Antidiabetic Drugs - Transes

ANTIDIABETIC DRUGS ◆ Reduced number of insulin

receptors
DIABETES MELLITUS ◆ Insulin receptors less responsive
➔ Diabetes mellitus (DM) actually is not a
single disease, but a group of GESTATIONAL DIABETES
progressive diseases. It is often ➔ Hyperglycemia that develops during
regarded as a syndrome rather than a pregnancy
disease ➔ Insulin must be given to prevent birth
➔ Two types defects
◆ Type 1 ➔ Usually subsides after delivery
◆ Type 2 ➔ 30% of patients may develop Type 2 DM
within 10 to 15 years
Signs & Symptoms
➢ Elevated fasting blood glucose (higher INSULINS
than 126 mg/dL) or a hemoglobin A1C ➔ Function as a substitute for the
(A1C) level greater than or equal to 6.5% endogenous hormone
➢ Polyuria ➔ Effects are the same as normal
➢ Polydipsia endogenous insulin
➢ Polyphagia ➔ Restores the diabetic patient’s ability to:
➢ Glycosuria ◆ Metabolized carbohydrates, fats,
➢ Unexplained weight loss and proteins
➢ Fatigue ◆ Store glucose in the liver
➢ Blurred vision ◆ Convert glycogen to fat stores
➔ Human insulin
MAJOR LONG-TERM COMPLICATIONS OF DM ◆ Derived insulin recombinant DNA
(BOTH TYPES) technologies
MACROVASCULAR (atherosclerotic plaque) ◆ Recombinant insulin produced
● Coronary arteries by bacteria and yeast
● Cerebral arteries ➔ Goal: tight glucose control
● Peripheral arteries ◆ To reduce the incidence of
MICROVASCULAR (capillary damage) long-term complications
● Retinopathy
● Neuropathy
RAPID ACTING
● Nephropathy
AGENT lispro (Humalog)
TYPE 1 DIABETES MELLITUS
➔ Lack of insulin production or production aspart (NovoLog)
of defective insulin
glulisine (Apidra)
➔ Affected patients need exogenous insulin
➔ Fewer than 10% of all diabetes cases ONSET 10-15 minutes
are type 1
➔ Complications 5-15 minutes
◆ Diabetic ketoacidosis (DKA)
◆ Hyperosmolar nonketotic 5-15 minutes
syndrome PEAK 1 hour

TYPE 2 DBETES MELLITUS 40-50 minutes

➔ Most common type: 90% on all cases
➔ Caused by insulin deficiency and 30-60 minutes
insulin resistance
DURATION 2-4 hours
➔ Many tissues are resistant to insulin
1
 Antidiabetic Drugs - Transes

2-4 hours VERY LONG ACTING

2 hours AGENT glargine (Lantus)

INDICATIONS Used for rapid detemir (Levemir)

reduction of glucose
level, to treat glargine (Toujeo)
postprandial
hyperglycemia, and/or ONSET 1 hour
to prevent nocturnal
hypoglycemia 6 hours

PEAK Continuous (no peak)

SHORT ACTING
DURATION 24 hours
AGENT regular (Humulin R,
Novolin R, Iletin II 24-36 hours
Regular)
INDICATIONS Used for basal dose
ONSET 30-60 minutes

PEAK 2-3 hours RAPID-ACTING INHALED INSULIN

DURATION 4-6 hours AGENT Afrezza

INDICATIONS Usually given 20-30 ONSET <15 minutes

minutes before meal;
may be taken alone or PEAK ~50 minutes
in combination with
longer-acting insulin DURATION 2-3 hours

INDICATIONS Used as rapid-acting

insulin
INTERMEDIATE ACTING

AGENT NPH (Neutral ORAL ANTIDIABETIC DRUGS

Protamine Hagedorn) ➔ Used for type 2 diabetes
➔ Treatment for type 2 diabetes includes
(Humulin N, Iletin II
Lente, Iletin II NPH, lifestyle modifications
Novolin N [NPH]) ◆ Diet, exercise, smoking cessation,
weight loss
ONSET 2-4 hours ➔ Oral Antidiabetic drugs may not be
effective unless the patient also makes
3-4 hours
behavioral or lifestyle changes
PEAK 4-12 hours

