Levsin Injection :: Schwarz

DESCRIPTION

LEVSIN® (hyoscyamine sulfate USP) is one of the principal anticholinergic/antispasmodic components of belladonna alkaloids. The empirical formula is (C 17 H 23 NO 3 ) 2 ·H 2 SO 4 ·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.

LEVBID Extended-Release Tablets contain 0.375 mg of hyoscyamine sulfate in a formulation designed for oral b.i.d. dosage. Each LEVBID Extended-Release Tablet also contains as inactive ingredients: lactose, magnesium stearate, FD&C yellow #6 and other ingredients.

LEVSIN/SL Tablets contain 0.125 mg hyoscyamine sulfate formulated for sublingual administration. However, the tablets may be chewed or taken orally. Each tablet also contains as inactive ingredients: colloidal silicon dioxide, dextrates, flavor, mannitol, and stearic acid.

LEVSIN Tablets contain 0.125 mg hyoscyamine sulfate formulated for oral administration. Each tablet also contains as inactive ingredients: acacia, confectioner's sugar, corn starch, lactose, powdered cellulose and stearic acid.

LEVSIN Elixir contains 0.125 mg hyoscyamine sulfate per 5 mL with 20% alcohol for oral administration. LEVSIN Elixir also contains as inactive ingredients: FD&C Red #40, FD&C Yellow #6, flavor, glycerin, purified water, sorbitol solution and sucrose.

LEVSIN Drops contain 0.125 mg hyoscyamine sulfate per mL with 5% alcohol for oral administration. LEVSIN Drops also contain as inactive ingredients: FD&C Red #40, FD&C Yellow #6, flavor, glycerin, purified water, sodium citrate, sorbitol solution, and sucrose.

LEVSIN Injection is a sterile solution containing 0.5 mg hyoscyamine sulfate per mL. The 1 mL ampuls contain as inactive ingredients: water for injection, pH is adjusted with hydrochloric acid when necessary.

LEVSINEX TIMECAPS contain 0.375 mg hyoscyamine sulfate in an extended-release formulation designed for oral b.i.d. dosage. Each capsule also contains as inactive ingredients: FD&C blue #1, D&C red #28, FD&C red #40, FD&C yellow #6, gelatin, lactose monohydrate, sodium lauryl sulfate, magnesium stearate, silicon dioxide, titanium dioxide and other ingredients.

CLINICAL PHARMACOLOGY

LEVSIN 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, the 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. LEVSIN inhibits gastrointestinal propulsive motility and decreases gastric acid secretion. LEVSIN also controls excessive pharyngeal, tracheal and bronchial secretions.

LEVSIN is absorbed totally and completely by sublingual administration as well as oral administration. Once absorbed, LEVSIN disappears rapidly from the blood and is distributed throughout the entire body. The half-life of LEVSIN is 2 to 3 1 / 2 hours. LEVSIN 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 passes the blood brain barrier and the placental barrier.

LEVBID releases 0.375 mg hyoscyamine sulfate at a controlled and predictable rate for 12 hours. The mean peak plasma concentration occurred at 4.20 hours. The mean (±SEM) apparent plasma elimination half-life is 7.47 hours (±0.60). Tablets may not completely disintegrate and may be excreted by some patients.

LEVSINEX TIMECAPS release 0.375 mg hyoscyamine sulfate at a controlled and predictable rate for 12 hours. The mean peak plasma concentration occurred at 4.66 hours. The mean (±SEM) apparent plasma elimination half-life is 6.21 hours (±0.43). Capsule contents may not completely disintegrate and may be excreted by some patients.

INDICATIONS AND USAGE

LEVSIN 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 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.

Parenterally administered LEVSIN is also effective in reducing gastrointestinal motility to facilitate diagnostic procedures such as endoscopy or hypotonic duodenography. LEVSIN may be used to reduce pain and hypersecretion in pancreatitis. LEVSIN may also be used in certain cases of partial heart block associated with vagal activity.

IN ANESTHESIA:

LEVSIN Injection is indicated as a pre-operative antimuscarinic to reduce salivary, tracheobronchial, and pharyngeal secretions; to reduce the volume and acidity of gastric secretions, and to block cardiac vagal inhibitory reflexes during induction of anesthesia and intubation. LEVSIN protects against the peripheral muscarinic effects such as bradycardia and excessive secretions produced by halogenated hydrocarbons and cholinergic agents such as physostigmine, neostigmine, and pyridostigmine given to reverse the actions of curariform agents.

IN UROLOGY:

LEVSIN Injection may also be used intravenously to improve radiologic visibility of the kidneys. It is also indicated along with morphine or other narcotics in symptomatic relief of biliary and renal colic.

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, LEVSIN 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 inlude 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, LEVSIN 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 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.

LEVBID Tablets may not completely disintegrate and may be excreted by some patients.

LEVSINEX capsule contents may not completely disintegrate and may be excreted by some patients.

Drug Interactions:

Additive adverse effects resulting from cholinergic blockade may occur when LEVSIN is administered concomitantly with other antimuscarinics, amantadine, haloperidol, phenothiazines, monoamine oxidase (MAO) inhibitors, tricyclic antidepressants or some antihistamines.

Antacids may interfere with the absorption of LEVSIN. Administer LEVSIN before meals; antacids after meals.

Carcinogenesis, Mutagenesis, Impairment of Fertility:

No long-term studies in animals have been performed to determine the carcinogenic, mutagenic or impairment of fertility potential of LEVSIN; 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. It is also not known whether LEVSIN can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. LEVSIN should be given to a pregnant woman only if clearly needed.

