Is glucagon an antidote for beta-blockers?
Glucagon as an Antidote. Glucagon is traditionally considered a first line antidote for beta-blocker overdose. In Australia, the toxicology community rarely advises the use of glucagon as an antidote, for these reasons:
What is Glucagon used to treat?
Glucagon - StatPearls - NCBI Bookshelf Glucagon is a medication used to manage and treat hypoglycemia as an antidote to beta-blocker and calcium channel blocker overdose, anaphylaxis refractory to epinephrine, and aid in passing food boluses. It is in the anti-hypoglycemic class of medications.
Is glucagon an antidote for calcium channel blockers?
Glucagon has also been used in the setting of calcium channel blocker toxicity In Australia, the toxicology community rarely advises the use of glucagon as an antidote, for these reasons: commonly induces vomiting, with concomitant aspiration risk in the unprotected airway
Why is glucagon not used as an antidote in Australia?
In Australia, the toxicology community rarely advises the use of glucagon as an antidote, for these reasons: commonly induces vomiting, with concomitant aspiration risk in the unprotected airway risk of distraction from the delivery of other therapies (e.g. high-dose insulin as an antidote or supportive measures)
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Why is glucagon antidote for beta blockers?
Because it may bypass the beta-receptor site, glucagon can be considered as an alternative therapy for profound beta-blocker intoxications. The doses of glucagon required to reverse severe beta-blockade are 50 micrograms/kg iv loading dose, followed by a continuous infusion of 1-15 mg/h, titrated to patient response.
What is the antidote for beta blocker overdose?
For cases of beta-blocker poisoning where symptomatic bradycardia and hypotension are present, high-dose glucagon is considered the first-line antidote. For cases of CCB poisoning where cardiotoxicity is evident, a combination of calcium and epinephrine should be used initially, reserving HDIDK for refractory cases.
What is the antidote for adrenergic drugs?
Intravenous fat emulsion (IFE) is a newer antidote that may be utilized in the poisoning of lipid-soluble β-adrenergic antagonists such as propranolol, penbutolol, timolol, metoprolol, carvedilol, and labetalol.
How does glucagon reverse calcium channel blocker overdose?
Glucagon is often referenced as a possible treatment for calcium channel blocker overdose because it can cause increases in heart rate, blood pressure, and cardiac contractility, without regard to calcium channels being blocked. These effects occur because glucagon directly increases cyclic AMP.
What is the antidote for lorazepam?
Lorazepam overdose can be treated with a specific benzodiazepine antidote medication known as flumazenil. This medication may be intravenously administered to help to reverse the effects of lorazepam overdose, but it may contribute to seizure risks.
What is the antidote for amlodipine?
Methylene blue has been proposed as an antidote for refractory shock from amlodipine poisoning because of its vasoconstrictive effects as a nitric oxide scavenger.
What is the antidote for propranolol?
Isoprenaline proved to be the best antidote for the treatment of propranolol intoxication antagonizing the bradycardia by 76% and the hypotension completely. The antagonistic activities of orciprenaline and prenalterol were lower than those of isoprenaline.
Which drug is antidote for calcium gluconate?
Calcium gluconate is used as a cardioprotective agent in high blood potassium. Calcium gluconate is the antidote for magnesium sulfate toxicity.
What is the most toxic beta-blocker?
Propranolol is the most toxic beta-blocker and the most frequently used in suicide attempts worldwide.
How does glucagon increase heart rate?
Glucagon is considered to exert cardiostimulant effects, most notably the enhancement of heart rate and contractility, due to the stimulation of glucagon receptors associated with Gs protein stimulation which causes adenylyl cyclase activation and the consequent increase in 3′,5′-cyclic adenosine monophosphate ...
What is calcium channel blocker overdose?
Calcium channel blocker (CCB) toxicity is one of the most lethal prescription drug overdoses; therefore, understanding the emergent management of such cases is essential. Overdoses of immediate-release CCBs are characterized by rapid progression to hypotension, bradydysrhythmia, and cardiac arrest.
How do you treat an overdose of calcium channel blockers?
Calcium channel blocker (CCB) overdose is often lethal. Conventional medical treatment includes IV calcium, high doses of catecholamines, insulin, and glucagon. A new inotropic drug, levosimendan, should be considered in severe CCB poisoning.
What is the antidote for propranolol?
Isoprenaline proved to be the best antidote for the treatment of propranolol intoxication antagonizing the bradycardia by 76% and the hypotension completely. The antagonistic activities of orciprenaline and prenalterol were lower than those of isoprenaline.
