CEVIMELINE capsule

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

CEVIMELINE HYDROCHLORIDE (UNII: P81Q6V85NP) (CEVIMELINE - UNII:K9V0CDQ56E)

Available from:

Sun Pharmaceutical Industries, Inc.

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Cevimeline hydrochloride capsules are indicated for the treatment of symptoms of dry mouth in patients with Sjögren’s Syndrome. Cevimeline is contraindicated in patients with uncontrolled asthma, known hypersensitivity to cevimeline, and when miosis is undesirable, e.g., in acute iritis and in narrow-angle (angle-closure) glaucoma.

Product summary:

Cevimeline is available as white, hard gelatin capsules containing 30 mg of cevimeline hydrochloride. Cevimeline hydrochloride capsules have a white opaque cap and a white opaque body. The capsules are imprinted with “EVOXAC” on the cap and “30 mg” on the body with a black bar above “30 mg”. It is supplied in child resistant bottles of: 100 capsules (NDC 63304-479-01). Store at 25°C (77°F); excursion permitted to 15° to 30°C (59° to 86°F). Rx only Distributed by: Sun Pharmaceutical Industries , Inc. Cranbury, NJ 08512 Revised 05/2018 Printed in U.S.A. USPI-CEV-0518-r100

Authorization status:

New Drug Application

Summary of Product characteristics

CEVIMELINE- CEVIMELINE CAPSULE
SUN PHARMACEUTICAL INDUSTRIES, INC.
----------
CEVIMELINE
CEVIMELINE HYDROCHLORIDE CAPSULES
DESCRIPTION
Cevimeline is cis -2’-methylspiro{1-azabicyclo [2.2.2] octane-3,
5’-[1,3]
oxathiolane} hydrochloride, hydrate (2:1). Its empirical formula is C
H
NOS.HCl.½
H O, and its structural formula is:
Cevimeline has a molecular weight of 244.79. It is a white to off
white crystalline powder
with a melting point range of 201 to 203 C. It is freely soluble in
alcohol and chloroform,
very soluble in water, and virtually insoluble in ether. The pH of a
1% solution ranges
from 4.6 to 5.6. Inactive ingredients include lactose monohydrate,
hydroxypropyl
cellulose, and magnesium stearate.
CLINICAL PHARMACOLOGY
_Pharmacodynamics_
Cevimeline is a cholinergic agonist which binds to muscarinic
receptors. Muscarinic
agonists in sufficient dosage can increase secretion of exocrine
glands, such as salivary
and sweat glands and increase tone of the smooth muscle in the
gastrointestinal and
urinary tracts.
_Pharmacokinetics_
Absorption: After administration of a single 30 mg capsule, cevimeline
was rapidly
absorbed with a mean time to peak concentration of 1.5 to 2 hours. No
accumulation of
active drug or its metabolites was observed following multiple dose
administration. When
administered with food, there is a decrease in the rate of absorption,
with a fasting t
of 1.53 hours and a t
of 2.86 hours after a meal; the peak concentration is reduced
by 17.3%. Single oral doses across the clinical dose range are dose
proportional.
Distribution: Cevimeline has a volume of distribution of approximately
6L/kg and is
<20% bound to human plasma proteins. This suggests that cevimeline is
extensively
bound to tissues; however, the specific binding sites are unknown.
10
17
2
o
MAX
MAX
Metabolism: Isozymes CYP2D6 and CYP3A3/4 are responsible for the
metabolism of
cevimeline. After 24 hours, 86.7% of the dose was recovered (16.0%
unchanged,
44.5% as cis and trans-sulfoxide, 22.3% of the dose as glucuronic acid
conj