Pharm Exam 3

Front 1

CO: mechanism of toxicity?

Back 1

[asphyxiant]

competitively binds Hb 200x better than O2

Front 2

CO toxicity: Tx?

Back 2

[asphyxiant]

100% O2

Front 3

CN: mech of toxicity?

Back 3

[asphyxiant]

binds Fe3+ of complex IV of electron transport chain (cyt a3) --> chain can't deliver e- to O2 = NO ATP SYNTH!

Front 4

CN toxicity: Tx?

Back 4

[asphyxiant]

Nitrite (NO2-)

inhalation/injection
rhodanase (body enzyme) converts CN- into SCN- (thiocynate) and SO3

Front 5

What is a chemical Asphyxiant?

Back 5

interfere with cell's ability to get/use O2

Front 6

What's the risk for paint strippers?

Back 6

methylene dichloride can be converted to CO (asphyxiant) in liver

Front 7

List the URT pollutants?

Back 7

SO2 (Sulfur dioxide)

Front 8

List the deep lung pollutants?

Back 8

O3 (Ozone), NO2 (Nitrogen dioxide)

Front 9

CO: Sx of toxicity?

Back 9

[asphyxiant]

tissue hypoxia: HA, confusion, syncope, tachycardia, brain damage

Front 10

Which pollutants are water soluble?

Back 10

SO2

(not O3 or NO2)

Front 11

MC Sx SO2 poisoning?

Back 11

[pollutant]

bronchoconstriction (esp asthma pt)

also conjunctival irritation

Front 12

Which Pollutants have immediate irritation vs. delayed irritation?

Back 12

immediate: SO2

delayed: O3, NO2

Front 13

Sources of SO2?

Back 13

[pollutant]

burning coal, acid rain

Front 14

What pollutant are farmers at risk for?

Back 14

NO2, found in silage (cowfeed)

Front 15

List the Aromatic hydrocarbons?

Back 15

[solvents]

Benzene, Toluene, Xylene

Front 16

Aromatic hydrocarbons: mech of toxicity?

Back 16

[solvents] (Benzene, Toluene, Xylene)

Organic solvents are CNS depressants

liver: Benzene metabolized (epoxidation) by P450 --> becomes mutagenic (genotoxin)

BM: Benzene is myelotoxic (thrombocytopenia, leukopenia, aplastic anemia)

Front 17

List the Alcohol solvents?

Back 17

Methanol, Ethylene glycol

Front 18

Methanol: mech of toxicity?

Back 18

[alcohol solvents]

metabo'd to Formaldehyde: binds proteins, water soluble, URT irritant

Formaldehyde metabo'd into Formic Acid: retinal toxicity, systemic acidosis

Front 19

Methanol toxicity: Tx?

Back 19

[alcohol solvents]

Ethanol: competes w/ methanol for metabolic enzymes (ADH) - so methanol not broken down to toxic Formaldehyde and Formic acid

Front 20

Ethylene glycol (antifreeze): mech of toxicity?

Back 20

[alcohol solvents]

metabo'd to Oxalic acid: acidosis, kidney damage (oxalate crystals)

Front 21

List the toxic Solvents?

Back 21

Aromatic hydrocarbons: Benzene/Toluene/Xylenes
Alcohols: Methanol, Ethylene glycol
Aliphatic hydrocarbons (gasoline)
Halogenated hydrocabons (methylene chloride, chloroform, CCl4, halothane)

Front 22

Halogenated hydrocarbons: mech of toxicity?

Back 22

[solvents] (methylene chloride, chloroform, CCl4, halothane)

P450 dependent:
methylene chloride --> CO (asphyxiant)
chloroform --> phosgene (pneumonitis)
CCl4 --> CCl3' radical
halothane --> radical (halothane hepatitis)

Also CNS depression, nephrotoxic, hepatotoxic, genotoxic

Front 23

List the Organophosphates?

Back 23

[insecticides]

Parathion, Malathion

Front 24

Organophosphates: MOA?

Back 24

[insecticides] (Parathion, Malathion)

Inhibits AChE via phosphorylation --> ACh accumulation paralyzes cholinergic transmission in CNS/PNS = kills insect!

Front 25

Organophosphate: Tx?

Back 25

[insecticides] (Parathion, Malathion)

Pralidoxime: dephosphorylate AChE --> reactivates

Atropine: reverse cholinergic poisoning

Cholestyramine: ^fecal excretion

Front 26

Organophosphates: Sx of toxicity?

Back 26

[insecticides]

"cholinergic poisoning": pinpoint pupils, sweating, bronchoconstriction, m fasciculations, paralysis

MCC death: resp failure

OPIDN (organophosphate-induced delayed neuropathy): ataxia, paralysis, axon/myelin degeneration, UMN lesion in legs

Front 27

List the Carbamates?

Back 27

[insecticides]

Carbaryl, Baygon

Front 28

Carbamates: MOA?

Back 28

[insecticides] (Carbaryl, Baygon)

inhibit AChE by carbamoylation

Front 29

Carbamates: Sx of toxicity?

Back 29

[insecticides] (Carbaryl, Baygon)

"cholinergic poisoning" (like Organophosphates): pinpoint pupils, sweating, bronchoconstriction, m fasciculations, paralysis

Front 30

Carbamates: Tx?

Back 30

[insecticides] (Carbaryl, Baygon)

Oximes (decarbamylater)

(Pralidoxime not effective, used for Organophosphates)

Front 31

Nicotine: MOA?

Back 31

[insecticides]

ANS ganglion, NMJ blocker

Front 32

Nicotine: toxicity?

Back 32

[insecticides]

@ high doses: loss of m fxn, resp paralysis

Front 33

List the Household insecticides?

Back 33

Pyrethrum, Rotenone

Front 34

Rotenone: MOA?

Back 34

[household insecticides]

bind complex I of ETC --> no ATP synth!

Front 35

Rotenone: toxicity?

Back 35

[household insecticides]

GI irritation

Front 36

Pyrethrum: toxicity?

Back 36

[household insecticides]

affects CNS: excitation, convulsions, tetanic paralysis

Front 37

Pyrethrum: Tx?

Back 37

[household insecticides]

Ivermectin (Cl- agonist)

Front 38

List the Herbicides?

Back 38

Paraquat, Chlorophenoxy compounds (agent orange)

Front 39

Chlorophenoxy cmpds: MOA?

Back 39

[herbicides]

probably uncoupling of oxidative phosphorylation

Front 40

Chlorophenoxy cmds: Sx of toxicity?

Back 40

[herbicides]

infertility, carcinogenic (NHL), teratogenic, coma/hypotonia

Front 41

Chlorophenoxy cmpds: toxic contaminant?

