this process .
Integrase inhibitors :3 drugs the ends by “ gravir”
1. Dolute-gravir.
2. Elvite- gravir.
3. Ralte- gravir.
HIV utilize the proteolytic enzyme “protease” to lytic the protein that form after translation, we can prevent this process by :
Inhibition of protease enzyme
Protease inhibitor :(for HIV therapy)
Drugs that end by “navir”
1. Ataza-navir,
2. Lopi-navir,
3. Indi-navir etc…
General HIV therapy :
- Fusion inhibitors
- Reverse transcriptase inhibitors
- Intigrase inhibitors.
- Protease inhibitors
Viral protein synthesis inhibitors :
Interferon-alpha
Viral uncoting inhibitors :
- Aman-tadine,
- Riman-tadine .
Viral nucleci acid synthesis inhibitor :
- Guanosine analogs (acyclovir, ganciclovir).
- Viral DNA polymerase inhibitors ( cidofovir, foscarnet )
- Guanine nucleutide synthesis ( ribavirin )
Viral Guanosine analogs :
1.Acy-clovir.
2.ganci-clovir.
3. Famci-clovir
4. Valacy-clovir
Direct viral DNA polymerase inhibitors:
- Cidofovir.
2.foscarnet.
Guanine nucleutide synthesis :
ribavirin
Neuroaminidase it’s enzyme that utilised it the virus to release from the cell, we can inhibit this enzyme by neuroaminidase inhibitors :
- Oselta-mivir.
- Zana-mivir
Drug of Choice to CMV :
Ganciclovir
Acy-clovir, famci-clovir, valacy-clovir this drugs use for
Viral dependent nucleosides :
1. HSV,
2. VZV,
3. Herpes zoster.
Why acyclovir have few adverse effects ?
Because it work only on infected cells
Drug of choice for HZV:
Famciclovir
Which drug have bitter oral bioavailability:
1. Acyclovir
2. Valacyclovir
Valacyclovir
Which antiviral therapy can cause obstructive crystalline nephropathy that may lead to acute renal failure ?
Acyclovir, famiclovir.valacyclovir
How to prevent the side effect that can develped after adminstration of acyclovir and other derivatives (obstructive crystalline nephropathy that may lead to acute renal faliure) ?
By good hydration
Amphotricin B can cause nephropathy, how we can treat this side effect ?
By good Hidration
Mutated of viral thymidine kinase lead to resistance of which drugs ?
Acyclovir and dervitaives
What’s the different between ganciclovir and val-ganciclovir ?
Valganciclovir have better bioavailability
Side effects of ganciclovir:
- Bone marrow supression
- Renal toxicity
Foscarnet mechanism of action
Direct inhibition of DNA\RNA polymerase , and HIV reverse transcriptase inhibitor.
CMV form resistance aginst ganciclovir by:
Mutated viral kinase
If CMV form resistance aginst ganciclovir, which drug we can use in the case ?
Foscarnet
Foscarnet clinical uses :
- CMV retinitis.
- Resistance of ganciclovir aginst CMV.
- Resistance of acyclovir aginst HSV.
Side effects of foscarnet :
- Nephrotoxicity
- Electrolytes abnormalitis “ hypokalemia, hypomagnesemia” that can lead to seizures
- Seizures ( by decrease Mg\ Na )
Mechanism of resistrance of foscarnet :
Mutated DNA polymerase
Cidofovir similar in mechanism and clinical uses with which antiviral drug ?
Foscarnet
Cidofovir better than foscarnet by :
- Long half life
- Does not cause electrolites abnormalitis like the foscarnet
Clinical uses of interferon beta :
Multiple sclerosis
Clinical uses of interferon gamma:
chronic granulomatus disease.
Which antiviral drug used in case of: chronic hepatits B,and C, kapsi sarcoma, hairy cell leukaemia, condylomata acuminata, renal cell carcinoma, malignant melanoma?
Interferon alpha
Hepatitis C therapy :
- Ledipasvir
- Ribavirin
- Sofos-bu-vir
- Sime-pre-vir
HCV protease inhibitor :
Sime-pre-vir
Viral phosphoprotein (NS5A) inhibitor. That used for HCV:
Ledi-pas-vir
Which anti-HCV inhibit synthesis of guanine nucleotides ?
Ribavirin
Which drug inhibit HCV RNA-dependent RNA polymerase ?
