General

**Off Market Drug**
This medication is no longer available in the United States. Information provided here is for reference purposes only.

Pronunciation
IN-soo-lin

Trade Name(s)

• Exubera

Pregnancy Category
Category C

Ther. class.
antidiabetics

Pharm. class.
hormones
pancreatics

Indications

Treatment of diabetes mellitus (types 1 and 2) in adults

Action

• Lower blood glucose by

» stimulating glucose uptake in skeletal muscle and fat

» inhibiting hepatic glucose production

• Other actions

» inhibition of lypolysis and proteolysis

» enhanced protein synthesis

Therapeutic Effect(s):
Control of blood glucose in diabetic patients

Pharmacokinetics

Absorption: Well absorbed from lung mucosa; is as rapidly absorbed as subcut rapid-acting insulin analogs and more rapidly than subcut regular human insulin. Absorption is not affected by body mass index. Absorption is enhanced in smokers.

Distribution: Widely distributed

Metabolism and Excretion: Metabolized by liver, spleen, kidney, and muscle

Half-life: 30–60 min

TIME/ACTION PROFILE (glucose lowering effects)

ROUTE	ONSET	PEAK	DURATION
inhaln	within 10 min	30–90 min	5–7 hr

Contraindication/Precautions

Contraindicated in:

• Hypoglycemia

• Hypersensitivity to insulin or to any other components of the formulation (sodium citrate, mannitol, glycine, sodium hydroxide)

• Underlying lung disease, including asthma or COPD (due to altered absorption)

• Patients who smoke or who have quit smoking within the last 6 mo (increased risk of hypoglycemia due to increased absorption)

Use Cautiously in:

• Hepatic/renal impairment (requirements may be less)

• Intercurrent respiratory illness (may alter requirements)

• Stress, pregnancy, and infection (may temporarily alter insulin requirements)

• Children <18 yr (safety not established)

Adverse Reactions/Side Effects

CV: chest pain.

Resp: cough, pulmonary function, dyspnea, bronchospasm (rare), sputum production.

GI: dry mouth.

Derm: urticaria.

Endo: HYPOGLYCEMIA, rebound hyperglycemia (Somogyi effect).

Misc: ALLERGIC REACTIONS INCLUDING ANAPHYLAXIS.

*CAPITALS indicates life-threatening.
*italic indicates most frequent.

Interactions

Drug-Drug

• Albuterol increases absorption.

• Bronchodilators and other inhaled medications may alter absorption; monitor blood glucose carefully

• Glucose lowering effects may be by corticosteroids, danazol, diazoxide, diuretics, sympathomimetic (adrenergic) agents, phenothiazines, somatropin, thyroid preparations, estrogens, progestins, protease inhibitor antiretrovirals, and atypical antipsychotics including olanzapine, quetiapine, clozapine, risperidone, aripiprazole, and ziprasidone

• Blood glucose lowering effects and the risk of hypoglycemia may be by oral antidiabetics, ACE inhibitors, disopyramide, fibrates, salicylates, fluoxetine, MAO inhibitors, pentoxiphylline, propoxyphene, and sulfonamides

• Beta blockers, guanethidine, and reserpine may block some signs of and delay recovery from hypoglycemia

Drug-Natural Products

• Glucosamine may worsen blood glucose control

• Chromium and coenzyme Q-10 may produce additive hypoglycemic effects

Route/Dosage

• Dose depends on blood glucose, response, and many other factors; additional longer acting insulin may be required.

• Inhaln (Adults):
Initial pre-meal dosing, further adjusted as needed/required—[Body weight (kg) × 0.05 mg/kg, rounded down to nearest whole mg number.
30–39.9 kg—1 mg/meal;
40–59.9 kg—2 mg/meal;
60–79.9 kg—3 mg/meal;
80–99.9 kg—4 mg/meal;
100–119.9 kg—5 mg/meal;
120–139.9 kg—6 mg/meal.

Availability

Each 1 mg blister is approximately equal to 3 Units of subcut regular insulin; each 3 mg blister is approximately equal to 8 Units of subcut regular insulin.

