pharmacology Flashcards

1
Q

important points regarding AMA on cell wall

A

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

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2
Q

extended spectrum penicillin’s spectrum of action

A

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)

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3
Q

prodrugs of ampicillin

A

better oral absorption (BPT)
1)Bac A
2)Piva A
3)Tal A

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4
Q

uses of penicillin (SMART GAYLES PH) QQ

A

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

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5
Q

infection ass. with severe allergic reaction if penicillin used

A

EBV

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6
Q

ampicillin is DoC in what conditions(2)

A

1)listeria meningitis
2)Enterococcus fecalis(not fecium)
also used in H influenza (doc-ceftriaxone)

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7
Q

DoC for surgical prophylaxis

A

Cefazolin(1st gen cephalo) given 30-60 min before skin incision since its effective against GPC (present on skin surface)

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8
Q

uses of different generation of cephalosporin

A

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

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9
Q

what is cephamycin its use and side effects

A

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

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10
Q

enumerate anti pseudomonal cephalo

A

1) cefoperazone
2)moxalactam
3)cefotolazane
4) ceftazidime
5)cefidercol

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11
Q

infections against which cephalo dont work(LAME)

A

listeria
atypical bacteria
MRSA(except 5th gen)
Enterococcus

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12
Q

2nd gen B lactamase names ,drugs combined with and use

A

+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

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13
Q

how to prevent vancomycin induced red man syndrome

A

since caused by fast injection which leads to histamine release causing flushing and hypotension
1) slow injection
2) given with Anti histaminics

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14
Q

cell membrane inhibitors,uses,forms s/e and limitations

A

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

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15
Q

Vancomycin uses in different forms
enumerate lipoglycopeptides
longest acting glycopeptide
iv im both form
S/E

A

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

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16
Q

Drugs acting on fungal cell wall and their uses+ S/E

A

+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

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17
Q

Allyamines drugs use and se

A

+ inhibit squalene epoxide
1)Terbenafine
2) Butenafine
3)naftifine
+Use - topical for tinea onychomycosis (dermatophyte toe nail infection)
+ S/E -Hepatotoxic
SJS

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18
Q

Antifungals which are DOC in different infections and certain special drugs for special situations(14)

A

+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

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19
Q

Special features and side-effect of different azoles(4)

A

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

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20
Q

Formulation and S/E of AMB

A

+ 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

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21
Q

Side-effect of griseofulvin

A

Most common= headache
Special = disulfiram like reaction= avoided in alcoholic
Other = hepatotoxicity
It is enzyme inducer

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22
Q

Banned (6)and new FQ

A

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

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23
Q

Mechanism of resistance to different AMA(10)

A

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

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24
Q

+Broad spectrum protein synthesis inhibitors(4)
+ Bacteriocidal
+Drugs on 30s
+drugs inhibiting translocation
+ drugs inhibiting initiation

