Long Acting Injectables Working

Long-Acting
Injectables
General
Dosing
Pharmacokinetics (ADME)
General
Information
Abilify
Maintena
(aripiprazole )
Initial:
400mg IM
Median half-life: 29.9 days for 300mg IM injection; 46.5 days for 400mg IM injection
Time to Steady-State: After 4 injections (approx 4 months)
Peak Plasma Concentration: Between 5-7 days
Onset of Action: 7-21 days
Major Metabolism: CYP 2D6 and 3A4; active metabolite dehydroaripiprazole
How supplied: 300,

400mg vials lyophilized
powder for reconstitution
with injection kit with
syringe, safety needle
and SWI
Q 4 weeks
Tolerability:
Establish PO tolerability
of aripirazole before
initiating extendedrelease IM injection.
Overlap:
Overlap with PO
aripiprazole or other
antipsychotic for 14 days
after the initial IM
injection per PI
Maintenance:
400mg IM; if side effects
present, can use 300mg
IM. No dose equivalents.
Frequency/Administrat
ion:
IM by deep gluteal or
deltoid injection Q 4
Fleishhacker, W.W.
et al. Pharmacokinetic
of Once-Monthly Aripiprazole Intramuscular Depot in Adult Patients with
weeks
(26 days) Study
th
Schizophrenia. [Poster] Presented at: The 164 Annual Meeting of the American Psychiatric Association. May 14-18, 2011; Honolulu,
HI.
Maximum:
400mg IM every 4
weeks (26 days)
Missed Doses:
2nd or 3rd dose missed:
>4 weeks but <5 weeks
administer next dose
ASAP. If >5 weeks since
last dose administer
PO Abilify for 14 days
with next injection
4th or subsequent doses
missed: >4 weeks but
<6 weeks since last
dose administer next
dose ASAP. If >6 weeks
since last dose
administer PO Abilify for
14 days with next
injection.
***Last updated 7/20/16 by Kylie Carpenter (P4 student)/ Karen Johnston PharmD
Key: PIPackage Insert; SSSteady State; POBy Mouth; IMIntramuscular; IVIntravascular; CRHCentral Regional Hospital
Needle: Gluteal 1.5-inch

22G safety needle;
Gluteal 2-inch 21G
safety needle for obese
patients.
Deltoid: 23G 1-inch
needle; 22G 1.5-inch
needle for obese
patients
Max volume/injection:
2 mL/injection
Refrigeration: No
refrigeration required
Reconstitution: Must
be reconstituted
Injection Site: Deltoid
or Gluteal
Abilify
Aristada
(Aripiprazole
Lauroxil)
Q4 weeks
or
Q6 weeks
(882mg only)
*Not on
formulary at
CRH
Initial:
Oral 10mg Qd =441mg
Qmonth.
Oral 15mg Qd = 662mg
Qmonth.
Oral 20mg or higher Qd =
882mg Qmonth.
Continue regimen and adjust
as needed for
symptom/adverse effects.
Half-life: 29-35 days

Time to Steady State: By week 12 after injection
Peak Plasma Concentration: about 41 days after administration
Onset of Action: absorption estimated to be 36 days and lag time from IM depot to appearance in central
compartment is about 5.4 days (41.4 days total)
Major metabolism: CYP3A4, CYP2D6
Bioavailability: 58% in comparison to oral aripiprazole administration
Tolerability:
Establish tolerability with oral
aripiprazole prior to initiating
Aristada
How supplied: 441mg,

662mg, or 882mg vial/kit
with syringe containing
Aristada aqueous
suspension
Needle: Gluteal, 20G
1.5-inch or 2-inch;
Deltoid (441mg only),
21G 1-inch or 20G 1.5inch
Max Vol/Injection:
1.6mL for 441mg
2.4mL for 662mg
3.2mL for 882mg
Overlap:
PI states that in conjunction
with the first IM injection,
administer treatment with oral
aripirazole for 21 consecutive
days
Refrigeration: all
materials should be
stored at room
temperature
be reconstituted
Frequency/Administration:
IM by gluteal (441, 662, and
882mg) or deltoid (441mg
only) injection
Q 4 weeks (441, 662, or
882mg) or Q6 weeks for
882mg only

