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Glucagon

Also known as GlucaGen, GlucaGen HypoKit, Baqsimi, Gvoke, glucagon hydrochloride

Pancreatic alpha-cell hormone used as an emergency treatment for severe hypoglycaemia.

clinically proven Hormonal & sexual approved drug

At a glance

Category
Hormonal & sexual
Status
approved drug
Made from
recombinant Expressed in Saccharomyces cerevisiae (GlucaGen) or in Escherichia coli (Lilly Glucagon); the sequence is identical to human glucagon.
Route
intramuscular, subcutaneous, intravenous, or intranasal (Baqsimi)
Half-life
about 32 minutes after a 1 mg subcutaneous dose, with peak plasma concentration at roughly 50 minutes 4; the intravenous half-life is shorter, of the order of minutes
Onset
blood glucose starts rising within about 10 minutes; most people regain consciousness within 10-15 minutes of an intramuscular dose
Molecular weight
3482.8 g/mol; the label gives 3,483 Da for the 29-residue chain 4
Sequence
HSQGTFTSDYSKYLDSRRAQDFVQWLMNT (29 amino acids, identical in humans and most mammals; produced recombinantly in yeast or E. coli)

Approved in the EU and US for decades as an injectable emergency kit. Newer formulations avoid reconstitution: Baqsimi nasal powder (EU marketing authorisation 16 December 2019 2), Gvoke ready-to-use autoinjector and prefilled syringe (FDA 2019), and the analogue dasiglucagon (Zegalogue). Prescription only, but supplied specifically so that a bystander rather than a clinician can administer it.

Doping status: Not listed by WADA

Checked against the WADA 2026 Prohibited List. For a specific product and country, Global DRO is the lookup athletes are expected to use — the List names substances, not brand names.

Glucagon was formerly extracted from beef and pork pancreas; the recombinant products contain no animal material.

Mechanism of action

Glucagon is secreted by the alpha cells of the pancreatic islets in response to falling blood glucose and is the principal counter-regulatory hormone opposing insulin. It binds the glucagon receptor, a class B G-protein-coupled receptor expressed most densely on hepatocytes. Receptor activation raises intracellular cAMP, activates protein kinase A, and through a phosphorylation cascade activates glycogen phosphorylase while simultaneously inactivating glycogen synthase. The net effect is rapid breakdown of hepatic glycogen and release of glucose into the circulation.

Glucagon also stimulates hepatic gluconeogenesis from amino acids and lactate, promotes fatty acid oxidation and ketogenesis, and suppresses glycolysis. In the therapeutic context of severe hypoglycaemia, however, only the glycogenolytic effect is fast enough to matter.

This dependence on hepatic glycogen defines the drug's limits. Glucagon will not work reliably in someone whose glycogen stores are already depleted — after prolonged fasting or starvation, in alcohol-induced hypoglycaemia, in adrenal insufficiency, or in chronic or prolonged hypoglycaemia. In those situations intravenous glucose is required and glucagon is a distraction. Even when it works, the effect is transient: glucose rises for perhaps 60-90 minutes, then falls again unless carbohydrate is eaten, which is why every label instructs giving oral carbohydrate as soon as the person can swallow safely.

Two effects outside glucose metabolism are exploited clinically. Glucagon relaxes gastrointestinal smooth muscle, which is why it is given as a diagnostic aid during endoscopy and radiological imaging. And it increases heart rate and contractility through hepatic and cardiac cAMP without going through beta-adrenoceptors, which is the rationale for high-dose glucagon in beta-blocker overdose.

Glucagon receptor agonism has also become a design element in metabolic drugs rather than only an emergency treatment: the dual and triple incretin agonists such as survodutide and retatrutide deliberately include glucagon receptor activity to increase energy expenditure alongside GLP-1 and GIP effects.

What the research shows

The evidence for glucagon in severe hypoglycaemia is solid, old and largely uncontroversial: it reliably raises blood glucose in people with intact liver glycogen. The more interesting recent evidence concerns delivery — specifically, whether a lay caregiver in a real emergency can actually administer the drug. On that measure the newer nasal and ready-to-use formulations substantially outperform the traditional reconstitution kit.

Research in humans

Rickels et al. (Diabetes Care, 2016) conducted a randomised crossover non-inferiority study of 3 mg intranasal glucagon versus 1 mg intramuscular glucagon in adults with type 1 diabetes and insulin-induced hypoglycaemia; nasal glucagon met the non-inferiority criterion for glycaemic recovery, with a slightly slower time to response 1. Simulated-emergency studies found that lay caregivers administered a full dose correctly in the large majority of attempts with the nasal device compared with a small minority using the traditional syringe kit — a difference that matters more in practice than any pharmacokinetic distinction. Glucagon's efficacy in beta-blocker and calcium channel blocker poisoning rests on case series and animal data rather than randomised trials.

