Pharmokinetics Flashcards

1
Q

Routes of administration for opiates

A

Oral
IV
SC
IM
Transdermal patch (fentanyl)
Epidural
Intrathecal
Patient-controlled analgesia (PCA)

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2
Q

Opioids get distributed throughout all tissues

A

Exert their principle analgesic effects after they reach the CNS

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3
Q

Where does biotransformation primarily take place?

A

Liver

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4
Q

Where and how does excretion occur?

A

Excretion of drug metabolite and to a lesser extent the intact drug in the urine via the kidneys

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5
Q

Morphine

A

Morphine-6-Glucuronide (more potent than morphine)

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6
Q

Meperidine

A

Has an active metabolite (normeperidine), which may cause seizures at thigh plasma levels (particularly in elderly patients and pts with impaired renal/hepatic function)
Not for chronic pain

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7
Q

Methadone

A

Very long duration of action

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8
Q

Time for peak efficacy
- Morphine

A

20 minutes

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9
Q

Time of the duration of action
- Morphine

A

4 hours

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10
Q

Time for peak efficacy
- Meperidine

A

15 mins

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11
Q

Time of duration of action
- Meperidine

A

2-4 hours

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12
Q

Time of peak efficacy
- Fentanyl

A

5 mins

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13
Q

Time of duration of action
- Fentanyl

A

15-30 mins

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14
Q

Intrathecal and epidural

A

Use significantly lower doses and provide regional analgesia while decreasing systemic side effects

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15
Q

Patient controlled analgesia (PCA pumps)

A

Allow patients to control opiate injections using a parenteral (I.V.) injection devise

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16
Q

Analgesia

A

They relieve pain both by raising the pain threshold at the SC level and by altering the brain’s perception of pain
Induce sleep in clinical situation when pain is present and sleep is neccessary

17
Q

Opiate analgesics

A

Represent the mainstay of therapy for the treatment of pts with acute (postoperative) and chronic pain

18
Q

Less drug is need to prevent what?

A

Recurrence of pain than to relieve it

19
Q

Cough suppression

A

Dextromethorphan

20
Q

Acute pulmonary edema
- morphine only

A

Morphine used to decrease anxiety and decrease the perception of shortness of breath

21
Q

Adjunct in anesthesia

A

Morphine
Fentanyl

22
Q

Treatment of diarrhea

A

Diphenoxylate and loperamide (OTC)

23
Q

Adverse effects of opiates

A

Sedation, drowsiness, mental clouding and coma (at toxic doses)
Mitosis (pinpoint pupil)
Euphoria
Constipation (severe)
Urinary retention
Respiratory depression
Nausea
Itching
Addiction liability

24
Q

Adverse effects of opiates
- Miosis (pinpoint pupil)

A

Important diagnostically bc other causes of coma and respiratory depression produce dilation of pupil

25
Q

Adverse effects of opiates
- Euphoria

A

D/t DA release in the nucleus accumbens

26
Q

Adverse effects of opiates
- Constipation (severe)

A

Stool softeners and laxatives should be initiated early

27
Q

Adverse effects of opiates
- Urinary retention

A

Increase antidiuretic hormone

28
Q

Adverse effects of opiates
- Respiratory depression (cardinal toxic effect)

A

D/t a reduction in the responsiveness of the respiratory center to increase CO2 tension

29
Q

Averse effects of opiates
- Itching

A

D/t opiate
Induced histamine release

30
Q

Opiates contraindications

A

Head trauma
Neonates
Opiate-induced miosis
Respiratory depression

31
Q

Opiates contraindications
- Head trauma

A

Increase intracranial pressure (ICP) from vasodilation and increase CSF volume

32
Q

Opiates contraindications
- Neonates

A

Should not receive morphine bc of their low conjugating capabilities and immaturity of BBB

33
Q

Opiates contraindications
- Opiate-induced miosis

A

Masks the pupillary response used to diagnose concussion

34
Q

Opiates contraindications
- Risk of respiratory depression

A

From heroin is related to its active metabolites (6- acetlymorphine and morphine)

35
Q

Tolerance

A

Repeated administration of therapeutic doses of the opiates causes gradual loss of effectiveness

36
Q

In order to reproduce the original response

A

Larger dose is needed

37
Q

Cross-tolerance

A

Pt tolerant to one opiate drug will also show some degree of tolerance to other opiate agonists

38
Q

Tolerance does not develop to

A

Mitosis and constipation