or Gluteal
Maximum:
882mg IM every 4 or 6 weeks
Missed dose adjustment: 6
weeks or less at 441 or 8
weeks or less for 662 or
882mg there is no need to
supplement. If 6-7 weeks
missed or 441mg or 8-12
weeks missed of 662 or 882,
supplement with 7 days or
oral. Supplement with 21
days oral if longer periods
missed.
Abilify Aristada [package insert]. Waltham, MA: Alkermes, Inc.; 2015.
Risperdal
CONSTA
(risperidone)
Q 2 weeks
Initial:
25mg IM per PI
No oral conversion
equivalents.
Median half-life: 3-6 days; complete elimination 7-8 weeks post last injection
Time to Steady State: After 4 injections (approx 2 months)
Peak Plasma Concentration: between 4-6 weeks
Onset of Action: release from microspheres begins~ 21 days post initial injection
Major metabolism: 2D6, active metabolite 9-OH-risperidone
Overlap:
Oral antipsychotic
supplementation is
recommended beginning
with the first injection
and should be continued
for the first 3 weeks of
IM treatment per
Package Insert
*Drug does not begin to
release from
microsphere emulsion
diluent vehicle until the
third week after
injection.
*Many clinicians will
overlap with PO
risperidone using a
judicious taper until
steady state
concentrations are
obtained
(~ 4 injections).
Maintenance:
12.5-50mg IM; dose
Lasser
R. Poster presented at Annual Meeting of APNA; October 4-7, 2002; Dallas, TX
adjustments
recommended no more
often than Q 4 weeks
Frequency/Administrat
ion:
IM by gluteal or deltoid
injection Q 2 weeks
Maximum:
50mg IM every 2 weeks
*Hepatic Adjustment
Required:
Max dose of 25mg in
hepatic impairment.
How supplied: 12.5, 25,

37.5, 50mg vial/kit with
syringe containing
diluent
(microsphere emulsion)
Needle: Gluteal, 20G
TW 2-inch; Deltoid, 21G
UTW 1-inch
Max Vol/Injection: 2
mL/injection
Refrigeration: Dose
pack must be
refrigerated
be reconstituted
or Gluteal
INVEGA
Sustenna
(paliperidone)
Q 4 weeks
Initial:
Day 1: 234mg (deltoid)
Day 8: 156mg (deltoid)
Conversion from PO:
*(tablets are non-formulary)
Pal PO 12mg/day=
Sustenna 234mg/month
Pal PO 6mg/day= Sustenna
117mg/month
Pal PO 3mg/day= Sustenna
39-78mg/month
Median half-life: 25-49 days; release can last as long as 126 days
Time to Steady State: 8 to 9 months (SS concentrations approached after 2nd injection / day 8)
Peak Plasma Concentration: 13 days
Onset of Action: Efficacy onset of 8 to 22 days
Major metabolism: no significant P450 metabolism; 59% drug excreted unchanged into urine
Needle: Deltoid: 23 G 1inch for <90kg and the

22 G 1 inch for >90kg;
Gluteal: 22 G 1 inch
Max Vol/Injection:
prefilled syringe
Conversion from
Risperdal Consta:
* Per Canadian PI
Consta (Q2 wks) to
Sustenna (Q4 wks)
Conversion:
12.5mg= 39mg 25mg=78mg
37.5mg=117mg
50mg=156mg
Tolerability: Confirm prior
tolerability with PO
paliperidone or PO/IM
risperidone prior to starting
Sustenna
How supplied: 39, 78,