Sofos-bu-vir
MecA gene encoded of :
PBP-2a
Cell wall synthesis occur by two mechanisms :
- Peotidoglycan synthesis
- Peptidoglycan cross-linking
Peptidoglycan synthesis inhibitors :
Glycopeptides :
1. Vancomycin
2. Biucatricin
Peptidoglycan cross-linking inhibitors ( transpeptidase inhibitors )
- Penecillinase sensitive penicillin
- Penicillinase resistance penicillin
- Anti-pseudomonal
- Caphalosporins
- Carbapenems
- Monobactam
Ribosomes consist of :
- 50 s subunit (large subunit)
- 30 s subunit (small subunit)
Unasyn it’s combination between :
- Ampicillin
- Sulbactam
Augmintin it’s combination between:
- Amoxicillin
- Clavulenic acid
Otitis media cause by
H-influnza
Neonatal meningitis cause by :
Listeria
Tratment of neonatal meningitis :
Ampicillin
Patient in ventilation, infected by pneumonia, which bacteria cause this pneumonia and which drugs most used to treated it?
- Cause: pseudomonas,
- treatment 4’th generation of cephalosporins :”cefepime”.
Disulfiram- like reaction cause by inhibition of which enzyme ?
Acetyl dehyd dehydrogenase
Which drug from B- lactams antibiotics work as disulfiram ?
Caphaosporins
How cephalosporins cause Vit k deficiency ?
- By killing the bacteria flora that found in the intestine and responsible for production of vitamin K .
- By decrease the activation of vitamin K in liver by inhibition of Epoxide reductase enzyme .
Why to avoid to uses of warfarin with cephalosporins?
To prevent the severe deficiency of vitamin k, because the two drugs decrease the activity of vitamin k in the liver by inhibition of epoxide peroxidase.
The reason of contraindication of cephalosporins with aminoglycosides ?
Because the cephalosporine increase the risk of nephrotoxicity of amninoglucosides
What’s ESBL “extended spectrum B-lactamase:
It’s type of B-lactamase that resistance to most B-lactam antibiotics : penicillin cephalosporins, monobactam.
Which bacteria contains ESBL “extended spectrum B-lactamase:
Only gram (-) bacteria : KEEP-3S
1. Klibsella
2. E.coli
3. Enterobacter
4. Pseudomonas
5. Salmonella
6. Serratia
7. Shigella
Drug of choice for ESBL :
Carbapnems
Which drug used with imipneme to increase the half-life of the drug ?
Cilastatin
How the imipenem cause seizures ?
By inhibition of GABA receptors
Why. The monobactams effects only on gram negative bacteria ?
Because it bind to PBP-3 that found only in gram (-) bacgteria
What’s meaning of synergetic effect of the drugs ?
1+1=3
Which drug synergetic with monobactam ?
Aminoglycosides
Vancomycin it’s bacteriosidal aginst all of the bacteria except one bacteria work as bacteristatic :
C.diffice
Vancomycin used as IV except on case that used as oral, which case ?.
In case of pseudomembranous colitis that cause by c.difficile
How the red man syndrome occurs ?
When the doctor administrate the vancomycin to the patient rapidly
administration of amoxicillin to patient with EBV pharyngitis lead to :
Maculopapular rash
Why the aminogycosides are bactericidal ?
Due to miss-reading of mRNA
Neomycin clinical use:
- Bowel surgery .
- Hepatic encephalopathy
How the neomycin can treat the hepatic encephalopathy ?
Neomycin kill the gram (-) bacteria that located as normal flora in GIT-this bacteria produce amonia ,when neomycin kill this bacteria it lead to decrease production of amonia that cause hepatic encephalopathy
Plasmed encoded of transport pump, it’s cause resistance for tetracycline, by which mechanism ?
By decrease uptake of the drug and increase efflux out of the drug
Which drug inhibit peptidyltransferase ?
Chloramphenicol
Drug of choice of rocky-mountain spotted fever :
Doxycycline
Drug of choice of rocky-mountain spotted fever in case of pregnancy : (for 1’st and 2nd trimester only)
Chloramphenicol
Using of chloramphenicol after the 2nd trimester of pregnancy lead to
Gray- babe syndrome
Side effects of chloramphenicol
- Anemia
- Aplastic anemia
- Gray baby syndrome
Liver responsible for detoxification of chloramphenicol by which enzyme?
UDP-Glucoronyltransferase
Treatment of gray baby syndrome
- Stop the drug
- Exchange transfusion phenobarbital (enzyme inducer- increase UDP-Glucoronyltransferase)
Which drug inactivate by acyl-transferase enzyme than encoded by plasmid ?
