Carbidopa/levodopa 50-200mg CR Tabs

Manufacturer ADVAGEN PHARMA Active Ingredient Carbidopa and Levodopa Extended- Release Tablets(kar bi DOE pa & lee voe DOE pa) Pronunciation kar bi DOE pa & lee voe DOE pa
It is used to treat Parkinson's disease.It is used to treat signs like Parkinson's disease caused by other health problems.It may be given to you for other reasons. Talk with the doctor.
đŸˇī¸
Drug Class
Antiparkinsonian agent
đŸ§Ŧ
Pharmacologic Class
Dopamine precursor; Aromatic L-amino acid decarboxylase inhibitor
🤰
Pregnancy Category
Category C
✅
FDA Approved
Jun 1978
âš–ī¸
DEA Schedule
Not Controlled

Overview

â„šī¸

What is this medicine?

This medication is used to treat Parkinson's disease. It contains two medicines: carbidopa and levodopa. Levodopa helps replace a natural substance in your brain called dopamine, which is low in Parkinson's disease. Carbidopa helps more levodopa get to your brain and reduces side effects. This is an extended-release tablet, meaning it releases the medicine slowly over time to provide more consistent symptom control.
📋

How to Use This Medicine

Taking Your Medication Correctly

To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. You can take this medication with or without food. Swallow the tablet whole - do not chew or crush it. If you have a product that can be broken in half, do not chew or crush it. Check with your pharmacist or doctor if you have any questions.

If you take an iron supplement or a multivitamin that contains iron, ask your doctor or pharmacist for guidance on how to take it with this medication. Iron may reduce the absorption of this medication in your body. Additionally, a diet high in protein, fat, or calories, as well as consuming acidic foods, may also affect how well your body absorbs this medication. Discuss your diet with your doctor, especially if you plan to make any changes.

Continue taking this medication even when you are not experiencing symptoms. Keep a record of your symptoms to track your progress. Take this medication at the same time every day, as directed by your doctor or healthcare provider, even if you feel well.

Storing and Disposing of Your Medication

Store your medication at room temperature, away from light and moisture. Keep it in a dry place, such as a closet or drawer, and avoid storing it in the bathroom. Keep all medications out of the reach of children and pets. Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so. If you have questions about disposing of your medication, consult your pharmacist. You may also have access to a drug take-back program in your area.

What to Do If You Miss a Dose

If you miss a dose, take it as soon as you remember. However, if it is close to the time for your next dose, skip the missed dose and resume your regular schedule. Do not take two doses at the same time or take extra doses to make up for a missed one.
💡

Lifestyle & Tips

  • Take this medication with food to reduce stomach upset, but avoid high-protein meals as they can reduce the absorption of the medicine. If you experience nausea, try taking it with a small, low-protein snack.
  • Do not crush, chew, or divide extended-release tablets. Swallow them whole.
  • Do not stop taking this medication suddenly without consulting your doctor, as it can lead to serious withdrawal symptoms (neuroleptic malignant syndrome-like syndrome).
  • Be aware of potential dizziness or lightheadedness, especially when standing up quickly. Change positions slowly.
  • Avoid driving or operating machinery until you know how this medication affects you, as it can cause drowsiness or sudden sleep attacks.
  • Maintain regular follow-up appointments with your doctor to monitor your symptoms and adjust your dose as needed.

Dosing & Administration

đŸ‘¨â€âš•ī¸

Adult Dosing

Standard Dose: Individualized, typically 50/200mg CR twice daily, separated by at least 6 hours.
Dose Range: 50 - 2000 mg

Condition-Specific Dosing:

Parkinson's Disease (Initial): Initially, 50 mg carbidopa/200 mg levodopa CR twice daily. Dosing should be individualized and adjusted gradually, usually at intervals of not less than 3 days. Max daily dose of levodopa is 2000 mg.
Conversion from IR Carbidopa/Levodopa: Approximately 10% more levodopa may be required when converting from immediate-release to extended-release. Patients receiving less than 700 mg/day of levodopa IR can be converted to 50/200 mg CR twice daily. Patients receiving 700-1000 mg/day of levodopa IR can be converted to 50/200 mg CR 3 times daily.
đŸ‘ļ

Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established
âš•ī¸

Dose Adjustments

Renal Impairment:

Mild: No specific dose adjustment recommended, use with caution.
Moderate: No specific dose adjustment recommended, use with caution.
Severe: No specific dose adjustment recommended, use with caution. Monitor for adverse effects.
Dialysis: Not significantly removed by dialysis. No specific dose adjustment, but monitor closely.

Hepatic Impairment:

Mild: No specific dose adjustment recommended, use with caution.
Moderate: No specific dose adjustment recommended, use with caution.
Severe: No specific dose adjustment recommended, use with caution. Monitor for adverse effects.

