Pharm - Endocrine and GI Flashcards

1
Q

Anti-thyroid classes

A

Iodides (Iodide 131, inorganic iodid)

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2
Q

Iodide 131 info

A
  • Carcinogenic at low doses, thyroablative at high doses
  • beta wave emission destroys surrounding tissues
  • generally results in hypothyroid
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3
Q

Inorganic iodide mechanism

A
  • High levels inhibit organification and hormone release (Wolff-Chaikoff effect)
  • Negative feedback loop
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4
Q

Inorganic iodide uses

A
  • Not for long-term therapy (function returns in a few days)

- Prevent thyroid from radioactive iodide exposure

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5
Q

Thioamide exemplar

A

Methimazole

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6
Q

Methimazole mechanism

A

Compete with thyroglobulin for oxidized iodide –> less available for T4 production (affects synthesis)

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7
Q

Methimazole adverse effects

A
  • Goiter, pruritic rash early in treatment, arthralgia

- serious: agranulocytosis, hepatotoxicity, vasculitis

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8
Q

Methimazole treatment exceptions

A
  • Thyroid storm treatment (propylthiouracil preferred)

- pregnancy, d/t teratogenicity

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9
Q

Hypothyroid treatment

A

Levothyroxine (equivalent to oral T4)

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10
Q

Levothyroxine dosing/ interactions/ side effects

A
  • take on empty stomach in morning, 4 hours away from calcium and iron supplements
  • monitor TSH if taking with PPI or antacids
  • may interfere with glycemic control
  • over-replacement/ long-term assoc w/ decreased bone mineral density
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11
Q

Combination contraceptives progestins of note

A
Cyproterone acetate (used in Diane 35 - only for acne)
Drospirenone (used in Yaz/Yasmine - CV mortality)
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12
Q

Combination contraceptives mechanism

A
  • suppress gonadotropin section –> inhibit ovulation

- causes endometrial atrophy, viscous cervical mucus, alter secretion and peristalsis in fallopian tubes

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13
Q

Non-contraceptive benefits

A

Increased bone mineral density

Decreased acne; ovarian, endometrial, colorectal cancer; peri-menopausal sxs; fibroids; benign breast disease

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14
Q

Combination contraceptives absolute contraindications

A
  • <6 weeks postpartum if breastfeeding
  • smoker over 35 (>15 cigarettes/day)
  • hypertension
  • current/past hx blood clots , cerebrovascular accident
  • complicated valvular heart dz
  • current breast cancer
  • migraine HA w/ neuro sxs
  • diabetes w/ end organ involvement
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15
Q

Combination contraceptives side effects

A

Irregular bleeding, breast tenderness and nausea, amenorrhea, chloasma, possibly weight gain and mood changes

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16
Q

Contraceptive risks

A
  • blood clots
  • cervical cancer
  • breast cancer (controversial
  • Heart attack and stroke when taking >50yg ethinyl estradiol
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17
Q

Contraceptive drug interactions

A
  • May cause contraceptive failure: antiseizure meds, ritonavir, griseofulvin, rifampin, St John’s Wort
  • Increase activity: acetaminophen, erythromycin, fluoxetine and fluvoxamine, fluconazole, grapefruit juice, vitamin C
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18
Q

Insulin types and info

A

Rapid - for postprandial glyemia
Short acting - regular, IV in hospital for ketosis
Intermediate - basal insulin level support
Long acting - best basal insulin support

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19
Q

Insulin adverse effects

A
  • hypoglycemia/ hypoglycemic support
  • lipodystrophy at injection site
  • allergic rxns
  • worsened hypokalemia
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20
Q

Drugs increase glucose

A

Corticosteroids, diltiazem, diuretics, estrogens, thyroid hormones

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21
Q

Drugs decrease glucose

A

Alcohol, ACEi, beta blockers, clonidine, fluoroquinolones, MAOi

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22
Q

Glucose regulating agents that increase body weight

A

Thiazolidinedione (or no effect), sulfonylureas

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23
Q

Glucose regulating agents that increase LDL

A

Thiazolidinedione (or no effect)

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24
Q

Glucose regulating agents that decrease LDL

A

Metformin

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25
Q

Insulin secretagogue (Sulfonylureas) exemplar

A

Glyburide

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26
Q

Sulfonylureas mechanism

A

Direct inhibition of channels in beta cells –> cellular depolarization and opening of ca2+ channel –> insulin release

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27
Q

Glyburide indications

A

In conjugation with metformin when additional glucose lowering is necessary, may stabilize sugars and reduce adverse effects

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28
Q

Glyburide adverse effects

A

Hypoglycemia, skin rashes, N/V, cholestasis

rarely leukopenia, thrombocytopenia, hemolytic anemia

29
Q

Renal glucose reabsorption inhibitors

A

Sodium-glucose cotransporter 2 inhibitors

30
Q

Sodium-glucose cotransporter 2 inhibitors exemplar

A

Canagliflozin

31
Q

SGLT2 mechanism

A

decreased renal reabsorption –> increased glucose excretion

32
Q

Canagliflozin adverse effects

A
  • increased UTI and yeast infection
  • may cause volume depletion
  • may cause acute renal injury (more likely in dehydration, heart failure, low BP, ACEi)
  • increased risk of osteoporosis, fracture
33
Q

