SYSTEMIC PHARM Flashcards
oral antifungal drugs
⦁ Griseofulvin
⦁ Terbinafine (Lamisil) = allylamine class
⦁ Itraconazole (Sporanox) = triazole class
terbinafine (Lamisil) is which antifungal class
allylamine = fungicidal
1st line therapy for fungal scalp infection
2nd line therapy for fungal scalp infection
1st = griseofulvin
2nd = terbinafine (Lamisil)
1st line therapy for nail scalp infection
2nd line therapy for nail scalp infection
1st = terbinafine (Lamisil)
2nd = itraconazole (sporanox)
duration of treatment for tinea capitis
griseofulvin x 8 weeks
MOA OF GRISEOFULVIN
FUNGISTATIC - inhibits fungal cell division
griseofulvin binds to keratin and makes keratin resistant to fungal invasion
GRISEOFULVIN IS FUNGI___________
STATIC
how to take griseofulvin
take with food to lessen GI upset
taking with a fatty meal can help increase absorption
Griseofulvin is deposited in the keratin layer of skin, hair and nails, and concentrates in the
liver, fat & skeletal muscle
metabolized in the liver
do you have to check LFTs while on griseofulvin
if being used > 8 weeks, check LFTs
monitor CBC
renal & hepatic function if on griseofulvin for long term
microsize vs ultramicrosize griseofulvin
2 formulations of Griseofulvin
- the smaller the particle size, the greater the bioavailability.
- So the ultramicrosize is less of a dose than microsize, but has a greater bioavailability, so need less of a dose of ultramicrosize
⦁ Microsize = 20-25 mg/kg/day
⦁ Ultramicrosize = 10-15 mg/kg/day
Griseofulvin Contraindications
- liver failure
- porphyria
- pregnancy (CATEGORY X)
- breastfeeding (not recommended)
- use with caution if hx of PCN allergy
use griseofulvin with caution in pts with
hx of pcn allergy; potential for cross reactivity
drugs that can induce lupus
procainamide hydralazine isoniazid methyldopa griseofulvin
ADVERSE REACTIONS OF GRISEOFULVIN
o Skin
⦁ photosensitivity
⦁ Erythema multiforme / SJS / TEN
o Liver
⦁ jaundice
⦁ elevated LFTs
o Bone Marrow
⦁ granulocytopenia
o Neuro
⦁ dizziness
⦁ headache
⦁ fatigue
o GI
⦁ nausea
⦁ vomiting
o Drug induced lupus like syndrome
griseofulvin drug interactions
which drugs in particular
warfarin, OCPs, barbiturates, alcohol, cyclosporine
- griseofulvin has multiple drug interactions
- metabolized through CYP1A2, CYP2C9, and CYP3A4
- beware in particular of Warfarin, OCPs, Alcohol, Barbiturates, Cyclosporine
griseofulvin monitoring
CBC
- renal & liver function if on long term therapy
terbinafine MOA
fungicidal
creates an ergotamine deficiency within fungal cell wall, leading to fungal cell death
Trials comparing griseofulvin to terbinafine
_____________ was superior for the treatment of infections from Trichophyton species
____________ was superior for the treatment of infections due to Microsporum
terbinafine
griseofulvin
griseofulvin distributes to the
hair, skin and nails
terbinafine distributes to the
skin & sebum
Multiple drug interactions with terbinafine including
metoprolol & tramadol
**THINK BETA BLOCKERS
drug interactions with beta blockers, such as tramadol & metoprolol
terbinafine (Lamisil)
obtain AST/ALTs prior to starting therapy on
terbinafine (Lamisil)
repeat if using for > 6 weeks
side effects of Lamisil
headache
diarrhea
elevated LFTs
altered sense of smell / taste
Lamisil monitoring
CBC
AST/ALTs prior to starting Lamisil, repeat if using for > 6 weeks
assess for changes to smell and/or taste
terbinafine for tinea capitis
2nd line for tinea capitis after griseofulvin
- approved for use in ≥ 4 years of age
- available in granules or tablets (ex: if can’t take griseofulvin and can’t swallow pills = give terbinafine granules and sprinkle onto non-acidic foods)
terbinafine for onychomycosis
- cure rate
- which patients would you give terbinafine to for onychomycosis
- greater efficacy & fewer SE than others
- 76% cure rate
- Patients who need Lamisil treatment
⦁ for cosmetic reasons (don’t like the way it looks)
⦁ have DM & onychomycosis
⦁ have a hx of lower extremity cellulitis & ipsilateral onychomycosis***
⦁ have pain or discomfort secondary to fungal infection
terbinafine dosing for fingernails vs toenails
- fingernails = 250mg x 6 wks
- toenails = 250mg x 12 wks
ITRACONAZOLE (SPORANOX) BBW
NEGATIVE INOTROPIC EFFECTS
Negative inotropic effects have been observed following intravenous administration. Discontinue or reassess use if signs or symptoms of heart failure (HF) occur during treatment.
itraconazole has a higher cure rate for ____________ therapy vs _________ therapy
higher cure rate with pulse therapy vs with continuous therapy
itraconazole (sporanox) = 2nd line therapy for onychomycosis
can cause altered sense of smell / taste
terbinafine (Lamisil)
contraindications to itraconazole
ventricular dysfunction
CHF
pregnancy
Concomitant use of other drugs that inhibit the CYP450 system
use with caution if hx of PCN allergy
griseofulvin
how to take itraconazole (sporanox) capsules vs solution
take capsules with food = better absorbed
take solution on an empty stomach
LOTS OF DRUG INTERACTIONS for itraconazole and other azole antifungals
- drug interactions such as with
PPIs, anxiolytics, pain meds, antiplatelets (Plavix / aspirin), antihypertensives, statins, etc.
adverse effects of itraconazole (sporanox)
⦁ Nausea ⦁ diarrhea ⦁ edema ⦁ headache ⦁ rash ⦁ abnormal LFTs ⦁ heart failure ⦁ arrhythmia ⦁ hearing loss ⦁ many more!
monitoring for itraconazole (sporanox)
⦁ baseline LFTs, then monthly if long term therapy
⦁ serum itraconazole concentrations - draw 2 weeks after starting therapy, regardless of when last dose was taken
so baseline LFTs are obtained for which drugs
terbinafine & itraconazole
check again for terbinafine if on > 6 weeks
check monthly for itraconazole if on long-term