Pharmacology

đŸ”Ŧ

Mechanism of Action

Carbidopa inhibits peripheral decarboxylation of levodopa by aromatic L-amino acid decarboxylase (AADC), allowing a greater proportion of levodopa to cross the blood-brain barrier for conversion to dopamine. Levodopa is a metabolic precursor of dopamine, which is deficient in the brains of patients with Parkinson's disease. Once in the brain, levodopa is decarboxylated to dopamine, replenishing dopamine stores in the substantia nigra.
📊

Pharmacokinetics

Absorption:

Bioavailability: Levodopa: Approximately 30% (variable for IR, CR is slower and more sustained). Carbidopa: Approximately 58%.
Tmax: Levodopa: 2-3 hours (for CR formulation). Carbidopa: 2-4 hours.
FoodEffect: High-protein meals can significantly reduce the absorption of levodopa due to competition for transport across the intestinal wall. Food generally delays and may decrease the extent of absorption for CR formulations.

Distribution:

Vd: Levodopa: Approximately 0.9-1.6 L/kg. Carbidopa: Not well characterized, but primarily extracellular.
ProteinBinding: Levodopa: 10-30% (low). Carbidopa: Approximately 36%.
CnssPenetration: Levodopa: Yes (after carbidopa inhibits peripheral metabolism). Carbidopa: Limited (does not cross BBB significantly).

Elimination:

HalfLife: Levodopa: Approximately 1.5-2 hours (when co-administered with carbidopa). Carbidopa: Approximately 2-3 hours.
Clearance: Levodopa: Approximately 0.3 L/hr/kg.
ExcretionRoute: Primarily renal (urine) as metabolites.
Unchanged: Levodopa: Less than 1% excreted unchanged. Carbidopa: Approximately 30% excreted unchanged.
âąī¸

Pharmacodynamics

OnsetOfAction: 30-60 minutes (slower than IR formulations)
PeakEffect: 2-4 hours
DurationOfAction: 4-6 hours or longer (due to extended-release formulation)

Safety & Warnings

âš ī¸

Side Effects

Serious Side Effects: Seek Medical Help Right Away

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:

Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high or low blood pressure, including:
+ Severe headache or dizziness
+ Passing out
+ Changes in eyesight
New or worsening behavioral or mood changes, such as:
+ Depression
+ Thoughts of suicide
Hallucinations (seeing or hearing things that are not there)
Feeling confused
Strong, uncontrollable urges (e.g., eating, gambling, sex, or spending money)
A skin lump or growth
Changes in the color or size of a mole
New or worsening trouble controlling body movements
Eyelid twitching
Muscle twitching
Stomach pain
Black, tarry, or bloody stools
Vomiting blood or coffee ground-like material
Chest pain or pressure
Fast or abnormal heartbeat
Fever, chills, or sore throat
Unexplained bruising or bleeding
Feeling extremely tired or weak
Dark urine or yellow skin and eyes
Changes in eyesight, eye pain, or severe eye irritation
Shortness of breath
Sudden, unexplained sleepiness, especially during activities like driving, eating, or talking

If you experience sudden sleepiness, do not drive or engage in activities that require alertness. Contact your doctor immediately.

Other Possible Side Effects

Like all medications, this drug can cause side effects. Many people may not experience any side effects or only minor ones. If you notice any of the following side effects or any others that bother you or do not go away, contact your doctor:

Bad dreams
Constipation
Dizziness or sleepiness
Dry mouth
Headache
Trouble sleeping
Some products may cause a dark red, brown, or black color to appear in your saliva, urine, or sweat (this is harmless but may discolor your clothes)
* Upset stomach or vomiting

This is not an exhaustive list of possible side effects. If you have questions or concerns, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
🚨

Seek Immediate Medical Attention If You Experience:

  • New or worsening involuntary movements (twitching, jerking, twisting)
  • Severe dizziness or fainting spells
  • Hallucinations (seeing or hearing things that aren't there)
  • Confusion or unusual thoughts
  • Unusual urges or behaviors (e.g., compulsive gambling, increased sexual urges, uncontrolled spending, binge eating)
  • Severe nausea or vomiting that doesn't improve
  • Darkening of urine, sweat, or saliva (harmless but can stain clothes)
  • Chest pain or irregular heartbeat
  • Muscle stiffness, fever, or sweating (signs of neuroleptic malignant syndrome-like syndrome, especially if medication is stopped suddenly)
📋

Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced.
Certain health conditions, including:
+ Glaucoma
+ Skin lumps or growths
+ A history of skin cancer
Medications you are currently taking, such as:
+ Reserpine or tetrabenazine
+ Linezolid or methylene blue
If you have taken specific medications for depression or Parkinson's disease within the last 14 days, including:
+ Isocarboxazid
+ Phenelzine
+ Tranylcypromine
+ Selegiline
+ Rasagiline (note: taking this medication with these drugs can lead to very high blood pressure)
* If you are taking another medication that contains the same active ingredient as this drug

This list is not exhaustive, and it is crucial to inform your doctor and pharmacist about all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any health problems you have. This will help ensure your safety while taking this medication. Never start, stop, or change the dose of any medication without consulting your doctor first.
âš ī¸

Precautions & Cautions

Important Information to Share with Your Healthcare Team

Inform all of your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. This will help ensure that you receive the best possible care.

