Exam 3 Drugs Flashcards
Accumulates in renal dysfxn
Isoniazid, Cycloserine
Broader/more potent that first azole.
Blastomycosis, sporotrichosis, paracoccidomycosis, histoplasmosis
capsule: acidic bev
soln: on empty stomach
Liver metab
BOX WARN: HF, Vent dysfxn
Itraconazole
This drug may cause optic neuritis due to higher doses of the medication or due to renal dysfxn.
Ethambutol
Enterohepatic cycling
Rifampin
First member azole but least active. Hepatotoxic, skin rash.
Good to tx mucocutaneous or vulvovaginal candida.
prophylaxis for bone marrow recipients/transplants with fungal infections
C. neoformans post-ampho/flu tx
Fluconazole
4 R’s
RNA poly. inh.
Revs P450
Red, orange
Rapid resistance used alone
Rifampin (a macrocyclic abx)
Do not take antacids with these
Quinolones, Methenamine, Isoniazid
First of the echinocandin class, and first line option for Candidiasis.
Second line option for invasive aspergillus. (For those pts who failed or couldn’t do an azole).
Increase dose w/P450 inducers like Rifampin
Caspofungin
Little difference between what is toxic and what is therapeutic
Corticosteroid/antipyeretic can be given before administration to prevent fever and chills.
K+/Magnesium supplements can help if cellular electrolyte leakage occurs causing hypokalemia, etc.
30-60 mins prior can also give Ibuprofen for associated pain with infusion
Heparin for possible thrombophlebitis preventing coagulation
Loading pt with sodium can minimize nephrotoxicity
Class of Abx need to monitor for with Amphotericin due to increased nephrotoxicity (aminoglycosides, vancomycin)
Things to remember for Ampho B
Used to treat tinea pedis (athlete’s foot), corporis(ring worm)
Tinea cruris (groin) x 1 week duration
Avoid: severe renal dysfxn, hepatic dysfxn, nursing mothers
Causes taste/visual disturbances, dyspepsia
Terbinafine
IV or PO (Same daily dose for IV or Oral because oral absorption is rapid and complete)
IV spared for pts unable to tolerate oral admin, amphotericin, etc
Use cautiously for liver dyfxn
Fluconazole
These are used first line for the tx of invasive candidiasis/candidemia.
These have an advantage because they hae no P450 interactions. Good for pts who had no other alternatives. Good for polypharmacy pts.
Anidulafungin and Micafungin
Used for dermatophytosis of scalp and hair; Fungistatic
1/per day dosing
Requires long duration of treatment, 6 to 12 months for onychomycosis. Pts need to be aware of the extent of tx.
Absorption is enhanced by high-fat meals
Contraindicated in pregnancy and porphyria (causes CNS effects - no sunbathing/tanning).
Griseolfulvin
When this is added to the TB tx regimen, it can cause 1-5% liver damage. Make sure to monitor liver fxn.
Pyrazinamide
Azoles inhibit CYP450 and are fungistatic agents. Explain how azoles interact with an inducer vs a substrate.
Inducers lower azole concentrations; azole inhibition of P450 will cause substrate retention
Prophylaxis for TB skin converters.
Bimodal distribution
Take on empty stomach if possible.
Isoniazid
This echinocandin is great especially for a pt who has severe hepatic dysfxn
Anidulafungin
Squalene epoxidase inhibitors like Terbinafine, naftifine, and butenafine are for cutaneous mycotic infections and are considered ____.
fungistatic
used as topicals for the most part
Like Terbinafine, these are used for topical treatment of tinea infections (corporis, cruris, pedis)
Naftifine and Butenafine
This drug inhibits fungal DNA synthesis/protein synthesis.
Available in various forms: shampoo, gel, cream, soln. Can be applied like a nail polish too.
1% shampoo tx for seborrheic dermatitis.
Cream, gel, suspension: Tinea pedis, cruris, corporis, versicolor; Cutaneous Candida
Cicloporox
This causes red-bron skin discoloration
Clofazimine
In RIPE therapy, if you suspect resistance is an issue what do you do?
Add Streptomycin to RIPE regimen.
Synthetic broad agent
Invasive aspergillosis, candidiasis, other serious infections
oral, IV
CYP450 (elimination)
inhibitor and substrate of P450
Visual/auditory hallucinations (concentration dependent)
Cyclosporine, phenytoin, triazolam, warfarin (toxicity caused)
Voriconazole
“Vori said she sees and hears things! spooky!”
