Pain Flashcards
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Nociceptive pain:
results from tissue injury
Neuropathic pain:
Does not result from tissue injury or damage
ex. fibromyalgia, diabetic neuropathy, chronic headaches, drug toxicities
Acute pain:
- Begins suddenly, feels sharp
- Do not prescribe ER/LA opioids for acute pain
Chronic pain:
- pain that persists beyond normal healing time
- cancer pain and non-cancer pain
Non-opioid analgesics:
- acetaminophen
- NSAIDs (selective & non-selective)
- salicylates
acetaminophen
- reduces pain (analgesia) and fever (antipyretic) but DOES NOT provide anti-inflammatory effects
- Does not inhibit thromboxane (no effect on platelets)
- Avoid APAP abbreviation!
combination products with acetaminophen include:
acetaminophen
- hydrocodone (Norco, Vicodin, Lortab, Lorcet*)
- oxycodone (Percocet, Endocet, Primlev)
- codeine: (Tylenol #2, 3, 4)
- tramadol (Ultracet)
- butalbital/caffeine (Fioricet)
- diphenhydramine (Tylenol PM)
- caffeine (Excedrin)
- caffeine + aspirin (Excedrin Extra Strength)
- caffeine + pyrilamine (Midol Complete)
- and in multiple cough & cold products and OTC combinations
FeverAll
acetaminophen suppositories 120mg
Ofirmev
acetaminophen IV for injection
concentration is 10mg/mL (in 100mL vials; caution with dosing
All IV acetaminophen doses should be prepared in the pharmacy.
$$$
pediatric dose (< 12 years old):
10-15mg/kg every 4-6 hours
Max: 5 doses/day
acetaminophen
Infant/Children’s suspension:
160mg/5mL
acetaminophen overdose:
(NTE) Not to exceed: 4000mg/day and 325mg/prescription dosing unit.
Overdoses can be accidental.
Antidote:
(NAC) N-acetylcysteine, oral or Acetadote IV
- NAC serves as a glutathione substrate
- it restores intracellular glutathione
- so acetaminophen can get metabolized to non-toxic metabolites
- available in both oral and IV formulations
- The Rumack-Matthew nomogram uses the serum acetaminophen level and time since ingestion to determine whether hepatotoxicity is likely
Mucomyst
oral acetylcysteine
Cetylev
acetylcysteine
Acetaminophen Drug interactions:
can be used with warfarin, but if used chronically (doses > 2grams/day), acetaminophen can increase the INR. Monitor accordingly.
NON - Steroidal Anti-inflammatory Drugs:
(COX)- cyclooxygenase selectivity
- COX enzymes catalyze conversion of arachidonic acid to prostaglandins and thromboxane A2
- COX-2 selective agents only block synthesis of COX-2
. Decreases GI risk (COX-1 is GI protective)
Non-aspirin boxed warnings (MedGuide)
- GI risk (GI bleeding and ulceration)
- CV risk (can increase risk for MI or stroke)
- CABG surgery
Non-selective NSAIDs: COX-1 & COX-2:
- ibuprofen
- aspirin
COX-2 selective NSAIDs:
- only block COX-2, which preserves COX-1, which is good since it is GI protective. So, using a COX-2 agent, decreases GI risk.
- celecoxib
Blocking COX-1 decreases the formation of (TxA2) thromboxane A2, which is required for both platelet activation and aggravation.
All prescription non-aspirin NSAIDs require a ________
MedGuide, due to the risks.
Non-aspirin Boxed Warnings:
GI risk-
NSAIDs can increase the risk of serious GI adverse events, including bleeding and ulceration.
Patients who are elderly, have a history of GI bleed or are taking systemic steroids, SSRIs or SNRIs are at the greatest risk.
Aspirin does not carry a boxed warning but still has this risk
Non-aspirin Boxed Warnings:
CV-
NSAIDs can increase the risk of MI and stroke.
Avoid use in patients with CV disease or risk factors.
Non-aspirin Boxed Warnings:
(CABG) Coronary Artery Bypass Graft Surgery-
NSAID use is Contraindicated after CABG surgery.
Antiplatelet therapy (commonly aspirin) is recommended after CABG surgery.
Side effects of ALL NSAIDs:
- decreased renal clearance
- increase blood pressure
-premature closure of the (PDA) ductus arteriosus - nausea (take with food)
- photosensitivity
Before Birth:
The ductus arteriosus (DA) connects the pulmonary artery to the aorta, allowing oxygenated blood to flow to the baby, bypassing the immature lungs.
DO NOT USE NSAIDs in the 3rd trimester (> or = to 30 weeks) of pregnancy. NSAIDs can prematurely close the DA.
After Birth:
The (DA) ductus arteriosus should close on its own. In some cases, it remains patent (open) and NSAIDs can be used to help it close.
IV NSAIDs (indomethacin, ibuprofen) can be used within 14 days of birth to close a patent ductus arteriosus (PDA)
Side effects of ALL NSAIDs:
- can decrease renal clearance by reducing blood flow to the glomerulus; additional nephrotoxic agents or dehydration increases the risk
ALL NSAIDs should be used cautiously (or avoided) in renal failure.
Side effects of ALL NSAIDs:
- can increase blood pressure. Use cautiously in patients with controlled hypertension and AVOID in patients with uncontrolled hypertension.
Side effects of ALL NSAIDs:
- can cause closure of the ductus arteriosus, which can lead to heart failure in the baby.
DO NOT USE NSAIDs in the 3rd trimester of pregnancy (> or = to 30 weeks).
Side effects of ALL NSAIDs:
- can cause photosensitivity.
SPF of at least 30
COX-1 & COX-2 Non-selective NSAIDs:
ibuprofen (Advil, Caldolor, Motrin)
indomethacin (Indocin)
naproxen (Aleve)
ketorolac (Toradol)
piroxicam (Feldene)
suldinac
increased COX-2 selectivity:
remember - lower risk of GI complications
celecoxib (Celebrex)
diclofenac (Voltaren)
meloxicam (Mobic)
etodolac
nabumetone
Salicylate NSAIDs:
Caldolor
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
ibuprofen
class: non-selective NSAID
Indications:
MOA:
Dosage forms:
Dosing:
Adults
OTC: 200-400mg every 4-6 hours
RX: 400-800mg every 6-8 hours
MAX: 3.2 grams /day
Pediatrics
5-10mg/kg/dose every 6-8 hours**
(as an antipyretic)
MAX: 40mg/kg/day
Contraindications:
Warnings:
Side Effects:
dyspepsia, abdominal pain, nausea
Monitoring:
Pearls/Notes:
Caldolor is the IV formulation of ibuprofen.
**NeoProfen injection is indicated for closure of PDA in premature infants.
OTC: limit self-treatment to < 10 days
Severe skin reactions, including SJS/TEN
Drug-Drug/Food interactions:
Advil
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
ibuprofen
Motrin IB
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
ibuprofen
Indocin
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
indomethacin
class: Non-selective NSAID
Indications:
- first NSAID approved for Gout
- IV formulation for PDA closure
MOA:
Dosage forms: capsule, oral suspension, suppository, injection
Dosing:
IR: 20-50mg BID-TID
CR: 75mg daily-BID
Tivorbex: 20mgTID or 40mg BID-TID
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
** High risk for CNS side effects (Avoid in psych conditions)
* The IR formulation is an older NSAID approved for Gout*
IV injection of Indomethacin, is indicated for closure of PDA in premature infants
Drug-Drug/Food interactions:
Tivorbex
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
indomethacin
class: Non-selective NSAID
Indications:
- first NSAID approved for Gout
- IV formulation for PDA closure
MOA:
Dosage forms: capsule, oral suspension, suppository, injection
Dosing:
Tivorbex: 20mgTID or 40mg BID-TID
- Tivorbex is micronized for faster dissolution*
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
** High risk for CNS side effects (Avoid in psych conditions)
* The IR formulation is an older NSAID approved for Gout*
Drug-Drug/Food interactions:
Aleve
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
naproxen
class: Non-selective NSAID
Indications: pain, fever
MOA:
Dosage forms:
Dosing:
OTC (pain, fever):200mg every 8-12 hours (1st dose can take 2 tabs)
Max: 3 tabs in 24 hours
RX: (inflammation, mild-mod pain): 500mg every 12 hours (or 250mg Q 6-8 hours)
Max: 1000mg/day (1250mg day 1)
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
- prescribers and patients sometimes prefer naproxen since it can be taken BID**
Drug-Drug/Food interactions:
Naproxen base 200mg = Naproxen Na 220mg
Naprelan
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
naproxen
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Naprosyn
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
naproxen
Vimovo
naproxen + esomeprazole
PPI in Vimovo is used to protect the GI tract.
