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3028PHM Human Pharm II > Drugs for Diabetes > Flashcards

Drugs for Diabetes Flashcards

1
Q

What are the main actions of insulin?

A

Inc glucose uptake

Inc glycogen synthesis

Dec glycogenolysis

Dec gluconeogenesis

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2
Q

What are the main actions of glucagon?

A

inc glycogenolysis

Inc gluconeogenesis

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3
Q

Considering insulin phases, what is the difference between T1DM and T2DM?

A

T2DM = missing only phase 2 of insulin regulation

T1DM = missing both phases 1 and 2 of insulin regulation

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4
Q

Summarise the key points of T1DM

A

Juvenile-onset –> immune mediated

Insulin dependent = little or no insulin produced

Usually non-obese and symptoms appear suddenly

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5
Q

Summarise the key points of T2DM

A

Adult onset

Non-insulin dependent diabetes = begins w/ insulin resistance –> eventual beta cell failure

Genetic basis, sx appear slowly

Require oral hypoglycaemic agents

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6
Q

What are the main symptoms of diabetes?

A

Hyperglycaemia

Glycosuria

Polyuria

Polydipsia

Insulin def

Diabetic ketoacidosis

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7
Q

What symptoms are more common in T1DM?

A

Lethargy

stupor

Weight loss

Kussmaul breathing (hyperventilation)

Smell of acetone

N/V, abdominal pain

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8
Q

What are the complications of diabetes?

A

Macrovascular disease = accelerated atheroma

Microangiopathy = retinopathy, nephropathy, neuropathy

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9
Q

What is HbA1c?

A

Glycosylated haemoglobin = glucose that is haem/protein bound

Ideal is 7% (53 mmol/mol)

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10
Q

What amino acids determine the length of action of the insulins?

A

B-3

B-28-30

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11
Q

List the different types of insulin

A

Human insulin

Insulin aspart (asp at B-28_

Insulin lispro (lys B-28, proline B-29)

Insulin glulisine (lysine B-3)

Insulin glargine (glycine A-21)

Insulin detemir (nothing on B-30)

Insulin degludec (nothing on B-30, may have missing B-29 lysine)

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12
Q

List the ultra short acting insulins

A

Insulin aspart

Insulin lispro

Insulin glulisine

Faster acting insulin aspart

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13
Q

List the short acting insulin

A

neutral insulin (human insulin ?)

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14
Q

List the long acting insulin

A

Isophane insulin

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15
Q

List the long acting insulin analogues

A

Insulin detemir

Insulin glargine

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16
Q

Outline the mechanism behind insulin release

A

Phase 1:
Glucose transported in through the GLUT4 transporter –> inc in ATP –> inhibition of K+ATPase channel –> depolarisation of beta cell –> opening of voltage gated Ca2+ channel –> release of insulin granules

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17
Q

Describe the mechanism behind diabetic ketoacidosis

A

Hyperglycaemia –> insufficient glucose uptake –> cells use proteins and fat as energy –> FFA broken down in liver to ketone bodies (kidney - ketonuria) –> acetoacetate converted to acetone in liver (exhaled - fruity breath)

Cont lipolysis –> inc ketogenesis –> exceeds elimination –> ketonaemia –> inc FFA lvls –> worsening acidosis

Initial compensation through Kussmaul breathing and buffering in blood –> blood and breathing no longer able to compensate –> ketoacidosis

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18
Q

What are some adverse effects of insulin?

A

Hypoglycaemia

Rebound hyperglycaemia

Insulin resistance

local reactions (lipodystrophy)

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19
Q

What are the counter regulatory sympathetic stimulation responses seen in diabetes?

A

Sweating

Anxiety

Palpitations

Tremor

20
Q

What are the main drug interactions associated with insulin?

A

B-adrenergic blockers = prolong hypoglycaemia due to inhibition of compensatory mechanisms

Diuretics, corticosteroids, oral contraceptives = inc blood glucose

Alcohol = precipitates hypoglycaemia due to depletion of hepatic glycogen

Salicylates, lithium, theophylline = precipitate hypoglycaemia –> enhance insulin sec and peripheral glucose utilisation

21
Q

List the oral drug classes used in T2DM

A

Metformin

SGLT2 inhibitors

DPP-4 inhibitors

Sulfonylureas

thiazolidinedione

Acarbose

22
Q

List the parenteral drugs used in diabetes

A

Insulin

GLP-1 analogue

23
Q

List the relevant sulfonylureas used in DM

A

*all end in -ide

Glibenclamide (long acting)

Gliclazide

Glipizide (short acting)

Glimepiride (short acting)

24
Q

What is the MOA of sulfonylureas?

A

Bind + inhibit K+ATPase channel —> inc insulin release from pancreatic beta cells in response to glucose

Act to inc insulin release

25
Q

Which sulfonylureas have a lesser affinity for the K+ATPase channel?

A

glimepride, Gliclazide

Augment second phase of insulin, little effect on 1st phase

26
Q

What are some ADRs of sulfonylureas?

