Orphenadrine Citrate, Uses, Side effects, Dosage, and brands etc

Introduction

Orphenadrine citrate is a medication primarily used as a muscle relaxant and pain reliever. It belongs to a class of drugs known as anticholinergic agents, which work by blocking the action of acetylcholine, a neurotransmitter involved in muscle contractions. Orphenadrine citrate is prescribed to alleviate muscle spasms and stiffness associated with musculoskeletal conditions, such as back pain, neck pain, and muscle injuries.

Orphenadrine citrate is available in various formulations, including tablets and injections, and is typically administered orally. It is usually part of a comprehensive treatment plan that includes rest, physical therapy, and other medications.

In addition to its muscle relaxant properties, orphenadrine citrate also possesses mild analgesic (pain-relieving) effects, further contributing to its efficacy in managing musculoskeletal pain.

History

The development of orphenadrine citrate is attributed to the work of George Rieveschl, a professor of chemistry at the University of Cincinnati. Rieveschl led a research program focused on antihistamines, and in 1943, one of his students, Fred Huber, synthesized diphenhydramine, which became the basis for the antihistamine Benadryl.

Rieveschl collaborated with Parke-Davis to test diphenhydramine, and the company licensed the patent from him. In 1947, Parke-Davis hired Rieveschl as their Director of Research. During his time there, Rieveschl led the development of orphenadrine, an analog of diphenhydramine. Orphenadrine was an anticholinergic drug closely related to diphenhydramine.

Before the development of other drugs like amantadine in the late 1960s, anticholinergics like orphenadrine were commonly used as the mainstay of treatment for Parkinson’s disease.

The work of George Rieveschl and the development of orphenadrine citrate have contributed to the field of pharmacology and the treatment of muscle spasms and associated conditions.

Mechanism of Action

Orphenadrine citrate exerts its pharmacological effects through multiple mechanisms of action. While the exact mode of action is not fully understood, the available research suggests the following:

Orphenadrine citrate is an anticholinergic drug that acts as a muscle relaxant. It has a high affinity for sodium-dependent reuptake into presynaptic terminals, which terminates the action of noradrenaline. This action contributes to its muscle relaxant properties and helps alleviate muscle pain and discomfort associated with strains, sprains, and other muscle injuries

Orphenadrine citrate also possesses anticholinergic activity, which means it blocks the effects of acetylcholine, a neurotransmitter involved in muscle contractions. By changing the way the body senses muscle pain, orphenadrine citrate helps relieve stiffness, pain, and discomfort.

Uses of Orphenadrine Citrate

Orphenadrine citrate is primarily used to treat muscle spasms and associated pain. It is often prescribed in combination with rest, physical therapy, and other treatments. Here are the main uses of orphenadrine citrate:

Muscle Spasms and Pain

Orphenadrine citrate is used to alleviate muscle spasms and associated pain caused by strains, sprains, or other muscle injuries. It helps relax certain muscles in the body, providing relief from stiffness, discomfort, and pain.

Adjunctive Treatment

Orphenadrine citrate is typically used in conjunction with rest, physical therapy, and other measures to enhance the effectiveness of treatment for muscle spasms and pain. It is not meant to be the sole treatment but rather a part of a comprehensive approach to managing musculoskeletal conditions.

Treatment of Musculoskeletal Disorders

It is commonly prescribed for the management of musculoskeletal disorders like fibromyalgia, rheumatoid arthritis, and osteoarthritis. Orphenadrine citrate helps to relieve the associated muscle stiffness, soreness, and discomfort.

Relief of Acute Torticollis

Orphenadrine citrate is often employed for the symptomatic relief of acute torticollis, commonly known as “wry neck.” It helps to relax the muscles of the neck and shoulder, reducing pain and improving range of motion.

Management of Spinal Cord Injury Symptoms

In cases of spinal cord injury, where muscle spasticity and rigidity are prevalent, orphenadrine citrate can be utilized to alleviate symptoms and improve mobility. It aids in reducing muscle tone and promoting comfort.

Treatment of Acute Back Pain

Orphenadrine citrate is prescribed for the short-term management of acute back pain, particularly when associated with muscle spasms. It helps to mitigate pain intensity and improve functional mobility during the acute phase of injury.

