pharmacology Flashcards
important points regarding AMA on cell wall
1)dont work on atypical bacteria
2)all cidal except cycloserine(static)
3)bacitracin iv - nephro and neurotoxic
4)cycloserine l/t neuropsychosis ( more seizures and suicides)
5)fosfomycin is given 3 gm orally for UTI in all irrespective of age and weight
extended spectrum penicillin’s spectrum of action
only penicillin against enterobactericiae
1)amino= only against E coli,salmonella,shigella and H influenza(doc is ceftriaxone)
2)carboxy- works against pseudomonas and proteus vulgaris as well
3) ureido- also against P mirabilis and klebsiella (carboxy doesnt)
prodrugs of ampicillin
better oral absorption (BPT)
1)Bac A
2)Piva A
3)Tal A
uses of penicillin (SMART GAYLES PH) QQ
1)Syphilis
2)meningiococcal meningitis(doc-ceftriaxone)
3)actinomycosis
4)Rat bite fever(spirillum)
5)Tetanus
6)Gas gangrene
7)Anthrax
8)Yaws(T. perteneu)
9)Leptospirosis
10)Every species of Strept and Staph
11)Pasturella
12) Human bite
infection ass. with severe allergic reaction if penicillin used
EBV
ampicillin is DoC in what conditions(2)
1)listeria meningitis
2)Enterococcus fecalis(not fecium)
also used in H influenza (doc-ceftriaxone)
DoC for surgical prophylaxis
Cefazolin(1st gen cephalo) given 30-60 min before skin incision since its effective against GPC (present on skin surface)
uses of different generation of cephalosporin
1st gen- gram positive (B lactamase resistant)
2nd gen - Anaerobes >gram + and -
3rd gen- serious gram -ve infections»>gram +ve but not against Anaerobes
4th gen- Pseudomonas and other gram -ve resistant to 3rd gen (nosocomial infections)it is also B lactamase resistant
5th gen- against resistant S aureus(mrsa,vrsa,lrsa)it is not B lactamase resitant neither does it work against pseudomonas
what is cephamycin its use and side effects
1) 2nd gen cephalo including
M- cefometazole
T-cefotetan
X-cefoxitin
are k/a cephamycin
2) used against B fragilis
3) along with cefoperazone , these contain MTT ring which is responsible for causing Disulfiram like reaction and also associated with ⬇️ fibrin = warfarin toxicity
enumerate anti pseudomonal cephalo
1) cefoperazone
2)moxalactam
3)cefotolazane
4) ceftazidime
5)cefidercol
infections against which cephalo dont work(LAME)
listeria
atypical bacteria
MRSA(except 5th gen)
Enterococcus
2nd gen B lactamase names ,drugs combined with and use
+used for MBL(metallo B lactamase ) producing E coli and Acenetobacter which are carbapenem resitant
+Normally Carbapenem are DoC for ESBL(extended spectrum B lactamase)
3 drugs are considered 2nd gen and are used with
1) avibactam with ceftazidime
2)Relebactam with imipenem
3)Vaborbactam with Meropenem
how to prevent vancomycin induced red man syndrome
since caused by fast injection which leads to histamine release causing flushing and hypotension
1) slow injection
2) given with Anti histaminics
cell membrane inhibitors,uses,forms s/e and limitations
1) lipopeptide-daptomycin
+ works again gram positive organisms
+MoA-detergent like action= depolarisn and death
+uses- i) MRSA,VRSA Except pneumonia
ii) VRE
+S/E-myopathy
2) POLYPEPTIDE-i) polymixin B
ii) polymixin E(colistin)
+for gram negative specially carbapenem resistant.
+cream-colistin sulphate
+Iv-cholisthetamate sodium
S/E -neuro and nephrotixic
+no use- BSP
burkholderia,serratia,proteus
note - these are cidal and never given oral
Vancomycin uses in different forms
enumerate lipoglycopeptides
longest acting glycopeptide
iv im both form
S/E
1) oral=
i) PMC
ii)S enterocolitis
2)parentral=
i) MRSA
ii)MRSE
iii)TSS - given with clindamycin
+3 drugs - Dalbavancin, Telavancin,Oritavancin
+longest= Dalbavancin
+ iv/im both- Teicoplanin
+S/E- nephro and ototoxic
Red man syndrome
Drugs acting on fungal cell wall and their uses+ S/E
+Echinocandins (- 1,3 BD glucan synthase)
1)Caspofungin
2)Anidulafungin
3)Micafungin
+USES-
1)Iv drug as p/o to prevent deep candidiasis and aspergillosis in I/c patient
2) micafungin as part of p/o of I/c pt along with posaconazole and fluconazole
+ SE-
1) Hepatotoxic but renal safe
Allyamines drugs use and se
+ inhibit squalene epoxide
1)Terbenafine
2) Butenafine
3)naftifine
+Use - topical for tinea onychomycosis (dermatophyte toe nail infection)
+ S/E -Hepatotoxic
SJS
Antifungals which are DOC in different infections and certain special drugs for special situations(14)
+AMB is the DOC in most infections but due to S/E , used mostly for only induction therapy followed by other drugs in maintainance.
