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SFM5 > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

sulfonylureas (SUs)

A

e. g.,
- gl(i/y)***ide
- glipizide, glimepiride, glyburide

mx:

  • stimulate insulin release
  • SUR1 AGonists

uses:
- OHA (oral hypoglycemic agent)
- decreases A1c by 1.5-2, fasting blood glucose (FBG) by ~60
- lean type 2 diabetics
- combine w/ other OHAs or basal insulin
- cheap, long history of safety

sFx/AEs:

  • hypOglycemia
  • weight gain
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2
Q

gl(I/y)***ide

A 
sulfonylureas
stimulate insulin release
decrease A1c 1.5-2, FBG 60
cheap
may cause hypOglycemia
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3
Q

glipizide

A 
sulfonylurea
stimulate insulin release
decrease A1c 1.5-2, FBG 60
cheap
may cause hypOglycemia
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4
Q

glimepiride

A 
sulfonylurea
stimulate insulin release
decrease A1c 1.5-2, FBG 60
cheap
may cause hypOglycemia
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5
Q

meglitinides

A

e. g.:
- –glinide
- repaglinide
- nateglinide

mx:

  • stimulate insulin release
  • SUR1 AGonist

uses:

  • OHA
  • permits dietary variability d/t rapid on and off = good for pts with erratic meal patterns
  • hepatic metabolism = can be used in renal disease
  • use w/ other OHA or basal insulin
  • repaglinide ~ SUs > nateglinide

sFx/AEs:

  • hypOglycemia
  • relative c/i in liver disease (hepatic metabolism)
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6
Q

repaglinide

A 
meglitinide
stimulate insulin release
decrease A1c 1.5-2, FBG 60
safe in renal disease, erratic meal patterns 
may cause hypOglycemia
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7
Q

biguanides

A

e. g.,
- metformin

mx:

  • decrease hepatic glucose output (HGO; mostly glycogenolysis)
  • increase GLUT4 translocation (insulin sensitivity)
  • may reduce appetite (anorectic)

uses:

  • first line OHA when renal fx preserved
  • no hypOglycemia
  • weight neutral
  • similar strength to SU – decrease A1c 1.5-2, FBG ~60

sFx/AEs

  • c/i in eGFR <30
  • GI discomfort
  • reduced B12 absorption
  • possible lactic acidosis
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8
Q

metformin

A

biguanide
first line OHA when renal fx preserved
c/i in eGFR <30

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9
Q

alpha-glucosidase inhibitors

A

e. g.,
- acarbose
- miglitol

mx:

  • delays carbohydrate absorption
  • intestinal glucosidase ANTagonist

use:

  • normal FBG, high postprandial BG
  • decrease A1c 0.5-1
  • decrease postprandial BG 50-60
  • limited hypoglycemia

sFx/AEs:

  • GI - flatulance, diarrhea, discomfort
  • hypoglycemia when combined with SU, meglitinides, insulin
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10
Q

acarbose

A

alpha-glucosidase inhibitor
delays carbohydrate absorption
decrease postprandial BG 50-60
GI side effects

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11
Q

thiazolidinediones

A

e. g.,
- –glitazone
- pioglitazone

mx:

  • PPAR-gamma receptor AGonists
  • relocate fat from muscle and liver to peripheral fat
  • increases peripheral insulin sensitivity

uses:

  • obese T2DM
  • lipodystrophy (inability to produce and maintain fat)
  • decrease A1c 0.5-1.5
  • decrease FBG 15-60
  • no hypoglycemia
  • safe in renal failure

sFx/AEs:

  • weight gain, esp w/ insulin cotherapy
  • fluid retention
  • edema
  • CHF
  • in women, fractures, decreased bone mineral density
  • caution in liver disease
  • c/i class 3-4 CHF
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12
Q

pioglitazone

A 
thiazolidinediones
PPAR-gamma-R AGonist
move fat from liver/muscle to periphery to increase peripheral insulin sensitivity
use in obese T2DM
safe in renal failure
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13
Q

DPP-IV inhibitors

A

e. g.,
- –gliptin
- alogliptin

mx:

  • increase glucose-dependent insulin secretion and glucagon suppression
  • inhibition of dipeptidyl-peptidase IV
  • increase portal GIP and GLP-1

uses:

  • mono therapy or combo w/ metformin, –glitazone, basal insulin
  • decrease A1c 0.5-0.8
  • decrease FBG and postprandial BG
  • once daily
  • weight neutral

sFx/AEs:

  • increased risk of pancreatitis
  • hypersensitivity incl SJS
  • nasopharyngitis
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14
Q

alogliptin

A 
DPP-IV inhibitor
increase portal GIP and GLP-1 to increase glucose-dependent insulin secretion
mono or combo
decrease A1c 0.5-0.8, FBG, ppBG
pancreatitis risk
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15
Q

SGLT2i

A

e. g.,
- –gliflozin
- empagliflozin

mx:

  • renal glucose wasting
  • inhibit SGLT2 transporter

uses:

  • add-on independent of A1c in CAD, CHF, CKD w/ eGFR >30
  • decrease A1c ~1
  • once daily
  • weight loss
  • bp control
  • decrease major adverse cardiac events, hospitalization for HF, progression of CKD

sFx/AEs

  • genital candiasis
  • UTI
  • dehydration
  • euglycemic DKA
  • Fournier’s gangrene
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16
Q

empagliflozin

A

SGLT2i
renal glucose wasting
T2DM, CAD, CHF, CKD (eGFR>30), weight loss, HTN
risk of euglycemic DKA, Fournier’s gangrene, genital candiasis/UTI, dehydration

