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Anti- Diabetic Agents
Alpha-glucosidase Inhibitors
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acarbose (Precose ®): |
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INDICATIONS: Monotherapy, as
indicated as an adjunct to diet to lower blood glucose in patients with
type 2 diabetes mellitus (noninsulin dependent, NIDDM) whose
hyperglycemia cannot be managed on diet alone. Combination with a sulfonylurea, metformin, or insulin in patients with type 2 diabetes mellitus (noninsulin dependent, NIDDM) when diet plus acarbose do not result in adequate glycemic control. The effect of acarbose to enhance glycemic control is additive to that of other hypoglycemic agents when used in combination. Mechanism of Action - Competitive inhibitor of pancreatic alpha-amylase and intestinal brush border ALPHA-glucosidases, resulting in delayed hydrolysis of ingested complex carbohydrates and disaccharides and absorption of glucose; dose-dependent reduction in postprandial serum insulin and glucose peaks; inhibits the metabolism of sucrose to glucose and fructose Dosing: Oral: - Adults: Dosage must be individualized on the basis of effectiveness and tolerance while not exceeding the maximum recommended dose Initial dose: 25 mg 3 times/day with the first bite of each main meal Maintenance dose: Should be adjusted at 4- to 8-week intervals based on 1-hour postprandial glucose levels and tolerance. Dosage may be increased from 25 mg 3 times/day to 50 mg 3 times/day. Some patients may benefit from increasing the dose to 100 mg 3 times/day. Maintenance dose ranges: 50-100 mg 3 times/day. Maximum dose: </= 60 kg: 50 mg 3 times/day >60 kg: 100 mg 3 times/day Patients receiving sulfonylureas: Acarbose given in combination with a sulfonylurea will cause a further lowering of blood glucose and may increase the hypoglycemic potential of the sulfonylurea. If hypoglycemia occurs, appropriate adjustments in the dosage of these agents should be made. Dosing adjustment in renal impairment: Clcr<25 mL/minute: Peak plasma concentrations were 5 times higher and AUCs were 6 times larger than in volunteers with normal renal function; however, long-term clinical trials in diabetic patients with significant renal dysfunction have not been conducted and treatment of these patients with acarbose is not recommended. Administration Should be administered with the first bite of each main meal. Supplied Tablet: 25 mg, 50 mg, 100 mg |
Miglitol (Glycet ®): |
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INDICATIONS Type 2 diabetes mellitus
(noninsulin-dependent, NIDDM): Monotherapy adjunct to diet to improve glycemic control in patients with type 2 diabetes mellitus (noninsulin-dependent, NIDDM) whose hyperglycemia cannot be managed with diet alone Combination therapy with a sulfonylurea when diet plus either miglitol or a sulfonylurea alone do not result in adequate glycemic control. The effect of miglitol to enhance glycemic control is additive to that of sulfonylureas when used in combination. Mechanism of Action In contrast to sulfonylureas, miglitol does not enhance insulin secretion; the antihyperglycemic action of miglitol results from a reversible inhibition of membrane-bound intestinal alpha-glucosidases which hydrolyze oligosaccharides and disaccharides to glucose and other monosaccharides in the brush border of the small intestine; in diabetic patients, this enzyme inhibition results in delayed glucose absorption and lowering of postprandial hyperglycemia Dosing Adults: Oral: 25 mg 3 times/day with the first bite of food at each meal; the dose may be increased to 50 mg 3 times/day after 4-8 weeks; maximum recommended dose: 100 mg 3 times/day Dosing adjustment in renal impairment : Miglitol is primarily excreted by the kidneys; there is little information of miglitol in patients with a Clcr<25 mL/minute Administration Should be taken orally at the start (with the first bite) of each main meal Supplied Tablet: 25 mg, 50 mg, 100 mg |
Biguanides (Including combination products)
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metformin (Glucophage ®): |
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Decreases hepatic glucose production, decreasing intestinal absorption
of glucose and improves insulin sensitivity (increases peripheral
