Test 4 Flashcards

1
Q

aspart

A
  • Insulin
  • rapid bind
  • allergy
  • DM type 1, 2, pregnancy
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2
Q

detemir

A
  • Insulin
  • long bind
  • allergy
  • DM type 1, 2, pregnancy
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3
Q

glargine

A
  • Insulin
  • long bind
  • allergy
  • DM type 1, 2, pregnancy
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4
Q

glulisine

A
  • Insulin
  • rapid bind
  • allergy
  • DM type 1, 2, pregnancy
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5
Q

lispro

A
  • Insulin
  • rapid bind
  • allergy
  • DM type 1, 2, pregnancy
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6
Q

NPH

A
  • Insulin
  • intermediate-length bind
  • allergy
  • DM type 1, 2, pregnancy
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7
Q

regular crystallin insulin

A
  • Insulin
  • short bind
  • allergy
  • DM type 1, 2, pregnancy
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8
Q

exenatide

A

-incretin-like agonist
-up glu-induced insulin release in beta cell, down glucagon from alpha cell
-
-DM type 2

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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!

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10
Q

pramlintide

A

-amylin analog
-Up insulin by inhibiting glucagon & suppressing appetite
-
-DM Type 1, 2

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11
Q

Chlorpropamide

A
  • sulfonylurea
  • Down K efflux->Up Ca in->Up insulin rls in pancreas.
  • tachyphylaxis
  • DM Type 2
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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
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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
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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
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15
Q

tolbutamide

A
  • sulfonylurea
  • Down K efflux->Up Ca in->Up insulin rls in pancreas.
  • tachyphylaxis
  • DM Type 2
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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
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17
Q

repaglinide

A
  • meglitinide
  • Down K efflux->Up Ca in->Up insulin rls in pancreas.
  • bad for renal/hepatic dz!
  • DM Type 2
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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
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19
Q

metformin

A
  • biguanide
  • Down gluconeogenesis by antag glucagon & activate AMP kinase
  • bad for lactic acidosis
  • DM Type 2
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20
Q

rosiglitazone

A
  • thiazolidinedione
  • Up PPARgamma-> up insulin sensitivity in tissues
  • Liver tox, weight gain, fluid retention
  • DM Type 2
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21
Q

pioglitazone

A
  • thiazolidinedione
  • Up PPARgamma-> up insulin sensitivity in tissues
  • Liver tox, weight gain, fluid retention
  • DM Type 2
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22
Q

acarbose

A
  • alpha glucosidase inhibitor
  • Down carbohydrate absorption
  • gassy diarrhea
  • DM Type 2
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23
Q

miglitol

A
  • alpha glucosidase inhibitor
  • Down carbohydrate absorption
  • gassy diarrhea
  • DM Type 2
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24
Q

bromocriptine

A

-
-DM Type 2

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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