17
Q

indications for basal+bolus insulin

A

any of:

  • FBG >250
  • A1c > 10
  • ketonuria
  • severely symptomatic hyperglycemia
  • T1DM

except in T1DM can ween if glucose control improves

18
Q

indications for bedtime (only) insulin

A

not at A1c on maximal oral and non-insulin tx
and*
A2c <10 (>10 is analog insulin)

19
Q

bedtime insulin dosing

A

10 units starting is “typical”

but more accurately:

  1. 1 units/kg in small, insulin sensitive, or CKD patients
    - e.g. 5 units for 110 lb pt
  2. 2 units/kg if obese AND FBG>200
    - e.g., 25 units for 275 lb pt

THEN
check BG daily
if FBG >130 3 days in a row, titrate up by 2 units
(then check again for 3 days, titrate up again 2 more units if still not at goal)
etc until goal is reached

up to 40-50 units or 0.5 units/kg is not uncommon

20
Q

basal-prandial insulin dosing

A

total daily dose: 0.3-0.5 units/kg
1/2 at bedtime, 1/2 before meals
split evenly between meals

e.g., 100 kg (220 lb):
30 units total daily dose starting (0.3 units/kg) =
15 units at bedtime (QHS)
5 units before each of 3 meals (TIC AC)

21
Q

when to titrate insulin

A
  • 10% increase to total daily dose if all BG >200
  • 15-20% increase if all BG >300
  • if some normal some high, fine tune to carb counts
  • be sure to check FBG at least 2-3 days in a row before increasing to avoid overnight hypOglycemia
22
Q

supplemental/correctional dosing of analog (short-acting) insulins

A

“fudge factor” = 1700

this helps you calculate their insulin sensitivity i.e. the amount that their BG should drop with a single insulin unit
which helps to make a supplemental/correction scale (how much to add before a meal, based on their BG)

insulin sensitivity = ff / TDD

e.g.,
for patient on 50 units TDD
insulin sensitivity = 1700 / 50 = 34
blood glucose should drop by 34 with each unit of insulin given

so
advise the patient to add 1 unit for each 35 above 150 before a meal (add 1 unit if BG 150-185, 2 units if BG 185-220, etc)

if pre-meal BG is too low (<80-90), reduce dose by 10%

23
Q

for a patient on 75 units TDD insulin, how much analog insulin should they add if their pre-meal BG is 250?

A

“fudge factor” = 1700
insulin sensitivity = ff/TDD = 1700 / 75 = 23
round off to 25

150 is max pre-meal goal
(250 - 150) / 25 = ***4 units

or 
150-175 1 unit
175-200 2 units
200-225 3 units
225-250 4 units
24
Q

correctional analog insulin based on carbohydrate to insulin ratio (CIR)

A

CIR fudge factor = 450
CIR = ff / TDD

CIR tells you g of carb you can eat per unit of insulin (or insulin to add per given amount of carbs)

e.g.,
TDD = 50 units
CIR = 450 / 50 = 7
take 1 unit insulin per 7 g carbs

25
Q

regular (R) insulin, SQ

A

PK:

  • 0.5-1 h onset
  • 2-4 h peak
  • 6-8 h duration

uses:
- premeal

advantages:

  • inexpensive
  • long safety track record
  • i.e. insurance

disadvantages:

  • take 30-60 min before meal
  • long tail = late lows
26
Q

rapid insulin analogs

A

e. g.,
- Aspart
- Lispro

PK:

  • 15-30 min onset
  • 1.5 h peak
  • 3-6 h duration

uses:

  • premeal
  • SQ or pumps

advantages:

  • stronger postprandial control with less hypOglycemia
  • less variable onset and duration

disadvantages:

  • more rapid DKA w/ insulin pump failure
  • $$$
27
Q

faster-acting aspart

A

PK:

  • 15 min onset
  • 1 h peak

uses:
- immediately before meal or w/in 20 min of meal

28
Q

NPH (N) insulin

A

(neutral protamine haegdorn)

PK:

  • 1-4 (~2) h onset
  • 6-10 h peak
  • 12-20 h duration

uses:
- basal/bedtime insulin

advantages:

  • inexpensive
  • can mix with R w/ no change in kinetics

disadvantages:
- peaks in afternoon if used in am or at 2-3 am if used before dinner, making it not true flat basal maintenance (lows around those times)

29
Q

glargine

A

long-acting insulin analog

PK:

  • 1.5 h onset
  • 20-24 h duration
  • flat/no peak

uses:
- basal/bedtime insulin
- can combine with prandial regimen, OHAs, GLP-1R AGonists

advantages

  • long acting
  • ~flat

disadvantages

  • can’t be combined with other insulins, so more injections
  • injection site pain
  • $$$
30
Q

GLP-1R AGonists

A

non-insulin injectable

e. g.,
- –glutide
- semaglutide (oral also)
- lira, dula, lixi

mx:

  • glucose-dependent insulin secretion and glucagon suppressant
  • appetite suppressant/satiety enhancement

uses:

  • first-line injectable when maxed on oral
  • OHA add-on
  • appetite suppressant
  • weight loss
  • limited hypoglycemia
  • pp control
  • decreased MACE (sema, lira, dula)
  • renal protection
  • 1 wk duration w/ sema, dula, exen

sFx/AEs:

  • GI (nausea, vomiting, diarrhea)
  • pancreatitis risk
  • possible C-cell neoplasia (rodents)
31
Q

semaglutide

A 
GLP-1R AGonist
oral and SQ
1 week duration
glucose-dependent insulin secretion, appetite suppression, weight loss
decreased MACE
renal protection

SFM5 (14 decks)

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