Unit 4: LA Drugs specifically

Question 1

lidocaine undergoes ____ metabolism in the liver

Answer 1

Metabolism: Oxidative dealkylation in liver, then hydrolysis. ​

metabolite is Xylidide

Question 2

max infiltration dose of lidocaine is ____

Answer 2

300 mgs plain & 500 mgs /c EPI​

Question 3

you will have prolonged clearance of lidocaine with what?

Answer 3

preg induced hypertension

Question 4

Prilocaines main metabolite is ____. what does it convert to?

Answer 4

Orthotoluidine
converts to Methemoglobinemia​

Dose > 600 mgs​

S/Sx: Cyanosis d/t decreased 02 carrying capacity​

TX: Methylene Blue ​

1 to 2 mgs/kg IV over 5 mins​

Total dose not to exceed 7 to 8 mg/kg​

Question 5

What is the max for methylane blue?

Answer 5

7-8mg/kg

Question 6

mepivacaine has a ___ duration of action

Answer 6

longer

you can use for longer surgeries

not used in OB

Question 7

bupivacaine is metabolized thru ____

What protein does it bind to?

Answer 7

Metabolism: aromatic hydroxylation, N-dealkylation, amide hydrolysis, and conjugation​

Protein (95%) binding site: α1-Acid glycoprotein​

Question 8

Ropivacaine​

Metabolism: ___
Metabolites: _____

Lesser system toxicity than ______​

Protein Binding: ______

Answer 8

Ropivacaine​

Metabolism: Hepatic cytochrome P450 enzymes​

Metabolites: can accumulate with uremic patients​

Lesser system toxicity than Bupivacaine​

Protein Binding: α1-acid glycoprotein​

Question 9

Dibucaine​

Metabolism: _____​

MOA: inhibits the activity of normal _______ (plasma cholinesterase) by more than 70%​

​

Answer 9

Dibucaine​: we dont use this because it would effect the metabolism of most of the other drugs we give

will use to diagnose prolongation of sux block

Metabolism: Liver​

MOA: inhibits the activity of normal butyrylcholinesterase (plasma cholinesterase) by more than 70%​

​

Question 10

Procaine​

Metabolite:

Answer 10

Procaine​

Metabolite: PABA, excreted unchanged in urine​

Question 11

Chloroprocaine​

Metabolism: Plasma ____ (3.5x faster)​

Pregnancy ______ plasma cholinesterase by 40%​

Answer 11

Chloroprocaine​

Metabolism: Plasma cholinesterase (3.5x faster)​

Pregnancy decreases plasma cholinesterase by 40%​

Question 12

Tetracaine​

Metabolism:

​

***Hydrolysis: chloroprocaine > procaine > tetracaine​

Answer 12

Tetracaine​

Metabolism: Slower than procaine​

​

***Hydrolysis: chloroprocaine > procaine > tetracaine​

Question 13

Benzocaine​

Unique: Weak _____ (pKa 3.5)​

Uses: Topical anesthesia of mucous membranes:​

Tracheal intubation, Endoscopy, Transesophageal echocardiography (TEE), Bronchoscopy​

Onset: _____​

Duration: ______ minutes​

Dose: Brief spray (20%) = ___ to ____ mgs​

Answer 13

Benzocaine​

Unique: Weak acid (pKa 3.5)​

Uses: Topical anesthesia of mucous membranes:​

Tracheal intubation, Endoscopy, Transesophageal echocardiography (TEE), Bronchoscopy​

Onset: rapid​

Duration: 30 to 60 minutes​

Dose: Brief spray (20%) = 200 to 300 mgs​

Question 14

if you give too much benzocaine you can cause ______

Answer 14

methemoglobinemia

• TX of 7-8 mg/kg

Question 15

Cocaine​

Metabolism: Plasma and liver ______​

Peak: _______​

Duration: _____ minutes after peak​

Elimination: ____ (24 to 36 hours)​

Caution: ??

Answer 15

Cocaine​

Metabolism: Plasma and liver cholinesterases​

Decreased in: Parturients, Neonates, Elderly, Severe Hepatic Disease​

Peak: 30 to 45 mins​

Duration: 60 minutes after peak​

Elimination: Urine (24 to 36 hours)​ (10-12% in the urine)

Caution: Coronary vasospasm, ventricular dysrhythmias, HTN, tachycardia, CAD​