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:

Hikma Pharmaceuticals USA Inc.

INN (International Name):

CEVIMELINE HYDROCHLORIDE

Composition:

CEVIMELINE HYDROCHLORIDE ANHYDROUS 30 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Cevimeline hydrochloride is indicated for the treatment of symptoms of dry mouth in patients with Sjögren’s Syndrome. Cevimeline hydrochloride 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 30 mg capsules is supplied as a white opaque cap and white opaque body with “54 190” printed on the cap and body, containing a white powder. NDC 0054-0334-25: Bottle of 100 Capsules Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.] Distr. by: Hikma Pharmaceuticals USA Inc. Berkeley Heights, NJ 07922 C50000416/01 Revised September 2020

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

CEVIMELINE HYDROCHLORIDE- CEVIMELINE HYDROCHLORIDE CAPSULE
HIKMA PHARMACEUTICALS USA INC.
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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. Gelatin
capsule shells contain: gelatin, monogramming ink, purified water,
sodium lauryl sulfate and titanium
dioxide. The monogramming ink contains: ammonium hydroxide, iron
oxide, isopropyl alcohol, n-butyl
alcohol, propylene glycol 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 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:_
10
17
2
MAX
MAX
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, th