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Pharma From Sure Success > Antimicrobial Drugs > Flashcards

Antimicrobial Drugs Flashcards

1
Q

Egs of diaminopyrimidines (2)

A

Trimethoprim
Pyrimethamine

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2
Q

Egs of nitrobenzene

A

Chloramphenicol

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3
Q

Egs of lincosamide (2)

A

Lincomycin
Clindamycin

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4
Q

Egs of glycopeptide (2)

A

Vancomycin
Teicoplanin

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5
Q

Nicotinic acid derivatives (3)

A

Isoniazid
Pyrizinamide
Ethambutol

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6
Q

Oxazolidinone eg

Eg of polypeptide (3)

A

Linezolide

Polymixin B
Colistin
Bacitracin

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7
Q

Eg of polyene (2)

A

Nystatin
Amphotericin B

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8
Q

Antibiotics obtained from fungi (3)

A

Penicillin, cephalosporin, griseofulvin

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9
Q

Antibiotics obtained from bacteria (3)

A

Polymixin B , Colistin, Bacitracin

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10
Q

Antibiotics obtained from actinomycetes (4)

A

Aminoglycosides
Tetracyclines
Macrolide
Chloramphenicol

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11
Q

Antibiotics with narrow spectrum of activity (3)

A

Penicillin G, streptomycin, erythromycin

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12
Q

Antibiotics with broad spectrum of activity (2)

A

Tetracycline
Chloramphenicol

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13
Q

What are the gram + cocci? (3)

A

Staphylococcus
Streptococcus
Enterococci

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14
Q

Gram -ve cocci (2)

A

Neisseria
Moraxella

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15
Q

What are the gram +ve rods ?

A

Actinomycetes
Bacillus
Clostridium
Diphtheria
Listeria monocytogenes

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16
Q

Antibiotics that become bactericidal at high concentrations (2)

A

Erythromycin
Nitrofurantoin

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17
Q

Antibiotics that inhibit cell wall synthesis are all ……

Another one that is bactericidal

A

Bactericidal

Those that cause leakage from cell membrane : polypeptides
Polyenes
Azoles

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18
Q

Those that inhibit protein synthesis are all ……except ……

A

Bacteriostatic
Except: aminoglycosides , streptogramin
Bactericidal

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19
Q

Short acting sulfonamides (4)

A

Diazine
Methizole
Oxaxole
Cysteine

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20
Q

Intermediate acting sulfonamide

Long acting sulfonamides

A

Sulfamethoxazole

Doxine
Methopyrazine

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21
Q

Topical sulfonamides

A

Sulfaacetamide sodium
Silver sulfadiazine
Mefetide

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22
Q

For RA and UC

A

Sulfasalazine

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23
Q

MOA of cotrimoxazole

A

PABA ——-> DHFA———THFA
FS. DHFR
Sulfonamide. Trimethoprim

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24
Q

Sulfonamide is a ……..inhibitor of PABA

A

Competitive inhibitor

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25
Q

Uses of sulfonamides

A

When combined with pyrimethamine
—resistant malaria, toxoplasma

When combined with cotrimoxazole
—SEPTRAN
STD: chanchroid, LGV
Enteritis: ecoli, shigella
P.carini, P.jejuni
Typhoid
Respiratory tract infection
Acute UTI
Nocardia

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26
Q

Adverse effects of sulfonamides

A

ABC of RASH
Aplastic anemia
Bilirubin displacement
Crystalluria
Rash
Acetylation
SLE
Hemolysis in G6PD

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27
Q

Adverse effects of trimethoprim

A
  1. N/V/ stomatitis
    2 megaloblastic anemia
  2. Pancytopenia
  3. Hyperkalemia
  4. Teratogenicity
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28
Q

MOA of dapsone

A

Structurally related to sulfonamides
Inhibits dihydroopeterate synthase
Prevents folic acid synthesis

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29
Q

First drug of nalidixic acid

A

Fluoroquinolones

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30
Q

Benefits of FQ (5)

A
  1. Highest potency
  2. Expanded spectrum
  3. Slow resistance
  4. Better toleratibilty
  5. Better tissue penetration
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31
Q

Classification of FQ

A

1st generation: gram -ve activity
nalidixic acid, oxalidinic acid

2nd generation: extended gram -ve activity
Norflox, lomeflox, ciproflox, oflox

3rd generation: gram -ve,gram+ve
Levoflox, spatiflox,gatiflox,peflox
Temaflox, tosiflox, moxiflox

4th generation: gram -ve,gram +ve, anerobes
Trova, sita, clina, gami,pruli, flero

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32
Q

Uses of FQ

A

4G SPECTRUM CT
4G: gonorrhoea,gynecological,gram -ve,,GI
S: septicemia
P: prophylaxis
E: enterocolitis
C: chanchroid
T: typhoid
R: resp tract
U: UTI
M: meningitis

C: conjunctivitis
T: Tb

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33
Q

Adverse effects of FQ (6)

A
  1. GIT: n/v/stomatitis
  2. CNS: due to GABA antagonist
    Sleep disturbance,mood disturbances, headaches,seizures
  3. CVS: Torsades de pointes: long Qt prolongation
    Sparflox, gati,moxiflox
  4. Phototoxic: lome >spar>peflox
  5. Bone and soft tissue:
    Tendinitis, tendon rupture
  6. Teratogenic
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34
Q

Most potent FQ

Least potent FQ

A

Ciprofloxacin

Norflox

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35
Q

Ciplox should not be taken with ….

FQ have low……

A

Food- as it delays absorption

CSF and aqueous level

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36
Q

FQ is ……

Peflox-use

A

Less active at acidic Ph

Meningeal infection- good CSF permiability

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37
Q

FQ with highest oral bioavailability

FQ with lowest oral bioavailability

A

Levoflox

Norflox

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38
Q

Drug with max plasma protein binding

Drug with highest first pass metabolism

A

Sparflox

Peflox

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39
Q

Longest acting FQ

FQ most potent against T.b

A

Sparflox

Moxiflox

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40
Q

What drug should not be given with FQ?

