Introduction to

Pain, Cough/Cold,
Allergy and GI
Abigail Geyer, PharmD
PGY1 Pharmacy Resident
Parkview Health │ Fort Wayne, IN
 OTC and
Prescription
Options

Pain and
Inflammatio
n
Pain and Inflammation: Objectives
• Understand the mechanistic differences between NSAIDs and
acetaminophen and how that impacts clinical effects
• List important adverse effects associated with NSAIDs,
acetaminophen, and opioids
• Select an appropriate treatment option for pain depending on patient
specific factors
Overview of Pain
• Definition: an unpleasant sensory and emotional experience associated with actual or
potential tissue damage or described in terms of such damage
• Nociceptive pain– pain in response to a noxious stimulus

Stimulation: reception
of noxious impulse at Transmission:
nociceptors from impulses are
tissue insult
Modulation:
transmitted from endogenous
Chemical compounds peripheral site Perception:
opiates, gate
released to sensitize toward spinal cord nociceptive
nociceptors
control theory,
information travels
Substance P and inhibitory
Prostaglandins, to brain
glutamate facilitate descending
bradykinin, histamine,
serotonin, transmission of pathways
leukotrienes, signal
substance P
 • Pain is subjective
• Patient report is the gold standard in assessment
• PQRST Characteristics
• Palliative, quality, radiation, severity/intensity,
temporal factors
• Ask questions!
Evaluating Pain
• Numeric rating scale, visual analog scale
• Wong-Baker FACES pain scale
 Nonsteroidal Anti-Inflammatory Drugs
(NSAIDs)

• Mechanism: inhibits prostaglandin

synthesis from arachidonic acid;
inhibits COX-1 and -2 in the periphery
• Antipyretic and analgesic
• Anti-inflammatory at higher doses
• Equally effective
• Ceiling effect
Cyclooxygenase (COX) 1 and 2
COX-1 COX-2

Produces prostaglandins Induced by noxious stimuli

that produce gastro- that lead to pain and
protective barrier inflammation

Prostaglandins that Located at sites of

promote renal perfusion inflammation

Inhibiting COX-2 leads to

Only COX-1 in platelets, GI
decrease sensitivity to
tract, kidneys
bradykinin, histamine
 • Aspirin– irreversibly inhibits COX-1 and -2
• Available strengths
• Low dose: 81 mg
• Regular strength: 325 mg
• Extra strength: 500 mg
• Maximum OTC daily dose: 4000 mg

Select • Adverse effects

• Gastrointestinal

NSAIDs • Local esophagitis/gastritis

• Systemic ulceration
• Hypersensitivity
• Reye’s Syndrome
• Vomiting and development of fatty liver with
encephalopathy
• Children and teens with viral illness
• Platelet inhibition
 Selected NSAIDs
Generic Name Brand name Usual Adult Dosing OTC? Notes
Diclofenac Voltaren 50 mg every 8 hours Rx
Etodolac Lodine 200 to 400 mg every 6 to 8 Rx
hours
Ibuprofen Motrin, Advil 200-400 mg every 4 to 6 OTC Adult dosing ≥ 12 years old
hours (OTC)
Up to 3200 mg in 3-4 divided
doses (Rx)
Naproxen Aleve 220 mg every 8 to 12 hours OTC Only for ≥ 12 years old
Ketorolac Toradol 10 mg every 4 to 6 hours Rx Limit 5 days of therapy
Celecoxib Celebrex 100 to 200 mg every 12 hours Rx COX-2 selective
Cardiac risk
 GI irritation and ulceration
• Risk factors: age > 60 years old,
h/o GI bleeding or ulceration,
higher doses, concomitant use of Bleeding
anticoagulant or corticosteroids

NSAID Adverse Acute kidney injury

Increased blood pressure,
Effects heart failure exacerbation

Use lowest dose possible

for shortest duration
possible
Acetaminophen (Tylenol)
• Mechanism: inhibits prostaglandin synthesis by
inhibiting COX in the CNS
• Antipyretic and analgesic
• No anti-inflammation
• Efficacy acetaminophen = efficacy of NSAID
• Adverse effects
• High doses/overdose hepatotoxicity
• Alcohol + acetaminophen = severe hepatic
necrosis
 Acetaminophen (Tylenol) Dosing
• Adult dosing (≥ 12 years old)
• Maximum daily dose is 4000 mg
• Extra strength 500 mg tablets: 2 tablets every 6 hours (max
of 6 in 24 hours)
• Regular strength 325 mg tablets: 2 tablets every 4 to 6
hours (max 10 in 24 hours)
• Arthritis strength 650 mg: 2 tablets every 8 hours (max 6 in
24 hours)
 Comparison of OTC Oral Analgesics
NSAID:
Aspirin Ibuprofen, APAP
Naproxen
Mild/moderate pain relief Mild/moderate pain relief Mild/moderate pain relief

