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Pharmacology > Antidiabetics 2 > Flashcards

Antidiabetics 2 Flashcards

1
Q

list the Non-insulin Antidiabetic Agents

A
  • Insulin Secretagogues
  • Biguanides
  • Thiazolidinediones (TZDs)
  • alpha-Glucosidase Inhibitors
  • Incretin Analogs
  • Inhibitors of DPP-IV
  • Amylin Analogs
  • Bile-Acid Sequestrants
  • SGLT2 Inhibitors
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2
Q

Sulfonylureas overview and moa?

A

• Effective at reducing fasting plasma glucose
(FPG) and HbA1C.

MOA
• Stimulate insulin release from beta cells: bind to the
SUR1 subunit and block the ATP-sensitive K+
channel in the beta cell membrane

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3
Q

First-generation Sulfonylureas example and overview, ae, and contraindication?

A

Chlorpropamide
• Long half-life.
• Hypoglycemia is common, particularly in elderly
patients. Contraindicated in elderly patients.
• Hyperemic flush when alcohol is ingested. Mainly
due to inhibition of aldehyde dehydrogenase.
• Chlorpropamide may potentiate action of
vasopressin and elicit an apparent syndrome of
inappropriate secretion of ADH (SIADH).

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4
Q

list three Second Generation Sulfonylureas, Differences between first and second generation?

A

• Glyburide (Glibenclamide)
• Glipizide
• Glimepiride
• Much more potent that first-generation agents.
• Lack some of the adverse effects and drug
interactions of first-generation agents.
• Have largely replaced first-generation agents.

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5
Q

How often do 2nd generation sulfonylureas cause hypoglycemia?

A

Glyburide
• Causes hypoglycemia in 20-30% of users.
Glipizide
• Short half-life. Less likely to cause hypoglycemia.
Causes hypoglycemia in 10-15% of users.
Glimepiride
• Causes hypoglycemia in only 9-14% of users.
Approved for once-daily use.

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6
Q

Sulfonylureas: Adverse Effects?

A
  • Hypoglycemia

* Weight gain

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7
Q

name 2 Meglitinides and their moa?

A

• Repaglinide
• Nateglinide
• Stimulate insulin release by binding to SUR1
and inhibiting ATP-sensitive K+ channel.
• Not as effective as sulfonylureas in reducing
FPG and HbA1C levels.

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8
Q

Meglitinides pk and dosing?

A

• In contrast with sulfonylureas, the meglinitides have a rapid onset and short duration of
action.
• They are postprandial glucose regulators.
• They must be taken before each meal; if the
meal is missed the drug must be omitted.

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9
Q

Meglitinides: Adverse Effects?

A

• Repaglinide: hypoglycemia.
• Nateglinide: less risk of hypoglycemia.
• Both: Weight gain.
• Meglitinides contain no sulfur. They may be
indicated for patients with sulfur or sulfonylurea
allergy.

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10
Q

What biguanide is currently available and overivew?

A

• Only currently available biguanide.
• Does not cause insulin secretion.
• Generally does not cause hypoglycemia, even in
large doses.
• Equivalent to sulfonylureas in reducing FPG and
HbA1C levels.

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11
Q

Metformin MOA?

A

• Metformin reduces glucose levels primarily by
inhibiting gluconeogenesis.
• Metformin inhibits gluconeogenesis by reducing
gene expression of gluconeogenic enzymes.
• Additionally, metformin increases insulin mediated
glucose utilization in muscle and liver.
• As a result of the improvement in glycemic
control, serum insulin concentrations decline
slightly.
• At the molecular level, these actions are mediated
at least in part by activation of AMP-activated
protein kinase (AMPK).

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12
Q

Metformin: Other Effects?

A
  • Reduces plasma TG by 15-20%.

* Decreases body weight.

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13
Q

Metformin: Indications?

A

• The American Diabetes Association (ADA)
recommends that metformin should be the
first-line agent in type 2 DM

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14
Q

Metformin: Adverse Effects?

A

• Largely GI: anorexia, nausea, vomiting,
abdominal discomfort, diarrhea.
• Long term use may interfere with B12
absorption.
• Small risk of potentially fatal lactic acidosis.
• Contraindicated in patients with renal disease,
hepatic disease, hypoxia, or alcoholism.

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15
Q

Thiazolidinediones (TZDs) examples and overview?

A

• Pioglitazone
• Rosiglitazone
• Decrease insulin resistance.
• Agonists of peroxisome proliferator-activated
receptor-gamma (PPAR-gamma).
• Intracellular receptors found in muscle, fat and
liver.

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16
Q

Thiazolidinediones (TZDs) moa, pk, and efficacy?