How does insulin reverse beta-blocker overdose?
High dose insulin (HDI) is indicated in cardiogenic shock due to calcium channel blocker (CCB) or beta blocker (BB) overdose. HDI improves cardiac myocyte function by enhancing carbohydrate utilization within the myocyte and via other direct inotropic effects.
What are the symptoms of beta-blocker overdose?
SymptomsIrregular heartbeat.Lightheadedness.Low blood pressure.Rapid or slow heartbeat.Heart failure (shortness of breath and swelling of the legs)Shock (extremely low blood pressure)
Do you give calcium for beta-blocker overdose?
Treatment with calcium salts may provide benefits for hypotensive patients who overdosed on beta-blockers alone or in combination with a calcium channel blocker. Cases refractory to fluids, atropine, and glucagon should be considered candidates for high-dose insulin, euglycemia (HIE) treatment.
What is glucagon used for?
Glucagon is a medication used to manage and treat hypoglycemia as an antidote to beta-blocker and calcium channel blocker overdose, anaphylaxis refractory to epinephrine, and aid in passing food boluses. It is in the anti-hypoglycemic class of medications. This activity describes the indications, actions, and contraindications for glucagon as a valuable agent in the management of acute hypoglycemia, beta-blocker and calcium channel blocker overdose, refractory anaphylaxis, and esophageal obstruction due to food bolus. This activity will highlight the mechanism of action, adverse event profile, and other key factors (e.g., off-label uses, dosing, pharmacodynamics, pharmacokinetics, monitoring, relevant interactions) pertinent for members of the healthcare team in managing patients with the indicated conditions.
How long should you monitor after glucagon injection?
Monitoring is recommended for up to 2 hours after administration due to the medication's duration of action.
What receptors do glucagon bind to?
Glucagon binds G-coupled surface receptors found throughout the body in varying concentrations; binding to the glucagon receptors in the liver, GI tract, heart, pancreas, fat, adrenal glands, and kidneys activate adenylate cyclase, which in turn raises cAMP levels. cAMP stimulates glycogenolysis and glucogenesis, resulting in the release of glucose, primarily from liver glycogen stores. The extrahepatic effects of glucagon are also mediated by adenylate cyclase, including relaxation of GI smooth muscle and positive inotropic effects. [9][10]
Does glucagon cause nausea?
Nausea is the most frequently encountered adverse effect of glucagon administration, with an incidence as high as 35% in some studies. Hypertension has been described up to 2 hours following administration for GI cases due to the inotropic effects of glucagon. Additionally, severe anaphylactic reactions, including hypotension, rash, and vomiting, have been observed due to the protein structure. Hypersensitivity reactions are rare, and most have occurred in the endoscopic setting with IV administration. Adverse reactions from glucagon administration become more likely with the IV route and when giving higher doses. [14][15]
Is glucagon safe for diabetics?
Severe hypoglycemia is a life-threatening event treated with oral carbohydrate intake, IV glucose, or glucagon by various routes. Glucagon has attractive traits in the diabetic population due to its simplicity of use and safe administration, not requiring patent IV access. Patients with decreased levels of consciousness cannot safely consume the oral carbohydrates needed to raise their blood sugar without risk of aspiration, and obtaining IV access can be problematic in the diabetic population, which can prevent prompt administration of IV glucose. IV glucose also runs the risk of severe tissue necrosis in the setting of IV medication extravasation. Glucagon is a reliable method of raising the patient's glucose and relieving severe hypoglycemia long enough for more definitive correction of the patient's glucose levels by mouth, particularly when IV access is unavailable to the provider or has failed. [4]
Is glucagon a polypeptide?
Glucagon is a polypeptide hormone commonly used in the treatment of severe hypoglycemia with FDA approval for the treatment of severe hypoglycemia and as a diagnostic aid in imaging of the GI tract. Glucagon has several off-label indications, including beta-blocker overdose therapy, calcium channel blocker overdose adjunctive therapy, and medical treatment of esophageal food impaction. Glucagon's indications have continued to develop since its discovery, and research is ongoing to treat asthmatic bronchospasm as a constituent in bi-hormonal artificial pancreases and more traditional insulin and the treatment of arrhythmias secondary to cardiac anaphylaxis. [1][2][3]
Can glucagon be administered intranasally?
