Pharmocolgy Unit 4 Flashcards
1
Q
penicillin G
A
penicillin; acid labile (IV or IM, not oral); procaine/benzathine forms -> water insoluble -> slow release over weeks; spectrum: gram+ and some gram- cocci (not gram- rods) adverse: allergies, neurotoxic, seizures, stevens-johnson syndrome (rash, swelling, blistering around mouth); uses: non penicillinase producing microbes
2
Q
penicillin V
A
penicillin; acid stable (orally effective-65% absorbed vs 35% for pen G)
3
Q
oxacillin
A
b-lactamase resistant; acid stable; food interferes w absorption; can be parenteral; spectrum/use: penicillinase-producing Staph and Strep; resistance: MRSA (BPB w low affinity for drugs); adverse: less than PenG,V, hepatitis at high dose
4
Q
amoxicillin
A
extended spectrum aminopenicillin; acid stable (oral - not affected by food); spectrum/use: non-lactamase gram- rods (E coli, H influenza, Salmonella, Shigella, not sub for penG,V), prophylaxis against bacterial endocarditis
5
Q
ampicillin
A
extended spectrum aminopenicillin; acid stable (oral); spectrum/use: non-lactamase gram- rods (E coli, H influenza, Salmonella, Shigella, not sub for penG,V),
6
Q
piperacillin
A
extended spectrum ureidopenicillin; parenteral admin; anti-pseudomonal; reserved for serious Klebsiella or Pseudomonas; combi w aminoglycosides to prevent resistance
7
Q
ticarcillin
A
extended spectrum caboxypenicillin; parenteral admin; antipseudomonal (rarely used alone)
8
Q
clavulonic acid
A
b-lactamase suicide inhibitor; no abx activity alone; used combi w extended spectrum penicillins (w amoxicllin = augmentin)
9
Q
sulbactam
A
b-lactamase suicide inhibitor; no abx activity alone; used combi w extended spectrum penicillins
10
Q
tazobactam
A
b-lactamase suicide inhibitor; no abx activity alone; used combi w extended spectrum penicillins
11
Q
1st gen cephalosporin/cephalexin
A
cephalosporin; most acid stable (oral); spectrum/use: broadest against gram+ (surgical prophylaxis, some gram- bacilli
12
Q
2nd gen cephalosporin/cefuroxime
A
cephalosporin; IV, IM; adverse: antabuse effect; spectrum/use: only group with significant activity against anaerobes (sinusitis, otitis, peritonitis, diverticulitis
13
Q
3rd gen cephalosporin/ceftazidime
A
cephalosporin: IV, IM; adverse: antabuse effect; resistance: induce AmpC; spectrum/use: anti-pseudomonal, -pneumococcal, serious gram- infections (meningitis, pneumonia, gonorrhea); used in children/infants with severe infection; pentrates CNS
14
Q
4th gen cephalosporin/cefepime
A
cephalosporin; IV, IM; resistance: indice AmpC; spectrum/use: anti-pseudomonal, high resistance to B-lactamases: useful in treating penicillin-resistant steptococci and enterobacter
15
Q
imipenem
A
carbapenem; has B-lactam ring-> blocks PDG x-linking; more efficient binding to PBPs than pcn or ceph; penetrates OM of gram-; broadest spectrum B-lactam drug (NOT MRSA, VRE); resistant to most B-lactamases but induces those that inactivate pcns and cephs; resistance: alterations in PBP; parenteral admin; renal metabolism and inactivation (admin w dehydropeptidase cilastatin); adverse: cross-allergenic w pcn, rare GI effects, superinfections, neurotoxic; uses: 2nd line therpay for serious nosocomial infection (klebsiella, E cloi)
16
Q
meropenem
A
carbapenem
17
Q
cilastatin
A
dehydropeptidase inhibitor
18
Q
aztreonam
A
monobactam; binds PBPs; relative resistance to B-lactamases; IV, IM use only (poor oral absorption); No X-reactitivity w pcns; spectrum: narrow, gram- aerobes (pseudomonas) NOT gram+, anaerobes; uses: gram- UTIs, lower RTIs, systemic infxn
19
Q
bacitracin
A
non-b-lactam PDG inhibitor; deple3tes lipid carrier for PDG synthesis; topical use only (poor absorption); narrow spectrum: gram+, Neisseria, T pallidum; toxicity: nephrotoxic; uses: skin and ophthalmic infection, combi w/ polymyxin B
20
Q
D-cycloserine
A
non-b-lactam PDG inhibitor; analog of D-ala, blocks D-ala addition (step2); good CNS penetration, oral, broad spectrum; toxicity: serious CNS effects; uses: 2nd line Tb drug
21
Q
daptomycin
A
