Test 4 Flashcards
1
Q
aspart
A
- Insulin
- rapid bind
- allergy
- DM type 1, 2, pregnancy
2
Q
detemir
A
- Insulin
- long bind
- allergy
- DM type 1, 2, pregnancy
3
Q
glargine
A
- Insulin
- long bind
- allergy
- DM type 1, 2, pregnancy
4
Q
glulisine
A
- Insulin
- rapid bind
- allergy
- DM type 1, 2, pregnancy
5
Q
lispro
A
- Insulin
- rapid bind
- allergy
- DM type 1, 2, pregnancy
6
Q
NPH
A
- Insulin
- intermediate-length bind
- allergy
- DM type 1, 2, pregnancy
7
Q
regular crystallin insulin
A
- Insulin
- short bind
- allergy
- DM type 1, 2, pregnancy
8
Q
exenatide
A
-incretin-like agonist
-up glu-induced insulin release in beta cell, down glucagon from alpha cell
-
-DM type 2
9
Q
sitagliptin
A
-incretin-like (stops incretin degradation)
-up glu-induced insulin release in beta cell, down glucagon from alpha cell
-
-DM type 2. Oral!
10
Q
pramlintide
A
-amylin analog
-Up insulin by inhibiting glucagon & suppressing appetite
-
-DM Type 1, 2
11
Q
Chlorpropamide
A
- sulfonylurea
- Down K efflux->Up Ca in->Up insulin rls in pancreas.
- tachyphylaxis
- DM Type 2
12
Q
glipizide
A
- sulfonylurea 2nd gen
- Down K efflux->Up Ca in->Up insulin rls in pancreas.
- Less side fx, longer duration than 1st gen
- DM Type 2
13
Q
glyburide
A
- sulfonylurea 2nd gen
- Down K efflux->Up Ca in->Up insulin rls in pancreas.
- Less side fx, longer duration than 1st gen
- DM Type 2
14
Q
glimepiride
A
- sulfonylurea 2nd gen
- Down K efflux->Up Ca in->Up insulin rls in pancreas.
- Less side fx, longer duration than 1st gen
- DM Type 2
15
Q
tolbutamide
A
- sulfonylurea
- Down K efflux->Up Ca in->Up insulin rls in pancreas.
- tachyphylaxis
- DM Type 2
16
Q
tolbutamide
A
- sulfonylurea 2nd gen
- Down K efflux->Up Ca in->Up insulin rls in pancreas.
- Less side fx, longer duration than 1st gen
- DM Type 2
17
Q
repaglinide
A
- meglitinide
- Down K efflux->Up Ca in->Up insulin rls in pancreas.
- bad for renal/hepatic dz!
- DM Type 2
18
Q
nateglinide
A
- phenylalanine analog
- Down K efflux->Up Ca in->Up insulin rls in pancreas.
- Safer than repaglinide for renal failure (& shorter)
- DM Type 2
19
Q
metformin
A
- biguanide
- Down gluconeogenesis by antag glucagon & activate AMP kinase
- bad for lactic acidosis
- DM Type 2
20
Q
rosiglitazone
A
- thiazolidinedione
- Up PPARgamma-> up insulin sensitivity in tissues
- Liver tox, weight gain, fluid retention
- DM Type 2
21
Q
pioglitazone
A
- thiazolidinedione
- Up PPARgamma-> up insulin sensitivity in tissues
- Liver tox, weight gain, fluid retention
- DM Type 2
22
Q
acarbose
A
- alpha glucosidase inhibitor
- Down carbohydrate absorption
- gassy diarrhea
- DM Type 2
23
Q
miglitol
A
- alpha glucosidase inhibitor
- Down carbohydrate absorption
- gassy diarrhea
- DM Type 2
24
Q
bromocriptine
A
-
-DM Type 2
25
canagliflozin
- inhibitor of glucose reabsorption
- Inhibit SGLT2 in kidney
- UTI's, up urination
- DM Type 2
26
thyroxine
- thyroid hormones
- T4
- thyrotoxicosis, cardiovascular stress
- hypothyroid
27
triiodothyronine
- thyroid hormones
- T3
- thyrotoxicosis, cardiovascular stress
- hypothyroid
28
T4+T3
- thyroid hormones
- T4, T3
- thyrotoxicosis, cardiovascular stress
- hypothyroid
29
propylthiouracil
- thioamides/thioureylenes
- stops thyroid peroxidase. ALSO inhibits peripheral conversion of T4->T3
- agranulocytosis, LIVER TOX
- hyperthyroid (safer during pregnancy)
30
methimazole
- thioamides/thioureylenes
- stops thyroid peroxidase
- agranulocytosis
- hyperthyroid
31
potassium iodide
-Other
-inhibits synth of T3 & T4. Oral, fast.
