Gabapentanoids Flashcards
Indicated use of gabapentanoids
Neuropathic pain
And
Focal seizures with or without secondary generalisation
Elimination of both drugs?
PREgablin = 98% excretes in urine unchanged
GABApentin = excreted unchanged (not metabolised)
Who is at greater risk of gabapentiniod misuse?
People with history or drug and alcohol use disorder
Or if used
Via non oral routes = nasal insufflation, iv injection
Features of an overdose of gabapentanoids
Dizziness
Ataxia
Confusion
Slurred speech
Myoclonic jerks
Seizures
Renamly cleared therefore toxicity to kidneys
Treatment for p
POSIONINg
Airway = intubated and ventilate
Circulation of IV FLUID = to resuscitate
Decontamination = activated charcoal (must be present within 2 hours after time of ingested
Why dose pregablin have a higher misuse then GABApentin?
- GABApentin has saturate absorption
- PREgablin more rapidly absorbed
- PREgablin has increased binding to voltage gated calcium channels
Pregablin PK
- 98% excreted in urine unchanged
= dose adjustment needed in renal impairment - Crosses BBB = not bound to plasma proteins
Gabapentin
PK
- Saturable absorption (increasing dose = decreasing bioavailabilty)
- Mostly unbound to plasma proteins
- Excreted in urine unchanged (no metabolites
Why does Pregablin have a higher misuse potential
- Gabapentin has a saturable absorption
- Pregablin is more readily absorbed
- Pregablin has increased bidning to voltage gated calcium channels