Rx Drugs Info

orphenadrine citrate (Orphenadrine citrateinjection 
[Bedford Laboratories]

Rx ONLY

DESCRIPTION

Orphenadrine citrate is the citrate salt of orphenadrine (±)-N,N-dimethyl-2-[(o-methyl-α-phenylbenzyl)oxy]-ethylamine citrate (1:1). It occurs as a white, crystalline powder having a bitter taste. It is practically odorless; sparingly soluble in water, slightly soluble in alcohol.

Each vial contains 60 mg of orphenadrine citrate in aqueous solution. Each vial also contains: sodium metabisulfite, 2 mg; sodium chloride, 5.8 mg; sodium hydroxide, to adjust pH; and water for injection, q.s. to 2 mL. The structural formula is:

Image from Drug Label Content

Molecular Formula: C18H23NO•C6H8O7 M.W.: 461.50

CLINICAL PHARMACOLOGY

The mode of therapeutic action has not been clearly identified, but may be related to its analgesic properties. Orphenadrine citrate does not directly relax tense muscles in man. Orphenadrine citrate also possesses anticholinergic actions.

INDICATIONS AND USAGE

Orphenadrine citrate is indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute painful musculoskeletal conditions.

CONTRAINDICATIONS

Contraindicated in patients with glaucoma, pyloric or duodenal obstruction, stenosing peptic ulcers, prostatic hypertrophy or obstruction of the bladder neck, cardio-spasm (megaesophagus) and myasthenia gravis.

Contraindicated in patients who have demonstrated a previous hypersensitivity to the drug.

WARNINGS

Some patients may experience transient episodes of light-headedness, dizziness or syncope. Orphenadrine citrate may impair the ability of the patient to engage in potentially hazardous activities such as operating machinery or driving a motor vehicle; ambulatory patients should therefore be cautioned accordingly.

Orphenadrine citrate injection contains sodium metabisulfite, a sulfite that may cause allergic-type reactions including anaphylactic symptoms and life-threatening or less severe asthmatic episodes in certain susceptible people. The overall prevalence of sulfite sensitivity in the general population is unknown and probably low. Sulfite sensitivity is seen more frequently in asthmatic than nonasthmatic people.

PRECAUTIONS

Confusion, anxiety and tremors have been reported in few patients receiving propoxyphene and orphenadrine concomitantly. As these symptoms may be simply due to an additive effect, reduction of dosage and/or discontinuation of one or both agents is recommended in such cases.

Orphenadrine citrate should be used with caution in patients with tachycardia, cardiac decompensation, coronary insufficiency, cardiac arrhythmias.

Safety of continuous long-term therapy with orphenadrine has not been established. Therefore, if orphenadrine is prescribed for prolonged use, periodic monitoring of blood, urine and liver function values is recommended.

Pregnancy

Teratogenic Effects; Pregnancy Category C

Safe use of orphenadrine has not been established with respect to adverse effects upon fetal development. Therefore, orphenadrine should be used in women of childbearing potential and particularly during early pregnancy only when in the judgment of the physician the potential benefits outweigh the possible hazards.

Pediatric Use

Safety and effectiveness in children have not been established; therefore, this drug is not recommended for use in the pediatric age group.

ADVERSE REACTIONS

Adverse reactions of orphenadrine are mainly due to the mild anticholinergic action of orphenadrine, and are usually associated with higher dosage. Dryness of the mouth is usually the first adverse effect to appear. When the daily dose is increased, possible adverse effects include: tachycardia, palpitation, urinary hesitancy or retention, blurred vision, dilatation of pupils, increased ocular tension, weakness, nausea, vomiting, headache, dizziness, constipation, drowsiness, hypersensitivity reactions, pruritus, hallucinations, agitation, tremor, gastric irritation, and rarely urticaria and other dermatoses. Infrequently, an elderly patient may experience some degree of mental confusion. These adverse reactions can usually be eliminated by reduction in dosage. Very rare cases of aplastic anemia associated with the use of orphenadrine tablets have been reported. No causal relationship has been established.

Rare instances of anaphylactic reaction have been reported associated with the intramuscular injection of orphenadrine citrate.

DRUG ABUSE AND DEPENDENCE

Orphenadrine has been chronically abused for its euphoric effects. The mood elevating effects may occur at therapeutic doses of orphenadrine.

OVERDOSAGE

Orphenadrine is toxic when overdosed and typically induces anticholinergic effects. In a review of orphenadrine toxicity, the minimum lethal dose was found to be 2 to 3 grams for adults; however, the range of toxicity is variable and unpredictable. Treatment for orphenadrine overdose is evacuation of stomach contents (when necessary), charcoal at repeated doses, intensive monitoring, and appropriate supportive treatment of any emergent anticholinergic effects.

DOSAGE AND ADMINISTRATION

Adults - One 2 mL vial (60 mg) intravenously or intramuscularly; may be repeated every 12 hours. Relief may be maintained by one (100 mg) orphenadrine citrate tablet twice daily.

Parenteral drug products should be inspected visually for particulate matter, whenever solution and container permit.

HOW SUPPLIED

Orphenadrine Citrate Injection USP is supplied as follows: Cartons of 10 (NDC 55390-059-10) 2 mL vials, each vial containing 60 mg of orphenadrine citrate in aqueous solution.

Store at controlled room temperature 15° to 30°C (59° to 86°F). [See USP.] Protect from light.

Single dose vial. Discard unused portion.

Manufactured by:                                                 Manufactured for:

Ben Venue Laboratories, Inc.                                Bedford Laboratories™

Bedford, OH 44146                                               Bedford, OH 44146

June 2008                                                   Div-ORP-P02


Orphenadrine citrate (Orphenadrine citrate)
PRODUCT INFO
Product Code 55390-059 Dosage Form INJECTION
Route Of Administration INTRAMUSCULAR, INTRAVENOUS DEA Schedule
INGREDIENTS
Name (Active Moiety) Type Strength
Orphenadrine citrate (Orphenadrine) Active 60 MILLIGRAM  In 2 MILLILITER
sodium chloride Inactive 5.8 MILLIGRAM  In 2 MILLILITER
sodium hydroxide to adjust pH Inactive  
sodium metabisulfite Inactive 2 MILLIGRAM  In 2 MILLILITER
water Inactive  
IMPRINT INFORMATION
Characteristic Appearance Characteristic Appearance
Color Score
Shape Symbol
Imprint Code Coating
Size
PACKAGING
# NDC Package Description Multilevel Packaging
1 55390-059-10 10 VIAL In 1 BOX contains a VIAL
1 2 MILLILITER In 1 VIAL This package is contained within the BOX (55390-059-10)

Revised: 06/2008Bedford Laboratories

Data are from FDA and U.S. National Library of Medicine.