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Pharma Midterm 3 Flashcards

1
Q

unique targets example of action

A
  • inhibition of cell wall synthesis (B-lactam)
  • Fungal cell membrane component:
  • folic acid synthesis (sulfonamides)
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2
Q

similar targets action

A

dihydrofolate reductase
protein synthesis inhibitors

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3
Q

protein synthesis inhibitor acting on 30S subunit

A
  • tetracyclines
  • Aminoglycosides
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4
Q

protein synthesis inhibitor acting on 50S subunit

A
  • Macrolides
  • Phenicols
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5
Q

Example of drug having dose dependent toxicity, high dose effect

A

Phenicols, can cause bone marrow suppression

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6
Q

Common target drugs example

A

Primary antineolastic agents
antiparasitic drugs (cholinergic substances)

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7
Q

Example of Category A drug TOTALLY banned, target animals

A

Vancomycin; for small animals

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8
Q

Category B drugs

A
  • fluroquinolones
  • 3-4th generation cephalosporin
  • colistin
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9
Q

Category C drugs, target animals

A

Macrolides, phenicols
smalls & Food producing

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10
Q

Category D drugs

A

tretracyclines
penicillines

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11
Q

Meaning of MIC (describing efficacy)

A

Concentration of antibacterial where Bacteria cannot GROW

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12
Q

Meaning of MPC (describing efficacy)

A

Concentration of antibacterial where we won’t select any mutant/resistant bacteria

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13
Q

Meaning of MBC (describing efficacy)

A

Concentration of antibacterial where Bacteria can be killed

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14
Q

Example of bactericidal

A

Aminoglycosides
Polypeptides
Fluoroquinolones
Metronidazole

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15
Q

Example of bacteriostatic

A

Tetracycline
Macrolides
Phenicols

(Post Traumatic Mouvement)

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16
Q

Define Postantibiotic effect

A

delayed antibacterial effect after concentration of the drug declined below the MIC (usually against Gram +)

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17
Q

define Synergistic, give example

A

Potentiate each other
penicillin + streptomycin

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18
Q

define additive, give example

A

broaden spectrum
gentamicin + metronidazol

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19
Q

define antagonist, give example

A

fights for the same subunit
erythromycin + florfenicol

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20
Q

Examples of transferring resistance between bacteria

A
  • conjugation
  • transduction (via bacteriophages)
  • transformation (from dead bacteria)
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21
Q

List the 5 resistance mechanisms

A
  • antibiotic degrading enzymes (penicillinase)
  • antibiotic transforming enzymes
  • increasing integrity of cell wall
  • increased efflux pump expression
  • modifying binding sites (MRSA)
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22
Q

List the antibacterial agents that are inhibitor of protein synthesis

A
  • aminoglycosides
  • tetracyclines
  • macrolides
  • lincosamides
  • pleuromutilins
  • phenicols
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23
Q

which type of tetracyclines have the best properties? Examples

A

Semisynthetically, doxycycline/minocycline

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24
Q

Short acting tetracyclines, (daily dose)

A

tetracyclines
oxytetracycline
chlortetracycline
(applied BID)

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25
Q

intermediate acting tetracycline

A

demeclocycline

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26
Q

long acting tetracycline + (daily dose)

A

Doxycycline
minocycline
(SID)

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27
Q

structural specificity of tetracyclines

A

lipophilic compounds because of 4 rings (moderate lipophilic)

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28
Q

mécanisme of action of tetracyclines (normal concentration)

A

inhibition of protein synthesis (30S subunit)

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29
Q

mechanism of action tetracyclines at high concentration

A

bacterialcidal, loss of functional integrity of cytoplasmic membrane

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30
Q

mode of action of tetracyclines

A

bacteriostatic

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31
Q

tétracycline resistant bacteria specie

A

E. Coli,
Salmonella spp.
Past. multocida
Manheimia haemolytica
Staphyloccocus aureus
streptococcus

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32
Q

antimicrobial spectrum of tetracyclines

A

aerobic &anaerobic
Gram + & -
(all bacteria types)

