carbidopa-levodopa

(redirected from Sinemet cr)
Also found in: Dictionary.

carbidopa-levodopa

Apo-Levocarb (CA), Co-carledopa (UK), Dom-Levo-Carbidopa (CA), Half Sinemet (UK), Novo-Levocarbidopa (CA), Nu-Levocarb (CA), Sinemet, Sinemet CR, Tilolec (UK)

Pharmacologic class: Dopamine agonist

Therapeutic class: Antiparkinsonian

Pregnancy risk category C

Action

After conversion to dopamine in CNS, levodopa acts as a neurotransmitter, relieving symptoms of Parkinson's disease. Carbidopa prevents destruction of levodopa, making more levodopa available to be decarboxylated to dopamine in brain.

Availability

Tablets: 10 mg carbidopa/100 mg levodopa, 25 mg carbidopa/100 mg levodopa, 25 mg carbidopa/250 mg levodopa

Tablets (extended-release): 25 mg carbidopa/100 mg levodopa, 50 mg carbidopa/200 mg levodopa

Indications and dosages

Idiopathic Parkinson's disease; parkinsonism; symptomatic parkinsonism

Conventional tablets-

Adults not currently receiving levodopa: Initially, 10 mg carbidopa/100 mg levodopa P.O. three to four times daily or 25 mg carbidopa/100 mg levodopa t.i.d.; may be increased q 1 to 2 days until desired effect occurs

Adults converting from levodopa alone (less than 1.5 g/day): Initially, 25 mg carbidopa/100 mg levodopa three to four times daily; may be increased q 1 to 2 days until desired effect occurs

Adults converting from levodopa alone (more than 1.5 g/day): Initially, 25 mg carbidopa/250 mg levodopa three to four times daily; may be increased q 1 to 2 days until desired effect occurs

Extended-release tablets-

Adults not currently receiving levodopa: Initially, 50 mg carbidopa/200 mg levodopa P.O. b.i.d., with doses spaced at least 6 hours apart

Adults converting from standard carbidopa-levodopa: Initiate therapy with at least 10% more levodopa content/day (may need up to 30% more) given at 4- to 8-hour intervals while awake; wait 3 days between dosage changes. Some patients may need higher dosages and shorter dosing intervals.

Contraindications

• Hypersensitivity to drug or tartrazine

• Angle-closure glaucoma

• MAO inhibitor use within past 14 days

• Malignant melanoma

• Breastfeeding

Precautions

Use cautiously in:

• cerebrovascular, renal, hepatic, or endocrine disease

• history of cardiac, psychiatric, or ulcer disease

• abrupt drug discontinuation or dosage

• pregnant patients

• children ages 18 and under (safety not established).

Administration

• Give dose as close as possible to time ordered to ensure stable drug blood level.

• Know that giving extended-release form with food increases drug bioavailability.

• If patient needs general anesthesia, continue drug therapy as appropriate (if he's allowed to have oral fluids and drugs).

Be aware that drug shouldn't be withdrawn abruptly.

Adverse reactions

CNS: anxiety, dizziness, hallucinations, memory loss, headache, numbness, confusion, insomnia, nightmares, delusions, psychotic changes, depression, dementia, poor coordination, worsening hand tremor

CV: cardiac irregularities, palpitations, orthostatic hypotension

EENT: blurred vision, diplopia, mydriasis, eyelid twitching, difficulty swallowing

GI: nausea, vomiting, diarrhea, constipation, abdominal pain or discomfort, flatulence, excessive salivation, dry mouth, anorexia, upper GI hemorrhage (with history of peptic ulcer)

GU: urinary retention, urinary incontinence, dark urine

Hematologic: hemolytic anemia, leukopenia

Hepatic: hepatotoxicity

Musculoskeletal: muscle twitching, involuntary or spasmodic movements

Respiratory: hyperventilation

Skin: melanoma, flushing, rash, abnormally dark sweat

Other: altered or bitter taste, burning sensation of tongue, tooth grinding (especially at night), weight changes, hot flashes, hiccups

Interactions

Drug-drug. Anticholinergics: decreased carbidopa-levodopa absorption

Antihypertensives: additive hypotension

Haloperidol, papaverine, phenothiazines, phenytoin, reserpine: reversal of carbidopa-levodopa effects

Inhalation hydrocarbon anesthetics: increased risk of arrhythmias

MAO inhibitors: hypertensive reactions

Methyldopa: altered efficacy of carbidopa-levodopa, increased risk of adverse CNS reactions

Pyridoxine: antagonism of carbidopa-levodopa effects

Selegiline: increased risk of adverse reactions

Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, bilirubin, blood urea nitrogen, lactate dehydrogenase, low-density lipoproteins, protein-bound iodine, uric acid: increased levels
Coombs' test: false-positive result

Granulocytes, hemoglobin, platelets, white blood cells: decreased values

Urine glucose, urine ketones: test interference

Drug-food. Foods rich in pyridoxine (liver, yeast, cereals): reversal of carbidopa-levodopa effects

Drug-herbs. Kava: decreased carbidopa-levodopa efficacy

Octacosanol: worsening of dyskinesia

Drug-behaviors. Cocaine use: increased risk of adverse reactions to carbidopa-levodopa

Patient monitoring

• Monitor patient for orthostatic hypotension.

• Assess patient's need for drug "holiday" if his response to drug decreases.

Patient teaching

Inform patient that muscle and eyelid twitching may indicate toxicity. Tell him to report these symptoms immediately.

Caution patient not to stop taking drug abruptly.

• Instruct patient to swallow extended-release tablets whole without crushing or chewing them.

• Advise patient to move slowly when sitting up or standing, to avoid dizziness or light-headedness caused by sudden blood pressure drop.

• Tell patient that drug may darken or discolor his urine and sweat.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, herbs, and behaviors mentioned above.

References in periodicals archive ?
A multinational, double-blind, RCT demonstrated that transdermal rotigotine patch may significantly improve 10 individual Modified PDSS-2 items including respiratory problems and snoring of PD patients.[28] A secondary study found that bedtime Sinemet CR may reduce OSA in PD patients.[96]
Response of gait to an acute challenge with Sinemet CR before and during its use as maintenance anti-parkinsonian therapy.
Merck & Co., meanwhile, has withdrawn a lawsuit alleging patent infringement related to Impax Laboratories Inc.'s filing of an Abbreviated New Drug Application for a generic version of Sinemet CR tablets.
DRUG DOSAGE COST/DAY [*] DOPAMINE PRECURSOR carbidopa and Start at 25 mg of carbidopa $1.86 (75 mg levodopa and 100 mg of levodopa and 300 mg per t.i.d.; maximum dosage is day) 200 mg and 800 mg per day carbidopa and 50 mg of carbidopa and 200 $3.16 (100 mg levodopa mg of levodopa b.i.d.; and 400 mg per controlled-release maximum dose is 400 mg and day) (Sinemet CR) 1,600 mg per day DOPAMINE AGOINSTS bromocriptine Start with 2.5 mg/day; final $3.34 (5 mg) dose is usually 5-7.5 mg/day pergolide Start with 0.05 mg/day; $3.70 (1 mg) (Permax) maximum of 5 mg/day pramipexole Start with 0.125 mg t.i.d.; $5.49 (1 mg (Mirapex) maximum of 1.5 mg t.i.d.
A controlled-release formulation (Sinemet CR), which is now available, is effective in regulating the response to medication in patients who are experiencing end-of-dose fluctuations.
(Atamet) and DuPont Pharma (Sinemet and Sinemet CR) to relieve the symptoms of Parkinson's disease.