Ethanol and Methanol Flashcards
What is the drug class of ethanol?
CNS depressant
What is the mechanism of action of ethanol?
General suppressant effct on most cells. Can inhibit excitatory (glutaminergic pathways) or activate inhibitory (GABAergic) pathways
What does GABA stand for?
Gamma Amino Butyric Acid
How does ethanol cause a mild diuretic effect?
Inhibition of ADH secretion
From where is ethanol absorbed?
The small intestine (less so from intestine)
What is carbonation’s effect on ethanol absorption?
Increases rate of gastric emptying so more rapid absorption.
What does alcohol dehydrogenase do?
Converts ethanol to acetaldehyde
What does acetaldehyde dehydrogenase do?
Converts acetaldehyde to acetyl CoA
What builds up in the body when ethanol is metabolized?
NADH (from alcohol dehydrogenase and acetaldehyde dehydrogenase)
What drug is given to discourage patients from drinking? (makes them feel ill when they drink alcohol?)
Disulfiram
What is disulfiram’s mechanism of action?
Inhibits acetaldehyde Dehydrogenase leading to an increase in acetaldehyde causing headache, severe nausea, and convulsions
What is a drug that can reduce ethanol craving during withdrawal?
Acamprosate - somehow alters GABA activity
What drug is given to inhibit alcohol dehydrogenase?
Fomepizol
What is the mechanism of action of inhaled general anesthetics?
Potentiation of inhibitory GABAergic neurons or blockade of glutamate (excitatory) neurons
How does lipid solubility affect potency of general anesthetics?
The higher the lipid solubility the more potent the general anesthetic
What is MAC?
Minimal alveolar concentration (ED50 of inhaled general anesthetics) The lower the MAC the more potent the drug
What effect does the Blood/Gas coefficient of an inhaled general anesthetic have?
High B/G coefficient = slower onset (need a lot more in blood before it becomes saturate enough to act)
What are the anesthetic effects of NO?
Good analgesic (pain killer), no amnesia
What are the halogenated hydrocarbons?
(FLURANEs) isoflurane, desflurane, sevoflurane
What is a side effect of the halogenated hydrocarbons?
Malignant hyperthermia
What is used to treat malignant hyperthermia from halogenated hydrocarbons?
Dantrolene
What are the intravenous general anesthetics?
Thiopental, propofol, etomidate (Barbiturates), midazolam
What is the mechanism of action of Thiopental?
Activates GABAergic pathway (rapid induction/recovery)
What is the mechanism of action of Propofol?
Activates GABA pathway
What is the mechanism of Ketamine?
Analog of phencyclidine. Binds to and activates a receptor which then blocks glutamate activity.
What is the mechanism of action of Etomidate?
Activates GABA receptors
What is the mechanism of action of Midazolam?
Activates GABAnergic neurons
To what drug class does thiopental belong?
Barbiturates I.V. general anesthetic
To what drug class does propofol belong?
Barbiturates I.V. general anesthetic
To what drug class does Ketamine belong?
Barbiturates I.V. general anesthetic
What is the structure of the local anesthetics?
Aromatic site connected by either an ester or amide linkage to an amino site
What are the local anesthetics that are linked by an ester?
Cocaine, benzocaine, procaine, benoximate and proparacaine (BBC PP)
What are the local anesthetics that are linked by an amide?
Lidocaine, articaine, mepivacaine, bupivacain, prilocaine, ropivacaine, etidocaine (P-MARBLE)
What is the mechanism of action of the local anesthetics?
They are weak bases which act on the Na+ channels of excitable tissue. Decrease neuronal conduction, repolarization rate, and increase refractory period
What kind of neurons are affected by local anesthetics?
More rapidly firing neurons are more sensitive, smaller fibers are more sensitive, myelinated fibers are more sensitive; pain>cold>warmth>touch>motor neurons
Do ester linked or amide linked local anesthetics have a longer duration?
Amide linkage last longer (metabolized in liver by P450) than ester bonded (hydrolyzed by a circulating plasma cholinesterase)
What are the side effects of the local anesthetics?
Blurred vision, tinnitus (ringing of ears), convulsions, comas, death, arrhythmias, tachycardia, allergic reactions
What is tetrodotoxin?
Found in liver and ovaries of pufferfish - irreversibly block Na+ channels causing repiratory paralysis and death
What is saxitoxin?
Found in shellfish “red tide” - cause respiratory paralysis and death
To what drug class does baclofen belong?
Neuronal treatment of spasticity
What is the mechanism of action of baclofen?
GABA agonist
What does diazepam and other benzodiazepines do? (mechanism of action)
Activate GABA receptors - used to treat spasticity
What is tizanidine used for?
Neuronal treatment of spasticity
What is the mechanism of action of tizanidine?
Alpha2 agonist
What drug is used to treat spasticity on the muscular level?
Dantrolene (orally administered)
What is the mechanism of action of dantrolene?
Inhibits stimulus induced release of Ca2+ from muscle sarcoplasmic reticulum