Elimination of Sparflox

A

NSAIDS- enhance CNS toxicity
Theophylline- ciplox and peflox increase toxicity

50% renal, 50% liver

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41
Q

FQ metabolized in liver (5)

A

Trova
Moxi
Peflox
Grepo
Nalidixic acid

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42
Q

Withdrawn from market coz of :
1. Temafloxacin
2. Grepafloxacin

A
  1. Immune hemolytic anemia
  2. Cardiotoxic
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43
Q

Withdrawal from market
3. Trovafloxacin

  1. Clinafloxacin
A
  1. Hepatotoxicity
  2. Phototoxcity
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44
Q

Gatiflox removed from market coz of ….

A

Hyperglycemia in elderly

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45
Q

MOA of FQ

A

Direct nucleic acid inhibitor
Inhibit DNA gyrase ( A subunit) in gram -ve
Inhibit topoisomerase 4: in gram +ve

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46
Q

DOC for anthrax

Most commonly used drug for diarrhoea

A

Ciprofloxacin

Ciprofloxacin

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47
Q

What is nalidixic acid ?

A

Non fluorinated quinolone used to rx UTI

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48
Q

MOA of Nitrofurantoin

A

Blocks acetyl CoA synthesis in bacterial carbohydrate metabolism

Used as urinary antiseptic in UTI

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49
Q

Why are aminoglycosides called so?

A

Coz they have amino groups linked glycosidically to >_2 amino sugar

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50
Q

Classification of aminoglycosides

A

Systemic: TANGSS KP
Tobramycin
Amikacin
Netilmicin
Gentamicin
Streptomycin
Sisomycin
Kanamycin
Paromomycin

Topical aminoglycosides
Neomycin
Framycetin

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51
Q

Egs of Ototoxic drugs (5)

A
  1. Aminoglycosides
  2. Furosemide
  3. Vancomycin
  4. Cisplatin
  5. Amphotericin B
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52
Q

Egs of nephrotoxic drugs (4)

A

Aminoglycosides
Amphotericin B
Cisplatin
Cyclosporine

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53
Q

MOA of aminoglycosides

A

Inihibition of initiation of protein synthesis and misreading of mRNA code

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54
Q

Spectrum of activity of Aminoglycosides

A

Only gram -ve bacteria.
Need oxygen for penetration, so not active in anerobes.

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55
Q

Aminoglycosides useful in bowel surgery

A

Neomycin

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56
Q

Dosage of aminoglycosides

A

Gentamycin , tobramycin ,siso,netilmycin
3- 5mg/kg/day

Streptomycin, amikacin : 7.5-25mg/kg/day

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57
Q

Aminoglycosides given for intestinal amibiasis and tapeworm

A

Paromycin

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58
Q

Most commonly used aminoglycosides

Sisomycin is similar to ….

A

Gentamycin

Gentamycin

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59
Q

Max activity of tobramycin is against …..org

……is no longer used due to toxicity

A

Pseudomonas

Kanamycin

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60
Q

Aminoglycosides useful against MRSA

Use of spectinomycin

A

Arbekacin

Rx of gonorrhoea in penicillin allergy patients

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61
Q

Aminoglycosides with widest spectrum

Topical ointments

A

Amikacin

Neomycin
Framycetin

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62
Q

Uses of paromycin (5)

A

Protozoal parasites:
Entameoba histolytica
Trichomonas vaginalis
Giardia lamblia
Cryptosporidium
Leishmania

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63
Q

Side effects of aminoglycosides

A

ONN HT
Ototoxicity
Nephrotoxicity
Neurotoxicity

Hypersensitivity
Teratogenic

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64
Q

Most vestibulotoxic AG

Most cochleotoxic

A

Streptomycin

Amikacin

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65
Q

Most nephrotoxic aminoglycosides

Least nephrotoxic aminoglycosides

A

Neomycin

Streptomycin

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66
Q

Maximum neuromuscular blockade

A

Streptomycin

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67
Q

Dosing sequence of AG

A

3 equal parts ( slowly over 60 mins) iv , every 8 hours

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68
Q

Dosing of Gentamycin as per renal clearance

A

> 70ml/min: 70% daily
50ml/min: 50% daily
30ml/min: 30% daily
20- 30ml/min: 80% on alternate days
10-20ml/min: 60% on alternate days
<10ml/min: 40% on alternate days

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69
Q

Why are macrolides called so?

A

Coz they have a big macro ring with attached sugars

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70
Q

Egs of macrolides

A

SET CAR
Spiramycin
Erythromycin
Tacrolimus
Clarithromycin
Azithromycin
Roxithromycin

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71
Q

Erythromycin is acid …….. hence given in …..form

Erythromycin undergoes …….circulation

A

Labile
Enteric coated form

Enterohepatic circulation and is excreted in bile

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72
Q

Erythromycin obtained from ……

Antibacterial spectrum of erythromycin

A

Streptomycetes erythreus

Gram +cocci
Gram -ve cocci
Gram + bacilli

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73
Q

MOA of erythromycin

A

Inhibit protein synthesis by inhibiting transfer of amino acids from A site to P site in 50S ribosome

It is bacteriostatic

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74
Q

Erythromycin can cause Qt prolongation if given along with: (3)

A

Astemizole
Terfenadine
Cisapride

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75
Q

Adverse effects of erythromycin

A

MACRO
Motilin receptor agonist
Allergy
Cholestasis
RO : Reversible ototoxicity

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76
Q

Cholestasis jaundice occurs …..days after Rx with erythromycin

Sms of cholestatic jaundice

A

10-20 days after therapy

Nausea,vomiting, abdominal cramps, jaundice, fever

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77
Q

Incidence of cholestatic jaundice is higher in ……

Uses of erythromycin

A

Pregnant women

C3LAW
Chancroid
Campylobacter
Corynebacterium
Legionella
Atypical pneumonia
Whooping cough -Bordetella pertusis

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78
Q

Erythromycin is DOC for ….(2)

A

Mycoplasma atypical pneumonia
Whooping cough

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79
Q

Azithromycin is DOC for ….(2)

A

Legionella
Chlamydia trachomatis

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80
Q

Clarithromycin is first line drug for ….

A

MAC

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81
Q

……, and ……macrolide inhibit CYP3A4 enzyme
This increases serum concentration of …… and ……

A

Erythromycin
Clarithromycin

Theophylline
Oral coagulants

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82
Q

MOA of lincosamides

What are the lincosamides ?

