Unit 5 Flashcards
Alpha fibers
alpha-skeletal muscle motor, proprioception
Beta- touch, pressure
Gamma- Skeletal muscle tone
Delta- fast pain, temp, touch
Beta fibers
Preganglionc ANS fibers
C fibers
Sympathetic- postganglionic ANS fibers
Dorsal root- slow pain, temp, touch
Block onset
- B
- C
- A gamma and A delta
- A alpha and a beta
VGNaC
1 alpha unit
2 betas
Resting (-70 mV): closed
Active (-70 to +35 mV): opens, Na flows outside to inside
Inactive (+35 to -70 mV): closed, inactivation gate until membrane potential reestablished
LA can bind in active and inactive phases- more frequent depol means more time for blockade (use dependent or phasic blockade)
Resting membrane potential
-70
3 Na+ out and 2 K+ in
LAs do not impact resting membrane potential or threshold
Mechanism of action LA
Weak bases
After injection LA dissociates into uncharge base and ionized, conjugate acid
PKa’s higher than 7.4= > 50% will exist as ionized conjugate acid
Uncharged base enters cell and becomes ionized due to acidic ECF
Only ionized, conjugate acid binds to LA binding site on alpha subunit
LA molecule construction
Benzene ring- lipophilic
Intermediate chain- ester or amide (has NH in it)
Tertiary amine- hydrophilic
Ester LA’s
No i before Caine suffix
Benzocaine, cocaine, chloroprocaine, procaine, tetracaine
Pseudocholinesterase metabolism
Low allergic potential- cross sensitivity if allergy happens, due to PABA
Amide type
I before suffix Caine
Articaine, bupivicaine, etidocaine, lidocaine, mepivicaine, ropivicaine
Hepatic/P450 metabolism
Extremely rare allergies
Onset of action
PKA- closer to pH of blood= larger fraction uncharged and able to cross and get to receptor
Dose- give large dose of chlorprocaine cause isn’t very potent even with high pKa
Concentration- higher concentration onset’s quicker
Potency
Lipid solubility- can get inside drug and be available to bind to receptor
Intrinsic vasodilating effect- cocaine, chloroprocaine, and ropi dont vasodilate, lido does
Duration of action
Protein binding- tissue reservoir to extend DOA, preferably bind to alpha a acid glycoprotein but can bind to albumin
Lipid solubility
Intrinsic vasodilating effect
Addition of vasoconstrictors- prolongs
Amide pKa
Bupivacaine- 8.1
Ropivacaine- 8.1
Lido- 7.9
Prilocaine- 7.9
Ester pKa’s
Procaine- 8.9
Chloroprocaine- 8.7
Tetracaine- 8.5