Antihistamines, Decongestants, and Cough Drugs | MyMerci
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Antihistamines, Decongestants, and Cough Drugs

Unit 6 · Topic 29Antihistamines, Decongestants, and Cough Drugs
1.Mechanism of Action

Antihistamines (H₁-receptor antagonists) block histamine at H₁ receptors. This reduces itching, sneezing, watery rhinorrhea, hives, and capillary leakage. They work best when taken before allergen exposure because they prevent histamine effects rather than reverse them.

  • First-generation drugs cross the blood-brain barrier and also block muscarinic, alpha-adrenergic, and serotonin receptors → sedation and anticholinergic effects; some are used as antiemetics or sleep aids.
  • Second-generation drugs cross into the brain far less and are more selective → little sedation at usual doses.

Decongestants (alpha₁-adrenergic agonists) constrict dilated blood vessels in the nasal mucosa, shrinking swollen tissue and opening the nasal passages. Oral drugs act systemically; topical sprays act locally but cause rebound vasodilation when overused.

Cough drugs

  • Antitussives suppress the cough reflex: centrally (dextromethorphan; opioids such as codeine and hydrocodone act on the medullary cough center) or peripherally (benzonatate numbs stretch receptors in the lungs and airways).
  • Expectorants (guaifenesin) are thought to increase the volume and lower the thickness of airway secretions.
  • Mucolytics break down mucus: acetylcysteine and carbocisteine disrupt disulfide bonds in mucoproteins; dornase alfa breaks down DNA in purulent sputum (cystic fibrosis).

Epinephrine (adrenaline) — the drug for anaphylaxis — stimulates alpha₁ receptors (vasoconstriction, less airway edema, raised blood pressure), beta₁ receptors (stronger heartbeat), and beta₂ receptors (bronchodilation and reduced mediator release from mast cells). Antihistamines do none of these airway and circulation actions.

2.Indications & Key Drugs
Drug (generic)Key useKey point
Diphenhydramine — prototype first-generationAllergic reactions, itching, motion sickness, acute dystoniaSedating, anticholinergic; avoid in older adults
Chlorpheniramine, hydroxyzine, promethazineAllergy, itching (hydroxyzine), nausea (promethazine)Hydroxyzine prolongs QT and is contraindicated in early pregnancy; promethazine has boxed warnings
Cetirizine — prototype second-generation; levocetirizine, loratadine, desloratadine, fexofenadineAllergic rhinitis, chronic urticariaOnce daily; cetirizine sedates slightly more than the others
Azelastine (intranasal)Allergic rhinitisBitter taste, some drowsiness
Intranasal corticosteroids (fluticasone, mometasone, budesonide)Most effective treatment for persistent allergic rhinitisFull effect in days to weeks; aim away from the septum
Pseudoephedrine — prototype oral decongestantNasal and sinus congestionRaises BP and heart rate
Phenylephrine (oral and nasal)CongestionOral form is ineffective as a decongestant (FDA 2024 finding); nasal spray is effective
Oxymetazoline (nasal spray)Short-term congestion reliefMaximum 3 days — rebound congestion
DextromethorphanDry, nonproductive coughSerotonergic; misuse at high doses
Codeine, hydrocodone (in cough products)Severe dry cough (prescription)Opioid risks; US prescription cough products limited to adults 18 and older
BenzonatateDry coughSwallow whole; fatal in young children
GuaifenesinProductive cough with thick mucusDrink fluids
Acetylcysteine (inhaled), carbocisteine (oral)Thick secretionsInhaled acetylcysteine can cause bronchospasm; oral/IV acetylcysteine is the acetaminophen antidote
Dornase alfaCystic fibrosisNebulized daily
Epinephrine (adrenaline) IM auto-injector or 1 mg/mL ampule; epinephrine nasal sprayAnaphylaxis — first and only first-line drug0.01 mg/kg IM mid-outer thigh, max 0.5 mg adult (0.3 mg child); auto-injector 0.15 mg (about 15–30 kg) or 0.3 mg (30 kg or more)

Anaphylaxis order: IM epinephrine first → call for help → lie flat with legs raised (or sitting up if breathing is hard) → oxygen and IV fluids → adjuncts (inhaled albuterol for wheeze, H₁ antihistamine for itching and hives). Antihistamines and corticosteroids do not replace epinephrine and do not treat airway obstruction or shock.

