Pharm -- Cns Drugs

Front 1

How do benzodiazepines work on seizure activity?

Back 1

Inhibit seizure activity by preventing spread across brain. Doesn't stop seizure at the focus.

Front 2

What is the MOA of the benzodiazepines?
(3)

Back 2

-Have own binding site on GABA
-Increase activity of GABA
-Increase Cl permeability (increses Cl ability to cross GABA channel)

Front 3

What is the benzo of choice for short-term sedationand acute agitation?
(<48 hrs)

Back 3

Midazolam

fastest onset of action, shortest duration of action

Front 4

How is Midazolam metabolized?

Back 4

Via oxidation in the liver (potential for drug interaction thru CYP 450)
-active metabolite is eliminated by the kidney (impaired renal - difficult time getting rid of drug)

Front 5

What is the benzo of choice for prolonged sedation?
(>48 hrs)

Back 5

Lorazepam
-slowest onset
-intermediate duration
-don't use if you want rapid awakening!

Front 6

Which is more potent - Midazolam or Lorazepam?

Back 6

Lorazepam

Front 7

How is Lorazepam metabolized?

Back 7

Through glucuronidation
-less drug interactions than other benzos
-even with liver disease will still be metabolized

Front 8

Which benzo has the potential for propylene glycol toxicity?

Back 8

Lorazepam
(liquid formulation made with propylene glycol)

Front 9

What is propylene glycol toxicity?

Back 9

Metabolic acidosis, paradoxical agitation, hypotension, acute tubular necrosis, and hyperosmolar states

Front 10

Name 2 signs of Lorazepam toxicity

Back 10

Metabolic acidosis
Hyperosmolar state

Front 11

Which benzo is long acting, lipophillic and takes a long time to eliminate?

Back 11

Diazepam

Front 12

Adverse effects of Benzos

Back 12

Hypotension
Respiratory depression
-elderly and renal impaired higher risk
Withdrawl syndrome

Front 13

What is the reversal agent for benzos?

Back 13

Romazacon
Flumanzil

Front 14

What is the MOA of propofol?

Back 14

1) Not fully understood - believed via GABA
2) unrelated to benzos or opiates, etc

Front 15

What are dosing parameters for propofol?

Back 15

5-50mg/kg/min
higher max doses are used
titrate to RASS (richmond agitation sedation scale)

Front 16

What is the onset, duration, and 1/2 life of propofol?

Back 16

Onset: 30 seconds
Duration: 3-10 minutes
-dose and rate dependent
1/2 life: 40 minutes (may be increased to 1-3 days with prolonged use)

Front 17

What are the adverse effects of propofol?

Back 17

Hypotension, bradycardia, Hypertriglyceridemia, local injection site rxn, green urine (initially high infection rate - so change tubing Q 12 hrs)

Front 18

What are S/S of propfol infusion syndrome?

Back 18

Hyperkalemia
Hypotension
Hepatomegaly
Metabolic acidosis
Rhabdo

Front 19

Which drug is a highly selective alpha2 agonist?

Back 19

Dexmedetomidine
(precedex)

Front 20

TRUE/FALSE
Dexmedetomidine causes respiratory depression.

Back 20

False

useful in pt's prone to drug-induced respiratory depression (sleep apnea, COPD, weaning of mechanical vent)

Front 21

What is the biggest adverse rxn to dexmedetomidine?

Back 21

Hypotension

Front 22

What drug can cause hyperthermia, severe muscle rigidity and rhabdo (and what is this syndrome called)?

Back 22

Haloperidol

neuroleptic malignant syndrome

Front 23

TRUE/FALSE

The incidence of EPS is less with IV vs. PO haloperidol.

Back 23

TRUE

Front 24

How does haloperidol work?

Back 24

Blocks dopamine receptors in CNS.

Front 25

Is haloperidol useful for immmediate control of anxiety?

