pregabalin

Action and Spectrum

Actions and spectrum: 

pregabalin is a medication used to treat neuropathic pain, seizures, and anxiety disorders. It works by binding to a specific type of calcium channel in the nervous system, reducing the release of certain neurotransmitters that are involved in pain and anxiety. 

pregabalin has a broad spectrum of activity and is effective against various types of neuropathic pain, including diabetic neuropathy, postherpetic neuralgia, and fibromyalgia.

It is also used to treat partial seizures in children over the age of 4 with epilepsy. Additionally, pregabalin is approved for the treatment of generalized anxiety disorder (GAD) in adults. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Lyrica 

• Blurred vision (1-12%) 
• Xerostomia (1-15%) 
• Ataxia (1-20%) 
• Somnolence (4-36%) 
• Fatigue (5-11%) 
• Dizziness (8-45%) 
• Tremor (11%) 
• Diplopia (12%) 
• Weight gain (16%) 
• Peripheral edema (16%)

Lyrica CR 

• Somnolence (0.5-11.4%) 
• Dizziness (3.4-17.1%)

1-10% 

Lyrica 

• Edema (8%) 
• Hypotension (2%) 
• Pain (5%) 
• Constipation (5%) 
• Accidental injury (4%) 
• Confusion (<7%) 
• Vertigo (1-4%) 
• Asthenia (5%) 
• Facial edema (<3%) 
• Neuropathy (2-9%) 
• Disorientation (<2%) 
• Weight gain (4%) 
• Abnormal thinking (2%) 
• Amnesia (<6%)

Lyrica CR 

• Headache (1.9-3.9%) 
• Balance disorder (0.5-2.6%) 
• Fatigue (2.4-3.9%) 
• Dry mouth (0.5-3.7%) 
• Peripheral edema (3.8-4.9%) 
• Joint swelling (1.9%) 
• increased ALT/AST (0.2-1.4%) 
• Vertigo (1-3.9%) 
• Vision blurred (0.5-3.7%) 
• increased Weight (2.5-3.8%) 
• Constipation (2.7%) 
• Nausea (3-3.4%) 
• Fatigue (1.4 -3.9%) 
• Nasopharyngitis (1.4-1.5%) 
• Diarrhea (1-1.4%)

<1% 

Anemia 

Gynecomastia 

Esophagitis 

Dystonia 

Hirsutism 

Addiction 

Diarrhea 

Epididymitis 

Dysmenorrhea 

Heart failure 

Uveitis 

breast enlargement  

Post marketing Reports 

Angioedema 

Creatinine kinase 

Pneumonia 

Bullous pemphigoid 

Suicidal behavior 

Decreased platelet count 

Viral infection 

Respiratory depression 

Black Box Warning

Black Box Warning: 

• Suicidal thoughts and behaviour: pregabalin may have an increased risk of suicidal thoughts, particularly in patients with a history of depression, anxiety, or other mental health conditions. Patients should be monitored closely for suicidal ideation or behaviour and any changes in mood or behaviour. 
• Abuse potential and dependence: pregabalin has the potential for abuse and dependence, particularly in people with a history of substance abuse or addiction. Patients should be monitored for signs of misuse or abuse, and the drug should be prescribed and dispensed with caution. 
• Respiratory depression: pregabalin may cause respiratory depression, particularly when taken with other drugs that have respiratory depressant effects. Patients have been monitored closely for respiratory depression, and the drug should be used with caution in patients with respiratory disorders. 
• Peripheral edema: pregabalin may cause peripheral edema, or swelling of the hands and feet. Patients should be monitored for signs of peripheral edema, and the drug should be used with caution in patients with heart failure or other conditions that may increase the risk of edema. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

pregabalin is contraindicated in patients who have demonstrated a hypersensitivity reaction to the drug or its components. It should also be avoided in patients with a history of angioedema. Additionally, pregabalin should not be used concomitantly with opioids, as it increases the risk of respiratory depression.  