cyclic lipopeptide, membrane depolarization; bactericidal; IV admin, renal excretion; spectrum/use: like vancomycin (gram+ including MRSA, ALSO TREATS VRE; adverse: myopathy $$$
22
Q
fosfomycin
A
non-b-lactam PDG inhibitor; analog of PEP, blocks step1 of PDG synthesis; broad spectrum; resistance: after multiple doses; toxicity: diarrhea, vaginitis; Uses: single dose oral tx for UTI by E. faecalis and E. coli
23
Q
vancomycin
A
non-b-lactam PDG inhibitor; binds D-ala terminus (substrate) and blocks X-linking of PDG; bacericidal in dividing cultures (except static in enterococci); IV admin (no IM) oral rarely (poor absorption); distributes to bone, meninges; renal excretion; narrow spectrum: gram+ (most MRSA); resistance: VRenterococci van genes, VRSA overexpress D-ala; toxicity: red man syndrome (too fast IV), ototoxic, nephrotoxic; uses: MRSA, pcn resistant S. pneumo (serious gram+ infections), combi w/ aminoglycosides-> expands spectrum to gram+
24
Q
amikacin
A
aminoglycoside; derivative of kanamycin but less toxic; treats bacteria resistant to genta/tobra, treats Mycobacteria Tb in combi therapy
25
gentamicin
aminoglycoside. resistance: poor drug uptake; synergistic w/ vanco or pcn -> extends use to gram+; main use: SEVERE GM- INFECTIONS (pseudomonas, klebsiella in HIV), topical for burns, wounds, skin lesions; adverse: ototoxic, mainly vestibular/ irreversible
26
neomycin (kanamycin)
aminoglycoside; limited to topical and oral use; widespread resistance; significant toxicity
27
tobramycin
aminoglycoside; very similar to gentamicin; more active against pseudomonas; uses: pseudomonas RTI in CF
28
streptomycin
aminoglycoside; high resistance linits use; uses: mycobacterial Tb (no longer 1st line bc of incr resistance); adverse: deafness in newborns when taken during pregnancy
29
spectinomycin
aminocyclitol; binds 30S->protein synthesis inhibitor->bacteriostatic; spectrum: mostly Gm- but also many Gm+; used in MRSA and enterococci, abx-resistant gonorrhea; given IM->rapid
30
tigecycline
first glycylglcine; tetracycline analog; similar to tetracycline but binds 30S higher affinity; uses: strains that are tetracycline-resistant and Hershey isolate of MRSA (VRSA); adverse: well tolerated, n/v
31
tetracycline
tetracycline; reversible bind 30S->bacteriostatic; deposits in bone in anactive form -> teeth discoloration, poor bone development in children; can cross placenta; excreted by kidneys; spectrum: very broad -> superinfections; uses: acne, rickettsia, chlamydia, mycoplasma, yersinia, borrelia; adverse: Gi irritation, C. diff colitis, heptotoxic, nephrotoxic; DONT give to pregnant women or children<8yo
32
doxycycline
tetracycline; best absorption among tetracyclines; photosensitivity; eliminated as inactive chelate in feces -> no affect on normal flora=safer
33
minocycline
tetracycline; vestibular disturbance in women; metabolized by liver ->feces
34
azithromycin
macrolide; more effective than erythromycin against anaerobes; unclear mechanism of excretion; adverse: structurally different from other macrolides and does NOT induce CYP3A4
35
clarithromycin
macrolide; more effective than erythromycin against anaerobes; metabolized in liver -> excreted by kidney; inhibits CYP3A4 -> affect on mulitple drugs: theophylline, warfarin, carbamazepine,
36
erythromycin
macrolide; only acid labile; penetrates into abscesses; excretion in bile; hepatotoxic: cholestatic hepatitis with erythromycin estolate (reversible); inhibits CYP3A4 -> affect on mulitple drugs: theophylline, warfarin, carbamazepine,
37
telithromycin
1st member of new drug class; semi-synthetic erythromycin derivative; increased acid stability, increased 50S affinity, reduces induction of resistance, not induce cross-R; binds 50S at 2 sites; conc-dependant bacericidal vs S. pneumoniae; oral -> well absorbed; hepatic metabolism, renal excretion; MLS-typeB is resistant to drug; uses: S pneumonia, H influenza, M catarrhalis, S aureus; CA-RTIs (pneumonia), bacterial sinusitis, chronic bronchitis; adverse: GI, diarrhea, nausea, abd pain, exacerbation of disease in myasthenia gravis; competes for CYP3A4 with other drugs
