MIDTERM 03 - Endocrine System Flashcards by Juan Carlos Cornelio

Target tissue is pituitary (Gland)

Hypothalamus

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Secretes releasing hormones (e.g., TRH, CRH, GnRH, GHRH) (Gland)

Hypothalamus

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Secretes GH, ACTH, TSH, LH, FSH, PRL/ADH, Oxytocin (Gland)

Pituitary (anterior/posterior)

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Multiple targets (Gland)

Pituitary (anterior/posterior)

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Secretes T3, T4, calcitonin (Gland)

Thyroid

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Targets are metabolism and bone (Gland)

Thyroid

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Secretes PTH (Gland)

Parathyroid

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Target tissues are bone and kidneys (Gland)

Parathyroid

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Secretes cortisol, aldosterone, adrenaline, and noradrenaline (Gland)

Adrenal (cortex/medulla)

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Target is whole body (Gland)

Adrenal (cortex/medulla)

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Secretes insulin, glucagon, and somatostatin (Gland)

Pancreas (Islets of Langerhans)

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Target tissues are liver, muscle, and adipose (Gland)

Pancreas (Islets of Langerhans)

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Secretes testosterone, estrogen, and progesterone (Gland)

Gonads (testes, ovaries)

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Targets reproductive organs (Gland)

Gonads (testes, ovaries)

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Secretes melatonin (Gland)

Pineal gland

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Targets CNS (circadian rhythm) (Gland)

Pineal gland

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Most hormones operate through __________ feedback loops

Negative

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HPA (ACTH → cortisol), HPT (TSH → T3/T4), HPG (LH/FSH → sex steroids) are part of the __________

Hypothalamic-pituitary axis

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cAMP (e.g., TSH, LH), IP3/DAG (e.g., GnRH), tyrosine kinase (e.g.,
insulin) are __________

Second messengers

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Autoimmune destruction of pancreatic β-cells → absolute insulin deficiency (Types of DM)

Type 1 DM

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Young age (<30 years), rapid onset (Types of DM)

Type 1 DM

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Treatment is insulin only (Types of DM)

Type 1 DM

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Insulin resistance + relative insulin deficiency (Types of DM)

Type 2 DM

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Older age, gradual onset (Types of DM)

Type 2 DM

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Treatment is oral antidiabetic drugs and insulin (Types of DM)

Type 2 DM

__________ is a peptide hormone; it is degraded in the GI tract so it must be injected

Insulin

Only regular insulin can be given __________; especially in DKA or hyperkalemia

Lispro, Aspart, and Glulisine are preferred for __________

Post-prandial glucose control

Glargine and Determir are used for __________, minimal peak

Basal control

__________ can be mixed with regular or rapid-acting insulin

NPH

__________ or __________ should NOT be mixed with other insulins (GD)

Glargine, Detemir

Lispro, Aspart, Glulisine (Types of insulin)

Rapid-acting

Regular insulin (Types of insulin)

Short-acting

NPH (Types of insulin)

Intermediate

Glargine, Determir (Types of insulin)

Long-acting

Degludec (Types of insulin)

Ultra-long

Onset: 10-20 min; peak: 1-3 hr; duration; 3-5 hr (Types of insulin)

Rapid-acting

Onset: 30-60 min; peak: 2-4 hr; duration: 5-8 hr (Types of insulin)

Short-acting

Onset: 1-2 hr; peak: 4-12 hr; duration: 12-18 hr (Types of insulin)

Intermediate

Onset: 1-2 hr; no peak; duration: ~24 hr (Types of insulin)

Long-acting

Onset: ~1 hr; flat peak; duration: >42 hr (Types of insulin)

Ultra-long

Inject right before meals (Types of insulin)

Rapid-acting

Only insulin used IV in emergencies (Types of insulin)

Short-acting

Cloudy; often BID (Types of insulin)

Intermediate

Basal insulin (Types of insulin)

