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{{Drugbox|
{{DrugProjectFormSinglePage
|IUPAC_name = 2-carbamoyloxyethyl-trimethyl-azanium
|authorTag={{KS}}
| CAS_number=51-83-2
|genericName=carbachol
| ATC_prefix=N07
|aOrAn=a
| ATC_suffix=AB01
|drugClass=cholinergic drug
| ATC_supplemental=
|indicationType=procedure
| PubChem=2551
|indication=[[glaucoma]], ocular [[hypertension]], [[miosis]] induction
| DrugBank=APRD00845
|adverseReactions=corneal clouding, bullous keratopathy, [[retinal detachment]], [[iritis|postoperative iritis]], [[flushing]], sweating, [[epigastric distress]], abdominal cramps, tightness in urinary bladder, [[headache]]
| C=6 | H=15 | N=2 | O=2 | charge=+
|blackBoxWarningTitle=<span style="color:#FF0000;">ConditionName: </span>
| molecular_weight = 147.196 g/mol
|blackBoxWarningBody=<i><span style="color:#FF0000;">ConditionName: </span></i>
| bioavailability= ?
 
* Content
 
<!--Adult Indications and Dosage-->
 
<!--FDA-Labeled Indications and Dosage (Adult)-->
|fdaLIADAdult===Indications==
* Intraocular use for obtaining miosis during surgery. In addition, MIOSTAT (carbachol intraocular solution, USP) reduces the intensity of intraocular pressure elevation in the first 24 hours after cataract surgery.
 
==Dosage==
 
* Glaucoma: 2 drops 0.75-3% solution in affected eye(s) up to 3 times daily
* Miosis induction - Surgical procedure: 0.5 mL of 0.01% solution INTRAOCULARLY, instilled into anterior chamber of the eye before or after securing sutures
|offLabelAdultGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.
|offLabelAdultNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.
|fdaLIADPed=There is limited information regarding <i>FDA-Labeled Use</i> of {{PAGENAME}} in pediatric patients.
|offLabelPedGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.
|offLabelPedNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.
|contraindications=* Should not be used in those persons showing hypersensitivity to any of the components of this preparation.
|warnings=* For single-dose intraocular use only. Discard unused portion. Intraocular carbachol 0.01% should be used with caution in patients with acute [[cardiac failure]], [[bronchial asthma]], [[peptic ulcer]], [[hyperthyroidism]], G.I. spasm, urinary tract obstruction and [[Parkinson's disease]].
|clinicalTrials='''Ocular''': Corneal clouding, persistent bullous keratopathy, retinal detachment and postoperative [[iritis]] following cataract extraction have been reported.
 
'''Systemic''': Side effects such as flushing, sweating, epigastric distress, abdominal cramps, tightness in urinary bladder, and [[headache]] have been reported with topical or systemic application of carbachol.
|postmarketing=There is limited information regarding <i>Postmarketing Experience</i> of {{PAGENAME}} in the drug label.
|useInPregnancyFDA='''Pregnancy'''
Category C. There are no adequate and well-controlled studies in pregnant women. MIOSTAT® (carbachol intraocular solution, USP) should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
|useInPregnancyAUS=* '''Australian Drug Evaluation Committee (ADEC) Pregnancy Category'''
 
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=* It is not known if this medication is excreted in breast milk. Exercise caution when administering to a nursing woman.
|useInPed=* Safety and efficacy in pediatric patients have not been established.
|useInGeri=* No overall differences in safety or effectiveness have been observed between elderly and younger 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=* Aseptically remove the sterile vial from the blister package by peeling the backing paper and dropping the vial onto a sterile tray. Withdraw the contents into a dry sterile syringe, and replace the needle with an atraumatic cannula prior to intraocular instillation. No more than one-half milliliter should be gently instilled into the anterior chamber for the production of satisfactory miosis. It may be instilled before or after securing sutures. Miosis is usually maximal within two to five minutes after application.
|monitoring=There is limited information regarding <i>Monitoring</i> of {{PAGENAME}} in the drug label.
|IVCompat=There is limited information regarding <i>IV Compatibility</i> of {{PAGENAME}} in the drug label.
|drugBox={{Drugbox2
| Watchedfields = changed
| verifiedrevid = 457629915
| IUPAC_name = 2-[(Aminocarbonyl)oxy]-''N'',''N'',''N''-trimethylethanaminium chloride
| image = Carbachol chloride.png
 
<!--Clinical data-->
| tradename = Miostat
| Drugs.com = {{drugs.com|monograph|carbachol}}
| pregnancy_US = C
| legal_status = Rx-only
| routes_of_administration = Oral-Tablet, {{nowrap|Injectable-solution}}, {{nowrap|Topical-eye drops}}
 
