Examining the uses and side effects of baclofen tablets

In recent decades, extensive efforts have been made in the field of research and development of drugs in order to improve the quality of life of people and treat various disorders. One of the drugs used as an auxiliary tool in the treatment of various disorders is baclofen. Baclofen is known as an agonist of beta receptors in the central nervous system and was originally used as a drug to lower blood pressure. But recent studies have shown that this drug has wider capabilities, including the treatment of addiction disorders, anxiety disorders and even some behavioral disorders.

Pharmaceutical forms of baclofen

All chemical and herbal medicines available in pharmacies are produced in different pharmaceutical forms according to the needs of doctors and patients. Baclofen in pharmaceutical forms including tablets 5 mg (generic), 10 mg (generic) and 20 mg (generic), oral solution 5 mg and 5 ml (Ozobax), oral suspension 25 mg and 5 ml (Fleqsuvy), 5, 10, and 20 mg oral granules, preservative-free intrathecal solution 500 mcg/mL (generic, Livorsal, Gablofen), 1,000 mcg/mL, 2,000 mcg/mL are available.

Uses of baclofen tablets

One of the main uses of this drug is in spasticity (muscle stiffness). This drug is suitable for spasticity caused by multiple sclerosis, especially for the relief of flexor spasm and accompanying pain, clonus and muscle stiffness. This product has great value in patients with spinal lesions and other spinal diseases, and it is also used as a muscle relaxant. It should also be noted that baclofen is used in children with spasticity with cerebral palsy and spasticity. Patients should strictly avoid using this product on their own without a doctor’s prescription.

Pharmacological effects and mechanism of action of baclofen

The exact mechanism of action of baclofen is not fully understood. This drug inhibits both monosynaptic and polysynaptic reflexes at the spinal level. This process probably takes place by reducing the release of excitatory neurotransmitters from afferent terminals. Although actions at supraspinal sites may also occur and contribute to its clinical effect. The absorption of this drug is 6 to 8 hours and the clearance is 30 ml per hour (IT) and its excretion is through urine and feces (85%; no change).

Dosage of baclofen tablets

The dosage is as follows:

Dosage of oral baclofen

1. It is suitable for spasticity caused by multiple sclerosis, especially for the relief of flexor spasms and accompanying pain, clonus and muscle stiffness.
2. Ozobax and Fleqsuvy may be of value in patients with spinal cord lesions and other spinal disorders.
3. Dosage should be 5 mg PO TID initially and after 3 days, the dose may be gradually increased by 5 mg every 3 days to 20 mg PO TID based on clinical response and tolerability.
4. The consumption of this product should not exceed 80 mg per day.

Dosage of intrathecal baclofen

1. Management of severe spasticity of spinal cord origin (eg, spinal cord injury, multiple sclerosis) or brain origin (eg, cerebral palsy, traumatic brain injury) is considered as an alternative to invasive neurosurgical procedures.
2. Titration (after the initial 24 hours) in the initial dose of the implant: 2 times the screening dose that gave a positive effect should be administered in a 24-hour period.
3. Spasticity of spinal origin: increase by 10 to 30% every 24 hours to achieve a favorable clinical effect.
4. Spasticity of cerebral origin: increase by 5-15% every 24 hours to achieve a favorable clinical effect.

Time to take baclofen

Considering that this drug is mainly excreted unchanged through the kidneys, the physician should consider dose modifications for the patient’s prescription considering renal impairment. Note that you should avoid excessive and non-prescription use of baclofen tablets, the time of use of this drug should be prescribed according to the patient’s physical condition, age (adults, children and the elderly) and medical records. This medicine is not recommended for skeletal muscle spasms caused by rheumatic disorders.

Time to take oral baclofen tablets in children

1. It is suitable for spasticity caused by multiple sclerosis, especially for the relief of flexor spasm with pain, clonus and muscle stiffness.
2. Ozobax: This product has great value in patients with spinal lesions and other spinal diseases.
3. The safety and effectiveness of this drug in children under 12 years old has not been proven.
4. In people over 12 years of age, start with a low dose, preferably in different PO doses.
5. Initially with 5 mg and after 3 days gradually increasing the dose by 5 mg every 3 days up to 20 mg PO TID based on clinical response and tolerance. (only by doctor’s order)
6. This product can be increased up to a maximum of 80 mg per day by the doctor if needed.

Time to take intrathecal baclofen tablets in children

1. Management of severe spasticity of spinal cord origin (such as spinal cord injury, multiple sclerosis) or cerebral origin (such as cerebral palsy, traumatic brain injury) in patients older than 4 years may be considered as an alternative to neurosurgical procedures.
2. In the screening phase, a test bolus: 50 micrograms is administered intrathecally to the patient with the barbatage method within 1 minute. If there is no response, take up to 75 mcg 24 hours later, and if still not enough, take 100 mcg 24 hours later.
3. Titration (after the initial 24 hours) Initial implant dose: 2 times the screening dose that gave a positive effect should be administered within 24 hours.
4. After the first 24 hours, the daily dose should be slowly increased by 5-15% only once every 24 hours, until the desired clinical effect is achieved.

