CENTRALLY ACTING SKELETAL MUSCLE RELAXANT SERENA JOHN. A 109
OBJECTIVES SKELETAL MUSCLE RELAXANT. CENTRALLY ACTING RELAXANTS. CLASSIFICATION OF DRUGS. EXAMPLES OF DRUGS. USES OF DRUGS. DIFFERENCE BETWEEN PERIPHERAL AND CENTRALLY ACTING MUSCLE RELAXANT.
SKELETAL MUSCLE RELAXANT They are drugs which act peripherally or centrally to reduce the skeleton muscle tone. Peripheral – used to produce muscle relaxation for surgery. Central – used for painful muscle spasm and spasmatic neurological conditions.
Centrally acting relaxant Drugs that reduce skeletal muscle tone and lessen muscle spasm by a selective action on CEREBROSPINAL AXIS , without altering consciousness. Depress spinal and supraspinal polysynaptic reflex involved in maintaining muscle tone. Have some sedative property.
CLASSIFICATIONS
EXAMPLES BACLOFENAC- GABA analogue [ GABA-B receptor agonist ] Primary site of action: Spinal Cord Decreases excitatory transmitter release and depresses both polysynaptic and monosynaptic reflexes. Preferred drug for symptomatic relief in neurological disorders such as multiple sclerosis, amyotropic lateral sclerosis, spinal injuries and flexor spasms.
Side effects: Drowsiness, Mental confusion, weakness, ataxia. Sudden withdrawal after chronic use may cause hallucination, tachycardia, seizure. THIOCOLCHICOSIDE- Chemically related to colchicine. GABA mimetic with additional analgesic action. Side Effects: Gastric upset , Photosensitivity.
TIZANIDINE- Clonidine Congener- Alpha 2 adrenergic agonist . Inhibits release of excitatory amino acids in spinal interneurons. Decreases muscle tone and frequency of muscle spasm without reducing its power. Should be avoided in patients receiving Antihypertensives drugs [CLONIDINE] . Side Effects: Dry mouth, Drowsiness, Night time insomnia, Hallucination.
DIAZEPAM- Prototype of BENZODIAZEPINES which acts on specific receptors in Brain. Enhances GABAergic tranmission . MEPHENESIN- Internunical neurone blocking agent. Used in counterirritant ointments.
CARISOPRODOL- Favourable Muscle relaxant: sedative activity ratio. Have weak analgesic, antipyretic, anticholinergic properties. Used in tissue injury, muscle sprains, disorders associated with local muscle spasm. CHLORMEZANONE- Relaxant with anti anxietic and hypnotic action. Used for tension state associated with increased muscle tone.
CHLORZOXAZONE- Pharmacologically similar to MEPHENESIN. Longer duration of action. METHOCARBAMOL- Less sedative and longer acting than MEPHENESIN. Oral: reflex muscle spasm and chronic neurological diseases. Utilized for orthopedic procedures and tetanus.
USES ACUTE MUSCLE SPASMS- MEPHENESIN- like and BZD muscle relaxant, combined with analgesics are used. TORTICOLLIS, LUMBAGO, BACKACHE, NEURALGIAS. ANXIETY AND TENSION- DIAZEPAM group of drugs and CHLORMEZANONE . SPASTIC NEUROLOGICAL DISEASES- BACLOFEN, DIAZEPAM, TIZANIDINE, DANTROLENE TETANUS- DIAZEPAM[ i.v. ] , METHOCARBAMOL . ELECTROCONVULSIVE THERAPY- DIAZEPAM ORTHOPEDIC MANIPULATIONS.