A

+CTCT
Clindamycin, tetracycline,tigecycline, chloramphenicol

+ Aminoglycosides, streptogramins

+ aminoglycosides, tetracycline,Tigecycline

+ MCQ =Macrolides, clindamycin, Quinpristin

+Linezolid , AG

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25
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
26
Treatment of gonorrhoea
1st line = Ceftraxone 500 mg im once +If N/A = Gentamycin im + oral azithro (2gm ) once + If resistance to ceftriaxone- Spectinomycin used
27
Special aminoglycosides features and drugs(11)
1) only on 30s = streptomycin and spectinomycin 2)No resistance = Amikacin and plazomycin 3)Not effective against = BATA = Burkholderia , acinetobacter , typhoid, anaerobes(since enter via 02 dependent porin) 4) streptomycin- PTT = Plague , Tularemia , TB 5) antitubercular = SACK = streptomycin, amikacin,capreomycin , kanamycin 6)anti pseudomonas - TAG = tobramycin, Amikacin,Gentamycin(also available as eyedrops and inhalational) 7) Arbekacin- MRSA 8)Gentamycin- combined with drugs on cell wall 9) Paramomycin- Protozoal infection = Kala azar and luminal amoebiasis 10) Framycetin and neomycin = creams 11) oral neomycin= Hepatic encephalopathy
28
Special features of linezolid (5)
1) 100% oral bioavailability 2) bacteriocidal for pneumococcus but bacteriostatic for MRSA,VRSA,VRE,MDR TB 3) narrow spectrum 4) renal safe 5) side-effects: COMB =chorioretinitis , optic neuritis,MAO inhibitor- serotonin syndrome, bone marrow suppression- measure platelets - less with Tedi and sutezolid.
29
Misc topical AMA
1) Mupirocin 2% cream = inhibit ITR = isoleucine T RNA synthetase 2) fusidic acid = inhibit elongation factor=impetigo(staph and strepto) 3)Retapamulin ] Inhibit peptidyl transferase = impetigo Lefamulin. ] Same = MRSA
30
+Uses of co-trimoxazole(Beer PINT CUP) + Double strength cotrimaxazole
Burkholderia Pneumocystis Isospora Nocardia Traveller’s diarrhoea Typhoid prophylaxis Cystitis, UTI, prostatitis + Sulpha 800 mg with 160 mg trimethoprim
31
Classification of sulphonamides(4)
1) systemic i) long acting (>12hrs)=sulfadoxine ii) intermediate acting(8-12 hrs) = sulphamethaxazole iii) short acting= sufacytine > sulfadiazine iv) most water soluble= least crystalluria=sulfisoxazole 2) Topical cream= silver sulphasalazine 1% and mafenide = burns 3) topical eyedrops= “. “. 10% and sulfacetamide= fungal keratitis 4) topical oral = for ulcerative colitis= sulfasalazine olsalazine mesalazine
32
+AMA classification based on properties(4) + forms of resistance(4) + safe in renal failure (RENAL PMT DIC)
+ 1) CDK with Long PAE = MARS = metronidazole, aminoglycosides,rifampcin,streptogramins(longest pae) 2)CTDK with Long PAE = DaFQ =daptomycin , FQ 3) TDK with Long PAE = AT = Azithromycin, tetracycline 4)TDK with Short PAE =CPEC =cephalosporin , penicillin, erythromycin, clindamycin + 1)drug dec. influx = Carbapenem in pseudomonas 2) drug efflux = p-gp = tetracycline,Tigecycline , chloroquine 3) enzymatic degradation= ABC = AG , beta lactams , Chloramphenicol 4) target mutation= decreased binding = MFM= macrolides, FQ, MRSA(PBP2a) + safe in RF =rifampcin ,erythromycin,naficillin, amoxicillin,linezolid, peF , MoxiF,TrovaF,Doxycycline,INH,Cefoperazone
33
Genes associated with resistance to antitubercular drugs
1)Isoniazid = KATg > InhA and KasA 2) Rifampcin = rpoB 3) Pyrazinamide = pncA > rbps1 and PAN D 4) ethambutol = embAB
34
+ATT with sterilisation action +ATT with fastest killing and decreasing infectivity + drug a/w hypothyroidism +requiring vit B6 p/0 +a/w optic neuritis +requiring platelet monitoring +a/w QT prolongation + used in MAC
+Rifampcin> pyrazinamide > bedaquiline +Isoniazid + ethionamide>PAS +ICE= Inh cycloserine and ethambutol +Ethambutol and Linezolid +Linezolid +Bedaquiline and delamanid + Rifabutin(not mpcin) ,Ethambutol strepto and Levo
