Anti-mycobacterial Agents/Antifungals Flashcards
Mycobacterium General
- Aerobic, Acid-fast bacilli or rods
- Mycolic acid in cell membrane absorbs carbofuschin stain after washing
- TB stains Lowenstein-Jensen w/ Malachire green
- MDRT + XDRT major problem of this decade
First Line TB Drugs
RIPE
Rifampin - RNA polymerase
Ethambutol - Cell Wall inhibitor
Isoniazid - Cell Wall inhibitor
Pyrazinamide - inhibits FA Synthetase
IsoNiazid
- BEST TB drug available
- Inhibition of synthesis enzymes for Mycolic acid via O2 dependent Catalase-Peroxidase reaction
- Bacteriostatic
- Reaches therapeutic levels in CSF + Caseous (Cheese) Necrosis
- Hepatotoxicity increases with age
Rifampin
- Bcteriocidal my blocking RNA Polymerase
- Efficacy Similar to Isoniazid
- Orange-Red Color of Excretions
- **No HIV
Ethambutol
- Bacteriostatic; unclear mechanism; Blocks Arabians-galactin, a component of mycobacterial cell wall
- AE: Green blindness, retrobulbar optic neuritis, headache, confusion, peripheral neuritis
Pyrazinamide
- Bactericidal
- similar to pyrazinamide acid
- AE: Hepatic dysfunction; Polyarthralgia; Hyperuricemia;Myalgia, and photosensitivity
Second line TB drugs
Aminoglycosides: Amikacins, Streptomycin, etc
Quinolones :Cipro, others
Hansen’s disease drugs (leprosy)
- Sulfones:
Dapsone: Most effective; Inhibits Folic Acid synthesis
Acedapsone: Alternative drug for Pneumocystic Pneumonia (Jirovecii)
Clofazimine: DNA Binding; Causes skin discoloration
Amphotericin B
- Polyene which forms pores in membrane
- Severe infections of Candida, Histoplasma, Cryptococcus, Neoformans, blast. Derm, Histo. Caps, Cocci. Imm, Paracocc, Asper, peni,
- AE: respiratory Stridor, Nephrotoxicity, Azotemia,
***Lipid formulations bind to mammalian membranes less readily therefore they reduce drug-induce renal repair
Flucytosine
- Fungistatic antimetabolite
- Systemic Candidas, cryptococcal infections, and chromomycosis
- AE: Reversible BM suppression + some GI effects
ImidAzoles + Triazoles
- Triazoles more slowly metabolized and have less effect on human sterol synthesis
- Azoles inhibits 14-a-demethylase which causes accumulation of sterols resulting in packing and inhibiting growth
- Ex. Ketoconazole, miconazole, Butoconazole, etc
Clotrimazole
- Topical or oral Azole; more pleasant taste than nystatin
- Mucosal + Cutaneous yeast infections
Miconazole
- Topical, Parenteral, and oral use Azole
- Cutaneous candidias + Vulvovaginitis caused by it.
- AE: Burnng, skin macerations, itching
Itraconazole
- Broad Spectrum antfungal
- Suppressive therapy histoplasmosis in HIV + Pts
Fluconazole
- Imidazole in immunocompromosed/immunocompetent patients
- Suppressive therapy and primary treatment of cryptococcal meningitis in AIDS patients; Treatment for Oral Candidas; Coccodioidal meningitis, Blastomycis, + Histoplasmosis
Ketoconazole
- oral or topical wide spectrum systemic Imidazole
- Oral candidias; Tinea; Many other fungi
- Metabolized by CYP3A4 - Terfenadine, astremizole, rifampin, phenytoin
- Endocrine abnormalities - loss of libido, gynecomastia, etc
Nystatin
- Similar to Amphotericin B
- Crypto; Candida, Hstoplasma, Blasto, Dermatop, Epidermo, Trichophy; Mcrosporum
- ALWAYS ORAL
- Mostly for candida infections of skin, mucosa (Thrush), vagina, and GI
- AE: Foul tase, Toxic parenteral; GI disturbance
Griseofulvin
- Fungistatic inhibitor of mitosis via spindle inhibition
- Systemic drug in disease of skin, hair, and nails
- Microsporum, Epidermophyton, trichophyton ONLY
- AE: Neurological disturbance, hepatic microsomal enzymes, hematologists disorders, and DIREC VASODILATOR
Echinocandins
- “Fungin”
- Anidulafungin: Fungicidal against candida + Aspergillus; inhibits Glucan synthase
- Micafungin: IV for esophageal candida, peritoneal abscesses, acute disseminated candidias; prophylaxis of patients undergoing hematopoietic stem cell transplant
- Caspofungin: Mucosal + Invasice candida, aspergillus, and Pneumocystis
Terbinafine
- Inhibits Fungal Squalene allylamine monoxygenase
- DEC risk of hepatotoxicity compared to itraconazole
- For Onychomycosis + Tinea Capitis
Other drugs for dermatophytes
Tolnafate
Naftifine
Undecylenic acid
Butenafine
