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Dental Therapeutics Exam 1 > Opiate Analgesia > Flashcards

Opiate Analgesia Flashcards

1
Q

Endogenous Opiates

A

Desensitize endogenous sensory perception during stress response, Regulate eating, Reduce immune response, Contribute to craving for tobacco or alcohol, Regulate gender-reproductive function

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2
Q

Classes of Endogenous Opiates

A

POMC - Pro-Opi-Melano-Cortin - Provides control over numerous bodily functions
Pro-Enkephalin to Enkephalin - Methionine and Leucine Enkephalin
Pro-Dynorphine to Dynorphine - Dysphoria or Withdrawl, Opiate antagonist almost, A and B
Endomorphins - Small peptides that are potent “mu” agonists (“mu” receptors for analgesia)
Orfanin FQ/Nociception - Opiate antagonists almost

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3
Q

Morphine

A

Opiate; Balanced agonism - Gi/Go (Analgesia)
Partial agonist - Beta-Arrestin (Ability to hold receptor inside cell limited)
Less likely to lead to rapid tolerance; Binds Mu and DM receptor

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4
Q

Mu Receptor

A

MOP; Analgesia, Respiratory depression, Sedation, Euphoria, Miosis, GI-Appetitie

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5
Q

Delta Receptor

A

DOP; Not as potent analgesia, Reward, Appetite, Endotoxic shock

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6
Q

Kappa Receptor

A

KOP; Not as potent analgesia (Mixed agonist), Diuresis, Locomotor, Miosis (weak), Respiratory depression (weak), Dysphoria, Anti-Mu

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7
Q

NOP Receptor

A

Opiate antagonist; Diuresis, Locomotor inhibition, Gender hormone regulation, Dysphoria, Increase appetite

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8
Q

NMDA Receptor

A

Glutamate receptor

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9
Q

Dentistry Opiates

A

Phenanthrene; Not in synthetic agents; In those from Opium itself; Morphine CII (Water soluble), Codeine CIII (Methylated on hydroxy group), Hydrocodone CII (Hydroxy group is ketone, More lipid soluble, More available oral), Oxycodone CII

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10
Q

Codeine

A

Active on Mu, Delta and DM receptor

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11
Q

Pentazocine

A

Mixed agonist and antagonist, Kappa receptor, Less respiratory depression, Not as profound analgesia

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12
Q

Meperidine

A

Shorter acting than Phenanthrene, Clinical, ex. Meperidine and Fentanyl

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13
Q

Methadone

A

Longer acting than Phenanthrene, Clinical, ex. Methadone, Levomethadryl (Orlamm), Propoxyphene

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14
Q

Opiate Agonists on CNS

A

(CNS - some PNS); Analgesia (“aching” pain), Sedation (not necessary for analgesia - excitation in some), Euphoria (May be dysphoria), Respiratory (Depression can cause death, May relieve oxygen deficiency anxiety in MI, “Stiff chest”), Miosis (Constrict), Cough suppression, Emetic - Antiemetic (Vomit), Craving, Appetite hormones - POMC/CART to anorexic, NPY and AgRP to arrexogenic neurons - Regulators of glucose homeostasis - Sense circulating adiposity - Signals like insulin and leptin; Other - Decrease hormones (CRF, GNRH, LH, FSH, Increase Prolactin and ADH), Learning and memory and Brain excitability-induced-seizure-like brain activity

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15
Q

POMC - Pro-Opi-Melano-Cortin Hormones

A

ACTH, Beta-Endorphin, MSH - Melanocyte Stimulating - MC1 = Pigment, MC2 = Cortisol, MC3 = Energy/Weight, MC4 = Satiety, Erection, MC5 = Adipocytes, Exocrine glands

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16
Q

CNS Action Sites of Opiates

A

Thalamus-Hypothalamus, Midbrain (PAG), Medulla, Dorsal Horn Spinal Cord; Insular cortex, Cingulate cortex, Frontal cortex

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17
Q

Opiate Agonists - Somatic Actions

A

Cardiovascular - Little direct heart action (except. endomorphin), Orthostatic hypotension (N.Solitarious and N.Ambiguouus); GI - Constipation, Dry mouth; Urinary retention, Uterine relaxation, Analgesia, Immune (CNS and PNS; Some release Histamine, Immune reaction inhibition, Peptides on nerve injury), Skin

18
Q

Opiate Drugs

A

Morphine, Codeine, Oxycodone, Oxymorphone, Hydrocodone, Hydromorphone, Meperidine, Fentanyl (Potent), Carfentanil (100X potency), Methadone, D-propoxyphene (Longer pharmacokinetics than Codeine), Tramadol & Tapentadol (Extended spectrum), Etorphine (1000X potency)

