Eperisone + Paracetamol Pharmacology
Eperisone + Paracetamol
Eperisone
Suppression of Spinal Reflexes: In spinal cats, eperisone HCl suppresses mono- and polysynaptic reflex potentials induced through spinal nerve efferent root stimulation to a similar degree.
Reduction of Muscle Spindle Sensitivity via ?-Motor Neurons: Eperisone HCl suppresses the activity of afferent nerve fibers (Ia fibers) from human muscle spindles at 20 min after administration. Eperisone HCl suppresses the spontaneous discharge of ?-motor neurons, but does not act directly on muscle spindles in animals. Accordingly, eperisone HCl reduces muscle spindle sensitivity via the ?-motor neurons.
Vasodilatation and Augmentation of Blood Flow: Vasodilatory Action: Eperisone HCl dilates the blood vessels due to Ca2+-antagonistic action (in guinea pigs) on the vascular smooth muscle and muscular sympatholytic actions (in humans).
Augmentation of Blood Flow: Eperisone HCl increases the volume of blood flow in skin, muscle, external and internal carotid arteries and vertebral arteries in humans, monkeys and dogs.
Analgesic Action and Inhibition of the Pain Reflex in the Spinal Cord: When eperisone HCl is perfused into the spinal cord of rats, a tail pinch-induced pain reflex is suppressed, but the reflex returns with the withdrawal of eperisone HCl. This suggests that eperisone HCl possesses an analgesic action at the spinal cord level.
Facilitation of Voluntary Movement: When eperisone HCl is used in the treatment of spastic paralysis in patients with cerebral apoplexy, it improves the cybex torque curve and electromyogram and facilitates voluntary movements eg, extension and flexion of the extremities, without reducing the muscular force.
2.Dizziness
3.Insomnia
4.Drowsiness
5.Numbness or trembling in the extremities
6.Hepatic and renal dysfunction
7.Haematological changes
8.Skin rashes
9.Itching
10.GI disturbances
11.Urinary disorders
12.Rarely, shock.
2.May impair ability to drive and operate machines.
Paediatric:Not recommended
2.Spastic spinal paralysis
3.Cervical spondylosis
4.Postoperative sequelae (including from cerebrospinal tumour)
5.Sequelae to trauma (e.g. spinal trauma or head injury)
6.Amyotrophic lateral sclerosis
7.Cerebral palsy
8.Spinocerebellar degeneration
9.Spinal vascular diseases and other encephalomyelopathies
10.Cervical syndrome, periarthritis of the shoulder, and lumbago
Paracetamol
It is more active on cyclo-oxygenase enzyme in brain. Peripherally it is a poor inhibitor of prostaglandin synthesis.
Analgesic action: Paracetamol raises the pain threshold and produces analgesic effect.
Antipyretic action: Paracetamol lowers fever by direct action on the thermoregulatory centre in the Hypothalamus and block the effects of endogenous pyrogen.
Distribution: It is distributed mostly in the body in unbound form.
Metabolism: It is extensively metabolised in the liver.
Excretion: Excreted in the urine.
2. Abdominal distress
3. Allergic reactions
4. Rash
2. Renal impairment
3. Hypertension
NEONATES : Contraindicated
2. Acute gout
3. Migraine
Charcoal: Activated, administered immediately reduces absorption of paracetamol.
Domperidone and metochlopramide: Enhance absorption of paracetamol.
Alcohol: Chronic excessive ingestion of alcohol potentiates hepatotoxicity of paracetamol.
Zidovudine: Effects zidovudine may be decreased.
500 - 1000 mg in 3 times daily
Maximum dose: 4 g / day
For migraine: 500 mg to be taken at the first sign of migraine attack and repeated 4 - 6 hourly until suppress mild attacks.
Children:
60 mg / kg body weight /day in 4 divided doses.
Maintenance dose: 75 mg / kg orally every 4 - 6 hours for 2 - 3 days. Haemodialysis can be done in emergency conditions.
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