Pharmacology 1 (DRUGS & FUNCTIONS)

ENZYME INDUCERS ENZYME INHIBITORS

 Omeprazole  Amiodarone
 Lansoprazole  Cimetidine
 Phenytoin  Quinolones
 Tobacco smoke  Fluvoxamine
 Barbiturates  Azole antifungals
 Rifampicin  Isoniazid
 Carbamazepine  Cimetidine
 Dexamethasone  Fluoxetine
 Alcohol (chronic)  Trancylpromine
 St. John's wort  Bupropion
 Primidone  Celecoxib
 Efavirenz  Paroxetine
 Ritonavir
 Sertraline
 Disulfiram
 Clarithromycin
 Erythromycin
 Graprefruit juice
 Imatinib
 Verapamil

PHARMACOLOGY OF AUTONOMIC NERVOUS SYSTEM

CHOLINERGIC AGONISTS

DIRECT ACTING INDIRECT ACTING INDIRECT ACTING REACTIVATION OF

(REVERSIBLE) (IRREVERSIBLE) ACETYLCHOLINESTERASE
 Acetylcholine  Ambenonium (TX  Echothiopate  Pralidoxime
 Bethanechol for Alzheimers)  Sarin
 Carbachol  Donepezil (TX for  Malathion
 Cevimeline Alzheimers)  Parathion
 Methacholine  Edrophonium  Isofluoropate
 Pilocarpine (short acting)  Soman
 Nicotine  Galantamine (TX  Tabun
 Varenicline for Alzheimers)
 Lobeline  Neostigmine
 Physostigmine
 Pyridostigmine
 Rivastigmine (TX
for Alzheimers)

Acetylcholine

 MIOCHOL-E – drug example

 A neurotransmitter that plays a role in memory, learning, attention, arousal and involuntary muscle movement.
Typically, acetylcholine is an excitatory mediator.
 MOST POTENT CHOLINERGIC AGONIST
 An ester of acetic acid and choline, Quaternary Ammonium Alcohol.
 Used in the DIAGNOSIS OF ENDOTHELIAL DYSFUNCTION.
  ACTIONS: Decrease in heart rate and cardiac output; Decrease in blood pressure.

Bethanechol

 URECHOLINE
 Structurally related to Ach
 Passes BBB
 Non polar
 Lacks nicotinic actions; strong muscarinic activity
 Major actions: Bladder and GI Tract
 Management of Ileus
 Treatment for Urinary Retention
 Resistant to cholinesterase – CARBAMIC ACID ESTERS
 Adverse effects: DUMB BELSS

Carbachol

 MIOSTAT
 Both muscarinic and nicotinic actions
 Resistant to cholinesterase – CARBAMIC ACID ESTERS
 Actions: effects on CV and GI systems; release of epinephrine; miosis
 Therapeutic applications: Treatment for glaucoma (lowers intraocular pressure)
 Adverse effects: DUMB BELSS

Pilocarpine

 Alkaloid (Pilocarpus jaborandi), tertiary amine

 Less potent but can penetrate the CNS – LIPOPHILICITY
 Muscarinic activity – primarily in ophthalmology