Download PPT file: Neuromuscular Blockers

An outline of the slideshow content:

• Neuromuscular blockers differ from each other in: • Mechanism of action • Duration of action • Speed of onset and offset of action • Selectivity of action and safety margin • Adverse effects
• Classification of Blockers
• Site of Action
• Non-depolarizing Block
• Comparison of Competitive and Depolarizing Blocking Agents
• Sequence of Paralysis: Fingers, orbit (small muscles) limbs neck Trunk Diaphragm,  Intercostals. Recovery in Reverse
• Adverse Effects/Toxicity
• Dual Block by Depolarizing Agents
• Other Effects of Neuromuscular Blockers
• Hemodynamic Effects of d-Tubocurarine and Pancuronium CO

Non-depolarizing blocking agents

Atracurium (Tracrium), Cisatracurium (Nimbex), Doxacurium (Nuromax), Gallamine (Flaxedil), Mivacurium (Mivacron), Pancuronium (Pavulon), Pipecuronium, Rapacuronium (Raplon)

Depolarizing blocking agents

Succinylcholine, Decamethonium

• First pass metabolism
• Patients in whom oral administration should be avoided
• P-glycoprotein (P-gp)
• Relevance of drug distribution in compartments
• Context specific half life
• Cytochrome 450
• Pharmacogenetics

Pharmacotherapy in critical care: pharmacokinetics

Recommended pharmacokinetics reading

Drotrecogin alfa (activated) (Xigris, marketed by Eli Lilly and Company) is a recombinant form of human activated protein C ( rhAPC) that has anti-thrombotic, anti-inflammatory, and profibrinolytic properties. Drotrecogin alpha (activated) belongs to the class of serine proteases. It is used mainly in intensive care medicine as a treatment for severe sepsis.

Quoting the MedWatch alert:

Xigris (Drotrecogin alfa [activated]) – Early Communication about an Ongoing Safety Review

The finding by Gentry et al. of an increased risk of death and serious bleeding events in patients treated with Xigris who also have baseline bleeding risk factors is consistent with the information in the current product label. Prescribers should refer to the product label for the specific contraindications, warnings, and, precautions and carefully weigh the increased risk of bleeding against the benefits of Xigris.

FDA is working with the manufacturer to further evaluate the incidence of serious bleeding events and mortality in patients who received Xigris. FDA will communicate its conclusions and any resulting recommendations to the public when the review is completed, which may take several months.The FDA urges both healthcare professionals and patients to report side effects from the use of Xigris to the FDA’s MedWatch Adverse Event Reporting program.

Some additional backgroung information on the marketing of Xigris (rhAPC) that is worth reading: Surviving Sepsis — Practice Guidelines, Marketing Campaigns, and Eli Lilly, N Engl J Med. 2006.