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ENDOCRINE

-For endocrine drugs you must understand normal endocrine physiology. (Refer to lecture slides about Hormone Secretion and
Feedback) Continue to refer back to the normal physiology images and see where the drugs’ mechanisms interact.

INSULIN
-Pharmacodynamics:
- Liver: Promotes storage of glucose  GLYCOGEN (carbohydrate polymer)
- Muscle Tissue: Promotes protein synthesis (anabolic effect)
- Adipose Tissue (Fat Cells): Promotes storage of free fatty acids (decrease fatty acid content in blood and puts it into adipose cells)
- Other Cells: promotes uptake of glucose from the blood (to be used as energy…Glycolysis/Citric Acid Cycle  ATP)
NOTE:
-alcohol use can increase hypoglycemia risk (especially important in patients that are on insulin therapy)
-Use of beta-blockers will mask symptoms of hypoglycemia. Profuse SWEATING will be the only indication of hypoglycemia
-HYPOTHYROIDISM: give these patients less dosage of insulin because it delays insulin breakdown
-HYPERTHYROIDISM: Increases renal clearance so - requiring more insulin

CLINICAL SXS:
-Hyperglycemia: Extreme thirst, frequent urination, dry skin, hunger, blurred vision, drowsiness, nausea
-Hypoglycemia: Shaking, sweating, anxious, dizziness, hunger, fast heartbeat, impaired vision, weakness/fatigue, headache, irritable
INSULIN
DRUG TRADE NAME MECHANISM OF ACTION USE ADVERSE EFFECT DRUG-DRUG
& INTERACTIONS
CONTRAINDICATIONS
INSULIN
Insulin Humalog, -synthetic exogenous insulin -Diabetes Type 1 -Hypoglycemia, INCREASED hypoglycemic
Novolin or -Diabetes Type 2 diabetic ketoacidosis, effect of insulin:
(Safe in pregnancy) Lantus -NOTE: use insulin c-peptide -Diabetic Somogyi Effect, ----anabolic steroids,
levels to distinguish Ketoacidosis (DKA) Hypersensitivity Rxns, salicylates, ETOH, Sulfa
exogenous insulin from Lipodystorphy, insulin drugs, ACE-Is,
endogenous hormone resistance Propranolol, MAO-Is
production
Contraindicated: DECREASED
-Children w/ closed hypoglycemic effect of
epiphyses (i.e. growth insulin:
plates if treating ----Corticosteroids,
growth failure Sympathomimetic drugs,
-Cancer patients INH, Thyroid hormones,
-Diabetics Niacin, Diuretics

PLEASE use the tables from lectures regarding short vs regular vs long-acting insulin. IT IS IMPORTANT TO KNOW the times it takes the different
insulin types to take effects and how long those effects last.
OTHER DIABETTIC AGENTS
Note: Most of them are oral administrations but some are not (pay attention!!!)
DRUG TRADE NAME MECHANISM OF ACTION USE ADVERSE EFFECT DRUG-DRUG
& CONTRAINDICATIONS INTERACTIONS

BIGUANIDES #1 drug of choice BI GOLLY KIDNEY


-Monitoring: Assess renal function, ketones, HbA1C before starting dosing (check every 6 months)
-Does NOT cause Hypoglycemia…metallic taste
Metformin Glucophage -↓production of glucose -Osteoperosis: -Metabolic Acidosis, gas, -Iodine-based contrast
(glucophage) by liver -1st line for post- dyspepsia, diarrhea, mediums used for
(Pregnancy -↓GI glucose menopausal female stomach pain, nausea, GI- imaging (ask patient to
Category B) absorption(the more -1st line for men > changes withhold metformin use
glucose absorbed, the 70 y/o 48hrs prior to elected
NOTE: inhibits more in the blood) -Careful use with elderly imaging procedures)
platelet -improves insulin (due to decline in renal
aggregation and sensitivity by ↑ function) -
reduces blood peripheral glucose
viscosity; favorable uptake and utilization Contraindications:
effects on lipids -DOES NOT STIMULATE -Renal or hepatic disease
Food decreases an INSULIN RELEASE FOR or major dysfunction
delays absorption BETA CELLS
-excreted by kidney -favorable effect on lipids - ETOH potentiates drugs
- GREAT FOR PCOS- - pts lose weight effect on lactate
DECREASE INSULIN metabolism
RESISTANCE. - watch patients anemia
offer b12 supplement
SULFONYLUREAS
: HbA1C (baseline, Q 3 months until proper dosage found, Q 6 months after that)
Monitor CBC and LFTs too-
Glipizide Glucotrol -↑ endogenous insulin -Diabetes Mellitus (DM -risk of HYPOGLYCEMIA -Cross-sensitivity with
(Pregnancy release from pancreatic Type II) -GI, dermatological rash, sulfonamides or thiazide
Category C) β-cells (patients must -Neurogenic Diabetes SIADH, hemolytic diuretics
Glyburide Diabeta have pancreatic Insipidus anemia, leukopenia,
(Pregnancy endocrine function) thrombocytopenia,
Category B) - METABOLIZED IN LIVER,
Glimepiride Amaryl -EXCRETED IN URINE arthralgias, myalgias, and
(Pregnancy AND FECES angioedema
Category C) -weight gain,
ANGIODEMA, PAIN IN
MUSCLES AND JOINTS
-ACE INHIB
-POTENTIATE EFFECTS
OF ANTIDIURETICS
α-GLUCOSIDASE INHIBITORS