A

Similar to macrolides

Lincomycin
Clindamycin

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83
Q

Uses of clindamycin

A
  1. DOC for topical acne Rx
  2. DOC for bacteroids fragilis
  3. Clindamycin-pyrimethamine: T gondi
  4. Clindamycin + primaquine= P. Jejuni
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84
Q

S/e of clindamycin

A

Diarrhea
Pseudomembraneous colitis

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85
Q

Eg of ketolides what are they?

A

Telithromycin

Semisynthetic derivative of erythromycin having 3 keto group

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86
Q

Indication of telithromycin

A

Macrolide resistant community acquired pneumonia

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87
Q

MOA of linezolid
Spectrum of linezolid

A

Same as macrolides

Gram + pathogen only

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88
Q

Linezolid uses (3)

A

Rx for VRSA,MRSA
Diabetic foot

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89
Q

S/e of linezolid (3)

A

Myelosuppression
Optic neuropathy
Inhibit MAO- cheese reaction with tyrosine containing food

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90
Q

Streptogramins are in ratio :

A

Quintupristin: dalfopristin= 30:70

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91
Q

Adverse effect of streptogramin

A

Iv only
Arthralgia- myalgia syndrome

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92
Q

Polymixin B and colistin are given only topically why?

A

Asss with nephrotoxicity and neurotoxicity when given systemically

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93
Q

Mupirocin is obtained from: …..
Given….

A

Pseudomonas flutoscens

Topically

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94
Q

2% topical ointment for staph, strept- impetigo, folliculitis etc is …..

A

Retapamulin

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95
Q

Fusidic acid MOA, use

A

Inhibit protein synthesis
Use: topical

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96
Q

Non antibiotic use of erythromycin (2)

A
  1. Motilin receptor agonist : dm gastroparesis
  2. Anti I.F effect : arthritis
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97
Q

MOA of tetracycline

A

Inhibition of new amino acetyl tRNA at A site of 30S ribosomes

It is bacteriostatic

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98
Q

Why are tetracyclines called so?
Obtained from …..

A

Coz they have 4 benzene rings

Actinomycetes

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99
Q

Classification of tetracyclines

A

Gp1: t1/2: 6-10 hrs
Tetracycline, chlortetracycline,o a cyclone

Gp2: t1/2: 12-13 hrs
Demeclocycline, lymecycline

Gp3: t1/2: 18-20 hrs
Doxycycline, minocycline

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100
Q

Resistance to tetracycline (3)

A
  1. Decrease influx, increase efflux
  2. Creating ribosomal protein cover-to decrease entry
  3. Creating tetracycline inactivating enzyme.
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101
Q

Uses of tetracyclines

A

VACUM The BedRoom
Vibrio
Acne
Chlamydia
Ureaplasma
Mycoplasma
Typhoid
Borellia
Rickettsia

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102
Q

Food retards absorption of all tetracycline except (2)

A

Doxycycline and minocycline

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103
Q

All tetracycline should be reduced in renal failure except ……

A

Doxycycline

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104
Q

Use of demeclocycline

Use of minocycline (3)

A

Rx of SIADH

Swimming pool granuloma caused by M.marinum
Topically acne, periodontitis

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105
Q

Adverse effects of tetracyclines

A

LK ADVI is PT Teacher
Liver damage
Kidney damage - except doxycycline
Antianabolic effect
D.I - demeclocycline
Vestibular toxicity: minocycline
Increased ICP
Phototoxic: with demeclocycline and doxycycline
Teeth and bone discoloration
Teratogenic

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106
Q

How does tetracycline cause teeth discoloration?

Tetracycline not given below ……yrs of age

A

By forming calcium tetracycline chelates and gets deposited on teeth

-<8 yrs age

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107
Q

Do not mix injectable tetracycline with …..

A

Penicillin - inactivation occurs

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108
Q

Tetracyclines should not be given along with ……drug

Should not be given …..

A

Diuretics

Intrathecally

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109
Q

Chronic tetracycline use can cause …..(2)

What is Fanconi’s syndrome?

A

Esophageal and vaginal candidiasis

Tetracycline beyond expiry date

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110
Q

Tigecycline is a ……analogue. Use

A

Minocycline
It is 20 times more potent than tetracyclines

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111
Q

Tigecycline is given for …..(3)
It is eliminated through …..

A

MRSA
VRE
Complicated skin and soft tissue and intra abdominal infections

Bile

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112
Q

Chloramphenicol is obtained through …..
It is a ……ring moeity. It is bacterio….

A

Streptomyces venzuelae

Nitrobenzene ring moeity
Bacteriostatic

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113
Q

MOA of chloramphenicol
At higher doses it inhibits …..

A

Inhibit peptide bond formation from P window to A window

Mamalian mitochondrial protein synthesis as well. Bone marrow cells are susceptible

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114
Q

Adverse effects of chloramphenicol

A

BIG Super Hypersensitivity
Bone marrow suppression
Irritable sms: n/v if ingested, pain on iv
Gray baby syndrome
Superinfections
Hypersensitivity reaction

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115
Q

What is gray baby syndrome?

A

Premature infants lack liver UDP- glucoronyl transferase characterized by :
Cyanosis
Abdominal distension
Hypothermia
CVS collapse
Death

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116
Q

Chloramphenicol is a potent enzyme inhibitor and inhibits …..(3)

A

Morphine ( respiratory depression)
Chlorpropamide (hypoglycemia)
Warfarin ( bleeding)

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117
Q

Daily dosing of chloramphenicol
What should be kept in mind?

A

Should not exceed 2-3g daily. Rx course <2 weeks should not exceed <28 gram.

Daily CBC should be done and if seen anemia /TCP, drug should be stopped.

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118
Q

Uses of chloramphenicol

A

BARE TB
Bacterial meningitis/ pyogenic meningitis
Anerobic infection
Rickettsia
Ear and eye infection( conjunctivitis & endopthalmitis)
Typhoid
Brucellosis

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119
Q

Bacterial cell wall structure consist of ….

A
  1. N-acetyl muramic acid (NAM)
  2. N-acetyl glucosamine (NAG)

Only NAM consists of peptidoglycan residues to it, and cleavage of last chain of NAM releases energy that helps transpeptidase in crosslinking NAM forming stability to bacterial cell wall

120
Q

Beta lactams are more susceptible to ……bacteria. Why?

