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4 Pharm Unit > Test 4 > Flashcards

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
Q

canagliflozin

A
  • inhibitor of glucose reabsorption
  • Inhibit SGLT2 in kidney
  • UTI’s, up urination
  • DM Type 2
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26
Q

thyroxine

A
  • thyroid hormones
  • T4
  • thyrotoxicosis, cardiovascular stress
  • hypothyroid
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27
Q

triiodothyronine

A
  • thyroid hormones
  • T3
  • thyrotoxicosis, cardiovascular stress
  • hypothyroid
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28
Q

T4+T3

A
  • thyroid hormones
  • T4, T3
  • thyrotoxicosis, cardiovascular stress
  • hypothyroid
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29
Q

propylthiouracil

A
  • thioamides/thioureylenes
  • stops thyroid peroxidase. ALSO inhibits peripheral conversion of T4->T3
  • agranulocytosis, LIVER TOX
  • hyperthyroid (safer during pregnancy)
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30
Q

methimazole

A
  • thioamides/thioureylenes
  • stops thyroid peroxidase
  • agranulocytosis
  • hyperthyroid
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31
Q

potassium iodide

A

-Other
-inhibits synth of T3 & T4. Oral, fast.
-
-Hyperthyroid (not sole therapy!), prevents uptake of radioactive Iodine

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32
Q

radioactive iodine

A

-Other
-destroys thyroid
-
-Hypothyroid (delayed). VERY slow acting (months)

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33
Q

propranolol

A
  • other
  • B blocker (nonselective)
  • heart failure/heart block
  • Treat cardiovascular symptoms of hyperthyroid
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34
Q

growth hormone

A
  • GH-related
  • stim IGF-1, antagonizes insulin
  • carpal tunnel, diabetes, hypothyroid
  • GH deficiency, chronic renal failure
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35
Q

sermorelin acetate

A
  • GH-related
  • GHRH analog
  • headache
  • GH deficiency, chronic renal failure
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36
Q

IGF-1

A

-GH-related
-IGF receptor agonist
-
-ONLY syndrome of GH resistance

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37
Q

pegvisomant

A

-GH-related
-GH antag doesn’t allow dimerization
-
-For hyper-GH syndromes

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38
Q

octreotide

A
  • somatostatin agonist
  • 2 & 5 receptor agonist
  • gallstones
  • For hyper-GH syndromes
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39
Q

bromocriptine

A
  • D2 agonist
  • suppresses prolactin
  • orthostatic hypotension
  • amenorrhea, infertility, galactorrhea
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40
Q

cabergoline

A
  • D2 agonist
  • suppresses prolactin
  • orthostatic hypotension
  • amenorrhea, infertility, galactorrhea
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41
Q

desmopressin

A

-Posterior pituitary
-stim V2 R’s: reabsorb water
-
-pituitary diabetes insipidus

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42
Q

vasopressin

A

-Posterior pituitary
-stim V1 R’s: vasoconstrict. and V2 R’s: reabsorb water
-
-pituitary diabetes insipidus

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43
Q

oxytocin

A

-Posterior pituitary
-modulates transmembrane ion currents in sm muscle
-
-induce labor

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44
Q

Vitamin D

A

-Vitamin D
-Increases Ca absorption and decreases excretion
-
-Ca deficiency, prostate and breast health

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45
Q

Vitamin D2

A
  • ergocalciferol

- Same as vit D

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46
Q

Vitamin D3

A
  • calcitriol

- Same as vit D

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47
Q

PTH/teriparatide

A

-Misc
-Low dose daily stimulates blasts
-
-Osteoporosis

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48
Q

calcitonin

A

-misc
-prevents bone resorption
-
-hypercalcemia or osteoporosis (nasal spray)

