Sedative, Alcohol, Durgs Of Abuse And Dementia Flashcards
3 families of sedative hypnotics?
Benzos (short acting, intermediate acting and long acting)
Barbs (ultra action, short action and long action)
Misc agents
Good definition of sedative and hypnotic?
Drug that decreases CNS activity, moderates excitement, and calms the recipient
Produces drowsiness and facilitates the onset and maintenance of sleep
5 clinical uses of sedative hypnotics?
Anxiety, insomnia, surgery/anesthesia, epilepsy, muscle relaxation
MOA of benzos and 5 clinical effects?
GABA A agonist, so increases chloride influx causing hyper-polarization and decreased number of APs
Sedation, hypnotic effects, muscle relaxation, anti anxiety, anti convulsants
MOA of barbiturates and spectrum of clinical effects?
GABA A agonist
Mild sedation to anesthesia
What drug is used to reverse benzo overdose?
Flumazenil
What is the metabolism and elimination of benzos?
CYP3a4 for phase 1
Glucuronidation for phase 2
1/2 life, active metabolites, pathway of metabolism, and rate on onset for the following benzos? Diazepam Oxazepam Lorazepam Alprazolam Clonazepam
Over 100, yes, oxidation, and very fast 5-15, none, conjugation, slow 10-20, none, conjugation, intermediate 12-15, insignificant, oxidation, fast 20-50, insignificant, ox/red, intermediate
Half life and rate of onset of the following benzos? Chlordiazepoxide Flurazepam Clorazepate Triazolam
Over 100 and intermediate
Over 100 and fast
Over 100 and fast
1.5-5 and intermediate
Big difference between the general idea of barb effects and benzo effects?
Benzos sort of hit a ceiling where no matter how much more you increase the dose, the effect plateaus.
Not the case for barbs. Their effect will go all the way to coma if you keep increasing the dose.
Prototype ultra short acting barb and typical indication?
Prototype short acting barb and typical indication?
Prototype long acting barb and typical indication?
Thiopental anesthesia
Secobarbital, insomnia
Phenobarbital seizures
2 problems with using benzos for insomnia?
Day time sedation and anterograde amnesia
Clinical use of Zolpidem, Zaleplon, and Eszopiclone?
MOA?
3 advantageous features?
Unique feature of zolpidem and exzopiclone?
What are they not used for?
Insomnia
GABA a agonist
Highly effective, rapid onset, and minimal hangover effects
Biphasic release for sustained sleep
Longer half life
Only used for sleep aids, none of the anxiety, anesthetic, convulsants stuff.
MOA of ramelteon?
Clinical use?
Agonist at melatonin 1 and 2 receptors
Insomnia
MOA of buspirone?
Metabolism of it?
Anxiety
CYP3a4
What is considered excessive drinking and heavy drinking for a man and woman?
Excessive
Women 4 or more in one setting
Men 5 or more in one setting
Heavy
Women 8 or more per week
Men 15 or more per week
5 step process of alcohol metabolism?
What order kinetics is alcohol and what does that mean?
Alcohol to acetaldehyde by ADH, to acetic acid by aldehyde dehydrogenase, to CO2 by oxygen, water and energy
Zero, meaning rate remains constant and is independent of concentration or amount
3 key pieces of information to consider for pharmacology of alcohol?
Ethanol undergoes extensive first pass metabolism by GI and liver ADH
Zero order kinetics
Typical adult can metabolize 1 drink per hour on average
3 things to do to treat acute alcohol intoxication?
Monitor respiratory depression and aspiration of vomit
Glucose can treat hypoglycemia or ketosis
Thiamine to protect against wernickes
What is the major pharmacological objective for acute withdrawal syndrome of alcohol and what two things to treat it?
Prevent seizures, delirium, arrhythmias, electrolyte imbalances
Benzos and thiamine
What is the primary treatment for alcohol dependence and what two other conditions are associated with alcoholism?
Psychosocial therapy
Depression and anxiety
Overdose effects of stimulants, cocaine?
Withdrawal symptoms of stimulants, cocaine?
Agitated, HTN, tachycardia, seizures, hallucinations, hyperthermia, delusions
Apathy, irritable, depression, increased sleep
Overdose effects of barbs, benzos, alcohol?
Withdrawal symptoms?
Dilated pupils, slurred speech, drunken behavior and basically depression of everything
Tremors, anxiety, insomnia, delirium
Overdose effects of heroin, strong opioids?
Withdrawal symptoms?
Constricted pupils, nausea and everything depressed
Nausea, chills, cramps, lacrimation,
Effect of ACHE blockers at muscarinic receptors and nicotinic receptors?
Stimulate muscarinic receptors
Stimulate then depress at nicotinic
4 therapeutic uses for ACHe inhibitors?
Diseases of the eye
GI an urinary tract problems
NMJ problem
Alzheimer’s