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Pharmacology > 15 The control of blood glucose and drug treatment of diabetes mellitus > Flashcards

15 The control of blood glucose and drug treatment of diabetes mellitus Flashcards

1
Q

15.01 INSULIN

Human recombinant insulin (or analogues) - actions

A

promotes tissue uptake and storage of glucose, amino acids and fats
acutely lowers blood glucose
inhibits hepatic glycogenolysis and gluconeogenesis
inhibits lipolysis
increases glycogen synthesis in muscle/liver
stimulates protein synthesis
longer-term effects on growth and gene expression

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2
Q

15.01 INSULIN

Human recombinant insulin (or analogues) - MOA

A

binding to its receptor (tyrosine kinase type) causes autophosphorylation of the receptor
subsequent tyrosine phosphorylation of ‘insulin receptor substrates’ leads to activation of SH2 domain proteins, which regulate the action of various intracellular enzymes and cell membrane glucose transporters

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3
Q

15.01 INSULIN

Human recombinant insulin (or analogues) - abs/distrib/elim

A

free insulin in the blood has a half-life of only 10 min so slow-release preparations are needed for regular use
given SC or IV
short-acting (3-5h): soluble (regular) insulin, insulin lispro, insulin aspart
intermediate-acting (10-12h): isophane insulin
long-acting (24h): insulin zinc suspension (crystalline), insulin glargine or detemir

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4
Q

15.01 INSULIN

Human recombinant insulin (or analogues) - clinical use

A

life-long treatment of type 1 diabetes
also for type 2 diabetes not controlled by oral hypoglycaemic agents
soluble insulin also for emergency IV treatment of diabetic ketoacidosis

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5
Q

15.01 INSULIN

Human recombinant insulin (or analogues) - adverse effects

A

hypoglycaemia - treated by glucose administration (by mouth, if conscious, otherwise IV or glucagon (IM))
weight gain (mainly in type 2 diabetes)

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6
Q

15.02 SULFONYLUREAS

Gliclazide, tolbutamide, glipizide, glimepiride, glibenclamide - actions

A

increase insulin release from functioning β-cells, thus producing the effects of insulin

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7
Q

15.02 SULFONYLUREAS

Gliclazide, tolbutamide, glipizide, glimepiride, glibenclamide - MOA

A

interaction with the sulfonylurea receptor (a subunit of the KATP channel in the cell membrane of β-cells) causes the K+ channel to close
this causes the cell to depolarise and activates voltage-dependent Ca2+ channels
Ca2+ entry stimulates exocytosis of insulin

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8
Q

15.02 SULFONYLUREAS

Gliclazide, tolbutamide, glipizide, glimepiride, glibenclamide - abs/distrib/elim

A

given orally, they bind extensively to plasma proteins
half-lives: tolbutamide 4h, glipizide 4h, glimepiride 5h, glibenclamide 10h
actions prolonged in patients with renal disease

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9
Q

15.02 SULFONYLUREAS

Gliclazide, tolbutamide, glipizide, glimepiride, glibenclamide - clinical use

A

type 2 diabetes mellitus, effective in 30% of patients

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10
Q

15.02 SULFONYLUREAS

Gliclazide, tolbutamide, glipizide, glimepiride, glibenclamide - adverse effects

A

association with cardiovascular disease and hypoglycaemia
weight gain

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11
Q

15.03 BIGUANIDES

Metformin - actions

A

lowers blood glucose concentration

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12
Q

15.03 BIGUANIDES

Metformin - MOA

A

inhibits gluconeogenesis in the liver by activating AMP-activated protein kinase
may also enhance tissue sensitivity to insulin
increases glucose uptake into tissues

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13
Q

15.03 BIGUANIDES

Metformin - abs/distrib/elim

A

given orally
half-life 3h
mostly excreted unchanged in urine (avoid in patients with renal insufficiency)

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14
Q

15.03 BIGUANIDES

Metformin - clinical use

A

type 2 diabetes (alone or with other oral hypoglycaemic agents)
particularly useful in obese patients

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15
Q

15.03 BIGUANIDES

Metformin - adverse effects

A

anorexia and GI upset including diarrhoea (leading to weight loss)
may rarely cause potentially fatal lactic acidosis
unlike sulfonylureas, does not cause hypoglycaemia