Glucagon can be administered IV as a bolus or infusion, IM, subcutaneously, and intranasally. Glucagon is available as a dehydrated powder termed a "Glucagon Emergency Kit," which is reconstituted with supplied sterile water or as a purpose formulated intranasal spray. Similar to epinephrine auto-injectors, a pre-filled glucagon injector has received approval, which injects into the patient's thigh. Healthcare providers will most often encounter the emergency kit formulation necessitating reconstitution before injecting the medication, but the intranasal spray may be encountered with increasing frequency in hypoglycemia kits for layperson use. The intranasal powder requires no preparation, and administration is via a spray into the patient's nose while holding the other nare closed. [11][12][13][14]
How should I use glucagon?
Use glucagon exactly as prescribed by your doctor. Hypoglycemia should be treated as quickly as possible. Having low blood sugar for too long can cause seizure, coma, or death.
How to keep glucagon from being hypoglycemic?
To keep from having severe hypoglycemia, follow your diet, medication, and exercise routines very closely. Store glucagon and any diluent at room temperature, away from moisture, heat, and light. Do not refrigerate or freeze.
What other drugs will affect glucagon?
This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed here. Tell your doctor about all medicines you start or stop using.
What hormone increases blood sugar?
Glucagon is a hormone that increases blood sugar levels. It also slows involuntary muscle movements of the stomach and intestines that aid in digestion.
When should glucagon be used?
Glucagon should be used to treat hypoglycemia only if the person is unable to eat, or is unconscious or having a seizure.
What are the symptoms of glucagon allergy?
Get emergency medical help if you have signs of an allergic reaction to glucagon: hives; difficulty breathing; fast or slow heartbeat; swelling of your face, lips, tongue, or throat.
Where is glucagon injected?
Glucagon is injected under the skin, into a muscle, or into a vein. You will be shown how to use the emergency injections for severe hypoglycemia. Call your doctor after each time you use a glucagon injection. Read and carefully follow any Instructions for Use provided with your medicine.
Usual Adult Dose for Diagnostic
For relaxation of the stomach, duodenal bulb, duodenum, and small bowel: IV: 0.2 mg to 0.5 mg IV prior to procedure IM: 1 mg IM prior to procedure For relaxation of the colon: IV: 0.5 mg to 0.75 mg IV prior to procedure IM: 1 mg to 2 mg IM prior to procedure Comments: -May be given IV or IM; onset of action will depend on the route of administration and the organ under examination. -This drug is not recommended in combination with anticholinergic agents due to the possibility of increased side effects. -After completion of the diagnostic procedure, oral carbohydrates should be given to patients who have been fasting as long as it is compatible with the procedure performed. Use: As diagnostic aid during radiologic examinations to temporarily inhibit movement of the gastrointestinal tract..
Usual Adult Dose for Hypoglycemia
Glucagon Emergency Kit and GlucaGen HypoKit: 1 mg IM/IV or subcutaneously once GVOKE Auto-Injector and Prefilled Syringes: 1 mg subcutaneously once REPEAT DOSE: An unconscious patient will usually awaken within 15 minutes following treatment; if response is delayed, may repeat dose while waiting for emergency assistance Nasal: 1 actuation (3 mg) into 1 nostril once -If there is no response after 15 minutes, may administer an additional 3 mg dose from a new device while waiting for emergency assistance Comments: -Administer IV only under medical supervision. -Patients should receive supplemental carbohydrates as soon as possible to restore liver glycogen and prevent recurrence of hypoglycemia. -Patients who do not respond should receive IV glucose. Use: For the treatment of severe hypoglycemia..
Usual Pediatric Dose for Hypoglycemia
Glucagon Emergency Kit and GlucaGen HypoKit: WEIGHT-BASED DOSING: Glucagon: Less than 20 kg: 0.5 mg (or 20 to 30 mcg/kg) IM/IV or subcutaneously once Glucagon: 20 kg or greater: 1 mg IM/IV or subcutaneously once GlucaGen: Less than 25 kg: 0.5 mg IM/IV or subcutaneously once GlucaGen: 25 kg or greater: 1 mg IM/IV or subcutaneously once AGE-BASED DOSING (when weight is unknown): Less than 6 years: 0.5 mg IM/IV or subcutaneously once 6 years or older: 1 mg IM/IV or subcutaneously once GVOKE Auto-Injector and Prefilled Syringes: 2 to 12 years (weight less than 45 kg): 0.5 mg subcutaneously once 2 to 12 years (weight 45 kg or greater): 1 mg subcutaneously once 12 years or older: 1 mg subcutaneously once REPEAT DOSE: An unconscious patient will usually awaken within 15 minutes following treatment; if response is delayed, may repeat dose while waiting for emergency assistance NASAL: 4 years or older: 1 actuation (3 mg) into 1 nostril once -If there is no response after 15 minutes, an additional 3 mg dose from a new device may be administered while waiting for emergency assistance Comments: -Administer IV only under medical supervision. -After patient has responded to treatment, supplemental carbohydrates should be given to restore liver glycogen and prevent recurrence of hypoglycemia. -Patients who do not respond should receive IV glucose. Uses: For the treatment of severe hypoglycemia. -Gvoke auto-injector and prefilled syringes for subcutaneous use are indicated in patients 2 years or older; Baqisimi nasal powder is indicated in patients 4 years or older..