A

Gram +ve bacteria- as they have more peptidoglycan to it.

121
Q

Resistance of beta lactams

A
  1. Altered permiability: decrease influx, increase efflux
  2. Formation of betalactamases/penicillinase
  3. Alteration of penicillin binding protein (pbp) so that betalactams can’t destroy the transpeptidases.
    MRSA is by this mechanism
122
Q

Uses of penicillin G

A

LAST MAN DP
leptospirosis
Actinomycetes
Staph,strept
Treponema, tetanus
Meningococcus
ANthrax
Diphtheria
Pneumococcus

123
Q

What are the extended spectrum penicillin?

A

A CT MAP
Amino gp: Amoxicillin, ampicillin
Carboxy gp: carbenicillin, ticarcillin
Ureido gp: Mezlocillin,Azlocillin,Piperacillin

Ureido group has the broadest spectrum

124
Q

Why are beta lactam antibiotics called so?
What are the egs?

A

Coz they have beta lactam rings next to thiazolidine ring

They are:
Penicillin
Cephalosporin
Carbapenems
Monobactams

125
Q

Who discovered penicillin?
Penicillin is obtained from….

A

Alexander Flemming

Fungus: penicillinium notatum, penicillium chrysogenum

126
Q

MOA of beta lactams

A

Bind to penicillin binding protein and block transpeptidase. Cell wall becomes unstable—> cell wall deficient bacteria, water gets in osmotically, bacteria swell and lysis.
Thus all beta lactams are bactericidal

127
Q

Natural penicillin was ……
3 problems with it

A

Penicillin G - benzyl penicillin
3 problems:
1. Acid labile
2. Penicillinase suseptible
3. Narrow spectrum- only gram +ve.

128
Q

Which is the acid resistant penicillin ?

A

Phenoxymethyl penicillin- penicillin V

129
Q

Depot IM formulation of penicillin G (2)

A
  1. Procaine penicillin G
  2. Benzathine penicillin G
130
Q

Penicillin G is excreted by …..

Prophylactic uses of penicillin G (3)

A

Kidneys

  1. Rheumatic fever
  2. Bacterial endocarditis
  3. Agranulocytosis
131
Q

DOC for treponema pallidum

What are the penicillinase resistant penicillin?

A

Benzathine penicillin

CONDoM
Cloxacillin
Oxacillin
Nafcillin
Methicillin

132
Q

Methicillin causes …..s/e

A

Interstitial nephritis

133
Q

Amoxicillin is better than ampicillin by :
(3)

A
  1. Oral bioavailability- doesn’t interfere with food absorption
  2. Incidence of diarrhoea is lower
  3. Preferred over ampicillin for bronchitis,
    UTI,
    SABE,
    Gonorrhoea

The disadvantage: it is less effective than ampicillin for shigella and H influenza.

134
Q

Adverse effects of penicillin G (3)

A
  1. Local reaction
  2. Hypersensitivity reaction
  3. Jarisch Heixermer reaction
135
Q

Antipseudomonal penicillin are

A

CT MAP
Carbenicillin
Ticarcillin
Mezlocillin
Azlocillin
Piperacillin

136
Q

What are the beta lactamase inhibitors?
What are they?

A

They are suicide drugs, given along with penicillin to prevent its degradation by betalactamases.

They inhibit beta lactamases first , so that beta lactams can now perform their action.

They are:
Clavulonic acid - with amoxicillin
Sulbactam with ampicillin
Tazobactam with piperacillin

They are combined like this as combinations are due to similar t1/2.

137
Q

Extended spectrum penicillinase inhibit all except ….

Beta lactam that resemble aminoglycosides s

A

Carbapenems

Monobactams

138
Q

Use of Monobactams (3)

A
  1. Only gram -ve orgs, no effect on gram +ve.
  2. Can be used for penicillin/cephalosporin allergy -esp ceftazidime allergy
  3. For those with renal insufficiency who can’t use aminoglycosides
139
Q

Carbapenems are DOC for …..
Imipenem is always given with …..

A

Enterobacteria

Cilastatin-as imipenem is degraded by renal dihydropeptidase 1. Vikas Yatin is inhibitor of this enzyme.

140
Q

S/e of carbapenems

A

Seizures at high levels - imipenem only.
Others are stable to renal dihydropeptidase, and do not cause seizures

141
Q

Main side effect reactions with
Methicillin:

Oxacillin

Cross reactivity of penicillin and cephalosporin is ….% of patients

A

Interstitial nephritis

Hepatitis

6-10%

142
Q

MOA of vancomycin
It is bacteri….

A

Inhibit mucopeptide cell wall formation by binding to D-ala D ala portion of cell wall precursors

Bactericidal

143
Q

Resistance of vancomycin

A

D-ala d-ala is changed to d-ala d-lac

144
Q

vancomycin is DOC for (2)

A
  1. MRSA
  2. Clostridium difficult

Gram +ve aerobic bacteria

145
Q

S/e of vancomycin (4)

A

Nephro toxicity
Ototoxicity
Thrombophlebitis
Diffuse red man syndrome - diffuse flushing
Rx: prerx of antihistamine, slow infusion rate.

146
Q

Drug more active against enterococci than vancomycin is ….

Use of teicoplanin (2)

S/e of teicoplanin

A

Teicoplanin

Endocarditis prophylaxis
Pseudomembranous colitis

Bronchi spasm-rarely

147
Q

Those betalactams that interfere with coagulation test (3)

A

Telavancin
Dalbevancin
Ortivancin

148
Q

Daptomycin is inactivated by …..
S/e of daptomycin (2)

A

Pulmonary surfactant

Myopathy
Eosinophilic pneumonia

149
Q

Bacitracin is mainly …..
Active against (3)

A

Topical
Staph,strept,clostridium difficle

150
Q

Use of fosfomycin

Use of cycloserine

A

Single 3gm to rx uncomplicated UTI in women
Safe in pregnancy

Used as second line drug in TB

151
Q

Cephalosporin are beta lactamase…..

A

Resistant , except first gen
Broader spectrum of activity

152
Q

Cephalosporin active against MRSA

A

5th generation

153
Q

How to remember cephalosporin generation?

A

Cef “a” — first gen except : cefaclor
Cef (pi)—- 4th generation
Cef (me,one,ten)—-3rd generation , moxilactam cefuroxime: 2nd generation
Cef (rol) ——5th generation

Rest all are second gen.