Back 25

No, use benzo

sedation is evident in 10-20 min. after IV haloperidol

Front 26

Which CNS drug can cause torsades de points?

Back 26

Haloperidol

prolonged QT - doses >35mg/day

Front 27

Name an alternative anxiolytic that does not have CNS depressant effects.

Back 27

Busbar

(Serotonin 5HT agonist)

Front 28

Name 4 characteristics of busbar.
(learned in class)

Back 28

1) not an anticonvulsant
2) Not a muscle relaxer
3) no withdrawl after termination
4) No potentiation of ethanol effects

Front 29

Name an alternative anxiolytic
which decreases sleep latency and has similar poperties as benzos?

Back 29

Zolpidem (ambien)
MOA unknown

Front 30

Is Zolpidem a controlled substance?

Back 30

YES

Front 31

What is an alternative anxiolytic that is taken in the middle of the night?

Back 31

Zaleplon (sonata)

lasts 4 hrs.

Front 32

What are the MOA of barbiturates?

Back 32

Prolongs the open time of Cl channels on GABA receptor

Front 33

How do barbiturates work on seizures?

Back 33

Prevent seizure discharge at focus and prevent spread of seizure

Front 34

Name a barbiturate used for seizure when can't control seizure activity.

Back 34

Pentobarbitol

Front 35

SE of barbiturates

Back 35

depress resp. ctr in brainstem
- frequent cause of death
concern in CHF and shock
avoid with liver disease
-induces liver enzymes
-induces own metabolism (lead to tolerance)
-drowsy/hung over feeling
-impairs motor performance

Front 36

What does stimulation of opioid receptors cause?

Back 36

analgesia, sedation, euphoria, pupillary constriction, respiratory depression, bradycardia, constipation, N/V, urinary retention, pruritis

Front 37

What opiod promotes release of histamine and what does this cause?

Back 37

Morphine

causes hypotension and itch

Front 38

Where is Morphine metabolized?

Back 38

liver, excreted in urine

Front 39

Are active metabolites of morphine accumulated in renal failure?

Back 39

Yes

Front 40

Does morphine require a renal adjustment?

Back 40

Yes, decrease dose by 50%

Front 41

Does fentanyl have active metabolites?

Back 41

No

Front 42

Is a dose adjustment required when using fentanyl?

Back 42

No

Front 43

Does fentanyl cause release of histamine?

Back 43

No
less likely to cause hypotension than MSO4

Front 44

What opioid is the preferred agent in patients with hemodynamic instability or renal failure?

Back 44

Fentanyl

Front 45

Fentanyl has potential for drug interactions.

TRUE/FALSE

Back 45

TRUE

through CYP450 pathway

Front 46

Morphine is more lipid soluble and faster acting than Fentanyl.

TRUE/FALSE

Back 46

FALSE
Fentanyl is more lipid soluble and faster acting than morphine.
-prolonged effect with infusion longer than 4hrs
-equivalent analgesia to MSO4 at a lower dose

Front 47

What is the drug of choice for acute pain?

Back 47

Fentanyl (typically in intubated pt's only)

Front 48

Which opioid is metabolized by the liver, has no active metabolites, no histamine release, and no CYP 450 interactions?

Back 48

Hydromorphone (dilaudid)
-slightly faster acting than MSO4
-duration of action similar to MSO4

Front 49

Adverse effects of opioids

Back 49

hypotension, bradycardia, respiratory depression**,
depress bowel movement, pruritis, N/V

Front 50

Which patients are at greatest risk of respiratory depression with the use of opioids?

Back 50

Pt's with sleep apnea syndrome or chronic hypercapnia

Front 51

Why is use limited to 5 days for Ketorolac use?

Back 51

-assoc. with 2 fold increase in risk of renal failure
-increased risk of GI bleeding

Front 52

When must a dose adjustment be made for Ketorolac?