Back 41

[herbicides]

TCDD (2,3,7,8-TetraChloroDibenzo-p-Dioxin) is toxic

Front 42

Paraquat: mech of toxicity?

Back 42

[herbicides]

metabo'd to free radical (O2-) --> causes lipid peroxidation

Front 43

Paraquat: Sx of toxicity?

Back 43

[herbicides]

lung (edema, fibrosis)

Front 44

Paraquat: Tx?

Back 44

[herbicides]

gastric lavage (rinsing), mineral adsorbents, hemoperfusion

CI: hyperbaric O2 (exacerbates oxidative damage)

Front 45

List the Insecticides?

Back 45

Nicotine
Organophosphates (Parathion, Malathion)
Chlorinated hydrocarbons (DDT, lindane)
Carbamates (Carbaryl, Baygon)
Household insecticides (Pyrethrum, Rotenone)

Front 46

Warfarin rodenticide: MOA?

Back 46

inhibit vit K-dependent factors (coags: II, VII, IX, X); massive systemic hemorrhage

Front 47

List the Chlorinated hydrocarbons?

Back 47

[insecticides]

DDT, Lindane

Front 48

Chlorinated hydrocarbons: MOA? Sx of toxicity?

Back 48

[insecticides] (DDT, Lindane)

inhibition of repolarization = interfere with inactivation of Na channels --> rapid firing of neurons

convulsions, tremors

Front 49

List the Heavy Metals?

Back 49

Mercury, Lead, Arsenic, Cadmium, Iron

Front 50

Lead: Tx?

Back 50

[heavy metal]

severe: EDTA (iv), Dimercaprol (im)

mild: Dimercaptosuccinate (Succimer) (oral), Penicillamine (oral)

Front 51

Lead: mech of toxicity?

Back 51

[heavy metal]

inhibits heme synth:
binds σ-ALA synthase/dehydratase/ferrochelatase --> accum of d-aminolevulonic acid and protoporphyrin IX (plasma/urine)

Front 52

Lead: Sx of toxicity

Back 52

[heavy metal]

Pica, anemia, encephalopathy, periph neuropathy (wristdrop)

(from lecture) Acute/sub-acute: abd pain, HA, encephalopthy, anemia (no lead lines in gums)

Front 53

Lead: absorption route?

Back 53

[heavy metal]

inhalation, oral (kids)

Front 54

Cadmium: absorption route?

Back 54

[heavy metal]

inhalation, oral

Front 55

Cadmium: mech of toxicity?

Back 55

[heavy metal]

lung: inhibits a1AT --> emphysema

oral: proximal tubular injury (kidney) --> proteinuria, B2-macroglobulin

Front 56

Cadmium: Tx?

Back 56

[heavy metal]

EDTA (iv)

Front 57

Why is dimercaprol CI in cadmium toxicity?

Back 57

[chelator]

oral cadmium toxicity causes proximal tubular injury (kidney)

Dimercaprol-Cadmium complex is extremely nephrotoxic!

don't use any thiol-containing drugs (^nephrotoxic)

Front 58

Mercury: route of absorption?

Back 58

[heavy metal]

oral (Hg salts can be converted to organic salt by gut flora = 90% abs), inhalation

Front 59

Mercury: mech of toxicity?

Back 59

[heavy metal]

Hg salts cause precipitation of proteins and destroys mucosal membranes --> hemorrhagic gastroenteritis

proximal tubular necrosis

inhibits sulfhydryl-containing enzymes

Front 60

What is Minamata dz?

Back 60

[heavy metal] (Mercury)

1950s birth defect epidemic in Japanese village due to methylmercury-contaminated seafood from factory)

Front 61

Mercury: Tx?

Back 61

[heavy metal]

N-acetyl Penacillamine (oral) - most effective

also Dimercaprol (im), Dimercaptosuccinate (Succimer) (oral)

Front 62

Arsenic: route of absorption?

Back 62

[heavy metal]

oral (very good), inhalation

Front 63

Arsenic: mech of toxicity?

Back 63

[heavy metal]

1. protein damage of caps increases vasc permeability --> vasodilation, vascular collapse, shock

2. inhibits anaerobic and oxidative phosphorylation

3. inhibits sulfhydryl-containing enzymes

4. Ar gas: intravascular hemolysis, oliguric renal failure

Front 64

Arsenic: Tx of toxicity?

Back 64

[heavy metal]

chelation (Penicillamine) not very beneficial

-- supportive therapy --
for acute toxicity: fluid/electrolyte replacement, BP support (dopamine)
for chronic toxicity: transfusion

Front 65

Iron: route of absorption?

Back 65

[heavy metal]

skin, oral (duod/jej), inhalation

Front 66

Iron: storage?

Back 66

[heavy metal]

in hepatocytes and reticuloendothelial cells (also muscle)

Front 67

Iron: mech of toxicity?

Back 67

[heavy metal]

oxidative damage: lipid peroxidation, damages liver (major storage site), heart, pancreas, ant. pituitary

Front 68

Iron: Sx of toxicity?

Back 68

[heavy metal]

GI bleed, gray cyanosis, jaundice

Front 69

Iron: Tx?

Back 69

[heavy metal]

Chelator: Deferoxamine (im/iv)

Front 70

Why is EDTA given IV?

Back 70

[chelator for Lead, Cadmium]

cannot cross cell membranes

Front 71

Why is EDTA given as a calcium disodium salt?

Back 71

[chelator for Lead, Cadmium]

to balance the calcium level

Front 72

Copper (Wilson's dz): Tx?

Back 72

Pencillamine, N-acetyl-penicillamine (oral)

if allergic, use Trientine

Front 73

Half-lives:

As?
Hg?
Cd?
Pb?

Back 73

[heavy metals]

As: 10hrs
Hg: 70days
Cd: 20yrs
Pb: 2mo in blood, 40yrs in bone

Front 74

EDTA: site of action?

Back 74

[chelators]

only chelates circulating metals bc can't cross membranes (highly polar)

Front 75

EDTA: uses?

Back 75

[chelators]

severe Pb poisoning, also cadmium

Front 76

EDTA: toxicity?

Back 76

[chelators] (for Pb, Cd)

renal tubular necrosis (metal-EDTA complex)
thrombophlebitis w/ rapid infusion

Front 77

Dimercaprol: uses?

Back 77

[chelators]

As, Hg, Pb (severe) poisoning

Front 78

Dimercaprol: route of administration?

Back 78

[chelators]

IM in peanut oil

Front 79

Dimercaprol: mech of toxicity?

Back 79

[chelators]

highly lipophilic = crosses membranes easily (high rate toxicity, 50%)

convulsions, HTN (from tachycardia and peripheral vasoconstriction), renal toxicity (reduce by alkalinizing urine)

Front 80

Deferoxamine: uses?

