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Carbidopa: Drug information

Carbidopa: Drug information
(For additional information see "Carbidopa: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Lodosyn
Pharmacologic Category
  • Anti-Parkinson Agent, Decarboxylase Inhibitor
Dosing: Adult

Parkinsonism:

Note: For patients receiving carbidopa/levodopa therapy, a carbidopa dose ≥75 mg/day may be necessary to decrease the risk of adverse effects from peripheral dopamine (Hoehn 1980; Kaakkola 1985).

Carbidopa augmentation in patients receiving carbidopa-levodopa:

Patients receiving carbidopa/levodopa 10/100: Oral: 25 mg daily with first daily dose of carbidopa/levodopa; if necessary, 12.5 to 25 mg may be given with each subsequent dose of carbidopa/levodopa; maximum: 200 mg/day (including from carbidopa/levodopa)

Patients receiving carbidopa/levodopa 25/250 or carbidopa/levodopa 25/100: Oral: 25 mg with any dose of carbidopa/levodopa throughout the day; maximum: 200 mg/day (including from carbidopa/levodopa)

Discontinuation of therapy: Discontinuation of carbidopa/levodopa therapy may result in neuroleptic malignant-like syndrome (Grimes 2019). Avoid sudden discontinuation or rapid dose reduction; some experts recommend a gradual taper over several weeks or more (Oliver 2021).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Older Adult

Refer to adult dosing.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Lodosyn: 25 mg [scored; contains fd&c yellow #6 (sunset yellow)]

Generic: 25 mg

Generic Equivalent Available: US

Yes

Administration: Adult

Administer with meals to decrease GI upset.

Use: Labeled Indications

Parkinsonism: Given with carbidopa/levodopa in the treatment of idiopathic Parkinson disease, postencephalitic parkinsonism, and symptomatic parkinsonism, which may follow injury to the nervous system by carbon monoxide and/or manganese intoxication.

Note: Administration of carbidopa allows use of a lower dosage of levodopa, more rapid titration, and a decrease in nausea and vomiting associated with levodopa. Use with carbidopa/levodopa in patients requiring additional carbidopa; carbidopa has no effect without levodopa.

Medication Safety Issues
High alert medication:

The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drugs that have a heightened risk of causing significant patient harm when used in error.

International issues:

Lodosyn [US] may be confused with Lidosen brand name for lidocaine [Italy]

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions are associated with concomitant administration with levodopa.

Cardiovascular: Cardiac arrhythmia, chest pain, edema, flushing, hypertension, hypotension, myocardial infarction, orthostatic hypotension, palpitation, phlebitis, syncope

Central nervous system: Abnormal dreams, abnormal gait, agitation, anxiety, ataxia, confusion, decreased mental acuity, delusions, dementia, depression (with or without suicidal tendencies), disorientation, dizziness, drowsiness, euphoria, extrapyramidal reaction, falling, fatigue, glossopyrosis, hallucination, headache, Horner's syndrome, impulse control disorder, insomnia, malaise, memory impairment, nervousness, neuroleptic malignant syndrome, nightmares, numbness, on-off phenomenon, paranoia, paresthesia, pathological gambling, peripheral neuropathy, psychosis, seizure (causal relationship not established), trismus

Dermatologic: Alopecia, bulla, diaphoresis, discoloration of sweat, skin rash

Endocrine & metabolic: Abnormal lactate dehydrogenase, glycosuria, hot flash, hyperglycemia, hypokalemia, increased libido (including hypersexuality), increased uric acid, weight changes

Gastrointestinal: Abdominal distress, abdominal pain, anorexia, bruxism, constipation, diarrhea, discoloration of saliva, duodenal ulcer, dysgeusia, dyspepsia, dysphagia, flatulence, gastrointestinal hemorrhage, heartburn, hiccups, nausea, sialorrhea, sore throat, vomiting, xerostomia

Genitourinary: Priapism, proteinuria, urinary frequency, urinary incontinence, urinary retention, urinary tract infection, urine discoloration

Hematologic & oncologic: Abnormal Coombs' test, agranulocytosis, anemia, decreased hematocrit, decreased hemoglobin, hemolytic anemia, leukopenia, malignant melanoma, thrombocytopenia

Hepatic: Abnormal alanine aminotransferase, abnormal alkaline phosphatase, abnormal aspartate transaminase, abnormal bilirubin levels, abnormal lactate dehydrogenase

Hypersensitivity: Angioedema, hypersensitivity reaction (bulla, IgA vasculitis, pruritus, urticaria)

Neuromuscular & skeletal: Back pain, dyskinesia (including choreiform, dystonic, and other involuntary movements), leg pain, muscle cramps, muscle twitching, shoulder pain, tremor, weakness

Ophthalmic: Blepharospasm, blurred vision, diplopia, mydriasis, oculogyric crisis (may be associated with acute dystonic reactions)

Renal: Increased blood urea nitrogen, increased serum creatinine

Respiratory: Cough, dyspnea, hoarseness, upper respiratory tract infection

Contraindications

Hypersensitivity to carbidopa or any component of the formulation; use of nonselective MAO inhibitor therapy with or within prior 14 days (however, may be administered concomitantly with the manufacturer's recommended dose of an MAO inhibitor with selectivity for MAO type B); narrow-angle glaucoma

Warnings/Precautions

Concerns related to adverse effects:

• Depression: Observe patients closely for development of depression with concomitant suicidal tendencies.

