3PD Top 200 drugs - Fall 2024 - Pain/musculoskeletal agents

Acetaminophen; Hydrocodone brand name

Norco, Lortab, Vicodin, Lorcet, Hysingla ER

Acetaminophen; Hydrocodone Therapeutic Class

Opioid Analgesic. C-II

Acetaminophen; Hydrocodone FDA Labeled indications

Pain, severe

Acetaminophen; Hydrocodone MOA

binds to opiate receptors, resulting in altered perception of pain.

Acetaminophen; Hydrocodone Box Warnings

Addiction, abuse, misuse, REMS, respiratory depression, accidental ingestion, neonatal opioid withdrawal, alcohol, CYP3A4/5 interactions, hepatotoxicity, concurrent use with benzodiazepines

Acetaminophen; Hydrocodone ADRs

Constipation, GI distress, somnolence

Acetaminophen; Hydrocodone Counseling Points

Use a stool softener and/or laxative for preventing constipation with chronic use.

May cause drowsiness; avoid driving or other tasks requiring motor coordination.

Avoid alcohol and other CNS depressants.

Baclofen Brand Name

Lioresal, Ozobax, Fleqsuvy

Baclofen Therapeutic class

Centrally Acting Skeletal Muscle Relaxant

Baclofen FDA labeled indications

Spasticity

Baclofen MOA

inhibits both monosynaptic and polysynaptic reflexes at the spinal level, possibly by hyperpolarization of afferent terminals, although actions at supraspinal sites may also occur and contribute to its clinical effect. It is an analogue of γ-aminobutyric acid (GABA)

Baclofen Box warnings

Avoid abrupt discontinuation of oral or intrathecal product

Baclofen ADRs

Nausea, asthenia, dizziness, somnolence, confusion

Baclofen Key counseling points

Because of the possibility of sedation, be cautioned regarding the operation of motor vehicles or dangerous machinery while taking.

be cautioned that the CNS effects may be additive to those of alcohol and other CNS depressants.

Burpenorphine/Naloxone brand name

Suboxone, Zubsolv

Burpenorphine/Naloxone Therapeutic class

Opioid Partial Agonist and Antagonist Combination. C-III

Burpenorphine/Naloxone FDA labeled indications

Opioid use disorder

Buprenorphine/Naloxone MOA

Bup: μ-opioid receptor partial agonist and alpha-opioid receptor antagonist.

Naloxone: μ-opioid receptor antagonist that causes opioid withdrawal when injected parenterally and is included in the formulation to reduce the risk of abuse.

Burpenorphine/Naloxone Box warnings

None

Buprenorphine/Naloxone ADRs

Vasodilation, sweating, headaches, insomnia, constipation, GI distress, opioid withdrawal, dizziness

Burpenorphine/Naloxone counseling points

Use a stool softener and/or laxative for preventing constipation.

May cause drowsiness; avoid driving or other tasks requiring motor coordination. Avoid alcohol and other CNS depressants.

Do not crush or swallow the sublingual tablet. Place the tablet under the tongue until it is dissolved. If you take ≥2 tablets at a time, place all of the tablets under the tongue together. If this is uncomfortable, place 2 tablets at a time under the tongue and repeat the process until all tablets have been taken. If you are using the sublingual film, place the film under the tongue until it is dissolved. If you need to take an additional film, place the new film on the opposite side from the first film. Do not chew, swallow, or move the film after placing it under the tongue.

Carisoprodol brand name

Soma, Vanadom

Carisoprodol therapeutic class

Centrally Acting Skeletal Muscle Relaxant. C-IV

Carisoprodol FDA labeled indications

Disorder of musculoskeletal system

Carisoprodol MOA

blocks interneuronal activity in descending reticular formation and spinal cord, resulting in muscle relaxation.

Carisoprodol Box Warnings

none

Carisoprodol ADRs

Drowsiness, dizziness

Carisoprodol counseling points

avoid consuming alcohol.

avoid activities requiring mental alertness or coordination until drug effects are known, as drug may cause dizziness or sedative effects.

Patients withdrawing from prolonged therapy should be monitored carefully for withdrawal symptoms, including seizures.

