local anesthetics

anti-arrhythmic

anti-epileptics

• -caine
• two i's = amide (longer acting)
• one i= ester
• vasodilators (EXCEPT FOR COCAINE- VASOCONSTRICTOR)

• amide
• cannot be given orally because of First Pass Effect

• Amides are longer lasting
• Esters can have side-effects
• Amides are metabolized hepatically

• also block potassium -->prolonged QT interval--> torsade de pointes --> treat with magnesium IV
• Quinidine
• Procainamide
• Disopyramide

• Lidocaine
• Mexiletine (similar to lidocaine, but decrease FPE)

• Flecainide

• Class IA
• atropine like effects (block muscarinic receptors)
• bronchodilation (helps asthma)
• cinchonism
• digoxin levels increased
• nausea & vomitting
• arrhythmia
• no erection (block muscarinic- block parasympathetic nervous system--> no erection)

• Class IA because it is metabolized in the liver to N-acetyl procaine-amide, which is a Class III so it's a Na and a K blocker = Class IA

• Na: membrane stabilization
• Ca: decreased transmitter release

• similar to TCAs
• side effects:
• H1 receptor blocker=sedation
• M receptor blocker= dry mouth
• Na & Kchannel blocker=arrhythmia
• Alpha R blocker=hypotension

CYP P450 3A4 Inducers

• St. John's wort
• efavirenz; nevirapine
• glucocortocoids
• rifampin
• carbamazepine
• phenytoin
• barbituates

• gum hyperplasia
• megaloblastic anemia (folate deficiency)
• peripheral neuropathy
• skin rash
• hirsuitism
• coarsening of facial features
• CNS symptoms
• Zero order kinetics (saturabel hepatic hydroxylation)

• Alcohol (only true-rest quickly saturable)
• Aspirin
• Heparin
• Theophyllin
• Phenytoin

• Traimterene
• Dapsone
• Phenytoin
• Trimethoprim
• Methotrexate