Insulin And Oral Hypoglycemics Flashcards by Yazan adnan

What are the insulin responsive cells

Muscle cells and adipose tissue

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What is the glucose transporter

GLUT 4

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What happens in TYPE 1 diabetes mellitus your

Autoimmune destruction of beta cells in the pancreas by T cells due to eliminated self tolerance

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What is type 2 diabetes mellitus

Insulin resistance in peripheral cells hence the pancreas will make even more insulin and over time it will get over worked causing beta cells to atrophy

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When is exogenous insulin given in type 2 diabetes

Later in the disease

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When is exogenous insulin given in type 1 diabetes

Immediately since the pancreas can’t make insulin anymore

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Whats the quickest area of absorption of insulin

1-abdomen
2-arms 
3-buttocks
4-thighs 
Closest to the pancreas the faster!

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What are insulin preparations categorised by

Onset of action and duration

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What are Rapid acting / short acting insulin

Bolus=prandial

Bolus insulin regimen—>given before meals to counter post meal increase in blood glucose

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What are intermediat acting and long acting insluins

They are basal (fasting) insulin regimen—> to maintain steady level given 1 or 2 times a day to regulate fasting blood glucose

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What drugs are inhibitors of insulin release

Somatostatin and a2 stimulation

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What happens when insulin drops

Lipolysis increases—> leading to increase in production of ketone which could lead to ketoacidosis

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Symptoms of ketoacidosis

Acetone breath, abonormal respiration and electrolyte depletion (vomiting, come and death)

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What is the only insulin given IV

Regular / human insulin

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Why is human insulin given iv

Produced and stored as a hexamer to remain stable within the body

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Normal insulin onset and duration

30 mins
5-8 hours
Peak 3-4 hrs

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What are the rapid acting insulin

LAG
Lispro
Aspart
Glulisine

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Rapid acting insulins duration, onset and peak

5-15 mins
3-4 hrs
1hr is the peak

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When is rapid acting insulin used

Injected before a meal

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What’s the insulin of choice for diabetic ketoacidosis

Rapid acting insulin

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Which insulin’s are used in insulin’s pumps

Rapid acting insulin

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Whats an intermediate acting insulin

NPH - isophane

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What are NPH and regular insulins

They are human insulins the rest are analogs

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NPH onset, duration and peak

1-2 hours
10-16 hours
Peak 4-13 hours

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What can NPH be used as

Can be used as basal insulin

What’s the concentration of most commercial insulin preparations

100 U/ml

What are the long acting insulins

Glargine, detemir (has a flat peak) and degludec

Which long acting insulin binds to albumin

Detemir

Long acting insulins onset , duration and peak

1-2 hours Glargine 24 hrs Detemir 20 hrs No peak effect for glargine

Which insulin can’t be mixed with other insulins in one syringe

Glargine

Long acting insulins side effects

Hypoglycaemia Lipodystrophy Weight gain

Where are endogenous and injected insulins metabolised

Endogenous insulin - 60% in liver and 40% in kidney | Injected insulin - 60% kidney and 40% liver

Sulfonylurea mode of administration

Oral

Sulfonylurea mechanism of action

- It works like ATP in pancreas work similarly to ATP leading to depolarisation by closing k+ channels - decreases hepatic gluconeogenesis - increase peripheral insulin sensitivity

1st generation sulfonylurea

Chlorpropamide Tolbutamide Tolazamide

2nd generation sulfonylurea

Glipizide, glyburide and glimeperide (3rd gen)

