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Pharmacology Histamine/GI > Drugs > Flashcards

Drugs Flashcards

1
Q

First gen antihistamines

A

Brompheniramine, cyproheptadine, diphenhydramine, promethazine, hydroxyzine, pyrilamine

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2
Q

Most sedating first gen antihistamines

A

diphenhydramine, promethazine (ethanolamines, phenothiazines)

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3
Q

First gen antihistamines with anti-cholinergic effects

A

diphenhydramine, promethazine

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4
Q

First gen antihistamines with local anesthetic effect

A

promethazine and pyrilamine

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5
Q

First gen antihistamines with anti-serotonin effect (headaches)

A

cyproheptadine and azatadine

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6
Q

First gen antihistamines with weak alpha-adrenergic antagonism

A

Phenothiazines (promethazine)

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7
Q

Second gen antihistamines

A

loratadine, desloratadine, fexofenadine, cetirizine, levocetirizine

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8
Q

Second gen antihistamine that has been withdrawn

A

Terfenidine

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9
Q

Second gen antihistamines with no anti-muscarinic activity

A

fexofenadine, cetirizine

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10
Q

Active metabolite of terfenadine

A

Fexofenadine

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11
Q

Active metabolite of hydroxyzine

A

Cetirizine

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12
Q

What other actions might cetirizine have?

A

Block LTC4 (contracts SM of bronchioles), migration of neutrophils, and infiltration of eosinophils

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13
Q

topical antihistamines (eye drops and nasal spray)

A

olopatadine, azelastine, KETOTIFEN

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14
Q

what is dimenhydrinate (Dramamine) and what is it used for?

A

diphenhydramine with chlorotheophylline salt, used for motion sickness

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15
Q

what are antihistamines used for motion sickness?

A

dimenhydrinate (Dramamine), meclizine (Antivert), promethazine (Phenergan)

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16
Q

why would you use an antihistamine (i.e. parenteral diphenhydramine) with epinephrine?

A

to treat anaphylaxis

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17
Q

What should you not mix first gen antihistamines with?

A

alcohol, anxiolytics, antipsychotics

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18
Q

Which drugs are contraindicated in urinary retention and narrow angle glaucoma, and why?

A

first gen antihistamines and (des)loratadine bc they have anti-muscarinic effects

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19
Q

What drug(s) causes extrapyramidal effects, and what are those effects?

A

promethazine (phenothiazine) - dystonia, akathisia, Parkinsonian rigidity

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20
Q

Mechanism of CNS depression by antihistamines

A

Histamine action on H1 receptors in the thalamic relay cell maintains their depolarization so they do not fire action potentials (wakefulness) but antihistamines remove this so the cells hyperpolarize and fire bursts of action potentials which lead to sleep

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21
Q

Antacids

A

NaHCO3, CaCO3, Al(OH)3, Mg(OH)3

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22
Q

Neutralizing capacity of NaHCO3 and adverse effects

A

High neutralizing capacity; fluid retention

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23
Q

Neutralizing capacity of CaCO3 (Tums) and adverse effects

A

Moderate neutralizing capacity; milk-alkali syndrome

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24
Q

Neutralizing capacity of Al(OH)3 (Alternagel) and adverse effects

A

High neutralizing capacity; constipation

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25
Q

Neutralizing capacity of Mg(OH)3 and adverse effects

A

High neutralizing capacity; diarrhea

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26
Q

What is the formula of Maalox/Mylanta?

A

Al(OH)3 and Mg(OH)3

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27
Q

What is Gaviscon (sodium alginate and antacids) and how does it work?

A

Viscous, weak base which prevents reflux and is effective in GERD (used for heartburn and indigestion)

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28
Q

What is Mylicon/Phazyme (Simethicone) and how does it work?

A

It is a mild surfactant which enhances release of gas (used to relieve pain from gas)

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29
Q

What does liver enzymes/drugs does cimetidine inhibit?

A

CYP2C6 and 2D9: warfarin, phenytoin, theophylline, benzodiazepines, sulfonylureas

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30
Q

What are side effects of cimetidine?

A

CNS effects when given IV to elderly pts (confusion, delirium, headaches), antiandrogen (gynecomastia, impotence), inhibition of estradiol metabolism (galactorrhea), thrombocytopenia

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31
Q

2nd gen H2 antagonists

A

Ranitidine (Zantac), Nizatidine, Famotidine (Pepcid)

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32
Q

Features/effects of 2nd gen H2 antagonists

A

increased bioavailability of ethanol (except famotidine), reduced interactions with the CYP450 system, greater potency, longer half life

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33
Q

Proton pump inhibitors

A

omeprazole, lansoprazole, raberprazole, pantoprazole

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34
Q

How does omeprazole become activated?