Animal and lab research

Animal work established the glycogenolytic mechanism and the cardiac effects that underpin the toxicological use. Dog and pig models of beta-blocker overdose provide most of the support for high-dose glucagon in that indication, since randomised human trials do not exist.

Caveats. Glucagon is ineffective in exactly the situations that most often produce severe hypoglycaemia outside diabetes — alcohol, starvation, adrenal insufficiency — which limits its role to insulin- and sulfonylurea-treated diabetes. Nausea and vomiting are frequent enough to be a real hazard in a person who is not fully conscious. Real-world outcome data are limited: most trials use induced hypoglycaemia in a controlled setting, which is not the same as an unconscious person on a kitchen floor. Head-to-head comparisons between the newer formulations are sparse and mostly manufacturer-sponsored.

What it is used for

  • Severe hypoglycaemia in people with diabetes treated with insulin or sulfonylureas, when the person cannot safely swallow carbohydrate 34
  • Diagnostic aid to inhibit gastrointestinal motility during endoscopy, barium studies, CT and MR enterography
  • Beta-blocker and calcium channel blocker overdose, at high doses (off-label but standard toxicology practice)
  • Glucagon stimulation test, used to assess growth hormone and cortisol reserve
  • Impacted oesophageal food bolus, to relax the lower oesophageal sphincter (evidence weak)
  • As a pharmacological principle, glucagon receptor agonism is now a deliberate component of dual and triple incretin agonists developed for obesity and metabolic disease

Dosing

Dose
Severe hypoglycaemia, the indication this product exists for: 1 mg intramuscularly or subcutaneously for adults and children weighing 25 kg or more; 0.5 mg for children under 25 kg or under approximately 6-8 years. The nasal and autoinjector products and the unrelated off-label poisoning dose are described separately in the notes below.
Frequency
A single dose. If there is no response within about 15 minutes, emergency medical services and intravenous glucose are needed; a second dose may be given while waiting if one is available.
Route
Intramuscular into the thigh or buttock, subcutaneous, or intranasal. Intranasal absorption does not depend on the person inhaling, which matters if they are unconscious.
Duration
Single emergency use, not a treatment course
  • Baqsimi nasal powder, severe hypoglycaemia: a single fixed 3 mg dose into one nostril, repeated once after 15 minutes if there is no response. The EU indication covers age 4 and over 2; the US label now covers age 1 and over 3. The 3 mg figure belongs to the nasal route only. It is three times the injected dose because nasal absorption is far less efficient, not because a larger dose is wanted, and it must never be read across to an injection.
  • Gvoke, severe hypoglycaemia: 1 mg by autoinjector or prefilled syringe from age 12, and from age 2 to under 12 either 0.5 mg below 45 kg or 1 mg at 45 kg and above — the same dose as the traditional kit, supplied ready to use 4.
  • Beta-blocker and calcium channel blocker poisoning, off-label, hospital only: 3-10 mg intravenously as a bolus, followed by an infusion titrated to effect. This is a different indication, a different route and roughly ten times the hypoglycaemia dose. It rests on case series and animal data rather than randomised trials, and it has no bearing on how a glucagon rescue kit is used.
  • Call emergency services. Glucagon is a bridge, not a resolution — the label instruction is to seek emergency help, then give oral carbohydrate as soon as the person is awake and able to swallow, to prevent recurrent hypoglycaemia as the effect wears off 4.
  • Turn the person on their side before or immediately after giving glucagon. Vomiting is common and an unconscious person can aspirate; the label gives this instruction explicitly 4.
  • Everyone using insulin, and their household or training partners, should know where the glucagon is kept and how to use it. In practice this is the single most common failure point: the kit exists but nobody present knows how to give it.
  • Glucagon will not work reliably if hepatic glycogen is depleted — the label names starvation, adrenal insufficiency and chronic hypoglycaemia 4, and alcohol-related hypoglycaemia behaves the same way. Intravenous glucose is the answer in those cases.
  • The doses above are the licensed regimens from official product information. This is reference material, not treatment advice.

These figures describe what the literature and published protocols report. They are not advice and not a dosing instruction.

