ANTIHISTAMINE

CETIRIZINE
(ce-tir'i-zeen)
Reactine , Zyrtec
Classifications: ANTIHISTAMINE; H1-RECEPTOR ANTAGONIST; NON-SEDATING
Prototype: Loratidine
Pregnancy Category: B

Availability
5 mg, 10 mg tablets; 5 mg, 10 mg chewable tablets; 5 mg/5 mL syrup

Actions
Cetirizine is a potent H1-receptor antagonist and thus an antihistamine without significant
anticholinergic or CNS activity. Low lipophilicity combined with its H1-receptor selectivity
probably accounts for its relative lack of anticholinergic and sedative properties.

Therapeutic Effects
Effectively treats allergic rhinitis, and chronic urticaria by eliminating or reducing the local and
systemic effects of histamine release.

Uses
Seasonal and perennial allergic rhinitis and chronic idiopathic urticaria.

Contraindications
Hypersensitivity to H1-receptor antihistamines; lactation, children <2 y.

Cautious Use
Moderate to severe renal impairment, pregnancy (category B), children.

Route & Dosage

Allergic Rhinitis
Adult: PO 5–10 mg once/d
Child: PO 2–5 y: 2.5 mg q.d. (max: 5 mg/d); 6 y: 5–10 mg q.d.

Chronic Urticaria
Adult: PO 10 mg q.d. or b.i.d.
Administration
Oral

 Consult physician about dosage if significant adverse effects appear. As elimination half-
life is prolonged in the older adult, dosage adjustments may be warranted.

Adverse Effects ( 1%)

GI: Constipation, diarrhea, dry mouth. CNS: Drowsiness, sedation, headache, depression.

Interactions
Drug: Theophylline may decrease cetirizine clearance leading to toxicity.

Pharmacokinetics
Absorption: Readily absorbed from GI tract. Peak: 1 h. Distribution: 93% protein bound;
minimal CNS concentrations. Metabolism: minimal. Elimination: 60% excreted unchanged in
urine within 24 h, 5% excreted in feces. Half-Life: 7.4 h.

Nursing Implications
Assessment & Drug Effects

 Monitor for drug interactions. As the drug is highly protein bound, the potential for
interactions with other protein-bound drugs exists.
 Monitor for sedation, especially the older adult.

Patient & Family Education

 Do not use in combination with OTC antihistamines.

 Do not engage in driving or other hazardous activities, before experiencing your
responses to the drug.
 Do not breast feed while taking this drug without consulting physician.

2.

FEXOFENADINE
(fex-o-fen'a-deen)
Allegra
Classifications: ANTIHISTAMINE; H1-RECEPTOR ANTAGONIST; NON-SEDATING
Prototype: Loratadine
Pregnancy Category: C

Availability
30 mg, 60 mg, 180 mg tablets; 60 mg capsules

Actions
Antihistamine competitively antagonizes histamine at the H1-receptor site; does not bind with
histamine to inactivate it. Not associated with anticholinergic or sedative properties.

Therapeutic Effects
Inhibits antigen-induced bronchospasm and histamine release from mast cells. Efficacy is
indicated by reduction of the following: nasal congestion and sneezing; watery or red eyes;
itching nose, palate, or eyes.

Uses
Relief of symptoms associated with seasonal allergic rhinitis, and chronic urticaria.

Contraindications
Hypersensitivity to fexofenadine; pregnancy (category C).

Cautious Use
Lactation; renal and hepatic insufficiency, hypertension, diabetes mellitus, ischemic heart
disease, increased ocular pressure, hyperthyroidism, renal impairment, or prostatic hypertrophy.
Safety and effectiveness in children <6 y are not established.

Route & Dosage

Allergic Rhinitis
Adult/Child: >12 y, PO 60 mg b.i.d.
Child: PO 6–11, 30 mg b.i.d.

Chronic Urticaria
Adult: PO 60 mg b.i.d.
Child: PO >6 y, 30 mg b.i.d.

Renal Impairment
Clcr <80 mL/min
Adult: PO 60 mg q.d.
Child: PO 30 mg q.d.

Administration
Oral

 Reduce starting dose for those with decreased kidney function.

 Do not give within 15 min of an aluminum- or magnesium-containing antacid.
 Store at 20°–25° C (68°–77° F). Protect from excess moisture.