A

Omeprazole travels to the parietal cell where it is protonated and becomes sulfenic acid, then it becomes dehydrated to cyclic sulfenamide and then binds irreversibly (forming a disulfide complex) to the H/K-ATPase

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35
Q

How long is the plasma half-life of PPIs, and how long is their duration of action?

A

plasma half-life: 1 hour

duration of action: 24 hours

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36
Q

What drugs’ metabolism is affected by the increase in gastric pH after taking PPIs?

A

digoxin, ketoconazole (require acidity for GI absorption)

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37
Q

What liver enzymes/drugs does omeprazole inhibit?

A

CYP2C19: diazepam, warfarin, phenytoin are increased, clopidogrel activity reduced

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38
Q

What drug can cause a vitamin B12 deficiency and why?

A

omeprazole, because it decreases the oral bioavailability of vit B12

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39
Q

Is the risk of osteoporotic fracture increased with PPIs?

A

Yes - long term use increases the risk of fracture

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40
Q

What is acid rebound?

A

Decreased acidity of the stomach leads to less somatostatin release and inhibition of gastrin, leading to hypergastrinemia, and increased gastric acid secretion upon withdrawal of acid-suppressing meds (occurs more commonly with H2 antagonists)

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41
Q

Sucralfate

A

Aluminum hydroxide complex of sucrose, polymerizes in the acidic pH and forms a protective barrier on injured mucosal tissue (ulcers), poorly absorbed, may reduce the absorption of tetracycline, phenytoin, and digoxin

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42
Q

Misoprostol

A

semi-synthetic prostaglandic E1 derivative, acts on parietal cells to reduce acid secretion, acts on superficial epithelial cells to increase mucous production, used in combo with long-term NSAIDs, adverse effects include diarrhea and causing abortion

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43
Q

How do you treat an H. pylori infection?

A

combo of bismuth salt + PPI/H2 blocker + abx (metranidazole, tetracycline, amoxicillin, clarithromycin) + ranitidine bismuth citrate

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44
Q

bismuth subsalicylate (Pepto Bismol)

A

converted in GI tract to bismuth salts and salicylic acid, used to treat mild diarrhea and part of a combination therapy for H. pylori, has antibacterial, antiviral, and antisecretory activity

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45
Q

metoclopramide

A

dopamine (D2) receptor antagonist which leads to increased Ach release and GI contraction; action at D2 receptor in area postrema also gives this drug anti-emetic action; used post-op and in diabetics for gastrioparesis, to relieve GERD, to facilitate small-bowel intubation, anti-emetic; side effects are sedation, Parkinson-like and extrapyramidal Sx, hyperprolactinemia (galactorrhea, gynecomastia, breast tenderness)

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46
Q

erythromycin

A

motilin agonist, but tolerance develops rapidly

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47
Q

5HT4 agonists (prokinetic)

A

cisapride
tegaserod - withdrawn bc cardiovascular toxicity
prucalopride - not available in the US

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48
Q

linaclotide

A

prokinetic; increases activity of guanylate cyclase (increases cGMP which decreases activity of pain fibers in the submucosa and increases activity of the CFTR pump which pumps Cl and HCO3 into the lumen), used to treat IBS/constipation/idiopathic constipation; taken 30 min before first meal; main adverse effect is diarrhea; not absorbed systemically

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49
Q

bulk-forming laxatives

A

psyllium, methylcellulose, bran, milk of magnesia - non-absorbable and form hydrophilic mass in the presence of water

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50
Q

osmotic laxatives

A

lactulose, polyethylene glycol - increase water in the intestinal lumen by osmotic force, leading to distension and an increase in peristalsis

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51
Q

stool softeners

A

docusate sodium, mineral oil, glycerin (surfactants and lubricants) - incorporate into stool to make passage easier, lubricate lower bowel to prevent stool impaction, can reduce the absorption of fat-soluble vitamins

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52
Q

anticholinergic anti-diarrheals

A

bentyl, dicyclomine

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53
Q

opiate anti-diarrheals

A

diphenoxylate (formulated with atropine for anti-muscarinic effects and decreased risk of abuse) and loperamide slow gastric emptying, do not cross BBB well, risk of constipation, contraindicated in ulcerative colitis and bacterial diarrhea

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54
Q

kaolin

A

magnesium aluminum silicate combined with pectin which absorbs bacterial toxins and fluid, reducing stool liquidity

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55
Q

fiber

A

anti-diarrheal

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56
Q

alosetron

A

5HT3 receptor antagonist, used in women with IBS and diarrhea, can cause severe constipation requiring hospitalization/surgery and ischemic colitis, blocks visceral afferent pain sensation and decreases colon motility, restricted use

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57
Q

D2 antagonist anti-emetics (area postrema)

A

promethazine, prochlorperazine

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58
Q

anticholinergic/antihistamine anti-emetics (nucleus of solitary tract)

