Generic Flexeril

Product Name	Price	Shipping	Total	Order
Cyclobenzaprine 10mg (Gen. for Flexeril) 120 Tabs	$149	free	$149	Order
Cyclobenzaprine 10mg (Gen. for Flexeril) 180 Tabs	$159	free	$159	Order

Cyclobenzaprine is a muscle relaxant. It works by blocking nerve impulses (or pain sensations) that are sent to your brain.

Cyclobenzaprine is used together with rest and physical therapy to treat skeletal muscle conditions such as pain or injury.

Cyclobenzaprine may also be used for purposes not listed in this medication guide.

Cyclobenzaprine, a medication with a structural resemblance to tricyclic antidepressants, operates centrally as a skeletal muscle relaxant. It is a tricyclic amine salt that exerts its effects within the central nervous system (CNS) to alleviate excessive muscle activity. The clinical applications of cyclobenzaprine are detailed below.

FDA-Approved Use

Cyclobenzaprine is sanctioned by the FDA for its role as an adjunct to rest and physical therapy in the alleviation of muscle spasms linked to acute, painful musculoskeletal conditions, for short-term use. It is important to note that cyclobenzaprine should only be employed for brief durations, typically up to 2 or 3 weeks. This limitation is due to the absence of substantial evidence supporting its efficacy for extended usage, as muscle spasms associated with acute, painful musculoskeletal conditions are typically of short duration. Prolonged therapy with this medication is seldom necessary.

Off-label Clinical Uses

1. Fibromyalgia Management: The American College of Rheumatology recommends duloxetine, milnacipran, and pregabalin as the primary treatment options for fibromyalgia. Additionally, cyclobenzaprine may offer potential benefits in addressing associated insomnia.
2. Myofascial Pain Resulting from Temporomandibular Disorders:
3. Exploring New Horizons: In a recent randomized controlled trial, sublingual administration of cyclobenzaprine showed promise in reducing symptoms associated with posttraumatic stress disorder (PTSD) while also enhancing sleep quality and psychosocial functioning. It is important to note that this is preliminary evidence, and further extensive research is essential to establish its efficacy.

Cyclobenzaprine’s Mechanism of Action

Cyclobenzaprine is a centrally acting skeletal muscle relaxant that bears a structural resemblance to tricyclic antidepressants. It alleviates skeletal muscle spasms originating locally without impeding muscle function. Preclinical studies have demonstrated that cyclobenzaprine effectively reduces hyperactivity in skeletal muscles. Current research suggests that its primary mode of action occurs within the central nervous system, particularly in the brain stem.

Cyclobenzaprine does not exert a direct influence on skeletal muscles or the neuromuscular junction. However, it may have an overlapping effect on the spinal cord, which contributes to its overall skeletal muscle relaxant properties. Available evidence suggests that the resulting impact of cyclobenzaprine involves a reduction in tonic somatic motor activity, affecting both the gamma (γ) and alpha (α) motor systems. Recent research also indicates that cyclobenzaprine acts as a receptor antagonist for the 5-HT2 receptor, which is responsible for its antispasmodic effect.

In clinical practice, cyclobenzaprine proves effective in relieving muscle spasms, diminishing local pain and tenderness, and enhancing the range of motion in cases of acute, painful musculoskeletal conditions. However, it’s important to note that cyclobenzaprine is not intended for the treatment of spasticity associated with cerebral or spinal cord pathology or for use in children with cerebral palsy, as it is not classified as an antispasticity medication.

