Lect 1

PROTEIN INHIBITORS

* BROAD-SPECTRUM ANTIBIOTIC

1. TETRACYCLINE

-general: bacteriostatic but bactericidal at high []

-moa: inhibit bact protein synthesis (30S)

-uses: resistant to almost ALL gram +/- COCCI except for N.gonorrhea but
sensitive to bacilli

-class:

i. Tetracycline (6-10 hrs) - short

ii. Democlocycline (12-13 hrs) – intermediate

iii. Doxycycline (18-20 hrs) – long-acting

-pk:

i. oral especially wf doxycycline (IV if required) coz food x TC

absorption

ii. x wf dairy products

iii. x in csf

iv. liverurine but doxycycline in bile

-a/e: epigastric pain + discoloration of teeth + hepatotoxic + nephrotoxic

2. CHLORAMPHENICOL

-general: bacteriostatic, from Streptomyces venezuelae

-moa: inhibit bact protein synthesis (50S), - 70S causes host toxicity

-pk:

i. oral

ii. distributed in csf

iii. liverurine

-a/e: bone marrow suppression + Gray Baby syndrome

3. MACROLIDES

-general: bacteriostatic but bactericidal at high []

-class:

i. natural- erythromycin

ii. semisynthetic- azithromycin

-moa: inhibit bact protein synthesis (50S) at ALKALINE pH

-pk:

i. x in csf

ii. liverbile

-a/e: severe epigastric pain (motilin receptor agonist)

-d/i: cytochrome enzyme inhibitor (not azithromycin)

4. CLINDAMYCIN

-general: clindamycin + lincomycin = lincosamide

-uses: serious infection of staph and strept (anaerobes)

-a/e: pseudomembranous colitis + NMJ block (IV)

5. LINEZOLID

-general: synthetic,bacteriostatic

-moa: inhibit bact protein synthesis (50S)

-uses: ONLY gram + (MRSA including vancomycin-resistant strains)

6. KETOLIDES

-general: struc related to macrolides

-uses: RT infection caused by macrolide-resistant bacteria

7. STREPTOGRAMINS

-moa: inhibit bact protein synthesis (50S and 70S)

-uses: MRSA infection

Lect 2

CELL WALL INHIBITORS

* FOSFOMYCIN – inhibit biosynthetic enzyme

* BACITRACIN – combined wf carrier molecules

* VANCOMYCIN – combined wf cell wall substrates

* BETA LACTAMS – inhibit attachment of new peptidoglycan into cell wall

* BROAD-SPECTRUM ANTIBIOTICS

* BACTERICIDAL

BETA-LACTAMS

* ALL r resistant to MRSA

1. PENICILLINS

-class:

i. natural- penicillin V + G (short) and procain benzylpenicillin

(long)

ii. semisynthetic-

a. AMPICILLIN (sulbactam)

b. anti-pseudomonal : TICARCILLIN (clavulanate) +

PIPERACILLIN (tazobactam)

c. anti-staph : METHICILLIN - penicillinase resistant

d. beta-lactamase inhibitor : *in bold

-a/e: allergy, git discomfort

2. CEPHALOSPORINS

-class:

i. 1st generation: more against gram + ( ), low against gram – and

less resistant to beta-lactamase

ii. 2nd

iii. 3rd

iv. 4th generation: more against gram – ( ), more resistant to beta-

lactamase

-a/e: same wf penicillin

3. CARBAPENEM

-progrug: imipenem

-pk: only iv

-a/e: some wf others but ++ cns (seizure) + cvs (hypotension)

4. MONOBACTAM

-prodrug: aztreonam

-uses: high gram -ve

-only iv + highly protein-bound

Lect 3

AMINOGLYCOSIDES

-prodrugs:

i. streptomycin

ii. gentamycin

iii. amikacin
 iv. neomycin

v. kanamycin – topical use

-moa: inhibit bact protein synthesis (30S)

- BACTERICIDAL

-uses: GRAM - ONLY

-pk:

i. iv for systemic infection, oral if want topical effect on gut

ii. x in csf

iii. NOT metabolised, excreted unchanged by kidney

iv. NARROW therapeutic window

-a/e: reversible nephrotoxicity + irreversible hearing impairment +

reversible balance disturbance

Lect 4

SPECTINOMYCIN

-general: derived from Streptomyces spectabilis

-uses: GRAM + AND –

-moa: inhibit protein synthesis (30S)

- bacteriostatic

-a/e: hypersensitivity

Lect 5

SYNTHETIC ANTIMICROBIALS (ANTI-FOLATES)

1. SULPHONAMIDES

-general: more soluble at ALKALINE pH

-moa: have structural similarity wf PABA hence can compete for

dihydropteroate sythase
-class:

i. oral

a. sulfadiazine – short

b. sulfamethoxazole – intermediate acting

c. sulfadoxine – long

ii. orally x absorbed:- sulfasalazine w is used in ulcerative

colitis

iii. topical:- sulfacetamide

-uses: GRAM – ONLY

-pk:

i. NEVER given iv or im

ii. cross BBB

iii. liverurine

-a/e: crystalluria + renal toxic + hypersensitivity rxn + haemolytic

anemia

2. TRIMETHOPRIM

-moa: competitively – dihydrofolate reductase

-uses: GRAM – AND +

-pk:

i. oral

ii. distributed in csf

iii. renal excretion (adjustment wf renal insufficiency)

3. SULFAMETHOXAZOLE + TRIMETHOPRIM = COTRIMOXAZOLE

-general: in ratio of 5:1

-iv or oral

-can produce SEQUENTIAL BLOCKADE