R-Glucagon

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R-Glucagon uses


DESCRIPTION

R-Glucagon for Injection (rDNA origin) is a polypeptidehormone identical to human R-Glucagon that increases blood glucose and relaxessmooth muscle of the gastrointestinal tract. R-Glucagon is synthesized in aspecial non-pathogenic laboratory strain of Escherichiacoli bacteria that has been genetically altered by the additionof the gene for R-Glucagon.

R-Glucagon is a single-chainpolypeptide that contains 29 amino acid residues and has a molecular weightof 3483.

The empirical formula is C153H225N43O49S.The primary sequence of R-Glucagon is shown below.

Crystalline R-Glucagon is a white to off-white powder. It isrelatively insoluble in water but is soluble at a pH of less than 3 or morethan 9.5.

R-Glucagon is available for use intravenously,intramuscularly, or subcutaneously in a kit that contains a vial of sterileglucagon and a syringe of sterile diluent. The vial contains 1 mg (1 unit)of R-Glucagon and 49 mg of lactose. Hydrochloric acid may have been added duringmanufacture to adjust the pH of the R-Glucagon. One International Unit of glucagonis equivalent to 1 mg of R-Glucagon.1 The diluent syringe contains12 mg/mL of glycerin, Water For Injection, and hydrochloric acid.

Primary Sequence of R-Glucagon

CLINICAL PHARMACOLOGY

R-Glucagon increases blood glucose concentration andis used in the treatment of hypoglycemia. R-Glucagon acts only on liver glycogen,converting it to glucose.

R-Glucagon administeredthrough a parenteral route relaxes smooth muscle of the stomach, duodenum,small bowel, and colon.

Pharmacokinetics

R-Glucagon has been studied following intramuscular,subcutaneous, and intravenous administration in adult volunteers. Administrationof the intravenous R-Glucagon showed dose proportionality of the pharmacokineticsbetween 0.25 and 2.0 mg. Calculations from a 1 mg dose showed a small volumeof distribution and a moderate clearance (mean, 13.5 mL/min/kg).The half-life was short, ranging from 8 to 18 minutes.

Maximum plasma concentrations of 7.9 ng/mL were achieved approximately20 minutes after subcutaneous administration (see Figure 1A). Withintramuscular dosing, maximum plasma concentrations of 6.9 ng/mL were attainedapproximately 13 minutes after dosing.

Glucagonis extensively degraded in liver, kidney, and plasma. Urinary excretion ofintact R-Glucagon has not been measured.

Pharmacodynamics

In a study of 25 volunteers, a subcutaneous doseof 1 mg R-Glucagon resulted in a mean peak glucose concentration of 136 mg/dL30 minutes after injection (see Figure 1B). Similarly, followingintramuscular injection, the mean peak glucose level was 138 mg/dL, whichoccurred at 26 minutes after injection. No difference in maximum blood glucoseconcentration between animal-sourced and rDNA glucagon was observed aftersubcutaneous and intramuscular injection.

Figure 1 Mean (±SE) serum R-Glucagon and blood glucose levels after subcutaneous injection of R-Glucagon (1 mg) in 25 normal volunteers

Figure 1A Figure 1B

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INDICATIONS AND USAGE

For the treatment of hypoglycemia:

R-Glucagon is indicated as a treatment for severehypoglycemia.

Because patients with type 1diabetes may have less of an increase in blood glucose levels compared witha stable type 2 patient, supplementary carbohydrate should be given as soonas possible, especially to a pediatric patient.

For use as a diagnostic aid:

R-Glucagon is indicated as a diagnostic aid in theradiologic examination of the stomach, duodenum, small bowel, and colon whendiminished intestinal motility would be advantageous.

Glucagonis as effective for this examination as are the anticholinergic drugs. However,the addition of the anticholinergic agent may result in increased side effects.

CONTRAINDICATIONS

R-Glucagon is contraindicated in patients with knownhypersensitivity to it or in patients with known pheochromocytoma.

WARNINGS

R-Glucagon should be administered cautiously to patientswith a history suggestive of insulinoma, pheochromocytoma, or both. In patientswith insulinoma, intravenous administration of R-Glucagon may produce an initialincrease in blood glucose; however, because of glucagon's hyperglycemiceffect the insulinoma may release insulin and cause subsequent hypoglycemia. A patient developing symptoms of hypoglycemia after a dose of R-Glucagon shouldbe given glucose orally, intravenously, or by gavage, whichever is most appropriate.