Long-acting

Flexible dosing; lowest hypoglycemia risk (Types of insulin)

Ultra-long

Includes metformin (Pharmacotherapy for DM)

Biguanides

First line for T2DM unless contraindicated (Pharmacotherapy for DM)

Biguanides

In liver and muscle cells, metformin inhibits __________; which increases AMP: ATP ratio and activates AMPK

Mitochondrial respiratory chain complex I

↓ Hepatic gluconeogenesis = __________ fasting glucose (Action of AMPK)

↓

↑ Insulin receptor activity = __________ glucose uptake in muscle (Action of AMPK)

↑

↑ GLUT4 translocation = __________ glucose entry into cells (Action of AMPK)

↑

↓ Lipogenesis, ↑ fatty acid oxidation = __________ metabolic profile (Action of AMPK)

↑

↓ Gluconeogenesis (main effect) → ↓ hepatic glucose output (Tissue target of biguanides)

Liver

↑ Insulin sensitivity → more glucose uptake via GLUT4 transporters (Tissue target of biguanides)

Muscle

↓ Lipolysis, ↓ inflammation (Tissue target of biguanides)

Adipose

↓ Glucose absorption, alters microbiome (Tissue target of biguanides)

Gut

↓ Insulin resistance → ↓ androgen production (Tissue target of biguanides)

Ovary (in PCOS)

__________ is freely filtered by the glomerulus

Glucose

Glucose is reabsorbed by ___________ (90%) and __________ (10%)

SGLT2, SGLT1

Glucose is filtered by the glomerulus and reabsorbed in proximal tubule by __________

SGLT

Includes empagliflozin and dapagliflozin (Pharmacotherapy for DM)

SGLT2 inhibitors ("-gliflozins")

__________ and __________ are specifically endorsed in patients with cardiovascular disease, heart failure, and chronic kidney disease (CKD) (SGLT2 inhibitors) (ED)

Empagliflozin, Dapagliflozin

Works even in late-stage T2DM (Features of SGLT2 inhibitors)

Insulin-dependent

None when used alone (Features of SGLT2 inhibitors)

Hypoglycemia risk

↓ (~2–3 kg) (Features of SGLT2 inhibitors)

Weight

↓ (~4 mmHg systolic) (Features of SGLT2 inhibitors)

Empagliflozin, dapagliflozin approved for HF and CKD (Features of SGLT2 inhibitors)

CV protection

Renal function, signs of UTI/general infections, ketones in DKA risk patients (Features of SGLT2 inhibitors)

Monitoring

Stay hydrated, monitor for genital irritation/infection, temporarily stop during acute illness (Sick day rule) (Features of SGLT2 inhibitors)

Patient advice

__________ is secreted from intestinal L-cells in response to food

Glucagon-like peptide-1 (GLP-1)

Mimic endogenous GLP-1 but are resistant to DPP-4 degradation (Pharmacotherapy of DM)

GLP-1 receptor agonists ("-glutides")

Decreases appetite and promote weight loss (Pharmacotherapy of DM)

GLP-1 receptor agonists ("-glutides")

__________ and __________ are recommended when weight loss is a goal, patient has CVD or high risk, and preferred over sulfonylureas for CV protection (GLP-1 receptor agonists) (SD)

Semaglutide, Dulaglutide

Brand names - Saxenda/Victoza (GLP-1 receptor agonists)

Liraglutide

Brand name - Trulicity (GLP-1 receptor agonists)

Dulaglutide

Brand names - Ozempic (inj), Rybelsus (oral) (GLP-1 receptor agonists)

Semaglutide

Brand names - Byetta (BID) / Bydureon (weekly) (GLP-1 receptor agonists)

Exenatide

Dosing is daily; also approved for weight loss (GLP-1 receptor agonists)

Liraglutide

Dosing is weekly; once-weekly pen, popular for convenience (GLP-1 receptor agonists)