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16
Q

15.04 MEGLITINIDES

Repaglinide, nateglinide - actions

A

lowers blood glucose concentration
stimulates insulin release from β-cells in pancreatic islets

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17
Q

15.04 MEGLITINIDES

Repaglinide, nateglinide - MOA

A

similar to sulfonylureas
interaction with the sulfonylurea receptor, which is a subunit of the KATP channel in the cell membrane of B cells, causes the K+ channel to close
this causes the cell to depolarise and activates voltage-dependent Ca2+ channels
Ca2+ entry stimulates exocytosis of insulin

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18
Q

15.04 MEGLITINIDES

Repaglinide, nateglinide - abs/distrib/elim

A

quick onset and short duration of action
half-lives: repaglinide 1h, nateglinide 1.5h
(its actions can be reduced by drugs that induce hepatic P450 enzymes, e.g. carbamazepine)

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19
Q

15.04 MEGLITINIDES

Repaglinide, nateglinide - clinical use

A

type 2 diabetes mellitus
rapid action allows good control of postprandial hyperglycaemia
may be combined with metformin or a glitazone
mainly metabolised in liver, so useful in patients with renal insufficiency

20
Q

15.04 MEGLITINIDES

Repaglinide, nateglinide - adverse effects

A

hypoglycaemia (uncommon unless its metabolism is inhibited by other drugs, e.g. gemfibrozil)

21
Q

15.05 GLUCAGON-LIKE PEPTIDE-1 AGONISTS

Exenatide, liraglutide, lixisenatide, dulaglutide, albliglutide - actions

A

lowers blood glucose after a meal by increasing insulin secretion, suppressing glucagon secretion and slowing gastric emptying

22
Q

15.05 GLUCAGON-LIKE PEPTIDE-1 AGONISTS

Exenatide, liraglutide, lixisenatide, dulaglutide,
albliglutide - MOA

A

glucagon-like peptide-1 (GLP-1) is secreted by L cells which are widely distributed in the gut, including in the ileum and colon as well as more proximally
release of gastric inhibitory polypeptide (GIP) and GLP-1 in response to ingested food provides an early stimulus to insulin secretion before absorbed glucose or other products of digestion reach the islet cells in the portal blood
GLP-1 also inhibits pancreatic glucagon secretion and slows the rate of absorption of digested food by reducing gastric emptying
it is also implicated in control of food intake via appetite and satiety

23
Q

15.05 GLUCAGON-LIKE PEPTIDE-1 AGONISTS

Exenatide, liraglutide, lixisenatide, dulaglutide, albliglutide - abs/distrib/elim

A

given via SC injection either daily or weekly (dulaglutide, albliglutide)
half lives: exenatide 2.4h, liraglutide 13h, lixisenatide 3h, dulaglutide 4.5 days, albiglutide 5 days

24
Q

15.05 GLUCAGON-LIKE PEPTIDE-1 AGONISTS

Exenatide, liraglutide, lixisenatide, dulaglutide, albliglutide - clinical use

A

type 2 diabetes mellitus, alone or in combination with other drugs
liraglutide is approved for treatment of obesity

25
Q

15.05 GLUCAGON-LIKE PEPTIDE-1 AGONISTS

Exenatide, liraglutide, lixisenatide, dulaglutide, albliglutide - adverse effects

A

nausea and diarrhoea
acute pancreatitis, rapid weight loss, hypoglycaemia (especially when used in combination with sulfonylureas)

26
Q

15.06 DIPEPTIDYL PEPTIDASE INHIBITORS

Sitagliptin, saxagliptin, vildagliptin, linagliptin, alogliptin - actions

A

lowers blood glucose by inhibiting dipeptidylpeptidase-4 (DPP-4)

27
Q

15.06 DIPEPTIDYL PEPTIDASE INHIBITORS

Sitagliptin, saxagliptin, vildagliptin, linagliptin, alogliptin - MOA

A

competitively inhibit DPP-4, thereby lowering blood glucose by potentiating endogenous incretins (GLP-1 and GIP) which stimulate insulin secretion

28
Q

15.06 DIPEPTIDYL PEPTIDASE INHIBITORS

Sitagliptin, saxagliptin, vildagliptin, linagliptin, alogliptin - abs/distrib/elim