Adverse Effects ( 1%)

CNS: Headache, drowsiness, fatigue. GI: Nausea, dyspepsia, throat irritation.

Interactions
Drug: ANTACIDS will decrease serum level of fexofenadine. Herbal: St. John's wort will
decrease serum level of fexofenadine.

Pharmacokinetics
Absorption: Rapidly absorbed from GI tract, 33% reaches systemic circulation. Onset: 1
h. Peak: 2–3 h. Duration: At least 12 h. Distribution: 60–70% bound to plasma
proteins. Metabolism: Only 5% of dose metabolized in liver. Elimination: 80% excreted in
urine, 11% in feces. Half-Life: 14.4 h.

Nursing Implications
Assessment & Drug Effects

 Monitor therapeutic effectiveness, which is indicated by decreased nasal congestion,

sneezing, watery or red eyes, and itching nose, palate, or eyes.

Patient & Family Education

 Note: Drug is well tolerated and causes minimal adverse effects.

 Do not breast feed while taking this drug without consulting physician.
3.

DIMENHYDRINATE
(dye-men-hye'dri-nate)
Apo-Dimenhydrinate , Calm-X, Dimenhydrinate
Injection, Dimentabs, Dinate, Dommanate, Dramanate, Dramamine, Dramilin, Dramocen,
Dramoject, Dymenate, Gravol , Hydrate, Marmine, Motion-Aid, Nauseatol
, Novodimenate , PMS Dimenhydrinate , Travamine , Travel Aid, Travel
Eze, Wehamine
Classifications: ANTIHISTAMINE (H1-RECEPTOR ANTAGONIST); ANTIEMETIC; ANTIVERTIGO
AGENT
Prototype: Diphenhydramine
Pregnancy Category: B

Availability
50 mg tablets; 50 mg/mL injection; 15.62 mg/5 mL, 12.5 mg/4 mL, 12.5 mg/5 mL liquid

Actions
H1-receptor antagonist and salt of diphenhydramine, with which it shares similar properties.

Therapeutic Effects
Precise mode of antinauseant action not known, but thought to involve ability to inhibit
cholinergic stimulation in vestibular and associated neural pathways.

Uses
Chiefly in prevention and treatment of motion sickness. Also has been used in management of
vertigo, nausea, and vomiting associated with radiation sickness, labyrinthitis, Ménière's
syndrome, stapedectomy, anesthesia, and various medications.

Contraindications
Narrow-angle glaucoma, prostatic hypertrophy. Safe use during pregnancy (category B),
lactation, or in children <2 y is not established.

Cautious Use
Convulsive disorders.

Route & Dosage

Motion Sickness
Adult: PO 50–100 mg q4–6h (max: 400 mg/24 h) IV/IM 50 mg as needed
Child: PO 2–6 y, up to 25 mg q6–8h (max: 75 mg/24 h); 6–12 y, 25–50 mg q6–8h (max:150
mg/24 h) IV/IM 2–6 y, 1.25 mg/kg q.i.d. up to 300 mg/d; 6–12 y, 1.25 mg/kg q.i.d. up to 300
mg/d

Administration
 Note: Give 30–60 min before treatment, then repeat 90 min after treatment, and again in
3 h to prevent radiation sickness.

Intramuscular

 Give undiluted and inject deep IM into a large muscle.

Intravenous

PREPARE: Direct: Dilute each 50 mg in 10 mL of NS.

ADMINISTER: Direct: Give each 50 mg or fraction thereof over 2 min.

INCOMPATIBILITIES Solution/additive: Aminophylline, amobarbital, butorphanol, chlorpr

omazine, glycopyrrolate, hydroxyzine, midazolam, pentobarbital,prochlorperazine, prom
azine, promethazine, thiopental.

 Store preferably at 15°–30° C (59°–86° F), unless otherwise directed by manufacturer.

 Examine parenteral preparation for particulate matter and discoloration. Do not use
unless absolutely clear.

Adverse Effects ( 1%)

CNS: Drowsiness, headache, incoordination, dizziness, blurred vision, nervousness,
restlessness, insomnia (especially children). CV: Hypotension, palpitation. GI: Dry mouth, nose,
throat; anorexia, constipation or diarrhea. Urogenital: Urinary frequency, dysuria.

