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Found. Pharm > Narcotic Analgesics > Flashcards

Narcotic Analgesics Flashcards

1
Q

Tolerance

A

Requiring higher doses to achieve the same effects of opioid
- Constipation is an exception

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2
Q

Stupor

A

Reduced consciousness
- Do not use heavy machinery

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3
Q

Classification

A

Chemical: Opioids and Opiates
Pharmacological: Narcotic Agonists
- Full or partial agonists of multiple specific opioid receptors
Therapeutic: Narcotic Analgesics for severe pain when NSAIDs are ineffective

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4
Q

Chemical Nomenclature: Opioids or Opiates

A

Opiates: Naturally occurring compounds in the botanical opium poppy (morphine, and codeine)
Opioids: Synthetic or semi-synthetic compound that are structurally similar to morphine
- bind to opiate receptors in the bind and mimic morphine
- Synthetic: Meperidine, fentanyl, methadone, tramadol, tapentadol
- Semi-synthetic: Hydrocodone, benzhydrocodone, oxycodone, heroin, hydromophone, oxymorphone, buprenorphine
Opioids is used to refer to ALL narcotic analgesics

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5
Q

Chemical Nomenclature

A
  • Phenanthrene: Morphine, Codeine, Heroin, Hydromorphone, Hydocodone
  • Phenylpiperidines: Oxycodone, Oxymorphone, Levorphanol, Naloxone, Buprenorphine
  • Diphenylheptanes: Methadone
  • Benzomorphans: Diphenoxylate, Loperamide, Pentazocine
  • Synthetic Opioid like Compounds: ADOL drugs: Tramadol and Tapentadol
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6
Q

Pharmacological Effects of Opioids

A
  • Analgesia: Pain relief&raquo_space; NSAIDs; no cardio protective, anti-inflammatory or antipyretic effect
  • Euphoria/Dysphoria: Happy/high feeling Vs dissatisfaction
  • Respiratory Depression: Most dangerous side effect
  • Physical Dependence: Major component of opioid addiction
  • Sedation: Side effects due to CNS depression
  • Miosis: Pupillary constriction, autonomic nervous system
  • Reduction of GI motility: Related to side effect of constipation
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7
Q

Pharmacological: Relative Strengths

A

Strong Agonists: AlfenTANYL, Heroin, Morphine, LevorPHANOL, SufenTANIL
Moderate/Low Agonists: Codeine, OxyCODONE, HydroCODONE, BenzhydroCODONE
Mixed Agonists/Antagonisits: Buprenorphine, Butorphanol, Pentazocine
Antagonists: Naloxone, Naloxegol, Naltrexone, Methylnaltrexone
Other Analgesics: Tramadol/Tapentadol

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8
Q

Therapeutic Nomenclature

A

Used for variety of indications
- Acute pain: using immediate release (IR)
- Non-Cancer chronic pain: when non responsive to alternative agents such as NSAIDs
- Chronic cancer pain: When alternative agents are insufficient, Preference toward extended release (ER) formulation
- Neuropathic pain: when non responsive to agents used for neuropathic pain (anti epileptic or antidepressant agents)

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9
Q

Therapeutic Applications

A

Anesthesia
- Adjunct to general anesthetics
- Morphine or fentanyl
Palliative sedation
- End of life sedation (focuses on relief of pain, anxiety and depression but is not curative)

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10
Q

Therapeutic Applications II

A

Antidiarrheals: Slows down GI motility and Use of opioid side effect for treatment of severe non infectious diarrhea
- Deodorized Tincture of Opium “Opium Tincture”*
– High alcoholic content of liquid form of drug
– CII used for non-infectious diarrhea
- Loperamide Hydrochloride (Imodium A-D) available OTC
– Potential abuse: euphoric effect in high doses
– Cardiac arrhythmias with excessive doses
Anti-tussives: Suppression of the cough reflex in brain
- Codeine: CII unless combined with acetaminophen; most effective
- Hydrpcpdpne bitrate: CII
- Dextromethorphen: mostly OTC - non controlled but has abuse potential

