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Advanced Pharmacology > Week 2 Endocrine > Flashcards

Week 2 Endocrine Flashcards

1
Q

A1C reduction with glucose

What is the gold standard?

A

Insulin

reduces A1C by about 2.5

Everything else about 1.5

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2
Q

What drugs to use when compelling need to minimize hypoglycemia? (4)

A

DPP4
GLP1
SGLT2
TZD

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3
Q

Thiazolidinediones (2)*

A

Rosiglitazone (Avandia)

Pioglitazone (Actos)

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4
Q

Beta-Adrenergic Antagonists

MOA

Common agents

AE

A

Acts by decreasing symptoms of adrenergic stimulation caused by T4 concentrations
Inhibits peripheral conversion of T4 to T3

Propanolol (non selective BB)

Decreased BP, bradycardia, cardiac arrest
CHF, Asthma

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5
Q

Insulin Preparations

A

Rapid
Short
Intermediate
Long

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6
Q

Biguanides Old Contraindications*

A

Male Creatinine >/- 1.5mg/dL

Female Creatinine >/- 1.4mg/dL

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7
Q

What drug?

Direct acting (categorized based on duration after injection)

Major SE: Hypoglycemia

A

Insulin

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8
Q

Causes/Diagnoses of Hypothyroidism (3)

T4 concentrations
TSH concentrations

A

Hashimoto’s thyroiditis
Surgery
Meds (Lithium, RAI, Amiodarone)

Decreased total and free T4
Elevated TSH

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9
Q

What insulin cannot be mixed with others?*

A

Long Acting*

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10
Q

Basal Insulin

Adults secrete about __ unit of insulin per ___ regardless of food intake

A

Secreted in small amounts throughout the day 50%

1 unit per hour

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11
Q

DPP-4 Inhibitors

Adverse Effects

A

Well tolerated
Pancreatitis (rare)
Heart disease?

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12
Q

What drug?

Activates PPAR (steroid hormon) -> insulin sensitivity

Major SE: Peripheral edema, heart failure, bone loss, weight gain

A

Thiazolidinediones

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13
Q

Thioureas*

AE(3)

A

Rash
Fluid Retention
Decreased WBC** reverses on discontinuation if caught early

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14
Q

Types of Therapy for Hyperthyroidism (3)

A

Surgery
Meds
Radioactive iodine

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15
Q

GLP-1 Agonists*

What is it?

A

Recombinant peptide that shares 53% of amino acid sequence w human GLP-1

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16
Q

SGLT 2 Inhibitors

Administration

A

Oral daily dosing

Dose must be adjusted for renal dysfunction

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17
Q

Canagliflozin (Invokana)

Dosing
Admin 
Renal Dose Adjustment 
Cost 
Patient Assistance
A 
100-300mg daily 
Before first meal of the day
Yes
350$ for 30 tablets 
Available
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18
Q

DPP-4 Inhibitors CV Safety

A

Overall they were neutral

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19
Q

Dapagliflozin (Farxiga)

Dosing 
Admin 
Renal Dose Adjustments 
Cost
Patient Assistance
A 
5-10mg daily 
In the morning with or without food 
Yes 
$350 for 30 tablets 
Available
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20
Q

Oral Combination Products a lot are combined with what drug?

A

Metformin

ie) Pioglitazone + Metformin, Glyburide + Metformin, etc

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21
Q

Thiazolidediones

AE (2)
____ Risk
Pioglitazone recommended against use if you have

A

Hepatotoxicity, Edema
Fracture (reduces osteoblastic activity and increases urinary calcium excretion)
Bladder Ca or hx

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22
Q

Hypoglycemia Picture of Sx

What do you do?

