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Pharmacology > Type II Diabetes Mellitus > Flashcards

Type II Diabetes Mellitus Flashcards

1
Q

Type 2 Diabetes

-Cause
-B-cell function
-Insulin
-Body type
-OOA

A

-Lifestyle, genetic
-B cell function –
normal
-Insulin resistance
- Obesity
-Onset less rapid,
milder symptoms

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2
Q

Classes of drugs?

A

D-I-A-G-S

  1. Insulin secretagogues
  2. Insulin sensitizers
  3. α-Glucosidase inhibitor
  4. Dipeptidyl Peptidase IV
    (DPP-IV) Inhibitor
  5. Glucagon-like peptide-1
    (GLP-1) Mimetic
  6. Sodium-glucose co-transporter 2 (SGLT2)
    inhibitors
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3
Q

Insulin secretagogues

  1. Insulin levels
  2. Action dependency
  3. Dosing(x2)
  4. S/E
    5.Microalbuminuria
A
  1. Insulin levels:
    ↑ basal and/or postprandial insulin levels
  2. Action
    dependency:
    Actions depend on functional β-cells
  3. Dosing(x2):
    Sulfonylureas: 1-2 times daily
    Meglitinides: 3-4 times daily
  4. S/E:
    -Weight gain,
    hypoglycaemia

5.Microalbuminuria:
Reduce microalbuminuria

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4
Q

Sulfonylureas

  1. Generation
  2. MOA
  3. Drugs
A
  1. Generation:
    2nd generation
  2. MOA:
    ↑ insulin secretion
    ↓ hepatic clearance of insulin
    ↓ Glucagon levels
  3. Drugs:
  4. Glibenclamide
  5. Gliclazide
  6. Glipazide
  7. Glimepiride
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5
Q

Sulfonylureas

  1. Metabolism
  2. Lipids
  3. Placenta
  4. Metabolites
A
  1. Metabolism:
    Metabolised in the liver
  2. Lipids:
    No effect on lipids
  3. Placenta:
    Crosses placenta
  4. Metabolites:
    Metabolites excreted by
    renal system
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6
Q

Sulfonylureas:

Drugs & DOA

A
  1. Drugs & DOA:
  2. Glibenclamide-Long acting 24hrs
  3. Gliclazide-Long acting 24hrs
  4. Glipazide-Short acting 12-24hrs
  5. Glimepiride-Short acting 12-24hrs
  6. A/E
  7. DI
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7
Q

Sulfonylureas
CI?

A

Significant hepatic / renal impairment – increases half-life

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8
Q

Sulfonylureas A/E?

A

1.Hypoglycemia
2. Nausea & vomiting
3. Allergic skin reactions
4. Minor disulfiram-like reactions
5.Headache, 6.Cardiotoxicity

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9
Q

Sulfonylureas DI?

A
  1. Aspirin & Sulphonamides potentiate the effects of SUs
  2. Hepatic enzyme inducers, corticosteroids, oral
    contraceptives ↓ the effects of SUs
  3. β-blockers mask the signs of hypoglycemi
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10
Q

Meglitinides

  1. Drugs
  2. Binding/MOA
  3. Combination
  4. Lipids
A
  1. Drugs:
    Repaglinide and Nateglanide
  2. Binding:
    Bind to ATP-dependent K+ channels,
    causing insulin release
  3. Combination:
    Not to be used in combination with SUs
    (↑s insulin secretion)
  4. Lipids:
    No effect on lipids
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11
Q

Repaglinide
combination?

A

Can be combined with
* metformin or
* thiazolidinediones

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12
Q

Repaglinide S/E-5?

A

adverse effects:
1. Hypoglycemia
2. Upper respiratory tract
infections
3. Weight gain
4. Bronchitis
5. Headache

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13
Q

Nateglinide MOA?

A
  1. Rapid onset of action (3x more than R)
    ↑s early phase insulin release
  2. Rapid-off action (5x more than R)
    ♦ Insulin return to pre-prandial levels 3-4 hrs
    ♦ ↓s risk of postprandial hypoglycemia
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14
Q

Nateglinide A/E-2?

A
  1. Nausea
  2. Diarrhea
  3. Mild hypoglycemia
  4. No increase in body weigh
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15
Q

Thiazolidinediones drugs?

A
  1. Rosiglitazone (withdrawn) 2.Pioglitazone
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16
Q

Thiazolidinediones

  1. Insulin
  2. Glucose
  3. Glucose uptake
  4. Therapeutic effect
  5. MOA-3
A
  1. Insulin:
    Insulin sensitizers – enhance effects of insulin
  2. Glucose:
    Decrease Glucose output in liver
  3. Glucose uptake:
    Decreases glucose uptake and increase insulin sensitivity in muscles
  4. Therapeutic effect:Therapeutic effect delayed for 4 – 12 weeks
  5. MOA:
    -Agonist at the peroxisome
    proliferator-activated
    receptor – γ (PPARγ)
    - Induces insulin gene
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17
Q

Thiazolidinedione - Pioglitazone

  1. LDL levels
  2. TG/FFA levels
  3. HDL levels
  4. Hypoglycaemia
A
  1. LDL levels:
    No effect on LDL levels
  2. TG/FFA levels:
    ↓ TG and FFA levels
  3. HDL levels:
    ↑ HDL levels
  4. Hypoglycaemia:
    ↓s risk of hypoglycemia
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18
Q

Thiazolidinedione - Pioglitazone therapeutic uses?

A
  1. Monotherapy
  2. With Sulfonylureas
  3. With Metformin
  4. With injected insulin
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19
Q

Thiazolidinedione - Pioglitazone caution?