154
Q

Cephalosporins have ……group

A

Methylthiotetrazole

155
Q

Cephalosporin can cause _______s/e (2)

A

Hypoprothrombinemia
Disulfiram like reaction

156
Q

S/e of ceftriaxone

A

Cholelithiasis

157
Q

Cephalosporin used for
1. Gonorrhoea
2. Typhoid
3. Surgical prophylaxis

A
  1. Ceftriazone
  2. Ceftriazone
    Cefoperazone
  3. First generation
158
Q

Moa of echinocandins
Egs

A

Inhibit 1-3 beta glycan- a component of fungal cell wall.
Caspofungin
Micofungin

159
Q

Echinocandins can be used for …..fever

A

Neutropenic fever not responding to antibiotics

160
Q

Echinocandin that requires
Loading dose
That which do not require loading dose

A

Loading dose: caspofungin

No loading dose: micafungin

161
Q

Ciclopirox MOA use.

A

Moa: inhibit DNA rna synthesis
Use : shampoo for seborrheic dermatitis

162
Q

MOA of polyene group

A

Ampho B and nystatin
Creates pores in bacterial cell membranes and increase in efflux of membrane ion

Thus causing fungicidal action

163
Q

How is amphoB given in iv?
How is amphoB given in rx?

A

Dilute with 5% glucose/ dextrose
Saline makes it very coarse

Ampho B + flucytosine = synergistic action.

164
Q

Adverse effects of ampho B (2)

A
  1. Mc infusion reaction : hypotension, fever, chills.( shake and bake syndrome)
  2. Nephrotoxicity: type 1 RTA: decrease K+, mg2+.

Thus ampho B is given as liposomal ampho b

165
Q

Source of amphoB

Source of nystatin

A

Streptomycetes Nodosum

Streptomycetes noceri

166
Q

MOA of Azoles

A

Inhibit new protein synthesis by inhibiting dimethylase .
(Lanosterol —x——> ergosterol

They are fungistatic

167
Q

S/e of imidazoles

Only oral azoles

A

Enzyme inhibitor
Adrenal suppression

Ketoconazole
Itraconazole

168
Q

Antifungal with longest t1/2, shortest t1/2

A

Longest: isavuconazole
Shortest: voriconazole

169
Q

Antifungal with both anti I.f and antipruritic action

Itraconazole is DOC for …(3)

A

Sertaconazole

Histioplasmosis
Sporotrichosis
Blastomycosis

170
Q

Antifungal effective on both dermatophytes and systemic

DOC for dermatophytes

A

Ketoconazole

Terbinafine

171
Q

Protein synthesis inhibitor of anti fungal

Inhibits dna and rna synthesis

A

Tavaborole

Flucytosine, ciclopirox

172
Q

Flucytosine useful for …..(2)

A

Candida
Cryptococcal

173
Q

S/e of flucytisine

Antifungals with renal elimination

A

BMS, hepatotoxic

Fluconazole
Flucytosine

174
Q

Voriconazole given for ….

Azole with no CNS penetration

A

Aspergillosis

Itraconazole

175
Q

S/e of griseofulvin
Important feature of griseofulvin

A

Disulfiram reaction

Can be taken with fatty meals

176
Q

S/e of voriconazole

Micafungin increase levels of ….(2)

A

Visual disturbances

Nifedipine
Cyclosporin

177
Q

Azole used for mucormycosis

Drug used as shampoo (2)

A

Posaconazole

Ketoconazole
Ciclopirox

178
Q

Ampho B is active against all except ..(2)

A
  1. Paracoccidiomycosis
  2. Chromomycosis
179
Q

Terbinafine is given …..
Butenafine is given ….

A

Both topical and oral
Topical

180
Q

Anti fungal to be avoided in ventricular dysfunction

Antifungal with widespread resistance
Use to rx……

A

Itraconazole

Griseofulvin
Only dermatophytes

181
Q

MOA of terbinafine
Doc for onychomycosis

A

Inhibit squalene epoxide, squalene increases, fungicidal action.

Terbinafine
Finger nail: 6weeks
Toe nail: 12 weeks

182
Q

Drug with relatively drug drug interaction

A

Micafungin

183
Q

Hyphal distortion is by …..

A

Tolnaftate

184
Q

MOA of human influenza virus

A

Human influenza virus has hemagluttinin and neuraminidase proteins on it, along with M2protein ion channels.
1. Uncoating:
Influenza binds to sialic acid on the host cell with HA and is pushed into the cell.
In the cell, matrix protein opens the ion channels and viral mrna is pushed out.

  1. Endonuclease:
    Viral mRNA goes to nucleus and the endonuclease enzyme takes host 5’ cap of host mrna and fixes it on viral mrna.

Viral mrna goes to ribosomes and forms structural and functional proteins.
These proteins goes to Golgi apparatus; gets packaged into vesicles and ready for exocytosis.

  1. Exocytosis
    When the vesicle reaches the cell membrane, it fuses with the cell membrane, and is still stuck to the sialic acid of the host cell with HA of virus.
    Neuraminidase of this virus comes and cleaves the HA-sialic acid bond and virus buds off and released.
185
Q

Antiinfluenza Drugs that inhibit M2 ion channels

A

Uncoating inhibitors: Amantadine
Rimantadine

186
Q

Which influenza does it uncoating inhibitors cover?

What are the adverse effects? (3)

A

Only influenza A

Ataxia
Livedo reticularis
Prolonged Qt interval—>TdP

187
Q

What are the drugs that inhibit endonuclease?
Which influenza does it cover? Importance ?

A

Baloxavir

Covers both influenza A&B
If given <48 hrs of sm onset.

188
Q

What antiinfluenza inhibit neuraminidase enzyme? Importance

A

Oseltamivir
Zanamivir

Works only when given less than 48 hrs of symptom onset and prophylaxis in adults and children > 5yrs.

189
Q

MOA of HBV

A

HbV is a partially ds DNA, binds to NCTP protein of human cell and gets into the cell.

Partially dsDNA is taken into the nucleus and forms complete ds DNA and can replicate consistently.

