ANTI TUBECULAR ANIBIOTICS- LEVO Flashcards
(107 cards)
1
Q
- obtained from Streptomyces
mediterranei - includes Rifampin and Rifabutin
A
RIFAMYCINS
2
Q
- Rifadin, Rimactane, Rifampicin
- the most active agent against TB
- enzyme INDUCER toxic effects are relatively infrequent
A
RIFAMPIN
3
Q
- when it is taken in combination with INH or
ethambutol, incidence of HEPATOTOXICITY is
significantly higher - S/E: reddish color of body secretions,hepatotoxicity
A
RIFAMPIN
4
Q
First Line Treatment for TB
A
- Rifampin
- Isoniazid
- Pyrazinamide
- Ethambutol
- Streptomycin
5
Q
PTB =
A
2 mos (RIPE w/ or w/o S)
6
Q
- Seromycin®
A
Cycloserine
7
Q
- isolated from different species of Streptomyces: S. orchidaceus, S. garyphalus, S. lavendulus
- MOA: prevents the synthesis of cross-linking peptide in the formation of bacterial cell walls
A
Cycloserine
8
Q
- isolated from Streptomyces
capreolus
A
Capreomycin
9
Q
- only aminoglycosides used for
tuberculosis - the first antibiotic effective in the treatment of TB (1944 by Waksman)
A
Streptomycin
10
Q
- study of fungi
A
MYCOLOGY
11
Q
studied Trichophyton schoenleinii (1839)
A
Schonlein & Gruby
12
Q
- reported the yeast-
like microorganism responsible for oral thrush (Candida albicans)
A
Langenbeck
13
Q
2 Groups of Fungal Infections
A
- Superficial mycoses
- Deep-seated mycoses
14
Q
- most common
- caused by dermatophytes
- includes tinea or ringworm
infections and Candida
infections
A
SUPERFICIAL MYCOSES
15
Q
Ringworm Infections:
A
- Tinea capitis
- Tinea barbae
- Tinea faceie
- Tinea cruris
- Tinea pedis
- Tinea manum
- Tinea ungium (Onchomycosis)
- Pityriasis versicolor
16
Q
SYSTEMIC MYCOSES
A
- Histoplasmosis
- Sporotrichosis
- Blastomycosis
- Coccidioidomycosis
- Cryptococcosis
- Paracoccidioidomycosis
17
Q
Opportunistic Fungal Infections
A
- Systemic candidiasis
- Aspergillosis
- Mucormycosis
- Pneumocystis carinii
18
Q
Cutaneous Infections
(Dermatophytoses)
A
- Microsporum
- Trichophyton
- Epidermophyton
- Malassezia furfur
19
Q
- refers to a group of fungal diseases in which both the skin and subcutaneous tissue are involved but typically no dissemination to the internal organ occurs
A
Subcutaneous Fungal Infections
20
Q
- tinea or ringworm
A
Dermatophytoses
21
Q
acidic, fatty substance in
and on the skin; functions as a
natural antifungal agent and part of the innate immune system
A
Sebum
22
Q
- an antifungal agent that is non-irritating and nontoxic
A
Propionic Acid
23
Q
- unstable to moisture, forming zinc hydroxide and propionic acid
- used as fungicide, particularly on adhesive tape
A
Zinc Propionate
24
Q
- used topically to treat superficial dermatomycoses caused by C. albicans and Trichophyton, Epidermophyton and Microsporum spp.
- from caprylic acid found in coconut or palm oil
A
Sodium Caprylate
25
* 10-Undecenoic acid
* obtained from the destructive
distillation of castor oil
* can be used in concentrations up to 10%
* traditionally used **for athlete's foot**
Undecylenic Acid
26
* activity is due to acetic acid
released by hydrolysis of the
compound by esterases present in the skin
Triacetin
27
* has both antiseptic and keratolytic properties
* a **poor antifungal agent**
Salicylic Acid
28
* contains 6% benzoic acid and 6% salicylic acid in a petrolatum base
* benzoic acid cannot penetrate the outer layer of the skin in infected areas thus used with keratolytic agents
Whitfield's Ointment
29
* used as a 1% cream for the treatment of superficial tinea infections
* lesion typically worsens before it improves
* iflammation and painful irritation are common
Haloprogin
30
* Vioform®
* 3% ointment or cream is used
as a treatment for **Trichomonas vaginalis** vaginitis
* Vioform HC® - combination with hydrocortisone
Clioquinol
31
* Vioform®
Clioquinol
32
* an agent of choice for cutaneous candidiasis, tinea corporis, tinea cruris, tinea pedis and tinea versicolor
* **second-line treatment for onychomycosis**
* MOA: at **low** concentrations, it blocks transport of amino acids into the cells; at **high** concentrations, membrane integrity is lost and cellular contents leak out
Ciclopirox Olamine
33
* Ancobon®
Flucytosine
34
* used only in combination with
Amphotericin B for the treatment of systemic mycoses and meningitis caused by ***Cryptococcus neoformans and Candida*** (synergistic)
* MOA: release 5-FU
Flucytosine
35
* Amphotericin B
* Nystatin
* Natamycin
POLYENES
36
* Fungizone®
* naturally occuring, produced by Streptomyces
nodosus
AMPHOTERICIN B
37
* MOA: binds to ERGOSTEROL present in the cell membrane disrupting membrane function, allowing electrolytes to leak out from the cell, resulting in cell death
AMPHOTERICIN B
38
* drug choice for systemic mycoses (disseminated forms of coccidioidomycosis, North American blastomycosis, cryptococcosis, histoplasmosis,
mucormycosis, aspergillosis and sporotrichosis)
* S/E: Renal toxicity, acute febrile reaction, anemia, phlebitis
AMPHOTERICIN B
39
* Mycostatin®
* first isolated from a strain of
***Streptomyces noursei***
NYSTATIN
40
* used for the treatment of Candida (monilial) infections
* administered as an oral agent for the treatment of oral candidiasis.