A

meclizine, scopolamine

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59
Q

5HT3 receptor antagonist anti-emetics (nucleus of solitary tract)

A

ondansetron, granisetron: prevent activation of chemoreceptor trigger zone and vagal afferents to vomiting center; combined with aprepitant and dexamethasone; used prophylactically for vomiting associated with anesthesia or for chemotherapy-induced nausea and vomiting

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60
Q

Cannabinoid anti-emetics

A

dronabinol, nabilone: used for nausea/vomiting associated with chemotherapy; synthetic THC (tetrahydrocannabinol); used in pts who are refractory to other anti-emetics; may cause psychoactive effects

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61
Q

human insulin cDNA in plasmid expressed in E. coli

A

Humilin (Lilly)

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62
Q

human insulin cDNA in plasmid expressed in transformed yeast

A

Novolin

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63
Q

ultra rapid onset/short action insulins names, onsets, peaks, duration, appearance

A

Lispro, Aspart, Glulisine; onset in 15 min; peak around 1-1.5 hours; duration 3-6 hours; appearance clear

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64
Q

rapid onset/short action insulin name, onset, peak, duration, appearance

A

Regular (R); onset in 30 min-1 hr; peak 2-4 hours; duration 8-12 hours; appearance clear

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65
Q

intermediate onset/action insulin name, onset, peak, duration, appearance, method of administration

A

NPH (neutral protamine hagedorn)(N); onset in 1-1.5 hrs; peak 4-12 hours; duration 24 hrs; appearance cloudy; injected subcutaneously

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66
Q

slow onset/long action insulins names, onsets, peaks, duration, appearance

A

Glargine, Detemir, Degludec; onset 1-2 hrs; peak 4-9 hrs; duration >24 hours; appearance clear

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67
Q

lispro

A

the P28 (proline) and K29 (lysine) positions are reversed, decreasing self-association (dimer and hexamer formation) of the insulin, and decreasing time to onset (injected immediately before meals)

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68
Q

aspart

A

P28 switched to aspartate, rapid onset, injected immediately before meals

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69
Q

glulisine

A

Asn3 and Lys29 are switched to Lys and Glu, rapid onset, injected immediately before meals

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70
Q

glargine

A

Asn21 of alpha-chain is changed to Gly, and 2 Arg are added to the end of the beta-chain, long acting, once daily injection; pH of 4 and precipitated when neutralized (post-injection)

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71
Q

detemir

A

Thr30 of the beta-chain is delected, Lys29 is myristylated, binds serum albumin, injected twice daily

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72
Q

degludec

A

Thr30 of beta-chain is replaced by gamma-Glu/c16 fatty acid, binds serum albumin, injected twice daily

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73
Q

what are some mixtures of short/long acting insulins?

A

NPH + R = humulin; NPL (neutral protamine lispro) + lispro = humalog

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74
Q

what insulins can be administered subcutaneously?

A

all preparations

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75
Q

what insulins can be administered via a insulin infusion pump?

A

buffered regular, all fast-acting (lispro, aspart, glulisine)

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76
Q

what insulins can be administered via an IV?

A

regular, for severe ketoacidosis or hyperglycemia

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77
Q

what insulins can be administered via inhalation?

A

Afrezza, or dry powder form of regular human insulin

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78
Q

What is afrezza used for and when is it contraindicated? What is a possible consequence?

A

used for preprandial insulin; contraindicated with asthma or COPD; may reduce lung fxn (decreased FEV)

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79
Q

what are adverse reactions to insulin?

A

hypoglycemia, lipodystrophy, lipoatrophy, or insulin resistance

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80
Q

agents which increase blood glucose

A

glucocorticoids, thyroid hormone + calcitonin, somatropin, oral contraceptives, catecholamines, isoniazid, phenothiazines, morphine

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81
Q

agents which increase risk of insulin hypoglycemia

A

beta blockers, ACE inhibitors, somatostatin, anabolic steroids, ethanol, MAO inhibitors, fluoxetine, exercise

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82
Q

sulfonylureas mechanism/effects

A

sulfonylurea binds to receptor, inactivates K+ channel and depolarizes the cell, activates voltage-gated Ca++ channels and increases exocytosis of insulin-containing granules, thus increasing Phase 1 insulin release; also increases beta cell sensitivity to glucose

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83
Q

first generation sulfonylureas

A

tolbutamide, tolazamide, chlorpropamide

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84
Q

second generation sulfonylureas

A

glipizide, glyburide, glimepiride

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85
Q

repaglinide

A

non-sulfonylurea hypoglycemic agent, taken preprandially, quick onset

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86
Q

starlix (nateglinide)

A

non-sulfonylurea K+ channel blocker, specific for pancreas vs. CV tissue, shorter T0.5 than repaglinide so lower risk of hypoglycemia, preprandial, synergistic with metformin

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87
Q

glinides

A

repaglinide (Prandin), nateglinide (Starlix), mitiglinide (Glufast)

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88
Q

adverse effects of sulfonylureas

A

prolonged hypoglycemia (bc of long half-life), neurological damage and death (due to hypoglycemia), weight gain, GI problems

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89
Q

drug interactions causing hyperglycemia with sulfonylureas by enhancing their action

A

salicylates, sulfonamides, phenylbutazone (NSAID), clofibrate

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90
Q

drugs interactions causing hyperglycemia with sulfonylureas by causing hypoglycemia also

A

alcohol, high dose salicylates

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91
Q

What are effects of glucagon-like peptide?

