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What drug class are pseudoephedrine and phenylephrine (Sudafed, Sudafed PE)?
Systemic (oral) decongestants / sympathomimetics
What is the MOA of oral decongestants like pseudoephedrine/phenylephrine?
They stimulate alpha-adrenergic receptors (and have some beta-agonist effects) in the nose/sinuses, constricting blood vessels and decreasing sinusoidal vessel engorgement and mucosal edema
What symptom(s) are pseudoephedrine/phenylephrine used to treat?
Nasal/sinus congestion; also can help cough related to post-nasal drip and may help eustachian tube congestion
Why do pseudoephedrine and phenylephrine cause raised BP, tachycardia, and arrhythmias?
Because of systemic alpha and beta agonist stimulation (norepinephrine-like effects) - this causes essentially all of the side effects
Name the CNS-related side effects of oral decongestants.
Insomnia, anxiety, nervousness, restlessness, tremor, anorexia (from stimulation of CNS by crossing the blood-brain barrier)
Name the urinary/GU side effects of oral decongestants and why they occur.
Urinary retention and stimulation of urethra/prostate smooth muscle, due to alpha agonism
What is the onset of action for oral decongestants?
Within 30 minutes to 2 hours; available as short-acting and long-acting (12 hr, 24 hr) tablets
Why is pseudoephedrine kept behind the pharmacy counter?
Because it can be used to manufacture methamphetamine (abuse concern)
Is phenylephrine or pseudoephedrine more effective as an oral decongestant?
Pseudoephedrine is typically more effective than phenylephrine
What age is pseudoephedrine/phenylephrine approved for per the FDA, and what age do manufacturers voluntarily recommend?
FDA: 2 years and older; manufacturers voluntarily increased the age to 4+ due to risk of overdose and lack of efficacy data in younger children
Why should patients with hyperthyroidism use oral decongestants with caution?
Because the drugs are stimulating to the cardiovascular and central nervous systems
Why should patients with cardiac problems or uncontrolled hypertension avoid oral decongestants?
Due to cardiovascular stimulation (increased BP, HR, palpitations, arrhythmia risk) from the drug's CV stimulating effects
Why should patients with BPH/prostate enlargement avoid oral decongestants?
The drugs contract smooth muscle around the urethra (alpha agonism) and can further inhibit urination
Why should diabetic patients use oral decongestants with caution?
Potential for peripheral vasoconstriction
Why are older adults generally cautioned against oral decongestants?
They often have many of the disease states (cardiac, BPH, hyperthyroid, etc.) that make these drugs risky
What rare but serious eye emergency can oral decongestants cause?
Acute angle-closure crisis / closed-angle glaucoma (emergency vision loss) - very rare
Are oral decongestants (pseudoephedrine/phenylephrine) safe in pregnancy and lactation?
AVOID - potential for birth defects and decreased milk production
What drug class is pseudoephedrine/phenylephrine contraindicated with, and why is this notable?
Contraindicated with MAOIs (rarely used antidepressants)
What drug class are oxymetazoline, topical phenylephrine, and naphazoline (Afrin, Neo-Synephrine)?
Topical nasal decongestants
What is the MOA of topical nasal decongestants?
Stimulate alpha-adrenergic receptors in the nose/sinuses, constricting blood vessels and decreasing sinusoidal vessel engorgement and mucosal edema (same MOA as oral, but applied topically)
What symptom do topical nasal decongestants treat?
Nasal/sinus congestion
What is the onset of action for topical nasal decongestants?
Rapid - within minutes
Why are topical nasal decongestants preferred over oral decongestants in pregnancy, breastfeeding, heart disease, and BPH?
They lack significant systemic absorption/side effects, so they are safer for these conditions than oral decongestants
Which topical decongestant is the least systemically absorbed and is preferred, and how often is it dosed?
Oxymetazoline - preferred agent, long acting, dosed twice a day (other topical decongestants are dosed every 4-6 hours)
What condition can occur with topical nasal decongestant overuse beyond 3-7 days?
Rhinitis medicamentosa (rebound congestion from overuse/too-long duration)
What local side effects can topical nasal decongestants cause?
Dry nose, bleeding due to dryness, local irritation (sneezing/burning/stinging), and trauma from improper use
What patient counseling point is important for topical nasal decongestant sprays/bottles?
Viral contamination can occur if the product is shared - keep the bottle clean and use separate bottles for separate people
Are topical nasal decongestants safe in pregnancy and lactation?
Yes - safe
What drug class is nasal saline (Neilmed, Ayr, Ocean sprays)?
Moisturizer
What is the MOA of nasal saline?