Back 80

[chelators]

iron poisoning

Front 81

Deferoxamine: toxicity?

Back 81

[chelators]

skin rash, histamine rls & shock, cataracts

Front 82

Penicillamine: uses?

Back 82

[chelators]

Pb, As, Hg, Cu (Wilson's) poisoning

Front 83

What do you use when you're allergic to Penicillamine?

Back 83

[chelators for Cu]

Trientine (triethylenetetramine) - teratogenic

Front 84

Penicillamine: toxicity?

Back 84

[chelator]

Vitamin B6 (pyridoxine) def, leucopenia, anaphylaxis

Front 85

Dimercaptosuccinate (Succimer): uses?

Back 85

[chelator]

As, Hg, Pb (mild) poisoning

Front 86

Dimercaptosuccinate (Succimer): toxicity?

Back 86

[chelator]

GI problems

Front 87

Dimercaptosuccinate (Succimer): route of admin?

Back 87

[chelator]

oral

Front 88

What can aflatoxin lead to?

Back 88

[carcinogen]

liver CA

Front 89

What can carcinogenic viruses lead to?

Back 89

[carcinogen]

lymphosarcoma

Front 90

What can carcinogenic dyes lead to?

Back 90

[carcinogen]

bladder CA

Front 91

What is the 2 stage theory of carcinogenesis?

Back 91

1. Initiation: alter DNA like p53 (single exposure sufficient) - eg. polycyclic hydrocarbones, benzopyrines, halogenated hydrocarbons, aflatoxin B1

2. Promotion: stim cell prolif (multiple exposures necessary) - eg. sex hormones, EGF, tetradecanoyl phorbol acetate (TPA), PKC

Front 92

List the polycyclic aromatic hydrocarbons?

Back 92

[carcinogens]

Benzo(a)pyrene

Front 93

How are polycyclic hydrocarbons activated to interact with DNA?

Back 93

[carcinogens] (Benzo(a)pyrene)


1. P450 mediated oxidation
2. epoxide formation
3. N-oxidation
4. converts non-polar hydrocarbons to polar compounds by adding oxygen so that it can interact with DNA

(same with aflatoxin B1)

Front 94

List the pathways that eliminate mutagenic cmpds? (4)

Back 94

1. glutathione conjugation: X + GSH --> X-GSH (mercapturic acid, not reactive)

2. epoxide hydrolase: converts epoxides to trans-dihydrodiols (excreted)

3. glucoronidation: makes things more water-soluble (urinate)

4. sulfation: uses PAPs to transfer sulfonate to drugs

Front 95

What type of mutation can mutagenic alkylations lead to on DNA?

Back 95

point mutations

Front 96

What type of mutation can mutagenic adducts lead to on DNA?

Back 96

frame shift mutations

eg. Benzo(a)pyrene, Aflatoxin B1

Front 97

Xeroderma pigmentosum: defect?

Back 97

defective nucleotide excision repair --> DNA damage by UV (AR)

Front 98

Cigarette smoke contains which carcinogens?

Back 98

[carcinogens]

Benzo(a)pyrene (Polycyclic aromatic hydrocabon)

Dimethylnitrosamine (Nitrosamines) - food perservatives

2-acetylaminofluorine (Aromatic amines) - dyes

Front 99

Benzo(a)pyrene: mech of toxicity?

Back 99

[carcinogens] (Polycyclic aromatic hydrocarbons)

activated by P450 epoxidation, forms adduct with guanosine --> frame shift mut

Front 100

Dimethylnitrosamine: mech of toxicity?

Back 100

[carcinogens] (Nitrosamines)

activated by acidic stomach

Front 101

2-acetylaminofluorine: can cause?

Back 101

[carcinogens] (Aromatic amines)

bladder CA in smokers

Front 102

Aflaxtoxin B1: mech of toxicity? can cause?

Back 102

[carcinogens]

activated by liver epoxidation (P450) from Aspergillus in peanuts --> forms adduct with guanosine --> frame-shift mut

HCC

Front 103

Vinyl chloride: can be found where? and what can it cause?

Back 103

[carcinogens] (Halogenated cmpds)

plastics industry (PVC pipes)

angiosarcoma of liver

Front 104

Vinyl chloride: mech of toxicity?

Back 104

[carcinogens] (Halogenated cmpds)

activated by GSH conjugation (not eliminated) and P450

Front 105

Which carcinogens form adduct with guanosine and cause frame-shift muts?

Back 105

[carinogens]

Benzo(a)pyrene (Polycyclic aromatic hydrocarbons)

Aflatoxin B1 (mycotoxin)

(these also require activation via P450-mediated epoxidation to bind DNA)

Front 106

Compare short-, intermediate-, long-acting glugocorticoids?

Back 106

short-acting: anti-inflamm effect = Na-retaining effect, 8-12hr (Hydrocortisone)

intermediate-acting: mostly anti-inflamm effect, 12-24hr (Prednisone/Prednisolone/Trimcinolone)

long-acting: only anti-inflamm effect, 24-36hr (Dexamethasone/Betamethasone)

Front 107

Important SE/CI of glucocorticoids?

Back 107

HTN!

don't give hydrocrotisone to someone with HTN

Front 108

Tx for Addison's dz?

Back 108

[glucocorticoids]

Hydrocortisone

Addison's dz = primary adrenocortical insufficiency

Front 109

Dx of Cushing's syndrome?

Back 109

[glucocorticoids]

Dexamethasone suppression test

Front 110

Tx for acute asthma attack?

Back 110

[glucocorticoids]

oral Prednisolone

Front 111

Tx for chronic asthma attack?

Back 111

[glucocorticoids]

inhalation therapy with glucocorticoids

Front 112

List the glucocorticoids? (6)

Back 112

Hydrocortisone
Prednisone
Prednisolone
Triamcinolone
Dexamethasone
Betamethasone

Front 113

Glucocorticoids: SE?

Back 113

HTN

topical: impaired wound healing, cataracts, skin atrophy

Front 114

Glucocorticoids: MOA?

Back 114

anti-inflamm and immunosuppressive:

decrease peripheral WBCs
inhibits AA synth
blocks cytokine/receptor synth (IL, TNF, GM-CSF)

also ^gluconeogenesis/m catabolism --> high blood glucose to resist stress

Front 115

Glucocorticoids: toxicity?

Back 115

^gastric acid/pepsin, mental changes, bone loss

Front 116

List the Mineralcorticoids? (2) and their effects

Back 116

Fludrocortisone: Na-retaining effect >> anti-inflamm effect

Desoxycorticosterone: less Na-retaining. NO anti-inflamm effect

Front 117

Mineralcorticoids: MOA?