19
Q

Morphine Elimination and Dose

A

CYP3A4 - Glucuronidation UTG, ER product (MS Contin Arymo, Kadian REMS)

20
Q

Codeine Elimination

A

CYP2D6 - UTG, 6CG,

21
Q

Oxycodone Elimination

A

CYP3A4 - Pglycoprotein Inducer; Extended release (Oxycontin - 2X potent as MSContin)

22
Q

Hydrocodone Elimination

A

CYP2D6, CYP3A4; Hysingla ER - REMS

23
Q

Fentanyl Elimination and Dose

A

CYP3A4, Transdermal patches (Duragesic - REMS), Oralet (lozenges, Sucrose based lozenges - Affects teeth)

24
Q

Methadone Elimination

A

CYP3A4

25
Q

Propoxyphene

A

CYP3A4

26
Q

Remifentanil

A

No p450 drug interactions, Anesthesia induction, Tissue phosphatases or esterases

27
Q

Meperidine

A

CYP3A4

28
Q

Tramadol

A

(Ultram), CIV, CYP3A4, Double half life of Codeine; Weak opiate and norepinephrine reuptake blocker, M1 metabolite - Actual opiate antagonist, 200X stronger as opiate than prodrug for pain (CYP2D6), More likely for chronic pain, Half-life longer than Codeine and metabolites (6-8hr)

29
Q

Tapentadol

A

(Nucynta), CII, Active; Not converted to active metabolite, Moderate to severe pain

30
Q

Contraindications to Opiates

A

Head Trauma (Greater pressure), Emphysema, Asthma, Other respiratory depressants, Chronic pain (Unless terminal illness), Hypothyroid or Addison’s Disease, When analgesia will obscure diagnosis, Black box warning for Codeine in children undergoing tonsillectomy or adenoidectomy

31
Q

Opiate Drug Interactions

A

CNS Depressants (Barbiturates, Benzodiazepines, Antihistamines etc), Local Anesthetics, Beta Blockers and Calcium Channel Blockers (Increase orthostatic hypotension), Neuroleptics (Sedation, Dopamine blocking drugs), Tricyclic Antidepressants (CNS depression), Mao-A-Inhibitors - Meperidine (Toxicity), Opiate Antagonists, P450, UGT or P-glycoprotein interactions

32
Q

Opiate Antagonist

A

Naloxane (Competitive inhibitor, No effect on normal, Oxycodone with bulky side chain), Nalmephene (Revex) - Kinetics identical to phenenthrene - effects may wear off before opiate, Naltrexone (Trexan, ReVia)

33
Q

Quatinary Opiate Antagonist

A

Reduce opiate constipation
Methylnaltrexone (Relistor)
Alvimopan (Entereg)

34
Q

Opiate Antagonist Use

A

Reverse opiate receptor actions of opiates (Reverse respiratory depression, Reverse analgesia, Precipitate withdrawl reactions in dependent, Reverse opiate overdose), May improve vascular function in septic shock, May reduce puritis in cholestatic jaundice, May reduce craving in alcohol or smoking cessation w/counseling, May partially antagonize effects of alcohol and sedative agents, Quaternary - Relieve opiate constipation or post op illius, Research use; Warning - 1-2hr observation, Cautious in creating withdrawal

35
Q

Mixed Agonist-Antagonist Analgesics

A

Kappa receptor agonists: Analgesics, Diuresis, Locomotor impairment; Mu receptor agonists: Mixed agents with partial agonism; Other antagonists - Levallorphan (Mixed), Nalorphine (Mixed); Differences to agonists - Ceiling or reduced respiratory depressant effect, Reduce abuse liability, More psychosis like side effect (Kappa/Sigma receptors, Withdraw from endogenous opiate), Precipitate withdrawal in opiate dependent, Produce drowsiness

36
Q

Buprenorphine

A

(Buprenx), CIII, Partial mu agonist, Kappa antagonist -Useful in opioid cessation therapy

37
Q

Rapid Detoxicfation

A

Young people w/out long dependence - Naltrexone (anesthesia), Clonidine (alpha2 - Symp overdrive)

38
Q

Withdrawal

A

Switch patient to long acting agent (Morphine to Methadone) and withdraw agent slowly, Clonidine detox, Naltrexone detox

39
Q

Maintenance

A

Methadone maintenance - Supply Methadone, Adjust dose to where it is difficult to overcome effect, Buprenorphine mixture - Suboxone

40
Q

Meperidine

A

(Demerol), Abuse by medical personnel - Pupillary constriction, Few GI side effect, Readily available; Analogs of Fentanyl are “designer drugs” - Potent, Increase in overdose and death

Dental Therapeutics Exam 1 (4 decks)

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