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CNS Depressants packet. Includes narcotic analgesics, anesthetics, sedative/hypnotics including barbiturates, benzodiazepines & phenothiazines which make up the anticonvulsants

Analgesics do what

Decrease perception of pain

Anesthetics do what

Decrease sensation

Analgesics are divided into what 2 classes

Opioid and Non-Opioids

Opioid category

1. Agonists
2. Antagonist
3. Agonist-antagonist

Non-Opioid category

1. Salicylates
3. Adjuncts

Definition for agonist

Binds to the receptor site and causes the expected response

Definition for antagonist

Binds to the receptor site and does not initiate the expected response (blocks the site)

Definition for agonist-antagonist

Binds to the sites and causes some of the expected response but partially blocks others|NOTE: this concept is also referred to as PARTIAL agonists or COMPETITIVE agonism

Opioids are aka


Opioids are a generic reference to

Morphine-like drugs/actions

Opioids aka Narcotics act on

Endorphin receptors to decrease ability to propagate pain impulses:
1. Mu
2. Kappa
3. Sigma

Endorphin receptor Mu

Most important- expected effects, and wants more

Endorphin receptor Kappa

(similar to Mu) strong sedation

Endorphin receptor Sigma

(for undesirable effects such as dysphoria, hallucinations, AMS) "bad trip"

General actions of Opioids

1. Analgesia
2. Respiratory depression
3. Constipation
4. Urinary retention
5. Cough suppression
6. Emesis
7. Increased ICP ( indirect thru co2 retention)
8. Euphoria/ dysphoria
9. Sedation
10. Miosis
11. Decreased Pre-load/afterload low BP

Narcotics to know

1. Morphine (prototype)
2. Meperidine (Demerol)
3. Hydromorphone (Dilaudid)
4. Hydrocodone (Vicodin)
5. Oxycodone (Percocet)
6. Propoxyphene (Darvon)
7. Fentanyl (Sublimaze)

Anidote for opioid narcotics

Naloxone (Narcan)

What do adjunct meds do

They're not actually analgesics.
They potentiate analgesics (enhance the effects of)|

Examples of adjunct meds

1. Benzodiazepines
2. Antihistamines
3. Caffeine

Opioid antagonist

Naloxone is the prototype ( only one)

nalaxone (Narcan)

1. It competes with opioid receptor sites to block effect of the narcotic
2. used to treat heroin and opioid overdoes
3. shorter half-life than the narcotic means the Narcan will wear off and narcotic will still be there and bind to receptors

titrate Narcan to effect means

to respiratory rate to at least 8.
don't slam it! just enough to get them breathing well (not too much,not too fast)

trade name for morphine sulfate

Duramorph, Astramorph

classification of morphine sulfate (Duramorph, Astramorph)

1. Narcotic analgesic
2. CNS depressant

mechanism of action for morphine sulfate (Duramorph, Astramorph)

1. binds to opiate receptor sites in CNS to block pain.
2. CNS depression (decreased HR, low BP, decreased LOC

Indications for morphine sulfate (Duramorph, Astramorph)

1. pain
2. chest pain of suspected AMI origin, Acute pulmonary edema

trade name for fentanyl


trade name for meperidine hydrocloride


trade name for hydromorphone


classification for fentanyl, meperidine hydrocloride, hydromorphone

1. CNS depressant
2. Narcotic analgesic

indication for fentanyl, meperidine hydrocloride, hydromorphone

pain management

classification for nalaxone (Narcan)

Narcotic antagonist

mechanism of action for nalaxone (Narcan)

reverses effects of certain narcotic and synthetic narcotic analgesics by competing with analgesic at opiate receptor site

indication for nalaxone (Narcan)

know or suspected narcotic overdose with respiratory rate <8 or decreased tidal volume


asprin (Bayer) aslo NSAID

what does NSAID represent

Non-Steroidal Anti-Inflammatory Drugs

what are 5 NSAIDs

1. acetaminophen (Tylenol)
2. ibuprofen (Motrin, Advil)
3. naproxen sodium (Naprosyn)- prescription med
4. naproxen sodium (Aleve)- OTC
5. ketorlac (Toradol) -ONLY DRUG BY IM OR IV (for emesis pt.)

