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Opioid Analgesics and Antagonists
Derivatives of Morphine (Synthetic and/or purified)
22
Medical
Professional
01/29/2013

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Cards

Term
Alfentanil
Definition
100% synthetic phenylpiperidine
DOC OUTPATIENT USE

80X potency morphine;Short duration

Rapid recovery w/o accumulation metabolites

LIPOPHYILIC LOLLIPOP

Used in cardiac surgery due to cardiac stability in combo with neuromuscle blockers
Term
Codiene
Definition
Chemically modified to reduce first pass effect. prodrug, analgesic = Morphine
CYP2D6 POLYMORPHISM ~1/10 means 10% wont relieve pain!!
Term
Fentanyl
Definition
100% synthetic phenylpiperidine

80X potency morphine;Short duration

Rapid recovery w/o accumulation metabolites

LIPOPHYILIC LOLLIPOP

Used in cardiac surgery due to cardiac stability in combo with neuromuscle blockers
Term
hydrocodone
Definition
Vicodin - semisynthetic from poppy plant with modified first pass effect

Potency ~ hydrocodone >> morphine/codeine
Term
Meperidine
Definition
100% synthetic compound with 1/10 the potency of morphine. Used in LABOR

NO BILIARY SPASM OR MIOSIS
ALSO CAUSES SEIZURES;TREMORS;CONVULSIONS

Avoid MAO inhibitors
Term
Methadone
Definition
100% synthetic oral agonist that is equipotent to morphine

complex pharmacokinetics means metabolites build up in body

HIGHEST RISK OPIOD
Term
Morphine
Definition
CNS: analgesic, respiratory depression, anti-tussive, miosis, tolerance, depencance

Periphral: CONSTIPATION, MUSCLE SPASM, analgesic.

Need to titrate (2/3).

Better against continuous dull over sharp stabbing!

Can cause truncal rigidity so combine with neuromuscular blocker surgery.

Depress medullary and pontine centers for breathing frequency as well as CO center

Trigger acute vomiting at low concentration!

CANNOT DEVELOPE TOLERANCE TO CONSTIPATION

Increases smooth muscle tone causing asthma, urinary retention, increased birthing time

INCREASES CNS PRESSURE, decreases bp for pulmonary edema
Term
Oxycodone
Definition
Percocet - semisynthetic from poppy plant with modified first pass effect

Potency ~ hydrocodone >> morphine/codeine
Term
Remifentanil
Definition
100% synthetic phenylpiperidine

80X potency morphine;Short duration

Rapid recovery w/o accumulation metabolites

LIPOPHYILIC LOLLIPOP

Used in cardiac surgery due to cardiac stability in combo with neuromuscle blockers
Term
Sufentanil
Definition
100% synthetic phenylpiperidine

80X potency morphine;Short duration

Rapid recovery w/o accumulation metabolites

LIPOPHYILIC LOLLIPOP

Used in cardiac surgery due to cardiac stability in combo with neuromuscle blockers
Term
Tapentadol
Definition
MIXED Moderate mu receptor agonist and NE reuptake inhibitor

stable congener of O-desmethyltramadol
Term
Tramadol
Definition
MIXED 5HT releaser, NE uptake inhibitor, weak mu agonist

MOA for analgesia mu independant

Same CYP2D6 as Codience

TOXICITY = SEIZURES
Term
Naloxone
Definition
IV Opioid Antagonists
SHORTEST 1-4HR
Term
Naltrexone
Definition
Oral Opioid Antagonists
-only one administered orally-

LONGEST 24-48HR
Term
Nalmefene
Definition
IV Opioid Antagonists
MID~ 10HR
Term
Phalanthrenes
Definition
Morphine, codiene, hydrocodone,oxycodone, dihydrocodiene

MOre phalanthrene arrive COD
Term
Phenylpiperidines
Definition
Mepiridine
fentanyl
alfentanyl
sufentanyl
remifentanyl

Me FEAL SURE phenylpiperidines
Term
phenyheptanones
Definition
methadone
Term
Tolerance Opioid
Definition
Opioid receptor upregulation at nociceptors stimulated by local
inflammation/ injury

Not same degree as stimulatory effect
can shift lethal dose
Term
contraindication opiods
Definition
Head injury
Hepatic/renal dysfunction
hypothyroid
pregnancy
Term
Morphine prototype
Definition
So Far: Morphine as a prototype
 Central actions (analgesia, respiratory depression,
antitussive, miosis, euphoria, dependence liability)
 Peripheral actions (constipation, increased smooth muscle
tone, analgesia)
 Acute toxicity (respiratory depression can be life
threatening)
 Tolerance and
Term
Concerns morphine
Definition
Pulmonary Edema
Acetominophen toxicity
polypharmacy

Morphine may trigger mast cell degranulation and make patient itchy--> switch classes
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