glucose uptake and utilization). Management of type 2 diabetes mellitus: Standard release tablet or oral solution: Dosing (Adults): Start: 500 mg twice daily (give with the morning and evening meals) or 850 mg once daily; increase dosage incrementally. (A lower recommended starting dose and gradual increased dosage is recommended to minimize gastrointestinal symptoms). Adjustment: Incremental dosing recommendations are based on dosage form: 500 mg tablet: One tablet/day at weekly intervals. 850 mg tablet: One tablet/day every other week. Oral solution: 500 mg twice daily every other week. Note: Doses of up to 2000 mg/day may be given in divided doses twice daily. If a dose >2000 mg/day is required, it may be better tolerated in three divided doses. Maximum recommended dose: 2550 mg/day. Extended release tablet: Initial: 500 mg once daily (with the evening meal). Dosage may be increased by 500 mg weekly. Maximum dose: 2000 mg once daily. If glycemic control is not achieved at maximum dose, may divide dose to 1000 mg twice daily. If doses >2000 mg/day are needed, switch to regular release tablets and titrate to maximum dose of 2550 mg/day. Renal dosing: Metformin is contraindicated in the presence of renal dysfunction defined as a serum creatinine >1.5 mg/dL in males, or >1.4 mg/dL in females and in patients with abnormal clearance. Hepatic impairment: Avoid metformin. Supplied: Tablet: 500 mg, 850 mg, 1000 mg. Extended release tablet: 500 mg, 750 mg, 1000 mg. Oral solution: 100 mg/ml (118 ml, 473 ml). |
Avandamet® (Rosiglitazone + Metformin) |
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Management of type 2 diabetes
mellitus: initial (previously receiving rosiglitazone 4 mg/day):
Avandamet® 2/500mg po bid. (previously receiving rosiglitazone 8
mg/day): 4/500mg po bid. (previously receiving metformin 1000 mg/day):
2/500mg po bid. (previously receiving metformin 2000 mg/day): 2/1000mg
po bid. Titrate in increments of rosiglitazone 4 mg and/or metformin 500 mg po daily. Maximum: 8 mg/2000 mg daily. Other: take with meals. When switching from metformin and rosiglitazone therapy given as separate tablets, starting dose of Avandamet is the dose of each drug previously taken. Dose titration should occur at 1 to 2 week intervals. If the dose of metformin is increased, dose titration should occur at 8 to 12 week intervals. If the dose of rosiglitazone is increased therapeutic response evaluation should be based on fasting plasma glucose values. Monitoring: renal function, baseline and at least annually. [Supplied: 1 mg/500 mg, 2 mg/500 mg, 4 mg/500 mg] . |
Glucovance (Glyburide + Metformin) |
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Management of type 2 diabetes mellitus: Dosing (initial): 1.25 mg/250 mg once or twice daily with meals. Dosage increases should be made in increments of 1.25 mg/250 mg per day every two weeks up to the minimum effective dose necessary to achieve adequate control of blood glucose. Glucovance 5 mg/500 mg should not be used as initial therapy due to an increased risk of hypoglycemia. Maximum recommended daily dose: 20 mg glyburide/2000 mg metformin. Administration: Glucovance should be given with meals and should be initiated at a low dose, with gradual dose escalation in order to avoid hypoglycemia (largely due to glyburide), to reduce GI side effects (largely due to metformin), and to permit determination of the minimum effective dose for adequate control of blood glucose for the individual patient. Glucovance Use in Previously Treated Patients: Recommended starting dose: 2.5 mg/500 mg or 5 mg/500 mg twice daily with meals. In order to avoid hypoglycemia, the starting dose of Glucovance should not exceed the daily doses of glyburide or metformin already being taken. The daily dose should be titrated in increments of no more than 5 mg/500 mg up to the minimum effective dose to achieve adequate control of blood glucose or to a maximum dose of 20 mg/2000 mg per day. [Supplied: 1.25 mg/250 mg, 2.5 mg/500 mg, 5 mg/500 mg tablet ] |
Metaglip (Glipizide + Metformin) |
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Management of type 2 diabetes mellitus: Dosing (initial): 2.5 mg/250 mg qd with a meal. For patients whose FPG is 280 to 320 mg/dl a starting dose of Metaglip 2.5 mg/500 mg twice daily should be considered. The efficacy of Metaglip in patients whose FPG exceeds 320 mg/dl has not been established. Dosage increases to achieve adequate glycemic control should be made in increments of one tablet per day every two weeks up to maximum of 10 mg/1000 mg or 10 mg/2000 mg per day given in divided doses. Maximum recommended daily dose: 20 mg glipizide/2000 mg metformin. Second-Line Therapy For patients not adequately controlled on either glipizide (or another sulfonylurea) or metformin alone: 2.5 mg/500 mg or 5mg/500mg bid with the morning and evening meals. In order to avoid hypoglycemia, the starting dose of Metaglip should not exceed the daily doses of glipizide or metformin already being taken. The daily dose should be titrated in increments of no more than 5 mg/500 mg up to the minimum effective dose to achieve adequate control of blood glucose or to a maximum dose of 20 mg/2000 mg per day. [Supplied: 2.5 mg/250 mg, 2.5 mg/500 mg, 5 mg/500 mg tablet ] |