A

GI dist = n/v/diarrhoea/constipation

Hypoglycaemia

Hypersensitivity reactions

blood disorders

cardiovascular mortality

27
Q

What drugs inc the effect of sulfonylureas? (cause hypos)

A

CYP inducers = azole antifungals, salicylates, sulphonamides

Clarithromycin, alcohol, ACE-i

Disopyramide, BB, MAO-i

28
Q

List the important biguanide used to treat diabetes and its MOA

A

Metformin

MOA = inc the activity of AMP-dependent kinase (AMPK) –> dec expression of G6P –> inhibits mitochondrial glycerol-3-phosphate

Dec cellular energy stores (ATP & phosphocreatine) –> activates AMPK

Facilitates glucose uptake by skeletal muscle and adipocytes, inhibits mitochondrial resp chain oxidation (promote peripheral glucose utilisation)

29
Q

What does metformin mediated activation of AMPK do?

A

Inc fatty acid oxidation

Inc glucose uptake

dec lipogenesis

dec gluconeogenesis

30
Q

What is the effect of metformin on the liver?

A

dec gluconeogenesis

Dec glycogenolysis

dec glucose production

31
Q

What is the effect of metformin on the intestine?

A

Inc anaerobic glucose metabolism

32
Q

What is the effect of metformin on the muscle?

A

Inc insulin-mediated glucose uptake

Inc glycogenesis

33
Q

What are some benefits to metformin?

A

Suppress appetite = less weight gain than sulfonylureas

May be cardioprotective

Improves adverse plasma lipid profile
- inc FFA oxidation
- Inc HDL
- Dec plasma triglycerides

34
Q

What are some notable ADRs of metformin?

A

Diarrhoea
- anorexia, abdominal discomfort, nausea, weight loss

Dec Vit B12 absorption

Metallic taste

Inhibition of pyruvate metabolism –> lactate accumulation –> lactic acidosis

35
Q

List the relevant thiazolidinediones and their MOA

A

Pioglitazone = no effect on insulin secretion, “insulin sensitizer”

MOA = its a ligand for PPARY (peroxisome proliferation activating receptor gamma) –> involved in regulation of genes involved in glucose and lipid metabolism

36
Q

What are some general effects of the PPAR-Y agonists used in diabetes?

A

Dec insulin resistance (both muscle and kidney) —> inc muscle glucose uptake and dec liver gluconeogenesis (inhibition of fructose-1,6-bisphosphate)

Inc glucose utilisation in peripheral tissues and ehances expression of cell glucose transporters (GLUT 1 and 4)

37
Q

Name a glucosidase inhibitor used in T2DM treatment and its MOA

A

Acarbose

MOA = competes w/ dietary oligosaccharides for alpha-glucosidase enz —> irreversibly binds to the enzyme –> slow digestion/absorption of glucose –> preprandial peak of glucose is low, BGC is more stable

38
Q

What are some ADRs for acarbose?

A

GI effects = flatulence, abdominal discomfort, diarrhoea

Abnormal liver function = hepatitis

39
Q

What are the actions of incretins (generally)?

A

Enhance glucose-dependent insulin secretion

Inhibit glucagon secretion –> dec hepatic glucose production

Slow gastric emptying

Inc satiety –> less food intake

Both GLP-1 and GIP are rapidly cleaved and inactivated by dipeptidyl peptidase 4 (DPP4)

40
Q

List the drugs that belong to the glucagon-like peptide-1 (GLP-1) analogue class and their overall MOA

A
  • all end in “-glutide”
    Exenatide

Liraglutide

Semaglutice

Dulaglutide

MOA = incretin mimics

41
Q

How are GLP-1 analogues used in diabetes and what are some of their ADRs?

A

Good adjuvant w/ metformin and/or sulfonylurea

ADRs:
- n/v
- diarrhoea, constipation, dyspepsia, GORD, abdominal pain
- hypoglycaemia, headache, dizziness, injection site reactions

- pancreatitis, allergic reactions
42
Q

What diabetic drugs belong in the Dipeptidyl peptidase-4 (DPP-4) inhibitor class?

A
  • “-gliptin”

Aloglipin

Linagliptin

Saxagliptin

Sitagliptin

Vildagliptin

43
Q

How are DPP-4 inhibitors used in diabetes and what are some of their ADRs?

A

Good adjuvant in dual therapy w/ metformin, a sulfonylurea, or a thiazolidinedione

ADRs:
- hypoglycaemia, n/c, acute pancreatitis

44
Q

What diabetic drugs belong in the Na+/glucose co-transporter 2 (SGLT2) inhibitor class?

A
  • “-gliflozin”

Canagliflozin

Dapagliflozin

Empagliflozin

ertugliflozin

45
Q

What is the MOA of SGLT2 inhibitors and what are some of their ADRs?

A

MOA = inhibit SGLT2 co-transporters in the kidney –> reduce glucose reabsorption

ADRs:
- genital infections, polyuria, UTI, dyslipidaemia, hypoglycaemia
- renal impairment
- Hypovolaemia, hypotension, dehydration
- euglycemic ketoacidosis

3028PHM Human Pharm II (17 decks)

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