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SP - Week 9 GI > DM2 > Flashcards

DM2 Flashcards

1
Q

DM drugs

A

 Insulin
 Metformin
 Sulfonylureas
 Thiazolidinediones
 Glucagon-like peptide 1 (GLP-1) mimetics
 Dipeptidyl peptidase-4 (DPP-4) inhibitors
 Sodium-glucose co-transporter 2 inhibitors (SGLT-2i)

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2
Q

SULFONYLUREAS 1st gen drugs exs.

A

-amide
 Tolbutamide (short acting)
 Chlorpropamide (long acting)

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3
Q

Chlorpropamide AE
(Why’s it not used as much anymore?)

A

 Long-acting: can cause severe hypoglycemia
 Causes flushing after alcohol because of a disulfiram-like effect
 ADH action: hyponatraemia and water intoxication

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4
Q

SULFONYLUREAS 2nd gen exs

A

Gl-, -ide
Glibenclamide (glyburide), glipizide, glimepiride, gliclazide

They’re More potent than 1st gen

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5
Q

MoA of Sulfonylureas

A
  1. Inhibit KATP channels on β-cells
  2. Depolarisation
  3. Ca2+ entry
  4. Insulin release
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6
Q

AE of Sulfonylureas in general

A
  1. Hypoglycemia
    - Can be severe and prolonged
    • Highest risk: chlorpropamide, glibenclamide
    • Low risk: tolbutamide
  2. Weight gain
  3. GI upset less common
  4. Allergic skin rashes and bone marrow toxicity
    • Sulfonamide moiety
  5. Most cross the placenta and enter breast milk.
    • Contraindicated in pregnancy and breastfeeding
    • Glyburide (and metformin) can be considered in pregnancy
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7
Q

CI of Sulfonylureas

A

Most cross the placenta and enter breast milk
 Contraindicated in pregnancy and breastfeeding
 Glyburide (and metformin) can be considered in pregnancy

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8
Q

Sulfonylureas Clinical use

A

 Early treatment of T2D (Not useful in T1D or late-stage T2D) + Require functional B cells
 Can be used as monotherapy if metformin is contraindicated or not tolerated
-Metformin is superior in terms of CV disease
prevention
 Can be combined with other drugs in dual or triple therapy
But not with insulin. DoNT choose 2 drugs that can lead to hypoglycaemia / weight gain

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9
Q

THIAZOLIDINEDIONES (GLITAZONES)
Older drugs exs and what do they cause

A

-one
 Ciglitazone/troglitazone caused liver toxicity
 Rosiglitazone thought to increase risk of heart attacks
Pioglitazone: only drug in this class of
clinical use in Europe

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10
Q

THIAZOLIDINEDIONES (GLITAZONES)
Benefits?

A

Significant adverse effects
 No beneficial effects on mortality
 Benefits on HbA1c (surrogate marker)

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11
Q

THIAZOLIDINEDIONES (GLITAZONES) MoA

A

 Activate the peroxisome proliferator-activated receptor-γ/ retinoid X receptor (PPARγ–RXR)

 Binds to DNA: transcription of several genes
-Effects are slow in onset (1-2 months after start of treatment)

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12
Q

PPARγ is found mainly in ? + what does it do?

A

PPARγ is found mainly in adipose tissue
 Decreases plasma triglyceride levels
 Increases lipogenesis and enhances uptake of fatty acids and glucose
 Differentiation of adipocytes

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13
Q

PPARγ found also in muscle and liver
Therefore?

A

 Reduced hepatic glucose output
 Increased glucose uptake into muscle
 Enhanced effectiveness of endogenous insulin (insulin sensitizers): lowers exogenous insulin requirements

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14
Q

AE of THIAZOLIDINEDIONES (GLITAZONES)

A
  1. Weight gain : Increased deposition of subcutaneous fat and fluid retention
  2. Fluid retention:
    • Promotes Na+ reabsorption in collecting ducts
    • Contraindicated in heart failure
  3. Increased cardiovascular risk
  4. Increased risk of fractures with chronic use
    - Shunting of mesenchymal cells into adipocyte lineage and away of osteogenesis
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15
Q

THIAZOLIDINEDIONES (GLITAZONES)
Clinical uses

A

 Can be used as monotherapy (when metformin
cannot be used) or as additive with other oral
hypoglycaemic drugs
 May lessen the progression of impaired glucose
tolerance to diabetes
 May reduce the need for exogenous insulin in
T2D

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16
Q

THIAZOLIDINEDIONES (GLITAZONES) other symptoms

A

headache, fatigue, GI disturbances

17
Q

THIAZOLIDINEDIONES (GLITAZONES)
CI

A

Contraindicated in pregnancy, breastfeeding, children

Contraindicated in heart failure

18
Q

GLP-1 MIMETICS
Exs.

