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Pharmacology > Endocrine Pharmacology > Flashcards

Endocrine Pharmacology Flashcards

1
Q

Levothyroxine

A

Synthetic T4 that is converted to T3 by 5’ deiodinase in peripheral tissue. T3 and to a smaller degree T4 ten bind to thyroid hormone nuclear receptors in target cells to exert their effects

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2
Q

Indications for levothyroxine

A

Hypothyroidism

Myxedema coma

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3
Q

MOA levothyroxine

A

Isomer of thyroid hormone T4, which like it is converted to T3 by 5’deiodinase. T3 binds thyroid hormone nuclear receptor which results in brain maturation, bone growth, beta adrenergic effects and increased basal metabolic rate

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4
Q

T3 has higher potency

A

10x higher

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5
Q

Side effects levothyroxine

A

Hyperthyroid symptoms

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6
Q

What are some hyperthyroid symptoms

A

Tachycardia, heat intolerance, tremors, arrhythmias

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7
Q

PTU (propylthiouracil)/methimazole

A

Used in patients with hyperthyroidism

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8
Q

MOA PTU /M

A

Block action of thyroid peroxidase, thus inhibiting thyroid hormone synthesis. Additionally PTU has peripheral activity blocking conversion of T4 to the more active T3

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9
Q

Side effects PTU/M

A

Agranulocytosis and skin rash

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10
Q

Additional side effects of PTU

A

Hepatotoxicity

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11
Q

Additional side effects methimazole

A

Teratogen

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12
Q

Indications for PTU/M

A

Hyperthyroidism

Bc inhibit thyroid hormone synthesis, helping to alleviate symptoms in patients

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13
Q

MOA PTU/M

A

Inhibits thyroid peroxidase which aids in oxidation of iodide. This interrupts the organification of iodine, which leads to inhibition of thyroid hormone synthesis

PTU blocks peripheral conversion of T4 to T3-alleviates symptoms of hyperthyroidism

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14
Q

Pride effects PTU/M

A

Agranulocytosis, skin rash, hepatotoxicity(PTU), teratogen (M)

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15
Q

Teratogen of M

A

Aphasia cutis, which is a congenital focal absence of epidermis. Preg should be on PTU and not M espicially in first trimester

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16
Q

Insulin

A

Analogs of human hormone
Short duration
Intermediate duration
Long duration

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17
Q

Rapid activating insulin’s

A

For meals eaten at same time of injection
10-30 minute onset
1-3 hours peak
3-6 hour duration

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18
Q

Examples of rapid acting insulting

A

Lispro (humalog)
Aspart (novolog)
Glulisine (apidra)

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19
Q

Insulin lispro

A

Rapid acing analog of regular insulin

Before or after eating

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20
Q

Aspart

A

Analog of human insulin with a rapid onset

5-10 min before meals

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21
Q

Glulisine

A

Synthetic analog of natural human insulin

Administered close to time of eating

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22
Q

Short acting insulin

A

Within 30-60 minutes as the onset of action is 30-60
2-4 hours peak
Duration 6-10 hours

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23
Q

Example of short acting insulin

A

Regular insulting (humulin R)

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24
Q

Regular insulin (humulin R)

A

Unmodified human insulin

Before meals to control postprandial hyperglycemia or infused subQ to provide basal glycemic control.

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25
Q

Immediate acting insulin

A

Half the day or overnight often combined with rapid or short acting insulin. Onset 1-2 hours peak 4-12 hours duration 15-24 hours

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26
Q

Example of intermediate acting insulin

A

Isophane NPH (humulin N)

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27
Q

Isophane humulin N

A

Intermediate acting bc onset of action is delayed and duration is longer. Therefore this insulin type cant be administered at mealtime to control postprandial hyperglycemia, but instead is used to provide glycemic control between meals and during the night

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28
Q

Long acting insulin

A

full day
Combined when needed with rapid or short acting insulin
Onset 1 hour
No peak

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29
Q

Example of long lasting insulin

A

Detemir (levemir)

Glargine (lantus)

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30
Q

Detemir (levemir)

A

Long acting for basal control.
Canc ause weight gain or hypoglycemia more than intermediate acting NPH.

