lOMoARcPSD|37761543
Endocrine Pharmacology
ADVANCED PHARMACOLOGY (Columbia University in the City of New York)
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lOMoARcPSD|37761543
DIABETES: INSULIN
Drug
Insulin lispro
(Humalog)
Rapid Acting
Insulin
Insulin aspart
(NovaLog)
Insulin glulisine
(Aventis)
Short Acting
Insulin
Intermediate
Acting
Regular Insulin
(Humulin R,
Novolin R)
NPH
(Humulin N,
Novolin N)
Timing
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Onset​: 15 - 30
mins
Peak​: 1 - 2 hours
Duration​: 3 - 4
hours
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Onset​: 30 mins
Peak​: 2 - 3 hours
Duration​: 4- 6
hours
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Onset​: 2 - 4 hrs
Peak​: 4 - 8 hrs
Duration​: 8- 12
hrs
Pharmacodynamics
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Long-Duration
Insulin
Insulin
glargine
(Lantus)
●
●
●
Onset​: 4 - 5 hrs
Peak​: none
Duration​: 22-24
hrs
Insulin
detemir
(Levemir)
●
●
●
Onset​: 2 hrs
Peak​: 3 - 9 hrs
Duration​: 14 - 24
hrs
●
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Analog of human insulin
Administered ​immediately before​ eating a meal
○ Ideally added to basal insulin regimen
Route: May be given IV
Appearance​: Clear
Administered ​30-45 minutes before​ meals
○ Requires meal time schedule planning
Route: May be given IV
Appearance​: Clear
Administered once or twice daily
○ Provides basal coverage for the entire day
Route: SubQ injection
○ NOT for emergency IV use
Appearance​: Cloudy
○ Only ​insulin that can be mixed with short-acting
Administered once daily
○ Provides basal coverage for the entire day
Route: SubQ injection
○ NOT for IV use
Appearance​: Clear
○ Can NOT be mixed with other types of insulin
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lOMoARcPSD|37761543
ORAL T2D DIABETIC DRUGS
Drug Class
Drug Names
Glyburide
Sulfonylureas
Glipizide
Glimepiride
Repaglinide
Pharmacodynamics
MOA:​ increases secretion of insulin from β cells
Adverse Effects / Safety
AE:
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Metabolism​:
● Hepatically metabolized
● Renally excreted
○ *Glyburide accumulates in patients
with CrCl <30 mL/min
MOA:​ increases secretion of insulin from β cells
Biguanides
Metformin
(Glucophage)
●
●
Hypoglycemia
Weight gain
●
NVD; metallic taste
●
AE:
Meglitinides
Nateglinide
●
●
Hypoglycemia
Skin - rash, photosensitivity,
hypersensitivity
GI - NVD, abnormal liver function
tests
Weight gain
Cardiotoxicity
Advantages​: rapid onset and short duration
● Preferred for busy meal skippers
● Can be used in patients w/ renal insufficiency
MOA:​ decreases hepatic glucose output and
increases glucose uptake in the periphery
AE:
Advantages:​ NO hypoglycemia
● Weight loss
● Decreases TG
Contraindications:
● Renal impairment
○ Specific ​eGFR​ guidelines
● Hepatic impairment
● Lactic acidosis
● Hypoxic states, alcohol abuse,
elderly, CHF
● Caution with ​contrast dye
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lOMoARcPSD|37761543
Thiazolidine
dione
Rosiglitazone
“-glitazones”
Pioglitazone
ɒ-glucosidase
Inhibitors
Acarbose
(Precose)
MOA:​ promotes glucose uptake into tissues
● Increases insulin sensitivity
● Decreases insulin resistance
● No effect on insulin secretion
Canagliflozin
“-flozin”
MOA:
● Act in intestine to delay absorption of Carbs
●
●
MOA:
● Blocks reabsorption of glucose in kidney
which reduces blood glucose levels
○ Resulting in glucosuria
Dapagliflozin
Administration​:
● PO once daily
Empagliflozin
Hepatotoxicity and edema
Fracture risk
Bladder cancer
Contraindications​:
● Exacerbates ​CHF
Miglitol (Glyset)
SGLT-2
Inhibitors
●
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●
Advantages​:
● Cardioprotective
● Weight loss; low risk of hypoglycemia
● Renal protection
● Lowers BP (?)