Fever Fever Fever

High doses have anti- High doses have anti-

inflammatory effect inflammatory effect
No anti-inflammatory effect

Do not use in kids/teens Pediatric dosing available Pediatric dosing available

ADR: GI, platelet inhibition,

Reye’s Syndrome
ADR: GI, renal, CV ADR: hepatotoxicity

For treating mild/moderate pain, efficacy is similar between agents so think about safety when selecting a product
 • Prescription, controlled substances
• Opioids are agonists at the opioid
receptors in the CNS (and GI tract)
• Mu– clinical effects
• Kappa– some analgesic effect,
Opioids dysphoria
• Delta
• Used to relieve moderate to severe pain
• Efficacy: Codeine < Hydrocodone <
Oxycodone, Morphine
Opioids
Addiction– a primary, chronic, neurobiological disease, with genetic, psychosocial and
environment factors influencing its development and manifestations

Physical dependence– a state of adaptation that is manifested by a drug class where

withdrawal syndrome can be produced by abrupt cessation, rapid dose reduction

Tolerance– state of adaptation in which exposure to a drug induces changes that result
in a diminution of one of more of the drug’s effects over time

Withdrawal syndrome– non-life-threatening occurrence where abrupt cessation of

drug precipitates withdrawal symptoms
 Adverse Effects
• CNS
• Lethargy, apathy, sedation
• Psychomotor function impairment
• Confusion, disorientation, impaired judgement
• Euphoria
• Respiratory depression
• Direct effect on brainstem
• Constipation
• Mu receptors in colon are activated slowed GI transit/motility
• Increase fluid, fiber, stimulant laxative
 Adverse Effects
• Pruritis/urticaria
• Histamine release from mast cells
• More common with natural products (morphine)
• Cough
• Reflex is depressed!
• Can be used as cough suppressant
• Nausea, vomiting
• Miosis
• Vasodilation
Opioid Equivalencies
Opioid Withdrawal
• Duration and severity depend on
• Duration of action of drug used
• Degree of physical dependence
• Symptoms
• Sweating
• Nausea, vomiting, diarrhea
• Runny nose
• Irritability
• Tremor
• Cramps
• Anorexia
• Muscle spasm
Topical Agents
• Counterirritants
• Produce a mild pain/irritation to decrease perception of more intense pain
• Cooling, warmth, itching
• Uses– temporary relief of minor aches and pains
Counterirritant Sensation Comments
Methyl salicylate Rubefacient Most common ingredient
Warmth Very toxic if ingested
Used as flavoring oil in SMALL quantities
Menthol Cooling Feels cool initially followed by warmth
Caution– allergic reaction possible
Camphor Cooling Never used in kids less than 2 years old
Other Topical Agents
Trolamine salicylate

• Mechanism: analgesic effect due to salicylate absorption at site of application

• Odor free

Lidocaine

• Patch, cream
• Mechanism: topical anesthetic; desensitizes nerves
• Used for temporary relief of minor pain

Capsaicin

• Mechanism: depletes substance P at the area of application

• Requires regular application and chronic use for effectiveness
• Causes feelings of burning and warmth when first starting.
 Skeletal Muscle Relaxants
• Prescription only
• Indications: relieve tight muscles or spasms
• Adverse effects: sedation, dizziness, anticholinergic
• Avoid alcohol
• Cyclobenzaprine, orphenadrine worst anticholinergic effects
 Skeletal Muscle Relaxants
Generic Name Brand Name Dose Notes
Baclofen Lioresal, Ozobax 5 mg daily up to three times daily
(max 80 mg daily)
Carisoprodol Soma 250 To 350 mg three times a day Should only be used short term
and at bedtime (2-3 weeks), may need tapered
off
Cyclobenzaprine Flexeril 5-10 mg three times daily
Metaxalone Skelaxin 800 mg three to four times daily
Orphenadrine Norflex 100 mg twice daily
Tizanidine Zanaflex 2 mg once daily, may titrate up to Gradually taper to reduce risk of
36 mg/day divided rebound symptoms (HTN,
tachycardia)
Drug interaction: Ciprofloxacin
Corticosteroids
Indications
• Inflammation: very potent
anti-inflammatory agents
• Asthma
• Autoimmune conditions
• Adrenocortical insufficiency,
bone pain
Adverse effects
• Short term: hyperglycemia,
HTN, psych, sodium/water
retention, weight gain, ulcer
• Long term: osteoporosis, skin
thinning, buffalo hump, moon
face, immunosuppression,
growth suppression, cataracts
 • Monitoring
• Blood pressure, blood glucose
• Weight gain, edema
• Stomach pain/bleeding