4-12 hours

DURATION 16-20 hours

16-20 hours

INDICATIONS Usually taken after

mood

2
 Antidiabetic Drugs - Transes
➔ Inhibit glucose and triglyceride production
➔ Biguanides in the liver
◆ metformin (Glucophage) ALPHA-GLUCOSIDASE INHIBITORS
➔ Sulfonylureas (SU) ➔ Reversible inhibit the enzyme
◆ Second generation: glimepiride ALPHA-GLUCOSIDASE in the small
(Amaryl), glipizide (Glucotrol), intestine
glyburide (DiaBeta, Micronase) ➔ Result in delayed absorption of glucose
➔ Glinides ➔ Must be taken with meals to prevent
◆ repaglinide (Prandin), nateglinide excessive postprandial blood glucose
(Starlix) elevations (with the “first bite” of a meal)
➔ Thiazolidinediones DIPEPTIDYL PEPTIDASE-IV (DPP-IV)
◆ pioglitazone (Actos) INHIBITORS
◆ rosiglitazone (Avandia) ➔ Delay breakdown of incretin hormones by
● Only available through inhibiting the enzyme DPP-IV
specialised manufacturer ➔ Incretin hormones increase insulin
programs synthesis and lower glucagon secretion
◆ Also known as glitazones ➔ Reduce fasting and postprandial glucose
➔ Alpha-glucosidase inhibitors concentrations
◆ acarbose (Precose), miglitol
(Glyset) ORAL ANTIDIABETIC DRUGS: ADVERSE
➔ Dipeptidyl peptidase-IV (DPP-IV) inhibitors EFFECTS
◆ sitagliptin (Januvia) BIGUANIDES (metformin)
◆ saxagliptin (Onglyza) ➔ Primarily affects GI tract: abdominal
◆ linagliptin (Tradjenta) bloating, nausea, cramping, diarrhea,
feeling of fullness
ORAL ANTIDIABETIC DRUGS: MECHANISM ➔ May also cause metallic taste, reduced
OF ACTION vitamin B12 levels
BIGUANIDES ➔ Lactic acidosis is rare but lethal if it occurs
➔ Decrease production of glucose by ➔ Does not cause hypoglycemia
liver SULFONYLUREAS
➔ Decrease intestinal absorption of glucose ➔ Hypoglycemia, hematologic effects,
➔ Increase uptake of glucose by tissues nausea, epigastric fullness, heartburn,
➔ Do not increase insulin secretion from the many others
pancreas (does not cause hypoglycemia) GLINIDES
SULFONYLUREAS ➔ Headache, hypoglycemic effects,
➔ Stimulate insulin secretion from the dizziness, weight gain, joint pain, upper
beta cells of the pancreas, thus respiratory infection or flu like symptoms
increasing insulin levels THIAZOLDINEDIONES
➔ Beta cell function must be present ➔ Moderate weight gain, edema, mild
➔ Improve sensitivity to insulin in tissues anemia
➔ Result in lower blood glucose levels ➔ Hepatic toxicity—monitor alanine
GLINIDES aminotransferase (ALT) levels
➔ Action similar to sulfonylureas ALPHA-GLUCOSIDASE INHIBITORS
➔ Increase insulin secretion from the ➔ Flatulence, diarrhea, abdominal pain
pancreas ➔ Do not cause hypoglycemia,
THIAZOLIDINEDIONES hyperinsulinemia, or weight gain
➔ Decrease insulin resistance
➔ “Insulin sensitizing drugs” INJECTABLE ANTIDIABETIC DRUGS
➔ Increase glucose uptake and use in Amylin agonists
skeletal muscle ● pramlintide (Symlin)
Incretin mimetics
3
 Antidiabetic Drugs - Transes
● exenatide (Byetta) DRUGS FOR ACID-RELATED GI DISORDERS
● liraglutide (Victoza)
GASTROESOPHAGEAL REFLUX DISEASE
INJECTABLE ANTIDIABETIC DRUGS: (GERD)
MECHANISM OF ACTION ➔ The most common disorder of the
AMYLIN AGONIST esophagus, is characterized by
➔ Mimics the natural hormone amylin regurgitation of gastric contents into the
➔ Slows gastric emptying esophagus and exposure of esophageal
➔ Suppresses glucagon secretion, reducing mucosa to gastric acid and pepsin
Hepatic glucose output
➔ Centrally modulate appetite and satiety GASTRITIS
➔ Used when other drugs have not achieved ACUTE GASTRITIS (gastrophy)
adequate glucose control ➔ Usually results from irritation of the gastric
➔ Subcutaneous injection mucosa by such substances as alcohol,
INCRETIN MIMETIC aspirin or other nonsteroidal
➔ Mimics the incretin hormones antiinflammatory drugs (NSAIDS), and
➔ Enhances glucose-driven insulin secretion others
from beta cells of the pancreas
➔ Only used for type 2 diabetes CHRONIC GASTRITIS
➔ Exenatide: Injection pen device ➔ Is usually caused by Helicobacter pylori
infection and it persists unless the
INJECTABLE ANTIDIABETIC DRUGS: infection is treated effectively. H. pylori
ADVERSE EFFECTS organisms may cause gastritis and
AMYLIN AGONIST ulceration by
➔ Nausea, vomiting, anorexia, headache
INCRETIN MIMETIC STRESS ULCERS
➔ Nausea, vomiting, and diarrhea ➔
➔ Rare cases of hemorrhagic or necrotising
pancreatitis NONSTEROIDAL ANTIINFLAMMATORY DRUG
➔ Weight loss GASTROPHY
➔ Damage to gastroduodenal mucosa by
aspirin and other NSAIDS