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49
Q

alendronate

A
  • bisphosphonates
  • Inhibit geranylgeranyl diphosphate synthase->down bone resorption
  • esophagitis, osteonecrosis of jaw
  • hypercalcemia or osteoporosis
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50
Q

etidronate

A
  • bisphosphonates
  • Slows dissolution of hydroxyapatite AND Inhibits geranylgeranyl diphosphate synthase->down bone resorption
  • esophagitis, osteonecrosis of jaw
  • hypercalcemia or osteoporosis
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51
Q

pamidronate

A
  • bisphosphonates
  • Inhibit geranylgeranyl diphosphate synthase->down bone resorption
  • esophagitis, osteonecrosis of jaw
  • hypercalcemia or osteoporosis
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52
Q

risendronate

A
  • bisphosphonates
  • Inhibit geranylgeranyl diphosphate synthase->down bone resorption
  • esophagitis, osteonecrosis of jaw
  • hypercalcemia or osteoporosis
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53
Q

tiludronate

A
  • bisphosphonates
  • Inhibit geranylgeranyl diphosphate synthase->down bone resorption
  • esophagitis, osteonecrosis of jaw
  • hypercalcemia or osteoporosis
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54
Q

denosumab

A

-RANKL antibody
-Adsorbs to RANKL so it can’t activate the RANK receptor in osteoclasts->down bone resorption
-
-osteoporosis

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55
Q

estradiol

A
  • 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
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56
Q

ethinyl estradiol

A
  • 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.
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57
Q

estrone sulfate

A
  • 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
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58
Q

diethylstilbestrol

A
  • 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
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59
Q

tamoxifen

A
  • SERM
  • antagonist at breast, agonist everywhere else
  • not mentioned in lecture
  • estrogen dependent breast cancer, osteoporosis, postmenopausal symptoms
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60
Q

raloxifene

A
  • 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
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61
Q

ospemifene

A
  • 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)
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62
Q

clomiphene

A
  • estrogen antagonist
  • antagonize inhibitory effects of estrogen on the pituitary and hypothalamus
  • bone resporption due to lack of estrogen, increase lipids
  • ovulation induction
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63
Q

fulvestrant

A
  • estrogen antagonist
  • antagonize inhibitory effects of estrogen on the pituitary and hypothalamus
  • bone resporption, increased lipids
  • ovulation induction
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64
Q

anastrozole

A
  • aromatase inhibitor
  • non-steroidal, inhibits conversion of androgen to estrogen
  • hot flashes
  • ovulation induction
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65
Q

exemestane

A
  • aromatase inhibitor
  • steroidal, inhibits conversion of androgen to estrogen
  • hot flashes
  • ovulation induction
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66
Q

drospirenone

A
  • 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
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67
Q

progesterone

A
  • 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
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68
Q

medroxyprogesterone acetate

A
  • 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
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69
Q

norethindrone

A
  • 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
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70
Q

norgestrel

A
  • 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)
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71
Q

ulipristal

A
  • 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)
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72
Q

RU 486

A
  • 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
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73
Q

FSH

A

-gonadotropins
-
-
- Induce follicular growth. IM!!

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74
Q

CG

A

-gonadotropins
-
-
- Diagnostics for pregnancy, induce ovulations IM!!!!

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75
Q

gonadorelin

A
  • GnRH and analogs
  • stimulate gonadotropin secretion
  • Google-Difficulty breathing, flushing, up HR, Itching
  • delayed puberty, anovulatory disorders
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76
Q

luprolide

A

-GnRH and analogs
-GnRH agonist, initial stim then suppresion
-
-Tx: Prostate Cancer! precocious puberty& androgen excess male, dysmenorrhea, ovulation induction

77
Q

cetrolix

A

-GnRH and analogs
-GnRh antagonist
-
-Tx:precocious puberty& androgen excess male, dysmenorrhea, ovulation induction

78
Q

testosterone

A

-Androgens-
-
-virilization, feminization, suppress HPG, (hepatic toxicity)
- hypogonadism replacement, catbolic states/muscle wastingTransdermal or buccal tablets

79
Q

testosterone propionate

A

-Androgens
-
-virilization, feminization, suppress HPG, (hepatic toxicity)
- hypogonadism replacement, catbolic states/muscle wasting. intramuscular

80
Q

methyltestosterone

A

-17a-alkylated androgens
-
- hepatic toxicity, virilization, feminization, suppress HPG
-hypogonadism replacement, catbolic states/muscle wasting

81
Q

danazole

A

-17a-alkylated androgens
-
-hepatic toxicity, virilization, feminization, suppress HPG
-hypogonadism replacement, catbolic states/muscle wasting

