SYSTEMIC PHARM Flashcards

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1
Q

oral antifungal drugs

A

⦁ Griseofulvin
⦁ Terbinafine (Lamisil) = allylamine class
⦁ Itraconazole (Sporanox) = triazole class

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2
Q

terbinafine (Lamisil) is which antifungal class

A

allylamine = fungicidal

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3
Q

1st line therapy for fungal scalp infection

2nd line therapy for fungal scalp infection

A

1st = griseofulvin

2nd = terbinafine (Lamisil)

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4
Q

1st line therapy for nail scalp infection

2nd line therapy for nail scalp infection

A

1st = terbinafine (Lamisil)

2nd = itraconazole (sporanox)

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5
Q

duration of treatment for tinea capitis

A

griseofulvin x 8 weeks

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6
Q

MOA OF GRISEOFULVIN

A

FUNGISTATIC - inhibits fungal cell division

griseofulvin binds to keratin and makes keratin resistant to fungal invasion

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7
Q

GRISEOFULVIN IS FUNGI___________

A

STATIC

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8
Q

how to take griseofulvin

A

take with food to lessen GI upset

taking with a fatty meal can help increase absorption

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9
Q

Griseofulvin is deposited in the keratin layer of skin, hair and nails, and concentrates in the

A

liver, fat & skeletal muscle

metabolized in the liver

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10
Q

do you have to check LFTs while on griseofulvin

A

if being used > 8 weeks, check LFTs

monitor CBC
renal & hepatic function if on griseofulvin for long term

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11
Q

microsize vs ultramicrosize griseofulvin

A

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

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12
Q

Griseofulvin Contraindications

A
  • liver failure
  • porphyria
  • pregnancy (CATEGORY X)
  • breastfeeding (not recommended)
  • use with caution if hx of PCN allergy
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13
Q

use griseofulvin with caution in pts with

A

hx of pcn allergy; potential for cross reactivity

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14
Q

drugs that can induce lupus

A
procainamide
hydralazine
isoniazid
methyldopa
griseofulvin
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15
Q

ADVERSE REACTIONS OF GRISEOFULVIN

A

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

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16
Q

griseofulvin drug interactions

which drugs in particular

A

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
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17
Q

griseofulvin monitoring

A

CBC

- renal & liver function if on long term therapy

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18
Q

terbinafine MOA

A

fungicidal

creates an ergotamine deficiency within fungal cell wall, leading to fungal cell death

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19
Q

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

A

terbinafine

griseofulvin

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20
Q

griseofulvin distributes to the

A

hair, skin and nails

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21
Q

terbinafine distributes to the

A

skin & sebum

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22
Q

Multiple drug interactions with terbinafine including

A

metoprolol & tramadol

**THINK BETA BLOCKERS

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23
Q

drug interactions with beta blockers, such as tramadol & metoprolol

A

terbinafine (Lamisil)

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24
Q

obtain AST/ALTs prior to starting therapy on

A

terbinafine (Lamisil)

repeat if using for > 6 weeks

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25
Q

side effects of Lamisil

A

headache
diarrhea
elevated LFTs
altered sense of smell / taste

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26
Q

Lamisil monitoring

A

CBC
AST/ALTs prior to starting Lamisil, repeat if using for > 6 weeks
assess for changes to smell and/or taste

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27
Q

terbinafine for tinea capitis

2nd line for tinea capitis after griseofulvin

A
  • 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)
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28
Q

terbinafine for onychomycosis

  • cure rate
  • which patients would you give terbinafine to for onychomycosis
A
  • 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
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29
Q

terbinafine dosing for fingernails vs toenails

A
  • fingernails = 250mg x 6 wks

- toenails = 250mg x 12 wks

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30
Q

ITRACONAZOLE (SPORANOX) BBW

A

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.

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31
Q

itraconazole has a higher cure rate for ____________ therapy vs _________ therapy

A

higher cure rate with pulse therapy vs with continuous therapy

itraconazole (sporanox) = 2nd line therapy for onychomycosis

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32
Q

can cause altered sense of smell / taste

A

terbinafine (Lamisil)

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33
Q

contraindications to itraconazole

A

ventricular dysfunction
CHF
pregnancy

Concomitant use of other drugs that inhibit the CYP450 system

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34
Q

use with caution if hx of PCN allergy

A

griseofulvin

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35
Q

how to take itraconazole (sporanox) capsules vs solution

A

take capsules with food = better absorbed

take solution on an empty stomach

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36
Q

LOTS OF DRUG INTERACTIONS for itraconazole and other azole antifungals

  • drug interactions such as with
A

PPIs, anxiolytics, pain meds, antiplatelets (Plavix / aspirin), antihypertensives, statins, etc.