A 
Shaky 
Fast Heartbeat 
Sweating 
Dizzy
Anxious 
Hungry 
Blurry Vision 
Weakness of Fatigue 
Headache
Irritable

Check -> Tx -> Check

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23
Q

Thyroid Hormones effect (2)

A

Growth and Development

Maintain metabolic stability

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24
Q

Short Acting Insulin (1)

A

Regular Humulin R

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25
Q

Biguanides New Contraindications*

A

GFR <30 = Contraindicated
GFR 30-45 = Do not start
GFR dips < 45 = Re-evaluate vs cut dose in half
GFR 30-60 with iodinated contrast = hold for 48 hrs

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26
Q

Adverse Effects of Insulin* (4)

A

Hypoglycemia
Insulin Allergy
Immune Insulin Resistance
Lipohypertrophy (rotate injection sites)

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27
Q

SGLT -2 CV Safety*

A

Significant CV reduction of residual CV risk!

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28
Q

GLP-1 Agonists (4)*

A

Exenatide (Byetta)
Liraglutide (Victoza)
Albiglutide (Tanzeum)
Duglaglutide (Trulicity)

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29
Q

Rapid Acting Insulin (3)

A 
Insulin Lispro (Humalog) 
Insulin Aspart (Novalog) 
Insulin Glulisine (Aventis)
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30
Q

Levothyroxine*

Considered a “____”
Produces physiologic levels of?
Onset

A

Prodrug
T4 and T3
2-3 wks

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31
Q

What drugs to use when ASCVD predominates

A

1) SGLT2i*

2) GLP 1

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32
Q

Bolus Insulin

Also called

Larger amounts secreted in response to food to

A

In response to food 50%

Premeal, mealtime, prandial, nutritional insulin

Decrease postprandial hyperglycemia

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33
Q

Duration of action of Insulin is ______ in pts with (2) failure

A

Prolonged

Hepatic and Renal

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34
Q

Intermediate Acting Insulin

Onset
Peak
Duration
\_\_\_ used for \_\_\_\_ IV use 
Usually administered 
Appearance*
A 
2-4 hr 
4-8 hr 
8-12 hr 
NOT for emergency 
1-2 times/day 
CLOUDY
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35
Q

Glucagon

A

Secreted by a cells

Increases hepatic glucose output -> increases blood glucose concentration

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36
Q

Thioureas*

MOA

A

Inhibits iodination of tyrosine
Coupling of iodotryrosines

PTU also inhibits peripheral conversion of T4 to T3
DOES NOT effect release of preformed T4 and T3

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37
Q

Glipizide (2)*

Duration
Active Metabolite
Elimination

A

Glucotrol, Glucotrol XL

12-16 hrs
Inactive
90% Hepatic

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38
Q

GLP 1 Agonists*

AE (3)

A

N/V
HA
Pancreatitis

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39
Q

Storage of Insulin*

A

Refrigerate if not in use
Room Temperature if in use/limit to 28 days

Away from direct heat or light

Check for clumps, frosting, failure to stay in suspension when mixed
Never use cloudy or discolored insulin except for NPH

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40
Q

Meglitinides Potential Advantages

_____ onset and ____ duration of action
May be used in pts with ____ insufficiency
May be useful in pts who ___ meals

AE (2)

A

Rapid, short
Renal
Skip

Hypoglycemia
Weight Gain

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41
Q

Diabetes Mellitus

A

A syndrome that develops when insulin secretion or activity are not sufficient to maintain blood glucose levels

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42
Q

Intermediate Acting Insulin (2)

A

NPH Humulin N

NPH Novolin N

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43
Q

*Insulin Dose based on:

Type 2:
Type 1:

Observe for

A

Total Body Weight

0.2 u/kg/day
Depends

Trends in hypoglycemia and hyperglycemia

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44
Q

Comparison of Common Agents

Equvalent Glucocorticoid dose, Mineralcorticoid potency

1) Hydrocortisone
2) Cortisone
3) Prednisone
4) Methylprednisolone
5) Dexamethasone

A

1) 20, +2
2) 25, +2
3) 5, +1
4) 4, +1
5) 0.75, 0

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45
Q

Levothyroxine Adverse Effects (4)*

A

HF
Angina (painful constriction of tightness)
MI
Hyperthyroidism

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46
Q

Short Acting Insulin

Onset 
Peak 
Duration 
Administered 
May be given 
Appearance
A 
30 min 
2-3 hr 
4-6 hr 
30-45 min before a meal*
IV
Clear
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47
Q

