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Orphenadrine: Drug information

Orphenadrine: Drug information
(For additional information see "Orphenadrine: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Pharmacologic Category
  • Skeletal Muscle Relaxant
Dosing: Adult
Pain, musculoskeletal, acute

Pain, musculoskeletal, acute:

Note: For skeletal muscle spasm and/or pain (eg, low back pain, neck pain) with muscle spasm, usually in combination with a nonsteroidal anti-inflammatory drug and/or acetaminophen (Ref). In general, muscle relaxants should be used temporarily (eg, for a few days or intermittently for a few days when needed) (Ref).

Oral: 100 mg twice daily.

IM, IV: 60 mg; may repeat every 12 hours.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Older Adult

Avoid use (Ref).

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

Frequency not defined:

Cardiovascular: Palpitations, tachycardia

Central nervous system: Agitation, confusion, dizziness, drowsiness, euphoria, hallucination, headache

Dermatologic: Pruritus, urticaria

Gastrointestinal: Constipation, gastric irritation, nausea, vomiting, xerostomia

Genitourinary: Urinary retention, urination hesitancy

Hypersensitivity: Hypersensitivity reaction

Neuromuscular & skeletal: Tremor, weakness

Ophthalmic: Blurred vision, increased intraocular pressure, mydriasis, nystagmus

Respiratory: Nasal congestion

<1%, postmarketing, and/or case reports: Anaphylaxis (injection), aplastic anemia

Contraindications

Hypersensitivity to orphenadrine or any component of the formulation; glaucoma; pyloric or duodenal obstruction, stenosing peptic ulcer; prostatic hypertrophy, bladder neck obstruction; cardiospasm (megaesophagus); myasthenia gravis

Warnings/Precautions

Concerns related to adverse effects:

• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).

Disease-related concerns:

• Abuse potential: Use with caution in patients with a history of substance use disorder; euphoria may occur at therapeutic doses and the potential for abuse exists.

• Cardiovascular disease: Use with caution in patients with heart failure, cardiac decompensation, coronary insufficiency, tachycardia, or cardiac arrhythmias.

Dosage form specific issues:

• Sulfites: Injection contains sodium bisulfite which may cause allergic reaction in some individuals.

Other warnings/precautions:

• Long-term use: Has not been evaluated for continuous long-term use; monitor closely.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Injection, as citrate:

Generic: 30 mg/mL (2 mL)

Tablet Extended Release 12 Hour, Oral, as citrate:

Generic: 100 mg

Generic Equivalent Available: US

Yes

Pricing: US

Solution (Orphenadrine Citrate Injection)

30 mg/mL (per mL): $9.36

Tablet, 12-hour (Orphenadrine Citrate ER Oral)

100 mg (per each): $2.18 - $2.31

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

IM: Administer deep IM.

IV: Administer undiluted via slow IV push over 2 to 5 minutes (Ref). Also refer to institution-specific policies and procedures.

Oral: Do not crush sustained-release drug product.

Bariatric surgery: Tablet, extended release: Some institutions may have specific protocols that conflict with these recommendations; refer to institutional protocols as appropriate. ER tablet should be swallowed whole. Do not cut, chew, or crush. No alternative oral formulations are available (injectable only). If safety and efficacy can be effectively monitored, no change in formulation or administration is required after bariatric surgery; however, consider IV or IM administration for acute relief.

Use: Labeled Indications

Pain, musculoskeletal, acute: Adjunct to rest, physical therapy, and other measures for the treatment of discomfort associated with acute painful musculoskeletal conditions.

Medication Safety Issues
Sound-alike/look-alike issues:

Norflex may be confused with norfloxacin, Noroxin

Older Adult: High-Risk Medication:

Beers Criteria: Orphenadrine is identified in the Beers Criteria as a potentially inappropriate medication to be avoided in patients 65 years and older (independent of diagnosis or condition) because most muscle relaxants are poorly tolerated in older adults due to anticholinergic effects caused by some muscle relaxants, risk of sedation, and an increased risk of fracture. Orphenadrine has strong anticholinergic properties. In addition, efficacy is questionable at doses tolerated by geriatric patients (Beers Criteria [AGS 2023]).

