Exam 1 Drugs + Brands + MOA (Self-Care)

Fever, Headache, Dysmenorrhoea, Musculoskeletal, Colds&Coughs, Allergic Rhinitis

Acetaminophen

Tylenol

MOA:

• Antipyretic: central inhibition of prostaglandins synthesis [PGE2 synthesis for fever]

• Analgesic: unclear

• weak inhibitor of PGF2 synthesis (for dysmenorrhea)

Ibuprofen

Motrin, Advil

MOA: analgesic, antipyretic, anti-inflammatory

• Inhibits COX 1 and COX 2 centrally and peripherally to reduce prostaglandins [PGE2 for fever]

• Inhibits PGF2 - alpha (involved in smooth muscle contraction) to reduce contraction in dysmenorrhea

Naproxen

Aleve (OTC), Naprosyn (Rx)

MOA:

• Inhibits COX-1 and COX-2 centrally and peripherally to reduce prostaglandins [PGE2 for fever]

Aspirin

Ecotrin, Bayer

MOA: Analgesic, antipyretic, and anti-inflammatory

• Inhibits COX-1 and COX-2 centrally and peripherally to reduce prostaglandins [PGE2 for fever]

• for antipyretic effect it works more peripherally

• For CV protection: MOA is irreversible anti-platelet effects (inhibits platelet aggregation)

Asprin, APAP, caffeine

Exedrine Migraine

caffeine - vasoconstriction

APAP and Naproxen

Tylenol with Naproxen

Ibuprofen + Acetaminophen

Advil Dual Action

NSAID or APAP + Decongestant (PE or phenylephrine)

Advil Cold and Sinus, Tylenol Cold and Sinus

Diclofenac gel

Voltaren gel

MOA: same MOA as oral NSAIDs, but only effective locally, which provides pain relief with low systemic absorption.

• not effective at treating inflammation

Trolamine salicylate

Aspercreme

Absorbed through the skin and concentrates the synovial fluid reducing pain at the site by inhibiting peripheral PG synthesis

Capsaicin

Zostrix, Capzasin

MOA Counterirritant – Stimulates TRPV1 and release of substance P inducing burning/warmth feeling, which goes away with regular use approximately 1-2 weeks Chronic pain reliever-- Chronically depletes substance P from sensory neurons both peripherally and centrally.

Lidocaine (4% OTC)

Salonpas, Aspercreme lidocaine, Tylenol Precise

MOA

Blocks the initiation and conduction of nerve impulses by decreasing the membrane permeability to sodium ions

Pseudoephedrine

Sudafed

MOA: stimulates alpha-adrenergic receptors in the nose/sinuses and causing vasoconstriction, decreasing sinusoid vessel engorgement and mucosal edema.

Phenylephrine (oral) + (Topical)

Sudafed PE (oral), Neosynephrine (topical)

MOA: stimulates alpha-adrenergic receptors in the nose/sinuses and causing vasoconstriction, decreasing sinusoid vessel engorgement and mucosal edema.

Oxymetazoline

Afrin

MOA: stimulates alpha-adrenergic receptors in the nose/sinuses and causing vasoconstriction, decreasing sinusoid vessel engorgement and mucosal edema.

Nasal Saline

Neilmed irrigation, Ayr, Ocean sprays

MOA: relieves nasal irritation and dryness, aiding in removal of thick/dried mucus from nose

Menthol/Camphor

Vicks, Mentholatum for Kids

Camphor MOA

Rubefacient---when applied vigorously (warm feeling)

Analgesic, anesthetic and antipruritic at concentrations < 3% = depresses cutaneous receptors

Counterirritant – 3-11% stimulates nerve endings to produce a mild sensation of pain/discomfort (cool sensation)

MOA nasal/chest congestion: menthol and camphor vapors stimulate sensory nerve endings creating a local anesthetic sensation and sense of improved airflow.

Menthol MOA

Flavoring agent—tiny quantities

Counterirritant – >1.25%, stimulates cutaneous receptor  (TRPM8) producing a cold sensation, followed by warmth

MOA General: Menthol stimulates TRPM8 receptors (anesthetic)

Anesthetic and antipruritic - at concentrations < 1% = depresses cutaneous receptors

MOA Cough: lozenges decrease throat irritation and increase saliva causing a reduction in cough. Suppresses cough reflex sensitivity.

