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Pfizer, Inc. Drugs
EXUBERA, like rapid-acting insulin analogs, has a more rapid onset of glucose-lowering activity compared to subcutaneously injected regular human insulin. EXUBERA has a duration of glucose-lowering activity comparable to subcutaneously injected regular human insulin and longer than rapid-acting insulin. EXUBERA doses should be administered immediately prior to meals (no more than 10 minutes prior to each meal).
In patients with type 1 diabetes, EXUBERA should be used in regimens that include a longer-acting insulin. For patients with type 2 diabetes, EXUBERA may be used as monotherapy or in combination with oral agents or longer-acting insulin.
Because of the effect of EXUBERA on pulmonary function, all patients should have pulmonary function assessed prior to initiating therapy with EXUBERA. Periodic monitoring of pulmonary function is recommended for patients being treated with EXUBERA (see PRECAUTIONS, Pulmonary Function).
EXUBERA is intended for administration by inhalation and must only be administered using the EXUBERA® Inhaler. Refer to the EXUBERA Medication Guide for a description of the EXUBERA® Inhaler and for instructions on how to use the inhaler.
Calculation of Initial Pre-Meal EXUBERA Dose
The initial dosage of EXUBERA should be individualized and determined based on the physician's advice in accordance with the needs of the patient. Recommended initial pre-meal doses are based on clinical trials in which patients were requested to eat three meals per day. Initial pre-meal doses may be calculated using the following formula: [Body weight (kg) X 0.05 mg/kg = pre-meal dose (mg)] rounded down to the nearest whole milligram number (e.g., 3.7 mg rounded down to 3 mg).
Approximate guidelines for initial, pre-meal EXUBERA doses, based on patient body weight, are indicated in Table 7:Table 7: Approximate Guidelines for Initial, Pre-Meal EXUBERA Dose (based on patient body weight) Patient Weight(in kg) Patient Weight(in lb) Initial Dose per Meal Number of 1 mg Blisters per Dose Number of 3 mg Blisters per Dose 30 to 39.9 kg 66 – 87 lb 1 mg per meal 1 - 40 to 59.9 kg 88 – 132 lb 2 mg per meal 2 - 60 to 79.9 kg 133 – 176 lb 3 mg per meal - 1 80 to 99.9 kg 177 – 220 lb 4 mg per meal 1 1 100 to 119.9 kg 221– 264 lb 5 mg per meal 2 1 120 to 139.9 kg 265 – 308 lb 6 mg per meal - 2
A 1 mg blister of EXUBERA inhaled insulin is approximately equivalent to 3 IU of subcutaneously injected regular human insulin. A 3 mg blister of EXUBERA inhaled insulin is approximately equivalent to 8 IU of subcutaneously injected regular human insulin. Table 8 provides the approximate IU dose of regular subcutaneous human insulin for EXUBERA inhaled insulin doses from 1 mg to 6 mg.Table 8: Approximate Equivalent IU Dose of Regular Human Subcutaneous Insulin for EXUBERA Inhaled Insulin Doses Ranging from 1 mg to 6 mg Dose (mg) Approximate Regular Insulin SC Dose in IU Number of 1 mg EXUBERA Blisters per Dose Number of 3 mg EXUBERA Blisters per Dose 1 mg 3 1 - 2 mg 6 2 - 3 mg 8 - 1 4 mg 11 1 1 5 mg 14 2 1 6 mg 16 - 2
Patients should combine 1 mg and 3 mg blisters so that the least number of blisters per dose are taken (e.g., a 4 mg dose should be administered as one 1 mg blister and one 3 mg blister). Consecutive inhalation of three 1 mg unit dose blisters results in significantly greater insulin exposure than inhalation of one 3 mg unit dose blister. Therefore, three 1 mg doses should not be substituted for one 3 mg dose (see CLINICAL PHARMACOLOGY, Pharmacokinetics). When a patient is stabilized on a dosing regimen that includes 3 mg blisters, and the 3 mg blisters become temporarily unavailable, the patient can temporarily substitute two 1 mg blisters for one 3 mg blister. Blood glucose should be monitored closely.
As with all insulins, additional factors that should be taken into consideration when determining the EXUBERA starting dose include, but are not limited to, patient's current glycemic control, previous response to insulin, duration of diabetes, and dietary and exercise habits.