117, 156, 234mg kit with
prefilled syringe, 2 safety
needles
Refrigeration: No
Reconstitution: No
reconstitution required
Cleton A, et al. Presented at
ASCPT; Orlando, FL; April 2-5,
2008.
Overlap: No PO
supplementation
recommended per PI
*Clinicians should be aware
of time to SS data
Maintenance:
Recommended: 117mg
monthly
Range: 39-234mg monthly
Frequency
Day 1 and 8 loading doses
must be deltoid.
Monthly Maintenance: IM by
gluteal or deltoid injection Q
4 weeks
Maximum:
234 IM every 4 weeks
*Renal adjustment
required: Not
recommended for use if
CrCL<50mL/min.
CrCL 50 - 79mL/min: 156mg
IM day 1, 117mg on Day 8,
78mg IM Q Month thereafter
Injection Site:
Day 1 and 8 LD must be
deltoid.
Maintenance dose may
be Deltoid or Gluteal
Invega Trinza
(Paliperidone
palmitate)
Q12 weeks
*Nonformulary at
CRH
Initial:
Initiate Invega Trinza
when next Invega
Sustenna injection is due
based on the previous
Sustenna dose.
Median half-life: 84-95 days in deltoid administration and 118-139 days in gluteal administration
Time to Steady State: Clinical opinion: Patient should already be at steady state since they must have 4
months of Sustenna injections prior to administration of Trinza.
Peak Plasma Concentration: 30-33 days
Onset of Action: release of the drug starts as early as day 1 and lasts as long as 18 months
Major metabolism: CYP3A4, CYP2D6, and P-gp
Sustenna conversion:
Sustenna 78mg= Trinza
273mg
410mg
546mg
819mg
Needle:
Deltoid: if <90kg use 1inch 22G thin wall
needle. If 90kg or more
use 1.5-inch 22G thin
wall needle
Gluteal: regardless of
weight use 1.5-inch 22G
thin wall needle
Tolerability: Must treat

with Invega Sustenna 1month injections for at
least 4 months prior to
use
Max Vol/Injection:
175mg (0.875mL),
263mg (1.315mL),
350mg (1.75mL),
525mg (2.625mL)
Overlap:
Per PI, no oral
supplementation needed.
*Clinicians should be
aware of time to SS data
Refrigeration: Store at
room temperature
be reconstituted and
inject within 5 minutes or
reconstitution
Frequency/Administrati
on:
IM by gluteal or deltoid
injection Q 3 months

or Gluteal
Maximum:
819mg IM every 3 months
*Renal adjustment
required:
Do not use if
CrCl<50mL/min
How supplied: 273mg,

410mg, 546mg, or
819mg vial/kit with
syringe containing
aqueous suspension
with needles
INVEGA TRINZA (paliperidone palmitate) | Pharmacokinetics. (n.d.). Retrieved July 20, 2016, from
https://www.invegatrinzahcp.com/pharmacokinetics.html
Zyprexa
Relprevv
(olanzapine)
Q 2 weeks for
150-300mg
Q 4 weeks for
405mg
Initial:
For first 8 weeks:
10mg PO = 210mg/2wks
OR 405mg/4 wks.
Median half-life: 30 days; exposure may persist for months after last injection
Time to Steady State: Approximately 3 months after multiple injections
Peak Plasma Concentration: 4 days
Onset of Action: Efficacy onset of 3 to 7 days
Major metabolism: glucuronidation and CYP 1A2 (major) and 2D6 (minor)
(PO= total daily dose)
Tolerability:
Confirm PO tolerability
to olanzapine prior to
initiating RELPREVV
*Black Box Warning:

Post-injection
sedation/delirium
syndrome (requires 3hour monitoring. In
outpatient settings,
patients must be
escorted home from the
facility)
*REMS program
How supplied: 210,
300mg, 405mg vial/kit
and 3ml vial diluent, 3
needles
Overlap:
No oral supplementation
recommended per PI
Needle: Gluteal ONLY:

One 19G 1 inch preattached needle; two
19G 1 inch needles.
Special Instructions:
Do not inject
intravenously or
subcutaneously.
After insertion of the
needle into the muscle,
aspirate for several
seconds to ensure that
no blood appears. Do
not massage the
injection site
Maintenance:
10mg po = 150mg/2 wks
OR 300mg/4 wks
OR 405mg/4 wks
Maximum:
300mg/14 days or
617mg/28 days
Max Vol/Injection: 2.7

mL/injection (405mg
dose)
Refrigeration: No
be reconstituted
Injection Site: Gluteal
Kurtz D, et al. From poster presented at SOBP,

Washington, DC. 2008.
HALDOL
Decanoate
(haloperidol)
Q 4 weeks
Initial:
Method 1: 10-15X PO
total daily dose
*Maximum of 100mg on
day 1 for nave pts, with
balance given in 3-7 days
Median half-life: 21 days; reports of measurable drug up to 6-months post last injection
Time to Steady State: After 3rd or 4th dose (approx 3 months)
Peak Plasma Concentration: ~ 6 days (range 3-9 days)
Onset of Action: Peak medication levels seen between 3-7 days after administration
Major metabolism: Oxidative dealkylation
Needle: 21G
recommended
PO overlap for 1st month

