skeletal muscle relaxants -decr ms tone
February 27, 2009 Leave a comment
- peripherally acting on NMJ Nm receptors (i.v. for short procedures) (quaternary -no BBB/oral/placenta) – nondeplz[dTB], deplz[SCh] –> paralysis(voluntary movts lost)
- directly acting on ms by decr Ca+2 release – dantrolene –> drug of choice in malignant hypothermia(from flourinated anaesthetics/SCh in succeptibles), decr UMNDspacticity in hemi/paraplegia,Cpalsy,MS,ALS,spinal inj.incr RP & decr excitation quinine -use in myotonia congenita, nocturnal leg cramps [ADR-decr ms strength,sedation,diarrhoea,liver toxicity]
- spamolytics acting centrally by decr spinal supraspinal reflexes of ms tone without affecting stretch reflex [ADR-sedation]–>
- pain<–>spasm: acute (overstretch,sprain,tear, dislocation,bursitis, rheumatoid disorders), torticollis,lumabago,backacke,neuralgias -mephenesin like/DZP +analgesics.
- deseased desc pathways(UPMND)–>spasticity: decerebrate rigidity, hemi/paraplegia, MS,ALS, Cpalsy, parkinsonism, spinal inj, stroke -DZP,baclofen,tizanidine.
- hyperreflexia of anxiety -DZP,chlormezanone.
- ECT, ortho manipulations,tetanus -DZP [w/ SCh]
| nondeplz/competitive Nm blocker | deplz/noncompetitive Nm blockers |
| bulky molecule – metabolized by AChE. | slender long flexible -cant be disossiated. |
| affinity to alfa subunits + physically block preventing subunits conformational changes. | affinity to alfa subunits + intrinsic partial deplz of Na+ ch. |
no Na+ ch opening -decr end plate pot -no AP –> initial weakness, flaccid paralysis first of small/fast response ms[eye,limbs] & last on head trunk[diaphragm] –> use in
[ADR- prolonged apnoea w/ long acting drugs: dTB,pan,dox,pipe -neostigmine reversal required] |
Na+ ch in open inactivated state –> initial fasciculatiins [soreness in man]. decr EPP -no AP –> flaccid paralysis [phase1] rapid onset & recovery w/out the ms sequence appreciation & only transient apnoea –> use intubation, endoscopy, ortho manipulations, ECT. [ADR- prolonged/high dose SCh/deficient pseudoChE/florinated anaesth --> phase2 slow onset & recovery of desensitization to ACh --> prolonged apnoea] |
| dTB,pancuronium,vecocuranium -block autonomic ganglia[Nn] –>vagal tachycardia. decr BP by ganglion block+limb ms paralysis+histamine (CI- hypovolemia, hepatic/renal insufficiency – so CISATRACURIUM can be used /w does not release histamine & undergoes hoffman elimination spontaneously in plasma) |
SCh stimulates autonomic ganglia –> vagal brdycardia initially, later sympth tachycardia. sympth HTN, incr postoperative Paralyticileus. |
| dTB causes high histamine release -flushing, decr BP, brspasm & incr secretions(ppt asthma) [not w/ cisatracurium, rocurarium] |
low histamine release -flushing |
| burns/tetanus + prolonged SCh deplz –> hyperkalaemia -arrhyth [CI- digitalized Pt] |