Hyoscyamine Sulfate

KAISER FOUNDATION HOSPITALS

FULL PRESCRIBING INFORMATION: CONTENTS*

• HYOSCYAMINE SULFATE DESCRIPTION
• Clinical Pharmacology
• Hyoscyamine Sulfate Indications and Usage
• Contraindications
• Warnings
• Precautions
• INFORMATION FOR PATIENTS
• DRUG INTERACTIONS
• PREGNANCY--PREGNANCY CATEGORY C
• HYOSCYAMINE SULFATE ADVERSE REACTIONS
• OVERDOSAGE
• HYOSCYAMINE SULFATE DOSAGE AND ADMINISTRATION
• HOW SUPPLIED
• STORAGE AND HANDLING
• Package Label - Principal Display Panel

FULL PRESCRIBING INFORMATION

HYOSCYAMINE SULFATE DESCRIPTION

Hyoscyamine Sulfate SL Tablets 0.125 mg are formulated for sublingual and oral administration. Hyoscyamine Sulfate SL
Tablets 0.125 mg disintegrate within seconds after placement under or on the tongue, allowing it to be swallowed with or
Hyoscyamine Sulfate is one of the principal anticholinergic/antispasmodic components of belladonna alkaloids. The empirical formula is
(C 17 H 23 NO 3) 2 •H 2SO4 •2H 2 O and the molecular weight is 712.85. Chemically, it is
benzeneacetic acid, (alpha) (hydroxymethyl)--, 8-methyl-8-azabicyclo [3.2.1.] oct-3-yl ester, [3(S)-endo]-, sulfate (2:1), dihydrate .

Each tablet also contains as inactive ingredients: aspartame, colloidal silicon dioxide, crospovidone, flavor, magnesium stearate, mannitol, microcrystalline cellulose.

Clinical Pharmacology

Hyoscyamine Sulfate inhibits specifically the actions of acetylcholine on structures innervated by postganglionic cholinergic nerves and on smooth muscles that respond to acetylcholine but lack cholinergic innervation. These peripheral cholinergic receptors are present in the autonomic
effector cells of the smooth muscle, cardiac muscle, the sinoatrial node, the atrioventricular node, and the exocrine glands. At therapeutic doses, it is completely devoid of any action on autonomic ganglia. Hyoscyamine Sulfate inhibits gastrointestinal propulsive motility and decreases gastric acid secretion. Hyoscyamine Sulfate also controls excessive pharyngeal, tracheal, and bronchial
secretions. Hyoscyamine Sulfate is absorbed totally and completely by sublingual as well as oral
administration. Once absorbed, Hyoscyamine Sulfate disappears rapidly from the blood and is distributed throughout the entire body. The half-life of Hyoscyamine Sulfate is 2 to 3 hours. Hyoscyamine Sulfate is partly hydrolyzed to tropic acid and tropine but the
majority of the drug is excreted in the urine unchanged within the first 12 hours. Only traces of this drug are found in breast milk. Hyoscyamine Sulfate passes the blood brain barrier and the placental barrier.

Hyoscyamine Sulfate Indications and Usage

Hyoscyamine Sulfate is effective as adjunctive therapy in the treatment of peptic ulcers. It can also be used to control gastric secretion, visceral spasm and hypermotility in spastic colitis, spastic bladder, cystitis, pylorospasm, and associated abdominal cramps. May be used in functional intestinal disorders to reduce symptoms such as those seen in mild dysenteries, diverticulitis, and
acute enterocolitis. For use as adjunctive therapy in the treatment of irritable bowel syndrome (irritable colon, spastic colon, mucous colitis) and functional gastrointestinal disorders. Also used as adjunctive therapy in the treatment of neurogenic bladder and neurogenic bowel disturbances (including the splenic flexure syndrome and neurogenic colon). Hyoscyamine Sulfate is indicated
along with morphine or other narcotics in symptomatic relief of biliary and renal colic; as a "drying agent" in the relief of symptoms of acute rhinitis; in the therapy of parkinsonism to reduce rigidity and tremors and to control associated sialorrhea and hyperhidrosis. May be used in the therapy of poisoning by anticholinesterase agents.

Contraindications

Glaucoma; obstructive uropathy (for example, bladder neck obstruction due to prostatic hypertrophy); obstructive disease of the gastrointestinal tract (as in achalasia, pyloroduodenal stenosis): paralytic ileus, intestinal atony of elderly or debilitated patients; unstable cardiovascular status in acute hemorrhage; severe ulcerative colitis; toxic megacolon complicating ulcerative
colitis; myasthenia gravis.

Warnings

In the presence of high environmental temperature, heat prostration can occur with drug use (fever and heat stroke due to
decreased sweating). Diarrhea may be an early symptom of incomplete intestinal obstruction, especially in patients with
ileostomy or colostomy. In this instance, treatment with this drug would be inappropriate and possibly harmful. Like other
anticholinergic agents, Hyoscyamine Sulfate SL Tablets 0.125 mg may produce drowsiness, dizziness or blurred vision. In this event,
the patient should be warned not to engage in activities requiring mental alertness such as operating a motor vehicle or other machinery
or to perform hazardous work while taking this drug. Psychosis has been reported in sensitive individuals given anticholinergic
drugs. CNS signs and symptoms include confusion, disorientation, short term memory loss, hallucinations, dysarthria, ataxia, coma,
euphoria, decreased anxiety, fatigue, insomnia, agitation and mannerisms, and inappropriate affect. These CNS signs and
symptoms usually resolve within 12 to 48 hours after discontinuation of the drug.