Back 117

help control body's water volume and [Na] & [K]

Front 118

Combo OCP: E effect? P effect?

Back 118

E: suppress ovulation

P: inhibit implantation

Front 119

P-only OCP: more effective or less effective than combo OCP?

Back 119

less effective

Front 120

What is the difference b/w Monophasic vs. Multiphasic combo OCPs?

Back 120

Monophasic: same amt of E & P delivered in each pill

Multiphasic: diff amt of E & P in each pill (more closely approximates NL PHYSIOLOGIC CYCLE)

Front 121

List the Estrogens? (4)

Back 121

1. Ethinyl estradiol
2. Premarin (conjugated E)
3. Mestranol
4. Diethylstilbestrol (DES)

Front 122

What are 2 E's used in combo OCPs?

Back 122

[estrogens]

1. Ethinyl estradiol (more common)
2. Mestranol

Front 123

When would you need to increase dose of E's?

Back 123

[estrogens]

when taking other Rx that ^P450 activity (eg. barbituates, carbamazepine, corticosteroids, griseofulvin, rifampin, etc.)

Front 124

List the classes of Progestins and differences?

Back 124

Class I: mimic physiologic P (Medroxyprogesterone)

Class II: mimic T, usu used as the progestin part in combo OCP (SE: andorgenic!) (Norethindrone/Norgestrel)

Front 125

Impt factors before considering OCP therapy?

Back 125

BMI, androgenic SE's, CI (smoking, E-responsive dysplasia)

Front 126

CI to OCP thearpy?

Back 126

h/o thromboembolic dz, vascular dz, MI, CV problems esp in smokers >35yo
h/o liver CA/dz (metabo)
CA: br, repro tract
abnl vaginal bleeding, preg

Front 127

HRT utility in menopause?

Back 127

Useful against: osteoporosis, vasomotor Sx, CVD, vaginitis

eg. 17-B-estradiol

Front 128

Difference b/w ERT vs. HRT?

Back 128

ERT: only E replacement
HRT: includes progestins

Front 129

List the SERMs?

Back 129

[selective estrogen receptor modulators] "antiestrogens"

Clomiphene (also pro-fertility)
Tamoxifen
Raloxifene

Front 130

How do SERMs act as E agonist AND E antagonist?

Back 130

[selective estrogen receptor modulator] "antiestrogens"

depends on tissue

Tamoxifen:
antagonist: Br (blocks ER+ tumors)
agonist: bone (anti-osteoporosis), uterus (endometrial hyperplasia)

Front 131

Raloxifene: effects?

Back 131

[selective estrogen receptor modulator] "antiestrogens"

same effects as Tamoxifen (blocks ER+ Br tumors, anti-osteoporosis, endometrial hyperplasia) but W/O endometrial effects

so no risk of endometrial CA with Raloxifene

Front 132

What are 2 pharmacological approaches to Tx of infertility?

Back 132

1. stimulate weak endocrine cycle (Clomiphene blocks negative feedback of E on hypoth and ant. pit --> GnRH --> FSH/LH)

2. start new cycle (HCG triggers ovulation)

Front 133

Ethinyl estradiol: advantages?

Back 133

[estrogens]

synthetic E, less first-pass effect (more effective @ lower dose)

Front 134

Mestranol: MOA?

Back 134

[estrogens]

synthetic E, metabo'd to ethinyl estradiol in body

Front 135

Diesthylstilbestrol: signif?

Back 135

[estrogens] "DES"

non-steroidal w/ E activity, used to prevent miscarriage long ago --> ectopic preg, infertility, vaginal adenoCA

Front 136

Mifepristone: uses?

Back 136

[antiprogesterones] "RU 486"

85% abortion rate, interferes with P, decline in B-hCG

Front 137

Type I vs. Type II DM? Basic Tx?

Back 137

Type I: childhood, autoAbs against pancreatic B cells, no insulin; Tx: insulin

Type II: adult onset, insulin resistance, decreased insulin secretion; Tx: diet/lifestyle (early), insulin (late)

Front 138

List the Rapid-acting insulins?

Back 138

[insulins]

Insulin aspart
Insulin lispro
Insulin glulisine

can be injected right before meals

Front 139

List the Short-acting insulins?

Back 139

[insulins]

Regular insulin

bound to zinc for stability

Front 140

List the Intermediate-acting insulins?

Back 140

[insulins]

Isophane insulin suspension (NPH) - complexed with protamine --> delays absorption of insulin by binding it

usu mixed with faster-acting insulins

Front 141

List the Long-acting insulins?

Back 141

[insulins]

Insulin detemir
Insulin glargine

provides steady-state, background insulin (last 12-24hrs)

acid formulation = can't be mixed with other insuls

Front 142

List the Mixtures of insulins? Advantages?

Back 142

[insulins]

NPL, Lispro
NPA, Aspart

combo of rapid- and intermediate-acting insulins provides tighter glycemic control

Front 143

Glucagon: uses?

Back 143

from A cells of pancreas

Tx: severe hypOglycemia in DM type 1 (insulin secretogogue)

--> ^blood glucose, ^insulin

Front 144

Are Oral antidiabetic drugs used in Type I or Type II DM?

Back 144

Type II, no use in Type I (only insulin)

(eg. hypoglycemic drugs, antihyperglycemic drugs)

Front 145

Insulin: MOA?

Back 145

binds to insulin-type receptors --> tyr kinase activity --> GLUT4 synth/recruitment --> glucose moves from blood to parenchyma via GLUT4

(GLUT2 in liver is insulin-independent, GLUT4 in skel m, adipose)

Front 146

List the Hypoglycemic drugs?

Back 146

1. Sulfonylureas (Tolazamide, Glipizide, Glyburide)
2. Meglitinides (Nateglinide, Repaglinide)
3. Incretins (Exantide)

Front 147

List the Antihyperglycemic drugs?

Back 147

1. Biguanides (Metformin)
2. Thiazolidinediones (Pioglitozone, Rosiglitazone)
3. a-glucosidase inhibitors (Acarbose)

Front 148

Sulfonylureas: MOA?

Back 148

[oral hypoglycemics] (Tolazamide, Glyburide, Glipizide)

inhibit pancreatic K+ channel to stimulate insulin secretion

Front 149

Meglitinides: MOA?

Back 149

[oral hypoglycemics] (Repaglinide, Nateglinide)

inhibit pancreatic K+ channel to stimulate insulin
secretion

can be used in pts with sulfur allergy

Front 150

Biguanides: MOA?

Back 150

[antihyperglycemics] (Metformin)

^glycolysis
^gluc removal from blood
\/gluconeogenesis
\/gluc absorption from GI
\/glucagon

Front 151

Biguanides: toxicity? CI?