A

stimulates insulin secretion and increases sensitivity to insulin, suppresses glucagon secretion, slows gastric emptying, reduces food intake, increases beta-cell mass and function

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92
Q

By what pathway does GLP-1 lead to increased beta cell mass?

A

GLP-1 + receptor –> GPCR beta gamma subunit –> ERK 1/2 phosphorylation –> increased gene transcription and beta cell proliferation

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93
Q

GLP-1 analogs

A

exenatide, victoza, tanzeum, dulaglutide

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94
Q

exenatide and victoza

A

GLP-1 analogs; co-administered with metformin, TzDs, or sulfonylureas; adverse effects are nausea, vomiting, pancreatitis, and thyroid cancer (monitor calcitonin levels)

95
Q

tanzeum

A

GLP-1 analog with a long half life because it is bound to serum albumin, injected SQ once/week

96
Q

dulaglutide

A

GLP-1 analog bound to IgG Fc, slowly released by reduction of the linking disulfide bonds, risk of thyroid C-cell tumors and contraindicated in patients with a family history of medullary thyroid cancer

97
Q

glucagon-like peptide 1 modulators (inhibitors of DPP-4)

A

januvia, nesina, tradjenta, onglyza

98
Q

januvia, nesina, tradjenta, onglyza - features and adverse effects

A

administered once daily, may facilitate weight loss, may be co-administered with metformin and TzDs, side effects: nausea, vomiting, constipation, headache, severe skin reactions, possible increased risk of infections (reduced white count) and cancers

99
Q

metabolism of januvia and nesina

A

not extensively metabolized, excreted in urine

100
Q

metabolism of tradjenta

A

not extensively metabolized, excreted in feces

101
Q

metabolism of onglyza

A

metabolized by CYP3A4/5, major metabolite is active, excreted in urine

102
Q

symlin

A

amylin analog, peptide hormone, slows gastric emptying, decreases food intake, decreases glucagon secretion, blunts postpradial blood glucose rise, used with insulin

103
Q

acarbose, miglitol

A

alpha glucosidase inhibitors; decreases carbohydrate absorption from the intestinal epithelium by inhibiting alpha glucosidases (maltase, sucrase, glucoamylase) on the brush border

104
Q

adverse effects of acarbose and miglitol

A

diarrhea, nausea, flatulence, acarbose can cause liver damage at higher doses

105
Q

sodium-glucose transporter 2 (SGLT2) inhibitors

A

canagliflozin, dapagliflozin, empagliflozin: increase glucose excretion in urine

106
Q

canagliflozin, dapagliflozin, empagliflozin

A

orally active, increases risk of genital/UT infections, increased urine flow/volume, increased risk of hypoglycemia with sulfonylureas and insulin, contraindicated in patients with renal impairment, do not use DAPAGLIFLOZIN in patients with bladder cancer

107
Q

metformin

A

anti-hyperglycemic agent, lower risk for hypoglycemia than sulfonylureas, activator of AMP-activated kinase (AMPK), in liver decreases gluconeogenesis and in muscle/fat increases glucose uptake and glycolysis

108
Q

metformin mechanism in muscles

A

AMP accumulates in muscles while exercising and activates AMPK, which phosphorylates TBC1D1/4 which promotes GTPase activity of Rab, which dissociates from GLUT4 and allows it to translocate to the membrane

109
Q

adverse effects of metformin

A

possible lactic acidosis, decreases B12 absorption

110
Q

what effect does metformin have on the blood lipid profile?

A

decreased serum LDL and triglycerides

111
Q

thiazolidinediones

A

rosiglitazone, pioglitazone (restricted prescribing due to CV toxicities, hepatotoxicity, and increased risk of bladder cancer)

112
Q

when are rosiglitazone and pioglitazone contraindicated?

A

CHF

113
Q

what is the mechanism of rosiglitazone and pioglitazone?

A

activate peroxisome proliferator-activated receptor gamma (PPARgamma), a transcription factor (particularly in adipocytes) - reduces insulin resistance and increases target cell response to insulin

114
Q

what happens to resistin, TNFalpha, and adiponectin in response to TzDs?

