NMJ Drugs Flashcards

1
Q

Pyridostigmine

A

Class: carbamate type cholinesterase inhibitor
Apps: treat MG (increase muscle tone), reverse actions of nondepolarizing neuromuscular blockers after surgery
Mech: lasts 3-6 hrs. competes with ACh for binding site on AChesterase. Potentiates at nictonic and muscarinic receptors.
Effects: increased muscarinic effects

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2
Q

Prednisone

A

Class: corticosteroid
Apps: immunosuppressant & anti-inflammatory
Mech: modifying transcription to inhibit leukocyte infiltration at site of inflammation. Interferes in function of mediators, and suppress humoral immune response. Prodrug - metabolized in liver to prednisolone.
Effects: withdrawal– fever, myalgia, malaise. Chronic use – ulcers, hyperglycemia, osteoporosis, glaucoma, adrenal insufficiency, behavioral disturbances.

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3
Q

Tubocurarine

A

Class: nondepolarizing, neuromuscular blocking agent.
Apps: skeletal muscle relaxant.
Mech: compete with ACh for cholinergic receptor sites at NMJ, results in paralysis.
Effects: has highest potential amount NM blocking agents to produce histamine release and vasodilation resulting in hypotention. Ganglia blockade can result in reduced GI motility.

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4
Q

Atracurium

A

Class: intermediate-acting, nondepolarizing, neuromuscular blocking agent.
Apps: as adjunct to general anesthesia to provide skeletal muscle relaxation. Aid in tracheal intubation.
Mech: compete with ACh AChR sites at NMJ, resulting in paralysis.
Effects: histamine release– flushing, edema, urticaria, pruritus, bronchospasms (less histamine produced than tubocurarine).

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5
Q

Rocuronium

A

Class: short-acting, nondepolarizing, neuromuscular blocking agent.
Apps: adjunct to anesthesia to provide skeletal muscle relaxation. Longer acting than succinylcholine. Rapid onset makes it useful alternative to succinylcholine. Aid in tracheal intubation.
Mech: compete with ACh for cholinergic receptor sites at NMJ, result in paralysis.
Effects: few. Causes little histamine release

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6
Q

Succinylcholine

A

Class: depolarizing-type, skeletal muscle relaxant.
Apps: for IV administration to produce rapid neuromuscular blockade (allows for intubation within 60 sec).
Mech: competes with ACh for the cholinergic receptors of the motor end plate – produces a prolonged depolarization that causes initial contraction followed by paralysis. Rapidly hydrolyzed by plasma pseudocholinesterase (t1/2 ~ 1 min.)
Effects: hyperkalemia in patients with burns, abdominal infections, tetanus, trauma, stroke, spinal cord injury, and neuromuscular disease. Patients with pseudocholinesterase mutations don’t efficiently metabolize it, thus prolonging its duration of action.

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7
Q

Diazepam

A

Class: benzodiazepine
Apps: anesthetic, skeletal muscle relaxant, anticonvulsant, anxiolytic/sedative/hypnotic
Mech: binds to allosteric site on GABA-A receptor-chloride channel complex, resulting in GABA-mediated increase in chloride conductance, hyperpolarization, and neuronal inhibition
Effects: long duration of action (active metabolites). dose-dependent headache, drowsiness, ataxia, dizziness, confusion, depression, syncope, fatigue, tremor, vertigo.

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8
Q

Baclofen

A

Class: skeletal muscle relaxant; spasmolytic drug
Apps: treat spasticity and improve mobility in patients with MS & other spinal cord lesions
Mech: activates GABA-B receptors in spinal cord which results in hyperpolarization by increasing K+ conductance
Effects: drowsiness, nausea/vomiting, constipation; muscular weakness, hypotonia. Withdrawal– spasticity, hallucinations, seizures.

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9
Q

Gabapentin

A

Class: oral anticonvulsant, neuropathic pain medication, spasmolytic drug
Apps: control seizures associated with epilepsy. Reduce pain and improve QOL measures in pts with wide range of neuropathic pain syndromes. Useful to manage spasticity.
Mech: not related to GABA system. Inhibits some classes of Ca2+ channels. Lipid soluble, excreted in urine.
Effects: fatigue, drowsiness.

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10
Q

Dantrolene

A

Class: spasmolytic drug, skeletal muscle relaxant.
Apps: for malignant hyperthermia. Muscle response to direct stimulation is attenuated; produces generalized, mild weakness of skeletal muscles and overall improvement in muscle tone.
Mech: peripherally acting relaxant, inhibits calcium release from SR.
Effects: little effects on cardiac or smooth muscle. Muscle weakness.

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11
Q

Botulinum toxin

A

Class: skeletal muscle relaxant
Apps: for cervical dystonia in adults, blepharospasm and strabismus associated with dystonia. For focal spasticity.
Mech: selective for ACh terminals, cleaves SNAP-25 proteins.
Effects: ptosis, superficial punctate keratitis, inflammation of cornea, xerophthalmia. Dysphagia, dyspnea.

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12
Q

Tizanidine

A

Class: CNS spasmolytic, muscle relaxant
Apps: for acute and intermittent management of increased muscle tone associated with spasticity.
Mech: centrally acting alpha-2 adrenergic agnoist. To treat spasms & muscle tightness caused by MS, back pain & spinal injuries.
Effects: weakness, sedation, xerostomia, dose-related hypotension in patients treated with single oral doses.

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13
Q

Azathioprine

A

Class: immunosuppressive
Apps: immunosupressant for MG, RA, SLE
Mech: metabolized to 6-mercaptopurine; inhibits DNA & RNA synthesis, resulting in inhibition of cell proliferation, especially leukocytes
Effects: nausea/vomiting; leukopenia and thrombocytopenia are dose-dependent

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