International issues:

Biorphen: Brand name for orphenadrine [Great Britain] but is also the brand name for phenylephrine (systemic) [US]

Flexin: Brand name for orphenadrine [Israel] but is also the brand name for cyclobenzaprine [Chile] and diclofenac [Argentina]

Flexin [Israel] may be confused with Floxin which is a brand name for flunarizine [Thailand], norfloxacin [South Africa], ofloxacin [US, Canada], and perfloxacin [Philippines]

Metabolism/Transport Effects

Substrate of CYP1A2 (minor), CYP2B6 (minor), CYP2D6 (minor), CYP3A4 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Acetylcholinesterase Inhibitors: May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Risk C: Monitor therapy

Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Alcohol (Ethyl): May enhance the CNS depressant effect of Orphenadrine. Risk X: Avoid combination

Alizapride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Amantadine: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Risk C: Monitor therapy

Azelastine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Botulinum Toxin-Containing Products: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Botulinum Toxin-Containing Products: Muscle Relaxants (Centrally Acting) may enhance the adverse/toxic effect of Botulinum Toxin-Containing Products. Specifically, the risk for increased muscle weakness may be enhanced. Risk C: Monitor therapy

Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Bromopride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Bromperidol: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Risk C: Monitor therapy

Cannabinoid-Containing Products: CNS Depressants may enhance the CNS depressant effect of Cannabinoid-Containing Products. Risk C: Monitor therapy

Chlorphenesin Carbamate: May enhance the adverse/toxic effect of CNS Depressants. Risk C: Monitor therapy

Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Risk X: Avoid combination

CNS Depressants: May enhance the CNS depressant effect of Orphenadrine. Risk X: Avoid combination

DexmedeTOMIDine: CNS Depressants may enhance the CNS depressant effect of DexmedeTOMIDine. Management: Monitor for increased CNS depression during coadministration of dexmedetomidine and CNS depressants, and consider dose reductions of either agent to avoid excessive CNS depression. Risk D: Consider therapy modification

Difelikefalin: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Dimethindene (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Risk X: Avoid combination

Flunarizine: CNS Depressants may enhance the CNS depressant effect of Flunarizine. Risk X: Avoid combination

Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Risk C: Monitor therapy

Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Risk C: Monitor therapy

Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Risk X: Avoid combination

Glycopyrronium (Topical): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Risk C: Monitor therapy

Ixabepilone: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Kava Kava: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Kratom: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Risk X: Avoid combination

Lisuride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Lofexidine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Metoclopramide: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

MetyroSINE: CNS Depressants may enhance the sedative effect of MetyroSINE. Risk C: Monitor therapy

Minocycline (Systemic): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Risk C: Monitor therapy

Nabilone: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Nitroglycerin: Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. Risk C: Monitor therapy

Olopatadine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Oxomemazine: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Risk X: Avoid combination

Piribedil: CNS Depressants may enhance the CNS depressant effect of Piribedil. Risk C: Monitor therapy

Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Risk X: Avoid combination

Potassium Citrate: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium citrate. Risk X: Avoid combination

Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Risk C: Monitor therapy

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Risk X: Avoid combination

Procarbazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Risk C: Monitor therapy

Revefenacin: Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. Risk X: Avoid combination

Rivastigmine: Anticholinergic Agents may diminish the therapeutic effect of Rivastigmine. Rivastigmine may diminish the therapeutic effect of Anticholinergic Agents. Management: Use of rivastigmine with an anticholinergic agent is not recommended unless clinically necessary. If the combination is necessary, monitor for reduced anticholinergic effects. Risk D: Consider therapy modification

Ropeginterferon Alfa-2b: CNS Depressants may enhance the adverse/toxic effect of Ropeginterferon Alfa-2b. Specifically, the risk of neuropsychiatric adverse effects may be increased. Management: Avoid coadministration of ropeginterferon alfa-2b and other CNS depressants. If this combination cannot be avoided, monitor patients for neuropsychiatric adverse effects (eg, depression, suicidal ideation, aggression, mania). Risk D: Consider therapy modification

ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Risk C: Monitor therapy

Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Risk C: Monitor therapy

Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Risk C: Monitor therapy

Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid concomitant use of anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of secretin. Risk D: Consider therapy modification

Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Risk X: Avoid combination

Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Risk C: Monitor therapy

Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Risk X: Avoid combination

Tolperisone: May enhance the adverse/toxic effect of Muscle Relaxants (Centrally Acting). Management: Monitor for increased sedation or CNS effects if tolperisone is combined with other centrally acting muscle relaxants. Consider decreasing the tolperisone dose if these agents are combined. Risk D: Consider therapy modification

Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Valerian: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Pregnancy Considerations

Animal reproduction studies have not been conducted.

Mechanism of Action

As an antihistamine, anticholinergic, and NMDA receptor antagonist, the exact mechanism of action in musculoskeletal pain is unknown, but may be related to analgesic properties. Orphenadrine does not directly relax skeletal muscles (Cheah 2020; manufacturer's labeling).