A

absorbed from the gut and administered once daily orally
eliminated partly by renal excretion and also metabolised by cytochrome P450 enzymes
half-lives: sitagliptin 12h (mainly renal clearance), saxagliptin 2-3h, vildagliptin 3h

29
Q

15.06 DIPEPTIDYL PEPTIDASE INHIBITORS

Sitagliptin, saxagliptin, vildagliptin, linagliptin, alogliptin - clinical use

A

type 2 diabetes mellitus in addition to other oral hypoglycaemic drugs

30
Q

15.06 DIPEPTIDYL PEPTIDASE INHIBITORS

Sitagliptin, saxagliptin, vildagliptin, linagliptin, alogliptin - adverse effects

A

heart failure (particularly saxagliptin or alogliptin), liver disease, GI adverse effects, pancreatitis
concern they may act as tumour promoters

31
Q

15.07 SGLT-2 INHIBITORS

Canagliflozin, dapagliflozin, empagliflozin - actions

A

reduce concentration of circulating glucose by promoting glucose excretion into the urine

32
Q

15.07 SGLT-2 INHIBITORS

Canagliflozin, dapagliflozin, empagliflozin - MOA

A

act by promoting glucose excretion into the urine, thereby reducing the concentration of circulating glucose
the resulting glycosuria is associated with an osmotic diuresis and salt excretion

33
Q

15.07 SGLT-2 INHIBITORS

Canagliflozin, dapagliflozin, empagliflozin - abs/distrib/elim

A

rapidly absorbed, with time to peak plasma concentrations of less than 2h
they are highly bound to plasma proteins (>80%)

34
Q

15.07 SGLT-2 INHIBITORS

Canagliflozin, dapagliflozin, empagliflozin - clinical use

A

type 2 diabetes mellitus - either alone (when metformin is inappropriate) or in combination with insulin or other oral hypoglycaemic agents

35
Q

15.07 SGLT-2 INHIBITORS

Canagliflozin, dapagliflozin, empagliflozin - adverse effects

A

significant increase in the risk of urinary tract and fungal infections such as candidal vaginitis or balanitis
susceptibility to diabetic ketoacidosis, volume depletion, fractures, acute renal impairment and lower limb amputations

36
Q

15.08 α-GLUCOSIDASE INHIBITORS

Acarbose, miglitol - actions

A

delay carbohydrate absorption from intestine

37
Q

15.08 α-GLUCOSIDASE INHIBITORS

Acarbose, miglitol - MOA

A

inhibits intestinal α-glucosidase and pancreatic α-amylase so reduces the rise in blood glucose which follows a meal
α-glucosidase is the enzyme responsible for breaking down starches and oligosaccharides to yield the absorbable monosaccharides

38
Q

15.08 α-GLUCOSIDASE INHIBITORS

Acarbose, miglitol - abs/distrib/elim

A

metabolised in GIT by bacteria and digestive enzymes
half-life 2h

39
Q

15.08 α-GLUCOSIDASE INHIBITORS

Acarbose, miglitol - clinical use

A

type 2 diabetes mellitus not controlled by other drugs

40
Q

15.08 α-GLUCOSIDASE INHIBITORS

Acarbose, miglitol - adverse effects

A

GI discomfort - flatulence, diarrhoea

41
Q

15.09 GLUCAGON

Human recombinant glucagon - actions

A

elevates blood glucose concentration
increases rate and force of heart contraction

42
Q

15.09 GLUCAGON

Human recombinant glucagon - MOA

A

glucagon activates adenylate cyclase by acting on G protein-coupled receptors linked to Gs
its actions thus mimic those of adrenaline-activating β adrenoceptors
it elevates blood glucose by stimulating hepatic gluconeogenesis and glycogenolysis and by inhibiting glycogen synthesis

43
Q

15.09 GLUCAGON

Human recombinant glucagon - abs/distrib/elim

A

glucagon is a peptide hormone - must be given by injection
plasma half-life 5 min

44
Q

15.09 GLUCAGON

Human recombinant glucagon - clinical use

A

emergency treatment of hypoglycaemia (caused by insulin overdose), when oral or IV glucose administration is not possible
(also used to treat heart failure precipitated by α-adrenoceptor antagonists)

45
Q

15.09 GLUCAGON

Human recombinant glucagon - adverse effects

A

uncommon
cardiac stimulation in patients taking β blockers or with pheochromocytoma

Pharmacology (34 decks)

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