35
+2 nd line drugs for leprosy + uses of dapsone +MoA dapsine
+COME= clarithro,Ofloxacin,Minocycline,ethionamide + Leave PMT Day= Leprosy , Pneumocystis , madura foot,Toxoplasma, Dermatitis herpatiformis + sulphonamide= - folate synthase
36
+Co receptor inhibitors in HIV +Inj 2nd line and only in HIV 1
+1) ccr5 = Maraviroc 2)ccr2 and 5= Cenicriviroc +Enfuvirtide = fusion inhibitor Ibalizumab= Cd4 —
37
+Specific side effects of specific NRTIs + working only on Hiv 1 + safest overall and its cross resitance
+1) Didanosine = pancreatitis 2)Zidovudine= BOMA= BM suppression,Optic neuritis,Myopathy,Alopecia 3)Stavudine =SLAP= Steatosis , Lipodystrophy syndrome , Acidosis(lactic) , Peripheral Neuropathy + Abacavir- also preferred in children but shows rash in HLA B5701 pt +Lamivudine cross with emtricitabine d/t M184V mutation
38
Nevirapine vs Efavirenz
Nevirapine= CYP3A4 substrate = rifampcin dec.its concentration and also a/w Hepatotoxicity Efavirenz=no cyp3a4 interaction = given with rifampcin but a/w neurotoxicity Also the most preferred drug in pregnancy
39
Special features of different protease inhibitors
1)common = m/c is GI abN but most specific= LDS 2) least LDS = atazanavir = max bilirubin increase 3) Tipranavir = ICH 4)Indinavir = renal stones 5)Saquinavir= QT prolongation 6) CYP interaction = max ritonavir and least Nelfinavir
40
New drugs of HCV New drugs for CMV
1) anti sense oligonucleotide= Miraversin(HCV ) and Fomiversin (CMV) 2) Cyclophillin A inhibtor = (HCV)Alispovir(cyclosporin also bind to Cyclophillin) 3)Terminal complex inhibitor = (CMV)Letermovir
41
+ Special s/e of luminal amoebicidal +SE of emitene + SE of pentamidine Se Sodium stibogluconate
1) Diloxanide = Flatulence 2)Iodoquinol= HypoT3 ( iodo) and Angioedema 3) Quindachlor = SMON (subacute myelo optic neuritis) + a/w vomiting and Cardiotoxic + a/w hypoglycaemia and HTN initially but later Hyperglycaemia (pancreatic damage) + QT prolongation , Pancreatitis and Nephrotixic
42
+Primaquine action on which stages + other pre erythrocytic drugs + vivax hypnozoite specific drug + doc P/O of malaria
+acts on all except erythrocytic stage and sporozoites(no drug against it) + Proguanil and Doxycycline + Tafenoquine +Mefloquine 250 mg once/wk >>Doxycyline 100mg/day(CQ= widespread resistance)
43
Drugs safe in malaria in pregnancy
+ Quinine and Clindamycin for falciparum and Chloroquine for vivax and ovale + ACT only in 2nd and 3rd trimesters + No radical cure in pregnancy since primaquine is C/I + But in complicated = life saving is iv artesunate
44
+Anti-cancer drug, which don’t cause bone marrow suppression(VBAC) + G csf and GM CSF drug + Keratinocyte growth factor my humour + auntie drugs associated with secondary cancer(EMPC)= cat D s/e
+vincristine bleomycin asparaginase and chlorambucil +Filgrastim and Molgramostim + Palifermin = used for mucus ulcers +Etoposide = early ca (<3 yrs) Mitoxantrone = AML M3 Procarbazine = max carcinogenic Cisplatin = late ca(>4yrs)
45
+MoA of CCNS drugs + Cell cycle specific anticancer drugs(PEAS HATE BED VITC) +drug acting on 3 phases
+bind to N7 guanine causing cross linking of DNA either by alkyl group or by platinum +1) G1= Palbocitinib , Etoposide , asparaginase and steroids 2)S ( Dna synthesis) = Hydroxyurea , Anti metabolites , Topetecan , Etoposide 3)G2 = Bleomycin , Etoposide , Doxorubicin 4)M(microtubule inhibitor)=Vincristine , Ixabiplone , Taxanes and Colchicine + Etoposide
46
+Classification of alkalyting agent + Drugs in each class