Off-label Uses

In addition to its approved indications, orphenadrine citrate may be used off-label for conditions such as tension headaches and migraine-associated muscle tension, though its efficacy for these purposes may vary.

Dosage

The dosage of orphenadrine citrate can vary depending on the individual’s age, medical condition, and response to treatment. Here is a general guideline for dosing:

Adults

For the treatment of muscle spasms and associated pain, the usual oral dosage is 100 mg of orphenadrine citrate two to three times daily, with the maximum recommended daily dose not exceeding 400 mg.

Elderly

Due to the increased risk of adverse effects in the elderly population, lower initial doses may be recommended, typically starting with 50 mg of orphenadrine citrate two to three times daily, with gradual dose titration based on individual response and tolerance.

Pediatric Population

Orphenadrine citrate is not typically recommended for use in children under 12 years of age due to limited safety and efficacy data in this population.

Side effects

Orphenadrine citrate, like any medication, can potentially cause side effects, ranging from mild to severe. It’s important to note that not everyone experiences these side effects, and some individuals may experience different reactions than others. Here are some common side effects associated with orphenadrine citrate:

Drowsiness: One of the most common side effects of orphenadrine citrate is drowsiness or sedation. This impairs cognitive and motor skills, affecting the ability to drive or operate machinery safely.

Dry Mouth: Orphenadrine citrate causes dry mouth, which is uncomfortable. Drinking water or using sugar-free gum or candy may help alleviate this symptom.

Blurred Vision: Some individuals experience blurred vision or difficulty focusing while taking orphenadrine citrate. It’s essential to avoid activities requiring clear vision until the effects subside.

Constipation: It causes constipation in some individuals. Increasing fluid intake and consuming fiber-rich foods may help alleviate this side effect.

Urinary Retention: It impairs bladder function, leading to difficulty urinating or urinary retention. If severe or persistent, medical attention should be sought.

Dizziness: Dizziness or lightheadedness may occur, especially when standing up quickly from a sitting or lying position. Taking precautions to change positions slowly helps reduce the risk of falls.

Nausea and Vomiting: Some individuals may experience nausea or vomiting while taking orphenadrine citrate. Taking the medication with food or dividing the dose may help minimize gastrointestinal upset.

Headache: Headaches are a potential side effect of orphenadrine citrate. If headaches become severe or persistent, medical advice should be sought.

Confusion or Delirium: In some cases, particularly in elderly individuals, this drug may cause confusion, disorientation, or delirium. Close monitoring is necessary, and any changes in mental status should be reported to a healthcare professional promptly.

Allergic Reactions: Although rare, allergic reactions to orphenadrine citrate can occur. Symptoms may include rash, itching, swelling, severe dizziness, or difficulty breathing. Immediate medical attention is necessary if an allergic reaction is suspected.

Drugs interaction

Orphenadrine citrate, a muscle relaxant used to treat muscle spasms and pain, may interact with other drugs. Here are some important points about drug interactions with it:

Orphenadrine citrate can cause drowsiness. It is important to avoid taking other medications that can also cause drowsiness, such as opioid pain or cough relievers (codeine, hydrocodone), alcohol, marijuana (cannabis), sleep or anxiety medications (alprazolam, lorazepam, zolpidem), other muscle relaxants (carisoprodol, cyclobenzaprine), and antihistamines (cetirizine, diphenhydramine). It is recommended to check the labels on all your medicines, including allergy or cough-and-cold products, as they may contain ingredients that cause drowsiness. Consult with your pharmacist about using these products safely

Orphenadrine citrate may interact with other medications, including prescription and over-the-counter medicines, vitamins, and herbal products. It is important to inform your healthcare provider about all the medicines you are currently using, including any changes in medication.

According to Drugs.com, there are 393 drugs known to interact with orphenadrine citrate. These interactions include 32 major interactions, 360 moderate interactions, and 1 minor interaction. It is important to consult with your healthcare provider or pharmacist to understand the specific interactions and their potential impact.

This medicine may interact with antipsychotics and sibutramine, among other medications. It is important to discuss any potential drug interactions with your healthcare provider before starting or stopping any medication.