Pharmacokinetics (Adult Data Unless Noted)

Onset of effect: Peak effect: Oral: 2 to 4 hours

Duration: 4 to 6 hours

Protein binding: 20%

Metabolism: Extensively hepatic

Half-life elimination: 14 to 16 hours

Excretion: Primarily urine (8% as unchanged drug)

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AE) United Arab Emirates: Norflex;
  • (AR) Argentina: Distalene;
  • (AU) Australia: Disipal | Norflex;
  • (BE) Belgium: Disipal | Norflex;
  • (CH) Switzerland: Norflex;
  • (CL) Chile: Plenactol;
  • (DE) Germany: Norflex | Orphenadrin;
  • (DO) Dominican Republic: Norflex;
  • (EC) Ecuador: Norflex;
  • (EE) Estonia: Norflex;
  • (EG) Egypt: Norflex;
  • (FI) Finland: Disipal | Norflex | Orfen | Parekin;
  • (FR) France: Disipal;
  • (GB) United Kingdom: Disipal | Norflex | Orphenadrine;
  • (GR) Greece: Disipal | Norflex;
  • (HK) Hong Kong: Norflex | Tensionlex;
  • (IE) Ireland: Disipal | Norflex;
  • (IL) Israel: Flexin;
  • (IN) India: Orphipal;
  • (IT) Italy: Disipal;
  • (JO) Jordan: Norflex;
  • (KE) Kenya: Norflex;
  • (KR) Korea, Republic of: Mesansin | Oldrin | Openadin sr | Opherine | Opheryl sr | Orasin | Orphedrine | Orphenadrine | Orpheran | Orpheraxin | Orpherin | Orpherine | Orpheryl | Otid | Phenacin | Scodrine | Slaxin | Terilax | Terirax xl;
  • (KW) Kuwait: Norflex;
  • (LB) Lebanon: Norflex | Orgasipal;
  • (LT) Lithuania: Disipal;
  • (LU) Luxembourg: Disipal | Norflex;
  • (LV) Latvia: Disipal;
  • (MX) Mexico: Norflex;
  • (MY) Malaysia: Norflex | Onadrine;
  • (NG) Nigeria: Epicoflex | Hicloflex | Norflex | Norpiflex;
  • (NL) Netherlands: Orfenadrine hcl;
  • (NO) Norway: Disipal | Lysantin;
  • (NZ) New Zealand: Disipal | Norflex;
  • (PE) Peru: Efaflex | Flamamed | Flexen | Miodrol | Norflex | Orfedrin | Orfelax | Orfenadrina | Orfenadrina citrato | Orfenadrina citrato mf | Pleren | Rexalgan;
  • (PK) Pakistan: Norflex | Orphenalax;
  • (PL) Poland: Disipal;
  • (PR) Puerto Rico: Flexor | Norflex;
  • (PT) Portugal: Norflex;
  • (SE) Sweden: Disipal | Norflex;
  • (SG) Singapore: Norflex;
  • (SI) Slovenia: Norflex;
  • (TH) Thailand: Norflex | Ofee | Omyphen | Orphena | Orphenadrine | Osphrine | Phemax;
  • (TW) Taiwan: Norflex | Tensionlex | Zinpin;
  • (UY) Uruguay: Efaflex | Norflex | Orfenadrina;
  • (VE) Venezuela, Bolivarian Republic of: Norflex;
  • (ZA) South Africa: Disipal | Norflex | Phenerine
  1. 2023 American Geriatrics Society Beers Criteria Update Expert Panel. American Geriatrics Society 2023 updated AGS Beers Criteria for potentially inappropriate medication use in older adults. J Am Geriatr Soc. 2023;71(7):2052-2081. doi:10.1111/jgs.18372 [PubMed 37139824]
  2. American Pain Society. Principles of Analgesic Use. 7th ed. American Pain Society; 2016.
  3. Cheah KY, Mah KY, Pang LH, et al. A randomized single-dose, two-period crossover bioequivalence study of two fixed-dose paracetamol/orphenadrine combination preparations in healthy volunteers under fasted condition. BMC Pharmacol Toxicol. 2020;21(1):45. doi:10.1186/s40360-020-00416-3 [PubMed 32576287]
  4. Chou R, Deyo R, Friedly J, et al. Systemic pharmacologic therapies for low back pain: a systematic review for an American College of Physicians clinical practice guideline. Ann Intern Med. 2017;166(7):480-492. doi:10.7326/M16-2458 [PubMed 28192790]
  5. Collins SR. Elsevier’s 2024 Intravenous Medications. 40th ed. Elsevier Health Sciences; 2023.
  6. Orphenadrine citrate ER tablets [prescribing information]. Princeton, NJ: Sandoz Inc; September 2009.
  7. Orphenadrine citrate injection [prescribing information]. Berkely Heights, NJ: Hikma; December 2019.
  8. van Tulder MW, Touray T, Furlan AD, Solway S, Bouter LM; Cochrane Back Review Group. Muscle relaxants for nonspecific low back pain: a systematic review within the framework of the Cochrane Collaboration. Spine (Phila Pa 1976). 2003;28(17):1978-1992. doi:10.1097/01.BRS.0000090503.38830.AD [PubMed 12973146]
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