-
-Hyperthyroid (not sole therapy!), prevents uptake of radioactive Iodine
32
radioactive iodine
-Other
-destroys thyroid
-
-Hypothyroid (delayed). VERY slow acting (months)
33
propranolol
- other
- B blocker (nonselective)
- heart failure/heart block
- Treat cardiovascular symptoms of hyperthyroid
34
growth hormone
- GH-related
- stim IGF-1, antagonizes insulin
- carpal tunnel, diabetes, hypothyroid
- GH deficiency, chronic renal failure
35
sermorelin acetate
- GH-related
- GHRH analog
- headache
- GH deficiency, chronic renal failure
36
IGF-1
-GH-related
-IGF receptor agonist
-
-ONLY syndrome of GH resistance
37
pegvisomant
-GH-related
-GH antag doesn't allow dimerization
-
-For hyper-GH syndromes
38
octreotide
- somatostatin agonist
- 2 & 5 receptor agonist
- gallstones
- For hyper-GH syndromes
39
bromocriptine
- D2 agonist
- suppresses prolactin
- orthostatic hypotension
- amenorrhea, infertility, galactorrhea
40
cabergoline
- D2 agonist
- suppresses prolactin
- orthostatic hypotension
- amenorrhea, infertility, galactorrhea
41
desmopressin
-Posterior pituitary
-stim V2 R's: reabsorb water
-
-pituitary diabetes insipidus
42
vasopressin
-Posterior pituitary
-stim V1 R's: vasoconstrict. and V2 R's: reabsorb water
-
-pituitary diabetes insipidus
43
oxytocin
-Posterior pituitary
-modulates transmembrane ion currents in sm muscle
-
-induce labor
44
Vitamin D
-Vitamin D
-Increases Ca absorption and decreases excretion
-
-Ca deficiency, prostate and breast health
45
Vitamin D2
- ergocalciferol
| - Same as vit D
46
Vitamin D3
- calcitriol
| - Same as vit D
47
PTH/teriparatide
-Misc
-Low dose daily stimulates blasts
-
-Osteoporosis
48
calcitonin
-misc
-prevents bone resorption
-
-hypercalcemia or osteoporosis (nasal spray)
49
alendronate
- bisphosphonates
- Inhibit geranylgeranyl diphosphate synthase->down bone resorption
- esophagitis, osteonecrosis of jaw
- hypercalcemia or osteoporosis
50
etidronate
- bisphosphonates
- Slows dissolution of hydroxyapatite AND Inhibits geranylgeranyl diphosphate synthase->down bone resorption
- esophagitis, osteonecrosis of jaw
- hypercalcemia or osteoporosis
51
pamidronate
- bisphosphonates
- Inhibit geranylgeranyl diphosphate synthase->down bone resorption
- esophagitis, osteonecrosis of jaw
- hypercalcemia or osteoporosis
52
risendronate
- bisphosphonates
- Inhibit geranylgeranyl diphosphate synthase->down bone resorption
- esophagitis, osteonecrosis of jaw
- hypercalcemia or osteoporosis
53
tiludronate
- bisphosphonates
- Inhibit geranylgeranyl diphosphate synthase->down bone resorption
- esophagitis, osteonecrosis of jaw
- hypercalcemia or osteoporosis
54
denosumab
-RANKL antibody
-Adsorbs to RANKL so it can't activate the RANK receptor in osteoclasts->down bone resorption
-
-osteoporosis
55
estradiol
- estrogens
- agonist at bone, breast, CV system, endometrium, vaginal epithelium
- block resorption of bone, increase HDL/lower LDL, increase risk of stroke/embolism, breast cancer, increase progesterone receptors
- too rapidly inactivated, synthetic analogues used instead
56
ethinyl estradiol
- estrogens
- agonist at bone, breast, CV system, endometrium, vaginal epithelium
- block resorption of bone, increase HDL/lower LDL, increase risk of stroke/embolism, breast cancer, increase progesterone receptors
- contraception (w/ progestin), suppression of HPG axis, replacement therapy. This is the most common in progestin + estrogen therapy.
57
estrone sulfate
- estrogens
- agonist at bone, breast, CV system, endometrium, vaginal epithelium
- block resorption of bone, increase HDL/lower LDL, increase risk of stroke/embolism, breast cancer, increase progesterone receptors
- contraception (w/ progestin), suppression of HPG axis, replacement therapy
58
diethylstilbestrol
- estrogens
- first non steroidal estrogen, no longer in use
- block resorption of bone, increase HDL/lower LDL, increase risk of stroke/embolism, breast cancer, increase progesterone receptors
- contraception (w/ progestin), suppression of HPG axis, replacement therapy
59
tamoxifen
- SERM
- antagonist at breast, agonist everywhere else
- not mentioned in lecture
- estrogen dependent breast cancer, osteoporosis, postmenopausal symptoms
60
raloxifene
- SERM
- antagonist at breast, agonist at bone and cardio, neutral on endometrium and vaginal epithelium.
- not mentioned in lecture
- estrogen dependent breast cancer, osteoporosis, postmenopausal symptoms
61
ospemifene
- SERM
- agonist at vaginal epithelium bone, and cardio, antagonist at breast, neutral at endometrium
- not mentioned in lecture
- VAGINAL ATROPHY (agonistic effect on vaginal epithelium)
62
clomiphene
- estrogen antagonist
- antagonize inhibitory effects of estrogen on the pituitary and hypothalamus
- bone resporption due to lack of estrogen, increase lipids
- ovulation induction
63
fulvestrant
- estrogen antagonist
- antagonize inhibitory effects of estrogen on the pituitary and hypothalamus
- bone resporption, increased lipids
- ovulation induction
64
anastrozole
- aromatase inhibitor
- non-steroidal, inhibits conversion of androgen to estrogen
- hot flashes
- ovulation induction
65
exemestane
- aromatase inhibitor
- steroidal, inhibits conversion of androgen to estrogen
- hot flashes
- ovulation induction
66
drospirenone
- progestin
- enhanced activity as mineralocorticoid antagonist and andgrogen antagonist. decrease amount and increase viscosity of cervial mucus to prevent fertilization (main).