Treximet
naproxen + sumatriptan
injection for migraines
Toradol
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
ketorolac
class: Non-selective NSAID
Indications:
- indicated as a continuation of IV or IM ketorolac
MOA:
Dosage forms: tablet, injection, nasal spray, ophthalmic
Dosing:
Oral: 10-20mg for first dose, then 10mg Q4-6 hours PRN
Max: 40mg/daily
IV: (> or = 50kg) 30mg for first dose or 30mg every 6 hours. (*decrease dose if 65 years old or older)
IM: (> or = 50mg) 60mg x 1 dose or 30mg every 6 hours (*decrease dose if 65 years or older)
**Boxed Warning:
- Oral ketorolac: for short-term moderate to severe acute pain only as continuation of IV or IM ketorolac (max combined duration IV/IM and PO/nasal is 5 days in adults);
- Not for intrathecal or epidural use
- Avoid in patients with advanced renal disease or at risk of renal impairment due to volume depletion
-Avoid use in labor and delivery and use aspirin or NSAIDs
- dose adjustment needed in 65 years old and greater or less than < 50kg
Contraindications:
Warnings:
increased bleeding, acute renal failure, liver failure and anaphylactic shock
Side Effects:
headache, injection site pain (often given IM)
Monitoring:
Pearls/Notes:
- Usually used after surgery, never before
-
Drug-Drug/Food interactions:
Acular
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
ketorolac ophthalmic
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Sprix
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
ketorolac nasal spray
class:
Indications:
MOA:
Dosage forms:
Dosing:
If less than 65 AND (> or = to 50kg): 1 spray in each nostril every 6-8 hours.
If 65 or older OR less than < 50kg: 1 spray in one nostril every 6-8 hours.
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
- nasal spray: prime 5 times before use. No additional priming is needed if additional doses are used. Discard 24 hours after opening.
Drug-Drug/Food interactions:
Feldene
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
piroxicam
class:
Indications:
MOA:
Dosage forms:
Dosing:
10-20mg daily
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
sulindac
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
class:
Indications:
MOA:
Dosage forms:
Dosing:
150-200mg BID
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Celebrex
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
celecoxib
class: COX-2 selective NSAID
Indications: OA osteoarthritis, RA- rheumatoid arthritis, acute pain, primary dysmenorrhea, ankylosing spondylitis
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Sulfa/Sulfonamide allergy
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
- Highest COX-2 selectivity
- Lower risk for GI complications (but still present)
- same risk for renal complications
- **Increases risk of MI/stroke (Avoid with CV risk and avoid higher doses/long duration in these patients.
- Avoid in pregnancy; risk greatest at > or = to 30 weeks gestation.
Drug-Drug/Food interactions:
Consensi
celecoxib + amlodipine
Indications:
Seglentis
celecoxib + tramadol
Indications:
Voltaren
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
diclofenac
class: COX-2 selective NSAID
Indications:
MOA:
Dosage forms:
Dosing:
oral tablet: 50-75mg BID-TID
gel- 2-4 grams to affected joint 4 times per day. (total body max 32 grams/day)
Boxed Warnings:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
- has some COX-2 selectivity.
- oral diclofenac formulations are not bioequivalent, even if same mg strength.
- gel comes with a dosing card (4.5inches = 4 grams)
Drug-Drug/Food interactions:
Cambia (diclofenac)
Flector-
Pennsaid-
Xyrlix-
Zipsor-
Zorvolex-
Cambia- powder for oral solution
- powder dissolve in water for migraines
Flector- transdermal patch
- applied to the painful area BID
- remove before an MRI
Xyrlix- topical solution
-
Zipsor- liquid filled capsules.
-
Zorvolex- capsules
-
Arthrotec
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
diclofenac + misoprostol
class:
Indications:
MOA:
Dosage forms:
Dosing:
Boxed Warnings:
avoid in females of child-bearing potential unless the female is capable of complying with effective contraceptive measures.
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
- misoprostol is used to replace the gut protective prostaglandins to decrease GI risk; can increase uterine contractions (which can terminate pregnancy) and causes cramping and diarrhea.
Drug-Drug/Food interactions:
Mobic
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
meloxicam
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Vivlodex
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
meloxicam
etodolac
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Relafen
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
nabumetone
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Salicylate NSAIDs
- aspirin
Boxed Warnings:
- NSAID hypersensitivity (nasal polyps)
- Risk of Reye’s syndrome
- Severe Skin reactions
aspirin is acetylsalicylic acid, so it causes nausea.
- buffered or coated aspirin reduces nausea
- this does not reduce risk of GI bleeds
- GI toxicity is dose-related and is low risk at cardioprotective doses
If using aspirin with ibuprofen, take aspirin 1 hour before or 8 hours after ibuprofen.
Aspirin is _________
acetylsalicylic acid
The aspirin buffered and EC (enteric-coated products DO NOT reduce the risk of __________. These products only provide additional benefit in reducing the risk of ________.
GI bleeds
nausea
Ecotrin
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
aspirin
class: Salicylate NSAID
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
** Avoid aspirin in children and teenagers with any viral infection due to potential risk of Reye’s syndrome (symptoms include somnolence, N/V, lethargy, confusion); other NSAIDs can be used in pediatrics**
Severe skin rash (rare) including SJS, TEN
Avoid in the third trimester of pregnancy due to fetal harm.
Side Effects:
*Dyspepsia, heartburn, bleeding, nausea
Monitoring:
Pearls/Notes:
* to decrease nausea, use EC or buffered product or take with food
*PPIs may be used to protect the gut with chronic NSAID use; consider the risks from chronic PPI use (decrease in bone density, increase in infection risk)
** Do NOT Use Durlaza or Yosprala when immediate effect is needed (e.g. myocardial infarction)
salicylate overdose can cause tinnitus
- methyl salicylate is a popular OTC topical found in BenGay, IcyHot, Thera-Gesic, Salonpas;
- aspirin has risk of gastritis/ulceration; the benefit of chronic (daily) use must outweigh the risk of GI bleeding.
Drug-Drug/Food interactions:
- additive bleeding risk with other agents that can increase bleeding risk, such as steroids.
- caution using aspirin with other Ototoxic agents (e.g. aminoglycosides, IV loop diuretics)
- Multiple NSAIDs should not be used together, except the addition of low dose aspirin for cardio protection when indicated. *If using aspirin for cardio protection and ibuprofen for pain, take aspirin one hour before or eight hours after ibuprofen.
-NSAIDs can increase level of lithium and methotrexate
Durlaza
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
aspirin ER capsule
class: Salicylate NSAID
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
** Avoid aspirin in children and teenagers with any viral infection due to potential risk of Reye’s syndrome (symptoms include somnolence, N/V, lethargy, confusion); other NSAIDs can be used in pediatrics**
Severe skin rash (rare) including SJS, TEN
Avoid in the third trimester of pregnancy due to fetal harm.
Side Effects:
*Dyspepsia, heartburn, bleeding, nausea
Monitoring:
Pearls/Notes:
* to decrease nausea, use EC or buffered product or take with food
*PPIs may be used to protect the gut with chronic NSAID use; consider the risks from chronic PPI use (decrease in bone density, increase in infection risk)
** Do NOT Use Durlaza or Yosprala when immediate effect is needed (e.g. myocardial infarction)
salicylate overdose can cause tinnitus
- methyl salicylate is a popular OTC topical found in BenGay, IcyHot, Thera-Gesic, Salonpas;
- aspirin has risk of gastritis/ulceration; the benefit of chronic (daily) use must outweigh the risk of GI bleeding.
Drug-Drug/Food interactions:
- additive bleeding risk with other agents that can increase bleeding risk, such as steroids.
- caution using aspirin with other Ototoxic agents (e.g. aminoglycosides, IV loop diuretics)
- Multiple NSAIDs should not be used together, except the addition of low dose aspirin for cardio protection when indicated. *If using aspirin for cardio protection and ibuprofen for pain, take aspirin one hour before or eight hours after ibuprofen.