Dulaglutide

Dosing is weekly (inj) and daily (oral); strongest glucose + weight loss effect (GLP-1 receptor agonists)

Semaglutide

Less commonly used (GLP-1 receptor agonists)

Exenatide

Most common; start low and go slow (GLP-1 receptor agonist SEs) (NV)

Nausea, Vomiting

Transient; improves over weeks (GLP-1 receptor agonist SEs)

Diarrhea

Caution in gastroparesis (GLP-1 receptor agonist SEs)

Delayed gastric emptying

Contraindicated if history of pancreatitis (GLP-1 receptor agonist SEs)

Pancreatitis (rare)

Avoid in patients with MEN2 or medullary thyroid cancer (esp. semaglutide/liraglutide) (GLP-1 receptor agonist SEs)

Thyroid C-cell tumors in rodents

Mild, transient (GLP-1 receptor agonist SEs)

Injection site reactions

__________ enzyme rapidly degrades GLP-1 and GIP (incretins)

Dipeptidylpeptidase (DPP-4)

Inhibits DDP-4 and prolongs GLP-1 and GIP activity (Pharmacotherapy for DM)

DDP-4 inhibitors ("-gliptins")

__________ and __________ are still used in Australia but have weaker evidence for CV benefit (DPP-4 inhibitors) (SL)

Sitagliptin, Linagliptin

Often used as a step-up therapy or when GLP-1 or SGLT2i are contraindicated (Pharmacotherapy for DM)

DPP-4 inhibitors ("-gliptins")

↑ (glucose-dependent) (DDP-4 inhibitor effects)

Insulin secretion

Minimal unless used with insulin/SU (DDP-4 inhibitor effects)

Hypoglycemia risk

Neutral (DDP-4 inhibitor effects)

Weight

Adjust except linagliptin (DDP-4 inhibitor effects)

Renal function

Neutral or slightly negative (saxagliptin) (DDP-4 inhibitor effects)

CV effects

Rare; caution if history (DDP-4 inhibitor effects)

Pancreatitis risk

Works by enhancing insulin secretion from pancreatic beta cells (Pharmacotherapy for DM)

Sulfonylureas ("gli-")

__________ is the most commonly used sulfonylurea; preferred over glibenclamide due to lower hypoglycemia risk (Sulfonylureas)

Gliclazide

Still used, but no longer first-line unless cost is a factor (Pharmacotherapy for DM)

Sulfonylureas ("gli-")

Diamicron; shorter-acting (Sulfonylureas)

Gliclazide

Diamicron MR; modified-release (Sulfonylureas)

Gliclazide MR

Amaryl; long-acting (Sulfonylureas)

Glimepiride

Not routinely used; long half-life (Sulfonylureas)

Glibenclamide (glyburide)

Preferred due to lower hypoglycemia risk (Sulfonylureas)

Gliclazide

Commonly prescribed once daily (Sulfonylureas)

Gliclazide MR

Lower hypoglycemia risk than glibenclamide (Sulfonylureas)

Glimepiride

Higher risk of hypoglycemia; not preferred in elderly (Sulfonylureas)

Glibenclamide (glyburide)

Activates PPARγ nuclear receptor which regulates genes for glucose and lipid metabolism (Pharmacotherapy for DM)

Thazolidinediones (Pioglitazone)

Still available, but used rarely; often added to metformin or DPP-4i (Pharmacotherapy for DM)

Thiazolidinediones (Pioglitazone)

Used with caution due to fluid retention, fracture risk, and bladder cancer warning (Pharmacotherapy for DM)

Thiazolidinediones (Pioglitazone)

Delayed onset; contraindicated in NYHA class III-IV (Pharmacotherapy for DM)

Thiazolidinediones (Pioglitazone)

Metformin (DM drug class)

Biguanide

Empagliflozin (DM drug class)

SGLT2 inhibitors

Semaglutide (DM drug class)