* not absorbed systemically whenadministered orally
* swish and swallow
NYSTATIN
41
* Natacyn®
* obtained from ***Streptomyces natalensis***
* fungicidal and fungistatic at the same concentration range
* supplied as 5% ophthalmic suspension intended for the treatment of fungal conjunctivitis, blepharitis, and keratitis
NATAMYCIN
42
Grifulvin®
Grisactin®
Gris-PEG®
* obtained from the mold
***Penicillium griseofulvum***
Griseofulvin
43
* MOA: interacts with the microtubules within the fungus to disrupt the mitotic spindle and inhibit mitosis (arrests cell
division in metaphase)
* absorption is increased by FATTY FOODS
* compliance with the drug regimen is mandatory
Griseofulvin
44
MOA
* inhibits squalene epoxidase resulting to shutting down of biosynthesis of ergosterol and cause an accumulation of
squalene, which destablizes the fungal cell membrane
ALLYLAMINES AND
RELATED COMPOUNDS
45
* Naftin®
* supplied in a 1% concentration in a cream and in a gel for the topical treatment of ringworm, athlete's foot and jock itch
NAFTIFINE
46
* Lamisil®
* available in 1% cream for topical administration for the treatment of tinea pedis, tinea corporis, and tinea cruris
TERBINAFINE
47
* Tinactin®, Aftate®, NP-27®
* not an allylamine but has MOA the same with allylamine compounds
* formulated into preparations
intended to be used with artificial fingernails to counteract the increased chance of ringworm of the
nail beds
TOLNAFTATE
48
* effective against most fungi that cause superficial infections of the skin and mucous membrane
* also exhibit activity against yeasts that cause systemic infections
MOA
* interacts with C-14-demethylase to block demethylation of lanosterol to
ergosterol, the principal sterol of fungal membranes. This inhibition disrupts membrane function and increases permeability
Antifungal Spectrum
49
Structure-Activity Relationships
* basic structural requirement for members of the azole class is a __________________________
* the most potent antifungal azoles possess _____________
Structure-Activity Relationships
* basic structural requirement for members of the azole class is a **weakly basic imidazole or 1,2,4- triazole ring**
* the most potent antifungal azoles possess **two or three aromatic rings**
50
* Lotrimin®, Mycelex®
* a broad-spectrum antifungal drug that is used topically for the **treatment of tinea
infections and candidiasis**
* 1% vaginal cream and tablets of 100 mg and 500 mg for vulvovaginal candidiasis
* extremely stable, with a shelf-life of more than 5 years
CLOTRIMAZOLE
51
* Spectazole®
* 1% cream for the topical treatment of local tinea infections and cutaneous candidiasis
ECONAZOLE
52
* Femstat®
* supplied as vaginal cream intended for vaginal candidiasis
BUTOCONAZOLE
53
* Exelderm®
* supplied in 1% concentration for the treatment of **local tinea infections**, such as jock itch, athlete's foot, and
ringworm
SULCONAZOLE
54
* Oxistat®
* used in cream and lotion
dosage forms in 1% concentration for the
treatment of tinea infections
OXICONAZOLE
55
* Vagistat®
* used for the treatment of
vulvovaginal candidiasis
TIOCONAZOLE
56
* Monistat®, Micastin®
* used as treatment for tinea
infections and cutaneous
candidiasis, vaginal candidiasis
* can be used also for systemic
infections but can cause
thrombophlebitis, pruritis, fever
and GI upset
MICONAZOLE
57
* Nizoral®
* a broad-spectrum antifungal that isadministered orally for the treatment of systemic fungal infections
* inhibits androgen and andrenal steroid synthesis
* has endocrine effects: gynecomastia, decreased libido, impotence, and menstrual irregularities
* absorption is increased with **acidic foods**
KETOCONAZOLE
58
* recommended for the treatment of the following systemic infections:
candidiasis (oral thrush and chronic mucocutaneous form),
coccidioidomycosis, blastomycosis, histoplasmosis, chromomycosis and
paracoccidioidomycosis
KETOCONAZOLE
59
* used orally to treat severe refractory cutaneous dermatophytic infections