-NSAIDs can increase level of lithium and methotrexate
Bufferin
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
aspirin
class: Salicylate NSAID
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
** Avoid aspirin in children and teenagers with any viral infection due to potential risk of Reye’s syndrome (symptoms include somnolence, N/V, lethargy, confusion); other NSAIDs can be used in pediatrics**
Severe skin rash (rare) including SJS, TEN
Avoid in the third trimester of pregnancy due to fetal harm.
Side Effects:
*Dyspepsia, heartburn, bleeding, nausea
Monitoring:
Pearls/Notes:
* to decrease nausea, use EC or buffered product or take with food
*PPIs may be used to protect the gut with chronic NSAID use; consider the risks from chronic PPI use (decrease in bone density, increase in infection risk)
** Do NOT Use Durlaza or Yosprala when immediate effect is needed (e.g. myocardial infarction)
salicylate overdose can cause tinnitus
- methyl salicylate is a popular OTC topical found in BenGay, IcyHot, Thera-Gesic, Salonpas;
- aspirin has risk of gastritis/ulceration; the benefit of chronic (daily) use must outweigh the risk of GI bleeding.
Drug-Drug/Food interactions:
- additive bleeding risk with other agents that can increase bleeding risk, such as steroids.
- caution using aspirin with other Ototoxic agents (e.g. aminoglycosides, IV loop diuretics)
- Multiple NSAIDs should not be used together, except the addition of low dose aspirin for cardio protection when indicated. *If using aspirin for cardio protection and ibuprofen for pain, take aspirin one hour before or eight hours after ibuprofen.
-NSAIDs can increase level of lithium and methotrexate
Non-acetylated Salicylates:
Salsalate
*Magnesium salicylate (Doan’s Extra Strength)
Choline Magnesium Trisalicylate
Diflunisal
Salicylate salts
Opioid analgesics:
-
-
mu
kappa
delta
Opioid analgesics:
Opioids are __________ in the CNS, which primarily produce __________ but can also cause euphoria and respiratory depression.
mu receptor agonists
pain relief
Opioid analgesics:
Opioids in combination (such as with acetaminophen) are used for moderate pain, and single opioid agents are used for severe pain.
Opioid analgesics:
Codeine, fentanyl, hydrocodone, hydromorphone, methadone, morphine, oxycodone and oxymorphone are classified as full receptor agonists.
Full agonists are used for acute and chronic pain and have no ceiling effect - the dose can go up. Opioids at high doses should be rotated with other opioids to reduce tolerance.
Opioid analgesics:
Morphine is a full agonist.
Buprenorphine is a partial agonist.
Naloxone is an antagonist.
Opioid analgesics:
Opioid Boxed Warnings:
- addiction, abuse and misuse can lead to overdose and death
- respiratory depression, which can be fatal
- use of any opioid with benzodiazepines or other CNS depressants including alcohol, can increase the risk of death
- Kadian, Embeda, Zohydro and Nucynta ER; DO NOT CONSUME alcohol with this medication, can cause potentially fatal overdose.
- accidental ingestion/exposure of even one dose in children can be fatal. Never give this medication to anyone else (includes patches).
- crushing, dissolving, or chewing of the long-acting products can cause delivery of a potentially fatal dose
- Life-threatening neonatal opioid withdrawal with prolonged use during pregnancy
Opioid analgesics:
Safety Concerns:
- approved Risk Evaluation and Mitigation Strategies (REMS)
- a REMS was approved for ER and LA opioid medications (including Nucynta ER)
Primary components of the REMS:
- education for the prescribers, and
- requirement that the prescribers counsel the patients
Physiological Adaptation (Physical Dependence)
- almost all patients using chronic opioids, including abusers, become physiologically adapted to the opioid, and experience physical withdrawal symptoms when the opioid is stopped, or a dose is late or missed.
- the symptoms include anxiety, tachycardia, shakiness, and shortness of breath. The withdrawal causes much suffering. Physiological adaptation is not addiction.
Addiction
a strong desire or compulsion to take the drug despite harm. Involves drug-seeking behavior, including exaggerating the pain or physical problems, getting prescriptions from multiple prescribers and/or prescription forgery.
Pseudo-Addiction
On occasion, a patient is seen at the pharmacy who appears anxious and states they ran out of medication or are afraid of running out too early. The person seems similar to an addict but is actually a legitimate pain patient with poorly controlled pain. The remedy is adequate analgesics, such as ER opioids for pain control.
Tolerance
A higher opioid dose is needed to produce the same level of analgesia that a lower dose previously provided. Tolerance develops overtime with chronic opioid use. It is important to distinguish whether the higher pain severity is due to a condition (e.g. cancer has spread), or a decrease in drug’s effectiveness due to tolerance, or both. If tolerance develops, it can be preferable to switch to another opioid rather than increase the dose.
Opioid Hyperalgesia
Present when the opioid dose is increased to treat the pain, but the pain becomes worse rather than better. This occurs occasionally. If suspected, a different class of analgesic or a switch to another opioid should be tried.
(BTP) Break Through Pain
Sharp spikes of severe pain that occur despite the use of an ER opioid.
Must be treated with a fast acting pain agent, such as an injection, transmucosal immediate-release fentanyl (TIRF) drugs (for cancer BTP only) or immediate release (IR) opioids (less expensive but not preferable). When multiple doses are required for BTP, a higher baseline dose can be required, or possibly a switch to a different opioid.
(OIRD) Opioid-Induced Respiratory Depression
The usual cause of fatality in opioid overdose. Hospitalized patients receiving IV opioids must be carefully monitored for sedation and oxygen saturation.
Centrally-Acting Opioid Antagonists
There are two drugs in this group; both block opioids from binding to the Mu receptor.
** Naloxone - is used to reverse respiratory depression
**Naltrexone - is most commonly used in combination with an opioid to block the use of other opioids that may be taken (inappropriately) at the same time.
For ALL Opioids (using morphine as the prototype):
Side Effects:
GI effects
- constipation, nausea, vomiting
- may require antiemetics, such as prochlorperazine or ondansetron
CNS effects
- sedation (somnolence), dizziness, changes in mood, confusion
Skin reactions
- flushing, pruritus, diaphoresis (may require an antihistamine)
Overdose: respiratory depression
Codeine C-II
in combinations with acetaminophen is a C-III
in combination with other antitussive products is a C-V
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
class: opioid
Indications:
MOA:
Dosage forms:
Dosing:
15 - 60mg every 4 hours as needed
Every 4-6 hours as needed, range 15-120mg codeine.
Max dose:
Boxed Warnings:
**Respiratory depression and death have occurred in children following tonsillectomy and/or adenoidectomy found to have evidence of being ultra-rapid metabolizers of codeine due to a CYP2D6 polymorphism; deaths have also occurred in nursing infants after being exposed to high concentrations of morphine because mothers were ultra-rapid metabolizers; use with CYP3A4 inducers/inhibitors of CYP2D6 should be carefully considered due to variable effects
Contraindications:
** Do NOT USE in children < 12 years (any indication) and < 18 years following tonsillectomy/adenoidectomy surgery; FDA recommends to avoid codeine-containing cough and cold products for children under 18 years of age
Warnings:
- adolescents between 12-18 years of age who are obese or have sleep apnea or severe lung disease are at increased risk of breathing problems
Side Effects:
Codeine has a high degree of GI side effects including constipation
Monitoring:
respiration rate
Pearls/Notes:
** Codeine-containing cough and cold preparations are no longer indicated in patients < 18 years of age- DO NOT USE
** Codeine, a prodrug, is metabolized to Morphine via CYP2D6
Drug-Drug/Food interactions:
Codeine-containing cough and cold preparations are no longer indicated in patients < 18 years of age - DO NOT USE
Codeine containing products:
codeine + chlorpheniramine /pseudoephedrine
codeine + promethazine
codeine + promethazine /phenylephrine
codeine + acetaminophen
Tylenol #2
Tylenol #3 = codeine 30mg + acetaminophen 300mg
Tylenol #4 = codeine 60mg + acetaminophen 300mg
Duragesic
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
fentanyl
class: opioid
Indications: chronic pain
MOA:
Dosage forms: patch (12, 25, 50, 75, 100mcg/hr)
Dosing:
Patch: apply 1 patch every 72 hours (can be every 48 hours)
Max dose:
Boxed Warnings:
Potential for medication errors when converting between dosage forms, use with strong or moderate CYP3A4 inhibitors can result in increased effects and potentially fatal respiratory depression, avoid exposing transdermal fentanyl to external heat.
