Pregabalin 20mg/ml Solution

Manufacturer ASCEND LABORATORIES Active Ingredient Pregabalin Oral Solution(pre GAB a lin) Pronunciation pre GAB a lin
It is used to help control certain kinds of seizures.It is used to treat painful nerve diseases.It is used to treat fibromyalgia.It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Anticonvulsant, Analgesic
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Pharmacologic Class
Gamma-aminobutyric acid (GABA) analogue
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Pregnancy Category
Category C
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FDA Approved
Dec 2004
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DEA Schedule
Schedule V

Overview

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What is this medicine?

Pregabalin is a medication used to treat certain types of nerve pain, such as pain from diabetes or shingles, and pain from fibromyalgia. It is also used to treat partial seizures and generalized anxiety disorder. It works by calming overactive nerves in the body.
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How to Use This Medicine

Taking Your Medication Correctly

To ensure you get the most benefit from your medication, follow these steps:

Take your medication exactly as directed by your doctor.
Read all the information provided with your medication and follow the instructions carefully.
You can take your medication with or without food.
If you are taking a liquid dose, measure it carefully using the measuring device that comes with the medication. If no device is provided, ask your pharmacist for one to ensure accurate measurement.

Continuing Your Medication Regimen

Continue taking your medication as instructed by your doctor or healthcare provider, even if you start to feel better. It is essential to complete the full course of treatment as directed.

Storing and Disposing of Your Medication

To maintain the quality and safety of your medication:

Store it in its original container at room temperature.
Keep it in a dry place, away from the bathroom.
Store your medication in a secure location where children cannot see or reach it, and where others cannot access it. Consider using a locked box or area to keep it safe.
Keep all medications out of reach of pets.

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 scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
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Lifestyle & Tips

  • Avoid alcohol and other CNS depressants (e.g., opioids, sedatives) as they can increase drowsiness and dizziness.
  • Do not drive or operate heavy machinery until you know how pregabalin affects you, as it can cause dizziness and somnolence.
  • Do not stop taking pregabalin suddenly, especially if you have been taking it for a long time or at high doses. This can lead to withdrawal symptoms like insomnia, nausea, headache, or anxiety. Your doctor will help you gradually reduce the dose.
  • Report any unusual changes in mood or behavior, including thoughts of self-harm, to your doctor immediately.
  • Report any swelling of the face, lips, tongue, or throat, or difficulty breathing, as these could be signs of a serious allergic reaction (angioedema).

Dosing & Administration

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Adult Dosing

Standard Dose: Varies by indication. Typically initiated at 75 mg BID or 50 mg TID (150 mg/day) and titrated up based on response and tolerability. Max 600 mg/day.
Dose Range: 150 - 600 mg

Condition-Specific Dosing:

Neuropathic Pain (Diabetic Peripheral Neuropathy): Initial: 50 mg TID (150 mg/day). Titrate to 100 mg TID (300 mg/day) within 1 week. Max: 300 mg BID (600 mg/day).
Postherpetic Neuralgia: Initial: 75 mg BID or 50 mg TID (150 mg/day). Titrate to 150 mg BID or 100 mg TID (300 mg/day) within 1 week. Max: 300 mg BID (600 mg/day).
Fibromyalgia: Initial: 75 mg BID (150 mg/day). Titrate to 150 mg BID (300 mg/day) within 1 week. Max: 225 mg BID (450 mg/day).
Partial Onset Seizures (Adjunctive Therapy): Initial: 75 mg BID (150 mg/day). Titrate to 150-300 mg BID (300-600 mg/day). Max: 300 mg BID (600 mg/day).
Generalized Anxiety Disorder (GAD): Initial: 150 mg/day. Titrate in 50 mg increments every 2-3 days. Max: 600 mg/day.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established for general use. For partial onset seizures (adjunctive therapy): 1 month to <4 years: 3.5 mg/kg/day in 3 divided doses. Max 14 mg/kg/day. Oral solution is preferred for this age group.
Child: For partial onset seizures (adjunctive therapy): 4 to <17 years: 2.5 mg/kg/day in 2-3 divided doses. Max 10 mg/kg/day. Oral solution is preferred for younger children.
Adolescent: Dosing for partial onset seizures (adjunctive therapy) is similar to adult dosing, starting at 75 mg BID (150 mg/day) and titrating up to 300-600 mg/day based on weight and response.
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Dose Adjustments

Renal Impairment:

Mild: CrCl 60 mL/min or greater: No adjustment needed.
Moderate: CrCl 30-59 mL/min: Reduce total daily dose by 50%. Administer in 2-3 divided doses. Max 300 mg/day.
Severe: CrCl 15-29 mL/min: Reduce total daily dose by 75%. Administer in 1-2 divided doses. Max 150 mg/day.
Dialysis: CrCl less than 15 mL/min: Reduce total daily dose by 80-90%. Administer in a single dose. Max 75 mg/day. A supplemental dose (e.g., 25-100 mg) should be given immediately following a 4-hour hemodialysis session.
Confidence: High

Hepatic Impairment:

Mild: No adjustment needed.
Moderate: No adjustment needed.
Severe: No adjustment needed (Pregabalin is negligibly metabolized by the liver).

Pharmacology

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Mechanism of Action

Pregabalin binds with high affinity to the alpha2-delta (ι2-δ) subunit of voltage-gated calcium channels in the central nervous system. While the precise mechanism of action is not fully understood, binding to the ι2-δ subunit is thought to modulate the release of several excitatory neurotransmitters, including glutamate, norepinephrine, and substance P. This modulation leads to a reduction in neuronal excitability and pain signaling.
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Pharmacokinetics

Absorption:

Bioavailability: >=90%
Tmax: Approximately 1.5 hours (fasted state)
FoodEffect: Food delays Tmax by approximately 2.5 hours and decreases Cmax by 25-30%, but does not significantly affect the extent of absorption (AUC).

Distribution:

Vd: Approximately 0.56 L/kg
ProteinBinding: <1%
CnssPenetration: Yes

Elimination:

HalfLife: Approximately 6.3 hours
Clearance: Primarily renal clearance, proportional to creatinine clearance.
ExcretionRoute: Renal (unchanged drug)
Unchanged: >90%
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Pharmacodynamics

OnsetOfAction: Within 1 week for some indications (e.g., neuropathic pain), but full effect may take longer with titration.
PeakEffect: Varies by indication and individual response, typically observed after dose titration.
DurationOfAction: Approximately 12 hours (consistent with BID dosing)
Confidence: High

Safety & Warnings

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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 or your caregiver 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
Changes in eyesight
Muscle pain or weakness
Changes in balance
Feeling confused
Shakiness
Trouble breathing, slow breathing, or shallow breathing
Blue or gray color of the skin, lips, nail beds, fingers, or toes
Memory problems or loss
Shortness of breath, significant weight gain, or swelling in the arms or legs
Fast or abnormal heartbeat
Fever, chills, or sore throat
Skin sores or any skin changes
Trouble speaking
Trouble sleeping
Trouble walking
Feeling high (excessive laughter and euphoria)
Twitching

If you experience extreme drowsiness, dizziness, or loss of consciousness, seek medical help immediately. Caregivers should also seek medical help right away if the patient is unresponsive, uncommunicative, or unable to wake up.

Suicidal Thoughts or Actions

Like other medications used to treat seizures, this drug may increase the risk of suicidal thoughts or behaviors, particularly in individuals with a history of suicidal ideation or attempts. If you or your caregiver notice any new or worsening symptoms, such as:

Depression
Anxiety, restlessness, or irritability
Panic attacks
Mood or behavioral changes

contact your doctor immediately. If suicidal thoughts or actions occur, seek medical help right away.

Low Platelet Counts

This medication may rarely cause low platelet counts, increasing the risk of bleeding. If you experience unexplained bruising or bleeding, contact your doctor immediately.

Other Side Effects

Most people do not experience significant side effects, but some may occur. If you experience any of the following side effects, contact your doctor if they bother you or persist:

Dizziness, drowsiness, fatigue, or weakness
Weight gain
Difficulty concentrating
Headache
Dry mouth
Constipation
Increased appetite
Upset stomach
Joint pain
Nose or throat irritation

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

  • Severe dizziness or drowsiness
  • Blurred vision or other vision changes
  • Swelling of hands, feet, or ankles (peripheral edema)
  • Unexplained weight gain
  • Muscle pain, tenderness, or weakness (especially if accompanied by fever or dark urine)
  • New or worsening depression, anxiety, or agitation
  • Thoughts of self-harm or suicide
  • Signs of allergic reaction: rash, hives, swelling of face/lips/tongue/throat, difficulty breathing or swallowing
  • Signs of respiratory depression: unusually slow or shallow breathing, extreme drowsiness, blue lips/fingernails
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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. Be sure to describe the symptoms you experienced.
If you have kidney disease, as this may affect how your body processes the medication.
* If you are breastfeeding, as you should not breastfeed while taking this medication.