For antimycobacterial tx of MAC in an HIV pt, what options are there?
Respiratory quinolones can be helpful. Azithromycin is preferred in combination with ethambutol + rifabutin for MAC (azithromycin doesn’t interfere with antiretrovirals).
Eye issues with TB tx
Optic neuritis (2 drugs)
Uveitis (1 drug)
Red/green color blindness (1 drug)
Make sure to get a baseline for ocular fxn before starting tx.
Optic neuritis (Isoniazid, ethambutol)
Uveitis (rifabutin)
Red/Green (ethambutol)
DOC for treating dermatophyte onychomycoses and tinea capitis
PO oral route needed for these two cases
Terbinafine
Commonly used to tx Candida and aspergillus (esp. in immunocompromised pts)
Oral susp tab, IV (take w food)
Glucoronidation (elimination)
Statin, citalopram, risperidone contraindications
Hepatotoxic
Posaconazole
Peripheral neuropathy, hepatitis
Injures neurons, hepatocytes
Isoniazid
An advantage of Rifapentine?
It has a longer half-life than rifampin and can be administered once a week. (Given 2x a week during the intensive phase).
Hypae distorter; fungistatic
NOT good for candida
Tx for Tinea pedis, cruris, corporis
1% soln, cream, powder
OTC and easy to p/u (be careful to counsel pts about these products that they are treating the right things appropriately).
Tolnaftate
For aspergilosis
Prodrug, IV, Oral (capsules)
Long half-life (130hrs), given in cycles
inhibitor and substrate of P450
Isavuconazole
Bone-marrow depression (chemo/radiation pts – be careful these meds also depress the bone marrow).
Lot of monitoring with these medications, this and amphotericin, to avoid adverse effects.
Amphotericin B and Flucytosine
“LIFTNAHHR” for the side effects of Ampho B
Low therapeutic index, injection site pain, fever/chills, NV/D/malaise, Anemia/arthralgia/myalgia, HA, Hypotension, Thromboplebitis, Renal Impairment
Topical azoles
Imidazoles
“ICE” for drugs that you need to have B6 supplementation
Isoniazid, Cycloserine, Ethionamide
Treats a variety of topical conditions: Tinea corporis, Tinea cruris, Tinea pedis, Oropharyngeal and vulvovaginal candidiasis.
Topical use associated with contact dermatitis, vulvar irritation and edema.
Thrush: Cotrimazole (lozenge); Miconazole (buccal)
Oral ketoconazole is rarely used anymore due to severe liver injury; adrenal insufficiency
Imidazoles
Azoles for cutaneous and/or systemic infections
Triazoles
Used in combination with Amphotericin B for the treatment of systemic mycosis and meningitis caused by C. neoformans and C. albicans. Almost never used alone due to resistance.
Flucytosine
Drug of choice for several life threatening mycoses (Candida albicans, histoplasma capsulatum, cryptococcus neoformans, protozoal infections).
Slow, IV infusion
Liposomal preps have decreased renal infusion toxicity
Amphotericin B
Polyene antifungal used for cutaneous and oral Candida.
Fungistatic/cidal
Not absorbed from the GI tract. Not used parenterally due to systemic toxicity.
Oral swish and swallow/spit agent for thrush.
Intravaginal for vulvovaginal candida. Topical for cutaneous.
Nystatin
Which drug can be considered to tx pneumonia caused by Jiroveci in HIV pts?
Dapsone
These are teratogenic and should be avoided in pregnancy unless the benefit outweighs the risk to fetus.
Azoles
Can be used solely for Candida urinary tract infections when fluconazole is not appropriate. Resistance still an issue
Flucytosine
“Right Now The Heat Burns” to remember the side effects of Flucytosine
Reversible Neutropenia, Thrombocytopenia, Hepatic Dys Fxn, Blood marrow depression
Other: serious enterocolitis
These drugs are antifungal cell wall inhibitors used to treat azole resistant apergillus, and candida (most species).
Given IV once daily. Has histamine/flush rxn when too rapid.
Echinocandins (end in ~fungin)
These two TB drugs can cause urate retention causing problems in gout patients.
Pyrazinamide and Ethambutol