Contraindications:
Warnings:
Side Effects:
Hyperhidrosis (excessive sweating), dry mouth, asthenia, loss of appetite, application site redness/erythema (patch)
Monitoring: respiration rate
Pearls/Notes:
*Analgesic effect can be seen 8-16 hrs after application; Do NOT stop other analgesics at first (decrease dose 50% for the first 12 hrs), discontinue all around the clock opioid drugs when the patch is applied
Outpatient use of fentanyl is for chronic pain management only
** Fentanyl is NOT used in opioid-naive patients; a patient who has been using equivalent to = Morphine 60mg/day for at least 7 days can be converted to a fentanyl patch**
-Apply patch to a hairless skin area (cut hair short if necessary)
- Do NOT apply > 1 patch each time
- Can be covered ONLY with a permitted adhesive film dressing Bioclusive or Tegaderm
- Do NOT cover with a heating pad or any other bandage
Dispose of patch in the toilet, some drug is still in the patch and can be lethal if obtained
*Keep away from children and pets
- Some patches need to be removed before MRI
Drug-Drug/Food interactions:
- Caution with other CNS depressants: additive somnolence, dizziness, confusion, increased risk of respiratory depression. These include alcohol, hypnotics, benzodiazepines and muscle relaxants. *Avoid Alcohol with ALL Opioids, especially ER formulations**.
- Increased risk of hypoxemia (low levels of oxygen in blood) with underlying respiratory disease (e.g. COPD) and sleep apnea.
- Fentanyl (is a CYP3A4 substrate), avoid use with CYP3A4 inhibitors, analgesic effect is decreased with CYP3A4 inducers.
Counseling points on Duragesic fentanyl patch:
-Apply patch to a hairless skin area (cut hair short if necessary), on a flat surface (chest, back, flank, upper arm) and change every 72 hours. Press in place an hold for 30 seconds.
- Do NOT apply > 1 patch each time
- Can be covered ONLY with a permitted adhesive film dressing Bioclusive or Tegaderm
- Do NOT cover with a heating pad or any other bandage
*Dispose of patch in the toilet
*Keep away from children and pets - Some patches need to be removed before MRI
Duragesic patch comes in what strengths:
12 mcg/h —> delivers 12.5mcg/hr
25 mcg/h
50 mcg/h
75 mcg/h
100 mcg/h
Sublimaze
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
fentanyl
class: opioid
Indications: chronic pain
MOA:
Dosage forms: injection
Dosing:
Max dose:
Boxed Warnings:
Potential for medication errors when converting between dosage forms, use with strong or moderate CYP3A4 inhibitors can result in increased effects and potentially fatal respiratory depression, avoid exposing transdermal fentanyl to external heat.
Contraindications:
Warnings:
Side Effects:
Hyperhidrosis (excessive sweating), dry mouth, asthenia, loss of appetite, application site redness/erythema (patch)
Monitoring: respiration rate
Pearls/Notes:
- Short half-life (t1/2) when given IV, (boluses given Q1-2hr); continuous infusion or PCA are most common
Outpatient use of fentanyl is for chronic pain management only
** Fentanyl is NOT used in opioid-naive patients; a patient who has been using equivalent to = Morphine 60mg/day for at least 7 days can be converted to a fentanyl patch**
Drug-Drug/Food interactions:
- Caution with other CNS depressants: additive somnolence, dizziness, confusion, increased risk of respiratory depression. These include alcohol, hypnotics, benzodiazepines and muscle relaxants. *Avoid Alcohol with ALL Opioids, especially ER formulations**.
- Increased risk of hypoxemia (low levels of oxygen in blood) with underlying respiratory disease (e.g. COPD) and sleep apnea.
- Fentanyl (is a CYP3A4 substrate), avoid use with CYP3A4 inhibitors, analgesic effect is decreased with CYP3A4 inducers.
What drugs are similar to fentanyl and are given IV only:
alfentanil (Alfenta)
remifentanil (Ultiva)
sufentanil (Dsuvia)
REMS program requires documentation of patients opioid tolerance with each prescription for ____________
transmucosal immediate release fentanyl
(systemic delivery of drug through the mucus membranes of oral cavity)
- buccal tablets = Fentora
- sublingual spray = Subsys
- oral lozenge on a stick “lollipop” = Actiq
Actiq
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
fentanyl
class: opioid
Indications: chronic cancer pain. Only for cancer BTP “break through pain”
MOA:
Dosage forms: lozenge on a stick “lollipop”
Dosing:
- Always start with 200mcg, can titrate to 4 BTP episodes/day.
Max dose:
Boxed Warnings:
Potential for medication errors when converting between dosage forms, use with strong or moderate CYP3A4 inhibitors can result in increased effects and potentially fatal respiratory depression, avoid exposing transdermal fentanyl to external heat.
Contraindications:
Warnings:
Side Effects:
Hyperhidrosis (excessive sweating), dry mouth, asthenia, loss of appetite, application site redness/erythema (patch)
Monitoring: respiration rate
Pearls/Notes:
Outpatient use of fentanyl is for chronic pain management only
** Fentanyl is NOT used in opioid-naive patients; a patient who has been using equivalent to = Morphine 60mg/day for at least 7 days can be converted to a fentanyl patch**
Drug-Drug/Food interactions:
- Caution with other CNS depressants: additive somnolence, dizziness, confusion, increased risk of respiratory depression. These include alcohol, hypnotics, benzodiazepines and muscle relaxants. *Avoid Alcohol with ALL Opioids, especially ER formulations**.
- Increased risk of hypoxemia (low levels of oxygen in blood) with underlying respiratory disease (e.g. COPD) and sleep apnea.
- Fentanyl (is a CYP3A4 substrate), avoid use with CYP3A4 inhibitors, analgesic effect is decreased with CYP3A4 inducers.
Lazanda
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
fentanyl
class: opioid
Indications: chronic pain
MOA:
Dosage forms: nasal spray
Dosing:
Max dose:
Boxed Warnings:
Potential for medication errors when converting between dosage forms, use with strong or moderate CYP3A4 inhibitors can result in increased effects and potentially fatal respiratory depression, avoid exposing transdermal fentanyl to external heat.
Contraindications:
Warnings:
Side Effects:
Hyperhidrosis (excessive sweating), dry mouth, asthenia, loss of appetite, application site redness/erythema (patch)
Monitoring: respiration rate
Pearls/Notes:
Outpatient use of fentanyl is for chronic pain management only
** Fentanyl is NOT used in opioid-naive patients; a patient who has been using equivalent to = Morphine 60mg/day for at least 7 days can be converted to a fentanyl patch**
Drug-Drug/Food interactions:
- Caution with other CNS depressants: additive somnolence, dizziness, confusion, increased risk of respiratory depression. These include alcohol, hypnotics, benzodiazepines and muscle relaxants. *Avoid Alcohol with ALL Opioids, especially ER formulations**.
- Increased risk of hypoxemia (low levels of oxygen in blood) with underlying respiratory disease (e.g. COPD) and sleep apnea.
- Fentanyl (is a CYP3A4 substrate), avoid use with CYP3A4 inhibitors, analgesic effect is decreased with CYP3A4 inducers.
Fentora
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
fentanyl
class: opioid
Indications: chronic pain
MOA:
Dosage forms: buccal tablets
Dosing:
Max dose:
Boxed Warnings:
Potential for medication errors when converting between dosage forms, use with strong or moderate CYP3A4 inhibitors can result in increased effects and potentially fatal respiratory depression, avoid exposing transdermal fentanyl to external heat.
Contraindications:
Warnings:
Side Effects:
Hyperhidrosis (excessive sweating), dry mouth, asthenia, loss of appetite, application site redness/erythema (patch)
Monitoring: respiration rate
Pearls/Notes:
Outpatient use of fentanyl is for chronic pain management only
** Fentanyl is NOT used in opioid-naive patients; a patient who has been using equivalent to = Morphine 60mg/day for at least 7 days can be converted to a fentanyl patch**
Drug-Drug/Food interactions:
- Caution with other CNS depressants: additive somnolence, dizziness, confusion, increased risk of respiratory depression. These include alcohol, hypnotics, benzodiazepines and muscle relaxants. *Avoid Alcohol with ALL Opioids, especially ER formulations**.