Acarbose-CHECK Precose - ↓ the rate of -Adjunct (not -GI sxs (eg. Flatulence), -Sulfonylureas & Insulin
LIVER FUNCTION carbohydrate monotherapy) for DM DIARRHEAH, ABD PAIN, (increased risk of
- degradation and Type II hypoglycemia risk hypoglycemia)
CABUSE TOOT absorption through -METABOLIZED BY
FLATOOTLANCE enzyme inhibition in the INTESTINAL BACTERIA Contraindications: -Digoxin (Acarbose)
(Category B) small intestines  AND DIGESTIVE -pts with inflammatory -Propranolol, ranitidine
Miglitol Glyset lowers peak glucose ENZYME(FLATULANCE) bowel disease (IBD), bowel (Miglitol)
after meals (controls -EXCRETED BY KIDNEY obstruction, or renal
postprandial glucose problems, ULCERTIVE
levels) COLITIS
-Pregnancy (despite being
HYPOGLYCEMIA IS category B)
TREATED WITH -PDO NOT USE IN Pediatrics
DEXTROSE NOT population
SUCROSE

TAKEN TID WITH FIRST


BITE OF MEAL
THIAZOLIDINEDIONES- GLITZI MEDS- 2 SISTERS ROSI AND PIO
(-glitazones)
Pregnancy Category C
-Monitor Liver Enzymes, HbA1C
Pioglitazone Actos -Fluid overload (edema)
Rosiglitazone Avandia -improving sensitivity to -adjunct or -URI, headach, Sinusitis, -Oral Contraceptives-
insulin in muscle and monotherapy for DM back pain, fatigue and REQUIRE HIGHER
adipose tissue and Type II myalgia DOSAGES
inhibiting hepatic -Risk of bladder cancer -Coricidin, steroids,
gluconeogenesis  -METABOLIZED- LIVER (pioglitazone) ketoconazole( DRUGS
makes the body more -EXCRETE- URINE AND DRUGS METABOLIZED
sensitive to insulin FECES AS METABOLITES -Contraindications: BY CYP 3A4
--Chronic Liver
Disease(HEAVY LIVER
PROCESSING) PRECAUTION
WI PTS WITH ELEVATED
LIVER ENZYMES
--Fluid Retention (CHF
patients) EXACERBATES HF
--NOT APPROVED FOR
Pediatric population UNDER
18
MEGLITINIDES
(-glinides)
Pregnancy Category C
-Get baseline HbA1C (recheck Q 3months) and LFTs
Nateglinide Starlix -increase release of -DM Type II -Hypoglycemia IN -CYP3A4 and 2C9
insulin from pancreatic - METABOLIZED: IN VULNERABLE POP inducers  increase
Repaglinide Prandin β-cells (close K+ LIVER- meglitinide metabolism
-POSTPANDRIAL channelsinflux of - EXCRETED- FECES -Contraindications: -ketoconazole
HYPERGLYCELMIA Ca2+insulin release) --Liver Disease/Failure -erythromycin
- --Pediatric patients
-TIME IN PLASMA IS
SHORT…ONLY LOWER
POST PRANDIAL BG
LEVELS
INCRETINS- LIPTIN
Monitor Renal Function and Thyroid Function
DDP-4 Inhibitors
(-gliptins) MONITOR LFT BASELINE AND ANNULALLY AND HBA1C Q 3MO
Sitagliptin Januvia -inhibit DPP-4 -DM Type II -Mild Weight loss -Sulfonylurea
(Category B) (NOTE: DPP-4 breaks -WELL TILERATED BY -GI symptoms- BAD AT FIRST (hypoglycemia)
down GLP-1)  ELDERLY headache, pancreatitis
Saxagliptin Onglyza increases GLP-1 in -EXPENSIVE (rare), hypoglycemia (when -ACE-I (increased risk of
(Category B) plasma mixed with sulfonylureas) angioedema)