Diagnostic Test Interference

Skin testing procedures should not be performed within 72 h after use of an antihistamine.

Interactions
Drug: Alcohol and other CNS DEPRESSANTS enhance CNS depression, drowsiness; TRICYCLIC
ANTIDEPRESSANTS compound anticholinergic effects.
Pharmacokinetics
Absorption: Readily absorbed from GI tract. Onset: 15–30 min PO; immediate IV; 20–30 min
IM. Duration: 3–6 h. Distribution: Distributed into breast milk. Elimination:Excreted in urine.

Nursing Implications
Assessment & Drug Effects

 Use side rails and supervise ambulation; drug produces high incidence of drowsiness.
 Note: Tolerance to CNS depressant effects usually occurs after a few days of drug
therapy; some decrease in antiemetic action may result with prolonged use.
 Monitor for dizziness, nausea, and vomiting; these may indicate drug toxicity.

Patient & Family Education

 Do not drive or engage in other potentially hazardous activities until response to drug is
known.
 Take 30 min before departure to prevent motion sickness; repeat before meals and upon
retiring.
 Do not breast feed while taking this drug without consulting physician.

4.

DESLORATADINE
(des-lor-a-ta'deen)
Clarinex, Clarinex Reditabs
Classifications: ANTIHISTAMINE, NON-SEDATING; H1-RECEPTOR ANTAGONIST
Prototype: Loratadine
Pregnancy Category: C

Availability
5 mg tablets; 2.5 mg, 5 mg orally dissolving tablets; 0.5 mg/mL syrup

Actions
A long-acting, nonsedating antihistamine with selective H1 receptor antagonist properties. The
drug reduces human mast cell release of the inflammatory cytokines. Therefore, it also exhibits
antiallergic effects.

Therapeutic Effects
It is more potent than loratadine as an antagonist at H1 receptors. Desloratadine is effective in
controlling allergic rhinitis and inhibiting histamine-induced wheals and flare (hives).

Uses
Treatment of seasonal or perennial allergic rhinitis and idiopathic urticaria.

Contraindications
Hypersensitivity to desloratadine or loratadine; neonates; pregnancy (category C); lactation.

Cautious Use
Renal and hepatic insufficiencies; bladder neck obstruction or urinary retention; prostatic
hypertrophy; glaucoma. Safety and efficacy in children <12 y not known.

Route & Dosage

Allergic Rhinitis, Idiopathic Urticaria

Adult: PO 5 mg q.d.

Renal Impairment
Adult:: PO Clcr <50 mL/min: 5 mg every other day

Hepatic Impairment
Adult: PO 5 mg every other day

Administration
Oral

 Note that drug should be given q.o.d. to patients with significant renal or hepatic
impairment.
 Store between 2°–25° C (36°–77° F).

Adverse Effects ( 1%)

Body as a Whole: Pharyngitis, fatigue, flu-like symptoms, myalgia. CNS: Somnolence,
dizziness. GI: Dry mouth, nausea, dry throat. Urogenital: Dysmenorrhea.

Interactions
Drug: No clinically significant interactions established.

Pharmacokinetics
Absorption: Well absorbed. Peak: 3 h. Distribution: 85–89% protein
bound. Metabolism: Extensively metabolized in liver to 3-hydroxydesloratadine, an active
metabolite. Elimination: Excreted equally in urine and feces. Half-Life: 27 h.

Nursing Implications
Assessment & Drug Effects

 Assess carefully for and report distressing or dangerous S&S that occur after initiation of
the drug. A variety of adverse effects, although not common, are possible. Some are an
indication to discontinue the drug.
 Monitor cardiovascular status and report significant changes in BP and palpitations or
tachycardia.
 Lab tests: Monitor periodically renal and liver function tests.
 Concurrent drugs: Monitor ECG when used in combination with any other drug that can
increase blood level of desloratidine in patients with preexisting cardiac disease.

5.

AZELASTINE HYDROCHLORIDE
(a-ze-las'teen)
Astelin, Optivar
Classifications: ANTIHISTAMINE; H1-RECEPTOR ANTAGONIST; OCULAR ANTIHISTAMINE
Prototype: Diphenhydramine
Pregnancy Category: C

Availability
137 mcg/spray nasal spray; 0.05% ophthalmic solution

Actions
First generation antihistamine that is a potent histamine H1 receptor antagonist.