- Increased risk of hypoxemia (low levels of oxygen in blood) with underlying respiratory disease (e.g. COPD) and sleep apnea.
- Fentanyl (is a CYP3A4 substrate), avoid use with CYP3A4 inhibitors, analgesic effect is decreased with CYP3A4 inducers.
Subsys
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
fentanyl
class: opioid
Indications: chronic pain
MOA:
Dosage forms: sublingual spray,
Dosing:
Max dose:
Boxed Warnings:
Potential for medication errors when converting between dosage forms, use with strong or moderate CYP3A4 inhibitors can result in increased effects and potentially fatal respiratory depression, avoid exposing transdermal fentanyl to external heat.
Contraindications:
Warnings:
Side Effects:
Hyperhidrosis (excessive sweating), dry mouth, asthenia, loss of appetite, application site redness/erythema (patch)
Monitoring: respiration rate
Pearls/Notes:
Outpatient use of fentanyl is for chronic pain management only
** Fentanyl is NOT used in opioid-naive patients; a patient who has been using equivalent to = Morphine 60mg/day for at least 7 days can be converted to a fentanyl patch**
Drug-Drug/Food interactions:
- Caution with other CNS depressants: additive somnolence, dizziness, confusion, increased risk of respiratory depression. These include alcohol, hypnotics, benzodiazepines and muscle relaxants. *Avoid Alcohol with ALL Opioids, especially ER formulations**.
- Increased risk of hypoxemia (low levels of oxygen in blood) with underlying respiratory disease (e.g. COPD) and sleep apnea.
- Fentanyl (is a CYP3A4 substrate), avoid use with CYP3A4 inhibitors, analgesic effect is decreased with CYP3A4 inducers.
Fentanyl dosage forms:
- injection = Sublimaze
- patch = Duragesic
- oral lozenge on a stick “lollipop” = Actiq
- nasal spray = Lazanda
- buccal tablets = Fentora
- sublingual spray = Subsys
Norco*
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
hydrocodone IR + acetaminophen
class: opioid
Indications:
MOA:
Dosage forms: 2.5, 5, 7.5, 10 + 325mg acetaminophen
Dosing:
- usual starting dose: 5mg/325mg every 6 hours
Max dose:
Boxed Warnings:
**initiation of CYP3A4 inhibitors can cause fatal overdose.
Contraindications:
Warnings:
acetaminophen and opioids: respiratory and/or CNS depression, constipation, hypotension, skin reactions (rare), caution in liver disease (avoid or limit alcohol intake) and in CYP2D6 poor metabolizers.
Side Effects: pruritus, dry mouth, constipation
Monitoring:
Pearls/Notes:
Hydrocodone containing cough and cold preparations are no longer indicated in patients less than < 18 years of age - DO NOT USE
Drug-Drug/Food interactions:
Vicodin
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
hydrocodone IR + acetaminophen
class: opioid
Indications:
MOA:
Dosage forms: 2.5, 5, 7.5, 10 + 325mg acetaminophen
Dosing:
- usual starting dose: 5mg/325mg every 6 hours
Max dose:
Boxed Warnings:
**initiation of CYP3A4 inhibitors can cause fatal overdose.
Contraindications:
Warnings:
acetaminophen and opioids: respiratory and/or CNS depression, constipation, hypotension, skin reactions (rare), caution in liver disease (avoid or limit alcohol intake) and in CYP2D6 poor metabolizers.
Side Effects: pruritus, dry mouth, constipation
Monitoring:
Pearls/Notes:
Hydrocodone containing cough and cold preparations are no longer indicated in patients less than < 18 years of age - DO NOT USE
Drug-Drug/Food interactions:
Lortab*
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
hydrocodone IR + acetaminophen
class: opioid
Indications:
MOA:
Dosage forms: 2.5, 5, 7.5, 10 + 325mg acetaminophen
Dosing:
- usual starting dose: 5mg/325mg every 6 hours
Max dose:
Boxed Warnings:
**initiation of CYP3A4 inhibitors can cause fatal overdose.
Contraindications:
Warnings:
acetaminophen and opioids: respiratory and/or CNS depression, constipation, hypotension, skin reactions (rare), caution in liver disease (avoid or limit alcohol intake) and in CYP2D6 poor metabolizers.
Side Effects: pruritus, dry mouth, constipation
Monitoring:
Pearls/Notes:
Hydrocodone containing cough and cold preparations are no longer indicated in patients less than < 18 years of age - DO NOT USE
Drug-Drug/Food interactions:
Lorcet
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
hydrocodone IR + acetaminophen
class: opioid
Indications:
MOA:
Dosage forms: 2.5, 5, 7.5, 10 + 325mg acetaminophen
Dosing:
- usual starting dose: 5mg/325mg every 6 hours
Max dose:
Boxed Warnings:
**initiation of CYP3A4 inhibitors can cause fatal overdose.
Contraindications:
Warnings:
acetaminophen and opioids: respiratory and/or CNS depression, constipation, hypotension, skin reactions (rare), caution in liver disease (avoid or limit alcohol intake) and in CYP2D6 poor metabolizers.
Side Effects: pruritus, dry mouth, constipation
Monitoring:
Pearls/Notes:
Hydrocodone containing cough and cold preparations are no longer indicated in patients less than < 18 years of age - DO NOT USE
Drug-Drug/Food interactions:
Tussicaps
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
hydrocodone + chlorpheniramine
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Hycodan
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
hydrocodone + homatropine
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Zohydro ER
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
hydrocodone ER
class:
Indications:
MOA:
Dosage forms: ER capsule
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
- hydrocodone is a substrate for CYP3A4
- preferably avoid use if breastfeeding
- ABUSE-DETERRENT formulation
Drug-Drug/Food interactions:
Hysingla ER
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
hydrocodone ER
class:
Indications:
MOA:
Dosage forms: ER tablet
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
- hydrocodone is a substrate for CYP3A4
- preferably avoid use if breastfeeding
- ABUSE-DETERRENT formulation
*- QT prolongation has occurred at doses greater than > 160mg/day
Drug-Drug/Food interactions:
Dilaudid
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
hydromorphone
class: opioid
Indications:
MOA:
Dosage forms: tablet, injection, solution, suppository
Dosing:
*Oral: 2-4mg every 4-6 hours as needed
*IV: 0.2-1mg every 2-3 hours as needed
Max dose:
Boxed Warnings:
**- Risk of medication error with high potency (HP) injection, (Use in Opioid-Tolerant patients only)
Contraindications:
*- opioid-naive patients for ER tablet
Warnings:
Side Effects:
pruritus, dry mouth, hyperhidrosis
Monitoring:
Pearls/Notes:
- Potent: start low, convert carefully; High risk for overdose
- commonly used in PCAs and epidurals
- (HP) high potency injection (10mg/mL) is a higher potency injection than Dilaudid (1mg/mL).
- ER tablet: ABUSE-DETERRENT formulation (crush and extraction resistant) contraindicated in opioid-naive patients
**- Two-week washout required between hydromorphone and MAO inhibitors
Drug-Drug/Food interactions:
Caution with CYP3A4 inhibitors, Use lower doses initially
Dolophine
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
methadone
class: opioid
Indications:
-approved for heroin detox (used more for pain; its cheap and it works)
MOA:
Dosage forms: tablet, solution,
Dosing:
Max dose:
Boxed Warnings:
** Life threatening QT prolongation (proarrhythmic) and serious arrhythmias (e.g. Torsades de Pointes) have occurred during treatment (most involve large, multiple daily doses), should be prescribed by professionals who know requirements for safe use, initiation of CYP inhibitors (or stopping inducers can cause fatal overdose.
