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
16
Q
Oxycodone
A
- Oxaydo, Oxecta
- Opioid agonist for mild to severe pain
- Used in combination with ASA, APAP, and ibuprofen
- Targiniq ER = Oxycodone and naloxone
17
Q
Apomorphine
A
- Apokyn
- Little analgesic activity may dperess respiration
- D2 receptor agonist - induces vomiting by directly acting on CTZ
18
Q
Hydrocodone
A
- Antitussive and pain relief
- Used for nail congestion and moderate pain as well
19
Q
Brands of Hydrocodone
A
- Histinex HC (Hydrocodone, phenylephrine) - nasal congestion
- Hycodan (Hydrocodone, homatropine) - prevent abuse
- Hycotuss (Hydrocodone and guaifenesin) - expectorant
- Tussionex (Hydrocodone and chlorpheniramine) - antihistamine
- Vicodin (hydrocodone + APAP) - pain relief
- Apadaz (Benzhydrocodone _ APAP) - acute pain, gi metabolism to hydrocodone
20
Q
Zohydro ER
A
- ER hydrocodone without APAP
- Can be crushed and abused
- Box warning: addiction, abuse, misuse, life threatening respiratory depression
21
Q
Pentazocine
A
- Talwin
- Oral
- Analgesic for mild to moderate pain
- Weak mu antagonist or partial agonist
- Blocks morphine analgesia and induces opioid withdrawal in the dependent
- DOESN’T block morphine respiratory depression
- Kappa agonist effects are blocked by naloxone
22
Q
Pentazocine Effects
A
only has limited respiratory depression risk
- Agonist at kappa and sigma receptors
- Withdrawal has mild morphine like syndrome
- Dysphoria and uncontrolled, strange thoughts occur with repeated high doses
23
Q
Butorphanol
A
- Stadol
- Parenteral supplement to balanced anesthesia for pre/post-operative analgesia
- Stadol NS (nasal spray) used to manage pain
- Mu antagonist (induces abstinence syndrome in dependent) and kappa agonist (analgesic activity)
- SE: limited respiratory depression, lower incidence of psychotomimetic effects, mild abstinence syndrome
24
Q
Buprenorphine
A
- Buprenex
- CIII
- Analgesic for moderate to severe pain
- Partial agonist at mu receptors (high affinity, low dissociation)
- Repiratory depression is less than other mu agonist, euphoria, and mild morphine type abstinence syndrome
- Replacement for methadone as a maintenance drug for opioid use disorder
- Displaces opioid and causes withdrawal, used for opioid maintenance and detoxification
25
Q
Suboxone
A
- Buprenorphine + Naloxone
- Comes in film versions too, some for pain therapy
- Can be given every 6-8 hours instead of once daily
- Analgesic effect wears off faster
26
Q
Tramadol
A
- Ultram
- 30% affinity for mu receptors but also blocks 5HT and NE reuptake
- Partially reversed by naloxone
- Can cause seizures and increase seizure risk
- Possible serotonin syndrome risk as well
27
Q
Ultracet
A
- Tramadol + APAP
- Hepatotoxicity blcok box warning, monitor APAP intake
- Converted to active metabolism by CYP2D6, avoid tramadol use in kids
28
Q
Tapentadol
A
- Nucynta
- Oral analgesic for moderate to moderately severe pain
- For neuropathic pain
- Mu opioid agonist and inhibition of NE reuptake
- CII
- Warnings about serotonin risk and risk for seizures
29
Q
Dextromethorphan
A
- OTC cough suppressant that is considered safe at therapeutic doses
- D-isomer of opiate agonist levorphanol
- No analgesic or addictive effects
- Doses 5-10 times the normal produce euphoria possible, PCP like effect?
30
Q
Diphenoxylate
A
- Lomotil
- For antidiarrhea effects
- CV
- Diphenoxylate has abuse potential so it is combined with atropine to make lomotil
- Atropine produces undesirable anticholinergic effects when taken more than therapeutic dose
31
Q
Loperamide
A
- Imodium
- OTC for diarrhea
- As effective as diphenoxylate
- Poorly absorbed after oral administration
- Acts directly on intestinal musculature to inhibit motility
32
Q
Analgesia in Pregnant/Lactation
A
Pregnancy
- Use APAP
- Avoid NSAIDs, codeine, hydrocodone, and tramadol
Lactation
- Use smallest doses for shortest durations
- Ibuprofen is NSAID of choice for breastfeeding mothers
33
Q
Opioid Overdose
A
-Triad of symptoms
1. Depressed respiration
2. Pinpoint pupils, hypoxia may cause pupils to dilate however
3, Coma - additive or synergistic effects to produce CNS and/or respiratory depression
-Treat by restoring respiration by administering naloxone
34
Q
Naloxone
A
- Evzio (injection), Narcan (nasal spray)
- May precipitate an opioid withdrawal syndrome
- Watch patient, usually only lasts 1-1.5 hours, could start another overdose after that time
- Usually patients recover enough to survive
35
Q
Pure Competitive Opioid Antagonists
A
- Naloxone, nalmefene, and naltrexone (ordered by increases in half life and duration)
- At all opioid receptors with no opioid agonist activity
- No effect when used without narcotics
- Can enhance pain in those with pain
- Withdrawal includes rhinorrhea, yawning, chills, piloerection, hyperventilation, muscular aches, vomiting, diarrhea
- Naltrexone used for treatment of opioid and alcohol dependence while others are used for suspected/known overdoses
36
Q
Naltrexone
A
- Vivitrol (ER injectable suspension)
- Oral, high dropout rates
- Long acting opioid receptor antagonist
- Overcomes problems of agonists like social resistance and no diversion of maintenance drug
- Treats alcohol and opioid dependence
- May be vulnerable to precipitation of withdrawal symptoms if transitioning from methadone or buprenorphine