Precautions

General: Use with caution in patients with: autonomic neuropathy, hyperthyroidism,coronary heart disease, congestive heart failure, cardiac arrhythmias, hypertension, and renal disease. Investigate any tachycardia before giving any anticholinergic drug since they may increase the heart rate. Use with caution in patients with hiatal hernia associated with reflux esophagitis.

INFORMATION FOR PATIENTS

Like other anticholinergic agents, Hyoscyamine Sulfate SL Tablets 0.125 mg may produce drowsiness, dizziness, or blurred vision. In this event, the patient should be warned not to engage in activities requiring mental alertness such as operating a motor vehicle or other machinery or to perform hazardous work while taking this drug. Use of Hyoscyamine Sulfate SL Tablets 0.125 mg may decrease sweating resulting in heat prostration, fever or heat stroke; febrile patients or those who may be exposed to elevated environmental temperatures should use caution.

Phenylketonurics:
Phenylketonuric patients should be informed that Hyoscyamine Sulfate SL Tablets 0.125 mg contains phenylalanine 2.2 mg per tablet.

DRUG INTERACTIONS

Additive adverse effects resulting from cholinergic blockade may occur when Hyoscyamine Sulfate SL Tablets 0.125 mg are administered concomitantly with other antimuscarinics, amantadine, haloperidol, phenothiazines, monoamine oxidase (MAO) inhibitors, tricyclic antidepressants or some antihistamines. Antacids may interfere with the absorption of Hyoscyamine Sulfate. Administer Hyoscyamine Sulfate SL Tablets 0.125 mg before meals; antacids after meals.

No long-term studies in animals have been performed to determine the carcinogenic, mutagenic or impairment of fertility potential of Hyoscyamine Sulfate SL Tablets 0.125 mg.

PREGNANCY--PREGNANCY CATEGORY C

Pregnancy--Pregnancy Category C:
Animal reproduction studies have not been conducted with Hyoscyamine Sulfate SL Tablets 0.125 mg. It is also not known whether Hyoscyamine Sulfate SL Tablets 0.125 mg can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Hyoscyamine
Sulfate SL Tablets 0.125 mg should be given to a pregnant woman only if clearly needed.

Nursing Mothers:
Hyoscyamine Sulfate is excreted in human milk. Caution should be exercised when Hyoscyamine Sulfate SL Tablets 0.125 mg is administered to a nursing woman.

HYOSCYAMINE SULFATE ADVERSE REACTIONS

Not all of the following adverse reactions have been reported with Hyoscyamine Sulfate. The following adverse reactions have been reported for pharmacologically similar drugs with anticholinergic/antispasmodic action. Adverse reactions may include dryness of the mouth; urinary
hesitancy and retention; blurred vision; tachycardia; palpitations; mydriasis; cycloplegia; increased ocular tension; loss of taste; headache; nervousness; drowsiness; weakness; dizziness; insomnia; nausea; vomiting; impotence; suppression of lactation; constipation; bloated feeling; allergic reactions or drug idiosyncrasies; urticaria and other dermal manifestations; ataxia; speech disturbance; some degree of mental confusion
and/or excitement (especially in elderly persons); and deceased sweating.

OVERDOSAGE

The signs and symptoms of overdose are headache, nausea, vomiting, blurred vision, dilated pupils, hot dry skin, dizziness, dryness of the mouth, difficulty in swallowing, and CNS stimulation.

Measures to be taken are immediate lavage of the stomach and injection of physostigmine 0.5 to 2 mg intravenously and repeated as necessary up to a total of 5mg. Fever may be treated symptomatically (tepid water sponge baths, hypothermic blanket). Excitement to a degree which demands attention may be managed with sodium thiopental 2% solution given slowly intravenously or chloral hydrate (100-200 ml of a 2% solution) by rectal
infusion. In the event of progression of the curare-like effect to paralysis of the respiratory muscles, artificial respiration should be instituted and maintained until effective respiratory action returns.

In rats, the LD 50 for Hyoscyamine Sulfate is 375 mg/kg. Hyoscyamine Sulfate is dialyzable.

HYOSCYAMINE SULFATE DOSAGE AND ADMINISTRATION

Dosage may be adjusted according to the conditions and severity of symptoms. Place Hyoscyamine Sulfate SL Tablets 0.125 mg under the tongue, allowing the tablet to rapidly disintegrate. May be taken with or without water. Tablets may also be placed on the tongue for oral disintegration, chewed, or swallowed orally.

Adults and pediatric patients 12 years of age and older: 1 to 2 tablets every four hours or as needed. Do not exceed 12 tablets in 24 hours.

Pediatric patients 2 to under 12 years of age: ½ to 1 tablet every four hours or as needed. Do not exceed 6 tablets in 24 hours.

HOW SUPPLIED

Hyoscyamine Sulfate S L Tablets 0.125 mg are white, mint-flavored, round and imprinted “VP 11” on one side and other side plain.

NDC 0179-0013-70 30 TAB in 1 Box, UNIT-DOSE

STORAGE AND HANDLING

Store at controlled room temperature, 20° - 25°C (68° - 77°F).
Protect from moisture.
Dispense in tight, light-resistant container as defined in USP.

KEEP THIS MEDICATION AND ALL
MEDICATIONS OUT OF THE
REACH OF CHILDREN.

Manufactured for: Vision Pharma, LLC
Wall, NJ 07719
www.visionpharma.com

Manufactured by: Sunrise Pharmaceutical, Inc.
Rahway, NJ 07065
INR 07/2008

Package Label - Principal Display Panel