Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C10H14N2O4 |
| Molecular Weight | 226.2292 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@@](CC1=CC(O)=C(O)C=C1)(NN)C(O)=O
InChI
InChIKey=TZFNLOMSOLWIDK-JTQLQIEISA-N
InChI=1S/C10H14N2O4/c1-10(12-11,9(15)16)5-6-2-3-7(13)8(14)4-6/h2-4,12-14H,5,11H2,1H3,(H,15,16)/t10-/m0/s1
Carbidopa is a competitive inhibitor of aromatic L-amino acid decarboxylase that does not cross the blood-brain barrier, is routinely administered with levodopa (LD) for the treatment of the symptoms of idiopathic Parkinson’s disease (paralysis agitans), postencephalitic parkinsonism, and symptomatic parkinsonism, which may follow injury to the nervous system by carbon monoxide intoxication and/or manganese intoxication. Current evidence indicates that symptoms of Parkinson’s disease are related to depletion of dopamine in the corpus striatum. Administration of dopamine is ineffective in the treatment of Parkinson’s disease apparently because it does not cross the blood-brain barrier. However, levodopa, the metabolic precursor of dopamine, does cross the blood- brain barrier, and presumably is converted to dopamine in the brain. When levodopa is administered orally it is rapidly decarboxylated to dopamine in extracerebral tissues so that only a small portion of a given dose is transported unchanged to the central nervous system. For this reason, large doses of levodopa are required for adequate therapeutic effect and these may often be accompanied by nausea and other adverse reactions, some of which are attributable to dopamine formed in extracerebral tissues. Carbidopa inhibits decarboxylation of peripheral levodopa. Carbidopa has not been demonstrated to have any overt pharmacodynamic actions in the recommended doses.
CNS Activity
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL1843 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Palliative | LODOSYN Approved UseLODOSYN is indicated for use with carbidopa-levodopa or with levodopa in the treatment of the symptoms of idiopathic Parkinson’s disease (paralysis agitans), postencephalitic parkinsonism, and symptomatic parkinsonism, which may follow injury to the nervous system by carbon monoxide intoxication and/or manganese intoxication. LODOSYN is for use with carbidopa-levodopa in patients for whom the dosage of carbidopa-levodopa provides less than adequate daily dosage (usually 70 mg daily) of carbidopa. LODOSYN is for use with levodopa in the occasional patient whose dosage requirement of carbidopa and levodopa necessitates separate titration of each medication. LODOSYN is used with carbidopa-levodopa or with levodopa to permit the administration of lower doses of levodopa with reduced nausea and vomiting, more rapid dosage titration, and with a somewhat smoother response. However, patients with markedly irregular (“on-off”) responses to levodopa have not been shown to benefit from the addition of carbidopa. Since carbidopa prevents the reversal of levodopa effects caused by pyridoxine, supplemental pyridoxine (vitamin B6), can be given to patients when they are receiving carbidopa and levodopa concomitantly or as carbidopa-levodopa. Launch Date2.30774407E11 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
108.57 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/30295551 |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: LEVODOPA |
CARBIDOPA plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
559.92 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/30295551 |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: LEVODOPA |
CARBIDOPA plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2.09 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/30295551 |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: LEVODOPA |
CARBIDOPA plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
64% |
CARBIDOPA plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Centrally mediated increased reflex vagal bradycardia after L-dopa in monoamine oxidase-inhibited anesthetized dogs. | 1976 Feb |
|
| Switching from pergolide to pramipexole in patients with Parkinson's disease. | 2001 |
|
| L-dopa induces dyskinesia in normal monkeys: behavioural and pharmacokinetic observations. | 2001 Aug |
|
| Duodenal levodopa infusion in Parkinson's disease--long-term experience. | 2001 Dec |
|
| Periodic limb movement disorder : a clinical and polysomnographic study. | 2001 Dec |
|
| Amantadine for dyskinesia in patients affected by severe Parkinson's disease. | 2001 Feb |
|
| Molecular mechanisms controlling the rate and specificity of catechol O-methylation by human soluble catechol O-methyltransferase. | 2001 Feb |
|
| Aldrin-induced locomotor activity: possible involvement of the central GABAergic-cholinergic-dopaminergic interaction. | 2001 Jan-Feb |
|
| Blood-brain barrier and neuronal membrane transport of 6-[18F]fluoro-L-DOPA. | 2001 Nov 15 |
|
| Post-stroke violent adventitial movement responsive to levo-dopa/carbi-dopa therapy. | 2001 Oct |
|
| Dopaminergic therapy with carbidopa L-dopa for left neglect after stroke: a case series. | 2001 Sep |
|
| Stereoselective effect of (R)- and (S)-1-methyl-1,2,3,4-tetrahydroisoquinolines on a mouse model of Parkinson's disease. | 2001 Sep 1 |
|
| Atypical presentation of dopa-responsive dystonia: generalized hypotonia and proximal weakness. | 2001 Sep 25 |
|
| Restless legs syndrome in the older adult: diagnosis and management. | 2002 |
|