Corticosteroids • Signs of infection

• Changes in mood/behavior, sleep
• Will need taper if used long term to prevent
adrenal suppression
• Nausea, vomiting, anorexia, headache,
lethargy, fever, muscle joint pain
Summary
• When selecting an agent to treat pain—
• What is the underlying cause/treat the source
• Inflammation
• Aches/pains
• Muscle spasms/tightness
• What safety concerns need addressed
• Use the lowest dose possible for the shortest duration appropriate
• Mild/moderate pain
• NSAIDs, APAP, topicals
• Moderate/severe pain
• Consider opioids +/- APAP short term
Cough, Cold
and Allergy
Cough, Cold and Allergies: Objectives
• For cough, cold, allergy explain:
• General therapeutic strategy
• Drug categories used for treatment
• Select an appropriate medication based on patient specific symptoms
• Discuss the difference between first- and second-generation
antihistamines
Common Cold
• Caused by a virus
• Rhinovirus most common cause
• Transmission
• Self-inoculation
• Inhalation of aerosolized particles
Symptom Comments
Scratchy/Sore throat Resolves quickly
Runny nose Nasal symptoms dominate by day 2-3 Usually BRIEF
Clear and runny secretions at first
Sneezing Variable
Nasal congestion Most bothersome complaint
Ocular Variable
Cough Infrequent- post nasal drip
Allergic Rhinitis
• Hypersensitivity reaction to allergen
• Seasonal and perennial allergies
• Histamine plays a major role in symptoms
• Sneezing, itching, runny nose
• Mucous production, nasal congestion
Cough, Cold and Allergy
• Treatment targeted toward symptoms
• Cough
• Cough suppressant
• Expectorant
• Nasal congestion
• Oral decongestant or nasal spray
• Allergies (runny nose, sneezing, itchy/watery eyes)
• Antihistamines
• Corticosteroid and anticholinergic nasal sprays
• Antihistamine and decongestant eye drops
• Be aware of combination products!
• Mechanism: block H1 receptors
• First-generation
• Lipophilic crosses blood Antihistamines
brain barrier leading to
sedation
• Second-generation
• Lipophobic CNS
penetration is minimal and
therefore nonsedating
Antihistamines
Allergy symptoms

• Eyes– itchy eyes, watery eyes

• Nasal symptoms– itchy nose, sneezing

Common cold symptoms

• Runny nose– first generation antihistamines might work

No decongestant activity
Antihistamine Adverse Effects

First generation
• Sedation and CNS depression
• Anticholinergic effects
• Dry mouth, eyes, nose
• Constipation
• Blurry vision
• Urinary retention

