CNS Part 1: Anxiolytics, Hypnotics, Alcohol, & Opoids Flashcards
- What effect does GABA have on the CNS?
GABA is the major INHIBITORY neurotransmitter of CNS (gaba normally causes opening of CL channels)
What effect do benzodiazepines have on GABA?
BZDs increase the affinity of GABA for GABA binding site (enhance CL channel opening & inhibitory effects in CNS)
- Describe how BZDs are used for anxiety disorder
4 serious, persistant anxiety
-used for short term therapy since can be addictive
(USE) What is the BZD Diazepam used for?
Treatment of Muscle Spasm
What are BZDs used for?
- Anxiety disorders
- Muscle disorders
- Amnesia
- Sleep disorders
How long should BZDs for sleep disorders be given?
2 weeks to avoid tolerance & withdrawl
a) What class does Flurazepam (Dalmane) belong to
b) What is it used for?
a) Long-acting BZD
b) increases sleep time
a) What class does belong to Triazolam (Halcion)
b) What is it used for?
a) Short-acting BZD
b) sleep induction
- What are the AE of Benzodiazepines?
Tolerance, Dependence, Withdrawl, CNS dependence (drowwsiness, & confusion, etc)
- What type of drug is a BZD antagonist?
Flumazenil (Romazicon); it reverses the effects of BZD
What is the MOA of Buspirone (Burpar)?
-Does NOT work on BZD receptors
It has anxiolytic effects (anti-anxiety)
What is the MOA of Barbituates?
Acts on GABA-a receptors & causes sedative & hypnotic effects (CNS depression)
What are the uses of Barbituates?
ANTICONVULSANT, Anesthesia, Anxiolytic, Hypnotic
What is an AE of barbituates?
Induction of CYP450 (drug interactions) (as a result, the drug level in the blood goes down)
What is an ex of a hypnotic?
Zolpidem (Ambien)
MOA: acts on BZD 1 receptors
a)What are the kinetics of Eszopiclone (Lunesta)?
effective up to 6 months of continuous use
What is the MOA of Ramelteone (Rozerem)?
melatonin agonist (MT1 & MT2)
What is the use of Rmelteon (Rozerem)?
insomnia
What is the MOA of antihistamines?
Competitive histamine -1 (H1) antagonist
What types of drugs are Ramelteone (Rozerem) and Eszopiclone (Lunesta)?
Hypnotics
*What is the MOA of Disulfiram (Antabuse)?
Blocks oxidation of acetaldehyde to acetate
interferes with ethanol metabolism
- What is the use of Disulfiram (Antabuse)?
Deter alcohol use
- What is a major AE of Disulfiram (Antabuse)?
N/V
tachycardia, hyperventilation, flusing
What is the MOA of opoids (pain)?
bind to opoid receptors in CNS to produce effects of neurotransmitters
What are examples of opoids?
Endorphins, Enkephalins, Dynorphins
Name the opoid receptors
mu, kappa (sedative), and delta
- What is the major receptor involved in opoid pain relied & respiratory depressant effects?
Mu
What is the MOA of opoid receptors?
Inhibit adenyl cyclase
What is the MOA of opoid analgesica
Bind to receptors in the CNS and inhibit the ascending pain pathway (CNS depression)
Define analgesia
increase in pain tolerance, alters pain perception
Define euphoria
sense of well being
Define respiratory supression
decreased sensitivity to carbon dioxide
*Define miosis
stimulation of mu and kappa receptors (enhanced parasympathetic stimulation of eye)
- What are the AE of opoids?
Analgesia, Euphoria, respiratory depression, cough reflex supression, miosis, emesis (N/V)
Which RX should you not use in patients with head injuries?
Opoids
What effect do opoids have on therespiratory system?
Causes respiratory depression–> carbon dioxide retention and dilation of cerebral vessels and increased CSF pressure
- Name a strong opoid agonist
Morphine
*Name a moderate/low opoid agonist
Codeine
*Name a mixed opoid agonist-antagonist
Pentazocine
- Name a partial opoid agonist
Buprenorphine
- Name a opoid antagonist
Naloxone
What are the uses of morphine?
analgesia, acute pulmonary edema, relief of diarrhea, and relief of cough
*What opoids suppress the cough reflex?
Codeine and dextromethorphan
What opoids provide relief of diarrhea?
Loperamide and diphenoxylate
What are the AE of morphine?
extension of opoid effects, increased ICP, urinary retention, stoppage of respiratory exchange
What is Meperidine (Demerol ) used for?
OB: less likely to prolong labor (less effect on SM of uterus)
What is an AE of meperidine (demerol)?
May cause pupil dilation, large dosing may cause toxic metabolite
What patients shoudl not take meperidine (Demerol)
Elderly
What is a use of methadone?
Controlled withdrawl from other opoids (heroin, morphine)
What is the MOA of pentazocine?
Provides analgesia by acting on receptors in SC; blocks morphine effect
What are the uses of opioid antagonists
reverse CNS depression of opiod overdose
- What are the 3 stages of opoid withdrwal symptoms?
- Stage 1: Anxiety & drug craving
- Stage 2: insomnia, Gi disturbance, Rhinorrhea, Mydiriasis, Diaphoresis
- Stage 3: Tachycardia, N/V, HTN, diarrhea, Fever, Chills, Tremors, Seizure, Muscle spasms
