1

CHAPTER 18 Gastrointestinal System

Antihistamine
Use

Provides symptomatic
relief of allergic symptoms;
sedative/antiemetic in
surgery/labor; decreases
post op nausea/vomiting;
adjunct to analgesics
in control of pain;
management of
motion sickness.

Example

Promethazine
hydrochloride
(Phenergan)

How it works

Half-life:
715 h

Route:
PO/IM/
Rectal/IV

Onset:
PO: 20 min
IM: 20 min
Rectal: 20 min
IV: 35 min

Pregnancy
category: C

Peaks:
2h

Duration:
PO/IM
Rectal/IV:
28 h

Pharmacokinetic:
Well absorbed from GI tract,
after IM administration:
Widely distributed;
metabolized in liver;
excreted in urine;
PB:6090%.

Antihistamine: Inhibits histamine at histamine receptor sites,

preventing, antagonizing most allergic effects (e.g., urticaria,
pruritus).

Antiemetic: Diminishes vestibular stimulation, depresses

labyrinthine function, acts on chemoreceptor trigger zone
(CTZ), producing antiemetic effect.

Sedative-hypnotic: Decreases stimulation to brain stem reticular

formation producing CNS depression.
Adult dose

Allergic symptoms: PO: 25 mg at bedtime of 12.5 mg

4 times/day; Rectal/IM/IV: 25 mg; may repeat in 2 hours.

Motion sickness: PO: 25 mg 3060 minutes before departure;

may repeat in 812 h, then every morning on arising and before
evening meal.

Antiemetic: PO/IM/IV/Rectal: 12.525 mg q46 h as needed.

Pre- and postop sedation; adjunct to analgesics: IM/IV: 2550 mg.
Before administration

Assess BP and pulse for bradycardia/tachycardia if patient is

given parenteral form.

If used as an antiemetic assess for dehydration (poor skin

turgor, dry mucous membranes, longitudinal furrows in tongue).

Obtain baseline blood work to include electrolyte levels.

Assess medical and drug history.
If used for pre-op sedation, have patient void before
administering medication and raise side rails to provide a
safe environment.

Pharmacology Demystified

Antihistamine

(continued)

Administration

PO: Give without regard to meals.

Scored tablets may be crushed.
IM: Note: Significant tissue necrosis may occur if given SubQ.
Inadvertent intra-arterial injection may produce severe
arteriospasm, resulting in severe circulation impairment.
Inject deep IM.

IV: May be given undiluted or dilute with 0.9% NaCl.

Final dilution should not exceed 25 mg/mL.

Administer at 25 mg/min rate through IV infusion tube.

A too rapid rate of infusion may result in transient fall in B/P,
producing orthostatic hypotension, reflex tachycardia; if patient
complains of pain at IV site, stop injection immediately
(possibility of intra-arterial needle placement/perivascular
extravasation).

Rectal: Refrigerate suppository; moisten with cold water before

inserting well into rectum.
After administration

Contraindications

Monitor vital signs.

Monitor serum electrolytes in patients with severe vomiting.
Assist with ambulation if drowsiness, lightheadedness occurs.
Maintain a safe environment.

Comatose, those receiving large doses of other CNS

depressants, acutely ill/dehydrated children, acute asthmatic
attack, vomiting of unknown etiology in children, Reyes
syndrome, those receiving MAO inhibitors.

Extreme caution: History of sleep apnea, young children,

family history of sudden infant death syndrome (SIDS), those
difficult to arouse from sleep.

Cautions: Narrow-angle glaucoma, peptic ulcer, prostatic

hypertrophy, pylorduodenal/ bladder neck obstruction, asthma,
COPD, increased intraocular pressure, cardiovascular disease,
hyperthyroidism, hypertension, seizure disorders.

CHAPTER 18 Gastrointestinal System

Antihistamine (continued)
Side effects/
adverse reaction

High incidence: drowsiness, disorientation. Hypotension,

confusion, syncope more likely in the elderly.

Frequent: Dry mouth, urinary retention, thickening of bronchial

secretions.

Occasional: Epigastric distress, flushing, visual disturbances,

hearing disturbances, wheezing, paresthesia, sweating, chills.

Rare: Dizziness, urticaria, photosensitivity, nightmares.

Fixed-combination form with pseudoephedrine may produce
mild CNS stimulation.
Adverse/toxic:

Paradoxical reaction (particularly in children) manifested as

excitation, nervousness, tremors, hyperactive reflexes,
convulsions. CNS depression has occurred in infants and
young children (respiratory depression, sleep apnea, SIDS).
Long-term therapy may produce extrapyramidal symptoms
noted as dystonia (abnormal movements), pronounced motor
restlessness (most frequently occurs in children), and
Parkinsonian symptoms (esp. noted in elderly). Blood
dyscrasias, particularly agranulocytosis, have occurred.
Patient education

Drowsiness and dry mouth may be an expected response to

drug. Sugarless gum, sips of tepid water may relieve dry
mouth. Coffee/tea may help reduce drowsiness.

Report visual disturbances.

Avoid tasks that require alertness and motor skills until
response to drug is established.

Avoid alcohol and other CNS depressants.