GLP-1 receptor agonist

Sitagliptin (DM drug class)

DPP-4 inhibitor

Gliclazide (DM drug class)

Sulfonylurea

Pioglitazone (DM drug class)

Thiazolidinedione

↓ hepatic gluconeogenesis (DM drug class)

Biguanide

↑ urinary glucose excretion (DM drug class)

SGLT2 inhibitor

↑ insulin, ↓ glucagon, delays gastric emptying (DM drug class)

GLP-1 receptor agonist

↑ endogenous GLP-1 (DM drug class)

DPP-4 inhibitor

↑ insulin release from β-cells (DM drug class)

Sulfonylurea

↑ insulin sensitivity via PPARγ (DM drug class)

Thiazolidinedione

Weight neutral, CV benefit (DM drug class)

Biguanide

CV, renal benefit, weight loss (DM drug class)

SGLT2 inhibitor

Weight loss, CV benefit (DM drug class)

GLP-1 receptor agonist

Weight neutral (DM drug class)

DDP-4 inhibitor

Cheap, effective (DM drug class)

Sulfonylurea

Durable effect (DM drug class)

Thiazolidinedione

GI upset, avoid if eGFR <30 (DM drug class)

Biguanide

Risk of UTI, euglycemic DKA (DM drug class)

SGLT2 inhibitor

GI upset, avoid in thyroid cancer (DM drug class)

GLP-1 receptor agonist

Rare pancreatitis (DM drug class)

DDP-4 inhibitor

Hypoglycemia, weight gain (DM drug class)

Sulfonylurea

Fluid retention, fractures (DM drug class)

Thiazolidinedione

↓ hepatic glucose production (DM drug class)

Biguanide

Renal glucose reabsorption (DM drug class)

SGLT2 inhibitor

Incretin system (DM drug class)

GLP-1 receptor agonists

Incretin degradation (DM drug class)

DDP-4 inhibitor

Insulin secretion (DM drug class)

Sulfonylureas

Insulin resistance (DM drug class)

Thiazolidinedione

Carb digestion (DM drug class)

Alpha-glucosidase inhibitors (rare in AU)

Inhibits hepatic gluconeogenesis; ↑ insulin sensitivity (DM drug class)

Biguanide

Blocks SGLT2 in proximal tubule → ↑ urinary glucose excretion (DM drug class)

SGLT2 inhibitor

↑ insulin, ↓ glucagon, ↓ gastric emptying, ↑ satiety (DM drug class)

GLP-1 receptor agonist

Inhibit DPP-4 enzyme → ↑ endogenous GLP-1/GIP (DM drug class)

DDP-4 inhibitor

Close ATP-sensitive K+ channels → depolarization → ↑ insulin (DM drug class)

Sulfonylurea

Activate PPARγ → ↑ insulin sensitivity (DM drug class)

Thiazolidinedione

Delay intestinal carbohydrate absorption (DM drug class)

Alpha-glucosidase inhibitors (rare in AU)

SOA is liver, muscle (DM drug class)

Biguanide

SOA is kidneys (DM drug class)

SGLT2 inhibitors

SOA is pancreas, brain, gut (DM drug class)

GLP-1 receptor agonists

SOA is pancreas, gut (DM drug class)

DPP-4 inhibitors

SOA is pancreatic beta cells (DM drug class)

Sulfonylureas

SOA is muscle, fat, liver (DM drug class)

Thiazolidinediones

SOA is intestine (DM drug class)

Alpha-glucosidase inhibitors (rare in AU)

Includes repaglinide and nateglinide (Pharmacotherapy for DM)

Meglitinides

Stimulate insulin secretion by binding to SUR1 (Pharmacotherapy for DM)

Meglitinides

Rapid onset, short duration; limited efficacy; outdated (Pharmacotherapy for DM)

Meglitinides

MIDTERM 03 - Endocrine System Flashcards

(161 cards)