Glitazones - Thiazolidinediones
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pioglitazone (Actos ®): |
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INDICATIONS - Type 2 diabetes
mellitus (noninsulin dependent, NIDDM), monotherapy: Adjunct to diet and
exercise, to improve glycemic control. Type 2 diabetes mellitus
(noninsulin dependent, NIDDM), combination therapy with sulfonylurea,
metformin, or insulin: When diet, exercise, and a single agent alone
does not result in adequate glycemic control Mechanism of Action Thiazolidinedione antidiabetic agent that lowers blood glucose by improving target cell response to insulin, without increasing pancreatic insulin secretion. It has a mechanism of action that is dependent on the presence of insulin for activity. Pioglitazone is a potent and selective agonist for peroxisome proliferator-activated receptor-gamma (PPARgamma). Activation of nuclear PPARgamma receptors influences the production of a number of gene products involved in glucose and lipid metabolism. Dosing (Adults): Oral: Monotherapy: Initial: 15-30 mg once daily; if response is inadequate, the dosage may be increased in increments up to 45 mg once daily; maximum recommended dose: 45 mg once daily Combination therapy: Maximum recommended dose: 45 mg/day. With sulfonylureas: Initial: 15-30 mg once daily; dose of sulfonylurea should be reduced if the patient reports hypoglycemia With metformin: Initial: 15-30 mg once daily; it is unlikely that the dose of metformin will need to be reduced due to hypoglycemia With insulin: Initial: 15-30 mg once daily; dose of insulin should be reduced by 10% to 25% if the patient reports hypoglycemia or if the plasma glucose falls to <100 mg/dL. Dosage adjustment in patients with CHF (NYHA Class II) in mono- or combination therapy: Initial: 15 mg once daily; may be increased after several months of treatment, with close attention to heart failure symptoms Elderly: No dosage adjustment is recommended in elderly patients. Dosage adjustment in hepatic impairment: Clearance is significantly lower in hepatic impairment. Therapy should not be initiated if the patient exhibits active liver disease or increased transaminases (>2.5 times the upper limit of normal) at baseline. Supplied Tablet: 15 mg, 30 mg, 45 mg |
rosiglitazone (Avandia ®): |
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INDICATIONS - Type 2 diabetes
mellitus (noninsulin dependent, NIDDM): Monotherapy: Improve glycemic control as an adjunct to diet and exercise. Combination therapy: In combination with a sulfonylurea, metformin, or insulin when diet, exercise, and a single agent do not result in adequate glycemic control. Mechanism of Action Thiazolidinedione antidiabetic agent that lowers blood glucose by improving target cell response to insulin, without increasing pancreatic insulin secretion. It has a mechanism of action that is dependent on the presence of insulin for activity. Dosing (Adults): Oral: Monotherapy: Initial: 4 mg daily as a single daily dose or in divided doses twice daily. If response is inadequate after 12 weeks of treatment, the dosage may be increased to 8 mg daily as a single daily dose or in divided doses twice daily. In clinical trials, the 4 mg twice-daily regimen resulted in the greatest reduction in fasting plasma glucose and Hb A1c. Combination therapy: With sulfonylureas: Initial: 4 mg daily as a single daily dose or in divided doses twice daily; dose of sulfonylurea should be reduced if the patient reports hypoglycemia. Doses of rosiglitazone >4 mg/day are not indicated in combination with sulfonylureas. With metformin: Initial: 4 mg daily as a single daily dose or in divided doses twice daily. If response is inadequate after 12 weeks of treatment, the dosage may be increased to 8 mg daily as a single daily dose or in divided doses twice daily. It is unlikely that the dose of metformin will need to be reduced due to hypoglycemia With insulin: Initial: 