Therapeutic Effects
Effective in the symptomatic treatment of seasonal allergic rhinitis and as a nasal decongestant.

Uses
Seasonal allergic rhinitis, itching associated with allergic conjunctivitis.

Contraindications
Hypersensitivity to azelastine; concurrent use of CNS depressants; pregnancy (category C),
lactation, children <3 y.

Cautious Use
Hepatic or renal disease; children <11 y; asthmatics.

Route & Dosage

Allergic Rhinitis
Adult: Intranasal 2 sprays per nostril b.i.d.
Child: Intranasal 5–11 y, 1 spray per nostril b.i.d.

Allergic Conjunctivitis
See Appendix A-1.

Administration
Intranasal

 Prime delivery unit before first use (see manufacturer's instructions).

 Instruct patient to clear nasal passages prior to drug installation; then tilt head forward
slightly and sniff gently when drug is sprayed into each nostril.
 Store the bottle upright at room temperature, 15°–30° C (59°–86° F).

Adverse Effects ( 1%)

Body as a Whole: Fatigue, dizziness. GI: Dry mouth, nausea. Metabolic: Weight
gain. CNS: Headache, somnolence. Respiratory: Pharyngitis, rhinitis, paroxysmal
sneezing, cough, asthma. Special Senses: Bitter taste, nasal burning, epistaxis, conjunctivitis.

Interactions
Drug: Alcohol and CNS DEPRESSANTS may cause reduced alertness.

Pharmacokinetics
Absorption: 40% absorbed from nasal inhalation. Peak: 2–3 h. Metabolism: Metabolized by
CYP450 to active metabolites. Elimination: Excreted primarily in feces. Half-Life: 22 h.
Nursing Implications
Assessment & Drug Effects

 Monitor level of alertness especially in older adults and with concurrent use of other CNS
depressants.

Patient & Family Education

 Follow manufacturer's directions for priming the metered dose spray unit before first use
and after storage of >3 d.
 Tilt head forward while instilling spray. Avoid getting spray in eyes.
 Do not drive or engage in potentially hazardous activities until response to drug is
known.
 Avoid concurrent use of CNS depressants, such as alcohol, while taking this drug.
 Discard spray unit and dispensing package bottle after 3 mo.
 Do not breast feed while using this drug.

ANTITUSSIVE

HYDROCODONE BITARTRATE
(hye-droe-koe'done)
Dihydrocodeinone Bitartrate, Hycodan, Robidone A, Vicodin (with acetaminophen)
Classifications: CENTRAL NERVOUS SYSTEM AGENT; NARCOTIC (OPIATE) AGONIST
ANALGESIC; ANTITUSSIVE
Prototype: Morphine
Pregnancy Category: C
Controlled Substance: Schedule III

Availability
5 mg hydrocodone usually with 500 mg or more acetaminophen

Actions
Morphine derivative similar to codeine but more addicting and with slightly greater antitussive
activity, and analgesic effect. CNS depressant with moderate to severe relief of pain. Available
in the United States only in combination with other drugs.

Therapeutic Effects
Suppresses cough reflex by direct action on cough center in medulla. CNS depressant with
moderate to severe relief of pain.
Uses
Symptomatic relief of hyperactive or nonproductive cough and for relief of moderate to
moderately severe pain. A common ingredient in a variety of proprietary mixtures.

Contraindications
Hypersensitivity to hydrocodone; lactation.

Cautious Use
Respiratory depression, asthma, emphysema; history of drug abuse or dependence; postoperative
patients; debilitated patients; children <1 y; pregnancy (category C); patients with preexisting
increased intracranial pressure.

Route & Dosage

Mild to Moderate Pain, Cough

Adult: PO 5–10 mg q4–6h prn (max: 15 mg/dose)
Child: PO 2–12 y, 1.25–5 mg q4–6h (max: 10 mg/dose)

Administration
Oral

 Give with food or milk to prevent GI irritation.

 Preserve in tight, light-resistant containers.

Adverse Effects ( 1%)

GI: Dry mouth, constipation, nausea, vomiting. CNS: Light-headedness, sedation,
dizziness, drowsiness, euphoria, dysphoria. Respiratory: Respiratory
depression. Skin: Urticaria, rash, pruritus.

