PERPHENAZINE tablet, film coated

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

PERPHENAZINE (UNII: FTA7XXY4EZ) (PERPHENAZINE - UNII:FTA7XXY4EZ)

Available from:

NCS HealthCare of KY, Inc dba Vangard Labs

INN (International Name):

PERPHENAZINE

Composition:

PERPHENAZINE 2 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Perphenazine is indicated for use in the treatment of schizophrenia and for the control of severe nausea and vomiting in adults. Perphenazine has not been shown effective for the management of behavioral complications in patients with mental retardation. Perphenazine products are contraindicated in comatose or greatly obtunded patients and in patients receiving large doses of central nervous system depressants (barbiturates, alcohol, narcotics, analgesics, or antihistamines); in the presence of existing blood dyscrasias, bone marrow depression, or liver damage; and in patients who have shown hypersensitivity to perphenazine tablets, their components, or related compounds. Perphenazine products are also contraindicated in patients with suspected or established subcortical brain damage, with or without hypothalamic damage, since a hyperthermic reaction with temperatures in excess of 104°F may occur in such patients, sometimes not until 14 to 16 hours after drug administration. Total body ice-packing is recommen

Product summary:

Perphenazine tablets, USP are round, unscored, film-coated white tablets available as: 2 mg: debossed GG 18 on one side and plain on the reverse side, supplied as: NDC 0615-3584-39 blisterpacks of 30 tablets 4 mg: debossed GG 107 on one side and plain on the reverse side, supplied as: NDC 0615-3585-39 blisterpacks of 30 tablets 8 mg: debossed GG 108 on one side and plain on the reverse side, supplied as: NDC 0615-4511-39 blisterpacks of 30 tablets Store at 20°-25°C (68°-77°F) (see USP Controlled Room Temperature). Dispense in a tight, light-resistant container.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

PERPHENAZINE- PERPHENAZINE TABLET, FILM COATED
NCS HEALTHCARE OF KY, INC DBA VANGARD LABS
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PERPHENAZINE TABLETS, USP
DESCRIPTION
Perphenazine
(4-[3-(2-chlorophenothiazin-10-yl)propyl]-1-piperazineethanol), a
piperazinyl
phenothiazine, having the chemical formula, C
H CIN OS. It is available as oral tablets containing 2
mg, 4 mg, 8 mg, and 16 mg of perphenazine.
Inactive ingredients: lactose (monohydrate), hydroxypropyl cellulose,
hydroxypropyl methylcellulose,
magnesium stearate, microcrystalline cellulose, polyethylene glycol,
starch (corn), titanium dioxide, and
polysorbate 80. Its structural formula is:
ACTIONS
Perphenazine has actions at all levels of the central nervous system,
particularly the hypothalamus.
However, the site and mechanism of action of therapeutic effect are
not known.
CLINICAL PHARMACOLOGY
PHARMACOKINETICS
Following oral administration of perphenazine tablets, mean peak
plasma perphenazine concentrations
were observed between 1 to 3 hours. The plasma elimination half-life
of perphenazine was independent
of dose and ranged between 9 and 12 hours. In a study in which normal
volunteers (n=12) received
perphenazine 4 mg q8h for 5 days, steady-state concentrations of
perphenazine were reached within 72
hours. Mean (%CV) C
and C
values for perphenazine and 7-hydroxyperphenazine at steady-state
are listed below:
PARAMETER
PERPHENAZINE
7-HYDROXYPERPHENAZINE
C
(pg/mL)
984 (43)
509 (25)
C
(pg/mL)
442 (76)
350 (56)
Peak 7-hydroxyperphenazine concentrations were observed between 2 to 4
hours with a terminal phase
half-life ranging between 9.9 to 18.8 hours. Perphenazine is
extensively metabolized in the liver to a
number of metabolites by sulfoxidation, hydroxylation, dealkylation,
and glucuronidation. The
pharmacokinetics of perphenazine covary with the hydroxylation of
debrisoquine which is mediated by
21
26
3
max
min
max
min
cytochrome P450 2D6 (CYP 2D6) and thus is subject to genetic
polymorphism – i.e., 7% to 10% of
Caucasians and a low percentage of Asians have little or no activity
a