Dose Adjustments
Elderly Patients: Diagnostic use: Dosing should be conservative, usually starting at the low end of the dosing range.
Precautions
CONTRAINDICATIONS: -Hypersensitivity to active substance or any product excipients; anaphylactic shock with breathing difficulties and hypotension have been reported -Pheochromocytoma because of risk of substantial increase in blood pressure -Insulinoma because of risk of hypoglycemia -Glucagonoma (when used as a diagnostic aid) due to risk of hypoglycemia Safety and efficacy for use as a diagnostic aid have not been established in patients younger than 18 years. Safety and efficacy of nasal administration have not been established in patients younger than 4 years. Safety and efficacy of Gvoke autoinjector and prefilled syringes have not been established in patients younger than 2 years. Consult WARNINGS section for additional precautions..
Other Comments
Administration advice: Nasal Use: -Do not push the plunger or test device prior to administration; each tube contains 1 device/1 dose; store in shrink wrapped tube until ready to use -Administer 1 actuation into 1 nostril by inserting tip of intranasal device into 1 nostril and pressing device plunger all the way until the green line is no longer showing; the dose does not need to be inhaled -If there is no response after 15 minutes, administer a second dose from a new device Parenteral Use: Glucagon Emergency Kit and GlucaGen HypoKit: -Completely dissolve powder with diluent provided in the kit; shake vial gently until dissolved; use immediately after reconstitution; discard any unused portion; if a second injection is needed, use a new kit -Administer IV, IM or subcutaneously; common injection sites include upper arms, thighs, or buttocks GVOKE Auto-Injector and Prefilled Syringes: -Do not open foil pouch until ready to administer -Administer subcutaneously in lower abdomen, outer thigh, or outer upper arm -Do not attempt to reuse; each device contains a single dose and cannot be reused Treatment of Severe Hypoglycemia: -Caregivers, family members, and school personnel may safely administer this drug after receiving proper instruction; emergency assistance should be sought immediately after administration -An unconscious patient will usually awaken within 15 minutes following treatment; if there is no response after 15 minutes, a second dose should be given while waiting for emergency assistance As a Diagnostic Aid: Restricted to use by medical personnel -The GlucaGen diagnostic kits and GlucaGen 10-packs are not intended to treat severe hypoglycemia because they are not packaged with a syringe and diluent necessary for rapid preparation and administration during an emergency -Completely dissolve powder with diluent provided or with 1 mL of sterile water for reconstitution; shake vial gently until dissolved Storage requirements: -Store at room temperature in original package; protect from light; do not freeze --Glucagon Emergency Kit and GlucaGen HypoKit: Use immediately after reconstitution; discard any unused portion --Gvoke Autoinjector and Prefilled Syringes: Store in original sealed foil pouch until time of use --Nasal: Store in shrink wrapped tube until ready to use; if tube has been opened, moisture may cause the product to be ineffective; discard tube after use General: -An unconscious person experiencing severe hypoglycemia will usually awaken within 15 minutes following glucagon administration; if response is delayed, a second dose may be administered; emergency aid should be sought so that IV glucose may be given if needed. -Once patient has responded to treatment for severe hypoglycemia, supplemental carbohydrates should be taken as soon as possible to restore liver glycogen and prevent recurrence of hypoglycemia. -When used as a diagnostic aid, oral carbohydrates should be given to patients who have been fasting as long as it is compatible with the procedure performed. Monitoring: -Severe hypoglycemia; Blood glucose should be obtained until patient is asymptomatic Patient advice: -Patients should be instructed to read the FDA-approved patient labeling (Patient Information and Instructions for Use) -Patients, family members, and caregivers should understand that severe hypoglycemia is a medical emergency and emergency medical assistance should be sought immediately after administering glucagon. -Patients, family members, and caregivers should be familiar with preparation and product use prior to the emergence of severe hypoglycemia; his/her physician should be informed each time a severe hypoglycemic reaction occurs. -Patients should understand that hypoglycemia affects a person's ability to concentrate and therefore tasks that require these abilities such as driving should be avoided until the risk of hypoglycemia is minimized..
