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Flumazenil is a GABAA-receptor
antagonist that can rapidly reverse the
effects of benzodiazepines.
GABAB receptor
Seizures
Sleep disorders
It is effective for spasticity due to spinal cord From Katzung: Basic and Clinical
Pharmacology, 11th edition, 2009.
lesions. It may also reduce pain in patients
with spasticity, perhaps by inhibiting the
release of substance P in the spinal cord.
Centrally acting muscle relaxant: Tizanidine
and clonidine
a2-adrenoceptor agonist
Reduce muscle spasm, probaly through
peripheral and central effects.
Side effects: drowsiness, hypotension, dry
mouth
Not only relieves spasticity but also produce muscle weakness, which
reduces its clinical usefulness.
Botulium toxin
Actions:
1. Depression of CNS: Degree of depression of the CNS
depends on the dose. At low doses, they produce sedation.
At higher doses, the drugs cause hypnosis, followed by
anesthesia, and finally, coma and death. The drugs have no
analgesic properties. Chronic use leads to tolerance.
2. Respiratory depression: suppress the chemoreceptor response
to CO2 and overdosage is followed by respiratory depression
and death.
3. Enzyme induction: induce p450 microsomal enzymes in the
liver.
Barbiturates
Therapeutic uses:
1. Anesthesia: Ultrashort-acting barbiturates, such as thiopental, are used
intravenously to induce anesthesia.
2. Anticonvulsant: Phenobarbital
3. Anxiety
Pharmacokinetics: Cross the blood-brain barrier. Absorbed orally and
distributed widely throughout the body. Redistribution is important in
causing the short duration of action of drugs (thiopental). Hepatic
metabolism.
Poisoning: Cause death resulting from drug
overdoses, which severely suppress
respiration and central cardiovescular center.
Treatment includes artificial respiration,
purging the stomach of its contents,
hemodialysis and alkalinization of the urine.