- headache, abnormal menstrual bleeding (when used with estrogen)
- contraceptive
67
progesterone
- progestins
- -decrease amount and increase viscosity of cervial mucus to prevent fertilization (main). also prevent ovulation by inhibiting hypothalamus and pituitary
- headache, abnormal menstrual bleeding (when used with estrogen)
- too rapidly inactivated, synthetic analogues used instead
68
medroxyprogesterone acetate
- Progestins
- decrease amount and increase viscosity of cervial mucus to prevent fertilization (main). also prevent ovulation by inhibiting hypothalamus and pituitary
- headache, abnormal menstrual bleeding (when used with estrogen)
- IM (3 months) contraception
69
norethindrone
- progestins
- decrease amount and increase viscosity of cervial mucus to prevent fertilization (main). also prevent ovulation by inhibiting hypothalamus and pituitary
- headache, abnormal menstrual bleeding (when used with estrogen)
- oral/IUD contraception
70
norgestrel
- progestins
- decrease amount and increase viscosity of cervial mucus to prevent fertilization (main). also prevent ovulation by inhibiting hypothalamus and pituitary
- headache, abnormal menstrual bleeding (when used with estrogen), NAUSEA and VOMITING, breast tenderness, dizziness, cramps
- oral/IUD/SubQ contraception, post-coital contraception (plan B)
71
ulipristal
- selective progesterone receptor modulator
- antagonizes actions of progesterone on granulosa cell receptors. This action of progesterone is needed for follicular rupture.
- headache, nausea, vomiting, dizziness
- post-coital contraception (within 5 days)
72
RU 486
- progestin receptor antagonist
- blocks progesterone effect on endometrium
- none listed (also glucocorticoid antagonist)
- oral for abortion/post-coital contraception, cushing's syndrome, type II DM
73
FSH
-gonadotropins
-
-
- Induce follicular growth. IM!!
74
CG
-gonadotropins
-
-
- Diagnostics for pregnancy, induce ovulations IM!!!!
75
gonadorelin
- GnRH and analogs
- stimulate gonadotropin secretion
- Google-Difficulty breathing, flushing, up HR, Itching
- delayed puberty, anovulatory disorders
76
luprolide
-GnRH and analogs
-GnRH agonist, initial stim then suppresion
-
-Tx: Prostate Cancer! precocious puberty& androgen excess male, dysmenorrhea, ovulation induction
77
cetrolix
-GnRH and analogs
-GnRh antagonist
-
-Tx:precocious puberty& androgen excess male, dysmenorrhea, ovulation induction
78
testosterone
-Androgens-
-
-virilization, feminization, suppress HPG, (hepatic toxicity)
- hypogonadism replacement, catbolic states/muscle wastingTransdermal or buccal tablets
79
testosterone propionate
-Androgens
-
-virilization, feminization, suppress HPG, (hepatic toxicity)
- hypogonadism replacement, catbolic states/muscle wasting. intramuscular
80
methyltestosterone
-17a-alkylated androgens
-
- hepatic toxicity, virilization, feminization, suppress HPG
-hypogonadism replacement, catbolic states/muscle wasting
81
danazole
-17a-alkylated androgens
-
-hepatic toxicity, virilization, feminization, suppress HPG
-hypogonadism replacement, catbolic states/muscle wasting
82
dutasteride
- anti-androgen
- 5a-reductase inhibitors,inhibits conversion to dihydrotestosterone
- erection/ejac. problems, down desire, testicular pain, depression
- Tx. Androgen excess, or androgen dependent disorders
83
finasteride
- antiandrogen
- 5a-reductase inhibitors, inhibits conversion to dihydrotestosterone
- erection/ejac. problems, down desire, testicular pain, depression
- Tx. Androgen excess, or androgen dependent disorders
84
bicalutamide
- anti-androgen
- androgen receptor antagonist
- not specified (google-nause, vomit, diarrhea, down sex desire,)
- Tx. Androgen excess, or androgen dependent disorders
85
flutamide
- anti-androgen
- androgen receptor antagonist
- not specified (google-nause, vomit, diarrhea, down sex desire,)
- Tx. Androgen excess, or androgen dependent disorders
86
nilutamide
- antiandrogen
- androgen receptor antagonist
- not specified (google-nause, vomit, diarrhea, down sex desire,)
- Tx. Androgen excess, or androgen dependent disorders
87
amphotericin B
- polyene
- bind ergosterol, compromise fungal cell membrane. fungicidal
- anaphylaxis, nephrotoxicity
- most life-threatening sytemic fungal infections
88
nystatin
- polyene
- bind ergosterol, compromise fungal cell membrane
- bitter and unpleasant taste, too toxic to be used parenterally
- topically to treat candida infections of the muscosa, skin, instestnal tract, and vagina
89
clotrimazole
- imidazoles