Relieves nasal irritation and dryness; aids in removal of thick/dried mucus from the nose
What symptoms does nasal saline treat?
Nasal congestion and dryness; withdrawal from nasal decongestants
What side effects can nasal saline cause?
Runny nose, mild stinging/burning (more comfortable if warmed ~30 seconds)
What ages can nasal saline be used in, and is it safe in pregnancy/lactation?
OK to use in any age; safe in pregnancy and lactation
What is the maximum recommended frequency for nasal irrigation?
BID (twice daily)
Is nasal irrigation or nasal saline spray more effective, and who should avoid irrigation?
Nasal rinse/irrigation is more effective than saline spray or drops, but is not recommended in infants and children who cannot administer it themselves
What are the cons of nasal saline irrigation?
Can be uncomfortable, and requires boiled/distilled water
What drug class are menthol and camphor (Vicks, Mentholatum)?
Local anesthetic / topical antitussive
What is the general MOA of menthol?
Stimulates TRPM8 receptors, producing an anesthetic (cooling) sensation
What is the MOA of menthol lozenges for cough?
Lozenges decrease throat irritation and increase saliva, causing a reduction in cough reflex sensitivity
What is the MOA of menthol/camphor chest rub for nasal/chest congestion?
Vapors stimulate sensory nerve endings within the nose/chest mucosa, creating a local anesthetic sensation and a sense of improved airflow
What symptoms do menthol lozenges treat?
Cold sensation/numbness in mouth, sore throat (localized), and can help dry cough
What symptoms does menthol/camphor chest rub treat?
Nasal or chest congestion (rub), and dry cough (rub)
What side effects can menthol lozenges cause?
Bad taste from menthol, numb taste buds which can reduce taste of foods
What side effects can menthol/camphor chest rub cause?
Ointments are greasy; localized skin irritation may occur with topical products; can cause burns if heated/vaporized and gets on skin
Are menthol lozenges safe in pregnancy and breastfeeding?
Yes - menthol lozenges are considered safe
Is menthol/camphor chest rub recommended in pregnancy and breastfeeding, even though the reference book says camphor is compatible?
Not recommended - if absorbed systemically it crosses the placenta and the fetus cannot metabolize it; compatible with breastfeeding but not recommended due to close proximity to the breasts
Why is camphor especially dangerous if a child eats the chest rub ointment?
As little as 4 teaspoons of camphor-containing ointment can be deadly - it can cause overdose in children
What precaution should be taken when applying menthol/camphor rub to young children's feet?
Cover with socks so they don't accidentally eat it
What is a choking risk associated with menthol/camphor lozenges?
Choking risk in children under 4-6 years and sometimes older adults
What ages are menthol/camphor lozenges and ointment approved for?
Ointment: adults and children 2+; lozenges: adults and children 6+
What drug class is dextromethorphan (Robitussin, Delsym)?
Antitussive (cough suppressant) - nonopioid
What is the MOA of dextromethorphan?
A nonopioid that acts centrally in the medulla to increase the cough threshold
What is the MOA of codeine as an antitussive?
An opioid that acts centrally on the cough control center (medulla) to increase the cough threshold
What symptom does dextromethorphan/codeine treat?
Dry cough
What side effects are associated with dextromethorphan?
Stomach discomfort (from sugar content), drowsiness/CNS depression, and abuse potential ('robotripping' - euphoria, hallucinations)
What side effects are associated with codeine?
Euphoria/risk of addiction, nausea/vomiting, sedation, dizziness, constipation, and respiratory depression (in overdose)
Is dextromethorphan safe in kids, older adults, pregnancy, and lactation?
Yes - safe in kids and older adults, and safe in pregnancy and lactation
When should dextromethorphan NOT be used for cough?
Not for productive coughs, unless the patient cannot sleep or the cough is interfering with ADLs
What caution applies to dextromethorphan and alcohol/CNS depressants?
Can be abused and should not be used with alcohol or CNS depressants
What drug interaction is dextromethorphan contraindicated with?
Contraindicated with MAOIs (rarely used antidepressants) - a DDI risk
Is codeine safe in children, pregnancy, or breastfeeding?
AVOID - not to be used in kids, pregnancy, or breastfeeding mothers
What is the scheduling status of codeine, and is it available OTC?
Codeine is a CS-V (Controlled Substance V) and is OTC in certain states
What age is dextromethorphan approved for per FDA vs. manufacturer recommendation?
FDA: 2+ years; manufacturer: 4+ years
What is the max dextromethorphan dose for a child aged 4-6 years?
30 mg/day maximum
What is the max dextromethorphan dose for a child aged 6-12 years?
60 mg/day maximum
What is the max dextromethorphan dose for a patient over 12 years?