Caution: 

• Suicidal thoughts or behaviour: pregabalin may increase the risk of suicidal thoughts or behaviour, particularly in people with a history of bipolar disorder, depression, or other mental health conditions. 
• Respiratory depression: pregabalin may cause respiratory depression, especially when used as combination drug that have similar effects on the respiratory system. 
• Dizziness and drowsiness: pregabalin may cause dizziness, drowsiness, or blurred vision, which can impair the ability to perform activities that require mental alertness, such as driving or operating machinery. 
• Dependence and withdrawal: pregabalin have the potential to cause dependence and withdrawal symptoms, particularly with long-term use or high doses. 
• Kidney disease: pregabalin is eliminated primarily through the kidneys, so people with kidney disease may require a lower dose or less frequent dosing to prevent the buildup of the drug in their system. 
• Elderly patients: Elderly patients may be more sensitive to the effects of pregabalin, including dizziness and drowsiness, and may require a lower dose or more frequent monitoring.

Comorbidities: 

pregabalin should be used under caution in patients with a history of substance abuse, including alcohol abuse, as it may increase the risk of abuse or dependence. It should also be used under caution in patients with a history of depression, suicidal ideation, or other mental health disorders, as it may increased risk of suicidal thoughts or behaviour. Additionally, pregabalin should be used with caution in patients with a history of kidney disease or heart disease, as these conditions may increase the risk of adverse effects. 

Pregnancy / Lactation

Pregnancy consideration: US FDA pregnancy category: Not assigned 

Lactation: pregabalin is excreted into human milk  

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: There is no evidence of risk to the fetus found in animal reproduction studies and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women. 
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh risks over benefits These category drugs should be prohibited for pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

pregabalin is a medication that belongs to the class of drugs called gabapentinoids. It is structurally like gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter, and binds to the alpha-2-delta subunit of voltage-gated calcium channels in the central nervous system. This binding results in a reduction in the release of neurotransmitters such as glutamate, substance P, and norepinephrine, which are involved in pain signaling and anxiety. 

pregabalin is rapidly absorbed after oral administration and reaches peak plasma concentrations within 1 to 1.5 hours. The drug is eliminated primarily through renal excretion, with a half-life of approximately 6 hours. pregabalin does not bind extensively to plasma proteins and does not induce or inhibit cytochrome P450 enzymes.  

Pharmacodynamics: 

pregabalin is a structural analog of the neurotransmitter gamma-aminobutyric acid (GABA), but it does not bind to GABA receptors. Instead, pregabalin selectively binds to the alpha-2-delta subunit of voltage-gated channels in the central nervous system (CNS). By binding to this subunit, it reduces the influx of calcium ions into the presynaptic nerve terminals, which reduces the release of several neurotransmitters, including glutamate, substance P, and norepinephrine. This inhibition of neurotransmitter release is thought to be responsible for pregabalin’s anxiolytic, anticonvulsant, and analgesic effects. Pregabalin has a rapid onset of action, with peak effects seen within an hour of administration, and it has a half-life of approximately 6 hours.  

Pharmacokinetics: 

Absorption 

pregabalin is well absorbed after oral administration, with peak plasma concentrations occurring within 1.5 hours. Food has no significant effect on the extent of absorption, but it slightly delays the time to peak concentration. 

Distribution 

Pregabalin has a small volume of distribution (0.56 L/kg) and is extensively bound to plasma proteins (≤ 98%). 

Metabolism 

pregabalin undergoes negligible metabolism in humans, with the majority excreted unchanged in the urine. 

Elimination and excretion 

pregabalin is primarily eliminated by kidneys as an unchanged drug, with an elimination half-life of approximately 6 hours. 

Adminstartion

Administration: 

pregabalin is administered orally as capsules or oral solution, with or without food. The frequency and dosage of administration depend on the condition that is being treated and the patient’s response to the medication. It is important to follow the doctor’s instructions for dosing and administration. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: pregabalin 

Pronounced: [ pre-GAB-a-lin ] 

Why do we use pregabalin? 

pregabalin is a medication that is primarily used to treat neuropathic pain, seizures, and anxiety disorders. It is approved by the US FDA for the following conditions: 

• Neuropathic pain with postherpetic neuralgia, diabetic peripheral neuropathy, 
• and spinal cord injury 
• Fibromyalgia 
• Partial onset seizures in adults 
• Generalized anxiety disorder (GAD) 

pregabalin is also sometimes used off-label to treat other conditions such as restless leg syndrome, insomnia, and chronic pain conditions. However, its use for these conditions is not officially approved by the FDA.