Endocrine Flashcards
How does hyper vs. hypothyroidism affect insulin? What consideration is needed for patients with these conditions?
- Hypothyroidism: delays insulin breakdown; patients will require less insulin units
- Hyperthyroidism: increased metabolism and renal clearance; requiring more insulin than baseline
What is the goal A1C for nonpregnant adults? How often is the A1C drawn?
- 7%
- Every 6 months for those who are compliant, every 3 months for those who are not
What are the pharmacodynamics of insulin? (5)
- Stimulates glucose entry into cells
- Increases storage of glucose as glycogen in muscle and liver cells
- Inhibits glucose production in liver and muscle cells
- Promotes protein synthesis by increasing amino acid transport into cells
- Enhances fat storage and prevents mobilization of fat for energy
There are several different forumulations of insulin, what are the onset, peak and duration of rapid acting & short acting insulins?
When should you instruct your patient to take their dose of short acting insulin?
*NOTE: clarifying this info as different times were presented in lecture vs. asynch. Info included is from asynch
- Rapid acting
- Onset 15 min
- Peak 30-90 min
- Duration 5 hours
- Short acting
- Onset 30 min
- Peak 2 hours
- Duration 3-7 hours
- Take 30 minutes before mealtime
There are several different forumulations of insulin, what are the onset, peak and duration of intermediate, long acting and ultra-long acting insulins?
*NOTE: clarifying this info as different times were presented in lecture vs. asynch. Info included is from asynch
- Intermediate: NPH insulin
- Onset 1-1.5 hours
- Peak 4-12 hours
- Duration 10-16 hours
- Long acting: Detemir, glargine
- Onset 3-6 hours
- Peak none
- Duration 20-24
- Ultra-long-acting: Degludec
- Onset 1 hour
- Peak none
- Duration 42 hour
What are some items of caution/contraindication related to insulin? (3)
- Careful monitoring of glucose in patients with: hepatic dysfunction, renal impairment, pregnancy, hypo or hyper thyroid
- Pregnancy/lactation: rapid or short acting approved - first line in pregnancy
- Peds: approved
What medication can mask symptoms of hypoglycemia and should be used in caution with most medications for diabetic patients?
Beta-blockers
Glucagon
Indication & Pharmacodynamics
Indication: hypoglycemic episode
Pharmacodynamics: accelerates liver glycogenolysis - results in increased breakdown of glycogen to glucose and inhibition of glycogen synthesis to increase blood glucose levels
Glucagon
Caution/contraindications: contraindication, when to avoid & Adverse fx (3)
- Caution/contraindications
- Contraindication: hypersensitivity to glucagon or lactose
- Avoid: insulinoma or pheochromocytoma
- Adverse fx: nausea, hypertension, hypersensitivity reaction
Biguanides: Metformin (Glucophage)
Indication & Pharmacodynamics
Indication: first-line diabetes management in patients older than 10
Pharmacodynamics: increases peripheral glucose uptake and utilization; decreases hepatic glucose production and intestinal absorption of glucose
Which anti-diabetic medications do NOT cause hypoglycemia alone? (4)
- Metformin
- Thiazolidinediones
- Alpha-glucosidase inhibitors
- Selective sodium-glucose cotransporter 2 inhibitors (SGLT-2)
Which anti-diabetic medications are considered insulin secretagogues? (2)
- Sulfonylureas
- Meglitinides
Biguanides: Metformin (Glucophage)
Effects on blood glucose levels & weight
- lowers postprandial and basal glucose levels
- Considered weight neutral
Biguanides: Metformin (Glucophage)
Caution/contraindications: avoid, caution, other considerations, pregnnacy, peds, monitoring
- Avoid: eGFR less than 30, liver disease
- Caution: eGFR 30-45, B12 anemia/deficiency
- Other considerations: Hold 48 hours before and after radiologic studies with contrast
- Pregnancy - may be considered; lactation: compatible
- Peds: 10+
- Monitoring: renal function, ketones, A1C
Biguanides: Metformin (Glucophage)
Adverse fx (6)
When do the GI ADRs tend to resolve?
- diarrhea
- bloating
- nausea
- flatulence
- HA
- vit B12 deficiency
GI issues usually resolved within 2 weeks after starting dose
Biguanides: Metformin (Glucophage)
Black box warning - how can you educate your patient to avoid this issue?