*Most clinicians overlap
with judicious taper until
SS achieved (~ 2-3 inj.)
Max Vol/Injection: 3
mL/injection
Method 2: 20X PO daily

dose (divided in
consecutive injections of
100mg to 200mg Q3-7
days until total amount
given)
Refrigeration: No
Reconstitution: No
Decrease decanoate dose

by 25% with 2nd and 3rd
injections until
maintenance dose
achieved.
No PO overlap
recommended
How supplied:
50mg/mL, 100mg/mL as
ampules or multiple
dose vials; must be
drawn up in a syringe
(use filter with ampules)

or Gluteal
Chang, W. et al. Schiz Res 1993; 9: 35-39
Method 3 Loading:
*several strategies have
been investigated
Sample Strategy
100mg Q week for 4
weeks, then 100mg Q 2
weeks for 4 weeks, then
100mg Q 4 weeks
SS was reached during
4th week with this
strategy in one small
study
Maintenance:
Range:10-15X previous
total daily PO dose
Maximum:
450mg IM/month
Prolixin
Decanoate
(fluphenazine)
Q 2 weeks,
but intervals
must be
individualized
Initial:
Method 1 (stable patients):
1.2X PO total daily dose
Median half-life: 14-16 days; measurable levels up to 24 weeks post last injection
PO overlap for 1st week

*Most clinicians overlap with
judicious taper until SS
achieved (~3-5 inj.)
Peak Plasma Concentration: ~1-2 days after injection (due to "dose dumping" phenomenon)
Method 2 (acutely ill): 1.6 X

PO total daily dose
Major metabolism: Aromatic hydroxylation, S- and N- desalkylation, glucoronidation
Time to Steady State: Approx 4-6 weeks (3-5 injections)
Onset of Action: Efficacy onset 48-96 hours; possibly earlier onset ~24 hours due to unesterified
fluphenazine in decanoate preparation
PO overlap for 1st week

*most clinicians overlap with
judicuous taper until steady
state (~3-5 inj.)
How supplied:
25mg/mL in 5 mL
multiple dose vial; must
be drawn up into a
syringe
Needle: at least 21G
Max Vol/Injection:
Provided as 25mg/mL
(CRH max= 50mg=
2mL)
Refrigeration: No
Reconstitution: No
Usual initial dose:

Range of 12.5-50mg IM
Injection Site: Gluteal

only
Frequency/
Administration:
Method 1:
Initial and Maintenance:
IM/SQ* Q2-3weeks
Method 2:
Initial: IM/SQ* Weekly
injections for first 4-6 weeks
Maintenance: IM/SQ* Q2-3
weeks
Maximum:
50mg IM Q2 weeks (CRH).
Do not exceed 100mg/dose.
*SQ administration rarely
used due to injection site
pain/abscess/nodules
Midha, K. et al. J Psychiatr Neurosci 1994; 19 (4): 254-64

Long Acting Injectables Working

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Long Acting Injectables Working

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Long-Acting

How supplied: 300,

Needle: Gluteal 1.5-inch

Half-life: 29-35 days

How supplied: 441mg,

Injection Site: Deltoid

Abilify Aristada [package insert]. Waltham, MA: Alkermes, Inc.; 2015.

How supplied: 12.5, 25,

Needle: Deltoid: 23 G 1inch for <90kg and the

How supplied: 39, 78,

Tolerability: Must treat

Injection Site: Deltoid

How supplied: 273mg,

*Black Box Warning:

Needle: Gluteal ONLY:

Max Vol/Injection: 2.7

Kurtz D, et al. From poster presented at SOBP,

PO overlap for 1st month

Method 2: 20X PO daily

Decrease decanoate dose

Injection Site: Deltoid

Chang, W. et al. Schiz Res 1993; 9: 35-39

PO overlap for 1st week

Method 2 (acutely ill): 1.6 X

Major metabolism: Aromatic hydroxylation, S- and N- desalkylation, glucoronidation

Time to Steady State: Approx 4-6 weeks (3-5 injections)

PO overlap for 1st week

Usual initial dose:

Injection Site: Gluteal

Midha, K. et al. J Psychiatr Neurosci 1994; 19 (4): 254-64

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