Safety Precautions

To avoid accidents, do not drive or perform tasks that require alertness until you know how this medication affects you. When getting up from a sitting or lying down position, rise slowly to reduce the risk of dizziness or fainting. Be cautious when climbing stairs.

Lab Tests and Monitoring

This medication may interfere with certain laboratory tests. Be sure to inform all of your healthcare providers and lab personnel that you are taking this medication. Follow your doctor's instructions for regular blood work and eye exams.

Special Considerations for People with Diabetes

If you have high blood sugar (diabetes), consult with your doctor about the best glucose tests to use while taking this medication.

Managing Your Medication

As the time approaches for your next dose, you may experience a decrease in the medication's effectiveness. If this occurs and bothers you, discuss it with your doctor.

Interactions with Other Substances

Before consuming alcohol, marijuana, or other forms of cannabis, or taking prescription or over-the-counter medications that may cause drowsiness, talk to your doctor.

Skin Cancer Risk

People with Parkinson's disease may have a higher risk of developing a type of skin cancer called melanoma. It is unclear if this medication also increases this risk. While taking this medication, have regular skin exams and discuss any concerns with your doctor.

Stopping or Changing Your Medication

Do not suddenly stop taking this medication or reduce your dose without consulting your doctor. Stopping or changing your medication abruptly can cause severe side effects, including fever, muscle cramps or stiffness, dizziness, severe headache, confusion, changes in thinking, abnormal heartbeat, or excessive sweating. If you experience any of these symptoms, contact your doctor immediately.

Pregnancy and Breastfeeding

If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor. You and your doctor will need to discuss the potential benefits and risks of this medication to you and your baby.
🆘

Overdose Information

Overdose Symptoms:

  • Severe involuntary movements (dyskinesias)
  • Palpitations or irregular heartbeat
  • Orthostatic hypotension (dizziness upon standing)
  • Nausea, vomiting
  • Confusion, agitation, psychosis
  • Insomnia

What to Do:

Seek immediate medical attention. Call 911 or your local emergency number. In the US, you can also call Poison Control at 1-800-222-1222. Management is supportive, including gastric lavage, IV fluids, and careful monitoring of cardiac and respiratory function. Antiarrhythmics may be needed for cardiac arrhythmias.

Drug Interactions

đŸšĢ

Contraindicated Interactions

  • Non-selective Monoamine Oxidase Inhibitors (MAOIs) (e.g., phenelzine, tranylcypromine) - risk of hypertensive crisis. Must be discontinued at least 2 weeks prior to initiating carbidopa/levodopa.
🔴

Major Interactions

  • Antipsychotics (e.g., haloperidol, chlorpromazine, risperidone, olanzapine) - may antagonize the effects of levodopa due to dopamine receptor blockade.
  • Iron salts (ferrous sulfate, gluconate) - can chelate levodopa, reducing its absorption.
  • Metoclopramide - may antagonize the effects of levodopa and increase risk of extrapyramidal symptoms.
  • High-protein diet - competition for absorption and transport across the blood-brain barrier, reducing levodopa efficacy.
🟡

Moderate Interactions

  • Antihypertensives - additive hypotensive effects, increasing risk of orthostatic hypotension.
  • Tricyclic Antidepressants (TCAs) - theoretical risk of increased blood pressure, though generally considered safe with careful monitoring.
  • Pyridoxine (Vitamin B6) - large doses (e.g., >10-25 mg) can reverse the effects of levodopa if carbidopa is not present in sufficient amounts (less relevant with carbidopa/levodopa combination).
đŸŸĸ

Minor Interactions

  • Antacids - may increase levodopa absorption slightly.

Monitoring

đŸ”Ŧ

Baseline Monitoring

Neurological assessment (motor function, cognitive status)

Rationale: To establish baseline severity of Parkinson's symptoms and identify any pre-existing cognitive impairment.

Timing: Prior to initiation of therapy.

Blood pressure (supine and standing)

Rationale: To assess for baseline orthostatic hypotension and monitor for drug-induced hypotension.

Timing: Prior to initiation of therapy.

