test 2 - opioids and hypnotics

Question 1

drugs included

Answer 1

morphine sulfate 
naloxone 
nalbuphine 
codeine 
zolpidem

Question 2

prototype for narcotic class

Answer 2

morphine

Question 3

morphine

Answer 3

(Schedule II)

is standard against which new analgesics are measured

Question 4

action of morphine

Answer 4

Central action on perception of pain. Primary site is sensory cortex. Also alters attitudes by psychological, sedative, and hypnotic effects.

Question 5

what receptors does morphine interact with

Answer 5

It is an agonist which interacts with mu and kappa receptors in brain and other tissues. Receptors are widely but unevenly distributed throughout CNS, with highest concentration in limbic system (frontal and temporal cortex, amygdala, and hippocampus), thalamus, striatum, hypothalamus, midbrain, and spinal cord.

Question 6

effects morphine has on CNS

Answer 6

analgesia, drowsiness, changes in mood, mental clouding

	a. constricted pupils (probably central action on oculomotor nerve) b. respiratory center--depresses brain stem, decreases response to CO2.  (may take up to 30 min. after IM injection to see this.) c. Post-medulla-chemoreceptor trigger zone (CTZ) is directly stimulated.  All clinically useful opioids produce some degree of N/V.

Question 7

Effects of morphine on CV

Answer 7

supine, no major effects on BP, pulse rate and rhythm. Does dilate
resistance vessels, leading to postural hypotension. Most opioids provoke the release of histamine which may be cause of hypotension. Does affect cerebral vessels, too. (Do NOT use with head injury - increases intracranial pressure)

Question 8

effects of morphine on GI

Answer 8

MAIN EFFECT IS CONSTIPATION!! SLOWS DOWN MOTILITY AND DECREASE SECRETIONS
stomach–decreases secretion of hydrochloric acid, decreases motility, increases tone in antrum and duodenum which leads to delay in gastric emptying (as much as 12 hours.) This is ½ of the cause of constipation.
b. small intestine–decreases biliary and pancreatic secretions, may increase non-propulsive contractions, decreases propulsive contractions markedly. Upper small intestine is affected more than lower. This is ¼ of constipation problem.

c. large intestine–decreases or abolishes propulsive contractions, increases tone to point of spasm, increases tone of sphincter. This is ¼ of constipation problem.
d. biliary tract–marked increase in biliary tract pressure which leads to spasm.

Question 9

effects of morphine on smooth muscle

Answer 9

ureter–increases tone and amplitude of contractions of ureters, especially lower 1/3

b. bladder–increases tone leading to urgency. Increases tone of sphincter leading to retention
c. uterus–prolongs labor; male-decreases libido
d. bronchial–large doses lead to bronchoconstriction

Question 10

effects of morphine on skin

Answer 10

therapeutic doses cause cutaneous blood vessels to dilate–leading to flushed and warm face, neck and upper thorax. (may be due to release of histamines–also reason for pruritus and sweating.)

Question 11

pharmacokinetics of morphine

Answer 11

Absorption–readily absorbed from GI tract but does have “first-pass” phenomenon in liver. Also absorbed from sub-cu and IM routes.
Distribution–rapid and wide. 1/3 is bound.
Metabolism–in liver
Excretion–by kidney, especially by glomerular filtration of metabolites

Question 12

dosage of morphine for adult/child

Answer 12

adult: 5-15 mg q4h
child: 0.1-0.2 mg/kg/dose

Question 13

ADRs of morphine

Answer 13

can readily see from effects under action.

can have allergic - skin rashes, edema. Tolerance, ABUSE!

Question 14

different types of opioids

Answer 14

meperidine (demerol)
percocet
percodan
vicodin and norco
dilaudid

Question 15

meperidine (demerol)

Answer 15

(Schedule II) is synthetic

GI effects are less, so less constipation and less biliary spasm; also less urinary retention; and less effect on uterus.
causes hypotension; good for rigors or post-anesthesia shivering; is not good for cough and diarrhea
Effects are additive; and don’t last as long; is also protein bound (40-60%); 50% escapes “first pass”

Question 16

percocet (oxycodone and acetaminophen)

Answer 16

schedule 2

Question 17

percodan (oxycodone and aspirin

Answer 17

Oxycodone is a derivative of Morphine. Is 5-6 times more potent than Codeine

Question 18

vicodin and norco

Answer 18

hydrocodone and acetaminophen

schedule 2

Question 19

dilaudid

Answer 19

hydromorphone

schedule 2

Question 20

Naloxone (narcan) classification

Answer 20

narcotic antagonist

Question 21

action of naloxone

Answer 21

Is a “pure” antagonist, with no agonist or resp. depressant effects. Blocks opioid receptor