Protocols

GlucaGen HypoKit (severe hypoglycaemia)

approved product information

Source: GLUCAGEN HYPOKIT (glucagon) prescribing information, DailyMed

Adults and children weighing 25 kg or more1 mg (1 mL) subcutaneously or intramuscularly into the upper arm, thigh or buttock
Children under 25 kg, or under 6 years if the weight is unknown0.5 mg (0.5 mL) by the same route
No response after 15 minutesone further dose from a new kit, while waiting for emergency help

A single rescue dose rather than a schedule: emergency services are called immediately after giving it, and carbohydrate is given by mouth as soon as the person can swallow. Glucagon works by mobilising liver glycogen, so it does little in someone whose glycogen is already depleted by starvation, prolonged hypoglycaemia or alcohol.

Baqsimi nasal powder (severe hypoglycaemia, age 4 and over)

approved product information

Source: BAQSIMI (glucagon) nasal powder prescribing information, DailyMed

Single dose3 mg - one actuation into one nostril
No response after 15 minutesa further 3 mg dose from a new device

One fixed dose from age 4 upwards, and it does not have to be inhaled - the powder is absorbed from the nasal mucosa, so it still works in an unconscious person and with a blocked nose.

Schedules are reproduced as their source states them. Units, IU and milligrams explains why the figures are not interchangeable between products.

Reconstitution

Vial sizes
1 mg lyophilised powder vial with a 1 ml prefilled syringe of diluent (traditional emergency kit), 0.5 mg and 1 mg ready-to-use autoinjector or prefilled syringe (Gvoke), 3 mg single-dose nasal device (Baqsimi)
Solvent
Sterile water for injection supplied in the kit's own prefilled syringe — for the traditional lyophilised kits only
Storage
Unreconstituted kits at room temperature, typically below 25 °C, in the original carton and protected from light; do not refrigerate the assembled kit unless the specific label says so, and do not freeze. Baqsimi is stored at up to 30 °C in its shrink-wrapped tube until use. Because these are emergency products, the practical storage rule is that they should be somewhere findable by someone else, and the expiry date should be checked periodically.

Worked example

This is the one entry in this category where reconstitution genuinely applies, and only to the older kits. GlucaGen HypoKit and the classic Lilly Glucagon Emergency Kit contain a vial of freeze-dried glucagon and a syringe of sterile water: inject the entire contents of the syringe into the vial, swirl gently until the solution is clear, withdraw the full dose and inject immediately. The reconstituted solution is for immediate single use and is not stored. Baqsimi, Gvoke and Zegalogue require no reconstitution at all, which is precisely why they were developed.

Do not reconstitute in advance. Do not use if the solution is gel-like, cloudy or discoloured, or if the powder has not fully dissolved. The dose is drawn up in full — glucagon kits are not partial-dose products, other than the fixed paediatric 0.5 mg mark on some syringes.

Work it out for Glucagon

Safety

Side effects

  • Nausea (about 26% with the nasal powder) and vomiting (about 15%), very common 3 — an aspiration hazard in a person who is not fully alert, which is why positioning on the side matters
  • Headache, about 18% with the nasal powder 3
  • Rebound hypoglycaemia once the effect wears off, if carbohydrate is not eaten
  • Transient hyperglycaemia after the dose
  • Tachycardia and a transient rise in blood pressure
  • Hypokalaemia, as glucose entry into cells carries potassium with it
  • Injection site reactions and, with autoinjectors, injection site pain
  • Nasal and upper airway irritation, watery eyes, nasal congestion and sneezing with the nasal powder 3; these are formulation effects, not glucagon effects
  • Hypersensitivity reactions including, rarely, anaphylaxis 4
  • In phaeochromocytoma, glucagon can precipitate a substantial rise in blood pressure by provoking catecholamine release 4

Do not use if

  • Known hypersensitivity to glucagon or to any of the excipients 4
  • Phaeochromocytoma — risk of a substantial increase in blood pressure from catecholamine release 4
  • Insulinoma — glucagon can provoke a paradoxical insulin surge and worse rebound hypoglycaemia 4
  • Glucagonoma, when glucagon is used as a diagnostic aid 4
  • Situations where hepatic glycogen is likely depleted — starvation, prolonged fasting, alcohol-induced hypoglycaemia, adrenal insufficiency, chronic hypoglycaemia 4. Glucagon is not contraindicated so much as unreliable here, and relying on it wastes time that intravenous glucose would use better
  • Caution in known glycogen storage disease

Interactions

Beta-blockers may exaggerate the transient rise in pulse and blood pressure after glucagon 4, though glucagon is also the antidote of choice in beta-blocker overdose at much higher doses. Indometacin can block the glucose-raising effect and may even allow hypoglycaemia to persist 4. Glucagon may potentiate the anticoagulant effect of warfarin 4. Insulin is glucagon's direct physiological antagonist, which is the whole point of the emergency indication. Glucagon may interfere with catecholamine assays and other laboratory tests when used as a diagnostic agent.

Sources