Antidiabetics Flashcards

1
Q

hallmark of untreated T1 DM is elevated levels of blood ___ and ___

patients have virtually no insulin secretion → must rely on _____ injected

A

hallmark of untreated T1 DM is elevated levels of blood glucose and ketone bodies

patients have virtually no insulin secretion → must rely on exogenous insulin injected

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2
Q

Type ___ DM is the most common form of the disease (over 90% of adults with DM have this type)

A

Type 2 DM is the most common form of the disease (over 90% of adults with DM have this type)

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3
Q

in T2 DM, insulin secretion is enough to restrain ____

there is hyperglycemia but no ____

A

in T2 DM, insulin secretion is enough to restrain ketogenesis

there is hyperglycemia but no ketoacidosis

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4
Q

The secretion of insulin by B cells is stimulated by (3)

A
  • Glucose (most important stimulus)
  • Amino acids
  • Gastrointestinal hormones (Incretins)
    • released after food ingestion
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5
Q

describe the image below

A

Incretin Effect - glucose given orally results in higher insulin levels than given IV because incretins released by gut enhance insulin secretion

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6
Q

describe the mechanism of insulin secretion

A

Hyperglycemia results in high ATP levels → close ATP-dependent K+ channels → membrane depolarization and opening of voltage-gated calcium channels → Ca2+ influx causes pulsatile insulin exocytosis

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7
Q

describe the insulin receptor and where they are found

A

consists of two covalently linked heterodimers, each containing an a subunit and a ß subunit

found in liver, muscle, adipose tissue

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8
Q

Insulin is inactivated by the enzyme ____, which is found mainly in the ___ (60%) and ___ (40%)

(ratio is reversed in insulin-treated diabetics receiving SC injections)

The half-life of circulating insulin is ____

A

Insulin is inactivated by the enzyme insulinase, which is found mainly in the liver (60%) and kidney (40%).

(ratio is reversed in insulin-treated diabetics receiving SC injections)

half-life of circulating insulin is 3-5 min

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9
Q

describe the effects of insulin

A
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10
Q

list the 3 injected, rapid-acting insulin analogs

A

Lispro

Aspart

Glulisine

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11
Q

Rapid-acting insulins mimic the ___ release of insulin

they have greater control of postprandial plasma glucose (PPG) and associated with less risk of ____

Given with a longer acting insulin to assure proper glucose control

A

Rapid-acting insulins mimic the prandial release of insulin

they have greater control of postprandial plasma glucose (PPG) and associated with less risk of hypoglycemic episodes

Given with a longer acting insulin to assure proper glucose control

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12
Q

Rapid-acting insulins should be injected ____

Peak serum levels seen ____ after injection
(50-120 minutes for regular insulin)

DOA is about ____

A

Rapid-acting insulins should be injected 15 min before a meal

Peak serum levels are seen ~ 1 hr after injection
(50-120 minutes for regular insulin)

DOA is about 3-4 hrs

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13
Q

Short-acting insulin: ____

Short-acting soluble human ____

Should be given ____ before a meal

Usually given SC (or IV in emergencies)

A

Short-acting insulin: Regular insulin

Short-acting soluble human crystalline zinc insulin

Should be given 30 minutes before a meal.

Usually given SC (or IV in emergencies)

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14
Q

Intermediate-Acting Insulin: ____

crystalline zinc insulin combined with __

what kind of appearance does this have?

Given __ only

A

Neutral protamine Hagedorn (NPH)
also called Isophane Insulin

crystalline zinc insulin combined with protamine

cloudy appearance

Given SC only

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15
Q

NPH is used for ___ control

usually given with ___ for ___ time control

A

NPH is used for basal control

usually given with rapid/short-acting insulin for meal time control

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16
Q

list long-acting insulin

A

Glargine

Detemir

Degludec

17
Q

Glargine modifications make it more ____ in acidic pH, but precipitates in ____ pH after SC injection

It cannot be mixed with ____

A

Glargine modifications make it more soluble in acidic pH, but precipitates in neutral pH after SC injection

It cannot be mixed with short acting insulin

18
Q

Detemir modifications increase _____ in SC tissue and fatty acid chain binds reversibly to ____

A

Detemir modifications increase self-aggregation in SC tissue and fatty acid chain binds reversibly to albumin

19
Q

What is the benefit of Glargine and Detemir?