Nursing Mothers:

LEVSIN is excreted in human milk. Caution should be exercised when LEVSIN is administered to a nursing woman.

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 decreased 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 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 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 LEVSIN is 375 mg/kg. LEVSIN is dialyzable.

DOSAGE AND ADMINISTRATION

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

LEVBID Extended-Release Tablets: Adults and pediatric patients 12 years of age and older: 1 to 2 tablets every 12 hours. Tablets are scored and may be broken to allow for dose titration if needed. Do not crush or chew tablets. Do not exceed 4 tablets in 24 hours.

LEVSIN/SL Tablets:   The tablets may be taken sublingually, orally or chewed. 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: 1 / 2 to 1 tablet every four hours or as needed. Do not exceed 6 tablets in 24 hours.

LEVSIN Tablets:   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: 1 / 2 to 1 tablet every four hours or as needed. Do not exceed 6 tablets in 24 hours.

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

Pediatric patients 2 to under 12 years of age:

Please see the following dosage guide based on body weight. The doses may be repeated every four hours or as needed. Do not exceed 6 teaspoonfuls in 24 hours.

Body Weight Usual Dose
10 kg (22 lb) 1 / 4  tsp (1.25 mL)
20 kg (44 lb) 1 / 2  tsp (2.5 mL)
40 kg (88 lb) 3 / 4  tsp (3.75 mL)
50 kg (110 lb)  1 tsp (5 mL)

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

Pediatric patients 2 to under 12 years of age:   1 / 4 to 1 mL every four hours or as needed. Do not exceed 6 mL in 24 hours.

Pediatric patients under 2 years of age:   The following dosage guide is based upon body weight. The doses may be repeated every four hours or as needed.

Body Weight Usual Dose Do Not Exceed
in 24 Hours
3.4 kg (7.5 lb)  4 drops 24 drops
  5 kg (11 lb)  5 drops 30 drops
  7 kg (15 lb)  6 drops 36 drops
 10 kg (22 lb)  8 drops 48 drops

LEVSIN Injection: The dose may be administered subcutaneously, intramuscularly, or intravenously without dilution. As with all parenteral drug products, LEVSIN Injection should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit.

Gastrointestinal Disorders:   The usual adult recommended dose is 0.5 to 1 mL (0.25 to 0.5 mg). Some patients may need only a single dose; others may require administration two, three, or four times a day at four hour intervals.

Diagnostic Procedures:   The usual adult recommended dose is 0.5 to 1 mL (0.25 to 0.5 mg) administered intravenously 5 to 10 minutes prior to the diagnostic procedure.

Anesthesia: Adults and pediatric patients over 2 years of age: As a pre-anesthetic medication, the recommended dose is 5 µg (0.005 mg) per kg of body weight. This dose is usually given 30 to 60 minutes prior to the anticipated time of induction of anesthesia or at the time the pre-anesthetic narcotic or sedatives are administered.

LEVSIN Injection may be used during surgery to reduce drug-induced bradycardia. It should be administered intravenously in increments of 0.25 mL and repeated as needed. To achieve reversal of neuromuscular blockade, the recommended dose is 0.2 mg (0.4 mL) LEVSIN Injection for every 1 mg neostigmine or the equivalent dose of physostigmine or pyridostigmine.

LEVSINEX TIMECAPS:   Adults and pediatric patients 12 years of age and older: 1 to 2 capsules every 12 hours. Dosage may be adjusted to 1 capsule every 8 hours if needed. Do not crush or chew capsules. Do not exceed 4 capsules in 24 hours.

HOW SUPPLIED

LEVBID Extended-Release Tablets (hyoscyamine sulfate, 0.375 mg) are light orange, capsule-shaped, scored tablets. They are coded SP538.

Bottles of 100 tablets                  NDC 0091-3538-01

Bottles of 500 tablets                  NDC 0091-3538-05

LEVSIN/SL Tablets (hyoscyamine sulfate tablets USP, 0.125 mg) are white, peppermint-flavored, octagonal shaped, scored, and imprinted with "SCHWARZ" on one side and "532" on the other.

Bottles of 100 tablets                  NDC 0091-3532-01

Bottles of 500 tablets                  NDC 0091-3532-05

LEVSIN Tablets (hyoscyamine sulfate tablets USP, 0.125 mg) are white, scored and imprinted with "SCHWARZ" on one side and "531" on the other.

Bottles of 100 tablets                  NDC 0091-3531-01

Bottles of 500 tablets                  NDC 0091-3531-05

LEVSIN Elixir (hyoscyamine sulfate elixir USP, 0.125 mg/ 5 mL) is orange colored and flavored and contains 20% alcohol.

Pint (473 mL) bottles                  NDC 0091-4532-16

LEVSIN Drops (hyoscyamine sulfate oral solution USP, 0.125 mg/mL) are orange colored and flavored.

15 mL Dropper bottles                  NDC 0091-4538-15

LEVSIN Injection (hyoscyamine sulfate injection USP, 0.5 mg/mL) is a clear, colorless and sterile solution.

1 mL ampuls-Box of 5                  NDC 0091-1536-05

LEVSINEX TIMECAPS (hyoscyamine sulfate, 0.375 mg) Extended-Release Capsules are brown and white capsules imprinted "SCHWARZ" and "537."

Bottles of 100 capsules                  NDC 0091-3537-01

Bottles of 500 capsules                  NDC 0091-3537-05

Store at controlled room temperature 15°-30°C (59°-86°F).



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