Further information
Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
Does glucagon reverse depression?
The effects of glucagon in reversing the cardiovascular depression of profound beta-block ade, including its mechanism of action, onset and duration of action, dosage and administration, cost and availability, and side effects are reviewed.
Does glucagon increase heart rate?
Glucagon increases heart rate and myocardial contractility, and improves atrioventricular conduction. These effects are unchanged by the presence of beta-receptor blocking drugs. This suggests that glucagon's mechanism of action may bypass the beta-adrenergic receptor site.
Can glucagon be used for beta blocker overdose?
Two cases of severe beta-blocker overdose are presented that were treated successfully with glucagon therapy. The effects of glucagon in reversing the cardiovascular depression of profound beta-blockade, including its mechanism of action, onset and duration of action, dosage and administration, cost …
How long does it take for glucagon to be administered?
Intramuscular or Intravenous dosage. Adults. 0.5 to 1 mg of glucagon IM or IV after 1 hour of coma. If patient does not awaken after 10 to 25 minutes, the dose may be repeated. For patients in a deep state of coma, IV dextrose should be administered in addition to glucagon for a more immediate response.
How long does glucagon last?
The time to maximum hyperglycemic activity is dependent upon the route of administration. The onset and duration of GI smooth muscle effects depends on dose and route of administration. The metabolism of glucagon has not been clearly defined, but it is extensively degraded by the liver, kidneys, and plasma. The plasma half-life of IV glucagon is approximately 8 to 18 minutes. [52413] The half-life of intranasal glucagon is 35 minutes and 45 minutes for intramuscular injection. [28627] [64497]
How does glucagon affect blood glucose?
Native human glucagon is a hormone synthesized by the alpha-2 cells of the pancreatic islets of Langerhans and acts to increase blood glucose. Glucagon increases blood glucose concentration by activating hepatic glucagon receptors, there by stimulating glycogen breakdown and release of glucose from the liver . Hepatic stores of glycogen are necessary for glucagon to produce an antihypoglycemic effect. As a result, blood glucose levels are increased within minutes of glucagon administration. Blood glucose concentration increase within 10 minutes of injection, with maximal blood glucose levels occurring 30 to 45 minutes after injection, depending on the route of administration. The duration of hyperglycemic action after intravenous or intramuscular injection is 60 to 90 minutes.
How much glucagon should I take for a stricture?
1 mg (dose range: 0.5 to 2 mg) IV has been used with some success. A second dose administered 5 to 10 minutes later is appropriate if needed. Limited data exist on the clinical application of this treatment, and although considered safe, its efficacy is variable. Glucagon is less effective in patients with structural abnormalities (i.e., strictures or rings) of the esophagus. In some patients, glucagon may promote spontaneous passage of an impacted foreign body by relaxing the lower esophageal sphincter; however, its use should not delay definitive endoscopic removal.
How much glucagon should I take?
Of note, FDA-approved product labeling does not provide specific recommendations for neonatal dosing, and there is a wide variance between the doses reported in the literature and pediatric doses recommended by the product labeling. In addition, recommendations from product labeling vary by specific product. For glucagon (recombinant by Eli Lilly), 0.02 to 0.03 mg/kg/dose or 0.5 mg/dose for patients weighing less than 20 kg is the recommended dose. For GlucaGen, 0.5 mg/dose for patients weighing less than 25 kg is recommended.
How long does glucagon affect the stomach?
The duration of hyperglycemic action after intravenous or intramuscular injection is 60 to 90 minutes. Extra hepatic effects of glucagon include relaxation of the smooth muscle of the stomach, duodenum, small bowel, and colon. The exact mechanism by which glucagon exerts its effects on GI smooth muscle are unknown.
How to inform patients of hypoglycemia?
Advise patients to avoid driving or operating machinery until ingesting a meal. Advise patients to inform their health care provider if hypoglycemia occurs so that treatment may be given if necessary. When used as a diagnostic aid in patients with diabetes mellitus, glucagon may cause hyperglycemia; monitor such patients for changes in blood glucose levels during treatment.
