11 - B) ANSTISPASTICS DRUGS

Question 1

MAIN SYSTEMS ON WITH THEY ACT

Answer 1

GABAERGIC SYSTEM, ADRENERGIC SYSTEM OR OTHER ALTERNATIVE SYSTEM

Question 2

BACLOPHEN

Answer 2

GABAENERGIC SYSTEM; Selective GABAB Agonist (blocks nervous transmission).
Oral & intrathecal
Main effect in spinal cord. Also analgesia. Not useful in epilepsy
Indication: Spasticity in multiple sclerosis / spinal cord lesions
Adverse effects: somnolence, loss of coordination, nauseas.
Rebound effect after sudden discontinuation.

Question 3

BENZODIAZEPINES; DIAZEPAN

Answer 3

GABAENERGIC SYSTEM; GABA A Positive allosteric modulators; muscle relaxant & anxiolytic effects

Oral.
Indications: Contractures, torticollis, lumbagos, multiple sclerosis …….
Adverse effects: sedation, dependence, tolerance…
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Question 4

VIGABATRIN

Answer 4

GABAENERGIC SYSTEM;

Inhibit GABA-transaminase
Clinical trials: similar effect to BACLOFEN

Question 5

TIZADINE

Answer 5

ADRENERGIC : α2 agonists

Agonist of central presynaptic α2-adrenergic R

Decreases the release of excitatory neurotransmitter

Decreases spinal reflexes & excessive muscle tone
Decreases muscle tension &
spasms frequency

Indication: myorelaxant in patients with
spasticity associated to multiple sclerosis
or spinal & brain lesions
Side effects: dry mouth (40%),
sedation, muscle weakness

Question 6

OTHER ANTISPASTICS

Answer 6

Botulinum

Cannabinoids

Question 7

CANNABINOIDS

Answer 7

Other antispastics perspectives.
Sativex
Oral spray
They act blocking the CB2 receptor present throughout the body. They are going to reduce brain plasticity and brain activity as AR.

Question 8

BOTULINUM

Answer 8

Other antispastics perspectives.

It blocks the release of ACh, so muscles cannot get contracted and suffer from paralysis till the toxin is degraded.