Intermediate/Long Uses (2)

A

Basal insulin needs

Not to cover meals

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48
Q

Thioureas (2)*

A

Propylthiouracil (PTU)

Methimazole (Tapazole)

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49
Q

DM Type II

A

NIDDM
- results from insulin secretory defect and insulin resistance
RELATIVE lack of insulin

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50
Q

Thyroid Hormone Synthesis and Release

A

Iodine + Tyrosine
Organification into T1 and T2
Coupling into T3 and T4
Secretion of T3 and T4 into circulation

T4 is solely secreted from thyroid gland

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51
Q

Gestational Diabetes

A

Onset or discovery of glucose intolerance during pregnancy

52
Q

Natural Thyroid Hormones
(____ Thyroid)

Dessicated (3) thyroid
Contains a ____ quanitity of T4 and T3
Bioavailability is ______
Allergies

A

Armour

Hog, Beef, Sheep
Standardized
Unpredictable

53
Q

Meglitinides

MOA

Onset
Peak
Duration
Metabolized

A

Same as sulfonylureas

15 min
60-90 min
< 4 hrs
CYP3A4

54
Q

DPP-4 Inhibitors (4)*

A

Sitagliptin (Januvia)
Saxagliptin (Ongylza)
Alogliptin (Nesina)
Lingagliptin (Tradjenta)

55
Q

What drugs to use when HF/CKD predominates

A

1) SGLT2i if eGFR is adequate

2) GLP-1

56
Q

Biguanides* (1)

A

Metformin (Glucophage)

57
Q

Medication-Induced Hyperglycemia

A 
Thiazide diuretics 
Protease inhibitors 
Atypical antipsychotics 
Glucocorticoids 
Calcineurin inhibitors 
Nicotinic acid 
Oral Contraceptives 
Phenytoin
58
Q

Biguanides Contraindications*

Impairments (2)

Contraindications (4)

A

Renal Impairment*
Hepatic Impairment = may decrease ability to eliminate lactic acid*

Hypoxic states
Acute or chronic alcohol abuse
Elderly
CHF on drug therapy

59
Q

Long Acting Insulin (5)

A 
Insulin Glargine (Lantus) 100n/mL
Insulin Glargine (Basaglar) 100u/mL
Insulin Glargine (Toujeo) 300u/mL
Insuline Detemir (Levemir) 
Insulin Degludec (Tresiba)
60
Q

DPP-4 Inhibitors

Administration

A

Once daily oral admin

Adjustment necessary for pts with renal dysfunction

61
Q

Combination Products* (3)

A 
Novolin or Humulin 70/30
     - NPH 70% Regular 30%
Novolog 70/50
     - Aspart protamine 70% Aspart 30%
Humalog 50/50  75/25
     - Lispro protamine 50% 75% Lispro 50% 25%
62
Q

Adverse Effects of Insulin*

Hypoglycemia*  
Signs of autonomic \_\_\_\_\_\_
     - Sympathetic (4)
     - Parasympathetic (2) 
     - May progress to (2) if untreated
A

Hyperactivity

 - Tachycardia, Palpitations, Sweating, Tremulousness
 - Nausea, Hunger 
 - Seizures, Coma
63
Q

SGLT 2 Inhibitors*

Potential Advantages (4)*

A

Weight Loss (75g urine glucose = 300kcal/day)
Decrease risk of hypoglycemia
Lowers BP
Renal Protection

64
Q

Liothyronine* T3 Cytomel*

Higher incidence of?
Why is not really used?