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33
Q

tétracyclines are very effective against

A
  • mycoplasme
  • rickettsiae
  • chlamydophilae (zoonotic)
  • Wolbachia spp. (bact. in heart worm)
  • Borrelia spp (lyme’s)
  • bordetella bronchiseptica (kennel cough)
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34
Q

drug of choice against Mycoplasma haemofelis

A

tetracyclines

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35
Q

drug of choice against anaplasma phagocytophilum

A

tetracyclines

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36
Q

how to treat heart worm

A

to avoid cytokine storm, should be killed very slowly
- doxycycline for 1 month : 10mg/Kg, BID

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37
Q

Can tetracycline be effective against protozoa

A

yes, most common in Hungary Babesia spp.

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38
Q

mechanism of resistance against tetracyclines

A
  • impaired uptake into bacteria
  • active efflux
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39
Q

bacterial tetracycline resistant ovo

A
  • pseudomonas aeruginosa
  • mycobacterium
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40
Q

tetracyclines acquired resistancy

A

E.Coli
Salmonella spp.
Pasteurella multocida, Mannheimia Haemolytica (Gram -)
Staphylococcus aureus, streptococci (Gram +)

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41
Q

administration of tetracyclines

A

often used orally, but bioavailability bad (5-10%)
action of short acting tetracyclines not good

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42
Q

AMEG classification of tetracyclines

A

D category “Prudent”

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43
Q

Long acting tetracyclines ADME

A

A= Excellent
D= Excellent (bone & can cross BBB)
M= low degree
E= mainly large intestine, bile

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44
Q

Classic Tetracyclines ADME

A

A: (10%) moderate, impaired by food
D: Good (bone)
M: Low degree
E: mainly urine

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45
Q

Indications of tetracyclines

A
  • Bronchopneumonia
  • Foot disease
  • Metritis, mastitis
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46
Q

application of tetracycline for foot diseases

A

spray form

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47
Q

Specific conditions treated with tetracyclines

A
  • Lyme disease (doxy, 6-8 weeks)
  • chlamydophilosis
  • feline mycoplasmosis
  • infectious keratoconjunctavitis in cattle
  • proliferative enteropathy in horses
  • heartworm
  • heartwater
    -nocardiosis
  • anaplasmosis
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48
Q

Side effects of tetracyclines

A
  • GI disturbance
  • Dysbacteriosis
  • collapse, hyperkalaemia (rapid IV injection)
  • tissue necrosis (IM)
  • yellow discoloration of teeth
  • photosensitivity
  • hepatotoxicity (high concentration)
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49
Q

Which phenicol is prohibited in food producing animals

A

Chloramphenicol

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50
Q

which phenicol is only used in poultry industry

A

tiamphenicol

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51
Q

which phenicol is widely used in farm animals

A

Florfenicol

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52
Q

structural specificity of phenicols

A

Lipophilic, small molecules (have excellent pharmacokinetic properties)

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53
Q

Mechanism of action of Phenicols

A

inhibition of protein synthesis (subunit 50S)

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54
Q

Mode of action of phenicols

A

Bacteriostatic

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55
Q

what are the mechanisms of resistance of phenicols

A
  • impaires uptake into bacteria
  • active efflux
  • Acetyl transferase (enzymes modify the structure of drug)
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56
Q

Antimicrobial spectrum of phenicols

A

broad
Aerobis & anaerobic
Gram + & -

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57
Q

which drug is the only authorized in fish against Aeromonas salmonicida & Vibrio anguillarum?

A

Florfenicol

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58
Q

AMEG classification of phenicols

A

C category “caution”

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59
Q

Can phenicols be used against Chlamidophila & Rickettsia

A

yes, but TTC are first choice (cheaper, more effective & cat D.)

