Guanidine: Difference between revisions

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{{DrugProjectFormSinglePage
{{DrugProjectFormSinglePage
|authorTag=<!--Overview-->
|authorTag={{AV}}<!--Overview-->
|genericName=guanidine hydrochloride
|genericName=guanidine hydrochloride
|aOrAn=a
|aOrAn=a
|drugClass=cholinesterase inhibitor
|drugClass=[[cholinesterase inhibitor]]
|indicationType=treatment
|indicationType=treatment
|indication=muscle weakness and easy fatigability associated with the myasthenic syndrome of Eaton-Lambert
|indication=muscle weakness and [[easy fatigability]] associated with the [[Eaton-Lambert syndrome|myasthenic syndrome of Eaton-Lambert]]
|adverseReactions=<!--Black Box Warning-->
|adverseReactions=<!--Black Box Warning-->
|blackBoxWarningTitle=Title
|blackBoxWarningTitle=Title
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<!--FDA-Labeled Indications and Dosage (Adult)-->
<!--FDA-Labeled Indications and Dosage (Adult)-->
|fdaLIADAdult=*Guanidine is indicated for the reduction of the symptoms of muscle weakness and easy fatigability associated with the myasthenic syndrome of Eaton-Lambert. It is not indicated for treating myasthenia gravis. The Eaton-Lambert syndrome is ordinarily differentiated from myasthenia gravis by the usual association of the syndrome with small cell carcinoma of the lung, but myography may be necessary to make the diagnosis.
|fdaLIADAdult=*Guanidine is indicated for the reduction of the symptoms of [[muscle weakness]] and [[easy fatigability]] associated with the myasthenic syndrome of Eaton-Lambert. It is not indicated for treating [[myasthenia gravis]]. The [[Eaton-Lambert syndrome]] is ordinarily differentiated from [[myasthenia gravis]] by the usual association of the syndrome with [[small cell carcinoma]] of the lung, but [[myography]] may be necessary to make the diagnosis.
=====Dosage=====
=====Dosage=====
*Initial dosage is usually between 10 and 15 mg/kg (5 to 7 mg/pound) of body weight per day in 3 or 4 divided doses. This dosage may be gradually increased to a total daily dosage of 35 mg/kg (16 mg/pound) of body weight per day or up to the development of side effects. As individual tolerance is highly variable, the dosage must be carefully titrated. Once a tolerable dose has been established, it should be continued. Occasionally removal of the primary neoplastic lesion may result in improvement of symptoms, permitting the discontinuance of guanidine.
*Initial dosage is usually between 10 and 15 mg/kg (5 to 7 mg/pound) of body weight per day in 3 or 4 divided doses. This dosage may be gradually increased to a total daily dosage of 35 mg/kg (16 mg/pound) of body weight per day or up to the development of side effects. As individual tolerance is highly variable, the dosage must be carefully titrated. Once a tolerable dose has been established, it should be continued. Occasionally removal of the primary neoplastic lesion may result in improvement of symptoms, permitting the discontinuance of guanidine.
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<!--Contraindications-->
<!--Contraindications-->
|contraindications=*Guanidine is contraindicated in individuals with a history of intolerance or allergy to this drug.
|contraindications=*Guanidine is contraindicated in individuals with a history of intolerance or [[allergy]] to this drug.


<!--Warnings-->
<!--Warnings-->
|warnings=*Fatal bone-marrow suppression, apparently dose related, can occur with guanidine.
|warnings=*Fatal [[bone-marrow suppression]], apparently dose related, can occur with guanidine.


*Safe use of guanidine hydrochloride in pregnancy has not been established. Therefore, the benefits of therapy must be weighed against the potential hazards. Because guanidine is excreted in milk, patients on this drug should discontinue breastfeeding.
*Safe use of guanidine hydrochloride in pregnancy has not been established. Therefore, the benefits of therapy must be weighed against the potential hazards. Because guanidine is excreted in milk, patients on this drug should discontinue [[breastfeeding]].


*Since there is inadequate experience in children who have received this drug, safety and efficacy in children have not been established.
*Since there is inadequate experience in children who have received this drug, safety and efficacy in children have not been established.
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====Precautions====
====Precautions====


*Baseline blood studies should be followed by frequent red and white blood cell and differential counts. The drug should be discontinued upon appearance of bone-marrow suppression. Concurrent therapy with other drugs that may cause bone-marrow suppression should be avoided.
*Baseline blood studies should be followed by frequent red and [[white blood cell]] and differential counts. The drug should be discontinued upon appearance of bone-marrow suppression. Concurrent therapy with other drugs that may cause bone-marrow suppression should be avoided.


