Anti-mycobacterial Agents/Antifungals

Question 1

Mycobacterium General

Answer 1

• 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

Question 2

First Line TB Drugs

Answer 2

RIPE

Rifampin - RNA polymerase
Ethambutol - Cell Wall inhibitor
Isoniazid - Cell Wall inhibitor
Pyrazinamide - inhibits FA Synthetase

Question 3

IsoNiazid

Answer 3

• 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

Question 4

Rifampin

Answer 4

• Bcteriocidal my blocking RNA Polymerase
• Efficacy Similar to Isoniazid
• Orange-Red Color of Excretions
• **No HIV

Question 5

Ethambutol

Answer 5

• Bacteriostatic; unclear mechanism; Blocks Arabians-galactin, a component of mycobacterial cell wall
• AE: Green blindness, retrobulbar optic neuritis, headache, confusion, peripheral neuritis

Question 6

Pyrazinamide

Answer 6

• Bactericidal
• similar to pyrazinamide acid
• AE: Hepatic dysfunction; Polyarthralgia; Hyperuricemia;Myalgia, and photosensitivity

Question 7

Second line TB drugs

Answer 7

Aminoglycosides: Amikacins, Streptomycin, etc

Quinolones :Cipro, others

Question 8

Hansen’s disease drugs (leprosy)

Answer 8

• Sulfones:

Dapsone: Most effective; Inhibits Folic Acid synthesis

Acedapsone: Alternative drug for Pneumocystic Pneumonia (Jirovecii)

Clofazimine: DNA Binding; Causes skin discoloration

Question 9

Amphotericin B

Answer 9

• 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

Question 10

Flucytosine

Answer 10

• Fungistatic antimetabolite
• Systemic Candidas, cryptococcal infections, and chromomycosis
• AE: Reversible BM suppression + some GI effects

Question 11

ImidAzoles + Triazoles

Answer 11

• 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

Question 12

Clotrimazole

Answer 12

• Topical or oral Azole; more pleasant taste than nystatin

- Mucosal + Cutaneous yeast infections

Question 13

Miconazole

Answer 13

• Topical, Parenteral, and oral use Azole
• Cutaneous candidias + Vulvovaginitis caused by it.
• AE: Burnng, skin macerations, itching

Question 14

Itraconazole

Answer 14

• Broad Spectrum antfungal

- Suppressive therapy histoplasmosis in HIV + Pts

Question 15

Fluconazole

Answer 15

• Imidazole in immunocompromosed/immunocompetent patients
• Suppressive therapy and primary treatment of cryptococcal meningitis in AIDS patients; Treatment for Oral Candidas; Coccodioidal meningitis, Blastomycis, + Histoplasmosis

Question 16

Ketoconazole

Answer 16

• 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

Question 17

Nystatin

Answer 17

• 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

Question 18

Griseofulvin

Answer 18

• 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

Question 19

Echinocandins

Answer 19

• “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

Question 20

Terbinafine

Answer 20

• Inhibits Fungal Squalene allylamine monoxygenase
• DEC risk of hepatotoxicity compared to itraconazole
• For Onychomycosis + Tinea Capitis

Question 21

Other drugs for dermatophytes

Answer 21

Tolnafate
Naftifine
Undecylenic acid
Butenafine