Question 22

pharmacokinetics of naloxone

Answer 22

Absorption: Oral–good, but “first pass” extensive (1/50th as potent as IV)
Distribution: IV–onset 1-2 min; SC/IM – 2-5 min; duration 1hr (IV); crosses placenta.
Metabolism: liver

Question 23

ADR of naloxone

Answer 23

will cause withdrawal symptoms if addicted to opioid

Question 24

dosage of naloxone for adult

Answer 24

0.01 mg/kg

usually 0.8 is usual dose for adult IV

Question 25

Special information of naloxone

Answer 25

Used to reverse narcotics effects of anesthesia, or in cases of overdose.
buprenorphine/naloxone – Suboxone/Subutex, is used for treatment of opioid dependence. Buprenorphine is a partial opioid agonist – combined with naloxone to avoid a “high.”
naltrexone

Question 26

naltrexone

Answer 26

ReVia, is used for alcohol dependence/withdrawal as well as opioid-dependent clients.

Question 27

Nalbuphine (nubain) classification

Answer 27

narcotic-agonist-antagonist

Question 28

action of nalbuphine

Answer 28

Combines with kappa receptors producing analgesia.

Also acts as a partial antagonist at mu receptors.

Question 29

pharmacokinetics of nalbuphine

Answer 29

Absorption: IM good; oral only 20% as potent as IM Can also be given SC or IV
Distribution: Onset 15 min. Duration 3-6 hr.
Metabolism: Liver
Excretion: Kidney

Question 30

ADRs of nalbuphine

Answer 30

Sedation, sweatiness, clamminess, N/V, dizziness, vertigo, dry mouth, headache, resp. depression.

Question 31

dose of nalbuphine

Answer 31

10mg/70kg

Question 32

special information of nalbuphine

Answer 32

Can be reversed by Narcan

					2. Has low abuse potential
					3. Also, buprenorphine

Question 33

codeine classification

Answer 33

Narcotic analgesic – oral; antitussive also

Question 34

action of codeine

Answer 34

Binds to opioid receptors and produces mild to moderate pain relief.
Converted to morphine when metabolized. Some individuals are “ultra- rapid” converters – who then achieve dangerously high morphine levels.

Question 35

pharmacokinetics of codeine

Answer 35

Absorption– readily oral (rarely given IV, IM, or subcu)
Distribution–
Metabolism– liver; 10% of dose is converted to morphine
Excretion– metabolite is slowly excreted by kidney

Question 36

adrs of codeine

Answer 36

respiratory depression, constipation, urinary retention, and miosis, though less than with morphine

Question 37

dosage of codeine

Answer 37

Adults – 15-60 mg every 3-6 hours (max 120 mg/24 hr)

Children >1 yr. = 0.5 mg/kg every 4-6 hours (max 60 mg/24 hr)

Question 38

special information of codeine

Answer 38

1. Requires higher dosing to achieve pain relief – side effects can be significant as dosing rises.
2. Can be an effective cough suppressant – but dose lower (10 mg)
3. 200 mg po codeine = 30 mg po morphine

Question 39

zolpidem (ambien) classification

Answer 39

Hypnotic, non-BZD (benzodiazepine)

Question 40

action of zolpidem

Answer 40

Binds to benzodiazepine receptors in the brain.

Question 41

pharmacokinetics of zolpidem

Answer 41

Absorption: rapidly absorbed from GI tract (given orally)
Distribution: peak concentration in 1-2 hours; half-life prolonged in elderly and those with hepatic dysfunction.
Metabolism: liver.
Excretion: urine, bile, feces.

Question 42

adrs of zolpidem

Answer 42

dizziness, headache, nausea, diarrhea, next-day drowsiness (only 1-2 %); higher incidence of ADRs with higher dosages (esp. > 20mg). Sleep driving, and other sleep-related behaviors also seen.

Question 43

dosage of zolpidem

Answer 43

5-10 immediately before bedtime (rapid onset)

Question 44

special information regarding zolpidem

Answer 44

1. Acts like a benzodiazepine but is structurally different.
2. *In January 2013, dosages were lowered (essentially cut in half); 5 mg for women, and 5-10 mg for men.
3. Short-term treatment not associated with withdrawal symptoms, tolerance, or dependence.
4. Ambien CR – is extended-release formula; also orally disintegrating tablets, oral spray, and sublingual tablets
5. Classified as Schedule IV
6. Also zaleplon (Sonata) and eszoplicone (Lunesta)
   (the “z” drugs).