38
clindamycin
lincosamide; binds 50S (MLS-B resistance); spectrum: most Gm+, better than macrolides vs anaerobes, esp B. fragilis (non-CNS), NOT Gm-; bacteriostatic; Resistance: slow, stepwise from methylase(MLS-B (erm), does not induce methylase expression; oral or parenteral; wide distribution including bone (active) low [] in CNS; metabolized by liver-> bile, renal excretion IMPAIRED IN HEPATIC FAILURE; uses: RTIs by anaerobes, GAS, MRSA, osteomyelitis; adverse: pseudomembranous colitis, rash, steven-johnson syndrome, anaphylaxis
39
quinupristin/dalfopristin (synercid)
streptogramins; IV; quinupristin binds 50S, dalfopristin enhances binding (bactericidal effect together, bacteriostatic individually); uses: MRSA, serious vanco-resistant Gm+ VRE, VRSA, S. pneumonia; adverse: pain, phlebitis at IV site; affects CYPs; resistance: quinupristin (erm-encoded methylase-> modify 50S ->MLS-B resistance, vgb-encoded lactonase -> modify drug); dalfopristin (vat/sat-encoded acetyltransferase ->modify drug, vga/vgb-encoded efflux pump)
40
sulfamethoxazole
sulfonamide; first abx used in US; competitively inhibits binding PABA to DHPS (high PABA (pus) inhibits activity); bacteriostatic; Selective: DHPS only function in bacteria, bacteria must synthesize folic acid; oral or IV; distributes all over incl CNS/CSF; hepatic metabolized -> renal excretion; spectrum: broad (many Gm+/-) also some arasites (plasmodium, toxoplasma) NOT rickettsia; Resistance: Staph, Strep, Enterobacteriaceae, Neisseria; X-resistance to all sufa: overproduce PABA, mutatnt DHPS, incr efflux; adverse: GI, rash, hemolytic anemia in G6PD deficiency, kernicterus in infants (compete w bili for albumin -> incr unconjugated bili}, stevens-johnson syndrome, marrow/hepatic toxic (uncommon) Uses: malaria, CNS toxoplasmosis, combi w trimethorpim for common infections
41
chloramphenicol
reversible binds 50S (subject to MLS-B resistance); bacteriostatic (-cidal from H influeza, N meningitidis; spectrum: very broad, most anaerobes, Gm- bacilli; resistance: drug modification, MLS-B); oral,parenteral; cross placenta; penetrates CNS; metabolized in liver-> renal excretion; uses: FEW, due to toxicity, those normally treated by tetracyclines that cant take them; adverse: hematologic, aplastic anemia, hypersensitivity, gray baby syndrome, inhibits CYPs
42
linezolid
binds novel site in 23S rRNA of 50S subunit (no MLS-B resistance); bacteriostatic; oral ->100% bioavailable; uses: tx MRSA, VREf, multi-drug resistant S. pneumoniae; No X-resistance w other protein synthesis inhibitors
43
mupirocin
topical use only; uses: impetigo from MRSA, GAS; inhibits isoleucyl tRNA synthase; rapidly metabolized to inactive (topical only); resistance reare
44
Trimethoprim
inhibits bacterial DHFR 100,000X better than humn DHFR; bacteriostatic alone;
45
tmp-sulfa
synergistic; bactericidal; oral; wide distribution; excreted in urine; spectrum: many Gm+/-, NOT pseudomonas, anaerobes, atypical bacteria; resistance: overexpress DHFR, mutant DHFR (plasmid); adverse: same as sulfas,bone marrow suppression and neutropenia, cause anti-folate effect; Uses: UTIs (decr efficacy among E coli); pneumocystis pneumonia in AIDS/transplant, sinusitis, otitis media, CA-MRSA
46
ciprofloxacin
fluoroquinolone; better for Gm- (incl pseudomonas); 2nd line anti-Tb
47
levofloxacin
fluoroquinolone; same for Gm+/-
48
moxifloxacin
fluoroquinolone; better for Gm+ (incl Strep)
49
amphotericin B
polyene; binds ergosterol-> forms pores-> ion leak -> cell death; broadest spectrum antifungal; uses: most life-threathening systemic infections (candida, aspergillus, cryptococcus) initial therapy; fungicidal; adverse: cholesterol binding accounts for toxicity; resistance: decreased ergosterol (azole tx); poor oral absorption -> used orally for GI topical tx, topical for superficial infxn, parenteral for systemic; extensive metabolism->excreted over 2 weeks by kidney; distribution in RE in lipid formulation ->liver, lung, spleen; NOT kidney (reduce toxicity), CSF (not for fungal mieningitis); adverse: local irritation, IV->immediate rxn to infusion: fever, chills, spasm, headache, hypotn, anaphylaxis, thrombophlebitis; IV->nephrotoxicity (reversible); drug interactions: incr digitalis toxicity, antagonize azoles, enhanced nephrotoxicity w aminoglycosides, cyclosporine