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11
Q

Dosage Guidelines

A
  • Opioids doses vary widely from one patient and one compound to another
  • Start with lowest available strength of an immediate release opioid and titrate dose upward for effect
  • Consideration:
    – Patient Factors (age/weight, pain, tolerances, illness)
    – Immediate Vs controlled release dosage
    – Route of administration (PO, IV, IM, transdermal and transmucosal)
    – Properties of specific drug (potency and average dose)
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12
Q

Dose Equivalent

A

Morphine: PO/IV/IM
Codeine: considered weak opioid
- Limited use alone due to ADE
Hydrocodone: similar potency to morphine
Hydromorphone: more potent than morphine
- 1mg = 5mg morphine
Oxycodone: more potent than morphine
Fentanyl: MOST potent and short acting
Methadone: More potent than morphine
- Used for OUD/Pain management
Meperidine: Less potent than morphine
- Quick onset of action

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13
Q

Abuse Deterrent Formulation

A
  • Alone or in combination with naloxone/naltrexone
  • Purpose: prevent abuse of opioid when crushed or injected
  • No generic available
  • Utilizes one or more mechanism to make their intentional recreational use more difficult
  • Mechanisms: Resist crushing, Resist dissolving, Release opioid antagonist
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14
Q

Short vs long-acting dosage

A

Immediate release dosage forms
- Preferred use to prevent pain tolerance
- Q4-6H PRN breakthrough pain
Long acting dosage forms
- To maintain pain relief throughout the day
Transdermal dosage forms
- considered a controlled release formulation
- Not for sever ACUTE pain
Transmucosal dosage forms
- Sublingual or buccal
– SL: under tongue absorbed directly by bloodstream bypassing liver for faster absorption
– Buccal: Absorbed through cheek; fast acting for chronic or breakthrough pain

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15
Q

Black Box Warning of Opioids

A
  • Hypoventilation
  • Extended release formulation
  • Not for children
  • Abuse & addiction potential
  • Avoid splitting of LA/ER/transdermal
  • Routes of administration
  • Abrupt treatment effects
  • Chronic use in pregnancy
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16
Q

Contraindication

A
  • Patients with significant respiratory depression
  • Patients with bronchial asthma
  • Patients with convulsive disorders
  • Addiction prone patients
  • Treatment of diarrhea
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17
Q

Warning and Precautions

A
  • Adverse dug reaction are DOSE dependent and specific to individual compounds
  • Pregnancy category C: Due to withdrawal syndrome in neonates (NAS: Neonatal abstinence syndrome) and evidence of birth defects in animal trials
    – If not essential => not recommended
    Somnolence
  • Recommendation of avoid driving or use of heavy machinery when initiated
18
Q

FDA and Storage Requirements

A

FDA on LA/ ER Formulations
- Company required to have post-marketing surveillance on LA/ER formulation
- Only for sever pain
- Mandate to warn patient of greater risk for addiction
Storage Requirements
- Stored within a secured cabinet or safe within the department
- C-III-C-V dispersed throughout non controlled substances o the shelf

19
Q

Drug-Drug Interaction

A
  • Avoid combination with opioids that can increase respiratory depression (alcohol, benzodiazepines, MAOls)
  • Medication that are enzyme inducers or inhibitors cause potential DDI since metabolized by liver enzymes (hydrocodone, codeine, tramadol, fentayl)
  • Specific enzyme inhibitors that can cause DDI with opioids (antibiotics: Clarithromycn, ketoconazole, CCB: Diltiazem and varapemil, Linezolid)
20
Q

Narcotic Antagonists - NAL

A

Naloxone HCI (Narcan): IV, IM, IN (Not PO)
- Reverses effect of severe opioid toxicity
- Should be made available for patients at risk of overdose
- Short half life so repetitive doses may be required (especially with LA/ER opioids)
- New Jersey overdose prevention act of 2013 (requires a prescription but may be dispense without one if standing order/collaborative practice exist)
Naltrexone: Systemically active with oral administration
- Not effective for overdose
- Treatment of alcohol withdraw and opioid use disorder as maintenance
Naloxegol (Movantik) 12.5 or 25 mg tablets
- Opioid induced constipation (OIC) for patients with chronic non cancer pain
- Chemically released to naltrexone but without crossing the blood brain barrier