Some of the dna gets converted via transcription to
1. mrna and goes to ribosomes to make proteins that goes to Golgi apparatus.
2. Pregenomic mrna

Reverse transcriptase converts pregenomic rna to dna and together with structural proteins in Golgi apparatus, gets packaged into vesicles and exocytosed.

190
Q

AntiHBV drugs that inhibit reverse transcriptase?

A

NRTI: lamivudine, entecavir
NtRTI: adefovir, tenofovir

191
Q

Which of the antiHBV drugs is responsible for fanconi syndrome ?

Which drug inhibit protein that forms MHC class 1 molecule?

A

Adefovir, tenofovir

Interferon alpha

192
Q

Adverse effects of INF alpha (2).

A

Teratogenic
Pancytopenia

193
Q

MOA of HCV

A

Virus gets into the human cell—> rna goes to RER—> forms big polyproteins:
NS3-NS4A-NS5A-NS5B

Enzyme NS3/4A protease cleaves these polyprotein into structural and functional proteins —> Golgi apparatus —> packaged into vesicles and exocytosed.

194
Q

AntiHCV drugs that inhibit NS3/4A protease?

A

Protease inhibitors -previr

195
Q

Drugs that inhibit NS5A protein

Drugs that inhibit NS5B protein

A

-asvir: daclatasvir, ledipasvir

-buvir: sofosbuvir,dasabuvir

196
Q

Which antiHCV drugs inhibit inosine 5PDH preventing guanosine nucleotide thereby preventing RNA formation?

Indication and s/e of above

A

Ribavirin

Indication:
Refractory HCV, as triple therapy:
Ribavirin+INF+ sofosbuvir

S/e: teratogenic, hemolytic anemia

197
Q

MOA of herpes

A

Viral DNA gets into the cell—> dna polymerase —> replication.
Some dna goes to nucleus, gets converted to RNA—> ribosomes—> proteins—Golgi apparatus —> exocytosis

198
Q

Drugs which inhibit DNA polymerase in herpes rx?

Which one is pyrophosphate analogye?

A

Cidofovir, foscarnet

Foscarnet

199
Q

Indication of DNA polymerase inhibitors of herpes rx?

A

Ganciclovir resistant CMV
Aciclovir resistant HSV

200
Q

Which DNA polymerase inhibitor causes seizures?

Which one causes crystal Nephropathy? What should be done?

A

Foscarnet

Cidofovir
Give along with IV fluids and probenecid

201
Q

Which anti herpetic drug is posphorylated ibto guanosine analogue?

Indications (3)

A

Aciclovir, valaciclovir

HSV esophagitis, meningitis, mucocutaneous lesions.

202
Q

Which guanosine analogue in herpes rx causes Nephropathy?

Which one causes TTP?

A

Aciclovir-give with IVF.

Aciclovir,valaciclovir

203
Q

Adverse effect of ganciclovir
Indications

A

A/e: BMS
Indication:
CMV: esophagitis, retinitis,
Pulmonary nodular amyloidosis

204
Q

RNA polymerase inhibitor for RSV is..
Fusion inhibitor is ….

A

Ribavirin

Pavlizumab

205
Q

Drug against Envelope proteins for HSV

206
Q

Terminase inhibitor of CMV

A

Letermovir

207
Q

Rx of human small pox. Viral target

A

Target: VP37 envelope wrapping protein
Drug: tecovirimat

208
Q

MOA of NRTI and NNRTI

A

Both block reverse transcriptase preventing conversion of viral RNA to DNA .
NRTI: conpetitive inhibitor-binds to active site

NNRTI: non competitive inhibitor-binds to allosteric site and cause conformational change of the reverse transcriptase enzyme.

209
Q

Egs of NRTI and NNRTI

A

NRTI: ZALES TD
Zidovudine
Abacavir
Lamivudine
Stavudine
Tenofovir
Didanosine

NNRTI:
-vir-
Nevirapine
Efavirenz

210
Q

MOA of protease inhibitors egs

A

Inhibit the cleaving of viral polyprotein.
Those that end with -navir

211
Q

MOA of entry inhibitors eg. (4)

A
  1. Blocks gp 41 to bind to CD4T cell- enfuvirtide
  2. Blocks CCR5 receptor : Maraviroc
  3. Blocks CD4 receptor: Ibalizumab
  4. Blocks binding of Gp120 to CD4: Fostemsavir
212
Q

What are the integrase inhibitors ? Eg

A

Blocks the integration of viral DNA into host DNA.
Those that end with -gravir.

213
Q

Integrase inhibitors are also called ……

A

Strand transfer inhibitors

214
Q

Combined side effect of NRTI and NNRTI

A

NRTI: mitochondrial injury-
Myopathy
Peripheral neuropathy
Hepatic steatosis
Lactic acidosis

NNRTI: Rash

215
Q

NRTI also effective against Hep B are :
(3)

A

Tenofovir
Emcitrabine
Lamivudine

216
Q

Safest NRTI

A

Lamivudine
Emcitrabine

217
Q

Lamivudine is a …..analog
Emtricitabine is a …….analog

A

Deoxycytidine analog

Fluorinated cytidine analog

218
Q

Abacavir is a …..analog
S/e

A

Guanosine analog

Hypersensitivity especially in HLAB5701 pts. This is called pharmacogenetics

219
Q

Only nucleotide in NRTI is ……s/e…(2)

A

Tenofovir
S/e: renal toxicity
Osteoporosis

220
Q

Tenofovir not suitable for lactose intolerant patients why?

A

Coz tenofovir is formulated with lactose.

221
Q

Toxicity of zidovudine
Other side effects (5)

A

Bone marrow suppression

Insomnia
Myopathy
Hyperpigmentation of skin and nails
Lactic acidosis
Hepatomegaly

222
Q

S/e of didanosine

S/e of stavudine (3)

A

Pancreatitis

Peripheral neuropathy
Lactic acidosis
Highest risk for lipodystrophy

223
Q

Toxicity of zalcitabine

Toxicity of nevirapine

A

Oral ulcer

Hepatotoxicity

224
Q

S/e of efavirenz
One thing to note is …..

A

Neuropsychiatric symptoms: vivid dreams
Qt prolongation —>Tdp

Avoid taking it with fatty meals

225
Q

Etavirine is given as …
Another drug given same is ….