- block ergosterol synthesis by binding and inhibiting fungal cytochrome P450 enzyme lanosterol 14-alpha-demethylase
- restricted to oral/topical use (minimal GI upset if swallowed)
- drug of choice for oropharyngeal candidiasis in AIDS patients
90
ketoconazole
- imidazole
- block ergosterol synthesis by binding and inhibiting fungal cytochrome P450 enzyme lanosterol 14-alpha-demethylase
- inhibit adrenal and gonadal steroid hormone synthesis, hepatitis
- "use is limited due to availability of safer drugs"
91
miconazole
- imidazole
- block ergosterol synthesis by binding and inhibiting fungal cytochrome P450 enzyme lanosterol 14-alpha-demethylase
- topical only (systemic use causes thrombophlebitis)
- jock itch, ringworm, athlete's foot, vaginal infections, oral thrush
92
fluconazole
- azole
- block ergosterol synthesis by binding and inhibiting fungal cytochrome P450 enzyme lanosterol 14-alpha-demethylase-
- none mentioned in lecture
- oral or IV for cryptococcal meningitis (good CNS penetration). not active against molds, C. krusei, or C. glabrata
93
itraconazole
- azole
- block ergosterol synthesis by binding and inhibiting fungal cytochrome P450 enzyme lanosterol 14-alpha-demethylase
- none emphasized in lecture
- aspergillus + some fluconazole-resistant candida species (especially esophageal candidiasis)
94
posaconazole
- azole
- block ergosterol synthesis by binding and inhibiting fungal cytochrome P450 enzyme lanosterol 14-alpha-demethylase
- rash, elevated hepatic enzymes, numerous drug interactions
- only azole with activity against zygomycoses (Rhizopus, Mucor). Prophylaxis against invasive fungal infections in BMT and neutropenia.
95
voriconazole
- azole
- block ergosterol synthesis by binding and inhibiting fungal cytochrome P450 enzyme lanosterol 14-alpha-demethylase
- none emphasized in lecture
- invasive mold infections in immunocompromised patients (invasive aspergillosis!)
96
efinaconazole
- azole
- block ergosterol synthesis by binding and inhibiting fungal cytochrome P450 enzyme lanosterol 14-alpha-demethylase
- SAFE (minor irritation)
- topical treatment of onychomycosis
97
terbinafine
- allylamine
- inhibits ergosterol synthesis by blockign squalene epoxidase. Fungicidal.
- co-admin w/ rifampicin doubles clearance of terbinafine. cimetidine decreases clearance.
- topical or oral for dermatophytes
98
anidulafungin
- echinocandin
- inhibit glucan synthesis, weakens fungal cell wall and causes lysis
- well tolerated
- IV primarily for Aspergillus and azole resistant candida
99
caspofungin
- echinocandin
- inhibit glucan synthesis, weakens fungal cell wall and causes lysis
- well tolerated
- IV primarily for Aspergillus and azole resistant candida
100
micafungin
- echinocandin
- inhibit glucan synthesis, weakens fungal cell wall and causes lysis
- well tolerated
- IV primarily for Aspergillus and azole resistant candida
101
flucytosine
- antimetabolite
- pyrimidine analog, inhibits fungal DNA/RNA synthesis. Fungal cell enzyme cytosine deaminase converts to active form (5-FU) then becomes 5-FdUMP which competitively inhibits thymidilate synthetase to block fungal DNA synthesis. 5-UTP incoportated into defective RNA to reduce protein synthesis as well.
- GI intolerance, bone marrow depression, anemia, leukopenia, thrombocytopenia
- oral for systemic candida and cryptococcus infections
102
griseofulvin
- mitotic spindle poison
- blocks fungal mitosis by interacting with polymerized microtubules
- INDUCES various CYP isoforms in liver and alters pharmacokinetics with warfarin and oral contraceptives
- oral for systemic treatment of dermatophytosis (now limited use)
103
ethambutol
- 1st line anti-MTB
- interferes with biosynthesis of cell wall arabinogalactan
- optic neuritis, color blindness
- effective against multiplying bacilli
104
isoniazid
- 1st line anti-MTB
- inhibits cell wall synthesis (INH-NAD adduct inhibits FASII system), must be converted to active form by bacterial enzyme (pro-drug)
- peripheral neuropathy, elevation of liver enzymes, hepatitis
- kills actively growing bacteria. also used as single drug for treatment of latent TB
105
pyrazinamide
- 1st line anti-MTB
- metabolized via pyrazinamidase (pncA) to pyrazinoic acid (pro-drug). Mechanism unknown (disrupts energy metabolism and membrane)
- hepatotoxicity, GI intolerance
- kills dormant TB and more active against phagocytized TB (lower pH)
106
rifampin
- 1st line anti-MTB and leprosy
- binds to beta subunit to prevent transcription of mRNA (inhibits RNA polymerase). Bactericidal.