• Powder for inhalations: 1 mg blister, 3 mg blister

Assessment

• Assess for signs and symptoms of hypoglycemia (anxiety; chills; cold sweats; confusion; cool, pale skin; difficulty in concentration; drowsiness; excessive hunger; headache; irritability; nausea; nervousness; rapid pulse; shakiness; unusual tiredness or weakness) and hyperglycemia (drowsiness; flushed, dry skin; fruit-like breath odor; frequent urination; loss of appetite; tiredness; unusual thirst) periodically during therapy.

• Monitor body weight periodically. Changes in weight may necessitate changes in insulin dose.

• Assess pulmonary function (spirometry [FEV₁] and DL_CO) prior to initiating therapy. Inhalation insulin is not recommended for patients with underlying lung disease (asthma, COPD).

• Monitor for bronchospasm. Occurs rarely, but if bronchospasm occurs, discontinue therapy and notify health care professional immediately. Re-administration should be attempted during close monitoring.

• Assess for intercurrent respiratory illness. Monitor blood glucose concentrations closely; may require dose adjustments.

• Monitor for signs of allergic reaction (rash, dyspnea, wheezing, tachycardia, sweating, low blood pressure).

Lab Test Considerations

• Monitor blood glucose and ketones every 6 hr during therapy, more frequently in ketoacidosis and times of stress. Glycosylated hemoglobin may also be monitored to determine effectiveness.

Toxicity and Overdose

• Overdose is manifested by symptoms of hypoglycemia. Mild hypoglycemia may be treated by ingestion of oral glucose. Severe hypoglycemia is a life-threatening emergency; treatment consists of IV glucose, glucagon, or epinephrine.

Potential Nursing Diagnoses

• Noncompliance (Patient/Family Teaching)

Implementation

• In patients with Type 1 diabetes, use with longer—acting insulins. In patients with Type 2 diabetes, use as monotherapy or in combination with oral agents or longer—acting insulins.

» Other inhaled medicinal products should be administered prior to administration of inhaled insulin.

» Patients should combine 1 mg and 3 mg blisters so that the least number of blisters/dose are taken. Consecutive inhalation of 3 1–mg blisters results in significantly greater insulin than 1 3–mg blister. Three 1–mg blisters should not be substituted for 1 3–mg dose. If 3–mg dose is unavailable, use two 1–mg blisters temporarily, check blood glucose, and notify health care professional.

• Inhaln: When used as a mealtime insulin, administer within 10 min before a meal. Following inhalation, close mouth and hold breath for 5 seconds; then breathe normally. Store at in a dry place at room temperature; do not refrigerate or freeze. Inhaler can be used for up to 1 yr from date of first use. Inhaler release unit should be changed every 2 wks. Chamber and mouthpiece should be cleaned weekly.

Patient/Family Teaching

• Instruct patient on administration technique as described in the Medication Guide. Do not open individual blisters; unopened blisters are placed in the inhaler. Never swallow contents of blister; for inhalation only. Do not try to re-use blisters; discard after 1 use. Advise patient to read the Medication Guide before initiating therapy and with each Rx refill. For problems with the inhaler or a replacement call 1–800–EXUBERA, then call health care professional for treatment instructions until replacement is received.

• Caution patient to avoid smoking during use of inhaled insulin.

• Explain to patient that this medication controls hyperglycemia but does not cure diabetes. Therapy is long term.

• Instruct patient in proper testing of serum glucose and ketones. These tests should be closely monitored during periods of stress or illness and health care professional notified of significant changes.

• Emphasize the importance of compliance with nutritional guidelines and regular exercise as directed by health care professional.

• Advise patient to consult health care professional prior to using alcohol or other medications concurrently with insulin.

• Advise patient to notify health care professional of medication regimen prior to treatment or surgery.

• Advise patient to notify health care professional if intercurrent respiratory illness, a change in breathing, nausea, vomiting, or fever develops, if unable to eat regular diet, or if blood glucose levels are not controlled.

• Instruct patient on signs and symptoms of hypoglycemia and hyperglycemia and what to do if they occur.

• Advise patient to notify health care professional if pregnancy is planned or suspected.

• Patients with diabetes mellitus should carry a source of sugar (candy, sugar packets) and identification describing their disease and treatment regimen at all times.

• Emphasize the importance of regular follow-up, especially during first few weeks of therapy.

Evaluation/Desired Outcomes

Control of blood glucose levels without the appearance of hypoglycemic or hyperglycemic episodes.

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