A

Cardiac events
Difficulty monitoring w conventional lab tests
$$

65
Q

Biguanides*

Caution with: *

Advantages (3)

AE(2)

A

Iodinated Contrast*

No hypoglycemia when used as monotherapy
Weight loss
Decrease triglycerides

N/V/D
Metallic taste

66
Q

Insuline Detemir

Onset
Peak
Duration
Appearance

A

2 hr
3-9 hr
14-24 hr
Clear

67
Q

SGLT2 Inhibitors (3)*

A

Canagliflozin (Invokana)
Dapagliflozin (Farxiga)
Empagliflozin (Jardiance)

68
Q

Pharmacologic Agents (10)

A 
Insulin 
Sulfonylureas
Meglitinides 
Biguanides 
a Glucosidase Inhibitors 
Thiazolidinediones 
GLP-1 Agonists 
DDP 4 Inhibitors 
SGLT 2 Inhibitors 
Amylin Agonists
69
Q

SGLT- The Bad

May 2016: All
June 2016: Canagliflozin
June 2016: Canag and Dapag
November 2016: All

A

Increased risk for DKA
Boxed warning for leg/foot amputations
Increased risk for acute kidney injury
Increased risk for bone loss

70
Q

Animal Insulin (2)

Human Insulin is produced through

Insulin is a ____ hormone that cannot be given ___

Circulating insulin has half life of only a few ___ dt rapid removal by (2)

A

Beef, Pork

Recombinant DNA Techniques

Peptide, PO

Minutes, Liver and Kidneys

71
Q

GLP 1 CV Safety

A

WE literally just wanted to prove it didn’t have cardiotoxic effects (thia)

But we found the opposite happened, not even just safety but they improved CV risk!

72
Q

Thyroid Hormones

A

T3 Triiodothyronine

T4 Thyroxine

73
Q

DPP Inhibitors*

MOA

A

Inhibits DPP-4 enzyme that is responsible for the breakdown on incretin hormones GLP-1

74
Q

Insulin Glargine

Onset
Peak
Duration
Appearance

A

4-5 hr
No peak
22-24 hr
Clear

75
Q

Tx of Adrenal Insufficiency

For Adrenal Crisis, Addisonian Crisis what do you use?

____ protein bound

Formulations (3)

A

Parenteral glucocorticoids

Highly

Oral: exhibits 100% absorption
IV: succinate
IM: acetate

76
Q

DM Complications

A 
Blindness
Heart Attack 
Kidney Failure 
Stroke 
Dental Problems 
Amputation 
Pregnancy Complication 
Nerve Damage 
Sexual Dysfunction 
Insulin Injection
77
Q

Insulin

A

Secreted by B cells

Promote uptake utilization and storage of glucose -> lowers plasma glucose concentration

78
Q

Glyburide (3)*

Duration
Active Metabolite
Elimination

A

Diabeta, Glynase, Prestab

12-24 hrs
Inactive
50% Hepatic/50% Renal (the only one w renal excretion)

79
Q

DM Type I

A

IDDM

  • results from B cell destruction
  • ABSOLUTE lack of insulin
80
Q

What is an essential component of both T3 and T4

A

Iodine

81
Q

SGLT 2 Inhibitors*

Concerns

A 
Limp amputation
Electrolyte disturbances
Decreased BP 
Bacterial urinary infections 
Fungal genital infections 
Malignancy
82
Q

Causes/Diagnosis of Hyperthyroidism (3)

T4 concentrations
TSH concentrations

A

Graves Disease
Thyroid stimulating antibodies
Meds (Amiodarone)

Elevated total and free T4
Suppressed TSH

83
Q

Empagliflozin (Jardiance)

Dosing 
Administration 
Renal Dose Adjustments 
Cost 
Patient Assistance
A 
10-25mg daily 
In the morning with or without food 
Yes
TBD
TBD
84
Q

Administration*

1)
sites (3)
accelerates absorption (3)
types (3)

2)
What insulins are given by this route (2)

A

1) SubQ
Abdomen, Butt, Arms/Legs
Exercise, Rubbing, Heat
Vial and Syringe, Pens, Pumps

2) IV
Rapid and Short

85
Q

Sulfonylureas*

Metabolism and Excretion

A

Hepatically metabolized
- caution w hepatic impairment

Renally excreted
- Glyburide may accumlate in pts w CrCL < 30ml/min

86
Q

Portable Pen Injectors

A

Vials of insulin + replaceable needles
More accurate dosing mechanisms
Faster and Easier than conventional syringes
Increased patient compliance