Do not mix and indicated onyl as subcutaneous injection

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31
Q

Glargine (lantus)

A

Once a day to mimic the basal rate of insulin normally in body
Indicated only as subcutaneous injection and not mixed (like detemir)

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32
Q

Metformin

A

Biguanide class of diabetic drugs. First line fo diabetes II and can also be used for PCOS

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33
Q

Side effects metformin

A

Lactic acidosis, GI distress

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34
Q

Who should not take metformin

A

Patients with renal failure

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35
Q

Indications for metformin

A

TIID

PCOS

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36
Q

Why metformin first line for DMII

A

Does not cause hypoglycemia inline othr drugs

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37
Q

PCOS metformin

A

Promote ovulation since insulin resistance may contribute to inhibition of normal ovulation. Can also assist with weight loss

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38
Q

MOA metformin

A

Unknown but decreases gluconeogenesis and increases insulin sensitivity

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39
Q

Side effects metformin

A

Lactic acidosis, GI distress (diarrhea nausea vomiting)

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40
Q

Contradiction to metformin

A

Renal failure

Creatinine greater than 1.5 mg/dL no no

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41
Q

Chlorpropamide and tolbutamide (or Incase 1st generation sulfonylureas)

A

Promote insulin release. Increasingcirculating insulin to maintain normal blood glucose levels int he body

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42
Q

Indications for chlorpropamide and tolbutamide

A

TIID who have the ability to produce insulin.

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43
Q

Why are first generation sulfonylureas rarely used

A

Lower potency and significant drug drug interactions

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44
Q

Side effects chlorpropamide and tolbutamide

A

Hypoglycemia and CV toxicity

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45
Q

Who should not take chlorpropamide and tolbutamide

A

Pregnant, breastfeeding, consuming alcohol, or taking beta blockers

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46
Q

MOA first generation sulfonylureas

A

Oral hypoglycemic rarely usedstimulate pancreatic islet cells to release insulin. Bind to ATP sensitive k channels and cause depolarization of the cell membrane. ca enters the cells while insulin is released into the blood stream

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47
Q

Indications 1st generation sulfonylureas

A

TIID

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48
Q

Side effects 1st generation sulfylureas

A

Hypoglycemia and possible cardiovascular toxicity

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49
Q

Hypoglycemia and sulfonylureas

A

Increase insulin release and may cause hypoglycemia .

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50
Q

Since these drugs are metabolized int he liver and excreted by the kidneys , dysfunction in either organs may cause drug toxicity and fatal hypoglycemia

A

Ok

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51
Q

1st gen sulfylurease cardiotixicity

A

Sudden cardiac deathmainly tolbutamide

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52
Q

Why no put someone on 1st gen suldyluearse on beta blocker

A

Reduces effects due to insulin suppression

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53
Q

Why avoid 1st gen sulfyurease in preg and breast feeding

A

Teratogen is and should be avoided during preg
Newborn severe hypoglycemia lasting 10 days.
Is in breast milk

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54
Q

Why avoid alcohol with 1st gen sulfyureasel drugs

A

Combo causes disulfiram-like reaction manifesting with flushing, palpitations, and nausea. Alcohol also potentials the hypoglycemic effects of the sulfonylurea medications

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55
Q

Gluburide and glipizide (2nd generation sulfonylureas)

A

Stimulate the release of insulin from pancreatic islet to increase the amount of circulating insulin to maintain blood glucose

56
Q

Indication for 2nd generation sulfyonlureas

A

TIID who can produce insulin

Replace 1st gen due to their increased potency and fewer sided drug drug interactions

57
Q

Side affect 2nd gen

A

Hypoglycemia

58
Q

Who should not take 2nd gen

A

Alcohol

Also not breastfeeding (except glyburide

59
Q

MOA 2nd gen

A

Replace 1st
Lower dose than 1
Clocks K channels in beta cells
Depolarizers cells..ca influx and insulin out!

60
Q

Indications 2nd gen

A

TIID

With some pancreatic function

61
Q

Side effects 2nd gen

A

Hypoglycemia

62
Q

What patients on 2nd gen are more susceptible to hypoglycemia

A

Hepatitis or renal failure

63
Q

2nd get are __ potent that 1st gen

A

More

Need lower dose

64
Q

Why avoid beta blockers on 2nd gen

A

Can mask hypoglycemia

Also decrease the effect by suppressing the release of insulin

65
Q

Why avoid alcohol with 2nd gen

A

Potentials hypoglycemia effects

66
Q

Why avoid 2ng gen in breastfeeding

A

Hypoglycemia in new Borns lasting 10 days

67
Q

How treat diabetic breast feeders

A

Insulin

68
Q

Pioglitazone (thiazolidonediones)

A

Stimulates receptors inthe body to increase cellular responses to insulin, thus decreasing insulin resistance.