4 mg daily as a single daily dose or in divided doses twice daily. Dose of insulin should be reduced by 10% to 25% if the patient reports hypoglycemia or if the plasma glucose falls to <100 mg/dL. Doses of rosiglitazone >4 mg/day are not indicated in combination with insulin. Elderly: No dosage adjustment is recommended Dosage comment in hepatic impairment: Clearance is significantly lower in hepatic impairment. Therapy should not be initiated if the patient exhibits active liver disease of increased transaminases (>2.5 times the upper limit of normal) at baseline. Monitoring Parameters Hemoglobin A1c, serum glucose; signs and symptoms of heart failure; liver enzymes (prior to initiation of therapy, then periodically thereafter). Patients with an elevation in ALT >3 times the upper limit of normal should be rechecked as soon as possible. If the ALT levels remain >3 times the upper limit of normal, therapy with rosiglitazone should be discontinued. Supplied Tablet: 2 mg, 4 mg, 8 mg |
Meglitinides
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Nateglinide (Starlix ®) |
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Management of type 2 diabetes mellitus (noninsulin dependent, NIDDM) as
monotherapy when hyperglycemia cannot be managed by diet and exercise
alone; in combination with metformin or a thiazolidinedione to lower
blood glucose in patients whose hyperglycemia cannot be controlled by
exercise, diet, or a single agent alone Mechanism of Action A phenylalanine derivative, nonsulfonylurea hypoglycemic agent used in the management of type 2 diabetes mellitus (noninsulin dependent, NIDDM); stimulates insulin release from the pancreatic beta cells to reduce postprandial hyperglycemia; amount of insulin release is dependent upon existing glucose levels Dosing (Adults): Management of type 2 diabetes mellitus: Oral: Initial and maintenance dose: 120 mg 3 times/day, 1-30 minutes before meals; may be given alone or in combination with metformin or a thiazolidinedione; patients close to Hb A1c goal may be started at 60 mg 3 times/day Elderly: No changes in safety and efficacy were seen in patients 65 years; however, some elderly patients may show increased sensitivity to dosing. Dosage adjustment in hepatic impairment: Increased serum levels seen with mild hepatic insufficiency; no dosage adjustment is needed. Has not been studied in patients with moderate to severe liver disease; use with caution. Administration Patients who are anorexic or NPO will need to have their dose held to avoid hypoglycemia. Supplied Tablet: 60 mg, 120 mg |
repaglinide (Prandin ®): |
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Management of type 2 diabetes mellitus (noninsulin dependent,
NIDDM); may be used in combination with metformin or
thiazolidinediones Mechanism of Action Nonsulfonylurea hypoglycemic agent of the meglitinide class (the nonsulfonylurea moiety of glyburide) used in the management of type 2 diabetes mellitus; stimulates insulin release from the pancreatic beta cells Dosing (Adults): Oral: Should be taken within 15 minutes of the meal, but time may vary from immediately preceding the meal to as long as 30 minutes before the meal Initial: For patients not previously treated or whose Hb A1c is <8%, the starting dose is 0.5 mg. For patients previously treated with blood glucose-lowering agents whose Hb A1c is >/= 8%, the initial dose is 1 or 2 mg before each meal. Dose adjustment: Determine dosing adjustments by blood glucose response, usually fasting blood glucose. Double the preprandial dose up to 4 mg until satisfactory blood glucose response is achieved. At least 1 week should elapse to assess response after each dose adjustment. Dose range: 0.5-4 mg taken with meals. Repaglinide may be dosed preprandial 2, 3 or 4 times/day in response to changes in the patient's meal pattern. Maximum recommended daily dose: 16 mg. Patients receiving other oral hypoglycemic agents: When repaglinide is used to replace therapy with other oral hypoglycemic agents, it may be started the day after the final dose is given. Observe patients carefully for hypoglycemia because of potential overlapping of drug effects. When transferred from longer half-life sulfonylureas (eg, chlorpropamide), close monitoring may be indicated for up to >/= 1 week. Combination therapy: If repaglinide monotherapy does not result in adequate glycemic control, metformin or a thiazolidinedione may be added. Or, if metformin or thiazolidinedione therapy does not provide adequate control, repaglinide