Celecoxib brand name

Celebrex

Celecoxib Class

Cyclooxygenase-2 (COX-2) Inhibitor - NSAID

Celecoxib FDA labeled indications

Osteoarthritis

Rheumatoid arthritis

Ankylosing spondylitis

Acute pain, primary dysmenorrhea

Celecoxib MOA

Inhibition of the COX-2 enzyme isoform is thought to be responsible for the anti-inflammatory effects

Celecoxib Box warnings

Cardiotoxicity, CABG

Celecoxib ADRs

HTN, headaches, GI distress, diarrhea

Celecoxib counseling Points

May take with food or milk to decrease GI upset.

May open capsule and pour into a teaspoon of applesauce.

Codeine with Acetaminophen brand name

Tylenol with Codeine

Codeine with Acetaminophen Class

Opioid. C-II (when in combination with acetaminophen, C-III for tablets, C-V for liquid)

Codeine with Acetaminophen FDA labeled indications

Pain

Codeine with Acetaminophen MOA

is 3-methylmorphine, a phenanthrene opioid with very low affinity for opioid receptors. Its analgesic activity appears to result from conversion to morphine.

Codeine with Acetaminophen box warnings

Abuse, REMs, respiratory depression, accidental ingestion, CYP2D6 in children, neonatal withdrawal syndrome, interactions with CYP3A4/5, 2D6, avoid concomitant benzodiazepines and CNS depressants

Codeine with Acetaminophen ADRs

Nausea, vomiting, constipation, somnolence

Codeine with Acetaminophen counseling points

If using chronically, use laxative for preventing constipation.

May cause drowsiness; avoid driving or other tasks requiring motor coordination. Avoid alcohol.

Cyclobenzaprine Hydrochloride brand name

Flexeril, Amrix, Fexmid

Cyclobenzaprine Class

Centrally Acting Skeletal Muscle Relaxant

Cyclobenzaprine FDA labeled indications

Skeletal muscle spasm

Cyclobenzaprine MOA

relieves skeletal muscle spasm of local origin without interfering with muscle function. It is ineffective in muscle spasm due to CNS disease. Evidence suggests that the net effect is a reduction in tonic motor activity, influencing both gamma (γ) and alpha (α) motor systems.

Cyclobenzaprine Box warning

none

Cyclobenzaprine ADRs

Xerostomia, headache, dizziness, drowsiness

Cyclobenzaprine counseling points

avoid activities requiring mental alertness or coordination until drug effects are known, as drug may cause dizziness or sedative effects.

Take extended-release capsule same time each day.

Diclofenac brand name

Voltaren, Voltaren XR

Diclofenac class

NSAID

Diclofenac FDA labeled indications

Pain

Dysmenorrhea

Migraine

Osteoarthritis

Rheumatoid arthritis

Ankylosing spondylitis

Diclofenac MOA

Nonselective inhibitor of cyclo-oxygenase-1 (COX-1) and cyclo-oxygenase-2 (COX-2).

Diclofenac box warning

Cardiovascular, GI risk, CABG

Diclofenac ADRS

Headaches, GI distress

Diclofenac counseling points

Take with food or milk to decrease GI upset.

Fentanyl (Transdermal) brand name

Duragesic

Fentanyl Class

Opioid Analgesic. C-II

Fentanyl FDA labeled indications

Pain, chronic

Chronic cancer pain, management of breakthrough

Fentanyl MOA

phenylpiperidine opioid agonist with predominant effects on the mu-opioid receptor and is about 50-100 times more potent as an analgesic than morphine.

Fentanyl box warnings

Respiratory depression; addiction, CYP3A4/5 interactions, fatalities in children; formulations not interchangeable; care with disposal; REMS program; concurrent use with benzodiazepines or other CNS depressants, neonatal withdrawal, medication errors, heat exposure

Fentanyl ADRs

Application site reactions, sweating, constipation, GI distress, confusion, headache, anxiety, urinary retention, fatigue

Fentanyl counseling points

Use a laxative for preventing constipation.

May cause drowsiness; avoid driving or other tasks requiring motor coordination.

Avoid alcohol and other CNS depressants.