50
nystatin
polyene; similar to AmpB; narrower spectrum than AmpB; TOO toxic for parenteral use; not metabolized; topical only (not well absorbed by GI, skin, mucous membranes; uses: topical for superficial mucosal, skin, vaginal candida; drug of choice for oral cavity infections; adverse: mild but bitter and unpleasant taste
51
clotrimazole
imidazole; restricted to oral/topical use; effective and more palatable than alternative nystatin; drug of choice for oropharyngeal candidiasis in AIDS; swallowed drug mild Gii upset->metabolized by liver
52
ketoconazole
imidazole; GREATEST propensity to inhibit mammal CYPs -> inhibit adrenal/gonadal steroig synthesis, interfere with other drug metabolism; cause symptomatic hepatitis; availability of safer drugs makes use limited
53
miconazole
imidazole; use limited by toxicity: thrombophlebitis p IV; effective topically vs candidiasis; uses: oropharyngeal candidiasis
54
fluconazole
triazole; similar to ketoconazole (more selctive for fungal CYPs); best CNS penetration (cryptococcal meningitis); resistance: Candida krusei (instrinsic) glabrata (common), NOT active against aspergllus mold; good oral bioavailablility (water soluble), IV available; uses: most common systemic antifungal; 1st line for invasive candida (not krusei), cryptococcal meningitis
55
itraconazole
triazole; broader spectrum than flconazole: includes dimorphic (histoplasma, blastomyces, coccidioidses, and aspergillus mold); absrobed well orally, IV available; uses: aspergillus and fluconazole-resistant candida
56
posaconazole
tirazole; newest azole; similar to voriconazole but only azole w activity vs zygomycoses (rhizopus, mucor); good oral bioavail; toxicity: rash, incr hepatic enzymes, no visual effects; numerous drug interactions; FDA approved for prophylaxis of invasive fungal infections (BMT w GvsHD, hematologic malignancy, and neutropenia)
57
voriconazole
triazole; same spectrum as itraconazole, more potent vs yeast and molds; excellent oral bioavail; low toxicity (transient visual side effects, rash, incr hepatc enzymes (inhibits CY3A4); uses: immunoompromised pts, aspergillosis (better survival vs AmpB, new standard of care?) fusarium infection, fluconazole-resistant candida
58
terbinafine
allylamine; inhibits ergosterol synthesis blocking aqualene epoxidase; fungicidal (elevated squalene=toxic); spectrum: dermatophytes (same as griseofluvin); topical or oral->good absorption-> accumulates in skin, nails, and fatty tissue (dermatophyte sites of infection); drug interactions: admin w rifampin doubles clearance of terbinafine, admin w cimetidine decr clearance by 1/3; uses: mainstay for skin, nail infections, unusual, refractory infetions.
59
anidulafungin
glucan synthesis inhibitor
60
caspofungin
glucan synthesis inhibitor-> weakens cell wall->lysis; spectrum: primarily aspergillus, azole-resistant candida; given IV; uses: (well tolerated) invasive candida, aspergillus, molds
61
micafungin
glucan synthesis inhibitor
62
flucytosin
5-fluorocytosine; orally effective for systemic cadida/cryptococcus meningitis; fungistatic; converted to 5-FU-> inhibits thymidylate synthetase->blocks DNA synthesis and protein synthesis; human cells inefficienty convert to 5-FU; uses: combi w fluconazole, AmpB ->synergistic effect (allows for reduced AmpB dose); resistance: common, enzyme mutations; high oral biovailable, good CNS penetration, renal excretion; adverse: GI intolerance, marrow depression->anemia, lukopenia, thrombocytopenia
63
griseofluvin
assoc w polymerized microtubules -> blocks mitosis; only use: oral/systemic tx for dermatophytosis (limited use); induces various CYPs -> alters warfarin, oral contraception, etc.