3.Adverse Effects
ClassAdverse effects
First-generation antihistaminesDrowsiness, impaired driving, dizziness, anticholinergic effects (dry mouth, blurred vision, constipation, urinary retention, confusion, delirium in older adults), paradoxical excitation in young children, thickened secretions
PromethazineBoxed warnings: fatal respiratory depression in children under 2 years; severe tissue injury and gangrene with injection (extravasation or intra-arterial injection) — deep IM is the preferred route
HydroxyzineQT prolongation; sedation
Second-generation antihistaminesHeadache, mild sedation (cetirizine), dry mouth
Oral decongestantsHypertension, tachycardia, palpitations, insomnia, nervousness, urinary retention; rarely stroke or dysrhythmia
Topical decongestantsRebound congestion (rhinitis medicamentosa) after more than about 3 days, nasal burning
Intranasal corticosteroidsNosebleeds, nasal irritation; rarely septal perforation
DextromethorphanDizziness, nausea; serotonin syndrome with serotonergic drugs; high doses cause dissociation and psychosis (misuse)
Codeine/hydrocodoneSedation, constipation, respiratory depression; codeine — fatal in ultra-rapid CYP2D6 metabolizers (especially children)
BenzonatateSedation, dizziness; chewing or sucking the capsule numbs the mouth and throat → choking, laryngospasm; hypersensitivity
GuaifenesinNausea, vomiting
Inhaled acetylcysteineBronchospasm, sulfur ("rotten egg") odor, nausea, stomatitis, rhinorrhea
EpinephrineTachycardia, tremor, anxiety, pallor, headache, hypertension; inadvertent injection into a finger can cause ischemia
4.Contraindications, Cautions & Interactions
  • First-generation antihistamines: avoid in older adults (Beers Criteria — falls, confusion), narrow-angle glaucoma, prostatic hyperplasia/urinary retention; additive CNS depression with alcohol, opioids, benzodiazepines, and sleep aids; additive anticholinergic effects with tricyclics and oxybutynin.
  • Promethazine: contraindicated under 2 years; avoid IV use where possible and never give intra-arterially or subcutaneously.
  • Oral decongestants: avoid with uncontrolled hypertension, coronary artery disease, dysrhythmias, hyperthyroidism, narrow-angle glaucoma, prostatic hyperplasia; contraindicated with MAO inhibitors (and within 14 days of stopping) — hypertensive crisis. Caution with diabetes.
  • Dextromethorphan: avoid with MAO inhibitors; caution with SSRIs, SNRIs, linezolid (serotonin syndrome).
  • Codeine and tramadol: contraindicated in children under 12 and after tonsillectomy/adenoidectomy in those under 18; avoid in breastfeeding; do not combine with benzodiazepines or alcohol.
  • Benzonatate: not for children under 10 years; keep out of reach — accidental ingestion by young children has caused seizures, cardiac arrest, and death.
  • Children: over-the-counter cough and cold products should not be given to children under 2 years (FDA) and are labeled not for use under 4 years. Honey may ease cough in children over 1 year — never under 1 year (infant botulism).
  • Pregnancy and lactation: loratadine and cetirizine are preferred antihistamines; intranasal corticosteroids are acceptable. Avoid oral decongestants in the first trimester and in hypertension of pregnancy; pseudoephedrine can reduce breast-milk supply.
  • Epinephrine: no absolute contraindication in anaphylaxis; beta-blockers may blunt the response (glucagon may be used when epinephrine fails in a client taking beta-blockers).
  • Hidden duplicates: combination cold products often contain acetaminophen — count it toward the daily maximum (see Topic 31).
5.Monitoring & Nursing Interventions

Listed in priority order.