82
Q

dutasteride

A
  • 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
Q

finasteride

A
  • antiandrogen
  • 5a-reductase inhibitors, inhibits conversion to dihydrotestosterone
  • erection/ejac. problems, down desire, testicular pain, depression
  • Tx. Androgen excess, or androgen dependent disorders
84
Q

bicalutamide

A
  • anti-androgen
  • androgen receptor antagonist
  • not specified (google-nause, vomit, diarrhea, down sex desire,)
  • Tx. Androgen excess, or androgen dependent disorders
85
Q

flutamide

A
  • anti-androgen
  • androgen receptor antagonist
  • not specified (google-nause, vomit, diarrhea, down sex desire,)
  • Tx. Androgen excess, or androgen dependent disorders
86
Q

nilutamide

A
  • antiandrogen
  • androgen receptor antagonist
  • not specified (google-nause, vomit, diarrhea, down sex desire,)
  • Tx. Androgen excess, or androgen dependent disorders
87
Q

amphotericin B

A
  • polyene
  • bind ergosterol, compromise fungal cell membrane. fungicidal
  • anaphylaxis, nephrotoxicity
  • most life-threatening sytemic fungal infections
88
Q

nystatin

A
  • 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
Q

clotrimazole

A
  • 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
Q

ketoconazole

A
  • 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
Q

miconazole

A
  • 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
Q

fluconazole

A
  • 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
Q

itraconazole

A
  • 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
Q

posaconazole

A
  • 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
Q

voriconazole

A
  • 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
Q

efinaconazole

A
  • azole
  • block ergosterol synthesis by binding and inhibiting fungal cytochrome P450 enzyme lanosterol 14-alpha-demethylase
  • SAFE (minor irritation)
  • topical treatment of onychomycosis
97
Q

terbinafine

A
  • 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
Q

anidulafungin

A
  • echinocandin
  • inhibit glucan synthesis, weakens fungal cell wall and causes lysis
  • well tolerated
  • IV primarily for Aspergillus and azole resistant candida
99
Q

caspofungin

A
  • echinocandin
  • inhibit glucan synthesis, weakens fungal cell wall and causes lysis
  • well tolerated
  • IV primarily for Aspergillus and azole resistant candida
100
Q

micafungin

A
  • echinocandin
  • inhibit glucan synthesis, weakens fungal cell wall and causes lysis
  • well tolerated
  • IV primarily for Aspergillus and azole resistant candida
101
Q

flucytosine

A
  • 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
Q

griseofulvin

A
  • 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
Q

ethambutol

A
  • 1st line anti-MTB
  • interferes with biosynthesis of cell wall arabinogalactan
  • optic neuritis, color blindness
  • effective against multiplying bacilli
104
Q

isoniazid

A
  • 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
Q

pyrazinamide

A
  • 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
Q

rifampin

A
  • 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
Q

streptomycin

A
  • former first line drug for MTB, now less useful due to increased resistance
  • not mentioned
  • not mentioned
  • Buruli Ulcer treatment
108
Q

capreomycin

A
  • 2nd line anti-MTB
  • blocks protein synthesis by targeting 16S rRNA, 70S ribosome, and rRNA methyltransferase
  • not given
  • tuberculosis
109
Q

ciproflaxacin

A
  • not given
  • not given
  • not given
  • atypical mycobacterial infections
110
Q

cycloserine

A
  • 2nd line anti-MTB
  • inhibits cell wall synthesis and peptidoglycan synthesis by acting as a D-alanine analogue
  • not mentioned
  • tuberculosis
111
Q

ethionamide

A
  • 2nd line anti-MTB
  • blocks mycolic acid synthesis/cell wall by targeting acyl carrier and protein reductase (inhA)
  • not mentioned
  • tuberculosis
112
Q

kanamycin

A
  • 2nd line anti-MTB
  • blocks protein synthesis by targeting 16s rRNA
  • not mentioned
  • tuberculosis
113
Q

rifabutin

A
  • anti-m. avium complex
  • not given
  • not given
  • not given
114
Q

dapsone

A
  • anti-leprosy
  • inhibits bacterial synthesis of dihydrofolic acid leading to inhibition of DNA and RNA synthesis
  • hemolysis, hepatitis, nausea, rash
  • leprosy
115
Q

albendazole

A
  • anihelminth (intestinal and cysts)
  • binds tubulin and inhibits glucose uptake
  • well absorbed
  • do not use in pregnancy
116
Q

mebindazole

A
  • anihelminth (intestinal only)
  • binds tubulin and inhibits glucose uptake
  • poorly absorbed
  • do not use in pregnancy
117
Q

Ivermectin

A
  • anihelminth
  • uses Cl- currents to kill microfilariae only not adults
  • Drug of choice for onchovera volvius but can be used for all
118
Q

praziquantal

A

-antihelminth
-Ca+ release, worm paralysis and damage.
-Effective against cestode adult and larval cysts,
active against all trematodes excepts one.