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37
Q

adverse effects of itraconazole (sporanox)

A
⦁	Nausea
⦁	diarrhea
⦁	edema
⦁	headache
⦁	rash
⦁	abnormal LFTs
⦁	heart failure
⦁	arrhythmia
⦁	hearing loss
⦁	many more!
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38
Q

monitoring for itraconazole (sporanox)

A

⦁ baseline LFTs, then monthly if long term therapy

⦁ serum itraconazole concentrations - draw 2 weeks after starting therapy, regardless of when last dose was taken

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39
Q

so baseline LFTs are obtained for which drugs

A

terbinafine & itraconazole

check again for terbinafine if on > 6 weeks

check monthly for itraconazole if on long-term

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40
Q

itraconazole dosing: continuous vs pulse therapy

A

o Continuous or Fixed
⦁ fingernails = 200mg qd x 6 wks
⦁ toenails = 200mg qd x 12 wks

o Pulse therapy
⦁ fingernails = 200mg BID x 1 wk/month x 2 months
⦁ toenails = 200mg BID x 1wk/month x 3 months

41
Q

First line therapy for the treatment of androgenic alopecia in men

A

Finasteride (Propecia)

42
Q

Finasteride (Propecia) MOA

A

5-alpha-reductase inhibitor
Ultimately inhibits the conversion of testosterone to dihydrotestosterone

Same as Proscar (used for BPH), but a lower dose

43
Q

Finasteride & PSA levels

A

5-alpha-reductase inhibitors decrease the PSA by about 50%, so in patients taking finasteride for ≥6 months, remember to double the PSA when comparing to normal (untreated) values

44
Q

Finasteride monitoring

A

obtain baseline PSA levels
re-check in 6 months

if PSA increases while on this med, refer to urology

if PSA doesn’t decrease by about 50% after 6 months of therapy, may indicate an increased risk for prostate cancer

45
Q

efficacy of finasteride (propecia)

A
  • after 2 years of therapy, hair counts may increase by about 25%
  • mostly used to maintain the hair they have left, because it only increases hair count slightly
46
Q

side effects of finasteride

A
⦁	sexual dysfunction (decreased libido, ejaculatory dysfunction, ED)
⦁	gynecomastia
⦁	testicular pain
⦁	depression
⦁	orthostatic hypotension
⦁	dizziness
⦁	weakness
47
Q

women of childbearing age should avoid contact with crushed or broken tablets of finasteride, because it is

A

TERATOGENIC!!!

48
Q

most common SE of finasteride

A

sexual dysfunction
orthostatic hypotension
dizziness
weakness

49
Q

finasteride metabolism

A
  • hepatic metabolism
  • caution for drug interactions
  • DON’T USE IN LIVER FAILURE
50
Q

finasteride dosage

A

1mg daily. Continuous dosing for a minimum of 1 year before assessment for efficacy.

Maximal results at 2 years

  • a much lower dose is used for alopecia (1mg qd) vs for BPH (5 mg qd)
51
Q

wait until _______ of therapy of finasteride before assessing efficacy

maximal results are seen at _________

A

1 year

max results at 2 years

52
Q

oral antibiotics used in derm

A
⦁	Cephalexin (Keflex)
⦁	Mupirocin (Bactroban)
⦁	Doxycycline
⦁	Minocycline (Minocin)
⦁	Clindamycin
53
Q

cephalexin (Keflex) distribution

A
  • 1st gen cephalosporin (beta-lactam antibiotic)
  • for skin / skin structure infections
  • Distribution = widely distributed to all body tissues, except does NOT penetrate the CSF well
54
Q

cephalexin (Keflex) is widely distributed to all body tissues, except

A

does NOT penetrate the CSF well

55
Q

dosage of keflex

A

⦁ skin / skin structure infections = 500mg Q6hrs

⦁ furunculosis & skin abscess = 250mg Q6hrs

56
Q

what bugs does Keflex cover

A

⦁ staph

⦁ strep

57
Q

Keflex pregnancy category

A

B (safe-ish!)