<!--Pharmacokinetic data-->
| bioavailability = low
| metabolism = ?
| metabolism = ?
| elimination_half-life= ?
| elimination_half-life = ?
| excretion = ?
| excretion = ?
| pregnancy_US = C
 
| legal_status = ?
<!--Identifiers-->
| routes_of_administration= Tablet, liquid
| CASNo_Ref = {{cascite|correct|CAS}}
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 51-83-2
| ATC_prefix = N07
| ATC_suffix = AB01
| ATC_supplemental = {{ATC|S01|EB02}} {{ATCvet|A03|AB92}}
| PubChem = 5831
| IUPHAR_ligand = 298
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB00411
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 5626
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 8Y164V895Y
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D00524
| ChEBI_Ref = {{ebicite|correct|EBI}}
| ChEBI = 3385
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 14
 
<!--Chemical data-->
| C=6 | H=15 | N=2 | O=2 | Cl = 1
| molecular_weight = 182.696 g/mol
| smiles = [Cl-].O=C(OCC[N+](C)(C)C)N
| InChI = 1/C6H14N2O2.ClH/c1-8(2,3)4-5-10-6(7)9;/h4-5H2,1-3H3,(H-,7,9);1H
| InChIKey = AIXAANGOTKPUOY-UHFFFAOYAV
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 1S/C6H14N2O2.ClH/c1-8(2,3)4-5-10-6(7)9;/h4-5H2,1-3H3,(H-,7,9);1H
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = AIXAANGOTKPUOY-UHFFFAOYSA-N
}}
}}
{{SI}}
|mechAction=* The exact mechanism by which carbachol lowers [[intraocular pressure]] is not precisely known.
|structure=* MIOSTAT® (carbachol intraocular solution, USP) is a sterile balanced salt solution of carbachol for intraocular injection. The active ingredient is represented by the chemical structure:


[[File:carbachol structure.png|thumb|none|600px|This image is provided by the National Library of Medicine.]]


==Overview==
Established name:
'''Carbachol''' (''Kar-ba-kol'', also known as carbamylcholine (marketed under the brand names '''Carbastat''', '''Carboptic''', '''Isopto Carbachol''', '''Miostat'''), is classified as a [[cholinergic]]. Thus, it acts as an AChR [[agonist]]. It is primarily used for various ophthalmic purposes, such as for treating [[glaucoma]], or for use during ophthalmic surgery. It is generally administered as an [[ophthalmic]] solution (i.e. eyedrop).


==Chemistry and pharmacology==
Carbachol
Carbachol is a [[choline]] [[ester]] and a positively charged quaternary ammonium compound. It is not well absorbed in the [[gastro-intestinal tract]] and does not cross the [[blood-brain barrier]]. It is usually administered topical ocular or through intraocular injection. Carbachol is not easily metabolized by [[cholinesterase]], it has a two to 5 minute onset of action and its duration of action is 4 to 8 hours with topical administration and 24 hours for intraocular administration. Since carbachol is poorly absorbed through topical administration, [[benzalkonium chloride]] is mixed in to promote absorption.


Carbachol is a [[parasympathomimetic]] that [[agonist|stimulates]] both [[muscarinic acetylcholine receptor|muscarinic]] and [[nicotinic acetylcholine receptor|nicotinic]] receptors. In topical ocular and intraocular administration its principal effects are [[miosis]] and increased [[aqueous humour]] outflow.
Chemical name:


In the cat and rat, carbachol is well-known for its ability to induce [[Rapid eye movement sleep|rapid eye movement]] (REM) sleep when microinjected into the [[pons|pontine reticular]] formation. Carbachol elicits this REM sleep-like state via activation of postsynaptic muscarinic [[acetylcholine|cholinergic]] receptors (mAChRs).
Ethanaminium, 2-[(aminocarbonyl)oxy]-N,N,Ntrimethyl-, chloride.


==Indications==
Molecular Formula: C6H15CIN2O2
Carbachol is primarily used in the treatment of [[glaucoma]], but it is also used during ophthalmic surgery. Carbachol eyedrops are used to decrease the pressure in the eye for people with glaucoma. It is sometimes used to constrict the pupils during [[cataract]] surgery.


Topical occular administration is used to decrease intraocular pressure in people with primary open-angle [[glaucoma]]. Intraocular administration is used to produce miosis after lens implantation during cataract surgery. Carbachol can also be used to stimulate bladder emptying if the normal emptying mechanism is not working properly.
Molecular Weight: 182.65


In most countries carbachol is only available by prescription.
Each mL contains: Active: carbachol 0.01%.


