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Pharmacology > Pancreatic Hormones, Antidiabetic Drugs and Glucagon > Flashcards

Pancreatic Hormones, Antidiabetic Drugs and Glucagon Flashcards

1
Q

Effects of Insulin

A

INCREASE

glucose uptake in muscle and adipose tissues
glycolysis
glycogen synthesis
protein synthesis
uptake of ions (K and PO4)

DECREASE

gluconeogenesis
glucogenolysis
lipolysis
ketogenesis
proteolysis
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2
Q

GLUT Transporters

A

GLUT 1 - all tissues esp red cells and brain

GLUT 2 - pancreas (B cells), liver, kidney, gut

GLUT 3 - placenta, brain, kidney

GLUT 4 - muscle, adipose

GLUT 5 - gut, kidney

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3
Q

RAPID Acting Insulin

A

LAG

Lispro
Aspart
Glulisine

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4
Q

SHORT Acting Insulin

A

Regular Insulin

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5
Q

INTERMEDIATE Acting Insulin

A

NPH

Lente Insulin

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6
Q

LONG ACTING Acting Insulin

A

Glargine
Detemir
Lantus

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7
Q

AMYLIN ANALOG

activates amylin receptors

decrease gastric emptying
decrease postprandial glucagon
increase satiety

also used for TYPE I DM

administered as an injectable preparation (SC) together with insulin to control post prandial glucose

A

AMYLIN ANALOG

Pramlintide

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8
Q

RAPID Acting Insulin

Injected a few mins prior to meals
Preferred insulin for continuous SC infusion devices

A

RAPID Acting Insulin

Lispro
Aspart
Glulisine

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9
Q

SHORT Acting Insulin

Injected more than an hour before meal

A

SHORT Acting Insulin

Regular Insulin

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10
Q

INTERMEDIATE Acting Insulin

Often combined w/ regular and rapid acting insulin

A

INTERMEDIATE Acting Insulin

NPH
Lente Insulin

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11
Q

LONG ACTING Acting Insulin

Called PEAKLESS insulin

A

LONG ACTING Acting Insulin

Glargine
Detemir
Lantus

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12
Q

BILE ACID SEQUESTRANTS

Binds bile acids
Increase GLP-1 secretion

A

BILE ACID SEQUESTRANTS

Colesevelam

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13
Q

GLP 1 AGONIST

(+) GLP 1 receptor –> dec post meal glucose excursions

dec gastric emptying

(-) gastric emptying

(-) glucagon secretion

produces satiety

administered as an injectable preparation (SC - long acting injectables)

A

GLP 1 AGONIST
-TIDE

Exenatide
Liraglutide
Dulaglutide
Semaglutide
Lixisenatide
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14
Q

DDP-IV INHIBITOR

Increase GLP-1 levels by (-) dipeptidyl peptidase IV (DPP IV)

A

DDP-IV INHIBITOR
-LIPTIN

Sitagliptin
Saxagliptin
Linagliptin
Tenelegliptin
Vildagliptin
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15
Q

Side effects of GLP-1 agonists

A

acute pancreatitis
N/V
weight loss
diarrhea

Liraglutide: has possible THYROID ca risk

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16
Q

Side effects of DDP-IV Inhibitor

A

headache

nasopharyngitis

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17
Q

SGLT2 Inhibitors

(-) SGLT2 transporter –> (-) reabsorption of the glucose in the kidneys back to the blood –> excretion of glucose out in the urine

A

SGLT2 Inhibitors

Sergliflozin
Remogliflozin
Dapagliflozin
Empagliflozin
Canagliflozin
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18
Q

Side effects of SGLT2 Inhibitors

A

increased incidence of UTI
weight loss
excessive thirst
strong smell of UTI

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19
Q

SULFONYLUREAS

closes ATP sensitive K channels –> insulin secretion

(-) pancreatic release of glucagon

increase insulin receptor binding

decrease hepatic extraction of insulin

A

SULFONYLUREAS

1st GEN
Chlorpropamide
Tolbutamide
Tolazamide

2nd GEN
Glipizide
Glimepiride
Glyburide
Gliclazide
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20
Q