Back 52

-renal impairment
-age >65
-wt<50 kg

Front 53

Which opioid can be an exicitatory neurotoxin and produce CNS excitation?

Back 53

Meperidine

Front 54

How is meperidine metabolized?

Back 54

-In the liver to form normeperidine.
-slowly excreted by kidney
-can accum. with repeated doses, esp with renal impairment

Front 55

What is drug and dose for shivering per lecture?

Back 55

Meperidine 25mg IV

Front 56

More hydrophobic, more potent
More hydrophobic, longer duration of action

Back 56

Aromatic group

Front 57

Shorter duration of action, metabolized plasma esterases
-can have hypersensitivity

Back 57

Ester bond

Front 58

Metabolized in liver, longer duration of action
-hypersensitivity rare, but drugs poorly tolerated with liver disease

Back 58

Amide bond

Front 59

How do nerve blocks work?

Back 59

by blocking ion channels
-principly Na channels (most potent)
-can block K channels at higher concentrations

Front 60

What are the therapeutic uses of local anesthetics?

Back 60

Analgesia, numbness
if with vasoconstrictor:
-decrease removal of anesthetic from site
-longer duration
-less systemic toxicity

Front 61

What type of anesthetic is Procaine (Novocain), how potent, how long acting (approx)?

Back 61

Ester,low potency, short duration of action

Front 62

What type of anesthetic is
Tetracaine, how potent, how long acting (approx)?

Back 62

Ester, more potent, longer duration, slower onset of effect than procaine

Front 63

What type of anesthetic is Liocaine, how potent, how long acting (approx)?

Back 63

Amide, fast onset, duration similar to tetracaine

Front 64

What is the most widely used local anesthetic?

Back 64

Lidocaine

Front 65

What type of anesthetic is Bupivicaine (Marcaine, Sensorcaine), and how long acting is it?

Back 65

Amide, very long duration of action.

Front 66

What is a measure of the concentration of anesthetic required to achieve the anesthetized state?

Back 66

Potency

Front 67

Highly soluble _____ pass into brain and fat.

Back 67

readily

Front 68

highly lipid soluble = ____
potent

Back 68

MOST

Front 69

less lipid soluble = ____ potent

Back 69

LEAST

Front 70

Agents with lowest MAC have the __________ lipid solubilities.

Back 70

greatest

Front 71

Adverse effects with Halothane

Back 71

Myocardial depressant (dec. CO and contraction);
can sensitize heart to catecholamines (EPI WITH CAUTION);
Halothane hepatitis (alg rxn);
Malignant hyperthermia** (genetically defective Ca release)

Front 72

What are S/S malignant hyperthermia?

Back 72

Muscle rigidity
lactic acid accumulation

Front 73

What is antidote for malignant hyperthermia?

Back 73

Dantrolene

Front 74

Why isn't halothane used frequently anymore?

Back 74

good hypnotic, poor analgesic and muscle relaxant

Front 75

Does enflurane have cardiac and respiratory effects like halothane?

Back 75

YES;
but does NOT sensitize heart to catecholamines.

Front 76

Avoid this inhaled anesthetic in seizure prone patients.

Back 76

Enflurane
(may cause sz esp. in high conc with low CO2 levels)

Front 77

Which inhaled anesthetic has NO cardiac depressant effect or sensitization to catecholamines and doesn't foster sz activity?

Back 77

Isoflurane

Front 78

Which inhaled anesthetic has potential for renal toxicity?

Back 78

Enflurane

Front 79

Name 2 ultra short acting barbiturates.
Hint: Meet the Falkers

Back 79

Methohexital sodium
Thiopental

Front 80

When are Methohexital sodium and Thiopental contraindicated?

Back 80

acute intermittent porphyria, shock

Front 81

This agent is a derivative of phencyclidine and causes dissociative anesthesia.

Back 81

Ketamine

Front 82

What is the antidote for opioids?

Back 82

Nalaxone