A

resistin and TNFalpha decrease, and adiponectin increases

115
Q

What adipokines are elevated in obesity?

A

leptin, angiotensinogen (AGE), plasminogen activator inhibitor 1 (PAI-1)

116
Q

What happens during growth of eunuchs and why?

A

Grow with long limbs and short torsos, because gonadal steroids promote epiphysial fusion

117
Q

somatropin, somatrem

A

growth hormones injected once daily, somatropin is less antigenic than somatrem

118
Q

nutropin depot

A

encapsulated form of somatropin, injected IM once or twice monthly

119
Q

side effects of growth hormone therapy in children

A

intracranial hypertension, visual changes, headache, nausea, type 2 DM, scoliosis

120
Q

side effects of growth hormone therapy in adults

A

peripheral edema, arthralgias, carpal tunnel syndrome, myalgias, mild to moderate nausea and headache, increases mortality in critically ill patients?

121
Q

mecasermin/mecasermine rinfabate

A

reconbinant IGF-1 and IGF-1/IGFBP-3; treat Laron-type dwarfism for example (GHR deficient, GH high, low plasma IGF-1, inheritable)

122
Q

sermoralin acetate

A

growth hormone releasing agonist - works on pituitary gland to make it release more GH (from Google)

123
Q

lanreotide, octreotide, pasireotide

A

somatostatin analogs which suppress GH release from growth hormone secreting tumors derived from growth hormone producing pituitary cells; all have greater affinity for SSTR2 and SSTR5 than other receptors, which are more important for GH inhibition

124
Q

pegvisomant

A

growth hormone antagonist which treats acromegaly - binds to the GH receptor and does not allows it to dimerize but not activate downstream pathways

125
Q

bromocriptine, carbegoline

A

dopamine agonists (prolactin antagonists) which activate D2 receptors, used to treat growth hormone secreting tumors derived from lactotrophic pituitary cells; also treats tumors which secrete BOTH GH and prolactin

126
Q

features of dopamine agonists (bromocriptine, carbegoline)

A

circulate bound to albumin, administered orally, metabolized and excreted in feces

127
Q

adverse reactions to dopamine agonists (bromocriptine, carbegoline)

A

nausea, headache, fatigue

128
Q

chorionic gonadotropin for injection

A

Pregnyl; purified from urine of pregnant women, has LH activity, used to treat infertility after doses of menotropins

129
Q

menotropins

A

menopur, pergonal, humegon, repronex; LH and FSH activities; purified from the urine of post-menopausal women; treats infertility by causing ovulation (with Pregnyl)

130
Q

urofollitropin

A

FSH activity; purified from the urine of menopausal women; same use as menotropins

131
Q

follitropin-alpha and follitropin-beta

A

recombinant human FSH; used instead of menotropins; half lives are shorter than human FSH because of different carbohydrate moieties

132
Q

recombinant human LH

A

lutropin alfa; used in combo with follitropin-alpha for women with LH deficiency but not to induce ovulation

133
Q

recombinant human chorionic gonadotropin

A

choriogonadotropin alfa

134
Q

Clomiphene

A

anti-estrogen used to induce ovulation in polycystic ovarian syndrome

135
Q

What drugs cause ovarian hyperstimulation

A

clomiphene and menopausal gonadotropins

136
Q

What adverse effect can occur in men treated with gonadotropins?

A

gynecomastia

137
Q

Thyrogen (thyrotropin)

A

half life 22 hours, removed by kidney, binds to TSH receptor and induces increased cAMP and increased TH production, used in tests involving radioactive iodine uptake by residual thyroid gland or metastasized thyroid carcinoma

138
Q

gonadorelin hydrochloride

A

GnRH for injection; diagnostic purposes; can cause headache, light-headedness, nausea, and flashing

139
Q

leuprolide acetate

A

GnRH for injection

140
Q

histrelin acetate

A

GnRH for injection

141
Q

nafarelin acetate

A

GnRH for nasal spray

142
Q

goserelin acetate

A

GnRH analog

143
Q

triptorelin pamoate

A

GnRH analog for injection

144
Q

ganirelix

A

GnRH antagonist; injected SQ; suppresses LH for assisted reproductive technology programs

145
Q

cetorelix

A

GnRH antagonist; injected SQ; suppresses LH for assisted reproductive technology programs

146
Q

abarelix

A

GnRH antagonist; injected SQ; treats advanced prostate cancer

147
Q

degarelix

A

GnRH antagonist; injected SQ; treats advanced prostate cancer

148
Q

synthetic gonadotropin releasing hormone characteristics

A

D-amino acids at position 6 (decrease proteolysis), ethylamide substituted for glycine at position 10 (increase affinity to receptor); used to treat female or male infertility (hypogonadotropic hypogonadism); constant use can lead to menopause-like Sx

149
Q

what does a weak response of LH to injected GnRH mean? what about a strong response?