MEGLITINIDE

closes ATP sensitive K channels –> insulin secretion

LOWEST RISK OF DEVELOPING HYPOGLYCEMIA since they have SHORT DURATION OF ACTION

A

MEGLITINIDE

Repaglinide
Nateglinide
Mitiglinide

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21
Q

Side effects of 1st gen Sulfonylureas

A

hypoglycemia
weight gain
disulfiram like reactions

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22
Q

Side effects of Meglitinide

A

hypoglycemia

weight gain

23
Q

BIGUANIDES

Dec postprandial and fasting glucose levels

Activates AMP stimulated protein kinase – (-) hepatic and renal gluconeogenesis

Stimulates glucose uptake and glycolysis in peripheral tissues

A

BIGUANIDES

Metformin

24
Q

Side effects of Metformin

A

GI disturbance
Lactic Acidosis - esp in renally and hepatically impaired patients
Vitamin B12 malabsorption – megaloblastic anemia
weight loss

does NOT cause hypoglycemia

25
Q

THIAZOLIDINEDIONES

Bind to PPAR-gamma and alpha –> increase tissues sensitivity, increase glucose uptake in muscles and adipose tissue

(-) hepatic gluconeogenesis

decrease fasting and postprandial hyperglycemia

increase FA uptake – increase glucose utilization

A

THIAZOLIDINEDIONES
-GLITAZONE

Pioglitazone
Rosiglitazone
Troglitazone

26
Q

Side effects Thiazolidinediones

fluid retention
bone fractures especially in women
macular edema
CHF

A

Troglitazone - HEPATIC FAILURE

Rosiglitazone and Troglitazone - CHF

Pioglitazone - 63% risk of BLADDER cancer

27
Q

ALPHA GLUCOSIDASE INHIBITORS

(-) intestinal alpha-glucosidase –> dec conversion of starch and disaccharides to monosaccharides –> dec post prandial hyperglycemia

A

ALPHA GLUCOSIDASE INHIBITORS

Acarbose
Miglitol
Voglibose

28
Q

Side effects of alpha glucosidase inhibitors

A

FLATULENCE

Acarbose - hepatotoxic

CI: renal and hepatic impairment and intestinal disorders

29
Q

DOC for OBESE patients

A

Metformin

does NOT cause hypoglycemia

30
Q

In Graves’ disease, the cause of the hyperthyroidism is the production of an antibody that does which of the following?

(A) Activates the pituitary thyrotropin-releasing hormone (TRH) receptor and stimulates TSH release
(B) Activates the thyroid gland TSH receptor and stimulates thyroid hormone synthesis and release
(C) Activates thyroid hormone receptors in peripheral tissues
(D) Binds to thyroid gland thyroglobulin and accelerates its
proteolysis and the release of its supply of T4 and T3
(E) Binds to thyroid-binding globulin (TBG) and displaces bound T4 and T3

A

(B) Activates the thyroid gland TSH receptor and stimulates thyroid hormone synthesis and release

31
Q

Methimazole reduces serum concentration of T3 primarily by which of the following mechanisms?

(A) Accelerating the peripheral metabolism of T3
(B) Inhibiting the proteolysis of thyroid-binding globulin
(C) Inhibiting the secretion of TSH
(D) Inhibiting the uptake of iodide by cells in the thyroid
(E) Preventing the addition of iodine to tyrosine residues on thyroglobulin

A

(E) Preventing the addition of iodine to tyrosine residues on thyroglobulin

32
Q

Though rare, a serious toxicity associated with the thioamides is which of the following?

(A) Agranulocytosis
(B) Lupus erythematosus-like syndrome
(C) Myopathy
(D) Torsades de pointes arrhythmia
(E) Thrombotic thrombocytopenic purpura (TTP)
A

(A) Agranulocytosis

33
Q

A 56-year-old woman presented to the emergency department with tachycardia, shortness of breath, and chest pain.
She had had shortness of breath and diarrhea for the last 2 d and was sweating and anxious. A relative reported that the patient had run out of methimazole 2 weeks earlier.
A TSH measurement revealed a value of <0.01 mIU/L (normal 0.4–4.0 mIU/L). The diagnosis of thyroid storm was made.

Which of the following is a drug that is a useful adjuvant in the treatment of thyroid storm?