Apply to clean, dry skin. Skin breaks may increase absorption.

Remove old patch when new patch applied.

Febrile patients may have increased absorption. Monitor carefully.

Hydrocodone Brand Name

Norco, Lorcet, Vicodin, Hysingla ER

Hydrocodone Therapeutic Class

Opioid Analgesic. C-II

Hydrocodone FDA Labeled indications

Pain, severe

Hydrocodone MOA

binds to opiate receptors, resulting in altered perception of pain.

Hydrocodone Box warning

Addiction, abuse, misuse, REMS, respiratory depression, accidental ingestion, neonatal opioid withdrawal, alcohol, CYP3A4/5 interactions, hepatotoxicity, concurrent use with benzodiazepines

Hydrocodone ADRs

Constipation, GI distress, somnolence

Hydrocodone Counseling Points

Use a stool softener and/or laxative for preventing constipation with chronic use.

May cause drowsiness; avoid driving or other tasks requiring motor coordination.

Avoid alcohol and other CNS depressants.

Hydrocortisone rectal brand name

Anusol-HC, Proctosol-HC

Hydrocortisone rectal FDA Labeled indications

Skin disorders, corticosteroid responsive

Ulcerative colitis and Proctitis

Hydrocortisone Therapeutic Classification

Topical Corticosteroid

Hydrocortisone MOA

anti-inflammatory, antipruritic, and vasoconstrictive properties, are thought to act by the induction of phospholipase A2-inhibitory proteins, lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.

Hydrocortisone Box warning

None

Hydrocortisone ADRs

None

Hydrocortisone counseling points

Apply thin layer to affected area of skin. Skin should be clean and intact at site of application. Avoid contact with eyes and do not ingest by mouth. Avoid occlusive dressings or tight-fitting clothes over site of administration. Wash hands after application.

Ibuprofen brand name

Motrin

Ibuprofen therapeutic class

NSAID

Ibuprofen FDA labeled indications

Fever

Pain, headache

Osteoarthritis or rheumatoid arthritis

Juvenile rheumatoid arthritis

Ibuprofen Box warning

Cardiovascular events, GI toxicity, CABG

Ibuprofen MOA

Nonselective inhibitor of cyclo-oxygenase-1 (COX-1) and cyclo-oxygenase-2 (COX-2), and reversibly alters platelet function and prolongs bleeding time.

Ibuprofen Counseling Points

Take with food or milk to decrease GI upset.

Counsel patients with heart failure to avoid NSAIDs as they may cause fluid retention which can exacerbate heart failure.

Ibuprofen common ADRs

None

Lidocaine Transdermal brand name

Lidoderm

Lidocaine therapeutic class

Local Anesthetic

Lidocaine FDA Labeled indications

Postherpetic neuralgia and localized pain

Lidocaine MOA

amide-type local anesthetic agent and is suggested to stabilize neuronal membranes by inhibiting the ionic fluxes required for the initiation and conduction of impulses

Lidocaine Box warning

None

Lidocaine ADRs

Skin irritation, somnolence

Lidocaine counseling points

Instruct patients on the appropriate application process. Leave patches on skin for no >12 h within a 24-h period

Caution patients to administer only as directed, to intact skin, without covering with occlusive dressing or tight clothes.

Meloxicam brand name

Mobic

Meloxicam Therapeutic Class

NSAID

Meloxicam FDA Labeled indications

Osteoarthritis

Rheumatoid arthritis

Juvenile rheumatoid arthritis

Meloxicam MOA

Nonselective inhibitor of COX-1 and COX-2 which results in decreased formation of prostaglandin precursors; has antipyretic, analgesic, and anti-inflammatory properties; reversibly alters platelet function and prolongs bleeding time.

Meloxicam Box warning

Cardiovascular thrombotic events, serious GI bleeding and perforation, CABG

Meloxicam ADRs

GI distress

Meloxicam Counseling Points

Take with food or milk to decrease GI upset.

For suspension, shake gently before using.

Avoid use around 20 wk gestation. Pregnant women should consult HCP before using.

Methocarbamol Brand name

Robaxin

Methocarbamol Therapeutic Class

Centrally Acting Skeletal Muscle Relaxant