Opioid Analgesics Part III (Other Drugs) Flashcards
1
Q
Mepergan
A
- Meperidine + Promethazine
- Analgesia, sefation, and anti-nausea effects
- Used as a preanesthetic medication
2
Q
Meperidine
A
- Demerol
- Moderate to severe pain
- Less smooth muscle spasm, constipation, and depresssion of cough reflex
- Equianalgesic to morphine
- NO MIOSIS
- SE: Tachycardia
3
Q
Meperidine Toxicity
A
- CNS excitation
- Increased seizure risk (normeperidine especially due to long half life)
- Metabolite is excreted by kidney, don’t use with renal insufficiency
- Naloxone doesn’t inhibit seizures and could worsen the sedative effects
4
Q
Hydromorphone
A
- Dilaudid
- Management of pain
- HP = high potency, Exalgo = ER
- WARNING: high potential for abuse and risk of respiratory depression that could result in death
5
Q
Oxymorphone
A
- Numorphan
- Suppository for moderate to severe pain
- Parenteral administration for moderate to severe pain, support of anesthesia, and relief of anxiety in patients with dyspnea
6
Q
Opana
A
- Oxymorphone
- Oral
- Black box warning for abuse potential
7
Q
Fentanyl
A
- Actiz
- Pain management
- Use IV, epidural
- 100x potency of morphine
- Lipid soluble, terminated by redistribution after IV administration
- Has other preparations like tozenge, film, tablets, patches
- Lazanda Nasal spray only for persistent cancer pain
8
Q
Carfentanil
A
- Synthetic opioid
- 10,000x more potent than morphine and 100x more potent than fentanyl
- Used to tranquilize large animals
9
Q
Fentanyl Black Box Warnings
A
- Abuse potential
- Repiratory depression
- CYP450 3A4 interactions, don’t use with 3A4 inducers since it can increase fentanyl concentration
- Risk of use in combination with benzos and CNS depressants which can cause profound sedation, respiratory depression, coma, and death
10
Q
Remifentanil
A
- Ultiva
- Similar to fentanyl in action and use
- Metabolized by plasma esterases and is eliminated in minutes
- Minute-to-minute control of analgesia
- Can intensify muscle tone causing truncal rigidity when given quickly via IV which can interfere with ventilation
11
Q
Heroin
A
- Diacetylmorphine
- No clinical use in USA
- Crosses BBB rapidly due to high lipid solubility
- Metabolized to monoacetylmorphine and morphine
- Morphine is responsible for the effects of heroin (same SE)
- Schedule 1
12
Q
Heroin Addictive Theory
A
- Ventral tegmental area (DA neurons) prohects to the nucleus accumbens as part of the mesolimbic system
- Most addictive substances affect this area as a final common path
- Faster a drug of abuse gets to this area the more addictive the substance tends to be
13
Q
Methadone
A
- Dolophine
- Orally active
- 15-40 hour half life
- Mu agonist
- Risk of QT prolongation, safe during pregnancy
- Uses: chronic pain, treat narcotic abstinence syndrome, maintenance of opioid use disorder
- Special license to prescribe for methadone maintenance
- Potential for diversion and abuse
- Satisfies cravings and allows a person to function in society
- Recommended minimum 12 mo treatment
- Prolongs QT interval
14
Q
Codeine
A
- Antitussive, analgesic + ASA/APAP
- 10% is metabolized to morphine by CYP2D6
- Limited by low potency (don’t use for severe pain), low affinity for receptor, and frequent N/V
- Prodrug of morphine with limited oral availability
15
Q
Codeine Black Box Warning
A
- Respiratory depression and death in children with CYP2D6 polymorphism that makes them ultra-rapid metabolizers
- Tramadol may have a similar problem
- Alternatives: NSAIDs and APAP, lowest effective weight-based dose used PRN only, CYP3A4 metabolized drugs