Exogenous R-Glucagon also stimulates the release ofcatecholamines. In the presence of pheochromocytoma, R-Glucagon can cause thetumor to release catecholamines, which may result in a sudden and marked increasein blood pressure. If a patient develops a sudden increase in blood pressure,5 to 10 mg of phentolamine mesylate may be administered intravenously in anattempt to control the blood pressure.

Generalized allergic reactions, including urticaria,respiratory distress, and hypotension, have been reported in patients whoreceived R-Glucagon by injection.

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PRECAUTIONS

General

R-Glucagon is effective in treating hypoglycemiaonly if sufficient liver glycogen is present. Because R-Glucagon is of littleor no help in states of starvation, adrenal insufficiency, or chronic hypoglycemia,hypoglycemia in these conditions should be treated with glucose.

Information for Patients

Refer patients and family members to the attachedInformation for the User for instructions describing the method of preparingand injecting R-Glucagon. Advise the patient and family members to become familiarwith the technique of preparing R-Glucagon before an emergency arises. Instructpatients to use 1 mg for adults and 1/2 the adult dose (0.5 mg) [0.5 unit]for pediatric patients weighing less than 44 lb (20 kg).

Patients and family members should be informedof the following measures to prevent hypoglycemic reactions due to insulin:


To prevent severe hypoglycemia, patients andfamily members should be informed of the symptoms of mild hypoglycemia andhow to treat it appropriately.

Family membersshould be informed to arouse the patient as quickly as possible because prolongedhypoglycemia may result in damage to the central nervous system. Glucagonor intravenous glucose should awaken the patient sufficiently so that oralcarbohydrates may be taken.

Patients shouldbe advised to inform their physician when hypoglycemic reactions occur sothat the treatment regimen may be adjusted if necessary.

Laboratory Tests

Blood glucose determinations should be obtainedto follow the patient with hypoglycemia until patient is asymptomatic.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Because R-Glucagon is usually given in a singledose and has a very short half-life, no studies have been done regarding carcinogenesis. In a series of studies examining effects on the bacterial mutagenesis assay, it was determined that an increase incolony counts was related to technical difficulties in running this assaywith peptides and was not due to mutagenic activities of the R-Glucagon.

Reproduction studies have been performed in ratsat doses up to 2 mg/kg R-Glucagon administered two times a day (up to 40 timesthe human dose based on body surface area, mg/m2) and have revealedno evidence of impaired fertility.

Pregnancy

Pregnancy Category B - Reproduction studies have not been performed with recombinantglucagon. However, studies with animal-sourced R-Glucagon were performed inrats at doses up to 2 mg/kg R-Glucagon administered two times a day (up to 40 timesthe human dose based on body surface area, mg/m2), and have revealedno evidence of impaired fertility or harm to the fetus due to R-Glucagon. Thereare, however, no adequate and well-controlled studies in pregnant women. Becauseanimal reproduction studies are not always predictive of human response, thisdrug should be used during pregnancy only if clearly needed.

Nursing Mothers

It is not known whether this drug is excretedin human milk. Because many drugs are excreted in human milk, caution shouldbe exercised when R-Glucagon is administered to a nursing woman. If the drugis excreted in human milk during its short half-life, it will be hydrolyzedand absorbed like any other polypeptide. R-Glucagon is not active when takenorally because it is destroyed in the gastrointestinal tract before it canbe absorbed.

Pediatric Use

For the treatment of hypoglycemia: The use ofglucagon in pediatric patients has been reported to be safe and effective.2-6

For use as a diagnostic aid: Effectiveness hasnot been established in pediatric patients.

Geriatric Use

Clinical studies of R-Glucagon did not include sufficientnumbers of subjects aged 65 and over to determine whether they respond differentlyfrom younger subjects. Other reported clinical experience has not identifieddifferences in responses between the elderly and younger patients. In general,dose selection for an elderly patient should be cautious, usually startingat the low end of the dosing range, reflecting the greater frequency of decreasedhepatic, renal, or cardiac function, and of concomitant disease or other drugtherapy.

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ADVERSE REACTIONS

Severe adverse reactions are very rare, although nauseaand vomiting may occur occasionally. These reactions may also occur with hypoglycemia. Generalized allergic reactions have been reported (see WARNINGS). In athree month controlled study of 75 volunteers comparing animal-sourced glucagonwith R-Glucagon manufactured through rDNA technology, no glucagon-specific antibodieswere detected in either treatment group.

OVERDOSAGE

Signs andSymptoms - If overdosage occurs, nausea, vomiting, gastric hypotonicity,and diarrhea would be expected without causing consequential toxicity.

