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Ther 201 LE 3 > Non-Beta Lactam Antibiotics > Flashcards

Non-Beta Lactam Antibiotics Flashcards

1
Q

Antifolate drugs MOA

A

inhibits folic acid (THF acid synthesis)

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2
Q

Cortimoxazole = _ + _

A

Sulfonamides

Trimethoprim

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3
Q

sulfonamides MOA

A

inhibits pteridine synthetase (since it is structurally similar to PABA) (PABA + PS)

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4
Q

trimethoprim MOA

A

inhibits DHF reductase (DHF -> THF)

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5
Q

Cortimoxazole indications

A

typhoid fever (1st line)
Pneumocystis jirovecii pneumonia
toxoplasmosis
nocardiosis

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6
Q

PK notes Cortimoxazole

A

wide distribution - crosses PLACENTA

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7
Q

Drugs which inhibit protein synthesis via 30S ribosome

A

Aminoglycosides

Tetracyclines

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8
Q

Drugs which inhibit protein synthesis via 50S ribosome

A

Macrolides
Chloramphenicol
Clindamycin

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9
Q

Aminoglycoside MOA (3)

A

1) inhibits initiation complex formation
2) misread RNA -> wrong protein
3) breaks up polysomes

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10
Q

clinical use of Aminoglycosides ALONE

A

UTI
//
combine with beta-lactam for other

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11
Q

adverse effects of Aminoglycoside

A

ototoxicity (irrev)
nephrotoxicity and neuro block (rev)
allergic rxn

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12
Q

given to reverse neuromuscular blockade due to Aminoglycoside

A

Ca gluconaate, Neostigmine

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13
Q

Tetracycline MOA

A

binds to 30S, blocks tRNA binding to Acceptor site on the mRNA ribosome complex - no peptide elongation

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14
Q

bacterial resistance mechanisms against tetracycline

A

1) impaired influx or impaired efflux by active transport protein pump Tet(AE) - G-
2) protects ribosome by producing proteins which interfere with tetracycline binding Tet(M) - G+

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15
Q

How are tetracyclines classified? What are the classifications

A

By half-life

1) Short-acting (6-8h)
2) Intermediate-Acting (12h)
3) Long-acting (16-18h)

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16
Q

Short-acting tetracycline drugs

A

Chlortetracycline

Oxytetracycline

17
Q

Intermediate-acting tetracycline drugs

A

Democlocycline

Methacycline

18
Q

Long-acting tetracycline drugs

A

Doxycycline
Minocycline
Tigecycline

19
Q

Longest acting tetracycline and half-life

A

Tigecycline, 36 hours

20
Q

Difference of route of excretion of long acting tetracyclines

A

Long-acting by biliary excretion unlike others which are renal

21
Q

Tetracycline clinical use

A

Chlamydia
Mycoplasma pneumonia
cholera (short term ok for <8yo)
leptospirosis

22
Q

tetracycline contraindicated for

A

pregnant & <8yo

23
Q

Aminoglycoside and TEtracycline difference in chemical properties

A

A - not acid stable, irreversibly binds

T - acid stable, reversible

24
Q

Macrolides MOA

A

inhibit translocation of tRNA from A to P site

25
Q

Macrolides examples

A

Erythromycins
Clarithomycin
Azithromycin
Roxithromycin

26
Q

Macrolides Pharmacokinetics

A

wide distribution but poor CSF penetration

27
Q

Drug interaction with Macrolides

A

(1) They decrease CYP1A2 and CYP3A3/4 levels -> elevated effects of other drugs
(2) +Terfenadine or Astemizole -> cardiac arrhythmias

28
Q

advantages of newer macrolides

A

less GI side effects

29
Q

macrolide indications

A 
atypical pneumonia
whooping cough (Borderella pertussis)
Gastroeneteritis
Diphtheria
Penicillin Hypersensitivity alternative drug
30
Q

chloramphenicol MOA

A

binds to 50S ribosomal subunit and inhibits transpeptidation (blocks P-A transfer)

31
Q

chloramphenicol chemistry

A

oral - palmitate
IV - succinate

palmitate inactive must be hydrolyzed in s.i. pure chloramphenicol does not dissolve in water

32
Q

T/F Oral route is preferred than IV route for chloramphenicol

A

T

succinate is an inactive produg, must be hydrolysed first but process is incomplete losing 30%

33
Q

Chloramphenicol indications

A

reserved for serious infections
H. influ - meningitis
1st line for typhoid feer
brain abscess

34
Q

Adverse effects of Chloramphenicol

A

Idiosyncratic aplastic anemia
Gray Baby syndrome
Optic Neuritis

Ther 201 LE 3 (9 decks)

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