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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

prodrugs of ampicillin

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

infection ass. with severe allergic reaction if penicillin used

A

EBV

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

enumerate anti pseudomonal cephalo

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

infections against which cephalo dont work(LAME)

A

listeria
atypical bacteria
MRSA(except 5th gen)
Enterococcus

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Side-effect of griseofulvin

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Uses of different tetracycline(6)

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Treatment of gonorrhoea

A

1st line = Ceftraxone 500 mg im once
+If N/A = Gentamycin im + oral azithro (2gm ) once
+ If resistance to ceftriaxone- Spectinomycin used

27
Q

Special aminoglycosides features and drugs(11)

A

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
Q

Special features of linezolid (5)

A

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
Q

Misc topical AMA

A

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
Q

+Uses of co-trimoxazole(Beer PINT CUP)
+ Double strength cotrimaxazole

A

Burkholderia
Pneumocystis
Isospora
Nocardia
Traveller’s diarrhoea
Typhoid prophylaxis
Cystitis, UTI, prostatitis

+ Sulpha 800 mg with 160 mg trimethoprim

31
Q

Classification of sulphonamides(4)

A

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
Q

+AMA classification based on properties(4)
+ forms of resistance(4)
+ safe in renal failure (RENAL PMT DIC)

A

+ 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
Q

Genes associated with resistance to antitubercular drugs

A

1)Isoniazid = KATg > InhA and KasA
2) Rifampcin = rpoB
3) Pyrazinamide = pncA > rbps1 and PAN D
4) ethambutol = embAB

34
Q

+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

A

+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
Q

+2 nd line drugs for leprosy
+ uses of dapsone
+MoA dapsine

A

+COME= clarithro,Ofloxacin,Minocycline,ethionamide
+ Leave PMT Day= Leprosy , Pneumocystis , madura foot,Toxoplasma, Dermatitis herpatiformis
+ sulphonamide= - folate synthase

36
Q

+Co receptor inhibitors in HIV
+Inj 2nd line and only in HIV 1

A

+1) ccr5 = Maraviroc
2)ccr2 and 5= Cenicriviroc
+Enfuvirtide = fusion inhibitor
Ibalizumab= Cd4 —

37
Q

+Specific side effects of specific NRTIs
+ working only on Hiv 1
+ safest overall and its cross resitance

A

+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
Q

Nevirapine vs Efavirenz

A

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
Q

Special features of different protease inhibitors

A

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
Q

New drugs of HCV
New drugs for CMV

A

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
Q

+ Special s/e of luminal amoebicidal
+SE of emitene
+ SE of pentamidine
Se Sodium stibogluconate

A

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
Q

+Primaquine action on which stages
+ other pre erythrocytic drugs
+ vivax hypnozoite specific drug
+ doc P/O of malaria

A

+acts on all except erythrocytic stage and sporozoites(no drug against it)
+ Proguanil and Doxycycline
+ Tafenoquine
+Mefloquine 250 mg once/wk&raquo_space;Doxycyline 100mg/day(CQ= widespread resistance)

43
Q

Drugs safe in malaria in pregnancy

A

+ 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
Q

+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

A

+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
Q

+MoA of CCNS drugs
+ Cell cycle specific anticancer drugs(PEAS HATE BED VITC)
+drug acting on 3 phases

A

+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
Q

+Classification of alkalyting agent
+ Drugs in each class

A

+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
Q

Uses and S/E of cyclophopamide and its uses

A

+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
Q

+ features of 1) melphalan 2) chlorambucil

A

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
Q

special features of busulfan (6 s/e)

A

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
Q

+Procarbazine use and its replacement
S/E
+Temozolamide
+thiotepa
+Altretamine

A

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
Q

Nitrosoureas use and s/e

A

+astrocytomas resitant to temozolamide
+BM suppression= Neutropenia -single dose = prolonged suppression

52
Q

+pump responsible for entry and resitance to platinum compounds
+ drug specific side effects
+management of nephrotoxicity

A

+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
Q

uses of platins in cancers(LOGHUR)

A

Lung ca, Osteosarcoma ,Gi cancer(with 5 FU),Head and neck ca,Urogenital(testis,ovary, cervical),Retinoblastoma , Radiosensitiser

54
Q

anti cancer Drugs on S phase and their mechanism of action

A

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
Q

s/e of hydroxyurea

A

skin pigmentation and painful skin ulcers

56
Q

Uses and antidote of different folate analogues

A

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
Q

Resistance mech and se of Mtx

A

+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
Q

Classification enumeration and uses of purine analogues

A

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
Q

Classification, enumeration of pyrimidine analogues.

A

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
Q

+Microtubule inhibitors classification and other drugs with similar actions
+ S/E and Uses

A

+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
Q

topoisomerase inhibitors , uses and drugs with similar action

A

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

62
Q

Antibiotics as anti cancers(MBA MSD Play)

A

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)

63
Q

1)enzyme as anti ca drug
2) Vitamin as anti cancer drug
3)Metals as anti cancer drug

A

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