Препарати для лікування невропатичного болю

Class/Drug	Dose*	Comments
Antiseizure drugs†
Carbamazepine	200–400 mg twice a day	Monitor CBC and liver function during treatment May decrease efficacy of oral contraceptives First-line treatment for trigeminal neuralgia
Gabapentin	300–1200 mg 3 times a day	Starting dose usually 300 mg once a day Dosing goal: 600–1200 mg 3 times a day Adjust dose in patients with renal insufficiency
Oxcarbazepine	600–1200 mg twice a day	Starting dose usually 300 mg once a day Considered as efficacious as carbamazepine for trigeminal neuralgia and useful for other paroxysmal neuropathic pain May cause hyponatremia or decrease efficacy of oral contraceptives Unlike carbamazepine, no CBC or liver function monitoring necessary
Phenytoin	300 mg once a day	Limited data; 2nd-line drug
Pregabalin	150–300 mg twice a day Starting dose usually 75 mg twice a day, increased by the same dosage weekly as necessary to a maximum of 300 mg orally twice a day	Mechanism similar to gabapentin but more stable pharmacokinetics Adjust dose in patients with renal insufficiency
Valproate	250–500 mg twice a day	Limited data, but strong support for treatment of migraine
Antidepressants
Amitriptyline	10–25 mg at bedtime (starting dose), increased weekly by the same dose to a maximum of 150 mg at bedtime	Dosing goal: About 100 mg/day (dosing for pain unlikely to be adequate for relieving depression or anxiety) Not recommended for older patients or patients with a heart disorder because it has strong anticholinergic effects May increase dose to 150 mg or sometimes higher
Desipramine or nortriptyline	10–25 mg at bedtime (starting dose), increased weekly by the same dose to maximum of 150 mg at bedtime	Better tolerated than amitriptyline; adverse effect profile better with desipramine than nortriptyline Dosing goal: About 100 mg/day (dosing for pain unlikely to be adequate for relieving depression or anxiety) Not recommended for older patients or patients with a heart disorder because it has strong anticholinergic effects May increase dose to 150 mg or sometimes higher
Duloxetine	20–60 mg once a day (starting dose) Starting at 20–30 mg once a day and increasing by the same dosage weekly to a goal of 60 mg/day; in some cases, increasing to 60 mg twice a day (especially in patients with concomitant depression or anxiety)	Better tolerated than tricyclic antidepressants Dosing goal for pain (60 mg/day) usually sufficient to treat concomitant depression or anxiety
Milnacipran	12.5 mg once a day on day 1, then increased to 12.5 mg twice a day on days 2 and 3, increased further to 25 mg twice a day on days 4 to 7, then 25 mg up to 4 times a day, not to exceed 200 mg/day	Effective for fibromyalgia; not used for neuropathic pain states
Venlafaxine	Extended-release (easiest to use): 37.5–75 mg once a day, increased to a target dose of 150–225 mg once a day	More norepinephrine reuptake inhibition at higher doses (≥ 150 mg/day); lower dosages ineffective for neuropathic pain Similar mechanism of action as duloxetine Effective for pain, depression, and anxiety at this dose
Central alpha-2 adrenergic agonists
Clonidine	0.1 mg once a day	Also can be used transdermally or intrathecally
Tizanidine	2 mg every 6–8 hours (maximum 3 doses a day), increased by 2–4 mg every 1–4 days as needed (maximum: 36 mg a day)	Less likely to cause hypotension than clonidine
Corticosteroids
Dexamethasone	0.5–4 mg 4 times a day	Used only for pain with an inflammatory component
Prednisone	5–60 mg once a day	Used only for pain with an inflammatory component
NMDA-receptor antagonists
Memantine	10–30 mg once a day	Limited evidence of efficacy
Dextromethorphan	30–120 mg 4 times a day	May have a role in neuropathic pain in patients who have developed tolerance or a lower pain threshold due to central sensitization In > 90% of whites, rapid metabolism via hepatic cytochrome P-450 2D6, reducing the therapeutic effect Metabolism of dextromethorphan blocked by quinidine Combination dextromethorphan/quinidine available for pseudobulbar affect in patients with amyotrophic lateral sclerosis
Oral sodium channel blockers
Mexiletine	150 mg once a day to 300 mg every 8 hours	Used only for neuropathic pain For patients with a significant heart disorder, cardiac evaluation recommended before the drug is started
Topical
Capsaicin 0.025–0.075% (eg, cream, lotion)	Apply 3 times a day	Some evidence of efficacy in neuropathic pain and arthritis
Capsaicin 8% patch	Up to 4 at one time†	Causes a severe sunburn-like skin reaction; oral opioids often required for up to 1 week after application of capsaicin 8% to manage the worsening cutaneous pain Meaningful pain relief for 3 months after a single application
EMLA	Apply 3 times a day, under occlusive dressing if possible	Usually considered for a trial if a lidocaine patch is ineffective; expensive
Lidocaine 5%	Daily	Available as patch
Other
Baclofen	Initially 5–10 mg 3 times a day; titrated to 60–120 mg in 3 divided doses	May act via GABA-B receptor Helpful in trigeminal neuralgia; used in other types of neuropathic pain
Pamidronate (injection)	60–90 mg/month IV	Evidence of efficacy in complex regional pain syndrome
* Route is oral unless otherwise indicated.
† Topical lidocaine 4–5% applied 1 hour before applying capsaicin can help limit irritation.
CBC = complete blood count; EMLA = eutectic mixture of local anesthetics; GABA = gamma-aminobutyric acid; NMDA = N-methyl-d-aspartate; WBCs = white blood cells.