Back 151

[antihyperglycemics] (Metformin)

GI, lactic acidosis

CI in alcoholics (renal/liver dz)

Front 152

Thiazolidinediones: MOA?

Back 152

[antihyperglycemics] (Pioglitazine, Rosiglitazone)

@ adipose tissue: binds PPAR-y --> stims trxn of genes involved in lipid metabo and insulin signaling

^GLUT4 transporters

Front 153

Thiazolidinediones: toxicity? CI?

Back 153

[antihyperglycemics] Pioglitazine, Rosiglitazone)

edema, metabo by P450 (^bioavailability of other P450 drugs, eg. OCPs)

CI: HF pts

Front 154

Exantide: MOA?

Back 154

[oral hypoglycemics] incretin analogue

glucagon-like peptide secreted in intestine in response to food

^blood glucose BUT also STIMS INSULIN SECRETION! (Tx: DM type II)

Front 155

a-glucosidase inhibitors: MOA?

Back 155

[antihyperglycemic] (Acarbose)

competitively inhibits GI enzymes that breakdown sugars for uptake - blocks uptake of starch

good for post-prandial but no effect on fasting glucose

Front 156

a-glucosidase inhibitors: toxicity?

Back 156

[antihyperglycemic] (Acarbose)

flatulence, diarrhea

Front 157

List the Thyroid agents?

Back 157

1. Thyroxine; T4 (less potent, more abundant than T3)
2. Levothyroxine: synthetic T4
3. Liothyronine: T3 (more potent, less abundant than T4)
4. Liotrix: synthetic T3/T4 mix

Front 158

List the Antithyroid agents? MOA?

Back 158

Propylthiouracil, Methimazole

both inhibit thyroperoxidase (which adds I- to thyroglobulin)

Propylthiouracil also inhibits deiodination of T4 peripherally (T4 no longer converted to T3)

Front 159

List the products of cyclooxygenase side of AA metabo?

Back 159

1. AA metabo'd to PGG2 by COX
2. then to PGH2
3. then to PGE2, PGF2a, PGD2, PGI2, or TXA2

Front 160

List the products of lipoxygenase side of AA metabo?

Back 160

Leukotrienes

Front 161

Misoprostol: MOA? uses?

Back 161

[AA metabolites]

PGE1 analog

suppresses gastric acid secretion (Pphlx: gastric ulcer in long-term aspirin therapy)

Front 162

Misoprostol: CI?

Back 162

[AA metabolites] "PGE1 analog"

preg (it is an abortifacient!)

Front 163

Dinoprostone: MOA? uses?

Back 163

[AA metabolites]

PGE2 analog via vaginal suppository

dilate cervix for labor or as abortifacient

Front 164

Latanoprost: MOA? uses?

Back 164

[AA metabolites]

PGF2a analog

Tx: ophthalmic HTN (glaucoma) or as abortifacient

Front 165

Thromboxane: MOA?

Back 165

[AA metabolites] (TXA2)

produced in plts: plt activator and vasoconstrictor (opposite of PGI2)

involved in thromboembolic dz

Front 166

Prostacyclin: MOA?

Back 166

[AA metabolites] (PGI2)

produced in endothelial cells: plt inhibitor and vasodilator (opposite of TXA2)

Front 167

LTB4: MOA?

Back 167

[AA metabolites] lipoxygenase pathway

leukocyte chemotaxis (inflamm)

Front 168

LTC4/LTD4: MOA?

Back 168

[AA metabolites] lipoxygenase pathway

bronchoconstriction

Front 169

List the NSAIDs?

Back 169

Aspirin
Diflunisal
Ibuprofen
Naproxen
Acetaminophen
Diclofenac/Ketorolac
Celecoxib (COX2i)
Rofecoxib (COX2i)
Zileuton (LOXi)

Front 170

Difference b/w COX-1 vs. COX-2?

Back 170

COX-1: housekeeping enzyme in most tissue (non-inflamm)

COX-2: inducible, in inflamm cells

selective COX-2 inhibitors (eg. Celecoxib, Rofecoxib) have less GI SE's (eg. ulcers)

Front 171

Aspirin: MOA?

Back 171

[NSAIDs] (non-selective COXi)

hydrolyzed to acetic acid and salicylate

IRREVERSIBLY binds plt COX (via acetylation)

Front 172

Aspirin: MOA?

Back 172

[NSAIDs] (non-selective COXi)

antipyresis, antiinflamm, analgesia
thromboembolic prophylaxis
RA (high doses)

may decrease risk of colon CA and Alzheimer's

Front 173

Aspirin: SE?

Back 173

1. tinnitus, vertigo, GI (thwart mucosal barrier that relies on PGs)

2. Reye's syndrome: kids w/ viral infxn Tx'd w/ ASA = rapid liver failure and encephalitis

3. due to inhibition of COX-1: disrupt hemostasis, respiratory acidosis, coma

Front 174

Salicylates and its effect on inflamm vs. analgesia?

Back 174

only ACETYLATED salicylates (like ASA) have both analgesia and antiinflamm effects

non-aceylated salicylates (Na salicylate) have antiinflamm effect but no analgesia effect bc the binding/inhib of COX is REVERSIBLE

Front 175

Acetaminophen: MOA? uses?

Back 175

[NSAIDs] (COX3i)

p-aminophenol derivative, inhibits COX3 in brain

no antiinflamm effect
used for mild fever (antipyretic) and pain (analgesic)

use instead of ASA in children (no risk for Reye's)

Front 176

Acetaminophen: toxicity?

Back 176

[NSAIDs] (COX3i)

liver/kidney dz

Antidote: N-acetylcysteine! (Tx: toxic liver metabolite)

Front 177

Ibuprofen: MOA? uses?

Back 177

[NSAIDs] (non-selective COXi)

propionate derivative

used widely: sports injuries, post-op pain, arthritis

Front 178

Ibuprofen: MOA? uses?

Back 178

[NSAIDs] (non-selective COXi)

less SE vs. ASA
chronic use: dyspepsia, HTN, gastric ulcer

Front 179

Naproxen: MOA? uses?

Back 179

[NSAIDs] (non-selective COXi)

propionate derivative (same as ibuprofen, same uses)

Front 180

Naproxen: toxicity?

Back 180

[NSAIDs] (non-selective COXi)

more irritating to GI than ibuprofen, MI

Front 181

Celecoxib: MOA? uses?

Back 181

[NSAIDs] (selective COX-2i)

antiinflamm, analgesic

minimal GI SE's and reduced effect on plt aggregation

Tx; osteoarthritis, RA, menustrual cramps, post-dental surg, orthopedic surg

Front 182

Celecoxib: toxicity?

