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NURA-671-01 Advanced Pharmacology > Oral: Opioids > Flashcards

Oral: Opioids Flashcards

1
Q

MOA: Opioids in general

A

Activates Mu1, Mu2, Kappa & Delta receptors located on the peripheral ends of primary afferent neurons to directly ⬇transmission or inhibit the release of neurotransmitters, thereby altering the pain threshold, pain perception, and inhibiting ascending pain pathways.

Opioids mimic endogenous substances at the receptors: presynaptic: ⬇ neurotransmitter release;
postsynaptic: hyperpolarize the neurons by ⬆ K conductance.

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2
Q

Side Effects: That apply to all opioids

A

Miosis, drowsiness, N//V/C (CRTZ), urinary retention, SOO spasm, pruritis;

⬇CBF, ICP if hypoventilation is prevented, ⬇response to CO2 and hypoxia;

DD resp depression, ⬇chest wall compliance, cough suppression,

⬇catecholamine release and cortisol;

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3
Q

Class: Morphine

A

Phenanthrene alkaloid natural opioid agonist

Prototype

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4
Q

Pharmacokinetics: Morphine

A

30% PB; 23% non-ionized; low lipid solubility
Onset = <5 min; peak 15-30 min
DOA = 3 hrs
E1/2t = 3 hrs
Hep + Renal Met
Active metabolite = morphine-3 glucoronide (less active) and morphine-6-glucoronide (650x more potent)
Excreted in urine as M3G – 1-12% unchanged + feces

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5
Q

Side Effects: Morphine

A

Histamine;
dose dependent⬇HR, BP, SVR, CO;

delayed resp dep in spinal and epidurals d/t low lipid solubility;

tolerance, dependence

⬇CBF, ICP;
⬇ CO2 response curve and shift to right;
inhibits SA/AV node, causing brdycardia;
urinary retention, pruritis, SOO spasm, N/V/C;

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6
Q

Contraindications: Morphine

A

Allergy, asthma, COPD, bronchospasm,
synergistic resp dep w/ benzos + other sedatives,
dec dose in renal dz, peds + elderly
⬇dose in RF, only give one (accumulation)

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7
Q

Dose: Morphine

A

IV: usually 2.5-15mg Q 3 – 4 hrs
Anes: 2 mg/kg
Gtt: 1 – 10 mg/hr

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8
Q

Class: Meperidine (Demporol)

A

phenyl-piperidine synthetic opioid agonist (w/an atropine-like structure)

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9
Q

MOA: Meperidine (Demporol)

A

Mu and Kappa receptors

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10
Q

Pharmacokinetics: Meperidine (Demporol)

A 
60% PB; 
10% non-ionized, low/moderate lipid solubility
Onset < 1 min, Peak: 5 – 10 min
DOA = 3 hrs
E1/2t = 3 hrs

normeperidine- longer acting (e1/2t 15-20 hrs) and 1/2 as potent as parent; can cause sz, confusion, hallucination, myoclonus

65% pulmonary 1st pass effect; liver metabolism to normeperidine and excreted in urine

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11
Q

Side Effects: Meperidine (Demporol)

A 
histamine; 
sz;
direct myocardial dep;
mouth dry; 
⬇shivering; 
dependence, tolerance;

urinary retention, N/V/C;
respiratory depression;

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12
Q

Contraindications: Meperidine (Demporol)

A

Fatal interaction with MAOIs;
metabolites accumulate with RF;
careful in CV, neuro disease, sz, asthma

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13
Q

Dose: Meperidine (Demporol)

A

IM/SQ/PO: 50 – 100 mg
IV: 25 – 75 mg
Shivering: 12.5 mg
Do not exceed 1 g/24 hrs.