87
Q

Incretin Mimetics

A

Food -> GLP 1 ->
Stimulates insulin release
Delays gastric emptying
Suppression of postpradial glucagon release

DPP-4 inhibits GLP 1

88
Q

Thiazolidinediones Contraindication*

A

May cause or exacerbate CHF*
Contraindicated in NYHA Class III or IV HF*
After initiation of dose, observe pts for s/s of HF

89
Q

Pancreatic Hormones (2)

A

Glucagon

Insulin

90
Q

Thioureas*

Well absorbed by the
___ is highly protein bound unlike ___ which is not significantly bound to protein
Both agents have ____ lives, however they
Patient becomes _____ over a 1-2 month period

A

GI
PTU, Methimazole
Short, accumulates in thyroid gland to exert longer effects
Euthyroid

91
Q

Sulfonylureas Adverse Effects*

A

Hypoglycemia (most common)*

Rash, Photosensitivity, Hypersensitivity

N/V, abnormal LFT’s

Weight Gain

92
Q

What drugs to use when compelling need to minimize weight gain or promote weight loss?

A

GLP 1

SGLT 2

93
Q

Secondary causes of DM (4)

A

Pancreatic Disease
Cystic Fibrosis
Endocrinopathies
Drugs and Chemicals

94
Q

Infusion Pump

A

Connected to subc catheter to deliver short acting insulin

Decreases glycemic variability

Does have logistical issues and is more expensive

95
Q

What drugs?

Promotes production of insulin when stimulated by food

Major SE: Pancreatitis

A

Incretins (GLP1 & DPP4 Inhibitors)

96
Q

Sulfonylureas

MOA

Secondary effects (2)

Therapeutic Use:

A

Increase secretion of preformed insulin by B cells by closing K+ channels

Increase insulin receptor sensitivity
Decrease hepatic glucose output

Type 2

97
Q

Biguanides*

MOA
Secondary effects

Therapeutic use

A

Decrease hepatic glucose output
Increases peripheral glucose uptake and utilization

Type 2 DM

98
Q

Thiazolidediones*

MOA + (3)

A

Binds to nuclear steroid hormone receptor and promotes glucose uptake into skeletal, muscle, and adipose tissue

  • Increases insulin sensitivity
  • Decreases insulin resistance
  • NO EFFECT ON INSULIN SECRETION*
99
Q

Iodine-Containing Compounds

MOA

Common Agents (2)

AE

A

Immediately inhibits release of T4 and T3

Lugols solution, Potassium iodide solutions (SSKI)

Rash, metallic taste, sore gums, GI discomfort, hypothyroidism

100
Q

Glimiperide (1)*

Duration
Active Metabolite
Elimination

A

Amaryl

24 hr
Weakly active
100% Hepatic

101
Q

Goals for Glycemic Control

1) A1C
2) Fasting Glucose
3) Peak postprandial glucose (1-2 hrs after meal)

A

1) <6.5-7.0%
2) 80-130
3) <180

102
Q

What drugs? (2)

Closes K+ channels -> insulin release

Major SE
Hypoglycemia, Weight Gain

A

Sulfonylureas

Meglitinides

103
Q

Liotrix (T4:T3 4:1) Thyrolar*

Why is not really used? (2)

A

No advantage over T4 alone

$$$$

104
Q

Drug of choice for thyroid replacement?*

Chemically ____
Expensive?
Free of ______

A

Levothyroxine

Stable
Inexpensive
Antigenicity

105
Q

Combination Products

Advantages

Disadvantages

A

Less injections/day
Less calculations by pt

Dose adjustments alter both products

106
Q

GLP 1 Agonists*

Precautions (2)

A

Not recommended in pts with CrCl <30 mL/min

Should not be used in pts with a personal or family hx of medullary thyroid cancer

107
Q

Synthetic Thyroid Hormones (3)*

A

Levothyroxine (T4, L-thyroxine, Synthroid, Levoxyl)

Liothyronine (T3 (Cytomel))

Liotrix (T4:T3 4:1) (Thyrolar)

108
Q

What drug?

