View source for Guanidine

{{DrugProjectFormSinglePage
|authorTag={{AV}}<!--Overview-->
|genericName=guanidine hydrochloride
|aOrAn=a
|drugClass=[[cholinesterase inhibitor]]
|indicationType=treatment
|indication=muscle weakness and [[easy fatigability]] associated with the [[Eaton-Lambert syndrome|myasthenic syndrome of Eaton-Lambert]]
|adverseReactions=<!--Black Box Warning-->
|blackBoxWarningTitle=Title
|blackBoxWarningBody=<i><span style="color:#FF0000;">ConditionName: </span></i>

* Content

<!--Adult Indications and Dosage-->

<!--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.
=====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 (Adult)-->
|offLabelAdultGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.

<!--Non–Guideline-Supported Use (Adult)-->
|offLabelAdultNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.

<!--Pediatric Indications and Dosage-->

<!--FDA-Labeled Indications and Dosage (Pediatric)-->
|fdaLIADPed=There is limited information regarding <i>FDA-Labeled Use</i> of {{PAGENAME}} in pediatric patients.

<!--Off-Label Use and Dosage (Pediatric)-->

<!--Guideline-Supported Use (Pediatric)-->
|offLabelPedGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.

<!--Non–Guideline-Supported Use (Pediatric)-->
|offLabelPedNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.

<!--Contraindications-->
|contraindications=*Guanidine is contraindicated in individuals with a history of intolerance or [[allergy]] to this drug.

<!--Warnings-->
|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]].

*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-->
|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]].

*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.

*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]].

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

*Cardiac: [[palpitation]], [[tachycardia]], [[atrial fibrillation]], [[hypotension]].
<!--Postmarketing Experience-->
|postmarketing=There is limited information regarding <i>Postmarketing Experience</i> of {{PAGENAME}} in the drug label.



<!--Drug Interactions-->
|drugInteractions=<!--Use in Specific Populations-->
|useInPregnancyAUS=

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of {{PAGENAME}} in women who are pregnant.
|useInLaborDelivery=There is no FDA guidance on use of {{PAGENAME}} during labor and delivery.
|useInNursing=There is no FDA guidance on the use of {{PAGENAME}} with respect to nursing mothers.
|useInPed=There is no FDA guidance on the use of {{PAGENAME}} with respect to pediatric patients.
|useInGeri=There is no FDA guidance on the use of {{PAGENAME}} with respect to geriatric patients.
|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.
|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]].
|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]].

<!--Administration and Monitoring-->
|administration=* Oral

|monitoring=There is limited information regarding <i>Monitoring</i> of {{PAGENAME}} in the drug label.

<!--IV Compatibility-->
|IVCompat=There is limited information regarding <i>IV Compatibility</i> of {{PAGENAME}} in the drug label.

<!--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.