58
Q

MOA of keflex

A

inhibits bacterial cell wall synthesis

inhibits bacterial cell wall synthesis by binding to one or more of the Penicillin-binding proteins (PBPs) which in turn inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls –> inhibits cell wall biosynthesis

59
Q

Keflex & renal dysfunction

A

Decrease keflex dose for severe renal impairment (CrCl < 10mL/min)

can still take Keflex with renal impairment, just have to lower the dose

60
Q

indications for mupirocin (Bactroban)

A

⦁ Impetigo (due to staph & strep) = ointment TID x 3-5 days

⦁ Treat secondarily infected skin lesions due to staph or strep = cream TID x 10 days

⦁ Intranasal to eradicate MRSA = BID x 5 days (use intranasal formula)

impetigo = ointment
2ndary infections = cream
intranasal MRSA = intranasal formula

61
Q

inhibits protein synthesis by binding to isoleucyl transfer-RNA synthetase

inhibits bacterial protein & RNA synthesis

A

mupirocin (Bactroban)

inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis.

62
Q

absorption of mupirocin

A

topical ointment & cream penetrates the outer layers of skin with some minimal systemic absorption

  • Intranasal - about 3% of what is applied is systemically absorbed in adults, but can be significant in neonates
63
Q

MOA OF TETRACYCLINES

A

Inhibition of protein synthesis by binding with the 30S ribosomal subunit (and possibly the 50S) of susceptible bacteria, may also cause alterations in the cytoplasmic membrane

64
Q

SE OF TETRACYCLINES

A

photosensitivity

65
Q

SE of doxycycline

A

nausea if taken on an empty stomach
can cause esophagitis if not taken with fluids
photosensitivity

66
Q

Absorption of Doxy may be delayed with

A

achlorydia (high pH)

67
Q

indications for doxy

A

⦁ Tick-borne rickettsial infections
⦁ Acne
⦁ Rosacea
⦁ off label when 1st line therapy is unavailable = animal & human bites, cellulitis secondary to MRSA, skin & soft tissue infections

68
Q

indications for minocycline

A

⦁ acne

⦁ off-label = MRSA cellulitis

69
Q

SE of minocycline

A

⦁ vertigo (especially at higher doses)
⦁ esophagitis if not taken with water (just like doxy)
⦁ GI upset if taken on an empty stomach (just like doxy)

70
Q

which acne antibiotic is associated with the most resistance

A

ERYTHROMYCIN

71
Q

reducing antibiotic resistance when treating acne

A
  • most resistance is associated with Erythromycin
  • to reduce abx resistance, start Benzoyl Peroxide 5 days prior to abx therapy, and continue during abx therapy
  • If BP not an option, note increased efficacy if using a topical retinoid + oral abx therapy
  • try to limit abx to 12-18 weeks
  • don’t change therapy too quickly (evaluate after 6-8 weeks, don’t give up after just a few weeks)
  • don’t give the same antibiotic in topical & oral form (ex: clindamycin)
72
Q

derm indications for clindamycin

A

⦁ Acne

⦁ Rosacea

73
Q

Avoid oral clindamycin for treatment of acne due to risk of

A

C. dif

74
Q
  • for treatment of severe, recalcitrant, nodular acne
  • Acne with many inflammatory nodules (greater than 5 mm) that is unresponsive to conventional therapy, including systemic antibiotics
A

Accutane (isotretinoin)

75
Q

Accutane MOA

A

⦁ shrinks sebaceous glands
⦁ decreases sebum production
⦁ decreases the number of sebum dependent bacteria Propionibacterium acnes

76
Q

The only acne medication that can permanently alter the natural course of the disorder

A

accutane

77
Q

duration of accutane

A

duration of therapy = 15-20 weeks
can discontinue sooner if the cyst count is decreased by > 70%
if a second course of therapy is necessary, it is of a shorter duration

78
Q

requirements with Accutane due to high risk of birth defects

A

EXTREMELY HIGH RISK OF BIRTH DEFECTS…

  • 2 forms of birth control required - have to have started at least 1 month prior to rx
  • 2 negative pregnancy tests prior to initial prescription
  • pregnancy test & counseling once a month
  • need to be a registered prescribed in IPledge program and document expertise in prescribing isotretinoin per FDA regulations
79
Q