Considerations for Dose Titration
After initiating EXUBERA therapy, as with other glucose-lowering agents, dose adjustment may be required based on the patient's need (e.g., blood glucose concentrations, meal size and nutrient composition, time of day and recent or anticipated exercise). Each patient should be titrated to their optimal dosage based on blood glucose monitoring results.
As for all insulins, the time course of EXUBERA action may vary in different individuals or at different times in the same individual.
EXUBERA may be used during intercurrent respiratory illness (e.g., bronchitis, upper respiratory tract infection, rhinitis). Close monitoring of blood glucose concentrations and dose adjustment may be required on an individual basis. Inhaled medicinal products (e.g. bronchodilators) should be administered prior to administration of EXUBERA.
Prophylaxis of Ischemic Complications in Unstable Angina and Non-Q-Wave Myocardial Infarction
In patients with unstable angina or non-Q-wave myocardial infarction, the recommended dose of FRAGMIN Injection is 120 IU/kg of body weight, but not more than 10,000 IU, subcutaneously (s.c.) every 12 hours with concurrent oral aspirin (75 to 165 mg once daily) therapy. Treatment should be continued until the patient is clinically stabilized. The usual duration of administration is 5 to 8 days. Concurrent aspirin therapy is recommended except when contraindicated.
Table 13 lists the volume of FRAGMIN, based on the 9.5 mL multiple-dose vial (10,000 IU/mL), to be administered for a range of patient weights.Table 13 Volume of FRAGMIN to be Administered by Patient Weight, Based on 9.5 mL Vial (10,000 IU/mL) Patientweight (lb) < 110 110 to 131 132 to 153 154 to 175 176 to 197 ≥198 Patientweight (kg) < 50 50 to 59 60 to 69 70 to 79 80 to 89 ≥90 Volume ofFRAGMIN (mL) 0.55 0.65 0.75 0.90 1.0 1.0
Prophylaxis of Venous Thromboembolism Following Hip Replacement Surgery
Table 14 presents the dosing options for patients undergoing hip replacement surgery. The usual duration of administration is 5 to 10 days after surgery; up to 14 days of treatment with FRAGMIN have been well tolerated in clinical trials.Table 14 Dosing Options for Patients Undergoing Hip Replacement Surgery Dose of FRAGMIN to be Given Subcutaneously Timing ofFirst Doseof FRAGMIN 10 to 14 HoursBeforeSurgery Within 2 HoursBeforeSurgery 4 to 8 HoursAfterSurgery* PostoperativePeriod† * Or later, if hemostasis has not been achieved. † Up to 14 days of treatment was well tolerated in controlled clinical trials, where the usual duration of treatment was 5 to 10 days postoperatively. ‡ Allow a minimum of 6 hours between this dose and the dose to be given on Postoperative Day 1. Adjust the timing of the dose on Postoperative Day 1 accordingly. § Allow approximately 24 hours between doses. PostoperativeStart --- --- 2500 IU‡ 5000 IU once daily PreoperativeStart - Day ofSurgery --- 2500 IU 2500 IU‡ 5000 IU once daily PreoperativeStart - EveningBefore Surgery§ 5000 IU --- 5000 IU 5000 IU once daily
Prophylaxis of Venous Thromboembolism Following Abdominal Surgery
In patients undergoing abdominal surgery with a risk of thromboembolic complications, the recommended dose of FRAGMIN is 2500 IU administered by s.c. injection once daily, starting 1 to 2 hours prior to surgery and repeated once daily postoperatively. The usual duration of administration is 5 to 10 days.
In patients undergoing abdominal surgery associated with a high risk of thromboembolic complications, such as malignant disorder, the recommended dose of FRAGMIN is 5000 IU s.c. the evening before surgery, then once daily postoperatively. The usual duration of administration is 5 to 10 days. Alternatively, in patients with malignancy, 2500 IU of FRAGMIN can be administered s.c. 1 to 2 hours before surgery followed by 2500 IU s.c. 12 hours later, and then 5000 IU once daily postoperatively. The usual duration of administration is 5 to 10 days.
Dosage adjustment and routine monitoring of coagulation parameters are not required if the dosage and administration recommendations specified above are followed.
Medical Patients with Severely Restricted Mobility During Acute Illness
In medical patients with severely restricted mobility during acute illness, the recommended dose of FRAGMIN is 5000 IU administered by s.c. injection once daily. In clinical trials, the usual duration of administration was 12 to 14 days.
