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
Insulin secretagogue (Sulfonylureas) exemplar
Glyburide
26
Sulfonylureas mechanism
Direct inhibition of channels in beta cells --> cellular depolarization and opening of ca2+ channel --> insulin release
27
Glyburide indications
In conjugation with metformin when additional glucose lowering is necessary, may stabilize sugars and reduce adverse effects
28
Glyburide adverse effects
Hypoglycemia, skin rashes, N/V, cholestasis | rarely leukopenia, thrombocytopenia, hemolytic anemia
29
Renal glucose reabsorption inhibitors
Sodium-glucose cotransporter 2 inhibitors
30
Sodium-glucose cotransporter 2 inhibitors exemplar
Canagliflozin
31
SGLT2 mechanism
decreased renal reabsorption --> increased glucose excretion
32
Canagliflozin adverse effects
- 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
Insulin sensitizing classes and exemplars
Biguanides - Metformin | Thiazolidinedione - Rosiglitazone
34
Metformin effects
- reduction of hepatic glucose output by inhibiting gluconeogenesis - increases insulin sensitivity in peripheral tissues
35
Metformin adverse effects
- most common are GI (diarrhea) - increased risk of lactic acidosis in some pop - clinically relevant deficiency of B12
36
Rosiglitazone mechanism
activation of PPAR-gamma --> increased insulin sensitivity in skeletal muscle and adipose tissue less effect on the liver than metformin
37
Rosiglitazone adverse effects
- 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
Incretin mimetic classes and exemplars
Glucagon-like peptide-1 agonists: Dulaglutide | Dipeptidyl peptidase-4 inhibitors: Sitagliptin
39
GLP1 agonists mechanism
stimulates insulin by binding to pancreatic CPCR
40
GLP1 agonist half life
2 minutes
41
Dulaglutide indications
when other glucose lowering agents are ineffective
42
Dulaglutide adverse effects
Nausea Increased risk of pancreatitis Possible increased risk of thyroid and pancreatic cancer
43
Sitagliptin info
Do not cause hypoglycemia or GI side effects can be used in renal insufficiency may cause joint and skeletal muscle pain
44
Dipeptidyl peptidase 4 inhibitors mechanism
doubles plasma GLP-1 levels
45
Alpha glucoside inhibitors exemplar
Acarbose
46
Acarbose mechanism
inhibits brush border breakdown of polysaccharides
47
Acarbose adverse effects
- increased flatulence - increases bioavailability of metformin - decreases iron absorption
48
H2 receptor antagonist exemplar
Ranitidine
49
H2 receptor antagonist mechanism
Competitive inhibition --> reduces gastric acid, pepsin, secretion of intrinsic factor
50
Ranitidine indications
- dyspepsia/ GERD/ heartburn | - Peptic ulcer disease - requires 6-8 weeks to heal 90% of ulcers
51
PPI exemplar
Omeprazole
52
PPI mechiasm
activated by protonation, irreversibly inactivate H+/K+/ATPase pump
53
Omeprazole indications
Peptic ulcer disease Zollinger-Ellison syndrome Most effective for dyspepsia/ GERD/ heartburn Prevents ulcers in pts taking NSAIDs
54
Omeprazole adverse effects
- 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
Cytoprotective drugs
Sucralfate, Misoprostol
56
Sucralfate mechanism
binds to ulcers, creating physical barrier
57
Misoprostol mechanism
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
Misoprostol indications
gastric and duodenal ulcers, pts taking NSAIDs long term | high risk pts
59
Misoprostol adverse effects, CI
Diarrhea and intestinal cramping | CI in pregnancy d/t inducing labor
60
Antacids exemplars
Aluminum and magnesium hydroxide
61
Antacids drawback
work for short time, aluminum causes constipation and magnesium diarrhea (together hopefully neither)
62
Antidiarrheal exemplar
Loperamide
63
Loperamide mechanism
opioid agonist with greater effect in intestinal smooth muscle
64
Loperamide CI
children under 2, possibly not when signs of infection are present
65
Prokinetic exemplar
Metoclopramide
66
Metoclopramide mechanism
Blocks D2 receptors --> prevents relaxation | increases release of ACh from enteric plexus
67
Metoclopramide indications
GERD, diabetic gastroparesis, intractable hiccup, drug induced / migraine related nausea
68
Metoclopramide adverse effects, CI
- drowsiness, extrapyramidal effects, seizures | - CI in seizure disorders, mechanical obstruction, HI hemorrhage, pheochromocytoma