Cheatography
https://cheatography.com
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This is a draft cheat sheet. It is a work in progress and is not finished yet.
Anti-TB drugs
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Isoniazid (INH) |
Ethambutol |
PAS (4-aminosalicylic acid) |
Rifampin |
Cycloserine |
Streptomycin |
Class: |
Hydrazide |
-- |
-- |
Rifamycin(ansamycins) |
|
Aminoglycoside |
MOA: |
1. Inhibits synthesis of mycolic acid |
Mycolic acid competitor on cell wall |
PABA inhibitor for folic acid |
Inhibits DNA-directed RNA polymerase |
|
Inhibit protein synthesis |
| |
2. Anti-metabolite of NAD |
Uses: |
Anti-TB |
Only for dividing mycobacteria |
2nd line anti-TB that can be given orally as Na salt. |
Anti-TB and Anti-lepral drug. |
Notes: |
|
|
Synthesis involves Kolbe reaction then reduction. |
Semi-synthetic from rifampicin. |
|
Kanamycin, gentamycinamikacin can also be anti-TB. |
Anti-tubercular combination "Rimactazide": Isoniazid (INH) + Rifampin
Anri-lepral drugs
Dapsone (DDS) |
Acedapsone |
Sulfoxone sodium |
Not water soluble or long acting so prodrugs were produced. |
Orally bioavailable and long acting. |
Can be injected (water soluble) |
| |
From acetylation of dapsone. |
Prodrug of dapsone. |
Sulphonamides
Sulphanilamide |
Sulfisoxazole |
Sulfdiazine & Sulfametoxazole |
Succinyl sulfathiazole |
Sulfasalazine |
Mafenide acetate |
Original sulphonamide form from prodrug dye, prontosil, in-vivo activation by azoreductase. |
Short-acting |
Intermediate-acting |
For GIT |
For ulcerative colitis |
Topical for burn therapy. |
| |
It's rapidly excreted so concentrates in urine. |
Silfadiazine: burn therapy |
They're poorly absorbed so they concentrate in GIT. |
Designed to be poorly absorbed from GIT to concentrate there. |
Not a typical sulfonamide. |
| |
UT antiseptic. |
Sulfamethoxazole is chosen in the cotrimoxazole combination to have the same t1/2 as trimethoprim. |
Prodrug hydrolyzed by amidase enzyme. |
A prodrug that's activated by bacterial azoreductase enzyme into 5-ASA (not absorbed/remain in large intestine) & antibacterial sulfapyridine. |
MOA: Anti-metabolite of PABA during THFA synthesis.
- Inhibition of enzymes DHFS & DHFR can provide safety and selectivity.
Synergistic combination: sulphamethoxazole + trimethoprim =Cotrimoxazole/septrin
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