An anesthetic is a drug to prevent pain during surgery, completely blocking any feeling as opposed to an analgesic. Propofol is one of the most commonly used intravenous drugs employed to induce and maintain general anesthesia. Take this Pharmacology test on local anesthetics and remind yourself of what you covered in your class this month.
Inactivated, voltage-gated, Na+ channels
Resting, voltage-gated ,K+ channels
Activated, ligand-gated, Ca++ channels
Inactivated, ligand-gated, K+ channels
Resting, ligand-gated, Na+ channels
Activated, voltage-gated, Ca++ channels
Resting fibers
Rapidly firing fibers
Fibers with high conduction velocity
Unmyelinated fibers
Fiber of large diameter
Rate of rise of the action potential
Amplitude of the action potential
Refractory period of the nerve
Conduction velocity of the nerve
Resting potential of nerve membrane
Motor function
Pain sensation
Muscle tone
Pain sensation
Vasomotor function
Increased extracellular concentration of Ca++
Increased extracellular concentration Na+
Decreased extracellular concentration of Cl-
Increased extracellular concentration of K+
Increased extracellular concentration of Mg++
The more negative the membrane potential, the lower the affinity for local anesthetics
The more negative the membrane potential, the higher the affinity for local anesthetics
The higher the frequency of firing of the fiber, the lower the affinity for local anesthetics
The lower the frequency of firing of the fiber, the higher the affinity for local anesthetics
The faster the conduction velocity of the fiber, the higher the affinity for local anesthetics
Tissue redistribution
Liver biotransformation
Systemic toxicity
Receptor binding
Half-life
They are very rich in drug-metabolizing enzymes
They are poorly vascularized, so that the drug reach slowly the nerve terminals
They are rich in extracellular K+ which lower the drug-receptor binding
They are rich in PABA which is a competitive antagonist of most local anesthetics
They have a low extracelluar pH, which hinders the drug diffusion into the cell
10%
24%
50%
76%
90%
Cocaine
Bupivacaine
Procaine
Tetracaine
Benzocaine
Benzocaine
Procaine
Tetracaine
Lidocaine
Bupivacaine
Benzocaine
Procaine
Cocaine
Prilocaine
Bupivacaine
To speed up the onset of the anesthetic effect
To increase the duration of anesthetic effect
To decrease the risk of systemic overdose toxicity of the drug
To decrease the risk of allergic reactions of the drug
To increase the affinity of the drug for the Na+ channels
Gastrointestinal system
Respiratory system
Urinary system
Immune system
Cardiovascular system
CNS
Procaine
Tetracaine
Lidocaine
Benzocaine
Prilocaine
Cocaine
Procaine
Benzocaine
Tetracaine
Lidocaine
Ventricular tachycardia
Abdominal colic
Drowsiness
Tonic-clonic convulsions
Disorientation
Lidocaine
Lidocaine plus epinephrine
Bupivacaine plus epinephrine
Benzocaine plus epinephrine
Benzocaine
Blockade of substance P receptors in the injured area
Blockade of Na+ channels in the radial nerve membranes
Activation of alpha-2 presynaptic receptors in the radial nerve terminals
Activation of opioid receptors in the injured area
Blockade of prostaglandin receptors in the injured area
The drug caused cardiotoxic effects which in turn triggered the CNS excitation
The drug mediated an allergic reaction in a sensitized patient
The drug inhibited glutamate reuptake into glutamatergic neurons
The drug activated the mesolimbic pathway in the CNS
The drug caused depression of the inhibitory neurons in the CNS
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Here's an interesting quiz for you.