loperamide

Absorption: Not well absorbed following oral administration.

Distribution: Does not cross the blood-brain barrier.

Protein Binding: 97%.

Metabolism/Excretion: Metabolized partially by the liver, undergoes enterohepatic recirculation; 30% eliminated in the feces. Minimal excretion in the urine.

Half-Life: 10.8 hr.

Time/Action Profile ⬆ ⬇

(relief of diarrhea)

ROUTE	ONSET	PEAK	DURATION
PO	1 hr	2.5–5 hr	10 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Patients in whom constipation must be avoided;
Abdominal pain of unknown cause, especially if associated with fever;
Alcohol intolerance (liquid only).

Use Cautiously in:

Hepatic impairment;
OB: Safety not established in pregnancy;
Pedi: Children 2 yr (safety and effectiveness not established);
Geri: Older adults may have sensitivity to effects.

Adv. Reactions/Side Effects ⬆ ⬇

CV: CARDIAC ARREST, QT interval prolongation, syncope, TORSADES DE POINTES, VENTRICULAR ARRHYTHMIAS

GI: constipation, abdominal pain/distention/discomfort, dry mouth, nausea, vomiting

Neuro: drowsiness, dizziness

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)

Interactions ⬆ ⬇

Drug-drug:

↑CNS depression with other CNS depressants, including alcohol, antihistamines, opioid analgesics, and sedative/hypnotics.
↑anticholinergic properties with other drugs having anticholinergic properties, including antidepressants and antihistamines.
Concurrent use of cimetidine, clarithromycin, erythromycin, gemfibrozil, itraconazole, ketoconazole, quinidine, quinine, or ritonavir may ↑ levels and risk of cardiac arrhythmias.

Drug-Natural Products:

Kava-kava, valerian, skullcap, chamomile, or hops can ↑ CNS depression.

Route/Dosage ⬆ ⬇

Acute Diarrhea

PO (Adults and Children ≥12 yr): 4 mg initially, then 2 mg after each loose stool. Maintenance dose usually 4–8 mg/day in divided doses (not to exceed 8 mg/day for OTC use or 16 mg/day for Rx use).
PO (Children 9–11 yr or 30–47 kg): 2 mg initially, then 1 mg after each loose stool (not to exceed 6 mg/24 hr; OTC use should not exceed 2 days).
PO (Children 6–8 yr or 24–30 kg): 1 mg initially, then 1 mg after each loose stool (not to exceed 4 mg/24 hr; OTC use should not exceed 2 days).
PO (Children 2–5 yr or 13–20 kg): 1 mg initially, then 0.1 mg/kg after each loose stool (not to exceed 3 mg/24 hr; OTC use should not exceed 2 days).

Chronic Diarrhea

PO (Adults ): 4 mg initially, then 2 mg after each loose stool. Maintenance dose usually 4–8 mg/day in divided doses (not to exceed 16 mg/day for Rx use).
PO (Children ): 0.08–0.24 mg/kg/day divided 2–3 times/day (not to exceed 2 mg/dose).

Reduction of Ileostomy Output

PO (Adults ): 2 mg 2–3 times daily (tablets or capsules only); may ↑ dose in 2 mg/day increments if output remains elevated (not to exceed 16 mg/day for Rx use).

Availability ⬆ ⬇

(Generic available)

Tablets: 2 mg^OTC
Capsules: 2 mg
Oral liquidmint: 1 mg/7.5 mL^OTC
In combination with: simethicone (Imodium Multi-Symptom Relief), see Appendix [not included in this PDA edition]).

Assessment ⬆ ⬇

Assess frequency and consistency of stools and bowel sounds prior to and during therapy.
Assess fluid and electrolyte balance and skin turgor for dehydration.

Implementation ⬆ ⬇

PO: Administer with clear fluids to help prevent dehydration, which may accompany diarrhea.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication as directed. Do not take missed doses, and do not double doses. In acute diarrhea, medication may be ordered after each unformed stool. Advise patient not to exceed the maximum number of doses.
May cause drowsiness. Advise patient to avoid driving or other activities requiring alertness until response to drug is known.
Advise patient that frequent mouth rinses, good oral hygiene, and sugarless gum or candy may relieve dry mouth.
Caution patient to avoid using alcohol and other CNS depressants concurrently with this medication.
Instruct patient to notify health care professional if diarrhea persists or if fever, abdominal pain, or distention occurs.
Rep: Advise females of reproductive potential to notify health care professional if breastfeeding.

section name header

Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