*Renal function may be affected in some patients receiving guanidine. Patients should therefore have regular urine examinations and serum creatinine determinations while taking this drug.
*Renal function may be affected in some patients receiving guanidine. Patients should therefore have regular urine examinations and [[serum creatinine]] determinations while taking this drug.


*Physicians should be given adequate precautions pertaining to the gastrointestinal side effects and the possibility of induced behavior disorders.
*Physicians should be given adequate precautions pertaining to the gastrointestinal side effects and the possibility of induced behavior disorders.
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<!--Clinical Trials Experience-->
<!--Clinical Trials Experience-->
|clinicalTrials=*Anemia, leukopenia, and thrombocytopenia resulting from bone-marrow suppression attributable to guanidine have been reported. Other adverse reactions that have been observed are:
|clinicalTrials=*[[Anemia]], [[leukopenia]], and [[thrombocytopenia]] resulting from [[bone-marrow suppression]] attributable to guanidine have been reported. Other adverse reactions that have been observed are:


*General: sore throat, rash, fever.
*General: [[sore throat]], [[rash]], [[fever]].


*Neurologic: paresthesia of lips, face, hands, feet; cold sensations in hands and feet; nervousness, lightheadedness, jitteriness, increased irritability; tremor, trembling sensation; ataxia; emotional lability; psychotic state; confusion; mood changes, and hallucinations.
*Neurologic: [[paresthesia]] of lips, face, hands, feet; cold sensations in hands and feet; [[nervousness]], [[lightheadedness]], [[jitteriness]], increased irritability; [[tremor]], trembling sensation; [[ataxia]]; [[emotional lability]]; psychotic state; [[confusion]]; mood changes, and [[hallucinations]].


*Gastrointestinal: dry mouth; gastric irritation; anorexia; nausea; diarrhea; abdominal cramping. Gastrointestinal side effects may preclude the use of guanidine as a desired form of therapy.
*Gastrointestinal: [[dry mouth]]; gastric irritation; [[anorexia]]; [[nausea]]; [[diarrhea]]; abdominal cramping. Gastrointestinal side effects may preclude the use of guanidine as a desired form of therapy.


*Dermatologic: rash, flushing or pink complexion; folliculitis; petechiae, purpura, ecchymoses; sweating; skin eruptions; dryness and scaling of the skin.
*Dermatologic: [[rash]], [[flushing]] or pink complexion; [[folliculitis]]; [[petechiae]], [[purpura]], [[ecchymoses]]; [[sweating]]; skin eruptions; [[dryness]] and scaling of the skin.


*Renal: elevation of blood creatinine, uremia; chronic interstitial nephritis, acute interstitial nephritis, and renal tubular necrosis.
*Renal: elevation of [[blood creatinine]], [[uremia]]; [[chronic interstitial nephritis]], [[acute interstitial nephritis]], and [[renal tubular necrosis]].


*Hepatic: abnormal liver function tests.
*Hepatic: abnormal [[liver function tests]].


*Cardiac: palpitation, tachycardia, atrial fibrillation, hypotension.
*Cardiac: [[palpitation]], [[tachycardia]], [[atrial fibrillation]], [[hypotension]].
<!--Postmarketing Experience-->
<!--Postmarketing Experience-->
|postmarketing=There is limited information regarding <i>Postmarketing Experience</i> of {{PAGENAME}} in the drug label.
|postmarketing=There is limited information regarding <i>Postmarketing Experience</i> of {{PAGENAME}} in the drug label.
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|useInGender=There is no FDA guidance on the use of {{PAGENAME}} with respect to specific gender populations.
|useInGender=There is no FDA guidance on the use of {{PAGENAME}} with respect to specific gender populations.
|useInRace=There is no FDA guidance on the use of {{PAGENAME}} with respect to specific racial populations.
|useInRace=There is no FDA guidance on the use of {{PAGENAME}} with respect to specific racial populations.
|useInRenalImpair=There is no FDA guidance on the use of {{PAGENAME}} in patients with renal impairment.
|useInRenalImpair=There is no FDA guidance on the use of {{PAGENAME}} in patients with [[renal impairment]].
|useInHepaticImpair=There is no FDA guidance on the use of {{PAGENAME}} in patients with hepatic impairment.
|useInHepaticImpair=There is no FDA guidance on the use of {{PAGENAME}} in patients with [[hepatic impairment]].
|useInReproPotential=There is no FDA guidance on the use of {{PAGENAME}} in women of reproductive potentials and males.
|useInReproPotential=There is no FDA guidance on the use of {{PAGENAME}} in women of reproductive potentials and males.
|useInImmunocomp=There is no FDA guidance one the use of {{PAGENAME}} in patients who are immunocompromised.
|useInImmunocomp=There is no FDA guidance one the use of {{PAGENAME}} in patients who are [[immunocompromised]].