Back 182

[NSAIDs] (selective COX-2i)

less GI SE's than non-selective COXi's

contains sulfonamide moiety (allergic Rx)
possible CV (stroke, MI) risk with COX2i (eg. Rofecoxib (Vioxx))

Front 183

Rofecoxib: toxicity?

Back 183

[NSAIDs] (selective COX-2i)

pulled from market (2004) for ^risk stroke, MI

Front 184

Zileuton: MOA?

Back 184

Lipoxygenase inhibitor: no leukotriene synth

Front 185

Diclofenac/Ketorlac: MOA?

Back 185

[NSAIDs] (non-selective COXi)


acetic acid derivatives
COX-1 affinity > COX-2

Front 186

List the Antiarthritis agents?

Back 186

1. NSAIDs
2. DMARDs (dz modifying antirheumatic drugs; eg. Methotrexate, Hydroxychloroquine, Sulfasalazine, Gold)

Front 187

What is a DMARD?

Back 187

Disease Modifying AntiRheumatic Drugs

actually retarde the progression of dz (unlike NSAIDs that only deal with Sx)

eg. Methotrexate, Hydroxychloroquine, Sulfasalazine, Gold

Front 188

Methotrexate: MOA? uses?

Back 188

[DMARD] / [IBD]

folic acid analog with cytotoxic and immunosuppressive activity

1ST LINE Tx in RA due to rapid onset, few SE

Front 189

Methotrexate: toxicity?

Back 189

[DMARD] [IBD]

hematotoxic
teratogenic

Front 190

Hydroxychloroquine: uses?

Back 190

[DMARD]

4-aminoquinolone

retards RA but not bone erosion

also used in Tx: malaria

Front 191

Hydroxychloroquine: toxicity?

Back 191

[DMARD]

ocular toxicity

Front 192

Sulfasalazine: MOA? uses?

Back 192

[DMARD] [IBD]

combo sulfonamide and salicylate separated by gut flora --> salicylate removes toxic oxygen metabolites produced by neutrophils

retards RA

Front 193

Sulfasalazine: toxicity?

Back 193

[DMARD] [IBD]

GI distress

Front 194

Azathioprine: MOA? uses?

Back 194

[immunsuppressants, cytotoxic agents] [IBD]

inhibits purine synth
inhibits cellular/humoral imm responses,
inhibits clonal expansion

given after organ transplant

Front 195

Cyclosporine: MOA? uses?

Back 195

[immunsuppressants] [IBD]

inhibits IL-2 synth --> blocks T-cell recruitment (cellular imm)

Front 196

List the Antigout agents?

Back 196

Colchicine (acute attack)
Probenecid (prohylaxis)
Allopurinol (prohylaxis)

Front 197

Colchicine: MOA? uses?

Back 197

[antigout]

binds tubulin in cells --> disrupts polymerization = cell motility = decrease leukocyte migration into joints

for acute attack/inflamm of gout

Front 198

Probenecid: MOA? uses?

Back 198

[antigout] uricosuric

^organic acid secretion (eg. uric acid) by competing for uptake receptors in proximal tubules

for prophylaxis of gout

Front 199

Allopurinol: MOA? uses?

Back 199

[antigout]

inhibits xanthine oxidase --> decrease uric acid synth

drug of choice for long-term therapy of gout

Front 200

Describe the synth of histamine and its cellular sources?

Back 200

synth from histidine by histidine decarboxylase

stored in mast cells, basophils, neurons, epidermis, gastric mucosa

Front 201

What are the releasers of histamine?

Back 201

1. IgE Abs on mast cells (type I hypersensitivity)
2. peptides that contain basic aa (Arg, Lys)
3. complement derivatives (anaphylatoxins: C3a, C4a, C5a)
4. substance P
5. bee/wasp venom (melittin, polistes kinin)

Front 202

What are the inhibitors of histamine rls?

Back 202

anything that ^cAMP

B-receptor activation and cAMP accumulation (eg. isoproterenol, Epi, theophylline)

Front 203

Effects of activation of H1 receptors?

Back 203

(Gq) SM effects: bronchoconstriction, vasodilation, edema (IgE-med allergy, mast cells)

Front 204

Effects of activation of H2 receptors?

Back 204

(Gs) parietal cell --> gastric acid secretion, (-) feedback on histamine via ^cAMP

Front 205

Effects of activation of H3 receptors?

Back 205

(Gi) presynaptic inhibitory heteroreceptor (inhibits rls of other NTs: DA, GABA, ACh, NE, and 5-HT)

Gi = decrease cAMP

Front 206

How is histamine degraded?

Back 206

via monoamine oxidase (MAO) and diamine oxidase

Front 207

What are the specific actions of histamine?

Back 207

1. IgE-med Type I hypersensitivity (rhinitis, urticaria, edema)
2. acid secretion in stomach
3. NT

Front 208

List the H1 receptor antagonists?

Back 208

Chlorpheneramine
Diphenhydramine (Benedryl) (also anti-emetic)
Fexofenadine
Loratadine/Terfenadine

Front 209

Indications of H1 receptor antags?

Back 209

IgE/immediate Type 1 hypersensitivities: allergy, pollinosis, urticaria, hay fever,

not indicated for asthma, cold

Front 210

H1 receptor antags: toxicity?

Back 210

(Chlorpheneramine, Diphenhydramine, Fexofenadine)

drowsiness (esp w/ EtOH), anticholinergic (dry mouth, blurred vision)

Front 211

Loratadine/Terfenadine: toxicity?

Back 211

[H1 receptor antags]

serious SE in hepatic dysfxn (bc metabo'd by P450) w/ concomitant admin of erythromycin or in OD -->

ventricular arrhythmias, QT prolongation

Front 212

List the H2 receptor antags?

Back 212

Cimetidine
Rantidine
Famotidine
Nizatidine

Front 213

Cimetidine: uses?

Back 213

[H2 receptor antag] "Tagamet"

inhibits secretion caused by histamine/gastrin/ACh

Tx: ulcers, Zollinger-Ellison syndrome

Front 214

Cimetidine: toxicity?

Back 214

[H2 receptor antags]

anti-androgen effects (gynecomastia, impotence, PRL secretion)

interferes with metabo of other P450 drugs (warfarin, lidocaine, phenobarbitol)

Front 215

Rantidine vs. Cimetidine: uses?

Back 215

[H2 receptor antags] "Zantac"

Rantidine:
binds P450 less (less SE)
longer-lasting (more effective in lower doses)
furan subunit (instead of imidazole ring)

Front 216

Famotidine: describe?