119
Q

artemether-lumefantrine

A
  • antimalarial
  • drug of choice for “self treatment” drug for most malaria
  • based of chineese herbs
120
Q

atovaquone-proguanil (Malarone)

A

-antimalarial
-Active against hypnozoite stage (liver)
-prophylaxis only against all types of malaria, and
treatment for CQ resistant P. falciparum

121
Q

chloroquine

A
  • antimalarial
  • digests vessicles of intra-erythrocyte parasite
  • used for prevention and treatment for all but CQ resistant P. falciparum
122
Q

mefloquine

A
  • antimalarial
  • digests vessicles of intra-erythrocyte parasite
  • prophylaxis ONLY against ALL types of malaria.
  • Can cause neuropsychiatric problems (dreams/hallucinations)
123
Q

metronidazole

A
  • antiprotozoal
  • disrupts DNA
  • Entamoeba and Giardia
124
Q

nitazoxanide

A
  • antiprotozoal
  • ferredoxin oxidoreductase
  • Cryptosporidium and resistant Giardia
125
Q

Cortisol

A
  • glucocorticoid
  • -mixed glucocorticoid/mineralcorticoid activation (50/50)
  • cushing syndrome/immunosuppression/hyperglycemia
126
Q

dexamethasone

A
  • glucocorticoid (No mineralcorticoid activity)

- cushing syndrome/immunosuppression/hyperglycemia

127
Q

prednisolone

A
  • glucocorticoid
  • mixed glucocorticoid/mineralcorticoid (more gluco)
  • oral or injectable
128
Q

fludrocortisone

A
  • mineralcorticoid
  • mixed glucocorticoid/mineralcorticoid (more mineral)
  • oral only
  • hypokalemia/hypernatremia/hypertension
  • DRUG OF CHOICE for mineralcorticoids
129
Q

spironolactone & Eplerenone

A
  • Aldosterone antagonists
  • Block aldosterone receptor
  • spironolactone also inhibits androgen synthesis pathway
130
Q

aminoglutethimide

A
  • adrenal cortex pathway inhibitor
  • prevents conversion of cholesterol to pregnenolone
  • treatment for cushings syndrome
131
Q

metyrapone

A
  • 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
Q

ketoconazole

A
  • adrenal cortex pathway inhibitor

- antifungal that inhibits many steps in MC, GC, & androgen synthesis

133
Q

ferrous fumarate

A
  • iron
  • ferrous better absorbed-325 tablet, 106mg iron
  • nausea, epigastric pain, constipation, diarrhea, black stool
  • iron deficiency- 2-3/day
134
Q

ferrous gluconate

A
  • iron
  • ferrous better absorbed/ 320 tablet, 37mg iron
  • -nausea, epigastric pain, constipation, diarrhea, black stool
  • iron deficiency- 3-4/day
135
Q

ferrous sulfate

A
  • iron
  • ferrous better absorbed-325mg/65mgiron
  • -nausea, epigastric pain, constipation, diarrhea, black stool
  • iron deficiency- 3-4/day
136
Q

cyanocobalamin

A
  • vitamin B12
  • anaphylaxis with IV, hypokalemia, secondary iron deficiency
  • parenteral for pernicious/resections-oral supplement deficient diet of B12
137
Q

folate

A

-folate
-
-mask B12 deficiency, reduce phenobarbital, phenytoin primidone, raltritrexed -all folate def. except for inhibiotrs of DHFR(leucovorin)

138
Q

deferoxamine

A
  • chelator
  • binds iron
  • IV can lead to hypotension, neurotoxicity, susceptible to infection
  • SubQ or IM for iron toxicity
139
Q

erythropoietin

A
  • 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
Q

Filgastrim

A

-Myeloid growth factor- G-CSF
-stim granulocyte colonies and neutrophils, promotes granulo release
-
-