69
Q

Pioglitazone is only effective int he presence of ___ and can only be used to treat ___

A

Insulin

TIID

70
Q

Side effects pioglitazone

A

Upper respiratory infections, muscle pain, sinusitis, headache, and heart failure, increased risk for bladder cancer, women taking this are more prone to bone fractures

71
Q

Why should liver enzymes be checked whole on pioglitazone

A

Liver toxicity risk

72
Q

Suffix for pioglitazone

A

Glitazones

Also referred to as TZds

73
Q

MOA thiasolidinedioners

A

Bind and stimulate peroxisome proliferator-activated receptor gamma (PPAR gamma), a nuclear cel transcription regulator that increases cellular response to insulin, espicially in peripheral tissues. This decreases insulin resistance in TIID

74
Q

Indications for thiazolidinediones

A

TIID

It increases uptake of glucose by skeletal muscle and fat cells, thus lowering blood sugar

75
Q

IDE effects pioglitasone

A 
Weight gain 
Heart failure 
Myalgia
Hypoglycemia
URI
76
Q

Considerations on pioglitazone

A

Risk of bladder cancer if high dose
(Pain urinating sign)
Increase risk of fracture in women (do weight bearing exercises and take VD)
Monitor liver enzymes almost taken off market due to hepatic toxicity

77
Q

Acarbose (precose) and miglitol (glyset) (alpha glucosidase inhibitors )

A

Control blood glucose by inhibiting an intestinal enzyme that converts complex carb into digestible forms so that decrease the rate of carb digestion and absorption and decrease rise of glucose after eating

78
Q

Indications for alpha glucoidase inhibitors

A

TIID

79
Q

Side effects alpha glucosidase inhibitors

A

Flatulence, cramps, diarrhea, and anemia..also may cause liver damage so do liver function test

80
Q

MOA alpha glucosidase inhibitors

A

Alpha glucosidase breaks down oligosaccharides and complex carbohydrates into digestible monosaccharides. Inhibit it.
Does not rely on presence of insulin

81
Q

Indication for acarbose and miglitol

A

TIID uncontrolled by diet and exercise

Can be given alone of with insulin and metformin

82
Q

Side effects acarbose and miglitol

A

Flatulence, diarrhea, anemia, cramps

83
Q

Anemia and acarbose and miglitol

A

Decrease SI ability to absorb iron

84
Q

Consideration acarbose and miglitol

A

Monitor Liver function test (AST, ALT)

85
Q

Why give oral glucose for hypoglycemia on alpha glucosidase inhibitors and not sucrose

A

Alpha glucosidase inhibitors interfere with sucrose hydrolysis and delta its effects

86
Q

Repaglinide and nateglinide (meglitinides)

A

Oral hypoglycemic medications classified as gliniders

87
Q

MOA glinides

A

Stimulate the pancreatic cells to release more insulin, decreasing blood glucose levels

88
Q

Side effects meglitinides

A

Hypoglycemia

89
Q

Why eat meglitinides within 30 min or administration

A

Short half life

90
Q

Gemfibrozil (lopid) if taken with (meglitinides)

A

A cholesterol med

Decreases the metabolism rate of meglitinides and should not be administered to prevent drug accumulation leading to hypoglycemia

91
Q

MOA meglitinides

A

Bind ATP dependent k channels on pancreatic beta cells to result in increase insulin increase by calcium influx

92
Q

Indication meglitinides

A

TIID who have decreased circulating insulin

Alone or in combo with metformin or glitazone

93
Q

Side effects meglitinides

A

Hypoglycemia

94
Q

Considerations meglitinides

A

Eat within 30 minutes
Glemfibrosil increases risk of hypoglycemia(a cholesterol medication which inhibits the metabolism of meglitinides and causes drug accumulation in blood)
Horn half life

95
Q

Sitagliptin (januvia and saxagliptin (onglyza) (DDP-4 inhibitors)

A

Antidiabetic meds that work by blocking DDP-4 enzyme, wallowing for increasedaction of incretin hormones and increased release of insulin

96
Q

DPP-4 inhibitors are only effective in the presence of ___ and can only be taken by patients with ___

A

Insulin

TIID

97
Q

Indication for DPP-4 inhibitors

A

Third line med for the treatment of diabetes and should only be used if first and second line medications have failed to provide adequate blood glucose control.