*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.
<!--Pharmacology-->

<!--Drug box 2-->
|drugBox={{Chembox2
| Watchedfields = changed
| verifiedrevid = 443849964
| ImageFileL1 = Guanidin.png
| ImageFileL1_Ref = {{chemboximage|correct|??}}
| ImageNameL1 = Skeletal formula of guanidine
| ImageFileR1 = Guanidine-2D.png
| ImageFileR1_Ref = {{chemboximage|correct|??}}
| ImageNameR1 = Skeletal formula of guanidine with the implicit carbon shown, and all explicit hydrogens added.
| ImageFileL2 = Guanidine-3D-balls.png
| ImageFileL2_Ref = {{chemboximage|correct|??}}
| ImageNameL2 = Ball and stick model of guanidine
| ImageFileR2 = Guanidine-3D-vdW.png
| ImageFileR2_Ref = {{chemboximage|correct|??}}
| ImageNameR2 = Spacefill model of guanidine
| IUPACName = Guanidine<ref>{{Cite web|title=Guanidine - Compound Summary|url=http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3520&loc=ec_rcs|work=PubChem Compound|publisher=National Center for Biotechnology Information|accessdate=29 February 2012|location=USA|date=16 September 2004|at=Identification}}</ref>
| Section1 = {{Chembox Identifiers
|  CASNo = 113-00-8
|  CASNo_Ref = {{cascite|correct|CAS}}
|  PubChem = 3520
|  PubChem_Ref = {{Pubchemcite|correct|Pubchem}}
|  ChemSpiderID = 3400
|  ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
|  UNII = JU58VJ6Y3B
|  UNII_Ref = {{fdacite|correct|FDA}}
|  EINECS = 204-021-8
|  DrugBank = DB00536
|  DrugBank_Ref = {{drugbankcite|correct|drugbank}}
|  MeSHName = Guanidine
|  ChEBI = 42820
|  ChEBI_Ref = {{ebicite|correct|EBI}}
|  ChEMBL = 821
|  ChEMBL_Ref = {{ebicite|correct|EBI}}
|  Beilstein = 506044
|  Gmelin = 100679
|  SMILES = [nH]:c(:[nH2]):[nH2]
|  SMILES1 = NC(N)=N
|  StdInChI = 1S/CH5N3/c2-1(3)4/h(H5,2,3,4)
|  StdInChI_Ref = {{stdinchicite|correct|chemspider}}
|  StdInChIKey = ZRALSGWEFCBTJO-UHFFFAOYSA-N
|  StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
}}
| Section2 = {{Chembox Properties
|  C = 1
|  H = 5
|  N = 3
|  MeltingPtC = 50
|  LogP = −1.251
}}
| Section3 = {{Chembox Thermochemistry
|  DeltaHf = −57–−55 kJ mol<sup>−1</sup>
|  DeltaHc = −1.0511–−1.0531 MJ mol<sup>−1</sup>
}}
| Section4 = {{Chembox Pharmacology
|  HalfLife = 7–8 hours
}}
| Section5 = {{Chembox Hazards
|  LD50 = 475 mg/kg (oral, rat)<ref>http://chem.sis.nlm.nih.gov/chemidplus/rn/50-01-1</ref>
}}
| Section6 = {{Chembox Related
|  OtherCpds = {{Unbulleted list|[[Urea]]|[[Biguanide]]}}
}}
}}

<!--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

<!--Structure-->
|structure=*Chemically, guanidine (aminomethanamidine) hydrochloride is a crystalline powder freely soluble in water and alcohol. The aqueous solution is neutral.

The structural formula is: 

: [[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]].

<!--Pharmacodynamics-->
|PD=There is limited information regarding <i>Pharmacodynamics</i> of {{PAGENAME}} in the drug label.

<!--Pharmacokinetics-->
|PK=There is limited information regarding <i>Pharmacokinetics</i> of {{PAGENAME}} in the drug label.

<!--Nonclinical Toxicology-->
|nonClinToxic=There is limited information regarding <i>Nonclinical Toxicology</i> of {{PAGENAME}} in the drug label.

<!--Clinical Studies-->
|clinicalStudies=There is limited information regarding <i>Clinical Studies</i> of {{PAGENAME}} in the drug label.

<!--How Supplied-->
|howSupplied=*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).


<!--Patient Counseling Information-->
|storage=*Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F) [see USP Controlled Room Temperature]. 

|fdaPatientInfo=There is limited information regarding <i>Patient Counseling Information</i> of {{PAGENAME}} in the drug label.

<!--Precautions with Alcohol-->
|alcohol=* Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

<!--Brand Names-->
|brandNames=*

<!--Look-Alike Drug Names-->
|lookAlike=<!--Drug Shortage Status-->
|drugShortage=
}}
<!--Pill Image-->

<!--Label Display Image-->

{{LabelImage
|fileName={{PAGENAME}}04.png|This image is provided by the National Library of Medicine.
}}

{{LabelImage
|fileName={{PAGENAME}}05.png|This image is provided by the National Library of Medicine.
}}

<!--Category-->

[[Category:Drug]]