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Summer Pharm (2016) ** > Opioids - the drugs > Flashcards

Opioids - the drugs Flashcards

1
Q

drugs in the order of onset

A

Fast:

Alfentanil, Remifentanil: 1-3 min (≈ 1.1 - 1.4 min to equilibrate with the brain)

Semi-fast:

Fentanyl ≈ 1-2 min (≈ 6.8 min to equilibrate with the brain)

Sufentanil 1-3 min (≈ 6.2 min to equilibrate with the brain)

Meperidine <5 min

Slow

Morphine ? (peak 15-30 min)

Hydromorphone <30 min

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2
Q

tetrazole fentanyl derivative

A

alfentanil

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3
Q

can cause seizure

A

Meperidine (Demerol)

normeperidine, the active metabolite, is long acting (3 days) and half as potent; redosing & stacking doses puts pts at risk for seizures

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4
Q

Alfentanil contraindication

A

Parkinson’s - drug decreases dopaminergic transmission

increased ICP

use with caustion in asthma, head injury, drug dependency, respiratory conditions

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5
Q

opioids in the order of non-ionized %

A

Meperidine 7%

Fentanyl 8.5%

Sufentanil 20%

Morphine 23%

Remifentanil 58%

Alfentanil 89%

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6
Q

oipoid that has some myocardial depression

A

Meperidine (Demerol)

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7
Q

drug that has more sedation but less euphoria than morhine

A

hydromorphone

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8
Q

Slows EEG

A

Alfentanil

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9
Q

no effect on HR or MAP

A

Alfentanil

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10
Q

opioids in the order of Vd

A

Low

Alfentanil 0.4 L/kg (27 L)

Remifentanil 0.4 L/kg (30 L)

High

Sufentanil 3 L/kg (123 L)

Morphine 4 L/kg (224 L)

Meperidine 4 L/kg (305 L)

Fentanyl 4 L/kg (335 L)

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11
Q

order of potency - with relative potencies

(compared with MSO4)

A
  1. Sufentanyl 1000 X MSO4
  2. Remifentanyl 100-150 X MSO4
  3. Fentanyl 100 X MSO4
  4. Alfentanyl 10-20 X MSO4
  5. Dilaudid (hydromorphone) 5 X MSO4
  6. Morphine (MSO4)
  7. Demerol 1/10 X MSO4
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12
Q

metabolized by the liver and small intestine

A

Sufentanil

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13
Q

opioids in the order of protein binding

A

Hydromorphone 20%

Morphine 35%

Meperidine 50-70%

Fentanyl 84%

Remifentanil 66-92%

Alfentanil 92%

Sufentanil 93%

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14
Q

Has muscarinic effect

A

Meperidine (Demerol)

due to atropine like structure

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15
Q

hydromorphone contraindications

A

gi obstruction

asthma

hypersensitivity

severe resp depression

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16
Q

Remifentanil - metabolism, Vd, PB

A

metabolism: nonspecific plasma and tissue esterases (not pseudocholinesterases -> not affected by cholinesterases deficiency)

Vd = 0.3-0.5L/kg (small)

PB: 66-93%

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17
Q

alfentanil context sensitive E½t

18
Q

drugs for neuraxial pain management

A

meperidine

morphine

fentanyl

19
Q

Alfentanil

metabolism, redistribution, E1/2t, Vd, PB

A

metabolism - liver to inactive metabolite noralfentanyl

rapid reditribution due to being 90% non-ionized

E1/2t = 90 min (1.5hrs)

Vd = 0.4L/kg (small) or 27 L

protein bound - 92% (mostly to alpha 1 acid glycoprotein)

20
Q

lowers BP more than fentanyl

A

alfentanil

21
Q

Histamine release

A

Morphine

Meperidine

Succinylcholine

Atracurium

Mivacurium

Barbiturates - if given FAST

22
Q

Meperidine

onset , DOA, Vd, E1/2t, PB

A

Onset < 5 min

DOA 3-4 hrs

Vd 3.5-5L/kg (large)

E1/2t 3-5 hrs

PB 40-70% (mostly to albumin & alpha 1 acid glycoprotein)

23
Q

Non-ionized percentages

A

Meperidine - 7%

Fentanyl - 8.5%

Sufentanyl - 20%

Morphine - 23%

Remifentanyl - 58%

Alfentanyl 89%

24
Q

Meperidine contraindications

A

MAOIs - serotonin syndrome

chronic kidney disease - seizures (normeperidine)

crosses the placenta and breast milk - avoid

25
Q

fentanyl context sensitive E½t

26
Q

increased heart rate

A

meperidine

atropine like structure

27
Q

drugs with pulmonary first pass effect

A

fentanyl 75%

sufentanil 75%

meperidine 65%

28
Q

alpha 2 agonistic effects

A

Meperidine (Demerol)

therefore causes sedation

alpha 2 + kappa activation = used in anti-shivering

29
Q

sufentanil context sensitive E½t

30
Q

order of potency

(high to low)

A
  1. Sufentanyl
  2. Remifentanyl
  3. Fentanyl
  4. Alfentanyl
  5. Dilaudid (hydromorphone)
  6. Morphine (MSO4)
  7. Demerol

She Ran Far Away Down Main Drive

31
Q

narcan/nalaxone class

A

N-alkyl derivative of oxymorphone

32
Q

order of potency - with relative potencies

compare to fentanyl

A
  1. Sufentanyl 10 X fentanyl
  2. Remifentanyl 1 - 1.5 X fentanyl
  3. Fentanyl
  4. Alfentanyl 1/5 X fentanyl
33
Q

Morphine metabolism

A

hepatic conjugation with glucoronic acid

renal excretion (metabolites as well as up to 12% excreted unchanged)

feces excretion: 7-10%

active metabolites: morphine-6-glucoronide (more potent) and normorphine

34
Q

remifentanil context sensitive E½t

35
Q

cannot be used in epidurals

A

Remifentanil - glycine prep

36
Q

bases or acid?

opioids

barbs

benzos

ketamine

A

opioid = weak base

barbs = alkaline in the bottle, acid at physiologic pH

benzos = bases

ketamine = base

propofol = acid

37
Q

Blocks Na+ channels

A

Meperidine (Demerol)

similar mech as local anesthetics

38
Q

fentanyl pharmacokinetics

PB

Metabolism/Excretion

Distribution/redistribution time

Duration of action

Vd

E1/2t

context sensitive E1/2t

A

the lungs take ≈ 75% of injected dose

80% bound to plasma (≈40% taken by the RBC)

distribution time of 1.7 minutes

redistribution time of 13 minutes

long acting due to the wide redistribution in body tissues (DOA = 60 min)

metabolized by the liver

less than 10% of fentanyl is excreted unchanged in the urine

Vd= 4L/kg (335L)

E1/2t 3-6 hrs

context sensitive E1/2t 260 min (≈4hrs)

39
Q

drug in the order for duration of action

A

remifentanil 10 min

sufentanil 30 min

Alfentanil 30-60 min

Fentanyl 1 hr

Meperidine 3 hrs

Morphine 3-4 hrs

Hydromorphone 4-5hrs

40
Q

opioid dosages

A

Sufentanil 0.1 - 1 mcg/kg

Remifentanil 0.5 - 1 mcg/kg

Fentanyl 25 - 100 mcg (analgesia 1-2mcg/kg)

Alfentanil 5 - 30 mcg/kg

Hydromorphone 0.5 - 2 mg

Morphine 2.5 - 15 mg

Meperidine 5 mg Q 5 min (Shivering 12.5-50mg)

Narcan 0.1 - 2 mg IV

Summer Pharm (2016) ** (17 decks)

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