Drug information of Pregabalin

Pregabalin


Pregabalin is an anti-epileptic drug, also called an anticonvulsant. It works by slowing down impulses in the brain that cause seizures. Pregabalin also affects chemicals in the brain that send pain signals across the nervous system.
Pregabalin is used to control seizures and to treat fibromyalgia. It is also used to treat pain caused by nerve damage in people with diabetes (diabetic neuropathy), herpes zoster (post-herpetic neuralgia), or spinal cord injury.

Mechanism of effect

Mechanism of pregabalin's antinociceptive and antiseizure effects is unknown. Effects may be related to high affinity binding to alpha-2 delta site (an auxiliary subunit of voltage-gated calcium channels) in CNS tissue

Pharmacodynamic

Pregabalin is a new anticonvulsant drug indicated as an add on therapy for partial onset seizures and for certain types of neuropathic pain. It was designed as a more potent successor to a related drug, gabapentin.

Pharmacokinetics

Well absorbed after oral administration; bioavailability is more than 90%. T max occurs within 1.5 h. Steady state was achieved within 24 to 48 h.
Vd is approximately 0.5 L/kg. Substrate for system L transporter, which is responsible for the transport of large amino acids across the blood brain barrier Negligible metabolism.
The half-life is 6.3 h. Largely eliminated by renal excretion; 90% excreted unchanged in urine. Mean renal Cl is approximately 67 to 80.9 mL/min.

Dosage

Partial-Onset Seizures :
Adults PO 75 mg twice daily or 50 mg 3 times daily initially, increased to 150 to 600 mg/day divided 2 or 3 times daily based on efficacy and tolerability (max, 600 mg/day).
Postherpetic Neuralgia :
Adults PO 75 mg twice daily or 50 mg 3 times daily initially, increased to 150 mg twice daily or 100 mg 3 times daily within 1 wk based on efficacy and tolerability.
If relief is insufficient after 2 to 4 wk, may increase up to 300 mg twice daily or 200 mg 3 times daily.

Alerts

1-Monitor for emergence or worsening of depression, suicidal thoughts or behavior, or any unusual changes in behavior
2-Monitor for weight gain and/or fluid retention, possibly exacerbating or leading to heart failure.
3-Carefully evaluate patients for a history of drug abuse and observe them for signs of pregabalin misuse or abuse (eg, development of tolerance, dose escalation, drug-seeking behavior).

Points of recommendation

• May be given with or without food.
• When discontinuing, taper gradually over a minimum of 1 wk.
• May cause dizziness and drowsiness, which may impair the ability to preform tasks such as driving or operating machinery.

Pregnancy level

C


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