- Black box warning: lactic acidosis - death, hypothermia, hypertension and resistance of bradyarrythmias
- Education
- Encourage keeping well hydrated
- Alcohol potentiates drug’s effect on lactate metabolism
Thiazolidinediones (TZDs)
Pioglitazone (Actos), rosiglitazone (avandia)
Pharmacodynamics
Pharmacodynamics: enhances insulin sensitivity by improving insulin action in the cell; increases utilization of insulin by liver and muscle cells; decreases hepatic glucose production
Thiazolidinediones (TZDs)
Pioglitazone (Actos), rosiglitazone (avandia)
Caution/contraindications: avoid, other considerations, pregnancy, peds, interactions, monitoring
- Avoid: NYHA class III & IV HF; ALT levels greater than 2.5 times above NL; active or hx of bladder cancer
- Other considerations: Increased risk for bone fractures
- Pregnancy/lactation: avoid
- Peds: 18+ ok
- Interactions: drugs metabolized by the CYP450 system; coricidin, corticosteroids, ketoconazole
- Monitoring: liver enzymes, A1C
Thiazolidinediones (TZDs)
Pioglitazone (Actos), rosiglitazone (avandia)
Adverse fx (6)
- fluid retention
- wt gain
- HA
- myalgia
- HTN
- URI
Sulfonylureas
Glipizide, glyburide, glimepiride
Pharmacodynamics
Pharmacodynamics: cause an increase in endogenous insulin secretion by the beta cells of the pancreas; reduces glucose release from the liver; potentiate the fx of ADH
Sulfonylureas
Glipizide, glyburide, glimepiride
Which of these need to be taken on an empty stomach vs. with food?
- Glipizide needs to be taken on an empty stomach
- others need to be taken with food
Sulfonylureas
Glipizide, glyburide, glimepiride
Caution/contraindications: avoid, caution, pregnancy, peds, interaction, monitoring
- Avoid: elderly, sulfa allergies, G6PD deficiency
- Caution: renal and hepatic impairment
- Pregnancy/lactation: avoid; but d/c 2-4 weeks before expected delivery date if using
- Peds: 18+ ok; 10-18 years - unlabeled recommendation
- Interaction: sulfonamides, thiazide diuretics; insulin can only be combined with glimepiride
- Monitoring: A1C, CBC
Sulfonylureas
Glipizide, glyburide, glimepiride
Adverse fx (12)
- hypoglycemia
- wt gain
- nausea
- epigastric fullness
- heartburn, rashes
- pruritis
- urticaria
- agranulocytosis
- SIADH
- hemolytic anemia
- leukopenia
- thrombocytopenia
Meglitinides
repaglinide (prandin), nateglinide (Starlix)
Pharmacodynamics
Which blood glucose levels does this medication effect? When does it need to be taken?
- Pharmacodynamics: block ATP-dependent potassium channels, depolarizing the membrane and facilitating calcium entry through calcium channels; increased calcium stimulates insulin release from pancreatic beta cells
- Reduce postprandial blood glucose levels
- Needs to be taken with a meal (30 min before)
Meglitinides
repaglinide (prandin), nateglinide (Starlix)
Caution/contraindications: avoid, caution, pregnancy, peds, interactions, monitoring
- Avoid: elderly
- Caution: renal and hepatic impairment
- Pregnancy/lactation: avoid
- Peds: 18+ ok
- Interactions: CYP450 inducers; antifungals, antimicrobials
- Monitoring: A1C
Meglitinides
repaglinide (prandin), nateglinide (Starlix)
Adverse fx (6)
- hypoglycemia
- wt gain
- HA
- diarrhea
- arthralgias
- chest or back pain
Alpha-glucosidase inhibitors
Acarbose, miglitol
Pharmacodynamics
Which blood glucose levels are affected? When should it be taken?
How much can this medication lower A1C?
- Pharmacodynamics: competitively inhibits absorption of complex carbohydrates from small bowel; delays carbohydrate digestion
- Best for post-prandial elevation, should be taken with the first bite of food
- Lower A1c by 1%, improve high triglycerides
Alpha-glucosidase inhibitors
Acarbose, miglitol
Caution/contraindications: avoid, caution, pregnancy, peds
- Avoid: bowel diseases, predisposition to intestinal obstruction
- Caution: renal and hepatic impairment
- Pregnancy/lactation: avoid
- Peds: avoid
Alpha-glucosidase inhibitors
Acarbose, miglitol
In a hypoglycemic episode, what should be used for management?
Hypoglycemia would be treated with milk as plain sucrose would not be well absorbed
Alpha-glucosidase inhibitors
Acarbose, miglitol
Adverse fx (4)
- flatulence
- diarrhea
- abdominal pain
- elevated serum transaminases
Selective sodium-glucose cotransporter 2 inhibitors (SGLT-2)
-flozins (canaglifozin, dapagliflozin)
Indications & Pharmacodynamics
Indication: first choice to add if A1C not at goal with metformin
Pharmacodynamics: inhibit renal SGLT-2 in the proximal tubule, blocking reabsorption of glucose in kidneys, increasing urinary glucose excretion and reduction of plasma glucose
Selective sodium-glucose cotransporter 2 inhibitors (SGLT-2)
-flozins (canaglifozin, dapagliflozin)
How much do these drugs reduce A1C?
What other diseases can it help reduce the risk for?
