EVOXAC- cevimeline hydrochloride capsule

Valsts: Amerikas Savienotās Valstis

Valoda: angļu

Klimata pārmaiņas: NLM (National Library of Medicine)

Aktīvā sastāvdaļa:

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

Pieejams no:

STAT RX USA LLC

SNN (starptautisko nepatentēto nosaukumu):

CEVIMELINE HYDROCHLORIDE

Kompozīcija:

CEVIMELINE HYDROCHLORIDE 30 mg

Ievadīšanas:

ORAL

Receptes veids:

PRESCRIPTION DRUG

Ārstēšanas norādes:

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.

Produktu pārskats:

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 Distributed and Marketed by: Daiichi Sankyo Pharma Development, a Division of Daiichi Sankyo, Inc. Edison, NJ 08837 PRT40  11/2006  Printed in U.S.A.

Autorizācija statuss:

New Drug Application

Produkta apraksts

EVOXAC - CEVIMELINE HYDROCHLORIDE CAPSULE
STAT RX USA LLC
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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.1/2 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 less than 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 as
N-oxide of cevimeline).
Approximatel