Renal and hepatic function tests

Rationale: To assess overall organ function, though specific dose adjustments are not typically required, caution is advised in severe impairment.

Timing: Prior to initiation of therapy.

📊

Routine Monitoring

Motor symptoms (bradykinesia, rigidity, tremor, gait)

Frequency: Regularly, at each follow-up visit (e.g., every 1-3 months during titration, then every 3-6 months)

Target: Optimal symptom control with minimal side effects.

Action Threshold: Worsening of symptoms, emergence of 'wearing-off' or 'on-off' phenomena, or development of dyskinesias.

Dyskinesias (involuntary movements)

Frequency: Regularly, at each follow-up visit

Target: Absence or minimal, non-disabling dyskinesias.

Action Threshold: Development of troublesome or disabling dyskinesias.

Psychiatric symptoms (hallucinations, delusions, impulse control disorders, depression)

Frequency: Regularly, at each follow-up visit

Target: Absence of new or worsening psychiatric symptoms.

Action Threshold: Emergence or worsening of psychiatric symptoms.

Orthostatic blood pressure

Frequency: Regularly, especially during dose titration and if symptoms of dizziness or syncope occur.

Target: Stable blood pressure without significant orthostatic drop.

Action Threshold: Significant drop in systolic (>20 mmHg) or diastolic (>10 mmHg) blood pressure upon standing, or symptomatic hypotension.

đŸ‘ī¸

Symptom Monitoring

  • Worsening of Parkinson's symptoms (tremor, stiffness, slowness)
  • New or worsening involuntary movements (dyskinesias)
  • Periods of 'wearing off' (symptoms return before next dose)
  • Sudden 'on-off' fluctuations
  • Dizziness or lightheadedness upon standing
  • Nausea or vomiting
  • Sleepiness or sudden onset of sleep
  • Hallucinations, delusions, confusion
  • Unusual urges or behaviors (e.g., gambling, hypersexuality, compulsive shopping, binge eating)
  • Darkening of urine, sweat, or saliva

Special Patient Groups

🤰

Pregnancy

Category C. Animal studies have shown adverse effects on fetal development. There are no adequate and well-controlled studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus.

Trimester-Specific Risks:

First Trimester: Potential for developmental toxicity observed in animal studies.
Second Trimester: Potential for developmental toxicity observed in animal studies.
Third Trimester: Potential for developmental toxicity observed in animal studies. May inhibit lactation.
🤱

Lactation

Levodopa is excreted into breast milk. Carbidopa/levodopa may inhibit lactation. Due to the potential for serious adverse reactions in breastfed infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Infant Risk: Moderate risk (L3). Potential for central nervous system effects in the infant and inhibition of lactation.
đŸ‘ļ

Pediatric Use

Safety and effectiveness in pediatric patients have not been established. Not indicated for use in children.

👴

Geriatric Use

Elderly patients may be more sensitive to the central nervous system side effects of carbidopa/levodopa, such as dyskinesias, hallucinations, and orthostatic hypotension. Dose titration should be done cautiously.

Clinical Information

💎

Clinical Pearls

  • Carbidopa/levodopa CR is designed to provide more sustained levodopa levels and reduce 'wearing-off' fluctuations compared to immediate-release formulations, but its absorption can be more variable.
  • Patients converting from immediate-release to CR may require a higher total daily dose of levodopa (approximately 10% more) due to differences in bioavailability.
  • Do not crush or chew CR tablets; this will destroy the extended-release properties and can lead to rapid absorption and increased side effects.
  • Counsel patients on the importance of avoiding high-protein meals close to dosing, as protein can interfere with levodopa absorption.
  • Monitor closely for impulse control disorders (e.g., pathological gambling, hypersexuality, compulsive shopping, binge eating) which can occur with dopaminergic therapies.
  • Sudden discontinuation of carbidopa/levodopa can lead to a neuroleptic malignant syndrome-like syndrome (fever, muscle rigidity, altered mental status, autonomic instability); taper off slowly if discontinuation is necessary.
🔄

Alternative Therapies

  • Dopamine agonists (e.g., pramipexole, ropinirole, rotigotine)
  • MAO-B inhibitors (e.g., selegiline, rasagiline, safinamide)
  • COMT inhibitors (e.g., entacapone, opicapone, tolcapone)
  • Amantadine (for dyskinesia and motor fluctuations)
  • Istradefylline (adenosine A2A receptor antagonist)
  • Pimavanserin (for Parkinson's disease psychosis)
💰

Cost & Coverage

Average Cost: $50 - $300+ per 30 tablets (generic 50-200mg CR)
Generic Available: Yes
Insurance Coverage: Tier 1 or Tier 2 (generic), Tier 3 or 4 (brand)
📚

General Drug Facts

If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide information about what was taken, the amount, and the time it occurred.