64
ferrous fumurate
iron
65
ferrous gluconate
iron
66
ferrous sulfate
iron
67
deferasirox
chelator
68
deferoxamine
chelator
69
Vit B12
vit
70
erythropoietin
growth factor; stimulates proliferation, maturation, and hemoglobin formation by erythroid progenitors; acts synergistically w IL-3 and GM-CSF; stimulates relsease of reticulocytes from marrow to circulation; uses: anemia of chronic renal failure, anemia in AIDS pts treated w AZT, anemia w cancer chemo, preoperatively for autologous transfusion; adverse: increased clotting, HTn, seizures, allergic rxn mild
71
G-CSF
growth factor; stimulates granulocyte colonies and neutrophi production
72
GM-CSF
growth factor; w IL-3 stimulates proliferation of granulocytes, monocytes, and megakaryocytes
73
ethambutol
1st line antiTb; active gainst mulitplying bacilli; blocks cell wall synthesis; resistance from embB gene mutation (arabinosyl transferase); adverse: optic neuritis (decr VA, red-green color blindness)
74
isoniazid (INH)
1st line antiTb; kills actively growing bacteria; passive penetration; used as single drug for latent Tb; prodrug activated by Tb enzyme; inhibits fatty acid synthase type II system; adverse: peripheral neuropathy (give vit B6), elevated liver enzymes, fatal hepatitis (pregnant/postpartum women)
75
pyrazinamide
1st line antiTb; prodrug -> intracellular PZA; kills less metabolically active when low proton pump action
76
rifampin
1st line antiTb, anti-leprosy; active against rapidly growoing and slow metabolizing bacilli, good penetration; inhibits prokaryotic RNA polymerase; broad spectrum Gm+/-; resistance by mutation in rpoB gene; adverse: orange color in urine, sweat, tears, rash, thrombocytopenia, nephritis, hepatitis, and drug interactions
77
streptomycin
1st line antiTb
78
capreomycin
2nd line antiTb
79
kanamycin
2nd line antiTb; blocks protein synthesis (16S rRNA)
80
rifabutin
anti MAC
81
dapsone
anti-leprosy; used in MDT form leprosy; inhibits synthesis of dihydrofolic acid-> blocking DNA/RNA synthesis; adverse: hemolysis, hepatitis, nausea and rash
82
aspart
rapid acting insulin (faster than wild type) aa sequence change (B28 pro->asp) promotes absorption by preventing self-assoc
83
detemir
long acting insulin; aa sequence change (c-terminus thr deleted, myristic acid added to c-terminus lys) incr self aggregation and binding to albumin
84
glargine
long acting insulin; aa sequence change (A21 asn->gly, arg added at B31,32) makes insulin soluble in acidic solution but precipitate at neutral pH, decr absorption
85
glulisine
rapid acting insulin (faster than wild type) aa sequence change (B3, B29 asn->lys, lys->glu) promotes absorption by preventing self-assoc
86
lispro
rapid acting insulin (faster than wild type) aa sequence change (B28,B29 pro->lys, lys->pro) promotes absorption by preventing self-assoc
87
NPH
intermediate acting insulin (slower than wild-type) wild-type sequence suspended in protamine -> forms complex that decr absorption (use waning in favor of long-acting)
88
regular crystalline insulin
short acting insulin (slower than wild-type) with wild-type
89
exenatide
incretin agonist; SQ injection; adverse: nausea, anorexia, headache, diarrhea, pancreatitis
90
sitagliptin
inhibitor of incretin degredation; oral; adverse: headaches, increased rate of infections, pancreatitis
91
pramlintide
synthetic amylin analog; SQ; used in DMII; given w insulin in DMI; inhibits glucagon secretion and has CNS-mediated anorectic effects; adverse: hypoglycemia, nausea, vomiting, anorexia
92
chlorpropamide
1st gen sulfonylurea; ~60 hr duration
93
glipizide
2nd gen sulfonylurea; 10-24 hr duration
94
glyburide
2nd gen sulfonylurea; 10-24 hr duration
95
glimepiride
2nd gen sulfonylurea; 12-24 hr duration
96
tolbutamide
1st gen sulfonylurea; 6-12 hr duration
97
repaglinide
meglitinide; same mechanism as sulfonylureas; more potent than 2nd gen sulfonylureas but shorter durtion (4-5 hr); adverse: hypoglycemia, use caution in renal/hepatic failure
98
nateglinide
D-phenylalanine analog; same mechanism as sulfonylureas/meglitinides; more potent but less sustained; adverse: hyoglycemia and other effects less pronounced than in meglitinides; safer in renal failure
99
metformin
biguanide; activate AMP-activated protein kinase (energy sensor); reduces hepatic glucose output; first choice drug for DM II; adverse: Gi discomfort, lactic acidosis, NO hypoglycemia
100
rosiglitazone