- orange color to urine sweat tears, rash, thrombocytopenia, nephritis, hepatitis, CYP 450 inducer
- kills rapidly growing and slowly metabolizing bacilli, also effective for leprosy and M. ulcerans (Buruli ulcer)
107
streptomycin
- former first line drug for MTB, now less useful due to increased resistance
- not mentioned
- not mentioned
- Buruli Ulcer treatment
108
capreomycin
- 2nd line anti-MTB
- blocks protein synthesis by targeting 16S rRNA, 70S ribosome, and rRNA methyltransferase
- not given
- tuberculosis
109
ciproflaxacin
- not given
- not given
- not given
- atypical mycobacterial infections
110
cycloserine
- 2nd line anti-MTB
- inhibits cell wall synthesis and peptidoglycan synthesis by acting as a D-alanine analogue
- not mentioned
- tuberculosis
111
ethionamide
- 2nd line anti-MTB
- blocks mycolic acid synthesis/cell wall by targeting acyl carrier and protein reductase (inhA)
- not mentioned
- tuberculosis
112
kanamycin
- 2nd line anti-MTB
- blocks protein synthesis by targeting 16s rRNA
- not mentioned
- tuberculosis
113
rifabutin
- anti-m. avium complex
- not given
- not given
- not given
114
dapsone
- anti-leprosy
- inhibits bacterial synthesis of dihydrofolic acid leading to inhibition of DNA and RNA synthesis
- hemolysis, hepatitis, nausea, rash
- leprosy
115
albendazole
- anihelminth (intestinal and cysts)
- binds tubulin and inhibits glucose uptake
- well absorbed
- do not use in pregnancy
116
mebindazole
- anihelminth (intestinal only)
- binds tubulin and inhibits glucose uptake
- poorly absorbed
- do not use in pregnancy
117
Ivermectin
- anihelminth
- uses Cl- currents to kill microfilariae only not adults
- Drug of choice for onchovera volvius but can be used for all
118
praziquantal
-antihelminth
-Ca+ release, worm paralysis and damage.
-Effective against cestode adult and larval cysts,
active against all trematodes excepts one.
119
artemether-lumefantrine
- antimalarial
- drug of choice for "self treatment" drug for most malaria
- based of chineese herbs
120
atovaquone-proguanil (Malarone)
-antimalarial
-Active against hypnozoite stage (liver)
-prophylaxis only against all types of malaria, and
treatment for CQ resistant P. falciparum
121
chloroquine
- antimalarial
- digests vessicles of intra-erythrocyte parasite
- used for prevention and treatment for all but CQ resistant P. falciparum
122
mefloquine
- antimalarial
- digests vessicles of intra-erythrocyte parasite
- prophylaxis ONLY against ALL types of malaria.
- Can cause neuropsychiatric problems (dreams/hallucinations)
123
metronidazole
- antiprotozoal
- disrupts DNA
- Entamoeba and Giardia
124
nitazoxanide
- antiprotozoal
- ferredoxin oxidoreductase
- Cryptosporidium and resistant Giardia
125
Cortisol
- glucocorticoid
- -mixed glucocorticoid/mineralcorticoid activation (50/50)
- cushing syndrome/immunosuppression/hyperglycemia
126
dexamethasone
- glucocorticoid (No mineralcorticoid activity)
| - cushing syndrome/immunosuppression/hyperglycemia
127
prednisolone
- glucocorticoid
- mixed glucocorticoid/mineralcorticoid (more gluco)
- oral or injectable
128
fludrocortisone
- mineralcorticoid
- mixed glucocorticoid/mineralcorticoid (more mineral)
- oral only
- hypokalemia/hypernatremia/hypertension
- DRUG OF CHOICE for mineralcorticoids
129
spironolactone & Eplerenone
- Aldosterone antagonists
- Block aldosterone receptor
- spironolactone also inhibits androgen synthesis pathway
130
aminoglutethimide
- adrenal cortex pathway inhibitor
- prevents conversion of cholesterol to pregnenolone
- treatment for cushings syndrome
131
metyrapone
- adrenal cortex pathway inhibitor
- prevents conversion of 11 desoxycortisol to cortisol & 11 deoxycorticosterone to corticosterone.
- Allows for a lot of deoxycorticosterone to persist which is a good mineralcorticoid.
- Treat cushing syndrome
132
ketoconazole
- adrenal cortex pathway inhibitor
| - antifungal that inhibits many steps in MC, GC, & androgen synthesis
133
ferrous fumarate
- iron
- ferrous better absorbed-325 tablet, 106mg iron
- nausea, epigastric pain, constipation, diarrhea, black stool
- iron deficiency- 2-3/day
134
ferrous gluconate
- iron
- ferrous better absorbed/ 320 tablet, 37mg iron
- -nausea, epigastric pain, constipation, diarrhea, black stool
- iron deficiency- 3-4/day
135
ferrous sulfate
- iron
- ferrous better absorbed-325mg/65mgiron
- -nausea, epigastric pain, constipation, diarrhea, black stool
- iron deficiency- 3-4/day
136
cyanocobalamin
- vitamin B12
-
- anaphylaxis with IV, hypokalemia, secondary iron deficiency
- parenteral for pernicious/resections-oral supplement deficient diet of B12
137
folate
-folate
-
-mask B12 deficiency, reduce phenobarbital, phenytoin primidone, raltritrexed -all folate def. except for inhibiotrs of DHFR(leucovorin)
138
deferoxamine
- chelator
- binds iron
- IV can lead to hypotension, neurotoxicity, susceptible to infection
- SubQ or IM for iron toxicity
139
erythropoietin
- Hematopoietic growth factor
- stim prolif,maturation and Hgb by CFU-E, synergy with IL3, and GMCSF expand BFU-E compartment, stim release of reticulocytes
- inc. clot during dialysis, hypert., seizures (allergic reaction mild infreq)
- anemia of renal failure, Aids tx w/AZT, cancer chemo, preop autologous trans.