may be added. The starting dose and dose adjustments for combination therapy are the same as repaglinide monotherapy. Carefully adjust the dose of each drug to determine the minimal dose required to achieve the desired pharmacologic effect. Failure to do so could result in an increase in the incidence of hypoglycemic episodes. Use appropriate monitoring of FPG and Hb A1c measurements to ensure that the patient is not subjected to excessive drug exposure or increased probability of secondary drug failure. If glucose is not achieved after a suitable trial of combination therapy, consider discontinuing these drugs and using insulin. Dosing adjustment in renal impairment: Clcr 40-80 mL/minute (mild to moderate renal dysfunction): Initial dosage adjustment does not appear to be necessary. Clcr 20-40 mL/minute: Initiate 0.5 mg with meals; titrate carefully. Supplied Tablet: 0.5 mg, 1 mg, 2 mg |
Sulfonylureas
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Chlorpropamide (Diabinese ®): |
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Mechanism of Action Stimulates insulin release from the pancreatic beta cells; reduces glucose output from the liver; insulin sensitivity is increased at peripheral target sites Dosing (Adults): Oral: The dosage of chlorpropamide is variable and should be individualized based upon the patient's response Initial dose: Adults: 250 mg/day in mild to moderate diabetes in middle-aged, stable diabetic Elderly: 100-125 mg/day in older patients Subsequent dosages may be increased or decreased by 50-125 mg/day at 3- to 5-day intervals Maintenance dose: 100-250 mg/day; severe diabetics may require 500 mg/day; avoid doses >750 mg/day Dosing adjustment/comments in renal impairment: Clcr<50 mL/minute: Avoid use Hemodialysis: Removed with hemoperfusion Peritoneal dialysis: Supplemental dose is not necessary Dosing adjustment in hepatic impairment: Dosage reduction is recommended. Conservative initial and maintenance doses are recommended in patients with liver impairment because chlorpropamide undergoes extensive hepatic metabolism. Supplied Tablet: 100 mg, 250 mg |
glimepiride (Amaryl ®): |
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Sulfonylurea. Management of type 2 diabetes mellitus (noninsulin
dependent, NIDDM) as an adjunct to diet and exercise to lower blood
glucose or in combination with metformin; use in combination with
insulin to lower blood glucose in patients whose hyperglycemia cannot be
controlled by diet and exercise in conjunction with an oral hypoglycemic
agent Mechanism of Action Stimulates insulin release from the pancreatic beta cells; reduces glucose output from the liver; insulin sensitivity is increased at peripheral target sites Dosing (Adults): Oral (allow several days between dose titrations): Adults: Initial: 1-2 mg once daily, administered with breakfast or the first main meal; usual maintenance dose: 1-4 mg once daily; after a dose of 2 mg once daily, increase in increments of 2 mg at 1- to 2-week intervals based upon the patient's blood glucose response to a maximum of 8 mg once daily Combination with insulin therapy (fasting glucose level for instituting combination therapy is in the range of >150 mg/dL in plasma or serum depending on the patient): initial recommended dose: 8 mg once daily with the first main meal After starting with low-dose insulin, upward adjustments of insulin can be done approximately weekly as guided by frequent measurements of fasting blood glucose. Once stable, combination-therapy patients should monitor their capillary blood glucose on an ongoing basis, preferably daily. Dosing adjustment/comments in renal impairment: Clcr<22 mL/minute: Initial starting dose should be 1 mg and dosage increments should be based on fasting blood glucose levels Elderly: Initial: 1 mg/day; dose titration and maintenance dosing should be conservative to avoid hypoglycemia Supplied Tablet: 1 mg, 2 mg, 4 mg |
glyburide (Micronase ®, Diabeta ®): |
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Sulfonylurea. Management of type 2 diabetes mellitus (noninsulin