1/10 potency of morphine

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14
Q

Class: Fentanyl, Sufentanil, Remifentanyl, Meperidine (Demporol)

A

phenyl-piperidine synthetic opioid agonist

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15
Q

Pharmacokinetics: Fentanyl

A 
80% PB; 
8.5% non-ionized; 
high lipid solubility
Onset: 2 min; 
DOA 30-60 min
E1/2t: 3-6 hrs; ctx sen 1/2t: 4.5 hrs "longest context sensitive 1/2 time of all the opioids***"

Min. active metabolite: Norfentanyl

75% pulmonary 1st pass effect; liver metabolism and excreted in urine

100x potency of morphine

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16
Q

Side Effects: Fentanyl

A

pruritus (“fentanyl nose itch”- even though no histamine release);
⬇HR, BP, SVR, CO;
sz-like activity;
wooden chest syndrome;

N/V/C, SOO spasm;
resp dep;

17
Q

Contraindications: Fentanyl

A

brady arrhythmias, liver disease, RF, head trauma, synergistic resp dep w/ bdzs + sedatives
dec dose in renal dz, peds, elderly

18
Q

Dose: Fentanyl

A

IV: 1 – 3 mcg/kg
Premed: 25 – 100 mcg
Intraop: 12.5-100 mcg

TOTAL:
1-10 mcg/kg if extubation is planned;
5-50 mcg/kg if to remain intubated;

19
Q

Pharmacokinetics: Sufentanil

A 
93% PB; 
20% non-ionized; 
highest lipid solubility
Onset 2 min; 
DOA 30 min
E1/2t: 2.5 hrs; ctx sen 1/2t: 30 min

Active metabolite: Desmeth-sufenanil (1/10 as potent)

60% pulmonary 1st pass effect; liver and sm. intestine and excreted in urine 1% unchanges

1,000x potency of morphine

20
Q

Side Effects: Sufentanil

A

⬇HR, BP, SVR, CO, cardiac arrest;
potent resp depressant, apnea, bronchospasm;
wooden chest/muscle rigidity;
dependence, tolerance

SOO spasm;
N/V/C, urinary retention, pruritus;

21
Q

Contraindications: Sufentanil

A

asthma, allergy, airway obstruction;

⬇dose in elderly and hypovolemia

22
Q

Dose: Sufentanil

A

analgesia boluses of 0.1-1 mcg/kg.

anesthesia:
dep on procedure*: 1-8 mcg/kg;
sole anesthesia: 8-50 mcg/kg

23
Q

Class: Alfentanyl

A

tetrazole fentanyl derivative synthetic opioid agonist

24
Q

Pharmacokinetics: Alfentanyl

A 
90% PB; 
90% non-ionized; 
high lipid solubility
Onset: 2 min; 
DOA: 30-60 min
E1/2/t: 1.5hr; Ctx Sen 1/2t: 1hr

Elimination: liver and sm. intestine; leaves the plasma in 30 min

10-20x potency of morphine

25
Q

Side Effects: Alfentanyl

A 
⬆ICP, slowing of EEG; 
no change in SVR or CO; 
skeletal muscle rigidity;
'
respiratory depression; 
SOO spasm, N/V/C, pruritus
26
Q

Contraindications: Alfentanyl

A

untreated parkinsons, ⬆ICP, respiratory depression

27
Q

Dose: Alfentanyl

A

Induction: 50-200 mcg/kg; analgesia: 5-30 mcg/kg

28
Q

Class: Remifentanyl

A

phenyl-piperidine synthetic opioid agonist with ester link

29
Q

MOA: Remifentanyl

A

selective for Mu Receptors

30
Q

Pharmacokinetics: Remifentanyl

A 
80% PB; 
67% non-ionized; 
high lipid solubility
Onset: 2 min
DOA: 10 min
E1/2t: 10min; Ctx sen 1/2t: 4 min

Elimination: metabolized by tissue plasma esterases

100x potency of morphine

31
Q

Side Effects: Remifentanyl

A

Dose dep ⬇HR, BP;

resp depression;
N/V/C, SOO spasm, pruritus

32
Q

Contraindications: Remifentanyl

A 
high doses = dec CMRO2 + CBF
do not use in epidurals/spinals (d/t glycine prep); allergy; 
caution in elderly;
preg class C
33
Q

Dose: Remifentanyl

A

Initial: 0.5-1 mcg/kg (over 30-60sec);
infusion: 0.05-2 mcg/kg/min;
additional bolus: 0.1-1 mcg/kg
NOT FOR INDUCTION

NURA-671-01 Advanced Pharmacology (18 decks)

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