  1. Anaphylaxis is the priority — for hives with throat tightness, stridor, wheeze, hypotension, or vomiting after an exposure: give IM epinephrine into the mid-outer thigh without delay, call for help, position, give oxygen, and prepare IV fluids. Repeat epinephrine every 5–15 minutes if needed. Monitor for a biphasic reaction and observe as the protocol directs.
  2. Airway and secretions — assess cough: do not suppress a productive cough that clears secretions; antitussives are for a dry, exhausting cough. Encourage fluids (unless restricted) to thin mucus. Give a bronchodilator before inhaled acetylcysteine and have suction ready.
  3. Safety — assess sedation and fall risk after first-generation antihistamines; use bed alarms and assist with ambulation for older adults; check for urinary retention (bladder scan if the client cannot void).
  4. Cardiovascular — check blood pressure and heart rate before and during decongestant therapy, especially with hypertension or heart disease.
  5. Injection safety — promethazine: deep IM preferred; if IV is used, dilute and give slowly through a patent large vein; stop immediately if the client reports burning or pain at the site.
  6. Medication reconciliation — list all over-the-counter products; look for duplicate acetaminophen, antihistamines, or dextromethorphan and for MAO inhibitor use.
6.Client Education
  • Choose non-sedating antihistamines (loratadine, fexofenadine, cetirizine) for daytime use. With any sedating antihistamine, do not drive or operate machinery, and avoid alcohol.
  • Take antihistamines before allergen exposure; intranasal corticosteroids work best when used daily.
  • Nasal decongestant sprays: no more than 3 days to avoid rebound congestion.
  • Clients with high blood pressure, heart disease, glaucoma, or prostate enlargement should ask a pharmacist before using decongestants or first-generation antihistamines.
  • Read every label — many cold products combine acetaminophen, an antihistamine, a decongestant, and dextromethorphan. Use one product at a time.
  • Benzonatate: swallow capsules whole; store locked away from children.
  • Children: no over-the-counter cough and cold medicines under 2 years (and follow the label, which says under 4); use saline drops, suction, and fluids; honey only after the first birthday; no codeine under 12.
  • Seek care for cough lasting more than 3 weeks, bloody sputum, high fever, or breathlessness.
  • Epinephrine auto-injector: carry two at all times; inject into the outer thigh (through clothing if needed) and hold as the device instructs; call emergency services after use; a second dose may be given after 5–15 minutes if symptoms persist; lie down with legs raised rather than standing up suddenly; check expiration dates. Epinephrine nasal spray devices are used as labeled.
7.Toxicity, Overdose & Antidotes
ToxicityFindingsManagement
First-generation antihistamine overdose (diphenhydramine)Anticholinergic toxidrome: hot dry flushed skin, dilated pupils, tachycardia, urinary retention, absent bowel sounds, agitation, delirium, hallucinations; seizures; wide QRS and dysrhythmiasSupportive care, benzodiazepines for agitation and seizures, sodium bicarbonate for wide-QRS dysrhythmias; physostigmine only in selected cases under expert guidance
Decongestant overdoseSevere hypertension, tachycardia, agitation, seizures, strokeBenzodiazepines, cooling, antihypertensive therapy as directed
Dextromethorphan overdoseAgitation, hallucinations, ataxia, tachycardia, serotonin syndrome (hyperthermia, clonus)Supportive care, benzodiazepines, cooling; naloxone may partly help at very high doses
Codeine/hydrocodone overdosePinpoint pupils, sedation, respiratory depressionNaloxone (see Topic 30)
Benzonatate ingestion (child)Restlessness, tremor, seizures, dysrhythmias, cardiac arrest within about an hourEmergency care immediately; supportive and advanced life support
Epinephrine excessSevere hypertension, dysrhythmias, chest painStop; monitor; supportive care. A digital injection may need warm soaks or phentolamine per protocol
8.High-Yield Points
  • Anaphylaxis: IM epinephrine first, 0.01 mg/kg mid-outer thigh (max 0.5 mg adult, 0.3 mg child); antihistamines are adjuncts only
  • First-generation antihistamines: sedation + anticholinergic effects — avoid in older adults, glaucoma, prostatic hyperplasia
  • Second-generation antihistamines are preferred for daytime allergy relief
  • Intranasal corticosteroids are the most effective drugs for persistent allergic rhinitis
  • Oral decongestants raise BP and heart rate — never with MAO inhibitors
  • Topical decongestant sprays: maximum 3 days (rebound congestion)
  • Oral phenylephrine is not effective as a decongestant (FDA proposal to remove it)
  • Do not suppress a productive cough; antitussives for dry cough
  • Dextromethorphan + SSRI/MAOI → serotonin syndrome
  • Benzonatate: swallow whole; deadly to young children
  • No OTC cough and cold products under 2 years; no honey under 1 year; no codeine under 12
  • Inhaled acetylcysteine → bronchospasm; give a bronchodilator first

Country Notes

United States

  • Pseudoephedrine is sold behind the pharmacy counter with photo identification and monthly purchase limits under federal law (Combat Methamphetamine Epidemic Act of 2005) because it can be used to make methamphetamine.
  • In November 2024 the FDA proposed removing oral phenylephrine as an over-the-counter nasal decongestant because it does not work; products may remain on shelves until a final order takes effect, so counsel clients to choose other options.
  • Prescription opioid cough products are labeled for adults 18 years and older only.

Philippines

  • Lagundi (Vitex negundo) and carbocisteine are commonly used for cough; record herbal products in the medication history; they do not replace medical assessment for cough lasting more than 3 weeks — tuberculosis must be considered.
  • Oral phenylephrine remains in many cold combinations sold locally; its decongestant effect is doubtful — counsel accordingly.
  • Many antihistamine and cough-cold combinations are sold without prescription; ask specifically about combination products to prevent duplicate acetaminophen (paracetamol) and sedating antihistamine doses.

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