CEVIMELINE HYDROCHLORIDE capsule

Riik: Ameerika Ühendriigid

keel: inglise

Allikas: NLM (National Library of Medicine)

Toimeaine:

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

Saadav alates:

Aurobindo Pharma Limited

Manustamisviis:

ORAL

Retsepti tüüp:

PRESCRIPTION DRUG

Näidustused:

Cevimeline hydrochloride capsules are indicated for the treatment of symptoms of dry mouth in patients with Sjögren’s Syndrome. Cevimeline hydrochloride capsules are 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.

Toote kokkuvõte:

Cevimeline Hydrochloride Capsules, 30 mg are available as white opaque, hard gelatin capsules containing 30 mg of cevimeline hydrochloride. Cevimeline hydrochloride capsules have a white opaque colored cap and white opaque colored body. The hard gelatin capsules are imprinted with ‘CEVH’ on the cap and ‘30’ on the body. They are supplied as follows:          Bottles of 100 capsules                        NDC 59651-422-01 (Child Resistant Closure)          Bottles of 500 capsules                        NDC 59651-422-05 Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Distributed by: Aurobindo Pharma USA, Inc. 279 Princeton-Hightstown Road East Windsor, NJ 08520 Manufactured by: Aurobindo Pharma Limited Hyderabad-500 032, India Issued: June 2022

Volitamisolek:

Abbreviated New Drug Application

Toote omadused

CEVIMELINE HYDROCHLORIDE - CEVIMELINE HYDROCHLORIDE CAPSULE
AUROBINDO PHARMA LIMITED
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CEVIMELINE HYDROCHLORIDE CAPSULES
RX ONLY
DESCRIPTION
Cevimeline is cis-2’-methylspiro {1-azabicyclo [2.2.2] octane-3,
5’ -[1,3] oxathiolane}
hydrochloride, hydrate (2:1). Its molecular 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 hydroxypropyl cellulose,
lactose
monohydrate, and magnesium stearate. The empty hard gelatin capsule
shell contains
gelatin and titanium dioxide. The capsules are printed with black ink
containing black iron
oxide, potassium hydroxide and shellac.
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
10
17
2
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
6 L/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