Back 216

[H2 receptor antags]

thiazole subunit (instead of imidazole ring of Cimetidine)
more effective than Ranitidine
no P450 interactions (45% absorbed, urinated unchanged) (Nizatidine has no P450 interactions too but 90% abs)


recall: Rantidine:
binds P450 less (less SE) vs. Cimetidine
longer-lasting (more effective in lower doses) vs. Cimetidine
furan subunit (instead of imidazole ring of Cimetidine)

Front 217

Nizatidine: describe?

Back 217

[H2 receptor antag]

no P450 interactions (90% absorbed, urinated unchanged)

Front 218

List the Pro-emetic drugs?

Back 218

Ipecac (Emetine)
Apomorphine

Front 219

Ipecac: MOA? uses?

Back 219

[pro-emetics]

direct effects on chemoreceptor trigger zone (medulla), which talks to vomiting center

for oral poisoning

Front 220

Apomorphine vs. Ipecac?

Back 220

[pro-emetics]

Apormorphine more potent and rapid-acting

Front 221

List the Anti-emetic drugs?

Back 221

1. Antihistamines (Diphenhydramine, Meclizine)
2. Anticholinergics (Scopolamine)
3. D2 antags (Metoclopramide, Promethazine)
4. 5HT3 antags (Ondansetron)
5. Cannabinoids (Marijuana, Dronabinol)

Front 222

Which anti-emetics are used for motion sickness and post-op nausea?

Back 222

1. Antihistamines (Diphenhydramine, Meclizine)
2. Anticholinergics (Scopolamine; dermal patch)

Front 223

Which anti-emetics are used for chemo/radio-induced nausea?

Back 223

1. D2 antags (Metoclopramide, Promethazine)
2. 5-HT3 antags (Ondansetron)
3. Cannabinoids (Marijuana, Dronabinol)

Front 224

List the Pro-kinetic (GI motility) drugs? uses?

Back 224

1. Cholinergics (Bethanachol, Neostigmine)
2. 5-HT4 agonists (Metoclopramide, Tegaserod)
3. others (Domperidone, Erythromycin)

post-op paralysis, diabetic gastroparesis, GERD (by ^LES P)

Front 225

Why aren't the Cholinergic pro-kinetic drugs used anymore?

Back 225

(Bethanachol, Neostigmine)

non-specificity

Front 226

Metoclopramide: toxicity?

Back 226

[5HT4 agonist pro-kinetic]

Parkinsonism, ^PRL

Front 227

Domperidone: MOA? uses?

Back 227

[antidopaminergic anti-emetic, pro-kinetic]

unlike Metoclopramide (5-HT4 agonist), can be used in Parkinson's bc does NOT cross BBB

Front 228

Erythromycin: uses in GI?

Back 228

[pro-kinetic]

direct effect on gastric SM

for diabetic gastroparesis

Front 229

List the Antidiarrheal agents?

Back 229

1. Intraluminal (Kaopectate, Metamucil, Bismuth salycilate (peptobismol))
2. Opiods (Loperamide, Diphenoxylate, Difenoxin)
3. Others (Octreotide, Cholestryamine)

Front 230

Intraluminal antidiarrheal agents: MOA?

Back 230

^stool viscosity and absorb water

Kaopectate (clay)
Metamucil (fiber)
Bismuth salycilate (peptobismol)

Front 231

Opiod antidiarrheal agents: MOA?

Back 231

inhibit enteric nerves presynpatically

Loperamide (imodium)
Diphenoxylate/Difenoxin (CNS effects, Rx only)

Front 232

Octreotide: uses?

Back 232

[antidiarrheal]

antisecretory effects, decreases colonic tone

for severe AIDS/chemo-induced diarrhea

Front 233

Cholestyramine: MOA? uses?

Back 233

[antidiarrheal] [bile acid sequestrant/antihyperlipidemic]

binds bile salts so no longer osmotically active

for ileal resection

Front 234

List the Laxatives?

Back 234

1. Bulk (Dietary fiber, Methylcellulose, Psyllium husk)
2. Osmotic (Mg salts, Phosphates, Glycerin, Lactulose, Polyethylene glycol soln)
3. Stimulant (Bisacodyl, Castor oil, Senna, Cascara)
4. Stool softeners (Mineral oil, Docusate)

Front 235

Bulk laxatives: MOA?

Back 235

(Dietary fiber, Methylcellulose, Psyllium husk)

retain water in stools and support bacterial growth --> ^bacterial fermentation produces short-chain fatty acids that stim colonic motility

Front 236

Osmotic laxatives: MOA? CI?

Back 236

(Mg salts, Phosphates, Glycerin, Lactulose, Polyethylene glycol soln)

pulls water into colon

CI: renal/cardiac dz (can produce electrolyte/fluid imbalances)

Front 237

Stimulant laxatives: MOA?

Back 237

(Bisacodyl, Castor oil, Senna, Cascara)

directly stim colonic motility, enhance secretion of fluid/electrolytes

Front 238

Stool softener: MOA?

Back 238

(Mineral oil, Docusate)

^water/fat into stool

Front 239

List the Antacids?

Back 239

Bicarbonate (alkaseltzer)
Ca carbonate (tums)
Mg hydroxide (laxative effect)
Al hydroxide (constipating effect)

Front 240

Antacids: MOA?

Back 240

[Bicarbonate (alkaseltzer)
Ca carbonate (tums)
Mg hydroxide (laxative effect)
Al hydroxide (constipating effect)]

weak organic bases that neutralize stomach acid

Front 241

H2 histamine antags that block parietal cell stimulation and lower stomach acid? uses?

Back 241

(-idine)

Cimetidine
Ranitidine
Famotidine
Nizatidine

GERD, PUD, non-ulcer dysplasia (1st line = PPIs)

Front 242

List the PPI's?

Back 242

(-prazole)

Omeprazole
Lansoprazole
Rabeprazole
Pantoprazole

Front 243

PPI: MOA?

Back 243

(-prazole)

Omeprazole
Lansoprazole
Rabeprazole
Pantoprazole

bind covalently and IRREVERSIBLY to proton pumps and deactivate them

(NEW pump must be synth'd to restore activity)

1ST LINE against GERD, PUD (more effective than H2 antags)

Front 244

What is the 1st line Tx for GERD and PUD?

Back 244

PPI (-prazole):
Omeprazole
Lansoprazole
Rabeprazole
Pantoprazole

(more effective than H2 antags)
(-idine)

Cimetidine
Ranitidine
Famotidine
Nizatidine

Front 245

List the Protective agents against peptic ulcers?

Back 245

Misoprostol (PGE analog)
Sucralafate (sulfated polysacch)

Front 246

Misoprostol: MOA? uses? SE?