A

weak response - pituitary dysfunction

strong response - hypothalamic lesion

150
Q

pasireotide

A

long acting somatostatin analog, used for acromegaly when surgery has not worked or is contraindicated

151
Q

sandostatin (octreotide acetate)

A

SST analog; used for metastatic carcinoid tumors, VIP-secreting adenomas, gastrinomas, gucagonoma, watery diarrhea-hypokalemia-and-achlorhydria syndrome (WDHA), acromegaly

152
Q

effect of octreotide acetate on GH vs insulin

A

better at suppressing GH than insulin, so useful for treatment of conditions because it doesn’t cause concurrent hyperglycemia

153
Q

side effects of octrotide acetate

A

nausea, abdominal cramps, flatulence, steatorrhea

154
Q

oxytocin (pitocin, syntocinon)

A

oxytocin; IV or nasal spray

155
Q

vasopressin (pitressin)

A

synthetic vasopressin

156
Q

desmopressin acetate

A

synthetic vasopressin with only ADH effect (little to no pressor effect); IV/SQ injection or nasal spray

157
Q

conivaptan HCL

A

vasopressin receptor antagonist; V1a and V2 antagonist; treats hyponatremia

158
Q

tolvaptan

A

vasopressin receptor antagonist; V2 > V1 receptors; treats hyponatremia

159
Q

demeclocycline

A

tetracycline antibiotic; suppresses ADH action through attenuation of cAMP production

160
Q

levothyroxine sodium

A

soidum salt of synthetic thyroxine available in tablets and for injection, most patients take this

161
Q

liothyronine sodium

A

sodium salt of triiodothyronine available in tablets or for injection; risk of cardiac toxicity

162
Q

liotrix

A

mixture of sodium salts of levothyroxine and liothyronine

163
Q

radioactive iodine 131

A

destroys thyroid gland; used to treat thyrotoxicosis in older patients; contraindicated in pregnancy and nursing; used to diagnose disorders of thyroid fxn

164
Q

propylthiouracil (PTU)

A

thioamide, interferes with thyroid hormone synthesis by interfering with thyroid peroxidase enzyme by inactivating the oxidized heme of the peroxidase; PTU inhibits peripheral conversion of T4 to T3 by inhibiting type 1 deiodinase; used in pregnancy because it doesn’t cross the placenta as much

165
Q

methimazole

A

thioamide, interferes with thyroid hormone synthesisby interfering with thyroid peroxidase enzyme by inactivating the oxidized heme of the peroxidase; preferred over PTU generally

166
Q

potassium iodide (lugol’s solution, SSKI, thyroshield, tablets)

A

preparations of iodide for hyperthyroidism

167
Q

ipodate

A

iodinated contrast media which inhibits the deiodination of T4 to T3; used for thyroid storm when thioamides and iodides are contraindicated

168
Q

amiodarone

A

has a very high iodine content

169
Q

fluoxymesterone

A

anabolic steroid with androgenic properties; oral admin

170
Q

methyltestosterone

A

Type B androgen preparation; 17alpha alkylation slows inactivation in liver, can cause liver damage; androgenic steroid; oral admin

171
Q

nandrolone decanoate

A

Type C androgen preparation; androgens with changes in the ring structure; anabolic steroid

172
Q

oxandrolone

A

anabolic steroid

173
Q

oxymetholone

A

anabolic steroid

174
Q

testosterone cypionate in oil

A

androgenic steroid; IM injection

175
Q

testosterone transdermal system

A

skin patch, keeps serum testosterone levels from fluctuating as much

176
Q

testosterone enanthate in oil

A

Type A androgen preparation; esterification of 17beta-hydroxyl group with carboxylic acids (more soluble in lipid vehicles for injection); androgenic steroid; IM injection

177
Q

abiaterone

A

inhibits 17alpha hydroxylase enzyme (blocks formation of testosterone upstream)

178
Q

bicalutamide

A

non steroid; competitively inhibits androgen receptor

179
Q

danazol

A

weak androgen used to treat endometriosis

180
Q

dutasteride

A

competitively inhibits 5alpha reducutase; treats BPH

181
Q

finasteride

A

competitively inhibits 5alpha reductase; treats BPH

182
Q

flutamide

A

non steroid; blocks androgen action by competitively binding to the androgen receptor

183
Q

nilutamide

A

non steroid; competitively inhibits androgen receptor

184
Q

fludrocortisone

A

F at 9alpha, leads to edema bc of Na+ retention, used for mineralocorticoid replacement therapy
tissue half life 8-12 hours

185
Q

prednisone/prednisolone

A

core structure: cortisol
prednisone has a ketone at the 11beta position and a DB between C1 and C2
prednisolone has a hydroxyl at the 11beta position and a DB between C1 and C2
intraconvertible by 11beta hydroxysteroid dehydrogenase
tissue half life 12-36 hours