141
Q

Sargramostim

A

-myeloid growth factor- GM-CSF
-w/IL3, stim prolif of gran, monoc, macro, megakaryocytes
-
-

142
Q

Penicillin G

A
  • 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
Q

Penicillin V

A
  • 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
Q

oxacillin

A
  • 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
Q

nafcillin

A
  • 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
Q

Amoxicillin

A
  • 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
Q

Ampicillin

A
  • 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
Q

Piperacillin

A
  • 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
Q

Carbenicillin

A
  • 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
Q

Clavulanic acid

A
  • beta-lactamase suicide inhibitor
  • structurally related to penicillins but poor antibiotic acitivity alone
  • NA
  • fixed concentrations with extended spectrum penicillins
151
Q

Sulbactam

A
  • beta-lactamase suicide inhibitor
  • structurally related to penicillins but poor antibiotic acitivity alone
  • NA
  • fixed concentrations with extended spectrum penicillins
152
Q

Tazobactam

A
  • beta-lactamase suicide inhibitor
  • structurally related to penicillins but poor antibiotic acitivity alone
  • NA
  • fixed concentrations with extended spectrum penicillins
153
Q

Cefazolin – 1st generation

A
  • 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
Q

Cefuroxime – 2nd generation

A
  • 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
Q

Cefotaxime – 3rd generation

A
  • 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
Q

Cefepime – 4th generation

A
  • 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
Q

imipenem

A
  • 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
Q

cilastatin

A
  • petidase inhibitor
  • inhibits dehydropeptidases
  • NA
  • imipenem always admin with cilastatin
159
Q

aztreonam

A
  • 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
Q

Bacitracin

A
  • 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
Q

D-Cycloserine

A
  • Non-beta-lactam
  • structural analog of D-alanine, blocks PDG synthesis
  • serious CNS effects, reversible
  • broad spec; restricted 2nd line for M. tuberculosis
162
Q

Fosfomycin

A
  • Non-beta-lactam
  • structural analog of PEP, blocks PDG synthesis
  • few adverse effects
  • single dose oral tx of uncomplicated UTIs (rapid resistance)
163
Q

Vancomycin

A
  • 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
Q

Daptomycin

A
  • Other-membrane depolarizer
  • Novel cyclic lipopeptide, cidal by membrane depolarization
  • myopathy
  • narrow spec G+ similar to vancomycin, treats VREF & MRSA
165
Q

gentamycin

A
  • 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
Q

neomycin

A
  • 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
Q

spectinomycin

A
  • aminocyclitol
  • binds 30s ribosomal subunit, bacteriostatic
  • NA
  • MRSA, enterococci, antibiotic-R gonorrhea
168
Q

tigecycline

A
  • glycylglycines
  • tetracycline analogue: reversible binding to 30s ribosomal subunit blocking A site
  • NA
  • tetracycline-R strains, Hershey isolate of MRSA
169
Q

tetracycline

A
  • 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
Q

doxycycline

A
  • 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
Q

minocycline

A
  • 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
Q

azithromycin

A
  • 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
Q

clarithromycin

A
  • 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
Q

erythromycin

A

-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
Q

telithromycin

A
  • 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
Q

clindamycin

A
  • 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
Q

quinupristin

A
  • 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
Q

dalfopristin

A
  • 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
Q

chloramphenicol

A

-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
Q

linezolid

A
  • 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
Q

mupirocin

A
  • protein synth inhibit other
  • inhibits isoleucyl tRNA synthetase; topical use ONLY
  • NA
  • impetigo caused by MRSA or Group A strep
182
Q

sulfamethoxazole

A

-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
Q

trimethoprim

A

-DHFR inhibitor
-DHFR inhibitor in folic acid synth pathyway (100,000x more selective for bacterial
over human); alone static
-NA
-combo with sulfamethoxazole;

184
Q

tmp-sulfa

A
  • 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
Q

ciprofloxacin

A
  • 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
Q

levofloxacin

A
  • 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
Q

moxifloxacin

A
  • 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
Q

Lanreotide

A
  • somatostatin analog
  • Acts on 2 & 5 receptors (not in pancreas)
  • gallstones
  • Hyper-GH syndromes

4 Pharm Unit (7 decks)

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