ACCUTANE SIDE EFFECTS

A

⦁ cheilitis
⦁ dry skin & mucous membranes
⦁ epistaxis
⦁ desquamation
⦁ photosensitivity
⦁ pruritus
⦁ ocular symptoms related to dysfunction of meibomian glands within conjunctiva –> can lead to corneal abrasion
⦁ more prone to cutaneous staph infections (paronychia, pyogenic granulomas)
⦁ temporary diffuse alopecia or nail brittleness
⦁ depression
⦁ hypertriglyceridemia (up to 45% of pts, Alcohol may potentiate this rxn)
⦁ elevated total & LDL cholesterol (up to 30%)

  • these SE usually resolve after discontinuation of the drug
80
Q

baseline Accutane labs

A
⦁	CBC with diff
⦁	ESR
⦁	fasting glucose
⦁	CPK
⦁	Pregnancy test x 2 (2nd test done 19 days after 1st test, and within 7 days of starting rx and within first 5 days of menstrual cycle)
⦁	LFTs
⦁	Lipid panel
81
Q

Accutane monitoring

A
  • monthly pregnancy test - until 1 month after d/c therapy
  • monthly CBC & glucose
  • weekly or biweekly Fasting LP & LFTs x first 4 weeks, then monthly
82
Q

DISCONTINUE ACCUTANE IF…

A

⦁ TG > 800

⦁ LFTx 3x the upper limit of normal

83
Q

retinoid acid derivative

A

accutane

84
Q

topical calcineurin inhibitors

A

Tacrolimus (Protopic)

Pimecrolimus (Elidel)

85
Q

indications for topical calcineurin inhibitors

A

⦁ atopic dermatitis
⦁ lichen planus
⦁ vitiligo
⦁ psoriasis

86
Q

BLACK BOX WARNING FOR topical calcineurin inhibitors

A
  • associated with rare cases of malignancy (skin cancer & lymphoma) - so should be limited to short-term and intermittent treatment using the minimum amount necessary for control of symptoms and only in involved areas
87
Q

BLACK BOX WARNING FOR topical calcineurin inhibitors = associated with rare cases of malignancy = __________ & _____________

A

skin cancer & lymphoma

88
Q

DO NOT USE TOPICAL CALCINEURIN INHIBITORS WHEN….

A

1) patient is < 2
2) patient is on systemic immunosuppressant (cyclosporine)
3) patient is immunocompromised

89
Q

MOA of topical calcineurin inhibitors

A

suppresses cellular immunity - by inhibiting T-lymphocyte activation; binds to an intracellular protein to inhibit calcineruin phosphatase activity

90
Q

Concomitant __________ with topical calcineurin inhibitors can cause redness & flushing

A

alcohol ingestion

so avoid TCIs with alcohol

also, sun protection recommended

91
Q

do NOT use topical calcineurin inhibitors under an

A

occlusive dressing!

it is a topical medication, but has enough systemic absorption to cause malignancy and interact with alcohol, so don’t occlude

92
Q

SE OF TACROLIMUS (PROTOPIC)

A
  • headache (20%)
  • skin burning at application site (58%)
  • pruritus (46%)
  • erythema (28%)
93
Q

ELIDEL (PIMECROLIMUS)

A
  • less burning reaction than with protopic
  • cream
  • 1 strength = 1%
94
Q

which topical calcineurin inhibitor has less burning SE

A

elidel

95
Q

drug induced lupus symptoms

A
  • arthralgia
  • myalgia
  • fever
  • malaise
  • rash
  • serositis

usually are on the drug for 1 month or more

multiple drugs can be responsible for drug-induced lupus

96
Q

mainstay of therapy for drug induced lupus

A

d/c drug

NSAIDS for symptom relief

Usually spontaneous resolution of clinical manifestations of the disease within several weeks to months after discontinuing the causative drug

97
Q

If drug-induced lupus symptoms don’t resolve within 4-8 weeks = give

A

HYDROXYCHLOROQUINE

98
Q

if drug-induced lupus symptoms are SEVERE or if quick relief is needed (like pleurisy or pericarditis) = give

A

systemic corticosteroids