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Flashcards in oral hypoglycemics Deck (23)
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1
Q

biguanides

A

e.g. Metformin

  • MOA: decreases blood glucose levels: ↓s hepatic glucose production, ↓s intestinal absorption of glucose, improves insulin sensitivity [increases peripheral glucose uptake and utilization.]
  • SE: abdominal pain; GI disturbance; vomiting B12 deficiency/lactic acidosis (rare) + caution in patients with renal failure
2
Q

sulphonyureas

‘squeeze the pancreas’

A

Eg. Gliclazide ,Tolbutamide, Glipizide, Glibenclamide.

  • MOA: act by stimulating β cells of the pancreas to release insulin.
  • SE: hypoglycemia + weight gain.
3
Q

thiazolidinediones

A

–eg. Pioglitazone.

•MOA: enhances cellular responsiveness to insulin, increases insulin-dependent glucose disposal and improves hepatic sensitivity to insulin.

[Activate PPAR-gamma receptor in adipocytes to promote adipogenesis and fatty acid uptake]

SE: weight gain, fluid retention, cardiac failure and hepatotoxicity [rare]

4
Q

alpha- glucosidase inhibitors

A

e.g. Acarbose

•MOA: Intestinal α-glucosidase inhibitor: prevents breakdown of disaccharides thus delays carb absorption → ↓ post-prandial blood glucose

SE: Loose stools/diarrhoea, Abdo pain / bloating Hepatotoxicity (rare)

5
Q

Meglitinides: “-glinide”

‘squeezes pancreas’

A

e.g repaglinide, nateglinide

•MOA: lower blood glucose by stimulation of insulin release from the pancreas

SE: Abdominal pain; constipation; diarrhoea; nausea; vomiting

6
Q

SGLT 2 inhibitors: “-liflozin”

‘kidnaaaaaay’

A

eg. dapagliflozin, canagliflozin, empagliflozin

  • MOA: blocks the reabsorption of glucose in the kidneys and promotes excretion of excess glucose in the urine
  • Note that these treatments are of no use whatsoever in type I / insulin-dependent diabetes because no insulin is secreted.
  • SE: hypoglycemia, stomach upset
7
Q

Insulin secretagogues: DPP-4 inhibitor, “-gliptin”

A

e.g. sitagliptin, linagliptin

  • MOA:competitive and reversible dipeptidyl peptidase (DPP)-4 enzyme inhibitor that works via slowing degradation incretin hormones [which increase the production and release of insulin from pancreatic beta cells and decrease the release of glucagon from pancreatic alpha cells.]
  • SE: Cough; nasopharyngitis, pancreatitis [rare]
8
Q

Insulin secretagogues: GLP-1 analogue “-tide”

A

eg. Exenatide, liraglutide

  • MOA: functional analog of the human incretin Glucagon-Like Peptide-1 (GLP-1). Incretins enhance glucose-dependent insulin secretion and increases insulin secretion only in the presence of elevated plasma glucose levels, avoiding inappropriately high insulin levels during fasting.
  • SE: GI upset: diarrhea, heartburn, indigestion, nausea, and vomiting
9
Q

summary pic of oral hypoglycemics

A
10
Q

insulin MOA, SE, natural profile of secretion

A

MOA: see diagram

SEs: wt gain, hypoglycemia

Natural profile of insulin secretion consists of two components:

  • Basal insulin
  • Meal-time bolus insulin
11
Q

what are the main diff insulin types

A

ultra fast acting

short acting insulin

intermediate acting insulin

long acting recombinant human insulin analogues

pre-mixed insulin

12
Q

ultra fast acting, examples

A

HUMALOG/NOVORAPID

  • works rapidly to normalise blood sugar levels. It typically begins working after 10-20 minutes, lasts 3 -5 hours.
13
Q

short acting insulin

A

HUMULIN S/ VELOSULIN/HYPURIN NEUTRAL

–Short acting insulin is not as quick as rapid acting insulin

–Short acting insulins will usually be taken before meals.

–Short acting insulins may also be called regular or neutral insulin.