ANTACIDS
➔ Alkaline substances that neutralise acids.
They react with hydrochloric acid in the
stomach to produce neutral, less acidic, or
poorly absorbed salts and to raise the pH
(alkalinity) of gastric secretions
➔ Raising the pH to approximately 3.5
neutralises more than 90% of gastric acid
and inhibits conversion of pepsinogen to
pepsin. Commonly used antacids are
aluminum, magnesium, and calcium
compounds
➔ Examples:
◆ Amphojel
◆ Gelusil
◆ Maalox

4
 Antidiabetic Drugs - Transes
HISTAMINE-2 RECEPTOR ANTAGONISTS ■ When added to antacids
(H2RAs) Simethicone does not affect
➔ Histaminic Receptors: gastric acidity. It reportedly
◆ H1 = activation causes decreases gas bubbles,
inflammatory/hypersensitivity thereby reducing GI
reactions distention and abdominal
◆ H2 = activation causes acid discomfort
production ○ Alginic acid (eg, in Gaviscon)
➔ Examples: produces a foamy, viscous layer on
◆ Cimetidine top of gastric acid
◆ Ranitidine (ZANTAC) ■ Thereby decreases back
◆ Famotidine flow of gastric acid onto
◆ Nizatidine esophageal mucosa while
the person is in a upright
PROTON PUMP INHIBITORS position
➔ These drugs bind irreversibly to the gastric
proton pump (ie, the enzyme H+, H2 Blockers
K+-ATPase) to prevent the “pumping” or ➔ Should be used with caution during
release of gastric acid from parietal cells pregnancy because it crosses placenta,
into the stomach lumen and therefore and it should not be taken during lactation
block the final step of acid production because it is excreted in breast milk
➔ Examples: ◆ Cimetidine can inhibit hepatic
◆ Omeprazole microsomal enzymes (may prolong
◆ Esomeprazole effects of other drugs)
◆ Lansoprazole H. Pylori Infection Treatment
◆ Pantoprazole ➔ Effective combinations include
antimicrobial and a PPI or an H2RA
SUCRALFATE ◆ For the antimicrobial component,
➔ A preparation of sulfated sucrose and two of the following
aluminum hydroxide that binds to normal drugs—amoxicillin, clarithromycin,
and ulcerated mucosa, forming a metronidazole,or tetracycline
protective barrier between the mucosa
and gastric acid, pepsin, and bile salts ❖ Proton-pump inhibitors are enteric-coated
➔ Should be taken before meals and should not be crushed
➔ Examples:
◆ Iselpin

NURSING CONSIDERATIONS
Aluminum side effects:
● Can cause constipation
● Hypophosphatenemia
Magnesium side effects:
● Can cause diarrhea
● Hypermagnesemia
Calcium
● “Acid-rebound”

❖ Some antacid mixtures contain other

ingredients
○ Simethicone is an antiflatulent drug