120 mg/day maximum
What is the minimum age for OTC codeine use?
Over 18 years of age
What drug class is diphenhydramine (Benadryl), chlorpheniramine, brompheniramine, and doxylamine?
Sedating / first-generation antihistamines
What is the general MOA of first-generation antihistamines?
Block histamine at central and peripheral histamine-1 (H1) receptor sites
What is the nasal-symptom MOA of first-generation antihistamines?
Act peripherally in the nose to dry up nasal secretions (anticholinergic effect)
What is the cough MOA of first-generation antihistamines?
Act centrally in the medulla to increase the cough threshold, AND decrease/dry up post-nasal drip peripherally to reduce cough
What is the insomnia/sedation MOA of first-generation antihistamines?
Cross the blood-brain barrier (BBB) to cause sedation
Why are second-generation antihistamines (Claritin, Zyrtec, Allegra) not effective for cough/cold?
They do not have the central/anticholinergic peripheral effects that first-generation antihistamines have
What symptoms do first-generation antihistamines treat in cough/cold?
Dry cough, rhinorrhea, and can help with sleep
List the anticholinergic side effects of diphenhydramine and what mnemonic-style effects they cause.
Dry eyes/blurred vision (no see), urinary retention/relaxes bladder muscle and can exacerbate BPH (no pee), dry mouth (no spit), constipation (no sh*t)
Why can diphenhydramine cause cognitive impairment in older adults?
It crosses the BBB and blocks necessary acetylcholine in the brain in older adults
What paradoxical reaction can occur in older adults and children under 6 with diphenhydramine?
Paradoxical reactions - excitability, restlessness, irritability (and rarely seizures in infants)
Are single-ingredient first-generation antihistamines safe in pregnancy?
Yes - single ingredient first-generation antihistamines are safe to use in pregnancy
Why should patients with BPH or difficulty urinating avoid diphenhydramine?
Anticholinergic effects relax the bladder muscle and can exacerbate BPH/urinary retention
Why should patients with closed-angle glaucoma avoid diphenhydramine?
Rare risk of causing acute angle-closure crisis
Why are all older adults cautioned regarding diphenhydramine (Beers List)?
It is on the Beers List due to anticholinergic burden, sedation, and cognitive impairment risk
Why should diphenhydramine not be combined with alcohol, other sedating drugs, or Alzheimer's medications?
It can increase sedation with alcohol/sedatives, and blocks the effects of Alzheimer's drugs via a pharmacodynamic drug interaction
Is diphenhydramine contraindicated in breastfeeding, and why?
Yes - contraindicated; can pass to the baby causing paradoxical effects/possible seizures, and can dry up breastmilk
What antidepressant class is diphenhydramine contraindicated with?
MAOIs (rarely used antidepressants)
What multi-ingredient product combines triprolidine and pseudoephedrine, and what is its age recommendation?
Actifed/Aprodine - approved 2+ per label but only recommended 6+ due to paradoxical reactions in children
What drug class is honey classified as for cough treatment?
Antitussive
What is the MOA of honey as a cough treatment?
Acts as a cough suppressant by coating the throat, decreasing irritation and reducing cough frequency; also has antimicrobial properties
What symptom does honey treat?
Dry cough
What side effects can honey cause?
Upset stomach or diarrhea from sugar content
What evidence supports honey's efficacy for cough?
Data supports honey as more effective than placebo (buckwheat honey formulation used in studies) and may be more effective than dextromethorphan
Is honey a good option for children under 6, and why?
Yes - may be a good alternative since data supports effectiveness in children ages 1-5 for treating nocturnal cough
What is the contraindication for honey, and why?
Avoid use in children under 1 year of age due to risk of botulism infection
Is honey safe in pregnancy and lactation?
Yes - safe
What drug class is guaifenesin (Mucinex, Robitussin)?
Protussive/expectorant
What is the MOA of guaifenesin for a productive ('chest congestion') cough?
Thins mucus and increases the volume of expectorated sputum
What is the MOA of guaifenesin for nasal congestion?
Thins nasal secretions
What type of cough is guaifenesin ineffective or minimally effective for?
Ineffective/minimally effective for a productive cough (despite being marketed as 'chest congestion' relief)
Where in the body does guaifenesin thin mucus?
Throughout the body - i.e., mucus in vaginal, nasal, and chest areas
What side effects can guaifenesin cause?
No major side effects; some patients may have GI side effects (nausea, diarrhea, stomach pain), which can be alleviated by taking with food
Why is guaifenesin considered a very safe OTC option?
No drug-drug interactions, can be used by almost all patients (healthy or with comorbidities), cannot overdose on it, and is safe in pregnancy and lactation