<!--Administration and Monitoring-->
<!--Administration and Monitoring-->
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<!--Overdosage-->
<!--Overdosage-->
|overdose=*Mild gastrointestinal disorders, such as anorexia, increased peristalsis, or diarrhea are early warnings that tolerance is being exceeded. These symptoms may be relieved by atropine, but nevertheless note should be taken of these symptoms and dosage reductions considered. Slight numbness or tingling of the lips and fingertips shortly after taking a dose of guanidine has been reported. This per se is not an indication to discontinue treatment and/or reduce dosage.
|overdose=*Mild gastrointestinal disorders, such as [[anorexia]], increased peristalsis, or [[diarrhea]] are early warnings that tolerance is being exceeded. These symptoms may be relieved by [[atropine]], but nevertheless note should be taken of these symptoms and dosage reductions considered. Slight [[numbness]] or tingling of the lips and fingertips shortly after taking a dose of guanidine has been reported. This per se is not an indication to discontinue treatment and/or reduce dosage.


*Severe guanidine intoxication is characterized by nervous hyperirritability, fibrillary tremors and convulsive contractions of muscle, salivation, vomiting, diarrhea, hypoglycemia, and circulatory disturbances. Administration of intravenous calcium gluconate may control the neuromuscular and convulsive symptoms and provide some relief of other toxic manifestations.
*Severe guanidine intoxication is characterized by nervous [[hyperirritability]], fibrillary [[tremors]] and convulsive contractions of muscle, [[salivation]], [[vomiting]], [[diarrhea]], [[hypoglycemia]], and circulatory disturbances. Administration of intravenous [[calcium gluconate]] may control the neuromuscular and convulsive symptoms and provide some relief of other toxic manifestations.


*Atropine is more effective than calcium in relieving the G.I. symptoms, circulatory disturbances, and changes in blood sugar.
*Atropine is more effective than [[calcium]] in relieving the G.I. symptoms, circulatory disturbances, and changes in blood sugar.
<!--Pharmacology-->
<!--Pharmacology-->


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<!--Mechanism of Action-->
<!--Mechanism of Action-->
|mechAction=* Guanidine apparently acts by enhancing the release of acetylcholine following a nerve impulse. It also appears to slow the rates of depolarization and repolarization of muscle cell membranes
|mechAction=* Guanidine apparently acts by enhancing the release of [[acetylcholine]] following a nerve impulse. It also appears to slow the rates of depolarization and repolarization of muscle cell membranes


<!--Structure-->
<!--Structure-->
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: [[File:{{PAGENAME}}01.png|thumb|none|400px|This image is provided by the National Library of Medicine.]]
: [[File:{{PAGENAME}}01.png|thumb|none|400px|This image is provided by the National Library of Medicine.]]
*Each tablet contains 125 mg of guanidine hydrochloride with no color additive in the base. It also contains the following inactive ingredients: colloidal silicon dioxide, magnesium stearate, mannitol, and microcrystalline cellulose.
*Each tablet contains 125 mg of guanidine hydrochloride with no color additive in the base. It also contains the following inactive ingredients: colloidal [[silicon dioxide]], magnesium stearate, [[mannitol]], and microcrystalline [[cellulose]].


<!--Pharmacodynamics-->
<!--Pharmacodynamics-->

Revision as of 13:05, 22 April 2015

Guanidine
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Aparna Vuppala, M.B.B.S. [2]

Disclaimer

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Overview

Guanidine is a cholinesterase inhibitor that is FDA approved for the treatment of muscle weakness and easy fatigability associated with the myasthenic syndrome of Eaton-Lambert. Common adverse reactions include .

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Dosage
  • Initial dosage is usually between 10 and 15 mg/kg (5 to 7 mg/pound) of body weight per day in 3 or 4 divided doses. This dosage may be gradually increased to a total daily dosage of 35 mg/kg (16 mg/pound) of body weight per day or up to the development of side effects. As individual tolerance is highly variable, the dosage must be carefully titrated. Once a tolerable dose has been established, it should be continued. Occasionally removal of the primary neoplastic lesion may result in improvement of symptoms, permitting the discontinuance of guanidine.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Guanidine in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Guanidine in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding FDA-Labeled Use of Guanidine in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Guanidine in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Guanidine in pediatric patients.

Contraindications

  • Guanidine is contraindicated in individuals with a history of intolerance or allergy to this drug.

Warnings

  • Safe use of guanidine hydrochloride in pregnancy has not been established. Therefore, the benefits of therapy must be weighed against the potential hazards. Because guanidine is excreted in milk, patients on this drug should discontinue breastfeeding.
  • Since there is inadequate experience in children who have received this drug, safety and efficacy in children have not been established.