(A) Amiodarone
(B) Betamethasone
(C) Epinephrine
(D) Propranolol
(E) Radioactive iodine
A

(D) Propranolol

34
Q

A 65-year-old man with multinodular goiter is scheduled for a near-total thyroidectomy. Which of the following drugs will be administered for 10–14 d before surgery to reduce the vascularity of his thyroid gland?

(A) Levothyroxine
(B) Liothyronine
(C) Lugol’s solution
(D) Prednisone
(E) Radioactive iodine
A

(C) Lugol’s solution

35
Q

Which of the following is a sign or symptom that would
be expected to occur in the event of chronic overdose with exogenous T4?

(A) Bradycardia
(B) Dry, puffy skin
(C) Large tongue and drooping of the eyelids
(D) Lethargy, sleepiness
(E) Weight loss
A

(E) Weight loss

36
Q

When initiating T4 therapy for an elderly patient with longstanding hypothyroidism, it is important to begin with small doses to avoid which of the following?

(A) A flare-up of exophthalmos
(B) Acute renal failure
(C) Hemolysis
(D) Overstimulation of the heart
(E) Seizures
A

(D) Overstimulation of the heart

Administration of regular doses can cause overstimulation of the heart and cardiac collapse

37
Q

A 27-year-old woman underwent near total thyroidectomy. She was started on levothyroxine. What hormone is produced in the peripheral tissues when levothyroxine is administered?

(A) Methimazole
(B) T3
(C) T4
(D) TSH
(E) FSH
A

(B) T3

38
Q

A 62-year-old woman presents with complaints of fatigue, sluggishness, and weight gain. She needs to nap several times a day, which is unusual for her. She has been taking T4 for the past 15 years without significant problems regarding her energy level. Her recent history is significant for diagnosis
of arrhythmia, and she is currently taking an antiarrhythmic drug.

What is the most likely cause of her current condition?

(A) Amiodarone
(B) Lidocaine
(C) Procainamide
(D) Sotalol
(E) Verapamil
A

(A) Amiodarone

Amiodarone is an iodine-containing antiarrhythmic drug
with complex effects on the thyroid gland and thyroid hormones.

One of its actions is to inhibit peripheral conversion of T4 to T3

39
Q

A 25-year-old woman presents with insomnia and fears she may have “something wrong with her heart.” She describes “her heart jumping out of her chest.” She feels healthy otherwise and reports she has lots of energy. Lab tests confirm hyperthyroidism.

Which of the following is a drug that produces a permanent reduction in thyroid activity?

(A) 131I
(B) Methimazole
(C) Propylthiouracil
(D) Thiocyanate (SCN–)
(E) Thyroglobulin
A

(A) 131I

40
Q

A 13-year-old boy with type 1 diabetes is
brought to the hospital complaining of dizziness. Laboratory findings include severe hyperglycemia, ketoacidosis, and a blood pH of 7.15.

Which of the following agents should be administered to achieve rapid control of the severe ketoacidosis in this diabetic boy?

(A) Glyburide
(B) Insulin glargine
(C) NPH insulin suspension
(D) Regular insulin
(E) Tolbutamide
A

(D) Regular insulin

41
Q

A 13-year-old boy with type 1 diabetes is
brought to the hospital complaining of dizziness. Laboratory findings include severe hyperglycemia, ketoacidosis, and a blood pH of 7.15

Which of the following is the most likely complication of insulin therapy in this patient?
(A) Dilutional hyponatremia
(B) Hypoglycemia
(C) Increased bleeding tendency
(D) Pancreatitis
(E) Severe hypertension
A

(B) Hypoglycemia

42
Q

A 24-year-old woman with type 1 diabetes wishes to try tight control of her diabetes to improve her long-term prognosis.

Which of the following regimens is most appropriate?

(A) Morning injections of mixed insulin lispro and insulin aspart
(B) Evening injections of mixed regular insulin and insulin glargine
(C) Morning and evening injections of regular insulin,
supplemented by small amounts of NPH insulin at
mealtimes
(D) Morning injections of insulin glargine, supplemented by small amounts of insulin lispro at mealtimes
(E) Morning injection of NPH insulin and evening injection of regular insulin

A

(D) Morning injections of insulin glargine, supplemented by small amounts of insulin lispro at mealtimes

43
Q

Which one of the following drugs promotes the release of endogenous insulin?