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60
Q

ADME of phenicols

A

A: Excellent (oral = IM/SC)
D: Excellent
M: extensive in liver
E: urine (inactive) & bile

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61
Q

Classification of different Half lives of phenicol

A

ruminants > swine > cat > dog

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62
Q

Administration of phenicol in Ru

A

every 2nd day

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63
Q

daily Administration of phenicol in Su

A

once daily

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64
Q

Administration of phenicol in feline

A

BID

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65
Q

Administration of phenicol in canine

A

TID

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66
Q

Side effects of phenicols

A

dose dependent : liver
Anaemia
CHLORAMPHENICOL - aplastic anaemia
long term: immunosuppression
pain at injection site (IM)

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67
Q

indication of phenicols for FPA

A

mainly Food producing animal (florfenicol):
Respiratory disease
foot disease
infectious keratoconjunctivitis
fish aeromonas infection

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68
Q

indication of phenicols for small animals

A

eye infection
prostatitis
meningitis
MRSA infection

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69
Q

chemistry of macrolides and outcome

A

lactone ring with sugar = lipophilic & weak base
so ion trapping inside cells and high IC concentration

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70
Q

Macrolides distribution

A

broad, but not to brain

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71
Q

mechanism of action of macrolides

A

Inhibition of protein synthesis (50S)

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72
Q

mode of action of macrolides

A

Bacteriostatic
(bactericidal high concentration, IC and Respiratory tract pathogens)

73
Q

Resistance to macrolides

A

not so common,
decreased permeability
degrading enzymes
modified binding sites (cross resistance with lincosamides & phenicols)

74
Q

Name of macrolide with 2 nitrogen

A

azalide
- AZITHROMYCIN
- gamithromycin

75
Q

name of macrolide with 3 nitrogen

A

triamilide,
- tulathromycin

76
Q

antimicrobial spectrum of macrolides

A

Gram +
Gram - (anaerobic):
- fastidious
- Campylobacter
- Brachyspira hyodysenteria
- Lawsonia intracellularis
- Bordetella bronchiseptica
- mycoplasma, chlamydophila
- Borrelia
- Rhodococcus equi

77
Q

what are the Gram - fastidious bacteria (6)

A

Pasteurella
manheima
histophylis
haemophylis
actinobacillus

78
Q

For which indication should tyrosine phosphate be used & why

A

Swine enteric disease : because only 15% bioavailability

79
Q

For which indication should tyrosine tartarate be used and why?

A

Swine respiratory disease : because 30% bioavailability

80
Q

IM and SC macrolides are used for which animals

A

Ruminants and swine

81
Q

How are macrolides given to horses, dogs and cats?

82
Q

most important fact about distribution of macrolides

A

Resp. tract (tonsillae)
intracellular

83
Q

Which other drug should macrolides NEVER be combined with

A

ionophor antibiotics

84
Q

Excretion of macrolides

A

90% by the bile

85
Q

macrolides side effects

A

GI irritation (vomiting, diarrhea)
dysbacteriosis (horses, rabbit, herbivore rodents)
tissue irritation

86
Q

macrolides cannot be used in horses (T/F)

A

True in adult horses, can be used in foals as they haven’t developed their intestinal flora

87
Q

indication of erythromycin

A

horses: R. equi (+rifampicin
smalls: campylobacteriosis

88
Q

indication of spiramycin

A

smalls: oral cavity infections
large: mastitis (but tissue irritation & long WP)

89
Q

why is tyrosine less used

A

frequent resistant

90
Q

indication of tylosin

A

(past) swine dysenter
lawsonia intracellularis
(su, ru, poultry) resp tract infection, necrotic enteritis
smalls: ONLY ARD in ca

per os

91
Q

which is the most cardiotoxic macrolide

A

Tilmicosin

92
Q

indication of tilmicosin

A

ONLY, Ru (SC) & Su(Po)
fastidious Gram - & Mycoplasma

93
Q

indication for tylvalosin

A

per os
Su & poultry
- B. hyodysenteria
- L. intracellularis
- Mycoplasmae
- Fastidious Gram -