Contraindications:
Warnings:
- Combination with other serotonergic drugs or MAO inhibitors can increase the risk of serotonin syndrome, methadone also blocks reuptake of NE
Side Effects:
hyperhidrosis
Monitoring:
Pearls/Notes:
-* due to variable half-life (15-55hrs), methadone is hard to dose safely
-* can decrease testosterone and contribute to sexual dysfunction
-* methadone is a major CYP3A4 substrate; AVOID use with inhibitors or lower methadone dose
- serotonergic agent
- also blocks reuptake of norepinephrine
Drug-Drug/Food interactions:
Methadose
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
methadone
class:
Indications:
MOA:
Dosage forms: tablet
Dosing:
**Methadose 40mg soluble tablet; for detox and maintenance treatment in opioid addicted patients only
Initial: 2.5-10mg every 8-12hrs
Max dose:
Boxed Warnings:
** Life0threatening QT prolongation and serious arrhythmias (e.g. Torsades de Pointes) have occurred during treatment (most involve large, multiple daily doses), should be prescribed by professionals who know requirements for safe use, initiation of CYP inhibitors (or stopping inducers can cause fatal overdose.
Contraindications:
Warnings:
- Combination with other serotonergic drugs or MAO inhibitors can increase the risk of serotonin syndrome, methadone also blocks reuptake of NE
Side Effects:
hyperhidrosis
Monitoring:
Pearls/Notes:
-* due to variable half-life, methadone is hard to dose safely
-* can decrease testosterone and contribute to sexual dysfunction
-* methadone is a major CYP3A4 substrate; AVOID use with inhibitors or lower methadone dose
Drug-Drug/Food interactions:
Methadone Intensol
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
methadone
Demerol
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
meperidine
class: analgesic
Indications:
off-label is used for shivering and shaking for surgery
MOA:
Dosage forms: tablet, solution, injection
Dosing:
oral/IM/SC: 50-150mg every 3-4 hours as needed
Contraindications:
Warnings:
- Renal impairment/elderly at risk for CNS toxicity, Avoid with or within 2 weeks of MAO inhibitor
Side Effects:
hyperhidrosis
Monitoring:
Pearls/Notes:
*- Not for chronic pain; short acting, toxic metabolite
*- Not for elderly
- renally cleared metabolite normeperidine that is lipophilic
- CNS toxicity including tremors, seizures with high levels
- No longer recommended as an analgesic (especially in elderly and renally impaired); Avoid for chronic pain and even short-term in elderly).
- if cannot avoid use for acute pain, use short term or single use (e.g. sutures in ER)
-** Use Off label for post-operative rigors (shivering)
- Short duration of action (pain controlled max 3 hours)
- Normeperidine (toxic metabolite) is renally cleared and can accumulate and cause CNS toxicity including seizures
- In combination with other drugs, it is Serotonergic and can increase risk of serotonin syndrome.
Drug-Drug/Food interactions:
MS Contin
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
morphine ER
class: opioid
Indications:
MOA:
Dosage forms: tablet
Dosing:
Boxed Warning:
- medication errors with oral solution (note strength), appropriate staff and equipment needed for intrathecal/epidural administration
Contraindications:
Warnings:
Side Effects:
pruritus, dry mouth, hyperhidrosis
Monitoring:
Pearls/Notes:
-* Do NOT use MSO4 or MS abbreviations for morphine or magnesium
-* Do NOT crush and chew any ER products; Kadian* can be opened and sprinkled on applesauce or soft food
- if renally impaired, start at a lower dose, or avoid morphine, due to accumulation of parent drug and/or active metabolite
-* diphenhydramine or similar can be given to block histamine-induced pruritus
Drug-Drug/Food interactions:
Kadian
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
morphine ER
class: opioid
Indications:
MOA:
Dosage forms: capsule
Dosing:
Boxed Warning:
- medication errors with oral solution (note strength), appropriate staff and equipment needed for intrathecal/epidural administration
Contraindications:
Warnings:
Side Effects:
pruritus, dry mouth, hyperhidrosis
Monitoring:
Pearls/Notes:
-* Do NOT use MSO4 or MS abbreviations for morphine or magnesium
-* Do NOT crush and chew any ER products; Kadian* can be opened and sprinkled on applesauce or soft food
- if renally impaired, start at a lower dose, or avoid morphine, due to accumulation of parent drug and/or active metabolite
-* diphenhydramine or similar can be given to block histamine-induced pruritus
Drug-Drug/Food interactions:
Roxanol
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
morphine
Duramorph
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
morphine
Infumorph
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
morphine
Roxicodone
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
oxycodone IR
class: opioid
Indications:
MOA:
Dosage forms: tablet
Dosing:
Max dose:
Boxed Warnings:
-* Initiation of CYP3A4 inhibitors (or stopping inducers) can cause fatal overdose, caution with oxycodone oral solution and oral concentrate (confusion between mg/mL and different concentrations)
Contraindications:
Warnings:
Side Effects:
-* pruritus, dry mouth, hyperhidrosis
Monitoring:
Pearls/Notes:
- Abuse-deterrent formulations: Oxaydo, OxyContin, Xtampza ER
- Xtampza ER capsules can be opened and contents administered with soft food or through a gastric tube
- Avoid high fat meals with higher doses (except re-formulated OxyContin)
- if renally impaired, start at a lower dose, or avoid oxycodone, due to accumulation of parent drug and/or active metabolite
Drug-Drug/Food interactions:
OxyContin
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
oxycodone CR
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
* Abuse-deterrent formulation
Drug-Drug/Food interactions:
Xtampza ER
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
oxycodone ER
class:
Indications:
MOA:
Dosage forms: capsule
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
* Abuse-deterrent formulation
Drug-Drug/Food interactions:
Endocet
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
oxycodone + acetaminophen
Percocet
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
oxycodone + acetaminophen
Opana*
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
oxymorphone
class:
Indications:
MOA:
Dosage forms: tablet (IR, ER), injection
Dosing:
-IR (opioid-naive): 5-10mg every 4-6 hours as needed
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
*- Do not use with moderate to severe liver impairment
- use low doses in elderly, renal or mild liver impairment; there will be higher drug concentrations in these patients
- Take on empty stomach
Safety issues:
– report abuse, misuse, diversion
– DO NOT USE with 3A4 inhibitors*
Drug-Drug/Food interactions:
Opioid Allergy:
the common drugs in the same chemical class that cross-react with each other have COD in the name for-
CODeine
hydroCODone
oxyCODone
Opioid Allergy:
the common drugs in the same chemical class that cross-react with each other have MORPH in the name for-
MORPHine
hydroMORPHone
oxyMORPHone
-
- difficulty breathing
- severe drop in blood pressure
- serious rash
- swelling of the face, lips, tongue, larynx
” we would want to use an agent in a different class”
_________ and _______ can be used for pruritus caused from opioids.
hydroxyzine
diphenhydramine
All oral opioids (except ____________) should be taken with food to lessen nausea.
All opioids cause constipation, referred to as ______________.
Unlike CNS depression, _________ does not improve over time without treatment; it must be anticipated AND treated.
So, when opioids are dosed around the clock, such as with an ER opioid, prophylaxis for constipation is required
oxymorphone
(OIC) opioid induced constipation
(OIC) opioid induced constipation
First line for OIC is __________ with or without _________
If these are not sufficient, specific medications for OIC that counteract the effects of the opioid receptor in the gut, _____________ can be used.
stimulant laxative +/- stool softener
(e.g. bisacodyl +/- docusate) (senna +/- docusate)
(PAMORAs) Peripherally Acting Mu-Opioid Receptor Antagonists
Relistor
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
methylnaltrexone
class: PAMORA
Indications: Tx of OIC
- indicated for OIC and are only effective when constipation is secondary to use of an opioid.
MOA: drug blocks mu opioid receptors in the gut to reduce constipation without affecting analgesia.
Dosage forms:
Dosing:
Max dose:
Contraindications:
- * GI Obstruction*
Warnings:
-* Risk of GI perforation*
Side Effects:
-* abdominal pain, flatulence, diarrhea, nausea
Monitoring:
Pearls/Notes:
-* Stay close to toilet after injecting
-* discontinue all laxatives prior to use
-* Only for patients on opioids who have FAILED OTC laxatives
- Do not use routinely; can often increase laxative to obtain effect
Drug-Drug/Food interactions:
Movantik
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
naloxegol
class: PAMORA
Indications: Tx of OIC
- indicated for OIC and are only effective when constipation is secondary to use of an opioid.
MOA: drug blocks mu opioid receptors in the gut to reduce constipation without affecting analgesia.
Dosage forms:
Dosing:
Max dose:
Contraindications:
- * GI Obstruction*
Warnings:
-* Risk of GI perforation*
Side Effects:
-* abdominal pain, flatulence, diarrhea, nausea
Monitoring:
Pearls/Notes:
-* Do NOT Use with strong CYP3A4 inhibitors (e.g. grapefruit); avoid use or reduce dose to 12.5mg daily with moderate CYP3A4 inhibitors.
