Levsin

DESCRIPTION

Levsin® tablets (hyoscyamine sulfate tablets USP) contain 0.125 mg hyoscyamine sulfate formulated for oral administration.

Levsin® (hyoscyamine) is one of the principalanticholinergic/antispasmodiccomponents ofbelladonnaalkaloids. The empirical formula is (C₁₇H₂₃NO₃)₂•H₂SO₄•2H₂O and the molecular weight is 712.85. Chemically, it is benzeneacetic acid, a-(hydroxymethyl)-, 8-methyl-8-azabicyclo [3.2.1.] oct-3-yl ester, [3(S)-endo]-, sulfate (2:1), dihydrate with the following structure:

Each tablet also contains as inactive ingredients: FD&C blue #1, lactose monohydrate, magnesium stearate, mannitol, starch and stearic acid.

INDICATIONS

Levsin® (hyoscyamine) is effective as adjunctive therapy in the treatment of peptic ulcer. 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). Also used in the treatment of infant colic (elixir and drops). Levsin® (hyoscyamine) 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.

DOSAGE AND ADMINISTRATION

Dosage may be adjusted according to the conditions and severity of symptoms.

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

Levsin® tablets (hyoscyamine sulfate tablets USP) 0.125 mg are round, blue colored tablets that are imprinted with “AP” on one side and “112” on the other.

Bottles of 100 tabletsNDC68220-112-10
Bottles of 500 tabletsNDC68220-112-50

Store at controlled room temperature 20°- 25°C (68° - 77°F); excursions permitted to15°- 30°C (59°- 86°F). Please refer to current USP.

Dispense in tight, light-resistant containers as defined in USP/NF with a child-resistant closure.

KEEP OUT OF REACH OF CHILDREN

Also available as:

Levsin®	Dosage Strength	Package Size	NDC
平板电脑	0.125mg	100	68220-112-10
平板电脑	0.125mg	500	68220-112-50
Sub-lingual平板电脑	0.125mg	100	68220-113-10
Sub-lingual Tablets	0.125mg	500	68220-113-50
Elixir	0.125mg/5 mL	Pint	0091-4532-16
Drops	0.125mg/mL	15mL	0091-4538-15
Injection	0.5mg/mL	Box of 5-1mL	0091-1536-05
Levbid® extended-	0.375mg	100	68220-115-10
release tablets	0.375mg	500	68220-115-50

Address medical inquiries to: Alaven Pharmaceutical LLC, 2260 Northwest Parkway, Suite A Marietta, GA 30067 Or call toll free 1-888-317-0001. Rev. 02/08.

SIDE EFFECTS

所有下列不良反应的reported with hyoscyamine sulfate. Adverse reactions may include dryness of the mouth; urinary hesitancy and retention; blurred vision;tachycardia;palpitations;mydriasis; increasedoculartension; loss of taste; headache; nervousness; drowsiness; weakness; fatigue; dizziness; insomnia; nausea; vomiting;impotence; constipation; bloated feeling; abdominal pain; diarrhea; allergic reactions or drug idiosyncrasies;urticariaand otherdermalmanifestations;ataxia; speech disturbance; some degree of mental confusion and/or excitement (especially in elderly persons); short-term memory loss; hallucinations; and decreased sweating.

DRUG INTERACTIONS

Additive adverse effects resulting from cholinergic blockade may occur when Levsin® (hyoscyamine) is administered concomitantly with other antimuscarinics, amantadine, haloperidol, phenothiazines, monoamine oxidase (MAO) inhibitors,tricyclic antidepressantsor someantihistamines.

Antacids may interfere with the absorption of Levsin® (hyoscyamine) . Administer Levsin® (hyoscyamine) before meals; antacids after meals.

警告

In the presence of high environmental temperature,heat prostrationcan occur with drug use (fever and heatstrokedue to decreased sweating). Diarrhea may be an early symptom of incompleteintestinal obstructionespecially in patients with ileostomy orcolostomy. In this instance, treatment with this drug would be inappropriate and possibly harmful. Like other anticholinergic agents, Levsin® (hyoscyamine) 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.

Psychosishas been reported in sensitive individuals given anticholinergic drugs including hyoscyamine sulfate. CNS signs and symptoms include confusion, disorientation, short-term memory loss, hallucinations,dysarthria, ataxia,euphoria, 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: autonomicneuropathy, hyperthyroidism, coronaryheart 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 withhiatalhernia associated withrefluxesophagitis.

Carcinogenesis, Mutagenesis, Impairment of Fertility

No long-term studies in animals have been performed to determine thecarcinogenic, mutagenic or impairment of fertility potential of Levsin® (hyoscyamine) ; however, 40 years of marketing experience with hyoscyamine sulfate shows no demonstrable evidence of a problem.

Pregnancy–Pregnancy Category C

Animal reproduction studies have not been conducted with Levsin® (hyoscyamine) . It is also not known whether Levsin® (hyoscyamine) can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Levsin® (hyoscyamine) should be given to a pregnant woman only if clearly needed.

Nursing Mothers

Levsin® (hyoscyamine) is excreted in human milk. Caution should be exercised when Levsin® (hyoscyamine) is administered to a nursing woman.

Geriatric Use

Reported clinical experience has not identified differences in safety between patients aged 65 and over and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function.

OVERDOSE

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.

措施的直接灌洗tomach and injection of physostigmine 0.5 to 2 mg intravenously and repeated as necessary up to a total of 5 mg. 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 orchloral hydrate(100-200 mL of a 2% solution) byrectalinfusion. In the event of progression of the curare-like effect toparalysisof the respiratory muscles, artificialrespirationshould be instituted and maintained until effective respiratory action returns.

In rats, the LD₅₀for hyoscyamine is 375 mg/kg. Levsin® (hyoscyamine) is dialyzable.

CONTRAINDICATIONS

Glaucoma; obstructive uropathy (for example,bladderneck obstruction due to prostatichypertrophy); obstructive disease of thegastrointestinal tract(as inachalasia, pyloroduodenalstenosis);paralytic ileus, intestinal atony of elderly or debilitated patients; unstablecardiovascularstatus in acutehemorrhage; severeulcerative colitis; toxic megacolon complicating ulcerativecolitis;myasthenia gravis.

CLINICAL PHARMACOLOGY

Levsin® (hyoscyamine) inhibits specifically the actions ofacetylcholineon structures innervated by postganglionic cholinergic nerves and on smooth muscles that respond to acetylcholine but lack cholinergicinnervation. These peripheral cholinergic receptors are present in the autonomic effector cells of thesmooth muscle, cardiac muscle, the sinoatrial node, theatrioventricularnode, and theexocrineglands. At therapeutic doses, it is completely devoid of any action on autonomic ganglia. Levsin® (hyoscyamine) inhibitsgastrointestinalpropulsive motility and decreasesgastricacid secretion. Levsin® (hyoscyamine) also controls excessive pharyngeal, tracheal and bronchial secretions.

Levsin® (hyoscyamine) is absorbed totally and completely bysublingualadministration as well as oral administration. Once absorbed, Levsin® (hyoscyamine) disappears rapidly from the blood and is distributed throughout the entire body. The half-life of Levsin® (hyoscyamine) is 2 to 3½ hours. Levsin® (hyoscyamine) 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. Levsin® (hyoscyamine) passes the blood brain barrier and the placental barrier.

PATIENT INFORMATION

Like other anticholinergic agents, Levsin® (hyoscyamine) 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 Levsin® (hyoscyamine) may decrease sweating resulting in heat prostration, fever or heat stroke;febrilepatients or those who may be exposed to elevated environmental temperatures should use caution.