Cyclobenzaprine is a centrally acting muscle relaxant, and its precise mechanism of action is not fully understood. However, it is believed to work by affecting the central nervous system (CNS) to reduce muscle hyperactivity and relieve muscle spasms. Some key aspects of its mechanism of action include:

1. Inhibition of Reflexes: Cyclobenzaprine appears to inhibit certain reflexes in the spinal cord, which can reduce muscle contractions and spasms.
2. Sedative Effect: It has a sedative effect on the CNS, which may help patients relax and alleviate muscle tension.
3. Potential Tricyclic Antidepressant Properties: Cyclobenzaprine shares a structural similarity to tricyclic antidepressants, and this resemblance may contribute to its muscle-relaxing effects.
4. Limited Impact on Muscle Strength: Unlike some other muscle relaxants, cyclobenzaprine generally does not significantly weaken muscle strength.

Important Information About Not Taking Cyclobenzaprine

You should not use cyclobenzaprine if you have an allergy to the medication, a certain type of thyroid disorder (hyperthyroidism), heart block, congestive heart failure, a heart rhythm disorder, or you have recently had a heart attack.

Do not use cyclobenzaprine if you have taken an MAO inhibitor in the past 14 days, such as isocarboxazid, linezolid, phenelzine, rasagiline, selegiline, or tranylcypromine.

Cyclobenzaprine Pregnancy Warnings

US FDA pregnancy category: B

Embryofetal development in rats and rabbits given approximately 3 and 15 times, respectively, the maximum recommended human dose (MRHD) was not adversely effected. Dams receiving this drug at doses 3 times or more the MRHD during pregnancy and lactation, had pups with decreased body weight and survival. There are no adequate and controlled studies in pregnant women.

US FDA pregnancy category B: Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well-controlled studies in pregnant women.
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Cyclobenzaprine Breastfeeding Warnings

This drug has been shown to be excreted in rat milk and achieve concentrations in the milk which are 50% of those in the rat maternal plasma. As this drug is closely related to the tricyclic antidepressants, some of which are known to be excreted in human milk, use caution especially when other drugs that cause sedation are used simultaneously.

Caution is recommended.

Cyclobenzaprine Levels and Effects while Breastfeeding

Summary of Use during Lactation

Amounts of cyclobenzaprine in milk appear to be very small and two infants apparently tolerated the drug in milk well. If cyclobenzaprine is required by the mother, it is not a reason to discontinue breastfeeding. Monitor the infant for (drowsiness, adequate weight gain, and developmental milestones), especially in neonates and preterm infants and when using combinations of sedating drugs.

Drug Levels

Maternal Levels. Two mothers were taking chronic cyclobenzaprine therapy. One mother was taking 5 mg once daily for temporomandibular joint pain and the other mother was taking 10 mg twice daily for fibromyalgia pain. Each collected milk at 0, 1, 2, 4, 6, 8 and 12 hours after a dose. After the 5 mg dose, the peak milk level was 6.6 mcg/L and the average level was 2.2 mcg/L. After the 10 mg dose, the peak milk level was 24.5 mcg/L and the average level was 10.3 mcg/L. These amounts resulted in the respective infant dosages of 0.3 mcg/kg and 0.7 mcg/kg daily. In both cases, the weight-adjusted dosage was 0.5% of the maternal dosage.

Infant Levels. Relevant published information was not found as of the revision date.

Effects in Breastfed Infants

Two mothers were taking chronic cyclobenzaprine therapy. One mother was taking 5 mg once daily for temporomandibular joint pain and the other mother was taking 10 mg twice daily for fibromyalgia pain. The latter mother was also taking unspecified antidepressants, levothyroxine, zolpidem, alprazolam and famotidine. Both mothers were breastfeeding their infants (extent not stated). Neither infant had any noticeable adverse reaction such as sedation.[1]

A search was performed of the shared database of all U.S. poison control centers for the time period of 2001 to 2017 for calls regarding medications and breastfeeding. Of 2319 calls in which an infant was exposed to a substance via breast milk, 7 were classified as resulting in a major adverse effect, and one of these involved cyclobenzaprine. A 16-day-old infant was exposed to cyclobenzaprine, acetaminophen and oxycodone in breast milk. The infant was admitted to the hospital in a noncritical care unit for bradycardia, hypotension, and respiratory arrest. The dosages and extent of breastfeeding were not reported and the infant survived.

