Opioids - the drugs Flashcards Preview

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

Flashcards in Opioids - the drugs Deck (40)
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1

drugs in the order of onset

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

2

tetrazole fentanyl derivative

alfentanil

3

can cause seizure

Meperidine (Demerol)

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

4

Alfentanil contraindication 

Parkinson's - drug decreases dopaminergic transmission

increased ICP

 

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

5

opioids in the order of non-ionized %

Meperidine 7%

Fentanyl 8.5%

Sufentanil 20%

Morphine 23%

Remifentanil 58%

Alfentanil 89%

6

oipoid that has some myocardial depression

Meperidine (Demerol)

7

drug that has more sedation but less euphoria than morhine 

hydromorphone

8

Slows EEG

Alfentanil

9

no effect on HR or MAP

Alfentanil

10

opioids in the order of Vd

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)

11

order of potency - with relative potencies

(compared with MSO4)

  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

12

metabolized by the liver and small intestine

Sufentanil

13

opioids in the order of protein binding 

Hydromorphone 20%

Morphine 35%

Meperidine 50-70%

Fentanyl 84%

Remifentanil 66-92%

Alfentanil 92%

Sufentanil 93%

 

14

Has muscarinic effect

Meperidine (Demerol)

due to atropine like structure 

15

hydromorphone contraindications

gi obstruction

asthma

hypersensitivity

severe resp depression

16

Remifentanil - metabolism, Vd, PB 

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

Vd = 0.3-0.5L/kg (small)

PB: 66-93%

17

alfentanil context sensitive E½t

60 min

18

drugs for neuraxial pain management 

meperidine

morphine

fentanyl

19

Alfentanil 

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

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

lowers BP more than fentanyl 

alfentanil

21

Histamine release

Morphine 

Meperidine

 

Succinylcholine

Atracurium

Mivacurium

Barbiturates - if given FAST

22

Meperidine 

onset , DOA, Vd, E1/2t, PB

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

Non-ionized percentages

Meperidine - 7%

Fentanyl - 8.5%

Sufentanyl - 20%

Morphine - 23%

Remifentanyl - 58%

Alfentanyl 89%

24

Meperidine contraindications

MAOIs - serotonin syndrome

chronic kidney disease - seizures (normeperidine)

crosses the placenta and breast milk - avoid

25

fentanyl context sensitive E½t

260 min

26

increased heart rate

meperidine

atropine like structure

27

drugs with pulmonary first pass effect

fentanyl 75%

sufentanil 75%

meperidine 65%

28

alpha 2 agonistic effects

Meperidine (Demerol)

therefore causes sedation

 alpha 2 + kappa activation = used in anti-shivering 

29

sufentanil context sensitive E½t

30 min

30

order of potency

(high to low)

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

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