- discontinue al laxatives prior to use; can reintroduce laxatives if suboptimal response after 3 days
Drug-Drug/Food interactions:
Symproic
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
naldemedine
class: PAMORA
Indications: Tx of OIC
- indicated for OIC and are only effective when constipation is secondary to use of an opioid.
MOA: drug blocks mu opioid receptors in the gut to reduce constipation without affecting analgesia.
Dosage forms:
Dosing:
Max dose:
Contraindications:
- * GI Obstruction*
Warnings:
-* Risk of GI perforation*
Side Effects:
-* abdominal pain, flatulence, diarrhea, nausea
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Amitiza
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
lubiprostone
class: Chloride channel activator
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Both tramadol and tapentadol are _________________ and inhibitors of ____________.
Tramadol also inhibits reuptake of _________
Mu-opioid receptor agonists
NE reuptake
5-HT
Ultram
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
tramadol C-IV
class: opioid-centrally acting analgesics
Indications:
MOA: drug is a MU-opioid receptor agonist and also an inhibitor of NE and 5-HT reuptake
Dosage forms: Tablet IR/ER, ER capsule, solution
Dosing:
IR: 50-100 mg every 4-6 hours; MAX 400mg/day
ER: 100mg once daily; MAX 300mg/day
if CrCl < 30mL/min, then for
IR increase dosing interval to every 12 hours
ER DO NOT USE
Boxed Warning:
-* respiratory depression and death have occurred in children following tonsillectomy and/or adenoidectomy found to have evidence of being ultra-rapid metabolizers of tramadol due to a CYP2D6 polymorphism; use with CYP3A4 inducers/inhibitors or CYP2D6 inhibitors should be carefully considered due to variable effects
Contraindications:
-* DO NOT USE in children < 12 years of age; or in children < 18 years of age following tonsillectomy/adenoidectomy surgery
-** DO NOT USE with concurrent MAO inhibitors or within 14 days
Warnings:
-Seizure risk (avoid in patients with seizure history, head trauma),
-** Risk of serotonin syndrome when used alone or with other serotonergic drugs or inhibitors of CYP2D6 or 3A4**,
CNS depression, hypoglycemia, respiratory depression (rare), avoid in patients who are suicidal, risk of breathing problems in adolescents aged 12-18 years with obesity, sleep apnea or lung disease, breastfeeding mothers should avoid due to increased risk of serious breathing problems in breastfed infants.
Side Effects:
-* dizziness, constipation, nausea, somnolence or insomnia, dry mouth, pruritus, flushing, headache
Pearls/Notes:
- on the Beers list: post marketing reports of hyponatremia and SIADH
- Tramadol requires conversion to active metabolite by CYP2D6; use with CYP2D6 inhibitors has variable effects due to mixed mechanism of action of tramadol
- Avoid with CYP2D6 inhibitors
Drug-Drug/Food interactions:
Ultracet
tramadol + acetaminophen
Seglentis
tramadol + celecoxib
Nucynta
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
tapentadol C-II
class: opioid
Indications:
MOA:
Dosage forms: Tablet IR and ER
Dosing:
IR: 50-100mg every 4-6 hours
ER: 50-250mg BID
If CrCl < 30mL/min; Use Not recommended
Max dose:
Contraindications:
* Do NOT USE with concurrent MAO inhibitors or within 14 days**
Warnings:
Can increase seizure risk (avoid in patients with seizure history or seizure risk), risk of serotonin syndrome when used with other serotonergic drugs.
Side Effects:
dizziness, constipation, nausea, somnolence or insomnia, dry mouth, pruritus
Monitoring:
Pearls/Notes:
-* Tapentadol is a stronger analgesic than tramadol
Drug-Drug/Food interactions:
Opioid Drug Interactions:
Methadone
- Caution with agents that worsen cardiac function or increase arrhythmia risk. (remember methadone causes QT prolongation and arrythmia)
- Caution with other serotonergic agents
Opioid Drug Interactions:
Meperidine
- Caution with agents that worsen renal function, elderly and those with seizure history.
- Caution with other serotonergic agents.
Opioid Drug Interactions:
Tramadol and Tapentadol
- Caution with other agents that lower the seizure threshold.
- Caution with other serotonergic agents.
- Avoid tramadol with CYP2D6 inhibitors (requires conversion)
- possibility of increased INR with warfarin; monitor
- Tapentadol: not with MAO inhibitors
Methadone, Meperidine, Tramadol and Tapentadol are ALL _____
serotonergic
Tramadol and Tapentadol avoid in those with a ________
seizure history
Opioid Abuse: is now an epidemic in the U.S.
The US government has created 5 strategies to prevent overdose death:
1
2
3
4
5
1- educate providers and general public about how to prevent and manage opioid overdose
2- ensure access to treatment for patients addicted to opioids
3- ensure ready access to naloxone. Encourage providers to discuss the availability of naloxone with all patients prescribed opioids or medications to treat OUD.
4- encourage the public to call 911
5- encourage prescribers to use state (PDMP) Prescription Drug Monitoring Programs
Some opioid combination products such as Suboxone and Bunavail are formulated with abuse-deterrent medication ________
naloxone
OxyContin and Hysingla ER are manufactured using specific technology designed to deter crushing, dissolving or other modifications.
(OIRD) Opioid Induced Respiratory Depression:
-An opioid prescription requires a risk/benefit assessment and monitoring.
- A prescription for naloxone should be offered to patients with elevated risk factors for OIRD.
-
-
-
Risk Factors:
- History of previous overdose
- Substance abuse
- Using large doses (greater than > or equal to 50MME dose)
- using with benzodiazepines, gabapentin, or pregabalin
- comorbid illness such as respiratory and psychiatric disease
Buprenorphine is a _____________.
It is used in lower doses to treat _______ and higher doses to treat ________.
partial mu-opioid agonist
pain
addiction
Buprenorphine is an agonist at ___________ and an antagonist at _____________.
low doses
higher doses
Naloxone is an __________.
opioid antagonist It replaces the opioid on the mu receptor.
Naloxone given by itself is used for _______
opioid overdose
The combination product buprenorphine/naloxone are used as alternatives to methadone for ___________.
buprenorphine suppresses _____________
naloxone helps prevent _________
opioid dependence
withdrawal symptoms
misuse
Naltrexone is an _________
It is available as a __________
opioid antagonist and normally is used to treat alcohol and opioid dependence.
daily oral formulation and a monthly IM injection (Vivitrol)
Drugs formulated to mitigate abuse:
- Suboxone, Troxyca ER, Embeda
) Formulated with an abuse deterrent medication (e.g. naloxone or naltrexone) - OxyContin, Hysingla ER Armyo
) designed to deter crushing or dissolving.
Opioid Overdose Management:
-
-
-
- extreme sleepiness
- slow or shallow breathing
- fingernails or lips turning blue or purple
- extremely small “pinpoint” pupils
- slow heartbeat
- low blood pressure
Opioid Overdose Management:
remember that opioids last longer than naloxone, so monitor closely for respiratory depression and provide repeat doses, as needed
Naloxone is available in two options:
Narcan (nasal spray):
Naloxone (injection):
What are pros and cons of each?
Narcan (nasal spray):
- onset of action is slower than injection
- a single use nasal spray (4mg) administered in 1 nostril
- DONT PRIME device or dose is wasted
- repeat doses in alternating nostrils may be needed
Naloxone (injection):
- generic formulation provided in multiple size vials
- separate syringe will be needed
- may need to repeat doses every 2-3 minutes until emergency medical assistance arrives
Vivitrol
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
naltrexone
class: Opioid Antagonist
Indications: (AUD) alcohol Use Disorder, (OUD) Opioid Use Disorder
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Narcan
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
naloxone
class: Opioid Antagonist
Indications: Opioid Overdose
MOA: drug competes with opioid at the Mu- opioid receptors, drug displaces opioids at opioid receptor sites.
Dosage forms: Nasal Spray
Dosing:
Nasal spray: 1 spray (4mg) can repeat.
