Pharm Flashcards
Sensation Sequence
Pain–>Cold–>Warmth
Resting potential of a nerve
-70mV due to Na/K pump moving 2K ions in and 3Na out (negative potential)
If a stimulus changes to -55mV then…
Na gates open. Na rushes in which DEPOLARIZES to +30mV (firing)
Repolarization to Hyperpolarization (describe what happens)
Na gates close, and K gates open. K rushes Out (repolar) to -90mV (hyperpolarization)
What channel does anesthetic work against?
Goes INTO nerve cell and blocks Na Channels. nerve doesnt respond
pH >7: what happens to LAH+?
LAH+–> LA+H+ (drug can move through lipid bilayer and bid to the NA channel)
pH <7: what happens to LAH+?
LA+H+–> LAH+ (much less of the anesthetic can bind to a Na Channel due to being unable to get through lipid layer)
Are local anesthetics basic or acidic?
basic
If an anesthetic is in an acidic environment the drug is…
ionized
Which LA are amides?
lido, mepivicaine, prilo, bupiv, ropiv, articiaine (thiophene ring instead of benzene)
where are amides metabolized
liver
What LA are esthers?
procaine, tetracaine
Where are esthers metabolized?
plasma
Benzodiazepines are most commonly used as…
anxiolysis, sedation, anxiety, anticonvulsant, muscle relaxors
Side effects of Benzos
decrease BP, HR, Respiration is normal, may increase confusion
Mechanism of benzos
Enhances GABA effect on GABAa receptors on chloride channels
What is the chemistry of LAs?
Aromatic Nucleus, Amide of ester link, and amino group
Ingredients in LA?
vasoconstrictors, antioxidant, sodium hydroxide (adjusts pH), sodium chloride (isotonic), methylparaben, sodium metabisulphite(vasoconstrictor preservative)
What might you be allergic to if allergic to LA?
esters because of the p-aminobenzoic acid (PABA)
methylparaben- maybe
Prilocaine metabolism
primary transformation in the liver and secondary in the lungs
Systemic toxicity signs of LA
circumoral numbness
tongue paresthesia
dizziness
tinnitus
blurred vision
restlessness
agitation
nervousness
paranoia
slurred speech
drowsiness
unconsciousness
Minimal to moderate toxicity signs
Euphoria
increase in BP
loss of consciousness
Severe toxicity signs
muscle twitch–> tonic clonic—>Respiratory Arrest
Seizure management? What drug to give?
Thiopental 1-2mg/kg to abruptly terminate the seizure.
What drugs or conditions can increase the threshold for LA induced seizures
Benzos and
hyperventilation
pH of a cell is usually what pH?
7.4
Will a LA with a low or high pKA be more available for cell absorption?
low (more absorption, faster onset)
What symptoms follow a seizure due to LA overdose?
Decrease of BP, HR, RR, and CNS depression
Lidocaine pKa?
7.8
Bupivicaine pKa?
8.1
Mepivacaine pKa?
7.7
Rank the LA in order of lipid solubility: Carbo, lido, marcaine
carbo, lido, marcaine
Septo: mg/lb, MRD
3.2mg/lb, 500mg
Marcaine: mg/lb, MRD
0.6 mg/lb, 90mg
Lido w/o vaso: mg/lb, MRD
2.0mg/lb, 300mg
lido w/ vaso: mg/lb, MRD
3.0mg/lb, 500mg
Carbo: mg/lb, MRD
3.0mg/lb, 400mg- natural vasoconstrictor mechanism
LA considerations: if a patient has a bisulfite allergy?
avoid vasoconstrictor