Inhibits glucose reabsorption by kidneys, increase glycosuria

Major SE: Genitourinary infections, polyuria

A

SGLT 2 Inhibitors

109
Q

Meds to treat Hyperthyroidism (4)

A

Thioureas
Iodine-containing compounds
B-adrenergic antagonists
Corticosteroids

110
Q

Technosphere Insulin

Dry ___ of human ___ insulin formulated to absorb onto ____ microparticles for ____ admin

Peak ~ ___ min

Metabolism similar to ____ insulin

Administered when?

Black Box Warning:

A

First inhaled product the “Dreamboat”

Powder, rDNA, Technosphere, pulmonary

15

Regular human

Before or within 20 min of starting

Bronchoconstriction
NO USE w COPD, Asthma
Not recommended for patients who smoke

111
Q

Insulin Administration

A

SQ or IV

112
Q

What drug?

Decreases gluconeogenesis
Increases glyolysis

Major SE: Lactic acidosis, GI symptoms

A

Metformin

113
Q

What drugs to use when cost is a major issue?

A

SU

TZD

114
Q

DPP-4 Inhibitors

FDA Warning 2015

A

Severe Joint Pain

115
Q

Therapeutic Uses of Insulin

1) Type 1
2) Type 2
3) DM of ______

A

1) Therapy of choice
2) For those who cannot control with diet, exercise, oral meds OR newly diagnosed presenting with severe, symptomatic hyperglycemia
3) Pregnancy

116
Q

Sulfonylureas (3)*

2nd gen

A

Glyburide (Diabeta, Glynase, Prestab)

Glipizide (Glucotrol, Glucotrol XL)

Glimepiride (Amaryl)

117
Q

Tx of Hypoglycemia*

1) Mild Hypoglycemia + Conscious, Able to Swallow
2) Severe Hypoglycemia + Unconscious/Stupor

A

1) Simple sugar, glucose
(juice, hard candy, sugar packets/glucose gel, tablets)

2) 20-50ml Dextrose 50% IV or 1mg Glucagon SQ/IM

118
Q

GLP 1 Agonists*

How is it administered?
How often?

A

Pre-filled pens for subcutaneous injection

Once or twice daily to once weekly

119
Q

SGLT 2 Inhibitors

Drug interactions

A

No major interactions

120
Q

Rapid Acting Insulin

Onset
Peak
Duration 
Administered
Ideally added to \_\_\_ insulin regimen 
May be given 
Appearance
A 
15-30 min
1-2 hr
3-4 hr 
Immediately before a meal*
Basal 
IV 
Clear
121
Q

____ channels determine resting membrane potential in __ cells

Glucose enters B cells via a membrane transporter __-__

KATP are blocked causing membrane _____ and opens ____ channels

Ca2+ signals ____ secretion

A

ATP Sensitive K+ (KATP)
B

Glut-2

Depolarization, Ca2+

Insulin

122
Q

SGLT 2 Inhibitors*

MOA

A

Inhibits sodium glucose transporter 2 in the proximal renal tubules -> reduces reabsorption of filtered glucose and increased urinary excretion of glucose

Thereby reducing plasma glucose concentrations

123
Q

Corticosteroids

MOA (2)

A

Decreases thyroid action

Suppresses immune response in Grave’s

124
Q

Insulin Dosing Pearls*

1 unit of insulin decreases blood glucose by:

Start ___ then ___ to meet nutritional needs

Wait ___ before adjusting dose

Insulin should never be stopped in:

A

50mg/dL (30-100)

low, increase

24 hrs

Type 1*

125
Q

The Role of the Adrenal Glands

3

A

Responsible for regulating stress response through synthesis of

1) Glucorticoids (cortisol)
2) Mineralcorticoids (Aldosterone)
3) Adrenal Androgens

126
Q

Non-Glycemic Goals

1) BP
2) LDL
3) Triglycerides

A

1) <130/80
2) <100, <70 CV disease
3) <150

127
Q

Rapid/Short Acting Uses (2)

A

Mealtime

Elevated Glucose

Advanced Pharmacology (14 decks)

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