Intravenous administration of R-Glucagon has been shown tohave positive inotropic and chronotropic effects. A transient increase inboth blood pressure and pulse rate may occur following the administrationof R-Glucagon. Patients taking β-blockers might be expected to have a greaterincrease in both pulse and blood pressure, an increase of which will be transientbecause of glucagon's short half-life. The increase in blood pressureand pulse rate may require therapy in patients with pheochromocytoma or coronaryartery disease.

When R-Glucagon was given inlarge doses to patients with cardiac disease, investigators reported a positiveinotropic effect. These investigators administered R-Glucagon in doses of 0.5 to16 mg/hour by continuous infusion for periods of 5 to 166 hours. Total dosesranged from 25 to 996 mg, and a 21-month-old infant received approximately8.25 mg in 165 hours. Side effects included nausea, vomiting, and decreasingserum potassium concentration. Serum potassium concentration could be maintainedwithin normal limits with supplemental potassium.

Theintravenous median lethal dose for R-Glucagon in mice and rats is approximately300 mg/kg and 38.6 mg/kg, respectively.

Becauseglucagon is a polypeptide, it would be rapidly destroyed in the gastrointestinaltract if it were to be accidentally ingested.

Treatment - To obtain up-to-date information about the treatment of overdose,a good resource is your certified Regional Poison Control Center. Telephonenumbers of certified poison control centers are listed in the Physicians'Desk Reference (PDR). In managing overdosage, consider the possibilityof multiple drug overdoses, interaction among drugs, and unusual drug kineticsin your patient.

In view of the extremely shorthalf-life of R-Glucagon and its prompt destruction and excretion, the treatmentof overdosage is symptomatic, primarily for nausea, vomiting, and possiblehypokalemia.

If the patient develops a dramaticincrease in blood pressure, 5 to 10 mg of phentolamine mesylate has been shownto be effective in lowering blood pressure for the short time that controlwould be needed.

Forced diuresis, peritonealdialysis, hemodialysis, or charcoal hemoperfusion have not been establishedas beneficial for an overdose of R-Glucagon; it is extremely unlikely that oneof these procedures would ever be indicated.

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DOSAGE AND ADMINISTRATION

General Instructions for Use:


Directions for Treatment of Severe Hypoglycemia:

Severe hypoglycemia should be treated initiallywith intravenous glucose, if possible.


Directions for Use as a Diagnostic Aid:

Dissolve the lyophilized R-Glucagon using the accompanyingdiluting solution and use immediately. Discard anyunused portion.

The dosesin the following table may be administered for relaxation of the stomach,duodenum, and small bowel, depending on the onset and duration of effect requiredfor the examination. Since the stomach is less sensitive to the effect ofglucagon, 0.5 mg (0.5 units) IV or 2 mg (2 units) IM are recommended.

* Administration of 2 mg (2 units) doses produces a higher incidence of nausea and vomiting than do lower doses.

Dose Route of Administration Time of Onset of Action Approximate Duration of Effect
0.25-0.5 mg

(0.25-0.5 units)

IV 1 minute 9-17 minutes
1-mg (1 unit) IM 8-10 minutes 12-27 minutes
2 mg* (2 units) IV 1 minute 22-25 minutes
2 mg* (2 units) IM 4-7 minutes 21-32 minutes

For examination of the colon, it is recommendedthat a 2 mg (2 units) dose be administered intramuscularly approximately 10 minutesprior to the procedure. Colon relaxation and reduction of patient discomfortmay allow the radiologist to perform a more satisfactory examination.

HOW SUPPLIED

R-Glucagon Emergency Kit for Low Blood Sugar (MS8031):

1 mg (1 unit) - (VL7529), with 1 mL ofdiluting solution (Hyporet®* HY7530) (1s) NDC 0002-8031-01

___________________________

* Hyporet® (disposablesyringe, Lilly).

Stability and Storage:

BeforeReconstitution - Vials of R-Glucagon, as well as the Diluting Solutionfor R-Glucagon, may be stored at controlled room temperature 20° to 25°C (68° to 77°F)[seeUSP].

The USP defines controlled room temperatureby the following: A temperature maintained thermostatically that encompassesthe usual and customary working environment of 20° to 25°C (68° to 77°F);that results in a mean kinetic temperature calculated to be not more than 25°C;and that allows for excursions between 15° and 30°C (59° and 86°F) that areexperienced in pharmacies, hospitals, and warehouses.

AfterReconstitution - R-Glucagon for Injection (rDNA origin) should beused immediately. Discard any unused portion.