Interactions
Drug: Alcohol and other CNS DEPRESSANTS compound sedation and CNS
depression. Herbal: St. John's wort increases sedation.

Pharmacokinetics
Onset: 10–20 min. Duration: 3–6 h. Distribution: Crosses placenta; distributed into breast
milk. Metabolism: Metabolized in liver. Elimination: Excreted in urine. Half-Life: 3.8 h.
Nursing Implications
Assessment & Drug Effects

 Monitor for effectiveness of drug for pain relief.

 Monitor for nausea and vomiting, especially in ambulatory patients.
 Monitor respiratory status and bowel elimination.

Patient & Family Education

 Avoid hazardous activities until response to drug is determined.

 Do not use alcohol or other CNS depressants; may cause additive CNS depression.
 Drink plenty of liquids for adequate hydration.
 Do not take larger doses than prescribed since abuse potential is high.
 Do not breast feed while taking this drug.

2.

GUAIFENESIN
(gwye-fen'e-sin)
Amonidrin, Anti-Tuss, Breonesin, Gee-Gee, GG-Cen, Glyceryl
Guaiacolate, Glycotuss, Glytuss, Guaituss, Hytuss, Malotuss, Mytussin, Mucinex, Nortussi
n, Resyl , Robitussin
Classifications: ANTITUSSIVE; EXPECTORANT
Pregnancy Category: C

Availability
100 mg/5 mL syrup; 100 mg/5 mL, 200 mg/5 mL liquid; 200 mg capsules; 300 mg sustained
release capsules; 100 mg, 200 mg, 1200 mg tablets; 600 mg sustained release tablets

Actions
Enhances reflex outflow of respiratory tract fluids by irritation of gastric mucosa.

Therapeutic Effects
Aids in expectoration by reducing adhesiveness and surface tension of secretions.

Uses
To combat dry, nonproductive cough associated with colds and bronchitis. A common ingredient
in cough mixtures.
Contraindications
Hypersensitivity to guaifenesin; pregnancy (category C), lactation.

Route & Dosage

Cough
Adult: PO 200–400 mg q4h up to 2.4 g/d
Child: PO <2 y: 12 mg/kg/d in 6 divided doses; 2–5 y: 50–100 mg q4h up to 600 mg/d; 6–11
y, 100–200 mg q4h up to 1.2 g/d

Administration
Oral

 Ensure that sustained release form of drug is not chewed or crushed. It must be
swallowed whole.
 Follow dose with a full glass of water if not contraindicated.
 Carefully observe maximum daily doses for adults and children.

Adverse Effects ( 1%)

GI: Low incidence of nausea. CNS: Drowsiness.

Diagnostic Test Interference

Guaifenesin may produce color interference with certain laboratory determinations of urinary 5-
hydroxyindoleacetic acid (5-HIAA) and vanillylmandelic acid (VMA).

Interactions
Drug: By inhibiting platelet function, guaifenesin may increase risk of hemorrhage in patients
receiving heparin therapy.

Pharmacokinetics
Not studied.

Nursing Implications
Assessment & Drug Effects
  Monitor for therapeutic effectiveness. Persistent cough may indicate a serious condition
requiring further diagnostic work.
 Notify physician if high fever, rash, or headaches develop.

Patient & Family Education

 Increase fluid intake to help loosen mucus; drink at least 8 glasses of fluid daily.
 Contact physician if cough persists beyond 1 wk.
 Contact physician if high fever, rash, or headache develops.
 Do not breast feed while taking this drug.

3.

DEXTROMETHORPHAN HYDROBROMIDE
(dex-troe-meth-or'fan)
Balminil DM , Benylin DM, Cremacoat 1, Delsym, DM Cough, Hold, Koffex
, Mediquell, Neo-DM , Ornex DM , Pedia Care, Pertussin 8 Hour Cough
Formula,Robidex , Robitussin DM, Romilar CF, Romilar Children's Cough, Sedatuss
, Sucrets Cough Control
Classifications: ANTITUSSIVE
Prototype: Benzonatate
Pregnancy Category: C

Availability
30 mg capsules; 2.5 mg, 5 mg, 7.5 mg, 15 mg lozenges; 10 mg/15 mL, 3.5 mg/5 mL, 7.5 mg/5
mL, 15 mg/5 mL liquid; 15 mg/15 mL, 10 mg/5 mL syrup

Actions
Nonnarcotic derivative of levorphanol. Chemically related to morphine but without central
hypnotic or analgesic effect or capacity to cause tolerance or addiction. Antitussive activity
comparable to that of codeine but is less likely than codeine to cause constipation, drowsiness, or
GI disturbances.