| [Serotonin syndrome: report of a fatal case and review of the literature]. | 2002 Apr |
|
| Transport of amino acid-related compounds mediated by L-type amino acid transporter 1 (LAT1): insights into the mechanisms of substrate recognition. | 2002 Apr |
|
| Selegiline: a second look. Six years later: too risky in Parkinson's disease. | 2002 Aug |
|
| Levodopa-carbidopa with occlusion in older children with amblyopia. | 2002 Dec |
|
| Screening for tetrahydrobiopterin deficiency among hyperphenylalaninemia patients in Southern China. | 2002 Feb |
|
| [Benefit of L-DOPA-without-DCI (decarboxylase inhibitor) therapy on wearing-off phenomenon in advanced stages of Parkinson's disease patients]. | 2002 Feb |
|
| Parkinson disease neuropathology: later-developing dementia and loss of the levodopa response. | 2002 Jan |
|
| [Rhabdomyolysis as a complication of Parkinson's disease]. | 2002 Jan-Feb |
|
| Nitecapone and selegiline as effective adjuncts to L-DOPA in reserpine-induced catatonia in mice. | 2002 Jan-Feb |
|
| The SSRI, citalopram, improves bradykinesia in patients with Parkinson's disease treated with L-dopa. | 2002 Jan-Feb |
|
| Levodopa-responsive rubral (Holmes') tremor. | 2002 Jul |
|
| [Atypical phenylketonuria treatment effectiveness]. | 2002 Jul-Sep |
|
| Gateways to Clinical Trials. June 2002. | 2002 Jun |
|
| In vivo metabolism and partitioning of 6-[18F]fluoro-L-meta-tyrosine in whole blood: a unified compartment model. | 2002 Jun 7 |
|
| Parkinsonism associated with interferon alpha therapy for chronic myelogenous leukemia. | 2002 Mar |
|
| Bruxism as presenting feature of Parkinson's disease. | 2002 Mar |
|
| Entacapone in restless legs syndrome. | 2002 Mar |
|
| Oral solution of levodopa ethylester for treatment of response fluctuations in patients with advanced Parkinson's disease. | 2002 Mar |
|
| Influence of layer position on in vitro and in vivo release of levodopa methyl ester and carbidopa from three-layer matrix tablets. | 2002 Mar |
|
| [Hallucinations caused by paroxetine taken together with a levodopa-carbidopa preparation]. | 2002 Mar 23 |
|
| Dopaminergic transmission in the rat striatum in vivo in conditions of pharmacological modulation. | 2002 Mar-Apr |
|
| Gender and pramipexole effects on levodopa pharmacokinetics and pharmacodynamics. | 2002 May 14 |
|
| Role of sphingosine synthesis inhibition in transcutaneous delivery of levodopa. | 2002 May 15 |
|
| Clozapine withdrawal symptoms in a Parkinson's disease patient. | 2002 Nov |
|
| Levodopa but not ropinirole induces an internalization of D1 dopamine receptors in parkinsonian rats. | 2002 Nov |
|
| The role of PET in localization of neuroendocrine and adrenocortical tumors. | 2002 Sep |
|
| Simultaneous determination of dopa and carbidopa enantiomers by capillary zone electrophoresis. | 2002 Sep |
|
| Quantitative description of loss of clinical benefit following withdrawal of levodopa-carbidopa and bromocriptine in early Parkinson's disease. | 2002 Sep |
|
| Repeated administration of piribedil induces less dyskinesia than L-dopa in MPTP-treated common marmosets: a behavioural and biochemical investigation. | 2002 Sep |
|
| Leg muscle strength is reduced in Parkinson's disease and relates to the ability to rise from a chair. | 2003 Feb |
|
| Binding site of salsolinol: its properties in different regions of the brain and the pituitary gland of the rat. | 2003 Jan |
|
| Neonatal dopa-responsive extrapyramidal syndrome in twins with recessive GTPCH deficiency. | 2003 Jan 28 |
|
| Quercetin potentiates L-Dopa reversal of drug-induced catalepsy in rats: possible COMT/MAO inhibition. | 2003 Jun |
|
| Optimizing levodopa pharmacokinetics: intestinal infusion versus oral sustained-release tablets. | 2003 May-Jun |
Sample Use Guides
Whether given with carbidopa-levodopa or with levodopa, the optimal daily dose of LODOSYN (CARBIDOPA tablets) must be determined by careful titration. Most patients respond to a 1:10 proportion of carbidopa and levodopa, provided the daily dosage of carbidopa is 70 mg or more a day. The maximum daily dosage of carbidopa should not exceed 200 mg, since clinical experience with larger dosages is limited. If the patient is taking carbidopa-levodopa, the amount of carbidopa in carbidopa-levodopa should be considered when calculating the total amount of LODOSYN to be administered each day.
Route of Administration:
Oral
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C38149
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NCI_THESAURUS |
C66884
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1545982
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DB00190
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28860-95-9
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KR87B45RGH
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34359
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249-271-9
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3258
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SUB06126MIG
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C61803
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SUB22639
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DTXSID4022735
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M3068
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KR87B45RGH
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ACTIVE MOIETY
METABOLITE (PARENT)
METABOLITE (PARENT)
PARENT (METABOLITE)
SALT/SOLVATE (PARENT)