94
Q

Tulathromycin, gamithromycin indications

A

Ru & Su (injection)
fastidious organisms
mycoplasmae
RESP TRACT INFECTIONS
long acting

95
Q

Tildipirosin indications

A

Ru & Su
RESP TRACT INFECTIONS
long acting

96
Q

indications for Azithromycin & clarithromycin

A

for Smalls, Hu & Eq
- Gram +
- Fastidious gram -
- Borrelia, Mycoplasmae, campylobacter, R. Equii
good lung concentration

97
Q

General properties of lincosamides

A

inhibition of 50S
Bacteriostatic
cross resistance w/ macrolides & phenicols
good absorption,distribution (not BBB) excreted by bile & urine

98
Q

toxicity of lincosamides

A

tissue irritation
DYSBACTERIOSIS
prohibited for horses, rabbit, herbivore rodents

99
Q

Lincosamides spectrum

A

gram + & anaerobic
B. hyodysenteriae, L. intracellularis
Mycoplasmae
Campylobacter

100
Q

Lincosamide drugs

A

Lincomycin
Clindamycin
Pirlimycin

101
Q

lincomycin indication

A

Food prod animals (injection)
- foot rot, wounds, mastitis, swine dysentery, respiratory tract

102
Q

clindamycin indication

A

smalls
- dermatitis, abscesses, oral cavity
- anal sacculitis (anaerobic bact)
- osteomyelitis

103
Q

Indication for Pirlimycin

104
Q

Pleuromutilins drugs

A

tiamulin, valnemulin

105
Q

tiamulin cannot be combined with …

A

ionophore anticoccidials

106
Q

G properties of pleuromutilins

A

inhibition of 50S
Bacteriostatic
cross resistance w/ macrolides & phenicols
good absorption,distribution (not BBB) excreted by bile & urine

107
Q

toxicity of pleuromutilins

A

skin erythema
vulvar edema
(from urine)

108
Q

pleuromutilins spectrum

A

Gram +
Fastidious
B. hyodysenteria, L. intracellularis
Mycoplasmae

109
Q

pleuromutilins indications

A
  • swine dysentery
  • proliferative enteropathy
  • mycoplasmosis + resp (su & poultry)
110
Q

mode of action of cephalosporins

A

bactericidal time dependent

111
Q

how can there be cephalosporin resistancy

A
  • ab ovo
  • b-lactamase production
  • PBP (penicillin binding proteins) mutation
112
Q

cephalosporin spectrum

A

different according to generations
gram -&raquo_space;> 4th
1st «&laquo_space;gram +

113
Q

oral 1st generation cephalosporin

A

cephalexine
cephadroxil

114
Q

parenteral 1st generation cephalosporin

A

Cephapirin
Cefalonium
Cephalotin
cephazoline

115
Q

1st generation cephalosporin is similar to

A

amoxicillin

116
Q

2nd generation cephalosporin spectrum

A
  • Gram - (against lactamase producers)
    E.coli, Salmonella, Klebsiella
  • Anaerobic bacteria
117
Q

3rd generation cephalosporin spectrum

A

weak Gram +
Gram - (most lactamase producers) + Pseudomonas aeruginosa
fastidious & anaerobic (pasteurella, manhemia)

118
Q

4th G. cephalosporin spectrum

A
  • Gram +
  • Gram - (lactase prod)
    (more active if MICs are lower)
  • fastidious & anaerobic
119
Q

Absorption of cephalosporin

A

oral & parenteral

120
Q

excretion of cephalosporin

A

kidney
Bile : cefoperazone, ceftriaxone & cefaclor)