Additionally, it is crucial to discuss all of your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. This includes any health problems you may have, as they can interact with this medication. To ensure your safety, do not start, stop, or change the dose of any medication without first consulting your doctor. This will help determine whether it is safe for you to take this medication in combination with your other medications and health conditions.
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Precautions & Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.

Before engaging in activities that require alertness or clear vision, such as driving, wait until you understand how this medication affects you.

If you experience changes in your seizures or if they worsen after starting this medication, consult your doctor promptly.

Do not abruptly stop taking this medication without first consulting your doctor, as this may increase your risk of side effects. If you need to discontinue this medication, your doctor will guide you on how to gradually stop taking it to minimize potential risks.

While taking this medication, avoid consuming alcohol. Additionally, before using marijuana, cannabis products, or prescription and over-the-counter medications that may cause drowsiness, discuss the potential risks with your doctor.

A rare but severe reaction called angioedema has been associated with this medication, which can be life-threatening in some cases. Symptoms may include swelling of the hands, face, lips, eyes, tongue, or throat, difficulty breathing, swallowing problems, or unusual hoarseness. Seek immediate medical attention if you experience any of these symptoms.

There is a risk of severe breathing problems when taking this medication, particularly in individuals who are also taking opioid pain medications or have pre-existing lung or breathing issues. This risk may be higher in people over 65 years old, and in some cases, breathing problems have been fatal. If you have concerns, discuss them with your doctor.

If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects.

Men who plan to father a child should discuss the potential risks with their doctor, as this medication has been shown to decrease fertility and cause sperm changes in male animals, and has also been linked to birth defects in the offspring of treated male animals. Although it is not known if these effects occur in humans, it is crucial to have this conversation.

If you are pregnant or planning to become pregnant, inform your doctor, as you will need to discuss the benefits and risks of using this medication during pregnancy.
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Overdose Information

Overdose Symptoms:

  • Somnolence
  • Confusion
  • Agitation
  • Restlessness
  • Seizures
  • Coma

What to Do:

In case of overdose, seek immediate medical attention or call Poison Control at 1-800-222-1222. Treatment is generally supportive and may include gastric lavage or emesis. Hemodialysis can remove pregabalin from the system if necessary.

Drug Interactions

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Moderate Interactions

  • CNS depressants (e.g., alcohol, benzodiazepines, opioids, barbiturates, sedatives, anxiolytics, muscle relaxants, antihistamines)
  • Thiazolidinedione antidiabetic agents (e.g., rosiglitazone, pioglitazone)

Monitoring

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Baseline Monitoring

Renal function (CrCl)

Rationale: Pregabalin is primarily renally excreted; dose adjustment is required in patients with impaired renal function.

Timing: Prior to initiation of therapy.

Baseline weight

Rationale: Pregabalin can cause weight gain.

Timing: Prior to initiation of therapy.

History of angioedema or hypersensitivity reactions

Rationale: To assess risk of severe hypersensitivity reactions.

Timing: Prior to initiation of therapy.

History of substance abuse

Rationale: Pregabalin is a Schedule V controlled substance with potential for abuse and dependence.

Timing: Prior to initiation of therapy.

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Routine Monitoring

Clinical response and tolerability

Frequency: Regularly during titration and maintenance.

Target: Optimal symptom control with minimal adverse effects.

Action Threshold: Lack of efficacy or intolerable side effects warrant dose adjustment or discontinuation.

Signs/symptoms of suicidal ideation or behavior

Frequency: Regularly, especially during initial therapy and dose changes.

Target: Absence of new or worsening suicidal thoughts/behavior.

Action Threshold: Any emergence or worsening of suicidal thoughts/behavior requires immediate clinical evaluation and intervention.

Weight

Frequency: Periodically, especially if concerns about weight gain.

Target: Stable weight or acceptable weight gain.

Action Threshold: Significant or problematic weight gain may require intervention.

Peripheral edema

Frequency: Periodically.

Target: Absence of or stable, non-problematic edema.

Action Threshold: Significant or worsening edema may require intervention.

Vision changes (e.g., blurred vision, diplopia)

Frequency: If patient reports symptoms.

Target: Normal vision.

Action Threshold: Persistent or severe vision changes warrant ophthalmologic evaluation.

Signs/symptoms of angioedema (e.g., swelling of face, mouth, throat)

Frequency: Patient education for self-monitoring.

Target: Absence of angioedema.

Action Threshold: Immediate medical attention if angioedema occurs.