14
Q

intermediate acting insulin: isophane insulin

A

NOVOLIN/HUMULIN I

–often taken in conjunction with a short acting insulin. Intermediate acting insulins start to act within the first hour of injecting, followed by a period of peak activity lasting up to 7 hours.

15
Q

Long acting recombinant human insulin analogues

A

Insulin glargine eg. LANTUS

consistent activity from within an hour after injecting up to 24 hours.

Insulin determir eg. LEVEMIR

slightly shorter than Lantus and therefore it is often injected twice rather once daily.

Insulin degludec eg. TRESIBA

  • ultra-long acting insulin, duration of _more than 42 hour_s
  • offers more flexibility in terms of injection timings.
16
Q

premixed insulin

A

▫ NOVOMIX

–30% = short acting

–70% = long acting

17
Q

name diff types of insulin regimes

A
  • Regimen should suit patient’s lifestyle
  • Must change needle everyday
  • recommend to test at least 4 times a day, including before each meal and before bed

1.BD biphasic regimen

  • Twice daily premixed insulin
  • suitable in people who have a consistent day to day routine
  • may allow some flexibility for adjusting doses but not as much as a basal-bolus regimen

2.Basal bolus regimen

▫Before meals: ultra fast insulin

▫Before bed: long acting insulin

3.Once daily before bed long acting insulin

▫Useful when switching from tablets in T2DM

Insulin pumps [continuous SC insulin] used if can’t achieve target HbA1c despite careful mx/recurrent disabling hypoglycemia

18
Q

nice recommended insulin regime for T1DM

A
  • Multiple daily injection basal-bolus insulin regimens are recommended for adults with type 1 diabetes.
  • Non-basal-bolus insulin regimens (that is, twice-daily mixed [biphasic], basal-only, or bolus-only regimens) are not recommended for adults with newly diagnosed type 1 diabetes.

For basal insulin replacement:

twice-daily insulin detemir should be offered, unless:

  • The person is achieving their agreed target on an existing regimen, in which case that can be continued.
  • Twice-daily basal insulin injection is not acceptable to the person, in which case once-daily insulin glargine or insulin detemir can be considered.
  • Insulin detemir is not tolerated, in which case once-daily insulin glargine can be considered.
  • Other basal insulin regimens should be considered only if the recommendations above do not deliver agreed targets. The person’s preferences and acquisition cost should be considered when an alternative insulin regimen is being decided.

For bolus/mealtime insulin replacement:

  • A rapid-acting insulin analogue injected before meals is recommended, rather than rapid-acting soluble human or animal insulins.
  • The routine use of rapid-acting insulin analogues after meals should be discouraged.
  • If the person has a strong preference for an alternative mealtime insulin, they should be offered their preferred insulin.
19
Q

nice recommended insulin regime for T2DM

A

Starting insulin

  • metformin should be continued. In terms of other drugs NICE advice: ‘Review the continued need for other blood glucose lowering therapies’
  • NICE recommend starting with human NPH insulin (isophane, intermediate acting) taken at bed-time or twice daily according to need
20
Q

DVLA + DM rules

A

Until recently people with diabetes who used insulin could not hold a HGV licence.

The DVLA changed the rules in October 2011. The following standards need to be met (and also apply to patients using other hypoglycaemic inducing drugs such as sulfonylureas):

  • there has not been any severe hypoglycaemic event in the previous 12 months
  • the driver has full hypoglycaemic awareness
  • the driver must show adequate control of the condition by regular blood glucose monitoring*, at least twice daily and at times relevant to driving
  • the driver must demonstrate an understanding of the risks of hypoglycaemia
  • here are no other debarring complications of diabetes

From a practical point of view patients on insulin who want to apply for a Group 2 (HGV) licence need to complete a VDIAB1I form.