A

Caution: heart failure /
History of heart failure

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20
Q

Thiazolidinedione - Pioglitazone A/E-5?

A
  1. Fluid retention (oedema)
  2. Weight gain
  3. Anaemia
  4. CVD
  5. Increased risk of cardiac ischaemi
21
Q

Biguanides - Metformin

  1. Obese patients
  2. MOA
A
  1. Obese patients-Decreases body weight
  2. MOA:
    Decreases hepatic glucose production, fasting insulin + Increase glucose uptake
22
Q

Biguanides - Metformin
insulin?

A

Does not stimulate insulin secretion

23
Q

Biguanides - Metformin insulin sensitivity?

A

↑ insulin sensitivity

24
Q

Biguanides - Metformin:

  1. TG, FFA & LDL
  2. HDL levels
  3. Macrovascular
A
  1. Decreases TG, FFA & LDL
  2. Increases HDL levels
  3. Decreases risk for the development
    of macrovascular complications
25
Q

Biguanides - Metformin uses?

A

In combination with SUs,
meglitinide,
thiazolidinediones,
insulin, or α-glucosidase
inhibiton

26
Q

Biguanides - Metformin CI-4?

A
  1. Renal Impairment & hepatic
    disease
  2. Alcohol abuse
  3. If predisposed to CV
    collapse, acute CHF,
    severe infection
  4. History of lactic acidosis
27
Q

Biguanides - Metformin A/E?

A
  1. GI disturbances –
    abdominal discomfort and
    diarrhoea, metallic taste,
    mild anorexia
  2. Lactic acidosis
28
Q

α-glucosidase inhibitor - Acarbose MOA-3?

A
  1. Inhibits the breakdown of complex CHO in small
    intestine
  2. Delays CHO absorption
  3. Inhibits glucoamylase > sucrase > maltase
    > dextranase
29
Q

α-glucosidase inhibitor - Acarbose benefits?

A

↓s postprandial hyperglycemia (hypoglycemia – rare)
* No effect on lipids or insulin levels

30
Q

Acarbose A/E?

A

*GI disturbances
* Dose-dependent toxicity

31
Q

Acarbose CI-3?

A
  1. Inflammatory bowel
    disease
  2. GI obstruction
    3.Cirrhosis
32
Q

Acarbose combination ?

A

Can be combined with
insulin, metformin or
sulfonylureas – additive
effect

33
Q

Dipeptidyl Peptidase IV
(DPP-IV) Inhibitors drugs?

A
  1. Sitagliptin
  2. Vildagliptin
    3.Saxagliptin
34
Q

Dipeptidyl Peptidase IV
(DPP-IV) Inhibitors insulin?

A

Extend action of insulin while
suppressing release of glucagon

35
Q

Dipeptidyl Peptidase IV
(DPP-IV) Inhibitors insulin combination?

A

Can be combined with
insulin, metformin or
sulfonylureas – additive
effect

36
Q

Dipeptidyl Peptidase IV
(DPP-IV) Inhibitors insulin A/E?

A
  1. Gastrointestinal
    discomfort
  2. Peripheral
  3. oedema
  4. liver dysfunction
37
Q

Dipeptidyl Peptidase IV
(DPP-IV) Inhibitors caution?

A

Renal impairement

38
Q

Glucagon-like peptide-1 (GLP-1) Mimetic drugs?

A
  1. Dulaglutide
  2. Exenatide
  3. Liraglutide
  4. Semaglutide
39
Q

Glucagon-like peptide-1 (GLP-1) Mimetic A/E-4?

A
  1. Hypoglycemia,
  2. Nausea& vomiting
  3. Rash
  4. Pancreatitis
40
Q

Glucagon-like peptide-1 (GLP-1) Mimetic CI?

A
  1. type 1 diabetes,
    ketoacidosis, severe
    renal impairment.
  2. Not for use in pregnancy
41
Q

Glucagon-like peptide-1 (GLP-1) Mimetic admin and dosage?

A

Admin: Administered
subcutaneously

Dosage:
1. Exenatide ( 2 x daily)
2. Liraglutide ( 1 x daily)
3. Semaglutide ( 1 x weekly

42
Q

Glucagon-like peptide-1 (GLP-1) Mimetic & weight loss?

A

May promote weight loss

43
Q

Glucagon-like peptide-1 (GLP-1) Mimetic & CVS?

A

Cardiovascular benefits

44
Q

Sodium-glucose co-transporter 2
(SGLT2) inhibitors drugs?

A
  1. Dapagliflozin
  2. Canagliflozin
  3. Empagliflozin
45
Q

Sodium-glucose co-transporter 2
(SGLT2) inhibitors MOA?

A

Competitive, selective
inhibitor of SGLT-2 –
preventing kidneys from
reabsorbing glucose into the
blood

46
Q

Sodium-glucose co-transporter 2
(SGLT2) inhibitors CI-3?

A
  1. Renal impairment
  2. Not for use in pregnancy or
    lactation
  3. Can be combined with metformin, pioglitazone or
    sitagliptin
47
Q

Sodium-glucose co-transporter 2
(SGLT2) inhibitors A/E-2?

A
  1. Increased risk of genital
    and urinary tract infections

2 Hypotension

48
Q

Glucagon-like peptide-1 (GLP-1) Mimetic MOA?

A
  1. Incretin mimetic
  2. Exhibits GLP-1 actions
  3. Insulin secretion
    4.Glucagon secretion

Pharmacology (44 decks)

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