Second generation
• No (low) sedation, no CNS effects
• Dizziness, nausea, headache
 Antihistamines
Generation Generic Name Brand Name Sedation Anticholinergic Primary Use
1st Clemastine Tavist XXX XXX Allergy, common cold
1st Diphenhydramine Benadryl XXX XXX Allergy, insomnia, cough
1st Doxylamine In Nyquil; Unisom XXXX XXX Common cold, insomnia
1st Chlorpheniramine Chlortimeton XX XX Allergy, common cold
1st Brompheniramine Dimetapp XX XX Allergy, common cold
2nd Cetirizine Zyrtec X (low) Minimal Allergy
2nd Levocetirizine Xyzal X (low) Minimal Allergy
2nd Fexofenadine Allegra -- -- Allergy
2nd Loratadine Claritin -- -- Allergy
1st Dimenhydrinate Dramamine XXX XXX Motion sickness
1st Promethazine Phenergan XXX XXX Anti-emetic
1st Hydroxyzine HCl Atarax XXX XXX Allergy/itching
1st Hydroxyzine pamoate Vistaril XXX XXX Sedation/anxiety
1st Meclizine Antivert, Bonine XX XX Vertigo, motion sickness
 Decongestants
• Mechanism: alpha-adrenergic agonists vasoconstriction of peripheral blood vessels in
nasal passage, decreases mucosal edema
• Oral nasal decongestants
• Pseudoephedrine
• Behind the counter
• Phenylephrine
• Less effective?
• Issues: CV effects, CNS stimulation, HTN, urinary retention, heat intolerance
• Nasal Sprays/drops
• Oxymetazoline
• Phenylephrine
• Rebound congestion
• With proper use, topical drugs are minimally absorbed
Intranasal Corticosteroids
• Intranasal corticosteroids
• Nasal symptoms– itchy nose, runny nose, sneezing,
congestion
• Eye symptoms– itchy, watery eyes
• Should be used consistently
• May take 2-3 weeks to see full benefit
• Best benefit seen when used prior to exposure
• Adverse effects Examples:
• Sneezing Fluticasone propionate (Flonase)
• Cough Mometasone furoate (Nasonex)
• Sore throat Budesonide (Rhinocort)
Triamcinolone acetonide (Nasacort)
• Nasal irritation/bleeding
Cough
• Non-productive/dry
• Stimulated by mechanical irritant
• Doesn’t serve a purpose– can safely be suppressed
• Productive/wet
• Usually associated with underlying inflammatory process
• Serves a purpose– don’t want to suppress
• Selection of agent to help with cough depends on quality of cough
 • Increase effectiveness of cough by making
mucus thinner
• Appropriate use: ineffective productive cough
Expectorants • Water
• Guaifenesin
• Take with plenty of water
• Adverse effects: nausea, GI upset
 Antitussives
• Works in the CNS to increase cough threshold
• Appropriate use: dry cough, short term
• Codeine
• Dextromethorphan
• OTC
• Equipotent with codeine
• Non-narcotic, no addictive properties at normal dosing
• Toxicity– neurologic, CV effects; confusion, excitation, nervousness, irritability,
hallucinations
• Can be a drug of abuse
• Diphenhydramine (first generation antihistamine)
• Benzonatate (Tessalon)
Ophthalmic Symptoms
• Ocular inflammation often a component of allergic rhinitis
• Itching, watering, redness
• Systemic oral antihistamines and intranasal corticosteroids can help
• Ophthalmic products also available

Drug Class Generic Name Brand Name

Antihistamines Azelastine Optivar Rx/OTC
Olopatadine Patanol Rx/OTC
NSAID Ketorolac Acular Rx
Lubricants Artificial tears OTC
Decongestants* Naphazoline Naphcon A OTC
Oxymetazoline Visine LR OTC
Antibiotics

• Reminder: antibiotics are not effective for

common cold (virus) or allergic rhinitis
• Sinusitis
• Otitis media
• Strep throat
Summary
• Target the symptoms present
• Be aware of combination products
• Can be helpful
• Always keep in mind safety of medications
• Prevention of common cold and allergies
GI:
Constipation,
Diarrhea and
Heartburn
GI: Objectives
• Identify the laxatives that are relatively quick acting verses those that
take 24-72 hours to work
• Select an appropriate laxative given patient specific factors
• Determine appropriate duration of self-treatment for
constipation/diarrhea
 • General definition
• Difficult (or infrequent) evacuation of feces
• Subjective
• Etiology
• Anything that limits liquid content of feces
Constipation • Anything that interferes with or slows the
movement of feces through colon Anything
that inhibits or impairs defecation
• Lifestyle
• Medications
• OTC treatment appropriate for ~ one week
 Constipation
Class Mechanism Products Onset Notes
Bulk forming Hydrophilic, absorb Psyllium >72 hours Take with plenty of liquid at least 2 hours
water adds bulk Methylcellulose Not for acute before/after medications
to stook which Calcium constipation Contraindication: fluid restriction, bowel
naturally stimulates polycarbophil Can be used to obstruction, esophageal problems
peristalsis prevent constipation