98
Q

Side effects DPP-4 inhibitors

A

URI, pancreatitis, hypersensitivity reactions

99
Q

Suffix DPP4 inhibitors

A

Gliptin

100
Q

MOA DPP-4 inhibitors

A

DPP4 inactivated incretin hormones so when blocked, the action of incretin is increased, releasing insulin

101
Q

Indications for DPP-4 inhibitors

A

TIID with insulin presence

Third line meds used in conjunction with diet and exercise

102
Q

Side effects DPP4 inhibitors

A

Pancreatitis, RURI and inflammation, SJS

103
Q

Consideration DPP4 inhibitors

A

3rd line if 1st and 2nd line fail

104
Q

Pramlintide (symlin)

A

Injectable hypoglycemic drug indicated for type 1 and 2 diabetes. It is a synthetic amylin analog

105
Q

MOA pramlintide (symlin)

A

Supplement mealtime insulin to maintain glucose despite insulin therapy

106
Q

Side effects pramlintide

A

Nausea and reactions at injection site also monitor for hypoglycemia

107
Q

Why avoid pramlintide with other drugs

A

It delay the absorption of other meds

108
Q

MOA pramlintide

A

Synthetic amylin analog mimics amylin. Amylin decreases postprandial levels of glucose by delaying gastric emptying and suppressing glucagon secretion. Also helps decrease caloric intake by increasing the sense of satiety

109
Q

Indications pramlintide

A

Type I and II diabetes

110
Q

How should we use pramlintide

A

Supplement at mealtime with insulin in patients who are unable to achieve glucose control despite optimal insulin therapy

It decreases postprandial glucose levels and minimized glucose fluctuations also decreases amount of mealtime insulin needed

111
Q

Side effects pramlintide

A

Nausea skin reactions at injection site (itching redness swelling)

112
Q

Considerations pramlintide

A

Hypoglycemia when combined with insulin -alone it does not cause hypoglycemia so decrease insulin dose

Causes delayed absorption of other drugs since it delays gastric emptying
Give other drugs at least one hour before take it

113
Q

Exenatide (byetta)

A

Injectable hypoglycemic drug indicated for patients with TIID

114
Q

MOA exenatide (byetta)

A

Incretin mimetic and GLP-1 synthetic analog

115
Q

Side effects exenatide (byetta)

A

Hypoglycemia, nausea, vomiting, diarrhea, pancreatitis, and renal failure

116
Q

Since exenatide delays gastric emptying it should be administer when

A

At least one hour after giving other medications.

117
Q

How is exenatide used

A

Adjunct therapy and administered with othe antidiabetic drugs

118
Q

MOA exenatide

A

Incretin mimetic that increases release from pancreatic beta cells
GLP-1 synthetic analog mimicking action of incretin.

119
Q

Describe incretin

A

Released from GI tract cells after meal and activate GLP1 receptors which slow gastric emptying, stimulate glucose dependent release of insulin, inhibit postprandial release of glucagon, and suppress appetite

120
Q

How do stitagliptin boost incretin

A

Preventing breakdown of the hormone

121
Q

Indications exenatide

A

TIID as adjunctive therapy to other antidiabetic meds such as metformin or sulfonylurea
Also used with lifestyle change

122
Q

Side effects exenatide

A

Hypoglycemia, nausea and vomiting, diarrhea, thyroid cancer, pancreatitis, renal failure

123
Q

Who should not take exenatide

A

History of pancreatitis

Severe renal impairment

124
Q

Consideration exenatide

A

Give one hour after other meds and use in adjunct

125
Q

Glucagon (GlucaGen)

A

Polypeptide hormone that causes the hepatic conversion of stored glycogen into readily available glucose.

126
Q

Indications for glucagon (glucaGen)

A

Hypoglycemia caused by insulin overdose and not related to starvation

127
Q

When is glucagon given

A

When IV glucose not available

128
Q

Side effects glucagon (GlucaGen)

A

Nausea and vomiting

129
Q

What do you do when patient is conscious after given glucagon

A

Oral carbs within an hour to avoid rebound hypoglycemia. If not improvement give 50% glucose

130
Q

MOA glucagon made by the alpha cells of the pancreas, glucagon increases the amount of circulating glucose readily available for use.

A

Yup

131
Q

What is glycogen

A

Form of glucose stored int he liver that converts to glucose when necessary
It promotes glycogenolysis or the hepatic conversion of stored glycogen into glucose for blood stream

132
Q

What does glucagon inhibit

A

Glycolysis(conversion of glucose to glycogen)

133
Q

Indications for glucagon

A

Hypoglycemic emergency

Treat immediately to prevent brain damage, coma, and death

134
Q

Who is glucagon not indicated for

A

Hypoglycemia from starvation due to lack of glycogen stores

135
Q

Side effects glucagon

A

Nausea and vomiting

136
Q

Considerations glucagon

A

Reconstitute powder
Consume oral carbs after regain consciousness
50% dextrose IV if o effect

Pharmacology (52 decks)

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