EVOXAC- cevimeline hydrochloride capsule

Land: USA

Språk: engelska

Källa: NLM (National Library of Medicine)

Aktiva substanser:

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

Tillgänglig från:

Daiichi Sankyo, Inc.

Administreringssätt:

ORAL

Receptbelagda typ:

PRESCRIPTION DRUG

Terapeutiska indikationer:

Cevimeline is 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.

Produktsammanfattning:

EVOXAC® is available as white, hard gelatin capsules containing 30 mg of cevimeline hydrochloride. EVOXAC® 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 63395-201-13). Store at 25°C (77°F) excursion permitted to 15°-30°C (59°-86°F) Rx only Manufactured for : Daiichi Sankyo, Inc. Basking Ridge, NJ 07920 Revised 04/2018 Printed in U.S.A. USPI-EVO-0418-r100

Bemyndigande status:

New Drug Application

Produktens egenskaper

EVOXAC- CEVIMELINE HYDROCHLORIDE CAPSULE
DAIICHI SANKYO, INC.
----------
EVOXAC CAPSULES
(CEVIMELINE HYDROCHLORIDE)
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.
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 conjugate and 4% of the dose