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Abdominal pain, flatulence,
diarrhea
Acarbose - increased LFT
Concerns:
● Limb amputation
● Electrolyte disturbances
● Decreased BP
● Bacterial UTI
● Fungal genital infections
● Malignancy
lOMoARcPSD|37761543
T2D: Incretin Mimetics
Drug Class
Drugs
Pharmacodynamics
GLP-1 Receptor
Agonists
Exenatide
“-tide”
Liraglutide
MOA:
● Stimulates insulin secretion and suppresses
glucagon
○ Slow gastric emptying/suppresses
appetite
DPP-4 inhibitors
“-gliptins”
Albiglutide
Administration:
● Pre-filled pens for​ subQ​ injection
Dulaglutide
Advantages​:
● Cardioprotective
Sitagliptin
Saxagliptin
Alogliptin
Linagliptin
Amylin Mimetics
Pramlintide
(Symlin)
MOA:
● Inhibits DPP-4 enzyme from breaking down
GLP-1
○ Enhances incretin
○ Stimulates insulin secretion
○ Suppress glucagon
Adverse Effects
AE:
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NV; headache
Pancreatitis
Caution:
● Not recommended if CrCl <30
mL/min
● Not recommended if family
history of thyroid cancer
Generally well-tolerated
AE​:
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Pancreatitis (rare)
Severe joint pain (FDA, 2015)
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Hypoglycemia
Nausea
Injection Site reactions
Administration:
● PO once daily
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Reduces postprandial levels of glucose by
delaying gastric emptying and suppressing
glucagon secretion
subQ injection
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lOMoARcPSD|37761543
THYROID DISORDERS
Hyperthyroidism
●
●
Hyperthyroidism​ - is elevated T3 and free T4 concentrations
Causes​:
○ Graves Disease
○ Thyroid-stimulating antibodies
○ Medication - Amiodarone
Drug
Thioureas
Propylthiouracil
(PTU)
Methimazole
(Tapazole)
Iodine
Containing
Compounds
Beta Adrenergic
Antagonists
Pharmacodynamics
Adverse Events
MOA:​ inhibits iodination of tyrosine and
iodotyrosine coupling
● PTU also inhibits peripheral conversion
of T3/T4
● Does ​not​ reduce already existing T3/T4
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Rash
Fluid retention
Leukopenia​ - decreased WBC
MOA:​ immediately inhibits release of T3/T4
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Rash
Sore gums
Metallic taste
GI discomfort
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Decreased BP
Bradycardia, cardiac arrest
CHF, asthma
●
N/a
EX: Lugol’s Solution
Potassium iodide solutions (SSKI)
MOA:​ decreasing adrenergic stimulation caused
from increased T3
EX: Propranolol
Corticosteroids
MOA:​ decreases thyroid action and immune
response in Grave’s disease
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lOMoARcPSD|37761543
Hypothyroidism
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Hypothyroidism - ​is decreased T3 and free T4 concentrations
Causes​:
○ Hashimoto’s Disease
○ Surgery
○ Medications - RAI, Lithium, Amiodarone
Drug
Natural
Thyroid
Hormones
Drug Names
Pharmacodynamics
●
Animal product that contains
standardized quantity of T3 and T4
Bioavailability is unpredictable
Variable response
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Allergies
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Drug of choice for thyroid
replacement
○ Stable, cheap, no antigenicity
Onset: 2-3 weeks
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HF
Angina
MI
Hyperthyroidism
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Higher incidence of cardiac events
Difficulty monitoring with conventional labs
Expensive
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Not commonly used - no real advantages over Levothyroxine
Expensive
Armour Thyroid
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Synthetic
Thyroid
Hormones
Levothyroxine
“Pro drug”
Liothyronine (Cytomel)
Liotrix
Adverse Events/Safety
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