Aspirin mechanism of action

Inhibits synthesis of cyclooxygenase (COX)

cyclooxygenase (COX) is the enzyme responsible for

synthesis of Prostaglandins and Thromboxane A2

desired aspirin effects

1. pain relief
2. decreased fever
3. decreased inflammation

undesirable aspirin effects

1. GI ulceration (increased GI acidity,decreased GI protection)
2. increased bleeding
3. decreased renal elimination
4. decreased uterine contractions during labor

acetaminophen (Tylenol) side effects differs from aspirin how

1. does not cause gastric ulceration
2. does not decrease platelet aggregation
3. no decreased renal flow
4. no decrease uterine contractions

acetaminophen (Tylenol) does this the same as aspirin

inhibits the synthesis of CNS prostaglandins

acetaminophen (Tylenol) also inhibits

leukocyte migration and release of lysosomes

ketorolac (Toradol) anti-inflammatory effects are

caused by decreased prostaglandin synthesis

ketorolac (Toradol) pain management

related to decreased inflammation

ketorolac (Toradol) also has

antipyretic effects which means "decreased fever"

how is ketorolac (Toradol) different from other NSAIDs

can be given IM or IV which is great for vomiting patients

ketorolac (Toradol) deters

"frequent flyers"

trade names for aspirin

1. acetylsalicylic acid
2. ASA
3. Bayer

classifications for aspirin (acetylsalicylic acid, ASA, Bayer)

1. antiplatelet
2. anticoagulant
4. antipyretic
5. analgesic

mechanism of action for aspirin (acetylsalicylic acid, ASA, Bayer)

1. blocks platelet aggregation
2. slows prostaglandin synthesis action which also impedes inflammation response

indication for aspirin (acetylsalicylic acid, ASA, Bayer)

chest pain because of antiplatelet

precautions with aspirin (acetylsalicylic acid, ASA, Bayer)

asthmatic patients (may increase viscosity of respiratory secretions and cause mucous plug formation)

acetaminophen (Tylenol) classification

1. analgesic
2. antipyretic

acetaminophen (Tylenol) mechanism of action

decreased prostaglandin synthesis

acetaminophen (Tylenol) indications

1. fever
2. pain

acetaminophen (Tylenol) contraindication

children < 3 years old should have children's tylenol

anesthetics means

loss of all sensation

usually with anesthetic you have a loss of

consciousness, decreased propagation of neural impulses

neuroleptanesthesia is also called

conscious sedation

what is neuroleptanesthesia used for

procedures that require the patient's cooperation such as joint reduction

neuroleptanesthesia is a combination of

neuroleptic/antipsychotic (diazepam, droperidol, ketamine) and narcotic analgesic (meperidine, morphine, fentanyl)
-usually a drug that does not cause a drop in BP

local anesthetics

1. exert their affect on area around injection
2. usually accompanied by epinephrine, lidocaine (Xylocaine), topical cocaine (i.e.drops)

general anesthetic gases

1. nitrous oxide (Nitronox)
2. halothane
3. ether

Intravenous General anesthetics

1. thiopental (Pentothal)- barbiturate
2. methohexital (Brevitol)- barbiturate

nitrous oxide (Nitronox) classification

1. analgesic gas mixture
2. CNS depressant
3. anesthetic

nitrous oxide (Nitronox) mechanism of action

depressing the CNS

nitrous oxide (Nitronox) indication

pain relief


produce anesthesia and hypnosis but no analgesia

barbiturates mechanism of action

unknown, but believed to act on RAS

ultra-short acting barbiturates

used for premedication for RSI
1. onset 20-60 seconds (immediately)
2. duration 5 minutes

why is the onset and duration ideal for RSI

if you're unable to intubate, at least the patient comeback and able to breath for themselves at 5 minutes

longer acting barbiturates

used for seizures, anxiety, and sedation

Benzodiazepines vs. barbiturates

barbiturates are more potent and more addictive than benzodiazepines

the only barbiturate

phenobarbital (Luminal)