Class/Drug

Dose*

Comments

Antiseizure drugs†

Carbamazepine

200–400 mg twice a day

Monitor CBC and liver function during treatment

May decrease efficacy of oral contraceptives

First-line treatment for trigeminal neuralgia

Gabapentin

300–1200 mg 3 times a day

Starting dose usually 300 mg once a day

Dosing goal: 600–1200 mg 3 times a day

Adjust dose in patients with renal insufficiency

Oxcarbazepine

600–1200 mg twice a day

Starting dose usually 300 mg once a day

Considered as efficacious as carbamazepine for trigeminal neuralgia and useful for other paroxysmal neuropathic pain

May cause hyponatremia or decrease efficacy of oral contraceptives

Unlike carbamazepine, no CBC or liver function monitoring necessary

Phenytoin

300 mg once a day

Limited data; 2nd-line drug

Pregabalin

150–300 mg twice a day

Starting dose usually 75 mg twice a day, increased by the same dosage weekly as necessary to a maximum of 300 mg orally twice a day

Mechanism similar to gabapentin but more stable pharmacokinetics

Adjust dose in patients with renal insufficiency

Valproate

250–500 mg twice a day

Limited data, but strong support for treatment of migraine

Antidepressants

Amitriptyline

10–25 mg at bedtime (starting dose), increased weekly by the same dose to a maximum of 150 mg at bedtime

Dosing goal: About 100 mg/day (dosing for pain unlikely to be adequate for relieving depression or anxiety)

Not recommended for older patients or patients with a heart disorder because it has strong anticholinergic effects

May increase dose to 150 mg or sometimes higher

Desipramine or nortriptyline

10–25 mg at bedtime (starting dose), increased weekly by the same dose to maximum of 150 mg at bedtime

Better tolerated than amitriptyline; adverse effect profile better with desipramine than nortriptyline

Dosing goal: About 100 mg/day (dosing for pain unlikely to be adequate for relieving depression or anxiety)

Not recommended for older patients or patients with a heart disorder because it has strong anticholinergic effects

May increase dose to 150 mg or sometimes higher

Duloxetine

20–60 mg once a day (starting dose)

Starting at 20–30 mg once a day and increasing by the same dosage weekly to a goal of 60 mg/day; in some cases, increasing to 60 mg twice a day (especially in patients with concomitant depression or anxiety)

Better tolerated than tricyclic antidepressants

Dosing goal for pain (60 mg/day) usually sufficient to treat concomitant depression or anxiety

Milnacipran

12.5 mg once a day on day 1, then increased to 12.5 mg twice a day on days 2 and 3, increased further to 25 mg twice a day on days 4 to 7, then 25 mg up to 4 times a day, not to exceed 200 mg/day

Effective for fibromyalgia; not used for neuropathic pain states

Venlafaxine

Extended-release (easiest to use): 37.5–75 mg once a day, increased to a target dose of 150–225 mg once a day

More norepinephrine reuptake inhibition at higher doses (≥ 150 mg/day); lower dosages ineffective for neuropathic pain

Similar mechanism of action as duloxetine

Effective for pain, depression, and anxiety at this dose

Central alpha-2 adrenergic agonists

Clonidine

0.1 mg once a day

Also can be used transdermally or intrathecally

Tizanidine

2 mg every 6–8 hours (maximum 3 doses a day), increased by 2–4 mg every 1–4 days as needed (maximum: 36 mg a day)

Less likely to cause hypotension than clonidine

Corticosteroids

Dexamethasone

0.5–4 mg 4 times a day

Used only for pain with an inflammatory component

Prednisone

5–60 mg once a day

Used only for pain with an inflammatory component

NMDA-receptor antagonists

Memantine

10–30 mg once a day

Limited evidence of efficacy

Dextromethorphan

30–120 mg 4 times a day

May have a role in neuropathic pain in patients who have developed tolerance or a lower pain threshold due to central sensitization

In > 90% of whites, rapid metabolism via hepatic cytochrome P-450 2D6, reducing the therapeutic effect

Metabolism of dextromethorphan blocked by quinidine

Combination dextromethorphan/quinidine available for pseudobulbar affect in patients with amyotrophic lateral sclerosis

Oral sodium channel blockers

Mexiletine

150 mg once a day to 300 mg every 8 hours

Used only for neuropathic pain

For patients with a significant heart disorder, cardiac evaluation recommended before the drug is started

Topical

Capsaicin 0.025–0.075% (eg, cream, lotion)

Apply 3 times a day

Some evidence of efficacy in neuropathic pain and arthritis

Capsaicin 8% patch

Up to 4 at one time†

Causes a severe sunburn-like skin reaction; oral opioids often required for up to 1 week after application of capsaicin 8% to manage the worsening cutaneous pain

Meaningful pain relief for 3 months after a single application

EMLA

Apply 3 times a day, under occlusive dressing if possible

Usually considered for a trial if a lidocaine patch is ineffective; expensive

Lidocaine 5%

Daily

Available as patch

Other

Baclofen

Initially 5–10 mg 3 times a day; titrated to 60–120 mg in 3 divided doses

May act via GABA-B receptor

Helpful in trigeminal neuralgia; used in other types of neuropathic pain

Pamidronate (injection)

60–90 mg/month IV

Evidence of efficacy in complex regional pain syndrome

* Route is oral unless otherwise indicated.

† Topical lidocaine 4–5% applied 1 hour before applying capsaicin can help limit irritation.

CBC = complete blood count; EMLA = eutectic mixture of local anesthetics; GABA = gamma-aminobutyric acid; NMDA = N-methyl-d-aspartate; WBCs = white blood cells.

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