Pregabalin
(S)-3-(Aminomethyl)-5-methylhexanoic acid
Also known as: Lyrica · CI-1008 · PD-144723 · Alzain · Axalid · pregabalina · prégabaline · pregabalinum
Reviewed by the VetSheet Veterinary TeamUpdated Apr 5, 2026Evidence-based veterinary reference
Audited v13 dosing evidence
Structured calculator evidenceOrthostatic tremor (extra-label)
Verified clinician required
- q8-12h
NA
Governing clinical context (3)
- ■ This medicine may be given with or without food. If your animal vomits or acts sick after getting it on an empty stomach, try giving the medicine with food or a small treat to see if this helps. If vomiting continues, contact your veterinarian.
- ■ When it is used for seizure control, do not suddenly stop giving this medicine.
- Store capsules and oral solution at room temperature (25°C [77°F]); excursions permitted between 15°C to 30°C (59°F-86°F).
Doses are a clinical reference for licensed veterinary professionals. Always confirm against the current label and the individual patient.
Overview
Pregabalin is a structural analog of GABA, similar to gabapentin, used primarily as an anticonvulsant and neuropathic pain analgesic in veterinary medicine.
- Key Uses: Adjunctive therapy for refractory or complex partial seizures, and management of chronic/neuropathic pain.
- Clinical Pearl: It is considered 3-10 times more potent than gabapentin, allowing for lower dosing volumes, which can be advantageous in small patients.
- Safety Profile: Generally well-tolerated, though sedation and ataxia are the most common dose-dependent side effects. Currently, there is limited but growing information regarding its safety and efficacy in dogs and cats.
Mechanism of action
Pregabalin is a structural analog of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA). Despite its structure, it does not bind directly to GABA receptors.
- Binds with high affinity to the alpha-2-delta (α2δ) subunit of voltage-gated calcium channels (CaV) in the central nervous system.
- Binding → Decreased calcium influx at nerve terminals → Inhibition of the release of excitatory neurotransmitters (e.g., glutamate, substance P, norepinephrine).
- This reduction in excitatory neurotransmission produces its analgesic, anticonvulsant, and anxiolytic effects.
Safety & warnings
Contraindications
- Hypersensitivity to pregabalin
- Pregnant animals (toxicity demonstrated in experimental studies)
- Abrupt discontinuation
Adverse effects
- Sedation
- Ataxia
- Somnolence
- Dizziness
- Difficulty with concentration/attention/memory
- Blurred vision
- Dry mouth
- Peripheral edema
- Constipation
- Weight gain
- Syncope
- Congestive heart failure
- Renal failure (reversible)
- Rhabdomyolysis
- Hypersensitivity reactions (angioedema, rash, blisters, wheezing)
- Decreased platelet production
- Increased creatine kinase
- Mild increases in hepatic enzyme activities (with prolonged therapy)
Precautions
Use with caution in patients with renal insufficiency; dosage adjustment should be considered (in humans, adjusted based on creatinine clearance). Use with caution in patients with heart failure. Abrupt discontinuation may lead to increased seizure frequency, diarrhea, headache, insomnia, or nausea. Weigh potential risks versus benefits in pregnant or nursing animals (FDA Category C in humans; very high dosages have caused skeletal malformations in rats and rabbits).
Drug interactions
In humans, coadministration may increase risks of edema and hives.
May cause additive CNS depression.
In humans, cited as possibly reducing anticonvulsant effectiveness, though substantive evidence is weak.
Monitoring
- Efficacy (seizure frequency, pain scores)
- Adverse effects (sedation, ataxia)
- Seizure frequency and severity
- Renal function (BUN, creatinine, USG)
- Hepatic enzyme activities (during prolonged therapy)
Pharmacokinetics
Half-life
Absorption
In humans, oral bioavailability is about 90%. Presence of food can delay the rate, but not the amount absorbed; can be administered regardless of feeding status.
Distribution
Not bound to plasma proteins. Apparent volume of distribution is about 500 mL/kg.
Metabolism
Hepatic metabolism is negligible and it does not appear to affect hepatic enzymes.
Elimination
Almost exclusively cleared unchanged by renal routes. Renal clearance of 67-81 mL/minute in young, healthy human subjects.
Overdose
There is limited experience with overdoses of pregabalin in veterinary medicine. One human ingested 8 grams without significant effect. There is no specific antidote for overdose. Standard decontamination protocols can be employed if indicated. Contact an animal poison center for more information.
Available products
Formulations
- Capsules
- 75 mg capsule
- 100 mg capsule
- 150 mg capsule
- 200 mg capsule
- 225 mg capsule
- 300 mg capsule
- 20 mg/ml oral solution
Human-labeled
- Pregabalin Oral Capsules: 25 mg, 50 mg, 75 mg, 100 mg, 150 mg, 200 mg, 225 mg, & 300 mg; Lyrica® (Pfizer); (Rx; C-V controlled substance)
- Pregabalin Oral Solution: 20 mg/mL; Lyrica® (Pfizer); (Rx; C-V controlled substance)
- Alzain capsules (various strengths)
- Axalid capsules (various strengths)
- Lyrica capsules (25 mg to 300 mg)
- Lyrica 20 mg/ml oral solution
Regulatory status
POM CD SCHEDULE 3
POM CD SCHEDULE 3
No regulatory data for: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Storage & stability
Store capsules and oral solution at room temperature, 25°C (77°F); excursions permitted between 15-30°C (59-86°F). Use the oral solution within the first 45 days after opening the bottle.
Client information
- What to Expect: The most common side effects seen in animals are sleepiness (sedation) and sometimes difficulty walking (ataxia). If these are severe or persist, contact your veterinarian.
- Important Warnings:
Do not stop abruptly! Suddenly stopping pregabalin without your veterinarian's approval may cause increased adverse effects and can trigger severe seizures in epileptic patients. Always taper the dose under veterinary guidance.
- Allergic Reactions: Although rare, if you notice a rash, hives, facial swelling, wheezing, or collapse, contact your veterinarian immediately.
- Administration: Can be given with or without food. If using the liquid form, discard any unused portion 45 days after opening.
VetSheet drug reference is intended for licensed veterinary professionals as a clinical decision-support aid, not a substitute for professional judgement or the manufacturer’s current label.