==Contraindications==
Inactives: sodium chloride 0.64%, potassium chloride 0.075%, calcium chloride dehydrate 0.048%, magnesium chloride hexahydrate 0.03%, sodium acetate trihydrate 0.39%, sodium citrate dihydrate 0.17%, sodium hydroxide and/or hydrochloric acid (to adjust pH) and Water for Injection. pH range is 6.5-7.5.
Use of carbachol, as well as all other muscarinic receptor agonists, is contraindicated in patients with asthma, coronary insufficiency, gastroduodenal ulcers, and incontinence. The [[parasympathomimetic]] action of this drug will exacerbate the symptoms of these disorders.
|PD=There is limited information regarding <i>Pharmacodynamics</i> of {{PAGENAME}} in the drug label.
|PK=There is limited information regarding <i>Pharmacokinetics</i> of {{PAGENAME}} in the drug label.
|nonClinToxic='''Carcinogenesis'''


==Overdose==
* Studies in animals to evaluate the carcinogenic potential have not been conducted.
The effects of a systemic overdose on a cholinergic will probably be similar to the effects of a [[nerve agent]], but weaker. However, when administered ocularly there is probably little risk of such effects.
|clinicalStudies=There is limited information regarding <i>Clinical Studies</i> of {{PAGENAME}} in the drug label.
|howSupplied=* In a 2.0 mL glass vial with a 1.5 mL fill, grey butyl stopper and aluminum seal packaged twelve to a carton.
 
:*NDC 0065-0023-15
|storage=* STORAGE: Store at 15° - 30°C (59° - 86°F).
|packLabel=<!--Patient Counseling Information-->
|fdaPatientInfo=There is limited information regarding <i>Patient Counseling Information</i> of {{PAGENAME}} in the drug label.
|alcohol=* Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
|brandNames=MIOSTAT
|drugShortage=
}}
{{PillImage
|fileName=No image.jpg
}}
{{LabelImage
|fileName=Miostat.jpg
}}
{{LabelImage
|fileName=Miostat ingredients and appearance.png
}}
<!--Pill Image-->


==External links==
* [http://www.rxlist.com/cgi/generic2/carbachol.htm RxList.com - Carbachol]




==References==
<!--Label Display Image-->
* Brenner, G. M. (2000). ''Pharmacology.'' Philadelphia, PA: W.B. Saunders Company. ISBN 0-7216-7757-6
* Canadian Pharmacists Association (2000). ''Compendium of pharmaceuticals and specialties'' (25th ed.). Toronto, ON: Webcom. ISBN 0-919115-76-4
* Carbachol (1998). ''MedlinePlus''. Retrieved June 27, 2004, from http://www.nlm.nih.gov/medlineplus/druginfo/uspdi/202110.html
* Carbachol (2003). ''RxList''. Retrieved June 27, 2004, from http://www.rxlist.com/cgi/generic2/carbachol.htm
* National Institute for Occupational Safety and Health. (2002). Choline, chloride, carbamate. In ''The registry of toxic effects of chemical substances.'' Retrieved June 27, 2004, from http://www.cdc.gov/niosh/rtecs/gad59f8.html
* Carbachol Chloride (2004). ''Hazardous Substances Data Bank''. Retrieved July 16, 2004, from http://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?hsdbb.htm (search carbachol).
{{Parasympathomimetics}}
{{Antiglaucoma preparations and miotics}}


[[Category:Quaternary ammonium compounds]]
 
 
 
 
<!--Category-->
[[Category:Choline esters]]
[[Category:Choline esters]]
[[Category:Carbamates]]
[[Category:Carbamates]]


[[de:Carbachol]]
[[Category:Drug]]
[[ja:カルバコール]]
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Latest revision as of 18:37, 18 August 2015

Carbachol
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: Kiran Singh, M.D. [2]

Disclaimer

WikiDoc MAKES NO GUARANTEE OF VALIDITY. WikiDoc is not a professional health care provider, nor is it a suitable replacement for a licensed healthcare provider. WikiDoc is intended to be an educational tool, not a tool for any form of healthcare delivery. The educational content on WikiDoc drug pages is based upon the FDA package insert, National Library of Medicine content and practice guidelines / consensus statements. WikiDoc does not promote the administration of any medication or device that is not consistent with its labeling. Please read our full disclaimer here.