• Dyskinesias: May cause or exacerbate dyskinesias.

• Impulse control disorders: Antiparkinson therapy has been associated with compulsive behaviors and/or loss of impulse control, which has manifested as pathological gambling, libido increases (hypersexuality), urges to spend money uncontrollably, and/or binge eating. Dose reduction or discontinuation of therapy has been reported to reverse these behaviors in some, but not all cases.

• Psychotic effects: May cause hallucinations and psychotic-like behavior.

• Somnolence: Patients have reported falling asleep while engaging in activities of daily living; this has been reported to occur without significant warning signs. Monitor for daytime somnolence or preexisting sleep disorder; caution with concomitant sedating medication; consider discontinuing if significant daytime sleepiness or episodes of falling asleep occur. Patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery, driving).

Disease-related concerns:

• Psychotic disorders: Avoid use in patients with major psychotic disorder.

Metabolism/Transport Effects

None known.

Drug Interactions

Droxidopa: Carbidopa may diminish the therapeutic effect of Droxidopa. Carbidopa may decrease serum concentrations of the active metabolite(s) of Droxidopa. Carbidopa may increase the serum concentration of Droxidopa. Risk C: Monitor therapy

Reserpine: Carbidopa may enhance the hypotensive effect of Reserpine. Reserpine may diminish the therapeutic effect of Carbidopa. Risk X: Avoid combination

Spiramycin: May decrease the serum concentration of Carbidopa. And thus may decrease the effectiveness of levodopa. Risk C: Monitor therapy

Tetrabenazine: May diminish the therapeutic effect of Carbidopa. Risk X: Avoid combination

Pregnancy Considerations

Carbidopa can be detected in the umbilical cord but absorption in fetal tissue is minimal (Merchant 1995). The incidence of Parkinson disease in pregnancy is relatively rare and information related to the use of carbidopa in pregnant women is limited to use with other agents. Refer to the carbidopa and levodopa monograph for additional information.

Breastfeeding Considerations

It is not known if carbidopa is present in breast milk. Due to the potential for serious adverse reactions in the breastfeeding infant, the manufacturer recommends a decision be made whether to discontinue breastfeeding or to discontinue the drug, taking into account the importance of treatment to the mother.

Dietary Considerations

May be taken with meals to decrease GI upset.

Monitoring Parameters

CBC, LFTs, renal function; BP, mental status; signs and symptoms of neuroleptic malignant syndrome if abrupt discontinuation required (as with surgery); periodic intraocular pressure (in patients with wide-angle glaucoma).

Mechanism of Action

Carbidopa is a decarboxylase inhibitor with little or no pharmacological activity when given alone in usual doses. Unlike levodopa, carbidopa does not cross the blood-brain barrier and only inhibits the decarboxylation of peripheral levodopa to dopamine. Coadministration of carbidopa with levodopa allows for higher central nervous system concentrations of dopamine with lower doses of levodopa. Reduced peripheral formation of dopamine also reduces peripheral adverse reactions, including nausea and vomiting.

Pharmacokinetics

Distribution: Does not cross the blood-brain barrier

Pricing: US

Tablets (Carbidopa Oral)

25 mg (per each): $10.50 - $21.85

Tablets (Lodosyn Oral)

25 mg (per each): $35.50

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Brand Names: International
  • Duodopa (IE);
  • Nakom (PL);
  • Prikap (AR)


For country abbreviations used in Lexicomp (show table)

REFERENCES

  1. Grimes D, Fitzpatrick M, Gordon J, et al. Canadian guideline for Parkinson disease. CMAJ. 2019;191(36):E989-E1004. doi:10.1503/cmaj.181504 [PubMed 31501181]
  2. Hoehn MM. Increased dosage of carbidopa in patients with Parkinson's disease receiving low doses of levodopa. A pilot study. Arch Neurol. 1980;37(3):146-149. doi:10.1001/archneur.1980.00500520044006 [PubMed 7356419]
  3. Kaakkola S, Männistö PT, Nissinen E, Vuorela A, Mäntylä R. The effect of an increased ratio of carbidopa to levodopa on the pharmacokinetics of levodopa. Acta Neurol Scand. 1985;72(4):385-391. doi:10.1111/j.1600-0404.1985.tb00888.x [PubMed 4082903]
  4. Lodosyn (carbidopa) [prescribing information]. Bridgewater, NJ: Bausch Health US, LLC; July 2020.
  5. Merchant CA, Cohen G, Mytilineou C, et al, "Human Transplacental Transfer of Carbidopa/Levodopa," J Neural Transm Park Dis Dement Sect, 1995, 9(2-3):239-42. [PubMed 8527007]
  6. Oliver D, Veronese S. Palliative approach to Parkinson disease and parkinsonian disorders. Post TW, ed. UpToDate. Waltham, MA: UpToDate Inc. http://www.uptodate.com. Accessed August 31, 2021.
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