CEVIMELINE HYDROCHLORIDE capsule

国家: 美国

语言: 英文

来源: NLM (National Library of Medicine)

有效成分:

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

可用日期:

Cosette Pharmaceuticals, Inc.

给药途径:

ORAL

处方类型:

PRESCRIPTION DRUG

疗效迹象:

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.

產品總結:

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 0713-0937-01). Store at 25°C (77°F) excursion permitted to 15°-30°C (59°-86°F) Rx only Marketed by: Cosette Pharmaceuticals, Inc. South Plainfield, NJ 07080 8-0937CP1       Iss. 07/2022 2000014961

授权状态:

New Drug Application

产品特点

CEVIMELINE HYDROCHLORIDE- CEVIMELINE HYDROCHLORIDE CAPSULE
COSETTE PHARMACEUTICALS, INC.
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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
10
17
2
o
MAX
MAX
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
c