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Diabetes > Medications > Flashcards

Medications Flashcards

1
Q

For sulphonylureas to be used, there should be some

A

residual number of β-cells

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2
Q

Which generation of sulphonylurea is preferred in diabetes ?

A

2nd generation

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3
Q

1st generation sulphonylureas

A

Chlorpropamide,
Tolbutamide,
Tolazamide,
Acetohexamide.

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4
Q

2nd generation sulphonylureas include

A

Glipizide,
Glibenclamide,
Glimepiride, and
Gliclazide.

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5
Q

MOA of sulphonylureas

A

They Inhibit K+-ATPase and hence closes K+channels in the β-cells. This leads to an influx of Ca2+ into the β-cells and this causes the release of insulin.

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6
Q

All sulphonylureas are metabolized in the

A

liver

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7
Q

Sulphonylureas have different excretion profiles

A

different excretion profiles

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8
Q

Which Sulphonylureas undergo Hepatic excretion

A

Glipizide and Gliclazide

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9
Q

Glibenclamide undergoes

A

40% hepatic excretion and 60% biliary excretion

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10
Q

SE of Sulphunlyureas

A

Weight gain
• Hypoglycemia
• Hyponatremia
• GI upset

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11
Q

How does Hyponatremia in Sulphunlyureas come about?

A

There is an increased sensitivity of ADH which dilutes the
system

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12
Q

INSULIN concentration in the plasma is higher WHEN GIVEN

A

Oral than when glucose is given through the IV route. Due to incretin hormones

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13
Q

Dpp4 inhibitors are also called

A

Incretins

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14
Q

The types of incretin hormones

A

Glucagon-like peptide-1 (GLP-1) and Gastric inhibitory polypeptide/Glucose-dependent insulinotropic peptide (GIP)

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15
Q

MOA of DPP4 INHIBITORS

A

DPP4 (Dipeptidyl peptidase 4) are enzymes that break down incretins, thereby, inhibition of DPP4 prolongs or preserves incretins.

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16
Q

Examples of DPP4 INHIBITORS

A

Vildagliptin,
Sitagliptin
Saxagliptin

17
Q

Gliptins or DPP4 inhibitors are metabolised by

A

Liver - CYP3A4 and CYP3A5.

18
Q

CYP3A4 and CYP3A5 are used in the metabolism of DPP4 inhibitors

A

Such medications include enzyme
inhibitors (e.g. Ketoconazole, Itraconazole, Voriconazole, Fluoxetine, Cimetidine, Clarithromycin, Erythromycin, etc.) and enzyme inducers (Phenytoin, Rifampicin, Carbamazepine, Phenobarbital, Barbiturates, Glucocorticoids, etc.)

19
Q

Galvus Met

A

(Vildagliptin + Metformin

20
Q

Contraindications of gliptins

A

•History of pancreatitis
• Type 1 diabetes or DKA
• Severe renal impairment
• Heart failure
• Hepatic impairment
• Hypersensitivity to the drug

21
Q

SE OF DPP4 INHIBITORS

A

GI disturbances
• Upper respiratory infections
• Acute pancreatitis
• Sitagliptin causes weight loss
• Nasopharyngitis
• Diarrhea
• Peripheral edema

22
Q

Sitagliptin causes

A

weight loss

23
Q

MOA of incretins

A

These medications mimic the incretins. They bind and activate incretin receptors and aid in insulin secretion. They activate the GLP-1.

24
Q

Examples of Incretin mimetics GLP-1

A

Exenatide
Liraglutide.

25
Q

Action of the mimetics is more

A

prolonged than that of the endogenous
incretins

26
Q

Between DPP4 and incretin Mimetics which is more effective?

A

DPP4 inhibitors will tend to be more effective than incretin mimetics. This is because DPP4 inhibitors stop the action of
DPP4 enzymes hence preventing the breakdown of incretins. However, when incretin mimetics are taken, there would
still be DPP4 enzymes in the system to break them down

27
Q

Contraindications of incretin mimetics

A

•Diabetic ketoacidosis
• Severe gastrointestinal disease
• Inflammatory bowel disease
• Diabetic gastroparesis

28
Q

Thiazolidinediones are agonists at the PPAR-γ receptor.

A

Peroxisome proliferator-activated receptor gamma (PPAR-γ or PPARG) found in adipose tissues, pancreatic β-cells, vascular
endothelium, and macrophages.

29
Q

when PPAR-γ is stimulated,

A

fat is utilized in the periphery and this increases insulin sensitivity.

30
Q

The anaemia caused by this Pioglitazone is termed

A

Dilutional anaemia

31
Q

Contraindications of Pioglitazone

A

History of heart failure
• Previous or active bladder cancer
• Uninvestigated macroscopic
haematuria

Diabetes (3 decks)

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