- March 15, 2022
- Newsletter
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Brand Name :
Lyrica, Lyrica CR
Synonyms :
pregabalin
Class :
Fibromyalgia Agents; Anticonvulsants, Other; Analgesics, Other
Brand Name :
Lyrica, Lyrica CR
Synonyms :
pregabalin
Class :
Fibromyalgia Agents; Anticonvulsants, Other; Analgesics, Other
Dosage Forms & Strengths
tablet, extended release (Schedule V)
330 mg
165 mg
82.5 mg
oral solution (Schedule V)
20mg/mL
Capsule (Schedule V)
300mg
225mg
200mg
150mg
100mg
75mg
50mg
25mg
Dosage Forms & Strengths
oral solution (Schedule V)
20mg/mL
Capsule (Schedule V)
300mg
225mg
200mg
150mg
100mg
75mg
50mg
25mg
Refer to the adult dosing regimen
hydroxyzine may enhance the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of opioid agonists
it increases the effect of CNS depressants
CNS depressants increase the effect of flunarizine
it increases the effect of CNS depressants
may increase the CNS depressant effect
may increase the adverse or toxic effect of anti-psychotic agents
may increase the adverse or toxic effect of anti-psychotic agents
may increase the adverse or toxic effect of anti-psychotic agents
may increase the adverse or toxic effect of anti-psychotic agents
may increase the adverse or toxic effect of anti-psychotic agents
CNS Depressants may enhance the CNS depressant effect of zolpidem
it increases the effect of CNS depressants
it increases the effect of CNS depressants
it increases the effect of CNS depressants
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.
Frequency defined
>10%
Lyrica
Lyrica CR
1-10%
Lyrica
Lyrica CR
<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:
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:
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 consideration: US FDA pregnancy category: Not assigned
Lactation: pregabalin is excreted into human milk
Pregnancy category:
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.
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
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:
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.