thiazolidinedione; increase insulin sensitivity in liver, fat, muscle: adverse: increase risk of heart failure and stroke *restricted by FDA
101
pioglitazone
thiazolidinedione; increase insulin sensitivity in liver, fat, muscle: adverse: increase risk of heart failure and bladder cancer
102
acarbose
a-glucosidase inhibitor; reduce carbohydrate absorption from gut
103
miglitol
a-glucosidase inhibitor; reduce carbohydrate absorption from gut
104
bromocriptine
D2 selective agonist; oral; incr morning dopaminergic activity -> incr insulin sensitivity and decr hepatic glucose output; adverse: nausea, fatigue; dizziniess, vomiting, headache, NO hypoglycemia or wt gain; ?? efficacy
105
canagliflozin
inhibitor of glucose/Na cotransport (SGLT2) in convoluted tubule in kidney->inhibit glucose reabsorption; oral; adverse: UTIs, increased urination
106
thyroxine
T4; potency=1; half-life 7days; less expensive; converted to T3 in periphery; oral IV, IM, tx lifelong
107
triiodothyronine
T3; potency=4; half-life 1 day; more expensive; oral, IM, IV for emergency myxedema coma; adverse: thyrotoxicosis, stress on CV system
108
propylthiouracil
thioamine; inhibits thyroid peroxidase: oxidation, iodination, coupling; also inhibits T4->T3 conversion; faster than MMI but less potent and shorter duration; treatment for pregnant women (instead of MMI)
109
methimazole
thioamine inhibits thyroid peroxidase: oxidation, iodination, coupling; slower but more potent than PTU; not used in hyperthyroid pregnant women during 1st tri
110
potassium iodide
inhibits release of T3 and T4; inhibits synthesis of T3 and T4; oral; course is fast but effect is transient; not sole therapy; adverse: safe and reversible, rash, swollen salivary glands; used to prevent I131 after nuclear accident
111
radioactive iodine
I131; concentrates in thyroid and causes local radiation damage; oral; adverse: delayed hypothyroidism, radiation exposure; time course slow (weeks); NOT used in pregnant/nursing mothers
112
propranolol
B blocker; alleviate symptoms of incr CV activity from hyperthyroid
113
cortisol
glucocorticoid; oral, injectable, topical; some MC activity
114
dexamethasone
pure glucocorticoid (no MC activity); oral, injectable, topical
115
prednisolone
glucocorticoid; oral, injectable; decr MC activity
116
fludrocortisone
Only mineralocorticoid; oral only; has GC activity; only useful as replacement therapy in adrenal insufficiency; adverse: fluid/electrolyte abnormalities, hypertension
117
spironolocatone
mineralocorticoid ; also androgen antagonist
118
eplerenone
mineralocorticoid antagonist; no anti-androgen activity
119
aminoglutethimide
inihibits conversion of cholesterol to pregnenolone (first step) t treat cushings
120
metyrapone
inhibits conversion of 11-deoxy to cortisol and corticosterone to treat cushings syndrome
121
ketoconazole
inhibits many steps in steroid synthesis to treat cushings
122
progestin+estrogen as contraception
discontinuous or continuous admin; main effect pituitary/hypothalamus; predictable menstrual periods;
123
ethinyl estradiol
estrogen in progestin+estrogen contraception
124
estrone sulfate
estrogen
125
diethylstilbestrol
estrogen; among first non-steroidal estrogens used; not used any more
126
tamoxifen
SERM; agonist everywhere but breast; PM symtoms, osteoporosis, E-dependant Breast CA
127
raloxifene
SERM; antagonist in breast and endometrium, neutral in vag epithelium; PM symptoms, osteoporosis, E-dependant breast CA
128
ospemifene
SERM; antagonist breast neutral in endometrium; approved for tx of vaginal atrophy in PM women
129
clomiphene
estrogen receptor antagonist; ovulation induction
130
fulvestrant
estrogen receptor antagonist; ovulation induction
131
anastrozole
non-steroidal aromatase inhibitor; tx estrogen-dependant breast CA; ovulation induction; adverse: hot flushes, plasma lipids and bone resorption
132
exemestane
steroidal aromastase inhibitor; tx estrogen-dependant breast CA; ovulation induction; adverse: hot flushes, plasma lipids and bone resorption
133
drospirenone
progestin; enhanced acitivity as mineralocorticoid and androgen antagonists; also as progestin in progestin+estrogen oral contraception
134
progesterone only contraception
continuous admin; prevents fertilization by decreasing amount and increasing viscosity of cervical mucus; prevent ovulation by inhibiting HPO axis; adverse: headache, abnormal menstrual bleeding
135
medroxyprogesterone acetate
progestin only contraaception; IM injection every 3 months (depo-provera)