phenobarbital (Luminal) classification

1. Barbiturate
2. sedative-hypnotic
3. CNS depressant

phenobarbital (Luminal) mechanism of action

1. inhibition of the RAS
2. increases seizure threshold

phenobarbital (Luminal) indication

1. seizure
2. status epilepticus

major group where anticonvulsant drugs live



decrease anxiety and inhibitions

hypnotics means to

induce sleep

classes of sedative-hypnotic drugs

1. barbiturates
2. benzodiazepines
3. alcohol

both Benzodiazepines and barbiturates promote

the effectiveness of GABA receptors in the CNS

Benzodiazepines promote

GABA receptors ONLY

barbiturates promote GABA and

at high doses stimulate GABA receptors

what is GABA

the chief CNS inhibitory neurotransmitter

Benzodiazepine mechanism of action

mediate anxiety and sedation in the cerebellum

Benzodiazepine receptors in basal ganglia and hippocampus

cause muscle relaxation and decreased memory and sensation

has high concentration of benzo receptors


5 Benzodiazepines

1. diazepam (Valium) pre-hospital
2. midazolam (Versed) pre-hospital
3. lorazepam (Ativan) hospital
4. triazolam (Halcion) home med
5. alprazolam (Xanax) home med

"non-benzo benzos"

1. zolpidem (Ambien)
2. buspirone (BusPar)
do the same as benzos (for going to sleep)

5 barbiturates

1. phenobarbital (Luminal)
2. amobarbital (Amytal)
3. pentobarbital (Nembutal)
4. secobarbital (Seconal)
NOTE: if pt. is on barbiturates, they're in bad shape mentally

other sedatives

1. etomidate (Amidate) most used in hospital
2. propofol (Diprivan)
3. ketamine (Ketalar) horse tranquilizer
4. droperidol (Inapsine) tranquilizer
5. haloperidol (Haldol) tranquilizer
6. cholorpromaZINE (ThoraZINE) tranquilizer causes dystonic reaction, effects reversed w/ Benedryl

seizures are caused by

hyperactive brain areas

seizure drug classes

multiple chemical classes of drugs are used to treat

Anticonvulsants do what

1. increase motor cortex threshold
2. decrease propagation of actions potentials
3. stabilize the cell membrane
-decrease Na,Ca influx (delay depolarization and prolong repolarization
-increase Cl influx (hyperpolarize membrane so it cannot depolarize again


1. phenobarbital (Luminal)


1. diazepam (Valium)
2. lorazepam (Ativan)
3. midazolam (Versed)

Anticonvulsants-Misc. Agents

1. phenytoin (Dilantin) increases seizure threshold, drip
2. valproic acid (Depakote) home med
3. carbamazepine (Tegretol) home med
4. acetylzolamide (Diamox) decreases altitude ICP

Anticonvulsants-Magnesium Sulfate

1. decreases striated muscle contractions
2. blocks peripheral neurotransmission by decreasing ACH at motor nerve terminals
3. used for seizures associated with pregnancy
4. side effects include respiratory depression, hypotension, and decreased muscle reflexes

classifications for diazepam (Valium), midazolam (Versed), lorazepam (Ativan)

1. CNS depressant
2. benzodiazepine
3. anticonvulsant
4. sedative/hypnotic/amnestic
5. skeletal muscle relaxant

general mechanism of action for diazepam (Valium), midazolam (Versed), lorazepam (Ativan)

1. suppresses seizure activity
2. relaxes skeletal muscles
3. induces amnesia by depressing the CNS

general indications for diazepam (Valium), midazolam (Versed), lorazepam (Ativan)

1. seizures
2. status epilepticus
3. pre medication for pacing
4. cardioversion
5. RSI

unique indication for midazolam (Versed)

"chemical restraint" or acute anxiety disorder

unique indication for lorazepam (Ativan)

alcohol withdrawals (so they don't seize)

classifications for etomidate (Amidate), propofol (Diprivan), and ketamine (Ketalar)

CNS depressant, anesthetic, sedative/hypnotic

mechanism of action for etomidate (Amidate), propofol (Diprivan), and ketamine (Ketalar)

produces analgesia and amnesia

indicaiton for etomidate (Amidate), propofol (Diprivan), and ketamine (Ketalar)

Rapid Sequence Intubation


Duramorph, Astramorph














acetlsalicylic acid, ASA, Bayer





nitrous oxide




















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