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Drugs, Supplies and Delivery
Pregabalin
Pregabalin is a medication primarily used for the treatment of neuropathic pain, epilepsy, and generalized anxiety disorder (GAD). It is also approved for the management of fibromyalgia and postherpetic neuralgia. Pregabalin is known for its efficacy in reducing pain and anxiety, as well as its role as an adjunctive therapy for partial seizures. This article provides a detailed overview of pregabalin, including its mechanism of action, uses, dosage, side effects, precautions, drug interactions, and generic names, referencing authoritative sources such as the British National Formulary (BNF), Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology.
Pregabalin exerts its therapeutic effects through its action on voltage-gated calcium channels in the central nervous system. Its key mechanisms include:
- Calcium Channel Modulation:
- Pregabalin binds to the α2-δ subunit of voltage-gated calcium channels in the central nervous system.
- This binding reduces the influx of calcium into nerve terminals, leading to a decrease in the release of excitatory neurotransmitters such as glutamate, norepinephrine, and substance P.
- Reduction of Excitatory Neurotransmission:
- By decreasing the release of excitatory neurotransmitters, pregabalin reduces neuronal excitability, which contributes to its anticonvulsant, analgesic, and anxiolytic effects.
- Neuropathic Pain Relief:
- Pregabalin’s ability to modulate calcium channels and reduce neurotransmitter release makes it effective in treating neuropathic pain conditions.
- Anxiolytic Effects:
- The reduction in excitatory neurotransmission also contributes to pregabalin’s efficacy in reducing anxiety symptoms.
Pregabalin is approved for a variety of clinical conditions, including:
- Neuropathic Pain:
- Diabetic peripheral neuropathy.
- Postherpetic neuralgia.
- Spinal cord injury-related neuropathic pain.
- Epilepsy:
- Adjunctive therapy for focal (partial) seizures with or without secondary generalization in adults.
- Generalized Anxiety Disorder (GAD):
- Treatment of generalized anxiety disorder in adults.
- Fibromyalgia:
- Management of fibromyalgia in adults.
- Off-Label Uses:
- Chronic pain syndromes.
- Restless legs syndrome.
- Social anxiety disorder.
The dosage of pregabalin varies depending on the indication, patient response, and tolerability. The following dosing guidelines are based on the British National Formulary (BNF) and clinical pharmacology references:
- Neuropathic Pain:
- Adults: Start with 150 mg daily in divided doses, increasing to 300–600 mg daily based on response and tolerability.
- Epilepsy:
- Adults: Start with 150 mg daily in divided doses, increasing to 300–600 mg daily.
- Generalized Anxiety Disorder (GAD):
- Adults: Start with 150 mg daily in divided doses, increasing to 300–600 mg daily.
- Fibromyalgia:
- Adults: Start with 150 mg daily in divided doses, increasing to 300–450 mg daily.
Important Considerations:
- Pregabalin is available in oral capsules and oral solution.
- Dose adjustments may be necessary for patients with renal impairment.
- The maximum daily dose is 600 mg, divided into two or three doses.
Pregabalin is generally well-tolerated, but it is associated with a range of side effects, some of which can be serious. Common side effects include:
- Central Nervous System:
- Dizziness, drowsiness, and headache.
- Cognitive impairment and memory problems.
- Gastrointestinal:
- Dry mouth, nausea, and constipation.
- Ophthalmological:
- Blurred vision and diplopia (double vision).
- Other:
- Weight gain and peripheral edema.
Serious Side Effects:
- Angioedema: A rare but serious allergic reaction characterized by swelling of the face, lips, and throat.
- Suicidal Thoughts: Like other anticonvulsants, pregabalin may increase the risk of suicidal thoughts or behavior.
Withdrawal Symptoms: Abrupt discontinuation can lead to symptoms such as insomnia, nausea, headache, and anxiety
Pregabalin requires careful monitoring and adherence to specific precautions to ensure patient safety:
- Renal Impairment:
- Dose adjustments are necessary for patients with impaired kidney function. The dose should be reduced in patients with a creatinine clearance (CrCl) of less than 60 mL/min.
- Pregnancy and Lactation:
- Pregabalin should be used during pregnancy only if the potential benefits outweigh the risks. It is excreted in breast milk, so breastfeeding is generally not recommended.
- Elderly Patients:
- Lower doses may be required due to increased sensitivity to side effects, particularly dizziness and sedation.
- Suicidal Risk:
- Monitor for worsening depression or suicidal thoughts, particularly in patients with mood disorders.
- Withdrawal:
Pregabalin should be tapered gradually to avoid withdrawal symptoms
Pregabalin has a low potential for drug interactions due to its lack of metabolism via cytochrome P450 enzymes. However, key interactions include:
- Central Nervous System Depressants:
- Alcohol, benzodiazepines, and opioids can enhance sedation and respiratory depression.
- Thiazolidinediones:
- Pregabalin may increase the risk of peripheral edema and weight gain when used with thiazolidinediones (e.g., pioglitazone).
- Other Interactions:
- ACE inhibitors: Increased risk of angioedema.
Pregabalin is the generic name for this medication. It is marketed under various brand names, depending on the country and manufacturer. Some examples include:
- Lyrica (a well-known brand in the United States and other regions).
- Pregabalin Accord.
- Pregabalin Mylan.
- Pregalin.