- Reduce A1C by 1%
- Reduce ACSVD risk, HF, and CKD progression
Selective sodium-glucose cotransporter 2 inhibitors (SGLT-2)
-flozins (canaglifozin, dapagliflozin)
Caution/contraindications: black box warning, avoid, other considerations, pregnancy, peds, monitoring
- Black box warning: risk of Fournier’s gangrene (from GU infection)
- Avoid: eGFR less than 30
- Other considerations: Increased risk for bone fractures; Canagliflozin: increased risk of amputation
- Pregnancy/lactation: avoid
- Peds: limited data
- Monitor: GU infections, sores on the lower limbs, new pain or tenderness
Selective sodium-glucose cotransporter 2 inhibitors (SGLT-2)
-flozins (canaglifozin, dapagliflozin)
Adverse fx (7)
- hyperkalemia
- GU fungal infections
- UTI
- renal insufficiency
- urinary frequency
- hypotension
- urticaria
Dipeptidyl Peptidase-4 (DPP-4) inhibitors
-gliptins
Pharmacodynamics
Pharmacodynamics: inhibit DPP-4 enzyme that inactivates GLP-1 and GIP hormones (incretin), which are hormones that increase insulin synthesis and release from pancreatic beta cells, decrease glucagon secretion from pancreatic alpha cells
Dipeptidyl Peptidase-4 (DPP-4) inhibitors
-gliptins
How much can this medication reduce A1C?
Which blood sugar levels does it impact?
- Lower A1C by 1%
- Impact pre and postprandial blood glucose levels
Dipeptidyl Peptidase-4 (DPP-4) inhibitors
-gliptins
Caution/contraindications: caution, pregnancy, peds, interaction, monitoring
- Caution: renal impairment (except for linagliptin)
- Pregnancy/lactation: Avoid
- Peds: limited data
- Interaction: ACE inhibitors
- Monitoring: renal function; A1C
Dipeptidyl Peptidase-4 (DPP-4) inhibitors
-gliptins
Adverse fx (4)
- hypersensitivity reactions
- acute pancreatitis
- arthralgias
- hypoglycemia
Glucagon-like Peptide 1 (GLP-1) Receptor agonists
-tides (exenatide, liraglutide)
Pharmacodynamics
Pharmacodynamics: analog of the incretin hormone GLP-1 (normally increases glucose-dependent insulin secretion, decreases inappropriate glucagon secretion, and slows gastric emptying)
Glucagon-like Peptide 1 (GLP-1) Receptor agonists
-tides (exenatide, liraglutide)
How much can this medication lower A1C?
Which blood sugar levels are impacted?
- Lower A1C by 2%
- Impacts pre and post prandial blood glucose
Glucagon-like Peptide 1 (GLP-1) Receptor agonists
-tides (exenatide, liraglutide)
Caution/contraindications: avoid, black box warning, pregnancy, peds, interactions
- Avoid: moderate to end stage renal disease, severe GI disease
- Black box warning: risk of thyroid c-cell tumors
- Pregnancy/lactation: limited data
- Peds: limited data
- Interactions: increased INR with warfarin, digoxin
Glucagon-like Peptide 1 (GLP-1) Receptor agonists
-tides (exenatide, liraglutide)
Adverse fx (6)
- nausea
- vomiting
- diarrhea
- injection site reaction
- HA
- pancreatitis
Thyroid agents
Levothyroxine (synthroid)
Indication & Pharmacodynamics
When should this medication be administered?
- Indication: Hypothyroidism; TSH greater than 10 or between 5-10 with goiter or positive antithyroid peroxidase antibodies
- Pharmacodynamics: synthetic form of T4. Normally converted to active metabolite T3, then able to bind to thyroid receptor proteins in the nucleus and exert metabolic fx through control of DNA transcription and protein synthesis
- Admin on an empty stomach 30 min prior to a meal
Thyroid agents
Levothyroxine (synthroid)
Caution/contraindications: monitoring, avoid, caution, pregnancy, peds
- Monitoring: check TSH levels 6-8 weeks after initiating treatment; goal TSH 0.3-3.0
- Avoid: recent MI
- Caution: cardiovascular disease, adrenal insufficiency
- Pregnancy/lactation: OK
- Peds: OK
Thyroid agents
Levothyroxine (synthroid)
Adverse fx (7)
- decreased bone mineral density with long term therapy
- increased HR
- increased BP
- anxiety
- nervousness
- insomnia
- weight loss
Antithyroid agents
Methimazole (Tapazole) & Propylthiouracil (PTU)
Indication & Pharmacodynamics
Indication: Hyperthyroidism
Pharmacodynamics: inhibits synthesis of thyroid hormones by blocking oxidation of iodine in the thyroid gland; does not inactivate circulating thyroid hormones
Antithyroid agents
Methimazole (Tapazole) & Propylthiouracil (PTU)
Caution/contraindications: peds, drug interactions, monitoring
Which medication can be used during the first vs. 2nd/3rd trimesters of pregnancy?
Note: black box warning related to PTU
- Pregnancy: PTU during first trimester, Methimazole for 2nd and 3rd; lactation: lowest dose
- Peds: OK
- Drug interactions: caution with meds that can suppress bone marrow, lithium, warfarin, OTC cold meds
- Monitoring: thyroid studies, CBC, liver/renal panels
- PTU specific black box warning: hepatotoxicity
Antithyroid agents
Methimazole (Tapazole) & Propylthiouracil (PTU)
Adverse fx (8)
- drowsiness
- HA
- arthralgia
- skin rash
- urticaria
- fever
- agranulocytosis
- hepatitis