Chloramphenicol
Treatment of anaerobic bacteria above the diaphragm :
Clindamycin
Treatment of anaerobic bacteria below the diaphragm :
Metronidazole
Initial complex inhibitors :
- Aminoglycoside :by bind to 30s
- Linezolid : by bind to 50s
Which syndrome characterised by : fever, confusion, agitation, hyperrflexia?
Serotonin syndrome
Antimicrobial drugs that inhibit translocation
- Macrolide
- Clindamycin
Which antimicrobial drug use for gastropariesis “GI motility disorders “
Erythromycin
Combination between Quinupristin and Dalfopristin =
Syner-cid
For simple UTI we use :
Sulfamethoxazole
Using of sulfonamide for new-born lead to
Kernicterus
To long duration of penicillin, we administration it in combination with :
Probenecid
Mechanism of Antifungal therapy: “
- Protein synthesis inhibitor
- Nucleic acid synthesis inhibitor
- Lanosterol synthesis inhibitor
- Ergosterol synthesis inhibitor ( inhibit the enzyme, or formation of membrane pores )
Which enzyme inhibit by azoles ?
14-alpha-demethylase (cytochrome p-450)
Candida infection therapy : (1st, 2nd, 3rd lines )
- 1st line : fluconazoles
- 2nd line : echinocandins
- 3rd line amphotrisin B
Which two drug that use for dermatophysis ?
- Teribuinafine
- Griseofulvin
Which anti fungal drug deposit in keratin-containing tissue. ?
Grieseofulvin
Microtubule inhibitors : in fungal , in human, in protozoa ?
- In fungal : griseofulvin
- In protozoa : mebendazole
- In human : anti-cancer therapy : paclitaxil, vincristine
Mechanism of anti-malarial therapy :
block detoxification of heme into hemozin
Which anti-fungal therapy characterised by the following side effects: teratogenic, carcinogenic, disulfram like reaction, decrease cytochrome p-450
Griseofulvin
The main mechanisms of HIV therapy
- Fusion inhibitors
- Reverse transcriptase inhibitor
- Integrase inhibitor
- Protease inhibitor
Side effect of integrase inhibitor of HIV :
Myopathy
Side effect of protease inhibitors of HIV
Metabolic complications :
1. Lipodystrophy
2. Dyslipidemia
3. Insulin resistance
Monophosphorylation of acyclovir by :
Thymidine kinase (viral kinase )
Monophosphorylation of ganciclovir by
CMV viral kinase
Which virus conatins thymidine kinase ?
HSV, VZV
Side effects of acyclovir
- Obstruction crystalline nephropathy
- Acute renal failure
Side effects of ganciclovir
- Bone marrow suppression
- Renal toxicity
Mechanism of ribavirin
Inhibit inosine monophosphate dehydrogenase, that convert IMP to GMP
Initial complex consist of
- 50s
- 30s
- mRNA
- Initiator tRNA
Peptide bond that connects the two tRNA formed by
Peptidyltransferase
TMP-SMX mechanism :
Sequentially block of folic acid synthesis
What’s kernicterus
Newborn have physiological jaundice that characterised by high level of bilirubin, bilirubin bind to albumin to prevent the penetration the BBB, using of sulfonamide lead to bind of the drug to albumin, therefore the bilibrubin will be free in the blood and it will pass BBB and deposit in basal ganglia and cause kernicterus
Which drug may cause hemolysis in case of G6PD deficiency
- Dapsone
- Sulfonamide
Triple therapy of H.pylori
- Clarithromycin
- PPI
- Amoxicillin or metronidazole
Treatment of megaloblastic anemia that cause by trimephorime ?
Folonic acid ( that convert to tetrahydrofloic acid with out dihydrofloate reductase
Drug of choice to atypical (chlamydia, mycoplasma) :
Macrolide
Drug of choice to listeria (neonatal meningitis ):
Ampicillin + gentamycin
Drug of choice to meningitis
Ceftriaxon
Drug of choice to pseudomonas
- Cefepime
- Ceftazidim,
Drug of choice to ESBL
Carbapenems
Which antimicrobial drugs may cause disulfram like reaction
- Metronidazole
- Cephalosporins
- Griseofulvin
Which antimicrobial drug may cause metallic test
- Metronidazole
- Terbinafine
Prophylaxis of meningitis
Rifampin
Drug of choice for atypical pneumonia
Azithromycin
Treatment of gonorrhea infection
Azithromycin + ceftriaxone
Daptomycin inactivate by
Pulmonary surfactant