186
Q

methylprednisone

A

core structure: cortisol
methylated at 6alpha position
potency similar to prednisolone
tissue half life 12-36 hours

187
Q

triamcinolone

A 
core structure: cortisol
F at 9alpha position, hydroxyl at 16alpha position
potency similar to prednisone
low oral bioavailability
increased hydrophilicity
tissue half life 12-36 hours
188
Q

dexamethasone, betamethasone

A 
16alpha hydroxyl (enantiomers)
tissue half life 36-54 hours
189
Q

topical glucocorticoids

A

triamcinolone acetonide
betamethasone valerate
higher lipophilicity so better potency in topical applications

190
Q

21-chlorocorticoids

A

clobetasol propionate (21-chloro analog of betametasone 17-propionate)
halobetasol propionate
halcinonide

high potency, topical application

191
Q

fluticasone propionate

mometasone furoate

A

medium potency
topical corticosteroids
poor dissolution into inflamed tissue despite high lipophilicity and high binding affinity

192
Q

inhaled glucocorticoids

A 
triamcinolone acetonide (acetonide is resistant to hydrolysis, more potent than prednisolone, also a topical glucocorticoid)
beclomethasone dipropionate (converted to 17 monopropionate by hydrolysis, more potent than dexamethasone)
193
Q

other inhaled glucocorticoids

A

flunisolide, budesonide, mometasone furoate (also a medium potent topical), fluticasone propionate (also a medium potent topical steroid)

194
Q

ethinyl estradiol, mestranol, quinestrol

A

17alpha alkylated estrogens, enhanced oral bioavailability

195
Q

estradiol valerate, estradiol cypionate

A

esterification of 17beta hydroxyl, slows absorption from injection site and prolongs action

196
Q

premarin

A

pregnant mare urine, mixture of estrogens (estrone sulfate 50-60% and equilin sulfate 20-30%)

197
Q

tamoxifen, toremifene

A

prodrug which is oxidized in vivo, partial estrogen agonist, used to treat/prevent breast cancer; weak estrogen agonist at endometrial cells, increases risk for thrombus, prevents osteoporosis (toremifene is similar)

198
Q

raloxifene, bazedoxifene

A

SERM (selective estrogen receptor modulator), prevents osteoporosis, decreases LDL, pro-thrombotic, decreases risk for breast cancer, does not stimulate endometrial cells, may cause hot flashes

199
Q

clomiphene

A

SERM, increases secretion of FSH and LH by inhibiting negative estradiol feedback. used in polycystic ovary syndrome to stimulate ovulation

200
Q

fulvestrant

A

selective estrogen receptor downregulator, pure receptor antagonist, used in patients who have become resistant to tamoxifen

201
Q

anastrozole, letrozole, exemestane

A

aromatase inhibitors (blocks conversion of testosterone to 17 beta estradiol), used in pts whose breast cancer has become resistant to tamoxifen

202
Q

norethindrone

A

used as progestin component in several formulations of oral contraceptives (mono-, bi-, and tri-phasic preparations)

203
Q

ethynoldiol diacetate

A

progestin?

204
Q

norgestimate –> levonorgestrel

A

norgestimate is prodrug, high oral bioavailability of levonorgestrel (2nd gen progestin); levonorgestrel is used in high dose as Plan B

205
Q

desogestrel –> etonogestrel

A

3rd gen progestin, prodrug desogestrel converted to etonogestrel, similar to levonorgestrel, high oral bioavailability, used in nuvaring and nexplanon

206
Q

drospirenone

A

4th gen progestin, antimineralocorticoid activity, negates side effects of ethynyl estradiol in combo therapy, antiandrogenic and no antiestrogen activity (desirable)

207
Q

medroxyprogesterone acetate

A

1st gen progestin, used for depo-provera

208
Q

mifepristone

A

progesterone antagonist, postcoital contraceptive, used with misoprostol (PGE) as abortifacient

209
Q

danazol

A

used for endometriosis, inhibits surge of LH and FSH and suppresses ovarian fxn, contraindicated with hepatic dysfunction and pregnancy

210
Q

phenytoin, rifampin

A

increases drug metabolizing enzymes in the liver, may interact with oral contraceptives

211
Q

tetracyclines

A

suppress gut flora that participate in enterohepatic recycling

212
Q

PTH

A

deletion of aa 1 and 2 eliminates activity; increases resorption of Ca2+ from collecting tubules (ECaC/TrpV5), increases Ca2+ resorption from bone, increases PO4 loss in urine, increases 1,25 (OH)2 D3 production by kidney; PTH release triggered by low serum Ca2+ levels and GPCR that binds Ca2+

213
Q

vitamin D

A

increases Ca2+ and PO4 absorption from small intestine via ECaC2/TrpV6 on brush border; inhibition of PTH; calbindins and vit D binding protein