How do they differ in administration?

A

they have a lower risk of hypoglycemia than NPH insulin

Glargine: 1x/day

Detemir: 2x/day

20
Q

when Degludec is injected SC, it forms ____ and binds to circulating ____ which delays its absorption

how does Degludec differ from Glargine/Detemir in absorption and administration?

A

when Degludec is injected SC, it forms multihexamers and binds to circulating albumin which delays its absorption

DOA > 42 hrs - does not have to be administered at the same time each day (unlike Glargine and Detemir)

21
Q

onset and duration of different Insulins

A
  • rapid: 1 hr peak
  • short: 3 hr peak
  • intermediate: 5 hr peak
  • long: 24 hr (no peak)
22
Q

Properties of Currently Available Preparations

23
Q

rapid and long-acting insulin analogs improve ___ levels, and reduce ____ compared with regimens with regular insulin and NPH insulin

A

rapid and long-acting insulin analogs improve HbA1C levels, and reduce hypoglycemia compared with regimens with regular insulin and NPH insulin

24
Q

The standard mode of insulin therapy is ___

When is it given IV?

A

The standard mode of insulin therapy is SC injection

IV: ketoacidosis, perioperative period, during labor and delivery, intensive care situations

25
describe inhaled insulin
Peak level at 12-15 min and decline to baseline in 3 hrs AE: **cough, throat pain, hypoglycemia.** Pulmonary function should be monitored **Contraindicated**: asthma, COPD, smokers
26
two methods used to achieve physiological pattern of insulin release
1. Basal-Bolus Insulin Regimens 2. Insulin Pump Therapy
27
Basal-Bolus Insulin Regimens
* 1 shot/day of long-acting insulin for **basal** coverage (at **bedtime** or **morning**), and * doses of **rapid**-acting analog for each **meal** * skip a meal? omit a premeal bolus * eat a larger meal than usual? increase the premeal bolus
28
an insulin ___ is the best way to mimic normal insulin secretion consists of a battery-operated pump and a computer that programs the pump to deliver \_\_\_\_
an insulin **pump** is the best way to mimic normal insulin secretion consists of a battery-operated pump and a computer that programs the pump to deliver **predetermined amounts of insulin**
29
what drugs are used in the insulin pump?
**rapid-acting:** Glulisine, Lispro, or Aspart
30
\_\_\_ is the most serious and common adverse reaction to insulin overdose there is ___ risk with rapid-acting insulin analogs than with regular or NPH insulin
**Hypoglycemia** is the most serious and common adverse reaction to insulin overdose there is **less** risk with rapid-acting insulin analogs than with regular or NPH insulin
31
describe management of **mild** and **severe** hypoglycemia
* **Mild** hypoglycemia in a conscious patient * orange juice, glucose, any sugar-containing beverage or food * **Severe** hypoglycemia with unconsciousness or stupor * IV glucose infusion (if not available: glucagon SC or IM)
32
list other drugs that can cause **hypoglycemia**
* **Ethanol** - inhibits gluconeogenesis * **B-blockers** - blocks effects of catecholamines on gluconeogenesis and glycogenolysis, masks sympathetically-mediated symptoms of hypoglycemia (eg tremor and palpitations) * **Salicylates** - enhance pancreatic B-cell sensitivity to glucose potentiating insulin secretion
33
list other drugs that can cause **hyperglycemia**
* **Epinephrine** - increased glycogenolysis and glucagon * **Glucocorticoids** - prednisolone, dexamethasone, beclomethasone, budesonide, flunisolide, fluticasone * Atypical Antipsychotic * HIV Protease inhibitors * Phenytoin * Clonidine * **CCBs** - verapamil, diltizaem, nifedipine, amlodipine * **Niacin** - causes insulin resistance → caution in diabetic pts * **Diuretics** - Thiozides: hydroclorothiozide, metolazone, chlorthalidone
34
describe management of diabetes in hospitalized patients
* Insulin = cornerstone treatment of hyperglycemia in hospitalized patients * Oral antidiabetic agents should be **discontinued** during acute illness and replaced with insulin (can be restarted on discharge)