Signs/symptoms of respiratory depression (especially with concomitant CNS depressants)

Frequency: Monitor closely, especially with co-administration of opioids or other CNS depressants.

Target: Normal respiratory rate and effort.

Action Threshold: Bradypnea, shallow breathing, or hypoxemia requires immediate intervention.

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Symptom Monitoring

  • Dizziness
  • Somnolence
  • Ataxia
  • Blurred vision
  • Weight gain
  • Peripheral edema
  • Dry mouth
  • Difficulty concentrating
  • Suicidal thoughts or behavior
  • Signs of hypersensitivity (rash, hives, swelling of face/lips/tongue/throat)
  • Signs of respiratory depression (slow, shallow breathing, extreme drowsiness)

Special Patient Groups

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Pregnancy

Pregabalin is classified as Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown developmental toxicity (skeletal malformations, growth retardation) at doses higher than human therapeutic doses.

Trimester-Specific Risks:

First Trimester: Potential for increased risk of major congenital malformations, particularly neural tube defects, based on some observational studies, though data are conflicting and require further investigation. Avoid if possible.
Second Trimester: Limited data. Risk of fetal growth restriction observed in animal studies.
Third Trimester: Limited data. Potential for neonatal withdrawal symptoms if discontinued abruptly near term.
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Lactation

Pregabalin is excreted into human milk. The amount of pregabalin ingested by a breastfed infant is estimated to be 7% of the maternal weight-adjusted dose. The American Academy of Pediatrics considers pregabalin to be of 'unknown effect' on the nursing infant. Monitor breastfed infants for sedation, poor feeding, and weight gain.

Infant Risk: L3 (Moderately safe). Monitor infant for drowsiness, poor feeding, and developmental milestones. Consider alternative if infant shows adverse effects.
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Pediatric Use

Approved for adjunctive treatment of partial onset seizures in patients 1 month of age and older. Dosing is weight-based. Safety and efficacy for other indications (neuropathic pain, fibromyalgia, GAD) have not been established in pediatric patients.

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Geriatric Use

Dose adjustment is necessary for elderly patients (65 years and older) due to age-related decline in renal function. Start with lower doses and titrate slowly. Elderly patients may be more susceptible to adverse effects such as dizziness, somnolence, and falls.

Clinical Information

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Clinical Pearls

  • Titration is key: Start low and go slow to minimize side effects and optimize efficacy.
  • Withdrawal symptoms: Abrupt discontinuation can lead to withdrawal symptoms (insomnia, nausea, headache, anxiety, sweating, diarrhea). Always taper the dose gradually over at least 1 week.
  • Potential for abuse/misuse: As a Schedule V controlled substance, pregabalin has a potential for abuse and dependence. Prescribe with caution in patients with a history of substance abuse.
  • Weight gain and edema: Counsel patients about potential weight gain and peripheral edema, especially if co-administered with thiazolidinediones.
  • CNS depressant effects: Warn patients about additive CNS depression with alcohol, opioids, and other sedatives. Advise against driving or operating machinery until effects are known.
  • Oral solution: The 20mg/ml oral solution is particularly useful for pediatric dosing, patients with dysphagia, or those requiring precise dose adjustments.
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Alternative Therapies

  • Gabapentin (for neuropathic pain, seizures)
  • Duloxetine (for neuropathic pain, fibromyalgia, GAD)
  • Venlafaxine (for neuropathic pain, GAD)
  • Tricyclic antidepressants (e.g., amitriptyline, nortriptyline for neuropathic pain)
  • SNRIs (e.g., milnacipran for fibromyalgia)
  • Other antiepileptic drugs (e.g., carbamazepine, oxcarbazepine, lamotrigine for seizures)
  • Benzodiazepines (e.g., alprazolam, lorazepam for GAD, short-term)
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Cost & Coverage

Average Cost: Varies widely by pharmacy, dosage, and quantity. Typically ranges from $50 to $300+ for a month's supply of generic. per 473 mL bottle of 20mg/mL solution
Generic Available: Yes
Insurance Coverage: Often covered by most insurance plans, typically Tier 1 or Tier 2 for generic. Brand name may require prior authorization or higher co-pay.
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General Drug Facts

If your symptoms or health issues persist or worsen, it's essential to contact your doctor promptly. To ensure safe use, never share your medication with others or take someone else's medication. This medication is accompanied by a Medication Guide, which provides crucial information. Please read this guide carefully and review it again whenever you receive a refill. If you have any questions or concerns about this medication, don't hesitate to consult your doctor, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.