1) Ketoconazole- topical shampoo for dandruff (seborrhic dermatitis)
2) Fluconazole (3C)- DoC for coccidiodes (better than AMB)
DoC for non serious candida and cryptococcal non meningitis
( For invasive candida and crypto = AMB)
3)Itraconazole -
i)Doc - Mycetoma and pseudo allerechia
ii)Maintainance of all dimorphic fungi except coccidiodes (flu)
4) Voriconazole
i)DOC - aspergillosis (better than AMB)
ii) Maintainance for moulds like rhizopus,scedosporium ,cladospora
+ not for mucor mycosis = isavuconazole and posaconazole
5)AMB- all except the above rare it is DOC
Also DoC for parasites- Kala azar and naeglaria
6) Nystatin(5%)- paint/ lotion for oral candidiasis
7)Natamycin- eye drops for fungal keratitis
8)clotrimazole- pessary for vaginal candidiasis
9)Efinaconazole- candida onychomycosis
10)Sertaconazole- anti pruritic and anti inflammatory
11)Griseofulvin- topical for Tinea capitis
12)5 Flucytosine- Add on with AMB for synergistic effect against cryptococcal meningitis
13)Nail laquer for onychomycosis- ciclopirox olamine and amorolfine
14) whitefield ointment - Benzoic acid(fungicidal) with salicylic acid(keratolytic) w
Special features and side-effect of different azoles(4)
All are fungistatic drugs ( griseo also static)
1) Ketoconazole -
i)Max cyp enzyme inhibitor (keto>Vori>Itra)(griseo is enzyme inducer)
ii) systemic use is dangerous so replaced by Itraconazole
iii) Max hepatotoxicity(Least fluconazole since no bile excretion)
iv) inhibit steroid synthesis= gynaecomastia, infertility, adrenal insufficiency( decreased test., GC,MC)
2)Fluconazole-
i) maximum CSF penetration(doc coccidiodes meningitis)
ii) only azole contraindicated in renal failure(excreted in urine)
iii) contraindicated in pregnancy- TOF
iv) Side effect – reversible alopecia
3)Itraconazole- long-term uses associated with:
i) skin cancer (SCC)
ii) hypertension(CHF)
4) voriconazole-
i) QT prolongation(also with posaconazole)
ii) visual disturbance
iii) since contains fluoride = fluorosis
Formulation and S/E of AMB
+ obtained S. nodosus
i) AMB - DOC(c amb) = deoxycholate = Max nephrotoxic but m/c in india
ii) AMB - CD= colloidal dispersion = max allergic reaction
iii)AMB-LC= lipid complex
iv)L AMB = liposomal= safest and longest
S/E-
i) allergy – infusion reaction= due to bacterial source. -subside with time=pre medication with steroids NSAIDS and antihistaminic
ii)azotemia-renal tubular acidosis= decreased potassium and magnesium= arrhythmia
So we give adequate hydration(2 L NS) before starting AMB and keep monitoring electrolytes
iii) anaemia-Normocytic hypochromic= decreased Ep from kidney
iv)Arachnoiditis-Intrathecal injection-prevention by steroids
Side-effect of griseofulvin
Most common= headache
Special = disulfiram like reaction= avoided in alcoholic
Other = hepatotoxicity
It is enzyme inducer
Banned (6)and new FQ
Gati– hypoglycaemia( approved in India for MDRTB)
Trova-hepatotoxicity
Tema-haemolytic anaemia
Grepa-QT prolongation
Clina-photosensitivity
Lome-both QT and photosensitivity
But max photosensitivity and QT prolongation with spar= longest acting
Newer-
i)Delafloxacin - MRSA
ii) Neo and ozenoxin- non-fluorinated quinalones
Mechanism of resistance to different AMA(10)
1) B lactams - B lactamase production or transpeptidase mutation (PBP2A)
2)Daptomycin - surfactant in lungs
3)Nitroimidazoles - NIM gene = NIM reductase = neutralise
4) FQ- Mutation in dna gyrase/TOP4 = decreased binding
5)Nitrofurantoin-urine with alkaline pH(proteus)
6)Chloramphenicol- enzymatic degradation by CAT( Chloramphenicol acetyl transferase)
7)Tetracycline - P gp efflux pumps (porins)
8) Tigecycline - similar to tetra
9)Macrolides- mutation in 50s = dec. binding
10) Aminoglycosides - enzymatic degradation by i)AGAT(acetyl) ii)AGPT(phosphoryl)iii)AGNT(nucleotide) No resitance in Amika and Plazomycin
+Broad spectrum protein synthesis inhibitors(4)
+ Bacteriocidal
+Drugs on 30s
+drugs inhibiting translocation
+ drugs inhibiting initiation
+CTCT
Clindamycin, tetracycline,tigecycline, chloramphenicol
+ Aminoglycosides, streptogramins
+ aminoglycosides, tetracycline,Tigecycline
+ MCQ =Macrolides, clindamycin, Quinpristin
+Linezolid , AG
Uses of different tetracycline(6)
1) tetracycline- i) P/O of cholera. ii) peptic ulcer
2)Demeclocycline -i) chronic SIADH
3)Minocycline - i) Acne ii) Leprosy
4) doxycycline- ABC BPL MRP
5) omadacycline and Eravacycline - HAI = skin and soft tissue , intra- abdominal and CAP
[same use for Tigecycline sp. for MRSA and Acinetobacter]
6)Sarecycline - severe acne