REFERENCES


Literature revised September 19, 2012

Marketed by: Lilly USA, LLC

Indianapolis,IN 46285, USA

PA 2286 AMP

Copyright © 1999, 2012, Eli Lilly and Company. All rights reserved.

INFORMATION FOR THE USER

R-Glucagon

FOR INJECTION

(rDNA ORIGIN)

BECOMEFAMILIAR WITH THE FOLLOWING INSTRUCTIONS BEFORE AN EMERGENCY ARISES. DO NOTUSE THIS KIT AFTER DATE STAMPED ON THE BOTTLE LABEL. IF YOU HAVE QUESTIONSCONCERNING THE USE OF THIS PRODUCT, CONSULT A DOCTOR, NURSE OR PHARMACIST.

Make sure that your relatives or close friends know thatif you become unconscious, medical assistance must always be sought. Glucagonmay have been prescribed so that members of your household can give the injectionif you become hypoglycemic and are unable to take sugar by mouth. If you areunconscious, R-Glucagon can be given while awaiting medical assistance.

Show your family members and others where you keep thiskit and how to use it. They need to know how to use it before you need it. They can practice giving a shot by giving you your normal insulin shots. Itis important that they practice. A person who has never given a shot probablywill not be able to do it in an emergency.

IMPORTANT


WARNING: THEPATIENT MAY BE IN A COMA FROM SEVERE HYPERGLYCEMIA (HIGH BLOOD GLUCOSE) RATHERTHAN HYPOGLYCEMIA. IN SUCH A CASE, THE PATIENT WILL NOT RESPOND TO R-Glucagon AND REQUIRES IMMEDIATE MEDICAL ATTENTION.

INDICATIONS FOR USE

Use R-Glucagon to treat insulincoma or insulin reaction resulting from severe hypoglycemia (low blood sugar).Symptoms of severe hypoglycemia include disorientation, unconsciousness, andseizures or convulsions. Give R-Glucagon if (1) the patient is unconscious (2) thepatient is unable to eat sugar or a sugar-sweetened product (3) the patientis having a seizure, or (4) repeated administration of sugar or a sugar-sweetenedproduct such as a regular soft drink or fruit juice does not improve the patient'scondition. Milder cases of hypoglycemia should be treated promptly by eatingsugar or a sugar-sweetened product. (See INFORMATIONON HYPOGLYCEMIA below for more information on the symptoms of hypoglycemia.)Glucagon is not active when taken orally.

DIRECTIONS FOR USE

TO PREPARE GLUCAGONFOR INJECTION


INFORMATIONON HYPOGLYCEMIA

Early symptomsof hypoglycemia (low blood glucose) include:

  • sweating
  • drowsiness
  • dizziness
  • sleep disturbances
  • palpitation
  • anxiety
  • tremor
  • blurred vision
  • hunger
  • slurred speech
  • restlessness
  • depressed mood
  • tingling in the hands, feet, lips, or tongue
  • irritability
  • lightheadedness
  • abnormal behavior
  • inability to concentrate
  • unsteady movement
  • headache
  • personality changes

If not treated, the patient may progress to severehypoglycemia that can include:

  • disorientation
  • seizures
  • unconsciousness
  • death

The occurrence of early symptoms calls for promptand, if necessary, repeated administration of some form of carbohydrate. Patientsshould always carry a quick source of sugar, such as candy mints or glucosetablets. The prompt treatment of mild hypoglycemic symptoms can prevent severehypoglycemic reactions. If the patient does not improve or if administrationof carbohydrate is impossible, R-Glucagon should be given or the patient shouldbe treated with intravenous glucose at a medical facility. R-Glucagon, a naturallyoccurring substance produced by the pancreas, is helpful because it enablesthe patient to produce his/her own blood glucose to correct the hypoglycemia.

POSSIBLE PROBLEMS WITHGLUCAGON TREATMENT

Severeside effects are very rare, although nausea and vomiting may occur occasionally.

A few people may be allergic to R-Glucagon or to one of theinactive ingredients in R-Glucagon, or may experience rapid heart beat for ashort while.

If you experience any other reactionswhich are likely to have been caused by R-Glucagon, please contact your doctor.

STORAGE

Before dissolving R-Glucagon with dilutingsolution - Store the kit at controlled room temperature between 20° to 25°C(68° to 77°F).

After dissolving R-Glucagon withdiluting solution - Should be used immediately. Discardany unused portion. Solutions should be clear and of a water-likeconsistency at time of use.