+1) nitrogen mustard 2)Nitrosamines 3) miscellaneous +1) nitrogen mustard = MCI MC = Mechlorethamine, Cyclophosphamide, Iphosphamide,Melphalan , Chlorombucil 2) Nitrosureas = Se Lo and Car mustine 3) Misc= BAD TTP = Busulfan , Altretamine , Dacarbazine and Procarbazine , Thiotepa and Temozolamide +Antibiotics with Alkylating agent action =MS = Mitomycin C , Streptozotocin
47
Uses and S/E of cyclophopamide and its uses
+BONBS WARS = burkitt lymphoma , Ovarian cancer ,NHL ,Breast Ca , Solid tu (neuroblastoma) Wegner , Acute cerbral vasculitis,RA, Steroid dependent nephrotic syndrome + breakdown = acrolein= Hhagic cystitis = bladder ca Mx= MESNA(iv for Rx and oral for PO) Ifosphamide is even more a/w H'hagic cystitis and also with neurotoxicity which requires methylene blue
48
+ features of 1) melphalan 2) chlorambucil
1)Mephalan(3M) = Max marrow suppression along with busulfan , used in myeloablation and for Multiple Myeloma 2) Chlorambucil - targets mature lymphocytes = used in CLL and least BM suppression , least emitogenic
49
special features of busulfan (6 s/e)
kills myelocytes = AML AND CML Spares lymphocytes S/E- i) Busulfan lung ii) BM suppression iii)Vaso occlusive disease = defibriotide iv) Neurotoxicity= seizures = need phenytoin v)Tumor lysis syndrome vi) cataract
50
+Procarbazine use and its replacement S/E +Temozolamide +thiotepa +Altretamine
was used in MOPP regimen of HL = Now ABVD with dacarbazine (also in Melanoma) s/e- i) infertility =ii) depression = iii) Disulfiram reaction +Temozolamide = good csf penetration= DoC astrocytoma and malignant gliomas +Thiotepa= OP = myeloablation +Altretamine = platinum resitant ovarian cancer
51
Nitrosoureas use and s/e
+astrocytomas resitant to temozolamide +BM suppression= Neutropenia -single dose = prolonged suppression
52
+pump responsible for entry and resitance to platinum compounds + drug specific side effects +management of nephrotoxicity
+copper transporter + Max emitogenic , nephrotoxic,ototoxic = Cisplatin Max Neurotoxicity= oxaliplatin Least s/e= Carboplatin + nephrotoxicity =ATN = decrease K Mg and Ca i) slow infusion of drug ii) adequate hydration iii) Mannitol to excrete and chloride to neutralise platin iv)Amifostine = nephro and radioprotector
53
uses of platins in cancers(LOGHUR)
Lung ca, Osteosarcoma ,Gi cancer(with 5 FU),Head and neck ca,Urogenital(testis,ovary, cervical),Retinoblastoma , Radiosensitiser
54
anti cancer Drugs on S phase and their mechanism of action
1) Hydroxyurea= Ribonucleotide reductase inhibitor ( no dUMP or other deoxy products)+inc HbF + Radiosensitiser= used in SCA and MPD except CML 2) Antimetabolites = competitive inhibition by mimicking molecules required for DNA synthesis= Folate/purine and pyrimidine analogues
55
s/e of hydroxyurea
skin pigmentation and painful skin ulcers
56
Uses and antidote of different folate analogues
1) Mtx= COMB All My Hairs Or People Will SCREAM antidote = folinic acid--->glucarpidase(enzyme)--->forced alkaline diuresis 2) Pemetrexed = mesothelioma (with 5FU)= folic acid and B12 3)Pralitrexate = Peripheral T cell leukemia = folic acid and vit B12 4) Trimetrexate= pneumocystis infection 1) inhibit THFR >TK and ADA 2,3,4= Thymidylate kinase
57
Resistance mech and se of Mtx
+resistance= 1) upregulation of DHFR 2)Decreased influx and inc. efflux 3)less polyglutamates formation +S/E= 1) GI mucous ulcers = Diarrhoea 2) Megaloblastic anemia 3)Hepatotoxicity 4) crystalluria 5)ILD So we do CBC LFT and CXR regularly +C/I= pregnancy (NTD) and lactation
58
Classification enumeration and uses of purine analogues
1) GUANINE ANALOGUES = A ) 6 Thioguanine B) 6 Mercaptopurine = Azathioprine Inhibit HGPRTase = Used in Resistant Lymphomas and organ Trx S/e= BM suppression and hepatotoxicity M= i) oral = XO ii) iv = TPMT ———> so with allopurinol = dose reduction by 75% 2)ADENINE ANALOGUES = A) Fludarabine = CLL(FCR) B) Cladribine = Histiocytosis , Hairy cell leukemia C) Pentostatin = - ADA = used in resistant a and b S/E= immunosuppressiom = Pneumocystis infection = Cotrimoxazole p/o