121
Q

cephalosporin side effects

A
  • allergy (eq. moderately tolerates)
  • dysbacteriosis
  • haematological
  • mild nephrotoxicity (if combined with AG)
122
Q

indication of 1st generation cephalosporins

A
  • mastitis/metritis
  • dermatitis, soft tissue infection
  • Resp infection
  • UTI
    (- preoperative : cephalozine) surgery > 1h
123
Q

Oral 2nd G. cephalosporins

A

Cefuroxine axetil
Cefaclor

124
Q

Parenteral 2nd G. cephalosporin

A

Cefuroxime
cefotetan, cefoxitin (anaerobic)

125
Q

2nd G cephalosporin indication

A

Dermatitis, soft tissue irritation
Resp infection
UTI

126
Q

3rd G cephalosporin oral

127
Q

parenteral 3rd G cephalosporins

A
  • Cefoperazone
  • Ceftiofur
  • Cefovecin
  • cefotriaxone & Cefotaxime (bone + brain & 2nd choice limes disease)
128
Q

3rd G Cephalosporin indication

A
  • dermatitis, soft tissue infections (cefovecin)
  • Resp infection
  • UTI
  • Menangitis, encephalitis (cefotriaxone)
  • osteomyelitis (cefotriaxone)
129
Q

AMEG categories for cephalosporins

A

Cat. B : 3rd & 4th G
Cat. C : 1st & 2nd G

130
Q

2 Other b-lactam ABs other than cephalosporins

A

Monobactams
Carbapenems

131
Q

Aztreonam
Tigemonam

A
  • parenteral
  • p.o.
    Cat A
    primary UTI
132
Q

Imipenem & meropenem

A

IV or IM
LAST RESORT AB (cat A)
highly active against all important pathogenic bacteria.

133
Q

structure of aminoglycosides

A

hydrophilic, eliminated by urine (so liver not included)

134
Q

Mechanism of action of aminoglycosides

A
  • cell membrane toxicity (oxidative stress)
  • RNA-structural damage
    do not give against anaerobic bacteria (O2 is needed)
135
Q

Mode of action of aminoglycosides

A

BACTERICIDALE concentration dependent
( spectinomycin has bacteriostatic effect)
good PAE (4-6 hours)

136
Q

aminoglycosides spectrum

A

gram - aerobic
- staphylococcus
- mycobacterium
micoplasma (spectinomycin)
pseudomonas (gentamycin)

137
Q

order of using aminoglycosides in case of resistant bacteria

A

Streptomycin > Neomycin > Gentamicin >Tobramycin, amikacin

138
Q

Absorption of aminoglycosides

A

p.o., parenteral, IV (if life threatening)

139
Q

distribution of aminoglycosides

A

systematic

140
Q

excretion of aminoglycosides

A

active form in urine (nephrotoxic must check if patient is hydrated)

141
Q

list aminoglycosides from most toxic to least

A

Neomycin > Gentamicin > Streptomycin > Amikacin > Spectinomycin

142
Q

With which other drugs should aminoglycosides not be combined with

A

muscle relaxants
furosimide

143
Q

indications of aminoglycosides

A
  • Resp infections
  • GI infection (esp enterobact)
  • UTI
  • Mastitis
  • Dermatitis
  • topical administration (eye, ear)
  • septicaemia
  • leishmaniasis
144
Q

Streptomycin

A

not alone, combined w/ penicillins
Su, Smalls
mastitis
1-3days

145
Q

Neomycin

A

alone & w/ penicillins
GI infections, mastitis
poultry & Su
not recommended to use systemically (most toxic) p.o. & topical

146
Q

Framycetin

A

component of neomycin produced by streptomyces fradiae
ear & eye infection
mastitis intrammamry infusion

147
Q

Gentamicin

A

alone
GI infection, mastitis
against pseudomonas aeruginosa

148
Q

Netilmicin

A

same as gentamicin:
GI infection, mastitis
against pseudomonas aeruginosa
but less ear & kidney toxicity and less activity against pseudomonas
+ lower respiratory tract infection

149
Q

Spectinomycin

A

poultry, Su
bacteriostatic
mycoplasma spp
GI infection

150
Q

Apramycin

A

p.o. bioavailability is better
Su
e.coli, diarrhea

151
Q

Tobramycin

A

toxic
Topical, parenteral
Pseudomonas aeruginosa

152
Q

Amikacin

A

parenteral only
pseudomonas aeruginosa
MRSA, MRSP (only one)

153
Q

paromycin

A

antiprotozoal treatment too
reduces effect of cryptosporidium parvum
antileishmanial

154
Q

aminoglycosides AMEG cat.

