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Therapeutics II > Insulins to treat diabetes > Flashcards

Insulins to treat diabetes Flashcards

1
Q

Insulin sources

A

-recombinant human insulin
-human insulin cDNA in plasmid (E.Coli or yeast)

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2
Q

Humulin

A

-insulin cDNA in plasmid in E. Coli

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3
Q

Novolin

A

-transformed yeast insulin cDNA

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4
Q

Units of insulin

A

-100 units/mL
-28 units/mg insulin
-humulin also available in 500units/mL

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5
Q

Insulins with rapid onset and short duration

A

-Lispro
-Aspart
-Glulisine

-mimic first phase

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6
Q

Rapid Onset/ Shortish Action

A

Regular (R)

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7
Q

intermediate onset and action

A

NPH (N)

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8
Q

slow onset/ long action

A

-Glargine
-Detemir
-Degludec

-mimic second phase

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9
Q

Modified insulin effect on dosing

A

-delay absorption to prolong onset and duration
-increase absorption to dec onset and duration
-provides flexible dosing
-basal levels vs preprandial dose
-2 phases
-slide 33

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10
Q

Insoluble Insulin Complexes

A

-Lente insulins (no longer used)
-NPH insulin

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11
Q

Semilente

A

-small amorphous particles

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12
Q

Lente

A

-small amorphous and large crystalline complexes
-slow absorption, long acting

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13
Q

Ultralente

A

-only large crystalline complexes
-very slow absorption, very long acting

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14
Q

Insulin hexamer

A

-nucleated by zinc
-trimer of dimers
-slide 35??

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15
Q

lente insulins

A

-zinc/insulin precipitates
-large complex size = prolong absorption from SC site
-monomer is absorbed
-slide 34

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16
Q

NPH insulin

A

-Neutral Protamine Hagedorn
-bound insulin to protamine
-tissue proteases free insulin from protamine
-slow absorption, long action

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17
Q

Mutated Human Insulins

A

-Lispro (humalog)
-Insulin Aspart (Novolog)
-Insulin Glulisine (Apidira)
-Insulin Glargine (Lantus)
-Insulin Detemir (Levemir)
-Insulin Degludec (Tresiba)

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18
Q

Lispro insulin

A

-HUMALOG
-reverse P28 (proline) and K29 (lysine) positions on insulin B chain = dec self-association
-insulin dimer and hexamer formation in reg insulin (not this one tho?)
-monomer absorbed faster
-5-15 min onset (quick)
-inj immediately before meals

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19
Q

Lispro insulin (humalog) counseling

A

-5-15 min onset
-inj immediately before meals

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20
Q

Insulin dimer

A

-slide 38

21
Q

Human insulin primary structure

A
22
Q

Insulin Aspart

A

-Novolog
-human, except P28 in B chain switched to aspartate
-5-15 min onset, short duration
-inj immediately before meals

23
Q

Insulin Glulisine

A

-Apidra
-Asn 3 and Lys 29 in B chain switch to Lys and Glu
-rapid onset, short duration
-inj immediately before meals

24
Q

Insulin Glargine

A

-Lantus
-Asn21 of chain switch to Gly
-2 Arg residues added to end of B chain (30 and 31)
-clear solution (pH 4)
-precipitates post injection
-slowly released from injection site (precipitation form) over 24 hours
-once daily
-no pronounced peak compared to NPH which is good and steady

25
Q

Insulin Detemir (Levemir)

A

-discontinued
-Thr 30 of B chain replaced by fatty acid
=makes insulin bind to serum albumin and itll ride around the body for awhile
-Lys 29 mysristylated
-bind serum albumin extensively
-clear solution
-inj once or twice daily

26
Q

Insulin Degludec

A

-Tresiba
-Thr 30 of B chain replaced by fatty acid
-binds albumin extensively
-clear solution
-inj once daily

27
Q

PK chart of insulins

A

-rapid insulins: spike that mimics first phase
-NPH spikes then falls
-basals: long flat curve

28
Q

Common Multi-dose insulin regimens

A

-fast onset, short action: take before meals
-long/intermediate acting: take at bedtime and AFTER breakfast

29
Q

Insulin mixtures

A

-NPH + regular
-NPL + Lispro
-Degludec + Aspart
-give preprandial bolus and prolonged basal level
-single injection

30
Q

Inhaled insulin

A

-Afrezza
-human insulin as dry powder
-rapid onset, SHORT duration
-use as pre-prandial insulin
-do NOT use in pt with asthma/COPD
-may reduce lung function (dec FEV)
-slide 50 structure

31
Q

Routes of admin

A

-all are SubQ
-insulin infusion pump: Buffered regular and rapid acting (lispro, aspart, glulisine)
-IV: regular (for severe hyperglycemia or ketoacidosis)
-inhalation: afrezza

32
Q

Types of pt using insulin

A

-Type I diabetics
-Pt with ketosis and hyperosmolar coma
-some type II

33
Q

Mode of action of insulin in diabetic

A

-dec liver glucose output
-inc fat storage
-inc glucose uptake

34
Q

Adverse reactions to insulin

A

-hypoglycemia
-lipodystrophy**
-Lipohypertrophy
-lipoatrophy
-insulin resistance

35
Q

Hypoglycemia

A

-too much insulin, not enough food
-weakness, sweating, hunger, tremor, seizures, coma
-neural cells need glucose

36
Q

Hypoglycemia tx

A

-glucose
-glucagon inj if cant swallow

37
Q

Agents that can inc BG in insulin users

A

-catecholamines*
-thyroid hormone
-isoniazid
-GCs*
-calcitonin
-phenothiazines
-oral contraceptices
-somatropin
-morphine*

-*inc glucose output from liver

38
Q

Agents that inc risk of insulin hypoglycemia

A

-ETHANOL**
-ACE-I
-somatostatin
-B-blockers*
-fluoxetine
-steroids
-MAO inhibitors
-vigorous exercise

39
Q

Lipodystophy

A

changes in fat at over used inj site

40
Q

Lipohypertrophy

A

-accumulation of fat in SC tissue
-more common

41
Q

Lipoatrophy

A

-loss of fat in SC tissue
-less common

42
Q

Insulin resistance

A

-immune response to insulin
-rarer

43
Q

Tx overview for type I DM

A

-insulin + diet + exercise
-always insulin bc they cant make any

44
Q

Overview of type II DM tx

A
  1. diet+exercise
  2. ”” + antidiabetic drugs
  3. diet/exercise + insulin
45
Q

Which insulin preparation has longest duration of

A

Glargine

46
Q

Which insulin prep is NOT genetically modified?

-Lispro
-Aspart
-Glulisine
-NPH

A

-NPH

-NPL is bc it with lispro?

47
Q

Lente insulins

A

-not using these
-large complex sixe = prolonged absorption
-Zn helps complex insulin = prolonged activity

48
Q

Ways to prolong action

A

-Zn (lente)
-protamine
-precipitation
-add fatty acid

Therapeutics II (55 decks)

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