Extended Treatment of Symptomatic Venous Thromboembolism in Patients with Cancer
In patients with cancer and symptomatic venous thromboembolism, the recommended dosing of FRAGMIN is as follows: for the first 30 days of treatment administer FRAGMIN 200 IU/kg total body weight subcutaneously (s.c.) once daily. The total daily dose should not exceed 18,000 IU. Table 15 lists the dose of FRAGMIN to be administered once daily during the first month for a range of patient weights.
Month 1Table 15 Dose of FRAGMIN to be Administered Subcutaneously by Patient Weight during the First Month Body Weight (lbs) Body Weight (kg) FRAGMIN Dose (IU)(prefilled syringe) once daily ≤ 124 ≤ 56 10,000 125 to 150 57 to 68 12,500 151 to 181 69 to 82 15,000 182 to 216 83 to 98 18,000 ≥ 217 ≥ 99 18,000
Months 2 to 6
Administer FRAGMIN at a dose of approximately 150 IU/kg, s.c. once daily during Months 2 through 6. The total daily dose should not exceed 18,000 IU. Table 16 lists the dose of FRAGMIN to be administered once daily for a range of patient weights during months 2–6.Table 16 Dose of FRAGMIN to be Administered Subcutaneously by Patient Weight during Months 2–6 Body Weight (lbs) Body Weight (kg) FRAGMIN Dose (IU)(prefilled syringe) once daily ≤ 124 ≤ 56 7,500 125 to 150 57 to 68 10,000 151 to 181 69 to 82 12,500 182 to 216 83 to 98 15,000 ≥ 217 ≥ 99 18,000
Safety and efficacy beyond six months have not been evaluated in patients with cancer and acute symptomatic VTE (see WARNINGS, Thrombocytopenia and ADVERSE REACTIONS, Patients with Cancer and Acute Symptomatic VTE).
Dose reductions for thrombocytopenia in patients with cancer and acute symptomatic VTE
In patients receiving FRAGMIN who experience platelet counts between 50,000 and 100,000/mm3, reduce the daily dose of FRAGMIN by 2,500 IU until the platelet count recovers to ≥100,000/mm3. In patients receiving FRAGMIN who experience platelet counts < 50,000/mm3, FRAGMIN should be discontinued until the platelet count recovers above 50,000/mm3.
Dose reductions for renal insufficiency in extended treatment of acute symptomatic venous thromboembolism in patients with cancer
In patients with severely impaired renal function (CrCl < 30 mL/min), monitoring for anti-Xa levels is recommended to determine the appropriate FRAGMIN dose. Target anti-Xa range is 0.5–1.5 IU/mL. When monitoring anti-Xa in these patients, sampling should be performed 4–6 hrs after FRAGMIN dosing and only after the patient has received 3–4 doses.
FRAGMIN is administered by subcutaneous injection. It must not be administered by intramuscular injection.
Subcutaneous injection technique: Patients should be sitting or lying down and FRAGMIN administered by deep s.c. injection. FRAGMIN may be injected in a U-shape area around the navel, the upper outer side of the thigh or the upper outer quadrangle of the buttock. The injection site should be varied daily. When the area around the navel or the thigh is used, using the thumb and forefinger, you must lift up a fold of skin while giving the injection. The entire length of the needle should be inserted at a 45 to 90 degree angle.
Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
After first penetration of the rubber stopper, store the multiple-dose vials at room temperature for up to 2 weeks. Discard any unused solution after 2 weeks.
Instructions for using the prefilled single-dose syringes preassembled with needle guard devices
Fixed dose syringes
To ensure delivery of the full dose, do not expel the air bubble from the prefilled syringe before injection. Hold the syringe assembly by the open sides of the device. Remove the needle shield. Insert the needle into the injection area as instructed above. Depress the plunger of the syringe while holding the finger flange until the entire dose has been given. The needle guard will not be activated unless the entire dose has been given. Remove needle from the patient. Let go of the plunger and allow syringe to move up inside the device until the entire needle is guarded. Discard the syringe assembly in approved containers.
Hold the syringe assembly by the open sides of the device. Remove the needle shield. With the needle pointing up, prepare the syringe by expelling the air bubble and then continuing to push the plunger to the desired dose or volume, discarding the extra solution in an appropriate manner. Insert the needle into the injection area as instructed above. Depress the plunger of the syringe while holding the finger flange until the entire dose remaining in the syringe has been given. The needle guard will not be activated unless the entire dose has been given. Remove needle from the patient. Let go of the plunger and allow syringe to move up inside the device until the entire needle is guarded. Discard the syringe assembly in approved containers.
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