Contraindications

Orphenadrine citrate has certain contraindications, which are situations or conditions in which the use of the medication is not recommended. Here are the contraindications for orphenadrine citrate:

• Hypersensitivity: Orphenadrine citrate is contraindicated in patients who have demonstrated a previous hypersensitivity to the drug. If you have experienced an allergic reaction or hypersensitivity to it in the past, it is important to avoid using this medication.
• Glaucoma: Orphenadrine citrate extended-release tablets are contraindicated in patients with glaucoma
• Pyloric or Duodenal Obstruction: This drug is contraindicated in patients with pyloric or duodenal obstruction.
• Stenosing Peptic Ulcers: It is contraindicated in patients with stenosing peptic ulcers
• Prostatic Hypertrophy or Obstruction of the Bladder Neck: This medication is contraindicated in patients with prostatic hypertrophy or obstruction of the bladder neck.
• Cardio-Spasm (Mega-Esophagus): It is contraindicated in patients with cardio-spasm (mega-esophagus)
• Gravis: This medication is contraindicated for patients with myasthenia gravis.

Warnings and Precautions

Orphenadrine citrate, a muscle relaxant used to treat muscle spasms and pain, has certain warnings, and precautions that should be considered. Here are some important points:

• Allergies: Before taking orphenadrine citrate, it is important to inform your doctor or pharmacist if you are allergic to it or if you have any other allergies. This medication may contain inactive ingredients that can cause allergic reactions or other problems
• Inactive Ingredients: Orphenadrine citrate products may contain inactive ingredients, such as sulfites, which can cause allergic reactions or other issues. It is advisable to consult with your pharmacist for more details about the specific inactive ingredients in the product you are using
• Pregnancy and Nursing: The use of orphenadrine citrate during pregnancy, nursing, or administering it to children or the elderly should be done under the guidance of a healthcare professional. It is important to consult with your healthcare provider for personalized advice regarding the use of this medication in these situations.
• Other Measures: Orphenadrine citrate is usually used as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute painful musculoskeletal conditions. It is important to follow the prescribed treatment plan and consult with your healthcare provider for guidance on the appropriate use of it.

Brands in Pakistan

Orphenadrine citrate is sold under many brand names in Pakistan. Here is a list of the most common brands:

NUBEROL FORTE

• Manufacturer: SEARLE PAKISTAN (PVT.) LTD.
• Trade Price: 61.20
• Retail Price: 72.00

ANOROL FORTE

• Manufacturer: MEDERA PHARMACEUTICALS (PVT) LTD.
• Trade Price: 29.75
• Retail Price: 35.00

CENADRIN

• Manufacturer: AKSON PHARMACEUTICALS (PVT) LTD.
• Trade Price: 29.75
• Retail Price: 35.00

GENBROL

• Manufacturer: GENIX PHARMA (PVT) LTD
• Trade Price: 35.00
• Retail Price: 35.00

GLORAL

• Manufacturer: GLOBAL PHARMACEUTICALS
• Trade Price: 29.75
• Retail Price: 35.00

MEDIGESIC FORTE

• Manufacturer: WILSHIRE LABORATORIES (PVT) LTD.
• Trade Price: 50.15, 150.45, 501.15
• Retail Price: 59.00, 177.00, 590.00

MUSEADOL FORTE

• Manufacturer: LISKO PAKISTAN (PVT) LTD
• Trade Price: 35.00
• Retail Price: 35.00

ORPHENAMED

• Manufacturer: MEDIFINE LABORATORIES
• Trade Price: 29.75
• Retail Price: 35.00

P-ORPH

• Manufacturer: SWISS PHARMACEUTICALS (PVT) LTD.
• Trade Price: 0.00
• Retail Price: 35.00

PAINCURE FORT

• Manufacturer: JAWA PHARMACEUTICALS (PVT) LTD.
• Trade Price: 0.00
• Retail Price: 0.00

PANGESIC FORTE

• Manufacturer: PANACEA PHARMACEUTICALS
• Trade Price: 0.00
• Retail Price: 22.00

SAMEROL-N FORTE

• Manufacturer: SAMI PHARMACEUTICALS (PVT) LTD.
• Trade Price: 35.05
• Retail Price: 41.24

Brands in Other countries

The most common brands of orphenadrine citrate all over the world are:

1. Norflex
2.  Norgesic
3. Norgesic Forte