not responsive to topical therapy and oral griseofulvin
* used topically in 2% concentration in a cream and shampoo for the management of cutaneous candidiasis and tinea infections
* S/E: (additional) hepatotoxicity
KETOCONAZOLE
60
* Terazol®
* used exclusively for the control of vulvovaginal moniliasis caused by ***Candida spp.***
* available in creams containing 0.4% and 0.8% of the free base intended for 7-day and 3-day treatment periods, respectively
TERCONAZOLE
61
* Sporanox®
* an orally active, broad-spectrum antifungal agent that has become an important **alternative to ketoconazole**
* lacks the endocrinologic effects of ketoconazole
ITRACONAZOLE
62
* DOC for tinea ungium
ITRACONAZOLE
63
* Diflucan®'
* administered orally and intravenously
* has excellent penetrability into the CSF
FLUCONAZOLE
64
drug of choice for Cryptococcal meningitis (Cryptococcus neoformans) -can be diagnosed through negative staining using Negrosin ink/India ink
FLUCONAZOLE
65
* can be acquired through pigeon droppings
* HIV patients (+ headache)
Cryptoccocal Meningitis
66
for subcutaneous and SYStemic fungal infections
**KIF SYS**
* Ketoconazole, Itraconazole,
Fluconazole
67
for SUPerficial mycoses
**MEC SUP**
* Miconazole, Econazole,
Clotrimazole
68
Newer Antifungal Agents
* Voriconazole
* Posaconazole
69
MOA
* act as non-competitive inhibitors of (1,3)--d-glucan synthase, an enzyme
complex that forms stabilizing
glucan polymers in the fungal cell wall
Echinocandins and
Pneumocandins
70
* Capsebon®
* supplied as shampoo for the
treatment of dandruff or
seborrheic dermatitis
Caspofungin
71
* produced from ***Aureobasidium pullulan***
MOA: acts as a tight-binding non- competitive inhibitor of the enzyme inositol phosphorylceramide synthase (IPC synthase), which is an essential enzyme for fungal
sphingolipid biosynthesis
AUREOBASIDINS
72
Common Pathogenic Protozoa:
* Entamoeba histolytica
* Balantidium coli
* Giardia lamblia
* Trichomonas vaginalis
* Pneumocystis carinii (now a fungi)
* Toxoplasma gondii
* Trypanosoma cruzi
* Trypanosoma brucei
* Leishmania donovani (Kala-azar)
73
* Flagyl®, Protostat®, Metro IV®
* the most useful nitroimidazole derivative for Amoebiasis, Trichominiasis and Giardiasis
* also has antibacterial activity
* S/E: disulfiram-like effect, metallic after- taste
* MOA: formation of reactive intermediate that binds to the DNA of microorganism
METRONIDAZOLE
74
* used in the treatment of asymptomatic carriers of ***Entamoeba histolytica***
DILOXANIDE
75
* recommended for acute and chronic intestinal amebiasis but is not effective in extraintestinal disease
* S/E: neuropathy
Iodoquinol
76
* obtained by extraction from ipecac (Caephalis ipecacuanha)
* MOA: inhibits protein synthesis in protozoal and
mammalian cells by preventing protein elongation
* S/E: severe GI distress, CV diseases,neuromuscular effects
* I: Amoebiasis, balantidial dysentery, fluke infestations (fascioliasis, paragonimiasis)
Emetine & Dehydroemetine
77
* NebuPent®, Pentam 300®
* used for the treatment of pneumonia caused by the opportunistic pathogenic
protozoan P. carinii, a frequent secondary invader associated with AIDS
* used for the prophylaxis and treatment of ***African trypanosomiasis and visceral
leishmaniasis***
PENTAMIDINE
78
* Mepron®
* MOA: may act as antimetabolite and interfere with the function of electron
transport enzymes
* S/E: GI distress
* originally for malaria but now used against P. carinii (alternative for TMP-SMX)
ATOVAQUONE
79
* used for the treatment of West African sleeping sickness, caused by ***Trypanosoma brucei gambiense***
* Indicated for the
meningoencephalitic stage of the disease
* S/E: myelosuppression (anemia, leukopenia, thrombocytopenia)
EFLORNITHINE
80
* Lampit®
* used for the treatment of South American trypanosomiasis caused
by ***Trypanosoma cruzi*** (Chagasdisease)
NIFURTIMOX
81
* Radanil®, Rochagan®
* used in the treatment of Chagas Disease
BENZNIDAZOLE
82