Overview

Carbachol is a cholinergic drug that is FDA approved for the procedure of glaucoma, ocular hypertension, miosis induction. Common adverse reactions include corneal clouding, bullous keratopathy, retinal detachment, postoperative iritis, flushing, sweating, epigastric distress, abdominal cramps, tightness in urinary bladder, headache.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Indications

  • Intraocular use for obtaining miosis during surgery. In addition, MIOSTAT (carbachol intraocular solution, USP) reduces the intensity of intraocular pressure elevation in the first 24 hours after cataract surgery.

Dosage

  • Glaucoma: 2 drops 0.75-3% solution in affected eye(s) up to 3 times daily
  • Miosis induction - Surgical procedure: 0.5 mL of 0.01% solution INTRAOCULARLY, instilled into anterior chamber of the eye before or after securing sutures

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

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

Non–Guideline-Supported Use

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

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

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

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

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

Non–Guideline-Supported Use

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

Contraindications

  • Should not be used in those persons showing hypersensitivity to any of the components of this preparation.

Warnings

Adverse Reactions

Clinical Trials Experience

Ocular: Corneal clouding, persistent bullous keratopathy, retinal detachment and postoperative iritis following cataract extraction have been reported.

Systemic: Side effects such as flushing, sweating, epigastric distress, abdominal cramps, tightness in urinary bladder, and headache have been reported with topical or systemic application of carbachol.

Postmarketing Experience

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

Drug Interactions

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

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. MIOSTAT® (carbachol intraocular solution, USP) should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Pregnancy Category (AUS):

  • Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Carbachol in women who are pregnant.

Labor and Delivery

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

Nursing Mothers

  • It is not known if this medication is excreted in breast milk. Exercise caution when administering to a nursing woman.

Pediatric Use

  • Safety and efficacy in pediatric patients have not been established.

Geriatic Use

  • No overall differences in safety or effectiveness have been observed between elderly and younger patients.

Gender

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

Race

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

Renal Impairment

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

Hepatic Impairment

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

Females of Reproductive Potential and Males

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

Immunocompromised Patients

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

Administration and Monitoring

Administration

  • Aseptically remove the sterile vial from the blister package by peeling the backing paper and dropping the vial onto a sterile tray. Withdraw the contents into a dry sterile syringe, and replace the needle with an atraumatic cannula prior to intraocular instillation. No more than one-half milliliter should be gently instilled into the anterior chamber for the production of satisfactory miosis. It may be instilled before or after securing sutures. Miosis is usually maximal within two to five minutes after application.

Monitoring

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

IV Compatibility

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

Overdosage

There is limited information regarding Carbachol overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.

Pharmacology

Template:Px
Carbachol
Systematic (IUPAC) name
2-[(Aminocarbonyl)oxy]-N,N,N-trimethylethanaminium chloride
Identifiers
CAS number 51-83-2
ATC code N07AB01 S01EB02 (WHO) Template:ATCvet
PubChem 5831
DrugBank DB00411
Chemical data
Formula Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox 
Mol. mass 182.696 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability low
Metabolism ?
Half life ?
Excretion ?
Therapeutic considerations
Pregnancy cat.

C(US)

Legal status

Template:Unicode Prescription only

Routes Oral-Tablet, Injectable-solution, Topical-eye drops

Mechanism of Action

Structure

  • MIOSTAT® (carbachol intraocular solution, USP) is a sterile balanced salt solution of carbachol for intraocular injection. The active ingredient is represented by the chemical structure:
This image is provided by the National Library of Medicine.

Established name:

Carbachol

Chemical name:

Ethanaminium, 2-[(aminocarbonyl)oxy]-N,N,Ntrimethyl-, chloride.

Molecular Formula: C6H15CIN2O2

Molecular Weight: 182.65

Each mL contains: Active: carbachol 0.01%.

Inactives: sodium chloride 0.64%, potassium chloride 0.075%, calcium chloride dehydrate 0.048%, magnesium chloride hexahydrate 0.03%, sodium acetate trihydrate 0.39%, sodium citrate dihydrate 0.17%, sodium hydroxide and/or hydrochloric acid (to adjust pH) and Water for Injection. pH range is 6.5-7.5.

Pharmacodynamics

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

Pharmacokinetics

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

Nonclinical Toxicology

Carcinogenesis

  • Studies in animals to evaluate the carcinogenic potential have not been conducted.

Clinical Studies

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

How Supplied

  • In a 2.0 mL glass vial with a 1.5 mL fill, grey butyl stopper and aluminum seal packaged twelve to a carton.
  • NDC 0065-0023-15

Storage

  • STORAGE: Store at 15° - 30°C (59° - 86°F).

Images

Drug Images

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

Patient Counseling Information

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

Precautions with Alcohol

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

Brand Names

MIOSTAT

Look-Alike Drug Names

There is limited information regarding Carbachol 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.

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