Precautions

Do not stop taking this medicine without consulting your doctor. If this drug is stopped suddenly, serious (rarely dangerous) problems may occur. If after stopping this medicine, symptoms such as itching, numbness and tingling of the skin, high fever, mental or mood changes (such as confusion), convulsions, worsening of muscle stiffness, symptoms of kidney problems, etc., inform the doctor immediately. If you have ever had a reaction to stop taking baclofen, consult your doctor before taking it.

1. Use with caution in patients who have had a stroke.
2. Not recommended for spasms with rheumatic disease, stroke, Parkinson’s.
3. It is better to take it with food to avoid stomach upset.
4. Use with caution in seizure disorders and kidney failure.
5. Abrupt discontinuation of the drug has resulted in adverse reactions including hallucinations, seizures, high fever, altered mental status, exaggerated rebound spasticity, and muscle stiffness, rarely leading to rhabdomyolysis, multiple organ system failure, and death.
6. May cause acute urinary retention associated with underlying disease. For this reason, it should be used with caution in patients with urinary obstruction.
7. Use with caution in patients with a history of autonomic dysreflexia. The presence of pain stimuli or their sudden cessation may cause an episode of autonomic dysreflexia.

Contraindications for baclofen tablets

1. Abrupt discontinuation of intrathecal baclofen has resulted in high fever, altered mental status, excessive rebound spasticity, and muscle stiffness, rarely leading to rhabdomyolysis, multiple organ system failure, and death.
2. Preventing sudden shutdowns requires careful attention to injection system planning and monitoring, timing and refilling procedures, and pump alarms. Advise patients and caregivers about the importance of scheduled refill visits and education about early signs of baclofen withdrawal.
3. Pay more attention to patients who are at apparent risk such as spinal cord injury at T-6 or higher, communication problems, history of withdrawal symptoms from oral or intrathecal baclofen, etc.

Side effects of baclofen tablets

Some of the side effects of this product include drowsiness, dizziness, weakness, headache, constipation, nausea or vomiting. If any of these effects persist or worsen, tell your doctor or pharmacist right away. Remember that this medication has been prescribed because your doctor has determined that the benefits to you are greater than the risk of side effects. Most patients who take this drug do not have serious side effects. However, some of the most important side effects of baclofen include the following.

Oral side effects

1. Drowsiness
2. dizziness weakness
3. nausea
4. hypotonia
5. tiredness
6. blood pressure
7. Headache
8. insomnia
9. Constipation and frequent urination

Intrathecal side effects

1. Urinary retention
2. Dizziness or seizures
3. Nausea and vomiting
4. Headache
5. Constipation and diarrhea
6. blood pressure
7. Pain and speech disorder
8. dry mouth
9. Increased salivation
10. Amblyopia

Baclofen drug interactions

Drug interactions may change how your medications work or increase your risk of serious side effects. Before going to the doctor, patients should prepare a list of the herbal and chemical medicines they use and show it to the doctor. Drugs (cannabis), sleep or anxiety drugs (such as alprazolam, lorazepam, zolpidem), other muscle relaxants (such as carisoprodol, cyclobenzaprine), or antihistamines (such as cetirizine, diphenhydramine) and… may cause drug interactions with this product. Be sure to tell your doctor about the medications you are taking before taking them.

Taking baclofen tablets during pregnancy and breastfeeding

There is not enough information about the risk of using this drug in pregnant women. Based on animal data, the oral administration of baclofen to pregnant rats led to an increase in the incidence of fetal structural abnormalities, which was also associated with maternal toxicity. All medicines used during pregnancy must be prescribed according to the doctor’s prescription, excessive use without a doctor’s prescription can cause side effects in the fetus and mother. Although there are no specific reports of dangerous side effects for pregnant women, excessive use of this drug without a prescription can be dangerous.

The effect of baclofen on breastfeeding

At recommended oral doses, baclofen is present in human milk. Also, no human data are available on the effects of this drug on breast milk production. If the medicine runs out, the prescription or it is suddenly stopped, we may see withdrawal symptoms in infants. Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need and any possible adverse effects on the nursing infant or the mother’s underlying medical condition. Note that pregnant women or nursing mothers should strictly avoid using this medicine without a prescription.

Storage conditions for baclofen tablets

Keep baclofen tablets out of the reach of children and animals. This product should be stored in a dry and cool place away from heat and light. Dispose of this product properly when it has expired or is no longer needed. Avoid pouring medicine into the street, toilet well and sewer.

The last word of baclofen medicine

As we mentioned in this article from the Green Positive Online Pharmacy magazine, baclofen is a widely used drug for the treatment of muscle spasm, which has generally been safe and effective in patients. However, the elderly, those with certain medical conditions or history, and those with kidney disorders should use this medicine with caution. Common side effects of baclofen include drowsiness, dizziness, weakness and fatigue, and of course more serious side effects, such as decreased level of consciousness, seizures and coma, which occur if the contraindications and precautions are not followed. If you experience any serious side effects, you should consult your doctor.

Source: site Medscape

Frequently asked questions about baclofen