A

• In diabetic patients glitazones promote glucose uptake and utilization in adipose tissue.
• Less effective than sulfonylureas and metformin in decreasing FPG and HbA1C levels.
• Their mechanism of action involves gene
regulation.
• Glitazones have a slow onset and offset of
activity over weeks or even months.

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17
Q

Thiazolidinediones (TZDs) effect on lipids

A

• The effects on lipids of pioglitazone are more
favourable than those of rosiglitazone.
• Compared with rosiglitazone, pioglitazone is associated with significant improvements in:
• HDL
• TG
• LDL particle concentration
• LDL particle size

18
Q

TZDs AE?

A

• Cause fluid retention, weight gain and edema.
• Cause or exacerbate CHF in some patients.
• Contraindicated in patients with Class III or IV
heart failure.
• In 2010 the FDA restricted use of rosiglitazone.
• In 2014, after revaluation of the data, the FDA
removed the restrictions placed on rosiglitazone.

19
Q

Troglitazone AE?

A

• Troglitazone was the first thiazolidinedione to be
approved.
• It caused severe hepatic toxicity and was
withdrawn.
• As a consequence, the FDA requires
monitoring of liver function with Tzd therapy.
• So far pioglitazone or rosiglitazone have not
been associated with hepatotoxicity.

20
Q

acarbose belong to what class and moa?

A

alpha-glucosidase inhibitors

Competitive inhibitor of
intestinal alpha-glucosidases.

• Reduces postprandial digestion of starch and
disaccharides.
• Minimizes upper intestinal carbohydrate
absorption and defers absorption to the distal
small intestine.
• This decreases postprandial hyperglycemia and
hyperinsulinemia.
• Evokes modest drop in HbA1C and FPG levels.

21
Q

Acarbose: Adverse Effects?

A

• Flatulence, diarrhea, abdominal pain.
• Contraindicated in IBS or any intestinal condition
worsened by gas and distension.
• Acarbose is associated with reversible hepatic
enzyme elevation.
• Periodical liver function monitoring is
required with acarbose therapy.

22
Q

Overview of Incretin Analogs:

A 
Exenatide
• Analog of glucagon like-polypeptide 1 (GLP-1).
• Derived from the
salivary gland of the
Gila monster. 
• Injectable.
• Full agonist at human GLP-1 receptors.
• Resistant to dipeptidyl peptidase IV (DPP-IV)
23
Q

Describe the Incretin Effect?

A

• Incretins, released
by the gut, enhance
insulin secretion.

Glucose in gut lumen stimulates incretin secretion

Incretins enhance glucose-stimulated insulin secretion

24
Q

Effects of Exenatide?

A
  • Enhances glucose-dependent insulin secretion.
  • Suppresses postprandial glucagon release.
  • Slows gastric emptying.
  • Decreases appetite.
  • May stimulate β-cell proliferation.
25
Q

Exenatide: Adverse Effects?

A

• Nausea, vomiting and diarrhea.
• Acute pancreatitis.
• Should not be used in patients with
gastroparesis.

26
Q

Inhibitors of DPP-IV overview

A

Sitagliptin
• Selective inhibitor of DPP-IV.
• Increases circulating GLP-1 and insulin levels.
• Given orally.

27
Q

Sitagliptin: Adverse Effects?

A

• Pancreatitis.
• Hypersensitivity reactions including urticaria,
angioedema, anaphylaxis, and skin reactions
such as Stevens-Johnson syndrome.

28
Q

Amylin Analogs: Pramlintide overview?

A

• Synthetic analog of amylin.
• Peptide co-secreted with insulin from pancreatic
β-cells.
• Inhibits food intake, gastric emptying, and
glucagon secretion.
• Injectable

29
Q

Bile-acid Sequestrants: Colesevelam?

A 
• Bile-acid sequestrant used to lower LDL
cholesterol.
• Approved for treatment of type 2 DM.
• Mechanism unclear.
• Given orally.
30
Q

SGLT2 Inhibitors overview

A

Canagliflozin
• Glucose is filtered by the glomerulus and
reabsorbed in the proximal tubule by sodium glucose
transporters (SGLTs).
• SGLT2 is responsible for most of glucose
reabsorption.
• Canagliflozin blocks SGLT2.
• This leads to decreased glucose reabsorption,
increased glucose excretion, and decreased
blood glucose levels.
• Given orally.

31
Q

Canagliflozin: Adverse Effects?

A

• Increased incidence of genital and urinary tract
infections.
• The osmotic diuresis can cause volume
depletion, increased serum creatinine levels,
hyperkalemia, hypermagnesemia,
hyperphosphatemia and hypotension.
• Contraindicated in patients with GFR < 45
ml/min/1.73 m2.

32
Q

INITIAL DRUG THERAPY for type 2 diabetes according to american diabetes association guidelines?