* Mel B®, Arsobal®
* DOC for the treatment of the later stages of both forms of African trypanosomiasis
* should be monitored for signs of arsenic toxicity
MELARSOPROL
83
* Pentostam
* a pentavalent antimonial compound intended primarily for the treatment of various forms of leishmaniasis
SODIUM STIBOGLUCONATE
84
* used as a long-term prophylactic agent for trypanosomiasis
* also used for prophylaxis of
onchocerciasis
SURAMIN
85
* are compounds used to control the mite Sarcoptes scabei, an organism that
thrives under conditions of poor personal hygiene
SCABICIDES
86
* are used to eliminate head,
body and crab lice
PEDICULICIDES
87
* obtained from Peru balsam and other resins
* immediate relief from itching
* complete cure is achieved with a single application of a 25% emulsion
* applied topically as lotion over the entire dampened body, except the face
BENZYL BENZOATE
88
* Eurax®
* available in 10% concentration in a lotion and cream intended for topical treatment of scabies
CROTAMITON
89
* derived from Crysanthemum plants
* MOA: nerve poisoning
PYRETHRIN
90
* enhances the pediculocide effects of pyrethrin
PIPERONYL BUTOXIDE
91
* for head lice only
* 10% shampoo
PERMETHRIN
92
* kwell
* Gamma-benzene hexachloride
* ADR: neurotoxicity
LINDANE
93
* Comprise a series of synthetic
antibacterial agents patterned after nalidixic acid (introduced for the treatment of UTI)
* 1,4-dihydro-4-oxo-3-pyridinecarboxylic acid moiety (essential for antibacterial
property)
QUINOLONES
94
DOC for pregnant women with
UTI
Penicillin & Cephalosporins
95
* NegGram®
* useful in the treatment of UTI in which Gram-negative bacteria predominate
* first generation quinolone
NALIDIXIC ACID
96
* Cinobac®
* same action and use with nalidixic acid but with greater oral bioavailability
CINOXACIN
97
* Noroxin®
* has broad-spectrum of activity against Gram-negative & Gram-positive bacteria
* I: UTI caused by E. coli, K. pneumoniae, Enterobacter cloacae, P. mirabilis, indole-
positive Morganella morganii, P.
aeruginosa, S. aureus, S. epidermidis and group D streptococci; single 800 mg
oral dose for uncomplicated gonorrhea
NORFLOXACIN
98
* Penetrex®
* I: UTI and sexually transmitted
diseases; approved for treatment of uncomplicated gonococcal urethritis and chancroid caused by Haemophilus ducreyi (single 400 mg dose)
* Short-elimination half-life dictates twice a day dosing for UTI
ENOXACIN
99
* Cipro®, Cipro IV®
* the **most potent fluoroquinolone**
* DOC for bacterial **gastroenteritis** caused
by Gram-negative bacilli
* used for respiratory tract infections such as bronchitis and pneumonia caused by
Gram-negative bacteria
* used for combating infections of the skin, soft tissues, bones and joints
CIPROFLOXACIN
100
Ciprofloxacin + Ceftriaxone =
DOC
for disseminated gonorrhea
101
* single dose Ciprofloxacin +
Doxycycline =
eradicates
gonococcal urethritis
102
* Floxin®, Floxin IV®
* resembles ciprofloxacin in its antibacterial spectrum and potency
* approved for the treatment of LRTI inc. bronchitis and pneumonia caused by
Gram-negative bacilli; pelvic inflammatory disease and highly active against gonococci and chlamydia
OFLOXACIN
103
recommended for the outpatient treatment of acute gonococcal urethritis
single 400 mg dose + doxycycline
104
* Maxaquin®
* only quinolone for which once daily oral dosing suffices
* causes the highest incidence of phototoxicity
* I: for acute bacterial exacerbation of chronic bronchitis causes by H.
influenzae, Moraxella catarrhalis, Streptococcus pneumoniae; prophylaxis
of infection following transurethral surgery; acute cystitis and chronic UTI
LOMEFLOXACIN
105
* newer fluoroquinolone
* exhibits higher potency against Gram-positive bacteria
* Has a long elimination half-life that permits once-a-day dosing for most indications
* Has impressive Gram-negative
bactericidal property
* Lowest phototoxicity incidence
SPARFLOXACIN
106
* newer fluoroquinolone
* L = Lungs (used for pneumonia)
LEVOFLOXACIN
107