Effects on Lactation and Breast Milk

Relevant published information was not found as of the revision date.

Before taking Cyclobenzaprine

You should not use cyclobenzaprine if you are allergic to it, or if you have:

• hyperthyroidism;
• heart block, heart rhythm disorder, congestive heart failure; or
• if you have recently had a heart attack.

Cyclobenzaprine is not approved for use by anyone younger than 15 years old.

Do not use cyclobenzaprine if you have taken an MAO inhibitor in the past 14 days. A dangerous drug interaction could occur. MAO inhibitors include isocarboxazid, linezolid, phenelzine, rasagiline, selegiline, and tranylcypromine.

Some medicines can interact with cyclobenzaprine and cause a serious condition called serotonin syndrome. Be sure your doctor knows if you also take stimulant medicine, opioid medicine, herbal products, or medicine for depression, mental illness, Parkinson’s disease, migraine headaches, serious infections, or prevention of nausea and vomiting. Ask your doctor before making any changes in how or when you take your medications.

To make sure cyclobenzaprine is safe for you, tell your doctor if you have:

• thyroid disease;
• liver disease;
• glaucoma;
• enlarged prostate; or
• problems with urination.

It is not known whether cyclobenzaprine will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant.

It may not be safe to breast-feed while using this medicine. Ask your doctor about any risk.

Older adults may be more sensitive to the effects of this medicine.

Cyclobenzaprine is usually taken taken for up to 2 or 3 weeks. Follow all directions on your prescription label and read all medication guides or instruction sheets. Your doctor may occasionally change your dose.

Follow your doctor’s dosing instructions very carefully.

Swallow the capsule whole and do not crush, chew, break, or open it.

Call your doctor if your symptoms do not improve after 3 weeks, or if they get worse.

Store at room temperature away from moisture, heat, and light.

What Happens if I Miss a Dose?

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What Happens if I Overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222. An overdose of cyclobenzaprine can be fatal.

Overdose symptoms may include severe drowsiness, vomiting, fast heartbeats, tremors, agitation, or hallucinations.

What should I avoid while Taking Cyclobenzaprine?

Avoid driving or hazardous activity until you know how this medicine will affect you. Your reactions could be impaired.

Avoid drinking alcohol. Dangerous side effects could occur.

Cyclobenzaprine Side Effects

Get emergency medical help if you have signs of an allergic reaction to cyclobenzaprine: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Stop using this medicine and call your doctor at once if you have:

• fast or irregular heartbeats;
• chest pain or pressure, pain spreading to your jaw or shoulder; or
• sudden numbness or weakness (especially on one side of the body), slurred speech, balance problems.

Seek medical attention right away if you have symptoms of serotonin syndrome, such as: agitation, hallucinations, fever, sweating, shivering, fast heart rate, muscle stiffness, twitching, loss of coordination, nausea, vomiting, or diarrhea.

Serious side effects may be more likely in older adults.

Common cyclobenzaprine side effects may include:

• drowsiness, tiredness;
• headache, dizziness;
• dry mouth; or
• upset stomach, nausea, constipation.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Using cyclobenzaprine with other drugs that make you drowsy can worsen this effect. Ask your doctor before using opioid medication, a sleeping pill, a muscle relaxer, or medicine for anxiety or seizures.

Tell your doctor about all your other medicines, especially:

• MAO inhibitors, such as isocarboxazid, linezolid, phenelzine, rasagiline, selegiline, or tranylcypromine;
• Any antidepressant or anxiety medications;
• bupropion (Zyban, for smoking cessation or Wellbutrin, for depression);
• meperidine;
• tramadol;
• verapamil;
• cold or allergy medicine that contains an antihistamine (Benadryl and others);
• medicine to treat Parkinson’s disease;
• medicine to treat excess stomach acid, stomach ulcer, motion sickness, or irritable bowel syndrome;
• medicine to treat overactive bladder; or
• bronchodilator asthma medication.