A

• Metformin is the preferred first agent.
• Started if lifestyle intervention did not achieve
HbA1c goals.
• Monotherapy with most non-insulin antidiabetic
agents can reduce HbA1c ~ 1%.
• Patients with HbA1c ≥9.0% are unlikely to
achieve HbA1c goals with monotherapy.
• Therefore, therapy may be started with a
combination of two noninsulin agents or with
insulin itself.

33
Q

ADVANCING TO DUAL COMBINATION THERAPY for type 2 diabetes according to american diabetes association guidelines?

A

• If monotherapy does not achieve HbA1c goal over
∼3 months, the next step is to add a second agent.
• The choice could be: oral agent, exenatide, or
insulin.
• The higher the HbA1c, the more likely insulin will be
required.
• If the two-drug combination fails to achieve the
glycemic target a third agent can be added.
• Diabetes is associated with progressive β-cell loss:
many patients will eventually need to be transitioned
to insulin.
• The decision to transition to insulin should be
favored when the HbA1c ≥ 8.5%.

34
Q

TRANSITION TO INSULIN THERAPY for type 2 diabetes according to american diabetes association guidelines?

A

• Insulin is typically begun at a low dose, with a
single injection of basal insulin.
• The dose is then uptitrated.
• If there is postprandial hyperglycemia the patient
will require addition of prandial insulin therapy.
• Typically, rapid-acting insulins are used: lispro,
aspart or glulisine.

35
Q

Describe insulin’s efficacy?

A

• Insulin is the most effective of diabetes
medications in lowering glycemia.
• It can decrease any level of elevated HbA1C to,
or close to, the therapeutic goal.
• There is no maximum dose of insulin beyond
which a therapeutic effect will not occur.
• Large doses of insulin may be necessary to
overcome the insulin resistance of type 2
diabetes.

36
Q

Patients with Severe Hyperglycemia criteria?

A 
Insulin may be warranted as initial therapy for
patients with type 2 diabetes with:
• Significant hyperglycemic symptoms
• Ketonuria
• HbA1c > 10%
• Random glucose > 300 mg/dL
37
Q

Management of Diabetes in Pregnancy?

A 
• Gestational Diabetes Mellitus
• Preexisting Type 1 Diabetes &amp; Type 2 Diabetes
•Insulin is the preferred agent.
•It does not cross the placenta to a
measurable extent.
38
Q

Choice of Insulin in Pregnancy?

A

• All insulins are category B except glargine,
glulisine, and degludec, which are C.
• Use of insulin preparations of low antigenicity
minimizes transplacental transport of insulin
antibodies.
• Human insulin is the least immunogenic
• Lispro, aspart, and glulisine are comparable in
immunogenicity to human insulin.
• Only lispro and aspart have been shown to be
safe in pregnancy.
• A typical regimen may start with a single dose of
bedtime NPH insulin.
• If postprandial glucose control is required
injections of lispro or aspart can be added.

39
Q

Complications of diabetes?

A 
CARDIOVASCULAR DISEASE
• Hypertension
• Dyslipidemia
• Antiplatelet Therapy
• NEPHROPATHY
• NEUROPATHY
• Neuropathic Pain
• Gastroparesis
• Erectile Dysfunction
40
Q

CVD considerations in diabetics?

A

• CVD is the major cause of morbidity and mortality for individuals with diabetes.
Hypertension
• Patients with diabetes and hypertension should
be given either an ACE inhibitor or an ARB.
Dyslipidemia
• Statins should be given, regardless of lipid
levels, to diabetic patients:
• With overt CVD
• Aged < 40 yr with CVD risk factors
• Aged > 40 yr with or without CVD risk

Antiplatelet Agents
• Aspirin therapy should be considered as a
primary prevention strategy in patients with type
1 or type 2 diabetes at increased CV risk.

41
Q

Glucagon uses?

A

Severe Hypoglycemia
• Used to treat severe hypoglycemia in patients
with diabetes treated with insulin.
Radiology Of The Bowel
• Used because of its ability to relax intestine.
beta-Blocker Poisoning
• Antidote for beta-blocker overdose.
Glucagon C-peptide Test
• Test for residual β-cell function in diabetes.

42
Q

Nephropathy and Neuropathy considerations in diabetes?

A

NEPHROPATHY
• ACE inhibitors or ARBs are recommended for
patients with albuminuria.

Neuropathic Pain
• Drugs used for neuropathic pain include:
• Amitriptyline
• Pregabalin
• Gabapentin
• Duloxetine
• Venlafaxine
• Valproate
• Opioids
Gastroparesis
• Gastroparesis symptoms may improve with
dietary changes and prokinetic agents such as
metoclopramide or erythromycin.
Erectile Dysfunction
• Treatments for erectile dysfunction may include
phosphodiesterase type 5 inhibitors.

Pharmacology (49 decks)

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