CEVIMELINE HYDROCHLORIDE capsule

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Novel Laboratories, Inc.

INN (International Name):

CEVIMELINE HYDROCHLORIDE

Composition:

CEVIMELINE HYDROCHLORIDE ANHYDROUS 30 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

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.

Product summary:

Cevimeline Hydrochloride Capsules are available as hard gelatin capsule with tan opaque cap and tan opaque body imprinted with "NL 999" on the cap and "30 mg" on the body with black ink, filled with white to off white granular powder. It is supplied in: Child-resistant bottles of 30 Capsules (NDC 40032-999-03) Child-resistant bottles of 100 Capsules (NDC 40032-999-01) Bottles of 500 Capsules (NDC 40032-999-05) Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature]. Dispense in a tight, light resistant container as defined in the USP/NF. Rx  Only Manufactured by:  Novel Laboratories, Inc. Somerset, NJ 08873 Iss. 02/2016 PI9990000101

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

CEVIMELINE HYDROCHLORIDE- CEVIMELINE HYDROCHLORIDE CAPSULE
NOVEL LABORATORIES, INC.
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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.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; a hard
gelatin capsule which contains D&C Yellow #10, FD&C Red #40, FD&C
Yellow #6, titanium dioxide
and gelatin; and an imprinting ink which contains shellac, iron oxide
black, isopropyl alcohol, butyl
alcohol, propylene glycol and ammonium hydroxide.
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 unknow