136
norethindrone
progestin only contraception; oral daily; IUD 5 yrs; also in progestin+estrogen oral contraception
137
norgestrel
progestin only contraception; oral daily; IUD 5yrs; postcoital contraception (higher dose, effective within 72 hrs of intercourse) NON PRESCRIPTION->adverse: n/v, headache, breast tenderness, abd cramps
138
ulipristal
SPRM; can be agonist or antagonist, depending on tissue; postcoital contraception; effective within 5 days of intercourse; inhibits ovulation by progesterone antagonism; prescription needed; drug of choice in ER
139
RU-486 (mifepristone)
progestin receptor antagonist; abortion w prostaglandin; also glucocorticoid antagonist used in cushings and DM II
140
FSH
gonadotropin; induce follicular growth
141
CG
gonadotropin; induce ovulation (like LH); diagnostic marker of pregnancy
142
gonadorelin
GnRH; stimulate gonadotropin secretion to treat delayed puberty in boys or girls and anovulatory women; admin as single injection fo via pump (pulsatile)
143
luprolide
GnRH agonist; after initial stimulation secretion is suppressed (desensitization) used as antiandrogen like antagonist
144
cetrorelix
GnRH antagonist; treat precocious puberty in boys and girls and androgen excess in males; treat endometriosus and dysmenorrhea; stop GnRh in ovulation-inductionprotocol
145
testosterone
androgen
146
testosterone propionate
androgen
147
methyltestosterone
17a-alkylated androgen; orally active
148
danazol
17a-alkylated androgen; orally active but more side effects (hepatotoxic)
149
dutasteride
5a-reductase inhibitor; antiandrogen
150
finasteride
5a-reductase inihibitor; antiandrogen
151
bicalutamide
androgen receptor antagonist
152
flutamide
androgen receptor antagonist
153
nilutamide
androgen receptor antagonist
154
progestin (noncontraception use)
suppress HPO axisto treat dysmenorrhea and endometriosis; P+E replacment therapy in ovarian dysfunction ad postmenopausal
155
growth hormone
human growth hormon; recombinant; SQ once daily or IM once/twice a month
156
sermorelin acetate
synthetic GHRH analog; for functioning pituitary
157
IGF-1
human, recombinant; used only in syndromes of GH resistance
158
pegvisomant
GH antagonist; SQ injection; nine aa mutation from wild-type GH; binds GH receptor but doesnt allow dimerization
159
ocreatide
somatostatin agonist; IM or SQ injection; selective for somatostatin receptor in pituitary; inhibit GH release; adverse: nausea, flatulence, ad pain, gallstones (20-30% incidence)
160
lanreotide
somatostatin agonist; IM or SQ injection; selective for somatostatin receptor in pituitary; inhibit GH release; adverse: nausea, flatulence, ad pain, gallstones (20-30% incidence)
161
bromocriptine
D2 agonist; oral; treat hyperprolactinemia -> amerorrhea, galactorrhea, infertility; adverse: nausea, headaches, orthostatic hypotension (adrenergic response)
162
cabergoline
D2 agonist; oral; treat hyperprolactinemia -> amerorrhea, galactorrhea, infertility; adverse: nausea, headaches, orthostatic hypotension (adrenergic response)
163
desmopressin
synthetic vasopressin
164
oxytocin
from post pituitary; modulates ion channels in myometrium to induce smooth muscle contraction in uterus; induces labor; V1-> or IM
165
vasopressin
acts on V1 -> vasoconstriction; V2 -> renal collecting tubule water resorption; replcement therapy for diabetes insipidus; oral, IV, SQ, or intranasal
166
Vit D
incr calcium absortion for GI tract
167
Vit D2 (ergocalciferol)
incr calcium absortion for GI tract
168
Vit D3 (calcitriol)
incr calcium absortion for GI tract
169
PTH/teriparatide
PTH;normally stimulate bone resorption; given at daily low dose leads to osteoblast stimulation and new bone formation;
170
calcitonin
from thyroid C cells; SQ, IM, intranasal; inhibit bone resorption and incr calcium excretion by kidneys -> decr serum calcium
171
alendronate
bisphosphonate; oral or parenteral; inhibits bone resorption
172
etidronate
bisphosphonate; retards dissolution of hydroxyapatite; slows osteoclasst resorption of bone; parenteral
173
pamidronate
bisphosphonate; parenteral; inhbits bone resorption
174
risedronate
bisphosphonate; oral or parenteral; inhibits bone resorption
175
tiludronate
bisphosphonate; oral or parenteral; inhibits bone resorption
176
denosumab
RANKYL antibody; inhibits bone resorption by binding RANKligand and prevent binding to RANK; RANK is osteoclast receptor that stimulates resorptive activity
177
enfuvirtide