dependent, NIDDM) Mechanism of Action Stimulates insulin release from the pancreatic beta cells; reduces glucose output from the liver; insulin sensitivity is increased at peripheral target sites Dosing (Adults) Oral: Initial: 2.5-5 mg/day, administered with breakfast or the first main meal of the day. In patients who are more sensitive to hypoglycemic drugs, start at 1.25 mg/day. Increase in increments of no more than 2.5 mg/day at weekly intervals based on the patient's blood glucose response Maintenance: 1.25-20 mg/day given as single or divided doses; maximum: 20 mg/day Elderly: Initial: 1.25-2.5 mg/day, increase by 1.25-2.5 mg/day every 1-3 weeks Micronized tablets (Glynase™ PresTab™): Adults: Initial: 1.5-3 mg/day, administered with breakfast or the first main meal of the day in patients who are more sensitive to hypoglycemic drugs, start at 0.75 mg/day. Increase in increments of no more than 1.5 mg/day in weekly intervals based on the patient's blood glucose response. Maintenance: 0.75-12 mg/day given as a single dose or in divided doses. Some patients (especially those receiving >6 mg/day) may have a more satisfactory response with twice-daily dosing. Dosing adjustment/comments in renal impairment: Clcr<50 mL/minute: Not recommended Dosing adjustment in hepatic impairment: Use conservative initial and maintenance doses and avoid use in severe disease Administration Administer with meals at the same time each day. Patients who are anorexic or NPO may need to have their dose held to avoid hypoglycemia. Supplied Tablet (Diabeta®, Micronase®): 1.25 mg, 2.5 mg, 5 mg Tablet, micronized (Glynase® PresTab®): 1.5 mg, 3 mg, 6 mg |
glipizide (Glucotrol ®): |
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Sulfonylurea. Mechanism of Action Stimulates insulin release from the pancreatic beta cells; reduces glucose output from the liver; insulin sensitivity is increased at peripheral target sites Dosing (Adults) Oral (allow several days between dose titrations): Adults: Initial: 5 mg/day; adjust dosage at 2.5-5 mg daily increments as determined by blood glucose response at intervals of several days. Immediate release tablet: Maximum recommended once-daily dose: 15 mg; maximum recommended total daily dose: 40 mg Extended release tablet (Glucotrol® XL): Maximum recommended dose: 20 mg When transferring from insulin to glipizide: Current insulin requirement </= 20 units: Discontinue insulin and initiate glipizide at usual dose Current insulin requirement >20 units: Decrease insulin by 50% and initiate glipizide at usual dose; gradually decrease insulin dose based on patient response. Several days should elapse between dosage changes. Elderly: Initial: 2.5 mg/day; increase by 2.5-5 mg/day at 1- to 2-week intervals Dosing adjustment/comments in renal impairment: Clcr<10 mL/minute: Some investigators recommend not using Dosing adjustment in hepatic impairment: Initial dosage should be 2.5 mg/day Administration Administer immediate release tablets 30 minutes before a meal to achieve greatest reduction in postprandial hyperglycemia. Extended release tablets should be given with breakfast. Patients who are NPO may need to have their dose held to avoid hypoglycemia. Monitoring Parameters Urine for glucose and ketones; monitor for signs and symptoms of hypoglycemia (fatigue, excessive hunger, profuse sweating, numbness of extremities), fasting blood glucose, hemoglobin A1c, fructosamine Supplied Tablet (Glucotrol®): 5 mg, 10 mg Tablet, extended release: 5 mg, 10 mg (Glucotrol® XL): 2.5 mg, 5 mg, 10 mg |
Tolazamide (Tolinase ®): |
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Adult (usual): Oral (doses >1000 mg/day normally do not improve diabetic control): Initial: 100-250 mg/day with breakfast or the first main meal of the day Fasting blood sugar <200 mg/dL: 100 mg/day Fasting blood sugar >200 mg/: 250 mg/day Patient is malnourished, underweight, elderly, or not eating properly: 100 mg/day AdAdjust dose in increments of 100-250 mg/day at weekly intervals to response. If >500 mg/day is required, give in divided doses twice daily; maximum daily dose: 1 g (doses >1 g/day are not likely to improve control) [Supplied 100 mg , 250 mg , 500 mg tablet] |
Tolbutamide (Orinase ®): |
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Divided doses may improve gastrointestinal tolerance Adults: Oral: Initial: 1-2 g/day as a single dose in the morning or in divided doses throughout the day. Total doses may be taken in the morning; however, divided doses may allow increased gastrointestinal tolerance. Maintenance dose: 0.25-3 g/day; however, a maintenance dose >2 g/day is seldom required. Elderly: Oral: Initial: 250 mg 1-3 times/day; usual: 500-2000 mg; maximum: 3 g/day [Supplied 500 mg tablet] |
Other |
Glucagon:
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Hypoglycemia: 1 mg IV/IM/SC. Onset 5-20min. May repeat in 20
minutes as needed. Note: If patient fails to respond to glucagon, I.V.