A

Category C, except spectinomycin (D)

155
Q

what is today’s most used penicillin

A

Amoxicillin

156
Q

Structure of Penicillins

A

B-lactam ring & thiazolidine ring

157
Q

mechanism of action of penicillins

A

inhibition of cell wall synthesis

158
Q

peptidoglycan structure & the bonds

A
  • N-acetyl - muramic acid/glucose amine chain
  • transpeptide bonds: transpeptidase, carboxipeptidase (PBP)
159
Q

mode of action of penicillins

A

bacteriocidal time dependent, act on dividing bacteria where new cell wall is synthesised (slow acting)

160
Q

can penicillins be combined with bacteriostatic?

A

no, will have no way of killing bacteria

161
Q

Why is it easier for penicillin to act on Gram + then Gram -

A

PBPs are located btwn cell wall & cell membrane , must reach and it is easier to penetrate gram + then gram -

162
Q

how can a bacteria have a ab ovo resistance

A
  • microplasma (no cell wall)
  • clamydia, brucella (brutal cell wall)
163
Q

how can we inhibit a B-lactamase production

A

adding clevulonic acid

164
Q

example of strains of bacteria having a PBP- gene mutation

A

MRSA, MRSP strains

165
Q

Narrow spectrum penicillins spectrum

A

most gram +
Gram - fastidious (PMHHA)
leptospira, borrelia spp
anaerobes

166
Q

Narrow spectrum penicillins active substances

A
  • Benzylpenicillin (Na,k / procaine / benzathine)
  • Phenoxymethyl - penicillin (orally)
  • penethamat (milk)
167
Q

ADME of narrow spectrum penecillins

A

A: oral (Phenoxymethyl - penicillin) otherwise parenteral
D: poor (not for intracellular)
M: hydrophilic so minimal (urine)
E: active form in urine

168
Q

side effects of procaine penicillin

A

piglets & foals are sensitive (lack procainase enzyme in liver)

169
Q

indication of narrow spectrum penicillins

A
  • resp infections
    1st choice for: Swine erysipelas
    anthrax
    tetanus
    necrotic enteritis
    streptoccocis
170
Q

Penicillinase stable penicillin active substance

A

Methicillin (acid sensitive)
Oxacillin, Cloxacillin, Dicloxacillin, Flucloxacillin, Nafcillin

O C D Fucks Neurons

171
Q

indication of penicillinase stable penicillins

A

dermatitis
mastitis

staphylococcus & streptococcus

172
Q

Extended spectrum penicillins spectrum

A

Gram + bacteria
Several Gram - (Fastidious, E.coli & salmonella, leptospira, borrelia)

173
Q

extended spectrum penicillins active substances

A

amoxicillin
ampicillin

174
Q

COmbination with amoxicillin

A

Clavulanic acid

175
Q

Combination with ampicillin

A

Sulbactam (B-lactamase inhibitor)

176
Q

oral absorption of ampicillin

A

weak (why it is not used)
feed reduces

177
Q

oral absorption of amoxicillin

A

good - excellent

178
Q

penicillins acting against pseudomonas spp.

A
  • piperacillin + tazobactam
  • ticarcillin
  • carbenicillin
179
Q

AMEG classification of penicillins

A
  • A: antipseudomonas
  • C: Extended spectrum
  • D: narrow & extended spectrum

Pharma MT (3 decks)

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