Therapeutic Effects
Controls cough spasms by depressing cough center in medulla. Temporarily relieves coughing
spasm.

Uses
Temporary relief of cough spasms in nonproductive coughs due to colds, pertussis, and
influenza.
Contraindications
Children <2 y, asthma, productive cough, persistent or chronic cough; hepatic function
impairment; pregnancy (category C).

Cautious Use
Chronic pulmonary disease; enlarged prostate; patients on MAO INHIBITORS.

Route & Dosage

Cough
Adult: PO 10–20 mg q4h or 30 mg q6–8h (max: 120 mg/d) or 60 mg of sustained action liquid
b.i.d.
Child: PO 2–6 y, 2.5–5 mg q4h or 7.5 mg q6–8h (max: 30 mg/d) or 15 mg sustained action
liquid b.i.d.; 6–12 y, 5–10 mg q4h or 15 mg q6–8h (max: 60 mg/d) or 30 mg sustained action
liquid b.i.d.

Administration
Oral

 Do not give lozenges to children <6 y.

 Ensure that extended release form of drug is not chewed or crushed. It MUST be
swallowed whole.
 Note: Although soothing local effect of the syrup may be enhanced if given undiluted,
depression of cough center depends only on systemic absorption of drug.

Adverse Effects ( 1%)

CNS: Dizziness, drowsiness, CNS depression with very large doses; excitability, especially in
children. GI: GI upset, constipation, abdominal discomfort.

Interactions
Drug: High risk of excitation, hypotension, and hyperpyrexia with MAO INHIBITORS.

Pharmacokinetics
Absorption: Readily absorbed from GI tract. Onset: 15–30 min. Duration: 3–6
h. Metabolism: Metabolized in liver. Elimination: Excreted in urine.

Nursing Implications
Assessment & Drug Effects

 Monitor for dizziness and drowsiness, especially when concurrent therapy with CNS
depressant is used.

Patient & Family Education

 Avoid irritants such as smoking, dust, fumes, and other air pollutants to lessen
unnecessary cough. Humidify ambient air to provide some relief.
 Note: Treatment aims to decrease the frequency and intensity of cough without
completely eliminating protective cough reflex.
 While dextromethorphan is available OTC, any cough persisting longer than 1 wk–10 d
needs to be medically diagnosed.

4.

BENZONATATE
(ben-zoe'na-tate)
Tessalon
Classifications: ANTITUSSIVE
Pregnancy Category: C

Availability
100 mg capsules

Actions
Nonnarcotic antitussive chemically related to tetracaine. Antitussive activity reported to be
somewhat less effective than that of codeine. Does not inhibit respiratory center at recommended
doses.

Therapeutic Effects
Decreases frequency and intensity of nonproductive cough.

Uses
Decreases frequency and intensity of nonproductive cough in acute and chronic respiratory
conditions. Also used in bronchoscopy, thoracentesis, and other procedures when coughing must
be avoided.

Contraindications
Safe use during pregnancy (category C) or lactation is not established.

Route & Dosage

Antitussive
Adult: PO 100 mg t.i.d. prn up to 600 mg/d
Child: PO <10 y, 8 mg/kg/d in 3–6 divided doses

Administration
Oral

 Ensure that soft capsules called perles are swallowed whole.

 Store in airtight containers protected from light.

Adverse Effects ( 1%)

Body as a Whole: Low incidence. CNS: Drowsiness, sedation headache, mild
dizziness. GI: Constipation, nausea. Skin: Rash, pruritus.

Pharmacokinetics
Onset: 15–20 min. Duration: 3–8 h.

Nursing Implications
Assessment & Drug Effects

 Auscultate lungs anteriorly and posteriorly at scheduled intervals.

 Observe character and frequency of coughing and volume and quality of sputum. Keep
physician informed.