Precautions

  • Baseline blood studies should be followed by frequent red and white blood cell and differential counts. The drug should be discontinued upon appearance of bone-marrow suppression. Concurrent therapy with other drugs that may cause bone-marrow suppression should be avoided.
  • Renal function may be affected in some patients receiving guanidine. Patients should therefore have regular urine examinations and serum creatinine determinations while taking this drug.
  • Physicians should be given adequate precautions pertaining to the gastrointestinal side effects and the possibility of induced behavior disorders.
  • Treatment should not be continued longer than necessary.

Adverse Reactions

Clinical Trials Experience

  • Gastrointestinal: dry mouth; gastric irritation; anorexia; nausea; diarrhea; abdominal cramping. Gastrointestinal side effects may preclude the use of guanidine as a desired form of therapy.

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Guanidine in the drug label.

Drug Interactions

There is limited information regarding Guanidine Drug Interactions in the drug label.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): There is no FDA guidance on usage of Guanidine in women who are pregnant.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Guanidine in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Guanidine during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Guanidine with respect to nursing mothers.

Pediatric Use

There is no FDA guidance on the use of Guanidine with respect to pediatric patients.

Geriatic Use

There is no FDA guidance on the use of Guanidine with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Guanidine with respect to specific gender populations.

Race

There is no FDA guidance on the use of Guanidine with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Guanidine in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Guanidine in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Guanidine in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Guanidine in patients who are immunocompromised.

Administration and Monitoring

Administration

  • Oral

Monitoring

There is limited information regarding Monitoring of Guanidine in the drug label.

IV Compatibility

There is limited information regarding IV Compatibility of Guanidine in the drug label.

Overdosage

  • Mild gastrointestinal disorders, such as anorexia, increased peristalsis, or diarrhea are early warnings that tolerance is being exceeded. These symptoms may be relieved by atropine, but nevertheless note should be taken of these symptoms and dosage reductions considered. Slight numbness or tingling of the lips and fingertips shortly after taking a dose of guanidine has been reported. This per se is not an indication to discontinue treatment and/or reduce dosage.
  • Atropine is more effective than calcium in relieving the G.I. symptoms, circulatory disturbances, and changes in blood sugar.

Pharmacology

Template:Chembox BeilsteinTemplate:Chembox ECNumberTemplate:Chembox E numberTemplate:Chembox GmelinTemplate:Chembox MeltingPtTemplate:Chembox LogPTemplate:Chembox ThermochemistryTemplate:Chembox PharmacologyTemplate:Chembox Lethal amounts (set)
Guanidine
Template:Chembox image sbs cell
Template:Chembox image sbs cell
Names
IUPAC name
Guanidine[1]
Identifiers
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
DrugBank
ECHA InfoCard Lua error in Module:Wikidata at line 879: attempt to index field 'wikibase' (a nil value). Lua error in Module:Wikidata at line 879: attempt to index field 'wikibase' (a nil value).
MeSH Guanidine
UNII
Properties
CH5N3
Molar mass 59.07 g·mol−1
Hazards
Related compounds
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
☑Y verify (what is ☑Y☒N ?)
Infobox references

Mechanism of Action

  • Guanidine apparently acts by enhancing the release of acetylcholine following a nerve impulse. It also appears to slow the rates of depolarization and repolarization of muscle cell membranes

Structure

  • Chemically, guanidine (aminomethanamidine) hydrochloride is a crystalline powder freely soluble in water and alcohol. The aqueous solution is neutral.

The structural formula is:

This image is provided by the National Library of Medicine.
  • Each tablet contains 125 mg of guanidine hydrochloride with no color additive in the base. It also contains the following inactive ingredients: colloidal silicon dioxide, magnesium stearate, mannitol, and microcrystalline cellulose.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Guanidine in the drug label.

Pharmacokinetics

There is limited information regarding Pharmacokinetics of Guanidine in the drug label.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Guanidine in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of Guanidine in the drug label.

How Supplied

  • Guanidine hydrochloride tablets: 125 mg, white, round tablet; impressed with the product identification number "KEY 74" on one side. Guanidine hydrochloride tablets are available in bottles of 100 (NDC 0085-0492-01).

Storage

  • Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F) [see USP Controlled Room Temperature].

Images

Drug Images

{{#ask: Page Name::Guanidine |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}

Package and Label Display Panel

{{#ask: Label Page::Guanidine |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}

Patient Counseling Information

There is limited information regarding Patient Counseling Information of Guanidine in the drug label.

Precautions with Alcohol

  • Alcohol-Guanidine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

Look-Alike Drug Names

There is limited information regarding Guanidine Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

  1. ↑ "Guanidine - Compound Summary". PubChem Compound. USA: National Center for Biotechnology Information. 16 September 2004. Identification. Retrieved 29 February 2012.
  2. ↑ http://chem.sis.nlm.nih.gov/chemidplus/rn/50-01-1


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{{#subobject: 

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