Basic1 Flashcards
Bioavalabilty
relative amount of a drug dose that reaches the systemic circulation unchanged and the rate at which this occurs
Drugs that easily pass through the lipid bilayer
small, nonpolar
Volume of distribution
Volume of tissue that the drug reaches
Vd=dose/concentration
Hepatic metabolism
Phase 1 (oxidation, reduction, hydrolysis): by p450 this occurs hydroxylation, dealkylation, deamination, desulration, epoxidation, dehalogenation Phase 2 (conjugation): conjoins hydrophobic drug molecules with polar moities to increase solubility and therefor renal clearance
Drugs with active metabolite
Morphine -> morphine 6-gluconoride (opioid)
Meperidine -> Normeperine (convulsant)
Atracuriun -> laudanosine (convulsant)
issues when pt is renally impaired
metabolism equations
Rate = Q (Cin - Cout)
Extration ratio =(Cin -Cout)/Cin
Clearance =Q X ER
Cockcroft-Gault equation (creatinine clearance)
Creatinine Clearance (ml/min) =[ (140-age) X weight] / 72 X serum creatinine
Tissue clearance
butylchilinesterase = Sux, mivacurium, 2 chroroprocaine, ester LA
nonspecific esters = remifentanil, atracurium
RBC esterases = esmolol
major plasma proteins for binding anesthetic drugs
albumin and alpha-1-acid glycoprotein
epidural opiods
must male their way out of the epidural space if they are to reach their site of action in the spinal cord’s dorsal horn
- lipid soluble drugs (fentanyl, sufentanyl) reach lower peak concentrations in the CSF compard to hydrophilic (morphine)
- lipiphylic drugs more easily transverse vascilar walls and therefor are cleared more rapidly
intrathecal opiods
- lipophilic opioids tend to move out of the aqueous CSF primarily diffusing across the meninges into epidural fat
- explains why morphine (hydrophylic) causes delayed respiratory depression (stays intrathecal and spreads up to brain)
Epidural LA
- intrathecal bioavalabilty increases with lipiphilicity (opposite of opioids)
LA Spinals
1) baricity of solution (adds glucose to make hyperbaric)
2) position of patient
3) concentration of LA
Tolerance vs dependence
Tolerance: requiring increased dosages of a drug to achieve similar effects
dependence: compulsive need of an individual to use a drug to function normally
types of tolerance
1) dispositional (metabolic): repeated use of a drug reduces the amount of drug available at site
2) reduced responsiveness (pharmacodynamic): repeated use alters nerve cell functions
3) behavioral (context-specific): reduces its effect in the environment where it is typically administered but not in other environments.
tachyphylaxis
acute decrease in response to a drug following its administration
half life
half life = 0.693/ Ke
Ke = rate constant
Clearance equation
Clearance = Vd X Ke
Renal clearance
Renal Clearance = concentration of drug in urine X volume of urine / concentration of drug in plasma
Anaphylaxis vs anaphylactoid
anaphylaxis: severe allergic reaction mediated by an aintigen antibody reaction ( type I) IgE
Anaphylactoid resembles anaphylaxis but is not IgE mediated ( does not require prior sensitization)
most common cause of anaphylaxis
NDNMB
latex allergy risks
chronic exposure to latex, neural tube defects, frequent caths
MOA of inhaled gasses
proposed:
enhance inhibitory receptors (GABA and glycine)
dampen excitatory pathways (nicotinic and glutamate)
Rate of equilibirum in gasses
rate is directly related to alveolar gas concentration
high partition coefficient= high solubility= slow rate of induction