MOA nasal/chest congestion: menthol and camphor vapors stimulate sensory nerve endings creating a local anesthetic sensation and sense of improved airflow.

Methyl Salicylate

Counterirritant and Rubefacient = HOT Causes vasodilation of cutaneous vasculature producing reactive hyperemia. Topical NSAID: inhibits both central (due to systemic salicylate properties) and peripheral PG synthesis at the site of application Minor anti-inflammatory effects due to systemic absorption

Dextromethorphan

Robitussin DM, Delsym,

MOA: non-opioid; acts centrally in medulla to increase cough threshold

Diphenhydramine + 1st gen antihistamine MOA

Benadryl

MOA: competitively, blocks histamine at central and peripheral histamine-1 (H1) receptor sites

MOA nasal: acts peripherally in nose to dry up nasal secretions (anticholinergic)

MOA cough: Acts centrally in medulla to increase cough threshold AND decreases/dries up post-nasal drip (peripherally) to reduce cough

MOA insomnia: Crosses blood brain barrier (BBB) to cause sedation

Chlorpheniramine

Chlortrimeton

Brompheniramine

Dimetapp

Triprolidine + pseudoephedrine

Actifed, Aprodine

Guaifenesin

Mucinex

MOA:

• chest congestion: thins mucus and increases the volume of expectorated sputum

• nasal congestion: thins nasal secretions

Benzocaine lozenge

Cepacol

MOA: decreases permeability of sodium ions/depresses cutaneous receptors, which results in blockage of nerve conduction to cause numbing

Zinc

Zicam

MOA:

• prevents adhesion of human rhinovirus to nasal epithelium

• inhibits viral replication by disrupting viral capsid formation

Vitamin C

Emergen-C

MOA: possibly affects rhinovirus and boosts immune system (increased levels of Vit C in WBCs)

Loratadine, Fexofenadine, Cetirizine, Levocetirizine, Desloratadine

• Claritin - Loratadine

• Allegra - Fexofenadine

• Zyrtec - Cetirizine

• Xyzal - Levocetirizine

• Clarinex - Desloratadine

MOA: Competitively block H1 receptors peripherally

Antihistamine + Pseudoephedrine

Claritin-D, Allegra-D, Zyrtec-D

Triamcinolone

Nasacort

MOA: Inhibit multiple inflammatory cells and mediators including histamine to effectively stop the allergic cascade

Fluticasone Furoate

Flonase Sensimist

MOA: Inhibit multiple inflammatory cells and mediators including histamine to effectively stop the allergic cascade

Fluticasone Propionate

Flonase

MOA: Inhibit multiple inflammatory cells and mediators including histamine to effectively stop the allergic cascade

Budesonide

Rhinocort

MOA: Inhibit multiple inflammatory cells and mediators including histamine to effectively stop the allergic cascade

Mometasone

Nasonex

MOA: Inhibit multiple inflammatory cells and mediators including histamine to effectively stop the allergic cascade

Azelastine nasal spray

Astepro

MOA: potent, selective H1 receptor antagonist (2nd generation antihistamine)

Cromolyn nasal spray

Nasalcrom

Blocks influx of Ca2+ into mast cells to stabilize and prevent mediator (histamine) release

Ketotifen

Zaditor, Alaway

Potent 2nd generation, selective H1 receptor antagonist

+

Mast cell stabilizer(inhibits release of histamine from mast cells)

Olopatadine

Pataday

Potent 2nd generation, selective H1 receptor antagonist

       +

Mast cell stabilizer(inhibits release of histamine from mast cells)

Pheniramine/naphazoline (opthalmic)

Naphcon-A, Opcon-A, Visine-A

MOA: Pheniramine is a selective H1 receptor antagonist   Naphazoline is an Alpha-1 receptor agonist — reduces redness

Fish Oil

Compete with arachidonic acid in the COX and lipoxygenase paths decreasing production of pro-inflammatory cytokines.

Glucosamine & Chondroitin MOA

Glucosamine: Mucopolysaccharide – Stimulates chondrocytes to produce cartilage and synoviocytes to produce synovial fluid and hyaluronic acid, inhibits matrix metalloproteinase and modulates inflammatory cytokine activity

Chondroitin: Chondroprotectant

Codeine

MOA: Opioid; acts centrally on the cough control center (medulla) to increase cough threshold.

Echinacea

may exhibit antiviral activity and boost immune function