214
Q

calcitonin

A

inhibits osteoclast bone resorption, increases Ca2+ and PO4 loss in urine (blocks resorption), stimulated by high serum calcium levels; Salmon and Human; used for paget’s, hypercalcemia (loses efficacy), osteoporosis >5 yrs postmenopause (alternative treatment)

215
Q

bisphosphonates

A

first line for osteoporosis; inhibit bone resorption; 50% of absorbed dose (10%) accumulates in bone; adverse effects = nausea, vomiting, diarrhea, “dronates”

216
Q

denosumab

A

humanized monoclonal Ab against RANKL; used for osteoporosis (2nd line); treats osteoporosis in postmenopausal women with a history of fractures, high risk of fractures, or intolerance to bisphosphonates; adverse effects are hypocalcemia, osteonecrosis of the jaw, atypical femur fractures, musculoskeletal pain, severe infections, and skin reactions

217
Q

teriparatide

A

second line for osteoporosis; amino acids 1-34 of parathyroid hormone produced in E. coli; stimulates osteoblast when injected SQ daily with oral Ca2+ and vit D; can cause orthostatic hypertension, hypercalcemia, arthralgias, and allergic reactions; interacts with PTH/PTHrp receptor (GPCR) on osteoblasts and kidney cells

218
Q

vitamid D analogs

A

zemplar, hectorol (prodrug hydroxylated by CYP 27 in liver); inhibit secretion of PTH with less effect on serum Ca2+ than 1,25 (OH)2 vit D3; treats secondary hyperparathyroidism; given 3X per week by IV or oral

219
Q

cinacalcet

A

treatment of secondary hyperparathyroidism in chronic kidney disease with dialysis (loss of 1,25 (OH)2 vit D3 production); decreases serum PTH levels and serum Ca2+ levels

220
Q

what is the mechanism of bisphosphonates

A

inhibits farnesyl pyrophosphate synthase (FPPS) and disrups prenylation of proteins in osteoclasts,

221
Q

how does teriparatide increase bone mass?

A

when administered constantly, increases RANKL (which signals for osteoclast formation) and decreases OPG (osteoprotegerin); when administered intermittently, increases pre-osteoblasts called cbfa1 and leads to increased osteoblast number/fxn and increased bone mass and strength

222
Q

what is the mechanism of denosumab?

A

binds to RANKL and prevents activation of RANK on osteoclast precursors, preventing differentiation of osteoclasts; injected SQ every 6 mo and pts concurrently take Ca2+ and VitD daily

223
Q

factors released from osteocytes that upregulate osteoblast/clast activity

A

prostaglandins, nitric oxide, dentin matrix protein 1

224
Q

factors released from osteocytes that downregulate osteoblast/clast activity

A

sclerostin, osteocalcin, matrix extracellular phosphoglycoprotein (MEPE)

225
Q

Paget’s disease

A

uncontrolled osteoclastic bone resorption and secondary poorly organized bone formation; Sx: bone pain, bone deformities, loss of hearing, hypercalcemia, may be caused by slow-acting virus

226
Q

how do loop diuretics (eg furosemide) affect serum Ca2+ levels?

A

the increase Ca2+ excretion because there is a decreased driving force for uptake with inhibition of Na+/K+/2Cl- co-transporter

227
Q

how do thiazides affect serum Ca2+ levels?

A

decreased Ca2+ excretion because increased driving force for uptake with inhibition of Na/Cl transporter in distal tubule

228
Q

How do PPIs and H2 antagonists affect serum Ca2+ levels?

A

decreased acidity of stomach decreases Ca2+ absorption (omeprazole may inhibit bone resorption)

229
Q

How do carbemazepine, isoniazid, theophylline, and rifampin affect serum Ca2+ levels?

A

they induce Vit D catabolic P450s, leading to lower serum Ca2+??

230
Q

which bisphosphonates treat Paget’s?

A

PagET’s
pamidronate
tiludronate
etidronate

231
Q

which bisphosphonates treat osteoporosis

A 
RAIZ
risedronate
alendronate
ibandronate
zoledronate (once/year infusion)
232
Q

second line treatments for osteoporosis

A

estrogens and SERMs: estradiol, premarin, raloxifene (least cancer risk, but inc. risk of VTE and stroke)

233
Q

teriparatide vs bisphosphonates

A

teriparatide builds bone mass at a higher rate than bisphosphonates, but they may cause bone cancer so reserved for severe cases of osteoporosis; also teriparatide must be injected daily

234
Q

treatment of hyperphosphatemia and prevention of calcific uremic arteriolopathy

A

lanthanum carbonate (decreases PO4 and Ca2+) and sevelamer (decreases serum PO4 selectively)

Pharmacology Histamine/GI (1 decks)

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