Carisoprodol is a synthetic propanediol carbamate derivative and an adjunct in the treatment of painful muscle spasms, Carisoprodol is a centrally acting skeletal muscle relaxant that relieves stiffness, pain, and discomfort caused by muscle injuries. Its mechanism of action is not clear yet; perhaps due to its sedative actions. (NCI04)
Carisoprodol is a centrally acting muscle relaxant that has been in use for more than fifty years without significant evidence for causing hepatic injury. Carisoprodol is a centrally acting muscle relaxant that has been in use for more than fifty years without significant evidence for causing hepatic injury.
Mechanism of Action
Carisoprodol is a CNS depressant that has sedative and skeletal muscle relaxant effects. The precise mechanism of action of the drug is not known. The skeletal muscle relaxant effects of orally administered carisoprodol are minimal and are probably related to its sedative effect. The drug does not directly relax the skeletal muscle and, unlike neuromuscular blocking agents, does not depress neuronal conduction, neuromuscular transmission, or muscle excitability. In animals, carisoprodol appears to modify the central perception of pain without abolishing peripheral pain reflexes and to have slight antipyretic activity, but these effects have not been demonstrated in clinical studies.
Carisoprodol is an increasingly abused, centrally-acting muscle relaxant. Despite the prevalence of carisoprodol abuse, its mechanism of action remains unclear. Its sedative effects, which contribute to its therapeutic and recreational use, are generally attributed to the actions of its primary metabolite, meprobamate, at GABA(A) receptors (GABA(A)R). Meprobamate is a controlled substance at the federal level; ironically, carisoprodol is not currently classified as such. Using behavioral and molecular pharmacological approaches, we recently demonstrated carisoprodol, itself, is capable of modulating GABA(A)R function in a manner similar to central nervous system depressants. Its functional similarities with this highly addictive class of drugs may contribute to the abuse potential of carisoprodol. The site of action of cariso
Originally approved by the FDA in 1959, carisoprodol is a centrally acting muscle relaxant used in painful musculoskeletal conditions in conjunction with physical therapy and other medications [rx]. This drug is available by itself in an oral tablet or combined with aspirin or in a fixed-dose combination with both aspirin and codeine [rx,rx].
In January 2012, this drug was classified as a Schedule IV substance under the controlled substances act in several US states due to alarming rates of abuse [rx,rx] despite having a low potential for abuse in addition to a low risk of dependence [rx].
Indications of Carisoprodol
- Carisoprodol is indicated for the relief of discomfort related to acute, painful musculoskeletal conditions. Important limitations of use. Should only be used for acute treatment periods up to two or three weeks. Adequate evidence of effectiveness for more prolonged use has not been established.
- Carisoprodol is indicated for the relief of discomfort related to acute, painful musculoskeletal conditions.
- Should only be used for acute treatment periods up to two or three weeks
- Nocturnal Leg Cramps
- Muscle Spasm
- Postoperative muscle spasm
Contraindications of Carisoprodol
- Severely Decreased Platelets
- Having Thoughts of Suicide
- Persons. to drug class common.
- Avoid abrupt withdrawal
- Caution in elderly pts
- Renal impairment
- CHF class III, IV NYHA
- Angioedema
- Angioedema risk
- Depression
- CNS depressant use
- Alcohol use
- The decrease in the Sharpness of Vision
- Atrioventricular Heart Block
- Chronic Heart Failure
- Suddenly serious symptoms of heart failure
- rhabdomyolysis
- Drowsiness
- Adequate evidence of effectiveness for more prolonged use has not been established
- Not recommended in pediatric patients less than 16 years of age
Dosage of Carisoprodol
- Strengths: 350 mg; 250 mg
Muscle Spasm
- 250 to 350 mg orally 3 times a day and at bedtime
- Duration of therapy: Up to 2 to 3 weeks
Side Effects of Carisoprodol
The Most Common
- Drowsiness
- Convulsions (seizures)
- hallucinations (seeing or hearing things that are not there)
- increase in muscle spasm, cramping, or tightness
- Loss of muscle coordination
- sleepiness or unusual drowsiness
- clumsiness or unsteadiness
- dizziness
- dry mouth
- false sense of well-being
- increased watering of mouth
- lightheadedness
- constipation;
- vision changes;
- breast swelling (in men or women); or
- decreased sex drive, impotence, or difficulty having an orgasm.
- blurred vision, tunnel vision, eye pain or swelling, or seeing halos
Common
- Bigger, dilated, or enlarged pupils (black part of the eye)
- blurred vision
- change in consciousness
- confusion as to time, place, or person
- difficult or troubled breathing
- false or unusual sense of well-being
- hallucinations
- headache
- holding false beliefs that cannot be changed by the fact
- inability to move the eyes
- increased blinking or spasms of the eyelid
- increased sensitivity of the eyes to light
- irregular, fast or slow, or shallow breathing
- loss of consciousness
- muscle stiffness or tightness
- pale or blue lips, fingernails, or skin
- sticking out of the tongue
- the trouble with breathing, speaking or swallowing
- uncontrolled eye movements
- uncontrolled twisting movements of the neck, trunk, arms, or legs
- unusual excitement, nervousness, or restlessness
- unusual facial expressions
- weakness of the arms and legs
Rare
- Anxiety
- deep or fast breathing with dizziness
- dry mouth
- the face is warm or hot to touch
- fainting feeling of constant movement of self or surroundings
- heartburn
- irritability
- nausea
- nervousness
- numbness of the feet, hands, and around the mouth
- pain or discomfort in the chest, upper stomach, or throat
- redness to face
- restlessness
- sensation of spinning
- shakiness and unsteady walk
- sleeplessness
- trouble sleeping
- unable to sleep
- unsteadiness, trembling, or other problems with muscle control or coordination
- vomiting
Drug Interactions Of Carisoprodol
Carisoprodol may interact with the following drugs, supplyments, & may change the efficacy of drugs
- amphetamine
- dextroamphetamine
- amphetamine
- dextroamphetamine
- zolpidem
- Fish Oil (omega-3 polyunsaturated fatty acids
- Fish Oil (omega-3 polyunsaturated fatty acids
- pregabalin
- esomeprazole
- antihistamines (e.g., cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
- antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
- aripiprazole
- antidiabetes medications
- barbiturates (e.g., butalbital, pentobarbital, phenobarbital)
- benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
- carbamazepine
- gabapentin
- levodopa – carbidopa
- magnesium sulfate
- mirtazapine
- monoamine oxidase inhibitors (MAOIs; e.g. rasagiline, selegiline, phenelzine, rasagiline, selegiline, )
- other muscle relaxants
- phenytoin
- selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine, paroxetine, sertraline)
- tapentadol
- topiramate
- tramadol
- tricyclic antidepressants (e.g., desipramine, nortriptyline)
Pregnancy & Lactation Of Carisoprodol
FDA Pregnancy Category – C
Pregnancy
- It is not known if carisoprodol is safe and effective for use in pregnant women. Tell your doctor if you’re pregnant or plan to become pregnant. Carisoprodol should be used during pregnancy only if the potential benefit justifies the potential risk. Call your doctor right away if you become pregnant while taking this drug.
Lactation
- It isn’t known if carisoprodol passes into breast milk. If it does, it may cause side effects in a child who is breastfed. Talk to your doctor if you breastfeed your child. You may need to decide whether to stop breastfeeding or stop taking this medication.
References