21
Q

Narcotic Antagonists - NAL II

A

Methylnaltrexone (Registro)
- Subcutaneous
- OIC: quick onset of action with bowl movement within 30 min
Alvimopan (Entereg)
- 12mg for post operative ileus (intestinal obstruction due to loss of peristalsis)
Naldemedine (Symproic):PO
- OIC once daily dose
Nalmefene - IV, IM, SubQ
- Longer duration of action and higher affinity for opioid receptor than naloxone

22
Q

Morphine Sulfate (Narcotic Agonists)

A
  • PO various strengths, IR and ER) 10-200 mg, suppositories, IM, IV, subcutaneous, epidural injection
  • Abuse deterrent formulations:
    – Arymo
    – Embeda
    – Kadian
23
Q

Codeine Sulfate - C-11 (Narcotic Agonists)

A
  • IV available but commonly used as oral
  • Weak opioid, commonly used in combination with acetaminophen or NSAIDs
24
Q

Hydromorphone - Dilaudid (Narcotic Agonists)

A
  • PO, IV, IM, Subcutaneous, Suppositories
  • Frequently used IV/IM in hospital setting
25
Q

Fentanyl and Fentanyl Citrate (Narcotic Agonists)

A
  • IV, IM, transdermal, transmucosal (buccal and sublingual), Intranasal
  • Heroin frequently laced with fentanyl and difficult to reverse with opioid antagonists
  • Not available/effective OP
  • Citrate=injection:IV, IM, Subcutaneous (Adjunct to regional anesthesia or pain management in critical care patients
    ActiQ - Lozenge on a stick for sever breakthrough pain
    Fentora - Transmucosal
    Abstral - Transmucosal
    Lazanda - Nasal spray
    Duragesic - transdermal patch
  • Lasting 72H (change every 3 days)
  • Precautions (avoid wounded skin, no heat (increase absorption), do not cut into smaller pieces, Fold patch and flush down toilet)
  • Transitioning from PI to transdermal patch: may take 12-24 hours for onset of patch effect
26
Q

Hydrocodone - bitartrate (Narcotic Agonists)

A
  • PO only; C-II
  • Vicodin and Vicodin HP (high potency)
  • Hysingla ER tablets: once daily; abuse deterrent formulation
27
Q

Oxycodone HCL (Oxycontin CR tabs) (Narcotic Agonists)

A
  • C-II only reformulated, hard to crush
  • Oxycontin ER capsules - abuse deterrent formulations
  • Xyampza ER capsules
  • Percocet tablets (with acetaminophen)
    – CII
28
Q

(Narcotic Agonists)

A
  • Alfentanil (alfenta) injection - IV only
  • Lecorphanol Tartrate (Levo-Dromoran)
    – PO, IV, IM
    – Adjunct to anesthesia preoperatively
  • Remifentanil HCI (Ultiva): IV, Adjunct to anesthesia
  • Sufentail Citrate: IV, Adjunct to anesthesia
  • Tapentadol HCI (Nucynta) PO: C-II similar to tramadol but more potent
  • Pentazocine (Talwin):C-IV
29
Q

Meperidine HCI - Demerol (Narcotic Agonists)

A
  • PO, IV
  • Similar to hydromorphone
  • C-II; less favored due to side effect of nausea
30
Q

Tramadol HCI - Ultram (ER), Ryzolt (ER) - (Narcotic Agonists)

A
  • Dual analgesic narcoticL opioid agonist and inhibits reuptake of norepinephrine and serotonin responsible for pain pathway
  • Opioid effect intended for short term
  • Used for moderate/severe pain; weaker than opioid agonist but stronger than NSAID
  • Less sedation/constipation
31
Q

Methadone- Dolophine (Narcotic Agonists)