dextrose must be given. Beta-blocker overdose: Separate glucagon receptors stimulate adenylcyclase improving heart rate, blood pressure and conduction defects. Adults: 3 - 5 mg (up to 10 mg) IV push (over 1 minute) followed by an IV drip - usually 1 to 5 mg/hour. Note: bolus dose may be repeated in 10 minutes. Usually causes nausea and vomiting. May give Reglan IV, Compazine or Tigan. Diagnostic aid: I.M., I.V.: 0.25-2 mg 10 minutes prior to procedure Monitor blood glucose levels in hypoglycemic patients until they are asymptomatic; effective in treating hypoglycemia only if sufficient liver glycogen is present; since liver glycogen availability is necessary to treat hypoglycemic patients, glucagon has virtually no effects on patients in states of starvation, adrenal insufficiency, or chronic hypoglycemia. (Recommended routes): IM, IV, or SC. Half-life: 8 to 18 minutes. |
exenatide
(Byetta ®):
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Mechanism: Analog of the hormone incretin (glucagon-like
peptide 1 or GLP-1) which increases insulin secretion, increases b-cell
growth/replication, slows gastric emptying, and may decrease food
intake. When added to sulfonylureas and/or metformin, it results in
additional lowering of hbA1c by approximately 0.5% to 1%. Dosing (Adjunctive therapy of type 2 diabetes): Initial: 5 mcg SQ bid within 60 min prior to a meal (morning and evening). After 1 month, may be increased to 10 mcg SQ twice daily (based on response). Renal Not recommended in patients CRCL < 30 ml/min. Supplied: Injection: [prefilled pen]: 250 mcg/ml (1.2 ml) [provides 5 mcg/dose]. 2.4 ml - [provides 10 mcg/dose] |
pramlintide
(Symlin ® )
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Indications: (1) Adjunctive treatment with mealtime insulin in type 1
diabetes mellitus (insulin dependent, IDDM) patients who have failed to
achieve desired glucose control despite optimal insulin therapy. (2)
Adjunctive treatment with mealtime insulin in type 2 diabetes mellitus
(noninsulin dependent, NIDDM) patients who have failed to achieve
desired glucose control despite optimal insulin therapy, with or without
concurrent sulfonylurea and/or metformin. Mechanism: Synthetic analog of human amylin cosecreted with insulin by pancreatic beta cells. Reduces postprandial glucose increases via the following mechanisms: 1) prolongation of gastric emptying time, 2) reduction of postprandial glucagon secretion, and 3) reduction of caloric intake through centrally-mediated appetite suppression. Dosage: Adult (usual): Type 1 diabetes mellitus (insulin dependent) Initial: 15 mcg SQ immediately prior to meals. Titrate in 15 mcg increments every 3 days (if no significant nausea occurs) to target dose of 30-60 mcg (consider discontinuation if intolerant of 30 mcg dose). Note: When initiating pramlintide, reduce current insulin dose (including rapidly and mixed-acting preparations) by 50% to avoid hypoglycemia. Type 2 diabetes mellitus: Initial: 60 mcg SQ immediately prior to meals. After 3-7 days, increase to 120 mcg prior to meals if no significant nausea occurs (if nausea occurs at 120 mcg dose, reduce to 60 mcg). If pramlintide is discontinued for any reason, restart therapy with same initial titration protocol. Administration: Do not mix with other insulins. Administer SQ into abdominal or thigh areas at sites distinct from concomitant insulin injections (do not administer into arm due to variable absorption). Rotate injection sites frequently. For oral medications in which a rapid onset of action is desired, administer 1 hr before, or 2 hrs after pramlintide, if possible. Supplied: Injection: Pramlintide acetate 0.6 mg/ml (5 ml). |
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