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Pharm > DM Hypoglycemics > Flashcards

DM Hypoglycemics Flashcards

1
Q

What are Insulin Sensitizers

A

Biguanides

Thiazolidinediones

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2
Q

Name a Biguanide

A

Metformin

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3
Q

MOA of Metformin

A

Lower hepatic glucose production

Raise density of insulin receptors at tissues

Lower intestinal glucose absorption

Improve muscular glucose absorption

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4
Q

Uses of Metformin

A

Does not affect insulin secretion

Take with meals or after meals to lower GI ADR

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5
Q

ADR of Metformin

A

GI issues - diarrhoea, vomiting, indigestion.

Raise risk of Vit B12 malabsorption and hence Vit B12 deficiency and can worsen symptoms of neuropathy

Use with caution in patients with renal problems

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6
Q

Names of Thiazolidinediones

A

Pioglitazone
Rosiglitazone

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7
Q

MOA of Thiazolidinediones

A

Raise insulin-dependent glucose disposal and lower insulin resistance in periphery and liver

Exact mechanism unclear.

Primary MOA is to activate nuclear transcription factor PPAR-gamma.

PPAR ligands regulate glucose metabolism, adipogenesis, improve insulin sensitivity at adipose tissues, liver and skeletal muscles.

Stimulation of receptors can raise production of GLUT 1 and GLUT 4, enhancing tissue sensitivity to insulin.

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8
Q

Uses of Thiazolidinediones

A

High glucose-lowering efficacy

Does not affect insulin secretion

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9
Q

ADR of Thiazolidinediones

A

Weight gain, peripheral edema, higher risk of HF (fluid retention) and bone fractures

Pioglitazone induce CYP450 activity and reduce serum concentrations of CYP450 metabolized drugs

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10
Q

What are examples of Insulin Secretagogues

A

Sulfonylurea

Meglitinides

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11
Q

MOA of Sulfonylurea

A

Stimulate insulin release from beta cells in pancreatic islets

Target b-cell ATP-sensitive K channel, which plays major role in controlling b-cell membrane potential

Bind to SU receptor proteins, subunits of K-ATP channels.

Drug binding inhibits K-ATP channel mediated K+ efflux, triggering Ca-dependent exocytosis of insulin granules from pancreatic b-cells

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12
Q

Efficacy of Sulfonylurea

A

Take 0.5h before food for better absorption

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13
Q

ADR of Sulfonylurea

A

Can cause weight gain (1-4kg) due to lipogenic effect of insulin

Risk for hypoglycaemia, highest in Glibenclamide. Especially in elderly and renal or hepatic impairment

Contraindicated for Sulfa Allergy

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14
Q

Names of Sulfonyurea

A

Glipizide

Glicazide

Glibenclamide

Glimepiride

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15
Q

Names of Meglitinides

A

Nateglinide

Repaglinide

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16
Q

MOA of Meglitinides

A

Bind and close ATP-dependent K channels on pancreatic beta cells in glucose-dependent manner stimulating insulin release.

This is mediated through unique binding site on SUR1 of beta cell that differs from sulfonylureas’ site of action.

17
Q

Efficacy of Meglitinides

A

Taken before meals to control post-prandial glucose levels - due to rapid onset and short DOA

18
Q

ADR of Meglitinides

A

Use with caution in hepatic impairment patients.

19
Q

Example of a a-Glucosidase inhibitors

A

Acarbose

20
Q

MOA of acarbose

A

a-glucosidase hydrolyzes oligosaccharides to glucose and other sugars

Reversibly inhibit membrane-bound a-glucosidase in intestinal brush borders, slowing down rise in glucose levels after a meal.

21
Q

ADR of acarbose

A

Higher glucose load in colon causes gaseous distension and flatulence

Stomachache, occasional diarrhoea, belching

Banned for patients with GI issues such as IBD, severe renal or hepatic disease.

22
Q

Examples of Incretin-based therapy drugs

A

Dipeptidyl Peptidase 4 Inhibitors

Glucagon-like Peptide-1 Receptor Agonist

23
Q

Names of DPP-4 inhibitors

A

Sitagliptin
Vildagliptin
Linagliptin

24
Q

MOA of DPP-4 inhibitors

A

DPP-4 is an enzyme that degrades the incretin hormones (stimulated with meals) GLP-1 and GIP.

DPP-4 inhibitors prolong action of endogenous incretins

This stimulates pancreatic B-cells to raise glucose-stimulated insulin release

Suppress a-cell mediated glucagon release and hepatic glucose production.

25
Q

Uses of DPP-4 inhibitors

A

Intermediate glucose-lowering efficacy

Neutral effect on weight

Minimal risk of hypoglycaemia”

26
Q

ADR of DPP-4 inhibitors

A

GI issues - Diarrhoea, nausea, stomachache

Flu-like symptoms - headache, runny nose, sore throat

Skin reactions

Use with caution in patients with history of pancreatitis”

27
Q

Names of GLP-1 Receptor Agonist

A

Exenatide

Liraglutide

Semaglutide

28
Q

MOA of GLP-1 Receptor Agonists

A

Activate GLP-1 receptor in pancreatic beta cells.

Raise insulin release in presence of elevated glucose

This insulin secretion subsides as blood glucose concentrations fall and approach euglycaemia.

29
Q

Uses of GLP-1 Receptor Agonist

A

Reduces appetite and helps weight loss (esp liraglutide)

Cardiorenal effects - Cardioprotective, with evidence of fall in major CVS events, composite kidney outcome driven by macroalbuminuria

30
Q

ADR of GLP-1 Receptor Agonist

A

GI issues - nausea, vomiting, diarrhoea

31
Q

Name examples of SGLT2 Inhibitors

A

Empagliflozin
Canagliflozin
Dapagliflozin

32
Q

MOA of SGLT2 Inhibitors

A

SGLT2 is a low-affinity, high-capacity glucose transporter. Responsible for 90% of reabsorption of filtered glucose from tubular lumen.

Reduces renal tubular glucose reabsorption without stimulating insulin release.

Lowers renal threshold for glucose

Raise urinary glucose excretion.

33
Q

Uses of SGLT2 Inhibitors

A

Reduce major CVS events

Reduce overall CV death

Reduce risk of hospitalization for HF

Reduce risk of kidney outcomes

Favourable effects on lipids and weight too

34
Q

ADR of SGLT2 Inhibitors

A

UTI and increased urination

Female genital mycotic infections

Higher risk of lower limb amputation (Canagliflozin)

Diabetic ketoacidosis, esp euglycaemic DKA

Pharm (20 decks)

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