Literature revised September 19, 2012

Marketed by: Lilly USA, LLC

Indianapolis, IN 46285, USA

PA 2286 AMP

Copyright © 1999, 2012, Eli Lilly and Company. All rights reserved.

Step 1 Figure Step 2 Figure Step 3 Figure Step 4 Figure

Lilly

Rx only

R-Glucagon Emergency Kit for Low Blood Sugar

R-Glucagon for Injection (rDNA origin) 1 mg (1 unit)

NDC 0002-8031-01

MS8031

Marketed by: Lilly USA, LLC

Indianapolis, IN 46285, USA

R-Glucagon: Product of Austria

Diluting Syringe: Product of Germany

R-Glucagon pharmaceutical active ingredients containing related brand and generic drugs:

Active ingredient is the part of the drug or medicine which is biologically active. This portion of the drug is responsible for the main action of the drug which is intended to cure or reduce the symptom or disease. The other portions of the drug which are inactive are called excipients; there role is to act as vehicle or binder. In contrast to active ingredient, the inactive ingredient's role is not significant in the cure or treatment of the disease. There can be one or more active ingredients in a drug.


R-Glucagon available forms, composition, doses:

Form of the medicine is the form in which the medicine is marketed in the market, for example, a medicine X can be in the form of capsule or the form of chewable tablet or the form of tablet. Sometimes same medicine can be available as injection form. Each medicine cannot be in all forms but can be marketed in 1, 2, or 3 forms which the pharmaceutical company decided based on various background research results.
Composition is the list of ingredients which combinedly form a medicine. Both active ingredients and inactive ingredients form the composition. The active ingredient gives the desired therapeutic effect whereas the inactive ingredient helps in making the medicine stable.
Doses are various strengths of the medicine like 10mg, 20mg, 30mg and so on. Each medicine comes in various doses which is decided by the manufacturer, that is, pharmaceutical company. The dose is decided on the severity of the symptom or disease.


R-Glucagon destination | category:

Destination is defined as the organism to which the drug or medicine is targeted. For most of the drugs what we discuss, human is the drug destination.
Drug category can be defined as major classification of the drug. For example, an antihistaminic or an antipyretic or anti anginal or pain killer, anti-inflammatory or so.


R-Glucagon Anatomical Therapeutic Chemical codes:

A medicine is classified depending on the organ or system it acts [Anatomical], based on what result it gives on what disease, symptom [Therapeutical], based on chemical composition [Chemical]. It is called as ATC code. The code is based on Active ingredients of the medicine. A medicine can have different codes as sometimes it acts on different organs for different indications. Same way, different brands with same active ingredients and same indications can have same ATC code.


R-Glucagon pharmaceutical companies:

Pharmaceutical companies are drug manufacturing companies that help in complete development of the drug from the background research to formation, clinical trials, release of the drug into the market and marketing of the drug.
Researchers are the persons who are responsible for the scientific research and is responsible for all the background clinical trials that resulted in the development of the drug.


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References

  1. Dailymed."GLUCAGON KIT [ELI LILLY AND COMPANY]". https://dailymed.nlm.nih.gov/dailym... (accessed August 28, 2018).

Frequently asked Questions

Can i drive or operate heavy machine after consuming R-Glucagon?

Depending on the reaction of the R-Glucagon after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider R-Glucagon not safe to drive or operate heavy machine after consumption. Meaning that, do not drive or operate heavy duty machines after taking the capsule if the capsule has a strange reaction on your body like dizziness, drowsiness. As prescribed by a pharmacist, it is dangerous to take alcohol while taking medicines as it exposed patients to drowsiness and health risk. Please take note of such effect most especially when taking Primosa capsule. It's advisable to consult your doctor on time for a proper recommendation and medical consultations.

Is R-Glucagon addictive or habit forming?

Medicines are not designed with the mind of creating an addiction or abuse on the health of the users. Addictive Medicine is categorically called Controlled substances by the government. For instance, Schedule H or X in India and schedule II-V in the US are controlled substances.

Please consult the medicine instruction manual on how to use and ensure it is not a controlled substance.In conclusion, self medication is a killer to your health. Consult your doctor for a proper prescription, recommendation, and guidiance.

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Review

sdrugs.com conducted a study on R-Glucagon, and the result of the survey is set out below. It is noteworthy that the product of the survey is based on the perception and impressions of the visitors of the website as well as the views of R-Glucagon consumers. We, as a result of this, advice that you do not base your therapeutic or medical decisions on this result, but rather consult your certified medical experts for their recommendations.

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The information was verified by Dr. Rachana Salvi, MD Pharmacology

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