Patient & Family Education

 Do not chew or allow perle to dissolve in mouth; swallow whole. If pedeyrle dissolves in
mouth, the mouth, tongue, and pharynx will be anesthetized. Also it is unpleasant to taste.
 Do not breast feed while taking this drug without consulting physician.

5.

CODEINE
(koe'deen)
CODEINE PHOSPHATE
Paveral
CODEINE SULFATE
Classifications: CENTRAL NERVOUS SYSTEM AGENT; NARCOTIC (OPIATE) AGONIST
ANALGESIC; ANTITUSSIVE
Prototype: Morphine
Pregnancy Category: C
Controlled Substance: Schedule II

Availability
15 mg, 30 mg, 60 mg tablets; 15 mg/5 mL oral solution; 30 mg, 60 mg injection

Actions
Opium derivative similar to morphine. In equianalgesic doses, parenteral codeine produces
degree of respiratory depression similar to that of morphine. In contrast to morphine, orally
administered codeine is about 60% as potent as the parenteral form. Histamine-releasing action
appears to be more potent than that of morphine and may result in hypotension, flushing, and
rarely bronchoconstriction.

Therapeutic Effects
Analgesic potency is about one-sixth that of morphine; antitussive activity is also a little less
than that of morphine.

Uses
Symptomatic relief of mild to moderately severe pain when control cannot be obtained by
nonnarcotic analgesics and to suppress hyperactive or nonproductive cough.

Contraindications
Hypersensitivity to codeine or other morphine derivatives; acute asthma, COPD; increased
intracranial pressure, head injury, acute alcoholism, hepatic or renal dysfunction,
hypothyroidism. Pregnancy (category C), lactation. Safe use in neonates not established.

Cautious Use
Prostatic hypertrophy, debilitated patients, very young and very old patients; history of drug
abuse.

Route & Dosage

Analgesic
Adult: PO/IM/SC 15–60 mg q.i.d.
Child: PO/IM/SC 0.5–1 mg/kg q4–6h prn (max: 60 mg/dose)

Antitussive
Adult: PO 10–20 mg q4–6h prn (max: 120 mg/24 h)
Child: PO 6–12 y: 5–10 mg q4–6h (max: 60 mg/24 h); 2–6 y: 2.5–5 mg q4–6h (max: 30 mg/24
h)

Administration
Oral

 Administer PO codeine with milk or other food to reduce possibility of GI distress.

Subcutaneous/Intramuscular

 Give parenterally to achieve greatest effectiveness. An oral dose is about 60% as

effective as an equal parenteral dose.
 Preserve in tight, light-resistant containers at 15°–30° C (59°–86° F) unless otherwise
directed.

Adverse Effects ( 1%)

Body as a Whole: Shortness of breath, anaphylactoid reaction. CV: Palpitation, hypotension,
orthostatic hypotension, bradycardia, tachycardia, circulatory
collapse. GI: Nausea,vomiting, constipation. CNS: Dizziness, light-headedness, drowsiness, seda
tion, lethargy, euphoria, agitation; restlessness, exhilaration, convulsions, narcosis, respiratory
depression. Skin: Diffuse erythema, rash, urticaria, pruritus, excessive perspiration, facial
flushing, fixed-drug eruption. Special Senses: Miosis. Urogenital: Urinary retention.

Interactions
Drug: Alcohol and other CNS DEPRESSANTS augment CNS depressant effects. Herbal: St.
John's wort may cause increase sedation.

Pharmacokinetics
Absorption: Readily absorbed from GI tract. Onset: 15–30 min. Peak: 1–1.5 h. Duration: 4–6
h. Distribution: Crosses placenta; distributed into breast milk. Metabolism:Metabolized in
liver. Elimination: Excreted in urine. Half-Life: 2.5–4 h.

Nursing Implications
Assessment & Drug Effects

 Record relief of pain and duration of analgesia.

 Evaluate effectiveness as cough suppressant. Treatment of cough is directed toward
decreasing frequency and intensity of cough without abolishing cough reflex, need to
remove bronchial secretions.
 Although codeine has less abuse liability than morphine, dependence is a major unwanted
effect.
 Supervision of ambulation and use other safety precautions as warranted since drug may
cause dizziness and light-headedness.
 Monitor for nausea, a common side effect. Report nausea accompanied by vomiting.
Change to another analgesic may be warranted.