Safe Deprescribing of Gabapentinoids

Abstract

Gabapentinoids are widely used off‐label for conditions for which the balance of harms and benefits is uncertain or unfavourable. Long‐term use of gabapentinoids in mental health conditions is affected by issues such as physical dependence, addiction, tolerance and withdrawal effects. Harms include numerous cognitive, physical and emotional effects, and spiking rates of accidental overdoses (especially when used with opioids). Withdrawal effects arise due to adaptation to chronic use of gabapentinoids – often termed physical dependence, distinct from addiction. Addiction is an issue for a minority of gabapentinoid users whilst withdrawal effects and physical dependence affect a larger group of patients taking medication as prescribed. Withdrawal effects can manifest as either physical or psychological symptoms and can be mistaken for a return of an underlying condition or onset of a new physical or mental health condition. The most severe withdrawal effects are suicidality, akathisia and protracted withdrawal syndromes which can last for months or years and can sometimes be debilitating. Careful tapering can minimise these effects. After long‐term use tapering should be gradual (months or years), and adjusted to a rate that the individual can tolerate. Dose reduction should be conducted in a hyperbolic pattern (so that decrements become smaller and smaller as the total dose gets lower) to reflect the hyperbolic relationship between dose and receptor occupancy (and clinical effects), as dictated by the law of mass action. In order to facilitate gradual hyperbolic tapering sometimes formulations other than widely available tablets or capsules will be required.