Emollient Increase wetting Docusate Up to 72 hours Take with plenty of water

capacity of May be used for Do not use with mineral oil
intestinal fluid acute constipation
Stool softener
Lubricant Coats stool and Mineral oil ~6 to 8 hours Do not take at bedtime or lay down for 30-
“traps” water Onset is quick 60 minutes  risk of aspiration causing
lipid pneumonia
Contraindication: bedridden patients,
difficulty swallowing
 Constipation
Class Mechanism Products Onset Notes
Stimulant Increase propulsive Bisacodyl– oral and Very effective Senna often recommended long-
peristalsis of the colon rectal 6-12 hours (oral) term for patient on opiates
Senna– oral 15-60 minutes Contraindications: pregnancy,
(rectal) bowel obstruction
Hyperosmotic Draws water into Glycerin (rectal only) Glycerin: 15-60 Miralax approved for patients 17
intestines increased Polyethylene glycol minutes years and older
volume/pressure 3350 (Miralax) Miralax: 1-3 days Dose is 17 gm mixed with
distends bowel and water/juice
stimulates peristalsis
Saline Draws water into Magnesium hydroxide Quick onset: 30-60 Magnesium can be absorbed
intestines increased Magnesium citrate minutes systemically– caution in renal
volume/pressure impairment
distends bowel and
stimulates peristalsis
Diarrhea
• Definition: abnormal increase in liquidity of and/or frequency of bowel movements
• Acute < 14 days
• Some cases are ok for self-care
• Etiology
• Medication
• Food intolerance
• Protozoal diarrhea
• Viral and bacterial gastroenteritis
• Complications
• Fluid and electrolyte imbalance
• CV collapse, renal failure
 Diarrhea
• Goals: prevent or correct fluid and electrolyte disturbances
• Fluids
• Oral rehydration solutions
• Hypertonic liquids: Colas, ginger ale, fruit juice
• Sports drinks (make ½ strength) and consume other source of sodium
• Symptomatic relief
• May reduce diarrhea but won’t resolve/stop altogether
• Relieve some of the symptoms
Diarrhea

Loperamide

• Opiate agonist
• Effects: decreased fecal volume, increased stool viscosity, decreased fluid and electrolyte loss
• Dosing: 4 mg after first BM, then 2 mg after each loose stool (8 mg/day max)
• Do not use > 48 hours

Bismuth subsalicylate

• Salicylate has anti-secretory effects

• Bismuth has antimicrobial and toxin adsorbent properties
• Prevention of Traveler’s diarrhea
• Adverse effects: black/gray tongue and stool
Heartburn
Definition: warm or burning sensation in the chest which may spread to
the neck/throat and occasionally the back
• Episodic/intermittent: infrequent, occasional
• Frequent: ≥2 days per week

Exclusions to self-treatment
• Frequent heartburn lasting > 3 months
• Heartburn that continues after 2 weeks of treatment
• Difficulty/painful swallowing, chronic hoarseness/cough, chest pain, vomiting blood/black
tarry stooks, unexplained weight loss

Treatment
• Avoid triggers
• Avoid eating large meals, lying down after eating
• Elevate head of bed
• OTC drug therapy
Heartburn: Antacids
• Mechanism: partially neutralize gastric hydrochloric acid
• Quick onset, short duration of action
Ingredient ADR Comments
Calcium Carbonate May cause belching, flatulence 10% absorbed
May cause constipation Can be a calcium supplement
Magnesium hydroxide Dose dependent diarrhea 5-10% absorbed
Avoid in renal disease
Aluminum hydroxide Dose dependent constipation 15-30% absorbed
Avoid in renal disease
Sodium bicarbonate Bloating, belching, flatulence Most rapid acting, but not
High Na load commonly recommended

• To treat heartburn (infrequent, episodic)

Heartburn: H2 Receptor Antagonist
• Mechanism: reversibly bind to H2 receptor on parietal cells to
decrease secretion of gastric acid
• Slightly delayed onset, longer duration
• Used to treat and prevent heartburn (infrequent/episodic)
• Options:
• Famotidine
• Ranitidine
• Cimetidine– careful of drug interactions!
 Heartburn: Proton Pump Inhibitors

• Mechanism: irreversibly binds to the actively working H/K/ATPase proton

pump of the parietal cell
• Used for frequent heartburn (not lasting > 3 months)
• Does not provide immediate relief
• Treatment course 14 days
• Options:
• Omeprazole
• Lansoprazole
• Esomeprazole
• Pantoprazole (Rx only)
Introduction to
Pain,
Cough/Cold,
Allergy and GI
Abigail Geyer, PharmD
abigail.geyer@parkview.com
PGY1 Pharmacy Resident
Parkview Health │ Fort Wayne, IN