140
Filgastrim
-Myeloid growth factor- G-CSF
-stim granulocyte colonies and neutrophils, promotes granulo release
-
-
141
Sargramostim
-myeloid growth factor- GM-CSF
-w/IL3, stim prolif of gran, monoc, macro, megakaryocytes
-
-
142
Penicillin G
- penicillin (beta-lactam)
- structural analogs of D-Ala-D-Ala blocking PDG X-linking
- allergies, dose-dep neurotoxicity & seizures, Stevens-Johnson syndrome
- Non-penicillinase producing microbes: S. pneumonia, staph spp, N. meningitides, Clostridum spp, Treponema pallidum
143
Penicillin V
- penicillin (beta-lactam)
- structural analogs of D-Ala-D-Ala blocking PDG X-linking
- allergies, Stevens-Johnson syndrome
- Non-penicillinase producing microbes: S. pneumonia, staph spp, N. meningitides, Clostridum spp, Treponema pallidum
144
oxacillin
- beta-lactamase R penicillins
- structural analogs of D-Ala-D-Ala blocking PDG X-linking
- hepatitis (high doses), allergies, Stevens-Johnson syndrome
- penicillinase-producing staph & strep
145
nafcillin
- beta-lactamase R penicillins
- structural analogs of D-Ala-D-Ala blocking PDG X-linking; hydrolyzed & destroyed by kidneys
- allergies, Stevens-Johnson syndrome
- penicillinase-producing staph & strep
146
Amoxicillin
- Extended spectrum penicillins
- structural analogs of D-Ala-D-Ala blocking PDG X-linking; better absorption than ampicillin, not affected by food
- NA
- non-lactamase G- bacilli (E. coli, H. influenza, Salmonella, Shigella)
147
Ampicillin
- Extended spectrum penicillins
- structural analogs of D-Ala-D-Ala blocking PDG X-linking
- NA
- non-lactamase G- bacilli (E. coli, H. influenza, Salmonella, Shigella)
148
Piperacillin
- Extended spectrum penicillins
- structural analogs of D-Ala-D-Ala blocking PDG X-linking-NA
- NA
- anti-pseudomonal; Klebsiella or Pseudomonas, often in combo with aminoglycoside to prevent resistance; non-lactamase G- bacilli (E. coli, H. influenza, Salmonella, Shigella)
149
Carbenicillin
- Extended spectrum penicillins
- structural analogs of D-Ala-D-Ala blocking PDG X-linking
- NA
- anti-pseudomonal; non-lactamase G- bacilli (E. coli, H. influenza, Salmonella, Shigella)
150
Clavulanic acid
- beta-lactamase suicide inhibitor
- structurally related to penicillins but poor antibiotic acitivity alone
- NA
- fixed concentrations with extended spectrum penicillins
151
Sulbactam
- beta-lactamase suicide inhibitor
- structurally related to penicillins but poor antibiotic acitivity alone
- NA
- fixed concentrations with extended spectrum penicillins
152
Tazobactam
- beta-lactamase suicide inhibitor
- structurally related to penicillins but poor antibiotic acitivity alone
- NA
- fixed concentrations with extended spectrum penicillins
153
Cefazolin – 1st generation
- cephalosporins (beta-lactam)
- structural analogs of D-Ala-D-Ala blocking PDG X-linking
- Disulfiram-like rxn, hypersensitivity (X-allergenic with pens) similar to pens (allergies etc)
- broadest spec against G+ cocci, effective against G- bacilli; used for surgical prophylaxis
154
Cefuroxime – 2nd generation
- cephalosporins (beta-lactam)
- structural analogs of D-Ala-D-Ala blocking PDG X-linking
- Disulfiram-like rxn, hypersensitivity (X-allergenic with pens) similar to pens (allergies etc)
- anaerobes
155
Cefotaxime – 3rd generation
- cephalosporins (beta-lactam)
- structural analogs of D-Ala-D-Ala blocking PDG X-linking
- Disulfiram-like rxn, hypersensitivity (X-allergenic with pens) similar to pens (allergies etc)
- anti-pseudomonal & -pneumoncoccal; serious G- infections (meningitis, pneumonia, gonorrhea)
156
Cefepime – 4th generation
- cephalosporins (beta-lactam)
- structural analogs of D-Ala-D-Ala blocking PDG X-linking
- Disulfiram-like rxn, hypersensitivity (X-allergenic with pens) similar to pens (allergies etc)
- anti-pseudomonal, Enterobacter, pens-R strep
157
imipenem
- carbapenems (beta-lactam)
- structural analogs of D-Ala-D-Ala blocking PDG X-linking, bind PBPs more efficiently & R to most beta-lactamases
- GI effects, superinfections, neurotoxicity, X-allergenicity to pens
- broadest activity of all beta-lactams; 2nd line therapy for serious nosocominal infections
158
cilastatin
- petidase inhibitor
- inhibits dehydropeptidases
- NA
- imipenem always admin with cilastatin
159
aztreonam
- monobactams
- structural analogs of D-Ala-D-Ala blocking PDG X-linking
- NA No X-reactivity with pens
- narrow (G- aerobes including Pseudomonas, penetrates CNS); G- UTIs, lower RTIs, systemic infections
160
Bacitracin