This list is not complete. Other drugs may interact with cyclobenzaprine, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible drug interactions are listed here.

Management of Toxicity of Cyclobenzaprine

Cyclobenzaprine toxicity can occur when an individual takes an excessive dose of the medication, either intentionally or unintentionally. Managing such cases involves several steps to mitigate the potential adverse effects. Here are the key components of managing cyclobenzaprine toxicity:

1. Assessment: Begin by assessing the patient’s condition, including vital signs, level of consciousness, and any symptoms or signs of toxicity. Gather information on the amount and time of ingestion, as well as any co-ingestants.
2. Supportive Care:
   • Ensure a patent airway and provide adequate oxygenation.
   • Administer intravenous fluids to maintain hydration.
   • Monitor vital signs, especially heart rate and blood pressure, and provide supportive care as needed.
3. Gastric Lavage or Activated Charcoal: Consider gastric lavage (stomach pumping) or activated charcoal administration within the first hour of ingestion for individuals who have ingested a substantial amount of cyclobenzaprine. These procedures can help limit further absorption.
4. Benzodiazepines: In cases of severe agitation or seizures, benzodiazepines such as diazepam or lorazepam may be used to control these symptoms.
5. Cardiovascular Monitoring: Continuously monitor the patient’s cardiovascular status, as cyclobenzaprine can affect heart rate and blood pressure. If there are significant cardiac disturbances, treatment measures such as intravenous fluids, atropine, or other medications may be necessary.
6. Activated Charcoal: Activated charcoal can be administered to adsorb the remaining cyclobenzaprine and prevent further absorption, especially within the first few hours after ingestion.
7. Gastric Acid Reduction: Proton pump inhibitors or H2 blockers may be considered to reduce gastric acid secretion, which can help minimize the risk of gastric injury.
8. Consultation with a Poison Control Center: In all cases of cyclobenzaprine toxicity, consulting with a poison control center or a medical toxicologist is advisable. They can provide guidance on management and treatment options.
9. Psychiatric Evaluation: For cases of intentional overdose, a psychiatric evaluation should be conducted to assess the patient’s mental state and provide appropriate mental health support.
10. Monitoring: Continue monitoring the patient’s condition for any signs of deterioration or delayed effects, as cyclobenzaprine’s effects can last for an extended period.

Is Cyclobenzaprine Addictive ?

Cyclobenzaprine, also known by brand names such as Flexeril, is generally not considered to be addictive in the same way that drugs with a high potential for abuse, such as opioids or certain sedatives, are. It does not produce the same intense euphoria or craving that is typically associated with addictive substances. However, there are some important considerations to keep in mind:

1. Potential for Dependence: While cyclobenzaprine itself is not considered highly addictive, there have been reports of dependence or withdrawal symptoms in some individuals who have used it for an extended period. This is more likely to occur in cases of long-term or misuse of the medication.
2. Abuse Potential: In some cases, individuals may misuse cyclobenzaprine by taking higher doses than prescribed or using it in combination with other substances to enhance its sedative effects. This kind of misuse is a concern and can be associated with risks.
3. Tolerance: Over time, some individuals may develop a tolerance to the effects of cyclobenzaprine, requiring higher doses to achieve the same level of muscle relaxation. This can potentially lead to an increased risk of misuse or dependence.
4. Psychological Factors: While the medication itself may not be highly addictive, psychological factors, such as the perception of relief it provides or a placebo effect, can contribute to its continued use beyond the prescribed duration.
5. Medical Supervision: The best way to use cyclobenzaprine is under the supervision of a healthcare professional who can monitor its use and ensure it is taken as prescribed for the intended medical purpose. Following the prescribed dosage and duration of use is essential to minimize the risk of misuse and potential dependence.