Other specific points for group 1 drivers:

  • if on insulin then patient can drive a car as long as they have hypoglycaemic awareness, not more than one episode of hypoglycaemia requiring the assistance of another person within the preceding 12 months and no relevant visual impairment. Drivers are normally contacted by DVLA
  • if on tablets or exenatide no need to notify DVLA. If tablets may induce hypoglycaemia (e.g. sulfonylureas) then there must not have been more than one episode of hypoglycaemia requiring the assistance of another person within the preceding 12 months
  • if diet controlled alone then no requirement to inform DVLA

*to demonstrate adequate control, the Secretary of State’s Honorary Medical Advisory Panel on Diabetes Mellitus has recommended that applicants will need to have used blood glucose meters with a memory function to measure and record blood glucose levels for at least 3 months prior to submitting their application

21
Q

other adverse SEs of insulin

A
  • Altered vision (uncommon) — on initiation of insulin treatment, altered vision may occur if blood glucose levels change markedly.
    • Reassure the person that this is usually temporary.
    • Advise the person to avoid changing their glasses until their blood glucose levels have stabilized.
  • Acute painful neuropathy resulting from rapid improvement of blood glucose control — rapid improvement in blood glucose control can lead to acute symptomatic neuropathy.
    • Reassure the person that this is a self-limiting condition that improves symptomatically over time.
    • Explain that the specific treatments for this condition:
      • Aim to make the symptoms tolerable until the condition resolves.
      • May not relieve pain immediately and may need to be taken regularly for several weeks to be effective.
    • Advise the use of simple analgesics (paracetamol or a nonsteroidal anti-inflammatory drug [NSAID] if indicated) and local measures (such as a bed cradle [a frame that attaches to the bed to keep sheets and blankets from touching and rubbing the body]) to relieve symptoms.
      • If simple analgesics are ineffective, offer treatment as described in the CKS topic on Neuropathic pain – drug treatment.
      • Simple analgesia may be continued until the effects of additional treatments have been established.
      • The use of weak opioids is not recommended due to the risk of dependency associated with their use.
    • Do not relax diabetes control if this condition is identified.
  • Insulin oedema (rare) — this occurs mostly in people with poor glucose control and progressive weight loss who are treated with relatively high doses of insulin.
    • Reassure the person that the oedema should resolve within 3–4 days after reduction of the insulin dose. Treatment with a diuretic is not indicated.
    • Consider other causes of oedema, for example heart failure — see the CKS topic on Heart failure - chronic.
22
Q

GLP-1 analogues eg. exenatide rules

A

Glucagon-like peptide-1 (GLP-1) mimetics (e.g. exenatide)

  • Exenatide is an example of a glucagon-like peptide-1 (GLP-1) mimetic.
  • These drugs increase insulin secretion and inhibit glucagon secretion.
  • One of the major advances of GLP-1 mimetics is that they typically result in weight loss, in contrast to many medications such as insulin, sulfonylureas and thiazolidinediones.

Exenatide must be given by subcutaneous injection within 60 minutes before the morning and evening meals. It should not be given after a meal.

Liraglutide is the other GLP-1 mimetic currently available. One the main advantages of liraglutide over exenatide is that it only needs to be given once a day.

Both exenatide and liraglutide may be combined with metformin and a sulfonylurea. Standard release exenatide is also licensed to be used with basal insulin alone or with metformin.

NICE state the following:

Consider adding exenatide to metformin and a sulfonylurea if:

  • BMI >= 35 kg/m² in people of European descent and there are problems associated with high weight, or
  • BMI < 35 kg/m² and insulin is unacceptable because of occupational implications or weight loss would benefit other comorbidities.

NICE like patients to have achieved a 11 mmol/mol (1%) reduction in HbA1c and 3% weight loss after 6 months to justify the ongoing prescription of GLP-1 mimetics.

The major adverse effect of GLP-1 mimetics is nausea and vomiting. The Medicines and Healthcare products Regulatory Agency has issued specific warnings on the use of exenatide, reporting that is has been linked to severe pancreatitis in some patients.

23
Q

Dipeptidyl peptidase-4 (DPP-4) inhibitors (e.g. Vildagliptin, sitagliptin)

A
  • oral preparation
  • trials to date show that the drugs are relatively well tolerated with no increased incidence of hypoglycaemia
  • do not cause weight gain

NICE guidelines on DPP-4 inhibitors

NICE suggest that a DPP-4 inhibitor might be preferable to a thiazolidinedione if further weight gain would cause significant problems, a thiazolidinedione is contraindicated or the person has had a poor response to a thiazolidinedione