HIV antiviral, entry inhibitor; injection; peptide mimic binds to HIV gp41 -> blocks membrane fusion; adverse: immunogenic->inflammation; resistance form gp41 mutations
178
maraviroc
HIV antiviral, entry inhibitor; small molecule inhibitor; binds CCR5 allosterically preventing HIV gp120/CCR5 interaction; testing for CXCR4 efficacy; resistance: gp120 mutations; salvage therapy; microbicide to block sexual transmission
179
AZT (zidovudine)
HIV antiviral, NRT inhibitor
180
emtricitabine
HIV antiviral, NRT inhibitor
181
lamivudine
HIV, hepatitis B antviral, NRT inhibitor
182
tenofovir
HIV antiviral, NtRT inhibitor; adverse: competes with other drugs for kidney tubule secretion; other hiv and herpes antiviral will elevate tenofovir in serum
183
efavirenz
HIV antiviral, NNRT inhibitor
184
nevirapine
HIV antiviral, NNRT inhibitor
185
ralgravir
HIV antiviral, integrase inhibitor; resistance from aa changes in integrase
186
ritonavir
HIV antiviral, protease inhibitor; blocks CYP 3A4
187
saquinavir
HIV antiviral, protease inhibitor; combination w ritonavir incr availability; many known drug interactions
188
palivizumab
RSV antiviral ab, entry inhibitor; prophylaxis for infants/children >2 yrs with CLD
189
ribavarin
guanosine analog; inhibits inosine monophosphate dehydrogenase resulting in GTP depletion (decr 5 capping of RNA); can base pair with cytidine or uridine -> mutations -> highly defective viral genome; mutations can bestow resistance; causes shift in Th1 to Th2 pheotype of CD4+ cells; Best broad spectrum antiviral available; treat hospitalized infant with RSV; standard of care for Hep C w IFNa
190
pegylated interferon
generates antiviral state in virally infected and nearby cells; HBV sensitive to antiviral state; standard of care for Hep C w ribavarin
191
acyclovir
a-herpes antiviral, nucleoside analog; effective 1st line drug; prodrug selectively activated by viral nucleoside kinase; no 3-OH; uses: tx HSV, VZ (immunocompromised), prophylaxis in BMT, HSV encephalitis (not very successful); short half-life, poor oral absorption; (elevate tenofovir levels
192
cidofovir
a,B,gamma-herpes antiviral, nucleoside analog; acycic nucleoside phosphonate derivate of cytosine; converted to active ANP-diphosphate by cellular kinase (no need for viral kinase and retain activity against TK (kinase) negative/altered HSV); competitive inhibitor of viral DNA polymerase and act as chain terminator
193
famciclovir
a-herpes antiviral, nucleoside analog; prodrug of penciclovir; oral
194
penciclovir
a-herpes antiviral, nucleoside analog; acyclic guanine derivative w 3-OH -.allows short chain extension but still causes termination
195
valacyclovir
a-herpes antiviral, nucleoside analog; effective 1st line drug; prodrug selectively activated by viral nucleoside kinase; no 3-OH; uses: tx HSV, VZ (immunocompromised), prophylaxis in BMT, HSV encephalitis (not very successful); povides more sustaing and higher levels in serum than acyclovir; (elevate tenofovir levels)
196
foscarnet
a,B,gamma-herpes antiviral, non-nucleoside analog of pyrophosphate -> binds to pyrophosphate -binding site on viral DNA polymerase -> noncompetitive inhibits polymerase activeity; 100X more selective for viral vs cellular polymerase
197
docosanol
a-herpes antiviral, non-nucleoside analog; saturates fatty alcohol that is approved as topical cream; mixed evidence of efficacy
198
ganciclovir
B,gamma-herpes antiviral, nucleoside analog; hydroxymethylated derivative of acyclovir; IV for life-threatening CMV infection (retinitis); effect beter than acyclovir on HSV, VZV, and CMV but TOXIC; adverse: granulocytopenia, thrombocytopenia, may not be reversible
199
fomivirsen
B,gamma-herpes antiviral, antisense RNA against CMV that can be used against CMV retinitis in immunocompromised pts
200
amantadine
influenza antiviral, uncoating inhibitor (resistance is widespread); block acidification of virion in endosome by binding M2; only works with influenza A; must be administered withine 48 hrs of onset, and prophylaxis; antiparkinson drug
201
oseltamivir (tamiflu)
influenza antiviral, neuraminidase inhibitor; blocks release of virion; works for A nd B; oral
202
zanamivir
influenza antiviral, neuraminidase inhibitor; blocks release of virion from cel; works with A and B; aerosol
203
telaprevir
hepatitis C antiviral, protease inhibitor; 12 week course parallel w IFNa and ribavarin; adverse: rashes, anemia and elevates statins in blood when taken together