Difference between first and second generation sulfonylurea

2nd generation is more potent and common

What glucose concentration are Sulfonylureas used for

Any glucose concentration since it secretes insulin regardless

Which oral hypoglycaemic drugs have the highest risk of hypoglycaemia

Sulfonylurea

Side effects of sulfonylurea

``` Hypoglycaemia Weight gain GI disturbances (nausea) Allergic reactions (SJS) Photosensitivity ```

1st generation sulfonylurea side effects

Disulfram like reaction (alcohol intolerance giving hangover like symptoms)

Sulfonylurea contraindications

DKA and DM1

Meglitinides mode of administration

Oral

Meglitinides mechanism of action

Prevent K+ channels from opening

List the meglitinides and their onset time

Repaglinide 30 mins | Nateglinide 10 mins

Meglitinides vs sulfonylurea

Meglitinides work faster but for shorter time than sulfonylurea

When are meglitinides taken

Taken before meals

Meglitinides side effects

Weight gain | Hypoglycaemia

What are incertins

Hormones which stimulate insulin release after a meal like GLP1 , which only gets released on an increase in glucose level to release insulin and inhibits glucagon release

What oral hypoglycaemics are glucose dependent

Incertins

List the GLP 1 receptor agonists

Exenatide and liraglutide

GLP1 agonists mode of administration

Subcutaneous

GLP1 agonist suffix

TIDE

GLP 1 agonist Mechanism of action

Increase insulin secretion Decrease glucagon release Enhance satiety

GLP 1 agonist adverse effects

GI disturbances Drop in appetite Increase in risk for acute pancreatitis Weight loss

Best drug for weight loss

GLP 1 agonists

List the DPP 4 inhibitors

Sitagliptin | Saxagliptin (orally)

DPP 4 inhibitors mechanism of action

They inhibit DPP-4 which is a protease which breaks down GLP-1 Same effect as incertins

DPP4 side effects

GI disturbances Headache NASOPHARYNGITIS mild respiratory and urinary infections

Which diabetes drugs have beneficial CV effects

GLP1 (LIRAGLUTIDE and SEMAGLUTIDE) | SGLT-2 inhibitor (EMPAGLIFLOZIN)

DPP4 inhibitors are contraindicated in which people

Hepatic and renal impairments | Teratogenic-pregnant women

What’s the mechanism of action biguanides and thiazolidinediones

Increase insulin sensitivity | Decrease production of glucose

List Biguanides

Metformin first line drug for type 2 diabetes

Metformin mechanism of action

- Inhibits hepatic gluconeogenesis - Increases GLUT4 receptors in the cell membrane - Decreases intestinal absorption of glucose

Metformin side effects

GI disturbances Weight gain Lactic acidosis

Metformin is contraindicated in who

Patients with renal dysfunction Hepatic dysfunction COPD In low vit B12

What does metformin cause to vitamin B12

Decreases it

List the thiazolidinediones

Rosiglitazone | Pioglitazone

Rosiglitazone and Pioglitazone mechanism of action

They are insulin sensitisers increasing sensitivity as they bind to PPAR GAMMA which increases the transcription of insulin responsive genes and decreases hepatic gluconeogenesis

Thiazolidinediones side effects

Increase risk of cardiovascular events MI AND STROKE | Fluids retention causing edema

Pioglitazone side effects

Increases the risk of bladder cancer and increases risk of osteopenia and fractures and liver failure

List alpha glycosides inhibitors

Acarbose and miglitol

alpha glycosides inhibitors mechanism of action

Delay breakdown of starch and carbohydrates to glucose hence it decrease post meal glucose

alpha glycosides inhibitors side effects

GI disturbances

List Synthetic amylin analogs

Pramlintide - injectable

What is amylin

A hormone secreted by B cells alongside insulin

Synthetic amylin analogs mechanism of action

Lowers blood glucose by delaying gastric emptying and inhibiting glucagon secretion and improving satiety

What is the only drug other than insulin used for both DM1 and DM2

Synthetic amylin analogs which is PRAMLINTIDE

list SGLT2 Inhibitors

Canagliflozin Dapagliflozon Suffix - gliflozin

SGLT 2 inhibitors

Decrease glucose concentration and decrease HBA1C concentration

What is SGLT 2

It’s a transporter in the kidney which accounts for 90% of absorbed glucose Blocking it causes glucosuria

SGLT2 inhibitors side effects

It causes glucosurea which leads to UTIs and genital infections