A

Combination drug

Emcitrabine -also given as combination drug

226
Q

Side effect of protease inhibitors (4)

A

Metabolic abnormalities: (4)
Dyslipidemia
Hyperglycaemia
Insulin resistance
Lipodystrophy

227
Q

All Protease inhibitors are potent ….

A

CYP3A4 inhibitors -increase risk of bleeding in hemophiliacs

228
Q

Protease inhibitor with least dyslipidemia
S/e (2)

A

Atazanavir
Hyperbilirubinemia
Nephrolithiasis

229
Q

The rationale for giving lopinavir + Ritonavir is ….

A

Ritonavir is a potent CYP 3A4 inhibitor. In low dose , it boosts all other protease inhibitors.

230
Q

Side effect of indinavir (2)

A

Indirect hyperbilirubinemia
Nephrolithiasis

231
Q

Nelfinavir has ….s/e
……is used with nelfinavir

A

Hepatotoxic
Sweetner aspartame is used with nelfinavir as it contains phenylalanine

232
Q

Least potent CYP3A4 inhibitor:

Prodrug of amprenavir

A

Saquinavir

Fosamprenavir

233
Q

S/e of raltegravir (2)
S/e of dolutegravir (2)

A

Myopathy
Rhabdomyolysis

Insomnia
Headache

234
Q

Why is carbotegravir always used with rilpivirine?

A

As it causes depression and hepatic dysfunction

235
Q

Indication for use of cobicistat

A

Pharmacokinetic enhancer
Used in combination with darunavir/atazanavir
Increases the effectiveness of the HIV meds.

236
Q

MOA of pyrantel palmoate

A

Direct depolarization blocker.
Binds to Nm receptor( where Ach normally binds); causes parasitic muscle contraction, but too much pyrantel palmoate desensitizes the Nm receptor—> muscle relaxation—>fecal excretion

Therefore pyrantel palmoate causes spastic paralysis in parasite

237
Q

MOA of piperazine

A

GABA agonist
Opens chloride channels->chloride comes into the parasite cell->hyperpolarization->muscle relaxation->fecal excretion.

Thus piperazine causes flaccid paralysis in worms

238
Q

MOA of ivermectin

A

Opens glutamate gated chloride channels->chloride gets in—>hyperpolarization—>muscle relaxation—>fecal excretion

239
Q

MOA of DEC - diethylcarbamazepine

A

Changes Arachnidonic acid metabolites in the worms, immune system recognises this and phagocytosis by monocytes.

240
Q

MOA of niclosamide

A

Inhibit glucose uptake—>no oxidative phosphorylation—>no energy —>worm die

241
Q

MOA of praziquantel

A

Destroys voltage gated calcium channel—>calcium gets inside the worm cell unregulated—>excess calcium —>rapid contraction—>paralysis

242
Q

MOA of mebendazole

A

Binds to beta tubulin —> inhibits polymerization—>inhibits mitotic spindle —>inhibits cell division —>cell death.

243
Q

MOA of metrifonate

A

Organophosphorus
Similar action of pyrantel palmoate-direct depolarization blocker.

244
Q

MOA of oxamniquine

MOA of bithionol

A

Blocks DNA synthesis in parasite

Blocks ATP synthesis in parasite

245
Q

Drugs causing uncoupling of oxidative phosphorylation (2)

A

Bithinol
Niclosamide

246
Q

DOC for trematodes
Egs (2)

A

Praziquantel

Blood fluke-schistosoma hematobium
Lung fluke-paragonimus westermani

247
Q

DOC for liver fluke is ….
(Fasciola hepatica)

A

Triclabendazole >bithinol

248
Q

DOC for cestodes is …..except…

A

Praziquantel
Except:
1. Neurocysticercosis: tenia solium(pork)
2. Hydatid disease ( echinococcus granulosus-dog tapeworm)

—DOC : albendazole

249
Q

DOC for nematodes except: (4)

A

Albendazole
1. Pinworm: mebendazole
2. Threadworm: ivermectin
3. Filariasis (wucheria bancrofti): DEC
4. Onchocerca volvulus: ivermectin

250
Q

DOC for guinea worm: dracunculosis

A

Metronidazole , niridazole

251
Q

Albendazole is DOC for (5)

A
  1. Cutaneous larva migrans
  2. Visceral larva migrans
  3. Toxocariasis
  4. Hydatid disease: 6months Rx
  5. Neurocysticercosis: 1 month Rx
252
Q

Drug given for neurocysticercosis

A

Albendazole + praziquantel

253
Q

Praziquantel is c/i in ……

A

Ocular cysticercosis

254
Q

Rx regimen for filariasis
Adverse effect (2)

A

Albendazole + DEC/ivermectin
Liver toxicity
Bone marrow toxicity

255
Q

Important thing about benzimidazoles

A

C/I in first trimester
Can be given in second /third trimester

256
Q

Uses of ivermectin (5)

A
  1. Onchocerciasis
  2. Lymphatic filariasis
  3. Scabies
  4. Head lice
  5. Strongyloides
257
Q

Antibiotic useful in filariasis

Antihelminth with immunomodulatory action

A

Doxycycline

Levimazole

258
Q

Drug with anti protozoal,antiviral,antihelminth activity

A

Nitazoxanide

259
Q

MOA of amebiasis

A

Cysts in the lumen (quadrinucleate) forms tennis racquet shaped structure-trophozoites—> cyst and is excreted.

  1. Patient can be an asymptomatic carrier
  2. Trophozoites can invade the intestinal lumen and cause amebic colitis
  3. Trophozoites can via blood go to liver and other organs and infect them -extraintestinal amebiasis
260
Q

Antiamebic drugs classification

A
  1. Patients with asm carrier :
    Rx with luminal agents -cysts in intestine are killed- diloxanide furoate
    Others : paramomycin, iodoquinol
  2. Amebic colitis + extraintestinal amebiasis:
    Start by killing Trophozoites:
    a. Metronidazole
    b. Emetine
    c. Chloroquine

Then Rx with luminal agents to kill the remaining cysts.

261
Q

S/e of emetine
Importance of chloroquine

A

Highly cardiotoxic

Kill liver amebiasis, not intestinal ones.