Back 246

[protective agents]

PGE analog, inhibits acid secretion and promotes mucus and HCO3- secretion

for peptic ulcers/recurrence

not used a lot due to GI upset, diarrhea

Front 247

Sucralafate: MOA? uses?

Back 247

[protective agent]

sulfated polysacch --> polymerizes in acidic environ (stomach acid) --> forms protective layer and buffers acid

for peptic ulcers/recurrence

Front 248

List the IBD agents?

Back 248

1. Aminosalicylates (Sulfasalazine, Mesalamine)
2. Glucocorticoids (Prednisone, Hydrocortisone, Budesonide)
3. Cytostatic/Immunosuppressants (Cyclosporine, 6-mercaptopurine, Azathioprine, Methotrexate)
4. Anti-TNF (Infliximab)

Front 249

Aminosalicylates: MOA?

Back 249

[IBD agents] (Sulfasalazine [DMARD], Mesalamine)

non-absorbable NSAIDs: not active until cleaved by gut flora, releases salicylic acid (NSAID) --> inhibits synth of PGs/leukotrienes (inflamm mediators)

Front 250

Aminosalicylates: toxicity?

Back 250

[IBD agents] (Sulfasalazine [DMARD], Mesalamine)

arthralgias, BM suppression, severe hypersensitivity rxns

Front 251

List the Glucocorticoids used in IBD?

Back 251

Glucocorticoids:
Prednisone (intemediate-acting)
Hydrocortisone (short-acting)
Budesonide

Front 252

List the cytostatic/immunosuppressant agents used in IBD? MOA?

Back 252

1. Cyclosporine (inhibits IL-2 synth & T cell recruitment)

2. 6-mercaptopurine (interferes w/ nucleotide/RNA/DNA synth)

3. Azathioprine (interferes w/ purine/DNA synth)

4. Methotrexate (FA analog)

Front 253

Infliximab: MOA?

Back 253

[IBD agents, immunosuppressant]

anti-TNFa mAb

Front 254

List the Antihyperlipidemic drugs?

Back 254

1. Statins (Atorvastatin, Simvastatin, Lovastatin, Pravastatin)
2. Fibric Acid derivatives (Gemfibrozil, Fenofibrate, Clofibrate)
3. Bile Acid sequestrants (Cholestyramine, Colestipol)
4. others (Niacin, Ezetimibe)

Front 255

Antihyperlipidemic drugs: effects on lipids?

Back 255

Statins: lower LDL, ^HDL
Fibric Acid derivatives: lower VLDL, TG, ^HDL
Niacin: lower LDL, VLDL, TG, ^HDL
Bile Acid sequestrants: lower LDL, chol
Ezetimibe: lower LDL, chol

Front 256

Statins: MOA?

Back 256

[antihyperlipidemic/antiatherosclerotic agents] (Atorvastatin, Simvastatin, Lovastatin, Pravastatin)

competitively inhibit HMG-CoA reductase (key enzyme for de novo chol synth)

--> lower LDL
--> ^HDL (HDL/LDL)

Front 257

Statins: pros/cons?

Back 257

[antihyperlipidemic/antiatherosclerotic agents] (Atorvastatin, Simvastatin, Lovastatin, Pravastatin)

pros: specific, effective, well-tolerated

cons: long term safety unknown, $$$, CI: preg/nursing (teratogenic)

Front 258

Fibric Acids: MOA?

Back 258

[antihyperlipidemic/antiatherosclerotic agents] (Gemfibrozil, Fenofibrate, Clofibrate)

bind with PPARs (peroxisome proliferator activated receptors) --> stim lipoprotein lipase (from adipose tissue) --> ^clearance of lipids, ^synth HDL

--> lower VLDL, TG
--> ^HDL (HDL/LDL)

Front 259

Fibric Acids: pros/cons?

Back 259

[antihyperlipidemic/antiatherosclerotic agents] (Gemfibrozil, Fenofibrate, Clofibrate)

pros: safe, effective, well-tolerated, cheaper than statins, potential antithrombotic effects

cons: more effective at reducing TG than chol (no effect on LDL), Clofibrate not used due to toxicity

SE: chol gallstones!

Front 260

Niacin (Nicotinic Acid): MOA?

Back 260

[antihyperlipidemic/antiatherosclerotic agents]

inhibit hormone-sensitive lipases --> decrease FFA available to liver for synth of TG

--> lower LDL, TG, VLDL
--> ^HDL (HDL/LDL)

Front 261

Niacin (Nicotinic Acid): pros/cons?

Back 261

[antihyperlipidemic/antiatherosclerotic agents]

pros: long clinical experience, least expensive

cons: flushing, itchiness, GI discomfort, reactivate gout via liver rxns!

CI: diabetics, preg

Front 262

Bile Acid sequestrants: MOA?

Back 262

[antihyperlipidemic/antiatherosclerotic agents] (Cholestyramine, Colestipol)

oral (GI action, no bloodstream)

anion exchange resins bind neg-charged bile acids in SI --> excreted (will increase chol synth/TO)

--> lower LDL, chol

use in combo with Statins to reduce increased chol synth/TO

Front 263

Bile Acid sequestrants: pros/cons?

Back 263

[antihyperlipidemic/antiatherosclerotic agents] (Cholestyramine, Colestipol)

pros: safe, effective
cons: GI effects (interferes with GI drug abs), exacerbates hypertriglyceridemia

CI: warfarin

Front 264

Ezetimibe: MOA?

Back 264

[antihyperlipidemic/antiatherosclerotic agents]

prodrug --> active glucuronide form

inhibits dietary chol uptake by jej epith by binding to protein Niemann-Pick-C1-Like1 (NPC1L1) --> excreted (will increase chol synth/TO)

--> lower LDL, chol

use in combo with Statins to reduce increased chol synth/TO

Front 265

Ezetimibe: pros/cons?

Back 265

[antihyperlipidemic/antiatherosclerotic agents]

pros: safe, effective, can use as monotherapy in Statin-intolerant pts

cons: no effect on TG absorption, can also cause hepatotoxicty in combo w/ Statins

Front 266

Etanercept: MOA? uses?

Back 266

[immunosuppressant]

TNF inhibitor by acting like a TNF receptor

for autoimmune dz

Front 267

Adalimumab: MOA? uses?

Back 267

[immunosuppressant]

anti-TNFa mAb

for autoimmune dz

Front 268

Anakinra: MOA? uses?

Back 268

[immunosuppressant]

IL-1 receptor antag

for RA

Front 269

Which carcinogens require P450-mediated oxidation to be able to interact with DNA?

Back 269

Benzo(a)pyrene (polycyclic aromatic hydrocarbon)

Aflatoxin B1 (Mycotoxin)