Insulin sensitizing classes and exemplars

A

Biguanides - Metformin

Thiazolidinedione - Rosiglitazone

34
Q

Metformin effects

A
  • reduction of hepatic glucose output by inhibiting gluconeogenesis
  • increases insulin sensitivity in peripheral tissues
35
Q

Metformin adverse effects

A
  • most common are GI (diarrhea)
  • increased risk of lactic acidosis in some pop
  • clinically relevant deficiency of B12
36
Q

Rosiglitazone mechanism

A

activation of PPAR-gamma –> increased insulin sensitivity in skeletal muscle and adipose tissue
less effect on the liver than metformin

37
Q

Rosiglitazone adverse effects

A
  • edema, increased plasma volume, increased risk of HF
  • CI in pts w/ or high risk of HF
  • increase risk of CV mortality
  • weight gain
  • decrease bone mineral density and increase risk of osteoporosis, fracture
38
Q

Incretin mimetic classes and exemplars

A

Glucagon-like peptide-1 agonists: Dulaglutide

Dipeptidyl peptidase-4 inhibitors: Sitagliptin

39
Q

GLP1 agonists mechanism

A

stimulates insulin by binding to pancreatic CPCR

40
Q

GLP1 agonist half life

A

2 minutes

41
Q

Dulaglutide indications

A

when other glucose lowering agents are ineffective

42
Q

Dulaglutide adverse effects

A

Nausea
Increased risk of pancreatitis
Possible increased risk of thyroid and pancreatic cancer

43
Q

Sitagliptin info

A

Do not cause hypoglycemia or GI side effects
can be used in renal insufficiency
may cause joint and skeletal muscle pain

44
Q

Dipeptidyl peptidase 4 inhibitors mechanism

A

doubles plasma GLP-1 levels

45
Q

Alpha glucoside inhibitors exemplar

A

Acarbose

46
Q

Acarbose mechanism

A

inhibits brush border breakdown of polysaccharides

47
Q

Acarbose adverse effects

A
  • increased flatulence
  • increases bioavailability of metformin
  • decreases iron absorption
48
Q

H2 receptor antagonist exemplar

A

Ranitidine

49
Q

H2 receptor antagonist mechanism

A

Competitive inhibition –> reduces gastric acid, pepsin, secretion of intrinsic factor

50
Q

Ranitidine indications

A
  • dyspepsia/ GERD/ heartburn

- Peptic ulcer disease - requires 6-8 weeks to heal 90% of ulcers

51
Q

PPI exemplar

A

Omeprazole

52
Q

PPI mechiasm

A

activated by protonation, irreversibly inactivate H+/K+/ATPase pump

53
Q

Omeprazole indications

A

Peptic ulcer disease
Zollinger-Ellison syndrome
Most effective for dyspepsia/ GERD/ heartburn
Prevents ulcers in pts taking NSAIDs

54
Q

Omeprazole adverse effects

A
  • commonly HA, nausea, diarrhea, abdominal pain, constipation, dizziness, fatigue, rash, pruritis
  • Allergic rxns, kidney disorders, dementia (inconclusive)
  • Long term - pneumonia, GI infections, vitamin and mineral deficiencies, osteoporosis and fracture
  • CI with clopidogrel
55
Q

Cytoprotective drugs

A

Sucralfate, Misoprostol

56
Q

Sucralfate mechanism

A

binds to ulcers, creating physical barrier

57
Q

Misoprostol mechanism

A

Prostoglandin E1 analog

  • binds to Pg receptors in stomach –> enhanced mucus production, blood flow, bicarbonate secretion
  • binds to PG receptors in parietal cells –> decreased acid secretion
58
Q

Misoprostol indications

A

gastric and duodenal ulcers, pts taking NSAIDs long term

high risk pts

59
Q

Misoprostol adverse effects, CI

A

Diarrhea and intestinal cramping

CI in pregnancy d/t inducing labor

60
Q

Antacids exemplars

A

Aluminum and magnesium hydroxide

61
Q

Antacids drawback

A

work for short time, aluminum causes constipation and magnesium diarrhea (together hopefully neither)

62
Q

Antidiarrheal exemplar

A

Loperamide

63
Q

Loperamide mechanism

A

opioid agonist with greater effect in intestinal smooth muscle

64
Q

Loperamide CI

A

children under 2, possibly not when signs of infection are present

65
Q

Prokinetic exemplar

A

Metoclopramide

66
Q

Metoclopramide mechanism

A

Blocks D2 receptors –> prevents relaxation

increases release of ACh from enteric plexus

67
Q

Metoclopramide indications

A

GERD, diabetic gastroparesis, intractable hiccup, drug induced / migraine related nausea

68
Q

Metoclopramide adverse effects, CI

A
  • drowsiness, extrapyramidal effects, seizures

- CI in seizure disorders, mechanical obstruction, HI hemorrhage, pheochromocytoma