262
Q

MOA of metronidazole

A

It’s is a nitro group that releases free radicals upon oxidation and damage the parasites
They are cidal drugs

263
Q

S/e of metronidazole (3)

A
  1. Metallic taste -anorexia
  2. Pancreatitis -rare.
  3. Disulfiram like reaction- due to accumulation of aldehyde dehydrogenase
264
Q

Drugs causing disulfiram like reaction

A

C: chlorpropamide, cefoperazone
G: griseofulvin
M: metronidazole
P: Procarbazine

265
Q

Uses of metronidazole (3)

A

A. Anti protozoal :
1. Amebiasis -amebic colitis and extraintestinal
2. Trichomonas vaginalis
3. Giardiasis

B. Antibacterial
1. Anerobic bacteria
Bacteroids fragilis
Pseudomembranous colitis
Acute necrotizing gingivitis-trench mouth.

  1. H.pylori- quadruple regimen
  2. Bacterial vaginosis

C. Antihelminth:
Guinea worm- dracunulosis

266
Q

Advantages of tinidazole over metronidazole

A

Tinidazole- decrease metallic taste
Better safety profile
Longer t1/2 than metronidazole

267
Q

Longest nitroimidazole drug

A

Secnidazole

268
Q

Classification of antimalarials based on : (4)

A
  1. Preerythrocytic phase. Prophylaxis
  2. Exoerythrocytic phase: radical cure
  3. Erythrocytic phase: clinical cure
  4. Gametocytic phase: prevent human-mosquito transmission.
269
Q

Infective form of parasite is ….

A

Sporozoite -present in the saliva of female anopheles mosquito.

270
Q

Definitive and intermediate host of malaria

A

Definitive: female anopheles mosquito
Intermediate: man

271
Q

Life cycle of plasmodium

A

Bite of mosquito —> sporozoites present in the saliva of mosquito gets into the human cell—>
1. Liver : preerythrocytic phase
Sporozoites—>merozoites
Exoerythrocytic phase:
Sporozoites—> hypnozoites
2. Blood:
Merozoites rupture the liver cells and gets into the blood.Erythrocytic phase.
Fever happens when the blood cells rupture ie, every 2nd-3rd day.

Merozoites can get converted to Trophozoites, schizonts and more merozoites.

Merozoites then can form gametocytes.

  1. Mosquito bite the infected person, the gametocytes goes to the intestine of the mosquito, fertilize and the zygote gets converted into sporozoites which gets to the saliva of the mosquito.
272
Q

Rx for chloroquine sensitive P, falciparum

A

Chloroquine + primaquine
( although p falciparum doesn’t have an Exoerythrocytic phase, primaquine is given for the gametocidal action.

273
Q

Rx for chloroquine resistant p falciparum

A

Artesunate + mefloquine
Artemether+ lemefantrine
Artesunate + sulfadioxime + pyrimethamine

274
Q

Rx for Chloroquine sensitive p.vivax

A

Chloroquine + primaquine

275
Q

Chloroquine resistant P.vivax (3)

A
  1. Artesunate + primaquine
  2. Quinine+ doxycycline
  3. Clinadamycin + primaquine
276
Q

Falciparum malaria is mainly seen in …….area

Rx for uncomplicated p.falciparum in pregnancy

A

North eastern states

1st trimester: quinine salt
2nd/3rd: area specific ACT

277
Q

DOC for p.vivax in pregnancy

A

Chloroquine

278
Q

Full form of NVBDCP

A

National vector borne disease control program

279
Q

MOA of chloroquine

A

Chloroquine gets taken up by infected RBC —> increased Ph in vesicle
Hb—>heme—>hemazoin
Inhibited by Cq

Heme increases—->toxic to the parasite.
Rupture of plasmodium membrane but not RBC.

280
Q

Drugs with MOA similar to chloroquine (3)

A

Quinine
Mefloquine
Lumefontrine

281
Q

Uses of chloroquine

A

REDLIP Mahatma Gandhi
Rheumatoid arthritis
Extraintestinal amoebiasis
DLE
Lepra reaction
Infectious mononucleosis
Photogenic reaction
Malaria
Giardiasis

282
Q

Chloroquine has a high Vd (100L/kg)
Adverse effects of chloroquine

A

ROOP Depress my Heart
Rash
Ototoxic
Oculotoxic
Peripheral neuropathy
Depress-myocardial depression
H-hypotension

283
Q

Drugs acting on Erythrocytic phase

A

Fast acting:
Mefloquine
Atorvaquine
Chloroquine
Halofantrine
Artemisin
ResQ (quinine)

Slow acting :
Proguanil
Tetracycline

284
Q

Uses of mefloquine (2)

A

Cq sensitive and resistant P falciparum
Cq resistant p vivax

285
Q

S/e of mefloquine

A

Sinus bradycardia
Neuropsychiatric sms: fuzzy thinking,nightmares

286
Q

Oldest antimalarial is …..obtained from….

A

Quinine
Bark of the Cinchona tree

287
Q

Define Cincchonism (5)

A
  1. Tinnitus
  2. High frequency hearing loss
  3. N/V
  4. Dysphoria
  5. Postural hypotension
288
Q

What are the other side effects of quinine (2)

A

Qt prolongation
Hypoglycemia-infuse with 5% dextrose

289
Q

How is pyrimethamine given? MOA?

A

MOA: DHFR inhibitor:
inhibits DHFA—->THFA

Infuse with 5% dextrose to prevent hypoglycemia
Given along with sulfonamide

290
Q

S/e of primaquine
C/I of primaquine

A
  1. N/V -prevented by taking with high fatty meals .
  2. megaloblastic anemia at high doses.

C/I : Hemolytic anemia in G6PD patients
Pregnancy

291
Q

MOA of primaquine

A

Contains reactive metabolite which desrupt ETC of parasite.

292
Q

Hemolytic anemia is seen in ….places (4)

A

Jharkand
Madhya Pradesh
Andra Pradesh
Assam

293
Q

Antimalarial given as single dose
Use.

A

Tafenoquine
Radical cure

294
Q

S/e of artemesin (2)

A

Reticulocytopenia
Neutropenia

295
Q

Artemesin obtained from ….

A

Artemesia-Chinese plant

296
Q

Water soluble artemesin
Lipid soluble artemesin

A

Water soluble: Artesunate
Lipid soluble: artemether

297
Q

Artemesin developed in india for IM use
Artemesin developed in india for oral use

A

Arteether

Arterolane

Pharma From Sure Success (10 decks)

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