59
Classification, enumeration of pyrimidine analogues.
1)URACIL ANALOGUES A) 5 FU = inhibit thymidylate synthase —>co factor = folinic acid —> together increase efficacy M= DPD = c/i in its deficiency Uses= HBG BMS = Head and neck, Breast and GI cancer , Bcc , Mycosis fungoides , Solar keratosis S/E = i)mucous ulcers = fulminant diarrhoea ii) Palmoplantar erythro dysesthesia B) Capecitabine = oral form of 5 FU C)FloxUridine = hepatic Metastatic CRC via Hepatic A. 2) URACIL ANALOGUES A) Gemcitabine = radiosensitiser for Pancreatic cancer B) Cytosine arabinoside /Cytarabine = AML(intrathecal)—>Cerebellar toxicity C) Azacytidine and Decitabine = -Methylation of DNA = use in MDS
60
+Microtubule inhibitors classification and other drugs with similar actions + S/E and Uses
+1)Vinca = i)Vincristine(oncovin) = max neurotoxicity and least BM suppression ii) Vinblastine = Max BM suppression and least Neurotoxicity Used in Blood cancers= AML ,HL,NHL,ALL (not in solid tumors) iii) Eribuline = taxane like action = Breast Cancer 2)Taxanes = i) Paclitaxel = hepatic excretion ii) Docetaxel = renal excretion, iii) Cabazitaxel Use= i)hormone resistant breast and prostrate cancer ii) Paclitaxel = Drug Eluting Stents iv) Ixabiplone = taxane like = in breast cancer v)Estramustine = taxane + estrogen like = prostrate ca vi) Colchicine = taxane like = - wbc migration = acute gouty attack S/E = since MT needed for NT movement, lead to i) neurotox = vinka : Foot drop and taxane : Glove stock Neuropathy ii) paralytic ileus iii) SIADH = vincristine max
61
topoisomerase inhibitors , uses and drugs with similar action
1) TOP 1 inhibitors= camptothecins i)topotecan ii) Irinotecan = SN38 by metabolism via UDP GT = C/I CNS And Gilbert syndrome also = anti AchE = inc. Ach = diarrhoea = Rx -->Loperamide 2)TOP 2 inhibitors = Epipododoxophyllin i)Etoposide = BEP and RCHEOP regimen ii)Teniposide Other drugs with similar action (antibiotics) i) Anthracyclines ii)Mitoxantrone
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Antibiotics as anti cancers(MBA MSD Play)
1)Anthracylines (-rubicin ) = 4 reds i)Doxo= max cardiotoxic ii)Ida= least iii) red -flare,urine,drug soln,Rediation recall syndrome Use= all ca like breast and bladder 2)Mitoxantrone = MAP = MS , AML , Prostrate ca mets l/t AML M3 3)Streptozotocin = doc insulinoma 4)Mitomycin C = i)intravesical for bladder ca ii) kills fibroblasts= dec. post injury fibrosis and scarring s/e= Hus TTP 5) BLEOMYCIN= oxidative DNA damage +rapid degradation d/t Hydrolase = No BM supp. Use= HL , Testicular ca S/E = no hydrolase in - i) Lungs = Fibrosis -->kills type 1 pneumocytes = decrease DLCO ii) skin = FIR= Flagellate pigmentation , Icthyosis , Raynaud phenomenon 6)Actinomycin D /dactomycin = Dna transcription inhibitor RDW= i) Rhabdomyosarcoma ii)Wilms tumor s/e= i) SIADH ii) Radiation recall syndrome 7) plica/mithramycin= kill osteoclasts (not used now)
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1)enzyme as anti ca drug 2) Vitamin as anti cancer drug 3)Metals as anti cancer drug
1)L asparaginase = protein breakdown esp. in lymphocytes = VPAD regimen of ALL +S/E= break body proteins too 2)ATRA= + Retinoic acid Receptor = maturn/differentiation of cancer cells = death of ca cells = used in APML also used in acne s/e= i) since fat sol. vit = metabolic syndrome ii) since rapid lympho maturn = go to lungs = ARDS= Retinoic acid / Leukocyte maturn syndrome iii) amenorrhea and infertility iv) teratogenic drug = preg. C/I v) vit A = Pseudotumor cerebrii 3) platinum and arsenic + AS203= resistant APML S/E= i) Mees line ii) QT prolongation