(A) Acarbose
(B) Canagliflozin
(C) Glipizide
(D) Metformin
(E) Miglitol
(F) Pioglitazone
A

(C) Glipizide

Glipizide is a second-generation sulfonylurea that promotes insulin release by closing potassium channels in pancreatic B cells

44
Q

Which of the following is an important effect of insulin?

(A) Increased conversion of amino acids into glucose
(B) Increased gluconeogenesis
(C) Increased glucose transport into cells
(D) Inhibition of lipoprotein lipase
(E) Stimulation of glycogenolysis

A

(C) Increased glucose transport into cells

45
Q

A 54-year-old obese patient with type 2 diabetes has a history of alcoholism. In this patient, metformin should either be avoided or used with extreme caution because the combination of metformin and ethanol increases the risk of which of the following?

(A) A disulfiram-like reaction
(B) Excessive weight gain
(C) Hypoglycemia
(D) Lactic acidosis
(E) Serious hepatotoxicity
A

(D) Lactic acidosis

46
Q

Which of the following drugs is taken during the first part of a meal for the purpose of delaying the absorption of dietary carbohydrates?

(A) Acarbose
(B) Exenatide
(C) Glipizide
(D) Pioglitazone
(E) Repaglinide
A

(A) Acarbose

47
Q

The PPAR-γ receptor that is activated by thiazolidinediones increases tissue sensitivity to insulin by which of the following mechanisms?

(A) Activating adenylyl cyclase and increasing the intracellular concentration of cAMP
(B) Inactivating a cellular inhibitor of the GLUT2 glucose transporter
(C) Inhibiting acid glucosidase, a key enzyme in glycogen breakdown pathways
(D) Regulating transcription of genes involved in glucose utilization
(E) Stimulating the activity of a tyrosine kinase that phosphorylates the insulin receptor

A

(D) Regulating transcription of genes involved in glucose utilization

48
Q

Which of the following drugs is most likely to cause hypoglycemia when used as monotherapy in the treatment of type 2 diabetes?

(A) Acarbose
(B) Canagliflozin
(C) Glyburide
(D) Metformin
(E) Miglitol
(F) Rosiglitazone
A

(C) Glyburide

The insulin secretagogues, including the sulfonylurea glyburide, can cause hypoglycemia as a result of their ability to increase serum insulin levels

49
Q

Which of the following patients is most likely to be treated with intravenous glucagon?

(A) An 18-year-old woman who took an overdose of cocaine and now has a blood pressure of 190/110 mm Hg
(B) A 27-year-old woman with severe diarrhea caused by a flare in her inflammatory bowel disease
(C) A 57-year-old woman with type 2 diabetes who has not taken her glyburide for the last 3 d
(D) A 62-year-old man with severe bradycardia and hypotension resulting from ingestion of an overdose of atenolol
(E) A 74-year-old man with lactic acidosis as a complication of severe infection and shock

A

(D) A 62-year-old man with severe bradycardia and hypotension resulting from ingestion of an overdose of atenolol

Glucagon acts through cardiac glucagon receptors to stimulate the rate and force of contraction of the heart.

Because this bypasses cardiac β adrenoceptors, glucagon is useful in the treatment of β-blocker-induced cardiac depression

50
Q

Side effects of 2nd gen Sulfonylureas

A

hypoglycemia (less)
photosensitivity
hematologic toxicity

Glibenclamide - CHOLESTATIC JAUNDICE

CI: hepatic and renal impairment

51
Q

1st line treatment for T2DM
DM prevention
PCOS
DOC for OBESE patients

A

Biguanide

Metformin

52
Q

Anti DM Drugs that cause weight GAIN

A

SIT

Sulfonylurea
Insulin
TZD

53
Q

Anti DM Drugs that cause weight LOSS

A

MSG

Metformin
SGLT2 (-)
GLP1 Agonist

54
Q

Anti DM Drugs that cause NEITHER weight loss or weight gain

A

DPP-4 (-)

Pharmacology (72 decks)

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