- Non-beta-lactam
- deletes lipid carrier for PDG synthesis
- severe nephrotoxicity
- topical app ONLY for skin/eye infections, good combo with polymyxin B; narrow spectrum (G+, Neisseria, T. pallidum)
161
D-Cycloserine
- Non-beta-lactam
- structural analog of D-alanine, blocks PDG synthesis
- serious CNS effects, reversible
- broad spec; restricted 2nd line for M. tuberculosis
162
Fosfomycin
- Non-beta-lactam
- structural analog of PEP, blocks PDG synthesis
- few adverse effects
- single dose oral tx of uncomplicated UTIs (rapid resistance)
163
Vancomycin
- Non-beta-lactam
- binds D-Ala-D-Ala growing end of pentapeptide, interferes with X-linking in PDGG synthesis
- red man syndrome, ototoxicity, nephrotoxicity
- narrow spec for serious G+ infecitons, MRSA, combo with aminoglycosides (cidal except static in enterococci)
164
Daptomycin
- Other-membrane depolarizer
- Novel cyclic lipopeptide, cidal by membrane depolarization
- myopathy
- narrow spec G+ similar to vancomycin, treats VREF & MRSA
165
gentamycin
- aminoglycosides
- irreversible binding to 30s bacterial ribosomal subunit & inhibiting protein synthesis at several levels; bactericidal & PAE
- ototoxicity (irreversible hearing loss), vestibular toxicity
- severe G-aerobe infections, combo therapy with vanc/pens for staph
166
neomycin
- aminoglycosides
- irreversible binding to 30s bacterial ribosomal subunit & inhibiting protein synthesis at several levels; bactericidal & PAE
- ototoxicity (irreversible hearing loss), vestibular toxicity, renal toxicity (reversible)
- widespread use for bowel surgeries (resistance), enterocolitis outbreaks
167
spectinomycin
- aminocyclitol
- binds 30s ribosomal subunit, bacteriostatic
- NA
- MRSA, enterococci, antibiotic-R gonorrhea
168
tigecycline
- glycylglycines
- tetracycline analogue: reversible binding to 30s ribosomal subunit blocking A site
- NA
- tetracycline-R strains, Hershey isolate of MRSA
169
tetracycline
- tetracyclines
- reversible binding to 30s ribosomal subunit blocking A site; oral admin decr by divalent and trivalent cations & when gastric pH elevated
- GI irritation, superinfections (pseudomembranous colitis), discoloration of teeth (not admin to pregnant women or children - fetal & childhood risks), renal/liver toxicity, photosensitivity, vestibular disturbances
- acne, Rickettsial diseases
170
doxycycline
- tetracyclines
- reversible binding to 30s ribosomal subunit blocking A site; oral admin decr by divalent and trivalent cations & when gastric pH elevated
- GI irritation, superinfections (pseudomembranous colitis), discoloration of teeth (not admin to pregnant women or children - fetal & childhood risks), renal/liver toxicity, photosensitivity, vestibular disturbances
- acne, Rickettsial diseases
171
minocycline
- tetracyclines
- reversible binding to 30s ribosomal subunit blocking A site; oral admin decr by divalent and trivalent cations & when gastric pH elevated
- GI irritation, superinfections (pseudomembranous colitis), discoloration of teeth (not admin to pregnant women or children - fetal & childhood risks), renal/liver toxicity, photosensitivity, vestibular disturbances
- acne, Rickettsial diseases
172
azithromycin
- macrolides
- reversibly bind to 50s subunit & competitively inhibit streptogramins, clindamycin, & chloramphenicol
- no CYP interactions
- alternative to pens with allergy, RTI from Legionella, mycoplasma; common bacterial infections
173
clarithromycin
- macrolides
- reversibly bind to 50s subunit & competitively inhibit streptogramins, clindamycin, & chloramphenicol
- inhibits CYP3A4
- alternative to pens with allergy, RTI from Legionella, mycoplasma; common bacterial infections
174
erythromycin
-macrolides
-reversibly bind to 50s subunit & competitively inhibit streptogramins, clindamycin, & chloramphenicol; oral
admin with salts, esters, or enteric coated tablets (acid labile)
-inhibits CYP3A4; GI disturbances, allergic cholestatic hepatitis (from erythromycin estolate)
-less effective against anaerobes than others in class; pentrates abscesses, alternative to pens with allergy, RTI from Legionella, mycoplasma; common bacterial infections
175
telithromycin
- Macrolide (ketolide)
- reversibly bind to 50s subunit & competitively inhibit streptogramins, clindamycin, & chloramphenicol; semi-synthetic der of erythromycin with incr acid stability, addinity for 50s ribosome, & reduced resistance; conc-dep bactericidal