A
  • Commonly used as oral form for maintenance treatment of opioid use disorder, addiction and pain
    –Dosed 60-120 mg PO daily
    – Suspension&raquo_space;> tablet/wafers
    – Closest monitored for two weeks
  • Prescribed for moderate to sever pain (lower cost)
    – Should be reseed for treating terminal cancer pain
32
Q

Narcotic Partial Agonists

A

Buprenorphine HCL (CIII) - Subutex
- Tablets (2 or 8mg), IV/IM, Transdermal
- Semi-synthetic; alternative option for OUD to methadone
- Less respiratory depression
Buprenorphine/Naloxone
- Sublingual: Zubsolv; Buccal film: Bunavail; SL film
- Combination with naloxone to prevent abuse potential - Naloxone PO is inactive

33
Q

Combination Products

A
  • Opioid + ASA + Acetaminophen + NSAID
  • Acetaminophen –Tylenol with codeine (CIII), Vicodin, Percocet (CII), Ultracet (CIV)
  • ASA (empirin, percodan)
  • Ibuprofen (Combunox)
  • B&O supprettes: Belladone & Opium suppositories
34
Q

Legal and Regulatory: Monitoring

A
  • Prescription Drug Monitoring Program (PDMPs)
  • Risk Evaluation and Mitigation Strategy (REMS)
  • DEA (Drug Enforcement Agency) Status
35
Q

PDMPs

A
  • Tracks every CDS prescription dispensed by any outpatient pharmacy
  • Patient name/address, prescriber identity, and pharmacy data available to health care provider and law enforcement personnel
  • Required programs exist in all states
  • New Jersey-PDMP: state wise database for monitoring CDS (C-II to C-V)
  • Pharmacies Required to report to New Jersey-PDMP at least Biweekly
36
Q

REMS

A
  • Available for many high risk meedication
  • REMS for Opioids
    – Morphine, hydromorphone, methadone, oxycodone, oxymorphone, transdermal fentanyl, and byprenorphine; immediate release transmucosal fentanyl products
    – Focus mostly on long acting or extended release (LA or ER) opioids due to propensity for addiction
    – Educational resources for perscribers
    – Medication guides
37
Q

DEA

A
  • Responsible in overseeing all CDS
  • Responsible for enforcing the controlled substances law and regulation in US
  • Review of controlled substance schedule: CI, CII, CII, CIV, CV
    – CI = no legitimate therapeutic use; illegal to prescribe and abuse
38
Q

Practical Consideration(CII

A
  • Prescription: Must include DEA + NPI number of prescriber in New Jersey - Serial number of blank - Limited to one CDS per script
  • Telephone/Electronic Scripts: Telephone orders not allowed for CIIs, E-Scribing is permitted
  • Post-Dated CIIs: Commonly occurs for CII that require > 30 day supply
  • Limits: 30 day limit form date of issue for RX to be valid (quant limits: NJ = QID for 30 days (120 units)
  • Refills: C-II CANNOT be refilled regardless - C-III to C-V: 5 refills within 6 month from date of issue
  • Partial Filling: DEA allow partial of C-II filing but remainder of RX MUST be filled within 72 hours
39
Q

Red & Green flags

A

Red Flags: Specialty doctor, Cash paying, Direction incorrect, Doctor shopping, Pharmacy shopping, Traveling far for RX
Green Flags: Physician/Patient know to pharmacy, Known chronic pain/terminal illness, Pain Management prescriber

40
Q

Prescription Requirement

A

Perception Requirement:
- Date of Issue
- Patient name/address
- MD name/address and DEA number (a MUST)
- Drug name, strength, and dosage form,
- Quantity prescribed
- Direction
- Number of refiles
- Signature of prescriber

41
Q

Labeling Requirement

A
  • Name/adress of pharmacy
  • Serial number of Rx
  • Date of fill / Date of issue
  • Patient name
  • MD name
  • Direction of use
  • Refill information
  • Cautionary label (PRN)
  • Caution Label

Found. Pharm (14 decks)

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