-NOTE: GLP-1 targets Contraindications: - MONITOR FOR


pancreas and ↑ insulin -Renal Dysfunction THYROID
and ↓ glucagon release; -Pediatric patients MEDULLARY
GLP-1 also decrease liver -Pancreatitis CANCER
glucose production -Previous thyroid nodules ESPECIALLY
THOSE WITH
PREVIIOUS
NODULES!
GLP-1 Receptor Agonists
(-glutides)
Pregnancy Category C
Dulaglutide- LA Trulicity -GLP-1 agnoists (mimics -DM Type II ONLY -Hypoglycemia -↑ INR if used with
natural incretins) COBINE WITH -Acute Pancreatitis warfarin (exenatide-
Exenatide-LA BYdureon -Promote release of METFORMN, -GI: nausea, vomiting, BYETTA)
EXENATIDE- SA BYETTA insulin from pancreas (β- SULFONULUREAS AND diarrhea—SUBSIDE IN TIME
Liraglutide-LA Saxenda cells) DURING INCREASE OTHERS
GLUCOSE - NATURALLY OCCURS Contraindications:
Albiglutide-LA Tanzeum -MIMIC INCRETINS IN BODY -Severe GI disease (colitis,
-Slow glucose absorption - NAUSE LESS IF THEY Crohn’s)
Lixisentatide-SA Lyxumia from gut + delays gastric GIVE DAILY -Renal Impairment/Failure-
emptying + promotes - KNOW LIVER FUNCTION
satiety LIRAGLUTIDE(VICTOZA)- BEFORE
TREAT OBESITY- FOOD -PREGNANT
60 MIN BEFORE BIG INTAKE AND WEIGHT
MEALS LOSS -SITE REACTION
DOSE 6 HRS APART
-MAJOR EPISOES OF
HYPOGLYCEMIA—SERIOUS
ADVERSE EFFECT.
SELECTIVE SODIUM GLUCOSE CO-TRANSPORTER 2 INHIBITORS
“SGLT-2 Inhibitors”
(-gliflozins)
Pregnancy Category C
Canagliflozin Inkovana- -Promotes loss of -DM Type II (only) as an -Genital fungal infection and -Multiple
DAILY BEFORE glucose in urine by adjunct to diet and Dehydration (educate
1ST MEAL blocking reabsorption in exercise (weight loss) patient to drink plenty of
Dapagliflozin Farxiga- ONCE the kidneys water)
DAILY WITH OR -ALWAYS CHECK -UTIs (cystitis,
WITHOUT EXPENSIVE pyelonephritis, prostatitis,
FOOD SAME urethritis, etc.)
TIME -Bladder cancer
Empagliflozin Jardiance -Increase in LDL
DAILY SAME -Allergic Reactions
TIME -Balantis
AMYLIN AGONIST- TYPE1 AND 2
Pregnancy Category C
Pramlintide (SQ) Symlin -Mimic natural amylin  INJECTABLE ONLY IN -Hypoglycemia (w/ poor
slows gastric emptying ABD THIGH SQ compliance)
-suppresses glucagon -BLACK BOX WARNING
secretion -METABOLIZED IN WHEN USED WITH INSULIN
-Increases satiety KIDNEY -
-suppresses postprandial -Modest weight loss
glucose rise - EXCRETED IN FECES (improved HbA1C)
-Gastroparesis
GLUCAGON
VERY IMPORTANT to monitor BG levels before and after injecting
Glucagon -Stimulates hepatic -Reversal of -Nausea, vomiting -Increases
(Pregnancy gluconeogenesis and hypoglycemia -Allergic Reactions anticoagulant effects of
Category B) glycogenolysis  raises -Prevent log sugars for oral anticoagulants
blood glucose levels colonoscopy after 3-day Contraindications: (OACs)
-Very fast acting preparations -Pheochromocytoma -
-BG RISE WITHUN 10IN -Insulinoma PHEOCHROMOCYTOMA
-CAN USE IN PREG -INSULINOMS
-CAN USENIN KIDS