**Repeat Dosing can be required (opioid can last longer than blocking agent)
Max dose:
Contraindications:
Warnings:
Side Effects:
Opioid-dependent: acute withdrawal symptoms (pain, anxiety, tachypnea- abnormal rapid breathing)
Nasal- nasal dryness/congestion/swelling
Monitoring:
Pearls/Notes:
- if patient is on opioids ATC, then patient will experience pain after administering naloxone, since opioid effects were reversed
Onset: ~5min
t1/2 = 30min - 120min
Drug-Drug/Food interactions:
Evzlo
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
naloxone
- autoinjector
- talks to you and tells you how to use it
class: Opioid Antagonist
Indications: Opioid Overdose
MOA: drug competes with opioid at the Mu- opioid receptors, drug displaces opioids at opioid receptor sites.
Dosage forms: autoinjector
Dosing:
IM- give in thigh through clothing, hold for 5 seconds, then call 911.
**Repeat Dosing can be required (opioid can last longer than blocking agent)
Max dose:
Contraindications:
Warnings:
Side Effects:
Opioid-dependent: acute withdrawal symptoms (pain, anxiety, tachypnea- abnormal rapid breathing)
Injection- site reactions (erythema/irritation)
Monitoring:
Pearls/Notes:
Onset: 2-5min
t1/2 = 30min - 90min
Drug-Drug/Food interactions:
Kloxxado
naloxone nasal spray
Zimhi
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
naloxone injection
class:
Indications:
MOA:
Dosage forms:
Dosing:
If for IV Infusion: 0.4mg/hr
SUBQ: 0.4-2mg every 2-3 min
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Onset: 2-5min
Drug-Drug/Food interactions:
Belbuca
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
buprenorphine C-III
class: Opioid Partial Agonist
Antagonist at higher doses
Indications:
MOA: drug exerts its analgesic effect via high-affinity binding to mu-opioid receptors in the CNS. Due to it being a partial mu-opioid agonist, its analgesic effects plateau at higher doses and it then behaves like an antagonist.
Dosage forms: buccal film
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Butrans
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
buprenorphine C-III
class: Opioid Partial Agonist
Antagonist at higher doses
Indications: treatment of (OUD) Opioid Use Disorder
MOA: drug exerts its analgesic effect via high-affinity binding to mu-opioid receptors in the CNS. Due to it being a partial mu-opioid agonist, its analgesic effects plateau at higher doses and it then behaves like an antagonist.
Dosage forms: Transdermal patch
5mcg/hr, 7.5mcg/hr, 10mcg/hr, 15mcg/hr, 20mcg/hr
Dosing:
(opioid-Naive): 5mcg/hr patch once weekly
Max dose:
Boxed Warnings:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
-** Apply to upper arm, upper chest, side of chest, upper back. [CHANGE WEEKLY].
-** Apply to a hairless or nearly hairless skin site
-** DO NOT USE same site for at least 3 weeks
- you should change the skin site where you apply each week, making sure that at least 3 weeks (21 days) pass before you re-use the same skin site
- Use only water to clean application site. You should NOT use soaps, alcohols, oils, lotions, or abrasive devices. Allow the skin to dry before you apply the patch.
-** Dispose of used patches in the patch disposal unit or fold and flush.
t1/2 = ~26 hours for transdermal patch
Drug-Drug/Food interactions:
Buprenex
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
buprenorphine C-III
class: Opioid Partial Agonist
Antagonist at higher doses
Indications:
MOA: drug exerts its analgesic effect via high-affinity binding to mu-opioid receptors in the CNS. Due to it being a partial mu-opioid agonist, its analgesic effects plateau at higher doses and it then behaves like an antagonist.
Dosage forms: injection
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Probuphine
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
buprenorphine C-III
class: Opioid Partial Agonist
Antagonist at higher doses
Indications:
MOA: drug exerts its analgesic effect via high-affinity binding to mu-opioid receptors in the CNS. Due to it being a partial mu-opioid agonist, its analgesic effects plateau at higher doses and it then behaves like an antagonist.
Dosage forms: implant kit
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Sublocade
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
buprenorphine C-III
class: Opioid Partial Agonist
Antagonist at higher doses
Indications:
MOA: drug exerts its analgesic effect via high-affinity binding to mu-opioid receptors in the CNS. Due to it being a partial mu-opioid agonist, its analgesic effects plateau at higher doses and it then behaves like an antagonist.
Dosage forms: once-monthly injection
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Suboxone
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
buprenorphine + naloxone C-III
class:
Indications: (OUD) Opioid Use Disorder
MOA:
Dosage forms: sublingual film
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Zubsolv
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
buprenorphine + naloxone C-III
class:
Indications:
MOA:
Dosage forms: sublingual tablet
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Bunavail
class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
buprenorphine + naloxone C-III
class:
Indications:
MOA:
Dosage forms: buccal film
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Adjuvants for Pain Management:
1)
2)
3)
4)
5)
1) Antiepileptic drugs
2) Antidepressants (SNRIs & TCAs)
3) Antispasmodics (muscle relaxants) with analgesic effects
4) Antispasmodics (muscle relaxants) work via sedation
5) Topical analgesics
Adjuvants for Pain Management:
- are useful in pain management though they are not classified as analgesics
- these drugs can be added on to opioid or non-opioid analgesics (multimodal treatment), to further relieve/control pain
- commonly used in pain associated with neuropathy (from diabetes or spinal cord injury), (PHN) postherpetic neuralgia, fibromyalgia, osteoarthritis (OA) and others.
-
Adjuvants for Pain Management:
are useful for neuropathic pain.
- (AED) antiepileptic drugs
- Antidepressants (TCAs and SNRIs)
TCAs and SNRIs block norepinephrine uptake, which has shown to be beneficial in neuropathic pain! SSRIs do NOT have this effect!
Neurontin
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gabapentin
Gralise
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gabapentin tablet
Horizant
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gabapentin ER tablet
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** for (PHN) postherpetic neuralgia and (RLS) restless leg syndrome
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Lyrica
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pregabalin C-IV
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*fibromyalgia
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Tegretol
Tegretol XR
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carbamazepine
Savella
Savella titration pack
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milnacipran
Elavil*
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amitriptyline
Norpramin
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desipramine
Cymbalta
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duloxetine
Lioresal
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baclofen
class:
- muscle relaxant WITH analgesic effects
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- ALL MUSCLE RELAXANTS: cause excessive sedation, dizziness, confusion, asthenia (muscle weakness)
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Flexeril*
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cyclobenzaprine
class:
- muscle relaxant WITH analgesic effects
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- ALL MUSCLE RELAXANTS: cause excessive sedation, dizziness, confusion, asthenia (muscle weakness)
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- **Serotonergic: Do not combine with other serotonergic agents
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Amrix
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cyclobenzaprine
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- muscle relaxant WITH analgesic effects
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- ALL MUSCLE RELAXANTS: cause excessive sedation, dizziness, confusion, asthenia (muscle weakness)
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Fexmid
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cyclobenzaprine
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- muscle relaxant WITH analgesic effects
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- ALL MUSCLE RELAXANTS: cause excessive sedation, dizziness, confusion, asthenia (muscle weakness)
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Zanaflex
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tizanidine
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- muscle relaxant WITH analgesic effects
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- ALL MUSCLE RELAXANTS: cause excessive sedation, dizziness, confusion, asthenia (muscle weakness)
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- Is a Centrally acting alpha-2 agonist
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Soma
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carisoprodol C-IV
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- muscle relaxant exerts effects via SEDATION
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- ALL MUSCLE RELAXANTS: cause excessive sedation, dizziness, confusion, asthenia (muscle weakness)
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Skelaxin
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metaxalone
class:
- muscle relaxant exerts effects via SEDATION
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- ALL MUSCLE RELAXANTS: cause excessive sedation, dizziness, confusion, asthenia (muscle weakness)
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Robaxin
Robaxin-750
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methocarbamol
class:
- muscle relaxant exerts effects via SEDATION
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- ALL MUSCLE RELAXANTS: cause excessive sedation, dizziness, confusion, asthenia (muscle weakness)
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Topical adjuvants:
Lidocaine patches-
- unique cause you can cut these to fit them on the area you want to place them on.
- can have on 1-3 patches a day for a max of 12 hours
Zostrix
capsaicin cream 0.025% and 0.075%
- comes from the red peppers
- needs to be applied multiple times a day
- wash hands really good after applying with soap and water. Avoid contact with sensitive area’s, such as eyes.