- GI, blurred vision; rare: liver damage/failure; contraindic in myasthenia gravis
- CA-RTIs, effective against S. pneumonia, H. influenza, M. catarrhalis, some S. aureus
176
clindamycin
- lincomycins
- binds 50s ribosomal subunit
- diarrhea, pseudomembranous colitis, skin rash, Stevens-Johnson syndrome, anaphylaxis; contraindic in liver failure
- RTIS caused by anaerobes, abscesses, MRSA, Group A strep, osteomyelitis
177
quinupristin
- streptogramins
- bind 50s ribosomal subunit, same site as macrolides; Quinupristin/dalfopristin (30:70 prep); combined cidal
- pain, phlebitis, dereg of drug levels that are metabolized by CYPs
- MRSA, vancomycin-R G+ infections, VREF, VRSA, Strep pneumoniae
178
dalfopristin
- streptogramins
- bind 50s ribosomal subunit, binds nearby macrolide spot > synergistically enhances quinupristin binding; Quinupristin/dalfopristin (30:70 prep); combined cidal
- pain, phlebitis, dereg of drug levels that are metabolized by CYPs
- MRSA, vancomycin-R G+ infections, VREF, VRSA, Strep pneumoniae
179
chloramphenicol
-protein synth inhibit other
-bind reversibly to 50s ribosome subunit at the peptidyltransferase site (site
near that of clindamycin & macrolides)
-hematological toxicities, aplastic anemia, gray baby syndrome
-restricted to infections not treatable by less toxic drugs; Rickettsial infections in patients who cannot take tetracycline
180
linezolid
- protein synth inhibit other
- binds novel site in 23s ribosomal RNA of 50s ribosomal unit; no X-reaction with other protein synthesis inhibs
- NA
- treat serious infections: MRSA, multi-drug R S. pneumoniae, VREF
181
mupirocin
- protein synth inhibit other
- inhibits isoleucyl tRNA synthetase; topical use ONLY
- NA
- impetigo caused by MRSA or Group A strep
182
sulfamethoxazole
-sulfonamides
-DHPS inhibitor in folic acid synth pathway, false substrate preventing binding of
PABA to DHPS; bacteriostatic, well-distributed (in CNS)
-hemolytic anemia (G6PD def), kernicterus, Stevens-Johnson syndrome; GI effects, rash, bone marrow/liver toxicity
-not used alone (combo with trimethoprim)! common bacterial infections (UTIs but R & toxicity), malaria, CNS toxoplasmosis
183
trimethoprim
-DHFR inhibitor
-DHFR inhibitor in folic acid synth pathyway (100,000x more selective for bacterial
over human); alone static
-NA
-combo with sulfamethoxazole;
184
tmp-sulfa
- Combo sulfonamide/DHFR inhib
- synergism bactericidal
- same toxicities as sulfamethoxazole (hemolytic anemia, kernicterus, Steves-Johnson syndrome); anti-folate effects (don't use in pregnant womenor alcoholics)
- CA-MRSA, UTIs, Pneumocystis pneumonia in immunocompromised, sinusitis, otitis media
185
ciprofloxacin
- fluoroquinolones
- inhibit bacterial DNA gyrase & topoisomerase > irrevers DNA damage; (older, better against G-) ciprofloxacin, levofloxacin, moxifloxacin (newer, better against G+); conc-dep killing: higher AUC/MIC better efficacy - target AUC/MIC: immunocompromised 100, immunocompetent 25
- GI issues, hepatotoxicity, MRSA & C. dif colonization, do NOT give to children (arthropathy) or athletes (achilles tendon rupture)
- nosocomial infections, complicated UTIs, bacterial prostatitis, pneumonias, STIs, osteomyelitis (majority of use inappropriate)
186
levofloxacin
- fluoroquinolones
- inhibit bacterial DNA gyrase & topoisomerase > irrevers DNA damage; (older, better against G-) ciprofloxacin, levofloxacin, moxifloxacin (newer, better against G+); conc-dep killing: higher AUC/MIC better efficacy - target AUC/MIC: immunocompromised 100, immunocompetent 25
- GI issues, hepatotoxicity, MRSA & C. dif colonization, do NOT give to children (arthropathy) or athletes (achilles tendon rupture)
- nosocomial infections, complicated UTIs, bacterial prostatitis, pneumonias, STIs, osteomyelitis (majority of use inappropriate)
187
moxifloxacin
- fluoroquinolones
- inhibit bacterial DNA gyrase & topoisomerase > irrevers DNA damage; (older, better against G-) ciprofloxacin, levofloxacin, moxifloxacin (newer, better against G+); conc-dep killing: higher AUC/MIC better efficacy - target AUC/MIC: immunocompromised 100, immunocompetent 25
- GI issues, hepatotoxicity, MRSA & C. dif colonization, do NOT give to children (arthropathy) or athletes (achilles tendon rupture)
- nosocomial infections, complicated UTIs, bacterial prostatitis, pneumonias, STIs, osteomyelitis (majority of use inappropriate)
188
Lanreotide
- somatostatin analog
- Acts on 2 & 5 receptors (not in pancreas)
- gallstones
- Hyper-GH syndromes