Buprenorphine ER injection

SUBLOCADE

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Pronunciation: byoo-pre-NOR-feen (SUB-loe-kayd)

Buprenorphine ER injection ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Buprenorphine ER injection ballicule

Buprenorphine ER injection SUBLOCADE mascot mnemonic cartoon — Visual mnemonic: Buprenorphine ER injection mascot
**“Sub blockade”**
SUBcutaneous SUButex

What it isA monthly SC depot of partial mu-opioid agonist and kappa antagonist; maintenance treatment of opioid use disorder.

Why this oneIts apparent terminal half-life 43-60 days creates a longer depot tail than BRIXADI monthly.

What limits itSubcutaneous administration only: intravenous injection can be catastrophic. REMS (IV self-injection risk); benzodiazepines and other depressants worsen respiratory risk.

Buprenorphine ER injection molecular structure (skeletal formula) — Molecular structure: Buprenorphine ER injection

FDA-approved for

opioid use disorder (moderate-severe) (2017)

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Risk of serious harm or death with intravenous administration — forms a solid mass on contact with body fluids (occlusion, local tissue damage, thromboembolic events including pulmonary emboli). Available only through the restricted SUBLOCADE REMS Program.

FDA dosing	Population	Start	Target	Max
Moderate to severe opioid use disorder (in patients on transmucosal buprenorphine)	Adults	Two initial 300 mg SC doses (second as early as 1 week after first)	100 mg SC monthly maintenance	300 mg monthly (may be considered)

Renal Undefined (not studied; clinical studies excluded renal impairment)

Hepatic Moderate to severe hepatic impairment: not candidates for SUBLOCADE (mild: no data indicating adjustment)

Administer maintenance doses at least 26 days apart; a single 300 mg dose may cover a two-month interval when needed

Instructions

Subcutaneous injection only (abdomen, thigh, buttock, or back of upper arm) by a healthcare provider — never IV/IM/intradermal
Patients not on buprenorphine should receive an initial dose (e.g., 4 mg) of transmucosal buprenorphine and be observed 1 hour before first injection
Rotate injection sites; monitor after injection for worsening withdrawal or sedation
Strongly consider prescribing naloxone
Monitor liver function before and during treatment

Available strengths

inj 100 mg/0.5 mL
inj 300 mg/1.5 mL

Cautions

Addiction, abuse, and misuse
Life-threatening respiratory and CNS depression (esp. with benzodiazepines/other CNS depressants)
Serious injection site reactions (increased with inadvertent IM/intradermal)
Neonatal opioid withdrawal syndrome
Adrenal insufficiency
Opioid withdrawal with abrupt discontinuation
Hepatitis/hepatic events
Hypersensitivity reactions
Precipitation of withdrawal in patients on full agonist opioids
Not appropriate for opioid-naive patients
QTc prolongation
Orthostatic hypotension

Adverse reactions

Constipation
Nausea
Vomiting
Headache
Injection site pain/pruritus
Fatigue
Elevated hepatic enzymes
Sedation/somnolence

Pregnancy Limited data do not indicate increased malformation risk; prolonged use can cause neonatal opioid withdrawal syndrome

Lactation Buprenorphine and norbuprenorphine present at low levels in human milk; exercise caution; consider benefits vs risk

Cost

Buprenorphine ER injection (SUBLOCADE)

Strength		#/mo	generic $/unit	CostPlus
100 mg/0.5 mL	inj	per unit		not offered
300 mg/1.5 mL	inj	per unit		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Buprenorphine ER injection is administered under clinical supervision and dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Other forms: Buprenorphine (SUBUTEX) · Buprenorphine buccal film (BELBUCA) · Buprenorphine SC (weekly/monthly) (BRIXADI) · Buprenorphine patch (BUTRANS)

Available combined with: Buprenorphine/ naloxone (SUBOXONE)

⚠ BOXED WARNINGS

Addiction, abuse and misuse
Life-threatening respiratory depression
Risk from concomitant use with benzodiazepines

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger3 / 4

Weight-gain liability0 / 4

Sedation liability2 / 4

QT / Torsades1 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilityRespiratory depression and dependence remain possible, especially with benzodiazepines, alcohol or other sedatives.

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Memory aids: interaction avatars

CYP3A4 substrate

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