A

Exenatide, liraglutadine, duraglutide,
lixisenatide, semaglutide

19
Q

GLP-1 MIMETICS
MoA

A

Mimic effects of GLP-1: longer acting

Mechanism of Action
 Increase insulin secretion
 Suppress glucagon secretion
 Slow gastric emptying
 Reduce food intake (by an effect on satiety) ->Associated with modest weight loss

20
Q

GLP-1 MIMETICS
RoA

A

SC administration
- Administered before the first and last meal of the day
 Modified Release (MR) formulation: once weekly
injections

21
Q

GLP-1 MIMETICS AE

A

Adverse effects
 Hypoglycaemia
 GI effects
 Pancreatitis is a rare but sometimes severe problem

22
Q

GLP-1 MIMETICS Clinical use

A

Clinical use
 In T2D, in combination with other drugs when
inadequate
!!  Recommended in patients with atherosclerotic
cardiovascular disease, high cardiovascular risk,
kidney disease or heart failure (in addition to
metformin). —> Cardiovascular benefits
 Recommended in obese patients, who have
failed on dual therapy

23
Q

DPP-4 INHIBITORS exs

A

-iptin
 Examples: sitagliptin, vildagliptin, saxagliptin,
linagliptin

24
Q

DPP-4 INHIBITORS MoA

A

 Competitively inhibit DPP-4
 Potentiate endogenous incretins (GLP-1 and GIP)

25
Q

DPP-4 INHIBITORS effect on weight + RoA

A

No effect on weight
 Administered orally
 Generally well-tolerated
- Less propensity for hypoglycaemia

26
Q

DPP-4 INHIBITORS AE

A

Adverse effects
 GI side effects
 Less common but potentially serious
-Occasional liver disease
- Worsening of heart failure (peripheral oedema)
- Pancreatitis

27
Q

DPP-4 INHIBITORS clinical uses

A

 Combination therapy with metformin (and/or other antihyperglycaemic agents) if blood glucose is not adequately controlled
[DONT COMBINE W GLP1 b/c they use the same pathway]

 As monotherapy if metformin is contraindicated or not tolerated
 Long-term experience and outcome evidence
lacking

28
Q

SODIUM-GLUCOSE CO-TRANSPORTER 2 (SGLT-2) INHIBITORS
Exs

A

—agliflozin

Canagliflozin, dapagliflozin,
empagliflozin

29
Q

Canagliflozin, dapagliflozin, empagliflozin
MoA

A

Block SGLT-2 in proximal tubule
 Increased glucose excretion
 Increased osmotic natriuresis
- Decrease in weight and blood pressure
- Reduced preload
- Reduced intra-glomerular pressure

 Benefits in renal and CV outcomes in CKD, HF
natriuresis

30
Q

SGLT-2 INHIBITORS AE

A

 Polyuria
 UTIs
 Vaginal yeast infections
 Hyperkalaemia
 Volume depletion (orthostatic hypotension)

31
Q

SGLT-2 INHIBITORS
Clinical uses

A
  1. T2D, usually in combination with other antidiabetic drugs (e.g. metformin, insulin)
    • Monotherapy if metformin is not tolerated
      ! - Recommended in patients with atherosclerotic
      cardiovascular disease, high cardiovascular risk, kidney disease or heart failure (in addition to metformin)
  2. Symptomatic chronic HF with reduced ejection fraction, inadequately controlled with a β-blocker, ACEI/ARB, and an aldosterone antagonist
  3. CKD with albuminuria, alongside an ACEI/ARB
32
Q

DIABETES MANAGEMENT

A

 Individualized glucose-lowering therapies
 Diet, exercise, and education as the foundation of the treatment program
 Use of metformin as the optimal first-line drug unless contraindicated
 After metformin, the use of 1 or 2 additional oral or injectable agents, with a goal of minimizing adverse effects if possible
 Ultimately, insulin therapy alone or with other agents if needed to maintain blood glucose control  Where possible, all treatment decisions should involve the patient, with a focus on patient preferences, needs, and values
 A major focus on comprehensive cardiovascular risk reduction

SP - Week 9 GI (3 decks)

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